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1.
Molecules ; 28(2)2023 Jan 09.
Article in English | MEDLINE | ID: mdl-36677731

ABSTRACT

Despite the current management options and therapeutics used in the treatment of diarrhoea, in Africa and Asia, diarrhoea remains a major concern, especially in children under the age of 5 years. Traditional knowledge of medicinal plants used in the management of diarrhoea symptoms can be explored for their efficacy. In Nigeria, the TMPs (Traditional Medicine Practitioners) have, over the years, employed medicinal plants in the management of diarrhoea symptoms. In our current and previous studies, we aimed at validating the effectiveness of Neorautanenia mitis in the management of diarrhoea as claimed by the TMPs. Out of the 20 compounds isolated from N. mitis, the compounds neodulin, pachyrrhizine, neotenone and dolineone were the most abundant, and in this study, neodulin showed a pronounced relaxation of the rhythmic contraction of the isolated rabbit jejunum in an organ bath in a concentration-dependent manner, with a complete relaxation at 60 µg/mL. Neotenone and dolineone showed a dose-dependent inhibition of defecation of 65.07%, and 50.01%, respectively, at 20 mg/kg in a castor-oil-induced diarrhoea model. This is a strong indication that compounds from N. mitis possess antidiarrhoeal properties, thereby giving credence to its traditional usage in diarrhoea therapy, and therefore validating its antidiarrhoeal activity and its being worthy of further investigation.


Subject(s)
Fabaceae , Plants, Medicinal , Animals , Rabbits , Antidiarrheals/pharmacology , Antidiarrheals/therapeutic use , Plant Extracts/therapeutic use , Phytotherapy , Diarrhea/drug therapy , Diarrhea/chemically induced , Castor Oil , Nigeria
2.
Data Brief ; 36: 107155, 2021 Jun.
Article in English | MEDLINE | ID: mdl-34041327

ABSTRACT

This article describes the dataset for the elucidation of the possible mechanisms of antidiarrhoeal actions of methanol leaves extract of Combretum hypopilinum (Diels) Combretaceae in mice. The plant has been used in traditional medicine to treat diarrhoea in Nigeria and other African countries. We introduce the data for the antidiarrhoeal activity of the methanol leaf extract of Combretum hypopilinum at 1,000 mg/kg investigated using charcoal meal test in mice with loperamide (5 mg/kg) as the standard antidiarrhoeal agent. To elucidate the possible mechanisms of its antidiarrhoeal action, naloxone (2 mg/kg), prazosin (1 mg/kg), yohimbine (2 mg/kg), propranolol (1 mg/kg), pilocarpine (1 mg/kg) and isosorbide dinitrate (150 mg/kg) were separately administered to different groups of mice 30 minutes before administration of the extract. Each mouse was dissected using dissecting set, and the small intestine was immediately removed from pylorus to caecum, placed lengthwise on moist filter paper and measured the distance travelled by charcoal relative to the length of the intestine using a calibrated ruler in centimetre. Besides, the peristaltic index and inhibition of charcoal movement of each animal were calculated and recorded. The methods for the data collection is similar to the one used to investigate the possible pathways involved in the antidiarrhoeal action of Combretum hypopilinum in mice in the research article by Ahmad et al. (2020) "Mechanisms of Antidiarrhoeal Activity of Methanol Leaf Extract of Combretum hypopilinum Diels (Combretaceae): Involvement of Opioidergic and (α1 and ß)-Adrenergic Pathways" (https://doi.org/10.1016/j.jep.2020.113750) [1]. Therefore, this datasets could form a basis for in-depth research to elucidate further the pharmacological properties of the plant Combretum hypopilinum and its bioactive compounds to develop standardized herbal product and novel compound for management of diarrhoea. It could also be instrumental for evaluating the plant's pharmacological potentials using other computational-based and artificial intelligence approaches, including predictive modelling and simulation.

