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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >An integrin-targeting glutathione-activated zinc(II) phthalocyanine for dual targeted photodynamic therapy
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An integrin-targeting glutathione-activated zinc(II) phthalocyanine for dual targeted photodynamic therapy

机译：一种整合素靶向谷胱甘肽活化的锌（II）酞菁用于双靶向光动力疗法

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摘要

A zinc(II) phthalocyanine substituted with three 2,4-dinitrobenzenesulfonate (DNBS) groups and a cyclic arginine-glycine-aspartic acid (cRGDfK) moiety was prepared and characterized. With three strongly electron-withdrawing DNBS groups, this compound was fully quenched in terms of fluorescence emission and singlet oxygen generation in N,N-dimethylformamide and phosphate buffered saline due to the strong photoinduced electron transfer effect. In the presence of glutathione (GSH), which is the most abundant intracellular thiol particularly in tumor cells, the DNBS moieties were cleaved, thereby restoring these photoactivities and making the conjugate as a GSH-activated photosensitizer. Being a well-known integrin antagonist, the cyclic RGD peptide sequence could enhance the localization of the conjugate in integrin-upregulated tumor cells. As shown by confocal laser scanning microscopy and flow cytometry, the intracellular fluorescence intensity of the conjugate was significantly higher in the integrin-positive A549 and MDA-MB-231 cells than in the integrin-negative MCF-7 and HEK293 cells. The photocytotoxicity of the conjugate against MDA-MB-231 cells was also higher than that toward MCF-7 cells. The results suggest that this dual-functional photosensitizer is a promising candidate for targeted photodynamic therapy. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：制备用三种2,4-二硝基苯磺酸盐（DNBS）基团和环状精氨酸 - 甘氨酸 - 天冬氨酸（CRGDFK）部分取代的锌（II）酞菁。由于强烈的光态电子转移效果，在N，N-二甲基甲酰胺和磷酸盐缓冲盐水中的荧光发射和单线氧产生方面，该化合物完全淬火该化合物。在谷胱甘肽（GSH）的存在下，其是细胞内硫醇特别丰富的细胞内硫醇，DNBS部分被切割，从而恢复这些光活性并使缀合物作为GSH活化的光敏剂制备。作为众所周知的整联素拮抗剂，环状RGD肽序列可以增强整合素上调肿瘤细胞中缀合物的定位。如通过共聚焦激光扫描显微镜和流式细胞术所示，整合素阳性A549和MDA-MB-231细胞中缀合物的细胞内荧光强度显着高于整联蛋白阴性MCF-7和HEK293细胞中。缀合物对MDA-MB-231细胞的光致毒性也高于MCF-7细胞的光致毒性。结果表明，这种双官能光敏剂是有针对性的光动力治疗的有希望的候选者。 （c）2019年Elsevier Masson SAS。版权所有。

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