Search Results (20)

Background: Porphyromonas gingivalis is one of the most prevalent periodontal pathogens, involved in the development of periodontitis, deep caries, pulpitis, endodontic infections, and peri-implantitis. Antiseptics are commonly used in the treatment of oral diseases, but their effectiveness against P. gingivalis remains only partially understood. This preliminary study investigated antimicrobial and antibiofilm activity of eight pure antiseptics: boric acid (BA), chlorhexidine (CHX), ethacridine lactate (ET), hydrogen peroxide (H₂O₂), octenidine (OCT), polyhexanide (PHMB), potassium permanganate (KMnO₄), and sodium hypochlorite (NaOCl), as well as five commercial rinses containing these agents, against periopathogen P. gingivalis ATCC 33277. Methods: Minimal inhibitory concentrations (MICs) were determined using the broth microdilution method. The Clinical Efficiency of MIC (CEMIC) was subsequently calculated. Antibiofilm activity was evaluated using the crystal violet method, LIVE/DEAD fluorescence assay and by measuring biofilm thickness with digital microscopy in combination with the author’s Python-based application Biofilm Thickness Analyzer. Results: OCT, CHX, PHMB and ET showed the strongest activity against P. gingivalis, in both its planktonic and biofilm forms. H₂O₂ and BA had variable MIC efficacy and moderate antibiofilm activity. In contrast, NaOCl and KMnO₄ demonstrated the weakest activity or no significant effect against P. gingivalis. Conclusions: The results have a translational dimension, supporting the potential clinical relevance of the selected compounds. However, this study was conducted strictly in vitro on a single strain under monomicrobial biofilm conditions. Therefore, while the findings suggest that mouthwashes containing OCT, CHX, and PHMB may be effective against P. gingivalis, their actual clinical efficacy in the treatment and prevention of oral diseases remains to be confirmed in in vivo studies. Full article

Objective: This study aimed to systematically investigate the potential antibacterial mechanisms of ethacridine in the treatment of diabetic foot ulcers (DFUs) by integrating network pharmacology, molecular docking, and molecular dynamics simulation approaches. Methods: The potential targets of ethacridine were predicted using the SwissTargetPrediction and PharmMapper databases and subsequently converted to gene symbols via the UniProt database. DFU-related and antibacterial-related targets were retrieved from the GeneCards and OMIM databases. The overlapping targets among ethacridine, DFU, and antibacterial-related genes were identified as candidate therapeutic targets. A “drug–disease–target” network was constructed using Cytoscape, while protein–protein interaction (PPI) networks were built through the STRING database. GO and KEGG enrichment analyses were performed using R software. Molecular docking was conducted to evaluate the binding affinities between core compounds and hub targets. Furthermore, molecular dynamics (MD) simulation was applied to assess the binding stability of the top-ranked compound–target complex. Finally, RT-qPCR was conducted on wound edge tissue samples from DFU patients treated with ethacridine to experimentally validate the mRNA expression of predicted hub genes. Results: A total of 302 potential ethacridine-related targets, 4264 DFU-related targets, and 1942 antibacterial-related targets were identified. Intersection analysis revealed 105 common targets potentially involved in the antibacterial effects of ethacridine against DFU. PPI network analysis highlighted 10 hub targets, including AKT1, EGFR, SRC, HSP90AA1, and MMP9. GO enrichment indicated significant involvement in responses to reactive oxygen species, regulation of inflammatory responses, responses to lipopolysaccharide, and bacterial molecular patterns. KEGG pathway analysis identified 157 relevant pathways, including the lipid and atherosclerosis, TNF signaling, IL-17 signaling, and the AGE–RAGE signaling pathways in diabetic complications. Molecular docking demonstrated favorable binding affinities (all < −5.0 kcal/mol) between ethacridine and the hub targets, with the strongest binding observed between MMP9 and ethacridine (−9.8 kcal/mol). These docking results suggest possible interaction tendencies that may contribute indirectly to Ethacridine’s network-level regulatory effects, rather than direct binding to all targets in vivo. Molecular dynamics simulation further confirmed the stable interaction between MMP9 and ethacridine. RT-qPCR validation in clinical DFU tissue samples demonstrated expression trends of key genes consistent with in silico predictions. These results reflect transcriptional regulation consistent with pathway modulation predicted by the network analysis, rather than direct protein–ligand binding across all targets. Conclusion: Ethacridine may exert antibacterial effects against bacterial biofilms in DFU through multi-target and multi-pathway mechanisms. These findings highlight ethacridine’s translational potential as a safe, readily available, and mechanistically validated topical agent for the clinical management of biofilm-associated diabetic foot infections. Full article

