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1.
Biol Pharm Bull ; 47(5): 997-999, 2024.
Article En | MEDLINE | ID: mdl-38777759

Patch tests are often used in safety evaluations to identify the substance causing skin irritation, but the same substance can sometimes give positive or negative results depending on the test conditions. Here, we investigated differences in the skin penetration of two test compounds under different application conditions. We studied the effects of the anionic surfactant sodium dodecyl sulfate (SDS) and the nonionic surfactant polysorbate 80 (PS) on skin penetration of the preservatives methylisothiazolinone (MT) and methylchloroisothiazolinone (MCT), which are used in cosmetics such as shampoos. The skin permeation of MT was enhanced by SDS but was unchanged by PS. Skin impedance decreased in the presence of SDS whereas PS had the same effect as the control aqueous solution, suggesting that SDS reduction of the barrier function of skin affects the permeation of MT, a hydrophilic drug. Application of a mixture of MCT and MT in the presence of SDS did not affect the skin permeation of MCT whereas the permeation of MT was enhanced by SDS, indicating that the skin permeation of MCT is less affected by SDS than is MT. Thus, attention should be paid to the possible effect of co-solutes, especially hydrophilic drugs.


Polysorbates , Skin Absorption , Skin , Sodium Dodecyl Sulfate , Surface-Active Agents , Thiazoles , Thiazoles/pharmacokinetics , Surface-Active Agents/pharmacology , Skin Absorption/drug effects , Polysorbates/pharmacology , Skin/metabolism , Skin/drug effects , Animals , Preservatives, Pharmaceutical , Swine , Cosmetics/pharmacokinetics , Electric Impedance , Permeability/drug effects
2.
Eur J Med Chem ; 271: 116449, 2024 May 05.
Article En | MEDLINE | ID: mdl-38691893

Methicillin-resistant Staphylococcus aureus (MRSA) is a widespread pathogen causing clinical infections and is multi-resistant to many antibiotics, making it urgent need to develop novel antibacterials to combat MRSA. Herein, we designed and prepared a series of novel osthole amphiphiles 6a-6ad by mimicking the structures and function of antimicrobial peptides (AMPs). Antibacterial assays showed that osthole amphiphile 6aa strongly inhibited S. aureus and 10 clinical MRSA isolates with MIC values of 1-2 µg/mL, comparable to that of the commercial antibiotic vancomycin. Additionally, 6aa had the advantages of rapid bacteria killing without readily developing drug resistance, low toxicity, good membrane selectivity, and good plasma stability. Mechanistic studies indicated that 6aa possesses good membrane-targeting ability to bind to phosphatidylglycerol (PG) on the bacterial cell membranes, thereby disrupting the cell membranes and causing an increase in intracellular ROS as well as leakage of proteins and DNA, and accelerating bacterial death. Notably, in vivo activity results revealed that 6aa exhibits strong anti-MRSA efficacy than vancomycin as well as a substantial reduction in MRSA-induced proinflammatory cytokines, including TNF-α and IL-6. Given the impressive in vitro and in vivo anti-MRSA efficacy of 6aa, which makes it a potential candidate against MRSA infections.


Anti-Bacterial Agents , Coumarins , Methicillin-Resistant Staphylococcus aureus , Microbial Sensitivity Tests , Methicillin-Resistant Staphylococcus aureus/drug effects , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Coumarins/chemistry , Coumarins/pharmacology , Coumarins/chemical synthesis , Animals , Cell Membrane/drug effects , Cell Membrane/metabolism , Molecular Structure , Structure-Activity Relationship , Humans , Dose-Response Relationship, Drug , Mice , Surface-Active Agents/pharmacology , Surface-Active Agents/chemistry , Surface-Active Agents/chemical synthesis
3.
Langmuir ; 40(21): 11106-11115, 2024 May 28.
Article En | MEDLINE | ID: mdl-38745419

Polycyclic aromatic hydrocarbons (PAHs), as persistent environmental pollutants, often reside in nonaqueous-phase liquids (NAPLs). Mycobacterium sp. WY10, boasting highly hydrophobic surfaces, can adsorb to the oil-water interface, stabilizing the Pickering emulsion and directly accessing PAHs for biodegradation. We investigated the impact of Triton X-100 (TX100) on this interfacial uptake of phenanthrene (PHE) by Mycobacteria, using n-tetradecane (TET) and bis-(2-ethylhexyl) phthalate (DEHP) as NAPLs. Interfacial tension, phase behavior, and emulsion stability studies, alongside confocal laser scanning microscopy and electron microscope observations, unveiled the intricate interplay. In surfactant-free systems, Mycobacteria formed stable W/O Pickering emulsions, directly degrading PHE within the NAPLs because of their intimate contact. Introducing low-dose TX100 disrupted this relationship. Preferentially binding to the cells, the surfactant drastically increased the cell hydrophobicity, triggering desorption from the interface and phase separation. Consequently, PAH degradation plummeted due to hindered NAPL access. Higher TX100 concentrations flipped the script, creating surfactant-stabilized O/W emulsions devoid of interfacial cells. Surprisingly, PAH degradation remained efficient. This paradox can be attributed to NAPL emulsification, driven by the surfactant, which enhanced mass transfer and brought the substrate closer to the cells, despite their absence at the interface. This study sheds light on the complex effect of surfactants on Mycobacteria and PAH uptake, revealing an antagonistic effect at low concentrations that ultimately leads to enhanced degradation through emulsification at higher doses. These findings offer valuable insights into optimizing bioremediation strategies in PAH-contaminated environments.


