Antiproliferative effect of benzophenones and their infl uence on cathepsin activity.
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Data
2010
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Resumo
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
quantifi cation 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.
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Antiproliferative, Cathepsin, Rheedia brasiliensis, Garciniaphenone
Citação
MURATA, R. M. et al. Antiproliferative effect of benzophenones and their infl uence on cathepsin activity. Phytotherapy Research , v. 24, p. 379-383, 2010. Disponível em: <http://onlinelibrary.wiley.com/doi/10.1002/ptr.2954/abstract>. Acesso em: 20 mai. 2017.