Radiolabeling of cidofovir with technetium-99m and biodistribution studies

Radiolabeling cidofovir with technetium-99m (99mTc-CDV) is an innovative procedure that enables real-time monitoring of the drug. Essays were performed in vitro, showing high radiolabel stability within 24 h. Blood clearance, biodistribution studies, and scintigraphic images were performed in healthy mice in order to evaluate the profile of the drug in vivo. 99mTc-CDV showed biphasic blood circulation time and significant kidney uptake, indicating that 99mTc-CDV is preferentially eliminated by the renal route. Bones also showed important uptake throughout the experiment. In summary, cidofovir was successfully labeled with technetium-99m and might be used in further studies to track the drug.

Diagnostic value of serum tumor makers for bone metastasis from lung cancer / 中华核医学与分子影像杂志

Objective To investigatethe significance of serum carbohydrate antigen (CA) 125,car cinoembryonic antigen (CEA),cytokeratin 19 fragment (CYFRA21-1),neuron-specific enolase (NSE),and squamous cell carcinoma antigen (SCCA) in the diagnosis of bone metastasis from lung cancer.Methods A total of 222 patients,including 91 lung cancer patients with bone metastasis (49 males,42 females,average age (60.07± 10.60) years;group A),75 lung cancerpatientswithout bone metastasis (57 males,18 females,average age (62.20± 12.63) years;group B),56 patients with benign lung diseases (34 males,22 females,average age (61.45± 10.66) years;group C) were recruited from January 2015 to January 2016.The electrochemiluminescence was applied to detect serum levels of CA125,CEA,CYFRA21-1,NSE and SCCA.Kruskal-Wallis,Wilcoxon rank sum test,x2 test and receiver operating characteristic (ROC) curve analysis were used to analyze data.Results The levels of serum CA125,CEA,CYFRA21-1,NSE in group A were higher than those in group B and C (H values:13.45-44.96,all P＜0.05);while SCCA was not significantly different among the 3 groups (H=2.56,P＞0.05).The areas under ROC curves for CA125,CEA,CYFRA21-1,NSE,SCCA were 0.667,0.702,0.602,0.664,0.440,respectively.The positive rate of serum NSE in small cell lung cancer (SCLC) patients was higher than that in non-small-cell lung cancer (NSCLC) patients (17/18 vs 32.88％ (24/73);x2=22.11,P＜0.05);CEA was highly expressed in adenocarcinoma,and SCCA was highly expressed in squamous cell carcinoma.Patients with grade Ⅲ+ Ⅳ metas tasis (n =52) had higher levels of CA 125,CEA,NSE compared to patients with Ⅰ + Ⅱ metastasis (n =39;z values:from-2.54 to-0.32,all P＜0.05).The sensitivity of combined detection of 5 tumor markers was 97.80％ (89/91),which was significantly higher than that of single tumor marker (x2 values:35.46-138.23,all P＜0.05).Conclusion Serum levels of CA125,CEA,CYFRA21-1,NSE and SCCA play a role in the diagnosis of bone metastasis from lung cancer,and the combined detection of the 5 tumor markers contribute to the early detection of bone metastases.

Optimization of SPECT/CT scan schemes in localizing preoperative parathyroid lesions / 中华核医学与分子影像杂志

Objective To compare the diagnostic efficiencies of different scanning schemes of dualphase 99Tcm-methoxyisobutylisonitrile (MIBI) planar imaging with or without SPECT/CT in the preoperative localization of parathyroid lesions.Methods Forty-two patients (20 males,22 females;average age (53.1 ± 14.8) years) with primary or secondary hyperparathyroidism who underwent parathyroidectomy from June 2011 to June 2016 were analyzed retrospectively.All patients underwent dual-phase 99Tcm-MIBI planar scan and dual-phase SPECT/CT scan.The images were collected according to the following 4 procedures:dualphase planar imaging (S1),dual-phase planar imaging+early-phase SPECT/CT (S2),dual-phase planar imaging+delayed-phase SPECT/CT (S3),dual-phase planar imaging+dual-phase SPECT/CT (S4).Pathological results were considered as the gold standard.A total of 168 parathyroid glands in 42 patients were evaluated by the 4 imaging procedures respectively.The diagnostic efficiencies were calculated and compared by x2 test.Results Seventy-eight abnormal parathyroid lesions were found.The diagnostic sensitivities of S1,S2,S3,S4 were 66.7％ (52/78),89.7％(70/78),69.2％(54/78),89.7％(70/78),and the accuracies were 78.6％ (132/168),94.0％ (158/168),85.1％ (143/168),94.0％ (158/168),respectively.The diagnostic accuracies of S2 and S4 were significantly higher than those of S1 and S3 (x2 values:17.027 and 7.176,both P＜0.01).Condusions The dual-phase planar imaging together with early-phase and dualphase SPECT/CT imaging have high diagnostic efficiencies in the preoperative localization of parathyroid lesions.Considering reducing radiation dose and examine time,the dual-phase planar imaging together with early-phase SPECT/CT is a better choice.

