[Research progress on in vitro effects of traditional Chinese medicine ingredients on liver UDP-glucuronosyltransferases]

Abstract

UDP-glucuronosyltransferases(UGTs) are the main phase Ⅱ metabolizing enzymes in the human body, participating in the glucuronidation of various chemicals in the body. Traditional Chinese medicine(TCM) ingredients affect the activities of UGTs involved in drug metabolism, and the fluctuations in the blood concentrations of drugs metabolized by UGTs will lead to the risk of TCM-TCM or TCM-chemical drug interaction, which will cause drug safety problems and affect drug efficacy. Therefore, it is essential to explore the effect of TCM ingredients on the activities of UGTs. The recombinant human UGTs method and liver microsomal incubation method are reliable and effective, and they are thus often used to study the effects of TCM ingredients on UGTs in the liver. Studies have reported that different TCM ingredients can induce or inhibit the activities of UGTs, while the systematical review remains to be carried out. This paper reviews the effects of different ingredients and extracts of TCM and Chinese patent medicines on recombinant human UGTs or liver microsomal UGTs, aiming to provide reference for the rational and safe use of TCM in clinical practice. From the perspective of drug-drug interaction mediated by UGTs, the exacting classical drug pairs and incompatibility principles of traditional Chinese medicine were clarified, which laid the foundation for exploring new drug compatibility.

Keywords: UDP-glucuronosyltransferases(UGTs); liver microsome; recombinant human UGTs; traditional Chinese medicine.