title: Alkamides from Echinacea angustifolia Interact with P-glycoprotein of primary brain capillary endothelial cells isolated from porcine brain blood vessels.
abstract: The blood-brain barrier prevents the passage of toxic compounds from blood circulation into brain tissue. Unfortunately, drugs for the treatment of neurodegenerative diseases, brain tumors, and other diseases also do not cross the blood-brain barrier. In the present investigation, we used isolated porcine brain capillary endothelial cells and a flow cytometric calcein-AM assay to analyze inhibition of P-glycoprotein, a major constituent of the blood-brain barrier. We tested 8 alkamides isolated from Echinacea angustifolia and found that four of them inhibited P-glycoprotein-mediated calcein transport in porcine brain capillary endothelial cells.
authors: Institute of Pharmacy and Molecular Biotechnology, Department of Pharmaceutical Technology and Pharmacology, University of Heidelberg, Heidelberg, Germany.
authors: Anne
authors: A
authors: Mahringer
authors: Karin
authors: K
authors: Ardjomand-Woelkart
authors: Rudolf
authors: R
authors: Bauer
authors: Gert
authors: G
authors: Fricker
authors: Thomas
authors: T
authors: Efferth
mesh_terms: D018435:ATP Binding Cassette Transporter, Subfamily B / Q000037:antagonists & inhibitors / Q000378:metabolism*; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D001812:Blood-Brain Barrier / Q000187:drug effects; D001921:Brain / Q000098:blood supply; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D020900:Echinacea / Q000737:chemistry*; D042783:Endothelial Cells / Q000187:drug effects* / Q000378:metabolism*; D005434:Flow Cytometry / Q000379:methods; D005452:Fluoresceins / Q000378:metabolism; D015394:Molecular Structure; D053284:Polyunsaturated Alkamides / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013552:Swine
chemical_list: D018435:ATP Binding Cassette Transporter, Subfamily B; D005452:Fluoresceins; D053284:Polyunsaturated Alkamides; C085925:calcein AM; C007740:fluorexon