Design,Synthesis, and Antibacterial Activity of Demethylvancomycin Analogues against Drug‐Resistant Bacteria

Five novel N‐substituted demethylvancomycin derivatives were rationally designed and synthesized by using a structure‐based approach. The in vitro antibacterial activities against methicillin‐resistant Staphylococcus aureus (MRSA), gentamicin‐resistant Enterococcus faecalis (GRE), methicillin‐resistant Streptococcus pneumoniae (MRS), and vancomycin‐resistant Enterococcus faecalis (VRE) were evaluated. One of the compounds, N‐(6‐phenylheptyl)demethylvancomycin ( 12 a ), was found to exhibit more potent antibacterial activity than vancomycin and demethylvancomycin. Compound 12 a was also found to be ～18‐fold more efficacious than vancomycin against MRSA; however, the two compounds were found to have similar efficacy against MRS. Furthermore, compound 12 a exhibited a favorable pharmacokinetic profile with a half‐life of 5.11±0.52 h, which is longer than that of vancomycin (4.3±1.9 h). These results suggest that 12 a is a promising antibacterial drug candidate for further preclinical evaluation.     

Antibacterial materials: structure–bioactivity relationship of epoxy–amine resins containing quaternary ammonium compounds covalently attached

Bifunctional aminoalkyldimethylpropylammonium salts (N‐(3‐aminopropyl)‐N,N‐dimethylpentylammonium chloride, N‐(3‐aminopropyl)‐N,N‐dimethyloctylammonium chloride, N‐(3‐aminopropyl)‐N,N‐dimethyldecylammonium chloride, N‐(3‐aminopropyl)‐N,N‐dimethyldodecylammonium chloride) are synthesized and their structure‐dependent antibacterial effect against Gram‐negative Escherichia coli and Gram‐positive Lactococcus lactis is investigated. To this end, resins prepared from bisphenol A diglycidyl ether (2,2‐bis[4‐(glycidyloxy)phenyl]propane) and diethylenetriamine (2,2′‐diaminodiethylamine) as matrix and the bifunctional aminoalkyldimethylpropylammonium salts in a ratio of 6 mol% compared to epoxy components are used. A dependence of antibacterial effect on alkyl chain length of the quaternary ammonium compounds is observed for both species. Furthermore, resins with N‐(3‐aminopropyl)‐N,N‐dimethyldecylammonium chloride in varying concentrations up to 16 mol% for both organisms show a concentration‐dependent antibacterial effect of the quaternary ammonium salt. The antibacterial materials are characterized by differential scanning calorimetry, infrared spectroscopy and rheological studies. © 2013 Society of Chemical Industry     

Broad-Spectrum Bactericidal Activity of a Synthetic Random Copolymer Based on 2-Methoxy-6-(4-Vinylbenzyloxy)-Benzylammonium Hydrochloride

Low-molecular-weight organic ammonium salts exert excellent antimicrobial effects by interacting lethally with bacterial membranes. Unfortunately, short-term functionality and high toxicity limit their clinical application. On the contrary, the equivalent macromolecular ammonium salts, derived from the polymerization of monomeric ammonium salts, have demonstrated improved antibacterial potency, a lower tendency to develop resistance, higher stability, long-term activity, and reduced toxicity. A water-soluble non-quaternary copolymeric ammonium salt (P7) was herein synthetized by copolymerizing 2-methoxy-6-(4-vinylbenzyloxy)-benzylammonium hydrochloride monomer with N, N-di-methyl-acrylamide. The antibacterial activity of P7 was assessed against several multidrug-resistant (MDR) clinical isolates of both Gram-positive and Gram-negative species. Except for colistin-resistant Pseudomonas aeruginosa, most isolates were susceptible to P7, also including some Gram-negative bacteria with a modified charge in the external membrane. P7 showed remarkable antibacterial activity against isolates of Enterococcus, Staphylococcus, Acinetobacter, and Pseudomonas, and on different strains of Escherichia coli and Stenotrophomonas maltophylia, regardless of their antibiotic resistance. The lowest minimal inhibitory concentrations (MICs) observed were 0.6–1.2 µM and the minimal bactericidal concentrations (MBC) were frequently overlapping with the MICs. In 24-h time–kill and turbidimetric studies, P7 displayed a rapid non-lytic bactericidal activity. P7 could therefore represent a novel and potent tool capable of counteracting infections sustained by several bacteria that are resistant to the presently available antibiotics.     

