Antidiarrheal action of Zataria multiflora hydroalcoholic and hexane extracts in mice

Introduction: Zataria multiflora Boiss. is an indigenous herbal plant found in many parts of Iran. This herb is traditionally used as a remedy for treating gastrointestinal disorders including diarrhea. Despite the existence of few pharmacological evidences which support the antispasmodic action of Z. multiflora in vitro, there is no scientific report about therapeutic efficacy of Z. multiflora in animal models. The objective of this research was to investigate the antispasmodic activity of hydroalcoholic and hexane extracts of Z. multiflora on intestinal peristaltic movement as well as assessment of its antidiarrheal action in mice. Methods: Dried leafy branches of Z. multiflora were coarsely powdered and subjected to extraction by ethanol or hexane in a percolator apparatus. Antispasmodic activity of Z. multiflora in vivo was assessed by investigating effect of the extracts on intestinal charcoal meal transit. The antidiarrheal activity of Z. multiflora extracts was evaluated by castor oil and magnesium sulfate-induced diarrhea. The inhibitory effects of the extracts were compared with the standard drug loperamide. Results: The antispasmodic activity of Z. multiflora (20 & 40 mg/kg) hydroalcoholic and hexane extracts was confirmed by a reduction in the distance traveled by charcoal meal alongside the small intestine. Z. multiflora extracts (20 & 40 mg/kg) also significantly attenuated the castor oil and magnesium sulfate-induced diarrhea. Loperamide was more efficacious in reducing number of total stools in both models of diarrhea. Conclusion: The obtained results have established a pharmacological evidence for the folkloric use of the Z. multiflora as an antidiarrhoeal and spasmodic agent

Antispasmodic activity of apigenin and luteolin, two components of Dracocephalum kotschyi extract, on rat ileum contractions

Introduction: Aerial parts of Dracocephalum kotschyi have been used as antispasmodic agents in Iranian traditional medicine. Recent pharmacological studies confirmed antispasmodic activity of D. kotschyi extract. The objective of this research was to investigate antispasmodic activities of apigenin and luteolin to find out if they are responsible for the spasmolytic activity of hydroalcoholic extract of D. kotschyi. Methods: Aerial parts of D. kotschyi were extracted with ethanol. Antispasmodic effect of hydroalcoholic extract of D. kotschyi, apigenin and luteolin were examined on KCl and/or acetylcholine (ACh)-induced contractions in rat isolated ileum. Results: Hydroalcoholic extract of D. kotschyi concentrations-dependently inhibited KCl and ACh induced contractions with IC50 values of 41±10 µg/mL and 133±19 μg/mL, respectively. Apigenin concentrations-dependently inhibited KCl and ACh induced contractions with IC50 values of 57±12 μM and 80±18 µM, respectively. Luteolin concentrations-dependently inhibited KCl induced contractions with IC50 values of 68±14 μM. Loperamide reduced both KCl and ACh induced contraction with IC50 values of 189±44 nM and 82±20 μM, respectively. Conclusion: In this study apigenin and luteolin were identified as two active ingredients responsible for antispasmodic activities of D. kotschyi extract

Study of antispasmodic action of Lavandula angustifolia Mill hydroalcoholic extract on rat ileum

Introduction: Lavender (Lavandula angustifolia Mill) is a herbal medicine widely used for gastrointestinal (GI) disorders. However, its pharmacological action on isolated ileum has not been studied. In this research effect of hydroalcoholic extract of L. angustifolia on isolate ileum contractions was studies and compared with loperamide. Methods: Hydroalcoholic extract of the plant was prepared by percolation method. The total flavonoid contents were assessed by colorimetric technique. A portion of rat ileum was suspended in an organ bath containing Tyrode’s solution. The tissue was kept under 1 g tension at 37°C and continuously gassed with O2. The tissue was stimulated with KCl (80 mM), acetylcholine (ACh, 2 μM) and electrical field stimulation (EFS). Effect of the L. angustifolia extract was studied on ileum contractions and compared with that of loperamide. Results: The yield of hydroalcoholic extract was 17% with total flavonoid content of 185 μg/mL in the stock solution. Loperamide in concentration dependent manner inhibited ileum contractile response to KCl, ACh and EFS. Hydroalcoholic extract of L. angustifolia (8-512 μg/mL) concentration dependently inhibited ileum contraction induced by KCl (IC50 = 88 ± 21 μg/mL), ACh (IC50 = 119 ± 251 μg/mL) and EFS (IC50 = 87 ± 33 μg/mL). The vehicle had no significant effect on ileum contractions. Conclusion: From this study it was concluded that L. angustifolia extract at microgram concentration shows an inhibitory effect on rat ileum smooth muscle. Therefore, isolation and identification of active ingredients are recommended

