Next Article in Journal
Characterization of Rice NADPH Oxidase Genes and Their Expression under Various Environmental Conditions
Previous Article in Journal
Senescence Marker Protein-30 (SMP30) Deficiency Impairs Myocardium-Induced Dilation of Coronary Arterioles Associated with Reactive Oxygen Species
Int. J. Mol. Sci. 2013, 14(5), 9424-9439; doi:10.3390/ijms14059424
Article

Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents

1,†
, 1,†
, 2
, 1,* , 3
 and 1,*
Received: 31 January 2013; in revised form: 12 April 2013 / Accepted: 15 April 2013 / Published: 29 April 2013
(This article belongs to the Section Biochemistry, Molecular Biology and Biophysics)
View Full-Text   |   Download PDF [1434 KB, uploaded 19 June 2014]   |   Browse Figures
Abstract: Several rhein-phosphonate derivatives (5ac) 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 µM), 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.
Keywords: rhein; phosphonate; synthesis; cytotoxicity; apoptosis; DNA binding rhein; phosphonate; synthesis; cytotoxicity; apoptosis; DNA binding
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


MDPI and ACS Style

Ye, M.-Y.; Yao, G.-Y.; Wei, J.-C.; Pan, Y.-M.; Liao, Z.-X.; Wang, H.-S. Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents. Int. J. Mol. Sci. 2013, 14, 9424-9439.

AMA Style

Ye M-Y, Yao G-Y, Wei J-C, Pan Y-M, Liao Z-X, Wang H-S. Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents. International Journal of Molecular Sciences. 2013; 14(5):9424-9439.

Chicago/Turabian Style

Ye, Man-Yi; Yao, Gui-Yang; Wei, Jing-Chen; Pan, Ying-Ming; Liao, Zhi-Xin; Wang, Heng-Shan. 2013. "Synthesis, Cytotoxicity, DNA Binding and Apoptosis of Rhein-Phosphonate Derivatives as Antitumor Agents." Int. J. Mol. Sci. 14, no. 5: 9424-9439.


Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert