Abstract
Microorganisms still remain as main hotspots in the global drug discovery avenue. In particular, fungi are highly prolific producers of a vast of structurally divers specialised secondary metabolites, which have displayed a myriad of biomedical potentialities. Intriguingly, isocoumarins is one distinctive class of fungal natural products polyketides, which demonstrated numerous remarkable biological and pharmacological activities. This review article provides a comprehensive state of the art over the period 2000-2022 about the discovery, isolation, classifications, and therapeutic potentialities of isocoumarins exclusively reported from fungi. Indeed, a comprehensive list of 351 structurally diverse isocoumarins were documented, classified according to their fungal sources [16 order/ 28 family/ 55 genera] where they have been originally discovered, alongside, their reported pharmacological activities wherever applicable. Also, recent insights around their proposed and experimentally proven biosynthetic pathways are also briefly discussed.