Journal
CHEMICAL & PHARMACEUTICAL BULLETIN
Volume 62, Issue 5, Pages 415-421Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/cpb.c13-00897
Keywords
flavonoid; anti-influenza virus; H1N1 Tamiflu-resistant virus; H3N2 virus
Funding
- National Science Council [NSC 99-2320-B-016-005-MY3, 100-EC-17-A-20-S1-028]
- Ministry of Economic Affairs of the Republic of China
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A series of novel flavones derivatives were synthesized based on modification of the active ingredients of a traditional Chinese medicine Scutellaria baicalensis GEORGI and screened for anti-influenza activity. The synthetic baicalein (flavone) analogs, especially with the B-rings substituted with bromine atoms, were much more potent than oseltamivir or ribavirin against H1N1 Tamiflu-resistant (H1N1 TR) virus and usually with more favorable selectivity. The most promising were 5b, 5c, 6b and 6c, all displaying an 50% effective concentration (EC50) at around 4.0-4.5 mu m, and a selective index (SI=50% cytotoxic concentration (CC50)/EC50)>70. For seasonal H3N2-infected influenza virus, both 5a and 5b with SI >17.3 indicated superior to ribavirin. The fiavonoids having both not-naturally-occurring bromo-substituted B-rings and appropriate hydroxyls positioning on the A-rings might be critical in determining the activity and selectivity against H1N1-Tamiflu-resistant infected influenza viruses.
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