Antidiarrhoeal Activity of the Alcoholic Extract of the Leaves of Butea frondosa Koen. Ex Roxb

The study evaluated the antidiarrhoeal property of the alcohol extract of Butea frondosa leaf on mice and rats. Studies revealed that at a dose of 25 and 75 mg/kg a considerable reduction in the extent of diarrhoea was observed but at a dose of 100 mg/kg the animals appeared completely constipated when subjected to castor oil induced diarrhoea and intestinal motility model. Therefore, Butea frondosa can be regarded as an effective antidiarrhoeal.     

Antidiarrhoeal Activity of Leaves of Melastoma malabathricum Linn.

The antidiarrhoeal effect of the water extract of Melastoma malabathricum Linn. (Melastomataceae) leaves were investigated by employing four experimental models of diarrhea in Swiss mice. Melastoma malabathricum water extract treated mice showed significant reduction in the fecal output and protected them from castor oil-induced diarrhoea. The extract also reduced the intestinal fluid secretion induced by magnesium sulphate and gastrointestinal motility after charcoal meal administration in the mice. No mortality and visible signs of general weakness was observed in the mice following the test extract administration up to 2000 mg/kg dose.     

Antidiarrhoeal activity of the standardised extract of <Emphasis Type="Italic">Cinnamomum tamala</Emphasis> in experimental rats

The present study was designed to investigate the antidiarrhoeal potential of 50% ethanolic extract of Cinnamomum tamala on experimentally induced castor oil diarrhoea, gastric emptying of phenol red meal, gastrointestinal transit of charcoal meal and in vitro mast cell degranulation activity. C. tamala extract (25, 50 and 100 mg/kg, orally) produced a dose-dependent reduction in the total amount of faecal matter in castor oil-induced diarrhoea. The mean distance travelled by charcoal meal at 50 and 100 mg/kg of extract showed a significant reduction in the secretion of gastrointestinal fluid accumulation by 32.5–65.0%. The Na⁺ and K⁺ concentrations on castor oil-induced fluid accumulation showed a greater inhibitory effect on Na⁺ levels than on K⁺ concentrations. C. tamala significantly reduced the lipid peroxidation (P < 0.001) and increased the catalase (P < 0.01) activity in comparison to the castor oil-induced groups. C. tamala leaf extract did not show any significant effect at a higher dose (15 mg/ml) on mast cell degranulation. However, the extract in the dose of 5 and 10 mg/ml conferred significant mast cell protective action (P < 0.001). The percentage of eugenol in extract is 3.8% w/w, and total tannin is 247.5 mg/g. The result indicates the Indian spice C. tamala is useful for diarrhoea.     

Anti-Inflammatory,Antipyretic And Antispasmodic Properties Of Chromolaena Odorata

A methanol extract of the leaves of Chromolaena odorata was evaluated for anti-inflammatory effects in the carrageenan-induced rat paw edema model as well as for antipyretic activity in mice. The effects of the extract on intestinal transit of charcoal meal and castor oil-induced diarrhoea were also investigated. The extract (50-200 mg/kg) inhibited paw edema in rats and produced significant (p &lt;0.05) reduction in rectal temperature of mice rendered hyperthermic by yeast suspension. Antimotility and antidiarrhoeal effects were produced by the extract in intact mice. This study establishes the out-inflammatory, antipyretic, and anti-spasmodic properties of C. odorata.     

Evaluation of antinociceptive and antidiarrhoeal properties of Manilkara zapota leaves in Swiss albino mice

Context Manilkara zapota (L.). P. Royen. (Sapotaceae) has been used in folk medicine to treat pain, diarrhoea, inflammation, arthralgia, and other disorders.

Objective Screening of Manilkara zapota leaves ethanol extract and its different solvent soluble fractions for possible antinociceptive and antidiarrhoeal activities in Swiss albino mice.

Materials and methods The extract and various fractions (200 and 400?mg/kg body weight; p.o.) were tested for peripheral and central antinociceptive activity by acetic acid-induced writhing and radiant heat tail-flick method, respectively; castor oil-induced diarrhoeal model was used to evaluate antidiarrhoeal activity at both doses. All the samples were administered once in a day and the duration of study was approximately 5?h.

