烯二炔类抗肿瘤抗生素力达霉素的作用机制研究进展  

Study on mechanisms of action of enediyne antitumor antibiotic lidamycin

作　　者：高瑞娟[1] 李电东[1] 甄永苏[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2006年第13期1039-1043,共5页Chinese Journal of New Drugs

基　　金：国家高技术研究发展计划(863计划)课题(2002AA2Z3107);国家重点基础研究发展规划项目(G2000057010);国家自然科学基金(30472042;30300424)

摘　　要：力达霉素(lidamycin,LDM)是一种用精原细胞法筛选得到的链霉菌Streptomyces globisporus C-1027代谢产物中分离获得的九元环烯二炔类抗肿瘤抗生素。LDM对体外试验培养癌细胞有极强的细胞毒作用,体内试验中对移植瘤疗效显著。现主要从断裂DNA、诱导细胞凋亡和裂亡、致细胞产生衰老样表型、抑制血管生成和改变肿瘤侵袭调节基因表达等方面阐述LDM强烈抗肿瘤作用的分子机制。Lidamycin （LDM）, one of nine-ring enediyne antitumor antibiotics, was isolated by spermatogonial assay from the metabolic products of Streptomyces globisporus C-1027, which was obtained from the soil samples at Qian-jiang County of Hubei Province, China. LDM exhibited potent cytotoxicity toward cultured carcinoma cells in vitro as well as significant therapeutic efficacy against transplantable tumors in vivo. This paper overviews the highly potent antitumor activities and mechanisms of LDM in respect of cutting DNA strands, inducing apoptosis and mitotic cell death, triggering senescence-like phenotype, inhibiting angiogenesis and modulating the gene expression of invasive tumors.

关 键 词：力达霉素 DNA损伤 细胞凋亡 细胞裂亡 衰老样表型 血管生成 

分 类 号：R979.14[医药卫生—药品]