Release Time:2019-03-11  Hits:

Indexed by: Journal Article

Date of Publication: 2017-12-01

Journal: DYES AND PIGMENTS

Included Journals: EI、SCIE、Scopus

Volume: 147

Page Number: 476-483

ISSN: 0143-7208

Key Words: Chrysophanol; Proton-activatable; Photosensitiser; Lysosomes; Anthraquinone dye

Abstract: 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.