Results Ethanol extract (400?mg/kg), petroleum ether fraction (400?mg/kg), and ethyl acetate fraction (400?mg/kg) showed significant peripheral antinociceptive activity having 59.89, 58.24, and 46.7% (p?<?0.001) of writhing inhibition, respectively, which is comparable with that of standard diclofenac (59.34% inhibition). The ethanol extract (400?mg/kg) and petroleum ether fraction (400?mg/kg) also showed promising central analgesic activity having 74.15 and 82.15% (p?<?0.001) elongation of reaction time, respectively, at 90?min after administration of sample which is also similar to that obtained by morphine (85.84% elongation). In antidiarrhoeal activity screening, ethanol extract (200 and 400?mg/kg) showed significant inhibition of defecation by 53.57 and 60.71%, respectively (p?<?0.001) compared with that of loperamide (71.42%).

Discussion and conclusion The findings of the studies demonstrated antinociceptive and antidiarrhoeal activities of M. zapota leaves which could be the therapeutic option against pain and diarrhoeal disease.     

Investigation on the gastroprotective and antidiarrhoeal properties of Aegle marmelos unripe fruit extract

The Study was designed to verify the gastroprotective and antidiarrhoeal effects of unripe fruit extract of Aegle marmelos Corr. The gastroprotective function of this extract was evaluated in rats against gastric mucosal damage induced by hypothermic restraint stress, absolute ethanol, and indomethacin, whereas the antidiarrhoeal activity was investigated by studying the influence on gastrointestinal transit as measured by a charcoal marker and on castor oil-induced accumulation of intestinal fluid in mice and also on contractile responses evoked by acetylcholine, histamine, serotonin, and barium chloride in isolated guinea-pig ileum, the results demonstrated that pretreatment of animals with unripe fruit extract (50 and 100 mg/kg, i.p.) produces a significant inhibition of gastric lesion induced by ethanol but not those induced by restraint stress or indomethacin and suggest a probable involvement of a prostaglandin-independent mechanism of gastroprotection. At similar doses, both the intestinal transit as well as the accumulation of intestinal fluids induced by castor oil in mice were significantly inhibited by raw fruit extract. Furthermore, the extract antagonized the contractile responses evoked by different agonists on guinea-pig ileum in vitro and its inhibitory potential for the drugs are in the order of acetylcholine > histamine > serotonin > barium chloride. Taken together, these results point out a possible antidiarrhoeal effect of unripe fruit extract of A. marmelos Corr., since inhibition of intestinal motility and secretion can control clinical diarrhoea.     

Antidiarrhoeal Activity of New Thiazolidinones Related to Loperamide

A series of thiazolidinones related to loperamide was synthesized and evaluated for antidiarrhoeal activity in mice, using the castor oil test. Of five compounds tested, antidiarrhoeal activity was found only for 2?(p-nitrophenyl)?3?{3?[(4?(p-chloro-phenyl)-4?hydroxy)piperidino]ethyl}-1,3?thiazolidin?4?one. The compound was less active than loperamide (ED50 values = 48.7 (24.8?95.6) and 0.91 (0.24?3.40) mg kg^?1, respectively), but was also less toxic (LD50 values = 745.9 (545.2?929.8) and 108.9 (85.5?138.7) mg kg^?1, respectively). Its antidiarrhoeal activity was counteracted by naloxone. Our results support the hypothesis that this compound, like loperamide, is an opiate-receptor agonist.     

Sulphated Polysaccharide Isolated from the Seaweed Gracilaria caudata Exerts an Antidiarrhoeal Effect in Rodents

Diarrhoea is a significant health problem for children in developing countries that causes more than 1 million deaths annually. This study aimed to evaluate the antidiarrhoeal effect of sulphated polysaccharide (PLS) from the alga Gracilaria caudata in rodents. For the evaluation, acute diarrhoea was induced in Wistar rats (150–200 g) by administration of castor oil (10 mg/kg). Then, different parameters, including enteropooling and gastrointestinal transit and its pharmacological modulation by opioid and cholinergic pathways, were assessed using activated charcoal in Swiss Mice (25–30 g). Secretory diarrhoea was examined using cholera toxin (CT) (1 mg/loop)‐treated, isolated intestinal loops from Swiss mice (25–30 g), which were also used to examine fluid secretion, loss of chloride ions into the intestinal lumen and absorption. In addition, a GM1‐dependent ELISA was used to evaluate the interaction between PLS, CT and the GM1 receptor. Pre‐treatment with PLS (10, 30 and 90 mg/kg) reduced faecal mass, diarrhoeal faeces and enteropooling. However, 90 mg/kg more effectively reduced these symptoms; therefore, it was used as the standard dose in subsequent experiments. Gastrointestinal transit was also reduced by PLS treatment via a cholinergic mechanism. Regarding the diarrhoea caused by CT, PLS reduced all study parameters, and the ELISA showed that PLS can interact with both the GM1 receptor and CT. These results show that PLS from G. caudata effectively improved the parameters observed in acute and secretory diarrhoea, which affects millions of people, and may lead to the development of a new alternative therapy for this disease.     