Clinical implications of DMSA Scan in Childhood Acute Pyelonephritis

PURPOSE: This study aimed to evaluate the relationships between 99mTecnicium-dimercaptosuccinic acid (DMSA) scan findings and clinical parameters including age and fever duration. METHODS: The positive rates for abnormal DMSA scans were analyzed according to the age of patients, fever duration prior to admission, and total fever duration. DMSA scan findings were divided into 3 categories: single defect, multifocal defects, and discrepant defects. We evaluated the detection rates of vesicoureteral reflux according to DMSA scan lesions. RESULTS: Among a total 320 cases, 141 (44.1%) had abnormal DMSA scans. The infant group (0-1 year of age) had a shorter total fever duration, and a lower C-reactive protein (CRP) value and DMSA positive rate (39.8% vs. 60.6%, P=0.002) compared to children group (2-15 years of age). Patients with abnormal scans had a longer total fever duration and higher CRP compared to those with normal scans. The positivity rate of abnormal scans did not differ between the patients with a short fever duration prior to admission of ≤2 days and those with longer fever duration of ≥3 days. However, patients with longer total fever duration had a higher rate of abnormal DMSA scans (P=0.02). Among cases with a single defect, multifocal defects, and discrepant defects, vesicoureteral reflux was observed in 22.4%, 60% and 70.6% of cases, respectively (P=0.004). CONCLUSION: Although DMSA scan has limitations in early diagnosis, DMSA scan findings may aid in the prediction of the severity of systemic inflammation and detection of vesicoureteral reflux.

Clinical implications of DMSA Scan in Childhood Acute Pyelonephritis

PURPOSE: This study aimed to evaluate the relationships between 99mTecnicium-dimercaptosuccinic acid (DMSA) scan findings and clinical parameters including age and fever duration. METHODS: The positive rates for abnormal DMSA scans were analyzed according to the age of patients, fever duration prior to admission, and total fever duration. DMSA scan findings were divided into 3 categories: single defect, multifocal defects, and discrepant defects. We evaluated the detection rates of vesicoureteral reflux according to DMSA scan lesions. RESULTS: Among a total 320 cases, 141 (44.1%) had abnormal DMSA scans. The infant group (0-1 year of age) had a shorter total fever duration, and a lower C-reactive protein (CRP) value and DMSA positive rate (39.8% vs. 60.6%, P=0.002) compared to children group (2-15 years of age). Patients with abnormal scans had a longer total fever duration and higher CRP compared to those with normal scans. The positivity rate of abnormal scans did not differ between the patients with a short fever duration prior to admission of ≤2 days and those with longer fever duration of ≥3 days. However, patients with longer total fever duration had a higher rate of abnormal DMSA scans (P=0.02). Among cases with a single defect, multifocal defects, and discrepant defects, vesicoureteral reflux was observed in 22.4%, 60% and 70.6% of cases, respectively (P=0.004). CONCLUSION: Although DMSA scan has limitations in early diagnosis, DMSA scan findings may aid in the prediction of the severity of systemic inflammation and detection of vesicoureteral reflux.

