Contrast agents for magnetic resonance angiographic applications: 1H and 17O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin

Silvio Aime; Monica Chiaussa; Giuseppe Digilio; Eliana Gianolio; Enzo Terreno

doi:10.1007/s007750050349

Contrast agents for magnetic resonance angiographic applications: ¹H and ¹⁷O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin

Silvio Aime, Monica Chiaussa, Giuseppe Digilio, Eliana Gianolio, Enzo Terreno

Research output: Contribution to journal › Article › peer-review

Abstract

The relaxometric properties of two Gd(III) DTPA-like complexes (DTPA = diethylenetriamine-N,N',N,N'_-pentaacetic acid) bearing different substituents for binding to human serum albumin (HSA) are compared. In spite of the structural differences of the recognition synthon and of the residual electric charge, the two chelates display an analogous binding affinity for the serum protein. Upon formation of the adducts with HSA, the exchange rates of the coordinated water appear slowed down by an amount corresponding to ca. 50% of the rates found for the free complexes. The relaxivity of [Gd(BOM)₃DTPA (H₂O)]^2- is significantly higher than that of MS-325 either in the free complex or in the macromolecular adduct. Finally, the effect of pH on the stability of the HSA adducts and on the values of their relaxivities has been investigated.

Original language	English
Pages (from-to)	766-774
Number of pages	9
Journal	Journal of Biological Inorganic Chemistry
Volume	4
Issue number	6
DOIs	https://doi.org/10.1007/s007750050349
Publication status	Published - Dec 1999
Externally published	Yes

Keywords

Contrast agents
Gadolinium(III) complexes
Human serum albumin
Magnetic resonance imaging
Proton relaxation enhancement

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10.1007/s007750050349

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Aime, S., Chiaussa, M., Digilio, G., Gianolio, E., & Terreno, E. (1999). Contrast agents for magnetic resonance angiographic applications: ¹H and ¹⁷O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin. Journal of Biological Inorganic Chemistry, 4(6), 766-774. https://doi.org/10.1007/s007750050349

@article{137f1cec60394402b75a637343f17a8a,

title = "Contrast agents for magnetic resonance angiographic applications: 1H and 17O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin",

abstract = "The relaxometric properties of two Gd(III) DTPA-like complexes (DTPA = diethylenetriamine-N,N',N,N'-pentaacetic acid) bearing different substituents for binding to human serum albumin (HSA) are compared. In spite of the structural differences of the recognition synthon and of the residual electric charge, the two chelates display an analogous binding affinity for the serum protein. Upon formation of the adducts with HSA, the exchange rates of the coordinated water appear slowed down by an amount corresponding to ca. 50% of the rates found for the free complexes. The relaxivity of [Gd(BOM)3DTPA (H2O)]2- is significantly higher than that of MS-325 either in the free complex or in the macromolecular adduct. Finally, the effect of pH on the stability of the HSA adducts and on the values of their relaxivities has been investigated.",

keywords = "Contrast agents, Gadolinium(III) complexes, Human serum albumin, Magnetic resonance imaging, Proton relaxation enhancement",

author = "Silvio Aime and Monica Chiaussa and Giuseppe Digilio and Eliana Gianolio and Enzo Terreno",

note = "Funding Information: Fig. 8 Plot of the relaxivity values (r1b) for Gd(III) complexes/ HSA adducts versus temperature at pH 5.5 and pH 8.5: A MS-325; B [Gd(BOM)3DTPA(H2O)]2–. The profiles of the HSA-bound complexes were calculated from solutions containing 0.1 mM of the complex and a large excess (1.7 mM) of HSA Acknowledgements We thank Dr. Pierfrancesco Morosini and Mr. Andrea Beltrami (Bracco S.p.a., Milan, Italy) for the syntheses of the samples of MS-325 and [Gd(BOM)3DTPA (H2O)]2– which were used in this study. We gratefully acknowledge the stimulating discussions with Drs. P.L. Anelli, L. Calabi, and F. Uggeri. Financial support from Bracco S.p.a., MURST, and CNR (Biotechnology Program L 95/95) is also gratefully acknowledged.",

year = "1999",

month = dec,

doi = "10.1007/s007750050349",

language = "English",

volume = "4",

pages = "766--774",

journal = "Journal of Biological Inorganic Chemistry",

issn = "0949-8257",

publisher = "Springer Verlag",

number = "6",

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Aime, S, Chiaussa, M, Digilio, G, Gianolio, E & Terreno, E 1999, 'Contrast agents for magnetic resonance angiographic applications: ¹H and ¹⁷O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin', Journal of Biological Inorganic Chemistry, vol. 4, no. 6, pp. 766-774. https://doi.org/10.1007/s007750050349

