Two new phenylpiperazines with atypical antipsychotic potential

Two new series of substituted arylpiperazines with heterocyclic 3-propoxy-benzimidazole or 3-propoxy-benzimidazole-2-thione groups were synthesized and their in vitro binding affinities for the D(2), 5-HT(1A), 5-HT(2A), and alpha(1)-adrenergic receptors determined. Among them, only two compounds with phenyl aryl-constituent (8a and 9a) showed 5-HT(2A)/D(2) pK(i) binding ratios proposed for atypical neuroleptics. As to their behavioral screening on rodents, both compounds exhibited a non-cataleptic action in rats and antagonized D-amphetamine-induced hyperlocomotion in mice, suggesting their possible atypical antipsychotic potency.     

Novel 9a-carbamoyl- and 9a-thiocarbamoyl-3-decladinosyl-6-hydroxy and 6-methoxy derivatives of 15-membered macrolides

An efficient method for the synthesis of diverse 9a-carbamoyl- and 9a-thiocarbamoyl-3-decladinosyl-6-hydroxy and 3-decladinosyl-6-methoxy derivatives of 15-membered azalides has been developed. These derivatives bear various alkyl and aryl groups attached to macrolide scaffold through urea or thiourea moieties at 9a position. Chemical transformations of hydroxy group at position C-3 afforded range of ketolides, anhydrolides, hemiketals, cyclic ethers, and acylides. It has been shown that 6-hydroxy and 6-methoxy derivatives undergo different chemical transformations under otherwise identical reaction conditions. Antimicrobial properties of prepared compounds were evaluated.     

Small-angle X-ray scattering reveals the solution structure of the peripheral stalk subunit H of the A1AO ATP synthase from Methanocaldococcus jannaschii and its binding to the catalytic A subunit

The H subunit of the A1AO ATP synthase is a component of one of the peripheral stalks connecting the A1 and AO domain. Subunit H of the Methanocaldococcus jannaschii A1AO ATP synthase was analyzed by small-angle X-ray scattering (SAXS) in order to determine the first low-resolution structure of this molecule in solution. Independent to the concentration used, the protein is dimeric and has a boomerang-like shape, divided into two arms of 12.0 and 6.8 nm in length. Circular dichroism (CD) spectroscopy revealed that subunit H is comprised of 78% alpha-helix and a coiled-coil arrangement. To understand the orientation of the helices and the localization of the N- and C-termini inside the dimer, three truncated forms of subunit H (H8-104, H1-98, and H8-98) were expressed, purified, and analyzed by CD. SAXS experiments of H1-98 show that the maximum dimension of the truncated protein dropped to 15.1 nm. Comparison of the low-resolution shapes of H and H1-98 indicates that this goes along with structural changes in the C-terminal arm of the boomerang-like structure. Together with the result of a disulfide formation of a fourth truncated form, H1-47, with a cysteine at position 47, the data suggest a parallel alpha-helical interaction. In addition, all four truncated proteins are dimeric in solution. Tryptophan emission spectra showed specific binding of H and H8-104 to the neighboring, catalytic A subunit, which could not be detected in the presence of H1-98. Finally, the arrangement of H within the A1AO ATP synthase is presented.     

Physico-chemical characterization and the in vitro genotoxicity of medical implants metal alloy (TiAlV and CoCrMo) and polyethylene particles in human lymphocytes

Background

The main objective of the present study was to investigate chemical composition and possible cyto/genotoxic potential of several medical implant materials commonly used in total hip joint replacement.

Methods

Medical implant metal alloy (Ti₆Al₄V and CoCrMo) and high density polyethylene particles were analyzed by energy dispersive X-ray spectrometry while toxicological characterization was done on human lymphocytes using multi-biomarker approach.

Results

Energy dispersive X-ray spectrometry showed that none of the elements identified deviate from the chemical composition defined by appropriate ISO standard. Toxicological characterization showed that the tested materials were non-cyto/genotoxic as determined by the comet and cytokinesis-block micronucleus (CBMN) assay. Particle morphology was found (by using scanning electron and optical microscope) as flat, sharp-edged, irregularly shaped fiber-like grains with the mean particle size less than 10 µm; this corresponds to the so-called "submicron wear". The very large surface area per wear volume enables high reactivity with surrounding media and cellular elements.

Conclusions

Although orthopedic implants proved to be non-cyto/genotoxic, in tested concentration (10 μg/ml) there is a constant need for monitoring of patients that have implanted artificial hips or other joints, to minimize the risks of any unwanted health effects.

General significance

The fractal and multifractal analyses, performed in order to evaluate the degree of particle shape effect, showed that the fractal and multifractal terms are related to the "remnant" level of the particles' toxicity especially with the cell viability (trypan blue method) and total number of nucleoplasmic bridges and nuclear buds as CBMN assay parameters.     

