Search

Loperamide is a well-known peripherally acting opiate used for the treatment of diarrhoea. To gain more knowledge on the structure-activity relationships of antidiarrhoeal drugs and to develop new active molecules, a series of aryl-cyano-piperidinoalkyl-thiazolidinones related to Loperamide was synthesized and screened for antidiarrhoeal activity in mice by castor oil test. To characterize the potency and toxicity of the synthesized compounds ED50 and LD50 values were also determined. The thiazolidinones 2-6 displayed antidiarrhoeal activity at doses ranging between 15 and 82 mg/kg. Although the results show that the synthesized compounds are 15- to 80-fold less active respect to the reference compound, Loperamide, they are much less toxic (> or = 1000 mg/kg and 108.9 mg/kg, respectively). Besides, to evaluate the involvement of opioid receptors in antidiarrhoeal activity, Naloxone was administered prior to test the 2-phenyl-3-{2-[(4-phenyl-4-cyano)piperidino]ethyl}-1,3-thiazolidin-4-one (2), the more active compound of this series. The results obtained by this study, suggest that the antidiarrhoeal activity of this series of thiazolidinone derivatives could involve the opioid receptors.

Medicinal plants have been used as traditional treatments for numerous human diseases for thousands of years. Diarrhoeal diseases continue to be a major cause of morbidity and mortality throughout the world and there is renewed interest in the discovery of novel compounds that can be used to fight these diseases. Numerous studies have validated the traditional use of antidiarrhoeal medicinal plants by investigating the biological activity of extracts of such plants, which have antispasmodic effects, delay intestinal transit, suppress gut motility, stimulate water adsorption or reduce electrolyte secretion. Of the numerous phytochemicals (such as alkaloids, tannins, flavonoids and terpenes) present in active extracts, tannins and flavonoids are thought to be responsible for antidiarrhoeal activity by increasing colonic water and electrolyte reabsorption. Others act by inhibiting intestinal motility. As some of the active ingredients are potentially toxic, there is a need to evaluate the safety of plant preparations. A few clinical trials have evaluated the safety and tolerability of traditional and herbal medicine preparations used to treat diarrhoea and generally indicate that minimal side effects are observed. However, with the increased popularity of plant-derived and herbal medicines in Western society, the benefits and potential dangers of these medicines must be considered.

International audience; Crude decoction, aqueous and ethanolic extracts of two medicinal plants (Psidium guajava and Diospyros mespiliformis), widely used in the central plateau of Burkina Faso to treat many diseases were evaluated for their antagonistic effects on caffeine induced calcium release from sarcoplasmic reticulum of rat skeletal muscle cells. These different extracts showed a decrease of caffeine induced calcium release in a dose dependent manner. Comparison of the results showed that Psidium guajava leaf extracts are more active than extracts of Diospyros mespiliformis and that crude decoctions show better inhibitory activity. The observed results could explain their use as antihypertensive and antidiarrhoeal agents in traditional medicine, by inhibiting intracellular calcium release.

Berberine is a benzyl tetra isoquinoline alkaloid which is widely used as an antimicrobial and an antidiarrhoeal. As berberine containing plants are virtually used in all forms of traditional medicine, our study aimed to examine the antioxidant activity of berberine using 2,2-diphenyl 1-picrylhydrazyl (DPPH) radical scavenging, nitric oxide scavenging, lipid peroxidation, superoxide scavenging, iron chelating activity and 2,2-azino bis(3-ethylbenzothiazoline-6-sulfonate) (ABTS) radical scavenging methods. The IC(50) values for all the models were calculated by regression analysis. In all the models tested, berberine showed its ability to scavenge the free radicals in a concentration dependent manner. The present study thereby justifies the therapeutic potential of berberine.

Aqueous extract of antidiarrhoeal formulation (ADF) containing Holarrhena antidysentrica, Aegle marmelos and Punica granatum was investigated for antidiarrhoeal activity against charcoal-induced gut transit, serotonin-induced diarrhoea and small intestine enteropooling in rats. The control, standard and test groups of experimental animals were administered with normal saline (p.o.), diphenoxylate hydrochloride (5 mg/kg, p.o.) and ADF (250 mg and 500 mg/kg, p.o.) respectively except the control group of small intestine enteropooling which received only 5% ethanol in normal saline (i.p.). Charcoal (10 ml/kg, p.o.) and serotonin were administered after 30 min, while was administered immediately afterwards. The distance traveled by charcoal in small intestine was measured after 15 and 30 min of charcoal administration, diarrhoea was observed every 30 min for six hour after serotonin administration and the volume of intestinal fluid was measured after 30 min of administration. Oral administration of ADF significantly inhibited the frequency of defaecation and decreased the propulsion of charcoal meal through the gastrointestinal tract, reduced the wetness of faecal dropping in serotonin-induced diarrhoea and also reduced the small intestine enteropooling. ADF may have potential to reduce the diarrhoea in rats.

Diarrhoea is a public health problem in developing countries. It is therefore important and useful to identify plants with antidiarrhoeal activity. Alchornea cordifolia is quoted by many traditional healers as a plant with this activity. The antidiarrhoeal activity of its leaf extract was investigated against castor oil induced diarrhoea in mice, using morphine as the standard reference drug. A significant (p < 0.01) dose related (100 mg/kg, 200 mg/kg, 400 mg/kg, 800 mg/kg) antidiarrhoeal activity of A. cordifolia leaf ethanol extract was observed with 800 mg/kg extract being the most effective. It delayed mouse intestinal transit accelerated by castor oil, inhibited the production of diarrhoeal faeces and modified the fluid and electrolyte transport across the colonic mucosa when administered intraluminally. Phytochemical screening revealed the presence of tannins and flavonoids which may account for the increased colonic water and electrolyte reabsorption, a mechanism suggested for the antidiarrhoeal activity of A. cordifolia. Copyright © 2004 John Wiley & Sons, Ltd.

