Antiproliferative Effect of Benzophenones and their Influence on Cathepsin Activity

作者：Murata Ramiro Mendonca^*; Yatsuda Regiane; dos Santos Marcelo Henrique; Kohn Luciana K; Martins Felipe Terra; Nagem Tanus Jorge; Alencar Severino Matias; de Carvalho Joao Ernesto; Rosalen Pedro Luiz

来源：Phytotherapy Research, 2010, 24(3): 379-383.

DOI：10.1002/ptr.2954

• antiproliferative
• cathepsin
• Rheedia brasiliensis
• garciniaphenone
• 7-epiclusianone

The antiproliferative activity of two prenylated benzophenones isolated from Rheedia brasiliensis. the tri-prenylated 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.

• 出版日期2010-3