Functional investigation of bone implant viability using radiotracers in a new model of osteonecrosis

OBJECTIVES: Conventional imaging methods are excellent for the morphological characterization of the consequences of osteonecrosis; however, only specialized techniques have been considered useful for obtaining functional information. To explore the affinity of radiotracers for severely devascularized bone, a new mouse model of isolated femur implanted in a subcutaneous abdominal pocket was devised. To maintain animal mobility and longevity, the femur was harvested from syngeneic donors. Two technetium-99m-labeled tracers targeting angiogenesis and bone matrix were selected. METHODS: Medronic acid and a homodimer peptide conjugated with RGDfK were radiolabeled with technetium-99m, and biodistribution was evaluated in Swiss mice. The grafted and control femurs were evaluated after 15, 30 and 60 days, including computed tomography (CT) and histological analysis. RESULTS: Radiolabeling achieved high (>95%) radiochemical purity. The biodistribution confirmed good blood clearance 1 hour after administration. For 99mTc-hydrazinonicotinic acid (HYNIC)-E-[c(RGDfK)2, remarkable renal excretion was observed compared to 99mTc-methylene diphosphonate (MDP), but the latter, as expected, revealed higher bone uptake. The results obtained in the control femur were equal at all time points. In the implanted femur, 99mTc-HYNIC-E-[c(RGDfK)2 uptake was highest after 15 days, consistent with early angiogenesis. Regarding 99mTc-MDP in the implant, similar uptake was documented at all time points, consistent with sustained bone viability; however, the uptake was lower than that detected in the control femur, as confirmed by histology. CONCLUSIONS: 1) Graft viability was successfully diagnosed using radiotracers in severely ischemic bone at all time points. 2) Analogously, indirect information about angiogenesis could be gathered using 999mTc-HYNIC-E-[c(RGDfK)2. 3) These techniques appear promising and warrant further studies to determine their potential clinical applications.

Multiple endocrine neoplasia type 1 with anterior mediastinal parathyroid adenoma: successful localization using Tc-99m sestamibi SPECT/CT

The most common manifestation of multiple endocrine neoplasia type 1 (MEN1) is hyperparathyroidism. Treatment of hyperparathyroidism in MEN patients is surgical removal of the parathyroid glands, however ectopic parathyroid gland is challenging for treatment. A 51-year-old female, the eldest of 3 MEN1 sisters, had hyperparathyroidism with ectopic parathyroid adenoma in the mediastinal para-aortic region, which was detected by technetium-99m (Tc-99m) sestamibi scintigraphy and single-photon emission computed tomography/computed tomography (SPECT/CT). She underwent total parathyroidectomy with video-assisted thoracoscopic surgery on an anterior mediastinal mass. Anterior mediastinal parathyroid adenoma in MEN1 patients is rare. Precise localization of an ectopic parathyroid gland with Tc-99m sestamibi SPECT/CT can lead to successful treatment of hyperparathyroidism. This is the first reported case in the literature of mediastinal parathyroid adenoma in MEN1 patient visualized by Tc-99m sestamibi SPECT/CT.

Synthesis and antimicrobial evaluation of two peptide LyeTx I derivatives modified with the chelating agent HYNIC for radiolabeling with technetium-99m

