Biotransformation and activity identification of icariin in human intestinal fungus Pichia occidentalis

  • J Asian Nat Prod Res. 2025 May 21:1-12. doi: 10.1080/10286020.2025.2493937.
Jia-Shuo Li  1 ,  Ru-Xin Yao  2 ,  Qing Lv  3 ,  Gang Wang  1 ,  Xue Wang  2 ,  Yu-Fei Wang  4 ,  Fang-Yu Yang  4 ,  Guo-Biao Liang  4 ,  Zhuang Miao  5
Affiliations
  • 1. Graduate School, Dalian Medical University, Dalian116000, China.
  • 2. School of Pharmacy, Dalian Medical University, Dalian116000, China.
  • 3. Laboratory Animal Center, Dalian Medical University, Dalian116000, China.
  • 4. Institute of Neurology, General Hospital of Shenyang Military Command, Shenyang110000, China.
  • 5. Anesthesiology, The First Affiliated Hospital of Dalian Medical University, Dalian116000, China.
PMID: 40396926 DOI: 10.1080/10286020.2025.2493937
Abstract

Compared to icariin, icariside II demonstrates superior absorption and metabolic properties along with enhanced bioactivity. In this study, using DXM-Glc fluorescence assay, Pichia occidentalis was identified as an intestinal fungus expressing functional glucosidase, which could efficiently convert icariin to icariside II via glycosidic bond hydrolysis, revealing the fungus-mediated intestinal glycoside metabolism pathway and determining the optimal conditions for the conversion, including temperature, drug loading, pH and reaction time. Meanwhile, icariside II exhibited anti-glioma activity, and its mechanism of action involved the inhibition of the activation of NF-κB signaling pathway in glioma cells.

Keywords
Biotransformation; Pichia occidentalis; anti-tumour; fungi; icariside II.
Products