[EXPERIMENTAL STUDY OF SPECIFIC ACTIVITY OF 1.3-DIAZINON-4 COM- POUND PYaTd1 DERIVATIVE IN VIVO].

AIM: Study anti-leprosy activity of.a 1.3-diazinon-4 compound derivative under the labora- tory code PYaTd1 on the model of intra-plantar infection of mice and evaluate the character of its antibacterial effect. MATERIALS AND METHODS: Study of specific activity was carried out in vivo on the experimental model of leprosy, proposed by Shepard C.C., that assumes execution of intraplantar infection of mice with a suspension of mycobacteria, produced from lepromas or autopsy tissue of a non-treated leprosy infected, or from tissues of experimental mice, previously infected with Mycobacterium leprae from non-treated patients. The study was carried out on 120 CBA line-mice infected with M.leprae (VIII passage) from patient M; Dapsone and PYaTdl compound were administered to animals next day after the infection with forage at a dose of 25 mg/kg for 4.5, 6, 9 and 11 months. The mice were split into 3 groups: control (infected.without treatment), com- parison (infected, receiving.dapsone), experimental (infected, receiving PYaTdl). After.the control term the mice were euthanized under chloroform anesthesia. Suspensions for quantification of mycobacteria were prepared from paw pads. Smears were stained by Ziehl-Nilsson. RESULTS: After 4.5 months the intensity of infect reproduction under, the effect of dapsone and PYaTd1 was reduced compared with control by 18 - 25 times. After a 6-mont course - by 50 - 75% and after 9 months - by 85 - 90%. After 11 months in mice that had received PYaTd1, an intensive suppression of microorganism reproduction as observed: the yield in paws was 70 times lower than in control. In the group that had received dapsone, a reduction of the number of mycobacteria by 20 - 25 times was detected, it was significantly less effective than under the conditions of PYaTd1 admnistration. CONCLUSION: A novel 1.3-diazinon- 4 derivative under the code PYaTd1 can actively supress reproduction of-M. leprae, that gives evidence regarding its specific anti-mycobacterial activity and determines perspectives of its further studies.

[Chronobiological aspects of the action of diaminodiphenylsulfone on hematological mice induces in summer and winter seasons ]. / Khronobiologicheskie aspekty vliianiia diaminodifenilsul'fona na gematologicheskie pokazateli u myshei v letnii i zimnii sezony goda.

Mice experiments were made to study effects of diaminodiphenylsulphone (DDS)--basic antileprous drug--on circadian rhythms of hemoglobin levels, counts of red cells and leukocytes. The time of the drug administration varied within the day while seasons of the year were two--winter and summer. Blood components were studied with unified methods. The results of the study showed that DDS has significant effects on the structure of circadian rhythms of the above blood components. These effects correlate with the season of the year and time of DDS administration.

Effects of horseradish root on functional activity of phagocytes, total blood cell count, and state of the liver in mice with experimental leprosy.

Therapy of experimental leprosy with dried and grated horseradish root administered perorally in a dose of 300 mg/kg mixed food and treatment with purified horseradish peroxidase increased myeloperoxidase activity of blood neutrophils, enhanced antimicrobial functions of phagocytes, decreased leukocytosis, normalized total blood cell count, and produced no adverse effects on the functional state of the liver in mice.

Effects of horseradish root on functional activity of phagocytes, total blood cell count, and state of the liver in mice with experimental leprosy

Therapy of experimental leprosy with dried and grated horseradish root administered perorally in a dose of 300 mg/kg mixed food and treatment with purified horseradish peroxidase increased myeloperoxidase activity of blood neutrophils, enhanced antimicrobial functions of phagocytes, decreased leukocytosis, normalized total blood cell count, and produced no adverse effects on the functional state of the liver in mice.

Effect of peroxidase in complex with basic antileprosy drugs on liver, blood, and functional activity of phagocytes in mice with experimental leprosy.

Therapeutic effect of lyophilized horseradish peroxidase in complex with the basic antileprosy drugs diaminodiphenylsulfone and rifampicin was studied in experimental leprosy. Oral therapy with drug complexes was more effective than monotherapy. Treatment with drug combinations activated myeloperoxidase in blood neutrophil, produced an antiinflammatory effect, stimulated cell immunity, and had no toxic effect on mouse liver.

Effects of peroxidase therapy on functional state of the liver and phagocytes and blood cell counts in mice with experimental leprosy.

We studied the effects of long-term therapy with horseradish peroxidase administered orally to mice with experimental leprosy. Horseradish peroxidase stimulated phagocyte myeloperoxidase activity that correlated with their functional activity, reduced leukocytosis, and produced no adverse effects on the liver.