Acid-Base Equilibrium of 5,5,6-Trihydroxy-6-Methyldihydropyrimidine-2,4(1,3)-Dione in the Gas Phase and in Water.

The first-stage acid-base equilibrium of 5,5,6-trihydroxy-6-methyldihydropyrimidine-2,4(1,3)-dione was studied for the first time in aqueous solutions. Its constant (pK = 9.23 ± 0.

Discovery of Potent Dengue Virus NS2B-NS3 Protease Inhibitors Among Glycyrrhizic Acid Conjugates with Amino Acids and Dipeptides Esters.

This study investigated a library of known and novel glycyrrhizic acid (GL) conjugates with amino acids and dipeptide esters, as inhibitors of the DENV NS2B-NS3 protease. We utilized docking algorithms to evaluate the interactions of these GL derivatives with key residues (His51, Asp75, Ser135, and Gly153) within 10 Å of the DENV-2 NS2B-NS3 protease binding pocket (PDB ID: 2FOM). It was found that compounds and exhibited unique binding patterns, forming hydrogen bonds with Asp75, Tyr150, and Gly153.

Effect of Herbicide-Resistant Oil-Degrading Bacteria on Plants in Soil Contaminated with Oil and Herbicides.

Biological remediation of agricultural soils contaminated with oil is complicated by the presence of residual amounts of chemical plant protection products, in particular, herbicides, which, like oil, negatively affect the soil microbiome and plants. In this work, we studied five strains of bacteria of the genera and , which exhibited a high degree of oil biodegradation (72-96%). All strains showed resistance to herbicides based on 2,4-D, imazethapyr and tribenuron-methyl, the ability to fix nitrogen, phosphate mobilization, and production of indole-3-acetic acid.

Gelation during Ring-Opening Reactions of Cellulosics with Cyclic Anhydrides: Phenomena and Mechanisms.

Cellulose esters are used in Food and Drug Administration-approved oral formulations, including in amorphous solid dispersions (ASDs). Some bear substituents with terminal carboxyl moieties (e.g.

ω-Carboxyl terminated cellulose esters are effective crystallization inhibitors for challenging drugs.

Polymeric additives are widely used to delay drug crystallization from supersaturated solutions, which is critical for enhancing oral bioavailability by amorphous solid dispersion (ASD). The efficacy of these polymers relies on their capacity to inhibit nucleation and subsequent crystal growth. Drug nucleation is pivotal to crystallization; therefore, effective polymers are essential for suppressing nucleation from supersaturated solutions.

Optimizing Allelopathy Screening Bioassays by Using Nano Silver.

Nano solutions are widely used in medicine and also have the potential to be used when performing allelopathy screening studies. The present experiment aimed to test the effectiveness of colloidal nano silver Silver-Amber© with nanoparticles of 20 nm (>20 mg/L at a purity level of 99.99%) as a carrier of allelochemicals in laboratory conditions.

Chronic Cerebellar Meningoencephalitis in Adulthood: A Report of a Rare Case.

The development of meningoencephalitis is a result of an inflammation of the meninges and the brain, which can cause neurological sequelae. Cerebellar meningoencephalitis in adult patients is extremely rare and requires special diagnostic approaches. The aim of this report is to present a rare case of meningoencephalitis and evaluate the diagnostic and therapeutic techniques.

Awake Craniotomy for a Frontal Astrocytoma: A Case Report.

Awake craniotomy is a surgical procedure that has been gaining significance over the past decades. Neuronavigation is an intraoperative technology that locates tumors and monitors the brain cortex during awake craniotomy. The presence of cerebral low-grade gliomas in the frontal lobe creates a risk of affecting vital centers of the brain cortex during surgery.

Double Trouble: A Case Report on the Surgical Management of Dual Intracranial Metastases.

Intracranial metastasis disease (IMD) has proven to be a frequent secondary occurrence, usually for primary cancers such as lung, breast, and melanoma, which have a high possibility of metastasizing to the brain. Due to the reasons listed above, treatment and early diagnosis are incredibly challenging. In the past decade, medicine has developed much better imaging solutions and radiological and surgical approaches, increasing the postoperative survival prognosis and achieving more time-efficient results.

Glycyrrhizic acid conjugates with amino acid methyl esters target the main protease, exhibiting antiviral activity against wild-type and nirmatrelvir-resistant SARS-CoV-2 variants.

COVID-19 pandemic is predominantly caused by SARS-CoV-2, with its main protease, Mpro, playing a pivotal role in viral replication and serving as a potential target for inhibiting different variants. In this study, potent Mpro inhibitors were identified from glycyrrhizic acid (GL) derivatives with amino acid methyl/ethyl esters. Out of the 17 derivatives semisynthesized, Compounds 2, 6, 9, and 15, with methionine methyl esters, D-tyrosine methyl esters, glutamic acid methyl esters, and methionines in the carbohydrate moiety, respectively, significantly inhibited wild-type SARS-CoV-2 Mpro-mediated proteolysis, with IC50 values ranging from 0.

Threading the needle: Achieving simplicity and performance in cellulose alkanoate ω-carboxyalkanoates for amorphous solid dispersion.

Most active pharmaceutical ingredients (APIs) suffer from poor water solubility, often keeping them from reaching patients. To overcome the issues of poor drug solubility and subsequent low bioavailability, amorphous solid dispersions (ASDs) have garnered much attention. Cellulose ester derivatives are of interest for ASD applications as they are benign, sustainable-based, and successful in commercial drug delivery systems, e.

Synthesis, modification and biological activity of 2,3-indoles of Glycyrrhetinic acid.

