In vitro assessment of 36 CYP2C9 allelic isoforms found in the Chinese population on the metabolism of glimepiride.
作者： Da-Peng Dai , Shuang-Hu Wang , Pei-Wu Geng , Guo-Xin Hu , Jian-Ping Cai
DOI: 10.1111/BCPT.12159
关键词:
摘要: Of the 57 reported CYP2C9 alleles, to date, 36 of them have been identified in Chinese population. The aim this study was assess catalytic characteristics these allelic isoforms and their effects on metabolism glimepiride vitro. Baculovirus-mediated expressing system used highly express wild-type 35 variants insect cell microsomes. Then, enzymatic each variant were evaluated using as substrate. Reactions performed at 37°C with microsomes 0.125–10 μM for 40 min. After termination, products extracted signal collection by LC-MS/MS. tested isoforms, only four (CYP2C9.40, CYP2C9.47, CYP2C9.51 CYP2C9.54) exhibited similar relative clearance values that CYP2C9.1. In addition, one (CYP2C9.36) showed a higher intrinsic value than protein, while remaining 30 significantly decreased (from 0.1% 87.2%) compared This provided most comprehensive data activities all population regard commonly antidiabetic drug, glimepiride. Our results indicate rare alleles decrease activity towards hydroxylation
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