Castor Oil-induced Diarrhea Model Research Articles

Assessment of the Potential Mechanisms of Anti-diarrhoeal Activities of Ethanol Extract of Monoon longifolium Leave in Wistar Rat

Background: Numerous diseases related to diarrhea are the primary cause of morbidity and mortality in underdeveloped countries, accounting for hundreds of thousands of deaths annually. Polyalthia longifolia, the false ashoka, commonly referred to as Monoon longifolium is a tree species from Asia. It is commonly found in southern india, Sri Lanka and Nigeria. Polyalthia longifolia has been utilized for decades to treat an extensive variety of illnesses, including diarrhea. Method: The plant was extracted with ethanol using cold maceration. Preliminary qualitative and quantitative phytochemical screening of ethanol extract of Polyalthia longifolia leaf was conducted using the techniquees of Harbone (1998); Trease and Evans (1978). The Lorke (1983) approach was used to calculate the Median Lethal Dose (LD50). Diarrhea caused by castor oil was produced using the Awouter et al., 1973 method. The testing for gastrointestinal transit was conducted using the Mascolo et al. (1996) technique. The Tietz (1994) method was used to conduct the electrolyte levels assay. The assay for kidney function indicators was conducted using Bartels and Bohmer's (1972) methodology. Results: The results of phytochemical screening showed that alkaloids and tannins occurred in high concentration, flavonoids and steroids occurred in moderate concentration, whereas terpenoids, glycosides and phenolic acid occurred in lowest concentration. The acute toxicity study revealed that the plant extract was not toxic even at the dose of 5000 mg/kg. Groups treated with 200,400, and 600 mg/kg b.w of extract showed significant (P < 0.05) inhibition in the frequency of defecation of wet feces and total fecal output compared with positive control. Similarly, Groups treated with 200, 400, and 600 mg/kg body weight of extract demonstrated significant (P < 0.05) antimotility activity when compared with the positive control. However, groups treated with 200,400 and 600mg/kg body weight showed a significant (P < 0.05) increase in chlorine and sodium with corresponding decrease in bicarbonate and potassium level when compared with the positive control. The results from kidney function markers showed that groups treated with 200, 400 and 600 mg/kg b.w in a dose dependent manner showed a significant (p < 0.05) reduction in creatine and urea when compared with positive control. Conclusion: The ethanol leaf extract of Polyalthia longifolia has considerable antidiarrheal activity on castor oil-induced diarrhea and gastrointestinal motility models, confirming the reason for its wide use in traditional treatment of diarrheal conditions.

Chemical profiling, toxicity assessment, anti-diarrhoeal, anti-inflammatory and antinociceptive activities of Canarium schweinfurthii Engl. (Burseraceae) bark in rats

Ethnopharmacological relevanceThe bark of Canarium schweinfurthii is used in ethnomedicine for the treatment of diabetes, pain, malaria, fever and diarrhoea. Aim of the studyThe chemical phytoconstituents, antidiarrheal, anti-inflammatory and antinociceptive effects and safety profile of the aqueous extract of Canarium schweinfurthii bark (AECSB) were investigated. Materials and methodsGas chromatography-mass spectrometry (GC-MS) was used to analyse the phytochemical composition. In the acute toxicity test, AECSB were administered up to 2 g/kg by oral gavage. For the subacute toxicity test (28 days), rats in group 1 (control) received no AECSB, while rats in groups 2–4 were administered different doses of AECSB. Charcoal meal transit and castor oil-induced diarrhoea models were used to study the antidiarrheal effect, while egg albumin/carrageenan and acetic acid/tail immersion models were used for the anti-inflammatory and antinociceptive studies, respectively. With the exception of the acute toxicity experiment, AECSB was administered orally at doses of 200, 400 and 800 mg/kg. ResultsBioactive phytoconstituents identified include p-cymene, δ-terpinene, linalool and phytol. No adverse effects or mortality were observed in acute and subacute studies. Treatment with AECSB (28 days) had no significant effect on organ weight, biochemical, hematologic and histopathologic parameters compared to the control groups (p > 0.05). Comparable antidiarrheal and antinociceptive effects were observed in both AECSB- and standard drug-treated groups, while the 400 and 800 mg/kg AECSB-treated groups showed remarkable anti-inflammatory effects compared to the standard drug-treated and control groups (p < 0.05). ConclusionAECSB has antidiarrheal, antinociceptive and anti-inflammatory effects and can be safely used for therapeutic purposes.

