Abstract��OBJECTIVE To investigate the hepatic toxicity of 8 monomers in Polygonum multiflorum using a combination of UDP-glucuronic acid transferase 1A1(UGT1A1 enzyme). METHODS Bilirubin was used as the substrate for UGT1A1. Incubation method in RLM in vitro was adopted to test the apparent inhibition constants(Ki) of different components. Furthermore the structure-activity relationship between the 8 components and UGT1A1 was analyzed. RESULTS The inhibition effects on UGT1A1 enzyme of the 8 components were in the following sequence: emodin-8-O-glc��emodin��citreorosein��(+)-catechin��gallic acid��physcion��rhein��emodin-6-O-glc. Moreover, there was a structure-activity relationship, and it was presumed that the 6-position hydroxyl group is an active and necessary group. CONCLUSION The established method in vitro is stable and feasible. Experimental results shows that the enzyme inhibition has structural selectivity, which provides an experimental basis for predicting the enzyme inhibition activity of the analogues of components of Polygonum multiflorum.
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WANG Qi, DAI Zhong, WANG Ya-dan, MA Shuang-cheng. Hepatotoxicity of Eight Components of Radix Polygonum multiflorum Thunb. in Rat Liver Microsome System in Vitro. Chinese Pharmaceutical Journal, 2018, 53(8): 589-593.
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2018, Vol. 53 
