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The metabolism and hepatotoxicity of ginkgolic acid (17 : 1) in vitro / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.) ; (6): 829-837, 2018.
Article in English | WPRIM | ID: wpr-812346
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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Full text: Available Index: WPRIM (Western Pacific) Main subject: Microsomes, Liver / Plant Extracts / Kinetics / Cells, Cultured / Chemistry / Salicylates / Glucuronosyltransferase / Rats, Sprague-Dawley / Cytochrome P-450 CYP1A2 / Ginkgo biloba Limits: Animals / Humans Language: English Journal: Chinese Journal of Natural Medicines (English Ed.) Year: 2018 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Microsomes, Liver / Plant Extracts / Kinetics / Cells, Cultured / Chemistry / Salicylates / Glucuronosyltransferase / Rats, Sprague-Dawley / Cytochrome P-450 CYP1A2 / Ginkgo biloba Limits: Animals / Humans Language: English Journal: Chinese Journal of Natural Medicines (English Ed.) Year: 2018 Type: Article