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Cissampelos capensis L.f. is a perennial climber widely used as a traditional medicine in South Africa. This study was aimed at providing a critical review of medicinal uses, phytochemical and pharmacological properties of C. capensis. Documented information on the pharmacological properties, phytochemistry and medicinal uses of C. capensis was collected from several online sources such as Scopus, Google Scholar, PubMed and Science Direct, and pre-electronic sources such as book chapters, books, journal articles and scientific publications obtained from the university library. This study revealed that leaf, rhizome and root infusions and decoctions of C. capensis are mainly used as a blood purifier, and traditional medicines for respiratory problems, ulcers, sores and wounds, skin and stomach cancers, snakebite, sexually transmitted infections, skin diseases, diabetes and gastrointestinal problems. Phytochemical compounds identified from the species include alkaloids, essential oils, flavonoids, phenolics, saponins and tannins. Pharmacological research revealed that C. capensis extracts and compounds isolated from the species have anthelmintic, antibacterial, antifungal, antidiabetic, antimalarial, hepatotoxicity, spermatozoa and cytotoxicity activities. Documentation of the medicinal uses, phytochemistry and pharmacological properties of C. capensis is vital as this information provides baseline data required for future research and development of health-promoting and pharmaceutical products. There is a need for extensive toxicological evaluations of crude extracts and compounds isolated from the species since C. capensis contains potentially toxic compounds.
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