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目的探讨人工合成钠离子通道阻断剂-钠离子胺类配体(sodium channel amine ligands,SCALs)对乳腺癌细胞株(MCF-7、MDA-MB-231)的抑制效果,以筛选高效的抗肿瘤药物。方法在药物作用后,采用MTT法检测肿瘤细胞的增殖活性;流式细胞术检测SCALs促进细胞凋亡及阻滞细胞周期的能力。结果 7种SCALs中的S1127对乳腺癌细胞敏感,肿瘤细胞增殖明显受到抑制,且其抑制率与药物浓度呈剂量-效应关系,S1127对MCF-7细胞和MDA-MB-231细胞的IC_(50)分别为17.2μM和21.8μM,在25μM时能促进80.6%的MCF-7细胞凋亡以及18.4%的MDA-MB-231细胞凋亡,并将细胞阻滞于G0/G1期。结论合成的钠离子通道阻断剂S1127具有显著杀伤乳腺癌细胞效应,将来有可能成为治疗肿瘤的一类新型备选药物。
Objective To investigate the inhibitory effect of synthetic sodium channel blockers sodium channel amine ligands (SCALs) on breast cancer cell lines (MCF-7, MDA-MB-231) Oncology drugs. Methods The proliferation of tumor cells was detected by MTT assay after drug treatment. The ability of SCALs to promote apoptosis and arrest the cell cycle was detected by flow cytometry. Results S1127 in 7 kinds of SCALs was sensitive to breast cancer cells, the proliferation of tumor cells was obviously inhibited, and the inhibition rate was dose-effect relationship with drug concentration. The IC 50 of S1127 to MCF-7 cells and MDA-MB-231 cells ) Were 17.2 μM and 21.8 μM, respectively, which promoted apoptosis of 80.6% MCF-7 cells and 18.4% of MDA-MB-231 cells at 25μM, and arrested cells in G0 / G1 phase. Conclusion The synthetic sodium channel blocker S1127 has a significant cytotoxic effect on breast cancer cells and may become a new class of alternative drugs for tumor treatment in the future.