bluuebunny/crossref_metadata_2025_split huggingface dataset:
Efficient synthesis of 2‐bromo‐1‐[18F]fluoroethane and its application in the automated preparation of 18F‐fluoroethylated radiopharmaceuticals
Authors: Comagic S. , Piel M. , Schirrmacher R. , Höhnemann S. , Rösch F. 
Published: April 2012

AbstractAn efficient synthesis of 2‐bromo‐1‐[18F]fluoroethane from commercially available 1,2‐dibromoethane and its integration into an automated preparation device was developed for the routine synthesis of 18F‐fluoroethylated radiopharmaceuticals. The precursor 1,2‐dibromoethane was reacted with the [18F]fluoride/Kryptofix®2.2.2./carbonate‐complex in acetonitrile at 70°C for 3 minutes. The crude reaction mixture was diluted with water, loaded on a LiChrolute ®EN‐cartridge, eluated with acetonitrile and passed through an Alumina ®B‐cartridge. The method can provide 2‐bromo‐1‐[18F]fluoroethane with 98% radiochemical purity completely free of 1, 2‐dibromoethan within 10 min, thus avoiding a purifying distillation step. This method was easily integrated into an automated system for the routine synthesis of 18F‐fluoroalkylated radiopharmaceuticals.
Preparation of 16α‐[18F]fluoroestradiol‐3‐sulphamate and 16α‐[18F]fluoroestradiol‐17β‐sulphamate in an automated module
Authors: Römer J. , Füchtner F. , Steinbach J. , Kasch H. 
Published: April 2012

AbstractThe procedure described can simultaneously provide about 3GBq 16α‐[18F]fluoroestradiol‐3‐sulphamate and about 1 GBq 16α‐[18F]fluoroestradiol‐17β‐sulphamate of high radiochemical purity. By treating 16α‐[18F]fluoroestradiol‐3, 17β‐disulphamate with Kryptofix 2.2.2 and potassium carbonate as a base, 16α‐[18F]fluoro‐estradiol‐17β‐sulphamate became accessible with a still higher radioactivity level.
Purification and concentration of radioiodine isotopes using platinum, palladium and nickel, and the application in heterogeneous catalysis
Authors: Braker A. H. , Moet F. P. , van der Zwart R. E. , Eersels J. L. H. , Herscheid J. D. M. 
Published: April 2012

AbstractIt is possible to concentrate and purify radioiodine using a small column, filled with platinum powder. Iodine is absorbed quantitatively in diluted sulfuric acid and desorbed in an alternating stream of hydrogen gas and an appropriate solvent. The chemical form of the eluted iodine is iodide, even when oxidation products of iodine are loaded on the column.As on‐column halogen exchange reactions were not successful, concentration and reactions on nickel and palladium columns are now under investigation.
Preparation of [11C]formaldehyde from [11C]methanol using silver‐containing ceramics
Authors: Roeda D. , Dollé F. , Crouzel C. 
Published: April 2012

AbstractA silver‐containing ceramics has been evaluated as a catalyst for oxidation of [11C]methanol to [11C]formaldehyde. 7.99 GBq of [11C]carbon dioxide was reduced to [11C]methanol which could be reoxidized to 1.73 GBq of [11C]formaldehyde in 5 minutes (25%, decay corrected).
Synthesis and in vivo evaluation of [18F]ORG 13063, a potential pet radioligand for the 5‐HT1A receptor
Authors: Vandecapelle M. , De Vos F. , Vermeirsch H. , Strijckmans K. , Leysen D. , Audenaert K. , Dierckx R. A. , Slegers G. 
Published: April 2012

