Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A

Energy Technology Data Exchange (ETDEWEB)

Quinlan, Casey L.; Kaiser, Stephen E.; Bolaños, Ben; Nowlin, Dawn; Grantner, Rita; Karlicek-Bryant, Shannon; Feng, Jun Li; Jenkinson, Stephen; Freeman-Cook, Kevin; Dann, Stephen G.; Wang, Xiaoli; Wells, Peter A.; Fantin, Valeria R.; Stewart, Al E.; Grant, Stephan K. (Pfizer)

2017-05-29

S-Adenosyl-L-methionine (SAM) is an enzyme cofactor used in methyl transfer reactions and polyamine biosynthesis. The biosynthesis of SAM from ATP and L-methionine is performed by the methionine adenosyltransferase enzyme family (Mat; EC 2.5.1.6). Human methionine adenosyltransferase 2A (Mat2A), the extrahepatic isoform, is often deregulated in cancer. We identified a Mat2A inhibitor, PF-9366, that binds an allosteric site on Mat2A that overlaps with the binding site for the Mat2A regulator, Mat2B. Studies exploiting PF-9366 suggested a general mode of Mat2A allosteric regulation. Allosteric binding of PF-9366 or Mat2B altered the Mat2A active site, resulting in increased substrate affinity and decreased enzyme turnover. These data support a model whereby Mat2B functions as an inhibitor of Mat2A activity when methionine or SAM levels are high, yet functions as an activator of Mat2A when methionine or SAM levels are low. The ramification of Mat2A activity modulation in cancer cells is also described.

Trypanosoma cruzi response to sterol biosynthesis inhibitors: morphophysiological alterations leading to cell death.

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Rafael Luis Kessler

Full Text Available The protozoan parasite Trypanosoma cruzi displays similarities to fungi in terms of its sterol lipid biosynthesis, as ergosterol and other 24-alkylated sterols are its principal endogenous sterols. The sterol pathway is thus a potential drug target for the treatment of Chagas disease. We describe here a comparative study of the growth inhibition, ultrastructural and physiological changes leading to the death of T. cruzi cells following treatment with the sterol biosynthesis inhibitors (SBIs ketoconazole and lovastatin. We first calculated the drug concentration inhibiting epimastigote growth by 50% (EC(50/72 h or killing all cells within 24 hours (EC(100/24 h. Incubation with inhibitors at the EC(50/72 h resulted in interesting morphological changes: intense proliferation of the inner mitochondrial membrane, which was corroborated by flow cytometry and confocal microscopy of the parasites stained with rhodamine 123, and strong swelling of the reservosomes, which was confirmed by acridine orange staining. These changes to the mitochondria and reservosomes may reflect the involvement of these organelles in ergosterol biosynthesis or the progressive autophagic process culminating in cell lysis after 6 to 7 days of treatment with SBIs at the EC(50/72 h. By contrast, treatment with SBIs at the EC(100/24 h resulted in rapid cell death with a necrotic phenotype: time-dependent cytosolic calcium overload, mitochondrial depolarization and reservosome membrane permeabilization (RMP, culminating in cell lysis after a few hours of drug exposure. We provide the first demonstration that RMP constitutes the "point of no return" in the cell death cascade, and propose a model for the necrotic cell death of T. cruzi. Thus, SBIs trigger cell death by different mechanisms, depending on the dose used, in T. cruzi. These findings shed new light on ergosterol biosynthesis and the mechanisms of programmed cell death in this ancient protozoan parasite.

A reassessment of the risk of rust fungi developing resistance to fungicides.

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Oliver, Richard P

2014-11-01

Rust fungi are major pathogens of many annual and perennial crops. Crop protection is largely based on genetic and chemical control. Fungicide resistance is a significant issue that has affected many crop pathogens. Some pathogens have rapidly developed resistance and hence are regarded as high-risk species. Rust fungi have been classified as being low risk, in spite of sharing many relevant features with high-risk pathogens. An examination of the evidence suggests that rust fungi may be wrongly classified as low risk. Of the nine classes of fungicide to which resistance has developed, six are inactive against rusts. The three remaining classes are quinone outside inhibitors (QoIs), demethylation inhibitors (DMIs) and succinate dehydrogenase inhibitors (SDHIs). QoIs have been protected by a recently discovered intron that renders resistant mutants unviable. Low levels of resistance have developed to DMIs, but with limited field significance. Older SDHI fungicides were inactive against rusts. Some of the SDHIs introduced since 2003 are active against rusts, so it may be that insufficient time has elapsed for resistance to develop, especially as SDHIs are generally sold in mixtures with other actives. It would therefore seem prudent to increase the level of vigilance for possible cases of resistance to established and new fungicides in rusts. © 2014 Society of Chemical Industry.

Nucleic adaptability of heterokaryons to fungicides in a multinucleate fungus, Sclerotinia homoeocarpa.

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Kessler, Dylan; Sang, Hyunkyu; Bousquet, Amanda; Hulvey, Jonathan P; Garcia, Dawlyn; Rhee, Siyeon; Hoshino, Yoichiro; Yamada, Toshihiko; Jung, Geunhwa

2018-06-01

Sclerotinia homoeocarpa is the causal organism of dollar spot in turfgrasses and is a multinucleate fungus with a history of resistance to multiple fungicide classes. Heterokaryosis gives rise to the coexistence of genetically distinct nuclei within a cell, which contributes to genotypic and phenotypic plasticity in multinucleate fungi. We demonstrate that field isolates, resistant to either a demethylation inhibitor or methyl benzimidazole carbamate fungicide, can form heterokaryons with resistance to each fungicide and adaptability to serial combinations of different fungicide concentrations. Field isolates and putative heterokaryons were assayed on fungicide-amended media for in vitro sensitivity. Shifts in fungicide sensitivity and microsatellite genotypes indicated that heterokaryons could adapt to changes in fungicide pressure. Presence of both nuclei in heterokaryons was confirmed by detection of a single nucleotide polymorphism in the β-tubulin gene, the presence of microsatellite alleles of both field isolates, and the live-cell imaging of two different fluorescently tagged nuclei using laser scanning confocal microscopy. Nucleic adaptability of heterokaryons to fungicides was strongly supported by the visualization of changes in fluorescently labeled nuclei to fungicide pressure. Results from this study suggest that heterokaryosis is a mechanism by which the pathogen adapts to multiple fungicide pressures in the field. Copyright © 2018 Elsevier Inc. All rights reserved.

Glyoxal bis(guanylhydrazone) as an inhibitor of polyamine biosynthesis in tumour cells.

OpenAIRE

Seppänen, P; Fagerström, R; Alhonen-Hongisto, L; Elo, H; Lumme, P; Jänne, J

1984-01-01

Glyoxal bis(guanylhydrazone), the parent compound of methylglyoxal bis(guanylhydrazone), was synthesized and tested for its ability to inhibit the biosynthesis of polyamines. It was found to be a powerful competitive inhibitor of adenosylmethionine decarboxylase (EC 4.1.1.50), yet the lack of the methyl group at the glyoxal portion increased the apparent Ki value for the enzyme by about 30-fold in comparison with methylglyoxal bis(guanylhydrazone). Glyoxal bis(guanylhydrazone) inhibited diami...

Identification of novel bacterial histidine biosynthesis inhibitors using docking, ensemble rescoring, and whole-cell assays

DEFF Research Database (Denmark)

Henriksen, Signe Teuber; Liu, J.; Estiu, G.

2010-01-01

histidine biosynthesis pathway, which is predicted to be essential for bacterial biomass productions. Virtual screening of a library of similar to 10(6) compounds identified 49 potential inhibitors of three enzymes of this pathway. Eighteen representative compounds were directly tested on three S. aureus......-and two Escherichia coli strains in standard disk inhibition assays. Thirteen compounds are inhibitors of some or all of the S. aureus strains, while 14 compounds weakly inhibit growth in one or both E. coli strains. The high hit rate obtained from a fast virtual screen demonstrates the applicability...

Synergistic mortality between a neonicotinoid insecticide and an ergosterol-biosynthesis-inhibiting fungicide in three bee species.

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Sgolastra, Fabio; Medrzycki, Piotr; Bortolotti, Laura; Renzi, Maria Teresa; Tosi, Simone; Bogo, Gherardo; Teper, Dariusz; Porrini, Claudio; Molowny-Horas, Roberto; Bosch, Jordi

2017-06-01

Neonicotinoid insecticides have been identified as an important factor contributing to bee diversity declines. Nonetheless, uncertainties remain about their impact under field conditions. Most studies have been conducted on Apis mellifera and tested single compounds. However, in agricultural environments, bees are often exposed to multiple pesticides. We explore the synergistic mortality between a neonicotinoid (clothianidin) and an ergosterol-biosynthesis-inhibiting fungicide (propiconazole) in three bee species (A. mellifera, Bombus terrestris, Osmia bicornis) following oral exposure in the laboratory. We developed a new approach based on the binomial proportion test to analyse synergistic interactions. We estimated uptake of clothianidin per foraging bout in honey bees foraging on seed-coated rapeseed fields. We found significant synergistic mortality in all three bee species exposed to non-lethal doses of propiconazole and their respective LD 10 of clothianidin. Significant synergism was only found at the first assessment times in A. mellifera (4 and 24 h) and B. terrestris (4 h), but persisted throughout the experiment (96 h) in O. bicornis. O. bicornis was also the most sensitive species to clothianidin. Our results underscore the importance to test pesticide combinations likely to occur in agricultural environments, and to include several bee species in environmental risk assessment schemes. © 2016 Society of Chemical Industry. © 2016 Society of Chemical Industry.

The Fungicidal Activity of Thymol against Fusarium graminearum via Inducing Lipid Peroxidation and Disrupting Ergosterol Biosynthesis

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Tao Gao

2016-06-01

Full Text Available Thymol is a natural plant-derived compound that has been widely used in pharmaceutical and food preservation applications. However, the antifungal mechanism for thymol against phytopathogens remains unclear. In this study, we identified the antifungal action of thymol against Fusarium graminearum, an economically important phytopathogen showing severe resistance to traditional chemical fungicides. The sensitivity of thymol on different F. graminearum isolates was screened. The hyphal growth, as well as conidial production and germination, were quantified under thymol treatment. Histochemical, microscopic, and biochemical approaches were applied to investigate thymol-induced cell membrane damage. The average EC50 value of thymol for 59 F. graminearum isolates was 26.3 μg·mL−1. Thymol strongly inhibited conidial production and hyphal growth. Thymol-induced cell membrane damage was indicated by propidium iodide (PI staining, morphological observation, relative conductivity, and glycerol measurement. Thymol induced a significant increase in malondialdehyde (MDA concentration and a remarkable decrease in ergosterol content. Taken together, thymol showed potential antifungal activity against F. graminearum due to the cell membrane damage originating from lipid peroxidation and the disturbance of ergosterol biosynthesis. These results not only shed new light on the antifungal mechanism of thymol, but also imply a promising alternative for the control of Fusarium head blight (FHB disease caused by F. graminearum.

Suppression of hop looper (Lepidoptera: Noctuidae) by the fungicide pyraclostrobin.

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Woods, J L; Gent, D H

2014-04-01

The hop looper, Hypena humuli Harris, is a reemergent pest of hop that often requires treatment to mitigate crop damage. In 4 yr of field trials, plots treated with fungicides were observed to sustain less hop looper defoliation compared with nontreated plots. Further investigation revealed that abundance of hop looper and associated defoliation were reduced when the fungicide pyraclostrobin was applied in late July to early August. Two other fungicides possessing active ingredients in the same chemical family (quinone outside inhibitor) did not reduce abundance of hop looper or its defoliation. Pyraclostrobin is efficacious against powdery mildew diseases, and the application timing evaluated in these studies corresponds with a period of juvenile susceptibility of hop cones to the disease. Use of fungicides containing pyraclostrobin at this time may have the ancillary benefit of reducing hop looper damage, potentially obviating the need for broad-spectrum insecticides later in the season. Follow-up studies are warranted to determine whether pyraclostrobin may inhibit other lepidopteran species.

Pharmacokinetics, Pharmacodynamics, and Stereoselective Metabolism of the 1,2,4-Triazole Fungicide, Triadimefon, in Vertebrate Species

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Questions Agricultural and pharmaceutical 1,2,4-triazole fungicides are potent cytochrome P450 modulators that can disrupt mammalian steroid biosynthesis. Triadimefon [(RS)-1-(4-chlorophenoxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one] is unique with respect to tumorige...

Effects of Conazole Fungicides on Spontaneous Activity in Neural Networks

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Hexaconazole (HEX), Tetraconazole (TET), Fluconazole (FLU), and Triadimefon (TRI) are conazole fungicides, used to control powdery mildews on crops, and as veterinary and clinical treatments. TRI, a demethylation inhibitor, is neurotoxic in vivo, and previous in vitro experiments...

Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis.

Science.gov (United States)

Francisco, Gerardo D; Li, Zhong; Albright, J Donald; Eudy, Nancy H; Katz, Alan H; Petersen, Peter J; Labthavikul, Pornpen; Singh, Guy; Yang, Youjun; Rasmussen, Beth A; Lin, Yang-I; Mansour, Tarek S

2004-01-05

Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and PRSP. 3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria.

Glyoxal bis(guanylhydrazone) as an inhibitor of polyamine biosynthesis in tumour cells.

Science.gov (United States)

Seppänen, P; Fagerström, R; Alhonen-Hongisto, L; Elo, H; Lumme, P; Jänne, J

1984-07-15

Glyoxal bis(guanylhydrazone), the parent compound of methylglyoxal bis(guanylhydrazone), was synthesized and tested for its ability to inhibit the biosynthesis of polyamines. It was found to be a powerful competitive inhibitor of adenosylmethionine decarboxylase (EC 4.1.1.50), yet the lack of the methyl group at the glyoxal portion increased the apparent Ki value for the enzyme by about 30-fold in comparison with methylglyoxal bis(guanylhydrazone). Glyoxal bis(guanylhydrazone) inhibited diamine oxidase (EC 1.4.3.6) activity as effectively as did methylglyoxal bis(guanylhydrazone). The cellular accumulation curves of glyoxal bis(guanylhydrazone) in L1210 cells were practically superimposable with those of methylglyoxal bis(guanylhydrazone), and the uptake of both compounds was distinctly stimulated by a prior treatment with 2-difluoromethylornithine. The drug decreased the concentration of spermidine in a dose-dependent manner and, in contrast with methylglyoxal bis(guanylhydrazone), without a concomitant accumulation of putrescine. The fact that putrescine concentrations were decreased in cells exposed to glyoxal bis(guanylhydrazone) was, at least in part, attributable to an inhibition of ornithine decarboxylase (EC 4.1.1.17) activity in cells treated with the compound. Under these experimental conditions equivalent concentrations of methylglyoxal bis(guanylhydrazone) [1,1'-[(methylethanediylidine)dinitrilo]diguanidine] elicited large increases in the enzyme activity. When combined with difluoromethylornithine, glyoxal bis(guanylhydrazone) potentiated the growth-inhibitory effect of that drug. Taking into consideration the proven anti-leukaemic activity of glyoxal bis(guanylhydrazone), its effectiveness to inhibit spermidine biosynthesis (without raising the concentration of putrescine) as well as its suitability for combined use with inhibitors of ornithine decarboxylase, this drug is apparently worthy of further testing in tumour-bearing animals, especially in

Trichoderma harzianum: Inhibition of mycotoxin producing fungi and toxin biosynthesis.

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Braun, H; Woitsch, L; Hetzer, B; Geisen, R; Zange, B; Schmidt-Heydt, M

2018-04-19

A quarter of the world-wide crop is spoiled by filamentous fungi and their mycotoxins and weather extremes associated with the climate change lead to further deterioration of the situation. The ingestion of mycotoxins causes several health issues leading in the worst case to cancer in humans and animals. Common intervention strategies against mycotoxin producing fungi, such as the application of fungicides, may result in undesirable residues and in some cases to a stress induction of mycotoxin biosynthesis. Moreover, development of fungicide resistances has greatly impacted pre- and postharvest fungal diseases. Hence there is the need to develop alternative strategies to reduce fungal infestation and thus mycotoxin contamination in the food chain. Such a strategy for natural competition of important plant-pathogenic and mycotoxin producing fungi could be Trichoderma harzianum, a mycoparasitic fungus. Especially in direct comparison to certain tested fungicides, the inhibition of different tested fungal species by T. harzianum was comparable, more sustainable and in some cases more effective, too. Besides substantially reduced growth rates, a transcriptional based inhibition of mycotoxin biosynthesis in the competed Aspergillus species could be shown. Furthermore it could be clearly observed by high-resolution Scanning Electron Microscopy (SEM) that T. harzianum actively attaches to the competitor species followed by subsequent enzymatic lysis of those mycelial filaments. The analyzed isolate of T. harzianum MRI349 is not known to produce mycotoxins. In this study it could be successfully proven that T. harzianum as a biological competitor is an effective complement to the use of fungicides. Copyright © 2018 Elsevier B.V. All rights reserved.

Residue-free wines: fate of some quinone outside inhibitor (QoI) fungicides in the winemaking process.

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Garau, Vincenzo Luigi; De Melo Abreu, Susana; Caboni, Pierluigi; Angioni, Alberto; Alves, Arminda; Cabras, Paolo

2009-03-25

The fate of three fungicide residues (fenamidone, pyraclostrobin, and trifloxystrobin) from vine to wine was studied to evaluate the decay ratio and the influence of the technological process. The aim of this work was to identify pesticides that can degrade rapidly or be eliminated together with byproduct (lees and cake) of the winemaking process to obtain wine free of residues. The disappearance rate on grapes was calculated as pseudo-first-order kinetics, and the half-life (t(1/2)) was in the range from 5.4 +/- 1.9 to 12.2 +/- 1.2 days. The mechanism of dissipation of the three quinone outside inhibitor (QoI) fungicides was studied using different model systems. It was observed that the main mechanism responsible for disappearance was photodegradation. For active ingredients (ai) the half-lives of fenamidone, pyraclostrobin, and trifloxystrobin were 10.2 +/- 0.8, 20.1 +/- 0.1, and 8.6 +/- 1.0 h, respectively, whereas for formulation higher half-lives were observed when epicuticular waxes were present (from 13.8 +/- 0.2 to 26.6 +/- 0.1 h). After winemaking, fenamidone, pyraclostrobin, and trifloxystrobin residues were not detected in the wine, but they were present in the cake and lees. This was due to the adsorption of pesticide residues to the solid parts, which are always eliminated at the end of the alcoholic fermentation. The data obtained in these experiments suggest that these three active ingredients could be used in a planning process to obtain residue-free wines.

Effects of Oral Exposure to Fungicides on Honey Bee Nutrition and Virus Levels.

Science.gov (United States)

Degrandi-Hoffman, Gloria; Chen, Yanping; Watkins Dejong, Emily; Chambers, Mona L; Hidalgo, Geoffrey

2015-12-01

Sublethal exposure to fungicides can affect honey bees (Apis mellifera L.) in ways that resemble malnutrition. These include reduced brood rearing, queen loss, and increased pathogen levels. We examined the effects of oral exposure to the fungicides boscalid and pyraclostrobin on factors affecting colony nutrition and immune function including pollen consumption, protein digestion, hemolymph protein titers, and changes in virus levels. Because the fungicides are respiratory inhibitors, we also measured ATP concentrations in flight muscle. The effects were evaluated in 3- and 7-d-old worker bees at high fungicide concentrations in cage studies, and at field-relevant concentrations in colony studies. Though fungicide levels differed greatly between the cage and colony studies, similar effects were observed. Hemolymph protein concentrations were comparable between bees feeding on pollen with and without added fungicides. However, in both cage and colony studies, bees consumed less pollen containing fungicides and digested less of the protein. Bees fed fungicide-treated pollen also had lower ATP concentrations and higher virus titers. The combination of effects we detected could produce symptoms that are similar to those from poor nutrition and weaken colonies making them more vulnerable to loss from additional stressors such as parasites and pathogens. Published by Oxford University Press on behalf of Entomological Society of America 2015. This work is written by US Government employees and is in the public domain in the US.

Effects of Sublethal Fungicides on Mutation Rates and Genomic Variation in Fungal Plant Pathogen, Sclerotinia sclerotiorum.

Science.gov (United States)

Amaradasa, B Sajeewa; Everhart, Sydney E

2016-01-01

Pathogen exposure to sublethal doses of fungicides may result in mutations that may represent an important and largely overlooked mechanism of introducing new genetic variation into strictly clonal populations, including acquisition of fungicide resistance. We tested this hypothesis using the clonal plant pathogen, Sclerotinia sclerotiorum. Nine susceptible isolates were exposed independently to five commercial fungicides with different modes of action: boscalid (respiration inhibitor), iprodione (unclear mode of action), thiophanate methyl (inhibition of microtubulin synthesis) and azoxystrobin and pyraclostrobin (quinone outside inhibitors). Mycelium of each isolate was inoculated onto a fungicide gradient and sub-cultured from the 50-100% inhibition zone for 12 generations and experiment repeated. Mutational changes were assessed for all isolates at six neutral microsatellite (SSR) loci and for a subset of isolates using amplified fragment length polymorphisms (AFLPs). SSR analysis showed 12 of 85 fungicide-exposed isolates had a total of 127 stepwise mutations with 42 insertions and 85 deletions. Most stepwise deletions were in iprodione- and azoxystrobin-exposed isolates (n = 40/85 each). Estimated mutation rates were 1.7 to 60-fold higher for mutated loci compared to that expected under neutral conditions. AFLP genotyping of 33 isolates (16 non-exposed control and 17 fungicide exposed) generated 602 polymorphic alleles. Cluster analysis with principal coordinate analysis (PCoA) and discriminant analysis of principal components (DAPC) identified fungicide-exposed isolates as a distinct group from non-exposed control isolates (PhiPT = 0.15, P = 0.001). Dendrograms based on neighbor-joining also supported allelic variation associated with fungicide-exposure. Fungicide sensitivity of isolates measured throughout both experiments did not show consistent trends. For example, eight isolates exposed to boscalid had higher EC50 values at the end of the experiment, and

Effects of Sublethal Fungicides on Mutation Rates and Genomic Variation in Fungal Plant Pathogen, Sclerotinia sclerotiorum.

Directory of Open Access Journals (Sweden)

B Sajeewa Amaradasa

Full Text Available Pathogen exposure to sublethal doses of fungicides may result in mutations that may represent an important and largely overlooked mechanism of introducing new genetic variation into strictly clonal populations, including acquisition of fungicide resistance. We tested this hypothesis using the clonal plant pathogen, Sclerotinia sclerotiorum. Nine susceptible isolates were exposed independently to five commercial fungicides with different modes of action: boscalid (respiration inhibitor, iprodione (unclear mode of action, thiophanate methyl (inhibition of microtubulin synthesis and azoxystrobin and pyraclostrobin (quinone outside inhibitors. Mycelium of each isolate was inoculated onto a fungicide gradient and sub-cultured from the 50-100% inhibition zone for 12 generations and experiment repeated. Mutational changes were assessed for all isolates at six neutral microsatellite (SSR loci and for a subset of isolates using amplified fragment length polymorphisms (AFLPs. SSR analysis showed 12 of 85 fungicide-exposed isolates had a total of 127 stepwise mutations with 42 insertions and 85 deletions. Most stepwise deletions were in iprodione- and azoxystrobin-exposed isolates (n = 40/85 each. Estimated mutation rates were 1.7 to 60-fold higher for mutated loci compared to that expected under neutral conditions. AFLP genotyping of 33 isolates (16 non-exposed control and 17 fungicide exposed generated 602 polymorphic alleles. Cluster analysis with principal coordinate analysis (PCoA and discriminant analysis of principal components (DAPC identified fungicide-exposed isolates as a distinct group from non-exposed control isolates (PhiPT = 0.15, P = 0.001. Dendrograms based on neighbor-joining also supported allelic variation associated with fungicide-exposure. Fungicide sensitivity of isolates measured throughout both experiments did not show consistent trends. For example, eight isolates exposed to boscalid had higher EC50 values at the end of the

Effects of Sublethal Fungicides on Mutation Rates and Genomic Variation in Fungal Plant Pathogen, Sclerotinia sclerotiorum

Science.gov (United States)

Amaradasa, B. Sajeewa

2016-01-01

Pathogen exposure to sublethal doses of fungicides may result in mutations that may represent an important and largely overlooked mechanism of introducing new genetic variation into strictly clonal populations, including acquisition of fungicide resistance. We tested this hypothesis using the clonal plant pathogen, Sclerotinia sclerotiorum. Nine susceptible isolates were exposed independently to five commercial fungicides with different modes of action: boscalid (respiration inhibitor), iprodione (unclear mode of action), thiophanate methyl (inhibition of microtubulin synthesis) and azoxystrobin and pyraclostrobin (quinone outside inhibitors). Mycelium of each isolate was inoculated onto a fungicide gradient and sub-cultured from the 50–100% inhibition zone for 12 generations and experiment repeated. Mutational changes were assessed for all isolates at six neutral microsatellite (SSR) loci and for a subset of isolates using amplified fragment length polymorphisms (AFLPs). SSR analysis showed 12 of 85 fungicide-exposed isolates had a total of 127 stepwise mutations with 42 insertions and 85 deletions. Most stepwise deletions were in iprodione- and azoxystrobin-exposed isolates (n = 40/85 each). Estimated mutation rates were 1.7 to 60-fold higher for mutated loci compared to that expected under neutral conditions. AFLP genotyping of 33 isolates (16 non-exposed control and 17 fungicide exposed) generated 602 polymorphic alleles. Cluster analysis with principal coordinate analysis (PCoA) and discriminant analysis of principal components (DAPC) identified fungicide-exposed isolates as a distinct group from non-exposed control isolates (PhiPT = 0.15, P = 0.001). Dendrograms based on neighbor-joining also supported allelic variation associated with fungicide-exposure. Fungicide sensitivity of isolates measured throughout both experiments did not show consistent trends. For example, eight isolates exposed to boscalid had higher EC50 values at the end of the experiment

Amelioration in secretion of hyperthermostable and Ca2+ -independent alpha-amylase of Geobacillus thermoleovorans by some polyamines and their biosynthesis inhibitor methylglyoxal-bis-guanylhydrazone.

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Uma Maheswar Rao, J L; Satyanarayana, T

2004-01-01

Effect of polyamines and their biosynthesis inhibitors on the production of hyperthermostable and Ca2+ -independent alpha-amylase by Geobacillus thermoleovorans MTCC 4220. The alpha-amylase was produced in starch-yeast extract-tryptone (SYT) broth with different polyamines (PA) and polyamine biosynthesis inhibitors, methylglyoxal-bis-guanylhydrazone (MGBG) and cyclohexylammonium sulphate (CHA) at 70 degrees C. The bacterial pellets were obtained after growing G. thermoleovorans at different temperatures, and used in determining total PA. The cell-free culture filtrates were used in alpha-amylase assays. During growth, total polyamines in biomass increased till 2 h, and thereafter, decreased gradually. The total polyamine content was very high in the biomass cultivated at 55 degrees C when compared with that of higher temperatures. Enzyme titre enhanced up to 70 degrees C, and thereafter declined. Extracellular enzyme and protein levels declined in the presence of exogenously added PA. The intracellular enzyme titres, however, were higher in putrescine (put) and spermidine (spd) than in spermine (spm). Polyamine biosynthesis inhibitor, MGBG enhanced secretion of alpha-amylase in a laboratory fermentor as well as shake flasks, although CHA did not affect it. The intracellular accumulation of put in the presence of MGBG appeared to enhance synthesis and secretion of alpha-amylase. Extracellular enzyme and protein levels were low in the presence of exogenously added PA, but their intracellular levels, however, were higher in put and spd than in spm. A substantial increase in the synthesis and secretion of alpha-amylase was attained in G. thermoleovorans in the presence of polyamine biosynthesis inhibitor MGBG.

Differential effects of lipid biosynthesis inhibitors on Zika and Semliki Forest viruses.

Science.gov (United States)

Royle, Jamie; Donald, Claire L; Merits, Andres; Kohl, Alain; Varjak, Margus

2017-12-01

The recent outbreak of infection with Zika virus (ZIKV; Flaviviridae) has attracted attention to this previously neglected mosquito-borne pathogen and the need for efficient therapies. Since flavivirus replication is generally known to be dependent on fatty acid biosynthesis, two inhibitors of this pathway, 5-(tetradecyloxyl)-2-furoic acid (TOFA) and cerulenin, were tested for their potentiality to inhibit virus replication. At concentrations previously shown to inhibit the replication of other flaviviruses, neither drug had a significant antiviral affect against ZIKV, but reduced the replication of the non-related mosquito-borne Semliki Forest virus (Togaviridae). Copyright © 2017 The Authors. Published by Elsevier Ltd.. All rights reserved.

Fluridone and norflurazon, carotenoid-biosynthesis inhibitors, promote seed conditioning and germination of the holoparasite Orobanche minor.

Science.gov (United States)

Chae, Sang Heon; Yoneyama, Koichi; Takeuchi, Yasutomo; Joel, Daniel M.

2004-02-01

Fluridone and norflurazon, two carotenoid-biosynthesis inhibitors, shortened the conditioning period required by seeds of Orobanche minor in order to respond to the germination stimulant strigol. Neither fluridone nor norflurazon alone induced seed germination of O. minor, they promoted strigol-induced germination. In addition, these compounds restored the conditioning and germination of seeds at a supraoptimal temperature (30 degrees C) as well as in the light. Gibberellic acid (GA(3)) showed similar promotive and protective effects on the conditioning and germination of O. minor seeds. Although fluridone and norflurazon are known to prevent abscisic acid (ABA)-biosynthesis, and stresses such as supraoptimal temperatures have been reported to induce ABA accumulation in plants, the amount of ABA in the seeds or that released from the seeds into the conditioning media was not affected by the fluridone treatment and by exposure to the supraoptimal temperature. These results indicate that the promotive and protective effects of fluridone and norflurazon on the conditioning and germination of O. minor seeds would be attributed to other perturbations rather than the inhibition of ABA-biosynthesis.

Effects of oral exposure to fungicides on honey bee nutrition and immunity

Science.gov (United States)

Worker bees fed pollen containing fungicides (boscalid and pyraclostrobin) that are respiratory inhibitors had lower ATP concentrations in thoracic muscle tissue than those fed untreated pollen in both cage and colony studies. Midgut protease activity, used an indicator of consumption, was higher in...

Effects of polyamine biosynthesis inhibitors on S-adenosylmethionine synthetase and S-adenosylmethionine decarboxylase activities in carrot cell cultures

Science.gov (United States)

S.C. Minocha; R. Minocha; A. Komamine

1991-01-01

Changes in the activites of S-adcnosylmethionine (SAM) synthetase (methionine adenosyltransferase, EC 2.5.1.6.) and SAM decarboxylase (EC 4.1.1.50) were studied in carrot (Daucus carota) cell cultures in response to 2,4-dichlorophenoxyacetic acid (2,4-D) and several inhibitors of polyamine biosynthesis. Activity of SAM synthetase increased...

Rieske iron-sulfur protein of the cytochrome bc(1) complex: a potential target for fungicide discovery.

Science.gov (United States)

Yang, Wen-Chao; Li, Hui; Wang, Fu; Zhu, Xiao-Lei; Yang, Guang-Fu

2012-07-23

The cytochrome bc(1) complex (complex III, cyt bc(1)) is an essential component of cellular respiration. Cyt bc(1) has three core subunits that are required for its catalytic activity: cytochrome b, cytochrome c(1), and the Rieske iron-sulfur protein (ISP). Although most fungicides inhibit this enzyme by binding to the cytochrome b subunit, resistance to these fungicides has developed rapidly due to their widespread application. Resistance is mainly associated with mutations in cytochrome b, the only subunit encoded by mitochondrial DNA. Recently, the flexibility and motion of the ISP and its essential role in electron transfer have received intense attention; this leads us to propose a new classification of cyt bc(1) inhibitors (three types of Q(o) inhibitors) that mobilize, restrict, or fix the rotation of the ISP. Importantly, the strengths of the ISP-inhibitor interactions correlate with inhibitor activity and the development of resistance to Q(o) inhibitors, thereby offering clues for designing novel cyt bc(1) inhibitors with high potency and a low risk of resistance. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurF.

Science.gov (United States)

Sova, Matej; Kovac, Andreja; Turk, Samo; Hrast, Martina; Blanot, Didier; Gobec, Stanislav

2009-12-01

Enzymes involved in the biosynthesis of bacterial peptidoglycan represent important targets for development of new antibacterial drugs. Among them, Mur ligases (MurC to MurF) catalyze the formation of the final cytoplasmic precursor UDP-N-acetylmuramyl-pentapeptide from UDP-N-acetylmuramic acid. We present the design, synthesis and biological evaluation of a series of phosphorylated hydroxyethylamines as new type of small-molecule inhibitors of Mur ligases. We show that the phosphate group attached to the hydroxyl moiety of the hydroxyethylamine core is essential for good inhibitory activity. The IC(50) values of these inhibitors were in the micromolar range, which makes them a promising starting point for the development of multiple inhibitors of Mur ligases as potential antibacterial agents. In addition, 1-(4-methoxyphenylsulfonamido)-3-morpholinopropan-2-yl dihydrogen phosphate 7a was discovered as one of the best inhibitors of MurE described so far.

Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells

Directory of Open Access Journals (Sweden)

Liang Y

2016-05-01

growth of aggressive castration-resistant human prostate cancer cell xenografts in vivo without any signs of toxicity to experimental animals. Importantly, RO did not reduce the viability of normal prostate cells in vitro. Our study is the first to demonstrate that the cholesterol biosynthesis inhibitor RO effectively suppresses growth of human prostate cancer cells. Our findings suggest that cholesterol biosynthesis inhibitors such as RO, when used in combination with commonly used chemotherapeutic drugs or ERβ specific ligands, could represent a novel therapeutic approach to prevent the growth of prostate cancer tumors. Keywords: prostate cancer, cholesterol biosynthesis inhibitor, cell viability, xenograft, castration resistant

Binding of the respiratory chain inhibitor ametoctradin to the mitochondrial bc1 complex.

Science.gov (United States)

Fehr, Marcus; Wolf, Antje; Stammler, Gerd

2016-03-01

Ametoctradin is an agricultural fungicide that inhibits the mitochondrial bc1 complex of oomycetes. The bc1 complex has two quinone binding sites that can be addressed by inhibitors. Depending on their binding sites and binding modes, the inhibitors show different degrees of cross-resistance that need to be considered when designing spray programmes for agricultural fungicides. The binding site of ametoctradin was unknown. Cross-resistance analyses, the reduction of isolated Pythium sp. bc1 complex in the presence of different inhibitors and molecular modelling studies were used to analyse the binding site and binding mode of ametoctradin. All three approaches provide data supporting the argument that ametoctradin binds to the Pythium bc1 complex similarly to stigmatellin. The binding mode of ametoctradin differs from other agricultural fungicides such as cyazofamid and the strobilurins. This explains the lack of cross-resistance with strobilurins and related inhibitors, where resistance is mainly caused by G143A amino acid exchange. Accordingly, mixtures or alternating applications of these fungicides and ametoctradin can help to minimise the risk of the emergence of new resistant isolates. © 2015 Society of Chemical Industry.

