title: Screening of target compounds from Fructus Piperis using high α₁A adrenoreceptor expression cell membrane chromatography online coupled with high performance liquid chromatography tandem mass spectrometry.
abstract: Benign prostatic hyperplasia (BPH) is a common disease in elderly men. The main treatment for BPH is α-adrenergic antagonists and 5α-reductase inhibitors. In this study, a two-dimensional (2D) α₁A cell membrane chromatography (CMC) online liquid chromatography/mass spectrometry system was built. Fructus Piperis, a traditional Chinese medicine and food homolog, was assayed with this 2D system. Piperine was identified as the active compound acting on α₁A receptors. A competitive binding assay and molecular docking assay were performed to investigate the binding sites and the affinity of piperine for the α₁A receptor. The results of the competitive binding assay (dissociation equilibrium constant of tamsulosin was 1.43 × 10(-6)M and piperine was 2.13 × 10(-6)M) and molecular docking assay (total score for tamsulosin binding with the α₁A receptor was 6.9719, and for piperine it was 4.4891) corresponded with the retention time of tamsulosin and piperine on the α₁A/CMC column.
authors: School of Medicine, Xi'an Jiaotong University, 76#, Yantan Westroad, Xi'an 710061, China.
authors: Shengli
authors: S
authors: Han
authors: Tao
authors: T
authors: Zhang
authors: Liuxin
authors: L
authors: Feng
authors: Nan
authors: N
authors: Lv
authors: Sicen
authors: S
authors: Wang
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000378:metabolism; D000368:Aged; D000470:Alkaloids / Q000302:isolation & purification / Q000378:metabolism*; D052117:Benzodioxoles / Q000302:isolation & purification / Q000378:metabolism*; D001665:Binding Sites; D001667:Binding, Competitive; D002462:Cell Membrane; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000737:chemistry / Q000378:metabolism*; D057809:HEK293 Cells; D006801:Humans; D008297:Male; D062105:Molecular Docking Simulation; D010880:Piperidines / Q000302:isolation & purification / Q000378:metabolism*; D053284:Polyunsaturated Alkamides / Q000302:isolation & purification / Q000378:metabolism*; D011470:Prostatic Hyperplasia / Q000188:drug therapy; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism*; D013449:Sulfonamides / Q000378:metabolism; D000077409:Tamsulosin; D053719:Tandem Mass Spectrometry / Q000379:methods
chemical_list: D058668:Adrenergic alpha-1 Receptor Antagonists; D000470:Alkaloids; D052117:Benzodioxoles; D004365:Drugs, Chinese Herbal; D010880:Piperidines; D053284:Polyunsaturated Alkamides; D018340:Receptors, Adrenergic, alpha-1; D013449:Sulfonamides; D000077409:Tamsulosin; C008922:piperine