共查询到20条相似文献,搜索用时 38 毫秒
1.
C. S. R. Gooden D. E. Snook Agamemnon A. Epenetos 《Cell biochemistry and biophysics》1993,22(1-3):49-59
It is essential in any method for radiolabeling antibody with99mTc that the labeling procedure is rapid and reliable, producing a highly stable99mTc-antibody complex with minimal effect on the immunoreactivity of the antibody. In the present study, analysis of the stability and homogeneity of radiolabeled (99mTc and125I) antibodies (HMFG1 and PR1A3) was carried out by fast protein liquid chromatography (FPLC) using superose-6 and S-200 columns, and by polyacrylamide gel electrophoresis (PAGE) followed by autoradiography. Superose 6 and S-200 gel filtration analysis showed the radiolabel (99mTc or125I) eluting with a retention time identical to that of native antibody. No peaks of relative molecular size (Mr) corresponding to possible antibody fragments were seen in either the UV or the radioactive FPLC elution profiles. PAGE analysis of99mTc labeled antibody, however, revealed the presence of a number of radiolabeled antibody fragments (Mr<IgG) that were not detected by the same analysis of125I labeled antibody. The stability of the radiolabeled antibodies in serum in vitro was also studied. FPLC (superose-6) analysis after 45 h incubation in normal serum in vitro revealed 3.3% (HMFG1), and 20% (PR1A3) of the99mTc on a molecule or aggregate with a Mr greater than that of IgG. There is also the appearance of small amounts of99mTc-labeled material with a Mr<IgG in the later fractions (2.2% for HMFG1 and 4.9% for PR1A3). Similar results were obtained using radioiodinated antibody, although the small amount of low molecular size material detected as a single peak with a longer retention time than the99mTc equivalent corresponds to free iodide. 相似文献
2.
99Tcm-pertechnetate is concentrated in the thyroid in the same way as iodide but it does not become organically bound. The uptake of 99Tcm is a measure of the thyroid trap, and this measurement is satisfactory as a routine test in the diagnosis of thyrotoxicosis. The reproducibility of the method is such that suppression tests can be carried out when necessary even when uptake is within the normal range of 0·4-3%. 99Tcm gives a low radiation dose to the thyroid and has certain other advantages over radioactive isotopes of iodine for early thyroid uptake measurements. It is particularly suitable when serial tests of thyroid function are required during treatment with an antithyroid drug. 相似文献
3.
Waldemar G. Johanson Jr. Marina G. Kennedy Frederick J. Bonte 《Applied microbiology》1973,25(4):592-594
The suitability of technetium (99mTc), a gamma emitter, for labeling of Diplococcus pneumoniae in studies of lung bacterial clearance was examined. A killed bacterial slurry with high specific activity was obtained with a ferric ascorbate reducing system. Approximately 5.5% of radioactive counts dissociated from labeled bacteria in 6 h. Rats were exposed to a uniformly mixed aerosol of untagged, viable pneumococci and killed, 99mTc-tagged pneumococci. The aerodynamic behavior of labeled and unlabeled pneumococci was similar. Viable bacterial counts and radioactive counts were determined in lung homogenates at intervals following exposure, and rates of bacterial killing and disappearance of radioactive counts were plotted. Radioactive counts did not increase in the liver during the period of observation, suggesting that the decrease in lung radioactivity represents mucociliary clearance and not release of isotope to the systemic circulation. The use of 99mTc for bacterial labeling provides advantages of technical simplicity and personnel safety compared to the use of beta-emitting isotopes. 相似文献
4.
