【摘要】 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。更多还原

【Abstract】 Objective To research the proliferation effect of 4-thio-5-(2-thiophen) uridine on melanin cells as a newanti-cancer drug in vitro. Methods The effect of 4-thio-5-( 2-thiophen) uridine on human melanin(A375),murine melanin(B16) and human normal fibroblasts was tested by MTT and Sulforhodamine B(SRB)methods. The cell cycles and apoptosis were detected by flowcytometry(FCM). Results The 4-thio-5-(2-thiophen) uridine could significantly inhibit melanoma cells proliferation in a dose-dependent manner between human and murine melanin cells,but it was no inhibition for normal fibroblasts form human skin.The flowcytometry showed that the 4-thio-5-( 2-thiophen) uridine could lead to G2 / Mcell cycle arrest,inhibited mitosis and induced apoptosis. Conclusions The cytotoxicity effect of 4-thio-5-(2-thiophen) uridine on melanin is significant,but it has no effect on normal skin cells. This showed the 4-thio-5-(2-thiophen)uridine has the potential to become a newand targeted anti-cancer drug.更多还原