| Summary: | Agar-based disc diffusion antimicrobial assay has shown that the ethyl acetate extract of the fermented broth of <i>Aspergillus</i> <i>giganteus</i> NTU967 isolated from <i>Ulva lactuca</i> exhibited significant antimicrobial activity in our preliminary screening of bioactive fungal strains. Therefore, column chromatography of the active principles from liquid- and solid–state fermented products of the fungal strain was carried out, and which had led to isolation of eleven compounds. Their structures were determined by spectral analysis to be seven new highly oxygenated polyketides, namely aspergilsmins A–G (<b>1</b>–<b>7</b>), along with previously reported patulin, deoxytryptoquivaline, tryptoquivaline and quinadoline B. Among these, aspergilsmin C (<b>3</b>) and patulin displayed promising anticancer activities against human hepatocellular carcinoma SK-Hep-1 cells and prostate cancer PC-3 cells with IC<sub>50</sub> values between 2.7–7.3 μM. Furthermore, aspergilsmin C (<b>3</b>) and patulin exhibited significant anti-angiogenic functions by impeding cell growth and tube formation of human endothelial progenitor cells without any cytotoxicity.
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