Diosgenin has been widely used as a precursor in the pharmaceutical industry. The conventional diosgenin production method, direct acid hydrolysis, can cause severe environmental pollution and has low production efficiency. In this study, the β-glucosidase FBG1 was successfully over-expressed in Pichia pastoris. The engineered yeast was grown in 5- and 50-L bioreactors to a high-cell-density, and the resulting recombinant FBG1 without purification was directly used for trillin biocatalysis. A novel enzymatic biocatalysis method was established through efficient biocatalysis of trillin by recombinant FBG1 and a practical diosgenin purification process. Diosgenin production reached ∼1.7 mg/mL under optimized biocatalysis conditions with a corresponding ∼94 % trillin conversion. The production process was further scaled up from 2 mL to 20, 200, and 2000 mL working volumes, producing equivalent efficiency. This recombinant enzyme biocatalysis process resulted in ∼680 mg diosgenin when 1 g trillin was processed, together with ∼90 % environmental impact elimination and ∼36 % cost reduction. Enzymatic biocatalysis can convert trillin into a high-value-added pharmaceutical precursor of diosgenin with high eco-efficiency, cost-effectiveness, and sustainability is presented here for the first time and is a promising method for future applications in industrial processes.

薯蓣皂苷元已被广泛用作制药工业的前体。传统的薯蓣皂苷元直接酸水解法生产环境污染严重，生产效率低。在本研究中，β-葡萄糖苷酶 FBG1 在毕赤酵母中成功过表达. 工程酵母在 5 升和 50 升的生物反应器中生长至高细胞密度，所得的重组 FBG1 未经纯化直接用于 Trillin 生物催化。通过重组FBG1对trillin的高效生物催化和实用的薯蓣皂苷元纯化工艺，建立了一种新的酶促生物催化方法。在优化的生物催化条件下，薯蓣皂苷元的产量达到约 1.7 mg/mL，相应的三苯甲基转化率为约 94%。生产过程进一步从 2 mL 扩大到 20、200 和 2000 mL 工作体积，产生了相同的效率。这种重组酶生物催化过程在加工 1 克三苯甲基时产生了约 680 毫克薯蓣皂苷元，同时减少了约 90% 的环境影响和降低了约 36% 的成本。