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1.
Brazilian green and red propolis stand out as commercial products for different medical applications. In this article, we report the antimicrobial activities of the hydroalcoholic extracts of green (EGP) and red (ERP) propolis, as well as guttiferone E plus xanthochymol (8) and oblongifolin B (9) from red propolis, against multidrug-resistant bacteria (MDRB). We undertook the minimal inhibitory (MIC) and bactericidal (MBC) concentrations, inhibition of biofilm formation (MICB50), catalase, coagulase, DNase, lipase, and hemolysin assays, along with molecular docking simulations. ERP was more effective by displaying MIC and MBC values <100 μg mL−1. Compounds 8 and 9 displayed the lowest MIC values (0.98 to 31.25 μg mL−1) against all tested Gram-positive MDRB. They also inhibited the biofilm formation of S. aureus (ATCC 43300 and clinical isolate) and S. epidermidis (ATCC 14990 and clinical isolate), with MICB50 values between 1.56 and 6.25 μg mL−1. The molecular docking results indicated that 8 and 9 might interact with the catalase's amino acids. Compounds 8 and 9 have great antimicrobial potential.  相似文献   

2.
In order to investigate virulence enhancement of entomopathogenic fungi, a Beauveria bassiana-sourced Pr1 protease (CDEP-1) was expressed by a methylotrophic yeast Pichia pastoris and then used as an additive to three gradient sprays of B. bassiana strain (Bb0062) onto apterous green peach aphid Myzus persicae adults in six bioassays. The resultant data fit well to a time–concentration–mortality model. Generally, the LC50 estimates of the fungal pathogen against the aphid species decreased with increasing CDEP-1 concentrations from 0 to 100 µg mL?1. The LC50s on days 5–7 after spray were reduced by 1.5–2.5-fold at the concentrations of 20–100 µg mL?1. However, sprays of 20–100 µg CDEP-1 mL?1 aqueous solution alone had no significant effect on aphid mortality compared to water spray only. Neither did inclusion of inactivated CDEP-1 at a concentration of 50 µg mL?1 affect significantly the fungal virulence to aphids. Our results confirm for the first time that the cuticle-degrading protease CDEP-1 enhanced fungal virulence due to acceleration of conidial germination and cuticle penetration. This suggests a new approach to utilising the protease in microbial control.  相似文献   

3.
Candida biofilms are tolerant to conventional antifungal therapeutics and the host immune system. The transition of yeast cells to hyphae is considered a key step in C. albicans biofilm development, and this transition is inhibited by the quorum-sensing molecule farnesol. We hypothesized that fatty acids mimicking farnesol might influence hyphal and biofilm formation by C. albicans. Among 31 saturated and unsaturated fatty acids, six medium-chain saturated fatty acids, that is, heptanoic acid, octanoic acid, nonanoic acid, decanoic acid, undecanoic acid and lauric acid, effectively inhibited C. albicans biofilm formation by more than 75% at 2 µg ml−1 with MICs in the range 100–200 µg ml−1. These six fatty acids at 2 µg ml−1 and farnesol at 100 µg ml−1 inhibited hyphal growth and cell aggregation. The addition of fatty acids to C. albicans cultures decreased the productions of farnesol and sterols. Furthermore, down-regulation of several hyphal and biofilm-related genes caused by heptanoic or nonanoic acid closely resembled the changes caused by farnesol. In addition, nonanoic acid, the most effective compound diminished C. albicans virulence in a Caenorhabditis elegans model. Our results suggest that medium-chain fatty acids inhibit more effectively hyphal growth and biofilm formation than farnesol.  相似文献   

