Inhibitory effect of egualen sodium: a new stable derivative of azulene on histamine release from mast cell-like cells in the stomach.
We studied the inhibitory effect of egualen sodium (ES) (sodium 3-ethyl-7-isopropyl-1-azulenesulfonate 1/3 hydrate, KT1-32), a new derivative and more stable compound than azulene, on histamine release from the mucosal histaminocytes and elucidated the mechanism for this action. ES prevented the histamine release from isolated mast cell-like cells of the guinea pig stomach induced by A23187 in a dose-dependent fashion. ES dose-dependently inhibited the histamine release from lung pieces of sensitized guinea pigs induced by an antigen-antibody reaction. ES also inhibited histamine release from rat peritoneal mast cells induced by compound 48/80 or antigen-antibody reaction. ES exhibited the membrane stabilizing activity on DPPC liposomes. These findings suggest that ES may prevent histamine release from histaminocytes induced by various stimuli and the stabilizing action of the cell membrane may be responsible for the inhibition of histamine release.
Akagi
M
M
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Tokushima, Japan. akagi@ph.bunri-u.ac.jp
Matsui
N
N
Mochizuki
S
S
Tasaka
K
K
D000731:Androstanes / Q000378:metabolism; D000818:Animals; D000897:Anti-Ulcer Agents / Q000737:chemistry / Q000494:pharmacology; D052176:Azulenes; D002152:Calorimetry, Differential Scanning; D000242:Cyclic AMP / Q000378:metabolism; D006168:Guinea Pigs; D006632:Histamine / Q000378:metabolism*; D066298:In Vitro Techniques; D008081:Liposomes; D008168:Lung / Q000187:drug effects / Q000378:metabolism; D008297:Male; D008407:Mast Cells / Q000187:drug effects* / Q000378:metabolism; D010529:Peritoneal Cavity / Q000166:cytology; D051381:Rats; D017208:Rats, Wistar; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*; D013270:Stomach / Q000166:cytology*
C415601:3-oxo-androstan-17-yl-(2'',2'',6'',6''-tetramethyl-N-oxyl)piperidyl butan-1',4'-dioate; D000731:Androstanes; D000897:Anti-Ulcer Agents; D052176:Azulenes; D008081:Liposomes; D012717:Sesquiterpenes; C403723:sodium 3-ethyl-7-isopropyl-1-azulenesulfonate; D006632:Histamine; D000242:Cyclic AMP