期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 11, 页码 3341-3343出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.029
关键词
Proteasome; Chymotrypsin-like activity; Sponge; Alkaloid
资金
- Ministry of Education, Culture, Sports, Science, and Technology of Japan [18032033, 19310140]
- Naito Foundation
- Astellas Foundation for Research on Metabolic Disorders
Aaptamine (1), isoaaptamine (2), and demethylaaptamine (3) were isolated from the marine sponge Aaptos suberitoides collected in Indonesia as inhibitors of the proteasome. They inhibited the chymotrypsin-like and caspase-like activities of the proteasome with IC50 values of 1.6-4.6 mu g/mL, while they showed less inhibition of the trypsin-like activity of the proteasome. The three compounds showed cytotoxic activities against HeLa cells, but their cytotoxicity did not correlate with their potency as proteasome inhibitors, strongly suggesting that their proteasomal inhibitory activity is dispensable to their cytotoxicity. (C) 2010 Elsevier Ltd. All rights reserved.
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