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Inhibition of Lipopolysaccharide‐Induced Nitric Oxide Production by Antofine and Its Analogues in RAW 264.7 Macrophage Cells
Authors:Hye‐Young Min  Su‐Hyun Song  Boeun Lee  Sanghee Kim  Sang Kook Lee
Affiliation:1. College of Pharmacy and Division of Life & Pharmaceutical Sciences, Ewha Womans University, 11‐1 Daehyun‐dong, Seodaemun‐ku, Seoul 120‐750, Korea, (phone: +82‐2‐3277‐2851;2. fax: +82‐2‐3277‐2851);3. College of Pharmacy, Seoul National University, San 56‐1, Shilim‐dong, Gwanak‐gu, Seoul 151‐742, Korea
Abstract:Based on the anti‐inflammatory activity of phenanthroindolizidine alkaloids, the inhibitory effect of antofine and its analogues on lipopolysaccharide (LPS)‐induced nitric oxide (NO) production was examined, and structure–activity relationships are discussed. Antofine and several analogues suppressed NO production in LPS‐stimulated RAW 264.7 cells. The MeO group at C(2), and the bulkiness of the substituents at C(3) and C(6) in the phenanthrene ring might be critical for this effect. Besides, regulation of iNOS expression might be involved in the inhibitory effect of antofine on LPS‐induced NO production in macrophage cells.
Keywords:Phenanthroindolizidine alkaloids  Antofine analogues  Nitric oxide (NO) production  iNOS Expression  Structure–  activity relationships (SAR)  Alkaloids  Inhibitors
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