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目的阐明海洋来源常现青霉菌(Penicillium flavidorsum)SHK1-27代谢生产的抗肿瘤活性产物。方法用摇床发酵培养生产菌SHK1-27,通过跟踪活性,分离、纯化制备发酵物中的活性产物;根据理化性质并利用波谱技术确定化合物结构;用SRB法评价对K562细胞的抗肿瘤活性。结果从SHK1-27发酵物中分离得到8个蒽醌类化合物,并分别鉴定为nidurufin(1)、averufin(2)、8-O-methylaverufin(3)、6,8-O-dimethylaverufin(4)、versicolorin B(5)、versicolorin A(6)、ver-siconol(7)和averantin(8)。化合物1~8对K562细胞均显示出不同程度的细胞增殖抑制活性,其中,1和8的活性最强,IC50分别为12.6、27.7μmol.L-1;2、5、6和7的活性次之,IC50分别为72.4、91.0、98.7和93.4μmol.L-1;3和4的活性最弱,IC50均大于100μmol.L-1。这些化合物的抗肿瘤活性与化学结构之间呈现出一定的相关性。结论化合物1~8均为首次从常现青霉菌(Penicilliumflavidorsum)代谢产物中分离得到,1、5和6系首次从青霉属真菌产物中得到,7为首次从自然界中得到。首次报道化合物1~8对K562细胞的抗肿瘤活性。
Objective To elucidate the antitumor activity of metabolites produced by marine fungus Penicillium flavidorsum SHK1-27. Methods The strain SHK1-27 was cultured by shaker fermentation. The activity of the product was determined by separation and purification. The structure of the compound was determined by spectroscopic techniques. The antitumor activity of K562 cells was evaluated by SRB method. Results Eight steroids were isolated from SHK1-27 fermentation broth and identified as nidurufin(1), averufin(2), 8-O-methylaverufin(3), 6,8-O-dimethylaverufin(4). , versicolorin B (5), versicolorin A (6), ver-siconol (7) and averantin (8). Compounds 1~8 showed different degrees of cell proliferation inhibitory activity against K562 cells, among which, 1 and 8 had the strongest activity with IC50 of 12.6, 27.7 μmol.L-1; 2, 5, 6 and 7 times respectively. The IC50 values were 72.4, 91.0, 98.7, and 93.4 μmol.L-1, respectively; the activity of 3 and 4 was the weakest, and the IC50 was greater than 100 μmol.L-1. There is a certain correlation between the antitumor activity and the chemical structure of these compounds. Conclusion Compounds 1-8 were isolated from the Penicillium flavidort metabolites for the first time. The first, fifth and sixth series were obtained from Penicillium genus fungal products for the first time. 7 was firstly obtained from nature. The antitumor activity of compound 1-8 on K562 cells was first reported.