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      The metabolism and hepatotoxicity of ginkgolic acid (17 : 1) in vitro

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          Abstract

          Pharmacological activities and adverse side effects of ginkgolic acids (GAs), major components in extracts from the leaves and seed coats of Ginkgo biloba L, have been intensively studied. However, there are few reports on their hepatotoxicity. In the present study, the metabolism and hepatotoxicity of GA (17 : 1), one of the most abundant components of GAs, were investigated. Kinetic analysis indicated that human and rat liver microsomes shared similar metabolic characteristics of GA (17 : 1) in phase I and II metabolisms. The drug-metabolizing enzymes involved in GA (17 : 1) metabolism were human CYP1A2, CYP3A4, UGT1A6, UGT1A9, and UGT2B15, which were confirmed with an inhibition study of human liver microsomes and recombinant enzymes. The MTT assays indicated that the cytotoxicity of GA (17 : 1) in HepG2 cells occurred in a time- and dose-dependent manner. Further investigation showed that GA (17 : 1) had less cytotoxicity in primary rat hepatocytes than in HepG2 cells and that the toxicity was enhanced through CYP1A- and CYP3A-mediated metabolism.

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          Author and article information

          Journal
          CJNM
          Chinese Journal of Natural Medicines
          Elsevier
          1875-5364
          20 November 2018
          : 16
          : 11
          : 829-837
          Affiliations
          1Institute of Drug Metabolism and Pharmaceutical Analysis, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Hangzhou 310058, China
          2Department of Pharmacy & Geriatrics Institute of Zhejiang Province, Zhejiang Hospital, Hangzhou 310013, China
          Author notes
          *Corresponding authors: YU Lu-Shan, Tel/Fax: 86-571-88208407, E-mail: zengsu@ 123456zju.edu.cn ; ZENG Su, yuls@ 123456zju.edu.cn

          ΔThese authors contributed to this work equally.

          These authors have no conflict of interest to declare.

          Article
          S1875-5364(18)30124-9
          10.1016/S1875-5364(18)30124-9
          Copyright © 2018 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.
          Funding
          Funded by: National Key Project of China
          Award ID: 2017YFC0908600
          Funded by: National Natural Science Foundation of China
          Award ID: 81173120
          Funded by: National Natural Science Foundation of Zhejiang Province
          Award ID: LQ15H310003
          This study was supported by the National Key Project of China (No. 2017YFC0908600), the National Natural Science Foundation of China (No. 81173120) and the National Natural Science Foundation of Zhejiang Province (No. LQ15H310003).
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          Research Articles

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