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α-Glucosidase inhibitory effect of sulochrin from aspergillusterreus and itsbrominated derivatives
Dewi, Rizna Triana1, Darmawan, Akhmad2, Mulyani, Hani3, Lotulung, Puspa Dewi N4, Minarti5, Megawati6.
Use of α-glucosidase inhibitorsisone of the therapeutic approaches for decreasing postprandial hyperglycemia. Sulochrin (1) from Aspergillusterreusas well as twosynthetic sulochrinderivatives were assessed for antidiabeticactivity against yeast and rat intestine α-glucosidase. Sulochrin showed potential inhibition against yeast α-glucosidase, through a non-competitivemode with an IC50value of 133.79 μM, and rat intestineα-glucosidase by uncompetitive mode with an IC50value of 144.59 μM.. Twosynthetic derivatives of sulochrinwere also preparedby brominationwhich resultedindibromo-sulochrin(2) and tribromo-sulochrin(3). Preliminary SAR studies of sulochrinderivatives revealed that the yeast α-glucosidase inhibitory activity of compound 2and 3increased than 1due to substitution of hydrogen atom with bromine with IC50values of 122.65 and 49.08 μM, respectively.However, the inhibitory activity against rat intestine α-glucosidase of 2and 3wasdecreased comparedto 1.To the best our knowledge, this is the first report of structure-activity relationship of sulochrinand its derivatives as α-glucosidase inhibitors. These results suggested that sulochrincan potentiallybe used as a lead compound to develop new α-glucosidase inhibitorfrom microorganisms.
Affiliation:
- Indonesian Institute of Sciences, Indonesia
- Indonesian Institute of Sciences, Indonesia
- Indonesian Institute of Sciences, Indonesia
- Indonesian Institute of Sciences, Indonesia
- Indonesian Institute of Sciences, Indonesia
- Indonesian Institute of Sciences, Indonesia
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Indexed by |
MyJurnal (2019) |
H-Index
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0 |
Immediacy Index
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0.000 |
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0 |
Indexed by |
Scopus (SCImago Journal Rankings 2016) |
Impact Factor
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- |
Rank |
Q4 (Multidisciplinary) |
Additional Information |
0.108 (SJR) |
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