Rheumatology 1999; 38: 1088-1093
© 1999 British Society for Rheumatology
Apocynin, a plant-derived, cartilage-saving drug, might be useful in the treatment of rheumatoid arthritis
Department of Rheumatology and Clinical Immunology, University Medical Centre Utrecht, PO Box 85500, 3508 GA Utrecht and
1 Department of Medicinal Chemistry, Faculty of Pharmacy, Utrecht University, The Netherlands
Correspondence to:
F. P. J. G. Lafeber, Department of Rheumatology and Clinical Immunology (F02.127), University Medical Centre Utrecht, PO Box 85500, 3508 GA Urecht, The Netherlands.
Objective. To investigate whether apocynin, 1-(4-hydroxy-3-methoxyphenyl)ethanone, is able to diminish inflammation-induced cartilage destruction in rheumatoid arthritis (RA), studied in a human in vitro model.
Methods. Apocynin was added to cultures of RA peripheral blood mononuclear cells (PBMNC). Cartilage-destructive activity was determined by addition of culture supernatant to tissue samples of human articular cartilage. In addition, the proliferation of PBMNC, their production of tumour necrosis factor alpha (TN-F
), interleukin (IL)-1 and IL-10, and T-cell production of interferon gamma (IFN-
) and IL-4, as measures for T1 and T2 cell activity, were determined.
Results. Apocynin was able to counteract RA PBMNC-induced inhibition of cartilage matrix proteoglycan synthesis, while no effect on inflammation-enhanced proteoglycan release was found. The effect was accompanied by a decrease in IL-1 and TNF-
production by the MNC. No effect on T-cell proliferation was found, but the production of IFN-
, IL-4 and T-cell-derived IL-10 was strongly diminished. Most important, apocynin did not show any direct adverse effects on chondrocyte metabolism; on the contrary, it diminished the release of proteoglycans from the cartilage matrix.
Conclusion. Apocynin in vitro inhibits inflammation-mediated cartilage destruction without having adverse effects on cartilage. The latter may be an advantage of apocynin over many other non-steroidal anti-inflammatory drugs. Therefore, apocynin might have an added beneficial effect in protecting RA patients from joint destruction.
KEY WORDS: Apocynin, Rheumatoid arthritis, Non-steroidal anti-inflammatory drugs, Cartilage
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