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Context: In China, the herb Sophora tonkinensis Gagnep. (Fabaceae, ST) (Committee of National Pharmacopeia. 2015) exhibits anti-inflammatory, antitumor, and antiviral effects. However, to date, there have been few studies on its gastrointestinal effect. Objective: The gastrointestinal effect of the methanol extract of ST rhizome (STR) was evaluated. Materials and methods: Study was conducted from February to December 2018. In vivo, antidiarrheal activity of STR (125, 250 and 500 mg/kg; orally) in castor oil-induced diarrheal mice was studied. In vitro, the effects of STR (0.01–10 mg/mL) on the isolated tissue preparations of rabbit jejunum were also investigated, the rabbit jejunum stripes were pre-contracted with Ach (10−5 M), K+ (60 mM) and tested in the presence of STR, the possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with STR or verapamil in Ca2+-free high-K+ (60 mM) solution containing EDTA. Results: STR (125, 250 and 500 mg/kg) exhibited antidiarrheal activity. STR (0.01–10 mg/mL) completely relaxed spontaneously contracting, Ach (10−5 M) and high K+ (60 mM) induced contracted jejunum with an EC50 value of 0.66 (0.49–0.96), 0.39 (0.28–0.44) and 0.17 (0.10–0.21), similar to verapamil. Concentration–response curves of CaCl2 could be significantly moved to the right and down in the presence of STR (0.3, 1 mg/mL). Discussion and conclusions: Results suggest the presence of antidiarrheal activity and spasmolytic effects of STR, possibly mediated through Ca2+ channel blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal disorders.

Context: In China, the herb Sophora tonkinensis Gagnep. (Fabaceae, ST) (Committee of National Pharmacopeia. 2015) exhibits anti-inflammatory, antitumor, and antiviral effects. However, to date, there have been few studies on its gastrointestinal effect. Objective: The gastrointestinal effect of the methanol extract of ST rhizome (STR) was evaluated. Materials and methods: Study was conducted from February to December 2018. In vivo, antidiarrheal activity of STR (125, 250 and 500 mg/kg; orally) in castor oil-induced diarrheal mice was studied. In vitro, the effects of STR (0.01–10 mg/mL) on the isolated tissue preparations of rabbit jejunum were also investigated, the rabbit jejunum stripes were pre-contracted with Ach (10−5 M), K+ (60 mM) and tested in the presence of STR, the possible spasmolytic effect was analyzed in the pretreatment of the jejunum preparations with STR or verapamil in Ca2+-free high-K+ (60 mM) solution containing EDTA. Results: STR (125, 250 and 500 mg/kg) exhibited antidiarrheal activity. STR (0.01–10 mg/mL) completely relaxed spontaneously contracting, Ach (10−5 M) and high K+ (60 mM) induced contracted jejunum with an EC50 value of 0.66 (0.49–0.96), 0.39 (0.28–0.44) and 0.17 (0.10–0.21), similar to verapamil. Concentration–response curves of CaCl2 could be significantly moved to the right and down in the presence of STR (0.3, 1 mg/mL). Discussion and conclusions: Results suggest the presence of antidiarrheal activity and spasmolytic effects of STR, possibly mediated through Ca2+ channel blocking activity, providing the pharmacological basis for its traditional uses in gastrointestinal disorders. [ABSTRACT FROM AUTHOR]

Context:Gaultheria trichophyllaRoyle (Ericaceae) and related species have been used in the traditional system of medicine for the treatment of diarrhoea, pain and inflammation. Objective:The present investigation exploresG. trichophyllafor its potential activity in hyperactive gut disorders. Materials and methods:Antidiarrheal activity was evaluated on castor oil induced diarrhoea in mice with reference to standard drug verapamil. Gut modulatory activity was performed on isolated jejunum tissue preparations on spontaneous and high potassium induced contractions. Butyrylcholinesterase (BChE) inhibitory activity was performed with anin vitrostudy. Extract was tested for toxicity in mice. Results:In thein vivostudies, the methanol extract ofG. trichophyllaand verapamil significantly (p < 0.05, 0.01, 0.001) inhibited the frequency of defecation as well as wetting of faeces when compared with the negative control. The methanol (Gt. MeOH) extract ofG. trichophyllacaused a dose-dependent inhibitory effect on spontaneous contractions in isolated rabbit jejunum preparations and exhibited a partial inhibitory effect against high K+ (80 mM) induced precontractions. Gt. MeOH shifted the Ca2+ concentration–response curves (CRCs) to the right, suggesting calcium channel blocking like constituents. In anin vitroassay Gt. MeOH inhibited BChE enzyme with an IC50values of 35.52 ± 1.17 μg/mL. The extract showed no toxicity in mice at the dose of 3 g/kg. Discussion and conclusion:This study provides evidence thatG. trichophyllapossesses combinations of inhibitory and stimulatory effects mediated through possible cholinergic and less potent calcium blocking constituents, respectively. The latter may be responsible for the antidiarrheal effect. [ABSTRACT FROM AUTHOR]

