کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1356722 981151 2008 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Structure–activity relationship of flavonoids as influenza virus neuraminidase inhibitors and their in vitro anti-viral activities
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Structure–activity relationship of flavonoids as influenza virus neuraminidase inhibitors and their in vitro anti-viral activities
چکیده انگلیسی

Flavonoids are polyphenolic compounds that widely exist in plant kingdom, and the structure–activity relationship (SAR) of 25 flavonoids was studied on neuraminidase (NA) activity of influenza virus. Three typical influenza virus strains A/PR/8/34 (H1N1), A/Jinan/15/90 (H3N2), and B/Jiangshu/10/2003 were used as the source of NAs, the average of IC50s of these compounds on these NAs was used in the SAR analysis. The order of potency for NA inhibition was as follows: aurones > flavon(ol)es > isoflavones > flavanon(ol)es and flavan(ol)es. The SAR analysis of flavonoids on influenza virus NAs revealed that for good inhibitory effect, the 4′-OH, 7-OH, C4O, and C2C3 functionalities were essential, and the presence of a glycosylation group greatly reduced NA inhibition. The in vitro anti-viral activities of eight flavonoids were evaluated using a cytopathic effect (CPE) reduction method, the assay results confirmed the SAR as influenza virus neuraminidase inhibitors. The findings of this study provide important information for the exploitation and utilization of flavonoids as NA inhibitors for influenza treatment.

The SAR analysis of flavonoids against influenza virus neuraminidase revealed that for good inhibitory effect, the 4′-OH, 7-OH, C4O and C2C3 functionalities were essential.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 15, 1 August 2008, Pages 7141–7147
نویسندگان
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