Rubone (2'-Hydroxy-2,4,4',5,6'-pentamethoxychalcone), a natural product and a modulator of miR-34a (microRNA-34), upregulates miR-34a expression in a p53-dependent manner, which in turn downregulates the expression of downstream targets Bcl-2, cyclin-D1, CDK6, SIRT1, and FOXP1, thereby inhibiting tumor growth and reversal of hepatocellular carcinoma (HCC) and chemoresistance in prostate cancer.

Methods: DU145-TXR and PC3-TXR cells were treated with Rubone (5, 10 μM, 48 hours) and protein expression was measured.
Results: Rubone significantly reversed the expression of miR-34a downstream gene targets in DU145-TXR and PC3-TXR cell lines. [1]

Methods: Rubone (20, 50 mg/kg, gavage, once every two days, 24 days) was used to treat HepG2 xenograft nude mice. Tumor volume and body weight were measured every 2 days. Mice were sacrificed and tumor tissues were collected for subsequent RNA extraction or tissue sections were sliced ​​and the expression levels of pri-miR34a, miR34a, cyclin D1, and Bcl-2 in xenograft tumors were measured by qRT-PCR.
Results: Rubone delayed tumor growth by 78.27% and 89.64% at doses of 20 and 50 mg/kg, respectively. Pri-miR34a and miR34a levels were upregulated in mouse xenograft tumors, while cyclin D1 and Bcl-2, which are targeted by miR34a, were downregulated. [4]