Refine
Document Type
- Article (60)
Language
- English (60)
Has Fulltext
- yes (60)
Is part of the Bibliography
- no (60)
Keywords
- - (39)
- drug resistance (4)
- antibiotic resistance (3)
- antimicrobial resistance (3)
- drug release (3)
- salivary tracer technique (3)
- <i>E. coli</i> (2)
- ESBL (2)
- aerogel (2)
- anti-biofilm (2)
- anticancer drug (2)
- antimicrobial photodynamic therapy (2)
- apoptosis (2)
- biological activities (2)
- biorelevant in vitro model (2)
- bolaform amphiphilic lipids (2)
- bolalipids (2)
- broiler (2)
- caffeine (2)
- celecoxib (2)
- cell cycle (2)
- chorioallantoic membrane model (2)
- colonic microbiota (2)
- drug delivery system (2)
- dynamic colon model (2)
- efavirenz (2)
- fenofibrate (2)
- hot melt extrusion (2)
- hydrogel (2)
- in vitro metabolization (2)
- inhibition (2)
- molecular docking (2)
- nanoemulsion (2)
- self-assembly (2)
- structure activity (2)
- sulfasalazine (2)
- synthesis (2)
- virulence (2)
- -anethole (1)
- 1,2,3-benzotriazoles (1)
- 1,2,4-triazoles (1)
- 2,4-diamino-1,3,5-triazines (1)
- 2-imino-2<i>H</i>-chromen-3-yl-1,3,5-triazines (1)
- 2-imino-coumarins (1)
- 2<i>H</i>-chromen-3-yl-1,3,5-triazines (1)
- 3D printing (1)
- 3D-QSAR (1)
- 3D-printing (1)
- 5637 (1)
- <i>Enterobacteriaceae</i> (1)
- <i>Lannea barteri</i> (1)
- <i>N</i>-acylhydrazones (1)
- <i>N</i>-sulfonylhydrazones (1)
- A549 (1)
- ADMET analysis (1)
- AMR (1)
- Alzheimer’s disease (1)
- AmpC (1)
- BCL11B (1)
- Bacillus cereus (1)
- Bakterien (1)
- CCHC zinc finger (1)
- CTX-M-1 (1)
- Centaurothamnus maximus (1)
- DNA–DNA hybridization (ddH) (1)
- DUOCAP (1)
- Drosera intermedia (1)
- Drosera rotundifolia (1)
- E. coli (1)
- EGFR inhibitor (1)
- EGFR-mutated (1)
- EMP-hybrid (1)
- EMT (1)
- ESBL- (1)
- ESBL/AmpC- (1)
- Ethiopia (1)
- Extrakt (1)
- FDM (1)
- GC-MS (1)
- GPx1 knockout (1)
- GastroDuo (1)
- Gerbstoff (1)
- Germany (1)
- H. aspersa Müller (1)
- HPMC (1)
- HepG2 (1)
- IncI1 (1)
- KYSE 70 (1)
- L. (1)
- MDR (1)
- MRI (1)
- MRI study (1)
- MimiCol (1)
- MimiCol3 (1)
- NSCLC (1)
- One Health (1)
- PLK1 inhibitors (1)
- R. chamaemorus (1)
- SEA (1)
- SLA 3D-printing (1)
- SiSo (1)
- SuperPred (1)
- SwissTargetPrediction (1)
- TIGER2h (1)
- TIGER2hs (1)
- USP apparatus 4 (1)
- USP apparatus 7 (1)
- X-ray analysis (1)
- ZEB1 (1)
- acetylcholinesterase inhibitors (1)
- acute toxicity (1)
- additive manufacturing (1)
- adherent human carcinoma cell lines (1)
- adhesion (1)
- amides (1)
- amorphous formulations (1)
- amorphous solid dispersion (1)
- anaerobic metabolism (1)
- anti-cancer (1)
- antibacterial (1)
- anticancer drugs (1)
- antifungal (1)
- antioxidant (1)
- antioxidant activity (1)
- aspiration (1)
- autophagy (1)
- biocontrol (1)
- biofilm (1)
- biopharmaceutics (1)
- biosecurity (1)
- biosynthesis gene cluster (BGC) (1)
- bortezomib (1)
- calves (1)
- cancer (1)
- cancer stem cells (1)
- capsule-in-capsule (1)
- carbon–carbon lyase (1)
- cattle (1)
- cell proliferation regulating inhibitor of protein phosphatase 2A (1)
- chiral resolution (1)
- chiral stationary phase (1)
- clinical chemistry (1)
- clinical study (1)
- coated (1)
- commensal (1)
- compression-coated tablet (1)
- continuous manufacturing (1)
- control measure (1)
- copolymer (1)
- cormorants (1)
- coumarins (1)
- cytotoxicity (1)
- depression (1)
- dermatophytosis (1)
- diet (1)
- dihydrochalcones (1)
- dissolution (1)
- dissolution method (1)
- dissolution methods (1)
- drug delivery (1)
- drug-eluting (1)
- dynamic simulation (1)
- ease of swallowing (1)
- educast (1)
- educational podcast (1)
- eosinophilic esophagitis (1)
- epidermal growth factor receptor (1)
- esophageal diseases (1)
- esophageal transport (1)
- esophagus (1)
- esophagus therapy (1)
- essential oil (1)
- essentials elements (1)
- ethnobotany (1)
- ex vivo measurements (1)
- exopolysaccharides (1)
- extended-spectrum ß-lactamase-producing (1)
- extracellular vesicles (1)
- extractions (1)
- fasted and fed state conditions (1)
