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Outline
To investigate the inhibitory effect of hyperoside on α-amylase and its mechanism of exerting hypoglycemic activity.
The inhibitory effect and type of hyperoside on α-amylase were evaluated via enzymatic kinetics. Fluorescence spectroscopy was used to observe the effect of hyperoside on α-amylase activity and its underlying mechanism. Molecular docking technology was employed to elucidate the molecular interactions between hyperoside and α-amylase from a microscopic perspective.
Hyperoside exhibited a significant inhibitory effect on α-amylase, with a median inhibitory concentration (IC50) of 1.081 mg/mL. The inhibition type was identified as reversible mixed competitive and non-competitive inhibition. Hyperoside induced a fluorescence quenching effect on α-amylase, and the quenching mode was determined to be static quenching. With the increase in hyperoside concentration, the maximum emission wavelength of α-amylase showed a blue shift, indicating a change in its spatial conformation. Molecular docking results revealed that hyperoside could enter the cavity of α-amylase,competitively bind to the active site, and interact with amino acid residues (THR163A, LEU165A, TRP59A,GLN63A, ARG195A, HIS201A, GLU233A, ASP300A and HIS305A) through hydrogen bonds and hydrophobic interactions. The binding energy between hyperoside and α-amylase was –8.3 kcal/mol, indicating a tight binding.
Hyperoside forms a complex with α-amylase, thereby hindering enzymatic catalysis of substrates,further diminishing enzymatic activity, and ultimately contributing to its hypoglycemic effect.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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