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2.
J Sep Sci ; 44(7): 1391-1403, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-33470534

RESUMO

Rauvolfia vomitoria is widely distributed in the tropical regions of Africa and Asia, and has been used in traditional folk medicine in China. Indole alkaloids were found to be major bioactive components, while the effects of diabetes mellitus on the pharmacokinetic parameters of the components have not been reflected in vivo. In this study, an efficient and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for the simultaneous determination of five ingredients of R. vomitoria in rats. Detection was implemented in multiple-reaction-monitoring mode with an electrospray positive-ionization source. Validation parameters were all in accordance with the current criterion. The established method was effectively employed to compare the pharmacokinetic behaviors of five alkaloids (reserpine, yohimbine, ajmaline, ajmalicine, and serpentine) between normal and type 2 diabetic rats. The single-dose pharmacokinetic parameters of the five alkaloids were determined in normal and diabetic rats after oral administration of 100 and 200 mg/kg body weight. The results indicated that diabetes mellitus significantly altered the pharmacokinetic characteristics of yohimbine, ajmaline, and ajmalicine after oral administration in rats. This is an attempt to provide some evidence for clinicians that may serve as a guide for the use of antidiabetic medicine in clinical practice.

3.
PLoS One ; 15(9): e0238179, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32881902

RESUMO

Carotenoid cleavage dioxygenase (CCD), a key enzyme in carotenoid metabolism, cleaves carotenoids to form apo-carotenoids, which play a major role in plant growth and stress responses. CCD genes had not previously been systematically characterized in Brassica napus (rapeseed), an important oil crop worldwide. In this study, we identified 30 BnCCD genes and classified them into nine subgroups based on a phylogenetic analysis. We identified the chromosomal locations, gene structures, and cis-promoter elements of each of these genes and performed a selection pressure analysis to identify residues under selection. Furthermore, we determined the subcellular localization, physicochemical properties, and conserved protein motifs of the encoded proteins. All the CCD proteins contained a retinal pigment epithelial membrane protein (RPE65) domain. qRT-PCR analysis of expression of 20 representative BnCCD genes in 16 tissues of the B. napus cultivar Zhong Shuang 11 ('ZS11') revealed that members of the BnCCD gene family possess a broad range of expression patterns. This work lays the foundation for functional studies of the BnCCD gene family.


Assuntos
Brassica napus/enzimologia , Dioxigenases/genética , Genoma de Planta , Proteínas de Plantas/genética , Arabidopsis/enzimologia , Brassica napus/genética , Carotenoides/metabolismo , Mapeamento Cromossômico , Dioxigenases/classificação , Dioxigenases/metabolismo , Regulação da Expressão Gênica de Plantas , Família Multigênica , Filogenia , Proteínas de Plantas/classificação , Proteínas de Plantas/metabolismo , Regiões Promotoras Genéticas
5.
BMC Pediatr ; 20(1): 210, 2020 05 12.
Artigo em Inglês | MEDLINE | ID: mdl-32398036

RESUMO

BACKGROUND: The infrared tympanic thermometer (IRTT) is a popular method for temperature screening in children, but it has been debated for the low accuracy and reproducibility compared with other measurements. This study was aimed to identify and quantify studies reporting the diagnostic accuracy of the new generation IRTT in children and to compare the sensitivity and specificity of IRTT under different cutoffs and give the optimal cutoff. METHODS: Articles were derived from a systematic search in PubMed, Web of Science Core Collection, and Embase, and were assessed for internal validity by the Quality Assessment of Diagnostic Accuracy Studies-2 (QUADAS-2). The figure of risk of bias was created by Review Manager 5.3 and data were synthesized by MetaDisc 1.4. RESULTS: Twelve diagnostic studies, involving 4639 pediatric patients, were included. The cut-offs varied from 37.0 °C to 38.0 °C among these studies. The cut-off 37.8 °C was with the highest sROC AUC (0.97) and Youden Index (0.83) and was deemed to be the optimal cutoff. CONCLUSION: The optimal cutoff for infrared tympanic thermometers is 37.8 °C. New Generation Tympanic Thermometry is with high diagnostic accuracy in pediatric patients and can be an alternative for fever screening in children.

