Work

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

Year: 2025

Type: article

Abstract: 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. .

Source: Medical Principles and Practice

DOI: 10.1159/000548995

Authors: Eslam ElNebrisi, Mohammad A. Ghattas, Noor Atatreh, Sonia Hasan, Murat Oz

Institutions: United Arab Emirates University, Ras al-Khaimah Medical and Health Sciences University, Al Ain University, Kuwait University

Language: English

Topic: Nicotinic Acetylcholine Receptors Study

Subfield: Molecular Biology

Field: Biochemistry, Genetics and Molecular Biology

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: diamond

OpenAlex ID: W4415354175