bluuebunny/crossref_metadata_2025_split huggingface dataset:
Radioiodinated analogs of xylamine: N‐(2‐chloroethyl)‐N‐ethyl‐2‐[125I]iodobenzylamine and N,N‐diethyl‐2‐[125I]iodobenzylamine as potential tools for monoamine uptake exploration by spect
Authors: Branger C. , Garreau L. , Frangin Y. , Chalon S. , Dubois P. , Dognon A.‐M. , Ombetta‐Goka J.‐E. , Besnard J.‐C. , Guilloteau D. 
Published: October 2006

AbstractIn order to improve the scintigraphy and radiotherapy of neuroendocrine tumors we synthesized two radioiodinated benzylamines [N‐(2‐chloroethyl)‐N‐ethyl‐2‐[125I]iodobenzylamine and N,N‐diethyl‐2‐[125I]iodobenzylamine], analogs of xylamine [N‐(2‐chloroethyl)‐N‐ethyl‐2‐methylbenzylamine]. Xylamine is an irreversible inhibitor of uptake and accumulation of noradrenaline. The two unlabelled iodinated derivatives [N‐(2‐chloroethyl)‐N‐ethyl‐2‐iodobenzylamine and N,N‐diethyl‐2‐iodobenzylamine] were synthesized, purified and checked by HPLC, NMR and mass spectrography. Their affinity for the noradrenaline transporter was determined in vitro on rat brain membrane homogenates with [3H]nisoxetine. Radioiodination was performed by iodide for bromide nucleophilic exchange from brominated precursors. The N,N‐diethyl‐2‐[125I]iodobenzylamine was obtained directly from N,N‐diethyl‐2‐bromobenzylamine. Radiosynthesis of N‐(2‐chloroethyl)‐N‐ethyl‐2‐[125I]iodobenzylamine required three steps. A new brominated precursor [N‐ethyl‐N‐(2‐bromobenzyl)glycine ethyl ester] which was stable for radiolabelling and suitable for reduction to N‐(2‐hydroxyethyl)‐N‐cthyl‐2‐[125I]iodobenzylamine was synthesized. N‐(2‐Hydroxyethyl)‐N‐ethyl‐2‐[125I]iodobenzylamine was converted to N‐(2‐chloroethyl)‐N‐ethyl‐2‐[125I]iodobenzylamine in the presence of an excess of thionyl chloride. Radioiodinated derivatives were purified and checked by HPLC.
N. C. A. radioiodination of idoxifene
Authors: Trivedi Mahendra , Potter Gerrard , Hammersley Peter , Carnochan Paul , Young Helen , Jarman Michael , Ott Robert 
Published: October 2006

AbstractWe describe a method for n.c.a. radioiodination of pyrrolidino tamoxifen (Idoxifene) based on the electrophilic destannylation of tributylstannyl pyrrolidino tamoxifen. The methods of separation using preparative tlc and HPLC give >95% radiochemical purity and >70% recovery.
Synthesis of 1,2[3H]‐1,2‐epoxy analogue of fructose‐6P, an affinity label of escherichia coli glucosamine‐6P synthase
Authors: Leriche Caroline , René Loïc , Derouet Florence , Rousseau Bernard , Badet Bernard 
Published: October 2006

Abstract1,2‐anhydroglucitol‐6P, a known inhibitor of glucose‐6P isomerase, behaved as a fructose‐6P site‐directed irreversible inhibitor of bacterial glucosamine‐6P synthase. The lack of reproducibility of the aldolase‐mediated condensation of dihydroxyacetone phosphate and glycidaldehyde followed by borohydride reduction previously described prompted us to develop a chemical route to this compound and its radiolabelled counterpart. The compound was synthesized in 13 steps from D‐arabinose with a 6% overall yield. Tritium introduction was performed at step 11 (3 → 4) allowing isolation of the title compound of high specific radioactivity.
Synthesis of Δ4‐3‐oxo‐steroids labelled specifically at the 6β ‐position
Authors: Toft P. , Liston A. J. , Viau A. Y. 
Published: October 2006