Severe diarrhoea after chemotherapy is a dose-limiting toxicity of first-line chemotherapeutic agents approved for the treatment of colorectal cancer including 5-fluorouracil + leucovorin (5-FU/LV) and irinotecan (CPT-11). This report explores the potential of the long-acting version of the somatostatin analogue octreotide, for secondary prophylaxis in patients suffering from chemotherapy-induced diarrhoea (CID). A case series of three patients in a general community setting with colorectal cancer and severe refractory diarrhoea after fluoropyrimidine or irinotecan therapy resulting in suspension of chemotherapy, hospitalization, and/or refusal of further treatment. After the failure of initial aggressive antidiarrhoeal therapy with loperamide and/or diphenoxylate-atropine, patients were treated with octreotide LAR (30 mg q28d). The ability of octreotide LAR to resolve diarrhoea, prevent further episodes of grade 3 or 4 gastrointestinal toxicity and prevent costly hospitalizations. Octreotide LAR 30 mg q28d speed resolution of diarrhoea and was able prevent further episodes during subsequent cycles of chemotherapy. One patient who initially refused chemotherapy because of CID was able to complete his treatment. All patients reported improvement in quality of life following resolution of diarrhoea with octreotide LAR and no further hospitalizations because of CID were necessary.

The efficacy of Arque-Ajeeb (AA), a compound formulation of Unani medicine was investigated for antidiarrhoeal activity against barium sulphate-induced gut motility and castor oil-induced diarrhoea in rats. The control, standard and test groups of experimental animals were administered with distilled water (p.o.), lomotil (p.o.) and AA (0.007 ml and 0.014 ml/100 g, p.o.) respectively. Barium sulphate and castor oil were administered after 15 and 60 min respectively in each group of first and second experiment. The distance traveled by barium sulphate in small intestine was measured after 15 and 30 min of barium sulphate administration and diarrhoea was observed every 30-min for six hour after castor oil administration. Oral administration of AA caused significant reduction in diarrhoea. AA may have the potential to reduce the diarrhoea in rats.

The antidiarrhoeal effects of the methanol extract of Zizyphus spina-christi stem bark were evaluated in laboratory rodents. Studies on castor oil induced diarrhoea, intraluminal fluid accumulation, and gastrointestinal transit time were carried out. Results obtained revealed that the extract caused a dose dependent protection of rats against castor oil induced diarrhoea, decreased the intraluminal fluid accumulation and gastrointestinal transit. The intraperitoneal and oral LD(50) values were found to be 346+/-5.6 and 1200+/-41.2 mg/kg in mice. Preliminary phytochemical screening revealed the presence of glycosides, resins, saponins, and tannins. It is suggested that the extract may contain biologically active components that may be useful against diarrhoea, thereby justifying its use in ethnomedical practice as an antidiarrhoeal agent.

The effect of a hot water extract of black tea (Camellia sinensis (L.) O. Kuntze, Theaceae) on upper gastrointestinal transit and on diarrhoea was investigated employing conventional rodent models of diarrhoea. Black tea extract was found to possess antidiarrhoeal activity in all the models of diarrhoea used. Naloxone (0.5 mg/kg i.p.) significantly inhibited the antidiarrhoeal activity of the extract as well as loperamide, thus indicating a role of the opioid system in the antidiarrhoeal activity of the extract.

The partitioned n-hexane, ethylacetate and residual methanol extracts of the root of Rumex maritimus were evaluated for antidiarrhoeal activity in mice using castor oil and serotonin induced diarrhoea and also charcoal motility test at 50, 100 and 200 mg/kg body weight dose. Among these, the methanol extract most significantly prolonged the time for induction of diarrhoea, reduced the frequency of diarrhoeal episodes and also decreased the propulsion of charcoal meal through the gastrointestinal tract.

Acorus calamus is a herb used for the appetite and as an aid to the digestion. It is used for fevers, stomach cramps and cholic. Their rhizomes were used for toothache and powdered rhizome for congestion. The rhizome part is also used to treat several diseases like asthma and bronchitis and as sedative. Native tribes treated cough by making a decoction of the plant as a carminative and also for cholic. It is a main medhya drug, which has the property of improving the memory power and intellect. Acorus calamus is used in the conditions of vata and kapha, stomatopathy, hoarseness, flatulence, dyspepsia, helminthiasis, amenorrhea, dysmenorrheal, nephropathy, calculi, stragury. Acorus calamus leaves, rhizomes and its essential oil has many biological activities16 like antispasmodic, carminative and also used for treatment of epilepsy, mental ailments, chronic diarrhea, dysentery, bronchial catarrh, intermittent and tumors. It also has the insecticidal, antifungal, antibacterial, tranquilizing, antidiarrhoeal, antidyslipidemic, neuroprotective, antioxidant, anticholinesterase, spasmolytic, vascular modulator activities. The parts used in most of the experimental studies are the leaves, roots and stem of the plant. The dry rhizome contains some of the yellow aromatic oil, calamus oil that are responsible for their medicinal and insecticidal properties. Studies were also done on their rhizome part and in its oils in order to identify the active constituents and its medicinal values.

The Anti-diarrhoeal effect of the aqueous extract of the aerial parts of in rosents was examined. At the doses of 125, 250, 500 mg/kg of the extract protected rats, in a dose increasing fashion against diarrhea promoted by castor oil dropping by38.09, 59.93 and 65.11% respectively. Further, it has significantly inhibited by 41.46% the gastrointestinal transit of charcoal in rats at 500 mg/kg dose of the extract. These data suggest that Peucedanum pastinacifolium shows antidiarrhoeal activity by inhibiting intestinal motility with no signs of acute toxicity which is correlated to its uses in folkloric medicine

Nigeria is naturally blessed with both savannah and tropical rainforests vegetation and these offer a wide distribution of plants believed to possesses secondary metabolites which are responsible for treating or curing various diseases. Several researches have been carried out in order to explore and identify the chemical compositions responsible for various pharmacological activities in Nigerian medicinal plants. This paper discussed the meaning and historical development of medicinal plants. A brief account of phytochemicals (alkaloids and flavonoids) were also given. The plants presented in this paper confirmed the pharmacological activities of these plants and includes; anticonvulsant, antioxidant, antibacterial, anxiolytic, antiinflammatory, antiulcer, anticancer, antiplasmodial, antitrypanosomal, antithypoid, antitumor, antileishmanial, antidiarrhoeal, antidiabetic, antituberculosis, analgesic as well as others.

