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目的探究新化合物4-硫-5-(2-噻吩基)尿嘧啶核苷酸体外对黑色素瘤细胞的增殖作用影响。方法利用MTT法和磺酰罗丹明B染色法对比考察该化合物对人黑色素瘤细胞(A375)、小鼠黑色素肿瘤细胞(B16)和人正常皮肤细胞体外增殖的影响,并利用流式细胞术检测不同药物浓度下该化合物对人黑色素瘤细胞(A375)周期的影响。结果 4-硫-5-(2-噻吩基)尿嘧啶核苷酸苷体外对人和小鼠的黑色素瘤细胞无种属特异性,均表现出剂量依赖性的抑制作用,但对正常皮肤细胞却无抑制作用;流式细胞术显示:4-硫-5-(2-噻吩基)尿苷导致剂量依赖性的G2细胞累积,抑制细胞有丝分裂;同时具有诱导细胞凋亡的作用。结论 4-硫-5-(2-噻吩基)尿嘧啶核糖核苷酸对黑色素瘤有明显抑制作用,对正常皮肤细胞无抑制作用表明该化合物对细胞作用时具有选择性,有可能成为新型靶向抗癌药物的候选者。
Objective To investigate the effects of 4-thio-5- (2-thienyl) uracil nucleotides on the proliferation of melanoma cells in vitro. Methods MTT assay and sulforhodamine B staining were used to compare the effects of the compound on the proliferation of human melanoma cells (A375), mouse melanoma cells (B16) and human normal skin cells in vitro. Flow cytometry Effect of the compound on the cycle of human melanoma cells (A375) at different drug concentrations. Results The 4-thio-5- (2-thienyl) uracil nucleoside showed no species-specific activity on human and mouse melanoma cells in vitro, all showed dose-dependent inhibition. However, normal skin cells Flow cytometry showed that 4-thio-5- (2-thienyl) uridine caused a dose-dependent accumulation of G2 cells and inhibited cell mitosis, and also had the effect of inducing apoptosis. CONCLUSION 4-thio-5- (2-thienyl) uracil ribonucleotide has obvious inhibitory effect on melanoma and no inhibitory effect on normal skin cells, indicating that the compound is selective for cell function and may be a new target Candidates for anticancer drugs.