一株海洋放线菌次级代谢产物的抗肿瘤活性研究

目的 对一株南海深海海洋沉积物来源放线菌SCSIO 11594分离出的5个天然次级代谢产物进行初步的抗肿瘤活性研究.方法 将5个天然次级代谢产物命名为化合物1~5,通过CCK8细胞毒性试验检测化合物作用于5株肿瘤细胞及1株正常肝脏细胞HL-7702后的效果,通过Graphad prism软件测定其IC50,并与经典抗肿瘤药物顺铂对比.结果 顺铂作用于5株肿瘤细胞的IC50值范围3.75~5.32μmol/L,化合物2作用于5株肿瘤细胞的IC50值范围0.24~0.74μmol/L,对肿瘤细胞的抑制作用是顺铂的10~20倍;化合物4作用于5株肿瘤细胞的IC50值范围0.28~6.93μmol/L,对肿瘤细胞的抑制作用是顺铂的1~10倍;化合物2和4作用于正常肝脏细胞HL-7702的IC50值分别为3.67μmol/L和12.47μmol/L,与作用于肿瘤细胞的IC50值相比,提示具有较好的抗肿瘤选择性.结论 放线菌SCSIO 11594分离出的次级代谢产物2和4具有较好的抗肿瘤活性和选择性,具有潜在的开发前景.

Inhibitory effect of the secondary metabolities from a marine-derived strain against human cancer cells

Objective To study the antineoplastic activity of five secondary metabolites from Streptomyces sp. SCSIO 11594 which is isolated from the south deep-sea sediment. Methods Five secondary metabolites from Strepto-myces sp. SCSIO 11594 were named compound 1~5. CCK8 cytotoxicity was applied to evaluate the antineoplastic activity of compound 1~5 on five tumor cell lines and a normal human liver cell line HL7702. Half maximal inhibitory concentra-tion (IC50) was detected through Graphad prism and then compared with that of the classical antitumor drug Cisplatin. Results IC50 values of Ciplatin against five tumor cell lines were in the range of 3.76~5.32 μmol/L. IC50 values of Compound 2 against five tumor cell lines ranged from 0.24~0.74μmol/L, which was 10~20-fold more cytotoxic than the positive control Cisplatin. IC50 values of Compound 4 against five tumor cell lines ranged from 0.28~6.93μmol/L, which was 1~10-fold more cytotoxic than Cisplatin. IC50 values of Compound 2 and Compound 4 against normal human liver cell line HL7702 were 3.67μmol/L and 12.47μmol/L. The results demonstrated that Compound 2 and Compound 4 had good cytotoxic selectivity. Conclusion Two secondary metabolites from Streptomyces sp. SCSIO 11594 (Compound 2 and Compound 4) have good antitumor activity and cytotoxic selectivity, which own a good development prospect.