Synthesis and Bioevaluation of Novel Technetium-99m-Labeled Complexes with Norfloxacin HYNIC Derivatives for Bacterial Infection Imaging.

To seek a novel Tc-labeled quinolone derivative for bacterial infection SPECT imaging that aims to lower nontarget organ uptake, a novel norfloxacin 6-hydrazinoicotinamide (HYNIC) derivative (HYNICNF) was designed and synthesized. It was radiolabeled with different coligands, such as tricine, trisodium triphenylphosphine-3,3',3″-trisulfonate (TPPTS), sodium triphenylphosphine-3-monosulfonate (TPPMS), and ethylenediamine-,'-diacetic acid (EDDA), to obtain three Tc-labeled norfloxacin HYNIC complexes, namely, [Tc]Tc-tricine-TPPTS-HYNICNF, [Tc]Tc-tricine-TPPMS-HYNICNF, and [Tc]Tc-EDDA-HYNICNF. These complexes were purified (RCP > 95%) and evaluated and for targeting bacteria.

Radiolabeling and evaluation of a novel [TcN] complex with deferoxamine dithiocarbamate as a potential agent for bacterial infection imaging.

In order to find a Tc-labeled deferoxamine radiotracer for bacterial infection imaging, deferoxamine dithiocarbamate (DFODTC) was successfully synthesized and it was radiolabeled with [TcN] core to prepare the TcN(DFODTC) complex. TcN(DFODTC) was obtained with high radiochemical purity without further purification. The complex was lipophilic and exhibited good in vitro stability.

Synthesis and Evaluation of Novel Norfloxacin Isonitrile Tc Complexes as Potential Bacterial Infection Imaging Agents.

To develop potential technetium-99m single-photon emission computed tomography (SPECT) imaging agents for bacterial infection imaging, the novel norfloxacin isonitrile derivatives CN4NF and CN5NF were synthesized and radiolabeled with a [Tc][Tc(I)] core to obtain [Tc]Tc-CN4NF and [Tc]Tc-CN5NF. These compounds were produced in high radiolabeling yields and showed hydrophilicity and good stability in vitro. The bacterial binding assay indicated that [Tc]Tc-CN4NF and [Tc]Tc-CN5NF were specific to bacteria.

Preparation and Bioevaluation of Novel Tc-Labeled Complexes with a 2-Nitroimidazole HYNIC Derivative for Imaging Tumor Hypoxia.

To develop novel Tc-labeled single-photon emission computed tomography (SPECT) radiotracers for imaging hypoxia, a novel HYNICNM ligand (6-hydrazinonicotinamide (HYNIC) 2-nitroimidazole derivative) was designed and synthesized. It was radiolabeled with technetium-99m using tricine/trisodium triphenylphosphine-3,3',3''-trisulfonate (TPPTS), tricine/sodium triphenylphosphine-3-monosulfonate (TPPMS) and tricine as co-ligands to obtain [Tc]Tc-tricine-TPPTS-HYNICNM, [Tc]Tc-tricine-TPPMS-HYNICNM, and [Tc]Tc-(tricine)-HYNICNM, respectively. The three technetium-99m complexes were radiolabeled in one step with a high yield (95%) and had good stability in saline and mouse serum.

Tc-CN7DG: A Highly Expected SPECT Imaging Agent of Cancer with Satisfactory Tumor Uptake and Tumor-to-Nontarget Ratios.

A novel glucose derivative (CN7DG) possessing an isonitrile as a coordinating group was synthesized, and Tc-CN7DG, which was expected to be a powerful tumor imaging agent for SPECT, was prepared in a kit by the reaction of CN7DG with SnCl·2HO and TcO. Tc-CN7DG exhibited good stability and was transported via glucose transporters. Biodistribution results in mice bearing A549 tumor models showed that Tc-CN7DG had a higher uptake at the tumor sites and better tumor/blood and tumor/muscle ratios than did [F]FDG and Tc-CN5DG.

Design, Preparation, and Evaluation of a Novel TcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent.

In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [TcN] core to obtain the TcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that TcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that TcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation.

Synthesis and evaluation of [TcN] core and [TcO] core labeled complexes with 4-nitroimidazole xanthate derivative for tumor hypoxia imaging.

A 4-nitroimidazole xanthate ligand (NMXT) was synthesized and radiolabeled with [TcN] core and [TcO] core to obtain TcN-NMXT and TcO-NMXT, respectively. The two Tc-complexes were prepared with high radiochemical purity and had good stability. The partition coefficient results indicated both of them were hydrophilic, and cellular uptake studies showed they exhibited good hypoxic selectivity.

Novel Tc-labelled complexes with thymidine isocyanide: radiosynthesis and evaluation as potential tumor imaging tracers.

A novel thymidine isocyanide (CN-TdR) functionalized at the N3 position of thymidine was synthesized and then radiolabelled with Tc(i) and [Tc(i)(CO)] cores to produce [Tc(CN-TdR)] and [Tc(CO)(CN-TdR)], respectively. Both of them were prepared with high radiochemical purity and were stable over 6 h in saline at ambient temperature and in serum at 37 °C. The partition coefficient results demonstrated that they were hydrophilic.

[Research on the ultraviolet reflectivity characteristic of simulative targets of oil spill on the ocean].

The authors set up an experiment instrument to measure the ultraviolet (UV) characteristic of oil spill simulation targets for the marine oil spill. After selecting appropriate conditions for experiments, the authors tested UV reflective spectrum of four simulation targets for oil spill (gasoline, kerosene, diesel fuel, lubricating oil). The authors calculated the UV absolute spectrum reflectivity of all testing targets from the standard white board as reference, whose UV reflectivity was given.