RESUMEN
The knowledge of interactions between different molecules is undoubtedly the driving force of all contemporary biomedical and biological sciences. Chemical biology/biological chemistry has become an important multidisciplinary bridge connecting the perspectives of chemistry and biology to the study of small molecules/peptidomimetics and their interactions in biological systems. Advances in structural biology research, in particular linking atomic structure to molecular properties and cellular context, are essential for the sophisticated design of new medicines that exhibit a high degree of druggability and very importantly, druglikeness. The authors of this contribution are outstanding scientists in the field who provided a brief overview of their work, which is arranged from in silico investigation through the characterization of interactions of compounds with biomolecules to bioactive materials.
Asunto(s)
Biología MolecularRESUMEN
Naturally occurring hydroxyapatite (HA) is the mineral phase of bone tissue. It is characterized by its bioactivity toward stimulating bone cells to proliferate and thus form new apatite layers. For this reason, it is a material commonly used in implantology for filling defects or covering implants (such as endoprostheses). There are several methods to obtain synthetic HA, and by controlling parameters such as temperature, pressure or the drying process, physicochemical parameters of the final powder can be affected. In the present study, HA was obtained by wet precipitation technique and subjected to two different drying methods, determining whether this parameter significantly affects the properties of the final material obtained. Analyzed Fourier-transform infrared spectroscopy (FT-IR) confirmed the presence of functional groups typical for HA. X-ray diffraction analysis (XRD) demonstrated that the materials are partially amorphous; however, the only phase was identified in HA. Scanning electron microscopy (SEM) was used to evaluate the surface morphology and the density, and average grain diameter was measured. Furthermore, HA powders were subjected to modification with the antibiotic clindamycin to determine the potential for use as a carrier for the active substance. The release rate of the drug was determined by high-performance liquid chromatography (HPLC). The differences in the characteristics of the powders were relatively small; however, they affected the rate of drug release from the material as well as the shape of the grains. The method of drying the powders was shown to affect the shape of the grains, as well as the porosity of the sinters prepared from it. A higher amount of clindamycin released into PBS was observed in material with more pores. The materials have demonstrated the potential to be used as a carrier for the active substance; however, further biological, as well as physicochemical, analysis is required.
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Bioactive calcium phosphate ceramics (CaPs) are one of the building components of the inorganic part of bones. Synthetic CaPs are frequently used as materials for filling bone defects in the form of pastes or composites; however, their porous structure allows modification with active substances and, thus, subsequent use as a drug carrier for the controlled release of active substances. In this study, four different ceramic powders were compared: commercial hydroxyapatite (HA), TCP, brushite, as well as HA obtained by wet precipitation methods. The ceramic powders were subjected to physicochemical analysis, including FTIR, XRD, and determination of Ca/P molar ratio or porosity. These techniques confirmed that the materials were phase-pure, and the molar ratios of calcium and phosphorus elements were in accordance with the literature. This confirmed the validity of the selected synthesis methods. CaPs were then modified with the antibiotic clindamycin. Drug release was determined on HPLC, and antimicrobial properties were tested against Staphylococcus aureus. The specific surface area of the ceramic has been demonstrated to be a factor in drug release efficiency.
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Regenerative medicine is becoming a rapidly evolving technique in today's biomedical progress scenario. Scientists around the world suggest the use of naturally synthesized biomaterials to repair and heal damaged cells. Hydroxyapatite (HAp) has the potential to replace drugs in biomedical engineering and regenerative drugs. HAp is easily biodegradable, biocompatible, and correlated with macromolecules, which facilitates their incorporation into inorganic materials. This review article provides extensive knowledge on HAp and collagen-containing compositions modified with drugs, bioactive components, metals, and selected nanoparticles. Such compositions consisting of HAp and collagen modified with various additives are used in a variety of biomedical applications such as bone tissue engineering, vascular transplantation, cartilage, and other implantable biomedical devices.
