Low solubility of reactants or products in aqueous solutions can result in the enzymatic catalytic reactions that can occur in non-aqueous solutions. In current study we investigated aqueous solutions containing different organic solvents / deep eutectic solvents (DESs) that can influence the protease enzyme's activity, structural, and thermal stabilities. Retroviral aspartic protease enzyme is responsible for the cleavage of the polypeptide precursors into mature viral components, a very crucial step for virus life cycle. In molecular dynamic simulations (MDS), the complex of the protease enzyme with Darunavirwas found highly stable in urea aqueous solution compared to when with the ethylene glycol (EG) or glycerol solvents. Particularly, in different organic solvents the presence of Darunavir induced protein-protein interactions within the protease homodimer. For the systems with EG or glycerol solvents, the flap domains of the enzyme formed an "open" conformation which lead to a weak binding affinity with the drug. Conserved D25 and G27 residues among this family of the aspartic protease enzymes made a stable binding with Darunavir in the urea systems. Unfolding of the protease dimer was initiated due to self-aggregation for the EG or glycerol organic solvents, which formed an "open" conformation for the flap domains. On the contrary lack of such clustering in urea solvent, the protease showed conventional structural folding in the presence or absence of the drug molecule. These novel findings may help to better understand the protease enzymes, which could be controlled by deep eutectic solvents.

• Klíčová slova
• Aggregation, Darunavir, HIV-1, Inhibitors, Molecular dynamics, Organic solvents, Protease, Structural folding,
• MeSH
• darunavir MeSH
• ethylenglykol * MeSH
• glycerol * MeSH
• močovina farmakologie   chemie   MeSH
• proteasy MeSH
• rozpouštědla chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• darunavir MeSH
• ethylenglykol * MeSH
• glycerol * MeSH
• močovina MeSH
• proteasy MeSH
• rozpouštědla MeSH

Mitragynine (MG) is the most abundant alkaloid component of the psychoactive plant material "kratom", which according to numerous anecdotal reports shows efficacy in self-medication for pain syndromes, depression, anxiety, and substance use disorders. We have developed a synthetic method for selective functionalization of the unexplored C11 position of the MG scaffold (C6 position in indole numbering) via the use of an indole-ethylene glycol adduct and subsequent iridium-catalyzed borylation. Through this work we discover that C11 represents a key locant for fine-tuning opioid receptor signaling efficacy. 7-Hydroxymitragynine (7OH), the parent compound with low efficacy on par with buprenorphine, is transformed to an even lower efficacy agonist by introducing a fluorine substituent in this position (11-F-7OH), as demonstrated in vitro at both mouse and human mu opioid receptors (mMOR/hMOR) and in vivo in mouse analgesia tests. Low efficacy opioid agonists are of high interest as candidates for generating safer opioid medications with mitigated adverse effects.

• MeSH
• analgetika chemie   farmakologie   MeSH
• chemické modely MeSH
• ethylenglykol chemie   MeSH
• lidé MeSH
• Mitragyna chemie   MeSH
• molekulární struktura MeSH
• myši knockoutované MeSH
• myši MeSH
• receptory opiátové mu agonisté   genetika   metabolismus   MeSH
• rostlinné extrakty chemie   farmakologie   MeSH
• sekologanin-tryptaminové alkaloidy chemie   farmakologie   MeSH
• vazba proteinů MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Research Support, N.I.H., Extramural MeSH
• Názvy látek
• 7-hydroxymitragynine MeSH Prohlížeč
• analgetika MeSH
• ethylenglykol MeSH
• receptory opiátové mu MeSH
• rostlinné extrakty MeSH
• sekologanin-tryptaminové alkaloidy MeSH

