Journal articles on the topic 'Eicosanoic acid Derivatives Physiological effect'
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1
Pope, Edward C., and Andrew F. Rowley. "The heart ofCiona intestinalis: eicosanoid-generating capacity and the effects of precursor fatty acids and eicosanoids on heart rate." Journal of Experimental Biology 205, no. 11 (June 1, 2002): 1577–83. http://dx.doi.org/10.1242/jeb.205.11.1577.
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SUMMARYEicosanoids are a group of oxygenated fatty-acid derivatives formed from C20 polyunsaturated fatty acids including arachidonic and eicosapentaenoic acids. In mammals, these compounds have been shown to be key molecules in several physiological processes including regulation of the vascular system. This study determined whether eicosanoids or their precursors are involved in the regulation of heart rate in the sea squirt Ciona intestinalis. Eicosanoid generation by both heart and blood cells was measured. The major lipoxygenase products formed were both derivatives of eicosapentaenoic acid,namely 8- and 12-hydroxyeicosapentaenoic acids (8-HEPE and 12-HEPE). Smaller amounts of 8,15-dihydroxyeicosapentaenoic acid (8,15-diHEPE) were also formed. The cyclo-oxygenase product prostaglandin E was also found in small amounts in the heart. Isolated hearts were exposed either to these fatty acid precursors or to 8-HEPE, 12-HEPE or prostaglandin E3, and the effect on heart rate was recorded. Both eicosapentaenoic and arachidonic acids stimulated the heart rate at concentrations between 50 and 200 μmoll-1. 12-HEPE(5 μmoll-1) and prostaglandin E3 (50μmoll-1) caused a modest increase in heart rate, while 8-HEPE had no significant effects at any of the time periods studied (≤180 min). Overall, the results show that arachidonic and eicosapentaenoic acids have limited effects on heart rate and only at concentrations unlikely to be routinely liberated in vivo. Similarly, the eicosanoids tested had a minor stimulatory activity on heart rate. The potential mechanisms for this stimulation are discussed. Overall, these results suggest that such compounds are of limited importance in regulating the heart and vascular system of sea squirts.
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Knight, John, Andrew F. Rowley, Mizue Yamazaki, and Anthony S. Clare. "Eicosanoids are modulators of larval settlement in the barnacle, Balanus amphitrite." Journal of the Marine Biological Association of the United Kingdom 80, no. 1 (February 1999): 113–17. http://dx.doi.org/10.1017/s0025315499001629.
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Eicosanoids are oxygenated derivatives of C20 polyunsaturated fatty acids known to play key roles in many physiological events in both invertebrates and vertebrates. The eicosanoid generating capacity of cypris larvae of the barnacle, Balanus amphitrite, was examined using enzyme immunoassay and high-performance liquid chromatography. These larvae generated the lipoxygenase products, 12-hydroxyeicosapentaenoic acid (HEPE), 8-HEPE and 8,15-diHEPE, together with the cyclooxygenase products, prostaglandin (PG) E, PGF and thromboxane (TX) B. Indomethacin, a selective cyclooxygenase inhibitor, caused a dose-dependent inhibition of PGE generation by B. amphitrite larvae, while esculetin and nordihydroguaiaretic acid (lipoxygenase inhibitors) also strongly inhibited the generation of 8-HEPE, 12-HEPE and 8,15-diHEPE. PGE2, PGE3 and 16,16-dimethyl PGE2 caused a dose-dependent inhibition of settlement of B. amphitrite larvae while indomethacin (25–100 μM) stimulated this process. Lipoxygenase products (8-HEPE, 12-HEPE and 8,15-diHEPE) as well as esculetin and nordihydroguaiaretic acid (10–100 μM) had no effect on the attachment of larvae.
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Calder, Philip C. "Eicosanoids." Essays in Biochemistry 64, no. 3 (August 18, 2020): 423–41. http://dx.doi.org/10.1042/ebc20190083.
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Abstract This article describes the pathways of eicosanoid synthesis, eicosanoid receptors, the action of eicosanoids in different physiological systems, the roles of eicosanoids in selected diseases, and the major inhibitors of eicosanoid synthesis and action. Eicosanoids are oxidised derivatives of 20-carbon polyunsaturated fatty acids (PUFAs) formed by the cyclooxygenase (COX), lipoxygenase (LOX) and cytochrome P450 (cytP450) pathways. Arachidonic acid (ARA) is the usual substrate for eicosanoid synthesis. The COX pathways form prostaglandins (PGs) and thromboxanes (TXs), the LOX pathways form leukotrienes (LTs) and lipoxins (LXs), and the cytP450 pathways form various epoxy, hydroxy and dihydroxy derivatives. Eicosanoids are highly bioactive acting on many cell types through cell membrane G-protein coupled receptors, although some eicosanoids are also ligands for nuclear receptors. Because they are rapidly catabolised, eicosanoids mainly act locally to the site of their production. Many eicosanoids have multiple, sometimes pleiotropic, effects on inflammation and immunity. The most widely studied is PGE2. Many eicosanoids have roles in the regulation of the vascular, renal, gastrointestinal and female reproductive systems. Despite their vital role in physiology, eicosanoids are often associated with disease, including inflammatory disease and cancer. Inhibitors have been developed that interfere with the synthesis or action of various eicosanoids and some of these are used in disease treatment, especially for inflammation.
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Rodríguez, María, Pilar G. Rebollar, Simona Mattioli, and Cesare Castellini. "n-3 PUFA Sources (Precursor/Products): A Review of Current Knowledge on Rabbit." Animals 9, no. 10 (October 15, 2019): 806. http://dx.doi.org/10.3390/ani9100806.
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This review compares the effects of different n-3 polyunsaturated fatty acid (PUFA) sources on biological activity, physiological/reproductive endpoints, and health implications with a special emphasis on a rabbit case study. Linoleic acid (LA) and α-linolenic acid (ALA) are members of two classes of PUFAs, namely the n-6 and n-3 series, which are required for normal human health. Both are considered precursors of a cascade of molecules (eicosanoids), which take part in many biological processes (inflammation, vasoconstriction/vasodilation, thromboregulation, etc.). However, their biological functions are opposite and are mainly related to the form (precursor or long-chain products) in which they were administered and to the enzyme–substrate preference. ALA is widely present in common vegetable oils and foods, marine algae, and natural herbs, whereas its long-chain PUFA derivatives are available mainly in fish and animal product origins. Recent studies have shown that the accumulation of n-3 PUFAs seems mostly to be tissue-dependent and acts in a tissue-selective manner. Furthermore, dietary n-3 PUFAs widely affect the lipid oxidation susceptibility of all tissues. In conclusion, sustainable sources of n-3 PUFAs are limited and exert a different effect about (1) the form in which they are administered, precursor or derivatives; (2) their antioxidant protections; and (3) the purpose to be achieved (health improvement, physiological and reproductive traits, metabolic pathways, etc.).
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Regulska, Magdalena, Magdalena Szuster-Głuszczak, Ewa Trojan, Monika Leśkiewicz, and Agnieszka Basta-Kaim. "The Emerging Role of the Double-Edged Impact of Arachidonic Acid- Derived Eicosanoids in the Neuroinflammatory Background of Depression." Current Neuropharmacology 19, no. 2 (December 31, 2020): 278–93. http://dx.doi.org/10.2174/1570159x18666200807144530.
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: Eicosanoids are arachidonic acid (AA) derivatives belonging to a family of lipid signalling mediators that are engaged in both physiological and pathological processes in the brain. Recently, their implication in the prolonged inflammatory response has become a focus of particular interest because, in contrast to acute inflammation, chronic inflammatory processes within the central nervous system (CNS) are crucial for the development of brain pathologies including depression. The synthesis of eicosanoids is catalysed primarily by cyclooxygenases (COX), which are involved in the production of pro-inflammatory AA metabolites, including prostaglandins and thromboxanes. Moreover, eicosanoid synthesis is catalysed by lipoxygenases (LOXs), which generate both leukotrienes and anti-inflammatory derivatives such as lipoxins. Thus, AA metabolites have double- edged pro-inflammatory and anti-inflammatory, pro-resolving properties, and an imbalance between these metabolites has been proposed as a contributor or even the basis for chronic neuroinflammatory effects. This review focuses on important evidence regarding eicosanoid-related pathways (with special emphasis on prostaglandins and lipoxins) that has added a new layer of complexity to the idea of targeting the double-edged AA-derivative pathways for therapeutic benefits in depression. We also sought to explore future research directions that can support a pro-resolving response to control the balance between eicosanoids and thus to reduce the chronic neuroinflammation that underlies at least a portion of depressive disorders.
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Drozd, Arleta, Dariusz Kotlęga, Przemysław Nowacki, Sylwester Ciećwież, Tomasz Trochanowski, and Małgorzata Szczuko. "Fatty Acid Levels and Their Inflammatory Metabolites Are Associated with the Nondipping Status and Risk of Obstructive Sleep Apnea Syndrome in Stroke Patients." Biomedicines 10, no. 9 (September 6, 2022): 2200. http://dx.doi.org/10.3390/biomedicines10092200.
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Background: This paper discusses the role of inflammation in the pathogenesis of nondipping blood pressure and its role in the pathogenesis of obstructive sleep apnea syndrome. The aim of the study was to assess the impact of free fatty acids (FAs) and their inflammatory metabolites on the nondipping phenomenon and the risk of sleep apnea in stroke patients. Methods: Sixty-four ischemic stroke patients were included in the prospective study. Group I consisted of 33 patients with a preserved physiological dipping effect (DIP), while group II included 31 patients with the nondipping phenomenon (NDIP). All subjects had FA gas chromatography and inflammatory metabolite measurements performed with the use of liquid chromatography, their 24 h blood pressure was recorded, and they were assessed with the Epworth sleepiness scale (ESS). Results: In the nondipping group a higher level of C16:0 palmitic acid was observed, while lower levels were observed in regard to C20:0 arachidic acid, C22:0 behenic acid and C24:1 nervonic acid. A decreased leukotriene B4 level was recorded in the nondipping group. None of the FAs and derivatives correlated with the ESS scale in the group of patients after stroke. Correlations were observed after dividing into the DIP and NDIP groups. In the DIP group, a higher score of ESS was correlated with numerous FAs and derivatives. Inflammation of a lower degree and a higher level of anti-inflammatory mediators from EPA and DHA acids favored the occurrence of the DIP. A high level of C18: 3n6 gamma linoleic acid indicating advanced inflammation, intensified the NDIP effect. Conclusions: We demonstrated potential novel associations between the FA levels and eicosanoids in the pathogenesis of the nondipping phenomenon. There are common connections between fatty acids, their metabolites, inflammation, obstructive sleep apnea syndrome and nondipping in stroke patients.
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Wang, Hongyu, Erdu Ren, Xiaoe Xiang, Yong Su, and Weiyun Zhu. "Dynamic Changes in Serum Metabolomic Profiles of Growing Pigs Induced by Intravenous Infusion of Sodium Butyrate." Metabolites 10, no. 1 (January 1, 2020): 20. http://dx.doi.org/10.3390/metabo10010020.
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This study aimed to explore the dynamic changes in metabolite profiles and metabolism pathways in the serum of growing pigs by intravenous infusion of sodium butyrate (SB). Fourteen crossbred growing barrows (BW = 23.70 ± 1.29 kg) fitted with jugular cannula were randomly allocated to the SB and control (Con) groups, each group consisted of seven replicates (pens), with one pig per pen. At 9:00 of each day during the experimental period, pigs in the SB group were infused with 10 mL of SB (200 mmol/L, pH 7.4, 37 °C) via precaval vein, while the Con group was treated with the same volume of physiological saline. On day 4, the blood of each pig was collected at 0, 30, 60, and 120 min after the intravenous infusion. Metabolites in the serum were detected by gas chromatograph-mass spectrometry analysis. Pathway analysis of metabolomic profiles showed that the differential metabolites mainly enriched in amino acid metabolism, lipid-related metabolism, and the tricarboxylic acid (TCA) cycle. More importantly, the relative concentrations of all eight essential amino acids, five non-essential amino acids, and two amino acid derivatives were decreased by the parenteral SB. In addition, SB significantly increased the relative concentrations of eicosanoic acid and octadecanoic acid and decreased the relative concentration of glycerol-3-phosphate at 0 min (three days after intravenous infusion of SB), which suggests that parenteral SB may increase stearates mobilization and decrease the biosynthesis of stearates. In conclusion, intravenous infusion of SB may induce more amino acids to synthesize proteins and affect fat metabolism through increasing fat mobilization and decreasing the biosynthesis of stearates. However, a further study is needed to understand the mechanism of extensive metabolic pathway changes induced by parenteral SB.