Enhanced ethanol production, volatile compound biosynthesis and fungicide removal during growth of a newly isolated Saccharomyces cerevisiae strain on enriched pasteurized grape musts

Energy Technology Data Exchange (ETDEWEB)

Sarris, Dimitris; Kotseridis, Yorgos; Galiotou-Panayotou, Maria; Papanikolaou, Seraphim [Department of Food Science and Technology, Agricultural University of Athens (Greece); Linga, Maria [Oinognosia, Wine analysis and consulting, Kiato (Greece)

2009-02-15

The kinetic behavior of a newly isolated Saccharomyces cerevisiae strain, grown on pasteurized grape musts enriched with industrial sugars, was studied after the addition of various concentrations [0.0 (reference), 0.4 and 2.4 mg/L] of the fungicide quinoxyfen to the medium. Batch-flask cultures were carried out. Significant quantities of biomass (10.0{+-}0.8 g/L) were produced regardless of quinoxyfen addition to the medium; therefore, the addition of the fungicide did not seriously inhibit biomass production. Ethanol was synthesized in very high quantities in all trials (highest concentrations 106.4-119.2 g/L). A slight decrease of ethanol production in terms of both absolute value and conversion yield of ethanol produced per sugar consumed was, however, observed when the quinoxyfen concentration was increased. The addition of quinoxyfen led to significantly lower ethylic ester levels, which also pertains to the acetates analyzed in this study. Fusel alcohol synthesis seemed to be activated when 0.4 mg/L quinoxyfen was added, but at 2.4 mg/L of added fungicide, no statistically significant differences were observed compared with the control trial. Volatile acid levels did not present a uniform trend in relation with the added fungicide. Finally, the fermentation was accompanied by a significant reduction of the fungicide concentration (79-82 wt% fungicide removal). (Abstract Copyright [2009], Wiley Periodicals, Inc.)

Inhibitors of amino acids biosynthesis as antifungal agents.

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Jastrzębowska, Kamila; Gabriel, Iwona

2015-02-01

Fungal microorganisms, including the human pathogenic yeast and filamentous fungi, are able to synthesize all proteinogenic amino acids, including nine that are essential for humans. A number of enzymes catalyzing particular steps of human-essential amino acid biosynthesis are fungi specific. Numerous studies have shown that auxotrophic mutants of human pathogenic fungi impaired in biosynthesis of particular amino acids exhibit growth defect or at least reduced virulence under in vivo conditions. Several chemical compounds inhibiting activity of one of these enzymes exhibit good antifungal in vitro activity in minimal growth media, which is not always confirmed under in vivo conditions. This article provides a comprehensive overview of the present knowledge on pathways of amino acids biosynthesis in fungi, with a special emphasis put on enzymes catalyzing particular steps of these pathways as potential targets for antifungal chemotherapy.

Synthesis of [triazole-3(5)-14C]-propiconazole stereoisomers

International Nuclear Information System (INIS)

Hadjidemetriou, D.; Loeffler, R.T.

1992-01-01

A preparation of all four stereoisomers of the fungicide and sterol biosynthesis inhibitor propiconazole (1-[2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-ylmethyl]-1H-1,2,4-triazole), labelled with [ 14 C] in the triazole ring, is described. (author)

Modulators of membrane drug transporters potentiate the activity of the DMI fungicide oxpoconazole against Botrytis cinerea

NARCIS (Netherlands)

Hayashi, K.; Schoonbeek, H.; Waard, de M.A.

2003-01-01

Modulators known to reduce multidrug resistance in tumour cells were tested for their potency to synergize the fungitoxic activity of the fungicide oxpoconazole, a sterol demethylation inhibitor (DMI), against Botrytis cinerea Pers. Chlorpromazine, a phenothiazine compound known as a calmodulin

Mycotoxin and fungicide residues in wheat grains from fungicide-treated plants measured by a validated LC-MS method.

Science.gov (United States)

da Luz, Suzane Rickes; Pazdiora, Paulo Cesar; Dallagnol, Leandro José; Dors, Giniani Carla; Chaves, Fábio Clasen

2017-04-01

Wheat (Triticum aestivum) is an annual crop, cultivated in the winter and spring and susceptible to several pathogens, especially fungi, which are managed with fungicides. It is also one of the most consumed cereals, and can be contaminated by mycotoxins and fungicides. The objective of this study was to validate an analytical method by LC-MS for simultaneous determination of mycotoxins and fungicide residues in wheat grains susceptible to fusarium head blight treated with fungicides, and to evaluate the relationship between fungicide application and mycotoxin production. All parameters of the validated analytical method were within AOAC and ANVISA limits. Deoxynivalenol was the prevalent mycotoxin in wheat grain and epoxiconazole was the fungicide residue found in the highest concentration. All fungicidal treatments induced an increase in AFB2 production when compared to the control (without application). AFB1 and deoxynivalenol, on the contrary, were reduced in all fungicide treatments compared to the control. Copyright © 2016 Elsevier Ltd. All rights reserved.

The effect of haem biosynthesis inhibitors and inducers on intestinal iron absorption and liver haem biosynthetic enzyme activities

International Nuclear Information System (INIS)

Laftah, A.H.; Simpson, R.J.; Peters, T.J.; Raja, K.B.

2008-01-01

The relation between haem biosynthesis and intestinal iron absorption is not well understood, we therefore investigated the effect of compounds that alter haem metabolism on duodenal iron absorption. CD1 mice were treated with either an inhibitor (succinyl acetone (SA)) or stimulator (2-allyl-2-isopropylacetamide (AIA)) of haem biosynthesis. 5-Aminolaevulinic acid (ALA) dehydratase and urinary ALA and porphobilinogen (PBG) levels, were determined. Intestinal iron absorption was assayed with in vivo and in vitro techniques. Liver hepcidin (Hamp1) and duodenal iron transporter mRNA levels were measured using RT-PCR. AIA caused increased hepatic ALA synthase (1.6-fold) and ALA dehydratase (1.4-fold, both p < 0.005) activities and increased urinary ALA and PBG excretion (2.1- and 1.4-fold, p < 0.005, p < 0.05, respectively). In vivo intestinal iron absorption was reduced to 49% of control (p < 0.005). Mice treated with SA showed decreased urinary ALA and PBG levels (75 and 55% control, both p < 0.005) and reductions in both ALA synthase and ALA dehydratase activities (77 and 56% control, p < 0.05, p < 0.005, respectively) in the liver. Liver and duodenal haem and cytochrome oxidase levels were not significantly decreased. Iron absorption was enhanced (1.26-fold, p < 0.05) and hepatic Hamp1 mRNA was reduced (53% of control, p < 0.05). In vitro duodenal iron uptake after mice were injected with SA also demonstrated an increase in Fe(III) reduction and uptake (1.27- and 1.41-fold, p < 0.01 respectively). Simultaneous injections of SA and ALA blocked the enhancing effect on iron absorption seen with SA alone. We conclude that alterations in haem biosynthesis can influence iron absorption and in particular, the intermediate ALA seems to be an inhibitor of iron absorption

Mixture effects of endocrine disrupting compounds in vitro

DEFF Research Database (Denmark)

Kjærstad, Mia Birkhøj; Taxvig, Camilla; Andersen, H. R.

2010-01-01

inhibitors of androgen biosynthesis and in the steroid synthesis assay using H295R cells, the inhibition of testosterone production was close to additive, whereas the inhibition of oestradiol production was over-estimated for the mixture of azole fungicides, when compared with the effect predicted when...

Synthesis, herbicidal, fungicidal and insecticidal evaluation of 3-(dichlorophenyl)- isocoumarins and (±)-3-(dichlorophenyl)-3,4-dihydroisocoumarins

International Nuclear Information System (INIS)

Qadeer, Ghulam; Rama, Nasim Hasan; Fan, Zhi-Jin; Liu, Bin; Liu, Xiu-Feng

2007-01-01

This is the first report showing that 3-(dichlorophenyl)isocoumarins and (±)-3,4-dihydroisocoumarins are plant and plant fungus growth inhibitors. 3-Dichlorophenylisocoumarins were synthesized by condensation of homophthalic acid with dichlorobenzoyl chlorides. The alkaline hydrolysis of these isocoumarins afforded keto acids. Racemic 3-(Dichlorophenyl)-3,4-dihydroisocoumarins were obtained by reduction of keto acids to racemic hydroxy acids, followed by cyclodehydration using acetic anhydride. The herbicidal, fungicidal and insecticidal activities of the synthesized compounds have been evaluated. Some of the synthesized compounds show excellent herbicidal and fungicidal activities but none of the synthesized compounds presented any insecticidal effects on the test insects. The findings of this study suggest that isocoumarins and related compounds may serve as lead compounds towards the design of bioactive herbicides and fungicides. (author)

Development of a novel multiplex DNA microarray for Fusarium graminearum and analysis of azole fungicide responses

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Deising Holger B

2011-01-01

Full Text Available Abstract Background The toxigenic fungal plant pathogen Fusarium graminearum compromises wheat production worldwide. Azole fungicides play a prominent role in controlling this pathogen. Sequencing of its genome stimulated the development of high-throughput technologies to study mechanisms of coping with fungicide stress and adaptation to fungicides at a previously unprecedented precision. DNA-microarrays have been used to analyze genome-wide gene expression patterns and uncovered complex transcriptional responses. A recently developed one-color multiplex array format allowed flexible, effective, and parallel examinations of eight RNA samples. Results We took advantage of the 8 × 15 k Agilent format to design, evaluate, and apply a novel microarray covering the whole F. graminearum genome to analyze transcriptional responses to azole fungicide treatment. Comparative statistical analysis of expression profiles uncovered 1058 genes that were significantly differentially expressed after azole-treatment. Quantitative RT-PCR analysis for 31 selected genes indicated high conformity to results from the microarray hybridization. Among the 596 genes with significantly increased transcript levels, analyses using GeneOntology and FunCat annotations detected the ergosterol-biosynthesis pathway genes as the category most significantly responding, confirming the mode-of-action of azole fungicides. Cyp51A, which is one of the three F. graminearum paralogs of Cyp51 encoding the target of azoles, was the most consistently differentially expressed gene of the entire study. A molecular phylogeny analyzing the relationships of the three CYP51 proteins in the context of 38 fungal genomes belonging to the Pezizomycotina indicated that CYP51C (FGSG_11024 groups with a new clade of CYP51 proteins. The transcriptional profiles for genes encoding ABC transporters and transcription factors suggested several involved in mechanisms alleviating the impact of the fungicide

Inhibitory Effects of Respiration Inhibitors on Aflatoxin Production

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Shohei Sakuda

2014-03-01

Full Text Available Aflatoxin production inhibitors, which do not inhibit the growth of aflatoxigenic fungi, may be used to control aflatoxin without incurring a rapid spread of resistant strains. A respiration inhibitor that inhibits aflatoxin production was identified during a screening process for natural, aflatoxin-production inhibitors. This prompted us to evaluate respiration inhibitors as potential aflatoxin control agents. The inhibitory activities of four natural inhibitors, seven synthetic miticides, and nine synthetic fungicides were evaluated on aflatoxin production in Aspergillus parasiticus. All of the natural inhibitors (rotenone, siccanin, aptenin A5, and antimycin A inhibited fungal aflatoxin production with IC50 values around 10 µM. Among the synthetic miticides, pyridaben, fluacrypyrim, and tolfenpyrad exhibited strong inhibitory activities with IC50 values less than 0.2 µM, whereas cyflumetofen did not show significant inhibitory activity. Of the synthetic fungicides, boscalid, pyribencarb, azoxystrobin, pyraclostrobin, and kresoxim-methyl demonstrated strong inhibitory activities, with IC50 values less than 0.5 µM. Fungal growth was not significantly affected by any of the inhibitors tested at concentrations used. There was no correlation observed between the targets of respiration inhibitors (complexes I, II, and III and their IC50 values for aflatoxin-production inhibitory activity. This study suggests that respiration inhibitors, including commonly used pesticides, are useful for aflatoxin control.

Inhibitory Effects of Respiration Inhibitors on Aflatoxin Production

Science.gov (United States)

Sakuda, Shohei; Prabowo, Diyan Febri; Takagi, Keiko; Shiomi, Kazuro; Mori, Mihoko; Ōmura, Satoshi; Nagasawa, Hiromichi

2014-01-01

Aflatoxin production inhibitors, which do not inhibit the growth of aflatoxigenic fungi, may be used to control aflatoxin without incurring a rapid spread of resistant strains. A respiration inhibitor that inhibits aflatoxin production was identified during a screening process for natural, aflatoxin-production inhibitors. This prompted us to evaluate respiration inhibitors as potential aflatoxin control agents. The inhibitory activities of four natural inhibitors, seven synthetic miticides, and nine synthetic fungicides were evaluated on aflatoxin production in Aspergillus parasiticus. All of the natural inhibitors (rotenone, siccanin, aptenin A5, and antimycin A) inhibited fungal aflatoxin production with IC50 values around 10 µM. Among the synthetic miticides, pyridaben, fluacrypyrim, and tolfenpyrad exhibited strong inhibitory activities with IC50 values less than 0.2 µM, whereas cyflumetofen did not show significant inhibitory activity. Of the synthetic fungicides, boscalid, pyribencarb, azoxystrobin, pyraclostrobin, and kresoxim-methyl demonstrated strong inhibitory activities, with IC50 values less than 0.5 µM. Fungal growth was not significantly affected by any of the inhibitors tested at concentrations used. There was no correlation observed between the targets of respiration inhibitors (complexes I, II, and III) and their IC50 values for aflatoxin-production inhibitory activity. This study suggests that respiration inhibitors, including commonly used pesticides, are useful for aflatoxin control. PMID:24674936

In vitro sensitivity reduction of Fusarium graminearum to DMI and QoI fungicides

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Aveline Avozani

2014-12-01

Full Text Available In Brazil, Fusarium head blight (FHB affecting wheat can cause up to 39.8% damage. Resistant cultivars are not available yet; thus, short-term disease control relies on the use of fungicides. The first step to improve control is to monitor fungal populations that are sensitivity to chemicals in order to achieve efficient FHB management. In vitro experiments were conducted to evaluate the inhibitory concentration (IC50 of fungicides for both mycelial growth and conidial germination of ten Fusarium graminearum isolates. The following demethylation inhibitor (DMI fungicides were tested: metconazole, prothioconazole and tebuconazole. In addition, pyraclostrobin and trifloxystrobin were included, representing QoI fungicides, as well as three co-formulations containing metconazole + pyraclostrobin, prothioconazole + trifloxystrobin, and tebuconazole + trifloxystrobin. For mycelial growth, the overall mean IC50 of isolates was: metconazole 0.07, prothioconazole 0.1, and tebuconazole 0.19 mg/L. For the co-formulations, it was: prothioconazole + trifloxystrobin 0.08, tebuconazole + trifloxystrobin 0.12, and metconazole + pyraclostrobin 0.14 mg/L. Regarding spore germination inhibition, IC50 for prothioconazole + trifloxystrobin was 0.06, for tebuconazole + trifloxystrobin, 0.12 mg/L, for QoI alone pyraclostrobin, was 0.09, and for trifloxystrobin, 0.28 mg/L. There was a sensitivity shift among isolates and the highest fungitoxicity to F. graminearum was confirmed for prothioconazole, metconazole and tebuconazole .

Proteomic profile of the plant-pathogenic oomycete Phytophthora capsici in response to the fungicide pyrimorph.

Science.gov (United States)

Pang, Zhili; Chen, Lei; Miao, Jianqiang; Wang, Zhiwen; Bulone, Vincent; Liu, Xili

2015-09-01

Pyrimorph is a novel fungicide from the carboxylic acid amide (CAA) family used to control plant-pathogenic oomycetes such as Phytophthora capsici. The proteomic response of P. capsici to pyrimorph was investigated using the iTRAQ technology to determine the target site of the fungicide and potential biomarker candidates of drug efficacy. A total of 1336 unique proteins were identified from the mycelium of wild-type P. capsici isolate (Hd3) and two pyrimorph-resistant mutants (R3-1 and R3-2) grown in the presence or absence of pyrimorph. Comparative analysis revealed that the three P. capsici isolates Hd3, R3-1, and R3-2 produced 163, 77, and 13 unique proteins, respectively, which exhibited altered levels of abundance in response to the pyrimorph treatment. Further investigations, using Cluster of Orthologous Groups of Proteins (COG) analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis identified 35 proteins related to the mode of action of pyrimorph against P. capsici and 62 proteins involved in the stress response of P. capsici to pyrimorph. Many of the proteins with altered expression were associated with glucose and energy metabolism. Biochemical analysis using d-[U-(14) C]glucose verified the proteomics data, suggesting that the major mode of action of pyrimorph in P. capsici is the inhibition of cell wall biosynthesis. These results also illustrate that proteomics approaches are useful tools for determining the pathways targeted by novel fungicides as well as for evaluating the tolerance of plant pathogens to environmental challenges, such as the presence of fungicides. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Potential mechanisms underlying response to effects of the fungicide pyrimethanil from gene expression profiling in Saccharomyces cerevisiae.

Science.gov (United States)

Gil, Fátima N; Becker, Jörg D; Viegas, Cristina A

2014-06-11

Pyrimethanil is a fungicide mostly applied in vineyards. When misused, residue levels detected in grape must or in the environment may be of concern. The present work aimed to analyze mechanisms underlying response to deleterious effects of pyrimethanil in the eukaryotic model Saccharomyces cerevisiae. Pyrimethanil concentration-dependent effects at phenotypic (inhibition of growth) and transcriptomic levels were examined. For transcriptional profiling, analysis focused on two sublethal exposure conditions that inhibited yeast growth by 20% or 50% compared with control cells not exposed to the fungicide. Gene expression modifications increased with the magnitude of growth inhibition, in numbers and fold-change of differentially expressed genes and in diversity of over-represented functional categories. These included mostly biosynthesis of arginine and sulfur amino acids metabolism, as well as energy conservation, antioxidant response, and multidrug transport. Several pyrimethanil-responsive genes encoded proteins sharing significant homology with proteins from phytopathogenic fungi and ecologically relevant higher eukaryotes.

Is Low Efficacy of Fungicides always a Consequence of Fungicide Resistance Development in Pathogen Populations?

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Brankica Tanović

2011-01-01

Full Text Available Efficacy of four fungicides with different modes of action (vinclozolin, pyrimethanil, benomyland fenhexamid in control of B. cinerea in raspberry, was investigated in the paper.The trials were conducted at two localities in commercial raspberry plantations. In the caseof unsatisfactory fungicide efficacy, qualitative and/or quantitative test of the susceptibilityof the isolates to particular fungicide was performed, to determine whether the low efficacyis a consequence of resistance development in the pathogen population. At both localities,pyrimethanil and fenhexamid demonstrated the highest efficacy (73.2-89.6%, whilethe efficacy of vinclozolin was statistically significantly lower (48.7-63.4% at both localities.However, qualitative and quantitative test of susceptibility to vinclozolin showed that all theisolates were susceptible to vinclozolin and that the reason for unsatisfactory efficacy shouldbe primarily sought in inadequate fungicide application

A Major Facilitator Superfamily Transporter-Mediated Resistance to Oxidative Stress and Fungicides Requires Yap1, Skn7, and MAP Kinases in the Citrus Fungal Pathogen Alternaria alternata.

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Li-Hung Chen

Full Text Available Major Facilitator Superfamily (MFS transporters play an important role in multidrug resistance in fungi. We report an AaMFS19 gene encoding a MFS transporter required for cellular resistance to oxidative stress and fungicides in the phytopathogenic fungus Alternaria alternata. AaMFS19, containing 12 transmembrane domains, displays activity toward a broad range of substrates. Fungal mutants lacking AaMFS19 display profound hypersensitivities to cumyl hydroperoxide, potassium superoxide, many singlet oxygen-generating compounds (eosin Y, rose Bengal, hematoporphyrin, methylene blue, and cercosporin, and the cell wall biosynthesis inhibitor, Congo red. AaMFS19 mutants also increase sensitivity to copper ions, clotrimazole, fludioxonil, and kocide fungicides, 2-chloro-5-hydroxypyridine (CHP, and 2,3,5-triiodobenzoic acid (TIBA. AaMFS19 mutants induce smaller necrotic lesions on leaves of a susceptible citrus cultivar. All observed phenotypes in the mutant are restored by introducing and expressing a wild-type copy of AaMFS19. The wild-type strain of A. alternata treated with either CHP or TIBA reduces radial growth and formation and germination of conidia, increases hyphal branching, and results in decreased expression of the AaMFS19 gene. The expression of AaMFS19 is regulated by the Yap1 transcription activator, the Hog1 and Fus3 mitogen-activated protein (MAP kinases, the 'two component' histidine kinase, and the Skn7 response regulator. Our results demonstrate that A. alternata confers resistance to different chemicals via a membrane-bound MFS transporter.

Ethylglyoxal bis(guanylhydrazone) as an inhibitor of polyamine biosynthesis in L1210 leukemia cells.

Science.gov (United States)

Seppänen, P; Ruohola, H; Jänne, J

1984-04-16

Ethylglyoxal bis(guanylhydrazone), a close derivative of the known anti-cancer drug methylglyoxal bis(guanylhydrazone), is also a powerful inhibitor of S-adenosylmethionine decarboxylase (EC 4.1.1.50), the enzyme needed for the synthesis of spermidine and spermine. There were, however, marked differences between the ethyl and methyl derivatives of glyoxal bis(guanylhydrazone) when tested in cultured L1210 cells. The cellular accumulation of ethylglyoxal bis(guanylhydrazone) represented only a fraction (20-25%) of that of the methyl derivative. Moreover, polyamine depletion, which is known to strikingly stimulate the uptake of methylglyoxal bis(guanylhydrazone), decreased, if anything, the uptake of ethylglyoxal bis(guanylhydrazone) by L1210 cells. The compound produced spermidine and spermine depletion fully comparable to that achieved with methylglyoxal bis(guanylhydrazone) at micromolar concentrations. Ethylglyoxal bis(guanylhydrazone) was growth-inhibitory to L1210 cells and produced an additive antiproliferative action when used together with 2-difluoromethylornithine. Ethylglyoxal bis(guanylhydrazone) was distinctly less effective than methylglyoxal bis(guanylhydrazone) in releasing bound polyamines from isolated cell organelles in vitro. Ethylglyoxal bis(guanylhydrazone) was also devoid of the early and profound mitochondrial toxicity typical to methylglyoxal bis(guanylhydrazone). These findings may indicate that this compound is a more specific inhibitor of polyamine biosynthesis with less intracellular polyamine 'receptor-site' activity than methylglyoxal bis(guanylhydrazone).

The benefits of combining elemental sulfur with a DMI fungicide to control Monilinia fructicola isolates resistant to propiconazole.

Science.gov (United States)

Holb, Imre J; Schnabel, Guido

2008-02-01

Management of demethylation inhibitor (DMI) fungicide resistance in Monilinia fructicola (G. Winter) Honey is a priority in peach orchards of the southeastern United States, but DMI fungicides are still an important component of antiresistance strategies in view of the few effective alternatives. The goal of this study was to investigate potential benefits of a sulfur/propiconazole mixture for the control of propiconazole-resistant isolates. The mixture provided the best control for propiconazole-resistant isolates, regardless of protective or curative application timings, or the presence or absence of fruit injury. Propiconazole-resistant isolates developed disease on detached fruit after protective or curative applications of propiconazole or its mixture with sulfur, but protective applications of the mixture significantly reduced (P = 0.05) disease symptoms compared with the individual compounds. Additive to slightly synergistic effects were observed for the mixture in protective treatments of peaches inoculated with propiconazole-resistant isolates. The results suggest that the addition of elemental sulfur to a DMI fungicide is likely to be a relatively inexpensive means to improve brown rot control in peach production areas where reduced sensitivity to DMI fungicides is suspected but has not led to noticeable control failure.

Enhancement of misonidazole radiosensitization by an inhibitor of glutathione biosynthesis

International Nuclear Information System (INIS)

Hodgkiss, R.J.; Middleton, R.W.

1983-01-01

A well known inhibitor of glutathione biosynthesis, buthione sulphoximine (S-n-butyl homocysteine sulphoximine, BSO) depletes non-protein sulphydryls (NPSH) in Chinese hamster cells in vitro, resulting in a marked increase in the radiosensitization efficiency of misonidazole. V79 379A Chinese hamster cells were maintained in suspension cultures and irradiated in monolayers using 250 kVp X-rays at a dose rate of 3.93 Gy/min. Radiosensitization by misonidazole alone gave results within 0.1 sensitizer enhancement ratio (s.e.r.) of the curve reported by Watts et al. (1980). GSH (2 mmol dm - 3 ) added to the extracellular medium resulted in a marked decrease in the radiosensitization efficiency of misonidazole, eliminating the effect at 0.1 mmol dm - 3 misonidazole (s.e.r. = 1.0 relative to nitrogen control). A marked enhancement of the radiosensitization by misonidazole was observed when the cells had been incubated with BSO (0.1 mmol dm - 3 ). BSO alone at this concentration gave s.e.r. = 1.17; misonidazole alone (0.1 mmol dm - 3 ) gave s.e.r. = 1.18 and misonidazole with BSO (both 0.1. mmol dm - 3 ) gave s.e.r. = 1.9. The BSO treatment gave little effect in aerated cells. The concentration of BSO needed to produce these effects in vitro is ca. 40-fold lower than doses tolerated by mice in repeated administrations. (U.K.)

Propiconazole-enhanced hepatic cell proliferation is associated with dysregulation of the cholesterol biosynthesis pathway leading to activation of Erk1/2 through Ras farnesylation

Energy Technology Data Exchange (ETDEWEB)

Murphy, Lynea A.; Moore, Tanya; Nesnow, Stephen, E-mail: nesnow.stephen@epa.gov

2012-04-15

Propiconazole is a mouse hepatotumorigenic fungicide designed to inhibit CYP51, a key enzyme in the biosynthesis of ergosterol in fungi and is widely used in agriculture to prevent fungal growth. Metabolomic studies in mice revealed that propiconazole increased levels of hepatic cholesterol metabolites and bile acids, and transcriptomic studies revealed that genes within the cholesterol biosynthesis, cholesterol metabolism and bile acid biosyntheses pathways were up-regulated. Hepatic cell proliferation was also increased by propiconazole. AML12 immortalized hepatocytes were used to study propiconazole's effects on cell proliferation focusing on the dysregulation of cholesterol biosynthesis and resulting effects on Ras farnesylation and Erk1/2 activation as a primary pathway. Mevalonate, a key intermediate in the cholesterol biosynthesis pathway, increases cell proliferation in several cancer cell lines and tumors in vivo and serves as the precursor for isoprenoids (e.g. farnesyl pyrophosphate) which are crucial in the farnesylation of the Ras protein by farnesyl transferase. Farnesylation targets Ras to the cell membrane where it is involved in signal transduction, including the mitogen-activated protein kinase (MAPK) pathway. In our studies, mevalonic acid lactone (MVAL), a source of mevalonic acid, increased cell proliferation in AML12 cells which was reduced by farnesyl transferase inhibitors (L-744,832 or manumycin) or simvastatin, an HMG-CoA reductase inhibitor, indicating that this cell system responded to alterations in the cholesterol biosynthesis pathway. Cell proliferation in AML12 cells was increased by propiconazole which was reversed by co-incubation with L-744,832 or simvastatin. Increasing concentrations of exogenous cholesterol muted the proliferative effects of propiconazole and the inhibitory effects of L-733,832, results ascribed to reduced stimulation of the endogenous cholesterol biosynthesis pathway. Western blot analysis of subcellular

The fungicide triadimefon affects beer flavor and composition by influencing Saccharomyces cerevisiae metabolism

Science.gov (United States)

Kong, Zhiqiang; Li, Minmin; An, Jingjing; Chen, Jieying; Bao, Yuming; Francis, Frédéric; Dai, Xiaofeng

2016-09-01

Despite the fact that beer is produced on a large scale, the effects of pesticide residues on beer have been rarely investigated. In this study, we used micro-brewing settings to determine the effect of triadimefon on the growth of Saccharomyces cerevisiae and beer flavor. The yeast growth in medium was significantly inhibited (45%) at concentrations higher than 5 mg L-1, reaching 80% and 100% inhibition at 10 mg L-1 and 50 mg L-1, respectively. There were significant differences in sensory quality between beer samples fermented with and without triadimefon based on data obtained with an electronic tongue and nose. Such an effect was most likely underlain by changes in yeast fermentation activity, including decreased utilization of maltotriose and most amino acids, reduced production of isobutyl and isoamyl alcohols, and increased ethyl acetate content in the fungicide treated samples. Furthermore, yeast metabolic profiling by phenotype microarray and UPLC/TOF-MS showed that triadimefon caused significant changes in the metabolism of glutathione, phenylalanine and sphingolipids, and in sterol biosynthesis. Thus, triadimefon negatively affects beer sensory qualities by influencing the metabolic activity of S. cerevisiae during fermentation, emphasizing the necessity of stricter control over fungicide residues in brewing by the food industry.

Impact of fungicides on weed growth

Directory of Open Access Journals (Sweden)

Nordmeyer, Henning

2014-02-01

Full Text Available The study has shown that fungicides influence the growth of weeds. The competition against crops will be substantially reduced. Bioassays in a climate chamber variation in temperature as well as different lightning phases and microplot trials under semi field levels were carried out to investigate the influence of fungicides on weed growth. Selected weed species (Alopecurus myosuroides, Viola arvensis, Galium aparine, Stellaria media, Lamium purpureum have been examined with different dose rates of fungicides (Adexar, Bravo 500, Diamant, Crupozin flüssig. Weed species showed a different sensitivity. There were leaf discoloration, contractions and growth inhibition. In some cases using common practise dose rates of fungicides more than 70% growth inhibition could be estimated 14 days after application in comparison to the untreated control. Effects were much stronger in bioassays than in semi field trials.

Stemphylium Leaf Blight of Garlic (Allium sativum in Spain: Taxonomy and In Vitro Fungicide Response

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Laura Gálvez

2016-10-01

Full Text Available The most serious aerial disease of garlic is leaf blight caused by Stemphylium spp. Geographical variation in the causal agent of this disease is indicated. Stemphylium vesicarium has been reported in Spain, whereas S. solani is the most prevalent species recorded in China. In this study, Stemphylium isolates were obtained from symptomatic garlic plants sampled from the main Spanish production areas. Sequence data for the ITS1–5.8S–ITS2 region enabled assignation of the isolates to the Pleospora herbarum complex and clearly distinguished the isolates from S. solani. Conidial morphology of the isolates corresponded to that of S. vesicarium and clearly discriminated them from S. alfalfae and S. herbarum on the basis of the size and septation pattern of mature conidia. Conidial morphology as well as conidial length, width and length:width ratio also allowed the Spanish isolates to be distinguished from S. botryosum and S. herbarum. Control of leaf blight of garlic is not well established. Few studies are available regarding the effectiveness of chemical treatments to reduce Stemphylium spp. incidence on garlic. The effectiveness of nine fungicides of different chemical groups to reduce Stemphylium mycelial growth in vitro was tested. Boscalid + pyraclostrobin (group name, succinate dehydrogenase inhibitors + quinone outside inhibitors, iprodione (dicar-boximide, and prochloraz (demethylation inhibitors were highly effective at reducing mycelial growth in S. vesicarium with EC₅₀ values less than 5 ppm. In general, the effectiveness of the fungicide was enhanced with increasing dosage.

Stemphylium Leaf Blight of Garlic (Allium sativum ) in Spain: Taxonomy and In Vitro Fungicide Response

Science.gov (United States)

Gálvez, Laura; Gil-Serna, Jéssica; García, Marta; Iglesias, Concepción; Palmero, Daniel

2016-01-01

The most serious aerial disease of garlic is leaf blight caused by Stemphylium spp. Geographical variation in the causal agent of this disease is indicated. Stemphylium vesicarium has been reported in Spain, whereas S. solani is the most prevalent species recorded in China. In this study, Stemphylium isolates were obtained from symptomatic garlic plants sampled from the main Spanish production areas. Sequence data for the ITS1–5.8S–ITS2 region enabled assignation of the isolates to the Pleospora herbarum complex and clearly distinguished the isolates from S. solani. Conidial morphology of the isolates corresponded to that of S. vesicarium and clearly discriminated them from S. alfalfae and S. herbarum on the basis of the size and septation pattern of mature conidia. Conidial morphology as well as conidial length, width and length:width ratio also allowed the Spanish isolates to be distinguished from S. botryosum and S. herbarum. Control of leaf blight of garlic is not well established. Few studies are available regarding the effectiveness of chemical treatments to reduce Stemphylium spp. incidence on garlic. The effectiveness of nine fungicides of different chemical groups to reduce Stemphylium mycelial growth in vitro was tested. Boscalid + pyraclostrobin (group name, succinate dehydrogenase inhibitors + quinone outside inhibitors), iprodione (dicar-boximide), and prochloraz (demethylation inhibitors) were highly effective at reducing mycelial growth in S. vesicarium with EC50 values less than 5 ppm. In general, the effectiveness of the fungicide was enhanced with increasing dosage. PMID:27721688

Stable Analogues of OSB-AMP: Potent Inhibitors of MenE the o-succinylbenzoate-CoA Synthetase from Bacterial Menaquinone Biosynthesis

Energy Technology Data Exchange (ETDEWEB)

Lu X.; Swaminathan S.; Zhou R.; Sharma I.; Li X.; Kumar G.; Tonge P. J.; Tan D. S.

2012-01-02

MenE, the o-succinylbenzoate (OSB)-CoA synthetase from bacterial menaquinone biosynthesis, is a promising new antibacterial target. Sulfonyladenosine analogues of the cognate reaction intermediate, OSB-AMP, have been developed as inhibitors of the MenE enzymes from Mycobacterium tuberculosis (mtMenE), Staphylococcus aureus (saMenE) and Escherichia coli (ecMenE). Both a free carboxylate and a ketone moiety on the OSB side chain are required for potent inhibitory activity. OSB-AMS (4) is a competitive inhibitor of mtMenE with respect to ATP (K{sub i} = 5.4 {+-} 0.1 nM) and a noncompetitive inhibitor with respect to OSB (K{sub i} = 11.2 {+-} 0.9 nM). These data are consistent with a Bi Uni Uni Bi Ping-Pong kinetic mechanism for these enzymes. In addition, OSB-AMS inhibits saMenE with K{sub i}{sup app} = 22 {+-} 8 nM and ecMenE with K{sub i}{sup OSB} = 128 {+-} 5 nM. Putative active-site residues, Arg222, which may interact with the OSB aromatic carboxylate, and Ser302, which may bind the OSB ketone oxygen, have been identified through computational docking of OSB-AMP with the unliganded crystal structure of saMenE. A pH-dependent interconversion of the free keto acid and lactol forms of the inhibitors is also described, along with implications for inhibitor design.

