Antidiarrheal effect of fractions from stem bark of Thespesia populnea in rodents: Possible antimotility and antisecretory mechanisms

ObjectiveTo evaluate antidiarrheal activity of the fractions of aqueous extract from stem barks of Thespesia populnea (Malvaceae).MethodsFrom the aqueous extract three fractions namely ethyl acetate fraction (EAF), methanolic fraction (MF) and residue fraction (RF) were made and studied for antidiarrheal activity. Antidiarrheal activity of the fractions were evaluated in castor oil induced diarrhea, prostaglandin E₂ (PG-E₂) induced diarrhea and charcoal meal test as in vivo models and the most potent fraction was further evaluated with in vitro models to determine the possible antimotility effect.ResultsIn castor oil induced diarrhea model, the RF (10, 25, 50 and 100 mg/kg, po.) and MF (100 mg/kg, po.) has significantly reduced the cumulative wet faecal mass, where as the EAF have not shown any significant antidiarrheal activity, RF was found to be more potent than MF. Based on these results and percentage yield, only RF was evaluated in PG-E₂ induced enteropooling and charcoal meal test. RF (10, 25 and 50 mg/kg) had shown significant inhibition of PG-E₂ induced secretions (antisecretory) and decreased the movement of charcoal in charcoal meal test indicating its antimotility activity. Furthermore, RF has showed significant inhibition of acetylcholine, histamine and BaCl₂ induced contractions on rat colon, guinea pig ileum and rabbit jejunum with EC₅₀ values of 241.7, 303.1 and 286.1 μg/mL, respectively indicating the antimotility effect of RF. The phytochemical analysis of RF showed presence of gums and mucilages and the possible mechanism may be the combination inhibition of elevated prostaglandin biosynthesis and reduced propulsive movement of the intestine.ConclusionsRF possesses good antidiarrheal activity comparing with other two fractions and the possible mechanism thought to be associated with combination of antisecretory and antimolity.     

Pharmacological properties and related constituents of stem bark of Pterocarpus erinaceus Poir. (Fabaceae)

ObjectiveTo screen methanol and dichloromethane extracts of stem bark of Pterocarpus erinaceus for anti-inflammatory, analgesic, in vitro antioxidant activities and phytochemical analysis.MethodsAnti-inflammatory activity was determined by using carrageenan induced-edema of mice paw and croton oil-induced edema of mice ear; analgesic effect was evaluated using acetic acid-induced writhing. Phytochemical screening of extracts was performed by thin layer chromatography. The chromatographic fractionation led to the isolation of main active components as friedelin, lupeol and epicathechin. The structures were established by TLC and nuclear magnetic resonance studies.ResultsBoth methanol and dichloromethane extracts, friedelin, lupeol and epicatechin showed a significant anti-inflammatory effect using croton oil induced-ear edema. Furthermore, the action of dichloromethane extract was more important. At the doses of 100 and 200 mg/kg, the methanol extract was able to reduce the carrageenan induced-hind paw edema, while at the doses of 100, 200 and 400 mg/kg, it showed an important analgesic effect against writhing induced by acetic acid injection of 38.8%, 68.0% and 74.3%, respectively. Antioxidative properties of methanol extract and its dichloromethane and ethyl acetate fractions were assessed by using the 1,1-diphenyl-2-picrylhydrazyl method. The methanol extract showed the stronger radical scavenging activity than dichloromethane and ethyl acetate fractions, with an antiradical power of 5, 3.5 and 2 respectively. The main components isolated from these extracts as friedelin, lupeol and epicathechin were responsible of these activities.ConclusionsThe results suggest that the stem bark extracts of Pterocarpus erinaceus possessed important anti-inflammatory, analgesic activities and strong antioxidant properties, therefore, they could be used as natural potential ingredients for pharma ceutical industry.     

