阿那曲唑
葡萄糖醛酸
谷胱甘肽
药理学
结合
芳香化酶抑制剂
芳香化酶
化学
医学
生物化学
乳腺癌
内科学
癌症
酶
多糖
数学分析
数学
作者
Siyu Ding,Siyu Liu,Yaxuan Chen,Ying Peng,Jiang Zheng
出处
期刊:Xenobiotica
[Informa]
日期:2022-04-03
卷期号:52 (4): 380-388
标识
DOI:10.1080/00498254.2022.2086503
摘要
Anastrozole (ANA), is an inhibitor of non-steroidal aromatase, widely employed for the treatment of breast cancer. However, ANA-associated liver injury cases have been documented in the application of the drug.The major purposes of the present study were to identify the structure of reactive metabolites derived from ANA and to study related metabolic pathways of ANA.We found ANA itself is an electrophilic species reactive to GSH. ANA can be metabolised to ANA-N+-glucuronide (1) catalysed by UGT1A4. An ANA GSH conjugate (2) was detected in bile and livers of rats treated with ANA. UGT1A4 participated in the phase II metabolic pathway.This work allowed us to better understand the mechanisms of the hepatotoxicity of ANA and provided new avenue to define the possible role of metabolic activation in hepatotoxicity.
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