Metallation of pentaphyrin with Lu(III) dramatically increases reactive-oxygen species production and cell phototoxicity |
| |
Authors: | Ballico Maurizio Rapozzi Valentina Xodo Luigi E Comuzzi Clara |
| |
Affiliation: | a Department of Chemical Science, University of Udine, Via del Cotonificio, 108, 33100 Udine, Italy b Department of Biomedical Science and Technology, University of Udine, P.le Kolbe, 4, 33100 Udine, Italy |
| |
Abstract: | Photodynamic therapy (PDT) is an emerging cancer treatment modality based on the excitation of a nontoxic photosensitizer with harmless visible light to produce reactive-oxygen species (ROS) that induce apoptosis and/or necrosis in cancer cells. As the efficacy of this therapy strongly depends of the nature of the photosensitizer, there is a great interest to develop new photoactive molecules. Here we report for the first time the synthesis, characterization and bioactivity of metal complexes between the non-aromatic expanded porphyrin, namely 20-[[4′-(Trimethylsilyl)ethoxycarbonyl]phenyl-2,13-dimethyl-3,12-diethyl-[24] iso-pentaphyrin (PCRed) and Zn(II) [Zn(II)-PCRed] or Lu(III) [Lu(III)-PCRed]. The complexation of these two diamagnetic heavy metal ions to PCRed improved the properties of the free photosensitizer as a PDT drug. We discovered that the 1:1 complex between PCRed and Lu(III) significantly increases the cellular uptake, ROS production and antiproliferative capacity in four cancer cell lines. Our study shows that metal complexation is a useful strategy to potentiate iso-pentaphyrin as a PDT drug. |
| |
Keywords: | Pentaphyrin Lu(III) PDT ROS Cell proliferation |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|