title: Divergent effects of suramin on in vitro and in vivo assays of cartilage degradation.
abstract: Proteinases are thought to be responsible for cartilage and bone erosion noted in chronic inflammatory conditions. Suramin [8-(3-benzamindo-4-meta-1-benzamindo)naphthalene-1,3,5-trisulfonic acid], 10(-5) and 10(-4) M, inhibited the release of a mouse macrophage-derived cartilage proteoglycan-degrading enzyme. At 10(-5) M it antagonized the activity of beta-glucuronidase and cathepsin D derived from the mouse macrophage, as well as similar enzymes secreted by rat macrophages in vivo. When cultured at 10(-4) M with rabbit knee cartilage, it antagonized the autolytic release of proteoglycan, indicating an inhibitory activity against a chondrocyte-derived neutral proteinase. After in vivo treatment at 10 mg/kg/day s.c., it was ineffective in preventing the cartilage and bone erosion noted in the adjuvant arthritic rat.
mesh_terms: D000818:Animals; D001169:Arthritis, Experimental / Q000378:metabolism / Q000473:pathology; D016282:Aspartic Acid Endopeptidases; D001862:Bone Resorption / Q000187:drug effects; D002358:Cartilage, Articular / Q000187:drug effects / Q000378:metabolism*; D003864:Depression, Chemical; D010450:Endopeptidases / Q000378:metabolism; D005260:Female; D008262:Macrophage Activation; D008264:Macrophages / Q000201:enzymology; D008297:Male; D051379:Mice; D011509:Proteoglycans / Q000378:metabolism; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013498:Suramin / Q000494:pharmacology*
chemical_list: D011509:Proteoglycans; D013498:Suramin; D010450:Endopeptidases; D016282:Aspartic Acid Endopeptidases