Synthesis, characterization and α‐amylase and α‐glucosidase inhibition studies of novel vanadyl chalcone complexes

Abstract

A series of chalcone ligands and their corresponding vanadyl complexes of composition [VO (L I-IV) 2 (H 2 O) 2 ]SO 4 (where L I = 1,3-Diphenylprop-2-en-1-one, L II = 3-(2-Hydroxy-phenyl)-1-phenyl-propenone, L III = 3-(3-Nitro-phenyl)-1-phenyl-propenone, L IV = 3-(4-Methoxy-phenyl)-1-phenyl-propenone) have been synthesized and characterized using various spectroscopic (Fouriertransform infrared, electrospray ionization mass, nuclear magnetic resonance, electron paramagnetic resonance, thermogravimetric analysis, vibrating sample magnetometer) and physico-analytic techniques. Antidiabetic activities of synthesized complexes along with chalcones were evaluated by performing in vitro and in silico α-amylase and α-glucosidase inhibition studies. The obtained results displayed moderate to significant inhibition activity against both the enzymes by vanadyl chalcone complexes. The most potent complexes were further investigated for the enzyme kinetic studies and displayed the mixed inhibition for both the enzymes. Further, antioxidant activity of vanadyl chalcone complexes was evaluated for their efficiency to release oxidative stress using 2,2-diphenyl-1-picryl-hydrazyl-hydrate assay, and two complexes (Complexes 2 and 4) have demonstrated remarkable antioxidant activity. All the complexes were found to possess promising antidiabetic and antioxidant potential.

Synthesis of an amantadine-based novel Schiff base and its transition metal complexes as potential ALP, α-amylase, and α-glucosidase inhibitors

“…The a-glucosidase inhibitory activity was measured following a reported method with slight modications. 60,61 Briey, 10 mL of sample solution and 30 mL of 0.1 M phosphate buffer (pH 6.8) containing a-glucosidase solution (0.2 U mL −1 ) was incubated in 96 well plates at 37 °C for 10 min. Aer pre-incubation, 30 mL of 5 mM p-nitrophenyl-a-D-glucopyranoside (PNPG) solution in 0.1 M phosphate buffer (pH 6.8) was added to each well incubated at 37 °C for another 20 min.…”