ursolic酸通过竞争性结合与谷胱甘肽S-转移酶的底物结合位点来减轻四坦型诱导的肝毒性。
抽象来源:
phytomedicine。 2022年9月; 104:154325。 EPUB 2022 7月6日。PMID: 35820303“> 35820303”> 35820303 Xiaoyao MA,Jiamin Peng,Xiaoying Wang,Min Jiang,Gang Bai
文章隶属关系:simeng chu
摘要:
背景:背景: tetrandrine(tetandrine a al bisbisbiat) Tetrandra S. Moore是中国唯一批准的硅化药物。但是,TET引起的肝毒性引起了安全问题。 TET诱导的潜在有毒靶标和机制尚不清楚。没有针对TET诱导的肝毒性开发的靶向解毒策略。 Ursolic Acid(UA),PentacyClic triterpene with liver protective effects, may have detoxification effects on TET-induced hepatotoxicity.
PURPOSE: This study aims to explore toxic targets and mechanism of TET and present UA as a potential targeted therapy for alleviating TET-induced肝毒性。
方法: 建立了TET诱导的肝伤害模型,以评估TET毒性和潜在的UA解毒效应。烷基修饰的TET和UA探针设计以识别潜在的肝靶标。 Pharmacological and molecular biology methods were used to explore the underlying toxicity/detoxification mechanism.
RESULTS: TET induced liver injury by covalently binding to the substrate-binding pocket (H-site) of glutathione S-transferases (GSTs) and inhibiting GST 活动。共价结合导致有毒代谢物积累D引起氧化还原失衡和肝损伤。 UA通过竞争性结合与GST H-site(
结论: