天然产物研究与开发 ›› 2016, Vol. 28 ›› Issue (6): 978-985.doi: 10.16333/j.1001-6880.2016.6.027

• 综述 • 上一篇    下一篇

白桦脂酸制备方法和药理活性研究进展

周亚敏,林丽美,夏伯候*   

  1. 湖南中医药大学湖南省中药不良成分快速检测及脱除工程技术研究中心中药有毒物质防控技术湖南省工程实验室,长沙 410208
  • 出版日期:2016-06-30 发布日期:2017-01-17

Review on Preparation Technology and Pharmacological Activity of Betulinic Acid

ZHOU Ya-min,LIN Li-mei,XIA Bo-hou*   

  1. Hunan University of Chinese Medicine,School of Pharmacy;Hunan Engineering Center for Rapid Test and Removal  of Toxic and Harmful Substances in Chinese Medicine;Hunan Engineering Laboratory for Prevention and Control Technology of Toxic Substances in Chinese Medicine,Changsha 410208,China
  • Online:2016-06-30 Published:2017-01-17

摘要: 天然产物已被用来防治人类疾病数千年,并在药物发现和发展中发挥越来越大的作用。白桦脂酸(betulinic acid,BA)又称白桦酸、桦木酸,是一种五环三萜酸,存在于多种植物中。近年来的研究表明,BA具有多种多样的生物活性,如抗肿瘤、抗病毒、抗炎、抗菌、抗疟疾等,尤其是在抗肿瘤和抗HIV方面,特别是针对黑色素肿瘤细胞具有专一的杀死作用,因此得到了广泛关注。更重要的是BA衍生物抗HIV Ⅱ期临床实验已经取得成功,所以BA目前已被认为是最具潜力的药物先导化合物之一。因此,本综述从BA的制备合成以及药理活性等方面对近年来的相关研究进行概括总结,以期为BA的研究和开发利用提供参考。

关键词: 白桦脂酸, 抗肿瘤, 制备, 药理活性

Abstract: Natural products have been used to combat human diseases for thousands of years and play an increasing role in drug discovery and development.Betulinic acid (BA) is a naturally pentacyclic triterpenoid which has demonstrated selective cytotoxicity against a number of specific tumor types,particularly melanoma tumor,and a variety of infectious agents such as HIV,bacteria and malaria.Many studies established a favorable safety margin for betulinic acid,as systemic side effects were not observed at any dose.More importantly,BA successfully passed anti-HIV phase II clinical trial recently,hence BA has been considered as one of the most promising drug lead compounds.This paper reviewed the research progress about the preparation technologies and pharmacological activities of BA in recent years,in order to provide reference for the research and development of BA.

Key words: betulinic acid, anticancer, preparation, pharmacological activity

中图分类号: 

R737.33