海洋放线菌H2003代谢产物中环二肽成分及其抗肿瘤活性的初步研究  

Structural identification and anti-tumor activity of Diketopi-perazines from secondary metabolites of marine-derived actinomycete H2003

作　　者：李冬[1] 朱伟明[1] 顾谦群[1] 崔承彬[1,2] 朱天骄[1] 刘红兵[1] 方玉春[1] 

机构地区：[1]教育部海洋药物重点实验室,山东省海洋药物重点实验室,中国海洋大学海洋药物与食品研究所 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《海洋科学》2007年第5期45-48,共4页Marine Sciences

基　　金：国家863计划项目(2003AA624020);山东省科技攻关项目(012110107);山东省重点基金项目(Z2001C01);国家教育部长江学者奖励计划项目;青岛市自然科学基金项目(04-2-JZ-81)

摘　　要：海洋来源放线菌H2003发酵产物的粗提物对小鼠乳腺癌细胞tsFT210具有明显的细胞毒活性。为了发现其抗肿瘤活性成分,采用活性跟踪的分离方法,经多次硅胶柱色谱、凝胶柱色谱及高效液相色谱分离,从菌株H2003发酵液中分离得到了7个环二肽化合物。经核磁共振光谱、质谱和旋光分析,其结构分别鉴定为cyclo(L-Leu-L-Pro)(1),cyclo(D-Val-L-Pro)(2),cyclo(Gly-L-Leu)(3),cyclo(L-Pro-L-Try)(4),cyclo(Gly-D-Phe)(5),cyclo(Gly-L-Pro)(6)和cyclo(L-Ala-L-Phe)(7)。其中化合物1通过SRB法测试表现出弱的抗肿瘤活性,系首次报道。The fermentation of the marine-derived actinomycete H2003 showed toxicity on tsFT210 cells. In order to isolate and identify the bioactive components, the secondary metabolite of the fermentation of H2003 was studied. Through bioassay-guided fractionation of necrosis on tsFT210 cells, seven diketopiperazines were isolated from the secondary metabolites of actinomycete H2003 by repeating chromatography over silica gel, sephadex LH-20 and HPLC. Their structures were identified by the spectroscopic methods and anti-tumor activities were assayed by SRB method. Compound（1） showed weak anti-tumor activity on tsFT210 cells.

关 键 词：海洋放线菌 次级代谢产物 环二肽 抗肿瘤活性 

分 类 号：Q516[生物学—生物化学]