Isolated compounds and semi-synthetic derivatives from Miconia ferruginata as inhibitors of cathepsins K and B and their cytotoxic evaluation

Resumo

Miconia genus, belonging to Melastomataceae family, is widely distributed in tropical America. Isolated compounds and semi-synthetic derivatives from Miconia ferruginata leaves were evaluated both for their cytotoxicity on tumor cell lines and against important proteolytic enzymes such as cathepsins B and K. Among the evaluated compounds, the mixture of methyl ursolate (2a) and oleanate (3a) showed considerable cytotoxicity against melanoma (MDA-MB435) and colon cancer (HCT-8) cell lines. In addition, it was also demonstrated that the mixture of ursolic (2) and oleanolic (3) acids inhibited of the cathepsin B, with IC₅₀ value of 13.02 μM. On the other hand, mixture of compounds 2a and 3a showed considerable activity against cathepsin K, with IC₅₀ value of 1.42 μM. The compound 5,6,7-trihydroxy 4’-methoxyflavone (1) showed no activity.