Effects of natural products on the function of human organic anion transporting polypeptide 1B1. 2012

Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
Institute of Life Sciences, Chongqing Medical University, Chongqing, PR China.

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.

UI MeSH Term Description Entries
D004970 Estrone An aromatized C18 steroid with a 3-hydroxyl group and a 17-ketone, a major mammalian estrogen. It is converted from ANDROSTENEDIONE directly, or from TESTOSTERONE via ESTRADIOL. In humans, it is produced primarily by the cyclic ovaries, PLACENTA, and the ADIPOSE TISSUE of men and postmenopausal women. Folliculin (Hormone),Estrone, (+-)-Isomer,Estrone, (8 alpha)-Isomer,Estrone, (9 beta)-Isomer,Estrovarin,Kestrone,Unigen,Wehgen
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001688 Biological Products Complex pharmaceutical substances, preparations, or matter derived from organisms usually obtained by biological methods or assay. Biologic,Biologic Drug,Biologic Product,Biological,Biological Drug,Biological Medicine,Biological Product,Biologics,Biopharmaceutical,Natural Product,Natural Products,Biologic Drugs,Biologic Medicines,Biologic Pharmaceuticals,Biologic Products,Biological Drugs,Biological Medicines,Biologicals,Biopharmaceuticals,Products, Biological,Drug, Biologic,Drug, Biological,Drugs, Biologic,Drugs, Biological,Medicine, Biological,Medicines, Biologic,Medicines, Biological,Pharmaceuticals, Biologic,Product, Biologic,Product, Biological,Product, Natural
D001692 Biological Transport The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments. Transport, Biological,Biologic Transport,Transport, Biologic
D057809 HEK293 Cells A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5. 293T Cells,HEK 293 Cell Line,HEK 293 Cells,Human Embryonic Kidney Cell Line 293,Human Kidney Cell Line 293,293 Cell, HEK,293 Cells, HEK,293T Cell,Cell, 293T,Cell, HEK 293,Cell, HEK293,Cells, 293T,Cells, HEK 293,Cells, HEK293,HEK 293 Cell,HEK293 Cell
D027361 Organic Anion Transporters Proteins involved in the transport of organic anions. They play an important role in the elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body. Membrane Transport Proteins, Organic Anion,OAT Transport Protein,OATP Transporter,Organic Anion Transport Polypeptide,Organic Anion Transport Polypeptides,Organic Anion Transport Protein,Organic Anion Transporter,OAT Transport Proteins,OATP Proteins,OATP Transporters,Organic Anion Transport Proteins,Anion Transporter, Organic,Anion Transporters, Organic,Protein, OAT Transport,Transport Protein, OAT,Transport Proteins, OAT,Transporter, OATP,Transporter, Organic Anion,Transporters, OATP,Transporters, Organic Anion
D027381 Liver-Specific Organic Anion Transporter 1 An organic anion transporter found in human and mouse liver. It is capable of transporting a variety organic anions and mediates sodium-independent uptake of bile in the liver. LST-1 Transport Protein,Organic Anion Transport Polypeptide C,Liver-Specific Organic Anion Transporter, LST-1,Oatp-C Transport Protein,SLC21A6 Transporter,Solute Carrier Family-21(Organic Anion Transporter), Member 6 Protein,LST 1 Transport Protein,Liver Specific Organic Anion Transporter 1,Liver Specific Organic Anion Transporter, LST 1,Oatp C Transport Protein,Transport Protein, LST-1,Transport Protein, Oatp-C,Transporter, SLC21A6

Related Publications

Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
February 2017, Molecular pharmaceutics,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
November 2009, Chemico-biological interactions,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
October 2007, Acta pharmacologica Sinica,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
November 2009, Protein science : a publication of the Protein Society,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
May 2006, Clinical pharmacology and therapeutics,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
January 2012, PloS one,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
September 2023, Pharmaceutics,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
April 2021, Biochimica et biophysica acta. Biomembranes,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
May 2024, Toxicology in vitro : an international journal published in association with BIBRA,
Lan-Xiang Wu, and Cheng-Xian Guo, and Qiang Qu, and Jing Yu, and Wang-Qing Chen, and Guo Wang, and Lan Fan, and Qing Li, and Wei Zhang, and Hong-Hao Zhou
October 2018, Xenobiotica; the fate of foreign compounds in biological systems,
Copied contents to your clipboard!