摘要
小檗碱(berberine)属于季铵型异喹啉类生物碱,又称黄连素。临床上用于治疗由细菌感染引起的胃肠道疾病。近年来研究发现,小檗碱具有良好的抗肿瘤作用,但由于其脂溶性差,难以透过细胞膜,限制了其临床应用。在此基础上,一些研究者通过对其化学结构进行改造和修饰,研究其各种药理作用的构效关系,发现了一系列抗肿瘤活性得到增强的衍生物。笔者主要综述小檗碱及其衍生物在抗肿瘤作用及其机制方面的研究进展,为基于小檗碱结构设计开发抗肿瘤药的研究者提供参考。
Berberine belongs to the quaternary ammonium type isoquinoline alkaloid known as berberinum. In traditional Chinese medicine, it has long been used to treat infections of the gastrointestinal tract disease caused by bacteria. Recent studies found that ber- berine has a good anti-tumor effect, but it is difficult pass through the cell membrane due to its poor fat-soluble, which limit its clinical application. By modifing chemical structure, some researchers have investigated the relationship between activity effects and structures of berberine and its derivatives, and have found a series of anti-tumor activity enhanced berberine derivatives. In this review, the recent research progress of the anti-tumor effects and their mechanisms of berberine and its derivatives are focused, which may provide reference for the design and development of anticancer drugs based on the structure of berberine
出处
《中国药学杂志》
CAS
CSCD
北大核心
2017年第6期429-433,共5页
Chinese Pharmaceutical Journal
基金
国家自然科学基金资助项目(81273556
81673478)