Biodegradation, Environmental , Mycobacterium , Octoxynol , Phenanthrenes , Surface-Active Agents , Phenanthrenes/chemistry , Phenanthrenes/pharmacology , Phenanthrenes/metabolism , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Mycobacterium/metabolism , Mycobacterium/drug effects , Mycobacterium/chemistry , Octoxynol/chemistry , Emulsions/chemistry , Alkanes/chemistry , Alkanes/metabolism , Hydrophobic and Hydrophilic Interactions
4.
Biotechnol Adv ; 73: 108373, 2024.
Article En | MEDLINE | ID: mdl-38704106

Biochemicals are widely used in the medicine and food industries and are more efficient and safer than synthetic chemicals. The amphipathic surfactants can interact with the microorganisms and embed the extracellular metabolites, which induce microbial metabolites secretion and biosynthesis, performing an attractive prospect of promoting the biochemical production. However, the commonness and differences of surfactant-mediated bio-manufacture in various fields are largely unexplored. Accordingly, this review comprehensively summarized the properties of surfactants, different application scenarios of surfactant-meditated bio-manufacture, and the mechanism of surfactants increasing metabolites production. Various biochemical productions such as pigments, amino acids, and alcohols could be enhanced using the cloud point and the micelles of surfactants. Besides, the amphiphilicity of surfactants also promoted the utilization of fermentation substrates, especially lignocellulose and waste sludge, by microorganisms, indirectly increasing the metabolites production. The increase in target metabolites production was attributed to the surfactants changing the permeability and composition of the cell membrane, hence improving the secretion ability of microorganisms. Moreover, surfactants could regulate the energy metabolism, the redox state and metabolic flow in microorganisms, which induced target metabolites synthesis. This review aimed to broaden the application fields of surfactants and provide novel insights into the production of microbial biochemicals.


Surface-Active Agents , Surface-Active Agents/metabolism , Surface-Active Agents/pharmacology , Surface-Active Agents/chemistry , Fermentation , Bacteria/metabolism , Biotechnology/methods , Lignin/metabolism , Lignin/chemistry , Industrial Microbiology/methods , Amino Acids/metabolism
5.
Colloids Surf B Biointerfaces ; 239: 113932, 2024 Jul.
Article En | MEDLINE | ID: mdl-38749165

Quaternary ammonium salts (QAS) are widely used in medicine, industry and agriculture as disinfectants, biocides, and fungicides. QAS have the ability to coat various surfaces, prevent adhesion of microorganisms to them and inhibit the formation of biofilm. A group of surfactants derived from benzoic acid with different chemical structures was tested: monomeric QAS with different alkyl chain lengths (C12, C14, C16), gemini QAS containing 12-carbon alkyl chains and linkers of various lengths (3,4,6 methylene groups), as well as multifunctional QAS. Among the tested surfactants, monomeric QAS showed the highest bactericidal and fungicidal activity. All three groups of tested compounds inhibited the filamentation of C. albicans. The best antimicrobial activity was demonstrated by the monomeric surfactant C12AA, while the multifunctional equivalent (2xC12AA) was characterized by good anti-adhesive activity. All tested compounds are non-mutagenic and cause low hemolysis of sheep erythrocytes. Multifunctional and gemini surfactants are also non-toxic.


Candida albicans , Hemolysis , Microbial Sensitivity Tests , Surface-Active Agents , Surface-Active Agents/pharmacology , Surface-Active Agents/chemistry , Surface-Active Agents/chemical synthesis , Sheep , Animals , Candida albicans/drug effects , Hemolysis/drug effects , Erythrocytes/drug effects , Biofilms/drug effects , Anti-Infective Agents/pharmacology , Anti-Infective Agents/chemistry , Anti-Infective Agents/chemical synthesis , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/chemical synthesis , Quaternary Ammonium Compounds/chemistry , Quaternary Ammonium Compounds/pharmacology , Quaternary Ammonium Compounds/chemical synthesis , Antifungal Agents/pharmacology , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry
6.
J Environ Manage ; 360: 121232, 2024 Jun.
Article En | MEDLINE | ID: mdl-38801804