6.
Clin Gastroenterol Hepatol ; 18(7): 1618-1625.e7, 2020 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31712074

RESUMO

BACKGROUND & AIMS: The EncephalApp Stroop test is a high-sensitivity but low-specificity test that has been used to identify patients with covert hepatic encephalopathy (CHE). We aimed to develop a new strategy to detect CHE, combining EncephalApp Stroop test score with scores from subtests of the psychometric hepatic encephalopathy scoring system (PHES). METHODS: We performed a survey of 569 adult volunteers (229 men) in 9 communities in Shanghai, China, administering the EncephalApp Stroop test to determine the range of scores in the general population. Data from the standard PHES, including the number connection test-A, number connection test-B (NCT-B), line tracing test, serial dotting test (SDT), and digit symbol test, were used as the reference standard for diagnosis of CHE. A combination of the EncephalApp Stroop with subtests of the PHES was used to establish a new strategy for CHE diagnosis. We validated our findings using data from 160 patients with cirrhosis from 5 centers China. RESULTS: We determined the range of EncephalApp Stroop test scores for the volunteers of different decades of age, education levels, and sexes. Age, education level, and sex were independently associated with EncephalApp Stroop test scores. A combination of scores from the EncephalApp Stroop test, the NCT-B, and the SDT identified patients with CHE with the highest level of accuracy, when the standard PHES was used as the reference standard. A combination of scores of 187 sec for the EncephalApp Stroop test and below -1 for the NCT-B or below -1 for the SDT identified patients with CHE with an area under the curve (AUC) of 0.86, 81.0% sensitivity, and 91.9% specificity, and 87.5% accuracy. In the validation cohort, these cutoff scores identified patients with CHE with an AUC of 0.88, 97.1% sensitivity, 79.3% specificity, and 86.9% accuracy. The average time to calculate this score was 374±140 sec, compared 424±115 sec for the entire PHES. CONCLUSION: Scores from the EncephalApp Stroop test, NCT-B, and SDT identify patients with CHE with approximately 87% accuracy, and in a much shorter time than the standard PHES. This score combination could be a valid and convenient method for identifying patients with CHE. chictr.org.cn number, ChiCTR-EDC-17012007, ChiCTR1800019954.

7.
Plant Physiol ; 182(1): 332-344, 2020 01.
Artigo em Inglês | MEDLINE | ID: mdl-31591151

RESUMO

N 6 -methyladenosine (m6A) is the most abundant modification of eukaryotic mRNA. Although m6A has been demonstrated to affect almost all aspects of RNA metabolism, its global contribution to the post-transcriptional balancing of translational efficiency remains elusive in plants. In this study, we performed a parallel analysis of the transcriptome-wide mRNA m6A distribution and polysome profiling in two maize (Zea mays) inbred lines to assess the global correlation of m6A modification with translational status. m6A sites are widely distributed in thousands of protein-coding genes, confined to a consensus motif and primarily enriched in the 3' untranslated regions, and highly coordinated with alternative polyadenylation usage, suggesting a role of m6A modification in regulating alternative polyadenylation site choice. More importantly, we identified that the m6A modification shows multifaceted correlations with the translational status depending on its strength and genic location. Moreover, we observed a substantial intraspecies variation in m6A modification, and this natural variation was shown to be partly driven by gene-specific expression and alternative splicing. Together, these findings provide an invaluable resource for ascertaining transcripts that are subject to m6A modification in maize and pave the way to a better understanding of natural m6A variation in mediating gene expression regulation.

