Bioactivity of Backhousia citriodora: antibacterial and antifungal activity

Backhousia citriodora products are used as bushfoods and flavorings and by the aromatherapy industry. The antimicrobial activity of 4 samples of B. citriodora oil, leaf paste, commercial tea (0.2 and 0.02 g/mL), and hydrosol (aqueous distillate) were tested against 13 bacteria and 8 fungi. Little or no activity was found to be associated with the leaf tea and hydrosol, respectively. Leaf paste displayed antimicrobial activity against 7 bacteria including Clostridium perfringens, Pseudomonas aeruginosa, and a hospital isolate of methicillin resistant Staphylococcus aureus (MRSA). The 4 essential oils were found to be effective antibacterial and antifungal agents; however, variation was apparent between oils that did not correlate with citral content. The antimicrobial activity of B. citriodoraessential oils was found to be greater than that of citral alone and often superior to Melaleuca alternifolia essential oil. B. citriodora has significant antimicrobial activity that has potential as an antiseptic or surface disinfectant or for inclusion in foods as a natural antimicrobial agent.     

Nanoparticles synthesized from soy protein: preparation, characterization, and application for nutraceutical encapsulation

Nanoparticles were synthesized from soy protein, one of the most abundant and widely utilized plant proteins, for nutraceutical and drug encapsulation. The preparation process consisted of dispersion, desolvation, drug incorporation, cross-linking, and evaporation. The role of each procedure in the formation of nanoparticles was systematically investigated by means of particle size, size distribution, and zeta potential as well as morphology observation. Curcumin as a model drug was encapsulated successfully into the nanoparticles, evidenced by Fourier transform infrared spectroscopy and X-ray diffraction patterns. The average size of the curcumin-loaded nanoparticles was 220.1 to 286.7 nm, and their zeta potential was around -36 mV. The highest encapsulation efficiency and loading efficiency achieved were 97.2% and 2.7%, respectively. The release of curcumin in phosphate buffer saline followed a biphasic pattern. Possible mechanisms of the formation of soy protein nanoparticles as well as the incorporation of curcumin were discussed based on the data obtained from this study.     

Antibacterial activity of Coriandrum sativum L. and Foeniculum vulgare Miller Var. vulgare (Miller) essential oils

Essential oils were extracted from the fruits of Coriandrum sativum L. and Foeniculum vulgare Miller var. vulgare (Miller) and assayed in vitro for antibacterial activity to Escherichia coli and Bacillus megaterium, bacteria routinely used for comparison in the antimicrobial assays, and 27 phytopathogenic bacterial species and two mycopathogenic ones responsible for cultivated mushroom diseases. A significant antibacterial activity, as determined with the agar diffusion method, was shown by C. sativum essential oil whereas a much reduced effect was observed for F. vulgare var. vulgare oil. C. sativum and F. vulgare var. vulgare essential oils may be useful natural bactericides for the control of bacterial diseases of plants and for seed treatment, in particular, in organic agriculture. The significant antibacterial activity of essential oils to the bacterial pathogens of mushrooms appears promising.     

不同乳化剂对姜黄素乳液理化稳定性的影响

姜黄素具有许多生物活性功能,但较差的溶解度和稳定性限制了其在食品和医药领域的应用。为筛选出具有良好稳定性的姜黄素乳液,本研究以亚麻籽油为姜黄素的油相载体,经高压均质法制备出姜黄素乳液中研究卵磷脂、吐温-80、阿拉伯胶和乳清分离蛋白4种食品级乳化剂对姜黄素乳液的理化特性和贮藏稳定性的影响,从包埋率、浊度、粒径、电位等方面进行稳定性评价。结果表明,吐温-80稳定的姜黄素乳液中姜黄素包埋率较高(76.98%),浊度和平均粒径最小,分别为848.0 NTR、214.23±1.52 nm;同时在贮藏期内姜黄素乳液的平均粒径变化最小,增长不到1%,贮藏稳定性表现良好。同时,4℃低温条件下姜黄素保留率最高,达到88.02%。结果表明,选用吐温-80作为乳化剂,姜黄素乳液具有最好的溶解性和稳定性,这为今后姜黄素在食品工业中的广泛应用提供了新思路。     

