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Calder, Philip C. „Eicosanoids“. Essays in Biochemistry 64, Nr. 3 (18.08.2020): 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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Regulska, Magdalena, Magdalena Szuster-Głuszczak, Ewa Trojan, Monika Leśkiewicz und 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, Nr. 2 (31.12.2020): 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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Pope, Edward C., und 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, Nr. 11 (01.06.2002): 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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Rodríguez, María, Pilar G. Rebollar, Simona Mattioli und Cesare Castellini. „n-3 PUFA Sources (Precursor/Products): A Review of Current Knowledge on Rabbit“. Animals 9, Nr. 10 (15.10.2019): 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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Wang, Hongyu, Erdu Ren, Xiaoe Xiang, Yong Su und Weiyun Zhu. „Dynamic Changes in Serum Metabolomic Profiles of Growing Pigs Induced by Intravenous Infusion of Sodium Butyrate“. Metabolites 10, Nr. 1 (01.01.2020): 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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Fehér, Evelin, István Szatmári, Tamás Dudás, Anna Zalatnai, Tamás Farkas, Bálint Lőrinczi, Ferenc Fülöp, László Vécsei und József Toldi. „Structural Evaluation and Electrophysiological Effects of Some Kynurenic Acid Analogs“. Molecules 24, Nr. 19 (26.09.2019): 3502. http://dx.doi.org/10.3390/molecules24193502.
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Kynurenic acid (KYNA), a metabolite of tryptophan, as an excitatory amino acid receptor antagonist is an effective neuroprotective agent in case of excitotoxicity, which is the hallmark of brain ischemia and several neurodegenerative processes. Therefore, kynurenine pathway, KYNA itself, and its derivatives came into the focus of research. During the past fifteen years, our research group has developed several neuroactive KYNA derivatives, some of which proved to be neuroprotective in preclinical studies. In this study, the synthesis of these KYNA derivatives and their evaluation with divergent molecular characteristics are presented together with their most typical effects on the monosynaptic transmission in CA1 region of the hippocampus of the rat. Their effects on the basic neuronal activity (on the field excitatory postsynaptic potentials: fEPSP) were studied in in vitro hippocampal slices in 1 and 200 μM concentrations. KYNA and its derivative 4 in both 1 and 200 μM concentrations proved to be inhibitory, while derivative 8 only in 200 μM decreased the amplitudes of fEPSPs. Derivative 5 facilitated the fEPSPs in 200 μM concentration. This is the first comparative study which evaluates the structural and functional differences of formerly and newly developed KYNA analogs. Considerations on possible relations between molecular structures and their physiological effects are presented.
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Yan, Xi Ming, Ming Ruo Ding, Ming Guo Liu, Jun Zhi Wang und Nian Yu Huang. „Study on Biomaterials of Anti-Gastric Trametenolic Acid B Semi-Synthetic Derivatives“. Advanced Materials Research 918 (April 2014): 32–35. http://dx.doi.org/10.4028/www.scientific.net/amr.918.32.
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Discovery of bioactive ingredients from plants and fungi is always the hot spots in medicinal chemistry. The trametenolic acid B was a bioactive lanostane-type triterpenoid inTrametes lactinea(Berk.) Pat. In this work, four semi-synthetic derivatives were synthesized, characterized and evaluated the anti-gastric cancer activities against HGC-27 cells with the aim of obtaining better anti-tumor agents. The compounds2aand3bpossessed good anti-proliferative effects under normal physiological conditions, and their anti-cancer effects increased as the pH decrease to 5.5 with the IC50of 17.55 and 10.63 μM, respectively. These compounds might be further developed as anti-gastric cancer drugs.
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Lupini, Antonio, Agostino Sorgonà, Maria Polsia Princi, Francesco Sunseri und Maria Rosa Abenavoli. „Morphological and physiological effects of trans-cinnamic acid and its hydroxylated derivatives on maize root types“. Plant Growth Regulation 78, Nr. 2 (17.06.2015): 263–73. http://dx.doi.org/10.1007/s10725-015-0091-5.
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Sugiyama, Hironori, Seiichi Matsugo, Tetsuya Konishi, Toshinari Takamura, Shuichi Kaneko, Yukari Kubo, Kyouhei Sato und Kan Kanamori. „Synthesis, Structure, and Physiological Effects of Peroxovanadium(V) Complexes Containing Amino Acid Derivatives as Ancillary Ligands“. Chemistry Letters 41, Nr. 4 (05.04.2012): 377–79. http://dx.doi.org/10.1246/cl.2012.377.
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Hoa, Nguyen Thi, Le Thi Ngoc Van und Quan V. Vo. „The hydroperoxyl antiradical activity of natural hydroxycinnamic acid derivatives in physiological environments: the effects of pH values on rate constants“. RSC Advances 12, Nr. 24 (2022): 15115–22. http://dx.doi.org/10.1039/d2ra02311c.
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Fotinos, Nicolas, Maruska Convert, Jean-Claude Piffaretti, Robert Gurny und Norbert Lange. „Effects on Gram-Negative and Gram-Positive Bacteria Mediated by 5-Aminolevulinic Acid and 5-Aminolevulinic Acid Derivatives“. Antimicrobial Agents and Chemotherapy 52, Nr. 4 (14.01.2008): 1366–73. http://dx.doi.org/10.1128/aac.01372-07.
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ABSTRACT Due mainly to the extensive use of antibiotics, the spread of multiresistant bacterial strains is one of the most worrying threats to public health. One strategy that can be used to overcome potential shortcomings might be the inactivation of these microorganisms by 5-aminolevulinic acid (5-ALA) or 5-ALA derivative-mediated photodynamic therapy (PDT). 5-ALA has no photoactive properties, but when it is given exogenously, it acts as a precursor of photosensitive porphyrins predominantly in tissues or organisms that are characterized by a high metabolic turnover, such as tumors, macrophages, and bacteria. However, the weak ability of 5-ALA to cross biological barriers has led to the introduction of more lipophilic derivatives, such as methyl aminolevulinate or hexyl aminolevulinate, which display improved capacities to reach the cytoplasm. Starting from the hypothesis that more lipophilic compounds carrying only a permanent positive charge under physiological conditions may more easily cross the bacterial multilayer barrier, we have tested the efficacies of some 5-ALA n-alkyl esters for the inactivation of bacteria. For this purpose, different bacterial strains were incubated with 5-ALA or its corresponding esters of different lipophilicities. Then, the bacteria were irradiated with light and the numbers of CFU post-PDT were counted and compared to those for the controls, which were kept in the dark. Furthermore, the total amount of accumulated porphyrins was quantified by high-pressure liquid chromatography analysis. In our studies, analysis of the bacterial extracts revealed the presence of all the porphyrins involved in heme biosynthesis, from uroporphyrin to protoporphyin IX. The efficacy of bacterial inactivation was a function of the total amount of porphyrins produced, independently of their nature. The 5-ALA methyl and butyl esters were the most effective compounds with respect to the photodynamic inactivation of bacteria. We observed significant differences in terms of the optimal drug concentration, bactericidal activities, and porphyrin production.
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Angeli, Andrea, Victor Kartsev, Anthi Petrou, Mariana Pinteala, Roman M. Vydzhak, Svitlana Y. Panchishin, Volodymyr Brovarets et al. „New Sulfanilamide Derivatives Incorporating Heterocyclic Carboxamide Moieties as Carbonic Anhydrase Inhibitors“. Pharmaceuticals 14, Nr. 8 (23.08.2021): 828. http://dx.doi.org/10.3390/ph14080828.
