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The crucial role of food in life has prompted a shift towards products that not only offer good quality and nutritional properties but also ensure the overall health of consumers. Probiotics, which are non-pathogenic microorganisms, can restore intestinal microbial balance when consumed in sufficient quantities. In this study, Limosilactobacillus fermentum ARD2 isolated from local yogurt was investigated for its probiotic properties. Various aspects of this strain were evaluated, including acid resistance (at pH levels of 2, 3 and 4), resistance to bile salts (at concentrations of 0.3, 0.5 and 0.7 %), antimicrobial activity using disk diffusion agar and well diffusion agar methods, resistance to common therapeutic antibiotics, evaluation of antioxidant activity, cell surface hydrophobicity, DNase enzyme activity, hemolytic activity, and biogenic amine and cholesterol absorption. The results of the acid resistance tests indicated that the viability of L. fermentum ARD2 increased as pH levels rose from 2 to 4, with a decrease observed over time at a constant pH over 3 hours. Growth was inhibited with increasing concentrations of bile salts. Antimicrobial testing revealed that the acidic and neutralized cell -free supernatant (aCFS and nCFS) had no significant antimicrobial effect on Escherichia coli, while nCFS showed no antimicrobial effect on Shigella dysenteriae. L. fermentum ARD2 exhibited resistance to Ciprofloxacin and was semi-sensitive to Penicillin and Nitrofurazone. The L. fermentum ARD2 showed considerable antioxidant activity, with DPPH and ABTS free radical inhibition rates of 41.40% and 43.60%, respectively. Additionally, it demonstrated the ability to reduce cholesterol absorption by 38.60%. The strain tested negative for DNase and hemolytic activities, and biogenic amine production was not observed. Based on these findings, L. fermentum ARD2 exhibits promising probiotic characteristics and could be utilized as a probiotic bacterium in food products. [ABSTRACT FROM AUTHOR]

Antimicrobial peptides (AMPs) are a promising class of antimicrobial drugs due to their broad-spectrum activity against microorganisms. However, their clinical application is limited by their potential to cause hemolysis, the destruction of red blood cells. To address this issue, we propose a deep learning model based on convolutional neural networks (CNNs) for predicting the hemolytic activity of AMPs. Peptide sequences are represented using one-hot encoding, and the CNN architecture consists of multiple convolutional and fully connected layers. The model was trained on six different datasets: HemoPI-1, HemoPI-2, HemoPI-3, RNN-Hem, Hlppredfuse, and AMP-Combined, achieving Matthew's correlation coefficients of 0.9274, 0.5614, 0.6051, 0.6142, 0.8799, and 0.7484, respectively. Our model outperforms previously reported methods and can facilitate the development of novel AMPs with reduced hemolytic activity, which is crucial for their therapeutic use in treating bacterial infections. [ABSTRACT FROM AUTHOR]

Developing novel, efficient, and safe peptide drugs from sea anemones has aroused great interest in countries around the world today. Sea anemones contain complex protein and peptide toxins, which determine the diversity of their biological activities. In this study, a variety of activities were assessed for crude venom extracted from five species of South China Sea anemones, including hemolytic, enzyme inhibition, anticancer, insecticidal, analgesic and lethal activities. The most toxic sea anemone was found to be Heteractis magnifica , which has high lethal activity in mice with an LD50 of 11.0 mg/kg. The crude venom of H. magnifica also exhibited a range of the most potent activities, including hemolytic, trypsin inhibitory, cytotoxic activity against U251 and A549 cells, insecticidal and analgesic activities. In addition, the crude venom of Stichodactyla haddoni was the most effective inhibitor of pepsin, and the crude venom of Heteractis crispa was extremely strong toxicity to HepG2 cells. These findings are of great significance for exploring the potential and application of South China Sea anemone resources, and are expected to provide new directions and possibilities for the development of novel anticancer drugs, analgesics and biopesticides. [ABSTRACT FROM AUTHOR]

ABSTRACT Antimicrobial peptides (AMPs) offer a promising strategy to address bacterial resistance by targeting bacterial membranes, bypassing the limitations of receptor site‐based approaches. This study focuses on combating the notorious multidrug resistance of Staphylococcus aureus using AMPs, particularly maximin peptides derived from Bombina maxima. Previous research suggested that maximin peptides could disrupt bacterial membranes among anuran AMPs. This prompted us to screen these maximin peptides to identify those with strong membrane‐targeting abilities against S. aureus. Initially, stability and activity assessments on all 89 peptides involved analyzing hydrogen bond dilution, peptide permeation, and hemolytic activity predictions, leading to the rationalization of four promising candidates: Max_5, Max_13, Max_21, and Max_45. When subjected to membrane simulations, the monomeric state of these peptides displayed partial helix‐coil transitions with significant structural interactions that disrupted the membrane, particularly for Max_5 and Max_13. Additionally, the multimeric states of these two peptides were examined through membrane simulations to elucidate their mechanisms of action. Analyses focusing on membrane thickness, lipid distortions, and curvature revealed that both Max_5 and Max_13 exerted strong membrane‐rupturing effects. These peptides seemed to operate by forming pores, facilitating lipid diffusion, creating cavities, and affecting membrane thickness, which allowed water penetration due to increased membrane fluidity, indicating the barrel‐stave pore model. Despite structural differences between Max_5 and Max_13, both peptides demonstrated similar outcomes, emphasizing their potential for future therapeutic applications. This study highlights the efficacy of computational methods in accelerating the identification of potent antimicrobial peptides, providing a pathway for developing novel antimicrobial therapies. [ABSTRACT FROM AUTHOR]

In numerous countries, the utilization of plants for both nutritional and therapeutic purposes is a common practice. However, the inadvertent use of these plants can pose risks due to their active molecules or microbiota. The traditional use of Herniaria glabra L. (H. glabra) plant in treating various diseases is well-known; however, its application in yogurt production raises concerns. In this study, Bacillus pumilus isolated from H. glabra was identified through 16s rRNA sequencing and MALDI-TOF MS (Matriks Assisted Lazer Desorption Ionization Time of Flight Massspectrometry). The bacterium's resistance under simulated gastrointestinal tract (GIT) conditions was assessed, followed by investigations into its aggregation ability, antibiotic resistance, hemolytic activity, and antagonistic potential through in vitro tests. The study revealed that B. pumilus exhibited 100% resistance to GIT conditions. Notably, the bacterium demonstrated strong autoaggregation (34.48%) and coaggregation abilities (49.82% for Escherichia coli, 49.13% for Listeria monocytogenes), signifying a potent aggregative potential. Sensitivity to most tested antibiotics was observed, while no antagonistic activity against tested bacteria was evident. Furthermore, the bacterium exhibited β-hemolytic activity, indicative of potential virulence. The findings suggest that this resistant yet virulent bacterium, with its hemolytic activity, could disrupt the GIT balance, posing serious health risks. The study underscores the need for caution and awareness regarding the potential dangers posed by bacteria in plant microbiota in herbal therapies. [ABSTRACT FROM AUTHOR]

Pure, Ni-doped, and Ni/Co–co-doped magnetite nanoparticles at different Co concentrations (1%, 2%, and 3%) and a constant concentration value of Ni were fabricated by the hydrothermal method. The nanoparticles were investigated by X-ray diffraction, field-emission scanning electron microscopy, energy-dispersive X-ray spectroscopy, a vibrating sample magnetometer, Fourier-transform infrared spectroscopy, and UV–visible spectroscopy. The X-ray diffraction showed that pure Fe3O4, Ni-Fe3O4, and 3%Ni-3%Co-Fe3O4 have cubic inverse-spinel structures, while the samples co-doped with Ni:Co (1%, 2%) revealed orthorhombic structure. The doping resulted in a reduction of the average crystalline size values from 47.755 to 9.927 nm. The morphology of all the samples was spherical, with a mean diameter in the range of 75–120 nm. The presence of Ni, Co, Fe, and O in a lattice of Ni/Co–co-doped Fe3O4 was confirmed by energy dispersive X-ray spectroscopy (EDS) analysis. The FTIR spectrum displayed two bands at 400–50 cm−1 and 520–480 cm−1, which were present in all samples. These vibration bands correlate to the ferrite spinel lattice vibration. The UV–visible absorption spectra of doped and co-doped samples showed a blue shift in the absorption edge as compared to undoped (pure) magnetite nanoparticles. The energy gap increased with doping and co-doping, from 1.5 to 2.6 eV. The measurement of the magnetic characteristics of pure Fe3O4 (Ms = 82.7 emu g−1, Mr = 8.4 emu g−1, and HC = 60 Oe). While in the case of Ni-doped and Ni/Co–co-doped samples, all the extracted magnetic parameters declined in comparison to pure Fe3O4. Furthermore, the hemolysis assay of all samples with concentrations ranging between 100 and 800 µg/ml was used in this study. After completing the study of hemolytic activity for all samples, the results revealed that the activity was concentration-dependent. [ABSTRACT FROM AUTHOR]

