A family of new compounds with sulfonamide and amide functional groups as potential Alzheimer's disease drugs were prepared by multistep synthesis. Thermal stability measurements recorded the initial decomposition in the range of 200-220°C, close above the melting point. The final compounds were tested for their ability to inhibit acetylcholinesterase and butyrylcholinesterase, and the in vitro dissolution behavior of selected compounds was studied through both lipophilic and hydrophilic matrix tablets. All nine tested derivatives were even more active in inhibiting acetylcholinesterase than the clinically used rivastigmine. Regression analysis of the obtained dissolution profiles was performed, and the effects of the pH and the release mechanism were determined. Some substances showed remarkable biological activity and became a subject of interest for further extensive study.
- MeSH
- acetylcholinesterasa metabolismus MeSH
- Alzheimerova nemoc * farmakoterapie MeSH
- butyrylcholinesterasa * metabolismus MeSH
- cholinesterasové inhibitory * farmakologie chemická syntéza chemie MeSH
- koncentrace vodíkových iontů MeSH
- lidé MeSH
- molekulární struktura MeSH
- rivastigmin farmakologie chemická syntéza chemie MeSH
- rozpustnost MeSH
- sulfonamidy * farmakologie chemie chemická syntéza MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
Phosphate-solubilising fungi (PSF) are beneficial microorganisms that play a pivotal role in plant growth by increasing the availability of phosphorus (P) in soil. Although phosphorus is an essential nutrient for plants, it often becomes inaccessible as it binds into insoluble forms. PSF effectively facilitate the release of this bound phosphorus through diverse mechanisms. Numerous fungal species demonstrate the ability to solubilise various types of phosphate compounds. Among the commonly researched PSF are Penicillium, Aspergillus, Rhizopus, Fusarium, Trichoderma, and Sclerotium. Moreover, yeasts such as Saccharomyces cerevisiae can potentially be leveraged as PSF. PSF secrete organic acids that chelate phosphate ions, thereby increasing their solubility in the soil. Moreover, PSF contribute to the decomposition of organic phosphorus compounds in soil by employing enzymes such as phosphatases, phytases, and phosphonatases. Furthermore, PSF can interact with other soil microorganisms, including nitrogen-fixing bacteria and arbuscular mycorrhizal fungi (AM-fungi), fostering synergistic effects that further enhance plant growth and nutrient absorption. The utilisation of PSF as biofertilisers offers numerous advantages over chemical fertilisers, including environmental friendliness, cost-effectiveness, and enhanced fertiliser utilisation efficiency. Furthermore, PSF can prove beneficial in challenging environments characterised by high phosphate sorption. Hence, this review serves as an updated study aimed at broadening the understanding of PSF and its potential applications in P solubilisation. This review also focuses on the diversity of PSF, the mechanisms underlying solubilisation, ecological roles of PSF in soil microbiome, and the benefits of sustainable agriculture. By delving into the ecological roles of PSF and their potential as biofertilisers, this study contributes to a deeper understanding of sustainable agriculture practices and addresses challenges in phosphate-scarce environments.
- MeSH
- fosfáty * metabolismus MeSH
- fosfor metabolismus MeSH
- houby * metabolismus růst a vývoj MeSH
- mykorhiza metabolismus fyziologie MeSH
- průmyslová hnojiva * analýza MeSH
- půda chemie MeSH
- půdní mikrobiologie * MeSH
- vývoj rostlin * MeSH
- zemědělství * metody MeSH
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
An increasing resistance of microbes to antibiotics, the emergence of multidrug-resistant and extremely resistant strains, and the long time needed to develop new antibiotics are driving the search for additional sources of antibacterial agents. The aim of the study was to compare the efficacy of Czech honeys with already available pharmaceutical agents containing medicinal honey, and to perform basic biochemical analysis of Czech samples, including detection of undesirable chemical substances. The results showed strong antibacterial activity of Czech honeydew honeys compared to the control group, especially against G+ pathogens, with an average MIC of 9.44% compared to 17.54%, and comparable activity against G- of 16.48% versus 16.66%. In addition to the strong antibacterial activity, this study confirmed the safety and quality of Czech honeys and helped to select the character of a possible source for in vivo testing and subsequent clinical trials.