8.
Proc Math Phys Eng Sci ; 475(2228): 20180812, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31534417

RESUMO

Tensegrities, consisting of axially pre-compressed bars and pre-stretched strings, hold broad applications in the design of, for instance, architectures, soft robotics and metamaterials. In this paper, we propose an enumeration-screening method to design planar tensegrities of simple polygonal shapes. In such a polygonal tensegrity, the strings are joined pair-wise to form a simple polygon (a planar shape consisting of straight, non-intersecting line segments) and only one bar is added at each node. The total number of simple polygonal tensegrities designed by this scheme increases exponentially with the number of bars. Moreover, we demonstrate that each of these designed topologies can produce a self-equilibrated and stable tensegrity configuration. This work helps understand the topological features of simple polygonal tensegrities, which can be used as elementary cells to design some novel two- and three-dimensional tensegrity structures.

9.
Soft Matter ; 15(42): 8441-8449, 2019 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-31465066

RESUMO

Epithelial tissues can become overcrowded during proliferation and growth, in which case excessive cells need to be constantly removed. Here, we employed a vertex dynamics model to explore the microscopic mechanisms that govern homeostasis in an overcrowded monolayer of epithelial cells. It is demonstrated that the monolayer under mechanical compression can maintain a constant cell density and an optimal stress level through cell extrusion. Interestingly, cells are always extruded at sites of stress singularity in the monolayer, which may be spontaneously generated through random movements of cell groups near the extruding cells, and the fluctuation of protein molecules aggregating along the cell surface facilitates the restoration of the monolayer to its equilibrium state. Our results provide a foundation to interpret recent experiments as well as shed light on the mechanisms that underlie epithelial development and maintenance.


Assuntos
Células Epiteliais/metabolismo , Estresse Mecânico , Citoesqueleto de Actina/química , Citoesqueleto de Actina/metabolismo , Membrana Celular/química , Membrana Celular/metabolismo , Movimento Celular , Simulação por Computador , Células Epiteliais/química , Modelos Biológicos , Termodinâmica
10.
J Dig Dis ; 20(3): 127-134, 2019 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-30714350

RESUMO

OBJECTIVE: Contrast-enhanced harmonic endoscopic ultrasonography (CH-EUS) is a valuable device to diagnose and determine the malignant potential of gastrointestinal stromal tumors (GIST) as early as possible when making clinical therapeutic decisions. This study aimed to estimate the ability of CH-EUS to discriminate between GIST and benign submucosal lesions (SML) and to predict their malignant potential. METHODS: PubMed, MEDLINE, EMBASE, the Web of Science, and Cochrane Central Register of Controlled Trials databases were screened. Using the data provided in the literatures, 2 × 2 tables were constructed to obtain the pooled sensitivity, specificity, positive likelihood ratio, and negative likelihood ratio. A receiver operating characteristic (ROC) curve was generated and the area under the ROC curve (AUROC) was calculated. RESULTS: Four studies with a total of 187 patients were identified to evaluate the value of CH-EUS in discriminating between GIST and benign SML. The pooled sensitivity, specificity, and AUROC were 89% (95% CI 0.82-0.93), 82% (95% CI 0.66-0.92), and 0.89, respectively. Five studies including 143 patients were analyzed to assess the accuracy of CH-EUS in determining the malignant potential of GIST. The pooled sensitivity, specificity, and AUROC curve of CH-EUS were 96% (95% CI 0.90-0.99), 53% (95% CI 0.40-0.66), and 0.92, respectively. CONCLUSIONS: CH-EUS is a safe, noninvasive method that can distinguish between GIST and benign subepithelial lesions and to predict their malignant potential to a certain extent. Large-scale, multicenter prospective studies are needed in the future.


