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.
Highlights
Datura metel belongs to family Solanaceae which grows throughout the year and is normally known as devil’s trumpet [1, 2]
A small portion of all obtained extracts was subjected to thin-layer chromatography (TLC), by using different solvent systems; the maximum separation was observed in n-hexane and ethyl acetate
Based on TLC profile, SB-9 was subjected to repeated pencil column chromatography (CC), eluting with n-hexane and ethyl acetate (14 : 86), which yielded white crystal
Summary
Datura metel belongs to family Solanaceae which grows throughout the year and is normally known as devil’s trumpet [1, 2]. An alkaloid known as scopolamine is a major compound isolated from D. metel has been reported for the treatment of different diseases such as bronchitis and asthma [2]. D. metel is used for the cure of epilepsy, heart disease, fever, diabetes, insanity, diarrhea, and a skin disease [5, 6] It is a key source of producing anolides, which is used for the treatment of pain and have hallucinogenic strength [7,8,9]. Its seeds are used for the treatment of dental pain It has extensive application in ayurvedic medication such as many classes of compounds isolated from the title plant that is used to treat hair fall and many skin-related infection disease [10]. Human α-glycosidase enzymes in the mucosal brush edge of the small intestine catalyzed the finale step of digestion of disaccharides and starch present in human food. α-
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