Inhibitory activity of minor phlorotannins from Ecklonia cava on α-glucosidase

Sae Rom Park, Jang Hoon Kim, Hae Dong Jang, Seo Young Yang, Young Ho Kim

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56 Scopus citations

Abstract

α-Glucosidase is an enzyme that plays a key role in raising blood sugar level and is considered a good target for developing drugs to treat type 2 diabetes. This study was performed to evaluate the inhibition of the catalytic reaction of α-glucosidase by minor phlorotannin derivatives (1–5) from Ecklonia cava. These derivatives demonstrated inhibitory activity, with IC50 values ranging from 2.3 ± 0.1 to 59.8 ± 0.8 μM. Among the phlorotannins identified, compounds 2 and 3–5 were revealed to be non-competitive and competitive inhibitors, respectively. Furthermore, a fluorescence-quenching study of receptor–ligand binding was performed to calculate the kinetic parameters (Ksv, Kq, and K). These signal data indicated a 1:1 ratio of ligand–receptor binding. The binding conformations of the phlorotannin ligands were visually solved through molecular simulation. In conclusion, these minor phlorotannins may serve as α-glucosidase inhibitors targeted for the treatment of type 2 diabetes.

Original languageEnglish
Pages (from-to)128-134
Number of pages7
JournalFood Chemistry
Volume257
DOIs
StatePublished - 15 Aug 2018

Keywords

  • Ecklonia cava
  • Fluorescence quenching
  • Laminariaceae
  • Molecular docking
  • Phlorotannin
  • α-Glucosidase inhibitor

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