【摘要】 目的:5-氟尿嘧啶-纳米金复合体(5-fluorouracil-gold nanoconjugate,5-FU-GNP)的合成及其对HepG2细胞增殖抑制作用的观察。方法:采用化学合成法制备5-FU-GNP,并通过荧光淬灭实验和动态激光散射仪对其进行鉴定。细胞实验分为5-FU处理组、5-FU-GNP处理组和空白对照组。将HepG2细胞种于放有盖玻片的6孔板,培养24h后各组分别加入1.25mg/mL的5-FU溶液、1.25mg/mL的5-FU-GNP溶液和无血清培养液2mL,继续培养24h后固定,原子力显微镜(AFM)观察药物对HepG2细胞的增殖抑制作用;MTT比色法检测各组HepG2细胞增殖抑制率。结果:5-FU(2.5mg/mL)的荧光强度为23620.7±752.9,5-FU-GNP(2.5mg/mL)荧光强度为1909.0±283.9(P<0.01);GNP粒径为(13.20±1.15)nm,5-FU-GNP粒径为(21.67±3.64)nm(P<0.05)。AFM观察到药物处理后HepG2细胞膜内陷,粗糙度增加,表面孔径增大,出现较大的孔洞,以5-FU-GNP处理组变化更为明显。MTT比色法结果显示5-FU-GNP处理组HepG2细胞增殖抑制率为(52.07±1.07)%,明显高于5-FU处理组:(36.78±3.24)%(P<0.01)。结论:本实验成功合成了5-FU-GNP,原子力显微镜及MTT检测结果证实其较单纯5-FU对HepG2细胞有更强的增殖抑制作用。更多还原

【Abstract】 Objective To synthesize the 5-fluorouracil-gold nanoconjugate(5-FU-GNP)and observe its inhibition effect on HepG2 cells.Methods 5-FU-GNP was prepared by chemosynthesis and identified by fluorescence quenching experiment and dynamic light scattering(DLS).HepG2 cells were divided into 3 groups:5-FU treatment group,5-FU-GNP treatment group and control group.After seeded in 6-well plate and cultured for 24 h,HepG2 cells were treated with 2 mL of 5-FU(1.25 mg/mL),5-FU-GNP(1.25 mg/mL)and serum-free medium respectively.The samples were fixed after 24h culture and the inhibitory effect of the drugs on HepG2 cells was observed by atomic force microscope(AFM).Inhibition ratio of the HepG2 cells in each group was detected by MTT colorimetric method.Results The fluorescence intensity of 5-FU(2.5 mg/mL)was 23 620.7 ± 752.9 and 5-FU-GNP(2.5 mg/mL)was 1 909.0 ± 283.9,P < 0.01;The average size of GNP was(13.20 ± 1.15)nm while 5-FU-GNP was(21.67 ± 3.64)nm,P < 0.05,When treated with 5-FU or 5-FU-GNP,HepG2 cells membrane invagination,the increased roughness,the increased surface pore size and the larger holes were observed by AFM.There were more significant changes in the 5-FU-GNP group.MTT showed that the HepG2 cells inhibition ratio of 5-FU-GNP treatment group[(52.07 ± 1.07)%] was higher than that of 5-FU group[(36.78 ± 3.24)%],P < 0.01.Conclusion 5-FU-GNP has been synthesized and indicated enhanced drug potency in vitro by AFM and MTT assay.更多还原