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

作者：Wiese Jutta; Aldemir Huelya; Schmaljohann Rolf; Gulder Tobias A M^*; Imhoff Johannes F^*

来源：Marine Drugs, 2017, 15(6): 191.

DOI：10.3390/md15060191

• PTP1B
• cladosporin
• asperentin
• Aspergillus
• deep-sea

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 Aspergillussydowii 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 M 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.

• 出版日期2017-6