Introduction: Allium Sativum, commonly known as garlic, a member of the family Liliaceae, is a species in the onion genus. Allium sativum is a bulbous plant with hermaphrodite flowers growing up to 1.2 m in height. The aim of this article was to review ethnopharmacology, Phytochemistry, and anti-breast cancer activities of Allium sativum. Methods: This review article was carried out by searching studies in PubMed, Medline, Web of Science, and IranMedex databases from 1995 to 2016.Totally, of 108 found articles, 47 articles were included. The search terms were “Allium sativum”, “Ethnopharmacology”, “anti-breast cancer”, “complementary medicine”. Result: It was shown that anti-breast activity of Allium sativum have been attributed to its oil-soluble sulfur ingredients, especially diallyl sulfide [DAS], diallyl disulfide [DADS], and diallyl trisulfide [DATS]. These compounds are not only inhibiting the growth of cancerous cells but also inhibits the proliferation of MCF-7 cells as well as cause MCF-7 cells death. Conclusion: Allium sativum was shown to hold anti-breast cancer activity due to both its phytochemical compound and mechanism of action. Selenium-enriched Allium sativum or organ selenium compounds protect better against breast cancer and inhibit both growth, proliferation of breast cancer cells. Besides, they cause breast cancerous cell apoptosis. Thus, Allium sativum and Allium sativum-derived compounds are shown to be good candidate for breast cancer control.