Abstract[18F]Org 13063 or 4‐[18F]fluoro‐N‐{2‐[4‐(6‐trifluoromethyl‐2‐pyridinyl)‐1‐piperazinyl]ethyl}benzamide was synthesized by nucleophilic aromatic substitution on the nitro precursor in a microwave oven (5 min, 700 W). Overall radiochemical yield was 20 % (EOB), chemical and radiochemical purity were respectively higher than 95 and 99 %. Specific activity was always higher than 18.5 GBq/μmol (500 mCi/μmol). Biodistribution studies in rabbits were performed leading to 0.77 % ID in the brain at 5 min p.i. Radioactivity concentration of brain was significantly higher than that of blood. However, no significant differences in % ID/g tissue of the different isolated brain regions (hippocampus, hypothalamus, striatum, cortex and cerebellum) could be demonstrated.
Synthesis and radiosynthesis with a positron emitter of EP 00652218, a potent antagonist of NK1 receptor, and of a fluoro analog for in vivo evaluation of the substance P receptor by pet
Authors: Guéret C. , Le Bas M. D. , Perrio C. , Dauphin F , Dhilly M. , Chazalviel L. , Emond P. , Chalon S. , Tymciu S. , Guilloteau D. , Lasne M.‐C. , Barré L. 
Published: April 2012

AbstractNeurokinins (NKs) are the most important of the peptides released from neuronal sensory afferents. In mammals different NKs [substance P (SP), neurokinin A (NKA) and neurokinin B (NKB)] act as neurotransmitters and neuromodulators.(1) The biological responses induced by these neuropeptides are mediated by three distinct receptors NK1, NK2 and NK3 respectively. The NK1 receptors are widely distributed throughout the CNS and peripheral nervous systems. In recent years, clinical studies with selective NK1 receptor antagonists showed results for the treatment of emesis, depression, anxiety, pain and migraine.(2) Since the discovery of the first selective non‐peptide NK1 antagonist CP‐96,345, a considerable research in this area has been developed by the pharmaceutical industry.(3) In 1995, Takeda company described a novel class of highly potent, selective, and orally active NK1 antagonists such as 6‐pyrido[3, 4‐b]pyridinecarboxamide derivatives.(4) In this series, EP 00652218 1 (Scheme 1) was shown to exhibit subnanomolar affinity (IC50: 0.21nM, in vitro inhibition of [125I]‐BH‐SP binding in human IM‐9 cells) towards the NK1 receptors. Moreover, SAR studies demonstrated that the bis (trifluoromethylbenzyl) moiety was essential for the affinity. This led us to consider that EP 00652218 1 could be a good candidate for in vivo imaging of NK1 receptors and that the design of pyridine or phenyl ring substituted analogs would retain a high affinity. In order to develop ligands that could be used either in PET or SPECT studies, we undertook the synthesis of compounds bearing an halogen atom (fluorine, bromine or iodine). In this paper we report both the synthesis and labelling of the reference EP 00652218 1 with carbon‐11 and of the analog 2 with fluorine‐18 (Schemes 1, 2 and 3).
Tibiofemoral cartilage contact biomechanics in patients after reconstruction of a ruptured anterior cruciate ligament
Authors: Hosseini Ali , Van de Velde Samuel , Gill Thomas J. , Li Guoan 
Published: April 2012

AbstractWe investigated the in vivo cartilage contact biomechanics of the tibiofemoral joint in patients after reconstruction of a ruptured anterior cruciate ligament (ACL). A dual fluoroscopic and MR imaging technique was used to investigate the cartilage contact biomechanics of the tibiofemoral joint during in vivo weight‐bearing flexion of the knee in eight patients 6 months following clinically successful reconstruction of an acute isolated ACL rupture. The location of tibiofemoral cartilage contact, size of the contact area, cartilage thickness at the contact area, and magnitude of the cartilage contact deformation of the ACL‐reconstructed knees were compared with those previously measured in intact (contralateral) knees and ACL‐deficient knees of the same subjects. Contact biomechanics of the tibiofemoral cartilage after ACL reconstruction were similar to those measured in intact knees. However, at lower flexion, the abnormal posterior and lateral shift of cartilage contact location to smaller regions of thinner tibial cartilage that has been described in ACL‐deficient knees persisted in ACL‐reconstructed knees, resulting in an increase of the magnitude of cartilage contact deformation at those flexion angles. Reconstruction of the ACL restored some of the in vivo cartilage contact biomechanics of the tibiofemoral joint to normal. Clinically, recovering anterior knee stability might be insufficient to prevent post‐operative cartilage degeneration due to lack of restoration of in vivo cartilage contact biomechanics. © 2012 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 30:1781–1788, 2012
Angiogenesis and myogenesis in mouse tibialis anterior muscles during distraction osteogenesis: VEGF, its receptors, and myogenin genes expression
Authors: Nishisho Toshihiko , Yukata Kiminori , Matsui Yoshito , Matsuura Tetsuya , Higashino Kosaku , Suganuma Katsuyoshi , Nikawa Takeshi , Yasui Natsuo 
Published: April 2012

