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