短链葡聚糖-姜黄素纳米乳液的制备及结构表征

利用短链葡聚糖(short glucan chains,SGC)的螺旋空间结构来包埋姜黄素(curcumin,CUR)。通过使用高剪切分散乳化机高速剪切溶液5 min,用纳米均质机在50 MPa压力下高压均质经剪切后的乳液2次制备成纳米乳液以提高其包埋率和载药量。XRD (x-ray diffraction)和TGA (thermogravimetric analysis)很好的验证了包合物的形成,通过TGA、SEM (scanning electron microscopy)、激光粒径分析仪等各种表征分析得出短链葡聚糖-姜黄素纳米乳液制备成功,所制得的乳液对姜黄素的包埋率和载药量都高于短链葡聚糖-姜黄素包合物,分别达到了71.11%和12.07%,说明制备成纳米乳液对姜黄素的包埋率和载药量都有了明显的提高。所制备的纳米乳液的粒径小于300 nm,粒径分布均一,Zeta电位观测表明所制得的乳液的稳定性有所提高。为提高食品及医药领域姜黄素的生物利用率提供了一定的参考意义。     

Chemical composition and antibacterial activity of the essential oil and the gum of Pistacia lentiscus Var. chia

The essential oil and gum of Pistacia lentiscus var. chia, commonly known as the mastic tree, are natural antimicrobial agents that have found extensive uses in medicine in recent years. In this work, the chemical composition of mastic oil and gum was studied by GC-MS, and the majority of their components was identified. alpha-Pinene, beta-myrcene, beta-pinene, limonene, and beta-caryophyllene were found to be the major components. The antibacterial activity of 12 components of mastic oil and the oil itself was evaluated using the disk diffusion method. Furthermore, attempts were made to separate the essential oil into different fractions in order to have a better picture of the components responsible for its antibacterial activity. Several trace components that appear to contribute significantly to the antibacterial activity of mastic oil have been identified: verbenone, alpha-terpineol, and linalool. The sensitivity to these compounds was different for different bacteria tested (Escherichia coli, Staphylococcus aureus, and Bacillus subtilis), which suggests that the antibacterial efficacy of mastic oil is due to a number of its components working synergistically. The establishment of a correlation between the antibacterial activity of mastic oil and its components was the main purpose of this research. Mastic gum was also examined, but it proved to be more difficult to handle compared to the essential oil.     

Fermentation enhances the biological activity of Allium cepa bulb extracts

In this study, we compared the analytical fingerprint and bioactivity of three onion extracts, including an aqueous, a methanol, and a fermented aqueous extract. The extracts were characterized by HPLC-DAD, LC-MS, and GC-MS analyses. The antibacterial, antigenotoxic, and antiproliferative activity of these extracts was assessed by means of agar disk diffusion, bacterial growth kinetics, a comet assay, cell cycle distribution analysis, and cell viability testing. Both the aqueous and methanolic extracts showed a typical flavonol-fingerprint as assessed by HPLC measurements and showed little to no bioactivity. The fermented aqueous extract, which lacks the usual onion flavonoid profile, was found to be the most active in all of the assays. This finding indicates that metabolites of onion compounds, generated by lactic acid fermentation, may be more active than their precursor substances.     

Human lysozyme possesses novel antimicrobial peptides within its N-terminal domain that target bacterial respiration

Human milk lysozyme is thought to be a key defense factor in protecting the gastrointestinal tract of newborns against bacterial infection. Recently, evidence was found that pepsin, under conditions relevant to the newborn stomach, cleaves chicken lysozyme (cLZ) at specific loops to generate five antimicrobial peptide motifs. This study explores the antimicrobial role of the corresponding peptides of human lysozyme (hLZ), the actual protein in breast milk. Five peptide motifs of hLZ, one helix-loop-helix (HLH), its two helices (H1 and H2), and two helix-sheet motifs, H2-β-strands 1-2 (H2-S12) or H2-β-strands 1-3 (H2-S13), were synthesized and examined for antimicrobial action. The five peptides of hLZ exhibit microbicidal activity to various degrees against several bacterial strains. The HLH peptide and its N-terminal helix (H1) were significantly the most potent bactericidal to Gram-positive and Gram-negative bacteria and the fungus Candida albicans . Outer and inner membrane permeabilization studies, as well as measurements of transmembrane electrochemical potentials, provided evidence that HLH peptide and its N-terminal helix (H1) kill bacteria by crossing the outer membrane of Gram-negative bacteria via self-promoted uptake and are able to dissipate the membrane potential-dependent respiration of Gram-positive bacteria. This finding is the first to describe that hLZ possesses multiple antimicrobial peptide motifs within its N-terminal domain, providing insight into new classes of antibiotic peptides with potential use in the treatment of infectious diseases.     

