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1.
Fish Shellfish Immunol ; 97: 432-439, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31883470

RESUMO

As a high mortality disease, Infectious spleen and kidney necrosis virus (ISKNV) can cause massive economic damage on mandarin fish farming industry in China, which seriously hindered the development of mandarin fish farming industry. In this research, SWCNTs (single-walled carbon nanotubes) as a candidate for DNA vaccine carrier was vaccinated by immersion (1, 2, 5, 10, 20 mg/L) in juvenile mandarin fish. In muscle, spleen and kidney tissues, the results showed that transcription and expression of MCP gene can be detected in pcDNA-MCP and SWCNTs-pcDNA-MCP groups after bath immunization. The immune response (immune-related genes expression, serum antibody production, enzyme activities and C3 content) was significantly enhanced in fish which vaccinated with SWCNTs-pcDNA-MCP in comparison with those vaccinated with pcDNA-MCP alone. After 14 d challenge, the RPS (relative percentage survival) can be enhanced which using SWCNTs as a carrier in SWCNTs-pcDNA-MCP (82.4%) group at 20 mg/L (the highest vaccine dose) than the naked pcDNA-MCP (54.2%) group. This study reveals that functionalized SWCNTs could be a promising immersion DNA vaccine carrier in aquaculture.

2.
Fish Shellfish Immunol ; 92: 133-140, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31173860

RESUMO

Infectious spleen and kidney necrosis virus (ISKNV) cause a high mortality disease which lead to significant economic loss on mandarin fish in China. There is no effective drug or vaccine against this fatal disease at present. Meanwhile, many drugs and vaccines had no effect in many cases account of several impenetrable barriers (cell, skin and gastrointestinal tract). Here we reported an immersion subunit vaccine system (SWCNTs-MCP) encoding MCP gene of ISKNV based on single-walled carbon nanotubes (SWCNTs). To evaluate its efficacy against ISKNV, we found a stronger and longer duration immune response (serum antibody production, enzyme activities and immune-related genes expression) can be induced in fish vaccinated with SWCNTs-MCP in comparison with those vaccinated with MCP alone. Importantly, SWCNTs can increase the immune protective effect of naked subunit vaccine by ca. 23.8%. Thereby, this study demonstrates that SWCNTs as a promising carrier for subunit vaccine might be used to vaccinate large-scale juvenile mandarin fish by bath administration approach.


Assuntos
Doenças dos Peixes/imunologia , Imunidade Inata , Iridoviridae/imunologia , Nanotubos de Carbono , Perciformes/imunologia , Vacinação/veterinária , Vacinas Virais/imunologia , Animais , Infecções por Vírus de DNA/imunologia , Infecções por Vírus de DNA/veterinária , Vacinas de Subunidades/imunologia
4.
J Am Soc Hypertens ; 12(1): 58-65, 2018 01.
Artigo em Inglês | MEDLINE | ID: mdl-29100861

RESUMO

The objective was to investigate the role of angiotensin II type 2 receptor during electrophysiological remodeling of left ventricular hypertrophic myocardium in spontaneously hypertensive rats (SHRs). A total of 36, aged 10 weeks, male SHRs were divided into three groups: control, valsartan, and valsartan + PD123319 groups (n = 12 in each). The systolic blood pressure, left ventricular mass index, ventricular effective refractory period, and ventricular fibrillation threshold (VFT) were also measured after 8 weeks. At the same time, INa, ICaL, Ito, and membrane capacitance were measured in left ventricular myocytes by whole-cell patch-clamp. The VFT of valsartan was higher than that of control (valsartan vs. CONTROL: 17.4 ± 0.6 mA vs. 15.8 ± 0.5 mA, P < .05). The VFT of valsartan was higher than that of valsartan + PD123319 (valsartan vs. valsartan + PD123319: 17.4 ± 0.6 mA vs. 16.6 ± 0.9 mA, P < .05). The density of Ito of valsartan was higher than that of control (valsartan vs. CONTROL: 14.7 ± 0.42 pA/pF vs. 11.2 ± 0.15 pA/pF, P < .05). The density of Ito of valsartan was higher than that of valsartan + PD123319 (valsartan vs. valsartan + PD123319: 14.7 ± 0.42 pA/pF vs. 13.6 ± 0.30 pA/pF, P < .05). The density of ICaL of valsartan was lower than that of control (valsartan vs. CONTROL: -4.6 ± 0.2 pA/pF vs. -6.9 ± 0.1 pA/pF, P < .05). The density of ICaL of valsartan was lower than that of valsartan + PD123319 (valsartan vs. valsartan + PD123319: -4.6 ± 0.2 pA/pF vs. -5.4 ± 0.1 pA/pF, P < .05). These results demonstrated that the stimulation of angiotensin II type 2 receptor improved electrophysiological remodeling of left ventricular hypertrophic myocardium in SHR.


