ABSTRACT
Glucuronidation is one of the most important metabolic reactions in vivo, while O-glucuronidation is the major reaction type. The synthesis of O-glucuronides is very helpful for the further studies on the evaluation of biological activity and safety of O-glucuronids, as well as drug metabolism and pharmacokinetic studies. The enzymatic catalysis process using UDP-glucuronosyltransferases (UGTs) is the major method for O-glucuronides biosynthesis. This review summarized the recent progress in enzymatic preparation of O-glucuronides by using different enzyme sources including plants, microorganisms, animals, and recombinant human UGTs. Furthermore, this review also summarized several new techniques to improve the efficacy for biosynthesis of O-glucuronides.