- fatty acid (1)
- films (1)
- flavonoids (1)
- flesh (1)
- food chain (1)
- food safety (1)
- formulation design (1)
- gastric emptying (1)
- glass transition (1)
- glutathione peroxidase-1 (1)
- high-resolution manometry (1)
- homodimerization (1)
- hotmelt extrusion (1)
- human intestinal mucosa (1)
- hybrid molecules (1)
- hydrazones (1)
- imaging tools (1)
- imidazo[2,1-<i>c</i>][1,2,4]triazol-3(5<i>H</i>)-imines (1)
- immobilized (1)
- implant (1)
- in silico target prediction (1)
- in vitro anticancer activity (1)
- in vitro antitumor activity (1)
- in vitro cytotoxic activity (1)
- in vitro dissolution (1)
- in vitro drug release (1)
- in vitro model (1)
- in vitro–ex vivo correlation (1)
- in vivo (1)
- in vivo disintegration (1)
- in vivo study (1)
- intervention measure (1)
- intervention measures (1)
- intestinal application (1)
- intravaginal ring (1)
- intravitreal implants (1)
- isoprenoid degradation (1)
- ketamine (1)
- kurstakin (1)
- leaf (1)
- lethal dose 50 (1)
- lipid mediators (1)
- local drug targeting (1)
- mTHPC (1)
- magnetic marker monitoring (1)
- magnetic resonance imaging (1)
- management measures (1)
- manufacturing science (1)
- materials science (1)
- medicinal herbs (1)
- medicinal plants (1)
- metabolites (1)
- miR-205-5p (1)
- miRNA (1)
- mini tablets (1)
- mobile learning (1)
- modeling (1)
- molecular weight (1)
- monocytes (1)
- monoterpene (1)
- mucoadhesion (1)
- mucoadhesive films (1)
- mucoadhesive polymer (1)
- nanoemulgel (1)
- naphthoquinones (1)
- necrosis (1)
- neutrophils (1)
- next-generation sequencing (1)
- non-small cell lung cancer (1)
- nutrients elements (1)
- one health (1)
- organic farming (1)
- oxidative stress (1)
- oxylipins (1)
- pediatrics (1)
- performance assessment (1)
- peristalsis (1)
- pharmacokinetics (1)
- pharmacy education (1)
- pharmacy students (1)
- photodynamic therapy (1)
- phylogenomics (1)
- physicochemical characterization (1)
- phytochemicals (1)
- pig (1)
- plant growth promotion (PGP) (1)
- platelets (1)
- podcast (1)
- polypharmacology (1)
- poorly soluble drug (1)
- poorly soluble drugs (1)
- porcine small intestine (1)
- poultry (1)
- propranolol HCl (1)
- protein folding (1)
- protein-protein docking (1)
- pulse oximetry (1)
- quercetin (1)
- quinolines (1)
- reactive oxygen species (1)
- regulatory gene (1)
- replica-exchange molecular dynamics (1)
- resistance (1)
- resistome (1)
- ring-opening reactions (1)
- rotating magnetic field (1)
- saliva flow (1)
- salivary tracer (1)
- scintigraphy (1)
- silver nanoparticles (1)
- site-specific application (1)
- site-specific drug delivery (1)
- slaughterhouse (1)
- spinning process (1)
- staphylococcal enterotoxin gene (1)
- staphylococcal enterotoxins (1)
- stem bark (1)
- structure (1)
- sub-ambient temperature (1)
- subcritical fluid chromatography (1)
- substituent (1)
- sulfonamides (1)
- supercritical CO<sub>2</sub> (1)
- supercritical fluid chromatography (1)
- tannins and flavonoids (1)
- tannins and flavonoids; anti-biofilm; E. coli; Epilobium; Filipendula; R. chamaemorus; biological activities; ethnobotany (1)
- telemetric capsules (1)
- tensile studies (1)
- terbinafine hydrochloride (1)
- texture analysis (1)
- thioureas (1)
- thumolycin (1)
- triamcinolone acetonide (1)
- ureas (1)
- urine test strips (1)
- user perspective (1)
- validation (1)
- virtual screening (1)
- vitreous substitute (1)
- wastewater (1)
- wild boar (1)
- wild ruminant (1)
- wildlife (1)
- (1)
Institute
- Institut für Pharmazie (60) (remove)
Publisher
- MDPI (60) (remove)
