熊去氧胆酸：独特的性质和临床应用,Meditsinskiy sovet = Medical Council

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熊去氧胆酸：独特的性质和临床应用
Meditsinskiy sovet = Medical Council Pub Date : 2023-05-29 , DOI: 10.21518/ms2023-136
M. V. Maevskay ₁

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熊去氧胆酸 (UDCA) 是一种天然的亲水性胆汁酸，在人体中仅占胆汁酸总量的一小部分 (5%)。其独特的特性使其可作为多种肝脏疾病的一线治疗方法。UDCA能够减少胆固醇向胆汁的分泌，与胆固醇分子形成混合胶束（液晶）并与多功能核受体相互作用，被积极用于治疗和预防胆石症。UDCA具有刺激肝胆分泌的能力，促进胆管细胞分泌碳酸氢盐，这与原发性胆汁性胆管炎（PBC）和原发性硬化性胆管炎（PSC）患者有关。UDCA 激活转运蛋白，如胆汁酸输出泵 (BSEP)、多重耐药蛋白 2 (MRP2) – 结合转运蛋白、2 型阴离子交换器 (AE2)，并促进它们向细胞小管膜移动。UDCA 作为一种多效剂，在调节各种细胞类型凋亡的经典线粒体途径中发挥独特的作用。UDCA 的双分子键可作为自由基的陷阱，抑制脂质过氧化过程。UDCA 渗透到线粒体膜的能力导致抑制负责产生超氧阴离子的线粒体氧化酶的活性。UDCA激活自噬并促进肝细胞有毒脂肪酸的消除，减少肝脏脂肪变性，UDCA具有抗炎、抗纤维化、免疫调节和抗癌作用。UDCA被纳入国际和俄罗斯临床指南，用于治疗各种肝病（PBC、PSC、妊娠期肝内胆汁淤积、药物性胆汁淤积、具有胆汁淤积成分的酒精性肝病）、胆石症、囊性纤维化患者。在非酒精性脂肪肝的药物治疗中，UDCA是唯一对肝脏和心血管系统具有双向作用的药物。

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Ursodeoxycholic acid: unique properties and clinical applications

Ursodeoxycholic acid (UDCA) is a natural hydrophilic bile acid, which is present in humans as a small fraction of the total amount of bile acids (5%). Its unique properties underlie its use in a number of liver diseases as a first-line therapy. The ability of UDCA to reduce the secretion of cholesterol into bile, form mixed micelles (liquid crystals) with cholesterol molecules and interact with multifunctional nuclear receptors, are actively used in the treatment and prevention of cholelithiasis. UDCA has the ability to stimulate hepatobiliary secretion, promotes the secretion of bicarbonate by cholangiocytes, which is relevant for patients with primary biliary cholangitis (PBC) and primary sclerosing cholangitis (PSC). UDCA activates transporter proteins such as bile acid export pump (BSEP), multiresistance protein 2 (MRP2) – conjugates transporter, type 2 anion exchanger (AE2), and promotes their movement to the canalicular membrane of cells. UDCA acts as a pleiotropic agent that plays a unique role in modulating the classical mitochondrial pathway of apoptosis in various cell types. Double molecular bonds of UDCA serve as a trap for free radicals, which suppresses the processes of lipid peroxidation. The ability of UDCA to penetrate into mitochondrial membranes leads to suppression of the activity of mitochondrial oxidase enzymes responsible for the production of superoxide anion. UDCA activates autophagy and promotes the elimination of toxic fatty acids from hepatocytes, reducing liver steatosis, UDCA has anti-inflammatory, antifibrotic, immunomodulatory and anticarcinogenic effects. UDCA is included in international and Russian clinical guidelines for the treatment of patients with various liver diseases (PBC, PSC, intrahepatic cholestasis of pregnancy, drug-induced cholestasis, alcoholic liver disease with cholestatic component), cholelithiasis, cystic fibrosis. In the pharmacotherapy of non-alcoholic fatty liver disease, UDCA is the only drug that has a bi-directional effect on the liver and cardiovascular system.

更新日期：2023-05-29

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