title: Spasmolytic effect of galetin 3,6-dimethyl ether, a flavonoid obtained from Piptadenia stipulacea (Benth) Ducke.
abstract: Piptadenia stipulacea (Benth) Ducke is a tree of the Caatinga, in Northeast Brazil, popularly known as "Jurema-branca", "Jurema malícia-da-serra", "Carcará" and "Calumbi". In folk medicine, a decoction or tincture of its bark and leaves are used to treat wounds and as healing agents. Galetin 3,6-dimethyl ether (FGAL) is a flavonoid isolated from the aerial components of Piptadenia stipulacea (Benth) Ducke. We decided to investigate a possible FGAL spasmolytic effect on preparations of both the guinea pig ileum and trachea, the rat uterus and the male rat aorta. FGAL inhibited oxytocin (IC(50) = 2.2 ± 0.4 × 10(-5) M) and carbachol (CCh)-induced (IC(50) = 7.7 ± 1.3 × 10(-5) M) phasic contractions in the rat uterus, but was more effective in the inhibition of the oxytocin-induced contractions. In the guinea pig ileum, FGAL equipotently inhibited CCh (IC(50) = 2.8 ± 0.4 × 10(-5) M) and histamine-induced (IC(50) = 2.3 ± 0.5 × 10(-5) M) phasic contractions. FGAL equipotently and concentration-dependently relaxed guinea pig trachea preparations pre-contracted with CCh, both in the absence (EC(50) = 0.8 ± 0.1 × 10(-5) M) and presence (EC(50) = 1.0 ± 0.1 × 10(-5) M) of a functional epithelium. FGAL also relaxed preparations of the rat aorta pre-contracted with phenylephrine in both the absence (EC(50) = 5.0 ± 1.1 × 10(-6) M) and presence (EC(50) = 5.4 ± 1.2 × 10(-6) M) of a functional endothelium. FGAL shows a non-selective spasmolytic effect on each of the smooth muscle preparations we have tested, but with a greater effect on those from the rat aorta. The relaxant effect on preparations of both the guinea pig trachea and the rat aorta seems to not involve the epithelium or endothelium-derived relaxing factors.
authors: Laboratório de Tecnologia Farmacêutica, Universidade Federal da Paraíba, Brazil. bagnolia@ltf.ufpb.br
authors: Cibério Landim
authors: CL
authors: Macêdo
authors: Luiz Henrique César
authors: LH
authors: Vasconcelos
authors: Ana Carolina de C
authors: AC
authors: Correia
authors: Italo Rossi Roseno
authors: IR
authors: Martins
authors: Daysianne Pereira
authors: DP
authors: de Lira
authors: Bárbara Viviana de Oliveira
authors: BV
authors: Santos
authors: Bagnólia Araújo
authors: BA
authors: da Silva
mesh_terms: D000818:Animals; D001011:Aorta / Q000187:drug effects; D001938:Brazil; D004305:Dose-Response Relationship, Drug; D007887:Fabaceae / Q000737:chemistry*; D005260:Female; D005419:Flavonoids / Q000302:isolation & purification* / Q000494:pharmacology*; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D010276:Parasympatholytics; D010936:Plant Extracts / Q000302:isolation & purification* / Q000494:pharmacology*; D051381:Rats; D014132:Trachea / Q000187:drug effects; D014599:Uterus / Q000187:drug effects
chemical_list: D005419:Flavonoids; D010276:Parasympatholytics; D010936:Plant Extracts; C570563:galetin 3,6-dimethyl ether