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1.
Steroids ; 101: 28-36, 2015 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-26048447

RESUMO

Eight new C21 steroidal glycosides, named cynsaccatols A-H (1-8), along with two known analogs (9-10), were isolated from the roots of Cynanchum saccatum. Their structures were determined on the basis of detailed spectroscopic analysis, as well as HRESIMS. All compounds (1-10) were tested for their cytotoxicity in vitro using three human cancer cell lines (HepG2, Hela and U251), and compounds 1, 4, 5, 9, 10 showed weak inhibitory activities against different cell lines, respectively.


Assuntos
Antineoplásicos/química , Antineoplásicos/farmacologia , Cynanchum/química , Glicosídeos/química , Glicosídeos/farmacologia , Raízes de Plantas/química , Esteroides/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Glicosídeos/isolamento & purificação , Humanos
2.
Vet Microbiol ; 172(3-4): 534-41, 2014 Aug 27.
Artigo em Inglês | MEDLINE | ID: mdl-24999233

RESUMO

The aim of this study was to investigate the trends and the diversity of CTX-M types of extended-spectrum ß-lactamase (ESBL) in Escherichia coli isolated from food animals in China over a ten-year period. From 2003 to 2012, 2815 E. coli isolates collected from diseased animals (chickens, pigs, and waterfowl) were screened for the prevalence of CTX-M genes. CTX-M-positive isolates were tested for their susceptibilities to 10 antimicrobial agents and the clonal relationship of CTX-M-producing E. coli isolates was also assessed. Overall, 677 (20.1%) of the 2815 E. coli isolates carried CTX-M genes. Eighteen different types of CTX-M ESBLs were identified, with CTX-M-14, CTX-M-55, and CTX-M-65 being the most dominant genotypes. The occurrence of CTX-M-producing E. coli increased significantly from 5.7% in 2003-2005 to 35.3% in 2009-2012 (p<0.0001). High genetic heterogeneities were observed in the CTX-M-producing E. coli isolates. Most CTX-M-producing strains were also resistant to other classes of antimicrobials. Compared to isolates carrying CTX-M-9 subgroup of ESBLs, isolates carrying CTX-M-1 subgroup ESBLs showed significantly higher resistance rates to ceftazidime, amikacin, and fosfomycin (p<0.01). The study reported the dramatic increase of CTX-M ESBLs in E. coli isolated from animals overtime in China. The increasing incidence of CTX-M-55 with high hydrolytic activity against ceftazidime and the widely spread co-resistance in CTX-M-producing isolates alarm the serious antimicrobial resistance situation in China and highlight the need for urgent control strategies to limit the dissemination of those resistant genes in China.


Assuntos
Cefalosporinas/farmacologia , Farmacorresistência Bacteriana/genética , Infecções por Escherichia coli/veterinária , Escherichia coli/efeitos dos fármacos , beta-Lactamases/metabolismo , Animais , China , Escherichia coli/enzimologia , Escherichia coli/genética , Infecções por Escherichia coli/epidemiologia , Microbiologia de Alimentos , Regulação Bacteriana da Expressão Gênica/fisiologia , Regulação Enzimológica da Expressão Gênica/fisiologia , Variação Genética , Genótipo , Prevalência , beta-Lactamases/genética
3.
Vet Microbiol ; 170(1-2): 89-96, 2014 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-24553411

RESUMO

This study was performed to determine the prevalence of plasmid-mediated quinolone resistance (PMQR) determinants and characterize the ciprofloxacin resistance in Escherichia coli isolated from different sources in China. PMQR determinants were detected by PCR amplification and sequencing in 2297 E. coli isolates randomly collected from animals, food and humans during 2004 to 2011. MICs of ciprofloxacin were determined by agar dilution method. Of the 2297 E. coli isolates, 43.6% harbored at least one PMQR gene. The most common PMQR gene was oqxAB (29.3%), followed by qnr (13.6%), aac(6')-Ib-cr (11.6%), and qepA (3.3%). 12.0% isolates carried two or more PMQR genes. The prevalence of PMQR genes in food animal isolates increased over time, from 38.7% in 2004 to 69.8% in 2011. The prevalence of PMQR/ciprofloxacin resistance among isolates from pig, chicken, duck, companion animals, animal food and human volunteers were 65.2%/69.6%, 42.4%/60.0%, 59.4%/65.0%, 28.6%/57.5%, 29.3%/25.6%, and 14.0/8.7%, respectively. Most isolates carrying qnr along showed susceptible to ciprofloxacin, and only 21.6% the isolates exhibited resistance to ciprofloxacin, which was significantly lower than those carrying other PMQR genes (65.2-89.9%) and those that do not (43.1%) (p<0.01). In conclusion, high frequency of ciprofloxacin resistance and PMQR genes was observed among E. coli isolates of different origins in China, with oqxAB being the most frequent. qnr-positive E. coli isolates have relatively low ciprofloxacin resistance rate compared with other PMQR determinants-carrying isolates and PMQR-negative isolates.


Assuntos
Antibacterianos/farmacologia , Ciprofloxacina/farmacologia , Farmacorresistência Bacteriana/genética , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Quinolonas/farmacologia , Animais , China , Escherichia coli/isolamento & purificação , Proteínas de Escherichia coli/genética , Microbiologia de Alimentos , Humanos , Testes de Sensibilidade Microbiana , Plasmídeos/genética , Prevalência
4.
Antimicrob Agents Chemother ; 57(8): 4068-71, 2013 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-23752509

RESUMO

The chimeric bla(CTX-M-123) gene was identified in two ceftazidime-resistant Escherichia coli isolates from animals in different Chinese provinces. Like other CTX-M-1/9 group hybrids (CTX-M-64 and CTX-M-132), the ends (amino acids 1 to 135 and 234 to 291) of CTX-M-123 match CTX-M-15 while the central part (122 to 241) matches CTX-M-14. bla(CTX-M-123) is carried on related, but not identical, ~90-kb IncI1 plasmids in the two isolates, and one isolate simultaneously carries the group 1 blaCTX-M-55 gene on an additional IncI2 plasmid.


Assuntos
Proteínas de Escherichia coli/metabolismo , Escherichia coli/enzimologia , Genes Bacterianos , Proteínas Mutantes Quiméricas/metabolismo , beta-Lactamases/metabolismo , Sequência de Aminoácidos , Animais , Proteínas de Bactérias/genética , Proteínas de Bactérias/metabolismo , Sequência de Bases , Ceftazidima/farmacologia , China , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Proteínas de Escherichia coli/classificação , Proteínas de Escherichia coli/genética , Recombinação Homóloga , Testes de Sensibilidade Microbiana , Dados de Sequência Molecular , Proteínas Mutantes Quiméricas/genética , Plasmídeos/genética , Plasmídeos/metabolismo , beta-Lactamases/classificação , beta-Lactamases/genética
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