Search Results (1,412)

Background: Salivary pH plays a critical role in oral health by influencing enamel demineralization, buffering capacity, and the ecology of oral microbiota. Essential oils such as Origanum vulgare (oregano) possess well-documented antimicrobial properties that may reduce acidogenic bacterial activity. However, the effects of edible delivery systems like jellies on salivary pH modulation and their potential interactions with hormonal states remain poorly understood. Methods: This study evaluated the in vitro antimicrobial activity of an oregano-oil-based jelly formulation against standard bacterial (Staphylococcus aureus, Streptococcus pyogenes, and Escherichia coli) and fungal (Candida albicans) strains using the Kirby–Bauer disc diffusion method. Additionally, a human trial (n = 91) measured salivary pH before and after administration of the oregano-oil jelly. Participants were characterized by age, smoking status, menopausal status, and presence of menstruation. Multiple linear regression was used to identify predictors of final salivary pH. Results: The oregano-oil jelly demonstrated strong in vitro antimicrobial activity, with inhibition zones up to 8 mm for E. coli and C. albicans. In vivo, mean unstimulated salivary pH increased from 6.94 to 7.07 overall, indicating a mild alkalinizing effect. However, menstruating participants showed a significant decrease in final pH (from 7.03 to 6.78). Multiple regression identified menstruation as a significant negative predictor (β = −0.377, p < 0.001) and initial pH as a positive predictor (β = +0.275, p = 0.002). Menopausal status was not a significant predictor, likely due to the small sample size. Conclusions: Oregano-oil jellies may represent a promising natural approach to support oral health by increasing salivary pH and providing strong antimicrobial activity. However, physiological states such as menstruation can significantly modulate this response, underscoring the importance of personalized or phase-aware oral care strategies. Further studies with larger, diverse cohorts and controlled hormonal assessments are needed to validate these findings and optimize product formulations. Full article

Background: Cerebral aneurysm (CA) is a focal or diffuse pathological dilation of the cerebral arterial wall that arises due to various etiological factors. It represents a serious vascular condition, particularly affecting the elderly, and carries a high risk of rupture and neurological morbidity. Clonidine (CL), an α2-adrenergic receptor agonist, has been reported to suppress aneurysm progression; however, its underlying molecular mechanisms, especially in relation to cerebral endothelial dysfunction, remain unclear. This study aimed to investigate the potential of CL to mitigate CA development by modulating apoptosis, inflammation, and oxidative stress in an Angiotensin II (Ang II)-induced endothelial injury model. Methods: Human brain microvascular endothelial cells (HBMECs) were used to establish an in vitro model of endothelial dysfunction by treating cells with 1 µM Ang II for 48 h. CL was administered 2 h prior to Ang II exposure at concentrations of 0.1, 1, and 10 µM. Cell viability was assessed using the MTT assay. Oxidative stress markers, including reactive oxygen species (ROS) and Nitric Oxide (NO), were measured using 2′,7′–dichlorofluorescin diacetate (DCFDA). Gene expression levels of vascular endothelial growth factor (VEGF), matrix metalloproteinases (MMP-2 and MMP-9), high mobility group box 1 (HMGB1), and nuclear factor kappa B (NF-κB) were quantified using RT-qPCR. Levels of proinflammatory cytokines; tumor necrosis factor-alpha (TNF-α), Interleukin-6 (IL-6), and interferon-gamma (IFN-γ); were measured using commercial ELISA kits. Results: Ang II significantly increased ROS production and reduced NO levels, accompanied by heightened proinflammatory cytokine release and endothelial dysfunction. MTT assay revealed a marked decrease in cell viability following Ang II treatment (34.18%), whereas CL preserved cell viability in a concentration-dependent manner: 44.24% at 0.1 µM, 66.56% at 1 µM, and 81.74% at 10 µM. CL treatment also significantly attenuated ROS generation and inflammatory cytokine levels (p < 0.05). Furthermore, the expression of VEGF, HMGB1, NF-κB, MMP-2, and MMP-9 was significantly downregulated in response to CL. Conclusions: CL exerts a protective effect on endothelial cells by reducing oxidative stress and suppressing proinflammatory signaling pathways in Ang II-induced injury. These results support the potential of CL to mitigate endothelial injury in vitro, though further in vivo studies are required to confirm its translational relevance. Full article

