强心苷抗肿瘤制剂的研究进展  

Advances in research on antitumor preparations of cardiac glycoside

作　　者：高丽娜 乔宏志[1] 胡立宏 GAO Li-na;QIAO Hong-zhi;HU Li-hong(Jiangsu Key Laboratory for Functional Substance of Chinese Medicine,School of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210023,China)

机构地区：[1]南京中医药大学药学院,江苏省中药功效物质重点实验室,江苏南京210023

出　　处：《药学学报》2020年第7期1528-1539,共12页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(81503259);江苏省自然科学基金资助项目(BK20151002);中国科协青年人才托举工程项目(2017QNRC001);中央本级重大增减支项目(2060302);江苏省六大人才高峰项目(SWYY-057);江苏省333工程;青蓝工程项目。

摘　　要：强心苷是一类对心脏具有显著生理活性的甾体苷类化合物,曾有多个品种获批用于治疗心力衰竭和心房颤动。近年来的研究发现,强心苷可明显抑制肿瘤细胞增殖,并对人源肿瘤表现出一定的选择性。但普遍存在的水溶性差、毒副作用大等问题限制了其在抗肿瘤领域的转化应用。通过现代制剂技术和治疗方案,改变药物的体内动力学与组织分布,降低强心苷用量和毒副作用,是解决强心苷成药性问题的有效策略。本文就强心苷在抗肿瘤方面的发展历程和作用机制进行归纳,重点对其近年来新型制剂领域的研发进展进行综述,并对未来的研究方向进行展望。Cardiac glycoside is a class of steroidal glycosides with significant physiological activities to the heart.Several drugs had been approved for the treatment of heart failure and atrial fibrillation.In recent studies,the researchers have found that cardiac glycoside can selectively inhibit the proliferation of human tumor cells and has potent antitumor efficacy.Unfortunately,the poor solubility and severe adverse effects of cardiac glycoside hindered further clinical application in the field of anticancer.It is an effective strategy to solve the"drug-like"problem of cardiac glycoside by changing the pharmacokinetics and distribution in vivo and reducing the dosage and side effects by virtue of modern preparations technology and treatment scheme.In this review,a brief introduction of the developmental course and mechanism of cardiac glycosides in anticancer field was made,and recent research progress of cardiac glycosides preparations were summarized and discussed.Finally,the further research direction was prospected.

关 键 词：强心苷 抗肿瘤 作用机制 药物制剂 纳米技术 毒性 

分 类 号：R943[医药卫生—药剂学]