抗癌光敏剂ZnPcSP在溶液中的存在状态及其对活性的影响  

Existence States and Activities of ZnPcSP as Photosensitizer Against Cancer in Solutions

作　　者：黄剑东[1] 刘尔生[1] 杨素苓[1] 薛金萍[1] 陈耐生[1] 黄金陵[1] 

机构地区：[1]福州大学化学系,功能材料研究所,福州350002

出　　处：《高等学校化学学报》2002年第12期2287-2291,共5页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金 (批准号 :2 98710 0 8);教育部骨干教师资助计划;福建省自然科学基金 (批准号 :C0 0 10 0 4)资助

摘　　要：研究了两亲性抗癌光敏剂磺基邻苯二甲酰亚胺甲基酞菁锌 ( Zn Pc SP)单体与聚集体的可见吸收光谱特征以及溶剂组成对其聚集平衡的影响 ,得到了 Zn Pc SP在一系列溶剂中的聚集平衡常数 .进而研究了存在状态对 Zn Pc SP的 S1 80 肿瘤抑瘤率的影响 .Zn Pc SP在生理盐水中主要以三聚体形式存在 ,而在 CEL溶液中 ,则主要以单体形式存在 ,后者对 S1 80的抑瘤率是前者的The sulfonated phthalimidomethyl phthalocyanine Zinc(ZnPcSP) is an amphiphilic photosensitizer against cancer. The characteristic absorption peak of monomer and aggregate of ZnPcSP were observed, and the effects of solution compositions on its aggregation were investigated. In 70% MeOH/H 2O, 70% EtOH/H 2O, 50% EtOH/H 2O, 70% i-PrOH/H 2O, 70% CH 2OHCHOHCH 3/H 2O, 50% DMSO/H 2O, 50% DMF/H 2O(volume fraction) and CEL solutions, ZnPcSP existed in the equilibrium between monomer and dimer, the dimerization constants were 1.314×10 5, 8.496×10 4, 9.753×10 4, 5.583×10 4, 3.809×10 5, 4.430×10 3, 8.679×10 3 mol/L, respectively. But trimerization of ZnPcSP took place in water and saline solution, and trimerization constants were 1.296×10 8 and 2.236×10 8 mol -2·L 2 respectively. Furthermore, the effect of existence states of ZnPcSP on the activities against S 180 carcinoma were estimated. The result showed that the inhibitory rate of ZnPcSP(3.1×10 -6 mol/L) in CEL solution mainly existing in the form of monomer was about 8 times higher than that of ZnPcSP in saline solution mainly existing in the form of trimer.

关 键 词：ZnPcSP 溶液 存在状态 两亲性酞菁 抗癌光敏剂 聚集态 电子吸收光谱 药物活性 药物设计 

分 类 号：R979.1[医药卫生—药品] R914.[医药卫生—药学]