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Calotropis procera, a multipurpose plant that is native to Asia and Africa has been reported to possess remedies for several temperate and tropical ailments. The use oits leaf for management of diabetes mellitus is popular among Nigerian populace, but investigation into its fraction which actually possesses the antidiabetic property is unavailable. Thus, fractionation and bioactivity of aqueous extract of Calotropis procera leaf was carried out in the present study. The mean values of results showed that five (05) different fractions (F1 – F5) were obtained from the fractionation. Volatile oils constituted 60% of the crude extract fractions followed by alkaloids (10%), phenols (10%), saponins (10%) and glycosides (10%). The in-vivo toxicity study of the extract showed tha there were no extract-related moralities and pathological signs such as visual observations for behavioural pattern (restlessness, respiratory, distress, diarrhoea, convulsion, salivation, lethargy and sleep), changes in physical appearance, fur, injury, pain, and signs of illness in the normal rats administered different doses (25 mg/kg, 50 mg/kg and 100 mg/kg body weights) of the extract of throughout the period of the treatment. The experimental animals administered the fractions generally and significantly showed increase (at P>0.05) in body weight. Alloxan induction significantly increased (at P>0.05) the blood glucose level of the experimental animals while the fractions mostly the volatile oil fraction also significantly decreased (at P>0.05) the blood glucose level of the animals. The volatile oil fraction appeared to possess the most active principle(s) against hyperglycemia and eventual diabetes mellitus. Systemically, the animals administered the fractions were pharmaco-kinetic and pharmaco-dynamic stable. Therefore, an in-depth research work on the toxicity of the fractions is hereby recommended.
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