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In recent years, much attention has been paid to the natural value of herbal compounds in order to prevent various diseases. It should be noted that garlic is one source for which extensive research has been done in terms of its various compounds and their effects on different diseases. Moreover, several countries have been interested in the potential effects of the various compounds existing in garlic (Allium sativum) since ancient times across many different centuries. Bioactive compounds of garlic are useful in prevention and treatment. The major physiological roles of garlic are that is has an antibiotic, anticancer, and antioxidant effect, demonstrates immune system enhancement, is an antidiabetic or hypoglycemic agent (glucose reducer), a liver protector, an antifibriolytic, an antithrombolytic, as well having a potential role in the prevention of cardiovascular diseases. The outstanding effects of active chemical compounds in garlic on health and treatments of various disorders have been extensively examined in animals as well as humans. In this chapter these are explained separately. Meanwhile, the interactions of garlic consumption with other drugs are mentioned in order to provide therapists and consumers with comprehensive information.