Identification of Fisetin as a Potential Therapeutic Target for Pseudoallergic Reactions

Strategic Insights -

Researchers at Xi'an Jiaotong University have identified fisetin, a compound found in the Rhus chinensis Mill herb, as a potential therapeutic target for pseudoallergic reactions. The compound was discovered using a cell membrane chromatography (CMC) technique, which allowed the researchers to screen for active components in complex systems. Fisetin was found to exhibit strong binding affinity with Mas-related G-protein coupled receptor member X2 (MrgprX2), a key receptor involved in pseudoallergic reactions.

The researchers used a previously constructed MrgprX2-HALO-tag/CMC-HPLC-MS system to identify fisetin as the first reported MrgprX2-targeting component from Rhus chinensis Mill. Through frontal analysis, they demonstrated that fisetin exhibits strong binding affinity (K = 2.02 mM) with MrgprX2, representing the first quantitative assessment of this interaction. Molecular docking revealed four key binding residues that form stable interactions with fisetin. Pharmacological validation using LAD2 cells confirmed fisetin's potent anti-allergic activity via MrgprX2 antagonism.

Key Takeaways:

  • Fisetin, a compound found in Rhus chinensis Mill, was identified as a potential therapeutic target for pseudoallergic reactions.
  • The compound was discovered using a cell membrane chromatography (CMC) technique.
  • Fisetin exhibits strong binding affinity (K = 2.02 mM) with MrgprX2, a key receptor involved in pseudoallergic reactions.
  • Molecular docking revealed four key binding residues that form stable interactions with fisetin.
  • Pharmacological validation using LAD2 cells confirmed fisetin's potent anti-allergic activity via MrgprX2 antagonism.
  • The research provides new perspectives for developing anti-pseudoallergic therapeutics.

Statistics:

  • K (binding affinity) for fisetin with MrgprX2: 2.02 mM.
  • Number of key binding residues: 4 (TRP248, ASP184, LEU247, and GLU164).

Sources:

  • Rhus chinensis Mill Derived Anti-Allergic Ingredients Screening Using MAS-Related G Protein-Coupled Receptor X2 Cell Membrane Chromatography. Biomedical Chromatography, 2025; 39(10).
  • Wiley-Blackwell - www.wiley.com/
  • Onlinelibrary.wiley.com/journal/10.1002/(ISSN)1099-0801
  • Xi'an Jiaotong University, School of Pharmacy, Health Science Center.