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目的阐明海洋暗蓝青霉Penicillium lividum BF-20代谢生产的抗肿瘤活性次级代谢物。方法 24℃静置25d发酵菌株P.lividum BF-20;采用活性跟踪分离纯化发酵物中的活性代谢物;根据理化性质和波谱方法(ESI MS、UV、IR、NMR等)鉴定化合物结构;采用磺酰罗丹明B蛋白染色法(SRB)法和流式细胞术评价化合物对K562细胞的抗肿瘤活性。结果从菌株P.lividumBF-20发酵物中分离得到2个活性酮类化合物,鉴定为1,7-dihydroxy-3-methyl-8-carbomethoxyxanthone(1)和1,6-dihydroxy-3-methyl-8-carbomethoxyxanthone(2)。SRB测定结果发现化合物1和2对K562细胞显示增殖抑制活性,IC50分别为4.02和39.46μmol/L。流式细胞术检测结果发现,当1浓度大于7.5μmol/L时能引起K562细胞的SubG1期细胞数明显增多,并呈一定的浓度相关性。结论化合物1和2首次从海洋暗蓝青霉P.lividum代谢产物中分离得到,1和2不同程度地抑制K562细胞的增殖。
Objective To elucidate the anti-tumor secondary metabolites metabolized by Penicillium lividum BF-20. Methods The active metabolites were isolated and purified from the fermentation of P.lividum BF-20 for 25 days at 24 ℃. The structures of the compounds were identified by physico-chemical properties and spectroscopic methods (ESI MS, UV, IR, NMR, etc.) The anti-tumor activity of the compounds on K562 cells was evaluated by sulforhodamine B protein staining (SRB) assay and flow cytometry. Results Two active ketones were isolated from the fermentation of P.lividumBF-20 and identified as 1,7-dihydroxy-3-methyl-8-carbomethoxyxanthone (1) and 1,6-dihydroxy-3-methyl- 8-carbomethoxyxanthone (2). SRB assay showed that compounds 1 and 2 showed inhibitory activity against K562 cells with IC50 of 4.02 and 39.46 μmol / L, respectively. The results of flow cytometry showed that when the concentration of 1 was higher than 7.5μmol / L, the number of SubG1-phase cells in K562 cells was significantly increased and showed a certain concentration correlation. Conclusion Compounds 1 and 2 were isolated from P.lividum metabolites for the first time. 1 and 2 inhibited the proliferation of K562 cells to some extent.