(1) Background: Tannacomp^® is a drug consisting of tannin albuminate, a complex of tannic acid (TA) and ethacridine lactate (Eta) used for treating acute and traveler’s diarrhea. TA is thought to modulate gastrointestinal barrier function, but the underlying mechanisms and whether Eta has similar effects remains unclear. (2) Methods: to investigate the effects of TA and Eta on the intestinal barrier, stress responses were induced in murine intestinal organoids by lipopolysaccharide (LPS) exposure or withdrawal of growth factors from cell culture medium (GF_Red). Further, organoids were exposed to either TA (0.01 mg/mL) or Eta (0.002 mg/mL) and markers of inflammatory response and gut barrier function were assessed. (3) Results: TA and Eta reduced several inflammatory markers such as interleukin 6, interleukin 1β, tumor necrosis factor α, and myeloid differentiation primary response 88 in stressed organoids. In addition, TA and Eta attenuated LPS- and GF_Red-mediated gut barrier dysfunctions, with normalization of tight junction, adherent junction and mucin gene expression and reduction of Nod2- and matrix metalloproteinase 7-dependent activation of antimicrobial peptides. (4) Conclusions: our data show that TA and Eta modulate markers of inflammation and the intestinal barrier and suggest novel mechanisms of action of this drug that could broaden its treatment indications. Full article

A fast and simple biotech method is presented for the simultaneous isolation and purification of transferrin (Tf) and immunoglobulin G (IgG) from the same pool-sample of human serum, yielding >98% pure proteins. Serum sample preparation was achieved by precipitation with ethacridine lactate (rivanol). Protein purification was performed with AKTA Avant 150 FPLC, using a Resource Q column. Three different buffers at pH 6.2 (MES, phosphate, and Bis-Tris) were tested. Isolated and purified proteins retained their native 3D structure, as shown by spectrofluorimetric measurements. Tf functionality was preserved, as confirmed by the retention of both the iron binding capacity and its ability to interact with the transferrin receptor (immunofluorescent staining), as well as the immunogenicity of IgG, as shown by Western blot analysis with immunodetection. The formation of IgG aggregates was avoided. This biotech method is a rapid, simple, and time-saving alternative to other methods for the isolation of extremely pure IgG and Tf, while it is also the only method so far described for their simultaneous isolation. Full article

