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.

Curcumin and dietary polyphenol research: beyond drug discovery

“…This, along with other chemistry features of curcumin, has generated enormous difficulties in the detailed dissection of mechanistic pathways underlying its bio-medical functions. Indeed, these features have been causing some confusion among drug developers and have been heavily debated recently [82][83][84][85] . However, investigations presented by numerous investigators, including our team, suggest that the implications of dietary polyphenol research are beyond the scope of drug development.…”

Attenuation of Pathogenicity in Candida albicans by Application of Polyphenols

“…In vitro, curcumin inhibits certain epigenetic enzymes (the histone deacetylases: HDAC1, HDAC3, HDAC8), transcriptional co-activator proteins [14]. Its analogues enjoy a range of biological activities such as antimicrobial, antioxidant, cytotoxic, anticancer, antiprotozoal, antihistaminic, antiulcer and anti-inflammatory activities which makes these compounds as special attraction for investigation.…”

Curcumin – A review on multipotential phytocompound

“…and Leishmania major [5]. Curcumin might be beneficial by acting against gut microbiota thus evading the condition for systemic circulation [28]. The gut microbiota also plays a significant part in curcumin metabolism and its bio-transformation because the microbiota is proficient at converting curcumin formulations into a range of catabolites [29].…”