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Skrabka, Henryk, and Elżbieta Jaskulska. "An evaluation of the physiological activity of 9-amine-9-fluorenephosphonic acid derivatives." Acta Agrobotanica 40, no. 1-2 (2013): 53–57. http://dx.doi.org/10.5586/aa.1987.006.
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The physiological activity of eleven 9-amine-9-fluorenephosphonic acid derivatives, synthesized at the Wrocław Polytechnic, was examined. The test plant was <i>Spirodela oligorrhiza</i>. The effect of these compounds on the increase of the dry matter of this plant was tested in eight-day experiments. The activity of the compounds was varied. The most toxic were nos. 2, 4, 9, 8, 5 and 6 which were lethal in low concentrations. Somewhat less toxic were nos. 7, 10 and 11; nos. 1 and 3 were the least toxic.
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ROBINSON, Brenton S., Charles S. T. HII, and Antonio FERRANTE. "Activation of phospholipase A2 in human neutrophils by polyunsaturated fatty acids and its role in stimulation of superoxide production." Biochemical Journal 336, no. 3 (December 15, 1998): 611–17. http://dx.doi.org/10.1042/bj3360611.
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Although polyunsaturated fatty acids (PUFA) have been shown to stimulate neutrophil responses such as the oxygen-dependent respiratory burst (superoxide production), the mechanisms involved still remain undefined. Here we investigate the effect of PUFA on the phospholipase A2 (PLA2)-signal transduction process in human neutrophils. Exogenous eicosatetraenoic acid [arachidonic acid; C20:4(n-6)] or docosahexaenoic acid [C22:6(n-3)] promoted the release of [3H]C20:4(n-6) from prelabelled neutrophils in a time- and dose-dependent manner, which is indicative of PLA2 activation. The release of [3H]C20:4(n-6) from the cells by C20:4(n-6) and C22:6(n-3) was suppressed by PLA2 inhibitors. Other PUFA {eicosapentaenoic [C20:5(n-3)], octadecatrienoic [γ-linolenic; C18:3(n-6)] and octadecadienoic [linoleic; C18:2(n-6)] acids} also had the ability to release [3H]C20:4(n-6); however, certain C20:4(n-6) derivatives [15-hydroperoxyeicosatetraenoic acid, 15-hydroxyeicosatetraenoic acid and C20:4(n-6) methyl ester] and saturated fatty acids [octadecanoic (stearic; C18:0) and eicosanoic (arachidic; C20:0) acids] had no significant effect. Treatment of the neutrophils with exogenous C22:6(n-3) caused the mass of endogenous unesterified C20:4(n-6) to increase. Incubation of the leucocytes with C20:4(n-6) or C22:6(n-3) evoked activation of the 85 kDa cytosolic PLA2 (cPLA2) and the 14 kDa secretory PLA2 (sPLA2), but not the cytosolic Ca2+-independent PLA2. In contrast, C20:0 did not activate any of the PLA2 isoforms. Activation of cPLA2 by PUFA was found to precede that of sPLA2. C22:6(n-3), C20:4(n-6) and other PUFA induced punctate localization of cPLA2 in the cells, which was not observed with saturated fatty acids. Pretreatment of the leucocytes with PLA2 inhibitors markedly decreased superoxide production induced by C20:4(n-6). These results show that PUFA activate PLA2 in neutrophils, which might have a mandatory role in biological responses.
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Chen, Yo-Shen, and James L. Steele. "Genetic Characterization and Physiological Role of Endopeptidase O from Lactobacillus helveticus CNRZ32." Applied and Environmental Microbiology 64, no. 9 (September 1, 1998): 3411–15. http://dx.doi.org/10.1128/aem.64.9.3411-3415.1998.
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ABSTRACT A previously identified insert expressing an endopeptidase from aLactobacillus helveticus CNRZ32 genomic library was characterized. Nucleotide sequence analysis revealed an open reading frame of 1,941 bp encoding a putative protein of 71.2 kDa which contained a zinc-protease motif. Protein homology searches revealed that this enzyme has 40% similarity with endopeptidase O (PepO) fromLactococcus lactis P8-2-47. Northern hybridization revealed that pepO is monocistronic and is expressed throughout the growth phase. CNRZ32 derivatives lacking PepO activity were constructed via gene replacement. Enzyme assays revealed that the PepO mutant had significantly reduced endopeptidase activity when compared to CNRZ32 with two of the three substrates examined. Growth studies indicated that PepO has no detectable effect on growth rate or acid production by Lactobacillus helveticusCNRZ32 in amino acid defined or skim milk medium.
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Małodobra-Mazur, Małgorzata, Dominika Lewoń, Aneta Cierzniak, Marta Okulus, and Anna Gliszczyńska. "Phospholipid Derivatives of Cinnamic Acid Restore Insulin Sensitivity in Insulin Resistance in 3T3-L1 Adipocytes." Nutrients 13, no. 10 (October 15, 2021): 3619. http://dx.doi.org/10.3390/nu13103619.
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Background: Insulin resistance (IR) is a condition in which the physiological amount of insulin is insufficient to evoke a proper response of the cell, that is, glucose utilization. Metformin is the first choice for therapy, thanks to its glycemic efficacy and general tolerability. In addition, various natural compounds from plant extracts, spices, and essential oils have been shown to provide health benefits regarding insulin sensitivity. In the present study, we analyzed the effect of phospholipid derivatives of selected natural aromatic acids on insulin action and their potential use to overcome insulin resistance. Methods: The 3T3-L1 fibroblasts were differentiated into mature adipocytes; next, insulin resistance was induced by palmitic acid (16:0). Cells were further cultured with phenophospholipids at appropriate concentrations. To assess insulin sensitivity, we measured the insulin-stimulated glucose uptake, using a glucose uptake test. Results: We showed that cinnamic acid (CA) and 3-methoxycinnamic acid (3-OMe-CA) restored the proper insulin response. However, 1,2-dicinnamoyl-sn-glycero-3-phosphocholine (1,2-diCA-PC) and 1-cinnamoyl-2-palmitoyl-sn-glycero-3-phosphocholine (1-CA-2-PA-PC) improved insulin sensitivity in insulin-resistant adipocytes even stronger, exhibiting more beneficial effects. Conclusions: The binding of aromatic acids to phosphatidylcholine increases their beneficial effect on insulin sensitivity in adipocytes and expands their potential practical application as nutraceutical health-promoting agents.
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Mohapatra, N. K., P. W. Cheng, J. C. Parker, A. M. Paradiso, J. R. Yankaskas, R. C. Boucher, and T. F. Boat. "Sulfate concentrations and transport in human bronchial epithelial cells." American Journal of Physiology-Cell Physiology 264, no. 5 (May 1, 1993): C1231—C1237. http://dx.doi.org/10.1152/ajpcell.1993.264.5.c1231.
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Inorganic sulfate concentrations in the cytoplasm of human bronchial epithelial cells exceeded levels in the bathing medium under all circumstances tested. Cell sulfate concentrations were directly related to medium sulfate concentrations and inversely related to medium chloride concentrations. In physiological media there was a sulfate compartment of approximately 0.3 mM that exchanged very slowly with extracellular sulfate. In media lacking chloride, sulfate was accumulated by the cells to a level as high as 2 mM. Sulfate uptake was markedly inhibited by external chloride and by stilbene sulfonic acid derivatives but was not affected by sodium in the medium. Efflux of 35SO4(2-) was stimulated by both chloride and sulfate in the bathing medium but inhibited by stilbenes. The following compounds had no effect on sulfate movements: phorbol esters, adenosine 3',5'-cyclic monophosphate derivatives, and okadaic acid. Changes in medium tonicity were likewise without effect. Our results suggest that human bronchial epithelial cells maintain a steady-state disequilibrium for inorganic sulfate. Furthermore, sulfate appears to exist in at least two compartments in the cells: one that is slowly exchangeable with sulfate in the medium and another exchangeable compartment that is of negligible size in physiological media but that becomes very large in media lacking chloride. Sulfate is transported by an anion exchanger of broad specificity that is not influenced by substances known to modulate chloride channels.
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To, Huong Thi Mai, Nga T. P. Mai, Minh Anh Ngo, Ngan Huyen Nguyen, Kieu Thi Hanh, Thi Trang Nguyen, Hien Thi Thu Vu, et al. "Physiological and molecular comparative analysis of two contrasting rice varieties under jasmonic acid treatment." Vietnam Journal of Biotechnology 17, no. 4 (November 2, 2020): 663–72. http://dx.doi.org/10.15625/1811-4989/17/4/14428.
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Rice is one of the most important crops but its productivity is severely threatened by both biotic and abiotic stresses. Jasmonic acid and its derivatives (referred to JA) are the lipid-based plant hormones that were commonly known as regulators of plant growth, development and defense responses. In this study, we compare the physiological and molecular responses of two rice accessions, G38 (Nep_nuong) and G11 (Tam-tron) to JA treatment. G38 plants under JA treatment experienced a reduction in shoot length, root weight, shoot weight and total plant weight which suggested its sensitiveness to JA, whereas G11 plants showed a less reduction in these traits. The expression levels of 12 JA-related genes were investigated in order to better understand how the JA biosynthesis and responses differ in these two contrasting rice accessions. A significantly higher expression level of a set of genes related to JA biosynthesis, signaling and response in G11 compare to G38 was observed. Furthermore, the inorganic phosphorus starvation (Pi) response was also examined in the two varieties G11 and G38. In low Pi condition (40 µM), G11 plants showed more roots, longer root length and shoot length, higher weight compared to the G38 plants which suggest that G11 did not suffer much effect of Pi deficiency. This study highlights the differences in JA growth response in 2 contrasting rice genotypes and also suggests the link between JA developmental response and the tolerance to the Pi starvation condition in rice.
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Khusainova, G. H., T. A. Popova, M. V. Kustova, and O. V. Ostrovsky. "EFFECT OF GABA AND GLUTAMIC ACID DERIVATIVES ON THE FUNCTIONAL ACTIVITY OF LIVER CELLMITOCHONDRIA IN VITRO UNDER CONDITIONS OF OXIDATIVE STRESS." Journal of Volgograd State Medical University 19, no. 1 (March 31, 2022): 147–52. http://dx.doi.org/10.19163/1994-9480-2022-19-1-147-152.
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The aim of the study was to study the effect of GABA derivatives on the functional activity of intact and oxidative stress-damaged mitochondria. Isolated mitochondria were obtained by differential centrifugation. Oxidative damage was simulated by incubation with tert-Butylhydroperoxide (200 nmol/ml, 10 min). The studied substances (baclofen, mefebut, neuroglutam, RGPU-238 compound, salifen, tolibut, phenibut, phenotropil) were added to intact and damaged mitochondria (1×10-5 M per 100 µl, 10 min of incubation), the functional state of mitochondria was studied using a polarographic method. It was revealed that salifen and phenotropil had a pronounced protective effect on the respiratory complexes of the electron transport chain.
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Oliveira, Hélder, Patrícia Correia, Lucinda J. Bessa, Marta Guimarães, Paula Gameiro, Victor de Freitas, Nuno Mateus, Luís Cruz, and Iva Fernandes. "Cyanidin-3-glucoside Lipophilic Conjugates for Topical Application: Tuning the Antimicrobial Activities with Fatty Acid Chain Length." Processes 9, no. 2 (February 12, 2021): 340. http://dx.doi.org/10.3390/pr9020340.
