Abstract
The chemical investigation of the marine sponge Dysidea frondosa discovered a pair of unprecedented bioconjugates that are composed of a meroterpene and an unusual psammaplysin alkaloid. The structures of frondoplysins A (1) and B (2) were characterized by analysis of HRMS and NMR data coupled with single-crystal X-ray diffraction. Frondoplysin A was found to be a potent inhibitor targeting protein-tyrosine phosphatase 1B (PTP1B) with an IC50 value of 0.39 μM.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Alkaloids / chemistry*
-
Alkaloids / pharmacology
-
Alkaloids / toxicity
-
Animals
-
Animals, Genetically Modified
-
Antioxidants / chemistry
-
Antioxidants / pharmacology
-
Crystallography, X-Ray
-
Dysidea / chemistry*
-
Enzyme Inhibitors / chemistry
-
Enzyme Inhibitors / pharmacology*
-
Magnetic Resonance Spectroscopy
-
Molecular Structure
-
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors
-
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
-
Zebrafish / genetics
Substances
-
Alkaloids
-
Antioxidants
-
Enzyme Inhibitors
-
PTPN1 protein, human
-
Protein Tyrosine Phosphatase, Non-Receptor Type 1