Lamiaceae (Labiatae) or the mint family is one of the most important families containing volatile oil. It is one of the largest plant families including 236 genera and more than 7,000 species. By reviewing the current available literature (2002-2018), many classes of secondary metabolites of this family were determined, viz., flavonoids (113 compounds), fatty derivatives (26 compounds) and sterols (15 compounds). Moreover, plants belonging to this family have been shown many biological activities such as antioxidant, cytotoxic, anti-inflammatory, antibacterial, antifungal, antiviral, analgesic, cardiovascular, hypoglycemic, hypolipidemic, antispasmodic, antiepileptic, anti-anxiety and anti-angiogenic. The most chemically investigated genus is Leonurus, while, Lavandula latifolia, Lamium garganicum, Lamium purpureum, Melissa officinalis and Moluccella laevis need more phytochemical attention. Regarding the biological investigation, Melissa officinalis was the most investigated species. Due to limited phytochemical and biological studies on many genera of the above family, we were encouraged to perform this review to help the researchers and orient them to carry out extensive studies on these plants to discover new or novel natural products.