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一种生物素化的内质网靶向的谷胱甘肽响应型锌(II)酞菁用于靶向光动力疗法。

A Biotinylated and Endoplasmic Reticulum-Targeted Glutathione-Responsive Zinc(II) Phthalocyanine for Targeted Photodynamic Therapy.

机构信息

Department of Biomedical Sciences, City University of Hong Kong, Tat Chee Avenue, Kowloon, Hong Kong.

School of Life Sciences, The Chinese University of Hong Kong, Shatin, N. T., Hong Kong.

出版信息

Chem Asian J. 2018 Nov 16;13(22):3509-3517. doi: 10.1002/asia.201800852. Epub 2018 Aug 13.

DOI:10.1002/asia.201800852
PMID:29956487
Abstract

A biotinylated glutathione (GSH)-responsive zinc(II) phthalocyanine has been prepared and characterized. With a 2,4-dinitrobenzenesulfonyl moiety, its fluorescence emission and singlet oxygen generation were silenced in its intact state. Upon exposure to high concentration of GSH, its photosensitizing properties were restored in phosphate buffered saline and inside tumor cells. It also showed preferential uptake on HepG2 human hepatocarcinoma cells (with higher biotin receptor expression) rather than Chinese hamster ovary (CHO) cells (with lower biotin receptor expression). Upon irradiation, it caused photocytotoxicity with an IC value down to 0.1 μm on HepG2 cells. Moreover, it can localize in the endoplasmic reticulum (ER), causing ER stress after light irradiation.

摘要

已制备并表征了一种生物素化谷胱甘肽(GSH)响应型锌(II)酞菁。带有 2,4-二硝基苯磺酰基部分,其荧光发射和单线态氧生成在完整状态下被沉默。当暴露于高浓度的 GSH 时,其光敏性质在磷酸盐缓冲液和肿瘤细胞内得到恢复。它还表现出对 HepG2 人肝癌细胞(具有更高的生物素受体表达)的优先摄取,而不是中国仓鼠卵巢(CHO)细胞(具有较低的生物素受体表达)。光照后,它在 HepG2 细胞上的 IC 值低至 0.1μm 时引起光细胞毒性。此外,它可以定位在内质网(ER)中,在光照射后引起 ER 应激。

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