马钱子生物碱血浆蛋白结合率的测定与比较

Determination and comparison of plasma protein binding rate of alkaloids from seed of Strychnou nux-vomica

目的:测定马钱子总生物碱中主要有效成分马钱子碱和士的宁的血浆蛋白结合率,并与同浓度单成分的血浆蛋白结合率进行比较。方法:采用超滤法和高效液相色谱法对马钱子生物碱在大鼠血浆中的血浆蛋白结合率进行测定。结果:单成分的马钱子碱在0.520,1.300,2.600 mg.L-1下的血浆蛋白结合率分别为(65.60±3.01)%,(68.20±7.80)%,(59.58±3.78)%。单成分的士的宁在0.936,2.340,4.680 mg.L-1下的血浆蛋白结合率分别为(66.17±6.36)%,(67.10±2.52)%,(57.21±0.79)%。马钱子总生物碱中马钱子碱在0.519,1.288,2.607 mg.L-1下的血浆蛋白结合率分别为(62.19±2.45)%,(69.55±5.84)%,(61.76±3.68)%;马钱子总生物碱中士的宁在0.940,2.338,4.674 mg.L-1下的血浆蛋白结合率分别为(54.79±3.55)%,(57.13±4.49)%,(59.31±3.65)%。结论:马钱子碱和士的宁与血浆蛋白具有中等强度的结合,马钱子总生物碱中马钱子碱与同浓度单体相比,蛋白结合率差异不大;总碱中士的宁与同浓度单体相比,蛋白结合率有所降低。

Objective： To determine the plasma protein binding rates of brucine and strychnine in total alkaloids from the seed of Strychnou nux-vomica, and make comparison with the single components at the same concentration. Method： Ultrafiltration was employed to determine the rat the plasma protein binding rate of the alkaloids from the seed of S. nux-vomica. The plasma concentrations were measured by RP-HPLC. Result： The protein binding rates of brucine were （ 65. 60 ±3.01 ） % , （ 68. 20 ± 7. 80 ） % , （ 59.58 ±3.78 ） % when the plasma concentrations was 0. 520,1. 300,2. 600 mg·L^-1 , respectively. The protein binding rates of strychnine was （66. 17 ±6. 36 ）% , （67.10 ±2. 52 ）% , （57. 21 ±0. 79 ）% when the plasma concentrations were 0. 936,2. 340,4. 680 mg ·L^-1 respectively. As to the total alkaloids from the seed of S. nux-vomica, The protein binding rate of brucine was （62. 19 ±2. 45 ）% , （69. 55 ±5.84）%, （61.76 ±3.68）% when the plasma concentrations were 0. 519,1. 288,2. 607 mg·L^-1 , respectively. And the protein binding rates of strychnine were （ 54. 79 ±3.55 ） %, （ 57.13 ±4.49 ） %, （ 59. 31 ±3.65 ） % when the plasma concentrations were 0. 940,2. 338,4. 674 mg ·L^-1, respectively. Conclusion： Brucine and strychnine have medium capacity in binding to plasma protein. In comparison with the single component of the same concentration, the protein binding rate of brucine in total alkaloids shows little difference, while there seems to be an obvious decrease for strychnine.