基于糖基化修饰的铂类抗肿瘤化合物研究进展  

Progress in Study of Platinum Antitumor Compounds Modified by Glycosylation

作　　者：张强 李绍青 刘薇 邵佳[2] 田金磊 魏金霞 ZHANG Qiang;LI Shao-qing;LIU Wei;SHAO Jia;TIAN Jin-lei;WEI Jin-xia(College of Chemistry,Nankai University,Tianjin 300071,China;Department of Pharmacy,Tianjin First Central Hospital,Tianjin 300192,China;Department of Military Pharmacy,Tianjin University of Traditional Chinese Medicine,Tianjin 301617,China)

机构地区：[1]南开大学化学学院,天津300071 [2]天津市第一中心医院药学部,天津300192 [3]天津中医药大学中药学院,天津301617

出　　处：《中国药学杂志》2020年第17期1409-1414,共6页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金项目资助(81803356,81703690);天津市自然科学基金项目资助(19JCQNJC12200);天津市第一中心医院科技基金资助(院CM201806)。

摘　　要：铂类药物是众多恶性肿瘤的关键治疗药物之一,然而传统铂类药物对肿瘤细胞靶向性差,存在明显的毒副作用,因而亟须提升铂类药物靶向性来增加其抗肿瘤活性。糖及其衍生物是机体细胞间传递信息不可或缺的基础物质,肿瘤细胞通过Warburg效应可对含有特定糖分子结构的药物分子产生特异性识别并有效吸收,通过对传统铂类药物进行糖基功能化修饰可有效提升其对肿瘤细胞的选择性。此外,通过合理的糖基化修饰,还可明显提升铂类药物的靶向性和水溶性,并有效降低其毒性,因此,对铂类化合物进行糖基化修饰是铂类药物研究领域的热点之一。基于此,笔者综述了近年来糖基化铂类化合物在抗肿瘤领域的研究进展。Platinum drugs are one of the key therapeutic drugs for many malignant tumors,but traditional platinum drugs have poor tumor targeting effect and obvious side effects,so it is necessary to improve the targeting of platinum drugs for increasing their antitumor activity.Sugars and their derivatives are indispensable substances for the transmission of information between cells.Tumor cells can specifically recognize,and effectively absorb drug molecules containing specific sugar through Warburg effect.The selectivity of traditional platinum drugs to tumor cells can be effectively improved by functional glycosylation.In addition,with reasonable glycosylation,there is significant improvement in the targeting effect and water solubility of platinum drugs,with low collateral effects.Therefore,the design of glycosyl platinum compounds is one of the hotspots in the field of anticancer platinum drugs.Based on the above background,the research progress in glycosylated platinum compounds in the field of antitumor treatment is reviewed.

关 键 词：糖基化 铂类化合物 抗肿瘤活性 

分 类 号：R914.5[医药卫生—药物化学]