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Background: Natural anthocyanins present a low solubility in lipophilic media, which compromises their effective application in lipophilic systems. In this work, cyanidin-3-O-glucoside (Cy3glc) was esterified by the addition of fatty acids with increasing chain-lengths and a structure-activity relationship was performed towards the description of the best analog for skin-care applications. Methods: By enzymatic hemi-synthesis, it was possible to obtain 5 structurally related derivatives of cyanidin-3-O-glucoside with successive C2 increments in the aliphatic chain. The stability in hanks buffer and DMEM with or without FBS was followed by HPLC. The cytotoxicity against keratinocytes was evaluated by MTT assay. The antioxidant capacity was determined by using the fluorescent probe DCF-DA. The effect on enzyme activity was evaluated towards tyrosinase, collagenase, and elastase enzymes by colorimetric assays. MIC and MBC values were obtained against reference strains and against multidrug-resistant isolates. Results: In physiological conditions, cy3glc−fatty acid derivatives are more stable and may be converted to the native anthocyanin. The 5 conjugates showed lower antioxidant capacity and enzymatic inhibitory activities in comparison to the anthocyanin precursor. However, concerning the antibacterial activity, the insertion of a fatty acid chain sprouted the antibacterial activity, showing a clear biphasic effect and a more effective effect on Gram-positive bacteria. Conclusions: Cy3glc-C10 was the most effective compound considering the antimicrobial activity, although a general reduction was observed among the other activities evaluated. This work prompt further assays with a different panoply of derivatives ranging other features including saturation vs. unsaturation, even vs. odd carbon content and linear vs. branched.
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Wu, Di, Mingjuan Gu, Zhuying Wei, Chunling Bai, Guanghua Su, Xuefei Liu, Yuefang Zhao, Lei Yang, and Guangpeng Li. "Myostatin Knockout Regulates Bile Acid Metabolism by Promoting Bile Acid Synthesis in Cattle." Animals 12, no. 2 (January 15, 2022): 205. http://dx.doi.org/10.3390/ani12020205.
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Myostatin (MSTN) is a major negative regulator of skeletal muscle mass and causes a variety of metabolic changes. However, the effect of MSTN knockout on bile acid metabolism has rarely been reported. In this study, the physiological and biochemical alterations of serum in MSTN+/− and wild type (WT) cattle were investigated. There were no significant changes in liver and kidney biochemical indexes. However, compared with the WT cattle, lactate dehydrogenase, total bile acid (TBA), cholesterol, and high-density lipoprotein (HDL) in the MSTN+/− cattle were significantly increased, and glucose, low-density lipoprotein (LDL), and triglycerides (TG) were significantly decreased, indicating that MSTN knockout affected glucose and lipid metabolism and total bile acids content. Targeted metabolomic analysis of the bile acids and their derivatives was performed on serum samples and found that bile acids were significantly increased in the MSTN+/− cattle compared with the WT cattle. As the only bile acid synthesis organ in the body, we performed metabolomic analysis on the liver to study the effect of MSTN knockout on hepatic metabolism. Metabolic pathway enrichment analysis of differential metabolites showed significant enrichment of the primary bile acid biosynthesis and bile secretion pathway in the MSTN+/− cattle. Targeted metabolomics data further showed that MSTN knockout significantly increased bile acid content in the liver, which may have resulted from enhanced bile acid synthesis due to the expression of bile acid synthesis genes, cholesterol 7 alpha-hydroxylase (CYP7A1) and sterol 27-hydroxylase (CYP27A1), and upregulation in the liver of the MSTN+/− cattle. These results indicate that MSTN knockout does not adversely affect bovine fitness but regulates bile acid metabolism via enhanced bile acid synthesis. This further suggests a role of MSTN in regulating metabolism.
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Delancey, Evan, Devin Allison, Hansa Raj KC, David F. Gilmore, Todd Fite, Alexei G. Basnakian, and Mohammad A. Alam. "Synthesis of 4,4′-(4-Formyl-1H-pyrazole-1,3-diyl)dibenzoic Acid Derivatives as Narrow Spectrum Antibiotics for the Potential Treatment of Acinetobacter Baumannii Infections." Antibiotics 9, no. 10 (September 28, 2020): 650. http://dx.doi.org/10.3390/antibiotics9100650.
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Acinetobacter baumannii has emerged as one of the most lethal drug-resistant bacteria in recent years. We report the synthesis and antimicrobial studies of 25 new pyrazole-derived hydrazones. Some of these molecules are potent and specific inhibitors of A. baumannii strains with a minimum inhibitory concentration (MIC) value as low as 0.78 µg/mL. These compounds are non-toxic to mammalian cell lines in in vitro studies. Furthermore, one of the potent molecules has been studied for possible in vivo toxicity in the mouse model and found to be non-toxic based on the effect on 14 physiological blood markers of organ injury.
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Khalaf, Reema Abu, Ghassan Abu Sheikha, Mahmoud Al-Sha'er, and Mutasem Taha. "Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors." Open Medicinal Chemistry Journal 7, no. 1 (November 29, 2013): 39–48. http://dx.doi.org/10.2174/1874104501307010039.
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As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.
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Shafiq, Shatha Ali, and Rasha Salam Sahib. "Antagonistic Activity of Agaricuscampestris mushroom Extracts Against some Human Pathogenic Bacterial Species." Asian Journal of Pharmaceutical Research and Development 10, no. 2 (April 15, 2022): 13–16. http://dx.doi.org/10.22270/ajprd.v10i2.1115.
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The present study focused on the evaluation of Agaricuscampestris mushroom extracts activity against four clinical isolates Escherichia coli; Pseudomonas aerginosa; Staphylococcus haemolyticus and Staphylococcus aureus. Agaricuscampestris mushroom extracts varied in their antimicrobial activity. The intensity of the antimicrobial effect is dependent upon the solvent , concentration of the mushroom extract and the organism being tested against .Therefore, The hot water and ethanolic extract 96%showed maximum inhibition at high concentrations specially at 500 mg/ml concentration( 17, 16, 19, 16 ) mm and ( 20,21,19,20) against E. coli , Pseudomonas aerginosa; Staphylococcus aureus and Staphylococcus haemolyticus respectively compared with methanolic extract . The ethyl acetate extract of the powder mushroom of Agaricuscampestris was analyzed to 9 chemical compounds belonged to fatty acids and their derivatives and included :-Nonadecane, Pentacosane, Octadecane, Heptadecane, Heneicosane, Hexadecane, 2,6,10,14-tetramethyl, Butanoic acid, 3,7-dimethyl-6-octenyl ester, Phthalic acid mono-2-ethylhexyl ester ,, Octanoic acid, heptadecyl ester.
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Srovnalova, Alzbeta, Sona Gurska, Milan Urban, Jan Sarek, Jiri Rehulka, Petr Dzubak, and Marian Hajduch. "Abstract 1530: Derivatives of betulinic acid act as modulators of the androgen receptor and report cytotoxicity towards cancer cell lines." Cancer Research 82, no. 12_Supplement (June 15, 2022): 1530. http://dx.doi.org/10.1158/1538-7445.am2022-1530.
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Abstract INTRODUCTION Triterpenoids are naturally occurring substances with a broad spectrum of beneficial effects for human health. Betulinic acid belongs to the group of pentacyclic triterpenoids and is well known for its antitumor activities. The library of about 1000 betulinic acid-derived triterpenes was collected and analyzed for cytotoxic activity on cancer and non-cancer cell lines (A549, CCRF-CEM, CEM-DNR, HCT116, K562, K562-TAX, U2OS, BJ and MRC-5) in our Institute over the last 20 years. Steroidal triterpenes are precursors of cholesterol, the precursor of testosterone, the fundamental ligand of the androgen receptor that is the key regulator in several physiological and pathological processes. Finding new modulators of androgen receptor is critical for the treatment of various androgen-dependent diseases, including prostate cancer or anabolic deficiencies. Betulinic acid and its derivatives showed structural similarity with steroids and therefore were selected to be tested for androgen receptor activity modulation. METHODS The stably transfected cell line HEK 293T GFP-AR was used to determine the translocation activity of the androgen receptor from the cytoplasm to the nucleus after the treatment with the derivatives. The high throughput fluorescent microscopy device and image analysis comprised the data, and compounds with the proved activity were selected for subsequent analysis. The luciferase reporter gene assay was further used to evaluate the effect of compounds on the transcriptional activity of the androgen receptor. The MTS assay was performed to assess the cytotoxicity. RESULTS Betulinic acid and its eight derivatives were identified to have 5-6 - fold higher translocation activity of AR (ratio cytoplasm GFP intensity/nuclear GFP intensity) than the negative control. Validation on luminescence luciferase reporter assay confirmed 4-5 - fold induction for five derivatives, whereas three derivatives were not active. Interestingly only two of them showed substantial cytotoxicities (IC50< 50 µM) as they possess significant inhibitory activity against all tested cancer cell lines with favorable therapeutic index against the non-cancer cell lines. CONCLUSION Derivatives of betulinic acid were proven to have modulatory activity on the androgen receptor pathway. The two derivatives of betulinic acid also displayed cytotoxicity towards almost all of the tested cancer cell lines. There could be not only AR modulation responsible for anticancer activity as the derivatives of betulinic acid are well know disruptors of mitochondrion functions as well. The synergy of these two mechanisms of action could potentiate the antitumor activity of the selected compounds. This work was supported by ENOCH CZ.02.1.01/0.0/0.0/16_019/0000868, CZ-OPENSCREEN - LM2018130, EATRIS-CZ - LM2018133. Citation Format: Alzbeta Srovnalova, Sona Gurska, Milan Urban, Jan Sarek, Jiri Rehulka, Petr Dzubak, Marian Hajduch. Derivatives of betulinic acid act as modulators of the androgen receptor and report cytotoxicity towards cancer cell lines [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2022; 2022 Apr 8-13. Philadelphia (PA): AACR; Cancer Res 2022;82(12_Suppl):Abstract nr 1530.
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Bian, Luyao, Huigang Sun, Ying Zhou, Yang Tao, and Chong Zhang. "Enhancement of Antioxidant Property of N-Carboxymethyl Chitosan and Its Application in Strawberry Preservation." Molecules 27, no. 23 (December 2, 2022): 8496. http://dx.doi.org/10.3390/molecules27238496.
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Bio-enzymatic grafting phenolic acid to chitosan derivative is an efficient and environmentally friendly molecular synthesis technology. In the present study, N-carboxymethyl chitosan (CMCS) was grafted with gallic acid (GA) using recombinant bacterial laccase from Streptomyces coelicolor as a catalyst. GA and CMCS were successfully grafted as determined by measuring amino acid content, Fourier transform infrared (FTIR) spectroscopy and ultraviolet-visible (UV-Vis) spectroscopy. Then, the effect of GA-g-CMCS coating on the freshness of strawberries at 20 ± 2 °C was explored. The physiological and biochemical quality indicators of strawberries during storage were monitored. The 1.5% GA-g-CMCS coating helped to protect the antioxidant properties and nutrients of strawberries and extend the shelf life. Specifically, it reduced the weight loss of strawberries during preservation (originally 12.7%) to 8.4%, maintained titratable acidity content (TA) residuals above 60% and reduced decay rate from 36.7% to 8.9%. As a bioactive compound, GA-g-CMCS has the potential to become an emerging food packing method. These results provide a theoretical basis and reference method for the subsequent synthesis and application of CMCS derivatives.
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Del Buono, Daniele, Francesca Luzi, and Debora Puglia. "Lignin Nanoparticles: A Promising Tool to Improve Maize Physiological, Biochemical, and Chemical Traits." Nanomaterials 11, no. 4 (March 26, 2021): 846. http://dx.doi.org/10.3390/nano11040846.
