Martínez-Gómez Maria A, Villanueva-Camañas R M, Sagrado Salvador, Medina-Hernández Maria J
Departamento de Química Analítica, Facultat de Farmacia, Universitat de Valencia, Burjassot, Valencia, Spain.
Electrophoresis. 2006 Nov;27(21):4364-74. doi: 10.1002/elps.200600216.
The enantiomeric resolution of compounds using HSA by means of affinity EKC (AEKC)-partial filling technique is the result of a delicate balance between different experimental variables such as protein concentration, running pH (background electrophoretic buffer (BGE), protein, and compound solutions), and plug length. In this paper, the possibility of using HSA as chiral selector for enantioseparation of 28 basic drugs using this methodology is studied. The effect of the physicochemical parameters, the structural properties of compounds, and compound-HSA protein binding percentages over their chiral resolution with HSA is outlined. Based on the results obtained, a decision tree is proposed for the "a priori" prediction of the capability of HSA for enantioseparation of basic drugs in AEKC. The results obtained indicated that enantioresolution of basic compounds with HSA depends on the hydrophobicity, polarity, and molar volume of compounds.
采用亲和毛细管电泳（AEKC）-部分填充技术，利用人血清白蛋白（HSA）对化合物进行对映体拆分，是不同实验变量（如蛋白质浓度、运行pH值（背景电泳缓冲液（BGE）、蛋白质和化合物溶液）以及塞子长度）之间微妙平衡的结果。本文研究了使用该方法将HSA用作手性选择剂对28种碱性药物进行对映体拆分的可能性。概述了物理化学参数、化合物的结构性质以及化合物与HSA的蛋白质结合百分比对其与HSA的手性拆分的影响。基于所得结果，提出了一个决策树，用于“先验”预测HSA在AEKC中对碱性药物进行对映体拆分的能力。所得结果表明，HSA对碱性化合物的对映体拆分取决于化合物的疏水性、极性和摩尔体积。
