Abstract
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.
References
- 1
Gabazza E C, Taguchi O, Kamada H, Hayashi T, Adachi Y, Suzuki K.
Progress in the understanding of protease-activated receptors.
Int J Hematol.
2004;
79
117-22
- 2 Bieth J G. Leukocyte elastase. In: Handbook of proteolytic enzymes. Barrett AJ,
Rawlings ND, Woessner FF, editors London; Academic Press 1998: pp 54-60
- 3
Uehara A, Muramoto K, Takada H, Sugawara S.
Neutrophil serine proteases activate human nonepithelial cells to produce inflammatory
cytokines through protease-activated receptor 2.
J Immunol.
2003;
170
5690-6
- 4
Melzig M F, Löser B, Ciesielski S.
Inhibition of neutrophil elastase activity by phenolic compounds from plants.
Pharmazie.
2001;
56
967-70
- 5
Rennert B, Melzig M F.
Free fatty acids inhibit the activity of Clostridium histolyticum collagenase and human neutrophil elastase.
Planta Med.
2002;
68
767-69
- 6 Powers J C, Harper J W. Inhibitors of serine proteinases. In: Proteinase inhibitors,
Barrett AJ, Salvesen G, editors Amsterdam; Elsevier Science Publishers 1986: pp 55-152
- 7
Ofosu F A, Freedman J, Dewar L, Song Y, Fenton J W.
A trypsin-like platelet protease propagates protease-activated receptor-1 cleavage
and platelet activation.
Biochem J.
1998;
336
283-9
- 8 Wichtl M (ed). Teedrogen und Phytopharmaka. Stuttgart; Wissenschaftliche Verlagsgesellschaft
2002
- 9
Bankova V S, De Castro S L, Marcucci M C.
Propolis: recent advances in chemistry and plant origin.
Apidoligie.
2000;
31
3-15
- 10
Sartor L, Pezzato E, Garbisa S.
(-)-Epigallocatechin-3-gallate inhibits leucocyte elastase: potential of the phyto-factor
in hindering inflammation, emphysema, and invasion.
J Leukoc Biol.
2002;
71
73-9
- 11
Baer D J, Judd J T, Clevidence BA,Tracy R P.
Dietary fatty acids affects plasma markers of inflammation in healthy men fed controlled
diets: a randomized crossover study.
Am J Clin Nutr.
2004;
79
967-73
- 12
Dong H, Chen S X, Kini R M, Xu H X.
Effect of tannin from Geum japonicum on the catalytic activity of thrombin and factor Xa of blood coagulation cascade.
J Nat Prod.
1998;
61
1356-60
Prof. Dr. M. F. Melzig
Institut für Pharmazie
Freie Universität Berlin
Königin-Luise-Str 2 +4
14195 Berlin
Germany
Phone: +49-30-838-51451
Fax: +49-30-838-51461
Email: melzig@zedat.fu-berlin.de
