Polyphenols with Anti-Inflammatory Properties: Synthesis and Biological Activity of Novel Curcumin Derivatives

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dc.contributor.authorGonzález, Yisett
dc.contributor.authorMojica-Flores, Randy
dc.contributor.authorMoreno-Labrador, Dilan
dc.contributor.authorCubilla-Rios, Luis
dc.contributor.authorRao, K. S. Jagannatha
dc.contributor.authorFernández, Patricia L.
dc.contributor.authorLarionov, Oleg V.
dc.contributor.authorLakey-Beitia, Johant
dc.date.accessioned2023-02-24T14:08:43Z
dc.date.available2023-02-24T14:08:43Z
dc.date.issued2023-02-12
dc.date.updated2023-02-24T14:08:44Z
dc.description.abstractHerein, we describe the synthesis and evaluation of anti-inflammatory activities of new curcumin derivatives. The thirteen curcumin derivatives were synthesized by Steglich esterification on one or both of the phenolic rings of curcumin with the aim of providing improved anti-inflammatory activity. Monofunctionalized compounds showed better bioactivity than the difunctionalized derivatives in terms of inhibiting IL-6 production, and known compound 2 presented the highest activity. Additionally, this compound showed strong activity against PGE2. Structure–activity relationship studies were carried out for both IL-6 and PGE2, and it was found that the activity of this series of compounds increases when a free hydroxyl group or aromatic ligands are present on the curcumin ring and a linker moiety is absent. Compound 2 remained the highest activity in modulating IL-6 production and showed strong activity against PGE2 synthesis.
dc.description.departmentChemistry
dc.identifierdoi: 10.3390/ijms24043691
dc.identifier.citationInternational Journal of Molecular Sciences 24 (4): 3691 (2023)
dc.identifier.urihttps://hdl.handle.net/20.500.12588/1772
dc.rightsAttribution 4.0 United States
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectcurcumin
dc.subjectcurcumin derivatives
dc.subjectsuccinate
dc.subjectdifunctionalized
dc.subjectmonofunctionalized
dc.subjectcytokine
dc.subjectIL-6
dc.subjectPGE2
dc.subjectanti-inflammatory activity
dc.subjectstructure–activity relationship
dc.titlePolyphenols with Anti-Inflammatory Properties: Synthesis and Biological Activity of Novel Curcumin Derivatives
dc.typeArticle

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