Search Results (148)

Bone diseases lead to an increasing demand for implants to treat long bone defects and for load-bearing applications. Osteoporosis care and accidental injuries are major contributors to this rising need. Our research aims to demonstrate innovative material systems and methods for preparing implants that can be used in regenerative medicine. We hypothesize that by combining titanium alloys (Ti6Al4V) with hydroxyapatite (Hap), we can enhance biocompatibility and tribo-mechanical performance, which are critical for the longevity of Ti-based surgical implants. Additionally, we investigate the application of laser surface treatments to expose the underlying porosity, thereby enhancing cell transport and promoting cell growth. In this study, we investigate the effects of two fabrication techniques—Spark Plasma Sintering (SPS) and powder metallurgy (PM)—on the properties of laser-textured Ti64/Hap biocomposites. Our findings demonstrate that the selected processing route significantly influences the microstructure, tribological performance, and surface properties of these materials. An X-ray diffraction (XRD) analysis corroborates our results from incubation studies in simulated body fluids, highlighting the impact of phase transformations during sintering on the chemical properties of Ti-Hap composites. Additionally, while laser surface texturing was found to slightly increase the friction coefficient, it markedly enhanced the wear resistance, particularly for the PM and SPS Ti + 5%Hap composites. Full article

In this study, two isomeric cathinone derivatives, N-butyl-norbutylone and N-ethylhexylone, seized on the illicit drug market in Poland, were described and characterized by various instrumental analytical methods. The compounds were characterized by electrospray ionization mass spectrometry, high-resolution mass spectrometry, gas chromatography–mass spectrometry, and nuclear magnetic resonance spectroscopy. The two investigated compounds were confirmed as 1-(2H-1,3-benzodioxol-5-yl)-2-(butylamino)butan-1-one and 1-(2H-1,3-benzodioxol-5-yl)-2-(ethylamino)hexane-1-one, both of which were cathinone derivatives available on the new psychoactive substances (NPS) market. The obtained analytical data should be useful for forensic and toxicological purposes for quick and reliable compound identification. Full article

This study investigates the physicochemical properties of hydrogels based on PVA and PVP crosslinked with PEGDA, focusing on their swelling capacity, surface roughness, incubation behavior, and structural modifications upon bioactive component incorporation. Swelling analysis demonstrated that the amount and molecular weight of PEGDA significantly influences the hydrogels’ sorption properties, with the highest swelling coefficient observed for samples with 2 mL PEGDA (575 g/mol) due to a looser network structure, while the lowest was recorded for 2.5 mL PEGDA (700 g/mol), indicating a denser network. Surface roughness analysis revealed that increasing the crosslinker amount led to higher roughness both before and after incubation, with samples containing 575 g/mol PEGDA being more susceptible to structural changes in an incubation environment. FT-IR spectroscopy confirmed the presence of characteristic functional groups, providing insight into the chemical stability and hydration properties of the hydrogels. Modification with a bioactive mixture (glucosamine, chondroitin, and MSM) was confirmed by spectral analysis, indicating successful integration without compromising the hydrogel matrix. The modified hydrogels demonstrated potential applications in regenerative medicine, particularly for joint disease treatment and cartilage tissue repair. Full article

Skin represents the largest organ in the human body, functioning as a protective barrier against environmental factors while playing a critical role in thermoregulation. Acne vulgaris is recognized as the most common dermatological condition affecting adolescents, and if left untreated, it can result in lasting skin damage and associated psychosocial challenges. This study aims to develop innovative polymeric biomaterials that could effectively support the treatment of acne vulgaris. The synthesis of these biomaterials involves the use of polyethylene glycol 6000, sodium alginate, and the antioxidant protein glutathione (GHS) to create polymeric hydrogels. These hydrogels were generated via a UV-mediated crosslinking process. To enhance the functional properties of the hydrogels, zinc oxide microparticles (ZnO), synthesized through a wet precipitation method, were incorporated into the formulations. Characterization of the ZnO was performed using Fourier-Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), particle sizer analysis, and Scanning Electron Microscopy (SEM). Additionally, the bioactivity of the synthesized materials was evaluated through incubation in media simulating physiological body fluids. The cytotoxic effects of the biomaterials were assessed using an indirect test on mouse fibroblast (L929) cells, in accordance with ISO 10993-5 guidelines. The results of our research indicate that the developed biomaterials exhibit potential as a carrier for active substances, contributing positively to the treatment of acne vulgaris and potentially improving overall skin health. Full article

