The ethyl acetate extract of an endophyte Epicoccum sorghinum exhibited anti-inflammatory activity at a concentration of <10 μg/mL. By bioassay-guided fractionation, one new compound, named epicorepoxydon A (1), and one unusual bioactive compound, 6-(hydroxymethyl)­benzene-1,2,4-triol (6), together with six known compounds, were isolated from E. sorghinum. The structures of all isolates were established by spectroscopic analyses. The relative configuration of 1 was deduced by the NOESY spectrum and its absolute configuration was determined by X-ray single-crystal analysis. The biological activities of all isolates were evaluated using four types of bioassays including cytotoxicity, anti-inflammatory, antiplatelet aggregation, and antiangiogenesis activities. Compounds 4 and 6 showed potent anti-inflammatory activity, compound 2 possessed potent antiplatelet aggregation and antiangiogenesis activities, and compound 6 demonstrated antiangiogenesis activity. This fungal species can cause a human hemorrhagic disorder known as onyalai. In this study, we identified the active components with antiplatelet aggregation and antiangiogenesis activities, which may be related to the hemorrhagic disorder caused by this fungus. Moreover, we proposed a biosynthetic pathway of the isolated polyketide secondary metabolites and investigated their structure–activity relationship (SAR). Our results suggested that E. sorghinum is a potent source of biologically active compounds that can be developed as antiplatelet aggregation and anti-inflammatory agents.

Utilizing the pER8:GUS transgenic plant bioassay system to monitor estrogenic activity-guided fractionation, one new constituent, erycaffrain A, together with 11 known compounds were isolated from the ethanolic extract of Erythrina caffra. The structures of the isolated compounds were identified in combination with spectroscopic analyses. This is the first study reporting the estrogenic activity of E. caffra. The new compound exhibited as a SREM, but also showed both estrogenic and anti-estrogenic activities in the MCF-7 cancer cell model. Several known phytoestrogens in this plant also revealed possible new functions for E. caffra stem.