Meloxicam

Meloxicam is a non-steroidal antiinflammatory agent that can pass through the blood-brain barrier, inhibits COX activity, with IC₅₀s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively. IC50 & Target:IC50: 0.49 µM (COX-2), 36.6 µM (COX-1)^[1] In Vitro:Meloxicam (Compound 5) is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC₅₀s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively^[1]. Meloxicam inhibits COX⁺ tumor cells, but shows no cytotoxicity on CF41.Mg or MDCK cells at 0.25-25 μg/mL. Furthermore, Meloxicam in combination with doxorubicin, has no synergistic effect on CF41.Mg cells. Meloxicam (0.25 μg/mL) decreases CF41.Mg cell migration and invasion, induces decrease in MMP-2 expression, and increases β-catenin phophorylation in CF41.Mg cells, but does not affect the CF41.Mg cell apoptosis^[2]. In Vivo:Meloxicam (10 mg/kg) alone or in combination with rutin significantly decreases paw liking time on 1st day by 55% and 49% compared with the formalin-treated group, respectively, however the combination reduces time non-significantly on 3rd day in mice. Meloxicam alone or in combination with rutin also decreases relative liver weights, reduces MDA contents, induces liver SOD activities, hampers IL-1β content, and significantly reduces the number of positive caspase-3 immunoreactive cells in mice^[3].