High Inhibitory Capacity Research Articles

Design and synthesis of cyclic lipidated peptides derived from the C-terminus of Cx43 for hemichannel inhibition and cardiac endothelium targeting.

A peptide segment that is 10 residues long at the C-terminal (CT) region of Cx43 is known to be involved in interactions, both with the Cx43 protein itself and with other proteins, that result in hemichannel (HC) activity regulation. Previously reported mimetic peptides based on this region (e.g., αCT1, CT10) have been revealed to be promising therapeutic agents in the context of cardiovascular diseases. In this work, novel approaches, such as C- and N-terminal modification and cyclization, to improve the proteolytic stability and bioavailability of the CT10 peptide are presented. These efforts resulted in a set of unprecedented potent cyclic inhibitors of HC-mediated ATP release with a half-life largely exceeding 24 hours. Additionally, the introduction of a lipophilic moiety with different solubilizing linkers led to the generation of a novel series of water-soluble and lipidated peptides that exhibited high inhibitory capacity in in vitro assays at submicromolar concentrations. A cardiac endothelium targeting strategy was also adopted, exploiting the ability of the CRPPR peptide to selectively deliver the peptides to endothelial cells.

Evaluation of Boerhavia diffusa and Eichhornia crassipes plant extracts in vitro as potential antifungal agents against human pathogenic fungi Candida albician and Candida tropicalis : A comparative study

Plant extracts are used to make herbal remedies with no side effects and little expense. During the COVID-19 pandemic, fungal species responsible for mucormycosis were found resistant to a variety of antifungals, including flucytosine, ketoconazole, fluconazole, voriconazole, itraconazole and echinocandins, due to their variable susceptibility. Amphotericin B is widely used as an antifungal agent due to its high inhibition capacity against various fungi. The present study aimed to compare the antifungal potential of Amphotericin B and herbal extract in vitro. The experiment was designed to measure zones of inhibition with the help of well-diffusion method. Four solvents, viz. methanol, chloroform, hexane and distilled water, were used to extract plant extract. The efficiency of plant extracts was found to be low compared to Amphotericin B (1.4mm). Chloroform extract of Boerhavia diffusa was found antifungal against Candida albician and C. tropicalis (0.45mm). Methanol and hexane extract of Eichhornia crassipes showed higher antifungal activity (1.35mm) and (1.75mm), respectively. The plant extracts also showed significant antifungal activity against C. tropicalis, revealing its potential to be used as a natural antifungal agent (1.1mm). Additionally, the findings showed that the chloroform and methanol extracts of B. diffusa and E. crassipes were also efficient against C. albician and C. tropicalis. The findings provide important insights about using plant extracts as a potential alternative to conventional antifungal agents.

Malvidin and Its Mono- and Di-Glucosides Forms: A Study of Combining Both In Vitro and Molecular Docking Studies Focused on Cholinesterase, Butyrylcholinesterase, COX-1 and COX-2 Activities

