scholarly journals Preparation and Evaluation of Novel Folate Isonitrile 99mTc Complexes as Potential Tumor Imaging Agents to Target Folate Receptors

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4552
Author(s):  
Junhong Feng ◽  
Xuran Zhang ◽  
Qing Ruan ◽  
Yuhao Jiang ◽  
Junbo Zhang
Keyword(s):  
Radiochemical Purity ◽  
Tumor Imaging ◽  
Folate Receptor ◽  
Imaging Agents ◽  
Folate Receptors ◽  
Biodistribution Studies ◽  
Specific Tumor ◽  
Folate Receptor Targeting ◽  
Preparation And Evaluation

In order to seek novel technetium-99m folate receptor-targeting agents, two folate derivatives (CN5FA and CNPFA) were synthesized and radiolabeled to obtain [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA complexes, which exhibited high radiochemical purity (>95%) without purification, hydrophilicity, and good stability in vitro. The KB cell competitive binding experiments indicated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specificity to folate receptor. Biodistribution studies in KB tumor-bearing mice illustrated that [99mTc]Tc-CN5FA and [99mTc]Tc-CNPFA had specific tumor uptake. Compared with [99mTc]Tc-CN5FA, the tumor/muscle ratios of [99mTc]Tc-CNPFA were higher, resulting in a better SPECT/CT imaging background. According to the results, the two 99mTc complexes have potential as tumor imaging agents to target folate receptors.

scholarly journals Design, Preparation, and Evaluation of a Novel 99mTcN Complex of Ciprofloxacin Xanthate as a Potential Bacterial Infection Imaging Agent

Molecules ◽  
2020 ◽  
Vol 25 (24) ◽  
pp. 5837
Author(s):  
Si’an Fang ◽  
Yuhao Jiang ◽  
Qianqian Gan ◽  
Qing Ruan ◽  
Di Xiao ◽  
...  
Keyword(s):  
Bacterial Infection ◽  
Radiochemical Purity ◽  
Binding Assay ◽  
Sterile Inflammation ◽  
Good Stability ◽  
Imaging Agent ◽  
Imaging Agents ◽  
Infection Imaging ◽  
Preparation And Evaluation

In order to seek novel technetium-99m bacterial infection imaging agents, a ciprofloxacin xanthate (CPF2XT) was synthesized and radiolabeled with [99mTcN]2+ core to obtain the 99mTcN-CPF2XT complex, which exhibited high radiochemical purity, hydrophilicity, and good stability in vitro. The bacteria binding assay indicated that 99mTcN-CPF2XT had specificity to bacteria. A study of biodistribution in mice showed that 99mTcN-CPF2XT had a higher uptake in bacterial infection tissues than in turpentine-induced abscesses, indicating that it could distinguish bacterial infection from sterile inflammation. Compared to 99mTcN-CPFXDTC, the abscess/blood and abscess/muscle ratios of 99mTcN-CPF2XT were higher and the uptakes of 99mTcN-CPF2XT in the liver and lung were obviously decreased. The results suggested that 99mTcN-CPF2XT would be a potential bacterial infection imaging agent.

scholarly journals New 55Co-labeled Albumin-Binding Folate Derivatives as Potential PET Agents for Folate Receptor Imaging

2019 ◽  
Vol 12 (4) ◽  
pp. 166 ◽  
Author(s):  
Lauren L. Radford ◽  
Solana Fernandez ◽  
Rebecca Beacham ◽  
Retta El Sayed ◽  
Renata Farkas ◽  
...  
Keyword(s):  
Folate Receptor ◽  
Small Animal ◽  
Small Animal Pet ◽  
Receptor Imaging ◽  
Albumin Binding ◽  
Liver Uptake ◽  
Biodistribution Studies ◽  
Positron Emission

