Identification of human UDP-glucuronosyltransferases involved in I3,II8-biapigenin glucuronidation in Vitro.

I3,II8-biapigenin is a biflavonoid compound with diverse pharmacological effects. The present study aimed to investigate the glucuronidation of I3,II8-biapigenin in the human liver microsomes (HLMs) and recombinant human UDP-glucuronosyltransferases (UGTs). Three glucuronidation metabolites of I3,II8-biapigenin were detected in HLMs. Both recombinant human UGTs and chemical inhibitors studies demonstrated that UGT1A1, UGT1A3, UGT1A9 and UGT1A10 were involved in the glucuronidation of I3,II8-biapigenin. The present investigation provided information for the drug-drug interaction potentials of I3,II8-biapigenin when co-administrated with UGTs inhibitors or inducers.