Journal of Autoimmunity (2001) 16, 449–455 doi:10.1006/jaut.2001.0507, available online at http://www.idealibrary.com on An Inhibitor of Inducible Nitric Oxide Synthase and Scavenger of Peroxynitrite Prevents Diabetes Development in NOD Mice Wilma L. Suarez-Pinzon 1 , Jon G. Mabley 2 , Ken Strynadka 3 , Robert F. Power 4 , Csaba Szabo ´ 2 and Alex Rabinovitch 1 1 Department of Medicine, University of Alberta, Edmonton, Alberta, Canada 2 Inotek Corporation, Beverly, Massachusetts, USA 3 Department of Pediatrics, University of Alberta, Edmonton, Alberta, Canada 4 Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, Alberta, Canada Received 4 December 2000 Revised version accepted 7 February 2001 Key words: free radicals, insulitis, nitric oxide, NOD mice, peroxynitrite Peroxynitrite (ONOO - ) is a highly reactive oxidant produced by the inter- action of the free radicals superoxide (O c - 2 ) and nitric oxide (NO c ). In a previous study, we found that peroxynitrite is formed in islet -cells of nonobese diabetic (NOD) mice. Here, we report that guanidinoethyldi- sulphide (GED), a selective inhibitor of inducible nitric oxide synthase (iNOS) and scavenger of peroxynitrite prevents diabetes in NOD mice. GED treatment of female NOD mice, starting at age 5 weeks, delayed diabetes onset (from age 12 to 22 weeks) and significantly decreased diabetes incidence at 30 weeks (from 80% to 17%). GED did not prevent pancreatic islet infiltration by leukocytes; however, -cells that stained positive for nitrotyrosine (a marker of peroxynitrite) were significantly decreased in islets of GED-treated mice (1±1%) compared with vehicle-treated mice (30±9%). In addition, GED significantly inhibited nitric oxide and nitrotyrosine formation and decreased destruction of -cells in NOD mouse islets incubated in vitro with the combination of proinflammatory cytokines interleukin 1-beta (IL-1), tumour necrosis factor-alpha (TNF-) and interferon-gamma (IFN-). These findings indicate that both superoxide and nitric oxide radicals contribute to islet -cell destruction in autoimmune diabetes via peroxynitrite formation in the -cells. © 2001 Academic Press Introduction Insulin dependent diabetes mellitus results from destruction of the insulin-producing pancreatic islet -cells by a response considered to be autoimmune [1]. Pancreatic islets are infiltrated by mononuclear cells of the immune system, mostly macrophages and T lymphocytes and this is followed by destruction of the -cells. Islet -cell destruction may result from direct contact with -cell specific cytotoxic T-lymphocytes, as well as from exposure to inflamma- tory products of activated macrophages and T-lymphocytes, such as cytokines, oxygen radicals, and nitric oxide [25]. In addition, the proinflamma- tory cytokines, interleukin 1-beta (IL-1), tumour necrosis factor-alpha (TNF-), and interferon gamma (IFN-) are cytotoxic to islet -cells via mechanisms that may involve production of oxygen radicals and/or nitric oxide in the -cells [411]. Peroxynitrite (ONOO - ) is a highly reactive oxidant species produced by the combination of the free radicals, superoxide (O c - 2 ) and nitric oxide (NO c )[12, 13]. Peroxynitrite production has been observed in many inflammatory conditions [14, 15] and current evidence suggests that peroxynitrite is a more potent and cytotoxic mediator than superoxide or nitric oxide alone [13, 15, 16]. Also, both rodent and human islets are highly sensitive to peroxynitrite-induced damage [17]. In a previous study, we found that peroxynitrite is formed in islet -cells of acutely-diabetic NOD mice [18]. The aim of the present study was to determine if prevention of peroxynitrite formation in -cells of autoimmune diabetes-prone NOD mice would prevent -cell destruction and diabetes development. Materials and Methods Animals Female and male NOD mice, 4 weeks of age, were purchased from Taconic (Germantown, NY, USA). The mice were housed and fed under specific pathogen- free conditions and were cared for according to the guidelines of the Canadian Council on Animal Care. Female NOD mice of this colony develop pancreatic islet infiltration by immune system cells (insulitis) Correspondence to: Alex Rabinovitch, M.D., 430 Heritage Medical Research Centre, University of Alberta, Edmonton, Alberta, Canada T6G 2S2. Fax: (780) 492-4666. E-mail: alex.rabinovitch@ualberta.ca 449 0896–8411/01/040449+07 $35.00/0 © 2001 Academic Press