Abstract[6β‐2H] Testosterone and [6β‐3H] Testosterone were each synthesized in good yield in three steps: Treatment of 5a, 6a‐ epoxy‐3, 3‐ethylene‐dioxyandrostan ‐17β‐ol with labelled lithium aluminum hydride is followed by deacetalation and dehydration under carefully controlled basic conditions.
The biosynthesis of 13C labeled starch granules as a source of uniformly labeled 13C D‐glucose
Authors: Buchholz J. R. , Christenson C. W. , Eakin R. T. , Fowler E. 
Published: October 2006

AbstractA potato plant has been grown in a closed chamber with CO2 enriched to a level of 31 at. % in 13C as the sole source of carbon. In 80 days the plant produced 1,684 g of tubers labeled with 29 at. % 13C. of the carbon fixed by the potato plant appromixately 70% was found in the tubers while 30% was found in the tops and roots. Recovered starch granules constituted 10% of the fresh weight of these tubers. A 16% yield of glucose was obtained, based on all of the carbon dioxide used. Distribution of the 13C label among the six species of carbon atoms in strach appears to be nearly uniform. The plant and tubers were indistinguishable from those grown on normal isotopic CO2 indicating no gross isotope effect at this level of 13C enrichement.
Substances naturelles marquees au cardopn14: Synthese de l'acide withranilioue (carboxylc 14C), precurseur bio‐sehtioe de l'ellipticine
Authors: Bac Nguyen Van , Herbert Michel , Pichat Louis , Dat‐Xuong Nguyen 
Published: October 2006

AbstractLa carbonisation du lithien du bromo‐2 acétanilide ne donne qu'sun faible rendement en acide anthranilique.La carbonisation du promure d'o‐chlorphénylmaanésium pur 14CO2 conduit à l'acide o‐chlorobenzoique ( carboxyle 14c ) dont l'a‐mination deshalogénante fournit l'acide anthranilique ( carboxyle 14C. ) avec un rendement radioactif global de 26% par rapport à Ba14CO3 une activité spécifique de 48 mCi/MM.
Arzneipflanzen, die unverstandene Naturapotheke
Authors: Müller‐Limmroth Wolf 
Published: October 2006

Abstract„Muß ich dies Körbchen bier voll Kraut und Blumen lesen: voll Pflanzen gift'ger Art und diensam zum Genesen. An vielen Tugenden sind viele drunter reich, ganz ohne Wert nicht eins, doch keins dem andern gleich. Oh, groß Kräfte sind's, weiß man sie recht zu pflegen, die Pflanzen, Krauter, Stein' in ihrem Innern hegen.
Serum insulin‐like growth factor II levels in normal adolescents and those with insulin dependent diabetes mellitus
Authors: Acerini C. L. , Clayton K. L. , Hintz R. , Baker B. , Watts A. , Holly J. M. P. , Dunger D. B. 
Published: October 2006

SummaryOBJECTIVE Unlike IGF‐I and its principal binding proteins, data regarding IGF‐II levels have not been well defined in normal subjects and those with insulin‐dependent diabetes mellitus (IDDM). We have therefore measured IGF‐II, as well as IGF‐I, and IGFBP‐3, levels In a large cohort of subjects with IDDM and in age/sex matched controls.PATIENTS One hundred and fourteen patients with IDDM (57 males, 57 females) and 89 control subjects (49 males, 40 females).MEASUREMENTS Random blood samples were obtained from each subject for the measurement of IGF‐II, IGF‐I and IGFBP‐3 levels.RESULTS Mean values of IGF‐II (±SEM) were 630 (±27.8) μg/l and 646 (±32.3) μg/l in female and male controls, compared to 569 (±23.3) μg/l and 623.3 (±28.1) μg/l in female and male diabetics respectively. IGF‐II levels did not differ significantly between the sexes or show any change with transition through puberty in either control or diabetic groups. In contrast, IGF‐I levels increased through puberty peaking at stages 3–5 in controls (P < 0.001) and G4–5 (P= 0.002) in diabetic males but not females. IGF‐I levels in all diabetics were generally lower than in controls, differences reaching significance at G4–5 in males (P= 0.002) and B5 in females (P= 0.002). IGFBP‐3 levels did not show any variation with puberty stage in diabetics, in contrast to controls where levels increased, peaking at G4–5 in males (P= 0.001) and B3 in females. IGFBP‐3 levels were lower in diabetics of both sexes and at all stages compared to controls (P range 0.047 to < 0.001). Multiple regression analysis revealed significant correlations between IGF‐II and IGFBP‐3 (F= 20.1, P= < 0.001) and reaffirmed previously observed associations for IGF‐I and IGFBP‐3. The sum of IGF‐I and IGF‐II (expressed as nmol/l) correlated with IGFBP3; r= 0.47 in controls and 0.60 in diabetics.CONCLUSIONS Insulin‐dependent diabetes mellitus is not associated with any significant changes in IGF‐II levels during puberty. The binding of IGFBP‐3 for both IGF‐I and IGF‐II is unaltered by insulin‐dependent diabetes mellitus.
Pharmacokinetics and pharmacodynamics of subcutaneous testosterone implants in hypogonadal men
Authors: Jockenhövel F. , Vogel E. , Kreutzer M. , Relnhardt W. , Lederbogen S. , Reinwein D. 
Published: October 2006

