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 (LC50 (trypan) similar to 1.3 mu M) and to TPS (LC50 trypan similar to 4.0 mu M and LC50 MTT similar to 8.3 mu M) than to RES (LC50 trypan similar to 8.9 mu M and LC50 MTT similar to 29.0 mu M), they were relatively resistant to TSO (LC50 trypan similar to 61.0 mu M and LC50 MTT > 100 mu M) and to TS (LC50 trypan >= 5.0 mu M and LC50 MTT >= 5.0 mu M). 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 (IC50 <= 25 mu M), these cells were resistant to growth inhibition by PIC (IC50 >= 50 mu M). 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.