Surfactant pollution is escalatitheng in eutrophic waters, but the effect of surfactant charge properties on the physiological and biochemical properties of toxin-producing microalgae remains inadequately explored. To address this gap, this study explores the effects and mechanisms of three common surfactants-cetyltrimethylammonium bromide (CTAB, cationic), sodium dodecyl sulfate (SDS, anionic), and Triton X-100 (nonionic)-found in surface waters, on the agglomeration behavior, physiological indicators, and Microcystin-LR (MC-LR) release of Microcystis aeruginosa (M. aeruginosa) by using UV-visible spectroscope, Malvern Zetasizer, fluorescence spectrometer, etc. Results suggest that charge properties significantly affect cyanobacterial aggregation and cellular metabolism. The CTAB-treated group demonstrates a ∼5.74 and ∼9.74 times higher aggregation effect compared to Triton X-100 and SDS (300 mg/L for 180 min) due to strong electrostatic attraction. Triton X-100 outperforms CTAB and SDS in polysaccharide extraction, attributed to its higher water solubility and lower critical micelle concentration. CTAB stimulates cyanobacteria to secrete proteins, xanthohumic acid, and humic acids to maintain normal physiological cells. Additionally, the results of SEM and ion content showed that CTAB damages the cell membrane, resulting in a ∼90% increase in the release of intracellular MC-LR without cell disintegration. Ionic analyses confirm that all three surfactants alter cell membrane permeability and disrupt ionic metabolic pathways in microalgae. This study highlights the relationship between the surface charge properties of typical surfactants and the dispersion/agglomeration behavior of cyanobacteria. It provides insights into the impact mechanism of exogenous surfactants on toxic algae production in eutrophic water bodies, offering theoretical references for managing surfactant pollution and treating algae blooms.


Microcystins , Microcystis , Surface-Active Agents , Microcystins/chemistry , Microcystins/metabolism , Microcystis/drug effects , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Octoxynol/chemistry , Octoxynol/pharmacology , Sodium Dodecyl Sulfate/chemistry , Sodium Dodecyl Sulfate/pharmacology
7.
Sci Rep ; 14(1): 11408, 2024 05 18.
Article En | MEDLINE | ID: mdl-38762671

In the enhanced oil recovery (EOR) process, interfacial tension (IFT) has become a crucial factor because of its impact on the recovery of residual oil. The use of surfactants and biosurfactants can reduce IFT and enhance oil recovery by decreasing it. Asphaltene in crude oil has the structural ability to act as a surface-active material. In microbial-enhanced oil recovery (MEOR), biosurfactant production, even in small amounts, is a significant mechanism that reduces IFT. This study aimed to investigate fluid/fluid interaction by combining low biosurfactant values and low-salinity water using NaCl, MgCl2, and CaCl2 salts at concentrations of 0, 1000, and 5000 ppm, along with Geobacillus stearothermophilus. By evaluating the IFT, this study investigated different percentages of 0, 1, and 5 wt.% of varying asphaltene with aqueous bulk containing low-salinity water and its combination with bacteria. The results indicated G. Stearothermophilus led to the formation of biosurfactants, resulting in a reduction in IFT for both acidic and basic asphaltene. Moreover, the interaction between asphaltene and G. Stearothermophilus with higher asphaltene percentages showed a decrease in IFT under both acidic and basic conditions. Additionally, the study found that the interaction between acidic asphaltene and G. stearothermophilus, in the presence of CaCl2, NaCl, and MgCl2 salts, resulted in a higher formation of biosurfactants and intrinsic surfactants at the interface of the two phases, in contrast to the interaction involving basic asphaltene. These findings emphasize the dependence of the interactions between asphaltene and G. Stearothermophilus, salt, and bacteria on the specific type and concentration of asphaltene.


Salinity , Surface Tension , Surface-Active Agents , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Water/chemistry , Geobacillus stearothermophilus , Sodium Chloride/chemistry , Petroleum , Calcium Chloride/chemistry
8.
Int J Mol Sci ; 25(8)2024 Apr 10.
Article En | MEDLINE | ID: mdl-38673760

This study aimed to evaluate how the combined presence of the synthetic fungicide azoxystrobin (AZ) and the biosurfactant-producing Bacillus sp. Kol B3 influences the growth of the phytopathogenic fungus Fusarium sambucinum IM 6525. The results showed a noticeable increase in antifungal effectiveness when biotic and abiotic agents were combined. This effect manifested across diverse parameters, including fungal growth inhibition, changes in hyphae morphology, fungal membrane permeability and levels of intracellular reactive oxygen species (ROS). In response to the presence of Fusarium and AZ in the culture, the bacteria changed the proportions of biosurfactants (surfactin and iturin) produced. The presence of both AZ and/or Fusarium resulted in an increase in iturin biosynthesis. Only in 72 h old bacterial-fungal co-culture a 20% removal of AZ was noted. In the fungal cultures (with and without the addition of the bacteria), the presence of an AZ metabolite named azoxystrobin free acid was detected in the 48th and 72nd hours of the process. The possible involvement of increased iturin and ROS content in antifungal activity of Bacillus sp. and AZ when used together are also discussed. Biosurfactants were analyzed by liquid chromatography with tandem mass spectrometry (LC-MS/MS). Microscopy techniques and biochemical assays were also used.


