青蒿截疟组合物与牛血清白蛋白的相互作用

利用荧光光谱法研究青蒿截疟组合物(青蒿素、青蒿乙素、青蒿酸与东莨菪内酯质量比为1∶1∶1∶1的混合体系,AAAS)与牛血清白蛋白(BSA)的相互作用.结果表明,与青蒿素单独作用相比,AAAS对BSA的荧光猝灭作用增强,并以静态猝灭为主;计算了298,303和310 K下的结合常数、结合位点数和热力学参数,表明AAAS与BSA之间具有较强的静电引力,相互作用过程是一个熵增加的自发分子间作用过程.AAAS对BSA的猝灭常数和结合常数均增大.结果表明,AAAS显著增加了青蒿素与血清白蛋白的结合作用,此过程可能是AAAS增加青蒿素抗疟疗效的重要体内环节.

Interaction of Antimalarial Components Combination from Artemisia annua L. with Bovine Serum Albumin

The interaction of arteannuin, arteannuic acid and scopoletin on the binding of artemisinin with bovine serum albumin(BSA) was investgated by fluorescent spectrometry. BSA fluorescence quenching effect was strengthened after the interaction of BSA with antimalarial components combinationAAAS, m(artemisinin):m(arteannuin B):m(arteannuic acid):m(scopoletin)=1:1:1:1] from Artemisia annua L. compared to that of BSA with artemisinin alone, and the fluorescence quenching effect was staitc quenching. The binding constant, binding point numbers and thermodynamic parameters at three temperature levels, for example, 298, 303 and 310 K were calculated, and the results revealed that the binding of AAAS with BSA had strong electrostatic attraction and the process was a spontaneous molecular interaction procedure in which entropy was increased. Compared with artemisinin, the quenching constants and the binding constant of AAAS with BSA were also increased. These results confirmed that arteannuin, arteannuic acid and scopoletin could significantly increased the binding of artemisinin with BSA, and the interaction of AAAS with BSA might be a key factor that improved the antimalarial efficacy of artemisinin in vivo.