Biological characterization of fenpicoxamid, a new fungicide with utility in cereals and other crops.

Science.gov (United States)

Owen, W John; Yao, Chenglin; Myung, Kyung; Kemmitt, Greg; Leader, Andrew; Meyer, Kevin G; Bowling, Andrew J; Slanec, Thomas; Kramer, Vincent J

2017-10-01

The development of novel highly efficacious fungicides that lack cross-resistance is extremely desirable. Fenpicoxamid (Inatreq™ active) possesses these characteristics and is a member of a novel picolinamide class of fungicides derived from the antifungal natural product UK-2A. Fenpicoxamid strongly inhibited in vitro growth of several ascomycete fungi, including Zymoseptoria tritici (EC 50 , 0.051 mg L -1 ). Fenpicoxamid is converted by Z. tritici to UK-2A, a 15-fold stronger inhibitor of Z. tritici growth (EC 50 , 0.0033 mg L -1 ). Strong fungicidal activity of fenpicoxamid against driver cereal diseases was confirmed in greenhouse tests, where activity on Z. tritici and Puccinia triticina matched that of fluxapyroxad. Due to its novel target site (Q i site of the respiratory cyt bc1 complex) for the cereals market, fenpicoxamid is not cross-resistant to Z. tritici isolates resistant to strobilurin and/or azole fungicides. Across multiple European field trials Z. tritici was strongly controlled (mean, 82%) by 100 g as ha -1 applications of fenpicoxamid, which demonstrated excellent residual activity. The novel chemistry and biochemical target site of fenpicoxamid as well as its lack of cross-resistance and strong efficacy against Z. tritici and other pathogens highlight the importance of fenpicoxamid as a new tool for controlling plant pathogenic fungi. © 2017 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry. © 2017 The Authors. Pest Management Science published by John Wiley & Sons Ltd on behalf of Society of Chemical Industry.

Phage display-derived inhibitor of the essential cell wall biosynthesis enzyme MurF

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Blewett Ann

2008-12-01

Full Text Available Abstract Background To develop antibacterial agents having novel modes of action against bacterial cell wall biosynthesis, we targeted the essential MurF enzyme of the antibiotic resistant pathogen Pseudomonas aeruginosa. MurF catalyzes the formation of a peptide bond between D-Alanyl-D-Alanine (D-Ala-D-Ala and the cell wall precursor uridine 5'-diphosphoryl N-acetylmuramoyl-L-alanyl-D-glutamyl-meso-diaminopimelic acid (UDP-MurNAc-Ala-Glu-meso-A2pm with the concomitant hydrolysis of ATP to ADP and inorganic phosphate, yielding UDP-N-acetylmuramyl-pentapeptide. As MurF acts on a dipeptide, we exploited a phage display approach to identify peptide ligands having high binding affinities for the enzyme. Results Screening of a phage display 12-mer library using purified P. aeruginosa MurF yielded to the identification of the MurFp1 peptide. The MurF substrate UDP-MurNAc-Ala-Glumeso-A2pm was synthesized and used to develop a sensitive spectrophotometric assay to quantify MurF kinetics and inhibition. MurFp1 acted as a weak, time-dependent inhibitor of MurF activity but was a potent inhibitor when MurF was pre-incubated with UDP-MurNAc-Ala-Glu-meso-A2pm or ATP. In contrast, adding the substrate D-Ala-D-Ala during the pre-incubation nullified the inhibition. The IC50 value of MurFp1 was evaluated at 250 μM, and the Ki was established at 420 μM with respect to the mixed type of inhibition against D-Ala-D-Ala. Conclusion MurFp1 exerts its inhibitory action by interfering with the utilization of D-Ala-D-Ala by the MurF amide ligase enzyme. We propose that MurFp1 exploits UDP-MurNAc-Ala-Glu-meso-A2pm-induced structural changes for better interaction with the enzyme. We present the first peptide inhibitor of MurF, an enzyme that should be exploited as a target for antimicrobial drug development.

Stable analogues of OSB-AMP: potent inhibitors of MenE, the o-succinylbenzoate-CoA synthetase from bacterial menaquinone biosynthesis.

Science.gov (United States)

Lu, Xuequan; Zhou, Rong; Sharma, Indrajeet; Li, Xiaokai; Kumar, Gyanendra; Swaminathan, Subramanyam; Tonge, Peter J; Tan, Derek S

2012-01-02

MenE, the o-succinylbenzoate (OSB)-CoA synthetase from bacterial menaquinone biosynthesis, is a promising new antibacterial target. Sulfonyladenosine analogues of the cognate reaction intermediate, OSB-AMP, have been developed as inhibitors of the MenE enzymes from Mycobacterium tuberculosis (mtMenE), Staphylococcus aureus (saMenE) and Escherichia coli (ecMenE). Both a free carboxylate and a ketone moiety on the OSB side chain are required for potent inhibitory activity. OSB-AMS (4) is a competitive inhibitor of mtMenE with respect to ATP (K(i) =5.4±0.1 nM) and a noncompetitive inhibitor with respect to OSB (K(i) =11.2±0.9 nM). These data are consistent with a Bi Uni Uni Bi Ping-Pong kinetic mechanism for these enzymes. In addition, OSB-AMS inhibits saMenE with K(i)(app) =22±8 nM and ecMenE with K(i)(OSB) =128±5 nM. Putative active-site residues, Arg222, which may interact with the OSB aromatic carboxylate, and Ser302, which may bind the OSB ketone oxygen, have been identified through computational docking of OSB-AMP with the unliganded crystal structure of saMenE. A pH-dependent interconversion of the free keto acid and lactol forms of the inhibitors is also described, along with implications for inhibitor design. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Structure-activity relationship of prenyl-substituted polyphenols from Artocarpus heterophyllus as inhibitors of melanin biosynthesis in cultured melanoma cells.

Science.gov (United States)

Arung, Enos Tangke; Shimizu, Kuniyoshi; Kondo, Ryuichiro

2007-09-01

A series of prenylated, flavone-based polyphenols, compounds 1-8, were isolated from the wood of Artocarpus heterophyllus. These compounds, which have previously been shown not to inhibit tyrosinase activity, were found to be active inhibitors of the in vivo melanin biosynthesis in B16 melanoma cells, with little or no cytotoxicity. To clarify the structural requirement for inhibition, some structure-activity relationships were studied, in comparison with related compounds lacking prenyl side chains. Our experiments indicate that both prenyl and OH groups, as well as the type of substitution pattern, are crucial for the inhibition of melanin production in B16 melanoma cells.

Annual Fungicide Loadings

Data.gov (United States)

U.S. Environmental Protection Agency — Pesticides, Herbicides, Fungicides...etc, are used for a variety of purposes, including control of household, lawn, and garden pests; for control of mosquitoes and...

Effect of fungicides on Wyoming big sagebrush seed germination

Science.gov (United States)

Robert D. Cox; Lance H. Kosberg; Nancy L. Shaw; Stuart P. Hardegree

2011-01-01

Germination tests of Wyoming big sagebrush (Artemisia tridentata Nutt. ssp. wyomingensis Beetle & Young [Asteraceae]) seeds often exhibit fungal contamination, but the use of fungicides should be avoided because fungicides may artificially inhibit germination. We tested the effect of seed-applied fungicides on germination of Wyoming big sagebrush at 2 different...

Triazole Fungicides Sensitivity of Sclerotinia homoeocarpa in Korean Golf Courses

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Ji Won Lee

2017-12-01

Full Text Available Chemical management of dollar spot in turf may lead to the development of Sclerotinia homoeocarpa populations with reduced fungicide sensitivity. The objective of this study was to investigate resistance of S. homoeocarpa isolates to triazole fungicides and to test cross-resistance among three triazole fungicides. A total of 66 isolates of S. homoeocarpa were collected from 15 golf courses across Korea, and tested via in vitro sensitivity assay against hexaconazole, propiconazole and tebuconazole. EC₅₀ values of the isolates to these fungicides were distributed in the range of 0.001–1.1 a. i. μg ml−1. Based on the EC₅₀ values, twelve representative strains were selected as sensitive isolates including control and insensitive isolates with respect to each fungicide. At a concentration of 0.1 a. i. μg ml−1 for all fungicides, the selected strains were distinguished as sensitive or resistant isolates with the mycelial growth inhibition rate of 50% as the criterion. The EC₅₀ values of resistant strains exposed to hexaconazole, propiconazole and tebuconazole were 20–50 times, 50–70 times, and 77 times greater, respectively, than that of the control strains. Two isolates of S. homoeocarpa S0–41 and Sh14-2-1 showed sensitivity toward all the fungicides used, while two other isolates Sh7-5-1 and Sh2-1-1 showed resistance to all fungicides. Each isolate showed similar resistance to the three types of triazole fungicides, whereby cross-resistance of isolates was confirmed in the present study; all three triazole fungicide combinations displayed significant correlation coefficients equivalent to or greater than 0.8.

The usefulness of fungicide mixtures and alternation for delaying the selection for resistance in populations of Mycosphaerella graminicola on winter wheat: a modeling analysis.

Science.gov (United States)

Hobbelen, P H F; Paveley, N D; Oliver, R P; van den Bosch, F

2013-07-01

A fungicide resistance model (reported and tested previously) was amended to describe the development of resistance in Mycosphaerella graminicola populations in winter wheat (Triticum aestivum) crops in two sets of fields, connected by spore dispersal. The model was used to evaluate the usefulness of concurrent, alternating, or mixture use of two high-resistance-risk fungicides as resistance management strategies. We determined the effect on the usefulness of each strategy of (i) fitness costs of resistance, (ii) partial resistance to fungicides, (iii) differences in the dose-response curves and decay rates between fungicides, and (iv) different frequencies of the double-resistant strain at the start of a treatment strategy. Parameter values for the quinine outside inhibitor pyraclostrobin were used to represent two fungicides with differing modes of action. The effectiveness of each strategy was quantified as the maximum number of growing seasons that disease was effectively controlled in both sets of fields. For all scenarios, the maximum effective lives achieved by the use of the strategies were in the order mixtures ≥ alternation ≥ concurrent use. Mixtures were of particular benefit where the pathogen strain resistant to both modes of action incurred a fitness penalty or was present at a low initial frequency.

Recent Trends in Studies on Botanical Fungicides in Agriculture

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Mi-Young Yoon

2013-03-01

Full Text Available Plants are attacked by various phytopathogenic fungi. For many years, synthetic fungicides have been used to control plant diseases. Although synthetic fungicides are highly effective, their repeated use has led to problems such as environmental pollution, development of resistance, and residual toxicity. This has prompted intensive research on the development of biopesticides, including botanical fungicides. To date, relatively few botanical fungicides have been registered and commercialized. However, many scientists have reported isolation and characterization of a variety of antifungal plant derivatives. Here, we present a survey of a wide range of reported plant-derived antifungal metabolites.

Impact of DMI and SDHI fungicides on disease control and CYP51 mutations in populations of Zymoseptoria tritici from Northern Europe

DEFF Research Database (Denmark)

Wieczorek, Thies Marten; Berg, Gunilla; Semaskiene, Roma

2015-01-01

Zymoseptoria tritici is a dominant pathogen in wheat causing Septoria leaf blotch (SLB), and sterol 14α-demethylation inhibitors fungicides (DMI) are commonly used for control in Northern Europe. In 14 winter wheat trials carried out in Denmark, Lithuania, and Sweden in the years 2011 to 2013, fu...

Synthesis and Fungicidal Activity of β-Carboline Alkaloids and Their Derivatives

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Zhibin Li

2015-07-01

Full Text Available A series of β-Carboline derivatives were designed, synthesized, and evaluated for their fungicidal activities in this study. Several derivatives electively exhibited fungicidal activities against some fungi. Especially, compound F5 exhibited higher fungicidal activity against Rhizoctonia solani (53.35% than commercial antiviral agent validamycin (36.4%; compound F16 exhibited high fungicidal activity against Oospora citriaurantii ex Persoon (43.28%. Some of the alkaloids and their derivatives (compounds F4 and F25 exhibited broad-spectrum fungicidal activity. Specifically, compound F4 exhibited excellent high broad-spectrum fungicidal activity in vitro, and the curative and protection activities against P. litchi in vivo reached 92.59% and 59.26%, respectively. The new derivative, F4, with optimized physicochemical properties, obviously exhibited higher activities both in vitro and in vivo; therefore, F4 may be used as a new lead structure for the development of fungicidal drugs.

Effect of gamma radiation on ''in vitro''' efficiency of fungicides

International Nuclear Information System (INIS)

Menten, J.O.M.; Oliveira, G.C.X.

1984-01-01

The activity of 60 Co gamma radiation on eight fungicides used in post-harvesting treatment of agricultural products, was studied. Rhizoctonia solani was used in biological test as indicator-fungus. The fungicides were submitted to gamma radiation doses of O (control), 1, 10, 100, 1000 and 10.000 kR, samples of the fungicides were added to the PSA culture media to obtain 0, 1, 10 and 100 ppm concentrations of the active component of each product and of each radiation dose. The ED 50 (concentration of fungicide necessary to cause 50% radial reduction of the fungic mycelium) of each fungicide in the different gamma radiation doses was determined. (M.A.C.) [pt

Protective, curative and eradicative activities of fungicides against grapevine rust

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Francislene Angelotti

2014-01-01

Full Text Available The protective, eradicative and curative activities of the fungicides azoxystrobin, tebuconazole, pyraclostrobin+metiram, and ciproconazole against grapevine rust, were determined in greenhouse. To evaluate the protective activity, leaves of potted ´Niagara´ (Vitis labrusca vines were artificially inoculated with an urediniospore suspension of Phakopsora euvitis four, eight or forteen days after fungicidal spray; and to evaluate the curative and eradicative activities, leaves were sprayed with fungicides two, four or eight days after inoculation. Disease severity was assessed 14 days after each inoculation. All tested fungicides present excellent preventive activity against grapevine rust; however, tebuconazole and ciproconazole provide better curative activity than azoxystrobin and pyraclostrobin+metiram. It was observed also that all tested fungicides significantly reduced the germination of urediniospore produced on sprayed leaves.

Fitness, Competitive Ability, and Mutation Stability of Isolates of Colletotrichum acutatum from Strawberry Resistant to QoI Fungicides.

Science.gov (United States)

Forcelini, Bruna B; Rebello, Carolina S; Wang, Nan-Yi; Peres, Natalia A

2018-04-01

Quinone-outside inhibitor (QoI) fungicides are used to manage anthracnose of strawberry, caused by Colletotrichum acutatum. However, selection for resistance to QoI fungicides was first reported in 2013 in Florida and, subsequently, in strawberry nurseries and production areas across the United States and Canada. C. acutatum resistance to QoIs is associated with the G143A point mutation in the cytochrome b gene. This mutation is known to be associated with field resistance even at high rates of QoI. In this study, we investigated the relative fitness and competitive ability of QoI-resistant and -sensitive C. acutatum isolates. A fitness comparison did not indicate any difference between resistant and sensitive isolates in aggressiveness, spore production, and mycelial growth at different temperatures. Additionally, in the absence of selection pressure, resistant and sensitive isolates were equally competitive. Cultivation of QoI-resistant and QoI-sensitive isolates for four culture cycles in vitro in the absence of azoxystrobin showed that QoI resistance was stable. The observed lack of fitness penalties and stability of the G143A mutation in QoI-resistant C. acutatum populations suggest that the interruption and further reintroduction of QoI fungicides might not be an option for strawberry nurseries and fruit production areas. Further investigation of alternative chemical and nonchemical C. acutatum control practices, in addition to the integration of multisite fungicides, is needed to reduce the occurrence and distribution of QoI-resistant populations in strawberry fields.

Occurrence of azoxystrobin, propiconazole, and selected other fungicides in US streams, 2005-2006

Science.gov (United States)

Battaglin, William A.; Sandstrom, Mark W.; Kuivila, Kathryn; Kolpin, Dana W.; Meyer, Michael T.

2011-01-01

Fungicides are used to prevent foliar diseases on a wide range of vegetable, field, fruit, and ornamental crops. They are generally more effective as protective rather than curative treatments, and hence tend to be applied before infections take place. Less than 1% of US soybeans were treated with a fungicide in 2002 but by 2006, 4% were treated. Like other pesticides, fungicides can move-off of fields after application and subsequently contaminate surface water, groundwater, and associated sediments. Due to the constant pressure from fungal diseases such as the recent Asian soybean rust outbreak, and the always-present desire to increase crop yields, there is the potential for a significant increase in the amount of fungicides used on US farms. Increased fungicide use could lead to increased environmental concentrations of these compounds. This study documents the occurrence of fungicides in select US streams soon after the first documentation of soybean rust in the US and prior to the corresponding increase in fungicide use to treat this problem. Water samples were collected from 29 streams in 13 states in 2005 and/or 2006, and analyzed for 12 target fungicides. Nine of the 12 fungicides were detected in at least one stream sample and at least one fungicide was detected in 20 of 29 streams. At least one fungicide was detected in 56% of the 103 samples, as many as five fungicides were detected in an individual sample, and mixtures of fungicides were common. Azoxystrobin was detected most frequently (45% of 103 samples) followed by metalaxyl (27%), propiconazole (17%), myclobutanil (9%), and tebuconazole (6%). Fungicide detections ranged from 0.002 to 1.15 μ/L. There was indication of a seasonal pattern to fungicide occurrence, with detections more common and concentrations higher in late summer and early fall than in spring. At a few sites, fungicides were detected in all samples collected suggesting the potential for season-long occurrence in some streams

Sertraline demonstrates fungicidal activity in vitro for Coccidioides immitis

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Simon Paul

2016-07-01

Full Text Available Coccidioidomycosis causes substantial morbidity in endemic areas. Disseminated coccidioidomycosis is an AIDS defining condition and treatment often requires lifelong antifungal therapy. Sertraline, a widely used serotonin-reuptake inhibitor anti-depressant, has demonstrated activity against Candida and Cryptococcus sp. both in vitro and in vivo. To evaluate if sertraline has activity against Coccidioides, the minimal inhibitory concentration (MIC and minimal fungicidal concentration (MFC of sertraline for four clinical isolates of C. immitis were determined. Sertraline was observed to have an MIC range of 4–8 µg/ml and MFC also of 4–8 µg/ml for Coccidioides. These MIC and MFC results for C. immitis are similar to those reported for Cryptococcus sp. suggesting sertraline may potentially have utility for the treatment of coccidioidomycosis.

Spatial and temporal distribution of fungicides applied to creeping bentgrass.

Science.gov (United States)

Hockemeyer, Kurt R; Latin, Richard

2015-05-01

Turf managers often rely on fungicides to limit damage caused by root diseases. Because fungicides are applied to aboveground surfaces and do not move basipetally, they are effective against root pathogens only when fungitoxic concentrations migrate to the rhizosphere. This research focused on the distribution of modern fungicides in verdure, thatch, sand, and roots of creeping bentgrass [ L. var. (Huds.) Farw.] maintained as a putting green. The fungicides azoxystrobin (methyl (E)-2-[2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl]-3-methoxyacrylate), propiconazole (1,2,4-triazole, 1-((2-(2,4-dichlorophenyl)-4-propyl-1,3-dioxolan-2-yl)methyl), pyraclostrobin (carbamic acid, [2-[[[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]phenyl]methoxy-,methyl ester), and thiophanate-methyl (dimethyl 4,'4-o-phenylenebis[3-thioallophanate]) were applied to replicate field plots in a water volume of 815 L ha. Plots were sampled at 0, 3, 7, 10, 14, 17, and 21 d after application by extracting cores measuring 1.9 cm in diameter by 3.8 cm deep. Cores were separated into verdure/thatch, sand, and roots before quantitative determination (liquid chromatography, triple quadrupole mass spectrometry) of fungicide residues. Fungicide residues in verdure/thatch declined steadily with time and support previously reported results describing fungicide depletion. Fungicides were detected in roots and sand within 5 h of application at very low (1-15 mg kg) concentrations and remained at low levels throughout the sampling period. Fungicides differed with respect to amounts recovered per turfgrass component. Azoxystrobin and propiconazole were associated with roots for the duration of the experiment, but pyraclostrobin was nearly undetectable. Near-zero levels of all fungicides were detected in the sand component. Half-life values in the verdure/thatch component ranged from 2.3 to 18.9 d. Copyright © by the American Society of Agronomy, Crop Science Society of America, and Soil Science Society of

Interactions between yeasts, fungicides and apple fruit russeting

NARCIS (Netherlands)

Gildemacher, P.R.; Heijne, B.; Silvestri, M.; Houbraken, J.; Hoekstra, E.; Theelen, B.; Boekhout, T.

2006-01-01

The effect of inoculations with yeasts occurring on apple surfaces and fungicide treatments on the russeting of Elstar apples was studied. Captan, dithianon and a water treatment were implemented to study the interaction between the fungicides, the inoculated yeast species and Aureobasidium

Biosynthesis of intestinal microvillar proteins. Processing of N-linked carbohydrate is not required for surface expression

DEFF Research Database (Denmark)

Danielsen, Erik Michael; Cowell, G M

1986-01-01

Castanospermine, an inhibitor of glucosidase I, the initial enzyme in the trimming of N-linked carbohydrate, was used to study the importance of carbohydrate processing in the biosynthesis of microvillar enzymes in organ-cultured pig intestinal explants. For aminopeptidase N (EC 3.4.11.2), aminop......Castanospermine, an inhibitor of glucosidase I, the initial enzyme in the trimming of N-linked carbohydrate, was used to study the importance of carbohydrate processing in the biosynthesis of microvillar enzymes in organ-cultured pig intestinal explants. For aminopeptidase N (EC 3...

Chemogenomics profiling of drug targets of peptidoglycan biosynthesis pathway in Leptospira interrogans by virtual screening approaches.

Science.gov (United States)

Bhattacharjee, Biplab; Simon, Rose Mary; Gangadharaiah, Chaithra; Karunakar, Prashantha

2013-06-28

Leptospirosis is a worldwide zoonosis of global concern caused by Leptospira interrogans. The availability of ligand libraries has facilitated the search for novel drug targets using chemogenomics approaches, compared with the traditional method of drug discovery, which is time consuming and yields few leads with little intracellular information for guiding target selection. Recent subtractive genomics studies have revealed the putative drug targets in peptidoglycan biosynthesis pathways in Leptospira interrogans. Aligand library for the murD ligase enzyme in the peptidoglycan pathway has also been identified. Our approach in this research involves screening of the pre-existing ligand library of murD with related protein family members in the putative drug target assembly in the peptidoglycan biosynthesis pathway. A chemogenomics approach has been implemented here, which involves screening of known ligands of a protein family having analogous domain architecture for identification of leads for existing druggable protein family members. By means of this approach, one murC and one murF inhibitor were identified, providing a platform for developing an antileptospirosis drug targeting the peptidoglycan biosynthesis pathway. Given that the peptidoglycan biosynthesis pathway is exclusive to bacteria, the in silico identified mur ligase inhibitors are expected to be broad-spectrum Gram-negative inhibitors if synthesized and tested in in vitro and in vivo assays.

Mode of action of the phenylpyrrole fungicide fenpiclonil in Fusarium sulphureum

NARCIS (Netherlands)

Jespers, A.B.K.

1994-01-01

In the last few decades, plant disease control has become heavily dependent on fungicides. Most modem fungicides were discovered by random synthesis and empirical optimization of lead structures. In general, these fungicides have specific modes of action and meet modem enviromnental

Effects of two commonly used fungicides on the amphipod Austrochiltonia subtenuis.

Science.gov (United States)

Vu, Hung T; Keough, Michael J; Long, Sara M; Pettigrove, Vincent J

2017-03-01

Fungicides are used widely in agriculture and have been detected in adjacent rivers and wetlands. However, relatively little is known about the potential effects of fungicides on aquatic organisms. The present study investigated the effects of 2 commonly used fungicides, the boscalid fungicide Filan ® and the myclobutanil fungicide Systhane ™ 400 WP, on life history traits (survival, growth, and reproduction) and energy reserves (lipid, protein, and glycogen content) of the amphipod Austrochiltonia subtenuis under laboratory conditions, at concentrations detected in aquatic environments. Amphipods were exposed to 3 concentrations of Filan (1 μg active ingredient [a.i.]/L, 10 μg a.i./L, and 40 μg a.i./L) and Systhane (0.3 μg a.i./L, 3 μg a.i./L, and 30 μg a.i./L) over 56 d. Both fungicides had similar effects on the amphipod at the organism level. Reproduction was the most sensitive endpoint, with offspring produced in controls but none produced in any of the fungicide treatments, and total numbers of gravid females in all fungicide treatments were reduced by up to 95%. Female amphipods were more sensitive than males in terms of growth. Systhane had significant effects on survival at all concentrations, whereas significant effects of Filan on survival were observed only at 10 μg a.i./L and 40 μg a.i./L. The effects of fungicides on energy reserves of the female amphipod were different. Filan significantly reduced amphipod protein content, whereas Systhane significantly reduced the lipid content. The present study demonstrates wide-ranging effects of 2 common fungicides on an ecologically important species that has a key role in trophic transfer and nutrient recycling in aquatic environments. These results emphasize the importance of considering the long-term effects of fungicides in the risk assessment of aquatic ecosystems. Environ Toxicol Chem 2017;36:720-726. © 2016 SETAC. © 2016 SETAC.

Lipid, membrane, and mitochondrial characteristics of Ustilago maydis following exposure to ergosterol biosynthesis inhibitors

Energy Technology Data Exchange (ETDEWEB)

Waterfield, W.F. III

1986-01-01

Pencoazole at 0.5 ..mu..g/ml inhibited ergosterol biosynthesis in U. maydis. Polar lipids of sporidia grown with 0.5 ..mu..g/ml penconazole for 7.5 or 22 hr or 1.0 ..mu..g/ml fenarimol for 7.5 hr contained more 18:2 than 18:1 fatty acids. There was usually more 18:1 than 18:2 fatty acids in polar lipids of untreated sporidia but this ratio was influenced by culture cell density. The high 18:2 to 18:1 ratio in the polar lipids from penconazole grown cells was unaffected by cell density. There was an increase in free fatty acids and these were enriched with 18:2 members in cells grown with 0.5 ..mu..g/ml penconazole for 22 hr. Unsaturation of triglycerides fatty acids did not differ appreciably from that of untreated sporidia. Untreated WT U. maydis protoplasts lysed more slowly in 0.3 M sorbitol than those prepared from WT sporidia grown for 16 hr with 1.0 ..mu..g/ml penconazole or 2.0 ..mu..g/ml fenarimol or from untreated erg-40 sporidia. Protoplasts were more permeable to crystal violet than were those from untreated WT sporidia. Mitochondria from untreated WT sporidia oxidizing pyruvate plus malate or succinate yielded higher ADP/O rations than mitochondria from erg-40 or penconazole grown WT sporidia. The mitochondrial ATPase of control cells had a Km of 0.8 mM ATP whereas the mitochondrial ATPase of penconazole grown WT and erg-40 had a Km value of 3.7 and 3.2 mM ATP, respectively. When the mitochondrial catalytic subunit of the ATPase from these mitochondria were solubilized, the Km did not differ. These studies suggest that changes in sterols and membrane fatty acids resulting from treatments with EBI fungicides cause increased membrane fluidity which affects membrane stability, permeability and activity of the mitochondrial ATPase.

The fungicidal and phytotoxic properties of benomyl and PPM in supplemented agar media supporting transgenic arabidopsis plants for a Space Shuttle flight experiment

Science.gov (United States)

Paul, A. L.; Semer, C.; Kucharek, T.; Ferl, R. J.

2001-01-01

Fungal contamination is a significant problem in the use of sucrose-enriched agar-based media for plant culture, especially in closed habitats such as the Space Shuttle. While a variety of fungicides are commercially available, not all are equal in their effectiveness in inhibiting fungal contamination. In addition, fungicide effectiveness must be weighed against its phytotoxicity and in this case, its influence on transgene expression. In a series of experiments designed to optimize media composition for a recent shuttle mission, the fungicide benomyl and the biocide "Plant Preservative Mixture" (PPM) were evaluated for effectiveness in controlling three common fungal contaminants, as well as their impact on the growth and development of arabidopsis seedlings. Benomyl proved to be an effective inhibitor of all three contaminants in concentrations as low as 2 ppm (parts per million) within the agar medium, and no evidence of phytotoxicity was observed until concentrations exceeded 20 ppm. The biocide mix PPM was effective as a fungicide only at concentrations that had deleterious effects on arabidopsis seedlings. As a result of these findings, a concentration of 3 ppm benomyl was used in the media for experiment PGIM-01 which flew on shuttle Columbia mission STS-93 in July 1999.

Acute toxicity of Headline® fungicide to Blanchard's cricket frogs (Acris blanchardi).

Science.gov (United States)

Cusaac, J Patrick W; Morrison, Shane A; Belden, Jason B; Smith, Loren M; McMurry, Scott T

2016-04-01

Previous laboratory studies have suggested that pyraclostrobin-containing fungicide formulations are toxic to amphibians at environmentally relevant concentrations. However, it is unknown if all pyraclostrobin formulations have similar toxicity and if toxicity occurs in different amphibian species. We investigated the acute toxicity of two formulations, Headline(®) fungicide and Headline AMP(®) fungicide, to Blanchard's cricket frogs (Acris blanchardi) based on a direct overspray scenario. In addition, we examined body residues of fungicide active ingredients in A. blanchardi following direct exposure to Headline AMP fungicide. Headline fungicide and Headline AMP fungicide had similar toxicity to A. blanchardi with calculated median lethal doses of 2.1 and 1.7 µg pyraclostrobin/cm(2), respectively, which are similar to the suggested maximum label rate in North American corn (2.2 and 1.52 µg pyraclostrobin/cm(2), respectively). Tissue concentrations of pyraclostrobin were lower than predicted based on full uptake of a direct dose, and did not drop during the first 24 h after exposure. Headline fungicides at corn application rates are acutely toxic to cricket frogs, but acute toxicity in the field will depend on worst-case exposure.

Increasing the Fungicidal Action of Amphotericin B by Inhibiting the Nitric Oxide-Dependent Tolerance Pathway

Directory of Open Access Journals (Sweden)

Kim Vriens

2017-01-01

Full Text Available Amphotericin B (AmB induces oxidative and nitrosative stresses, characterized by production of reactive oxygen and nitrogen species, in fungi. Yet, how these toxic species contribute to AmB-induced fungal cell death is unclear. We investigated the role of superoxide and nitric oxide radicals in AmB’s fungicidal activity in Saccharomyces cerevisiae, using a digital microfluidic platform, which enabled monitoring individual cells at a spatiotemporal resolution, and plating assays. The nitric oxide synthase inhibitor L-NAME was used to interfere with nitric oxide radical production. L-NAME increased and accelerated AmB-induced accumulation of superoxide radicals, membrane permeabilization, and loss of proliferative capacity in S. cerevisiae. In contrast, the nitric oxide donor S-nitrosoglutathione inhibited AmB’s action. Hence, superoxide radicals were important for AmB’s fungicidal action, whereas nitric oxide radicals mediated tolerance towards AmB. Finally, also the human pathogens Candida albicans and Candida glabrata were more susceptible to AmB in the presence of L-NAME, pointing to the potential of AmB-L-NAME combination therapy to treat fungal infections.

Identification of QoI fungicide-resistant genotypes of the wheat pathogen Zymoseptoria tritici in Algeria

Directory of Open Access Journals (Sweden)

Nora ALLIOUI

2016-05-01

Full Text Available Septoria tritici blotch caused by Zymoseptoria tritici is currently one of the most damaging diseases on bread and durum wheat crops worldwide. A total of 120 monoconidial isolates of this fungus were sampled in 2012 from five distinct geographical locations of Algeria (Guelma, Annaba, Constantine, Skikda and Oran and assessed for resistance to Quinone outside Inhibitors (QoI, a widely used class of fungicides for the control of fungal diseases of wheat. Resistance was screened using a mismatch PCR assay that identified the G143A mitochondrial cytochrome b substitution associated with QoI resistance. The isolates were QoI-sensitive, since all possessed the G143 wild-type allele, except for three isolates (two from Guelma and one from Annaba, which had fungicide resistance and possessed the A143 resistant allele. QoI resistance was confirmed phenotypically using a microplate bioassay in which the resistant isolates displayed high levels of half-maximal inhibitory azoxystrobin concentrations (IC50s when compared to sensitive reference isolates. Genetic fingerprinting of all isolates with microsatellite markers revealed that the three resistant isolates were distinct haplotypes, and were are not genetically distinguishable from the sensitive isolates. This study highlights QoI-resistant genotypes of Z. tritici in Algeria for the first time, and proposes a management strategy for QoI fungicide application to prevent further spread of resistance across the country or to other areas of Northern Africa.

Tomato strigolactones are derived from carotenoids and their biosynthesis is promoted by phosphate starvation

OpenAIRE

López-Ráez, Juan A.; Charnikhova, Tatsiana;; Gómez-Roldán,Victoria;; Matusova, Radoslava;; Kohlen, Wouter;; De Vos, Ric;; Verstappe, Francel;; Puech-Pages, Virginie;; Bécard, Guillaume;; Mulder, Patrick;; Bouwmeester, Harro;

2008-01-01

Strigolactones are rhizosphere signalling compounds that mediate host location in arbuscular mycorrhizal (AM) fungi and parasitic plants. Here, the regulation of the biosynthesis of strigolactones is studied in tomato (Solanum lycopersicum). * Strigolactone production under phosphate starvation, in the presence of the carotenoid biosynthesis inhibitor fluridone and in the abscisic acid (ABA) mutant notabilis were assessed using a germination bioassay with seeds of Orobanche ramosa; a hyphal b...

Involvement of a lipoxygenase-like enzyme in abscisic Acid biosynthesis.

Science.gov (United States)

Creelman, R A; Bell, E; Mullet, J E

1992-07-01

Several lines of evidence indicate that abscisic acid (ABA) is derived from 9'-cis-neoxanthin or 9'-cis-violaxanthin with xanthoxin as an intermediate. (18)O-labeling experiments show incorporation primarily into the side chain carboxyl group of ABA, suggesting that oxidative cleavage occurs at the 11, 12 (11', 12') double bond of xanthophylls. Carbon monoxide, a strong inhibitor of heme-containing P-450 monooxygenases, did not inhibit ABA accumulation, suggesting that the oxygenase catalyzing the carotenoid cleavage step did not contain heme. This observation, plus the ability of lipoxygenase to make xanthoxin from violaxanthin, suggested that a lipoxygenase-like enzyme is involved in ABA biosynthesis. To test this idea, the ability of several soybean (Glycine max L.) lipoxygenase inhibitors (5,8,11-eicosatriynoic acid, 5,8,11,14-eicosatetraynoic acid, nordihydroguaiaretic acid, and naproxen) to inhibit stress-induced ABA accumulation in soybean cell culture and soybean seedlings was determined. All lipoxygenase inhibitors significantly inhibited ABA accumulation in response to stress. These results suggest that the in vivo oxidative cleavage reaction involved in ABA biosynthesis requires activity of a nonheme oxygenase having lipoxygenase-like properties.

