CAJ | 학술논문

目的:研发针对中国南方和东南亚高发恶性肿瘤鼻咽癌的新型靶向抗癌药.方法:用本课题组合成的一种新型吲哚满酮类化合物IF239处理培养的鼻咽癌细胞系(CNE),酸性磷酸酶法测定化合物IF239对CNE细胞百分活率的影响;光学显微镜下观察细胞形态变化和黏附状态的改变;流式细胞术检测细胞周期时相的改变;Western blot检测细胞周期关键调控分子的变化.结果:IF239对CNE细胞具有强大的杀伤作用,其抗肿瘤机制可能与抑制细胞黏附和诱导细胞周期阻滞于G_2/M期有关;而G_2/M期阻滞与IF239上调cyclin B1和细胞周期蛋白依赖激酶1(CDK1)磷酸化水平有关.结论:IF239对CNE细胞的增殖抑制作用显著,其作用机制独特,具有潜在应用前景.
목적:연발침대중국남방화동남아고발악성종류비인암적신형파향항암약.방법:용본과제조합성적일충신형신타만동류화합물IF239처리배양적비인암세포계(CNE),산성린산매법측정화합물IF239대CNE세포백분활솔적영향;광학현미경하관찰세포형태변화화점부상태적개변;류식세포술검측세포주기시상적개변;Western blot검측세포주기관건조공분자적변화.결과:IF239대CNE세포구유강대적살상작용,기항종류궤제가능여억제세포점부화유도세포주기조체우G_2/M기유관;이G_2/M기조체여IF239상조cyclin B1화세포주기단백의뢰격매1(CDK1)린산화수평유관.결론:IF239대CNE세포적증식억제작용현저,기작용궤제독특,구유잠재응용전경.
Objective: To develop novel targeted anticancer medicines for effective treatment of nasopharyngeal carcinoma ( NPC) , a prevalent malignant disease in southern China and southeast Asia.Methods: CNE cells were treated with a novel indolinone IF239 synthesized by our research group. Cell viability was determined by the acid phosphatase assay ( APA). Morphologic changes and adhesion status of CNE cells treated with IF239 were observed under a light microscope. Flow cytometry was used to analyze the cell cycle phases . Key regulating molecules in the cell cycle progression were detected by Western blotting. Results: IF239 had potent cytotoxic effect on CNE cells. The possible antitumor mechanisms of IF239 involved inhibition of cell adhesion and cell cycle arrest in the G2_/M phase. Moreover,G2_/M arrest caused by IF239 was related to up-regulation of both cyclin B1 and the phosphorylation level of CDK1. Conclusion: IF239 has high anticancer activity over CNE cells, and has unique anticancer mechanisms, suggesting that IF239 has promising application potentials.