Eicosanoids are lipid mediators generated from arachidonic acid with pro- and anti-inflammatory properties. Despite these lipid mediators being known for decades, quantitative determination in biological samples is still challenging due to low abundance, instability, the existence of regio- and stereoisomers, and a wide polarity range that hampers chromatographic separation. In this study, we developed a supercritical fluid chromatography mass spectrometry (SFC-MS) platform for the quantification of relevant eicosanoids. Application of a chiral amylose-based column and modifier combination of 2-propanol/acetonitrile offered separation and sufficient resolution of 11 eicosanoids (5-, 12-, 15-HETE, PGB1, LTB4, t-LTB4, 20-OH-LTB4, PGE2, PGD2, PGF2α, TxB2) with baseline separation of isobaric analytes within 12 min. The method was validated in terms of range (78–2500 ng/mL), linearity, accuracy, precision, and recovery according to EMA guidelines. Finally, we confirmed the method’s applicability by quantifying eicosanoid levels in human primary blood cells. In conclusion, we present a validated SFC-MS method for the determination of relevant eicosanoids in biological samples with a wide range of polarity while maintaining baseline separation of isobars, which allows coupling to a single quadrupole mass detector.
Seventeen bacterial strains able to suppress plant pathogens have been isolated from healthy Vietnamese crop plants and taxonomically assigned as members of the Bacillus cereus group. In order to prove their potential as biocontrol agents, we perform a comprehensive analysis that included the whole-genome sequencing of selected strains and the mining for genes and gene clusters involved in the synthesis of endo- and exotoxins and secondary metabolites, such as antimicrobial peptides (AMPs). Kurstakin, thumolycin, and other AMPs were detected and characterized by different mass spectrometric methods, such as MALDI-TOF-MS and LIFT-MALDI-TOF/TOF fragment analysis. Based on their whole-genome sequences, the plant-associated isolates were assigned to the following species and subspecies: B. cereus subsp. cereus (6), B. cereus subsp. bombysepticus (5), Bacillus tropicus (2), and Bacillus pacificus. These three isolates represent novel genomospecies. Genes encoding entomopathogenic crystal and vegetative proteins were detected in B. cereus subsp. bombysepticus TK1. The in vitro assays revealed that many plant-associated isolates enhanced plant growth and suppressed plant pathogens. Our findings indicate that the plant-associated representatives of the B. cereus group are a rich source of putative antimicrobial compounds with potential in sustainable agriculture. However, the presence of virulence genes might restrict their application as biologicals in agriculture.
Overexpression of polo-like kinase 1 (PLK1) has been found in many different types of cancers. With its essential role in cell proliferation, PLK1 has been determined to be a broad-spectrum anti-cancer target. In this study, 3D-QSAR, molecular docking, and molecular dynamics (MD) simulations were applied on a series of novel pteridinone derivatives as PLK1 inhibitors to discover anti-cancer drug candidates. In this work, three models—CoMFA (Q² = 0.67, R² = 0.992), CoMSIA/SHE (Q² = 0.69, R² = 0.974), and CoMSIA/SEAH (Q² = 0.66, R² = 0.975)—of pteridinone derivatives were established. The three models that were established gave R²(pred) = 0.683, R²(pred) = 0.758, and R²(pred) = 0.767, respectively. Thus, the predictive abilities of the three proposed models were successfully evaluated. The relations between the different champs and activities were well-demonstrated by the contour chart of the CoMFA and CoMSIA/SEAH models. The results of molecular docking indicated that residues R136, R57, Y133, L69, L82, and Y139 were the active sites of the PLK1 protein (PDB code: 2RKU), in which the more active ligands can inhibit the enzyme of PLK1. The results of the molecular dynamic MD simulation diagram were obtained to reinforce the previous molecular docking results, which showed that both inhibitors remained stable in the active sites of the PLK1 protein (PDB code: 2RKU) for 50 ns. Finally, a check of the ADME-Tox properties of the two most active molecules showed that molecular N° 28 could represent a good drug candidate for the therapy of prostate cancer diseases.
