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Preparation and sonodynamic activities of water-soluble tetra-alpha-(3-carboxyphenoxyl) zinc(II) phthalocyanine and its bovine serum albumin conjugate

机译:水溶性四-α-(3-羧基苯氧基)锌(II)酞菁及其牛血清白蛋白结合物的制备及声动力学活性

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Sonodynamic therapy (SDT) is a new approach for cancer treatment, involving the synergistic effect of ultrasound and certain chemical compounds termed as sonosensitizers. A water-soluble phthalocyanine, namely tetra-alpha-(3-carboxyphenoxyl) zinc(II) phthalocyanine (ZnPcC4), has been prepared and characterized. The interactions between ZnPcC4 and bovine serum albumin (BSA) were also investigated by absorption and fluorescence spectroscopy. It was found that there were strong interactions between ZnPcC4 and BSA with a binding constant of 6.83 x 10(7) M-1. A non-covalent BSA conjugate of ZnPcC4 (ZnPcC4-BSA) was prepared. Both ZnPcC4 and ZnPcC4-BSA exhibited efficient sonodynamic activities against HepG2 human hepatocarcinoma cells. Compared with ZnPcC4, conjugate ZnPcC4-BSA showed a higher sonodynamic activity with an IC50 value of 7.5 mu M. Upon illumination with ultrasound, ZnPcC4-BSA can induce an increase of intracellular reactive oxygen species (ROS) level, resulting in cellular apoptosis. The results suggest that the albumin conjugates of zinc(II) phthalocyanines functionalized with carboxyls can serve as promising sonosensitizers for sonodynamic therapy. (C) 2014 Elsevier B.V. All rights reserved.
机译:声动力疗法(SDT)是一种用于癌症治疗的新方法,涉及超声和某些称为声敏剂的化合物的协同作用。已经制备并表征了水溶性酞菁,即四-α-(3-羧基苯氧基)锌(II)酞菁(ZnPcC4)。 ZnPcC4和牛血清白蛋白(BSA)之间的相互作用也通过吸收和荧光光谱进行了研究。发现在ZnPcC4和BSA之间有很强的相互作用,结合常数为6.83 x 10(7)M-1。制备了ZnPcC4的非共价BSA缀合物(ZnPcC4-BSA)。 ZnPcC4和ZnPcC4-BSA均表现出针对HepG2人肝癌细胞的有效声动力学活性。与ZnPcC4相比,共轭ZnPcC4-BSA具有更高的声波动力学活性,IC50值为7.5μM。在超声照射下,ZnPcC4-BSA可以诱导细胞内活性氧(ROS)水平升高,从而导致细胞凋亡。结果表明,用羧基官能化的锌(II)酞菁锌清蛋白缀合物可以用作声动力学治疗的有希望的声敏剂。 (C)2014 Elsevier B.V.保留所有权利。

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