Pub Date : 2009-06-25DOI: 10.2174/1876388X00901010024
M. Thakur
{"title":"DEDICATION: Wolfgang Becker (1952-2002)","authors":"M. Thakur","doi":"10.2174/1876388X00901010024","DOIUrl":"https://doi.org/10.2174/1876388X00901010024","url":null,"abstract":"","PeriodicalId":88754,"journal":{"name":"The open nuclear medicine journal","volume":"1 1","pages":"24-24"},"PeriodicalIF":0.0,"publicationDate":"2009-06-25","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68126484","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2009-05-20DOI: 10.2174/1876388X00901010015
M. Mitterhauser, D. Haeusler, L. Mien, J. Ungersboeck, L. Nics, R. Lanzenberger, K. Sindelar, H. Viernstein, R. Dudczak, K. Kletter, H. Spreitzer, W. Wadsak
Introduction: Since the Adenosine-A3-receptor was identified in the late 1990´s, there is little data available de- scribing its distribution in vivo. Recently, we introduced ( 18 F)FE@SUPPY as the first PET-tracer for this receptor. In the present investigation we translated this fluoroethyl-ester into the fluoroethyl-thioester ( 18 F)FE@SUPPY:2 (5-ethyl 2,4- diethyl-3-((2-( 18 F)fluoroethyl) sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate). Aims of the present study were the evaluation of (1) the automatized preparation of both ( 18 F)FE@SUPPY-derivatives, (2) the biodistribution of ( 18 F)FE@SUPPY:2, (3) the lipophilicity and (4) the comparison of the findings of ( 18 F)FE@SUPPY and ( 18 F)FE@SUPPY:2. Methods: The automated preparations of both ( 18 F)FE@SUPPY-analogs were performed on a GE TRACERlab FxFN syn- thesizer using suitable precursors. Biodistribution experiments were performed using Sprague-Dawley rats/Him:OFA. Lipophilicity of the compounds was determined using an HPLC assay. Results: 22 automated radiosyntheses were performed for both radiotracers. Specific radioactivity was 70 ± 26GBq/� mol for ( 18 F)FE@SUPPY and 340 ± 140GBq/� mol for ( 18 F)FE@SUPPY:2. Biodistribution experiments evinced bowels and liver as organs with highest uptake and intermediate uptake in kidney, lung and heart. LogP values of both molecules ranged from 3.99 to 4.12 at different pH. Conclusion: From a radiopharmaceutical perspective, drastically better specific radioactivities would militate in favour of ( 18 F)FE@SUPPY:2; preclinical evaluations, so far, do not permit the decision upon the selection of the optimum ( 18 F)FE@SUPPY-derivative. With ( 18 F)FE@SUPPY:2, we are able to provide a second potential tracer that could help to further characterize the still quite unexplored Adenosine-A3-receptor.
{"title":"Automatisation and First Evaluation of [18F]FE@SUPPY:2, an AlternativePET-Tracer for the Adenosine A3 Receptor: A Comparison with[18F]FE@SUPPY","authors":"M. Mitterhauser, D. Haeusler, L. Mien, J. Ungersboeck, L. Nics, R. Lanzenberger, K. Sindelar, H. Viernstein, R. Dudczak, K. Kletter, H. Spreitzer, W. Wadsak","doi":"10.2174/1876388X00901010015","DOIUrl":"https://doi.org/10.2174/1876388X00901010015","url":null,"abstract":"Introduction: Since the Adenosine-A3-receptor was identified in the late 1990´s, there is little data available de- scribing its distribution in vivo. Recently, we introduced ( 18 F)FE@SUPPY as the first PET-tracer for this receptor. In the present investigation we translated this fluoroethyl-ester into the fluoroethyl-thioester ( 18 F)FE@SUPPY:2 (5-ethyl 2,4- diethyl-3-((2-( 18 F)fluoroethyl) sulfanylcarbonyl)-6-phenylpyridine-5-carboxylate). Aims of the present study were the evaluation of (1) the automatized preparation of both ( 18 F)FE@SUPPY-derivatives, (2) the biodistribution of ( 18 F)FE@SUPPY:2, (3) the lipophilicity and (4) the comparison of the findings of ( 18 F)FE@SUPPY and ( 18 F)FE@SUPPY:2. Methods: The automated preparations of both ( 18 F)FE@SUPPY-analogs were performed on a GE TRACERlab FxFN syn- thesizer using suitable precursors. Biodistribution experiments were performed using Sprague-Dawley rats/Him:OFA. Lipophilicity of the compounds was determined using an HPLC assay. Results: 22 automated radiosyntheses were performed for both radiotracers. Specific radioactivity was 70 ± 26GBq/� mol for ( 18 F)FE@SUPPY and 340 ± 140GBq/� mol for ( 18 F)FE@SUPPY:2. Biodistribution experiments evinced bowels and liver as organs with highest uptake and intermediate uptake in kidney, lung and heart. LogP values of both molecules ranged from 3.99 to 4.12 at different pH. Conclusion: From a radiopharmaceutical perspective, drastically better specific radioactivities would militate in favour of ( 18 F)FE@SUPPY:2; preclinical evaluations, so far, do not permit the decision upon the selection of the optimum ( 18 F)FE@SUPPY-derivative. With ( 18 F)FE@SUPPY:2, we are able to provide a second potential tracer that could help to further characterize the still quite unexplored Adenosine-A3-receptor.","PeriodicalId":88754,"journal":{"name":"The open nuclear medicine journal","volume":"1 1","pages":"15-23"},"PeriodicalIF":0.0,"publicationDate":"2009-05-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68125427","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2009-04-09DOI: 10.2174/1876388X00901010009