The absorption of drugs with narrow absorption windows in the upper small intestine can be improved with a mucoadhesive drug delivery system such as enteric films. To predict the mucoadhesive behaviour in vivo, suitable in vitro or ex vivo methods can be performed. In this study, the influence of tissue storage and sampling site on the mucoadhesion of polyvinyl alcohol film to human small intestinal mucosa was investigated. Tissue from twelve human subjects was used to determine adhesion using a tensile strength method. Thawing of tissue frozen at −20 °C resulted in a significantly higher work of adhesion (p = 0.0005) when a low contact force was applied for one minute, whereas the maximum detachment force was not affected. When the contact force and time were increased, no differences were found for thawed tissue compared to fresh tissue. No change in adhesion was observed depending on the sampling location. Initial results from a comparison of adhesion to porcine and human mucosa suggest that the tissues are equivalent.
Humans consume snail flesh as part of their diet. To assess its nutritional value and toxicity, chemical analyses were conducted to confirm the presence of protein, total and reduced carbohydrates, fat, fatty acid composition and mineral components. Furthermore, an acute toxicity study was carried out to determine the safety of Helix aspersa Müller snail flesh. H. aspersa Müller snail flesh exhibits a high nutritional content, a good ω3/ω6 ratio and higher levels of unsaturated fatty acids. Various minerals have been found in the flesh of H. aspersa Müller. Around 76.91 kcal, or 3.84% of the energy of a daily meal of 2000 kcal, are present in 100 g of this flesh. The evaluation of the antioxidant capacity indicated that the flesh’s extracts contained a large quantity of antioxidant biomolecules. Administration of the aqueous extract of H. aspersa Müller flesh didn’t cause death in laboratory rats, indicating that the lethal dose 50 is greater than 2000 mg·kg−1 body weight. The consumption of the flesh of H. aspersa Müller is highly recommended for human consumption due to its high concentration of nutrients and essential elements, as well as unsaturated fats, and due to its safety.
The microbiome of the colon is characterized by its great diversity. This varies not only intra- but also interindividually and is influenced by endogenous and exogenous factors, such as dietary and lifestyle factors. The aim of this work was to investigate the extent to which the degradation of the drug sulfasalazine is influenced by different microbiota. Therefore, the in vitro model MimiCol3 was used, which represents the physiological conditions of the ascending colon. In addition to a representative physiological volume, the pH value, redox potential and an anaerobic atmosphere are important to provide the bacteria with the best possible growth conditions. Stool samples were taken from three healthy subjects, comparing omnivorous, vegetarian and meat-rich diets, and cultured for 24 h. However, the nutrient medium used for cultivation led to the alignment of the bacterial composition of the microbiota. The previously observed differences between the diets could not be maintained. Nevertheless, the similar degradation of sulfasalazine was observed in all microbiota studied in MimiCol3. This makes MimiCol3 a suitable in vitro model for metabolism studies in the gut microbiome.
Development of Test Programs for the Biorelevant Characterization of Esophageal-Applied Dosage Forms
(2023)
In the local treatment of the esophageal mucosa, the retention time of the different dosage forms, such as tablets, films or liquids, is of high relevance for the effective treatment of diseases. Unfortunately, there are only few in vitro models describing the esophageal route of administration. To predict the behaviour of an esophageal-applied dosage form, it is necessary to simulate the site of application in a biorelevant way. The aim of this work was to develop two test setups for an esophageal peristalsis model which was described in a previous study. Different parameters such as flow rate, peristalsis, angle of inclination or mucous membrane were varied or introduced into the model. A stimulated and unstimulated modus were developed and tested with two different dosage forms. The time until the dosage form was cleared from the in vitro model was shorter with the stimulated than with the unstimulated modus. Also, esophageal-applied films had a prolonged transit time compared to a viscous syrup. The modification of the simulated esophageal surface made it possible to estimate the retention time of the dosage forms. It could be demonstrated that the residence time of a dosage form depends on different parameters affecting each other.
