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

Ligang Yu; Qiong Wang; Ka-Wing Yeung; Wing-Ping Fong; Pui-Chi Lo

doi:10.1002/asia.201800852

Author(s)

Ligang Yu
Qiong Wang
Ka-Wing Yeung
Wing-Ping Fong
Pui-Chi Lo

Related Research Unit(s)

Department of Biomedical Sciences

Detail(s)

Original language	English
Pages (from-to)	3509-3517
Journal / Publication	Chemistry - An Asian Journal
Volume	13
Issue number	22
Online published	28 Jun 2018
Publication status	Published - 16 Nov 2018

Link(s)

DOI	DOI https://doi.org/10.1002/asia.201800852 Final Published version
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Link to Scopus	https://www.scopus.com/record/display.uri?eid=2-s2.0-85052389401&origin=recordpage
Permanent Link	https://scholars.cityu.edu.hk/en/publications/publication(22e40a61-dd06-4a24-b2ec-ebdbbab8b67d).html

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 IC₅₀ value down to 0.1 μm on HepG2 cells. Moreover, it can localize in the endoplasmic reticulum (ER), causing ER stress after light irradiation.