Effect of Natural β‐Glucosidase Inhibitors in Reducing Toxicity of Amygdalin in Persicae Semen

Amygdalin can be decomposed into hydrocyanic acid, which is the primary source of Persicae Semen toxicity, by gut flora. Here, the inhibitory activity of β‐glucosidase for test herb extracts was first determined and compared. In turn, optimization of the ratio of substrate and inhibitor in vitro and LD₅₀ values of extracts, serum and liver contents of amygdalin in vivo was measured. Lycii Cortex was found to be the best inhibitory activity for β‐glucosidase. The ratio of amygdalin‐to‐Lycii Cortex extract of 7.19:8.18 (mmol L^?1/mg mL^?1) can be relatively suitable for inhibiting β‐glucosidase activity in test in vitro reaction system. After mixed with Lycii Cortex extract, the toxicity of Persicae Semen ethanol extract in mice is significantly reduced and more amygdalin can be absorbed into the bloodstream. The study provides useful information for reducing toxicity of Persicae Semen and suggests how to better use these natural β‐glucosidase inhibitors in the utilization of glycosides and aglycones. Copyright © 2017 John Wiley & Sons, Ltd.