title: Research on drug-receptor interactions and prediction of drug activity via oriented immobilized receptor capillary electrophoresis.
abstract: 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.
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Chunye
authors.initials: C
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Xuejiao
authors.initials: X
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Hui
authors.initials: H
authors.lastname: Jing
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Miao
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Lingzhi
authors.initials: L
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Yan
authors.initials: Y
authors.lastname: Han
authors.affiliation: School of Pharmacy, Xi'an Medical University, Xi'an, P. R. China.
authors.forename: Cuixia
authors.initials: C
authors.lastname: Cui
mesh_terms: D004347:Drug Interactions; D019075:Electrophoresis, Capillary / Q000379:methods*; D006801:Humans; D055767:Immobilized Proteins / Q000737:chemistry* / Q000378:metabolism*; D008956:Models, Chemical; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism*; D010936:Plant Extracts; D018343:Receptors, Adrenergic, beta-2; D015203:Reproducibility of Results
chemical_list: D055767:Immobilized Proteins; D004364:Pharmaceutical Preparations; D010936:Plant Extracts; D018343:Receptors, Adrenergic, beta-2
keywords: Capillary electrophoresis; Drug activity; Interaction; Oriented covalent immobilization