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A new diketopiperazine-like inhibitor of bone morphogenetic protein-induced osteoblastic differentiation produced by marine-derived Aspergillus sp. BFM-0085

机译:一种新的Diketopiperazine抑制剂的骨形态发生蛋白诱导的骨髓细胞分化,由海洋衍生的曲霉菌Sp产生。 BFM-0085

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摘要

A new diketopiperazine-like compound, designated protuboxepin K (1), was isolated together with the known structurally related protuboxepin A (2) from culture broth of the marine-derived fungal strain Aspergillus sp. BFM-0085 isolated from a sediment sample of Tokyo Bay. The structure of protuboxepin K was elucidated by spectroscopic data, including 1D and 2D NMR. Compounds 1 and 2 inhibited bone morphogenetic protein (BMP)-induced alkaline phosphatase activity with IC50 values of 4.7 and 25.2 mu M, respectively, in mutant BMP receptor-carrying C2C12(R206H) cells.
机译:一种新的Diketoperazine化合物,指定的Protuboxepin K(1)与来自海洋衍生的真菌菌株Aspergillus sp的培养液中的已知的结构相关的protuboxeina(2)分离。 BFM-0085与东京湾的沉积物样本隔离。 通过光谱数据阐明protuboxepin k的结构,包括1D和2D NMR。 化合物1和2分别抑制骨形态发生蛋白(BMP)抑制的碱性磷酸酶,其分别在突变BMP受体的C2C12(R206H)细胞中分别具有4.7和25.2μm的IC 50值。

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    Kitasato Univ Grad Sch Pharmaceut Sci Dept Microbial Chem Minato Ku 5-9-1 Shirokane Tokyo;

    Kitasato Univ Sch Pharm Dept Microbial Chem Minato Ku 5-9-1 Shirokane Tokyo 1088641 Japan;

    Kitasato Univ Grad Sch Pharmaceut Sci Dept Microbial Chem Minato Ku 5-9-1 Shirokane Tokyo;

    Saitama Med Univ Res Ctr Genom Med Div Pathophysiol 1397-1 Yamane Hidaka Saitama 3501241 Japan;

    Tokyo Univ Marine Sci &

    Technol Grad Sch Marine Sci &

    Technol Minato Ku 4-5-7 Konan Tokyo;

    Kitasato Univ Grad Sch Pharmaceut Sci Dept Microbial Chem Minato Ku 5-9-1 Shirokane Tokyo;

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  • 正文语种 eng
  • 中图分类 药学;
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