[Effect of bonafton on the formation of specific suppressor cells]. / Vliianie bonaftona na formirovanie spetsificheskikh kletok-supressorov.

Administration of an antiviral agent bonafton (1.5 mg/kg, intraperitoneally) for 5 days to mice immunized with a supraoptimal dose of ram erythrocytes (5 X 10(9)) was followed by inhibition of suppressor-cell induction in the animal spleen. An adoptive transfer of the splenic cells of these mice to syngeneic recipients caused in the latter less specific inhibition of humoral and cellular immune responses than it was during the use of splenocytes from hyperimmunized donor mice not receiving bonafton. The inhibitory effect of the drug was more manifest toward the suppressor-cells of the delayed-type hypersensitivity than the cells suppress antibody formation.

[Immunostimulating effects in the body induced by bonafton]. / Immunostimuliruiushchie éffekty, vyzyvaemye v organime bonaftonom.

Study of the primary immune response in CBA mice which were injected with bonafton (1.5-3 mg/kg i.p.) for 3 days has revealed stimulation of antibody formation. The maximal effect as regards the humoral immune response has been recorded on the drug use in a dose of 2 mg/kg. It has been discovered that bonafton (1-3 mg/kg) also activated the cell immune response--delayed type hypersensitivity.

[Electron microscopic studies of experimental staphylococcal infections in mice as chemotherapeutic models]. / Elektronno-mikroskopicheskie issledovaniia éksperimental'nykh stafilokokkovykh infektsii myshei kak khimioterapevticheskikh modelei.

Study of ultrastructural changes in the brain and renal tissues has shown that both intracerebral and intraperitoneal administration of staphylococcus in low infecting doses leads to the development in the brain and renal tissues of acute purulent inflammation, with a dramatic growth of infectious process and involvement of all parts of the organs under consideration. The presence in the brain tissues and in its meninges of inflammatory pyonecrotic foci might attest to the necrotic purulent encephalomeningitis, whereas the presence in the cortex and renal medullary substance of histiolymphocytic infiltration and foci of necrosis might be evidence of necrotic glomerulonephritis of bacterial etiology.

[Activity of di-N-hydroxyquinoxaline and depot-sulfanilamide derivatives in experimental NAG infection]. / Aktivnost' proizvodnykh di-N-oksikhinoksalina i depo-sil'fanilamidov pri éksperimental'noi NAG-infektsii.

In experiments in vitro dioxidineeee was highly effective as regards all the test cultures of NAG-vibrios. The MTC ranged within 1 to 62 micrograms/ml. Bactericidal action of the drug became manifest at concentrations from 4 to 250 micrograms/ml. The derivatives of di-N-oxide quinoxaline, dioxidin and quinoxidine exerted a chemotherapeutic effect and sterilizing action in experimental NAG-infection. The action of the drugs was potentiated upon combined use with lysozyme. As far as depo-sulfanilamides are concerned, sulfalenee was little active, while sulfamonomethoxine ineffective in experimental NAG-infection.

[Effect of riodoxol on herpes simplex virus morphogenesis in experimental eye infection]. / Vliianie riodoksola na morfogenez virusa gerpesa prostogo pri éksperimetal'noi infektsii glaz.

The effect of riodoxol on herpes simplex type 1 viruses was studied. It was shown to affect multiplication and maturation of the virus as manifested in the appearance of virions with incomplete nucleoid structure and long-term presence of virions in cytoplasmic vacuoles in cells. Submicroscopic changes suggest a dual effect of riodoxol on herpes simplex virus: on the DNA replicative cycle and on the stage of late maturation of virus at the time of its release from the nucleus.'

[Pharmacokinetics and antiviral activity of riodoksol in an ointment and in ophthalmic drug films in ocular herpes]. / Farmakokinetika i protivovirusnaia aktivnost' riodoksol v mazi i glaznykh lekarstvennykh plenkakh pri oftal'mogerpese.

A study was made on the pharmacokinetics in rabbit eye tissues of a new antiviral drug riodoksol in the form of ointment and biosoluble eye films. The pharmacokinetics of the drug was studied in eye tissues of normal rabbits and in those infected with herpes simplex virus. It was disclosed that four-fold application of 0.25% ointment produced the therapeutic concentration of the drug only in the cornea. Application of eye films made it possible to attain the therapeutic concentrations of riodoksol in the cornea and, within the first 3 hours, in the iris and humor of the anterior chamber. No differences were found in the drug concentrations in the tissues of intact and infected animals. Appraisal of the therapeutic efficacy of riodoksol regimens devised in experimental surface herpetic keratitis of rabbits has shown an adequacy of a single administration of eye films containing 0.5 mg of the substance and four-fold application of 0.25% ointment.

[Effect of dioxidine on DNA and RNA synthesis in Staphylococcus aureus]. / Vliianie dioksidina na sintez DNK i RNK u zolotistogo stafilokokka.

The effect of dioxidin on DNA and RNA synthesis by Staphylococcus aureus was studied with the use of labeled precursors and evaluated from the kinetics of DNA and RNA accumulation by the culture. It was shown that dioxidin inhibits DNA synthesis by Staphylococcus aureus cells, with the synthesis of RNA being almost not affected. The main effect manifests within the first hour of the drug interplay with the microbial cell, it is reversible and appears to be realized by the mechanisms of DNA synthesis regulation. Dioxidin does not form complexes or cross-linkages with the DNA molecule. The action of dioxidin on the microbial cell manifests in the derangement of the activity and biosynthesis of extracellular DNase.

