A Review on Pharmacological Diversity of Chalcone Derivatives

About Authors:
Hardwari L. Yadav, P.K. Singour, R.S. Pawar, U. K. Patil
Department of Pharmaceutical Chemistry,
VNS Institute of Pharmacy,

Neelbud, Bhopal (M.P.)

Chalcone are the important constituent of many natural sources and have variety of biological activities. The novel chalcone derivatives isolated from the fruits of Mallotus philippinensis called mallotophilippens. The chalcones are synthesize by claisen-schmidt base catalyzed condensation of appropriate aromatic ketones or substituted aromatic ketones with benzaldehyde or substituted benzaldehydes. Chalcones, considered as the precursors of flavonoids and isoflavonoids, are abundant in edible plants, and have also been shown to display a diverse array of pharmacological activities. Recent reports suggest antimicrobial activity of chalcones (antibacterial and antifungal), as well as antileishmanial, antimalarial, antiviral and anti-inflammatory activities of these compounds.

Reference ID: PHARMATUTOR-ART-1164

Chalcones considered as the precursors of flavonoids and isoflavonoids are abundant in edible plants and have also been shown to display a diverse array of pharmacological activities. Chalcones or 1, 3-diaryl-2-propen-1-ones belong to the flavonoid family. Chemically they consist of open-chain flavonoids in which the two aromatic rings are joined by a three-carbon α, ß-unsaturated carbonyl system. Chalcones have been reported to possess many useful properties, including anti-inflammatory, antimicrobial, antifungal, antioxidant, cytotoxic, antitumor and anticancer, antimalarial, antileishmanial, antidiabetic activities. The presence of α β unsaturated ketone group in chalcone is responsible for their different activities.1, 2

A number of chalcone derivatives, have also been found to inhibit several important enzymes in cellular systems, including xanthine oxidase, aldose reductase, epoxide hydrolase, protein tyrosine Kinase,and quinone reductase.3

2. Anti-inflammatory properties
Inflammatory stimulation, macrophages produce NO, prostanoids and proinflammatory cytokines such as interleukin (IL)-1b and TNF-α. NO is generated by NO synthase (NOS) and induces tissue injury at the inflammatory site. Three isoforms of NOS have been identified; endothelial (eNOS), neuronal NOS (nNOS) and inducible NOS (iNOS). Among the three, iNOS is expressed in response to various inflammatory stimuli and causes a large amount of NO to be produced by macrophages during the inflammatory process. TNF-α is one of the most important proinflammatory cytokines and is produced mainly by activated monocytes and macrophages. It induces various biological responses including tissue injury, shock and apoptosis. TNF- α also induces the secretion of cytokines such as IL-1, IL-6 and IL-10, and activates T cells and other inflammatory cells.6

The inhibition of prostaglandin E2 (PGE2) and nitric oxide (NO) production has been proposed as a potential therapy for different inflammatory disorders. Large amounts of NO may lead to tissue damage. In inflammatory diseases such as rheumatoid arthritis, excessive NO production by activated macrophages has been observed. Therefore, it would be interesting to develop potent and selective inhibitors of NO for potential therapeutic use. Chalcone derivatives show anti-inflammatory activity by inhibit the cyclooxygenase (Cox), nitric oxide synthase enzyme and tumor necrosis factor-α.1, 4, 5 

The pathway of release of different chemical mediators responsible for inflammation is given in figure 1.

Chemical structure of 2’ hydroxychalcone derivatives5


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