Document Type

Article

Original Publication Date

2012

Journal/Book/Conference Title

Evidence-Based Complementary and Alternative Medicine

Volume

2012

DOI of Original Publication

10.1155/2012/872458

Comments

Originally published at

http://dx.doi.org/10.1155/2012/872458

Date of Submission

August 2014

Abstract

Many active components of herbal products are small organic anions, and organic anion transporters were previously demonstrated to be a potential site of drug-drug interactions. In this study, we assessed the inhibitory effects of six hydrophilic components of the herbal medicine Danshen, lithospermic acid, protocatechuic acid, rosmarinic acid, salvianolic acid A, salvianolic acid B, and tanshinol, on the function of the murine organic anion transporters, mOat1 and mOat3. All of Danshen components significantly inhibited mOat1- and mOat3-mediated substrate uptake () with lithospermic acid (LSA), protocatechuic acid, rosmarinic acid (RMA), and salvianolic acid A (SAA) producing virtually complete inhibition under test conditions. Kinetic analysis demonstrated that LSA, RMA, and SAA were competitive inhibitors. As such, values were estimated as  μM for LSA,  μM for RMA, and  μM for SAA on mOat1-mediated transport, and as  μM for LSA,  μM for RMA, and  μM for SAA on mOat3-mediated transport. These data suggest that herb-drug interactions may occur in vivo on the human orthologs of these transporters in situations of polypharmacy involving Danshen and clinical therapeutics known to be organic anion transporter substrates.

Rights

Copyright © 2012 Li Wang and Douglas H. Sweet. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Is Part Of

VCU Pharmaceutics Publications

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