核酸与抗癌药物的作用和广义荧光猝灭方程

Interactions of nucleic acid with anticancer drugs and generalized fluorescence quenching equation

通过荧光法在不同温度下研究了2种抗癌新药:吡柔比星和表柔比星与小牛胸腺DNA的作用,分别应用荧光猝灭和荧光加强理论公式计算了它们的结合常数等,进而分别计算了它们的热力学函数.首先,热力学研究结果表明核酸与药物作用属于氢键和/或Van der Waals力;其次,即使是核酸类生物大分子其与药物的作用,荧光猝灭和荧光加强公式的计算结果仍符合等效性规律;第三,本文对这些猝灭图、双倒数图、生成常数、和热力学数据的差异进行了综合分析比较,结果表明,基于荧光加强理论公式(4)获得的图谱和数值显示更为合理.因而我们建议,即使在研究受体-底物的荧光猝灭反应时,采用荧光加强理论公式(4)可以获得更符合实际的结果.结合以前的类似结果,我们指出:对于任何生物大分子和活性小分子(含金属离子)之间由给体-受体作用所导致的荧光猝灭和荧光加强效应,均可应用我们导出的荧光加强理论公式(4)进行处理,因此我们定名其为广义的荧光猝灭方程.

Use fluorescence to research the reactions of calf thymus DNA at different temperatures, with two types of anti-cancer drugs： pirarubicin and epirubicin, respectively use fluorescence quench- ing and fluorescence enhancement theoretical formula to calculate the binding constants, and then cal- culate the thermodynamic functions. At first, the thermodynamics findings show that the force be- tween nucleic acid and drugs is belonging to hydrogen bond and/or Van der Waals force; Second, even at the case of nucleic acid biopolymers and the drugs, the results of fluorescence quenching and fluo- rescence enhancement formula are still in line with the equivalent of law; Third, the paper comprehen- sively analyzed and compared the differences of the quenching charts, double reciprocal plots, binding constants and thermodynamic data, and the results shows that： based on the fluorescence enhance- ment formula（4）, the patterns and values obtained are more rational, and therefore we recommend that even for the receptor-substrate fluorescence quenching reaction study, the fluorescence enhance- ment formula（4） can lead to more realistic results. Combined with previous similar results, we de- fine： for fluorescence quenching and enhancement effects induced by donor-acceptor action between all biological macromolecules and small molecules （or metal ions）, it can apply with the fluorescence en- hancement formula （4）, so we define this type as the generalized fluorescence quenching equation.