کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358574 | 981349 | 2016 | 6 صفحه PDF | دانلود رایگان |
Sixteen novel hesperetin derivatives containing Mannich base moiety were designed and synthesized and their anti-inflammatory activities were evaluated by inhibiting tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) in mouse RAW264.7 macrophages. Compounds 3a–3k showed better hydrophilic, while compounds 3l–3p with aromatic groups was hydrophobic. The anti-inflammatory activity of title compounds was correlated with log P values, among them, compounds 3c, 3e and 3i with minus log P values exhibited best anti-inflammatory activity through decreasing both IL-6 and TNF-α. Furthermore, the expression of LPS-induced notch1 and inos was reduced by compounds 3c, 3e, and 3i, and compound 3e attenuated LPS-induced inos protein levels in a dose-dependent manner.
Novel hesperetin derivatives exhibited higher anti-inflammatory activity through decreasing both IL-6 and TNF-α. Western blot analysis revealed that compound 3e inhibited LPS-induced notch1 and inos proteins in RAW264.7 macrophages.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 5, 1 March 2016, Pages 1460–1465