We recently described the development and application of a new bioorthogonal conjugation, the triazinium ligation. To explore the wider application of this reaction, in this work, we introduce a general method for synthesizing C3-substituted triazinium salts based on the Liebeskind-Srogl cross-coupling reaction and catalytic thioether reduction. These methods enabled the synthesis of triazinium derivatives for investigating the effect of different substituents on the ligation kinetics and stability of the compounds under biologically relevant conditions. Finally, we demonstrate that the combination of a coumarin fluorophore attached to position C3 with a C5-(4-methoxyphenyl) substituent yields a fluorogenic triazinium probe suitable for no-wash, live-cell labeling. The developed methodology represents a promising synthetic approach to the late-stage modification of triazinium salts, potentially widening their applications in bioorthogonal reactions.

• MeSH
• fluorescenční barviva * chemie   chemická syntéza   MeSH
• kumariny chemie   chemická syntéza   MeSH
• lidé MeSH
• molekulární struktura MeSH
• soli * chemie   MeSH
• triaziny * chemie   chemická syntéza   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• fluorescenční barviva * MeSH
• kumariny MeSH
• soli * MeSH
• triaziny * MeSH

The aim of the study was to investigate the effect of potassium-based emulsifying salts (ES; 2% wt/wt concentration) with different phosphate chain lengths (dipotassium hydrogenphosphate [K2HPO4; DKP], tetrapotassium diphosphate [K4P2O7; KTPP], pentapotassium triphosphate [K5P3O10; TKPP]) on the physicochemical, viscoelastic, textural, tribological, thermal, and sensory properties of processed cheese (PC; 40% wt/wt DM, 50% wt/wt fat in DM) during a 60d storage period (6°C ± 2°C). On the whole, the hardness of all PC samples increased with the increasing chain length of ES (DKP < TKPP < KTPP) and the prolonging storage period. Moreover, the hardness results were in accordance with those of the rheological analysis. All PC samples exhibited a more elastic character (G' > G″; tan δ < 1). The type of potassium-based ES affected the binding of water into the structure of the PC. Furthermore, the study confirmed that the manufactured PC received optimal sensory scores, without any excessive bitterness. It could be concluded that the type of applied ES and storage length affected the functional properties of PC. Finally, the information provided in this study could serve as a tool for the dairy industry to help appropriately select potassium-based ES for PC manufacture with desired properties.

• Klíčová slova
• potassium-based emulsifying salts, processed cheese, rheological properties, textural properties, thermal properties,
• MeSH
• draslík * MeSH
• manipulace s potravinami MeSH
• reologie * MeSH
• soli MeSH
• sýr * analýza   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• draslík * MeSH
• soli MeSH

This study investigated microplastics (MPs) in commercial sea salts from Bangladesh. The presence of MPs in the 18 sea salt bands was 100 %, where the mean MPs abundance was 471.67 MPs/kg, ranging between 300 and 670 MPs/kg. The maximum number of MPs in the 300-1500 μm size class was significantly higher than the 1500-3000 μm and 3000-5000 μm size class. The most dominant color was black. Fibers and foams were the dominant shapes. The highest number of MPs was 41 %, obtained from coarse salt grains. Four types of polymers were mainly identified from the analyzed samples: PP, PE, PET, and PA. The mean polymer risk index value among these sea salts was 539 to 1257. The findings of this study can be helpful for consumers, salt industries, and policymakers to be aware of or reduce MP contamination levels in sea salts during production and consumption.

• Klíčová slova
• Commercial salt, Contamination, Health risk, Microplastic, Table salt,
• MeSH
• chemické látky znečišťující vodu * analýza   MeSH
• kuchyňská sůl analýza   MeSH
• mikroplasty * MeSH
• monitorování životního prostředí MeSH
• plastické hmoty MeSH
• soli MeSH
• Publikační typ
• časopisecké články MeSH
• Geografické názvy
• Bangladéš MeSH
• Názvy látek
• chemické látky znečišťující vodu * MeSH
• kuchyňská sůl MeSH
• mikroplasty * MeSH
• plastické hmoty MeSH
• soli MeSH

