4.6 Article

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

期刊

MOLECULES
卷 27, 期 8, 页码 -

出版社

MDPI
DOI: 10.3390/molecules27082574

关键词

Garcinia schomburgakiana; schomburgkianone I; benzoylphloroglucinol; alpha-glucosidase inhibition; antimicrobial inhibition; molecular docking model

资金

  1. Thailand Science Research and Innovation Fundamental Fund
  2. Thammasat University Research Fund [TUFT-FF11/2565]

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The novel compound schomburgkianone I and the reported compound guttiferone K exhibited potent inhibition against alpha-glucosidase and showed strong antibacterial activity. These compounds are potential candidates for diabetes treatment.
alpha-Glucosidase plays a role in hydrolyzing complex carbohydrates into glucose, which is easily absorbed, causing postprandial hyperglycemia. Inhibition of oc-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 alpha-glucosidase inhibition (IC50s of 21.2 and 34.8 mu M, 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 mu g/mL. The MIC value of compound 1 against S. aureus was 13.32 mu M. An in silico molecular docking model suggested that both compounds are potent inhibitors of enzyme alpha-glucosidase and are therefore leading candidates as therapies for diabetes mellitus.

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