Background/Objectives: The principal aim of this work was to prepare a liposomal drug delivery system based on the commercial drug doxorubicin (DOX) and a budding agent with promising anticancer activity, 9-(N-piperazinyl)-5-methyl-12(H)-quino [3,4-b][1,4]benzothiazinium chloride (9-PBThACl). Methods: A spectrophotometric methodology was used to meticulously investigate the drug entrapment and release characteristics of the new liposomal complexes (L) based on dipalmitoylphosphatidylcholine (DPPC) with human serum albumin (HSA) and its defeated analog (dHSA). Results: The impact of the operational parameters (temperature and pH) on the liposome/drug(s)/(d)HSA, namely [L_{DPPC/9-PBThACl/DOX} ]:(d)HSA] systems, as well as the polarity of the phospholipid bilayer, was examined. In order to compare the experimental findings, mathematical models were employed to specify the analytical factors controlling the process of drug release/potential drug release from liposomes. The observed variations in the drug encapsulation and release profiles were due to the combination of liposomal conjugates with human plasma protein. Conclusions: It was proven that changes in the environmental pH directly affect the percentage of drug entrapment in liposomes and the medicine release efficiency. Moreover, the grouping tendency of the liposomal combinations was investigated using a principal component analysis (PCA) and a hierarchical clustering analysis (HCA). Finally, an analysis of variance (ANOVA) confirmed the statistical impact of pH buffering and changing temperature factors on the drug release characteristics of liposomal conjugates. Full article

1-Hydroxy-N-phenylnaphthalene-2-carboxamide and a series of seventeen other carboxanilides in the anilide part of dichlorinated, trichlorinated, dibrominated, tribrominated, and chlorinated/brominated variants have recently been reported as biologically active compounds mainly with antibacterial, antimycobacterial, and anticancer effects. Since lipophilicity is one of the factors influencing the bioavailability (absorption, distribution, metabolism, and elimination), activity, and even toxicity of bioactive compounds, all the derivatives were investigated for their lipophilic and hydrophilic properties. All eighteen compounds were analyzed by reversed-phase high-performance liquid chromatography (RP-HPLC). The procedure was performed under isocratic conditions with methanol as the organic modifier in the mobile phase using an end-capped non-polar C18 stationary reversed-phase column. The lipophilicity values are expressed as the logarithm of the capacity factor k (for the mobile phase water/methanol) and the distribution coefficients D at pH values of 6.5 and 7.4 (for the mobile phase buffer/methanol), as well as the calculated values of log P/Clog P by various methods. 1-Hydroxy-N-(3,4,5-trichlorophenyl)naphtha- lene-2-carboxamide and N-(4-bromo-3-chlorophenyl)-1-hydroxynaphthalene-2-carboxamide are the most lipophilic compounds of the whole series; on the other hand, surprisingly, unsubstituted 1-hydroxy-N-phenylnaphthalene-2-carboxamide is not the least lipophilic derivative. The mutual correlations between the experimental and predicted lipophilicity values are low; in addition, there are large deviations in the cross-correlations between log k and log D, which are due to the presence of a free ionizable phenolic group in the molecule. Full article

Recently reported multihalogenated (CF₃/Cl) anilides of 1-hydroxynaphthalene-2-carboxanilides showed significant activity against both the reference strain Staphylococcus aureus ATCC 29213 and clinical isolates of methicillin-resistant S. aureus (MRSA). This fact inspired further investigation of the effect of these compounds on staphylococci. Chemoproteomics is a tool for investigating protein targets of potential drugs. It makes it possible to understand the effect of a bioactive molecule on a living system. An activity-based protein profiling (ABPP) method was employed using highly active and inactive ring-substituted 1-hydroxynaphthalene-2-carboxanilides as probes. The experiment was performed on the universally sensitive collection strain S. aureus ATCC 29213. Tryptic cleavage of proteins was performed prior to HPLC-MS/MS analysis. Protein profiles of control samples (S. aureus cells) and profiles of S. aureus treated with inactive/active derivatives were investigated and compared to one another. More than 1000 proteins were analyzed, with approximately 70% of the proteins increased and 30% of the proteins decreased after treatment with the investigated compounds. Treatment with the inactive compound mainly resulted in the expression of various proteins, so it can be assumed that the changes in the protein profile did not affect the basic biochemical pathways or that the microorganism was able to adapt by activating other pathways/expressing other proteins, surviving. Treatment with the highly active agent resulted in much smaller proteomic changes (mainly, the inhibition of several proteins compared to the inactive compound), and S. aureus failed to adapt and was killed. Full article

