Biological targeting or molecular targeting is the main strategy in drug development and disease prevention. However, the problem of "off-targets" cannot be neglected. Naturally derived drugs are preferred over synthetic compounds in pharmaceutical markets, and the main goals are high effectiveness, lower cost, and fewer side effects. Single-target drug binding may be the major cause of failure, as the pathogenesis of diseases is predominantly multifactorial. Naturally derived drugs are advantageous because they are expected to have multitarget effects, but not off-targets, in disease prevention or therapeutic actions. The capability of phytochemicals to modulate molecular signals in numerous diseases has been widely discussed. Among them, stilbenoids, especially resveratrol, have been well-studied, along with their potential molecular targets, including AMPK, Sirt1, NF-κB, PKC, Nrf2, and PPARs. The analogues of resveratrol, pterostilbene, and hydroxylated-pterostilbene may have similar, if not more, potential biological targeting effects compared with their original counterpart. Furthermore, new targets that have been discussed in recent studies are reviewed in this paper.
Keywords: 3′-hydroxypterostilbene; molecular targets; pterostilbene; resveratrol; stilbenoids.