SummaryOBJECTIVE There are advantages and disadvantages with all of the presently available types of testosterone replacement for hypogonadal men. We performed this investigation to establish detailed data about the pharmacokinetics, pharmacodynamics, feasibility and side‐effects of subcutaneously implanted testosterone (T) pellets.DESIGN AND MEASUREMENT In a single‐dose, open‐label, non‐randomized study, 6 T‐pellets, each containing 200 mg of fused crystalline T, were Implanted in the subdermal fat tissue of the lower abdominal wall of 14 hypogonadal men. Blood samples for determination of T, LH, FSH, 5α‐dihydrotestosterone (DHT), sex hormone binding globulin (SHBG) and oestradiol (E2) were obtained at 0, 0.5, 1, 2, 4, 8, 12, 24, 36, 48 hours and on day 21 after implantation and then every 3 weeks until day 189, and on days 246 and 300 during follow‐up. In another 36 hypogonadal men the feasibility and side‐effects of T‐pellets were evaluated.PATIENTS Fourteen patients participated in the detailed pharmacokinetic study and another 36 patients in the assessment of feasibility and side‐effects. All patients (age range 18–61 years) suffered from primary or secondary hypogonadism (T < 3.6nmol/l).RESULTS The pharmacokinetic study in 14 hypogonadal men revealed an initial short‐lived burst release of T with a peak concentration of 49.0 ± 3.7 nmol/l at 0–5 ± 0.13 days which was followed by a stable plateau lasting until day 63 (day 2, 35.2 ± 2.3; day 63, 34.8 ± 2.6 nmol/l). Thereafter serum T gradually declined and was close to baseline concentrations on day 300. Apparent terminal elimination half‐life (t1/2) was 70.8 ± 10.7 days and apparent mean residence time 87.0 ± 45 days. On average, serum T was below 10 nmol/l after 180 days. Absorption of T followed a zero‐order release kinetic with an absorption half‐time of 74.7 days (95% confidence Interval: 71.1–78.5) and was almost complete by day 189 (95.9 ± 0.84%). Serum DHT and E2 were significantly elevated from day 21 to day 105 and correlated significantly with T (DHT, r = 0–65, P < 00001, E2, r = 067, P < 0.0001). SHBG was significantly decreased from day 21 to day 168. In 6 men with primary hypogonadism T suppressed LH and FSH to the eugonadal range from day 21 to 126 and 42 to 105, respectively, with nadirs occurring at day 84 (LH) and day 63 (FSH). LH and FSH were highly inversely correlated with T (r=−0.47 and −0.57).The only side‐effect observed during 112 implantations in the total group of 50 men were 6 local infections (5.4%) leading to extrusion of 5 pellets In 3 men. When given the choice, all patients except one preferred T‐pellets to their previous T medication for permanent substitution therapy.CONCLUSION T‐pellets are the androgen formulation with the longest biological action and strongest pharmacodynamic efficacy in terms of gonadotrophin suppression. The pharmacokinetic features are advantageous compared to other T preparations and the patient acceptance is high.
Fulminant methicillin‐sensitive Staphylococcus aureus infection in a healthy adolescent, highlighting ‘Panton–Valentine leucocidin syndrome’
Authors: Swaminathan A. , Massasso D. , Gotis‐Graham I. , Gosbell I. 
Published: October 2006