Biochemical changes induced by fungicides in nitrogen fixing Nostoc sp.

Science.gov (United States)

Deviram, G V N S; Pant, Gaurav; Prasuna, R Gyana

2013-01-01

The present study indicates the effect of fungicides (approved by WHO) and their behavior on nitrogen fixer of rice eco system Nostoc sp. Application of plant protecting chemicals at recommended levels braced up the growth of blue green algae thereby enhancing heterocyst formation and nitrogenase activity. Nostoc sp demoed varying degrees of sensitivity to fungicides. Biomass yield, protein, carbohydrate content reduced after 3pg/mL concentration. Heterocyst damage was observed from 4μg/mL, Proline content increased with increase in fungicide concentration, utmost yellowing of the culture started from 4μg/mL. The decreasing order of the toxicity to Nostoc sp with fungicides was Mancozeb> Ediphenphos> Carbendazim> Hexaconazole.

Triterpenoid biosynthesis in Euphorbia lathyris latex

International Nuclear Information System (INIS)

Hawkins, D.R.

1987-11-01

The structures of triterpenols, not previously been known, from Euphorbia lathyris latex are reported. A method for quantifying very small amounts of these compounds was developed. Concerning the biochemistry of the latex, no exogenous cofactors were required for the biosynthesis and the addition of compounds such as NADPAH and ATP do not stimulate the biosynthesis. The addition of DTE or a similar anti-oxidant was found to help reduce the oxidation of the latex, thus increasing the length of time that the latex remains active. The requirement of a divalent cation and the preference for Mn in the pellet was observed. The effect of several inhibitors on the biosynthesis of the triterpenoids was examined. Mevinolin was found to inhibit the biosynthesis of the triterpenoids from acetate, but not mevalonate. A dixon plot of the inhibition of acetate incorporation showed an I 50 concentration of 3.2 μM. Fenpropimorph was found to have little or no effect on the biosynthesis. Tridemorph was found to inhibit the biosynthesis of all of the triterpenoids with an I 50 of 4 μM. It was also observed that the cyclopropyl containing triterpenols, cycloartenol and 24-methylenecycloartenol were inhibited much more strongly than those containing an 8-9 double bond, lanosterol and 24-methylenelanosterol. The evidence indicates, but does not definetely prove, that lanosterol and 24-methylenelanosterol are not made from cycloartenol and 24-methylenecycloartenol via a ring-opening enzyme such as cycloeucalenol-obtusifoliol isomerase. The possibilty that cycloartenol is made via lanosterol was investigated by synthesizing 4-R-4- 3 H-mevalonic acid and incubating latex with a mixture of this and 14 C-mevalonic acid. From the 3 H/ 14 C ratio it was shown that cycloartenol and 24-methylenecycloartenol are not made via an intermediate containing as 8-9 double bond. 88 refs., 15 figs., 30 tabs

Terrestrial exposure and effects of Headline AMP(®) Fungicide on amphibians.

Science.gov (United States)

Cusaac, J Patrick W; Mimbs, William H; Belden, Jason B; Smith, Loren M; McMurry, Scott T

2015-08-01

Recent studies have demonstrated that a pyraclostrobin-containing fungicide (Headline(®) Fungicide--Headline(®) Fungicide and Headline AMP(®) Fungicide are registered trademarks of BASF) is toxic to amphibians at environmentally relevant concentrations. However, these studies were performed in a laboratory setting of a worst-case direct exposure in clean media. Interception of spray by the crop canopy and ground cover used by animals for security cover will influence exposure. Thus, risk to amphibians is unclear in an environmentally realistic field environment. We tested exposure and toxicity of Headline AMP(®) Fungicide to amphibians in multiple agricultural habitat scenarios (e.g., within treated crop vs. grassy areas adjacent to crop) and at two rates during routine aerial application. Specifically, we placed Woodhouse's toads (Bufo woodhousii) and Blanchard's cricket frogs (Acris blanchardi) in enclosures located within treated and untreated corn (VT stage, approximate height = 3 m), and in the potential drift area (adjacent to treated corn) during aerial application of Headline AMP Fungicide at either 731 or 1052 ml/ha (70 and 100 % the maximum application rate in corn, respectively). Mean concentrations of pyraclostrobin measured at ground level were ≤19 % of nominal application rate in all areas. Overall, mean mortality of recovered individuals of both species was ≤15 %, and mortality within Headline AMP Fungicide-treated corn (where risk was anticipated to be highest) was <10 %. It is important to understand that application timing, interception by the crop canopy (which varies both within and between crop systems), and timing of amphibian presence in the crop field influences risk of exposure and effects; however, our results demonstrate that amphibians inhabiting VT stage corn during routine aerial application of Headline AMP Fungicide are at low risk for acute mortality, matching existing laboratory results from acute toxicity studies of

Peroxidase enzymes regulate collagen extracellular matrix biosynthesis.

Science.gov (United States)

DeNichilo, Mark O; Panagopoulos, Vasilios; Rayner, Timothy E; Borowicz, Romana A; Greenwood, John E; Evdokiou, Andreas

2015-05-01

Myeloperoxidase and eosinophil peroxidase are heme-containing enzymes often physically associated with fibrotic tissue and cancer in various organs, without any direct involvement in promoting fibroblast recruitment and extracellular matrix (ECM) biosynthesis at these sites. We report herein novel findings that show peroxidase enzymes possess a well-conserved profibrogenic capacity to stimulate the migration of fibroblastic cells and promote their ability to secrete collagenous proteins to generate a functional ECM both in vitro and in vivo. Mechanistic studies conducted using cultured fibroblasts show that these cells are capable of rapidly binding and internalizing both myeloperoxidase and eosinophil peroxidase. Peroxidase enzymes stimulate collagen biosynthesis at a post-translational level in a prolyl 4-hydroxylase-dependent manner that does not require ascorbic acid. This response was blocked by the irreversible myeloperoxidase inhibitor 4-amino-benzoic acid hydrazide, indicating peroxidase catalytic activity is essential for collagen biosynthesis. These results suggest that peroxidase enzymes, such as myeloperoxidase and eosinophil peroxidase, may play a fundamental role in regulating the recruitment of fibroblast and the biosynthesis of collagen ECM at sites of normal tissue repair and fibrosis, with enormous implications for many disease states where infiltrating inflammatory cells deposit peroxidases. Copyright © 2015 American Society for Investigative Pathology. Published by Elsevier Inc. All rights reserved.

Sensitivity of Phakopsora pachyrhizi (soybean rust) isolates to fungicides and the reduction of fungal sporulation based on fungicide and timing of application

Science.gov (United States)

Soybean rust is a damaging foliar fungal disease of soybean in many soybean-growing areas throughout the world. Strategies to manage soybean rust include the use of foliar fungicides. Fungicides types, the rate of product application, and the number and timing of applications are critical components...

In vitro screening of fungicides and antagonists against Sclerotium ...

African Journals Online (AJOL)

A study was conducted in the microbiology laboratory of Plant Pathology Department, Bangabandhu Sheikh Mujibur Rahman Agricultural University, Gazipur, during 2010 to 2011 to control Sclerotium rolfsii with fungicides and Trichoderma harzianum. Six fungicides namely Provax-200, Bavistin, Ridomil, Dithane M-45, ...

Factors influencing activity of triazole fungicides towards Botrytis cinerea.

NARCIS (Netherlands)

Stehmann, C.; Waard, de M.A.

1996-01-01

The activity of triazole fungicides towards Botrytis cinerea was investigated in vitro (radial growth on fungicide-amended agar) and in vivo (foliar-sprayed tomato plants and dip-treated grapes). In both tests the benzimidazoles, benomyl and thiabendazole, and the dicarboximides, iprodione and

Biosynthesis of collagen by fibroblasts kept in culture

International Nuclear Information System (INIS)

Machado-Santelli, G.M.

1978-01-01

The sinthesis of collagen is studied in fibroblasts of different origins with the purpose of obtaining an appropriate system for the study of its biosynthesis and processing. The percentage of collagen synthesis vary according to the fibroblast origin. Experiences are performed with fibroblasts kept in culture from: chicken - and guinea pig embryos, carragheenin - induced granulomas in adult guinea pig and from human skin. The collagen pattern synthesized after acetic acid - or saline extractions in the presence of inhibitors is also determined. This pattern is then assayed by poliacrilamide - 5% - SDS gel electrophoresis accompanied by fluorography. The importance of the cell culture system in the elucidation of collagen biosynthesis is pointed out. (M.A.) [pt

Analysis of the Staphylococcus aureus capsule biosynthesis pathway in vitro: characterization of the UDP-GlcNAc C6 dehydratases CapD and CapE and identification of enzyme inhibitors.

Science.gov (United States)

Li, Wenjin; Ulm, Hannah; Rausch, Marvin; Li, Xue; O'Riordan, Katie; Lee, Jean C; Schneider, Tanja; Müller, Christa E

2014-11-01

Polysaccharide capsules significantly contribute to virulence of invasive pathogens, and inhibition of capsule biosynthesis may offer a valuable strategy for novel anti-infective treatment. We purified and characterized the enzymes CapD and CapE of the Staphylococcus aureus serotype 5 biosynthesis cluster, which catalyze the first steps in the synthesis of the soluble capsule precursors UDP-D-FucNAc and UDP-L-FucNAc, respectively. CapD is an integral membrane protein and was obtained for the first time in a purified, active form. A capillary electrophoresis (CE)-based method applying micellar electrokinetic chromatography (MEKC) coupled with UV detection at 260 nm was developed for functional characterization of the enzymes using a fused-silica capillary, electrokinetic injection, and dynamic coating with polybrene at pH 12.4. The limits of detection for the CapD and CapE products UDP-2-acetamido-2,6-dideoxy-α-D-xylo-hex-4-ulose and UDP-2-acetamido-2,6-dideoxy-β-L-arabino-hex-4-ulose, respectively, were below 1 μM. Using this new, robust and sensitive method we performed kinetic studies for CapD and CapE and screened a compound library in search for enzyme inhibitors. Several active compounds were identified and characterized, including suramin (IC50 at CapE 1.82 μM) and ampicillin (IC50 at CapD 40.1 μM). Furthermore, the cell wall precursors UDP-D-MurNAc-pentapeptide and lipid II appear to function as inhibitors of CapD enzymatic activity, suggesting an integrated mechanism of regulation for cell envelope biosynthesis pathways in S. aureus. Corroborating the in vitro findings, staphylococcal cells grown in the presence of subinhibitory concentrations of ampicillin displayed drastically reduced CP production. Our studies contribute to a profound understanding of the capsule biosynthesis in pathogenic bacteria. This approach may lead to the identification of novel anti-virulence and antibiotic drugs. Copyright © 2014 Elsevier GmbH. All rights reserved.

Design, synthesis, and fungicidal activities of imino diacid analogs of valine amide fungicides.

Science.gov (United States)

Sun, Man; Yang, Hui-Hui; Tian, Lei; Li, Jian-Qiang; Zhao, Wei-Guang

2015-12-15

The novel imino diacid analogs of valine amides were synthesized via several steps, including the protection, amidation, deprotection, and amino alkylation of valine, with the resulting structures confirmed by (1)H and (13)C NMR and HRMS. Bioassays showed that some of these compounds exhibited good fungicidal activity. Notably, isopropyl 2-((1-((1-(3-fluorophenyl)ethyl)amino)-3-methyl-1-oxobutan-2-yl)amino)propanoate 5i displayed significant levels of control, at 50%, against Erysiphe graminis at 3.9μM as well as a level of potency very similar to the reference azoxystrobin, which gave 60% activity at this concentration. The present work demonstrates that imino diacid analogs of valine amides could be potentially useful key compounds for the development of novel fungicides against wheat powdery mildew. Copyright © 2015 Elsevier Ltd. All rights reserved.

Triazole fungicide tebuconazole disrupts human placental trophoblast cell functions

Energy Technology Data Exchange (ETDEWEB)

Zhou, Jinghua [Key Laboratory of Environmental Remediation and Ecological Health, Ministry of Education, Zhejiang University, Hangzhou 310058 (China); Zhang, Jianyun [Research Center for Air Pollution and Health, College of Environmental and Resource Sciences, Zhejiang University, Hangzhou 310058 (China); Li, Feixue [Zhejiang Key Laboratory of Organ Development and Regeneration, Institute of Developmental and Regenerative Biology, College of Life and Environmental Sciences, Hangzhou Normal University, Hangzhou 310036 (China); Liu, Jing, E-mail: jliue@zju.edu.cn [Key Laboratory of Environmental Remediation and Ecological Health, Ministry of Education, Zhejiang University, Hangzhou 310058 (China); Research Center for Air Pollution and Health, College of Environmental and Resource Sciences, Zhejiang University, Hangzhou 310058 (China)

2016-05-05

Highlights: • Tebuconazole (TEB) inhibited the proliferation of human placental trophoblasts. • TEB changed cell cycle distribution of G1 and G2 phases of trophoblasts. • TEB induced apoptosis of trophoblasts via mitochondrial pathway. • TEB decreased the invasive and migratory capacities of trophoblasts. • TEB altered the mRNA levels of key regulatory genes in trophoblasts - Abstract: Triazole fungicides are one of the top ten classes of current-use pesticides. Although exposure to triazole fungicides is associated with reproductive toxicity in mammals, limited information is available regarding the effects of triazole fungicides on human placental trophoblast function. Tebuconazole (TEB) is a common triazole fungicide that has been extensively used for fungi control. In this work, we showed that TEB could reduce cell viability, disturb normal cell cycle distribution and induce apoptosis of human placental trophoblast cell line HTR-8/SVneo (HTR-8). Bcl-2 protein expression decreased and the level of Bax protein increased after TEB treatment in HTR-8 cells. The results demonstrated that this fungicide induced apoptosis of trophoblast cells via mitochondrial pathway. Importantly, we found that the invasive and migratory capacities of HTR-8 cells decreased significantly after TEB administration. TEB altered the expression of key regulatory genes involved in the modulation of trophoblast functions. Taken together, TEB suppressed human trophoblast invasion and migration through affecting the expression of protease, hormones, angiogenic factors, growth factors and cytokines. As the invasive and migratory abilities of trophoblast are essential for successful placentation and fetus development, our findings suggest a potential risk of triazole fungicides to human pregnancy.

Triazole fungicide tebuconazole disrupts human placental trophoblast cell functions

International Nuclear Information System (INIS)

Zhou, Jinghua; Zhang, Jianyun; Li, Feixue; Liu, Jing

2016-01-01

Highlights: • Tebuconazole (TEB) inhibited the proliferation of human placental trophoblasts. • TEB changed cell cycle distribution of G1 and G2 phases of trophoblasts. • TEB induced apoptosis of trophoblasts via mitochondrial pathway. • TEB decreased the invasive and migratory capacities of trophoblasts. • TEB altered the mRNA levels of key regulatory genes in trophoblasts - Abstract: Triazole fungicides are one of the top ten classes of current-use pesticides. Although exposure to triazole fungicides is associated with reproductive toxicity in mammals, limited information is available regarding the effects of triazole fungicides on human placental trophoblast function. Tebuconazole (TEB) is a common triazole fungicide that has been extensively used for fungi control. In this work, we showed that TEB could reduce cell viability, disturb normal cell cycle distribution and induce apoptosis of human placental trophoblast cell line HTR-8/SVneo (HTR-8). Bcl-2 protein expression decreased and the level of Bax protein increased after TEB treatment in HTR-8 cells. The results demonstrated that this fungicide induced apoptosis of trophoblast cells via mitochondrial pathway. Importantly, we found that the invasive and migratory capacities of HTR-8 cells decreased significantly after TEB administration. TEB altered the expression of key regulatory genes involved in the modulation of trophoblast functions. Taken together, TEB suppressed human trophoblast invasion and migration through affecting the expression of protease, hormones, angiogenic factors, growth factors and cytokines. As the invasive and migratory abilities of trophoblast are essential for successful placentation and fetus development, our findings suggest a potential risk of triazole fungicides to human pregnancy.

Pathogenicity and fungicide sensitivity of the causal agent of ...

African Journals Online (AJOL)

The pathogenicity of the fungus and its cross-infection potential were determined on mango, avocado, papaya and banana fruits. The sensitivity of the pathogen to fungicides was determined by assessing radial mycelial growth on potato dextrose agar (PDA) amended with nine different fungicides (Bendazim, Funguran, ...

Curative and eradicant action of fungicides to control Phakopsora pachyrhizi in soybean plants

Directory of Open Access Journals (Sweden)

Erlei Melo Reis

Full Text Available ABSTRACT Experiments were carried out in a growth chamber and laboratory to quantify the curative and eradicant actions of fungicides in Asian soybean rust control. The experiments were conducted with the CD 214 RR cultivar, assessing the following fungicides, separately or in association, chlorothalonil, flutriafol, cyproconazole + trifloxystrobin, epoxiconazole + pyraclostrobin, cyproconazole + azoxystrobin, and cyproconazole + picoxystrobin. The fungicides were applied at four (curative and nine days after inoculation (eradicant treatment. Treatments were evaluated according to the density of lesions and uredia/cm2, and the eradicant treatment was assessed based on the necrosis of lesions/uredia and on uredospore viability. Except for the fungicide chlorothalonil, there was curative action of latent/virtual infections by the fungicides. Penetrant fungicides that are absorbed have curative and eradicant action to soybean rust.

Leaching of two fungicides in spent mushroom substrate amended soil: Influence of amendment rate, fungicide ageing and flow condition.

Science.gov (United States)

Álvarez-Martín, Alba; Sánchez-Martín, María J; Ordax, José M; Marín-Benito, Jesús M; Sonia Rodríguez-Cruz, M

2017-04-15

A study has been conducted on the leaching of two fungicides, tebuconazole and cymoxanil, in a soil amended with spent mushroom substrate (SMS), with an evaluation of how different factors influence this process. The objective was based on the potential use of SMS as a biosorbent for immobilizing pesticides in vulnerable soils, and the need to know how it could affect the subsequent transport of these retained compounds. Breakthrough curves (BTCs) for 14 C-fungicides, non-incubated and incubated over 30days, were obtained in columns packed with an unamended soil (S), and this soil amended with SMS at rates of 5% (S+SMS5) and 50% (S+SMS50) under saturated and saturated-unsaturated flows. The highest leaching of tebuconazole (>50% of the total 14 C added) was found in S when a saturated water flow was applied to the column, but the percentage of leached fungicide decreased when a saturated-unsaturated flow was applied in both SMS-amended soils. Also a significant decrease in leaching was observed for tebuconazole after incubation in the column, especially in S+SMS50 when both flows were applied. Furthermore, cymoxanil leaching was complete in S and S+SMS when a saturated flow was applied, and maximum peak concentrations were reached at 1pore volume (PV), although BTCs showed peaks with lower concentrations in S+SMS. The amounts of cymoxanil retained only increased in S+SMS when a saturated-unsaturated flow was applied. A more relevant effect of SMS for reducing the leaching of fungicide was observed when cymoxanil was previously incubated in the column, although mineralization was enhanced in this case. These results are of interest for extending SMS application on the control of the leaching of fungicides with different physicochemical characteristics after different ageing times in the soil and water flow conditions applied. Copyright © 2017 Elsevier B.V. All rights reserved.

Novel guanidine-based inhibitors of inosine monophosphate dehydrogenase.

Science.gov (United States)

Iwanowicz, Edwin J; Watterson, Scott H; Liu, Chunjian; Gu, Henry H; Mitt, Toomas; Leftheris, Katerina; Barrish, Joel C; Fleener, Catherine A; Rouleau, Katherine; Sherbina, N Z; Hollenbaugh, Diane L

2002-10-21

A series of novel guanidine-based small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH) was explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.

Involvement of a Lipoxygenase-Like Enzyme in Abscisic Acid Biosynthesis 1

Science.gov (United States)

Creelman, Robert A.; Bell, Erin; Mullet, John E.

1992-01-01

Several lines of evidence indicate that abscisic acid (ABA) is derived from 9′-cis-neoxanthin or 9′-cis-violaxanthin with xanthoxin as an intermediate. 18O-labeling experiments show incorporation primarily into the side chain carboxyl group of ABA, suggesting that oxidative cleavage occurs at the 11, 12 (11′, 12′) double bond of xanthophylls. Carbon monoxide, a strong inhibitor of heme-containing P-450 monooxygenases, did not inhibit ABA accumulation, suggesting that the oxygenase catalyzing the carotenoid cleavage step did not contain heme. This observation, plus the ability of lipoxygenase to make xanthoxin from violaxanthin, suggested that a lipoxygenase-like enzyme is involved in ABA biosynthesis. To test this idea, the ability of several soybean (Glycine max L.) lipoxygenase inhibitors (5,8,11-eicosatriynoic acid, 5,8,11,14-eicosatetraynoic acid, nordihydroguaiaretic acid, and naproxen) to inhibit stress-induced ABA accumulation in soybean cell culture and soybean seedlings was determined. All lipoxygenase inhibitors significantly inhibited ABA accumulation in response to stress. These results suggest that the in vivo oxidative cleavage reaction involved in ABA biosynthesis requires activity of a nonheme oxygenase having lipoxygenase-like properties. PMID:16668998

Evaluation of fungicides and biopesticides for the control of fusarium wilt of tomato

International Nuclear Information System (INIS)

Akhtar, T.; Iftikhar, Y.

2017-01-01

Fusarium wilt is highly destructive soil borne pathogen in tomato. Current study was carried out to evaluate commercially available fungicides and bio-fungicides in-vitro and in-vivo, for their efficacy against Fusarium oxysporum f.sp. lycopersici. Firstly four fungicides were evaluated under laboratory conditions. Three promising fungicides, two biopesticides and Trichoderma harzianum were further applied both in greenhouse and field experiments. During in-vitro studies PDA amended with fungicides with different treatments at the rate 1% almost completely inhibited the growth of Fol with varying degree of success whereas Nativo being the most effective treatment with 98% reduction in growth as compared to control. Nativo significantly reduced the disease incidence (32.75 %) at concentration of 1%. While Poly-beta-hydroxyl-butyric-acid effectively promoted the tomato growth. Maximum reduction in disease (30.14 %) was expressed by Nativo followed by Teagro (25.06 %) under field conditions. Nativo was found to be the most effective fungicide for management of Fol both In vitro and In vivo. Further field evaluations of the fungicides are required. (author)

Disruption of quercetin metabolism by fungicide affects energy production in honey bees (Apis mellifera).

Science.gov (United States)

Mao, Wenfu; Schuler, Mary A; Berenbaum, May R

2017-03-07

Cytochrome P450 monooxygenases (P450) in the honey bee, Apis mellifera , detoxify phytochemicals in honey and pollen. The flavonol quercetin is found ubiquitously and abundantly in pollen and frequently at lower concentrations in honey. Worker jelly consumed during the first 3 d of larval development typically contains flavonols at very low levels, however. RNA-Seq analysis of gene expression in neonates reared for three days on diets with and without quercetin revealed that, in addition to up-regulating multiple detoxifying P450 genes, quercetin is a negative transcriptional regulator of mitochondrion-related nuclear genes and genes encoding subunits of complexes I, III, IV, and V in the oxidative phosphorylation pathway. Thus, a consequence of inefficient metabolism of this phytochemical may be compromised energy production. Several P450s metabolize quercetin in adult workers. Docking in silico of 121 pesticide contaminants of American hives into the active pocket of CYP9Q1, a broadly substrate-specific P450 with high quercetin-metabolizing activity, identified six triazole fungicides, all fungal P450 inhibitors, that dock in the catalytic site. In adults fed combinations of quercetin and the triazole myclobutanil, the expression of five of six mitochondrion-related nuclear genes was down-regulated. Midgut metabolism assays verified that adult bees consuming quercetin with myclobutanil metabolized less quercetin and produced less thoracic ATP, the energy source for flight muscles. Although fungicides lack acute toxicity, they may influence bee health by interfering with quercetin detoxification, thereby compromising mitochondrial regeneration and ATP production. Thus, agricultural use of triazole fungicides may put bees at risk of being unable to extract sufficient energy from their natural food.

Additive and synergistic antiandrogenic activities of mixtures of azol fungicides and vinclozolin

Energy Technology Data Exchange (ETDEWEB)

Christen, Verena [University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences, Gründenstrasse 40, CH-4132 Muttenz (Switzerland); Crettaz, Pierre [Federal Office of Public Health, Division Chemical Products, 3003 Bern (Switzerland); Fent, Karl, E-mail: karl.fent@fhnw.ch [University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences, Gründenstrasse 40, CH-4132 Muttenz (Switzerland); ETH Zürich, Department of Environmental System Sciences, Institute of Biogeochemistry and Pollution Dynamics, Universitätsstrasse 16, CH-8092 Zürich (Switzerland)

2014-09-15

Objective: Many pesticides including pyrethroids and azole fungicides are suspected to have an endocrine disrupting property. At present, the joint activity of compound mixtures is only marginally known. Here we tested the hypothesis that the antiandrogenic activity of mixtures of azole fungicides can be predicted by the concentration addition (CA) model. Methods: The antiandrogenic activity was assessed in MDA-kb2 cells. Following assessing single compounds activities mixtures of azole fungicides and vinclozolin were investigated. Interactions were analyzed by direct comparison between experimental and estimated dose–response curves assuming CA, followed by an analysis by the isobole method and the toxic unit approach. Results: The antiandrogenic activity of pyrethroids deltamethrin, cypermethrin, fenvalerate and permethrin was weak, while the azole fungicides tebuconazole, propiconazole, epoxiconazole, econazole and vinclozolin exhibited strong antiandrogenic activity. Ten binary and one ternary mixture combinations of five antiandrogenic fungicides were assessed at equi-effective concentrations of EC{sub 25} and EC{sub 50}. Isoboles indicated that about 50% of the binary mixtures were additive and 50% synergistic. Synergism was even more frequently indicated by the toxic unit approach. Conclusion: Our data lead to the conclusion that interactions in mixtures follow the CA model. However, a surprisingly high percentage of synergistic interactions occurred. Therefore, the mixture activity of antiandrogenic azole fungicides is at least additive. Practice: Mixtures should also be considered for additive antiandrogenic activity in hazard and risk assessment. Implications: Our evaluation provides an appropriate “proof of concept”, but whether it equally translates to in vivo effects should further be investigated. - Highlights: • Humans are exposed to pesticide mixtures such as pyrethroids and azole fungicides. • We assessed the antiandrogenicity of

Additive and synergistic antiandrogenic activities of mixtures of azol fungicides and vinclozolin

International Nuclear Information System (INIS)

Christen, Verena; Crettaz, Pierre; Fent, Karl

2014-01-01

Objective: Many pesticides including pyrethroids and azole fungicides are suspected to have an endocrine disrupting property. At present, the joint activity of compound mixtures is only marginally known. Here we tested the hypothesis that the antiandrogenic activity of mixtures of azole fungicides can be predicted by the concentration addition (CA) model. Methods: The antiandrogenic activity was assessed in MDA-kb2 cells. Following assessing single compounds activities mixtures of azole fungicides and vinclozolin were investigated. Interactions were analyzed by direct comparison between experimental and estimated dose–response curves assuming CA, followed by an analysis by the isobole method and the toxic unit approach. Results: The antiandrogenic activity of pyrethroids deltamethrin, cypermethrin, fenvalerate and permethrin was weak, while the azole fungicides tebuconazole, propiconazole, epoxiconazole, econazole and vinclozolin exhibited strong antiandrogenic activity. Ten binary and one ternary mixture combinations of five antiandrogenic fungicides were assessed at equi-effective concentrations of EC 25 and EC 50 . Isoboles indicated that about 50% of the binary mixtures were additive and 50% synergistic. Synergism was even more frequently indicated by the toxic unit approach. Conclusion: Our data lead to the conclusion that interactions in mixtures follow the CA model. However, a surprisingly high percentage of synergistic interactions occurred. Therefore, the mixture activity of antiandrogenic azole fungicides is at least additive. Practice: Mixtures should also be considered for additive antiandrogenic activity in hazard and risk assessment. Implications: Our evaluation provides an appropriate “proof of concept”, but whether it equally translates to in vivo effects should further be investigated. - Highlights: • Humans are exposed to pesticide mixtures such as pyrethroids and azole fungicides. • We assessed the antiandrogenicity of pyrethroids and

Control of Vascular Streak Dieback Disease of Cocoa with Flutriafol Fungicides

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Febrilia Nur'aini

2014-12-01

Full Text Available Vascular streak dieback caused by the fungus Oncobasidium theobromae is one of the important diseases in cocoa crop in Indonesia. One approach to control the disease is by using fungicides. The aim of this research was to determine the effect of class triazole fungicides to the intensity of the vascular streak dieback disease on cocoa seedling phase, immature and mature cocoa. Experiments were conducted in Kotta Blater, PTPN XII and Kaliwining, Indonesian  Coffee and Cocoa Research Institute. Flutriafol 250 g/l with a concentration 0,05%, 0,1% and 0,15% foliar sprayed on cocoa seedlings, immature and mature cocoa. Active compound combination of Azoxystrobin and Difenoconazole with 0,1% concentration used as a comparation fungicides. The result showed that Flutriafol with 0,05%, 0,1% and 0,15% concentration and Azoxystrobin & Difenoconazol with 0,1% concentration could suppress the vascular streak dieback disease on seedlings. On immature plants, the application of Flutriafol was not effectively suppress the vascular streak dieback disease whereas the fungicide comparison could suppress with the efficacy level of 46.22%. On mature plants,both of fungicides could not suppress the vascular streak dieback disease. Key words: Fungicide, cocoa, vascular streak dieback, triazole, flutriafol, azoxystrobin+difenoconazol

Bioengineered silver nanoparticles using Curvularia pallescens and its fungicidal activity against Cladosporium fulvum

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Abdallah M. Elgorban

2017-11-01

Full Text Available Microorganisms based biosynthesis of nanomaterials has triggered significant attention, due to their great potential as vast source of the production of biocompatible nanoparticles (NPs. Such biosynthesized functional nanomaterials can be used for various biomedical applications. The present study investigates the green synthesis of silver nanoparticles (Ag NPs using the fungus Curvularia pallescens (C. pallescens which is isolated from cereals. The C. pallescens cell filtrate was used for the reduction of AgNO3 to Ag NPs. To the best of our knowledge C. pallescens is utilized first time for the preparation of Ag NPs. Several alkaloids and proteins present in the phytopathogenic fungus C. pallescens were mainly responsible for the formation of highly crystalline Ag NPs. The as-synthesized Ag NPs were characterized by using UV–Visible spectroscopy, X-ray diffraction and transmission electron microscopy (TEM. The TEM micrographs have revealed that spherical shaped Ag NPs with polydisperse in size were obtained. These results have clearly suggested that the biomolecules secreted by C. pallescens are mainly responsible for the formation and stabilization of nanoparticles. Furthermore, the antifungal activity of the as-prepared Ag NPs was tested against Cladosporium fulvum, which is the major cause of a serious plant disease, known as tomato leaf mold. The synthesized Ag NPs displayed excellent fungicidal activity against the tested fungal pathogen. The extreme zone of reduction occurred at 50 μL, whereas, an increase in the reduction activity is observed with increasing the concentration of Ag NPs. These encouraging results can be further exploited by employing the as synthesized Ag NPs against various pathogenic fungi in order to ascertain their spectrum of fungicidal activity.

Control of sugar beet powdery mildew with strobilurin fungicides

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Karaoglanidis George S.

2006-01-01

Full Text Available Powdery mildew, caused by Erysiphe betae is a major foliar disease of sugar beet in areas with dry and relatively warm weather conditions throughout the world. In the present study, four fungicides belonging to the relatively new class of strobilurin fungicides, azoxystrobin, kresoxim-methyl pyraclostrobin and trifloxystrobin were evaluated in three different application doses (100, 150 and 200 mg a.i. ha–1 during 2003-2004 for the control of the disease. Among the four strobilurin fungicides tested trifloxystrobin and kresoxim-methyl were the most effective with control efficiency values higher than 94% compared to the control treatment even when applied at lower application dose of 100 mg a.i. ha–1. Azoxystrobin and pyraclostrobin showed a poor to modest activity against the disease even when applied at the highest application dose of 200 μg a.i. ha–1. Disease severity, in terms of AUDPC values was significantly correlated to decreased root yield, while no significant correlation existed among disease severity and sugar content of the roots or sucrose yield. In addition, the efficiency of tank mixtures of four strobilurin fungicides applied at 100 μg a.i. ha–1 with two sterol demethylation - inhibiting fungicides (DMIs, difenoconazole and cyproconazole applied at 62.5 and 25 mg a.i. ha–1, respectively, was evaluated. The mixtures of azoxystrobin and pyraclostrobin with either difenoconazole or cyproconazole provided a better control efficiency compared to the single application of each mixture partner, while the tank mixtures of trifloxystrobin and kresoxim-methyl with either difenoconazole or cyproconazole provided a better control efficiency compared to single application of difenoconazole or cyproconazole and similar control efficiency compared to the efficiency obtained by single application of the strobilurin fungicides.

Inhibition of glycolipid biosynthesis by N-(5-adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin protects against the inflammatory response in hapten-induced colitis

NARCIS (Netherlands)

Shen, Chong; Bullens, Dominique; Kasran, Ahmad; Maerten, Philippe; Boon, Louis; Aerts, Johannes M. F. G.; van Assche, Gert; Geboes, Karel; Rutgeerts, Paul; Ceuppens, Jan L.

2004-01-01

Since glycolipid biosynthesis is potentially involved in immunological and inflammatory responses, we tested the effect of a novel inhibitor of intracellular glycolipid biosynthesis N-(5-adamantane-1-yl-methoxy-pentyl)-deoxynojirimycin (AMP-DNM) in two hapten-induced colitis models: trinitrobenzene

Triterpenoid biosynthesis in Euphorbia lathyris latex

Energy Technology Data Exchange (ETDEWEB)

Hawkins, D.R.

