土壤链霉菌Streptomyces ardus WS-65090产生的teleocidin类化合物及其生物活性研究

Teleocidin compounds from the soil-derived Streptomyces ardus WS-65090 and their bioactivities

研究土壤链霉菌Streptomyces ardus WS-65090的次级代谢产物及其生物活性。采用制备高效液相色谱,从该菌株发酵液的乙酸乙酯提取物中共分离得到5个teleocidin类化合物,通过HR-MS、1D、2D-NMR、IR等波谱分析、化学转化及与文献报道波谱数据比较等方法将其鉴定为14-O-acetylteleocidin B-2(1)、14-O-acetylteleocidin B-3(2)、teleocidin B-2(3)、teleocidin B-3(4)、teleocidin A-2(5),其中化合物1为新化合物,2为新的天然产物。杀虫活性测试表明化合物1~5对草地贪夜蛾、棉铃虫、小菜蛾和蚜虫均具有毒杀活性,其LC_(50)值为36.5~305.7μg/mL。体外细胞毒活性实验结果表明化合物1~5对A875、HepG2和Marc-145细胞系具有较强的细胞毒活性,其IC_(50)值为3.08~18.40μM。

To investigate the secondary metabolites produced by Streptomyces ardus WS-65090 from soil and their bioactivities.Five teleocidin compounds(1-5)were isolated from the ethyl acetate extract of fermentation culture of S.ardus strain WS-65090 by preparative HPLC.The compounds were elucidated as new teleocidin analogue 14-O-acetylteleocidin B-2(1),and new naturally occurring teleocidin analogue 14-O-acetylteleocidin B-3(2),and three known compounds teleocidin B-2,B-3 and A-2(3-5)by extensive spectroscopic analysis,including HR-MS,1D and 2D NMR,combined with chemical transformation methods and comparison with literature data,etc.Insecticidal activities and cytotoxicity of compounds 1-5 were investigated under laboratory conditions.All compounds showed insecticidal activities against Spodoptera frugiperda,Helicoverpa armigera,Plutella xylostella,and Aphis craccivora with LC_(50) values from 36.5 to 305.7μg/mL,and exhibited cytotoxicity against A875,HepG2 and Marc-145 cell lines with IC_(50) from 3.08 to 18.40μM.