Evaluation of Medicago sativa ethanol leaf extract for antidiarrheal activity in Wistar rats

Aim: Medicago sativa leaf is traditionally used for the treatment of gastrointestinal disorders in Nigeria. This research investigates the in vivo antidiarrheal activity of M. sativa (Alfalfa) leaf extract in Wistar rats. Method: The study employed three models: castor oil-induced diarrhea, gastrointestinal motility (charcoal meal), and castor oil-induced intestinal fluid accumulation. The phytochemical analysis as well acute toxicity tests were carried out in the leaf extract. Results: The results demonstrate a dose-dependent and significant antidiarrheal effect of M. sativa leaf extract. In the castor oil-induced diarrhea model, the extract reduced fecal frequency, delayed onset, and lowered severity, with the highest effect at 600 mg/kg compared to a positive control (Loperamide). Gastrointestinal motility was inhibited by the extract in a dose-dependent manner, achieving maximum effect at 600 mg/kg, comparable to atropine sulfate. The castor oil-induced intestinal fluid accumulation model revealed a significant decrease in fluid volume at 600 mg/kg, exhibiting a potent inhibitory effect. The oral LD50 values obtained were greater than 5000 mg/kg in rats Conclusion: This study provides compelling evidence of Medicago sativa leaf extract's potential as an antidiarrheal agent in Wistar rats. Further investigations could explore its mechanism of action and safety profile, contributing valuable insights to the development of novel antidiarrheal therapies.

Evaluation of the antidiarrheal activity of the Heliotropium indicum (Indian heliotrope) methanol leaf extract and formulation into oral suspensions

ABSTRACT Introduction: For many years, diarrhoea has been a leading cause of millions of annual deaths in both developing and developed regions. Consequently, searching for novel sources of antidiarrheal drugs has become a key emphasis in contemporary research Aim: This study aims to evaluate the safety and antidiarrheal potential of Heliotropium indicum methanol leaf extract (HIMLE) and to formulate stable suspensions for further application. Methods: The safety and antidiarrheal potential of Heliotropium indicum methanol leaf extract (HIMLE) were assessed, and stable suspensions were formulated and characterized. Phytochemical constituents were determined using standard methods Acute toxicity testing, conducted under the Organization for Economic Cooperation and Development-423 guidelines, revealed a lethal dose (LD50) greater than 3000 mg/kg body weight (bw). Antidiarrheal effects were evaluated using a castor oil-induced diarrhoea model in Wistar rats, with groups receiving different doses of HIMLE and control. Results: The phytochemical screening revealed the presence of Flavonoids, Phenols, Tannins, Saponins, Alkaloids and Steroids. The extract demonstrated a dose-dependent reduction in intestinal transit and frequency of watery stool, with promising results compared to the positive control, loperamide. Structured vehicle suspensions, formulated at 1.25% w/v with carboxyl methylcellulose, polyvinylpyrrolidone, and tragacanth, exhibited stability over four weeks. The suspensions effectively inhibited diarrhoea in a dose-dependent manner. Formulations 4.60±2.73. 4.64±1.64 and 4.73±1.91 exhibit similar pH trends with slight variations, while Formulations 6.50±0.23 and 6.70±0.23 demonstrate higher pH values; additionally, viscosity tends to decrease as rotational speed decreases across all formulations. at 60 rpm.. Conclusion: The study suggests that HIMLE possesses significant antidiarrheal activity. The formulated suspensions proved effective in controlling diarrhoea in Wistar rats, highlighting the potential therapeutic application of Heliotropium indicum methanol leaf extract. His significant antidiarrheal activity could be accounted for by pharmacological effects. Keywords: Heliotropium indicum, methanol leaf extract, acute toxicity, structured vehicle, antidiarrhea

Pickle water ameliorates castor oil-induced diarrhea in mice by regulating the homeostasis of the gut microbiota and intestinal mucosal barrier.

Diarrhea is a common clinical condition that can potentially be fatal. Current treatment options often have side effects, such as constipation and vomiting, and there remains a need for more effective therapies. Pickled vegetables, a famous traditional food in China, have been suggested in clinical studies to alleviate diarrhea in children, particularly through the use of pickle water (PW). However, the pharmacological effects and mechanisms of PW on intestinal health remain unclear. This study aimed to explore the protective effects of PW on castor oil-induced diarrhea in ICR mice and to investigate its potential mechanisms. To evaluate the antidiarrheal effects of PW, we used a castor oil-induced diarrhea model in ICR mice. Various indices were measured to assess the severity of diarrhea. After euthanizing the mice, oxidative stress markers in the ileum were assessed using biochemical methods, and the expression of tight junction-related proteins in the ileum was analyzed using Western blot. Additionally, 16S rRNA high-throughput sequencing was used to evaluate the diversity and composition of the intestinal flora. The results showed that PW supplementation reduced body weight without significantly affecting organ index and liver function in the castor oil-induced diarrhea mice. PW also effectively reduced the dilution rate, diarrhea index, average loose stool grade, propelling distance of carbon powder, and intestinal propulsive rate while improving the pathological abnormality in the ileum. Furthermore, PW enhanced the activities of total antioxidant capacity (T-AOC), glutathione peroxidase (GSH-PX), and catalase (CAT) while reducing malonaldehyde (MDA) levels. PW also increased the expression of tight junction proteins zonula occludens-1 (ZO-1) and occludin in the ileum. Additionally, the analysis of 16S rDNA revealed that PW increased both α and β diversity, improved the composition of the intestinal flora, and restored it to a normal level. Collectively, dietary PW administration ameliorates Castor oil-induced diarrhea by restoring tight junctions between intestinal mucosal cells, suppressing oxidative stress, and regulating the composition of intestinal flora. These findings suggest that PW may be a promising strategy for managing diarrhea.

