Login / Signup

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

Huy Truong NguyenThanh-Trung NguyenThuc-Huy DuongTran Nguyen Minh AnChuong Hoang NguyenThi-Hong-Anh NguyenJirapast Sichaem
Published in: Molecules (Basel, Switzerland) (2022)
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 (IC 50s 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.
Keyphrases
  • molecular docking
  • staphylococcus aureus
  • molecular dynamics simulations
  • high resolution
  • magnetic resonance
  • biofilm formation
  • case control
  • oxidative stress
  • mass spectrometry