Journal articles: 'Biologically active metabolite'

1

Savchuk, Ya I., K. S. Tsyhanenko, O. V. Andrienko, and I. M. Kurchenko. "The New Biologically Active Metabolites from Aspergillus niveus 2411." Mikrobiolohichnyi Zhurnal 83, no. 4 (August 17, 2021): 74–85. http://dx.doi.org/10.15407/microbiolj83.04.074.

Full text

Abstract:

Pharmacological science possesses a significant number of compounds with antibiotic activity. By now the chemical structures have been identified and their properties have been described for the great number; many of them found practical use. But the main stimulus for the further new antibiotic compounds search is the acquired resistance of pathogenic organisms. Our previous investigations were devoted to antibiotic activity of Aspergillus niveus that is known as a producer of ferment preparations with wide activity spectrum. Aim. This investigation became the follow-up of our previous studies and its main task was to isolate, purify and obtain biologically active metabolite(s) from A. niveus 2411 strain in crystalline form, and to study its (their) physicochemical properties and biological activity. Methods. Biologically active metabolites were obtained by extraction, two-step column chromatography and recrystallization methods. The obtained substances were characterized by physical-chemical and microbiological methods. Results. Two substances in crystalline form with different spectrum of antibiotic activity against indicator test-cultures were obtained. The substance AN4 showed antibacterial, antifungal, and phytotoxic activities, while AN7 showed only antibacterial activity. Neither of obtained compounds showed dermatocidal or toxigenic activity in rabbit skin test. Obtained spectral characteristics of substances suggest that AN4 and AN7 substances are similar and belong to compounds with cyclic structures, have double linkage, methyl, aromatic, and carboxyl groups. Conclusions. Obtained data showed that antibiotic activity of A. niveus 2411 depend on the complex of biologically active metabolites with different biological and physicochemical properties. Two compounds AN4 and AN7 were isolated and purified from the fungal cultural filtrate of A. niveus 2411. The data of IR and UV spectra of these compounds and their profiles of biological activity don’t have significant differences with those of citrinin – a metabolite of A. niveus with antibiotic properties. However, based on the results obtained and comparisons with the data of other authors on metabolites of A. niveus, we suggest that the substances we isolated may be derivatives of citrinin.

APA, Harvard, Vancouver, ISO, and other styles

2

Choudhry, Satish C., Peter S. Belica, David L. Coffen, Antonino Focella, Hubert Maehr, Percy S. Manchand, Lucia Serico, and Roxana T. Yang. "Synthesis of a biologically active vitamin D2 metabolite." Journal of Organic Chemistry 58, no. 6 (March 1993): 1496–500. http://dx.doi.org/10.1021/jo00058a034.

Full text

APA, Harvard, Vancouver, ISO, and other styles

3

Krajčová, A., V. Schulzová, J. Lojza, L. Křížová, and J. Hajšlová. "Phytoestrogens in bovine plasma and milk – LC-MS/MS analysis." Czech Journal of Food Sciences 28, No. 4 (September 6, 2010): 264–74. http://dx.doi.org/10.17221/138/2010-cjfs.

Full text

Abstract:

Phytoestrogens belong to a group of polyphenolic plant metabolites which induce biological responses, based on their structural similarity to 17β-estradiol. In order to investigate the relationship between the levels of these biologically active compounds and beneficial health effects, it is neccesary to quantify accurately their levels in foods and biological fluids. In this study, HPLC-MS/MS method for the determination of isoflavones genistein, daidzein, and estrogenic metabolite-equol in bovine plasma and milk was optimised and validated. The method allowed low limits of detection: 5, 2.5 and 0.5 ng/ml for genistein, daidzein and equol, respectively, thus enabling to determine the effect of phytoestrogen-rich diet on the concentration of isoflavones and the metabolite in biological fluids of cows. The feeding experiment, carried out with four dairy cows, showed that a soy-based diet significantly increased both plasma and milk contents of biologically potent equol, therefore, the latter commodity could be an alternative source of this estrogenic metabolite, namely for the consumers who are not capable to convert it from the isoflavone precursors consumed in the diet.

APA, Harvard, Vancouver, ISO, and other styles

4

Sułkowska-Ziaja, Katarzyna, Bożena Muszyńska, and Anna Firlej. "Biologically active compounds from selected aphyllophorales mycelial cultures." Folia Biologica et Oecologica 10 (November 30, 2014): 73–79. http://dx.doi.org/10.2478/fobio-2014-0004.

Full text

Abstract:

For a long time fungi belonging to Basidiomycota phylum have been in the center of attention because of the presence in their fruiting bodies of compounds with known therapeutic activity. Mycelial cultures of two aphyllophorales species occurring in Poland, Hydnum repandum L., and Sparassis crispa (Wulf.) Fr., were analyzed in our study. The main aim of the study was qualitative and quantitative analysis of extracts obtained from the mycelial cultures for the presence of known biologically active compounds, including phenolic acids, non-hallucinogenic indole compounds and sterols. For analyses a reversed-phase chromatography (RP-HPLC) method was used. The presence of eight phenolic acids including gallic, gentisic, p-hydroxybenzoic, caffeic, p-coumaric protocatechuic, syringic, vanillic and cinnamic acids was confirmed in the extracts obtained from the biomass. The quantitatively predominant metabolites in biomass from in vitro cultures of H. repandum and S. crispa were protocatechuic acid (6.23 μg/g DW) and p-hydroxybenzoic acid (4.52 μg/g DW). Derivatives of indole such as indole, serotonin, tryptamine and tryptophan were measured quantitatively. Their total content was estimated as 1.28 μg/g DW and 3.07 μg/g DW in H. repandum and S. crispa extracts, respectively. The major metabolite found was tryptophan. In addition, ergosterol, one of the sterols present in the biomass of in vitro cultures of S. crispa was analyzed (700.87 μg/g DW). The obtained results confirm the hypothesis that mycelial cultures of domestic species of aphyllophorales are able to accumulate biologically active metabolites.

APA, Harvard, Vancouver, ISO, and other styles

5

Cheng, Tian, Clara Chepkirui, Cony Decock, Josphat C. Matasyoh, and Marc Stadler. "Skeletocutins M–Q: biologically active compounds from the fruiting bodies of the basidiomycete Skeletocutis sp. collected in Africa." Beilstein Journal of Organic Chemistry 15 (November 19, 2019): 2782–89. http://dx.doi.org/10.3762/bjoc.15.270.

Full text

Abstract:

During the course of screening for new metabolites from basidiomycetes, we isolated and characterized five previously undescribed secondary metabolites, skeletocutins M–Q (1–5), along with the known metabolite tyromycin A (6) from the fruiting bodies of the polypore Skeletocutis sp. The new compounds did not exhibit any antimicrobial, cytotoxic, or nematicidal activities. However, compound 3 moderately inhibited the biofilm formation of Staphylococcus aureus (S. aureus), while compounds 3 and 4 performed moderately in the ʟ-leucine-7-amido-4-methylcoumarin (ʟ-Leu-AMC) inhibition assay. These compounds represent the first secondary metabolites reported to occur in the fruiting bodies by Skeletocutis. Interestingly, tyromycin A (6) was found to be the only common metabolite in fruiting bodies and mycelial cultures of the fungus, and none of the recently reported skeletocutins from the culture of the same strain were detected in the basidiomes.

APA, Harvard, Vancouver, ISO, and other styles

6

Nofiani, Risa. "Urgensi dan Mekanisme Biosintesis Metabolit Sekunder Mikroba Laut." Jurnal Natur Indonesia 10, no. 2 (November 20, 2012): 120. http://dx.doi.org/10.31258/jnat.10.2.120-125.

