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Structure Elucidation and Antimalarial Activity of Apicidin F: An Apicidin-Like Compound Produced by Fusarium Fujikuroi

Structure Elucidation and Antimalarial Activity of Apicidin F: An Apicidin-Like Compound Produced by Fusarium Fujikuroi

Katharina Walburga von Bargen, Eva-Maria Niehaus, Klaus Bergander, Reto Brun, Bettina Tudzynski, Hans-Ulrich Humpf

J Nat Prod. 2013 Nov 22;76(11):2136-40.

PMID: 24195442

Abstract:

Apicidins are cyclic tetrapeptides with histone deacetylase inhibitory activity. Since their discovery in 1996 a multitude of studies concerning the activity against protozoa and certain cancer cell lines of natural and synthetic apicidin analogues have been published. Until now, the only published natural sources of apicidin are the fungus Fusarium pallidoroseum, later known as F. semitectum and two unspecified Fusarium strains. The biosynthetic origin of apicidins could be associated with a gene cluster, and a biosynthetic pathway has been proposed. Recently, our group was able to identify for the first time an apicidin-like gene cluster in F. fujikuroi that apparently does not lead to the production of any known apicidin analogue. By overexpressing the pathway-specific transcription factor we were able to identify a new apicidin-like compound. The present study provides the complete structure elucidation of the new compound, named apicidin F. Activity evaluation against Plasmodium falciparum showed good in vitro activity with an IC50 value of 0.67 μM.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP183506663	Apicidin		183506-66-3	Price

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