Molecules最新文献

BODIPY compounds are important organic dyes with exceptional spectral and photophysical properties and numerous applications in different scientific fields. Their widespread applications have flourished due to their easy structural modifications, which enable the preparation of different molecular structures with tunable spectral and photophysical properties. To date, researchers have mostly devoted their efforts to modifying BODIPY meso-position or pyrrole rings, whereas the substitution of fluorine atoms remains largely unexplored. However, chemistry of the boron atom is possible, and it enables tuning of the photophysical properties of the dyes, without tackling their spectral properties. Furthermore, modifications of boron affect the solubility and aggregation propensity of the molecules. This review article highlights methods for the preparation of 4-substituted compounds and the most important reactions on the boron of the BODIPY dyes. They were divided into reactions promoted by Lewis acid (AlCl₃ or BCl₃), or bases such as alkoxides and organometallic reagents. By using these two methodologies, it is possible to cleave B-F bonds and substitute them with B-C, B-N, or B-O bonds from different nucleophiles. A special emphasis in this review is given to still underdeveloped photochemical reactions of the boron atom of BODIPY dyes. These reactions have the potential to be used in the development of a new line of BODIPY photo-cleavable protective groups (also known as photocages) with bio-medicinal and photo-pharmacological applications, such as drug delivery.

Studies were conducted focusing on the drying of chili pepper fruits (Capsicum annuum L.), cultivar Cyklon, using convective (AD), convective-microwave (AMD), vacuum (VD), and freeze-drying (FD) methods. The influence of the drying method and temperature on the kinetics of the process and selected quality attributes of the dried product were evaluated. It was demonstrated that the Midilli model best described the drying kinetics for all methods across the entire measurement range. FD and VD produced dried products with the highest brightness and the greatest value of the a* color parameter. The lowest b* color parameter was observed for the product dried using FD at 40 °C, while the highest b* value was noted for samples dried using AMD (100 W) at 60 °C. The highest carotenoid retention was achieved with the FD method at 40 °C, while the lowest carotenoid content was found in the product obtained using the AMD method (100 W) at 60 °C. The smallest losses of capsaicinoids were observed after FD drying at 40 °C, while the largest were found for AMD (100 W) at 60 °C. The analysis of chili pepper fruit extracts revealed the quantitative composition of 12 main phenolic compounds using the UHPLC-UV method. The highest polyphenol content was obtained with FD, while the lowest total polyphenol content was recorded after AD. Regardless of temperature, the total flavonoid content was highest in extracts from FD products, and the lowest flavonoid content was found after AMD at 100 W. For all drying methods analyzed, the total flavonoid content in the pepper extracts decreased with increasing temperature.

Efficiently treating wastewater, particularly the elimination of heavy metal ions from water systems, continues to be one of the most pressing and complex challenges in modern environmental management. In this work, reduced graphene oxide coupled silver molybdate binary nanocomposites (RGO-Ag₂MoO₄ NCs) have been prepared via hydrothermal method. The crystalline nature and surface properties of the developed RGO-Ag₂MoO₄ NCs were proved by XRD, FTIR, SEM, and EDS techniques. Adsorption experiments demonstrated that the nanocomposites (NCs) effectively removed Pb(II) ions within 120 min, achieving a maximum removal efficiency ranging from 94.96% to 86.37% for Pb(II) concentrations between 20 and 100 mg/L at pH 6. Kinetic studies showed that the adsorption process followed a pseudo-second order model. Isotherm analysis presented that the Langmuir model provided the greatest fit for the equilibrium data, with a monolayer adsorption capacity of 128.94 mg/g. Thermodynamic analysis revealed that the adsorption process was spontaneous and endothermic. The results of this study highlight RGO-Ag₂MoO₄ NCs as a highly promising and eco-friendly material for the effective elimination of Pb(II) ions from wastewater. Their strong adsorption capacity, coupled with sustainable properties, makes them an efficient solution for addressing lead contamination, offering significant potential for practical applications in water treatment systems.