3.
J Ethnopharmacol ; 269: 113750, 2021 Apr 06.
Article in English | MEDLINE | ID: mdl-33359856

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: The plant Combretum hypopilinum Diels (Combretaceae) is used in traditional medicine for the treatment of diarrhoea and other diseases in Africa. Previously, the antidiarrhoeal activity of its methanol leaf extract was reported. However, the mechanism(s) responsible for this activity is yet to be evaluated. AIM OF THE STUDY: This study aimed to elucidate the possible mechanism(s) of antidiarrhoeal activity of methanol leaf extract of Combretum hypopilinum (MECH) in mice. MATERIALS AND METHODS: Phytochemical screening and acute toxicity study were conducted according to standard methods. Adult mice were orally (p.o) administered distilled water (10 ml/kg), MECH (1000 mg/kg) and loperamide (5 mg/kg). The probable mechanisms of antidiarrhoeal activity of MECH were investigated following pretreatment with naloxone (2 mg/kg, subcutaneously), prazosin (1 mg/kg, s.c), yohimbine (2 mg/kg, intraperitoneally), propranolol (1 mg/kg, i.p), pilocarpine (1 mg/kg, s.c) and isosorbide dinitrate (150 mg/kg, p.o) 30 min before administration of MECH (1000 mg/kg). The mice were then subjected to castor oil-induced intestinal motility test. RESULTS: The oral median lethal dose (LD50) of MECH was found to be higher than 5000 mg/kg. There were significant (p < 0.05) decrease in the charcoal movement in the mice treated with the MECH (1000 mg/kg) and loperamide (5 mg/kg). The pretreatment of the mice with naloxone, prazosin and propranolol each significantly (p<0.05) reversed the antidiarrhoeal activity produced by MECH. CONCLUSION: The results obtained in this study suggest the probable involvement of opioidergic and (α1 and ß)-adrenergic systems in the antidiarrhoeal activity of the methanol leaf extract of Combretum hypopilinum.


Subject(s)
Antidiarrheals/pharmacology , Combretum/chemistry , Diarrhea/drug therapy , Plant Extracts/pharmacology , Receptors, Adrenergic/drug effects , Receptors, Opioid/drug effects , Animals , Antidiarrheals/therapeutic use , Castor Oil/toxicity , Diarrhea/chemically induced , Female , Gastrointestinal Motility/drug effects , Lethal Dose 50 , Loperamide/pharmacology , Loperamide/therapeutic use , Male , Medicine, African Traditional , Methanol/chemistry , Mice , Nitric Oxide/metabolism , Plant Extracts/chemistry , Plant Extracts/therapeutic use , Plant Leaves/chemistry , Receptors, Cholinergic/drug effects , Signal Transduction/drug effects
4.
Microb Pathog ; 149: 104582, 2020 Dec.
Article in English | MEDLINE | ID: mdl-33086104

ABSTRACT

The main objective of the present investigation was to mechanistically evaluate the potency of the root extract (EEC), its bioactive chloroform fraction (CEC) and eriosematin E (ECM) isolated from Eriosema chinense against Shigella flexneri-induced sub-chronic model of infectious diarrhoea using in vitro, in vivo, and in silico methods. The in vitro antibacterial activity against pathogenic strain of S. flexneri demonstrated maximum effect of ECM followed by CEC and EEC in inhibiting growth of bacteria. Further, for in vivo evaluation, was carried out by inducing diarrhoea to the rats by administering oral suspension of S. flexneri to the animals, which was followed by treatment for a period of 6 days. EEC at 200, CEC at 100 and ECM at 10 mg/kg, p.o. showed promising effect, where EEC and ECM were found to be more effective showing maximum % protection on 6th day. Results also demonstrated a significant restoration of altered antioxidants, pro-inflammatory cytokines (IL-1ß and TNF-α) expression, electrolyte balance, Na+/K+-ATPase activity and was also supported by histopathological examinations. Molecular docking study revealed that, eriosematin E inactivated the protease activity of SepA, a protein secreted by Shigella, which is responsible for disruption of epithelial barrier integrity. Thus, the overall observation confirmed the role of eriosematin E from E. chinense in treatment of Shigella flexneri-induced infectious diarrhoea.


Subject(s)
Antidiarrheals , Fabaceae , Animals , Antidiarrheals/pharmacology , Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Molecular Docking Simulation , Rats , Shigella flexneri
5.
J Ethnopharmacol ; 251: 112561, 2020 Apr 06.
Article in English | MEDLINE | ID: mdl-31926988

