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

发布时间：2018-03-23 08:13

本文选题：硅酞菁　切入点：白蛋白　出处：《光谱学与光谱分析》2015年02期 　论文类型：期刊论文

【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。
[Abstract]:The interaction of five derivatives of axonal nucleosides (cytidine, azacytidine, methyl cytidine, uridine and methyl uridine) modified with bovine serum albumin (BSA) was studied by fluorescence spectrometry. There is a strong interaction between them and BSA, and the binding constant is between 4.90 mol-1 / L and 83.18 脳 10 ~ 5 mol-1 / L. The non-covalent complex of bis [5- (5) -O- (isopropyl) -cytidyl] siphocyanine (SiPc1) and BSA was further prepared. The molar ratio of the two complexes is that the absorption spectra of 1:1.SiPc1-BSA and SiPc1 in the visible region are not significantly different. The maximum absorption bands of Q band are located near 686nm, and there is no significant difference in absorption intensity between them, which indicates that SiPc1 binds to albumin. The photodynamic anticancer activity test showed that SiPc1-BSA had high photodynamic anticancer activity. The IC50 value of HepG2 was 3.0 脳 10 ~ (-7) mol / L ~ (-1), and the photodynamic activity of SiPc1-BSA was higher than that of SiPc1(PBS (7.0 脳 10 ~ (-7) mol L ~ (-1)), which could be attributed to the higher uptake rate of SiPc1-BSA.
【作者单位】：福州大学化学化工学院;
【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
【分类号】：O657.3;R943

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