Antimicrobial and cytotoxic activity of 18 prenylated flavonoids isolated from medicinal plants: Morus alba L., Morus mongolica Schneider, Broussnetia papyrifera (L.) Vent, Sophora flavescens Ait and Echinosophora koreensis Nakai

Antimicrobial activity of the 18 prenylated flavonoids, which were purified from five different medicinal plants, was evaluated by determination of MIC using the broth microdilution methods against four bacterial and two fungal microorganisms (Candida albicans, Saccaromyces cerevisiae, Escherichia coli, Salmonella typhimurium, Staphylococcus epidermis and S. aureus). Papyriflavonol A, kuraridin, sophoraflavanone D and sophoraisoflavanone A exhibited a good antifungal activity with strong antibacterial activity. Kuwanon C, mulberrofuran G, albanol B, kenusanone A and sophoraflavanone G showed strong antibacterial activity with 5–30 μg/ml of MICs. Morusin, sanggenon B and D, kazinol B, kurarinone, kenusanone C and isosophoranone were effective to only gram positive bacteria, and broussochalcone A was effective to C. albicans. IC₅₀ values of papyriflavonol A, kuraridin, sophoraflavanone D, sophoraisoflavanone A and broussochalcone A in HepG2 cells were 20.9, 37.8, 39.1, 22.1, and 22.0 μg/ml, respectively. These results support the use of prenylated flavonoids in Asian traditional medicine to treat microbial infection and indicate a high potential for prenylated flavonoids as antimicrobial agents as well as anti-inflammatory agents.     

霉克舒对致病性浅部真菌的体外抑菌作用研究

从湛江地区 15 4例癣病患者分离真菌 ,评价一种新的抗真菌药—霉克舒对上述真菌菌株的体外抑菌活性。应用琼脂稀释法测定霉克舒对浅部真菌的最小抑菌浓度 (MIC) ,同时以兰美抒作为对照药物。从 15 4例癣病患者中分离出 14 1株真菌 ,其中以红色毛癣菌和须癣毛癣菌为主 ,分别占 6 6 .7%和 14 .2 %。霉克舒的抑菌作用与兰美抒相比略强或相当 ;对霉克舒各单一成分的初步抑菌效果进行比较 ,复合物的抑菌作用明显强于水杨酸或特比萘芬等单一成分。上述结果显示 ,霉克舒在体外对常见致病性浅部真菌具有较强的抗菌活性。     

Inhibition ofStreptococcus mutans and Other Oral streptococci by hop (Humulus lupulus L.) constituents

We report the inhibition of the causative agents of dental caries, Streptococcus mutans and other oral streptococci, by the antimicrobially active ingredients of the hop plant (Humulus lupulus L.). The hop constituents studied were purified beta acid, xanthohumol, isoalpha acid and tetra iso-alpha acid. Cruder hop extracts were also investigated. The antimicrobial activity of these hop constituents was tested against four strainsof Streptococcus mutans as well as one strain each ofStreptococcus sanguis andStreptococcus salivarius and compared to antimicrobial essential oils used in mouthwashes in two independent assay systems. We found that all tested hop constituents inhibited the Streptococci. The minimum inhibitory concentration at pH 7.5 ranged from 2 to 50 μg/ml depending on the microorganism and hop phytochemical tested. Contrary to a previous report, there was no activity enhancement by ascorbic acid over and above the enhancement due to pH lowering. Thére was no resistance development to beta acid after 10 passages in a subinhibitory concentration of this acid. Antimicrobial activity of hop constituents was found to be greater than other plant products such as thymol, nerol, cinnamon oil, oil of clove, menthol and eucalyptol. The possibilities of using hop constituents in mouthwashes are discussed.     

Photo-catalytic preparation of silver-coated TiO2 particles for antibacterial applications

Colloidal silver has been known to have unique antimicrobial activity that may be useful in the construction of antibacterial materials (self-cleaning materials) to aid in the fight against bacteria-related infections. In this study, silver-coated TiO₂ (Ag/TiO₂) particles prepared through the photo-reduction of Ag⁺ were investigated as an antibacterial agent against Escherichia coli and Staphylococcus aureus. The deposition of Ag onto the surface was confirmed with SEM and EDS analysis of the post-reaction particles. It was also determined that the initial concentration of Ag⁺ in solution played a significant role in the effective size of the post-irradiation particles. The antibacterial effectiveness of the Ag/TiO₂ was evaluated through the determination of the minimum inhibitory concentration (MIC) of AgTiO₂ for each species of bacteria. The MIC values for the Ag/TiO₂, on both E. coli and S. aureus, were much lower than the MIC values for Ag metal, and quite comparable to the MIC values for AgNO₃. A disc diffusion/antibiotic sensitivity test was also performed using the Ag/TiO₂ particles and the results compared with the results obtained for Ag metal, AgNO₃ and common antibacterial agents; tetracycline, chloramphenicol, erythromycin, and neomycin. The zone of inhibition diameters for the Ag/TiO₂ particles were found to be comparable with those of the other antimicrobial agents.     

