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.