Since the ancient times, garlic (Allium sativum) has been known as medicinal plant, used in various forms: fresh, as food ingridient, but also in medicinal preparations as infusion, decoct, syrup, tincture and extract. Due to its very complex chemical composition, biological activity of garlic highly depends on the mode of plant material processing. Essential oil of garlic is a product of the heating process during hydro-distillation and it is mainly composed of allyl and methyl sulphide derivatives derived by decomposition of allicin. Due to the lack allicin in its chemical composition, garlic oil has been neglected by scientists for a long time. Recent studies revealed very wide spectrum of activities exhibited by garlic oil and its main components diallyl mono-, di- and trisulphide. It has been reported that they possess high biological potential as antimicrobial, antioxidant, cardioprotective, antitumor and antidiabetic compounds.