Synthesis and Structural Characterisation of Selective Non‐Carbohydrate‐Based Inhibitors of Bacterial Sialidases

The major human pathogen Streptococcus pneumoniae plays a key role in several disease states including septicaemia, meningitis and community‐acquired pneumonia. Although vaccines against S. pneumoniae are available as prophylactics, there remains a need to identify and characterise novel chemical entities that can treat the diseases caused by this pathogen. S. pneumoniae expresses three sialidases, enzymes that cleave sialic acid from carbohydrate‐based surface molecules. Two of these enzymes, NanA and NanB, have been implicated in the pathogenesis of S. pneumoniae and are considered to be validated drug targets. Here we report our studies on the synthesis and structural characterisation of novel NanB‐selective inhibitors that are inspired by the β‐amino‐sulfonic acid family of buffers.     

Preparation of O‐diallylammonium chitosan with antibacterial activity and cytocompatibility

In this study, a derivative of chitosan, O‐hydroxy‐2,3‐propyl‐N‐methyl‐N,N‐diallylammonium chitosan methyl sulfate (O‐MDAACS), was synthesized by reacting chitosan with methyl diallyl ammonium. The O‐MDAACS was confirmed by Fourier transform infrared spectroscopy and ¹H NMR. Characterization was conducted including X‐ray diffraction, differential scanning calorimetry and thermogravimetry. The antibacterial activities of O‐MDAACS against Staphylococcus aureus and Klebsiella pneumoniae were evaluated. The minimum inhibitory concentrations on O‐MDAACS were 3.7% and 23% of those on chitosan against S. aureus and K. pneumonia, respectively. The minimum bactericidal concentrations on O‐MDAACS were 7% and 36% of those on chitosan against S. aureus and K. pneumonia, respectively. Thus the antibacterial activity of O‐MDAACS was higher than that of chitosan. The cytocompatibility was evaluated in vitro with L929 fibroblasts. The results showed that after 72 h incubation the cell viability on O‐MDAACS was about 12% and 59% higher than those on chitosan and on control, respectively. © 2012 Society of Chemical Industry     

Synthesis and Antimicrobial Evaluation of Bis-morpholine Triazine Quaternary Ammonium Salts

Efficient, environmentally and economically sustainable, and nontoxic antibacterial products are of global relevance in the fight against microorganism contamination. In this work, an easy and straightforward method for the synthesis of bis-morpholino triazine quaternary ammonium salts (bis-mTQAS) is reported, starting from 2,4,6-trichloro-1,3,5-triazine or 2,4-dichloro-6-methoxy-1,3,5-triazine and various N-alkylmorpholines. Bis-mTQAS were tested as antimicrobials against Gram-negative and Gram-positive bacterial strains. The best-performing bis-mTQAS were found to achieve total disinfection against Staphylococcus aureus ATCC 25923 and Escherichia coli ATCC 25922 at 50 and 400 μg/mL, respectively. Distinctively, bis-mTQAS with the highest antimicrobial efficiency had lowest cytotoxicity.     

Antibacterial activity of novel insoluble bead‐shaped polymer‐supported multiquaternary ammonium salts

This study describes the effect of antibacterial activity of newly reported five different novel insoluble bead‐shaped polymer‐supported multiquaternary ammonium salts (PM quats) viz., bis‐quat, tris‐quat (2 Nos.), tetrakis‐quat, hexakis‐quat containing two, three, four, and six quaternary ammonium groups, respectively. The presence of number of quaternary ammonium groups in each salt was established already through Fourier‐transform infrared spectroscopy, thermogravimetric analysis, scanning electron microscopy, and chloride ion analyzes. The antibacterial activities of these five different PM quats against three different bacteria viz., Staphylococcus aureus, Klebsiella pneumoniae, and Pseudomonas aeruginosa were investigated by serial dilution and spread plate method and compared the same with a monoquat containing single quaternary ammonium group. The extent of antibacterial activity has been measured in terms of colony forming units (CFU) at different time intervals. The observed results show that all the PM quats exhibited excellent‐antibacterial activity against each bacterium. On the basis of the CFU values, the antibacterial activity was found to increase from bis‐quat to hexakis‐quat, which reveals that the activity of PM quats increases with increase in the number of quaternary ammonium groups. The mechanism of interaction of quats with bacterial cytoplasmic membrane has been explained as an adsorption‐like phenomenon. The reusability of highly active hexakis‐quat against Staphylococcus aureus was studied and the activity was found to reduce after first cycle. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010     

