海洋来源aspergillus sp. BFM-0085 产生的一种新的骨形态发生蛋白诱导成骨细胞分化的二酮哌嗪样抑制剂。
A new diketopiperazine-like inhibitor of bone morphogenetic protein-induced osteoblastic differentiation produced by marine-derived Aspergillus sp. BFM-0085.
机构信息
Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
Department of Microbial Chemistry, School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
出版信息
J Antibiot (Tokyo). 2020 Aug;73(8):554-558. doi: 10.1038/s41429-020-0316-3. Epub 2020 May 21.
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 IC values of 4.7 and 25.2 μM, respectively, in mutant BMP receptor-carrying C2C12(R206H) cells.
一种新的二酮哌嗪类化合物，命名为原盒菌素 K（1），与已知结构相关的原盒菌素 A（2）一起从海洋来源的真菌 Aspergillus sp. BFM-0085 的发酵液中分离得到，该真菌分离自东京湾的沉积物样本。原盒菌素 K 的结构通过包括 1D 和 2D NMR 在内的光谱数据阐明。化合物 1 和 2 在携带突变型 BMP 受体的 C2C12(R206H)细胞中分别以 4.7 和 25.2 μM 的 IC 值抑制骨形态发生蛋白（BMP）诱导的碱性磷酸酶活性。
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