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: The plant Psidium guajava L. (Myrtaceae), commonly used as an edible fruit is traditionally used worldwide in treatment of various gastrointestinal problems including diarrhoea. The leaves of the plant have also been evaluated for antidiarrhoeal activity in various chemical induced diarrhoea models. OBJECTIVE: The main objective of the present study was to evaluate the potency of P. guajava leaves and its major biomarker quercetin against enteropathogenic Escherichia coli (EPEC) induced infectious diarrhoea using preclinical and computational model. MATERIAL AND METHODS: P. guajava alcoholic leaf extract (PGE) was initially standardized using HPLC taking quercetin as a biomarker and was then subjected to antidiarrhoeal evaluation on rats in an EPEC induced diarrhoea rat model. The study included assessment of various behavioral parameters, initially for 6 h and then for up to 24 h of induction which was followed by estimation of stool water content, density of EPEC in stools and blood parameters evaluation. The colonic and small intestinal tissues of the treated animals were subjected to various biochemical estimations, in vivo antioxidant evaluation, estimation of ion concentration, Na+/K+-ATPase activity, assessment of pro-inflammatory cytokines and histopathological studies. Further, the major biomarker off PGE, quercetin was subjected to molecular docking studies with Na+/K+-ATPase and EPEC. RESULTS: The results demonstrated a significant antidiarrhoeal activity of quercetin (50 mg/kg), PGE at 200 and 400 mg/kg, p.o., where quercetin and PFGE at 200 mg/kg, p.o. were found to be more prominent, as confirmed through higher % protection, water content of stools and density of EPEC in stools. PGE and its biomarker quercetin also significantly recovered the WBC, Hb, platelets loss and also revealed a significant restoration of altered antioxidants level, pro-inflammatory cytokines (IL-1ß and TNF-α) expression and had positive influence on Na+/K+-ATPase activity. The docking studies of quercetin with Na+/K+-ATPase showed favourable interactions and residues Glu 327, Ser 775, Asn 776, Glu 779 and Asp 804 of Na+/K+-ATPase were adequately similar to quercetin for donating ligands for binding, while quercetin was also found to terminate the linkage between mammalian cells and EPEC thus, preventing further infection from EPEC. CONCLUSION: Inhibition in intestinal secretion, reduced nitric oxide production and inflammatory expression along with reactivation of Na+/K-ATPase activity could be attributed to the observed antidiarrhoeal potential of PGE against infectious diarrhoea, where quercetin was confirmed to be the main contributing factor.


Subject(s)
Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Enteropathogenic Escherichia coli , Escherichia coli Infections/drug therapy , Plant Extracts/therapeutic use , Psidium , Quercetin/therapeutic use , Animals , Antidiarrheals/pharmacology , Colon/drug effects , Colon/pathology , Escherichia coli Infections/metabolism , Escherichia coli Infections/pathology , Female , Intestine, Small/drug effects , Intestine, Small/metabolism , Male , Molecular Docking Simulation , Nitric Oxide/metabolism , Plant Extracts/pharmacology , Plant Leaves , Quercetin/pharmacology , Rats, Wistar , Sodium-Potassium-Exchanging ATPase/metabolism
6.
Microb Pathog ; 138: 103807, 2020 Jan.
Article in English | MEDLINE | ID: mdl-31629796

ABSTRACT

The leaves of the plant Psidium guajava L. (Myrtaceae) has been traditionally used in treatment of various gastrointestinal disorders including diarrhoea and have also been reported for its potent antidiarrhoeal activity on various chemical induced diarrhoea models. The objective of our present study was to evaluate the potency of the leaf extract of the plant Psidium guajava (PGE) along with its major biomarker quercetin against Shigella flexneri-induced sub chronic model of infectious diarrhoea. PGE at 100, 200 and 400 mg/kg, p.o. and quercetin at 50 mg/kg, p.o. were administered to Shigella flexneri-induced diarrhoeal rats for five days and various behavioural parameters were evaluated on 1st, 3rd and 5th day of treatment. This was followed by assessment of stool water content, density of Shigella flexneri in stools and blood parameters examination. After treatment, colon and small intestine of rats was dissected and subjected to biochemical estimations, cytokine profiling, antioxidant evaluations, ion concentration determination, Na+/K+-ATPase activity and histopathology. Molecular docking studies on crystal structure of Secreted Extracellular Protein A (SepA) from Shigella flexneri with biomarker quercetin was also performed. PGE at 200 mg/kg followed by quercetin depicted maximum antidiarrhoeal potential, which was confirmed through diarrhoea score and % protection, while PGE at 400 mg/kg showed similar effect to PGE 200 mg/kg thus, the later may have ceiling effect. PGE and quercetin also significantly reduced the density of Shigella flexneri in stools, water content of stools and restored the alterations observed in blood parameters, antioxidant status and pro-inflammatory cytokines (IL-6 and TNF-α) expression. These parameters contributed in normalization of electrolyte balance, reactivation of Na+/K+-ATPase activity and repairing of epithelial tissue damage, confirmed through histopathology. Docking simulation studies revealed the role of quercetin in inactivating the protease activity of SepA, a protein secreted by Shigella, which disrupts epithelial barrier integrity during infection and also manages its signal production. Thus, the overall results confirmed the role of quercetin as a major biomarker for the observed antidiarrhoeal potential of P. guajava against Shigella flexneri induced infectious diarrhoea.