Characterization, antibiofilm, and mechanism of action of novel PEG-stabilized lipid nanoparticles loaded with terpinen-4-ol

Terpinen-4-ol, an active component of tea tree oil, exhibits broad-spectrum antimicrobial activity. However, the high volatilization of terpinen-4-ol and its nonwettability property have limited its application. Our objective was to synthesize novel nanocarriers to deliver and protect terpinen-4-ol. The polyethylene glycol (PEG)-stabilized lipid nanoparticles were prepared and characterized by scanning electron microscope, Zetasizer, and differential scanning calorimetry. These nanoparticles had an average diameter of 397 nm and a Ζ-potential of 10 mV after being modified by glycine. Results showed that homogeneous particle size, high drug loading, stability, and targeting were obtained by the nanoparticles. Liquid chromatography/mass spectrometry showed a sustained release trend from nanoparticles for terpinen-4-ol. Minimum inhibitory concentration and minimum biofilm eradication concentration were tested against Candida albicans ATCC 11231. Studies on isolated mitochondria showed the blockage of biofilm respiration and inhibition of enzyme activity. The effects can be ascribed to localization of terpinen-4-ol on the membrane of mitochondria.     

Preparation and enhancement of oral bioavailability of curcumin using microemulsions vehicle

A new microemulsions system of curcumin (CUR-MEs) was successfully developed to improve the solubility and bioavailability of curcumin. Several formulations of the microemulsions system were prepared and evaluated using different ratios of oils, surfactants, and co-surfactants (S&CoS). The optimal formulation, which consists of Capryol 90 (oil), Cremophor RH40 (surfactant), and Transcutol P aqueous solution (co-surfactant), could enhance the solubility of curcumin up to 32.5 mg/mL. The pharmacokinetic study of microemulsions was performed in rats compared to the corresponding suspension. The stability of microemulsions after dilution was excellence. Microemulsions have significantly increased the C(max) and area under the curve (AUC) in comparison to that in suspension (p < 0.05). The relative bioavailability of curcumin in microemulsions was 22.6-fold higher than that in suspension. The results indicated that the CUR-MEs could be used as an effective formulation for enhancing the oral bioavailability of curcumin.     

Isolation, identification, and quantification of roasted coffee antibacterial compounds

Coffee brew is a widely consumed beverage with multiple biological activities due both to naturally occurring components and to the hundreds of chemicals that are formed during the roasting process. Roasted coffee extract possesses antibacterial activity against a wide range of microorganisms, including Staphylococcus aureus and Streptococcus mutans, whereas green coffee extract exhibits no such activity. The naturally occurring coffee compounds, such as chlorogenic acids and caffeine, cannot therefore be responsible for the significant antibacterial activity exerted by coffee beverages against both bacteria. The very low minimum inhibitory concentration (MIC) found for standard glyoxal, methylglyoxal, and diacetyl compounds formed during the roasting process points to these alpha-dicarbonyl compounds as the main agents responsible for the antibacterial activity of brewed coffee against Sa. aureus and St. mutans. However, their low concentrations determined in the beverage account for only 50% of its antibacterial activity. The addition of caffeine, which has weak intrinsic antibacterial activity, to a mixture of alpha-dicarbonyl compounds at the concentrations found in coffee demonstrated that caffeine synergistically enhances the antibacterial activity of alpha-dicarbonyl compounds and that glyoxal, methylglyoxal, and diacetyl in the presence of caffeine account for the whole antibacterial activity of roasted coffee.     

