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Published on: January 31, 2014
Collagenase inhibitors from Viola yedoensis
Naohiro Oshima1, Yuji Narukawa, Tadahiro Takeda
1Keio University, Minato-ku, Tokyo, Japan.
Journal of Natural Medicines
|April 25, 2012
Summary
Viola yedoensis extracts yielded potent inhibitors of Clostridium histolyticum collagenase (ChC). Scopoletin and esculetin were identified, with scopoletin showing significant activity. Further modifications enhanced ChC inhibition.
Area of Science:
- Natural Product Chemistry
- Enzymology
- Pharmacology
Background:
- Clostridium histolyticum collagenase (ChC) plays a role in tissue degradation.
- Natural products are a rich source of enzyme inhibitors.
- Viola yedoensis is a plant with potential medicinal properties.
Purpose of the Study:
- To isolate and identify compounds from Viola yedoensis that inhibit Clostridium histolyticum collagenase (ChC).
- To evaluate the inhibitory activity of isolated compounds against ChC.
- To investigate structure-activity relationships for ChC inhibition.
Main Methods:
- Solvent extraction of Viola yedoensis using acetone and methanol.
- Guided fractionation based on ChC inhibition assays.
- Isolation and structural elucidation of active compounds using chromatographic and spectroscopic techniques.
- Chemical modification of phenolic hydroxy groups to assess structure-activity relationships.
Main Results:
- Esculetin (IC(50) 12 μM) and scopoletin (IC(50) 1.8 μM) were isolated as active ChC inhibitors.
- Several other compounds including trans-p-coumaric acid, rutin, and isovitexin were also isolated.
- Modification of esculetin showed that small O-alkyl groups enhanced activity, while larger groups decreased it.
- Scoparone (6,7-dimethoxycoumarin) demonstrated potent ChC inhibition (IC(50) 24 nM).
Conclusions:
- Viola yedoensis contains compounds with significant Clostridium histolyticum collagenase inhibitory activity.
- Scopoletin is a promising ChC inhibitor from this plant source.
- Structural modifications, particularly O-alkylation, can modulate inhibitory potency, with scoparone being a highly effective derivative.
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