青蒿素抗肿瘤衍生物的研究进展  

Advances in research of anti-tumor artemisinin derivatives

作　　者：梁津豪 皮荣标[2] 刘中秋 于思[1] 雷玉 何细新[1] LIANG Jin-hao;PI Rong-biao;LIU Zhong-qiu;YU Si;LEI Yu;HE Xi-xin(School of Pharmaceutical Sciences,Guangzhou University of Chinese Medicine,Guangzhou 510006,China;School of Pharmaceutical Sciences,Sun Yat-Sen University,Guangzhou 510006,China)

机构地区：[1]广州中医药大学中药学院,广州510006 [2]中山大学药学院,广州510006

出　　处：《中国新药杂志》2018年第23期2781-2787,共7页Chinese Journal of New Drugs

基　　金：广州市科技计划[穗科创字(2016)172号]

摘　　要：青蒿素是一种具有强大抗疟疾活性及广谱抗肿瘤活性的天然产物。随着肿瘤细胞多药耐药等问题的日益严峻,具有长期用药安全和多种抗肿瘤作用机制的青蒿素及其衍生物逐渐成为研究的热点。本文选择2014—2017年期刊报道的以青蒿素为母体的抗肿瘤衍生物,并以其设计策略分3类进行了综述:青蒿素与抗肿瘤分子或药效基团强强杂合、与一些具有提高其抗肿瘤活性的特殊分子的功能性结合、青蒿素单体的结构简化及聚合,并对其共同问题及发展方向进行了探讨。Artemisinin is a natural product with strong antimalarial activities and broad-spectrum anti-tumor activities.As problems of multidrug resistance in tumor cells increasing severely,artemisinin and its derivatives have gradually been attracted because of its long-term safety and diverse anti-tumor mechanisms.Some anti-tumor derivatives of artemisinin,published covering 2014--2017,have been selected.According to their design strategies,3issues were reviewed in this paper,namely combining an anti-tumor molecule (or its key pharmacophoric groups)to functional conjugation molecules,making structural simplification,and polymerization of artemisinin monomers.The common problems and future development of them were discussed at the end of this paper.

关 键 词：青蒿素 抗肿瘤 衍生物 设计策略 

分 类 号：R914[医药卫生—药物化学]