Glycerolipids as selective thrombin inhibitors from the fungus Stereum hirsutum.
A dry extract of Stereum hirsutum exhibited a significant inhibitory activity on thrombin (34%). A bioassay oriented fractionation of the extract of Stereum hirsutum has led to the isolation of two active fractions. On the basis of spectroscopic data, chemical reactions, and GC-MS analysis, complex mixtures of diacylglycerophospholipids (DAGPs) and diacylglycerols (DGs) have been isolated and identified. Docking studies suggest that some isolated compounds could bind to the thrombin active site in a similar manner as previously reported phosphonate thrombin inhibitors.
Doljak
Bojan
B
Department of Pharmaceutical Biology, Faculty of Pharmacy, University of Ljubljana, Askerceva 7, 1000 Ljubljana, Slovenia.
Cateni
Francesca
F
Anderluh
Marko
M
Procida
Giuseppe
G
Zilic
Jelena
J
Zacchigna
Marina
M
D001487:Basidiomycota / Q000737:chemistry*; D004075:Diglycerides / Q000737:chemistry; D005227:Fatty Acids / Q000737:chemistry; D008401:Gas Chromatography-Mass Spectrometry; D005990:Glycerol / Q000737:chemistry*; D020404:Glycerophospholipids / Q000737:chemistry; D008024:Ligands; D008055:Lipids / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D012015:Reference Standards; D013917:Thrombin / Q000037:antagonists & inhibitors*
D004075:Diglycerides; D005227:Fatty Acids; D020404:Glycerophospholipids; D008024:Ligands; D008055:Lipids; D013917:Thrombin; D005990:Glycerol