Low
cancer survival rates and the serious side effects often associated with current chemotherapeutics highlight the need for new and effective nontoxic
anticancer agents. Since 1997 when Jang and colleagues first described
resveratrol's ability to inhibit
carcinogenesis, it has consistently proven effective at
tumor inhibition in diverse human
cancer models. This finding has raised the hope that
resveratrol would pioneer a novel class of nontoxic chemotherapeutics. As a consequence of initial basic and preclinical studies,
resveratrol is now being extensively promoted in the unregulated nutraceutical sector. However, some fundamental aspects of
resveratrol's action need to be understood before it can be developed into a clinically viable anticancer
drug. These areas pertain to the key mechanism(s) by which
resveratrol potentiates its antitumor effects. Current research suggests that these mechanisms might be through novel pathways, requiring an understanding of cellular uptake, sentinel targets, and in vivo
biological networks. The metabolism of
resveratrol and its bioavailability also warrant further consideration in light of recent in vitro and in vivo studies. Finally, we need to appreciate the sorts of information about
resveratrol that may translate between different disease entities. We present a critical discussion of these issues and suggest important experiments that could pave the way to the successful translation of
resveratrol to the clinic.