Subject(s)
Anti-Bacterial Agents/pharmacology , Bacterial Proteins/antagonists & inhibitors , Diarrhea/microbiology , Plant Extracts/pharmacology , Psidium/metabolism , Quercetin/pharmacology , Shigella flexneri/drug effects , Animals , Anti-Bacterial Agents/chemistry , Biomarkers , Cytokines/metabolism , Diarrhea/diagnosis , Diarrhea/drug therapy , Disease Models, Animal , Female , Inflammation Mediators/metabolism , Male , Molecular Docking Simulation , Molecular Dynamics Simulation , Plant Extracts/chemistry , Psidium/chemistry , Quercetin/chemistry , Rats , Shigella flexneri/enzymology , Structure-Activity Relationship
7.
Acta Trop ; 193: 84-91, 2019 May.
Article in English | MEDLINE | ID: mdl-30807750

ABSTRACT

The main objective of the present study was to evaluate the potential of eriosematin E (ECM) isolated from the roots of Eriosema chinense against enteropathogenic Escherichia coli (EPEC) induced diarrhoea. ECM isolated from the bioactive chloroform fraction of E. chinense was subjected to antidiarrhoeal evaluation on rats against diarrhoea, induced by the oral suspension of EPEC. The study included evaluation of behavioral parameters for 6 h and up to 24 h of induction, followed by estimation of water content, the density of EPEC in stools and evaluation of various blood parameters. Further, the colonic and small intestinal tissues were subjected to biochemical estimations, antioxidant evaluation, determination of ion concentration, Na+/K+ -ATPase activity, pro-inflammatory cytokines assessment and histopathology. Finally, the impact of ECM on Na+/K+-ATPase was studied through molecular docking studies. Significant antidiarrhoeal potential of ECM was demonstrated at 5 and 10 mg/kg, p.o., however, ECM at 10 mg/kg, p.o. was found to be more effective, as confirmed through higher % protection, density of EPEC in stools and water content of stools. ECM also significantly increased the level of WBC, Hb, platelets and revealed restoration of altered antioxidants, pro-inflammatory cytokines (IL-1ß and TNF-α) status and also reactivated the suppressed Na+/K+-ATPase activity, which was also confirmed through docking studies showing H-bonding of hydroxyl group of ECM with amino acids Asp 190, Asn 167 and Glu 169 thus, maintaining proper electrolyte balance and also prevented epithelial tissue damage. The overall effect of ECM may be attributed to the decline in the elevated level of cytokines, inhibition in nitric oxide production and reactivation of Na+/K+-ATPase activity resulting in reduced intestinal secretion.


Subject(s)
Diarrhea/drug therapy , Enteropathogenic Escherichia coli , Escherichia coli Infections/complications , Fabaceae , Plant Extracts/therapeutic use , Animals , Antioxidants/metabolism , Cytokines/metabolism , Diarrhea/microbiology , Feces/chemistry , Intestinal Mucosa/drug effects , Intestinal Mucosa/metabolism , Intestines , Plant Extracts/analysis , Plant Extracts/pharmacology , Plant Roots , Rats , Sodium-Potassium-Exchanging ATPase/metabolism
8.
Phytomedicine ; 24: 127-133, 2017 Jan 15.
Article in English | MEDLINE | ID: mdl-28160852

ABSTRACT

BACKGROUND: Roots of the plant Eriosema chinense Vogel (Fabaceae) is distributed mainly over the Eastern Himalayan region of India and China. The roots of the plant are used as a vegetable by the people of Northern Australia, China and North East India and are used traditionally by the tribal people of Meghalaya (India) for the treatment of diarrhoea. It has been reported to have significant antidiarrhoeal, cytotoxic and antimycobacterial activity. PURPOSE/OBJECTIVE: The present investigation was undertaken to isolate a lead molecule responsible for the observed antidiarrhoeal activity. METHODS: Eriosematin E, a prenylated flavanone, was isolated using column chromatography and was characterized by comparing its melting point and spectroscopic data (UV, IR, 1H NMR, 13C NMR, Mass Spectra) from literature. Eriosematin E (2.5, 5 and 10mg/kg p.o.) was then screened for normal faecal excretion rate and castor oil-induced diarrhoea models in rats. Further, it was examined for small intestinal transit, intestinal fluid accumulation and PGE2 induced enteropooling models in rats. Biochemical estimations and Na+ and K+ concentration in intestinal fluid were also determined along with colonic histopathological studies. RESULTS: The results illustrated a significant (P< 0.05) reduction in normal faecal output at 10mg/kg p.o. after 5th and 7thh of treatment and also showed maximum protection of 69.43% from diarrhoea in the castor oil-induced diarrhoea model. Significant results were also observed at the maximum effective dose of eriosematin E (10mg/kg p.o.) in inhibiting peristaltic index (small intestinal transit) and reducing intestinal fluid volume of castor oil induced and PGE2 induced enteropooling models. Further, eriosematin E restored all the alterations in biochemical parameters such as nitric oxide, protein, DNA, superoxide dismutase, catalase and lipid peroxidation. It also significantly recovered Na+ and K+ loss from body and confirmed its protective nature through the histopathological studies. CONCLUSION: The study corroborates the antidiarrhoeal potential of eriosematin E which may be attributed to its antisecretory and antioxidant potential.


