Apicidin, a fungal metabolite, contains potent and broad antiprotozoal characteristics in vitro against Apicomplexan parasites. This compound has also been shown to be active in mice against Plasmodium berghei. Apicidin is an HDAC inhibitor. Mechanistic studies utilizing Apicidin inhibition in low nanomolar concentration has been shown to cause hyperacetylation of histones in the Apicomplexan HDAC (histone deacetylase), which causes hyperacetylation of histones within the parasite. It has been reported that Apicidin also contains a wide range of antiproliferative activity against various cancer cell lines in mice, again through HDAC inhibition. Apicidin has also been shown to stimulate apoptosis via induction of Fas/Fas ligand. Furthermore, it has been reported to dramatically decrease HIF-1α levels and therefore reduce transcriptional activity of HIF-1 in murine cell lines. Apicidin is an inhibitor of HDAC3 and N-CoR.
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