类降脂药
化学
非诺贝特
高脂血症
肝保护
甘油三酯
过氧化物酶体增殖物激活受体
药理学
受体
吉非罗齐
内科学
生物化学
内分泌学
胆固醇
酶
医学
谷胱甘肽
糖尿病
作者
Yundong Xie,Jiping Liu,Yongheng Shi,Bin Wang,Xiaoping Wang,Wei Wang,Meng Sun,Xinya Xu,Lifei Cheng,Shipeng He
标识
DOI:10.1016/j.bioorg.2021.105454
摘要
The bis-benzodioxole-fibrate hybrids were designed by structural simplification and bioisostere principle. Lipids lowering activity was preliminarily screened by Triton WR 1339 induced hyperlipidemia mice model, in which T3 showed the best hypolipidemia, decreasing plasma triglyceride (TG) and total cholesterol (TC), which were better than sesamin and fenofibrate (FF). T3 was also found to significantly reduce TG, TC and low density lipoprotein cholesterin (LDL-C) both in plasma and liver tissue of high fat diet (HFD) induced hyperlipidemic mice. In addition, T3 showed hepatoprotective activity, which the noteworthy amelioration in liver aminotransferases (AST and ALT) was evaluated and the histopathological observation exhibited that T3 inhibited lipids accumulation in the hepatic and alleviated liver damage. The expression of PPAR-α receptor involved lipids metabolism in liver tissue significantly increased after T3 supplementation. Other potent activity, such as antioxidation and anti-inflammation, was also observed. The molecular docking study revealed that T3 has good affinity activity toward to the active site of PPAR-α receptor. Based on these findings, T3 may serve as an effective hypolipidemic agent with hepatoprotection.
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