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Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits

This study deals with α-glucosidase and β-secretase inhibitory screening of extract/fractions and isolated daturaolone (1), namely, 3-oxo-6-β-hydroxy-β-amyrin (daturaolone) from chloroform fraction of Datura metel L. Among entire fractions, the chloroform soluble fraction showed excellent activity a...

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Autores principales: Bawazeer, Saud, Rauf, Abdur, Bawazeer, Sami
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7468596/
https://www.ncbi.nlm.nih.gov/pubmed/32908922
http://dx.doi.org/10.1155/2020/8530165
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author Bawazeer, Saud
Rauf, Abdur
Bawazeer, Sami
author_facet Bawazeer, Saud
Rauf, Abdur
Bawazeer, Sami
author_sort Bawazeer, Saud
collection PubMed
description This study deals with α-glucosidase and β-secretase inhibitory screening of extract/fractions and isolated daturaolone (1), namely, 3-oxo-6-β-hydroxy-β-amyrin (daturaolone) from chloroform fraction of Datura metel L. Among entire fractions, the chloroform soluble fraction showed excellent activity against α-glucosidase with % inhibition 90.8 with IC(50)160.2 ± 1.85 μg and daturaolone (1) with 98.7% inhibition with IC(50)840.4 ± 1.74 μM, respectively. Similarly, extract and daturaolone (1) also exhibited significant activity against the β-secretase enzyme (BACE1) with % activities 88.27 and 95.19 and with IC(50) values 304.21 ± 2.98 μg and 260.70 ± 1.87 μM, respectively, as compared to the standard inhibitor (Ans670, Sta671, Val672)-amyloid-β/A4 precursor protein 770 fragments 662-675) with % activity 94.21 and IC(50) value 289.24 ± 1.60 μM. This finding encourages and opens a new window for further detail phytochemical investigation on D. metel in order to isolate novel compounds with promising enzyme inhibitory potential.
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spelling pubmed-74685962020-09-08 Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits Bawazeer, Saud Rauf, Abdur Bawazeer, Sami Biomed Res Int Research Article This study deals with α-glucosidase and β-secretase inhibitory screening of extract/fractions and isolated daturaolone (1), namely, 3-oxo-6-β-hydroxy-β-amyrin (daturaolone) from chloroform fraction of Datura metel L. Among entire fractions, the chloroform soluble fraction showed excellent activity against α-glucosidase with % inhibition 90.8 with IC(50)160.2 ± 1.85 μg and daturaolone (1) with 98.7% inhibition with IC(50)840.4 ± 1.74 μM, respectively. Similarly, extract and daturaolone (1) also exhibited significant activity against the β-secretase enzyme (BACE1) with % activities 88.27 and 95.19 and with IC(50) values 304.21 ± 2.98 μg and 260.70 ± 1.87 μM, respectively, as compared to the standard inhibitor (Ans670, Sta671, Val672)-amyloid-β/A4 precursor protein 770 fragments 662-675) with % activity 94.21 and IC(50) value 289.24 ± 1.60 μM. This finding encourages and opens a new window for further detail phytochemical investigation on D. metel in order to isolate novel compounds with promising enzyme inhibitory potential. Hindawi 2020-08-25 /pmc/articles/PMC7468596/ /pubmed/32908922 http://dx.doi.org/10.1155/2020/8530165 Text en Copyright © 2020 Saud Bawazeer et al. http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Research Article
Bawazeer, Saud
Rauf, Abdur
Bawazeer, Sami
Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title_full Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title_fullStr Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title_full_unstemmed Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title_short Potent In Vitro α-Glucosidase and β-Secretase Inhibition of Amyrin-Type Triterpenoid Isolated from Datura metel Linnaeus (Angel's Trumpet) Fruits
title_sort potent in vitro α-glucosidase and β-secretase inhibition of amyrin-type triterpenoid isolated from datura metel linnaeus (angel's trumpet) fruits
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7468596/
https://www.ncbi.nlm.nih.gov/pubmed/32908922
http://dx.doi.org/10.1155/2020/8530165
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