Establishment of rat liver microsome-hydrogel system for in vitro phase II metabolism and its application to study pharmacological effects of UGT substrates

Studies on the efficacy evaluation of UDP-glucuronosyltransferases (UGTs) substrates often ignore the existence of active metabolites. However, the present study aims to establish an in-vitro Phase II metabolism system to predict their pharmacological effects after metabolism. Rat liver microsomes (RLMs) encapsulated in a F127′-Acr-Bis (FAB) hydrogel were placed in the incubation system. Baicalein (BA) was chosen as a model drug and the metabolic activity was investigated by quantitating the metabolite Baicalin (BG). The 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay was used to measure the cell viability in Traditional cell culture system (TCCS) and Microsome-hydrogel added to cell culture system for Phase II metabolism (MHCCS-II). Finally, MHCCS-II was applied to predict the metabolic effects of Oroxylin A (OA) and Wogonin (W). Compared to TCCS group, for HepG2 and MCF-7 cells, BA in MHCCS-II led to lower survival ratios of cells (P