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论文类型： 期刊论文

发表时间： 2017-12-01

发表刊物： DYES AND PIGMENTS

收录刊物： Scopus、SCIE、EI

卷号： 147

页面范围： 476-483

ISSN号： 0143-7208

关键字： Chrysophanol; Proton-activatable; Photosensitiser; Lysosomes; Anthraquinone dye

摘要： Exploiting the tumor microenvironment provides a new strategy for cancer treatment. In order to develop the microenvironment-selective photosensitiser, we rationally designed a proton-activatable aminated-chrysophanol derivative-compound 3, which combines fluorescence and reactive oxygen species regulated by the tumor acidic microenvironment for the first time. Furthermore, two PET tertiary amine substituents introduced by compound 3 enhance the cellular uptake, prolong the wavelength of the absorption, and increase the phototoxicity. Not only can compound 3 distinguish the cancer cells from normal cells but also the tumor from the normal tissue by the higher fluorescence intensity in cancer cells and tissues. Additionally, lysosome destruction test proves cell necrosis in lysosomal related pathway. We believe that the proton-activatable photosensitiser modulated by tumor acidic microenvironment offers a good chance for the cancer treatment in clinic. (C) 2017 Elsevier Ltd. All rights reserved.