植物性原料合成熊去氧胆酸的研究进展  

Progress in the synthesis of ursodeoxycholic acid from plant-source materials

作　　者：陈旺 刘格歌[1] CHEN Wang;LIU Ge-ge(School of Biological Science and Engineering,Shaanxi University of Technology,Hanzhong 723000,China;Qinba State Key Laboratory of Biological Resources and Ecological Environment,ShaanxiUniversity of Technology,Hanzhong 723000,China)

机构地区：[1]陕西理工大学生物科学与工程学院,陕西汉中723000 [2]陕西理工大学秦巴生物资源与生态环境省部共建国家重点实验室(培育),陕西汉中723000

出　　处：《中国药物化学杂志》2023年第1期49-58,共10页Chinese Journal of Medicinal Chemistry

基　　金：陕西省科技厅项目(2022JM-576,2022SF-406)。

摘　　要：熊去氧胆酸可溶解胆固醇结石,改善胆汁淤积性疾病的肝功能,在临床上广泛用于治疗各种肝胆疾病。过去,熊去氧胆酸主要从活熊胆中引流胆汁进行提取,但该方法步骤繁杂且违反了动物保护法,来源受限,无法满足工业生产的需求。目前,熊去氧胆酸可通过胆酸、7-酮石胆酸、鹅去氧胆酸或猪去氧胆酸作为起始原料进行化学合成、微生物或酶法合成。然而以上原料都是从动物胆汁酸中提取分离而得,属于动物性原料,可能存在致病菌、病毒和过敏源等问题。植物性原料可避免动物原料的各种安全风险,且来源更为广泛、价格更为低廉。近几年由植物性原料合成熊去氧胆酸的研究成为甾体药物合成研究的热点之一。本文作者对这一领域的研究进展进行综述,以期为相关研究提供有价值的参考。Ursodeoxycholic acid was widely used in clinical treatment of hepatobiliary diseases.It was mainly extracted from the drainage bile of live bear bile.This method violated the animal protection law and has limited source.At present,ursodeoxycholic acid can be commonly produced by transformation of cholic acid,chenodeoxycholic acid or hyodeoxycholic acid.However,animal cholic acid raw materials could have the problem of pathogenic bacteria and virus infection.Plant-source materials can avoid various risks of animal materials,and have wider sources and lower prices.In recent years,the synthesis of ursodeoxycholic acid from plant-source materials had become one of the hot spots in the research of steroid drug synthesis.In this paper,the research progress in recent years was reviewed in order to provide guidance for the relevant researchers.

关 键 词：熊去氧胆酸 化学合成 豆甾醇 薯蓣皂苷元 雄烯二酮 去氢表雄酮 双降醇 

分 类 号：R914[医药卫生—药物化学]