L. Pochet

3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo.

In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate. Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT1080 or MDA-MB231 cells were treated i.p. 3 days week−1 with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents.

Study of the influence of g-cyclodextrin on the molsidomine photostability

Molsidomine, a very useful therapeutic agent for the treatment of coronary heart disease, is extremely light sensitive. The aim of this work is to study the influence of cyclodextrins on the molsidomine photostability. Different molsidomine-γ-cyclodextrin (CD) complexes were prepared by spray-drying and the inclusion could be demonstrated by different methods as the DSC and the FTIR spectroscopy. The photostability was tested at 4500 lux. We could show that γ-CD would not have a better protective effect on molsidomine than lactose, mannitol or NaCl, in the same weight ratio and that there is a linear relationship between the half life time and the percentage of molsidomine contained in the mixtures or the complexes.