TY - JOUR
T1 - Pharmacological basis for the medicinal use of Holarrhena antidysenterica in gut motility disorders
AU - Gilani, Anwarul Hassan
AU - Khan, Aslam
AU - Khan, Arif Ullah
AU - Bashir, Samra
AU - Rehman, Najeeb Ur
AU - Mandukhail, Saf Ur Rehman
N1 - Funding Information:
This study was supported by the Higher Education Commission of Pakistan, as indigenous M.Phil/PhD scholarship awarded to Aslam Khan.
PY - 2010/11
Y1 - 2010/11
N2 - 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 0.3-10mg/mL caused pyrilamine-sensitive spasmogenic effect. When tested in spontaneously contracting rabbit jejunum preparations, HaCE (0.01-3.0mg/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 (0.01-0.3mg/mL). HaCE inhibited the high K+ (80mM)-induced contractions at concentration range of 0.01-1.0mg/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.
AB - 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 0.3-10mg/mL caused pyrilamine-sensitive spasmogenic effect. When tested in spontaneously contracting rabbit jejunum preparations, HaCE (0.01-3.0mg/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 (0.01-0.3mg/mL). HaCE inhibited the high K+ (80mM)-induced contractions at concentration range of 0.01-1.0mg/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.
KW - Ca antagonist
KW - Constipation
KW - Diarrhea
KW - Histaminergic
KW - Holarrhena antidysenterica
KW - Spasmogenic
KW - Spasmolytic
UR - http://www.scopus.com/inward/record.url?scp=78049480495&partnerID=8YFLogxK
U2 - 10.3109/13880201003727960
DO - 10.3109/13880201003727960
M3 - Article
C2 - 20822397
AN - SCOPUS:78049480495
SN - 1388-0209
VL - 48
SP - 1240
EP - 1246
JO - Pharmaceutical Biology
JF - Pharmaceutical Biology
IS - 11
ER -