1987-11-01

The structures of triterpenols, not previously been known, from Euphorbia lathyris latex are reported. A method for quantifying very small amounts of these compounds was developed. Concerning the biochemistry of the latex, no exogenous cofactors were required for the biosynthesis and the addition of compounds such as NADPAH and ATP do not stimulate the biosynthesis. The addition of DTE or a similar anti-oxidant was found to help reduce the oxidation of the latex, thus increasing the length of time that the latex remains active. The requirement of a divalent cation and the preference for Mn in the pellet was observed. The effect of several inhibitors on the biosynthesis of the triterpenoids was examined. Mevinolin was found to inhibit the biosynthesis of the triterpenoids from acetate, but not mevalonate. A dixon plot of the inhibition of acetate incorporation showed an I/sub 50/ concentration of 3.2 ..mu..M. Fenpropimorph was found to have little or no effect on the biosynthesis. Tridemorph was found to inhibit the biosynthesis of all of the triterpenoids with an I/sub 50/ of 4 ..mu..M. It was also observed that the cyclopropyl containing triterpenols, cycloartenol and 24-methylenecycloartenol were inhibited much more strongly than those containing an 8-9 double bond, lanosterol and 24-methylenelanosterol. The evidence indicates, but does not definetely prove, that lanosterol and 24-methylenelanosterol are not made from cycloartenol and 24-methylenecycloartenol via a ring-opening enzyme such as cycloeucalenol-obtusifoliol isomerase. The possibilty that cycloartenol is made via lanosterol was investigated by synthesizing 4-R-4-/sup 3/H-mevalonic acid and incubating latex with a mixture of this and /sup 14/C-mevalonic acid. From the /sup 3/H//sup 14/C ratio it was shown that cycloartenol and 24-methylenecycloartenol are not made via an intermediate containing as 8-9 double bond. 88 refs., 15 figs., 30 tabs.

Alpha-Difluoromethylornithine, an Irreversible Inhibitor of Polyamine Biosynthesis, as a Therapeutic Strategy against Hyperproliferative and Infectious Diseases

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Nicole LoGiudice

2018-02-01

Full Text Available The fluorinated ornithine analog α-difluoromethylornithine (DFMO, eflornithine, ornidyl is an irreversible suicide inhibitor of ornithine decarboxylase (ODC, the first and rate-limiting enzyme of polyamine biosynthesis. The ubiquitous and essential polyamines have many functions, but are primarily important for rapidly proliferating cells. Thus, ODC is potentially a drug target for any disease state where rapid growth is a key process leading to pathology. The compound was originally discovered as an anticancer drug, but its effectiveness was disappointing. However, DFMO was successfully developed to treat African sleeping sickness and is currently one of few clinically used drugs to combat this neglected tropical disease. The other Food and Drug Administration (FDA approved application for DFMO is as an active ingredient in the hair removal cream Vaniqa. In recent years, renewed interest in DFMO for hyperproliferative diseases has led to increased research and promising preclinical and clinical trials. This review explores the use of DFMO for the treatment of African sleeping sickness and hirsutism, as well as its potential as a chemopreventive and chemotherapeutic agent against colorectal cancer and neuroblastoma.

Purine biosynthesis is the bottleneck in trimethoprim-treated Bacillus subtilis.

Science.gov (United States)

Stepanek, Jennifer Janina; Schäkermann, Sina; Wenzel, Michaela; Prochnow, Pascal; Bandow, Julia Elisabeth

2016-10-01

Trimethoprim is a folate biosynthesis inhibitor. Tetrahydrofolates are essential for the transfer of C 1 units in several biochemical pathways including purine, thymine, methionine, and glycine biosynthesis. This study addressed the effects of folate biosynthesis inhibition on bacterial physiology. Two complementary proteomic approaches were employed to analyze the response of Bacillus subtilis to trimethoprim. Acute changes in protein synthesis rates were monitored by radioactive pulse labeling of newly synthesized proteins and subsequent 2DE analysis. Changes in protein levels were detected using gel-free quantitative MS. Proteins involved in purine and histidine biosynthesis, the σ B -dependent general stress response, and sporulation were upregulated. Most prominently, the PurR-regulon required for de novo purine biosynthesis was derepressed indicating purine depletion. The general stress response was activated energy dependently and in a subpopulation of treated cultures an early onset of sporulation was observed, most likely triggered by low guanosine triphosphate levels. Supplementation of adenosine triphosphate, adenosine, and guanosine to the medium substantially decreased antibacterial activity, showing that purine depletion becomes the bottleneck in trimethoprim-treated B. subtilis. The frequently prescribed antibiotic trimethoprim causes purine depletion in B. subtilis, which can be complemented by supplementing purines to the medium. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Mutants of Venturia ineaqualis (Cook) Wint. apple scar resistant to fungicides

International Nuclear Information System (INIS)

Bedianashvili, Ts.V.; D'yakov, Yu.T.

1987-01-01

Mutants of apple scab resistant to zineb and bayleton fungicides have been obtained upon action of UV irradiation and nitrosome-thylurea. Using tetrade analysis, two zineb resistence genes have been found. The mutations are pleiotropic and lead to increase in resistance to other fungicides, decrease in growth rate on artificial media, increase in spore size, sporulation, and aggressiveness, decrease in competitiveness at in vitro growth. The resistance is supposed to be determined by decrease in membrane permeability for fungicides

Biological activity of triazole fungicides towards Botrytis cinerea

OpenAIRE

Stehmann, C.

1995-01-01

Botrytis cinerea Pers. ex Fr., the causal agent of grey mould, is one of the most ubiquitous plant pathogens. The fungus is of high economic importance in various major crops and during transport and storage of agricultural products. Protectant fungicides such as chlorothalonil, dichlofluanid, folpet or thiram are widely used for disease control. Since their introduction in the 1960S/1970s, systemic fungicides such as the benzimidazoles or dicarboximides have bee...

In vitro response of phaeoramularia angolensis to commonly used fungicides in Kenya

International Nuclear Information System (INIS)

Juma, I.M.; Siboe, M.

1996-01-01

The leaf and fruit spot disease of citrus spp. caused by the fungus Phaeoramularia angolensis Kirk is new and epidemic in Kenya, with a 100% crop yield loss. Poor response to fungicide application led to the suspicion that the fungus was resistant to conventional fungicides, hence the difficulties experienced in its control. Therefore the study was carried out to establish wether P.angolensis isolates from Western Kenya were screened for resistance. The following fungicides were used: copper fungicides(Cupric hydroxide 50% WP or kocide 101 and copper oxychloride 50% WP), Mancozeb 70% WP (Dithane M45)and Propineb 80% WPC (Antracol). Mancozeb 70% WP and Propineb were the most effective with LD-5-0 at 0.03 ppm and 0.25 ppm respectively. Copper fungicide LD-5-0 was above 3000 ppm (current manufacturers' recommended dosage is 7,500 ppm and 6,900 ppm for kocide 101 and copper oxychloride respectively). There was no obvious evidence of resistance. The fungi- static characteristics of copper fungicides and the application of wrong dosage and timing could be the reason for the difficulties experienced in the control of the disease. (author) 14 refs., 2 tables, 1 graph

Phytotoxicity: An Overview of the Physiological Responses of Plants Exposed to Fungicides

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Maria Celeste Dias

2012-01-01

Full Text Available In the last decades, the use of fungicides in agriculture for fungi diseases control has become crucial. Fungicide research has produced a diverse range of products with novel modes of action. However, the extensive use of these compounds in the agriculture system raises public concern because of the harmful potential of such substances in the environment and human health. Moreover, the phytotoxic effects of some fungicides are already recognized but little is known about the impact of these compounds on the photosynthetic apparatus. This paper presents a comprehensive overview of the literature considering different classes of fungicides and their effects on plant physiology, with particular emphasis on photosynthesis.

Management of Anthracnose in Soybean using Fungicide

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Subash Subedi

2015-12-01

Full Text Available Experiments on soybean (Glycine max L. Meril were carried out aiming to control anthracnose (pod blight caused by fungus, Colletotrichum truncatum with five treatments represented by different fungicidal sprays against control receiving no spray with three replicates of each under field conditions during two consecutive years from 2012 to 2013. In 2012, the higher Percent Disease Control (PDC and Percent Yield Increase (PYI were estimated in plot treated with SAAF (Carbendazim 12% + Mancozeb 63% followed by Mancozeb fungicides. The mean Pod Infection (PI was low in plots treated with SAAF followed by Mancozeb. Almost similar trends of disease control were observed in 2013. The lower Percent Disease Index (PDI was 46.25% and mean PI was 29.67% with higher yield value of 2431.25 kg/ha obtained from the plots sprayed with SAAF then by Mancozeb. The results showed that, the combined treatment with fungicides, SAAF followed by Mancozeb were effective to control anthracnose or pod blight disease of soybean to increase the yield.

A new mechanism for reduced sensitivity to demethylation-inhibitor fungicides in the fungal banana black Sigatoka pathogen Pseudocercospora fijiensis.

Science.gov (United States)

Diaz-Trujillo, Caucasella; Chong, Pablo; Stergiopoulos, Ioannis; Cordovez, Viviane; Guzman, Mauricio; De Wit, Pierre J G M; Meijer, Harold J G; Scalliet, Gabriel; Sierotzki, Helge; Lilia Peralta, Esther; Arango Isaza, Rafael E; Kema, Gerrit H J

2017-11-04

The Dothideomycete Pseudocercospora fijiensis, previously Mycosphaerella fijiensis, is the causal agent of black Sigatoka, one of the most destructive diseases of bananas and plantains. Disease management depends on fungicide applications, with a major contribution from sterol demethylation-inhibitors (DMIs). The continued use of DMIs places considerable selection pressure on natural P. fijiensis populations, enabling the selection of novel genotypes with reduced sensitivity. The hitherto explanatory mechanism for this reduced sensitivity was the presence of non-synonymous point mutations in the target gene Pfcyp51, encoding the sterol 14α-demethylase enzyme. Here, we demonstrate a second mechanism involved in DMI sensitivity of P. fijiensis. We identified a 19-bp element in the wild-type (wt) Pfcyp51 promoter that concatenates in strains with reduced DMI sensitivity. A polymerase chain reaction (PCR) assay identified up to six Pfcyp51 promoter repeats in four field populations of P. fijiensis in Costa Rica. We used transformation experiments to swap the wt promoter of a sensitive field isolate with a promoter from a strain with reduced DMI sensitivity that comprised multiple insertions. Comparative in vivo phenotyping showed a functional and proportional up-regulation of Pfcyp51, which consequently decreased DMI sensitivity. Our data demonstrate that point mutations in the Pfcyp51 coding domain, as well as promoter inserts, contribute to the reduced DMI sensitivity of P. fijiensis. These results provide new insights into the importance of the appropriate use of DMIs and the need for the discovery of new molecules for black Sigatoka management. © 2017 The Authors. Molecular Plant Pathology published by British Society for Plant Pathology and John Wiley & Sons Ltd.

Spread of Botrytis cinerea Strains with Multiple Fungicide Resistance in German Horticulture.

Science.gov (United States)

Rupp, Sabrina; Weber, Roland W S; Rieger, Daniel; Detzel, Peter; Hahn, Matthias

2016-01-01

Botrytis cinerea is a major plant pathogen, causing gray mold rot in a variety of cultures. Repeated fungicide applications are common but have resulted in the development of fungal populations with resistance to one or more fungicides. In this study, we have monitored fungicide resistance frequencies and the occurrence of multiple resistance in Botrytis isolates from raspberries, strawberries, grapes, stone fruits and ornamental flowers in Germany in 2010 to 2015. High frequencies of resistance to all classes of botryticides was common in all cultures, and isolates with multiple fungicide resistance represented a major part of the populations. A monitoring in a raspberry field over six seasons revealed a continuous increase in resistance frequencies and the emergence of multiresistant Botrytis strains. In a cherry orchard and a vineyard, evidence of the immigration of multiresistant strains from the outside was obtained. Inoculation experiments with fungicide-treated leaves in the laboratory and with strawberry plants cultivated in the greenhouse or outdoors revealed a nearly complete loss of fungicide efficacy against multiresistant strains. B. cinerea field strains carrying multiple resistance mutations against all classes of site-specific fungicides were found to show similar fitness as sensitive field strains under laboratory conditions, based on their vegetative growth, reproduction, stress resistance, virulence and competitiveness in mixed infection experiments. Our data indicate an alarming increase in the occurrence of multiresistance in B. cinerea populations from different cultures, which presents a major threat to the chemical control of gray mold.

[Effect of five fungicides on growth of Glycyrrhiza uralensis and efficiency of mycorrhizal symbiosis].

Science.gov (United States)

Li, Peng-ying; Yang, Guang; Zhou, Xiu-teng; Zhou, Liane-yun; Shao, Ai-juan; Chen, Mei-lan

2015-12-01

In order to obtain the fungicides with minimal impact on efficiency of mycorrhizal symbiosis, the effect of five fungicides including polyoxins, jinggangmycins, thiophanate methylate, chlorothalonil and carbendazim on the growth of medicinal plant and efficiency of mycorrhizal symbiosis were studied. Pot cultured Glycyrrhiza uralensis was treated with different fungicides with the concentration that commonly used in the field. 60 d after treated with fungicides, infection rate, infection density, biomass indexes, photosyn- thetic index and the content of active component were measured. Experimental results showed that carbendazim had the strongest inhibition on mycorrhizal symbiosis effect. Carbendazim significantly inhibited the mycorrhizal infection rate, significantly suppressed the actual photosynthetic efficiency of G. uralensis and the most indicators of biomass. Polyoxins showed the lowest inhibiting affection. Polyoxins had no significant effect on mycorrhizal infection rate, the actual photosynthetic efficiency of G. uralensis and the most indicators of biomass. The other three fungicides also had an inhibitory effect on efficiency of mycorrhizal symbiosis, and the inhibition degrees were all between polyoxins's and carbendazim's. The author considered that fungicide's inhibition degree on mycorrhizal effect might be related with the species of fungicides, so the author suggested that the farmer should try to choose bio-fungicides like polyoxins.

In vivo sensitivity of Phakopsora pachyrhizi to DMI and QoI fungicides

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Erlei Melo Reis

2015-03-01

Full Text Available In in vivo experiments the sensitivity of 18 isolates of Phakopsora pachyrhizi from several regions of Brazil to IDM fungicides (cyproconazole, epoxiconazole and tebuconazole and an IQE (pyraclostrobin were evaluated. The assessments were based on leaflet uredia density. Inhibitory concentration (IC50 and sensitivity reduction factor were determined for all fungicide x strain interactions. Tebuconazole sensitivity reduction was detected for most fungus isolates. In contrast, there was no fungicide shift in sensitivity of the fungus to pyraclostrobin. We conclude that the control failure of soybean rust found in some farms is due to the reduced sensitivity of the fungus to the IDM fungicide and that it remains sensitive to pyraclostrobin.

Coating with fungicide and different doses of fertilizer in vinhatico ...

African Journals Online (AJOL)

Thus, the aim of this study was to evaluate and identify the physical and physiological quality of mahogany seeds that are coated with fertilizer and fungicide. The treatments were: seed coating with sand + lime + fungicide with different doses of fertilizers. The seeds were evaluated in the laboratory and in a greenhouse.

Effectiveness of Fungicide on Soybean Rust in the Southeastern United States: A Meta-Analysis

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Mary Delaney

2018-05-01

Full Text Available Soybean rust (SBR, caused by the fungus Phakopsora pachyrhizi Sydow, has been of concern to soybean (Glycine max Merrill growers in the southern United States since its introduction in 2004. As this fungus develops, pustules become numerous on the underside of leaves, which then turn yellow and drop prematurely, resulting in fewer pods, and poorly developed seeds. Our objective was to evaluate the efficacy of fungicide use in controlling SBR by conducting a meta-analysis of 61 published and unpublished trials across the southern United States from 2004 to 2014. We analyzed fungicide efficacy based on factors such as specific classes of fungicide, active ingredients, number of fungicide applications, target growth stage upon initial application, level of disease pressure, and year of the study. Fungicides significantly increased yield and 100-seed weight and decreased the severity of SBR. The means of SBR severity, yield, and 100-seed weight in fungicide-treated plants were 9% (95% confidence interval: 2%, 21%, 128% (121%, 135%, and 121% (116%, 128%, respectively, of those calculated in the control plants. By using meta-analysis to analyze fungicide efficacy across multiple field trials, we were able to determine that one application of a strobilurin fungicide when plants were either beginning pod development (R3 or developing seeds (R5 was the most cost-effective approach to controlling SBR and increasing 100-seed weight.

Nanosulfur: A Potent Fungicide Against Food Pathogen, Aspergillus niger

International Nuclear Information System (INIS)

Choudhury, Samrat Roy; Goswami, Arunava; Nair, Kishore K.; Kumar, Rajesh; Gopal, Madhuban; Devakumar, C.; Gogoi, Robin; Srivastava, Chitra; Subhramanyam, B. S.

2010-01-01

Elemental sulfur (S 0 ), man's oldest eco-friendly fungicide for curing fungal infections in plants and animals, is registered in India as a non-systemic and contact fungicide. However due to its high volume requirement, Indian agrochemical industry and farmers could not effectively use this product till date. We hypothesize that intelligent nanoscience applications might increase the visibility of nanosulfur in Indian agriculture as a potent and eco-safe fungicide. Sulfur nanoparticles (NPs) were synthesized bottom-up via a liquid synthesis method with average particle size in the range of 50-80 nm and the shapes of the NPs were spherical. A comparative study of elemental and nano-sulfur produced has been tested against facultative fungal food pathogen, Aspergillus niger. Results showed that nanosulfur is more efficacious than its elemental form.

Nanosulfur: A Potent Fungicide Against Food Pathogen, Aspergillus niger

Science.gov (United States)

Choudhury, Samrat Roy; Nair, Kishore K.; Kumar, Rajesh; Gogoi, Robin; Srivastava, Chitra; Gopal, Madhuban; Subhramanyam, B. S.; devakumar, C.; Goswami, Arunava

2010-10-01

Elemental sulfur (S0), man's oldest eco-friendly fungicide for curing fungal infections in plants and animals, is registered in India as a non-systemic and contact fungicide. However due to its high volume requirement, Indian agrochemical industry and farmers could not effectively use this product till date. We hypothesize that intelligent nanoscience applications might increase the visibility of nanosulfur in Indian agriculture as a potent and eco-safe fungicide. Sulfur nanoparticles (NPs) were synthesized bottom-up via a liquid synthesis method with average particle size in the range of 50-80 nm and the shapes of the NPs were spherical. A comparative study of elemental and nano-sulfur produced has been tested against facultative fungal food pathogen, Aspergillus niger. Results showed that nanosulfur is more efficacious than its elemental form.

The influence of fungicides on the growth of Trichoderma asperellum.

Science.gov (United States)

De Schutter, B; Aerts, R; Rombouts, L

2002-01-01

Numbers of strains of Trichoderma asperellum are known as biological control agents of certain root pathogens of tomato (Lycopersicon esculentum). The restricted use of fungicides is sometimes useful in combination with these biological control agents. Therefore some experiments were conducted to evaluate the growth of T. asperellum in the presence of fungicides as Previcur (active substance propamocarb) and Sumico (with the active substance carbendazim and diethofencarb). The influence of these fungicides was first examined in laboratory conditions. The fungus was brought on a potato dextrose agar where the fungicides Previcur, Sumico and carbendazim were added in a concentration of 0.1x, 1x and 10x the recommended dose. The growth of T. asperellum was totally inhibited by the three Sumico and carbendazim concentrations. T. asperellum knew a small but significant decrease of growth when the 10x dose of Previcur was added. Afterwards the influence of these fungicides on the fungus was tested in field conditions in the greenhouse. The fungus was applied to the roots of the tomato plant, which was grown on a rockwool medium. Previcur and Sumico were submitted to the plants using the normal procedure. The results of the tests showed that in field conditions there was no effect of the fungicide treatment on the presence of the fungus, although the laboratory tests showed the opposite for Sumico. To explain this contradiction two other experiments were conducted to follow the migration of the Sumico after treatment. A residue analysis showed that the highest concentration of Sumico was detected in the rockwool medium, and some residues were found in the drain water and the stems. Even with a 100x recommended dose of Sumico the fungus was still present the day after the treatment.

Efficacy of Strobilurin-related and Multi-site Fungicide Mixtures Against Apple Scab

Directory of Open Access Journals (Sweden)

Emil Rekanović

2007-01-01

Full Text Available The efficacy of several fungicide mixtures in controlling Venturia inaequalis in apple was evaluated in field trials. The efficacies of Flint Plus (trifloxystrobin + captan and Tercel (pyraclostrobin+ dithianon in comparison with standard fungicides Zato 50-WG (trifloxystrobin and Stroby + Delan (kresoxim-methyl + dithianon were tested in the localities Mihajlovac, Radmilovac and Landol in 2004 and 2005. Both tested fungicides exhibited high efficacy in controlling apple scab. There were significant differencies in the efficacies of Flint Plus (91.3-98.5% and Zato 50-WG (68.2% and 78.4%; and Tercel (88.7-93.5% and Stroby + Delan (77.9% and 82.1%. Our experiments showed that the investigated fungicide mixtures arehighly effective against V. inaqeulais, even under high disease pressure.

Assessment of spent mushroom substrate as sorbent of fungicides: influence of sorbent and sorbate properties.

Science.gov (United States)

Marín-Benito, Jesús M; Rodríguez-Cruz, M Sonia; Andrades, M Soledad; Sánchez-Martín, María J

2012-01-01

The capacity of spent mushroom substrate (SMS) as a sorbent of fungicides was evaluated for its possible use in regulating pesticide mobility in the environment. The sorption studies involved four different SMS types in terms of nature and treatment and eight fungicides selected as representative compounds from different chemical groups. Nonlinear sorption isotherms were observed for all SMS-fungicide combinations. The highest sorption was obtained by composted SMS from Agaricus bisporus cultivation. A significant negative and positive correlation was obtained between the K(OC) sorption constants and the polarity index values of sorbents and the K(OW) of fungicides, respectively. The statistic revealed that more than 77% of the variability in the K(OW) could be explained considering these properties jointly. The other properties of both the sorbent (total carbon, dissolved organic carbon, or pH) and the sorbate (water solubility) were nonsignificant. The hysteresis values for cyprodinil (log K(OW)= 4) were for all the sorbents much higher (>3) than for other fungicides. This was consistent with the remaining sorption after desorption considered as an indicator of the sorption efficiency of SMS for fungicides. Changes in the absorption bands of fungicides sorbed by SMS observed by FTIR permitted establishing the interaction mechanism of fungicides with SMS. The findings of this work provide evidence for the potential capacity of SMS as a sorbent of fungicides and the low desorption observed especially for some fungicides, although they suggest that more stabilized or humified organic substrates should be produced to enhance their efficiency in environmental applications. Copyright © by the American Society of Agronomy, Crop Science Society of America, and Soil Science Society of America, Inc.

Reduced fungicide doses in cereals: Which parameters to consider?

DEFF Research Database (Denmark)

Jørgensen, Lise Nistrup

2015-01-01

dose. In spring barley the economically optimum input can vary from 0-2 treatments with a total fungicide use equivalent to 0.25 to 0.5 times the recommended dose. Applying reducing rates should never result in significant inferior control and economical yield losses. A recent review concluded......, the pathogen, disease pressure and timing of treatments. Certain diseases are known to require higher input (40- 75% rates) for achieving satisfactory control – this is the case for Septoria leaf blight, Rhynchosporium net blotch and Fusarium head blight, whereas most rust diseases generally have been found...... on well-established disease attack. Rates also have to be adjusted according to canopy structures. Early timing on a small canopy requires less fungicide than a full canopy around heading. The knowledge gathered concerning fungicide rates has led to great focus on the importance of optimizing timing...

Soilless plant growth media influence the efficacy of phytohormones and phytohormone inhibitors.

Science.gov (United States)

Best, Norman B; Hartwig, Thomas; Budka, Joshua S; Bishop, Brandon J; Brown, Elliot; Potluri, Devi P V; Cooper, Bruce R; Premachandra, Gnanasiri S; Johnston, Cliff T; Schulz, Burkhard

2014-01-01

Plant growth regulators, such as hormones and their respective biosynthesis inhibitors, are effective tools to elucidate the physiological function of phytohormones in plants. A problem of chemical treatments, however, is the potential for interaction of the active compound with the growth media substrate. We studied the interaction and efficacy of propiconazole, a potent and specific inhibitor of brassinosteroid biosynthesis, with common soilless greenhouse growth media for rice, sorghum, and maize. Many of the tested growth media interacted with propiconazole reducing its efficacy up to a hundred fold. To determine the molecular interaction of inhibitors with media substrates, Fourier Transform Infrared Spectroscopy and sorption isotherm analysis was applied. While mica clay substrates absorbed up to 1.3 mg of propiconazole per g substrate, calcined clays bound up to 12 mg of propiconazole per g substrate. The efficacy of the gibberellic acid biosynthesis inhibitor, uniconazole, and the most active brassinosteroid, brassinolide, was impacted similarly by the respective substrates. Conversely, gibberellic acid showed no distinct growth response in different media. Our results suggest that the reduction in efficacy of propiconazole, uniconazole, and brassinolide in bioassays when grown in calcined clay is caused by hydrophobic interactions between the plant growth regulators and the growth media. This was further confirmed by experiments using methanol-water solvent mixes with higher hydrophobicity values, which reduce the interaction of propiconazole and calcined clay.

Insect P450 inhibitors and insecticides: challenges and opportunities.

Science.gov (United States)

Feyereisen, René

2015-06-01

P450 enzymes are encoded by a large number of genes in insects, often over a hundred. They play important roles in insecticide metabolism and resistance, and growing numbers of P450 enzymes are now known to catalyse important physiological reactions, such as hormone metabolism or cuticular hydrocarbon synthesis. Ways to inhibit P450 enzymes specifically or less specifically are well understood, as P450 inhibitors are found as drugs, as fungicides, as plant growth regulators and as insecticide synergists. Yet there are no P450 inhibitors as insecticides on the market. As new modes of action are constantly needed to support insecticide resistance management, P450 inhibitors should be considered because of their high potential for insect selectivity, their well-known mechanisms of action and the increasing ease of rational design and testing. © 2014 Society of Chemical Industry.

Toxicity, sublethal effects, and potential modes of action of select fungicides on freshwater fish and invertebrates

Science.gov (United States)

Elskus, Adria A.

2012-01-01

Despite decades of agricultural and urban use of fungicides and widespread detection of these pesticides in surface waters, relatively few data are available on the effects of fungicides on fish and invertebrates in the aquatic environment. Nine fungicides are reviewed in this report: azoxystrobin, boscalid, chlorothalonil, fludioxonil, myclobutanil, fenarimol, pyraclostrobin, pyrimethanil, and zoxamide. These fungicides were identified as emerging chemicals of concern because of their high or increasing global use rates, detection frequency in surface waters, or likely persistence in the environment. A review of the literature revealed significant sublethal effects of fungicides on fish, aquatic invertebrates, and ecosystems, including zooplankton and fish reproduction, fish immune function, zooplankton community composition, metabolic enzymes, and ecosystem processes, such as leaf decomposition in streams, among other biological effects. Some of these effects can occur at fungicide concentrations well below single-species acute lethality values (48- or 96-hour concentration that effects a response in 50 percent of the organisms, that is, effective concentration killing 50 percent of the organisms in 48 or 96 hours) and chronic sublethal values (for example, 21-day no observed adverse effects concentration), indicating that single-species toxicity values may dramatically underestimate the toxic potency of some fungicides. Fungicide modes of toxic action in fungi can sometimes reflect the biochemical and (or) physiological effects of fungicides observed in vertebrates and invertebrates; however, far more studies are needed to explore the potential to predict effects in nontarget organisms based on specific fungicide modes of toxic action. Fungicides can also have additive and (or) synergistic effects when used with other fungicides and insecticides, highlighting the need to study pesticide mixtures that occur in surface waters. For fungicides that partition to

Differences in sensitivity between earthworms and enchytraeids exposed to two commercial fungicides.

Science.gov (United States)

Bart, Sylvain; Laurent, Céline; Péry, Alexandre R R; Mougin, Christian; Pelosi, Céline

2017-06-01

The use of pesticides in crop fields may have negative effects on soil Oligochaeta Annelida, i.e., earthworms and enchytraeids, and thus affect soil quality. The aim of this study was to assess the effects of two commercial fungicide formulations on the earthworm Aporrectodea caliginosa and the enchytraeid Enchytraeus albidus in a natural soil. The fungicides were Cuprafor micro® (copper oxychloride), commonly used in organic farming, and Swing Gold® (epoxiconazole and dimoxystrobin), a synthetic fungicide widely used in conventional farming to protect cereal crops. Laboratory experiments were used to assess the survival, biomass loss and avoidance behaviour. No lethal effect was observed following exposure to the copper fungicide for 14 days, even at 5000mgkg -1 of copper, i.e. 650 times the recommended dose (RD). However, a significant decrease in biomass was observed from 50mgkg -1 of copper (6.5 times the RD) for A. caliginosa and at 5000mgkg -1 of copper (650 times the RD) for E. albidus. These sublethal effects suggest that a longer period of exposure would probably have led to lethal effects. The EC50 avoidance for the copper fungicide was estimated to be 51.2mgkg -1 of copper (6.7 times the RD) for A. caliginosa, and 393mgkg -1 of copper (51 times the RD) for E. albidus. For the Swing Gold® fungicide, the estimated LC50 was 7.0 10 -3 mLkg -1 (6.3 times the RD) for A. caliginosa and 12.7 10 -3 mLkg -1 (11.0 times the RD) for E. albidus. No effect on biomass or avoidance was observed at sublethal concentrations of this synthetic fungicide. It was concluded that enchytraeids were less sensitive than earthworms to the two commercial fungicides in terms of mortality, biomass loss and avoidance behaviour. Therefore we discuss the different strategies possibly used by the two Oligochaeta species to cope with the presence of the pesticides were discussed, along with the potential consequences on the soil functions. Copyright © 2017 Elsevier Inc. All rights

Evaluating Susceptibility to Commercial Fungicide of Endophytic Fungi Isolated from Roses (Rosa hybrida

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Ingrid Carolina Corredor Perilla

2007-01-01

Full Text Available Fungal endophytes have shown their potential as biocontrol agents; however, their application in commercial fields remains limited. Continuously applying fungicides to crops (specifically to roses may have harmful effects on endophyte growth. Endophytic fungi were isolated from R. hybrida and their susceptibility to fungicides regularly used for controlling important pathogens was analysed. This was performed in vitro, mixing several fungicide concentrations with standard medium for fungal endophytes; growth inhibition was then measured. The susceptibility of Botrytis cinerea (3015 strain, one of the most important pathogens affecting roses in Colombia, was also assessed using the same protocols. Active ingredients, such as boscalid, captan, iprodione and pyrimethanyl, showed susceptibility ranging from not sensitive (³73.75% to regularly sensitive (³48.75% - <61.25% for 45.45% of the fungal endophytes assessed. Endophytic fungi were highly susceptible to fungicides such as pyrimethanyl, carboxin plus thiram, fludioxonyl plus ciprodinyl and prochloraz. B. cinerea (3015 strain presented high susceptibility (<23.75% to fungicides such as pyrimethanyl, carboxin and thiram, fludioxonil and ciprodinyl, prochloraz. Although B. cinerea showed the greatest growth in controls, the endophytic fungi being assessed grew better in different media with fungicides. The results revealed some of these fungal endophytes’ potential for integrated pest management (IPM in roses in Colombia (3002, 3003, 3004, 3005 and 3006 strains, taking into account correct application time, application frequency and both fungal endophyte and fungicide dosage which may greatly limit fungal endophyte growth.

Induced effect of Ca2+ on dalesconols A and B biosynthesis in the culture of Daldinia eschscholzii via calcium/calmodulin signaling.

Science.gov (United States)

Lu, Yanhua; Pan, Zhenghua; Tao, Jun; An, Faliang

2018-02-01

Dalesconols (dalesconols A and B) were isolated from Daldinia eschscholzii and have remarkable immunosuppressive activity. In this study, the response of fungal growth, intra- and extracellular Ca 2+ , and dalesconols production after CaCl 2 addition were reported for the first time. After supplementation with 5 mM Ca 2+ at 24 h, dalesconols production reached 84.33 mg/L, which resulted in a 1.57-fold enhancement compared to the control. The key role of calcium/calmodulin signaling in dalesconols biosynthesis was confirmed by treatment with Ca 2+ channel and calmodulin inhibitors. The transcriptional levels of dalesconols biosynthetic genes were up-regulated after CaCl 2 addition and down-regulated after inhibitors were added. The results demonstrated that Ca 2+ addition induces dalesconols biosynthesis through up-regulation of dalesconols biosynthesis genes via regulation of calcium/calmodulin signaling. This study provided an efficient strategy for improving dalesconols production and would facilitate further research on the biosynthesis and regulation of dalesconols. Copyright © 2017 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

Assessing the impact of fungicide enostroburin application on bacterial community in wheat phyllosphere.

Science.gov (United States)

Gu, Likun; Bai, Zhihui; Jin, Bo; Hu, Qing; Wang, Huili; Zhuang, Guoqiang; Zhang, Hongxun

2010-01-01

Fungicides have been used extensively for controlling fungal pathogens of plants. However, little is known regarding the effects that fungicides upon the indigenous bacterial communities within the plant phyllosphere. The aims of this study were to assess the impact of fungicide enostroburin upon bacterial communities in wheat phyllosphere. Culture-independent methodologies of 16S rDNA clone library and 16S rDNA directed polymerase chain reaction with denaturing gradient gel electrophoresis (PCR-DGGE) were used for monitoring the change of bacterial community. The 16S rDNA clone library and PCR-DGGE analysis both confirmed the microbial community of wheat plant phyllosphere were predominantly of the gamma-Proteobacteria phyla. Results from PCR-DGGE analysis indicated a significant change in bacterial community structure within the phyllosphere following fungicide enostroburin application. Bands sequenced within control cultures were predominantly of Pseudomonas genus, but those bands sequenced in the treated samples were predominantly strains of Pantoea genus and Pseudomonas genus. Of interest was the appearance of two DGGE bands following fungicide treatment, one of which had sequence similarities (98%) to Pantoea sp. which might be a competitor of plant pathogens. This study revealed the wheat phyllosphere bacterial community composition and a shift in the bacterial community following fungicide enostroburin application.

