Water-soluble metal naphthalocyanines--near-IR photosensitizers: cellular uptake, toxicity and photosensitizing properties in NHIK 3025 human cancer cells.
Metal naphthalocyanine complexes (MNCSs) absorb light in the near-IR spectral region (760 nm) where tissue penetration is optimal and they have been proposed as agents for photodynamic therapy (PDT). Sulphonated derivatives of tris-(2,3-naphthalocyanato) bis-chloroaluminium(III) and zinc(II) with various degrees of sulphonation were prepared. Cellular uptake, aggregation in cellular environments, cytotoxicity and photosensitizing properties were studied. Three of the four dyes studied were taken up by cells to a satisfactory degree and were not cytotoxic at the concentration used (10 micrograms ml-1). The least sulphonated sample of zinc naphthalocyanine produced some phototoxic effects (LD50 = 1.12 J cm-2). All the other samples of sulphonated naphthalocyanine were found to be aggregated inside the NHIK 3025 cells, preventing any significant PDT effect.
Yates
N C
NC
Department of Biophysics, Norwegian Radium Hospital, Oslo.
Moan
J
J
Western
A
A
D001693:Biological Transport, Active; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D004396:Coloring Agents; D006801:Humans; D007259:Infrared Rays; D009282:Naphthalenesulfonates / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D009942:Organometallic Compounds / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D010777:Photochemistry; D011838:Radiation-Sensitizing Agents / Q000493:pharmacokinetics / Q000633:toxicity; D012995:Solubility; D013055:Spectrophotometry, Infrared; D014407:Tumor Cells, Cultured / Q000187:drug effects* / Q000378:metabolism / Q000528:radiation effects; D014867:Water
D004396:Coloring Agents; D009282:Naphthalenesulfonates; D009942:Organometallic Compounds; D011838:Radiation-Sensitizing Agents; D014867:Water