Photocytotoxicity, cellular uptake and subcellular localization of amidinophenylporphyrins as potential photodynamic therapeutic agents: An in vitro cell study

Sizhe Zhu, Fengshou Wu, Kai Wang*, Yunman Zheng, Zaoying Li, Xiulan Zhang, Rick W K WONG

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

23 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)4513-4517
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number20
DOIs
Publication statusPublished - 15 Oct 2015

Scopus Subject Areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

User-Defined Keywords

  • Cellular uptake
  • Localization
  • PDT
  • Porphyrin

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