Zhen Li and Florence Shin Gee Cheung contributed equally to the work.
Interaction of the Bioactive Flavonol, Icariin, with the Essential Human Solute Carrier Transporters
Article first published online: 21 NOV 2013
© 2013 Wiley Periodicals, Inc.
Journal of Biochemical and Molecular Toxicology
Volume 28, Issue 2, pages 91–97, February 2014
How to Cite
Li, Z., Cheung, F. S. G., Zheng, J., Chan, T., Zhu, L. and Zhou, F. (2014), Interaction of the Bioactive Flavonol, Icariin, with the Essential Human Solute Carrier Transporters. J. Biochem. Mol. Toxicol., 28: 91–97. doi: 10.1002/jbt.21540
- Issue published online: 4 FEB 2014
- Article first published online: 21 NOV 2013
- Manuscript Accepted: 25 OCT 2013
- Manuscript Revised: 13 OCT 2013
- Manuscript Received: 17 SEP 2013
- Solute Carrier Transporters;
Solute carrier transporters (SLCs), in particular the organic anion transporting polypeptides (OATPs) and organic anion/cation transporters (OATs/OCTs), are responsible for the cellular entry of many clinically important drugs in body. They largely influence drug safety and efficacy. Icariin is a flavonol widely present in many herbal preparations, which is used to improve sexual function and prevent osteogenesis. However, precautions are necessary in therapies containing icariin due to its involvement in drug–drug/herb interactions, possibly mediated through competing drug uptake via membrane-transporter proteins. This study is the first to comprehensively evaluate the interactions between icariin and a range of essential SLCs. Our data demonstrated that icariin can significantly inhibit OATP1B3- and OATP2B1-mediated cellular uptake of specific substrates (IC50 of 3.0 ± 1.3 and 6.4 ± 1.9 μM, respectively). Our study revealed that icariin can potentially compete with coadministrated drugs for particular SLCs, which may impact the therapeutic outcome of regimens.