The synthesis of 2,3-indoles of Glycyrrhetinic acid (GLA) and its methyl ester was carried out by the Fischer reaction. Reductive transformations of GLA methyl ester 2,3-indole were carried out to obtain 11-deoxo- and 9,12-diene analogs. N-methylation of 2,3-indole gave N-methyl-indole-11-oxo-18β-olean-12-en-30-oic acid.

The impact of the application of compochar on soil moisture, stress, yield and nutritional properties of legumes under drought stress.

Nowadays, when climate change is becoming more and more evident, drought stress plays a very important role, including in agriculture. The increasing number of years with extreme temperatures in the Czech Republic has a negative impact on agricultural production, among other things. Therefore, ways are being sought to reduce these negative impacts.

Solvent-Free Synthesis of Multifunctional Block Copolymer and Formation of DNA and Drug Nanocarriers.

The synthesis of well-defined multifunctional polymers is of great importance for the development of complex materials for biomedical applications. In the current work, novel and multi-amino-functional diblock copolymer for potential gene and drug delivery applications was successfully synthesized. A highly efficient one-step and quantitative modification of an alkyne-functional polycarbonate-based precursor was performed, yielding double hydrophilic block copolymer with densely grafted primary amine side groups.

Priming of seeds with stabilized nanomicelles: effects on seedling development and photosynthetic function.

Natural and synthetic polymers are widely explored for improving seed germination and plant resistance to environmental constraints. Here, for the first time, we explore stabilized nanomicelles composed of the biocompatible triblock co-polymer (SPM) as a priming agent for (var. RAN-1) seeds.

Tuning polymer-blood and polymer-cytoplasm membrane interactions by manipulating the architecture of poly(2-oxazoline) triblock copolymers.

Bioactive moieties designed to bind to cell membrane receptors benefit from coupling with polymeric carriers that have enhanced affinity to the cell membrane. When bound to the cell surface, such carriers create a "2D solution" of a ligand with a significantly increased concentration near a membrane-bound receptor compared to a freely water-soluble ligand. Bifunctional polymeric carriers based on amphiphilic triblock copolymers were synthesized from 2-pent-4-ynyl oxazoline, 2-nonyl oxazoline and 2-ethyl oxazoline.

Green Synthesis and the Evaluation of a Functional Amphiphilic Block Copolymer as a Micellar Curcumin Delivery System.

Polymer micelles represent one of the most attractive drug delivery systems due to their design flexibility based on a variety of macromolecular synthetic methods. The environmentally safe chemistry in which the use or generation of hazardous materials is minimized has an increasing impact on polymer-based drug delivery nanosystems. In this work, a solvent-free green synthetic procedure was applied for the preparation of an amphiphilic diblock copolymer consisting of biodegradable hydrophobic poly(acetylene-functional carbonate) and biocompatible hydrophilic polyethylene glycol (PEG) blocks.

Components of the Phenylpropanoid Pathway in the Implementation of the Protective Effect of Sodium Nitroprusside on Wheat under Salinity.

Nitric oxide (NO) is a multifunctional, gaseous signaling molecule implicated in both physiological and protective responses to biotic and abiotic stresses, including salinity. In this work, we studied the effects of 200 µM exogenous sodium nitroprusside (SNP, a donor of NO) on the components of the phenylpropanoid pathway, such as lignin and salicylic acid (SA), and its relationship with wheat seedling growth under normal and salinity (2% NaCl) conditions. It was established that exogenous SNP contributed to the accumulation of endogenous SA and increased the level of transcription of the pathogenesis-related protein 1 () gene.

Biodegradable Hydrogels Based on Chitosan and Pectin for Cisplatin Delivery.

Preparation of stable hydrogels using physically (electrostatically) interacting charge-complementary polyelectrolyte chains seems to be more attractive from a practical point of view than the use of organic crosslinking agents. In this work natural polyelectrolytes-chitosan and pectin-were used, due to their biocompatibility and biodegradability. The biodegradability of hydrogels is confirmed by experiments with hyaluronidase as an enzyme.

Three-Dimensional Nucleic Acid Nanostructures Based on Self-Assembled Polymer-Oligonucleotide Conjugates of Comblike and Coil-Comb Chain Architectures.

Spherical nucleic acids have emerged as a class of nanostructures, exhibiting a wide variety of properties, distinctly different from those of linear nucleic acids, and a plethora of applications in therapeutics and diagnostics. Herein, we report on preparation of 3D nucleic acid nanostructures, prepared by self-assembly of polymer-oligonucleotide conjugates. The latter are obtained by grafting multiple alkyne-functionalized oligonucleotide strands onto azide-modified homo-, block, and random (co)polymers of chloromethylstyrene via initiator-free click coupling chemistry to form conjugates of comblike and coil-comb chain architectures.

Nanoarchitectonics of Spherical Nucleic Acids with Biodegradable Polymer Cores: Synthesis and Evaluation.

Spherical nucleic acids (SNAs) have gained significant attention due to their unique properties allowing them to overcome the challenges that face current nanocarriers used for gene therapies. The aim of this study is to synthesize and characterize polymer-oligonucleotide conjugates of different architecture and to evaluate the possibility of forming SNAs with biodegradable cores. Initially, two types of azide (multi)functional polyester-based (co)polymers were successfully synthesized and characterized.

Ecotoxicity Study of Additives Composed of Zinc and Boron.

The high use of additives containing zinc borate and their limited solubility in water both lead to its persistence and accumulation in biological systems. On the other hand, soluble forms of boron are easily available to plant roots and are taken up by plants. There are no ecotoxicological data available for zinc borate, the industrial utilization of which is widespread.