Background: Singlet oxygen (¹O₂) generation in biological samples remains a significant challenge. Studying the mechanism of ¹O₂ action during photodynamic therapy (PDT) in atherosclerotic plaques in vitro represents an innovative cardiological approach. Atherosclerosis, a chronic and progressive disease, is characterized by plaque buildup inside arterial walls. Objectives: This study focused on the use of spin–lattice (T₁) and spin–spin (T₂) relaxation times measured by Magnetic Resonance Imaging (MRI) before and after the administration of indocyanine green-mediated PDT (ICG-PDT). Methods: To enhance visualization of morphological changes in atherosclerotic plaques, the clinically approved MRI contrast agent Gadovist was utilized. A total of 12 atherosclerotic plaque samples were collected from six patients undergoing endarterectomy. The generation of ¹O₂ in these plaques was assessed using quantitative MRI measurements and microscopic imaging, which visualized structural changes induced by PDT. Results: This research explores the potential of T₁ and T₂ relaxation times as indicators of PDT efficacy, while Gadovist helped provide evidence of ¹O₂ diffusion within the samples. Conclusions: Considering advancements in modern treatment, PDT may offer a novel approach for targeting atherosclerosis. Full article

Background: People with cystic fibrosis (pwCF) frequently suffer from chronic lung infections, with Pseudomonas aeruginosa being the predominant pathogen contributing to disease progression and morbidity. The increasing prevalence of multi-drug-resistant (MDR) P. aeruginosa has diminished treatment options. Antimicrobial peptides (AMPs) have emerged as promising alternatives to conventional antibiotics due to their unique membrane-targeting mechanisms. OMN51, a novel bioengineered AMP derived from capitellacin, was evaluated for antimicrobial activity against P. aeruginosa in sputum samples from pwCF. This study aimed to compare the bactericidal effects of OMN51 with those of a range of conventional antibiotics known to have activity against P. aeruginosa clinical isolates derived from pwCF. Methods:P. aeruginosa clinical isolates were obtained from fifty-six unique sputum cultures of pwCF at a tertiary-university-affiliated hospital. Minimum inhibitory concentrations (MICs) of OMN51 and comparator antibiotics were determined using broth microdilution. Antimicrobial susceptibility was evaluated using the Kirby–Bauer disc diffusion method. Results: OMN51 demonstrated in vitro bactericidal activity across all P. aeruginosa isolates, including MDR strains. MIC values for OMN51 ranged from 4 to 16 µg/mL, with no observed resistance or cross-resistance. Comparative analysis revealed the superior efficacy of OMN51 compared with conventional antibiotics. Conclusions: OMN51 exhibits robust in vitro activity against MDR P. aeruginosa, supporting its candidacy as a therapeutic agent for MDR P. aeruginosa- associated infections. Further studies are warranted to assess pharmacokinetics and in vivo safety and efficacy. OMN51 represents a first-in-class, membrane-targeting therapeutic showing promise against MDR P. aeruginosa. Full article