Malvidin, one of the six most prominent anthocyanins found in various fruits and vegetables, may possess a wide range of health-promoting properties. The biological activity of malvidin and its glycosides is not entirely clear and has been relatively less frequently studied compared to other anthocyanins. Therefore, this study aimed to determine the relationship between the structural derivatives of malvidin and their anti-cholinergic and anti-inflammatory activity. The study selected malvidin (Mv) and its two sugar derivatives: malvidin 3-O-glucoside (Mv 3-glc) and malvidin 3,5-O-diglucoside (Mv 3,5-diglc). The anti-inflammatory activity was assessed by inhibiting the enzymes, specifically COX-1 and COX-2. Additionally, the inhibitory effects on cholinesterase activity, particularly acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), were evaluated. Molecular modeling was also employed to examine and visualize the interactions between enzymes and anthocyanins. The results revealed that the highest inhibitory capacity at concentration 100 µM was demonstrated by Mv 3-glc in relation to AChE (26.3 ± 3.1%) and BChE (22.1 ± 3.0%), highlighting the crucial role of the glycoside substituent at the C3 position of the C ring in determining the inhibitory efficiency of these enzymes. In addition, the glycosylation of malvidin significantly reduced the anti-inflammatory activity of these derivatives compared to the aglycone form. The IC50 parameter demonstrates the following relationship for the COX-1 enzyme: Mv (12.45 ± 0.70 µM) < Mv 3-glc (74.78 ± 0.06 µM) < Mv 3,5-diglc (90.36 ± 1.92 µM). Similarly, for the COX-2 enzyme, we have: Mv (2.76 ± 0.16 µM) < Mv 3-glc (39.92 ± 3.02 µM) < Mv 3.5-diglc (66.45 ± 1.93 µM). All tested forms of malvidin exhibited higher activity towards COX-2 compared to COX-1, indicating their selectivity as inhibitors of COX-2. Theoretical calculations were capable of qualitatively replicating most of the noted patterns in the experimental data, explaining the impact of deprotonation and glycosylation on inhibitory activity. It can be suggested that anthocyanins, such as malvidins, could be valuable in the development of treatments for inflammatory conditions and Alzheimer’s disease and deserve further study.

The Influence of Aging on the Structure and Properties of Composite Materials Based on Polyurethane and Silver Nanoparticles

The aging processes and their influence on structure, thermophysical and antimicrobial properties of polymer nanocomposites based on segmented polyurethane and silver nanoparticles were studied. It was established that an increase in the intensity of intermolecular interactions of polyurethane occurred regardless of the concentration of silver in the silver nanoparticles due to a change in the packing of macromolecules. It was shown that in the process of aging of composites, the effective size of crystallites of polymer matrix decreases and varies in the range of 1.35–1.50 nm. The most pronounced effect of aging is manifested on the melting temperatures of the crystalline phase of polyurethane and the degree of crystallinity. It was found that polyurethane–silver nanoparticle composites exhibit a very high inhibitory capacity against Staphylococcus aureus, Escherichia coli, and Candida albicans. It is shown that aging processes do not affect the antimicrobial characteristics of the studied materials, which indicates their stability. Due to their unique characteristics, synthesized nanocomposite films can be promising for use as antimicrobial coatings in various applications.

Identification of Polyphenols in Sea Fennel (Crithmum maritimum) and Seaside Arrowgrass (Triglochin maritima) Extracts with Antioxidant, ACE-I, DPP-IV and PEP-Inhibitory Capacity.

Sea fennel and seaside arrowgrass are two abundant but underutilized halophytes along the Atlantic and Mediterranean coasts. This study investigated the antioxidant capacity and the potential antihypertensive (Angiotensin Converting Enzyme I, ACE-I inhibition), hypoglycaemic (Dipeptidyl Peptidase IV, DPP-IV inhibition), and nootropic (Prolyl Endopeptidase, PEP inhibition) activity of their polyphenol extracts. They had a high phenol content (21-24 mEq GA/g), antioxidant capacity evaluated using the ABTS (17-2 mg ascorbic acid/g) and FRAP (170-270 mM Mohr's salt/g) assays, and effective ACE-inhibiting properties (80-90% inhibiting activity at final concentration of 0.5 mg/mL). Additionally, the sea fennel extract displayed high DPP-IV inhibitory capacity (73% at 1 mg/mL), while the seaside arrowgrass extract exhibited potent Prolyl endopeptidase inhibitory capacity (75% at 1 mg/mL). Fractionation by HPLC concentrated the bioactive molecules in two fractions, for which the composition was analyzed by LC-MS/MS. Different chlorogenic acids seemed to play an important role in the bioactivity of sea fennel extract, and different flavonoids, mainly apigenin, luteolin and chrysoeriol, in the bioactivity of the seaside arrowgrass extract. Given their potential health benefits, these extracts could serve as valuable bioactive ingredients and could potentially encourage the cultivation of these species in regions where traditional crops face challenges in growth.

