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Three new pigment protein tyrosine phosphatases inhibitors from the insect parasite fungus Cordyceps gracilioides: terreusinone A, pinophilin C and cryptosporioptide A.
- Source :
-
Molecules (Basel, Switzerland) [Molecules] 2015 Apr 02; Vol. 20 (4), pp. 5825-34. Date of Electronic Publication: 2015 Apr 02. - Publication Year :
- 2015
-
Abstract
- Three new pigment compounds--terreusinone A (1), pinophilin C (2) and cryptosporioptide A (3)-were isolated from a solid culture of Cordyceps gracilioides. The structures of these compounds were determined by extensive spectroscopic analysis including HRESIMS, 1D- and 2D-NMR. The structure of terreusinone A (1) was further confirmed by single-crystal X-ray crystallographic diffraction analysis. In an in vitro activity assay, 1, 2 and 3 exhibited high inhibitory activity against PTP1B, SHP2, CDC25B, LAR and SHP1. Terreusinone A (1) inhibited PTP1B, SHP2, CDC25B, LAR and SHP1 enzyme with IC50 values 12.5, >50, 4.1, 10.6, 5.6 µg/mL, respectively; pinophilin C (2) with IC50 values 6.8, 8.0, 4.5, 4.7, 3.4 µg/mL, respectively; and cryptosporioptide A (3) with IC50 values 7.3, 5.7, 7.6, >50, 4.9 µg/mL, respectively.
- Subjects :
- Acrylates chemistry
Acrylates isolation & purification
Acrylates pharmacology
Animals
Crystallography, X-Ray
Enzyme Inhibitors chemistry
Enzyme Inhibitors isolation & purification
Molecular Structure
Pigments, Biological chemistry
Pigments, Biological pharmacology
Polyketides chemistry
Polyketides pharmacology
Coleoptera microbiology
Cordyceps chemistry
Enzyme Inhibitors pharmacology
Pigments, Biological isolation & purification
Polyketides isolation & purification
Protein Tyrosine Phosphatases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1420-3049
- Volume :
- 20
- Issue :
- 4
- Database :
- MEDLINE
- Journal :
- Molecules (Basel, Switzerland)
- Publication Type :
- Academic Journal
- Accession number :
- 25849805
- Full Text :
- https://doi.org/10.3390/molecules20045825