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Effects of natural products on the function of human organic anion transporting polypeptide 1B1.
- Source :
-
Xenobiotica . Apr2012, Vol. 42 Issue 4, p339-348. 10p. 1 Chart, 2 Graphs. - Publication Year :
- 2012
-
Abstract
- In this study, the effects of 136 naturally occurring products, which have been reported to play important roles in modification of Cytochrome P450 (CYP450) activities, on the uptake of estrone-3-sulfate (E3S), a typical OATP1B1 substrate, were evaluated using human embryonic kidney 293 cells stably expressing OATP1B1. At a concentration of 100 μM, 42 natural products inhibited OATP1B1-mediated [3H]E3S uptake by more than 50%, and five of them significantly inhibited OATP1B1-mediated [3H]E3S by more than 80% with the following rank order of potency: quercetin > astragaloside IV > icariin > glycyrrhizic acid > ginsenoside Rc. Inhibitory effects of these natural products on OATP1B1 activity were in a concentration-dependent manner. 11 natural compounds were found exhibiting greater than 50% inhibition at 30 μM with IC50 values ranging from 14.6 ± 3.3 to 28.5 ± 3.0 μM. In conclusion, our data suggest that modification of OATP1B1 transport activity by these natural occurring products may be a mechanism for natural product–drug interactions in humans. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 00498254
- Volume :
- 42
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- Xenobiotica
- Publication Type :
- Academic Journal
- Accession number :
- 72409103
- Full Text :
- https://doi.org/10.3109/00498254.2011.623796