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 IC₅₀ values (2.3 ± 1.1 μM and 3.3 ± 1.2 μM, 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 (IC₅₀ = 6.3 ± 0.2 nM and 3.7 ± 0.1 μM, 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.

Key words

Polyprenylated benzophenones - allergy - anaphylaxis - ileum contraction - Garcinia brasiliensis - Clusiaceae

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