Glucose-functionalized amino-OPEs as biocompatible photosensitizers in PDT.

Authors :: Deni E
Zamarrón A
Bonaccorsi P
Carmen Carreño M
Juarranz Á
Puntoriero F
Sciortino MT
Ribagorda M
Barattucci A
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2016 Mar 23; Vol. 111, pp. 58-71. Date of Electronic Publication: 2016 Jan 28.
Publication Year :: 2016
Abstract: Photodynamic therapy (PDT) is a minimally invasive procedure that can provide a selective eradication of neoplastic diseases by the combined effect of a photosensitizer, light and oxygen. New amino oligo(phenylene-ethynylene)s (OPEs), bearing hydrophilic glucoside terminations, have been prepared, characterized and tested as photosensitizers in PDT. The effectiveness of these compounds in combination with UVA light has been checked on two tumor cell lines (HEp-2 and HeLa cells, derived from a larynx carcinoma and a cervical carcinoma, respectively). The compounds triggered a mitotic blockage that led to the cell death, being the effect active up to 3 μm concentration. The photophysical properties of OPEs, such as high quantum yield, stability, singlet oxygen production, biocompatibility, easy cell-internalization and very good response even at low concentration, make them promising photosensitizers in the application of PDT.<br /> (Copyright © 2016 Elsevier Masson SAS. All rights reserved.)