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Reactions of amphotericin B, a polyenic macrolide antibiotic, with aromatic aldehydes and H3PO2 resulted in formation of its new hydrophosphoryl derivatives. Physico-chemical and biological properties of the compounds were investigated. The biological studies showed that the hydrophosphoryl derivatives of amphotericin B were low toxic and had antifungal and antiviral activities.

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Reactions of levorin, a polyenic macrolide antibiotic, with aromatic aldehydes and hypophosphorous acid resulted in formation of its amino phenylphosphonium derivatives. Physicochemical and biological properties of the derivatives were studied. The levorin amino phenylphosphonium derivatives were shown to be low toxic and have antifungal and antiviral activities.

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Anti-influenzal action of bacterial and pancreatic RNAases was studied. It was shown in ovo that the RNAases had distinct virus inhibiting activity with respect to various strains of the grippe A virus and did not practically differ by their activity from remantadin but unlike it had inhibitory action on the grippe B virus. The anti-influenzal activity of bacterial RNAase in contrast to pancreatic one was detected not only in experiments with developing chick embryos but also in albino mice with lethal influenzal infection. The index of the animal protection by the preparation amounted to 54-90 per cent depending on the virus infecting dose and RNAase administration route, the lifespan of the animals being increased by 2.4 to 3.8 days. It was shown that the anti-influenzal effect of bacterial RNAase correlated with high levels of the exogenic enzyme in blood of the animals after the preparation intravenous administration. Elimination of RNAase was observed already within the first 4 hours after the experiment start. Intranasal administration allowed to increase the residence time of RNAase in blood up to 8 hours at the account of its gradual absorption from the administration site and the preparation availability increased more than 2-fold. The results provided the basis for recommending the intranasal route of bacterial RNAase administration for use in further investigation of RNAase antiviral activity.

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Roseofungin, a pentaen was used as an example in investigation of certain characteristics of inactivation of polyenic antibiotics. An inactivation product of the antibiotic having no antiviral or antimycotic activity was isolated by TLC and column chromatography on Sefadex LH-20. UV, IR and EPR spectroscopy showed that this product was cys-tetraen without conjugation of the lactone carbonyl to the polyenic system.

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The antiinfluenza activity of roseofungin, a polyenic macrolide antibiotic was studied in vitro on surviving fragments of the chick embryo chorionallantoic membranes and in ovo on growing chick embryos. It was shown that the antibiotic activity against influenza A and B viruses was sufficiently high. The activity of roseofungin against influenza A virus did not differ from that of remantadin, the most active inhibitor of influenza virus reproduction. However, the activity of roseofungin against influenza B virus was an advantage of this antibiotic over remantadin, which had practically no effect on this virus type. A statistically significant protective effect of roseofungin (p less than 0.05) was shown on the animals with experimental influenza. The study on the antiviral activity of roseofungin against the DNA-containing variolovaccine virus revealed that it markedly inhibited the plague reduction. Roseofungin had a pronounced inhibitory effect on cell neoplastic transformation induced by the RNA-containing oncogenic virus of Rous sarcoma.

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Clear antiviral activity of carbonyl-conjugated pentaene macrolides, such as flavofungin, mycothicin, brunefungin and flavopentin was shown on models with infectious and oncogenic viruses. The antibiotics were active against influenza A and B virus. The effect was most pronounced in the in vitro and in ovo systems. On a model of experimental influenza infection of mice with the lethal outcome, antiinfluenzal activity of flavofungin was comparable to that of remantadin. However, unlike the latter one flavofungin and brunefungin inhibited the growth of influenza B virus. The drugs had a pronounced inhibitory effect on variolavaccine virus and prevented formation of foci of cell neoplastic transformation infected with various strains of Rous sarcoma virus.

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The inhibitory effect of flavopentin was shown on the models of infectious and oncogenic viruses. Flavopentin is a polyenic antibiotic belonging to pentaenes. The characteristic features of the polyene interaction with the plasma membrane of the host cell were defined with the use of the luminescence analysis, when the antibiotic was applied with the therapeutic or prophylactic purposes in experimental influenzal infection.

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It was shown experimentally that polyenic antibiotics, i. e. amphotericin B and sodium levorin markedly increased the specific immunogenic properties and interferonogenic activity of inactivated influenza virus vaccine prepared with various methods from highly reproductive recombinants. The rate of pneumonia and death from influenza among the vaccinated mice treated with inactivated influenza virus vaccine and one of the polyenic antibiotics was lower than that among the animals treated with the vaccine alone (P less than 0.05). Correlation between the increase in the immunological response, the decrease in the virus reproduction rate in the lungs and addition of the antibiotics into the vaccine was also observed. It is recommended that inactivated influenza virus vaccine be used in conjunction with polyenic antibiotics.

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