Differences in the Proteolytic System of Lactic Acid Bacteria Affect the Release of DPP-IV Inhibitory Peptides from Whey Proteins

This work analyzed the antidiabetic activity of peptides from whey proteins after hydrolysis by Lactobacillus rhamnosus GG and Streptococcus thermophilus SY-102, emphasizing the differences between the proteolytic systems of both bacteria. Peptide fractions from whey proteins may have biological functions, such as antidiabetic functions, which inhibit the DPP-IV enzyme, and lactic acid bacteria could release them. A whey solution of 10% was fermented with selected lactic acid bacteria in monoculture and coculture, analyzing kinetic parameters and the proteolytic profile, using the 2,4,6-trinitrobenzene sulfonic acid technique for free amino groups’ determination and Tris-tricine polyacrylamide gel electrophoresis. An in vitro inhibition assay of the DPP-IV enzyme was used. The kinetic parameters showed a faster duplication rate in the monoculture with L. rhamnosus GG than in the co-culture, which was related to lactic acid production. Co-culture does not have the highest production of free amino groups and peptides. Still, peptide fractions with lower molecular weight (<2 kDa) were found and showed a high DPP-IV inhibitory capacity that was maintained from the middle of the fermentation to the end (55.4%). In comparison, the monoculture of L. rhamnosus GG increased from 0 to 63.3%. This demonstrates that the proteolytic capacity and the proteolytic system of each lactic acid bacteria determine the structure of the released peptides.

Characterization and genomic analysis of a broad-spectrum lytic phage HZ2201 and its antibiofilm efficacy against Pseudomonas aeruginosa

Pseudomonas aeruginosa is a clinically common conditionally pathogenic bacterium, and the abuse of antibiotics has exacerbated its drug resistance in recent years. This has resulted in extensive reports about the usage of Pseudomonas aeruginosa phage as a novel antibacterial drug. In this study, we isolated a novel phage HZ2201 with a broad lytic spectrum. The lytic rate of this phage against Pseudomonas aeruginosa reached 78.38% (29/37), including 25 multi-drug- and carbapenem-resistant Pseudomonas aeruginosa strains. Transmission electron microscopy revealed that phage HZ2201 belongs to the class Caudoviricetes. Biological characterization showed that phage HZ2201 had an latent period of 40 min, a lytic period of 20 min, and a burst size of 440 PFU/cell, with improved tolerance to temperature and pH. Considering genomic analysis, the HZ2201 genome was a circular double-stranded DNA with a size of 45,431 bp and a guanine-cytosine (G + C) content of 52.16%, and contained 3 tRNAs. 27 of the 74 open reading frames (ORFs) annotated by the Rapid Annotation using Subsystem Technology (RAST) tool could be matched to the genomes of known functions, and no genes related to virulence and antibiotic resistance were found. The phylogenetic tree suggests that phage HZ2201 is highly related to the phage ZCPS1 and PaP3, and ORF57 and ORF17 are predicted to encode a holin and an endolysin, respectively. Cell lysis by HZ2201 proceeds through the holin-endolysin system, suggesting that it is a novel phage. Additionally, we demonstrated that phage HZ2201 has a high inhibitory capacity against Pseudomonas aeruginosa biofilms. The results of our study suggest that phage HZ2201 is a novel potential antimicrobial agent for treating drug-resistant Pseudomonas aeruginosa infection.

