Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B

Wiese, Jutta, Aldemir, Hülya, Schmaljohann, Rolf, Gulder, Tobias and Imhoff, Johannes F. (2017) Asperentin B, a New Inhibitor of the Protein Tyrosine Phosphatase 1B Marine Drugs, 15 (6). p. 191. DOI 10.3390/md15060191.

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Abstract

In the frame of studies on secondary metabolites produced by fungi from deep-sea environments we have investigated inhibitors of enzymes playing key roles in signaling cascades of biochemical pathways relevant for the treatment of diseases. Here we report on a new inhibitor of the human protein tyrosine phosphatase 1B (PTP1B), a target in the signaling pathway of insulin. A new asperentin analog is produced by an Aspergillus sydowii strain isolated from the sediment of the deep Mediterranean Sea. Asperentin B (1) contains an additional phenolic hydroxy function at C-6 and exhibits an IC50 value against PTP1B of 2 μM in vitro, which is six times stronger than the positive control, suramin. Interestingly, asperentin (2) did not show any inhibition of this enzymatic activity. Asperentin B (1) is discussed as possible therapeutic agents for type 2 diabetes and sleeping sickness.

Document Type: Article
Keywords: PTP1B; cladosporin; asperentin; Aspergillus; deep-sea
Research affiliation: OceanRep > The Future Ocean - Cluster of Excellence
OceanRep > GEOMAR > FB3 Marine Ecology > FB3-MI Marine Microbiology
Refereed: Yes
DOI etc.: 10.3390/md15060191
ISSN: 1660-3397
Related URLs:
Projects: Future Ocean
Expeditions/Models:
Date Deposited: 07 Jul 2017 12:28
Last Modified: 19 Dec 2017 12:49
URI: http://eprints.uni-kiel.de/id/eprint/38765

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