Background: The search for natural bioactive metabolites having potential anticancer property dates back to the Ebers papyrus written in 1550 BC. Natural products from medicinal plants and microorganisms are the most consistent and productive source for the “first-in-class” drugs. After two decades of research, a great deal of interest has been generated by discovery of remarkable pharmacological agents from endophytic fungi residing asymptomatically within plant tissues.
Objective: This review substantially covers the novel cytotoxic compounds isolated from endophytic fungi associated with terrestrial and mangrove plants as well as other microorganisms such as lichens, during 2011- 2015. These natural compounds are described based on their cytotoxic activity profiles, chemical nature and potential structure–activity relationship deduced from the biochemical and cytotoxic studies. The anti-cancerous activities of the compounds discussed in this review are taken from the published reports exhibiting activity against specific cancer cell lines along with the mechanism of action. These compounds are exclusively isolated from endophytic fungi.
Conclusion: Endophytic fungi can be exploited for isolation of new reliable, economical and environmentally safe natural bioactive molecules having wide range of applications in agriculture, medicine and food industry. Over the past few decades much progress has been achieved though, still many issues such as optimizing the fermentation culture conditions for increasing the compound yield, elucidating biosynthetic pathway of the compounds in the endophytic fungi needs to be further clarified and resolved.