Full text

Abstract:

Marine microorganism is one of biologically active potential resources of secondary metabolites. Its potency areso promising that the knowledge of how its secondary metabolite occured need to be studied and collected. Thoseknowledges will enable further study is improving secondary metabolite production in the laboratory. In nature,secondary metabolites synthesis occur when there are effect of both biotic and abiotic factors such as sea waterand microbe symbiosis with other living materials. When this is explained in metabolic pathways, secondarymetabolite synthesis affected by available nutrient and regulated by autoinducer molecules through quorum sensingmechanism

APA, Harvard, Vancouver, ISO, and other styles

7

Okeke, Boniface, Mourad Kaouadji, Françoise Seigle-Murandi, and Régine Steiman. "Setosol, a Biologically Active Heptaketide-like Metabolite from thePleiochaeta setosaPhytopathogen." Bioscience, Biotechnology, and Biochemistry 58, no. 4 (January 1994): 734–36. http://dx.doi.org/10.1271/bbb.58.734.

Full text

APA, Harvard, Vancouver, ISO, and other styles

8

Nishizawa, Rena, Toshihiko Nishiyama, Katsuya Hisaichi, Naoki Matsunaga, Chiaki Minamoto, Hiromu Habashita, Yoshikazu Takaoka, et al. "Spirodiketopiperazine-based CCR5 antagonists: Lead optimization from biologically active metabolite." Bioorganic & Medicinal Chemistry Letters 17, no. 3 (February 2007): 727–31. http://dx.doi.org/10.1016/j.bmcl.2006.10.084.

Full text

APA, Harvard, Vancouver, ISO, and other styles

9

Higgs, Richard E., James A. Zahn, Jeffrey D. Gygi, and Matthew D. Hilton. "Rapid Method To Estimate the Presence of Secondary Metabolites in Microbial Extracts." Applied and Environmental Microbiology 67, no. 1 (January 1, 2001): 371–76. http://dx.doi.org/10.1128/aem.67.1.371-376.2001.

Full text

Abstract:

ABSTRACT Screening microbial secondary metabolites is an established method to identify novel biologically active molecules. Preparation of biological screening samples from microbial fermentation extracts requires growth conditions that promote synthesis of secondary metabolites and extraction procedures that capture the secondary metabolites produced. High-performance liquid chromatography (HPLC) analysis of fermentation extracts can be used to estimate the number of secondary metabolites produced by microorganisms under various growth conditions but is slow. In this study we report on a rapid (approximately 1 min per assay) surrogate measure of secondary metabolite production based on a metabolite productivity index computed from the electrospray mass spectra of samples injected directly into a spectrometer. This surrogate measure of productivity was shown to correlate with an HPLC measure of productivity with a coefficient of 0.78 for a test set of extracts from 43 actinomycetes. This rapid measure of secondary metabolite productivity may be used to identify improved cultivation and extraction conditions by analyzing and ranking large sets of extracts. The same methods may also be used to survey large collections of extracts to identify subsets of highly productive organisms for biological screening or additional study.

APA, Harvard, Vancouver, ISO, and other styles

10

Ghoneim, Mohammed M., Guoyi Ma, Atef A. El-Hela, Abd-Elsalam I. Mohammad, Saeid Kottob, Sayed El-Ghaly, Stephen J. Cutler, and Samir A. Ross. "Biologically Active Secondary Metabolites from Asphodelus Microcarpus." Natural Product Communications 8, no. 8 (August 2013): 1934578X1300800. http://dx.doi.org/10.1177/1934578x1300800822.

Full text

Abstract:

Bioassay guided fractionation of the ethanolic extract of Asphodelus microcarpus Salzm.et Vivi (Asphodelaceae) resulted in the isolation of one new metabolite, 1,6-dimethoxy-3-methyl-2-naphthoic acid (1) as well as nine known compounds: asphodelin (2), chrysophanol (3), 8-methoxychrysophanol (4), emodin (5), 2-acetyl-1,8-dimethoxy-3-methylnaphthalene (6), 10-(chrysophanol-7’-yl)-10-hydroxychrysophanol-9-anthrone (7), aloesaponol-III-8-methyl ether (8), ramosin (9) and aestivin (10). The compounds were identified by 1D and 2D NMR and HRESIMS. Compounds 3, 6 and 10 were isolated for the first time from this species. Compounds 3 and 4 showed moderate to weak antileishmanial activity with IC50 values of 14.3 and 35.1 μg/mL, respectively. Compound 4 exhibited moderate antifungal activity against Cryptococcus neoformans with an IC50 value of 15.0 μg/mL, while compounds 5, 7 and 10 showed good to potent activity against methicillin resistant Staphylococcus aureus (MRSA) with IC50 values of 6.6, 9.4 μg/mL and 1.4 μg/mL respectively. Compounds 5, 8 and 9 displayed good activity against S. aureus with IC50 values of 3.2, 7.3 and 8.5 μg/mL, respectively. Compounds 7 and 9 exhibited a potent cytotoxic activity against leukemia LH60 and K562 cell lines. Compound 10 showed potent antimalarial activities against both chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum with IC50 values in the range of 0.8-0.7 μg/mL without showing any cytotoxicity to mammalian cells.

APA, Harvard, Vancouver, ISO, and other styles

11

Comas, Laura, Esther Polo, M. Pilar Domingo, Yulán Hernández, Maykel Arias, Patricia Esteban, Luis Martínez-Lostao, Julián Pardo, Jesús Martínez de la Fuente, and Eva M. Gálvez. "Intracellular Delivery of Biologically-Active Fungal Metabolite Gliotoxin Using Magnetic Nanoparticles." Materials 12, no. 7 (April 2, 2019): 1092. http://dx.doi.org/10.3390/ma12071092.

Full text

APA, Harvard, Vancouver, ISO, and other styles

12

Calverley, Martin J. "Synthesis of mc 903, a biologically active vitamin D metabolite analogue." Tetrahedron 43, no. 20 (January 1987): 4609–19. http://dx.doi.org/10.1016/s0040-4020(01)86903-9.

Full text

APA, Harvard, Vancouver, ISO, and other styles

13

CHOUDHRY, S. C., P. S. BELICA, D. L. COFFEN, A. FOCELLA, H. MAEHR, P. S. MANCHAND, L. SERICO, and R. T. YANG. "ChemInform Abstract: Synthesis of a Biologically Active Vitamin-D2 Metabolite (I)." ChemInform 24, no. 28 (August 20, 2010): no. http://dx.doi.org/10.1002/chin.199328294.

Full text

APA, Harvard, Vancouver, ISO, and other styles

14

Brown, Sarah M., Michael Holtzman, Thomas Kim, and Evan D. Kharasch. "Buprenorphine Metabolites, Buprenorphine-3-glucuronide and Norbuprenorphine-3-glucuronide, Are Biologically Active." Anesthesiology 115, no. 6 (December 1, 2011): 1251–60. http://dx.doi.org/10.1097/aln.0b013e318238fea0.

Full text

Abstract:

Background The long-lasting high-affinity opioid buprenorphine has complex pharmacology, including ceiling effects with respect to analgesia and respiratory depression. Plasma concentrations of the major buprenorphine metabolites norbuprenorphine, buprenorphine-3-glucuronide, and norbuprenorphine-3-glucuronide approximate or exceed those of the parent drug. Buprenorphine glucuronide metabolites pharmacology is undefined. This investigation determined binding and pharmacologic activity of the two glucuronide metabolites, and in comparison with buprenorphine and norbuprenorphine. Methods Competitive inhibition of radioligand binding to human μ, κ, and δ opioid and nociceptin receptors was used to determine glucuronide binding affinities for these receptors. Common opiate effects were assessed in vivo in SwissWebster mice. Antinociception was assessed using a tail-flick assay, respiratory effects were measured using unrestrained whole-body plethysmography, and sedation was assessed by inhibition of locomotion measured by open-field testing. Results Buprenorphine-3-glucuronide had high affinity for human μ (Ki [inhibition constant] = 4.9 ± 2.7 pM), δ (Ki = 270 ± 0.4 nM), and nociceptin (Ki = 36 ± 0.3 μM) but not κ receptors. Norbuprenorphine-3-glucuronide had affinity for human κ (Ki = 300 ± 0.5 nM) and nociceptin (Ki = 18 ± 0.2 μM) but not μ or δ receptors. At the dose tested, buprenorphine-3-glucuronide had a small antinociceptive effect. Neither glucuronide had significant effects on respiratory rate, but norbuprenorphine-3-glucuronide decreased tidal volume. Norbuprenorphine-3-glucuronide also caused sedation. Conclusions Both glucuronide metabolites of buprenorphine are biologically active at doses relevant to metabolite exposures, which occur after buprenorphine. Activity of the glucuronides may contribute to the overall pharmacology of buprenorphine.

