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1.
Antiviral Res ; 120: 126-33, 2015 Aug.
Artículo en Inglés | MEDLINE | ID: mdl-26072310

RESUMEN

Influenza virus continues to remain one of the leading human respiratory pathogens causing significant morbidity and mortality around the globe. Due to short-term life cycle and high rate of mutations influenza virus is able to rapidly develop resistance to clinically available antivirals. This makes necessary the search and development of new drugs with different targets and mechanisms of activity. Here we report anti-influenza activity of camphor derivative 1,7,7-trimethylbicyclo[2.2.1]heptan-2-ylidene-aminoethanol (camphecene). In in vitro experiments it inhibited influenza viruses A(H1, H1pdm09, H3 and H5 subtypes) and B with EC50's lying in micromolar range. Due to low cytotoxicity it resulted in high selectivity indices (74-661 depending on the virus). This effect did not depend on susceptibility or resistance of the viruses to adamantane derivatives amantadine and rimantadine. The compound appeared the most effective when added at the early stages of viral life cycle (0-2h p.i.). In direct hemagglutinin inhibition tests camphecene was shown to decrease the activity of HA's of influenza viruses A and B. The activity of camphecene was further confirmed in experiments with influenza virus-infected mice, in which, being used orally by therapeutic schedule (once a day, days 1-5 p.i.) it decreased specific mortality of animals infected with both influenza A and B viruses (highest indices of protection 66.7% and 88.9%, respectively). Taken together, these results are encouraging for further development of camphecene-based drug(s) and for exploration of camphor derivatives as highly prospective group of potential antivirals.


Asunto(s)
Antivirales/administración & dosificación , Alcanfor/análogos & derivados , Alcanfor/administración & dosificación , Etanolaminas/administración & dosificación , Hemaglutininas/metabolismo , Virus de la Influenza A/efectos de los fármacos , Virus de la Influenza B/efectos de los fármacos , Administración Oral , Animales , Antivirales/efectos adversos , Antivirales/farmacología , Alcanfor/efectos adversos , Alcanfor/farmacología , Supervivencia Celular/efectos de los fármacos , Modelos Animales de Enfermedad , Evaluación Preclínica de Medicamentos , Etanolaminas/efectos adversos , Etanolaminas/farmacología , Femenino , Ratones Endogámicos BALB C , Pruebas de Sensibilidad Microbiana , Infecciones por Orthomyxoviridae/tratamiento farmacológico , Análisis de Supervivencia , Resultado del Tratamiento
2.
Antibiot Khimioter ; 45(6): 13-6, 2000.
Artículo en Ruso | MEDLINE | ID: mdl-10904803

RESUMEN

The cycloferon efficacy was investigated in the treatment of experimental herpesvirus kerato-conjunctivitis in rabbits. The model was demonstrated to reflect the main aspects of herpesvirus eye lesions in humans. Cycloferon application similarly to that of known interferon inducer poludan has been shown to enhance processes of inflammation and subsequent regeneration of eye tissues as well as to decrease mortality of animals due to the generalization of infection.


Asunto(s)
Acridinas/uso terapéutico , Inductores de Interferón/uso terapéutico , Queratitis Herpética/tratamiento farmacológico , Animales , Evaluación Preclínica de Medicamentos , Iridociclitis/diagnóstico , Iridociclitis/tratamiento farmacológico , Iridociclitis/patología , Iridociclitis/virología , Queratitis Herpética/diagnóstico , Queratitis Herpética/patología , Queratitis Herpética/virología , Polirribonucleótidos/uso terapéutico , Conejos , Simplexvirus/aislamiento & purificación , Factores de Tiempo
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