Background/Objectives: Mycobacterium abscessus (MAB) is a highly resilient pathogen that causes difficult-to-treat pulmonary infections, particularly in individuals with cystic fibrosis (CF) and other underlying conditions. Its ability to form robust biofilms within the CF lung environment is a major factor contributing to its resistance to antibiotics and evasion of the host immune response, making conventional treatments largely ineffective. These biofilms, encased in an extracellular matrix, enhance drug tolerance and facilitate metabolic adaptations in hypoxic conditions, driving the bacteria into a persistent, non-replicative state that further exacerbates antimicrobial resistance. Treatment options remain limited, with multidrug regimens showing low success rates, highlighting the urgent need for more effective therapeutic strategies. Methods: In this study, we employed artificial sputum media to simulate the CF lung environment and conducted high-throughput screening of 24,000 compounds from diverse chemical libraries to identify inhibitors of MAB biofilm formation, using the Crystal Violet (CV) assay. Results: The screen established 17 hits with ≥30% biofilm inhibitory activity in mycobacteria. Six of these compounds inhibited MAB biofilm formation by over 60%, disrupted established biofilms by ≥40%, and significantly impaired bacterial viability within the biofilms, as confirmed by reduced CFU counts. In conformational assays, select compounds showed potent inhibitory activity in biofilms formed by clinical isolates of both MAB and Mycobacterium avium subsp. hominissuis (MAH). Key compounds, including ethacridine, phenothiazine, and fluorene derivatives, demonstrated potent activity against pre- and post-biofilm conditions, enhanced antibiotic efficacy, and reduced intracellular bacterial loads in macrophages. Conclusions: This study results underscore the potential of these compounds to target biofilm-associated resistance mechanisms, making them valuable candidates for use as adjuncts to existing therapies. These findings also emphasize the need for further investigations, including the initiation of a medicinal chemistry campaign to leverage structure–activity relationship studies and optimize the biological activity of these underexplored class of compounds against nontuberculous mycobacterial (NTM) strains. Full article

Background/Objectives: Pseudomonas aeruginosa rapidly acquires antibiotic resistance and demonstrates increasing tolerance to antiseptics. This study evaluated the activity of eight antiseptics against P. aeruginosa, assessed its ability to develop adaptation to these antiseptics, and, for the first time, determined the Karpinski Adaptation Index (KAI) for this bacterium. Methods: The minimal inhibitory concentration (MIC), susceptibility to antibiotics, bactericidal time according to EN 1040:2005, adaptation potential, and KAI of P. aeruginosa strains were evaluated. Results: The most effective antiseptics against P. aeruginosa, based on MIC activity, were octenidine dihydrochloride (OCT; mean MIC 11.3 ± 4.5 µg/mL), polyhexamethylene biguanide (PHMB; MIC 22.6 ± 8.0 µg/mL), and chlorhexidine digluconate (CHX; MIC 26.6 ± 14.4 µg/mL). Sodium hypochlorite (NaOCl) and ethacridine lactate (ET) showed moderate activity, while boric acid (BA), povidone-iodine (PVI), and potassium permanganate (KMnO₄) exhibited the weakest MIC activity. MIC values for NaOCl (95 ± 15.4 µg/mL) and KMnO₄ (>10 mg/mL) were close to or exceeded the clinical concentrations used in commercial products. OCT, CHX, and PVI exhibited the fastest bactericidal effect within 1 min. Bactericidal times were up to 15 min for PHMB, up to 60 min for ET, and more than 60 min for BA, NaOCl, and KMnO₄. The lowest KAI values, indicating a low resistance risk, were observed for OCT (0.12), PHMB (0.19), and BA (0.19). Moderate resistance risk was noted for PVI (0.21), CHX (0.29), and ET (0.47). The highest KAI values, signifying a very high resistance risk, were found for NaOCl (1.0) and KMnO₄ (≥1.0). Conclusions: Antiseptics like OCT, CHX, and partially PVI can be critical in quick antibacterial action on infected wounds, while agents such as PHMB might be reserved for cases where prolonged contact times are possible. Given the rapid adaptation of P. aeruginosa to the clinical concentrations of NaOCl and KMnO₄ currently in use, reconsideration of their effectiveness in treating skin and mucous membrane infections is recommended. Full article