Renal scintigraphy is an imaging method that uses small amount of radioactive materials called radiotracers, a Gamma camera and a computer to evaluate kidney functions and its anatomy. The present work reports the comparison of the relative renal functions (RRF) calculated with technetium-99m dimercaptosuccinic acid (99mTc‑DMSA) and technetium-99m diethylenetriaminepentaacetic acid (99mTc‑DTPA) for kidney patients of ages between 5 months and 71 years. A total of 50 patients including 29 male and 21 female has been selected and studied for renography. The mean RRFs have been found to be 52.68 ± 23.63% and 47.32 ± 23.63% respectively for the left and right kidneys with 99mTc-DMSA measurement. With 99mTc-DTPA the values are 52.74 ± 23.54% and 47.26 ± 23.54% for the same. In bivariate correlation analysis, a significant positive correlation (r = 0.996, P < .001) has been found between the RRFs calculated with the two methods. Following the patients’ diagnosis, in ANOVA test, no difference has been found between the RRFs calculated for the left and right kidneys. In Bland-Altman plots, the mean difference between the two methods has been found to be 0.1 and the correlation limit lies between −4.3 and 4.2. According to the result obtained in the present work, both the 99mTc-DMSA and 99mTc-DTPA scanning methods provide almost the same RRF values. It is, therefore, always not necessary to calculate the RRFs with both the methods. This study suggests that 99mTc-DMSA may be the primary choice for the evaluation of RRF, but if the glomerular filtration rate (GFR) and renogram curve are required, 99mTc-DTPA can be the obvious selection. 相似文献
5.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1988,15(4):409-417
Three cardiac glycosides, two natural, cymarin and convallotoxin and one synthetic, strophanthidin-β-d-glucoside were converted to their thiosemicarbazone and subsequently radiolabeled with 99mTc by chelation. The resulting radioactive chelate complexes were evaluated in animals to determine the suitability of this class of compounds for myocardial imaging. It was observed from the animal biodistribution data of the three radioactive compounds, there was a considerable variation in the heart to non-target organ uptake ratio. A possible explanation of this variation was offered in the light of their lipophilic character, protein binding ability and affinity towards non-target receptors. It is anticipated that this study may help to develop a 99mTc-cardiac glycoside complex with better distribution characteristics, and such a compound may offer a suitable alternative to 201Tl, which is at present used for myocardial imaging. 相似文献
6.
《Médecine Nucléaire》2007,31(1):29-32
The aim of this technical note is to evaluate an easy method to measure 99mTc samples with an activity of 1000, 100 and 10 Bq/L. This study is performed with a gamma-camera detector in two departments of Nuclear medicine in Avignon and in Nîmes. We develop a procedure to measure 99mTc radioactive waste at the two hospitals output in accordance with the DGS/DHOS no. 2001/323 circular requests of the Ministry for Employment and Solidarity. 相似文献
7.
Autoradiographic model experiments with 67Ga and 99mTc 总被引:1,自引:0,他引:1
Summary In order to evaluate the feasibility to localize correctly 67Ga citrate and 99mTc pertechnetate in tissues, the resolution of these radioactive compounds were measured in a model system using four different autoradiographic techniques, wet as well as dry.Wet autoradiographic techniques gave an almost complete loss of 67Ga. In deparaffinized sections of fixed and paraffin-embedded tissue the remaining 67Ga, which was probably bound to proteins, gave a resolution of 2.6 . 99mTc was either completely lost in wet techniques or the procedure could not be performed at all because of the very short half life of 99mTc.The resolution of 67Ga in a dry autoradiographic technique (according to Stumpf) was 6.9 and the resolution of 99mTc 22.6 .The technique in which frozen sections are thawed on dry film and consequently dryed, gave slightly better resolutions than the dry technique (according to Stumpf) with 67Ga as well as 99mTc.It is concluded that for the histological localization of 67Ga and 99mTc a dry technique is required. However, the use of a wet technique can be considered, provided a loss of the radioisotope is acceptable and the procedure is controlled by a dry technique. 相似文献
8.
Elisa Palma Bruno L. Oliveira João D. G. Correia Lurdes Gano Leonor Maria Isabel C. Santos Isabel Santos 《Journal of biological inorganic chemistry》2007,12(5):667-679
Aiming to develop new bone-seeking radiotracers based on the organometallic core fac-[99mTc(CO)3]+ with improved radiochemical and biological properties, we have prepared new conjugates with phosphonate pendant groups. The
conjugates comprise a chelating unit for metal coordination, which corresponds to a pyrazolyl-containing backbone (pz) with
a N,N,N donor-atom set, and a pendant diethyl phosphonate (pz-MPOEt), phosphonic acid (pz-MPOH) or a bisphosphonic acid (pz-BPOH)
group for bone targeting. Reactions of the conjugates with the precursor [99mTc(H2O)3(CO)3]+ yielded (mote than 95%) the single and well-defined radioactive species [99mTc(CO)3(κ3-pz-MPOEt)]+ (1a), [99mTc(CO)3(κ3-pz-MPOH]+ (2a) and [99mTc(CO)3(κ3-pz-BPOH)]+ (3a), which were characterized by reversed-phase high-performance liquid chromatography . The corresponding Re surrogates (1–3), characterized by the usual analytical techniques, including X-ray diffraction analysis in the case of 1, allowed for macroscopic identification of the radioactive conjugates. These radioactive complexes revealed high stability
both in vitro (phosphate-buffered saline solution and human plasma) and in vivo, without any measurable decomposition. Biodistribution
studies of the complexes in mice indicated a fast rate of blood clearance and high rate of total radioactivity excretion,
occurring primarily through the renal–urinary pathway in the case of complex 3a. Despite presenting moderate bone uptake (3.04 ± 0.47% injected dose per gram of organ, 4 h after injection), the high stability
presented by 3a and its adequate in vivo pharmacokinetics encourages the search for new ligands with the same chelating unit and different
bisphosphonic acid pendant arms. 相似文献
9.