Novel Acyl Phosphate Mimics that Target PlsY,an Essential Acyltransferase in Gram‐Positive Bacteria

PlsY is a recently discovered acyltransferase that executes an essential step in membrane phospholipid biosynthesis in Gram‐ positive bacteria. By using a bioisosteric replacement approach to generate substrate‐based inhibitors of PlsY as potential novel antibacterial agents, a series of stabilized acyl phosphate mimetics, including acyl phosphonates, acyl α,α‐difluoromethyl phosphonates, acyl phosphoramides, reverse amide phosphonates, acyl sulfamates, and acyl sulfamides were designed and synthesized. Several acyl phosphonates, phosphoramides, and sulfamates were identified as inhibitors of PlsY from Streptococcus pneumoniae and Bacillus anthracis. As anticipated, these inhibitors were competitive inhibitors with respect to the acyl phosphate substrate. Antimicrobial testing showed the inhibitors to have generally weak activity against Gram‐positive bacteria with the exception of some acyl phosphonates, reverse amide phosphonates, and acyl sulfamates, which had potent activity against multiple strains of B. anthracis.     

Determination of Kinetics and the Crystal Structure of a Novel Type 2 Isopentenyl Diphosphate: Dimethylallyl Diphosphate Isomerase from Streptococcus pneumoniae

Isopentenyl diphosphate isomerase (IDI) is a key enzyme in the isoprenoid biosynthetic pathway and is required for all organisms that synthesize isoprenoid metabolites from mevalonate. Type 1 IDI (IDI‐1) is a metalloprotein that is found in eukaryotes, whereas the type 2 isoform (IDI‐2) is a flavoenzyme found in bacteria that is completely absent from human. IDI‐2 from the pathogenic bacterium Streptococcus pneumoniae was recombinantly expressed in Escherichia coli. Steady‐state kinetic studies of the enzyme indicated that FMNH₂ (K_M =0.3 μM ) bound before isopentenyl diphosphate (K_M =40 μM ) in an ordered binding mechanism. An X‐ray crystal structure at 1.4 Å resolution was obtained for the holoenzyme in the closed conformation with a reduced flavin cofactor and two sulfate ions in the active site. These results helped to further approach the enzymatic mechanism of IDI‐2 and, thus, open new possibilities for the rational design of antibacterial compounds against sequence‐similar and structure‐related pathogens such as Enterococcus faecalis or Staphylococcus aureus.     

Synthesis of Amido‐N‐imidazolium Salts and their Applications as Ligands in Suzuki–Miyaura Reactions: Coupling of Hetero‐ aromatic Halides and the Synthesis of Milrinone and Irbesartan

A new catalytic system based on palladium‐amido‐N‐heterocyclic carbenes for Suzuki–Miyaura coupling reactions of heteroaryl bromides is described. A variety of sterically bulky, amido‐N‐imidazolium salts were synthesized in high yields from the corresponding anilines. This catalytic system effectively promoted Suzuki–Miyaura couplings of heteroaryl bromides and chlorides with a range of boronic acids to give the corresponding aryl compounds in high yield. The yield was increased with increasing steric bulkiness of the substituted group. Especially, 1‐(2,6‐diisopropylphenyl)‐3‐N‐(2,4,6‐tri‐tert‐butylphenylacetamido)imidazolium bromide ( 4bc ) exhibited 850,000 TON in the coupling reaction of 2‐bromopyridine and phenylboronic acid. In addition, pharmaceutical compounds such as milrinone and irbesartan were synthesized via Suzuki–Miyaura coupling using sterically bulky, amido‐N‐imidazolium salt ( 4bc ) as a ligand.     