蒲公英不同部位抑菌作用及代谢物差异的UPLC-MS/MS分析

为了研究蒲公英不同部位抑菌作用和代谢物成分的差异,本物采用打孔法和超高效液相色谱串联质谱(UPLC-MS/MS)方法,研究了蒲公英根、茎叶和花的水提取物和醇提取物对5种致病菌的抑菌作用,并对不同部位的代谢物成分进行了定性和定量分析。结果表明,蒲公英不同部位初提取物对变形杆菌、嗜根考克氏菌和枯草芽孢杆菌均有抑菌作用,而对大肠杆菌和铜绿假单胞菌均无抑菌作用;醇提法的抑菌效果优于水提法,花提取物的抑菌活性最强,根最弱。蒲公英的不同部位共鉴定出449种代谢物,根、茎叶和花中相对含量最高的物质分别为反油酸(脂类)、γ-亚麻酸(脂类)和木犀草素(黄酮类);且根、茎叶和花中相对含量排名前20的物质中黄酮类分别有0种、3种和8种,表明黄酮类物质可能是蒲公英中的主要抑菌活性物质。正交偏最小二乘法-判别分析(OPLS-DA)结果显示,木犀草素-7-O-葡萄糖苷在花中上调幅度最大,橙皮素C-丙二酰己糖苷为根中特有物质。本研究结果为利用蒲公英不同部位研制和开发新型药物提供了理论依据。     

Enzyme-assisted processing increases antimicrobial and antioxidant activity of bilberry

The effects of nine cell wall-degrading enzymes on the antimicrobial and antioxidant activities of bilberry were studied. Antimicrobial activity was measured using the human pathogens Salmonella enterica sv. Typhimurium and Staphylococcus aureus as test strains. Enzyme treatments liberated phenolics from the cell wall matrix, which clearly increased the antimicrobial activity of berry juices, press cakes, and berry mashes on the basis of plate counts. Antibacterial effects were stronger against Salmonella than against Staphylococcus bacteria. In general, the increase in activity measured as colony-forming units per milliliter was 3-5 logarithmic units against Salmonella and 1-2 units against Staphylococcus bacteria. Increase in antimicrobial activity was observed only in acidic conditions, which is also the natural environment in various berry products, such as juices. The activity profile of the pectinase preparation affected the chemistry of the phenolics due to the presence of deglycosylating activities in some preparations. The difference in phenolic profiles was reflected in the antimicrobial effects. Bilberry mashes treated with Pectinex Ultra SP-L, Pectinex 3 XL, and Pectinex BE XXL were most efficient against Salmonella bacteria, whereas mashes treated with Pectinex Smash, Pectinex BE 3-L, and Biopectinase CCM showed the strongest antimicrobial activity against Staphylococcus bacteria. Due to the liberation of phenolics from the cell wall matrix the antioxidant activity measured as radical scavenging activity was also increased on average about 30% by the enzymatic treatments. The highest increase in phenolic compounds was about 40%. Highest increases in anthocyanins and in antioxidant activity were observed in berry mash treated with Pectinex Smash XXL enzyme, and the lowest increase was observed after treatment with Pectinex BE 3-L. Enzyme-assisted processing is traditionally used to improve berry and fruit juice yields. However, enzymatic treatments also have an impact on the functional properties of the products. The increased liberation of phenolics from the cell wall matrix can prolong the shelf life of berry products by limiting the growth of contaminants during processing or storage. The increased amount of phenolic compounds may also have a positive effect on gut well-being.     

Curcuma longa L. constituents inhibit sortase A and Staphylococcus aureus cell adhesion to fibronectin

