College of Pharmacy and Research Institute of Pharmaceutical Sciences, Chonnam National University, Gwangju, Republic of Korea.
Nat Prod Res. 2022 Aug;36(16):4103-4113. doi: 10.1080/14786419.2021.1975702. Epub 2021 Sep 10.
Microbial transformation is an important tool to perform selective conversion of compounds to derivatives which are difficult to produce synthetically. In order to obtain icariside II and icaritin, the active components in Herba Epimedii , biotransformation studies using microbes as biocatalysts were carried out. Icariside II () and icaritin () were produced through biotransformation of icariin () using the fungi and var. in 98% and 92% yields, respectively. In the subsequent transformation studies, was deglycosylated to form by , whereas was further converted to a novel compound icaritin-3--β-d-glucopyranoside () and previously known icaritin-3,7--β-d-diglucopyranoside () by . Biological evaluation of these compounds using MTT assay exhibited potent cytotoxic activities against human cancer cell lines A549, A375P, and MCF-7, with icariin being the most active, indicating that glycosylation plays a role in the cytotoxic activity.
微生物转化是一种重要的工具，可以将化合物选择性地转化为难以通过合成方法得到的衍生物。为了获得淫羊藿中的活性成分朝藿定 II 和朝藿定甲素，我们使用微生物作为生物催化剂进行了生物转化研究。通过真菌 和 var. 对朝藿定苷（）进行生物转化，分别以 98%和 92%的产率得到了朝藿定 II（）和朝藿定甲素（）。在随后的转化研究中，通过 使 去糖基化生成 ，而 进一步转化为一种新的化合物朝藿定甲素-3--β-D-吡喃葡萄糖苷（）和之前已知的朝藿定甲素-3,7--β-D-二吡喃葡萄糖苷（）。采用 MTT 法对这些化合物进行的生物评价显示，它们对人肺癌细胞系 A549、A375P 和 MCF-7 具有很强的细胞毒性活性，其中朝藿定苷的活性最强，表明糖基化在细胞毒性活性中发挥了作用。