Background Current diagnostic methods and imaging techniques are not able to differentiate septic and aseptic inflammation. Thus, reliable methods are sought to provide this distinction and scintigraphic imaging is an interesting option, since it is based on physiological changes. In this context, radiolabeled antimicrobial peptides have been investigated as they accumulate in infectious sites instead of aseptic inflammation. The peptide LyeTx I, from the venom of Lycosa erythrognatha, has potent antimicrobial activity. Therefore, this study aimed to synthesize LyeTx I derivatives with the chelating compound HYNIC, to evaluate their antimicrobial activity and to radiolabel them with 99mTc. Methods Two LyeTx I derivatives, HYNIC-LyeTx I (N-terminal modification) and LyeTx I-K-HYNIC (C-terminal modification), were synthesized by Fmoc strategy and purified by RP-HPLC. The purified products were assessed by RP-HPLC and MALDI-ToF-MS analysis. Microbiological assays were performed against S. aureus (ATCC® 6538) and E. coli (ATCC® 10536) in liquid medium to calculate the MIC. The radiolabeling procedure of LyeTx I-K-HYNIC with 99mTc was performed in the presence of co-ligands (tricine and EDDA) and reducing agent (SnCl2. 2H2O), and standardized taking into account the amount of peptide, reducing agent, pH and heating. Radiochemical purity analysis was performed by thin-layer chromatography on silica gel strips and the radiolabeled compound was assessed by RP-HPLC and radioactivity measurement of the collected fractions. Data were analyzed by ANOVA, followed by Tukey test (p-values < 0.05). Results Both LyeTx I derivatives were suitably synthesized and purified, as shown by RP-HPLC and MALDI-ToF-MS analysis. The microbiological test showed that HYNIC-LyeTx I (N-terminal modification) did not inhibit bacterial growth, whereas LyeTx I-K-HYNIC (C-terminal modification) showed a MIC of 5.05 μmol.L−1 (S. aureus) and 10.10 μmol.L−1 (E. coli). Thus, only the latter was radiolabeled with 99mTc. The radiochemical purity analysis of LyeTx I-K-HYNIC-99mTc showed that the optimal radiolabeling conditions (10 μg of LyeTx I-K-HYNIC; 250 μg of SnCl2. 2H2O; pH = 7; heating for 15 min) yielded a radiochemical purity of 87 ± 1 % (n= 3). However, RP-HPLC data suggested 99mTc transchelation from LyeTx I-K-HYNIC to the co-ligands (tricine and EDDA). Conclusions The binding of HYNIC to the N-terminal portion of LyeTx I seems to affect its activity against bacteria. Nevertheless, the radiolabeling of the C-terminal derivative, LyeTx I-K-HYNIC, must be better investigated to optimize the radiolabeled compound, in order to use it as a specific imaging agent to distinguish septic and aseptic inflammation.(AU)

Synthesis and antimicrobial evaluation of two peptide LyeTx I derivatives modified with the chelating agent HYNIC for radiolabeling with technetium-99m

Current diagnostic methods and imaging techniques are not able to differentiate septic and aseptic inflammation. Thus, reliable methods are sought to provide this distinction and scintigraphic imaging is an interesting option, since it is based on physiological changes. In this context, radiolabeled antimicrobial peptides have been investigated as they accumulate in infectious sites instead of aseptic inflammation. The peptide LyeTx I, from the venom of Lycosa erythrognatha, has potent antimicrobial activity. Therefore, this study aimed to synthesize LyeTx I derivatives with the chelating compound HYNIC, to evaluate their antimicrobial activity and to radiolabel them with 99mTc. Methods Two LyeTx I derivatives, HYNIC-LyeTx I (N-terminal modification) and LyeTx I-K-HYNIC (C-terminal modification), were synthesized by Fmoc strategy and purified by RP-HPLC. The purified products were assessed by RP-HPLC and MALDI-ToF-MS analysis. Microbiological assays were performed against S. aureus (ATCC® 6538) and E. coli (ATCC® 10536) in liquid medium to calculate the MIC. The radiolabeling procedure of LyeTx I-K-HYNIC with 99mTc was performed in the presence of co-ligands (tricine and EDDA) and reducing agent (SnCl2. 2H2O), and standardized taking into account the amount of peptide, reducing agent, pH and heating. Radiochemical purity analysis was performed by thin-layer chromatography on silica gel strips and the radiolabeled compound was assessed by RP-HPLC and radioactivity measurement of the collected fractions. Data were analyzed by ANOVA, followed by Tukey test (p-values 0.05). Results Both LyeTx I derivatives were suitably synthesized and purified, as shown by RP-HPLC and MALDI-ToF-MS analysis. The microbiological test showed that HYNIC-LyeTx I (N-terminal modification) did not inhibit bacterial growth, whereas LyeTx I-K-HYNIC (C-terminal modification) showed a MIC of 5.05 mol.L1 (S. aureus) and 10.10 mol.L1 (E. coli). Thus, only the latter was radiolabeled with 99mTc. The radiochemical purity analysis of LyeTx I-K-HYNIC-99mTc showed that the optimal radiolabeling conditions (10 g of LyeTx I-K-HYNIC; 250 g of SnCl2. 2H2O; pH = 7; heating for 15 min) yielded a radiochemical purity of 87 ± 1 % (n= 3). However, RP-HPLC data suggested 99mTc transchelation from LyeTx I-K-HYNIC to the co-ligands (tricine and EDDA). Conclusions The binding of HYNIC to the N-terminal portion of LyeTx I seems to affect its activity against bacteria. Nevertheless, the radiolabeling of the C-terminal derivative, LyeTx I-K-HYNIC, must be better investigated to optimize the radiolabeled compound, in order to use it as a specific imaging agent to distinguish septic and aseptic inflammation.

