There is no author summary for this article yet. Authors can add summaries to their articles on ScienceOpen to make them more accessible to a non-specialist audience.
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.
Author and article information
Journal
Title:
Chinese Journal of Natural Medicines
Abbreviated Title:
Chinese Journal of Natural Medicines