Background Pleurostylia capensis Turcz (Loes) is a tree species found in Africa that has been used in traditional medicine for various ailments.Aim This review aims to investigate the phytochemistry, pharmacology and toxicity of P. capensis Turcz (Loes) and its ethnomedicinal uses.Method A comprehensive search was conducted using electronic databases, including PubMed, Scopus and Web of Science. The keywords used were ‘Pleurostylia capensis’, ‘phytochemistry’, ‘pharmacology’, ‘toxicology’ and ‘ethnomedicine’. Studies were included if they reported on the phytochemical composition, pharmacological activities, toxicological evaluations and/or ethnomedicinal uses of Pleurostylia capensis.Results A phytochemical analysis revealed the presence of various bioactive compounds including alkaloids, flavonoids, terpenoids and phenolic compounds. Pharmacological studies have reported the plant’s potential as an anti-inflammatory, antioxidant, antimicrobial and a potential agent for bone and articular cartilage regeneration. Toxicological evaluations have shown that the plant is safe for human consumption at recommended doses.Conclusion The review highlights the potential of Pleurostylia capensis as a source of bioactive compounds with pharmacological activities. Toxicological evaluations have also shown that the plant is safe for human consumption. The review provides useful information for further research on the development of new drugs from natural products.Contribution This review provides a comprehensive summary of the phytochemistry, pharmacology, toxicology of Pleurostylia capensis and its ethnomedicinal uses. The review highlights the potential of the plant as a source of bioactive compounds and provides a basis for further research on the development of new drugs from natural products.