Computational design of quinoxaline molecules as VEGFR-2 inhibitors: QSAR modelling, pharmacokinetics, molecular docking, and dynamics simulation studies

Cancer is a deadly condition characterized by accelerated cell proliferation. According to the World Health Organization, global cancer cases are projected to reach 22 million by 2030. Therefore, the relentless search for safer and more effective anticancer drugs remains an imperative direction in the research and progression of drugs targeting cancer. This work utilized a ligand-based approach to designing more effective quinoxaline derivatives for the VEGFR-2 enzyme, an important protein in the pathogenesis of breast cancer. To accomplish this task, a statistically validated QSAR model was built using quinoxaline derivatives. The developed model was used for the virtual screening of the quinoxaline derivatives, from which compound 8 with a high inhibitory capacity (pIC50 = 5.357) was selected as the design template from which five hypothetical molecules with better VEGFR-2 inhibitory capacities ranging from pIC50 = 5.43 to 6.16 were designed. Docking studies were performed with the designed molecules as ligands and the VEGFR-2 active site residues, and they were found to have docking scores ranging from −171.384 to −182.241 kcal/mol, which outperformed the template ligand with a score of −170.579 kcal/mol. MD simulation predicted a stable docked complex and that the ligands did not leave the VEGFR-2 active site over the course of 200ns simulation. The designed quinoxaline molecules exhibit drug-like and desired ADMET parameters, as revealed by the outcomes of drug-likeness and pharmacological profiling. Hence, this research could be significant in unearthing novel breast cancer-targeting molecules.

Phenolic compounds, antioxidant capacity, and α-amylase and α-glucosidase inhibitory activity of ethanol extracts of perilla seed meal.

Perilla frutescens is a medicinal herb that is commonly cultivated in Asian countries. Perilla seed is extensively pressed for cooking oil extraction. However, phenolic chemicals are still abundant in pressed perilla seed meal (PSM), which was previously thought to be useless after oil extraction. In our study, PSM was extracted using five solvents (water and 25%, 50%, 75%, and 100% ethanol) based on different ethanol concentrations, and its antioxidant activity, phenolic compounds, and inhibitory effects against key enzymes related to diabetes mellitus were evaluated. The 75% ethanol extract had higher phenolic (105.58 mg GAE/g DW) and flavonoid (66.52 mg QE/g DW) contents and showed better antioxidant and inhibitory effects against α-glucosidase and α-amylase. Analysis of the phenolic compounds of the five extracts by HPLC indicated the presence of apigenin, rosmarinic acid, benzoic acid, caffeic acid, and vanillic acid. Therefore, because of its high antioxidant activity and inhibitory capacity against enzymes relevant to diabetes, the 75% ethanol extract of perilla seed meal has the most potential to be used as a functional or nutraceutical food in the prevention and treatment of oxidation and diabetes.

Efficacy of a Novel Antibacterial Agent Exeporfinium Chloride, (XF-73), Against Antibiotic-Resistant Bacteria in Mouse Superficial Skin Infection Models.

The number of incidences of antimicrobial resistance is rising continually, necessitating new and effective antibacterial drugs. The present study aimed to assess the in vitro and in vivo activity of XF-73 against antibiotic-resistant Staphylococcus aureus (S. aureus) isolates and to investigate the potential mechanism of action of XF-73. The in vitro antibacterial activity of XF-73 and comparator antibacterial drugs, (mupirocin, fusidine, retapamulin, vancomycin, erythromycin, linezolid and daptomycin), against S. aureus (both antibiotic sensitive and resistant strains) was assessed using a broth microdilution method. Two different superficial Staphylococcal skin infection murine models were established to study the in vivo efficacy of XF-73 against antibiotic-resistant strains. The effect of XF-73 on the ultrastructure and cellular morphology of S. aureus was studied using transmission electron microscopy (TEM) and scanning electron microscopy (SEM). The MICs (minimum inhibitory concentration) determined by the broth microdilution method for XF-73 demonstrated that the compound had a high potency against S. aureus isolates with varying susceptibility to the study drugs. Also, the antibacterial activity of XF-73 was superior or similar to most of the tested antibacterial drugs. We also found that the XF-73 dermal formulation significantly inhibited S. aureus survival in both the murine skin tape-stripping and suture superficial skin infection models, maintained a consistently high inhibitory capacity against the antibiotic-resistant strains tested and was significantly more effective than mupirocin ointment, a commonly used antibiotic for the treatment of skin infections. The morphological studies using TEM suggest that XF-73 had a rapid (2 minute) bacterial cell wall disruption activity, with longer incubation (10 minute) subsequently causing membrane damage. SEM analysis demonstrated that this cell wall and cell membrane disruption did not lead to disintegration of the plasma membrane, and did not cause bacterial cell lysis. Therefore, XF-73 may be an effective drug alternative to combat multi-drug-resistant skin infections in the clinical setting.

