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Ethnopharmacological relevance Ricinus communis L., commonly known as castor oil plant, is a precious traditional medicine with a history of thousands of years in the world. Castor oil plant has high traditional and medicinal values for treating liver infections, stomach ache, flatulence, constipation, inflammation, warts, colic, enteritis, fever, headache, and as a counter irritant. Its diverse phytochemicals have a wide range of valuable medicinal activities including hepatoprotective, anti-nociceptive, antioxidant, antiulcer, anticancer, anti-inflammatory, central analgesic, antidiabetic, antimicrobial, antiviral, and wound healing activity. Aim of the work To provide a complete characterization of the composition of Ricinus communis leaves using ultra-performance liquid chromatography coupled with hybrid triple time-of-flight mass spectrometry (UPLC-Triple TOF-MS/MS) and different chromatographic techniques and to evaluate its antiviral potential using three mechanisms against three common viruses. Materials and methods R. communis leaves were extracted with 70% methanol and further partitioned with solvents of increasing polarities: petroleum ether, dichloromethane (CH2Cl2), ethyl acetate, and n-butanol. The CH2Cl2 and n-butanol fractions were subjected to repeated chromatographic separation to isolate the phytochemicals, and their structures were elucidated using nuclear magnetic resonance spectroscopy. UPLC-Triple TOF-MS/MS was performed to determine the different phytochemicals in the ethyl acetate fraction. The antiviral activity of the extracts was investigated using the maximum nontoxic concentration of each against the challenge dose of the virus (CDV) and 1/10 and 1/100 dilutions of the CDV for Coxsackie B virus type 4 (COXB4), herpes simplex virus type 1 (HSV1), and hepatitis A virus (HAV) using Vero cell cultures that were treated according to three protocols to test for anti-replicative, protective, and anti-infective antiviral activity. Cell viability was evaluated using the MTT colorimetric assay and each experiment is repeated three times independently of each other. Results R. communis leaves possessed antiviral activity. Evaluation of the anti-replicative activity showed that all extracts possessed high anti-replicative activity against HAV especially methanol and methylene chloride fractions and moderate activity against COXB4; butanol > methylene chloride and ethyl acetate > methanol. All extracts showed protective activity against HAV, especially butanol extract, while methanol extracts showed higher non-significant antiviral protective activity against HSV1 vs Acyclovir. Almost no anti-infective effects were recorded for any extract against the studied viruses. Conclusion The discriminatory effect against each virus by different mechanisms suggests the presence of different chemical compounds. The alkaloid and phenolic derivatives of the extracts of R. communis leaves may help develop a drug to prevent or treat common viral infections. Further investigations are recommended to define the bioactive antiviral properties of R. communis leaves.

The plant Combretum hypopilinum Diels (Combretaceae) is used in traditional medicine for the treatment of diarrhoea and other diseases in Africa. Previously, the antidiarrhoeal activity of its methanol leaf extract was reported. However, the mechanism(s) responsible for this activity is yet to be evaluated.This study aimed to elucidate the possible mechanism(s) of antidiarrhoeal activity of methanol leaf extract of Combretum hypopilinum (MECH) in mice.Phytochemical screening and acute toxicity study were conducted according to standard methods. Adult mice were orally (p.o) administered distilled water (10 ml/kg), MECH (1000 mg/kg) and loperamide (5 mg/kg). The probable mechanisms of antidiarrhoeal activity of MECH were investigated following pretreatment with naloxone (2 mg/kg, subcutaneously), prazosin (1 mg/kg, s.c), yohimbine (2 mg/kg, intraperitoneally), propranolol (1 mg/kg, i.p), pilocarpine (1 mg/kg, s.c) and isosorbide dinitrate (150 mg/kg, p.o) 30 min before administration of MECH (1000 mg/kg). The mice were then subjected to castor oil-induced intestinal motility test.The oral median lethal dose (LDThe results obtained in this study suggest the probable involvement of opioidergic and (α

Ethnopharmacological relevance Nymphaea lotus, which is widely distributed throughout tropical Africa, enjoys a number of ethnomedical uses in Nigeria. Traditionally, the rhizomes of N. lotus are used to cure diarrhoea. Aim of study This study aims to evaluate the antidiarrhoeal activity of the methanol rhizome extract of N. lotus plant in laboratory animals. Materials and methods The extract was screened for activity against castor oil-induced diarrhoea and magnesium sulphate-induced diarrhoea as well as effect on gastric transit time in mice. The effect of methanol rhizome extract of Nymphaea lotus on the perfused isolated tissue preparation was also determined. Results For castor oil-induced diarrhoea, the extract at doses of 200, 400 and 800 mg/kg produced significant reduction in the frequency of diarrhoea (at p

Ethnopharmacological relevance The use of marine seaweeds as a source of natural compounds with medicinal purposes is increasing in Western countries in the last decades, becoming an important alternative in the traditional medicine of many developing countries, where diarrhea still remains a severe public health problem, with high rates of mortality and morbidity. Sulfated polysaccharides (PLS) extracted from red seaweeds can exhibit therapeutic effects for the treatment of gastrointestinal disorders. Thus, the pharmacological properties of the PLS from Gracilaria cervicornis , an endemic seaweed found in the Brazilian northeast coast, was evaluated as an alternative natural medication for diarrhea. Aim of the study This study aimed to evaluate the antidiarrheal activity of sulfated polysaccharides (PLS) extracted from the red seaweed G. cervicornis in Swiss mice pre-treated with castor oil or cholera toxin. Materials and methods The seaweed Gracilaria cervicornis was collected at Flecheiras beach (city of Trairi, State of Ceara, Brazil) and the PLS was obtained through enzymatic extraction and administered in mice (25–30 g) before diarrhea induction with castor oil or cholera toxin. For the evaluation of the total number of fecal output and diarrheal feces, the animals were placed in cages lined with adsorbent material. The evaluation of intestinal fluid accumulation (enteropooling) on castor oil-induced diarrhea in mice occurred by dissecting the small intestine and measuring its volume. The determination of Na + /K + -ATPase activity was measured in the small intestine supernatants by colorimetry, using commercial biochemistry kits. The gastrointestinal motility was evaluated utilizing an activated charcoal as a food tracer. The intestinal fluid secretion and chloride ion concentration were evaluated in intestinal closed loops in mice with cholera toxin-induced secretory diarrhea. The binding ability of PLS with GM1 and/or cholera toxin was evaluated by an Enzyme-Linked Immunosorbent Assay (ELISA). Results The G. cervicornis PLS showed antidiarrheal effects in both acute and secretory diarrhea, reducing the total number of fecal output, diarrheic stools, intestinal fluid accumulation, and increasing small intestine Na + /K + -ATPase activity on castor oil-induced diarrhea. However, the PLS did not affect gastrointestinal motility, indicating that this compound has a different action mechanism than loperamide. In secretory diarrhea, the PLS decreased intestinal fluid secretion and small intestine chloride excretion, binding with GM1 and/or cholera toxin and blocking their attachment to the enterocyte cell surface. Conclusions In conclusion, PLS has a significant antidiarrheal effect in acute and secretory diarrhea. Further investigation is needed towards its use as a natural medicine to treat diarrhea.

