Chalcone or (E)-1,3-diphenyl-2-propene-1-one scaffold has gained considerable scientific
interest in medicinal chemistry owing to its simple chemistry, ease in synthesizing a variety of
derivatives and exhibiting a broad range of promising pharmacological activities by modulating
several molecular targets. A number of natural and (semi-) synthetic chalcone derivatives have
demonstrated admirable anti-inflammatory activity due to their inhibitory potential against various
therapeutic targets like Cyclooxygenase (COX), Lipooxygenase (LOX), Interleukins (IL), Prostaglandins
(PGs), Nitric Oxide Synthase (NOS), Leukotriene D4 (LTD4), Nuclear Factor-κB (NF-
κB), Intracellular Cell Adhesion Molecule-1 (ICAM-1), Vascular Cell Adhesion Molecule-1
(VCAM-1), Monocyte Chemoattractant Protein-1 (MCP-1) and TLR4/MD-2, etc. The chalcone
scaffold with hydroxyl, methoxyl, carboxyl, prenyl group and/or heterocyclic ring substitution like
thiophene/furan/indole showed promising anti-inflammatory activity. In this review, a comprehensive
study (from the year 1991 to 2016) on multi-targets of inflammatory interest, related inflammation
reactions and their treatment by chalcone-based inhibitors acting on various molecular targets
entailed in inflammation, Structure-Activity Relationships (SARs), Mechanism of Actions
(MOAs), and patents are highlighted.
Erythromycin exerts in vivo
anti-inflammatory activity downregulating cell adhesion molecule expression
