[Effect of Mycobacterium tuberculosis on activity of lysosomal enzymes in mouse peritoneal macrophages]. / Vliianie mikobakterii tuberkulëza na aktivnost lizosomalnykh fermentov peritonealnykh makrofagov myshei.

The studies of the effects produced by M. tuberculosis various strains on the activity of lysosomal enzymes in peritoneal mouse macrophages demonstrated multidirectional influence of the bacilli. Non-sedimentary activity rose in matrical enzymes indicating lysosomal membranes instability due to M. tuberculosis infection followed by hydrolase activation and hydrolases escape into the cytosol. An inhibiting action of pathogenic mycobacteria on lysosomal proteases is suggested.

[Biotransformation of the 14C-hydrogenated analog of phenazepam in inbred mice]. / Biotransformatsiia 14C-gidrirovannogo analoga fenazepama v organizme myshei inbrednykh linii.

The elimination of 14C-hydrogenated analogue of phenazepam and its metabolites was studied in inbred C57B1/6 (B/6), BALB-c (C) and CBA mice. The kinetics of two-phase elimination of 14C-compounds with urine and feces was similar in all the above mouse strains. The excretion was realized mainly with feces, exceeding elimination with urine 5-6-fold in B6 mice and 10-11-fold in C and CBA mice. Some interstrain quantitative differences in metabolite composition were found. No metabolite was detected whose concentration would indicate a predominating direction of biotransformation of 14C-hydrogenated phenazepam analogue or distinguish it from other mouse strains. In the organism of mice, 14C-hydrogenated phenazepam analogue undergoes active aromatic hydroxylation and methoxylation via heterocycle (and possibly via chlorine-containing ring). At the same time dehydrogenation of 14C-hydrogenated phenazepam analogue molecule was not recorded.

[Distribution of the 14C-hydrated analog of phenazepam in the organs and tissues of mice]. / Raspredelenie 14C-gidrirovannogo analoga fenazepama v nekotorykh organakh i tkaniakh myshei.

The absorption kinetics of hydrated phenazepam analog into the liver, spleen, brain, kidney, blood, lungs, heart, skeletal and fat tissues is studied at 0.25-24 hour intervals after its intraperitoneal (i/p) administration to mice. Drug concentration in the above mentioned organs was maximal 0.5-1 hour later. The decrease of the drug and its metabolite level in the organs under study is a biexponential process, consisting of "quick" (1-6 hours) and "slow" phases. The rate of absorption of hydrated phenazepam analog into the organs and tissues and its elimination is lower than that of phenanzepam.