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| 1 | Mangiferin,a natural xanthone,accelerates gastrointestinal transit in mice involving cholinergic mechanism显示文摘AIM:To investigate the effects of mangiferin on gastrointestinal transit(GIT) in normal and constipated mice,together with the possible mechanism.METHODS:Intragastrically-administered charcoal mealwas used to measure GIT in overnight starved Swiss mice.In the first experiments,mangiferin(3 mg/kg,10 mg/kg,30 mg/kg,and 100 mg/kg,po) or tegaserod(1 mg/kg,ip) were administered 30 min before the charcoal meal to study their effects on normal transit.In the second series,mangiferin(30 mg/kg) was tested on delayed GIT induced by several different pharmacological agonists(morphine,clonidine,capsaicin) or antagonists(ondansetron,verapamil,and atropine) whereas in the third series,mangiferin(30 mg/kg,100 mg/kg and 300 mg/kg) or tegaserod(1 mg/kg) were tested on 6 h fecal pellets outputted by freely fed mice.The ratio of wet to dry weight was calculated and used as a marker of fecal water content.RESULTS:Mangiferin administered orally significantly(P < 0.05) accelerated GIT at 30 mg/kg and 100 mg/kg(89% and 93%,respectively),similarly to 5-hydroxytryptamine4(5-HT4) agonist tegaserod(81%) when compared to vehicle-treated control(63%).Co-administered mangiferin(30 mg/kg) totally reversed the inhibitory effect of opioid agonist morphine,5-HT3-receptor antagonist ondansetron and transient receptor potential vanilloid-1 receptor agonist capsaicin on GIT,but only to a partial extent with the GIT-delay induced by 2-adrenoceptor agonist clonidine,and calcium antagonist verapamil.However,co-administered atropine completely blocked the stimulant effect of mangiferin on GIT,suggesting the involvement of muscarinic acetylcholine receptor activation.Although mangiferin significantly enhanced the 6 h fecal output at higher doses(245.5 ± 10.43 mg vs 161.9 ± 10.82 mg and 227.1 ± 20.11 mg vs 161.9 ± 10.82 mg of vehicle-treated control,at 30 and 100 mg/kg,P < 0.05,respectively),the effect of tegaserod was more potent(297.4 ± 7.42 mg vs 161.9 ± 10.82 mg of vehicle-treated control,P < 0.05).Unlike tegaserod,which showed an enhanced water content in fecal pellets(59.20% ± 1.09% vs 51.44% ± 1.19% of control,P < 0.05),mangiferin evidenced no such effect,indi-cating that it has only a motor and not a secretomotor effect.CONCLUSION:Our data indicate the prokinetic action of mangiferin.It can stimulate the normal GIT and also overcome the drug-induced transit delay,via a cholinergic physiological mechanism. | Talita Cavalcante Morais Synara Cavalcante Lopes Karine Maria Martins Bezerra Carvalho Bruno Rodrigues Arruda Francisco Thiago Correia de Souza Maria Teresa Salles Trevisan Vietla Satyanarayana Rao Flávia Almeida Santos | 2012 | World Journal of Gastroenterology2012，18，25： | 3 |
| 2 | Evaluation of the gastrointestinal anti-motility effect of Anacardium occidentale stem bark extract:A mechanistic study of antidiarrheal activity显示文摘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. | Blessing O.Omolaso Francis S.Oluwole Olugbenga A.Odukanmi Julius K.Adesanwo Ahmed A.Ishola Kayode E.Adewole | 2021 | Journal of Pharmaceutical Analysis2021，11，6： | 0 |
| 3 | Elenoside increases intestinal motility显示文摘AIM: To study the effects of elenoside, an arylnaph- thalene lignan from Justicia hyssopifolia , on gastro- intestinal motility in vivo and in vitro in rats. METHODS: Routine in vivo experimental assessments were catharsis index, water percentage of boluses, intestinal transit, and codeine antagonism. The groups included were vehicle control (propylene glycol-ethanol- plant oil-tween 80), elenoside (i.p. 25 and 50 mg/kg), cisapride (i.p. 10 mg/kg), and codeine phosphate (intragastric route, 50 mg/kg). In vitro approaches used isolated rat intestinal tissues (duodenum, jejunum, and ileum). The effects of elenoside at concentrations of 3.2 x 10-4, 6.4 x 10-4 and 1.2 x 10-3 mol/L, and cisapride at 10-6 mol/L were investigated. RESULTS: Elenoside in vivo produced an increase in the catharsis index and water percentage of boluses and in the percentage of distance traveled by a suspension of activated charcoal. Codeine phosphate antagonized the effect of 25 mg/kg of elenoside. In vitro, elenoside in duodenum, jejunum and ileum produced an initial decrease in the contraction force followed by an increase. Elenoside resulted in decreased intestinal frequency in duodenum, jejunum, and ileum. The in vitro and in vivo effects of elenoside were similar to those produced by cisapride. CONCLUSION: Elenoside is a lignan with an action similar to that of purgative and prokinetics drugs. Elenoside, could be an alternative to cisapride in treatment of gastrointestinal diseases as well as a preventive therapy for the undesirable gastrointestinal effects produced by opioids used for mild to moderate pain. | E Navarro SJ Alonso R Navarro J Trujillo E Jorge | 2006 | World Journal of Gastroenterology2006，12，44： | 0 |
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