Hydroxycamptothecin (HCPT) is commonly used in the treatment of liver cancer; however, its low water solubility and poor stability significantly limit its clinical application. In recent years, research on exosomes has deepened considerably. Exosomes possess a unique phospholipid bilayer structure, enabling them to traverse tissue barriers, which provides natural advantages as drug carriers. Nevertheless, delivering exosomes safely and efficiently to target cells remains a major challenge. In this study, we utilized the affinity of the SP94 peptide for human liver cancer cell receptors. HCPT was coated with exosomes in our experimental design, and the exosome membrane was modified with SP94 peptide to facilitate drug delivery to liver cancer cells. Exosomes were purified from bone marrow mesenchymal stem cells, and targeted peptides were attached to their surfaces via post-insertion techniques. Subsequently, HCPT was incorporated into the exosomes through electroporation. Using the HepG2 hepatoma cell line, we evaluated a series of in vitro pharmacodynamics and studied pharmacokinetics and tissue distribution in animal models. The results indicated that ligand-targeted, modified drug-carrying exosomes significantly enhance drug bioavailability, prolong retention time in vivo, and facilitate liver targeting. Moreover, this approach reduces drug nephrotoxicity, enhances anti-tumor efficacy, and lays the groundwork for the development of novel liver cancer-targeting agents.

Studies on particulate air pollution indicate that a new type of pollutant should be considered from mainly fossil fuel combustion and automobile exhaust emissions, i.e., environmentally persistent free radicals. These radicals, ubiquitous in the environment, have a long life span and are capable of producing harmful reactive oxygen species. Samples of dandelion were collected in 2020 and 2021 in spring and late summer. Roots, leaves, flower stalks, and inflorescences of Taraxacum sp. were collected from six sites with three plants each, along with monitoring of particulate matter air pollution. Four sites were located at streets with heavy traffic and two were control sites in the rural part of the city. The free radical content in each part of the plant was measured by electron paramagnetic resonance. The leaf was selected as the most appropriate part of the plant for the measurement of carbon-derived free radicals. The g_eff value and the total number of spins were calculated. Relationships were found between location, season, and measurements. The electron paramagnetic resonance spectrum consists of at least two components, which can be attributed to C-type radicals and mixed C + O radicals. Their increase in numbers in the fall seasons, compared to the spring seasons, is also noticeable. It has also been observed that leaves collected in autumn have a higher g_eff value, which is probably related to the higher amount of oxygen- and carbon-derived free radicals.

Activating tumor necrosis factor receptor 1 (TNFR1) with tumor necrosis factor alpha (TNFα) is one of the key pathological mechanisms resulting in the exacerbation of rheumatoid arthritis (RA) immune response. Despite various types of drugs being available for the treatment of RA, a series of shortcomings still limits their application. Therefore, developing novel peptide drugs that target TNFα-TNFR1 interaction is expected to expand therapeutic drug options. In this study, the detailed interaction mechanism between TNFα and TNFR1 was elucidated, based on which, a series of linear peptides were initially designed. To overcome its large conformational flexibility, two different head-to-tail cyclization strategies were adopted by adding a proline-glycine (GP) or cysteine-cysteine (CC) to form an amide or disulfide bond between the N-C terminal. The results indicate that two cyclic peptides, R1_CC4 and α_CC8, exhibit the strongest binding free energies. α_CC8 was selected for further optimization using virtual mutations through in vitro activity and toxicity experiments due to its optimal biological activity. The L16R mutant was screened, and its binding affinity to TNFR1 was validated using ELISA assays. This study designed a novel cyclic peptide structure with potential anti-inflammatory properties, possibly bringing an additional choice for the treatment of RA in the future.

The present study evaluated the physicochemical parameters, polyphenolics content, levels of heat-induced compounds (acrylamide, furfural, 5-hydroxymethylfurfural), antioxidant properties, as well as sensory quality of shortbread cookies enriched with dried sea buckthorn fruit (SBF). The SBF-enriched cookies were prepared by replacing 1, 2, 3, or 5% of the flour with dried sea buckthorn fruit. Our results showed the presence of 12 phenolic acids and 5 flavonoids in the SBF, while two phenolic acids and two flavonoids were detected in the cookies. Most of the compounds were identified in the cookies enriched with 5% SBF. Among the phenolic acids, benzoic acid was the most abundant, while among the flavonoids, quercetin was the most abundant. 5-hydroxymethylofurfural was not detected in any cookies, and the addition of SBF contributed to the presence of furfural in baked products and increased the amount of acrylamide, and their content increased with the amount of SBF addition. The addition of sea buckthorn fruit at 5% distinctly exceeded the benchmark level of acrylamide in the cookies and worsened their sensory quality. It should also be noted that SBF significantly (p < 0.05) improved the antioxidant potential determined by two tests, ABTS and DPPH. The SBF-enriched cookies were characterized by significantly higher values of crispness and browning index compared to the control cookies. The results of the study indicate that SBF can be successfully used as a component of bakery products. In conclusion, the cookies with SBF can show improved technological and functional properties and constitute an added value bakery product that could provide health benefits.