Evaluation of the fungicidal activity of the aqueous extracts of some medicinal plants against Fusarium spp

To assess the performance of the aqueous extracts of Rhus coriaria, Boswellia carterii, Nigella sativa and Aloe vera. Three concentrations (5%, 10%, and 15%) for each extract were tested in vitro for their activity against three isolates of Fusarium spp. All extracts have a high inhibitory capacity against tested isolates. An inhibition percentage for selected isolates was increased with concentrations (5%, 10%, 15%). The concentration of Rhus coriaria extract 15 % resulted in a significant increase in inhibition percentage of mycelial growth of Fusarium sp.1 (63.17%), Fusarium sp2 (61.69%) and Fusarium sp3 (59.35%) compared to other concentrations, the concentration of Boswellia carterii extract 10% led to a significant increase in inhibition percentage of mycelial growth of Fusarium sp2 (82.45 %) compared to concentration 5% (73.67 %), the concentration of Nigella sativa extract 15% was recorded high inhibition percentage in Fusarium sp2 (66.15 %) compared to concentration 5% (22.21%). In contrast, concentrations 5% and 10% were recorded highest inhibition percentages in Fusarium sp3, reaching 31.73 % and 22.02%, respectively, compared to concentration 15% (4.90%). Keywords: Rhus coriaria, Boswellia carterii, Nigella sativa, Aloe vera and Fusarium spp

Inhibition of the extracellular enzyme A disintegrin and metalloprotease with thrombospondin motif 4 prevents cardiac fibrosis and dysfunction.

Heart failure is a condition with high mortality rates, and there is a lack of therapies that directly target maladaptive changes in the extracellular matrix (ECM), such as fibrosis. We investigated whether the ECM enzyme known as A disintegrin and metalloprotease with thrombospondin motif (ADAMTS) 4 might serve as a therapeutic target in treatment of heart failure and cardiac fibrosis. The effects of pharmacological ADAMTS4 inhibition on cardiac function and fibrosis were examined in rats exposed to cardiac pressure overload. Disease mechanisms affected by the treatment were identified based on changes in the myocardial transcriptome. Following aortic banding, rats receiving an ADAMTS inhibitor, with high inhibitory capacity for ADAMTS4, showed substantially better cardiac function than vehicle-treated rats, including ∼30% reduction in E/e' and left atrial diameter, indicating an improvement in diastolic function. ADAMTS inhibition also resulted in a marked reduction in myocardial collagen content and a down-regulation of transforming growth factor (TGF)-β target genes. The mechanism for the beneficial effects of ADAMTS inhibition was further studied in cultured human cardiac fibroblasts producing mature ECM. ADAMTS4 caused a 50% increase in the TGF-β levels in the medium. Simultaneously, ADAMTS4 elicited a not previously known cleavage of TGF-β-binding proteins, i.e. latent-binding protein of TGF-β and extra domain A-fibronectin. These effects were abolished by the ADAMTS inhibitor. In failing human hearts, we observed a marked increase in ADAMTS4 expression and cleavage activity. Inhibition of ADAMTS4 improves cardiac function and reduces collagen accumulation in rats with cardiac pressure overload, possibly through a not previously known cleavage of molecules that control TGF-β availability. Targeting ADAMTS4 may serve as a novel strategy in heart failure treatment, in particular, in heart failure with fibrosis and diastolic dysfunction.

