4.1 Article

Facile synthesis of a polyether-tethered dimeric berberine as a highly effective DNA-cleaving agent in the presence of Cu(II)ion

Journal

MEDCHEMCOMM
Volume 4, Issue 10, Pages 1400-1404

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c3md00136a

Keywords

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Funding

  1. Program for New Century Excellent Talents in University [NCET-11-0920]
  2. National Natural Science Foundation of China [21102070]
  3. Department of Education of Guangdong Province [C1030388, 2012KJCX0024]
  4. Guangdong Provincial Department of Science and Technology of China [2012B050100007]
  5. Program for Pearl River New Stars of Science and Technology in Guangzhou [2011J2200071]

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A polyether-tethered dimeric berberine was synthesized and found to be capable of efficiently converting pBR322 DNA into open circular and linear forms in the presence of Cu(II) ions under physiological conditions, most probably via an oxidative mechanism. Michaelis-Menten analysis afforded ca. 3.5 x 10(9)-fold rate acceleration over uncatalyzed cleavage of supercoiled DNA. The probable mode of action is also briefly discussed.

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