熊去氧胆酸的合成研究进展

Research Progress on Synthesis of Ursodeoxycholic Acid

熊去氧胆酸(UDCA)是一种多功能亲水性胆汁酸,是治疗胆汁淤积性肝病的重要药物之一。以胆酸(CA)、猪去氧胆酸(HDCA)、鹅去氧胆酸(CDCA)等为起始原料的化学合成法已广泛应用于工业化生产;生物合成主要以CDCA或CA为底物,经氧化还原脱氢酶异构化得到UDCA,工艺绿色、环保、高效,是该类药物合成研究的主要方向。本文对UDCA的化学、生物合成方法进行了综述,分析并展望了现有技术的优势及发展方向。

Ursodeoxycholic acid(UDCA)is a multifunctional hydrophilic bile acid,which can protect bile duct cells from damage by improving the secretion of bile acid.It is one of the essential drugs for the treatment of cholestatic liver disease.At present,the synthesis of UDCA includes two pathways:chemical synthesis and biosynthesis.Cholic acid(CA),Hyodeoxycholic acid(HDCA),and Chenodeoxycholic acid(CDCA)were frequently selected as the starting materials for chemical synthesis.Chemical synthesis technology is more mature,which is mostly used in industrial production at present.Biosynthesis is mainly based on CDCA or CA as substrate and UDCA is obtained by redox dehydrogenase isomerization.This method is green,environmentally friendly and efficient,and it is the main research direction of this kind of drug synthesis at present.In this paper,recent developments of the chemical and biological synthesis strategies of UDCA were reviewed,and the advantages and development directions of the existing preparation technologies were discussed.