Inhibited Castor Oil-induced Diarrhea Research Articles

EVALUATION OF ANTIDIARRHEAL ACTIVITY OF ETHANOLIC LEAF EXTRACT OF ERIOBOTRYA JAPONICA LINDL

Objective: The study was carried out to investigate the antidiarrheal activity of ethanolic leaf extract of Eriobotrya japonica (EEJ) using various models of experimental diarrhea.Methods: Antidiarrheal property of EEJ at 100, 200, and 400 mg/kg/bwt was evaluated using castor oil-induced diarrhea, castor oil-induced enteropooling, and gastrointestinal propulsive models of experimental diarrhea in Sprague Dawley rats of both sexes, weighing 200–250 g. Cytotoxicity test of EEJ was performed using brine shrimp bioassay.Results: Toxicity assay of EEJ showed a lethal concentration value of 1225 μg/ml suggesting non-toxicity. EEJ significantly (p<0.05) and dose-dependently (100, 200 and 400 mg/kg/bwt) inhibited castor oil-induced diarrhea by 38.1%, 76.19%, and 100%, respectively, and enteropooling by 28%, 56%, and 88%, respectively, compared with control. Pre-treatment with yohimbine, α2-adrenoceptor blocker significantly reversed the protective effect of EEJ (400 mg/kg) against castor oil-induced diarrhea and against castor oil-induced enteropooling, suggesting the involvement of α2-adrenoceptors in antidiarrheal property of EEJ. Furthermore, EEJ significantly (p<0.05) and dosedependently (100, 200, and 400 mg/Kg/bwt) inhibited gastrointestinal motility by 28%, 62%, and 83.92%, respectively.Conclusion: The study has demonstrated the antidiarrheal potential of ethanolic leaf extract of EEJ, which may be attributable to its dual antisecretory and antimotility activities probably through activation of the sympathetic α2-adrenergic pathway.

Studies to determine antidiarrhoeal and spasmolytic activities of extract of Aegle marmelos. L fruit

Objective: To investigate and determine the antidiarrhoeal and spasmolytic potential of fruit of Aegle marmelos is due to CCBs compounds and not tannic acid.Materials and methods: The extract of ripe and dry fruit of A. marmelos (Am.Cr) was prepared in methanol: water (70:30). The antidiarrhoeal activities of the extract, loperamide and tannic acid were studied in vivo; in castor oil induced diarrhoeal model in mice whereas spasmolytic effect was studied in vitro; in isolated mice ileum. Calcium channel blocking (CCB) activity was investigated after preincubation of mice ileum by Am. Cr or loperamide and subsequent adding of K+80 mM.Results: Am. Cr inhibited castor oil-induced diarrhoea: onset of diarrhoea, total no. of faeces, and total no. of wet faeces dose-dependently, the dose of 800 mg/mL was found statistically significant, total weight of feces and total weight of wet faeces were also inhibited. Concentration-dependent inhibition of spontaneous contraction and contractile effect of K+80 mM after pre-incubation by Am. Cr were confirmed in isolated mice ileum. The results of Am. Cr are comparable with Loperamide. Tannic acid produced neither antidiarrhoeal effect nor exhibited CCB activity, however relaxant effect was observed in isolated mice ileum.Conclusion: The antidiarrhoeal and spasmolytic effects of Am.Cr may be mediated through compounds which posses CCB effect. Tannic acid exhibited relaxant effect only which is not sufficient evidence scientifically to classify as antidiarrhoeal.Bangladesh Journal of Medical Science Vol.17(2) 2018 p.205-211

The efficacy of a sulphated polysaccharide fraction from Hypnea musciformis against diarrhea in rodents

Seaweeds are sources of diverse bioactive compounds, such as sulphated polysaccharides. This study was designed to evaluate the chemical composition and anti-diarrheal activity of a fraction of sulphated polysaccharide (PLS) obtained from the red seaweed Hypnea musciformis in different animal models, and to elucidate the underlying mechanisms. PLS was obtained by aqueous extraction, with a yield of 31.8% of the seaweed dry weight. The total carbohydrate content accounted for 99% of the sample. The sulfate content of the polysaccharide was 5.08% and the percentage of carbon was 25.98%. Pretreatment with all doses of PLS inhibited castor oil-induced diarrhea, with reduction of the total amount of stool, diarrheal stools, and the severity of diarrhea. PLS (90mg/Kg) decreased castor oil- and PGE2-induced enteropooling. In addition, PLS (90mg/Kg) increased the Na+/K+-ATPase activity in the small intestine and reduced gastrointestinal transit, possibly via activation of cholinergic receptors. Interestingly, the cholera toxin-induced fluid secretion and Cl− ion levels decreased in the intestinal contents of the animals pretreated with PLS (90mg/kg), probably via reduction of toxin—GM1 receptor binding. In conclusion, PLS exerts anti-diarrheal activity by increasing Na+/K+-ATPase activity, inhibiting gastrointestinal motility, and blocking the toxin—GM1 receptor binding.