Assuntos
Endossonografia/métodos , Tumores do Estroma Gastrointestinal/diagnóstico por imagem , Meios de Contraste , Diagnóstico Diferencial , Humanos , Valor Preditivo dos Testes
11.
Chin J Integr Med ; 25(11): 831-836, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30484019

RESUMO

OBJECTIVE: To develop an improved version of the Quality-of-Life Assessment instrument for Lung Cancer Patients Based on Traditional Chinese Medicine (QLASTCM-Lu) and to evaluate its psychometric property. METHODS: The structured group method and the theory in developing rating scale were employed to revise the preliminary scale. The psychometric property (reliability, validity, and responsiveness) of the established QLASTCM-Lu (modified) were evaluated by quality of life data measured in 100 lung cancer patients. Statistical analyses were made accordingly by way of correlation analysis, factor analysis and paired t-test. RESULTS: The internal consistency reliability of the overall scale and all domains was from 0.80 to 0.94. Correlation and factor analyses demonstrated that the scale was good in construct validity. The criterion validity was formed with European Organization for Research and Treatment of Cancer-Quality of Life Questionnaire-Lung Cancer (EORTC QLQ-LC43) as the criterion. Statistically significant changes were found apart from such domain as "mental condition" and "social function", with the standardized response means being close to those of QLQ-LC43. CONCLUSION: QLASTCM-Lu (modified) could be used to measure the quality of life of lung cancer patients with good reliability, validity and a certain degree of responsiveness.


Assuntos
Neoplasias Pulmonares/psicologia , Medicina Tradicional Chinesa/métodos , Psicometria/métodos , Qualidade de Vida , Inquéritos e Questionários , Adulto , Idoso , Emoções , Feminino , Humanos , Neoplasias Pulmonares/diagnóstico , Neoplasias Pulmonares/epidemiologia , Masculino , Pessoa de Meia-Idade , Psicometria/normas , Melhoria de Qualidade , Reprodutibilidade dos Testes , Fatores Socioeconômicos
12.
Yi Chuan ; 40(7): 546-560, 2018 Jul 20.
Artigo em Chinês | MEDLINE | ID: mdl-30021718

RESUMO

The molecular mechanisms of pathogen persistence within host cells are emerging hotspots, and one of the causes of its persistence is the acid resistance of bacteria. Currently, tuberculosis remains a serious threat to global public health and it is caused by Mycobacterium tuberculosis. In particular, acid resistance of M. tuberculosis and its persistence within macrophages contribute significantly to tuberculosis. Investigations have uncovered three major mechanisms underlying its acid resistance: the control of proton entry, metabolic regulation of intracellular acid-base balance and regulation of the two-component signaling system. In this review, we summarize the overall regulation network of M. tuberculosis in the acidic environment, aiming at providing a new overall idea for treating M. tuberculosis persistence and exploring new targets for tuberculosis control.


Assuntos
Macrófagos/microbiologia , Mycobacterium tuberculosis/genética , Transdução de Sinais , Tuberculose , Equilíbrio Ácido-Base , Humanos
13.
Biomed Environ Sci ; 31(4): 261-271, 2018 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-29773089

RESUMO

OBJECTIVE: To investigate the prevalence and possible factors influencing metabolic syndrome in people from Guizhou Province and to explore the predictive value of the fat-to-muscle ratio in diagnosing metabolic syndrome. METHODS: A multistage stratified sampling method was used in this cross-sectional study of 20-80 years old Han and Bouyei populations from Guizhou Province, southwestern China, from October-December 2012. The study included 4,553 cases of metabolic syndrome, that was defined according to 2005 International Diabetes Federation criteria. The receiver operating characteristic curve was used for determining the sensitivity, specificity, and predictive ability of the fat-to-muscle ratio for the diagnosis of metabolic syndrome. RESULTS: The age-standardized prevalence of metabolic syndrome was 11.38% (men: 9.76%; women: 12.72%) for Han and 4.78% (men: 4.43%; women: 5.30%) for Bouyei populations. In Guizhou Province, the cut-off value for the men fat-to-muscle ratio was 0.34, the area under the curve was 0.95, and the sensitivity and specificity were 0.94 and 0.85, respectively. The cut-off value for the women fat-to-muscle ratio was 0.55, the area under the curve was 0.91, and the sensitivity and specificity were 0.93 and 0.79, respectively. CONCLUSION: The fat-to-muscle ratio is highly predictive of metabolic syndrome in Guizhou Province, and a useful reference indicator.


