Antifungal activity and antidiarrheal activity via antimotility mechanisms of (-)-fenchone in experimental models

(-)-小茴香酮在实验模型中通过抗运动机制发挥抗真菌和止泻作用

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作者:Michelle Liz de Souza Pessoa, Leiliane Macena Oliveira Silva, Maria Elaine Cristina Araruna, Catarina Alves de Lima Serafim, Edvaldo Balbino Alves Júnior, Alessa Oliveira Silva, Matheus Marley Bezerra Pessoa, Hermes Diniz Neto, Edeltrudes de Oliveira Lima, Leônia Maria Batista

Aim

To investigate antidiarrheal activity related to gastrointestinal motility, intestinal secretion and antimicrobial activity.

Background

(-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species, such as Foeniculum vulgare and Peumus boldus, used to treatment of gastrointestinal diseases. Pharmacological studies report its anti-inflammatory, antioxidant, and antinociceptive activity.

Conclusion

The antidiarrheal effect of (-)-fenchone in this study involves antimotility effect and not involve antisecretory mechanisms. (-)-Fenchone presents antifungal activity; however, it did not show antibacterial activity.

Methods

A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity. Intestinal transit and gastric emptying protocols were used to assess a possible antimotility effect. Muscarinic receptors, presynaptic α2-adrenergic and tissue adrenergic receptors, KATP channels, nitric oxide were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms. The antimicrobial activity was evaluated in the minimum inhibitory concentration model, the fractional inhibitory concentration index using the (-)-fenchone association method with standard antifungal agents.

Results

(-)-Fenchone (75, 150 and 300 mg/kg) showed antidiarrheal activity, with a significant decrease in the evacuation index. This activity is possibly related to a percentage of reduced intestinal transit (75, 150 and 300 mg/kg). The antimotility effect of (-)-fenchone decreased in the presence of pilocarpine, yohimbine, propranolol, L-NG-nitroarginine methyl ester or glibenclamide. In the enteropooling model, no reduction in intestinal fluid weight was observed. (-)- Fenchone did not show antibacterial activity; on the other hand, inhibits the growth of strains of fungi with a minimum fungicide concentration of 32 μg/mL. However, when it was associated with amphotericin B, no synergism was observed.

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