Antidiarrheal coumarins from Psydrax schimperianus (A. Rich.) Bridson roots

Ethnopharmacological relevancePsydrax schimperianus (A. Rich.) Bridson. roots are used for the treatment of diarrhea in West Arsi zone, Ethiopia. Aim of the studyThis study aimed to investigate the in vivo antidiarrheal activity of crude extract and coumarins isolated from the roots of Psydrax schimperianus to provide a pharmacological basis for its traditional use as an antidiarrheal agent in Ethiopia. Materials and methodsThe crude root extract of P. schimperianus was tested in vivo for antidiarrheal efficacy in mice utilizing castor oil-induced diarrhea, gastrointestinal transit time, and enteropooling models at doses of 100, 200, and 400 mg/kg. Phytochemical investigation of the crude root extract led to the isolation of two coumarins, isoscopoletin, and scoparone. Isoscopoletin and scoparone were evaluated for antidiarrheal activity against castor oil-induced diarrhea model at 10 mg/kg and 20 mg/kg doses. ResultsThe crude root extract of P. schimperianus, at doses of 100, 200, and 400 mg/kg, inhibited defecation by 37.5%, 46.2%, and 61.2%, respectively. At a dose of 20 mg/kg, scoparone and isoscopoletin reduced defecation by 61.2% and 66.6%, respectively. ConclusionThe study warrants further investigation of isoscopoletin and scoparone towards development as a novel treatment for diarrheal diseases.

Ethanol Extract of Glycyrrhiza uralensis Fisch: Antidiarrheal Activity in Mice and Contraction Effect in Isolated Rabbit Jejunum.

To evaluate the antidiarrheal effect of ethanol extract of Glycyrrhiza uralensis Fisch root (GFR) in vivo and jejunal contraction in vitro. In vivo, 50 mice were divided into negative control, positive control (verapamil), low-, medium- and high-dose GFR (250, 500, 1,000 mg/kg) groups by a random number table, 10 mice in each group. The antidiarrheal activity was evaluated in castor oil-induced diarrhea mice model by evacuation index (EI). In vitro, the effects of GFR (0.01, 0.03, 0.1, 0.3, 1, 3, and 10 g/L) on the spontaneous contraction of isolated smooth muscle of rabbit jejunum and contraction of pretreated by Acetylcholine (ACh, 10 µmol/L) and KCl (60 mmol/L) were observed for 200 s. In addition, CaCl2 was accumulated to further study its mechanism after pretreating jejunal smooth muscle with GFR (1 and 3 g/L) or verapamil (0.03 and 0.1 µmol/L) in a Ca2+-free-high-K+ solution containing ethylene diamine tetraacetic acid (EDTA). GFR (500 and 1,000 mg/kg) significantly reduced EI in castor oil-induced diarrhea model mice (P<0.01). Meanwhile, GFR (0.01, 0.03, 0.1, 0.3, 1, 3, and 10 g/L) inhibited the spontaneous contraction of rabbit jejunum (P<0.05 or P<0.01). Contraction of jejunums samples pretreated by ACh and KCl with 50% effective concentration (EC50) values was 1.05 (0.71-1.24), 0.34 (0.29-0.41) and 0.15 (0.11-0.20) g/L, respectively. In addition, GFR moved the concentration-effect curve of CaCl2 down to the right, showing a similar effect to verapamil. GFR can effectively against diarrhea and inhibit intestinal contraction, and these antidiarrheal effects may be based on blocking L-type Ca2+ channels and muscarinic receptors.

Evaluation of Antidiarrheal Activity of 80% Methanol Extract and Solvent Fractions of the Leaves of Withania somnifera (L.) Dunal in Swiss Albino Mice.

