抗癌抗生素格尔德霉素衍生物17AAG的研究进展  

Advances on Anticancer Antibiotic Geldanamycin Derivative 17AAG

作　　者：易凤炎 周长林[1] 顾觉奋[1] 

机构地区：[1]中国药科大学生命科学与技术学院,江苏南京210009 [2]南通秋之友生物科技有限公司,江苏南通226200

出　　处：《药学进展》2015年第8期598-602,共5页Progress in Pharmaceutical Sciences

摘　　要：格尔德霉素是一种苯醌安莎霉素类抗生素,有极强的抗肿瘤活性,其衍生物17AAG(17-丙烯胺-17-去甲氧基格尔德霉素)是格尔德霉素的17位甲氧基被烯丙胺基取代所得,与格尔德霉素相比,其毒性更低,抗癌活性更高。综述17AAG的作用机制、治疗应用、药代动力学、毒性等研究进展。Geldanamycin is a benzoquinone ansamycin antibiotic with strong anti-tumor activity. Its derivative 17AAG（17-allylamino-17-demethoxy-geldanamycin） is obtained by substituting allylamine for geldanamycin＇s 17-methoxy, which has shown lower toxicity and higher antitumor activity, compared with geldanamycin.The advances on the mechanism of action, therapeutic use, pharmacokinetics and toxicity of 17 AAG were reviewed.

关 键 词：17AAG 抗癌抗生素 作用机制 治疗应用 药代动力学 毒性 

分 类 号：R96[医药卫生—药理学]