TY - JOUR
T1 - Photocytotoxicity, cellular uptake and subcellular localization of amidinophenylporphyrins as potential photodynamic therapeutic agents
T2 - An in vitro cell study
AU - Zhu, Sizhe
AU - Wu, Fengshou
AU - Wang, Kai
AU - Zheng, Yunman
AU - Li, Zaoying
AU - Zhang, Xiulan
AU - WONG, Rick W K
N1 - Funding Information:
The authors are grateful for the financial support of the Wuhan Science and Technology Talent Training Program of Chenguang Project (Grant no. 2015070404010190 ), Key Project of Scientific Research Project of Hubei Provincial Department of Education (Grant no. D20141506 ) and Scientific Research Foundation of Wuhan Institute of Technology (Grant no. K201542 ).
PY - 2015/10/15
Y1 - 2015/10/15
N2 - 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.
AB - 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.
KW - Cellular uptake
KW - Localization
KW - PDT
KW - Porphyrin
UR - http://www.scopus.com/inward/record.url?scp=84942833319&partnerID=8YFLogxK
U2 - 10.1016/j.bmcl.2015.08.072
DO - 10.1016/j.bmcl.2015.08.072
M3 - Journal article
C2 - 26338364
AN - SCOPUS:84942833319
SN - 0960-894X
VL - 25
SP - 4513
EP - 4517
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 20
ER -