Background/Objectives: Adaptation can reduce or completely eliminate the effectiveness of antibiotics and antiseptics at clinical concentrations. To our knowledge, no studies have examined fungal adaptation to antiseptics. This study aimed to preliminarily investigate the potential for Candida albicans adaptation to eight antiseptics. Methods: The minimal inhibitory concentration (MIC), drug susceptibility, adaptation to antiseptics, and Karpinski Adaptation Index (KAI) of C. albicans strains were assessed. Results: The antiseptics with the most effective MICs activity against C. albicans were octenidine dihydrochloride (OCT), chlorhexidine digluconate (CHX), and polyhexamethylene biguanide (polyhexanide, PHMB). Sodium hypochlorite (NaOCl) and ethacridine lactate (ET) demonstrated moderate activity, while boric acid (BA), povidone–iodine (PVI), and potassium permanganate (KMnO₄) showed the weakest activity. The MIC values for NaOCl and KMnO₄ were close to or equal to the clinical concentrations used in commercial products. The studied strains were susceptible to econazole, miconazole, and voriconazole. Resistance to other drugs occurred in 10–30% of the strains. Antifungal resistance remained unchanged after antiseptic adaptation testing. The lowest KAI values, indicating very low resistance risk, were observed for CHX, OCT, and PHMB. PVI and BA presented a low risk, ET a moderate risk. KMnO₄ and NaOCl had the highest KAI values, indicating high and very high resistance risk in Candida yeasts. Conclusions: C. albicans strains can adapt to antiseptics to varying extents. For most antiseptics, adaptation does not significantly affect their clinical efficacy. However, due to adaptation, NaOCl and KMnO₄ may become ineffective against C. albicans strains even at clinical concentrations. Full article

Ecosystems are negatively impacted by pharmaceutical-contaminated water in different ways. In this work, a new biosorbent obtained by immobilizing Lactococcus lactis in a calcium alginate matrix was developed for the removal of pharmaceuticals from aqueous solutions. Ethacridine lactate (EL) was selected as the target drug. Lactococcus Lactis biomass was chosen for the biosorbent synthesis for two reasons: (i) the microbial biomass used in the food industry allows the development of a low-cost biosorbent from available and renewable materials, and (ii) there is no literature mentioning the use of Lactococcus Lactis biomass immobilized in natural polymers as a biosorbent for the removal of pharmaceuticals. The characterization of the synthesized biosorbent named 5% LLA was performed by scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) analysis. Additionally, particle size and the point of zero charge were established. Batch biosorption investigations showed that using 5% LLA at an initial pH of 3.0 and a biosorbent dose of 2 g/L resulted in up to 80% EL removal efficiency for all EL initial concentrations (20–60 mg/L). Four equilibrium isotherms, given in the order of Redlich–Peterson > Freundlich > Hill > Temkin, are particularly relevant for describing the experimental data for EL biosorption on the 5% LLA biosorbent using correlation coefficient values. Kinetic parameters were determined using kinetic models such as pseudo-first-order, pseudo-second-order, Elovich, Avrami and Weber–Morris. The pseudo-second-order kinetics model provides the greatest fit among the evaluated equations, with correlation coefficients greater than 0.99. According to the study’s findings, the developed biocomposite is a potentially useful material for the removal of pharmaceuticals from aqueous matrices. Full article

The emergence of drug-resistant bacterial strains that reduce the effectiveness of antimicrobial agents has become a major ongoing health concern in recent years. It is therefore necessary to find new antibacterials with broad-spectrum activity against both Gram-positive and Gram-negative bacteria, and/or to use nanotechnology to boost the potency of already available medications. In this research, we examined the antibacterial efficacy of sulfamethoxazole and ethacridine lactate loaded two-dimensional glucosamine functionalized graphene-based nanocarriers against a range of bacterial isolates. Graphene oxide was first functionalized with glucosamine, which as a carbohydrate moiety can render hydrophilic and biocompatible characters to the GO surface, and subsequently loaded with ethacridine lactate and sulfamethoxazole. The resulting nanoformulations had distinct, controllable physiochemical properties. By analyzing the formulation using Fourier Transform Infrared Spectroscopy (FTIR), X-ray diffraction (PXRD), a thermogravimetric analysis (TGA), zetasizer, and a morphological analysis using Scanning Electron Microscopy and Atomic Force Microscopy, researchers were able to confirm the synthesis of nanocarriers. Both nanoformulations were tested against Gram-negative bacteria, including Escherichia coli K1, Serratia marcescens, Pseudomonas aeruginosa, Salmonella enterica, as well as Gram-positive bacteria, including Bacillus cereus, Streptococcus pyogenes, and Streptococcus pneumoniae. Importantly, ethacridine lactate and its nanoformulations exhibited significant antibacterial properties against all bacteria tested in this study. When tested for minimum inhibitory concentration (MIC), the results were remarkable and revealed that ethacridine lactate presented MIC₉₀ at 9.7 µg/mL against S. enteric, and MIC₉₀ at 6.2 µg/mL against B. cereus. Notably, ethacridine lactate and its nanoformulations showed limited toxicity effects against human cells using lactate dehydrogenase assays. Overall, the results revealed that ethacridine lactate and its nanoformulations possess antibacterial activities against various Gram-negative and Gram-positive bacteria and that nanotechnology can be employed for the targeted delivery of effective drugs without harming the host tissue. Full article

