Noncompetitive Inhibition of RvH1N1 Neuraminidase by Luteolin and Rosmarinic Acid Isolated from Perilla frutescens

다국어 초록 (Multilingual Abstract)

The influenza neuraminidase (E.C. 3.2.1.18) is an antiviral target of high pharmaceutical interest because of its essential role in cleaving sialic acid residues from surface glycoproteins and facilitating release of virions from infected cell. In this context, polyphenolic compounds including luteolin, rosmarinic acid, and apigenin from Perilla frutescens were evaluated for their inhibitory effect on recombinant virus H1N1 neuraminidase. Among the test compounds, luteolin and rosmarinic acid inhibited the rvH1N1 neuraminidase with an IC50 of 8.4 and 46.7 μM, respectively. The inhibition kinetics analyzed by Dixon plots indicates that luteolin and rosmarinic acid are noncompetitive inhibitor and inhibition constant, Ki, were established as 14.3 and 43.9 μM, respectively. Subsequently, we also analyzed the rosmarinic acid and luteolin contents of 383 accessions of perilla seed germplasms by high performance liquid chromatography (HPLC). The rosmarinic acid and luteolin contents of perilla seeds were ranged from 15.7 μg/g to 2,894.9 μg/g and from 1.6 μg/g to 949.1 μg/g, respectively.