APA, Harvard, Vancouver, ISO, and other styles

15

Bachurin, S. O., A. A. Dunaevetskii, V. S. Lyubimov, and I. V. Martynov. "Kinetic features of biologically active compounds. 1. Irreversible metabolite inhibition of enzymes." Pharmaceutical Chemistry Journal 25, no. 8 (August 1991): 521–26. http://dx.doi.org/10.1007/bf00777413.

Full text

APA, Harvard, Vancouver, ISO, and other styles

16

BAUMANN, M. H., J. P. PABLO, S. F. ALI, R. B. ROTHMAN, and D. C. MASH. "Noribogaine (12-Hydroxyibogamine): A Biologically Active Metabolite of the Antiaddictive Drug Ibogaine." Annals of the New York Academy of Sciences 914, no. 1 (September 2000): 354–68. http://dx.doi.org/10.1111/j.1749-6632.2000.tb05210.x.

Full text

APA, Harvard, Vancouver, ISO, and other styles

17

Semar, Martin, Heidrun Anke, Wolf-Rüdiger Arendholz, Robert Veiten, and Wolfgang Steglich. "Lachnellins A, B, C, D, and Naphthalene-l,3,8-triol, Biologically Active Compounds from a Lachnellula Species (Ascomycetes)." Zeitschrift für Naturforschung C 51, no. 7-8 (August 1, 1996): 500–512. http://dx.doi.org/10.1515/znc-1996-7-808.

Full text

Abstract:

Abstract In the course of our search for new biologically active metabolites, lachnellin A (1), a metabolite with high cytotoxic and antimicrobial activities, the structurally related lachnellins B, C and D (3, 4, 7), and naphthalene-1,3,8-triol (8), an inhibitor of malate synthase (EC 4.1.3.2), were isolated from submerged cultures of the ascomycete Lachnellula sp. A 32 -8 9 . The antimicrobial, cytotoxic and phytotoxic activities of lachnellin A depended on its reactivity and could be abolished by the addition of cysteine. The enzyme inhibiting activity of (8) was due to reactive intermediates during melanization and was no longer observed in the presence of serum albumin. In addition, rac-scytalone (9), (+)-trans-3,4-dihydro-3,4,8-trihy-droxy-1(2H)-naphthalenone (10). 2,5-dihydroxytoluene (11), and (R)-(-)-5-methylmellein (12) were obtained from the same source and biologically characterized.

APA, Harvard, Vancouver, ISO, and other styles

18

Kolomietc, Andrey, Nadezda Nicolaeva, Victoria Larina, and Nataliya Chupakhina. "Growing optimization of suspension cultures of medicinal plant cells." E3S Web of Conferences 291 (2021): 02022. http://dx.doi.org/10.1051/e3sconf/202129102022.

Full text

Abstract:

Suspension cell cultures allow to save plant material when obtaining biologically active compounds of natural origin. As a result of the studies, optimal parameters were selected to increase the formation of biologically active metabolites in suspension cell cultures of such medicinal plants as Maackia amurensis Rupr., Hyssopus officinalis L. and Saposhnikovia divaricata (Turcz.) Schischk. Medicinal plants are a large group of plants used as raw materials for the production of medicinal and preventive drugs for medical and animal use. The assortment of phytopreparations is constantly expanding due to the increased demand for natural remedies, due to their less aggressive and toxic nature compared to synthetic ones [1]. Cultivation of medicinal plants in the form of isolated cells in vitro is one of the most modern technologies for rapidly obtaining a large biomass of plant material with stable growth features year-round under controlled conditions [2]. It is known that cells in vitro grow faster and have peculiarities of synthesis and accumulation of biologically active substances compared to intact plants [3]. Isolated cells, unlike tissue cells, also have an advantage for their use as a source of active metabolites, since they have the ability to release these compounds into the intercellular space [4]. The goal of this paper was to select parameters for increasing the biosynthetic activity of cultured suspension cultures of medicinal plant cells in vitro by optimizing cultivation conditions and introducing precursors of secondary metabolite biosynthesis into the nutrient media.

APA, Harvard, Vancouver, ISO, and other styles

19

Strugnell, S., V. Byford, H. L. J. Makin, R. M. Moriarty, R. Gilardi, L. W. LeVan, J. C. Knutson, C. W. Bishop, and G. Jones. "1α,24(S)-dihydroxyvitamin D2: a biologically active product of 1α-hydroxyvitamin D2 made in the human hepatoma, Hep3B." Biochemical Journal 310, no. 1 (August 15, 1995): 233–41. http://dx.doi.org/10.1042/bj3100233.

Full text

Abstract:

A major metabolite of the vitamin D analogue 1 alpha-hydroxyvitamin D2 in human liver cells in culture has been identified as 1 alpha,24(S)-dihydroxyvitamin D2 [1 alpha,24(S)-(OH)2D2]. 1 alpha-Hydroxyvitamin D3 incubated with the same cells gives rise to predominantly 25- and 27-hydroxylated products. Our identification of 1 alpha,24(S)-dihydroxyvitamin D2 is based on comparisons of the liver cell metabolite with chemically synthesized 1 alpha,24(S)-(OH)2D2 and 1 alpha,24(R)-(OH)2D2 by using HPLC, GC and GC-MS techniques. The stereochemical orientation of the 24-hydroxyl group was inferred after X-ray-crystallographic analysis of the 24(R)-OH epimer. 1 alpha,24(S)-Dihydroxyvitamin D2 binds strongly to the vitamin D receptor and is biologically active in growth hormone and chloramphenicol acetyltransferase reporter gene expression systems in vitro, but binds poorly to rat vitamin D-binding globulin, DBP. We suggest that this metabolite, 1 alpha,24(S)-(OH)2D2, possesses the spectrum of biological properties to be useful as a drug in the treatment of psoriasis, metabolic bone disease and cancer.

APA, Harvard, Vancouver, ISO, and other styles

20

Stadler, Marc, Timm Anke, Johannes Dasenbrock, and Wolfgang Steglich. "Phellodonic Acid, a New Biologically Active Hirsutane Derivative from Phellodon melaleucus (Thelephoraceae, Basidiomycetes) [1]." Zeitschrift für Naturforschung C 48, no. 7-8 (August 1, 1993): 545–49. http://dx.doi.org/10.1515/znc-1993-7-803.

Full text

Abstract:

Abstract A new hirsutane derivative, phellodonic acid (1), has been isolated from fermentations of Phellodon melaleucus strain 87113. Its structure was elucidated by spectroscopic methods. The compound exhibits antibiotic activities towards bacteria and fungi. 1 is the first bioactive metabolite from cultures of a species belonging to the family Thelephoraceae.

APA, Harvard, Vancouver, ISO, and other styles

21

Miller, Duncan A., and Hector F. DeLuca. "Biosynthesis of retinoyl-β-glucuronide, a biologically active metabolite of all-trans-retinoic acid." Archives of Biochemistry and Biophysics 244, no. 1 (January 1986): 179–86. http://dx.doi.org/10.1016/0003-9861(86)90107-4.

