In vitro activity: Golgicide A inhibits the effect of shiga toxin on protein synthesis with an IC50 of 3.3 μM. Golgicide A causes a decrease in GBF1-mediated Arf1 activation, arrests secretion of soluble and membrane-anchored proteins and then impairs retrograde toxin transport. Golgicide A decreases HCV RNA levels in FLRP1 cells and J6/JFH1 cells. In addition, Golgicide A causes redistribution of NS5A and accumulation of infectious viral particles in J6/JFH1 cells.
Cell Assay: Golgicide A inhibits the effect of shiga toxin on protein synthesis with an IC50 of 3.3 μM in Vero cells. Immunofluoresence experiments demonstrates that Golgicide A causes complete dispersal of the medial-Golgi markers giantin and the cis-Golgi marker GM130 and results in a rapid redistribution of COPI from the Golgi. Also, Golgicide A causes a decrease in GBF1-mediated Arf1 activation, impairs retrograde toxin transport and arrests secretion of soluble and membrane-anchored proteins. Golgicide A decreases HCV RNA levels and causes redistribution of NS5A in FLRP1 cells and J6/JFH1 cells. In addition, Golgicide A causes accumulation of infectious viral particles in J6/JFH1 cells. |