Smart collagen/xanthan gum-based hydrogels with antibacterial effect, drug release capacity and excellent performance in vitro bioactivity for wound healing application

The design of hydrogels based on natural polymers that have modulation of antibacterial capacity, ideal performance in release capacity of encapsulated drugs, and desired bioactivity for applications in wound healing represents a modern trend in biomaterials. In this work, novel hydrogels of semi-interpenetrating polymeric networks based on collagen and xanthan gum (XG) were investigated. The linear chains of XG can semi-interpenetrate inside to matrix of crosslinked collagen with polyurethane under physiological conditions, generating amorphous surfaces with fibrillar-granular reliefs that have accelerated gelation time (about 15 min), super water absorption (up to 3100%) and high inhibition capacity of pathogenic bacteria such as Escherichia coli (up to 100% compared to amoxicillin at 20 ppm). The increment of XG in the hydrogel (up to 20 wt.%) allows for improvement in the storage module, resistance to thermal degradation, slow the rate of hydrolytic and proteolytic degradation, allowing to encapsulate and controlled release of molecules such as ketorolac and methylene blue; besides, it shows to keep the metabolic activity of fibroblasts and monocytes at 48 h of evaluation, without observing cytotoxic effects. The bioactivity of these hydrogels is improved since they have excellent hemocompatibility and enhanced cell proliferation. Specifically, the hydrogel with 20 wt.% of XG shows to decrease the production of tumor necrosis factor-α and CCL-2 cytokines, increasing the production of transforming growth factor-β in human monocytes, which could be used to modulate inflammation and regenerative capacity in wound healing strategies.

Characterization of the phytochemical content, antioxidant activity and inhibition capacity against α-glucosidase of different flower parts of seven lotuses (Nelumbo)

In an era that highly emphasizes health and eating art, consumption of edible flowers, such as lotus, with pretty appearance and high nutritive quality is becoming increasingly attractive. Therefore, this study assessed the three flower parts, receptacle, stamen and petal of 7 different lotuses for their nutritional qualities, in terms of total polyphenol content (TPC), flavonol content and constituent, antioxidant activity and inhibition capacity against α-glucosidase. The results showed that the antioxidant activity of each plant part was significantly correlated with TPC. The receptacle of ‘Yijian Lian’ (Nelumbo) had the highest TPC, the highest antioxidant activity and a very high inhibition capacity against α-glucosidase. The receptacle of ‘Bianlian’ (Nelumbo) had the highest inhibition capacity against α-glucosidase. 14 flavonols were identified in all 7 lotus flowers. The American lotus contained the highest flavonol levels in any of the three flower parts compared to the others. Our characterization of these different lotuses provides valuable insights and resources which may accelerate the development of food or medicine from lotus flowers.

The Effect of Ginger (Zingiber officinale Roscoe) Aqueous Extract on Postprandial Glycemia in Nondiabetic Adults: A Randomized Controlled Trial.

Ginger has shown beneficial effects on blood glucose control due to its antioxidant and anti-inflammatory properties. The present study investigated the effect of ginger aqueous extract on postprandial glucose levels in nondiabetic adults and characterized its antioxidant activity. Twenty-four nondiabetic participants were randomly assigned into two groups (NCT05152745), the intervention group (n = 12) and the control group (n = 12). Both groups were administered 200 mL of an oral glucose tolerance test (OGTT), after which participants in the intervention group ingested 100 mL of ginger extract (0.2 g/100 mL). Postprandial blood glucose was measured while fasting and after 30, 60, 90, and 120 min. The total phenolic content, flavonoid content, and antioxidant activity of ginger extract were quantified. In the intervention group, the incremental area under the curve for glucose levels decreased significantly (p < 0.001) and the maximum glucose concentration significantly reduced (p < 0.001). The extract possessed a polyphenolic content of 13.85 mg gallic acid equivalent/L, a flavonoid content of 3.35 mg quercetin equivalent/L, and a high superoxide radical inhibitory capacity (45.73%). This study showed that ginger has a beneficial effect on glucose homeostasis under acute conditions and encourages the use of ginger extract as a promising source of natural antioxidants.

