title: Effects of natural products on the function of human organic anion transporting polypeptide 1B1.
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 [(3)H]E3S uptake by more than 50%, and five of them significantly inhibited OATP1B1-mediated [(3)H]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 IC(50) 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.
authors: Institute of Life Sciences, Chongqing Medical University, Chongqing, PR China.
authors: Lan-Xiang
authors: LX
authors: Wu
authors: Cheng-Xian
authors: CX
authors: Guo
authors: Qiang
authors: Q
authors: Qu
authors: Jing
authors: J
authors: Yu
authors: Wang-Qing
authors: WQ
authors: Chen
authors: Guo
authors: G
authors: Wang
authors: Lan
authors: L
authors: Fan
authors: Qing
authors: Q
authors: Li
authors: Wei
authors: W
authors: Zhang
authors: Hong-Hao
authors: HH
authors: Zhou
mesh_terms: D001688:Biological Products / Q000494:pharmacology*; D001692:Biological Transport; D004970:Estrone / Q000031:analogs & derivatives / Q000378:metabolism; D057809:HEK293 Cells; D006801:Humans; D027381:Liver-Specific Organic Anion Transporter 1; D027361:Organic Anion Transporters / Q000378:metabolism*
chemical_list: D001688:Biological Products; D027381:Liver-Specific Organic Anion Transporter 1; D027361:Organic Anion Transporters; C503999:SLCO1B1 protein, human; D004970:Estrone; C017296:estrone sulfate