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Carbonic Anhydrases (CAs) are ubiquitous metalloenzymes involved in several disease conditions. There are 15 human CA (hCA) isoforms and their high homology represents a challenge for the discovery of potential drugs devoid of off-target side effects. For this reason, many synthetic and pharmacologic research efforts are underway to achieve the full pharmacological potential of CA modulators of activity. We report here a novel series of sulfanilamide derivatives containing heterocyclic carboxamide moieties which were evaluated as CA inhibitors against the physiological relevant isoforms hCA I, II, IX, and XII. Some of them showed selectivity toward isoform hCA II and hCA XII. Molecular docking was performed for some of these compounds on isoforms hCA II and XII to understand the possible interaction with the active site amino acid residues, which rationalized the reported inhibitory activity.
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Al Mijan, Mohammad, Woo-Jin Sim und Tae-Gyu Lim. „Physiological Effects of Green-Colored Food-Derived Bioactive Compounds on Cancer“. Applied Sciences 11, Nr. 23 (29.11.2021): 11288. http://dx.doi.org/10.3390/app112311288.
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Green-colored foods, such as broccoli, sprouts, soybean, and green leafy vegetables are considered one of the representative healthy foods for containing various functional ingredients that can combat chronic diseases, including diabetes, obesity, and cancer. Herein, we reviewed the anti-cancer activities and the underlying mechanisms of some important bioactive compounds, such as sulforaphane, catechins, chlorophyll, isoflavone, indole dervatives, and lutein, present in green-colored foods. In vivo and clinical studies suggest that sulforaphane, a sulfur-containing compound found in cruciferous vegetables, can ameliorate prostate and breast cancer symptoms by arresting cell-cycle progression and modulating Ki67 and HDAC expression. A green tea compound, known as epigallocatechin-3-gallate (EGCG), has shown remarkable anti-cancer effects against prostate cancer and lung adenocarcinoma in human trials through its antioxidative defense and immunomodulatory functions. Chlorophyll, a natural pigment found in all green plants, can regulate multiple cancer-related genes, including cyclin D1, CYP1A, CYP1B1, and p53. Epidemiological studies indicate that chlorophyll can substantially reduce aflatoxin level and can mitigate colon cancer in human subjects. Remarkably, the consumption of soy isoflavone has been found to be associated with the lower incidence and mortality of breast and prostate cancers in East Asia and in Canada. In vivo and in vitro data point out that isoflavone has modulatory effects on estrogen and androgen signaling pathways and the expression of MAPK, NfκB, Bcl-2, and PI3K/AKT in different cancer models. Other green food bioactive compounds, such as indole derivatives and lutein, also exhibited suppressing effects in rodent models of lung, liver, stomach, cervical, and prostate cancers. In addition, some micronutrients, such as folate, riboflavin, retinoic acid, and vitamin D3 present in green foods, also showed potential cancer suppressing effects. Taken together, these data suggest potential chemopreventive functions of the bioactive compounds from green-colored foods. This paper could be beneficial for further research on the anti-carcinogenic effects of green-colored food-derived compounds, in order to develop green chemotherapeutics for cancers.
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Małodobra-Mazur, Małgorzata, Dominika Lewoń, Aneta Cierzniak, Marta Okulus und Anna Gliszczyńska. „Phospholipid Derivatives of Cinnamic Acid Restore Insulin Sensitivity in Insulin Resistance in 3T3-L1 Adipocytes“. Nutrients 13, Nr. 10 (15.10.2021): 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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Ali, Md Sarafat, und Kwang-Hyun Baek. „Jasmonic Acid Signaling Pathway in Response to Abiotic Stresses in Plants“. International Journal of Molecular Sciences 21, Nr. 2 (17.01.2020): 621. http://dx.doi.org/10.3390/ijms21020621.
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Plants as immovable organisms sense the stressors in their environment and respond to them by means of dedicated stress response pathways. In response to stress, jasmonates (jasmonic acid, its precursors and derivatives), a class of polyunsaturated fatty acid-derived phytohormones, play crucial roles in several biotic and abiotic stresses. As the major immunity hormone, jasmonates participate in numerous signal transduction pathways, including those of gene networks, regulatory proteins, signaling intermediates, and proteins, enzymes, and molecules that act to protect cells from the toxic effects of abiotic stresses. As cellular hubs for integrating informational cues from the environment, jasmonates play significant roles in alleviating salt stress, drought stress, heavy metal toxicity, micronutrient toxicity, freezing stress, ozone stress, CO2 stress, and light stress. Besides these, jasmonates are involved in several developmental and physiological processes throughout the plant life. In this review, we discuss the biosynthesis and signal transduction pathways of the JAs and the roles of these molecules in the plant responses to abiotic stresses.
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Bayer, Ilker S. „Hyaluronic Acid and Controlled Release: A Review“. Molecules 25, Nr. 11 (06.06.2020): 2649. http://dx.doi.org/10.3390/molecules25112649.
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Hyaluronic acid (HA) also known as hyaluronan, is a natural polysaccharide—an anionic, non-sulfated glycosaminoglycan—commonly found in our bodies. It occurs in the highest concentrations in the eyes and joints. Today HA is used during certain eye surgeries and in the treatment of dry eye disease. It is a remarkable natural lubricant that can be injected into the knee for patients with knee osteoarthritis. HA has also excellent gelling properties due to its capability to bind water very quickly. As such, it is one the most attractive controlled drug release matrices and as such, it is frequently used in various biomedical applications. Due to its reactivity, HA can be cross-linked or conjugated with assorted bio-macromolecules and it can effectively encapsulate several different types of drugs, even at nanoscale. Moreover, the physiological significance of the interactions between HA and its main membrane receptor, CD44 (a cell-surface glycoprotein that modulates cell–cell interactions, cell adhesion and migration), in pathological processes, e.g., cancer, is well recognized and this has resulted in an extensive amount of studies on cancer drug delivery and tumor targeting. HA acts as a therapeutic but also as a tunable matrix for drug release. Thus, this review focuses on controlled or sustained drug release systems assembled from HA and its derivatives. More specifically, recent advances in controlled release of proteins, antiseptics, antibiotics and cancer targeting drugs from HA and its derivatives were reviewed. It was shown that controlled release from HA has many benefits such as optimum drug concentration maintenance, enhanced therapeutic effects, improved efficiency of treatment with less drug, very low or insignificant toxicity and prolonged in vivo release rates.
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Lin, Wei-Jiun, Han-Chen Ho, Sheng-Chang Chu und Jui-Yu Chou. „Effects of auxin derivatives on phenotypic plasticity and stress tolerance in five species of the green alga Desmodesmus (Chlorophyceae, Chlorophyta)“. PeerJ 8 (09.03.2020): e8623. http://dx.doi.org/10.7717/peerj.8623.
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Green microalgae of the genus Desmodesmus are characterized by a high degree of phenotypic plasticity (i.e. colony morphology), allowing them to be truly cosmopolitan and withstand environmental fluctuations. This flexibility enables Desmodesmus to produce a phenotype–environment match across a range of environments broader compared to algae with more fixed phenotypes. Indoles and their derivatives are a well-known crucial class of heterocyclic compounds and are widespread in different species of plants, animals, and microorganisms. Indole-3-acetic acid (IAA) is the most common, naturally occurring plant hormone of the auxin class. IAA may behave as a signaling molecule in microorganisms, and the physiological cues of IAA may also trigger phenotypic plasticity responses in Desmodesmus. In this study, we demonstrated that the changes in colonial morphs (cells per coenobium) of five species of the green alga Desmodesmus were specific to IAA but not to the chemically more stable synthetic auxins, naphthalene-1-acetic acid and 2,4-dichlorophenoxyacetic acid. Moreover, inhibitors of auxin biosynthesis and polar auxin transport inhibited cell division. Notably, different algal species (even different intraspecific strains) exhibited phenotypic plasticity different to that correlated to IAA. Thus, the plasticity involving individual-level heterogeneity in morphological characteristics may be crucial for microalgae to adapt to changing or novel conditions, and IAA treatment potentially increases the tolerance of Desmodesmus algae to several stress conditions. In summary, our results provide circumstantial evidence for the hypothesized role of IAA as a diffusible signal in the communication between the microalga and microorganisms. This information is crucial for elucidation of the role of plant hormones in plankton ecology.