This work describes the preparation of transparent TiO₂ nanotube (TNT) arrays on fluorine-doped tin oxide (FTO) substrates. An optimized electrolyte composition (0.2 mol dm-3 NH₄F and 4 mol dm-3 H₂O in ethylene glycol) was used for the anodization of Ti films with different thicknesses (from 100 to 1300 nm) sputtered on the FTO glass substrates. For Ti thicknesses 600 nm and higher, anodization resulted in the formation of TNT arrays with an outer nanotube diameter around 180 nm and a wall thickness around 45 nm, while for anodized Ti thicknesses of 100 nm, the produced nanotubes were not well defined. The transmittance in the visible region (λ = 500 nm) varied from 90% for the thinnest TNT array to 65% for the thickest TNT array. For the fabrication of transparent TNT arrays by anodization, the optimal Ti thickness on FTO was around 1000 nm. Such fabricated TNT arrays with a length of 2500 nm exhibit stable photocurrent densities in aqueous electrolytes (~300 µA cm-2 at potential 0.5 V vs. Ag/AgCl). The stability of the photocurrent response and a sufficient transparency (≥65%) enables the use of transparent TNT arrays in photoelectrochemical applications when the illumination from the support/semiconductor interface is a necessary condition and the transmitted light can be used for another purpose (photocathode or photochemical reaction in the electrolyte).

• Klíčová slova
• FTO, TiO2, anodization, nanotubular, photocurrent, sputtered Ti, transparent,
• MeSH
• amoniové sloučeniny MeSH
• elektrody MeSH
• ethylenglykol chemie   MeSH
• fluor chemie   MeSH
• fluoridy chemie   MeSH
• fotochemické procesy MeSH
• kvartérní amoniové sloučeniny chemie   MeSH
• nanotechnologie metody   MeSH
• nanotrubičky chemie   ultrastruktura   MeSH
• sloučeniny cínu chemie   MeSH
• sluneční energie MeSH
• titan chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• Názvy látek
• ammonium fluoride MeSH Prohlížeč
• amoniové sloučeniny MeSH
• ethylenglykol MeSH
• fluor MeSH
• fluoridy MeSH
• kvartérní amoniové sloučeniny MeSH
• sloučeniny cínu MeSH
• stannic oxide MeSH Prohlížeč
• titan MeSH
• titanium dioxide MeSH Prohlížeč

The conservation of sturgeons is of critical importance, and optimization of long-term storage is crucial to cell survival. This study aimed to examine the viability rates of several variations of sturgeon testicular cells storage at -80 °C for purpose of a short-term storage in a deep freezer or shipment on dried ice. Testes extracted from three immature fish were cut into small pieces, immersed in a cryomedium composed of phosphate buffered saline with 0.5% bovine serum albumin, 50 mM glucose, and 1.5 M ethylene glycol as a cryoprotectant, chilled from 10 to -80 °C at a cooling rate of 1 °C per min, and stored under varying conditions. Our results revealed a significant effect of storage conditions on the number of living and dead cells (p > 0.05). Samples that were stored for 7 days at -80 °C showed a considerable decline in terms of cell viability compared to samples stored for 2 days storage at -80 °C or in LN. This result indicated that testicular cells can be stored at -80 °C and/or on dry ice, for 2 days with minimum loss of viability.

• Klíčová slova
• Aciperserids, Cryopreservation, Germ cells, Sterlet,
• MeSH
• ethylenglykol farmakologie   MeSH
• kryoprezervace metody   MeSH
• kryoprotektivní látky farmakologie   MeSH
• ohrožené druhy MeSH
• ryby * MeSH
• teplota MeSH
• testis cytologie   MeSH
• uchovávání orgánů metody   MeSH
• viabilita buněk MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• ethylenglykol MeSH
• kryoprotektivní látky MeSH

