RXRgamma and PPARgamma ligands in combination to inhibit proliferation and invasiveness in colon cancer cells

Published on Thursday, 29 October 2015


Nuclear retinoid X receptors (RXRs) and peroxisome proliferator-activated receptors (PPARs are potential candidates as drug target for cancer prevention and treatment.

We investigated if the rexinoid 6-OH-11-O-hydroxyphenantrene (IIF) potentiates the antitumoral properties of PPARgamma ligands as ciglitazone and pioglitazone, on two colon cancer cell lines: HCA-7 and HCT-116.

Drugs inhibited cell growth and induced apoptosis synergistically.

The combination resulted in a decrease of cyclooxigenase-2, metalloproteinases-2 and -9 expression level and activity while PPARgamma, RXRgamma and tissue inhibitors of metalloproteinase-1 and -2 expression were increased.

Finally, IIF potentiated PPAR transcriptional activity by enhancement of peroxisome proliferator response elements transactivation.



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See also All-Trans-Retinoic Acid (ATRA - analogues and/or derivatives).