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. 2015 Oct 1;5:14782. doi: 10.1038/srep14782

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Copyright © 2015, Macmillan Publishers Limited

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(A) None of the NSAIDs ibuprofen, diclofenac, and indometacin showed any agonistic or competitive antagonistic activity in the full-length FXR reporter gene assay. Compounds were assessed at 10 or 30 μM alone and in competition with GW4064 (3 μM), OCA (3 μM) and CDCA (20 μM). (B) The increased relative activity of NSAIDs when combined with OCA (3 μM) (suggestive of FXR agonism) does not result from increased reporter (firefly luciferase) activity but from a toxicity driven decrease in the activity of the control gene (renilla luciferase). The effect does therefore not represent an (agonistic) activity on FXR. (C) Western blotting on β-actin confirms the toxic activity of OCA and NSAIDs in combination (normalized on cell number). (*p < 0.05; **p < 0.01; ***p < 0.001).