Inhibitory effect of hydroalcoholic and flavonoids extracts of Dracocephalum kotschyi, and its components luteolin, apigenin and apigenin-4’-galactoside on intestinal transit in mice

Introduction: Dracocephalum kotschyi is an Iranian indigenous herbal plant which has been reported to have antispasmodic activity in vitro. The antispasmodic activity of hydroalcoholic extract of D. kotschyi is reported to be due to its flavonoids constituents including apigenin and luteolin. The objective of this research was to compare antispasmodic activities of hydroalcoholic and flavonoids extracts of D. kotschyi on ileum contractions in vivo. In addition, spasmolytic activity of apigenin, luteolin and apigenin-4'-galactoside were compared. Methods: The hydroalcoholic extract was prepared by percolation method. Flavonoids extract was obtained by solvent-solvent extraction. Antispasmodic effect of the test compounds was assessed by measurement of percent small intestine transit following oral administration of a charcoal meal and compared with control group and standard drug loperamide. Results: Biochemical assessment of flavonoids content of the extracts showed that ethyl-acetate fraction contained higher quantity of flavonoids. Loperamide (2.5 mg/kg) reduced charcoal meal movement by 58% in comparison to control group. Hydroalcoholic extract of D. kotschyi (20 mg/kg) and its ethyl-acetate fraction (20 mg/kg) reduced the intestinal charcoal meal transit by 32% and 90%, respectively. Apigenin, luteolin and apigenen-4'-galactoside with oral dose of 20 mg/kg inhibited intestinal movement of the charcoal meal 93%, 89% and 45%, respectively in comparison with the vehicle treated control groups. Conclusion: This study confirms that both the hydroalcoholic and flavonoids extracts of D. kotschyi have antispasmodic properties in vivo. Antimotility of apigenen-4'-galactoside in mice is probably due to release of apigenin in the gastrointestinal tract

Development of a validated HPLC method for determination of an active component in Pycnocycla spinosa and tablets prepared from its extract

Introduction: Pycnocycla spinosa, a native plant of Iran with approved antispasmodic and antidiarrheal activities, could be a suitable candidate and an alternative remedy for the treatment of diarrhea and irritable bowel syndrome (IBS). Therefore, the aim of this study is formulation of an acceptable dosage form and development of a validated high-performance liquid chromatography (HPLC) method for analysis of active ingredients in its extract and pharmaceutical forms.Methods: Different formulations of P. spinosa tablets were prepared by wet granulation method. The prepared tablets were evaluated for hardness, friability, disintegration time and drug assay. HPLC was carried out based on the extract active ingredient: 6-(4-hydroxy-3-methoxyphenyl)-hexanoic acid (HMPHA) determination in P. spinosa extract and tablets.Results: The mean weight, friability, hardness, and disintegration time of selected formulation (tablet 5 mg) were 217.26 mg, 0.69, 53.6 N and 95.8 seconds, respectively. Similar acceptable results were also found for 10 mg tablets. The assay test showed that the content of HMPHA in each 5 mg and 10 mg tablets were 1.64 μg and 3.59 μg, respectively. The HPLC method showed a good linearity and suitability in its working range: 4.5 to 15 μg/mL.Conclusion: The data showed that the selected formulation of P. spinosa tablets has acceptable physicochemical features

Study of antispasmodic action of Lavandula angustifolia Mill hydroalcoholic extract on rat ileum

