Synthesis of radioiodinated carnosine for hepatotoxicity imaging induced by carbon tetrachloride and its biological assessment in rats

2020 ◽  
Vol 108 (5) ◽  
pp. 397-408 ◽  
Author(s):  
Safaa B. Challan ◽  
Fawzy A. Marzook ◽  
Ayman Massoud

AbstractThe imaging of organs is very important in the field of diagnosis especially in case of liver diseases. In the present work, carnosine was successfully labeled with iodine-131 at room temperature in acidic medium using chloramine-T (Ch-T) as moderate oxidizing agent. The parameters affecting labeling of carnosine such as amount of oxidizing agent, amount of substrate, pH value of the reaction mixture, reaction temperature and reaction time, were investigated. The best conditions for formation of 131I-carnosine (131I-CAR) complex were 40 μg of chloramine-T (Ch-T), 75 μg of carnosine, pH 4 and 45 min reaction time at room temperature. The radiochemical yield for 131I-CAR complex was (91 ± 0.11) % at optimum conditions and the labeled complex was stable for 2 h after labeling process. Biodistribution study was achieved using three groups of rats (normal, treated by inactive carnosine and hepatotoxicity rats induced by CCl4). Hepatotoxicity of liver was evaluated using different biochemical markers such as ALT, AST and ALK.P. The 131I-CAR complex showed selective bio-localization in stomach and liver and its selectivity increases in acquired hepatotoxicity. The biological distribution indicates that the suitability of 131I-CAR as a potential hepatotoxicity imaging to detect hepatitis and medical prognosis.

2019 ◽  
Vol 19 (4) ◽  
pp. 841
Author(s):  
Maula Eka Sriyani ◽  
Dian Ayu Utami ◽  
Mega Susilo Dwike ◽  
Eva Maria Widyasari ◽  
Muharram Marzuki ◽  
...  

Quercetin is one of the flavonoid groups with antioxidant activity. The objective of this study was to achieve the labeled compound of 131I-quercetin as a radiotracer for diagnosis and cancer therapy with high labeling efficiency and radiochemical purity. The labeling procedure was conducted by the oxidation reaction using chloramine-T. The effect of pH, reaction time, amount of oxidizing agent and ligand were evaluated in this research. Quercetin was successfully labeled with iodine-131 at pH 11 at room temperature for 10 min mixed in 1000 rpm with the amount of quercetin and chloramine-T is 0.4 and 0.3 mg, respectively. The results demonstrated that the ratio of quercetin/Na131I was 2 × 105. The 131I-quercetin labeling efficiency was 92.03 ± 2.20%, and radiochemical purity of 131I-quercetin was 99.34 ± 0.58%. The results showed that 131I-quercetin could be a radiotracer candidate for diagnosis and cancer therapy.


2019 ◽  
Vol 12 (1) ◽  
pp. 25
Author(s):  
Ana R. Durante ◽  
Danielle V. Sobral ◽  
Ana C. Miranda ◽  
Érika V. de Almeida ◽  
Leonardo L. Fuscaldi ◽  
...  

Parkinson’s disease (PD) is a neurodegenerative disease characterized by the loss of dopaminergic neurons in the substantia nigra pars compacta, leading to alteration of the integrity of dopaminergic transporters (DATs). In recent years, some radiopharmaceuticals have been used in the clinic to evaluate the integrity of DATs. These include tropane derivatives such as radiolabeled β-CIT and FP-CIT with iodine-123 (123I), and TRODAT-1 with metastable technetium-99 (99mTc). Radiolabeling of β-CIT with radioactive iodine is based on electrophilic radioiodination using oxidizing agents, such as Chloramine T or Iodo-Gen®. For the first time, the present work performed a comparative study of the radiolabeling of β-CIT with iodine-131 (131I), using either Chloramine T or Iodo-Gen® as oxidizing agents, in order to improve the radiolabeling process of β-CIT and to choose the most advantageous oxidizing agent to be used in nuclear medicine. Both radiolabeling methods were similar and resulted in high radiochemical yield (> 95%), with suitable 131I-β-CIT stability up to 72 h. Although Chloramine T is a strong oxidizing agent, it was as effective as Iodo-Gen® for β-CIT radiolabeling with 131I, with the advantage of briefer reaction time and solubility in aqueous medium.