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Maru, J. J., G. R. Patel und Rakesh Yadav. „Spectral and Microbial Studies of some Newly Synthesized Schiff Base Derivatives of 2-(1H-Benzo[d]Oxazole-2-ylthio)-N-(4-Acetylphenyl)Acetamide“. International Letters of Chemistry, Physics and Astronomy 44 (14.01.2015): 57–65. http://dx.doi.org/10.56431/p-6c3m08.
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The author has synthesized novel biological active compounds by condensation of N-(4-Acetyl-phenyl)-2-(benzooxazol-2-ylsulfanyl)-acetamide with defferent substituted of acid hydrazide in the presence of catalytic amount of acetic acid. A series of benzoxazole having azomethine group were confirmed by various spectroscopic techniques. The new compounds were examined for antibacterial effects again different strain of bacteria and antifungal were high to lowest Minimum Inhibition Concentration (MIC) values.
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Avcu, Ferit, Burak Cem Soner, Oguzhan Yildiz, Kamile Ozturk, Pinar Elci, Meral Sarper und Ali Ugur Ural. „EFFECTS of Zoledronic ACID On eNOS Exppression and Vascular Contractility IN Rat Aorta“. Blood 116, Nr. 21 (19.11.2010): 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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Del Buono, Daniele, Francesca Luzi und Debora Puglia. „Lignin Nanoparticles: A Promising Tool to Improve Maize Physiological, Biochemical, and Chemical Traits“. Nanomaterials 11, Nr. 4 (26.03.2021): 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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El-Nagar, Asmaa, Abdelnaser A. Elzaawely, Naglaa A. Taha und Yasser Nehela. „The Antifungal Activity of Gallic Acid and Its Derivatives against Alternaria solani, the Causal Agent of Tomato Early Blight“. Agronomy 10, Nr. 9 (16.09.2020): 1402. http://dx.doi.org/10.3390/agronomy10091402.
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Tomato (Solanum lycopersicum L.) is among the most important vegetable crops worldwide. Early blight disease, caused by Alternaria solani, is a destructive foliar disease of tomato and other Solanaceae species. Herein, we investigated the in vitro antifungal properties of gallic acid and two of its derivatives (syringic and pyrogallic acids) against A. solani during 2019 and 2020 seasons. The physiological and biochemical effects of these compounds on infected tomato plants were also investigated using the whole plant bioassay. The in vitro investigation showed that all tested compounds showed fungistatic action and inhibited the mycelial radial growth of A. solani in a dose-dependent manner. In two separate pot-experiments, those compounds efficiently suppressed the development of the disease symptoms and area under disease progress curve (AUDPC), without any phytotoxic effects on the treated tomato plants. Additionally, all tested compounds positively enhanced the biochemical traits of treated plants including the chlorophyll content, the total soluble phenolics, the total soluble flavonoids, and the enzymatic activities of catalase, peroxidase, and polyphenol oxidase during 2019 and 2020 seasons. Moreover, the treatment with gallic acid and its derivatives significantly increased all yield components of A. solani-infected tomato plants such as the total number of flowers and fruits, and the fruit yield for each tomato plant in both experiments. Considering the fungitoxicity of phenolic acids against A. solani with no phytotoxicity on treated tomato plants, we believe that gallic acid and its derivatives might be a sustainable eco-friendly control strategy to reduce the usage of chemical fungicides partially or entirely against A. solani particularly, and fungal diseases in general.
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Khalaf, Reema Abu, Ghassan Abu Sheikha, Mahmoud Al-Sha'er und 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, Nr. 1 (29.11.2013): 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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Villacorta, Luis, Francisco J. Schopfer, Jifeng Zhang, Bruce A. Freeman und Y. Eugene Chen. „PPARγ and its ligands: therapeutic implications in cardiovascular disease“. Clinical Science 116, Nr. 3 (08.01.2009): 205–18. http://dx.doi.org/10.1042/cs20080195.
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The relevance of PPARγ (peroxisome-proliferator-activated receptor γ) as an important therapeutic target for the treatment of diabetes arises from its hypoglycaemic effects in diabetic patients and also from the critical role in the regulation of cardiovascular functions. From a clinical perspective, differences between current FDA (Food and Drug Administration)-approved PPARγ drugs have been observed in terms of atherosclerosis and cardiac and stroke events. The adverse effects of PPARγ-specific treatments that hamper their cardiovascular protective roles, affirm the strong need to evaluate the efficacy of the current drugs. Therefore active research is directed towards high-throughput screening and pharmacological testing of a plethora of newly identified natural or synthetic compounds. In the present review we describe the rationale behind drug design strategies targeting PPARγ, based on current knowledge regarding the effects of such drugs in experimental animal models, as well as in clinical practice. Regarding endogenous PPARγ ligands, several fatty acid derivatives bind PPARγ with different affinities, although the physiological relevance of these interactions is not always evident. Recently, NO-derived unsaturated fatty acids were found to be potent agonists of PPARs, with preferential affinity for PPARγ, compared with oxidized fatty acid derivatives. Nitroalkenes exert important bioactivities of relevance for the cardiovascular system including anti-inflammatory and antiplatelet actions, and are important mediators of vascular tone. A new generation of insulin sensitizers with PPARγ function for the treatment of diabetes may serve to limit patients from the increased cardiovascular burden of this disease.
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Szelest, Monika, Katarzyna Walczak und Tomasz Plech. „A New Insight into the Potential Role of Tryptophan-Derived AhR Ligands in Skin Physiological and Pathological Processes“. International Journal of Molecular Sciences 22, Nr. 3 (22.01.2021): 1104. http://dx.doi.org/10.3390/ijms22031104.
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The aryl hydrocarbon receptor (AhR) plays a crucial role in environmental responses and xenobiotic metabolism, as it controls the transcription profiles of several genes in a ligand-specific and cell-type-specific manner. Various barrier tissues, including skin, display the expression of AhR. Recent studies revealed multiple roles of AhR in skin physiology and disease, including melanogenesis, inflammation and cancer. Tryptophan metabolites are distinguished among the groups of natural and synthetic AhR ligands, and these include kynurenine, kynurenic acid and 6-formylindolo[3,2-b]carbazole (FICZ). Tryptophan derivatives can affect and regulate a variety of signaling pathways. Thus, the interest in how these substances influence physiological and pathological processes in the skin is expanding rapidly. The widespread presence of these substances and potential continuous exposure of the skin to their biological effects indicate the important role of AhR and its ligands in the prevention, pathogenesis and progression of skin diseases. In this review, we summarize the current knowledge of AhR in skin physiology. Moreover, we discuss the role of AhR in skin pathological processes, including inflammatory skin diseases, pigmentation disorders and cancer. Finally, the impact of FICZ, kynurenic acid, and kynurenine on physiological and pathological processes in the skin is considered. However, the mechanisms of how AhR regulates skin function require further investigation.
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Reang, Jurnal, Prabodh Chander Sharma, Vijay Kumar Thakur und Jaseela Majeed. „Understanding the Therapeutic Potential of Ascorbic Acid in the Battle to Overcome Cancer“. Biomolecules 11, Nr. 8 (31.07.2021): 1130. http://dx.doi.org/10.3390/biom11081130.