Ethnopharmacological relevance Mangifera indica L. leaves have a long history of indigenous use, as an antidiarrhoeal agent among others, without any scientific study that has substantiated or refuted this claim. Therefore, the aims of this study were to determine the secondary metabolites in the aqueous extract of Mangifera indica leaves and its acclaimed antidiarrhoeal activity in rats. Materials and methods The aqueous leaf extract of Mangifera indica was screened for its constituent secondary plant metabolites. In each of the diarrhoeal models, female albino rats were assigned into 5 groups (A, B, C, D and E) containing five animals each such that rats in groups A and B were the positive and negative controls respectively while those in groups C, D and E received 25, 50 and 100 mg/kg body weight of the extract respectively in addition to specific requirements of the model. Results The extract contained alkaloids (4.20 mg/g), flavonoids (13.60 mg/g), phenolics (1.50 mg/g) and saponins (3.10 mg/g) while tannins, anthraquinones, cardiac glycosides and steroids were not detected. In the castor oil-induced diarrhoeal model, the onset time of diarrhoea was significantly prolonged by the 25 and 50 mg/kg body weight whereas there was no episode in the 100 mg/kg body weight treated animals. The extract (25 and 50 mg/kg body weight) decreased the number, water content, fresh weight and total number of wet feaces and increased the inhibition of defecations. All the doses of the extract significantly increased the Na + –K + ATPase activity in the small intestine. The extract dose dependently decreased the masses and volume of intestinal fluid with corresponding increase in inhibition of intestinal fluid content in the castor oil-induced enteropooling model. The extract also reduced the distance travelled by charcoal meal in the 30 min gastrointestinal transit model. All these changes were similar to the reference drugs with the 100 mg/kg body weight of the extract exhibiting the most profound antidiarrhoeal activity. Conclusion The study concluded that the aqueous extract of Mangifera indica leaves possess antidiarrhoeal activity in chemical induced diarrhoeal models and thus justifies its age long folkloric use in managing diarrhoea. The presence of alkaloids, flavonoids, phenolics, saponins and enhancement of Na + –K + ATPase activity might play roles in the antidiarrhoeal activity of the plant extract.

Priva adhaerens (Forssk.) Chiov., a wildly growing plant, is reported in central Uganda to be an effective traditional remedy for diarrhea. The objective of this study was to provide a scientific basis for the ethnopharmacological utility of this plant whose aqueous leaf and shoot extract was evaluated for acute toxicity and antidiarrheal activity using a murine model.Acute toxicity of the aqueous leaf and shoot extract was assessed after determining the major phytochemicals present in the extract. The aqueous leaf and shoot extract was assayed against castor oil-induced diarrhea, transit time, and enteropooling, in comparison to loperamide, a standard drug.The oral LD50 value obtained for Priva adhaerens aqueous extract was greater than 5000mg/kg in rats; the aqueous leaf and shoot extract possessed several important phytochemicals. Furthermore, the aqueous extract significantly, and dose-dependently, reduced frequency of stooling in castor oil-induced diarrhea, intestinal motility, and castor oil-induced enteropooling in rats.This murine model shows that it is relatively safe to orally use the aqueous leaf and shoot extract of Priva adhaerens. The aqueous extract contains phytochemicals that are active for the treatment of diarrhea in a rat model.

Cyperus species are famous for their traditional uses and very commonly used for their anti-spasmodic and anti-diarrheal activities. Cyperus niveus Retz. is used in local traditional system of medicine in Pakistan to treat diarrhea and emesis.The aim of the study was to validate the traditional uses and to provide the possible mechanisms for the medicinal use of Cyperus niveus Retz. as anti-spasmodic, anti-diarrheal and anti emetic.The in-vivo studies of anti-diarrheal, charcoal meal GI transit test and anti-emetic activities were conducted in rats, mice and chicks respectively, while isolated tissues of rabbit's jejunum and rat's ileum were used for in-vitro experiments. Phytochemical analysis was also undertaken.The phytochemical study of hydro-ethanolic extract of Cyperus niveus Retz. showed the presence of flavonoids, phenols, alkaloids, tannins, saponins and glycosides. Cn. Cr caused significant inhibition of castor oil-induced diarrhea in rats (300,500700mg/kg) using loperamide (10mg/kg, p.o) as standard. Cn. Cr also significantly decreased the motility in charcoal meal GI transit test at 100-200mg/kg in mice, using atropine (3.0mg/kg) as positive control. In jejunum tissue, Cn. Cr relaxed carbachol(1µM) and KThis study shows the presence of antidiarrheal and spasmolytic activities in Cyperus niveus Retz. extract, mediated by dual blocking mechanisms of muscarinic receptors and Ca

