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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.
AuthorsJosiane Sabbadini Neves, Luciana Pontes Coelho, Renato Sérgio Balão Cordeiro, Marcia Paranho Veloso, Patricia Machado Rodrigues e Silva, Marcelo Henrique dos Santos, Marco Aurélio Martins
JournalPlanta medica (Planta Med) Vol. 73 Issue 7 Pg. 644-9 (Jun 2007) ISSN: 0032-0943 [Print] Germany
PMID17562491 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 7-epiclusianone
  • Allergens
  • Anti-Allergic Agents
  • Benzophenones
  • Benzoquinones
  • Phthalazines
  • Plant Extracts
  • benzophenone
  • azelastine
Topics
  • Allergens
  • Animals
  • Anti-Allergic Agents (administration & dosage, pharmacology, therapeutic use)
  • Benzophenones (administration & dosage, pharmacology, therapeutic use)
  • Benzoquinones (administration & dosage, pharmacology, therapeutic use)
  • Dose-Response Relationship, Drug
  • Female
  • Fruit
  • Garcinia
  • Guinea Pigs
  • Ileum (drug effects)
  • Inhibitory Concentration 50
  • Male
  • Muscle Contraction (drug effects)
  • Phthalazines (pharmacology)
  • Phytotherapy
  • Plant Extracts (administration & dosage, pharmacology, therapeutic use)
  • Trachea (drug effects)

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