Subject(s)
Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Fabaceae/chemistry , Flavanones/therapeutic use , Intestines/drug effects , Plant Extracts/therapeutic use , Plant Roots/chemistry , Animals , India , Male , Phytotherapy , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Rats
9.
J Ethnopharmacol ; 176: 225-31, 2015 Dec 24.
Article in English | MEDLINE | ID: mdl-26514064

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Caladium bicolor (Araceae) is a horticulture plant also used by some traditional medicine practitioners in the treatment of diarrhoea and other gastrointestinal disorders. This study was conducted to evaluate the antidiarrhoeal activity of the aqueous leaf extract of C. bicolor and its possible mechanisms of action in rodents. MATERIALS AND METHODS: Normal and castor oil-induced intestinal transit and castor oil-induced diarrhoea tests were carried out in mice while gastric emptying and enteropooling tests were conducted in rats following the administration of distilled water (10 ml/kg, p.o.), C. bicolor extract (1-50mg/kg, p.o.) and loperamide (5mg/kg, p.o.). The probable mechanisms of action of C. bicolor was investigated following pre-treatment with yohimbine (10mg/kg, s.c.; α2-adrenoceptor antagonist), pilocarpine (1mg/kg, s.c.; non-selective muscarinic receptor agonist), prazosin (1mg/kg, s.c.; α1-adrenoceptor antagonist) and propranolol (1mg/kg, i.p.; non-selective ß-adrenoceptor antagonist) 15 min prior to administration of C. bicolor extract (50mg/kg, p.o.). After 30 min of pre-treatment with these drugs, the mice were subjected to the castor oil-induced intestinal transit test. RESULTS: C. bicolor extract did not produce significant (p>0.05) effect on normal intestinal transit unlike loperamide which caused significant (p<0.001) inhibition (61.57%). The extract caused significant (p<0.001) dose-dependent inhibition of castor oil-induced intestinal transit with peak effect, 100% inhibition, elicited at the dose of 50mg/kg compared to 86.97% inhibition for loperamide. Yohimbine and pilocarpine most significantly (p<0.001) reversed this effect of the extract. In the castor oil-induced diarrhoea test, the extract (1mg/kg) and loperamide significantly (p<0.05, 0.01) delayed the onset of diarrhoea. For diarrhoea score, the extract (1 and 50mg/kg) inhibited diarrhoea development (47.53% and 43.83% inhibition, respectively) like loperamide (5mg/kg; 54.94%). The in vivo antidiarrhoeal index of the extract at 1 and 50mg/kg was 50.07% and 42.81% respectively compared to 58.15% for loperamide. CONCLUSIONS: The results obtained in this study suggest that the aqueous leaf extract of C. bicolor possess antidiarrhoeal activity due to its anti-motility effect possibly via antagonist action on intestinal muscarinic receptors and agonist action on intestinal α2-adrenoceptors. This justifies the use of the extract in traditional medicine for the treatment of diarrhoea.


Subject(s)
Adrenergic alpha-2 Receptor Agonists/therapeutic use , Antidiarrheals/therapeutic use , Araceae , Diarrhea/drug therapy , Muscarinic Antagonists/therapeutic use , Plant Extracts/therapeutic use , Adrenergic alpha-2 Receptor Agonists/pharmacology , Adrenergic alpha-2 Receptor Agonists/toxicity , Adrenergic alpha-2 Receptor Antagonists/pharmacology , Animals , Antidiarrheals/pharmacology , Antidiarrheals/toxicity , Castor Oil , Diarrhea/chemically induced , Diarrhea/metabolism , Female , Gastric Emptying/drug effects , Gastrointestinal Transit/drug effects , Intestinal Secretions/metabolism , Male , Mice , Muscarinic Agonists/pharmacology , Muscarinic Antagonists/pharmacology , Muscarinic Antagonists/toxicity , Phytotherapy , Pilocarpine/pharmacology , Plant Extracts/pharmacology , Plant Extracts/toxicity , Plant Leaves/chemistry , Rats , Toxicity Tests, Acute , Water/chemistry , Yohimbine/pharmacology
10.
J Pharm Pharmacol ; 66(12): 1808-17, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25130980

