Flavonolignans silybin and dehydrosilybin, isolated from the seeds of the milk thistle (Silybum marianum) have chemoprotective effects and they act as potent regulators of the cell cycle. New derivatives of silybin will be prepared, e.g., conjugates with saturated and unsaturated fatty acids, aromatic phenolic acids (e.g. gallate), conjugates with other antioxidants (e.g. tokoferol) and multivalent/oligomeric derivatives. Also dehydrosilybin and possibly other flavonolignans of silymarin complex will be used for these derivatizations. New compounds will be tested for chemoprotective and antiangiogenic activity aiming at anticancer preparations with suppressed negative cytotoxic effects. (en)
Příprava konjugátů silybinu s mastnými a fenolovými kyselinami pomocí chemických a enzymových metod s cílem přípravy účinných antiangiogenních a chemoprotektivních preparátů
Byly připraveny konjugáty silybinu s mastnými kyselinami, testy na antivirotickou aktivitu (virus chřipky) pokázaly výraznou aktivitu při nízké cytotoxicitě. Konjugáty byly použity k separaci silybinu A a B pomocí lipas. Serie galoyl derivátů silybinů A a B a dehydrosilybinu byla testována na antiangiogenní aktivitu. Nejvyšší aktivitu (inhibice HUVEC proliferace) měl 7-O-galloylsilybin. (cs)
Newly prepared silybin fatty acid conjugates proved to be active against influenza virus without substantial cyctotoxicity. These conjugates were used for the silybin A and B separation using lipases. Series of silybin A and B and dehydrosilybin galloyl derivatives was tested for antiangiogenic activity. The highest activity (HUVEC proliferation inhibition) has 7-O-galloylsilybin. (en)