Applications of Leonotis leonurus L. R. has shown that the plant has diverse activities such as anticonvulsant, antinociceptive, anti-inflammatory, antidiabetic, antibacterial, anti-oxidant, anthelmintic activities and hypoglycemic properties, which justifies the herb use in the management and control of pain, arthritic, diabetes, dermatological, hypertension, anti-inflammatory and wound healing properties. Thirty seven secondary metabolites were reported, which includes 21 labdane diterpenes which are chemotaxonomic markers for the Leonotis genus and the mint family, Lamiaceae. The leaf, flowers and sepals essential oils are mostly constituted by monoterpenoids and sesquiterpenoids.