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研究深海沉积物来源的链霉菌Streptomyces malaysiensis OUCMDZ-2167的活性天然产物.采用硅胶和凝胶柱色谱及高效液相色谱等手段,从链霉菌S.malaysiensis OUCMDZ-2167的发酵产物中分离纯化了1个新的呋喃衍生物1以及10个已知物2~11;采用质谱、紫外、红外、核磁共振和比旋光等方法将其结构分别鉴定为:4-羟甲基呋喃-2-甲酸甲酯(1)、呋喃-2,4-二甲酸二甲酯(2)、格尔德霉素(3)、17-O-去甲基格尔德霉素(4)、尼日利亚菌素(5)、尼日利亚菌素钠(6)、30-O-乙酰基尼日利亚菌素(7)、奥布菌素(8)、洋橄榄叶素(9)、surugapyrone A(10)和杀菌素A(11).采用细胞计数试剂盒-8(CCK-8)和噻唑蓝(MTT)法分别评价了化合物对K562和MCF-7及A549肿瘤细胞株的细胞毒活性,结果表明:化合物3、5~9对A549的半数抑制浓度(IC_(50))分别为2.56±0.30、0.96±0.03、0.96±0.04、0.81±0.05、7.11±0.90和4.09±0.70μmol·L-1,化合物5~9对K562的IC_(50)值分别1.46±0.11、1.08±0.03、0.48±0.10、4.68±0.19和9.60±0.50μmol·L-1,化合物5、8和9对MCF-7的IC_(50)值分别为0.29±0.15、4.05±0.50和4.81±0.70μmol·L-1;其中化合物5~8对K562和A549以及化合物5和8对MCF-7的细胞毒活性为首次报道.
To study the active natural product of Streptomyces malaysiensis OUCMDZ-2167 from deep-sea sediment, 1 (1) was isolated and purified from the fermentation product of Streptomyces sp. Malaysiensis OUCMDZ-2167 by silica gel, gel column chromatography and high performance liquid chromatography New furan derivatives 1 and 10 known compounds 2 ~ 11. Their structures were identified as: methyl 4-hydroxymethylfuran-2-carboxylate by mass spectrometry, ultraviolet, infrared, nuclear magnetic resonance and specific rotation, (2), geldanamycin (3), 17-O-desmethylgeldanamycin (4), nigerianin (5) , Niacin Sodium (6), 30-O-acetyl Niriomycin (7), Abutilin (8), Olivin (9), surugapyrone A (10) and spinosyn A The cytotoxic activities of the compounds against K562, MCF-7 and A549 tumor cell lines were evaluated by cell counting kit-8 (CCK-8) and MTT assay, respectively. The results showed that the compounds 3-5, The IC50 values of A549 were 2.56 ± 0.30, 0.96 ± 0.03, 0.96 ± 0.04, 0.81 ± 0.05, 7.11 ± 0.90 and 4.09 ± 0.70 μmol·L-1, respectively. The IC_ (50) (50) points 1.48 ± 0.11, 1.08 ± 0.03, 0.48 ± 0.10, 4.68 ± 0.19 and 9.60 ± 0.50μmol·L-1 respectively. The IC 50 values of compound 5, 8 and 9 for MCF-7 were 0.29 ± 0.15 and 4. 05 ± 0.50 and 4.81 ± 0.70μmol·L-1. The cytotoxic activity of compounds 5 to 8 to MCF-7 on K562 and A549 and compounds 5 and 8 was first reported.