Resveratrol (Res), a natural polyphenol compound found in grapes and red wine has been shown to exhibit anti-tumor, anti-oxidant and anti-inflammation effects. However, the molecular targets as well as mechanisms of action contributing to the health promoting effects of Res are largely unknown. In our study, through dietary or pharmaceutical consumption levels, we investigated the effects of Res on inflammation-driven immune responses in human THP-1 monocytes and human Phorbol 12-myristate 13-acetate (PMA) differentiated THP-1-derived (P-THP-1) macrophages. Our results showed that Res induced anti-proliferation in THP-1 monocytes with S phase arrest at dietary concentrations, and, however, induced cell apoptosis and caused G0/G1 phase arrest at pharmaceutical concentrations. In addition, Res showed different effects on pro-inflammatory cytokines in different cell lines. Furthermore, similar analysis on pterostilbene and genistein revealed the possible effect was attributed to specific stilbene structure. In conclusion, resveratrol and pterostilbene appeared to play different roles of inflammatory response in THP-1 and P-THP-1 cells.