Biosorbtive removal of the antibacterial drug, ethacridine lactate (EL), from aqueous solutions was investigated using as biosorbent Saccharomyces pastorianus residual biomass immobilized in calcium alginate. The aim of this work was to optimize the biosorption process and to evaluate the biosorption capacity in the batch system. Response surface methodology, based on a Box–Behnken design, was used to optimize the EL biosorption parameters. Two response functions (removal efficiency and biosorption capacity) were maximized dependent on three factors: initial concentration of EL solution, contact time, and agitation speed. The highest values for the studied functions (89.49%, 26.04 mg/g) were obtained in the following operational conditions: EL initial concentration: 59.73 mg/L; contact time: 94.26 min; agitation speed: 297.57 rpm. A number of nonlinear kinetic models, including pseudo-first-order, pseudo-second-order, Elovich, and Avrami, were utilized to validate the biosorption kinetic behavior of EL in the optimized conditions. The kinetic data fitted the pseudo-first-order and Avrami models. The experimental results demonstrated that the optimized parameters (especially the agitation speed) significantly affect biosorption and should be considered important in such studies. Full article

Two types of biosorbents, based on Saccharomyces pastorianus immobilized in calcium alginate, were studied for the removal of pharmaceuticals from aqueous solutions. Synthetized biocomposite materials were characterized chemically and morphologically, both before and after simulated biosorption. Ethacridine lactate (EL) was chosen as a target molecule. The process performance was interpreted as a function of initial solution pH, biosorbent dose, and initial pharmaceutical concentration. The results exhibited that the removal efficiencies were superior to 90% for both biosorbents, at the initial pH value of 4.0 and biosorbent dose of 2 g/L for all EL initial concentrations tested. Freundlich, Temkin, Hill, Redlich-Peterson, Sips, and Toth isotherms were used to describe the experimental results. The kinetic data were analyzed using kinetic models, such as pseudo-first order, pseudo-second order, Elovich, and Avrami, to determine the kinetic parameters and describe the transport mechanisms of EL from aqueous solution onto biosorbents. Among the tested equations, the best fit is ensured by the pseudo-second-order kinetics model for both biosorbents, with the correlation coefficient having values higher than 0.996. The many potential advantages and good biosorptive capacity of Saccharomyces pastorianus biomass immobilized in calcium alginate recommend these types of biocomposite materials for the removal of pharmaceuticals from aqueous solutions. Full article

In this study, ethacridine lactate removal from aqueous solution using a biosorbent material based on residual microbial biomass and natural polymers in fixed-bed continuous column was investigated. Composite beads of Saccharomyces pastorianus residual biomass and calcium alginate were obtained by immobilization technique. The prepared biosorbent was characterized by Fourier transformed infrared spectroscopy, scanning electron microscopy, and analysis of point of zero charge value. Then, laboratory-scale experiments by fixed-bed column biosorption were conducted in continuous system. To this purpose, the column bed high (5 cm; 7.5 cm), initial pollutant concentration (20 mg/L; 40 mg/L), and solution flow through the column (0.6 mL/min; 1.5 mL/min) were considered the main parameters. Recorded breakthrough curves suggest that lower flow rates, greater bed heights, and a lower concentration of ethacridine lactate led to an increased biosorption of the target compound. The biosorption dynamic was investigated by nonlinear regression analysis using the Adams–Bohart, Yoon–Nelson, Clark, and Yan mathematical models. Conclusively, our research highlights, firstly, that the obtained biosorbent material has the required properties for retaining the ethacridine lactate from aqueous solution in continuous system. Secondly, it emphasizes that the modeling approach reveals an acceptable fitting with the experimental data for the Yoon–Nelson, Clark, and Yan models. Full article