A pharmacological evaluation of antidiarrhoeal activity of leaves extract of Murraya koenigii in experimentally induced diarrhoea in rats

ObjectiveTo evaluate anti-diarrhoeal activity of aqueous and alcoholic extract of the leaves of Murraya koenigii (M. koenigii)by using models of castor oil induced diarrhoea, charcoal meal test and PGE₂ induced diarrhoea.MethodsAlcoholic extract (400 mg/kg) and aqueous extract (200 mg/kg) of leaves of Murraya koenigii were used with loperamide as standard. Albino Wistar rats of both sexes weighing between 150–250 g were used for the anti-diarrhoeal activity.ResultsThe result suggested that it could act centrally and inhibit the PGE₂ to give anti-diarrhoeal effects. Result of charcoal meal test also suggested its anti-muscarnic activity.ConclusionsThese findings indicate that aqueous extract of the leaves of M. koenigii displays good anti-diarrhoeal activity, corroborating the folk use of M. koenigii preparations and contributing for its pharmacological validation.     

Homopterocarpin contributes to the restoration of gastric homeostasis by Pterocarpus erinaceus following indomethacin intoxication in rats

ObjectiveTo investigate the restorative effect of Pterocarpus erinaceus (P. erinaceus) and homopterocarpin, an isoflavonoid isolated from it, on indomethacin-induced disruption in gastric homeostasis in rats.MethodsAdult rats were divided into five groups and fasted for 48 h before treatment. Group 1 received olive oil (vehicle), group 2 received 25 mg/kg indomethacin while groups 3–5 received cimetidine (100 mg/kg), homopterocarpin (25 mg/kg) and P. erinaceus ethanolic stem bark extract (100 mg/kg) respectively. After 1 h, all the groups except group 2 were administered 25 mg/kg of indomethacin. One hour later, the rats were sacrificed and the ulcer index and other gastroprotective indices were evaluated.ResultsIndomethacin caused significant injury to the stomach of the rats as reflected in the ulcer indices (9.0±1.4) as compared with that of control (2.0±0.0). Equally, there were significant increases in gastric acid concentration and malondialdehyde level in the stomachs of the ulcerated animals compared with the control. However mucus content, reduced gluthatione level and gastric pH were significantly reduced in the ulcerated animals compared with the control. Pretreatment with either Pterocarpus bark extract or homopterocarpin reversed the effects of indomethacin on the evaluated parameters.ConclusionsThese results indicate that both homopterocarpin and Pterocarpus extract offered gastroprotection against indomethacin-induced ulcer by antioxidative mechanism and the modulation of gastric homeostasis. The results also suggest that homopterocarpin might be responsible for, or contribute to the antiulcerogenic property of P. erinaceus.     

Analgesic activity of Cryptostegia grandiflora (Roxb.) R.br. leaves methanol extract using mice

ObjectiveTo evaluate analgesic property of leaf methanol extract of Cryptostegia grandiflora (Roxb.) R.Br. using mice.MethodsAnalgesic activity was evaluated by abdominal writhing and tail flick methods using Swiss albino mice. Acetyl salicylic acid was used as standard drug.ResultThe leaf methanol extract did not show any signs of toxicity upto 5000 mg/kg b.w. The leaf methanol extract (LME) was tested at three different dosages viz., 250, 500 and 750 mg/kg b.w. orally. All the three doses of LME showed significant (P < 0.001) analgesic activity, among them dose at 750 mg/kg b.w. showed 62.93% inhibition, but less effective than standard acetyl salicylic acid (93.70%) as revealed by writhing test. In Tail-flick model, the LME at the dose of 500 mg/kg b.w. showed significant activity (P < 0.001) when compared to the other two doses as evidence by the increase in the latency of tail response to thermal stimulation.ConclusionsThis investigation revealed that the C. grandiflora LME demonstrated significant analgesic effect in both abdominal writhing and tail flick models. Among the three different doses tested, the 500 mg/kg b.w. was found to be more potent. The results of this investigation revealed that the LME of C. grandiflora possesses significant analgesic property and supported the traditional medicinal claims on C. grandiflora.     

The antidiarrheal action of bismuth subsalicylate in the mouse and the rat

The antidiarrheal effectiveness of bismuth subsalicylate was determined in two species of laboratory animals. Doses of castor oil were, at first, found to accelerate significantly the movement of a charcoal test meal along the small intestine of the mouse and rat and also to increase both the fecal output (dry or wet weight) and the frequency of diarrhea in mice. Bismuth subsalicylate significantly prevented the enhancement of charcoal-meal transport induced by castor oil in both mice and rats. Increased fecal output (dry or wet weight) and increased frequency of diarrhea in mice were also significantly reduced by bismuth subsalicylate in a dose-related fashion. The findings in these experiments lead to the definitive conclusion that bismuth subsalicylate exerts antidiarrheal activity in the mouse and in the rat and support its use in therapy of common clinical diarrheal states.     