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Cancer, a fatal disease, is also one of the main causes of death worldwide. Despite various developments to prevent and treat cancer, the side effects of anticancer drugs remain a major concern. Ascorbic acid is an essential vitamin required by our bodies for normal physiological function and also has antioxidant and anticancer activity. Although the body cannot synthesize ascorbic acid, it is abundant in nature through foods and other natural sources and also exists as a nutritional food supplement. In anticancer drug development, ascorbic acid has played an important role by inhibiting the development of cancer through various mechanisms, including scavenging reactive oxygen species (ROS), selectively producing ROS and encouraging their cytotoxicity against tumour cells, preventing glucose metabolism, serving as an epigenetic regulator, and regulating the expression of HIF in tumour cells. Several ascorbic acid analogues have been produced to date for their anticancer and antioxidant activity. The current review summarizes the mechanisms behind ascorbic acid's antitumor activity, presents a compilation of its derivatives and their biological activity as anticancer agents, and discusses delivery systems such as liposomes, nanoparticles against cancer, and patents on ascorbic acid as anticancer agents.
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Salachna, Piotr, und Anna Pietrak. „Evaluation of Carrageenan, Xanthan Gum and Depolymerized Chitosan Based Coatings for Pineapple Lily Plant Production“. Horticulturae 7, Nr. 2 (29.01.2021): 19. http://dx.doi.org/10.3390/horticulturae7020019.
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Some natural polysaccharides and their derivatives are used in horticulture to stimulate plant growth. This study investigated the effects of coating bulbs with carrageenan-depolymerized chitosan (C-DCh) or xanthan-depolymerized chitosan (X-DCh) on growth, flowering, and bulb yield as well as physiological and biochemical attributes of pineapple lily (Eucomis autumnalis). The results showed that treatment with C-DCh or X-DCh significantly increased all growth parameters, bulb yield, greenness index, stomatal conductance, total N, total K, and total sugar content of bulbs and accelerated anthesis as compared with untreated bulbs. The positive impact of coatings on plant growth and physiological attributes depended on the type of biopolymer complexes. The X-DCh treatment exhibited the greatest plant height, fresh weight, daughter bulb number, greenness index, stomatal conductance, total N, K, and sugar content. However, this treatment induced a significant decrease in L-ascorbic acid, total polyphenol content and antioxidant activity. Overall, the results of this study indicated high suitability of C-DCh and X-DCh as bulb coatings for pineapple lily plant production.
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Ramabulana, Anza-Tshilidzi, Paul A. Steenkamp, Ntakadzeni E. Madala und Ian A. Dubery. „Profiling of Altered Metabolomic States in Bidens pilosa Leaves in Response to Treatment by Methyl Jasmonate and Methyl Salicylate“. Plants 9, Nr. 10 (27.09.2020): 1275. http://dx.doi.org/10.3390/plants9101275.
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Bidens pilosa (Asteraceae) is an edible medicinal plant with many bioactivities reported to have a health-beneficial role in controling various diseases. Though B. pilosa contain a diverse array of natural products, these are produced in relatively low concentrations. A possible way to enhance secondary metabolite production can be through the use of elicitors. Here, the effects of exogenous treatments with two signal molecules—methyl jasmonate (MeJA) and methyl salicylate (MeSA)—on the metabolomic profiles of B. pilosa leaves were investigated. Plants were treated with 0.5 mM of MeJA or MeSA and harvested at 12 h and 24 h. Metabolites were extracted with methanol and separated on an ultra-high performance liquid chromatography system hyphenated to quadrupole time-of-flight mass spectrometry detection. Data was subjected to multivariate statistical analysis and modeling for annotation of metabolites. Hydroxycinnamic acid (HCA) derivatives, such as caffeoylquinic acids (CQAs), tartaric acid esters (chicoric acid and caftaric acid), chalcones, and flavonoids were identified as differentially regulated. The altered metabolomes in response to MeSA and MeJA overlapped to a certain extent, suggestive of a cross-talk between signaling and metabolic pathway activation. Moreover, the perturbation of isomeric molecules, especially the cis geometrical isomers of HCA derivatives by both treatments, further point to the biological significance of these molecules during physiological responses to stress. The results highlight the possibility of using phytohormones to enhance the accumulation of bioactive secondary metabolites in this plant.
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Katagi, Manjunatha S., Jennifer Fernandes, Shivalingrao Mamledesai, Sujatha M.L., Rekha A. und Girish Bolakatti. „Schiff Base Oxime Derivatives Reactivate Chlorpyrifos-induced Acetylcholinesterase Inhibition“. INNOSC Theranostics and Pharmacological Sciences 2, Nr. 1 (02.07.2019): 12–16. http://dx.doi.org/10.26689/itps.v2i1.499.
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Background: The biological effects of organophosphorus (OP) compounds are connected with the irreversible inhibition of acetylcholinesterase (AChE), an important neuromediator acetylcholine (ACh) splitting enzyme in the human body at the synaptic clefts. Due to this inhibition, AChE is unable to fulfil its physiological function resulting in the accumulation of ACh, which, in turn over stimulates the parasympathetic nerve receptors, and causes fatal cholinergic crisis.
Objective: The objective of the study was to synthesize a series of Schiff base oximes and to assess their evaluating for their in vitro reactivating potency against chlorpyrifos inhibited AChE.
Methods: The amino group of 4-amino acetophenone exploited by treating with substituted benzaldehyde in the presence of glacial acetic acid to form Schiff base (1a-1f). The titled compounds (2a-2f) were prepared by treating Schiff base with hydroxylamine hydrochloride in the presence of alcohol. Through structural and spectral analysis, the structure of compounds was confirmed. The synthesized compounds were evaluated for their reactivation efficacy against chlorpyrifos-inhibited rat brain AChE by Ellman's method.
Results: The pralidoxime (2-PAM) was potent reactivation against chlorpyrifos-inhibited AChE at the concentration tested (0.001 M). In this case, the compounds 2a (40.4%, 60 min) and 2d (37.9%, 60 min) showed promising reactivation as compared to 2-PAM (40.6%, 60min) against chlorpyrifos-inhibited AChE.
Conclusion: Compounds having chloro (2a) and nitro (2d) substitution on 4th position gave good activity against chlorpyrifos-inhibited AChE. Moreover, these Schiff base oximes seem to be very promising because of their sufficient reactivation strength at lower concentration (10-3 M).
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Serreli, Gabriele, Micaela Rita Naitza, Sonia Zodio, Vera Piera Leoni, Martina Spada, Maria Paola Melis, Anna Boronat und Monica Deiana. „Ferulic Acid Metabolites Attenuate LPS-Induced Inflammatory Response in Enterocyte-like Cells“. Nutrients 13, Nr. 9 (10.09.2021): 3152. http://dx.doi.org/10.3390/nu13093152.
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Ferulic acid (FA) is a polyphenol pertaining to the class of hydroxycinnamic acids present in numerous foods of a plant origin. Its dietary consumption leads to the formation of several phase I and II metabolites in vivo, which represent the largest amount of ferulates in the circulation and in the intestine in comparison with FA itself. In this work, we evaluated their efficacy against the proinflammatory effects induced by lipopolysaccharide (LPS) in intestinal Caco-2 cell monolayers, as well as the mechanisms underlying their protective action. LPS-induced overexpression of proinflammatory enzymes such as inducible nitric oxide synthase (iNOS) and the consequent hyperproduction of nitric oxide (NO) and cyclic guanosine monophosphate (cGMP) were limited by physiological relevant concentrations (1 µM) of FA, its derivatives isoferulic acid (IFA) and dihydroferulic acid (DHFA), and their glucuronidated and sulfated metabolites, which acted upstream by limiting the activation of MAPK p38 and ERK and of Akt kinase, thus decreasing the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-ĸB) translocation into the nucleus. Furthermore, the compounds were found to promote the expression of Nrf2, which may have contributed to the downregulation of NF-ĸB activity. The overall data show that phase I/II metabolites retain the efficacy of their dietary free form in contrasting inflammatory response.
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Holeček, Milan. „Histidine in Health and Disease: Metabolism, Physiological Importance, and Use as a Supplement“. Nutrients 12, Nr. 3 (22.03.2020): 848. http://dx.doi.org/10.3390/nu12030848.
