Inhibition of thrombin activity by selected natural products in comparison to neutrophil elastase.
Enzymatic thrombin activity is significantly inhibited only by a few selected natural phenolic compounds (myricetin, rosmarinic acid, caffeic acid phenethyl ester) but more strongly by unsaturated fatty acids like erucic acid and oleic acids. Compared to the inhibitory potential against neutrophil elastase, thrombin activity is rather weakly inhibited by phenolic compounds and fatty acids. Because of the importance of thrombin as a ligand for protease-activated receptor 1 (PAR-1), which is involved in inflammation, the inhibition of thrombin activity by natural compounds might enhance the anti-inflammatory effects of neutrophil elastase inhibition.
Melzig
Matthias F
MF
Institut für Pharmazie, Freie Universität Berlin, Berlin, Germany. melzig@zedat.fu-berlin.de
Henke
Kristin
K
D000818:Animals; D002417:Cattle; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D005230:Fatty Acids, Nonesterified / Q000494:pharmacology; D019272:Leukocyte Elastase / Q000037:antagonists & inhibitors*; D008517:Phytotherapy; D010946:Plants, Medicinal; D013917:Thrombin / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D005230:Fatty Acids, Nonesterified; D019272:Leukocyte Elastase; D013917:Thrombin