Cytotoxic copper(II) complex of tripyridoquinoxaline with DNA hydrolase activity

A monomeric copper(II) complex, [Cu(tpq)2(H2O)2](ClO4)2, (tpq = tripyridoquinoxaline), has been synthesized and characterized spectroscopically. This complex has been found to bind DNA intercalatively and the DNA binding constant, Kb, for this complex has been determined from absorption measurements and was found to be (5.7 ± 0.3) × 103 M−1. This complex successfully promotes hydrolytic cleavage of plasmid DNA, producing single and double DNA strand breaks in the absence of any added cofactor. The amount of conversion of the supercoiled form of plasmid to the nicked circular form depends on the concentration of the copper complex as well as the duration of the incubation of the complex with DNA. The rate of conversion of SC to NC has been determined to be 2.65 × 10−4 s−1 at pH 7.2 in the presence of 80 μM of the complex. This complex has also been shown to be cytotoxic towards A549 lung adenocarcinoma cells. This complex has been shown to bring about apoptosis of the cancerous A549 cell line.

The monomeric copper(II) complex [Cu(tpq)2(H2O)2](ClO4)2 has been found to promote hydrolytic cleavage of DNA and bring about apoptosis in cancerous cell lines.Figure optionsDownload as PowerPoint slideHighlights
► A monomeric Cu(II) intercalator brings about hydrolytic cleavage of DNA.
► This complex has been found to be cytotoxic to cancerous cell line.
► The observed cytotoxicity could be due to its ability to bring about apoptotic cell death.
► This compound may have potential application in chemotherapy.