Antifungal Agents , Bacillus , Fusarium , Pyrimidines , Strobilurins , Surface-Active Agents , Strobilurins/pharmacology , Fusarium/drug effects , Fusarium/growth & development , Fusarium/metabolism , Bacillus/metabolism , Surface-Active Agents/pharmacology , Surface-Active Agents/metabolism , Antifungal Agents/pharmacology , Pyrimidines/pharmacology , Reactive Oxygen Species/metabolism , Microbial Sensitivity Tests
9.
Bioresour Technol ; 400: 130690, 2024 May.
Article En | MEDLINE | ID: mdl-38614150

Microbial enhanced oil recovery (EOR) has become the focus of oilfield research due to its low cost, environmental friendliness and sustainability. The degradation and EOR capacity of A. borkumensis through the production of bio-enzyme and bio-surfactant were first investigated in this study. The total protein concentration, acetylcholinesterase, esterase, lipase, alkane hydroxylase activity, surface tension, and emulsification index (EI) were determined at different culture times. The bio-surfactant was identified as glycolipid compound, and the yield was 2.6 ± 0.2 g/L. The nC12 and nC13 of crude oil were completely degraded, and more than 40.0 % of nC14-nC24 was degraded by by A. borkumensis. The results of the microscopic etching model displacement and core flooding experiments showed that emulsification was the main mechanism of EOR. A. borkumensis enhanced the recovery rate by 20.2 %. This study offers novel insights for the development of environmentally friendly and efficient oil fields.


Alcanivoraceae , Biodegradation, Environmental , Petroleum , Surface-Active Agents , Surface-Active Agents/pharmacology , Surface-Active Agents/chemistry , Alcanivoraceae/metabolism , Petroleum/metabolism , Acetylcholinesterase/metabolism , Lipase/metabolism , Surface Tension , Emulsions
10.
ACS Appl Mater Interfaces ; 16(17): 22558-22570, 2024 May 01.
Article En | MEDLINE | ID: mdl-38637157

The development of nanopesticides provides new avenues for pesticide reduction and efficiency improvement. However, the size effect of nanopesticides remains unclear, and its underlying mechanisms of influence have become a major obstacle in the design and application of pesticide nanoformulations. In this research, the noncarrier-coated emamectin benzoate (EB) solid dispersions (Micro-EB and Nano-EB) were produced under a constant surfactant-to-active ingredient ratio by a self-emulsifying-carrier solidification technique. The particle size of Micro-EB was 162 times that of spherical Nano-EB. The small size and large specific surface area of Nano-EB facilitated the adsorption of surfactants on the surface of the particles, thereby improving its dispersibility, suspensibility, and stability. The pinning effect of nanoparticles significantly suppressed droplet retraction and rebounding. Moreover, Nano-EB exhibited a 25% higher retention of the active ingredient on cabbage leaves and a 70% higher washing resistance than Micro-EB, and both were significantly different. The improvement of abilities in wetting, spreading, and retention of Nano-EB on crop leaves contributed to the increase in foliar utilization, which further resulted in a 1.6-fold enhancement of bioactivity against target Spodoptera exigua compared to Micro-EB. Especially, Nano-EB did not exacerbate the safety risk to the nontarget organism zebrafish with no significant difference. This study elaborates the size effect on the effectiveness and safety of pesticide formulations and lays a theoretical foundation for the development and rational utilization of efficient and environmentally friendly nanopesticides.


Ivermectin , Ivermectin/analogs & derivatives , Nanoparticles , Particle Size , Spodoptera , Ivermectin/pharmacology , Ivermectin/chemistry , Animals , Spodoptera/drug effects , Nanoparticles/chemistry , Insecticides/pharmacology , Insecticides/chemistry , Plant Leaves/chemistry , Plant Leaves/metabolism , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Brassica/drug effects
11.
Int J Pharm ; 656: 124120, 2024 May 10.
Article En | MEDLINE | ID: mdl-38621613

While various non-ionic surfactants at low concentrations have been shown to increase the transport of P-gp substrates in vitro, in vivo studies in rats have shown that a higher surfactant concentration is needed to increase the oral absorption of e.g. the P-gp substrates digoxin and etoposide. The aim of the present study was to investigate if intestinal digestion of surfactants could be the reason for this deviation between in vitro and in vivo data. Therefore, Kolliphor EL, Brij-L23, Labrasol and polysorbate 20 were investigated for their ability to inhibit P-gp and increase digoxin absorption in vitro. Transport studies were performed in Caco-2 cells, while P-gp inhibition and cell viability assays were performed in MDCKII-MDR1 cells. Polysorbate 20, Kolliphor EL and Brij-L23 increased absorptive transport and decreased secretory digoxin transport in Caco-2 cells, whereas only polysorbate 20 and Brij-L23 showed P-gp inhibiting properties in the MDCKII-MDR1 cells. Polysorbate 20 and Brij-L23 were chosen for in vitro digestion prior to transport- or P-gp inhibiting assays. Brij-L23 was not digestible, whereas polysorbate 20 reached a degree of digestion around 40%. Neither of the two surfactants showed any significant difference in their ability to affect absorptive or secretory transport of digoxin after pre-digestion. Furthermore, the P-gp inhibiting effects of polysorbate 20 were not decreased significantly. In conclusion, the mechanism behind the non-ionic surfactant mediated in vitro P-gp inhibition seemed independent of the intestinal digestion and the results presented here did not suggest it to be the cause of the observed discrepancy between in vitro and in vivo.


