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VOLTAGE-DEPENDENT Ca2+ ENTRY BLOCKING ACTIVITY OF HEDERA HELIX LEAF EXTRACT EXPLAINS ITS MEDICINAL USE IN HYPERACTIVE GUT DISORDERS

ABDUL JABBAR SHAH 1*, MUNASIB KHAN 2, MANZOOR AHMAD 3, HASSAN SHER 4

1.Department of Pharmacy, COMSATS Institute of Information Technology, University Road, Abbottabad, Pakistan
2 .Department of Pharmacy, Malakand University, Dir (lower), KPK, Pakistan
3 .Department of Chemistry, University of Malakand, Dir (Lower), KhyberPukhtunkhwa, Pakistan
4 .Institute of Plant Sciences and Biodiversity, University of Swat, Swat, KhyberPukhtunkhwa, Pakistan
*corresponding author: jabbarshah@ciit.net.pk

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Hedera helix L. (Araliaceae Family) has traditional reputation in gastrointestinal disorders, such as diarrhoea and spasms. This work investigated the pharmacological base of H. helix leaves in these disorders. In a castor oil-induced diarrhoeal model in mice, the aqueous methanolic extract from Hedera helix leaves (Hh.Cr), has provided 18 - 84% protection, similar to verapamil. In isolated rabbit jejunum preparations, Hh.Cr was found more potent against high K+ pre-contractions than spontaneous, similar to verapamil. This suggests that Hh.Cr mediates this effect through possible voltage-dependent Ca2+ channel blockade. This hypothesis was further strengthened when pre-incubation of the intestinal tissue with Hh.Cr (0.3 - 3 mg/mL) caused a rightward shift in the Ca2+ concentration-response curves, similar to verapamil. The extract was found safe in mice (5 g/kg). Hh.Cr possesses antidiarrheal and spasmolytic effects, mediated, possibly, through voltage-dependent Ca2+ entry blockade and provides pharmacological reasons for its medicinal use in diarrhoea and spasm.