Relationship between the structure of diamine platinum(II) complexes and their cytostatic activity as measured on plant roots

The amine substituent effect in compounds [Pt(diamine)Cl₂] on inhibition of maize and cucumber root growth and branching has been investigated. The diamines used were ethylenediamine (en),N-methylethylenediamine (men),N,N-dimethylethylenediamine (N,N-dmen),N,N-dimethylethylenediamine (N,N-dmen),N,N,N,N-tetramethylethylenediamine (tmen), 1,2-propanediamine (1,2-pn), 2-methyl-1,2-propanediamine (ibn), 2,3 dimethyl-2,3-butanediamine (C-tmen), 1,3-propanediamine (1,3-pn), 2,2-dimethyl-1,3-propanediamine (C₂-dm-1,3 pn),N,N-dimethyl-1,3-propanediamine (N,N-dm-1,3-pn). Increased substitution of hydrogen atoms of the amine part with CH₃ groups reduces the cytostatic activity of complexes. The substitution of hydrogen atoms of NH₂ and vicinal CH₂ groups displays similar results. C-2 dimethylation (C-dm-1,3-pn) does not change the activity of the complex compared with (1,3-pn). It was observed that maize and cucumber roots differ in their relative sensitivity to various complexes. All complexes containing pn and their substituted analogs inhibited cucumber root growth weaker than that in maize. A comparison of obtained data with earlier published results concerning antitumor activity of complexes shows that they correlate in a similar manner with increased substitution of amino groups. Therefore, roots may be used as cheap test objects for primary screening of cytostatics. The general tendency of a decrease in cytostatic activity goes parallel with the number of Nor vicinal C-methyl groups and seems to arise from a decrease in hydrogen-bonding potential; however, some other possible reasons are also discussed. The activity discrimination by different species in our experiments and clearly different results forN,N-dimethylation depending on the chelate ring size (en and pn derivatives) on maize cannot be attributed to slower ligand-exchange kinetics from methylation. It is possible to assume that the major role in cytostatic activity of platinum complexes belongs to a cell repair system, i.e. the ability to eliminate platinum diamine fragments from DNA, depending on the number and strength of hydrogen bonds formed by thecis-diamine fragment.     

Effects of the antidepressant pirlindole and its dehydro-derivative on the activity of monoamine oxidase-a and on GABAA receptors

The effects of pirlindole and dehydro-pirlindole on GABA_A receptors and MAO-A activity were investigated in vitro. Pirlindole was inactive as a GABA antagonist. Dehydro-pirlindole exhibited partial and selective blockade of a subset of GABA_A receptors with an EC₅₀ of 12μM and maximum reversal (ΔB_opt) of 42%. Inhibition of rat brain and human placenta MAO-A by both compounds was much more potent (with IC₅₀ range 0.3–0.005 μM). Their effects on MAO-A activity were partially reversible in vitro. In contrast to pirlindole, dehydro-pirlindole may act not only as MAO-A inhibitor but also as a clozapine-like selective GABA_A receptor blocker, preferentially blocking a subset of GABA_A receptors that are not sensitive to DMCM or Ro 5-4864. Pirlindole is the generic name of the drug pyrazidol.     

Study of Uridine Effect on the Development of Audiogenic Tonic Seizures in Krushinsky–Molodkina Strain Rats

The latency of tonic seizure in response to loud sound (in rats of the Krushinsky–Molodkina strain with audiogenic epilepsy) had been slightly (although statistically significantly) longer after chronic uridine injections (100 mg/kg, i.p., three times a day during 9 or 12 days). The recovery time from the tonic seizure was shorter after 12 days of injections in comparison to the 9-day injection period. At the same time, the intensity of tonic seizures provoked by loud sound did not change after chronic uridine injections. The lack of uridine anticonvulsive effect demonstrated in the audiogenic epilepsy model contradicts the anticonvulsant effects of uridine in experiments with other seizure models, in which the epileptic foci were localized in the forebrain structures.     

