INTRODUCTION: Ziziphora clinopodioides subsp. bungeana (Juz.) Rech.f. is used in traditional medicine for various purposes. Previous phytochemical studies focused on phenolic compounds, but triterpenoids were almost overlooked. OBJECTIVE: The study focused on the isolation of compounds with dual antidiabetic activity from the aerial parts of Z. clinopodioides subsp. bungeana. MATERIALS AND METHODS: Separation of CHCl3-soluble fraction by silica gel column chromatography using different mobile phases and purification of compounds by semi-preparative HPLC or preparative TLC. The structures of pure compounds were elucidated by 1D and 2D NMR experiments along with HRMS. Compound 1 was additionally identified by the single crystal X-ray diffraction method. α-Glucosidase inhibitory assay and GLUT4 expression and translocation in C2C12 myotubes were conducted to evaluate antidiabetic potential of isolated compounds. RESULTS: This phytochemical study led to the isolation of 20 compounds, including a unique monoterpene diperoxy dimer (1). Compounds 7 and 9-11 displayed more potent α-glucosidase inhibitory activity (IC50 45.3-135.3 μM) than acarbose used as a positive control (IC50 264.7 μM), while only pomolic acid (5) increased GLUT4 translocation in C2C12 myotubes in a significant manner. CONCLUSION: Extensive chromatographic separation led to the isolation and identification of a unique monoterpene diperoxy dimer (1) from aerial parts of Z. clinopodioides subsp. bungeana. Some triterpenes inhibited α-glucosidase, another increased GLUT4 translocation. Although none of the isolated compounds demonstrated dual antidiabetic activity, selected triterpenes proved to be potent antidiabetic agents in vitro.
- MeSH
- alpha-Glucosidases metabolism MeSH
- Cell Line MeSH
- Lamiaceae * chemistry MeSH
- Hypoglycemic Agents * pharmacology chemistry isolation & purification MeSH
- Glycoside Hydrolase Inhibitors pharmacology isolation & purification chemistry MeSH
- Mice MeSH
- Plant Components, Aerial chemistry MeSH
- Glucose Transporter Type 4 metabolism MeSH
- Plant Extracts chemistry pharmacology MeSH
- Triterpenes * pharmacology chemistry isolation & purification MeSH
- Animals MeSH
- Check Tag
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
In the shadow of SARS-CoV-2, influenza seems to be an innocent virus, although new zoonotic influenza viruses evolved by mutations may lead to severe pandemics. According to WHO, there is an urgent need for better antiviral drugs. Blocking viral hemagglutinin with multivalent N-acetylneuraminic acid derivatives is a promising approach to prevent influenza infection. Moreover, dual inhibition of both hemagglutinin and neuraminidase may result in a more powerful effect. Since both viral glycoproteins can bind to neuraminic acid, we have prepared three series of amphiphilic self-assembling 2-thio-neuraminic acid derivatives constituting aggregates in aqueous medium to take advantage of their multivalent effect. One of the series was prepared by the azide-alkyne click reaction, and the other two by the thio-click reaction to yield neuraminic acid derivatives containing lipophilic tails of different sizes and an enzymatically stable thioglycosidic bond. Two of the three bis-octyl derivatives produced proved to be active against influenza viruses, while all three octyl derivatives bound to hemagglutinin and neuraminidase from H1N1 and H3N2 influenza types.
- MeSH
- Influenza, Human * drug therapy MeSH
- Hemagglutinin Glycoproteins, Influenza Virus metabolism MeSH
- Hemagglutinins pharmacology MeSH
- N-Acetylneuraminic Acid pharmacology metabolism MeSH
- Neuraminic Acids MeSH
- Humans MeSH
- Neuraminidase metabolism MeSH
- Influenza A Virus, H1N1 Subtype * MeSH
- Influenza A Virus, H3N2 Subtype MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
Boron derivatives have great potential in cancer diagnostics and treatment. Borocaptates are used in boron neutron capture therapy and potentially in proton boron fusion therapy. This work examines modulation effects of two borocaptate compounds on radiation-induced DNA damage. Aqueous solutions of pBR322 plasmid containing increasing concentrations of borocaptates were irradiated with 60Co gamma rays or 30 MeV protons. Induction of single and double DNA strand breaks was investigated using agarose gel electrophoresis. In this model system, representing DNA without the intervention of cellular repair mechanisms, the boron derivatives acted as antioxidants. Clinically relevant boron concentrations of 40 ppm reduced the DNA single strand breakage seven-fold. Possible mechanisms of the observed effect are discussed.