- Publikační typ
- časopisecké články MeSH
The toxicity of food additives is widely studied and concerns many consumers worldwide. Synthetic food colors are often considered an unnecessary risk to consumer health. Since the European Food Safety Authority's (EFSA) re-evaluation between 2009 and 2014, the body of scientific literature on food colors has grown, and new evaluations are being published by the Joint FAO/WHO Expert Committee on Food Additives (JECFA). Therefore, this narrative review aims to review the toxicological data that have become available since 2014. The reviewed colors are Quinoline Yellow, Sunset Yellow, Azorubine, Amaranth, Ponceau 4R, Erythrosine, Allura Red, Patent Blue, Indigo Carmine, Brilliant Blue FCF, Green S, Brilliant Black, Brown HT, and Lithol Rubine BK. Tartrazine was not included in this paper; the overwhelming amount of recent data on Tartrazine toxicity requires more space than this review can provide. The issues regarding the toxicity of synthetic food colors and real population exposures are being regularly examined and reviewed by relevant authorities, such as the EFSA and JECFA. The current ADI limits set by the authorities are mostly in agreement, and they seem safe. However, the EFSA and JECFA assessments of some of the colors are more than a decade old, and new evidence will soon be required.
- Publikační typ
- časopisecké články MeSH
- přehledy MeSH
OBJECTIVE: To report the outcome of SLN staging in the SENTIX international prospective trial of SLN biopsy in patients with cervical cancer with an intensive ultrastaging protocol and central quality control and to evaluate how the intensity of pathological assessment correlates with metastatic detection rate in SLNs. METHODS: Eligible were patients with stages T1a1/LVSI+ to T1b2 (<4 cm, ≤2 cm for fertility sparing), common tumor types, no suspicious lymph nodes on imaging, and bilateral SLN detection. SLNs were examined intraoperatively and processed by an intensive protocol for ultrastaging (paraffin blocks sectioned completely in 150-μm intervals/levels). SLNs from each site were submitted for central quality control. RESULTS: In the SENTIX SLN study, 647 out of 733 enrolled patients underwent SLN ultrastaging, identifying 12.5% (81/647) with node positive, N1 cases. Intraoperative detection revealed metastases in 56.8% (46/81) of these cases, categorized into macrometastases (83.7%), micrometastases (26.3%), and isolated tumor cells (9.1%). Ultrastaging identified additional metastatic involvement in 43.2% (35/81) of patients, with detailed sectioning revealing metastases (MAC/MIC) at first level in 20 cases (24.7%), at levels 2-4 in 9 cases (11.1%), and at level ≥5 in 6 cases (7.4%). CONCLUSION: SLN ultrastaging detects additional 43% of N1 (MAC/MIC) in patients with negative LNs by imaging and intraoperative pathological assessment. The detection rate of positive SLN correlates with the intensity (number of levels) of ultrastaging. Examination of four levels from paraffin blocks, which detects >90% of patients with N1, is a reasonable compromise for an international standard for ultrastaging. STUDY REGISTRATION: NCT02494063 (ClinicalTrials.gov).