Assuntos
Hipertensão , Hipertrofia Ventricular Esquerda , Imidazóis/farmacologia , Piridinas/farmacologia , Receptor Tipo 2 de Angiotensina/metabolismo , Bloqueadores do Receptor Tipo 1 de Angiotensina II/farmacologia , Bloqueadores do Receptor Tipo 2 de Angiotensina II/farmacologia , Animais , Modelos Animais de Doenças , Fenômenos Eletrofisiológicos , Hipertensão/complicações , Hipertensão/tratamento farmacológico , Hipertrofia Ventricular Esquerda/etiologia , Hipertrofia Ventricular Esquerda/metabolismo , Hipertrofia Ventricular Esquerda/fisiopatologia , Hipertrofia Ventricular Esquerda/prevenção & controle , Ratos , Ratos Endogâmicos SHR , Resultado do Tratamento , Valsartana/farmacologia , Remodelação Ventricular/efeitos dos fármacos , Remodelação Ventricular/fisiologia
5.
ACS Comb Sci ; 19(11): 708-713, 2017 11 13.
Artigo em Inglês | MEDLINE | ID: mdl-28985045

RESUMO

A microwave-assisted regioselective synthesis of 3-functionalized indole derivatives via a three-component domino reaction of anilines, arylglyoxal monohydrates, and cyclic 1,3-dicarbonyl compounds is described. The main advantages of this protocol are short reaction times, practical simplicity, its metal-free nature, the availability of starting materials, green solvents, and high regioselectivity.


Assuntos
Indóis/síntese química , Micro-Ondas , Compostos de Anilina/química , Técnicas de Química Sintética , Técnicas de Química Combinatória , Glioxal/química
6.
Org Biomol Chem ; 15(24): 5112-5116, 2017 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-28589976

RESUMO

With the assistance of the same bidentate directing group, the first example of sequential, controllable C-H functionalization of ß-arylethylamines at different positions for the construction of polysubstituted arenes is reported. Pd-Catalyzed highly regioselective ortho-C-H functionalization reactions of meta-aryl substituted arylethylamines are performed, including alkynylation, iodination, acetoxylation and amination, which led to a concise approach to the synthesis of polysubstituted ß-arylethylamine derivatives.

7.
J Org Chem ; 82(13): 6831-6839, 2017 07 07.
Artigo em Inglês | MEDLINE | ID: mdl-28617597

RESUMO

An efficient synthesis of isoindolin-1-ones from oxalyl amide-protected benzylamines, through ruthenium-catalyzed intramolecular C(sp2)-H carbonylation, has been developed. Variously substituted benzylamines could be well tolerated in this new protocol, affording the corresponding products in moderate to excellent yields. This approach constitutes the first example of Ru(II)-catalyzed C(sp2)-H carbonylation with isocyanate as a novel commercially available carbonyl source.

8.
Mol Divers ; 21(2): 293-304, 2017 May.
Artigo em Inglês | MEDLINE | ID: mdl-28144767

RESUMO

A concise, efficient one-pot synthesis of functionalized chromeno[4,3-b]pyridine derivatives via a three-component reaction of 4-oxo-4H-chromene-3-carbaldehydes, malononitrile or cyanoacetates, and aromatic amines under catalyst-free conditions in an environmentally friendly medium (ethanol-water, 3:1 v/v) is described. This synthesis involves a group-assisted purification process, which avoids traditional recrystallization and chromatographic purification methods.