Titanium (Ti) alloys, renowned for their exceptional physicochemical properties and high biocompatibility, are widely utilized in orthopedic and dental implants; however, their lack of intrinsic antimicrobial activity significantly increases the risk of implant-associated infections, often leading to severe complications and implant failure. Developing antimicrobial coatings on Ti implants is therefore a promising strategy. In this study, tannic acid (TA) coatings were deposited by immersing Ti alloy surfaces—beforehand activated by low-temperature oxygen plasma—in TA solutions at 2, 5, and 8 wt%. Coatings were characterized by scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), water contact angle (WCA) measurements, and Folin–Ciocalteu release assays, and their cytocompatibility and antimicrobial performance were assessed in vitro. Surface characterization confirmed the formation of uniform TA layers, and WCA measurements indicated enhanced hydrophilicity relative to unmodified Ti (82.0° ± 3.6°), with values decreasing as TA concentration increased (from 35.2° ± 3.2° for 2% TA to 26.6° ± 2.8° for 8% TA). TA release profiles exhibited an initial burst followed by sustained diffusion, with 5% and 8% coatings releasing significantly more TA than 2% coatings. Coatings containing ≥ 5% TA demonstrated bactericidal activity—achieving > 2-log₁₀ reductions—against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa, and also showed inhibitory effects against Candida albicans. Importantly, all coatings remained cytocompatible with NIH/3T3 fibroblasts, and the released tannic acid hydrolysis products (particularly gallic acid) enhanced their proliferation. These findings indicate that plasma-activated titanium surfaces coated with ≥5 wt% tannic acid impart broad-spectrum antimicrobial efficacy and hold potential to reduce implant-associated infections and improve long-term outcomes in orthopedic and dental applications. Full article

Objectives: The global rise in multidrug resistance underscores the urgent need for the development of novel and effective antimicrobial agents. Semi-organic iodine-containing complexes, owing to their unique properties, low likelihood of resistance development, and stability under various conditions, represent a promising avenue for the design of new therapeutic strategies. This study describes the synthesis of semi-organic iodine-containing complexes and the in vitro evaluation of their impact on antibiotic susceptibility modulation in the multidrug-resistant pathogenic microorganisms S. aureus and E. coli. Methods: The physicochemical properties of the semiorganic compounds were characterized using UV-Vis spectroscopy, potentiometric, and titrimetric methods. Evaluation of antimicrobial activity was obtained according to CLSI protocols. The impact of semiorganic compounds on the in vitro susceptibility of MDR strains was evaluated by the disk diffusion method. Results: This study evaluated the effects of iodine-containing complexes KC-270 and KC-271 on the antibiotic susceptibility of Staphylococcus aureus BAA-39 and Escherichia coli BAA-196. The most pronounced effect was observed with KC-270 applied during the lag phase, which enhanced the activity of several antibiotics and, in some cases, restored susceptibility. KC-271 exhibited a weaker and more limited impact. The findings suggest that KC-270 has potential as a modulator of antibiotic susceptibility, particularly when administered at early stages of bacterial growth. Conclusions: The results support the ability of amino acid-based iodine coordination compounds to influence the antibiotic susceptibility of pathogenic bacteria, highlighting their potential as adjuvant agents to improve the effectiveness of current antimicrobial therapies. However, although changes in susceptibility were detected, neither compound fully eliminated resistance in the multidrug-resistant strains, indicating the necessity for further research into their mechanisms of action and possible synergistic interactions with antibiotics. Full article

Transdermal drug delivery (TDD) is an increasingly important non-invasive method for administering active pharmaceutical ingredients (APIs) through the skin barrier, offering advantages such as improved therapeutic efficacy and reduced systemic side effects. As demand increases for patient-friendly and minimally invasive treatment options, TDD has attracted substantial attention in research and clinical practice. This review summarizes recent advances enhancing skin permeability through chemical enhancers (e.g., ethanol, fatty acids, terpenes), physical (e.g., iontophoresis, microneedles, sonophoresis), and nanotechnological methods (e.g., liposomes, ethosomes, solid lipid nanoparticles, and transferosomes). A comprehensive literature analysis, including scientific publications, regulatory guidelines, and patents, was conducted to identify innovative methods and materials used to overcome the barrier properties of the stratum corneum. Special emphasis was placed on in vitro, ex vivo, and in vivo evaluation techniques for such as Franz diffusion cells for assessing drug permeation and skin interactions. The findings highlight the importance of active physical methods, passive nanostructured systems, and chemical penetration enhancers. In conclusion, integrating multiple analytical techniques is essential for the rational design and optimization of effective transdermal drug delivery systems. Full article

