|Cyclic versus hemi-bastadins. Pleiotropic anti-cancer effects: from apoptosis to anti-angiogenic and anti-migratory effects|Mathieu, V.; Wauthoz, N.; Lefranc, F.; Niemann, H.; Amighi, K.; Kiss, R.; Proksch, P. (2013). Cyclic versus hemi-bastadins. Pleiotropic anti-cancer effects: from apoptosis to anti-angiogenic and anti-migratory effects. Molecules 18(3): 3543-3561. dx.doi.org/10.3390/molecules18033543
In: Molecules. MDPI: Basel. ISSN 1420-3049, more
bastadins; hemibastadins; angiogenesis; apoptosis; cancer
|Authors|| || Top |
- Mathieu, V.
- Wauthoz, N.
- Lefranc, F.
- Niemann, H.
- Amighi, K.
- Kiss, R.
- Proksch, P.
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.