Assuntos
Piridinas/química , Piridinas/síntese química , Técnicas de Química Sintética , Etanol/química , Química Verde , Água/química
9.
Sci Rep ; 6: 38410, 2016 12 02.
Artigo em Inglês | MEDLINE | ID: mdl-27910930

RESUMO

Controlling and reducing the formation of pathogenic biofilm on tooth surface is the key to the prevention and treatment of the biofilm-associated oral diseases. Antimicrobial peptides (AMPs), considered as possible future alternatives for conventional antibiotics, have been extensively studied for the control of bacterial infection. Due to the rapid dilution and degradation by human saliva, AMP preparations designed for oral use with longer retention and higher efficacy are in urgent need. To this end, a hydroxyapatite (HAp)-binding antimicrobial peptide (HBAMP), which is based on the fusion of a specific HAp-binding heptapeptide (HBP7) domain and a broad-spectrum antimicrobial peptide (KSLW) domain, has been developed in our laboratory. HBAMP was supposed to form a contact-active antibacterial interface on tooth surface to inhibit the formation of biofilms. In this study, we investigated its binding behaviour, antibacterial activity against bacteria in both planktonic and sessile states, enzymatic stability in human saliva, and cytocompatibility to human gingival fibroblasts (HGFs). Our findings suggest that HBAMP could adsorb on tooth surface to provide effective antibacterial activity with improved retention. This study provides a proof-of-concept on using conjugated molecules to promote antibacterial efficacy by synergistically actions of HBAMP free in solution and bound on tooth surface.


Assuntos
Antibacterianos/farmacologia , Peptídeos Catiônicos Antimicrobianos/farmacologia , Biofilmes/efeitos dos fármacos , Preparações de Ação Retardada/farmacologia , Durapatita/química , Plâncton/efeitos dos fármacos , Actinomyces viscosus/efeitos dos fármacos , Actinomyces viscosus/crescimento & desenvolvimento , Sequência de Aminoácidos , Peptídeos Catiônicos Antimicrobianos/química , Biofilmes/crescimento & desenvolvimento , Células Cultivadas , Preparações de Ação Retardada/química , Fibroblastos/efeitos dos fármacos , Fibroblastos/microbiologia , Fibroblastos/patologia , Gengiva/citologia , Gengiva/microbiologia , Humanos , Lactobacillus acidophilus/efeitos dos fármacos , Lactobacillus acidophilus/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Plâncton/crescimento & desenvolvimento , Ligação Proteica , Saliva/química , Saliva/microbiologia , Streptococcus mutans/efeitos dos fármacos , Streptococcus mutans/crescimento & desenvolvimento , Streptococcus sanguis/efeitos dos fármacos , Streptococcus sanguis/crescimento & desenvolvimento
10.
Org Lett ; 18(23): 5998-6001, 2016 12 02.
Artigo em Inglês | MEDLINE | ID: mdl-27934363

RESUMO

The first example of oxidative C-H/C-H cross-coupling of oxalyl amide-protected benzylamines and various heteroarenes in the presence of a rhodium(III) catalyst has been developed. The route provides a means of synthesizing ortho-heteroarylated benzylamines. The methodology presents broad substrate scope, great functional group tolerance, and good to excellent yields in the synthesis of substituted benzylamines. The study also reveals that the thienoisoquinoline derivatives can be accessed through the intramolecular amination of thiophenyl-substituted benzylamines with palladium(II).

11.
J Org Chem ; 81(13): 5681-9, 2016 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-27286881

RESUMO

Pd-catalyzed regioselective coupling of γ-C(sp(3))-H bonds of oxalyl amide-protected amino acids with heteroaryl and aryl iodides is reported. A wide variety of iodides are tolerated, giving the corresponding products in moderate to good yields. Various oxalyl amide-protected amino acids were compatible in this C-H transformation, thus representing a practical method for constructing non-natural amino acid derivatives.

12.
Chem Commun (Camb) ; 52(42): 6903-6, 2016 May 25.
Artigo em Inglês | MEDLINE | ID: mdl-27142086

RESUMO

The first bidentate directing group assisted highly selective meta arylation of ß-arylethylamine derivatives via palladium/norbornene catalysis is reported, and the range of aryl iodides for the oxalyl amide assisted meta-selective arylation reactions is broadest yet reported. This meta arylation also proceeds well with thiophene derivatives, giving the corresponding products in satisfactory yields. And three-step functionalization of arylethyloxalamide with three different functional groups is successfully performed.