Effect of the content of starch on the biocompatibility, bacterial inhibition, and drug release performance of semi-IPN collagen-polyurethane hydrogels

This work studied the effect of content of starch on the structure and properties of hydrogels generated by semi-interpenetrating the polysaccharide in the collagen-polyurethane matrix and generating biomaterials in the hydrogel state potentially useful in biomedicine. Starch increased the reticulation of the polymeric matrix by hydrogen bonding with the collagen fibers. The maximum swelling degree was observed for the formulation containing 40 wt.% of starch. The microstructure of these materials is semi-crystalline and the increase of the content of starch avoids the segregation of starch granules in the matrix, generating homogeneous surfaces that tend to release less glucose-rich degradation by-products and encapsulated ketorolac. Materials with low content of starch (10–20 wt.%) improve both the mechanical and thermal stability of the hydrogels and the ketorolac release performance. The matrices activated the metabolism of monocytes and fibroblasts, favoring their proliferation. The presence of starch in semi-IPN hydrogels confers high inhibition capacity of E. coli and a slow rate of hydrolytic and proteolytic degradation. The results of cell signaling for important cytokines in the wound healing process indicated that the CS20% matrix shows favorable modulation of TNF-α, MCP-1, and TGF-β secretion, so it could be successfully applied in the treatment of chronic wounds.

Green and biodegradable surfactant based shale inhibitors for water based fluids

In recent decades, many shale inhibitors have been developed to reduce clay swelling and improve drilling efficiency. Among these categories, biomolecules and biosurfactants have received much attention due to their high inhibition capacity, biodegradability, low toxicity, and compatibility with water-based drilling fluids. In this study, two green surfactants, Flaxseed Protein (FP) and Flaxseed Mucilage (FM) were extracted and analysed through a series of laboratory measurements to evaluate their efficiency as effective shale inhibitors. The results obtained indicated that both surfactants have good survivability and functionality under different temperature conditions. They also possess the necessary functional groups to reduce interfacial tension, alter surface wettability and encapsulate clays to reduce hydration. It was also found that both surfactants are compatible with salt (KCl) and the presence of salts does not affect their functionalities. The results of the bentonite dispersion and shale inhibition tests also revealed that FM with its gelling properties forms a thin layer around the clay, while FP with its positive surface charge adsorbs on the clay surface where the affinity of the clay to interact with water decreases.

Comparison of three different COVID-19 vaccine platforms (CoronaVac, BTN162b2, and Ad5-nCoV) in individuals with and without prior COVID-19: Reactogenicity and neutralizing antibodies

Neutralizing antibodies (NAbs) can be indicators of collective immunity, vaccine efficacy, and the longevity of the humoral response. This study aimed to compare reactogenicity and NAbs generated by three different COVID-19 vaccine platforms in individuals with and without prior COVID-19. 336 individuals vaccinated (112 with CoronaVac [inactivated virus], 112 with BNT162b2 [messenger RNA], and 112 with Ad5-nCoV [non-replicating viral vector]) were included. NAbs were quantified with the cPass SARS-CoV-2 kit. Individuals immunized with the Ad5-nCoV showed higher reactogenicity than those immunized with the other vaccines (p < 0.001). The BTN162b2 vaccine-induced NAbs with higher inhibition capacity than the other platforms in the first dose. In individuals without prior COVID-19, the Ad5-nCoV vaccine generated lower NAbs against SARS-CoV-2 than those induced by two doses of the BTN162b2 (Ad5-nCoV 72.10 [55.6-93.4] vs. BTN162b2 98.41 [98.16-98.56], p < 0.0001). One individual did not generate NAbs (0.89%) after a complete immunization with CoronaVac; in BTN162b2, all generated these antibodies, and in the Ad5-nCoV group, four individuals (3.57%) did not generate NAbs. Comorbidities, gender, age, and reactogenicity did not significantly influence the generation of NAbs (p > 0.05); however, a history of COVID-19 before vaccination was associated with antibodies with greater neutralizing capacity after the first dose (p < 0.01). In conclusion, the mRNA vaccine (BTN162b2) had a remarkable better ability to produce NAbs and lower reactogenicity than the other platforms, whereas the Ad5-nCov vaccine induced the lowest NAbs response in individuals without a history of COVID-19; therefore, we suggest that a booster could benefit these individuals.

