Anti-inflammatory and immunomodulating effects of the novel agent gamma-(2-aminoethylamino)-2-butyrothienone. 1st communication: inhibitory effects on mouse paw edema.
A series of 4-hydroxy-(or-amino)-ethyl-amino butyrophenones or butyrothienones were synthesized. For detail studies on antiinflammatory effects, gamma-(2-aminoethylamino)-2-butyrothienone (gamma-ABT) was chosen as representative of these new non-steroidal anti-inflammatories (NSAID). The effect on mouse paw edema induced by various phlogistic agents was first investigated. The inhibitory effect of gamma-ABT on carrageenin-induced edema was remarkable and nearly equal to that of indometacin. Similarly to indometacin, gamma-ABT inhibited the early and late stage of yeast-induced edema in contrast to concanavalin A (Con A) induced edema which was only inhibited by gamma-ABT. Both the above induced edema are supposed to be unrelated to prostaglandins in the rat system. gamma-ABT displayed an inhibitory effect on nystatin-induced edema similar to indometacin suggesting that gamma-ABT has significant membrane stabilizing action and a strong blocking action on synthesis of prostaglandins. gamma-ABT inhibited as well the sustained edema induced by mustard. In conclusion gamma-ABT is an effective agent not only on acute but also on subacute and chronic inflammation and its mode of action appears similar to other NSAID. gamma-ABT posses in addition the advantage of antioxidant activity which is not shared by selective cyclooxygenase inhibitors and thus should be potentially effective in autoimmune diseases.
Gavalas
A
A
Department of Genetics, Development and Molecular Biology, School of Biology, Faculty of Sciences, Aristotelian University, Thessaloniki, Greece.
Kourounakis
L
L
Litina
D
D
Kourounakis
P
P
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002351:Carrageenan; D003208:Concanavalin A; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy* / Q000473:pathology; D005260:Female; D005528:Foot / Q000473:pathology; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008815:Mice, Inbred Strains; D009149:Mustard Plant; D009761:Nystatin; D037121:Plant Lectins; D010946:Plants, Medicinal; D013876:Thiophenes / Q000494:pharmacology*; D015003:Yeasts
D000894:Anti-Inflammatory Agents, Non-Steroidal; D037121:Plant Lectins; D013876:Thiophenes; D003208:Concanavalin A; C070063:gamma-(2-aminoethylamino)-2-butryothienone; D009761:Nystatin; D002351:Carrageenan; D007213:Indomethacin