Zusammenfassung Es wird eine Methode zur Mikrohistoautoradiographie wasserlöslicher Isotope beschrieben und an der Verteilung von 131J sowie 99mTc in der Magenschleimhaut demonstriert.Auf Grund mikrohistoautoradiographischer Untersuchungen wird gezeigt, daß Technetium-99m selektiv durch die Belegzellen der Magenschleimhaut ausgeschieden wird. Jod-131 wird demgegenüber von den Hauptzellen des Oberflächenepithels der Magenschleimhaut sezerniert. Die selektive Anreicherung von Technetium-99m in den Belegzellen macht wahrscheinlich, daß Technetium in den Belegzellen eine unmittelbare metabolisch gesteuerte Ausscheidung erfährt. Autoradiographisch wird somit in den Schleimhautzellen nach Gabe von Technetium fast die gesamte Aktivität im Fundus und nur wenig im Antrum gesehen. Die Aktivitätsverteilung in den Lymphgefäßen und Kapillaren der Submucosa ist in Antrum und Fundus gleich.Die Ergebnisse der quantitativen Bestimmung der Aktivitätsverteilung in den verschiedenen Magenabschnitten in Abhängigkeit von der Zeit geben eine gute Bestätigung der mikrohistoautoradiographischen Befunde.
Distribution of Technetium-99m and Jodine-131 in the gastric mucosaA technique to determine microhistoautoradiographical distribution of water soluble isotopes
Summary A method for microhistoautoradiographic examination of water soluble radioactive isotopes and its use in studying the distribution of 131J and 99mTc in the gastric mucosa is described.It is shown that technetium is selectively secreted by the parietal cells of the gastric mucosa. In contrast 131J is secreted by the chief and mucosal cells. The selective accumulation of 99mTc in the parietal cells suggests that technetium is secreted via a metabolic pathway. The main activity of 99mTc is observed in the gastric fundus. The distribution of both isotopes within the submucous lymphoid and capillary vessels of the antrum and fundus is equal.The microhistoautoradiographic results in the different parts of the stomach are confirmed by quantitative scintillation counting.相似文献
10.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1992,19(3):375-388
Different derivatives of MAG3 carrying amino acids such as d- or l-alanine, d-serine, d-2-aminobutyric acid, d-valine or d-phenylglycine were synthesized and their 99mTc-complexes were evaluated in mice and a baboon. The efficiency of renal handling of the examined 99mTc-complexes is influenced not only by their lipophilicity but also to a great extent by their configuration and the site of substitution. The renal excretion characteristics of 99mTc-MAGAG-DA are superior to those of 99mTc-MAG3 and the studied 99mTc-complexes in both animal species.In an attempt to improve the renal handling of 99mTc-MAG3 and to evaluate the effect of derivatization we have synthesized different derivatives of MAG3 in which one or more glycyl groups are replaced by other amino acids such as d- or l-alanine, D-serine, D-2-aminobutyric acid, D-valine or D-phenylglycine. Due to the presence of a chiral centre in the ligand core, exchange labelling of each of the MAG3 derivatives results in the formation of two diastereomeric technetium complexes. These isomers were separated by HPLC and evaluated in mice. Biodistribution in mice indicates that the efficiency of renal handling of the examined 99mTc-complexes is not only influenced by their lipophilicity but also to a great extent by their configuration. The renal excretion characteristics of isomer dA of 99mTc-MAGAG in mice are superior to those of all other studied 99mTc-complexes and also of the reference compound [131I]Hippuran. The isomers lB of several alanyl derivatives of 99mTc-MAG3 exhibit a pronounced renal retention in both mice and baboon. The results of the evaluation in a baboon confirm the superiority of 99mTc-MAGAG-dA over 99mTc-MAG3 and the other studied 99mTc-complexes. 相似文献
11.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1989,16(4):419-421
Iodine-131-labeled iodo-antipyrine and 99mTc-labeled erythrocytes were used to measure water content in lungs. These radioactive tracers were injected into 11 dogs with injured lungs. Blood samples were drawn and the animals sacrificed. The lungs were removed, weighed and homogenized. Samples of blood and lung homogenate were assayed for 131I and 99mTc. Samples were also weighed before and after drying to a constant weight at 70–76 °C. Extravascular lung water was determined by the dual-isotope technique and again by gravimetric analysis. The average ratio of the results from the two different methods was 1.14 ± 0.20. The two methods were also compared by regression analysis and the correlation coefficient was 0.97 ± 0.09. 相似文献
12.
