Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens
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Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens. / Malik, Abd.; Ardalani, Hamidreza; Anam, Syariful; McNair, Laura M.; Kromphardt, Kresten Jon Korup; Frandsen, Rasmus John Normand; Franzyk, Henrik; Stærk, Dan; Kongstad, Kenneth Thermann.
I: Fitoterapia, Bind 142, 104522, 2020.Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt
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T1 - Antidiabetic xanthones with α-glucosidase inhibitory activities from an endophytic Penicillium canescens
AU - Malik, Abd.
AU - Ardalani, Hamidreza
AU - Anam, Syariful
AU - McNair, Laura M.
AU - Kromphardt, Kresten Jon Korup
AU - Frandsen, Rasmus John Normand
AU - Franzyk, Henrik
AU - Stærk, Dan
AU - Kongstad, Kenneth Thermann
PY - 2020
Y1 - 2020
N2 - 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
AB - 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
U2 - 10.1016/j.fitote.2020.104522
DO - 10.1016/j.fitote.2020.104522
M3 - Journal article
C2 - 32088281
VL - 142
JO - Fitoterapia
JF - Fitoterapia
SN - 1971-551X
M1 - 104522
ER -
ID: 236272644