- MeSH
- Boron * MeSH
- DNA radiation effects MeSH
- Plasmids genetics MeSH
- DNA Damage MeSH
- Boron Neutron Capture Therapy * MeSH
- Publication type
- Journal Article MeSH
The aim of this contribution is to provide an overview of comparison of two types of eye lens dosemeter systems. The comparison was performed at the Department of Intravenous Cardiology using patient and physician phantoms and supplemented by dose simulation using the Monte Carlo method. The tests were performed in several specific geometries and in addition to eye lens dosemeters the value of a personal dosemeter located at the reference point was also monitored. The value of Hp(3) and Hp(10) was monitored. It is clear from the results that film dosemeters achieve more correct results in most cases. It is probably due to a better correction for the angle of exposure. This assumption must be verified by more detailed measurements in laboratory conditions.
- MeSH
- Radiation Dosage MeSH
- Radiology, Interventional methods MeSH
- Cardiology * methods MeSH
- Humans MeSH
- Lens, Crystalline * MeSH
- Occupational Exposure * analysis MeSH
- Radiation Protection * methods MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
Performance in strike combat sports is mostly evaluated through the values of the net force, acceleration, or speed to improve efficient training procedures and/or to assess the injury. There are limited data on the upper limb striking area, which can be a useful variable for contact pressure assessment. Therefore, the aim of this study was to determine the contact area of the upper limb in three different strike technique positions. A total of 38 men and 38 women (n = 76, 27.3 ± 8.5 years of age, 73.9 ± 13.8 kg of body weight, 173.3 ± 8.4 cm of body height) performed a static simulation of punch with a fist, palm strike, and elbow strike, where three segments of the right upper limb were scanned. The analysis of 684 images showed a correlation (r = 0.634) between weight and punch technique position in men and significant differences in elbow strike (p < 0.001) and palm strike (p < 0.0001) between women and men. In both groups, the palm demonstrated the largest area and the elbow the smallest one. These data may be used to evaluate strike contact pressure in future studies in forensic biomechanics and assessment of injury in combat sports and self-defense.
- Publication type
- Journal Article MeSH
Dietary plant glucosides are phytochemicals whose bioactivity and bioavailability can be modified by glucoside hydrolase activity of intestinal microbiota through the release of acylglycones. Bifidobacteria are gut commensals whose genomic potential indicates host-adaption as they possess a diverse set of glycosyl hydrolases giving access to a variety of dietary glycans. We hypothesized bifidobacteria with β-glucosidase activity could use plant glucosides as fermentation substrate and tested 115 strains assigned to eight different species and from different hosts for their potential to express β-glucosidases and ability to grow in the presence of esculin, amygdalin, and arbutin. Concurrently, the antibacterial activity of arbutin and its acylglycone hydroquinone was investigated. Beta-glucosidase activity of bifidobacteria was species specific and most prevalent in species occurring in human adults and animal hosts. Utilization and fermentation profiles of plant glucosides differed between strains and might provide a competitive benefit enabling the intestinal use of dietary plant glucosides as energy sources. Bifidobacterial β-glucosidase activity can increase the bioactivity of plant glucosides through the release of acylglycone.
- Publication type
- Journal Article MeSH
Centromeres contain specialized nucleosomes at which histone H3 is partially replaced by the centromeric histone H3 variant cenH3 that is required for the assembly, maintenance, and proper function of kinetochores during mitotic and meiotic divisions. Previously, we identified a KINETOCHORE NULL 2 (KNL2) of Arabidopsis thaliana that is involved in the licensing of centromeres for the cenH3 recruitment. We also demonstrated that a knockout mutant for KNL2 shows mitotic and meiotic defects, slower development, reduced growth rate, and fertility. To analyze an effect of KNL2 mutation on global gene transcription of Arabidopsis, we performed RNA-sequencing experiments using seedling and flower bud tissues of knl2 and wild-type plants. The transcriptome data analysis revealed a high number of differentially expressed genes (DEGs) in knl2 plants. The set was enriched in genes involved in the regulation of the cell cycle, transcription, development, and DNA damage repair. In addition to comprehensive information regarding the effects of KNL2 mutation on the global gene expression, physiological changes in plants are also presented, which provides an integrated understanding of the critical role played by KNL2 in plant growth and development.