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Lignin, and its derivatives, are the subject of current research for the exciting properties shown by this biomass. Particularly attractive are lignin nanoparticles for their eco- and biocompatibility compared to other nanomaterials. In this context, the effect of nanostructured lignin microparticles (LNP), obtained from alkaline lignin by acid treatment, on maize plants was investigated. To this end, maize seeds were primed with LNP at five concentrations: 80 mg L−1 (T80), 312 mg L−1 (T312), 1250 mg L−1 (T1250), 5000 mg L−1 (T5000) and 20,000 mg L−1 (T20000). Concerning the dose applied, LNP prompted positive effects on the first stages of maize development (germination and radicle length). Furthermore, the study of plant growth, biochemical and chemical parameters on the developed plants indicated that concerning the dose applied. LNP stimulated beneficial effects on the seedlings (fresh weight and length of shoots and roots). Besides, specific treatments increased the content of chlorophyll (a and b), carotenoid, and anthocyanin. Finally, the soluble protein content showed a positive trend in response to specific dosages. These effects are significant, given the essential biological function performed by these biomolecules. In conclusion, this research indicates as the nanostructured lignin microparticles can be used, at appropriate dosages, to induce positive biological responses in maize. This beneficial action deserves attention as it candidates LNP for biostimulating a crop through seed priming.
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Avcu, Ferit, Burak Cem Soner, Oguzhan Yildiz, Kamile Ozturk, Pinar Elci, Meral Sarper, and Ali Ugur Ural. "EFFECTS of Zoledronic ACID On eNOS Exppression and Vascular Contractility IN Rat Aorta." Blood 116, no. 21 (November 19, 2010): 4318. http://dx.doi.org/10.1182/blood.v116.21.4318.4318.
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Abstract Abstract 4318 Zoledronic acid (ZOL) is a potent nitrogen-containing bisphosphonate used in the treatment of skeletal metabolic disorders and bone metastatic diseases. It has been shown that the nitrogenous bisphosphonates inhibits enzymes of mevalonate pathway. Similar with statin derivatives, ZOL affects the biological activity of geranyl-geranylated proteins in mevalonate pathway, as shown for the small GTPase RhoA. Although, beneficial effects of statin derivatives on vascular tissue have been reported, there is no study on effects and of ZOL on endothelial functions in vascular tissue and mechanisms of its action. It is important to elucidate the mechanism regulating NO production for endothelial cells to develop new therapeutic strategies for the treatment of impaired endothelial function associated with the vascular diseases. The aim of this study is to demonstrate the molecular mechanism of ZOL in the regulation of endothelial responses and eNOS expression in rat aorta. For his aim, potassium chloride and phenyleprine induced vasoconstriction was evaluated in endothelium intact and denuded isolated rat aorta preparations (n=6) after incubation with ZOL 100 μM and the results were compared with those without ZOL incubation. In addition, to evaluate endothelium dependent or independent effects of ZOL, vasodilator effects of acetylcholine and sodium nitroprussid were tested in the presence and absence of ZOL. To evaluate the influence of protein geranylation in effect of ZOL, contractile effect of phenylephrine vasocontractions was tested after incubation with ZOL in the presence of geranylgeranyl pyrophosphate and farnesyl pyrophosphate, important enzymes of mevolonate pathway. In addition, eNOS mRNA expressions were evaluated with RT-PCR in intact rat aorta or after incubation with ZOL. According to our results, incubation with ZOL decreased potassium chloride and phenylephrine-induced contractions significantly. This decrease was reversed NO-syntase inhibitor Nı,-nitro-L-arginine methyl esther (L-NAME) 0.1mM. Additionally, incubation with ZOL, increased endothelium-dependent acethycholine-induced relaxations and this effect of ZOL was inhibited by L-NAME. In rat aorta preparations incubated with ZOL, eNOS mRNA expression was increased significantly (1.52 fold) compared with control group. According to these results, we herein provide the first experimental evidence for the physiological role of ZOL in the regulation of eNOS expression and the contractility in the vascular tissues. This effect of ZOL is probably via its influence on RhoA. Since the restoration of NO bioactivity is a major target of present pharmacological and non-pharmacological treatments in cardiovascular medicine, further laboratory and clinical studies to explore the effect of ZOL on vascular endothelium may be helpful to demonstrate the possible benefits. Disclosures: No relevant conflicts of interest to declare.
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Thirunarayanan, Ganesamoorthy, and K. G. Sekar. "Spectral QSAR and QPR Study of some (<i>E</i>)-4-(((2-Hydroxy-6-(Substituted Phenyl)-1,6 Dihydropyrimidin-4-yl)Methyl)Diazenyl)Benzoic Acid Derivatives." International Letters of Chemistry, Physics and Astronomy 36 (July 15, 2014): 10–20. http://dx.doi.org/10.56431/p-l8rcqg.
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A series of titled compounds were synthesized and recorded the infrared and NMR spectra. The assigned spectral group frequencies were correlated with Hammett substituent constants, F and R parameter. From the statistical analysis results, the effect of substituents on the spectral group frequencies has been studied.
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Milanović, Žiko, Dušan Dimić, Milan Žižić, Dejan Milenković, Zoran Marković, and Edina Avdović. "Mechanism of Antiradical Activity of Newly Synthesized 4,7-Dihydroxycoumarin Derivatives-Experimental and Kinetic DFT Study." International Journal of Molecular Sciences 22, no. 24 (December 9, 2021): 13273. http://dx.doi.org/10.3390/ijms222413273.
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Coumarin derivatives have proven beneficial biological activities, but the mechanism of their radical scavenging potency is not fully understood. In this study, the antiradical capacity of two newly synthesized 4,7-dihydroxycoumarin derivatives: (E)-3-(1-((3-hydroxy-4-methoxyphenyl)amino)-ethylidene)-2,4-dioxochroman-7-yl acetate (A-3OH) and (E)-3-(1-((4-hydroxy-3-methoxyphenyl)amino)ethylidene)-2,4-dioxochroman-7-yl acetate (A-4OH) towards HO• were examined by Electron Paramagnetic Resonance (EPR) Spectroscopy and Density Functional Theory (DFT). The compounds were fully characterized by the elemental microanalysis, IR, and NMR spectroscopies. The effect of pH on the acid–base equilibria is separately discussed and the predominant species at the physiological pH were determined. Several common mechanisms (Hydrogen Atom Transfer (HAT), Single-Electron Transfer followed by Proton Transfer (SET-PT), Sequential Proton Loss followed by Electron Transfer (SPLET), Radical Adduct Formation (RAF), and Intramolecular Hydrogen Atom Abstraction (iHAA)) of radical scavenging were investigated based on thermodynamic and kinetic parameters. EPR results indicated that both compounds significantly reduce the amount of present HO•. The results of the kinetic DFT study demonstrated that both compounds predominantly exhibit antiradical capacity through HAT and SPLET mechanisms. The estimated overall rate constants (koverall) proved that A-4OH shows better antioxidant capacity than A-3OH which is well-correlated with the results obtained by EPR measurement.
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Zav’yalova, O. A., Yu A. Marsyanova, Yu V. Abalenikhinа, A. F. Ishtulin, and A. E. Gorelova. "The influence of metals of variable valence on the oxidative modification of albumin amino acid residues." NAUKA MOLODYKH (Eruditio Juvenium) 9, no. 3 (September 30, 2021): 369–76. http://dx.doi.org/10.23888/hmj202193369-376.
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BACKGROUND: The constancy of the protein composition of the body is one of the most important conditions for normal vital activity. Deviations in the content of the main bioelements, in particular, mixed valence metals, caused by environmental factors, improper nutrition and other factors, lead to various disorders. One of the properties of metals of mixed valence is the abil-ity to cause metal-catalyzed oxidation of proteins in joint action with active forms of oxygen. It seems interesting to study the oxidative modification of the amino acid residues of albumin and the change in its properties. AIM: To study the effect of reactive oxygen intermediates generated by the Fenton reaction in the presence of Fe2+ and Cu2+ on the oxidative modification of amino acid residues of bovine serum albumin. MATERIALS AND METHODS: The study was carried out on bovine serum albumin (BSA), which was incubated for 2 hours in a mixture of Fenton's reagents – FeSO4 + H2O2 and in a mixture of СuSO4 + H2O2. The quantitative protein content in the samples was determined with the bromcresol green reagent (Albumin-Olvex). The content of carbonyl derivatives of proteins was estimated by the method of R.L. Levine modified by E.E. Dubinina. The content of thiol groups in albumin samples from the control and experimental groups was determined by the Ellman method with DTNB (under non-denaturing conditions. RESULTS: The presented results demonstrate that under the action of Cu2+ ions, the formation of carbonyl derivatives of aliphatic amino acids of albumin is less than in the presence of Fe2+, which can be explained by the different degrees of albumin affinity to metals of variable valence. The rate of mobility of oxidatively modified albumin in polyacrylamide gel decreases, which is explained by protein aggregation due to bityrosine cross-links. CONCLUSION: Variable valence metals affect the modification of albumin. The change in the functional properties of the protein is of physiological significance, including the case of extracellular mobilization of iron and copper.
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Lin, Jingjing, Mei Tang, Ru Zhao, Qianqian Du, Longying Shen, Guohua Du, Yafen Zhang, Yan Li, and Xiandao Pan. "Synthetic Optimization of Ellipticine and Antitumor Activity of Novel Hexacyclic Derivatives of Ellipticine." Current Pharmaceutical Design 25, no. 33 (November 19, 2019): 3578–89. http://dx.doi.org/10.2174/1381612825666190404122650.
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Background: For decades, a great deal of research work has been done to synthesize ellipticine and its derivatives because of their potential antitumor properties and anti-HIV activities. However, the resonance structures in different media, a low level of solubility at physiological pH and systemic toxicity have prevented the use of ellipticine as a therapeutic agent. Besides, the low yield and complex steps of ellipticine synthesis limit its application. Methods: A high-yield synthetic procedure of ellipticine has been optimized, and the total yield was up to 50% without silica gel column chromatography. Novel hexacyclic ellipticine derivatives were synthesized by coupling ellipticine with o-aminobenzoic acid. Their cytotoxicities against HCT116, MGC803, HT29 and MCF-7 tumor cells were evaluated. Results: The synthesis process of ellipticine was optimized, and the total yield of the synthetic route was increased to 50% through several operation steps optimization. Fourteen ellipticine hexacyclic derivatives were synthesized. The synthetic compounds were screened for anti-tumor activity in vivo and in vitro, and some of the derivatives had good anti-tumor activity. Conclusion: Compared with ellipticine, the compound 1l showed higher antitumor activity and better tolerance to tumor models. The compound 1l treatment increased the percentage of late apoptotic cells from 3.1% (DMSO) to 21.6% (20.0 μM) in NCI-H460 cells. It also was observed the effect of 1l on G2 phase arrest was similar as that of ellipticine. The mechanism of action indicated compound 1l could be a topoisomerase IIα poison. These studies provided the basis for the pharmacodynamics and toxicology of ellipticine, and further clarifies the structureactivity relationship of antitumor activity of ellipticine.
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Borrego-Muñoz, Paola, Diego Cardenas, Felipe Ospina, Ericsson Coy-Barrera, and Diego Quiroga. "Second-Generation Enamine-Type Schiff Bases as 2-Amino Acid-Derived Antifungals against Fusarium oxysporum: Microwave-Assisted Synthesis, In Vitro Activity, 3D-QSAR, and In Vivo Effect." Journal of Fungi 9, no. 1 (January 13, 2023): 113. http://dx.doi.org/10.3390/jof9010113.
