99mTc-labeled-1-thio-β-d-glucose as a new tool to temporomandibular joint inflammatory disorders diagnosis

Brasileiro, Cláudia Borges; Pacheco, Cinthia Mara da Fonseca; Queiroz-Junior, Celso Martins; Lima, Carla Flávia de; Silva, Juliana Batista da; Campos, Tânia Maria Mendonça

doi:10.1016/j.apradiso.2010.06.002

Cited by 5 publications

(6 citation statements)

References 41 publications

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“…Although the uptake of various 99m Tc‐labelled glucose derivatives in tumour have been reported earlier, their comparison is very difficult because of the heterogeneity of the type of tumours used. However, analysis of previously reported data showed that tumour uptake in most of them is low, in the same order of 99m Tc‐labelled glucose derivative 5 , specially at longer retention times and even those that have higher tumour uptake have low tumour/blood ratio.…”

Section: Resultsmentioning

confidence: 93%

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Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Fernández

Crócamo

Incerti

et al. 2012

Labelled Comp Radiopharmac

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Development of a 99mTc-labelled glucose derivative as a single-photon emission computed tomography analogue to [ 18 F]-2-fluoro-2-deoxy-D-glucose (FDG) is considered of great interest. Herein, we present the synthesis and preliminary bioevaluation of a 99m Tc(CO) 3 -glucose derivative. Derivatization of glucose at C2 was achieved using the so-called 'click chemistry', forming a histidine-like, 1,4-disubstituted triazole adequate as donor atom system for Tc(I)-tricarbonyl complexes. Synthesis of the intermediate azide derivative was achieved by conventional organic chemistry. Because of the efficiency and selectivity of this cycloaddition, labelling was performed in 'one pot', adding the tricarbonyl precursor fac-[ 99m Tc(CO) 3 (H 2 O) 3 ] + to the same vial where the click reaction has taken place without any further purification. A single product with radiochemical purity higher than 90% was obtained. It was stable for at least 4 h in reaction milieu and exhibited high hidrophilicity (log P of À1.2) and low binding to plasma proteins (5 AE 1%). Biodistribution in C57BL/6 mice bearing induced Lewis murine lung carcinoma is characterized by low blood and liver uptake and rapid urinary excretion. 99m Tc complex showed moderate tumour uptake but significant retention until 2 h post-injection. Soft tissue clearance was fast leading to significantly higher uptake in tumour in comparison to muscle (p = 0.05) at all time points. Overall, biodistribution of our compound was very similar to that of [ 18 F]-FDG. However, tumour uptake was significantly higher for [ 18 F]-FDG, probably because of high hidrophilicity of our derivative that may hinder cell penetration. Similarity to biodistribution of FDG is a promising outcome, and modifications of the chelator and linker might improve biological results.

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Section: Resultsmentioning

confidence: 93%

“…Although several groups have reported the preparation of 99m Tc‐labelled glucose and glucosamine analogues, to our knowledge, none of them has yet the expected properties, and further research in this area is still necessary …”

Section: Introductionmentioning

confidence: 99%

Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Fernández

Crócamo

Incerti

et al. 2012

Labelled Comp Radiopharmac

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“…The tumor uptake of 99m Tc-1-TG was clearly visualized by scintigraphic imaging, showing potential as a new type of radiopharmaceutical for melanoma imaging. In addition, 99m Tc-1-TG has been successfully used for inflammation imaging [32].…”

Section: Preclinical Development Of Glucose-based Radiopharmaceutimentioning

confidence: 99%

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG

Han

Wang

Chen

et al. 2019

Contrast Media & Molecular Imaging

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Glucose homeostasis plays a key role in numerous fundamental aspects of life, and its dysregulation is associated with many important diseases such as cancer. The atypical glucose metabolic phenomenon, known as the Warburg effect, has been recognized as a hallmark of cancer and serves as a promising target for tumor specific imaging. At present, 2-deoxy-2-[18F]fluoro-glucose (18F-FDG)-based positron emission tomography/computed tomography (PET/CT) represented the state-of-the-art radionuclide imaging technique for this purpose. The powerful impact of 18F-FDG has prompted intensive research efforts into other glucose-based radiopharmaceuticals for positron emission tomography (PET) and single-photon emission computed tomography (SPECT) imaging. Currently, glucose and its analogues have been labeled with various radionuclides such as 99mTc, 111In, 18F, 68Ga, and 64Cu and have been successfully investigated for tumor metabolic imaging in many preclinical studies. Moreover, 99mTc-ECDG has advanced into its early clinical trials and brings a new era of tumor imaging beyond 18F-FDG. In this review, preclinical and early clinical development of glucose-based radiopharmaceuticals for tumor metabolic imaging will be summarized.

