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首页> 外文期刊>Bulletin of the Chemical Society of Japan >Total Synthesis of Stylissatin A, A Cyclic Peptide That Inhibits Nitric Oxide Production
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Total Synthesis of Stylissatin A, A Cyclic Peptide That Inhibits Nitric Oxide Production

机译:曲线合成型抑制一氧化氮生产的环状肽

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摘要

Stylissatin A is a proline-rich cyclic heptapeptide isolated from the Papua New Guinean marine sponge Stylissa massa. The first synthesis of stylissatin A was achieved by a combination of solid-phase and solution-phase peptide synthesis. The natural and synthetic samples of stylissatin A showed comparable inhibitory effects on nitric oxide production with negligible cytotoxicity in lipopolysaccharide (LPS)-stimulated murine macrophage RAW264.7 cells (EC50 = 73 mu M for synthetic sample). Furthermore, while the D-allo-Ile(5) epimer was less potent, a tert-butyl ether analog of stylissatin A was approximately six times more potent than the natural product (EC50 = 12 mu M).
机译:Trysissatin A是从巴布亚新几内亚海绵Stylsa Massa中分离的富含脯氨酸的环状肽。 通过固相和溶液相肽合成的组合实现了曲调A的第一合成。 曲调A的天然和合成样品对脂多糖(LPS) - 刺激的鼠巨噬细胞Raw264.7细胞(EC50 =73μm用于合成样品的胰岛素毒性,具有可忽略的细胞毒性的相当抑制作用。 此外,虽然D-Allo-ILE(5)缩小剂不太有效,但晶状体A的叔丁基醚类似物比天然产物(EC50 =12μm)大约六倍。

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    Univ Tsukuba Sch Integrat &

    Global Majors SIGMA Tsukuba Ibaraki 3058571 Japan;

    Univ Tsukuba Grad Sch Pure &

    Appl Sci 1-1-1 Tennodai Tsukuba Ibaraki 3058571 Japan;

    Univ Tsukuba Grad Sch Pure &

    Appl Sci 1-1-1 Tennodai Tsukuba Ibaraki 3058571 Japan;

    Univ Tsukuba Grad Sch Pure &

    Appl Sci 1-1-1 Tennodai Tsukuba Ibaraki 3058571 Japan;

    Univ Tsukuba Grad Sch Pure &

    Appl Sci 1-1-1 Tennodai Tsukuba Ibaraki 3058571 Japan;

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  • 正文语种 eng
  • 中图分类 化学;
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