Context: Carpolobia lutea G. Don (Polygalaceae) leaf is reputable as an antidiarrheal agent among the Efik and Ibibio tribe of Akwa Ibom State, Nigeria. The crude extract is reported to show antidiarrheal and antiulcer effects in rodents. Objective: The isolation and characterization of drug molecules from the leaf fraction with antidiarrheal bioactivity and determination of mechanism of action are reported. Material and methods: Gradient extraction by maceration yielding n-hexane, chloroform, ethyl acetate, and ethanol fractions (770 mg/kg) were used to establish the fractions suitable for drug discovery. The antidiarrheal effect of the leaf fractions of Carpolobia lutea was evaluated using castor oil-induced diarrhea, castor oil-induced intestinal transit, and enteropooling. Results: Results indicate that all fractions produced a significant ( p < 0.01-0.001) decrease in castor oil-induced diarrhea in rats. This effect was not antagonized by isosorbide dinitrate (150 mg/kg, p.o), diphenoxylate (5 × 10−3 mg/kg p.o) and yohimbine (1 mg/kg, s.c.) except for the chloroform fraction. The ethyl acetate fraction produced 100% inhibition of intestinal transit, an effect greater than pure drug. Phytochemical analysis of the ethyl acetate fraction yielded polyphenolic compounds. Conclusion: The leaf fractions contain two types of antidiarrheal agents, one mediating its effect through α1-presynaptic adrenoceptor while the other does not. Polyphenols isolated may in part lend credence for observed antidiarrheal activity. [ABSTRACT FROM AUTHOR]

Context: Alocasia indica Schott (Araceae) is used in several regions of India, especially in rural communities, by traditional medicine practitioners to treat diarrhea. However, no scientific data are available to justify the traditional potentials of the plant species in gastrointestinal disorders. Objective: To evaluate the antidiarrheal and in vitro antiprotozoal activities of extracts of leaves of Alocasia indica using various pharmacological models. Materials and methods: In vitro antidiarrheal activity of aqueous and ethanol extracts of Alocasia indica was evaluated against Escherichia coli, Salmonella typhimurium, Shigella flexneri and Staphylococcus aureus by agar well diffusion method. In vivo antidiarrheal activity of the extracts was studied against recinolic acid-induced diarrhea and magnesium sulfate-induced diarrhea. The effect of the extracts on normal intestinal transit, recinolic acid-induced intestinal transit, recinolic acid-induced intestinal fluid accumulation (enteropooling) and gastric emptying was assessed. In vitro antiprotozoal activity of aqueous and ethanol extracts of Alocasia indica was studied against Entamoeba histolytica and Giardia intestinalis. Results: The aqueous and ethanol extracts exhibited significant in vitro antidiarrheal activity compared to the standard drug ciprofloxacine (10 µµg/mL). The plant extracts showed significant (P <0.05) and dose-dependent antidiarrheal activity comparable to that of the reference drug, loperamide (10 mg/kg). The plant extracts exhibited significant in vitro antiprotozoal activity against both protozoa compared to the standard amebicidal and giardicidal drugs, metronidazole and emetine. Discussion and conclusion: The results showed that the extracts of Alocasia indica have significant antidiarrheal and in vitro antiprotozoal activities which support its use in traditional herbal medicine practice. [ABSTRACT FROM AUTHOR]

