title: Anti-inflammatory and immunosuppressive effects of the enaminone E121.
abstract: Asthma is a chronic inflammatory disease of the airways. The treatment of asthma is far from optimal and hence the need for novel therapeutic agents exists. The purpose of this study was to assess the anti-asthma effects of an enaminone, E121, and also its effects on human peripheral blood mononuclear cell proliferation and cytokine release. The effects of E121 were assessed in an ovalbumin-induced model of airway inflammation and airway hyperresponsiveness. In addition, the effects of E121 on phytohemagglutinin (PHA), anti-CD3 monoclonal antibody and lipopolysaccharide (LPS)-induced human peripheral blood mononuclear cell proliferation and cytokine release, respectively, were assessed. Treatment of mice with E121 significantly decreased the ovalbumin-induced increase in airway total cell influx and eosinophil infiltration and this was associated with an inhibition of ovalbumin-induced airway hyperresponsiveness. Moreover, E121 reduced PHA and anti-CD3-induced human peripheral blood mononuclear cell proliferation in vitro. E121 also inhibited PHA, anti-CD3 monoclonal antibody and LPS-induced cytokine release from human peripheral blood mononuclear cell cultures. These findings indicate that E121 exhibits anti-inflammatory and immunosuppressive activities.
authors.affiliation: Department of Applied Therapeutics, Kuwait University, Kuwait. ahmed.elhashim@hsc.edu.kw
authors.forename: Ahmed
authors.initials: A
authors.lastname: El-Hashim
authors.forename: Shida
authors.initials: S
authors.lastname: Yousefi
authors.forename: Ivan
authors.initials: I
authors.lastname: Edafiogho
authors.forename: Raj
authors.initials: R
authors.lastname: Raghupathy
authors.forename: Mariam
authors.initials: M
authors.lastname: Yousif
authors.forename: Hans-Uwe
authors.initials: HU
authors.lastname: Simon
mesh_terms: D000328:Adult; D000814:Aniline Compounds / Q000276:immunology / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D018927:Anti-Asthmatic Agents / Q000276:immunology / Q000494:pharmacology* / Q000627:therapeutic use; D000893:Anti-Inflammatory Agents / Q000276:immunology / Q000494:pharmacology* / Q000627:therapeutic use; D001249:Asthma / Q000139:chemically induced / Q000188:drug therapy* / Q000276:immunology; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D003509:Cyclohexanecarboxylic Acids / Q000276:immunology / Q000494:pharmacology* / Q000627:therapeutic use; D016207:Cytokines / Q000276:immunology; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007166:Immunosuppressive Agents / Q000276:immunology / Q000494:pharmacology* / Q000627:therapeutic use; D007249:Inflammation / Q000188:drug therapy / Q000276:immunology; D007963:Leukocytes, Mononuclear / Q000166:cytology / Q000187:drug effects; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008875:Middle Aged; D010047:Ovalbumin / Q000276:immunology
chemical_list: D000814:Aniline Compounds; D018927:Anti-Asthmatic Agents; D000893:Anti-Inflammatory Agents; D003509:Cyclohexanecarboxylic Acids; D016207:Cytokines; C483746:E 121 compound; D007166:Immunosuppressive Agents; D010047:Ovalbumin