Aminopeptidase N inhibition could be involved in the anti-angiogenic effect of dobesilates

作者：Farsa Oldrich^*; Sedlakova Sarka; Podlipna Jana; Maxa Jaroslav

来源：Journal of the Serbian Chemical Society, 2015, 80(5): 605-612.

DOI：10.2298/JSC131128032F

• 2,5-dihydroxybenzenesulfonic acid salts
• effect on CD13 activity
• neovascularization
• carcinogenesis
• vasculopathies

Calcium, magnesium and zinc 2,5-dihydroxybenzenesulfonates (dobesilates) were synthesized by sulfonation of hydroquinone with sulfuric acid under mild conditions. To form the salts, neutralization with calcium carbonate followed by cation exchange by means of magnesium or zinc sulfates was performed. The dobesilates were characterized by standard spectral methods and by AAS for metal content and then tested for inhibitory activity against aminopeptidase N. The calcium and magnesium 2,5-dihydroxybenzenesulfonates exhibited rather weak inhibitory activity to aminopeptidase N, as demonstrated by the IC50 values of 978.0 and 832.1 mu mol L-1, respectively, while zinc 2,5-dihydroxybenzenesulfonate reached a more significant inhibitory activity characterized by an IC50 value of 77.4 mu mol L-1. The results of the inhibition activity suggest that the inhibition of aminopeptidase N could play a role in the anti-angiogenic activity of 2,5-dihydroxybenzenesulfonates.

• 出版日期2015