Since ancient times, indigenous plants have been used by traditional healers for treating various ailments. Sutherlandia frutescens is one of the most commonly used medicinal plants of southern Africa. This widely distributed plant has been traditionally used to treat cancer and HIV patients; however scientific validation is still in high demand. The purpose of this book was to provide a phytochemical characterisation of various extracts prepared. This book further contains evidence that various chemotypes of S. frutescens are present. Subsequent biological characterisation was carried out to preliminary ascertain whether this medicinal plant could have anti-cancer and/or immune-modulating properties and which compounds might be responsible for these actions. This book could assist in providing a clearer perspective on the role S. frutescens plays in combating various diseases and therefore, should be useful for researchers in drug discovery, natural product chemistry, botany or anyone interested in South African medicinal plants and their traditional uses.