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Article Publish Status: FREE
Abstract Title:

Eckol as a Potential Therapeutic against Neurodegenerative Diseases Targeting Dopamine D₃/D₄ Receptors.

Abstract Source:

Mar Drugs. 2019 Feb 10 ;17(2). Epub 2019 Feb 10. PMID: 30744179

Abstract Author(s):

Pradeep Paudel, Su Hui Seong, Sangwook Wu, Suhyun Park, Hyun Ah Jung, Jae Sue Choi

Article Affiliation:

Pradeep Paudel

Abstract:

The G protein-coupled receptor (GPCR) family of proteins comprises signaling proteins that mediate cellular responses to various hormones and neurotransmitters, and serves as a prime target for drug discovery. Towards our goal of discovering secondary metabolites from natural sources that can function as neuronal drugs, we evaluated the modulatory effect of eckol on various GPCRs via cell-based functional assays. In addition, we conducted in silico predictions to obtain molecular insights into the functional effects of eckol. Functional assays revealed that eckol had a concentration-dependent agonist effect on dopamine D₃ and D₄ receptors. The half maximal effective concentration (EC) of eckol for the dopamine D₃ and D₄ receptors was 48.62 ± 3.21 and 42.55 ± 2.54 µM, respectively, while the ECvalues of dopamine as a reference agonist for these two receptors were 2.9 and 3.3 nM, respectively. In silico studies revealed that a low binding energy in addition to hydrophilic, hydrophobic,π⁻alkyl, and π⁻π T-shaped interactions are potential mechanisms by which eckol binds to the dopamine receptors to exert its agonist effects. Molecular dynamics (MD) simulation revealed that Phe346 of the dopamine receptors is important for binding of eckol, similar to eticlopride and dopamine. Our results collectively suggest that eckol is a potential D₃/D₄ agonist for the management of neurodegenerative diseases, such as Parkinson's disease.

Study Type : In Vitro Study

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