Trifluoromethylcinnamanilide Michael Acceptors for Treatment of Resistant Bacterial Infections

A series of thirty-two anilides of 3-(trifluoromethyl)cinnamic acid (series 1) and 4-(trifluoromethyl)cinnamic acid (series 2) was prepared by microwave-assisted synthesis. All the compounds were tested against reference strains Staphylococcus aureus ATCC 29213 and Enterococcus faecalis ATCC 29212 and resistant clinical isolates of methicillin-resistant S. aureus (MRSA) and vancomycin-resistant E. faecalis (VRE). All the compounds were evaluated in vitro against Mycobacterium smegmatis ATCC 700084 and M. marinum CAMP 5644. (2E)-3-[3-(Trifluoromethyl)phenyl]-N-[4-(trifluoromethyl)phenyl]prop-2-enamide (1j), (2E)-N-(3,5-dichlorophenyl)-3-[3-(trifluoromethyl)phenyl]prop-2-enamide (1o) and (2E)-N-[3-(trifluoromethyl)phenyl]-3-[4-(trifluoromethyl)-phenyl]prop-2-enamide (2i), (2E)-N-[3,5-bis(trifluoromethyl)phenyl]-3-[4-(trifluoromethyl)phenyl]-prop-2-enamide (2p) showed antistaphylococcal (MICs/MBCs 0.15–5.57 µM) as well as anti-enterococcal (MICs/MBCs 2.34–44.5 µM) activity. The growth of M. marinum was strongly inhibited by compounds 1j and 2p in a MIC range from 0.29 to 2.34 µM, while all the agents of series 1 showed activity against M. smegnatis (MICs ranged from 9.36 to 51.7 µM). The performed docking study demonstrated the ability of the compounds to bind to the active site of the mycobacterial enzyme InhA. The compounds had a significant effect on the inhibition of bacterial respiration, as demonstrated by the MTT assay. The compounds showed not only bacteriostatic activity but also bactericidal activity. Preliminary in vitro cytotoxicity screening was assessed using the human monocytic leukemia cell line THP-1 and, except for compound 2p, all effective agents did show insignificant cytotoxic effect. Compound 2p is an interesting anti-invasive agent with dual (cytotoxic and antibacterial) activity, while compounds 1j and 1o are the most interesting purely antibacterial compounds within the prepared molecules.     

Synthesis and Antimicrobial Evaluation of Some Novel Thiazole,Pyridone, Pyrazole,Chromene, Hydrazone Derivatives Bearing a Biologically Active Sulfonamide Moiety

This study aimed for the synthesis of new heterocyclic compounds incorporating sulfamoyl moiety suitable for use as antimicrobial agents via a versatile, readily accessible N-[4-(aminosulfonyl)phenyl]-2-cyanoacetamide (3). The 2-pyridone derivatives were obtained via reaction of cyanoacetamide with acetylacetone or arylidenes malononitrile. Cycloaddition reaction of cyanoacetamide with salicyaldehyde furnished chromene derivatives. Diazotization of 3 with the desired diazonium chloride gave the hydrazone derivatives 13a–e. Also, the reactivity of the hydrazone towards hydrazine hydrate to give Pyrazole derivatives was studied. In addition, treatment of 3 with elemental sulfur and phenyl isothiocyanate or malononitrile furnished thiazole and thiophene derivatives respectively. Reaction of 3 with phenyl isothiocyanate and KOH in DMF afforded the intermediate salt 17 which reacted in situ with 3-(2-bromoacetyl)-2H-chromen-2-one and methyl iodide afforded the thiazole and ketene N,S-acetal derivatives respectively. Finally, reaction of 3 with carbon disulfide and 1,3-dibromopropane afforded the N-[4-(aminosulfonyl) phenyl]-2-cyano-2-(1,3-dithian-2-ylidene)acetamide product 22. All newly synthesized compounds were elucidated by considering the data of both elemental and spectral analysis. The compounds were evaluated for both their in vitro antibacterial and antifungal activities and showed promising results.     

