Castor Oil-induced Diarrhea Research Articles

In vivo evaluation of anti-diarrheal activity of hydroalcoholic extract and solvent fractions of the leaf of Leucas deflexa Hook.f (Lamiaceae) in Rodents

The emergence of antibiotic-resistant bacteria has intensified the search for novel antidiarrheal drug. Plant-derived extracts offer promising alternatives due to their ability to modulate gut motility and enhance water absorption. The leaves of Leucas deflexa Hook.f., a plant native to Ethiopia, have been traditionally utilized in the treatment of diarrheal diseases. Nonetheless, its traditional application has yet to be scientifically confirmed. Hence, the aim of the present study was to evaluate antidiarrheal activity of the crude extract and fractions of the leaf of Leucas deflexa Hook.f (Lamiaceae). Healthy Swiss albino mice were randomly divided into five groups per experimental model: castor oil-induced diarrhea, gastrointestinal motility, and anti-enteropooling assays. The control group received distilled water (10 ml/kg), while the positive control was treated with loperamide (3 mg/kg). The remaining groups were administered various dosages (LD100, LD200, and LD400 mg/kg) of a hydroalcoholic extract or its fractions from Leucas deflexa Hook.f. The crude extract and chloroform fraction substantially (P < 0.001) delayed the onset of diarrhea, reduced fecal frequency, and decreased total fecal weight at all administered doses compared to the negative control. The butanol and aqueous fractions exhibited a substantial antidiarrheal effect at doses of 200 mg/kg and 400 mg/kg, respectively. All treatments, including the crude extract, chloroform, butanol, and aqueous fractions, substantially (P < 0.001) reduced the volume and weight of intestinal contents at various doses. Additionally, the chloroform, aqueous fraction, and crude extract at doses of 100, 200, and 400 mg/kg substantially inhibited gastrointestinal motility compared to the negative control. The results of this study corroborate the traditional use of Leucas deflexa leaves in the treatment of diarrhea. These findings give a scientific justification for further exploration of the underlying mechanisms and potential therapeutic applications of this plant extract.

Antidiarheal Activity of Methanol Seed Extract of Cola Acuminata Schott &amp; Endl (Malvaceae) In Mice

Cola acuminata nut extract has been shown to relax smooth muscles of the intestine in vitro, and this has made the plant popular as a potential antidiarrheal agent. This study aimed at evaluating the antidiarrheal activity of methanolic seed extract of Cola acuminata in mice. The extract was subjected to phytochemical analysis. The acute toxicity (LD50) study was conducted according to Lorke's method. The antidiarrheal activity was evaluated using castor oil-induced diarrhea and charcoal meal method in mice. Groups of mice were orally administered water (10 ml/kg), charcoal, Cola acuminata nut extract (150, 300 and 600 mg/kg), loperamide 2mg/kg, and atropine 1 mg/kg before castor oil. Phytochemical screening revealed the presence of alkaloids, cardiac glycosides, tannins, triterpenes, and saponins. The oral LD50 of the extract was estimated to be 2154 mg/kg. The extract produced a significant p &lt; 0.05 increase in time of onset of diarrhea compared to the distilled water group. The extract produced dose dependent inhibition of the number of wet faeces. Extract at 600 mg/kg had more protection against diarrhea than the Loperamide. The extract did not significantly (p &gt; 0.05) affect the intestinal movement of charcoal meal.

Phytochemical Screening, Antioxidant, Cytotoxic, Analgesic, Antidiarrheal Activity and GC-MS Analysis of the Leaves of Stachyphrynium Placentarium

