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C-Methylated Flavonoids from Cleistocalyx operculatus and Their Inhibitory Effects on Novel Influenza A (H1N1) Neuraminidase

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

  • Trong-Tuan Dao
  • Bui-Thanh Tung
  • Phi-Hung Nguyen
  • Phuong-Thien Thuong
  • Sung-Sik Yoo
  • Eun-Hee Kim
  • Sang-Kyum Kim
  • Won-Keun Oh

As part of an ongoing study focused on the discovery of anti-influenza agents from plants, four new (1-4) and 10 known (5-14) C-methylated flavonoids were isolated from a methanol extract of Cleistocalyx operculatus buds using an influenza H1N1 neuraminidase inhibition assay. Compounds 4, 7, 8, and 14, with a chalcone skeleton, showed significant inhibitory effects on the viral neuraminidases from two influenza viral strains, H1N1 and H9N2. Compound 4 showed the strongest inhibitory activity against the neuraminidases from novel influenza H1N1 (WT) and oseltamivir-resistant novel H1N1 (H274Y mutant) expressed in 293T cells with IC50 values of 8.15 ± 1.05 and 3.31 ± 1.34 μM, respectively. Compounds 4, 7, 8, and 14 behaved as noncompetitive inhibitors in the kinetic studies. These results indicate that C-methylated flavonoids from C. operculatus have the potential to be developed as neuraminidase inhibitors for novel influenza H1N1.

OriginalsprogEngelsk
TidsskriftJournal of Natural Products
Vol/bind73
Udgave nummer10
Sider (fra-til)1636-42
Antal sider7
ISSN0163-3864
DOI
StatusUdgivet - 22 okt. 2010

ID: 169013313