Hard bone disease is a clinical problem affecting more than 20 million people annually worldwide, with significant health, social, and economic consequences. For successful integration of any implant, the key aspects are bone regeneration, osseointegration at the bone–implant interface, and the mitigation of inflammation. The purpose of this research work is to demonstrate an innovative material system and method of biomaterial preparation for regenerative medicine. A number of studies were carried out for both hydroxyapatite powder and composites. Wet-precipitated synthesized hydroxyapatite was compared to commercial products through accurate physicochemical studies that confirmed the high purity of the obtained calcium phosphate without any impurities. Ti/HAp composites before and after sintering were compared by XRF, XRD, SEM, EDS, PSA, and roughness measurements, and the Vickers microhardness was analyzed. The fabrication of the biomaterial was based on a bottom-up approach, which involved fabricating HAp particles with specific morphologies using powder metallurgy (PM) to sinter Ti composites. The resulting gradient structures consisting of two compositions (5%HAp%5CMC and 10%HAp10%CMC) mimic the structure of bone tissue. The created pores of 10–100 µm in size will allow bone cells to penetrate the implant and regenerate bone. In turn, the introduction of hydroxyapatite into the material reduces the microhardness of the composite and introduces properties such as bioactivity. The developed composite material contains a combination of Ti alloy and hydroxyapatite (HAp), creating an excellent biomaterial that promotes bone growth and eliminates the problem of implant loosening by integrating it into the bone. This material requires further research, especially biological research. However, it shows promising potential for further experiments. Full article

Restoring the structures and functions of tissues along with organs in human bodies is a topic gathering attention nowadays. These issues are widely discussed in the context of regenerative medicine. Excipients/delivery systems play a key role in this topic, guaranteeing a positive impact on the effectiveness of the drugs or therapeutic substances supplied. Advances in materials engineering, particularly in the development of hydrogel biomaterials, have influenced the idea of creating an innovative material that could serve as a carrier for active substances while ensuring biocompatibility and meeting all the stringent requirements imposed on medical materials. This work presents the preparation of a natural polymeric material based on pullulan modified with silymarin, which belongs to the group of flavonoids and derives from a plant called Silybum marianum. Under UV light, matrices with a previously prepared composition were crosslinked. Before proceeding to the next stage of the research, the purity of the composition of the matrices was checked using Fourier-transform infrared (FT-IR) spectroscopy. Incubation tests lasting 19 days were carried out using incubation fluids such as simulated body fluid (SBF), Ringer’s solution, and artificial saliva. Changes in pH, electrolytic conductivity, and weight were observed and then used to determine the sorption capacity. During incubation, SBF proved to be the most stable fluid, with a pH level of 7.6–7.8. Sorption tests showed a high sorption capacity of samples incubated in both Ringer’s solution and artificial saliva (approximately 350%) and SBF (approximately 300%). After incubation, the surface morphology was analyzed using an optical microscope for samples demonstrating the greatest changes over time. The active substance, silymarin, was released using a water bath, and then the antioxidant capacity was determined using the Folin–Ciocâlteu test. The tests carried out proved that the material produced is active and harmless, which was shown by the incubation analysis. The continuous release of the active ingredient increases the biological value of the biomaterial. The material requires further research, including a more detailed assessment of its balance; however, it demonstrates promising potential for further experiments. Full article

In this work, the synthesis, structural analysis and anticancer properties of 5-methyl-9-trifluoromethyl-12H-quino[3,4-b][1,4]benzothiazinium chloride (3) are described. Compound 3 was synthesized by reacting 1-methyl-4-butylthio-3-(benzoylthio)quinolinium chloride with 4-(trifluoromethyl)aniline, respectively. The structure of the resulting product was determined using ¹H-NMR and ¹³C-NMR spectroscopy as well as HR-MS spectrometry. The spatial geometry of agent 3 and the arrangement of molecules in the crystal (unit cell) were also confirmed using X-ray diffraction. The tetracyclic quinobenzothiazinium system is fairly planar because the dihedral angle between the planes formed by the benzene ring and the quinoline system is 173.47°. In order to obtain insight into the electronic charge distribution of the investigated molecule, electronic structure calculations employing the Density Functional Theory (DFT) were performed. Moreover, antiproliferative activity against a set of pancreatic cancer cell lines was tested, with compound 3 showing IC₅₀ values against human primary pancreatic adenocarcinoma BxPC-3 and human epithelioid pancreatic carcinoma Panc-1 of 0.051 µM and 0.066 µM, respectively. The IC₅₀ value of cytotoxicity/cell viability of the investigated compound assessed on normal human lung fibroblasts WI38 was 0.36 µM. Full article

