苦碟子中2个倍半萜内酯的牛血清白蛋白结合率的测定

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-C₁₈ 色谱柱（4.6 mm×250 mm，5 μm），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1.0 mL·min^-1，柱温30 ℃，检测波长272 nm，进样量10 μL；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 determine the bovine serum albumin binding rate of Ixerin Z,11,13α-dihydroixerin Z on sesquiterpene lactones of Ixeris sonchifolia. Methods: The total concentration of Ixerin Z and 11,13α-dihydroixerin Z as well as the free drugs were determined by HPLC method. The separation was performed on a Zorbax SB-C₁₈ column (4.6 mm×250 mm,5 μm). A linear gradient elution of solvent water(A)and methanol(B)was applied with the following program:0-5 min,30% B → 37% B;5-15 min,37% B → 52% B and 15-22 min,52% B → 60% B. The flow rate was set as 1.0 mL·min^-1. The temperature of column was set at 30℃. The detection wavelength was set at 272 nm. And the injection volume was 10 μL. The protein binding rates of Ixerin Z and 11,13α-dihydroixerin Z were determined by equilibrium dialysis method at 37℃. Results: The protein-binding rate of Ixerin Z and 11, 13α-dihydroixerin Z at low,middle and high concentration were 51.21%,54.72%,52.14% and 50.63%,52.82%, 50.28%,respectively. Conclusion: The two sesquiterpene lactones have moderate intensity protein-binding rate. And the binding rates are not remarkable concentration-dependent manner of Ixerin Z,11,13α-dihydroixerin Z.

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