Tetradehydrohalicyclamine B,a new proteasome inhibitor from the marine sponge Acanthostrongylophora ingens |
| |
| Authors: | Hikaru Kato Ahmed H El-Desoky Yuya Takeishi Tatsuo Nehira Esther D Angkouw Remy EP Mangindaan Nicole J de Voogd Sachiko Tsukamoto |
| |
| Institution: | 1. Department of Natural Products, Graduate School of Pharmaceutical Sciences, Kumamoto University, Oe-honmachi 5-1, Kumamoto 862-0973, Japan;2. Pharmaceutical and Drug Industries Research Division, Pharmacognosy Department, National Research Centre, PO 12622, 33 El Bohouth St., Dokki, Giza, Egypt;3. Graduate School of Integrated Arts and Sciences, Hiroshima University, 1-7-1 Kagamiyama, Higashi-hiroshima 739-8521, Japan;4. Faculty of Fisheries and Marine Science, Sam Ratulangi University, Kampus Bahu, Manado 95115, Indonesia;5. Naturalis Biodiversity Center, P.O. Box 9517, 2300 RA Leiden, The Netherlands |
| |
| Abstract: | A new halicyclamine derivative, tetradehydrohalicyclamine B (1), was isolated from the marine sponge Acanthostrongylophora ingens, along with halicyclamine B (2) as proteasome inhibitors. Compound 1 is the second example found to have a pyridinium ring in the halicyclamine family. Although the relative configuration of 2 was previously determined by X-ray crystallographic analysis, here we determined the absolute configuration of 2 by ECD experiment. Compounds 1 and 2 inhibited the constitutive proteasome as well as the immunoproteasome. The inhibitory activities of 2 were 4- to 10-fold more potent than those of 1. |
| |
| Keywords: | Proteasome inhibitor Constitutive proteasome Immunoproteasome Halicyclamine Corresponding author |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
