Apigenin isolated from A. americana encodes Human and Aspergillus oryzae S2 α-amylase inhibitions: credible approach for antifungal and antidiabetic therapies

Abstract

extract was analyzed by reverse phase HPLC for characterization. Among phenolic compounds identified, apigenin was observed to be present. The finding showed an inhibitory effect of apigenin towards Human and S2 α-amylases. Apigenin inhibition towards Human and α-amylase activities was observed to be competitive. IC50 and % inhibition of apigenin for α-amylase were 3.98 and 1.65 fold higher than for Human α-amylase. The inhibition of the described biocatalyst activity was significantly lowered when apigenin was pre-incubated with starch. In addition to the catalytic residues, 44 amino acid residues were involved on α-amylase-apigenin interactions while only 11 amino acid residues were exposed for Human α-amylase-apigenin complex. The binding site of apigenin showed 76 polar contacts for S2 α-amylase against 44 interactions for Human α-amylase. The docking studies confirmed the mode of action of apigenin and strongly suggested a higher inhibitory activity towards fungal amylase which was experimentally exhibited. These findings provided a rational reason to establish apigenin capability as a therapeutic target for postprandial hyperglycaemia modulation and antifungal therapy.

Effect of some Pseudomonas strains and Agave americana L. on wheat germination under salt stress

“…Depending on the characteristics of the isolated molecule, the bioactive potential is selective. A. oryzae α-amylase was more inhibited by the isolated compounds puerarin and apigenin from this plant species (95).…”

Effect of Artemisia extract on glycemic control: A systematic review and meta‐analysis of randomized controlled trial

“…Studies suggested that apigenin, one of the flavones, may play an anti‐diabetic role via facilitating GLUT‐4 translocation in skeletal muscles, 42 down‐regulating CD38 expression, 42 protecting β‐cell function through inhibition of inflammatory signalling pathways, 43‐45 modulating the activity of AMPK and related gene expression 46‐50 which in turn enhances peripheral insulin sensitivity, 42 and targeting PPARγ 43 and DPP‐4 51 . It is claimed that apigenin not only restrains α‐glucosidase, 52 but also binds to starch and hence ameliorates postprandial hyperglycaemia 53 . Apigenin may also protect vital organs against diabetes complications 42 …”

“…51 It is claimed that apigenin not only restrains α-glucosidase, 52 but also binds to starch and hence ameliorates postprandial hyperglycaemia. 53 Apigenin may also protect vital organs against diabetes complications. 42 Results of Khan et al study 54 showed protective effects of carnosol, anextract isolated from Artemisia, on Langerhans islets.…”

Hunting Bioactive Molecules from the Agave Genus: An Update on Extraction and Biological Potential

“…Puerarin and apigenin isolated from this species showed greater inhibitory effects against A. oryzae α-amylase, while p-coumaric acid proved a major inhibitor to human α-amylase at IC 50 : 98.8 µM, with an inhibition rate 2.3 times higher than acarbose. Thus, isolated flavonoids may be used as therapeutic agents for postprandial glycemia [52,53].…”