Alternative chromatographic system for the quality control of lipophilic technetium-99m radiopharmaceuticals such as [99mTc(MIBI)6]+

Knowledge of the radiochemical purity of radiopharmaceuticals is mandatory and can be evaluated by several methods and techniques. Planar chromatography is the technique normally employed in nuclear medicine since it is simple, rapid and usually of low cost. There is no standard system for the chromatographic technique, but price, separation efficiency and short time for execution must be considered. We have studied an alternative system using common chromatographic stationary phase and alcohol or alcohol:chloroform mixtures as the mobile phase, using the lipophilic radiopharmaceutical [99mTc(MIBI)6]+ as a model. Whatman 1 modified phase paper and absolute ethanol, Whatman 1 paper and methanol:chloroform (25:75), Whatman 3MM paper and ethanol:chloroform (25:75), and the more expensive ITLC-SG and 1-propanol:chloroform (10:90) were suitable systems for the direct determination of radiochemical purity of [99mTc(MIBI)6]+ since impurities such as99mTc-reduced-hydrolyzed (RH),99mTcO4- and [99mTc(cysteine)2]-complex were completely separated from the radiopharmaceutical, which moved toward the front of chromatographic systems while impurities were retained at the origin. The time required for analysis was 4 to 15 min, which is appropriate for nuclear medicine routines.

Efeito da fração não-oleosa doRicinus communisna biodistribuição comTecnécio-99m em camundongos / Effect of non-oily fraction ofRicinus communis on the bio distribution with Technetium-99m in mice

RESUMO Ricinus communisé uma planta pertence à família Euforbiaceae. A partir de seus frutos é extraído o óleo de rícino e outra fração altamente tóxica (fração não-oleosa). Neste estudo, foi avaliado o efeito da fração não oleosa de R. communis(FNORC) na biodistribuição do Tc-99m em camundongos sadios e em animais transplantados com Sarcoma-180 (S180). Para avaliação da biodistribuição do Tc-99m, o percentual de atividade radioativa total injetada (ATI%) foi mensurada utilizando um contador gama. Os resultados mostraram que, em animais sadios, houve aumento da captação do Tc-99m após o tratamento com FNORC pelos rins, cérebro e estômago. Apenas houve diminuição da absorção deste radioisótopo nos músculos. Em animais com tumor, houve redução significativa da captação do Tc-99m no coração, pulmões e tumor, e foi observado o aumento da captação apenas nos rins. Foi observada também a diminuição da concentração das proteínas plasmáticas totais em animais com tumor após tratamento com FNORC e atividade antitumoral significativa. Diante desses dados, conclui-se que fração não oleosa de R. communis possui atividade antitumoral significativa, porém altera a biodistribuição do Tc-99m, fato este que pode resultar em falhas nos processos de diagnóstico por imagem que utilizem este radioisótopo como marcador.

ABSTRACT Ricinus communis is a plant belonging to the Euforbiaceae family. From its fruits, it is extracted the castor oil and another highly toxic fraction (non-oily fraction). In this study, we evaluated the effect of the non-oily fraction of R. communis (NOFRC) on the bio distribution of Tc-99m in healthy mice and in animals transplanted with Sarcoma-180 (S180). To evaluate the bio distribution of theTc-99m, the percentage of the total injected radioactivity (% TIR) was measured through a gamma counter. There was an increase in the capitation of Tc-99m after the treatment with NOFRC in the kidneys, brain, and stomach of healthy animals. A decrease in the reception of this radionuclide was only found in the muscles. In animals with tumour, there was a significant reduction in the uptake of Tc-99m in the heart, lungs and tumour. An increase in the capitation was only observed in the kidneys. It was also observed a reduction in the total plasma protein concentration in animals with tumours after the treatment with NOFRC, besides significant antitumor activity. We concluded that there is antitumor activity in the NOFRC, but that it alters the biodistribution of Tc-99m, a fact which may result in failures in the diagnostic imaging process using this radioisotope as a marker.

