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      Antidiarrheal Action of Hydroalcoholic Extract of Pycnocycla spinosa in Comparison with Loperamide and Dicyclomine

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          Abstract

          Pycnocycla spinosa Decne. ex Boiss. var. spinosa (Fam. Umbelliferae) is an essential oil-containing wild plant growing in central part of Iran. Hydroalcoholic extract of Pycnocycla spinosa has antispasmodic and antidiarrheal activity. The aim of this study was to further investigate antidiarrheal and small intestinal transit effect of P. spinosa extract for a comparison with loperamide and dicyclomine.

          Male mice fasted over night with free access to water, were treated with P. spinosa extract, loperamide, dicyclomine or vehicle (p.o.). After thirty min, castor oil was given orally to the animals. In separate groups, magnesium sulphate was given in the beginning and 30 min after the extract or drugs were administered. The onset and number of wet defecation on the absorbent paper was recorded for each animal for 2.5 h. In another group of mice, intestinal transit of charcoal meal after the administration of extract, loperamide or dicyclomine was determined and compared with the control group.

          P. spinosa extract sharply reduced castor oil and magnesium sulphate induced diarrhea. The extract, in dose of 1 mg/Kg, had antidiarrheal effect similar to loperamide (2 mg/Kg) and with dose of 0.5 mg/Kg, its antidiarrheal action was greater than that of dicyclomine (5 mg/Kg). Unlike dicyclomine, P. spinosa extract significantly reduced the small intestinal transit of charcoal meal. However, its inhibitory effect on intestinal transit was less than loperamide.

          This study shows that anti-diarrhea l effect of P. spinosa extract is similar to loperamide. The inhibition of intestinal propulsion is a most likely mechanism that may account for anti-diarrhea l activity of the extract.

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          Most cited references17

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          Antispasmodic and anti-diarrhoeal effect of Satureja hortensis L. essential oil.

          Satureja hortensis L. (Lamiaceae) is an annual herb that is used in the traditional medicine of Iran for treating stomach and intestinal disorders. The antispasmodic activity of S. hortensis essential oil (SHEO) was assessed on contractions of isolated ileum, induced by KCl and acetylcholine, and compared with the effect of atropine and dicyclomine. SHEO inhibited the response to 80 mM KCl in a concentration-dependent manner (pD(2)=1.55+/-0.09 microg/ml; this is negative log concentration of SHEO causing 50% of maximum inhibition) and attenuating the maximum inducible response of acetylcholine concentration-response curve. Effect of SHEO on KCl was similar to that of dicyclomine. Dicyclomine (3.46 and 34.6 ng/ml) also reduced the response to acetylcholine on rat isolated ileum without altering the maximum response and shifted the acetylcholine concentration-response curve to the right by 16-fold at 34.6 ng/ml (100 nM) bath concentration, while atropine only inhibited the response to acetylcholine. This study shows that SHEO is a relaxant of rat isolated ileum. In addition to antispasmodic activity in vitro, essential oil of this plant at a dose of 0.1 ml/100 g inhibited castor oil induced diarrhoea in mice. As the inhibition of contractile overactivity of the ileum is the base of the treatment of some gastrointestinal disorders such as colic, SHEO may have clinical benefits for treatment of these conditions.
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            A dictionary of Iranian plant name.

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              Loperamide: blockade of calcium channels as a mechanism for antidiarrheal effects.

              The antidiarrheal opiates loperamide, fluperamide, diphenoxylate and fetoxylate inhibited binding of [3H]nitrendipine to membranes from guinea-pig cerebral cortex with Ki values of 0.5 to 10 microM. Loperamide and fluperamide reversed the tiapamil elicited lowering of [3H]nitrendipine binding with IC50 values of 0.2 to 0.5 microM, indicating a verapamil-like action of these drugs. An oral dose of 1 mg/kg of loperamide reduced gastrointestinal motility and gave concentrations of 0.45 +/- 0.19, 0.38 +/- 0.22 and 0.49 +/- 0.25 microM in the duodenum, jejunum and ileum, respectively. The apparent Ki for loperamide in preventing calcium-induced contractions of guinea-pig ileum depolarized with 80 mM potassium was 0.10 microM. We propose that calcium channel antagonism is responsible at least in part for the antidiarrheal actions of loperamide and related agents. Evidence includes the calcium antagonist actions of loperamide at antidiarrheal doses, the constipating effects of certain calcium antagonists and the failure of opiate antagonists to prevent some intestinal effects of loperamide.
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                Author and article information

                Journal
                Iran J Pharm Res
                Iran J Pharm Res
                IJPR
                Iranian Journal of Pharmaceutical Research : IJPR
                Shaheed Beheshti University of Medical Sciences (Tehran, Iran )
                1735-0328
                1726-6890
                Autumn 2011
                : 10
                : 4
                : 835-841
                Affiliations
                [a ] Department of Pharmacology, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran.
                [b ] Isfahan Pharmaceutical Sciences Research Center, Isfahan University of Medical Sciences, Isfahan, Iran.
                Author notes
                [* ]Corresponding author: E-mail: hsadraei@yahoo.com
                Article
                ijpr-10-835
                3813056
                24250420
                ffc00288-cef2-47db-9fa3-716a0810d942
                © 2011 by School of Pharmacy, Shaheed Beheshti University of Medical Sciences and Health Services

                This is an Open Access article distributed under the terms of the Creative Commons Attribution License, ( http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : June 2010
                : December 2010
                Categories
                Original Article

                antidiarrheal,extract,pycnocycla spinosa,anti-spasm,intestine

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