Assuntos
Tecido Adiposo/fisiologia , Grupo com Ancestrais do Continente Asiático , Composição Corporal/genética , Composição Corporal/fisiologia , Síndrome Metabólica/genética , Músculo Esquelético/fisiologia , Adulto , Idoso , Idoso de 80 Anos ou mais , China/epidemiologia , Predisposição Genética para Doença , Humanos , Síndrome Metabólica/epidemiologia , Pessoa de Meia-Idade , Adulto Jovem
14.
Genes (Basel) ; 9(3)2018 Mar 16.
Artigo em Inglês | MEDLINE | ID: mdl-29547590

RESUMO

Cytokinin oxidase/dehydrogenases (CKXs) play a critical role in the irreversible degradation of cytokinins, thereby regulating plant growth and development. Brassica napus is one of the most widely cultivated oilseed crops worldwide. With the completion of whole-genome sequencing of B. napus, genome-wide identification and expression analysis of the BnCKX gene family has become technically feasible. In this study, we identified 23 BnCKX genes and analyzed their phylogenetic relationships, gene structures, conserved motifs, protein subcellular localizations, and other properties. We also analyzed the expression of the 23 BnCKX genes in the B. napus cultivar Zhong Shuang 11 ('ZS11') by quantitative reverse-transcription polymerase chain reaction (qRT-PCR), revealing their diverse expression patterns. We selected four BnCKX genes based on the results of RNA-sequencing and qRT-PCR and compared their expression in cultivated varieties with extremely long versus short siliques. The expression levels of BnCKX5-1, 5-2, 6-1, and 7-1 significantly differed between the two lines and changed during pod development, suggesting they might play roles in determining silique length and in pod development. Finally, we investigated the effects of treatment with the synthetic cytokinin 6-benzylaminopurine (6-BA) and the auxin indole-3-acetic acid (IAA) on the expression of the four selected BnCKX genes. Our results suggest that regulating BnCKX expression is a promising way to enhance the harvest index and stress resistance in plants.

15.
Zhongguo Zhong Yao Za Zhi ; 43(1): 119-122, 2018 Jan.
Artigo em Chinês | MEDLINE | ID: mdl-29552821

RESUMO

In order to explore the anti-inflammatory activity and active ingredient basis from the leaves of the Belamcanda chinensis and Iris tectorum, we established an HPLC method for simultaneous determination of six anti-inflammatory active ingredient contents in the root of the B. chinensis and I. tectorum as well as their leaves with different dry methods, and the anti-inflammatory effects of the extract were studied by the mouse ear swelling experiment. The HPLC analysis was performed on an Agilent WondaSil© C18-WR(4.6 mm×250 mm,5 µm),with isocratic elution of acetonitrile-0.1% ortho-phosphoric acid solution at a flow rate of 1. 0 mL·min⁻¹ and the detection was carried out at 265 nm. The chemical compositions of the B. chinensis and I. tectorum are similar but the contents of them are obviously different. Both rhizome and leaf extract of B. chinensis and I. tectorum had inhibitory effects on inflamed mice induced by dimethylbenzene and had anti-inflammatory effects by animal experiment, which could lay the material and active foundation for the development of the non-medicinal parts of the B. chinensis and I. tectorum.


Assuntos
Anti-Inflamatórios/farmacologia , Iris (Planta)/química , Compostos Fitoquímicos/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Camundongos , Compostos Fitoquímicos/isolamento & purificação , Folhas de Planta/química , Rizoma/química
16.
Bioorg Med Chem Lett ; 27(24): 5457-5462, 2017 12 15.
Artigo em Inglês | MEDLINE | ID: mdl-29132751