4.
Phenylpyrazole insecticides are successful for crop protection and public hygiene by blocking gamma-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride (GluCl) channels. A series of novel phenylpyrazoles containing arylimine or 1-methoxyaryl groups were designed and synthesized. The addition reaction of methanol to the imines 111 was investigated and the cayno addition products 1315 were obtained. The compounds 115 were confirmed by 1H NMR and elemental analysis. The results of bioassay indicated that some compounds exhibited comparable bioactivity to fipronil against a broad spectrum of insects such as bean aphid (Aphis craccivora), mosquito (Culex pipiens pallens), diamondback moth (Plutella xylostella) and Oriental armyworm (Mythimna separata). Especially, the foliar contact activity against bean aphid of compound 7 at 10 µg mL−1 was 68%, the larvacidal activity against mosquito of compounds 5, 13 and 15 at 0.0025 µg mL−1 was 100%, the larvacidal activity against diamondback moth of compounds 9 and 11 at 0.05 µg mL−1 was 100%, the larvacidal activity against Oriental armyworm of compound 9 at 1 µg mL−1 was 100%. The 3-cayno moiety on pyrazole ring was essential for the high insecticidal activities against bean aphid, diamondback moth and Oriental armyworm, while the 3-carbimidate moiety on pyrazole ring was crucial to the excellent high insecticidal activities against mosquito.  相似文献   

5.
The extracts of five invasive plants were investigated for antifungal and antibiofilm activities against Candida albicans, C. glabrata, C. krusei, and C. parapsilosis. The antifungal activity was evaluated using the microdilution assay and the antibiofilm effect by measurement of the metabolic activity. Ethanol and ethanol-water extracts of Reynoutria japonica leaves inhibited 50 % of planktonic cells at 250 μg mL−1 and 15.6 μg mL−1, respectively. Ethanol and ethanol-water extracts of Baccharis halimifolia inhibited >75 % of the mature biofilm of C. albicans at 500 μg mL−1. The essential oil (EO) of B. halimifolia leaves was the most active (50 % inhibition (IC50) at 4 and 74 μg mL−1against the maturation phase and 24 h old-biofilms of C. albicans, respectively). Oxygenated sesquiterpenes were the primary contents in this EO (62.02 %), with β-caryophyllene oxide as the major component (37 %). Aromadendrene oxide-(2), β-caryophyllene oxide, and (±)-β-pinene displayed significant activities against the maturation phase (IC50=9–310 μ mol l−1) and preformed 24 h-biofilm (IC50=38–630 μ mol l−1) of C. albicans with very low cytotoxicity for the first two compounds. C. albicans remained the most susceptible species to this EO and its components. This study highlighted for the first time the antibiofilm potential of B. halimifolia, its EO and some of its components.  相似文献   

6.

An efficient micropropagation protocol was developed for Jeffersonia dubia using sucker explants. High frequency of multiple shoot formation was induced when the sucker explants were cultured on Chu’s (N6) medium with different concentrations of thidiazuron (TDZ) plus 0.54 µM α-naphthaleneacetic acid (NAA). The maximum frequency of shoot formation (96.2 %) was obtained on N6 medium with 2.27 µM TDZ plus 0.54 µM NAA. The highest mean number of shoots per explant (13.6) was obtained in temporary immersion system using an immersion frequency of 30 s every 30 min. The highest frequency of rooting (100 %), number of roots per shoot (5.8), and root length (6.3) was observed in half-strength N6 medium supplemented with 2.69 µM NAA. The regenerated plantlets (30 days old) were successfully acclimatized in the greenhouse with 98 % survival rate. The berberine content and cytotoxicity were higher in in vitro-developed calli and shoots than in leaves of field-grown plants. The greatest content of berberine was found in shoots (1381 μg g−1) followed by calli (1092 μg g−1) and leaves of field-grown plants (92 μg g−1). At 1000 μg mL−1 concentration, growth inhibition rate of berberine, callus, shoot, and leaf (in vivo) extracts were 68.4, 57.1, 54.2, and 17.7 %, respectively.

