Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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Homoisoflavonoids from Caesalpinia sappan Displaying Viral Neuraminidases Inhibition
Hyung Jae JeongYoung Min KimJang Hoon KimJi Young KimJi-Young ParkSu-Jin ParkYoung Bae RyuWoo Song Lee
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2012 Volume 35 Issue 5 Pages 786-790

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Abstract

In this study, twelve neuraminidase (NA) inhibitory compounds 112 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 IC50 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.

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© 2012 The Pharmaceutical Society of Japan
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