Journal
FITOTERAPIA
Volume 142, Issue -, Pages -Publisher
ELSEVIER
DOI: 10.1016/j.fitote.2020.104522
Keywords
Type 2 diabetes; Endophytic fungi; Penicillium canescens; alpha-Glucosidase inhibitors; Xanthone; Competitive inhibition
Categories
Funding
- Apotekerfonden af 1991
- Carlsberg Foundation
- Danish Agency for Science, Technology, and Innovation via the National Research Infrastructure funds
- Lembaga Pengelola Dana Pendidikan (LPDP), Ministry of Finance, Republic of Indonesia, through the BUDI-LN scholarship program 2016
- Danish National Research Foundation [DNRF137]
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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. alpha-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 a-glucosidase inhibitors. In our ongoing efforts to identify novel alpha-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 alpha-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 alpha-glucosidase with IC50 values of 38.80 +/- 1.01 mu M, 32.32 +/- 1.01 mu M, and 75.20 +/- 1.02 mu M, respectively. Further pharmacological characterization revealed a mixed-mode inhibition for 5, a competitive inhibition for 7, while 11 acted as a non-competitive inhibitor.
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