2-氨基甲基-放线菌素D抑制肿瘤细胞增殖的特征

The characteristics of mAct D in inhibiting the proliferation of cancer cells

目的:研究2-氨基甲基-放线菌素D(2-aminomethyl-actinomycin D,mAct D)在对肿瘤细胞和正常细胞的增殖抑制活性及光、热稳定性几方面的特点,为mAct D的进一步开发利用提供理论依据。方法:采用Alamar blue法研究mAct D对体外培养的肿瘤细胞和正常的肝细胞增殖活性的影响;分别进行不同温度的热处理及不同时间的光照处理后检测mActD对肿瘤细胞增殖的影响,从而推测它们的光热稳定性;以上研究结果均以放线菌素D(actinomycin D,Act D)做对照。结果:与Act D相比,mAct D对各肿瘤细胞具有更高的增殖抑制活性,而对正常肝细胞HL7702和人胚肾细胞293T具有更低的抑制活性;两种化合物经过不同温度水浴和不同时间光照处理后,两者的抗肿瘤活性都有所降低,但是mAct D对肿瘤细胞的增殖抑制活性降低较平缓,显示出更高的光、热稳定性。结论:mAct D较Act D相比具有更多的优点,具有成为抗肿瘤新药的潜在价值。

OBJECTIVE To investigate the characteristics of 2-aminomethyl actinomycin D in the inhibiting activity of cancer cells, normal cells and optothermal stability, and to provide theoretical basis for the further exploitation of reAct D. METHODS The inhibiting activity of mAct D was detected by Alamar blue method. To detect the optothermal stability, Act D and mActD were treated with different temperature and light for different time, and then their inhibited proliferation activities in HepG2 cells were detected. RFNULTS Compared with Act D, reAct D showed higher inhibiting activity in cancer cells and lower in HL7702 and 293T cells. The antitumor activities of Act D and reAct D after light, heat treatment were both reduced, but compared with Act D, the activity of mAct D reduced slower. It was suggested that mAct D showed higher optothermal stability. CONCLUSION matt D showed more advantages than Act D, which suggested that mAct D was a potential new anticancer drug.