Pupalia lappacea is a medicinal plant found in savannah and woodland localities and forest path sides from Senegal to Southern Nigeria. It has been used in the management of diarrhoea in Nigerian traditional medicine. This study was designed to evaluate the antidiarrhoeal activity of the hydroethanolic leaf extract of Pupalia lappacea (PL).The antidiarrhoeal activity of PL was evaluated using the normal and castor oil-induced intestinal transit, castor oil-induced diarrhoea, gastric emptying and intestinal fluid accumulation tests in rodents.PL (100-400mg/kg, p.o.) produced a significant dose-dependent decrease in normal and castor oil-induced intestinal transit compared with the control group (distilled water 10ml/kg, p.o.). This effect was significantly (P0.05) inhibited by pilocarpine (1mg/kg, s.c.) but not by yohimbine (10mg/kg, s.c.), prazosin (1mg/kg, s.c.), or propranolol (1mg/kg, i.p.). The extract produced a dose-dependent and significant increase in the onset of diarrhoea. PL (100-400mg/kg) also reduced the diarrhoea score, number and weight of wet stools. The in-vivo antidiarrhoeal index (ADIin vivo) of 56.95% produced by the extract at the dose of 400mg/kg was lower compared to that produced by loperamide 5mg/kg (77.75%). However, PL (400mg/kg) significantly increased gastric emptying in rats but significantly reduced the volume of intestinal content in the intestinal fluid accumulation test. Phytochemical analysis of the extract revealed the presence of alkaloids, saponins, and fixed oils and fats. The acute toxicity studies revealed that the extract is relatively safe when given orally; no death was recorded at a dose of 10g/kg.Results showed that the hydroethanolic leaf extract of Pupalia lappacea possesses antidiarrhoeal activity possibly mediated by antimuscarinic receptor activity.

An ethnopharmacological survey indicated that the bark from Qualea parviflora Mart. (Vochysiaceae) could be used to treat gastrointestinal disorders, such as diarrhea and intestinal inflammation. The objective of this study was to evaluate the effects of a methanolic extract from the bark of Qualea parviflora (QP) in an experimental model of diarrhea and intestinal inflammation induced in rodents.The antidiarrheal and antispasmodic effects of QP were investigated by measuring intestinal motility, diarrhea, and intestinal fluid accumulation in rodents after challenging with a cathartic agent. In addition, the effects of QP on the contractility of the isolated mice-ileum preparation were determined. Acute intestinal inflammation was induced in male Wistar rats by the rectal administration of trinitrobenzenesulfonic acid (TNBS) in 50% ethanol (0.25 mL). QP was administered orally (for 5 days) prior to the induction of inflammation. The colonic injury and extent of inflammation were assessed by macroscopic damage scores and lesion length. The enhanced colonic mucosal injury, inflammatory response, and oxidative stress were evaluated by myeloperoxidase (MPO) activity; the tumor necrosis factor alpha (TNF-α), interleukin 1β (IL1-β), and malondialdehyde (MDA) levels; and the glutathione (GSH) content.Oral treatment with QP (500 mg/kg) delayed the onset of diarrhea, reduced the amount of liquid stool, and decreased the severity of the diarrhea and the evacuation index in rodents challenged with castor oil (p0.01). Additionally, QP (150-500 µg/mL) demonstrated effective antispasmodic activity against carbachol-induced contractions of mouse ileum in vitro. Oral treatment (25 and 50 mg/kg/day) with QP significantly reduced the intestinal inflammation induced by TNBS in rats (52% and 45%, respectively). Improvement of colonic mucosal injury by treatment with QP was demonstrated by a decrease in MDA levels and an increase in GSH content in colonic tissue. QP also prevented intestinal inflammation as evidenced by reduced cytokine levels (TNF-α and IL1-β) and low MPO activity.The ethnopharmacological usefulness of the bark from Qualea parviflora against diarrhea containing blood and mucus was supported by the observed antidiarrheal, antispasmodic, and intestinal antiinflammatory properties of this medicinal plant.

Ocimum kilimandscharicum Baker ex Güerke, commonly referred to as Kapur Tulsi, is a medicinal herb that belongs to the family of Lamiaceae. It is traditionally popular for its gastroprotective effects, including its use as a digestive and anti-diarrhoeal.The present study aims to prove the anti-diarrhoeal activity of aqueous extract of leaves of Ocimum kilimandscharicum in animal models.The aqueous extract was tested at three different dose levels (100, 200 and 400mg/kg, p.o. in rats and the corresponding doses in mice) against castor-oil induced diarrhoea model and castor oil induced enteropooling assay in rats; and charcoal meal test/intestinal motility test in mice. The parameters observed were the onset of defecation, cumulative faecal weight and consistency of faeces in the castor oil induced diarrhoea model; the weight of intestinal content in castor oil induced enteropooling assay; and the distance travelled by charcoal in the intestinal motility test.A significant delay in the onset of defecation (p0.05), reduction in the cumulative faecal weight (p0.001), along with a change in the faecal consistency from watery to solid form was observed at the dose of 200mg/kg in the castor oil-induced diarrhoea model. Similarly, the extract at the doses of 100mg/kg (p0.01) and 200mg/kg (p0.001) significantly decreased the weight of intestinal content in castor oil induced enteropooling assay. In the charcoal meal test the extract at the dose of 280mg/kg (corresponding to 200mg/kg in rats) significantly (p0.01) reduced the distance travelled by charcoal.The aqueous extract of leaves of Ocimum kilimandscharicum showed anti-diarrhoeal activity, which may be due to its anti-motility and anti-secretory effects, which thus proved the traditional claims.