2018 ◽  
Vol 106 (9) ◽  
pp. 751-757 ◽  
Author(s):  
M. H. Sanad ◽  
H. M. Talaat ◽  
I. T. Ibrahim ◽  
G. M. Saleh ◽  
L. A. Abouzeid

Abstract The present study was oriented to synthesis radioiodinated celiprolol (Cel) for a potential cardiac imaging. Celiprolol has been labeled using 125I with chloramine-T (Ch-T) as an oxidizing agent. The key effective factors such as amount of oxidizing agent, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to optimize the iodination. The biological distribution indicates the suitability of radioiodinated Cel as a novel tracer to image heart.


2012 ◽  
Vol 476-478 ◽  
pp. 1926-1929
Author(s):  
Xiao Cai Yu ◽  
Dong Dong Hu ◽  
Qian Du ◽  
Xv Zheng ◽  
Ji Yao Guo

Nanoscale titanium dioxide (TiO2) has been fabricated through a sound sol-gel method at room temperature with Tetra-n-butyl Titanate as the precursor, and the particles are characterized by XRD and TEM techniques. The results manifest that the as-prepared TiO2 is amorphous with the anatase structure and its size is around 33.2nm. Five factors, including dosage of TiO2, initial concentration of diesel, pH value, photocatalytic degradation reaction time and the presence of H2O2, are considered in the diesel degradation experiments. An orthogonal test is carried out to optimize the photocatalytic degradation of diesel pollutants based on the single-factor experiments. It reveals that when the dosage of TiO2 is 1.0g/L, the initial concentration of diesel is 0.5g/L, pH value is 6, the reaction time is 4h and the H2O2 dosage is 0.09%, the removal rate of diesel pollutants can up to 88%. Besides, the influence of each factor on removing diesel can be arranged in decreasing order: initial concentration of diesel> photocatalytic reaction time> pH value> TiO2 dosage> H2O2 dosage.


2011 ◽  
Vol 331 ◽  
pp. 368-371 ◽  
Author(s):  
Li Ping Wang ◽  
Yu Chuan Guo ◽  
Yi Zhong Chen ◽  
Er Deng Du ◽  
Yong Jing Mao

It is difficult to treat printing and dyeing wastewater, for printing and dying wastewater features complex composition, high chromaticity and many toxic substances.The paper studied the effect of the compound of inorganic and organic coagulant with Fenton reagent on the treatment of printing and dyeing wastewater. The effect of other factors were also investigated, including pH value, flocculants, Fenton reagent and reaction time. The results showed that, under the conditions of room temperature, pH 9, PAFCS dosage 100mg/L, PAMC 4mg/L, pH 4, H2O2 dosage 1.0mL/L, FeSO4•7H2O dosage 150 mg/L, the reaction time 60 min, the CODCr removal was high over 91%, and the color was also significantly removed.


2005 ◽  
Vol 48 (spe2) ◽  
pp. 69-72 ◽  
Author(s):  
Akinkunmi Ganiyu Akanji ◽  
Emiko Muramoto ◽  
José de Souza Caldeira Filho ◽  
Renata Martinussi Couto ◽  
Elaine Bortoletti de Araújo

Radioactive isotopes of iodine, mainly iodine-131 have been broadly used in many monoclonal antibody radioiodination settings, employing different methods. In this study, using a Chloramine-T procedure, the influence of incubation time, CT mass, and Ab/activity ratio on the radiochemical yield of the anti-CD20 antibody labeled with iodine-131 was observed. Radiochemical yield was > 97 %, employing different Chloramine-T masses, independently of incubation time. Radiochemical purity was above 99 % after purification of the labeled compound. The relationship between Ab mass and radioactivity was tested and no difference was observed when 90.6 MBq (2.45mCi) of activity was incorporated in the Ab-mass range studied. Biodistribution study in normal Swiss mice showed higher uptake by the liver and intestines. Low thyroid uptake indicated a suitable in vivo stability. Slight blood uptake was considered a result of circulating radioactivity in normal organs and tissues. A favorable biological distribution of 131I-anti-CD20 suggests this radiopharmaceutical may be effectively used in the therapy of Non Hodgkin Lymphoma.