Preparation and properties of silver‐containing nylon 6 nanofibers formed by electrospinning

Nylon 6 nanofibers containing silver nanoparticles (nylon 6/silver) were successfully prepared by electrospinning. The structure and properties of the electrospun fibers were studied with the aid of scanning electron microscopy, transmission electron microscopy, energy‐dispersive spectroscopy, and X‐ray diffraction. The structural analysis indicated that the fibers electrospun at maximum conditions were straight and that silver nanoparticles were distributed in the fibers. Finally, the antibacterial activities of the nylon 6/silver nanofiber mats were investigated in a broth dilution test against Staphylococcus aureus (Gram‐positive) and Klebsiella pneumoniae (Gram‐negative) bacteria. It was revealed that nylon 6/silver possessed excellent antibacterial properties and an inhibitory effect on the growth of S. aureus and K. pneumoniae. On the contrary, nylon 6 fibers without silver nanoparticles did not show any such antibacterial activity. Therefore, electrospun nylon 6/silver nanocomposites could be used in water filters, wound dressings, or antiadhesion membranes. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009     

Antibacterial and Bacterium Adsorbing Macromolecules

Currently studies on antibacterial macromolecules, i. e., bactericidal and bacteriostatic ones, have been made to develop a new utilization field of polymeric materials. In these studies, there are immobilizations of iodine to quaternary ammonium salts, antibiotics, antibacterial groups to macromolecular substances, as well as syntheses of polymers with quaternary ammonium salts, biguanide groups, quaternary pyridinium salts, sulphonium salts, phosphonium salts, and other antibacterial groups. On the other hand, studies have been made of bacterium adsorbing macromolecules, which can remove by adsorbing bacterial cells in water. The macromolecules are the ones based on poly(4‐vinylpyridine‐co‐divinylbenzene), crosslinked poly(3‐ and 4‐chloromethylated styrene‐g‐amine), and poly(glycidyl methacrylate‐g‐amine), as well as filters and microporous membranes are covered with a macromolecule based on quaternized poly(4‐vinylpyridine‐co‐styrene). Here, a review is made of the syntheses and preparation of the respective macromolecules, as well as of their antibacterial activities and the bacterium adsorbing activities.     

Harnessing Multiple,Nonproteogenic Substitutions to Optimize CSP:ComD Hydrophobic Interactions in Group 1 Streptococcus pneumoniae

Streptococcus pneumoniae (pneumococcus) is a human pathobiont that causes drastic antibiotic-resistant infections and is responsible for millions of deaths universally. Pneumococcus pathogenicity relies on the competence-stimulating peptide (CSP)-mediated quorum-sensing (QS) pathway that controls competence development for genetic transformation and, consequently, the spread of antibiotic resistance and virulence genes. Modulation of QS in S. pneumoniae can therefore be used to enervate pneumococcal infectivity as well as minimize the susceptibility to resistance development. In this work, we sought to optimize the interaction of CSP1 with its cognate transmembrane histidine kinase receptor (ComD1) through substitution of proteogenic and nonproteogenic amino acids on the hydrophobic binding face of CSP1. The findings from this study not only provided additional structure–activity data that are significant in optimizing CSP1 potency, but also led to the development of potent QS modulators. These CSP-based QS modulators could be used as privileged scaffolds for the development of antimicrobial agents against pneumococcal infections.     

Development of Streptococcus pneumoniae Pan-Group Quorum-Sensing Modulators

The rapid increase in multidrug-resistant pathogens is a major health concern that could bring mankind back to the pre-antibiotic era. Streptococcus pneumoniae is a highly recombinogenic opportunistic pathogen that causes a variety of deadly diseases and rapidly develops resistance to current antibiotic treatments. S. pneumoniae pathogenicity is dependent on a cell-density communication mechanism, or quorum sensing (QS), termed the competence regulon. In this work, we set out to design signal-based QS modulators capable of affecting the two specificity groups found in S. pneumoniae. Through systematic analysis and rational design, we were able to construct peptide-based pan-group QS activators and inhibitors with activities in the nanomolar range. These novel analogues are privileged scaffolds for the development of anti-virulence therapeutics against S. pneumoniae infections.     

Preparation of iodine containing quaternary amine methacrylate copolymers and their contact killing antimicrobial properties

A novel quaternary amine methacrylate monomer (QAMA) was synthesized by amination of dimethacrylate with piperazine followed by its quaternization using an alkyl iodide. Copolymerization of QAMA with 2‐hydroxyethyl methacrylate was carried out by free radical bulk polymerization technique at room temperature using ammonium persulfate and N,N,N′,N′‐tetramethyl ethylenediamine as a redox initiator. The monomer as well as copolymers was characterized by FTIR and ¹H NMR spectral studies. Thermal and physical characteristics of copolymers of varying compositions of QAMA were evaluated by thermogravimetric analysis, differential calorimetry, contact angle and scanning electron microscopy. The antibacterial activity of the synthesized quaternary amine dimethacrylate copolymers against Escherichia coli and Staphylococcus aureus was studied by zone of inhibition and colony count method. QAMA copolymers showed broad‐spectrum contact killing antibacterial properties without releasing any active agent as checked by iodide‐selective ion meter. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 102: 1038–1044, 2006     