The Value of SPECT/CT in Localizing Pain Site and Prediction of Treatment Response in Patients with Chronic Low Back Pain

In many circumstances, causing sites of low back pain (LBP) cannot be determined only by anatomical imaging. Combined functional and morphological imaging such as bone scan with single-photon emission computed tomography/computed tomography (SPECT/CT) may be helpful in identifying active lesions. The purpose of this study was to evaluate the usefulness of bone SPECT/CT in localizing the pain site and the treatment of chronic LBP. One hundred seventy-five patients suffering from chronic LBP who underwent SPECT/CT were included, retrospectively. All of the patients received multiple general treatments according to the symptoms, and some of them underwent additional target-specific treatment based on SPECT/CT. Numerical rating scale (NRS) pain score was used to assess the pain intensity. Of 175 patients, 127 showed good response to the given therapies, while the rest did not. Overall, 79.4% of patients with definite active lesions showed good response. Patients with mild active or no lesions on SPECT/CT had relatively lower response rate of 63.0%. Good response was observed by the treatment with the guidance of active lesions identified on SPECT/CT. SPECT/CT could be useful in identifying active lesions in patients with chronic LBP and guiding the clinicians to use adequate treatment.

Extramedullary Pulmonary Hematopoiesis Causing Pulmonary Hypertension and Severe Tricuspid Regurgitation Detected by Technetium-99m Sulfur Colloid Bone Marrow Scan and Single-Photon Emission Computed Tomography/CT

Extramedullary pulmonary hematopoiesis is a rare entity with a limited number of case reports in the available literature only. We report the case of a 66-year-old man with known primary myelofibrosis, in whom a Technetium-99m sulfur colloid bone marrow scan with single-photon emission computed tomography (SPECT)/CT revealed a pulmonary hematopoiesis as the cause of pulmonary hypertension and severe tricuspid regurgitation. To the best of our knowledge, this is the first description of Technetium-99m sulfur colloid SPECT/CT imaging in this rare condition.

Research on damage of salivary glands in patients with subacute thyroiditis by means of radionuclide imaging / 中华内分泌代谢杂志

The function of salivary glands in patients with subacute thyroiditis was evaluated.The data of patients with subacute thyroiditis,primary hypothyroidism,and normal controls undergoing radionuclide scanning were reviewed and compared retrospectively.The ratio of target to non-target values in the salivary glands were decreased in patients with subacute thyroiditis.Thyroid and salivary glands in patients with subacute thyroiditis might be damaged simultaneously and both developed pharyngeal symptoms partly due to the damaged salivary glands.

Studies Involving a Commercial Extract of Three Ballerina: ii- Evaluation of the in Vitro Effect on the Labeling of Blood Constituents of rats with Technetium-99m and on the Morphology of the Red Blood Cell.

The aim of this work is to characterize (electric conductivity and refractive index) a Three Ballerina (TB) and to evaluate its in vitro effect on the labeling of blood constituents with 99mTc and on the morphology of the red blood cells (RBC). Anticoagulated whole blood (Wistar rat) was incubated with a TB extract and the labeling of the blood constituents with technetium-99m (99mTc) was performed. Plasma (P) and blood cells (BC) were isolated and aliquots were also precipitated with trichloroacetic acid to separate soluble (SF) and insoluble fractions (IF). The %ATI in these samples was calculated. The morphology of the treated RBC showed no shape’s qualitative alterations. The TB extract was characterized with an electric conductivity of 1.35±0.04mSv/cm and refractive index of 2.21±0.15%BRIX. TB extract decreased significantly (p<0.05) the radioactivity distribution in the cellular compartment from 96.97±1.30% to 88.48±7.13%, and in IF-P from 74.29±4.12 to 14.26±5.73%. In conclusion, our data show some physical chemical parameters that could be suitable to characterize the preparation of an extract of TB. Moreover, substances present in the TB extract should probably have an effect on transport of the ions through the RBC membrane and/or should have redoxi properties and the stannous ion would decrease and could justify the effect on the fixation of the radioactivity on the plasma proteins. Moreover, although our experiments were carried out with animals, it is suggested precaution in the interpretation of the examinations that use labeled blood constituents in patients who are undergone TB extract.