AbstractAngiogenesis and myogenesis occur in the surrounding skeletal muscles following distraction osteogenesis, but their molecular mechanisms remain unclear. The present study investigated morphological features of lengthened muscles and the time course change of vascular endothelial growth factor (VEGF), its receptors (VEGFR‐1 and VEGFR‐2) and myogenin gene expression profiles related to angiogenesis and myogenesis in tibialis anterior (TA) muscles with a mouse model of distraction osteogenesis, which involves 1 week of waiting period (latency phase), 2 weeks of intermittent distraction (distraction phase), and 5 weeks of remodeling period (consolidation phase). Macroscopic findings showed that lengthened TA muscles increased to approximately 42% longer and 10% heavier at the end of the process when compared to pre‐surgery. During the distraction phase, VEGF and its receptors were induced in the vascular endothelial cells, myogenin‐positive satellite cells and myocytes, and subsequently, capillary progression and myogenesis were increased. Real‐time RT‐PCR showed that Vegf, Vegfr‐1, Vegfr‐2, and myogenin genes expression was enhanced during the muscle lengthening. Vegf and Vegfr‐1 were upregulated following the recession of angiogenesis at the consolidation phase. We conclude that upregulation of VEGF and its receptors by mechanical tension‐stress could be involved in the process of angiogenesis and myogenesis in lengthened muscles. © 2012 Orthopaedic Research Society. Published by Wiley Periodicals, Inc. J Orthop Res 30:1767–1773, 2012
Identification of biomarkers of meat tenderisation and its use for early classification of Asturian beef into fast and late tenderising meat
Authors: Sierra Verónica , Fernández‐Suárez Verónica , Castro Pedro , Osoro Koldo , Vega‐Naredo Ignacio , García‐Macía Marina , Rodríguez‐Colunga Pepa , Coto‐Montes Ana , Oliván Mamen 
Published: April 2012

AbstractBACKGROUND: The objective of this work was to study the post‐mortem evolution of potential biomarkers (µ‐calpain activity and proteolytic profile) of meat tenderisation in bovine longissimus dorsi (LD) muscle from several biotypes coming from two beef breeds (‘Asturiana de los Valles’ and ‘Asturiana de la Montaña’) and showing different levels of muscular hypertrophy (mh/mh, mh/+, + /+).RESULTS: LD samples were taken at 2, 12, 24 and 48 h and 3, 7, 14 and 21 days post‐mortem. The presence of muscular hypertrophy produced a faster rate of pH decline, faster exhaustion of µ‐calpain activity and earlier occurrence of proteolytic changes. Changes in the electrophoretic pattern of some peptides from sarcoplasmic (glyceraldehyde‐3‐phosphate dehydrogenase) and myofibrillar (troponin T and troponin I) muscle extracts within the first 24 h significantly correlated with meat toughness and allowed accurate discrimination of meat products into two groups: (1) fast tenderising meat, coming from mh‐biotypes, and (2) late tenderising meat, from normal (+/+) biotypes.CONCLUSION: Early monitoring (within 24 h after slaughter) of selected biomarkers in LD muscle allowed accurate prediction of ultimate meat toughness and could be used in the meat industry as a tool for early classification of beef into fast and late tenderising meat. Copyright © 2012 Society of Chemical Industry
Nutrient content, in vitro ruminal fermentation characteristics and methane reduction potential of tropical tannin‐containing leaves
Authors: Bhatta Raghavendra , Saravanan Mani , Baruah Luna , Sampath Koratekere T 
Published: April 2012

