来自一种海洋蓝藻奥氏藻属（Okeania sp.）的甾醇O-酰基转移酶抑制剂双鞘藻酰胺A、B和C。
Biseokeaniamides A, B, and C, Sterol O-Acyltransferase Inhibitors from an Okeania sp. Marine Cyanobacterium.
作者信息
Iwasaki Arihiro, Tadenuma Takato, Sumimoto Shimpei, Ohshiro Taichi, Ozaki Kaori, Kobayashi Keisuke, Teruya Toshiaki, Tomoda Hiroshi, Suenaga Kiyotake
机构信息
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.
出版信息
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。
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