Jpn. J. Pharmacol. 85 (1), 101-104 (2001)

Rhein, an Active Metabolite of Diacerein, Suppresses the Interleukin-1a-Induced Proteoglycan Degradation in Cultured Rabbit Articular Chondrocytes

Tadafumi Tamura* and Kenji Ohmori

Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd., Shimotogari, Nagaizumi, Sunto, Shizuoka 411-8731, Japan
*Corresponding author. FAX: +81-559-86-7430

Abstract: Diacerein has proved to be effective in the treatment of osteoarthritis. We investigated the effects of rhein, an active metabolite of diacerein, on the degradation of recombinant human interleukin-1a (rhIL-1a)-induced proteoglycan and matrix metalloproteinases (MMPs) release from rabbit articular chondrocytes. Chondrocytes were treated for 24 h with rhein in the presence of rhIL-1a. Rhein suppressed the rhIL-1a-induced proteoglycan degradation. In addition, rhein decreased the rhIL-1a-induced proMMP-3 production and reduced the MMPs activity. These results suggested that diacerein might have a protective effect on proteoglycan degradation via the suppressive effect of rhein on the production of proMMPs.

Keywords: Diacerein, Rhein, Chondroprotection

Copyright The Japanese Pharmacological Society

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