Evaluation of the antimalarial potential of Icacina senegalensis Juss (Icacinaceae)

ObjectiveTo evaluate in vivo antimalarial activity of methanol leaf extract of Icacina senegalensis.MethodsThe extract was investigated for activity against early and established malaria infections using Swiss albino mice infected with Plasmodium berghei at dose levels of 25, 50 and 100 mg/kg. Chloroquine (10 mg/kg) was used as positive control.ResultsA dose dependent chemo-suppression of the parasites was observed at different dose levels of the extract tested with a considerable mean survival time.ConclusionsThe results support further investigation on components of traditional medicines as potential new antimalarial agents.     

Antitrypanosomal potentials of the extract and fractions of Abrus precatorius seeds

ObjectiveTo evaluate the in vivo trypanocidal activity of the methanol extract and fractions of Abrus precatorius seeds in mice.MethodsParasiteamia was induced unto mice by intraperitoneal injection of 1.25×10⁵ Trypanosoma in normal saline. Five days when a high level of parasiteamia was established treatment commenced until ten days. The mice were treated with 10, 20 and 40 mg/kg bt. of the extract and 5 and 10 mg/kg bt. of the fraction (F₂), respectively for 5 days. Diminazene aceturate at the dose of 3.5 mg/kg bt. for two days was used as the reference drug. The level of parasitaemia and packed cell volume (PCV) of the animals estimated.ResultsAt doses of 10, 20 and 40 mg/kg the crude extract showed a sharp reduction in the level of parasitaemia in mice compared with the untreated group. The mice treated with F₂ at doses of 5 and 10 mg/kg showed a sharp reduction in the level of parasitamia to zero in day 9, and a gradual recovery from the 12th day of treatment. This effect is comparable to that of the mice treated with 7 mg/kg of standard drug diminazene aceturate. The PCV of the treated showed a gradual decrease with time, but not as much as the untreated group. Phytochemical screening revealed the presence of glycosides, alkaloids, carbohydrates, tannins and proteins in the Abrus precatorius powder while F₂ was rich in alkaloids.ConclusionsThis study shows that both the extract and the fractions of Abrus precatorius seeds exhibited a promising trypanocidal property. Alkaloids may be responsible for the observed activity.     

Antimotility effects of extracts and fractions of Eastern Nigeria mistletoe (Loranthus micranthus Linn)

ObjectiveTo evaluate the antimotility activity of Eastern Nigerian mistletoe[Loranthus micranthus (L. micranthus) Linn] parasitic on six different host trees viz. Baphia nitida, Persia americana, Kola accuminata, Irvingia gabonensis, Citrus simensis and Pentacletra macrophylla (P. mycrophylla).MethodsThe antimotility of the methanol extracts and solvent fractions were evaluated in castor oil induced diarrheoa in rats.ResultsThe methanol extracts (200 mg/kg, i.p.) inhibited defeacation significantly (P < 0.05) 4 h after administration (75.73% to 93.33%) more than that of atropine sulphate (2 mg/kg, i.p.) which inhibited defeacation by 80.0%. The methanol extract (200 mg/kg, i.p.) of L. micranthus parasitic on P. mycrophylla exhibited significant (P<0.05) inhibition in gastrointestinal transit (67.6%) more than that of atropine sulphate (2 mg/kg, i.p.) which inhibited gastrointestinal transit by 26.4%. The solvent fractions of L. micranthus parasitic on P. mycrophylla at dose levels of 150 mg/kg inhibited significantly the gastrointestinal transit of mice. Fraction F₅ exhibited inhibitory activity which was comparable to loperamide (73.3%).ConclusionThe methanol extract of L. micranthus parasitic on P. macrophylla exhibits higher antimotility activity that other extracts. The solvent fractions could serve as source of novel antimotility agents.     

