Search Results (46)

The Ib-M1 peptide exhibits bactericidal activity against Escherichia coli O157:H7 and low toxicity in mammalian cells. The present study aimed to evaluate the effect of Ib-M1 on E. coli O157:H7 membrane permeabilization. For this purpose, the minimum inhibitory concentrations of Ib-M1 for E. coli O157:H7 and ML35 were measured. The permeability of the E. coli outer and inner membranes was determined by measuring N-phenyl-1-naphthylamine and O-nitrophenyl-β-galactosidase hydrolysis, respectively after bacterial exposure to antimicrobial peptides and control antibiotics. Morphological changes in antimicrobial-exposed E. coli O157:H7 were evaluated by scanning electron microscopy following treatment with antimicrobial peptides. Ib-M1 expressed activity against E. coli O157:H7 and ML35 at minimal inhibitory concentrations (MIC) of 2.9 ± 1.7 and 6.3 ± 0 μM, respectively. The peptide induced permeabilization of the outer membrane of E. coli O157:H7 at all concentrations evaluated and permeabilization of the inner membrane after 50 min at concentrations between 1× MIC and 8× MIC. The morphological changes induced by Ib-M1 led to significant alterations in bacterial shape including collapsed cells and pronounced surface roughness and invaginations. In conclusion, physiological and morphological evidence indicates that the Ib-M1 antimicrobial effect against E. coli O157:H7 is mediated by its permeabilizing action on the outer and inner bacterial membranes. Full article

In the present work, we describe the synthesis of a new heterocyclic derivative, 2-(naphthalen-1-yl)-2,3,5,6-tetrahydro-1H-isoquinolino[8,1,2-hij]quinazoline 1, using the reaction between the aminal 1,3,6,8-tetraazatricyclo[4.4.1.1^3,8]dodecane 2 (TATD) and 1-naphthylamine 3 as the first scaffold of a four-step linear synthetic route. In the first step, a condensation catalyzed by acetic acid in 96% ethanol was carried out, leading to the formation of the intermediate 3-(naphthalen-1-yl)-1,2,3,4-tetrahydrobenzo[h]quinazoline 4. Subsequently, this intermediate was acylated with 2-chloroacetyl chloride in the presence of triethylamine and under an inert atmosphere, obtaining the compound 2-chloro-1-(3-(naphthalen-1-yl)-3,4-dihydrobenzo[h]quinazolin-1(2H)-yl)ethan-1-one 5. In the third step, an intramolecular Friedel–Crafts cyclization was carried out using aluminum trichloride as a catalyst, yielding 2-(naphthalen-1-yl)-1,2,3,6-tetrahydro-5H-isoquinolino[8,1,2-hij]quinazolin-5-one 6. Finally, the reduction of this lactam with phosphorus pentachloride and sodium borohydride under anhydrous conditions led to the further closure of the polycyclic system, yielding the final product 1. The proposed route demonstrates the feasibility of using TATD 2 as a versatile precursor for constructing condensed heterocyclic systems of structural interest and potential relevance in advanced organic synthesis. Full article

A series of silica-supported, nitrogen-doped carbon-encapsulated cobalt–nickel alloy catalysts (Co_xNi_y@NC/SiO₂) was successfully synthesized and systematically evaluated for the liquid-phase hydrogenation of 1-nitronaphthalene to 1-naphthylamine. Physicochemical characterization confirmed that the incorporation of nickel promotes the formation of Co–Ni alloys and modulates the electronic structure of the catalysts. The catalytic performance was found to be highly sensitive to the Co/Ni ratio, with Co₂Ni₁@NC/SiO₂ exhibiting the most outstanding activity. Under optimized reaction conditions (90 °C, 0.6 MPa H₂, 5.5 h), both the conversion of 1-nitronaphthalene and the selectivity toward 1-naphthylamine reached approximately 99%. The catalyst also demonstrated excellent stability and recyclability, attributed to the protective nitrogen-doped carbon shell and the synergistic interaction between the Co–Ni alloy and M–N_x active sites. This work provides a new strategy for designing efficient and robust non-noble-metal catalysts for hydrogenation reactions. Full article