Assessment of the antidiarrhoeal properties of the aqueous extract and its soluble fractions of Chebulae Fructus (Terminalia chebula fruits)

Context Chebulae Fructus is used as an herbal remedy for diarrhoea in traditional Chinese medicine. However, there is no scientific evidence to support its antidiarrhoeal activity.

Objective This study evaluates the antidiarrhoeal properties of Chebulae Fructus aqueous extract (CFAE) and determines the active fraction.

Materials and methods The antidiarrhoeal effect of CFAE (200–800?mg/kg) was investigated by determining the wet dropping, intestinal transit in BALB/c mice and enteropooling in Wister rats. The protective effects of the CFAE on the intestinal and liver were tested by histopathological analyses. The antidiarrhoeal fraction was determined by castor oil-induced diarrhoea and its main constituents were identified by HPLC-ESI-MS.

Results The extract at doses of 200, 400 and 800?mg/kg reduced the diarrhoea by 9.1, 40.0 and 58.2% and inhibited intestinal transit by 18.3, 24.1 and 35.7%, respectively. Additionally, the CFAE (200, 400 and 800?mg/kg) decreased the volume of enteropooling by 47.1, 58.8 and 64.7%, respectively. Mice treated with castor oil presented morphological alterations in the small intestine and the liver. However, the lesions of mice treated with CFAE were alleviated. Moreover, the ethyl acetate fraction was the active fraction of CFAE, the fraction (41.7, 83.4 and 166.8?mg/kg) reduced the diarrhoea by 9.1, 38.2 and 54.5%, respectively. The major components of the ethyl acetate fraction were tannins, including gallic acid, 3, 4, 6-tri-O-galloyl-β-d-Glc, corilagin and ellagic acid according to the HPLC-ESI-MS analysis.

Conclusion The CFAE possessed antidiarrhoeal property and the ethyl acetate fraction was its main active fraction.     

Loperamide oxide in acute diarrhoea: a double-blind, placebo-controlled trial

Background: Loperamide is an established treatment of acute diarrhoea with only rare adverse reactions. The pro-drug loperamide oxide is converted to loperamide by anaerobic bacteria in the lower alimentary tract. With the use of loperamide oxide, it was expected to obtain similar antidiarrhoeal efficacy as with loperamide, but with a lower dose and a lower plasma concentration. The incidence of adverse reactions might be reduced with the use of loperamide oxide. Methods: Loperamide oxide (0.5 and 1 mg capsules) was compared with placebo in a double-blind treatment of acute diarrhoea of 242 patients. Relief of diarrhoea was significantly more rapid for either dose of loperamide oxide than for placebo. Both the investigators’and the patients’global assessment of the treatment significantly favoured the loperamide oxide 1 mg capsule, but not 0.5 mg, over placebo. Adverse experiences were less frequent in the drug-treated than in the placebo-treated group. Conclusion: These results suggest that loperamide oxide 1 mg produces effective relief of diarrhoeal symptoms.     

Evaluation of Antidiarrheal Potential of Emblica officinalis.

ABSTRACT

The antidiarrheal potential of the methanol extract of the fruit of Emblica officinalis. Gaertn. Euphorbiaceae was evaluated using several experimental models of diarrhea in Wistar albino rats. The methanol extract showed a significant inhibitory effect on rats with diarrhea induced by castor oil and magnesium sulfate. The methanol extract produced a significant reduction in gastrointestinal motility in charcoal meal tests in rats. It also significantly inhibited PGE₂-induced enteropooling as compared to control animals. The results obtained establish the efficacy and substantiate the use of this herbal remedy as a nonspecific treatment for diarrhea in folk medicine.     

Antidiarrheal Activity of the Fruits of Vitex doniana. in Laboratory Animals

Abstract

The effect of different doses of the aqueous extract of Vitex doniana. Sweet (Verbenaceae) on acetylcholine and histamine-induced contractions on isolated guinea pig ileum was evaluated. The effect of the extract on intestinal peristalsis and castor oil–induced diarrhea in mice was also studied. The results showed that the extract possess a concentration-dependent inhibition of both acetylcholine and histamine-induced contractions. The extract (at doses of 150–650 mg/kg) also inhibited gastric peristalsis in mice fed charcoal meal and significantly protected mice against castor oil–induced diarrhea. Phytochemical screening of the extract revealed the presence of anthraquinones, flavonoids, saponins, sterols, and tannins. The findings in this study indicate that the aqueous extract of V. doniana. fruits may contain some pharmacologically active components that perhaps will be useful as antidiarrheal agents. The findings have also validated the use of this plant in traditional cure of diarrhea.     

