Aspergillus flocculosus represents a relatively recent fungal source of interesting secondary metabolites. A. flocculosus, as a fungal endophyte, had been isolated from different sources including plants as Markhamia platycaly, sponges for example Phakellia fusca, algae for example Padina sp. as well as sea sediment. This review presents a literature survey for the reported secondary metabolites isolated from A. flocculosus, demonstrating the potential biological activities of the reported metabolites. This review presents a comprehensive literature survey of the secondary metabolites isolated from the fungus A. flocculosus reporting eighty secondary metabolites belonging to different chemical classes including: steroids, meroterpenoids and diketopiperazine alkaloids, drimane sesquiterpenoids as well as their nitro benzoyl derivatives as well as cerebrosides. Secondary metabolites reported from A. flocculosus possess numerous biological activities including anticancer, anti-inflammatory, anti-trypanosomal, antimicrobial and neuroprotective activities. Despite the relatively limited reports for secondary metabolites represented in this review, the chemical diversity and the potential biological activities of the reported metabolites reported herein encourages for further in depth research for novel bioactive secondary metabolites from A. flocculosus especially those derived as endophytes from marine resources.