New anti-invasive compounds: Results from the Indo-Belgian screening program

Vanhoecke, Barbara W.; Depypere, Herman T.; De Beyter, Anicée; Sharma, Sunil K.; Parmar, Virinder S.; De Keukeleire, Denis; Bracke, Marc E.

doi:10.1351/pac200577010065

Pure Appl. Chem., 2005, Vol. 77, No. 1, pp. 65-74

http://dx.doi.org/10.1351/pac200577010065

New anti-invasive compounds: Results from the Indo-Belgian screening program

Barbara W. Vanhoecke¹, Herman T. Depypere¹, Anicée De Beyter², Sunil K. Sharma³, Virinder S. Parmar³, Denis De Keukeleire⁴ and Marc E. Bracke²

¹ Department of Gynaecological Oncology, University Hospital, University of Gent, Gent, Belgium
² Laboratory of Experimental Cancerology, University Hospital, University of Gent, Gent, Belgium
³ Bioorganic Laboratory, Department of Chemistry, University of Delhi, Delhi –110 007, India
⁴ Laboratory of Pharmacognosy and Phytochemistry, Faculty of Pharmaceutical Sciences, University of Gent, Gent, Belgium

Abstract: The development of anti-invasive and anti-metastatic drugs is a major challenge in current cancer research. A model to study invasion in vitro consisted of organotypic confronting cultures of human MCF-7/6 mammary cancer cells with embryonic chicken heart fragments. Untreated cultures show occupation and destruction of the normal heart fragments within eight days. Inhibition of invasion was observed after addition of the following alkaloids and (poly)phenolics to the culture medium: (+)-catechin, tangeretin, xanthohumol, 3,7‑dimethoxyflavone, prenylated chalcones, a pyrazole derivative, an isoxazolylcoumarin, and a prenylated desoxybenzoin. The action targets have been found both in the cancer cells and the surrounding host tissue. We hope that the further characterization of these targets will eventually lead to the development of clinically applicable anti-invasive drugs.