R. Jankowsky B. Noll B. Johannsen 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》1999,724(2):6077
Diagnostically used 99mTc kit radiopharmaceuticals were analyzed using capillary zone electrophoresis with radioactivity detection: 99mTc-bis(bis(2-ethyloxyethyl)phosphino)ethane (99mTc-Myoview, 99mTc-Tetrofosmin), 99mTc-trans(1,2-bis(dehydro-2,2,5,5,-tetramethyl-3-furanone-4-methylene-amino)ethane)-tris(3-methoxy-1-propyl)phosphine) (99mTc-Technescan Q12, 99mTc-Furifosmin), 99mTc-methoxyisobutylisonitrile (99mTc-MIBI), 99mTc-
,
-ethylenecysteine diethylester dimer (99mTc-ECD), 99mTc-d,l-hexamethylene propyleneamine oxime (99mTc-HMPAO), 99mTc-diethylenetriaminepentaacetic acid (99mTc-DTPA), 99mTc-ethylene hepatobiliary iminodiacetic acid (99mTc-EHIDA), 99mTc-
,
-ethylenecysteine dimer (99mTc-EC), 99mTc-mercaptoacetylglycylglycylglycine (99mTc-MAG3), 99mTc-dimercaptosuccinic acid (99mTc-DMSA), 99mTc-methylene diphosphonate (99mTc-MDP) and 99mNaTcO4. A pressure-driven capillary zone electrophoresis was employed to detect small anions of high electrophoretic mobility and cations within one run. Effective 99mTc complex charges could be determined by a neutral internal standard. All complexes showed the expected electrophoretic behaviours in view of their charges. Pure products were obtained for the majority of the studied complexes. In the case of 99mTc-Q12, 99mTc-EHIDA and 99mTc-MDP, complex mixtures were detected. The high potential of CE for the analysis of 99mTc radiopharmaceuticals could be shown. 相似文献
13.
《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》1999,724(2):365-371
Diagnostically used 99mTc kit radiopharmaceuticals were analyzed using capillary zone electrophoresis with radioactivity detection: 99mTc-bis(bis(2-ethyloxyethyl)phosphino)ethane (99mTc-Myoview, 99mTc-Tetrofosmin), 99mTc-trans(1,2-bis(dehydro-2,2,5,5,-tetramethyl-3-furanone-4-methylene-amino)ethane)-tris(3-methoxy-1-propyl)phosphine) (99mTc-Technescan Q12, 99mTc-Furifosmin), 99mTc-methoxyisobutylisonitrile (99mTc-MIBI), 99mTc-l,l-ethylenecysteine diethylester dimer (99mTc-ECD), 99mTc-d,l-hexamethylene propyleneamine oxime (99mTc-HMPAO), 99mTc-diethylenetriaminepentaacetic acid (99mTc-DTPA), 99mTc-ethylene hepatobiliary iminodiacetic acid (99mTc-EHIDA), 99mTc-l,l-ethylenecysteine dimer (99mTc-EC), 99mTc-mercaptoacetylglycylglycylglycine (99mTc-MAG3), 99mTc-dimercaptosuccinic acid (99mTc-DMSA), 99mTc-methylene diphosphonate (99mTc-MDP) and 99mNaTcO4. A pressure-driven capillary zone electrophoresis was employed to detect small anions of high electrophoretic mobility and cations within one run. Effective 99mTc complex charges could be determined by a neutral internal standard. All complexes showed the expected electrophoretic behaviours in view of their charges. Pure products were obtained for the majority of the studied complexes. In the case of 99mTc-Q12, 99mTc-EHIDA and 99mTc-MDP, complex mixtures were detected. The high potential of CE for the analysis of 99mTc radiopharmaceuticals could be shown. 相似文献
14.
