Fungal mediated biotransformation of melengestrol acetate, and T-cell proliferation inhibitory activity of biotransformed compounds
| Autor: | Atia-tul-Wahab, Zharylkasyn A. Abilov, Almas Jabeen, Saira Javed, M. Iqbal Choudhary, Shynar Zhumagaliyeva, Atta-ur-Rahman |
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| Rok vydání: | 2020 |
| Předmět: |
medicine.drug_class
T cell T-Lymphocytes 01 natural sciences Biochemistry Anti-inflammatory Melengestrol acetate chemistry.chemical_compound Mice Structure-Activity Relationship Biotransformation Drug Discovery medicine Animals Humans Molecular Biology IC50 Melengestrol Acetate Cell Proliferation Dose-Response Relationship Drug Molecular Structure 010405 organic chemistry Chemistry Organic Chemistry Substrate (chemistry) 3T3 Cells In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry medicine.anatomical_structure Fermentation Seeds Phyllachorales Rhizopus Hormone |
| Zdroj: | Bioorganic chemistry. 104 |
| ISSN: | 1090-2120 |
| Popis: | Glomerella fusaroide, and Rhizopus stolonifer were effectively able to transform the steroidal hormone melengestrol acetate (MGA) (1) into four (4) new metabolites, 17α-acetoxy-11α-hydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dione (2), 17α-acetoxy-11α-hydroxy-6-methyl-16-methylenepregna-1,4,6-triene-3,20-dione (3), 17α-acetoxy-6,7α-epoxy-6β-methyl-16-methylenepregna-4,6-diene-3,20-dione (4), and 17α-acetoxy-11β,15β-dihydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dione (5). All these compounds were structurally characterized by different spectroscopic techniques. The objective of the current study was to assess the anti-inflammatory potential of melengestrol acetate (1), and its metabolites 2–5. The metabolites and the substrate were assessed for their inhibitory effects on proliferation of T-cells in vitro. The substrate (IC50 = 2.77 ± 0.08 µM) and its metabolites 2 (IC50 = 2.78 ± 0.07 µM), 4 (IC50 = 2.74 ± 0.1 µM), and 5 (IC50 = |
| Databáze: | OpenAIRE |
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