Mitracarpus villosus [Swartz] DC formerly known as Mitracarpus scaber (Zuccarini) is an annual herb which is widely used in the West African traditional system of medicine as an antibiotic for the management of several disease conditions. The quantitative and qualitative phytochemical analysis from previous research have revealed that saponins, flavonoids, tannins, phenols, alkaloid, soluble carbohydrate, cyanide, cardiac glycoside, steroid, terpenoid, essential oil and reducing sugar are the major constituents of M. Villosus. However, resins, coumarins and anthraquinones are also present in the plant. Furthermore, stigmasterols, pentalongin, azaanthroquinones, gallic acid, 3,4,5-trimethoxybenzoic acid, 4-methoxyacetophenone, 3,4,5trimethoxyacetophenone, kaempferol-3-O-rutinoside, rutin, psoralen, oleanolic and ursolic acids have been isolated from Mitracarpus villosus. The essential oils of Mitracarpus villosus, is dominated by the long-chain aldehyde pentadecanal and the polyunsaturated fatty acid ester methyl (7Z,10Z,13Z)-hexadecatrienoate, with lesser quantities of 2,3-dimethylnaphthoquinone, and α-pinene. These compounds are reported to possess several biological and pharmacological activities, although the antibiotic potential of Mitracarpus villosus is well known, the chemical compounds detected in the plant possess; antioxidant, antidiabetic, antiviral, anticonvulsant, antiinflammatory, antitumour, antihyperlycemic, antihyperlipidemic, antihypertensive activities to mention a few. The cardiovascular protective effect and ability to ameliorate neurodegenerative disorder have also been reported for some of the compounds. Based on the chemical constituents of the plant, M. villosus is a potential candidate for the management of diseases like cancer, HIV and AIDS, liver disease, cardiovascular diseases and neurodegenerative disorders and other diseases. However, this claim is subject to scientific studies.