title: Antianaphylactic properties of 7-epiclusianone, a tetraprenylated benzophenone isolated from Garcinia brasiliensis.
abstract: Prior studies have emphasized the anti-inflammatory and antioxidant properties of polyisoprenylated benzophenone derivatives, but their putative effect on allergic conditions has not yet been addressed. In the current study, the naturally occurring 7-epiclusianone, isolated from Garcinia brasiliensis, was investigated to check its effectiveness on allergen-evoked intestinal spasm. The standard antiallergic azelastine was used for comparison. We found that 7-epiclusianone and azelastine inhibited antigen-induced contractions of guinea pig ileum with similar IC (50) values (2.3 +/- 1.1 microM and 3.3 +/- 1.2 microM, respectively). A similar blockade of anaphylactic histamine release from the ileum was also noted. In contrast, azelastine was more potent than 7-epiclusianone to prevent spasms induced by histamine (IC (50) = 6.3 +/- 0.2 nM and 3.7 +/- 0.1 microM, respectively). These findings reveal that 7-epiclusianone is clearly active against the anaphylactic response and should be considered as a molecular template in drug discovery for allergic syndromes.
authors.affiliation: Laboratory of Inflammation, Department of Physiology and Pharmacodynamics, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), Rio de Janeiro, RJ, Brazil.
authors.forename: Josiane Sabbadini
authors.initials: JS
authors.lastname: Neves
authors.forename: Luciana Pontes
authors.initials: LP
authors.lastname: Coelho
authors.forename: Renato Sérgio Balão
authors.initials: RS
authors.lastname: Cordeiro
authors.forename: Marcia Paranho
authors.initials: MP
authors.lastname: Veloso
authors.forename: Patricia Machado
authors.initials: PM
authors.lastname: Rodrigues e Silva
authors.forename: Marcelo Henrique
authors.initials: MH
authors.lastname: dos Santos
authors.forename: Marco Aurélio
authors.initials: MA
authors.lastname: Martins
mesh_terms: D000485:Allergens; D000818:Animals; D018926:Anti-Allergic Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D001577:Benzophenones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D016227:Benzoquinones / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D005260:Female; D005638:Fruit; D029760:Garcinia; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects*; D020128:Inhibitory Concentration 50; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D010793:Phthalazines / Q000494:pharmacology; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D014132:Trachea / Q000187:drug effects*
chemical_list: C118110:7-epiclusianone; D000485:Allergens; D018926:Anti-Allergic Agents; D001577:Benzophenones; D016227:Benzoquinones; D010793:Phthalazines; D010936:Plant Extracts; C047723:benzophenone; C020976:azelastine