Investigation of in vivo antioxidant activity of Euphorbia helioscopia latex and leaves methanol extract: a target against oxidative stress induced toxicity

ObjectiveTo evaluate in vivo antioxidant activity of latex and leaves methanol extract of Euphorbia helioscopia using mice as experimental animals.MethodsThe plant was collected, identified, dried under shade, ground to fine powder and extraction was done. Latex was collected in dried bottles by cutting the stem. Oxidative stress was induced in mice with acute toxic dose of paracetamol administered intrperitoneally. Latex and leaves methanol extract (600 and 1 200 mg/kg) orally, once a day, were given to mice for two weeks. Then oxidative stress biomarkers were measured in tissue homogenates and serum.ResultsLeaves methanol extract exhibited prominent in vivo antioxidant effect as compared to latex. Results showed significant rise in antioxidant enzymes (catalase, superoxide dismutase and glutathione) levels at 1 200 mg/kg dose of extract. Thus, extract helped to detoxify the free radicles by increasing antioxidant enzymes levels. Malondialdehyde value decreased significantly with extract (1 200 mg/kg) which was indicator of extract's power to inhibit the generation of free radicals. Extract (1 200 mg/kg) exhibited maximum cure against stress induced changes in liver, kidney, lipid profile parameters and complete blood count.ConclusionsLeaves methanol extract of Euphorbia helioscopia raised antioxidant enzymes levels in mice. It showed hepatorenal-curative effect, hypolipidemic effect and hemostasis potential. Thus, it can help the biological systems to fight against stress induced pathological conditions.     

Antimalarial potency of the leaf extract of Aspilia africana (Pers.) C.D. Adams

ObjectiveTo investigate the antimalarial activity of ethanol extract of Aspilia africana (A. africana) leaf.MethodsThe ethanol extract of A. africana leaf (100–400 mg/kg) was screened for blood schizonticidal effect against chloroquine-sensitive Plasmodium berghei (P. berghei) in mice both in early and established models of antimalarial studies.ResultsThe leaf extract exhibited significant (P<0.05) antiplasmodial activity in 4-day early infection and in established infection tests with a considerable mean survival time comparable to that of standard drug, chloroquine (10 mg/kg).ConclusionsThe findings show that ethanol extract of A. africana leaf possesses potent antiplasmodial activity which justify the use in ethnomedicine and can be developed in malaria therapy.     

Antidiarrhoeal efficacy of Mangifera indica seed kernel on Swiss albino mice

ObjectiveTo examine the antidiarrhoeal activity of alcoholic and aqueous seed kernel extract of Mangifera indica (M. indica) on castor oil-induced diarrhoeal activity in Swiss albino mice.MethodsMango seed kernels were processed and extracted using alcohol and water. Antidiarrhoeal activity of the extracts were assessed using intestinal motility and faecal score methods.ResultsAqueous and alcoholic extracts of M. indica significantly reduced intestinal motility and faecal score in Swiss albino mice.ConclusionsThe present study shows the traditional claim on the use of M. indica seed kernel for treating diarrhoea in Southern parts of India.     

Saccharomyces boulardii Inhibits Water and Electrolytes Changes Induced by Castor Oil in the Rat Colon

The biotherapeutic agent Saccharomyces boulardii has been shown to inhibit castor oil-induced diarrhoea in rats. The present study investigated the mechanism(s) of this antidiarrhoeal effect in terms of water and electrolyte (sodium, potassium and chloride) changes using two rat models. A single oral dose of S. boulardii of up to 12 × 10¹⁰ CFU/kg of viable cells did not inhibit castor oil-induced fluid secretion in the enteropooling model. However, the yeast dose dependently reduced castor oil induced fluid secretion into the colon, with a significant protection at 12 × 10¹⁰ CFU/kg. In this model, castor oil reversed net sodium and chloride absorption into net secretion, and increased net potassium secretion into the lumen. Single pre-treatment with S. boulardii at 4 and 12 × 10¹⁰ CFU/kg dose dependently decreased these electrolyte changes. In conclusion, S. boulardii possesses potent anti-secretory properties versus water and electrolyte secretion induced by castor oil in the rat colon.     

Analgesic and anti-inflammatory activities of Piper nigrum L.