AN ASSESSMENT ON THE PROTECTION OF GYMNEMA SYLVESTRE EXTRACTS AGAINST CASTOR OIL – INDUCED DIARRHOEA IN RATTUS NOVERGICUS

Diarrhoea is one of the main causes of death worldwide in children and adult alike. In view of this problem, the World Health Organization has encouraged studies for treatment and prevention of diarrhoea diseases depending on traditional medicinal practices. Anti-diarrhoeal effect of crude aqueous extracts of the stem, leaf and flower of Gymnema sylvestre was assessed in castor oil-induced diarrhoea at doses of 700, 1500 and 2000 mg/kg b.w, using Rattus novergicus. At these doses the extracts inhibited castor oil-induced diarrhoea in dose dependent fashion. There was significant (p<0.05) reduction in defecation severity when compared with the reference drug and control. The flower extract is more potent followed by the stem and the leaf. The result obtained in this study indicates that the aqueous extracts of Gymnema sylvestre may contain varied pharmacologically active ingredients with potent anti-diarrhoeal activity.

Species Differences in the Antidiarrheal and Antispasmodic Activities of Lepidium sativum and Insight into Underlying Mechanisms

The aim of this study was to see if the crude extract of Lepidium sativum (Ls.Cr) exhibits species specificity in its antidiarrheal and antispasmodic activities along with insight into the underlying mechanisms using the in-vivo and in-vitro experiments. Ls.Cr inhibited castor oil-induced diarrhea in mice at doses (300 and 1000 mg/kg) three times higher dose than for rats. In isolated rat ileum and jejunum, Ls.Cr completely inhibited carbachol (CCh), low K⁺ (25 mM) and high K⁺ (80 mM)-induced contractions, while in guinea-pig tissues, Ls.Cr caused complete inhibition of only CCh-induced contraction. In rabbit tissues, Ls.Cr completely inhibited CCh and low K⁺-induced contractions sensitive to K⁺ channel antagonists. Pretreatment of guinea-pig and rat tissues with Ls.Cr caused a rightward shift in CCh-induced contractions in a pattern similar to dicyclomine, while in rabbit and rat tissues, Ls.Cr shifted isoprenaline curves to the left similar to papaverine. These data indicate that the antidiarrheal and antispasmodic activities of L. sativum are species dependent, mediating its antispasmodic effect through combinations of multiple pathways including activation of K⁺ channels, and inhibition of muscarinic receptors, Ca⁺⁺ channels and PDE enzyme. Rat tissues showed the highest potency. Based on the results, we recommend using multiple species to know the real pharmacological profile of medicinal products.

Studies on Antidiarrheal and Antispasmodic Activities of Lepidium sativum Crude Extract in Rats

This study was aimed to provide the pharmacological basis for the medicinal use of Lepidium sativum in diarrhea using in vivo and in vitro assays. The seed extract of Lepidium sativum (Ls.Cr) at 100 and 300 mg/kg inhibited castor oil-induced diarrhea in rats. In isolated rat ileum, Ls.Cr (0.01-5 mg/mL) reversed carbachol (CCh, 1 µM) and K(+) (80 mM)-induced contractions with higher potency against CCh, similar to dicyclomine. Preincubation of rat ileum with a lower concentration of Ls.Cr (0.03 mg/mL) caused a rightward parallel shift in the concentration-response curves (CRCs) of CCh without suppression of the maximum response, while at the next higher concentration (0.1 mg/mL), it produced a non-parallel rightward shift with suppression of the maximum response, similar to that of dicyclomine. Ls.Cr shifted the CRCs of Ca(++) to the right with suppression of the maximum response, similar to verapamil. These data suggest that Lepidium sativum seed extract possesses antidiarrheal and spasmolytic activities mediated possibly through dual blockade of muscarinic receptors and Ca(++) channels, though additional mechanism(s) cannot be ruled out and this study explains its medicinal use in diarrhea and abdominal cramps.