Context: This study evaluated the in vitro and in vivo antidiarrheal activity, oral acute toxicological profile, and developed a chemical fingerprint of Berberis aristata Linn. (Berberidaceae). Materials and methods: The ethanol (by maceration) and aqueous (by Soxhlet) extracts of Berberis aristata bark were used for the study. The study involved the antimicrobial (minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) by micro dilution) and antidiarrheal (castor oil induced diarrhea, charcoal motility) tests. The active principle, berberine was characterized by different spectroscopic and chromatographic techniques. Results: The MIC and MBC (of both extracts) against all strains of Shigella were recorded between 125 to 500 µg/mL and 300 to 600 µg/mL, respectively. The MIC and MBC values of berberine are almost comparable to standard ciprofloxacin. UV and IR spectroscopy along with HPTLC and HPLC studies showed presence of berberine in the extracts. The onset of castor oil induced diarrhea was delayed and number of diarrheal episodes was reduced by both the extracts in a dose dependent manner. Similarly, the length of intestine traveled by the feed was also significantly reduced in the charcoal motility test by both the extracts. LD50 of >5000 mg/kg body weight was observed for both extracts in the acute oral toxicity studies with Swiss albino mice. Conclusion: The results validate in vivo and in vitro antidiarrheal activity of Berberis aristata extracts and provide its chemical fingerprint. [ABSTRACT FROM AUTHOR]

This study describes the antidiarrheal, antisecretory, and bronchodilatory activities of Hypericum perforatum Linn. (Hypericaceae), commonly known as St. John’s wort, to justify its traditional use in the hyperactivity of the gastrointestinal and respiratory systems. The crude extract of Hypericum perforatum (Hp.Cr) at a dose of 500 mg/kg caused 20% protection against castor oil-induced diarrhea in mice and 60% at 1000 mg/kg ( p < 0.05 vs. saline). Hp.Cr at 300 and 1000 mg/kg reduced the castor oil-induced fluid accumulation in mice to 107.0 ± 3.3 g ( p < 0.01) and 84.0 ± 4.2 g ( p < 0.001) respectively, whereas in the castor oil-treated group, it was 126.9 ± 3.9 g. When tested against carbachol (CCh)-mediated bronchoconstriction in rats under anesthesia, Hp.Cr dose-dependently (3– 30 mg/kg) suppressed the CCh (1 μmol/kg)-induced increase in the inspiratory pressure. Thus this study rationalizes the Hypericum perforatum usefulness in overactive gut and airways disorders, such as diarrhea and asthma. [ABSTRACT FROM AUTHOR]

The ethanol extract (50%) of the whole plant of Amaranthus spinosus Linn. (Amaranthaceae) (ASE) significantly inhibited travel of a charcoal meal at three different doses of ASE, but when 400 mg/kg of ASE was repeated in the presence of yohimbine, intestinal propulsive inhibition decreased, while morphine reversed the activity. The percentages related to controls for the onset of diarrhea were 16.58, 83.42, and 116.18% at doses of 100, 200, and 400 mg/kg of ASE, while with morphine this value was 123.93% compared to controls. The percentage purging frequency related to controls was 41.09, 64.38, 71.23, and 86.30% at three different doses of ASE and with morphine, respectively. The inhibitions in intestinal accumulation were 8.9, 48.16, and 68.06% at doses of 100, 200, and 400 mg/kg of ASE, respectively, compared to control, while inhibition with yohimbine was 50.78%. Antidiarraheal indices of ASE were 23.55, 49.16, and 76.53 at the three different doses of ASE, while morphine had a maximum index of 88.45. Protection in ethanol- induced ulcer was 51.07, 55.91, 77.95, and 60.75%, but in aspirin-induced ulcer it was 41.33, 61.77, 80.88, and 74.66% at doses of 100, 200, and 400 mg/kg of ASE and with cimetidine, respectively. Lipid peroxidation was also associated with a concomitant decrease in ulcer index, while protection was 56.96, 63.29, 81.01, and 52.32% at three different doses of ASE and with cimetidine in cold restraint-induced ulcer. [ABSTRACT FROM AUTHOR]

