Abstract
EFFECTS OF ARTESUNATE ON CONTRACTILITY TO DRUGS AND OTHER ACTIVITIES OF THE SMOOTH MUSCLE PREPARATIONS.

*Tologbonse A. A., Unekwe P. C., Essien G. E., Abu J. M., Mbagwu H.O.C, Hillary E.O. and Udoh M. N.

ABSTRACT

This study was aimed at evaluating the effect and safety profile of artesunate on drugs induced contractility in different isolated smooth muscle preparations in guinea pigs and mice using in vitro andin vivo experimental procedures/ standard protocols in an organ bath set up. Artesunate (4.0 x 10 - 6 - 4.0 x 10 – 3mg/ml) when applied alone and separately excited marked variable effects on guinea pig ileum and mouse rectum. In some preparation it showed no response, while in others it produced slight phasic contraction when external calcium (Ca2+) ion was introduced. The slight phasic contractile activity was abolished by verapamil (5x10-3mg/ml). artesunate (4.0 x 10 - 6 - 4.0 x 10 – 5) caused marked significant induced contraction – dependent inhibition of acetylcholine, potassium chloride and histamine in depolarizing tyrode solution (p< 0.05). The Inhibitory response maxima of artesunate on acetylcholine induced contraction is relatively moderate when compared to the inhibitory effect of atropine (10-5 M). Subacute toxicity study of oral administration of artesunate (2.0, 2.5, and 5mg/kg b.w), twice daily for 3 days in Plasmodium bergheiberghei infected mice revealed a normal cellular profile of smooth muscle structure. The result shows that artesunate seems to act via non-specific receptor mechanism, with appreciable calcium channel blocking activity and it is safe at therapeutic doses.

Keywords: Artesunate, Contractility, Smooth muscle, Plasmodium bergheiberghei, and toxic.


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