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7.
Bacterial leaf blight of rice (BLB), caused by Xanthomonas oryzae pv oryzae, is one of the most serious bacterial diseases in China. Presently, bismerthiazol has been the major bactericide for the control of BLB, however, bismerthiazol‐resistant strains of X. oryzae pv. oryzae have appeared in the field in China. Zinc thiazole is a novel bactericide with strong antibacterial activity against Xanthomonas spp. In this study, sensitivity of 109 X. oryzae pv. oryzae strains to zinc thiazole was determined. The EC50 values for zinc thiazole in inhibiting bacterial growth of the 109 X. oryzae pv. oryzae strains were 0.53–9.62 µg mL?1 with the average EC50 value of 4.82 ± 1.86 µg/ml. The minimum inhibitory concentration (MIC) values of zinc thiazole against the 109 X. oryzae pv. oryzae strains were assessed and the results showed that the MIC values of zinc thiazole for completely inhibiting the growth of these 109 strains ranged from 5.0 to 40.0 µg mL?1. In the evaluation of protective and curative activity test, zinc thiazole exhibited great activity against BLB and provided over 88% control efficacy (at 300 µg mL?1) 1 and 3 days before or after inoculations, which was also higher that that of bismerthiazol in the corresponding treatments. Our field trials showed that zinc thiazole at 375 g.a.i ha?1 provided over 70% control efficacy in 2012 and over 80% control efficacy in 2013 at both sites. Moreover, in all the four field trials, zinc thiazole at 250 g.a.i ha?1 provided higher control efficacy than that of bismerthiazol at 250 g.a.i ha?1. Taken together, zinc thiazole is therefore an alternative tool for the management of BLB.  相似文献   

8.
9.
Abstract

Acinetobacter baumannii is a biofilm forming multidrug resistant (MDR) pathogen responsible for respiratory tract infections. In this study, aluminium oxide nanoparticles (Al2O3 NPs) were synthesized and characterized by TEM and EDX and shown to be spherical shaped nanoparticles with a diameter < 10?nm. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) for the Al2O3 NPs ranged between 125 and 1,000?µg ml?1. Exposure to NPs caused cellular membrane disruption, indicated by an increase in cellular leakage of the contents. Biofilm inhibition was 11.64 to 70.2%, whereas attachment of bacteria to polystyrene surfaces was reduced to 48.8 to 51.9% in the presence of NPs. Nanoparticles also reduced extracellular polymeric substance production and the biomass of established biofilms. The data revealed the non-toxic nature of Al2O3 NPs up to a concentrations of 120?µg ml?1 in HeLa cell lines. These results demonstrate an effective and safer use of Al2O3 NPs against the MDR A. baumannii by targeting biofilm formation, adhesion and EPS production.  相似文献   

10.
Emergence and rapid spread of multidrug-resistant (MDR) bacteria including Vibrio cholerae are a global public health issue. Much attention has been paid to natural compounds, such as spices and herbs to find novel antimicrobial compounds as they are considered to be cheaper alternatives to develop as a drug. Here, we show that methanol extract of white pepper could inhibit the growth of V. cholerae O1 El Tor variant, responsible for the recent outbreaks/epidemics. Furthermore, we demonstrate for the first time that piperine, the major component of white pepper, showed a dose-dependent bactericidal effect on V. cholerae growth irrespective of their biotypes and serogroups in the presence of 200 and 300 µg ml−1 of piperine, respectively. Piperine also inhibited the growth of MDR strains of Pseudomonas aeruginosa, Escherichia coli isolated from poultry and enterohemorrhagic/enteroaggregative E. coli O104 in the presence of 200 µg ml−1. Interestingly, we did not observe any significant inhibitory effect of piperine on E. coli strains isolated from healthy person even up to 200 µg ml−1. Our data suggest that piperine could be a novel antimicrobial agent in therapeutic and preventive applications against infections caused by pathogenic bacteria including MDR strains.  相似文献   

11.
A novel chiral sensing platform, employing silver nanoparticles capped with N‐acetyl‐L‐cysteine (NALC‐Ag NPs), was utilized for the discrimination of L‐tyrosine and D‐tyrosine. This nanosensor, which could be used as an optical sensing unit and chiral probe, was characterized by transmission electron microscopy (TEM) and resonance Rayleigh scattering (RRS) spectroscopy. After the proposed sensing platform interacted with L‐tyrosine and D‐tyrosine, a decreased resonance scattering signal was only obtained from L‐tyrosine. This phenomenon offered a useful assay for the selectivity and determination of L‐tyrosine with the RRS method. The linear range and detection limit of L‐tyrosine were 0.2838–20.0 µg⋅mL‐1 and 0.0860 µg⋅mL‐1, respectively. In addition, experimental factors such as acidity, interaction time, and the concentration of enantiomers were investigated with regard to the effect on enantioselective interaction. Chirality 27:194–198, 2015. © 2014 Wiley Periodicals, Inc.  相似文献   