Study of Biological Activities and ADMET-Related Properties of Novel Chlorinated N-arylcinnamamides

A series of eighteen 4-chlorocinnamanilides and eighteen 3,4-dichlorocinnamanilides were designed, prepared and characterized. All compounds were evaluated for their activity against gram-positive bacteria and against two mycobacterial strains. Viability on both cancer and primary mammalian cell lines was also assessed. The lipophilicity of the compounds was experimentally determined and correlated together with other physicochemical properties of the prepared derivatives with biological activity. 3,4-Dichlorocinnamanilides showed a broader spectrum of action and higher antibacterial efficacy than 4-chlorocinnamanilides; however, all compounds were more effective or comparable to clinically used drugs (ampicillin, isoniazid, rifampicin). Of the thirty-six compounds, six derivatives showed submicromolar activity against Staphylococcus aureus and clinical isolates of methicillin-resistant S. aureus (MRSA). (2E)-N-[3,5-bis(trifluoromethyl)phenyl]- 3-(4-chlorophenyl)prop-2-enamide was the most potent in series 1. (2E)-N-[3,5-bis(Trifluoromethyl)phenyl]-3-(3,4-dichlorophenyl)prop-2-enamide, (2E)-3-(3,4-dichlorophenyl)-N-[3-(trifluoromethyl)phenyl]prop-2-enamide, (2E)-3-(3,4-dichloro- phenyl)-N-[4-(trifluoromethyl)phenyl]prop-2-enamide and (2E)-3-(3,4-dichlorophenyl)- N-[4-(trifluoromethoxy)phenyl]prop-2-enamide were the most active in series 2 and in addition to activity against S. aureus and MRSA were highly active against Enterococcus faecalis and vancomycin-resistant E. faecalis isolates and against fast-growing Mycobacterium smegmatis and against slow-growing M. marinum, M. tuberculosis non-hazardous test models. In addition, the last three compounds of the above-mentioned showed insignificant cytotoxicity to primary porcine monocyte-derived macrophages.     

Manufacture and performance of ethylamine hydroxyethyl chitosan/cellulose fiber in N-methylmorpholine-N-oxide system

Ethylamine hydroxyethyl chitosan (EHC), a novel chitosan derivative which is soluble in aqueous N-methylmorpholine-N-oxide (NMMO) and antibacterial to Escherichia coli (E. coli) was synthesized. The structure, solubility and antibacterial capability of EHC were investigated. Results demonstrated the potential application for EHC in manufacture of antibacterial EHC/cellulose Lyocell fiber. Through environment-friendly Lyocell process in aqueous NMMO, the EHC/cellulose fiber was successfully fabricated and the various properties of EHC/cellulose fiber were studied. Results showed the EHC/cellulose fiber exhibited favorable consistency, antibacterial activity, mechanical properties and water retention compared with the fiber without EHC.     

Preparation of nylon-6/chitosan composites by nanospider technology and their use as candidate for antibacterial agents

Electrospun nylon-6/chitosan (nylon-6/Ch) nanofibers were prepared by nanospider technology. Quaternary ammonium salts as antibacterial agent were immobilized onto electrospun nylon-6/Ch nanofibers via surface modification by soaking the mat in aqueous solution of glycidyltrimethylammonium chloride (GTMAC) at room temperature overnight to give nylon-6/N-[(2-hydroxy-3-trimethylammonium)propyl] chitosan chloride (nylon-6/HTCC). The morphological, structural and thermal properties of the nylon-6/ch nanofibers were studied by field-emission scanning electron microscopy (FE-SEM), X-ray diffraction (XRD), Fourier transform-infrared (FT-IR) spectroscopy, and thermogravimetric analysis (TGA). Biological screening has demonstrated the antibacterial activity of the electrospun nanofibers against Gram negative bacteria, Escherichia coli 35218, and Pseudomonas aeruginosa and Gram positive bacteria, Staphylococcus aureus 24213 among the tested microbes. Thus, the study ascertains the value of the use of electrospun nanofibers, which could be of considerable interest to the development of new antibacterial materials for biomedical applications.     

