α-Glucosidase Inhibitory and Antimicrobial Benzoylphloroglucinols from Garcinia schomburgakiana Fruits: In Vitro and In Silico Studies

Molecules. 2022 Apr 15;27(8):2574. doi: 10.3390/molecules27082574.

Abstract

α-Glucosidase plays a role in hydrolyzing complex carbohydrates into glucose, which is easily absorbed, causing postprandial hyperglycemia. Inhibition of α-glucosidase is therefore an ideal approach to preventing this condition. A novel polyprenylated benzoylphloroglucinol, which we named schomburgkianone I (1), was isolated from the fruit of Garcinia schomburgkiana, along with an already-reported compound, guttiferone K (2). The structures of the two compounds were determined using NMR and HRESIMS analysis, and comparisons were made with previous studies. Compounds 1 and 2 exhibited potent α-glucosidase inhibition (IC50s of 21.2 and 34.8 µM, respectively), outperforming the acarbose positive control. Compound 1 produced wide zones of inhibition against Staphylococcus aureus and Enterococcus faecium (of 21 and 20 mm, respectively), compared with the 19 and 20 mm zones of compound 2, at a concentration of 50 µg/mL. The MIC value of compound 1 against S. aureus was 13.32 µM. An in silico molecular docking model suggested that both compounds are potent inhibitors of enzyme α-glucosidase and are therefore leading candidates as therapies for diabetes mellitus.

Keywords: Garcinia schomburgakiana; antimicrobial inhibition; benzoylphloroglucinol; molecular docking model; schomburgkianone I; α-glucosidase inhibition.

MeSH terms

  • Anti-Infective Agents*
  • Fruit
  • Garcinia* / chemistry
  • Glycoside Hydrolase Inhibitors / chemistry
  • Molecular Docking Simulation
  • Staphylococcus aureus
  • alpha-Glucosidases

Substances

  • Anti-Infective Agents
  • Glycoside Hydrolase Inhibitors
  • alpha-Glucosidases