Synthesis of Tetrahydrohonokiol Derivates and Their Evaluation for Cytotoxic Activity against CCRF-CEM Leukemia, U251 Glioblastoma and HCT-116 Colon Cancer Cells
Marketa Bernaskova,
Nadine Kretschmer,
Wolfgang Schuehly,
Antje Huefner,
Robert Weis,
Rudolf Bauer
Affiliations
Marketa Bernaskova
Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Universitätsplatz 1, University of Graz, 8010 Graz, Austria
Nadine Kretschmer
Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Universitätsplatz 4, University of Graz, 8010 Graz, Austria
Wolfgang Schuehly
Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Universitätsplatz 4, University of Graz, 8010 Graz, Austria
Antje Huefner
Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Universitätsplatz 1, University of Graz, 8010 Graz, Austria
Robert Weis
Department of Pharmaceutical Chemistry, Institute of Pharmaceutical Sciences, Universitätsplatz 1, University of Graz, 8010 Graz, Austria
Rudolf Bauer
Department of Pharmacognosy, Institute of Pharmaceutical Sciences, Universitätsplatz 4, University of Graz, 8010 Graz, Austria
Biphenyl neolignans such as honokiol and magnolol, which are the major active constituents of the Asian medicinal plant Magnolia officinalis, are known to exert a multitude of pharmacological and biological activities. Among these, cytotoxic and tumor growth inhibitory activity against various tumour cell lines are well-documented. To further elucidate the cytotoxic effects of honokiol derivatives, derivatizations were performed using tetrahydrohonokiol as a scaffold. The derivatizations comprised the introduction of functional groups, e.g., nitro and amino groups, as well as alkylation. This way, 18 derivatives, of which 13 were previously undescribed compounds, were evaluated against CCRF-CEM leukemia cells, U251 glioblastoma and HCT-116 colon cancer cells. The results revealed no significant cytotoxic effects in any of the three tested cell lines at a test concentration of 10 µM.