Self-aggregation and antibacterial activity of N-acylated chitosan

Chitosan was selectively N-acylated with acetic, propionic and hexanoic anhydrides under homogeneous condition to prepare N-acetyl chitosan (NACS), N-propionyl chitosan (NPCS) and N-hexanoyl chitosan (NHCS), respectively. NACSs with different N-acetylation degrees were obtained by controlling the degree of N-acetylation. The chemical structures of N-acylated chitosans including degree of deacetylation (DD), weight-average molecular weight (M_w), radius of gyration (〈S₂〉_Z^1/2) and crystal structure were studied by FTIR, GPC-LLS and X-ray diffraction techniques. Aggregation behavior of N-acylated chitosan was investigated by rheometer. Intramolecular aggregation of NPCS and NACS was stronger with NPCS stronger than NACS. The effect of concentration of polymer, concentration of salt and temperature on self-aggregation of NACS and NPCS was investigated. Hydrophobic interaction of N-acylated chitosan substituted with longer acyl chains was stronger. With moderate DD, intramolecular aggregation occurs predominantly. In vitro antibacterial activity test of N-acylated chitosans was evaluated against two Gram-positive bacteria and two Gram-negative bacteria. Relative inhibition time (RIT) of NHCS with concentration of 1 mg/ml against Escherichia coli and Pseudomonas aeruginosa was more than 2-6 times longer than that of NACS and NPCS. N-acylated chitosan with lower DD had inhibitory effect on the growth of bacteria than that with moderate DD. The results showed that intermolecular aggregation characteristic of N-acetylated chitosans with low DD may help in forming bridge to interact with bacterial cell.     

Chemo-Enzymatic Synthesis and Antimicrobial Evaluation of Alkyloxy Propanol Amine-Based Cationic Ether Lipids

The present study involved the synthesis and antimicrobial evaluation of alkyloxy propanol amine-based cationic lipids N,N-dimethyl-1-octadecylamino-3-alkyloxy-2-propanol (series A, 7a–e) and N-methyl-N,N-di-(2-hydroxy-3-alkyloxy-2 propyl) octadecylamine (series B, 9a–e) and their acetylated derivatives (8a–e and 10a–e). A simple three-step chemo-enzymatic approach was employed for the synthesis of 7a–e and 9a–e in 71–80 and 67–88 % yields, respectively. The first step involved the synthesis of a series of glycidyl ethers from a series of alcohols (C₄, C₈, C₁₀, C₁₂, C₁₄) which were opened in the second step with octadecylamine to obtain 1-octadecylamino-3-alkyloxy-2 propanol (5a–e) and N,N-di-(2-hydroxy-3-alkyloxypropyl) octadecylamine (6a–e). In the third step, alkyloxy propanolamines (5a–e, 6a–e) were quaternized using methyl iodide to yield quaternized ammonium salts. The quaternized ammonium salts were enzymatically acetylated using Candida antarctica lipase-B based immobilized enzyme Novozym 435 to obtain their acetylated derivatives. The quaternized salts as well as their acetylated derivatives were evaluated for antibacterial and antifungal properties. The title compounds were found to possess moderate to good antibacterial activities against all the studied bacterial strains namely, Bacillus subtilis, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Klebsiella aerogenes compared to streptomycin and cetyl trimethyl ammonium bromide (CTAB). The title compounds exhibited relatively good antifungal activities against Candida albicans and no significant activities against other fungal strains namely, Saccharomyces cerevisiae, Rhizopus oryzae and Aspergillus niger when compared to amphotericin B and CTAB.     

