水溶性卟啉及其系列金属化合物的合成、抗癌活性及其作用机制研究

Synthesis, Anticancer Activity and Mechanism of Water-soluble Porphyrin and Metalloporphyins

合成了水溶性四 -[( 4-三甲铵基 )苯基 ]卟啉 TAPP及其金属卟啉化合物 MTAPP,其中 M=Zn( ) ,Cu( ) ,Fe( ) ,Co ( ) ,Ni ( ) ,Mn( ) .通过元素分析、紫外 -可见光谱确定了化合物的组成和结构 .以紫外 -可见光谱、荧光光谱及粘度法等手段研究了卟啉化合物 TAPP和金属卟啉化合物 Zn TAPP与小牛胸腺 DNA的相互作用 ,结果表明 ,TAPP,Zn TAPP与 DNA相互作用使紫外 -可见光谱发生了 8～ 1 2 nm的红移 ,并出现了明显的减色效应 .荧光光谱强度明显增大 ,吸收峰位发生变化 .以艾氏腹水癌 ( Ac)和肝癌( Hept)细胞为靶细胞 ,采用 MTT染色法评价了化合物的抗癌活性 。

A water soluble porphyrin tetrakis[4 (trimethylammoniumly)phenyl]porpyrin (TAPP) and its metalloporphyrin derivatives MTAPP with M = Zn(Ⅱ), Cu(Ⅱ), Fe(Ⅲ), Co(Ⅲ), Ni (Ⅱ), Mn(Ⅲ) , containing various functional groups within the porphyrin have been synthesized and characterized by elemental analysis, and UV Vis spectra. Binding of TAPP and Zn TAPP with calf thymus DNA was investigated by absorption spectra, fluorescence spectra and viscosity measurements. Addition of CT DNA resulted in obvious hypochromism and bathochromic of 12 nm in absorption spectra, and an enhancement in fluorescence spectra were also observed. The anticancer activities of these complexes were also tested by MTT on two mice tumor cells of Ac and Hept, the results indicated that Co(Ⅲ) TAPP showed a high inhibitory action and high anticancer activity in cell.