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新型三唑-卟啉衍生物的合成、表征及对膀胱癌细胞的光动力活性。

Synthesis, Characterization and Photodynamic Activity against Bladder Cancer Cells of Novel Triazole-Porphyrin Derivatives.

机构信息

LAQV-REQUIMTE, Department of Chemistry, University of Aveiro, 3810-193 Aveiro, Portugal.

Coimbra Institute for Clinical and Biomedical Research (iCBR), Faculty of Medicine, University of Coimbra, 3000-548 Coimbra, Portugal.

出版信息

Molecules. 2020 Mar 31;25(7):1607. doi: 10.3390/molecules25071607.

DOI:10.3390/molecules25071607
PMID:32244514
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7180931/
Abstract

Novel triazole-porphyrin derivatives (TZ-PORs) were synthesized through the Heck reaction and then incorporated into polyvinylpyrrolidone (PVP) micelles. After verifying that this incorporation did not compromise the photophysical and chemical features of TZ-PORs as photosensitizers, the phototoxicity of the formulations towards cancer cells was screened. Biological studies show high photodynamic activity of all PVP-TZ-POR formulations against a bladder cancer cell line with a particular highlight to PVP-TZ-POR and that are able to significantly reduce HT-1376 cell viability, while they had no effect on control ARPE-19 cells.

摘要

新型三唑-卟啉衍生物（TZ-PORs）通过 Heck 反应合成，然后整合到聚乙烯吡咯烷酮（PVP）胶束中。在证实这种整合并不影响 TZ-PORs 作为光敏剂的光物理和化学特性后，对制剂对癌细胞的光毒性进行了筛选。生物学研究表明，所有 PVP-TZ-POR 制剂对膀胱癌细胞系均具有高的光动力活性，特别是 PVP-TZ-POR 和 ，它们能够显著降低 HT-1376 细胞活力，而对对照 ARPE-19 细胞没有影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/0d11e2791d61/molecules-25-01607-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/283bfdbc7efe/molecules-25-01607-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/f5ea940a5e3a/molecules-25-01607-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/fae248e3a78d/molecules-25-01607-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/d7f8ad10e46c/molecules-25-01607-sch004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/21c2e685be83/molecules-25-01607-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/efa8d6c39d85/molecules-25-01607-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/c19678bfa768/molecules-25-01607-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/4d4052a0d40f/molecules-25-01607-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/0d11e2791d61/molecules-25-01607-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/283bfdbc7efe/molecules-25-01607-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/f5ea940a5e3a/molecules-25-01607-sch002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/fae248e3a78d/molecules-25-01607-sch003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/d7f8ad10e46c/molecules-25-01607-sch004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/21c2e685be83/molecules-25-01607-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/efa8d6c39d85/molecules-25-01607-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/c19678bfa768/molecules-25-01607-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/4d4052a0d40f/molecules-25-01607-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0bc3/7180931/0d11e2791d61/molecules-25-01607-g005.jpg

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