Antimicrobial peptides have emerged as a potential alternative to combat the growing threat towards antimicrobial resistance. Owing to a large number of possible combinations of twenty naturally occurring amino acids, it is extremely resource intensive to experimentally identify whether a given peptide has desired therapeutic properties. To expedite the screening of therapeutic peptides, we propose a classification framework that can simultaneously predict the antibacterial activity, hemotoxicity, and efficacy against three most common pathogens i.e., Staphylococcus aureus , Escherichia coli , and Pseudomonas aeruginosa for any given peptide. The proposed framework uses support vector machine algorithm with amino acid compositions, sequence analysis, and physicochemical properties as features to develop three binary classifiers. Our models resulted in accuracies of 97.3 %, 86.2 %, and 84.1 % for antibacterial activity, combined efficacy against all three pathogens, and hemotoxicity, respectively. Explainable machine learning algorithm was implemented for each model to elucidate meaningful insights. It was evident that physicochemical properties along with the occurrence of certain amino acids play the most important role in determining antibacterial activity, efficacy, and hemolytic activity of peptides. The entire framework is made accessible freely in form of a web tool, which will further aid in rapid screening of antibacterial peptides with high therapeutic potential. [Display omitted] • Framework to screen antibacterial peptides with high efficacy and low hemotoxicity. • Predicts efficacy against three pathogens – S. aureus , E. coli , and P. aeruginosa. • Insights extracted from proposed models are in agreement with experimental findings. • Physicochemical properties play a crucial role in determining therapeutic potential. • Amino acid sequence affects efficacy more than antibacterial or hemolytic activity. [ABSTRACT FROM AUTHOR]

Abstract Antimicrobial peptides (AMPs) are a promising class of antimicrobial drugs due to their broad-spectrum activity against microorganisms. However, their clinical application is limited by their potential to cause hemolysis, the destruction of red blood cells. To address this issue, we propose a deep learning model based on convolutional neural networks (CNNs) for predicting the hemolytic activity of AMPs. Peptide sequences are represented using one-hot encoding, and the CNN architecture consists of multiple convolutional and fully connected layers. The model was trained on six different datasets: HemoPI-1, HemoPI-2, HemoPI-3, RNN-Hem, Hlppredfuse, and AMP-Combined, achieving Matthew’s correlation coefficients of 0.9274, 0.5614, 0.6051, 0.6142, 0.8799, and 0.7484, respectively. Our model outperforms previously reported methods and can facilitate the development of novel AMPs with reduced hemolytic activity, which is crucial for their therapeutic use in treating bacterial infections.

Colibacillosis is an intestinal tract infection in poultry caused by Escherichia coli. It is one of the leading causes of mortality and results in significant economic losses for the poultry farming sector due to its high incidence rate. Recently, E. coli has been considered a predominant bacterial pathogen that is responsible for diarrhea and bloodstream infections in chickens and ducks in Vietnam. In this study, E. coli strains associated with diarrhea were isolated from chicken and duck feces and intestines collected from poultry farms in Hai Phong province using a Macconkey selective medium. The obtained isolates were initially identified by the MALDITOF MS method, screened for hemolytic activity, and finally identified by 16S rRNA gene sequencing. As a result, eight E. coli strains exhibiting hemolytic activity were identified. Among them, E. coli_5, E. coli_6, and E. coli_8 strains were clustered with E. coli O78:H51, whereas E. coli_3 was grouped with E. coli O78:H4; E. coli_4 and E. coli_7 were clusterd with E. coli O25b: H4; and E. coli_9 and E. coli_16 were grouped with E. coli O26:H11. Our results provide insights into the genetic diversity of E. coli strains associated with diarrhea in poultry farms in Hai Phong province. The isolated strains will be further characterized for the development of effective strategies to control colibacillosis in poultry. [ABSTRACT FROM AUTHOR]

Saponins are glycosides widely distributed in the plant kingdom and have many pharmacological activities. However, their tendency to bind to cell membranes can cause cell rupture, limiting their clinical use. In the previous study, aristatoside C and davisianoside B were isolated from Cephalaria species. Cytotoxicity assays showed that they are more active on A‐549 cell lines than doxorubicin but caused hemolysis. In the current research, aristatoside C and davisianoside B were loaded to phytosomes called ALPs and DLPs respectively, and characterized for particle size, zeta potential, encapsulation efficiency, release kinetic, hemolytic activity, and cytotoxicity on A‐549 cell line. DLPs maintained the cytotoxic activity of the free saponins against A‐549 cells with IC50 of 9,64±0,02 μg/ml but dramatically reduced their hemolytic activity. Furthermore, temperature and time‐dependent stability studies based on the size and zeta potential of ALPs and DLPs revealed that the phytosomes have sustained release properties over 2 weeks. Overall, DLPs displayed cytotoxicity against A‐549 cells with minimal hemolysis and sustained release, highlighting their potential as nanotherapeutics for clinical applications. [ABSTRACT FROM AUTHOR]

Objective: In this work, in order to optimize the structure of histidine-containing antifungal peptides with a "linear" type of amphipathicity (LTA), we carried out the synthesis and comparative screening of the antifungal activity of a series of histidine-containing SAMPs (F2H7, F2H10, F2H13, F2H16, H10, H10F2) with a "linear" type of amphipathicity that we constructed de novo. We also aimed to study their hemolytic properties, to assess their therapeutic index, and to compare the obtained results with similar data for the antifungal histidine-rich 12-mer peptide P113 (AKRHHGYKRKFH), a drug candidate known as PAC-113, one of the shortest and most active analogues of the natural antifungal histidine-rich peptide Hst 5. Methods: Peptides were synthesized by a solid phase method using a Fmoc-based strategy. To determine the antifungal activity of the peptides, we used the opportunistic fungus strain Candida albicans EMTK 34. The number of microorganisms (titer) in the suspension was determined by optical density at a wavelength of 595 nm. To determine the antifungal activity of the peptides, cell cultures were co-incubated with the studied peptides in 96-well plates. The cells were incubated with the drug for 24 h at 37°C. To assess the antifungal activity of the studied peptides, their minimum inhibitory concentrations (MIC50) were determined, i.e. such peptide concentration at which the growth of microorganisms was suppressed by 50%. To assess the toxicity of the peptides, their hemolytic activity was determined, which was tested against fresh human erythrocytes using a photometric method. To assess the selectivity of the action of peptides, the values of the minimum hemolytic concentration (MHC) of the peptides were determined and the values of their therapeutic index (TI) were calculated as the ratio of the minimum hemolytic concentration (MHC) to the MIC50 value. Results and Discussion: It was shown that the antifungal activity of the studied SAMPLTA increases with an increase in the number of histidine residues in their composition, reaching the maximum value for the histidine-containing peptide F2H16 (MIC50 = 1.0 µM). It has been shown that as the chain length of peptides increases, their hemolytic toxicity also increases. The TI values for these peptides were 233, 247, 79, and 60, respectively. It has been shown that, against C. albicans, histidine-containing SAMP-LTA derivatives with phenylalanine residues at the N-terminus of the peptide (F2H10) are less effective compared to similar peptides (H10F2) containing phenylalanine residues at the C-terminus. Among the studied peptides, the most active was the H10 peptide (MIC50 = 0.7 µM), which does not contain phenylalanine residues, which in its antifungal activity is not only more effective than all other histidine-containing peptides, including the F2H16 peptide with 16 histidine residues, but also 4– 5 times more effective than the antifungal peptide P113 (MIC50 = 3.4 µM), a short active fragment of natural Hst 5, well known from the literature. Among all the studied peptides, H10 and P113 have minimal (almost zero) values of hemolytic activity. However, due to its higher antifungal activity, the selectivity of the H10 peptide (TI > 1400) exceeds the selectivity of the P113 peptide (TI > 340) by more than 4 times. Conclusions: Thus, peptide H10, due to its high antifungal activity, low hemolytic toxicity and, accordingly, high therapeutic significance, can be used as a promising antifungal peptide drug. [ABSTRACT FROM AUTHOR]