AbstractA 14‐year‐old immunocompetent adolescent presented systemically unwell with left knee septic arthritis. Within several days, disseminated bone and soft tissue collections became evident, associated with deep venous thrombosis and pulmonary involvement. Methicillin‐sensitive Staphylococcus aureus was isolated, harbouring Panton–Valentine leucocidin genes. Aggressive antibiotic and surgical therapies eventually lead to recovery. Intrafamilial spread of the pathogenic isolate was shown by household screening. This presentation is consistent with ’PVL Syndrome’ and is typical of severe S. aureus infection emerging in young populations globally.
Flow‐mediated dilatation in overweight and obese women with polycystic ovary syndrome
Authors: Brinkworth GD , Noakes M , Moran LJ , Norman R , Clifton PM 
Published: October 2006

Objective  There remains a large degree of disagreement about the association of polycystic ovary syndrome (PCOS) with impaired endothelial dysfunction and cardiovascular disease (CVD) risk. The purpose of this study was to determine whether overweight and obese women with PCOS have impaired endothelial function compared with weight‐matched controls without PCOS and whether endothelial function is associated with cardiovascular risk markers and hormonal parameters.Design  Cross‐sectional analysis.Setting  An outpatient trial at the Commonwealth Scientific Industrial Research Organisation Clinical Research Unit.Population  Overweight and obese women with PCOS (n= 12) and weight‐matched controls without PCOS (n= 10).Methods  Endothelial function, cardiovascular risk markers and hormonal parameters were assessed in the patients.Main outcome measures  Endothelial function was assessed by flow‐mediated dilatation (FMD) of the brachial artery using high‐resolution ultrasound. Lipid profile, fasting insulin level, glucose level, insulin resistance, C‐reactive protein level, folate level, Vitamin B12 level and hormonal parameters.Results  Women with PCOS had significantly higher testosterone levels (P < 0.001) and free androgen index (P= 0.006) compared with the controls without PCOS. Both groups were normoinsulinaemic, and there were no significant differences in any of the markers of CVD between women with and without PCOS. Furthermore, FMD was similar in both groups (PCOS 6.1 ± 1.2% versus control 5.6 ± 1.0%, P= 0.77).Conclusions  Compared with a group of weight‐matched women with similar metabolic profiles, normoinsulinemic, overweight and obese women with PCOS did not show any greater impairment in endothelial function assessed by FMD. A normoinsulinemic phenotype of PCOS with low metabolic risk factors may reduce the risk of endothelial dysfunction in overweight and obese women with this syndrome. Further studies are required that directly compare FMD in normoinsulinemic and hyperinsulinaemic women with PCOS.
Location of resistance factors in the leaves of potato and wild tuber‐bearing Solanum species to the aphid Myzus persicae
Authors: Alvarez A. E. , Tjallingii W. F. , Garzo E. , Vleeshouwers V. , Dicke M. , Vosman B. 
Published: October 2006