Full text

APA, Harvard, Vancouver, ISO, and other styles

22

Dixon, David P., Jonathan D. Sellars, and Robert Edwards. "The Arabidopsis phi class glutathione transferase AtGSTF2: binding and regulation by biologically active heterocyclic ligands." Biochemical Journal 438, no. 1 (July 27, 2011): 63–70. http://dx.doi.org/10.1042/bj20101884.

Full text

Abstract:

The plant-specific phi class of glutathione transferases (GSTFs) are often highly stress-inducible and expressed in a tissue-specific manner, suggestive of them having important protective roles. To date, these functions remain largely unknown, although activities associated with the binding and transport of reactive metabolites have been proposed. Using a sensitive and selective binding screen, we have probed the Arabidopsis thaliana GSTFs for natural product ligands from bacteria and plants. Uniquely, when overexpressed in bacteria, family members GSTF2 and GSTF3 bound a series of heterocyclic compounds, including lumichrome, harmane, norharmane and indole-3-aldehyde. When screened against total metabolite extracts from A. thaliana, GSTF2 also selectively bound the indole-derived phytoalexin camalexin, as well as the flavonol quercetin-3-O-rhamnoside. In each case, isothermal titration calorimetry revealed high-affinity binding (typically Kd<1 μM), which was enhanced in the presence of glutathione and by the other heterocyclic ligands. With GSTF2, these secondary ligand associations resulted in an allosteric enhancement in glutathione-conjugating activity. Together with the known stress responsiveness of GSTF2 and its association with membrane vesicles, these results are suggestive of roles in regulating the binding and transport of defence-related compounds in planta.

APA, Harvard, Vancouver, ISO, and other styles

23

Lagoutte-Renosi, Jennifer, Florentin Allemand, Christophe Ramseyer, Vahideh Rabani, and Siamak Davani. "Influence of Antiplatelet Agents on the Lipid Composition of Platelet Plasma Membrane: A Lipidomics Approach with Ticagrelor and Its Active Metabolite." International Journal of Molecular Sciences 22, no. 3 (January 31, 2021): 1432. http://dx.doi.org/10.3390/ijms22031432.

Full text

Abstract:

Lipids contained in the plasma membrane of platelets play an important role in platelet function. Modifications in the lipid composition can fluidify or rigidify the environment around embedded receptors, in order to facilitate the access of the receptor by the drug. However, data concerning the lipid composition of platelet plasma membrane need to be updated. In addition, data on the impact of drugs on plasma membrane composition, in particular antiplatelet agents, remain sparse. After isolation of platelet plasma membrane, we assessed, using lipidomics, the effect of ticagrelor, a P2Y12 antagonist, and its active metabolite on the lipid composition of these plasma membranes. We describe the exact lipid composition of plasma membrane, including all sub-species. Ticagrelor and its active metabolite significantly increased cholesterol and phosphatidylcholine ether with short saturated acyl chains 16:0/16:0, and decreased phosphatidylcholine, suggesting overall rigidification of the membrane. Furthermore, ticagrelor and its active metabolite decreased some arachidonylated plasmalogens, suggesting a decrease in availability of arachidonic acid from the membrane phospholipids for synthesis of biologically active mediators. To conclude, ticagrelor and its active metabolite seem to influence the lipid environment of receptors embedded in the lipid bilayer and modify the behavior of the plasma membrane.

APA, Harvard, Vancouver, ISO, and other styles

24

Li, Shipeng, Ye Chen, Ying Duan, Yinhui Zhao, Di Zhang, Liyan Zang, and Huiyuan Ya. "Widely Targeted Metabolomics Analysis of Different Parts of Salsola collina Pall." Molecules 26, no. 4 (February 20, 2021): 1126. http://dx.doi.org/10.3390/molecules26041126.

Full text

Abstract:

Salsola collina Pall has a long history of being used as a traditional medicine to treat hypertension, headache, insomnia, constipation and vertigo. However, only a few biologically active substances have been identified from S. collina. Here, the shoots and roots of S. collina, namely L-Sc and R-Sc, were studied. The primary and secondary metabolites were investigated using ultrahigh-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UPLC-ESI-MS/MS). A total of 637 putative metabolites were identified and these metabolites were mainly classified into ten different categories. Correlation analysis, hierarchical clustering analysis, principal component analysis and orthogonal partial least squares discriminant analysis of metabolites showed that the L-Sc samples could be clearly separated from the R-Sc samples. Differential accumulated metabolite analysis revealed that most of differential primary metabolites were significantly lower in the L-Sc than in the R-Sc. Conversely, the major differential secondary metabolites had higher levels in the L-Sc than in the R-Sc. Further analysis indicated that the flavonoids were the major putative antioxidant components and most of putative antioxidant components exhibited higher relative concentrations in the L-Sc than the R-Sc. These results improve our understanding of metabolite accumulation and provide a reference for the study of medicinal value in S. collina.

APA, Harvard, Vancouver, ISO, and other styles

25

Garbrecht, Mark R., Thomas J. Schmidt, Zygmunt S. Krozowski, and Jeanne M. Snyder. "11β-Hydroxysteroid dehydrogenase type 2 and the regulation of surfactant protein A by dexamethasone metabolites." American Journal of Physiology-Endocrinology and Metabolism 290, no. 4 (April 2006): E653—E660. http://dx.doi.org/10.1152/ajpendo.00396.2005.

Full text

Abstract:

Glucocorticoid (GC) metabolism by the 11β-hydroxysteroid dehydrogenase (HSD) system is an important prereceptor regulator of GC action. The HSD enzymes catalyze the interconversion of the endogenous, biologically active GC cortisol and its inactive 11-dehydro metabolite cortisone. The role of the HSD enzymes in the metabolism of synthetic GCs, such as dexamethasone (Dex), is more complex. The human lung is a classic GC-sensitive organ; however, the roles of the HSD enzymes (HSD1 and HSD2) in the human lung are poorly understood. In the present study, we examined the expression of the HSD enzymes in human adult and fetal lung tissues and the human lung epithelial cell line NCI-H441. We observed that human adult and fetal lung tissues, as well as H441 cells, express HSD2 protein and that it is upregulated by Dex (10−7 M). By contrast, HSD1 protein was undetectable. We also show that the Dex-mediated regulation of surfactant protein A is attenuated by inhibition of HSD2 activity. Furthermore, we demonstrate that unlike the inactive, 11-dehydro metabolite of cortisol (i.e., cortisone), the 11-dehydro metabolite of Dex, 11-dehydro-Dex, competes for binding to the GC receptor (GR) in human lung epithelial cells and retains GR agonist activity. Together, these data suggest that differences exist in the biological activities of the metabolites of cortisol and Dex.

APA, Harvard, Vancouver, ISO, and other styles

26

RETNOWATI, YULIANA, SUKARTI MOELJOPAWIRO, TJUT SUGANDAWATY DJOHAN, and ENDANG SUTARININGSIH SOETARTO. "Antimicrobial activities of actinomycete isolates from rhizospheric soils in different mangrove forests of Torosiaje, Gorontalo, Indonesia." Biodiversitas Journal of Biological Diversity 19, no. 6 (October 9, 2018): 2196–203. http://dx.doi.org/10.13057/biodiv/d190627.