Compared with traditional lubricants, polyol ester lubricants exhibit superior oxidative stability and have been widely applied in extreme operating conditions such as aviation engines. However, under high-temperature conditions, polyol esters are still susceptible to oxidation and therefore require the addition of antioxidants. N-phenyl-α-naphthylamine is an excellent high-temperature antioxidant used in polyol ester. However, a notable issue is that oil sludge may form when this antioxidant is used at high temperatures. Excessive sludge can lead to a series of problems such as oil circuit blockage, more severe mechanical wear, and poor heat dissipation performance. In this work, oil sludge formation from N-phenyl-α-naphthylamine was simulated via high-temperature oxidation experiments in a polyol ester base oil. The formed sludge was then characterized by various advanced techniques, such as FT-IR, GPC, TGA, MALDI-TOF MS, and XPS. The results showed that the oil sludge was mainly composed of derivatives of polyol esters and N-phenyl-α-naphthylamine, along with some metal components. Further analysis showed that polymerization reactions between antioxidant molecules are the key factors leading to sludge generation, and polycyclic aromatic compounds formed by polymerization are responsible for inducing sludge generation in polyol esters. Full article

Increased bacterial resistance to current antibiotics leads to a depletion of therapeutic options in medicine. One of the problems of current therapy is methicillin-resistant Staphylococcus aureus (MRSA), which, in addition to resistance to β-lactam antibiotics, is multidrug-resistant. Some strains can also produce biofilms, a multicellular structure that is resistant or tolerant to various antibiotics. In hospitals worldwide, about 15% of invasive infections are caused by MRSA. Extracts of Rubus caesius (dewberry) contain high concentrations of compounds such as phenolic acids, flavonoids, tannins, and anthocyanins, which have potential antibacterial properties. This study is the first to demonstrate the activity of aqueous and ethanolic extracts of dewberry leaves (L_H2O, L_EtOH) and stems (S_H2O, S_EtOH) against S. aureus and Staphylococcus epidermidis. The most active extracts were L_EtOH (MIC 0.16 ± 0.40–1.56 ± 0.23 mg/mL) and L_H2O (MIC 0.16 ± 0.20–10 mg/mL). The study showed that L_EtOH, S_EtOH and L_H2O extracts inhibited biofilm formation by clinical strains MRCN (methicillin-resistant coagulase-negative staphylococci) and MRSA (biofilm biomass reduction from 40 to 100%). Furthermore, 3,3′—dipropylthiacarbocyanine (DiSC₃(5)) and N-phenyl-naphthylamine (NPN) were used to show that L_EtOH and S_EtOH caused the membrane depolarization of the strains studied. We also showed that the extracts acted synergistically and additively with cefoxitin and amikacin, reducing the MIC values of the antibiotics used by 8- to 16-fold and of the extracts tested by 4- to 8-fold. This study provides new data on potential antibacterial drugs of therapeutic importance. Full article

Background: There is substantial evidence supporting the role of genetic alterations in chemically induced carcinogenesis. We analyzed the existing literature to gather data on genetic alterations linked to human carcinogens and their possible connection to genotoxic outcomes. The review emphasizes carcinogenic substances and occupational exposures identified as “carcinogenic to humans”. In particular, we searched for studies describing genotoxic alterations linked to agents and occupational exposures for which the International Agency for Research on Cancer has found sufficient evidence of an association with bladder cancer. Methods: The review was carried out in compliance with the PRISMA standards. A comprehensive search of the PubMed database was conducted to identify studies published through March 2024. Results: We identified 60 studies that evaluated genetic alterations for 16 carcinogenic agents and occupations (such as aluminum production, 4-aminobiphenyl, auramine production, benzidine, chlornaphazine, cyclophosphamide, firefighters, magenta production, 2-naphthylamine, opium consumption, ortho-toluidine, painters, the rubber manufacturing industry, Schistosoma haematobium infection, X-radiation, gamma-radiation) in healthy humans. Conclusions: The genotoxic effects of chemical agents in healthy individuals have been well studied and characterized. Additionally, this review presents numerous studies concerning occupational exposure but not exclusively. Genotoxicity assessments have mainly been conducted on biological materials such as blood, peripheral blood lymphocytes, urine, and buccal epithelial cells. The most frequently examined genotoxic effects were DNA damage, chromosomal abnormalities, and micronuclei. Standardized data to clearly define a dose–response relationship for predicting delayed health effects are still lacking. Full article