Multicomponent crystals containing diclofenac and acridine (1) and diclofenac and 6,9-diamino-2-ethoxyacridine (2) were synthesized and structurally characterized. The single-crystal XRD measurements showed that compound 1 crystallizes in the triclinic P-1 space group as a salt cocrystal with one acridinium cation, one diclofenac anion, and one diclofenac molecule in the asymmetric unit, whereas compound 2 crystallizes in the triclinic P-1 space group as an ethanol solvate monohydrate salt with one 6,9-diamino-2-ethoxyacridinium cation, one diclofenac anion, one ethanol molecule, and one water molecule in the asymmetric unit. In the crystals of the title compounds, diclofenac and acridines ions and solvent molecules interact via N–H⋯O, O–H⋯O, and C–H⋯O hydrogen bonds, as well as C–H⋯π and π–π interactions, and form heterotetramer bis[⋯cation⋯anion⋯] (1) or heterohexamer bis[⋯cation⋯ethanol⋯anion⋯] (2). Moreover, in the crystal of compound 1, acridine cations and diclofenac anions interact via N–H⋯O hydrogen bond, C–H⋯π and π–π interactions to produce blocks, while diclofenac molecules interact via C–Cl⋯π interactions to form columns. In the crystal of compound 2, the ethacridine cations interact via C–H⋯π and π–π interactions building blocks, while diclofenac anions interact via π–π interactions to form columns. Full article

Pharmaceuticals are recognized as emerging water microcontaminants that have been reported in several aquatic environments worldwide; therefore, the elimination of these pollutants is a global challenge. This study aimed to develop a biosorbent based on Saccharomyces pastorianus residual biomass encapsulated in a calcium alginate matrix and to evaluate its biosorption performance to remove Ethacridine Lactate (EL) from aqueous solutions. Firstly, the synthesis and characterization of biosorbent has been carried out. Then, the impact of main parameters on biosorption process were investigated by batch experiments. Finally, the kinetics behavior and equilibrium isotherms were evaluated. The resulted beads have an irregular and elongated shape with about 1.89 mm ± 0.13 mm in size with a homogeneous structure. The best removal efficiency for EL of over 85% was obtained at acidic pH 2 and 25 °C for 50 mg/L initial concentration and 2 g/L biosorbent dose. The pseudo-second-order and intraparticle diffusion kinetics describe the biosorption process. The maximum calculated biosorption capacity was 21.39 mg/g similar to that recorded experimentally. The equilibrium biosorption data were a good fit for Freundlich and Dubinin–Radushkevich isotherms. Our findings reveal that the low cost and eco-friendly obtained biosorbent can be easily synthesized and suitable to remove Ethacridine Lactate from water matrices. Full article

Issues arising in wound healing are very common, and chronic wound infections affect approximately 1.5% of the population. The main substances used in wound washing, cleansing and treatment are antiseptics. Today, there are many compounds with a known antiseptic activity. Older antiseptics (e.g., boric acid, ethacridine lactate, potassium permanganate, hydrogen peroxide, iodoform, iodine and dyes) are not recommended for wound treatment due to a number of disadvantages. According to the newest guidelines of the Polish Society for Wound Treatment and the German Consensus on Wound Antisepsis, only the following antiseptics should be taken into account for wound treatment: octenidine (OCT), polihexanide (PHMB), povidone-iodine (PVP-I), sodium hypochlorite (NaOCl) and nanosilver. This article provides an overview of the five antiseptics mentioned above, their chemical properties, wound applications, side effects and safety. Full article