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L-histidine (HIS) is an essential amino acid with unique roles in proton buffering, metal ion chelation, scavenging of reactive oxygen and nitrogen species, erythropoiesis, and the histaminergic system. Several HIS-rich proteins (e.g., haemoproteins, HIS-rich glycoproteins, histatins, HIS-rich calcium-binding protein, and filaggrin), HIS-containing dipeptides (particularly carnosine), and methyl- and sulphur-containing derivatives of HIS (3-methylhistidine, 1-methylhistidine, and ergothioneine) have specific functions. The unique chemical properties and physiological functions are the basis of the theoretical rationale to suggest HIS supplementation in a wide range of conditions. Several decades of experience have confirmed the effectiveness of HIS as a component of solutions used for organ preservation and myocardial protection in cardiac surgery. Further studies are needed to elucidate the effects of HIS supplementation on neurological disorders, atopic dermatitis, metabolic syndrome, diabetes, uraemic anaemia, ulcers, inflammatory bowel diseases, malignancies, and muscle performance during strenuous exercise. Signs of toxicity, mutagenic activity, and allergic reactions or peptic ulcers have not been reported, although HIS is a histamine precursor. Of concern should be findings of hepatic enlargement and increases in ammonia and glutamine and of decrease in branched-chain amino acids (valine, leucine, and isoleucine) in blood plasma indicating that HIS supplementation is inappropriate in patients with liver disease.
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Srovnalova, Alzbeta, Sona Gurska, Milan Urban, Jan Sarek, Jiri Rehulka, Petr Dzubak und 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, Nr. 12_Supplement (15.06.2022): 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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Ferrari, Nicoletta, Magnus Pfahl und Giovanni Levi. „Retinoic Acid Receptor γ1 (RARγ1) Levels Control RARβ2 Expression in SK-N-BE2(c) Neuroblastoma Cells and Regulate a Differentiation-Apoptosis Switch“. Molecular and Cellular Biology 18, Nr. 11 (01.11.1998): 6482–92. http://dx.doi.org/10.1128/mcb.18.11.6482.
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ABSTRACT Vitamin A and its derivatives (retinoids) have profound effects on the proliferation and differentiation of many cell types and are involved in a diverse array of developmental and physiological regulatory processes, including those responsible for the development of the mature nervous system. Retinoid signals are mediated by retinoic acid (RA) receptors (RARs) and retinoid X receptors (RXRs), which show distinct spatio-temporal patterns of expression during development and in adult tissues. We have used SK-N-BE2(c) neuroblastoma cells to study the effects of reciprocal regulation of expression of various RARs. We show that in these cells RARγ1 acts as a repressor of RARβ2 transcription in the absence of an agonist. In the presence of RA, the expression of RARγ1 is reduced and that of RARβ2 is induced. Overexpression of RARγ1 neutralizes the effects of RA on RARβ induction. Expression of an RARγ1-specific antisense construct leads to the constitutive expression of RARβ2. Although both overexpression of RARγ1 and its reduction of expression can result in inhibition of cell proliferation, they induce different morphological changes. Reduction of RARγ1 (and induction of RARβ) leads to increased apoptosis, whereas RARγ1 overexpression leads to differentiation in the absence of apoptosis. Thus, RARγ1 appears to control a differentiation-apoptosis switch in SK-N-BE2(c) neuroblastoma cells.
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Arróniz-Crespo, María, Encarnación Núñez-Olivera, Javier Martínez-Abaigar, Hans Becker, Jochen Scher, Josef Zapp, Rafael Tomás und Nathalie Beaucourt. „Physiological changes and UV protection in the aquatic liverwort Jungermannia exsertifolia subsp. cordifolia along an altitudinal gradient of UV-B radiation“. Functional Plant Biology 33, Nr. 11 (2006): 1025. http://dx.doi.org/10.1071/fp06096.
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Here we report the effects of a natural altitudinal gradient of UV-B radiation, from 1140 to 1816 m altitude, on the physiology of the aquatic liverwort Jungermannia exsertifolia Steph. subsp. cordifolia (Dumort.) Váña collected in mountain streams. Photosynthetic pigments, net photosynthesis and dark respiration rates, chlorophyll fluorescence, protein concentration, sclerophylly, and UV-absorbing compounds [both global UV absorbance of methanol-extractable UV-absorbing compounds (MEUVAC) and concentrations of five individual compounds] were measured. Two new caffeic acid derivatives were discovered: 5″-(7″,8″-dihydroxycoumaroyl)-2-caffeoylmalic acid and 5″-(7″,8″-dihydroxy-7-O-β-glucosyl-coumaroyl)-2-caffeoylmalic acid, whereas three additional compounds were already known in other species: p-coumaroylmalic acid, phaselic acid (both compounds in their cis- and trans- forms) and feruloylmalic acid. Most physiological variables changed considerably along the altitudinal gradient, but only six showed significant linear relationships with altitude: MEUVAC levels, the concentrations of the two new secondary compounds, the maximal apparent electron transport rate through PSII (ETRmax) and the maximal non-photochemical quenching (NPQmax) increased with altitude, whereas photoinhibition percentage decreased. A principal components analysis (PCA) was conducted to rank the values of the physiological and ecological variables obtained along the altitudinal transect, showing that those variables correlated with altitude were responsible for the ordination of the sampling points. The liverwort was not adversely affected by the changing conditions along the altitudinal gradient and, in particular, by the increasing UV-B irradiance, probably because the characteristics shown by high-altitude populations may confer tolerance to high UV-B levels. The response to UV-B of the two new compounds suggests that they could be used as indicators of the spatial changes in UV-B radiation.
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Li, Tong, Ruiguo Wang und Peilong Wang. „The Development of an Ultra-Performance Liquid Chromatography–Tandem Mass Spectrometry Method for Biogenic Amines in Fish Samples“. Molecules 28, Nr. 1 (26.12.2022): 184. http://dx.doi.org/10.3390/molecules28010184.
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Biogenic amines (BAs) are a group of substances that are formed from amino acids by decarboxylation or amination and transamination of aldehydes and ketones. They may have either an aliphatic, aromatic, or heterocyclic structure. Their quantity determines their effects and optimum amounts are essential for physiological functions, but excess BAs causes various toxic effects throughout the human body. In our study, to rapidly determine 14 BAs (histamine, tyramine, dopamine, tryptamine, serotonin, putrescine, spermine, spermidine, octopamine, benzylamine, 1-Phenylethanamine, cadaverine, 2-Phenethylamine, and agmatine) in real fish samples, an ultra-performance liquid chromatography–tandem mass spectrometry method was established. The fish sample was extracted by acetonitrile with 0.1% formic acid and stable biogenic amine derivatives could be obtained by benzoyl chloride derivatization with a shorter reaction time. The method showed good linearity with a linear range of 3–4 orders of magnitude and regression coefficients ranging from 0.9961 to 0.9999. The calculated LODs ranged from 0.1 to 20 nM and the LOQs ranged from 0.3 to 60 nM. Satisfactory recovery was obtained from 84.6% to 119.3%. The proposed method was employed to determine the concentration levels of biogenic amine derivatives in different fish. The results indicated that this method was suitable for the analysis of biogenic amines.
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Krzyżanowska-Kowalczyk, Justyna, Mariusz Kowalczyk, Michał B. Ponczek, Łukasz Pecio, Paweł Nowak und Joanna Kolodziejczyk-Czepas. „Pulmonaria obscura and Pulmonaria officinalis Extracts as Mitigators of Peroxynitrite-Induced Oxidative Stress and Cyclooxygenase-2 Inhibitors–In Vitro and In Silico Studies“. Molecules 26, Nr. 3 (26.01.2021): 631. http://dx.doi.org/10.3390/molecules26030631.
