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目的 :研究嗜线虫杆菌次级代谢产物吲哚衍生物的抗肿瘤活性。方法 :用有机溶剂萃取和硅胶柱层析对嗜线虫杆菌发酵液进行提取和分离 ,获得吲哚衍生物 ,用MTT法测定其体外杀肿瘤细胞作用 ,利用裸鼠接种人HeLa细胞模型检测其体内抗肿瘤活性。结果 :从发酵液粗提物中分离得到 5个组分 ,从有抗肿瘤活性的组分中再分离得到化合物 3 吲哚乙基 (3’ 甲基 2’ 酮 )戊酰胺 ,其对HepG2 ,HeLa,HT 2 9,BGC 82 3和K5 6 2的IC50 分别为(0 .12± 0 .0 1) ,(1.83± 0 .0 2 ) ,(6 .16± 0 .5 2 ) ,(1.4 5± 0 .12 ) ,(5 .90± 1.17) μg·mL-1,对正常人肺成纤维细胞MRC 5和正常人肝细胞L 0 2生长的影响很小。接种HeLa肿瘤细胞裸鼠连续灌服上述吲哚衍生物 (2 ,4和 8mg·kg-1) 7d ,抑瘤率分别为 4 8.1% ,5 6 .5 %和 72 .2 %。结论 :嗜线虫杆菌发酵液来源的 3 吲哚乙基 (3’ 甲基 2’ 酮 )戊酰胺具有较强的抗肿瘤活性。
Objective: To study the antitumor activity of the indole derivatives of the second metabolite of. Methods: Extraction and separation of the fermentation broth of H. cordis by organic solvent extraction and silica gel column chromatography were used to obtain indole derivatives. MTT assay was used to determine the effect of killing tumor cells in vitro. The nude mice inoculated with HeLa cells were used to detect the in vivo Antitumor activity. Results: Five components were isolated from the crude extracts of the fermentation broth. Indole ethyl (3 ’methyl 2’ keto) pentanamide was isolated from the components with antitumor activity and the inhibitory effect on HepG2, The IC50s of HeLa, HT2 9, BGC 82 3 and K5 6 2 were (0.12 ± 0.01), (1.83 ± 0.22), (6.16 ± 0.52), (1.4 5 ± 0.12) and (5.90 ± 1.17) μg · mL-1, respectively, had little effect on the growth of MRC 5 in normal human lung and L 0 2 in normal human hepatocytes. The nude mice inoculated with HeLa tumor cells continuously inoculated with the aforementioned indole derivatives (2, 4 and 8 mg · kg-1) for 7 days, the tumor inhibition rates were 4 8.1%, 56.5% and 72.2%, respectively. CONCLUSION: 3 indole ethyl (3 ’methyl 2’ keto) pentanamide derived from the fermentation broth of H. cordis has strong anti-tumor activity.