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从海洋小单孢菌FIM02-523的发酵液中分离到一个新的缩肽类化合物rakicidin B1(1)及两个已知化合物rakicidin A(2)和rakicidin B(3)。通过一维、二维核磁图谱、红外光谱、紫外光谱和高分辨质谱确定了3个化合物的结构。测定了3个化合物对HCT-8、MGC803、A549、A375、Hep G2和CASKI 5种人肿瘤细胞株的细胞毒活性,结果显示化合物1、2和3对这些肿瘤细胞株均具有显著的抑制活性(对这5个肿瘤细胞株,化合物1的IC50值分别为0.341,0.121,0.394,0.066和2.516μg/m L;化合物2的IC50值分别为0.731,0.991,0.226,0.040和0.576μg/m L;化合物3的IC_(50)值分别为0.347,0.104,0.216,0.041和2.239μg/m L),化合物1和3的抗肿瘤活性相当。
A novel depsipeptide rakicidin B1 (1) and two known compounds rakicidin A (2) and rakicidin B (3) were isolated from the fermentation broth of FIM02-523. The structures of three compounds were confirmed by one-dimensional and two-dimensional nuclear magnetic resonance spectra, infrared spectra, ultraviolet spectra and high resolution mass spectra. The cytotoxic activities of three compounds on human tumor cell lines HCT-8, MGC803, A549, A375, Hep G2 and CASKI were determined. The results showed that compounds 1, 2 and 3 had significant inhibitory activities on these tumor cell lines (For these 5 tumor cell lines, IC50 values for compound 1 were 0.341, 0.121, 0.344, 0.066 and 2.516 μg / m L, respectively; IC50 values for compound 2 were 0.731, 0.991, 0.226, 0.040 and 0.576 μg / ; Compound 3 has IC50 values of 0.347, 0.104, 0.216, 0.041 and 2.239 μg / mL, respectively), and compounds 1 and 3 have comparable antitumor activity.