Large-scale isolation and antitumor mechanism evaluation of compounds from the traditional Chinese medicine 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 C. militaris. Seven monomeric compounds, N6-(2-hydroxyethyl) adenosine (HEA), ergosterol (E), ergosta-7,22-diene-3,5,6-triol (EI), 5 alpha,8 alpha-epidioxy(22E,24R)-ergosta-6,22-dien-3 beta-ol (ED),ergosta-7,22-dien-3 beta,5 alpha-dihydroxy-6-one (EO), (20S,22E,24R)-Eegosta-7,22-dien-3 beta,5 alpha,6 beta,9 alpha-tetraol (ET), and (24S)-5,22-stigmastadien-3 beta-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 HEA 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. (C) 2021 Elsevier Masson SAS. All rights reserved.

Automated summary

A large-scale platform was established to extract seven monomeric compounds from the fruiting bodies of C. militaris, with their pharmacological activities and antitumor effects verified through experiments. The anti-insomnia effect of one compound was tested, and interactions with cell proteins were studied. The biosynthetic pathways of active monomers were determined, providing a foundation for the development of novel natural medicines.