Wang Dahong, Yuan Jiangfeng, Tao Wenyi
College of Food and Bioengineering, Henan University of Science and Technology.
College of Food and Bioengineering, Henan University of Science and Technology,Luoyang, Henan, China.
Iran J Pharm Res. 2014 Winter;13(1):171-80.
This work was to isolate and identify the bioactive secondary metabolite which was produced by myxobacterium Stigmatella eracta WXNXJ-B, and to evaluate its antitumor and apoptosis-inducing effects. The results showed that one novel compound (molecular formula C29H25NO3) was isolated, purified by Sephadex LH-20 column chromatography and preparative RP-HPLC, and identified as 5-(6-benzyl-quinolin-3-ylmethyl)-6- phenyl-3,7-dioxa- bicycle [4.1.0] heptan-3-one (named as quinoxalone) according to its UV, IR, HRMS and NMR spectra. The compound showed strong antitumor activity on B16, HepG2, MCF-7, SGC-7901, MDA-MB231 and CT-26 six tumor cell lines in-vitro. Nevertheless, it showed less cytotoxic to the mouse normal spleen cells (IC50 was 836.27 ± 13.02 µg mL(-1)). The cytotoxic study on HepG2 cells in-vitro showed that quinoxalone could induce the change of cell nuclear and arrested the cell division in the S and G2/M phase. Our results suggest that quinoxalone could be a potential anti-cancer agent.
本研究旨在分离和鉴定由粘细菌直立刺柱菌WXNXJ-B产生的具有生物活性的次生代谢产物，并评估其抗肿瘤和诱导凋亡的作用。结果表明，通过Sephadex LH-20柱色谱和制备型RP-HPLC分离并纯化得到一种新型化合物（分子式为C29H25NO3），根据其紫外光谱、红外光谱、高分辨质谱和核磁共振谱鉴定为5-(6-苄基喹啉-3-基甲基)-6-苯基-3,7-二氧杂双环[4.1.0]庚烷-3-酮（命名为喹喔酮）。该化合物在体外对B16、HepG2、MCF-7、SGC-7901、MDA-MB231和CT-26六种肿瘤细胞系表现出较强的抗肿瘤活性。然而，它对小鼠正常脾细胞的细胞毒性较小（IC50为836.27±13.02μg mL(-1)）。体外对HepG2细胞的细胞毒性研究表明，喹喔酮可诱导细胞核变化并使细胞分裂停滞在S期和G2/M期。我们的结果表明，喹喔酮可能是一种潜在的抗癌药物。