ATP Binding Cassette Transporter, Subfamily B, Member 1 , Digoxin , Polysorbates , Surface-Active Agents , Animals , Dogs , Humans , ATP Binding Cassette Transporter, Subfamily B, Member 1/metabolism , ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors , Biological Transport/drug effects , Caco-2 Cells , Cell Survival/drug effects , Digestion/drug effects , Digoxin/pharmacokinetics , Glycerides/metabolism , Intestinal Absorption/drug effects , Madin Darby Canine Kidney Cells , Polysorbates/pharmacology , Surface-Active Agents/pharmacology
12.
Toxicol Appl Pharmacol ; 486: 116939, 2024 May.
Article En | MEDLINE | ID: mdl-38643951

Idiopathic pulmonary fibrosis (IPF) is an irreversible disease which considered the most fatal pulmonary fibrosis. Pulmonary toxicity including IPF is the most severe adverse effect of bleomycin, the chemotherapeutic agent. Based on the fact that, exogenous surfactants could induce alveolar stabilization in many lung diseases, the aim of this study was to explore the effects of low cost biosurfactants, surfactin (SUR) and sophorolipids (SLs), against bleomycin-induced pulmonary fibrosis in mice due to their antioxidant, and anti-inflammatory properties. Surfactin and sophorolipids were produced by microbial conversion of frying oil and potato peel wastes using Bacillus halotolerans and Candida parapsilosis respectively. These biosurfactants were identified by FTIR, 1H NMR, and LC-MS/MS spectra. C57BL/6 mice were administered the produced biosurfactants daily at oral dose of 200 mg kg-1 one day after the first bleomycin dose (35 U/kg). We evaluated four study groups: Control, Bleomycin, Bleomycin+SUR, Bleomycin+SLs. After 30 days, lungs from each mouse were sampled for oxidative stress, ELISA, Western blot, histopathological, immunohistochemical analyses. Our results showed that the produced SUR and SLs reduced pulmonary oxidative stress and inflammatory response in the lungs of bleomycin induced mice as they suppressed SOD, CAT, and GST activities also reduced NF-κß, TNF-α, and CD68 levels. Furthermore, biosurfactants suppressed the expression of TGF-ß1, Smad-3, and p-JNK fibrotic signaling pathway in pulmonary tissues. Histologically, SUR and SLs protected against lung ECM deposition caused by bleomycin administration. Biosurfactants produced from microbial sources can inhibit the induced inflammatory and fibrotic responses in bleomycin-induced pulmonary fibrosis.


Anti-Inflammatory Agents , Antioxidants , Bleomycin , Candida parapsilosis , Mice, Inbred C57BL , MicroRNAs , Pulmonary Fibrosis , Smad3 Protein , Surface-Active Agents , Transforming Growth Factor beta1 , Animals , Pulmonary Fibrosis/chemically induced , Pulmonary Fibrosis/prevention & control , Pulmonary Fibrosis/pathology , Pulmonary Fibrosis/metabolism , Bleomycin/toxicity , Antioxidants/pharmacology , Transforming Growth Factor beta1/metabolism , Anti-Inflammatory Agents/pharmacology , Smad3 Protein/metabolism , Mice , Candida parapsilosis/drug effects , Surface-Active Agents/pharmacology , MicroRNAs/metabolism , Male , Signal Transduction/drug effects , Bacillus , Lung/drug effects , Lung/pathology , Lung/metabolism , Oxidative Stress/drug effects , Oleic Acids
13.
Pestic Biochem Physiol ; 201: 105897, 2024 May.
Article En | MEDLINE | ID: mdl-38685223

Solid nanodispersion (SND) is an important variety of nanopesticides which have been extensively studied in recent years. However, the key influencing factors for bioactivity enhancement of nanopesticides remain unclear, which not only limits the exploration of relevant mechanisms, but also hinders the precise design and development of nanopesticides. In this study, we explored the potential of SND in enhancing the bioactivity of nanopesticides, specifically focusing on abamectin SND prepared using a self-emulsifying-carrier solidifying technique combined with parameter optimization. Our formulation, consisting of 8% abamectin, 1% antioxidant BHT (2,6-di-tert-butyl-4-methylphenol), 12% complex surfactants, and 79% sodium benzoate, significantly increased the pseudo-solubility of abamectin by at least 3300 times and reduced its particle size to a mere 15 nm, much smaller than traditional emulsion in water (EW) and water-dispersible granule (WDG) forms. This reduction in particle size and increase in surface activity resulted in improved foliar adhesion and retention, enabling a more efficient application without the need for organic solvents. The inclusion of antioxidants also enhanced photostability compared to EW, and overall stability tests confirmed SND's resilience under various storage conditions. Bioactivity tests demonstrated a marked increase in toxicity against diamondback moths (Plutella xylostella L.) with abamectin SND, which exhibited 3.7 and 7.6 times greater efficacy compared to EW and WDG, respectively. These findings underscore the critical role of small particle size, high surface activity, and strong antioxidant properties in improving the performance and bioactivity of abamectin SND, highlighting its significance in the design and development of high-efficiency, eco-friendly nanopesticides and contributing valuably to sustainable agricultural practices.