Background: Antibiotics are antimicrobial drugs used to treat and prevent infections. Unconscious use of antibiotics leads to many negative results. This study aimed to emphasize the negative aspects of antibiotics by determining their effects on purified enzymes. Methods: Beta glucosidase enzymes (BGLs) were purified from rat liver and kidney tissues using the sepharose-4B-LTyrosine-1-Naphthylamine hydrophobic interaction chromatography method. Liver BGL enzyme was purified 30.2-fold with a yield of 43.4%, while kidney BGL was purified 5.1-fold with a yield of 12.2%. Purified enzymes were visualized using SDS–PAGE. In vitro inhibition effects of ampicillin cefuroxime, amoxicillin–clavulanate, cefazolin sodium, gentamicin, and ceftriaxone antibiotics were determined on purified BGLs. Results: Ampicillin was found to inhibit rat liver and kidney BGLs competitively and uncompetitively, with IC50 values of 69.56 and 25.30 mM, respectively. Other antibiotics investigated did not significantly reduce liver BGL activity. Cefuroxime inhibited rat kidney BGL uncompetitively with IC50 values of 76.88 mM, while amoxicillin–clavulanate and cefazolin sodium inhibited it noncompetitively, with IC50 values of 41.32 and 98.81 mM, respectively. Gentamicin and ceftriaxone, whose effects were investigated, did not reduce kidney BGL activity. Conclusions: Some of the commonly used antibiotics reduce liver and kidney BGL activity, and this indicates that they may potentially impair metabolic functions. These results emphasize that caution should be exercised when using antibiotics. Full article

Helicobacter pylori (H. pylori) infection is a widespread gastric infectious disease, posing significant challenges due to the increasing prevalence of antibiotic resistance. This study aimed to evaluate the synergistic antibacterial activity of Takifugu obscurus skin peptides (TSPs) and the cell-free supernatant of Lactobacillus plantarum WUH3 (LCFS) in developing a potential green and efficient dietary supplement therapy. Using enzymatic hydrolysis and ultrafiltration techniques, the most bioactive peptide fraction, TSPb (1–3 kDa), was identified. The effects of TSPb and LCFS—both individually and in combination—on H. pylori biofilm function, membrane morphology, and internal structure were systematically analyzed using urease activity, N-phenyl naphthylamine (NPN) uptake, nucleic acid leakage, scanning electron microscopy (SEM), and infrared (IR) spectroscopy. The results showed that both LCFS and TSPb significantly inhibited H. pylori urease activity, with inhibition rates of 53.60% and 54.21% at 24 h, respectively, and the highest inhibition rate of 74.64% was observed with their combined treatment. SEM, NPN fluorescence, and nucleic acid leakage analyses revealed distinct mechanisms of action for each treatment. LCFS treatment caused membrane surface loosening and morphological deformation, while TSPb induced the formation of localized membrane pores. IR spectroscopy further confirmed that the combined treatment led to a more severe disruption of the lipid and protein structure within the bacterium. Overall, compared to individual treatments, the combination of TSPb and LCFS exhibited enhanced intracellular penetration and a more significant effect on bacterial viability. This study successfully identified TSPb as a highly bioactive peptide and elucidated its potential synergistic antibacterial mechanism with LCFS. These findings provide scientific evidence for the development of functional antimicrobial foods and gastric health dietary supplements, offering a promising strategy for the prevention and management of H. pylori infections. Full article

A concise, transition metal-free four-step synthetic pathway has been developed for the synthesis of tetracyclic heterosteroidal compounds, 14-aza-12-oxasteroids, starting from readily available 2-naphthol analogues. After conversion of 2-naphthols to 2-naphthylamines by the Bucherer reaction, subsequent selective C-acetylation was achieved via the Sugasawa reaction and reduction of the acetyl group using borohydride, which resulted into the corresponding amino-alcohols. The naphthalene-based amino-alcohols underwent double dehydrations and double intramolecular cyclization with oxo-acids leading to one-pot formation of a C-N bond, a C-O bond and an amide bond in tandem, to generate two additional rings completing the steroidal framework. A series of 14-aza-12-oxasteroids were synthesized using our developed synthetic strategy in moderate yields, and the structure of one of the final products, 12a-Methyl-11-phenyl-11,12a-dihydro-1H-naphtho[2,1-d]pyrrolo[2,1-b][1,3]oxazin-3(2H)-one, was further confirmed by single crystal X-ray crystallography. Full article

