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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MDPI AG
2019-08-01
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| Series: | Scientia Pharmaceutica |
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| Online Access: | https://www.mdpi.com/2218-0532/87/3/21 |
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| author | Krisyanti Budipramana Junaidin Junaidin Komar Ruslan Wirasutisna Yanatra Budi Pramana Sukrasno Sukrasno |
| author_facet | Krisyanti Budipramana Junaidin Junaidin Komar Ruslan Wirasutisna Yanatra Budi Pramana Sukrasno Sukrasno |
| author_sort | Krisyanti Budipramana |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-04-11T22:23:00Z |
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| id | doaj.art-8b11c8b8c3f04a6f998deb27b48eba93 |
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| issn | 2218-0532 |
| language | English |
| last_indexed | 2024-04-11T22:23:00Z |
| publishDate | 2019-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Scientia Pharmaceutica |
| spelling | doaj.art-8b11c8b8c3f04a6f998deb27b48eba932022-12-22T03:59:59ZengMDPI AGScientia Pharmaceutica2218-05322019-08-018732110.3390/scipharm87030021scipharm87030021An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i>Krisyanti Budipramana0Junaidin Junaidin1Komar Ruslan Wirasutisna2Yanatra Budi Pramana3Sukrasno Sukrasno4Pharmaceutical Biology Researched Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaMuhammadiyah Tangerang College of Pharmacy, Tangerang 15118, IndonesiaPharmaceutical Biology Researched Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaFaculty of Industrial Technology, Universitas PGRI Adi Buana, Surabaya 60234, IndonesiaPharmaceutical Biology Researched Group, School of Pharmacy, Bandung Institute of Technology, Bandung 40132, IndonesiaBackground: <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.https://www.mdpi.com/2218-0532/87/3/21α-glucosidase inhibitordiabetes mellitusDPP-4-inhibitor<i>Ganoderma</i>in silicostellasterol |
| spellingShingle | Krisyanti Budipramana Junaidin Junaidin Komar Ruslan Wirasutisna Yanatra Budi Pramana Sukrasno Sukrasno An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> Scientia Pharmaceutica α-glucosidase inhibitor diabetes mellitus DPP-4-inhibitor <i>Ganoderma</i> in silico stellasterol |
| title | An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> |
| title_full | An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> |
| title_fullStr | An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> |
| title_full_unstemmed | An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> |
| title_short | An Integrated In Silico and In Vitro Assays of Dipeptidyl Peptidase-4 and α-Glucosidase Inhibition by Stellasterol from <i>Ganoderma australe</i> |
| title_sort | integrated in silico and in vitro assays of dipeptidyl peptidase 4 and α glucosidase inhibition by stellasterol from i ganoderma australe i |
| topic | α-glucosidase inhibitor diabetes mellitus DPP-4-inhibitor <i>Ganoderma</i> in silico stellasterol |
| url | https://www.mdpi.com/2218-0532/87/3/21 |
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