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This paper describes the plant-mediated preparation of silver nanoparticles with aqueous extract and infusion of Cistus incanus leaves. To evaluate aqueous extract and infusion antioxidant capacity and total phenolic content the DPPH and Folin-Ciocalteau methods were utilized. The antioxidant capacity and total phenolic content of extract and infusion were equal to 85.97 ± 6.54 mg gallic acid equivalents per gram of dry weight.; 10.76 ± 0.59 mg/mL and 12.65 ± 1.04 mg gallic acid equivalents per gram of dry weight.; 3.10 ± 0.14 mg/mL, respectively. The formed nanoparticles displayed the characteristic absorption band in the 380-450 nm wavelength range. The average size of particles was in the 68.8-71.2 nm range. Morphology and phase composition analysis revealed the formation of spherical nanoparticles with a face-centred cubic structure. Immune compatibility tests of nanoparticles and plant extracts showed no activation of the THP1-XBlue™ monocyte. Cytotoxicity tests performed with L929 mice fibroblasts showed that nanoparticles should be utilized at a concentration of 16 ppm. The minimum inhibitory concentrations determined with the microdilution method for nanoparticles prepared with plant infusion for S. aureus and S. epidermidis were 2 ppm and 16 ppm, respectively.
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In the present work, hydroxyapatite-polymer materials were developed. The preparation, as well as characterization of the ceramic-polymer composites based on polyvinylpyrrolidone, sodium alginate, and gelatin were described. The system was enriched with the addition of common sage extract (Salvia officinalis). The antioxidant potential of sage aqueous extract and total polyphenol content was determined. The antioxidant capacity and total phenolic content of extract were equal to 86.06 ± 0.49% and 16.21 ± 0.58 mg gallic acid equivalents per gram of dry weight, respectively. Incubation studies in selected biological liquids were carried out to determine the biomineralization capacity on the surface of the composites and to examine the kinetics of release of the active substances from within the material. As a result of the incubation, a gradual release of the extract over time from the polymer matrix was observed; moreover, the appearance of new apatite layers on the composite surface was recorded as early as after 14 days, which was also confirmed by energy-dispersive X-ray spectroscopy (EDS) microanalysis. The composites were analyzed with Fourier transform infrared spectroscopy (FTIR) spectroscopy, and the morphology was recorded by scanning electron microscope (SEM) imaging. The in vitro biological studies allowed their cytotoxic effect on the reference L929 fibroblasts to be excluded. Further analysis of the biomaterials showed that enrichment with polyphenols does not support the adhesion of L929 cells to the surface of the material. However, the addition of these natural components stimulates human monocytes that constitute the first step of tissue regeneration.
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This study involves the synthesis of hydroxyapatite and describes the preparation and characterization of polymer coatings based on poly(ethylene glycol) diacrylate and poly(ethylene glycol) and modified with bovine serum albumin and hydroxyapatite. Hydroxyapatite was obtained by wet chemical synthesis and characterized by X-ray diffraction and FTIR spectroscopy, and its Ca/P molar ratio was determined (1.69 ± 0.08). The ceramic and bovine serum albumin were used in the preparation of composite materials with the polymeric matrix. The chemical composition of coatings was characterized with FTIR spectroscopy, and their morphology was recorded with SEM imaging. Moreover, the measurements of surface roughness parameters and stereometric research were performed. The prepared coatings were subjected to in vitro studies in simulated body fluid and artificial saliva. Changes in chemical composition and morphology after immersion were examined with FTIR spectroscopy and SEM imaging. Based on the conducted research, it can be stated that applied modifiers promote the biomineralization process. The roughness analysis confirmed prepared materials were characterized by the micrometer-scale topography. The materials morphology and roughness, and the morphology of the newly formed apatite deposit, were dependent on the type of the used modifier, and the artificial fluid used in in vitro studies.
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The study was focused on the phytochemicals-mediated biosynthesis of silver nanoparticles using leaf extracts and infusions from Cynara scolymus. To identify the antioxidant activity and total phenolic content, the 1,1-diphenyl-1-picrylhydrazyl and Folin-Ciocalteau methods were applied, respectively. The formation and stability of the reduced silver ions were monitored by UV-vis spectrophotometer. The particle sizes of the silver nanoparticles were characterised using the dynamic light scattering technique and scanning electron microscope. The phase composition of the obtained silver nanoparticles was characterised by X-ray diffraction. The silver nanoparticles suspension, artichoke infusion, and silver ions were separately tested towards potential cytotoxicity and pro-inflammatory effect using mouse fibroblasts and human monocytes cell line, respectively. The total phenolic content and antioxidant activity of ethanol extract and infusion were found significantly higher as compared to aqueous extract and infusion. The UV-visible spectrophotometric analysis revealed the presence of the characteristic absorption band of the Ag nanoparticles. Moreover, it was found that with the increasing volume of plant extract, the average size of particles was increased. Biocompatibility results evidently showed that silver nanoparticles do not induce monocyte activation, however in order to avoid their cytotoxicity suspension at a concentration <2â ppm should be applied.