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Macrocarpal C isolated from Eucalyptus globulus inhibits dipeptidyl peptidase 4 in an aggregated form.

Authors
  • Kato, Eisuke1
  • Kawakami, Kazuhiro1
  • Kawabata, Jun1
  • 1 a Laboratory of Food Biochemistry, Division of Applied Bioscience, Graduate School of Agriculture , Hokkaido University , Kita-ku , Hokkaido , Japan Sapporo. , (Japan)
Type
Published Article
Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
Publisher
Informa UK (Taylor & Francis)
Publication Date
Dec 01, 2018
Volume
33
Issue
1
Pages
106–109
Identifiers
DOI: 10.1080/14756366.2017.1396458
PMID: 29148282
Source
Medline
Keywords
License
Unknown

Abstract

Dipeptidyl peptidase 4 (DPP-4) inhibitors are used for the treatment of type-2 diabetes mellitus. Various synthetic inhibitors have been developed to date, and plants containing natural DPP-4 inhibitors have also been identified. Here, 13 plant samples were tested for their DPP-4 inhibitory activity. Macrocarpals A-C were isolated from Eucalyptus globulus through activity-guided fractionation and shown to be DPP-4 inhibitors. Of these, macrocarpal C showed the highest inhibitory activity, demonstrating an inhibition curve characterised by a pronounced increase in activity within a narrow concentration range. Evaluation of macrocarpal C solution by turbidity, nuclear magnetic resonance spectroscopy and mass spectrometry indicated its aggregation, which may explain the characteristics of the inhibition curve. These findings will be valuable for further study of potential small molecule DPP-4 inhibitors.

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