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 in vivo, biotransformation studies using microbes as biocatalysts were carried out. Icariside II (2) and icaritin (3) were produced through biotransformation of icariin (1) using the fungi Hormoconis resinae and Mortierella ramanniana var. angulispora in 98% and 92% yields, respectively. In the subsequent transformation studies, 2 was deglycosylated to form 3 by Gliocladium deliquescens, whereas 3 was further converted to a novel compound icaritin-3-O-β-d-glucopyranoside (4) and previously known icaritin-3,7-O-β-d-diglucopyranoside (5) by Mucor hiemalis. 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.
Demethylzeylasteral (DZ) used as a control in the bioassays was purchased from Biopurify Phytochemicals Ltd. (Chengdu, China).
Microbial transformation of icariin and its derivatives
期刊名：Natural Product Research
文献编号：
文献地址： https://www.tandfonline.com/doi/abs/10.1080/14786419.2021.1975702?journalCode=gnpl20
发表日期：10 Sep 2021
文献编号：
文献地址： https://www.tandfonline.com/doi/abs/10.1080/14786419.2021.1975702?journalCode=gnpl20
发表日期：10 Sep 2021
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