Evaluation of the gastrointestinal anti-motility effect of Anacardium occidentale stem bark extract:A mechanistic study of antidiarrheal activity  

作　　者：Blessing O.Omolaso Francis S.Oluwole Olugbenga A.Odukanmi Julius K.Adesanwo Ahmed A.Ishola Kayode E.Adewole 

机构地区：[1]Department of Physiology,Faculty of Basic Medical Sciences,University of Medical Sciences,Ondo City,340001,Ondo State,Nigeria [2]Department of Physiology,College of Medicine,University of Ibadan,Ibadan,200001,Nigeria [3]Department of Chemistry,Obafemi Awolowo University,Ile-Ife,230001,Osun State,Nigeria [4]Central Research Laboratories Limited,University Road Ilorin,Kwara State,240001,Nigeria [5]Department of Biochemistry,Faculty of Basic Medical Sciences,University of Medical Sciences,340001,Ondo State,Nigeria

出　　处：《Journal of Pharmaceutical Analysis》2021年第6期776-782,共7页药物分析学报（英文版）

摘　　要：Diarrhea is a prevalent gastrointestinal problem associated with fatal implications.It is a huge public health concern that requires better alternatives to current drugs.This study investigated the mechanisms involved in the antidiarrheal activity of Anacardium occidentale(Ao) stem bark extract,a plant commonly used in the management of diarrhea in Nigeria.Methanolic stem bark extract of the plant was partitioned into three fractions:hexane fraction,ethyl acetate fraction(Ao EF) and methanol fraction.In vitro studies on the effect of these fractions on guinea pig ileum(GPI) strips,as well as the modulatory effect of Ao EF on standard agonists-and antagonists-induced GPI contraction and relaxation,revealed Ao EF as the most active fraction.In vivo studies to assess the effect of Ao EF on the dopaminergic,muscarinic,and serotonergic pathways were carried out using gastric emptying(GE) and gastrointestinal transit(GT) as experimental end points.Ao EF was subjected to GC-MS analysis,while the identified compounds were docked with the muscarinic acetylcholine receptor M3(CHRM3) using Autodock Vina.Results indicated that Ao EF inhibited GE and GT via inhibition of CHRM3.In addition,GC-MS analysis revealed the presence of 24 compounds in Ao EF,while docking indicated that octadecanoic acid 2-(2-hydroxylethoxy)ethyl ester exhibited the highest binding affinity to CHRM3.This study indicated that the antidiarrheal activity of Ao is through its antimotility effect via the inhibition of the muscarinic pathway.And since none of the identified compounds exhibited higher binding affinity to CHRM3 relative to loperamide,the antimotility activity of these phytoconstituents may be via synergism.

关 键 词：Anacardium occidentale ANTIDIARRHEAL Muscarinic receptor Gastric emptying Gut motility GC-MS analysis 

分 类 号：R285[医药卫生—中药学]