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

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.