The inhibitory activity of Curcuma longa L. (turmeric) rhizome constituents against sortase A, a bacterial surface protein anchoring transpeptidase, from Staphylococcus aureus ATCC 6538p was evaluated. The activity of the isolated compounds (1-4) was compared to that of the positive control,p-hydroxymecuribenzoic acid (pHMB). The biologically active components of C. longa rhizome were characterized by spectroscopic analysis as the curcuminoids curcumin (1), demethoxycurcumin (2), and bisdemethoxycurcumin (3). Curcumin was a potent inhibitor of sortase A, with an IC50 value of 13.8 +/- 0.7 microg/mL. Bisdemethoxycurcumin (IC50 = 31.9 +/- 1.2 microg/mL) and demethoxycurcumin (IC50 = 23.8 +/- 0.6 microg/mL) were more effective than pHMB (IC50 = 40.6 +/- 1.2 microg/mL). The three isolated compounds (1-3) showed no growth inhibitory activity against S. aureus strain Newman, with minimum inhibitory concentrations (MICs) greater than 200 microg/mL. Curcumin also exhibited potent inhibitory activity against S. aureus cell adhesion to fibronectin. The suppression of fibronectin-binding activity by curcumin highlights its potential for the treatment of S. aureus infections via inhibition of sortase activity. These results indicate that curcumin is a possible candidate in the development of a bacterial sortase A inhibitor.     

New bioactive biomaterials based on quaternized chitosan

Chitosan was chemically modified to produce quaternary ammonium salts in order to improve its antimicrobial activity and physicochemical properties. Quaternization of N-alkyl chitosan derivatives was carried out using alkyl iodide to elaborate water-soluble cationic polyelectrolytes ( N, N, N-trimethylchitosan, TMC). TMC was characterized by (1)H NMR spectroscopy; the quaternization degree was determined from (1)H NMR spectra and by titration of iodide ion. The antibacterial activity of hydroxypropylcellulose (HPC) films or coatings associated with chitosan or TMC as biocide was evaluated against the growth of Listeria monocytogenes and Salmonella typhimurium. The HPC-chitosan and HPC-TMC coatings exhibited a total inhibition on solid medium of both bacterial strains. Experiments conducted in liquid medium showed that the inhibitory activity against the growth of Listeria innocua was improved after chemical modification. Moreover, physicochemical properties of films were evaluated to determine their potential for food applications. The addition of the antibacterial agents showed a significant impact on the moisture barrier and mechanical properties of HPC films.     

Antioxidant activity of Myristica malabarica extracts and their constituents

The 1,1-diphenyl-2-picrylhydrazyl (DPPH) assay of the ether, methanol, and aqueous extracts of the spice Myristica malabarica (rampatri) revealed the methanol extract to possess the best antioxidant activity. Column chromatography of the methanol extract led to the isolation of a new 2-acylresorcinol and four known diarylnonanoids of which the diarylnonanoid, malabaricone C, showed the maximum DPPH scavenging activity. Malabaricone C could prevent both Fe(II)- and 2,2'-azobis(2-amidinopropane)dihydrochloride-induced lipid peroxidation (LPO) of rat liver mitochondria more efficiently than curcumin. The anti-LPO activity of malabaricone C was attributed to its better radical scavenging and Fe(II) chelation capacities. The superior activity of malabaricone C was rationalized by a systematic structure-activity correlation of the results obtained with the structurally related diarylnonanoids and curcumin. Malabaricone C also prevented the gamma-ray-induced damage of pBR322 plasmid DNA in a concentration-dependent manner. The radioprotective activity was found to correlate with its (*)OH radical scavenging property, which matched well with that of d-mannitol.     

Modification of curcumin with polyethylene glycol enhances the delivery of curcumin in preadipocytes and its antiadipogenic property

Conjugation of curcumin (CCM) by polyethylene glycol (PEG) has been previously developed to improve water solubility of the natural form of CCM and its antiproliferative role in some human cancer cell lines. This study examined the cellular uptake kinetics of the natural form of CCM and CCM-PEG. Their cytotoxic effect in proliferating preadipocytes and antiadipogenic property in differentiating preadipocytes had also been investigated. CCM and CCM-PEG were found to be differently absorbed in 3T3-L1 preadipocytes and adipocytes with a limited amount of CCM-PEG absorption in the cell. The improved water solubility of CCM-PEG was correlated with increased cellular retention of CCM in 3T3-L1 cells, particularly in preadipocytes. Consequently, CCM-PEG treatment sensitized proliferating preadipocytes to CCM-induced cell toxicity. Furthermore, incubation of differentiating 3T3-L1 cells with CCM-PEG resulted in improvement of the inhibitory role of CCM in adipocyte differentiation with no toxic effect. These results suggest that pegylation-improved water solubility and cellular retention of CCM may be uniquely useful for improving the delivery of CCM in preadipocytes and its antiadipogenic ability.     