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In this manuscript, the synthesis of enamine-type Schiff bases 1–48 derived from the amino acids L-Ala, L-Tyr, and L-Phe was carried out. Their in vitro activity and in vivo protective effect against Fusarium oxysporum were also evaluated through mycelial growth inhibition and disease severity reduction under greenhouse conditions. The in vitro activity of test compounds 1–48 showed half-maximal inhibitory concentrations (IC50) at different levels below the 40 mM range. Deep analysis of the IC50 variations indicated that the size of the substituent on the acetylacetone derivatives and the electronic character on the cyclohexane-3-one fragment influenced the antifungal effect. 3D-QSAR models based on atoms (atom-based approach) were built to establish the structure–activity relationship of the test Schiff bases, showing a good correlation and predictive consistency (R2 > 0.70 and Q2 > 0.60). The respective contour analysis also provided information about the structural requirements for potentiating their antifungal activity. In particular, the amino acid-related fragment and the alkyl ester residue can favor hydrophobic interactions. In contrast, the nitrogen atoms and enamine substituent are favorable regions as H-donating and electron-withdrawing moieties. The most active compounds (40 and 41) protected cape gooseberry plants against F. oxysporum infection (disease severity index < 2), involving adequate physiological parameters (stomatal conductance > 150 mmol/m2s) after 45 days of inoculation. These promising results will allow the design of novel Schiff base-inspired antifungals using 2-amino acids as precursors.
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Gémes, Borbála, Eszter Takács, Inna Székács, Robert Horvath, and András Székács. "Comparative Assessment of the Inhibitory Potential of the Herbicide Glyphosate and Its Structural Analogs on RGD-Specific Integrins Using Enzyme-Linked Immunosorbent Assays." International Journal of Molecular Sciences 23, no. 20 (October 17, 2022): 12425. http://dx.doi.org/10.3390/ijms232012425.
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Transmembrane glycoprotein integrins play crucial roles in biochemical processes, and by their inhibition or activation, different signal pathways can be disrupted, leading to abnormal physiological functions. We have previously demonstrated the inhibitory effect of glyphosate herbicide’s active ingredient on cell adhesion and its αvβ3 integrin antagonist effect. Therefore, it appeared particularly exciting to investigate inhibition of glyphosate and its metabolites on a wider range of Arg-Gly-Asp (RGD) binding integrins, namely αvβ3, α5β1 and αllbβ3. Thus, the purpose of this study was to assess how extended the inhibitory effect observed for glyphosate on the integrin αvβ3 is in terms of other RGD integrins and other structurally or metabolically related derivatives of glyphosate. Five different experimental setups using enzyme-linked immunosorbent assays were applied: (i) αvβ3 binding to a synthetic polymer containing RGD; (ii) αvβ3 binding to its extracellular matrix (ECM) protein, vitronectin; (iii) α5β1 binding to the above polymer containing RGD; (iv) αllbβ3 binding to its ECM protein, fibrinogen and (v) αvβ3 binding to the SARS-CoV-2 spike protein receptor binding domain. Total inhibition of αvβ3 binding to RGD was detected for glyphosate and its main metabolite, aminomethylphosphonic acid (AMPA), as well as for acetylglycine on α5β1 binding to RGD.
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Suresh, Reshma, Perayil Jayachandran, Angel Fenol, Raja Biswas, Sajitha Krishnan, K. Aswini Kumar, Darshan Devang Divakar, and Sajith Vellappally. "Effect of Non-Surgical Periodontal Therapy on the Serum Sialic Acid Levels in Diabetic Patients with Periodontitis." Acta Medica (Hradec Kralove, Czech Republic) 62, no. 3 (2019): 109–16. http://dx.doi.org/10.14712/18059694.2019.134.
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Sialic acid (SA), a family of acetylated derivatives of neuraminic acid, an acute phase reactant by itself. It usually occurs as a terminal component at the non-reducing end of carbohydrate chains of glycoproteins and glycolipids. SA participates in multiple physiological functions, such as cell-to-cell interactions, cell migration and proliferation. Diabetes mellitus (DM) is a chronic metabolic disorder characterized by rise in blood glucose level. Periodontitis is a chronic inflammatory disease of the periodontal tissue, leading to destruction of bone surrounding the tooth and ultimately tooth loss. There is a two way relationship between diabetes mellitus and periodontitis. Periodontitis is the sixth complication of diabetes along with retinopathy, nephropathy, neuropathy, macrovascular disease, and altered wound healing. Inflammatory mediators like interleukin-6 and tumor necrosis factor-alpha produced during periodontal inflammation can interfere with the actions of insulin receptors and worsen the glycemic control of diabetic patients. Periodontitis is a major cause of tooth loss, affecting over 300 million people and bacteria associated with periodontitis are also linked with systemic problems like endocarditis, atherosclerosis. Recent work has highlighted a major role for the host sugar sialic acid in the biofilm physiology and host-pathogen interactions of T. forsithya, a key periodontal pathogen. There exists a need for a biomarker, for early detection of disease evolution and more robust therapy efficacy measurements. Serum sialic acids were estimated in Indian population by diphenylamine method and Thiobarbituric acid method. The average values were 68 ± 2.6 mg percent by DPA method and 56 ± 5 mg percent by TBA (thiobarbituric acid assay) method. Age and sex showed no influence on serum sialic acid level. Objectives of the present study was to compare (TSSA) level in healthy subjects, subjects with (CMP) with and without (NIDDM) and its effect on non-surgical periodontal therapy. In the present study, the participants were divided into three groups: Group A, B and C. Group A consists of systemically healthy subjects, Group B consists of subjects with (CMP) while Group C consists of subjects with (CMP) with (NIDDM) and results of this study indicated that, at baseline, there were significant differences between Group A, B and Group C with respect to all the clinical parameters, including (GI), (OHI-S), (PPD), (CAL), (TSSA) and (HbA1c) levels. Thus (TSSA) level could be considered as novel biomarker in the progression of periodontal disease and diabetic status. Periodontitis could be considered as a potential, modifiable, and independent risk factor for the development of diabetes. Early detection of elevated (TSSA) level may help in interpreting the progression of periodontitis, risk of development of diabetes mellitus in future and also to prevent complications.
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Vasyutkina, Elena A., Yulia A. Yugay, Valeria P. Grigorchuk, Olga V. Grishchenko, Varvara D. Stepochkina, and Yury N. Shkryl. "Overexpression of the <i>Ib-rolB/C</i> gene perturbs biosynthesis of caffeoylquinic acid derivatives in transgenic calli of sweet potato." Ecological genetics 20, no. 1S (December 8, 2022): 28–29. http://dx.doi.org/10.17816/ecogen112334.
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Ipomoea batatas is a root crop widely cultivated in South America, Africa, and Asia. This is also a source of caffeoylquinic acid derivatives (CQAs) with potential health-promoting benefits. Sweet potato genome carries two separate cellular T-DNA (cT-DNA) regions (IbT-DNA1 and IbT-DNA2). Especially, IbT-DNA2 contains five ORFs homologous to the Agrobacterium rhizogenes T-DNA, namely ORF13, ORF14, ORF17n, ORF18/ORF17n, and RolB/RolC proteins [1]. Unfortunately, presently there is insufficient information on IbT-DNA2 genes function in the physiological processes of sweet potatoes.
In this study, expressional levels of the IbT-DNA2 genes and the effect of Ib-rolB/C overexpression were examined using I. batatas cell culture. We discovered that I. batatas cT-DNA genes were not expressed in callus, and abiotic stresses and chemical elicitors affected their transcriptional levels weakly. Additionally, two Ib-rolBC-transgenic cell lines have been established though Agrobacterium-mediated transformation of I. batatas callus cells. Overexpression of Ib-rolB/C gene reduced biomass accumulation of transgenic cell lines by 1.21.6 times and increased the CQAs content by 1.51.9-fold. To justify the metabolic fluctuations, the study also looked into the expression patterns of the major biosynthetic genes, namely bPAL, IbC4H, Ib4CL, IbHCT, and IbHQT. The obtained data demonstrated that the overexpression of the Ib-rolB/C reduced the IbPAL transcript but considerable increase in the transcript levels of the IbHQT. We propose that this result was obtained through as-yet-uncharacterized signaling pathways activated by RolB/RolC.
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Dapoza, C., C. Castrillo, J. Balcells, S. Martín-Orúe, and J. A. Guada. "On the variation of urinary excretion of creatinine and purine derivatives in pregnant and lactating ewes given diets with different protein contents." Animal Science 68, no. 3 (April 1999): 555–66. http://dx.doi.org/10.1017/s135772980005058x.
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AbstractThe effect of the physiological state and dietary protein level on urinary excretion of creatinine (C) and purine derivatives (PD) was studied in two experiments carried out with pregnant and lactating ewes to evaluate whether the PD/C ratio in urine can he confidently used as an index of PD excretion. In both experiments ewes were given ammonia-treated straw and concentrates including different levels of fish meal and the excretion in urine and milk and the plasma concentration of C, allantoin (AL), xanthine, hypoxanthine and uric acid was measured.Creatinine excretion (in urine and milk) was higher in pregnant ewes than in those lactating (492 and 420 (s.e. 10.0) μmol/kg maternal live weight0.75) and no significant differences were found due to number of foetuses and dietary protein level. The coefficient of variation was 0·10 in both pregnancy and lactation and individual variation accounted for proportionately 0·78 and 0·93 of total variation. The AL/C ratio in urine was highly correlated with daily AL excretion (r = 0·90 and 0·78 in pregnant and lactating ewes, respectively). Changes in PD excretion with experimental treatments were mainly reflected in AL, as the main component (0-83) of total PD. Most of the variation in AL excretion was explained by differences in rumen fermentable organic matter intake (RFOMI) (R2 = 0·79) and AL excretion did not differ between treatments when expressed per kg of RFOMI. In contrast to this the ratio AL/digestible organic matter intake decreased with increasing levels of fish meal in the diet. Urinary PD excretion was better related to estimated PD kidney tubular load (r = 0·76) than to PD plasma concentration (r = 0·64).The results suggest that creatinine excretion is scarcely affected by the number of foetuses in pregnancy and dietary protein level but if the AL/С in urine is used instead of total collection as an index of purines absorbed in the duodenum, differences in urinary creatinine excretion due to physiological state must be accounted for.
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Ogorodnik, A. G., V. A. Yanchenko, L. S. Bobkova, N. M. Seredinska, and A. M. Demchenko. "Synthesis and anаlgеsic activity 5-methyl-3-aryl[1,2,4]triazolo[4,3-a]pyrimidin-7-oles derivatives." Farmatsevtychnyi zhurnal, no. 2 (August 14, 2018): 55–61. http://dx.doi.org/10.32352/0367-3057.2.17.07.
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Pain is a signal of inflammation and disruption of the body. It is the most important protective and adaptive mechanism that ensuring the safety of the individual. A strong and prolonged effect of "pain" irritant arising in injuries or after surgical manipulation transforms the protective reaction of the body to harmful factor that is the cause of secondary violations physiological processes.
The aim of this work was the synthesis of substances in a series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol and study the analgesic effect of the synthesized compounds.
The objects of our research were selected derivatives of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol, which were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanilpirymidyn-4-ol (1) with the corresponding substituted benzoic acid hydrazide The primary evaluation of analgesic activity conducted on thermal stimulation models («hot plate»).
A number of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives were synthesized, and their structure and purity were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship.
The screening for analgesic activity for 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol derivatives in in vivo experiments on hot plate models showed that the highest activity Was noted for the compound containing the methyl group in the fourth position of the aryl substituent, which is 184.28% of the change in the latent period of the reaction, which exceeds the action of the reference preparation of ketorolac by 71.57%. The introduction of halogens into the aryl moiety leads to a decrease in the analgesic activity of the compounds.
A series of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidine-7-ol derivatives were synthesized by condensation and subsequent cyclization of 6-methyl-2-metylsulfanylpirymydyn-4-ol with relevant substituted hydrazide of benzoic acid. The structure and purity of obtained compounds were confirmed by 1H NMR spectroscopy. The analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pyrimidin-7-ol was investigated in order to reveal the structure-activity relationship.
The screening of analgesic activity of 5-methyl-3-aryl [1,2,4] triazolo [4,3-a] pirymidyn-7-ol derivatives in vivo models for «hot plate» shows that the highest activity was noted for compound containing methyl group in the fourth position of the aryl substituent, which is 184.28% change latent period reaction, that exceeds effect reference drug ketorolac at 71.57%. The introduction of halogens in the aryl fragment leads to a decrease analgesic activity of compounds.
