Akanthomins A-C, aphidicolin analogs from a fungus Akanthomyces sp., that inhibit cell cycle.

ABSTRACT

Natural products that inhibit cell cycle progression may have potential as anticancer agents. In this study, cell cycle inhibition of microbial culture extracts was screened by fluorescent images using HeLa/Fucci2 cells. The culture extract of a fungus, Akanthomyces sp., inhibited the cell cycle progression at the S/G2/M phases, and bioassay-guided fractionation of the extract afforded three previously undescribed aphidicolin derivatives, namely akanthomins A-C, and an undescribed chromone glycoside, specifically 9-hydroxyeugenetin 9-O-ß-d-(4-O-methyl)glucopyranoside, in addition to aphidicolin. The chemical structures of these compounds were elucidated by spectroscopic analysis and chemical derivatization. Using a flow cytometer, akanthomin A and aphidicolin were found to inhibit cell cycle progression at the S phase.