ObjectiveTo evaluate and compare the analgesic and anti-inflammatory activity of pure compound, piperine along with hexane and ethanol extracts of Piper nigrum L. fruit in mice and rats.MethodsThe analgesic activity was determined by tail immersion method, analgesy-meter, hot plate and acetic acid induced writhing test. While the anti-inflammatory activity was evaluated by carrageenan-induced paw inflammation in rats.ResultsPiperine at a dose of 5 mg/kg and ethanol extract at a dose of 15 mg/kg after 120 min and hexane extract at a dose of 10 mg/kg after 60 min exhibited significant (P<0.05) analgesic activity by tail immersion method, in comparison to ethanol extract at a dose of 10 mg/kg using analgesy-meter in rats. However, with hotplate method, piperine produced significant (P<0.05) analgesic activity at lower doses (5 and 10 mg/kg) after 120 min. A similar analgesic activity was noted with hexane extract at 15 mg/kg. However, in writhing test, ethanol extract significantly (P<0.05) stopped the number of writhes at a dose of 15 mg/kg, while piperine at a dose of 10 mg/kg completely terminated the writhes in mice. In the evaluation of anti-inflammatory effect using plethysmometer, piperine at doses of 10 and 15 mg/kg started producing anti-inflammatory effect after 30 min, which lasted till 60 min, whereas hexane and ethanol extracts also produced a similar activity at a slightly low dose (10 mg/kg) but lasted for 120 min.ConclusionsIt is concluded from the present study that Piper nigrum L possesses potent analgesic and anti-inflammatory activities.     

Effects of Lactuca sativa extract on exploratory behavior pattern,locomotor activity and anxiety in mice

ObjectiveTo evaluate antianxiety property of Lactuca sativa, an important and commonly used leafy vegetable known for its medicinal properties belongs to Asteraceae family.MethodsElevated plus maze (EPM), open field test (OFT), rat exposure test, hyponeophagia and marble burying test were performed in mice models to assess the exploratory behaviour and to assess anxiolytic property of hydro-alcohol extract of Lactuca sativa. Diazepam (1 mg/kg body wt.) served as the standard anxiolytic agent for all the tests. The dried extract of the plant leaf in doses of 100, 200 and 400 mg/kg body weight was administered orally to mice for duration of 15 or 30 days and evaluated exploratory behaviour, locomotor and anxiolytic activities.ResultsTime spent and number of entries into the open arm was measured in EPM followed by total locomotor activity in OFT and latency to enter the food zone in hyponeophagia.ConclusionsThe study suggested that hydro-alcohol extract of Lactuca sativa leaves possess potent anxiolytic property.     

Antinociceptive and anti-inflammatory activities of crude extracts of Ipomoea involucrata leaves in mice and rats

ObjectiveTo investigate antinociceptive and anti-inflammatory activities of crude extract from Ipomoea involucrata leaves (Convolvulaceae) in mice and rats.MethodsThe antinociceptive activity was tested using acetic acid-induced abdominal writhing test in mice. The anti-inflammatory activity was evaluated using egg albumin induced oedema of rat paw.ResultsPhytochemical screening showed the presence of alkaloids, flavonoids, saponins, terpenoids and tannin. At the doses of 25–100 mg/kg, Ipomoea involucrata exhibited dose-dependent and significant increase in pain threshold in acetic acid –induced writhing test of mice (P<0.05, student t-test) The administration of Ipomoea involucrata leaf extract (25–100 mg/kg) showed dose-dependent decreases in paw volume of egg albumin induced oedema in rats and a significant higher anti-inflammatory activity compared to the standard control (Aspirin).ConclusionsThese results support the claims on the traditional use of the of Ipomoea involucrata leaves in the treatment of toothache, rheumatic pains and other inflammatory conditions. Studies on the isolation and structural elucidation of the active principle are still needed being carried out.     

