Title:Curcumin: Structure-Activity Relationship Towards its Role as a Versatile Multi-Targeted Therapeutics
Volume: 14
Issue: 4
Author(s): Manika Awasthi, Swati Singh, Veda P. Pandey and Upendra Dwivedi*
Affiliation:
- Bioinformatics Infrastructure Facility, Center of Excellence in Bioinformatics, Department of Biochemistry, University of Lucknow, Lucknow-226007,India
Keywords:
Curcumin, β-dicarbonyl moiety, enone moeity, O-methoxy phenol, polypharmacology, structure-activity relationship.
Abstract: Curcumin, a polyphenolic pigment of turmeric, is one of the very promising natural products
that have been extensively investigated from both the biological and structural point of view. It has been
shown to possess activity towards variety of targets at cellular and molecular levels that provide a basis
for its use against multiple human diseases. In recent decades, it has been subjected to various pharmacological,
biochemical and clinical investigations which proposed its multifaceted therapeutic potential
being attributed mainly to its unique chemical structure and physicochemical properties. Thus, this review
discusses the structure-activity relationship of curcumin in relation to its biological activities to
gain more understanding on the mechanistic basis of its therapeutic action. Curcumin is a diferuloylmethane
molecule with two ferulic acid residues joined by a seven carbon methylene bridge. The three important
structural features of curcumin include two aromatic o-methoxy phenolic groups, β-dicarbonyl
moiety and a seven carbon linker containing two enone moeities. Extensive research in the last two decades
has provided evidence for the role of these different functional groups in its crucial biological activities.
In addition to this, the polypharmacology of curcumin may also be attributed to the unexpected
chemical diversity exhibited by its metabolites. Structural modifications in these specific functional
moeities of curcumin have led to the development of new analogues with improved physicochemical
properties and biological activity either by affecting its solubility, specificity or potency. Thus, the understanding
of such structure-activity relationship may impose the exploration of the range of its biological
activity.