The alarming rise in antimicrobial resistance (AMR) has created a significant public health challenge, necessitating the discovery of new therapeutic agents to combat infectious diseases and oxidative stress-related disorders. The Lentzea flaviverrucosa strain E25-2, isolated from Moroccan forest soil, represents a potential avenue for such research. This study aimed to identify the isolate E25-2, obtained from soil in a cold Moroccan ecosystem, and further investigate its antimicrobial and antioxidant activities. Phylogenetic analysis based on 16S rRNA gene sequences revealed the strain's classification within the Lentzea genus, with a sequence closely resembling that of Lentzea flaviverrucosa AS4.0578 (96.10% similarity). Antimicrobial activity in solid media showed moderate to strong activity against Staphylococcus aureus ATCC 25923, Bacillus cereus strain ATCC 14579, Escherichia coli strain ATCC 25922, Candida albicans strain ATCC 60193 and 4 phytopathogenic fungi. In addition, ethyl acetate extract of this isolate demonstrated potent antimicrobial activity against 7 clinically multi-drug resistant bacteria. Furthermore, it demonstrated antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, as well as a significant increase in ferric reducing antioxidant power. A significant positive correlation was observed between antioxidant activities and total content of phenolic compounds (p < 0.0001), along with flavonoids (p < 0.0001). Furthermore, gas chromatography-mass spectrometry (GC-MS) analysis revealed the presence of amines, hydroxyl groups, pyridopyrazinone rings, esters and pyrrolopyrazines. The Lentzea genus could offer promising prospects in the fight against antibiotic resistance and in the prevention against oxidative stress related diseases. [ABSTRACT FROM AUTHOR]

The increasing global focus on green nanotechnology research has spurred the development of environmentally and biologically safe applications for various nanomaterials. Nanotechnology involves crafting diverse nanoparticles in terms of shapes and sizes, with a particular emphasis on environmentally friendly synthesis routes. Among these, biogenic approaches, including plant-based synthesis, are favored for their safety, simplicity, and sustainability. Silver nanoparticles, in particular, have garnered significant attention due to their exceptional effectiveness, biocompatibility, and eco-friendliness. Cannabis (Cannabis sativa L.) has emerged as a promising candidate for aiding in the green synthesis of silver nanoparticles. Leveraging the phytochemical constituents of Cannabis, researchers have successfully tailored silver nanoparticles for a wide array of applications, spanning from biomedicine to environmental remediation. This review explores the properties, synthesis mechanisms, and applications of silver nanoparticles obtained from Cannabis. Additionally, it delves into the recent advancements in green synthesis techniques and elucidates the optical properties of these nanoparticles. By shedding light on plant-based fabrication methods for silver nanoparticles and their diverse bionanotechnology applications, this review aims to contribute to the growing body of knowledge in the field of green nanotechnology. Through a comprehensive examination of the synthesis processes, mechanistic aspects, and potential applications, this review underscores the importance of sustainable approaches in nanoparticle synthesis and highlights the potential of Cannabis-derived silver nanoparticles in addressing various societal and environmental challenges. [ABSTRACT FROM AUTHOR]

Probiotics are non -pathogenic and beneficial bacteria that contribute to improving digestive health, preventing various types of cancer, and boosting the body's immune system, among other benefits. The aim of this study was to investigate the probiotic potential and antimicrobial activity of the strain Lacticaseibacillus rhamnosus JCM 1136. In this research, the probiotic and safety characteristics of the strain were assessed, including acid resistance at pH 2, 3, and 4, bile resistance (0%, 0.3%, 0.5%, and 0.7% bile salt concentration), hydropHobicity, potential for producing DNase enzyme and biogenic amines, hemolytic activity, antioxidant activity, cholesterol absorption capacity, and resistance to common antibiotics. The antimicrobial effect of the strain against pathogenic bacteria (Shigella dysenteriae, Salmonella typhimurium, Escherichia coli, Staphylococcus aureus, Listeria innocua, and Bacillus cereus) was evaluated using the agar well diffusion and disk diffusion methods. The results showed that L. rhamnosus JCM 1136 exhibited survival capability at different pH levels. The growth of the strain decreased with increasing bile salt concentration. L. rhamnosus JCM 1136 showed intermediate to the antibiotic Ampicillin and sensitivity to other antibiotics. The hydropHobicity, antioxidant activity by DPPH and ABTS methods, and cholesterol absorption capacity of the strain were 50.0 ± 50.53%, 50.0 ± 23.44%, 62.0 ± 50.48%, and 43.0 ± 55.41%, respectively. No production of DNase enzyme, biogenic amines, or hemolytic activity was observed in the strain. L. rhamnosus JCM 1136 exhibited a greater antimicrobial effect against Gram -positive bacteria. The results indicate that L. rhamnosus JCM 1136 possesses desirable probiotic characteristics and can be used in the production of probiotic food products. [ABSTRACT FROM AUTHOR]

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Developing novel, efficient, and safe peptide drugs from sea anemones has aroused great interest in countries around the world today. Sea anemones contain complex protein and peptide toxins, which determine the diversity of their biological activities. In this study, a variety of activities were assessed for crude venom extracted from five species of South China Sea anemones, including hemolytic, enzyme inhibition, anticancer, insecticidal, analgesic and lethal activities. The most toxic sea anemone was found to be Heteractis magnifica, which has high lethal activity in mice with an LD50 of 11.0 mg/kg. The crude venom of H. magnifica also exhibited a range of the most potent activities, including hemolytic, trypsin inhibitory, cytotoxic activity against U251 and A549 cells, insecticidal and analgesic activities. In addition, the crude venom of Stichodactyla haddoni was the most effective inhibitor of pepsin, and the crude venom of Heteractis crispa was extremely strong toxicity to HepG2 cells. These findings are of great significance for exploring the potential and application of South China Sea anemone resources, and are expected to provide new directions and possibilities for the development of novel anticancer drugs, analgesics and biopesticides.

Abstract The present study focused on evaluating the antibacterial properties, radical scavenging, and photocatalytic activities of Centaurea behen-mediated silver nanoparticles (Cb-AgNPs). The formation of Cb-AgNPs was approved by UV–Vis spectrometry, Fourier-transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy (SEM), energy dispersive X-ray and X-ray diffraction. The results showed that the obtained AgNPs have a maximum absorbance peak at 450 nm with spherical morphology and an average size of 13.03 ± 5.8 nm. The catalytic activity of the Cb-AgNPs was investigated using Safranin O (SO) solution as a cationic dye model. The Cb-AgNPs performed well in the removal of SO. The coupled physical adsorption/photocatalysis reaction calculated about 68% and 98% degradation of SO dye under solar irradiation. The Cb-AgNPs inhibited the growth of gram-negative or positive bacteria strains and had excellent DPPH radicals scavenging ability (100% in a concentration of 200 µg/ml) as well as a good effect on reducing coagulation time (at concentrations of 200 and 500 µg/mL reduced clotting time up to 3 min). Considering the fact that green synthesized Cb-AgNPs have antioxidant and antibacterial properties and have a good ability to reduce coagulation time, they can be used in wound dressings. As well as these NPs with good photocatalytic activity can be a suitable option for degrading organic pollutants.

