Cargando…
Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall.
Neuropeltis racemosa Wall. (Convolvulaceae) is wildly distributed in Asia. Its stem is used as the component in traditional Thai recipes for treatments of muscle rigidity, skin disorder, dysentery, and hypoglycemia. However, the chemical constituents and biological activities of N. racemosa have not...
Autores principales: | , , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8839375/ https://www.ncbi.nlm.nih.gov/pubmed/35163903 http://dx.doi.org/10.3390/molecules27030639 |
_version_ | 1784650354422448128 |
---|---|
author | Sakulkeo, Oraphan Wattanapiromsakul, Chatchai Pitakbut, Thanet Dej-adisai, Sukanya |
author_facet | Sakulkeo, Oraphan Wattanapiromsakul, Chatchai Pitakbut, Thanet Dej-adisai, Sukanya |
author_sort | Sakulkeo, Oraphan |
collection | PubMed |
description | Neuropeltis racemosa Wall. (Convolvulaceae) is wildly distributed in Asia. Its stem is used as the component in traditional Thai recipes for treatments of muscle rigidity, skin disorder, dysentery, and hypoglycemia. However, the chemical constituents and biological activities of N. racemosa have not been reported. From a screening assay, N. racemosa stem crude extract showed the potent effect on alpha-glucosidase inhibition at 2 mg/mL as 96.09%. The bioassay-guiding isolation led to 5 compounds that were identified by spectroscopic techniques as scopoletin (1), syringic acid (2), methyl 3-methyl-2-butenoate (3), N-trans-feruloyltyramine (4), and N-trans- coumaroyltyramine (5). Compounds 1, 4, and 5 exhibited an IC(50) of 110.97, 29.87, and 0.92 µg/mL, respectively, while the IC(50) of positive standard, acarbose was 272.72 µg/mL. Kinetic study showed that compound 1 performed as the mixed-type inhibition mechanism, whereas compounds 4 and 5 displayed the uncompetitive inhibition mechanism. The docking study provided the molecular understanding of isolated aromatic compounds (1, 2, 4 and 5) to alpha-glucosidase. Hence, this study would be the first report of isolated compounds and their anti-alpha-glucosidase activity with the mechanism of action from N. racemosa. Thus, these active compounds will be further studied to be the lead compounds among natural antidiabetic drugs. |
format | Online Article Text |
id | pubmed-8839375 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-88393752022-02-13 Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. Sakulkeo, Oraphan Wattanapiromsakul, Chatchai Pitakbut, Thanet Dej-adisai, Sukanya Molecules Article Neuropeltis racemosa Wall. (Convolvulaceae) is wildly distributed in Asia. Its stem is used as the component in traditional Thai recipes for treatments of muscle rigidity, skin disorder, dysentery, and hypoglycemia. However, the chemical constituents and biological activities of N. racemosa have not been reported. From a screening assay, N. racemosa stem crude extract showed the potent effect on alpha-glucosidase inhibition at 2 mg/mL as 96.09%. The bioassay-guiding isolation led to 5 compounds that were identified by spectroscopic techniques as scopoletin (1), syringic acid (2), methyl 3-methyl-2-butenoate (3), N-trans-feruloyltyramine (4), and N-trans- coumaroyltyramine (5). Compounds 1, 4, and 5 exhibited an IC(50) of 110.97, 29.87, and 0.92 µg/mL, respectively, while the IC(50) of positive standard, acarbose was 272.72 µg/mL. Kinetic study showed that compound 1 performed as the mixed-type inhibition mechanism, whereas compounds 4 and 5 displayed the uncompetitive inhibition mechanism. The docking study provided the molecular understanding of isolated aromatic compounds (1, 2, 4 and 5) to alpha-glucosidase. Hence, this study would be the first report of isolated compounds and their anti-alpha-glucosidase activity with the mechanism of action from N. racemosa. Thus, these active compounds will be further studied to be the lead compounds among natural antidiabetic drugs. MDPI 2022-01-19 /pmc/articles/PMC8839375/ /pubmed/35163903 http://dx.doi.org/10.3390/molecules27030639 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Sakulkeo, Oraphan Wattanapiromsakul, Chatchai Pitakbut, Thanet Dej-adisai, Sukanya Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title | Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title_full | Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title_fullStr | Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title_full_unstemmed | Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title_short | Alpha-Glucosidase Inhibition and Molecular Docking of Isolated Compounds from Traditional Thai Medicinal Plant, Neuropeltis racemosa Wall. |
title_sort | alpha-glucosidase inhibition and molecular docking of isolated compounds from traditional thai medicinal plant, neuropeltis racemosa wall. |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8839375/ https://www.ncbi.nlm.nih.gov/pubmed/35163903 http://dx.doi.org/10.3390/molecules27030639 |
work_keys_str_mv | AT sakulkeooraphan alphaglucosidaseinhibitionandmoleculardockingofisolatedcompoundsfromtraditionalthaimedicinalplantneuropeltisracemosawall AT wattanapiromsakulchatchai alphaglucosidaseinhibitionandmoleculardockingofisolatedcompoundsfromtraditionalthaimedicinalplantneuropeltisracemosawall AT pitakbutthanet alphaglucosidaseinhibitionandmoleculardockingofisolatedcompoundsfromtraditionalthaimedicinalplantneuropeltisracemosawall AT dejadisaisukanya alphaglucosidaseinhibitionandmoleculardockingofisolatedcompoundsfromtraditionalthaimedicinalplantneuropeltisracemosawall |