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.

Preview	Text Wiese_AsperentinB_2017-1.pdf - Published Version Available under License Creative Commons: Attribution 4.0. Download (449Kb) | Preview
Preview	Text marinedrugs-15-00191-s001.pdf - Supplemental Material Available under License Creative Commons: Attribution 4.0. Download (1529Kb) | Preview

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.

Actions (login required)

View Item