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BACKGROUND   Endophytic fungi, present mainly in the Ascomycota and Basidiomycota phyla, are associated with different plants and represent important producers of bioactive natural products. Brazil has a rich biodiversity of plant species, including those reported as being endemic. Among the endemic Brazilian plant species,  Vellozia gigantea  (Velloziaceae) is threatened by extinction and is a promising target to recover endophytic fungi.    OBJECTIVE   The present study focused on bioprospecting of bioactive compounds of the endophytic fungi associated with  V. gigantea , an endemic, ancient, and endangered plant species that occurs only in the rupestrian grasslands of Brazil.    METHODS   The capability of 285 fungal isolates to produce antimicrobial and antimalarial activities was examined. Fungi were grown at solid-state fermentation to recover their crude extracts in dichloromethane. Bioactive extracts were analysed by chromatographic fractionation and NMR and displayed compounds with antimicrobial, antimycobacterial, and antimalarial activities.    FINDINGS   Five fungi produced antimicrobial and antimalarial compounds. Extracts of  Diaporthe miriciae  showed antifungal, antibacterial, and antimalarial activities;  Trichoderma effusum  displayed selective antibacterial activity against methicillin-resistant  Staphylococcus aureus  and  Mycobacterium intracellulare ; and three  Penicillium  species showed antibacterial activity.  D. miriciae  extract contained highly functionalised secondary metabolites, yielding the compound epoxycytochalasin H with high antimalarial activity against the chloroquine-resistant strain of  Plasmodium falciparum , with an IC 50  approximately 3.5-fold lower than that with chloroquine.    MAIN CONCLUSION   Our results indicate that  V. gigantea  may represent a microhabitat repository hotspot of potential fungi producers of bioactive compounds and suggest that endophytic fungal communities might be an important biological component contributing to the fitness of the plants living in the rupestrian grassland.

memórias do instituto oswaldo cruz

Antimycobacterial and antimalarial activities of endophytic fungi associated with the ancient and narrowly endemic neotropical plant Vellozia gigantea from Brazil