Antidiarrheal and antispasmodic activities of Salvia officinalis are mediated through activation of K+ channels

This study was conducted to provide pharmacological basis for the medicinal use of Salvia officinalis in diarrhea. The crude extract of S. officinalis was studied using the in vivo and in vitro assays. The crude extract inhibited castor oil-induced diarrhea in mice at the dose of 100 and 300 mg/kg. In isolated rabbit jejunum, it caused a dose-dependent (0.1-3 mg/mL) relaxation of spontaneous as well as low K+ (25 mM) and high K+ (80 mM)-induced contractions, being distinctly more potent on low K+. Pretreatment of tissue with 4-aminopyridine (1 mM) almost completely blocked the inhibitory effect of crude extract on low K+. These results indicate that the crude extract of S. officinalis possesses antidiarrheal and antispasmodic activities mediated possibly through the dominant activation of voltage-dependent K+ channels and this study provides sound pharmacological basis for its medicinal use in diarrhea and gut spasm.

Antidiarrhoeal effects of ethanolic leaf extract ofErythrina indicaL. in experimental animals

The ethanolic extract of the leaves of Erythrina indica significantly modified normal defecation frequency as well as inhibited castor oil-induced diarrhoea in Wistar rats. In addition, the extract showed a significant reduction in gastrointestinal motility in charcoal meal test. Phytochemical tests revealed that the main constituents were alkaloids. These findings suggested that the ethanolic extract of leaves of Erythrina indica elicits potent antidiarrhoeal effects and thus substantiated its traditional claim as an antidiarrhoeal agent.

Anti-diarrhoeal activity of the methanolic leaf extract of Phyllanthus muellerianus

The methanolic leaf extract of Phyllanthus muellerianus was investigated for anti-diarrhoeal activity. The anti-diarrhoeal activities were investigated using the castor oil-induced diarrhoea, magnesium sulphateinduced diarrhoea, small intestinal and distal colonic propulsion, isolated rabbit jejunum and castor oil-induced intestinal fluid accumulation. The results revealed that the methanolic leaf extract of Phyllanthus muellerianus significantly (p < 0.05) and dose-dependently inhibited castor oil-induced diarrhoea, magnesium sulphateinduced diarrhoea, and also inhibited small intestinal propulsion and distal colonic propulsion. The extract inhibited the spontaneous movement of the isolated rabbit jejunum and reduced castor oil-induced intestinal fluid accumulation. The intraperitoneal LD50 of the extract in mice was found to be 547.7 mg/kg and preliminary phytochemical screening revealed the presence of tannins, carbohydrates, free anthraquinones and flavonoids. The results of this study indicate the presence of biologically active substance(s) which may be beneficial in the management of diarrhoea.© 2009 International Formulae Group. All rights reserved.Key words: Phyllanthus muellerianus, Euphobiaceae, Herbal medicine, Anti-diarrhoea.

English

The leaf base of&nbsp;Sorghum bicolor&nbsp;(Family: Gramineae, Poaceae) was cold-macerated with 70% v/v methanol. The aqueous methanolic extract was further fractionated into non-polar, medium polar and very polar components using hexane, ethylacetate and water (aqueous), respectively. The gastrointestinal effects of these extracts were tested on intestinal motility (transit) in mice, castor oil-induced diarrhoeal model in rats, isolated rabbit jejunum, guinea pig ileum and rat stomach fundus strip. The oral and intraperitoneal LD50&nbsp;values for the extracts were determined in mice and rats. The aqueous methanolic extract (100 &ndash; 400 mg/kg i.p) significantly (P &lt; 0.05) and dose-dependently decreased the intestinal motility, inhibited castor oil-induced diarrhoea, produced concentration-dependent relaxation of rabbit jejunum with half maximal effective concentration (EC50) of 0.21 mg/ml. This extract also produced both non-myogenic and slight relaxation effects on guinea pig ileum and a contraction on rat stomach fundus strips. Both aqueous and ethylacetate fractions also reduced intestinal motility. However, ethylacetate fraction caused greater reduction than the aqueous fraction. The oral LD50&nbsp;value for the aqueous methanolic extact in both rats and mice was found to be &ge; 2000 mg/kg while the intraperitoneal values are 1414.2 mg/kg in rats and 1341.6 mg/kg in mice. The intrapertoneal value for both aqueous and ethylacetate fractions is &ge; 2000 mg/kg in mice. The study provided scientific bases for the traditional use of&nbsp;S. bicolor&nbsp;for treatment of gastrointestinal related problems such as diarrhoea. &nbsp; Key words:&nbsp;Sorghum bicolor, gastrointestinal, motility, diarrhoea, jejunum, ileum, fundus.