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The Pulmonaria species (lungwort) are edible plants and traditional remedies for different disorders of the respiratory system. Our work covers a comparative study on biological actions in human blood plasma and cyclooxygenase-2 (COX-2) -inhibitory properties of plant extracts (i.e., phenolic-rich fractions) originated from aerial parts of P. obscura Dumort. and P. officinalis L. Phytochemical profiling demonstrated the abundance of phenolic acids and their derivatives (over 80% of the isolated fractions). Danshensu conjugates with caffeic acid, i.e., rosmarinic, lithospermic, salvianolic, monardic, shimobashiric and yunnaneic acids were identified as predominant components. The examined extracts (1–100 µg/mL) partly prevented harmful effects of the peroxynitrite-induced oxidative stress in blood plasma (decreased oxidative damage to blood plasma components and improved its non-enzymatic antioxidant capacity). The cellular safety of the extracts was confirmed in experimental models of blood platelets and peripheral blood mononuclear cells. COX-2 inhibitor screening evidently suggested a stronger activity of P. officinalis (IC50 of 13.28 and 7.24 µg/mL, in reaction with synthetic chromogen and physiological substrate (arachidonic acid), respectively). In silico studies on interactions of main components of the Pulmonaria extracts with the COX-2 demonstrated the abilities of ten compounds to bind with the enzyme, including rosmarinic acid, menisdaurin, globoidnan A and salvianolic acid H.
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Chuyan, E. N., I. S. Mironyuk, M. Yu Ravaeva, T. V. Grishina, I. V. Cheretaev und S. E. Chernobai. „Changes in micro- and central hemodynamic parameters in rats under the action of acetylsalicylic acid and its coordination compounds with metals“. Regional blood circulation and microcirculation 20, Nr. 4 (10.01.2022): 75–86. http://dx.doi.org/10.24884/1682-6655-2021-20-4-75-86.
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Introduction. The cutaneous blood circulation is a representative model both for studying the mechanisms of vascular diseases and for assessing the current state of the central hemodynamics in preclinical researches of various chemical compounds. Aim. The changes in the parameters of cutaneous microcirculation and central hemodynamics (heart rate and blood pressure) were studied in the animals under the action of acetylsalicylic acid and its coordination compounds with cations of cobalt, zinc, nickel and manganese at a dose of 20 mg/kg. Materials and methods. The research was conducted using the laser Doppler flowmetry method on the Lazma-MC device (manufactured by RPE Lazma, Russia) and the NIBP200A system (Biopac Systems, Inc., USA). Results. The study shows that animals develop bradycardia, and microcirculation and central hemodynamics change in two ways after the introduction of acetylsalicylic acid and the tested metal salicylates. These ways are hypotension-related hyperemia (acetylsalicylic acid and cobalt salicylate) and ischemia (zinc, nickel and manganese salicylates) associated with hypertension. Conclusion. The obtained data confirm the cardiotropic activity of new coordination compounds. The data also prove that the generation of the acetylsalicylic acid derivatives allows enhancing it physiological effects, as well as obtaining completely new molecules. The molecules are different from the precursor one and are necessary for the production of effective drugs.
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Jiang, Ni-Hao, und 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, Nr. 7 (27.03.2021): 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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Dougkas, Anestis, Christopher K. Reynolds, Ian D. Givens, Peter C. Elwood und Anne M. Minihane. „Associations between dairy consumption and body weight: a review of the evidence and underlying mechanisms“. Nutrition Research Reviews 24, Nr. 1 (15.02.2011): 72–95. http://dx.doi.org/10.1017/s095442241000034x.
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As the incidence of obesity is reaching ‘epidemic’ proportions, there is currently widespread interest in the impact of dietary components on body-weight and food intake regulation. The majority of data available from both epidemiological and intervention studies provide evidence of a negative but modest association between milk and dairy product consumption and BMI and other measures of adiposity, with indications that higher intakes result in increased weight loss and lean tissue maintenance during energy restriction. The purported physiological and molecular mechanisms underlying the impact of dairy constituents on adiposity are incompletely understood but may include effects on lipolysis, lipogeneis and fatty acid absorption. Furthermore, accumulating evidence indicates an impact of dairy constituents, in particular whey protein derivatives, on appetite regulation and food intake. The present review summarises available data and provides an insight into the likely contribution of dairy foods to strategies aimed at appetite regulation, weight loss or the prevention of weight gain.
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Liang, Xin, Ruyi Qian, Dan Wang, Lijuan Liu, Chengliang Sun und Xianyong Lin. „Lipid-Derived Aldehydes: New Key Mediators of Plant Growth and Stress Responses“. Biology 11, Nr. 11 (29.10.2022): 1590. http://dx.doi.org/10.3390/biology11111590.
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Aldehydes, derivatives of lipids, are ubiquitously produced through non-enzymatic and enzymatic pathways in higher plants and participate in many physiological and biological processes. Increasing evidence demonstrates that aldehydes are involved in plants response to many abiotic stresses, such as light, drought, heat and nutrient deficiency. In plant cells, endogenously triggered or exogenously applied high concentrations of aldehydes can damage proteins and nucleic acid, disturb redox homeostasis, and consequently inhibit plant growth; therefore, they are considered cytotoxins. Aldehyde levels are also used as biomarkers to evaluate the health status of plants. Further genetic research shows that several enzymes have strong capacities to detoxify these electrophilic aldehydes. Small molecules, such as carnosine and glutathione, also exhibit the ability to scavenge aldehydes, effectively promoting plant growth. Recently, increasing evidence has shown that certain aldehydes at certain concentrations can upregulate survival genes, activate antioxidant responses, increase defense against pathogens and stimulate plant growth. This review summarizes recent studies of lipid-derived aldehydes in higher plants, mainly focusing on the generation pathway, toxic effects, and detoxification strategies. In addition, the signaling effects of aldehydes in plants are also discussed.
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Hussain, M., Manuel Reigosa und Adele Muscolo. „Carbon (δ13C) and Nitrogen (δ15N) Stable Isotope Composition Provide New Insights into Phenotypic Plasticity in Broad Leaf Weed Rumex acetosa under Allelochemical Stress“. Molecules 23, Nr. 10 (25.09.2018): 2449. http://dx.doi.org/10.3390/molecules23102449.
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Phenolic compounds, hydroquinone and cinnamic acid derivatives have been identified as major allelochemicals with known phytotoxicity from allelopathic plant Acacia melanoxylon R. Br. Several phenolic compounds such as ferulic acid (FA), p-hydroxybenzoic acid (pHBA) and flavonoid (rutin, quercetin) constituents occur in the phyllodes and flowers of A. melanoxylon and have demonstrated inhibitory effects on germination and physiological characteristics of lettuce and perennial grasses. However, to date, little is known about the mechanisms of action of these secondary metabolites in broad-leaved weeds at ecophysiological level. The objective of this study was to determine the response of Rumex acetosa carbon isotope composition and other physiological parameters to the interaction of plant secondary metabolites (PSM) (FA and pHBA) stress and the usefulness of carbon isotope discrimination (Δ13C) as indicative of the functional performance of intrinsic water use efficiency (iWUE) at level of plant leaf. R. acetosa plant were grown under greenhouse condition and subjected to PSM stress (0, 0.1, 0.5, 1.0, and 1.5 mM) for six days. Here, we show that FA and pHBA are potent inhibitors of Δ13C that varied from 21.0‰ to 22.9‰. Higher pHBA and FA supply enhanced/retard the Nleaf and increased the Cleaf while ratio of intercellular CO2 concentration from leaf to air (Ci/Ca) was significantly decreased as compared to control. Leaf water content and leaf osmotic potential were decreased following treatment with both PSM. The Ci/Ca decreased rapidly with higher concentration of FA and pHBA. However, iWUE increased at all allelochemical concentrations. At the whole plant level, both PSM showed pronounced growth-inhibitory effects on PBM and C and N concentration, root fresh/dry weight, leaf fresh/dry weight, and root, shoot length of C3 broad leaf weed R. acetosa. Carbon isotope discrimination (Δ) was correlated with the dry matter to transpiration ratio (transpiration efficiency) in this C3 species, but its heritability and relationship to R. acetosa growth are less clear. Our FA and pHBA compounds are the potent and selective carbon isotope composition (δ13C) inhibitors known to date. These results confirm the phytotoxicity of FA and pHBA on R. acetosa seedlings, the reduction of relative water content and the induction of carbon isotope discrimination (Δ) with lower plant biomass.
