丹参酮ⅡA及其类似物的全合成和结构修饰研究进展  

Advances in Research on Total Synthesis and Structural Modification of Tanshinone IIA and Its Analogues

作　　者：许昌胜[1] 陈莉[1] 

机构地区：[1]中国药科大学天然药物化学教研室,江苏南京210009

出　　处：《药学进展》2013年第2期58-65,共8页Progress in Pharmaceutical Sciences

摘　　要：丹参酮ⅡA具有抗肿瘤、抗炎抑菌及抗心血管疾病等广泛药理活性,但该化合物同时存在脂溶性高、半衰期短和生物利用度低等缺点,使其临床应用受到限制。因此研究人员不断尝试对丹参酮ⅡA进行结构改造,以期改善其理化性质和药动学参数。综述丹参酮ⅡA及其类似物的全合成和结构修饰的研究进展。TanshinoneⅡA shows a wide range of obvious pharmacological activities, such as antitu- mor, antibacterial, anti-inflammatory and anti-cardiovascular disease. However, its clinical use is limited because of the high lipid solubility, short half-life and low bioavailability. Therefore, the researchers have continuously attempted to make structural modification with tanshinone ⅡA, so as to achieve novel tanshi- none ⅡA analogues which have good physicochemical properties and pharmacokinetic parameters. The progresses in research on the total synthesis and structural modification of tanshinone ⅡA and its analogues were reviewed in this paper.

关 键 词：丹参酮ⅡA 全合成 结构改造 药理活性 新药开发 

分 类 号：R284[医药卫生—中药学]