Pharmacological studies of loperamide, an anti-diarrheal agent. I. Effects on diarrhea induced by castor oil and prostaglandin E. (author's transl)]

Effects of loperamide on diarrhea induced by castor oil and prostaglandin E1 were investigated in rats and mice and compared with those of narcotic analgesics, atropine, mecamylamine and local anesthetics. The following results were obtained. Loperamide markedly suppressed the appearance of diarrhea induced by oral administration of castor oil in rats and the ED50 values for 1 and 2 hr protection was 0.082 and 0.42 mg/kg p.o., respectively. Loperamide markedly suppressed the appearance of diarrhea induced by i.v. administration of prostaglandin E1 and the ED50 value for 2 hr protection was 0.24 mg/kg p.o. in rats. The ID120 min value of loperamide which was calculated on the basis of the dose producing a 20% or more inhibition of the charcoal transport in the small intestine for 120 min was 0.8 mg/kg p.o. in mice and this activity was 9.2 times more potent than that of morphine. The analgesic ED50 value (Haffner's method) and LD50 value of loperamide was 149 and 249 mg/kg p.o., respectively. These results suggest that loperamide has a potent anti-diarrheal activity and specificity to the gastrointestinal tract and inhibits the effect of prostaglandin E1 and ricinoleic acid on the intestinal tract in rats.     

Anti-inflammatory Properties of Amaranthus spinosus Leaf Extract

The methanol extract of Amaranthus spinosus L. leaves was evaluated for anti-inflammatory activities in different animal models. The effect of the plant extract was also studied on castor oil–induced diarrhea and gastric mucosal integrity. The extract (25–100 mg/kg) inhibited the carrageenan-induced rat paw edema and produced significant (p < 0.05) inhibition of acetic acid–induced increased vascular permeability. Inhibition of the cotton pellet granuloma was also inhibited by 100 mg/kg of the plant extract. Analgesic activity was exhibited with the significant and dose-related reduction in the number of writhings induced with acetic acid, as well reduction in paw licking induced by injection of formalin in mice. The extract (50 and 100 mg/kg) produced gastric erosion in rats, following repeated administration for 4 days, and with 25–100 mg/kg of the extract, there was a statistically significant (p < 0.05) reduction in castor oil–induced diarrhea in rats. These results demonstrate the anti-inflammatory properties of the leaf extract of A. spinosus. It is also suggested that the plant extract probably acts by the inhibition of prostaglandin biosynthesis.     

Role of the Rosa canina L. leaf extract as an antidiarrheal drug in rodents

Objectives:

The objective of the study was to investigate the effect of the leaf extract of Rosa canina L. against experimental diarrhea induced by castor oil in rodents.

Materials and Methods:

The methanol extract of Rosa canina L. (30 and 60 mg/kg body weight) was administered orally to two groups of mice (five animals per group) in order to evaluate the activity of the extract against the castor oil-induced diarrhea model in mice. Two other groups received normal saline and diphenoxylate (5 mg/kg) as positive control. The effect of the extract on intestinal transit and castor oil-induced intestinal fluid accumulation (enteropooling) was assessed. The effects of the extract on the isolated rabbit jejunum and on the isolated rat ileum were studied.

Results:

The preliminary phytochemical screening of the leaf extract of Rosa Canina L. revealed the presence of alkaloids, flavonoids, glycosides, saponins, and volatile oil. Intraperitoneal LD50 of the extract was found to be 455.19 ± 23 mg/kg in mice. The antidiarrheal effect of the methanolic extract exhibited a concentration-dependent inhibition of the spontaneous pendular movement of the isolated rabbit jejunum and inhibited acetylcholine-induced contraction of the rat ileum. A dose-dependent decrease in gastrointestinal transit was observed with extracts (30 and 60 mg/kg), which also protected mice against castor oil-induced diarrhea and castor oil-induced fluid accumulation, respectively.

Conclusions:

The presence of some of the phytochemicals in the leaf extract may be responsible for the observed effects, and also the basis for its use in traditional medicine as an antidiarrheal drug.     

Antidiarrhoeal activity of piperine in mice

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.     

