Screening licorice for H2 receptor-binding anti-ulcer components using affinity chromatography

Area of Science:

• Pharmacology
• Biochemistry
• Analytical Chemistry

Background:

• Histamine H2 receptor (H2R) is a key therapeutic target.
• Efficient drug screening methods are urgently needed.
• Current methods lack detailed binding mode analysis.

Purpose of the Study:

• To develop an innovative H2R-based chromatography technique for rapid drug screening.
• To identify and characterize bioactive compounds from complex matrices.
• To elucidate the binding interactions of identified compounds with H2R.

Main Methods:

• Immobilized H2R chromatography column preparation.
• Kinetic interaction analysis of ligands with H2R.
• High-performance liquid chromatography coupled with ion trap mass spectrometry (HPLC-IT-MS) for compound identification.
• Competitive displacement assays and molecular docking simulations.

Main Results:

• Successfully screened and identified liquiritin as a bioactive compound.
• Demonstrated that liquiritin competes with nizatidine and ranitidine for H2R binding sites.
• Observed unique binding interactions of famotidine with H2R, distinct from other ligands.
• Elucidated the molecular mechanisms behind observed drug-receptor interactions.

Conclusions:

• The established H2R receptor chromatography model effectively screens bioactive components and determines binding modes.
• This method provides a foundation for screening traditional Chinese medicine compounds.
• Preliminary insights into the mechanisms of action of screened compounds were obtained.