Direct preparation of monodisperse core-shell microspheres with surface antibacterial property by using bicationic viologen surfmer

By exploringly introducing a bicationic viologen, N-hexyl-N'-(4-vinylbenzyl)-4,4′-bipyridinium bromide chloride (HVV) to dispersion polymerization of styrene (St) in a mixture of methanol and water, we achieved the following results: (1) monodisperse, core-shell microspheres with antibacterial surface were prepared by a simple one-step procedure, (2) diameter, core radii and shell thickness of resultant particles could be controlled by concentrations of HVV, monomer and initiator, and composition of media, (3) HVV could act not only as a monomer as that in previous modifications, but also as an efficient, novel stabilizer, and its copolymerization with St at interfacial layer and coagglutination of (co-)oligomers on core surface due to its moderate reactivity and hydrophilicity were conceived to be main reasons for formation of core-shell structures. Effects of HVV on polymerization behavior of St, evolution of core-shell structure, and morphology, size of particles were investigated. Moreover, antibacterial activity of resulted microspheres against Staphylococcus aureus was assayed.     

Mixed Stability and Antimicrobial Properties of Gluconamide-Type Cationic Surfactants

The stability of anionic-cationic surfactant solutions and the antimicrobial properties of novel N,N-dimethyl-N-[3-(gluconamide/lactobionamide)]propyl-N-alkylammonium bromides (CnDGPB and CnDLPB), N-methyl-N-hydroxyethyl group-N-[3-(gluconamide)-propyl]-N-alkylammonium bromide (CnMHGPB) and star-shaped gluconamide-type cationic surfactants N-dodecyl-N,N-bis[(3-d-gluconylamido)propyl]-N-alkylammonium bromide (CnDBGB) were investigated. Mixed stability in combination with sodium n-alkylbenzenesulfonate (LAS) was determined via transmittance; stability is achieved when percent transmittance was greater than 90 %. Transmittance results suggest that these cationic surfactants can form stable solutions with anionic surfactants over a broad concentration range. The inhibition activity of C _n DBGB is the best among the three kinds of glucocationic surfactants. Antimicrobial activity of C₁₂ surfactants was the best, C₁₄ was the second and C₁₀ was the worst. Moreover, antibacterial activity of glucose-based cationic surfactants was greater than lactose-based cationic surfactants.     

Development of g-C3N4/ZnO nanocomposite as a novel,highly effective and durable photocatalytic antibacterial coating for cotton fabric

Photocatalytic antibacterial coats are considered among the best solutions to bacterial contamination of fabrics, with the drawback of reduced efficacy after continued use and washing. In the present study, the g-C₃N₄/ZnO (CNZ) nanocomposite has been introduced as a novel cotton fabric coating, with high durability, and CNZ nanopowders were synthesized using a two-step thermal synthesis process and directly coated onto cotton fabric using the sonication technique. The synthesized nanoparticles (NPs) were examined using X-ray diffraction (XRD), UV–visible spectroscopy, photoluminescence (PL), Brunauer-Emmett-Teller (BET), and Fourier transform infrared (FTIR) analyzes. Besides, the SEM analysis confirmed the successful deposition of NPs on cotton fabric. The photodegradation of methylene blue (MB) stain was assessed as a functional test for the photocatalytic effectiveness of the coated fabric, then its antibacterial properties were evaluated under visible light, by direct contact with bacterial suspensions and culturing. The results revealed that the CNZ-coated cotton fabric containing 30% ZnO (CNZ-30) has significant photocatalytic antibacterial activity against both Escherichia coli (gram-negative), and Staphylococcus aureus (gram-positive) bacteria. The bacterial reduction rate of CNZ-30 coated fabric for both E. coli and S. aureus was above 98%, even after 18 washing cycles. This excellent performance is attributed to the effective coupling of ZnO with g-C₃N₄, improved light absorption, and reduced e⁻/h⁺ pair recombination rates. This study novel coating method can offer an environmentally friendly, cost-effective, and simple process to manufacture hybrid CNZ antibacterial cotton in the textile industry.     