Evaluation of anti-diarrhoeal properties of methanolic Root extract of &lt;i&gt;Piliostigma reticulatum&lt;/i&gt; in rats

Piliostigma reticulatum (DC) Hoechst (Leguminosae) is an evergreen shrub reputed to possess a number of medicinal properties. The methanolic extract of Piliostigma reticulatum root (Leguminosae) was evaluated for anti-diarrhoeal activity in rats using castor oilinduced diarrhoea and fluid accumulation and activated charcoal test models. Phytochemical screening revealed the presence of tannins, glycosides, saponins, sterols, alkaloid and balsam. The extract (at doses of 100 and 200 mg/kg) and atropine (3 mg/kg) significantly inhibited castor oil-induced diarrhoea (53.5 72.1%) and fluid accumulation (35.17 71.03%) and small intestinal transit (9.38 21.74%) in the rats. The results obtained in this study revealed that the extract has remarkable anti-diarrhoeal effect, which may be due to the presence of the tannins, alkaloids and saponins constituents and can thus be used in the treatment of non-specific diarrhoea. Keywords:Piliostigma reticulatum, Anti-diarrhoeal activity, Rat, Gastrointestinal tract.JOPAT Vol. 12 2007: pp. 44-50

Evaluation of antipsychotic and anti-diarrhoeal activities of ethanolic extract of roots of Rubia cordifolia Linn

The objective of the present study was to assess the antipsychotic and antidiarrhoeal activities of ethanolic extract of roots of Rubia cordifolia in mice and rats. The antipsychotic activity of ethanolic extract of roots of Rubia cordifolia (ERC) was evaluated by observing its effect on amphetamineinduced stereotyped behavior in mice. Effect of ERC was also studied on motor coordination and locomotion in mice. The antidiarrhoeal activity was evaluated using castor oil-induced diarrhoea and excretion of sodium and potassium ions in the intestinal secretion in rats and gastrointestinal transit in mice. The ERC inhibited amphetamine-induced stereotyped behaviour, diminished locomotion and impaired motor coordination. ERC inhibited castor oil-induced diarrhoea, decreased both sodium and potassium excretion in the intestine and decreased gastrointestinal transit. Thus the present study confirms the anti-diarrhoeal activity of Rubia cordifolia. Further studies are necessary to evaluate the potential of Rubia cordifolia as an antipsychotic.

Antidiarrheal activity of dehydroleucodine isolated from Artemisia douglasiana

Dehydroleucodine (DhL), a sesquiterpene lactone obtained from Artemisia douglasiana, was screened for antidiarrheal effects. DhL inhibited castor oil-induced diarrhea in mice by judged by a decrease in the number of wet faeces in the DhL-treatment groups. DhL significantly reduced intestinal transit in mice. Yohimbine and phentolamine counteracted the inhibitory effect of DhL. It is suggested that α 2-adrenergic receptors mediate the effect of DhL in intestinal motility. DhL reduced also intraluminal accumulation of fluid. Thus, the antidiarrheal activity of DhL is possibly related, at least in part, to its inhibitory action against gastrointestinal motility and the inhibition of enteropooling property.

Pharmacological studies of anti-diarrhoeal activity of Gentianopsis paludosa

The pharmacological studies of anti-diarrhoeal activity of Gentianopsis paludosa were carried out. The 75% ethanol extract (100–400 mg/kg) of Gentianopsis paludosa inhibited castor oil-induced diarrhoea and also reduced gastrointestinal motility in the charcoal meal test in mice. In the rabbit-isolated ileum, the extract showed inhibitory effects not only on its spontaneous contraction, but also on acetylcholine (Ach, 0.1 mM)- and KCl (60 mM)-induced contractions. Furthermore, the ethanol extract (0.4–0.6 mg/ml) shifted the CaCl 2 dose–effect curves to the right in a non-competitive manner and significantly reduced the acetylcholine-induced contraction of isolated ileum in Ca 2+-free solution like verapamil (0.1 mM), which suggest that the extract interferes with Ca 2+ movement. These results support the traditional use of Gentianopsis paludosa in the treatment of diarrhoea.

