Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens

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  • Abd Malik, University of Copenhagen, Faculty of Health Sciences, Universitas Muslim Indonesia
  • ,
  • Hamidreza Ardalani
  • Syariful Anam, University of Copenhagen, Faculty of Health Sciences, Tadulako University
  • ,
  • Laura Mikél McNair, University of Copenhagen, Faculty of Health Sciences
  • ,
  • Kresten J.K. Kromphardt, Technical University of Denmark
  • ,
  • Rasmus John Normand Frandsen, Technical University of Denmark
  • ,
  • Henrik Franzyk, University of Copenhagen, Faculty of Health Sciences
  • ,
  • Dan Staerk, University of Copenhagen, Faculty of Health Sciences
  • ,
  • Kenneth T. Kongstad, University of Copenhagen, Faculty of Health Sciences

Worldwide, 463 million people are affected by diabetes of which the majority is diagnosed with Type 2 Diabetes (T2D). T2D can ultimately lead to retinopathy, nephropathy, nerve damage, and amputation of the lower extremities. α-Glucosidase, responsible for converting starch to monosaccharides, is a key therapeutic target for the management of T2D. However, due to substantial side effects of currently marketed drugs, there is an urgent need for the discovery of new α-glucosidase inhibitors. In our ongoing efforts to identify novel α-glucosidase inhibitors from Nature, we are investigating the potential of endophytic filamentous fungi as sustainable sources of hits and/or leads for future antihyperglycemic drugs. Here we report one previously unreported xanthone (5) and two known xanthones (7 and 11) as α-glucosidase inhibitors, isolated from an endophytic Penicillium canescens, recovered from fruits of Juniperus polycarpos. The three xanthones 5, 7, and 11 showed inhibitory activities against α-glucosidase with IC50 values of 38.80 ± 1.01 μM, 32.32 ± 1.01 μM, and 75.20 ± 1.02 μM, respectively. Further pharmacological characterization revealed a mixed-mode inhibition for 5, a competitive inhibition for 7, while 11 acted as a non-competitive inhibitor.

Original languageEnglish
Article number104522
JournalFitoterapia
Volume142
ISSN0367-326X
DOIs
Publication statusPublished - Apr 2020
Externally publishedYes

    Research areas

  • Competitive inhibition, Endophytic fungi, Penicillium canescens, Type 2 diabetes, Xanthone, α-Glucosidase inhibitors

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