[Chemical modification of an antineoplastic antibiotic bleomycetin by the C-end fragment].

Bleomycetin, an antitumor antibiotic, was subjected to chemical modification by the C-end fragment i.e. the residue of 3-[(4-aminobutyl)amino]propylamine (spermidine++) with acylation, carbamoylation and reducing alkylation, which yielded its new semisynthetic derivatives.

[Production and antineoplastic activity of new asymmetric azines on the rubomycin base].

New alkulidene hydrazones of rubomycin (daunorubicin) with the linear or branched chain of the carbon atoms were studied: rubomycin 13-(hexylidene-2")-hydrazone, rubomycin 13-(heptylidene-3")-hydrazone and rubomycin 13-(4"-methylpentylidene-2")-hydrazone. Alkylidene hydrazones of the formamidine derivatives were also studied: 13:cyclohexylidene hydrazone of 3'-desamino-3'-dimethylformamidine rubomycin and 13-(5"-oxypentyliden-2") hudrazone of 3'-desamino-3'-dimethylformamidine rubomycin. The latter two alkylidene hydrazones were modified twice.

[Study of toxicity and antineoplastic activity of 14-substituted derivatives of rubomycin and carminomycin].

Toxicity and antitumor activity of five derivatives of rubomycin and carminomycin were studied in animals. The derivatives were prepared by modification of the methyl C-14 group. These were the following: 14-chlorrubomycin, 14-chlorcarminomycin, 14-salicyloyloxyrubomycin, 14-salicyloyloxycarminomycin and 14-quinaldinoyloxyrubomycin.

[Glycopeptide antibiotics: eremomycin, vancomycin, and teicoplanin. Comparison of several parameters of pharmacokinetics and antimicrobial activity].

Pharmacokinetic parameters of eremomycin (Institute of New Antibiotics, the USSR Academy of Medical Sciences), teichoplanin (Lepetit) and vancomycin (Eli Lilly) were compared after their intravenous administration to rats in the same dose of 50 mg/kg. It was shown that the area under the concentration time curve of eremomycin was 2 times smaller than that of teichoplanin and 6 times larger than that of vancomycin. The mean retention time of eremomycin was close to that of teichoplanin and 1.

[Eremomycin--a new antibiotic of the polycyclic glycopeptide group].

Eremomycin is a novel antibacterial antibiotic. It was isolated at the Institute of New Antibiotics, the USSR Academy of Medical Sciences from the culture fluid of actinomycete INA-238. By its physico-chemical and biological properties the antibiotic was classified as belonging to the group of polycyclic glycopeptides.

[Preclinical toxicological study of the new antibiotic eremomycin. Chronic toxicity and effect on intrauterine development of rats].

Toxicity of eremomycin was studied after its multiple parenteral administration to albino rats, guinea pigs and dogs in doses equivalent by the body surface to the daily doses for humans i. e. 1 and 3 g.

[Preclinical toxicological study of the new antibiotic eremomycin. Its acute toxicity for laboratory animals].

Eremomycin is relatively low toxic. LD50 of eremomycin on its intravenous administration to albino mice amounted to 1760 (1460-2130) mg/kg. It is 2.

[Toxicity of rubomycin 13-cyclohexylidene hydrazone].

The systemic effect and toxicity of rubomycin 13-cyclohexylidene hydrazone (RCH) were studied in comparison to those of rubomycin on noninbred albino mice. The drugs were used intravenously in single doses or a course consisting of 5 injections. When used intravenously in a single dose RCH was 2 times less toxic than rubomycin.

[Antitumor activity of doxorubicin in respect to solid tumors in mice].

Antitumor activity of doxorubicin, an antibiotic prepared in the USSR was studied with respect to 4 solid tumors of mice: lymphosarcoma LIO-1, sarcoma 180, pregastric cancer OZh5 and melanoma B-16. Doxorubicin showed high antitumor activity against lymphosarcoma and sarcoma 180. However, it was somewhat lower than that of rubomycin and carminomycin.

[Toxicity and antimicrobial properties of the new aminoglycoside antibiotic 535].

LD50 of antibiotic 535 (3'-desoxykanamycin C) on its intravenous, subcutaneous and oral administration to albino mice was 225, 1150 and at least 5000 mg/kg respectively. After a single subcutaneous administration to rabbits in a dose of 10 mg/kg antibiotic 535 was rapidly absorbed and detected in the blood and organs of the animals for 24 hours. The antibiotic was mainly excreted with the urine.

[Space-occupying masses in the right atrial cavity. Findings in segmental echo scanning].

A total of 1665 patients were examined with the aid of two-dimensional echocardiography scanning. Of these, 3 patients had sizable formations in the right atrium. During scanning, the sizable formations were recorded within the planes of echolocation, whereas the use of one-dimensional echocardiography enabled a sizable formation to be detected but in one patient.

