Abstract
In this study, twelve neuraminidase (NA) inhibitory compounds 1-12 were isolated from heartwood of Caesalpinia sappan on the basis of their biological activities against three types of viral NAs. Of isolated homoisoflavonoids, sappanone A (2) showed the most potent NAs inhibitory activities with IC(50) values of 0.7 µM [H1N1], 1.1 µM [H3N2], and 1.0 µM [H9N2], respectively, whereas saturated homoisoflavonoid (3) did not show significantly inhibition. This result revealed that α,β-unsaturated carbonyl group in A-ring was the key requirements for viral NAs inhibitory activity. In our enzyme kinetic study, all NA inhibitors screened were found to be reversible noncompetitive types.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiviral Agents / chemistry
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Antiviral Agents / isolation & purification
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Antiviral Agents / pharmacology*
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Caesalpinia / chemistry*
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Cell Line
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Dogs
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology
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Flavonoids / chemistry
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Flavonoids / isolation & purification
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Flavonoids / pharmacology*
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Influenza A Virus, H1N1 Subtype / drug effects
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Influenza A Virus, H1N1 Subtype / enzymology
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Influenza A Virus, H3N2 Subtype / drug effects
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Influenza A Virus, H3N2 Subtype / enzymology
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Influenza A Virus, H9N2 Subtype / drug effects
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Influenza A Virus, H9N2 Subtype / enzymology
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Influenza A virus / drug effects*
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Influenza A virus / enzymology
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Inhibitory Concentration 50
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Neuraminidase / antagonists & inhibitors*
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Orthomyxoviridae Infections / drug therapy
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Orthomyxoviridae Infections / virology
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Phytotherapy
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Plant Extracts / chemistry
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Viral Proteins / antagonists & inhibitors*
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Wood
Substances
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Antiviral Agents
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Enzyme Inhibitors
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Flavonoids
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Plant Extracts
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Viral Proteins
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Neuraminidase