Solubilization and anticancer-activity enhancement of Methotrexate by novel dendrimeric nanodevices synthesized in one-step reaction.
Solubilization and anticancer-activity enhancement of Methotrexate by novel dendrimeric nanodevices synthesized in one-step reaction.
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DOI：
10.1016/j.bioorg.2012.01.002
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发表时间：
2012-04
影响因子：
5.1
通讯作者：
Delia Soto‐Castro;Jorge A. Cruz-Morales;M. T. Ramírez Apán;Patricia Guadarrama
中科院分区：
文献类型：
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作者：
Delia Soto‐Castro;Jorge A. Cruz-Morales;M. T. Ramírez Apán;Patricia Guadarrama
描述了用于靶向癌症治疗的基于 PAMAM 框架的纳米器件的一步合成。通过尺寸区分正确分离并表征了四种水溶性纳米器件（命名为 F1 至 F4 级分）。从细胞生长抑制百分比的生物学测定来看，作为纳米器件一部分的甲氨蝶呤（化疗药物）的抗癌活性通常比癌细胞系有所增加，尤其是在人类淋巴细胞的情况下，细胞生长抑制百分比急剧下降（超过80％），因此，纳米器件在健康细胞和患病细胞之间表现出良好的区分能力。从表征可以得出结论，合成的纳米器件提供了药物运输的双重方案：封装和缀合。
The one-step synthesis of nanodevices based on PAMAM framework for targeted cancer therapy is described. Four water-soluble nanodevices (named fractions F1 to F4) were rightly separated by size discrimination, and characterized. From biological assays of cell growth inhibition percentage, the anticancer activity of Methotrexate (chemotherapeutic drug) as part of a nanodevice, generally increases over cancer cell lines and notably, in case of human lymphocytes, the cell growth inhibition percentage decreases drastically (more than 80%), thus, the nanodevices exhibited a favorable discrimination between healthy and diseased cells. From the characterization it can be conclude that the synthesized nanodevices provide a dual scenario of drug transportation: encapsulation and conjugation.