The goal of the present study is to analyze the phytochemicals, antioxidants, cytotoxic, analgesic and anti-diarrheal properties of the leaves of Stachyphrynium placentarium methanol extract as well as its dichloromethane soluble fraction using GC-MS technique. The leaves of the S. placentarium were extracted with methanol and designated as SPM. Phytochemicals investigation exhibited the presence of several important secondary metabolites. Antioxidants such as total phenolic content, flavonoids content, total antioxidant, reducing power capacity and DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay SPM revealed non-significant antioxidant properties. The cytotoxicity study of the extract showed significant cytotoxicity (LC50 35.1093 µg/mL) compared to standard vincristine sulfate (LC50 0.482 µg/mL). Analgesic study of S. placentarium by hot plate model indicates both the doses exhibited significant central analgesic activity compared with the control. The maximum analgesic activity was observed at 90 min. SPM (500 mg/kg) is 60.21 %. SPM250 also showed a significant percentage of elongation or latency from 30 to 150 min 57.00, 59.64, 59.88, 58.07 and 53.71 %, respectively 30 min time interval. In the acetic acid writhing test, S. placentarium significantly outperformed the control and standard (SPM250 - 52.27 %, SPM500 - 34.09 and STD - 27.27 %), showing a significant increase in peripheral analgesic activity (p &lt; 0.001). Antidiarrheal activity of SPM showed that SPM250 and SPM500 substantially decreased the feces in castor oil-induced diarrhea (p &lt; 0.05). According to the study, the incidence and severity of diarrhea are significantly reduced by SPM500. Four chemicals are found in the dichloromethane-soluble portion of the methanol extract of S. placentarium leaves, according to GC-MS studies such as Octadecane, 6-methyl- (1.326 %), Dodecane (1.02 %), 1-Iodo-2-methylundecane (0.47 %), tetradecanoic acid 12-methyl, methyl ester (72.64 %). Tetradecanoic acid exhibits anti-inflammatory, anticancer, 5-reductase inhibitory, antioxidant, hemolytic and antifibrinolytic properties. HIGHLIGHTS The phytochemicals, antioxidants, cytotoxic, analgesic and anti-diarrheal properties of Stachyphrynium placentarium methanol extract (SPM) leaves. The dichloromethane soluble fraction is examined using Gas chromatography–mass spectrometry (GC-MS) and identified Octadecane, 6-methyl-, Dodecane, 1-Iodo-2-methylundecane, tetradecanoic acid 12-methyl, methyl ester. The brine shrimp lethality test exhibited that SPM has significant cytotoxicity (LC50 35.1093 µg/mL) compared to vincristine sulphate (LC50 0.482µg/mL), the extract showed significant cytotoxicity (LC50 35.1093 µg/mL). S. placentarium at both dosages (250 and 500 mg) provided significant central analgesia compared to the control in a hot plate model. In the acetic acid writhing test, S. placentarium showed significantly higher peripheral analgesic action (SPM250 - 52.27, SPM500 - 34.09 and STD - 27.27 %) compared to control and standard. In castor oil-induced diarrhoea, SPM250 and SPM500 (250 and 500 mg) showed significantly reduced faeces production (p &lt; 0.05). GRAPHICAL ABSTRACT

Unveiling the therapeutic potentialities and chemical characterization of methanolic Merremia vitifolia (Burm.f) Hallier f. stem extract: A Multi-faceted investigation via in vitro, in vivo, and in silico approaches

Current study focused on Merremia vitifolia an ethnomedicinal plant, aiming to explore its medicinal properties comprehensively. Through qualitative and quantitative analysis, the study investigated the phytochemical components of M. vitifolia stem extract and assessed its antioxidant, anti-inflammatory, analgesic, antidepressant, anxiolytic, locomotor, and antidiarrheal activities. The evaluation involved a combination of in vitro, in vivo, and in silico approaches.In-vitro antioxidant activity was determined using the DPPH scavenging assay, while anti-inflammatory activity was assessed via a protein denaturation assay. In-vivo experiments included tests for antidepressant effects (FST, TST), anxiolytic effects (EPM, HBT), locomotor effects (OFT, HCT), and analgesic activity (formalin-induced licking test and acetic acid-induced writhing test). Additionally, the antidiarrheal effect was evaluated through castor oil-induced diarrhea and gastrointestinal motility tests. Fifteen bioactive compounds were identified based on their biological activities from GC/MS data and subjected to in silico molecular docking; ADME/T profiling and pass prediction.MEMVS had an IC50 value of 74.97 μg/mL and MEMVS elicited 77.17 ± 0.39 % inhibition protein denaturation compared to standard (87.23 ± 0.30 %) at 500 μg/mL. In addition, MEMVS induced a dose-dependent reduction in analgesic, neuropharmacological assay, inhibition in diarrheal feces count, and intestinal motility with a significant value (aP< 0.001). In computer-aided investigation, all compounds adhere to Lipinski's rule of five and demonstrate highest binding affinity to isolates compared to standard drugs, confirming laboratory findings.Research findings suggest that MEMVS holds promising potential, as a multifaceted therapeutic agent, exhibiting antioxidant, analgesic, anti-inflammatory, anti-diarrheal and neuropharmacological properties. However, further investigation is needed to fully harness its medicinal benefits.

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 &lt; 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 &lt; 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 &lt; 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 &lt; 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.

