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The photodynamic activity of dimethyl 131-[2-(guanidinyl)ethylamino] chlorin e6 photosensitizers in A549 tumor

Gao, Y.-H.; Lovreković, V.; Kussayeva, Akmaral; Chen, D.-Y.; Margetić, Davor; Chen, Z.-L. (2019) The photodynamic activity of dimethyl 131-[2-(guanidinyl)ethylamino] chlorin e6 photosensitizers in A549 tumor. European Journal of Medicinal Chemistry, 177 . pp. 144-152. ISSN 0223-5234

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Effective photosensitizers are particularly important factor in clinical photodynamic therapy (PDT). However, there is scarcity of photosensitizers for simultaneous cancer photo-diagnosis and targeted PDT. Herein, two novel dimethyl 2-(guanidinyl)ethylamino chlorin e6 photosensitizers were synthesized and their efficacy in PDT in A549 tumor was investigated. It was showed that compounds 3 and 4 have a long absorption wavelength in the near infrared region and strong fluorescence emission with slow photo-bleaching rate and markedly strong ability of 1O2 generation. They exhibited lower cytotoxicity and higher photo-cytotoxicity in vitro compared to the known anticancer drug m-THPC in MTT assay in A549 lung cancer cell lines. Compound 4 exhibit better inhibition effect than compound 3 and the IC50 value of compound 4 was 0.197 μM/L under 2 J/cm2 laser irradiation, while compound 3 showed better anti-tumor effects compared to compound 4 in vivo. Intracellular ROS generation was found to be responsible for apoptotic cell death in DCFDA assay. Subcellular localization confirmed the damage site of compounds 3 and 4 in PDT. These findings suggest that the two novel photosensitizers might serve as potential photosensitizers for improved therapeutic efficiency of PDT.

Item Type: Article
Uncontrolled Keywords: chlorin e6 derivative; guanidine; photodynamic therapy; photosensitizers; reactive oxygen species; tumor
Subjects: NATURAL SCIENCES > Chemistry > Organic Chemistry
Divisions: Division of Organic Chemistry and Biochemistry
Project titleProject leaderProject codeProject type
Cikloadicijske strategije prema policikličkim gvanidinima-CycloGuDavor MargetićIP-2018-01-3298HRZZ
Depositing User: Davor Margetić
Date Deposited: 11 Dec 2020 08:30
DOI: 10.1016/j.ejmech.2019.05.050

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