Ethnopharmacological relevance: In the Greco-Arab (Unani) traditional medicine, Fumaria parviflora Linn. is widely used in hypreractive gut and respiratory disorders including diarrhea, abdominal cramps, indigestion and asthma but scientific studies to provide rational for these medicinal uses are sparse. This study was therefore undertaken to provide ethnopharmacological basis for its medicinal use in diarrhea, abdominal cramps and asthma. Materials and methods: The in vivo studies were conducted in mice and rats while isolated gut and tracheal preparations of rat, guinea-pig and rabbit were suspended in respective tissue baths to measure the isotonic and isometric responses, using Power Lab electronic recorder. Results: The aqueous-methanol extract of Fumaria parviflora (Fp.Cr) protected against diarrhea caused by castor oil in rats and mice, similar to loperamide and dicyclomine, and bronchospasm caused by carbachol (CCh) in rats, similar to aminophylline. In the in vitro studies, Fp.Cr relaxed CCh and isotonic high K+ physiological salts solutions-induced contractions in jejunum, ileum and tracheal preparations of rat, guinea-pig and rabbit. Fp.Cr was predominately more potent against CCh than isotonic high K+ solutions-induced contractions, similar to dicyclomine, suggesting the presence of anticholinergic and calcium channel blocking (CCB) activities, which were confirmed when Fp.Cr shifted the CCh and Ca2+ concentration–response curves, constructed in rat ileum and trachea, towards right. Among intestinal preparations from various species, both anticholinergic and CCB effects of Fp.Cr were exhibited at lower concentrations in rat than the other species. In tracheal preparations, Fp.Cr was the most potent in its CCB effect in rabbit. Within species, CCB effect of Fp.Cr was produced at lower concentrations in rat jejunum than ileum and trachea, whereas, anticholinergic effect was produced at higher concentration in rat trachea than intestine. Conclusion: This study, showing the presence of antidiarrheal, antispasmodic and bronchodilator activities in Fumaria parviflora possibly mediated through dual blockade of muscarinic receptors and Ca2+ channels, provides sound basis for its medicinal uses in diarrhea, abdominal cramps and may be used as bronchodilator in asthma. Species and tissue-dependency of these effects underscores the importance of utilizing multiple tissues and species to get more meaningful results.

Diarrhea remains one of the main killers of children aged below five years. Traditional antidiarrheal remedies form a potentially viable source of novel low cost efficacious treatments in low resource settings. There is therefore a pressing need to scientifically evaluate these remedies.This study aimed to investigate the in vivo and in vitro antidiarrheal activity of freeze dried Bidens biternata, a herb used in traditional Ayurvedic medicine in the management of diarrhea.In the castor oil test, twenty (20) adult Sprague-Dawley rats were randomized to a negative control (normal saline, n=5), a positive control (5mg/kg loperamide, n=5), and two test groups. The low dose test group received 200mg/kg Bidens biternata extract (n=5) while the high dose test group received 400mg/kg B. biternata extract (n=5). Castor oil (4ml/kg) was then administered to the animals one hour after administration of the respective treatments after which the total mass of fecal output excreted after four (4) hours was determined. In the charcoal meal test fifteen (15) Sprague Dawley rats were randomized to a control group (normal saline 5ml/kg orally, n=5), a positive control group (atropine sulfate 0.1mg/kg i.p., n=5) and a test group (400mg/kg B. biternata extract, n=5). Charcoal meal was then administered via oral gavage to each rat thirty (30) minutes after the administration of the various treatments. The distance covered by the charcoal meal from the pylorus was then determined after sacrifice of the animals thirty minutes after the meal. In the enteropooling test twenty (20) Sprague-Dawley rats were randomized to a control group (5% v/v ethanol in normal saline, n=5), a positive control group (5mg/kg loperamide, n=5) and a test group (400mg/kg B. biternata extract, n=5). For each group prostaglandin E2 (PGE2) (100μg/kg) was administered immediately after the treatments. The animals were then sacrificed half an hour later and the volume of the small intestine contents determined. The effects of different concentrations of B. biternata extract (0.5. 1.0, 2.0, 3.0 and 5.0mg/ml) on jejunal contraction were investigated and a dose-response curve constructed using the experimental data after which The ED50 dose was determined. The effect of tamsulosin (α1 adrenergic blocker), yohimbine (α2 adrenergic blocker), propranolol (β adrenergic blocker) and naloxone (μ opioid blocker) on the contractile activity of the extract were also investigated. The experimental data were expressed as mean±standard error of mean (SEM) and then analyzed using one-way ANOVA followed by Tukey's post hoc test in cases of significance (set at p0.05).The freeze dried extracts of B. biternata had significant antidiarrheal effects in the castor oil induced diarrhea model (p0.01) with the highest activity being observed at the 400mg/kg dosage level (1.66±0.81g vs. 4.54±0.51g control, p=0.01). B. biternata extract had significant effects on intestinal motility in the charcoal meal test compared to the control group (43.61±4.42% vs. 60.54±3.33%: p0.05). B. biternata extract had a significant effect on PGE2 induced enteropooling (3.06±0.07ml vs. 4.74±0.10ml; p0.001). The freeze dried extracts of B. biternata had a significant negative effect on the contractility of the isolated rabbit jejunum (p0.001). The effects of the extract were significantly attenuated by tamsulosin (53.94±4.20% vs. 80.57±4.09%; p0.01) and naloxone (53.94±4.20% vs. 73.89±7.26%; p0.05). Yohimbine (p0.05) and propranolol (p0.05) however did not have any significant effect on the contractile activity of the extract.The freeze dried extract of B. biternata possess significant antidiarrheal activity in both in vitro and in vivo models which appears to be mediated by modulating both the intestinal motility as well as the secretory activity. The results of this study also validate its traditional use as an antidiarrheal remedy.

In our search for plants useful in the treatment of diarrhoea, we investigated the ethyl acetate extract of Baphia nitida (BN) using intestinal transit, enteropooling and gastric emptying tests in mice and rats. In the castor oil intestinal transit test, BN produced a significant (P

Emilia coccinea (Sims) G. Don is reported to possess a number of medicinal properties including antidiarrhoeal and antimicrobial activities. The antidiarrhoeal effects of both methanol and aqueous extracts of the leaves of Emilia coccinea were studied in rats against castor oil-induced diarrhoea at the doses of 200, 400 and 600 mg/kg body weight. The methanol extract, and to a lesser extent the aqueous extract, significantly prolonged the time for diarrhoeal induction; it reduced the frequency of diarrhoea episodes and decreased the propulsion of charcoal meal through the gastrointestinal tract in a dose dependent manner. The aqueous extract did not have any antimicrobial activity at the tested concentration (5 mg/ml), but the methanol extract was most active on Escherichia coli. These results may support the fact that this plant is used traditionally to cure diarrhoea.

