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Characterization of metabolic activity, isozyme contribution and species differences of bavachin, and identification of efflux transporters for bavachin‐O‐glucuronide in HeLa1A1 cells

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Characterization of metabolic activity, isozyme contribution and species differences of bavachin, and identification of efflux transporters for bavachin‐O‐glucuronide in HeLa1A1 cells

Journal of Pharmacy and Pharmacology

Fecha de publicación: 9 de julio de 2020

DOI: https://doi.org/10.1111/jphp.13324

Autores: Yang Li, Chunxia Xu, Jinjin Xu, Zifei Qin, Shishi Li, Liufang Hu, Zhihong Yao, Frank J. Gonzalez, Xinsheng Yao

Background: Bavachin is a bioactive natural flavonoid with oestrogen‐like activity. Here, we aimed to investigate its metabolic and disposal fates involving in CYPs, UGTs and efflux transporters.

Methods: Phase I metabolism and glucuronidation were performed by human liver microsomes (HLM). Reaction phenotyping and activity correlation analysis were performed to identify the main CYP and UGT isozymes. Chemical inhibition and gene knock‐down approaches were employed to explore the function of BCRP and MRPs.

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