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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Joo, Jeongmin Lee, Doohyun Wu, Zhexue Shin, Jung-Hoon Lee, Hye Suk Kwon, Byoung-Mog Huh, Tae-Lin Kim, Yang-Weon Lee, Su-Jun Kim, Tae Wan Lee, Taeho Liu, Kwang-Hyeon |
| Description | Author Affiliation: Joo J ( College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu, Korea.) |
| Abstract | Obovatol, a major constituent of the leaves of Magnolia obovata Thunb, is known to inhibit nuclear factor-κB activity and arachidonic acid-induced platelet aggregation. This study was performed to identify the metabolites of obovatol in human liver microsomes. Human liver microsomes incubated with obovatol in the presence of NADPH and/or UDPGA resulted in the formation of six metabolites, M1-M6. M1 and M2 were identified as hydroxyobovatol, on the basis of liquid chromatography/tandem mass spectrometric (LC-MS/MS) analysis. M1, M2 and obovatol were further metabolized to their glucuronide conjugates, obovatol-glucuronide (M3), obovatol-diglucuronide (M4) and hydroxyobovatol-glucuronide (M5 and M6). The inhibitory potency of obovatol on eight major human P450s was also investigated in human liver microsomes. In these experiments, obovatol strongly inhibited CYP2C19-mediated S-mephenytoin hydroxylase activity with an IC(50) value of 0.8 µM, which could have implications for drug-drug interactions. |
| File Format | HTM / HTML |
| ISSN | 01422782 |
| Issue Number | 4 |
| Volume Number | 34 |
| e-ISSN | 1099081X |
| Journal | Biopharmaceutics & Drug Disposition |
| Language | English |
| Publisher | Wiley |
| Publisher Date | 2013-05-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Discipline Pharmacology Cytochrome P-450 Enzyme System Drug Effects Microsomes, Liver Enzymology Phenyl Ethers Pharmacology Aryl Hydrocarbon Hydroxylases Metabolism Chromatography, Liquid Cytochrome P-450 Cyp2c19 Humans Inhibitory Concentration 50 Magnolia Chemistry Nadp Administration & Dosage Tandem Mass Spectrometry Uridine Diphosphate Glucuronic Acid Journal Article Research Support, Non-u.s. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology Pharmacology (medical) Pharmaceutical Science |
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