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.
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。
