生物转化对天然药物进行结构修饰的研究进展

摘要

Biotransformation in structural modification of natural drugs is one of the effective ways for screening active compounds. According to the diversity and specificity of enzymes in biological systems and the selectivity and specificity characteristics of biotransformation with fewer by-products, this paper provide a systematic review on the common bio-transformation methods in structural modification of natural medicine in recent years, such as hydroxylation, glycosyla-tion, hydrolysis and epoxidation reactions, etc. Meanwhile, it also provides a review on the practical application of bio-transformalion in the development of new drugs and the change of activity of natural substances, such as changing the cytotoxic activity and enhancing anti-drug resistance, reducing toxicity or increasing bioavailability, etc.%利用生物转化对天然药物进行结构修饰,是筛选活性化合物的有效途径之一.本文根据生物体系中酶的多样性和特异性以及生物转化具有副产物少、选择性和专一性强等特点,系统性的综述了近几年来在天然药物资源开发利用研究中生物转化进行结构修饰的常见反应类型:羟基化、糖基化、水解和环氧化反应等,并简述了生物转化法在开发具有活性的新药物和改变天然药物活性如改变细胞毒性、增强抗耐药性、减小毒副作用或提高生物利用率等方面的实际应用.