Iwasaki Arihiro, Tadenuma Takato, Sumimoto Shimpei, Ohshiro Taichi, Ozaki Kaori, Kobayashi Keisuke, Teruya Toshiaki, Tomoda Hiroshi, Suenaga Kiyotake
Department of Chemistry, Faculty of Science and Technology, Keio University , 3-14-1 Hiyoshi, Kohoku-ku, Yokohama, Kanagawa 223-8522, Japan.
Graduate School of Pharmaceutical Sciences, Kitasato University , 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
J Nat Prod. 2017 Apr 28;80(4):1161-1166. doi: 10.1021/acs.jnatprod.7b00137. Epub 2017 Mar 15.
Biseokeaniamides A, B, and C (1-3), structurally novel sterol O-acyltransferase (SOAT) inhibitors, were isolated from an Okeania sp. marine cyanobacterium. Their structures were elucidated by spectroscopic analyses and degradation reactions. Biseokeaniamide B (2) exhibited moderate cytotoxicity against human HeLa cancer cells, and compounds 1-3 inhibited both SOAT1 and SOAT2, not only at an enzyme level but also at a cellular level. Biseokeaniamides (1-3) are the first linear lipopeptides that have been shown to exhibit SOAT-inhibitory activity.
双鞘海鞘酰胺A、B和C（1-3）是从一种鞘海鞘属海洋蓝细菌中分离得到的结构新颖的固醇O-酰基转移酶（SOAT）抑制剂。通过光谱分析和降解反应阐明了它们的结构。双鞘海鞘酰胺B（2）对人宫颈癌细胞HeLa表现出中等细胞毒性，化合物1-3不仅在酶水平而且在细胞水平上均抑制SOAT1和SOAT2。双鞘海鞘酰胺（1-3）是首批被证明具有SOAT抑制活性的线性脂肽。
