血管内皮生长因子-阿柔比星脂质体靶向杀伤恶性黑素瘤细胞的实验观察

目的 应用包裹阿柔比星的血管内皮生长因子（VEGF）的长循环脂质体（阿柔比星-VEGF-SSL）于体外靶向杀伤恶性黑素瘤细胞。方法 通过体外结合试验，验证阿柔比星-VEGF-SSL对恶性黑素瘤A375细胞的特异结合能力。通过体外细胞毒试验（MTT），检测阿柔比星-VEGF-SSL对A375细胞增殖活性的影响。结果 阿柔比星-VEGF-SSL可与A375细胞特异结合，结合率可达非特异性脂质体的2.15倍。阿柔比星-VEGF-SSL可特异抑制A375细胞的增殖活性。48 h细胞毒试验阿柔比星-VEGF-SSL抑制A375细胞增殖活性的作用与游离阿柔比星相似（P ＞ 0.05），优于无VEGF的阿柔比星脂质体（阿柔比星-SSL）（P ＜ 0.05），而对非靶细胞（黑素细胞）增殖活性的抑制作用弱于两者。0.5 h预处理试验表明：缩短药物与细胞接触时间后，阿柔比星-VEGF-SSL仍保持较强抑制A375细胞增殖活性的作用。结论 阿柔比星-VEGF-SSL可特异性识别恶性黑素瘤A375细胞，并作为良好载体将阿柔比星带入瘤细胞，显著抑制A375细胞的增殖活性，实现其靶向杀伤作用。

Targeted killing of malignant melanoma cells by aclarubicin liposome conjugated with vascular endothelial growth factor

Objective To evaluate the targeted killing of malignant melanoma cells by aclarubicin liposomes conjugated with vascular endothelial growth factor(ADM-VEGF-SSL)in vitro.Metheds To detect the binding abilitv of liposomes to malignant melanoma(MM)cells,the human malignant melanoma cell line A375 was cultured in the presence of ADM-VEGF-3H-SSL or ADM-3H-SSL for 2 days followed by the detection of radioactivity of these cells.Then.A375 cells were cultured with various concentrations(0.01,0.1,1,10,100 mol/L)of ADM-VEGF-SSL,ADM-SSL or free ADM for 48 hours in the 48-hour cytotoxity test,or for 0.5 hour followed by another 48-hour culture in drug-free medium in the 0.5-hour cytotoxity test.After that,MTT assay was used to detect the survival rate of these cells.Results ADM-VEGF-SSL could specifically bind to and kill A375 cells.The binding rate of ADM-VEGF-SSL was 2.15 folds as high as that of ADM-SSL.The survival rate of A375 cells after being treated with ADM-VEGF-SSL for 48 hour was similar to that with flee ADM(P＞0.05).but lower than that with ADM-SSL(P＜0.05),while the survival rate of melanocytes treated with ADM-VEGF-SSL was higher than that with free ADM or ADM-SSL(both P＜0.05).As shown by the 0.5-hour cytotoxity test.shortening the treatment course did not attenuate the effect of ADM-VEGF-SSL on A375 cells.Conclusions ADM-VEGF-SSL can specifically recognize A375 cells.efficiently deliver adriamycin into tumor cells,markedly inhibit the proliferation of A375 cells,and eventually,a targeted kill of these cells is realized.