ABSTRACT Resveratrol (3,5,4’-trans-trihydroxystilbene, RV) is a phytoalexin produced by a variety of plants in response to stress. In vivo and in vitro studies have highlighted its anti-inflammatory, antioxidant, antiaging, chemopreventive and chemotherapeutic properties. A number of RV analogues have been synthesized/isolated to improve the efficacy of the lead compound. We tested a wide range of concentrations of RV and its analogue 3,5,4’-trans-trimethoxystilbene (TRV), a natural stilbene present in five different plants, on human prostate cancer cell lines (DU145), examining growth inhibition, cell cycle progression, sirtuins’ activity and DNA damage. Employing half the concentration of TRV compared to a given concentration of RV proved to be more efficient than the lead compound in eliciting the chemotherapeutic effects, by inhibiting DU145 cell growth, inducing DNA damage, decreasing both the percentage of cells in G1 phase and sirtuins’ activity. We hypothesize that methoxy substitution in 3,5,4’ in the stilbene rings, ameliorates lipophilicity of TRV, thus increasing the cytotoxic effect on DU145. The data we found encouraged us both to investigate on new synthetic compounds and to utilize stilbenoids, in particular TRV, as chemotherapeutic agents.
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