Wines are the subject of an increasing number of investigations. The benefits of red wine became widely recognized after the observation of “French paradox” [8–10]. It has been found that there is a low mortality rate from ischemic heart disease among French people despite their high consumption of saturated fatty acids and the prevalence of other risk factors. The health-protective properties of wine are attributed to their antioxidant activity, i.e. the capability to scavenge reactive oxygen species, ROS . An imbalance between antioxidants and oxygen species results in oxidative stress leading to cellular damage. The phenolic compounds present in wine show beneficial physiological properties including protection against coronary heart disease, as well as anti-inflammatory and anti-carcinogenic activity. Most of the beneficial effects of wine are attributed to the presence of flavonoids, resveratrol, phenolic acids and other antioxidants. This paper reviews the significance of different compounds present in wine and their effect on human health. Chapter 1 focuses on flavonoids: flavonols, flavan-3-ols and anthocyanidins (Fig. 1) [14–29]. This class of compounds can exist both in a simple form, as aglycones, and bounded with sugars, as glycosides. The presence of phenolic hydroxyl group in these compounds is essential for their antioxidant activity and enables to scavenge free radicals in vivo. Chapter 2 describes chemical and physicochemical properties of resveratrol (Fig. 2) [30-41] which is the main antioxidant in wine. Moreover, this compound has been shown to inhibit the oxidation of low density lipoproteins and the aggregation of platelets [44-47]. Resveratrol also exhibits anti-inflammatory and anticancer properties [48, 49]. Chapter 3 reveals that wines are also a good source of other antioxidants [50–55] as phenolic acids (Fig. 3), tyrosol and hydroxytyrosol (Fig. 4), and also melatonin (Fig. 5). Unfortunately, some wines can include mycotoxins, mainly ochratoxin A [59, 60] (Fig. 6), which is produced by the phytopatogenic fungi, Aspergillus carbonarius. All types of red wine contain different amounts of ethanol and phenolic antioxidants, and therefore it is probable that the cardioprotective effect of red wine is caused by both these kinds of components [57–58]. Epidemiological observations, clinical and experimental in vitro research prove that regular and moderate intake of wine, particularly red wine, reduces cardiovascular morbidity and mortality [66–70].