Antitumor Compounds from Cordyceps Militaris

We established a large-scale separation and purification platform to obtain kilogram amounts of natural compounds from the extraction of the fruiting bodies of <i>C. militaris. </i>Seven monomeric compounds, N6-(2-hydroxyethyl) adenosine (HEA), ergosterol (E), ergosta-7,22-diene-3,5,6-triol (EI), 5α,8α-epidioxy-(22<i>E</i>,24<i>R</i>)-ergosta-6,22-dien-3β-ol (ED), ergosta-7,22-dien-3β,5α-dihydroxy-6-one(EO),(20<i>S</i>,22<i>E</i>,24<i>R</i>)-Eegosta-7,22-dien-3β,5α,6β,9α-tetraol22<i>E</i>,24<i>R</i>-ergosta-7,22-diene-3β,5α,6β,9α-tetraol (ET), and (24<i>S</i>)-5,22-stigmastadien-3β-ol (SE), were harvested using different solvents, and the structure of each compound was identified. The activities and functions of the isolated compounds were tested by label-free, real-time cell analysis methods at the cellular level, and their antitumor effects were verified using mouse models of Lewis and H22 tumors. The anti-insomnia effect of HEAadenosine was tested in an anti-insomnia mouse model. The interactions between E and 8 A549 cell proteins were determined. The biosynthetic pathways of HEA and E, which possess pharmacologically active monomers, were determined. This platform can provide a theoretical basis for the further development and discovery of novel natural medicines.