Synthetic porcine lactoferricin with a 20-residue peptide exhibits antimicrobial activity against Escherichia coli, Staphylococcus aureus, and Candida albicans

Lactoferricins are positively charged, highly basic peptides that are generated upon gastric pepsin cleavage of various lactoferrins. In the past decade, there has been active investigation of the key antimicrobial segments of the various shorter synthetic bovine and human lactoferricins, but not in porcine lactoferricin. These studies have demonstrated the distinct solution structures of lactoferricin in bovine and human and established the multifunctional nature of the antibacterial, antifungal, antiendotoxin, and antiviral activities of lactoferricins. However, the protective effects of porcine lactoferricins have yet to be elucidated. In the present study, a series of synthetic derivatives of porcine, bovine, and human lactoferricins with 20-residue and 9-residue peptides were prepared to investigate their antimicrobial nature. We found that the 20-residue porcine lactoferricin (LFcin P-20) displayed antimicrobial activity against Escherichia coli ATCC25922, Staphylococcus aureus ATCC25923, and Candida albicans ATCC14053. The minimal inhibitory concentrations and minimal bactericidal concentrations of LFcin P-20 ranged from 12 to 25 microM when tested in bacteria and fungi. LFcin P-20 was 4 times more effective than human lactoferricin (LFcin H-20), but slightly less effective than bovine lactoferricin (LFcin B-20).     

玉米醇溶蛋白-壳聚糖纳米营养递送粒子的制备及性质

利用蛋白质和多糖构建纳米营养递送载体，是提高食品活性物质稳定性及利用率的重要手段。为了构建具有缓释特性的纳米营养递送体系，该研究以玉米醇溶蛋白（zein）为基材，构建玉米醇溶蛋白-壳聚糖纳米营养递送体系，以姜黄素（Cur）为营养模型，探究了壳聚糖分子量、zein与壳聚糖质量比对纳米粒子及其负载Cur性能的影响，通过扫描电子显微镜（Scanning Electron Microscope，SEM）、傅里叶红外光谱（Fourier Transform Infrared Spectroscopy，FTIR）等方法表征其结构，阐明复合纳米粒子形成机制，探讨其稳定性和缓释性能。结果表明：不同分子量的壳聚糖对纳米粒子的粒径、多分散性指数和zeta电位有影响。高分子量壳聚糖的加入可使纳米粒子粒径减小，且更加稳定。在zein与高分子量壳聚糖质量比为8∶1时，制备纳米粒子粒径较小（80.13 nm），其zeta电位为46.18 mV；在此条件下，当姜黄素添加量为1.0%时，其包封率和负载量分别为82.93%和8.29%；通过SEM观察，纳米粒子呈球形，分布均匀；氢键及静电相互作用是组装该纳米粒子的作用力；壳聚糖的引入提高了纳米粒子的pH值、离子及储藏稳定性，扩展了其应用范围；与游离的姜黄素相比，纳米营养递送粒子呈现明显的缓释特性。研究结果为构建具有缓释特性的营养递送体系提供了理论基础。     

Main antimicrobial compounds in table olives

The inhibitors involved in the lactic acid fermentation of table olives were investigated in aseptic olive brines of the Manzanilla and Gordal varieties. Phenolic and oleosidic compounds in these brines were identified by high-performance liquid chromatography with ultraviolet and electrospray ionization mass spectrometry detection, and several substances were also characterized by nuclear magnetic resonance. Among these compounds, the dialdehydic form of decarboxymethyl elenolic acid linked to hydroxytyrosol showed the strongest antilactic acid bacteria activity, and its presence in brines could explain the growth inhibition of these microorganisms during olive fermentation. However, it was found that the dialdehydic form of decarboxymethyl elenolic acid, identified for the first time in table olives, and an isomer of oleoside 11-methyl ester were also effective against Lactobacillus pentosus and can, therefore, contribute to the antimicrobial activity of olive brines. It must also be stressed that the three new inhibitors discovered in table olive brines exerted a more potent antibacterial activity than the well-studied oleuropein and hydroxytyrosol.