doi:10.1038/nindia.2009.281 Published online 30 August 2009
Researchers have designed a new class of organic compounds that are structurally close to curcumin and can check inflammation1.
In studies with human umbilical vein endothelial cells, they found that one of the organic compounds looks promising and works better than curcumin in stopping inflammatory flare-ups.
Cell surface proteins known as inter-cellular adhesion molecule -1 (ICAM-1) are highly expressed on leukocytes (a type of white blood cells) during inflammation. Curcumin containing beta-diketones stifles the expression of ICAM-1. But curcumin has drawbacks such as poor bioavailability and toxicity on cells.
To overcome this, the researchers synthesized 4-Acyl-5-pyrazolones, a class of asymmetric beta-diketones that differ from curcumin as they lack some functional organic groups. They studied the efficacy of the compounds with human umbilical vein endothelial cells (HUVEC) and compared them with their metal derivatives.
The tested compounds were found to be non-toxic. Of all the compounds, 4-benzoyl-3-methyl-1-phenyl-pyrazol-5-one is the best to inhibit inflammation in HUVEC.
"This compound is less toxic than curcumin," says Balaram Ghosh, one of the researchers. This research may lead to developing better anti-inflammatory molecules using the best inhibitor as a lead molecule, he concludes.
The authors of this work are from: Università di Roma 'La Sapienza'and Vecchio Istituto Chimico, Piazzale Aldo Moro, Rome; Università di Camerino, Camerino (MC), Italy; Vassar College, Poughkeepsie, NY, USA; and Institute of Genomics and Integrative Biology, Delhi, India.
Caruso, F. et al. Inhibitory effect of b-diketones and their metal complexes on TNF-a induced expression of ICAM-1 on human endothelial cells. Bioorg. Med. Chem. 17, 6166-6172 (2009) | Article |