从细脚拟青霉分离的新环二肽与新十元环内酯

摘要

Paecilomyces tenuipes with high edible and medicinal value was the anamorph of Cordyceps takaomontana. Four compounds were isolated from the cultured broth of Paecilomyces tenuipes by repeated column chromatography over RP-18, sephadex LH-20 and silica gel. Their structures were determined on the basis of NMR data, HRMS-EI technique and X-ray single crystal diffraction. One novel diketopiperazine ( 3 S )-6-benzyl-3-isopropyl-1-methylpiperazine-2 , 5-dione ( 1 ) and one novel ten-membered macrolide (4S,10R)-4-hydroxy-10-methyloxecane-2,8-dione(2), together with two known ten-membered macrolides Cepharosporolide C(3) and Cepharosporolide E(4) were obtained. Compound 1 showed the moderate cytoto-xicity in the MTT assay against prostate cancer cells 22 RV1 and DU-145 with inhibition rate of 37.8% and 38.6%, and those of compound 2 were 32.5% and 40.6%, respectively.%利用反相色谱、凝胶色谱和硅胶色谱从细脚拟青霉发酵液中分离得到4个活性化合物.通过核磁共振波谱、质谱、X射线晶体衍射分析和理化数据鉴定化合物1为新环二肽[(3S)-6-苯乙基-3-异丙基-1-甲基-2,5-二酮哌嗪],化合物2为新十元环内酯[(4S,10R)-4-羟基-8-氧代-10-甲基癸内酯],化合物3为Cepharos-porolide C,化合物4为Cepharosporolide E.细胞毒性实验结果表明,5μmol/L的化合物1对前列腺癌细胞22RV1和DU-145的抑制率分别为37.8%和38.6%,5μmol/L的化合物2对前列腺癌细胞22RV1和DU-145的抑制率分别为32.5%和40.6%,具有一定抗肿瘤活性.