Department of Cell and Developmental Biology, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA.
Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0358, USA.
Bioorg Med Chem. 2010 Mar 15;18(6):2115-2122. doi: 10.1016/j.bmc.2010.02.007. Epub 2010 Feb 10.
The cellular activity of norrisolide (7), a novel Golgi-vesiculating agent, was dissected as function of its chemical structure. This natural product induces irreversible vesiculation of the Golgi membranes and blocks protein transport at the level of the Golgi. The Golgi localization and fragmentation effects of 7 depend on the presence of the perhydroindane core, while the irreversibility of fragmentation depends on the acetyl group of 7. We show that fluorescent derivatives of norrisolide are able to localize to the Golgi apparatus and represent important tools for the study of the Golgi structure and function.
诺里斯内酯（7）是一种新型的高尔基体囊泡形成剂，其细胞活性与其化学结构有关。该天然产物可诱导高尔基体膜不可逆囊泡化，并阻断高尔基体水平的蛋白质运输。7 的高尔基体定位和片段化作用取决于其过氢茚烷核心的存在，而片段化的不可逆性则取决于 7 的乙酰基。我们表明，诺里斯内酯的荧光衍生物能够定位于高尔基体器官，并且是研究高尔基体结构和功能的重要工具。
