Inhibitory activity of palladium(II) and platinum(II) complexes with isoxazole and its derivatives

The investigation of the inhibitory activity on the membrane bonded ATP-ase of the M(L)₂X₂ complexes [where M = Pd(II), Pt(II); L = isoxazole(isox), 3,5-dimethylisoxazole(3,5-diMeisox), 3-methyl,5-phenylisoxazole(3-Me,5-Phisox), 3,5-diphenylisoxazole-(3,5-diPhisox), and 4-amino-3,5-dimethylisoxazole(4-ADI); X = Cl, Br] is reported. These results show that the complexes with isox and its methyl and phenyl derivatives have a much stronger inhibitory effect than the corresponding free ligands; in the 4-ADI compounds this activity drops. The Pd(II) complexes have a greater effect than the Pt(II) derivatives. The interaction occurs with SH groups and probably also with other active centers of the enzyme. These conclusions have been correlated with the E.S.C.A. spectra. These measurements show that the electron density of the complexes on the central metal ion and N_ring atom or N_ring and N-hexocyclic atoms on passing from chloride to bromide derivatives changes slightly.     

Co-operative response of chemically excitable membrane: I. Formulation: Unified theory of co-operativity

The lattice-model of Changeux, Thiery, Tung & Kittel (1966) was extended in order to examine the co-operative response of chemically excitable membrane and the exact mathematical correspondence to the Ising model was shown. In this model, two conformational states S and R with different affinities for the ligand are assumed to be accessible to each protomer, which is interacting with the nearest-neighbor protomers. The model is applicable to any kind of symmetrically interacting system consisting of oligomers and lattices and is an extension of previously proposed models of allosteric protein. It includes the model of Monod, Wyman, & Changeux (1965) and that of Koshland, Némethy & Filmer (1966) as the extreme cases of the oligomer. By assuming that a state-transition from S to R in a protomer is accompanied by a unit increase in conductance, the characteristics of dose-response curves of chemically excitable membrane are examined. The Hill's coefficient n_H of dose-response curve, the measure of the co-operativity, is shown to be proportional to the square of the mean fluctuation of the state function, the fraction of protomers in R state.     

Cytochemistry and ultrastructure of frog pancreatic exo- and endocrine epithelium under normal conditions]

The pancreatic epithelium of intact frog has been studied using morphometry, cytochemistry and electron microscopy. A low level of DNA synthesis was shown to be characteristic of pancreatic epithelium of frogs caught in winter. The B/A cell volume ratio is 3.68 +/- 0.16 and 2.55 +/- 0.36 in small and median pancreatic islets, resp. A-, B-, D-cells are found in pancreatic islets, and intermediate acinar A and acinar B cells in intact frog pancreas.     

Genetic structure of the population of Ashkhabad City of the Turkmen SSR]

Some genetical demographic characteristics of population of Ashkhabad city were studied by direct interviewing of women aged over 18 years. The influence of urbanization on the basic genetical-demographic indices was found, the indices being essentially different from those of rural population studied elsewhere. Analysis of intensity and the structure of marriage migrations showed considerable ethnic subdivision in Ashkhabad population and stability of marriage policy in an every ethnic group. The level and structure of inbreeding as well as positive marriage assortativity are of the same order as in the Turkmen rural population.     

Genetic determination of rheumatoid arthritis. Distribution of certain Mendelian markers in the light of correspondence of the disease heritability to the model of single autosomal two-allele locus with incomplete penetrance

The study on the nature of distribution of certain mendelian markers aimed at specifying their role in determination of rheumatoid arthritis disease was carried out, based on the material from the Family Data Bank of the Department of Epidemiology and Genetics of the rheumatic diseases in this institute comprising data on 200 families of patients with definite rheumatoid arthritis (RA). Antigens of HLA-system (the loci A, B, DR), ABO blood groups, Rh, MN and P, phenotypes of acid erythrocyte phosphatase and the types of haptoglobin were studied. Based on the data from this and the previous studies, it is established that the steadiest deviations of the RA patients groups from the general population concerned the frequency of HLA A11, B12, B27 and DR4, blood group P and phenotypes of the acid erythrocyte phosphatase. When using additional controls--a group of healthy mothers of women-probands from the families with the type of marriage "healthy x healthy", and analysing some pair combinations of the HLA system antigens, it was demonstrated that the most clearly their role in formation of the disease display the antigens DR4, and in their absence--DR3, and B12, whereas accumulation of A11 and B27 depended on the presence of other antigens of HLA loci--A and B. Taken together, these data may imply that genetic markers under study serve, when in certain combinations, as "modifiers" of the major gene, or, in a general case, of major genes of multifactorial disease affecting its appearance and clinical manifestations.     

Genetic determination of rheumatoid arthritis

The study on the nature of genetic determination of the definite rheumatoid arthritis (RA) and its forms was carried out, based on the material comprising clinical data on 189 probands and their 1st and 2nd degree relatives (713 subjects) which is contained in the computer Family Data Bank at the Department of Epidemiology and Genetics of this institute. The heritability coefficient "in narrow sense" (80%) obtained within the framework of the multifactorial threshold model confirmed once more important role of genetic factors in the appearance of the disease. The study of genetic heterogeneity within the framework of the Ch. Smith's and T. Reich's models failed to reveal any independent genetically RA forms. An assumption of the essential role of the genes localized in the X chromosome, based on diverse susceptibility of sexes, received no conformation. It has been shown that the RA distribution in the population and families may well be described by means of a variant of the single autosomal two-allele locus model with incomplete and differentiated for two sexes penetrance. The model parameters obtained, a particular penetrance of the mutant homozygote in both sexes equalling 100%, and penetrance of the normal homozygote equalling 0 in men and reaching 0 (0.028%) in women testify to a very essential influence of the major gene on determination of RA.     

Sensitivity of Mycoplasma hominis cultures isolated from clinical material to certain antibiotics]

Sensitivity to II antibiotics of 80 strains of M. hominis isolated from patients with various inflammatory processes of the urogenital tract was studied by the method of suppressing the metabolic activity. Inhibition of the arginine metabolism of mycoplasma was used as a test for determination of the growth suppression. All the strains tested were highly sensitive to tetracycline and lincomycin. Kanamycin and neomycin were less active against M. hominis. All the strains tested were resistant to erythromycin, oleandomycin, ristomycin, novobiocin and streptomycin. The inhibitory effect of tetracycline and lincomycin on M. hominis decreased by the 5th day.     

Lysozyme activity in the leukocytes and blood serum of white rats administered massive doses of penicillin preparations]

Activity of lysozyme in the blood serum and leucocytes was determined. The experiments were carried out on albino unbred rats weighing 170 to 200 gm. Benzylpenicillin and oxacillin were administered intramuscularly in doses of 500000 Units/kg or 20000 gamma/kg once every 24 hours for 2, 4 and 6 days. The activity of lysozyme was determined by the turbidimetric and agar-diffusion methods. It was found that the activity of lysozyme in the leucocytes increased by the 5th day accompanied by a simultaneous decrease in its level in the serum followed by reaching the initial values. The data are indicative of the fact that the use of antibiotics in mega-doses is not contraindicated from the point of view of their effect on lysozyme activity.