Infections caused by oxacillin-resistant Staphylococcus pseudintermedius are increasingly common in veterinary medicine. The indiscriminate use of antibiotics by pet owners worsens this problem, reducing treatment efficacy and creating the need for alternative therapies. This study aimed to evaluate the inhibitory effect of clove essential oil (Syzygium aromaticum) on both oxacillin-resistant and susceptible S. pseudintermedius. Thirty-five isolates from dogs with otitis externa were analyzed. The bacteria were identified by phenotypic tests and tested for susceptibility to 22 antibiotics using disk diffusion. Resistance genes (mecA and blaZ) were detected using conventional PCR. Among the isolates, 34.28% (12/35) were positive for mecA, and 97.14% (34/35) for blaZ. The essential oil’s efficacy was assessed using broth microdilution to determine its minimum inhibitory concentration (MIC). Clove oil showed an average MIC and minimum bactericidal concentration (MBC) of 6.4 mg/mL, inhibiting both resistant and susceptible isolates. In conclusion, clove essential oil demonstrated in vitro antimicrobial activity against S. pseudintermedius. Full article

In the present study, novel conjugated lignin/chitosan nanoparticles (LCNPs) were synthesized by a first-time simple green methodology using interfacial co-assembly between both biopolymers. The physicochemical (ζ-potential, size, concentration of surface acidic/basic groups), structural (surface functional groups), and morphological characteristics of the blank and quercetin-encapsulated (Q-LCNPs) nanoparticles were analyzed by the Boehm method, Fourier-transform infrared spectroscopy (FTIR), transmission electron microscopy (TEM), and X-ray diffraction (XRD). The experimentally determined encapsulation capacity was satisfactory—95.75%. The in vitro quercetin release efficiency in acidic solution that simulated the gastric microenvironment was 21.9%, followed by 68.5% and 99.8% cumulative release efficiency in simulated intestinal media at pH 7.4 and 6.8, respectively. The satisfactory applicability of the Weibull and sigmoidal mathematical models towards the experimental in vitro release data was indicative of the remarkable roles of diffusion and relaxation mechanisms. Full article

Background/Objectives: Combination therapies using traditional Chinese medicine and Western drugs have gained attention for their enhanced therapeutic effects and reduced side effects. Toujie Quwen Granules (TQG), known for its antiviral properties, particularly against respiratory viruses, could offer new treatment strategies when combined with antiviral drugs like arbidol, especially for diseases such as Coronavirus disease. This study investigates the synergistic mechanisms between arbidol and components from TQG against the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) main protease (M^pro). Methods: We identified compounds from TQG via existing data. Multi-ligand molecular docking, pharmacokinetic/toxicity screening, and preliminary simulations were performed to assess potential synergistic compounds with arbidol. UPLC-Q-Exactive Orbitrap-MS verified the presence of these compounds. Extended simulations and in vitro assays, including Luciferase and surface plasmon resonance, validated the findings. Results: Five compounds interacted with arbidol in synergy based on docking and preliminary dynamics simulation results. Only Baicalein (HQA004) could be identified in the herbal remedy by untargeted metabolomics, with ideal pharmacokinetic properties, and as a non-toxic compound. Extended simulations revealed that HQA004 enhanced arbidol’s antiviral activity via a “Far” Addition Mechanism #2, with an optimal 2:1 arbidol:HQA004 ratio. The movements of arbidol (diffusion and intramolecular conformational shifts) in the system were significantly reduced by HQA004, which may be the main reason for the synergism that occurred. In vitro experiments confirmed an increased inhibition of M^pro by the combination. Conclusions: HQA004 demonstrated synergistic potential with arbidol in inhibiting M^pro. The development of combination therapies integrating Western and herbal medicine is supported by these findings for effective antiviral treatments. Full article