Piperine is a piperidine-ring containing alkaloid and a major constituent of Piper nigrum Linn. and Piper longum Linn. species, belonging to the Piperaceae family. The present study explored their mode of action in gastrointestinal disorders, such as diarrhea and colic. Piperine at the dose of 10 mg/kg provided complete protection from castor oil-induced diarrhea in mice, similar to that of loperamide. In isolated rabbit jejunum preparations, piperine exhibited concentration-dependent inhibition of spontaneous contractions with an EC50 value of 149.1 μM (89.26–249.20, 95% CI). When used to treat high K+ (80 mM)-induced sustained contractions, piperine inhibited such contractions with an EC50 value of 80.86 μM (56.10–116.50, 95% CI), which suggested a calcium channel blocking (CCB) effect. The CCB effect was further confirmed when pretreatment of the tissues with piperine (10–100 μM) caused a rightward shift in the Ca++ concentration–response curves (CRCs) in Ca++-free medium, similar to that caused by verapamil. Loperamide also caused the inhibition of spontaneous and high K+-induced contractions as well as shifted the Ca++ CRCs to the right at concentrations of 1–10 μM. These data indicate that piperine exhibits antidiarrheal and antispasmodic activities, mediated possibly through calcium channel blockade. [ABSTRACT FROM AUTHOR]

The effect of the aqueous (aq) seed extract of Aframomum melegueta K. Schum. (Zingiberaceae) on castor oil-induced diarrhea, intestinal fluid secretion, and gastrointestinal transit was investigated in the study. Castor oil (10 ml/kg, p.o.) induced copious diarrhea in all rats 3h after treatment. Furthermore, it produced a significant increase in the volume of intestinal fluid secretion in rats and also enhanced intestinal transit in mice. The aq seed extract of A. melegueta (100–500 mg/kg, p.o.) offered significant protection against diarrhea induced by the oil. At a dose range of 250–500 mg/kg, the extract reduced significantly the volume of fluid secretion in castor oil-treated rats. At these doses, it also demonstrated a significant antitransit activity in a dose-related manner. Acetylsalicylic acid (100 mg/kg, p.o.) delayed diarrhea and reduced the number of animals with diarrheal droppings to 20%. At the same dose level, acetylsalicylic acid reduced significantly the volume of intestinal fluid secretion but lacked antitransit property in castor oil-treated animals. N-Nitro-L-arginine methyl ester (L-NAME) (2.5–10 mg/kg, i.p.) dose-dependently reduced the number of animals with diarrhea. At 50 mg/kg i.p., it offered 100% protection against diarrhea induced by the oil. Furthermore, L-NAME (10 mg/kg, i.p.) significantly inhibited both the intestinal fluid secretion and gastrointestinal transit induced by castor oil. However, L-NAME (10 mg/kg, i.p.) did not significantly modify the antidiarrheal effect of A. melegueta. L-Arginine, a substrate of nitric oxide synthase or isosorbide dinitrate, a nitric oxide donor, did not alter the effect of A. melegueta on diarrhea. Ascorbic acid (100 mg/kg, p.o.) and α-tocopherol (20 mg/kg, p.o.) reduced the number of animals with diarrhea to 80% and 70%, respectively. However, they both lacked significant activities on intestinal fluid secretion and gastrointestinal transit induced by castor oil. The combination of ascorbic acid (100 mg/kg, p.o.) or α-tocopherol (20 mg/kg, p.o.) with A. melegueta (500 mg/kg) offered higher protection against diarrhea than the extract alone. Considering these results together, it may be inferred that Aframomum melegueta seed extract may be a useful antidiarrheal agent. [ABSTRACT FROM AUTHOR]

The antidiarrheal potential of the methanol extract of the fruit of Emblica officinalis Gaertn. (Euphorbiaceae) was evaluated using several experimental models of diarrhea in Wistar albino rats. The methanol extract showed a significant inhibitory effect on rats with diarrhea induced by castor oil and magnesium sulfate. The methanol extract produced a significant reduction in gastrointestinal motility in charcoal meal tests in rats. It also significantly inhibited PGE2-induced enteropooling as compared to control animals. The results obtained establish the efficacy and substantiate the use of this herbal remedy as a nonspecific treatment for diarrhea in folk medicine. [ABSTRACT FROM AUTHOR]