Synthesis and characterization of a new polymer–drug conjugate with pH-induced activity

A well-defined, stimuli-responsive tetrapolymer with pH-responsive characteristics and targeting specificity has been synthesized by radical copolymerization of methacrylic acid, N-(2-hydroxypropyl)methacrylamide, methacryloyl glycylglycyl sulfamethoxazole, and N-(methacryloyl)glycylglycine 4-nitrophenyl ester. The structure and properties of tetrapolymer were investigated by NMR, FT-IR, UV–visible absorption, TEM and gel permeation chromatography. Incorporation of maleimide linker into tetrapolymer facilitates its conjugation with antibody fragments, as demonstrated by the solid-phase immunoassay experiments. The TEM image shows that tetrapolymer had self-assembled a spherical micelle with a diameter ranging from 50 to 150 nm. Altering the pH of the solution leads to a different extent of aggregation at pH 6.5–3.5, responding in accordance with the properties associated with the extracellular environment of solid tumors and endocytosis. Furthermore, fluorescence spectroscopy indicated a critical micelle concentration (CMC) of 1 mg/mL. Because of the solvation and ionization effects, the tetrapolymer showed considerably enhanced antibacterial activities against Escherichia coli in the presence of DMSO and the antibacterial activity increased with decreasing pH value.     

A comparative study of silicon nitride and SiAlON ceramics against E. coli

In recent decades, due to some limitations from alumina (Al₂O₃) and zirconia (ZrO₂), silicon nitride (Si₃N₄) has been investigated as a novel bioceramic material, mainly in situations where a bone replacement is required. Si₃N₄ ceramics and its derivative form, SiAlON, possess advantages in orthopedics due to their mechanical properties and biologically acceptable chemistry, which accelerates bone repair. However, biological applications require additional properties, enabling stronger chemical bonding to the surrounding tissue for better fixation and the prevention of bacteria biofilm formation. Therefore, two commercial Si₃N₄ and SiAlON ceramics were investigated in this study and compared to each other according to their material properties (like wetting angles and surface chemistry) and their antibacterial behaviors using E. coli. Results provided evidence of a 15% reduction in E. coli colonization after just 24 h on Si₃N₄ compared to SiAlON which is impressive considering no antibiotics were used. Further, a mechanism of action is provided. In this manner, this study provides evidence that Si₃N₄ should be further studied for a wide range of antibacterial orthopedic, or other suitable biomaterial applications.     

Synthesis of dynamic g-C3N4/Fe@ZnO nanocomposites for environmental remediation applications

An effective g-C₃N₄/Fe@ZnO heterostructured photocatalyst was synthesized by a simple chemical co-precipitation method and characterized by X-ray diffraction, Fourier transform infrared spectroscopy, transmission electron microscopy and ultraviolet–visible spectroscopy. Transmission electron microscopy revealed that 7-8 nm-sized 1%Fe@ZnO nanoparticles were evenly distributed on g-C₃N₄ nanosheets to form a hybrid composite. The photocatalytic effectiveness of the composites was assessed against methylene blue dye, and it was found that the 50%g-C₃N₄/Fe@ZnO photocatalyst was more efficient in harvesting solar energy to degrade dye than the ZnO, 1%Fe@ZnO, g-C₃N₄, g-C₃N₄/ZnO and (10, 25, 40, 60 & 75 wt%) g-C₃N₄/Fe@ZnO samples. The antibacterial competency of the samples was also explored against Gram-positive (Bacillus subtilis, Staphylococcus aureus and Streptococcus salivarius) and Gram-negative (Escherichia coli) bacteria through the well diffusion method. The 50%g-C₃N₄/Fe@ZnO nanocomposite exhibited a superior antibacterial action compared to that of the rest of the samples. The exceptionally improved photocatalytic and antimicrobial efficiency of the 50%g-C₃N₄/Fe@ZnO composite was primarily accredited to the synergic outcome of the interface established between Fe@ZnO nanoparticles and g-C₃N₄ nanosheets.     

