Ibuprofen (NSC 256857)

2 years -80 in solvent

Taken orally every day

Bladder epithelial cell line T24, RT-4 transitional cell papilloma bladder cell line, 5637 primary carcinoma bladder cell line, HCT-116, MDAMB231, MCF7, HEK293, A549, SKOV3 and DU145

Dissolved in DMSO at a concentration of 200 mM for making the stock solution, final concentration ca.2 mM

Dissolved in DMSO and diluted in saline

Ibuprofen works by inhibiting the enzyme cyclooxygenase COX-1 and COX-2, which convert arachidonic acid to prostaglandin H2 (PGH2). Its action is similar to aspirin, indomethacin and all other NSAIDs in intact cells, broken cells, and purified enzyme preparations. [1] Ibuprofen inhibits the constitutive activation of NF-kappaB and IKKalpha in the androgen-independent prostate tumor cells PC-3 and DU-145. It sensitizes prostate cells to ionizing radiation and blocks stimulated activation of NF-kappaB following exposure to TNFalpha or ionizing radiation in the androgen-sensitive prostate tumor cell line LNCaP. Both of these cannot be attributed directly to inhibition of IkappaB-alpha kinase but to inhibition of an upstream regulator of IKKalpha. [2] Ibuprofen exerts an anticancer effect by reducing survival of cancer cells. Ibuprofen is more efficacious than aspirin and acetaminophen, and comparable with (R)-flurbiprofen and indomethacin in induction of p75NTR protein (a tumor and metastasis suppressor) expression in cell lines from bladder and other organs. [3]

48 hours

Each cell line is incubated with Ibuprofen of various concentrations for 48 hours. Cell survival is estimated by the MTT assay, and cell death is determined by Hoechst staining used to distinguish between intact cell nuclei and fragmented nuclei undergoing cell death. Cells are lysed and analyzed by western blotting for detection of the p75NTR protein.

Ibuprofen (NSC 256857, Dolgesic) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50 of 13 μM and 370 μM, respectively.