India possesses a rich biodiversity of the medicinal plants that were still not explored completely. In the present review, an attempt has been made to congregate the detailed Pharmacognostical and Pharmacological importance of Cicer arietinum Linn (Leguminosae). Morphoanatomy of the root part, physicochemical, morphological, histological parameters, traditional and pharmacological studies of Cicer arietinum Linn and the plant posses’ anti-inflammatory activity, anti-microbial activity, anti-oxidant activity, anti-pyretic, anticonvulsant, antidiarrhoeal, antihyperglycaemic, hemolytic activity etc. The roots and seeds of Cicer arietinum Linn contain several medicinal properties. This review will be definitely helpful for the researchers as well as the clinicians dealing with Cicer arietinum to know its proper usage, as the plant appears to be highly valuable due to its pharmacological and medicinal properties and can possibly help to differentiate the drug from its other species.

The aim of this study is to assess the self-medication practice among dental students. MATERIALS AND METHOD: The descriptive cross-sectional questionnaire-based study was conducted among 100 patients reporting to the Saveetha Dental college.The patients were requested to answer the questionnaire. Datas were collected and analysed. BACKGROUND: Self-medication is universal phenomenon and it is widely practiced worldwide and often considered as a use of self-care.Self Medication means taking drugs without the advice of a physician and getting treatment. RESULTS: Findings revealed that 58% Respondent claimed to be involved in self medication.Drugs or drug groups commonly used for self-medication included analgesics (38%) followed by antibiotics (17%), antipyretics (15%), antidiarrhoeal (13%), antihistamines and antacids (6%) and vitamin tablets (5%). The disease for which self medications were commonly used were cough and common cold (35%) followed by fever (30%), diaarhoea (10%), allergy (8%), headache (6%), nausea and vomiting (7%) and ulcers (4%). 69 % had no side effects and 31% had side effects

Objective To evaluate the antidiarrhoeal effect of alcoholic extract of Rotula aquatica by using different experimental models.

The folkloric claim ofMusa paradisiacasap in the management of diarrhoea is yet to be substantiated or refuted with scientific data. Therefore, the aim of the current study was to screen the sap ofM. paradisiacafor both its secondary metabolites and antidiarrhoeal activity at 0.25, 0.50, and 1.00 mL in rats. Secondary metabolites were screened using standard methods while the antidiarrhoeal activity was done by adopting the castor oil-induced diarrhoeal, castor oil-induced enteropooling, and gastrointestinal motility models. The sap contained flavonoids, phenolics, saponins, alkaloids, tannins, and steroids while cardiac glycosides, anthraquinones, triterpenes, cardenolides, and dienolides were not detected. In the castor oil-induced diarrhoeal model, the sap significantly (P<0.05) prolonged the onset time of diarrhoea, decreased the number, fresh weight, and water content of feaces, and increased the inhibition of defecations. Na+-K+-ATPase activity in the small intestine increased significantly whereas nitric oxide content decreased. The decreases in the masses and volumes of intestinal fluid by the sap were accompanied by increase in inhibition of intestinal fluid content in the enteropooling model. The sap decreased the charcoal meal transit in the gastrointestinal motility model. In all the models, the 1.00 mL of the sap produced changes that compared well with the reference drugs. Overall, the antidiarrhoeal activity ofMusa paradisiacasap attributed to the presence of alkaloids, phenolics, flavonoids, and/or saponins which may involve, among others, enhancing fluid and electrolyte absorption throughde novosynthesis of the sodium potassium ATPase and/or reduced nitric oxide levels.

Mangroves being stress tolerant plants possess unique metabolites with significant amount of bioactive compounds which could be isolated and evaluated for possible drug development with suitable biotechnology tools. The mangrove genus Xylocarpus comprises of four species viz. Xylocarpus granatum (Koenig), X. moluccensis (lamk.) and X. mekongensis Pierre and X. rumphii. However, X. rumphii is a less abundant mangrove plant. There have been reports that different species of Xylocarpus are used ethnomedicinallly for treatment of various diseases such as fever, malaria, cholera, diarrhoea, swelling of breast, elephantiasis, inflammation, dyslipidemia, pain, hyperglycaemia etc. Recent studies revealed that the extracts from different parts of the plant such as leaves, stem, bark and fruits possess phytoconstituents like alkaloids, glycosides, steroids, limnoids, terpenoids, flavonoids, tannins and other phenolics. Further, it has been established that the different solvent extracts of the plants have exhibited antimicrobial and antidiarrhoeal activities against a number of human pathogens which could be correlated to their phytoconstituents such as flavonoids, alkaloids, limnoids, tannins etc. The present study is aimed at compiling information on phytochemical, pharmacological and ethnomedicinal properties of mangrove plants of genus Xylocarpus, with a view to critically assess the legitimacy of the use of these plants for antimicrobial and antidiarrhoeal activities as well as providing directions for further research.

The phytochemical screening, extraction and antimicrobial analysis of the crude extracts from the seeds and pods of Acacia nilotica Linn, the roots of Uvaria afzelii Sc and Terminalia avicennioides Guill & Perr were carried out using standard methods. The results of the phytochemical screening showed that the plants contained saponins, flavonoids, phenols, tannins, terpenoids and triterpenoids. The results of the antibacterial screening showed that the ethyl acetate extract of Acacia nilotica Linn exhibited the highest activities against the test microbes with zones of inhibition diameter ranging from 27-32 mm. It was closely followed by the ethyl acetate extract of Terminalia aviccenoides with zones of inhibition diameter ranging from 25-30 mm and finally, the ethyl acetate extract of Uvaria afzelii with zones of inhibition ranging from 24-29 mm. The results of Minimum Inhibitory Concentration (MIC) showed that the extracts of the plants gave MIC values at a concentration of 800, 700, 600 μg/cm3 against Escherichia coli, Vibro cholerea, Shigella dysentriae and Salmonella enteritidis respectively. The Minimum Bactericidal Concentration (MBC) values occur at the same concentration against the same microbes. The results of this study showed that the ethylacetate extract of the seeds and pods of Acacia nilotica was the most active against diarrhoea causing organisms and may be a potential source of a broad spectrum antibiotic for the treatment of diarrhoea.

This article has been withdrawn at the request of editor. The Publisher apologizes for any inconvenience this may cause. The full Elsevier Policy on Article Withdrawal can be found at http://www.elsevier.com/locate/withdrawalpolicy .