Novel functionalized monomers based on kojic acid: snythesis,characterization, polymerization and evalution of antimicrobial activity

Two novel acrylate monomers, [5-(benzyloxy)-4-oxo-4H-pyran-2-yl]methyl acrylate and {1-[(5-(benzyloxy)-4-oxo-4H-pyran-2-yl)methyl]-1,2,3-triazol-4-yl}methyl acrylate were synthesized by the reaction of 5-benzyloxy-2-(hydroxymethyl)-4H-pyran-4-one and 5-(benzyloxy)-2-{[4-(hydroxymethyl)-1,2,3-triazol-1-yl]methyl}-4H-pyran-4-one with acryloyl chloride in the presence of triethylamine, respectively. These monomers were polymerized using 2,2^′-azobisisobutyronitrile (AIBN) as the initiator in N,N-dimethylformamide:14-dioxane (10:1) solution. The thermal behavior of the polymers was investigated by thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The synthesized compounds were evaluated for their antibacterial and antifungal activites aganist bacteria and fungi using the disk diffusion method. The results indicated that some of these compounds demonstrated moderate to good antibacterial and antifungal activities.     

Antimicrobial and Hypoglycemic Activities of Novel N-Mannich Bases Derived from 5-(1-Adamantyl)-4-substituted-1,2,4-triazoline-3-thiones

The reaction of 5-(1-adamantyl)-4-ethyl or allyl-1,2,4-triazoline-3-thione with formaldehyde solution and various 1-substituted piperazines yielded the corresponding N-Mannich bases. The newly synthesized N-Mannich bases were tested for in vitro inhibitory activities against a panel of Gram-positive and Gram-negative bacteria and the yeast-like pathogenic fungus Candida albicans. Six compounds showed potent antibacterial activity against one or more of the tested microorganisms, while two compounds exhibited moderate activity against the tested Gram-positive bacteria. None of the newly synthesized compounds were proved to possess marked activity against Candida albicans. The oral hypoglycemic activity of six compounds was determined in streptozotocin (STZ)-induced diabetic rats. Four compounds produced significant strong dose-dependent reduction of serum glucose levels, compared to gliclazide at 10 mg/kg dose level (potency ratio > 75%).     

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.     

Introducing a Semi-Coated Model to Investigate Antibacterial Effects of Biocompatible Polymers on Titanium Surfaces

Peri-implant infections from bacterial biofilms on artificial surfaces are a common threat to all medical implants. They are a handicap for the patient and can lead to implant failure or even life-threatening complications. New implant surfaces have to be developed to reduce biofilm formation and to improve the long-term prognosis of medical implants. The aim of this study was (1) to develop a new method to test the antibacterial efficacy of implant surfaces by direct surface contact and (2) to elucidate whether an innovative antimicrobial copolymer coating of 4-vinyl-N-hexylpyridinium bromide and dimethyl(2-methacryloyloxyethyl) phosphonate (VP:DMMEP 30:70) on titanium is able to reduce the attachment of bacteria prevalent in peri-implant infections. With a new in vitro model with semi-coated titanium discs, we were able to show a dramatic reduction in the adhesion of various pathogenic bacteria (Streptococcus sanguinis, Escherichia coli, Staphylococcus aureus, Staphylococcus epidermidis), completely independently of effects caused by soluble materials. In contrast, soft tissue cells (human gingival or dermis fibroblasts) were less affected by the same coating, despite a moderate reduction in initial adhesion of gingival fibroblasts. These data confirm the hypothesis that VP:DMMEP 30:70 is a promising antibacterial copolymer that may be of use in several clinical applications.     