A series of new unique acetylene derivatives of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonamide 3a–f and 6a–f were prepared by reactions of 8-hydroxy- and 8-methoxyquinoline- 5-sulfonyl chlorides with acetylene derivatives of amine. A series of new hybrid systems containing quinoline and 1,2,3-triazole systems 7a–h were obtained by reactions of acetylene derivatives of quinoline-5-sulfonamide 6a–d with organic azides. The structures of the obtained compounds were confirmed by ¹H and ¹³C NMR spectroscopy and HR-MS spectrometry. The obtained quinoline derivatives 3a–f and 6a–f and 1,2,3-triazole derivatives 7a–h were tested for their anticancer and antimicrobial activity. Human amelanotic melanoma cells (C-32), human breast adenocarcinoma cells (MDA-MB-231), and human lung adenocarcinoma cells (A549) were selected as tested cancer lines, while cytotoxicity was investigated on normal human dermal fibroblasts (HFF-1). All the compounds were also tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and representatives of multidrug-resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis. Only the acetylene derivatives of 8-hydroxyquinoline-5-sulfonamide 3a–f were shown to be biologically active, and 8-hydroxy-N-methyl-N-(prop-2-yn-1-yl)quinoline-5-sulfonamide (3c) showed the highest activity against all three cancer lines and MRSA isolates. Its efficacies were comparable to those of cisplatin/doxorubicin and oxacillin/ciprofloxacin. In the non-cancer HFF-1 line, the compound showed no toxicity up to an IC₅₀ of 100 µM. In additional tests, compound 3c decreased the expression of H3, increased the transcriptional activity of cell cycle regulators (P53 and P21 proteins), and altered the expression of BCL-2 and BAX genes in all cancer lines. The unsubstituted phenolic group at position 8 of the quinoline is the key structural fragment necessary for biological activity. Full article

One of the definitions of chemical biology is that it is a scientific discipline spanning the fields of chemistry, biology, and physics; it primarily involves the application of chemical techniques, tools, analyses, and often compounds (also known as chemical probes), which are produced through synthetic chemistry, in order to study and manipulate biological systems [...] Full article

Nowadays, lipidomics plays a crucial role in the investigation of novel biomarkers of various diseases. Its implementation into the field of clinical analysis led to the identification of specific lipids and/or significant changes in their plasma levels in patients suffering from cancer, Alzheimer’s disease, sepsis, and many other diseases and pathological conditions. Profiling of lipids and determination of their plasma concentrations could also be helpful in the case of drug therapy management, especially in combination with therapeutic drug monitoring (TDM). Here, for the first time, a combined approach based on the TDM of colistin, a last-resort antibiotic, and lipidomic profiling is presented in a case study of a critically ill male patient suffering from Pseudomonas aeruginosa-induced pneumonia. Implementation of innovative analytical approaches for TDM (online combination of capillary electrophoresis with tandem mass spectrometry, CZE-MS/MS) and lipidomics (liquid chromatography–tandem mass spectrometry, LC-MS/MS) was demonstrated. The CZE-MS/MS strategy confirmed the chosen colistin drug dosing regimen, leading to stable colistin concentrations in plasma samples. The determined colistin concentrations in plasma samples reached the required minimal inhibitory concentration of 1 μg/mL. The complex lipidomics approach led to monitoring 545 lipids in collected patient plasma samples during and after the therapy. Some changes in specific individual lipids were in good agreement with previous lipidomics studies dealing with sepsis. The presented case study represents a good starting point for identifying particular individual lipids that could correlate with antimicrobial and inflammation therapeutic management. Full article

The search for the ideal metallic material for an implant is still a difficult challenge for scientists due to the phenomenon of corrosion and the consequent disruption of the implant structure. Prevention is the application of coatings that protect the implant, activate the tissues for faster regeneration, and also prevent inflammation through antibacterial and antiviral effects. The present study focuses on the selection of components for a Ti-6Al-4V alloy coating. These days, researchers are taking an intense interest in extracts of natural origin. It was decided to take a look at Sideritis raeseri, which contains vitamins and valuable elements and is rich in polyphenols, as well as antioxidants. The composition of coatings based on a PEG polymer reinforced with brushite and the S. raeseri extract with the proteins L-carnosine, fibroin, or sericin was developed. The samples were subjected to detailed physiochemical analysis, including potentiometry and electrical conductivity analysis, Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), X-ray diffraction (XRD) analysis, and UV-VIS spectroscopy. The study demonstrated that polyphenols were successfully released from the coatings during incubation in vitro. The osteointegration process can be supported by a number of factors, such as the release of polyphenols from implant coatings to prevent bacterial, viral, and fungal infections. Subjecting the samples to 14 days of incubation demonstrated their interactions with the incubation fluids, an ion exchange between the medium and the materials. An analysis of the surface morphology exhibited the presence of brushite crystals and their increased number after incubation, indicating the bioactivity of the formed coatings. Full article