Effect of rosemary (Rosmarinus officinalis) extract on the biodistribution of 99mTc sulphur colloid and on the radiolabeled blood constituents

With this study we evaluated the effects of the herb rosemary (Rosmarinus officinalis L. Lamiaceae) extract on the labeling of blood constituents with technetium-99m (99mTc) labeled sulphur colloid and on the biodistribution of 99mTc-Sulphur Colloid in Wistar albino rats. For this purpose, two groups of animals (male wistar rats, 130-140 g) were treated (1 mL) with a rosemary extract (750 mg/kg body wt.,n=9) and water (control, n=9) separately by gavage for five days. 99mTc-Sulphur Colloid was administrated by intravenous injection; organs/tissues were withdrawn and weighted. Blood was centrifuged, plasma and blood cells were isolated. The radioactivity was counted to calculate the percentage of activity per gram for each organ/tissue and percentage of activity in blood cells and plasma. A significant increase (p<0.05) in the uptake of 99mTc-Sulphur Colloid in the liver after the treatment with rosemary extract was observed. These results indicate that the substances or metabolites of the rosemary extract would change the biodistribution of99mTc-Sulphur Colloid.

Renal Manifestations and Imaging Studies of Kawasaki Disease

PURPOSE: The aim of this study was to verify renal inflammation following Kawasaki disease (KD) using single photon emission computed tomography along with Technetium-99m dimercaptosuccinic acid scintigraphy (DMSA renal SPECT). METHODS: From March 2011 to October 2011, 15 patients diagnosed with KD at the National Health Insurance System Ilsan Hospital were enrolled in the study. All patients underwent DMSA renal SPECT to evaluate renal involvement during the acute phase of KD. Urine beta2-microglobulin (beta2-MG), a marker of renal proximal tubular dysfunction, was also measured to assess renal damage. RESULTS: All 15 patients had normal renal function test results. However, microscopic hematuria and pyuria were observed in 13% and 33% of the patients, respectively. Moreover, urine beta2-MG was elevated in 46% of the patients. In addition, patients were divided into two groups based on beta2-MG level: those with an increased beta2-MG level, and those with a normal beta2-MG level. No significant differences were found between these two groups in clinical characteristics, laboratory, sonography, and echocardiography findings. All patients' DMSA renal SPECT scans were normal. CONCLUSION: Our study showed that mild abnormalities in the urinalysis and elevated urine beta2-MG were the only findings of renal involvement in KD. However, no aggressive renal manifestations were detected on DMSA renal SPECT.

Anti toxic effect of broccoli extract on stannous dichloride toxicity / Efeito antitóxico do extrato de brócolis na toxicidade do dicloreto de estanho

PURPOSE: Since Technetium-99m (99mTc) has favorable physical and chemical characteristics, it is widely used radioisotope in Nuclear Medicine. However, stannous dichloride (SnCl2) has been widely used as a reducing agent in labeling procedure of pharmaceutical with radionuclide, it has been realized that SnCl2 have genotoxic and cytotoxic effects on biological systems. In previous studies, it has been shown that some herbal extract can reduce genotoxic and cytotoxic effects of SnCl2. In the present study, it is aimed to evaluate the effect of the broccoli extract on the survival of E. coli ATCC 25922 strain against to toxic effects of SnCl2. METHODS: Broccoli was extracted with methanol extraction. HPLC and TLC analysis of broccoli extract were performed. Then antitoxicity and dose response assays were performed on bacterial strain. RESULTS: The broccoli extract had dose dependent protective effect against SnCl2 toxic effect on E. coli. CONCLUSIONS: The consumption of broccoli may alter the stannous dichloride toxicity. Broccoli extract may use as a new protective strategies against the toxic effect of SnCl2 on patients who were taken 99mTc radiopharmaceuticals.

