The use of traditional medicine in treating a variety of both human and animal infections is ancient and still relevant. This is due to the resistance exhibited by most pathogenic microbial stains to currently-used antibiotics. The current work reports the phytochemistry, ethno-medicinal uses, toxicology, and most important pharmacological activities that validate the use of the plant species in African traditional medicine. Curtisia dendata is used in the treatment of many human and animal infections, including diarrhea, skin and related conditions, sexually transmitted infections, cancer, and a variety of ethno-veterinary infections. Pharmacologically, the plant species exhibited potent antimicrobial activity against a variety of pathogens. Further, both extracts and compounds isolated from the plant species exhibited potent antioxidant, anticancer, anti-parasitic, anti-inflammatory, and other important biological activities. Phytochemically, the plant species possess a variety of compounds, particularly triterpenes, that may well explain the various pharmacological activities of the plant species. The toxicological parameters, antimicrobial activities against microorganisms related to sexually transmitted infections, anti-diabetic effects, and inflammatory properties of the plant species are not well studied and still need to be explored. The biological activities observed validate the use of the plant species in African traditional medicine, particularly in the treatment of pulmonary infections associated with Mycobacterium species, and may well be due to the presence of triterpenes prevalent in the leaves.