RESUMO
A series of secondary amines combining monoterpenoid and aminoadamantane moieties have been synthesized. Their cytotoxic activity against human cancer cells CEM-13, MT-4, and U-937 has been studied for the first time. Most of the obtained compounds exhibited a significant cytotoxic activity with the median cytotoxic dose (CTD50) ranging from 6 to 84 µM. The most promising results were obtained for compound 2b which was synthesized from 1-aminoadamantane and (-)-myrtenal and revealed a high activity against all tumor lines used (CTD50 = 12 ÷ 21 µM) along with low toxicity with respect to MDCK cells (CTD50 = 1500 µM). The synthesized amines do not exert the genotoxic effect on cells of the biosensor strain based on recombinant E. coli cells bearing the pRAC-gfp plasmid.
Assuntos
Adamantano/química , Adamantano/farmacologia , Antineoplásicos/química , Antineoplásicos/farmacologia , Monoterpenos/química , Mutagênicos/química , Mutagênicos/farmacologia , Animais , Linhagem Celular Tumoral , Cães , Humanos , Células Madin Darby de Rim CaninoRESUMO
The synthesis and biological evaluation of a novel series of dimeric camphor derivatives are described. The resulting compounds were studied for their antiviral activity, cyto- and genotoxicity. Compounds 3a and 3d in which the quaternary nitrogen atoms are separated by the C5H10 and С9H18 aliphatic chain, exhibited the highest efficiency as an agent inhibiting the reproduction of the influenza virus A(H1N1)pdm09. The cytotoxicity data of compounds 3 and 4 revealed their moderate activity against malignant cell lines; compound 3f had the highest activity for the CEM-13 cells. These results show close agreement with the data of independent studies on toxicity of these compounds, in particular that the toxicity of compounds strongly depends on spacer length.
Assuntos
Antivirais/química , Compostos Bicíclicos com Pontes/química , Cânfora/análogos & derivados , Compostos de Amônio Quaternário/química , Animais , Antivirais/síntese química , Antivirais/toxicidade , Sítios de Ligação , Compostos Bicíclicos com Pontes/síntese química , Compostos Bicíclicos com Pontes/toxicidade , Cânfora/síntese química , Cânfora/toxicidade , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cães , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Humanos , Vírus da Influenza A Subtipo H1N1/efeitos dos fármacos , Vírus da Influenza A Subtipo H1N1/metabolismo , Células Madin Darby de Rim Canino , Simulação de Acoplamento Molecular , Testes de Mutagenicidade , Estrutura Terciária de Proteína , Compostos de Amônio Quaternário/síntese química , Compostos de Amônio Quaternário/toxicidade , Proteínas da Matriz Viral/química , Proteínas da Matriz Viral/metabolismoRESUMO
The prevalence of Borrelia burgdorferi sensu lato (s.l.) genospecies in West Siberia as well as in many other regions of Russia remains insufficiently investigated. In the present study a total of 151 adult female ticks Ixodes persulcatus Schulze, collected at three localities in eastern regions of West Siberia, where Lyme disease is endemic, were examined for the presence of the spirochete B. burgdorferi s.l. by polymerase chain reaction targeting the 23S-5S rRNA intergenic spacer regions. Spirochetal DNA was detected in on average 15.2+/-3.0% of the ticks examined. The infection rate of adult ticks with B. burgdorferi s.l. at various localities ranged from 8.6+/-3.4% to 29.0+/-7.6%, being greatest in the northernmost site studied and decreasing southwards. The restriction patterns obtained after MseI digestion of the 23S-5S rRNA intergenic spacer amplicons assigned 23 DNA samples to the following genomic groups: 19 to B. garinii (12 to group NT29 and seven to group 20047(T)), three to B. afzelii, and one to mixed B. afzelii and B. garinii NT29. We have not detected other genospecies, which were found in ticks in Europe, the Russian Far East and Japan. Thus, the ticks examined were associated only with two genospecies of Borrelia burgdorferi s.l. pathogenic to humans (B. garinii and B. afzelii), and B. garinii was the major genospecies infecting adult I. persulcatus in eastern regions of West Siberia.
Assuntos
Grupo Borrelia Burgdorferi/classificação , Ixodes/microbiologia , RNA Bacteriano/análise , Animais , Grupo Borrelia Burgdorferi/genética , Grupo Borrelia Burgdorferi/isolamento & purificação , Reação em Cadeia da Polimerase , Polimorfismo de Fragmento de Restrição , RNA Bacteriano/genética , RNA Ribossômico 23S/genética , RNA Ribossômico 5S/genética , Federação Russa , SibériaRESUMO
PCR assays were used to test adult Ixodes persulcatus ticks from Western Siberia, Russia, for Borrelia burgdorferi sensu lato, tick-borne encephalitis virus (TBEV), and the human granulocytic ehrlichiosis (HGE) agent. Of the 150 ticks that were studied, 38% were infected with B. burgdorferi, 46% were infected with TBEV, and 8% were infected with the HGE agent. These three pathogens were distributed in the ticks independently of one another.