12.
Nanotechnology is an emerging field with tremendous potential and usage of medicinal plants and green preparation of nanoparticles (NPs) is one of the widely explored areas. These have been shown to be effective against different biological activities such as diabetes mellitus, cancer, antioxidant, antimicrobial, etc. The current studies focus on the green synthesis of zinc NPs (ZnO NPs) from aqueous leaf extract of Murraya koenigii (MK). The synthesized Murraya koeingii zinc oxide NPs (MK ZnO NPs) were characterized using UV–visible spectroscopy, dynamic light scattering (DLS), Fourier transform infrared (FTIR) spectroscopy, field emission scanning electron microscopy (FESEM), energy-dispersive spectrum (EDS) and cyclic voltammetry (CV). The synthesized MK ZnO NPs were evaluated for their in vitro antidiabetic, antioxidant, antimicrobial, and cytotoxic activity. They demonstrated significant antidiabetic and cytotoxic activity, as well as moderate free-radical scavenging and antibacterial activity.  相似文献   

13.
We aimed to characterize and investigate the antibacterial potential of the native stingless bees geopropolis volatile oils (VO) for the search of potentially new bioactive compounds. Geopropolis samples from Melipona bicolor schencki, M. compressipes manaosensis, M. fasciculata, M. quadrifasciata, M. marginata and M. seminigra merrillae were collected from hives in South Brazil. VO were obtained by hydrodistillation and characterised by gas chromatography coupled to mass spectrometry (GC/MS). Antimicrobial activity was assessed by microplate dilution method. The lowest MIC against cell walled bacteria was 219±0 μg mL−1 from M. quadrifasciata geopropolis VO with Staphylococcus aureus. The M. b. schencki geopropolis VO minimal inhibition concentration (MIC) was 424±0 μg mL−1 against all the mycoplasma strains evaluated. Fractionation resulted in the reduction of 50 % of the MIC value from the original oil. However, its compounds’ synergism seems to be essential to this activity. Antibiofilm assays demonstrated 15.25 % eradication activity and 13.20 % inhibition of biofilm formation after 24 h for one subfraction at 2× its MIC as the best results found. This may be one of the essential mechanisms by which geopropolis VOs perform their antimicrobial activity.  相似文献   

14.
A chemiluminescent method using flow injection (FI) was investigated for rapid and sensitive determination of enalapril maleate and atenolol, which are used in the treatment of hypertension. The method is based on the sensitizing effect of these drugs on the Ce(IV)–sulfite reaction. The different experimental parameters affecting the chemiluminescence (CL) intensity were carefully studied and incorporated into the procedure. The method permitted the determination of 0.01–3.0 µg mL?1 of enalapril maleate in bulk form with correlation coefficient r = 0.99993, lower limit of detection (LOD) 0.0025 µg mL?1 (S/N = 2) and lower limit of quantitation (LOQ) 0.01 µg mL?1. The linearity range of atenolol in bulk form was 0.01–2.0 µg mL?1 (r = 0.99989) with LOD of 0.0003 µg mL?1 (S/N = 2) and LOQ of 0.01 µg mL?1. In biological fluids the linearity range of enalapril maleate was 0.1–2.0 µg mL?1 in both urine and serum, and for atenolol the linearity range was 0.1–1.0 µg mL?1 in both urine and serum. The method was also applied to the determination of the drugs in their pharmaceutical preparations. Copyright © 2009 John Wiley & Sons, Ltd.  相似文献   

