3,5,3′,4′,5′-Pentamethoxystilbene (MR-5), a Synthetically Methoxylated Analogue of Resveratrol, Inhibits Growth and Induces G1 Cell Cycle Arrest of Human Breast Carcinoma MCF-7 Cells

• DOI: 10.1021/jf903067g
• Publication Date: 2009-11-16T18:58:10Z
• Authors: Min-Hsiung Pan; Chih-Li Lin; Jie-Heng Tsai; Chi-Tang Ho; Wei-Jen Chen
• Keywords: MCF-7

3,5,3′,4′,5′-Pentamethoxystilbene (MR-5) is a synthetically methoxylated analogue of resveratrol and has been suggested to have antitumor activity because structural similarity resveratrol. Herein, we investigate the antiproliferative effect MR-5 in human breast cancer MCF-7 cells demonstrate that had more potent inhibition on cell growth compared with other derivatives. Exploring growth-inhibitory mechanisms MR-5, found it accompanied by G1 cycle arrest, which coincides marked regulatory proteins, including decreased cyclins (D1/D3/E) cyclin-dependent kinases (CDK2/4/6) increased CDK inhibitors (CKIs) such as p15, p16, p21, p27. Furthermore, increase CKI levels resulted concomitant their interactions CDK4 CDK2, along strong kinase accumulation hypophosphorylated Rb. also modulated some critical activities related regulation, Akt, mitogen-activated protein (ERK1/2), p38 (p38 MAPK), focal adhesion (FAK) cells. In total, our results affects multiple cellular targets contribute its provide novel information for synthetic chemists design new agents introduction group(s) basic compound.