Background Withaniasomnifera is an important medicinal plant for the treatment of diarrhea in Ethiopian folklore medicine. The aim of this study was to evaluate the antidiarrheal activity of Withania somnifera leaves in Swiss albino mice. Materials and Methods Hydromethanolic crude extraction and solvent fractionation were done using cold maceration technique. 80% methanol was used as a solvent in crude extraction, while distilled water, n-butanol, and chloroform were employed during fractionation. Castor oil-induced diarrhea, enteropooling, and gastrointestinal motility models were employed to evaluate antidiarrheal activity. Mice were randomly divided into five groups (six mice per group): negative control, which received 2% Tween 80 in distilled water; positive control, which received 3 mg/kg loperamide; and three test groups (III, IV, and V), which were treated with 100 mg/kg, 200 mg/kg, and 400 mg/kg of crude extract and solvent fractions, respectively. Results The crude extract, aqueous, and n-butanol fractions significantly delayed the onset of diarrhea at 200 mg/kg and 400 mg/kg dose. There was a significant reduction in the number and weight of stools at all tested doses of the crude extract and aqueous fraction, and at 200 mg/kg and 400 mg/kg of n-butanol fraction. Significant reduction in volume and weight of intestinal contents was observed at all tested doses of the crude extract, and at 200 mg/kg and 400 mg/kg of aqueous and n-butanol fractions. All tested doses of the crude extract and 200 mg/kg and 400 mg/kg of the aqueous and n-butanol fractions significantly reduced the motility of charcoal meal. Conclusion This study demonstrated that the crude extract and solvent fractions of the Withania somnifera leaves have antidiarrheal activity and supported the folklore use of the plant.

Dual Inhibition of Phosphodiesterase and Ca++ Channels Explains the Medicinal Use of Balanites aegyptiaca (L.) in Hyperactive Gut Disorders.

The present study attempted to evaluate and rationalize the medicinal use of the methanolic extract of the fruits of Balanites aegyptiaca (B. aegyptiaca) in the treatment of hyperactive gut disorders. The in vivo, castor oil-induced diarrhea model in mice was followed to test its antidiarrheal effect. To test the antispasmodic effect and to explore its pharmacodynamic details, isolated small intestines (ileum) obtained from rats were selected to provide physiological conditions for the ex vivo assays. In the in vivo assays, the orally administered extract of B. aegyptiaca protected mice from diarrheal drops with resultant percent inhibitions of 40% and 80% at the respective doses of 200 mg/kg and 400 mg/kg, while the highest protection (100%) was observed with a positive control drug, loperamide, at 10 mg/kg. In the ileum, B. aegyptiaca produced an antispasmodic effect in a concentration-dependent manner by inhibiting the carbachol (CCh; 1 µM) and high K+ (80 mM)-evoked spasms with resultant EC50 values of 1.44 mg/mL (1.08–1.78) and 1.27 mg/mL (0.98–1.66), respectively. Papaverine, a known phosphodiesterase enzyme (PDE) inhibitor and blocker of Ca++ channels (CCB), also inhibited both CCh and high K+ induced contractions at comparable EC50 values of 8.72 µM (7.92–9.24) and 8.14 µM (7.62–8.84), respectively. Contrary to the extract and papaverine, verapamil showed distinctly higher potency in regard to inhibiting high K+, compared to CCh-evoked spasms that had EC50 values of 0.16 µM (0.13–0.261) and 2.54 µM (2.28–2.92), respectively. The inhibitory effects of B. aegyptiaca on PDE were further confirmed when the pre-incubated extract shifted the isoprenaline-mediated relaxation curves (CRCs) towards the left, similar to papaverine, whereas the CCB-like effect was confirmed when the pre-incubated tissues with B. aegyptiaca caused deflection in the Ca++ CRCs towards the right, constructed in Ca++ free medium with suppression of the maximum response. Thus, this study provides detailed, mechanistic support for the medicinal use of B. aegyptiaca in the treatment of hyperactive gut disorders.

Anti-diarrhoeal effect of methanol leaf fraction of Cola hispida Brenan and Keay in rats

Purpose: To evaluate the anti-diarrhoeal activity of 20 % methanol leaf fraction of Cola hispida (MLFC) using castor oil-induced diarrhoea model in rats.&#x0D; Methods: The activity of MLFC against castor oil-induced diarrhoea, intestinal fluid accumulation (enteropooling), and gastrointestinal motility were evaluated. The experimental animals were grouped into five, each with four animals. Group 1 received distilled water, while group 2 received loperamide and served as negative and standard control groups respectively. Groups 3 - 5 were administered 200, 400 and 600 mg/kg of MLFC respectively. One-hour post-treatment, castor oil (p.o.) was used to induce diarrhoea in all the groups. The activity of MLFC was tested against castor oil-induced looseness of stool, fluid accumulation in the intestine and intestinal motility of charcoal meal. Its effect on electrolyte concentration in the small intestinal content was assessed; furthermore, its effect on the electrolyte concentrations of Na+, Cl-, K+, and HCO3- in supernatants obtained from the intestinal loop effluents of the rats was evaluated.&#x0D; Results: The MLFC produced a significant (p &lt; 0.05) and dose-dependent decrease in the severity of diarrhoea and frequency of watery stool passed in castor oil-induced diarrhoea, enteropooling, gastrointestinal transit of charcoal meal in rats and serum concentrations of sodium and chloride ions, while significant (p &lt; 0.05) increase in potassium and bicarbonate ion concentrations were observed when compared with diarrhoeal control group. Similar inhibitory effects were obtained for loperamide control group.&#x0D; Conclusion: The results of the study indicate that methanol leaf fraction of Cola hispida possesses anti-diarrhoeal properties by inhibiting intestinal peristalsis and hypersecretion of water and electrolytes. Thus, the findings lend some support to the traditional use of the plant for the treatment of diarrhoea.

