Species of Combretum are highly valued in Africa due to the plethora of traditional medicinal uses they may offer. Species such as Combretum molle, Combretum erythrophyllum, Combretum album, Combretum apiculatum, Combretum caffrum and Combretum quadrangulare are commonly utilized and are known to contain medicinally important phytochemicals. Traditionally, they are used to treat bacterial infections, venereal diseases, abdominal pain, sores, infertility, and labour pains, while displaying, anti-viral, anti-parasitic, cytotoxic, and mutagenic activity. There have been numerous studies released on the presence, isolation and bioactivity of phytochemicals. However, the transformation of the isolate into a drug of pharmacological importance has yet to be appraised on a large scale. Therefore, further evaluation of this genus and particularly the transformation of the isolates needs to be explored. This review aimed to collate current and prudent information pertaining to the presence of secretory structures in relation to potential medicinal properties, ethnopharmacological applications and bioactive compounds present within selected Combretum species.