[Antitumor activity of doxorubicin in the treatment of hemocytoblastosis La and various ascites tumors in mice].

Antitumor activity of doxorubicin made in the USSR was studied on mice in respect to three transplantable tumors (lymphadenosis NK/LI, sarcoma 37 and Ehrlich's carcinoma) and hemocytoblastosis La. Doxorubicin injected intravenously 4 times was shown to be highly active against the above ascites tumors. The highest inhibitory effect of doxorubicin was observed in respect to the development of Ehrlich's carcinoma.

[Toxicity, pharmacokinetics and pharmacodynamics of Soviet-made doxorubicin].

The LD50 of doxorubicin, prepared at the Institute of New Antibiotics of the Academy of Medical Sciences of the USSR was 4.6, 12.5, 13.

[Study of the toxicity of carminomycin 13-cyclohexylidenhydrazone].

The systemic effect and toxicity of carminomycin 13-cyclohexylidenhydrazone (CCH) were studied on noninbred albino mice in comparison to carminomycin. The preparation was administered intravenously and orally. It was shown that CCH was 1.

[Synthesis and antitumor properties of carminomycin 13-cyclohexylidenhydrazone].

Carminomycin 13-cyclohexylidenhydrazone (CCH) was prepared by interaction of carminomycin 13-hydrazone with cyclohexane. The antiblastomic properties of CCH were studied on mice with transplantable tumors. The preparation was administered intravenously or orally.

[Acute toxicity of the N-acyl derivatives of carminomycin and rubomycin].

Synthesis of 2 new N-acyl derivatives of carminomycin and rubomycin (N-L-leucylcarminomycin and N-sarcolysylrubomycin) is described. Acute toxicity of the new and 4 known N-acyl derivatives: N-acetylcarminomycin, N,L-alanylcarminomycin, N-D-phenylalanylcarminomycin and N-D-phenylalanylrubomycin was studied on albino mice. It was shown that the N-acyl derivatives of carminomycin and rubomycin had lower acute toxicity than the initial drugs.

[Synthesis of rubomycin 13-tert-butoxycarbonylhydrazone and the study of its antitumor action].

13-Tert-butoxycarbonylhydrazone of rubomycin was prepared on interaction of rubomycin with tert-butoxycarbonylhydrazine. The new compound showed a high antitumor activity with respect to lymphosarcoma LIO-1 and Garding-Passey melanoma. The compound had no advantages over the initial rubomycin in the treatment of these tumors, was inferior to rubomycin with respect to its activity against leukemia P-388 and unlike rubomycin had practically no effect on leukemia L-1210.

[Synthesis, toxicity and antitumor action of carminomycin azine (carminazine)].

Carminomycin azine designated as carminazine was prepared by condensation of carminomycin with hydrazine hydrate. It was shown in the experiments on mice that the toxicity of carminazine was 2 and 7 times lower than that of carminomycin on its intravenous and oral administration respectively. The effect of both drugs on hemopoiesis of the mice was similar.

[Pharmacokinetics of tobramycetin and gentamycin and the mechanism of their elimination by the kidneys].

After subcutaneous administration of tobramycetin (tobramycin) to rabbits in single doses equivalent to the daily therapeutic doses for humans calculated for the body surface and those exceeding them by 3 times, the antibiotic was rapidly absorbed into the blood and detected within 30 and 72 hours respectively. Tobramycetin penetrated into all organs of the animals. Its highest levels were found in the kidneys and the lowest in the brain tissue.

[Measurement of the electrical impedance of the chest cavity under physical load for the detection of left ventricular insufficiency in ischemic heart disease].

The suggested index of transthoracic impedance time course during loading (20 and 50 V) correlates significantly with the complex index of phase analysis (ratio of the duration of the tension and ejection periods), the stroke and cardiac indices and the QAd index determined by rheography and, at the same time, it is more informative. Its highly significant connection with tolerance to physical load is also noted.

[Effect of Soviet bleomycin-bleomycetin on the body of animals in multiple parenteral administration].

Toxicity of bleomycetin was studied on 3 animal species (rats, rabbits and dogs). The antibiotic was administered intramuscularly and intravenously in various doses for a prolonged period of time. The death of the rats, rabbits and dogs treated with repeated lethal doses of bleomycetin was due to its toxic effect on the kidneys and probably lungs.

[Toxicity, pharmacokinetics and pharmacodynamics of the Soviet bleomycin, bleomycetin, in a single administration to laboratory animals].

Toxicity of bleomycetin (bleomycin A2) administered intravenously, intraperitoneally, subcutaneously or intramusculary in a single dose to animals was almost identical. On its oral administration bleomycetin was 10--14 times less toxic than on its parenteral use. Rats were somewhat less sensitive to bleomycetin than mice.