Anti-diarrhoeal effect of methanol leaf fraction of Cola hispida Brenan and Keay in rats

Purpose: To evaluate the anti-diarrhoeal activity of 20 % methanol leaf fraction of Cola hispida (MLFC) using castor oil-induced diarrhoea model in rats.&#x0D; Methods: The activity of MLFC against castor oil-induced diarrhoea, intestinal fluid accumulation (enteropooling), and gastrointestinal motility were evaluated. The experimental animals were grouped into five, each with four animals. Group 1 received distilled water, while group 2 received loperamide and served as negative and standard control groups respectively. Groups 3 - 5 were administered 200, 400 and 600 mg/kg of MLFC respectively. One-hour post-treatment, castor oil (p.o.) was used to induce diarrhoea in all the groups. The activity of MLFC was tested against castor oil-induced looseness of stool, fluid accumulation in the intestine and intestinal motility of charcoal meal. Its effect on electrolyte concentration in the small intestinal content was assessed; furthermore, its effect on the electrolyte concentrations of Na+, Cl-, K+, and HCO3- in supernatants obtained from the intestinal loop effluents of the rats was evaluated.&#x0D; Results: The MLFC produced a significant (p &lt; 0.05) and dose-dependent decrease in the severity of diarrhoea and frequency of watery stool passed in castor oil-induced diarrhoea, enteropooling, gastrointestinal transit of charcoal meal in rats and serum concentrations of sodium and chloride ions, while significant (p &lt; 0.05) increase in potassium and bicarbonate ion concentrations were observed when compared with diarrhoeal control group. Similar inhibitory effects were obtained for loperamide control group.&#x0D; Conclusion: The results of the study indicate that methanol leaf fraction of Cola hispida possesses anti-diarrhoeal properties by inhibiting intestinal peristalsis and hypersecretion of water and electrolytes. Thus, the findings lend some support to the traditional use of the plant for the treatment of diarrhoea.

Antidiarrheal Effect of 80% Methanol Extract and Fractions of Clerodendrum myricoides (Hochst.) Vatke (Lamiaceae) Leaf in Swiss Albino Mice.

Background Diarrhea is one of the tempting symptoms of diseases in the world. In Ethiopian traditional medicine practices, Clerodendrum myricoides is utilized for the treatment of diarrhea without scientific evidence. Objective This study was aimed to evaluate the antidiarrheal activity of 80% methanol extract and fractions of the leaf of Clerodendrum myricoides in mice. Methods The crude extract was prepared by maceration in 80% methanol and then fractionated using hexane, chloroform, and distilled water. Antidiarrheal activity was assessed by castor oil-induced diarrhea, enteropooling, and gastrointestinal motility models using onset of diarrhea, number and weight of feces, volume and weight of intestinal contents, and distance travelled by charcoal meal as main parameters. Negative controls received either distilled water or 2% Tween 80 (10 ml/kg), positive controls received 3 mg/kg loperamide or 1 mg/kg atropine, and the test groups received 100, 200, and 400 mg/kg doses of the extract. Results The crude extract and chloroform fraction significantly prolonged the onset of diarrhea at 200 and 400 mg/kg and decreased the number of wet, total, and weight of fresh feces at all tested doses. Hexane fraction has a significant antidiarrheal effect on the onset, number, and weight of feces at 400 mg/kg. The crude extract and chloroform fraction at all tested doses, as well as aqueous fraction at 200 mg/kg and 100 mg/kg, produced significant reduction in volume and weight of intestinal contents. Additionally, hexane fraction showed significant reduction of volume and weight of the intestinal content at 400 mg/kg. In the gastrointestinal motility test model, both chloroform fraction and crude extract at all tested doses and aqueous fraction at 200 mg/kg and 400 mg/kg showed a significant antidiarrheal effect as compared to the negative control. Conclusion The leaf of Clerodendrum myricoides showed antidiarrheal activity which supports the traditional use.

