Planta Med 2012; 78 - PD95
DOI: 10.1055/s-0032-1320453

The alkaloid 1-hydroxy-rutaecarpine inhibits cathepsin activity

MC de M Burger 1, SD Ramalho 1, JB Fernandes 1, M de Fátima das G F da Silva 1, PC Vieira 1
  • 1Department of Chemistry, Federal University of São Carlos, São Carlos -SP, 13565–905, Brazil

Cathepsins B, L and K are cysteine proteases involved in various physiological and pathological processes. CatB and L are involved in tumoral processes while catK in cases of bone resorption. In a search for cathepsin inhibitors we have isolated from Metrodorea stipullaris, a number of compounds, among them the alkaloid 1-hydroxy-rutaecarpine which displayed moderate inhibitory activity on those enzymes. The alkaloid showed inhibition of 79% on cathepsin B, 100% on cathepsin L and 87.5% on cathepsin K, at the concentration of 125µg/ml for the three cathepsins. IC50 experiments were run and the values obtained are described in the table below.

Fig.1: 1-hydroxy-rutaecarpine

Tab.1: IC50 values