Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes.

Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes. Research Abstract Details 

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Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes. Abstract Text:

Feng Gao,Hui Chao,Jin-Quan Wang,Yi-Xian Yuan,Bin Sun,Yuan-Fang Wei,Bin Peng,Liang-Nian Ji,Feng Gao,Hui Chao,Jin-Quan Wang,Yi-Xian Yuan,Bin Sun,Yuan-Fang Wei,Bin Peng,Liang-Nian Ji,

Many antitumor drugs act as topoisomerase inhibitors, and the inhibitions are usually related to DNA binding. Here we designed and synthesized DNA-intercalating Ru(II) polypyridyl complexes Delta--[Ru(bpy)(2)(uip)](2+) and Lambda-[Ru(bpy)(2)(uip)](2+) (bpy is 2,2'-bipyridyl, uip is 2-(5-uracil)-1H-imidazo[4,5-f][1,10]phenanthroline). The DNA binding, photocleavage, topoisomerase inhibition, and cytotoxicity of the complexes were studied. As we expected, the synthesized Ru(II) complexes can intercalate into DNA base pairs and cleave the pBR322 DNA with high activity upon irradiation. The mechanism studies reveal that singlet oxygen ((1)O(2)) and superoxide anion radical (O (2) (*-) ) may play an important role in the photocleavage. The inhibition of topoisomerases I and II by the Ru(II) complexes has been studied. The results suggest that both complexes are efficient inhibitors towards topoisomerase II by interference with the DNA religation and direct topoisomerase II binding. Both complexes show antitumor activity towards HELA, hepG2, BEL-7402, and CNE-1 tumor cells.

Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes. Publishing Authors By Initials

F Gao,H Chao,JQ Wang,YX Yuan,B Sun,YF Wei,B Peng,LN Ji,F Gao,H Chao,JQ Wang,YX Yuan,B Sun,YF Wei,B Peng,LN Ji,

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Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes. Journal Published:

PUBLICATION TYPE: Research Support, Non-U.S. Gov

Journal: Journal of biological inorganic chemistry : JBIC :

VOLUME: 12

Page Numbers: 1015-27

Journal Abbreviation: J. Biol. Inorg. Chem.

ISSN: 0949-8257

DAY: 21

MONTH: 07

YEAR: 2007

Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes. Information

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LANGUAGE: eng

NlmUniqueID: 9616326

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Grant and Affiliation Information for Targeting topoisomerase II with the chiral DNA-intercalating ruthenium(II) polypyridyl complexes.

AFFILIATION: Key Laboratory of Bioinorganic and Synthetic Chemistry of Ministry of Education, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, People's Republic of China.

Country: Germany

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MEDLINETA: J Biol Inorg Chem

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