Context:
The substantial increase in the number of diabetics has encouraged the search for new pharmacological strategies to face this problem. In this regard, triazole and its derivatives have attracted considerable attention for the past few decades due to their pharmacological significance.
Objective:
Evaluation of the inhibitory activity of α-glucosidase and α-amylase in essential oils extracted from plant
Eruca vesicaria
(L) Cav. subsp.
longirostris
(Brassicaceae) (EVL) and to verify whether the triazoles and thiadiazol bearing the lipophilic 4-methylthiobutyl group synthesized from the essential oil contribute to this activity.
Materials and methods:
The essential oils were extracted by hydrodistillation from leaf, stem, root, and fruit of EVL, and their chemical compositions were analyzed by gas chromatography and gas chromatography-mass spectrometry. We present here the synthesis of three new types of 1,2,4-triazole-thiol and 1,3,4-thiadiazol and the structures were confirmed by NMR, mass spectrometry. The α-glucosidase and α-amylase inhibitory activities were investigated
in vitro
.
Results:
The main compound in fruit, stem, and root was erucin (96.6, 85.3, and 83.7%, respectively). The three essential oils of the fruit, stem, and root have strong inhibitory activity on α-glucosidase and α-amylase; IC
50
values of roots were 0.81 ± 0.02 μg/mL and 0.13 ± 0.01 μg/mL, respectively. Derivatives
1 b
,
2 b
,
3 b,
and
2c
showed remarkable inhibitory activity against α-glucosidase with potencies better than that of acarbose with IC
50
values ranging between 0.49 and 1.43 μM.
Conclusions:
Current results indicate that ECL fruit essential oil can be used as a natural precursor for the synthesis of triazoles as potential hypoglycemic agents.
This work describes the study of the chemical composition and bioactivity of the essential oils (EOs) of the different organs (leaves, flowers, stems and roots) from Eruca vesicaria. According to the GC and GC/MS analysis, all the EOs were dominated by erucin (4‐methylthiobutyl isothiocyanate) with a percentage ranging from 17.9 % (leaves) to 98.5 % (roots). The isolated EOs were evaluated for their antioxidant (DPPH, ABTS and β‐carotene/linoleic acid), antibacterial and inhibitory property against α‐amylase and α‐glucosidase. Most EOs exhibited an interesting α‐glucosidase and α‐amylase inhibitory potential. The roots essential oil was found to be the most active with IC50 values of 0.80±0.06 and 0.11±0.01 μg mL−1, respectively. The essential oil of roots exhibited the highest antioxidant activity (DPPH, PI=92.76±0.01 %; ABTS, PI=78.87±0.19; and β‐carotene, PI=56.1±0.01 %). The isolated oils were also tested for their antibacterial activity against two Gram‐positive and three Gram‐negative bacteria. Moderate results have been noted by comparison with Gentamicin used as positive control.
The essential oils (EOs) of different organs (flowers, vegetative parts (stems + leaves) and roots) of Achillea cretica were investigated. Antioxidant and antimicrobial activity of the essential oils were also evaluated. They have been analyzed by a combination of GC and GC/MS. Twenty-five, twenty-nine and twenty-five compounds, accounting for 97.9%, 98.80% and 96.20% of the root, (stem + leaf), and flower oils, were identified, respectively. The EOs were rich in monoterpenes (camphor, borneol, camphene and 1,8-cineola) and camphor was identified as a major constituent. Furthermore, the antioxidant activity was evaluated by DPPH, ABTS and ferric reducing assays. The isolated oils showed significant radical-scavenging activity evidenced by IC50 value for ABTS radical (in between IC50 =62 µg/mL and IC50 = 70 µg/mL). The antibacterial activity was tested against two Gram-positive and three Gram-negative bacteria using the broth dilution method. The flowers essential oil shows an excellent inhibitory effect on S. aureus
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