Background/Objectives: Candidiasis, primarily caused by Candida albicans, and sporotrichosis, mainly caused by Sporothrix schenckii, are skin fungal infections that pose serious threats to global health. The Candida auris is a great concern in immunocompromised individuals, and while Sporothrix brasiliensis cause sporotrichosis, an infection commonly found in cats, this disease can be transmitted to humans through scratches or bites. Existing treatments for these fungal infections often cause problems related to resistance and significant side effects. Consequently, development of alternative therapeutic approaches such as nanotechnology-based topical lipid-based formulations is interesting. Thus, the objectives of this study were to prepare clove oil (CO)-in-water nanoemulsions (NEs) containing amphotericin B (AmB) and characterize them with respect to stability, release profile, and in vitro cytotoxic activity against Candida and Sporothrix strains. As a future alternative for the treatment of fungal skin diseases. Methods: Chemical analysis of clove oil was obtained by GC-MS. The NEs were produced using an ultrasound (sonicator) method with varying proportions of CO, Pluronic^® F-127, and AmB. The NEs were characterized by droplet size, morphology, stability and in vitro release profile. The antifungal and cytotoxic activity against C. albicans, C. auris, S. schenckii, and S. brasiliensis were ascertained employing agar diffusion and colorimetric MTT assay methods. A checkerboard assay was carried out using clove oil and amphotericin B against C. auris. Results: Eugenol was the major compound identified in CO at a concentration of 80.09%. AmB-loaded NEs exhibited particle sizes smaller than 50 nm and a polydispersity index below 0.25. The optimal Ne (NEMLB-05) remained stable after 150 days of storage at 4 °C. It exhibited rapid release within the first 24 h, followed by a slow and controlled release up to 96 h. NEMLB-05 more effectively inhibited C. auris compared to free AmB and also demonstrated greater activity against C. albicans, S. schenckii, and S. brasiliensis. Clove oil and amphotericin B presented synergism inhibiting the growth of C. auris. Conclusions: The selected CO-in-water NEs containing AmB demonstrated promising potential as a topical therapeutic alternative for treating fungal infections. Full article

This study focuses on the search for new effective synthetic antimicrobial compounds as a tool against the widespread presence of microorganisms resistant to existing drugs. Five derivatives of [1,3]thiazolo[3,2-b][1,2,4]triazoles were synthesized using an accessible protocol based on electrophilic heterocyclization and were characterized using infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopies, and their in vitro antimicrobial and antifungal activities were evaluated using the agar plate diffusion method and the microdilution plate procedure. Both antibacterial (Gram-positive and Gram-negative) and antifungal activities were found for the examined samples. The minimum inhibitory concentration (MIC) varied from 0.97 to 250 µg/mL, and the minimum bactericidal concentration (MBC) from 1.95 to 500 µg/mL. Compound 2a showed good antifungal action against Candida albicans and Saccharomyces cerevisiae with minimum fungicidal concentration (MFC) 125 and MIC 31.25 µg/mL. The molecular docking revealed that the 2-heptyl-3-phenyl-6,6-trimethyl-5,6-dihydro-3H-[1,3]thiazolo[3,2-b][1,2,4]triazol-7-ium cation stands out as a highly promising candidate for further investigation due to a wide range of interactions, including conventional hydrogen bonds, π–σ, π–π T-shaped, and hydrophobic alkyl interactions. The synthesis and preliminary evaluation of [1,3]thiazolo[3,2-b][1,2,4]triazoles yielded promising antimicrobial and antifungal candidates. The diverse interaction profile of the 2-heptyl derivative salt allows this compound’s selection for further biological studies. Full article