Subnanomolar Inhibitor of Cytochrome bc1 Complex Designed via Optimizing Interaction with Conformationally Flexible Residues

Science.gov (United States)

Zhao, Pei-Liang; Wang, Le; Zhu, Xiao-Lei; Huang, Xiaoqin; Zhan, Chang-Guo; Wu, Jia-Wei; Yang, Guang-Fu

2009-01-01

Cytochrome bc1 complex (EC 1.10.2.2, bc1), an essential component of the cellular respiratory chain and the photosynthetic apparatus in photosynthetic bacteria, has been identified as a promising target for new drugs and agricultural fungicides. X-ray diffraction structures of the free bc1 complex and its complexes with various inhibitors revealed that the phenyl group of Phe274 in the binding pocket exhibited significant conformational flexibility upon different inhibitors binding to optimize respective π-π interactions, whereas the side chains of other hydrophobic residues showed conformational stability. Therefore, in the present study, a strategy of optimizing the π-π interaction with conformationally flexible residues was proposed to design and discover new bc1 inhibitors with a higher potency. Eight new compounds were designed and synthesized, among which compound 5c with a Ki value of 570 pM was identified as the most promising drug or fungicide candidate, significantly more potent than the commercially available bc1 inhibitors including azoxystrobin (AZ), kresoxim-methyl (KM), and pyraclostrobin (PY). To our knowledge, this is the first bc1 inhibitor discovered from structure-based design with a potency of subnanomolar Ki value. For all of the compounds synthesized and assayed, the calculated binding free energies correlated reasonably well with the binding free energies derived from the experimental Ki values with a correlation coefficient of r2 = 0.89. The further inhibitory kinetics studies revealed that compound 5c is a non-competitive inhibitor with respect to substrate cytochrome c, but is a competitive inhibitor with respect to substrate ubiquinol. Due to its subnanomolar Ki potency and slow dissociation rate constant (k−0 = 0.00358 s−1), compound 5c could be used as a specific probe for further elucidation of the mechanism of bc1 function and as a new lead compound for future drug discovery. PMID:19928849

Estimation of sorption coefficients for fungicides in soil and turfgrass thatch

Energy Technology Data Exchange (ETDEWEB)

Dell, C.J.; Throssell, C.S.; Bischoff, M. [Purdue Univ., West Lafayette, IN (United States)] [and others

1994-01-01

Environmental fates of turf-applied fungicides are not well understood. The role of thatch as a sorptive surface for fungicides has not been evaluated. Thatch may decrease mobility of fungi and decrease their potential to be transported off-site. Batch type sorption studies were conducted to determine sorption coefficients (K{sub f}) for the fungicides triadimefon, [1-(4-chlorophenoxy)-3,3-dimethyl 1-1(1H-1,2,4- triazol-l-g-l) butanone], vinclozolin [3-(3,5-dichlorophenyl)-5-methyl- 5-vinyl-1,3-oxazolidine-2,4-dione], and chloroneb (1,4-dichloro-2,5-dimethoxybenzone) in thatch and in the underlying soil.

Consequences of co-applying insecticides and fungicides for managing Thrips tabaci (Thysanoptera: Thripidae) on onion.

Science.gov (United States)

Nault, Brian A; Hsu, Cynthia L; Hoepting, Christine A

2013-07-01

Insecticides and fungicides are commonly co-applied in a tank mix to protect onions from onion thrips, Thrips tabaci Lindeman, and foliar pathogens. Co-applications reduce production costs, but past research shows that an insecticide's performance can be reduced when co-applied with a fungicide. An evaluation was made of the effects of co-applying spinetoram, abamectin and spirotetramat with commonly used fungicides, with and without the addition of a penetrating surfactant, on onion thrips control in onion fields. Co-applications of insecticides with chlorothalonil fungicides reduced thrips control by 25-48% compared with control levels provided by the insecticides alone in three of five trials. Inclusion of a penetrating surfactant at recommended rates with the insecticide and chlorothalonil fungicide did not consistently overcome this problem. Co-applications of insecticides with other fungicides did not interfere with thrips control. Co-applications of pesticides targeting multiple organisms should be examined closely to ensure that control of each organism is not compromised. To manage onion thrips in onion most effectively, insecticides should be applied with a penetrating surfactant, and should be applied separately from chlorothalonil fungicides. © 2012 Society of Chemical Industry.

Chemical management in fungicide sensitivity of Mycosphaerella fijiensis collected from banana fields in México.

Science.gov (United States)

Aguilar-Barragan, Alejandra; García-Torres, Ana Elisa; Odriozola-Casas, Olga; Macedo-Raygoza, Gloria; Ogura, Tetsuya; Manzo-Sánchez, Gilberto; James, Andrew C; Islas-Flores, Ignacio; Beltrán-García, Miguel J

2014-01-01

The chemical management of the black leaf streak disease in banana caused by Mycosphaerella fijiensis (Morelet) requires numerous applications of fungicides per year. However this has led to fungicide resistance in the field. The present study evaluated the activities of six fungicides against the mycelial growth by determination of EC50 values of strains collected from fields with different fungicide management programs: Rustic management (RM) without applications and Intensive management (IM) more than 25 fungicide application/year. Results showed a decreased sensitivity to all fungicides in isolates collected from IM. Means of EC50 values in mg L(-1) for RM and IM were: 13.25 ± 18.24 and 51.58 ± 46.14 for azoxystrobin, 81.40 ± 56.50 and 1.8575 ± 2.11 for carbendazim, 1.225 ± 0.945 and 10.01 ± 8.55 for propiconazole, 220 ± 67.66 vs. 368 ± 62.76 for vinclozolin, 9.862 ± 3.24 and 54.5 ± 21.08 for fludioxonil, 49.2125 ± 34.11 and 112.25 ± 51.20 for mancozeb. A molecular analysis for β-tubulin revealed a mutation at codon 198 in these strains having an EC50 greater than 10 mg L(-1) for carbendazim. Our data indicate a consistency between fungicide resistance and intensive chemical management in banana fields, however indicative values for resistance were also found in strains collected from rustic fields, suggesting that proximity among fields may be causing a fungus interchange, where rustic fields are breeding grounds for development of resistant strains. Urgent actions are required in order to avoid fungicide resistance in Mexican populations of M. fijiensis due to fungicide management practices.

Population density of Beauveria bassiana in soil under the action of fungicides and native microbial populations

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Flávia Barbosa Soares

2017-08-01

Full Text Available This study investigated whether populations of naturally-occurring soil bacteria, fungi and actinomycetes influence the effect of fungicides on the survival and growth of Beauveria bassiana. The toxicity of methyl thiophanate, pyraclostrobin, mancozeb and copper oxychloride at the recommended doses was analyzed in culture medium and in soil inoculated with fungus at various time points after addition of fungicides. All fungicides completely inhibited the growth and sporulation of B. bassiana in the culture medium. The fungicides were less toxic in soil, emphasizing the action of the microbial populations, which interfered with the toxic effects of these products to the fungus. Actinomycetes had the greatest influence on the entomopathogen, inhibiting it or degrading the fungicides to contribute to the survival and growth of B. bassiana in soil. Native populations of fungi and bacteria had a smaller influence on the population density of B. bassiana and the action of fungicides towards entomopathogen. The toxic effect of the fungicides was greater when added to the soil one hour before or after inoculation than at 48h after inoculation.

Comparative efficacy of different fungicides against fusarium wilt of chickpea (cicer arietinum l.)

International Nuclear Information System (INIS)

Maitlo, S.A.

2014-01-01

Fusarium wilt caused by Fusarium oxysporum f. sp. ciceris (Foc) is the most serious and widespread disease of chickpea, causing a 100% loss under favorable conditions. Fourteen fungicides were evaluated against wilt pathogen In vitro with five different concentrations ranging from 1-10000 ppm. Among these only Carbendazim and Thiophanate-methyl was found as the most effective at all used concentrations. Other fungicides like Aliette, Nativo, Hombre-excel and Dividend star were found to be moderately effective. Whereas, remaining fungicides were ineffective against the targeted pathogen. Generally, a positive co-relation was observed between increasing concentrations of the tested fungicides and inhibition of Foc. Based on In vitro results Carbendazim, Thiophanate-methyl, Aliette, Dividend-star, Hombre-excel, Score and Nativo were selected for pot and field experiments. The higher concentrations of the few fungicides completely inhibited the pathogen as well as found to be phytotoxic and suppressed the plant growth while lower concentrations promoted the growth of chickpea plants. On over all bases, the Carbendazim and Thiophanate-methyl, followed by Aliette and Nativo were more effective in reducing the impact of pathogen as well as enhancing the plant growth in greenhouse experiment. Under field conditions, all fungicides except Score remarkably decreased the disease development and subsequently increased the plant growth as well as grain yield as compared to untreated plants. (author)

Additive and synergistic antiandrogenic activities of mixtures of azol fungicides and vinclozolin.

Science.gov (United States)

Christen, Verena; Crettaz, Pierre; Fent, Karl

2014-09-15

Many pesticides including pyrethroids and azole fungicides are suspected to have an endocrine disrupting property. At present, the joint activity of compound mixtures is only marginally known. Here we tested the hypothesis that the antiandrogenic activity of mixtures of azole fungicides can be predicted by the concentration addition (CA) model. The antiandrogenic activity was assessed in MDA-kb2 cells. Following assessing single compounds activities mixtures of azole fungicides and vinclozolin were investigated. Interactions were analyzed by direct comparison between experimental and estimated dose-response curves assuming CA, followed by an analysis by the isobole method and the toxic unit approach. The antiandrogenic activity of pyrethroids deltamethrin, cypermethrin, fenvalerate and permethrin was weak, while the azole fungicides tebuconazole, propiconazole, epoxiconazole, econazole and vinclozolin exhibited strong antiandrogenic activity. Ten binary and one ternary mixture combinations of five antiandrogenic fungicides were assessed at equi-effective concentrations of EC25 and EC50. Isoboles indicated that about 50% of the binary mixtures were additive and 50% synergistic. Synergism was even more frequently indicated by the toxic unit approach. Our data lead to the conclusion that interactions in mixtures follow the CA model. However, a surprisingly high percentage of synergistic interactions occurred. Therefore, the mixture activity of antiandrogenic azole fungicides is at least additive. Mixtures should also be considered for additive antiandrogenic activity in hazard and risk assessment. Our evaluation provides an appropriate "proof of concept", but whether it equally translates to in vivo effects should further be investigated. Copyright © 2014 Elsevier Inc. All rights reserved.

In vitro Determination of Fungicide Inhibitory Concentration for Phakopsora pachyrhizi isolates

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Bianca Moura

2016-06-01

Full Text Available ABSTRACT In vitro assays were preformed to obtain the IC50 of eight fungicides against Phakopsora pachyrhizi isolates from Passo Fundo, RS, Ponta Grossa, PR, and Primavera do Leste, MT. Different concentrations of the fungicides were added to Petri dishes containing soybean leaf extract agar medium. One milliliter of P. pachyrhizi uredospore suspension at the concentration of 3.0 x 104 uredospores/mL was added to each dish for subsequent viability quantification. Only pyraclostrobin and the mixture trifloxystrobin + prothioconazole showed IC50 values inferior to 1.0 mg/L for all tested isolates, demonstrating high fungitoxicity. There was not loss of sensitivity to any of the tested fungicides.

The complete genome sequence of Bacillus velezensis 9912D reveals its biocontrol mechanism as a novel commercial biological fungicide agent.

Science.gov (United States)

Pan, Hua-Qi; Li, Qing-Lian; Hu, Jiang-Chun

2017-04-10

A Bacillus sp. 9912 mutant, 9912D, was approved as a new biological fungicide agent by the Ministry of Agriculture of the People's Republic of China in 2016 owing to its excellent inhibitory effect on various plant pathogens and being environment-friendly. Here, we present the genome of 9912D with a circular chromosome having 4436 coding DNA sequences (CDSs), and a circular plasmid encoding 59 CDSs. This strain was finally designated as Bacillus velezensis based on phylogenomic analyses. Genome analysis revealed a total of 19 candidate gene clusters involved in secondary metabolite biosynthesis, including potential new type II lantibiotics. The absence of fengycin biosynthetic gene cluster is noteworthy. Our data offer insights into the genetic, biological and physiological characteristics of this strain and aid in deeper understanding of its biocontrol mechanism. Copyright © 2017 Elsevier B.V. All rights reserved.

Evaluating Headline fungicide on alfalfa production and sensitivity of pathogens to pyraclostrobin

Science.gov (United States)

Headline fungicide was recently registered for management of foliar diseases on alfalfa. The effect of disease control on yield, forage quality, and potential return on investment for fungicide application was determined for field experiments conducted at five locations in 2012, three in Wisconsin a...

Effect of fungicide on Fusarium verticillioidesmycelial morphology and fumonisin B1 production

Directory of Open Access Journals (Sweden)

Tatiana de Á. Miguel

2015-03-01

Full Text Available The effect of fludioxonil + metalaxyl-M on the mycelial morphology, sporulation and fumonisin B1 production by Fusarium verticillioides 103 F was evaluated. Scanning electron microscopy analysis showed that the fungicide caused inhibition of hyphal growth and defects on hyphae morphology such as cell wall disruption, withered hyphae, and excessive septation. In addition, extracellular material around the hyphae was rarely observed in the presence of fludioxonil + metalaxyl-M. While promoting the reduction of mycelial growth, the fungicide increased sporulation of F. verticillioides compared to the control, and the highest production occurred on the 14th day in the treatments and on the 10th day in the control cultures. Fumonisin B1production in the culture media containing the fungicide (treatment was detected from the 7th day incubation, whereas in cultures without fungicide (control it was detected on the 10th day. The highest fumonisin B1 production occurred on the 14th day, both for the control and for the treatment. Fludioxonil + metalaxyl - M can interfere in F. verticillioides mycelial morphology and sporulation and increase fumonisin B1 levels. These data indicate the importance of understanding the effects of fungicide to minimize the occurrence of toxigenic fungi and fumonisins.

Effect of fungicide on Fusarium verticillioides mycelial morphology and fumonisin B₁ production.

Science.gov (United States)

Miguel, Tatiana de Á; Bordini, Jaqueline G; Saito, Gervásio H; Andrade, Célia G T de J; Ono, Mario A; Hirooka, Elisa Y; Vizoni, Édio; Ono, Elisabete Y S

2015-03-01

The effect of fludioxonil + metalaxyl-M on the mycelial morphology, sporulation and fumonisin B 1 production by Fusarium verticillioides 103 F was evaluated. Scanning electron microscopy analysis showed that the fungicide caused inhibition of hyphal growth and defects on hyphae morphology such as cell wall disruption, withered hyphae, and excessive septation. In addition, extracellular material around the hyphae was rarely observed in the presence of fludioxonil + metalaxyl-M. While promoting the reduction of mycelial growth, the fungicide increased sporulation of F. verticillioides compared to the control, and the highest production occurred on the 14 (th) day in the treatments and on the 10 (th) day in the control cultures. Fumonisin B 1 production in the culture media containing the fungicide (treatment) was detected from the 7 (th) day incubation, whereas in cultures without fungicide (control) it was detected on the 10 (th) day. The highest fumonisin B 1 production occurred on the 14 (th) day, both for the control and for the treatment. Fludioxonil + metalaxyl - M can interfere in F. verticillioides mycelial morphology and sporulation and increase fumonisin B 1 levels. These data indicate the importance of understanding the effects of fungicide to minimize the occurrence of toxigenic fungi and fumonisins.

Post-infection activities of fungicides against Cercospora arachidicola of peanut (Arachis hypogaea).

Science.gov (United States)

Johnson, Robert C; Cantonwine, Emily G

2014-08-01

Despite strong indirect evidence of post-infection activity by a selection of systemic fungicides against Cercospora arachidicola, the causal organism of early leaf spot of peanut, direct post-infection activities in this pathosystem have yet to be reported in detail. This study was conducted to describe the activities of pyraclostrobin, penthiopyrad and prothioconazole on early leaf spot when each fungicide was applied after pathogen penetration began and throughout the incubation period. Most C. arachidicola penetration events occurred between 3 and 5 days after inoculation (dai), and the mean incubation period was 11.8 dai. Post-infection activities of the systemic fungicides were similar for all dependent variables measured. Systemic fungicides reduced lesion density compared with the non-treated control when applied at 3, 5 and 7 dai, and disease severity was >60% less for leaves treated with a systemic fungicide at all application dates (3, 5, 7, 9, 11 and 13 dai). Pyraclostrobin, penthiopyrad and prothioconazole showed similar systemic mobility within peanut leaves and activities against C. arachidicola, and appear to completely arrest the development of the pathogen at least 2 days post penetration, and limit pathogen colonization even when applications occur after symptom onset. © 2013 Society of Chemical Industry.

Screening Phytophthora rubi for fungicide resistance

Science.gov (United States)

Preliminary results from the survey for fungicide resistance in Phytophthora were reported at the 2016 Washington Small Fruit Conference. Phytophthora was isolated from diseased plants in 28 red raspberry fields and tested against mefenoxam, the active ingredient of Ridomil. Most isolates were ident...

Chemical management in fungicide sensivity of Mycosphaerella fijiensis collected from banana fields in México

Science.gov (United States)

Aguilar-Barragan, Alejandra; García-Torres, Ana Elisa; Odriozola-Casas, Olga; Macedo-Raygoza, Gloria; Ogura, Tetsuya; Manzo-Sánchez, Gilberto; James, Andrew C.; Islas-Flores, Ignacio; Beltrán-García, Miguel J.

2014-01-01

The chemical management of the black leaf streak disease in banana caused by Mycosphaerella fijiensis (Morelet) requires numerous applications of fungicides per year. However this has led to fungicide resistance in the field. The present study evaluated the activities of six fungicides against the mycelial growth by determination of EC50 values of strains collected from fields with different fungicide management programs: Rustic management (RM) without applications and Intensive management (IM) more than 25 fungicide application/year. Results showed a decreased sensitivity to all fungicides in isolates collected from IM. Means of EC50 values in mg L−1 for RM and IM were: 13.25 ± 18.24 and 51.58 ± 46.14 for azoxystrobin, 81.40 ± 56.50 and 1.8575 ± 2.11 for carbendazim, 1.225 ± 0.945 and 10.01 ± 8.55 for propiconazole, 220 ± 67.66 vs. 368 ± 62.76 for vinclozolin, 9.862 ± 3.24 and 54.5 ± 21.08 for fludioxonil, 49.2125 ± 34.11 and 112.25 ± 51.20 for mancozeb. A molecular analysis for β-tubulin revealed a mutation at codon 198 in these strains having an EC50 greater than 10 mg L−1 for carbendazim. Our data indicate a consistency between fungicide resistance and intensive chemical management in banana fields, however indicative values for resistance were also found in strains collected from rustic fields, suggesting that proximity among fields may be causing a fungus interchange, where rustic fields are breeding grounds for development of resistant strains. Urgent actions are required in order to avoid fungicide resistance in Mexican populations of M. fijiensis due to fungicide management practices. PMID:24948956

Chemical management in fungicide sensivity of Mycosphaerella fijiensis collected from banana fields in México

Directory of Open Access Journals (Sweden)

Alejandra Aguilar-Barragan

2014-01-01

Full Text Available The chemical management of the black leaf streak disease in banana caused by Mycosphaerella fijiensis (Morelet requires numerous applications of fungicides per year. However this has led to fungicide resistance in the field. The present study evaluated the activities of six fungicides against the mycelial growth by determination of EC50 values of strains collected from fields with different fungicide management programs: Rustic management (RM without applications and Intensive management (IM more than 25 fungicide application/year. Results showed a decreased sensitivity to all fungicides in isolates collected from IM. Means of EC50 values in mg L-1 for RM and IM were: 13.25 ± 18.24 and 51.58 ± 46.14 for azoxystrobin, 81.40 ± 56.50 and 1.8575 ± 2.11 for carbendazim, 1.225 ± 0.945 and 10.01 ± 8.55 for propiconazole, 220 ± 67.66 vs. 368 ± 62.76 for vinclozolin, 9.862 ± 3.24 and 54.5 ± 21.08 for fludioxonil, 49.2125 ± 34.11 and 112.25 ± 51.20 for mancozeb. A molecular analysis for β-tubulin revealed a mutation at codon 198 in these strains having an EC50 greater than 10 mg L-1 for carbendazim. Our data indicate a consistency between fungicide resistance and intensive chemical management in banana fields, however indicative values for resistance were also found in strains collected from rustic fields, suggesting that proximity among fields may be causing a fungus interchange, where rustic fields are breeding grounds for development of resistant strains. Urgent actions are required in order to avoid fungicide resistance in Mexican populations of M. fijiensis due to fungicide management practices.

Strong lethality and teratogenicity of strobilurins on Xenopus tropicalis embryos: Basing on ten agricultural fungicides

International Nuclear Information System (INIS)

Li, Dan; Liu, Mengyun; Yang, Yongsheng; Shi, Huahong; Zhou, Junliang; He, Defu

2016-01-01

Agricultural chemical inputs have been considered as a risk factor for the global declines in amphibian populations, yet the application of agricultural fungicides has increased dramatically in recent years. Currently little is known about the potential toxicity of fungicides on the embryos of amphibians. We studied the effects of ten commonly used fungicides (four strobilurins, two SDHIs, two triazoles, fludioxonil and folpet) on Xenopus tropicalis embryos. Lethal and teratogenic effects were respectively examined after 48 h exposure. The median lethal concentrations (LC50s) and the median teratogenic concentrations (TC50s) were determined in line with actual exposure concentrations. These fungicides except two triazoles showed obvious lethal effects on embryos; however LC50s of four strobilurins were the lowest and in the range of 6.81–196.59 μg/L. Strobilurins, SDHIs and fludioxonil induced severe malformations in embryos. Among the ten fungicides, the lowest TC50s were observed for four strobilurins in the range of 0.61–84.13 μg/L. The teratogenicity shared similar dose–effect relationship and consistent phenotypes mainly including microcephaly, hypopigmentation, somite segmentation and narrow fins. The findings indicate that the developmental toxicity of currently-used fungicides involved with ecologic risks on amphibians. Especially strobilurins are highly toxic to amphibian embryos at μg/L level, which is close to environmentally relevant concentrations. - Highlights: • Effects of ten agricultural fungicides were tested on Xenopus tropicalis embryos. • Strobilurin fungicides showed strong lethal and teratogenic effects on embryos. • Lowest LC50 and TC50 were observed for strobilurins in ten fungicides. • μg/L level of toxic concentrations for strobilurins was environmentally relevant. • Teratogenicity shared similar dose–effect relationship and main phenotypes. - Strobilurins induced strong lethality and teratogenicity on Xenopus

Thrombin-induced rabbit platelet microbicidal protein is fungicidal in vitro.

Science.gov (United States)

Yeaman, M R; Ibrahim, A S; Edwards, J E; Bayer, A S; Ghannoum, M A

1993-03-01

Platelet microbicidal protein (PMP) is released from platelets in response to thrombin stimulation. PMP is known to possess in vitro bactericidal activity against Staphylococcus aureus and viridans group streptococci. To determine whether PMP is active against other intravascular pathogens, we evaluated its potential fungicidal activity against strains of Candida species and Cryptococcus neoformans. Anionic resin adsorption and gel electrophoresis confirmed that the fungicidal activity of PMP resided in a small (approximately 8.5-kDa), cationic protein, identical to previous studies of PMP-induced bacterial killing (M.R. Yeaman, S.M. Puentes, D.C. Norman, and A.S. Bayer, Infect. Immun. 60:1202-1209, 1992). When assayed over a 180-min period in vitro, the susceptibilities of these fungi to PMP varied considerably. Generally, Candida albicans strains (mean survival, 33.5% +/- 6.9% [n = 6]) as well as isolates of Candida glabrata (mean survival, 50.8% +/- 2.9% [n = 2]) were the most susceptible to killing by PMP, while Candida guillermondii and Candida parapsilosis were relatively resistant to PMP-induced killing. Compared with C. albicans, C. neoformans was relatively resistant to the fungicidal activity of PMP, with a mean survival among the isolates studied of 77.4% +/- 12.4% (n = 6). Against C. albicans, PMP-induced fungicidal activity was time dependent (range, 0 to 180 min), PMP concentration dependent (range, 10 to 150 U/ml), and inversely related to the fungal inoculum (range, 5 x 10(3) to 1 x 10(5) CFU/ml). Scanning electron microscopy of PMP-exposed C. albicans and C. neoformans cells revealed extensive surface damage and collapse, suggesting that the site of PMP fungicidal action may directly or indirectly involve the fungal cell envelope.

Control Efficacy of Fungicides on Chinese Cabbage Clubroot under Several Conditions

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Min-Yong Eom

2011-08-01

Full Text Available To develop the efficient screening methods for antifungal compound active to Chinese cabbage clubroot caused by Plasmodiophora brassicae, the control efficacy of three fungicides fluazinam, ethaboxam, and cyazofamid on the disease was tested under several conditions such as soil types, cultivars of Chinese cabbage, growth stages of the host, and inoculum concentrations. The in vivo antifungal activities of the fungicides on clubroot of two Chinese cabbage cultivars were hardly different. At 7- and 14-day-old seedlings, the fungicides were more effective to control of clubroot than at 21-day-old seedlings. In a commercial horticulture media soil (CNS, disease severity of untreated controls was higher and control activity of the fungicides was less than in a mixture of CNS and upland soil (1:1, v/v. Disease development of the seedlings inoculated with P. brassicae at 1.8×10(7 spores/pot to 1.1×10(9 spores/pot was almost same, but control efficacy of the fungicides was negatively correlated with inoculum dosages. To effectively select in vivo antifungal compound on Chinese cabbage clubroot, 14-day-old seedlings need to be inoculated with P. brassicae by drenching the spore suspension to give 1×10(8 spores/pot 1 day after chemical treatment. To develop clubroot, the inoculated plants are incubated in a growth chamber at 20℃ for 2 days, and then cultivated in a greenhouse (20±5℃ for four weeks.

The effect of using a fungicide along with bactericide in the main ...

African Journals Online (AJOL)

quarternized compounds), and a fungicide (2-thiocyanomethylthio benzothiazole based) commonly used in Turkish leather industry were chosen. The bactericides were added into the main soaking float with and without different concentrations of fungicide. In each trial, liquor samples were taken at the end of the main ...

Yield of Potato as Influenced by Crop Sanitation and Reduced Fungicidal Treatments

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Fontem, DA.

1995-01-01

Full Text Available The effects of crop sanitation and reduced sprays of "Ridomil plus®" (12 % metalaxyl + 60 % cuprous oxide on the control of potato (Solanum tuberosum late blight caused by Phytophthora infestans were evaluated in two field experiments in 1993 in Dschang, Cameroon. In the first experiment, sanitation (five weekly removals of blighted leaves and two fungicidal treatments were initiated from first symptoms. In the second experiment, both fungicidal sprays were made at varying rates. Marketable yields increased by 50 % in sanitation-treated plots, by 94 % in plots sprayed with Ridomil plus (2.24 kg a. i./ha, or by 55 % in those exposed to both control methods. The fungicide equivalence of the sanitation treatment was two sprays of Ridomil plus at 0.76 kg a. i./ha. These results suggest that proper removal of diseased leaves or reduced fungicidal protection may be an effective late blight control method in potato farming.

Multiple nucleobase transporters contribute to boscalid sensitivity in Aspergillus nidulans.

Science.gov (United States)

Kalampokis, Ioannis F; Kapetanakis, George C; Aliferis, Konstantinos A; Diallinas, George

2018-03-01

The development of fungicide-resistant fungal populations represents a major challenge for the agrochemical and agri-food sectors, which threatens food supply and security. The issue becomes complex for fungi that cause quantitative and qualitative losses due to mycotoxin biosynthesis. Nonetheless, currently, the molecular details underlying fungicide action and fungal resistance mechanisms are partially known. Here, we have investigated whether plasma membrane transporters contribute to specific fungicide uptake in the model fungus Aspergillus nidulans. Independent physiological tests and toxicity screening of selected fungicides provided evidence that the antifungal activity of Succinate Dehydrogenase Inhibitors (SDHIs) is associated with the expression of several nucleobase-related transporters. In particular, it was shown that a strain genetically inactivated in all seven nucleobase-related transporters is resistant to the fungicide boscalid, whereas none of the single null mutants exhibited significant resistance level. By constructing and testing isogenic strains that over-express each one of the seven transporters, we confirmed that five of them, namely, UapC, AzgA, FycB, CntA, and FurA, contribute to boscalid uptake. Additionally, by employing metabolomics we have examined the effect of boscalid on the metabolism of isogenic strains expressing or genetically lacking boscalid-related nucleobase transporters. The results confirmed the involvement of specific nucleobase transporters in fungicide uptake, leading to the discovery of corresponding metabolites-biomarkers. This work is the first report on the involvement of specific transporters in fungicide uptake and toxicity and their impact on fungal metabolism regulation and results might be further exploited towards the deeper understanding of fungal resistance to fungicides. Copyright © 2018 Elsevier Inc. All rights reserved.

Method validation for strobilurin fungicides in cereals and fruit

DEFF Research Database (Denmark)

Christensen, Hanne Bjerre; Granby, Kit

2001-01-01

Strobilurins are a new class of fungicides that are active against a broad spectrum of fungi. In the present work a GC method for analysis of strobilurin fungicides was validated. The method was based on extraction with ethyl acetate/cyclohexane, clean-up by gel permeation chromatography (GPC......) and determination of the content by gas chromatography (GC) with electron capture (EC-), nitrogen/phosphorous (NP-), and mass spectrometric (MS-) detection. Three strobilurins, azoxystrobin, kresoxim-methyl and trifloxystrobin were validated on three matrices, wheat, apple and grapes. The validation was based...

An evaluation of some fungicides in the management of fruit and leaf ...

African Journals Online (AJOL)

Four fungicide treatments viz Ben late (Benomyl), Cupravit (Copper oxychloride), Dithane M45 (Mancozeb), and. Ben late alternated with Dithane M45 were applied to control P!laeoramularia angolensi~ In a block of the variety. "Valencia" in the citrus orchard at Kiige, Uganda. No fungicide was applied to the control.

Occurrence and Environmental Effects of Boscalid and Other Fungicides in Three Targeted Use Areas in the United States

Science.gov (United States)

Reilly, T. J.; Smalling, K. L.; Wilson, E. R.

2011-12-01

Fungicides are typically used to control the outbreak of persistent, historically significant plant diseases like late blight (caused by Phytophthora infestans and responsible for the Irish Potato famine of 1846) and newer plant diseases like Asian Soy Rust, both of which are potentially devastating if not controlled. Of the more than 67,000 pesticide products currently registered for use in the United States, over 3,600 are used to combat fungal diseases. Although they are widely used, relatively little is known about the fate and potential secondary effects of fungicides in the aquatic environment. Even less is known about the fate and environmental occurrence of recently registered fungicides including boscalid, which was first registered for use in the US in 2003. Unlike most other pesticides, multiple fungicides are typically applied as a prophylactic crop protectant upwards of ten times per season (depending upon conditions and crop type), but at lower application rates than herbicides or insecticides. This difference in usage increases the likelihood of chronic exposure of aquatic ecosystems to low concentrations of fungicides. Using a newly developed analytical method, the U.S. Geological Survey measured 33 fungicides in surface water and shallow groundwater in three geographic areas of intense fungicide use across the US. Sampling sites were selected near or within farms using prophylactic fungicides at rates and types typical of the crop type and their geographic location. At least one fungicide was detected in 75% of the surface waters (n=60) and 58% of the groundwater (n=12) samples. Twelve fungicides were detected in surface- and groundwater including boscalid (72%), azoxystrobin (51%), pyraclostrobin (40%), chlorothalonil (38%) and pyrimethanil (28%). Boscalid was the most frequently detected pesticide and has not been previously documented in the aquatic environment. In this study, an average of 44% of the pesticide concentration in a water sample

Bioremediation of fungicides by spent mushroom substrate and its associated microflora.

Science.gov (United States)

Ahlawat, O P; Gupta, Pardeep; Kumar, Satish; Sharma, D K; Ahlawat, K

2010-10-01

Experiments were conducted both under in vitro and in situ conditions to determine the biodegradation potential of button mushroom spent substrate (SMS) and its dominating microbes (fungi and bacteria) for carbendazim and mancozeb, the commonly used agricultural fungicides. During 6 days of incubation at 30 ± 2°C under broth culture conditions, highest degradation of carbendazim (17.45%) was recorded with B-1 bacterial isolate, while highest degradation of mancozeb (18.05%) was recorded with Trichoderma sp. In fungicide pre-mixed sterilized SMS, highest degradation of carbendazim (100.00-66.50 μg g(-1)) was recorded with mixed inoculum of Trichoderma sp. and Aspergillus sp., whereas highest degradation of mancozeb (100.00-50.50 μg g(-1)) was with mixed inoculum of Trichoderma sp., Aspergillus sp. and B-I bacterial isolate in 15 days of incubation at 30 ± 2°C. All these microbes both individually as well as in different combinations grew well and produced extracellular lignolytic enzymes on SMS, which helped in fungicides degradation. Under in situ conditions, among three different proportions of SMS (10, 20 and 30%, w/w) mixed with fungicide pre-mixed soil (100 μg g(-1) of soil), the degradation of carbendazim was highest in 30% SMS treatment, while for mancozeb it was in 20% SMS treatment. The residue levels of both fungicides decreased to half of their initial concentration after 1 month of SMS mixing.

Inhibition of chitin biosynthesis in cultured imaginal discs: Effects of alpha-amanitin, actinomycin-D, cycloheximide, and puromycin.

Science.gov (United States)

Oberlander, Herbert; Ferkovich, Stephen; Leach, Eddie; Van Essen, Frank

1980-02-01

Wing imaginal discs isolated from last instar larvae of the Indian meal moth,Plodia interpunctella, produced chitin when incubated in vitro with ≧2×10 -7 M 20-hydroxyecdysone. Chitin biosynthesis was initiated 8 h after the conclusion of a 24-h treatment with hormone. Simulataneous incubation of wing discs with 20-hydroxyecdysone and either inhibitors of RNA synthesis (alpha-amanitin, actinomycin-D) or inhibitors of protein systhesis (cycloheximide, puromycin) prevented chitin biosynthesis. We conclude from our results that RNA and protein synthesis must continue undiminished during the hormone-contact period, and that synthesis of protein, but not of new RNA is required during the posthormone culture period. Our findings are consistent with the hypothesis that ecdysteroids stimulate insect metamorphosis by promoting the synthesis of new RNA and protein during a hormone-dependent phase followed by hormone-independent protein synthesis.

Effects of Fungicides, Time of Application, and Application Method on Control of Sclerotinia Blight in Peanut

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Jason E. Woodward

2015-01-01

Full Text Available Field studies were conducted from 2007 to 2010 to evaluate the response of peanut cultivars to different fungicides, application timings, and methods. Overall, fungicides reduced Sclerotinia blight incidence and increased pod yields when applied to susceptible and partially resistant cultivars. Disease suppression was greater when full fungicide rates were applied preventatively; however, yields between fungicide treated plots were similar. Lower levels of disease and higher yields were achieved with the partially resistant cultivar Tamrun OL07 compared to the susceptible cultivars Flavor Runner 458 and Tamrun OL 02. Despite possessing improved resistance Tamrun OL07 responded to all fungicide applications. While similar levels of disease control were achieved with broadcast or banded applications made during the day or at night, the yield response for the different application methods was inconsistent among years. A negative relationship (slope = −73.8; R2=0.73; P<0.01 was observed between final disease incidence ratings and yield data from studies where a fungicide response was observed. These studies suggest that both boscalid and fluazinam are effective at controlling Sclerotinia blight in peanuts. Alternative management strategies such as nighttime and banded applications could allow for lower fungicide rates to be used; however, additional studies are warranted.

Amino Acid Precursor Supply in the Biosynthesis of the RNA Polymerase Inhibitor Streptolydigin by Streptomyces lydicus▿†

OpenAIRE

Gómez, Cristina; Horna, Dina H.; Olano, Carlos; Palomino-Schätzlein, Martina; Pineda-Lucena, Antonio; Carbajo, Rodrigo J.; Braña, Alfredo F.; Méndez, Carmen; Salas, José A.

