Biological and Pharmaceutical Bulletin
Online ISSN : 1347-5215
Print ISSN : 0918-6158
ISSN-L : 0918-6158
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1,3-Selenazol-4-one Derivatives Inhibit Inducible Nitric Oxide-Mediated Nitric Oxide Production in Lipopolysaccharide-Induced BV-2 Cells
Young-Joon ParkMamoru KoketsuJeong Min KimJoo-Hong YeoHideharu IshiharaKwang-Gill LeeSun Yeou KimChong-Kook Kim
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2003 Volume 26 Issue 12 Pages 1657-1660

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Abstract

Activated microglia extensively produce nitric oxide (NO) by inducing expression of inducible NO synthase (iNOS). NO plays a deleterious role in brain inflammation and neuronal death. In the present study, we investigated the effects of 1,3-selenazol-4-one derivatives (Sz-A, B, C, D and E) on NO production and iNOS expression in lipopolysaccharide (LPS)-induced BV-2 cells, a murine microglia cell line. Among these compounds, Sz-B and C remarkably inhibited LPS-induced NO production relative to that of Sz-A, D, and E at 5 μM in BV-2 cells. Sz-B and C dose-dependently inhibited NO production at 1, 5, and 10 μM without toxicity to BV-2 cells. Sz-B and C also dose-dependently suppressed iNOS expression at the same concentrations in LPS-induced BV-2 cells. This result suggests that Sz-B and C inhibit iNOS-mediated NO production in LPS-induced BV-2 cells. Structurally, Sz-B and C bear an ethyl or methyl group at the 5 positions of the 4-selenazolone skeletons, which could play an important role in inhibiting iNOS-mediated NO production.

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© 2003 The Pharmaceutical Society of Japan
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