Bangladesh is abundant in medicinal plants. The bioactive compounds in medicinal plants provide novel therapeutic opportunity of improving human health. But, the benefit-risk balance is usually less considered during formulation of traditional medicine. However, the plants that we included in this study are not studied regarding their hemolytic and anti-venom properties. Thus, we aimed to evaluate and compare the hemolytic activity, antioxidant activity, and phospholipase A2 (PLA2) enzyme neutralization efficacy of aqueous and methanolic extracts of eight known medicinal plants including Asparagus racemosus (root), Withania somnifera (root), Syzygium cumini (leaf), Psidium guajava (leaf), Basella alba (leaf and seed), Morus indica (leaf), M. laevigata (leaf), and M. latifolia (leaf). The results of the hemolytic activity test suggested that the methanolic extracts of S. cumini, P. guajava, B. alba (leaf and seed), M. indica, M. laevigata, and M. latifolia showed significantly higher hemolytic activity compared to their aqueous extracts. The methanolic extracts of A. racemosus, W. somnifera, P. guajava, M. laevigata, and M. latifolia showed remarkable antioxidant activity. Moreover, the results of the PLA2 enzyme neutralization activity test revealed that both aqueous and methanolic extracts of P. guajava, S. cumini, and B. alba (leaf) have significant PLA2 neutralization capacity. Altogether, the aqueous extracts of all plants, except A. racemosus root, have ignorable hemolytic effect. Additionally, P. guajava and S. cumini leaf aqueous extracts have promising PLA2 inhibitory effect and may become the potential source of bioactive compounds for anti-venom drug development. [ J Adv Biotechnol Exp Ther 2024; 7(1.000): 118-135]

The present study focused on evaluating the antibacterial properties, radical scavenging, and photocatalytic activities of Centaurea behen-mediated silver nanoparticles (Cb-AgNPs). The formation of Cb-AgNPs was approved by UV–Vis spectrometry, Fourier-transform infrared spectroscopy, transmission electron microscopy, scanning electron microscopy (SEM), energy dispersive X-ray and X-ray diffraction. The results showed that the obtained AgNPs have a maximum absorbance peak at 450 nm with spherical morphology and an average size of 13.03 ± 5.8 nm. The catalytic activity of the Cb-AgNPs was investigated using Safranin O (SO) solution as a cationic dye model. The Cb-AgNPs performed well in the removal of SO. The coupled physical adsorption/photocatalysis reaction calculated about 68% and 98% degradation of SO dye under solar irradiation. The Cb-AgNPs inhibited the growth of gram-negative or positive bacteria strains and had excellent DPPH radicals scavenging ability (100% in a concentration of 200 µg/ml) as well as a good effect on reducing coagulation time (at concentrations of 200 and 500 µg/mL reduced clotting time up to 3 min). Considering the fact that green synthesized Cb-AgNPs have antioxidant and antibacterial properties and have a good ability to reduce coagulation time, they can be used in wound dressings. As well as these NPs with good photocatalytic activity can be a suitable option for degrading organic pollutants. [ABSTRACT FROM AUTHOR]

Lipophilicity is a physicochemical parameter well known as a decisive factor for predicting the successful development of a drug. Thus, a balance between potency and physicochemical properties during medicinal chemistry optimization is needed. In this study, the lipophilicity of isoindole-1,3(2H)-dione derivatives designed as phosphodiesterase 10A (PDE10A) inhibitors was determined by chromatographic [reversed-phase thin-layer chromatography (RP-TLC) and ultra-performance liquid chromatography/mass spectrometry (UPLC/MS)] and in silico methods. To assess the correlation between the obtained lipophilicity parameters, principal component analysis (PCA) was performed. logP values obtained by chromatographic (logPRP-TLC and logPUPLC/MS) and in silico methods were compared using the PCA method. The results of PCA revealed that logPUPLC/MS and in silico clogP provided by the ChemDraw program were highly correlated. Compounds' drug likeness was screened, and the pharmacokinetic properties were predicted. All the investigated compounds displayed drug-likeness properties, and they met the criteria of Lipinski's rule of five, which predicted the oral bioavailability of drug candidates. Analysis of the influence of physicochemical properties on the biological activity showed that the compounds with increased potency on PDE10A had significantly higher topological polar surface area (TPSA) values. The blood‒brain barrier permeability and the hemolytic activity of model compound 18 were examined. The model compound 18 displayed no toxicity effect on erythrocytes in the hemolytic assay and good parallel artificial membrane permeability. The results showed that phthalimide compounds with benzimidazole moiety are a source of compound-targeted inhibition of PDE10A with balanced physicochemical and drug-likeness properties. [ABSTRACT FROM AUTHOR]

This study represents an advancement in the field of composite material engineering, focusing on the synthesis of composite materials derived from porous hydroxyapatite via surface modification employing cucurbit[n]urils, which are highly promising macrocyclic compounds. The surface modification procedure entailed the application of cucurbit[n]urils in an aqueous medium onto the hydroxyapatite surface. A comprehensive characterization of the resulting materials was undertaken, employing analytical techniques including infrared (IR) spectroscopy and scanning electron microscopy (SEM). Subsequently, the materials were subjected to rigorous evaluation for their hemolytic effect, anti-inflammatory properties, and cytotoxicity. Remarkably, the findings revealed a notable absence of typical hemolytic effects in materials incorporating surface-bound cucurbit[n]urils. This observation underscores the potential of these modified materials as biocompatible alternatives. Notably, this discovery presents a promising avenue for the fabrication of resilient and efficient biocomposites, offering a viable alternative to conventional approaches. Furthermore, these findings hint at the prospect of employing supramolecular strategies involving encapsulated cucurbit[n]urils in analogous processes. This suggests a novel direction for further research, potentially unlocking new frontiers in material engineering through the exploitation of supramolecular interactions. [ABSTRACT FROM AUTHOR]

The present investigation evaluated the toxic effect and bioactive potential of marine macro algae Caulerpa scalpelliformis. The crude methanolic extract was fractionated in diethylaminoethyl (DEAE) cellulose column chromatography using NaCl (0.1–10 M). The fractions were dialyzed and freeze-dried. The active fractions (F1, F2, and F3) were obtained using TLC chromatography. The crude methanolic extract and fractions showed strong hemolytic activity of 129.55, 73.73, 43.47, and 37.73 HT/mg in chicken blood, respectively, the human blood group (AB and O) showed considerable hemolytic activity of 73.73, 43.47, and 37.73 HT/mg, respectively, and the fraction (F3) had no activity. The acute toxic effect of the crude methanolic extract and fractions (F1, F2, and F3) showed the lethal dose (LD50) at 176, 121.5, 138, and 152 mg/kg body weight. The crude methanolic extract and fractions indicated strong analgesic activity at the ratio of 0.26, 0.37, 0.11, and 0.10 using the tail flick test in mice at 12.5 mg/kg body weight. These results suggest that the methanolic extract and its fractions from C. scalpelliformis may be potential pharmacological agents. [ABSTRACT FROM AUTHOR]

Abstract Saponins are glycosides widely distributed in the plant kingdom and have many pharmacological activities. However, their tendency to bind to cell membranes can cause cell rupture, limiting their clinical use. In the previous study, aristatoside C and davisianoside B were isolated from Cephalaria species. Cytotoxicity assays showed that they are more active on A‐549 cell lines than doxorubicin but caused hemolysis. In the current research, aristatoside C and davisianoside B were loaded to phytosomes called ALPs and DLPs respectively, and characterized for particle size, zeta potential, encapsulation efficiency, release kinetic, hemolytic activity, and cytotoxicity on A‐549 cell line. DLPs maintained the cytotoxic activity of the free saponins against A‐549 cells with IC50 of 9,64±0,02 μg/ml but dramatically reduced their hemolytic activity. Furthermore, temperature and time‐dependent stability studies based on the size and zeta potential of ALPs and DLPs revealed that the phytosomes have sustained release properties over 2 weeks. Overall, DLPs displayed cytotoxicity against A‐549 cells with minimal hemolysis and sustained release, highlighting their potential as nanotherapeutics for clinical applications.

