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Study on hepatotoxicity of physcion based on liver metabolism in vitro / 中国中药杂志
China Journal of Chinese Materia Medica ; (24): 2367-2372, 2019.
Article in Chinese | WPRIM | ID: wpr-773085
ABSTRACT
To evaluate the hepatotoxicity risks of physcion on the basis of the bilirubin metabolism mediated by glucuronidation of UDP-glucuronosyltransferases 1A1(UGT1A1 enzyme). The monomers were added into the rat liver microsomes to test the hepatotoxicity by using bilirubin as UGT1A1 enzyme substrate, with apparent inhibition constant K_i as the evaluation index. Liver microsome incubation in vitro was adopted to initiate phase Ⅱ metabolic reaction and investigate the inhibitory effect of physcion. Then the phase Ⅰ and Ⅱ metabolic reactions were initiated to investigate the comprehensive inhibition of metabolites and prototype components. The results showed that when only the phase Ⅱ reaction was initiated, physcion directly acted on the UGT1A1 enzyme in a prototype form, exhibited weak inhibition and the inhibition type was mixed inhibition; When the phase Ⅰ and Ⅱ reactions were initiated simultaneously, the inhibitory effects of physcion on UGT1A1 enzyme became strong and the inhibition type was mixed inhibition, suggesting that physcion had phase Ⅰ and Ⅱ metabolic processes, and the metabolites had strong inhibitory effect on UGT1A1 enzyme. This experiment preliminarily proved that the metabolites of physcion may be the main components to induce hepatotoxicity.
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Full text: Available Index: WPRIM (Western Pacific) Main subject: Microsomes, Liver / Kinetics / Emodin / Glucuronosyltransferase / Toxicity / Chemical and Drug Induced Liver Injury / Metabolism Limits: Animals Language: Chinese Journal: China Journal of Chinese Materia Medica Year: 2019 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Main subject: Microsomes, Liver / Kinetics / Emodin / Glucuronosyltransferase / Toxicity / Chemical and Drug Induced Liver Injury / Metabolism Limits: Animals Language: Chinese Journal: China Journal of Chinese Materia Medica Year: 2019 Type: Article