Journal
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Volume 14, Issue 5, Pages 9424-9439Publisher
MDPI
DOI: 10.3390/ijms14059424
Keywords
rhein; phosphonate; synthesis; cytotoxicity; apoptosis; DNA binding
Funding
- 973 Project [2011CB512005, 2012CB723501]
- National Natural Science Foundation of China [81260472, 21101035]
- Guangxi Natural Science Foundation of China [2011GXNSFD018010, 2010GXNSFF013001]
- Bagui Scholar project
- Foundation of Ministry of Education Innovation Team [IRT1225]
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Several rhein-phosphonate derivatives (5a-c) were synthesized and evaluated for in vitro cytotoxicity against HepG-2, CNE, Spca-2, Hela and Hct-116 cell lines. Some compounds showed relatively high cytotoxicity. Especially compounds 5b exhibited the strongest cytotoxicity against HepG-2 and Spca-2 cells (IC50 was 8.82 and 9.01 mu M), respectively. All the synthesized compounds exhibited low cytotoxicity against HUVEC cells. Further experiments proved that 5b could disturb the cell cycle in HepG-2 cells and induce apoptosis. In addition, the binding properties of a model conjugate 5b to DNA were investigated by methods (UV-Vis, fluorescence, CD spectroscopy). Results indicated that 5b showed moderate ability to interact ct-DNA.
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