Pharmacological basis for the medicinal use of Holarrhena antidysenterica in gut motility disorders

Author： Gilani Anwarul Hassan Khan Aslam Khan Arif-ullah Bashir Samra Rehman Najeeb-ur Mandukhail Saf-ur-Rehman

ISSN： 1388-0209

Source： Pharmaceutical Biology (Formerly International Journal of Pharmacognosy), Vol.48, Iss.11, 2010-11, pp. : 1240-1246

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Abstract

Context: Holarrhena antidysenterica Wall. (Apocynaceae) is widely used in traditional medical system for treatment of constipation, colic, and diarrhea.Aim: This study was carried out to provide pharmacological basis for medicinal use of Holarrhena antidysenterica in gastrointestinal disorders.Materials and methods: Hydro-ethanolic crude extract of Holarrhena antidysenterica (HaCE) and its fractions were studied in various gastrointestinal isolated tissue preparations.Results: In guinea pig ileum tissues, HaCE at 0.3-10 mg/mL caused pyrilamine-sensitive spasmogenic effect. When tested in spontaneously contracting rabbit jejunum preparations, HaCE (0.01-3.0 mg/mL) caused moderate stimulation, followed by a relaxant effect at next higher concentrations. In presence of pyrilamine, the contractile effect was blocked and the relaxation was observed at lower concentrations (0.01-0.3 mg/mL). HaCE inhibited the high K⁺ (80 mM)-induced contractions at concentration range of 0.01-1.0 mg/mL and shifted Ca⁺⁺ concentration response curves to the right, like that caused by verapamil. Activity-directed fractionation revealed that the spasmogenic component was concentrated in the aqueous fraction, while the spasmolytic component was concentrated in the organic fraction.Discussion and conclusion: These results indicate that the gut stimulant and relaxant activities of Holarrhena antidysenterica are mediated possibly through activation of histamine receptors and Ca⁺⁺ channel blockade, respectively and this study provides sound mechanistic background for its usefulness in gut motility disorders such as constipation, colic, and possibly diarrhea.