2018 ◽  
Vol 106 (10) ◽  
pp. 843-850 ◽  
Author(s):  
H. M. Sanad ◽  
Alhussein A. Ibrahim

Abstract The present work has been oriented to prepare radioiodinated olmesartan for a potential cardiac imaging. Olmesartan has been labeled using 125I or 131I with N-bromosuccinimide (NBS) as an oxidizing agent. Many factors like amount of N-bromosuccinimide, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to optimize high yield of [125I]iodoolmesartan. The biological distribution indicates the suitability of [125I]iodoolmesartan as a novel tracer to image heart.


2018 ◽  
Vol 106 (4) ◽  
pp. 329-336 ◽  
Author(s):  
M. H. Sanad ◽  
Ebtisam. A. Marzook ◽  
Safaa B. Challan

AbstractThe present study is oriented to synthesis of radioiodinated olmesartan medoxomil (OM) for potential cardiac imaging. Olmesartan medoxomil has been labeled with [125/131I] using chloramine-T (Ch-T) as an oxidizing agent. The key effective factors such as amount of oxidizing agent, amount of substrate, pH, reaction temperature and reaction time, have been systematically studied to get high radiochemical yield of the [125I]olmesartan medoxomil reaching values of 98.5%. The labeled compound was separated and purified using thin layer chromatography (TLC), paper electrophoresis and high performance liquid chromatography (HPLC). The biological distribution indicates the suitability of [125I]olmesartan medoxomil as a novel tracer to image heart with high heart/blood ratio within 30 min which was detected by gamma camera.


2005 ◽  
Vol 48 (spe2) ◽  
pp. 79-83
Author(s):  
Maria Tereza Colturato ◽  
Emiko Muramoto ◽  
Elaine Bortoleti de Araújo

Various tumor cells express significantly higher amounts of VIP receptors (VIPR) that provided the basis for the clinical use of radiolabeled VIP for the in vivo localization of tumors. This work studied the labeling of VIP and VIP10-28 with iodine-131 to compare the biological distribution of the labeled compounds in Nuce mice and the affinity for tumor cells. Both VIP and VIP10-28 peptides contain two tyrosine residues, in positions 10 and 22, that are theoretically equally susceptible to radioiodination employing oxidative electrophilic substitution using oxidizing agents like Chloramine T. Radiochemical purity of the reaction mixture was determined by electrophoresis and HPLC. The VIP peptide and the fragment were labeled with radioiodine with good radiochemical yield (above 96%). Suitable, but important differences can be observed in biological distribution studies. Comparatively, blood clearance was faster for labeled VIP and perhaps because of this, the uptake in tumor was lower, especially during the first hour. These differences observed in the biological distribution of the compounds can be related to the lipophilicity of the labeled compounds.


2012 ◽  
Vol 610-613 ◽  
pp. 2401-2404
Author(s):  
Yu Ping Tian ◽  
Shen Pan Chen

The simulated dye wastewater of direct fast scarlet was disposed of by the coagulant of FeSO4. The effects of reaction time, the original pH value, coagulant dosages and temperature were discussed. The results showed that, at room temperature, the original pH was 7.9, the FeSO4 dosage was 1.2 g / L, then after stirring for 15mins, the coagulation effect was the most obvious, and the removal rate of chroma achieved 95.3%.


Sign in / Sign up

Export Citation Format

Share Document