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|Title: ||Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one|
|Authors: ||Harley, B. K.|
Amponsah, I. K.
Ben, I. O.
Adongo, D. W.
Mireku-Gyimah, N. A.
Baah, M. K.
Mensah, A. Y.
Fleischer, T. C.
|Keywords: ||Glucose uptake|
|Issue Date: ||Feb-2021|
|Citation: ||Amponsah, I.K., Boakye, A., Orman, E., Armah, F.A., Harley, B.K., Amponsah, I.K., Ben, I.O., Adongo, D.W., Mireku-Gyimah, N.A., Baah, M.K., Mensah, A.Y. and Fleischer, T.C. (2021). Myrianthus libericus: Possible mechanisms of hypoglycaemic action and in silico prediction of pharmacokinetics and toxicity profile of its bioactive metabolite, friedelan-3-one. Biomedicine & Pharmacotherapy, 137, p.111379, 8(3), p.e09150. https://doi.org/10.1016/j.biopha.2021.111379|
|Abstract: ||The hypoglycaemic and anti-hyperlipidaemic effects of the 70% ethanol stem bark extract of Myrianthus libericus
(MLB), used traditionally in the management of diabetes in Ghana, was evaluated in this study using streptozotocin (45 mg/kg)-induced diabetic rats. In vitro hypoglycaemic activities of the extract and one of its principal
compounds, friedelan-3-one were then investigated using α-amylase inhibitory and glucose uptake assay in
C2C12 myotubes. In silico analysis of the pharmacokinetic and toxicity properties of the compound was also
performed. MLB significantly (p < 0.001) reduced the elevated blood glucose levels and corrected considerably
(p < 0.01) the altered serum lipid profiles of the diabetic rats which was comparable to glibenclamide (5 mg/kg).
Together with friedelan-3-one, the extract markedly inhibited the activity of α-amylase and promoted glucose
uptake in C2C12 cells. Whereas MLB significantly (p < 0.001) up-regulated PI3K and PPARγ transcripts with a
corresponding increase in GLUT-4 transcripts within the muscle cells, friedelan-3-one only up-regulated PI3K and
GLUT-4 transcripts to promote glucose transport. Friedelan-3-one was shown to be non-carcinogenic, non-hepatotoxic, has decent oral bioavailability and a good compound for optimisation into a drug candidate. The study
has demonstrated that MLB possess hypoglycaemic and anti-hyperlipidaemic activities and could be used as a
therapeutic agent in the management of diabetes mellitus.|
|Appears in Collections:||College of Health Sciences|
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