Gmelina arborea (G. arborea) is a bio-prospective plant belonging to family verbenaceae. It is widely used for it’s medicinal properties from ancient times. The present paper comprehensively reviewed the traditional uses, medicinal properties and chemical constituents isolated from G. arborea based on literature reported as well as critical analysis of the research. The present article is aimed to provide information on recent advances and new foundations and direction for further exploring G. arborea for its applications. Pharmacological research reviewed that G. arborea possess various medicinal properties and biological activities including antidiuretic, antidiarrhoeal, antipyretic, antianalgesic, antioxidant, antidiabetic, antihelmintic, antibacterial, antifungal, cardiopotective, insecticidal, antiulcer, gastro-protective, anticancer, antihyperlipidemic and immunomodulatory activity. It has been reported for its applications in treatment of bone fracture, hypertension and regeneration of β-cells. The main chemical constituents of G. arborea include lignans, iridoid glycoside, flavonoids, flavons, flavone glycoside and sterols. The present review provides all the references and beneficial directions to explore further application of G. arborea.

The antidiarrhoeal activity of the methanol extract of the dried seeds of Strychnos potatorum (MESP) has been evaluated out in rats using different models (castor oil-induced diarrhoea, effects on gastrointestinal motility and on PGE(2)-induced gastric enteropooling. MESP (100, 200 and 400 mg/kg, p.o.) significantly (P0.001) inhibited the frequency of defaecation and reduced the wetness of faecal droppings in castor oil-induced diarrhoea, decreased the propulsion of charcoal meal through the gastrointestinal tract, and also reduced the PGE(2)-induced enteropooling.

The antidiarrhoeal activity of the essential oil obtained from A. ludoviciana was analyzed. Nonanal was identified as the compound responsible for this biological effect. The pure compound was tested on castor oil-, magnesium sulfate-, arachidonic acid- and PGE 2 -induced diarrhoea in CD1 mice. In addition, its effect on the intestinal transit of Wistar rats stimulated by castor oil was studied. Nonanal showed a significant inhibitory effect on mice with diarrhoea induced with castor oil, MgSO 4 and arachidonic acid. However, with the PGE 2 -induced diarrhoea model, the effect was smaller. It also showed an important delayed the intestinal transit activity 30 min after its administration. The compound does not have a constipating effect because it does not showed any effect on normal defecation of mice. The nonanal isolated from A. ludoviciana showed symptomatic relief of induced diarrhoea.

The antidiarrhoeal activity of the seed extract of Albizzia lebbeck (Benth.) was investigated employing conventional rodent models of diarrhoea, i.e. castor oil-induced diarrhoea, upper gastrointestinal transit (u.g.t.) and fluid secretion. It was found that the aqueous methanol extract of Albizzia lebbeck seeds (2.5-5 mg/kg i.p.) possessed antidiarrhoeal activity which strengthens the earlier use of the seeds in the treatment of diarrhoea and dysentery. The antidiarrhoeal dose of the extract was at least 10-30 times less than the LD(50) dose. The extract (2.5-5 mg/kg i.p.) potentiated the antidiarrhoeal activity of loperamide (1 mg/kg i.p.). Nalaxone (0.5 mg/kg i.p.) significantly inhibited the antidiarrhoeal activity of the extract as well as loperamide, thus indicating a role of the opioid system in the antidiarrhoeal activity of the extract.

The excessive production of reactive oxygen species in nervous tissues is considered one of the major risk factors of neurodegenerative diseases. During the last two decades, much attention has been paid to the antioxidant and anti-inflammatory activity of natural products and compounds isolated from natural products which are often characterized by high efficacy and low adverse effects. Berberine is an isoquinoline alkaloid, widely present in different medicinal herbs, especially in the genus Berberis. It is mainly used as antidiarrhoeal, antibacterial, antifungal, and antiprotozoal agent. However, current research has focused on its beneficial role in neurodegenerative diseases, mainly due to its powerful antioxidant effect. The therapeutic potential of Berberine in different neurodegenerative diseases such as Alzheimer, Parkinson and Huntington disease has been brought to evidence by numerous studies. However, a limited number of reviews focus on the beneficial role of Berberine against neurodegeneration. The main objective of this review is to discuss the role of oxidative stress in neurodegeneration and the potential role of antioxidant compounds, in particular Berberine which is analyzed in its chemical structure, source, bioavailability, therapeutic potential, with special attention to its mechanism of action at a molecular level. © 2015 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Sp. z o.o. All rights reserved.

Background The fruit of Rosa moschata has traditionally been used for the treatment of abdominal spasm and diarrhoea. Therefore, the aim of this study was to investigate mechanism(s) responsible for its medicinal use in gut spasm and diarrhea. Methods Hydro-methanolic extract of Rosa moschata (Rm.Cr) was studied in isolated rabbit’s jejunal preparations for possible antispasmodic activity. Based upon in vitro relaxant activity in isolated gut preparations, in vivo antidiarrheal activity was carried out in mice to confirm its antidiarrheal effect. Acute toxicity study was performed to determine safe dose range before in vivo experiments. Results In isolated rabbits’ jejunal preparations, Rm.Cr inhibited the spontaneous and high K+-induced contractions with respective EC50 values of 0.66 (0.44-0.97; n = 5) and 2.28 mg/mL (1.43-3.62; n = 5), like that of verapamil. This suggests the presence of calcium channel blocking (CCB) activity as a possible mode of action. The Ca++ channel blocking activity was further confirmed when pre-treatment of isolated jejunums with Rm.Cr (1-5 mg/mL) caused a rightward shift in the Ca++ concentration-response curves (CRCs), similar to verapamil. Rm.Cr was safe up to 2000 mg/kg for in vivo acute toxicity. Rm.Cr provided 55% and 80% protection from diarrhoea in respective doses of 100 mg/kg and 1000 mg/kg. These data indicates that the crude extract of Rosa moschata possesses Ca++ antagonist-like constituent(s), which explains its inhibitory effect on gut motility; a mechanism that underlies its antidiarrheal and antispasmodic activities. Conclusion The study shows that the crude extract of fruits of Rosa moschata possesses antispasmodic effects mediated possibly through voltage gated Ca++ channel blockade, which provides sound pharmacological base to its medicinal use in gut spasms and diarrhoea, though additional mechanism(s) cannot be ruled out.