Introduction: Lavender (Lavandula angustifolia Mill) is a herbal medicine widely used for gastrointestinal (GI) disorders. However, its pharmacological action on isolated ileum has not been studied. In this research effect of hydroalcoholic extract of L. angustifolia on isolate ileum contractions was studies and compared with loperamide. Methods: Hydroalcoholic extract of the plant was prepared by percolation method. The total flavonoid contents were assessed by colorimetric technique. A portion of rat ileum was suspended in an organ bath containing Tyrode’s solution. The tissue was kept under 1 g tension at 37°C and continuously gassed with O2. The tissue was stimulated with KCl (80 mM), acetylcholine (ACh, 2 μM) and electrical field stimulation (EFS). Effect of the L. angustifolia extract was studied on ileum contractions and compared with that of loperamide. Results: The yield of hydroalcoholic extract was 17% with total flavonoid content of 185 μg/mL in the stock solution. Loperamide in concentration dependent manner inhibited ileum contractile response to KCl, ACh and EFS. Hydroalcoholic extract of L. angustifolia (8-512 μg/mL) concentration dependently inhibited ileum contraction induced by KCl (IC50 = 88 ± 21 μg/mL), ACh (IC50 = 119 ± 251 μg/mL) and EFS (IC50 = 87 ± 33 μg/mL). The vehicle had no significant effect on ileum contractions. Conclusion: From this study it was concluded that L. angustifolia extract at microgram concentration shows an inhibitory effect on rat ileum smooth muscle. Therefore, isolation and identification of active ingredients are recommended

Effect of Hydroalcoholic Extract of Pycnocycla spinosa on Rat Isolated Bladder Contraction

Introduction Pycnocycla spinosa Decne. Ex Boiss. var. spinosa (Fam. Umbelliferae) is a wild plant, growing in Iran (1, 2). Hydroalcoholic extract of P. spinosa is a potent relaxant of isolated ileum (3). In addition, P. spinosa extract was shown to have anti-diarrheal action at doses of 250 mg/kg to 1 mg/kg in mice (3). The anti-spasmodic action of P. spinosa extract is very similar to that of dicyclomine (4) and its anti-diarrheal dose on castor oil-induced diarrhea is very close to that of loperamide (5) and diphenoxylate (6). Therefore, P. spinosa extract could be an alternative remedy for the treatment of gastrointestinal spasm and diarrhea. The underlying mechanism of anti-diarrheal action of P. spinosa extract is most likely related to its gut motility inhibition. It has been shown that P. spinosa extract inhibits ileum contraction induced by KCl, acetylcholine (ACh) and serotonin (3) and therefore, P. spinosa extract may have an inhibitory effect on other smooth muscles, including bladder. Thus, the objective of this study was to investigate the effect of P. spinosa extract on rat isolated bladder contractions for the purpose of comparison with the ileum. Experimental Plant material Aerial parts of P. spinosa were collected and prepared as described before Abstract Hydroalcoholic extract of Pycnocycla spinosa is a relaxant of rat ileum and inhibits diarrhea in mice. As P. spinosa extract has spasmolytic activity on ileum, it could also affect other smooth muscles like bladder. Therefore, the aim of this study was to determine the effect of P. spinosa extract on rat bladder contraction. In an in vitro study, the effects of P. spinosa extract, nifedipine and propantheline were tested on isolated rat bladder contractions induced by acetylcholine (ACh, 10 M) and KCl (80 mM). P. spinosa extract, concentration-dependently, inhibited the bladder contractions induced by ACh with an IC50 of 265±28 mg/ml, and KCl with an IC50 of 518±86 mg/ml. The muscarinic cholinoceptor antagonist, propantheline, inhibited the response of ACh without affecting KCl response. Nifedipine, on the other hand, abolished the KCl response, while partially inhibiting the ACh contraction in rat bladder. The antispasmodic effect of P. spinosa extract on bladder was observed at higher concentrations as compared to that of ileum. Therefore, it is unlikely that P. spinosa extract at anti-diarrheal doses affect the normal bladder emptying function

Antidiarrhoeal assessment of hydroalcoholic and hexane extracts of Dracocephalum kotschyi Boiss. and apigenin in mice

Dracocephalum kotschyi Boiss, a member of Labiatae family, is a native plant to Iran, which has been reported to have immunomodulatory, antihyperlipidemic and antispasmodic activities. The objective of this research was to study the antispasmodic and antidiarrhoeal activities of hydroalcoholic and hexane extracts of D. kotschyi in mice. Furthermore, the antidiarrhoeal and antispasmodic effect of apigenin, a flavonoid constituent of D. kotschyi, was also studied. Hydroalcoholic and hexane extracts were obtained from aerial part of D. kotschyi using percolation method. Antispasmodic effect of the test compounds was assessed by measurement of small intestine transit following oral administration of a charcoal meal. Diarrhoea was induced by administration of either castor oil (0.5 ml) or magnesium sulphate (MgSO4) (10% w/v solution). Both the hydroalcoholic and hexane extracts of D. kotschyi (10 and 20 mg/kg) reduced the intestinal charcoal meal transit. Loperamide (2 mg/kg) and apigenin (2 and 10 mg/kg) inhibited intestinal movement of the charcoal meal and also inhibited castor oil and MgSO4-induced diarrhoea. The hydroalcoholic and hexane extracts of D. kotschyi (10 and 20 mg/kg) also significantly inhibited the castor oil and MgSO4-induced diarrhoea in mice in comparison with the vehicle-treated control groups. This study confirms that both the hydroalcoholic and hexane extracts of D. kotschyi has antispasmodic and antidiarrhoeal properties in vivo and could be a suitable remedy for treatment of gastrointestinal disorders in which smooth muscle spasm and/or diarrhoea plays a significant roles

Antidiarrheal action of Zataria multiflora hydroalcoholic and hexane extracts in mice

Introduction: Zataria multiflora Boiss. is an indigenous herbal plant found in many parts of Iran. This herb is traditionally used as a remedy for treating gastrointestinal disorders including diarrhea. Despite the existence of few pharmacological evidences which support the antispasmodic action of Z. multiflora in vitro, there is no scientific report about therapeutic efficacy of Z. multiflora in animal models. The objective of this research was to investigate the antispasmodic activity of hydroalcoholic and hexane extracts of Z. multiflora on intestinal peristaltic movement as well as assessment of its antidiarrheal action in mice. Methods: Dried leafy branches of Z. multiflora were coarsely powdered and subjected to extraction by ethanol or hexane in a percolator apparatus. Antispasmodic activity of Z. multiflora in vivo was assessed by investigating effect of the extracts on intestinal charcoal meal transit. The antidiarrheal activity of Z. multiflora extracts was evaluated by castor oil and magnesium sulfate‑induced diarrhea. The inhibitory effects of the extracts were compared with the standard drug loperamide. Results: The antispasmodic activity of Z. multiflora (20 & 40 mg/kg) hydroalcoholic and hexane extracts was confirmed by a reduction in the distance traveled by charcoal meal alongside the small intestine. Z. multiflora extracts (20 & 40 mg/kg) also significantly attenuated the castor oil and magnesium sulfate‑induced diarrhea. Loperamide was more efficacious in reducing number of total stools in both models of diarrhea. Conclusion: The obtained results have established a pharmacological evidence for the folkloric use of the Z. multiflora as an antidiarrhoeal and spasmodic agent

Antispasmodic effect of hydroalcoholic and flavonoids extracts of Dracocephalum kotschyi on rabbit bladder

Introduction: Dracocephalum kotschyi extract has antispasmodic activities on smooth muscle including ileum, uterus and trachea. The objective of this research was to investigate antispasmodic activity of hydroalcoholic and flavonoids extracts of D. kotschyi on rabbit bladder contractions. Methods: Rabbits were euthanized by carbon dioxide asphyxiation and the whole bladder was dissected out and immersed in the Tyrode’s solution. Longitudinal bladder strips were mounted vertically in an organ bath at 37°C and gassed continuously with O2 . Bladder strips were contracted with acetylcholine (ACh), KCl, or electrical field stimulation (EFS). Isotonic tension of the tissue was recorded before and after addition of hydroalcoholic or flavonoids rich extracts of D. kotschyi. Nifedipine and propantheline were used as standard drugs. Results: Standard drug propantheline, prevented bladder phasic contraction induced by ACh (1µM) without affecting KCl response. On the other hand, cumulative addition of nifedipine attenuated the tonic contractions induced by KCl (20mM) on bladder smooth muscle. Hydroalcoholic and flavonoids extracts of D. kotschyi at concentration ranges of 10-320 µg/ mL in a concentration dependent way inhibited bladder tonic contraction induced by KCl (n=6). Both extracts also in a concentration-dependent manner relaxed EFS and ACh-induced contractions (range, 20–1280 µg/mL) of bladder smooth muscle in vitro. Complete inhibition was achieved with the highest used concentrations of the extracts. The inhibitory effect of the extract was reversible following washing the tissues with fresh Tyrode’s solution. Conclusion: This study clearly demonstrated that D. kotschyi extracts were able to prevent contractions induced by ACh, KCl or EFS in isolated rabbit bladder. This means that people consuming this medicinal plant may face urinary retention which could be a problem for patients with prostate hypertrophy. On the other hand, this plant might be useful in patients with urinary incontinence. However, its usefulness must be assessed in the controlled clinical trials