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

World J Gastroenterol. 2020 Nov 21;26(43):6795-6809. doi: 10.3748/wjg.v26.i43.6795.

Abstract

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.

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

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.

Keywords: (-)-Fenchone; Antifungal; Diarrhea; Monoterpenes; Motility.

MeSH terms

  • Antidiarrheals* / pharmacology
  • Antidiarrheals* / therapeutic use
  • Antifungal Agents* / pharmacology
  • Antifungal Agents* / therapeutic use
  • Camphanes
  • Diarrhea / chemically induced
  • Diarrhea / drug therapy
  • Gastrointestinal Motility
  • Humans
  • Models, Theoretical
  • Norbornanes
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use

Substances

  • Antidiarrheals
  • Antifungal Agents
  • Camphanes
  • Norbornanes
  • Plant Extracts
  • fenchone