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2017 ; 60
(5
): 1620-1637
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The Essential Medicinal Chemistry of Curcumin
#MMPMID28074653
Nelson KM
; Dahlin JL
; Bisson J
; Graham J
; Pauli GF
; Walters MA
J Med Chem
2017[Mar]; 60
(5
): 1620-1637
PMID28074653
show ga
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.