The methanol extract of Xylocarpus granatum bark was studied for its antidiarrhoeal properties in experimental diarrhoea, induced by castor oil and magnesium sulphate in mice. At the doses of 250 and 500 mg/kg per oral, the methanol extract showed significant and dose-dependent antidiarrhoeal activity in both models. The extracts also significantly reduced the intestinal transit in charcoal meal test when compared to atropine sulphate (5 mg/kg; i.m.). The results showed that the extracts of Xylocarpus granatum bark have a significant antidiarrhoeal activity and supports its traditional uses in herbal medicine.

Anacardium occidentale L. (Anacardiaceae) is commonly known as the cashew tree. It is native to tropical America and extracts of the leaves, bark, roots, chestnut net and exudate have been traditionally used in northeast Brazil for the treatment of various diseases. The exudate of the cashew tree (cashew gum) has been exploited by locals since ancient times for multiple applications, including the treatment of diarrheal diseases.The primary aim of the present study is to evaluate the antidiarrheal activity of cashew gum (CG), a complex heteropolysaccharide from the exudate of the cashew tree, using various models.The antidiarrheal activity of cashew gum (CG) against acute diarrhea was investigated using the castor oil-induced diarrhea model. The effects of CG on gastrointestinal transit and castor oil- and PGE2- induced enteropooling were also examined in rodents. In addition, the effect of CG against secretory diarrhea was investigated using a model of fluid secretion in cholera toxin-treated intestinal closed loops in live mice.Cashew gum (30, 60, and 90 mg/kg, p.o.) showed a significant (P0.05-0.01) antidiarrheal effect in rats with castor oil-induced diarrhea, inhibiting the total amount of stool and diarrheal stools. The 60 mg/kg dose of CG exhibited excellent antidiarrheal activity and significantly reduced the severity of diarrhea (diarrhea scores) in rats. CG (60 mg/kg) significantly (P0.05) decreased the volume of castor oil- and PGE2-induced intestinal fluid secretion (enteropooling). In addition, similar to loperamide (standard drug, 5 mg/kg, p.o.), CG treatment reduced the distance traveled by a charcoal meal in the 30-min gastrointestinal transit model by interacting with opioid receptors. In cholera toxin-induced secretory diarrhea, CG (60 mg/kg) significantly inhibited the intestinal fluid secretion and decreased Cl(-) ion loss in the cholera toxin(-)treated isolated loops model of live mice by competitively binding to cholera toxin-GM1 receptors.In conclusion, our results indicate that a complex heteropolysaccharide extracted from the exudate of A. occidentale L. has antidiarrheal activity in acute, inflammatory, and secretory diarrhea models, which could justify its traditional use in the treatment of diarrhea in northeast Brazil. The antidiarrheal activity might be explained by the capacity of CG to inhibit gastrointestinal motility and thereby reduce the accumulation of intestinal fluid and the secretion of water and chloride ions in the lumen of the intestine.

The methanol (MeOH) extract of the barks of Xylocarpus moluccensis, and different fractions of this extract were studied for antidiarrhoeal activity using castor oil- and magnesium sulphate-induced diarrhoea models in mice. At the doses of 250 and 500 mg/kg, the MeOH extract showed significant antidiarrhoeal activity in both models. The EtOAc fraction (EAF) and the residual MeOH fraction (RMF) exhibited similar activity using a dose of 250 mg/kg in both models. No antidiarrhoeal activity was observed with the chloroform fraction (CHF) at the test doses. When tested for antibacterial effect, the MeOH extract displayed moderate inhibitory activity against Escherichia coli, Vibrio cholera, Staphylococcus aureus, Staphylococcus epidermis, Shigella dysentery, Staphylococcus pyogenes, Salmonella typhi, Pseudomonas aeruginosa and Enterobacter aerogenes. While the CHF inhibited the growth of Escherichia coli, Vibrio cholerae, Shigella dysenteriae, Shigella sonnei, Staphylococcus epidermis, Staphylococcus pyogenes and Pseudomonas aeruginosa, the EAF was active against all test organisms except Vibrio cholera and Staphylococcus epidermis. The RMF inhibited the growth of all the test organisms with moderate zone of inhibition. On the basis of these findings, it can be assumed that Xylocarpus moluccensis could be a potential source for novel 'lead' discovery for antidiarrhoeal drug development.

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.

Mangifera indica is commonly grown in many parts of the world. Its seeds have been used for anti-diarrhoeal activity in Indian traditional medicine. This study evaluates the potential anti-diarrhoeal activity of methanolic (MMI) and aqueous (AMI) extracts of seeds of M. indica in experimental diarrhoea, induced by castor oil and magnesium sulphate in mice. Both MMI and AMI were given orally in the dose of 250 mg/kg, showed significant anti-diarrhoeal activity comparable with that of the standard drug loperamide. However, only MMI significantly reduced intestinal transit in charcoal meal test as compared with atropine sulphate (5 mg/kg; im). The in vitro antimicrobial activity of MMI and AMI showed variable results. While, AMI significantly inhibited growth of Streptococcus aureus and Proteus vulgaris, both MMI and AMI did not show any significant effect on growth of E. coli and Klebsiella. The results illustrate that the extracts of M. indica have significant anti-diarrhoeal activity and part of the activity of MMI may be attributed to its effect on intestinal transit.