Evaluation of antibacterial effects of contemporary orthodontic bonding materials

Aim: The aim of this study was to evaluate the antibacterial effects of five orthodontic bonding materials commonly used in orthodontics. Materials and Methods: The antibacterial effects of five orthodontic bonding materials were evaluated against Streptococcus mutans and Streptococcus salivarius by direct contact test (DCT). Using the DCT technique, quintet specimens of Transbond XT, Blugloo, Grengloo, Light Bond, and Opal Bond were applied to the bottom and the walls of the five wells of a 96-microtiter plate with a height of 2 mm. Samples were prepared in two sets: 1-day samples and 7-day samples. Ten microliters of bacterial suspension were added to each well for direct contact with each material for 1h at 37 °C. Bacterial growth was then measured in a microplate spectrophotometer hourly at 600 nm for 24 h. Five uncoated wells with identical inoculum sizes served as positive controls. The data obtained at the end of 24 h was statistically analyzed with one-way ANOVA, and post hoc comparisons were done using Tamhane’s T2 test. Results: Blugloo generally showed better antibacterial activity than the other materials. Transbond XT did not show any antibacterial activity. There was a statistically significant difference between Transbond XT and Light Bond in the 1-day sample against S. mutans (p < 0.05). No statistically significant differences were found among the other groups (p > 0.05). Conclusion: Blugloo had the most potent antibacterial activity against S. salivarious.     

Synthesis and water absorbency of polyampholytic hydrogels with antibacterial activity

Amphoteric terpolymers of acrylic acid (AA), acrylamide (AM), and N,N′‐dimethyl‐N‐ethylmeth‐acryloxylethylammoniumbromide (DMAEA‐EB) with varied compositions P[AA‐AM‐(DMAEA‐EB)] were synthesized by inverse suspension polymerization. The components of P[AA‐AM‐(DMAEA‐EB)] were verified by FTIR spectroscopy. The water absorption ability and antibacterial activity of the copolymer against Escherichia coli(E. coli) and Staphylococcus hyicus(S. hyicus) suspended in sterilized physiological saline were investigated. The introduction of  N⁺R₄ may increase the water absorbency of P[AA‐AM‐(DMAEA‐EB)] in some degree because of the excellent hydrophilicity of  N⁺R₄. The AA‐AM‐(DMAEA‐EB) hydrogels exhibited high antibacterial activity against bacteria tested. The process of adsorption between live bacteria cells and resins was at least partially reversible. A peak of antibacterial efficiency existed with increasing contact time. The resin killed 96.6% E. coli organisms and 90.3% S. hyicus organisms, respectively, within 30 min of contact at dosage of 0.1g. The concentration of DMAEA‐EB has a special effect on the antibacterial activity of the polyampholytic hydrogels, which is different from polycation. It was observed that the antibacterial activity of the resin with 2 mol % of DMAEA‐EB is superior to the copolymers tested with other compositions. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009     

Electrospun Sandwich‐Structure Composite Membranes for Wound Dressing Scaffolds with High Antioxidant and Antibacterial Activity

In this study, the sandwich‐structured composite (SSC) membranes with well‐antibacterial and antioxidant properties, which have the promising application as wound dressing, are successfully fabricated by combining an electrospinning process. The SSC membranes are composed of three layers, including the bottom polyvinylidene fluoride fibrous layer, the middle curcumin/polylactic acid (PLA) microsphere layer, and the top enrofloxacin/PLA fibrous layer, respectively. The obtained SSC membranes are characterized in terms of morphology, component, and mechanical property using scanning electronic microscope, X‐ray diffractometer, Fourier transform infrared spectroscopy, and universal electronic testing machine, respectively. Moreover, in vitro drug release, antioxidant activity, antimicrobial activity, and biocompatibility of the SSC membranes are also evaluated. The results showed that the obtained composite membranes indeed possess the sandwich structure, where the middle microsphere layer is located between two fibrous surface layers. It is found that the drug‐loaded SSC membranes show excellent antioxidant activity against ^?OH and DPPH free radicals and antibacterial activity against Staphylococcus aureus, Escherichia coli, Streptococcus pneumoniae, Pseudomonas aeruginosa, and Candida albicans. The combination of electrospinning and electrospraying opens up a new way to fabricate a variety of composite membranes with a sandwich structure, which have promising potential application as wound dressing scaffolds.     

