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Antidiarrheal and Antispasmodic Activities of Buddleja polystachya are Mediated Through Dual Inhibition of Ca++ Influx and Phosphodiesterase Enzyme
Authors:Najeeb‐ur Rehman  Anwarul‐Hassan Gilani  Aslam Khan  Maryam Nazneen  Ali A El Gamal  Ghada A Fawzy  Hanan Y Al‐Ati  Maged S Abdel‐kader
Institution:1. Natural Products Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, Pakistan;2. Department of Pharmacy, College of Health Sciences, Mekelle University, Mekelle, Ethiopia;3. Department of Pharmacology, Institute of Basic Medical Sciences, Khyber Medical University, Peshawar, Pakistan;4. Pharmacognosy Department, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia;5. Pharmacognosy Department, College of Pharmacy, University of Mansoura, Mansoura, Egypt;6. Pharmacognosy Department, College of Pharmacy, Cairo University, Cairo, Egypt;7. Department of Pharmacognosy, College of Pharmacy, Salman Bin Abdulaziz University, Alkharj, Saudi Arabia
Abstract:This study describes the antidiarrheal and antispasmodic activities of the hydro‐alcoholic extract of Buddleja polystachya (Bp.Cr) with possible mode of action explored along with activity‐directed fractionation. Bp.Cr and its aqueous (Bp.Aq) and organic fractions, petroleum ether (Bp.Pet), dichloromethane (Bp.DCM), ethylacetate (Bp.EtAc) and butanol (Bp.But), were tested using the in‐vivo and in‐vitro assays. The crude extract (100–300 mg/kg) showed 20 and 60% protection of castor oil‐induced diarrhea in mice. In isolated rabbit jejunum, Bp.Cr like papaverine inhibited spontaneous and high K+ (80 mM)‐induced contractions equi‐potently. In guinea‐pig ileum, Bp.Cr showed a moderate spasmogenic effect. The activity‐directed fractionation revealed that the spasmolytic activity was concentrated in the organic fractions and spasmogenic component in the aqueous fraction. Amongst the organic fractions, BP.DCM and Bp.Pet inhibited spontaneous and high K+‐induced contractions equi‐potently, while Bp.But, like verapamil was more potent against high K+. The crude extract and its organic fractions caused rightward shift in the Ca++‐concentration response curves (CRCs), similar to verapamil, and all except Bp.But potentiated the isoprenaline‐inhibitory CRCs to the left, similar to papaverine. The results of this study indicate that the crude extract of B. polystachya possesses antidiarrheal and antispasmodic activities, mediated possibly through dual inhibition of Ca++ influx and phospodiesterase enzyme. Copyright © 2015 John Wiley & Sons, Ltd.
Keywords:Buddleja polystachya  antidiarrheal  spasmolytic  Ca++ antagonist  phosphodiesterase inhibition
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