Previously most of the applications of targeting components have been based on the enhanced permeability and retention effect achieved using folic acid, which consider the side effects of the targeting components to some extent. Herein, we report a new strategy to decorate the surface of MOFs using a pemetrexed (MTA) targeting molecule, affording a new drug delivery system of ALA@UIO-66-NH-FAM/MTA (ALA = 5-amino-levulinic acid and FAM = 5-carboxyfluorescein). The confocal microscopy and flow cytometry results showed that ALA@UIO-66-NH-FAM/MTA presented a better targeting effect compared to ALA@UIO-66-NH-FAM/FA (FA = folic acid) and indicated a gradually increasing tendency of the targeting effect with the increasing expression of folate receptors on the tumor cell cytomembrane. Furthermore, the cytotoxicity experiment indicates that the combination of chemotherapy and photodynamic therapy is a more effective therapy model than single chemotherapy and photodynamic therapy. This work demonstrates the first attempt at folic acid antagonist (MTA) modification for NMOFs, providing a new concept for the design of MOFs with folate receptor targeting capacity for clinical applications.

中文翻译：

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多功能和多功能的金属有机骨架纳米复合物，用于化学光动力疗法。

以前，靶向成分的大多数应用都是基于使用叶酸实现的增强的渗透性和保留效果，而叶酸在某种程度上考虑了靶向成分的副作用。在此，我们报告了一种新的策略，该方法使用培美曲塞（MTA）靶向分子修饰MOF表面，从而提供了ALA @ UIO-66-NH-FAM / MTA（ALA = 5-氨基乙酰丙酸和FAM = 5-羧基荧光素）。共聚焦显微镜和流式细胞术结果表明，与ALA @ UIO-66-NH-FAM / FA（FA =叶酸）相比，ALA @ UIO-66-NH-FAM / MTA的靶向效果更好叶酸受体在肿瘤细胞细胞膜上表达增加的靶向作用。此外，细胞毒性实验表明，化学疗法和光动力疗法相结合比单化学疗法和光动力疗法更有效。这项工作证明了对NMOF进行叶酸拮抗剂（MTA）修饰的首次尝试，为具有叶酸受体靶向能力的MOF设计提供了新的概念，可用于临床应用。