Max Kaufmann Jorgen Marqverson Kenneth E. Stanley Christian Mouritzen Hans Hvid-Hansen 《Cancer immunology, immunotherapy : CII》1986,22(1):56-61
Summary The distribution of Corynebacterium parvum labeled with 131iodine or 99mtechnetium was studied in 17 patients with bronchogenic carcinoma. The labeled bacteria were given intravenously or intrapleurally and monitored by whole-body gamma tracking and samples of blood and urine. Even though the rate of physical decay is quite different for 131iodine and 99mtechnetium, the tracking time of labeled bacteria was limited to 24 h after injection for both radioactive isotopes. Technetium labeling was preferred because of greater imaging resolution and less radiation dose to the patient. Following intravenous administration, labeled C. parvum was found predominantly in the liver and spleen, and in a lesser amount in the lung. Radioactivity was confined to the pleural cavity after intrapleural injection. These results suggest the combined intravenous and intrapleural route of adjuvant immunosupportive agents such as C. parvum for operable lung cancer patients. 相似文献
15.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1988,15(4):451-457
The Chromatographic and in vivo behaviour in mice of the 99mTcN- and 99mTc(Sn)-complexes of 2-mercaptopyridine, 2-mercaptopyrimidine, thiouracil, 6-mercaptopurine and thioguanine is compared. The biological distribution of the 99mTcN-complexes is generally different to that of the 99mTc(Sn)-complexes of the same ligand with the difference being very dependent on the structure of the ligand. The 99mTcN-mercaptopyrimidine complex has potential as a blood-cell labelling agent. 相似文献
16.
The building blocks fac-[99mTc{κ3-HB(timMe)3}(CO)3] and fac-[99mTc{κ3-R(μ-H)B(timMe)2}(CO)3] [R is H (4a), Ph (5a); timMe is 2-mercapto-1-methylimidazolyl] were obtained almost quantitatively by reacting fac-[99mTc(CO)3(H2O)3]+ with the corresponding scorpionate. These compounds cross the intact blood–brain barrier in mice, with significant retention in the case of 4a and 5a. Using 4a as the lead structure, we have synthesized the functionalized complexes fac-[M{κ3-H(μ-H)B(timBu-pip)2}(CO)3] [M is Re (8), 99mTc (8a); timBu-pip is methyl[4-((2-methoxyphenyl)-1-piperazinyl)butyl](2-mercapto-1-methylimidazol-5-yl)methanamide] and fac-[M{κ
3-H(μ-H)B(timMe)(timBu-pip)}(CO)3] [M is Re (9), 99mTc (9a)] and evaluated their potential as radioactive probes for the targeting of brain 5-HT1A serotonergic receptors. The Re complexes exhibit excellent affinity [IC50=0.172 ± 0.003 nM (8); IC50=0.65 ± 0.01 nM (9)] for the 5-HT1A receptor. The radioactive congeners (99mTc) have shown an initial brain uptake of 1.38 ± 0.46%ID g−1 (8a) and 0.43 ± 0.12%ID g−1 (9a), but suffer from a relatively fast washout. 相似文献
17.
