Curcumin Derivatives as Allosteric Modulator of α7-nAChR: Functional and Molecular Docking Insights.

UNLABELLED: <p>

Background

Curcumin has emerged as promising candidate for therapeutic modulation of neurodegenerative disorders by acting on α7-nicotinic acetylcholine receptor (α7-nAChR).

OBJECTIVE

This study aimed to evaluate the potential of curcumin metabolites and derivatives as positive allosteric modulators (PAMs) of α7-nAChR.

MATERIALS AND

METHODS

Functional properties of α7-nAChR were assessed using two-electrode voltage clamp techniques in Xenopus oocytes, and molecular docking studies were employed to identify high-affinity binding sites.

RESULTS

The findings reveal that curcumin metabolites and derivatives also potentiate α7-nAChR and interact with a common transmembrane domain binding site on α7-nAChR, demonstrating potent modulatory effects. Notably, these derivatives exhibit superior binding energies compared to the established PAM PNU-120596.

CONCLUSION

The study underscores the therapeutic potential of curcumin metabolites and derivatives as receptor-specific natural agents for managing neurodegenerative and inflammatory diseases. </p>.