title: Spasmolytic activity of trachylobanes ent-7α-acetoxytrachyloban-18-oic acid and ent-7α-hydroxytrachyloban-18-oic acid isolated from Xylopia langsdorfiana A. St-Hil. & Tul. (Annonaceae).
abstract: We aimed to investigate the possible spasmolytic activity of ent-7α-acetoxytrachyloban-18-oic acid (1) and ent-7α-hydroxytrachyloban-18-oic acid (2) on smooth muscle models. In male rat aorta and rat uterus, both diterpenes were unable to trigger spasmolytic action. However, 2 relaxed guinea-pig trachea: Compounds 1 and 2 antagonised, significantly and concentration-dependently, carbachol- and histamine-induced phasic contractions in guinea-pig ileum. Moreover, they induced a significant and concentration-dependent relaxation in pre-contracted (KCl, carbachol or histamine) guinea-pig ileum, with 2 being 15 times more potent than 1 in histamine-contracted ileum. These dissimilar results may be due to chemical differences between them. Thus, we demonstrated that 1 and 2 seem to be promising spasmolytic agents, although further studies are required to elucidate the spasmolytic action mechanism.
authors.affiliation: Laboratório de Tecnologia Farmacêutica Prof. Delby Fernandes de Medeiros, Universidade Federal da Paraíba, João Pessoa, Paraíba, Brazil.
authors.forename: Rosimeire F
authors.initials: RF
authors.lastname: Santos
authors.forename: Italo R R
authors.initials: IR
authors.lastname: Martins
authors.forename: Fabio de S
authors.initials: Fde S
authors.lastname: Monteiro
authors.forename: Rafael de A
authors.initials: Rde A
authors.lastname: Travassos
authors.forename: Daniele I
authors.initials: DI
authors.lastname: Janebro
authors.forename: Josean F
authors.initials: JF
authors.lastname: Tavares
authors.forename: Marcelo S
authors.initials: MS
authors.lastname: Silva
authors.forename: Bagnólia A
authors.initials: BA
authors.lastname: da Silva
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D001011:Aorta / Q000187:drug effects; D001938:Brazil; D004224:Diterpenes / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D010276:Parasympatholytics / Q000302:isolation & purification / Q000494:pharmacology*; D024301:Plant Bark / Q000737:chemistry*; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology*; D051381:Rats; D014132:Trachea / Q000187:drug effects; D014599:Uterus / Q000187:drug effects; D054336:Xylopia / Q000737:chemistry*
chemical_list: D004224:Diterpenes; D010276:Parasympatholytics; D010936:Plant Extracts; C572780:ent-7alpha-acetoxytrachyloban-18-oic acid; C572781:ent-7alpha-hydroxytrachyloban-18-oic acid