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目的对海洋放线菌Micromonospora sp.(M2DG17)中的活性次生代谢产物进行研究。方法在活性追踪分离思路的指导下,综合利用硅胶开放柱色谱、ODS中低压柱色谱、Sephadex LH-20凝胶柱色谱以及高效液相色谱等分离技术进行化合物的分离、纯化;利用化合物理化性质和波谱学分析对单体化合物进行结构鉴定,并对其进行活性评价。结果从海洋放线菌Micromonospora sp.(M2DG17)发酵物中分离得到了7个化合物,分别鉴定为3-羟甲基-β-卡巴林(3-hydroxymethyl-β-carboline,1)、3-甲基-β-卡巴林(3-methyl-β-carbo-line,2)、β-卡巴林(β-carboline,3)、环(L-脯-L-苯丙)二肽[Cyclo-(L-Pro-L-Phe),4]、环(L-脯-L-缬)二肽[Cyclo-(L-Pro-L-Val),5]、环(L-脯-L-亮)二肽[Cyclo-(L-Pro-L-Leu),6]以及环(L-脯-L-异亮)二肽[Cyclo-(L-Pro-L-Ile),7],并对单体化合物进行了HCT116细胞生长抑制活性测试。结论化合物1~4、6为首次从该菌中分离得到,化合物2显示出弱的HCT116细胞生长抑制活性(IC50为65.0μmol.L-1)。
Objective To study the active secondary metabolites in marine actinomycetes Micromonospora sp. (M2DG17). Methods Under the guidance of the method of active tracing and separation, the compounds were isolated and purified by silica gel column chromatography, ODS low pressure column chromatography, Sephadex LH-20 gel column chromatography and high performance liquid chromatography. The chemical and physical properties The structure of the monomer compounds was identified by spectroscopic analysis and the activity of the compounds was evaluated. Results Seven compounds were isolated from the marine actinomycetes Micromonospora sp. (M2DG17) and identified as 3-hydroxymethyl-β-carboline (1), 3- 3-methyl-β-carbo-line (2), β-carboline (3), cyclo-L- (L-Pro-L-Val), 4], Cyclo- (L-Pro-L-Val) (Cyclo- (L-Pro-L-Leu) 6], and cyclic (L-Pro-L- Compounds were tested for HCT116 cell growth inhibitory activity. Conclusions Compounds 1 to 4 and 6 were isolated from this strain for the first time. Compound 2 showed weak growth inhibitory activity against HCT116 cells (IC50: 65.0 μmol·L-1).