Pentamethinium indolium salts are promising fluorescence probes and anticancer agents with high mitochondrial selectivity. We synthesized two indolium pentamethinium salts: a cyclic form with quinoxaline directly incorporated in the pentamethinium chain (cPMS) and an open form with quinoxaline substitution in the γ-position (oPMS). To better understand their properties, we studied their interaction with mitochondrial phospholipids (cardiolipin and phosphatidylcholine) by spectroscopic methods (UV-Vis, fluorescence, and NMR spectroscopy). Both compounds displayed significant affinity for cardiolipin and phosphatidylcholine, which was associated with a strong change in their UV-Vis spectra. Nevertheless, we surprisingly observed that fluorescence properties of cPMS changed in complex with both cardiolipin and phosphatidylcholine, whereas those of oPMS only changed in complex with cardiolipin. Both salts, especially cPMS, display high usability in mitochondrial imaging and are cytotoxic for cancer cells. The above clearly indicates that conjugates of pentamethinium and quinoxaline group, especially cPMS, represent promising structural motifs for designing mitochondrial-specific agents.

• Klíčová slova
• Fluorescence mitochondrial probe, Pentamethinium salt, Quinoxaline,
• MeSH
• chinoxaliny farmakologie   MeSH
• fosfatidylcholiny MeSH
• kardiolipiny * MeSH
• protinádorové látky * farmakologie   chemie   MeSH
• soli MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• 4-chlorophenyl methyl sulfide MeSH Prohlížeč
• chinoxaliny MeSH
• fosfatidylcholiny MeSH
• kardiolipiny * MeSH
• protinádorové látky * MeSH
• soli MeSH

This article presents the study results of the hypoglycemic properties among 1,2,4-triazole derivatives synthesized at the Department of Physical and Colloidal Chemistry of the Zaporizhzhia State Medical University. Today, many people have a sedentary way of life, also most of their diet contains products that they frequently use, which increase the level of glucose in the blood, which can provoke the development of serious diseases. Therefore, to date, the creation of drugs that exhibit hypoglycemic activity and have a low level of toxicity remains an urgent task for medicine and pharmacy. In the first stage of our research, acute toxicity prediction was performed. The hypoglycemic activity of the synthesized compounds was assessed by performing an intraperitoneal glucose tolerance test (IPGTT) with a change in the blood glucose concentration of the animal after its single intraperitoneal administration in the form of a 40% solution at a dose of 2 g/kg of rat body weight. Thirty-eight compounds of the different classes were studied for hypoglycemic activity. Zinc (II) 2-{5-[(3,4-methoxyphenyl)-3H-1,2,4-triazole-3-yl]thio} acetate (3.18) showed the highest efficiency in terms of the ability to lower blood glucose levels, namely, by 27.3% (approximately 1.3 times).

• Klíčová slova
• 1,2,4-triazole, hypoglycemic activity, intraperitoneal glucose tolerance test,
• MeSH
• hypoglykemika * farmakologie   MeSH
• krevní glukóza MeSH
• krysa rodu Rattus MeSH
• soli * MeSH
• triazoly farmakologie   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• 1,2,4-triazole MeSH Prohlížeč
• hypoglykemika * MeSH
• krevní glukóza MeSH
• soli * MeSH
• triazoly MeSH

We compared the efficiency of real-time PCR analysis of FII (c.*97G>A, G20210A) and FV Leiden (c.1601G>A) thrombophilic mutations in the samples obtained from venous blood treated with various anti coagulant agents (EDTA, heparin, and sodium fluoride with potassium oxalate), or from clotted venous blood; one hundred samples of wild-type subjects were tested. Genomic DNA extracts and whole blood specimens modified by 90 °C heating were analysed by real-time PCR analysis; cycle threshold values were subsequently evaluated. Real-time PCR analysis for the FII gene assay performed in DNA extracts from EDTA blood samples revealed a median Ct value of 19.3. Similar Ct values were apparent in the DNA extracts obtained from the heparinized blood and sodium fluoride with potassium oxalatetreated samples: 18.5 and 18.9, respectively. Significantly higher Ct values were found in extracts from clotted blood with medians of 20.6 (tubes with inert separation gel) and 20.5 (tubes without the gel, both P < 0.001). The data on the FV real-time PCR analysis were very comparable to the FII assay. In the modified whole blood, the samples treated with heparin salts showed significantly lower Ct values (P < 0.001) in both assays when compared with the samples with EDTA, sodium fluoride with potassium oxalate, and with the samples with clotted blood. Our results indicate that real-time PCR analyses of thrombophilic mutations were not negatively influenced by the presence of heparin salts in collection tubes. Blood samples with various anticoagulants might be exchangeable for each other when DNA analysis of thrombophilic mutations is required.