Staphylococcus aureus is a common pathogen found in chronic wounds and it produces virulence factors that inhibit wound healing. There is no standard infection model, so culture supernatants based on different media are used to study the properties of this pathogen. To develop an in vitro infection model, we therefore compared the influence of different culture media on the virulence factors of S. aureus supernatants and their toxicity toward keratinocytes. Supernatants were prepared in brain heart infusion (BHI) broth, lysogeny broth (LB), nutrient broth (NB), and tryptic soy broth (TSB). We assessed bacterial growth, the protein content of the supernatants, and a range of biological activities. SDS-PAGE revealed distinct protein bands consistent with S. aureus hyaluronidase and hemolytic toxins. Hyaluronidase was present in all supernatants and the total activity was similar in BHI, LB, and TSB, but significantly lower in NB. The analysis of hemolytic activity on blood agar and sheep erythrocytes revealed that TSB supernatants showed the highest hemolytic activity closely followed by BHI. Finally, cell viability assays using HaCaT keratinocytes revealed concentration-dependent toxicity for all supernatants, particularly TSB. Our work therefore shows that the culture medium can affect the virulence factors in S. aureus supernatants and also influences their cytotoxicity. These aspects should be considered when using culture supernatants for in vitro studies, and the quantification of virulence factors may improve the relevance and reproducibility of such studies.

The alarming rise in antimicrobial resistance (AMR) has created a significant public health challenge, necessitating the discovery of new therapeutic agents to combat infectious diseases and oxidative stress-related disorders. The Lentzea flaviverrucosa strain E25-2, isolated from Moroccan forest soil, represents a potential avenue for such research. This study aimed to identify the isolate E25-2, obtained from soil in a cold Moroccan ecosystem, and further investigate its antimicrobial and antioxidant activities. Phylogenetic analysis based on 16S rRNA gene sequences revealed the strain’s classification within the Lentzea genus, with a sequence closely resembling that of Lentzea flaviverrucosa AS4.0578 (96.10% similarity). Antimicrobial activity in solid media showed moderate to strong activity against Staphylococcus aureus ATCC 25923, Bacillus cereus strain ATCC 14579, Escherichia coli strain ATCC 25922, Candida albicans strain ATCC 60193 and 4 phytopathogenic fungi. In addition, ethyl acetate extract of this isolate demonstrated potent antimicrobial activity against 7 clinically multi-drug resistant bacteria. Furthermore, it demonstrated antioxidant activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radicals, as well as a significant increase in ferric reducing antioxidant power. A significant positive correlation was observed between antioxidant activities and total content of phenolic compounds (p

Abstract Background and objectives Microbial cells capability to tolerate the effect of various antimicrobial classes represent a major worldwide health concern. The flexible and multi-components nanocomposites have enhanced physicochemical characters with several improved properties. Thus, different biological activities of biosynthesized starch/silver-selenium nanocomposite (St/Ag-Se NC) were assessed. Methodology The St/Ag-Se NC was biosynthesized using Cladosporium cladosporioides CBS 174.62 (C. cladosporioides) strain. The shape and average particle size were investigated using scanning electron microscope (SEM) and high-resolution transmission electron microscope (HR-TEM), respectively. On the other hand, the St/Ag-Se NC effect on two cancer cell lines and red blood cells (RBCs) was evaluated and its hydrogen peroxide (H2O2) scavenging effect was assessed. Moreover, its effects on various microbial species in both planktonic and biofilm growth forms were examined. Results The St/Ag-Se NC was successfully biosynthesized with oval and spherical shape and a mean particle diameter of 67.87 nm as confirmed by the HR-TEM analysis. St/Ag-Se NC showed promising anticancer activity toward human colorectal carcinoma (HCT-116) and human breast cancer (MCF-7) cell lines where IC50 were 21.37 and 19.98 µg/ml, respectively. Similarly, little effect on RBCs was observed with low nanocomposite concentration. As well, the highest nanocomposite H2O2 scavenging activity (42.84%) was recorded at a concentration of 2 mg/ml. Additionally, Staphylococcus epidermidis (S. epidermidis) ATCC 12,228 and Candida albicans (C. albicans) ATCC 10,231 were the highly affected bacterial and fungal strains with minimum inhibitory concentrations (MICs) of 18.75 and 50 µg/ml, respectively. Moreover, the noticeable effect of St/Ag-Se NC on microbial biofilm was concentration dependent. A high biofilm suppression percentage, 87.5% and 68.05%, were recorded with S. epidermidis and Staphylococcus aureus (S. aureus) when exposed to 1 mg/ml and 0.5 mg/ml, respectively. Conclusion The biosynthesized St/Ag-Se NC showed excellent antioxidant activity, haemocompatibility, and anti-proliferative effect at low concentrations. Also, it exhibited promising antimicrobial and antibiofilm activities.

Abstract Background Mycobacterium abscessus, a fast-growing non-tuberculous mycobacterium, is an emerging opportunistic pathogen responsible for chronic bronchopulmonary infections in people with respiratory diseases such as cystic fibrosis (CF). Due to its intrinsic polyresistance to a wide range of antibiotics, most treatments for M. abscessus pulmonary infections are poorly effective. In this context, antimicrobial peptides (AMPs) active against bacterial strains and less prompt to cause resistance, represent a good alternative to conventional antibiotics. Herein, we evaluated the effect of three arenicin isoforms, possessing two or four Cysteines involved in one (Ar-1, Ar-2) or two disulfide bonds (Ar-3), on the in vitro growth of M. abscessus. Methods The respective disulfide-free AMPs, were built by replacing the Cysteines with alpha-amino-n-butyric acid (Abu) residue. We evaluated the efficiency of the eight arenicin derivatives through their antimicrobial activity against M. abscessus strains, their cytotoxicity towards human cell lines, and their hemolytic activity on human erythrocytes. The mechanism of action of the Ar-1 peptide was further investigated through membrane permeabilization assay, electron microscopy, lipid insertion assay via surface pressure measurement, and the induction of resistance assay. Results Our results demonstrated that Ar-1 was the safest peptide with no toxicity towards human cells and no hemolytic activity, and the most active against M. abscessus growth. Ar-1 acts by insertion into mycobacterial lipids, resulting in a rapid membranolytic effect that kills M. abscessus without induction of resistance. Conclusion Overall, the present study emphasized Ar-1 as a potential new alternative to conventional antibiotics in the treatment of CF-associated bacterial infection related to M. abscessus.

Background and objectives: Microbial cells capability to tolerate the effect of various antimicrobial classes represent a major worldwide health concern. The flexible and multi-components nanocomposites have enhanced physicochemical characters with several improved properties. Thus, different biological activities of biosynthesized starch/silver-selenium nanocomposite (St/Ag-Se NC) were assessed. Methodology: The St/Ag-Se NC was biosynthesized using Cladosporium cladosporioides CBS 174.62 (C. cladosporioides) strain. The shape and average particle size were investigated using scanning electron microscope (SEM) and high-resolution transmission electron microscope (HR-TEM), respectively. On the other hand, the St/Ag-Se NC effect on two cancer cell lines and red blood cells (RBCs) was evaluated and its hydrogen peroxide (H2O2) scavenging effect was assessed. Moreover, its effects on various microbial species in both planktonic and biofilm growth forms were examined. Results: The St/Ag-Se NC was successfully biosynthesized with oval and spherical shape and a mean particle diameter of 67.87 nm as confirmed by the HR-TEM analysis. St/Ag-Se NC showed promising anticancer activity toward human colorectal carcinoma (HCT-116) and human breast cancer (MCF-7) cell lines where IC50 were 21.37 and 19.98 µg/ml, respectively. Similarly, little effect on RBCs was observed with low nanocomposite concentration. As well, the highest nanocomposite H2O2 scavenging activity (42.84%) was recorded at a concentration of 2 mg/ml. Additionally, Staphylococcus epidermidis (S. epidermidis) ATCC 12,228 and Candida albicans (C. albicans) ATCC 10,231 were the highly affected bacterial and fungal strains with minimum inhibitory concentrations (MICs) of 18.75 and 50 µg/ml, respectively. Moreover, the noticeable effect of St/Ag-Se NC on microbial biofilm was concentration dependent. A high biofilm suppression percentage, 87.5% and 68.05%, were recorded with S. epidermidis and Staphylococcus aureus (S. aureus) when exposed to 1 mg/ml and 0.5 mg/ml, respectively. Conclusion: The biosynthesized St/Ag-Se NC showed excellent antioxidant activity, haemocompatibility, and anti-proliferative effect at low concentrations. Also, it exhibited promising antimicrobial and antibiofilm activities. [ABSTRACT FROM AUTHOR]

