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Cationic Versus Anionic Phthalocyanines for Photodynamic Therapy: What a Difference the Charge Makes.

Abstract：

:The literature reports on cationic and anionic phthalocyanines (Pcs) for photodynamic therapy suggest systematically significant differences in activity. In this work, ten different zinc(II) Pcs with carboxylate functions or quaternary nitrogens (hydrophilic anionic, hydrophilic cationic, amphiphilic anionic, and amphiphilic cationic) were investigated, with the aim of revealing reasons for such differences. In vitro assays on HeLa, MCF-7, and HCT-116 cells confirmed higher photoactivity for cationic Pcs (EC50 ∼ 3-50 nM) than for anionic Pcs (EC50 ∼ 0.3-10 μM), the latter being additionally significantly more active in serum-free medium. The environmental pH, binding to serum proteins, interaction with biomembranes, differences in subcellular localization, and relocalization after irradiation were found to be the main factors contributing to the generally lower photoactivity of anionic Pcs than that of the cationic derivatives. This result is not limited only to the presented derivatives and should be considered in the design of novel photosensitizers.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Kollar J,Machacek M,Halaskova M,Lenco J,Kucera R,Demuth J,Rohlickova M,Hasonova K,Miletin M,Novakova V,Zimcik P

doi

10.1021/acs.jmedchem.0c00481

subject

Has Abstract

pub_date

2020-07-23 00:00:00

pages

7616-7632

issue

14

eissn

0022-2623

issn

1520-4804

journal_volume

63

pub_type

杂志文章

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