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目的:研究苦碟子中倍半萜内酯类化合物苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白的结合率。方法:采用HPLC法测定苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的总浓度及游离药物浓度,色谱分离采用Zorbax SB-C_(18)色谱柱(4.6 mm×250 mm,5μm),以水(A)-甲醇(B)为流动相,线性梯度洗脱(0~5 min,30%B→37%B;5~15 min,37%B→52%B;15~22 min,52%B→60%B),流速1.0mL·min~(-1),柱温30℃,检测波长272 nm,进样量10μL;在37℃条件下,应用平衡透析法测定苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白结合率。结果:低、中、高3个浓度下,苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z的牛血清白蛋白结合率分别为51.21%、54.72%、52.14%和50.63%、52.82%、50.28%。结论:苦荬菜内酯Z和11,13α-二氢苦荬菜内酯Z具有中等强度的蛋白结合率,且无明显的浓度依赖性。
OBJECTIVE: To study the binding rate of sesquiterpene lactones zusanliu Z and 11,13α-dihydrodibenzoyl-lactone Z bovine serum albumin in Kudiezi. Methods: The total concentration and free drug concentration of Zanthoxylulose Z and 11,13α-Dihydrodibenzoyllactone Z were determined by HPLC. The chromatographic separation was performed on a Zorbax SB-C 18 column (4.6 mm × 250 (0-5 min, 30% B → 37% B; 5-15 min, 37% B → 52% B) using a mobile phase of water-methanol (B) 15 ~ 22 min, 52% B → 60% B), the flow rate was 1.0 mL · min -1, the column temperature was 30 ℃, the detection wavelength was 272 nm and the injection volume was 10 μL. At 37 ℃, The bovine serum albumin binding rate of bitter lactone Z and 11,13α-dihydrodibenzoyl-lactone Z was measured. Results: The bovine serum albumin binding rates of bitter lactone Z and 11,13α-dihydrodibenzoyl-lactone Z were 51.21%, 54.72%, 52.14% and 50.63 %, 52.82%, 50.28%. CONCLUSIONS: Bitterness lactone Z and 11,13α-dihydrodibenzoyllactone Z have moderately strong protein binding rates without significant concentration dependence.