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“…63 Obviously, there is the inherent risk of contamination, during manipulation of PBMC cells and isolation and labeling of leukocytes. 63 A recent patent PI0904754-9, developed by the research group coordinated by the author, has shown that Tc-99m-labeled thio-sugar analogues of glucose are efficient in detecting inflammations. 64 Previous synthesis studies had been successfully performed using 5-thio-Dglucose; however, due to cost issues, there was a need to replace the thio-sugar molecule.…”

Section: Synthesis Of Tracers For In Vivo Monitoringmentioning

confidence: 99%

“…65 The importance of thio-sugars in inflammations was demonstrated in the temporomandibular joint (TMJ) of rats. 63 The patent involves 5-thio-glucose and 1-beta-thio-D-glucose labeled with Tc-99m. 64 The results show significant differences in the uptake of 99m Tc-1-TG in the inflamed TM joint compared to the control, with high renal excretion.…”

Section: Synthesis Of Tracers For In Vivo Monitoringmentioning

confidence: 99%

The role of regulatory T cells, interleukin-10 and in vivo scintigraphy in autoimmune and idiopathic diseases – Therapeutic perspectives and prognosis

Falcão

Campos

2017

Rev. Assoc. Med. Bras.

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Previous studies have demonstrated the expression of the CD25 marker on the surface of naturally occurring T cells (T regs ) of mice, which have a self-reactive cellular profile. Recently, expression of other markers that aid in the identification of these cells has been detected in lymphocyte subtypes of individuals suffering of autoimmune and idiopathic diseases, including: CD25, CTLA-4 (cytotoxic T-lymphocyte antigen 4), HLA-DR (human leukocyte antigen) and Interleukin 10 (IL-10), opening new perspectives for a better understanding of an association between such receptors present on the cell surface and the prognosis of autoimmune diseases. The role of these molecules has already been described in the literature for the modulation of the inflammatory response in infectious and parasitic diseases. Thus, the function, phenotype and frequency of expression of the α-chain receptor of IL-2 (CD25) and IL-10 in lymphocyte subtypes were investigated. Murine models have been used to demonstrate a possible correlation between the expression of the CD25 marker (on the surface of CD4 lymphocytes) and the control of self-tolerance mechanisms. These studies provided support for the presentation of a review of the role of cells expressing IL-2, IL-10, HLA-DR and CTLA-4 receptors in the monitoring of immunosuppression in diseases classified as autoimmune, providing perspectives for understanding peripheral regulation mechanisms and the pathophysiology of these diseases in humans. In addition, a therapeutic approach based on the manipulation of the phenotype of these cells and ways of scintigraphically monitoring the manifestations of these diseases by labeling their receptors is discussed as a perspective. In this paper, we have included the description of experiments in ex vivo regulation of IL-10 and synthesis of thio-sugars and poly-sugars to produce radiopharmaceuticals for monitoring inflammation. These experiments may yield benefits for the treatment and prognosis of autoimmune diseases.

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99mTc-labeled-1-thio-β-d-glucose as a new tool to temporomandibular joint inflammatory disorders diagnosis

Cited by 5 publications

References 41 publications

Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG

The role of regulatory T cells, interleukin-10 and in vivo scintigraphy in autoimmune and idiopathic diseases – Therapeutic perspectives and prognosis

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99mTc-labeled-1-thio-β-d-glucose as a new tool to temporomandibular joint inflammatory disorders diagnosis

Cited by 5 publications

References 41 publications

Preparation and preliminary bioevaluation of a 99mTc(CO)3‐glucose derivative prepared by a click chemistry route

Preparation and preliminary bioevaluation of a 99mTc(CO)3‐glucose derivative prepared by a click chemistry route

Nuclear Imaging of Glucose Metabolism: Beyond 18F-FDG

The role of regulatory T cells, interleukin-10 and in vivo scintigraphy in autoimmune and idiopathic diseases – Therapeutic perspectives and prognosis

Contact Info

Product

Resources

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Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Preparation and preliminary bioevaluation of a ^99mTc(CO)₃‐glucose derivative prepared by a click chemistry route

Nuclear Imaging of Glucose Metabolism: Beyond ¹⁸F-FDG