The palliative treatment options for advanced hepatocellular carcinoma (HCC) are currently not satisfying. The use of photodynamic therapy (PDT) has gained much attention in the treatment of several cancers and has been approved as an alternative approach in treating different forms of cancers. We investigated for the first time the PDT effects of tetra-triethyleneoxysulfonyl zinc phthalocyanine (ZnPc) on HCC cells. Photoactivation of ZnPc loaded HCC cells resulted in a dose- and time- dependent growth inhibitory effect, the production of reactive oxygen species (ROS), induced cytotoxic effects and the induction of apoptosis in the investigated HCC cells (HepG2 and Huh-7). ZnPc-PDT inhibited the proliferation of HCC cells by up to 90% accompanied by a down-regulation of the activity and expression of the proliferation relevant mitogen-activated protein kinase (MAPK)-protein extracellular signal-regulated (ERK ½). Moreover, an up-regulation of proapoptotic BAX and a down-regulation of antiapoptotic B-cell lymphoma 2 (Bcl-2) expressions were observed with both proteins implicated in mitochondria-driven apoptosis. The investigation of the anti-tumor effect of ZnPc-PDT in vivo using the chicken chorioallantoic membrane assays (CAM) revealed a strong reduction in the size of HCC tumor plagues >80% after 4 days of PDT-treatment without affecting the survival of the developing embryo. The pronounced anti-proliferative and anti-tumor effects of ZnPc-PDT both in vitro and in vivo render ZnPc-PDT as a promising palliative treatment option for hepatocellular carcinoma.

目前对于晚期肝细胞癌（HCC）的姑息治疗选择并不令人满意。光动力疗法（PDT）的使用已在几种癌症的治疗中引起了广泛关注，并已被批准作为治疗不同形式癌症的替代方法。我们首次研究了四三亚乙基氧基磺酰基锌酞菁（ZnPc）对HCC细胞的PDT效应。负载ZnPc的HCC细胞的光活化导致剂量和时间依赖性生长抑制作用，活性氧物质（ROS）的产生，诱导的细胞毒性作用以及所研究的HCC细胞（HepG2和Huh-7）的凋亡诱导作用。ZnPc-PDT抑制HCC细胞的增殖达90％，并伴随着活性的下调以及与增殖相关的促分裂原活化蛋白激酶（MAPK）-蛋白细胞外信号调节（ERK½）的表达。此外，与线粒体驱动凋亡相关的两种蛋白均观察到凋亡前BAX的上调和抗凋亡B细胞淋巴瘤2（Bcl-2）的表达下调。ZnPc-PDT的抗肿瘤作用研究PDT治疗4天后，使用鸡绒囊尿囊膜测定（CAM）进行的体内实验显示，HCC肿瘤的大小大大减少了> 80％，而没有影响发育中的胚胎的存活。ZnPc-PDT在体外和体内的显着抗增殖和抗肿瘤作用使ZnPc-PDT成为肝细胞癌的有希望的姑息治疗选择。