AbstractBACKGROUND: Plant tannins as rumen modifiers are better than chemicals or antibiotic‐based modifiers since these compounds are natural products which are environmentally friendly and therefore have a better acceptance with regard to feed safety issues. Tropical plants containing phenols such as tannins were found to suppress or eliminate protozoa from the rumen and reduce methane and ammonia production. The screening of these plants is an important step in the identification of new compounds and feed additives which might contribute to mitigate rumen methanogenesis. The present study was carried out to determine the efficacy of tannins from tropical tree leaves for their methane reduction properties.RESULTS: Activity of tannins, as represented by the increase in gas volume with the addition of polyethylene glycol (PEG)‐6000 as a tannin binder (tannin bioassay) was highest in Ficus bengalensis (555%), followed by Azardirachta indica (78.5%). PEG addition did not alter (P > 0.05) methane percentage in Ficus racemosa, Glyricidia maculata, Leucena leucocephala, Morus alba and Semaroba glauca, confirming that tannins in these samples did not affect methanogenesis. The increase (P < 0.05) in protozoa population with PEG was maximal in Ficus religiosa (50), followed by Moringa oleifera (31.2), Azardirachta indica (29.9) and Semaroba glauca (27.5). There was no change (P > 0.05) in the protozoa population in Autocarpus integrifolia, Ficus bengalensis, Jatropha curcus, Morus alba and Sesbania grandiflora, demonstrating that methane reduction observed in these samples per se was not due to defaunation effect of the tannin. The increase in total volatile fatty acid concentration in samples with PEG ranged from 0.6% to > 70%. The highest increase (%) in NH3‐N was recorded in Azardirachta indica (67.4), followed by Ficus mysoriensis (35.7) and Semaroba glauca (32.6) leaves, reflecting strong protein binding properties of tannin.CONCLUSION: The results of our study established that in vitro methanogenesis was not essentially related to the density of protozoa population. Tropical tree leaves containing tannins such as Autocarpus integrifolia, Jatropha curcus and Sesbania grandiflora have the potential to suppress methanogenesis. Therefore tannins contained in these plants could be of interest in the development of new additives in ruminant nutrition. Copyright © 2012 Society of Chemical Industry
Enhancing the polyphenol content of a red‐fleshed Japanese plum (Prunus salicina Lindl.) nectar by incorporating a polyphenol‐rich extract from the skins
Authors: de Beer Dalene , Steyn Naomi , Joubert Elizabeth , Muller Nina 
Published: April 2012

AbstractBACKGROUND: Plum skins are a waste product generated during production of plum juice or pulp. Polyphenols, shown to have various health‐promoting properties, can be recovered from this waste product. Red‐fleshed plum nectar formulations containing plum skin extract in varying amounts were characterised in terms of intensity of sensory attributes, consumer acceptability, colour, polyphenol content and antioxidant activity. Commercial beverages containing red fruits were used as benchmarks.RESULTS: The polyphenolic profile of the plum skin extract was similar to that of the pulp, including anthocyanins, flavonols, flavan‐3‐ols and a phenolic acid. Addition of the extract to plum nectar, which enhanced the colour, polyphenol content and antioxidant capacity, was limited by its negative sensory impact. The formulations were deemed acceptable by consumers, although a decrease in positive sensory attributes (plum flavour, plum aroma and sweetness) and an increase in negative sensory attributes (plant‐like flavour, plant‐like aroma, acidity and astringency) were observed with increasing skin extract content. The formulations compared favourably with commercial beverages in terms of colour total polyphenol content and antioxidant activity.CONCLUSION: Plum skins were successfully used to enhance the functional status of plum nectar. Use of a functional ingredient from plum skins is, therefore, a feasible value‐addition strategy. Copyright © 2012 Society of Chemical Industry
Effects of high hydrostatic pressure on structure and colour of red ginseng (Panax ginseng)
Authors: Ghafoor Kashif , Kim Sun‐Ok , Lee Dong‐Un , Seong Kijun , Park Jiyong 
Published: April 2012

