羧基单取代酞菁锌的合成与光动力抗癌活性  

Synthesis and photodynamic anticancer activities of Zinc(Ⅱ) phthalocyanines mono-substituted with carboxyl moieties

作　　者：林斌 黄剑东 柯美荣 LIN Bin;HUANG Jian-dong;KE Mei-rong(Minjiang Teacher College,Fuzhou,Fujian 350008,China;College of Chemistry,Fuzhou University,Fuzhou,Fujian 350108,China)

机构地区：[1]闽江师范高等专科学校,福建福州350018 [2]福州大学化学学院,福建福州350108

出　　处：《宁德师范学院学报（自然科学版）》2020年第3期235-240,共6页Journal of Ningde Normal University(Natural Science)

基　　金：2014年国家自然科学基金项目(21301031).

摘　　要：合成了二个α位单取代羧基修饰酞菁锌配合物,即1-(4-羧基苯氧基)酞菁锌(1)和1-[4-(2-羧基乙基)苯氧基]酞菁锌(2),并研究了它们的光谱性质、光敏化能力和光动力抗癌活性.结果表明,配合物1和2均为优秀的单线态氧光敏剂,单线态氧量子产率(Φ△)可达到0.66~0.68.当以0.5%非离子表面活性剂Cremophor EL为助剂时,两个配合物在生理溶液中以有利于光动力治疗的单体形式存在,均显示了较高的离体光动力抗癌活性.由于具有更高的细胞摄取率,1-(4-羧基苯氧基)酞菁锌(1)显示了相对稍高的抗癌活性,其对人胃癌细胞MGC803的半数抑制浓度(IC50值)为0.11μmol·L-1.Two α-mono-substituted Zinc(Ⅱ) phthalocyanines(ZnPcs) modified with carboxyl moieties,namely 1-(4-carboxyl phenoxyl) Zinc(Ⅱ) phthalocyanine(1) and 1-[4-(2-carboxyl ethyl) phenoxyl] Zinc(Ⅱ)phthalocyanine(2) have been synthesized. Their spectral properties, photosensitizing activities, and photodynamic anticancer activities have also been investigated.The results indicate that both 1 and 2 are excellent singlet oxygen generators,with the quantum yields (Φ△) up to 0.66-0.68.When formulated with non-ionic surfactant Cremophor EL,both compounds are in the form of monomer,which is favorable for photodynamic therapy,and exhibit high in vitro photodynamic anticancer activities.Due to the higher cellular uptake, ZnPc 1 show slightly higher anticancer activity against human gastric carcinoma MGC803 cells, with an IC50 value of 0.11 μmol·L-1.

关 键 词：酞菁锌 合成 单线态氧 光动力抗癌活性 

分 类 号：O644[理学—物理化学]