Characterization the affinity of α1Aadrenoreceptor by cell membrane chromatography with frontal analysis and stoichiometric displacement model.
As a bionic chromatographic method, cell membrane chromatography (CMC) has been used widely in screening active components in traditional Chinese medicine. Nevertheless, few studies have characterized the affinity between drug and receptor by CMC model. In this study, the alpha 1 adrenoreceptor (α1AAR) high expression CMC method, combined with frontal analysis and stoichiometric displacement model respectively, was established for characterizing the affinity of seven alkaloids binding to the α1AAR. The results indicate that the seven alkaloids have similar interaction strengths with tamsulosin hydrochloride (α1AAR antagonist) between them and α1AAR. In addition, electrostatic force is the main intermolecular forces between tamsulosin hydrochloride and seven alkaloids and α1AAR. The study provides a versatile approach for the characterization the affinity between drug and receptor by CMC model.
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.
Fen
F
Wei
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.
Sicen
S
Wang
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.
Nan
N
Lv
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China.
Yusi
Y
Bu
School of Pharmacy, Health Science Center, Xi'an Jiaotong University, Xi'an 710061, China. Electronic address: xiexiaoyu@xjtu.edu.cn.
Xiaoyu
X
Xie
D058668:Adrenergic alpha-1 Receptor Antagonists / Q000378:metabolism; D000470:Alkaloids / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism*; D002851:Chromatography, High Pressure Liquid / Q000295:instrumentation*; D004365:Drugs, Chinese Herbal / Q000378:metabolism*; D004867:Equipment Design; D015870:Gene Expression; D057809:HEK293 Cells; D006801:Humans; D008954:Models, Biological; D011485:Protein Binding; D018340:Receptors, Adrenergic, alpha-1 / Q000235:genetics / Q000378:metabolism*; D013449:Sulfonamides / Q000378:metabolism; D000077409:Tamsulosin
D058668:Adrenergic alpha-1 Receptor Antagonists; D000470:Alkaloids; D004365:Drugs, Chinese Herbal; D018340:Receptors, Adrenergic, alpha-1; D013449:Sulfonamides; D000077409:Tamsulosin
Cell membrane chromatography; Frontal analysis; Stoichiometric displacement model; α(1) Adrenoreceptor