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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.