Full text

Abstract:

Retnowati Y, Moeljopawiro S, Djohan TjS, Soetarto ES. 2018. Antimicrobial activities of actinomycetes isolates from rhizospheric soil on different mangrove forests of Torosiaje, Gorontalo, Indonesia. Biodiversitas 19: 2196-2203. Mangrove forests are very productive ecosystems that form unique saline environment very rich in organic matter, containing nitrogen and sulfur available for microorganisms. Mangrove forest as an extreme environment is promising to be sources of antibiotic-producing actinomycetes. The objectives of this study were to analyze the antimicrobial activities of metabolites produced by actinomycete isolates from rhizospheric soil of mangrove forest of Torosiaje, Gorontalo, Indonesia, and identify the active compound for novel antibiotics production. Six isolates from a coastal mangrove forest was selected to produce secondary metabolite. The crude extract of the six selected actinomycete isolates showed antimicrobial activities against pathogenic microbes; the highest antimicrobial activities was indicated by metabolite produced by FUAm2-h1 and FMBg2-x3 isolates. The metabolite crude extracts produced by two potential isolates inhibited growth of pathogenic microbe on MIC value of 0.0625 to 0.5mgmL-1. Bio-autography assay detected an active compound on Rf value of 0.94, especially on extracellular metabolite produced by strain FUAm2-h1. The bioactive compounds were identified by liquid chromatography joined with low-resolution mass spectroscopy (LC/MS) and analysed by MEDINA's database The active compounds composed of 17 substances, and only 3 substances showed a high quantity with molecular weight of 507.37, 344.32 and 563.66 mol G-1, respectively. FTIR analyses identified the functional groups in the active compounds consisted of amide, amine, alkuna, alkane, NO2 nitro compound, alcohol, ether, carboxylic acid, ester and C-H aromatic ring. The biosynthesis of antibiotic on FUAm2-h1 and FMBg2-x3 isolates was regulated by double genes, i.e., PKS-II and NRPS genes. The antimicrobial activities of two actinomycete isolates showed the performance of antibiotics suspected as aromatics polyketides group. The FUAm2-h1 and FMBg2-x3 isolates showed high similarity with Streptomyces qinglanensis strain 172205 and Streptomyces sanyensis strain 219820, respectively, in terms of 16S rRNA gene sequences. The potential of those selected actinomycetes from extreme environments of mangrove forest constitute a source of promising actinomycete strains producing biologically active secondary metabolites.

APA, Harvard, Vancouver, ISO, and other styles

27

Lian, Thang Tung, Se-Yeoun Cha, Myat Myat Moe, Yong Ju Kim, and Keuk Soo Bang. "Effects of Different Colored LEDs on the Enhancement of Biologically Active Ingredients in Callus Cultures of Gynura procumbens (Lour.) Merr." Molecules 24, no. 23 (November 27, 2019): 4336. http://dx.doi.org/10.3390/molecules24234336.

Full text

Abstract:

Conventional fluorescent lamps that are used in tissue culture are costly light sources, exhibiting excessive wavelength emission-bandwidth that must be replaced by alternative, less costly, and much lower power-consuming energy sources. The use of Light-Emitting Diodes (LEDs) is the best option due to their potential role as elicitors of secondary metabolite production in many plant models. Gynura procumbens (G. procumbens) is widely used for treating various diseases. Here, leaf explants were cultivated in MS medium that was supplemented with 0.5 mg/L of naphthaleneacetic acid (NAA) and 2.0 mg/L of benzylaminopurine (BAP) for 30 days under white, blue, and red LEDs. Secondary metabolites were analyzed by High Performance Liquid Chromatography (HPLC) and Liquid Chromatography-Mass Spectrometry (LC-MS). Blue LEDs elicited the highest antioxidant activity, total flavonoid, and phenolic content. Furthermore, the content of cyanidin-monoglucosides significantly increased under blue light.

APA, Harvard, Vancouver, ISO, and other styles

28

Mancini, Raffaella, Enza Piccolo, Stefania Mariggio', Beatrice Maria Filippi, Cristiano Iurisci, Paolo Pertile, Christopher P. Berrie, and Daniela Corda. "Reorganization of Actin Cytoskeleton by the Phosphoinositide Metabolite Glycerophosphoinositol 4-Phosphate." Molecular Biology of the Cell 14, no. 2 (February 2003): 503–15. http://dx.doi.org/10.1091/mbc.e02-04-0179.

Full text

Abstract:

Glycerophosphoinositol 4-phosphate (GroPIns-4P) is a biologically active, water-soluble phospholipase A metabolite derived from phosphatidylinositol 4-phosphate, whose cellular concentrations have been reported to increase in Ras-transformed cells. It is therefore important to understand its biological activities. Herein, we have examined whether GroPIns-4P can regulate the organization of the actin cytoskeleton, because this could be a Ras-related function involved in cell motility and metastatic invasion. We find that in serum-starved Swiss 3T3 cells, exogenously added GroPIns-4P rapidly and potently induces the formation of membrane ruffles, and, later, the formation of stress fibers. These actin structures can be regulated by the small GTPases Cdc42, Rac, and Rho. To analyze the mechanism of action of GroPIns-4P, we selectively inactivated each of these GTPases. GroPIns-4P requires active Rac and Rho, but not Cdc42, for ruffle and stress fiber formation, respectively. Moreover, GroPIns-4P induces a rapid translocation of the green fluorescent protein-tagged Rac into ruffles, and increases the fraction of GTP-bound Rac, in intact cells. The activation of Rac by GroPIns-4P was near maximal and long-lasting. Interestingly, this feature seems to be critical in the induction of actin ruffles by GroPIns-4P.

APA, Harvard, Vancouver, ISO, and other styles

29

Taddeo, Vito, Ulises Castillo, Morena Martínez, Jenny Menjivar, Ignacio Jiménez, Marvin Núñez, and Isabel Bazzocchi. "Development and Validation of an HPLC-PDA Method for Biologically Active Quinonemethide Triterpenoids Isolated from Maytenus chiapensis." Medicines 6, no. 1 (March 7, 2019): 36. http://dx.doi.org/10.3390/medicines6010036.

Full text

Abstract:

Background: Quinonemethide triterpenoids, known as celastroloids, constitute a relatively small group of biologically active compounds restricted to the Celastraceae family and, therefore, they are chemotaxonomic markers for this family. Among this particular type of metabolite, pristimerin and tingenone are considered traditional medicines in Latin America. The aim of this study was the isolation of the most abundant celastroloids from the root bark of Maytenus chiapensis, and thereafter, to develop an analytical method to identify pristimerin and tingenone in the Celastraceae species. Methods: Pristimerin and tingenone were isolated from the n-hexane-Et2O extract of the root bark of M. chiapensis through chromatographic techniques, and were used as internal standards. Application of a validated RP HPLC-PDA method was developed for the simultaneous quantification of these two metabolites in three different extracts, n-hexane-Et2O, methanol, and water, to determine the best extractor solvent. Results: Concentration values showed great variation between the solvents used for extraction, with the n-hexane–Et2O extract being the richest in pristimerin and tingenone. Conclusions: M. chiapensis is a source of two biologically active quinonemethide triterpenoids. An analytical method was developed for the qualification and quantification of these two celastroloids in the root bark extracts of M. chiapensis. The validated method reported herein could be extended and be useful in analyzing Celastraceae species and real commercial samples.

APA, Harvard, Vancouver, ISO, and other styles

30

Singab, Raghda, Ahmed Elissawy, Walid Elkhatib, Mahmoud Yassien, and Nadia Hassouna. "Biotransformation of caffeic acid into a promising biologically active metabolite by Candida albicans isolate CI-24." Archives of Pharmaceutical Sciences Ain Shams University 2, no. 1 (January 1, 2018): 37–46. http://dx.doi.org/10.21608/aps.2018.18733.

Full text

APA, Harvard, Vancouver, ISO, and other styles

31

Keereetaweep, Jantana, and Kent D. Chapman. "Lipidomic Analysis of Endocannabinoid Signaling: Targeted Metabolite Identification and Quantification." Neural Plasticity 2016 (2016): 1–13. http://dx.doi.org/10.1155/2016/2426398.