Several sturgeon species are near extinction; therefore an efficient conservation strategy is required. Germ stem cells can be used for long-term storage and restoration of genetic information using surrogate reproduction. This study compared cryopreservation procedures of early stages of Siberian sturgeon Acipenser baerii testicular and ovarian cells. Whole gonad tissue or dissociated cells were frozen at a cooling rate of 1 °C/min in phosphate buffered saline with 0.5% bovine serum albumin, 50 mM glucose, and one of four different 1.5 M cryoprotectants: dimethyl sulfoxide, glycerol, ethylene glycol, or dimethyl sulfoxide with propanediol. The number of living cells obtained from 0.1 g of gonadal tissue after freeze/thaw of both whole tissue and dissociated cells was higher using ethylene glycol than with other cryoprotectants. Although there were no differences in the number of living cells in cryopreserved whole tissue vs. dissociated cells, the number of dead cells was lower with whole tissue cryopreservation, indicating that cells that died during freeze/thaw were digested during subsequent enzymatic dissociation. This resulted in more than 90% live cells after freeze/thaw and dissociation. The thawed tissue cryopreserved using ethylene glycol as protectant as well as fresh gonadal tissue were dissociated, and the cells were labelled by PKH26 and transplanted into larvae of sterlet Acipenser ruthenus. Ninety days post-transplant of both fresh and cryopreserved cells, introduced cells proliferated in more than half of the recipients.

• Klíčová slova
• Cryopreservation, Germ cells, Germ-line chimera, Oogonia, Spermatogonia, Sturgeon,
• MeSH
• dimethylsulfoxid farmakologie   MeSH
• ethylenglykol farmakologie   MeSH
• glycerol farmakologie   MeSH
• kryoprezervace metody   MeSH
• kryoprotektivní látky farmakologie   MeSH
• ohrožené druhy MeSH
• orgánové kultury - kultivační techniky MeSH
• ovum cytologie   účinky léků   transplantace   MeSH
• proliferace buněk účinky léků   MeSH
• propylenglykol farmakologie   MeSH
• ryby fyziologie   MeSH
• spermie cytologie   účinky léků   transplantace   MeSH
• viabilita buněk účinky léků   MeSH
• zmrazování MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• dimethylsulfoxid MeSH
• ethylenglykol MeSH
• glycerol MeSH
• kryoprotektivní látky MeSH
• propylenglykol MeSH

This study examined the effect of cryoprotectants on DNA integrity, antioxidant defense, and resistance to oxidative stress in cryopreserved sterlet Acipenser ruthenus sperm. The freeze-thaw process significantly influenced sperm motility, with significant differences among cryoprotectants. In vitro exposure of cryopreserved sperm to the xanthine-xanthine oxidase (X-XO) system as a model reactive oxygen species inducer resulted in a lesser motility rate and velocity compared to the control, and there was a decrease in these variables in a time- and dose-dependent manner. The greatest X (0.6mM)-XO (0.05U/mL) concentration and incubation period (30min) was associated with 62% DNA fragmentation in sperm cryopreserved with 10% ethylene glycol (EG). The maximum lipid peroxidation (LPO) and carbonyl derivatives of proteins (CP) was also observed in sperm cryopreserved with 10% EG and exposed to the X-XO system at a concentration of 0.6mM X-0.05U/mL XO. The frozen/thawed sperm containing 10% EG and that with 10% dimethyl sulfoxide (DMSO) had a significant enhancement of superoxide dismutase (SOD) and glutathione reductase (GR) activity. The current study confirms that EG is not effective for cryopreservation, and sterlet sperm were highly sensitive to free radicals after cryopreservation with EG.

