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The Essential Medicinal Chemistry of Curcumin.


ABSTRACT: Curcumin is a constituent (up to ?5%) of the traditional medicine known as turmeric. Interest in the therapeutic use of turmeric and the relative ease of isolation of curcuminoids has led to their extensive investigation. Curcumin has recently been classified as both a PAINS (pan-assay interference compounds) and an IMPS (invalid metabolic panaceas) candidate. The likely false activity of curcumin in vitro and in vivo has resulted in >120 clinical trials of curcuminoids against several diseases. No double-blinded, placebo controlled clinical trial of curcumin has been successful. This manuscript reviews the essential medicinal chemistry of curcumin and provides evidence that curcumin is an unstable, reactive, nonbioavailable compound and, therefore, a highly improbable lead. On the basis of this in-depth evaluation, potential new directions for research on curcuminoids are discussed.

SUBMITTER: Nelson KM 

PROVIDER: S-EPMC5346970 | biostudies-literature | 2017 Mar

REPOSITORIES: biostudies-literature

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The Essential Medicinal Chemistry of Curcumin.

Nelson Kathryn M KM   Dahlin Jayme L JL   Bisson Jonathan J   Graham James J   Pauli Guido F GF   Walters Michael A MA  

Journal of medicinal chemistry 20170111 5


Curcumin is a constituent (up to ∼5%) of the traditional medicine known as turmeric. Interest in the therapeutic use of turmeric and the relative ease of isolation of curcuminoids has led to their extensive investigation. Curcumin has recently been classified as both a PAINS (pan-assay interference compounds) and an IMPS (invalid metabolic panaceas) candidate. The likely false activity of curcumin in vitro and in vivo has resulted in >120 clinical trials of curcuminoids against several diseases.  ...[more]

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