五环三萜类化合物微生物转化研究进展

Advances in microbial transformation of pentacyclic triterpenes

五环三萜类化合物是自然界中含量较多、分布较广的一类重要天然有机化合物,具有抗肿瘤、抗糖尿病、抗病毒、抗氧化、抗菌等多种生物活性。通过微生物转化技术对其进行结构改造和修饰,为生物活性筛选提供更多结构新颖的先导化合物,进而为研发出生物活性更强的五环三萜类新药奠定基础。本文对五环三萜类化合物的3种结构类型(齐墩果烷型、乌苏烷型和羽扇豆烷型)中最具代表的5个化合物,即齐墩果酸、甘草酸、甘草次酸、熊果酸和白桦脂酸在近10年微生物转化研究成果上进行综述,为天然产物生物转化研究和新药开发提供参考。

Pentacyclic triterpenoids are an important class of natural organic compounds that are abundant and widely distributed in nature,with a variety of biological activities such as anti-tumour,anti-diabetic,anti-viral,anti-oxidant and anti-bacterial.Structural modification of pentacyclic triterpenoids by biotransformation technology can provide more lead compounds with novel structures for bioactivity screening,and thus lay the foundation for the development of new pentacyclic triterpenoids with greater bioactivity.In this paper,the five most representative compounds of the three structural types of pentacyclic triterpenoids(oleanolane-type,ursane-type and lupinane-type),namely oleanolic acid,glycyrrhetinic acid,glycyrrhizic acid,ursolic acid and betulinic acid,are reviewed in the last 10 years of biotransformation research results to provide reference for natural product biotransformation research and new drug development.