[Prospects for improvements of pharmacologic radioprotective agents]. / Nekotorye perspektivy sovershenstvovaniia farmakologicheskikh sredstv protivoluchevoi zashchity.

For solving the problems of medicamentous prevention and treatment of radiation lesions it seems reasonable to change from the empirical methods of anti-radial agent search to the rational one based on the evaluation of potential capacity of the agents to start some mechanisms of radioprotective effect realization. Several groups of such mechanisms were selected including the universal general biologic connected with ADP-ribosylation and nitrogen oxide metabolism. It is proved that on the base of the chosen approaches it is possible to improve some significant characteristics of radioprotectors and to obtain the polyfunctional radioprotective agents and prescriptions.

[A new approach to the prevention and treatment of lesions caused by bacterial toxins: prospects for using inhibitors of ADP ribosylation]. / Novyi podkhod k profilaktike i lecheniiu porazhenii bakterial 'nymi toksinami: perspektivy primeneniia ingibitorov ADF-ribozilirovaniia.

The damaging action of a number of bacterial toxins is determined by their capacity for blocking the specific functions of regulatory proteins of eukaryotic cells by ADP-ribosylation. Experiments, made with the use of type B botulinic toxin and 3,N-butyrylaminobenzamide as an example, have demonstrated that specific ADP-ribosylation inhibitors are capable of making up a new group of highly active antagonists of microbial toxins.

[Experimental study of radiation protective efficacy of Vinca alkaloid drugs]. / Eksperimental'noe izuchenie radiozashchitnoi éffektivnosti lekarstvennykh preparatov na osnove alkaloidov vinkovoi gruppy.

In experiments with rats and dogs exposed to whole-body nonlethal and lethal gamma-radiation (2; 2,9 or 7.5 Gy) the radioprotective efficacy Vinca alkaloids drugs was investigated. It has been shown that enterally administered Vincanor (10 mg/kg over a three-day period) increased the radioresistance of animals. The prolonged radioprotective effect of Vincanor are discussed with regard to the phenomenon of sequential partial DNA synthesis inhibition in radiosensitive tissues.

[The antiviral activity of inhibitors of ADP ribosylation in experimental alpha- and bunyavirus infections]. / Protivovirusnaia aktivnost' nekotorykh ingibitorov ADF-ribozilirovaniia pri éksperimental'nykh al'fa- i bun'iavirusnykh infektsiiakh.

The prophylactic and therapeutic effects of ADP-ribosylation inhibitors, 3,N-acetylaminobenzamide and 3,N-butyrylaminobenzamide, were studied in mice inoculated with an alphavirus or a bunyavirus. Both drugs were shown to have high levels of antiviral activity when given as a single subcutaneous injection in a dose of 10 mg/kg while increasing the number of injections did not increase their efficacy or might even decrease it.

[The pharmacological mechanisms of the radioprotective effect under whole-body conditions and the prospects of the search for radioprotectors]. / Farmakologicheskie mekhanizmy radiozashchitnogo éffekta v usloviiakh tselostnogo organizma i perspektivy izyskaniia radioprotektorov.

On the basis of the current views of the pharmacological agents action and the analysis of the structural and functional mechanisms of the radioprotection realization a unitary hypothesis of the radioprotective effect development has been formulated. Three stages of its development in animals and humans have been distinguished. The proposed hypothesis allows to substantiate a strategy of the search for new antiradiation drugs.

[An experimental study of the amides of aromatic carboxylic acids as radiosensitizing agents]. / Eksperimental'noe izuchenie amidov aromaticheskikh karbonovykh kislot v kachestve radiosensibiliziruiushchikh sredstv.

In experiments with mice a study was made of the radiosensitizing efficacy of 10 aromatic carbonic acid amides, benzene, naphthalene, pyridine and quinoline derivatives. It has been found, for this group of substances, that there is a direct correlation between the ability of the substance to reduce the splenic endocolonies production and the inhibitory activity with regard to poly(ADP-ribose) polymerase of thymocyte nuclei. Within the group of substances under study, new agents are found and described and new relationships are revealed between their chemical structure and biological activity.

[An experimental study of ADP-ribosylation inhibitors as anti-influenza agents]. / Eksperimental'noe izuchenie nekotorykh ingibitorov ADF-ribozilirovaniia v kachestve protivogrippoznykh sredstv.

Tri-substituted benzamide derivatives are described as a new class of antiviral drugs. Three compounds (3, N-acetylaminobenzamide, 3, N-butyrylaminobenzamide, and 3-methoxybenzamide) protected mice inoculated with influenza type A virus. 3, N-acetylaminobenzamide was found to be most active. It is suggested that the antiviral effect may be due to the specific inhibitory action of these compounds on NAD(+)-dependent ADP-ribosylation.

[Inhibitors of ADP ribosylation as antiviral agents: an experimental study in a model of HIV infection]. / Ingibitory ADF-ribozilirovaniia kak protivovirusnye sredstva: éksperimental'noe izuchenie na modeli VICh-infektsii.

The paper deals with further search for substances modifying metabolic processes, changing the conditions of virus existence in the host cell and, consequently, possessing a certain antiviral activity. The antiviral effects of aromatic carbonic acids amides including trisubstituted benzamides and nicotinamide were tested. Five out of 8 substances tested possessed antiviral activity which might be due to their capacity to inhibit the activity of the enzymes of ADP-ribosylation. By blocking cellular processes of ADP-ribosylation, the substances under study depressed DNA capacity for reparation, inhibited differentiation and transformation of cells, i.e. had an indirect effect on reproduction of viruses. The universal nature of the processes coursing with participation of NAD(+)-dependent ADP-ribosylation suggests that the range of antiviral activity of inhibitors of mono- and poly-ADP-ribosylation would not be limited to HIV infection but would be rather wide.

[Radioprotective activity of complexes of copper, cobalt and zinc with substituted acylhydrazones]. / Radiozashchitnaia aktivnost' kompleksov medi, kobal'ta i tsinka s zameshchennymi atsilgidrazonami.

Acylhydrazone metal complexes belong to a new class of radioprotective agents that have a cytostatic effect increasing, in some cases, the survival rate of irradiated animals by 40-60 per cent compared to irradiated controls. The most active drugs are hypotoxic and applied in much lower doses than ordinary S-containing radioprotective agents to achieve the same protective effect.

[Radioprotective efficacy of acyl hydrazones]. / Radiozashchitnaia éffektivnost' atsilgidrazonov.

As was shown in experiments with rats and mice some acyl hydrazones have a pronounced radioprotective effect. The protective efficiency makes 40-55 per cent with the preparation doses of 1-10 mg/kg. The toxicity of hydrazones is 2 g/kg which is lower, than that of the known sulfur-containing agents and substituted indolylalkylamines. The radio-protective efficiency of the drug depends on its complex-forming ability.