[EFFECTIVENESS OF FULLERENE-(TRIS-AMINOCAPRONIC ACID) HYDRATE IN THE MODEL OF EXPERIMENTAL VIRAL-BACTERIAL PNEUMONIA OF MICE].

AIM: Study the effectiveness of the substance and various drug formulations of fullerene-(tris-aminocapronic acid) hydrate (FTAAH onwards) in the model of experimental viral-bacterial pneumonia of mice. MATERIALS AND METHODS: BALB/c mice were infected with influenza virus A/California/04/2009 and subsequently infected with Staphylococcus aureus. The animals were treated after viral infection with the substance and various drug forms of FTAAH, as well as comparative preparations--oseltamivir and arbidol. Therapy effectiveness was evaluated by clinical indicators (survival, lifespan, animal mass decrease reduction), virological (virus titer), microbiological (density of bacteria in lungs) parameters, confirmed by pathomorphological characteristics of lungs. RESULTS: FTAAH therapy in injectable form was effective in the model of a combined viral-bacterial pneumonia of mice by all the studied criteria: treatment increased mice survival, reduced the decrease of their body weight, resulted in a reduction of virus titers and density of bacteria in lungs, that correlated with the data from morphological study and signs of bronchopneumonia resolution in mice. FTAAH therapy in rectal form depended on animal infection schemes, as well as preparation dose, increasing with its increase. CONCLUSION: FTAAH substance is effective in the model of experimental viral-bacterial pneumonia of mice.

[The antiretroviral agent Fullevir].

The antiretroviral properties of Fullevir (sodium salt of fullerenepolyhydropolyaminocaproic acid) manufactured by IntelFarm Co.) were studied in the human cell culture infected with human immunodeficiency virus (HIV). The agent was ascertained to be able to protect the cell from the cytopathic action of HIV. The 90% effective concentration (EF90) was 5 microg/ml. The 50% average toxic concentration was 400 microg/ml. Testing of different (preventive and therapeutic) Fullevir dosage regimens has shown that the drug is effective when used both an hour before and an hour after infection and when administered simultaneously with cell infection. The longer contact time for the agent with the cells increased the degree of antiviral defense. Co-administration of Fullevir and the HIV reverse transcriptase inhibitor Retrovir (azidothymidine) showed a synergistic antiretroviral effect. Thus, Fullevir may be regarded as a new promising antiretroviral drug for the treatment of HIV infection.

[Fullevir: in vitro and in vivo antiherpetic activity].

The antiherpetic properties of a fullerene derivative with aminocaproic acid (manufactured by Intelfarm Co. as Fullevir) were studied in in vitro (in sensitive cell cultures) and in vivo (on a murine model of experimental herpetic encephalitis) experiments. Fullevir was found to protect tissue culture cells from the cytodestructive action of herpes simplex virus type 1. It was estimated that ED50 = 5.3 microg/ml and ED90 = 29.1 microg/ml. The agent was most effective when it was administered before and 30 minutes after cell culture infection. The in vivo study established that Fullevir showed a significant protective effect in experimental herpetic encephalitis. The protection rates were 29.8% and 41.0% with the total doses of Fullevir of 500 mg/kg (p < 0.007) and 1000 mg/kg (p < 0.004), respectively. Thus, the in vitro and in vivo studies demonstrated the antiherpetic effect of a fullerene-aminocaproic acid complex (1-hydrofullereneaminocaproic acid, sodium salt) having the trade name Fullevir.