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Badeau, Maija, Veera Vihma, Tomi S. Mikkola, Aila Tiitinen, and Matti J. Tikkanen. "Estradiol Fatty Acid Esters in Adipose Tissue and Serum of Pregnant and Pre- and Postmenopausal Women." Journal of Clinical Endocrinology & Metabolism 92, no. 11 (November 1, 2007): 4327–31. http://dx.doi.org/10.1210/jc.2007-1372.
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Abstract Context: The 17β-estradiol fatty acid esters are hormone derivatives with long-lasting estrogenic effect. They are transported in serum lipoproteins and thought to be sequestered in adipose tissue. Objective: Our objective was to determine the 17β-estradiol fatty acid ester concentrations in serum and adipose tissue in women of various hormonal states. Design: After several chromatographic steps separating esterified from free estradiol, time-resolved fluoroimmunoassay was used as a quantifying tool. Participants: Samples were obtained from pregnant women undergoing cesarean section (n = 13), or premenopausal (n = 8) and postmenopausal women (n = 6) during gynecological surgery. Main Outcome Measures: 17β-Estradiol and 17β-estradiol fatty acid ester concentrations in serum, and visceral and sc adipose tissue were examined. Results: The ratio of esterified to free estradiol in plasma increased with decreasing estradiol level from 0.5% in pregnant, to 15% in premenopausal and 110% in postmenopausal women. Estradiol esters constituted about 10% of the free estradiol present in adipose tissue in pregnancy. In nonpregnant women, most of the adipose tissue estradiol was in esterified form, the median ester to free ratio being elevated to 150–490%. After menopause, the overwhelming majority of estradiol in both free and esterified form was present in adipose tissue. Conclusions: The overall higher ester to free estradiol ratio in adipose tissue than in serum indicates active esterification capacity in adipose tissue. The predominance of esterified and free estradiol in postmenopausal adipose tissue compared with serum suggests in situ production and storage. Whether the estradiol esters have an independent physiological role in adipose tissue remains to be clarified.
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Debnath, Biswojit, Waqar Islam, Min Li, Yueting Sun, Xiaocao Lu, Sangeeta Mitra, Mubasher Hussain, Shuang Liu, and Dongliang Qiu. "Melatonin Mediates Enhancement of Stress Tolerance in Plants." International Journal of Molecular Sciences 20, no. 5 (February 27, 2019): 1040. http://dx.doi.org/10.3390/ijms20051040.
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Melatonin is a multifunctional signaling molecule, ubiquitously distributed in different parts of plants and responsible for stimulating several physiological responses to adverse environmental conditions. In the current review, we showed that the biosynthesis of melatonin occurred in plants by themselves, and accumulation of melatonin fluctuated sharply by modulating its biosynthesis and metabolic pathways under stress conditions. Melatonin, with its precursors and derivatives, acted as a powerful growth regulator, bio-stimulator, and antioxidant, which delayed leaf senescence, lessened photosynthesis inhibition, and improved redox homeostasis and the antioxidant system through a direct scavenging of reactive oxygen species (ROS) and reactive nitrogen species (RNS) under abiotic and biotic stress conditions. In addition, exogenous melatonin boosted the growth, photosynthetic, and antioxidant activities in plants, confirming their tolerances against drought, unfavorable temperatures, salinity, heavy metals, acid rain, and pathogens. However, future research, together with recent advancements, would support emerging new approaches to adopt strategies in overcoming the effect of hazardous environments on crops and may have potential implications in expanding crop cultivation against harsh conditions. Thus, farming communities and consumers will benefit from elucidating food safety concerns.
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Yakoviichuk, O. V., O. O. Danchenko, M. M. Danchenko, A. S. Fedorko, and I. O. Kulyk. "ЖИРНОКИСЛОТНИЙ СКЛАД МІОКАРДУ ГУСЕЙ ЗА ДІЇ ВІКАСОЛУ." Scientific Issue Ternopil Volodymyr Hnatiuk National Pedagogical University. Series: Biology 77, no. 3 (September 24, 2019): 32–38. http://dx.doi.org/10.25128/2078-2357.19.3.4.
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In science vicasol is known to be relative to the energy and antioxidant systems of tissues closely related to the biosynthesis and oxidation of fatty acids. This effect may cause changes in the fatty acid composition of tissues, and numerous works on the positive effect of quinones and their derivatives on the myocardial function, suggest that the proper dose and feeding can increase the stability and productivity of poultry. The given was aims to study the effect of vicasol on the fatty acid composition of goose myocardium.
Myocardium was chosen as a biological object. Biological material was collected every 7 days throughout the period from the 21st to the 35th day of ontogeny, characterized by the state of physiological tension of geese. Feeding of geese with vicasol at a dose of 0.7 mg / kg body weight began with the 3rd day of ontogeny. Fatty acid analysis in myocardial tissues was performed by gas-liquid chromatography, pre-fabric samples were processed with the method by Palmer (1971) to obtain tissue lipid extracts.
According to the results of the study, due to various changes in the content of the entire spectrum of fatty acids of the tissue during the experiment - the use of vicasol causes a slight increase in the unsaturation and the total content of unsaturated fatty acids in the myocardium of geese. These fluctuations are realized depending on the physiological state of the body. where vicasol can stimulate both the biosynthesis processes of individual fatty acids and their mitochondrial and microsomal oxidation, as evidenced by multidirectional reliable changes in the content of their entire spectrum. In particular, on the 21st day, the content of docosopentaenoic acid increased by 36.3% whereas the content of docosohexaenoic and linolenic acids decreased by an average of 21–24%, on the 28th day the content of eicosatetraic and docosahexaenoic acids increased whereas the content of the linoleic acids dropped by 22.6% in control groups. On the 35th day, the content of basic unsaturated fatty acids: palmitooleic, linoleic, linolenic and docosohexaenoic acids increased in the tissue under the influence of vicasol with complete depletion of docosopentaenoic acid. These fluctuations in fatty acid composition cause a slight increase in the total content of unsaturated fatty acids and increase the unsaturation of myocardial lipids on the 28th and 35th days of ontogeny of geese. Based on previous results regarding the antioxidant state of myocardium affected by vicasol and the given findings, which prove changes in the content of the entire spectrum of fatty acids during the selected ontogeny, vicasol can be used in poultry farming as a tool to improve the quality and the resilience of poultry.
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Shen, Changchao, Wenwei Tang, Dongqiang Zeng, Hongle Xu, Wangcang Su, and Renhai Wu. "Isoxadifen-Ethyl Derivatives Protect Rice from Fenoxaprop-P-Ethyl–associated Injury during the Control of Weedy Rice." Weed Science 65, no. 5 (August 2, 2017): 579–87. http://dx.doi.org/10.1017/wsc.2017.27.
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Fenoxaprop-P-ethyl, a phenoxy herbicide of the aryloxy–phenoxy–propionic acid group, had a strong control effect when applied POST to weedy rice in this study, with the effective concentrations of 294 μM and 218 μM of herbicide causing 50% inhibition (IC50) in plant height and fresh weight values, respectively. However, fenoxaprop-P-ethyl caused phytotoxicity in cultivated rice. Isoxadifen-ethyl, a widely used herbicide safener in rice, can decrease the phytotoxicity caused by fenoxaprop-P-ethyl. Owing to the extremely similar morphological features and physiological properties of weedy and cultivated rice, it is not practical to spray isoxadifen-ethyl directly on cultivated rice plants to safen them. Applying the safener directly to cultivated rice seeds may be a practical alternative method. To improve the biological activity of isoxadifen-ethyl seed treatments, novel compounds were designed by splicing other groups, including amines, amino acids, and 2- methoxy-5-nitrophenol sodium salt, to the parental structure of isoxadifen-ethyl. Through hydrolysis, acyl chlorination, acyl amination, and esterification, a series of isoxadifen-ethyl derivatives were synthesized and their structures were determined by mass spectrometry and1H nuclear magnetic resonance spectroscopy. The biological activities of five of the isoxadifen-ethyl derivatives, which possessed recovery effects similar to isoxadifen-ethyl, were able to relieve herbicide phytotoxicity. In pot experiments, isoxadifen-ethyl showed almost no activity as a seed treatment, while three derivative compounds, when used independently as seed treatments, were able to prevent the damage caused by fenoxaprop-P-ethyl. The results will help to develop a new control method for weedy rice, thereby decreasing production costs and increasing farmers’ incomes.
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Hung, Shiou-Fen, Yu-Han Wen, Lu-Yi Yu, Hsin-Cheng Chiu, Yi-Ting Chiang, and Chun-Liang Lo. "Development of a Rapid-Onset, Acid-Labile Linkage Polyplex-Mixed Micellar System for Anticancer Therapy." Polymers 13, no. 11 (May 31, 2021): 1823. http://dx.doi.org/10.3390/polym13111823.
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In the treatment of cancers, small interfering ribonucleic acids (siRNAs) are delivered into cells to inhibit the oncogenic protein’s expression; however, polyanions, hydrophilicity, and rapid degradations in blood, endosomal or secondary lysosomal degradation hamper clinal applications. In this study, we first synthesized and characterized two copolymers: methoxy poly(ethylene glycol)-b-poly(2-hydroxy methacrylate-ketal-pyridoxal) and methoxy poly(ethylene glycol)-b-poly(methacrylic acid-co-histidine). Afterwards, we assembled two polymers with the focal adhesion kinase (FAK) siRNA, forming polyplex-mixed micelles for the treatment of the human colon cancer cell line HCT116. In terms of the physiological condition, the cationic pyridoxal molecules that were conjugated on the copolymer with ketal bonds could electrostatically attract the siRNA. Additionally, the pyridoxal could form a hydrophobic core together with the hydrophobic deprotonated histidine molecules in the other copolymer and the hydrophilic polyethylene glycol (PEG) shell to protect the siRNA. In an acidic condition, the pyridoxal would be cleaved from the polymers due to the breakage of the ketal bonds and the histidine molecules can simultaneously be protonated, resulting in the endosome/lysosome escape effect. On the basis of our results, the two copolymers were successfully prepared and the pyridoxal derivatives were identified to be able to carry the siRNA and be cleavable by the copolymers in an acidic solution. Polyplex-mixed micelles were prepared, and the micellar structures were identified. The endosome escape behavior was observed using a confocal laser scanning microscopy (CLSM). The FAK expression was therefore reduced, and the cytotoxicity of siRNA toward human colon cancer cells was exhibited, rapidly in 24 h. This exceptional anticancer efficiency suggests the potential of the pH-sensitive polyplex-mixed micellar system in siRNA delivery.
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Piotrowska, Alicja, Romuald Czerpak, Joanna Adamowicz, Alicja Biedrzycka, and Marta Potocka. "Comparison of stimulatory effect of cytokinins adenine and urea derivatives on the level of some components in Wolffia arrhiza (L.) Wimm. (Lemnaceae)." Acta Societatis Botanicorum Poloniae 74, no. 2 (2011): 111–18. http://dx.doi.org/10.5586/asbp.2005.015.
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The effect of cytokinins with different chemical structures, adenine-type: N6-benzylaminopurine (BAP), N6-furfurylaminopurine (FAP) and derivative of urea - 1,3-diphenylurea (DPU) applied in optimal physiological concentrations of 10<sup>-6</sup>-10<sup>-4</sup> M on the mixotrophic plant <em>Wolffia arrhiza</em> during the period of 20 days of culture, was examined. The cytokinin highest influence on the metabolites level in <em>W. arrhiza</em> fresh weight was demonstrated in the range of concentrations 10<sup>-6</sup>-10<sup>-5</sup> M between the 5th and the 10th day of culture. Among used cytokinins, the highest stimulative effect on the content of water-soluble proteins can be attributed to DPU (181%), slightly lower to BAP (167%) and the lowest to FAP (113%) in comparison with the control culture (100%). BAP was found to exert the most stimulative activity on nucleic acids accumulation (DNA+RNA) to the maximum value (127%). FAP and DPU possessed weaker stimulative activity increasing the nucleic acid content to the level of 120% and 118%, properly. The content of monosaccharides was stimulated to the highest level of 174% in FAP treated plants, to 151% in case of BAP and in case of DPU to 144%. Whereas, the highest increase of the photosynthetic pigments content (chlorophyll a and b as well as total carotenoids) to the range of 123-146% in <em>W. arrhiza</em> culture in the presence of DPU, was observed. Under the influence of FAP the accumulation of photosynthetic pigments was stimulated less effectively to the range of 113-140%. When the plants grew with BAP the chlorophylls and carotenoids contents increased to the lowest values of 119-131%. On the other hand, the content of total carotenoids was stimulated only during the first days of culture, then between the 15th and the 20th day it was inhibited by all applied adenine and urea-type cytokinins to the value of 70%. The results indicate that there is no quantitative correlation between the structure of all analysed cytokinins and their influence on the biochemical responses of <em>W. arrhiza</em>.
