天然产物研究与开发 ›› 2012, Vol. 23 ›› Issue (6): 843-.doi: A

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生物转化对天然药物进行结构修饰的研究进展

贺赐安1,余旭亚1*,孟庆雄1,王亚明2   

  1. 1昆明理工大学生命科学与技术学院,昆明 650224;2昆明理工大学化工学院,昆明 650224
  • 收稿日期:2010-08-05 出版日期:2012-07-04 发布日期:2012-07-06
  • 基金资助:

    国家自然科学基金项目(6392-20070009)

Research in Structural Modification of Biotransformation of Natural Drugs

HE Ci-an1, YU Xu-ya1*, MENG Qing-xiong1, WANG Ya-ming2   

  1. 1College of Life Science and Technology, Kunming University of Science and Technology; 2College of Chemical Engineering, Kunming University of Science and Technology, Kunming 650224, China
  • Received:2010-08-05 Online:2012-07-04 Published:2012-07-06

摘要: 利用生物转化对天然药物进行结构修饰,是筛选新的天然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新活性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。

关键词: 生物转化, 结构修饰, 天然药物, 生物活性

Abstract: The use of biological transformation of structural modification of natural drugs is one of the effective ways for screening new natural active compounds. According to the diversity and specificity of enzymes in biological systems and biotransformation with fewer by-products, strong selectivity and specificity characteristics, this paper is the systematic overview of the common way of structural modification of biological transformation researched in the development and utilization of natural medicine resources in recent years, such as hydroxylation, glycosylation, hydrolysis and epoxidation reactions, etc. It outlines the practical application of biological transformation in the development of new drugs and changes of the activity of natural substances, such as changing the cytotoxic activity and enhancing anti-drug resistance, reducing toxicity or increasing bioavailability, etc.

Key words: biological transformation, structural modification, natural drugs, bioactivity

中图分类号: 

Q819