Efficient Photodynamic Killing of Gram-Positive Bacteria by Synthetic Curcuminoids

In our previous study, we have demonstrated that curcumin can efficiently kill the anaerobic bacterium Propionibacterium acnes by irradiation with low-dose blue light. The curcuminoids present in natural plant turmeric mainly include curcumin, demethoxycurcumin, and bisdemethoxycurcumin. However, only curcumin is commercially available. Eighteen different curcumin analogs, including demethoxycurcumin and bisdemethoxycurcumin, were synthesized in this study. Their antibacterial activity against Gram-positive aerobic bacteria Staphylococcus aureus and Staphylococcus epidermidis was investigated using the photodynamic inactivation method. Among the three compounds in turmeric, curcumin activity is the weakest, and bisdemethoxycurcumin possesses the strongest activity. However, two synthetic compounds, (1E,6E)-1,7-bis(5-methylthiophen-2-yl)hepta-1,6-diene-3,5-dione and (1E,6E)-1,7-di(thiophen-2-yl)hepta-1,6-diene-3,5-dione, possess the best antibacterial activity among all compounds examined in this study. Their chemical stability is also better than that of bisdemethoxycurcumin, and thus has potential for future clinical applications.     

PG-2, a Potent AMP against Pathogenic Microbial Strains,from Potato (Solanum tuberosum L cv. Gogu Valley) Tubers Not Cytotoxic against Human Cells

In an earlier study, we isolated potamin-1 (PT-1), a 5.6-kDa trypsin-chymotrypsin protease inhibitor, from the tubers of a potato strain (Solanum tuberosum L cv. Gogu Valley). We established that PT-1 strongly inhibits pathogenic microbial strains, but not human bacterial strains, and that its sequence shows 62% homology with a serine protease inhibitor. In the present study, we isolated an antifungal and antibacterial peptide with no cytotoxicity from tubers of the same potato strain. The peptide (peptide-G2, PG-2) was isolated using salt-extraction, ultrafiltration and reverse-phase high performance liquid chromatography (RP-HPLC). Matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF/MS) showed the protein to have a molecular mass of 3228.5 Da, while automated Edman degradation showed the N-terminal sequence of PG-2 to be LVKDNPLDISPKQVQALCTDLVIRCMCCC-. PG-2 exhibited antimicrobial activity against Candida albicans, a human pathogenic yeast strain, and Clavibacter michiganensis subsp. michiganensis, a plant late blight strain. PG-2 also showed antibacterial activity against Staphylococcus aureus, but did not lyse human red blood cells and was thermostable. Overall, these results suggest PG-2 may be a good candidate to serve as a natural antimicrobial agent, agricultural pesticide and/or food additive.     

Construction of g-C3N4/TiO2/Ag composites with enhanced visible-light photocatalytic activity and antibacterial properties

In this study, the multifunctional carbon nitride based composite graphitic-C₃N₄ (g-C₃N₄)/TiO₂/Ag was prepared through a simple and efficient vacuum freeze-drying route. TiO₂ and Ag nanoparticles were demonstrated to decorate onto the surface of g-C₃N₄ sheet. In the ultraviolet–visible absorption test, a narrower band gap and red-shift of light absorption edge were observed for g-C₃N₄/TiO₂/Ag compared to pristine g-C₃N₄ and single-component modified g-C₃N₄/TiO₂. The photodegradation property of g-C₃N₄/TiO₂/Ag was investigated toward the degradation of methylene blue (abbreviated as MB) under the irradiation of visible light. These results indicated that the degradation performance of organic dyes for g-C₃N₄/TiO₂/Ag was obviously improved compared with g-C₃N₄/TiO₂ and g-C₃N₄. The reaction rate constant of MB degradation for g-C₃N₄/TiO₂/Ag was 4.24 times higher than that of pristine g-C₃N₄. In addition, such rationally constructed nanocomposite presented evidently enhanced antibacterial performance against the Gram-negative Escherichia coli. Concentration dependent antibacterial performance was systematically investigated. And 84% bacterial cell viability loss had been observed at 500 μg/mL g-C₃N₄/TiO₂/Ag within 2 h visible light irradiation.