title: 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): a novel non-nitrogenous ligand for 5-HT2B receptor.
abstract: Chromones are a class of natural products found in almost every known terrestrial plant with over 4000 naturally occurring derivatives having been isolated and structurally elucidated. Recently, 5-hydroxy-2-(2-phenylethyl)chromone (5-HPEC), isolated from Imperata cylindrical, showed neuroprotective activity against glutamate induced excitotoxicity in primary cultures of rat cortical cells. In comparison to other naturally occurring neuroprotective chromones, 5-HPEC contains fewer hydroxyl groups. Here we report our most recent characterization on this interesting natural product against a number of CNS receptors for the purpose to identify the potential molecular targets that may be related to its biological activity. Based on our studies, including radiobinding assays, calcium flux functional assays and molecular modeling studies, 5-HPEC may represent a type of novel nonnitrogenous ligands to the 5-HT2B receptor.
authors.affiliation: Department of Pharmacology and Toxicology, Virginia Commonwealth University, 410 North 12th Street, PO Box 980613, Richmond, VA 23298-0613, United States. Electronic address: williamsda2@vcu.edu.
authors.forename: Dwight A
authors.initials: DA
authors.lastname: Williams
authors.affiliation: Department of Medicinal Chemistry, Virginia Commonwealth University, BioTech One, Suite 205, 800 E. Leigh St., PO Box 980540, Richmond, VA 23298-0540, United States.
authors.forename: Saheem A
authors.initials: SA
authors.lastname: Zaidi
authors.affiliation: Department of Medicinal Chemistry, Virginia Commonwealth University, BioTech One, Suite 205, 800 E. Leigh St., PO Box 980540, Richmond, VA 23298-0540, United States. Electronic address: yzhang2@vcu.edu.
authors.forename: Yan
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D000818:Animals; D001665:Binding Sites; D002867:Chromones / Q000737:chemistry* / Q000378:metabolism; D008024:Ligands; D062105:Molecular Docking Simulation; D009584:Nitrogen / Q000737:chemistry*; D006109:Poaceae / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D017434:Protein Structure, Tertiary; D051381:Rats; D044403:Receptor, Serotonin, 5-HT2B / Q000737:chemistry* / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: C508837:5-hydroxy-2-(2-phenylethyl)chromone; D002867:Chromones; D008024:Ligands; D044403:Receptor, Serotonin, 5-HT2B; D058830:Serotonin 5-HT2 Receptor Antagonists; D009584:Nitrogen
keywords: 5-HT2B receptor; Antagonist; Chromone; Neuroprotection