CAJ | 학술논문

目的：评估化合物1-[4′-（（3R，5R）-金刚烷基）苯基）]正丁胺盐酸盐（T44）的体外抗肿瘤活性，并初步探索可能的分子机制，为这种化合物的综合应用提供实验依据。方法四甲基偶氮唑蓝比色法检测 T44对细胞的体外生长抑制作用；细胞形态观察法研究 T44对细胞形态的影响；流式细胞仪法检测 T44作用下肿瘤细胞周期和凋亡率的变化；蛋白印迹法检测 T44对不同周期蛋白表达的影响；细胞划痕实验检测 T44对肿瘤细胞迁移能力的影响。结果 T44对检测的11株肿瘤细胞的增殖均有抑制效果，对正常细胞人胚肺成纤维细胞也具有一定的增殖抑制作用，半数抑制浓度值为（16.58±3.49）μmol/ L，高于受测的大部分肿瘤细胞；T44能导致肿瘤细胞凋亡和周期阻滞；T44能影响周期蛋白的表达并能降低 HCT116细胞的迁移能力。结论 T44主要通过促进细胞凋亡来发挥抗肿瘤作用。
목적：평고화합물1-[4′-（（3R，5R）-금강완기）분기）]정정알염산염（T44）적체외항종류활성，병초보탐색가능적분자궤제，위저충화합물적종합응용제공실험의거。방법사갑기우담서람비색법검측 T44대세포적체외생장억제작용；세포형태관찰법연구 T44대세포형태적영향；류식세포의법검측 T44작용하종류세포주기화조망솔적변화；단백인적법검측 T44대불동주기단백표체적영향；세포화흔실험검측 T44대종류세포천이능력적영향。결과 T44대검측적11주종류세포적증식균유억제효과，대정상세포인배폐성섬유세포야구유일정적증식억제작용，반수억제농도치위（16.58±3.49）μmol/ L，고우수측적대부분종류세포；T44능도치종류세포조망화주기조체；T44능영향주기단백적표체병능강저 HCT116세포적천이능력。결론 T44주요통과촉진세포조망래발휘항종류작용。
Objective In order to provide experimental evidence for the comprehensive application of compound T44,we explored the possible mechanisms of its anti-tumor effects. Methods MTT assay was used to measure cell proliferation. Transition of cell cycle and apoptosis were tested by flow cytometer,respectively. Capacity of cell migration was detected by scratch assay. Western blotting was applied for determining the expression of different cyclins. Detection of cell morphology change was utilized to observe the influence on HCT116 cells. Results The proliferation of 11 kinds of tumor cell lines were decreased markedly as compared with those of control cells,and they showed distinct sensibility with one another. Half maximal(50% )inhibitory concemtration of human lung fibroblasts was(16. 58 ± 3. 49)μmol/ L,higher than most of the tumor cell lines. T44 treated HCT116 cells decreased cell migration and altered cyclins expression,as well. T44 could also lead to cell cycle block and apoptosis. Conclusion T44 participated into the control of tumor proliferation probably by modulation of cell cycle and induction of apoptosis.