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Molecules 2013, 18(3), 3543-3561; doi:10.3390/molecules18033543
Article

Cyclic versus Hemi-Bastadins. Pleiotropic Anti-Cancer Effects: from Apoptosis to Anti-Angiogenic and Anti-Migratory Effects

1,* , 2
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1 Laboratoire de Toxicologie, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), Campus de la Plaine, Boulevard du Triomphe, 1050 Brussels, Belgium 2 Laboratoire de Pharmacie Galénique et de Biopharmacie, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), Campus de la Plaine, Boulevard du Triomphe, 1050 Brussels, Belgium 3 Service de Neurochirurgie, Hôpital Erasme, ULB, Route de Lennik, 1070 Brussels, Belgium 4 Institute of Pharmaceutical Biology and Biotechnology, Heinrich-Heine University Düsseldorf, Universitätsstrasse 1, 40225 Düsseldorf, Germany
* Author to whom correspondence should be addressed.
Received: 16 January 2013 / Revised: 4 February 2013 / Accepted: 8 March 2013 / Published: 19 March 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Bastadins-6, -9 and -16 isolated from the marine sponge Ianthella basta displayed in vitro cytostatic and/or cytotoxic effects in six human and mouse cancer cell lines. The in vitro growth inhibitory effects of these bastadins were similar in cancer cell lines sensitive to pro-apoptotic stimuli versus cancer cell lines displaying various levels of resistance to pro-apoptotic stimuli. While about ten times less toxic than the natural cyclic bastadins, the synthetically derived 5,5'-dibromohemibastadin-1 (DBHB) displayed not only in vitro growth inhibitory activity in cancer cells but also anti-angiogenic properties. At a concentration of one tenth of its in vitro growth inhibitory concentration, DBHB displayed actual antimigratory effects in mouse B16F10 melanoma cells without any sign of cytotoxicity and/or growth inhibition. The serum concentration used in the cell culture media markedly influenced the DBHB-induced antimigratory effects in the B16F10 melanoma cell population. We are currently developing a specific inhalation formulation for DBHB enabling this compound to avoid plasmatic albumin binding through its direct delivery to the lungs to combat primary as well as secondary (metastases) tumors.
Keywords: bastadins; hemibastadins; angiogenesis; apoptosis; cancer bastadins; hemibastadins; angiogenesis; apoptosis; cancer
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).
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Mathieu, V.; Wauthoz, N.; Lefranc, F.; Niemann, H.; Amighi, K.; Kiss, R.; Proksch, P. Cyclic versus Hemi-Bastadins. Pleiotropic Anti-Cancer Effects: from Apoptosis to Anti-Angiogenic and Anti-Migratory Effects. Molecules 2013, 18, 3543-3561.

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