Polyphenolic profile and ethno pharmacological activities of Callistemonsubulatus (Cheel) Craven leaves cultivated in Egypt

Ethnopharmacological relevanceThe genus Callistemon (syn. Melaleuca) of the myrtle family (Myrtaceae) has been documented as an integral part in the ethnobotanical system of the indigenous people of Australian mainland and many of its islands. Several Callistemons including the species subulatus were used by aboriginal Australians for making rafts, roofs for shelters, bandages, and food recipes, in addition to the management of wounds, infections, pain, cough, bronchitis, and gastrointestinal tract (GIT) disorders. Aim of the studyThe current study is designed to document the therapeutic effect of the aqueous methanolic extract (AME) of C. sabulatus Chell (syn. M. sabulata) leaves in the management of diarrhea and pain. Also, its influence on additional pharmacological modalities that are related to oxidative stress just as skin aging. Ultimately, the polyphenolic profile of the extract is disclosed and correlated to the aforementioned bioactivities. Materials and methodsThe extract was fractionated using various chromatography techniques and the structures of the isolated compounds were determined based on their chemical and spectral data. The antioxidant activity was assessed using multiple models, including 2,2-diphenyl-picrylhydrazyl (DPPH), oxygen radical absorbance capacity (ORAC) and β-carotene bleaching assays. The anti-skin aging effect was evaluated using different relevant enzymatic assays. The antinociceptive activity was investigated using acetic acid-induced writhing, hot plate test, and formalin-induced paw licking in mice models. The antidiarrheal activity was gauge using the castor oil induced diarrhea, enter pooling and gastrointestinal motility in vivo models. ResultsDiverse polyphenols, including quercetin-3-O-β-D-glucuronopyranoside (1), kaempferol-3-O-β-D-glucuronopyranoside (2), strictinin (3), quercetin-3-O-(2``-O-galloyl)-β-D-glucuronopyranoside (4), afzelin (5), di-galloyl glucose (6), mono-galloyl glucose (7), acacetin (8), apigenin-6,7-dimethyl ether (9), kaempferol trimethyl ether (10), dimethoxy chrysin (11), quercetin (12), kaempferol (13), methyl gallate (14), and gallic acid (15) were identified. The extract exhibited as significant antioxidant activity even better than that of Trolox or BHT. Moreover, it exerts elastase, tyrosinase, and collagenase inhibition activities, in addition to the significant peripheral and central analgesic activity in a dose-dependent manner (P < 0.0001). In castor oil induced diarrhea model, AME significantly prolonged the diarrhea onset, decreased the frequency of defecation, and weight of feces. Likewise, it exhibited a significant reduction in the gastrointestinal motility in charcoal meal model (P < 0.0001) and a considerable inhibitory effect on gastrointestinal transit and peristaltic index with all investigated doses (P < 0.0001). ConclusionEthnobotanicals are versatile resources for the management of various ailments by indigenous people and the experimental research is utmost to validate and uncover their pharmacological relevance. C. sabulatus leaves have strong antioxidant, analgesic, anti-skin aging, and antidiarrheal activities which are validated for the first time by various in vitro and in vivo models. The metabolic profile of the unprecedented AME of C. sabulatus leaves compromises a wide array of bioactive polyphenolic metabolites including, flavonoids, tannins, and phenolic acids that are correlated to the observed bioactivities. Altogether, ethnobotanicals with high and diverse contents of polyphenols are potential candidates for the management of various human aliments including neuropathies, GIT disorders, and skin aging conditions.

Antidiarrheal activity of aqueous extract of leaves of Euphorbia hirta L.

Context: Euphorbia hirta L. is widely distributed in the Indian subcontinent and has many ethnomedicinal uses. Traditionally, the leaves of E. hirta have been used as antidiarrheal agents, for bronchial and respiratory diseases and against conjunctivitis. Aims: To evaluate the antidiarrheal activity of the aqueous extract of leaves of Euphorbia hirta. Methods: Steam and aqueous extracts of leaves of E. hirta were evaluated for their antidiarrheal activity by in vitro antiprotozoal and antimicrobial activity testing, in vivo evaluation of % protection against diarrhea in castor-oil induced rat diarrhea model, gastrointestinal transit and enteropooling assays in rat model and ex vivo tissue contractility studies. Results: Steam and aqueous extracts of leaves of E. hirta demonstrated antiprotozoal activity against Entamoeba histolytica and Giardia lamblia with MICs ranging from 31.25-62.5 µg/mL to 125-250 µg/mL. Both the extracts showed antibacterial activity against Salmonella abony, Escherichia coli and Shigella boydii. In vivo antidiarrheal activity evaluation in castor-oil induced diarrhea model in rats revealed that the steam extract at a dose of 1621 mg/kg body weight (b.w.) produced % inhibition in defecation comparable to loperamide (4 mg/kg b.w.). Aqueous extract produced significant reduction in fecal output when compared to the untreated control group (p&lt;0.05). However, the extracts failed to have any significant effect on the gastrointestinal transit of charcoal meal in rats. Also, gastric fluid accumulation was significantly reduced by steam extract at 2162 mg/kg b.w. and aqueous extract at 100 mg/kg b.w. (p&lt;0.05) when compared to the untreated group. The smooth muscle relaxation produced by the steam extract on the isolated rat ileum was comparable to that produced by atropine (0.05-0.4 µg/mL). Conclusions: The results of this study provide support for the traditional use of Euphorbia hirta leaves as an antidiarrheal agent.

