In Vitro evaluation of the cytotoxic and anti-proliferative properties of resveratrol and several of its analogs

Resveratrol (RES), a component of red wine, possesses anti-inflammatory properties. The studies described in the present work were aimed at evaluating the potential for RES and related stilbene analogs (piceatannol, PIC; pterostilbene, TPS; trans-stilbene, TS; and trans-stilbene oxide, TSO) to exhibit toxicity towards RAW 264.7 mouse macrophages. The effect of TS, TSO, RES and TPS on RAW 264.7 macrophage viability was determined by two standard methods: (a) the MTT assay and (b) the trypan blue dye exclusion test. Whereas macrophages were more sensitive to PIC (LC(50 trypan) ∼ 1.3 μM) and to TPS (LC(50 trypan) ∼ 4.0 μM and LC(50 MTT) ∼ 8.3 μM) than to RES (LC(50 trypan) ∼ 8.9 μM and LC(50 MTT) ∼ 29.0 μM), they were relatively resistant to TSO (LC(50 trypan) ∼ 61.0 μM and LC(50 MTT) > 100 μM) and to TS (LC(50 trypan) ≥ 5.0 μM and LC(50 MTT) ≥ 5.0 μM). The ability of selected stilbenes (RES, TPS and PIC) to exhibit growth inhibitory effects was also examined. Although RES and TPS were observed to inhibit cell proliferation in macrophages (IC(50) ≤ 25 μM), these cells were resistant to growth inhibition by PIC (IC(50) ≥ 50 μM). The data obtained in the present analysis demonstrate that substituted stilbene compounds such as RES have the capacity to exhibit cytotoxic and anti-proliferative activities in macrophages.