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去氧熊去氧胆酸在胆汁淤积性和代谢性疾病中的潜力。

Potential of nor-Ursodeoxycholic Acid in Cholestatic and Metabolic Disorders.

作者信息

Trauner Michael, Halilbasic Emina, Claudel Thierry, Steinacher Daniel, Fuchs Claudia, Moustafa Tarek, Pollheimer Marion, Krones Elisabeth, Kienbacher Christian, Traussnigg Stefan, Kazemi-Shirazi Lili, Munda Petra, Hofer Harald, Fickert Peter, Paumgartner Gustav

机构信息

Division of Gastroenterology and Hepatology, Department of Internal Medicine III, Medical University of Vienna, Vienna, Austria.

出版信息

Dig Dis. 2015;33(3):433-9. doi: 10.1159/000371904. Epub 2015 May 27.

Abstract

24-nor-ursodeoxycholic acid (norUDCA) is a side-chain shortened derivate of ursodeoxycholic acid (UDCA). Since norUDCA is only ineffectively conjugated with glycine or taurine, it has specific physicochemical and therapeutic properties distinct from UDCA. Nonamidated norUDCA undergoes cholehepatic shunting enabling 'ductular targeting' and inducing a bicarbonate-rich hypercholeresis, with cholangioprotective effects. At the same time it has direct anti-inflammatory, antilipotoxic, anti fibrotic, and antiproliferative properties targeting various liver cell populations. norUDCA appears to be one of the most promising novel treatment approaches targeting the liver and the bile duct system at multifactorial and multicellular levels. This review article is a summary of a lecture given at the XXIII International Bile Acid Meeting (Falk Symposium 194) on 'Bile Acids as Signal Integrators and Metabolic Modulators' held in Freiburg, October 8-9, 2014, and summarizes the recent progress with norUDCA as a novel therapeutic approach in cholestatic and metabolic (liver) disorders.

摘要

24-去甲熊去氧胆酸(norUDCA)是熊去氧胆酸(UDCA)侧链缩短的衍生物。由于norUDCA与甘氨酸或牛磺酸的结合效果不佳,它具有与UDCA不同的特定物理化学性质和治疗特性。未酰胺化的norUDCA进行胆肝分流,实现“胆小管靶向”并诱导富含碳酸氢盐的胆汁分泌过多,具有胆管保护作用。同时,它对各种肝细胞群体具有直接的抗炎、抗脂毒性、抗纤维化和抗增殖特性。norUDCA似乎是在多因素和多细胞水平上针对肝脏和胆管系统的最有前途的新型治疗方法之一。这篇综述文章是2014年10月8日至9日在弗莱堡举行的第XXIII届国际胆汁酸会议(福克研讨会194)上关于“胆汁酸作为信号整合剂和代谢调节剂”的讲座总结,并总结了norUDCA作为胆汁淤积性和代谢性(肝脏)疾病新型治疗方法的最新进展。

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