2011-01-01

Biosynthesis of the hybrid polyketide-nonribosomal peptide antibiotic streptolydigin, 3-methylaspartate, is utilized as precursor of the tetramic acid moiety. The three genes from the Streptomyces lydicus streptolydigin gene cluster slgE1-slgE2-slgE3 are involved in 3-methylaspartate supply. SlgE3, a ferredoxin-dependent glutamate synthase, is responsible for the biosynthesis of glutamate from glutamine and 2-oxoglutarate. In addition to slgE3, housekeeping NADPH- and ferredoxin-dependent glu...

Factors influencing the toxicity of Headline® fungicides to terrestrial stage toads.

Science.gov (United States)

Cusaac, J Patrick W; Mimbs, William H; Belden, Jason B; Smith, Loren M; McMurry, Scott T

2017-10-01

Amphibians are susceptible to exposure from contaminants via multiple pathways. Pyraclostrobin fungicides have been shown to be toxic to terrestrial amphibians at environmentally relevant concentrations; however, these studies did not account for factors that may influence exposure and effects, such as fungicide formulation, age of the individual, exposure route, and physiological state of the individual. We examined Headline® and Headline AMP® fungicide toxicity to adult Anaxyrus cognatus and Anaxyrus woodhousii by direct overspray, as well as acute toxicity of Headline AMP to juvenile A. cognatus through direct overspray, previously exposed soils, and diet. We also assessed effects of hydration state on fungicide toxicity in juvenile A. cognatus and sublethal effects of fungicide exposure on prey-orientation ability of juvenile A. cognatus. Neither formulation of Headline caused mortality of adult A. cognatus and A. woodhousii at up to 5 times the maximum label rate in North American corn (1052 and 879 mL formulation/ha for Headline AMP and Headline fungicides, respectively, corresponding to 1.52 and 2.2 μg pyraclostrobin/cm 2 , respectively). Exposures of juvenile A. cognatus to Headline AMP via direct overspray and previously exposed soils (2 types) resulted in median lethal rate (LR50) values of 2.4, 3.34, and 3.61 μg pyraclostrobin/cm 2 , respectively. Dietary Headline AMP exposure was not toxic, prey-orientations were not influenced by exposure, and effects were similar between dehydrated and hydrated treatments (LR50 = 2.4 and 2.3 μg pyraclostrobin/cm 2 , respectively). These results, combined with exposure concentrations reported in previous studies, suggest that risk of acute mortality for amphibians in terrestrial environments is low and is dictated by body size and site-specific factors influencing exposure. Environ Toxicol Chem 2017;36:2679-2688. © 2017 SETAC. © 2017 SETAC.

Conazole fungicides inhibit Leydig cell testosterone secretion and androgen receptor activation in vitro

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Maarke J.E. Roelofs

2014-01-01

Full Text Available Conazole fungicides are widely used in agriculture despite their suspected endocrine disrupting properties. In this study, the potential (anti-androgenic effects of ten conazoles were assessed and mutually compared with existing data. Effects of cyproconazole (CYPRO, fluconazole (FLUC, flusilazole (FLUS, hexaconazole (HEXA, myconazole (MYC, penconazole (PEN, prochloraz (PRO, tebuconazole (TEBU, triadimefon (TRIA, and triticonazole (TRIT were examined using murine Leydig (MA-10 cells and human T47D-ARE cells stably transfected with an androgen responsive element and a firefly luciferase reporter gene. Six conazoles caused a decrease in basal testosterone (T secretion by MA-10 cells varying from 61% up to 12% compared to vehicle-treated control. T secretion was concentration-dependently inhibited after exposure of MA-10 cells to several concentrations of FLUS (IC50 = 12.4 μM or TEBU (IC50 = 2.4 μM in combination with LH. The expression of steroidogenic and cholesterol biosynthesis genes was not changed by conazole exposure. Also, there were no changes in reactive oxygen species (ROS formation that could explain the altered T secretion after exposure to conazoles. Nine conazoles decreased T-induced AR activation (IC50s ranging from 10.7 to 71.5 μM and effect potencies (REPs were calculated relative to the known AR antagonist flutamide (FLUT. FLUC had no effect on AR activation by T. FLUS was the most potent (REP = 3.61 and MYC the least potent (REP = 0.03 AR antagonist. All other conazoles had a comparable REP from 0.12 to 0.38. Our results show distinct in vitro anti-androgenic effects of several conazole fungicides arising from two mechanisms: inhibition of T secretion and AR antagonism, suggesting potential testicular toxic effects. These effects warrant further mechanistic investigation and clearly show the need for accurate exposure data in order to perform proper (human risk assessment of this class of compounds.

The effect of the Falcon 460 EC fungicide on soil microbial communities, enzyme activities and plant growth.

Science.gov (United States)

Baćmaga, Małgorzata; Wyszkowska, Jadwiga; Kucharski, Jan

2016-10-01

Fungicides are considered to be effective crop protection chemicals in modern agriculture. However, they can also exert toxic effects on non-target organisms, including soil-dwelling microbes. Therefore, the environmental fate of fungicides has to be closely monitored. The aim of this study was to evaluate the influence of the Falcon 460 EC fungicide on microbial diversity, enzyme activity and resistance, and plant growth. Samples of sandy loam with pH KCl 7.0 were collected for laboratory analyses on experimental days 30, 60 and 90. Falcon 460 EC was applied to soil in the following doses: control (soil without the fungicide), dose recommended by the manufacturer, 30-fold higher than the recommended dose, 150-fold higher than the recommended dose and 300-fold higher than the recommended dose. The observed differences in the values of the colony development index and the eco-physiological index indicate that the mixture of spiroxamine, tebuconazole and triadimenol modified the biological diversity of the analyzed groups of soil microorganisms. Bacteria of the genus Bacillus and fungi of the genera Penicillium and Rhizopus were isolated from fungicide-contaminated soil. The tested fungicide inhibited the activity of dehydrogenases, catalase, urease, acid phosphatase and alkaline phosphatase. The greatest changes were induced by the highest fungicide dose 300-fold higher than the recommended dose. Dehydrogenases were most resistant to soil contamination. The Phytotoxkit test revealed that the analyzed fungicide inhibits seed germination capacity and root elongation. The results of this study indicate that excessive doses of the Falcon 460 EC fungicide 30-fold higher than the recommended dose to 300-fold higher than the recommended dose) can induce changes in the biological activity of soil. The analyzed microbiological and biochemical parameters are reliable indicators of the fungicide's toxic effects on soil quality.

Sterol Biosynthesis Pathway as Target for Anti-trypanosomatid Drugs

Directory of Open Access Journals (Sweden)

Wanderley de Souza

2009-01-01

Full Text Available Sterols are constituents of the cellular membranes that are essential for their normal structure and function. In mammalian cells, cholesterol is the main sterol found in the various membranes. However, other sterols predominate in eukaryotic microorganisms such as fungi and protozoa. It is now well established that an important metabolic pathway in fungi and in members of the Trypanosomatidae family is one that produces a special class of sterols, including ergosterol, and other 24-methyl sterols, which are required for parasitic growth and viability, but are absent from mammalian host cells. Currently, there are several drugs that interfere with sterol biosynthesis (SB that are in use to treat diseases such as high cholesterol in humans and fungal infections. In this review, we analyze the effects of drugs such as (a statins, which act on the mevalonate pathway by inhibiting HMG-CoA reductase, (b bisphosphonates, which interfere with the isoprenoid pathway in the step catalyzed by farnesyl diphosphate synthase, (c zaragozic acids and quinuclidines, inhibitors of squalene synthase (SQS, which catalyzes the first committed step in sterol biosynthesis, (d allylamines, inhibitors of squalene epoxidase, (e azoles, which inhibit C14α-demethylase, and (f azasterols, which inhibit Δ24(25-sterol methyltransferase (SMT. Inhibition of this last step appears to have high selectivity for fungi and trypanosomatids, since this enzyme is not found in mammalian cells. We review here the IC50 values of these various inhibitors, their effects on the growth of trypanosomatids (both in axenic cultures and in cell cultures, and their effects on protozoan structural organization (as evaluted by light and electron microscopy and lipid composition. The results show that the mitochondrial membrane as well as the membrane lining the protozoan cell body and flagellum are the main targets. Probably as a consequence of these primary effects, other important changes take

Field efficacy of different fungicide mixtures in control of net blotch on barley

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Stepanović Miloš

2016-01-01

Full Text Available Seven fungicide mixtures (epoxiconazol + metconazole, boscalid + epoxiconazole, pyraclostrobin + epoxiconazole, prothioconazole + tebuconazole, picoxistrobin + cyproconazole, azoxystrobin + cyproconazole and spiroxamine + tebuconazole + triadimenol were evaluated for control of net blotch of barley caused by Drechslera teres, as well as yield losses, over the 2010 and 2011 growing seasons. Two applications of the fungicide combination pyraclostrobin + epoxiconazole at the rate of 1.0 l ha-1 were the most effective treatment in controlling the disease and improving yield in both experimental years. Treatments with the fungicide mixtures epoxiconazol + metconazole and spiroxamine + tebuconazole + triadimenol showed the least effectiveness in disease control, as well as yield increase.

Emerging resistance against different fungicides in Lasiodiplodia theobromae, the cause of mango dieback in Pakistan

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Rehman ur Ateeq

2015-01-01

Full Text Available Dieback of mango caused by Lasiodiplodia theobromae is among several diseases responsible for low crop production in Pakistan. To further complicate the issue, resistance in L. theobromae is emerging against different fungicides. L. theobromae was isolated from diseased samples of mango plants collected from various orchards in the Multan District. The efficacy of different fungicides viz. copper oxychloride, diethofencarb, pyrachlostrobin, carbendazim, difenoconazole, mancozeb, and thiophanate-methyl was evaluated in vitro using a poison food technique. Thiophanate-methyl at all concentrations was found to be the most effective among five systemic fungicides against L. theobromae, followed by carbendazim, difenoconazole and diethofencarb. The fungicides, i.e., thiophanate-methyl, difenoconazole, carbendazim and diethofencarb showed maximum efficacy with increasing concentration. The isolates of L. theobromae showed some resistance development against the tested fungicides when compared with previous work. These investigations provide new information about chemical selection for the control of holistic disease in mango growing zones of Pakistan.

Effect of fungicide on Fusarium verticillioides mycelial morphology and fumonisin B 1 production

Science.gov (United States)

Miguel, Tatiana de Á.; Bordini, Jaqueline G.; Saito, Gervásio H.; Andrade, Célia G.T. de J.; Ono, Mario A.; Hirooka, Elisa Y.; Vizoni, Édio; Ono, Elisabete Y.S.

2015-01-01

The effect of fludioxonil + metalaxyl-M on the mycelial morphology, sporulation and fumonisin B 1 production by Fusarium verticillioides 103 F was evaluated. Scanning electron microscopy analysis showed that the fungicide caused inhibition of hyphal growth and defects on hyphae morphology such as cell wall disruption, withered hyphae, and excessive septation. In addition, extracellular material around the hyphae was rarely observed in the presence of fludioxonil + metalaxyl-M. While promoting the reduction of mycelial growth, the fungicide increased sporulation of F. verticillioides compared to the control, and the highest production occurred on the 14 th day in the treatments and on the 10 th day in the control cultures. Fumonisin B 1 production in the culture media containing the fungicide (treatment) was detected from the 7 th day incubation, whereas in cultures without fungicide (control) it was detected on the 10 th day. The highest fumonisin B 1 production occurred on the 14 th day, both for the control and for the treatment. Fludioxonil + metalaxyl - M can interfere in F. verticillioides mycelial morphology and sporulation and increase fumonisin B 1 levels. These data indicate the importance of understanding the effects of fungicide to minimize the occurrence of toxigenic fungi and fumonisins. PMID:26221120

Fungicidal Drugs Induce a Common Oxidative-Damage Cellular Death Pathway

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Peter Belenky

2013-02-01

Full Text Available Amphotericin, miconazole, and ciclopirox are antifungal agents from three different drug classes that can effectively kill planktonic yeast, yet their complete fungicidal mechanisms are not fully understood. Here, we employ a systems biology approach to identify a common oxidative-damage cellular death pathway triggered by these representative fungicides in Candida albicans and Saccharomyces cerevisiae. This mechanism utilizes a signaling cascade involving the GTPases Ras1 and Ras2 and protein kinase A, and it culminates in death through the production of toxic reactive oxygen species in a tricarboxylic-acid-cycle- and respiratory-chain-dependent manner. We also show that the metabolome of C. albicans is altered by antifungal drug treatment, exhibiting a shift from fermentation to respiration, a jump in the AMP/ATP ratio, and elevated production of sugars; this coincides with elevated mitochondrial activity. Lastly, we demonstrate that DNA damage plays a critical role in antifungal-induced cellular death and that blocking DNA-repair mechanisms potentiates fungicidal activity.

Phenotypical and Molecular Characterisation of Fusarium circinatum: Correlation with Virulence and Fungicide Sensitivity

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Martin Mullett

2017-11-01

Full Text Available Fusarium circinatum, causing pine pitch canker, is one of the most damaging pathogens of Pinus species. This study investigated the use of phenotypical and molecular characteristics to delineate groups in a worldwide collection of isolates. The groups correlated with virulence and fungicide sensitivity, which were tested in a subset of isolates. Virulence tests of twenty isolates on P. radiata, P. sylvestris and P. pinaster demonstrated differences in host susceptibility, with P. radiata most susceptible and P. sylvestris least susceptible. Sensitivity to the fungicides fludioxonil and pyraclostrobin varied considerably between isolates from highly effective (half-maximal effective concentration (EC50 < 0.1 ppm to ineffective (EC50 > 100 ppm. This study demonstrates the potential use of simply acquired phenotypical (cultural, morphological and molecular metrics to gain a preliminary estimate of virulence and sensitivity to certain fungicides. It also highlights the necessity of including a range of isolates in fungicide tests and host susceptibility assays, particularly of relevance to tree breeding programmes.

Biosynthesis of promatrix metalloproteinase-9/chondroitin sulphate proteoglycan heteromer involves a Rottlerin-sensitive pathway.

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Nabin Malla

Full Text Available BACKGROUND: Previously we have shown that a fraction of the matrix metalloproteinase-9 (MMP-9 synthesized by the macrophage cell line THP-1 was bound to a chondroitin sulphate proteoglycan (CSPG core protein as a reduction sensitive heteromer. Several biochemical properties of the enzyme were changed when it was bound to the CSPG. METHODOLOGY/PRINCIPAL FINDINGS: By use of affinity chromatography, zymography, and radioactive labelling, various macrophage stimulators were tested for their effect on the synthesis of the proMMP-9/CSPG heteromer and its components by THP-1 cells. Of the stimulators, only PMA largely increased the biosynthesis of the heteromer. As PMA is an activator of PKC, we determined which PKC isoenzymes were expressed by performing RT-PCR and Western Blotting. Subsequently specific inhibitors were used to investigate their involvement in the biosynthesis of the heteromer. Of the inhibitors, only Rottlerin repressed the biosynthesis of proMMP-9/CSPG and its two components. Much lower concentrations of Rottlerin were needed to reduce the amount of CSPG than what was needed to repress the synthesis of the heteromer and MMP-9. Furthermore, Rottlerin caused a minor reduction in the activation of the PKC isoenzymes δ, ε, θ and υ (PKD3 in both control and PMA exposed cells. CONCLUSIONS/SIGNIFICANCE: The biosynthesis of the proMMP-9/CSPG heteromer and proMMP-9 in THP-1 cells involves a Rottlerin-sensitive pathway that is different from the Rottlerin sensitive pathway involved in the CSPG biosynthesis. MMP-9 and CSPGs are known to be involved in various physiological and pathological processes. Formation of complexes may influence both the specificity and localization of the enzyme. Therefore, knowledge about biosynthetic pathways and factors involved in the formation of the MMP-9/CSPG heteromer may contribute to insight in the heteromers biological function as well as pointing to future targets for therapeutic agents.

SYNTHESIS AND FUNGICIDAL ACTIVITY OF ACETYL ...

African Journals Online (AJOL)

a

large varieties of new sulfur based crop protection chemicals in development around the world. [14, 15]. Methods ... sulfur fission viz, the resonance – stabilized benzyl (or isomeric tropylium) cation [19]. The elimination of ... two well – established fungicides so as to compare their activities with those of compounds 1(a. – d).

Effects of triazole fungicides on androgenic disruption and CYP3A4 enzyme activity.

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Lv, Xuan; Pan, Liumeng; Wang, Jiaying; Lu, Liping; Yan, Weilin; Zhu, Yanye; Xu, Yiwen; Guo, Ming; Zhuang, Shulin

2017-03-01

Triazole fungicides are widely used as broad-spectrum fungicides, non-steroidal antiestrogens and for various industrial applications. Their residues have been frequently detected in multiple environmental and human matrices. The increasingly reported toxicity incidents have led triazole fungicides as emerging contaminants of environmental and public health concern. However, whether triazole fungicides behave as endocrine disruptors by directly mimicking environmental androgens/antiandrogens or exerting potential androgenic disruption indirectly through the inhibition of cytochrome P450 (CYP450) enzyme activity is yet an unresolved question. We herein evaluated five commonly used triazole fungicides including bitertanol, hexaconazole, penconazole, tebuconazole and uniconazole for the androgenic and anti-androgenic activity using two-hybrid recombinant human androgen receptor (AR) yeast bioassay and comparatively evaluated their effects on enzymatic activity of CYP3A4 by P450-Glo™ CYP3A4 bioassay. All five fungicides showed moderate anti-androgenic activity toward human AR with the IC 50 ranging from 9.34 μM to 79.85 μM. The anti-androgenic activity remained no significant change after the metabolism mediated by human liver microsomes. These fungicides significantly inhibited the activity of CYP3A4 at the environmental relevant concentrations and the potency ranks as tebuconazole > uniconazole > hexaconazole > penconazole > bitertanol with the corresponding IC 50 of 0.81 μM, 0.93 μM, 1.27 μM, 2.22 μM, and 2.74 μM, respectively. We found that their anti-androgenic activity and the inhibition potency toward CYP3A4 inhibition was significantly correlated (R 2 between 0.83 and 0.97, p pesticides and structurally similar chemicals should fully consider potential androgenic disrupting effects and the influences on the activity of CYP450s. Copyright © 2016 Elsevier Ltd. All rights reserved.

In vitro colonial inhibition of an isolate from Colletotrichum acutatum Simmonds to fungicide treatments

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Dagoberto Guillén Sánchez

2018-02-01

Full Text Available The aim of the research was to evaluate the in vitro sensitivity of Colletotrichum acutatum antracnosis to seven fungicides. It began with an isolate preserved in the ceparium of the Phytopathology Laboratory of the High School Studies of Xalostoc, Morelos. A completely randomized design was used to evaluate the fungicides benomyl, diphenoconazole, azoxystrobin, trifloxystrobin, copper oxychloride, fluoxastrobin and captan, at high, medium and low doses, for a total of 22 treatments with six repetitions. Sterile distilled water was applied to the control. The treatments were applied at a rate of 5 mL per plate, which contained PDA medium and a mycelial disc (Ø 5 mm. The inoculated plates were incubated at 24 °C, in 12 hour photoperiod. The colony diameter was measured every 24 hours and the percent inhibition was calculated. A bifactorial variance analysis was performed, according to Fungicide and Dose; and the differences between treatments were detected by the LSD test with 95 % confidence. The diameter of the colony and the percentage of inhibition did not show differences for dose levels, without significant effects for the interaction of both factors, fungicides, and dose. However, all doses of the different fungicides inhibited colony growth compared to the control. The benomyl, difenoconazol and captan fungicides were able to totally reduce the growth of the C. acutatum colony; followed by copper oxychloride, azoxystrobin, fluoxastrobin and trifloxystrobin in decreasing order. Only benomyl, difenoconazol, captan and copper oxychloride achieved more than 50 % inhibition.

Sensitivity of some nitrogen fixers and the target pest Fusarium oxysporum to fungicide thiram.

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Osman, Awad G; Sherif, Ashraf M; Elhussein, Adil A; Mohamed, Afrah T

2012-03-01

This study was carried out to investigate the toxic effects of the fungicide thiram (TMTD) against five nitrogen fixers and the thiram target pest Fusarium oxysporum under laboratory conditions. Nitrogen fixing bacteria Falvobacterium showed the highest values of LD(50) and proved to be the most resistant to the fungicide followed by Fusarium oxysporum, while Pseudomonas aurentiaca was the most affected microorganism. LD(50) values for these microorganisms were in 2-5 orders of magnitude lower in comparison with LD(50) value for Fusarium oxysporum. Thiram was most toxic to Pseudomonas aurentiaca followed by Azospirillum. The lowest toxicity index was recorded for Fusarium oxysporum and Flavobacterium. The slope of the curve for Azomonas, Fusarium oxysporum and Flavobacterium is more steep than that of the other curves, suggesting that even a slight increase of the dose of the fungicide can cause a very strong negative effect. Thiram was more selective to Pseudomonas aurentiaca followed by Azospirillum, Rhizobium meliloti and Azomonas. The lowest selectivity index of the fungicide was recorded for Falvobacterium followed by Fusarium oxysporum. The highest safety coefficient of the fungicide was assigned for Flavobacterium, while Pseudomonas aurentiaca showed the lowest value.

Effects of azole fungicides on the function of sex and thyroid hormones

DEFF Research Database (Denmark)

Kjærstad, Mia Birkhøj; Andersen, Helle Raun; Taxvig, Camilla

Azole-fungicides are frequently used in Denmark. Epoxiconazole, propiconazole, and tebuconazole had endocrine disrupting properties in cell based assays. In rats, epoxiconazole and tebuconazole increased gestational length, maternal progesterone level, and masculinized female-offspring. Besides, ......, tebuconazole caused feminization of male-offspring. Similar effects were previously demonstrated for prochloraz. The results indicate that azole-fungicides in general have endocrine disrupting properties....

EFFICACY OF FUNGICIDES AGAINST CALONECTRIA PAUCIRAMOSA IN POT AZALEA.

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Heungens, K; Pauwels, E

2015-01-01

Calonectria (formerly Cylindrocladium) infection of pot azalea (Rhododendron simsii Planch) is an important disease problem in which usually one or two of the four plants per pot show progressing leaf and especially stem lesions, leading to mortality of the respective plant and rendering the pot unmarketable. This may occur in a later stage of the growing season, leading to significant commercial losses. The main objective of this study was to test a range of fungicides for their efficacy against this pathogen. To test the fungicides, a bioassay was first developed in which mycelium and conidiospores of the pathogen were produced on Potato Dextrose Agar, blended in water, and dilutions of the resulting suspension inoculated at the base of 11-week-old cuttings three weeks after they had been trimmed. Disease progression was monitored up to 7 weeks post inoculation and a disease index on a scale of 0 to 3 was established. In the actual efficacy trial, the following fungicides (with corresponding active ingredient(s)) were tested as preventive treatments: Topsin M 70 WG (thiophanate-methyl), Sporgon (prochloraz), Signum (boscalid+pyraclostrobin), Switch (cyprodinyl+fludioxonil), Flint 50WG (trifloxystrobin), Ortiva Top (azoxystrobin+difenoconazole) and Fungaflor (imazalil). Disease expression started after about 2 weeks, increased approximately 1 index level, and leveled off 5 weeks after inoculation. The best control was observed with Sporgon, Ortiva Top and Signum. Switch produced intermediate effects and insufficient control was observed with Topsin, Flint and Fungaflor. These results explain why specific standard fungicide treatments, such as those with Topsin, fail to control the disease, while they can be effective against a different Calonectria species such as C. pseudonaviculata, the cause of boxwood blight.

Effect of fungicides on epiphytic yeasts associated with strawberry

Science.gov (United States)

Debode, Jane; Van Hemelrijck, Wendy; Creemers, Piet; Maes, Martine

2013-01-01

We studied the effect of two commonly used fungicides on the epiphytic yeast community of strawberry. Greenhouse and field experiments were conducted applying Switch (cyprodinil plus fludioxonil) or Signum (boscalid plus pyraclostrobin) to strawberry plants. Yeasts on leaves and fruits were assessed on treated and untreated plants at several time points via plating and denaturing gradient gel electrophoresis (DGGE) analysis. The yeast counts on plates of the treated plants were similar to the control plants. Unripe fruits had 10 times larger yeast concentrations than ripe fruits or leaves. Some dominant yeast types were isolated and in vitro tests showed that they were at least 10 times less sensitive to Switch and Signum as compared with two important fungal strawberry pathogens Botrytis cinerea and Colletotrichum acutatum, which are the targets for the fungicide control. DGGE analysis showed that the applied fungicides had no effect on the composition of the yeast communities, while the growing system, strawberry tissue, and sampling time did affect the yeast communities. The yeast species most commonly identified were Cryptococcus, Rhodotorula, and Sporobolomyces. These results point toward the potential applicability of natural occurring yeast antagonists into an integrated disease control strategy for strawberry diseases.

ApoB-100 secretion by HepG2 cells is regulated by the rate of triglyceride biosynthesis but not by intracellular lipid pools.

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Benoist, F; Grand-Perret, T

1996-10-01

Triglycerides (TGs), cholesteryl esters (CEs), cholesterol, and phosphatidylcholine have been independently proposed as playing regulatory roles in apoB-100 secretion; the results depended on the cellular model used. In this study, we reinvestigate the role of lipids in apoB-100 production in HepG2 cells and in particular, we clarify the respective roles of intracellular mass and the biosynthesis of lipids in the regulation of apoB-100 production. In a first set of experiments, the pool size of cholesterol, CEs, and TGs was modulated by a 3-day treatment with either lipid precursors or inhibitors of enzymes involved in lipid synthesis. We used simvastatin (a hydroxymethylglutaryl coenzyme A reductase inhibitor), 58-035 (an acyl coenzyme A cholesterol acyltransferase inhibitor), 5-tetradecyloxy-2-furancarboxylic acid (TOFA, an inhibitor of fatty acid synthesis), and oleic acid. The secretion rate of apoB-100 was not affected by the large modulation of lipid mass induced by these various pre-treatments. In a second set of experiments, the same lipid modulators were added during a 4-hour labeling period. Simvastatin and 58-035 inhibited cholesterol and CE synthesis without affecting apoB-100 secretion. By contrast, treatment of HepG2 cells with TOFA resulted in the inhibition of TG synthesis and apoB-100 secretion. This effect was highly specific for apoB-100 and was reversed by adding oleic acid, which stimulated both TG synthesis and apoB-100 secretion. Moreover, a combination of oleic acid and 58-035 inhibited CE biosynthesis and increased both TG synthesis and apoB-100 secretion. These results show that in HepG2 cells TG biosynthesis regulates apoB-100 secretion, whereas the rate of cholesterol or CE biosynthesis has no effect.

Resistance of Botrytis cinerea to fungicides controlling gray mold on strawberry in Brazil

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Ueder Pedro Lopes

Full Text Available ABSTRACT The aim of this study was to evaluate the resistance of Botrytis cinerea to the fungicides currently used for its control in Brazil. Isolates of the fungus were collected from different strawberry-producing fields in the states of Espírito Santo, Minas Gerais, and São Paulo, Brazil. First, a total of 183 isolates were identified at the species level using specific primers for the glyceraldehyde-3-phosphate dehydrogenase (G3PDH gene. The isolates were grown on potato dextrose agar (PDA containing the fungicides procymidone, iprodione, and thiophanate-methyl in different concentrations: 0.0 (control, 0.1; 1.0; 10.0; 100.0 and 1,000.0 μg∙mL−1. The percentage of mycelial growth inhibition was used to determine the effective concentration of the fungicide that was able to inhibit colony growth by 50% (EC50. Approximately 25.7% of the isolates were resistant to iprodione, 53.0% were resistant to procymidone, and 93.0% were resistant to thiophanate-methyl. Moreover, crossresistance and multiple resistance were verified, with 19.7% of the isolates showing resistance to 3 fungicides simultaneously. This finding explains the ineffectiveness of fungicides application to control gray mold in strawberry fields in Brazil and highlights the need for new strategies to manage this disease in the culture.

Plastid-to-Nucleus Retrograde Signals Are Essential for the Expression of Nuclear Starch Biosynthesis Genes during Amyloplast Differentiation in Tobacco BY-2 Cultured Cells1[W][OA

Science.gov (United States)

Enami, Kazuhiko; Ozawa, Tomoki; Motohashi, Noriko; Nakamura, Masayuki; Tanaka, Kan; Hanaoka, Mitsumasa

2011-01-01

Amyloplasts, a subtype of plastid, are found in nonphotosynthetic tissues responsible for starch synthesis and storage. When tobacco (Nicotiana tabacum) Bright Yellow-2 cells are cultured in the presence of cytokinin instead of auxin, their plastids differentiate from proplastids to amyloplasts. In this program, it is well known that the expression of nucleus-encoded starch biosynthesis genes, such as ADP-Glucose Pyrophosphorylase (AgpS) and Granule-Bound Starch Synthase (GBSS), is specifically induced. In this study, we investigated the roles of plastid gene expression in amyloplast differentiation. Microarray analysis of plastid genes revealed that no specific transcripts were induced in amyloplasts. Nevertheless, amyloplast development accompanied with starch biosynthesis was drastically inhibited in the presence of plastid transcription/translation inhibitors. Surprisingly, the expression of nuclear AgpS and GBSS was significantly repressed by the addition of these inhibitors, suggesting that a plastid-derived signal(s) that reflects normal plastid gene expression was essential for nuclear gene expression. A series of experiments was performed to examine the effects of intermediates and inhibitors of tetrapyrrole biosynthesis, since some of the intermediates have been characterized as candidates for plastid-to-nucleus retrograde signals. Addition of levulinic acid, an inhibitor of tetrapyrrole biosynthesis, resulted in the up-regulation of nuclear AgpS and GBSS gene expression as well as starch accumulation, while the addition of heme showed opposite effects. Thus, these results indicate that plastid transcription and/or translation are required for normal amyloplast differentiation, regulating the expression of specific nuclear genes by unknown signaling mechanisms that can be partly mediated by tetrapyrrole intermediates. PMID:21771917

Radiotracer studies of fungicide residues in food plants

International Nuclear Information System (INIS)

1990-04-01

Agricultural fungicides are chemicals used on seeds, crops and in soils throughout the growing season. Fungicide treatments may lead to various levels of chemical residues in food commodities. Primary emphasis has been placed on ethylenebisdithiocarbamates (EBDCs), an important group of agrofungicides used in preparations for spraying or dusting major crops such as apples, pears, broccoli, cabbages, egg plants, cauliflower, grapes, lettuce, peppers, celery, cucumbers and tomatoes. Treatments with EBDCs result in terminal residues containing ethylenthiourea (ETU). This is a toxicologically significant decomposition product which has attracted considerable attention in recent years due to indications of its potential goitrogenic and carcinogenic properties. In recognition of the need for a coordinated examination of ETU levels in food, particularly under tropical conditions, the program of radiotracer techniques as a tool for studying fungicide residue problems on food was initiated in 1984. In current studies, three EBDCs, maneb, zineb and mancozeb from different manufacturers in different countries were analysed. This report describes the model protocols (Annexes I, II and III) as they were set up for determination of residues in commodities and soil, using radiotracer and conventional chromatographic techniques . In the 16 papers presented in this report C 14 -labelled EBDCs are determined in plants, vegetables, and soils, before and after cooking, as a function of time and of other agricultural parameters. Refs, figs and tabs

Effects of Fungicide Treatment on Free Amino Acid Concentration and Acrylamide-Forming Potential in Wheat.

Science.gov (United States)

Curtis, Tanya Y; Powers, Stephen J; Halford, Nigel G

2016-12-28

Acrylamide forms from free asparagine and reducing sugars during frying, baking, roasting, or high-temperature processing, and cereal products are major contributors to dietary acrylamide intake. Free asparagine concentration is the determining factor for acrylamide-forming potential in cereals, and this study investigated the effect of fungicide application on free asparagine accumulation in wheat grain. Free amino acid concentrations were measured in flour from 47 varieties of wheat grown in a field trial in 2011-2012. The wheat had been supplied with nitrogen and sulfur and treated with growth regulators and fungicides. Acrylamide formation was measured after the flour had been heated at 180 °C for 20 min. Flour was also analyzed from 24 (of the 47) varieties grown in adjacent plots that were treated in identical fashion except that no fungicide was applied, resulting in visible infection by Septoria tritici, yellow rust, and brown rust. Free asparagine concentration in the fungicide-treated wheat ranged from 1.596 to 3.987 mmol kg -1 , with a significant (p fungicide treatment, the increases in acrylamide ranging from 2.7 to 370%. Free aspartic acid concentration also increased, whereas free glutamic acid concentration increased in some varieties but decreased in others, and free proline concentration decreased. The study showed disease control by fungicide application to be an important crop management measure for mitigating the problem of acrylamide formation in wheat products.

Effects of azole fungicides on the function of sex and thyroid hormones

DEFF Research Database (Denmark)

Kjærstad, Mia Birkhøj; Andersen, Helle Raun; Taxvig, Camilla

Resumé: Azole-fungicides are frequently used in Denmark. Epoxiconazole, propiconazole, and tebuconazole had endocrine disrupting properties in cell based assays. In rats, epoxiconazole and tebuconazole increased gestational length, maternal progesterone level, and masculinized female-offspring. B......-offspring. Besides, tebuconazole caused feminization of male-offspring. Similar effects were previously demonstrated for prochloraz. The results indicate that azole-fungicides in general have endocrine disrupting properties...

Effectiveness of Different Classes of Fungicides on Botrytis cinerea Causing Gray Mold on Fruit and Vegetables

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Joon-Oh Kim

2016-12-01

Full Text Available Botrytis cinerea is a necrotrophic pathogen causing a major problem in the export and post-harvest of strawberries. Inappropriate use of fungicides leads to resistance among fungal pathogens. Therefore, it is necessary to evaluate the sensitivity of B. cinerea to various classes of fungicide and to determine the effectiveness of different concentrations of commonly used fungicides. We thus evaluated the effectiveness of six classes of fungicide in inhibiting the growth and development of this pathogen, namely, fludioxonil, iprodione, pyrimethanil, tebuconazole, fenpyrazamine, and boscalid. Fludioxonil was the most effective (EC₅₀ < 0.1 μg/ml, and pyrimethanil was the least effective (EC₅₀ = 50 μg/ml, at inhibiting the mycelial growth of B. cinerea. Fenpyrazamine and pyrimethanil showed relatively low effectiveness in inhibiting the germination and conidial production of B. cinerea. Our results are useful for the management of B. cinerea and as a basis for monitoring the sensitivity of B. cinerea strains to fungicides.

Effectiveness of fungicides in protecting Douglas-fir shoots from infection by Phytophthora ramorum

Science.gov (United States)

G.A. Chastagner; E.M. Hansen; K.L. Riley; W. Sutton

2006-01-01

The effectiveness of 20 systemic and contact fungicides in protecting Douglas-fir seedlings from infection by Phytophthora ramorum was determined. Some systemic products were applied about a week prior to bud break, while most treatments were applied just after bud break. In addition to the fungicides, two surfactants were included in the post-bud...

