Eight novel acetophenone mono- and bis-C-glucosides were obtained by whole cells harboring an engineered C-glycosyltransferase. Optimization of the fed-bath process improved the yield of 4a to 0.97 mg/mL with 95% conversion rate, which is 2.9-fold higher than that of the single-bath. Four mono-C-glucosides (1a–4a) exhibited potent SGLT2 inhibitory activities with IC₅₀ values at 10⁻⁶ M. These findings provide a cost-effective and practical synthetic strategy to produce structurally diverse and novel bioactive C-glucosides for drug discovery.

中文翻译：

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使用工程C-糖基转移酶在大肠杆菌中生产苯乙酮C-糖苷

通过携带工程化的C-糖基转移酶的全细胞获得了八种新的苯乙酮单-和双-C-葡萄糖苷。通过优化饲喂浴工艺，将4a的产量提高到0.97 mg / mL，转化率达到95％，比单浴提高了2.9倍。四种单-C-糖苷（1a - 4a）表现出有效的SGLT2抑制活性，IC ₅₀值为10 ^-6M  。这些发现提供了一种经济有效的合成策略，可生产结构多样且新颖的生物活性C-糖苷用于药物开发。