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Steinhardt, M., und H. H. Thielscher. „Wachstum und Entwicklungsqualität von Milchrindkälbern in Gruppenhaltung mit Tränkeautomatenfütterung. Physiologische Variablen und deren Änderungen in spezifischen Altersperioden“. Archives Animal Breeding 43, Nr. 1 (10.10.2000): 27–44. http://dx.doi.org/10.5194/aab-43-27-2000.
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Abstract. Title of the paper: Growth and development quality of dairy calves reared in groups with an automatic milk feeder. Physiological variables and their changes at specific age periods On 38 dairy calves (20 male, 18 female) measurements of growth Performance and of body temperature (RT) and blood sampling were made at 15, 30, 60 and 90 days of age of the calves. Blood was analysed for acid-base balance, biochemical and hematological values, minerals and hemoglobin derivatives. Effects of season (groupl: calvings from October tili December; group 2: calvings from January tili April) and of gender were considered. Growth Performance was different between the groups at all age points. Group effects existed at 15 days (RT, Hk, MetHb, Laktat, P), at 30 days (RT, P), at 60 days (Hb, O2CAP, pH, BE, HCO3, P), at 90 days (pCO2, blood urea, Mg, Fe). Gender effects became obvious at 30 days (O2CONT, O2SAT, MetHb, HHb, pCO2). Interactions of group and gender occured at 15 days (P), at 30 days (O2CONT, pCO2), at 60 days (COHb, Mg) and at 90 days (Hb, O2CAP). Between age point mean differences could be found for acid-base Status, total protein, albumin, Creatinine, blood urea, glucose, Mg and for the hematological variables. In most cases between age point changes of variables showed strong negativ correlations with the starting values at 15 days of age. Directed changes of most variables within life age periods developed with different degrees depending on development quality and on specific husbandry conditions.
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Petreska, Jasmina, Gjose Stefkov, Svetlana Kulevanova, Kalina Alipieva, Vassya Bankova und Marina Stefova. „Phenolic Compounds of Mountain Tea from the Balkans: LC/DAD/ESI/MSn Profile and Content“. Natural Product Communications 6, Nr. 1 (Januar 2011): 1934578X1100600. http://dx.doi.org/10.1177/1934578x1100600107.
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Twenty-one samples of Sideritis species ( S. scardica, S. raeseri, S. taurica, S. syriaca and S. perfoliata) from various locations on the Balkan Peninsula were evaluated for their chemical constituents. Chemical analyses were focused on secondary metabolites, particularly phenolic compounds, which have several roles in the plant physiological processes and have demonstrated significant health beneficial effects. The occurrence of hydroxycinnamic acids, phenylethanoid glycosides and flavonoids has been investigated in taxonomically related taxa of the genus Sideritis. A systematic method for phenolic compounds identification was developed using tandem mass spectrometry coupled to high performance liquid chromatography with diode array detection. Scanning for precursor ions of commonly found phenolics in Sideritis species using LC/MSn with an ion trap instrument permitted the specific determination of hydroxycinnamic acid derivatives, and phenylethanoid and flavonoid glycosides. Further characterization of each phenolic compound was performed using MS/MS production analysis and common–neutral-loss analysis. This online technique allowed identification of three hydroxycinnamic acid derivatives, eight phenylethanoid glycosides, and twenty-four flavonoid glycosides. All the taxa analysed produced very similar phenolic patterns characterized by the presence of 5-caffeoylquinic acid, lavandulifolioside, verbascoside, hypolaetin 7- O-[6′”- O-acetyl]-allosyl(1→2)glucoside, apigenin 7-(4″- p-coumaroylglucoside), 4′- O-methylisoscutellarein 7- O-[6′”- O-acetyl]-allosyl(1→2)glucoside, and minor amounts of isoverbascoside, apigenin 7- O-allosyl(1→2)glucoside, isoscutellarein 7- O-allosyl-(1→2)-[6′- O-acetyl]-glucoside, hypolaetin 7- O-allosyl-(1→2)-[6″- O-acetyl]-glucoside and 4′- O-methylhypolaetin 7- O-[6′”- O-acetyl]-allosyl-(1→2)-[6′- O-acetyl]-glucoside. These results show that the investigated species are systematically very closely related. Phenylethanoid glycosides and flavonoid acetylglycosides are dominant and constitute 90% of the total phenolic compounds compared with hydroxycinnamic acid and flavonoid 7- O-glycosides. Principal component analysis (PCA) was performed for the nature and content of the different compounds to be correlated to the particular Sideritis species and also to the locations.
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Wang, Yanyan, Yang Wang, Hefei Bai, Yuqian Han und Fang Yu. „An ABCG-Type Transporter Facilitates ABA Influx and Regulates Camptothecin Biosynthesis in Camptotheca acuminata“. International Journal of Molecular Sciences 23, Nr. 24 (17.12.2022): 16120. http://dx.doi.org/10.3390/ijms232416120.
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Camptothecin (CPT) and its derivatives from Camptotheca acuminata have antitumor effects as a DNA topoisomerase I inhibitor. Previous studies have shown that application of exogenous abscisic acid (ABA) significantly promoted the accumulation level of CPT and induced the expression of CPT biosynthetic genes, which revealed that ABA signaling is effectively involved in regulating CPT biosynthesis in C. acuminata. In this study, an ABA transporter, CaABAT, which encodes a plasma membrane protein belonging to the ABCG subfamily, was identified in C. acuminata, and its ABA import activity was confirmed by transport assay in yeast cells. Real-time PCR analysis showed that CaABAT was predominately expressed in C. acuminata leaves and its expression could be significantly upregulated by exogenous ABA treatment. Silencing of CaABAT down-regulated the expression of ABA response genes, which indicated that translocation of ABA by CaABAT should initiate changes in plant physiological status in response to ABA signaling, thus leading to decreased expression of CPT biosynthesis pathway genes and low accumulation levels of CPT in C. acuminata.
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Karkischenko, N. N., V. N. Karkischenko, Yu V. Fokin, L. A. Taboyakova, O. V. Alimkina und 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, Nr. 2 (10.06.2020): 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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Shen, Changchao, Wenwei Tang, Dongqiang Zeng, Hongle Xu, Wangcang Su und Renhai Wu. „Isoxadifen-Ethyl Derivatives Protect Rice from Fenoxaprop-P-Ethyl–associated Injury during the Control of Weedy Rice“. Weed Science 65, Nr. 5 (02.08.2017): 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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Okamoto, Lillian L., Caleb C. Reichhardt, Brian Griffin, Laura A. Smith, Gordon Murdoch und 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 (03.11.2020): 333. http://dx.doi.org/10.1093/jas/skaa278.592.
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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.
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Ghias, Mehreen, Syed Wadood Ali Shah, Fakhria A. Al-Joufi, Mohammad Shoaib, Syed Muhammad Mukarram Shah, Muhammad Naeem Ahmed und Muhammad Zahoor. „In Vivo Antistress Effects of Synthetic Flavonoids in Mice: Behavioral and Biochemical Approach“. Molecules 27, Nr. 4 (18.02.2022): 1402. http://dx.doi.org/10.3390/molecules27041402.