Synthesis and Properties of Organosilicon Quaternary Salts Surfactants

Diethyl-benzyl-[3-methyldimethoxyl)]silpropyl ammonium chloride (DEBSAC) was synthesized from N,N-diethyl-aminopropyl-methyldimethoxysilane (DEAPMDES) and benzyl chloride. Diethyl-2,3-epoxypropyl-[3-methyldimethoxyl)] silpropyl ammonium chloride (DEEPSAC) was synthesized from DEAPMDES and epoxy chloropropane. Trimethyl-[3-methyldimethoxyl)] silpropyl ammonium chloride (TMSAC) was synthesized from trimethylamine and γ-chloropropylmethyldimethoxysilane (CPMDMS). The products were characterized by ¹H NMR, ¹³C NMR, and IR. The surface tension measurements showed that the organosilicon quaternary salts exhibit a lower surface tension and a lower critical micelle concentration (CMC) than the hydrocarbon counterparts. The plate count method experiments illustrated that DEEPSAC has a better degree of antibacterial activity against Escherichia coli than DEBSAC. The solubilizing effects of the organosilicon quaternary salts on organosilicone were studied by pseudo-ternary phase diagrams of synthesized products/cosurfactant(n-butanol)/water/octamethylcyclotetrasiloxane. The solubilizing activities decreased in the order of TMSAC > DEBSAC > DEEPSAC.     

Effects of trans‐10,cis‐12 and cis‐9,trans‐11 CLA on atherosclerosis in apoE/LDLR−/− mice

The objective of our studies was to verify the potential health‐related, anti‐atherogenic potency of CLA isomers, fed to apolipoprotein E and LDL receptor double knockout mice (apoE/LDLR^?/?), representing a reliable model of atherogenesis. Additionally, the effect of CLA isomers on liver steatosis was observed. In a “long experiment” (LONG), 2‐month‐old mice with no atherosclerosis were randomly assigned to three experimental groups and fed for the next 4 months. In a “short experiment” (SHORT), 4‐month‐old mice, with pre‐established atherosclerosis, were randomly assigned to three experimental groups and fed for the next 2 months. The experimental diets were: AIN‐93G (control), AIN‐93G + 0.5% trans‐10,cis‐12 CLA (t10,c12), and AIN‐93G + 0.5% cis9,trans‐11 CLA (c9,t11). In both experiments, c9,t11 CLA increased mice body weight. In mice fed t10,c12 CLA weight of liver was threefold (p<0.05) increased what was linked with hepatic steatosis observed in LONG and SHORT experiment. In LONG experiment, t10,c12 CLA significantly (p<0.05) increased plasma TAGs, whereas no such effect was observed in SHORT one. In mice receiving the CLA isomers the level of PPARα and SREBP‐1 mRNA in liver were significantly decreased. The expression of their target genes like ACO (PPARα) or FAS (SREBP‐1) were not changed. Only c9,t11 increased ACO level in LONG experiment. There were no isomer‐specific effects of CLA isomers on the area of atherosclerotic plaque. In conclusion, our results do not support the notion that CLA isomers supplementation to the diet has anti‐atherosclerotic effects. CLA isomers have no effect on atherosclerosis in apoE/LDLR^?/? mice. Practical applications: CLAs have been shown to occur naturally in food. In the last 10 years, attempts have been made to enrich animal‐derived foods in CLA isomers through animal nutrition strategies. Indeed, these attempts resulted in production of functional food such as CLA‐enriched milk (butter and cheese), ruminant and non‐ruminant meat, as well as eggs. In addition to natural foodstuff, dietary CLA supplements can also contribute to CLA intake in humans. Commercial CLA preparations, fed to laboratory animals, showed several health‐related properties, including anti‐adipogenic, anti‐carcinogenic, anti‐atherogenic, and anti‐inflammatory effects. The underlying mechanisms of action, however, are only poorly understood. The major objective of our studies was to verify the potential health‐related, namely anti‐atherogenic potency of CLA isomers, fed to apoE/LDLR^?/? mice, representing unique and reliable model of atherogenesis. Additionally, effect of CLA isomers on steatosis was observed.