Effect of non-steroidal anti-inflammatory drugs (NSAIDS) on glycosyltransferase activity from human osteoarthritic cartilage.
The effect of non-steroidal anti-inflammatory drugs (NSAIDs) on the activity of glycosyltransferases required for the synthesis of the polysaccharide chains of proteoglycans, was studied in human osteoarthritic cartilage in vitro. Using exogenous acceptors, salicylate and indomethacin suppressed the activity of glucuronyl- and xylosyltransferases in a concentration-dependent manner, but had little effect on N-acetylgalactosaminyl- and galactosyltransferases. When used at a concentration derived from the values found in the synovial fluid, salicylate, indomethacin and chloroquine significantly suppressed the activity of glucuronyl- and xylosyltransferases, while tiaprofenic acid, paracetamol (acetaminophen), floctafenine, ketoprofen, ibuprofen and tenoxicam had no effect on the enzymes. An alteration of some glycosyltransferases could explain the reported suppressive effect of some NSAIDs on cartilage proteoglycan synthesis.
David
M J
MJ
Department of Biochemistry, Claude Bernard University, Lyon, France.
Vignon
E
E
Peschard
M J
MJ
Broquet
P
P
Louisot
P
P
Richard
M
M
D000368:Aged; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D002358:Cartilage, Articular / Q000187:drug effects* / Q000201:enzymology; D002738:Chloroquine / Q000494:pharmacology; D003864:Depression, Chemical; D005260:Female; D014453:Glucuronosyltransferase / Q000187:drug effects / Q000378:metabolism; D016695:Glycosyltransferases / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D008875:Middle Aged; D010003:Osteoarthritis / Q000201:enzymology*; D010430:Pentosyltransferases / Q000187:drug effects / Q000378:metabolism; D011422:Propionates / Q000494:pharmacology; D011509:Proteoglycans / Q000096:biosynthesis; D012459:Salicylates / Q000494:pharmacology; D000097608:UDP Xylose-Protein Xylosyltransferase
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002738:Chloroquine; D014453:Glucuronosyltransferase; D016695:Glycosyltransferases; D007213:Indomethacin; D010430:Pentosyltransferases; D011422:Propionates; D011509:Proteoglycans; D012459:Salicylates; D000097608:UDP Xylose-Protein Xylosyltransferase; C021270:tiaprofenic acid