- MeSH
- biopsie sentinelové lymfatické uzliny * metody MeSH
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- lymfatické metastázy * MeSH
- nádory děložního čípku * patologie chirurgie MeSH
- prospektivní studie MeSH
- senioři MeSH
- sentinelová uzlina * patologie chirurgie MeSH
- staging nádorů * MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
Sex-typicality displayed as sexual dimorphism of the human face is a key feature enabling sex recognition. It is also believed to be a cue for perceiving biological quality and it plays an important role in the perception of attractiveness. Sexual dimorphism of human faces has two main components: sexual shape dimorphism of various facial features and sexual color dimorphism, generally manifested as dimorphism of skin luminance, where men tend to be darker than women. However, very little is known about the mutual relationship of these two facets. We explored the interconnection between the dimorphism of face shape and dimorphism of face color in three visually distinct populations (Cameroonian, Czech, and Vietnamese). Our results indicated that populations which showed a significant dimorphism in skin luminance (Cameroon, Vietnam) had low levels of sexual shape dimorphism, while a population with higher levels of sexual shape dimorphism (Czech Republic) did not exhibit a significant dimorphism of skin luminance. These findings suggest a possible compensatory mechanism between various domains of sexual dimorphism in populations differing in the levels of shape and color dimorphism.
- MeSH
- dospělí MeSH
- lidé MeSH
- obličej * anatomie a histologie MeSH
- pigmentace kůže * MeSH
- pohlavní dimorfismus * MeSH
- Check Tag
- dospělí MeSH
- lidé MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- Geografické názvy
- Česká republika MeSH
- Vietnam MeSH
Research has shown that external relative to internal focus (IF) instructions may improve motor performance as well as cognitive function (e.g., attentional stability and task-focus). The aim of the study was to examine the influence of attentional focus instructions on skill acquisition and learning of an aiming task in individuals with hearing impairments. The participants (N = 39, Mage = 17.87 ± 1.88 years) performed a bowling task with their dominant hand to knock down as many pins as possible. On day 1, they were randomly divided into three attentional focus groups; IF (focus on your throwing hand), external focus (EF) (focus on the pins), and control (no-focus) instructions. Each participant performed 36 trials, divided into 3 blocks of 12 trials. Attentional focus instructions were given before each block, with a brief reminder provided after each 3 trials. On day 2, retention and transfer (further distance) tests were performed. Results showed that while there were no significant differences between groups in the pre-test, the EF group outperformed both IF and control groups in retention and transfer tests. No significant difference was found between the control and IF. The findings suggest that the advantages of the external relative to the IF and no-focus instructions may generalize to individuals with hearing impairments.
Autonomic control of heart rate is well known in adult subjects, but limited data are available on the development of the heart rate control during childhood and adolescence. Continuous 12-lead electrocardiograms were recorded in 1045 healthy children and adolescents (550 females) aged 4 to 19 years during postural manoeuvres involving repeated 10-min supine, unsupported sitting, and unsupported standing positions. In each position, heart rate was measured, and heart rate variability indices were evaluated (SDNN, RMSSD, and high (HF) and low (LF) frequency components were obtained). Quasi-normalized HF frequency components were defined as qnHF = HF/(HF + LF). These measurements were, among others, related to age using linear regressions. In supine position, heart rate decreases per year of age were significant in both sexes but lower in females than in males. In standing position, these decreases per year of age were substantially lowered. RMSSD and qnHF indices were independent of age in supine position but significantly decreased with age in sitting and standing positions. Correspondingly, LF/HF proportions showed steep increases with age in sitting and standing positions but not in the supine position. The study suggests that baseline supine parasympathetic influence shows little developmental changes during childhood and adolescence but that in young children, sympathetic branch is less responsive to vagal influence. While vagal influences modulate cardiac periods in young and older children equally, they are less able to suppress the sympathetic influence in younger children.
