引用本文:	李冬,朱伟明,顾谦群,崔承彬,朱天骄,刘红兵,方玉春.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[J].海洋科学,2007,31(5):45-48.

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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
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
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

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。

关键词: 海洋放线菌次级代谢产物环二肽抗肿瘤活性

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基金项目: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)

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

Abstract:

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.

Key words: marine-derived actinomycete secondary metabolite diketopiperazine anti-tumor activity