I. Vermeltfoort, P. Raijmakers, O. Bondarenko, A. Zwijnenburg, M. Hofman, G. Teule, A. Beek, A. Rossum
Background: In cardiac syndrome X, which is a syndrome defined as chest pain, positive exercise stress testing and/or reversible myocardial perfusion defects during myocardial scintigraphy and normal coronary angiograms, the ischemic origin is still debated. No previous study compared the myocardial perfusion in stress first-pass cardiac magnetic resonance (CMR) versus stress single-photon emission computed tomography (SPECT) in cardiac syndrome X. Methods: We performed stress SPECT and CMR imaging for 20 syndrome X patients. Perfusion analysis of the CMR was done by using the normalized upslope of myocardial signal enhancement to derive the myocardial perfusion index (MPI) and the myocardial perfusion reserve index (MPRI). The SPECT images were visually scored by 3 observers using a seg- mental model. Results: An MPRI of 1.2 was found for 31 (9%) of the 335 segments, indicating local ischemia. SPECT indicated re- versible perfusion defects for 39 (12%) of the 335 segments. However, the combination of both an MPRI 1.2 and a re- versible perfusion defect was detected in only 3 segments. Conclusions: Our data show about 10% stress-induced myocardial perfusion abnormalities on CMR and SPECT, suggest- ing local ischemia. However, only in 1% of the segments there was concordance for the presence of myocardial ischemia with both exams. This result may be evidence for the variability over time of the mechanisms responsible for coronary microvascular dysfunction.
{"title":"Correlation of Myocardial Perfusion on Cardiac Magnetic Resonance Versus Myocardial Perfusion Scintigraphy in Cardiac Syndrome X","authors":"I. Vermeltfoort, P. Raijmakers, O. Bondarenko, A. Zwijnenburg, M. Hofman, G. Teule, A. Beek, A. Rossum","doi":"10.2174/1876388X00901010009","DOIUrl":"https://doi.org/10.2174/1876388X00901010009","url":null,"abstract":"Background: In cardiac syndrome X, which is a syndrome defined as chest pain, positive exercise stress testing and/or reversible myocardial perfusion defects during myocardial scintigraphy and normal coronary angiograms, the ischemic origin is still debated. No previous study compared the myocardial perfusion in stress first-pass cardiac magnetic resonance (CMR) versus stress single-photon emission computed tomography (SPECT) in cardiac syndrome X. Methods: We performed stress SPECT and CMR imaging for 20 syndrome X patients. Perfusion analysis of the CMR was done by using the normalized upslope of myocardial signal enhancement to derive the myocardial perfusion index (MPI) and the myocardial perfusion reserve index (MPRI). The SPECT images were visually scored by 3 observers using a seg- mental model. Results: An MPRI of 1.2 was found for 31 (9%) of the 335 segments, indicating local ischemia. SPECT indicated re- versible perfusion defects for 39 (12%) of the 335 segments. However, the combination of both an MPRI 1.2 and a re- versible perfusion defect was detected in only 3 segments. Conclusions: Our data show about 10% stress-induced myocardial perfusion abnormalities on CMR and SPECT, suggest- ing local ischemia. However, only in 1% of the segments there was concordance for the presence of myocardial ischemia with both exams. This result may be evidence for the variability over time of the mechanisms responsible for coronary microvascular dysfunction.","PeriodicalId":88754,"journal":{"name":"The open nuclear medicine journal","volume":"1 1","pages":"9-14"},"PeriodicalIF":0.0,"publicationDate":"2009-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"68125347","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2009-01-01DOI: 10.2174/1876388X00901010001
Tung-Kwang Lee, Kevin F O'Brien, Weidong Wang, Chao Sheng, Tao Wang, Roberta M Johnke, Ron R Allison