Contrast agents for magnetic resonance angiographic applications: ¹H and ¹⁷O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin. / Aime, Silvio; Chiaussa, Monica; Digilio, Giuseppe et al.
In: Journal of Biological Inorganic Chemistry, Vol. 4, No. 6, 12.1999, p. 766-774.

Research output: Contribution to journal › Article › peer-review

TY - JOUR

T1 - Contrast agents for magnetic resonance angiographic applications

T2 - 1H and 17O NMR relaxometric investigations on two gadolinium(III) DTPA-like chelates endowed with high binding affinity to human serum albumin

AU - Aime, Silvio

AU - Chiaussa, Monica

AU - Digilio, Giuseppe

AU - Gianolio, Eliana

AU - Terreno, Enzo

N1 - Funding Information: Fig. 8 Plot of the relaxivity values (r1b) for Gd(III) complexes/ HSA adducts versus temperature at pH 5.5 and pH 8.5: A MS-325; B [Gd(BOM)3DTPA(H2O)]2–. The profiles of the HSA-bound complexes were calculated from solutions containing 0.1 mM of the complex and a large excess (1.7 mM) of HSA Acknowledgements We thank Dr. Pierfrancesco Morosini and Mr. Andrea Beltrami (Bracco S.p.a., Milan, Italy) for the syntheses of the samples of MS-325 and [Gd(BOM)3DTPA (H2O)]2– which were used in this study. We gratefully acknowledge the stimulating discussions with Drs. P.L. Anelli, L. Calabi, and F. Uggeri. Financial support from Bracco S.p.a., MURST, and CNR (Biotechnology Program L 95/95) is also gratefully acknowledged.

PY - 1999/12

Y1 - 1999/12

N2 - The relaxometric properties of two Gd(III) DTPA-like complexes (DTPA = diethylenetriamine-N,N',N,N'-pentaacetic acid) bearing different substituents for binding to human serum albumin (HSA) are compared. In spite of the structural differences of the recognition synthon and of the residual electric charge, the two chelates display an analogous binding affinity for the serum protein. Upon formation of the adducts with HSA, the exchange rates of the coordinated water appear slowed down by an amount corresponding to ca. 50% of the rates found for the free complexes. The relaxivity of [Gd(BOM)3DTPA (H2O)]2- is significantly higher than that of MS-325 either in the free complex or in the macromolecular adduct. Finally, the effect of pH on the stability of the HSA adducts and on the values of their relaxivities has been investigated.

AB - The relaxometric properties of two Gd(III) DTPA-like complexes (DTPA = diethylenetriamine-N,N',N,N'-pentaacetic acid) bearing different substituents for binding to human serum albumin (HSA) are compared. In spite of the structural differences of the recognition synthon and of the residual electric charge, the two chelates display an analogous binding affinity for the serum protein. Upon formation of the adducts with HSA, the exchange rates of the coordinated water appear slowed down by an amount corresponding to ca. 50% of the rates found for the free complexes. The relaxivity of [Gd(BOM)3DTPA (H2O)]2- is significantly higher than that of MS-325 either in the free complex or in the macromolecular adduct. Finally, the effect of pH on the stability of the HSA adducts and on the values of their relaxivities has been investigated.

KW - Contrast agents

KW - Gadolinium(III) complexes

KW - Human serum albumin

KW - Magnetic resonance imaging

KW - Proton relaxation enhancement

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U2 - 10.1007/s007750050349

DO - 10.1007/s007750050349

M3 - Article

SN - 0949-8257

VL - 4

SP - 766

EP - 774

JO - Journal of Biological Inorganic Chemistry

JF - Journal of Biological Inorganic Chemistry

IS - 6

ER -