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Molecules 2016, 21(6), 800;

In Vitro Assessment of CYP-Mediated Drug Interactions for Kinsenoside, an Antihyperlipidemic Candidate

Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University, Ansan Gyeonggi-do 426-791, Korea
School of Pharmacy, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, China
Author to whom correspondence should be addressed.
Academic Editor: Marcello Iriti
Received: 7 April 2016 / Revised: 7 June 2016 / Accepted: 15 June 2016 / Published: 18 June 2016
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Kinsenoside, the herb-derived medicine isolated from the plant Anoect chilus, has diverse pharmacological actions, and it is considered to be a promising antihyperlipidemic drug candidate. This study evaluates the effects of kinsenoside on CYP enzyme-mediated drug metabolism in order to predict the potential for kinsenoside-drug interactions. Kinsenoside was tested at different concentrations of 0.1, 0.3, 1, 3, 10, 30, and 100 µM in human liver microsomes. The c Cktail probe assay based on liquid chromatography-tandem mass spectrometry was conducted to measure the CYP inhibitory effect of kinsenoside. Subsequently, the metabolism profiles of amlodipine and lovastatin in human liver microsomes were analyzed following co-incubation with kinsenoside. The concentration levels of the parent drug and the major metabolites were compared with the kinsenoside-cotreated samples. The effect of kinsenoside was negligible on the enzyme activity of all the CYP isozymes tested even though CYP2A6 was slightly inhibited at higher concentrations. The drug-drug interaction assay also showed that the concomitant use of kinsenoside has a non-significant effect on the concentration of lovastatin or amlodipine, and their major metabolites. So, it was concluded that there is almost no risk of drug interaction between kinsenoside and CYP drug substrates via CYP inhibition. View Full-Text
Keywords: kinsenoside; human liver microsomes; drug interactions; CYP inhibition kinsenoside; human liver microsomes; drug interactions; CYP inhibition

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Rehman, S.U.; Choi, M.S.; Kim, I.S.; Luo, Z.; Xue, Y.; Yao, G.; Zhang, Y.; Yoo, H.H. In Vitro Assessment of CYP-Mediated Drug Interactions for Kinsenoside, an Antihyperlipidemic Candidate. Molecules 2016, 21, 800.

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