AI Article Synopsis
- - The extract studied is used in East Asia for various conditions like diarrhea, inflammation, and fever and is rich in prenylated flavonoids, including sophoraflavone and kushenol.
- - The research found that the extract inhibited several cytochrome P450 (CYP) enzymes, which are important for drug metabolism, with varying levels of inhibition for each enzyme.
- - Prenylated flavonoids showed selective inhibition of CYP isoforms, suggesting that the extract may impact drug interactions when taken with medications relying on these enzymes for metabolism.
Article Abstract
possesses several pharmacological properties and has been widely used for the treatment of diarrhea, inflammation, abscess, dysentery, and fever in East Asian countries. is a major source of prenylated flavonoids, such as sophoraflavone and kushenol. In this study, we examined the effects of extract and its prenylated flavonoids on cytochrome P450 (CYP) isoform activity in human liver microsomes. The extract inhibited CYP2C8, CYP2C9, CYP2C19, and CYP3A activities, with IC values of 1.42, 13.6, 19.1, and 50 g/mL, respectively. CYP2B6 was only inhibited in human liver microsomes preincubated with the extract. CYP3A4 was more strongly inhibited by the extract in the presence of NADPH, suggesting that the extract may inhibit CYP2B6 and CYP3A4 via mechanism-based inactivation. Prenylated flavonoids also inhibited CYP isoforms with different selectivity and modes of action. Kushenol I, leachianone A, and sophoraflavone G inhibited CYP2B6, whereas kushenol C, kushenol I, kushenol M, leachianone A, and sophoraflavone G inhibited CYP3A4 via mechanism-based inhibition. Our results suggest that may contribute to herb-drug interactions when coadministered with drugs metabolized by CYP2B6, CYP2C8, CYP2C9, and CYP3A4.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6436327 | PMC |
| http://dx.doi.org/10.1155/2019/2673769 | DOI Listing |
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