A mechanistic evaluation of the traditional uses of Nepeta ruderalis in gastrointestinal and airway disorders

Context: Nepeta ruderalis Buch.-Ham. (Lamiaceae), locally known as Badranj Boya, is an aromatic herb used traditionally as an antispasmodic, antidiarrhoeal, and anti-asthamatic remedy.

Objective: Aqueous methanolic extract of N. ruderalis was studied to investigate its traditional uses.

Materials and methods: Study was conducted from September 2015 to February 2016. In vitro spasmolytic and broncho-relaxant activity of crude extract of N. ruderalis (whole plant) was evaluated at 0.01–10?mg/mL final bath concentration in isolated rabbit jejunum and tracheal tissues, using PowerLab data acquisition system (Transonic Systems Inc., Ithaca, NY). In vivo antidiarrhoeal activity was evaluated in castor oil-induced diarrhoeal mice at the dose of 300 and 500?mg of crude extract orally.

Results: Crude extract of N. ruderalis completely relaxed spontaneously contracting, high K⁺ (80?mM) and carbachol (1?μM) induced contracted jejunum with an EC₅₀ value of 5.85 (5.45–6.27), 4.0 (3.80–4.23) and 2.86 (2.48–3.29), similar to verapamil. Nr.Cr relaxed high K⁺ and carbachol induced contractions, at 5 and 10?mg/mL with an EC₅₀ value of 2.37 (2.11–2.67) and 3.26 (2.9–3.67), respectively, and also displaced calcium concentration–response curves toward right at 0.1 and 0.3?mg/mL. Nr.Cr exhibited antidiarrhoeal protection at a dose of 300 and 500?mg/kg, similar to verapamil, whereas no acute toxicity signs were seen up to 5?g/kg in healthy mice.

Discussion and conclusion: Results suggest the presence of spasmolytic and broncho-relaxant effects in the crude extract of N. ruderalis, possibly mediated through calcium channel-blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal and airway disorders.     

Naloxone inhibits the anti-diarrhoeal activity of loperamide.

1 Subcutaneous prostaglandin E2 (2.5 mg/kg) produces profuse diarrhoea in fed rats. 2 Pretreatment of rats with subcutaneous loperamide (1.0 mg/kg) completely prevents prostaglandin-induced diarrhoea. If naloxone is administered prior to loperamide injections the activity of the antidiarrhoeal compound is completely destroyed. 3 These data provide strong evidence that the antidiarrhoeal activity of loperamide is mediated via the opiate receptor.     

Suppression of castor oil-induced diarrhoea by α2-adrenoceptor agonists

The effects of systemic administration of alpha 2-adrenoceptor agonists on migrating myoelectric complexes and castor oil-induced diarrhoea of the small intestine were studied in conscious rats. Castor oil (1 mg/kg, intraduodenally) disrupted the migrating myoelectric complexes and induced irregular spiking activity with sporadic bursts of myoelectric activity. This change of motility pattern was present concomitant with diarrhoea 1-2 h after instillation of castor oil and during the whole period of diarrhoea. Pre-treatment with clonidine (5-10 micrograms/kg i.v.) or oxymetazoline (5.6-11.2 micrograms/kg i.v.), a peripherally active alpha 2-agonist, inhibited the irregular spiking induced by castor oil and no diarrhoea occurred during the experimental period of 6 h. Thus, the antidiarrhoeal action of peripherally acting alpha 2-adrenoceptor agonists such as oxymetazoline, may be of clinical value in the treatment of diarrhoea.     

Antidiarrheal Activity of the Aqueous Extract of Punica granatum. (Pomegranate) Peels

Abstract

The antidiarrheal effects of the aqueous extract of Punica granatum. L. (Punicaceae) peels were evaluated in rats. Studies were carried out on the isolated rat ileum, gastrointestinal motility in vivo., and on castor oil–induced diarrhea in rats. The results revealed that the extract exhibited a concentration-dependent inhibition of the spontaneous movement of the isolated rat ileum and attenuated acetylcholine-induced contractions. The extract (100, 200, 300, and 400 mg/kg) also caused a dose-dependent decrease of gastrointestinal transit and markedly protected rats against castor oil–induced diarrhea enteropooling. The intraperitoneal injection LD₅₀ of the extract was found to be 1321 ± 15 mg/kg in mice. A preliminary phytochemical screening of the aqueous extract of Punica granatum. peels gave positive tests for tannins, flavonoids, and alkaloids. The results obtained showed that the aqueous extract of Punica granatum. peels may contain some biologically active principles that may be active against diarrhea, and this may be the basis for its traditional use for gastrointestinal disorders.