Spatial and temporal dynamics of Siberian silk moth large-scale outbreak in dark-needle coniferous tree stands in Altai

The spatial and temporal dynamics of fir stands damage caused by a large-scale outbreak of the Siberian silk moth (Dendrolimus sibiricus Tschetv.) in the Altai Mountains has been studied using remote sensing and GIS methods. It is ascertained that forest damages are dissimilar relative to the surface features. The pest outbreak initially occurred on the southwest slopes with mean values of 10° and elevation of 400 m asl. The damages further extended both upward and downward, involving slopes of high steepness and the eastern exposure. The total area of the dead stands comprised 6000 ha, 45% of which were lost due to secondary pest (xylophagous insects) attacks. It is indicated that the use of remote sensing made it possible to determine the beginning of a pest outbreak with one-decade precision. The Siberian silk moth large-scale outbreak occurred against an increase in air temperatures, a decrease in precipitation, and a reduction in late frosts. The tree plants weakened by the Siberian silk moth and water stress were affected by xylophagous insect attacks. The observed and predicted warming and climate aridity increase will facilitate Siberian silk moth outbreaks both within its range and northward of the current margins of the range.     

Expression and inheritance of a desynaptic phenotype with impaired homologous synapsis in rye

The cytological phenotype was studied in a desynaptic form isolated from a population of rye cultivar Vyatka. The primary defect of desynaptic plants was identified as nonhomologous (heterologous) chromosome synapsis, which was observed by electron microscopy of synaptonemal complexes (SCs) in meiotic prophase I. Synapsis defects involved switches of synapsing axial elements to nonhomologous partners, asynapsis in the switching region, and foldbacks formed by the SC lateral elements. Defective bivalent formation was observed at later stages: the univalent number varied and multivalent chromosome associations were observed in single cells in metaphase I. The desynaptic phenotype was controlled by two recessive genes, sy8a and sy8b, which acted and were inherited independently. In a hybrid combination with line Ku-2/63, the desynaptic phenotype was suppressed by the dominant allele of a third gene for inhibitor I; the segregation in hybrid families corresponded to 57:7.     

Breeding Success Affects the Apparent Survival of Grassland Passerines

The apparent adult survival rate is one of the key population parameters of migratory birds. The widely used Cormack–Jolly–Seber capture–mark–recapture model has a number of disadvantages, the main one of which is the impossibility of discerning mortality and permanent emigration. The accuracy of survival estimates can be increased using a multistate capture–mark–recapture model, with the help of which it is possible to assess the survival of successful and unsuccessful birds separately. We used this model to estimate the apparent survival rates of adults in local populations of three ground-nesting passerines: Booted Warbler (Iduna caligata), Whinchat (Saxicola rubetra), and Yellow Wagtail (Motacilla flava), all breeding on abandoned agricultural lands. We studied the reproductive success of 472 marked pairs and analyzed individual capture histories of 814 birds. The previous reproductive success was found to influence significantly the apparent survival of adults. This relation was best expressed in the Yellow Wagtail (apparent survival of successful birds, φ = 0.39 ± 0.06, vs. that of unsuccessful birds, φ = 0.19 ± 0.06) and the Whinchat (apparent survival of successful birds, φ = 0.32 ± 0.05, vs. apparent survival of unsuccessful birds, φ = 0.10 ± 0.05), but a little lower in the Booted Warbler (apparent survival of successful birds, φ = 0.33 ± 0.17, vs. apparent survival of unsuccessful birds, φ = 0.16 ± 0.13). Unsuccessful individuals leave the study area for good, while most of the successful birds return there the next year. Thus, the apparent survival rate of passerines evaluated with capture–recapture models is determined to a considerable degree by the previous reproductive success within local populations.     

Experimental study of the protective activity of vaccines made from 7 Pseudomonas aeruginosa immunotypes

Monovaccines were prepared from seven P. aeruginosa immunotypes (according to Fisher's classification) and three P. aeruginosa production strains belonging to immunotypes 2, 3, and 7. The immunogenic potency of these monovaccines was studied in direct and cross experiments on the active protection of mice. The study revealed that the monovaccines prepared from P. aeruginosa of seven immunotypes possessed both specific and cross protective activity. Protective cross activity was revealed also in the vaccines prepared from the production strains. When tested in mice challenged with the corresponding homologous strains, the monovaccines prepared from immunotypes 2, 3, 4 and 7 proved to possess higher immunogenic potency than monovaccines prepared from immunotypes 1, 5 and 6.