title: Gallium phthalocyanine photosensitizers: carboxylation enhances the cellular uptake and improves the photodynamic therapy of cancers.
abstract: The octacarboxyl gallium (GaPcC) and metal-free (H2PcC) phthalocyanines were prepared using the carboxyl as the peripheral substituent. The carboxylation improves the intracellular delivery of these two PcCs into KB and QGY cancer cells as compared to that of sulfonated aluminum phthalocyanines (AlPcS), a popularly used photosensitizer (PS). Moreover, GaPcC maintains high photoproduction of singlet oxygen. With a short incubation time of 3 hours, GaPcC accumulates sufficiently in both KB and QGY cells and improves photodynamic therapy (PDT) by effectively killing these cancer cells. AlPcS and H2PcC show much lower PDT effects under the same conditions, because AlPcS have a slow cellular uptake rate resulting in a low cellular amount and the ability of H2PcC to produce 1O2 is low. Carboxylation is a promising way to prepare water-soluble metal phthalocyanines (MPcCs) and facilitates the cellular uptake of MPcCs for PDT improvement.
authors.affiliation: State Key Laboratory of Surface Physics and Department of Physics, Fudan University, Shanghai 200433, PR China.
authors.forename: Jin F
authors.initials: JF
authors.lastname: Zhao
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.forename: Ji-Yao
authors.initials: JY
authors.lastname: Chen
authors.forename: Wadzanai
authors.initials: W
authors.lastname: Chidawanykia
authors.forename: Tebello
authors.initials: T
authors.lastname: Nyokong
authors.forename: Kazuyuki
authors.initials: K
authors.lastname: Ishii
authors.forename: Nagao
authors.initials: N
authors.lastname: Kobayashi
mesh_terms: D001692:Biological Transport; D002277:Carcinoma; D049109:Cell Proliferation / Q000187:drug effects / Q000528:radiation effects; D002470:Cell Survival / Q000187:drug effects / Q000528:radiation effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000494:pharmacology*; D005708:Gallium; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D007259:Infrared Rays; D054833:Isoindoles; D008113:Liver Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D008856:Microscopy, Fluorescence; D000077274:Nasopharyngeal Carcinoma; D009303:Nasopharyngeal Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010778:Photochemotherapy / Q000379:methods; D017319:Photosensitizing Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D026082:Singlet Oxygen / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D056831:Coordination Complexes; D007211:Indoles; D054833:Isoindoles; D017319:Photosensitizing Agents; D026082:Singlet Oxygen; D005708:Gallium; C013647:phthalocyanine