Novel anti-ulcer α,β-unsaturated lactones inhibit compound 48/80-induced mast cell degranulation.

作者: Alicia B Penissi , Mariano E Vera , María L Mariani , María I Rudolph , Juan P Ceñal

DOI: 10.1016/J.EJPHAR.2009.03.052

关键词: PharmacologyBiochemistryButenolideMast cellCell DegranulationCompound 48/80KetotifenChemistrySesquiterpene lactoneTolonium chlorideDegranulation

摘要: The present study was designed to examine the effects of a sesquiterpene lactone isolated from Artemisia douglasiana Besser (dehydroleucodine), xanthanolide Xanthium cavanillesii Schouw (xanthatin) and semisynthetic butenolide (3-benzyloxymethyl-5H-furan-2-one) on mast cell degranulation induced by compound 48/80. Peritoneal cells male adult Sprague-Dawley rats were purified in Percoll, preincubated presence test lactones (dehydroleucodine, xanthatin or 3-benzyloxymethyl-5H-furan-2-one) then challenged with activator 48/80 (10 microg/ml). Concentration-response kinetic studies serotonin release evoked 48/80, evaluation viability morphology light electron microscopy, comparative using ketotifen sodium chromoglycate carried out. Serotonin studies, out together morphological showed effectiveness above stabilize cells. chromoglycate, well known stabilizers, following order potency dehydroleucodine=xanthatin>3-benzyloxymethyl-5H-furan-2-one> =ketotifen/sodium inhibit provides first strong evidence favour hypothesis that dehydroleucodine, 3-benzyloxymethyl-5H-furan-2-one 48/80-induced peritoneal cells, acting thus as stabilizers. Our findings may provide an insight into design novel pharmacological agents which be used regulate response.

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