13.
J Org Chem ; 81(12): 5256-62, 2016 06 17.
Artigo em Inglês | MEDLINE | ID: mdl-27213988

RESUMO

Pd-catalyzed regioselective coupling of ß-C(sp(2))-H bonds in aromatic amines protected by oxalyl amide with carbon monoxide is reported. The reaction could tolerate various functional groups and could afford good to excellent yields of the corresponding 3,4-dihydroisoquinolinone derivatives. Remarkably, it could also tolerate ß-arylethylamino acid and thiopheneethylamine derivatives, thus showing their potential for producing several important units for bioactive compound synthesis.

14.
J Huazhong Univ Sci Technolog Med Sci ; 35(6): 785-792, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26670426

RESUMO

Recent report on epidemiology of acute kidney injury (AKI) is lacking for Chinese children. We aimed to investigate the risk factors for stage and prognostic factors for renal recovery in hospitalized children. Pediatric patients (≤18 years old) admitted during 2003 to 2013 were enrolled in this study. AKI was defined and staged using Kidney Disease Improving Global Outcomes (KDIGO) criteria. Logistic regression analysis was performed to determine the risk factors and prognostic factors. The morbidity of pediatric AKI was 0.31% (205/65 237). There were 45 (22.0%) cases in stage III, 30 (14.6%) cases in stage II and 130 (63.4%) cases in stage III. The majority of etiologies were intrinsic renal defects (85.4%). Age, weight, vomit, etiology, blood urea nitrogen (BUN) at admission and several blood gas measurements were associated with AKI stage III. Age (OR=0.894; 95% CI, 0.832-0.962; P=0.003), vomit (OR=2.375; 95% CI, 1.058-5.333; P=0.036) and BUN at admission (OR=1.135; 95% CI, 1.085-1.187; P<0.001) were identified as independent risk factors for AKI stage III. After treatment, 172 (83.9%) patients achieved complete or partial recovery. The mortality was 3.9%. Variables were found as prognostic factors for renal recovery, such as age, stage, hospital stay, BUN at discharge, white blood cells, red blood cells, platelets (PLTs), blood pH and urine blood. Among them, AKI stage (stage III vs. stage I; OR, 6.506; 95% CI, 1.640-25.816; P=0.008), BUN at discharge (OR, 0.918; 95% CI, 0.856-0.984; P=0.016) and PLTs (OR, 1.007; 95% CI, 1.001-1.013; P=0.027) were identified as independent prognostic factors. AKI is still common in Chinese hospitalized children. Identified risk factors and prognostic factors provide guiding information for clinical management of AKI.


Assuntos
Lesão Renal Aguda/epidemiologia , Adolescente , Criança , Pré-Escolar , China/epidemiologia , Feminino , Humanos , Lactente , Recém-Nascido , Masculino , Prognóstico , Estudos Retrospectivos , Fatores de Risco
15.
J Org Chem ; 80(18): 9297-306, 2015 Sep 18.
Artigo em Inglês | MEDLINE | ID: mdl-26309049

RESUMO

A method for palladium-catalyzed oxalyl amide-directed arylation of α-unsubstituted aliphatic amines with aryl iodides has been developed. A wide variety of aryl iodides are tolerated in this transformation, affording various γ-arylpropylamine derivatives. Heterocyclic iodides can also be competent reagents in this γ-C(sp(3))-H bonds transformation.

16.
J Org Chem ; 80(16): 8435-42, 2015 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-26193420

RESUMO

A simple and efficient one-pot construction of pyrazolo[3,4-e]indolizine derivatives via a diethylamine-catalyzed three-component domino reaction of arylglyoxals, cyclic 1,3-diones, and 5-aminopyrazoles under microwave irradiation is described. In this one-pot transformation, seven bonds and two new rings are efficiently formed. This synthesis was confirmed to follow the group-assisted-purification (GAP) chemistry process, which can avoid traditional recrystallization or chromatography purification methods.