Full text

Abstract:

The endocannabinoidsN-arachidonoylethanolamide (or anandamide, AEA) and 2-arachidonoylglycerol (2-AG) belong to the larger groups ofN-acylethanolamines (NAEs) and monoacylglycerol (MAG) lipid classes, respectively. They are biologically active lipid molecules that activate G-protein-coupled cannabinoid receptors found in various organisms. After AEA and 2-AG were discovered in the 1990s, they have been extensively documented to have a broad range of physiological functions. Along with AEA, several NAEs, for example,N-palmitoylethanolamine (PEA),N-stearoylethanolamine (SEA), andN-oleoylethanolamine (OEA) are also present in tissues, usually at much larger concentrations than AEA. Any perturbation that involves the endocannabinoid pathway may subsequently alter basal level or metabolism of these lipid mediators. Further, the altered levels of these molecules often reflect pathological conditions associated with tissue damage. Robust and sensitive methodologies to analyze these lipid mediators are essential to understanding how they act as endocannabinoids. The recent advances in mass spectrometry allow researchers to develop lipidomics approaches and several methodologies have been proposed to quantify endocannabinoids in various biological systems.

APA, Harvard, Vancouver, ISO, and other styles

32

WA, Elkhateeb. "Lichentherapy: Highlights on the Pharmaceutical Potentials of Lichens." Open Access Journal of Microbiology & Biotechnology 6, no. 2 (2021): 1–10. http://dx.doi.org/10.23880/oajmb-16000190.

Full text

Abstract:

Lichens exist in every continent and have a history of being used as food, medicine, a source of dyes and animal feed. Lichens are now being used as natural indicators of climate change and for air quality monitoring worldwide. Lichens play an important role in many ecosystems and exist as a symbiotic association between fungi and algae or cyanobacteria. This symbiosis results in the production of unique secondary metabolites known as lichen substances, which arise within the thalli and are typically in crystal form on the surface of the fungal hyphae. Recently, lichens and their secondary metabolites have been receiving increased attention due to their nutritional value and pharmaceutical potential. This review aims to highlight on the importance and variety of common lichen substances (secondary metabolites). Finally, the commercialization of lichens is growing but, in the future, metabolic and biotechnological approaches can be used as an alternative product to overcome the limited availability of biologically active, commercially valuable and medicinally important secondary metabolite components.

APA, Harvard, Vancouver, ISO, and other styles

33

Krohn, Karsten, Karsten Beckmann, Hans-Jürgen Aust, Siegfried Draeger, Barbara Schulz, Stefan Busemann, and Gerhard Bringmann. "Biologically Active Metabolites from Fungi, 10. Generation of the Palmarumycin Spiroacetal Framework by Oxidative Cyclization of an Open Chain Metabolite fromConiothyrium palmarum." Liebigs Annalen 1997, no. 12 (December 1997): 2531–34. http://dx.doi.org/10.1002/jlac.199719971216.

Full text

APA, Harvard, Vancouver, ISO, and other styles

34

Krishnamoorthy, Rajapandiyan, Abdulraheem R. Adisa, Vaiyapuri Subbarayan Periasamy, Jegan Athinarayanan, Subash-Babu Pandurangan, and Ali A. Alshatwi. "Colonic Bacteria-Transformed Catechin Metabolite Response to Cytokine Production by Human Peripheral Blood Mononuclear Cells." Biomolecules 9, no. 12 (December 5, 2019): 830. http://dx.doi.org/10.3390/biom9120830.

Full text

Abstract:

Human gut microbes are a profitable tool for the modification of food compounds into biologically active metabolites. The biological properties of catechins have been extensively investigated. However, the bioavailability of catechin in human blood plasma is very low. This study aimed to determine the biotransformed catechin metabolites and their bioactive potentials for modulating the immune response of human peripheral blood mononuclear cells (PBMCs). Biotransformation of catechin was carried out using in-vitro gut microbial biotransformation method, the transformed metabolites were identified and confirmed by gas chromatography-mass spectrometry (GC–MS) and high-performance liquid chromatography-mass spectrometry (HPLC–MS). Present observations confirmed that the catechin was biotransformed into 11 metabolites upon microbial dehydroxylation and C ring cleavage. Further, immunomodulatory potential of catechin metabolites was analyzed in peripheral blood mononuclear cells (PBMCs). We found up-regulation of anti-inflammatory cytokine (IL-4, IL-10) and down-regulation of pro-inflammatory (IL-16, IL-12B) cytokine may be due to Th2 immune response. In conclusion, biotransformed catechin metabolites enhance anti-inflammatory cytokines which is beneficial for overcoming inflammatory disorders.

APA, Harvard, Vancouver, ISO, and other styles

35

Weisell, Janne, Jouko Vepsäläinen, and Petri A. Turhanen. "Two strategies for the synthesis of the biologically important ATP analogue ApppI, at a multi-milligram scale." Beilstein Journal of Organic Chemistry 11 (November 13, 2015): 2189–93. http://dx.doi.org/10.3762/bjoc.11.237.

Full text

Abstract:

Two strategies for the synthesis of the ATP (adenosine triphosphate) analogue ApppI [1-adenosin-5’-yl 3-(3-methylbut-3-enyl)triphosphoric acid diester] (1) are described. ApppI is an active metabolite of the mevalonate pathway and thus is of major biological significance. Chemically synthezised ApppI was purified by using triethylammonium bicarbonate as the counter ion in ion-pair chromatography and characterized by 1H, 13C, 31P NMR and MS spectroscopical methods.

APA, Harvard, Vancouver, ISO, and other styles

36

Hosny, Noha M., Katherine Huddersman, Noha N. Atia, and Samia M. El-Gizawy. "Novel Heterogeneous Fenton’s-Like Catalysis for Degradation of Colchicine Coupled with Extraction of Its Biologically Active Metabolite." Journal of Molecular Liquids 295 (December 2019): 111870. http://dx.doi.org/10.1016/j.molliq.2019.111870.

Full text

APA, Harvard, Vancouver, ISO, and other styles

37

Jacyno, John M., John S. Harwood, Horace G. Cutler, and Deanne M. Dulik. "Structure and solution-state conformation of botcinolide, a new biologically active metabolite from the fungus Botrytis cinerea." Tetrahedron 50, no. 40 (January 1994): 11585–92. http://dx.doi.org/10.1016/s0040-4020(01)85653-2.

Full text

APA, Harvard, Vancouver, ISO, and other styles

38

Siu-Caldera, Mei-Ling, Sara Peleg, Anne-Marie Kissmeyer, Lise Binderup, and G. Satyanarayana Reddy. "Metabolism of 1α,25(OH)2-20-epi-D3 Into a Stable, Biologically Active, Intermediary Metabolite. † 418." Pediatric Research 41 (April 1997): 72. http://dx.doi.org/10.1203/00006450-199704001-00438.

Full text

APA, Harvard, Vancouver, ISO, and other styles

39

Naidoo, Devashan, Lenka Poštová Slavětínská, Adeyemi O. Aremu, Jiri Gruz, Ondrej Biba, Karel Doležal, Johannes Van Staden, and Jeffrey F. Finnie. "Metabolite profiling and isolation of biologically active compounds fromScadoxus puniceus, a highly traded South African medicinal plant." Phytotherapy Research 32, no. 4 (December 11, 2017): 625–30. http://dx.doi.org/10.1002/ptr.6000.

Full text

APA, Harvard, Vancouver, ISO, and other styles

40

Chen, Jianchun, Jian-Kang Chen, John R. Falck, Siddam Anjaiah, Jorge H. Capdevila, and Raymond C. Harris. "Mitogenic Activity and Signaling Mechanism of 2-(14,15- Epoxyeicosatrienoyl)Glycerol, a Novel Cytochrome P450 Arachidonate Metabolite." Molecular and Cellular Biology 27, no. 8 (February 5, 2007): 3023–34. http://dx.doi.org/10.1128/mcb.01482-06.

