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目的研究黄直丝链霉菌18522代谢产物中的环二肽类细胞周期抑制剂。方法采用温敏型小鼠乳腺癌tsFT210细胞的流式细胞术模型,以细胞周期抑制活性为指标,对黄直丝链霉菌18522发酵液和菌丝体的氯仿提取物进行活性成分追踪分离;根据理化性质和光谱数据鉴定化合物的化学结构;采用流式细胞术测定化合物的细胞周期抑制活性。结果从氯仿提取物中分离得到6个环二肽类化合物,分别鉴定为环(丙-亮)[cyclo(Ala-Leu),1]、环(丙-异亮)[cyclo(Ala-Ile),2]、环(丙-缬)[cyclo(Ala-Val),3]、环(苯丙-亮)[cyclo(Phe-Leu),4]、环(丙-脯)[cyclo(Ala-Pro),5]和环(苯丙-缬)[cyclo(Phe-Val),6];流式细胞术测试结果表明,化合物1~6均显示细胞周期G0/G1期抑制活性。结论首次报道化合物1~6具有细胞周期抑制活性。
Objective To study the cyclic dipeptide cell cycle inhibitors in the metabolites of Streptomyces lividans. Methods The flow cytometry model of tsFT210 cells was established. The cell cycle inhibitory activity was taken as an index to trace the active constituents of the chloroform extracts of Streptomyces lividans 18522 and mycelia. According to the physicochemical properties And spectral data to identify the chemical structure of the compound; the cell cycle inhibitory activity of the compound was determined using flow cytometry. Results Six cyclic dipeptides were isolated from the chloroform extract and identified as cyclo (Ala-Leu), Cyclo [Ala (Ala) -Leu] 2], cyclo (Ala-Val) 3, cyclo (Phe-Leu) 4, cyclo [ Pro and 5 and cyclo (Phe-Val) 6, respectively. The results of flow cytometry showed that compounds 1-6 exhibited inhibitory activity in G0 / G1 phase of the cell cycle. Conclusions The first reported compound 1 ~ 6 has cell cycle inhibitory activity.