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Research on drug–receptor interactions and prediction of drug activity via oriented immobilized receptor capillary electrophoresis

Liu, Chunye, Zhang, Xuejiao, Jing, Hui, Miao, Yanqing, Zhao, Lingzhi, Han, Yan, Cui, Cuixia
Electrophoresis 2015 v.36 no.19 pp. 2433-2441
capillary electrophoresis, coatings, correlation, drugs, equations, fluorescence emission spectroscopy, fluorescence microscopy, infrared spectroscopy, microwave treatment, prediction, solutes
Oriented covalent immobilized β₂‐adrenergic receptor (β₂‐AR) CE (OIRCE) was developed to determine the interactions between a set of natural extracts of Radix Paeoniae Rubra (NERPR) and β₂‐AR, and to predict the activity of NERPR. The inner capillary surface is chemically bonded with stable β₂‐AR coating via microwave‐assisted technical synthesis. The modified capillaries were characterized via infrared spectroscopy and fluorescence microscopy. Furthermore, the bonding amounts of β₂‐AR were first obtained via fluorescence spectroscopy method. In determining the amount of bonded β₂‐AR, the regression equation A = 576 707C + 35.449 and the correlation coefficient 0.9995 were obtained. This result revealed an excellent linear relationship in the range of 2 × 10⁻⁴ mg/mL to 1 × 10⁻³ mg/mL. The normalized capacity factor (KRCE) was obtained using OIRCE in evaluating drug–receptor interactions. Related theories and equations were used to calculate KRCE values from apparent migration times of a solute and EOF. The order of KRCE and the binding constant (Kb) values between drugs and β₂‐AR was well consistent. The results confirmed that the OIRCE and KRCE values can be effectually used to investigate drug‐receptor interactions, and OIRCE has the potential to predict drug activity and to select leading compounds from natural chemicals.