中兽医医药杂志2025，Vol.44Issue(3)：47-54,8.DOI:10.13823/j.cnki.jtcvm.2025.020
胆汁酸肠肝循环转运体及其在血脂调节药物研发中的应用
Bile acid enterohepatic circulation transporter and its application in the development of hypolipidemic drug
摘要
Abstract
Hyperlipidemia is also a risk factor for fatty liver and cardiovascular diseases.Lipid deposition can aggravate the occurrence and development of fatty liver,induce atherosclerosis,and seriously endanger health.Hypercholesterolemia is a representative hyperlipidemia.Cholesterol can't be directly metabolized and excreted in the body.It needs to be metabolized into bile acids and then excreted with feces.The enterohepatic circulation(EHC)of bile acids is important to maintain the homeostasis of bile acid metabolism.One of the ideas for the development of lipid-lowering drugs is to reduce the cholesterol level by regulating bile acid metabolism.Activators/inhibitors for bile acids transporters and their regulatory factors can inhibit bile acids reabsorption and reduce liver bile acid load by affecting the activity or expression of bile acid transporters.The conversion of cholesterol to bile acids is increased by negative feedback,thereby,blood lipid levels is improved.The EHC of bile acids is mainly mediated by BSEP,NTCP,ASBT,IBABP,OSTα/β,and regulated such as FXR and intestinal flora.ASBT and NTCP are the two spotlight bile acid transporters and their inhibitors are mostly used in the prevention and treatment of blood lipid regulation.ASBT inhibitors have good potential for the development of hypolipidemic drugs.Moreover,it is of great significance for the improvement of blood lipids in special groups because it can reduce the reabsorption of intestinal bile acids and maintain intestinal lubrication.At present,a variety of hypolipidemic drugs with different targets have been applied to clinical practice and have shown good effects.However,there is still a lack of animal-specific hypolipidemic drugs in the field of domestic veterinary drugs.Therefore,the further discuss on the regulation mechanism of bile acids EHC transporters and exploring new lipid-lowering targets can provide more reference for the development of lipid-lowering drugs for animals.关键词
高脂血症/胆汁酸代谢/肠肝循环/转运体Key words
hyperlipidemia/bile acids metabolism/enterohepatic circulation/transporters分类
农业科技引用本文复制引用
范丽萍,陶琦,张治杰,葛闻博,杨亚军,李剑勇..胆汁酸肠肝循环转运体及其在血脂调节药物研发中的应用[J].中兽医医药杂志,2025,44(3):47-54,8.基金项目
国家自然科学基金面上项目(32373071) （32373071）
