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在生理酸度(pH=7.4)下,采用紫外及荧光等分子光谱法研究了自制的双(β-二酮)Ti(Ⅳ)新型抗肿瘤前药与DNA之间的相互作用,考察了前药和溴化乙锭与鱼精DNA结合的竞争性.研究结果表明:DNA通过静态猝灭作用机制猝灭前药的荧光,并测得其在298K和308K时的猝灭常数(Kq)分别为8.590 3×1011和7.192 2×1011 L·mol-1·s-1,结合常数(Kd)分别为5.583 9×104和4.798 1×104 L·mol-1,结合位点数(n)为1.16和0.97;DNA的存在使前药的紫外吸收光谱发生减色效应且吸收波长产生红移;前药分子可插入DNA中置换出于DNA结合的溴化乙锭.这些结果说明前药分子以嵌插方式与DNA进行结合.
Under physiological acidity (pH = 7.4), the interaction between the novel bis (β-diketone) Ti (Ⅳ) antitumor prodrug and DNA was studied by UV and fluorescence spectroscopy. The effects of prodrug And the binding of ethidium bromide to fish sperm DNA.The results show that DNA quenches the fluorescence of the prodrug through static quenching mechanism and the quenching constants (Kq) of the prodrug at 298K and 308K are respectively 8.590 3 × 1011 and 7.192 2 × 1011 L · mol-1 · s-1 respectively. The binding constants (Kd) were 5.583 9 × 104 and 4.798 1 × 104 L · mol-1, respectively. The number of binding sites (n) 0.97; the presence of DNA discards the prodrug UV absorption spectrum and red shifts the absorption wavelength; the prodrug molecule can be inserted into the DNA to displace the DNA-bound ethidium bromide.These results indicate that the prodrug molecule is inserted Way and DNA combination.