Fig. 2.
HDACi screen and antiparasitic and cytotoxicity activities correlation. Screen for anti-HDAC activity (A). HDAC activity of HeLa nuclear extracts and of recombinant HDAC 1, 3, 6, and 8 proteins was a certained in the presence of 1.0 μM of each of the 8 synthesized compounds, as well as of SAHA. The experiments were carried out in triplicate, and the results are expressed as the percentage of deacetylase activity compared to the untreated control. Inhibition of T. gondii deacetylase activity by SAHA and the compound 363 (B). The total protein extract of T. gondii tachyzoites were prepared as described in the Materials and Methods section. The deacetylase activity was determined after the addition of 0.125 μM of compound 363 or of SAHA. The results are expressed as the percentage of deacetylase activity compared to untreated T. gondii protein extracts. The results are the mean of 4 experiments, carried out in triplicate. Correlation between HDACi and anti T. gondii activity or cytotoxicity potency (C).