RESUMO

A series of new 3-substitutedphenyl-4-substitutedbenzylideneamino-1,2,4-triazole Mannich bases and bis-Mannich bases were synthesized through Mannich reaction with high yields. Their structures were confirmed by means of IR, 1H NMR, 13C NMR and elemental analysis. The preliminary bioassay indicated that compounds 7g, 7h and 7l exhibited potent in vitro inhibitory activities against ketol-acid reductoisomerase (KARI) with Ki value of (0.38 ±â€¯0.25), (6.59 ±â€¯2.75) and (8.46 ±â€¯3.99) µmol/L, respectively, and were comparable with IpOHA. They could be new KARI inhibitors for follow-up research. Some of the title compounds also exhibited obvious herbicidal activities against Echinochloa crusgalli and remarkable in vitro fungicidal activities against Physalospora piricola and Rhizoctonia cerealis. The SAR of the compounds were analyzed, in which the molecular docking revealed the binding mode of 7g with the KARI, and the 3D-QSAR results provided useful information for guiding further optimization of this kind of structures to discover new fungicidal agents towards Rhizoctonia cerealis.


Assuntos
Antifúngicos/síntese química , Herbicidas/síntese química , Cetol-Ácido Redutoisomerase/antagonistas & inibidores , Bases de Mannich/química , Triazóis/química , Antifúngicos/química , Antifúngicos/farmacologia , Sítios de Ligação , Echinochloa/efeitos dos fármacos , Echinochloa/enzimologia , Fungos/efeitos dos fármacos , Fungos/enzimologia , Herbicidas/química , Herbicidas/farmacologia , Cetol-Ácido Redutoisomerase/metabolismo , Cinética , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Relação Quantitativa Estrutura-Atividade
17.
Bioorg Med Chem Lett ; 26(19): 4661-4665, 2016 10 01.
Artigo em Inglês | MEDLINE | ID: mdl-27575481

RESUMO

A series of novel 5-substituted-1,3,4-oxadiazole Mannich bases and bis-Mannich bases have been conveniently synthesized in good yields. Their structures were characterized by IR, (1)H NMR, (13)C NMR and elemental analysis. The preliminary bioassay results indicated that some of the compounds showed promising in vitro fungicidal activities towards several test plant fungi; some of them exhibited significant herbicidal activities against Brassica campestris and excellent in vitro inhibitory activities against rice ketol-acid reductoisomerase (KARI). Among 14 novel compounds, 8c, 8d and 8m showed potent KARI inhibitory activities with Ki value of (0.96±0.42), (3.86±0.49) and (3.10±0.71) µmol/L, respectively, and were comparable with IpOHA. These compounds could be novel KARI inhibitors for further investigation. The density functional theory (DFT) calculations and molecular docking were carried out to study the structure-activity relationship (SAR) of the active inhibitors in this Letter.


Assuntos
Inibidores Enzimáticos/farmacologia , Cetol-Ácido Redutoisomerase/antagonistas & inibidores , Bases de Mannich/síntese química , Bases de Mannich/farmacologia , Oxidiazóis/química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Bases de Mannich/química , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Espectrofotometria Infravermelho , Relação Estrutura-Atividade
18.
Guang Pu Xue Yu Guang Pu Fen Xi ; 36(3): 635-9, 2016 Mar.
Artigo em Chinês | MEDLINE | ID: mdl-27400496

RESUMO

The polycrystalline silicon thin films play an important role in the field of electronics. In the paper, α-SiAl composite membranes on glass substrates was prepared by magnetron co-sputtering. The contents of Al radicals encapsulated-in the α-Si film can be adjusted by changing the Al to Si sputtering power ratios. The as-prepared α-Si films were converted into polycrystalline films by using a rapid thermal annealing (RTP) at low temperature of 350 degrees C for 10 minutes in N2 atmosphere. An X-ray diffractometer, and Raman scattering and UV-Visible-NIR Spectrometers were used to characterize the properties of the Pc-Si films. The influences of Al content on the properties of the Pc-Si films were studied. The results showed that the polycrystalline silicon films were obtained from α-SiAl composite films which were prepared by magnetron co-sputtering at a low temperature following by a rapid thermal annealing. The grain size and the degree of crystallization of the Pc-Si films increased with the increase of Al content, while the optical band gap was reduced. The nc-Si films were prepared when the Al to Si sputtering power ratio was 0.1. And a higher Crystallization rate (≥ 85%) of polycrystalline silicon films were obtained when the ratio was 0.3. The band gaps of the polycrystalline silicon films can be controlled by changing the aluminum content in the films.

