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.
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Authors | Josiane Sabbadini Neves, Luciana Pontes Coelho, Renato Sérgio Balão Cordeiro, Marcia Paranho Veloso, Patricia Machado Rodrigues e Silva, Marcelo Henrique dos Santos, Marco Aurélio Martins |
Journal | Planta medica
(Planta Med)
Vol. 73
Issue 7
Pg. 644-9
(Jun 2007)
ISSN: 0032-0943 [Print] Germany |
PMID | 17562491
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- 7-epiclusianone
- Allergens
- Anti-Allergic Agents
- Benzophenones
- Benzoquinones
- Phthalazines
- Plant Extracts
- benzophenone
- azelastine
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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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