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

作　　者：Michelle Liz de Souza Pessoa Leiliane Macena Oliveira Silva Maria Elaine Cristina Araruna Catarina Alves de Lima Serafim Edvaldo Balbino Alves Junior Alessa Oliveira Silva Matheus Marley Bezerra Pessoa Hermes Diniz Neto Edeltrudes de Oliveira Lima Leonia Maria Batista 

机构地区：[1]Department of Pharmaceutical Sciences,IPeFarM,Federal University of Paraiba,Joao Pessoa 58051-970,Paraiba,Brazil [2]Health Sciences Center,Federal University of Paraiba,JoaoPessoa 58051-970,Paraiba,Brazil [3]Postgraduate Program in Natural and Synthetic Bioactive Products,Universidade Federal da Paraiba,João Pessoa 58051-900,Brazil

出　　处：《World Journal of Gastroenterology》2020年第43期6795-6809,共15页世界胃肠病学杂志（英文版）

摘　　要：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 32μg/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.

关 键 词：(-)-Fenchone MONOTERPENES DIARRHEA MOTILITY ANTIFUNGAL 

分 类 号：R285[医药卫生—中药学]