Study of the Gastrointestinal Properties of Acalypha aff. mollis

ABSTRACT The antidiarrheal activity of hexane, chloroform, methanol and aqueous extracts of Acalypha aff. mollis was evaluated in mice with diarrhea induced by castor oil and MgSO4. Both the aqueous and methanol extracts of the plant significantly inhibited castor oil-induced diarrhea (maximum inhibition was 54.35 and 30.57 percent, respectively), but failed to inhibit MgSO4-induced diarrhea. The aqueous extract also inhibited small intestine transit in both untreated and castor oil-treated rats. This antidiarrheal activity was not associated with an antimicrobial effect. Instead, tannins detected in phytochemical screening could probably contribute to the antidiarrheal action. Acalypha aff. mollis extracts did not modify normal defecation patterns.

Anti-diarrheal and spasmolytic activities and acute toxicity study of Soonkijangquebo, a herbal anti-diarrheal formula

The anti-diarrheal and spasmolytic activities of Soonkijangquebo™ (SKJQB), a Korean herbal anti-diarrheal formulation, were subjected to pharmacological evaluation. SKJQB, at a dose of 50–200 mg/kg, inhibited castor oil-induced diarrhea in mice. The median effective dose (ED 50) for the anti-diarrheal effect was 93 mg/kg. In isolated rabbit jejunum preparations, SKJQB produced a spasmolytic effect by the relaxation of spontaneous contractions in a dose-dependent manner. The median effective concentration (EC 50) for the spasmolytic effect was 3.6 mg/ml. In isolated guinea pig ileum preparations, SKJQB also produced a spasmolytic effect by reduction of acetylcholine-induced contractions. When tested against calcium channel blockade in rabbit jejunum, SKJQB caused a dose-dependent rightward shift in the Ca 2+ dose–response curves, similar to that produced by verapamil, a well-known calcium antagonist. In an acute toxicity study in Sprague–Dawley rats, the median lethal dose (LD 50) of SKJQB was greater than 2000 mg/kg, and no pathological changes were noticed in macroscopic examination by necropsy of rats treated with SKJQB. Thus, SKJQB may be safely used as a spasmolytic as well as an anti-diarrheal agent.

Antidiarrhoeal effects of Ocimum gratissimum leaf extract in experimental animals

The aqueous extract of the leaves of Ocimum gratissimum was screened for antidiarrhoeal effects. The extract inhibited castor oil-induced diarrhoea in rats as judged by a decrease in the number of wet faeces in the extract-treated rats. In addition, the extract inhibited the propulsive movement of intestinal contents. On the isolated ileum of guinea-pig, the extract showed no direct action; however, it reduced the responses of the guinea-pig ileum to acetylcholine, nicotine and histamine. Phytochemical tests revealed the main constituents as tannins, steroids, triterpenoid and carbohydrates. These findings suggested that the aqueous extract of the leaves of O. gratissimum might elicit an antidiarrhoeal effect by inhibiting intestinal motility, partly via muscarinic receptor inhibition.

Relationship between the antidiarrhoeal effects of Hange-Shashin-To and its active components.

This study was designed to examine the relationship between the antidiarrhoeal effects of Hange-Shashin-To (TJ-14) and its active components. Oral treatment with TJ-14 at 1000 mg/kg significantly inhibited castor oil-induced diarrhoea. Both the 50% methanol eluate fraction (fraction III) and the methanol eluate fraction (fraction IV) showed antidiarrhoeal effects at oral doses of 68 mg/kg and 63 mg/kg, respectively, corresponding to 1000 mg/kg of TJ-14. TJ-14 (1000 mg/kg, p.o.) showed a significant increase in blood corticosterone levels. Increased blood corticosterone was noted after the oral administration of 63 mg/kg of fraction IV. The inhibitory activity of TJ-14 on cyclooxygenase-2 (COX-2) was also observed in fractions III and IV. The main component of fraction III was Scutellariae Radix-derived baicalin. Fraction IV contained Glycyrrhizae Radix-derived glycyrrhizin and isoliquiritin, Coptidis Rhizoma-derived berberine, coptisine and palmitine. Ginseng Radix-derived saponins were also present in fraction IV. These compounds inhibited castor-oil induced diarrhoea at oral doses of 10 or 30 mg/kg. Thus, the present results indicate that Scutellariae Radix, Glycyrrhizae Radix, Ginseng radix and Coptidis Rhizoma-derived components are involved in the antidiarrhoeal action of TJ-14.