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Fig. 2 | Molecular Medicine

Fig. 2

From: 2′,3′,4′-Trihydroxychalcone changes estrogen receptor α regulation of genes and breast cancer cell proliferation by a reprogramming mechanism

Fig. 2

The synergistic effect of 2′,3′,4′-THC is selective for ERs. A U2OS cells cotransfected with GAL-TK-Luc and an expression vector for GAL4-DBD-full-length ERα were treated with 10 nM E2 and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. B U2OS cells cotransfected with GAL-TK-Luc and an expression vector for GAL4-DBD-ERα LBD were treated with 10 nM E2 and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. C U2OS cells cotransfected with ERE-TK-Luc and an expression vector for ERβ were treated with 10 nM E2 and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. D U2OS cells cotransfected with GRE-TK-Luc and human GR were treated with 10 nM dexamethasone (Dex) and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. E U2OS cells cotransfected with human tyrosine aminotransferase 3 (TAT3)-Luc reporter gene and human AR were treated with 10 nM dihydrotestosterone (DHT) and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. F U2OS cells cotransfected with TAT3-Luc and human PR-B were treated with 10 nM progesterone (Prog) and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. G U2OS cells cotransfected with PPAR-RE-Luc and human PPARγ were treated with 10 μM rosiglitazone (Ros) and 5 μM 2′,3′,4′-THC alone or in combination for 24 h. Luciferase activity was measured in cellular lysates with a luminometer. RLU is relative light units. The data shown are mean of triplicate samples ± SE. H, I 2′,3′,4′-THC does not alter PXR and CAR1 activity. H PXR and I CAR1 activity was assayed with Puracyp’s trademark stable reporter cell lines. RIF, Rifampicin is a PXR agonist. CITCO, 6-(4-Chlorophenyl)imidazo[2,1-b][1,3]thiazole-5-carbaldehyde O-(3,4-dichlorobenzyl)oxime is a CAR agonist

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