Ivermectin , Ivermectin/analogs & derivatives , Ivermectin/pharmacology , Ivermectin/chemistry , Animals , Insecticides/pharmacology , Insecticides/chemistry , Particle Size , Antioxidants/pharmacology , Antioxidants/chemistry , Nanoparticles/chemistry , Moths/drug effects , Surface-Active Agents/pharmacology , Surface-Active Agents/chemistry , Larva/drug effects , Emulsions
14.
Sheng Wu Gong Cheng Xue Bao ; 40(3): 786-798, 2024 Mar 25.
Article Zh | MEDLINE | ID: mdl-38545977

Rhamnolipids (RLs) have emerged as one of the most promising classes of biosurfactants. The ratio of mono-RL to di-RL plays a significant role in determining its performance. Therefore, strains whose production of mono-RL and di-RL are manuplable, have advantage on applications in various scenarios. In this study, we developed a rhlC deletion mutant strain in Pseudomonas aeruginosa PAO1, which produced primarily mono-RL. Subsequently, we generated two complemented strains by integrating the arabinose-induced PBAD-rhlC gene, either directly into the chromosomes or expressing it on plasmids. Our results indicate that the ratio of mono-RL to di-RL synthesized by the complemented strain gradually decreased as the concentration of arabinose (the inducer) increased. Consequently, there was a decrease in emulsification ability and an increase in surface tension and critical micelle concentration (CMC) of the corresponding rhamnolipids. The complemented strains without inducer can produce a small amount of di-rhamnolipids, which enhanced the surfactant properties. Notably, the rhamnolipids induced by 0.10% arabinose exhibited the most potent antibacterial effect.


Arabinose , Glycolipids , Glycolipids/pharmacology , Anti-Bacterial Agents/pharmacology , Surface-Active Agents/pharmacology , Pseudomonas aeruginosa/genetics
15.
J Dent ; 144: 104961, 2024 May.
Article En | MEDLINE | ID: mdl-38527516

OBJECTIVES: Lipopeptide Biosurfactant (LB) is a bacteria derived compound able to reduce surface tension between water and hydrophobic substances and exhibit antimicrobial and anti-biofilm properties. This study aimed to investigate the antimicrobial and anti-biofilm effect of a Lipopeptide Biosurfactant (LB) on Enterococcus faecalis, and its potential use in root canal treatment, either as a standalone irrigation solution or in conjunction with sodium hypochlorite (NaOCl). METHODS: LB was extracted from Bacillus clausii isolate and the dry extract was diluted in deionized water. The antimicrobial effect of LB against planktonic E. faecalis was evaluated by determining the Minimal Inhibitory Concentration (MIC50). The anti-biofilm effect was evaluated by Minimal Biofilm Inhibitory Concentration (MBIC50) and Minimal Biofilm Eradication Concentration (MBEC50) assays on biofilm grown on dentin specimen surface. To evaluate the effectiveness of LB as a single irrigation solution and as a pre-irrigation prior to NaOCl, live and dead bacterial cells were quantified using Confocal Laser Scanning Microscopy (CLSM), and cell biomass was assessed. RESULTS: LB exhibited an MIC50 and MBIC50 of 100 ppm, with an MBEC50 of 1000 ppm, resulting in 52.94 % biofilm inhibition and 60.95 % biofilm eradication on dentin specimens. The effectiveness was concentration-dependent, at 500 ppm, LB demonstrated comparable antimicrobial efficacy to 2.5 % NaOCl. Pre-irrigation with LB resulted in lower biofilm biomass compared to NaOCl alone. CONCLUSION: Pre-irrigation with LB enhanced the antimicrobial effect when followed by NaOCl irrigation. Consequently, LB shows promise as both a standalone root canal irrigation solution and as an adjunct to NaOCl in root canal treatment. CLINICAL SIGNIFICANCE: The study highlights the potential of Lipopeptide Biosurfactant (LB) as an environmentally friendly irrigation solution for root canal treatment, demonstrating potent antimicrobial and anti-biofilm properties against Enterococcus faecalis. LB exhibits concentration-dependent efficacy comparable to 2.5 % NaOCl and can be used as a standalone irrigation solution or in conjunction with NaOCl.


