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Molecules 2011, 16 1390 Bel-7402 cells, signifying that there was a selective uptake of TαPcZn in Bel-7402 cells and TαPcZn-PDT would be expected to directly damage DNA, and that TαPcZn-PDT significantly resulted in the proliferation inhibition, apoptosis induction, S cell cycle arrest, and down-regulation of Bcl-2 and Fas. Taken together, we conclude that TαPcZn-PDT inhibits the proliferation of Bel-7402 cells by triggering apoptosis and arresting the cell cycle. Keywords: tetra-α-(4-carboxyphenoxy) phthalocyanine zinc; photodynamic therapy; human hepatoma Bel-7402 cells; proliferation; apoptosis; cell cycle 1. Introduction Hepatocellular carcinoma is one of the most common malignant tumors in the world. Currently, the traditional therapies of surgery, chemotherapy and radiation therapy play an important role in the systemic treatment of hepatocellular carcinoma. However, the treatment outcome is generally poor. Thus, it is very important to find an effective alternative treatment for hepatocellular carcinoma. Photodynamic therapy (PDT) is a novel and promising antitumor treatment in which photosensitizing drugs that are excited with an appropriate wavelength of light significantly result in photochemical destruction of tumors by yielding reactive oxygen species (ROS), such as singlet oxygen and free radicals [1-3]. Compared with traditional therapies, the outstanding advantage of PDT is that it destroys tumor through selective uptake of photosensitisers and precise application of the light with modern fiber-optic systems, and does not harm the normal surrounding tissues seriously. Photosensitisers play a key role in PDT. At present，only a few porphyrin photosensitisers (Porfimer sodium, Talaporfin, Temoporfin, Verteporfin) are approved for the treatment of cancer in humans. Although these photosensitisers have demonstrated a wider spectrum of antitumor effects, they have various deficiencies that spur the development of better photosensitiser candidates [4,5]. As a result of the desirable electronic absorption and photophysical properties, phthalocyanines, containing a planar macrocycle with an 18 π-electron system, are one of the most potential photosensitiser candidates [6,7]. Furthermore, inasmuch as hydrophilic group redounds to the transport of drug in the body and lipophilic group conduces to the uptake of drug in cancer cells, phthalocyanines with hydrophilic/lipophilic structure may become promising candidates for selective photosensitisers. Recently, accumulated evidences have demonstrated highly selective growth inhibitory effects of hydrophilic/lipophilic phthalocyanines-mediated PDT in a variety of cancer cells [8-10]. However, the effect of new hydrophilic/lipophilic tetra-α-(4-carboxyphenoxy) phthalocyanine zinc (TαPcZn, Figure 1)-mediated PDT (TαPcZn-PDT) on human hepatocellular carcinoma Bel-7402 cells and underlying mechanisms have not been clarified. Apoptosis or programmed cell death is a form of cell death in which a programmed sequence of events leads to the elimination of cells without releasing harmful substances into the surrounding area. Apoptosis plays a crucial role in developing and maintaining health by eliminating old cells, unnecessary cells, and unhealthy cells [11,12]. Nowadays, a number of studies have shown that apoptosis is one key pathways in PDT process [13,14].PDF Image | Zinc-Mediated Photodynamic Therapy Inhibits the Proliferation
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