Methanolic Crude Extract of Hagenia abyssinica Possesses Significant Antidiarrheal Effect: Evidence for In Vivo Antidiarrheal Activity.

Background Hagenia abyssinica is one of the most commonly used medicinal plants for the treatment of diarrhea in Ethiopia. Therefore, this study aimed to evaluate the antidiarrheal effect of methanol crude extract of H. abyssinica leaves in mice. Methods Acute toxicity testing was conducted using Organization for Economic Cooperation and Development guidelines. The antidiarrheal activity of the crude extract of H. abyssinica was investigated using three animal models such as small intestine transit, enteropooling, and castor oil-induced diarrhea models. The extract was administered at three different doses (100, 200, and 400 mg/kg) to the test groups, while the positive control group received 3 mg/kg of loperamide and the negative control group received 10 ml/kg of vehicle (distilled water). Results The crude extract of H. abyssinica did not exhibit death at the limit dose (2 g/kg) throughout the observation period. In the castor oil-induced model, the crude extract at a dose of 200 and 400 mg/kg exhibited a significant (P < 0.05) antimotility effect as compared to the negative control. The crude extract revealed a significant reduction in the volume and weight of intestinal contents at 200 and 400 mg/kg doses of the extract. Moreover, the highest antidiarrheal index (ADI) was obtained with the dose of 400 mg/kg of crude extract, which was comparable to the standard drug. Conclusion The crude extract of Hagenia abyssinica possesses antidiarrheal activity and supports the traditional use of H. abyssinica for the management of diarrhea.

Effects of Essential Oils of Elettaria cardamomum Grown in India and Guatemala on Gram-Negative Bacteria and Gastrointestinal Disorders

The present study examined the chemical composition and antimicrobial and gastrointestinal activity of the essential oils of Elettaria cardamomum (L.) Maton harvested in India (EC-I) and Guatemala (EC-G). Monoterpenes were present in higher concentration in EC-I (83.24%) than in EC-G (73.03%), whereas sesquiterpenes were present in a higher concentration in EC-G (18.35%) than in EC-I (9.27%). Minimum inhibitory concentrations (MICs) of 0.5 and 0.25 mg/mL were demonstrated against Pseudomonas aeruginosa in EC-G and EC-I, respectively, whereas MICs of 1 and 0.5 mg/mL were demonstrated against Escherichia coli in EC-G and EC-I, respectively. The treatment with control had the highest kill-time potential, whereas the treatment with oils had shorter kill-time. EC-I was observed to be more potent in the castor oil-induced diarrhea model than EC-G. At 100 and 200 mg/kg, P.O., EC-I exhibited 40% and 80% protection, respectively, and EC-G exhibited 20% and 60% protection, respectively, in mice, whereas loperamide (10 mg/kg, i.p., positive control) exhibited 100% protection. In the in vitro experiments, EC-I inhibited both carbachol (CCh, 1 µM) and high K+ (80 mM)-induced contractions at significantly lower concentrations than EC-G. Thus, EC-I significantly inhibited P. aeruginosa and E. coli and exhibited more potent antidiarrheal and antispasmodic effects than EC-G.

Assessment of Antidiarrheal and Superoxide Scavenging Activities of Ethanolic Frond Extract from Stenochlaena palustris Bedd.

The present study aimed to evaluate the antidiarrheal and superoxide scavenging activities of ethanolic extract of Stenochlaena palustris, an edible fern from Blechnaceae family. The antidiarrheal activity was determined against castor oil induced diarrhea model, gastrointestinal transit and enteropooling tests in Swiss albino mice. The test groups received various doses (100, 200, and 400 mg/kg, body weight) of the extract, whereas positive control received loperamide (3 mg/kg, b.w.) and negative control was supplied with 1% tween-80 in distilled water (10 mL/kg, b.w.). At three test doses (100, 200 and 400 mg/kg), the extract showed significant (p 0.001) and dose dependent antidiarrheal activity in all models. The delay and reduction in the onset, frequency, and weight of diarrheic feces as well as inhibition of the gastrointestinal transit and intraluminal fluid accumulation were observed in all models and highly comparable to the standard loperamide. The extract also exhibited high inhibitory ability to scavenge superoxide anion (O₂SUP• –/SUP). The highest percentage inhibition of superoxide anion was found to be 84.32 ± 0.15% at the concentration 800 μg/mL.

