Antioxidant, antiinflammatory and antiinvasive activities of biopolyphenolics

Shashwat Malhotra, Gaurav Shakya, Ajit Kumar, Barbara W. Vanhoecke, Ashok L. Cholli, Hanumantharao G. Raj, Luciano Saso, Balaram Ghosh, Marc E. Bracke, Ashok K. Prasad, Shyam Biswal, Virinder S. Parmar

Research output: Contribution to journalReview articlepeer-review

25 Scopus citations


A large number of polyphenolic and heterocyclic compounds, i.e. 4-methylcoumarins, 4-methylthionocoumarins, xanthones, pyrazoles, pyrazolylacrylonitriles, flavones and isoflavones have been tested for their antioxidant activity towards NADPH-catalysed liver-microsomal lipid peroxidation with a view to establish their structure-activity relationship. Inhibition of microsomal lipid peroxidation by 7,8-dihydroxy-4-methylcoumarin (DHMC, 2) and 7,8-diacetoxy-4-methylcoumarin (DAMC, 3) was intriguing. We also found that dihydroxy and diacetoxy derivatives of 4-methylthionocoumarin were more potent in comparison to the corresponding coumarin derivatives in inhibiting TNF-α induced expression of ICAM-1. The effect of nine different xanthones has been examined on the modulation of cytokine-induced expression of ICAM-1 in human endothelial cells. 1,4-Dihydroxyxanthone (10) showed enhanced antioxidant activity as well as the inhibition of the expression of cell adhesion molecules, such as ICAM-1, VCAM-1 and E-selectin on endothelial cells in a concentration and time dependent manner. Antioxidant activity of different pyrazoles and pyrazolylacrylonitriles and antiinvasive activity of flavones and isoflavones against solid tumors have also been studied.

Original languageEnglish (US)
Pages (from-to)119-139
Number of pages21
Issue number6
StatePublished - Jun 15 2008


  • Coumarins
  • Flavones and isoflavones
  • Reactive oxygen species
  • Xanthones

ASJC Scopus subject areas

  • Organic Chemistry


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