4.4 Article

Giganteone A and malabaricone C as potential pharmacotherapy for diabetes mellitus

Journal

NATURAL PRODUCT RESEARCH
Volume 36, Issue 6, Pages 1581-1586

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1080/14786419.2021.1885405

Keywords

Myristica cinnamomea King; giganteone A; malabaricone C; malabaricone E; α -glucosidase inhibitory activity

Funding

  1. Ministry of Higher Education, Malaysia [FP002-2018A]
  2. University of Malaya [RP001-2012, BK002-2015]

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Malabaricone C and Giganteone A show potential as antidiabetic agents by controlling glycemic levels, inhibiting oxidative stress, and acting as potent alpha-glucosidase inhibitors.
The use of antidiabetic agents which control glycemic levels in the blood and simultaneously inhibit oxidative stress is an important strategy in the prevention of Diabetes Mellitus and its complications. In our previous study, malabaricone C (3) and its dimer, giganteone A (5) exhibited significant DPPH free radical scavenging activities which were lower than the activity of the positive control, ascorbic acid. These compounds were evaluated for their alpha-glucosidase inhibitory activities at different concentrations (0.02-2.5 mM) in the present study. Compounds 3 (IC50 59.61 mu M) and 5 (IC50 39.52 mu M) were identified as active alpha-glucosidase inhibitors, each respectively being 24 and 37 folds more potent than the standard inhibitor, acarbose. Based on the molecular docking studies, compounds 3 and 5 docked into the active site of the alpha-glucosidase enzyme, forming mainly hydrogen bonds in the active site.

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