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Ahmed, Ishtiaq, Saif Ur Rehman, Shiva Shahmohamadnejad, Muhammad Anjum Zia, Muhammad Ahmad, Muhammad Muzammal Saeed, Zain Akram, Hafiz M. N. Iqbal, and Qingyou Liu. "Therapeutic Attributes of Endocannabinoid System against Neuro-Inflammatory Autoimmune Disorders." Molecules 26, no. 11 (June 3, 2021): 3389. http://dx.doi.org/10.3390/molecules26113389.
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In humans, various sites like cannabinoid receptors (CBR) having a binding affinity with cannabinoids are distributed on the surface of different cell types, where endocannabinoids (ECs) and derivatives of fatty acid can bind. The binding of these substance(s) triggers the activation of specific receptors required for various physiological functions, including pain sensation, memory, and appetite. The ECs and CBR perform multiple functions via the cannabinoid receptor 1 (CB1); cannabinoid receptor 2 (CB2), having a key effect in restraining neurotransmitters and the arrangement of cytokines. The role of cannabinoids in the immune system is illustrated because of their immunosuppressive characteristics. These characteristics include inhibition of leucocyte proliferation, T cells apoptosis, and induction of macrophages along with reduced pro-inflammatory cytokines secretion. The review seeks to discuss the functional relationship between the endocannabinoid system (ECS) and anti-tumor characteristics of cannabinoids in various cancers. The therapeutic potential of cannabinoids for cancer—both in vivo and in vitro clinical trials—has also been highlighted and reported to be effective in mice models in arthritis for the inflammation reduction, neuropathic pain, positive effect in multiple sclerosis and type-1 diabetes mellitus, and found beneficial for treating in various cancers. In human models, such studies are limited; thereby, further research is indispensable in this field to get a conclusive outcome. Therefore, in autoimmune disorders, therapeutic cannabinoids can serve as promising immunosuppressive and anti-fibrotic agents.
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Jiang, Ni-Hao, and Shi-Han Zhang. "Effects of Combined Application of Potassium Silicate and Salicylic Acid on the Defense Response of Hydroponically Grown Tomato Plants to Ralstonia solanacearum Infection." Sustainability 13, no. 7 (March 27, 2021): 3750. http://dx.doi.org/10.3390/su13073750.
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Bacterial wilt, caused by soilborne pathogenic bacterium Ralstonia solanacearum, is a serious and widespread disease that affects global tomato production. Both silicon (Si) and salicylic acid (SA) play important roles in enhancing tomato resistance against bacterial wilt, however, their combined effects on the defense responses of infected tomato plants remain unknown. Hence, the combined effects of Si and SA on physiological and biochemical parameters of R. solanacearum-infected tomato plants were investigated. The combination treatment of Si and SA significantly decreased disease incidences, lipoxygenase (LOX) activity and ethylene (ET) production. The combined treatments were more prominent in improving the morphological traits of root systems, such as root length, root surface area, average root diameter and root volume. The activities of polyphenol oxidase (PPO) and peroxidase (POD) and the concentrations of total soluble phenolics (TSPs) and lignin-thioglycolic acid (LTGA) derivatives were significantly increased in the plants with combined treatments. Si in combination with SA could significantly enhance neutral invertase (NI) and acid invertases (AI) activities in the leaves of tomato plants at 3 days post-infection (dpi) compared with application of Si alone. Three defense-related genes, PAL, POD and pathogenesis-related protein 1 (PR1), were significantly induced in Si+SA treatment at 7 dpi when compared with individual application of Si or SA. The expression level of salicylic acid-binding protein 2 (SABP2) was significantly higher for combination treatment when compared with treatment of Si or SA alone. The possible mechanisms involved in the synergistic effects of Si and SA on the control of tomato bacterial wilt were proposed. This study indicates that under hypertonic conditions, the combined application of 2.0 mM potassium silicate (K2SiO3) and 0.5 mM SA had a synergistic effect on the control of tomato bacterial wilt.
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Sobhi, Hany F., Xinjie Zhao, Peter Plomgaard, Miriam Hoene, Jakob S. Hansen, Benedikt Karus, Andreas M. Niess, et al. "Identification and regulation of the xenometabolite derivatives cis- and trans-3,4-methylene-heptanoylcarnitine in plasma and skeletal muscle of exercising humans." American Journal of Physiology-Endocrinology and Metabolism 318, no. 5 (May 1, 2020): E701—E709. http://dx.doi.org/10.1152/ajpendo.00510.2019.
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Little is known about xenometabolites in human metabolism, particularly under exercising conditions. Previously, an exercise-modifiable, likely xenometabolite derivative, cis-3,4-methylene-heptanoylcarnitine, was reported in human plasma. Here, we identified trans-3,4-methylene-heptanoylcarnitine, and its cis-isomer, in plasma and skeletal muscle by liquid chromatography-mass spectrometry. We analyzed the regulation by exercise and the arterial-to-venous differences of these cyclopropane ring-containing carnitine esters over the hepatosplanchnic bed and the exercising leg in plasma samples obtained in three separate studies from young, lean and healthy males. Compared with other medium-chain acylcarnitines, the plasma concentrations of the 3,4-methylene-heptanoylcarnitine isomers only marginally increased with exercise. Both isomers showed a more than twofold increase in the skeletal muscle tissue of the exercising leg; this may have been due to the net effect of fatty acid oxidation in the exercising muscle and uptake from blood. The latter idea is supported by a more than twofold increased net uptake in the exercising leg only. Both isomers showed a constant release from the hepatosplanchnic bed, with an increased release of the trans-isomer after exercise. The isomers differ in their plasma concentration, with a four times higher concentration of the cis-isomer regardless of the exercise state. This is the first approach studying kinetics and fluxes of xenolipid isomers from tissues under exercise conditions, supporting the hypothesis that hepatic metabolism of cyclopropane ring-containing fatty acids is one source of these acylcarnitines in plasma. The data also provide clear evidence for an exercise-dependent regulation of xenometabolites, opening perspectives for future studies about the physiological role of this largely unknown class of metabolites.
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Todorov, Petar, Stela Georgieva, Desislava Staneva, Petia Peneva, Petar Grozdanov, Ivanka Nikolova, Evgenia Vasileva-Tonkova, and Ivo Grabchev. "Study of Novel Peptides for Antimicrobial Protection in Solution and on Cotton Fabric." Molecules 27, no. 15 (July 26, 2022): 4770. http://dx.doi.org/10.3390/molecules27154770.
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Some new N- and C-modified biomolecular peptide analogues of both VV-hemorphin-5 and VV-hemorphin-7 with varied amino acids (Cys, Glu, His), 1-adamantanecarboxylic acid, and niacin (nicotinic acid) were synthesized by solid-phase peptide synthesis—Fmoc (9-fluorenylmethoxy-carbonyl) chemistry and were characterized in water solutions with different pH using spectroscopic and electrochemical techniques. Basic physicochemical properties related to the elucidation of the peptide structure at physiological pH have been also studied. The results showed that the interaction of peptide compounds with light and electricity preserves the structural and conformational integrity of the compounds in the solutions. Moreover, textile cotton fibers were modified with the new compounds and the binding of the peptides to the surface of the material was proved by FTIR and SEM analysis. Washing the material with an alkaline soap solution did not show a violation of the modified structure of the cotton. Antiviral activity against the human respiratory syncytial virus (HRSV-S2) and human adenovirus serotype 5 (HAdV-5), the antimicrobial activity against B. cereus and P. aeruginosa used as model bacterial strains and cytotoxic effect of the peptide derivatives and modified cotton textile material has been evaluated. Antimicrobial tests showed promising activity of the newly synthesized compounds against the used Gram-positive and Gram-negative bacteria. The compounds C-V, H-V, AC-V, and AH-V were found slightly more active than NH7C and NCH7. The activity has been retained after the deposition of the compounds on cotton fibers.
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Marounek, M., Z. Volek, T. Taubner, D. Duškova, L. Kalachniuk, and V. Khomych. "ГІПОХОЛЕСТЕРОЛЕМІЧНА ДІЯ N–АЛКІЛАМІДОВАНОГО АЛЬГІНАТУ." Scientific Messenger of LNU of Veterinary Medicine and Biotechnologies 18, no. 3(71) (October 10, 2016): 59–62. http://dx.doi.org/10.15421/nvlvet7113.
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It is known that in the process of digestion and absorption of nutrients, one of the key roles belongs to polysaccharides (among which there are alginic acid), which have the ability to increase viscosity and form a gel in the intestine. Previously, we studied the physiological effects of pectin, cellulose and their amidated derivatives that have demonstrated growth of hypocholesterolemic activity in the rats. From here, it was decided to investigate the hypocholesterolemic effect of N–alkylamidated alginate on laboratory animals. That’s why, female rats were fed according to three diets, namely the control (1) and two experimental (2 and 3), which contained cholesterol (10 g/kg) and different amounts N–alkylamidated alginate (0 and 40 g / kg, respectively), and all animals fed also palm oil. N–alkylamidated alginate significantly lowered the level of cholesterol (total and LDL) in serum and liver and of hepatic total lipids in the rats, which were on cholesterol–containing diet. In the faeces of animals that consumed N–alkylamidated alginate, it was observed increased concentrations of fat from 61 to 91 mg / g, while the concentration of cholesterol, bile acids and total sterols was not significantly changed.Hence, decrease cholesterolemia in rats (that consumed N–alkylamidated alginate) is probably based more on the removal of fat from the intestine, rather than on the interruption of enterohepatic circulation of cholesterol.
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Karkischenko, N. N., V. N. Karkischenko, Yu V. Fokin, L. A. Taboyakova, O. V. Alimkina, and M. M. Borisova. "Between Cognitivity and Neuropathies: Neuroimaging of the Effects of GABAergic Modulation of the Hippocampus and Prefrontal Neocortexis by Normalized Brain Electrograms." Journal Biomed, no. 2 (June 10, 2020): 12–38. http://dx.doi.org/10.33647/2074-5982-16-2-12-38.
