Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2015-08-28 , DOI: 10.1016/j.bmcl.2015.08.072 Sizhe Zhu , Fengshou Wu , Kai Wang , Yunman Zheng , Zaoying Li , Xiulan Zhang , Wai-Kwok Wong
The cell-based studies of 5, 10, 15, 20-Tetrakis (4-amidinophenyl) porphyrin (Por1), its Zn complex (Por2) and amidinophenyl bisporphyrin (Por3) were carried out to examine their photocytotoxicity, cellular uptake and sub-cellular localization with human nasopharyngeal carcinoma cell (HK-1), using 5, 10, 15, 20-Tetrakis (N-methyl-4-pyridyl) porphyrin (H2TMPyP) as a reference. These porphyrins showed low dark-cytotoxicity and high photo-cytotoxicity against HK-1. The amphiphilic amidinophenyl bisporphyrin (Por3) displayed better cellular uptake than the single hydrophilic Por1, Por2 and H2TMPyP. As seen from the extent of overlapping of the fluorescence profiles, lysosomal localization of amidinophenylporphyrin Por1–Por3 and mito/lyso localization of the H2TMPyP occurred in the cells. The results suggest these porphyrins with amidine group could be used as potential agents in photodynamic therapy.
中文翻译:
potential基苯基卟啉作为潜在的光动力治疗剂的光细胞毒性,细胞吸收和亚细胞定位:体外细胞研究
进行了基于细胞的5、10、15、20-四(4- phy基苯基)卟啉(Por1),其锌配合物(Por2)和a基双联卟啉(Por3)的研究,以检查它们的光细胞毒性,细胞摄取和亚使用5、10、15、20-四(N-甲基-4-吡啶基)卟啉(H 2 TMPyP)作为参考,对人鼻咽癌细胞(HK-1)进行细胞定位。这些卟啉对HK-1显示出低的暗细胞毒性和高的光细胞毒性。两亲性a基苯基双卟啉(Por3)显示出比单个亲水性Por1,Por2和H 2更好的细胞摄取TMPyP。从荧光图谱的重叠程度可以看出,细胞中发生了mid基苯基卟啉Por1 - Por3的溶酶体定位和H 2 TMPyP的线粒体/溶酶定位。结果表明这些带有am基的卟啉可以作为光动力疗法的潜在药物。