Antidiarrheal, anti-inflammatory and antioxidant effects of Anethum graveolens L. fruit extract on castor oil-induced diarrhea in rats.

Between food and medicine, nutraceuticals are widely used in human health for the prevention and treatment of various diseases. This study aims to determine the cytoprotective effects of Anethum gravelons fruit extract (AGFAE) on castor oil-induced diarrhea in rats due to its phytochemical and antioxidant properties. Male rats were divided into six groups of six animals each: Control (C), Castor oil (CO), CO + different doses of AGFAE (50, 100, and 200 mg/kg, b.w., p.o.), and the CO + loperamide group (LOP, 10 mg/kg, b.w., p.o.). In vitro, the chemical composition of aqueous Dill fruit extract showed strong antioxidant activity, with a high content of total polyphenols, flavonoids, and tannins. In our invivo studies, pre-treatment with AGFAE reduced malondialdehyde and hydrogen peroxide levels and maintained normal activity of enzymatic and non-enzymatic antioxidants in the gastric and intestinal mucosa. In addition, we found that AGFAE prophylaxis improved the stability of many plasma biochemical parameters altered by castor oil intoxication, such as C-reactive protein concentrations and alkaline phosphatase activities. We suggest that AGFAE phenolic compounds had significant protection against diarrhea involving several mechanisms such as reducing hypersecretion, peristaltic, inflammation, and preserving the endogenous antioxidant levels.

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.

ANTIDIARRHOEAL POTENTIAL OF FRACTIONS OBTAINED FROM METHANOL EXTRACT OF BRIDELIA ATROVIRIDIS (EUPHORBIACEAE) LEAVES ON CASTOR OIL-INDUCED DIARRHOEA IN SWISS ALBINO MICE

Background: Diar r hoea constitutes a major health concern, especially for children under the age of five. Orthodox drugs available for the treatment of diarrhoea are fraught with some challenges not limited to high cost, adulteration and toxic side effects, thereby making a case for alternative remedies, with several medicinal plants known to contain biologically active components that possess curative properties against diarrhoea.Objective: The study was under taken to evaluate the effect of fr actions (ethylacetate, n-butanol and residual aqueous) obtained from methanol extract of Bridelia atroviridis leaves on castor oil induced diarrhoea in Swiss albino mice.Methods: Powder ed plant mater ial was extr acted with absolute methanol using soxhlet apparatus and further fractionated successively with ethyl acetate, n-butanol and distilled water. In castor oil-induced diarrhoea, castor oil-induced enteropooling and electrolyte concentration tests, fasted mice divided into nine (9) groups of five mice each were administered 250 and 500 mg/kg of fractions obtained from B atroviridis leaves while standard drug (loperamide) was administered at 3 mg/kg.Results: However , only aqueous fraction (250 and 500 mg/kg) showed significant (p&lt;0.05) difference in volume of intestinal content when compared to castor oil control group.Conclusions: This study provides scientific data on the antidiarrhoeal potential of fractions obtained from methanol extract of Bridelia atroviridis leaves on castor oil-induced diarrhoea in Swiss albino mice, hence justifying its use in traditional medicine.

Antidepressant, Antidiarrheal, Thrombolytic and Phytochemical Profiling of Ethanol Extract of Amomum aromaticum Leaves: In vivo and In vitro Approaches

The study evaluated several pharmacological effects including antidepressant, antidiarrheal and thrombolytic activities of ethanol extract of Amomum aromaticum leaves (EEAA). Upon the assessment for qualitative phytochemical groups in the extract, several doses of EEAA (1000 - 4000 mg/kg) were studied to find acute oral toxicity in mouse for safe dose selection. Then EEAA was tested whether it demonstrates antidepressant activity in tail suspension test (TST) and forced swim test (FST). Antidiarrheal and clot lysis activities of EEAA were evaluated in castor oil-induced diarrhoea in mouse and In vitro clot lysis method, respectively. Oral administration of EEAA (1000 - 4000 mg/kg) showed no morality after 10 days, and no sign of acute toxicity observed within 24 hrs post-treatment. The qualitative phytochemical screening showed the presence of carbohydrate, alkaloid, flavonoid, tannin, saponin, and polyphenol groups in EEAA. The TST and FST resulted with significant improvement in mobility in mice treated with EEAA (400 mg/kg), where fluoxetine (20 mg/kg) was used as standard in both tests. EEAA treatment also showed a moderate dose-dependent anti-diarrheal effect. The 400 mg/kg oral dosing for 14 days decreased the rate of defecation by 52.8% compared to the control group. This study also demonstrated that EEAA possesses clot lysis activity. Hence, further intense investigations are suggested to identify specific potential active phytochemicals. Bangladesh Pharmaceutical Journal 27(1): 51-58, 2024 (January)

