New“all-in-one”theranostic systems,combining a magnetic resonance imaging(MRI)contrast agent with a biphotonic photodynamic therapy(2P-PDT)photosensitiser generating cytotoxic singlet oxygen,were envisaged and synth...New“all-in-one”theranostic systems,combining a magnetic resonance imaging(MRI)contrast agent with a biphotonic photodynamic therapy(2P-PDT)photosensitiser generating cytotoxic singlet oxygen,were envisaged and synthesised.They are based on azamacrocycles,regiospecifically functionalised by two-photon PDTπ-conjugated dibromobenzene-picolinate photosensitisers and acetate,able to complex gadolinium(III)and allow an MRI signal.Our approach was to use two different macrocyclic platforms,tacn and pyclen,for modulating simultaneously the structures,properties and solubility of the complexes.Photophysical properties of the ligands and their gadolinium(III)complexes were fully investigated.The Gd^(3+)-pyclen derivative showed the best water solubility and the greatest value of singlet oxygen generation of the series withΦ_(Δ)=0.53 enabling in vitro studies.The biological PDT activity under mono and biphotonic excitation was evaluated in human breast cancer cells(MCF-7).While a very low dark toxicity was observed,an almost total cell death was induced after only 3 successive irradiations of 1.57 s.Finally,its relaxivity was measured in a DMSO/H_(2)O solvent mixture with r_(1p)=11.21 and r_(2p)=24.60 mM^(-1)s^(-1)at 3.0 T and T_(1)-and T_(2)-weighted phantom MR images were obtained highlighting a first generation of“all-in-one”PDT/MRI theranostic agents.展开更多
The development of nuclear magnetic resonance (NMR) imaging as a clinical diagnostic modality has promoted the need for a new class of pharmaceuticals. These drugs would be administered to a patient to enhance the ima...The development of nuclear magnetic resonance (NMR) imaging as a clinical diagnostic modality has promoted the need for a new class of pharmaceuticals. These drugs would be administered to a patient to enhance the image contrast between the normal and diseased tissues. The image intensity in ~1HNMR imaging, composed of the NMR signals of water protons, is dependent on the nuclear relaxation times. Complexes of paramagnetic transition and lanthanide ions, which can decrease the relaxation times of nearby nuclei via dipolar interactions, have received much attention as the potential con-展开更多
In recent years, a great deal of interest has been focused on nitrogen-containing extractants for the separation of actinides from lanthanides. In this study, we synthesized a polyazamacrocycle-type C8-cyclen ligand c...In recent years, a great deal of interest has been focused on nitrogen-containing extractants for the separation of actinides from lanthanides. In this study, we synthesized a polyazamacrocycle-type C8-cyclen ligand comprising four tertiary alkyl amino groups, for the extraction of Am3+ and Eu3+. The C8-cyclen demonstrated a weak ability to extract and separate Am3+ and Eu3+ that increased with the increasing "softness" of the aqueous anions. The extraction behavior of Am3+ and Eu3+ indicated coordination interactions between the C8-cyclen and the Am3+ and Eu3+ ions. The suppression of Am3+ or Eu3+ extraction by acid depended on the media anions involved.展开更多
基金ANR(SADAM ANR-16-CE07-0015-02)Hungarian National Research,Development and Innovation Office(NKFIH K-128201 and 134694 projects)+1 种基金EU and co-financed by the European Regional Development Fund under the project GINOP-2.3.2-15-2016-00008French National Research Agency(ANR-10-INBS-04,«Investments for the future»)。
文摘New“all-in-one”theranostic systems,combining a magnetic resonance imaging(MRI)contrast agent with a biphotonic photodynamic therapy(2P-PDT)photosensitiser generating cytotoxic singlet oxygen,were envisaged and synthesised.They are based on azamacrocycles,regiospecifically functionalised by two-photon PDTπ-conjugated dibromobenzene-picolinate photosensitisers and acetate,able to complex gadolinium(III)and allow an MRI signal.Our approach was to use two different macrocyclic platforms,tacn and pyclen,for modulating simultaneously the structures,properties and solubility of the complexes.Photophysical properties of the ligands and their gadolinium(III)complexes were fully investigated.The Gd^(3+)-pyclen derivative showed the best water solubility and the greatest value of singlet oxygen generation of the series withΦ_(Δ)=0.53 enabling in vitro studies.The biological PDT activity under mono and biphotonic excitation was evaluated in human breast cancer cells(MCF-7).While a very low dark toxicity was observed,an almost total cell death was induced after only 3 successive irradiations of 1.57 s.Finally,its relaxivity was measured in a DMSO/H_(2)O solvent mixture with r_(1p)=11.21 and r_(2p)=24.60 mM^(-1)s^(-1)at 3.0 T and T_(1)-and T_(2)-weighted phantom MR images were obtained highlighting a first generation of“all-in-one”PDT/MRI theranostic agents.
基金Project supported by the National Natural Science Foundaion of China.
文摘The development of nuclear magnetic resonance (NMR) imaging as a clinical diagnostic modality has promoted the need for a new class of pharmaceuticals. These drugs would be administered to a patient to enhance the image contrast between the normal and diseased tissues. The image intensity in ~1HNMR imaging, composed of the NMR signals of water protons, is dependent on the nuclear relaxation times. Complexes of paramagnetic transition and lanthanide ions, which can decrease the relaxation times of nearby nuclei via dipolar interactions, have received much attention as the potential con-
基金supported by the National Natural Science Foundation of China(91226110)the Program for Changjiang Scholars and Innovative Research Team in University
文摘In recent years, a great deal of interest has been focused on nitrogen-containing extractants for the separation of actinides from lanthanides. In this study, we synthesized a polyazamacrocycle-type C8-cyclen ligand comprising four tertiary alkyl amino groups, for the extraction of Am3+ and Eu3+. The C8-cyclen demonstrated a weak ability to extract and separate Am3+ and Eu3+ that increased with the increasing "softness" of the aqueous anions. The extraction behavior of Am3+ and Eu3+ indicated coordination interactions between the C8-cyclen and the Am3+ and Eu3+ ions. The suppression of Am3+ or Eu3+ extraction by acid depended on the media anions involved.