[Electron microscopic study of the antiviral action of bonafton in experimental influenza infection]. / Elektronno-mikroskopicheskoe izuchenie protivovorusnogo deistviia bonaftona pri éksperimental'noi grippoznoi infektsii.

Action of bonaphthon on influenza A virus was studied in experimental influenzal pneumonia of mice. Bonaphthon was shown to lower 1.5-2 fold the reproduction of influenza virus in pulmonary tissue as compared with control. It is suggested that the mechanism of bonaphthon action may be due both to the inhibition of the synthesis of virus-specific membrane protein by the cells and to disordered transport of this polypeptide to the cell membranes. Bonaphthon proved to exert the most favorable effect in the course of its preventive administration in the early stages of infection.

[Basic trends and the prospects for creating new synthetic chemotherapeutic preparations]. / Osnovnye napravleniia i perspektivy sozdaniia novykh sinteticheskikh khimioterapevticheskikh preparatov.

Chemotherapy and chemoprophylaxis play a significant role in control of various infectious diseases. The use of chemotherapeutic drugs is associated with a number of difficulties, such as development of drug resistance in pathogenic microorganism during the treatment, possible toxic effects of drugs on their prolonged use, inefficiency of chemotherapy in bacteria carriers, etc. In spite of the achievements in chemotherapy of acute bacterial infections, tuberculosis, lepra, mycoses, protozoal infections, it is necessary to have available new drugs for the treatment of these diseases. The achievements in chemotherapy of viral infections are relatively modest. However, therapy of such infections is of great importance for medicine. Highly effective broad-spectrum antiviral agents may play a significant role in the control of widely spread viral diseases of man and cattle. Such drugs will be of great significance in prevention of complications in persons with viral infections and studying the diseases of supposed viral etiology. For the successful solution of the problems of chemotherapy, a proper strategy in the development of the research work in this field is of importance.

[Mechanism of the antiherpetic action of bonafton]. / O mekhanizme protivogerpeticheskogo deistviia bonaftona.

The mechanism of antiherpetic action of bonaphthon was studied in experimental herpetic keratitis of rabbits infected with herpes simplex type I virus (Koptev and IC strains). Electron microscopy demonstrated that the drug inhibits herpes virus production and proliferation of virus infection because of partial impairment of the nucleocapsid "assembly" in the cell nucleus. It is assumed that the action of bonaphthon may be consequent on the inhibition of the cell synthesis of cytoplasmatic proteins incorporated into the capsids and on the derangement of the transport of virus capsid components to the cell nucleus, where these components are assembled. It has been shown that the intensity of virus reproduction in the cells decreases threefold under the effect of bonaphthon as compared to control.

[Rat postnatal development after bonafton exposure]. / Postnatal'noe razvitie krys posle vozdeistviia bonaftona.

The first generation progeny of rats received days 10-13 of pregnancy a new antiviral drug bonaphthon (400 mg/kg) which exerts a toxic effect on females. The progeny did not show postnatal death or reduction of the life span. Moreover, no impairment of muscle work capacity, basal metabolism, cardiovascular system, peripheral blood parameters, or changes in the function of organs and systems were recorded. Morphological and functional deviations in the liver of 2-month-old progeny were unstable and got repaired by 3 months of age.

[Pyrrolo(3,2-d)pyrimidines as potential antitumor agents]. / Pirrolo(3,2-d)pirimidiny kak potentsial'nye protivoopukholevye agenty.

Antibacterial and antitumor properties of pyrrolo (3,2-d) pyrimidines having diverse substituents in the second, fourth and sixth position were investigated. Forty-four compounds were examined in vitro and 20 in vivo. A number of the derivatives were shown to inhibit the growth of M. tuberculosis H37Rv and lactic acid bacteria Lactobacillus casei 7469. Antibacterial activity depends on the character of the substituents in positions 2, 4 and 6. The tested compounds when administered per os to mice with sarcoma 180 (a solid variety) proved several dozen times less toxic than 6-mercaptopurine. Some of them inhibited the tumour growth up to 50%. The data obtained in vitro experiments indicate that the mechanism of the antitumour action of pyrrolo (3,2-d) yrimidines from that of 6-mercaptopurine.

[Effect of quinolaline di-N-oxide derivatives on the DNAse and plasmocoagulase of Staphylococcus aureus]. / Vliianie proizvodnykh di-N-okisi khinoksalina na DNK-azu i plazmokoagulazu zolotistogo stafilokokka.

The effect of the di-N-oxide quinoxaline on the activity and biosynthesis of DNA-ase and plasmocoagulating properties of the Staphylococcus aureus, strain Zhaev, was studied. The highest action in respect to DNA-ase of the Staphylococcus is shown to display dioxydine (1,4-di-N-oxide of 2,3-dioxymethylquinoxaline). Under its effect there takes place a significant fall of the DNA-ase activity and the plasmocoagulating properties of the staphylococcus. In cultures treated with dioxydine or its biologically active analogues the ability to biosynthetize DNA-ase with subsequent cultivationon on a medium containing no compounds is not restored. A possible mechanism of action produced by the study drugs is suggested.