This study presents current status of performance of radiopharmaceutical activity measurements using radionuclide calibrators in Belgium. An intercomparison exercise was performed among 15 hospitals to test the accuracy of 99mTc, 18F and 111In activity measurements by means of radionuclide calibrators. Four sessions were held in different geographical regions between December 2013 and February 2015. The data set includes measurements from 38 calibrators, yielding 36 calibrations for 99mTc and 111In, and 21 calibrations for 18F. For each radionuclide, 3 ml of stock solution was measured in two clinical geometries: a 10 ml glass vial and a 10 ml syringe. The initial activity was typically 100 MBq for 99mTc, 15 MBq for 111In and 115 MBq for 18F. The reference value for the massic activity of the radioactive solutions was determined by means of primary and secondary standardisation techniques at the radionuclide metrology laboratory of the JRC.The overall results of the intercomparison were satisfactory for 99mTc and 18F, since most radionuclide calibrators (>70%) were accurate within ±5% of the reference value. Nevertheless, some devices underestimated the activity by 10–20%. Conversely, 111In measurements were strongly affected by source geometry effects and this had a negative impact on the accuracy of the measurements, in particular for the syringe sample. Large overestimations (up to 72%) were observed, even when taking into account the corrections and uncertainties supplied by the manufacturers for container effects. The results of this exercise encourage the hospitals to perform corrective actions to improve the calibration of their devices where needed. 相似文献
18.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1991,18(7):695-703
Direct labeling involves 99mTc binding to different donor groups on the protein, giving multiple binding sites of various affinities resulting in an in vivo instability. The stability has been considerably improved by activating the antibody using a controlled reduction reaction (using 2-aminoethanethiol). This reaction generates sulfhydryl groups, which are known to strongly bind 99mTc. The direct 99mTc antibody labeling method was explored using whole antibodies and fragments. Analytical methods were developed for routine evaluation of radiolabeling yield and in vitro stability.Stable direct antibody labeling with 99mTc requires the generation of sulfhydryl groups, which show high affinity binding sites for 99mTc. Such groups are obtained with 2-aminoethanethiol (AET), which induces the reduction of the intrachain or interchain disulfide bond, with no structural deterioration or any loss of immunobiological activity of the antibody. The development of fast, reliable analytical methods has made possible the qualitative and quantitative assessment of technetium species generated by the radiolabeling process. Labeling stability is determined by competition of the 99mTc-antibody bond with three ligands, Chelex 100 (a metal chelate-type resin), free DTPA solution and 1% HSA solution.Very good 99mTc-antibody stability is obtained with activated IgG (IgGa) and Fab′ fragment, which makes these substances possible candidates for immunoscintigraphy use. 相似文献
19.
《International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology》1991,18(2):215-226
A series of 99mTc-bis(aminoethanethiol)-fatty acid (99mTc-BAT-fatty acid) analogs were synthesized and evaluated as potential tracers of myocardial metabolism. The BAT-fatty acid precursors were prepared using a new synthetic route that avoids the use of strong reducing agents such as lithium aluminum hydride. Biodistribution studies of the no-carrier-added 99mTc-complexes were conducted in rats using [125I]IPPA as an internal standard. The myocardial uptake of the 99mTc-BAT-fatty acid analogs was significantly less than that of [125I]IPPA and indicates the 99mTc analogs are not suitable candidates for SPECT-based myocardial imaging studies. 相似文献
20.
Joerg Kotzerke Robert Punzet Roswitha Runge Sandra Ferl Liane Oehme Gerd Wunderlich Robert Freudenberg 《PloS one》2014,9(8)
99mTc is the standard radionuclide used for nuclear medicine imaging. In addition to gamma irradiation, 99mTc emits low-energy Auger and conversion electrons that deposit their energy within nanometers of the decay site. To study the potential for DNA damage, direct DNA binding is required. Plasmid DNA enables the investigation of the unprotected interactions between molecules and DNA that result in single-strand breaks (SSBs) or double-strand breaks (DSBs); the resulting DNA fragments can be separated by gel electrophoresis and quantified by fluorescent staining. This study aimed to compare the plasmid DNA damage potential of a 99mTc-labeled HYNIC-DAPI compound with that of 99mTc pertechnetate (99mTcO4
−). pUC19 plasmid DNA was irradiated for 2 or 24 hours. Direct and radical-induced DNA damage were evaluated in the presence or absence of the radical scavenger DMSO. For both compounds, an increase in applied activity enhanced plasmid DNA damage, which was evidenced by an increase in the open circular and linear DNA fractions and a reduction in the supercoiled DNA fraction. The number of SSBs elicited by 99mTc-HYNIC-DAPI (1.03) was twice that caused by 99mTcO4
− (0.51), and the number of DSBs increased fivefold in the 99mTc-HYNIC-DAPI-treated sample compared with the 99mTcO4
− treated sample (0.02 to 0.10). In the presence of DMSO, the numbers of SSBs and DSBs decreased to 0.03 and 0.00, respectively, in the 99mTcO4
– treated samples, whereas the numbers of SSBs and DSBs were slightly reduced to 0.95 and 0.06, respectively, in the 99mTc-HYNIC-DAPI-treated samples. These results indicated that 99mTc-HYNIC-DAPI induced SSBs and DSBs via a direct interaction of the 99mTc-labeled compound with DNA. In contrast to these results, 99mTcO4
− induced SSBs via radical formation, and DSBs were formed by two nearby SSBs. The biological effectiveness of 99mTc-HYNIC-DAPI increased by approximately 4-fold in terms of inducing SSBs and by approximately 10-fold in terms of inducing DSBs. 相似文献