The antioxidant activity of Murraya koenigii (L.) Spreng (Family: Rutaceae), leaves was investigated in male wistar rats. Potassium dichromate was used to induce oxidative stress. The traditional medical literature describes its potential role as a source of many vitamins, flavonoids, phenols and domestic remedy for many human disorders. The whole plant is considered to be tonic, antidiarrhoeal, febrifuge, blood purifier and as stomachic. In the present study animals were divided into four groups Group I (Control), Group II (Potassium dichromate), Group III (Murraya koenigii + Potassium dichromate) and Group IV (Murraya koenigii). in vivo antioxidant activity of Murraya koenigii inhibited the toxicity of potassium dichromate. The GSH content in liver (1.79 +/- 0.019) and kidney (1.967 +/- 0.013) of Group IV rats significantly (p < 0.05) increased whereas, hepatic malondialdehyde content in liver (2.44 +/- 0.29) and kidney (2.34 +/- 0.057) was significantly (p < 0.05) reduced as compare to control. However, Chromate significantly (p < 0.05) decreased the reduced glutathione (GSH) content and increases hepatic malondialdehyde (MDA) content in both liver and kidney as compared to control. Further post treatment with Murraya koenigii (Group III) significantly (p

Background Traditionally, Operculina turpethum has been used in a wide range of ailments such as, gastrointestinal disturbances and asthma. It is found in China, South Asia, Pacific Islands, and Australia. This study was aimed to provide a possible pharmacological basis for the medicinal use of O. turpethum in gut and airways disorders. Methods Castor oil-induced diarrhoeal mice model and isolated tissue preparations such as, rabbit jejunum and guinea-pig tracheal preparations were used to test the antidiarrhoeal, antispasmodic and bronchodilator effects and the possible mode of action(s) of the 70% aqueous-ethanolic extract of O. turpethum black variety (OTB). Results In the castor oil-induced diarrhoea in mice, the crude extract of OTB caused a dose-dependent (300–1000 mg/kg) protection from diarrhoea, similar to that of loperamide. In isolated rabbit jejunum preparations, OTB produced a dose-dependent inhibition of spontaneous and high K+(80 mM)-induced contractions with resultant median effective concentrations (EC50 with 95% confidence interval) of 1.04 mg/ml (0.59-1.54) and 0.12 mg/ml (0.10-0.15; n = 4) respectively, thus showing more potency against K+. Pretreatment of the tissue with OTB (0.01 and 0.03 mg/ml) caused a rightward shift in the concentration response curves of Ca++, similar to that of verapamil. In isolated guinea-pig tracheal preparations, OTB caused inhibition of carbachol and high K+-induced constriction at similar concentrations with respective EC50 value of 0.66 mg/ml (0.53-0.82) and 0.59 mg/ml (0.45-0.62). Activity-directed fractionation revealed that the ethyl acetate fraction was more potent than the parent crude extract and hexane fraction. Conclusion These results suggest that the crude extract of O. turpethum possesses antidiarrhoeal, antispasmodic and bronchodilator activities, mediated possibly through the presence of Ca++ antagonist like constituent(s), though additional mechanism(s) cannot be ruled out. Thus, this study provides the evidence for the medicinal use of plant in diarrhoea and asthma.

Objective To scientifically validate the traditional substitution of roots of highly expensive Aconitum heterophyllum (AH) with rhizomes of Cryptocoryne spiralis (CS) in the treatment of diarrhoea. Methods Different fractions from root/rhizome extract of both the plant were subjected to faecal excretion rate and castor oil-induced diarrhoea models. Further, bioactive fractions from both plants, i.e. chloroform (CAH) from AH at 50 mg/kg p.o. and ethyl acetate (EACS) from CS at 100 mg/kg p.o., were examined for small intestinal transit, intestinal fluid accumulation and PGE2-induced enteropooling models in rats. Biochemical estimations and Na+ and K+ concentration in intestinal fluid were also determined along with antibacterial studies. Phytochemical standardisation of AH and CS was performed by quantifying aconitine for the former and stigmasterol for the latter using HPLC. Key findings CAH and EACS illustrated a significant reduction in faecal output rate and demonstrated a protection of 63.068% at CAH 50 and 59.090% at EACS 100 mg/kg p.o. in castor oil-induced diarrhoea model. The fractions also persuaded promising effects in all the other models, restored alterations in biochemical parameters and showed potential antibacterial activity. Conclusion The antidiarrhoeal potential of AH and CS may be attributed to an antimotility and antisecretory type of effect.

A study was undertaken to evaluate the effect of aqueous and methanolic plant extracts of Acorus calamus rhizome, Pongamia glabra leaves, Aegle marmelos unripe fruit and Strychnos nux-vomica root bark for their antidiarrhoeal potential against castor-oil induced diarrhoea in mice. The methanolic plant extracts were more effective than aqueous plant extracts against castor-oil induced diarrhoea. The methanolic plant extracts significantly reduced induction time of diarrhoea and total weight of the faeces. The result obtained establish the efficacy of these plant extracts as antidiarrhoeal agents.

Peppers are common food ingredients used worldwide. They are also added in traditional antidiarrhoeal formulations of different herbs. Piperine (1) is an alkaloidal constituent of black and long peppers recently established as a bioavailability enhancer of drugs and other substances. As a part of efforts to study its effects on the gastrointestinal tract, the experiments were performed to determine the rationale, if any, for its use in traditional antidiarrhoeal formulations. Antidiarrhoeal activity of 1 against castor oil, MgSO4 and arachidonic acid was studied in mice. It significantly inhibited diarrhoea produced by these cathartics at 8 and 32 mg/kg p.o. dose. Inhibition of castor oil induced enteropooling by 1 suggests its inhibitory effect on prostaglandins. The results validate the rationale for its use in traditional antidiarrhoeal formulations.

