α-Amylase Inhibition: Some Practical Considerations

Abstract

Enzyme inhibitors are important tools of nature for regulating the activity of enzymes in case of emergency. Proteinaceous inhibitors are the best studied in this group. Comparatively less is known about the inhibitors of -amylase, which might be an attractive candidate having potentials in various fields, from the treatment of diabetes to crop protection. The area has benefited from the recent determination of structures of -amylases, inhibitors and complexes. Besides, discussing various types of -amylase inhibitors and their structural basis of inhibition, the biotechnological approaches for exploitation of its inhibitory function have been outlined in this minireview.

Bioevaluation of synthetic pyridones as dual inhibitors of α‐amylase and α‐glucosidase enzymes and potential antioxidants

“…abund. ): 382 (M + , 100), 384 (M+2, 98), 355 (14), 303 (8), 275 (20), 260 (7); Anal. calcd for C 19 H 12 BrFN 2 O: C,59.55;H,3.16;N,7.31;Found: C,59.57;H,3.17;N, Bromo-2-fluorophenyl)-6-(4-chlorophenyl)-2-oxo-1,2-dihydropyridine-3-carbonitrile (33) Light yellow amorphous solid; yield: 75%; M.p. : 337°C-339°C; 1 H-NMR (400 MHz, DMSO-d 6 ): δ 13.02 (br.s, 1H, N-H), 7.94 (br.s, 2H, H-2′, H-6′), 7.87 (dd, J 6,F = 4 Hz, J 6,4 = 1.2 Hz, 1H, H-6), 7.80 (m, 1H, H-4), 7.60 (d, J 3′,2′/5′,6′ = 8 Hz, 2H, H-3′, H-5′), 7.44 (t, J 3,4/3,F = 8 Hz, 1H, H-3), 6.93 (br s, 1H, H-a); EI MS m/z (% rel.…”

“…3.2.1.1) and α-glucosidases are crucial enzymes in the digestive tract that catalyze the conversion of dietary carbohydrates into simple monosaccharides. [7][8][9] Inhibiting the enzymes α-amylase and α-glucosidase can thus limit carbohydrate digestion, lengthening the overall digestion period, reducing glucose absorption, and blunting postprandial plasma glucose levels. [10] In practice, medications like acarbose, voglibose, and miglitol suppress α-amylase and α-glucosidase, but they cause unpleasant side effects such as bloating, flatulence, abdominal pain, and diarrhea.…”

Study of molecular and functional diversity of plant cystine knot miniproteins

“…They vary greatly in both structure and size, ranging from small molecules (<1 kDa) such as carbohydrates, organic acids [41] and polyphenolics [42] to large proteins with the mass >56 kDa [43]. Both classes of α-amylase inhibitors have attracted attentions as tools in agriculture and antidiabetic management [44,45]. Genes encoding amylase inhibitors have been successfully introduced into crop plants, rendering them pathogenresistant.…”

“…Since then, much has been known about various families of α-amylase inhibitors. Many reviews have been published, covering their occurrence, activity specificities, chemical and structural properties, inhibitory mechanisms, and applications of transgenic plants in crop protection and nutrition remedy [45,[52][53][54].…”

“…Many α-amylase inhibitors have been reported to be bifunctional [74]. The first function is their activities against α-amylases from various sources.…”