- MeSH
- autonomní nervový systém * fyziologie MeSH
- dítě MeSH
- dospělí MeSH
- elektrokardiografie metody MeSH
- lidé MeSH
- mladiství MeSH
- mladý dospělý MeSH
- postura těla fyziologie MeSH
- předškolní dítě MeSH
- srdeční frekvence * fyziologie MeSH
- supinační poloha MeSH
- Check Tag
- dítě MeSH
- dospělí MeSH
- lidé MeSH
- mladiství MeSH
- mladý dospělý MeSH
- mužské pohlaví MeSH
- předškolní dítě MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
Neoadjuvant chemotherapy (NAC) is the preferred treatment option in locally advanced breast cancer (BC). The administration of NAC is associated with a wide range of adverse effects. This pilot observational prospective study examined the effect of NAC using anthracycline + cyclophosphamide (AC) followed by paclitaxel (PTx) on a portfolio of 22 plasma and urinary amino acids, plasma proteins (albumin, prealbumin, transferrin), and products of nitrogen metabolism (urea, creatinine, uric acid) in plasma and urine. Plasma and 24-h urine samples were obtained from ten patients with early breast cancer (N1-3 N0-2 M0), at the following time points: before the start of NAC and during the AC/PTx treatment period (a total of 8 measurements at three-weekly intervals). Amino acids were analyzed using ion exchange chromatography. There were no significant differences in the measured parameters in plasma and urine between pre-NAC and during AC- and PTx-treatment. No trend was detected. A significant difference in the portfolio of plasma and urinary amino acids was found only in the pre-treatment period compared to the control group. Levels of eight plasma amino acids (8/22) were significantly reduced and those of nine urine amino acids were increased (9/22). Nitrogenous catabolites in plasma and urine were not indicative of increased protein catabolism during the anthracycline and taxane treatment periods. A slightly positive nitrogen balance was accompanied by an average weight gain of 3.3 kg (range 0-6 kg). The AC/PTx treatment regimen did not cause significant changes in the monitored laboratory parameters.
- MeSH
- aminokyseliny * moč krev MeSH
- antracykliny terapeutické užití aplikace a dávkování MeSH
- cyklofosfamid * terapeutické užití MeSH
- dospělí MeSH
- dusík * moč MeSH
- kreatinin moč krev MeSH
- krevní proteiny * metabolismus analýza MeSH
- lidé středního věku MeSH
- lidé MeSH
- nádory prsu * farmakoterapie krev moč MeSH
- neoadjuvantní terapie * MeSH
- paclitaxel * terapeutické užití aplikace a dávkování MeSH
- pilotní projekty MeSH
- prospektivní studie MeSH
- protokoly antitumorózní kombinované chemoterapie terapeutické užití MeSH
- senioři MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- senioři MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- pozorovací studie MeSH
The oviduct provides an optimal environment for the final preparation, transport, and survival of gametes, the fertilization process, and early embryonic development. Most of the studies on reproduction are based on in vitro cell culture models because of the cell's accessibility. It creates opportunities to explore the complexity of directly linked processes between cells. Previous studies showed a significant expression of genes responsible for cell differentiation, maturation, and development during long-term porcine oviduct epithelial cells (POECs) in vitro culture. This study aimed at establishing the transcriptomic profile and comprehensive characteristics of porcine oviduct epithelial cell in vitro cultures, to compare changes in gene expression over time and deliver information about the expression pattern of genes highlighted in specific GO groups. The oviduct cells were collected after 7, 15, and 30 days of in vitro cultivation. The transcriptomic profile of gene expression was compared to the control group (cells collected after the first day). The expression of COL1A2 and LOX was enhanced, while FGFBP1, SERPINB2, and OVGP1 were downregulated at all selected intervals of cell culture in comparison to the 24-h control (p-value < 0.05). Adding new detailed information to the reproductive biology field about the diversified transcriptome profile in POECs may create new future possibilities in infertility treatments, including assisted reproductive technique (ART) programmes, and may be a valuable tool to investigate the potential role of oviduct cells in post-ovulation events.
- MeSH
- buněčné kultury metody MeSH
- epitelové buňky * metabolismus cytologie MeSH
- kultivované buňky MeSH
- prasata MeSH
- regulace genové exprese MeSH
- stanovení celkové genové exprese MeSH
- transkriptom * MeSH
- vejcovody u zvířat metabolismus cytologie MeSH
- vejcovody metabolismus cytologie MeSH
- zvířata MeSH
- Check Tag
- ženské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