Development of a natural antifungal formulation for grated cheese and a microencapsulation approach using whey protein isolate and maltodextrin blend.

The antifungal activity of natural antimicrobials such as essential oils (EOs), citrus extracts, and other natural derivatives was evaluated against 10 fungal strains using minimum inhibitory concentration (MIC) analysis. Compounds having the highest inhibitory activity at the lowest concentrations were subsequently selected to evaluate the possible synergistic interactions by checkerboard method (FIC). The results showed that citrus extract A (CEA) and EOs rich in cinnamaldehyde had the highest inhibitory capacity against evaluated strains (Aspergillus niger, Aspergillus versicolor, Aureobasidium pullulans, Eurotium rubrum, Paecilomyces spp., Penicillium chrysogenum, Penicillium citrinum, Penicillium commune, Penicillium crustosum, and Penicillium roqueforti). The stability of the antifungal mixture was then optimized using lecithin and sucrose monopalmitate (SMP) as surfactants. Stability test showed that lecithin:SMP at HLB 10 maintains emulsion stability for 15 days of storage at 4°C. Encapsulation process for the loaded emulsion was optimized using whey protein isolate (WPI) and maltodextrin (MD) blend with ratios WPI:MD (1:2) and WPI:MD (1:3). The results showed that WPI:MD (1:3) led to a higher physicochemical stability (-40.5mV), encapsulation efficiency (91%), and antifungal activity (315ppm). Microencapsulation maintained the available active compounds content more prolonged with an average interval of 7 days compared to the nonencapsulated formulations during storage at 4°C.

PEDOT:PSS in Solution Form Exhibits Strong Potential in Inhibiting SARS-CoV-2 Infection of the Host Cells by Targeting Viruses and Also the Host Cells.

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has caused a global pandemic with over 5 million fatalities. Vaccines against this virus have been globally administered; however, SARS-CoV-2 variants with spike protein mutations are continuously identified with strong capability to escape vaccine-elicited protection. Due to the high mutation rate and transmission ability, the development of a broad-spectrum SARS-CoV-2 inhibitor is highly in demand. In this study, the effect of poly(3,4-ethylenedioxythiophene):poly(styrene sulfonate) (PEDOT:PSS) against SARS-CoV-2 was investigated. The treatment of pseudoviruses carrying the SARS-CoV-2 spike protein with PEDOT:PSS strongly blocked SARS-CoV-2 pseudovirus infection in human ACE2-expressing cells without causing cytotoxicity. Specifically, PEDOT:PSS showed great potential in both inactivating viruses and rendering antiviral activity to the treated cells. The effects of other PEDOT:PSS solutions with different chemical ratios and properties were also validated to find the high inhibition capacity against SARS-CoV-2 pseudovirus infection. The transcriptomic data reveal that PEDOT:PSS-treated cells were endowed with transcriptional alteration, and it could be reverted after the removal of PEDOT:PSS from the culture medium. Importantly, PEDOT:PSS also exhibited broad-spectrum inhibition effects on the pseudovirus carrying the spike protein isolated from different variants. In combination with the advantage of high biocompatibility, PEDOT:PSS could thus be considered a potential therapeutic and prophylactic material against SARS-CoV-2.