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Plant polyphenolics as anti-invasive cancer agents

Marc Bracke UGent, Barbara Vanhoecke UGent, Lara Derycke UGent, Selin Bolca UGent, Sam Possemiers UGent, Arne Heyerick UGent, Chris Stevens UGent, Denis De Keukeleire UGent, Herman Depypere UGent and Willy Verstraete UGent, et al. (2008) ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY. 8(2). p.171-185
abstract
Because invasion is, either directly or via metastasis formation, the main cause of death in cancer patients, development of efficient anti-invasive agents is an important research challenge. We have established a screening program for potentially anti-invasive compounds. The assay is based on organotypic confronting cultures between human invasive cancer cells and a fragment of normal tissue in three dimensions. Anti-invasive agents appeared to be heterogeneous with regard to their chemical nature, but plant alkaloids, polyphenolics and some of their synthetic congeners were well represented. Even within this group, active compounds were quite diverse: (+)-catechin, tangeretin, xanthohumol and other prenylated chalcones, 3,7-dimethoxyflavone, a pyrazole derivative, an isoxazolylcoumarin and a prenylated desoxybenzoin. The data gathered in this system are now applied in two projects. Firstly, structure-activity relationships are explored with computer models using an artificial neural network approach, based on quantitative structural descriptors. The aim of this study is the prediction and design of optimally efficient anti-invasive compounds. Secondly, the metabolism of orally ingested plant polyphenolics by colonic bacteria is studied in a simulator of the human intestinal microbial ecosystem ( SHIME) and in human intervention trials. This method should provide information on the final bioavailability of the active compounds in the human body, with regard to microbial metabolism, and the feasibility of designing pre-or probiotics that increase the generation of active principles for absorption in the gastro-intestinal tract. The final and global aim of all these studies is to predict, synthesize and apply in vivo molecules with an optimal anti-invasive, and hence an anti-metastatic activity against cancer.
Please use this url to cite or link to this publication:
@article{866921,
  abstract     = {Because invasion is, either directly or via metastasis formation, the main cause of death in cancer patients, development of efficient anti-invasive agents is an important research challenge. We have established a screening program for potentially anti-invasive compounds. The assay is based on organotypic confronting cultures between human invasive cancer cells and a fragment of normal tissue in three dimensions. Anti-invasive agents appeared to be heterogeneous with regard to their chemical nature, but plant alkaloids, polyphenolics and some of their synthetic congeners were well represented. Even within this group, active compounds were quite diverse: (+)-catechin, tangeretin, xanthohumol and other prenylated chalcones, 3,7-dimethoxyflavone, a pyrazole derivative, an isoxazolylcoumarin and a prenylated desoxybenzoin. The data gathered in this system are now applied in two projects. Firstly, structure-activity relationships are explored with computer models using an artificial neural network approach, based on quantitative structural descriptors. The aim of this study is the prediction and design of optimally efficient anti-invasive compounds. Secondly, the metabolism of orally ingested plant polyphenolics by colonic bacteria is studied in a simulator of the human intestinal microbial ecosystem ( SHIME) and in human intervention trials. This method should provide information on the final bioavailability of the active compounds in the human body, with regard to microbial metabolism, and the feasibility of designing pre-or probiotics that increase the generation of active principles for absorption in the gastro-intestinal tract. The final and global aim of all these studies is to predict, synthesize and apply in vivo molecules with an optimal anti-invasive, and hence an anti-metastatic activity against cancer.},
  author       = {Bracke, Marc and Vanhoecke, Barbara and Derycke, Lara and Bolca, Selin and Possemiers, Sam and Heyerick, Arne and Stevens, Chris and De Keukeleire, Denis and Depypere, Herman and Verstraete, Willy and Williams, CA and McKenna, ST and Tomar, S and Sharma, D and Prasad, AK and DePass, AL and Parmar, VS},
  issn         = {1871-5206},
  journal      = {ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY},
  keyword      = {TEA POLYPHENOLS,LUNG METASTASIS,PROSTATE-CANCER,HUMULUS-LUPULUS L.,CELLS IN-VITRO,UROKINASE-PLASMINOGEN-ACTIVATOR,CHICK HEART INVITRO,CARCINOMA CELLS,BREAST-CANCER,E-CADHERIN},
  language     = {eng},
  number       = {2},
  pages        = {171--185},
  publisher    = {BENTHAM SCIENCE PUBL LTD},
  title        = {Plant polyphenolics as anti-invasive cancer agents},
  volume       = {8},
  year         = {2008},
}

Chicago
Bracke, Marc, Barbara Vanhoecke, LARA DERYCKE, Selin Bolca, Sam Possemiers, Arne Heyerick, Chris Stevens, et al. 2008. “Plant Polyphenolics as Anti-invasive Cancer Agents.” Anti-cancer Agents in Medicinal Chemistry 8 (2): 171–185.
APA
Bracke, Marc, Vanhoecke, B., DERYCKE, L., Bolca, S., Possemiers, S., Heyerick, A., Stevens, C., et al. (2008). Plant polyphenolics as anti-invasive cancer agents. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 8(2), 171–185.
Vancouver
1.
Bracke M, Vanhoecke B, DERYCKE L, Bolca S, Possemiers S, Heyerick A, et al. Plant polyphenolics as anti-invasive cancer agents. ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY. SHARJAH: BENTHAM SCIENCE PUBL LTD; 2008;8(2):171–85.
MLA
Bracke, Marc, Barbara Vanhoecke, LARA DERYCKE, et al. “Plant Polyphenolics as Anti-invasive Cancer Agents.” ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY 8.2 (2008): 171–185. Print.