Biofilms , Enterococcus faecalis , Lipopeptides , Microbial Sensitivity Tests , Root Canal Irrigants , Sodium Hypochlorite , Surface-Active Agents , Biofilms/drug effects , Root Canal Irrigants/pharmacology , Enterococcus faecalis/drug effects , Surface-Active Agents/pharmacology , Sodium Hypochlorite/pharmacology , Lipopeptides/pharmacology , Humans , Microscopy, Confocal , Dentin/microbiology , Dentin/drug effects , Bacillus/drug effects , Dental Pulp Cavity/microbiology , Anti-Infective Agents/pharmacology , Anti-Bacterial Agents/pharmacology
16.
Int J Biol Macromol ; 266(Pt 2): 130861, 2024 May.
Article En | MEDLINE | ID: mdl-38490384

The formation of dual-layer asymmetric porous structures in surfactant-based systems is significantly influenced by emulsions. Surfactants self-assemble to alter the conformational arrangement of polysaccharides, while gravity disrupts the initial uniformity of the established equilibrium droplet concentration gradient in the emulsion, thus achieving delamination. Specifically, high-speed rotation and non-instantaneous freezing allow the gelatin solution to form two different states of foam layers. The integrated dual-layer asymmetric porous structure, composed of polysaccharides and tannic acid, is constructed with gelatin as a skeleton and surfactant. This innovative approach eliminates the need to consider the toxicity of chemically synthesized surfactants and expands the concept of gelatin utilization. This intriguing structure exhibits a variety of desirable characteristics within 30 days (e.g., tailorable performance, ultrarapid antioxidant activity, efficient antibacterial activity, low differential blood clotting index, and good hemocompatibility and cytocompatibility), suggesting its potential as a valuable reference for applying hierarchical porous structures, thereby offering more formulation flexibility for biomaterials with adjustable properties.


Gelatin , Polyphenols , Polysaccharides , Surface-Active Agents , Tannins , Gelatin/chemistry , Tannins/chemistry , Polysaccharides/chemistry , Polysaccharides/pharmacology , Porosity , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Surface-Active Agents/chemical synthesis , Biocompatible Materials/chemistry , Biocompatible Materials/pharmacology , Antioxidants/chemistry , Antioxidants/pharmacology , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Humans , Animals , Emulsions/chemistry , Blood Coagulation/drug effects
17.
J Pharm Pharmacol ; 76(6): 631-645, 2024 Jun 06.
Article En | MEDLINE | ID: mdl-38507715

PURPOSE: Although resveratrol (RES) is an efficacious molecule, its therapeutic activity is impeded by significant limitations, such as rapid oral absorption, poor oral bioavailability, and low water solubility. Therefore, the preparation of RES in different pharmaceutical carriers represents an important tool to enhance its therapeutic applications. This study aims to potentiate the anti-cancer activity of RES by formulating it into a novel nanocarrier called Smart Lipid. METHODS: RES-loaded Smart Lipids were prepared by high-shear hot homogenization method utilizing a 21 × 32 factorial design with three factors at different levels: the total lipid concentration, the concentration of surfactant, and the type of surfactant. The responses were evaluated based on entrapment efficiency percentages and particle size. RESULTS: Our novel optimized RES-loaded Smart Lipid formula showed small particle size (288.63 ± 5.55 nm), good zeta potential (-16.44 ± 0.99 mV), and an entrapment efficiency of 86.346 ± 3.61% with spherical, clearly distinct, and no signs of fusion by transmission electron microscopy. Further characterization was done using differential scanning calorimetry, which showed no interaction between the drug and other components as the optimum lyophilized formula showed a peak at 54.75°C, which represents the lipid mixture, with an undetectable characteristic peak of the drug, which indicates entrapment of the drug, and the structure of the compounds was confirmed by Fourier transform-infrared spectroscopy, in which the majority of the drug's characteristic peaks disappeared when loaded into Smart Lipid, which may indicate Smart Lipid's ability to reduce the stretching and bending between bonds in RES. In addition, the optimized formula showed a sustained release pattern compared to RES suspension. Finally, the cytotoxic activity of the optimized RES-loaded Smart Lipid on different cell lines (human breast adenocarcinoma (MCF7), human hepatocellular carcinoma (HepG2), and human colon cancer cells (HT29)) was assessed through MTT assay (7-fold reduction in the IC50, from 3.7 ± 0.5 µM for free RES to 0.5 ± 0.033 µM for Smart Lipid loaded formula against MCF7, 3-fold reduction in the IC50 against HepG2 cells, from 10.01 ± 0.35 to 3.16 ± 0.21 µMm, and a more than 10-fold reduction in the IC50 from more than 100 to 10 ± 0.57 µM against HT-29 cells) and its effect on cell cycle progression and apoptosis induction were assessed using flow cytometry and annexin V kit, respectively. Our results showed that RES-loaded Smart Lipid significantly reduced cell viability, induced cell cycle arrest at G0/G1 phase, and apoptosis compared to free formula and free RES suspension. CONCLUSION: Loading RES into this novel kind of nanocarrier enhanced RES absorption, cellular accumulation, and improved its anticancer properties.