15.
Young (16-day-old) Sorghum bicolor plants of a late- and slow-senescing Texas A&M line (B 35) and of an early- and fast-senescing descendant of an Ethiopian landrace (E 36-1) were subjected to drought stress by decreasing the soil water content to 30% field capacity over 6 days. Plant water potentials decreased from − 2 bar (controls) to − 10 to − 18 bar, and this drought stress resulted in: (1) differential phenotypic reactions and (2) differential decreases in photosynthesis rates in the two cultivars. While E 36-1 tended to lose viable leaf area from the leaf tips downwards, B 35 showed a gradual overall drying of the leaf. At the same time, photosynthesis rates decreased from 31.5 ± 1.6 to 12.3 ± 5.0 µmol CO2 m−2 s−1 (E 36-1) and from 30.5 ± 1.6 to 3.3 ± 2.6 µmol CO2 m−2 s−1 (B 35), respectively. In vitro enzyme activities of phosphoenolpyruvate carboxylase (PEPCase), malate dehydrogenase (MDH) and malic enzyme (ME) on a leaf area basis exceeded the photosynthesis rates. Pyruvate phosphate dikinase (PPDK) activity was close to the photosynthesis rates in control plants and higher than the photosynthesis rates in drought-stressed plants. Thus, none of the enzymes appeared to limit photosynthesis under drought stress, and likely bottleneck enzyme activities of the C3 pathway in the bundle-sheath cells, i.e. ribulose-1,5-bisphosphate carboxylase (RubisCO) and stromal fructose-1,5-bisphosphatase (sFBPase), also showed sufficient activities to sustain higher photosynthesis rates than those observed in the stressed plants. However, under drought stress, total leaf malate concentrations were higher in B 35 (up to 33.1 µmol g−1 FW) than in E 36-1 (up to 22.4 µmol g−1 FW). In particular, at the presumed cytosolic pH of 7.0–7.3, S. bicolor PEPCase was strongly inhibited by malate. In contrast with the in vitro PEPCase enzyme activities, the A/Ci curves suggested a stronger decrease in the in vivo activity of the enzyme in B 35 under drought stress than in E 36-1. It is therefore suggested that photosynthesis under drought stress may be inhibited differentially through feedback malate inhibition of PEPCase in S. bicolor.  相似文献   

16.
Baseline sensitivity and efficacy of thifluzamide in Rhizoctonia solani   总被引:1,自引:0,他引:1  
Thifluzamide is a SDHI (succinate dehydrogenase inhibitor) fungicide, which interferes with succinate ubiquinone reductase in the mitochondrial electron transport chain of fungi. Presently, jinggangmycin is the major fungicide extensively used for the control of rice sheath blight caused by Rhizoctonia solani and resistance to jinggangmycin was first reported to occur in China. A total of 128 isolates of R. solani from Anhui Province of China were characterised for the baseline sensitivity to thifluzamide. The isolates were very sensitive to thifluzamide and the baseline sensitivity curve was unimodal with an average EC50 value of 0.058 ± 0.012 µg mL?1. However, EC50 values of boscalid (another SDHI fungicide) for inhibition of mycelial growth of 22 arbitrarily selected R. solani isolates ranged from 1.89 to 2.68 µg mL?1. Thifluzamide applied at 110 µg mL?1 exhibited excellent protective and curative activity against rice sheath blight and provided 81.1–91.0% protective or curative control efficacy. In field trials in 2010 and 2011, control efficacies of thifluzamide at 82 g.a.i ha?1 15 and 30 days after second application were 84.2% and 86.7%, respectively, suggesting excellent activity against sheath blight. There was a statistically significant difference in the efficacy between thifluzamide and boscalid or jinggangmycin. These results suggested that thifluzamide should be a good alternative fungicide to jinggangmycin for the control of rice sheath blight.  相似文献   

17.
A new, simple and sensitive spectrofluorimetric method has been developed for the determination of pregabalin (PG) in capsules. The method is based on the reaction between pregabalin and fluorescamine in borate buffer solution of pH 10 to give a highly fluorescent derivative that is measured at 487 nm after excitation at 390 nm. The different experimental parameters affecting the development and stability of the reaction product were carefully studied and optimized. The fluorescence intensity concentration plot was rectilinear over the range of 0.01–0.3 µg mL?1 with a lower detection limit of 0.0017 µg mL?1 and limit of quantitation of 0.005 µg mL?1. The developed method was successfully applied to the analysis of the drug in its commercial capsules. The mean percentage recovery of PG in its capsule was 99.93±1.24 (n = 3). Statistical comparison of the results with those of the comparison method revealed good agreement and proved that there was no significant difference in the accuracy and precision of the two methods. A proposed reaction pathway was postulated. Copyright © 2010 John Wiley & Sons, Ltd.  相似文献   

