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目的研究氯吡格雷对人参皂苷Rg1血浆蛋白结合率影响。方法建立人参皂苷Rg1在胎牛血清及透析外液中含量测定方法,随机分成人参皂苷Rg1低、中、高三种浓度单独组(浓度分别为0.4、1.0、5.0 mg/L)和人参皂苷Rg1低、中、高三种浓度合并氯吡格雷组(人参皂苷Rg1浓度依次为0.4、1.0、5.0 mg/L,合并使用2.0 mg/L氯吡格雷),采用平衡透析法观察合并使用氯吡格雷时对人参皂苷Rg1的血清蛋白结合率影响,采用同源模建方法(homology modeling)构建牛血清白蛋白(bovine serum albumin,BSA)三维构建结构,在此基础上采用分子对接方法观察氯吡格雷和人参皂苷Rg1与BSA间结合效应,观察在血浆蛋白结合率层面的相互作用。结果人参皂苷Rg1低、中、高三种浓度单独组与胎牛血清蛋白结合率分别为(11.2±2.1)%、(13.4±2.2)%、(14.6±1.4)%,人参皂苷Rg1在低、中、高三种浓度合并氯吡格雷组血浆蛋白结合率分别下降,分别为(6.5±2.3)%、(9.2±1.5)%、(12.1±1.7)%,差异有统计学意义(P<0.05),分子对接结果显示两个化合物与BSA存在竞争结合效应。结论平衡透析法和分子对接实验综合表明氯吡格雷对人参皂苷Rg1血浆蛋白结合率存在影响作用。
Objective To study the effect of clopidogrel on plasma protein binding rate of ginsenoside Rg1. Methods The method for determining the content of ginsenoside Rg1 in fetal bovine serum and dialysis was established and randomly divided into low, medium and high concentrations of ginsenoside Rg1 (concentration 0.4,1.0,5.0 mg / L) and low ginsenoside Rg1 , Middle and high concentrations of clopidogrel group (ginsenoside Rg1 concentrations followed by 0.4,1.0,5.0 mg / L, the combined use of 2.0 mg / L clopidogrel), the use of equilibrium dialysis observed with clopidogrel on Ginsenoside Rg1 serum protein binding rate, homology modeling method (homology modeling) to build bovine serum albumin (bovine serum albumin, BSA) three-dimensional structure, based on the use of molecular docking method observed clopidogrel and ginseng The binding effect between saponin Rg1 and BSA was observed and the interaction at the level of plasma protein binding was observed. Results The binding rates of ginsenoside Rg1 to fetal bovine serum albumin were (11.2 ± 2.1)%, (13.4 ± 2.2)% and (14.6 ± 1.4)% respectively in low, middle and high concentrations of ginsenoside Rg1. (6.5 ± 2.3)%, (9.2 ± 1.5)% and (12.1 ± 1.7)% respectively in the three concentrations of clopidogrel group, the difference was statistically significant (P <0.05) The molecular docking results showed that the two compounds competed for binding with BSA. Conclusion The balanced dialysis and docking experiments showed that clopidogrel had an effect on the plasma protein binding rate of ginsenoside Rg1.