Thienopyrimidine derivatives prevent cartilage destruction in articular disease.
The effects of a series of thienopyrimidine derivatives on the prevention of cartilage destruction in articular disease were investigated. Anti-degenerative activity was assayed on culture of nasal pig cartilage in the presence or in the absence of interleukin 1beta (IL-1beta). The amount of glycosaminoglycans (GAGs) and the production of nitric oxide (NO) in the culture medium were determined. Some thienopyrimidine derivatives, in the presence of IL-beta, blocked the cartilage breakdown by inhibiting both the NO production and GAGs release in a dose-dependent manner.
Cardile APV
Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Catania, Italy. panico@mbox.unict.it
Santagati
A
A
Gentile
B
B
D000818:Animals; D002357:Cartilage Diseases / Q000188:drug therapy* / Q000517:prevention & control; D002358:Cartilage, Articular / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D006025:Glycosaminoglycans / Q000378:metabolism; D007375:Interleukin-1 / Q000494:pharmacology; D009569:Nitric Oxide / Q000378:metabolism; D011743:Pyrimidines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013440:Sulfides / Q000138:chemical synthesis / Q000494:pharmacology*; D013552:Swine
D006025:Glycosaminoglycans; D007375:Interleukin-1; D011743:Pyrimidines; D013440:Sulfides; C476003:thienopyrimidine; D009569:Nitric Oxide