The multifold bioactive medicinal properties of ginseng have been closely linked to its antioxidative ability, which is related to its ginsenoside content. Since the key mechanism of radiation-induced cell death and tissue damage is the generation of reactive oxygen species (ROS) that attack cellular DNA, this study focuses on the impact of a standardized North American ginseng extract (NAGE) on (137)Cs-induced oxidative stress in human peripheral lymphocytes (PBL) obtained from 10 healthy individuals (6M/4F), 42.7 +/- 4.6 years of age. At two different time points (0 h and 24 h before irradiation), we applied NAGE (250 - 1000 microg ml(-1)) to mononuclear cell cultures for cytokinesis-block micronuclei (MN) assay and determination of the state of oxidative stress in PBL. We found that at both time points, NAGE significantly reduced the MN yields in PBL after irradiation (1 and 2 Gy) in a concentration-dependent manner (P<0.001). Compared with radiation alone, the maximum reduction rate of MN yield were 51.1% and 49.1% after 1 Gy and 2 Gy exposures, respectively. We also found that before irradiation the presence of NAGE in the culture medium resulted in a significant increased intracellular total antioxidant capacity (TAC) in PBL. At both time points, the increment of (137)Cs-induced MN yields in PBL was positively correlated with the increment of intracellular ROS production (R = 0.6 - 0.7, P = 0.002), but negatively correlated with the reduction of TAC levels (R = -0.4 -0.5, P = 0.02 - 0.004). However, the presence of NAGE in the culture medium significantly increased the TAC levels, while concomitantly decreasing both ROS production and MN yields in PBL (P<0.001). Our findings that NAGE is effective in protecting human PBL against radiation-induced oxidative stress should encourage further in vivo study of dietary supplementation with NAGE as an effective natural radiation countermeasure.
{"title":"American Ginseng Modifies Cs-Induced DNA Damage and Oxidative Stress in Human Lymphocytes.","authors":"Tung-Kwang Lee, Kevin F O'Brien, Weidong Wang, Chao Sheng, Tao Wang, Roberta M Johnke, Ron R Allison","doi":"10.2174/1876388X00901010001","DOIUrl":"https://doi.org/10.2174/1876388X00901010001","url":null,"abstract":"<p><p>The multifold bioactive medicinal properties of ginseng have been closely linked to its antioxidative ability, which is related to its ginsenoside content. Since the key mechanism of radiation-induced cell death and tissue damage is the generation of reactive oxygen species (ROS) that attack cellular DNA, this study focuses on the impact of a standardized North American ginseng extract (NAGE) on (137)Cs-induced oxidative stress in human peripheral lymphocytes (PBL) obtained from 10 healthy individuals (6M/4F), 42.7 +/- 4.6 years of age. At two different time points (0 h and 24 h before irradiation), we applied NAGE (250 - 1000 microg ml(-1)) to mononuclear cell cultures for cytokinesis-block micronuclei (MN) assay and determination of the state of oxidative stress in PBL. We found that at both time points, NAGE significantly reduced the MN yields in PBL after irradiation (1 and 2 Gy) in a concentration-dependent manner (P<0.001). Compared with radiation alone, the maximum reduction rate of MN yield were 51.1% and 49.1% after 1 Gy and 2 Gy exposures, respectively. We also found that before irradiation the presence of NAGE in the culture medium resulted in a significant increased intracellular total antioxidant capacity (TAC) in PBL. At both time points, the increment of (137)Cs-induced MN yields in PBL was positively correlated with the increment of intracellular ROS production (R = 0.6 - 0.7, P = 0.002), but negatively correlated with the reduction of TAC levels (R = -0.4 -0.5, P = 0.02 - 0.004). However, the presence of NAGE in the culture medium significantly increased the TAC levels, while concomitantly decreasing both ROS production and MN yields in PBL (P<0.001). Our findings that NAGE is effective in protecting human PBL against radiation-induced oxidative stress should encourage further in vivo study of dietary supplementation with NAGE as an effective natural radiation countermeasure.</p>","PeriodicalId":88754,"journal":{"name":"The open nuclear medicine journal","volume":"1 1","pages":"1-8"},"PeriodicalIF":0.0,"publicationDate":"2009-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2782928/pdf/nihms157103.pdf","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"28536020","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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