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基于去甲斑蝥素和氨基硫脲的抗肿瘤及抗癌活性,设计合成了新型化合物——去甲去氢斑蝥素缩氨基硫脲(DNCT),并采用荧光光谱法和紫外可见吸收光谱法研究了去甲去氢斑蝥素缩氨基硫脲与牛血清白蛋白(BSA)的相互作用。研究结果表明,DNCT对BSA的荧光猝灭机理为静态猝灭;在25、30、37℃下,DNCT与BSA的结合常数分别为1.43×10~5、6.56×10~4、3.68×10~4L/mol,结合位点数分别为1.09、1.02、0.97,结合距离为2.97 nm(25℃)。热力学研究发现,DNCT与BSA主要是通过疏水作用结合。同步荧光显示,DNCT对BSA构象有一定的影响。
Based on the antitumor and anticancer activity of norcantharidin and thiosemicarbazone, a novel compound, norepinephrine thiosemicarbazone (DNCT), was designed and synthesized, and its fluorescence and UV-Vis absorption spectra were studied The interaction of norcantharidin thiosemicarbazone with bovine serum albumin (BSA) was studied. The results showed that the fluorescence quenching mechanism of BSA by DNCT was static quenching. The binding constants of DNCT and BSA at 25,30 and 37 ℃ were 1.43 × 10 ~ 5,6.56 × 10 ~ 4 and 3.68 × 10 ~ 4L / mol. The number of binding sites was 1.09, 1.02 and 0.97, respectively, and the binding distance was 2.97 nm (25 ℃). Thermodynamic studies found that, DNCT and BSA mainly by hydrophobic interaction. Synchronous fluorescence showed that DNCT had some influence on BSA conformation.