Comparative Analysis of Three Different Methods for Monitoring the Use of Green Bridges by Wildlife

Green bridges are used to decrease highly negative impact of roads/highways on wildlife populations and their effectiveness is evaluated by various monitoring methods. Based on the 3-year monitoring of four Croatian green bridges, we compared the effectiveness of three indirect monitoring methods: track-pads, camera traps and active infrared (IR) trail monitoring system. The ability of the methods to detect different species and to give good estimation of number of animal crossings was analyzed. The accuracy of species detection by track-pad method was influenced by granulometric composition of track-pad material, with the best results obtained with higher percentage of silt and clay. We compared the species composition determined by track-pad and camera trap methods and found that monitoring by tracks underestimated the ratio of small canids, while camera traps underestimated the ratio of roe deer. Regarding total number of recorder events, active IR detectors recorded from 11 to 19 times more events then camera traps and app. 80% of them were not caused by animal crossings. Camera trap method underestimated the real number of total events. Therefore, an algorithm for filtration of the IR dataset was developed for approximation of the real number of crossings. Presented results are valuable for future monitoring of wildlife crossings in Croatia and elsewhere, since advantages and disadvantages of used monitoring methods are shown. In conclusion, different methods should be chosen/combined depending on the aims of the particular monitoring study.     

Assessing Attitudes towards Statistics among Medical Students: Psychometric Properties of the Serbian Version of the Survey of Attitudes Towards Statistics (SATS)

Background

Medical statistics has become important and relevant for future doctors, enabling them to practice evidence based medicine. Recent studies report that students’ attitudes towards statistics play an important role in their statistics achievements. The aim of the study was to test the psychometric properties of the Serbian version of the Survey of Attitudes Towards Statistics (SATS) in order to acquire a valid instrument to measure attitudes inside the Serbian educational context.

Methods

The validation study was performed on a cohort of 417 medical students who were enrolled in an obligatory introductory statistics course. The SATS adaptation was based on an internationally accepted methodology for translation and cultural adaptation. Psychometric properties of the Serbian version of the SATS were analyzed through the examination of factorial structure and internal consistency.

Results

Most medical students held positive attitudes towards statistics. The average total SATS score was above neutral (4.3±0.8), and varied from 1.9 to 6.2. Confirmatory factor analysis validated the six-factor structure of the questionnaire (Affect, Cognitive Competence, Value, Difficulty, Interest and Effort). Values for fit indices TLI (0.940) and CFI (0.961) were above the cut-off of ≥0.90. The RMSEA value of 0.064 (0.051–0.078) was below the suggested value of ≤0.08. Cronbach’s alpha of the entire scale was 0.90, indicating scale reliability. In a multivariate regression model, self-rating of ability in mathematics and current grade point average were significantly associated with the total SATS score after adjusting for age and gender.

Conclusion

Present study provided the evidence for the appropriate metric properties of the Serbian version of SATS. Confirmatory factor analysis validated the six-factor structure of the scale. The SATS might be reliable and a valid instrument for identifying medical students’ attitudes towards statistics in the Serbian educational context.     

Croatian children's views towards importance of health care information

The aim of research was to investigate: the need for health care information of Croatian adolescents aged from 13 to 18 years; the difference in evaluation of the frequency of receiving information between hospitalized and healthy children; if the hospitalized children expectations about the frequency of receiving health care information differed significantly from information they have actually received; whose information was most comprehensible to the hospitalized children (doctors, parents, other health care givers). The children were either hospitalized in the pediatrics departments or were high schools pupils (healthy children). The hospitalized children "Completely agreed" (92.7%) with the statement "When I am sick, I should receive information about my health" in comparison to the healthy children (85.1%). In comparison to healthy children, the hospitalized children assessed that doctors, other health care givers and parents should give them information more frequently. The experience of hospitalized children indicate that they received less information then they have actually excepted. The information received from doctors was mostly in correlation with the understanding of this information. We concluded that the children want to be informed about their health, especially hospitalized children. Health care professionals should offer understandable health care information according to the children's expectation.     

The effects of 6 weeks of preseason skill-based conditioning on physical performance in male volleyball players

The purpose of this study was to determine the changes in physical performance after a 6-week skill-based conditioning training program in male competitive volleyball players. Sixteen male volleyball players (mean ± SD: age 22.3 ± 3.7 years, body height 190.7 ± 4.2 cm, and body mass 78.4 ± 4.5 kg) participated in this study. The players were tested for sprinting (5- and 10-m sprint), agility, and jumping performance (the vertical-jump test, the spike-jump test, and the standing broad jump [SBJ]). Compared with pretraining, there was a significant improvement in the 5- and 10-m speed. There were no significant differences between pretraining and posttraining for lower-body muscular power (vertical-jump height, spike-jump height, and SBJ) and agility. Based on our results, it could be concluded that a preseason skill-based conditioning program does not offer a sufficient stimulus for volleyball players. Therefore, a general conditioning and hypertrophy training along with specific volleyball conditioning is necessary in the preseason period for the development of the lower-body strength, agility and speed performance in volleyball players.