Investigation on the metabolic characteristics of isobavachin in Psoralea corylifolia L. (Bu-gu-zhi) and its potential inhibition against human cytochrome P450s and UDP-glucuronosyltransferases.

ABSTRACT:

Objectives

Isobavachin is a phenolic with anti-osteoporosis activity. This study aimed to explore its metabolic fates in vivo and in vitro, and to investigate the potential drug-drug interactions involving CYPs and UGTs.

Methods

Metabolites of isobavachin in mice were first identified and characterized. Oxidation and glucuronidation study were performed using liver and intestine microsomes. Reaction phenotyping, activity correlation analysis and relative activity factor approaches were employed to identify the main CYPs and UGTs involved in isobavachin metabolism. Through kinetic modelling, inhibition mechanisms towards CYPs and UGTs were also explored.

Key findings

Two glucuronides (G1 - G2) and three oxidated metabolites (M1 - M3) were identified in mice. Additional

SUBMITTER: Xing H 

PROVIDER: S-EPMC8861878 | biostudies-literature | 2020 Dec

REPOSITORIES: biostudies-literature