Ethnopharmacological relevance The fructus Alpinia oxyphylla Miq. (AOM) has been used for treating diarrhea with spleen deficiency and gastralgia for thousands of years. A number of traditional Chinese medicine formulae provide AOM as an alternative herbal treatment for diarrhea, but the scientific basis for this usage has not been well defined. Aim of the study In this study, we tried to investigate the antidiarrheal activity and possible mechanisms of Fructus AOM, aiming to enrich our understanding to the scientific meanings and theoretical significance of Fructus AOM in clinical practice. Materials and methods The fructus of AOM collected from Hainan province in China were macerated in the 95% ethanol to obtain the crude 95% ethanol extract, followed by subjected to chromatographic separation over a Diaion HP20 column to obtain 90% and 50% ethanol eluted fractions. The activities of the crude extract and fractions on castor oil induced acute diarrhea, rhubarb induced chronic diarrhea, gastrointestinal transit (GIT) in mice, and contractions of isolated guinea-pig ileum were evaluated. Additionally, nitric oxide (NO), gastrointestinal peptides gastrin (GAS), motilin (MTL) and somatostatin (SS) levels that related to gastrointestinal motilities were detected to demonstrate the potential mechanisms. Ultimately, LC–MS/MS method was utilized to ensure the chemical consistency. Results The 95% ethanol extract and 90% ethanol eluted fraction significantly delayed the onset time and decreased the wet faeces proportion compared with control group in the castor oil induced acute diarrhea mice. In terms of further evaluation of antidiarrheal activity, the 95% ethanol extract and 90% ethanol elution displayed significant inhibition of the intestinal propulsion at the two highest oral doses of 20 g crude drug/kg and 1 g/kg. Moreover the 95% ethanol extract (10 and 20 g crude drug/kg) and 90% ethanol elution (0.5 and 1 g/kg) could significantly inhibit the GIT, which was partially attributed to the increase in NO and SS levels, and the decreased MTL. In vitro spontaneous contractions of the isolated guinea pig ileum induced by carbachol, neostigmine and histamine were attenuated by both the extract and elution. Phytochemical analysis of 95% ethanol extract and its fractions identified the presence of diphenylheptanes, sesquiterpenes, and flavones as the major components. Conclusions Our in vivo and in vitro data could partly support and justify the traditional usage of Fructus AOM on the treatment of diarrhea in traditional medicine.

Ethnopharmacological relevance Linum usitatissimum , commonly known as Flaxseed has traditionally been used for the management of diarrhea and gastrointestinal infections. This study was planned to assess pharmacological basis for the medicinal use of Flaxseed in infectious and non-infectious diarrhea. Materials and methods The crude aqueous-methanolic extract of Flaxseed was studied using the in vivo castor oil-induced diarrhea, gut motility and enteropooling assays. Mechanistic basis was further elucidated by testing the inhibitory effect on spontaneously contracting isolated rabbit jejunum preparations, suspended in a 10 ml tissue bath containing Tyrode׳ solution, maintained at 37 °C and aerated with carbogen. Antibacterial efficacy of the Flaxseed extract was tested against different enteric and non-enteric pathogenic bacteria using in vitro antibacterial assays. Results Flaxseed extract reduced the diarrheal score in mice, by 39%, 63.90% and 68.34% at the respective doses of 100, 300 and 500 mg/kg. Intestinal secretions were reduced by 24.12%, 28.09% and 38.80%, whereas the intestinal motility was reduced by 31.66%, 46.98% and 56.20% at respective doses of 100, 300 and 500 mg/kg. When tested on isolated rabbit jejunum preparations, Flaxseed extract produced a dose-dependent inhibition of both spontaneous and high K + (80 mM)-induced contractions, and shifted the concentration–response curves of Ca ++ to the right with suppression of the maximum response, similar to that caused by verapamil. Flaxseed extract was found to possess bactericidal activity at the tested concentrations of 12.5 mg/ml, against vancomycin-resistant Enterococcus faecalis (100%), Escherichia coli K1 (88.88%), methicillin-resistant Staphylococcus aureus (98.76%), Bacillus cereus (92.64%), Pseudomonas aeruginosa (76.83%) and Salmonella typhi (26.91±3.35%). The concentration of 10 mg/ml showed bactericidal effects against all the aforementioned pathogens except Escherichia coli K1, whereas for Pseudomonas aeruginosa and Salmonella typhi , it was bacteriostatic at this concentration. Conclusions Our results indicate that Linum usitatissimum (Flaxseed) extract exhibits antidiarrheal and antispasmodic activities by virtue of its antimotility and antisecretory effects which are mediated possibly through inhibition of Ca ++ channels, though additional mechanism(s) cannot be ruled out. Flaxseed extract proved effective against both enteric and non-enteric pathogens causing diarrhea, thus ensuring wide coverage and rationalizing its medicinal use in both the infectious and non-infectious diarrhea.

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.

Satureja hortensis L. (Lamiaceae) is an annual herb that is used in the traditional medicine of Iran for treating stomach and intestinal disorders. The antispasmodic activity of S. hortensis essential oil (SHEO) was assessed on contractions of isolated ileum, induced by KCl and acetylcholine, and compared with the effect of atropine and dicyclomine. SHEO inhibited the response to 80 mM KCl in a concentration-dependent manner (pD2=1.55±0.09 μg/ml; this is negative log concentration of SHEO causing 50% of maximum inhibition) and attenuating the maximum inducible response of acetylcholine concentration–response curve. Effect of SHEO on KCl was similar to that of dicyclomine. Dicyclomine (3.46 and 34.6 ng/ml) also reduced the response to acetylcholine on rat isolated ileum without altering the maximum response and shifted the acetylcholine concentration–response curve to the right by 16-fold at 34.6 ng/ml (100 nM) bath concentration, while atropine only inhibited the response to acetylcholine. This study shows that SHEO is a relaxant of rat isolated ileum. In addition to antispasmodic activity in vitro, essential oil of this plant at a dose of 0.1 ml/100 g inhibited castor oil induced diarrhoea in mice. As the inhibition of contractile overactivity of the ileum is the base of the treatment of some gastrointestinal disorders such as colic, SHEO may have clinical benefits for treatment of these conditions.

Methanol extract of Punica granatum seed was evaluated for antidiarrhoeal activity against different experimental models of diarrhoea in rats. P. granatum seed extract treated animals showed significant inhibitory activity against castrol-oil induced diarrhoea and PGE2 induced enteropooling in rats. The extract also showed a significant reduction in gastro-intestinal motility in charcoal meal test in rats. The results obtained established the efficacy of P. granatum seed extract as an antidiarrhoeal agent.

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.