The ESKAPE pathogen-associated antimicrobial resistance is a global public health issue, and novel therapeutic strategies are urgently needed. The short cationic antimicrobial peptide (AMP) family represents an important subfamily of scorpion-derived AMPs, but high hemolysis and poor antimicrobial activity hinder their therapeutic application. Here, we recomposed the hydrophilic face of Ctriporin through lysine substitution. We observed non-linear correlations between the physiochemical properties of the peptides and their activities, and significant deviations regarding the changes of antimicrobial activities against different bacterial species, as well as hemolytic activity. Most importantly, we obtained two Ctriporin analogs, CM5 and CM6, these two have significantly reduced hemolytic activity and more potent antimicrobial activities against all tested antibiotic-resistant ESKAPE pathogens. Fluorescence experiments indicated they may perform the bactericidal function through a membrane-lytic action model. Our work sheds light on the potential of CM5 and CM6 in developing novel antimicrobials and gives clues for optimizing peptides from the short cationic AMP family. [ABSTRACT FROM AUTHOR]

The selection of effective antibiotics is becoming increasingly limited due to the emergence of bacterial resistance. Designing and developing nanoscale antibacterials is a strategy for effectively addressing the antibiotic crisis. In this work, AgNPs@AMP nanoparticles were synthesized to take advantage of the synergistic antibacterial activity of the (LLRR)3 antimicrobial peptide (AMP) and silver nanoparticles (AgNPs). Based on morphological structure characterization and biocompatibility analysis, the inhibitory properties of AgNPs@AMP on Escherichia coli (E. coli) and Staphylococcus aureus (S. aureus) were evaluated. The results demonstrated that AMP and AgNPs were physically bound to form AgNPs@AMP nanoparticles, which had better solution stability, improved nanomaterial properties, and overcame the hemolytic activity of AMP and the cytotoxicity of AgNPs. The inhibitory activity of AgNPs@AMP against E. coli and S. aureus was significantly higher than that of AMP and AgNPs. It was capable of disrupting the morphology and internal structure of cells, damaging the cell membrane, and inhibiting the activity of enzymes related to the material-energy metabolism of the tricarboxylic acid cycle. Compared to AMP and AgNPs, AgNPs@AMP were found to effectively inhibit the infection of mouse wounds and promote their healing. Therefore, AMP-modified AgNPs can enhance their biocompatibility and antibacterial activity, and they can be further developed as a potential antimicrobial agent. [ABSTRACT FROM AUTHOR]

The toxicological impact of airborne polluting ultrafine particles (UFPs, also classified as nanoparticles with average sizes of less than 100 nm) is an emerging area of research pursuing a better understanding of the health hazards they pose to humans and other organisms. Hemolytic activity is a toxicity parameter that can be assessed quickly and easily to establish part of a nanoparticle's behavior once it reaches our circulatory system. However, it is exceedingly difficult to determine to what extent each of the nanoparticles present in the air is responsible for the detrimental effects exhibited. At the same time, current hemolytic assessment methodologies pose a series of limitations for the interpretation of results. An alternative is to synthesize nanoparticles that model selected typical types of UFPs in air pollution and evaluate their individual contributions to adverse health effects under a clinical assay of osmotic fragility. Here, we discuss evidence pointing out that the absence of hemolysis is not always a synonym for safety; exposure to model nanopollutants, even at low concentrations, is enough to increase erythrocyte susceptibility and dysfunction. A modified osmotic fragility assay in combination with a morphological inspection of the nanopollutant–erythrocyte interaction allows a richer interpretation of the exposure outcomes. Membrane–nanoparticle interplay has a leading role in the vulnerability observed. Therefore, future research in this line of work should pay special attention to the evaluation of the mechanisms that cause membrane damage. [ABSTRACT FROM AUTHOR]

A new composite material, ZnO/Yb2Zn-TiO6@g-C3N4 has been synthesized by simple hydrothermal process. This composite has been characterized using various material characterization techniques and was found to have a heterojunction amongst Yb2Zn-TiO6 and g-C3N4, leading to higher light absorption and poorer charge carrier recombination rates. Furthermore, the evaluation of the charge carrier density revealed that the incorporation of small sized ZnO (40 nm) into Yb2Zn-TiO6@g-C3N4 led to heightened disintegration of the photoinduced charge carriers. This observation implies that the presence of said metal oxide enhances the photocatalytic performance by greatly promoting the effective separation of charge carriers for various applications. When tested with bromothymol blue, the 20 wt% ZnO/Yb2Zn-TiO6@g-C3N4 composite showed a photodegradation rate several times greater (98 %) than individual ZnO, C3N4 and Yb2Zn-TiO6, respectively. The degradation efficiency of the ZnO/Yb2Zn-TiO6@g-C3N4 nanostructure in the absence of light was 24 %. The increased photoactivity of the composite material is due to the efficient separation of charge carriers and also due to the high redox capabilities resulting from the heterojunction. The composite also demonstrated stable photocatalytic performance over five cyclic runs and was effective in treating real printed ink wastewater. Furthermore, ZnO/Yb2Zn-TiO6@g-C3N4 was found to have excellent antibacterial properties in opposition to Escherichia coli, (Inhibition = 16(±0.2) mm) as well as Bacillus subtilis (Inhibition = 22(±0.3) mm). The MIC of the said nanomaterials against Escherichia coli as well as Bacillus subtilis were 50 µg/mL and 30 µg/mL respectively. The detailed explanation of the photodegradation mechanism was also provided. The use of this composite material can help to reduce the harmful effects of contaminants and microbes in aquatic environments and promote environmental sustainability.

Holothurians (or sea cucumbers) are echinoderms and are found in all areas of the world oceans. These animals produce special low-molecular metabolites - triterpene glycosides, which are a means of chemical protection of holothurians from predators. The content of triterpene glycosides in the tissues of holothurians can reach a significant amount of up to 1 g/kg, and especially many of these compounds are localized in the Cuvierian tubules - special protection organ presents in a number of tropical holothurians. Tritirepene glycosides of holothurians are quite toxic, they exhibit hemolytic, cytotoxic and neurotoxic activity at a concentration range of 1×104–1×106 M. The toxic properties of glycosides are based on the ability of these compounds to interact with ∆5-sterols (mainly cholesterol) of plasma membranes and form ion-conducting complexes. In turn, this leads to a change in the ion permeability and selectivity of biomembranes, disruption of barrier properties, ion homeostasis and osmolarity of cells, and further to cell lysis and death.Contact with holoturias when diving in shallow water, which is fraught with damage to the eyes and mucous membranes by triterpene glycosides, may be of some danger to humans. Excessive consumption of commercial edible holothurians in food, especially without prior heat treatment, as is customary in some South-East Asia countries, can lead to diarrhea and dyspepsia. Triterpene glycosides in the bloodstream can lead to blood lysis and serious consequences up to death.The holothurians are animals commercially harvested in Russia. They are used in food and for the preparation of medicinal supplements and preparations. Excessive consumption of commercial edible holothurians for food, especially without long-term boiling, as is customary in Southeast Asia, can lead to diarrhea and dyspepsia. Triterpene glycosides in the bloodstream can lead to blood lysis and serious consequences up to death. The use of dietary supplements with an uncontrolled glycoside content is fraught with similar consequences, and the presence of immunosuppressants among glycosides that have fallen into such additives and drugs can worsen the condition of patients or sick animals. Control of the qualitative and quantitative content of glycosides in food and medicinal products from holothurians should be an integral part of measures to improve the biological safety of citizens of the Russian Federation.

