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Anti-Cancer Agents in Medicinal Chemistry


ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Gallium Phthalocyanine Photosensitizers: Carboxylation Enhances the Cellular Uptake and Improves the Photodynamic Therapy of Cancers

Author(s): Jin F. Zhao, Jing Wang, Ji-Yao Chen, Wadzanai Chidawanykia, Tebello Nyokong, Kazuyuki Ishii and Nagao Kobayashi

Volume 12, Issue 6, 2012

Page: [604 - 610] Pages: 7

DOI: 10.2174/187152012800617740

Price: $65


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.

Keywords: Phthalocyanine, Cellular uptake, Singlet oxygen, Photodynamic therapy

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