In-Vivo Antidiarrhoea Evaluations of Methanol Leaf Extract and Fractions of Chrysophyllum albidum

Background and Objectives: In Nigeria, traditional use of medicinal plants, like Chrysophyllum albidum, for diarrhoea persists. This study assessed its effectiveness in treating diarrhoea in rats. Methods: Extract and Fractions from the plant were tested for antidiarrhoea effect. The process involved methanol extraction and fractionation using hexane, ethyl acetate, and butanol. Rat models were used to evaluate the effects on castor oil-induced diarrhoea, enteropooling, and gastrointestinal motility. Results: Defecation caused by castor oil-induced diarrhoea was inhibited significantly by 53.55, 78.48 and 74.69 % at 500 mg/kg of methanol extract, ethyl acetate, and n-hexane fraction respectively, and by 50.99 and 63.69 % at 250 and 500 mg/kg of butanol fraction respectively. The volume of intestinal content and weight of intestinal content were reduced by 76.74 and 80 % at 500 mg/kg of ethyl acetate fraction. Also, the volume of intestinal content and weight of intestinal content were reduced by 70.93 and 70.83 % at 500 mg/kg of n-hexane fraction. At 250 and 500 mg/kg, the ethyl acetate fraction inhibited intestinal motility by 58.65% and 76.50% respectively. The n-hexane fraction at 500 mg/kg showed a 66.35% inhibition. Conclusion: These fractions from Chrysophyllum albidum leaves exhibit potential antidiarrhoea compounds, as evidenced across all three study models. Ongoing research aims to isolate these compounds for further investigation.

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.

Antispasmodic and antidiarrheal effects of Juniperus oxycedrus L. on the jejunum in rodents.

Functional bowel disorders (FBD) have a major potential to degrade the standards of public life. Juniperus oxycedrus L. (J. oxycedrus) (Cupressaceae) has been described as a plant used in traditional medicine as an antidiarrheal medication. The present study is the first to obtain information on the antispasmodic and antidiarrheic effects of J. oxycedrus aqueous extract through in vitro and in vivo studies. An aqueous extract of J. oxycedrus (AEJO) was extracted by decoctioning air-dried aerial sections of the plant. Antispasmodic activity was tested in an isolated jejunum segment of rats exposed to cumulative doses of drogue extract. The antidiarrheic activity was tested using diarrhea caused by castor oil, a transit study of the small intestine, and castor oil-induced enteropooling assays in mice. In the jejunum of rats, the AEJO (0.1, 0.3 and 1 mg/ml) diminished the maximum tone induced by low K+ (25 mM), while it exhibited a weak inhibitory effect on high K+ (75 mM) with an IC50=0.49 ± 0.01 mg/ml and IC50=2.65 ± 0.16 mg/ml, respectively. In the contractions induced by CCh (10-6 M), AEJO diminished the maximum tone, similar to that induced by low K+ (25 mM). with an IC50=0.45 ± 0.02 mg/ml. The inhibitory effect of AEJO on low K+ induced contractions was significantly diminished in the presence of glibenclamide (GB) (0.3 µM) and 4-aminopyrimidine (4-AP) (100 µM), with IC50 values of 1.84 ± 0.09 mg/ml. and 1.63 ± 0.16 mg/ml, respectively). The demonstrated inhibitory effect was similar to that produced by a non-competitive antagonist acting on cholinergic receptors and calcium channels. In castor oil-induced diarrhea in mice, AEJO (100, 200, and 400 mg/kg) caused an extension of the latency time, a reduced defecation frequency, and a decrease in the amount of wet feces compared to the untreated group (distilled water). Moreover, it showed a significant anti-motility effect and reduced the amount of fluid accumulated in the intestinal lumen at all tested doses. These findings support the conventional use of Juniperus oxycedrus L. as a remedy for gastrointestinal diseases.

Bioactivity-guided isolation of potential antidiarrheal constituents from Euphorbia hirta L. and molecular docking evaluation.

