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The friend leukemia integration 1 (Fli-1) gene is involved in the expression control of key genes in multiple pathogenic/physiological processes, including cell growth, differentiation, and apoptosis; this implies that Fli-1 is a strong candidate for drug development. In our previous study, a 3',5'-diprenylated chalcone, (E)-1-(2-hydroxy-4-methoxy-3,5-diprenyl) phenyl-3-(3-pyridinyl)-propene-1-one ( C10 ), was identified as a novel anti-prostate cancer (PCa) agent. Here, we investigated the molecular mechanisms underlying the anti-cancer effects of C10 on the growth, metastasis, and invasion of PC3 cells in vitro. Our results show that C10 exhibited a strong inhibitory effect on proliferation and metastasis of PC3 cells via several cellular and flow cytometric analyses. Further mechanism studies revealed that C10 likely serves as an Fli-1 agonist for regulating the expression of Fli-1 target genes including phosphatidylinositol 3-kinase ( P110 ), murine double minute2 ( MDM2 ), B-cell lymphoma-2 ( Bcl-2 ), Src homology-2 domain-containing inositol 5-phosphatase 1 ( SHIP-1 ), and globin transcription factor-1 ( Gata-1 ) as well as the phosphorylation of extracellular-regulated protein kinases 1 ( ERK1 ). Further, we confirmed that C10 can regulate the expressions of vascular endothelial growth factor 1 ( VEGF-1 ), transforming growth factor-β2 ( TGF-β2 ), intercellular cell adhesion molecule-1 ( ICAM-1 ), p53, and matrix metalloproteinase 1 ( MMP-1 ) genes associated with tumor apoptosis, migration, and invasion. Thus, C10 exhibits stronger anticancer activity with novel molecular targets and regulatory molecular mechanisms, indicating its great potency for development as a novel targeted anticancer drug.

international journal of molecular sciences

Fli-1 Activation through Targeted Promoter Activity Regulation Using a Novel 3’, 5’-diprenylated Chalcone Inhibits Growth and Metastasis of Prostate Cancer Cells