Ethnopharmacological relevance Polygonum chinense Linn., a folk medicine, has long been used for the treatment of diarrhea and enteritis in southwestern China. However, the components responsible for its anti-diarrheal activity are still poorly understood. Aim of the study To determine anti-diarrheal activities of Polygonum chinense L. and to identify its active components through bioactivity-guided isolation technique. Materials and methods Animals were orally administered with the extract of Polygonum chinense L. The anti-diarrheal effects of 75% ethanol extract, four fractions with different polarities from 75% ethanol extract, different eluates collected from Diaion HP-20 macroporous resin chromatography, ellagic acid and corilagin, were examined based on mouse models of castor oil- and magnesium sulfate-induced diarrhea. Results The results showed that the 75% ethanol extract of Polygonum chinense L. exhibited significant anti-diarrheal activities in a dose-dependent manner in two mouse models. Through in vivo bioactivity-guided fractionation processes, n -butanol and aqueous fractions were found to exhibit prominent anti-diarrheal activities, and two major compounds, ellagic acid and corilagin, from these active fractions were found to possess anti-diarrheal effects. Conclusion Present study provides evidence of the utilization of Polygonum chinense L. for diarrhea, and ellagic acid and corilagin are two components contributing to the anti-diarrheal effect.

Flos populi (male inflorescence of Populus tomentosa Carrière) has been traditionally used in East Asian countries for the treatment of various inflammatory diseases, strengthening the spleen and stomach, anti-rheumatic, anti-tumor and anti-diarrhoeal.To evaluate the in vivo or in vitro anti-diarrhoeal and anti-microbial activity of Flos populi aqueous extract.Acute toxicity of Flos populi aqueous extract (FPAE) was investigated. Castor oil-induced diarrhoea method was used to evaluate the anti-diarrhoeal activity, inhibition of defecation and diarrhoea were determined in mice, effects on castor oil-induced enteropooling, intestinal transit and intestinal fluid secretion in rats or mice. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of FPAE against strains of three clinical bacterial isolates and one reference strain were used to test the anti-microbial activity.The FPAE reduced the frequency of diarrhoea episodes and decreased the propulsion of charcoal meal through the gastrointestinal tract in a dose dependent manner. FPAE (100-500 mg/kg, p.o.) produced dose-dependent and significant (P0.01) protection of mice against castor oil-induced diarrhoea. FPAE, dose-dependently and significantly (P0.01) delayed the onset of castor-oil induced diarrhoea, decreased the frequency of defecation, and reduced the severity of diarrhoea. Compared with control animals, FPAE, dose-dependently and significantly (P0.01) decreased the volume of castor oil-induced intestinal fluid secretion, and reduced the number, weight and wetness of faecal droppings. There was no deaths or abnormalities in behaviour seen in the acute toxicity test. The aqueous extract displayed anti-microbial effects to three species of bacteria in anti-microbial test.The findings of this study indicate that FPAE possesses anti-diarrhoeal property in rats and mice and confirm the ethnomedicinal use of Flos Populi as a valuable natural remedy for the treatment, management and/or control of diarrhoea. These results may support the fact that this plant is traditionally used to cure diarrhoea.

Aim of the study To evaluate the antidiarrhoeal properties of Alstonia congensis leaves claimed to be effective for the treatment of diarrhoea by traditional healers during our ethnopharmacological investigation conducted in Kinshasa, Democratic Republic of Congo. Materials and methods The aqueous extract (decoction), and the 80% hot methanol extract (Soxhlet extraction) were obtained. This last extract was fractionated. The antidiarrhoeal activity was evaluated using castor oil and magnesium sulphate-induced diarrhoea in animals. The potential antibacterial activity of all samples was also assessed in vitro. Results At all oral doses of 100 and 200 mg/kg body weight, all A. congensis samples showed significant and dose-dependent antidiarrhoeal activity in treated Wistar rats characterised by significant increase of onset time and decrease of all other diarrhoeal parameters at various degrees compared to untreated groups in both models. At the highest oral dose of 200 mg/kg bodyweight, the 80% hot methanol and aqueous extracts produced 79.8±2.1% and 78.6±0.5%, and 75.0±2.1% and 71.4±2.1% inhibition of defecation and diarrhoea respectively against castor oil-induced diarrhoea, and 75.0±1.2% and 73.3±1.2% inhibition of diarrhoea respectively against magnesium sulphate-induced diarrhoea. The 80% hot methanol and aqueous detannified extracts showed low activity (42–47% inhibition of defecation and/or diarrhoea in both tests) suggesting that tannins may be responsible for the observed activity. At the same oral doses, the total alkaloid extract, the chloroform soluble fraction rich in alkaloids, the 80% methanol and the alkaline aqueous soluble subfractions produced more than 50% inhibition of defecation and/or diarrhoea in both tests. From the antibacterial testing in vitro, results indicated that all A. congensis samples exhibited an antibacterial activity mainly against bacteria implicated in diarrhoea with MIC and MBC values in the range of 15.6–500 μg/ml. The most active samples were the aqueous (decoction) and the 80% hot methanol dried extracts, the chloroform subfraction rich in alkaloids and the total alkaloid extract (MIC: 15.7–125 μg/ml, MBC: 31.2–250 μg/ml). Proteus varibilis was found to be the most resistant microorganism. Conclusion These reported results can partly support and justify the traditional use of extracts from Alstonia congensis leaves for the treatment of diarrhoea in tradittional medicine.

Ethnopharmacological relevance Carum roxburghianum is traditionally used in hyperactive gastrointestinal and respiratory disorders. The present study was carried out to investigate the possible gut and airways relaxant potential of Carum roxburghianum to rationalize its folk uses. Materials and methods Crude extract of Carum roxburghianum (Cr.Cr) was studied in in vivo and in vitro techniques. Results Cr.Cr exhibited protective effect against castor oil-induced diarrhea in mice at 100–1000 mg/kg. In rabbit jejunum preparations, Cr.Cr (0.03–3.0 mg/mL) caused relaxation of spontaneous and K + (80 mM)-induced contractions at similar concentrations, like papaverine. Pretreatment of tissues with Cr.Cr (0.1–1.0 mg/mL) shifted Ca ++ concentration–response curves (CRCs) to right, like verapamil. Cr.Cr (0.03 and 0.1 mg/mL) caused leftward shift of isoprenaline-induced inhibitory CRCs, similar to papaverine. In isolated guinea-pig ileum, Cr.Cr (0.01 and 0.03 mg/mL) produced rightward parallel shift of acetylcholine-curves, like atropine. Cr.Cr (1.0–30 mg/kg) caused suppression of carbachol (CCh, 100 μg/kg)-induced increase in inspiratory pressure of anaesthetized rats. In guinea-pig trachea, Cr.Cr (0.03–1.0 mg/mL) relaxed CCh and high K + -induced contractions, shifted isoprenaline-induced inhibitory CRCs to left at 0.1 and 0.3 mg/mL and CCh-curves parallel to right (0.01 and 0.03 mg/mL). Cr.Cr did not cause any mortality of mice up to 10 g/kg dose. Conclusion These results indicate that Carum roxburghianum possess combination of antidiarrheal, antispasmodic and bronchodilatory effects, which provides pharmacological basis to its traditional use in the disorders of gut and airways hyperactivity, like diarrhea, colic and asthma.

