脱氢枞基苯甲酰腙衍生物与DNA作用及抗癌活性研究

DNA Binding and Anticancer Properties of Dehydroabietyl Benzoylhydrazone Derivatives

以脱氢枞酸为原料,合成了脱氢枞基-2-羟基苯甲酰腙（4）和脱氢枞基-2-羟基-5-溴苯甲酰腙（6）,并用IR、元素分析、1H NMR和MS进行了表征。运用黏度分析、紫外吸收光谱和荧光光谱等方法研究了鲑鱼精DNA与4和6的相互作用,结果表明,4和6是以插入模式与DNA发生作用,且4的结合能力强于6。采用MTT法探究该类化合物对人体癌细胞的抑制作用,结果表明：在浓度25和50μmol/L下,4和6对4种肿瘤细胞He La,MCF-7,HL-60和Hep G-2都表现出较高的抑制活性,抑制率为73.9%~92.3%,均接近或超过临床上使用的顺铂（抑制率为66.3%~92.7%）。

Dehydroabietyl-2-hydroxy benzoylhydrazone （ 4 ） and dehydroabietyl-2-hydroxy-5-bromo benzoylhydrazone （ 6 ） were synthesized from dehydroabietic acid and characterized by IR, 1H NMR, MS spectra and elemental analysis . Their interactions with Salmon sperm DNA were investigated by viscosity analysis, UV, and fluorescence spectrometry, etc. The experimental results showed that they were bound to DNA by intercalation and the binding ability of 4 is stronger than that of 6. The anticancer experiments by MTT method indicated that the compounds has high growth inhibitory activities on the selected cancer cells （HeLa, MCF-7, HL-60, and HepG-2） with the inhibitory rates of 73. 9% -92. 3% at the concentrations of 25 and 50μmol/L. Their anticancer activities were all close to or greater than that of Cisplatin （66. 3% -92. 7%）.