• MeSH
• DNA MeSH
• EDTA farmakologie   MeSH
• fluorid sodný MeSH
• heparin farmakologie   MeSH
• kvantitativní polymerázová řetězová reakce MeSH
• kyselina oxalová MeSH
• lidé MeSH
• mutace genetika   MeSH
• soli * MeSH
• trombofilie * genetika   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• DNA MeSH
• EDTA MeSH
• fluorid sodný MeSH
• heparin MeSH
• kyselina oxalová MeSH
• soli * MeSH

Pollution with heavy metal salts is an important environmental problem today, having an adverse effect on public health. The endocrine system maintains homeostasis in the body. The antioxidant protection (GPX-1) of the pineal gland in mature rats was studied. Animals of the experimental group represented a model of microelementosis, achieved by adding a mixture of heavy metal salts for 90 days to drinking water: zinc (ZnSO4×7H2O) - 5 mg/l, copper (CuSO4×5H2O) - 1 mg/l, iron (FeSO4) - 10 mg/l, manganese (MnSO4×5H2O) - 0.1 mg/l, lead (Pb(NO3)2) - 0.1 mg/l, and chromium (K2Cr2O7) - 0.1 mg/l. Morphological, statistical and immunohistochemical (GPX-1) research methods were used. Long-term (90-days) intake of heavy metal salts mixture in the body of experimental animals brought about development of the general adaptation syndrome, the stage of chronic stress "subcompensation" in the pineal gland. Morphological rearrangements were of nonspecific polymorphic nature as severe hemodynamics disorder in the organ, impairment of vascular wall morphology, development of tissue hypoxia and oxidative stress, accompanied by processes of accelerated apoptosis in part of pinealocytes, by a significant decrease in glutathione peroxidase level in the organ and reactive astrogliosis as a response to the damaging agent's action. Along with the negative changes in the pineal gland, a compensatory-adaptive processes with signs of functional stress also occurred. A sufficiently high degree of glutathione peroxidase activity in 39% of pinealocytes located perivascularly, active adaptive glial reaction and activation of synthetic processes in some pinealocytes were also observed.

• Klíčová slova
• GPX-1, Heavy metals, Oxidative stress, Pineal gland, Reactive astrogliosis,
• MeSH
• epifýza mozková * MeSH
• glutathionperoxidasa MeSH
• krysa rodu Rattus MeSH
• soli MeSH
• těžké kovy * toxicita   MeSH
• zvířata MeSH
• Check Tag
• krysa rodu Rattus MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• glutathionperoxidasa MeSH
• soli MeSH
• těžké kovy * MeSH

In the protein purification, drug delivery, food industry, and biotechnological applications involving protein-polyelectrolyte complexation, proper selection of co-solutes and solution conditions plays a crucial role. The onset of (bio)macromolecular complexation occurs even on the so-called "wrong side" of the protein isoionic point where both the protein and the polyelectrolyte are net like-charged. To gain mechanistic insights into the modulatory role of salts (NaCl, NaBr, and NaI) and sugars (sucrose and sucralose) in protein-polyelectrolyte complexation under such conditions, interaction between bovine serum albumin (BSA) and sodium polystyrene sulfonate (NaPSS) at pH = 8.0 was studied by a combination of isothermal titration calorimetry, fluorescence spectroscopy, circular dichroism, and thermodynamic modeling. The BSA-NaPSS complexation proceeds by two binding processes (first, formation of intrapolymer complexes and then formation of interpolymer complexes), both driven by favorable electrostatic interactions between the negatively charged sulfonic groups (-SO3-) of NaPSS and positively charged patches on the BSA surface. Two such positive patches were identified, each responsible for one of the two binding processes. The presence of salts screened both short-range attractive and long-range repulsive electrostatic interactions between both macromolecules, resulting in a nonmonotonic dependence of the binding affinity on the total ionic strength for both binding processes. In addition, distinct anion-specific effects were observed (NaCl < NaBr < NaI). The effect of sugars was less pronounced: sucrose had no effect on the complexation, but its chlorinated analogue, sucralose, promoted it slightly due to the screening of long-range repulsive electrostatic interactions between BSA and NaPSS. Although short-range non-electrostatic interactions are frequently mentioned in the literature in relation to BSA or NaPSS, we found that the main driving force of complexation on the "wrong side" are electrostatic interactions.

