Université de Limoges, Laboratoire de Chimie des Substances Naturelles, Faculté des Sciences et Techniques, 123 Av. Albert Thomas, 87060 Limoges, France.
J Photochem Photobiol B. 2011 Jun 2;103(3):201-6. doi: 10.1016/j.jphotobiol.2011.03.005. Epub 2011 Mar 14.
Porphyrin-polyamine conjugates bearing two (cis or trans position) or four spermidine or spermine units were synthesized. We studied the photostability, the hydrophilic/lipophilic balance of porphyrin-polyamine derivatives and the production of singlet oxygen. All these compounds possess physicochemical features required for their use in PDT. Then, we investigated the photocytotoxic efficacy of these porphyrin-polyamine derivatives and the cell death pathway implicated. All compounds appear to be more efficient than Photofrin® to induce HaCat and MCF7 cell death, essentially by apoptosis. Collectively, these data show that porphyrin-polyamine conjugates could be promising phototherapeutic agents.
合成了带有两个(顺式或反式位置)或四个亚精胺或精胺单元的卟啉-多胺缀合物。我们研究了卟啉-多胺衍生物的光稳定性、亲水/亲脂平衡和单线态氧的产生。所有这些化合物都具有用于 PDT 的理化特性。然后,我们研究了这些卟啉-多胺衍生物的光细胞毒性作用及其涉及的细胞死亡途径。所有化合物似乎比 Photofrin®更有效地诱导 HaCat 和 MCF7 细胞死亡,主要通过细胞凋亡。总之,这些数据表明卟啉-多胺缀合物可能是有前途的光疗剂。