The antiproliferative activity of two prenylated benzophenones isolated from Rheedia brasiliensis, the triprenylated garciniaphenone and the tetraprenylated benzophenone 7‐epiclusianone, was investigated against human cancer cell lines. The antiproliferative activity on melanoma (UACC‐62), breast...

The antiproliferative activity of two prenylated benzophenones isolated from Rheedia brasiliensis, the triprenylated garciniaphenone and the tetraprenylated benzophenone 7‐epiclusianone, was investigated against human cancer cell lines. The antiproliferative activity on melanoma (UACC‐62), breast (MCF‐7), drug‐resistant breast (NCI‐ADR), lung/non‐small cells (NCI460), ovarian (OVCAR 03), prostate (PC03), kidney (786‐0), lung (NCI‐460) and tongue (CRL‐1624 and CRL‐1623) cancer cells was determined using spectrophotometric quantification of the cellular protein content. The effect of these benzophenones on the activity of cathepsins B and G was also investigated. Garciniaphenone displayed cytostatic activity in all cell lines, whereas 7‐epiclusianone showed a dose‐dependent cytotoxic effect. The IC50 values for cell proliferation revealed that 7‐epiclusianone is more active than garciniaphenone against most of the cell lines. Furthermore, the antiproliferative effects demonstrated by garciniaphenone and 7‐epiclusianone were related to their cathepsin inhibiting properties. In conclusion, 7‐epiclusianone is a promising naturally occurring agent which displays multiple inhibitory effects which may be working in concert to inhibit cancer cell proliferation in vitro. The putative pathway by which 7‐epiclusianone affects cancer cell development may involve cathepsin inhibition

CONSELHO NACIONAL DE DESENVOLVIMENTO CIENTÍFICO E TECNOLÓGICO - CNPQ

141253/2005-3

FINANCIADORA DE ESTUDOS E PROJETOS - FINEP

1110/06

fechado