AbstractAnalysis of electrically recorded feeding behaviour of aphids was combined with colony‐development tests to search for sources of resistance to Myzus persicae (Sulzer) (Homoptera: Aphididae) in tuber‐bearing Solanum species (Solanaceae), aiming at a reduction of potato leaf roll virus (PLRV) transmission. Twenty genotypes, originating from 14 gene bank accessions, representing 13 wild tuber‐bearing Solanum spp., three Solanum tuberosum L. (potato) cultivars, and one S. tuberosum breeding line, were selected. Colony‐development tests were carried out in no‐choice experiments by placing adult aphids on plants of each genotype and counting numbers of nymphs and adults on young plants after 8 and 15 days, and on flowering plants after 14 and 30 days. Large differences were observed among genotypes: some developed small colonies and others developed large ones. Also, in a few genotypes, resistance in mature plants was different for leaves of different ages; young leaves were resistant to aphids whereas old senescent leaves were susceptible. The electrical penetration graph (DC‐EPG system) technique was used to study aphid feeding behaviour on each Solanum genotype for 6 h. Electrical penetration graph (EPG) results also showed large differences among the genotypes, indicating resistance at the leaf surface and at three different levels of plant tissue (epidermis, mesophyll, and phloem). Therefore, it was concluded that different mechanisms of resistance to M. persicae exist among the genotypes analysed. EPGs recorded from aphids on Solanum berthaultii Hawkes and Solanum tarijense Hawkes with and without glandular trichomes showed that strong surface resistance can bias EPG parameters associated with resistance located in deeper tissues. Experimental evidence is presented that the resistance to aphids in the genotypes with glandular trichomes strongly depends on these morphological structures.
Characterization of Membrane Association Domains within the
Tomato Ringspot Nepovirus
X2 Protein, an Endoplasmic Reticulum-Targeted Polytopic MembraneProtein
Authors: Zhang Guangzhi , Sanfaçon Hélène 
Published: October 2006

ABSTRACT

Replication
of nepoviruses (family
Comoviridae
) occurs in association with
endoplasmic reticulum (ER)-derived membranes. We have previously shown
that the putative nucleoside triphosphate-binding protein (NTB) of
Tomato ringspot nepovirus
is an integral membrane protein with
two ER-targeting sequences and have suggested that it anchors the viral
replication complex (VRC) to the membranes. A second highly hydrophobic
protein domain (X2) is located immediately upstream of the NTB domain
in the RNA1-encoded polyprotein. X2 shares conserved sequence motifs
with the comovirus 32-kDa protein, an ER-targeted protein implicated in
VRC assembly. In this study, we examined the ability of X2 to associate
with intracellular membranes. The X2 protein was fused to the green
fluorescent protein and expressed in
Nicotiana benthamiana
by
agroinfiltration. Confocal microscopy and membrane flotation
experiments suggested that X2 is targeted to ER membranes. Mutagenesis
studies revealed that X2 contains multiple ER-targeting domains,
including two C-terminal transmembrane helices and a less-well-defined
domain further upstream. To investigate the topology of the protein in
the membrane, in vitro glycosylation assays were conducted using X2
derivatives that contained N-glycosylation sites introduced at the N or
C termini of the protein. The results led us to propose a topological
model for X2 in which the protein traverses the membrane three times,
with the N terminus oriented in the lumen and the C terminus exposed to
the cytoplasmic face. Taken together, our results indicate that X2 is
an ER-targeted polytopic membrane protein and raises the possibility
that it acts as a second membrane anchor for the
VRC.
Pathogenesis of a Genogroup II Human Norovirus in Gnotobiotic Pigs
Authors: Cheetham Sonia , Souza Menira , Meulia Tea , Grimes Sheila , Han Myung Guk , Saif Linda J. 
Published: October 2006

ABSTRACT

We
evaluated the gnotobiotic (Gn) pig as a model to study the pathogenesis
of human norovirus (HuNoV) and to determine the target cells for viral
replication. Sixty-five Gn pigs were inoculated with fecal filtrates of
the NoV/GII/4/HS66/2001/US strain or with pig-passaged intestinal
contents (IC) and euthanized acutely (
n
= 43) or after
convalescence (
n
= 22). Age-matched Gn piglets
(
n
= 14) served as mock-inoculated controls.
Seventy-four percent (48/65) of the inoculated animals developed mild
diarrhea compared to 0 of 14 controls. Pigs from postinoculation days
(PID) 1 to 4 tested positive for HuNoV by reverse
transcription-PCR of rectal swab fluids (29/65) and IC
(9/43) and by antigen (Ag) enzyme-linked immunosorbent assay (ELISA)
using antiserum to virus-like particles of HuNoV GII/4. No
control pigs were positive. Histopathologic examination showed mild
lesions in the proximal small intestine of only one pig (1/7).
Seroconversion after PID 21 was detected by antibody ELISA in 13 of 22
virus-inoculated pigs (titers, 1:20 to 1:200) but not in controls.
Immunofluorescent microscopy using a monoclonal antibody to HuNoV GII
capsid revealed patchy infection of duodenal and jejunal enterocytes of
18 of 31 HuNoV-inoculated pigs with a few stained cells in the ileum
and no immunofluorescence (IF) in mock-inoculated controls.
Immunofluorescent detection of the viral nonstructural N-terminal
protein antigen in enterocytes confirmed translation. Transmission
electron microscopy of intestines from HuNoV-inoculated pigs showed
disrupted enterocytes, with cytoplasmic membrane vesicles containing
calicivirus-like particles of 25 to 40 nm in diameter. In summary,
serial passage of HuNoV in pigs, with occurrence of mild diarrhea and
shedding, and immunofluorescent detection of the HuNoV structural and
nonstructural proteins in enterocytes confirm HuNoV replication in Gn
pigs.
At Least 50% of Human-Specific HERV-K (HML-2) Long Terminal Repeats Serve In Vivo as Active Promoters for Host Nonrepetitive DNA Transcription
Authors: Buzdin Anton , Kovalskaya-Alexandrova Elena , Gogvadze Elena , Sverdlov Eugene 
Published: October 2006

