Abstract
Curcumin has been reported to possess multifunctional bioactivities with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. Up to now, multiple approaches are being sought to overcome these limitations to obtaining “super curcumin”, and many analogues of curcumin have been designed and synthesized. In all of those analogues, a series of mono-carbonyl curcumin analogues deleting the β-diketone draw our attention. Since the seven-carbon β-diketone linker in curcumin may be responsible for its instability, the series of mono-carbonyl curcumin analogues deleting the β-diketone may be potential prodrug with improved pharmacokinetic and pharmacodynamic properties. This review just focuses on these more stable mono-carbonyl analogues of curcumin, and shows the new class of active structure by introducing the synthesis and anticancer activity of them.
Highlights
Curcumin,1,7-bis-(3-hydroxy-4-methoxyphenyl)-1,6-heptadiene-3,5-dione, (Figure 1) is a key active component in the traditional herb Curcuma Longa and has been used for centuries throughout Asia as a food additive, cosmetic, and as a traditional herbal medicine
Liang et al [22] have made some studies on in vitro stability and in vivo pharmacokinetic about a series of mono-carbonyl analogues of curcumin, and the results indicated that the stability of these mono-carbonyl analogues was greatly enhanced in vitro and their pharmacokinetic profiles were significantly improved in vivo
Liang et al [22] designed and synthesized a series of mono-carbonyl analogues of curcumin and examined their stability in vitro and pharmacokinetic in vivo, the results indicated that the stability of these mono-carbonyl analogues was greatly enhanced in vitro and their pharmacokinetic profiles were significantly improved in vivo
Summary
Curcumin,1,7-bis-(3-hydroxy-4-methoxyphenyl)-1,6-heptadiene-3,5-dione, (Figure 1) is a key active component in the traditional herb Curcuma Longa and has been used for centuries throughout Asia as a food additive, cosmetic, and as a traditional herbal medicine. As a spice, it provides curry with its distinctive color and flavor. Multiple approaches have been sought to overcome these limitations, and many analogues of have been designed and synthesized [10,11,12,13,14,15,16] Evidences from both in vitro and in vivo studies show that the β-diketone moiety is responsible for the instability and weak pharmacokinetic profiles of curcumin. This review will focus on these more stable mono-carbonyl analogues of curcumin
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