Anti-Diarrhoeal Properties of Stem Bark of Cassia Abbreviataagainst Castor Oil-Induced Diarrhoea in Swiss Albino Mice

Objectives: The main objective of the study was to explore the in-vivo anti-diarrheal properties of Methanol, Ethanol, Hot and Coldwater fractions of Cassia abbreviata (Fabaceae) stem bark in mice model in order to validate its traditional use.&#x0D; Study Design: This study was an experimental based study, where we used 30 Swiss albino mice and these were divided into five groups of six mice.&#x0D; Methods: The test groups (group three, four and five) received various doses of the crude extracts (100, 200 and 400 mg/kg) respectively, whereas the positive control (group two) received Loperamide (5mg/kg) as standard reference drug and negative control (group one) received distilled water (10ml/kg). The antidiarrheal activity of the four extracts from stem bark of Cassia abbreviata were evaluated in a castor oil-induced diarrhea model in mice and compared with Loperamide. Whereas the effect of methanol extract on gastrointestinal motility was also determined by the oral administration of charcoal meal. Data was analyzed using STATA version 13, presented as means and standard deviation, ANOVA, Bonferroni post hoc and Pearson tests were done.&#x0D; Results: The severity of diarrhea was reduced significantly (p&lt;0.001) by the four extracts (400mg/kg doses) where Methanol, Ethanol, Hot and Coldwater extracts had 64.5%, 62.4%, 60.9% and 59.7% respectively, whereas the standard drug Loperamide had 67.7% diarrhea inhibition. This was evidenced by reduction in frequency of diarrheal episodes and stool outputs when compared to the control group. The intestinal peristalsis was significantly (p&lt;0.001) reduced by methanol extract (53.3%) at 400mg/kg when compared to Loperamide (65.5%). &#x0D; Conclusion: It was concluded that all the four extracts from the stem bark of Cassia abbreviata scientifically displayed anti-diarrheal properties, which require further scientific studies leading to identification of the actual compounds.

Pharmacological Activities of Crinum viviparum: A Laboratory-based Study

ABSTRACT The phytochemical composition of the ethanolic extract of Crinum viviparum was determined and the anti-bacterial, anti-inflammatory, thrombolytic, and anti-diarrheal activities were investigated by applying disc diffusion, egg albumin (in vitro), clot lysis, and castor oil-induced diarrhea model in mice (in vivo), respectively. The results suggested that the crude ethanolic extract of the plant contained alkaloids, tannins, flavonoids, steroids, and terpenoids. The extract was anti-bacterial against Escherichia coli, Bacillus subtilis, Staphylococcus aureus and Salmonella enterica. The plant showed anti-inflammatory and thrombolytic activities in a concentration-dependent manner. C. viviparum extract was anti-diarrheal in Swiss albino mice at 250 and 500 mg kg−1.

Antifungal activity and antidiarrheal activity via antimotility mechanisms of (-)-fenchone in experimental models.

BACKGROUND(-)-Fenchone is a bicyclic monoterpene present in essential oils of plant species, such as Foeniculum vulgare and Peumus boldus, used to treatment of gastrointestinal diseases. Pharmacological studies report its anti-inflammatory, antioxidant, and antinociceptive activity.AIMTo investigate antidiarrheal activity related to gastrointestinal motility, intestinal secretion and antimicrobial activity.METHODSA castor oil-induced diarrhea model was used to evaluate antidiarrheal activity. Intestinal transit and gastric emptying protocols were used to assess a possible antimotility effect. Muscarinic receptors, presynaptic α2-adrenergic and tissue adrenergic receptors, KATP channels, nitric oxide were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms. The antimicrobial activity was evaluated in the minimum inhibitory concentration model, the fractional inhibitory concentration index using the (-)-fenchone association method with standard antifungal agents.RESULTS(-)-Fenchone (75, 150 and 300 mg/kg) showed antidiarrheal activity, with a significant decrease in the evacuation index. This activity is possibly related to a percentage of reduced intestinal transit (75, 150 and 300 mg/kg). The antimotility effect of (-)-fenchone decreased in the presence of pilocarpine, yohimbine, propranolol, L-NG-nitroarginine methyl ester or glibenclamide. In the enteropooling model, no reduction in intestinal fluid weight was observed. (-)- Fenchone did not show antibacterial activity; on the other hand, inhibits the growth of strains of fungi with a minimum fungicide concentration of 32 μg/mL. However, when it was associated with amphotericin B, no synergism was observed.CONCLUSIONThe antidiarrheal effect of (-)-fenchone in this study involves antimotility effect and not involve antisecretory mechanisms. (-)-Fenchone presents antifungal activity; however, it did not show antibacterial activity.