Assuntos
Dietilaminas/química , Indolizinas/síntese química , Pirazóis/síntese química , Catálise , Ciclização , Indolizinas/química , Micro-Ondas , Estrutura Molecular , Pirazóis/química
17.
J Org Chem ; 80(16): 7896-904, 2015 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-26197216

RESUMO

A highly regioselective palladium-catalyzed ester-directed ortho-olefination of phenyl acetic and propionic esters with olefins via C-H bond activation has been developed. A wide variety of phenyl acetic and propionic esters were tolerated in this transformation, affording the corresponding olefinated aromatic compounds. The ortho-olefination of heterocyclic acetic and propionic esters also took place smoothly giving the products in good yields, thus proving the potential utility of this protocol in synthetic chemistry.


Assuntos
Alcenos/síntese química , Ésteres/química , Compostos Organometálicos/química , Paládio/química , Alcenos/química , Catálise , Estrutura Molecular
18.
J Org Chem ; 80(2): 1025-33, 2015 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-25521750

RESUMO

A concise and efficient three-component domino reaction has been developed for the synthesis of polyfunctionalized indenopyridine and hydroisoquinoline derivatives via the cleavage of a C­C bond under transition-metal-free conditions. This reaction provides facile access to complex nitrogen-containing heterocycles by simply mixing three common starting materials in EtOH in the presence of 20 mol % NaOH under microwave irradiation conditions.


Assuntos
Carbono/química , Compostos Heterocíclicos/química , Indenos/química , Nitrogênio/química , Piridinas/química , Micro-Ondas , Estrutura Molecular
19.
Chem Commun (Camb) ; 51(8): 1528-31, 2015 Jan 28.
Artigo em Inglês | MEDLINE | ID: mdl-25501740

RESUMO

Two series of novel functionalized polyhydroisoquinoline derivatives have been synthesized via the three-component domino reaction of glutaraldehyde and malononitrile with a series of ß-ketoamides under microwave irradiation conditions in the presence of a catalytic amount of Et3N (10 mol%). This reaction represents the first reported process for the facile conversion of a ß-ketoamide to a hydroisoquinoline via a C-N bond cleavage reaction without the need for a multistep reaction process.


Assuntos
Isoquinolinas/síntese química , Amidas/química , Amidas/efeitos da radiação , Catálise , Glutaral/química , Glutaral/efeitos da radiação , Isoquinolinas/química , Micro-Ondas , Nitrilos/química , Nitrilos/efeitos da radiação
20.
Toxicol Rep ; 2: 785-791, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-28962414

RESUMO

Liquid-liquid extraction (LLE) is the most commonly sample preparation procedure used by forensic toxicologists in China for screening drugs in whole human blood. It extracts numerous substances from blood including targeted drugs and interfering substances, specifically triglycerides (TG). With increasing prevalence of hyperlipidemia, the influences of TG on LLE and on subsequent analysis with gas chromatography-mass spectrometry (GC-MS) may become a major issue for forensic laboratories. This study aims to elucidate the influences of TG on LLE and to provide possible solutions to this problem. Nineteen commonly encountered drugs in forensic cases were spiked to human whole blood with different TG concentrations. Diethyl ether, ethyl acetate/hexane mixed solutions, chlorobutane and several other frequently used solvents were tested for the extraction of drugs from spiked whole blood. The supernatant organic layer was evaporated to dryness and reconstituted with methanol. The resultant products were analyzed by GC-MS, and the extraction recovery was calculated. LLE with diethyl ether, ethyl acetate/hexane (9:1) and chlorobutane all possessed effective and reliable extraction recoveries for blood sample with low TG concentrations (0.63-6.85 mmol/L). At high TG concentrations, diethyl ether produced a highly turbid substance that could not be further analyzed using GC-MS. Extraction recoveries drastically dropped for ethyl acetate/hexane (9:1) mixture at high TG concentrations, while chlorobutane experienced minimal drops in extraction recoveries. In conclusion, TG levels in whole blood noticeably influence drug recovery to variable extents depending on the LLE solvent. Chlorobutane showed minimal influences from TG content in whole blood and thus is the recommended LLE solvent for forensic drug extraction.

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