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Merck

[Mechanisms of action of diacerein, the first inhibitor of interleukin-1 in osteoarthritis].

Presse medicale (Paris, France : 1983) (2004-07-01)
Marie Solignac
ABSTRACT

DEGRADATION AND REPAIR: Osteoarthritis generally occurs in a context of an overloaded normal cartilage matrix or normal loading of a vulnerable cartilage matrix. Interleukin-1 appears to be principally indicated in degradation phenomena while transforming growth factor (TGFbeta) is mainly implicated in phenomena of excessive synovial and chondrocyte repair observed at the same time as degradation. MECHANISMS OF ACTION OF DIACEREIN: Diacerein is a slow acting symptomatic treatment of osteoarthritis which has demonstrated efficacy on functional manifestations of osteoarthritis and on the structural component. Two mechanisms of action have been validated: in vitro inhibition of interleukin-1 (IL-1) synthesis, the main cytokine involved in cartilage destruction, and activity on the synthesis of proteoglycans, and hyaluronic acid, the principal component of cartilage. Other studies presented here have provided further details concerning other mechanisms of action of diacerein.

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Sigma-Aldrich
Diacerein, ≥95% (HPLC)
Diacerein, European Pharmacopoeia (EP) Reference Standard