Aim of the study Wei-Chang-An-Wan (WCAW), a traditional pharmaceutical preparation, has been used for treating various gastrointestinal (GI) diseases for several decades, but it is still poorly understood how it works on those disorders. This study was to investigate the effects of WCAW extract on GI tract. Materials and methods The activities of the methanol extract (ME) of WCAW on castor oil-induced diarrhoea, gastrointestinal transit (GIT) in mice, and contractions of isolated rabbit jejunum were investigated. We further assessed the safety of ME in vivo. Additionally, a HPLC fingerprint of ME was appraised to ensure its chemical consistency. Results Ten peaks were identified in the HPLC fingerprint of ME. At the doses of 400 and 800 mg/kg, ME significantly protected mice against castor oil-induced diarrhoea as well as the number of faeces and wet faeces. Interestingly, administration of ME significantly accelerated GIT in normal mice and reduced stimulated GIT induced by neostigmine. ME also dose-dependently attenuated spontaneous contractions of the isolated rabbit jejunum, and those induced by acetylcholine (Ach) and neostigmine. Moreover, oral administration of ME up to 5 g/kg did not produce any toxic effects. Taken together, ME is able to inhibit diarrhoea, increase normal GIT, and decrease GIT induced by neostigmine, which indicate that ME might play a bidirectional role in GI tract. Conclusions Our study provides a scientific basis for the clinical use of WCAW.

Ethnopharmacological relevance Geranium incanum Burm. f. (Geraniaceae) is used in South Africa especially in rural communities by traditional medicine practitioners to treat diarrhoea. However, scientific evidence does not exist in any literature to corroborate the claim of therapeutic success of the plant species in diarrhoea. Aim of study The study intended to investigate the antidiarrhoeal activity of the leaf aqueous extract of Geranium incanum in mice. Materials and Methods Castor oil induced diarrhoeal test was used to assess the antidiarrhoeal activity of Geranium incanum. Gastrointestinal tract transit of charcoal meal test was used to assess the antipropulsive activity of the plant extract while the acute toxicity study and phytochemical analysis were carried out using well established protocols and methods. Results The antidiarrhoeal activity of Geranium incanum was investigated by studying the effect of leaf aqueous extract of the plant species on castor oil-induced diarrhoea in mice. The leaf aqueous extract of Geranium incanum significantly reduced faecal output in castor oil -induced diarrhoea and also significantly reduced the number of diarrhoeal episodes. Geranium incanum significantly delayed the onset of diarrhoea induced by castor oil and significantly reduced the number of animals exhibiting diarrhoea. Loperamide, a standard antidiarrhoeal drug, produced similar effects to the leaf aqueous extract of Geranium incanum on castor oil-induced diarrhoea. Both Geranium incanum and loperamide significantly reduced the intestinal propulsion of charcoal meal in mice. The phytochemical analysis of the leaves revealed the presence of tannins, saponins particularly steroidal saponin, and flavonoids. The LD 50 of the plant species obtained was greater than 4000 mg/kg (p.o.). Conclusion The data obtained indicate that the leaf aqueous extract of Geranium incanum has both antidiarrhoeal and antipropulsive activities The data also show that the plant material given orally may be safe and/or non toxic in mice. However, further investigation on the acute toxicity and on the mechanism of the antidiarrhoeal effect of the plant species needs to be carried out.

The effect of the aqueous extract of Mezoneuron benthamianum (MB) on experimentally induced diarrhoea, intestinal propulsive movement (IPM) and intestinal fluid accumulation (enteropooling) were investigated in rats and mice. The extract (400, 800 and 1600 mg/kg, orally) produced a significant (p0.05) and dose-dependent reduction in propulsion in the castor oil-induced intestinal transit in mice. The mean peristaltic index (%) for these doses of extract, control, (distilled water, 10 ml/kg, p.o.) and morphine, (10 mg/kg, s.c.) were 73.48, 69.34, 57.27, 89.93 and 31.56, respectively. The effect of the extract at the highest dose was significantly (p0.05) lower than that of the standard drug. This effect was antagonised by yohimbine (1mg/kg, s.c.). In a dose-dependent manner, the extract delayed the onset of diarrhoea, produced a significant decrease in the frequency of defaecation, severity of diarrhoea and protected the mice treated with castor oil. Total diarrhoea scores were 12.0+/-0.63, 10.3+/-2.06, 8.5+/-2.15, 7.1+/-0.91 and 5.8+/-0.79 for control, extract (400, 800 and 1600 mg/kg) and morphine, respectively. The extract significantly decreased the volume (ml) of intestinal fluid secretion induced by castor oil (1.75+/-0.02 to 0.93+/-0.04) compared with 1.90+/-0.05 for control. The inhibitory effect on fluid accumulation by the extract was also attenuated by yohimbine (1.0 mg/kg). Preliminary phytochemical screening revealed the presence of flavonoids, tannins, cardiac glycosides, anthraquinones and saponins. Administration of the extract up to 2 g/kg (orally) did not produce any toxic effect in the acute toxicity studies in mice. The LD(50) of the extract when given intraperitoneally was 1021.31 mg/kg. The results obtained show that MB possesses anti-diarrhoeal activity due to its inhibitory effects on gastrointestinal propulsion and intestinal fluid accumulation. The antagonistic actions of yohimbine in the experiments suggest a role for the a(2)-adrenergic receptor system.