Antiproliferative effect of benzophenones and their influence on cathepsin activity |
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| Authors: | Ramiro Mendonça Murata Regiane Yatsuda Marcelo Henrique dos Santos Luciana K Kohn Felipe Terra Martins Tanus Jorge Nagem Severino Matias Alencar João Ernesto de Carvalho Pedro Luiz Rosalen |
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| Institution: | 1. Department of Physiological Sciences, Faculty of Dentistry of Piracicaba, State University of Campinas (UNICAMP), SP, Brazil;2. Department of Pharmacy, Laboratory of Phytochemistry and Medicinal Chemistry, Federal University of Alfenas (UNIFAL‐MG), MG, Brazil;3. The Chemical, Biological and Agricultural Pluridisciplinary Research Center (CPQBA), State University of Campinas (UNICAMP), SP, Brazil;4. Department of Chemistry, Federal University of Ouro Preto (UFOP), MG, Brazil;5. Department of Agri‐Food Industry, Food and Nutrition, Luiz de Queiroz College of Agriculture, University of S?o Paulo (USP), SP, Brazil |
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| Abstract: | 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. Copyright © 2009 John Wiley & Sons, Ltd. |
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| Keywords: | antiproliferative cathepsin Rheedia brasiliensis garciniaphenone 7‐epiclusianone |
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