Baohuoside I has better in vivo bioactivities than Icariin. Its preparation methods, such as acid hydrolysis, are of low efficiency, with undesirable byproducts. The objective of this study was to establish a novel catalysis system for its clean and efficient preparation via biphase enzymatic hydrolysis. β-glucosidase was selected from five commercial enzymes due to the best catalysis performance. After optimization of conditions, a biphase system was constructed with EtOAc and HAc-NaAc buffer (pH 4.5) (5:1, v/v) containing Icariin/β-glucosidase (3.2:1, w/w), and hydrolysis was performed at 60 °C for 2 h. Consequently, the conversion rate of Icariin was 99.92 ± 0.11% (n = 3), and the processing capacity in the system was increased from 20 mg/mL to 50 mg/mL, 2.5 times that of conventional enzymatic hydrolysis, meanwhile the procedure was much simplified. Additionally, complete hydrolysis with conversion rate at 99.14% had been achieved after the enzyme solution was used twice. The newly proposed strategy is a clean and efficient approach for the preparation of Baohuoside I and also a promising technology for producing secondary glycosides or aglycones.

宝火苷I的体内生物活性优于伊卡瑞林。其制备方法，例如酸水解，效率低，副产物不合需要。这项研究的目的是建立一种新型的催化体系，用于通过双相酶解法清洁，高效地进行制备。由于最佳的催化性能，β-葡萄糖苷酶选自5种商业酶。在优化条件后，用EtOAc和含有伊卡霉素/ β-葡萄糖苷酶（3.2：1，w / w）的HAc-NaAc缓冲液（pH 4.5）（5：1，v / v）构建双相系统。），然后在60°C下水解2小时。结果，伊car素的转化率为99.92±0.11％（n = 3），系统的处理能力从20 mg / mL增加到50 mg / mL，是常规酶水解的2.5倍，同时该过程大大简化了。另外，在两次使用该酶溶液之后，已经实现了完全水解，转化率为99.14％。新提出的策略是一种制备宝火苷I的干净有效的方法，也是一种生产次生糖苷或苷元的有前途的技术。