• Klíčová slova
• Cryopreservation, Cryoprotectant, DNA damage, Reactive oxygen species, Sperm quality, Sterlet sperm,
• MeSH
• acetamidy farmakologie   MeSH
• dimethylsulfoxid farmakologie   MeSH
• DNA účinky léků   MeSH
• ethylenglykol farmakologie   MeSH
• fragmentace DNA účinky léků   MeSH
• kryoprezervace veterinární   MeSH
• kryoprotektivní látky farmakologie   MeSH
• methanol farmakologie   MeSH
• oxidace-redukce účinky léků   MeSH
• oxidační stres účinky léků   MeSH
• ryby * fyziologie   MeSH
• spermie účinky léků   MeSH
• zvířata MeSH
• Check Tag
• mužské pohlaví MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• acetamidy MeSH
• dimethylacetamide MeSH Prohlížeč
• dimethylsulfoxid MeSH
• DNA MeSH
• ethylenglykol MeSH
• kryoprotektivní látky MeSH
• methanol MeSH

We report a novel and multifaceted approach for the quick synthesis of highly stable single-stranded DNA (ssDNA) functionalized gold nanoparticles (AuNPs). The method is based on the combined effect of surface passivation by (1-mercaptoundec-11-yl)hexa(ethylene glycol) and low pH conditions, does not require any salt pretreatment or high excess of ssDNA, and can be generalized for oligonucleotides of any length or base sequence. The synthesized ssDNA-coated AuNPs conjugates are stable at salt concentrations as high as 3.0 M, and also functional and specific toward DNA-DNA hybridization, as shown from UV-vis spectrophotometry, scanning electron microscopy, gel electrophoresis, fluorescence, and small angle X-ray scattering based analyses. The method is highly flexible and shows an additional advantage of creating ssDNA-AuNP conjugates with a predefined number of ssDNA strands per particle. Its simplicity and tenability make it widely applicable to diverse biosensing applications involving ssDNA functionalized AuNPs.

• Klíčová slova
• DNA functionalization, gold nanoparticles, oligo ethylene glycol, salt-stability, specificity, surface passivation, variable DNA density,
• MeSH
• ethylenglykol chemie   MeSH
• fluorescence MeSH
• hybridizace nukleových kyselin MeSH
• jednovláknová DNA chemie   genetika   MeSH
• kovové nanočástice chemie   MeSH
• oligonukleotidy chemie   genetika   MeSH
• zlato chemie   MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• ethylenglykol MeSH
• jednovláknová DNA MeSH
• oligonukleotidy MeSH
• zlato MeSH

OBJECTIVES: A simple, cost-effective, and fast gas chromatography method with mass spectrometry detection (GC-MS) for simultaneous measurement of ethylene glycol, 1,2-propylene glycol and glycolic acid was developed and validated for clinical toxicology purposes. DESIGN AND METHODS: Successful derivatization of glycolic acid with isobutyl chloroformate was achieved directly in serum/urine while glycols are simultaneously derivatized by phenylboronic acid. The entire sample preparation procedure is completed within 10 min. RESULTS: The assay was proved to be quadratic in the range of 50 to 5000 mgL(-1) with adequate accuracy (96.3-105.8%) and precision (CV ≤ 8.9%). CONCLUSION: The method was successfully applied to quantify the selected compounds in serum of patients from emergency units and the results correlated well with parallel GC-FID measurements (R(2) 0.9933 for ethylene glycol and 0.9943 for glycolic acid).

• Klíčová slova
• Chloroformate, GC-MS, Glycolic acid, Glycols, Toxicology,
• MeSH
• analýza nákladů a výnosů * MeSH
• časové faktory MeSH
• ethylenglykol krev   moč   MeSH
• glykoláty krev   moč   MeSH
• lidé MeSH
• náhlé příhody MeSH
• plynová chromatografie s hmotnostně spektrometrickou detekcí ekonomika   metody   MeSH
• toxikologie MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• ethylenglykol MeSH
• glycolic acid MeSH Prohlížeč
• glykoláty MeSH

