A B C
Z. Naturforsch. 2012, 67b, 731 – 746
doi:10.5560/ZNB.2012-0107
Synthesis and Cytotoxic Activity of Methyl Glycyrrhetinate Esterified with Amino Acids
René Csuk, Stefan Schwarz, Bianka Siewert, Ralph Kluge, and Dieter Ströhl
Martin-Luther-Universität Halle-Wittenberg, Bereich Organische Chemie, Kurt-Mothes-Str. 2, D-06120 Halle (Saale), Germany
Reprint requests to Prof. Dr. René Csuk. Fax: 0049 345 5527030. E-mail: rene.csuk@chemie.uni-halle.de
Received April 19, 2012 / published online July 18, 2012
Methyl glycyrrhetinate was esterified at position C3 of ring A using different amino acids. A short, unbranched chain of four carbon atoms with two amino groups in positions 2 and 4 was shown to be the most active compound of this series (IC50 =0.8  µM on liposarcoma Lipo cells). These compounds trigger apoptosis as shown by an acridine orange/ethidium bromide assay, trypan blue tests and DNA-laddering experiments.
Key words: Glycyrrhetinic Acid, Antitumor Activity, Apoptosis
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