| Literature DB >> 17765550 |
Shunji Aoki1, Yasuo Watanabe, Daiki Tanabe, Masayoshi Arai, Hideaki Suna, Katsushiro Miyamoto, Hiroshi Tsujibo, Kazutake Tsujikawa, Hiroshi Yamamoto, Motomasa Kobayashi.
Abstract
Previously, bioassay-guided separation led us to isolate eleven novel steroidal alkaloids named cortistatins from the marine sponge Corticium simplex. These cortistatins were classified into three types based on the chemical structure of the side chain part, that is, isoquinoline, N-methyl piperidine or 3-methylpyridine units. From the structure-activity relationship study, the isoquinoline unit in the side chain was found to be crucial for the anti-angiogenic activity of cortistatins. Cortistatin A (1) showed cytostatic growth-inhibitory activity against human umbilical vein endothelial cells (HUVECs). Cortistatin A (1) also inhibited VEGF-induced migration of HUVECs and bFGF-induced tubular formation. Although cortistatin A (1) showed no effect on VEGF-induced phosphorylation of ERK1/2 and p38, which are one of the signaling pathways for migration and tubular formation, the phosphorylation of the unidentified 110kDa protein in HUVECs was inhibited by the treatment with cortistatin A.Entities:
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Year: 2007 PMID： 17765550 DOI： 10.1016/j.bmc.2007.08.017
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641