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

Huy Truong Nguyen, Thanh-Trung Nguyen, Thuc‐Huy Duong, Tran Nguyen Minh An, Chuong Hoang Nguyen, Thi-Hong-Anh Nguyen, Jirapast Sichaem

2022Molecules22 citationsDOIOpen Access PDF

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.

Topics & Concepts

AcarboseIn silicoChemistryAntimicrobialPostprandialStaphylococcus aureusIn vitroEnzymeStereochemistryPositive controlBiochemistryTraditional medicineBiologyBacteriaDiabetes mellitusMedicineOrganic chemistryGeneticsGeneEndocrinologyNatural Compound Pharmacology StudiesCarbohydrate Chemistry and SynthesisNatural Antidiabetic Agents Studies
α-Glucosidase Inhibitory and Antimicrobial Benzoylphloroglucinols from Garcinia schomburgakiana Fruits: In Vitro and In Silico Studies | Litcius