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Cytotoxic activity, cell imaging and photocleavage of DNA induced by a Pt(II) cyclophane bearing 1,2 diamino ethane as a terminal ligand

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Cytotoxic activity, cell imaging and photocleavage of DNA induced by a Pt(II) cyclophane bearing 1,2 diamino ethane as a terminal ligand. / Coogan, Michael.
In: MedChemComm, Vol. 2, No. 12, 2011, p. 1208-1216.

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@article{681ab92851dd4089ba3d8fc5ac61582c,
title = "Cytotoxic activity, cell imaging and photocleavage of DNA induced by a Pt(II) cyclophane bearing 1,2 diamino ethane as a terminal ligand",
abstract = "A PtII complex [{Pt(en)L}2]·4PF6 (Ptcyp) (LH2 = N,N′-bis(salicylidene)-p-phenylenediamine, en = 1,2-diamino ethane) shows high cytotoxicity against HeLa cells (IC50—11.5 μM) and against Dalton's lymphoma (DL) cells (IC50—0.65 nM); UV-vis titration of Ptcyp with calf thymus DNA (CT-DNA) demonstrated its DNA binding, which could be further quantified by competitive fluorescence titration of DNA, Ptcyp and ethidium bromide. Circular dichroism studies suggest that Ptcyp interacts with CT-DNA by intercalation in an aqueous medium containing a minimum amount of DMSO. Agarose gel electrophoresis showed that Ptcyp is able to convert a supercoiled pBR322 plasmid DNA into a nicked circular DNA in DMSO, but to a much lower extent in an aqueous medium. However, with UV irradiation, Ptcyp is able to cause concentration-dependent nicking of supercoiled DNA in an aqueous medium. These findings indicate the DNA binding and UV exposure-dependent DNA cleavage properties of Ptcyp. Cell imaging studies using the HeLa cell line carried out in the presence of Ptcyp represent one of the first examples of Pt complexes applied as fluorophores in cell imaging and strongly support its interaction with DNA.",
author = "Michael Coogan",
year = "2011",
doi = "10.1039/C1MD00159K",
language = "English",
volume = "2",
pages = "1208--1216",
journal = "MedChemComm",
issn = "2040-2511",
publisher = "Royal Society of Chemistry",
number = "12",

}

RIS

TY - JOUR

T1 - Cytotoxic activity, cell imaging and photocleavage of DNA induced by a Pt(II) cyclophane bearing 1,2 diamino ethane as a terminal ligand

AU - Coogan, Michael

PY - 2011

Y1 - 2011

N2 - A PtII complex [{Pt(en)L}2]·4PF6 (Ptcyp) (LH2 = N,N′-bis(salicylidene)-p-phenylenediamine, en = 1,2-diamino ethane) shows high cytotoxicity against HeLa cells (IC50—11.5 μM) and against Dalton's lymphoma (DL) cells (IC50—0.65 nM); UV-vis titration of Ptcyp with calf thymus DNA (CT-DNA) demonstrated its DNA binding, which could be further quantified by competitive fluorescence titration of DNA, Ptcyp and ethidium bromide. Circular dichroism studies suggest that Ptcyp interacts with CT-DNA by intercalation in an aqueous medium containing a minimum amount of DMSO. Agarose gel electrophoresis showed that Ptcyp is able to convert a supercoiled pBR322 plasmid DNA into a nicked circular DNA in DMSO, but to a much lower extent in an aqueous medium. However, with UV irradiation, Ptcyp is able to cause concentration-dependent nicking of supercoiled DNA in an aqueous medium. These findings indicate the DNA binding and UV exposure-dependent DNA cleavage properties of Ptcyp. Cell imaging studies using the HeLa cell line carried out in the presence of Ptcyp represent one of the first examples of Pt complexes applied as fluorophores in cell imaging and strongly support its interaction with DNA.

AB - A PtII complex [{Pt(en)L}2]·4PF6 (Ptcyp) (LH2 = N,N′-bis(salicylidene)-p-phenylenediamine, en = 1,2-diamino ethane) shows high cytotoxicity against HeLa cells (IC50—11.5 μM) and against Dalton's lymphoma (DL) cells (IC50—0.65 nM); UV-vis titration of Ptcyp with calf thymus DNA (CT-DNA) demonstrated its DNA binding, which could be further quantified by competitive fluorescence titration of DNA, Ptcyp and ethidium bromide. Circular dichroism studies suggest that Ptcyp interacts with CT-DNA by intercalation in an aqueous medium containing a minimum amount of DMSO. Agarose gel electrophoresis showed that Ptcyp is able to convert a supercoiled pBR322 plasmid DNA into a nicked circular DNA in DMSO, but to a much lower extent in an aqueous medium. However, with UV irradiation, Ptcyp is able to cause concentration-dependent nicking of supercoiled DNA in an aqueous medium. These findings indicate the DNA binding and UV exposure-dependent DNA cleavage properties of Ptcyp. Cell imaging studies using the HeLa cell line carried out in the presence of Ptcyp represent one of the first examples of Pt complexes applied as fluorophores in cell imaging and strongly support its interaction with DNA.

U2 - 10.1039/C1MD00159K

DO - 10.1039/C1MD00159K

M3 - Journal article

VL - 2

SP - 1208

EP - 1216

JO - MedChemComm

JF - MedChemComm

SN - 2040-2511

IS - 12

ER -