title: Antidiarrheal and Antispasmodic Activities of Buddleja polystachya are Mediated Through Dual Inhibition of Ca(++) Influx and Phosphodiesterase Enzyme.
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.
authors.affiliation: Natural Products Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, 74800, Pakistan.|Department of Pharmacy, College of Health Sciences, Mekelle University, Mekelle, Ethiopia.
authors.forename: Najeeb-ur
authors.initials: NU
authors.lastname: Rehman
authors.affiliation: Natural Products Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, 74800, Pakistan.|Department of Pharmacy, College of Health Sciences, Mekelle University, Mekelle, Ethiopia.
authors.forename: Anwarul-Hassan
authors.initials: AH
authors.lastname: Gilani
authors.affiliation: Natural Products Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, 74800, Pakistan.|Department of Pharmacology, Institute of Basic Medical Sciences, Khyber Medical University, Peshawar, Pakistan.
authors.forename: Aslam
authors.initials: A
authors.lastname: Khan
authors.affiliation: Natural Products Research Division, Department of Biological and Biomedical Sciences, The Aga Khan University Medical College, Karachi, 74800, Pakistan.
authors.forename: Maryam
authors.initials: M
authors.lastname: Nazneen
authors.affiliation: Pharmacognosy Department, College of Pharmacy, King Saud University, P.O. Box 22452, Riyadh, 11495, Saudi Arabia.|Pharmacognosy Department, College of Pharmacy, University of Mansoura, Mansoura, 35516, Egypt.
authors.forename: Ali A
authors.initials: AA
authors.lastname: El Gamal
authors.affiliation: Pharmacognosy Department, College of Pharmacy, King Saud University, P.O. Box 22452, Riyadh, 11495, Saudi Arabia.|Pharmacognosy Department, College of Pharmacy, Cairo University, Cairo, 11562, Egypt.
authors.forename: Ghada A
authors.initials: GA
authors.lastname: Fawzy
authors.affiliation: Pharmacognosy Department, College of Pharmacy, King Saud University, P.O. Box 22452, Riyadh, 11495, Saudi Arabia.
authors.forename: Hanan Y
authors.initials: HY
authors.lastname: Al-Ati
authors.affiliation: Department of Pharmacognosy, College of Pharmacy, Salman Bin Abdulaziz University, Alkharj, Saudi Arabia.
authors.forename: Maged S
authors.initials: MS
authors.lastname: Abdel-kader
mesh_terms: D000818:Animals; D000930:Antidiarrheals / Q000494:pharmacology*; D032861:Buddleja / Q000737:chemistry*; D002118:Calcium / Q000378:metabolism*; D002368:Castor Oil / Q000009:adverse effects; D003967:Diarrhea / Q000188:drug therapy; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007583:Jejunum / Q000187:drug effects; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D010276:Parasympatholytics / Q000494:pharmacology*; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism; D035261:Plant Components, Aerial / Q000737:chemistry; D010936:Plant Extracts / Q000494:pharmacology*; D011817:Rabbits; D014700:Verapamil / Q000494:pharmacology
chemical_list: D000930:Antidiarrheals; D010276:Parasympatholytics; D010726:Phosphodiesterase Inhibitors; D010936:Plant Extracts; D002368:Castor Oil; D014700:Verapamil; D010727:Phosphoric Diester Hydrolases; D002118:Calcium
keywords: Buddleja polystachya; Ca++ antagonist; antidiarrheal; phosphodiesterase inhibition; spasmolytic