Overexpression of folate receptors (FRs) on different tumor types (e.g., ovarian, lung) make FRs attractive in vivo targets for directed diagnostic/therapeutic agents. Currently, no diagnostic agent suitable for positron emission tomography (PET) has been adopted for clinical FR imaging. In this work, two 55Co-labeled albumin-binding folate derivatives-[55Co]Co-cm10 and [55Co]Co-rf42-with characteristics suitable for PET imaging have been developed and evaluated. High radiochemical yields (≥95%) and in vitro stabilities (≥93%) were achieved for both compounds, and cell assays demonstrated FR-mediated uptake. Both 55Co-labeled folate conjugates demonstrated high tumor uptake of 17% injected activity per gram of tissue (IA/g) at 4 h in biodistribution studies performed in KB tumor-bearing mice. Renal uptake was similar to other albumin-binding folate derivatives, and liver uptake was lower than that of previously reported [64Cu]Cu-rf42. Small animal PET/CT images confirmed the biodistribution results and showed the clear delineation of FR-expressing tumors.

scholarly journals Tumor imaging using P866, a high-relaxivity gadolinium chelate designed for folate receptor targeting

2008 ◽  
Vol 60 (6) ◽  
pp. 1337-1346 ◽  
Author(s):  
Claire Corot ◽  
Philippe Robert ◽  
Eric Lancelot ◽  
Philippe Prigent ◽  
Sébastien Ballet ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Folate Receptor ◽  
Receptor Targeting ◽  
Gadolinium Chelate ◽  
High Relaxivity ◽  
Folate Receptor Targeting

scholarly journals Synthesis and Biological Evaluation of O-[3-18F-fluoropropyl]-α-methyl Tyrosine in Mesothelioma-Bearing Rodents

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
I-Hong Shih ◽  
Fan-Lin Kong ◽  
Mohammad S. Ali ◽  
Yinhan Zhang ◽  
Dong-Fang Yu ◽  
...  
Keyword(s):  
Radiochemical Purity ◽  
Biological Evaluation ◽  
Synthesis Methods ◽  
Automated Synthesis ◽  
Imaging Studies ◽  
Biodistribution Studies ◽  
Synthesis And Biological Evaluation ◽  
Automated Methods

Radiolabeled tyrosine analogs enter cancer cells via upregulated amino acid transporter system and have been shown to be superior to18F-fluoro-2-deoxy-D-glucose (18F-FDG) in differential diagnosis in cancers. In this study, we synthesized O-[3-19F-fluoropropyl]-α-methyl tyrosine (19F-FPAMT) and used manual and automated methods to synthesize O-[3-18F-fluoropropyl]-α-methyl tyrosine (18F-FPAMT) in three steps: nucleophilic substitution, deprotection of butoxycarbonyl, and deesterification. Manual and automated synthesis methods produced18F-FPAMT with a radiochemical purity >96%. The decay-corrected yield of18F-FPAMT by manual synthesis was 34% at end-of-synthesis (88 min). The decay-corrected yield of18F-FPAMT by automated synthesis was 15% at end-of-synthesis (110 min).18F-FDG and18F-FPAMT were used forin vitroandin vivostudies to evaluate the feasibility of18F-FPAMT for imaging rat mesothelioma (IL-45).In vitrostudies comparing18F-FPAMT with18F-FDG revealed that18F-FDG had higher uptake than that of18F-FPAMT, and the uptake ratio of18F-FPAMT reached the plateau after being incubated for 60 min. Biodistribution studies revealed that the accumulation of18F-FPAMT in the heart, lungs, thyroid, spleen, and brain was significantly lower than that of18F-FDG. There was poor bone uptake in18F-FPAMT for up to 3 hrs suggesting itsin vivostability. The imaging studies showed good visualization of tumors with18F-FPAMT. Together, these results suggest that18F-FPAMT can be successfully synthesized and has great potential in mesothelioma imaging.

scholarly journals Active Targeted Nanoformulations via Folate Receptors: State of the Art and Future Perspectives

