TRK-530 is a novel bisphosphonate derivative. We examined the anti-inf
lammatory effects of TRK-530 on adjuvant arthritis (AA) rats. When TRK
-530 at a dose of 2.5 mg/kg was administered for 2 weeks to AA rats, i
t inhibited destructive changes in arthritic joints such as paw edema,
bone loss and joint degeneration. TRK-530 also inhibited splenomegaly
and suppressed the increase in serum sialic acid which is measured as
a systemic parameter of inflammation. To clarify the inhibitory mecha
nism of TRK-530, interleukin-1 (IL-1)-like activities of resident peri
toneal macrophages in AA rats given TRK-530 were compared with those o
f control rats. We found that TRK-530 inhibited IL-1-like activity ind
uced by bacterial lipopolysaccharide 6 weeks after administration when
the IL-1-like activities of control rats were still at high levels, T
hese findings suggest that TRK-530 exerts anti-inflammatory activities
in AA rats.