Asian Science Citation Index is committed to provide an authoritative, trusted and significant information by the coverage of the most important and influential journals to meet the needs of the global scientific community.  
ASCI Database
308-Lasani Town,
Sargodha Road,
Faisalabad, Pakistan
Fax: +92-41-8815544
Contact Via Web
Suggest a Journal
International Journal of Pharmacology
Year: 2005  |  Volume: 1  |  Issue: 1  |  Page No.: 79 - 84

Inhibitory Activities of New Series of 4, 5-diaryl Thiadiazoles Derivatives on Lipopolysaccharide-induced Cox-2 Expression

Seyed Nasser Ostad, Mohsen Amini, Zahra Haghipour, Leila Karimi and Latifeh Navidpour    

Abstract: Recent studies have suggested cyclooxygenase-2 (COX-2) expression as a mechanism involved in carcinogenesis. It has also been suggested that changes in COX-2 expression level can be considered as a possible therapeutic target in tumors. Therefore, it was decided to synthesize a new series of 4, 5-diaryl thiadiazoles (compounds 1-5) as COX-2 inhibitors and evaluate their inhibitory activity on COX-2 expression. The COX-2 expression was induced by lipopolysaccharide (LPS) in bovine aortic endothelial (BAE-1) cells and the protein expression was evaluated by immunocytochemistry (ICC). The inhibitory activity of these compounds has been compared with celecoxib and rofecoxib as selective COX-2 inhibitors and indomethacin as a non-selective COX inhibitor. The cytotoxicity of these compounds was measured in different concentrations (10-3 -103 μg mL-1 ) by trypan blue dye exclusion method. The results showed that the cell viability following exposure to 10-2 μg mL-1 of each one of compounds 1-4 was about 90%. Among all tested compounds, compound 4 at 10-2 μg mL-1 showed significant inhibition on COX-2 expression determined by ICC. This effect of compound 4 was comparable to rofecoxib and celecoxib. It is concluded that, the new synthesized compounds and in particular, the compound 4 can be considered for further evaluation as new COX-2 inhibitors.

Cited References   |    Fulltext    |   Related Articles   |   Back
  Related Articles

Copyright   |   Desclaimer   |    Privacy Policy   |   Browsers   |   Accessibility