title: Gastroprotective effects of L-lysine salification of ketoprofen in ethanol-injured gastric mucosa.
abstract: Ketoprofen L-lysine salt (KLS), a NSAID, is widely used for its analgesic efficacy and tolerability. L-lysine salification was reported to increase the solubility and the gastric absorption and tolerance of ketoprofen. Since the management of NSAIDs gastrotoxicity still represents a major limitation in prolonged therapies, mainly when gastric lesions are present, this study investigated the gastro-protective activity of L-lysine by using a well-established model of gastric mucosa injury, the ethanol-gastric injury model. Several evidences show that the damaging action of ethanol could be attributed to the increase of ROS, which plays a key role in the increase of lipid peroxidation products, including malonyldialdehyde and 4-hydroxy-2-nonenal. With the aim to unravel the mechanism of L-lysine gastroprotection, cellular MDA levels and 4-HNE protein adducts as markers of lipid peroxidation and a panel of key endogenous gastro-protective proteins were assayed. The data obtained indicate a gastroprotective effect of L-lysine on gastric mucosa integrity.
authors.affiliation: Department of Life, Health and Environmental Sciences, University of L'Aquila, via Vetoio, L'Aquila, Italy; Sbarro Institute for Cancer Research and Molecular Medicine, Temple University, Philadelphia, Pennsylvania.
authors.forename: Annamaria
authors.initials: A
authors.lastname: Cimini
authors.forename: Laura
authors.initials: L
authors.lastname: Brandolini
authors.forename: Roberta
authors.initials: R
authors.lastname: Gentile
authors.forename: Loredana
authors.initials: L
authors.lastname: Cristiano
authors.forename: Paola
authors.initials: P
authors.lastname: Menghini
authors.forename: Alessia
authors.initials: A
authors.lastname: Fidoamore
authors.forename: Andrea
authors.initials: A
authors.lastname: Antonosante
authors.forename: Elisabetta
authors.initials: E
authors.lastname: Benedetti
authors.forename: Antonio
authors.initials: A
authors.lastname: Giordano
authors.forename: Marcello
authors.initials: M
authors.lastname: Allegretti
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002478:Cells, Cultured; D000431:Ethanol / Q000494:pharmacology*; D005753:Gastric Mucosa / Q000378:metabolism*; D006801:Humans; D007660:Ketoprofen / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D015227:Lipid Peroxidation / Q000187:drug effects / Q000502:physiology; D008239:Lysine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D009569:Nitric Oxide / Q000378:metabolism
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D009569:Nitric Oxide; D000431:Ethanol; C029946:ketoprofen lysine; D007660:Ketoprofen; D008239:Lysine