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Published on: June 6, 2015
Plant polyphenolics as anti-invasive cancer agents
M E Bracke1, B W A Vanhoecke, L Derycke
1Laboratory of Experimental Cancer Research, Department of Radiotherapy, Nuclear Medicine and Experimental Cancer Research, Ghent University Hospital, Belgium.
Anti-Cancer Agents in Medicinal Chemistry
|February 22, 2008
Summary
Developing effective anti-invasive cancer agents is crucial. This study screened compounds using organotypic cultures, identifying diverse active molecules like plant alkaloids and polyphenolics for future drug design.
Area of Science:
- Oncology
- Pharmacology
- Drug Discovery
Background:
- Cancer invasion and metastasis are leading causes of mortality.
- Developing effective anti-invasive agents is a significant research challenge.
Purpose of the Study:
- To establish a screening program for identifying anti-invasive compounds.
- To explore structure-activity relationships and predict novel anti-invasive agents.
- To investigate the bioavailability and microbial metabolism of plant polyphenolics.
Main Methods:
- Organotypic confronting cultures of human cancer cells and normal tissue in 3D.
- Artificial neural network analysis of quantitative structural descriptors for structure-activity relationships.
- Simulator of the Human Intestinal Microbial Ecosystem (SHIME) and human trials for polyphenol metabolism.
Main Results:
- Identified diverse anti-invasive compounds, including plant alkaloids, polyphenolics (e.g., (+)-catechin, xanthohumol), and synthetic derivatives.
- Established a system for predicting and designing efficient anti-invasive molecules.
- Initiated studies on the gastrointestinal bioavailability of plant polyphenolics.
Conclusions:
- The developed screening system effectively identifies diverse anti-invasive compounds.
- Computational and metabolic studies are advancing the design of novel anti-cancer agents.
- The research aims to predict, synthesize, and apply molecules with optimal anti-metastatic activity in vivo.
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