Liu Meijing, Liu Changhui, Chen Hao, Huang Xiaotao, Zeng Xiaohui, Zhou Juncheng, Mi Suiqing
Institute of Clinical Pharmacology, Guangzhou University of Chinese Medicine, Jichang Road 12, Guangzhou 510405, Guangdong Province, PR China.
College of food and drug, Anhui Science and Technology of University, Fengyang 233100, Anhui Province, PR China.
Eur J Pharmacol. 2017 Nov 15;815:1-9. doi: 10.1016/j.ejphar.2017.10.003. Epub 2017 Oct 7.
Schaftoside (SS) is a bioactive compound present in the Herba Desmodii Styracifolii (DS), a herb that has been used to treat cholelithiasis and urolithiasis in Chinese medicine. Whether SS inhibits cholesterol (Ch) gallstone formation has not been investigated. This study examined the effects of oral intake of SS on Ch gallstone formation in C57BL/6 mice fed a lithogenic diet. The rate of gallstone formation was recorded. Levels of Ch, triglycerides (TG) and bile salts (BS) were measured in the bile and serum. Liver histopathology was examined microscopically, and mRNA expression levels of key genes involved in cholesterol and bile metabolism were determined by qPCR. Mice fed SS were protected against gallstone formation, had increased biliary levels of BS, and reduced biliary Ch levels, resulting in a lower Ch saturation index (CSI). In addition, mice fed SS had lower serum TG and Ch levels, increased mRNA expression of liver X receptor α, ATP binding cassette transporter 5/8 (ABCG5/8), and ileal bile acid binding protein (IBABP) in the ileum, and of farnesoid X receptor and bile salt export protein (BSEP) in the liver and ileum. SS also protected against histologically determined liver damage. Overall, these data indicate that SS protects against Ch gallstone formation in mice, and that the effect is mediated by activation of ileal liver X receptor α and hepatic farnesoid X receptor.
夏佛托苷（SS）是广金钱草（DS）中存在的一种生物活性化合物，广金钱草是一种在中医中用于治疗胆结石和尿路结石的草药。SS是否抑制胆固醇（Ch）胆结石形成尚未得到研究。本研究考察了口服SS对喂食致石性饮食的C57BL/6小鼠Ch胆结石形成的影响。记录胆结石形成率。测定胆汁和血清中Ch、甘油三酯（TG）和胆汁盐（BS）的水平。显微镜检查肝脏组织病理学，并通过qPCR测定参与胆固醇和胆汁代谢的关键基因的mRNA表达水平。喂食SS的小鼠可预防胆结石形成，胆汁中BS水平升高，胆汁Ch水平降低，导致Ch饱和指数（CSI）降低。此外，喂食SS的小鼠血清TG和Ch水平较低，回肠中肝脏X受体α、ATP结合盒转运体5/8（ABCG5/8）和回肠胆汁酸结合蛋白（IBABP）的mRNA表达增加，肝脏和回肠中法尼醇X受体和胆汁盐输出蛋白（BSEP）的mRNA表达增加。SS还可预防组织学确定的肝脏损伤。总体而言，这些数据表明SS可预防小鼠Ch胆结石形成，且该作用是通过激活回肠肝脏X受体α和肝脏法尼醇X受体介导的。