ABSTRACT

OBJECTIVE: To scientifically validate the traditional substitution of roots of highly expensive Aconitum heterophyllum (AH) with rhizomes of Cryptocoryne spiralis (CS) in the treatment of diarrhoea. METHODS: Different fractions from root/rhizome extract of both the plant were subjected to faecal excretion rate and castor oil-induced diarrhoea models. Further, bioactive fractions from both plants, i.e. chloroform (CAH) from AH at 50 mg/kg p.o. and ethyl acetate (EACS) from CS at 100 mg/kg p.o., were examined for small intestinal transit, intestinal fluid accumulation and PGE2 -induced enteropooling models in rats. Biochemical estimations and Na(+) and K(+) concentration in intestinal fluid were also determined along with antibacterial studies. Phytochemical standardisation of AH and CS was performed by quantifying aconitine for the former and stigmasterol for the latter using HPLC. KEY FINDINGS: CAH and EACS illustrated a significant reduction in faecal output rate and demonstrated a protection of 63.068% at CAH 50 and 59.090% at EACS 100 mg/kg p.o. in castor oil-induced diarrhoea model. The fractions also persuaded promising effects in all the other models, restored alterations in biochemical parameters and showed potential antibacterial activity. CONCLUSION: The antidiarrhoeal potential of AH and CS may be attributed to an antimotility and antisecretory type of effect.


Subject(s)
Aconitum/chemistry , Antidiarrheals/therapeutic use , Araceae/chemistry , Diarrhea/drug therapy , Plant Extracts/therapeutic use , Animals , Antidiarrheals/isolation & purification , Antidiarrheals/toxicity , Castor Oil/pharmacology , Diarrhea/chemically induced , Female , Gastrointestinal Transit/drug effects , India , Male , Medicine, Ayurvedic , Plant Extracts/isolation & purification , Plant Extracts/toxicity , Rats , Rhizome/chemistry , Toxicity Tests, Acute
11.
J Ethnopharmacol ; 151(2): 984-9, 2014 Feb 03.
Article in English | MEDLINE | ID: mdl-24342781

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Pupalia lappacea is a medicinal plant found in savannah and woodland localities and forest path sides from Senegal to Southern Nigeria. It has been used in the management of diarrhoea in Nigerian traditional medicine. This study was designed to evaluate the antidiarrhoeal activity of the hydroethanolic leaf extract of Pupalia lappacea (PL). MATERIALS AND METHODS: The antidiarrhoeal activity of PL was evaluated using the normal and castor oil-induced intestinal transit, castor oil-induced diarrhoea, gastric emptying and intestinal fluid accumulation tests in rodents. RESULTS: PL (100-400mg/kg, p.o.) produced a significant dose-dependent decrease in normal and castor oil-induced intestinal transit compared with the control group (distilled water 10ml/kg, p.o.). This effect was significantly (P<0.05) inhibited by pilocarpine (1mg/kg, s.c.) but not by yohimbine (10mg/kg, s.c.), prazosin (1mg/kg, s.c.), or propranolol (1mg/kg, i.p.). The extract produced a dose-dependent and significant increase in the onset of diarrhoea. PL (100-400mg/kg) also reduced the diarrhoea score, number and weight of wet stools. The in-vivo antidiarrhoeal index (ADIin vivo) of 56.95% produced by the extract at the dose of 400mg/kg was lower compared to that produced by loperamide 5mg/kg (77.75%). However, PL (400mg/kg) significantly increased gastric emptying in rats but significantly reduced the volume of intestinal content in the intestinal fluid accumulation test. Phytochemical analysis of the extract revealed the presence of alkaloids, saponins, and fixed oils and fats. The acute toxicity studies revealed that the extract is relatively safe when given orally; no death was recorded at a dose of 10g/kg. CONCLUSION: Results showed that the hydroethanolic leaf extract of Pupalia lappacea possesses antidiarrhoeal activity possibly mediated by antimuscarinic receptor activity.


Subject(s)
Amaranthaceae , Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Plant Extracts/therapeutic use , Animals , Castor Oil , Diarrhea/chemically induced , Ethanol/chemistry , Female , Gastric Emptying/drug effects , Gastrointestinal Transit/drug effects , Male , Mice , Phytotherapy , Plant Leaves/chemistry , Rats , Rats, Wistar , Solvents/chemistry , Toxicity Tests, Acute , Water/chemistry
12.
Article in English | MEDLINE | ID: mdl-24146500

