Planta Med 2000; 66(8): 751-753
DOI: 10.1055/s-2000-9563
Letter
© Georg Thieme Verlag Stuttgart · New York

Inhibition of Neutrophil Elastase Activity by Cinnamic Acid Derivatives from Cimicifuga racemosa

Beate Löser1 , Sven O. Kruse2 , Matthias F. Melzig1,*, Adolf Nahrstedt2
  • 1 Institut für Pharmazie, Humboldt-Universität, Berlin, Germany
  • 2 Institut für Pharmazeutische Biologie und Phytochemie, Westfälische Wilhelms-Universität, Münster, Germany
Further Information

Publication History

Publication Date:
31 December 2000 (online)

Abstract

Caffeic acid, fukinolic acid as well as cimicifugic acids A, B, E and F isolated from the rhizomes of Cimicifuga racemosa (Ranunculaceae) inhibited the activity of neutrophil elastase (EC 3.4.21.37) in a dose-dependent manner. An IC50 of 93 μmol/L was determined for caffeic acid and 0.23 μmol/L for fukinolic acid. Cimicifugic acid A inhibited the enzyme with an IC50 of 2.2 μmol/L, cimicifugic acid B with 11.4 μmol/L, and cimicifugic acid F with 18 μmol/L. Cimicifugic acid E was only a very weak inhibitor.

References

  • 1 Keiser  H,, Greenwald  R A,, Feinstein  G,, Janoff  A.. Degradation of cartilage proteoglycan by human granule neutral proteases - a model of joint injury.  Journal of Clinical Investigations. 1976;;  57 625-32
  • 2 Baggiolini  M,, Schnyder  J,, Bretz  U,, Dewald  B,, Ruch  W.. Cellular mechanisms of proteinase release from inflammatory cells and the degradation of extracellular proteins.  Ciba Foundation Symposium. 1979;;  75 105-21
  • 3 Pipoly  D J,, Crouch  E C.. Degradation of native type IV procollagen by human neutrophil elastase. Implication for leukocyte mediated degradation of basement membranes.  Biochemistry. 1987;;  26 5748-54
  • 4 Fischbach  W,, Becker  W,, Mossner  J,, Ohlemuller  H,, Koch  W,, Borner  W.. Leukocyte elastase in chronic inflammatory bowel diseases: A marker of inflammatory activity?.  Digestion. 1987;;  37 88-95
  • 5 Melzig  M F,, Löser  B,, Lobitz  G O,, Tamayo-Castillo  G,, Merfort  I.. Inhibition of granulocyte elastase activity by caffeic acid derivatives.  Die Pharmazie. 1999;;  54 712
  • 6 Kusano  G,, Takahira  M,, Shibano  M,, Kusano  A,, Okamoto  Y,, Tsujibo  H,, Numata  A,, Inamori  Y.. Studies on inhibitory activities of fukiic acid esters on germination, α-amylase and carboxy peptidase A.  Biological and Pharmaceutical Bulletin. 1998;;  21 997-9
  • 7 Kruse  S O,, Löhning  A,, Pauli  G F,, Winterhoff  H,, Nahrstedt  A.. Fukiic and piscidic acid esters from the rhizome of Cimicifuga racemosa and the in vitro estrogenic activity of fukinolic acid.  Planta Medica. 1999;;  65 763-4
  • 8 Sakamura  S,, Yoshihara  T,, Katsuhiko  T.. The constituents of Petasites japonicus: Structure of fukiic acid and fukinolic acid.  Agricultural and Biological Chemistry. 1973;;  37 1915-21
  • 9 Umezawa  H,, Aoyagi  T,, Okura  A,, Morishima  H,, Takeuchi  T.. Elastinal, a new elastase inhibitor produced by Actinomycetes.  Journal of Antibiotics. 1973;;  26 787-9
  • 10 Sakai  S,, Ochiai  H,, Nakajima  K,, Terasawa  K.. Inhibitory effect of ferulic acid in macrophage inflammatory protein-2 production in a murine macrophage cell line.  Cytokine. 1997;;  9 242-8
  • 11 Tang  W,, Eisenbrand  G.. Chinese drugs of plant origin. Berlin:; Springer, 1992: 315
  • 12 Tyler  V E.. The Honest Herbal. New York:; Pharmaceutical Products Press, Haworth Press Inc., 1993: 45-6
  • 13 Stein  R L.. Catalysis by human leukocyte elastase: III. Steady-state kinetics for the hydrolysis of p-nitrophenyl esters.  Archives of Biochemistry and Biophysics. 1985;;  236 677-80

Prof. Dr. Matthias F. Melzig

Institute of Pharmacy Humboldt-University Berlin

Goethestr. 54

13086 Berlin

Germany

Email: matthias=melzig@pharma.hu-berlin.de