Full text

Abstract:

ABSTRACT Arachidonic acid is an essential constituent of cell membranes that is esterified to the sn-2 position of glycerophospholipids and is released from selected phospholipid pools by tightly regulated phospholipase cleavage. Metabolism of the released arachidonic acid by the cytochrome P450 enzyme system (cP450) generates biologically active compounds, including epoxyeicosatrienoic acids (EETs) and hydroxyeicosatetraenoic acids. Here we report that 2-(14,15-epoxyeicosatrienoyl)glycerol (2-14,15-EG), a novel cP450 arachidonate metabolite produced in the kidney, is a potent mitogen for renal proximal tubule cells. This effect is mediated by activation of tumor necrosis factor alpha-converting enzyme (ADAM17), which cleaves membrane-bound transforming growth factor α (proTGF-α) and releases soluble TGF-α as a ligand that binds and activates epidermal growth factor receptor (EGFR). The present studies additionally demonstrate that the structurally related 14,15-EET stimulates release of soluble heparin-binding EGF-like growth factor as an EGFR ligand by activation of ADAM9, another member of the ADAM family. Thus, in addition to the characterization of 2-14,15-EG's mitogenic activity and signaling mechanism, our study provides the first example that two structurally related biologically active lipid mediators can activate different metalloproteinases and release different EGFR ligands in the same cell type to activate EGFR and stimulate cell proliferation.

APA, Harvard, Vancouver, ISO, and other styles

41

HASEGAWA, Hideo, Ryuichi SUZUKI, Chisato WAKABAYASHI, Jun MURATA, Yasuhiro TEZUKA, Ikuo SAIKI, and Shigetoshi KADOTA. "Synthesis of a Biologically Active Fluorescent Derivative of GM1, a Main Ginseng Saponin Metabolite Formed by Intestinal Bacteria." Biological & Pharmaceutical Bulletin 21, no. 5 (1998): 513–16. http://dx.doi.org/10.1248/bpb.21.513.

Full text

APA, Harvard, Vancouver, ISO, and other styles

42

Mawer, E. B., M. Davies, P. E. Still, G. Jones, J. C. Knutson, and C. W. Bishop. "1,24(S)-Dihydroxyvitamin D2, a biologically active analogue of vitamin D, is a naturally occurring metabolite in humans." Bone 17, no. 3 (September 1995): 321. http://dx.doi.org/10.1016/8756-3282(95)97356-k.

Full text

APA, Harvard, Vancouver, ISO, and other styles

43

Al-oanzi, Ziad H., Stephen P. Tuck, Nicholas Raj, John S. Harrop, Gregory D. Summers, David B. Cook, Roger M. Francis, and Harish K. Datta. "Assessment of Vitamin D Status in Male Osteoporosis." Clinical Chemistry 52, no. 2 (February 1, 2006): 248–54. http://dx.doi.org/10.1373/clinchem.2005.059568.

Full text

Abstract:

Abstract Background: Clinical assessment of vitamin D status often relies on measuring total circulating 25-hydroxyvitamin D3 (25OHD3), but much of each vitamin D metabolite is bound to plasma vitamin D–binding protein (DBP), such that the percentage of free vitamin is very low. We hypothesized that measurement of free rather than total 1,25-dihydroxyvitamin D3 [1,25(OH)2D3] and 25OHD3 may provide better assessment of vitamin D status. We therefore aimed to assess vitamin D status in men with idiopathic osteoporosis, in whom possible secondary causes of osteoporosis had been excluded, and to determine the extent of change in biologically active “free” vitamin D caused by variation in plasma DBP concentrations. Methods: We measured 1,25(OH)2D3 and 25OHD3 in plasma samples from 56 men with idiopathic osteoporosis [mean (SD) age, 59.6 (13.6) years; range, 21–86 years] and 114 male controls [62.4 (10.4) years; range, 44–82 years]. Results: Mean total plasma 25OHD3 in the 56 men with osteoporosis and the 114 controls was 44.7 (21) and 43.3 (17) nmol/L, respectively; total plasma 1,25(OH)2D3 measured in randomly selected men with osteoporosis (n = 50) and controls (n = 50) was 90 (37) and 103 (39) pmol/L, respectively. Mean plasma DBP was significantly higher (P <0.001) in men with osteoporosis [224 (62) mg/L; n = 56] than in the controls [143 (34) mg/L; n = 114], but calculated free plasma 25OHD3 and 1,25(OH)2D3 were significantly lower in the osteoporotic men than in controls [6.1 (3.1) vs 9.1 (4.4) pmol/L (P <0.00001) and 77 (37) vs 142 (58) fmol/L (P <0.00001), respectively]. Conclusions: Measurement of total vitamin D metabolites alone, although providing a crude assessment of vitamin D status, may not give an accurate indication of the free (biologically active) form of the vitamin. The ratio of total 25OHD3 and 1,25(OH)2D3 to plasma DBP, rather than total circulating vitamin D metabolites, may provide a more useful index of biological activity. Further studies are required to substantiate this hypothesis.

APA, Harvard, Vancouver, ISO, and other styles

44

Weidle, Paul J., Clement Zeh, Amy Martin, Richard Lando, Frank Angira, Joseph Osoga, Paul Ogindo, Sonali Girde, Timothy D. Minniear, and Timothy K. Thomas. "Nelfinavir and Its Active Metabolite, Hydroxy-t-Butylamidenelfinavir (M8), Are Transferred in Small Quantities to Breast Milk and Do Not Reach Biologically Significant Concentrations in Breast-Feeding Infants Whose Mothers Are Taking Nelfinavir." Antimicrobial Agents and Chemotherapy 55, no. 11 (August 29, 2011): 5168–71. http://dx.doi.org/10.1128/aac.05273-11.

Full text

Abstract:

ABSTRACTAntiretroviral drugs cross from maternal plasma to breast milk and from breast milk to the infant in different concentrations. We measured concentrations of nelfinavir and its active metabolite (M8) in maternal plasma and breast milk from women and in dried blood spots collected from their infants at delivery and postnatal weeks 2, 6, 14, and 24 in the Kisumu Breastfeeding Study, Kisumu, Kenya. Nelfinavir-based antiretroviral regimens given to mothers as prevention of mother-to-child HIV transmission (PMTCT) do not expose the breast-feeding infant to biologically significant concentrations of nelfinavir or M8.

APA, Harvard, Vancouver, ISO, and other styles

45

Neacsu, Madalina, Vassilios Raikos, Yara Benavides-Paz, Sylvia H. Duncan, Gary J. Duncan, James S. Christie, Alexandra M. Johnstone, and Wendy R. Russell. "Sapogenol is a Major Microbial Metabolite in Human Plasma Associated with High Protein Soy-Based Diets: The Relevance for Functional Food Formulations." Foods 9, no. 4 (April 3, 2020): 422. http://dx.doi.org/10.3390/foods9040422.

Full text

Abstract:

Legumes are a source of health-promoting macro- and micronutrients, but also contain numerous phytochemicals with useful biological activities, an example of which are saponins. Epidemiological studies suggest that saponins may play a role in protection from cancer and benefit human health by lowering cholesterol. Therefore, they could represent good candidates for specialised functional foods. Following the consumption of a soya-rich high-protein weight-loss diet (SOYA HP WL), the concentrations of Soyasaponin I (SSI) and soyasapogenol B (SSB) were determined in faecal samples from human volunteers (n = 10) and found to be between 1.4 and 17.5 mg per 100 g fresh faecal sample. SSB was the major metabolite identified in volunteers’ plasma (n = 10) after consumption of the soya test meal (SOYA MEAL); the postprandial (3 h after meal) plasma concentration for SSB varied between 48.5 ng/mL to 103.2 ng/mL. The metabolism of SSI by the gut microbiota (in vitro) was also confirmed. This study shows that the main systemic metabolites of soyasaponin are absorbed from the gut and that they are bioavailable in plasma predominantly as conjugates of sapogenol. The metabolism and bioavailability of biologically active molecules represent key information necessary for the efficient development of functional foods.

