雷公藤甲素与人血清白蛋白间的体外结合特性

The interaction between triptolide and human serum albumin in vitro

采用平衡透析法研究雷公藤甲素与人血清白蛋白的结合率,结果表明当雷公藤甲素的浓度分别为3.60,7.20和36.0μg/m L时,其与人血清白蛋白的结合率分别为（24.2±2.0）%,（18.4±0.4）%和（6.30±0.3）%.应用荧光淬灭法研究雷公藤甲素与人血清白蛋白间的相互作用机制,结果表明TP与HSA之间的结合为静态淬灭过程,在300,305和310 K温度下结合常数分别为1.3×10~4,7.8×10~3和3.8×10~3L/mol,主要作用力为范德华力.

In the present work,the binding rate of triptolide （ TP） with human serum albumin （ HSA） was studied by equilibrium dialysis method. The results indicated that the drug？protein binding rates were （24. 2 ± 2. 0）%,（18. 4 ± 0. 4）% and （6. 30 ± 0. 3）% at the TP concentrations of 3. 60,7. 20 and 36. 0 μg/mL, respectively. Additionally,the binding mechanism of TP and HSA was investigated by fluorescence quenching method. The results showed that the binding constants at the temperatures of 300,305 and 310 K were 1. 3 × 104 , 7. 8 × 103 and 3. 8 × 103 L/mol,respectively. The binding between TP and HSA is a static quenching process and the main binding force between them is Van der Waals’ force.