ABSTRACT

This study was undertaken to evaluate the antidiarrhoeal activity of 3, 7, 4'-trihydroxy-3'-(8″-acetoxy-7″-methyloctyl)-5, 6-dimethoxyflavone, a flavonoid isolated from the stem bark of Stereospermum kunthianum. The antidiarrhoeal activity was evaluated using rodent models with diarrhoea. The normal intestinal transit, castor oil-induced intestinal transit and castor oil-induced diarrhoea tests in mice as well as castor oil-induced intestinal fluid accumulation in rats were employed in the study. The animals were pretreated with distilled water (10 ml/kg for mice, 5 ml/kg for rats), dimethoxyflavone (25 mg/kg or 50 mg/kg), morphine (10 mg/kg), or indomethacin (10 mg/kg) before induction of diarrhoea with castor oil (0.2ml for mice and 2ml for rats). Dimethoxyflavone dose dependently and significantly reduced (P<0.05) castor oil-induced intestinal motility. Its antimotility effect at the dose of 50 mg/kg was higher compared to that of morphine (10 mg/kg). Dimethoxyflavone (25 mg/kg and 50 mg/kg) caused a delay in the onset of diarrhoea reduction in the number and weight of wet stools and total stools in mice with castor oil-induced diarrhoea compared to the distilled water treated mice. Treatment with dimethoxyflavone (25 mg/kg or 50 mg/kg) did not produce any remarkable effect on castor oil-induced intestinal fluid accumulation in rats and normal intestinal transit in mice. The results indicate that dimethoxyflavone possesses antidiarrhoeal activity due to its intestinal antimotility effect and inhibition of other diarrhoeal pathophysiological processes. In conclusion, dimethoxyflavone reduced the frequency and severity of diarrhoea in the diarrhoeal models studied.


Subject(s)
Antidiarrheals/therapeutic use , Bignoniaceae/chemistry , Diarrhea/drug therapy , Flavones/therapeutic use , Phytotherapy , Plant Extracts/therapeutic use , Animals , Antidiarrheals/pharmacology , Castor Oil , Defecation/drug effects , Diarrhea/chemically induced , Feces , Flavones/pharmacology , Gastrointestinal Motility/drug effects , Mice , Mice, Inbred Strains , Plant Bark , Plant Extracts/pharmacology , Plant Stems , Rats , Rats, Wistar
13.
Article in English | MEDLINE | ID: mdl-23983341

ABSTRACT

Piliostigma reticulatum (Caesalpiniaceae) is used in Africa as a traditional medicine for the treatment of many diseases, such as malaria, tuberculosis and diarrhoea. We investigated the antidiarrhoeal properties of a crude ethanol extract from the stem bark of Piliostigma reticulatum (EEPR) in Wistar albino rats to substantiate its traditional use and to determine its phytochemical constituents. The antidiarrhoeal activity of the plant extract was evaluated in a castor oil-induced diarrhoea model in rats and compared with loperamide. The effect of the extract on gastrointestinal motility was also determined by the oral administration of charcoal meal and castor oil-induced intestinal fluid accumulation (enteropooling). EEPR showed remarkable dose-dependent antidiarrhoeal activity evidenced by a reduction of defecation frequency and change in consistency. Extracts at 250, 500 and 1000 mg/kg body weight significantly reduced diarrhoeal faeces. EEPR also significantly inhibited gastrointestinal motility and castor oil-induced enteropooling at 500 and 1000 mg/kg, similar to the inhibition obtained in control rats treated by atropine. Phytochemical screening revealed the presence of tannins, flavonoids, polyphenols and reducing sugars in the stem bark of P. reticulatum. No mortality or visible signs of general weakness were observed in the rats following administration of the crude extract in doses up to 6000 mg/kg body weight in an acute toxicity study. Our results show that the stem bark of P. reticulatum possesses antidiarrhoeal activity and strongly suggest that its use in traditional medicine practice could be justified.


Subject(s)
Antidiarrheals/therapeutic use , Diarrhea/drug therapy , Gastrointestinal Motility/drug effects , Magnoliopsida/chemistry , Phytotherapy , Plant Extracts/therapeutic use , Animals , Antidiarrheals/pharmacology , Atropine/pharmacology , Castor Oil , Charcoal , Defecation/drug effects , Diarrhea/chemically induced , Dose-Response Relationship, Drug , Feces , Female , Loperamide/pharmacology , Loperamide/therapeutic use , Male , Medicine, African Traditional , Plant Bark , Plant Extracts/pharmacology , Plant Stems , Polyphenols/analysis , Polyphenols/pharmacology , Polyphenols/therapeutic use , Rats , Rats, Wistar , Tannins/analysis , Tannins/pharmacology , Tannins/therapeutic use
14.
Asian Pac J Trop Biomed ; 2(6): 430-2, 2012 Jun.
Article in English | MEDLINE | ID: mdl-23569944

ABSTRACT

OBJECTIVE: To evaluate the antidiarrhoeal property of methanol extract of the leaves of Rauwolfia serpentina (R. serpentina) in experimental diarrhoea induced by castor oil in mice. METHODS: Doses of 100, 200 and 400 mg/kg R. serpentina leaf methanol extracts were administered to castor oil induced diarrhoea mice to determine its antidiarrhoeal activity. RESULTS: All doses of the extract and the reference drug atropine sulphate (3 mg/kg, i.p.) produced a dose-dependent reduction in intestinal weight and fluid volume. The extracts also significantly reduced the intestinal transit in charcoal meal test when compared to diphenoxylate Hcl (5 mg/kg, p.o.). CONCLUSIONS: The results show that the extract of R. serpentina leaves has a significant antidiarrhoeal activity and supports its traditional uses in herbal medicine.


