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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 C2C12 cells Hypoglycaemic effect α-amylase inhibition Friedelan-3-one Myrianthus libericus |
Issue Date: | Feb-2021 |
Publisher: | Elsevier |
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. |
URI: | http://hdl.handle.net/123456789/15953 |
Appears in Collections: | College of Health Sciences
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