Effect ofDioscorea bulbiferaand its Major Bioactive Compound, Diosgenin on CYP450 Mediated Drug Metabolism
| Autor: | Govind Prasad Dubey, Kaliappan Ilango, Thangavel Mahalingam Vijayakumar, Aruna Agrawal, Ramasamy Mohan Kumar |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Pharmacology
chemistry.chemical_classification biology CYP3A4 Dioscorea bulbifera Cytochrome P450 Plant Science Sapogenin Diosgenin Toxicology biology.organism_classification Agricultural and Biological Sciences (miscellaneous) Bioactive compound chemistry.chemical_compound Complementary and alternative medicine chemistry Triterpene Drug Discovery biology.protein Drug metabolism |
| Zdroj: | Journal of Biologically Active Products from Nature. 5:313-321 |
| ISSN: | 2231-1874 2231-1866 |
| Popis: | Cytochrome P450 (CYP450) inhibition by the bioactive molecules of herbs leading to greater potential for toxicity of co-administered drugs. Diosgenin is an important bioactive steroidal sapogenin from Dioscorea bulbifera belonging to the triterpene group and is of great interest to the pharmaceutical industry. The purpose of this study was, to find whether D. bulbifera and Diosgenin influences the effect on rat CYP450 enzymes and its important isoforms (CYP3A4, CYP2D6) by using high through put screening. CYP450-CO Complex assay was performed in rat pooled liver microsomes to calculate percentage inhibition of test samples on CYP450. IC values were determined by fluorometric assays of CYP3A4 and CYP2D6. Mode of inhibition of Diosgenin on these CYPs were further assessed by molecular docking studies with the Glide (Schrodinger Inc. U.S.A.). In CYP450 inhibition assay, the inhibitory potential of herb extract (40.44±1.28 %) was found to be less than positive control (72.08±1.96 %). In fluorometric assay, he... |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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