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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.


ABSTRACT: 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 IC50160.2 ± 1.85 μg and daturaolone (1) with 98.7% inhibition with IC50840.4 ± 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 IC50 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 IC50 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.

SUBMITTER: Bawazeer S 

PROVIDER: S-EPMC7468596 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature

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

Bawazeer Saud S   Rauf Abdur A   Bawazeer Sami S  

BioMed research international 20200825


This study deals with <i>α</i>-glucosidase and <i>β</i>-secretase inhibitory screening of extract/fractions and isolated daturaolone (<b>1</b>), namely, 3-oxo-6-<i>β</i>-hydroxy-<i>β</i>-amyrin (daturaolone) from chloroform fraction of <i>Datura metel</i> L. Among entire fractions, the chloroform soluble fraction showed excellent activity against <i>α</i>-glucosidase with % inhibition 90.8 with IC<sub>50</sub>160.2 ± 1.85 <i>μ</i>g and daturaolone (<b>1</b>) with 98.7% inhibition with IC<sub>50<  ...[more]

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