Inhibition Of Defecation Research Articles

Analgesic, Antidiarrheal and CNS-depressant Activities of Flemingia macrophylla (Willd.)

Plants are the priceless sources of bioactive natural compounds. Medicinal plants have been used since time immemorial in both developing and developed countries. Flemingia macrophylla (Willd.) is widely used as a hereditary medicines. The current study was designed to observe the analgesic, antidiarrheal and CNS depressant activities of methanol extract of the leaves of F. macrophylla (MEFM) and its petroleum ether (PEFM), dichloromethane (DFM), chloroform (CFM) and aqueous (AFM) fractions. The analgesic activities was assessed by acetic acid induced writhing method at doses 200- and 400- mg/kg body weight. The CNS-depressant effect was assayed by phenobarbitone sodium-induced sleeping time test. The anti-diarrheal activity of the extract was evaluated using castor oil-induced diarrhea in mice. The crude extract displayed significant peripheral analgesic activity at both test doses with 56.72- to 59.70-% inhibition of writhing responses, respectively. In CNS-depressant test, the extract revealed its activity in a dose dependent manner. In screening for antidiarrheal activity, the extract exhibited 20.83 and 41.67 % inhibition of defecation at 200- and 400-mg/kg bw, respectively whereas the standard loperamide (50 mg/kg bw) displayed 70.83 % inhibition of defecation. Bangladesh Pharmaceutical Journal 23(2): 141-145, 2020

Bioactivities of Aeschynomene aspera (Fabaceae) Leaf Extract

Aeschynomene aspera (Family- Fabaceae), a traditionally used medicinal plant, is aquatic, perennial, erect subshrub up to 200 cm tall with compound leaves and locally it is called Shola (Bangladesh), Laugaun (India). The study started with phytochemical screening of ethanolic leaf extract of A. aspera followed by bioactivity study such as in-vitro antioxidant activity by free radical (DPPH) scavenging assay, estimation of total phenolic as well as total flavonoid contents and the analgesic, antidiarrheal and anthelmintic activities. Analgesic, antidiarrheal and anthelmintic activities were evaluated by acetic acid induced writhing inhibition in mice, castor oil induced diarrheal episode in mice and using living parasites Haemonchus contortus, respectively. The presence of carbohydrate, reducing sugar, glycosides, tannins, alkaloids, steroids, gums and flavonoids was estimated with the help of phytochemical screening. In DPPH scavenging assay the extract showed IC50 value of 86.14μg/mL where ascorbic acid showed 12.02μg/mL. It also exhibited total phenolic and flavonoid contents as 461.09 GAE/100g and 297.20mg Quercetin/100g of dried plant extract. About 36% and 61% writhing inhibitions were observed in mice at 250 and 500mg/kg doses of A. aspera leaf extract, respectively. Anthelmintic activity showed by the extract was dose dependent. The extract also showed 46.01 and 71.68% inhibition of defecation in mice at doses 250 and 500 mg/kg, respectively. All these suggest that the A. aspera extract possesses antioxidant, analgesic, anthelmintic and antidiarrheal activities. Bangladesh Pharmaceutical Journal 23(2): 109-116, 2020

Anti-diarrhoeal activity of aqueous extract of Cochlospermum planchonii (Hook Fx. Planch) leaves in female Wistar rats

Background: The folkloric use of Cochlospermum planchonii is yet to be substantiated with scientific evidence. Aim: The aqueous extract of C. planchonii leaves was evaluated for anti-diarrhoeal activity at 125, 250 and 500 mg/kg body weight in female Wistar rats. Setting: This research is a phytopharmacological investigation. Methods: Animal were monitored for indicators of diarrhoea in the 3 models after treatments. Results: An aqueous extract of C. planchonii leaves contained 10 secondary metabolites, with alkaloids (16.05 mg/L) occurring the most, whilst quinones (0.7 mg/L) were the least. The extract significantly ( p < 0.05) prolonged the onset time of diarrhoea, decreased water content, fresh weight and total number of wet faeces in a dose-dependent manner, and increased the percentage inhibition of defecation. The extract produced dose-specific changes on intestinal superoxide dismutase, glucose and reduced glutathione whereas the levels of intestinal Na + /K + -ATPase, alkaline phosphatase, catalase, nitric oxide were significantly ( p < 0.05) increased in the castor oil-induced diarrhoeal model. The masses and volumes of intestinal fluid decreased significantly ( p < 0.05) whereas the inhibition of intestinal fluid content increased like those of atropine-treated diarrhoeal rats in the enteropooling model. The extract dose-dependently decreased the distance travelled by the charcoal meal and increased the intestinal nitric oxide and acetylcholinesterase in the charcoal meal transit model. Conclusion: The aqueous extract of C. planchonii leaves exhibited anti-diarrhoeal activity via anti-motility and anti-secretory means. The flavonoids, alkaloids, tannins, phenolics and saponins might have acted to enhance the activities of Na + /K + -ATPase, antioxidant enzymes, intestinal glucose levels and the neurotransmitters.

Synthesis and Evaluation of Disubstituted Benzimidazole Derivatives as Potential Analgesic and Antidiarrheal Agents

The present study is aimed at the synthesis and biological evaluation of a variety of disubstituted benzimidazole derivatives. The disubstituted benzimidazoles, identified as 3a, 3b, 3c, and 3d were synthesized through condensation of o-phenylenediamine compounds with aromatic aldehydes in the presence of ammonium salt as a catalyst and characterized by infrared spectroscopy and 1H nuclear magnetic resonance spectra. The compounds were screened for analgesic and antidiarrheal activities using acetic acid-induced writhing and castor oil-induced diarrhea models, respectively in Swiss mice. Compounds 3c, 3a, and 3b at a dose of 25 mg/kg decreased the number of writhes by 88.81, 69.40 and 64.93 %, respectively (P<0.05) as compared to standard aceclofenac (88.81 %). Derivatives 3d and 3a displayed promising antidiarrheal activity (P<0.05) at both 25 (inhibition of defecation 67.64 and 56.45 %, respectively) and 50 mg/kg dose levels (80.65 and 75.81% inhibition respectively) in comparison to standard loperamide (85.48% inhibition at a dose of 25 mg/kg). Among the synthesized derivatives, 3a emerged as the most effective analgesic and antidiarrheal agent, and it might be employed as a lead compound for future investigation.

Evaluation of Analgesic, Antidiarrheal and Anti-hyperglycemic Activities of Dactyloctenium australe (Poaceae)

Dactyloctenium australe belongs to the family of Poaceae. It is also called gramineae or true grasses. Poaceae is the fifth largest family of flowering plants. The current study was conducted on methanol extract of the aerial parts of D. australe (MEDA) to evaluate its in vivo analgesic activity by acetic acidinduced writhing method in mice. The plant extract was also evaluated for antidiarrheal and antihyperglycemic activities using castor oil-induced diarrhea and oral glucose tolerance test, respectively. In acetic acid-induced writhing test, the extract showed 52.18 % and 62.40 % inhibition of writhing at the doses of 200-400mg/kg body weight, respectively while standard aspirin at the dose of 50 mg/kg bw showed 58.12 % writhing inhibition. In anti-hyperglycemic test, the extract revealed its activity in a dose dependent manner. In antidiarrheal activity test, the extract exhibited 48.54 % and 72.92 % inhibition of defecation at the doses of 250-500mg/kg bw, respectively whereas the standard loperamide (3 mg/kg bw) displayed 70.24 % inhibition of defecation. Bangladesh Pharmaceutical Journal 22(1): 85-91, 2019

Bioactivity studies on Zanthoxylum budrunga wall (Rutaceae) root bark

BackgroundThe root-bark of the medicinally important plant Zanthoxylum budrunga (ZBRB) brooks a variety of uses in ethnobotanical and ethnomedicinal practice in Bangladesh and thus demands biological investigation to reveal its therapeutic potentiality. So, the present study was perpetrated to explore antioxidant, analgesic, antidiarrhoeal, and a cytotoxic activity of ethanolic root-bark extract of Zanthoxylum budrunga and was also to quantify the major bioactive polyphenolic constituents by HPLC analysis.MethodsTotal phenolic content was measured spectrophotometrically by using Folin Chiocalteu’s reagent while in vitro antioxidant activity was determined by means of 2, 2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging assay and reducing power assay. HPLC analysis was performed to identify and quantify the major bioactive polyphenolic constituents present in the extract. Acetic acid induced writhing test and hot-plate test were conducted to evaluate the analgesic activity of the crude extract. On the other hand, in vivo antidiarrheal potentiality was investigated by using experimentally castor oil induced diarrhoea in mice and brine shrimp lethality bio-assay was implemented to check the cytotoxic potentiality of the crude extract.ResultsZanthoxylum budrunga showed DPPH scavenging activity (IC50 54.27 μg/mL), while the total phenolic content was 647.91 mg GAE/100 g of extract. ZBRB also showed concentration dependent ferric reducing power activity. At the doses of 250 and 500 mg/kg, ZBRB exhibited statistically significant (P < 0.001) inhibition of writhing in test mice (64.58 and 77.78%, respectively). In hot-plate test, ZBRB, at the above dose levels, significantly (P < 0.001) prolonged pain threshold with response time of 5.80 and 6.81 s, respectively. In castor oil induced diarrhoeal episode in mice, ZBRB exhibited 66.56% and 83.39% inhibition of defecation at the doses of 250 and 500 mg/kg, respectively (P < 0.001). The LC50 (Median lethal concentration) value of ZBRB in brine shrimp lethality bioassay was found to be 21.84 μg/mL. In the HPLC analysis, (+)-catechin, caffeic acid and quercetin were detected with the concentration of 17.94 mg/100, 3.72 mg/100 and 11.95 mg/100 g of ethanolic extract of ZBRB, respectively.ConclusionThe results rationalize the uses of the plant in traditional medicine for diarrhoeal as well as pain management. Catechin, caffeic acid, and other phenolics constituents might have some function in the observed activity.

Preliminary Phytochemical Screenings and Pharmacological Activities of Three Medicinal Plants of Bangladesh

The present study was designed to evaluate the preliminary phytochemical screening and antimicrobial, antidiarrheal, anti-inflammatory, analgesic, antipyretic, anxiolytic, thrombolytic and membrane stabilizing properties of the methanolic extract of three medicinal plants Perilla ocymoides L., Murraya koenigii (Linn.) Spreng., Baliospermum montanum (Wild.) Muell growing in Bangladesh. In antimicrobial test, maximum zone of inhibition was found against Salmonella typhi (18.0 mm) and Escherichia coli (17.0 mm) by B. montanum extract. In the castor oil-induced antidiarrheal assay, the methanol extract of M. koenigii showed maximum 50% inhibition of defecation. During in-vitro anti-inflammatory test, the methanol extract of B. montanum at 500 μg/ml, b.w. revealed 39.62% inhibition of protein denaturation. Due to analgesia, the M. koenigii extract showed 53.29% inhibition of acetic acidinduced writhing reflex in experimental mice. Antipyretic effect of P. ocymoides, M. Koenigii and B. montanum extractives was assessed by Brewer’s yeast-induced pyrexia in mice. The B. montanum extract possesses significant anxiolytic effect that was evidenced by both hole cross test and open field test in mice. In thrombolytic assay, the highest activity (57.81%) was observed by B. montanum extract. Results of the preliminary phytochemical screenings demonstrated the presence of alkaloids, glycosides, flavonoids, reducing sugars, gums etc.Dhaka Univ. J. Pharm. Sci. 16(2): 195-203, 2017 (December)

Investigations of Sedative and Antidiarrheal Activity of &lt;i&gt;Commelina appendiculata&lt;/i&gt; in Swiss Albino Mice

The aim of the present study was to investigate the sedative and antidiarrheal activity of ethanol extract ofC. appendiculataat the doses of 100 and 200 mg/kg body weight per oral (p.o) inSwiss albinomice. Sedative activity of the extract (100 and 200 mg/kg, p.o.) was assessed utilizing thiopental sodium-induced sleeping time model to evaluate sedative potential of the extract, hole cross to evaluate motor activity and open field test to evaluate exploratory behaviour. The extract also produced rapid onset and maximized the duration of sleeping time when administered with thiopental sodium. The extract fundamentally (p &lt; 0.05-0.001) diminished motor action and exploratory conduct of mice in hole cross and open field test separately. In antidiarreal activity study, the concentrate (200 mg/kg) likewise demonstrated most extreme inhibition of defecation (90.64% and 80.95%) in both models individually. The present study demonstrates that the ethanol extract ofC. appendiculatahave central nervous system (CNS) depressant and antidiarrheal properties. In this manner, the plant may be further investigated to find for its pharmacological active natural products.

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

Context Manilkara zapota (L.). P. Royen. (Sapotaceae) has been used in folk medicine to treat pain, diarrhoea, inflammation, arthralgia, and other disorders.Objective Screening of Manilkara zapota leaves ethanol extract and its different solvent soluble fractions for possible antinociceptive and antidiarrhoeal activities in Swiss albino mice.Materials and methods The extract and various fractions (200 and 400 mg/kg body weight; p.o.) were tested for peripheral and central antinociceptive activity by acetic acid-induced writhing and radiant heat tail-flick method, respectively; castor oil-induced diarrhoeal model was used to evaluate antidiarrhoeal activity at both doses. All the samples were administered once in a day and the duration of study was approximately 5 h.Results Ethanol extract (400 mg/kg), petroleum ether fraction (400 mg/kg), and ethyl acetate fraction (400 mg/kg) showed significant peripheral antinociceptive activity having 59.89, 58.24, and 46.7% (p < 0.001) of writhing inhibition, respectively, which is comparable with that of standard diclofenac (59.34% inhibition). The ethanol extract (400 mg/kg) and petroleum ether fraction (400 mg/kg) also showed promising central analgesic activity having 74.15 and 82.15% (p < 0.001) elongation of reaction time, respectively, at 90 min after administration of sample which is also similar to that obtained by morphine (85.84% elongation). In antidiarrhoeal activity screening, ethanol extract (200 and 400 mg/kg) showed significant inhibition of defecation by 53.57 and 60.71%, respectively (p < 0.001) compared with that of loperamide (71.42%).Discussion and conclusion The findings of the studies demonstrated antinociceptive and antidiarrhoeal activities of M. zapota leaves which could be the therapeutic option against pain and diarrhoeal disease.

Anti-diarrhoeal and anti-microbial activity of Flos populi (male inflorescence of Populus tomentosa Carrière) aqueous extracts

Ethnopharmacological relevanceFlos populi (male inflorescence of Populus tomentosa Carrière) has been traditionally used in East Asian countries for the treatment of various inflammatory diseases, strengthening the spleen and stomach, anti-rheumatic, anti-tumor and anti-diarrhoeal. Aim of the studyTo evaluate the in vivo or in vitro anti-diarrhoeal and anti-microbial activity of Flos populi aqueous extract. Materials and methodsAcute toxicity of Flos populi aqueous extract (FPAE) was investigated. Castor oil-induced diarrhoea method was used to evaluate the anti-diarrhoeal activity, inhibition of defecation and diarrhoea were determined in mice, effects on castor oil-induced enteropooling, intestinal transit and intestinal fluid secretion in rats or mice. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of FPAE against strains of three clinical bacterial isolates and one reference strain were used to test the anti-microbial activity. ResultsThe FPAE reduced the frequency of diarrhoea episodes and decreased the propulsion of charcoal meal through the gastrointestinal tract in a dose dependent manner. FPAE (100–500mg/kg, p.o.) produced dose-dependent and significant (P<0.01) protection of mice against castor oil-induced diarrhoea. FPAE, dose-dependently and significantly (P< 0.01) delayed the onset of castor-oil induced diarrhoea, decreased the frequency of defecation, and reduced the severity of diarrhoea. Compared with control animals, FPAE, dose-dependently and significantly (P< 0.01) decreased the volume of castor oil-induced intestinal fluid secretion, and reduced the number, weight and wetness of faecal droppings. There was no deaths or abnormalities in behaviour seen in the acute toxicity test. The aqueous extract displayed anti-microbial effects to three species of bacteria in anti-microbial test. ConclusionThe findings of this study indicate that FPAE possesses anti-diarrhoeal property in rats and mice and confirm the ethnomedicinal use of Flos Populi as a valuable natural remedy for the treatment, management and/or control of diarrhoea. These results may support the fact that this plant is traditionally used to cure diarrhoea.

Evaluation of Antinociceptive, Antidiarrheal and Antimicrobial Activities of Leaf Extracts of Clerodendrum indicum

Introduction: The methanolic extracts and its different partitioning fractions of leaves of Clerodendrum indicum were evaluated for their anti-nociceptive, anti-diarrheal and in vitro antimicrobial activities. Methods: The anti-nociceptive activity was evaluated using the acetic acid-induced writhing test in mice; the anti-diarrheal activity was investigated by the effect of extracts on castor oil-induced diarrhea while the in vitro antimicrobial activities were examined by the disc diffusion method. Results: In the acetic acid-induced writhing test, the methanolic extract at a dose of 200 and 400 mg/kg showed a significant (p<0.001) and dose-dependent reduction in the number of writhes with 62.57% and 70.76% of inhibition, respectively, while the CCL4 fraction at the same dose showed potent anti-nociceptive activity (p<0.001) with 73.09% of inhibition of writhing which was even higher than that of standard diclofenac sodium (55.56% inhibition). The methanolic extract, CCL4 and chloroform fraction showed moderate activity against the tested microorganisms in terms of both zones of inhibition (ranged from 9–13 mm, 10–13 mm and 10–13 mm, respectively, at a concentration of 400 µg/disc) and spectrum of activity. In castor oil-induced diarrhea testing, the methanolic extract and chloroform fraction at a dose of 400 mg/kg produced 21.74% and 26.96% inhibition of defecation, respectively, which were found to be comparable to that of standard drug loperamide (37.39% inhibition at 50 mg/kg ) with regard to the severity of diarrhea. Conclusion: The results of the investigation demonstrated that the methanolic extract and its different fractions of leaves of Clerodendrum indicum possess significant anti-nociceptive, antimicrobial and antidiarrheal activities.

