期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 20, 期 14, 页码 4437-4442出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.05.044
关键词
Ubiquitin-activating enzyme inhibitor; Indole alkaloid; Hyrtios reticulatus; Marine sponge
资金
- Ministry of Education, Culture, Sports, Science and Technology of Japan [22310138, 22406001]
- Naito Foundation
- Astellas Foundation for Research on Metabolic Disorders
- Uehara Memorial Foundation
- Grants-in-Aid for Scientific Research [22310138, 22406001] Funding Source: KAKEN
Hyrtioreticulins A-E (1-5) were isolated from the marine sponge Hyrtios reticulatus, along with a known alkaloid, hyrtioerectine B (6). Structural elucidation on the basis of spectral data showed that 1, 2, and 5 are new tetrahydro-beta-carboline alkaloids, while 3 and 4 are new azepinoindole-type alkaloids. Hyrtioreticulins A and B (1 and 2) inhibited ubiquitin-activating enzyme (E1) with IC50 values of 0.75 and 11 mu g/mL, respectively, measured by their inhibitory abilities against the formation of an E1-ubiquitin intermediate. So far, only five E1 inhibitors, panapophenanthrine, himeic acid A, largazole, and hyrtioreticulins A and B (1 and 2), have been isolated from natural sources and, among them, 1 is the most potent E1 inhibitor. (C) 2012 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据