Antimalarial and analgesic activities of ethanolic leaf extract of Panicum maximum

ObjectiveTo evaluate antiplasmodial and analgesic activities of ethanolic leaf extract/fractions of Panicum maximum.MethodsThe crude leaf extract (47–190 mg/kg) and fractions (chloroform, ethyl acqeous and methanol; 96 mg/kg) of Panicum maximum were investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice and for analgesic activity against chemical and heat-induced pains. The antiplasmodial activity during early and established infections as well as prophylactic were investigated. Artesunate at 5 mg/kg and pyrimethamine at 1.2 mg/kg were used as positive controls. Analgesic activity of the crude extract/fractions was also evaluated against acetic acid, formalin and heat-induced pains.ResultsThe extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine sensitive Plasmodium berghei infection in prophylactic, suppressive and curative models in mice. These reductions were statistically significant (P<0.001). They also improved the mean survival time from 13 to 28 days compared with control (P<0.001). The activities of extract/fractions were incomparable to that of the standard drugs (Artesunate and pyrimethamine). On chemically and thermally-induced pains, the extract inhibited acetic acid and formalin-induced inflammation as well as hot plate-induced pain in mice. These inhibitions were statistically significant (P<0.001) and in a dose-dependent fashion.ConclusionsPanicum maximum leaf extract has antiplasmodial and analgesic activities which may in part be mediated through the chemical constituents of the plant.     

Antiplasmodial and antipyretic studies on root extracts of Anthocleista djalonensis against Plasmodium berghei

ObjectiveTo evaluate the antimalarial activities of ethanolic root extract/fractions of Anthocleista djalonensis (A. djalonensis) in Plasmodium berghei (P. berghei) infected mice.MethodsA. djalonensis root extract (175–1 000 mg/kg) and fractions (chloroform, ethyl acetate and methanol; 250 and 500 mg/kg) were investigated for antiplasmodial activity against chloroquine-sensitive Plasmodium berghei infections in mice and for antipyretic activity against dinitrophenol, amphetamine and yeast-induced pyrexia. The antiplasmodial activity during early and established infections as well as prophylactic were investigated. Artesunate (5 mg/kg) and pyrimethamine (1.2 mg/kg) were used as positive controls. Antipyretic activity of the crude extract was also evaluated against dinitrophenol, amphetamine and yeast-induced pyrexia.ResultsThe extract and its fractions dose-dependently reduced parasitaemia induced by chloroquine sensitive Plasmodium berghei infection in prophylactic, suppressive and curative models in mice. These reductions were statistically significant (P<0.001). They also improved the mean survival time from 13 to 28 days relative to control (P<0.001). The activities of extract/fractions were comparable to that of the standard drugs used (chloroquine and pyrimethamine). On pyrexia induced by dinitrophenol, amphetamine and yeast, the extract inhibited significantly (P<0.05 – 0.001) and in a dose-dependent fashion temperature rise caused by these pyrogens.ConclusionsA. djalonensis root extract has antiplasmodial and antipyretic activities which may in part be mediated through the chemical constituents of the plant.     

Antimalarial potency of the methanol leaf extract of Maerua crassifolia Forssk (Capparaceae)

ObjectiveTo investigate the in vivo antiplasmodial effect of methanol leaf extract of Maerua crassifolia in mice infected with chloroquine sensitive Plasmodium berghei berghei.MethodsThe extract was evaluated for activity against early infection, curative effect against established infection at dose levels of 100, 200 and 400 mg/kg p.o. Chloroquine at 10 mg/kg was used as standard drug.ResultsA dose dependent chemo-suppression of the parasites was obtained at different dose levels of the extract tested with a considerable mean survival time.ConclusionsThe results support continued investigation of components of traditional medicines as potential new antimalarial agents.     

Pain management in mice using methanol extracts of three plants belongs to family Amaranthaceae

ObjectiveTo investigate the analgesic activity of methanolic extract of Amaranthus viridis (A. viridis), Amaranthus caudatus (A. caudatus) and Amaranthus spinosus (A. spinosus).MethodsIn this study, the analgesic activity of methanol extracts of all three plants at doses of 200 and 400 mg/kg were investigated by acetic acid-induced writhings test, hot plate test and tail immersion test for mice.ResultsIt was found that all the three plants showed significant pain management effect (P<0.01) at a dose of 400 mg/kg, but showed a less significant effect at a dose of 20 mg/kg in the entire tests used for evaluation of analgesic activities (P<0.05).ConclusionsMethanol extracts of A. viridis, A. caudatus and A. spinosus show potent analgesic activities, and this study provides the scientific proof for their traditional claims.