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首页> 外文期刊>RSC Advances >Synthesis and biological evaluation of an epidermal growth factor receptor-targeted peptide-conjugated phthalocyanine-based photosensitiser
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Synthesis and biological evaluation of an epidermal growth factor receptor-targeted peptide-conjugated phthalocyanine-based photosensitiser

机译：表皮生长因子受体靶向肽偶联的酞菁类光敏剂的合成与生物学评价

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摘要

A peptide-conjugated zinc( II ) phthalocyanine containing the epidermal growth factor receptor-targeted heptapeptide QRHKPRE has been prepared. The conjugate labelled as ZnPc-QRH* can selectively bind to the cell membrane of HT29 human colorectal adenocarcinoma cells in 10 min followed by internalisation upon prolonged incubation via receptor-mediated endocytosis, leading to localisation in lysosomes eventually. By manipulating the incubation time, the subcellular localisation of the conjugate can be varied and the cell-death pathways induced upon irradiation can also be altered. It has been found that photosensitisation initiated at the cell membrane and in the lysosomes would trigger cell death mainly through necrosis and apoptosis respectively. Intravenous administration of the conjugate into HT29 tumour-bearing nude mice resulted in higher accumulation in the tumour than in most major organs. The selective binding of this conjugate to tumour has also been demonstrated by comparing the results with those of the analogue with a scrambled peptide sequence (EPRQRHK). The overall results indicate that ZnPc-QRH* is a promising EGFR-targeted photosensitiser for photodynamic therapy.
机译：已经制备了包含表皮生长因子受体靶向的七肽QRHKPRE的肽缀合的锌（II）酞菁锌。标记为ZnPc-QRH *的缀合物可以在10分钟内选择性结合HT29人结肠直肠腺癌细胞的细胞膜，然后通过受体介导的内吞作用长时间孵育后内在化，最终导致溶酶体中的定位。通过控制孵育时间，可以改变缀合物的亚细胞定位，并且还可以改变照射后诱导的细胞死亡途径。已经发现，在细胞膜和溶酶体中引发的光敏作用将分别主要通过坏死和细胞凋亡触发细胞死亡。与大多数主要器官相比，将结合物静脉内给药于HT29荷瘤裸鼠中导致肿瘤中更高的蓄积。通过将结果与具有杂乱肽序列（EPRQRHK）的类似物的结果进行比较，也证明了该缀合物与肿瘤的选择性结合。总体结果表明，ZnPc-QRH *是一种有前途的针对EGFR的光动力疗法光敏剂。

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