Multidrug-resistant (MDR) bacteria, especially Escherichia coli, are a major contributor to healthcare-associated infections globally, posing significant treatment challenges. This study explores the efficacy of (−)-epigallocatechin gallate (EGCG), a natural constituent of green tea, in combination with ampicillin (AMP) to restore the effectiveness of AMP against 40 isolated MDR E. coli strains. Antimicrobial activity assays were conducted to determine the minimum inhibitory concentrations (MIC) of EGCG using the standard microdilution technique. Checkerboard assays were employed to assess the potential synergistic effects of EGCG combined with AMP. The pharmacodynamic effects of the combination were evaluated through time-kill assays. Outer membrane disruption was analyzed by measuring DNA and protein leakage and with assessments using N-phenyl-1-naphthylamine (NPN) and rhodamine 123 (Rh123) fluorescence dyes. Biofilm eradication studies involved biofilm formation assays and preformed biofilm biomass and viability assays. Scanning electron microscopy (SEM) was used to examine changes in cellular morphology. The results indicated that EGCG demonstrated activity against all isolates, with MICs ranging from 0.5 to 2 mg/mL, while AMP exhibited MIC values between 1.25 and 50 mg/mL. Importantly, the EGCG-AMP combination showed enhanced efficacy compared to either treatment alone, as indicated by a fractional inhibitory concentration index between 0.009 and 0.018. The most pronounced synergy was observed in 13 drug-resistant strains, where the MIC for EGCG dropped to 8 µg/mL (from 1 mg/mL alone) and that for AMP to 50 µg/mL (from 50 mg/mL alone), achieving a 125-fold and 1000-fold reduction, respectively. Time-kill assays revealed that the bactericidal effect of the EGCG-AMP combination occurred within 2 h. The mechanism of EGCG action includes the disruption of membrane permeability and biofilm eradication in a dose-dependent manner. SEM confirmed that the combination treatment consistently outperformed the individual treatments. This study underscores the potential of restoring AMP efficacy in combination with EGCG as a promising strategy for treating MDR E. coli infections. Full article

The concentration of small molecules reflects the normality of physiological processes in the human body, making the development of simple and efficient detection equipment essential. In this work, inspired by a facile strategy in point-of-care detection, two devices were fabricated to detect small molecules via photocurrent measurement. A linear response of the photocurrent against the concentration of the small molecules was found. In the first device, metal ions were introduced into gel substrates made by xanthan gum to enhance photocurrent response. N-phenyl-2-naphthylamine was measured when iron or manganese ions were used. L-Phenylalanine was measured when the gel was modified by samarium, iron, cerium, or ytterbium ions. L-(+)-Arabinose was detected via the gels modified by iron or holmium ions. D-(+)-Mannose was detected when the gel was modified by ytterbium, manganese, chromium, or sodium ions. L-Methionine was detected in the gels modified by samarium, zinc, or chromium ions. The second device was based on a paper sheet. A sugar-like molecule was first synthesized, which was then used to modify the paper. The detection was possible since the photocurrent showed a linear trend against the concentration of D-Trehalose. A linear fit was conducted to derive the sensitivity, whose value was found to be 5542.4. This work offers a novel, simple, and environmentally sustainable platform that is potentially useful in remote areas lacking medical devices. Full article

Nipah virus (NiV) is known to be a highly pathogenic zoonotic virus, which is included in the World Health Organization Research & Development Blueprint list of priority diseases with up to 70% mortality rate. Due to its high pathogenicity and outbreak potency, a therapeutic countermeasure against NiV is urgently needed. As NiV needs to be handled within a Biological Safety Level (BSL) 4 facility, we had developed a safe drug screening platform utilizing a baculovirus expression vector system (BEVS) based on a NiV-induced syncytium formation that could be handled within a BSL-1 facility. To reconstruct the NiV-induced syncytium formation in BEVS, two baculoviruses were generated to express recombinant proteins that are responsible for inducing the syncytium formation, including one baculovirus exhibiting co-expressed NiV fusion protein (NiV-F) and NiV attachment glycoprotein (NiV-G) and another exhibiting human EphrinB2 protein. Interestingly, syncytium formation was observed in infected insect cells when the medium was modified to have a lower pH level and supplemented with cholesterol. Fusion inhibitory properties of several compounds, such as phytochemicals and a polysulfonated naphthylamine compound, were evaluated using this platform. Among these compounds, suramin showed the highest fusion inhibitory activity against NiV-induced syncytium in the baculovirus expression system. Moreover, our in silico results provide a molecular-level glimpse of suramin’s interaction with NiV-G’s central hole and EphrinB2’s G-H loop, which could be the possible reason for its fusion inhibitory activity. Full article

