Abstract |
We have evaluated the inhibitory activity of flavone, nobiletin, and heptamethoxyflavone on matrix metalloproteinase ( MMP) activity in the rat. MMP in 9000-g supernatant fraction of lung homogenate was activated by p-aminophenyl mercuric acetate (APMA), and gelatinolytic activity was determined by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) followed by Coomassie staining. This activity should be related to MMP-2 and/or MMP-9 and was confirmed by gelatin zymography. Fluorescent-conjugated collagen used as a substrate for collagenolytic activity wasinvestigated by SDS-PAGE also. The film in-situ zymography method was applied to rat brain and lung tissue in the same manner. Flavone and nobiletin inhibited the APMA-stimulated gelatinolytic activity and also the collagenolytic activity by more than 75%. The film in-situ zymography method indicated that these compounds might be potent inhibitors of MMP, suggesting the specific inhibition of localized MMP in brain hippocampus and/or lung terminal bronchioles, which may contribute to the prevention of some types of brain disease or cancer invasion and metastasis.
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Authors | K Sasaki, N Tateoka, H Ando, F Yoshizaki |
Journal | The Journal of pharmacy and pharmacology
(J Pharm Pharmacol)
Vol. 57
Issue 4
Pg. 459-65
(Apr 2005)
ISSN: 0022-3573 [Print] England |
PMID | 15831206
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Flavones
- Flavonoids
- Matrix Metalloproteinase Inhibitors
- 3,3',4',5,6,7,8-heptamethoxyflavone
- Gelatin
- Collagen
- nobiletin
- Matrix Metalloproteinases
- flavone
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Topics |
- Animals
- Brain
(drug effects, enzymology, metabolism)
- Collagen
(metabolism)
- Electrophoresis, Polyacrylamide Gel
(methods)
- Flavones
(pharmacology)
- Flavonoids
(pharmacology)
- Gelatin
(metabolism)
- Lung
(drug effects, enzymology, metabolism)
- Matrix Metalloproteinase Inhibitors
- Matrix Metalloproteinases
(metabolism)
- Rats
- Rats, Wistar
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