TY - JOUR
T1 - Characterization the affinity of α1A adrenoreceptor by cell membrane chromatography with frontal analysis and stoichiometric displacement model
AU - Wei, Fen
AU - Wang, Sicen
AU - Lv, Nan
AU - Bu, Yusi
AU - Xie, Xiaoyu
N1 - Publisher Copyright:
© 2016 Elsevier B.V.
PY - 2017/1/1
Y1 - 2017/1/1
N2 - 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 (α1A AR) 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 α1A AR. The results indicate that the seven alkaloids have similar interaction strengths with tamsulosin hydrochloride (α1A AR antagonist) between them and α1A AR. In addition, electrostatic force is the main intermolecular forces between tamsulosin hydrochloride and seven alkaloids and α1A AR. The study provides a versatile approach for the characterization the affinity between drug and receptor by CMC model.
AB - 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 (α1A AR) 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 α1A AR. The results indicate that the seven alkaloids have similar interaction strengths with tamsulosin hydrochloride (α1A AR antagonist) between them and α1A AR. In addition, electrostatic force is the main intermolecular forces between tamsulosin hydrochloride and seven alkaloids and α1A AR. The study provides a versatile approach for the characterization the affinity between drug and receptor by CMC model.
KW - Cell membrane chromatography
KW - Frontal analysis
KW - Stoichiometric displacement model
KW - α Adrenoreceptor
UR - https://www.scopus.com/pages/publications/85007206633
U2 - 10.1016/j.jchromb.2016.11.002
DO - 10.1016/j.jchromb.2016.11.002
M3 - 文章
C2 - 27836488
AN - SCOPUS:85007206633
SN - 1570-0232
VL - 1040
SP - 273
EP - 281
JO - Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
JF - Journal of Chromatography B: Analytical Technologies in the Biomedical and Life Sciences
ER -