Klein Couto Gabriela, Rodrigues João Carlos, Pacheco Bruna Silveira, Damé Simões Lucas, Paschoal Júlia Damé, Seixas Fabiana Kommling, Acunha Thiago V, Iglesias Bernardo Almeida, Collares Tiago
Molecular and Cellular Oncology Research Group, Cancer Biotechnology Laboratory, Technological Development Center, Federal University of Pelotas, Pelotas, Brazil.
Laboratory of Bioinorganic and Porphyrinoid Materials, Chemistry Department, Federal University of Santa Maria, Santa Maria, Brazil.
Photodiagnosis Photodyn Ther. 2020 Sep;31:101942. doi: 10.1016/j.pdpdt.2020.101942. Epub 2020 Aug 3.
Tetra-cationic porphyrins with peripheral Pt (II) -bipyridyl complexes demonstrated a potential as photosensitizers to be used in photodynamic therapy (PDT). First-line transition metals, such as zinc (II), copper (II) and nickel (II), can be incorporated into the porphyrin nucleus, making this molecule more selective and more effective for this therapy in combating to tumor cells, such as metastatic melanoma. We characterized these derivatives to verify the improvement in selectivity of platinum (II) 4-PtTPyP porphyrins. Receptors such as LDL and endothelin (ERT-B) were investigated, as well as the binding affinity of two antioxidants: catalase model enzymes and superoxide dismutase. Human serum albumin (SAH) HSA binding properties have been verified. In addition, we evaluated the antitumor action of such metalloporphyrins in an in vitro cell viability. Our results demonstrated that porphyrins have significant antitumor potential when exposed to white light conditions. The affinity for the LDL receptor was better when compared to platinum porphyrin 4-PtTPyP without addition of metals and the affinity for the endothelin receptor was higher than the control used in this study. Still, the interaction with the HSA showed the possibility of this connection taking photosensitizers to places of interest, such as the delivery of medicines.
具有外周Pt(II)-联吡啶配合物的四价阳离子卟啉显示出作为光动力疗法（PDT）中使用的光敏剂的潜力。一线过渡金属，如锌(II)、铜(II)和镍(II)，可以掺入卟啉核中，使该分子在对抗肿瘤细胞（如转移性黑色素瘤）方面对这种疗法更具选择性和有效性。我们对这些衍生物进行了表征，以验证铂(II) 4-PtTPyP卟啉选择性的提高。研究了诸如低密度脂蛋白（LDL）和内皮素（ERT-B）等受体，以及两种抗氧化剂的结合亲和力：过氧化氢酶模型酶和超氧化物歧化酶。验证了人血清白蛋白（SAH）HSA的结合特性。此外，我们在体外细胞活力实验中评估了此类金属卟啉的抗肿瘤作用。我们的结果表明，卟啉在白光条件下具有显著的抗肿瘤潜力。与未添加金属的铂卟啉4-PtTPyP相比，其对LDL受体的亲和力更好，对内皮素受体的亲和力高于本研究中使用的对照。此外，与HSA的相互作用表明这种连接有可能将光敏剂带到感兴趣的部位，如药物递送。