The aqueous (WE) and ethanol (EE) leaf extracts of Pentaclethra macrophylla were tested for antidiarrhoeal activity using experimental animal models. The i.p. LD50 values were established to be 770 mg/kg and 280 mg/kg for the aqueous (WE) and ethanol (EE) extracts, respectively. Antidiarrhoeal potential of the extracts was evidenced by a significant reduction in faecal output and protection from castor oil-induced diarrhoea in rats treated with the extracts. In addition the extracts significantly (p

Forty six aqueous extracts from 38 medicinal plant species belonging to different families were selected on the basis of their traditional medicinal use as antidiarrhoeic agents. They were submitted in a broad biological screening including antibacterial, antiamoebic and antispasmodic activities. The results of the testing have indicated that 37 extracts (80.43%), 33 (71.74%) and 32 (69.54%) exhibited some level of antibacterial, antiamoebic and antispasmodic activity respectively. Only 8 plant extracts (17.39%) would act as antidiarrhoeic agents by a triple pronounced antibacterial, antiamoebic and antispasmodic action. They include aqueous extracts from Euphorbia hirta whole plant, leaves of Psidium guajava and Tithonia diversifolia, root bark of Alchornea cordifolia, Heinsia pulchella, Paropsia brazzeana, Rauwolfia obscura and Voacanga africana.

The bark of M. urundeuva (Anacardiaceae) used in popular medicine as an antidiarrhoeal agent has been investigated for its effects on castor oil-induced diarrhoea and on intestinal motility. In rats, the ethanol extract of stem bark significantly inhibited the castor oil-induced diarrhoea, small intestinal transit and accumulation of fluid volume at an oral dose of 400mg/kg. Furthermore, the plant extract caused marked inhibition of the contractile responses evoked by acetylcholine and histamine on guinea-pig ileum in vitro. These results point to a possible antidiarrhoeic effect of M. urundeuva bark extract since inhibition of intestinal motility and secretion can greatly control clinical diarrhoea.

The antidiarrhoeal activity of the hexane, chloroform, methanol and aqueous extracts of Waltheria americana, Commelina coelestis and Alternathera repens, was tested on mice with diarrhoea induced by castor oil and MgSO4. The methanol extract of C. coelestis and A. repens and aqueous extract of A. repens, presented antidiarrhoeal effect, monitored by number of liquid feces defecated and intestinal transit of a suspension of graphite with castor oil in Wistar rats.

In children, the treatment of acute diarrhoea with the World Health Organization (WHO) standard oral rehydration solution (ORS) provides effective rehydration but does not reduce the severity of diarrhoea. In community practice, carob bean has been used to treat diarrhoeal diseases in Anatolia since ancient times. In order to test clinical antidiarrhoeal effects of carob bean juice (CBJ), 80 children, aged 4-48 months, who were admitted to SSK Tepecik Teaching Hospital with acute diarrhoea and mild or moderate dehydration, were randomly assigned to receive treatment with either standard WHO ORS alone or a combination of standard WHO ORS and CBJ. Three patients were excluded from the study because of excessive vomiting. In the children receiving ORS + CBJ the duration of diarrhoea was shortened by 45%, stool output was reduced by 44% and ORS requirement was decreased by 38% compared with children receiving ORS alone. Weight gain was similar in the two groups at 24 h after the initiation of the study. Hypernatraemia was detected in three patients in the ORS group but in none of those in the ORS + CBJ group. The use of CBJ in combination with ORS did not lead to any clinical metabolic problem. We therefore conclude that CBJ may have a role in the treatment of children's diarrhoea after it has been technologically processed, and that further studies would be justified.

BACKGROUND: A substantial number of patients with advanced HIV infection suffer from intractable diarrhoea. The aim of this study was to evaluate whether potent antiretroviral therapy could alleviate such diarrhoea. METHODS: In an open randomized study the effect of the HIV protease inhibitor indinavir in combination with nucleoside analogue reverse transcriptase inhibitors on chronic HIV-related diarrhoea was investigated in 14 late-stage (CD4+ lymphocyte count

The methanol extract of Cyperus rotundus rhizome, given orally at the doses of 250 and 500 mg/kg b.w., showed significant antidiarrhoeal activity in castor oil induced diarrhoea in mice. Among the fractions, tested at 250 mg/kg, the petroleum ether fraction (PEF) and residual methanol fraction (RMF) were found to retain the activity, the latter being more active as compared to the control. The ethyl acetate fraction (EAF) did not show any antidiarrhoeal activity.

Objective To investigate analgesic, antidiarrhoeal and cytotoxic activities of the ethanol extract of Passiflora foetida L. (Passifloraceae) by three experimental methods. Methods Analgesic activity of the ethanol extract of Passiflora foetida L. (EEPF) was carried out using acetic acid-induced writhing inhibition in mice. The method of castor oil-induced diarrhoea in mice was utilized to evaluate antidiarrhoeal activity. The cytotoxic activity of EEPF was explored with a brine shrimp lethality bioassay. Results The extract showed 68.75% and 30.00% inhibition of writhe at the doses of 500 and 250 mg/kg body weight, respectively. The extract increased the mean latent period prior to diarrhoeal onset to about 1.55 h and 1.17 h, and decreased the mean number of stools to 4.4 and 5.6 at the doses of 500 and 250 mg/kg body weight. The extract also demonstrated cytotoxic activity in the brine shrimp lethality assay, and the median lethal concentration for brine shrimp nauplii was 80 μg/mL. Conclusion The results suggest that the plant extract has analgesic and antidiarrhoeal activities, supporting its uses in traditional medicine. The results also demonstrate that the plant extract possesses cytotoxic activities.

Background: Plants of the family Combretaceae are amongst the most widely used plants for traditional medicinal purposes in southern Africa. In particular, many species of Combretum and Terminalia are used for their antibacterial, antifungal, antiprotozoal, antiviral, antidiarrhoeal, analgesic, antimalarial, antioxidant, anti-inflammatory and anticancer activities, yet their antimicrobial potential has not been rigorously studied and compared. Materials and Methods: A survey of antimicrobial activity was undertaken on selected South African Combretum and Terminalia species. Sixteen extracts from 6 Combretum and 2 Terminalia plant species with a history of medicinal usage were investigated by disc diffusion assay against a panel of bacteria and fungi and their MIC values were determined. Toxicity was determined using the Artemia franciscana nauplii bioassay. Results: All extracts tested displayed broad spectrum antibacterial activity, inhibiting the growth of 12-16 (75-100%) of the bacteria tested, with Gram-positive and Gram-negative bacteria being approximately equally susceptible. Potent antibacterial activities (generally in the range 200-5000 μg/ml) were evident for all Combretaceae extracts against both Gram-positive and Gram-negative bacteria. Similarly, the extracts also displayed good antifungal activity, inhibiting the growth of 2-3 (66.7-100%) of the fungal species tested, with fungal growth inhibition activities generally in the range 200-4000 μg/ml. In general, the Terminalia extracts had better efficacies than the Combretum extracts. Furthermore, the methanol extracts were generally better antimicrobial agents than the water extracts. All extracts were also shown to be non-toxic in the Artemia nauplii bioassay. Conclusion: The lack of toxicity of these extracts and their inhibitory bioactivity against a panel of bacteria and fungi indicate their potential as medicinal agents and partially validate their usage in multiple South African traditional medicinal systems.