APA, Harvard, Vancouver, ISO, and other styles

46

Paponov, Martina, Manya Antonyan, Rune Slimestad, and Ivan A. Paponov. "Decoupling of Plant Growth and Accumulation of Biologically Active Compounds in Leaves, Roots, and Root Exudates of Hypericum perforatum L. by the Combination of Jasmonate and Far-Red Lighting." Biomolecules 11, no. 9 (August 27, 2021): 1283. http://dx.doi.org/10.3390/biom11091283.

Full text

Abstract:

The plant hormone jasmonic acid (JA) fine tunes the growth–defense dilemma by inhibiting plant growth and stimulating the accumulation of secondary compounds. We investigated the interactions between JA and phytochrome B signaling on growth and the accumulation of selected secondary metabolites in Hypericum perforatum L., a medically important plant, by spraying plants with methyl jasmonate (MeJA) and by adding far-red (FR) lighting. MeJA inhibited plant growth, decreased fructose concentration, and enhanced the accumulation of most secondary metabolites. FR enhanced plant growth and starch accumulation and did not decrease the accumulation of most secondary metabolites. MeJA and FR acted mostly independently with no observable interactions on plant growth or secondary metabolite levels. The accumulation of different compounds (e.g., hypericin, flavonols, flavan-3-ols, and phenolic acid) in shoots, roots, and root exudates showed different responses to the two treatments. These findings indicate that the relationship between growth and secondary compound accumulation is specific and depends on the classes of compounds and/or their organ location. The combined application of MeJA and FR enhanced the accumulation of most secondary compounds without compromising plant growth. Thus, the negative correlations between biomass and the content of secondary compounds predicted by the growth-defense dilemma were overcome.

APA, Harvard, Vancouver, ISO, and other styles

47

Helaly, Soleiman E., Wilawan Kuephadungphan, Patima Phainuphong, Mahmoud A. A. Ibrahim, Kanoksri Tasanathai, Suchada Mongkolsamrit, Janet Jennifer Luangsa-ard, Souwalak Phongpaichit, Vatcharin Rukachaisirikul, and Marc Stadler. "Pigmentosins from Gibellula sp. as antibiofilm agents and a new glycosylated asperfuran from Cordyceps javanica." Beilstein Journal of Organic Chemistry 15 (December 16, 2019): 2968–81. http://dx.doi.org/10.3762/bjoc.15.293.

Full text

Abstract:

In the course of our exploration of the Thai invertebrate-pathogenic fungi for biologically active metabolites, pigmentosin A (1) and a new bis(naphtho-α-pyrone) derivative, pigmentosin B (2), were isolated from the spider-associated fungus Gibellula sp. Furthermore, a new glycosylated asperfuran 3, together with one new (6) and two known (4 and 5) cyclodepsipeptides, was isolated from Cordyceps javanica. The pigmentosins 1 and 2 showed to be active against biofilm formation of Staphylococcus aureus DSM1104. The lack of toxicity toward the studied microorganism and cell lines of pigmentosin B (2), as well as the antimicrobial effect of pigmentosin A (1), made them good candidates for further development for use in combination therapy of infections involving biofilm-forming S. aureus. The structure elucidation and determination of the absolute configuration were accomplished using a combination of spectroscopy, including 1D and 2D NMR, HRMS, Mosher ester analysis, and comparison of calculated/experimental ECD spectra. A chemotaxonomic investigation of the secondary metabolite profiles using analytical HPLC coupled with diode array detection and mass spectrometry (HPLC–DAD–MS) revealed that the production of pigmentosin B (2) was apparently specific for Gibellula sp., while the glycoasperfuran 3 was specific for C. javanica.

APA, Harvard, Vancouver, ISO, and other styles

48

Fiorito, Serena, Federica Ianni, Francesca Preziuso, Francesco Epifano, Luca Scotti, Tonino Bucciarelli, and Salvatore Genovese. "UHPLC-UV/Vis Quantitative Analysis of Hydroxylated and O-prenylated Coumarins in Pomegranate Seed Extracts." Molecules 24, no. 10 (May 22, 2019): 1963. http://dx.doi.org/10.3390/molecules24101963.

Full text

Abstract:

A simple and rapid analytical UHPLC methodology with spectrophotometric (UV/Vis) detection, coupled with different extraction procedures, has been perfected to investigate the presence of biologically active O-prenylated umbelliferone derivatives, such as auraptene and umbelliprenin, in pomegranate (Punica granatum L.) seed extracts. Absolute ethanol was the most efficient extraction solvent in terms of yields, after a short ultrasound-assisted. The highest concentration values recorded under these experimental conditions were 1.99 μg/g of dry extract and 6.53 μg/g for auraptene and umbelliprenin, respectively. The parent metabolite umbelliferone was also detected (0.67 μg/g). The extraction and UHPLC analytical methodology set up in the present study proved to be an efficient, powerful, and versatile technique for the simultaneous qualitative analysis and quantification of oxyprenylated coumarins in pomegranate seed extracts. The characterization of such secondary metabolites in the mentioned phytopreparation represents, to the best of our knowledge, the first example in the literature.

APA, Harvard, Vancouver, ISO, and other styles

49

Van Scott, M. R., M. R. McIntire, and D. C. Henke. "Arachidonic acid metabolism and regulation of ion transport in rabbit Clara cells." American Journal of Physiology-Lung Cellular and Molecular Physiology 259, no. 4 (October 1, 1990): L213—L221. http://dx.doi.org/10.1152/ajplung.1990.259.4.l213.

Full text

Abstract:

Sonicates of freshly isolated Clara cells produced thromboxane B2 (TxB2), prostaglandin (PG) D2, PGE2, PGF2 alpha, hydroxyheptadecatrienoic acid (HHT), and 12-hydroxyeicosatetraenoic acid (12-HETE) as detected using high-performance liquid chromatography (HPLC). Sonicates of Clara cells cultured on collagen matrices produced the same metabolites. Rates of [3H]arachidonic acid metabolism increased in culture, but the changes were not associated with changes in cell number. Sonicates of freshly isolated tracheal cells produced mainly 12-HETE. Cyclooxygenase products were not produced consistently. Sonicates of tracheal cultures produced significant quantities of TxB2, PGD2, PGE2, PGF2 alpha, and HHT, but 12-HETE remained the major metabolite. Equivalent short-circuit current (Ieq) across cultured Clara cell epithelia was unaffected by bilateral exposure to TxB2, PGD2, PGE2, PGF2 alpha, HHT, or 12-HETE. A minor (1%) decrease in transepithelial resistance (Rt) followed exposure to PGD2. Indomethacin had no significant effect on Rt or Ieq, but exposure of indomethacin-pretreated preparations to PGE2 revealed a minor (2%) increase in Ieq. In contrast, tracheal cell epithelia exhibited significant changes in Rt and Ieq in response to PGF2 alpha, PGE2, and HHT. These results indicate that Clara cells metabolize arachidonic acid to biologically active eicosanoids, but the resulting products do not play a major role in regulation of transepithelial ion transport by this cell type.

APA, Harvard, Vancouver, ISO, and other styles

50

Seidi, Zahra, Esfandiar Fateh, and Amir Aynehband. "Changes in secondary metabolite and biologically active compounds of Ajowan (Trachyspermum ammi L.) upon organic and conventional production systems." Acta Ecologica Sinica 41, no. 3 (June 2021): 215–22. http://dx.doi.org/10.1016/j.chnaes.2021.02.009.

Full text

APA, Harvard, Vancouver, ISO, and other styles

Journal articles on the topic 'Biologically active metabolite'

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles