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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 rate of brucine and strychnine, the main active components in the total alkaloids of Strychnos nux vomica, and to compare their plasma protein binding rates with single components of the same concentration. Methods: The plasma protein binding rate of Strychnos alkaloids in rat plasma was determined by ultrafiltration and high performance liquid chromatography. Results: The plasma protein binding rates of single-component brucine at (0.520,1.300,2.600 mg.L-1) were (65.60 ± 3.01)%, (68.20 ± 7.80)% and (59.58 ± 3.78)%, respectively. The plasma protein binding rates of single-component strychnine at (0.936,2.340,4.680 mg.L-1) were (66.17 ± 6.36)%, (67.10 ± 2.52)% and (57.21 ± 0.79)%, respectively. The plasma protein binding rates of brucine in the total alkaloids of Strychnos nux - vomica were (62.19 ± 2.45)%, (69.55 ± 5.84)% and (61.76 ± 3.68)% at 0.519, 1.288 and 2.607 mg · L -1, (54.79 ± 3.55)%, (57.13 ± 4.49)%, (59.31 ± 3.65)%, respectively. The plasma protein binding rate of strychnine in strychnos alkaloids at 0.940, 2.338 and 4.674 mg.L- . CONCLUSIONS: Both strychnine and strychnine have moderate binding to plasma proteins. There was no significant difference in protein binding between strychnine and strychnine in the total Strychnos alkaloids. Compared with the same concentration of monomer, the protein binding rate decreased.