Synthesis and biological evaluation of novel schisanhenol derivatives as potential hepatoprotective agents
Synthesis and biological evaluation of novel schisanhenol derivatives as potential hepatoprotective agents
复制标题
作为潜在保肝剂的新型五味子酚衍生物的合成和生物学评价。
DOI：
10.1016/j.ejmech.2021.113919
复制
发表时间：
2021-10-21
影响因子：
6.7
通讯作者：
Mu, Shuzhen
中科院分区：
文献类型：
--
作者：
Deng, Lulu;Cheng, Shasha;Mu, Shuzhen
合成了21种新的五味子酚衍生物，并采用MTT法评价了它们对刀豆蛋白A （cona）所致肝损伤的保护作用。数据表明，在相同条件下，大多数衍生物的保护活性与阳性对照（二甲基二羧酸联苯，DDB）相当或更好。其中，化合物1b对Con a诱导的免疫损伤的保护作用最强。体外机制研究表明，1b通过IL-6/JAK2/STAT3信号通路抑制Con A治疗引起的细胞凋亡和炎症反应。与此一致的是，它在Con a诱导的免疫性肝损伤小鼠中也表现出显著的肝保护活性。这些结果清楚地表明，1b可能是一种靶向IL-6/STAT3信号通路的高效肝保护剂。(C) 2021 ElsevierMasson SAS。版权所有。
Twenty-one new schisanhenol derivatives were synthesized, and their hepatoprotective effects against liver injury induced by concanavalin A (Con A) were evaluated in vitro using an MTT assay. The data indicated that most derivatives exhibited equivalent or better protective activity than the positive control (dimethyl dicarboxylate biphenyl, DDB) under the same conditions. Among them, compound 1b showed the most potent hepatoprotective activity against Con A-induced immunological injury. Mechanistic studies in vitro revealed that 1b inhibited cell apoptosis and inflammatory responses caused by Con A treatment via IL-6/JAK2/STAT3 signaling pathway. Consistently, it also exhibited significant hepatoprotective activity in mice with Con A-induced immunological liver injury. These results clearly indicated that 1b might be a highly potent hepatoprotective agent targeting IL-6/STAT3 signaling pathway. (C) 2021 ElsevierMasson SAS. All rights reserved.