Hepatic Metabolism of Sakuranetin and Its Modulating Effects on Cytochrome P450s and UDP-Glucuronosyltransferases.

作者: Hyesoo Jeong , Jimin Lee , Soolin Kim , Yoo Yeo , Hyunyoung So

DOI: 10.3390/MOLECULES23071542

关键词: EriodictyolNaringeninMetabolic pathwayCYP2B6BiochemistryChemistryDrug metabolismMicrosomeCytochrome P450Sakuranetin

摘要: Sakuranetin (SKN), found in cherry trees and rice, is a flavanone with various pharmacological activities. It biosynthesized from naringenin rice or trees, the metabolism of SKN has been studied non-human species. The present study aimed to investigate metabolic pathways human liver microsomes identify phase I II metabolites, as well evaluate potential for drug–herb interactions through modulation drug metabolizing enzymes (DMEs). HPLC-DAD HPLC-electrospray mass spectrometry were used stability metabolites incubated SKN. inhibit DMEs was evaluated by monitoring formation DME-specific product. cytochrome P450 2B6 3A4-inductive effects using promoter reporter assays hepatocarcinoma cells. major include B-ring hydroxylation, 5-O-demethylation, conjugation glutathione glucuronic acid. identified eriodictyol. be UDP-glucuronosyltransferases (UGT) 1A9 inhibitor, whereas it induced transactivation pregnane X receptor-mediated (CYP) 3A4 gene.

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