Euphorbia hirta L., a member of the Euphorbiaceae family, is extensively used as a folk medicine across various regions. In China, its decoction is traditionally consumed to alleviate diarrhea. This study aimed to evaluate the antidiarrheal activities of Euphorbia hirta and to identify its bioactive constituents through a bioactivity-guided isolation technique. Oral administration of E. hirta extract to mice was conducted to assess its effects on diarrhea. The anti-diarrheal effects were investigated in an aqueous extract and in three fractions of varying polarities derived from the aqueous extract, as well as in different eluates from D-101 macroporous resin, and in the compounds quercitrin and isoquercitrin, using mouse models with castor oil-induced diarrhea. The aqueous extract demonstrated significant anti-diarrheal activities in a dose-dependent manner in the castor oil-induced diarrheal model. Notably, the ethyl acetate (EtOAc) fraction showed prominent effects. Through bioactivity-guided isolation, two major compounds, isoquercitrin and quercitrin from the active fraction were found to possess antidiarrheal effects. Molecular docking studies revealed that the affinity energy of isoquercitrin and quercitrin were -8.5 and -8.2 kcal mol-1, respectively, which were comparable to the reference drug loperamide, with an affinity energy of -9.1 kcal mol-1. This research provides evidence supporting the development of E. hirta as a therapeutic agent for diarrhea, with isoquercitrin and quercitrin emerging as two key constituents that are likely responsible for its antidiarrheal activity. These findings validate the traditional use of E. hirta and highlight its potential as a natural treatment for diarrhea.

Exploring the Antidiarrheal Properties of Papaya Leaf: Insights In Vivo Study in Mice-Model and In Silico Analysis at M3 Muscarinic Acetylcholine Receptor Interaction.

Diarrhea caused by gut motility involves 5-HT3 serotonin receptor (5-HT3R) antagonist, M3 muscarinic acetylcholine receptor (M3-AchR), and H1 histamine receptor (H1R) via their respective agonist. Papaya (Carica papaya L.) leaf is an herbal medicine to treat diarrhea in Indonesia, though this has not yet been proven scientifically. This study aimed to determine the antidiarrheal properties of papaya leaf through in vivo and in silico studies. In the mice model, papaya leaves were infused with distilled water and subjected to in vivo antidiarrheal study using castor oil-induced diarrhea. In silico molecular docking study of nineteen secondary metabolites was carried out on the M3-AchR (PDB ID: 5ZHP) using AutoDock Tools 1.5.6, while ADMET was predicted by pre-ADMET. The results showed that papaya leaf infusion caused a decrease in the total number of feces, an increase in the onset time of diarrhea, a reduction in the frequency of diarrhea, and an increase in the percentage of inhibition of diarrhea. Quercetin 3-rutinoside, a flavonoid glycoside, is potentially an antidiarrheal remedy at M3-AchR. ADMET prediction showed good distribution on the target and was not toxic, but absorption needed to be considered. We concluded that the antidiarrheal activity of papaya leaf infusion was dose-dependent. Based on a molecular docking study, the flavonoid glycoside was very effective as an antidiarrheal remedy. ADMET prediction showed a specific distribution to the target and was not toxic.

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

Antidiarrheal Activities of the Methanol Leaf Extracts of Olinia rochetiana (Oliniaceae) Against Castor Oil-Induced Diarrhea in Mice.

Olinia rochetiana has been used traditionally to cure diarrheal disease. Therefore, this study aimed to investigate the acute toxicity and antidiarrheal effect of O. rochetiana leaf extracts. Cold maceration was used to extract plant leaf powder with 80% methanol. The extract's antidiarrheal action was tested against a castor oil-induced diarrheal model, a charcoal meal test, and enteropooling tests at doses of 100, 200, and 400 mg/kg. Negative controls received the vehicle at 10 mL/kg, while positive controls received loperamide at 3 mg/kg. From the study, no apparent toxicity was observed when a single dose of 2000 mg/kg was administered. In the castor oil-induced model, the extract delayed the onset of diarrhea, reduced stool frequency, and decreased wet feces weight and number in a dose-dependent manner at 200 mg/kg (p < 0.05) and 400 mg/kg (p < 0.01). The percent reduction in moist feces at 100, 200, and 400 mg/kg was 54.2, 23.97, and 18.26%, respectively, indicating a significant dose-dependent decrease. In a charcoal meal test, the extracts at 200 and 400 mg/kg revealed a peristaltic index of 65 and 46%, respectively, with considerable inhibition of charcoal transport at 23 and 39%. The weight and volume of intestinal contents dropped significantly at a dose of 400 mg/kg (p < 0.01), which is 0.43 mg/kg, in the enteropooling test when compared with the tested dose. The computed in vivo antidiarrheal index revealed diarrheal inhibition values of 46.06 and 71.06% at 200 and 400 mg/kg, respectively. In the current investigation, O. rochetiana showed significant antidiarrheal activity with no symptoms of toxicity in mice.