• MeSH
• chlorid sodný MeSH
• cukry MeSH
• polyelektrolyty MeSH
• polystyreny MeSH
• sacharosa MeSH
• sérový albumin hovězí * chemie   MeSH
• soli * MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Research Support, N.I.H., Extramural MeSH
• Názvy látek
• chlorid sodný MeSH
• cukry MeSH
• polyelektrolyty MeSH
• polystyrene sulfonic acid MeSH Prohlížeč
• polystyreny MeSH
• sacharosa MeSH
• sérový albumin hovězí * MeSH
• soli * MeSH

Mitochondria generate energy and building blocks required for cellular growth and function. The notion that mitochondria are not involved in the cancer growth has been challenged in recent years together with the emerging idea of mitochondria as a promising therapeutic target for oncologic diseases. Pentamethinium salts, cyan dyes with positively charged nitrogen on the benzothiazole or indole part of the molecule, were originally designed as mitochondrial probes. In this study, we show that pentamethinium salts have a strong effect on mitochondria, suppressing cancer cell proliferation and migration. This is likely linked to the strong inhibitory effect of the salts on dihydroorotate dehydrogenase (DHODH)-dependent respiration that has a key role in the de novo pyrimidine synthesis pathway. We also show that pentamethinium salts cause oxidative stress, redistribution of mitochondria, and a decrease in mitochondria mass. In conclusion, pentamethinium salts present novel anti-cancer agents worthy of further studies.

• Klíčová slova
• Dihydroorotate dehydrogenase, Metastasis, Migration, Mitochondria, Pentamethinium salts,
• MeSH
• dihydroorotátdehydrogenasa MeSH
• dýchání MeSH
• lidé MeSH
• mitochondrie metabolismus   MeSH
• nádory * metabolismus   MeSH
• oxidoreduktasy působící na CH-CH vazby * metabolismus   MeSH
• soli metabolismus   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• dihydroorotátdehydrogenasa MeSH
• oxidoreduktasy působící na CH-CH vazby * MeSH
• soli MeSH

Data on alkaloid interactions with the physiologically important transition metals, iron and copper, are mostly lacking in the literature. However, these interactions can have important consequences in the treatment of both Alzheimer's disease and cancer. As isoquinoline alkaloids include galanthamine, an approved drug for Alzheimer's disease, as well as some potentially useful compounds with cytostatic potential, 28 members from this category of alkaloids were selected for a complex screening of interactions with iron and copper at four pathophysiologically relevant pH and in non-buffered conditions (dimethyl sulfoxide) by spectrophotometric methods in vitro. With the exception of the salts, all the alkaloids were able to chelate ferrous and ferric ions in non-buffered conditions, but only five of them (galanthine, glaucine, corydine, corydaline and tetrahydropalmatine) evoked some significant chelation at pH 7.5 and only the first two were also active at pH 6.8. By contrast, none of the tested alkaloids chelated cuprous or cupric ions. All the alkaloids, with the exception of the protopines, significantly reduced the ferric and cupric ions, with stronger effects on the latter. These effects were mostly dependent on the number of free aromatic hydroxyls, but not other hydroxyl groups. The most potent reductant was boldine. As most of the alkaloids chelated and reduced the ferric ions, additional experimental studies are needed to elucidate the biological relevance of these results, as chelation is expected to block reactive oxygen species formation, while reduction could have the opposite effect.

• Klíčová slova
• alkaloid, chelation, copper, iron, reduction,
• MeSH
• Alzheimerova nemoc * MeSH
• chelátory chemie   MeSH
• cytostatické látky * MeSH
• dimethylsulfoxid MeSH
• galantamin MeSH
• hydroxylový radikál MeSH
• isochinoliny farmakologie   MeSH
• lidé MeSH
• měď chemie   MeSH
• reaktivní formy kyslíku MeSH
• redukční činidla MeSH
• soli MeSH
• železo chemie   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• chelátory MeSH
• cytostatické látky * MeSH
• dimethylsulfoxid MeSH
• galantamin MeSH
• hydroxylový radikál MeSH
• isochinoliny MeSH
• měď MeSH
• reaktivní formy kyslíku MeSH
• redukční činidla MeSH
• soli MeSH
• železo MeSH