天然产物皂苷类化合物生物转化的研究进展

皂苷是苷元为三萜或螺甾烷类的一类较复杂的糖苷类化合物。天然来源皂苷为底物,采用生物转化技术获取了大量结构新颖的化合物,尤其是具有良好活性的皂苷转化产物,为新药的研究与开发提供了极为有价值的先导化合物。皂苷按母核结构可分为三萜皂苷和甾体皂苷,目前文献报道了89个天然来源皂苷单体的生物转化研究,其中三萜皂苷56个,甾体皂苷33个。皂苷类化合物的生物转化方法包括酶催化、微生物和肠道菌群转化,皂苷的生物酶和微生物转化工艺的研究与优化,是目前规模化制备活性次级皂苷的主要途径。皂苷类化合物的生物转化反应主要包括水解、氧化还原和重排等反应,最终生成苷元、次级糖苷或其衍生物。大多数皂苷的生物转化途径主要是经糖链水解反应,生成多个含糖基较少的次级皂苷,吸收入血并达到靶器官,发挥治疗作用。稀有次级皂苷制备、先导化合物发现和新药开发是皂苷类化合物生物转化研究的主要方向。利用微生物和肠道菌群转化技术研究皂苷的体内代谢与作用机制,也将成为该类成分生物转化研究中的热点。结合国内外近30年来的研究成果,对皂苷类成分的生物转化技术、转化反应类型和转化途径的研究进展进行总结,以期为皂苷类成分生物转化的深入研究和开发利用提供科学依据。

Biotransformation of Natural Saponins

Saponin is a kind of complex compounds with triterpenoid or spiral aglycones.Natural saponins are used as substrates,and many novel compounds are obtained by biotransformation technology. Especially, converted products of saponins with strong activities provide valuable lead compounds for the research and development of new drugs. Saponins can be divided into triterpenoid saponin and steroidal saponin according to the structure of the mother nucleus. There are about 89 reported saponin components,including 56 triterpenoid saponins and 33 steroidal saponins. Biological enzyme catalysis,microbial transformation and intestinal microflora transformation are the main bioconversion technologies and key development directions of saponins. The research and optimization technology of biological enzyme and microbial transformation of saponins are the effective methods to prepare active secondary saponins. The biotransformation reaction of saponins mainly includes hydrolysis,redox and rearrangement,resulting in the formation of aglycones,secondary glycosides and their derivatives. The hydrolysis of saponin sugar chains was the main biological transformation pathway, and could generate a number of secondary saponins with less glycosyl groups. The secondary saponins could be absorbed into blood and become real active ingredients in body. Preparation of rare secondary saponins,discovery of lead compounds and development of new drugs are the main directions of biotransformation of saponins. The studies on the metabolism and mechanism of natural saponins by microbial and intestinal microbial biotransformation will also become hotspots. According to relevant papers at home and abroad,the researches on transformation technique,transformation approach and transformation reaction of saponins from natural products in the past thirty years were summarized, and the prospects of research and development were also analyzed to provide scientific basis for further study and comprehensive utilization of these conversion products.