Study on potential hepatotoxicity of rhein in Rhei Radix et Rhizoma based on liver metabolism / 中国中药杂志
China Journal of Chinese Materia Medica
;
(24): 412-417, 2020.
Article
in Chinese
| WPRIM
| ID: wpr-1008352
ABSTRACT
The bilirubin metabolism mediated by the phase Ⅱ metabolizing enzyme UGT1A1 in the liver was evaluated to study the potential hepatotoxicity risk based on investigation on the inhibitory effect of rhein and its metabolites on the UGT1A1 enzyme in Rhei Radix et Rhizoma. Firstly, in vitro liver microsomes incubation was used to initiate the phase Ⅱ metabolic reaction to investigate the inhibitory effect of rheinon UGT1A1 enzyme. Secondly, the phase Ⅰ and phase Ⅱ metabolic reactions were initiated to investigate the hepatotoxicity risk of rhein metabolites. It was found that the rhein and its phase Ⅱ metabolites had no significant inhibitory effect on UGT1A1 enzyme, but its phase Ⅰ metabolites significantly reduced UGT1A1 enzyme activity. Based on the metabolites analysis, it is speculated that the rhein phase Ⅰ metabolite rheinhydroxylate and its tautomers have certain hepatotoxicity risks, while the toxicity risk induced by the prototype and phase Ⅱ metabolites of rheinglucoside, rheinglucuronic acid and rhein sulfate is small.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Microsomes, Liver
/
Drugs, Chinese Herbal
/
Anthraquinones
/
Glucuronosyltransferase
/
Rhizome
/
Chemical and Drug Induced Liver Injury
/
Liver
Limits:
Humans
Language:
Chinese
Journal:
China Journal of Chinese Materia Medica
Year:
2020
Type:
Article
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