Seki Reiko, Nagai Kenichiro, Kobayashi Keisuke, Shigeno Satoru, Shirahata Tatsuya, Kobayashi Yoshinori, Ohshiro Taichi, Tomoda Hiroshi
Medical Research Laboratories, Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
Department of Microbial Chemistry, Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo, 108-8641, Japan.
J Antibiot (Tokyo). 2025 Jan;78(1):26-34. doi: 10.1038/s41429-024-00785-5. Epub 2024 Nov 14.
Celludinones A and B, isolated from the fungus Talaromyces cellulolyticus BF-0307, were inhibitors of sterol O-acyltransferase (SOAT). Further searches for their congeners in the culture broth of the fungus by LC/UV and LC/MS analysis resulted in the discovery of four structurally related compounds, including a new dihydroisobenzofuran named celludinone C (1). The structure of 1, including its absolute stereochemistry, was elucidated by 1D/2D NMR and electronic circular dichroism (ECD) spectra. All of these compounds inhibited both SOAT1 and 2, with IC values ranging from 8.5 to 30 µM.
从解纤维素篮状菌BF - 0307中分离得到的纤维地菌素A和B是固醇O - 酰基转移酶(SOAT)的抑制剂。通过LC/UV和LC/MS分析在该真菌的培养液中进一步寻找它们的同系物,结果发现了四种结构相关的化合物,包括一种名为纤维地菌素C(1)的新二氢异苯并呋喃。通过一维/二维核磁共振和电子圆二色(ECD)光谱阐明了1的结构,包括其绝对立体化学。所有这些化合物均抑制SOAT1和SOAT2,IC值范围为8.5至30 μM。