Microbially initiated pitting on 316L stainless steel

Pitting corrosion of 316L stainless steel ennobled in the presence of manganese-oxidizing bacteria, Leptothrix discophora, was studied in a low-concentration sodium chloride solution. Corrosion coupons were first exposed to the microorganisms in a batch reactor until ennoblement occurred, then sodium chloride was added, which initiated pitting. The pits had aspect ratios (length divided by width) and shapes closely resembling the aspect ratio and the shape of the bacteria, which suggested that the microorganisms were involved in pit initiation.     

Synthesis of benzoylthiourea derivatives and analysis of their antibacterial performance against planktonic Staphylococcus aureus and its biofilms

Following the appearance of several antimicrobial agents to control the spread of infections, two major challenges have emerged: (i) the occurrence and blowout of multiresistant bacteria and the increase of chronic diseases and (ii) difficult-to-eradicate infections. In this study, we tested five benzoylthiourea derivatives for their ability to inhibit and stop bacterial growth and evaluated the possible influence of 1,2,4-triazolyl-benzoylthiourea derivative 4 on the formation and eradication of Staphylococcus aureus biofilms. Benzoylthiourea derivatives 4 , 6 , 10 , 11 and 13 were obtained in one or two steps with low cost and subjected to tests to identify their minimum inhibitory concentration (MIC) and minimum bactericidal concentration. In vitro tests were also performed to assess their effects on biofilm formation and in preformed biofilms and scanning electron microscopy was used to visualize the effects on biofilm formation. The 1,2,4-triazolyl-benzoylthiourea derivative 4 showed bacteriostatic activity against the S. aureus HU25 clinical strain with an MIC of 16 µg ml⁻¹, which is below the toxic concentration (at 2500 µg ml⁻¹, 62·25% of the cells remained viable). Compound 4 also effectively prevented biofilm formation at the three subinhibitory concentrations tested (1/2 MIC, 1/4 MIC and 1/8 MIC) as confirmed by scanning electron microscopy. For breakdown of formed biofilms, the main influence was at a subinhibitory concentration (1/2 MIC). These findings make compound 4 a strong candidate for studies on the development of new antimicrobial and antibiofilm agents.     

Influence of hydrocarbon-stapling on membrane interactions of synthetic antimicrobial peptides

Cyclization has been recognized as a valuable technique for increasing the efficacy of small molecule and peptide therapeutics. Here we report the application of a hydrocarbon staple to a rationally-designed cationic antimicrobial peptide (CAP) that acquires increased membrane targeting and interaction vs. its linear counterpart. The previously-described CAP, 6K-F17 (KKKKKK-AAFAAWAAFAA-NH₂) was used as the backbone for incorporation of an i to i?+?4 helical hydrocarbon staple through olefin ring closing metathesis. Stapled versions of 6K-F17 showed an increase in non-selective membrane interaction, where the staple itself enhances the degree of membrane interaction and rate of cell death while maintaining high potency against bacterial membranes. However, the higher averaged hydrophobicity imparted by the staple also significantly increases toxicity to mammalian cells. This deleterious effect is countered through stepwise reduction of the stapled 6K-F17’s backbone hydrophobicity through polar amino acid substitutions. Circular dichroism assessment of secondary structure in various bacterial membrane mimetics reveals that a helical structure may improve – but is not an absolute requirement for – antimicrobial activity of 6K-F17. Further, phosphorus-31 static solid state NMR spectra revealed that both non-toxic stapled and linear peptides bind bacterial membranes in a similar manner that does not involve a detergent-like mechanism of lipid removal. The overall results suggest that the technique of hydrocarbon stapling can be readily applied to membrane-interactive CAPs to modulate how they interact and target biological membranes.     

Molecular mechanism of Arabidopsis thaliana profilins as antifungal proteins

Background

It remains an open question whether plant phloem sap proteins are functionally involved in plant defense mechanisms.

PINK1 Phosphorylates MIC60/Mitofilin to Control Structural Plasticity of Mitochondrial Crista Junctions

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Antimicrobial activity of some plant extracts against bacterial strains causing food poisoning diseases

Prevention of food spoilage and food poisoning pathogens is usually achieved by use of chemical preservatives which have negative impacts including: human health hazards of the chemical applications, chemical residues in food & feed chains and acquisition of microbial resistance to the used chemicals. Because of such concerns, the necessity to find a potentially effective, healthy safer and natural alternative preservatives is increased. Within these texts, Plant extracts have been used to control food poisoning diseases and preserve foodstuff. Antimicrobial activity of five plant extracts were investigated against Bacillus cereus, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhi using agar disc diffusion technique. Ethanolic extracts of Punica granatum, Syzygium aromaticum, Zingiber officinales and Thymus vulgaris were potentially effective with variable efficiency against the tested bacterial strains at concentration of 10 mg/ml while extract of Cuminum cyminum was only effective against S. aureus respectively. P. granatum and S. aromaticum ethanolic extracts were the most effective plant extracts and showed bacteriostatic and bactericidal activities against the highly susceptible strains of food borne pathogenic bacteria (S. aureus and P. aeruginosa) with MIC's ranged from 2.5 to 5.0 mg/ml and MBC of 5.0 and 10 mg/ml except P. aeruginosa which was less sensitive and its MBC reached to 12.5 mg/ml of S. aromaticum respectively. These plant extracts which proved to be potentially effective can be used as natural alternative preventives to control food poisoning diseases and preserve food stuff avoiding healthy hazards of chemically antimicrobial agent applications.