Assessment of the antidiarrhoeal properties of the aqueous extract, the 80% methanol extract and its soluble fractions of the leaves of Alstonia congensis Engl. (Apocynaceae) in Wistar rats

Aim of the studyTo evaluate the antidiarrhoeal properties of Alstonia congensis leaves claimed to be effective for the treatment of diarrhoea by traditional healers during our ethnopharmacological investigation conducted in Kinshasa, Democratic Republic of Congo. Materials and methodsThe aqueous extract (decoction), and the 80% hot methanol extract (Soxhlet extraction) were obtained. This last extract was fractionated. The antidiarrhoeal activity was evaluated using castor oil and magnesium sulphate-induced diarrhoea in animals. The potential antibacterial activity of all samples was also assessed in vitro. ResultsAt all oral doses of 100 and 200mg/kg body weight, all A. congensis samples showed significant and dose-dependent antidiarrhoeal activity in treated Wistar rats characterised by significant increase of onset time and decrease of all other diarrhoeal parameters at various degrees compared to untreated groups in both models. At the highest oral dose of 200mg/kg bodyweight, the 80% hot methanol and aqueous extracts produced 79.8±2.1% and 78.6±0.5%, and 75.0±2.1% and 71.4±2.1% inhibition of defecation and diarrhoea respectively against castor oil-induced diarrhoea, and 75.0±1.2% and 73.3±1.2% inhibition of diarrhoea respectively against magnesium sulphate-induced diarrhoea. The 80% hot methanol and aqueous detannified extracts showed low activity (42–47% inhibition of defecation and/or diarrhoea in both tests) suggesting that tannins may be responsible for the observed activity. At the same oral doses, the total alkaloid extract, the chloroform soluble fraction rich in alkaloids, the 80% methanol and the alkaline aqueous soluble subfractions produced more than 50% inhibition of defecation and/or diarrhoea in both tests. From the antibacterial testing in vitro, results indicated that all A. congensis samples exhibited an antibacterial activity mainly against bacteria implicated in diarrhoea with MIC and MBC values in the range of 15.6–500μg/ml. The most active samples were the aqueous (decoction) and the 80% hot methanol dried extracts, the chloroform subfraction rich in alkaloids and the total alkaloid extract (MIC: 15.7–125μg/ml, MBC: 31.2–250μg/ml). Proteus varibilis was found to be the most resistant microorganism. ConclusionThese reported results can partly support and justify the traditional use of extracts from Alstonia congensis leaves for the treatment of diarrhoea in tradittional medicine.

HU-308: a specific agonist for CB(2), a peripheral cannabinoid receptor.

Two cannabinoid receptors have been identified: CB(1), present in the central nervous system (CNS) and to a lesser extent in other tissues, and CB(2), present outside the CNS, in peripheral organs. There is evidence for the presence of CB(2)-like receptors in peripheral nerve terminals. We report now that we have synthesized a CB(2)-specific agonist, code-named HU-308. This cannabinoid does not bind to CB(1) (K(i) > 10 microM), but does so efficiently to CB(2) (K(i) = 22.7 +/- 3.9 nM); it inhibits forskolin-stimulated cyclic AMP production in CB(2)-transfected cells, but does so much less in CB(1)-transfected cells. HU-308 shows no activity in mice in a tetrad of behavioral tests, which together have been shown to be specific for tetrahydrocannabinol (THC)-type activity in the CNS mediated by CB(1). However, HU-308 reduces blood pressure, blocks defecation, and elicits anti-inflammatory and peripheral analgesic activity. The hypotension, the inhibition of defecation, the anti-inflammatory and peripheral analgesic effects produced by HU-308 are blocked (or partially blocked) by the CB(2) antagonist SR-144528, but not by the CB(1) antagonist SR-141716A. These results demonstrate the feasibility of discovering novel nonpsychotropic cannabinoids that may lead to new therapies for hypertension, inflammation, and pain.

Complex factors in inhibition of defecation: Review and case study

Control of eliminative problems in children through planned reinforcedment is briefly reviewed. Constipation can be less amenable than frequent soiling to modification by a strictly operant methodology, and raises the possibility of congenital anomalies. Since birth, a 4-yr-old boy had been subjected to several hospitalizations, numerous inconclusive medical examinations, daily laxatives, and suppositories for chronic constipation. With the introduction of repetitive suggestions and a material reinforcer, bowel movements were accelerated from nil unless suppositories were used, to a terminal rate of one per day without suppositories or laxatives of any kind.