Synthesis,spectroscopic studies and biological evaluation of acridine derivatives: The role of aggregation on the photodynamic efficiency |
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| Authors: | Carles Felip-León Olga Martínez-Arroyo Santiago Díaz-Oltra Juan F Miravet Nadezda Apostolova Francisco Galindo |
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| Institution: | 1. Universitat Jaume I, Departamento de Química Inorgánica y Orgánica, Avda. Sos Baynat s/n, 12071 Castellón, Spain;2. Universitat de València, Departamento de Farmacología, Avda. Blasco Ibañez n.15-17, 46010 Valencia, Spain;3. Universitat Jaume I, Departamento de Educación, Avda. Sos Baynat s/n, 12071 Castellón, Spain |
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| Abstract: | Two new photoactive compounds (1 and 2) derived from the 9-amidoacridine chromophore have been synthesized and fully characterized. Their abilities to produce singlet oxygen upon irradiation have been compared. The synthesized compounds show very different self-aggregating properties since only 1 present a strong tendency to aggregate in water. Biological assays were conducted with two cell types: hepatoma cells (Hep3B) and human umbilical vein endothelial cells (HUVEC). Photodynamic therapy (PDT) studies carried out with Hep3B cells showed that non-aggregating compound 2 showed photoxicity, ascribed to the production of singlet oxygen, being aggregating compound 1 photochemically inactive. On the other hand suspensions of 1, characterized as nano-sized aggregates, have notable antiproliferative activity towards this cell line in the dark. |
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| Keywords: | Self-aggregation Organic nanoparticles 9-Amidoacridine Photodynamic therapy Singlet oxygen |
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