AbstractBACKGROUND: The conventional method of processing ginseng (Panax ginseng) roots into red ginseng involves mainly heating and drying processes. In the present study, this method was modified by using high hydrostatic pressure (HHP) to improve the physicochemical characteristics of red ginseng.RESULTS: The HHP process (600 MPa for 1 min) significantly improved the histological properties of red ginseng by increasing cellular disruption and release of cell contents. The total reducing sugar content was significantly (P < 0.05) higher (increased from 10.67 to 15.25 mg g−1) in red ginseng processed at 600 MPa for 1 min. Similarly, the total free amino acid content also increased significantly (from 2.81 to 7.77 mg g−1). The HHP process resulted in superior and more even colouration and gave an attractive visual appearance to red ginseng. The optical density at 420 nm and Hunter's colour a value (redness) of extracts prepared from red ginseng increased significantly (P < 0.05) with the application of HHP.CONCLUSION: HHP‐processed red ginseng has significantly higher reducing sugar and free amino acid contents together with a more compact cell structure and superior visual quality (brighter red colour). Hence the application of HHP in red ginseng processing can result in ginseng products of improved quality compared with those obtained by the conventional method. Copyright © 2012 Society of Chemical Industry
Outer‐sphere reduction of hexacyanoferrate(III) by enolizable and nonenolizable aldehydes in alkaline medium
Authors: Bera Ashok K. , Pal Biswajit , Sen Gupta Kalyan K. 
Published: April 2012

AbstractOuter‐sphere reduction of hexacyanoferrate(III) by some enolizable/nonenolizable aldehydes (viz., aliphatic, heterocyclic, and aromatic aldehydes) in alkaline medium has been studied spectrophotometrically at λmax = 420 nm. The reactions are first order each in [aldehyde] and [Fe(CN)63−]. The rate increases with an increase in [OH−] in the oxidation of aliphatic and heterocyclic aldehydes, whereas it is independent of [OH−] in the reaction with aromatic aldehydes. The intervention of free radicals in the reaction mixture was carried out using both acrylonitrile and acrylamide scavenger in two different experiments. The kinetic results indicate that the oxidation of benzaldehyde in aqueous medium proceeds at a slower rate than the aliphatic aldehydes (other than formaldehyde) and furfural. The values of third‐order rate constant (k3) at 308 K in the oxidations of some aliphatic aldehydes and furfural follow the order (CH3)2CH > CH3CH2 > CH3 > C4H3O > H. The rate constants correlate with Taft's σ* value, the reaction constant being negative (–9.8). The pseudo–first‐order rate constants in the oxidations of benzaldehyde and substituted benzaldehydes follow the order NO2 > H > Cl > OCH3. The Hammett plot is also linear with a ρ value (0.6488) for meta‐ and para‐substituted benzaldehydes. The kinetic isotope effect for benzaldehyde (kH/kD = 1.93 at 303 K) was obtained. The rate‐determining step is the outer‐sphere formation of Fe(CN)64− and free radicals, which is followed by the rapid oxidation of free radicals by Fe(CN)63− to give products. The kinetic data and hence thermodynamic parameters have been used to distinguish enolizable and nonenolizable aldehydes. An attempt has also been made to correlate kinetic data with hydration equilibrium constants of some aliphatic aldehydes. © 2012 Wiley Periodicals, Inc. Int J Chem Kinet 44: 494–505, 2012
Size‐Controlled Fabrication of Polydiacetylene‐Embedded Microfibers on a Microfluidic Chip
Authors: Yoo Imsung , Song Simon , Yoon Bora , Kim Jong‐Man 
Published: April 2012

