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作 者:李倩 于丹[1] 国立东[1] 都晓伟[1] LI Qian;YU Dan;GUO Li-dong;DU Xiao-wei(College of Pharmacy,Heilongjiang University of Chinese Medicine,Harbin 150040,China)
机构地区:[1]黑龙江中医药大学药学院,黑龙江哈尔滨150040
出 处:《中草药》2022年第22期7264-7278,共15页Chinese Traditional and Herbal Drugs
基 金:国家自然科学基金资助项目(81872967)。
摘 要:皂苷类化合物是天然药物中存在的一类重要化学成分,通过微生物技术可以将其转化为多种衍生物,常用的微生物主要为细菌和真菌,转化反应以水解脱去糖基为主,来提高转化产物的生物利用度和药理活性。此外,通过羟基化、糖基化、羰基化和酯化等反应,能够降低底物的不良反应,改善药物功效。甾体皂苷的微生物转化主要以皂苷与皂苷元之间的相互转化为主,是实现某些特殊皂苷类化合物规模化生产的有效途径。以人参皂苷、甘草次酸、黄芪皂苷、薯蓣皂苷、知母皂苷等为例,分析并阐述皂苷类化合物的微生物发酵转化机制,以期为皂苷类成分生物合成及新药研究开发提供参考。Saponins are a class of important chemical components in natural medicines. Microbial fermentation technology can convert saponins into various derivatives. The microorganisms that can transform saponins are mainly bacteria and fungi. The hydrolysis reaction is the main method, and the sugar group is removed, which can improve the bioavailability and pharmacological activity of the transformation product. In addition, through reactions such as hydroxylation, glycosylation, carbonylation, and esterification, the side effects of the substrate are reduced, and the drug efficacy is improved. The microbial transformation of steroidal saponins is mainly based on the mutual transformation between saponins and sapogenins, which is an effective way to realize the large-scale production of some special saponins. In this paper, ginsenoside, glycyrrhetinic acid, astragaloside, dioscin, timosaponin and other medicinal materials are used as examples to analyze the microbial transformation mechanism of saponins, in order to provide reference for the biosynthesis of saponins and the development of new drugs.
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