白桦脂酸制备方法和药理活性研究进展

Review on Preparation Technology and Pharmacological Activity of Betulinic Acid

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HIVⅡ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。

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 pentacyclie triterpenoid which has demonstrated selective cytotoxicity against a number of specific tumor types, particularly melanoma tumor, and a variety of infectious a- gents such as HIV, bacteria and malaria. Many studies established a favorable safety margin for betulinic acid, as system- ic side effects were not observed at any dose. More importantly, BA successfully passed anti-I-IIV phase II clinical trial recently, hence BA has been considered as one of the most promising drug lead compounds. This paper reviewed the re- search progress about the preparation technologies and pharmacological activities of BA in recent years,in order to pro- vide reference for the research and development of BA.