Objective The aim of our study was to characterize the effect of P-317, a novel cyclic derivative of morphiceptin, on gastrointestinal (GI) motility and abdominal pain in mouse models mimicking symptoms of diarrhoea-predominant irritable bowel syndrome (IBS-D). Methods The effect of P-317 on mouse intestinal motility was characterized in vitro and in vivo in physiological and pathopysiological conditions. The antinociceptive action of P-317 was characterized in the mustard oil-induced abdominal pain model and the writhing test. Locomotor activity and grip-strength tests were used to evaluate the effect of P-317 in the central nervous system (CNS). To translate our study to clinical conditions, the semi-quantitative expression of μ-opioid receptors (MOP) and κ-opioid receptors (KOP) messenger RNA (mRNA) in human colonic samples from IBS-D patients was quantified. Key findings In vitro, P-317 (10−10–10−6 M) inhibited colonic and ileal smooth muscle contractions in a concentration-dependent, β-funaltrexamine and nor-binaltorphimine-reversible manner. In vivo, P-317 (0.1 mg/kg, i.p. and 1 mg/kg, p.o.) inhibited GI transit, displayed a potent antinociceptive action in abdominal pain tests and did not influence the CNS. Conclusion P-317 produced a potent analgesic and antidiarrhoeal action in the mouse GI tract after oral administration. Given lower expression of MOP and KOP mRNA in IBS-D patients, P-317 is a promising peptide-based drug candidate for IBS-D therapy.

Aim: The roots of Potentilla fulgens Wall. ex Hook. (Rosaceae) have been used in the indigenous system of medicine in Northeast India to treat diarrhoea. The aim of this study was to investigate the safety and protective effects of P. fulgens root extract in experimentally induced diarrhoea in mice. Methods: The protective effects of P. fulgens root extract was investigated against experimentally induced diarrhoea in mice, using four experimental models, i.e. measurement of faecal output, castor oil model, prostaglandin E2 (PGE2) enteropooling assay and gastrointestinal transit test. The safety assessment of root extract was done in mice on the basis of general signs and symptoms of toxicity, food water intake and mortality of animals following their treatment with various doses of extract (100 and ndash;3200 mg/kg). In addition, the serum glutamate oxaloacetate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), cholesterol and total protein of experimental mice were also monitored to assess the toxicity of root extract. Results: In the safety assessment studies, P. fulgens root extract did not showed any visible signs of toxicity, but mortality was observed in a single animal at 3200 mg/kg dose of extract. The extract also did not showed any adverse effects on the studied serum parameters of experimental animals. In the antidiarrhoeal tests, administration of 800 mg/kg dose of extract to mice showed 50% protection from diarrhoea evoked by castor oil. In addition, the extract also showed 29.27% reduction in PGE2-induced intestinal secretion as compared to 30.31% recorded for loperamide, a standard anti-diarrhoeal drug. Conclusions: The results of this study indicate that P. fulgens root extract possesses significant anti-diarrhoeal properties. Therefore, the roots of this plant can be an effective traditional medicine for the protection from diarrhoea. [J Intercult Ethnopharmacol 2014; 3(3.000): 103-108]

Tannins, a group of major active components of Chinese rhubarb and widely distributed in nature, have a significant antidiarrhoeal activity. Aquaporins (AQPs) 2 and 3 play important roles in regulating water transfer during diarrhoea. The present study aims to determine the effect of the total tannins extract of rhubarb on aquaporins (AQPs) 2 and 3 in diarrhoea mice and HT-29 cells both induced by magnesium sulphate (MgSO4). Our results showed that rhubarb tannins extract (RTE) significantly decreased the faecal water content in colon and evaluation index of defecation of diarrhoea mice. Interestingly, RTE could markedly reduce the mRNA and protein expression levels of AQPs 2 and 3 in apical and lateral mucosal epithelial cells in the colons of diarrhoea mice and HT-29 cells both induced by MgSO4in a dose-dependent manner. Furthermore, RTE suppressed the production of cyclic monophosphate- (cAMP-) dependent protein kinase A catalytic subunitsα(PKA C-α) and phosphorylated cAMP response element-binding protein (p-CREB, Ser133) in MgSO4-induced HT-29 cells. Our data showed for the first time that RTE inhibit AQPs 2 and 3 expressionin vivoandin vitrovia downregulating PKA/p-CREB signal pathway, which accounts for the antidiarrhoeal effect of RTE.

A survey was conducted in a sample of 29 pharmacies in the Badinh district of Hanoi, Vietnam, to determine the knowledge and behaviour of pharmacy staff in dealing with cases of acute diarrhoea in children. The survey found that antibiotics and antidiarrhoeal drugs were suggested in the majority of cases (45 per cent and 69 per cent, respectively) while oral rehydration salts (ORS) were suggested in only one case. In about 80 per cent of the observed cases in which antibiotics were supplied, one to four tablets were given, enough for only one to two days. The advice given by pharmacy staff to purchasers was poor. Only about half the pharmacy staff asked for information about the stool, age of the child and frequency of diarrhoea, while questions about medicines that had already been taken, feeding and health status were rarely asked. In about 10 per cent of the cases, no questions at all were asked. The mean cost of the treatment was $ 0.53 (95 per cent CI = 0.37–0.68). Constraints of knowledge, time and finance could be the reasons for this inappropriate management of childhood diarrhoea.