19.
Neurol Res ; 38(7): 647-54, 2016 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27238733

RESUMO

OBJECTIVE: To characterize the early delayed and late-delayed cognitive dysfunction induced by various doses of whole brain irradiation in young rats. METHODS: One-month-old Sprague-Dawley male rats were divided randomly into the 0 (control), 0 (anesthesia control), 2, 10, 20, and 30-Gy groups. Each group was then subdivided into 4 groups according to the experimental intervals: 1, 2, 3, and 6 months after radiation. Rats were irradiated using a 4-MeV electron beam, which was generated by a linear accelerator. Sequential behavioral tests, including open field, novel location and novel object recognition and Morris water maze were performed after radiation. Changes in gross neurological symptoms, body weight, topical skin response, and histopathology were observed. RESULTS: In the open field test, there were no radiation-induced alterations found. In the novel location and novel object recognition tests, rats of the 20-Gy group spent less time exploring the novel object and novel location 3 months after irradiation. During the place navigation test, the spatial working memory of the 30 and 20-Gy irradiated rats were impaired from 1 to 2 months after irradiation, respectively. In the spatial probe test, the 20 and 30-Gy irradiated rats spent less time in the critical region compared to control rats at 3 and 6 months post-irradiation. Morphological changes, including edema, vascular dilation, focal necrosis, demyelination, and adjacent reactive gliosis were observed in the 30-Gy irradiation group. CONCLUSION: More than 20 Gy of whole brain irradiation dose can cause significant cognitive dysfunction in young rats.


Assuntos
Encéfalo/efeitos da radiação , Transtornos Cognitivos/etiologia , Transtornos Cognitivos/patologia , Lesões Experimentais por Radiação/complicações , Análise de Variância , Animais , Peso Corporal/efeitos da radiação , Encéfalo/patologia , Modelos Animais de Doenças , Relação Dose-Resposta à Radiação , Comportamento Exploratório/efeitos da radiação , Masculino , Aprendizagem em Labirinto/efeitos da radiação , Exame Neurológico , Ratos , Ratos Sprague-Dawley , Reconhecimento Psicológico/efeitos da radiação , Fatores de Tempo
20.
Eur J Med Chem ; 117: 167-78, 2016 Jul 19.
Artigo em Inglês | MEDLINE | ID: mdl-27092414

RESUMO

A series of novel carboxamide compounds 19a-19j, 20a-20j and 22a-22d containing piperazine and arylsulfonyl moieties have been synthesized. The bioassay results showed that some compounds exhibited favorable herbicidal activities against dicotyledonous plants and many of them possessed excellent antifungal activities. Among 24 novel compounds, some showed superiority over the commercial fungicides Chlorothalonil, Dimethomorph, Thiophanate-methyl, Iprodione, and Zhongshengmycin at 500 mg/L concentration. Some compounds also exhibited high KARI inhibitory activity at 100 µg/mL concentration and could be used as new KARI lead inhibitors for further studies. Moreover, SAR of these new compounds were comprehensively investigated using different computational methods in which 3D-QSAR model obtained provided useful information for further structural optimization for the discovery of new fungicides. The results of this research will contribute to explore comprehensive biological activities of piperazine-containing compounds in different areas of chemistry.


Assuntos
Amidas/síntese química , Antifúngicos/síntese química , Herbicidas/síntese química , Relação Quantitativa Estrutura-Atividade , Amidas/farmacologia , Antifúngicos/farmacologia , Ácidos Arilsulfônicos/química , Herbicidas/farmacologia , Piperazina , Piperazinas/química
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