Abstract
We recently characterized the PKI55 protein as an endogenous protein kinase C (PKC) inhibitor and investigated, in vitro, the potential anti-inflammatory actions of its N-terminal peptides 1-16 (peptide 5), 1-8 (peptide 8) and 1-5 (peptide 9). We showed their ability to inhibit chemotaxis in human polymorphonuclear leukocytes activated by the N-formyl tripeptide for-Met-Leu-Phe-OMe. In this work, we evaluated the anti-inflammatory and the analgesic effects of the selected peptides by in vivo experiments carried out in the mouse. The peptides 5, 8 and 9 (0.1 and 10 nmol i.c.v.) were effective in both the parameters chosen to test the anti-inflammatory activity, i.e., the xylene-induced ear edema and the acetic acid-induced infiltration of neutrophils in the peritoneal cavity. In addition, they displayed analgesic effect, evaluated by the acetic acid-induced writhing test. All the peptides' effects were shared by the reference compounds, dexamethasone and indomethacin (10 mg kg(-1) i.p.), but not by the 9-scramble peptide (10 nmol i.c.v.). The peptide 9, which represents the shortest active sequence of the PKI55 protein, was tested in the ear edema model even following intraperitoneal (i.p.) administration and proved to be effect...Continue Reading
References
Sep 1, 1992·Agents and Actions·M J MulqueenA D Sedgwick
Dec 1, 1986·Journal of Pharmacological Methods·S E Laursen, J K Belknap
Jan 1, 1993·Agents and Actions·S KucheraD Schrier
Jan 1, 1997·Cellular Signalling·J E MerrittJ S Nixon
Jan 8, 1998·Endocrinology·A V Turnbull, C L Rivier
Sep 9, 2000·Neuroscience Letters·D H KimD K Song
Mar 29, 2003·Biochemical Pharmacology·David J Grainger, Jill Reckless
Oct 18, 2003·Journal of Molecular Evolution·Rita SelvaticiEnrico Gandini
Mar 9, 2004·Peptides·Bariş CakirBerrak C Yeğen
May 17, 2005·Mini Reviews in Medicinal Chemistry·Rahul Jain, Suresh Chawrai
Dec 20, 2005·Neuroscience·O J Igwe
Mar 7, 2006·European Journal of Pharmacology·Rita SelvaticiSusanna Spisani
Nov 14, 2006·Journal of Inorganic Biochemistry·Anna MessereAlessandra Romanelli
Jan 20, 2007·Physiology & Behavior·Pierre MormèdeIsabelle Veissier
Mar 31, 2007·Cellular Microbiology·Ok S ShinLinden T Hu
May 1, 2007·Archives of Biochemistry and Biophysics·Rita SelvaticiAnna Siniscalchi
Sep 4, 2007·Gastroenterology·Daniel P PooleJohn B Furness
Jan 2, 2008·The Veterinary Journal·M Carmen MarcaM Jesús Rodríguez-Yoldi
Jan 3, 2008·The FEBS Journal·Rita SelvaticiSusanna Spisani
Aug 20, 2008·Nature Immunology·Charles R Mackay
Oct 28, 2008·The Journal of Surgical Research·Sebastian SchublBo Liu
Dec 6, 2008·Trends in Endocrinology and Metabolism : TEM·Eric N ChurchillDaria Mochly-Rosen
Dec 20, 2008·Biochimie·Monica BorgattiRita Selvatici
Apr 28, 2009·Bioorganic & Medicinal Chemistry·Sara CesariniElisabetta Barocelli