Interaction of myricetin, ampelopsin (dihydromyricetin), and their sulfate metabolites with serum albumin, cytochrome P450 (CYP2C9, 2C19, and 3A4) enzymes, and organic anion-transporting polypeptides (OATP1B1 and OATP2B1)

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388971%3A_____%2F24%3A00599120" target="_blank" >RIV/61388971:_____/24:00599120 - isvavai.cz</a>

Result on the web

<a href="https://bpspubs.onlinelibrary.wiley.com/doi/10.1002/prp2.70021" target="_blank" >https://bpspubs.onlinelibrary.wiley.com/doi/10.1002/prp2.70021</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1002/prp2.70021" target="_blank" >10.1002/prp2.70021</a>

Result language

angličtina

Original language name

Interaction of myricetin, ampelopsin (dihydromyricetin), and their sulfate metabolites with serum albumin, cytochrome P450 (CYP2C9, 2C19, and 3A4) enzymes, and organic anion-transporting polypeptides (OATP1B1 and OATP2B1)

Original language description

Myricetin (MYR) and ampelopsin (AMP, or dihydromyricetin) are flavonoid aglycones found in certain plants and dietary supplements. During the presystemic biotransformation of flavonoids, mainly sulfate and glucuronide derivatives are produced, which are the dominant metabolites in the circulation. In this study, we tested the interactions of MYR, myricetin-3 '-O-sulfate (M3 ' S), AMP, and ampelopsin-4 '-O-sulfate (A4 ' S) with human serum albumin (HSA), cytochrome P450 enzymes (CYPs), and organic anion-transporting polypeptides (OATPs) using in vitro models, including the recently developed method for measuring flavonoid levels in living cells. M3 ' S and MYR bound to albumin with high affinity, and they showed moderate displacing effects versus the Site I marker warfarin. MYR, M3 ' S, AMP, and A4 ' S exerted no or only minor inhibitory effects on CYP2C9, CYP2C19, and CYP3A4 enzymes. M3 ' S and MYR caused considerable inhibitory actions on OATP1B1 at low micromolar concentrations (IC50 = 1.7 and 6.4 mu M, respectively), while even their nanomolar levels resulted in strong inhibitory effects on OATP2B1 (IC50 = 0.3 and 0.4 mu M, respectively). In addition, M3 ' S proved to be a substrate of OATP1B1 and OATP2B1. These results suggest that MYR-containing dietary supplements may affect the OATP-mediated transport of certain drugs, and OATPs are involved in the tissue uptake of M3 ' S.

Czech name

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Czech description

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Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

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OECD FORD branch

30104 - Pharmacology and pharmacy

Project

<a href="/en/project/GA23-04654S" target="_blank" >GA23-04654S: Chemoenzymatic preparation and biological activity of metabolites of food polyphenols</a><br>

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2024

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Pharmacology Research & Perspectives

ISSN

2052-1707

e-ISSN

2052-1707

Volume of the periodical

12

Issue of the periodical within the volume

5

Country of publishing house

GB - UNITED KINGDOM

Number of pages

12

Pages from-to

e70021

UT code for WoS article

001324324900001

EID of the result in the Scopus database

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