Abstract Amburana cearensis tree is used in various applications, from artisanal to pharmaceutical use. However, the gum extracted from its exudate has not yet been investigated. This study aimed to the physicochemical and structural characterization of Amburana cearensis Gum (AcG) by elemental, rheological, and thermal analyses, X-ray diffraction (XRD), high-Performance Liquid Chromatography (HPLC), Gel Permeation Chromatography (GPC), Infrared Spectroscopy (FTIR), UV-Vis spectroscopy and nuclear magnetic resonance (NMR). Additionally, a hemolytic assay was performed to evaluate the biocompatibility of AcG using human erythrocytes. The results showed that AcG consists of β-D-Galactopyranose monomers linked by glycosidic bonds (1→3). At the same time, the side chains exhibit β-Galactopyranose (1→6) and α-L-Arabinofuranoside (1→3,6) monomers as non-reducing terminals, whose biocompatibility was excellent in the model used. AcG was described for the first time as a biopolymer that could have broad applications in the pharmaceutical and cosmetic industries, justifying the interest in further studies about AcG applications.

The number of people affected by cancer and antibiotic-resistant bacterial infections has increased, such that both diseases are already seen as current and future leading causes of death globally. To address this issue, based on a combined in silico and in vitro approach, we explored the anticancer potential of known antibacterials with a thiazolidinedione–thiosemicarbazone (TZD–TSC) core structure. A cytotoxicity assessment showed encouraging results for compounds 2–4, with IC50 values against T98G and HepG2 cells in the low micromolar range. TZD–TSC 3 proved to be most toxic to cancer cell lines, with IC50 values of 2.97 ± 0.39 µM against human hepatoma HepG2 cells and IC50 values of 28.34 ± 2.21 µM against human glioblastoma T98G cells. Additionally, compound 3 induced apoptosis and showed no specific hemolytic activity. Furthermore, treatment using 3 on cancer cell lines alters these cells' morphology and further suppresses migratory activity. Molecular docking, in turn, suggests that 3 would have the capacity to simultaneously target HDACs and PPARγ, by the activation of PPARγ and the inhibition of both HDAC4 and HDAC8. Thus, the promising preliminary results obtained with TZD–TSC 3 represent an encouraging starting point for the rational design of novel chemotherapeutics with dual antibacterial and anticancer activities. [ABSTRACT FROM AUTHOR]

Numerous amphibian species, particularly those of the genus Rana, have been found to produce linear, amphiphilic, and cationic antimicrobial peptides (AMPs). Such AMPs are gaining more attention in pharmaceutical applications due to their principal method of action, which involves penetrating and rupturing the intended cell membranes with relatively low resistance. Brevinin is a large family of AMPs extensively studied during the last few decades, primarily consisting of two groups of peptides: Brevinin-1 and Brevinin-2. These peptides are cationic and establish secondary structures in the biological membrane environment. In this discussion, we explore the effects of structural parameters (net charge, hydrophobicity, amphiphilicity, helicity, peptide length, etc.) of Brevinin on their antimicrobial activity. As a general rule, an increased net charge tends to enhance antimicrobial activity. However, it is important to note that excessive net charges can also elevate hemolytic activity. The amino acid composition significantly influences hydrophobicity and helicity, which, in turn, impact the activity of the peptides. Moreover, these structural parameters are interconnected; modifying one parameter will affect others. Striking an optimal balance in these factors will provide a Brevinin analog with the highest antimicrobial activity and the lowest hemolytic activity. [ABSTRACT FROM AUTHOR]

The creation of mitochondria-targeted vector systems is a new tool for the treatment of socially significant diseases. Phosphonium groups provide targeted delivery of drugs through biological barriers to organelles. For this purpose, a new class of alkyl(diethylAmino)(Phenyl) Phosphonium halides (APPs) containing one, two, or three diethylamino groups was obtained by the reaction of alkyl iodides (bromides) with (diethylamino)(phenyl)phosphines under mild conditions (20 °C) and high yields (93–98%). The structure of APP was established by NMR and XRD. A high in vitro cytotoxicity of APPs against M-HeLa, HuTu 80, PC3, DU-145, PANC-1, and MCF-7 lines was found. The selectivity index is in the range of 0.06–4.0 μM (SI 17-277) for the most active APPs. The effect of APPs on cancer cells is characterized by hyperproduction of ROS and depolarization of the mitochondrial membrane. APPs induce apoptosis, proceeding along the mitochondrial pathway. Incorporation of APPs into lipid systems (liposomes and solid lipid nanoparticles) improves cytotoxicity toward tumor cells and decrease toxicity against normal cell lines. The IC50s of lipid systems are lower than for the reference drug DOX, with a high SI (30–56) toward MCF-7 and DU-145. APPs exhibit high selective activity against Gram-positive bacteria S. aureus 209P and B. segeus 8035, including methicillin-resistant S. aureus (MRSA-1, MRSA-2), comparable to the activity of the fluoroquinolone antibiotic norfloxacin. A moderate in vivo toxicity in CD-1 mice was established for the lead APP. [ABSTRACT FROM AUTHOR]

Biologically active peptides have attracted increasing attention in research on the development of new drugs. Mastoparans, a group of wasp venom linear cationic α-helical peptides, have a variety of biological effects, including mast cell degranulation, activation of protein G, and antimicrobial and anticancer activities. However, the potential hemolytic activity of cationic α-helical peptides greatly limits the clinical applications of mastoparans. Here, we systematically and comprehensively studied the hemolytic activity of mastoparans based on our wasp venom mastoparan family peptide library. The results showed that among 55 mastoparans, 18 had strong hemolytic activity (EC50 ≤ 100 μM), 14 had modest hemolytic activity (100 μM < EC50 ≤ 400 μM) and 23 had little hemolytic activity (EC50 > 400 μM), suggesting functional variation in the molecular diversity of mastoparan family peptides from wasp venom. Based on these data, structure–function relationships were further explored, and, hydrophobicity, but not net charge and amphiphilicity, was found to play a critical role in the hemolytic activity of mastoparans. Combining the reported antimicrobial activity with the present hemolytic activity data, we found that four mastoparan peptides, Parapolybia-MP, Mastoparan-like peptide 12b, Dominulin A and Dominulin B, have promise for applications because of their high antimicrobial activity (MIC ≤ 10 μM) and low hemolytic activity (EC50 ≥ 400 μM). Our research not only identified new leads for the antimicrobial application of mastoparans but also provided a large chemical space to support the molecular design and optimization of mastoparan family peptides with low hemolytic activity regardless of net charge or amphiphilicity. [ABSTRACT FROM AUTHOR]

Piperazine is a privileged moiety that is a structural part of many clinical drugs. Piperazine-based scaffolds have attracted the attention of pharmaceutical and medicinal scientists to develop novel, efficient therapeutic agents owing to their significant and promising biological profile. In the current study, an ecofriendly ultrasonic-assisted synthetic approach was applied to achieve a novel series of 1-tosyl piperazine dithiocarbamate acetamide hybrids 4a–4j, which was evaluated for in vitro tyrosinase inhibition and thrombolytic and hemolytic cytotoxic activities. Among all the piperazine-based dithiocarbamate acetamide target molecules 4a–4j, the structural analogs 4d displayed excellent tyrosinase inhibition efficacy (IC50 = 6.88 ± 0.11 µM) which was better than the reference standard drugs kojic acid (30.34 ± 0.75 µM) and ascorbic acid (11.5 ± 1.00 µM), respectively, which was further confirmed by in silico induced-fit docking (IFD) simulation Good tyrosinase activities were exhibited by 4g (IC50 = 7.24 ± 0.15 µM), 4b (IC50 = 8.01 ± 0.11 µM) and 4c (IC50 = 8.1 ± 0.30 µM) dithiocarbamate acetamides, which were also better tyrosinase inhibitors than the reference drugs but were less active than the 4d structural hybrid. All the derivatives are less toxic, having values in the 0.29 ± 0.01% to 15.6 ± 0.5% range. The scaffold 4b demonstrated better hemolytic potential (0.29 ± 0.01%), while a remarkably high thrombolytic chemotherapeutic potential was displayed by analog 4e (67.3 ± 0.2%). [ABSTRACT FROM AUTHOR]

