叶酸受体介导卵巢癌细胞靶向白蛋白纳米粒的体外研究-中国显微图像网.PDFVIP

_______________________________________________________________________________ 叶酸受体介导卵巢癌细胞靶向白蛋白纳米粒的体外研究* 1 1△ 1 2 1 3 张良珂P P 侯世祥P P 毛声俊P P 魏大鹏P P 宋相容P P 乔小蓉P 1. 四川大学华西药学院药剂教研室 （成都610041 ）； 2. 四川大学基础医学与法医学院免疫教研室；3. 四川大学分析测试中心 【摘要】 目的 研究能通过叶酸受体介导靶向肿瘤细胞的叶酸偶联白蛋白纳米粒。方法 利用叶酸活性酯在碱 性条件下与白蛋白纳米粒表面上的氨基反应，制得叶酸偶联的白蛋白纳米粒。以荧光定量法确定浓度、时间、 游离叶酸对肿瘤细胞摄取叶酸偶联白蛋白纳米粒的影响程度。结果 成功制备了叶酸偶联白蛋白纳米粒。叶酸 偶联白蛋白纳米粒的肿瘤细胞摄取量随纳米粒浓度增大、培养时间延长而增加，肿瘤细胞对叶酸偶联白蛋白纳 米粒的摄取可被过量的外源性游离叶酸所抑制。结论 叶酸偶联白蛋白纳米粒能通过细胞膜上的叶酸受体介导 内吞入胞，可显著靶向于叶酸受体丰富的肿瘤细胞。 【关键词】 白蛋白纳米粒 叶酸受体 靶向 Study on the ovarian tumor cell targetability of folate receptor-mediated albumin nanoparticles 【Abstract 】Objective To study folate-conjugated albumin nanoparticles targeting to tumor cells via folate receptor-mediated endocytosis. Methods The activated folic acid (N-hydroxysuccinimide ester of folic acid) were conjuated to the surface of BSANP via the amino groups. The extent that concentration, incubated time and free folate influenced uptake of folate-BSANPs by SKOV3 cell was determined respectively using fluorescence spectrophotometer. Results Folate-conjugated BSANP (Folate-BSANP) was successfully achieved. Uptake of folate-BSANPs by tumor cells was gradually increased while extending incubated time or increasing concentration of folate-BSANPs and could be competitively inhibited by excess free folate. Conclusion Folate-BSANP could be delivered into tumor cells via folate receptor-mediated endocytosis and significantly targeted to tumor cells with rich folate receptors. 【Key words 】Albumin nanoparticles ; Folate receptor ; Targeting 随着对细胞膜表面叶酸受体认识的逐步深入研 进行了研究，并选用人卵巢癌 SKOV3 细胞作为模型 究发现，在多种肿瘤细胞(如卵巢癌、肺癌、乳腺癌、