18.
Grapevine trunk pathogens (GTPs) cause serious damage to grapevines and have significant economic impacts. There is no effective protection against grapevine trunk diseases. Newly designed AgSe nanoparticles (NPs) and CuSe NPs, single-element Ag NPs, Cu NPs, Se NPs and selected chemicals or chemical agents such as sodium arsenite, 8-hydroxyquinoline, silver nitrate, colloidal silver, Altron Silver fertilizer and silver thiosulfate complex (NH4)3/Ag(S2O3)2 were tested in vitro against two serious GTPs Diaporthe eres, Eutypa lata and Diplodia seriata isolated from walnut. The most significant inhibition of fungal growth was observed for silver nitrate and AgSe NPs, which showed the highest level of half the maximum effective EC50 concentration with the lowest concentrations. In the case of silver nitrate at a concentration of 1000 mg L−1, 79% inhibition of mycelial growth was observed for the pathogen E. lata, 48% for D. seriata and 54% for D. eres. AgSe NPs, in which the concentration of silver is 2588 mg L−1 and that of selenium is 902 mg L−1, showed 68% inhibition of mycelial growth in the pathogen E. lata, 54% in D. seriata and 58% in D. eres.  相似文献   

19.
The essential oil from the annual plant Lepidium virginicum L. was chemically characterized in three consecutive years (2018–2020). The essential oils were evaluated in vitro and in situ on the causal agent of anthracnose in tamarillo fruits (Solanum betaceum). The main volatile constituents were phenylacetonitrile (>60 %), linalool (>10 %), limonene (>7 %) and α-terpineol (>5 %). The essential oil (MIC, 19–30 μg mL−1), phenylacetonitrile (MIC, 45 μg mL−1) and α-terpineol (MIC, 73 μg mL−1) caused a significant inhibition in the conidial viability from a wild strain of Colletotrichum acutatum, which was isolated and identified as a causal agent of anthracnose. The inoculation of conidia from C. acutatum in non-symptomatic tamarillo fruits, followed by the in situ treatment with different concentrations of the essential oil (>30 μg mL−1), phenylacetonitrile and α-terpineol, significantly (p<0.01) avoided the degradation of anthocyanins (delphinidin 3-O-rutinoside, cyanidin 3-O-rutinoside and pelargonidin 3-O-rutinoside) and carotenoids (β-cryptoxanthin and β-carotene) as well as retarded yellowing and necrosis triggered by anthracnose at least for 10 days. Our results suggest the potential use of the essential oil from L. virginicum as a natural component to preserve the nutraceutical content of tamarillo fruits against C. acutatum infection.  相似文献   

20.
The extraction and characterization of the essential oils (EO) from Satureja montana L., Myristica fragrans H. and Cymbopogon flexuosus and the determination of their antibacterial and antioxidant activities were achieved. The EO were identified by gas chromatography/mass spectrometry and quantified by gas chromatography using a flame ionization detector. The antibacterial potential against Escherichia coli and Staphylococcus aureus was evaluated by cell susceptibility assays and by scanning electron microscopy. The antioxidant activity was evaluated by the 2,2-diphenyl-1-picrylhydrazyl assay, by β-carotene bleaching and by determining the reducing power. Borneol (36·18%), γ-terpineol (12·66%) and carvacrol (11·07%) were the principal components in the EO from S. montana, and sabinene (49·23%) and α-pinene (13·81%) were found in the EO from M. fragrans. Geranial (59·66%) and neral (38·98%) isomers were the only major components in the EO from C. flexuosus. The EO from S. montana was effective against E. coli, with minimum inhibitory and bactericidal concentrations (MIC and MBC) of 6·25 µl ml−1, whereas bactericidal potential against both was observed for the EO from M. fragrans; MIC = 6·25 µl ml−1 for S. aureus and MBC = 12·5 µl ml−1 for E. coli. A significant protective role on lipid substrates in the β-carotene bleaching assay was seen for the EO from S. montana and M. fragrans. Overall, such EO can be promising agents against pathogenic bacteria and for protecting biomolecules during oxidative stress.  相似文献   

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