OBJETIVO: Em face de suas características físico-químicas, o Tecnécio-99m (99mTc) é um radiofármaco amplamente utilizado na Medicina Nuclear. Todavia, o dicloreto de estanho (SnCl2) tem sido largamente aplicado como um agente redutor no procedimento farmacêutico de marcação com radionuclídeos. Constatou-se que o SnCl2 apresenta efeitos genotóxicos e citotóxicos nos sistemas biológicos. Em estudos prévios, foi demonstrado que alguns extratos de ervas podem reduzir tais efeitos. O estudo atual objetivou avaliar os efeitos do extrato de brócolis na sobrevida da cepa E. coli ATCC 25922, exposta ao efeito tóxico do SnCl2. MÉTODOS: O extrato de brócolis foi obtido mediante extração com metanol. Analises com HPLC e TLC foram efetuadas. Avaliou-se a antitoxicidade e realizou-se um ensaio dose-resposta para uma cepa de bactérias. RESULTADOS: O extrato de brócolis mostrou um efeito protetor dose dependente para os efeitos tóxicos do SnCl2 sobre a E. coli. CONCLUSÕES: O consumo de brócolis pode alterar a toxicidade do dicloreto de estanho. O extrato de brócolis pode ser utilizado como uma nova estratégia para proteção de pacientes contra os efeitos tóxicos do SnCl2, nos quais foi administrado o radiofármaco Tecnécio-99m.

Comparison of two peptide radiotracers for prostate carcinoma targeting

OBJECTIVES: Scintigraphy is generally not the first choice treatment for prostate cancer, although successful studies using bombesin analog radiopeptides have been performed. Recently, a novel peptide obtained using a phage display library demonstrated an affinity for prostate tumor cells. The aim of this study was to compare the use of a bombesin analog to that of a phage display library peptide (DUP-1) radiolabeled with technetium-99m for the treatment of prostate carcinoma. The peptides were first conjugated to S-acetyl-MAG3 with a 6-carbon spacer, namely aminohexanoic acid. METHODS: The technetium-99m labeling required a sodium tartrate buffer. Radiochemical evaluation was performed using ITLC and was confirmed by high-performance liquid chromatography. The coefficient partition was determined, and in vitro studies were performed using human prostate tumor cells. Biodistribution was evaluated in healthy animals at various time points and also in mice bearing tumors. RESULTS: The radiochemical purity of both radiotracers was greater than 95 percent. The DUP-1 tracer was more hydrophilic (log P = -2.41) than the bombesin tracer (log P = -0.39). The biodistribution evaluation confirmed this hydrophilicity by revealing the greater kidney uptake of DUP-1. The bombesin concentration in the pancreas was greater than that of DUP-1 due to specific gastrin-releasing peptide receptors. Bombesin internalization occurred for 78.32 percent of the total binding in tumor cells. The DUP-1 tracer showed very low binding to tumor cells during the in vitro evaluation, although tumor uptake for both tracers was similar. The tumors were primarily blocked by DUP1 and the bombesin radiotracer primarily targeted the pancreas. CONCLUSION: Further studies with the radiolabeled DUP-1 peptide are recommended. With further structural changes, this molecule could become an efficient alternative tracer for prostate tumor diagnosis.

Technetium-99m-labeled deoxynivalenol from Fusarium mycotoxin alters organ toxicity in BALB/c mice by oral and intravenous route

The toxicity of deoxynivalenol, both intravenously and orally, was investigated in male and female BALB/c mice. Technetium-99m (99m Tc)-labeled deoxynivalenol was administered to mice by tail vein injection and orally dosed. Distribution of labeled deoxynivalenol at 26 hours was monitored by gamma-scintigraphy. In the evaluated organs, the accumulation of radioactive deoxynivalenol was correlated with the amount of radioactivity. In addition, the toxicity of deoxynivalenol was measured by biochemical assays followed by histopathological findings. Kidney and hepatic marker enzymes were significantly increased in intravenously administered deoxynivalenol as compared to orally treated mice. Intravenously treated mice showed severe damage in liver and kidney when compared to those orally exposed. Biodistribution of 99mTc-labeled deoxynivalenol differed between oral and intravenous treatment. In intravenously exposed mice, deoxynivalenol was distributed primarily in the liver and kidney whereas in oral exposure, it was found in the stomach and intestines after 26 hours. Deoxynivalenol toxicity, associated with its biodistribution and organ toxicity, was greatest where it had accumulated. The results show that the toxicity of deoxynivalenol is associated with organ accumulation.(AU)