Novel Curcumin Derivatives: Targeted for Anti-Inflammatory Activity
Abstract
Curcuminwhich is commonly used as a spice is also well documented as the golden nutraceutical which is chemically called as diferuloylmethane. Numerous studies have indicated that curcumin is a highly potent antimicrobial agent and has been shown to be active against various chronic diseases including various types of cancers, diabetes, obesity, cardiovascular, pulmonary, neurological and autoimmune diseases. Recently the study has been reported thatthe curcumin also act as an Anti-inflammatory agent by the inhibition of eicosanoids generating enzyme including phospholipase A2, cyclooxygenases and lipoxygenases. In this article we have reported the synthesis and evaluation of novel curcumin derivatives (1, 7-bis(4-(3-substituted) benzoyloxy-3 mthoxyphenyl)hepta-1, 6-diene-3, 5-dione) asanti-inflammatory agents. The chemical structures of the synthesized compounds were verified on the basis of spectral data and elemental analysis. In vitroAntiinflammatory activity was determined by using Plethysmometer with Paw volume method by using Celecoxib as standard. The molecular docking studies were also carried out by V Life MDS software into the active site of COX-2 enzymes (PDB ID: 3NL1). The compounds 2g and 2j haveshown to be good anti-inflammatory agent with highest docking scores with-4.0083, -3.9576 and 54.61%, 50.46% inhibition respectively compared with 53.46% inhibition of standard Celecoxib. The anti-inflammatory activity and docking results highlighted the fact, that the value of curcumin as a nutraceutical can be increases through thechemical modification.
Keywords
Curcumin, Nutraceutical, Molecular docking, Anti-inflammatory, COX-2 enzyme