Anti-inflammatory Cerebrosides from Cultivated Cordyceps militaris

Cordyceps militaris (bei-chong-chaw, northern worm grass) is a precious and edible entomopathogenic fungus, which is widely used in traditional Chinese medicine (TCM) as a general booster for the nervous system, metabolism, and immunity. Saccharides, nucleosides, mannitol, and sterols were isolated from this fungus. The biological activity of <i>C. militaris</i> was attributed to the saccharide and nucleoside contents. In this study, the aqueous methanolic fraction of <i>C. militaris</i> fruiting bodies exhibited a significant anti-inflammatory activity. Bioactivity-guided fractionation of the active fraction led to the isolation of eight compounds, including one new and two known cerebrosides (ceramide derivatives), two nucleosides, and three sterols. Cordycerebroside A (<b>1</b>), the new cerebroside, along with soyacerebroside I (<b>2</b>) and glucocerebroside (<b>3</b>) inhibited the accumulation of pro-inflammatory iNOS protein and reduced the expression of COX-2 protein in LPS-stimulated RAW264.7 macrophages. This is the first study on the isolation of cerebrosides with anti-inflammatory activity from this TCM