AbstractA microfluidic technique was employed to fabricate polydiacetylene (PDA)‐embedded hydrogel microfibers. By taking advantage of calcium ion‐induced insoluble hydrogel formation, supramolecularly assembled diacetylene (DA)‐surfactant complexes were successfully immobilized in the calcium alginate fibers. Thus, instantaneous microfiber formation was observed when the core flow of DA supramolecules‐containing alginate solution met the sheath flow of calcium ions. UV irradiation of the resulting fibers afforded blue colored PDAs, and the formation of a conjugated polymer was confirmed by heat‐induced phase transition and by Raman spectroscopy. By adjusting the core and sheath flow rates, PDA‐embedded hydrogel fibers of various sizes were obtained.
Diabetic renal disease in older people
Authors: Akerman Catherine , Kirk Adam , Hewitt Jonathan 
Published: April 2012

AbstractAs the population ages and the prevalence of diabetes increases, more and more older people will suffer from diabetic complications, including renal disease. There are very few studies of older diabetic people with renal disease and most of our knowledge and treatment base are derived from information generated in younger patients.In older people, blockade of the renin‐angiotensin system seems to be as important as it is in younger people; however, these drugs are often prescribed at suboptimal doses. Further, while glycaemic and blood pressure control is paramount, factors such as cognitive impairment and postural hypotension can make the management of these aspects difficult in older people. Cardiovascular disease is very common in people with chronic renal disease, and thus older people are also likely to benefit from cardiovascular risk factor protection.Estimating renal function in older people can also be less reliable due to reduced muscle mass and less well validated measures of renal function. However, when end‐stage renal disease is established, many treatment options, including renal replacement therapy, are well tolerated and are being increasingly used in older people.This article discusses the evidence and treatments available for older people with diabetic renal disease. Copyright © 2012 John Wiley & Sons.
Renewal of driving licences and long duration insulin‐treated diabetes: a comparison of medical assessment and self‐reporting by drivers
Authors: Rees Simon DR , Browne Andrew , Major Heather G , Frier Brian M 
Published: April 2012

AbstractThe Driver and Vehicle Licensing Agency (DVLA) relies on self‐declaration of a relevant medical condition, such as insulin‐treated diabetes, in determining medical fitness for licensing Group 1 (car or motorcycle) drivers. Problems such as severe hypoglycaemia (requiring the assistance of another person) may lead to revocation of the licence, but may not always be reported.The aim of the present study was to assess the sensitivity and accuracy of medical self‐declaration in drivers who had insulin‐treated diabetes of long duration.The study took place in 2007–08, involving 2779 drivers who had insulin‐treated diabetes for 15 years or more when applying to renew their Group 1 licence. The driver's self‐declaration was compared with the assessment made independently by their doctor as a medical report. Responses were analysed to assess risk of severe hypoglycaemia and presence of impaired awareness of hypoglycaemia (IAH); the accuracy and sensitivity of self‐declarations were evaluated.Overall, self‐declarations of 293 drivers (10.5%) were inconsistent with their doctors' reporting of recorded episodes of severe hypoglycaemia or IAH. This inconsistency was greatest in those treated with insulin for 20 years or more and in older drivers aged over 49 years. Detailed examination of these 293 cases with inconsistent declarations resulted in 25 drivers (8.5% of this subgroup) being refused a licence.One in 10 drivers with insulin‐treated diabetes of long duration (10.5%) had returned inaccurate self‐reports, resulting in 25 (8.5% of this group) having their licence refused. This resulted in a review of the process of licence renewal for those with insulin‐treated diabetes. Copyright © 2012 John Wiley & Sons.