轴向核苷修饰硅酞菁与白蛋白非共价复合物的制备与光动力活性  

Non-Covalent Albumin Conjugates of Silicon(Ⅳ)Phthalocyanines Axially Substituted with Nucleoside:Preparation and in vitro Photodynamic Activities

作　　者：杨晓梅[1] 郑碧远[1] 蔡悦[1] 林爱兰[1] 沈小敏[1] 张汉辉[1] 黄剑东[1] 

机构地区：[1]福州大学化学化工学院,福建福州350108

出　　处：《光谱学与光谱分析》2015年第2期457-461,共5页Spectroscopy and Spectral Analysis

基　　金：国家自然科学基金项目(21172037);国家大学生创新创业训练计划项目(20121038613);国家理科基地人才基金项目(J2012-028)资助

摘　　要：通过荧光光谱法研究了5种轴向核苷（胞苷、氮杂胞苷、甲基胞苷、尿苷和甲基尿苷）衍生物修饰硅酞菁与牛血清白蛋白（BSA）的相互作用,结果表明,它们与BSA存在较强的相互作用,结合常数在（4.90~83.18）×105 mol-1·L之间。因此,进一步制备了二[5’-（2’,3’-O-异丙基）-胞苷氧基]硅酞菁（SiPc1）与BSA的非共价复合物（SiPc1-BSA）,复合物中两者的摩尔比为1∶1。SiPc1-BSA与SiPc1在可见区的吸收光谱没有明显区别,两者的Q带最大吸收带均位于686nm附近,且吸收强度没有明显区别,这说明SiPc1结合到白蛋白后,其光谱性质没有受到明显改变。光动力抗癌活性测试表明,SiPc1-BSA具有较高的光动力抗癌活性,对人肝癌细胞HepG2的IC50值为3.0×10-7 mol·L-1,且SiPc1-BSA的光动力活性高于SiPc1（PBS药剂形式,IC50值为7.0×10-7 mol·L-1）,这主要可归因于SiPc1-BSA具有更高癌细胞摄取率。The interactions of bovine serum albumin （BSA） with five novel silicon （IV） phthalocyanines（SiPcl-5） axially modi- fied by nucleosides （cytidine, 5-N-cytidine, methyl cytidine, uridine and methyl uridine） derivatives were studied by fluorescence spectroscopy. The results show that there are strong interactions between these silicon phthalocyanines and BSA with a binding constant of（4.90~83.18）× 105 mo1-1 · L. Therefore, the non-covalent BSA conjugate of bis（2＇,3＇-O-isopropyl-cytidine-oxy） phthalocyaninatosilicon（Ⅳ） （SiPcl） was further been prepared. The molar ratio of phthalocyanine to albumin was found to be 1 ： 1 for the obtained SiPcl-BSA conjugate. The absorption spectra of SiPel and SiPcl-BSA in the visible region have no signifi- cant difference, both showing an Q-band maximum at about 686 nm. It indicates that the spectroscopic characteristics of SiPcl are not affected by binding to albumin. The SiPcl-BSA conjugate exhibits high photodynamic activity against human hepatoma cell line HepG2 with an IC50 value of 3.0× 10_7 mol · L-1. By comparsion, SiPcl-BSA has a higher photodynarnic activity than SiPcl （in PBS formation, ICs0 =7.0×10-7 mol · L-1 ）, which can be attributed to its higher cellular uptake.

关 键 词：硅酞菁 白蛋白 非共价复合物 光动力治疗 核苷 

分 类 号：O644[理学—物理化学]