State Key Laboratory of Component-Based Chinese Medicine, Tianjin University of Traditional Chinese Medicine, 10 Poyanghu Road, Jinghai District, Tianjin 301617, China.
Haihe Laboratory of Modern Chinese Medicine, 10 Poyanghu Road, Jinghai District, Tianjin 301617, China.
Molecules. 2023 Mar 30;28(7):3093. doi: 10.3390/molecules28073093.
Diosgenin (DSG), a steroidal sapogenin derived from the tuberous roots of yam, possesses multiple biological properties. DSG has been widely used as a starting material for the industrial production of steroid drugs. Despite its significant pharmacological activities, moderate potency and low solubility hinder the medicinal application of DSG. Biotransformation is an efficient method to produce valuable derivatives of natural products. In this work, we performed the biotransformation of DSG using five strains. Compounds - were isolated and identified from . Compounds and showed potent cytotoxicity against the A549, MCF-7, and HepG2 cell lines. Compounds and are novel entities, and each possesses a terminal carboxyl group attached to the spiroacetal ring. Remarkably, exhibited significant cell protective effects for kidney, liver, and vascular endothelial cells, suggesting the therapeutic potential of this compound in chronic renal diseases, atherosclerosis, and hypertension. We further optimized the fermentation conditions aiming to increase the titer of compound . Finally, the yield of compound was improved by 2.9-fold and reached 32.4 mg/L in the optimized conditions. Our study lays the foundation for further developing compound as a cell protective agent.
薯蓣皂苷元(DSG)是一种甾体皂素,来源于山药的块茎根,具有多种生物学特性。DSG 已被广泛用作甾体药物工业生产的起始原料。尽管其具有显著的药理活性,但中等效力和低溶解度限制了 DSG 在医学上的应用。生物转化是一种生产天然产物有价值衍生物的有效方法。在这项工作中,我们使用五种菌株对 DSG 进行了生物转化。从 中分离并鉴定出化合物 -。化合物 和 对 A549、MCF-7 和 HepG2 细胞系表现出很强的细胞毒性。化合物 和 是新的实体,每个都具有连接到螺缩酮环的末端羧基。值得注意的是, 对肾脏、肝脏和血管内皮细胞表现出显著的细胞保护作用,表明该化合物在慢性肾病、动脉粥样硬化和高血压中的治疗潜力。我们进一步优化了发酵条件,旨在提高化合物 的产量。最后,在优化条件下,化合物 的产量提高了 2.9 倍,达到 32.4mg/L。我们的研究为进一步将化合物 开发为细胞保护剂奠定了基础。