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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 study the characteristics of 2-aminomethyl-actinomycin D (mAct D) on the proliferation inhibition of tumor cells and normal cells and its light and thermal stability. Provide further theoretical basis for further development and utilization. Methods: Alamar blue method was used to study the effect of mAct D on the proliferation of tumor cells and normal liver cells in vitro. The effects of mActD on the proliferation of tumor cells were examined by heat treatment at different temperatures and light treatments at different times, Of light and heat stability; the above results are actinomycin D (actinomycin D, Act D) as a control. Results: Compared with Act D, mAct D had higher proliferation inhibitory activity on tumor cells and lower inhibitory activity on normal hepatocytes HL7702 and human embryonic kidney 293T cells. The two compounds were different temperature water bath and different After the time light treatment, the antitumor activity of both of them decreased, but mAct D reduced the proliferation inhibitory activity of tumor cells more gently and showed higher light and thermal stability. Conclusion: mAct D has more advantages than Act D, and has the potential value of becoming a new anti-tumor drug.