We set out to ascertain the role of tachykinins, neurokinin A and substance P, in castor oil-induced diarrhoea in rats as disclosed by the inhibitory effect of the non-peptide NK1- and NK2-receptor antagonists, SR 140333 and SR 48968, respectively. SR 48968 (0.02 to 20 μg kg−1, s.c. or p.o.), and the opioid receptor agonist loperamide (1–10 mg kg−1, p.o.), dose-dependently prevented castor oil effects: % inhibition vs castor oil, diarrhoea 0 to 100, increase in faecal mass 7 to 90 and water content 16 to 90. SR 140333 (0.02 to 20 μg kg−1, s.c.) and the platelet activating factor antagonist SR 27417 (5 to 500 μg kg−1, p.o.) did not prevent the increase in faecal water content, but reduced faecal mass (35 to 66%) and diarrhoea (0 to 57%). The R-enantiomers of tachykinin NK1 and NK2 receptor antagonists, SR 140603 and SR 48605 (both at 2 or 20 μg kg−1, s.c.) had no effect other than reducing faecal mass at the highest dose tested. SR 48968 (20 μg kg−1, p.o.) but not loperamide (10 mg kg−1, p.o.) given 24 h before castor oil, still slightly but significantly reduced by 30% the increase of faecal mass output; both treatments significantly reduced (30 to 70%) the effect of castor oil on faecal water content, although the incidence of diarrhoea was only slightly less than in controls. In castor oil-treated rats, naloxone (2 mg kg−1, s.c.) completely blocked the antidiarrhoeal action of loperamide (10 mg kg−1, p.o.) but not of SR 48968 (20 μg kg−1, p.o.); a similar result was obtained on faecal mass and water content. Castor oil strongly increased the occurrence of manometrically recorded propulsive giant contractions (500 to 1000% over control values) of transverse and distal colon, this effect being significantly prevented (80 to 100%) by SR 48968 and loperamide and partially by SR 140333 (35% distal colon, 70% transverse colon). In castor oil free rats, loperamide but not SR 48968 or SR 140333 significantly reduced by 50% the gastrointestinal transit of a charcoal test meal, as well as 24 h faecal mass output. Consistently, loperamide, unlike the tachykinin receptor antagonists, had a dramatic effect on manometric recordings of intestinal motility, reducing all kinds of colonic contractions. Our findings suggest that castor oil diarrhoea in rats entails activation of NK1 and NK2 receptors by endogenous tachykinins, whose antagonists may have a potential as antidiarrhoeal agents free from the constipating action of opioids.

Ethnobotanical studies indicate that Helianthemum glomeratum is a plant widely used in Maya communities to treat diarrhoeas. A possible mechanism to counteract infectious diarrhoea would be by inhibiting the growth of the enteropathogen causing the disease. The aim of this work was to study the antimicrobial activity of H. glomeratum against bacterial enteropathogens isolated from faeces of children with acute diarrhoea or dysentery. A methanol extract obtained from the leaves and stems was highly active against Shigella spp and Vibrio cholerae; activity against Salmonella spp and Escherichia coli isolates was also present. Acetone/water extract from the roots was also highly active against Shigella and Vibrio isolates. Further chemical fractionation indicated that antibacterial activity was associated with the polyphenolic fraction. Shigella spp causes severe dysentery in children and Vibrio cholerae causes severe watery diarrhoea. Antidiarrhoeal activity of H. glomeratum may be due, at least in part, to the antimicrobial activity of polyphenolics against bacterial enteropathogens commonly associated with the disease. © 1997 by John Wiley & Sons, Ltd.

In addition to kaempferol and quercetin already found in the roots from Cuphea pinetorum, bioassay-guided fractionation of the crude extract of the aerial part of this species gave four flavonoid glycosides, quercetin-3-O-α-rhamnopyranoside, luteolin-7-O-β-d-glucopyranoside, apigenin-7-O-α-l-rhamnopyranoside and apigenin-7-O-β-d-glucopyranoside, as well as squalen and β-sitosterol. In vitro antiamoebic and antigiardial activities of isolated compounds indicated that kaempferol is the principal antiprotozoal agent in C. pinetorum. Based on finding this antiprotozoal inhibitor, flavonoids were studied in order to elucidate structure-activity relationships. These data suggest that kaempferol may play an important role in antidiarrhoeal activity of C. pinetorum. Copyright © 2005 John Wiley & Sons, Ltd.

The roots of the plant Eriosema chinense are traditionally used by the tribal people of North East India for treatment of diarrhoea. Therefore, the present investigation was undertaken to scientifically validate the traditional claim that these roots have an antidiarrhoeal effect. Ethanol extract along with three fractions, ethyl acetate, chloroform, and hexane, as well as isolated lupinifolin from the chloroform fraction, were screened for the normal faecal excretion rate and castor oil-induced diarrhoea model. The results demonstrated a significant (p

Background Rotavirus is the most common cause of severe secretory diarrhoea in infants and young children globally. The rotaviral enterotoxin, NSP4, has been proposed to stimulate calcium-activated chloride channels (CaCC) on the apical plasma membrane of intestinal epithelial cells. We previously identified red wine and small molecule CaCC inhibitors. Objective To investigate the efficacy of a red wine extract and a synthetic small molecule, CaCC inh -A01, in inhibiting intestinal CaCCs and rotaviral diarrhoea. Design Inhibition of CaCC-dependent current was measured in T84 cells and mouse ileum. The effectiveness of an orally administered wine extract and CaCC inh -A01 in inhibiting diarrhoea in vivo was determined in a neonatal mouse model of rotaviral infection. Results Screening of ∼150 red wines revealed a Cabernet Sauvignon that inhibited CaCC current in T84 cells with IC 50 at a ∼1:200 dilution, and higher concentrations producing 100% inhibition. A >1 kdalton wine extract prepared by dialysis, which retained full inhibition activity, blocked CaCC current in T84 cells and mouse intestine. In rotavirus-inoculated mice, oral administration of the wine extract prevented diarrhoea by inhibition of intestinal fluid secretion without affecting rotaviral infection. The wine extract did not inhibit the cystic fibrosis chloride channel (CFTR) in cell cultures, nor did it prevent watery stools in neonatal mice administered cholera toxin, which activates CFTR-dependent fluid secretion. CaCC inh -A01 also inhibited rotaviral diarrhoea. Conclusions Our results support a pathogenic role for enterocyte CaCCs in rotaviral diarrhoea and demonstrate the antidiarrhoeal action of CaCC inhibition by an alcohol-free, red wine extract and by a synthetic small molecule.