The interaction of calf thymus DNAwith [CuL(ClO4)]ClO4·H2O (1) and [ZnLBr]Br·H2O (2) (L = 9,12,15,18,27,28-hexaaza-29-oxatetracyclo[24.2.1.02,7.020,25]enneicosa-2,4,6,20,22,24,26,281-octaene) dicationic complexes in aqueous solution at neutral pH, was investigated by variable-temperature UV-vis absorption, circular dichroism and fluorescence spectroscopy. The values of the DNA-binding constants of these complexes, determined by competitive binding spectrofluorimetric titrations of ethidium bromide (EB)–DNA solutions, are (6.7 ± 0.5) × 106 M−1 for CuL2+ and (4.7 ± 0.5) × 105 M−1 for ZnL2+. These data together with a through analysis of the spectroscopic behaviour consistently suggest that both compounds are effective DNA binders. Interestingly, the DNA-binding strength of these complexes has been found to be correlated to their in vitro cytotoxic activity toward human breast carcinoma cells, although the complex with lower DNA-binding affinity is more active. In fact, biological studies showed that when the compounds are delivered through the cell membrane by a lipidic carrier, the cell survival is sensibly reduced, up to 58% with 1 and to 31% with 2.

Terenzi, A., Fanelli, M., Ambrosi, G., Amatori, S., Fusi, V., Giorgi, L., et al. (2012). DNA binding and antiproliferative activity toward human carcinoma cells of copper(II) and zinc(II) complexes of a 2,5-diphenyl[1,3,4]oxadiazole derivative. DALTON TRANSACTIONS, 41(41), 4389-4395 [10.1039/c2dt11759b].

DNA binding and antiproliferative activity toward human carcinoma cells of copper(II) and zinc(II) complexes of a 2,5-diphenyl[1,3,4]oxadiazole derivative

TERENZI, Alessio
Membro del Collaboration Group
;
TURCO LIVERI, Vincenzo
Membro del Collaboration Group
;
BARONE, Giampaolo
Membro del Collaboration Group
2012-01-01

Abstract

The interaction of calf thymus DNAwith [CuL(ClO4)]ClO4·H2O (1) and [ZnLBr]Br·H2O (2) (L = 9,12,15,18,27,28-hexaaza-29-oxatetracyclo[24.2.1.02,7.020,25]enneicosa-2,4,6,20,22,24,26,281-octaene) dicationic complexes in aqueous solution at neutral pH, was investigated by variable-temperature UV-vis absorption, circular dichroism and fluorescence spectroscopy. The values of the DNA-binding constants of these complexes, determined by competitive binding spectrofluorimetric titrations of ethidium bromide (EB)–DNA solutions, are (6.7 ± 0.5) × 106 M−1 for CuL2+ and (4.7 ± 0.5) × 105 M−1 for ZnL2+. These data together with a through analysis of the spectroscopic behaviour consistently suggest that both compounds are effective DNA binders. Interestingly, the DNA-binding strength of these complexes has been found to be correlated to their in vitro cytotoxic activity toward human breast carcinoma cells, although the complex with lower DNA-binding affinity is more active. In fact, biological studies showed that when the compounds are delivered through the cell membrane by a lipidic carrier, the cell survival is sensibly reduced, up to 58% with 1 and to 31% with 2.
2012
Settore CHIM/03 - Chimica Generale E Inorganica
Terenzi, A., Fanelli, M., Ambrosi, G., Amatori, S., Fusi, V., Giorgi, L., et al. (2012). DNA binding and antiproliferative activity toward human carcinoma cells of copper(II) and zinc(II) complexes of a 2,5-diphenyl[1,3,4]oxadiazole derivative. DALTON TRANSACTIONS, 41(41), 4389-4395 [10.1039/c2dt11759b].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10447/62737
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