Drug Carriers , Lipids , Particle Size , Resveratrol , Resveratrol/pharmacology , Resveratrol/administration & dosage , Resveratrol/chemistry , Humans , Lipids/chemistry , Drug Carriers/chemistry , Hep G2 Cells , Nanoparticles/chemistry , Drug Compounding/methods , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/administration & dosage , Solubility , Calorimetry, Differential Scanning , Surface-Active Agents/chemistry , Surface-Active Agents/pharmacology , Cell Line, Tumor , Chemistry, Pharmaceutical/methods , Drug Liberation , Drug Design/methods , MCF-7 Cells , Antineoplastic Agents, Phytogenic/pharmacology , Antineoplastic Agents, Phytogenic/administration & dosage , Antineoplastic Agents, Phytogenic/chemistry , Stilbenes/pharmacology , Stilbenes/chemistry , Stilbenes/administration & dosage
18.
Ann Ig ; 36(4): 487-497, 2024.
Article En | MEDLINE | ID: mdl-38545674

Introduction: The correct method of surface disinfection in hospitals is an essential tool in the fight against the spread of healthcare-associated infections caused by multi-resistant microorganisms. Currently, there are many disinfectants on the market that can be used against different microorganisms. However, the effectiveness of different active molecules is controversial in the literature. Study design: The aim of this study was to evaluate the effectiveness of wipes based on hydrogen peroxide (1.0 %) and highly specific plant-based surfactants, contained in H2O2TM (Hi-speed H2O2TM) products, against some hospital-associated microorganisms. Methods: The effectiveness of the wipes was tested against nosocomial and control strains of methicillin-resistant Staphylococcus aureus, carbapenem-resistant Pseudomonas aeruginosa, Klebsiella pneumoniae carbapenemase, Aspergillus fumigatus and Candida parapsilosis. Specifically, in vitro activity was assessed using three different techniques: stainless steel surface testing, surface diffusion testing and well diffusion test. Results: The three different methods tested confirm the wipes' good effectiveness against the most common multi-resistant bacteria and against fungi. Conclusions: These data show that the tested wipes could be a valid adjunct to the disinfection process and could assist in the prevention of healthcare-associated infections.


Cross Infection , Disinfectants , Disinfection , Hydrogen Peroxide , Disinfection/methods , Hydrogen Peroxide/pharmacology , Cross Infection/prevention & control , Disinfectants/pharmacology , Humans , Health Facilities , Surface-Active Agents/pharmacology , Methicillin-Resistant Staphylococcus aureus/drug effects
19.
J Vis Exp ; (204)2024 Feb 23.
Article En | MEDLINE | ID: mdl-38465928

Cationic nanostructures have emerged as an adjuvant and antigen delivery system that enhances dendritic cell maturation, ROS generation, and antigen uptake and then promotes antigen-specific immune responses. In recent years, retinoic acid (RA) has received increasing attention due to its effect in activating the mucosal immune response; however, in order to use RA as a mucosal adjuvant, it is necessary to solve the problem of its dissolution, loading, and delivery. Here, we describe a cationic nanoemulsion-encapsulated retinoic acid (CNE-RA) delivery system composed of the cationic lipid 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOTAP), retinoic acid, squalene as the oil phase, polysorbate 80 as surfactant, and sorbitan trioleate 85 as co-surfactant. Its physical and chemical properties were characterized using dynamic light scattering and a spectrophotometer. Immunization of mice with the mixture of antigen (ovalbumin, OVA) and CNE-RA significantly elevated the levels of anti-OVA secretory immunoglobulin A (sIgA) in vaginal lavage fluid and the small intestinal lavage fluid of mice compared with OVA alone. This protocol describes a detailed method for the preparation, characterization, and evaluation of the adjuvant effect of CNE-RA.


Adjuvants, Immunologic , Immunization , Female , Animals , Mice , Adjuvants, Immunologic/pharmacology , Adjuvants, Immunologic/chemistry , Mucous Membrane , Vaccination , Antigens , Immunity, Mucosal , Surface-Active Agents/pharmacology , Ovalbumin , Mice, Inbred BALB C
20.
Biomed Khim ; 70(1): 61-68, 2024 Feb.
Article En | MEDLINE | ID: mdl-38450682

Using the method of shotgun mass spectrometry, we have evaluated changes in the proteomic profile of HaCat cells in response to the treatment with sodium dodecyl sulfate (anionic surfactant) and Triton-X100 (non-ionic surfactant) in two concentrations (12.5 µg/ml and 25.0 µg/ml). The study revealed induction of orphan CYP2S1 (biotransformation phase I) in response to Triton-X100. We have identified proteins of II (glutathione-S-transferases, GSTs) and III (solute carrier proteins, SLCs) biotransformation phases, as well as antioxidant proteins (peroxiredoxins, PRDXs; catalase, CAT; thioredoxin, TXN). Thus, proteins of all three xenobiotic detoxification phases were detected. The presented results suggest a new prospect of using HaCaT keratinocytes as a model of human epidermis for studying the metabolism of drugs/toxicants in human skin in vitro.


Proteomics , Surface-Active Agents , Humans , Surface-Active Agents/pharmacology , Keratinocytes , Cell Line , Skin , Octoxynol , Cytochrome P-450 Enzyme System
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