Institute of Biochemistry, Splaiul Independentei 296, 060031 Bucharest 17, Romania.
Biometals. 2010 Jun;23(3):485-92. doi: 10.1007/s10534-010-9312-6. Epub 2010 Feb 27.
A number of studies have reported the anti-tumoral activity of lactoferrin, a property mediated by a variety of mechanisms such as inhibitory effects on tumor cell growth, NK cell activation, and enhancement of apoptosis. Liposomes are known to be an efficient drug delivery system which can enhance the therapeutic potential of the encapsulated compounds. We have used positively charged liposomes composed of phosphatidylcholine (PC), dioleoylphosphatidylethanolamine (DOPE), cholesterol (Chol) and stearylamine (SA) (6:1:2:1 M ratio) as a carrier system for bovine iron-free Lf (ApoBLf), and compared the in vitro effect of free and liposome-entrapped ApoBLf on the growth and morphology of murine melanoma B16-F10 cells. Liposomal formulation of ApoBLf was found to enhance the capacity of the protein to inhibit the cell proliferation by affecting cell cycle progression. The effect appeared to be due to the capacity of liposomes to increase the uptake of the protein and its accumulation into cells and probably to protect it from degradation, as revealed by fluorescence microscopy and flow cytometry. Our results demonstrate the ability of liposomes to improve the anti-tumor activity of Lf and suggest that liposomal protein may have a potential therapeutic use in the prevention and/or treatment of cancer diseases.
许多研究报告了乳铁蛋白的抗肿瘤活性，这种性质是通过多种机制介导的，如抑制肿瘤细胞生长、NK 细胞激活和增强细胞凋亡。脂质体已被证明是一种有效的药物递送系统，能够增强包封化合物的治疗潜力。我们使用由磷脂酰胆碱（PC）、二油酰基磷脂酰乙醇胺（DOPE）、胆固醇（Chol）和硬脂胺（SA）（6:1:2:1 M 比）组成的带正电荷的脂质体作为牛无铁乳铁蛋白（ApoBLf）的载体系统，并比较了游离和脂质体包封的 ApoBLf 对鼠黑色素瘤 B16-F10 细胞生长和形态的体外影响。发现 ApoBLf 的脂质体配方增强了该蛋白抑制细胞增殖的能力，从而影响细胞周期进程。这种作用似乎是由于脂质体能够增加蛋白的摄取及其在细胞内的积累，并可能保护其免受降解，这一点通过荧光显微镜和流式细胞术得到了证实。我们的结果证明了脂质体能够提高乳铁蛋白的抗肿瘤活性，并表明脂质体蛋白在预防和/或治疗癌症疾病方面可能具有潜在的治疗用途。
