title: Procyanidins are potent inhibitors of LOX-1: a new player in the French Paradox.
abstract: Lectin-like oxidized LDL receptor-1 (LOX-1) is an endothelial receptor for oxidized LDL (oxLDL) and plays multiple roles in the development of cardiovascular diseases. We screened more than 400 foodstuff extracts for identifying materials that inhibit oxLDL binding to LOX-1. Results showed that 52 extracts inhibited LOX-1 by more than 70% in cell-free assays. Subsequent cell-based assays revealed that a variety of foodstuffs known to be rich in procyanidins such as grape seed extracts and apple polyphenols, potently inhibited oxLDL uptake in Chinese hamster ovary (CHO) cells expressing LOX-1. Indeed, purified procyanidins significantly inhibited oxLDL binding to LOX-1 while other ingredients of apple polyphenols did not. Moreover, chronic administration of oligomeric procyanidins suppressed lipid accumulation in vascular wall in hypertensive rats fed with high fat diet. These results suggest that procyanidins are LOX-1 inhibitors and LOX-1 inhibition might be a possible underlying mechanism of the well-known vascular protective effects of red wine, the French Paradox.
authors.affiliation: Department of Vascular Physiology, National Cerebral and Cardiovascular Center, Osaka, Japan.
authors.forename: Taichi
authors.initials: T
authors.lastname: Nishizuka
authors.forename: Yoshiko
authors.initials: Y
authors.lastname: Fujita
authors.forename: Yuko
authors.initials: Y
authors.lastname: Sato
authors.forename: Atushi
authors.initials: A
authors.lastname: Nakano
authors.forename: Akemi
authors.initials: A
authors.lastname: Kakino
authors.forename: Shunji
authors.initials: S
authors.lastname: Ohshima
authors.forename: Tomomasa
authors.initials: T
authors.lastname: Kanda
authors.forename: Ryo
authors.initials: R
authors.lastname: Yoshimoto
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Sawamura
mesh_terms: D000818:Animals; D044946:Biflavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D016466:CHO Cells; D002392:Catechin / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006224:Cricetinae; D003412:Cricetulus; D004353:Drug Evaluation, Preclinical; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D005602:France; D006801:Humans; D008077:Lipoproteins, LDL / Q000378:metabolism; D008297:Male; D027845:Malus / Q000737:chemistry; D008954:Models, Biological; D010636:Phenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D058105:Polymerization; D059808:Polyphenols; D044945:Proanthocyanidins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D051127:Scavenger Receptors, Class E / Q000037:antagonists & inhibitors* / Q000378:metabolism; D014920:Wine
chemical_list: D044946:Biflavonoids; D005419:Flavonoids; D008077:Lipoproteins, LDL; C495137:OLR1 protein, human; D010636:Phenols; D059808:Polyphenols; D044945:Proanthocyanidins; D051127:Scavenger Receptors, Class E; C099252:oxidized low density lipoprotein; C017674:procyanidin; D002392:Catechin