A simple, cost effective, and fast gas chromatography method with flame ionization detection (GC-FID) for simultaneous measurement of ethylene glycol, 1,2-propylene glycol and glycolic acid was developed and validated for clinical toxicology purposes. This new method employs a relatively less used class of derivatization agents - alkyl chloroformates, allowing the efficient and rapid derivatization of carboxylic acids within seconds while glycols are simultaneously derivatized by phenylboronic acid. The entire sample preparation procedure is completed within 10 min. To avoid possible interference from naturally occurring endogenous acids and quantitation errors 3-(4-chlorophenyl) propionic acid was chosen as an internal standard. The significant parameters of the derivatization have been found using chemometric procedures and these parameters were optimized using the face-centered central composite design. The calibration dependence of the method was proved to be quadratic in the range of 50-5000 mg mL(-1), with adequate accuracy (92.4-108.7%) and precision (9.4%). The method was successfully applied to quantify the selected compounds in serum of patients from emergency units.

• Klíčová slova
• Chloroformate, Experimental design, GC, Glycolic acid, Glycols,
• MeSH
• chromatografie plynová metody   MeSH
• ethylenglykol krev   otrava   moč   MeSH
• glykoláty krev   otrava   moč   MeSH
• lidé MeSH
• plamínková ionizace metody   MeSH
• propylenglykol krev   otrava   moč   MeSH
• sérum chemie   MeSH
• studie případů a kontrol MeSH
• toxikologie metody   MeSH
• urgentní zdravotnické služby * MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• srovnávací studie MeSH
• Názvy látek
• ethylenglykol MeSH
• glycolic acid MeSH Prohlížeč
• glykoláty MeSH
• propylenglykol MeSH

We have analyzed the molecular mechanisms of photoinduced cell death using porphyrins with similar structure differing only in the position of the ethylene glycol (EG) chain on the phenyl ring. Meta- and para-positioned EG chains targeted porphyrins to different subcellular compartments. After photoactivation, both types of derivatives induced death of tumor cells via reactive oxygen species (ROS). Para derivatives pTPP(EG)4 and pTPPF(EG)4 primarily accumulated in lysosomes activated the p38 MAP kinase cascade, which in turn induced the mitochondrial apoptotic pathway. In contrast, meta porphyrin derivative mTPP(EG)4 localized in the endoplasmic reticulum (ER) induced dramatic changes in Ca(2+) homeostasis manifested by Ca(2+) rise in the cytoplasm, activation of calpains and stress caspase-12 or caspase-4. ER stress developed into unfolded protein response. Immediately after irradiation the PERK pathway was activated through phosphorylation of PERK, eIF2α and induction of transcription factors ATF4 and CHOP, which regulate stress response genes. PERK knockdown and PERK deficiency protected cells against mTPP(EG)4-mediated apoptosis, confirming the causative role of the PERK pathway.

• MeSH
• apoptóza účinky léků   účinky záření   MeSH
• ethylenglykol chemie   MeSH
• fotochemoterapie * MeSH
• genový knockdown MeSH
• homeostáza účinky léků   účinky záření   MeSH
• iniciační kaspasy metabolismus   MeSH
• kaspasa 2 metabolismus   MeSH
• kinasa eIF-2 nedostatek   genetika   metabolismus   MeSH
• lidé MeSH
• mitogenem aktivované proteinkinasy p38 metabolismus   MeSH
• nádorové buněčné linie MeSH
• porfyriny chemie   farmakologie   MeSH
• reaktivní formy kyslíku metabolismus   MeSH
• signální transdukce účinky léků   účinky záření   MeSH
• stres endoplazmatického retikula účinky léků   účinky záření   MeSH
• subcelulární frakce účinky léků   metabolismus   účinky záření   MeSH
• vápník metabolismus   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH
• práce podpořená grantem MeSH
• Názvy látek
• CASP4 protein, human MeSH Prohlížeč
• ethylenglykol MeSH
• iniciační kaspasy MeSH
• kaspasa 2 MeSH
• kinasa eIF-2 MeSH
• mitogenem aktivované proteinkinasy p38 MeSH
• PERK kinase MeSH Prohlížeč
• porfyriny MeSH
• reaktivní formy kyslíku MeSH
• vápník MeSH