South Africa has a long history and strong belief in traditional herbal medicines. Using
ethnobotanical knowledge as a lead, a large number of South African medicinal plants
have been discovered to possess a wide spectrum of pharmacological properties. In
this review, bioprospecting of endophytes is highlighted by following the advantages of
the ethnomedicinal approach together with identifying unique medicinal plants where
biological activity may be due to endophytes. This review focuses on the current status
of South African medicinal plants to motivate the research community to harness the
benefits of ethnobotanical knowledge to investigate the presence of endophyticmicrobes
from the most potent South Africanmedicinal plants. The potential chemical diversity and
subsequent putative medicinal value of endophytes is deserving of further research. A
timely and comprehensive review of literature on recently isolated endophytes and their
metabolites was conducted.Worldwide literature from the last 2 years demonstrating the
importance of ethnobotanical knowledge as a useful approach to discover endophytic
microbes was documented. Information was obtained from scientific databases such
as Pubmed, Scopus, Scirus, Google Scholar, Dictionary of Natural Products, Chemical
Abstracts Services, official websites, and scientific databases on ethnomedicines.
Primary sources such as books, reports, dissertations, and thesises were accessed
where available. Recently published information on isolated endophytes with promising
bioactivity and their bioactive natural products worldwide (2015-2017) was summarized.
The potential value of South African medicinal plants as sources of endophytes is
discussed. The insights provided through this study indicate that medicinal plants in South Africa are highly under-investigated sources of potentially useful endophytic
microbes. New approaches may be used by medicinal plant scientists for further
exploration of natural products from endophytic fungi and bacteria in southern Africa.