Psammaplin A (PsA) is a phenolic natural product isolated from a marine sponge, which showed a potent cytotoxicity against several cancer cell lines. In present study, PsA was found to inhibit mammalian aminopeptidase N (APN) that plays a key role in tumor cell invasion and angiogenesis. PsA inhibited the APN activity with an IC50 of 18 μM in a non-competitive manner. Moreover, PsA potently inhibited the proliferation of several cancer and endothelial cells. Interestingly, the anti-proliferative effect of PsA was dependent on the cellular amount of APN expression. Finally, PsA suppressed the invasion and tube formation of endothelial cells stimulated by basic fibroblast growth factor. These data demonstrate that PsA is a new inhibitor of APN and can be developed as a novel anti-angiogenic agent.
Bibliographical noteFunding Information:
This work was supported by a grant number M102KM010001-03K1301-01911 for the 21C Frontier Functional Proteomics Center from the Ministry of Science and Technology, Republic of Korea and the Brain Korea 21 Project.
All Science Journal Classification (ASJC) codes
- Cancer Research