Bladder cancer, which has a rising incidence, is the 10th most common cancer. The transitional cell carcinoma histotype is aggressive and often current therapies are ineffective. We investigated the anti-proliferative effect of quercetin, a natural flavonoid, in combination with the alkylating agent mafosfamide (MFA) on two human bladder cancer cell lines, namely RT112 and J82, representing the progression from low-grade to high-grade tumors, respectively. In both cell types, the combined treatment led to a synergic reduction in cell viability confirmed by a combination index of less than one, though different biological responses were noted. In J82 cells, MFA alone and, to a lesser extent, with quercetin caused cell cycle arrest in the G2/M phase, but only the combined treatment triggered apoptotic cell death. In contrast, in RT112 cells, quercetin induced autophagy, evidenced by the autophagosome formation and the increase in LC-3 lipidation. Interestingly, the synergistic effect was observed only when cells were pre-treated with MFA for 24 h before adding quercetin, not in the reverse order. This suggests that quercetin may help overcome MFA resistance to apoptosis. Although further studies are needed, investigating the combined effects of quercetin and MFA could help elucidate the mechanisms of drug resistance in bladder cancer treatment.

The coupling of Solid-Phase Microextraction (SPME) technology with gas chromatography (GC) has a well-established and successful history. Traditionally, SPME fibers have been the most popular form thanks to their versatility and the ease with which they can be fully automated. However, alternative geometries for SPME have been developed over the years, beginning with Stir Bar Sorptive Extraction (SBSE) and later evolving into Thin-Film SPME (TF-SPME) devices. Each of these formats offers distinct advantages and disadvantages, which are explored in this study. The primary objective of this study was to comprehensively compare available forms of SPME devices, with a special focus on the advantages of TF-SPME, a novel microextraction method particularly suited for the analysis of odorants in food. The study involved analyzing a standard mixture of 11 key food odorants, representing a range of polarities, to evaluate the efficiency of TF-SPME devices in terms of the number of analytes extracted. Furthermore, four types of TF-SPME devices were compared against each other in both standard mixtures and actual food samples. The final stage of the study employed GCxGC-ToFMS analysis to showcase the potential of the most efficient HLB-TF-SPME device in the non-targeted analysis of complex samples, exemplified by unfiltered wheat beer. This analysis demonstrated the significant capability of HLB-TF-SPME in capturing and identifying a wide range of volatile compounds in complex matrices.

Endometriosis is a gynecological disease for which the diagnostics are difficult and often invasive; therefore, non-invasive diagnostic methods using sensitive and specific parameters present in easily available body fluid such as blood serum are needed for the detection of this disease. Our study aimed to answer the question of whether there are any differences between women with advanced endometriosis (AE), patients with gynecological diseases other than endometriosis (NE), and healthy women (control) in terms of the number of antennas of N-glycans from serum IgG. The degree of branching of IgG N-glycans was determined by a modified lectin ELISA with biotinylated lectin Con A (Canavalia ensiformis agglutinin) recognizing α-linked mannose, specifically reacting with biantennary N-glycans. The PHA-L/Con A ratio was calculated from the obtained N-glycan reactivities with Con A and PHA-L (Phaseolus vulgaris leucoagglutinin, specific to tri- and/or tetra-antennary N-linked glycans). The expression of Con A-reactive biantennary N-glycans in serum IgG was significantly lower in the control group than in the NE group (p = 0.045). The values of the PHA-L/Con A ratio were significantly higher in the NE group than in the AE and control groups (p = 0.019 and p = 0.022, respectively). The PHA-L/Con A ratio could be taken into account as a parameter helpful in the non-invasive diagnosis of advanced endometriosis, thus differentiating this disease from other gynecological diseases with an inflammatory background.