Phytochemical characterization, anti-diarrhoeal, analgesic, anti-inflammatory activities and toxicity profile of Ananas comosus (L.) Merr (pineapple) leaf in albino rats

Ethnopharmacological relevanceAnanas comosus (pineapple) leaf is used in ethnomedicine to treat diarrhoea, inflammation, pain, bacterial infections and oedema. Aim of the studyThe aim of this study was to investigate the anti-diarrhoeal, anti-inflammatory and analgesic effects as well as the toxicity profile of the aqueous Ananas comosus leaf extract (AACLE) in rats. MethodsMethanol ACLE was subjected to gas chromatography-mass spectrometry (GC-MS) analysis. In the acute toxicity study, a single oral dose of up to 5000 mg/kg AACLE was administered. In the subacute toxicity study (28 days), rats in groups 2–4 received AACLE orally. The anti-diarrhoeal effect was studied using charcoal meal and castor oil-induced diarrhoea. Anti-inflammatory and analgesic tests were measured using egg albumin-induced paw oedema and acetic acid-induced writhing methods, respectively. For the subacute toxicity, anti-diarrhoeal, analgesic, and anti-inflammatory studies, AACLE was administered orally to rats at doses of 200, 400, and 600 mg/kg body weight. ResultsHexadecanoic acid methyl ester, 2-methoxy-4-vinylphenol, n-hexadecanoic acid and n-heptadecanol-1 were identified among other compounds with known pharmacological activities by GC-MS analysis. No deaths, behavioural changes, or signs of toxicity were observed in the acute toxicity study. Treatment with AACLE (28 days) decreased aspartate aminotransferase, alanine transaminase, total cholesterol, triglycerides, and low-density lipoprotein cholesterol, while high-density lipoprotein cholesterol, glutathione, and catalase increased when compared with control (P < 0.05). Treatment with AACLE did not cause significant changes in haematological or renal function parameters. Treatment with AACLE inhibited gastrointestinal motility and castor oil-induced diarrhoea in rats. Treatment with AACLE resulted in a dose-dependent (200–600 mg/kg) significant (P < 0.05) anti-diarrhoeal, analgesic, and anti-inflammatory effect compared to standard drugs. ConclusionOur study revealed that ACLE is not toxic but contains bioactive compounds with anti-diarrhoeal, anti-inflammatory, antimicrobial, and hepatoprotective activity. AACLE has antidiarrhoeal, analgesic and anti-inflammatory activity in rats, which justifies its therapeutic use in traditional medicine.

Assessment of phytochemicals, antioxidant properties, and in vivo antidiarrheal activity of date palm (Phoenix dactylifera L.)

ABSTRACT Date palm (Phoenix dactylifera L.) has a significant role in our daily life due to its diverse nutritional composition and potential health benefits. This study was designed to evaluate the phytochemicals, antioxidant, and antidiarrheal potential of various extracts of Ajwa whole fruit, date palm pit, and flesh. The extracts with the highest phytochemical quantities were further subjected to bio-assay assessment against castor oil-induced diarrhea using different animal models. The results indicated that Ajwa whole fruit extract (AWFE) exhibited higher amount of total phenolic contents (TPC: 36 ± 16 mg/g GAE), total flavonoid contents (TFC: 360 ± 135 mg/g RE), and 2, 2-diphenyl-1-picrylhydrazyl (DPPH: 60 ± 7%) in hydro-ethanolic extracts. In vivo results revealed that Ajwa whole fruit 60% hydro-ethanolic extract at high dose (2000 mg/kg) showed significantly (p < .05) highest protective effect against diarrheal changes in mice. In case of AWFE, the intestinal contents % inhibition was slightly higher (72%) as compared to that of loperamide control (70%). High dose of Ajwa whole (2000 mg/kg) demonstrated less effectiveness (66 ± 11%) in comparison with loperamide (78 ± 8%) regarding % inhibition of fluid accumulation in enteropooling studies. High dose (2000 mg/kg) of Ajwa also reduced intestinal transit time by decreasing the % distance (53 ± 1%) in comparison with loperamide (57 ± 1%). The % inhibition of charcoal meal traveling of AWFE (38 ± 2%) was also significantly higher as compared to loperamide (26 ± 1%). The findings of the current study reveal that AWFE might be consumed as an ingredient in daily food products to counter effect the symptoms of 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.