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A comparative analysis conducted across the entire range of normalized brain electrograms (NBE) revealed the selective effect of gamma-aminobutyric acid (GABA) derivatives in the hippocampus and frontal pole of the neocortex. A signifi cant similarity in the level of activation of these brain regions was revealed under the action of glutamine and, particularly, gabapentin. For gabapentin, the activity of the hippocampus is more comparable to that in the anterior suprasilvius gyrus. Under the action of pregabalin, NBE revealed a similarity between the hippocampus and the proreal gyrus, with a more pronounced activity being registered in the range of 1–10 Hz. The NBE activity in the anterior suprasilvian gyrus was lower than that in the proreal gyrus. Under the action of phenibut, the activity of the hippocampus was higher than that of the prefrontal cortex across the 30–40 Hz range; however, under the action of aminalon, this phenomenon was observed for all the analysed rhythms. The predominant effect of GABA derivatives on the high-frequency components of the γ-rhythms of NBE was established. The most pronounced activation effects in γ-rhythms were characteristic of aminalon, while the most pronounced effects of deprimation were characteristic of gabapentin. The overall picture of the γ-rhythm activity was similar under the administration of glutamine, pregabalin and phenibut, as well as being generally close to the background level. The effects of glutamine and pregabalin in the analysis of NBE showed similarities across the frequency ranges of about 40–44 Hz and 60–64 Hz. The effects of pregabalin, gabapentin, and phenibut were similar across the frequency range of about 52–62 Hz. In the high-frequency γ-rhythms, gabapentin, pregabalin and phenibut were characterized by peaks in the range of 44–50 Hz, 40–55 Hz and 35–40 Hz, respectively. Aminalon showed no similarities with other GABA derivatives and was characterized by an extremum in the γ-rhythm at a frequency of about 41 Hz. Using instrumental methods for assessing cognitive behaviour and the mathematical analysis of NBE, the signifi cant role of the intercalary neurons (basket cells) of the hippocampus and prefrontal cortex in the implementation of glutamate and GABA effects was established. It was confi rmed that GABA derivatives function as the main mediator of intercalary neurons in the systemic activity of the brain. The maximum values of NBE under the action of all the GABA derivatives under study coincide with the pharmacodynamic and pharmacokinetic parameters of these drugs. A comparative analysis of the effects of glutamate and all the studied GABA derivatives revealed the greatest similarity of the former with phenibut. Aminalon, being a synthetic analogue of GABA, differs from all other drugs under study by the highest activation of the general level of NBE. The effects of neuroimaging refl ect the properties and nature of the effect of drugs on cognitive functions, intra-centre relations of the brain and higher nervous activity. New mechanisms of the systemic action of GABA derivatives were studied. The obtained results confi rm that the normalized electrographic activity of various parts of the brain can be used to identify certain physiological and pathogenetic mechanisms of the most important functions of the brain and their disorders. Activation of the GABAergic stress-limiting system can be considered as one of the promising methods for the selection of approaches to preventing and treating diseases associated with neurogenic and psychogenic factors.
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Chabowski, Dawid S., Katie E. Cohen, Ossama Abu-Hatoum, David D. Gutterman, and Julie K. Freed. "Crossing signals: bioactive lipids in the microvasculature." American Journal of Physiology-Heart and Circulatory Physiology 318, no. 5 (May 1, 2020): H1185—H1197. http://dx.doi.org/10.1152/ajpheart.00706.2019.
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The primary function of the arterial microvasculature is to ensure that regional perfusion of blood flow is matched to the needs of the tissue bed. This critical physiological mechanism is tightly controlled and regulated by a variety of vasoactive compounds that are generated and released from the vascular endothelium. Although these substances are required for modulating vascular tone, they also influence the surrounding tissue and have an overall effect on vascular, as well as parenchymal, homeostasis. Bioactive lipids, fatty acid derivatives that exert their effects through signaling pathways, are included in the list of vasoactive compounds that modulate the microvasculature. Although lipids were identified as important vascular messengers over three decades ago, their specific role within the microvascular system is not well defined. Thorough understanding of these pathways and their regulation is not only essential to gain insight into their role in cardiovascular disease but is also important for preventing vascular dysfunction following cancer treatment, a rapidly growing problem in medical oncology. The purpose of this review is to discuss how biologically active lipids, specifically prostanoids, epoxyeicosatrienoic acids, sphingolipids, and lysophospholipids, contribute to vascular function and signaling within the endothelium. Methods for quantifying lipids will be briefly discussed, followed by an overview of the various lipid families. The cross talk in signaling between classes of lipids will be discussed in the context of vascular disease. Finally, the potential clinical implications of these lipid families will be highlighted.
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Studenok, A. "The effect of autonomic nervous system tone on the content of cyclic and acyclic aminoacids in the serum of chickens." Naukovij vìsnik veterinarnoï medicini, no. 2 (168) (December 9, 2021): 158–67. http://dx.doi.org/10.33245/2310-4902-2021-168-2-158-167.
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Regulation of metabolic and physiological functions of the whole organismis a complex neurohumoral process. Its functioning is supported by many organs and systems. One of the main roles here is performed by the autonomic nervous system. The mutual influence of its departments – sympathetic and parasympathetic, provide stable homeostasis and balanced work of all organs and structures. The sympathetic department is responsible for energy resource mobilization and adaptation. Without its influence, a rapid response of the cardiovascular and endocrine systems to the body's needs arising from changes in the internal or external environment is impossible. Dominant sympathetic tone provides activation of gluconeogenes is and glycogenolysis, lipolysis, etc. In contrast, the parasympathetic division is responsible for energy conservation and nutrient accumulation. Its dominant activity causes a decrease in heart rate, increase in pupil diameter depending on light flux, secretion of saliva and digestive juices, acceleration of motility of the gastrointestinal tract. However, to date, the existence of the influence of the tone of the autonomic nervous system on the content of proteins and their derivatives in the serum has not been studied enough. Proteins and their main components – aminoacids are indispensable in the construction and functioning of the whole organism of all living beings. Deficiency or absence of at least one essential amino acid can lead to disruption of various functional systems of the body, adverse health effects, and in the case of long-term deficiency and death. Studies to determine the content of amino acids in the serum of chickens with different dominant tone of the autonomic nervous system revealed different contents of individual cyclic and acyclic amino acids. The content of phenylalanine in sympathicotonic chickens differed significantly compared with the bird, which had a balanced tone (P˂0.05). In contrast, the tyrosine content was almost the same in all groups of animals. The amino acids leucine/ isoleucine and alanine were not significantly predominant in the different samples, but tended to be higher in sympathetic and vagotonic chickens. The study suggests that the dominance of the sympathetic and parasympathetic divisions of the autonomic nervous system or their balanced tone on the content of amino acids in the serum of chickens. Key words: sympathicotonia, vagotonia, normotony, phenylalanine, alanine, leucine/isoleucine, tyrosine.
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Nabokina, Svetlana M., Thomas Y. Ma, and Hamid M. Said. "Mechanism and regulation of folate uptake by human pancreatic epithelial MIA PaCa-2 cells." American Journal of Physiology-Cell Physiology 287, no. 1 (July 2004): C142—C148. http://dx.doi.org/10.1152/ajpcell.00011.2004.
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After the liver, the pancreas contains the second highest level of folate among human tissues, and folate deficiency adversely affects its physiological function. Despite that, nothing is currently known about the cellular mechanisms involved in folate uptake by cells of this important exocrine organ or about folate uptake regulation. We have begun to address these issues, and in this report we present the results of our findings on the mechanism of folate uptake by the human-derived pancreatic MIA PaCa-2 cells. Our results show folic acid uptake to be 1) temperature and energy dependent; 2) pH dependent, with a markedly higher uptake at acidic pH compared with neutral or alkaline pH; 3) Na+ independent; 4) saturable as a function of substrate concentration (apparent Km = 0.762 ± 0.10 μM); 5) inhibited (with similar affinity) by reduced, substituted, and oxidized folate derivatives; and 6) sensitive to the inhibitory effect of anion transport inhibitors. RT-PCR and Western blot analysis showed expression of the human reduced folate carrier (hRFC) at the RNA and protein levels, respectively. The functional contribution of hRFC in carrier-mediated folate uptake was confirmed by gene silencing using gene-specific small interfering RNA. Evidence also was found suggesting that the folate uptake process by MIA PaCa-2 cells is regulated by cAMP- and protein tyrosine kinase (PTK)-mediated pathways. These studies demonstrate for the first time the involvement of a specialized, acidic pH-dependent, carrier-mediated mechanism for folate uptake by human pancreatic MIA PaCa-2 cells. The results also show the involvement of hRFC in the uptake process and suggest the possible involvement of intracellular cAMP- and PTK-mediated pathways in the regulation of folate uptake.
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Fedorenko, S. "ПРООКСИДАНТНО–АНТИОКСИДАНТНИЙ СТАТУС КОРІВ ЗА ГОНАДОПАТІЙ." Scientific Messenger of LNU of Veterinary Medicine and Biotechnologies 18, no. 3(71) (October 16, 2016): 178–81. http://dx.doi.org/10.15421/nvlvet7140.
Full textAbstract:
Situational increase in the concentration of free oxide in the body for a reduction of antioxidant defense is accompanied by the development of pathological processes.One of the major cell damage by free radicals is the destruction of the fatty acids that make up cell membranes (lipid peroxidation). Peroxidation of lipids of biological membranes causes a disturbance of the barrier function and reduces the enzymatic activity; disintegrates receptor binding and vesicular transport. This leads to disruption of cellular activity, accelerated apoptosis degeneration, necrobiosis, atrophy and necrosis.The damaging effect of oxygen radicals in the cell antioxidant defense system opposed., protection function is performed by enzymes – superoxide dismutase, catalase, glutathione reductase, and low molecular weight non–enzymatic antioxidants (carotenoids, tocopherol), water soluble vitamins (ascorbic acid).Thus, the oxidation of lipid structures underlying the development of many diseases, including pathologies animal reproductive organs.Among the disorders of the reproductive function in cows is quite common gonadopathy such as gonadodystrophy, hypogonadism and hypoluteolisis on background endometritis (diorganspathology).The emergence and development of ovarian pathologies cows hypothetically can be supplemented by the existence of violations, failures in the prooxidant–antioxidant system, as the basis of these pathologies is a violation tropism, of complex mechanisms for metabolism and preserve cell structure and ovarian tissue.To determine the concentration of free oxide derivatives and antioxidant protection status in cows for ovariodystrophy, hypogonadism and diorgan pathology (endometritis↔hypoluteolisis) presents the materials the article.It is found that for cows ovarian pathologies compared to animals with the normal physiological state gonads malondialdehyde erythrocytes in blood was significantly increased by 10.4 –23.2 mm/l (25.3 – 56.8%), catalase activity was reduced to 13–14,4 m / H2O2 / l–min (56.9– 91.1%), reduced glutathione was reduced to 0.68–0.8 (16.1–19.1%).Installed status data of the antioxidant system in cows with gonadopathy show quite important determinant role in the genesis of ovarian pathologies.
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Okamoto, Lillian L., Caleb C. Reichhardt, Brian Griffin, Laura A. Smith, Gordon Murdoch, and Kara J. Thornton. "PSIX-28 Examining the effects of estradiol, trenbolone acetate, or polyamines on bovine satellite cell differentiation." Journal of Animal Science 98, Supplement_4 (November 3, 2020): 333. http://dx.doi.org/10.1093/jas/skaa278.592.
Full textAbstract:
Abstract The mechanism through which anabolic implants improve skeletal muscle growth of beef animals is incompletely understood. Polyamines (PA) are bioactive amino acid derivatives that act as potent growth stimulants. The objective of this study was to determine effects of anabolic implants, PA and their precursors on bovine satellite cell (BSC) differentiation. Primary BSC were cultured to approximately 80% confluency, at which time they were induced to differentiate in the presence of 3% horse serum (Con) and treated with 10nM TBA, 10 nM E2, or 10nM TBA and 10 nM E2 (ETBA), 10 mM methionine (Met), 8 mM ornithine (Orn), 2 mM putrescine (Put), 1.5 mM spermidine (Spd) or 0.5 mM spermine (Spe). Total mRNA was isolated 0, 2, 4, 8, 12, 24, or 48 h post-treatment and abundance of paired box transcription factor 7 (Pax7) and myogenic differentiation factor (MyoD) were analyzed. Treatment with the hormones (TBA, E2, or ETBA) and PA (Orn, Put, Spd, and Spe) increased (P < 0.05) abundance of MyoD 4 h post-treatment when compared to Con cultures. However, 24 h post-treatment, MyoD abundance was decreased in the presence of hormone treatments when compared to the Con, while the PA treatments increased (P < 0.05) abundance of MyoD when compared to the Con cultures. Treatment with either the hormones or PA had no effect (P > 0.05) on Pax7 abundance at 2, 4, 8, 12, 24, or 48 h post-treatment when compared to Con cultures (P > 0.05). These results indicate that treatment with PA or hormones increases abundance of MyoD, though temporally different indicating that these two classes of growth promoters impact differentiation via alternate physiological pathways. Additional research is underway in order to determine the effects of both PA and hormones on differentiation of primary BSC.