The anti-diabetic activity of ginger powder (Zingiber officinale) has been recently promoted, with the recommendation to be included as one of the dietary supplements for diabetic patients. However, previous studies presented different results, which may be caused by degradation and metabolic changes of ginger components, gingerols, shogaols and paradols. Therefore, we prepared 10 ginger active components, namely 6-, 8-, 10-paradols, 6-, 8-, 10-shogaols, 6-, 8-, 10-gingerols and zingerone, and evaluated their anti-hyperglycemic activity. Among the tested compounds, 6-paradol and 6-shogaol showed potent activity in stimulating glucose utilization by 3T3-L1 adipocytes and C2C12 myotubes. The effects were attributed to the increase in 5′ adenosine monophosphate-activated protein kinase (AMPK) phosphorylation in 3T3-L1 adipocytes. 6-Paradol, the major metabolite of 6-shogaol, was utilized in an in vivo assay and significantly reduced blood glucose, cholesterol and body weight in high-fat diet-fed mice.

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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.