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Natural flavonoids, in addition to some of their synthetic derivatives, are recognized for their remarkable medicinal properties. The present study was designed to investigate the in vitro antioxidant and in vivo antistress effect of synthetic flavonoids (flavones and flavonols) in mice, where stress was induced by injecting acetic acid and physically through swimming immobilization. Among the synthesized flavones (F1–F6) and flavonols (OF1–OF6), the mono para substituted methoxy containing F3 and OF3 exhibited maximum scavenging potential against DPPH (2,2-diphenyl-1-picrylhydrazyl) with IC50 of 31.46 ± 1.46 μg/mL and 25.54 ± 1.21 μg/mL, respectively. Minimum antioxidant potential was observed for F6 and OF6 with IC50 values of 174.24 ± 2.71 μg/mL and 122.33 ± 1.98 μg/mL, respectively, in comparison with tocopherol. The ABTS scavenging activity of all the synthesized flavones and flavonols were significantly higher than observed with DPPH assay, indicating their potency as good antioxidants and the effectiveness of ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonate) assay in evaluating antioxidant potentials of chemical substances. The flavonoids-treated animals showed a significant (* p < 0.05, ** p < 0.01 and *** p < 0.001, n = 8) reduction in the number of writhes and an increase in swimming endurance time. Stressful conditions changed plasma glucose, cholesterol and triglyceride levels, which were used as markers when evaluating stress in animal models. The level of these markers was nearly brought to normal when pre-treated with flavones and flavonols (10 mg/kg) for fifteen days in experimental animals. These compounds also considerably reduced the levels of lipid peroxidation (TBARS: Thiobarbituric acid reactive substances), which was significant (* p < 0.05, ** p < 0.01 and *** p < 0.001, n = 8) compared to the control group. A significant rise in the level of catalase and SOD (super oxide dismutase) was also observed in the treated groups. Diazepam (2 mg/kg) was used as the standard drug. Additionally, the flavonoids markedly altered the weight of the adrenal glands, spleen and brain in stress-induced mice. The findings of the study suggest that these flavonoids could be used as a remedy for stress and are capable of ameliorating diverse physiological and biochemical alterations associated with stressful conditions. However, further experiments are needed to confirm the observed potentials in other animal models, especially in those with a closer resemblance to humans. Toxicological evaluations are also equally important.
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Timoneda, Joaquín, Lucía Rodríguez-Fernández, Rosa Zaragozá, M. Marín, M. Cabezuelo, Luis Torres, Juan Viña und Teresa Barber. „Vitamin A Deficiency and the Lung“. Nutrients 10, Nr. 9 (21.08.2018): 1132. http://dx.doi.org/10.3390/nu10091132.
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Vitamin A (all-trans-retinol) is a fat-soluble micronutrient which together with its natural derivatives and synthetic analogues constitutes the group of retinoids. They are involved in a wide range of physiological processes such as embryonic development, vision, immunity and cellular differentiation and proliferation. Retinoic acid (RA) is the main active form of vitamin A and multiple genes respond to RA signalling through transcriptional and non-transcriptional mechanisms. Vitamin A deficiency (VAD) is a remarkable public health problem. An adequate vitamin A intake is required in early lung development, alveolar formation, tissue maintenance and regeneration. In fact, chronic VAD has been associated with histopathological changes in the pulmonary epithelial lining that disrupt the normal lung physiology predisposing to severe tissue dysfunction and respiratory diseases. In addition, there are important alterations of the structure and composition of extracellular matrix with thickening of the alveolar basement membrane and ectopic deposition of collagen I. In this review, we show our recent findings on the modification of cell-junction proteins in VAD lungs, summarize up-to-date information related to the effects of chronic VAD in the impairment of lung physiology and pulmonary disease which represent a major global health problem and provide an overview of possible pathways involved.
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Ramiro-Cortijo, David, Pratibha Singh, Yan Liu, Esli Medina-Morales, William Yakah, Steven D. Freedman und Camilia R. Martin. „Breast Milk Lipids and Fatty Acids in Regulating Neonatal Intestinal Development and Protecting against Intestinal Injury“. Nutrients 12, Nr. 2 (19.02.2020): 534. http://dx.doi.org/10.3390/nu12020534.
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Human breast milk is the optimal source of nutrition for infant growth and development. Breast milk fats and their downstream derivatives of fatty acids and fatty acid-derived terminal mediators not only provide an energy source but also are important regulators of development, immune function, and metabolism. The composition of the lipids and fatty acids determines the nutritional and physicochemical properties of human milk fat. Essential fatty acids, including long-chain polyunsaturated fatty acids (LCPUFAs) and specialized pro-resolving mediators, are critical for growth, organogenesis, and regulation of inflammation. Combined data including in vitro, in vivo, and human cohort studies support the beneficial effects of human breast milk in intestinal development and in reducing the risk of intestinal injury. Human milk has been shown to reduce the occurrence of necrotizing enterocolitis (NEC), a common gastrointestinal disease in preterm infants. Preterm infants fed human breast milk are less likely to develop NEC compared to preterm infants receiving infant formula. Intestinal development and its physiological functions are highly adaptive to changes in nutritional status influencing the susceptibility towards intestinal injury in response to pathological challenges. In this review, we focus on lipids and fatty acids present in breast milk and their impact on neonatal gut development and the risk of disease.
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Ren, Wei, Qian Wang, Li Chen und Yanping Ren. „Transcriptome and Metabolome Analyses of Salt Stress Response in Cotton (Gossypium hirsutum) Seed Pretreated with NaCl“. Agronomy 12, Nr. 8 (04.08.2022): 1849. http://dx.doi.org/10.3390/agronomy12081849.
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Abiotic stresses adversely influence crop productivity and salt stress is one limiting factor. Plants need to evolve their defense mechanisms to survive in such fluctuating scenarios at either the biochemical, physiological, or molecular level. The analytical/critical investigations of cotton (Gossypium hirsutum) plants that involve looking into transcriptomic and metabolomic profiles could give a comprehensive picture of the response of the cotton plant to salt stress. This study was conducted on pre-treated cotton seeds by soaking them in a 3% sodium chloride (NaCl) solution at room temperature for 0.5, 1, and 1.5 h. In total, 3738 and 285 differentially expressed genes (DEGs) and metabolites, respectively, were discovered. The prominent DEGs included AtCCC1, EP1, NHE, AtpOMT, GAST1, CLC-c, ARP, AtKIN14, AtC3H2, COP9, AtHK-2, and EID1 to code for the regulation of seed growth, abscisic acid receptor PYR/PYL, a cellular response regarding stress tolerance (especially to salt) and germination, jasmonic acid, salicylic acid, and auxin-activated signaling pathways. A more significant amount of transcription factors, including the ethylene-responsive TFs ERF (205), bHLH (252), ZF-domains (167), bHLH (101), MYB (92), NAC (83), GATA (43), auxin-responsive proteins (30), MADs-box (23), bZIP (27), and HHO (13) were discovered in samples of NaCl-pretreated cotton seedlings under different treatments. The functional annotations of DEGs exposed their important roles in regulating different phytohormones and signal-transduction-mediated pathways in salt-treated seeds. The metabolites analysis revealed differential accumulation of flavonols, phenolic acid, amino acids, and derivatives in seedling samples treated for 0.5 h with NaCl. The conjoint analysis that showed most of the DEGs were associated with the production and regulation of glucose-1-phosphate, uridine 5′-diphospho-D-glucose, and 2-deoxyribose 1-phosphate under salt stress conditions. These results indicated positive effects of NaCl 0.5 h treatments on seedlings’ germination and growth, seemingly by activating specific growth-promoting enzymes and metabolites to alleviate adverse effects of salt stress. Hence, seed pre-treatment with NaCl can be beneficial in future cotton management and breeding programs to enhance growth and development under salt stress.