Fu N W, Guo R, Yan L X, Huang L, Xu H J
Cancer Institute, Chinese Academy of Medical Sciences, Beijing.
Zhongguo Yao Li Xue Bao. 1991 Sep;12(5):457-61.
Zinc sulfonated phthalocyanine (ZnSPc) 10 mg.kg-1 was injected iv into mice bearing S-180 and RA795 lung carcinoma, after 24 h tumor site were irradiated with red light. In mice bearing S-180, tumor regression rate was 31.8-43.5%, tumor growth inhibition rate was 57.4%. The highest concentration was in tumor tissue 24 h after injection of this dye, on d 5 it still retained relatively highest concentration. However, in most other tissues the dye was not detected at this time, disappearance of ZnSPc from plasma was rapid, it showed an open two compartment model, t1/2 alpha 135.8 min, t1/2 beta 70.1 h, Vd 1.92 x 10(-3) L. In blood, most ZnSPc was bound with plasma protein, the peak light absorption showed blue shift. ZnSPc 2.5 micrograms.ml-1 plus light, percent of DNA double strands greatly decreased, this indicated that DNA was one of target sites for ZnSPc photodynamic action.
将10毫克/千克的磺化锌酞菁(ZnSPc)静脉注射到荷S-180和RA795肺癌的小鼠体内,24小时后用红光照射肿瘤部位。在荷S-180的小鼠中,肿瘤消退率为31.8%-43.5%,肿瘤生长抑制率为57.4%。注射该染料后24小时肿瘤组织中浓度最高,第5天时仍保持相对较高浓度。然而,此时在大多数其他组织中未检测到该染料,ZnSPc从血浆中消失迅速,呈现开放二室模型,t1/2α为135.8分钟,t1/2β为70.1小时,分布容积为1.92×10⁻³升。在血液中,大多数ZnSPc与血浆蛋白结合,峰值光吸收呈现蓝移。2.5微克/毫升的ZnSPc加光处理后,DNA双链的比例大幅下降,这表明DNA是ZnSPc光动力作用的靶点之一。