Due to the growth in the application of antibacterial nanomaterials (NMs), there is an increased potential for ingestion by humans. Evidence shows that NMs can induce dysbiosis in the gut microbiota in vivo. However, in vitro investigation of the antibacterial activity of NMs on gut-relevant, commensal bacteria has been neglected, with studies predominantly assessing NM toxicity against pathogenic bacteria. The current study investigates the antibacterial activity of copper oxide (CuO) NMs to Escherichia coli K12, Enterococcus faecalis, and Lactobacillus casei using a combination of approaches and evaluates the importance of reactive oxygen species (ROS) production as a mechanism of toxicity. The impact of CuO NMs (100, 200, and 300 μg/mL) on the growth and viability of bacterial strains was assessed via plate counts, optical density (OD) measurements, well and disc diffusion assays, and live/dead fluorescent imaging. CuO NMs reduced the viability of all bacteria in a concentration-dependent manner in all assays except the diffusion assays. The most sensitive methods were OD measurements and plate counts. The sensitivity of bacterial strains varied depending on the method, but overall, the results suggest that E. coli K12 is the most sensitive to CuO NM toxicity. The production of ROS by all bacterial strains was observed via DCFH-DA fluorescent imaging following exposure to CuO NMs (300 μg/mL). Overall, the data suggests that CuO NMs have antibacterial activity against gut-relevant bacteria, with evidence that NM-mediated ROS production may contribute to reductions in bacterial viability. Our findings suggest that the use of a combination of assays provides a robust assessment of the antibacterial properties of ingested NMs, and in particular, it is recommended that plate counts and OD measurements be prioritised in the future when screening the antibacterial properties of NMs. Full article

Prunus leaf extracts are rich in phenolic and flavonoid compounds like rutin, and they are known for their antioxidant potential. This study compares the bioactivity and stability of leaf extracts from Prunus domestica L. (EL), Prunus salicina Lindl. (JL), and Prunus cerasifera Ehrh. (CL) and evaluates the dermal safety of a cream containing the extract with the most favorable in vitro properties for potential cosmetic use. Ethanolic extracts were assessed for total phenolic and condensed tannin contents, as well as antioxidants, using DPPH assay and lipid peroxidation inhibitory activities. The CL extract exhibited moderate total phenolic content, the highest condensed tannin content, and strong antioxidant (IC₅₀ = 22.1 ± 3.1 µg/mL) and anti-lipid peroxidation (62.3 ± 1.0%) activities. Based on these results, CL was incorporated into a cream formulation (CCL), which was then evaluated for physicochemical properties, antioxidant retention, and in vitro skin permeation using Franz diffusion cells. The formulation remained physically stable under ambient conditions and retained antioxidant activity above 74.5% under thermal cycling conditions. Rutin from the CCL formulation was retained within the Strat-M™ membrane (4.0 ± 1.1%), which was 5.7-fold higher than that of the control (0.7 ± 0.6%) over 8 h; however, it was not detected in the receptor chamber under these in vitro conditions. A semi-open patch test conducted on 26 healthy volunteers under double-blind conditions revealed no signs of irritation, confirming the formulation’s dermal safety. Overall, the findings support the feasibility of using P. cerasifera extract as a stable antioxidant component in topical skincare formulations. Full article

The present study aimed to identify the active chemical compounds, mainly phenolic acids, of Champia parvula and Moringa oleifera, evaluate the pharmacokinetic properties of their primary compounds, and assess a novel method for the biocontrol of blue mold by evaluating the antifungal activity of both extracts. Gas chromatography (GC) and high-performance liquid chromatography (HPLC) were utilized to identify the active chemical compounds, mainly phenolic acids. GC illustrated the presence of long-chain aliphatic fatty acids like eicosanoic acid with the formation of oct-1-en-3-ol compounds attached. Catechin was the main bioactive component among the several bioactive compounds identified by HPLC analysis, exhibiting favorable pharmacokinetic behavior, including good absorption, distribution, and metabolic stability. According to the findings, both extracts had antifungal activity, but C. parvula extract (100 mg/mL) exhibited the strongest in vitro and in vivo antifungal activity, with the highest percentages of inhibition (disk diffusion method) against Penicillium expansum, Penicillium crustosum, and Talaromyces atroroseus, ranging between 62.67 and 100%. C. parvula extract (100 mg/mL) could fully inhibit the pathogenicity and aggressiveness of the five tested strains in apple fruits (in vivo). In conclusion, the extract from C. parvula and M. oleifera shows potential antifungal properties and a high phytochemical content. Full article