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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2014, Vol. 19 ›› Issue (12): 1371-1375.

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“N-in-One Cocktail” method to evaluate inhibition effects of 4-hydroxylmethylphenyl-O-β-D-pyranosyl alloside on CYP450 enzymes

JIA Yuan-wei1, PENG Ying2, SUN Jian-guo2, XIE Hai-tang1, CHU Ji-ru1, SHEN Jie1   

  1. 1Anhui Provincial Center for Drug Clinical Evaluation, Clinical Pharmacy Department, Yijishan Hospital of Wanan Medical College, Wuhu 241001, Anhui, China;
    2Key Laboratory of Pharmacokinetics and Drug Metabolism, China Pharmaceutical University, Nanjing 210009, Jiangsu, China
  • Received:2014-09-12 Revised:2014-11-21 Published:2020-07-20

Abstract: AIM: To investigate potential food-drug or drug-drug interactions, 4-hydroxylmethylphenyl- O-β-D-pyranosyl alloside was evaluated in vitro against human drug-metabolizing cytochrome P450 (CYP) enzymes using “N-in-One Cocktail” method based on UFLC-ESI-MS/MS techniques. METHODS: CYP450 enzyme specific probe drugs were incubated with or without helicid respectively in human microsomes. The specific substrates used in this study were phenacetin (CYP1A2), phenacetin (CYP2D6), chlorzoxazone (CYP2E1), tolbutamide (CYP2C9), omeprazole (CYP2C19, CYP3A), midazolam (CYP3A4), testosterone (CYP3A4), midazolam (CYP2C). The concentrations of nine substrate metabolites were determined. RESULTS: 4-hydroxylmethylphenyl-O-β-D-pyranosyl alloside (0-200 μmol/L) had no significant inhibition on the activities of the stuied cytochrome P450 enzymes. CONCLUSION: 4-hydroxylmethylphenyl-O-β-D-pyranosyl alloside can't arise envents of clinical values through CYP enzyme inhibitions.

Key words: 4-hydroxylmethylphenyl-O-β-D-pyranosyl alloside, human liver microsome, cytochrome P450, inhibition

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