An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i>
Background: <i>Ganoderma</i> fungus is rich in terpenoids. These compounds are known for their anti-hyperglycemic activities. However, the study of terpenoids as the secondary metabolite from <i>Ganoderma</i> as a dipeptidyl peptidase-4 (DPP-4) inhibitor remains unexplored. I...
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| Main Authors: | , , , , |
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| Format: | Book |
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MDPI AG,
2019-08-01T00:00:00Z.
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| Summary: | Background: <i>Ganoderma</i> fungus is rich in terpenoids. These compounds are known for their anti-hyperglycemic activities. However, the study of terpenoids as the secondary metabolite from <i>Ganoderma</i> as a dipeptidyl peptidase-4 (DPP-4) inhibitor remains unexplored. In addition, we examined the α-glucosidase inhibition activity. Objective: This study aimed to isolate the major terpenoid from non-laccate <i>Ganoderma</i> and examined its inhibitor activity on DPP-4 and α-glucosidase enzymes, and its interaction. Methods: The compound was isolated using column chromatography from <i>Ganoderma australe</i>. The structure of the isolated compound was confirmed by <sup>1</sup>H and <sup>13</sup>C nuclear magnetic resonance spectroscopy, while the inhibitory activity was evaluated using an enzymatic assay. The interaction of the isolated compound with DPP-4 and α-glucosidase enzymes was investigated using an in silico study. Results: The isolated compound was identified as stellasterol; IC<sub>50</sub> values for DPP-4 and α-glucosidase inhibitor were 427.39 µM and 314.54 µM, respectively. This study revealed that the inhibitory effect of stellasterol on DPP-4 enzyme is through hydrophobic interaction, while the α-glucosidase enzyme is due to the interaction with six amino acids of the enzyme. Conclusion: Stellasterol is the major component of the steroid from <i>G. australe</i>. Enzyme inhibitory assay and in silico study suggest that stellasterol may contribute antidiabetic activity with a mechanism closer to acarbose rather than to sitagliptin. |
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| Item Description: | 2218-0532 10.3390/scipharm87030021 |