Pharmaceutics ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 14
Author(s):  
Cristina Martín-Sabroso ◽  
Ana Isabel Torres-Suárez ◽  
Mario Alonso-González ◽  
Ana Fernández-Carballido ◽  
Ana Isabel Fraguas-Sánchez
Keyword(s):  
Inflammatory Diseases ◽  
Folate Receptor ◽  
Pharmacological Treatments ◽  
Potential Therapeutic Target ◽  
Folate Receptors ◽  
Normal Tissues ◽  
Pathological Conditions ◽  
Selective Delivery ◽  
Folate Receptor Targeting ◽  
Therapeutic Tools

In normal tissues, the expression of folate receptors is low and limited to cells that are important for embryonic development or for folate reabsorption. However, in several pathological conditions some cells, such as cancer cells and activated macrophages, overexpress folate receptors (FRs). This overexpression makes them a potential therapeutic target in the treatment of cancer and inflammatory diseases to obtain a selective delivery of drugs at altered cells level, and thus to improve the therapeutic efficacy and decrease the systemic toxicity of the pharmacological treatments. Two strategies have been used to achieve this folate receptor targeting: (i) the use of ligands with high affinity to FRs (e.g., folic acid or anti-FRs monoclonal antibodies) linked to the therapeutic agents or (ii) the use of nanocarriers whose surface is decorated with these ligands and in which the drug is encapsulated. This manuscript analyzes the use of FRs as a target to develop new therapeutic tools in the treatment of cancer and inflammatory diseases with an emphasis on the nanoformulations that have been developed for both therapeutic and imaging purposes.

Preparation and Preliminary Evaluation of 68 Ga-Acridine: An Attempt to Study the Potential of Radiolabeled DNA Intercalator as a PET Radiotracer for Tumor Imaging

2020 ◽  
Vol 20 (13) ◽  
pp. 1538-1547 ◽  
Author(s):  
Subhajit Ghosh ◽  
Tapas Das ◽  
Shishu K. Suman ◽  
Haladhar D. Sarma ◽  
Ashutosh Dash
Keyword(s):  
Radiochemical Purity ◽  
Tumor Imaging ◽  
Raji Cell ◽  
Biological Behavior ◽  
Preliminary Evaluation ◽  
Dna Intercalator ◽  
Tumor Accumulation ◽  
The Stability

Introduction: Acridine is a well-known DNA intercalator and thereby gets easily inserted within DNA. As uncontrolled rapid cell division is one of the primary characteristics of the tumors, it is expected that acridine or its suitable derivatives will have preferential accumulation in the tumorous lesions. Therefore, an attempt was made to radiolabel an acridine derivative with 68Ga and study the potential of the 68Ga-acridine complex as a PET agent for tumor imaging. Methods: 9-aminoacridine was coupled with p-NCS-benzyl-DOTA to render it suitable for labeling with 68Ga. The purified acridine-DOTA conjugate was radiolabeled with 68Ga, eluted from a 68Ge/68Ga radionuclide generator. Various radiolabeling parameters were optimized and the stability of the radiolabeled preparation was studied. The biological behavior of the 68Ga-acridine complex was studied both in vitro and in vivo using Raji cell line and fibrosarcoma tumor bearing Swiss mice, respectively. Results: 68Ga-acridine complex was obtained with ~100% radiochemical purity under the optimized reaction conditions involving incubation of 2mg/mL of ligand at 100°C for 30 minutes. The complex maintained a radiochemical purity of >95% in normal saline and >65% in human blood serum at 3h post-incubation. In vitro cellular study showed (3.2±0.1)% uptake of the radiotracer in the Raji cells. Biodistribution study revealed significant tumor accumulation [(11.41±0.41)% injected activity in per gram] of the radiotracer within 1h postadministration along with uptake in other non-target organs such as, blood, liver, GIT kidney etc. Conclusion: The present study indicates the potential of 68Ga-acridine as a PET agent for imaging of tumorous lesions. However, further detailed evaluation of the agent is warranted to explore its actual potential.

Sign in / Sign up

Export Citation Format

Share Document