ABSTRACT
We report the first genome-wide comparison of in vivo promoter activities of a group of human-specific endogenous retroviruses in healthy and cancerous germ line tissues. To this end, we employed a recently developed technique termed genomic repeat expression monitoring. We found that at least 50% of human-specific long terminal repeats (LTRs) possessed promoter activity, and many of them were up- or downregulated in a seminoma. Individual LTRs were expressed at markedly different levels, ranging from ∼0.001 to ∼3% of the housekeeping beta-actin gene transcript level. We demonstrated that the main factors affecting the LTR promoter activity were the LTR type (5′-proviral, 3′ proviral, or solitary) and position with regard to genes. The averaged promoter strengths of solitary and 3′-proviral LTRs were almost identical in both tissues, whereas 5′-proviral LTRs displayed two- to fivefold higher promoter activities. The relative content of promoter-active LTRs in gene-rich regions was significantly higher than that in gene-poor loci. This content was maximal in those regions where LTRs “overlapped” readthrough transcripts. Although many promoter-active LTRs were mapped near known genes, no clear-cut correlation was observed between transcriptional activities of genes and neighboring LTRs. Our data also suggest a selective suppression of transcription for LTRs located in gene introns.
Viral and Cellular Determinants of the Hepatitis C Virus Envelope-Heparan SulfateInteraction
Authors: Barth Heidi , Schnober Eva K. , Zhang Fuming , Linhardt Robert J. , Depla Erik , Boson Bertrand , Cosset Francois-Loic , Patel Arvind H. , Blum Hubert E. , Baumert Thomas F. 
Published: October 2006

ABSTRACT

Cellular
binding and entry of hepatitis C virus (HCV) are the first steps of
viral infection and represent a major target for antiviral antibodies
and novel therapeutic strategies. We have recently demonstrated that
heparan sulfate (HS) plays a key role in the binding of HCV envelope
glycoprotein E2 to target cells (Barth et al., J. Biol. Chem.
278:
41003-41012, 2003). In this study, we characterized
the HCV-HS interaction and analyzed its inhibition by antiviral host
immune responses. Using recombinant envelope glycoproteins, virus-like
particles, and HCV pseudoparticles as model systems for the early steps
of viral infection, we mapped viral and cellular determinants of HCV-HS
interaction. HCV-HS binding required a specific HS structure that
included N-sulfo groups and a minimum of 10 to 14 saccharide subunits.
HCV envelope binding to HS was mediated by four viral epitopes
overlapping the E2 hypervariable region 1 and E2-CD81 binding domains.
In functional studies using HCV pseudoparticles, we demonstrate that
HCV binding and entry are specifically inhibited by highly sulfated HS.
Finally, HCV-HS binding was markedly inhibited by antiviral antibodies
derived from HCV-infected individuals. In conclusion, our results
demonstrate that binding of the viral envelope to a specific HS
configuration represents an important step for the initiation of viral
infection and is a target of antiviral host immune responses in vivo.
Mapping of viral and cellular determinants of HCV-HS interaction sets
the stage for the development of novel HS-based antiviral strategies
targeting viral attachment and
entry.