Antianaphylactic properties of 7-epiclusianone, a tetraprenylated benzophenone isolated from Garcinia brasiliensis.
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.
Neves
Josiane Sabbadini
JS
Laboratory of Inflammation, Department of Physiology and Pharmacodynamics, Oswaldo Cruz Institute, Oswaldo Cruz Foundation (FIOCRUZ), Rio de Janeiro, RJ, Brazil.
Coelho
Luciana Pontes
LP
Cordeiro
Renato Sérgio Balão
RS
Veloso
Marcia Paranho
MP
Rodrigues e Silva
Patricia Machado
PM
dos Santos
Marcelo Henrique
MH
Martins
Marco Aurélio
MA
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*
C118110:7-epiclusianone; D000485:Allergens; D018926:Anti-Allergic Agents; D001577:Benzophenones; D016227:Benzoquinones; D010793:Phthalazines; D010936:Plant Extracts; C047723:benzophenone; C020976:azelastine