With the continuous advancement of industrial technology, higher demands have been placed on the properties of gear oils, such as oxidation stability and shear resistance. Herein, the oxidation stability of high-viscosity metallocene poly-$\alpha$-olefins (mPAOs) was improved by chemical modification via aromatic amine alkylation. The modified mPAO base oils were synthesized separately with diphenylamine (mPAO-DPA) and N-phenyl-$\alpha$-naphthylamine (mPAO-NPA), and their applicability in industrial gear oil formulations was evaluated. The composition and physicochemical properties of the obtained samples were assessed using ¹H NMR spectroscopy, Fourier transform infrared spectroscopy, gel permeation chromatography, and the American Society for Testing and Materials standards (ASTM D445, ASTM D2270, ASTM D92, etc.) confirming the successful completion of the alkylation reaction. The oxidation stability of the samples was also evaluated using pressurized differential scanning calorimetry. The initial oxidation temperature of mPAO-NPA (230 °C) was 53 °C higher than that of mPAO, and the oxidation induction period of mPAO-DPA was nearly twice that of mPAO-NPA. Thermogravimetric analysis in air revealed the increased thermal decomposition temperature and improved thermal stability of modified mPAO. ISO VG 320 industrial gear oils were formulated using mPAO alkylated with N-phenyl-$\alpha$-naphthylamine(Lub-2) and commercially purchased PAO100 (Lub-1) as base oil components. The antioxidant performance of two industrial gear oils was evaluated through oven oxidation and rotating oxygen bomb tests. The oxidation induction period of Lub-2 was 30% higher than that of Lub-1, with the latter having a lower acid number and a smaller increase in viscosity at 40 °C. Finally, the friction performance of the samples was assessed on a four-ball friction tester, revealing the synergistic effect of the mPAO-NPA base oil with the HiTEC 3339 additive, forming a more stable oil film with a smaller wear scar diameter. Full article

The present work reports the synthesis of indigo-dye-incorporated polyaniline (Indigo-PANI), poly(1-naphthylamine) (Indigo-PNA), poly(o-phenylenediamine) (Indigo-POPD), polypyrrole (Indigo-PPy), and polythiophene (Indigo-PTh) via an ultrasound-assisted method. The synthesized oligomers were characterized using FTIR, UV–visible spectroscopy, X-ray diffraction (XRD), scanning electron microscopy (SEM), fluorescence studies, and thermogravimetric analysis (TGA). The experimental data were theoretically compared to analyze the vibrational and electronic spectra via time-dependent density-functional theory (TD-DFT) by applying the Becke, three-parameter, and Lee-Yang-Parr (B3LYP) method with a 6-311G (d,p) basis set. The experimental, theoretical vibrational, and electronic spectra were found to be in close agreement and confirmed the successful incorporation of indigo dye in PANI, PNA, POPD, PPy, and PTh. These studies confirmed that multifunctional oligomers could be synthesized through a facile technique by incorporating dye moieties to enhance their optoelectronic properties, allowing them to be utilized as near-infrared-emitting probes for photodynamic therapy. Full article

To investigate the role of candidate genes for salt–alkali tolerance in cucumber (Cucumis sativus L.), this study screened CsTAU1 in the glutathione pathway from previous transcriptome data for cloning and functional analysis. Clone cucumber CsTAU1 contains one 675 bp open reading frame, containing one GST-N-Tau domain and one GST-C-Tau domain, and is expressed in cytoplasm. After successfully constructing overexpression vectors of CsTAU1 (+) and CsTAU1 (−), they were transferred into cucumber varieties ‘D1909’ (high salt alkali resistance) and ‘D1604’ (low salt alkali resistance) for salt–alkali resistance identification. It was found that under salt–alkali stress, CsTAU1 (+)-overexpressing plants showed strong resistance to salt–alkali stress, while CsTAU1 (−)-overexpressing plants showed the opposite situation. qRT-PCR analysis was performed on other glutathione pathway-related genes in CsTAU1-overexpressing plants. The expression patterns of LOC101219529 and LOC105434443 were the same as CsTAU1, and the introduction of CsTAU1 (+) increased the chlorophyll, α-Naphthylamine oxidation, glutathione S-transferase (GST), and catalase (CAT) content of cucumber. The research results provide a theoretical basis for cultivating salt–alkali-tolerant cucumber varieties. Full article