Regular moderate wine consumption is often associated with reduced morbidity and mortality from a variety of chronic diseases in which inflammation is the root cause. This review is focused on three of the numerous bioactive compounds present in wine: resveratrol, hydroxytyrosol and melatonin. Resveratrol and hydroxytyrosol are polyphenols. Melatonin, recently described in wine, is an indoleamine. Their structures, concentrations in wine, bioavailability, pharmacokinetic and health promoting properties are reviewed. Resveratrol seems to be one of the most promising compounds due to its bioactivity, with wine being the main source of resveratrol in diet. Hydroxytyrosol, which its main source in diet is olive oil has been also found in both red and white wine in considerable amounts. Melatonin has been found in wine in low amounts. However, both high bioactivity and bioavailability have been attributed to it. They show antioxidant, cardioprotective, anticancer, antidiabetic, neuroprotective and antiaging activities. However, human studies are still in the initial stages and therefore further studies are needed. (We recommend that you consult the full text of this article)