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[嘧啶衍生物轴向修饰的硅酞菁的光谱性质、光动力抗癌活性及与白蛋白的相互作用]

[Spectral properties, photodynamic anticancer activity and the interaction with albumin of silicon phthalocyanine axially modified by pyrimidine derivatives].

作者信息

Shen Xiao-Min, Jiang Xiong-Jie, Zhu Yu-Jiao, Zhang Han-Hui, Huang Jian-Dong

机构信息

College of Chemistry and Chemical Engineering, Fuzhou University, Fuzhou 350108, China.

出版信息

Guang Pu Xue Yu Guang Pu Fen Xi. 2013 Aug;33(8):2148-52.

PMID:24159865
Abstract

Photophysical photochemical properties, in vitro photodynamic anticancer activity and interaction with albumin of a new axially modified silicon phthalocyanine, i. e. di (2-amino-6-trifluoromethyl-4-pyrimidinyloxy) silicon phthalocyanine (SiPcF), were studied in the present paper. The Q band maximum absorption of SiPcF located at 686 nm with the molar absorption coefficient of 2.3 x 10(5) mol(-1) * L * cm(-1). The fluorescence emission of SiPcF peaked at 694 nm with a fluorescence quantum yield of 0.46. Its singlet oxygen quantum yield produced by photosensitization is 0.38, suggesting that SiPcF is an effective 1O2 photosensitizer. There is strong interaction between SiPcF and bovine serum albumin (BSA). The binding constant is 4.33 x 10(5) mol X L(-1) and the number of binding sites is 1. In vitro experiments show that SiPcF had a high photodynamic anticancer activity against human hepatoma cells HepG2 with an IC50 value down to 5 x 10(-7) mol X L(-1).

摘要

本文研究了一种新型轴向修饰的硅酞菁,即二(2-氨基-6-三氟甲基-4-嘧啶氧基)硅酞菁(SiPcF)的光物理、光化学性质、体外光动力抗癌活性及其与白蛋白的相互作用。SiPcF的Q带最大吸收位于686nm,摩尔吸收系数为2.3×10⁵mol⁻¹·L·cm⁻¹。SiPcF的荧光发射峰位于694nm,荧光量子产率为0.46。其通过光敏化产生的单线态氧量子产率为0.38,表明SiPcF是一种有效的¹O₂光敏剂。SiPcF与牛血清白蛋白(BSA)之间存在强烈相互作用。结合常数为4.33×10⁵mol·L⁻¹,结合位点数为1。体外实验表明,SiPcF对人肝癌细胞HepG2具有高光动力抗癌活性,IC50值低至5×10⁻⁷mol·L⁻¹。

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