Subject(s)
Antidiarrheals/administration & dosage , Diarrhea/drug therapy , Plant Extracts/administration & dosage , Rauwolfia/chemistry , Animals , Antidiarrheals/isolation & purification , Diarrhea/chemically induced , Diarrhea/pathology , Disease Models, Animal , Dose-Response Relationship, Drug , Intestines/pathology , Mice , Plant Extracts/isolation & purification , Plant Leaves/chemistry
15.
Article in Chinese | WPRIM (Western Pacific) | ID: wpr-500378

ABSTRACT

Objective:To evaluate the antidiarrhoeal property of methanol extract of the leaves of Rauwolfia serpentina (R. serpentina) in experimental diarrhoea induced by castor oil in mice. Methods:Doses of 100, 200 and 400 mg/kg R. serpentina leaf methanol extracts were administered to castor oil induced diarrhoea mice to determine its antidiarrhoeal activity. Results: All doses of the extract and the reference drug atropine sulphate (3 mg/kg, i.p.) produced a dose-dependent reduction in intestinal weight and fluid volume. The extracts also significantly reduced the intestinal transit in charcoal meal test when compared to diphenoxylate Hcl (5 mg/kg, p.o.). Conclusions: The results show that the extract of R. serpentina leaves has a significant antidiarrhoeal activity and supports its traditional uses in herbal medicine.

16.
Article in English | LILACS | ID: lil-613286

ABSTRACT

Desmostachya bipinnata root has been used in the Indian traditional system of medicine for treatment of diarrhoea and dysentery. The antidiarrhoeal effect of both alcoholic and aqueous extracts of the roots of Desmostachya bipinnata were studied in rats against castor oil induced diarrhoea and charcoal meal test at the doses of 200 and 400 mg/kg body weight. The alcoholic extract and to a lesser extent aqueous extract significantly reduced the weight of the faces and decreased the propulsion of charcoal meal through the gastrointestinal tract. The phytochemical screening of the extracts showed the presence of alkaloids, glycosides, flavonoids, tannins, phytosterol, terpenoids, polyphenolics, protein and carbohydrates. These results may support the fact that this plant is used traditionally to cure diarrhoea.


La raíz de Desmostachya bipinnata ha sido utilizada en el sistema tradicional de medicina Hindú para el tratamiento de diarrea y disentería. El efecto antidiarreico de los extractos alcohólicos y acuosos de los extractos de la raíz de Desmostachya bipinnata fueron estudiados en ratas, utilizando la diarrea inducida por aceite de castor y el ensayo de la prueba por carbón en dosis de 200 y 400 mg/kg de peso corporal. El extracto alcohólico y en menor grado, el extracto acuoso, redujeron significativamente la propulsión de carbón a través del tracto gastrointestinal. El análisis de los extractos mostrarón la presencia de alcaloides, glicósidos, flavonoides, taninos, fitoesterol, terpenoides, polifenoles, proteínas y carbohidratos. Estos resultados pueden apoyar el hecho de que esta planta sea usada tradicionalmente para curar la diarrea.


Subject(s)
Animals , Rats , Antidiarrheals/pharmacology , Diarrhea/drug therapy , Ethanol/pharmacology , Plant Extracts/pharmacology , Poaceae/chemistry , Plant Roots/chemistry , Castor Oil , Diarrhea/chemically induced , Gastrointestinal Motility , Rats, Wistar
17.
Indian J Pharm Sci ; 71(6): 691-5, 2009 Nov.
Article in English | MEDLINE | ID: mdl-20376227

ABSTRACT

The antidiarrhoeal effect of the water extract of Melastoma malabathricum Linn. (Melastomataceae) leaves were investigated by employing four experimental models of diarrhea in Swiss mice. Melastoma malabathricum water extract treated mice showed significant reduction in the fecal output and protected them from castor oil-induced diarrhoea. The extract also reduced the intestinal fluid secretion induced by magnesium sulphate and gastrointestinal motility after charcoal meal administration in the mice. No mortality and visible signs of general weakness was observed in the mice following the test extract administration up to 2000 mg/kg dose.

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