Yongfu Li, Xiaoqiang Chen, Jinrong Huang, Feng Shi, β-glucosidase-assisted extraction of Gastrodia elata enhances gastrodigenin production and α-glucosidase inhibition: mechanisms and in vivo glycemic regulation, Food Bioscience, Volume 82, 2026, 109298, ISSN 2212-4292.

发表期刊：Food Bioscience

发表时间：2026

Abstract:

Gastrodia elata is an edible plant whose phenolic compounds show α-glucosidase inhibitory activity. Through screening, it was found that 4-hydroxybenzyl alcohol (HBA) is the most potent inhibitor (IC50 = 0.0406 mg/mL). However, HBA occurs at very low levels in native G. elata, making it difficult to acquire sufficient active components via routine approaches. Different from conventional organic solvent extraction and microbial fermentation, the β-glucosidase-catalyzed strategy developed here has the advantages of short processing time, mild reaction conditions and environmental friendliness. Compared with water extraction, this method increased HBA content by 9.76 fold and improved α-glucosidase inhibitory activity by 5.31 fold. Enzymolysis conditions were optimized via response surface methodology at 51.5°C, 6 U/mL and 4.7 h, yielding 832 μg/mL HBA with an inhibition rate of 71.4%. Pearson correlation confirmed HBA as an important contributor to the bioactivity (r = 0.6669). Mechanistic analyses via kinetics, spectroscopy, molecular docking, and 100 ns molecular dynamics simulations revealed HBA acts as a non-competitive inhibitor binding to the allosteric site at Ser236, Asn317, and His423. The optimized extract (5% v/v, 322 μM HBA) significantly promoted glucose consumption and glycogen synthesis in insulin-resistant HepG2 cells without cytotoxicity. It also dose-dependently reduced glucose, triglyceride, and total cholesterol in high-glucose-stimulated zebrafish larvae. This efficient catalytic approach achieves high HBA enrichment and clarifies the underlying inhibitory mechanism, supporting G. elata extract as a promising functional food for glycemic and lipid regulation.

https://doi.org/10.1016/j.fbio.2026.109298