The increasing global focus on green nanotechnology research has spurred the development of environmentally and biologically safe applications for various nanomaterials. Nanotechnology involves crafting diverse nanoparticles in terms of shapes and sizes, with a particular emphasis on environmentally friendly synthesis routes. Among these, biogenic approaches, including plant-based synthesis, are favored for their safety, simplicity, and sustainability. Silver nanoparticles, in particular, have garnered significant attention due to their exceptional effectiveness, biocompatibility, and eco-friendliness. Cannabis (Cannabis sativa L.) has emerged as a promising candidate for aiding in the green synthesis of silver nanoparticles. Leveraging the phytochemical constituents of Cannabis, researchers have successfully tailored silver nanoparticles for a wide array of applications, spanning from biomedicine to environmental remediation. This review explores the properties, synthesis mechanisms, and applications of silver nanoparticles obtained from Cannabis. Additionally, it delves into the recent advancements in green synthesis techniques and elucidates the optical properties of these nanoparticles. By shedding light on plant-based fabrication methods for silver nanoparticles and their diverse bionanotechnology applications, this review aims to contribute to the growing body of knowledge in the field of green nanotechnology. Through a comprehensive examination of the synthesis processes, mechanistic aspects, and potential applications, this review underscores the importance of sustainable approaches in nanoparticle synthesis and highlights the potential of Cannabis-derived silver nanoparticles in addressing various societal and environmental challenges.

The combination scattering spectroscopy method investigated strains of the epidermal staphylococcus with hemolytic activity and without hemolytic activity. The main spectral differences of the studied groups are established. Complex analysis was used to estimate hemolytic activity using combined scattering (SR) spectroscopy and mathematical approaches. [ABSTRACT FROM AUTHOR]

Summary: Phaeocystis globosa frequently proliferates in eutrophic waters and forms ichthyotoxic algal blooms that cause massive fish mortalities in marine ecosystems. One of the ichthyotoxic metabolites was identified as the glycolipid‐like hemolytic toxin, reported to be initiated under light conditions. However, the association between hemolytic activity (HA) and photosynthesis of P. globosa remained unclear.Light spectra (blue, red, green, and white) and 3‐(3,4‐dichlorophenyl)‐1,1‐dimethylurea (DCMU) were selected as the stressors to stimulate the hemolytic response of P. globosa in relation to the light and dark photosynthesis reaction.Hemolytic activity in P. globosa was sensitive to the light spectrum as it decreased from 93% to nearly undetectable (1.6%) within 10 min of transfer from red (630 nm) to green light (520 nm). This indicates that the vertical transformation of P. globosa from deep to surface waters (dominated by green light and all light spectra, respectively) may drive the hemolytic response in coastal waters. However, regulation of photosynthetic electron transfer in the light reaction of P. globosa was excluded by the evidence of inconsistent response of HA to photosynthetic activity.The biosynthesis of HA may interfere with the pathway of photopigments diadinoxanthin or fucoxanthin, and the metabolism of three‐ and five‐carbon sugars (GAP and Ru5P, respectively), which ultimately lead to changes in the alga's hemolytic carbohydrate metabolism. [ABSTRACT FROM AUTHOR]

The antimicrobial activity of SJGAP (skipjack tuna GAPDH-related antimicrobial peptide) and four chemical analogs thereof was determined under different physicochemical conditions, including different pH values, the presence of monovalent and divalent cations, and after a heating treatment. The toxicity of these five peptides was also studied with hemolytic activity assays, while their stability under human gastrointestinal conditions was evaluated using a dynamic in vitro digestion model and chromatographic and mass spectrometric analyses. The antibacterial activity of all analogs was found to be inhibited by the presence of divalent cations, while monovalent cations had a much less pronounced impact, even promoting the activity of the native SJGAP. The peptides were also more active at acidic pH values, but they did not all show the same stability following a heat treatment. SJGAP and its analogs did not show significant hemolytic activity (except for one of the analogs at a concentration equivalent to 64 times that of its minimum inhibitory concentration), and the two analogs whose digestibility was studied degraded very rapidly once they entered the stomach compartment of the digestion model. This study highlights for the first time the characteristics of antimicrobial peptides from Scombridae or homologous to GAPDH that are directly related to their potential clinical or food applications. [ABSTRACT FROM AUTHOR]

Magnetic Beta zeolite was synthesized under hydrothermal conditions by doping aluminosilicate gel with magnetite nanoparticles. The strength of Fe3O4 nanoparticle fixation in the composite synthesized under hydrothermal conditions was evaluated in comparison with the samples prepared by coprecipitation. The efficiency of the adsorption and desorption of 5-fluorouracil antitumor drug on samples of Beta zeolite and Beta–Fe3O4 magnetic nanocomposite was studied. The kinetics of the 5-fluorouracil release from the composite was described using the Higuchi model. The physicochemical properties of the samples were characterized. The hemolytic activity of the initial Beta zeolite and magnetic composite based on it toward human blood cells and the ability for biodegradation in a synthetic biological medium were studied with the aim of ensuring safe use of the materials as drug carriers. The results of the study allow conclusions on the possibility of using the magnetic nanocomposites in vivo. [ABSTRACT FROM AUTHOR]

The study investigates the physicochemical, porous/textural, and adsorptive properties, as well as the biological activity of BEA, RHO, PAU, and FAU(Y) synthetic zeolites. The adsorption capacity of the zeolites for oxytocin, lysozyme, and albumin—markers of low- and medium-molecular-weight pathological proteins—was measured. The concentration-dependent effects of the zeolites on the viability of human endothelial cells (Ea.hy926) were evaluated. At concentrations of 2.5 to 10 mg/mL, the Y zeolite was found to exhibit no pronounced cytotoxicity. In the presence of the BEA, the cell viability decreased to 80% even at 2.5 mg/mL. The RHO and PAU were shown to have the highest cytotoxicity and significantly inhibit the growth of human cells (down to 23–35%). The study demonstrated that only BEA and Y, among the synthetic zeolites tested, have good biomedical potential due to their high adsorption capacity, low hemolytic activity, and low cytotoxicity. [ABSTRACT FROM AUTHOR]

The ubiquity of pathogenic E. coli isolate possessing antimicrobial resistance was investigated in seafood samples procured from major seafood supply chain markets established for export and domestic consumption along Tuticorin coast. Out of 63 seafood samples examined, 29 (46%) were found to be contaminated by pathogenic E. coli harbouring one or more genes of virulent potential. Based on virulome profiling, 9.55% of isolates belonged to enterotoxigenic E. coli (ETEC), 8.08% to enteroaggregative E. coli (EAEC), 7.35% to enterohemorrhagic E. coli (EHEC), 2.20% to enteropathogenic E. coli (EPEC), and 2.20% to uropathogenic E. coli (UPEC). All the 34 virulome positive and haemolytic pathogenic E. coli have been serogrouped as O119, O76, O18, O134, O149, O120, O114, O25, O55, O127, O6, O78, O83, O17 and clinically significant O111, O121, O84, O26, O103, and O104 (non-O157 STEC) serotypes in this study. Multi-drug resistance (MDR) (≥ 3 antibiotic classes/sub-classes) was exhibited in 38.23% of the pathogenic E. coli, and 17.64% were extensive drug resistant (XDR). Extended spectrum of β-lactamase (ESBL) genotypes were confirmed in 32.35% isolates and 20.63% isolates harboured ampC gene. One sample (Penaeus semisulcatus) collected from landing centre (L1) harboured all ESBL genotypes blaCTX-M, blaSHV, blaTEM, and ampC genes. Hierarchical clustering of isolates revealed the separation of ESBL isolates into three clusters and non-ESBL isolates into three clusters based on phenotypic and genotypic variations. Based on dendrogram analysis on antibiotic efficacy pattern, carbapenems and β-lactam inhibitor drugs are the best available treatment for ESBL and non-ESBL infections. This study emphasizes the significance of comprehensive surveillance of pathogenic E. coli serogroups that pose serious threat to public health and compliance of AMR antimicrobial resistant genes in seafood that hinder seafood supply chain. [ABSTRACT FROM AUTHOR]