Despite recent advances in the treatment of non-small cell lung cancer (NSCLC), acquired drug resistance to targeted therapy remains a major obstacle. Epithelial-mesenchymal transition (EMT) has been identified as a key resistance mechanism in NSCLC. Here, we investigated the mechanistic role of key EMT-regulating small non-coding microRNAs (miRNAs) in sublines of the NSCLC cell line HCC4006 adapted to afatinib, erlotinib, gefitinib, or osimertinib. The most differentially expressed miRNAs derived from extracellular vesicles were associated with EMT, and their predicted target ZEB1 was significantly overexpressed in all resistant cell lines. Transfection of a miR-205-5p mimic partially reversed EMT by inhibiting ZEB1, restoring CDH1 expression, and inhibiting migration in erlotinib-resistant cells. Gene expression of EMT-markers, transcription factors, and miRNAs were correlated during stepwise osimertinib adaptation of HCC4006 cells. Temporally relieving cells of osimertinib reversed transition trends, suggesting that the implementation of treatment pauses could provide prolonged benefits for patients. Our results provide new insights into the contribution of miRNAs to drug-resistant NSCLC harboring EGFR-activating mutations and highlight their role as potential biomarkers and therapeutic targets.
Background and Objectives: Alzheimer’s disease (AD) stands as a pervasive neurodegenerative ailment of global concern, necessitating a relentless pursuit of remedies. This study aims to furnish a comprehensive exposition, delving into the intricate mechanistic actions of medicinal herbs and phytochemicals. Furthermore, we assess the potential of these compounds in inhibiting human acetylcholinesterase through molecular docking, presenting encouraging avenues for AD therapeutics. Materials and Methods: Our approach entailed a systematic exploration of phytochemicals like curcumin, gedunin, quercetin, resveratrol, nobiletin, fisetin, and berberine, targeting their capability as human acetylcholinesterase (AChE) inhibitors, leveraging the PubChem database. Diverse bioinformatics techniques were harnessed to scrutinize molecular docking, ADMET (absorption, distribution, metabolism, excretion, and toxicity), and adherence to Lipinski’s rule of five. Results: Results notably underscored the substantial binding affinities of all ligands with specific amino acid residues within AChE. Remarkably, gedunin exhibited a superior binding affinity (−8.7 kcal/mol) compared to the reference standard. Conclusions: These outcomes accentuate the potential of these seven compounds as viable candidates for oral medication in AD treatment. Notably, both resveratrol and berberine demonstrated the capacity to traverse the blood-brain barrier (BBB), signaling their aptitude for central nervous system targeting. Consequently, these seven molecules are considered orally druggable, potentially surpassing the efficacy of the conventional drug, donepezil, in managing neurodegenerative disorders.
Synthesis of Quercetin-Loaded Silver Nanoparticles and Assessing Their Anti-Bacterial Potential
(2023)
The study delves into the multifaceted potential of quercetin (Qu), a phytoconstituent found in various fruits, vegetables, and medicinal plants, in combination with silver nanoparticles (AgNPs). The research explores the synthesis and characterization of AgNPs loaded with Qu and investigates their pharmaceutical applications, particularly focusing on antibacterial properties. The study meticulously evaluates Qu’s identity, and physicochemical properties, reaffirming its suitability for pharmaceutical use. The development of Qu-loaded AgNPs demonstrates their high drug entrapment efficiency, ideal particle characteristics, and controlled drug release kinetics, suggesting enhanced therapeutic efficacy and reduced side effects. Furthermore, the research examines the antibacterial activity of Qu in different solvents, revealing distinct outcomes. Qu, both in methanol and water formulations, exhibits antibacterial activity against Escherichia coli, with the methanol formulation displaying a slightly stronger efficacy. In conclusion, this study successfully synthesizes AgNPs loaded with Qu and highlights their potential as a potent antibacterial formulation. The findings underscore the influence of solvent choice on Qu’s antibacterial properties and pave the way for further research and development in drug delivery systems and antimicrobial agents. This innovative approach holds promise for addressing microbial resistance and advancing pharmaceutical formulations for improved therapeutic outcomes.