Synthesis of Novel (E) -α-(methoxyimino) Benzeneacetate Derivatives and their Fungicidal Activities

International Nuclear Information System (INIS)

Wang, X.; Chen, P.; Pang, Y.; Zhao, Z.; Wu, G.; Wang, H.

2015-01-01

In order to find novel strobilurin derivatives with good fungicidal activities, a series of (E)-α-(methoxyimino)benzeneacetate analogues containing 1,2,4-triazole Schiff base moiety were designed and synthesized. Their structures were confirmed by IR,1H-NMR, HRMS or elemental analyses. The antifungal activities indicated that compounds 6 showed moderate to good fungicidal activities against Rhizoctonia solani, Botrytis cinereapers, Fusarium graminearum and Blumeria graminis at the concentration 50 μ g/mL. For example, compounds 6e and 6h exhibited promising antifungal activity against Rhizoctonia solani, Botrytis cinereapers and Fusarium graminearum. Compounds 6g and 6j had higher fungicidal activities against Blumeria graminis at the concentration of 50 μ g/ml, inhibitory rate is 95.32 percentage and 89.67 percentage, respectively. (author)

Degradation of three fungicides following application on strawberry and a risk assessment of their toxicity under greenhouse conditions.

Science.gov (United States)

Sun, Caixia; Cang, Tao; Wang, Zhiwei; Wang, Xinquan; Yu, Ruixian; Wang, Qiang; Zhao, Xueping

2015-05-01

The health risk to humans of pesticide application on minor crops, such as strawberry, requires quantification. Here, the dissipation and residual levels of three fungicides (pyraclostrobin, myclobutanil, and difenoconazole) were studied for strawberry under greenhouse conditions using high-performance liquid chromatography (HPLC)-tandem mass spectrometry after Quick, Easy, Cheap, Effective, Rugged, and Safe extraction. This method was validated using blank samples, with all mean recoveries of these three fungicides exceeding 80%. The residues of all three fungicides dissipated following first-order kinetics. The half-lives of pyraclostrobin, myclobutanil, and difenoconazole were 1.69, 3.30, and 3.65 days following one time application and 1.73, 5.78, and 6.30 days following two times applications, respectively. Fungicide residue was determined by comparing the estimated daily intake of the three fungicides against the acceptable daily intake. The results indicate that the potential health risk of the three fungicides was not significant in strawberry when following good agricultural practices (GAP) under greenhouse conditions.

Fungicide Efficacy in Peach Rusty Spot Control in Serbia

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Nenad Dolovac

2010-01-01

Full Text Available Rusty Spot has long been known as a harmful peach disease in many parts of the world. During the past several years, rusty spot infection of the late-maturing peach cultivars (Summerset, Suncrest, Fayette and O’Henry caused significant yield losses in Serbia.Although the etiology of the disease is still unknown, there are numerous studies attempting to set a strategy for its control and recommend appropriate chemical and other peach protection methods. However, because of specific environmental conditions in Serbia, recommended protection method using repeated fungicide treatments, starting from petal fall, did not prove to be efficient and the rate of infection in some susceptible peach cultivars reached 100%. In 2003 and 2004 a field trial was conducted in order to test the efficacy of fungicides (a.i. kresoxim-methyl, flusilazole and sulfur for the efficient control of Rusty Spot epidemics. The trial was carried out under conditions of natural infection on the peach cv. Summerset at the locality of Bela Crkva, Serbia. In the ntreated control plots,high disease incidence was recorded with the percentage of affected fruit surface ranging from 33.5% in the first, up to the 35.4% in the second year of the trail. Among fungicides included in the trial, kresoxim-methyl proved to be the most efficient (90.25% in the first and 91.12% in the second year of the trial, flusilazole exhibited lower efficacy (87.28% and 80.61%, respectively while sulfur was the least efficient 82.33% and 80.30%, respectively. Determination of the most efficient fungicide for the peach rusty spot control in Serbia provides basic nformation for further investigations which will include optimization of treatment terms, as well as additional agro-technical control measures.

Esterase isozymes patterns of grape vine (Vitis vinifera L. are altered in response to fungicide exposure

Directory of Open Access Journals (Sweden)

Gleice Ribeiro Orasmo

2015-10-01

Full Text Available Current analysis characterizes the effect of different fungicides often applied for pest control on a-and b-esterase patterns of four economically important table-wine grape cultivars (Italia, Rubi, Benitaka and Brasil of Vitis vinifera. The a- and b-esterase patterns in bud leaves of the cultivars were assessed by native PAGE analysis. Cabrio Top® compound inhibited Est-2, Est-5, Est-6, Est-7, Est-8, Est-9 and Est-10 carboxylesterases, whereas Est-4, Est-11, Est-12, Est-13, Est-14 acetylesterases and Est-16 carboxylesterase were detected as weakly stained bands. Carboxylesterases and acetylesterases were also detected as weakly stained bands when exposed to fungicides Orthocide 500®, Positron Duo® and Folicur PM®. No changes in a- and b-esterase patterns were reported when the vines were exposed to the fungicides Rovral SC®, Kumulus DF®, Curzate M®, Score® or Cuprogarb 500®. The evidence of functional changes in carboxylesterase and acetylesterase levels in current study is a warning to grape producers on the dangers inherent in the indiscriminate use of potent and modern fungicides extensively used in agriculture. The inhibition effect of fungicides on esterase isozyme molecules seems to be independent of the fungicide chemical.

2-Fluoro-L-Fucose Is a Metabolically Incorporated Inhibitor of Plant Cell Wall Polysaccharide Fucosylation

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Wallace, Ian S.

2015-01-01

The monosaccharide L-fucose (L-Fuc) is a common component of plant cell wall polysaccharides and other plant glycans, including the hemicellulose xyloglucan, pectic rhamnogalacturonan-I (RG-I) and rhamnogalacturonan-II (RG-II), arabinogalactan proteins, and N-linked glycans. Mutations compromising the biosynthesis of many plant cell wall polysaccharides are lethal, and as a result, small molecule inhibitors of plant cell wall polysaccharide biosynthesis have been developed because these molecules can be applied at defined concentrations and developmental stages. In this study, we characterize novel small molecule inhibitors of plant fucosylation. 2-fluoro-L-fucose (2F-Fuc) analogs caused severe growth phenotypes when applied to Arabidopsis seedlings, including reduced root growth and altered root morphology. These phenotypic defects were dependent upon the L-Fuc salvage pathway enzyme L-Fucose Kinase/ GDP-L-Fucose Pyrophosphorylase (FKGP), suggesting that 2F-Fuc is metabolically converted to the sugar nucleotide GDP-2F-Fuc, which serves as the active inhibitory molecule. The L-Fuc content of cell wall matrix polysaccharides was reduced in plants treated with 2F-Fuc, suggesting that this molecule inhibits the incorporation of L-Fuc into these polysaccharides. Additionally, phenotypic defects induced by 2F-Fuc treatment could be partially relieved by the exogenous application of boric acid, suggesting that 2F-Fuc inhibits RG-II biosynthesis. Overall, the results presented here suggest that 2F-Fuc is a metabolically incorporated inhibitor of plant cellular fucosylation events, and potentially suggest that other 2-fluorinated monosaccharides could serve as useful chemical probes for the inhibition of cell wall polysaccharide biosynthesis. PMID:26414071

[In vitro susceptibility of Trichoconiella padwickii to various active ingredients used as fungicides in the cultivation of rice].

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Lovato Echeverria, Alfonso D; Gutiérrez, Susana A; Carmona, Marcelo A

The aim of this study was to evaluate in vitro the mycelial susceptibility of Trichoconiella padwickii to different active ingredients through average median concentration IC 50 calculation. Inoculum disks were seeded on bean agar at different concentrations (0.1; 1; 10; 30, 50; 100 and 1000mg/l) of various fungicides. After seven days the colony diameter was measured. The data obtained were fitted to nonlinear regression models. Susceptibility was classified using the scale proposed by Edgington. The results show that the pathogen is very sensitive to products that act on the respiratory chain (quinone outside inhibitors [QoI] and succinate dehydrogenase inhibitors [SDHI]) and cell membrane (multi-site contact activity), and moderately sensitive to those products interfering with cell division (methyl benzimidazole carbamates [MBC]), synthesis of nucleic acids (phenylamides [PA]) and osmotic signal transduction (multi-site contact activity). This work is the first record on the sensitivity of T. padwickii. Copyright © 2017 Asociación Argentina de Microbiología. Publicado por Elsevier España, S.L.U. All rights reserved.

3-cyanoindole-based inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.

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Dhar, T G Murali; Shen, Zhongqi; Gu, Henry H; Chen, Ping; Norris, Derek; Watterson, Scott H; Ballentine, Shelley K; Fleener, Catherine A; Rouleau, Katherine A; Barrish, Joel C; Townsend, Robert; Hollenbaugh, Diane L; Iwanowicz, Edwin J

2003-10-20

A series of novel small molecule inhibitors of inosine monophosphate dehydrogenase (IMPDH), based upon a 3-cyanoindole core, were explored. IMPDH catalyzes the rate determining step in guanine nucleotide biosynthesis and is a target for anticancer, immunosuppressive and antiviral therapy. The synthesis and the structure-activity relationships (SAR), derived from in vitro studies, for this new series of inhibitors is given.

Synthesis and Fungicidal activity of some sulphide derivatives of O-Ethyl-N-substituted phenylcarbamates

International Nuclear Information System (INIS)

Imeokparia, F.A.

2006-01-01

Monosulphides of O-ethyl-N-substituted phenylcarbamates were prepared by the reaction between O-ethyl-N-substituted phenylcarbamates and sulphur dichloride, while the corresponding disulphides were prepared by the reaction between O-ethyl-N-substituted phenylcarbamates and sulphur monochloride. The synthesized compounds were characterized by elemental analysis, thin layer chromatography (TLC), Fourier-transform infrared, and /sup 1/H and /sup 13/C nuclear magnetic resonance spectroscopic techniques. In vitro fungicidal assay of these sulphides against Fusarium oxysporum, Aspergillus niger, Aspergillus flavus and Rhizopus stolonifer showed that they had Greater fungicidal activity than their parent carbamates. The synthesized sulphides were more active towards A. Niger and A. flavus. Unlike the parent carbamates, the type of substituents attached to the aromatic nucleus of these sulphides had little or no effect on their fungicidal activity as there was insignificant variation in the fungicidal activity of the monosulphide and the disulphide derivatives of O-ethyl-N-substituted phenylcarbamates. (author)

Herbicidal and Fungicidal Activities of Lactones in Kava (Piper methysticum).

Science.gov (United States)

Xuan, T D; Elzaawely, A A; Fukuta, M; Tawata, S

2006-02-08

This is the first report showing that kava lactones are plant and plant fungus growth inhibitors. Aqueous extract of kava roots showed high allelopathic potential and strongly suppressed germination and growth of lettuce, radish, barnyardgrass, and monochoria. Nine kava lactones were detected using GC-MS including desmethoxyyagonin, kavain, 7,8-dihydrokavain, hydroxykavain, yagonin, 5,6,7,8-tetrahydroxyyagonin, methysticin, dihydromethysticin, and 11-hydroxy-12-methoxydihydrokavain. Quantities of desmethoxyyagonin, kavain, 7,8-dihydrokavain, yagonin, methysticin, and dihydromethysticin detected were 4.3, 6.9, 18.6, 5.7, 1.4, and 5.4 mg/g of dry weight, respectively. These six major lactones in kava roots showed great herbicidal and antifungal activities. Growth of lettuce and barnyardgrass were significantly inhibited at 1-10 ppm, and four plant fungi including Colletotrichum gloeosporides, Fusarium solani, Fusarium oxysporum, and Trichoderma viride were significantly inhibited at 10-50 ppm. The biological activities of kava lactones were characterized by different double-bond linkage patterns in positions 5,6 and 7,8. The findings of this study suggest that kava lactones may be useful for the development of bioactive herbicides and fungicides.

Corn silage from corn treated with foliar fungicide and performance of Holstein cows.

Science.gov (United States)

Haerr, K J; Lopes, N M; Pereira, M N; Fellows, G M; Cardoso, F C

2015-12-01

Foliar fungicide application to corn plants is used in corn aimed for corn silage in the dairy industry, but questions regarding frequency of application and its effect on corn silage quality and feed conversion when fed to dairy cows remain prevalent. The objective of this study was to evaluate the effects of various foliar fungicide applications to corn on dry matter intake (DMI), milk production, and milk composition when fed to dairy cows. Sixty-four Holstein cows with parity 2.5±1.5, 653±80kg of body weight, and 161±51d in milk were blocked and randomly assigned to 1 of 4 corn silage treatments (total mixed ration with 35% of the dry matter as corn silage). Treatments were as follows: control (CON), corn silage with no applications of foliar fungicide; treatment 1 (1X), corn silage from corn that received 1 application of pyraclostrobin (PYR) foliar fungicide (Headline; BASF Corp.) at corn vegetative stage 5; treatment 2 (2X), corn silage from corn that received the same application as 1X plus another application of a mixture of PYR and metconazole (Headline AMP; BASF Corp.) at corn reproductive stage 1 ("silking"); and treatment 3 (3X), corn silage from corn that received the same applications as 2X as well as a third application of PYR and metconazole at reproductive stage 3 ("milky kernel"). Corn was harvested at about 32% dry matter and 3/4 milk line stage of kernel development and ensiled for 200d. Treatments were fed to cows for 5wk, with the last week being used for statistical inferences. Week -1 was used as a covariate in the statistical analysis. Dry matter intake tended to be lower for cows fed corn silage treated with fungicide than CON (23.8, 23.0, 19.5, and 21.3kg for CON, 1X, 2X, and 3X, respectively). A linear treatment effect for DMI was observed, with DMI decreasing as foliar fungicide applications increased. Treatments CON, 1X, 2X, and 3X did not differ for milk yield (34.5, 34.5, 34.2, and 34.4kg/d, respectively); however, a trend for

Virtual screening for potential inhibitors of bacterial MurC and MurD ligases.

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Tomašić, Tihomir; Kovač, Andreja; Klebe, Gerhard; Blanot, Didier; Gobec, Stanislav; Kikelj, Danijel; Mašič, Lucija Peterlin

2012-03-01

Mur ligases are bacterial enzymes involved in the cytoplasmic steps of peptidoglycan biosynthesis and are viable targets for antibacterial drug discovery. We have performed virtual screening for potential ATP-competitive inhibitors targeting MurC and MurD ligases, using a protocol of consecutive hierarchical filters. Selected compounds were evaluated for inhibition of MurC and MurD ligases, and weak inhibitors possessing dual inhibitory activity have been identified. These compounds represent new scaffolds for further optimisation towards multiple Mur ligase inhibitors with improved inhibitory potency.

Disruption of Sphingolipid Biosynthesis Blocks Phagocytosis of Candida albicans.

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Fikadu G Tafesse

2015-10-01

Full Text Available The ability of phagocytes to clear pathogens is an essential attribute of the innate immune response. The role of signaling lipid molecules such as phosphoinositides is well established, but the role of membrane sphingolipids in phagocytosis is largely unknown. Using a genetic approach and small molecule inhibitors, we show that phagocytosis of Candida albicans requires an intact sphingolipid biosynthetic pathway. Blockade of serine-palmitoyltransferase (SPT and ceramide synthase-enzymes involved in sphingolipid biosynthesis- by myriocin and fumonisin B1, respectively, impaired phagocytosis by phagocytes. We used CRISPR/Cas9-mediated genome editing to generate Sptlc2-deficient DC2.4 dendritic cells, which lack serine palmitoyl transferase activity. Sptlc2-/- DC2.4 cells exhibited a stark defect in phagocytosis, were unable to bind fungal particles and failed to form a normal phagocytic cup to engulf C. albicans. Supplementing the growth media with GM1, the major ganglioside present at the cell surface, restored phagocytic activity of Sptlc2-/- DC2.4 cells. While overall membrane trafficking and endocytic pathways remained functional, Sptlc2-/- DC2.4 cells express reduced levels of the pattern recognition receptors Dectin-1 and TLR2 at the cell surface. Consistent with the in vitro data, compromised sphingolipid biosynthesis in mice sensitizes the animal to C. albicans infection. Sphingolipid biosynthesis is therefore critical for phagocytosis and in vivo clearance of C. albicans.

Arabidopsis DREB2C modulates ABA biosynthesis during germination.

Science.gov (United States)

Je, Jihyun; Chen, Huan; Song, Chieun; Lim, Chae Oh

2014-09-12

Plant dehydration-responsive element binding factors (DREBs) are transcriptional regulators of the APETELA2/Ethylene Responsive element-binding Factor (AP2/ERF) family that control expression of abiotic stress-related genes. We show here that under conditions of mild heat stress, constitutive overexpression seeds of transgenic DREB2C overexpression Arabidopsis exhibit delayed germination and increased abscisic acid (ABA) content compared to untransformed wild-type (WT). Treatment with fluridone, an inhibitor of the ABA biosynthesis abrogated these effects. Expression of an ABA biosynthesis-related gene, 9-cis-epoxycarotenoid dioxygenase 9 (NCED9) was up-regulated in the DREB2C overexpression lines compared to WT. DREB2C was able to trans-activate expression of NCED9 in Arabidopsis leaf protoplasts in vitro. Direct and specific binding of DREB2C to a complete DRE on the NCED9 promoter was observed in electrophoretic mobility shift assays. Exogenous ABA treatment induced DREB2C expression in germinating seeds of WT. Vegetative growth of transgenic DREB2C overexpression lines was more strongly inhibited by exogenous ABA compared to WT. These results suggest that DREB2C is a stress- and ABA-inducible gene that acts as a positive regulator of ABA biosynthesis in germinating seeds through activating NCED9 expression. Copyright © 2014 Elsevier Inc. All rights reserved.

Changes in antioxidants potential, secondary metabolites and plant hormones induced by different fungicides treatment in cotton plants.

Science.gov (United States)

Mohamed, Heba Ibrahim; Akladious, Samia Ageeb

2017-10-01

The use of fungicides for an effective control of plant diseases has become crucial in the last decades in the agriculture system. Seeds of cotton plants were treated with systemic and contact fungicides to study the efficiency of seed dressing fungicides in controlling damping off caused by Rhizoctonia solani under greenhouse conditions and its effect on plant growth and metabolism. The results showed that Mon-cut showed the highest efficiency (67.99%) while each of Tondro and Hemixet showed the lowest efficiency (31.99%) in controlling damping off. Rhizolex T, Mon-cut and Tondro fungicides caused significant decrease in plant height, dry weight of plant, phytohormones, photosynthetic pigments, soluble sugars, soluble proteins, total free amino acids but caused significant increases in total phenols, flavonoids, antioxidant enzymes, ascorbic acid, reduced glutathione, MDA and hydrogen peroxide as compared with untreated plants. On the other hand, the other fungicides (Maxim, Hemixet and Flosan) increased all the above recorded parameters as compared with untreated plants. Our results indicated that the fungicides application could be a potential tool to increase plant growth, the antioxidative defense mechanisms and decreased infection with plant diseases. Copyright © 2017 Elsevier B.V. All rights reserved.

Marked radiosensitization of cells in culture to x ray by 5-chlorodeoxycytidine coadministered with tetrahydrouridine, and inhibitors of pyrimidine biosynthesis

International Nuclear Information System (INIS)

Perez, L.M.; Mekras, J.A.; Briggle, T.V.; Greer, S.

1984-01-01

The authors approach to overcome the problem of rapid catabolism and general toxicity encountered with 5-halogenated analogues of deoxyuridine (5-bromo, chloro or iododeoxyuridine), which has limited their use as tumor radiosensitizers, is to utilize 5-chlorodeoxycytidine (CldC) with tetrahydrouridine (H 4 U). They propose that CldC, coadministered with H 4 U, is metabolized in the following manner: CldC → CldCMP → CldUMP → → CldUTP → DNA. All the enzymes of this pathway are elevated in many human malignant tumors and in HEp-2 cells. In x irradiation studies with HEp-2 cells, limited to 1 or 2 radiation doses. They obtained 3.0 to 3.8 apparent dose enhancement ratios when cells were preincubated with inhibitors of pyrimidine biosynthesis. Enzymatic studies indicate that this toxicity may be tumor selective. Preliminary toxicity studies indicate that mice will tolerate treatment protocols with marginal weight loss (4%). In this approach the authors seek to obtain preferential conversion of CldC to CldUTP at the tumor site by taking advantage of quantitative differences in enzyme levels between tumors and normal tissues

Fungicide application and phosphorus uptake by hyphae of arbuscular mycorrhizal fungi into field-grown peas

DEFF Research Database (Denmark)

Schweiger, P.F.; Spliid, N.H.; Jakobsen, I.

2001-01-01

The effect of two commercial fungicide formulations on phosphorus (P) uptake into peas via hyphae of a native arbuscular mycorrhizal (AM) fungal community was examined in the field. The fungicides contained carbendazim or a mixture of propiconazole and fenpropimorph as their active ingredients...... from overall P uptake, Fungicides were added to the soil inside the HCs at concentrations assumed to reflect their concentration in the surrounding soil. At two harvests, plant growth, total P and P-32 uptake as well as root length density and AM root colonisation were measured. Length of hyphae inside...

Using Epidemiological Principles to Explain Fungicide Resistance Management Tactics: Why do Mixtures Outperform Alternations?

Science.gov (United States)

Elderfield, James A D; Lopez-Ruiz, Francisco J; van den Bosch, Frank; Cunniffe, Nik J

2018-07-01

Whether fungicide resistance management is optimized by spraying chemicals with different modes of action as a mixture (i.e., simultaneously) or in alternation (i.e., sequentially) has been studied by experimenters and modelers for decades. However, results have been inconclusive. We use previously parameterized and validated mathematical models of wheat Septoria leaf blotch and grapevine powdery mildew to test which tactic provides better resistance management, using the total yield before resistance causes disease control to become economically ineffective ("lifetime yield") to measure effectiveness. We focus on tactics involving the combination of a low-risk and a high-risk fungicide, and the case in which resistance to the high-risk chemical is complete (i.e., in which there is no partial resistance). Lifetime yield is then optimized by spraying as much low-risk fungicide as is permitted, combined with slightly more high-risk fungicide than needed for acceptable initial disease control, applying these fungicides as a mixture. That mixture rather than alternation gives better performance is invariant to model parameterization and structure, as well as the pathosystem in question. However, if comparison focuses on other metrics, e.g., lifetime yield at full label dose, either mixture or alternation can be optimal. Our work shows how epidemiological principles can explain the evolution of fungicide resistance, and also highlights a theoretical framework to address the question of whether mixture or alternation provides better resistance management. It also demonstrates that precisely how spray tactics are compared must be given careful consideration. [Formula: see text] Copyright © 2018 The Author(s). This is an open access article distributed under the CC BY 4.0 International license .

Meta-analysis of yield response of hybrid field corn to foliar fungicides in the U.S. Corn Belt.

Science.gov (United States)

Paul, P A; Madden, L V; Bradley, C A; Robertson, A E; Munkvold, G P; Shaner, G; Wise, K A; Malvick, D K; Allen, T W; Grybauskas, A; Vincelli, P; Esker, P

2011-09-01

The use of foliar fungicides on field corn has increased greatly over the past 5 years in the United States in an attempt to increase yields, despite limited evidence that use of the fungicides is consistently profitable. To assess the value of using fungicides in grain corn production, random-effects meta-analyses were performed on results from foliar fungicide experiments conducted during 2002 to 2009 in 14 states across the United States to determine the mean yield response to the fungicides azoxystrobin, pyraclostrobin, propiconazole + trifloxystrobin, and propiconazole + azoxystrobin. For all fungicides, the yield difference between treated and nontreated plots was highly variable among studies. All four fungicides resulted in a significant mean yield increase relative to the nontreated plots (P pyraclostrobin (256 kg/ha), and lowest for azoxystrobin (230 kg/ha). Baseline yield (mean yield in the nontreated plots) had a significant effect on yield for propiconazole + azoxystrobin (P pyraclostrobin, propiconazole + trifloxystrobin, and propiconazole + azoxystrobin but not to azoxystrobin. Mean yield difference was generally higher in the lowest yield and higher disease severity categories than in the highest yield and lower disease categories. The probability of failing to recover the fungicide application cost (p(loss)) also was estimated for a range of grain corn prices and application costs. At the 10-year average corn grain price of $0.12/kg ($2.97/bushel) and application costs of $40 to 95/ha, p(loss) for disease severity pyraclostrobin, 0.62 to 0.93 for propiconazole + trifloxystrobin, 0.58 to 0.89 for propiconazole + azoxystrobin, and 0.91 to 0.99 for azoxystrobin. When disease severity was >5%, the corresponding probabilities were 0.36 to 95, 0.25 to 0.69, 0.25 to 0.64, and 0.37 to 0.98 for the four fungicides. In conclusion, the high p(loss) values found in most scenarios suggest that the use of these foliar fungicides is unlikely to be profitable when

Occurrence and persistence of fungicides in bed sediments and suspended solids from three targeted use areas in the United States.

Science.gov (United States)

Smalling, Kelly L; Reilly, Timothy J; Sandstrom, Mark W; Kuivila, Kathryn M

2013-03-01

To document the environmental occurrence and persistence of fungicides, a robust and sensitive analytical method was used to measure 34 fungicides and an additional 57 current-use pesticides in bed sediments and suspended solids collected from areas of intense fungicide use within three geographic areas across the United States. Sampling sites were selected near or within agricultural research farms using prophylactic fungicides at rates and types typical of their geographic location. At least two fungicides were detected in 55% of the bed and 83% of the suspended solid samples and were detected in conjunction with herbicides and insecticides. Six fungicides were detected in all samples including pyraclostrobin (75%), boscalid (53%), chlorothalonil (41%) and zoxamide (22%). Pyraclostrobin, a strobilurin fungicide, used frequently in the United States on a variety of crops, was detected more frequently than p,p'-DDE, the primary degradate of p,p'-DDT, which is typically one of the most frequently occurring pesticides in sediments collected within highly agricultural areas. Maximum fungicide concentrations in bed sediments and suspended solids were 198 and 56.7 μg/kg dry weight, respectively. There is limited information on the occurrence, fate, and persistence of many fungicides in sediment and the environmental impacts are largely unknown. The results of this study indicate the importance of documenting the persistence of fungicides in the environment and the need for a better understanding of off-site transport mechanisms, particularly in areas where crops are grown that require frequent treatments to prevent fungal diseases. Published by Elsevier B.V.

Method for in vitro screening of aquatic fungicides

Science.gov (United States)

Bailey, T.A.

1983-01-01

Methods were developed for in vitro screening of candidate aquatic fungicides for efficacy against Achlya fiagellata, A. racemosa, Saprolegnia hypogyna and S. megasperma. Agar plugs containing fungal hyphae, removed from the edge of actively growing colonies, were placed in the depressions of spot plates containing 1a??0, 10a??0 and 100 mg/I of the candidate compounds for 15 or 60 min. After exposure, the plugs were transferred on to filter papers (0a??45-A?m pore) in a holder, rinsed, and then placed on cornmeal agar medium in tri-petri dishes. The plates were checked for mycelial growth after 48, 96 and 168 h of incubation in a lighted (400-800 A?m) environmental control chamber at 20A?2A?C. Criteria for the acceptance or rejection of candidate aquatic fungicides for further study were based on the antifungal spectrum index (ASI) comparisons between respective compounds and malachite green after 48 h and the concentration level producing complete growth inhibition. Candidate compounds whose ASI was less than 50% that of malachite green after 48 h or did not inhibit growth at levels less than 100 mg/l were rejected. This method provides a base from which in vivo and definitive test regimens can be developed. Preliminary in vitro screening of candidate fungicides reduces the need for costly in vivo tests on compounds that have low antifungal activity.

[The inhibitor of free radical processes decrease of protein biosynthesis in gun short wound tissues and weaken development of the general adaptation syndrome].

Science.gov (United States)

Todorov, I N; Bogdanov, G N; Mitrokhin, Iu I; Varfolomeev, V N; Sidorenko, L I; Mishchenko, D V

2006-01-01

The dynamics of total protein biosynthesis and procollagen biosynthesis in skeletal muscle of injury tissues with the antioxidant BHT (dibunol) treatment and with common healing were studied. The obtained date indicate that the AO treatment reduce the rate of biosynthesis both the total proteins and procollagen at the 3th day of healing. Dibunol also considerably reduce the protein biosynthesis in adrenals and brake of corticosteroids biogenesis as measured by ESR-signals intensity of reduced adrenodoxine. AO treatment also reduce the protein biosynthesis in thymus, spleen and bone marrow. The lowering of functional activity of endocrine and immune systems indicate that the AO significantly inhibit the systemic reactions of organism induced by acute wound affect. It was suggested that as "primary mediator" of stress-reaction may be considered lipoperoxide radicals and decay products of lipohydroperoide.

Multiple resistance of Botrytis cinerea from kiwifruit to SDHIs, QoIs and fungicides of other chemical groups.

Science.gov (United States)

Bardas, George A; Veloukas, Thomas; Koutita, Olga; Karaoglanidis, George S

2010-09-01

Botrytis cinerea Pers.: Fr. is a high-risk pathogen for fungicide resistance development that has caused resistance problems on many crops throughout the world. This study investigated the fungicide sensitivity profile of isolates from kiwifruits originating from three Greek locations with different fungicide use histories. Sensitivity was measured by in vitro fungitoxicity tests on artificial nutrient media. Seventy-six single-spore isolates were tested for sensitivity to the SDHI fungicide boscalid, the QoI pyraclostrobin, the anilinopyrimidine cyprodinil, the hydroxyanilide fenhexamid, the phenylpyrrole fludioxonil, the dicarboxamide iprodione and the benzimidazole carbendazim. All isolates from Thessaloniki showed resistance to both boscalid and pyraclostrobin, while in the other two locations the fungal population was sensitive to these two fungicides. Sensitive isolates showed EC(50) values to boscalid and pyraclostrobin ranging from 0.9 to 5.2 and from 0.04 to 0.14 mg L(-1) respectively, while the resistant isolates showed EC(50) values higher than 50 mg L(-1) for boscalid and from 16 to > 50 mg L(-1) for pyraclostrobin. All QoI-resistant isolates carried the G143A mutation in cytb. Sensitivity determinations to the remaining fungicides revealed in total eight resistance phenotypes. No isolates were resistant to the fungicides fenhexamid and fludioxonil. This is the first report of B. cinerea field isolates with resistance to both boscalid and pyraclostrobin, and it strongly suggests that there may be a major problem in controlling this important pathogen on kiwifruit. (c) 2010 Society of Chemical Industry.

Amino acid precursor supply in the biosynthesis of the RNA polymerase inhibitor streptolydigin by Streptomyces lydicus.

Science.gov (United States)

Gómez, Cristina; Horna, Dina H; Olano, Carlos; Palomino-Schätzlein, Martina; Pineda-Lucena, Antonio; Carbajo, Rodrigo J; Braña, Alfredo F; Méndez, Carmen; Salas, José A

2011-08-01

Biosynthesis of the hybrid polyketide-nonribosomal peptide antibiotic streptolydigin, 3-methylaspartate, is utilized as precursor of the tetramic acid moiety. The three genes from the Streptomyces lydicus streptolydigin gene cluster slgE1-slgE2-slgE3 are involved in 3-methylaspartate supply. SlgE3, a ferredoxin-dependent glutamate synthase, is responsible for the biosynthesis of glutamate from glutamine and 2-oxoglutarate. In addition to slgE3, housekeeping NADPH- and ferredoxin-dependent glutamate synthase genes have been identified in S. lydicus. The expression of slgE3 is increased up to 9-fold at the onset of streptolydigin biosynthesis and later decreases to ∼2-fold over the basal level. In contrast, the expression of housekeeping glutamate synthases decreases when streptolydigin begins to be synthesized. SlgE1 and SlgE2 are the two subunits of a glutamate mutase that would convert glutamate into 3-methylaspartate. Deletion of slgE1-slgE2 led to the production of two compounds containing a lateral side chain derived from glutamate instead of 3-methylaspartate. Expression of this glutamate mutase also reaches a peak increase of up to 5.5-fold coinciding with the onset of antibiotic production. Overexpression of either slgE3 or slgE1-slgE2 in S. lydicus led to an increase in the yield of streptolydigin.

Effects of 2 fungicide formulations on microbial and macroinvertebrate leaf decomposition under laboratory conditions

Science.gov (United States)

Elskus, Adria; Smalling, Kelly L.; Hladik, Michelle; Kuivila, Kathryn

2016-01-01

Aquatic fungi contribute significantly to the decomposition of leaves in streams, a key ecosystem service. However, little is known about the effects of fungicides on aquatic fungi and macroinvertebrates involved with leaf decomposition. Red maple (Acer rubrum) leaves were conditioned in a stream to acquire microbes (bacteria and fungi), or leached in tap water (unconditioned) to simulate potential reduction of microbial biomass by fungicides. Conditioned leaves were exposed to fungicide formulations QUILT (azoxystrobin + propiconazole) or PRISTINE (boscalid + pyraclostrobin), in the presence and absence of the leaf shredder, Hyalella azteca (amphipods; 7-d old at start of exposures) for 14 d at 23 °C. QUILT formulation (~ 0.3 μg/L, 1.8 μg/L, 8 μg/L) tended to increase leaf decomposition by amphipods (not significant) without a concomitant increase in amphipod biomass, indicating potential increased consumption of leaves with reduced nutritional value. PRISTINE formulation (~ 33 μg/L) significantly reduced amphipod growth and biomass (p<0.05), effects similar to those observed with unconditioned controls. The significant suppressive effects of PRISTINE on amphipod growth, and the trend towards increased leaf decomposition with increasing QUILT concentration, indicate the potential for altered leaf decay in streams exposed to fungicides. Further work is needed to evaluate fungicide effects on leaf decomposition under conditions relevant to stream ecosystems, including temperature shifts and pulsed exposures to pesticide mixtures.

Occurrence of boscalid and other selected fungicides in surface water and groundwater in three targeted use areas in the United States.

Science.gov (United States)

Reilly, Timothy J; Smalling, Kelly L; Orlando, James L; Kuivila, Kathryn M

2012-09-01

To provide an assessment of the occurrence of fungicides in water resources, the US Geological Survey used a newly developed analytical method to measure 33 fungicides and an additional 57 current-use pesticides in water samples from streams, ponds, and shallow groundwater in areas of intense fungicide use within three geographic areas across the United States. Sampling sites were selected near or within farms using prophylactic fungicides at rates and types typical of their geographic location. At least one fungicide was detected in 75% of the surface waters and 58% of the groundwater wells sampled. Twelve fungicides were detected including boscalid (72%), azoxystrobin (51%), pyraclostrobin (40%), chlorothalonil (38%) and pyrimethanil (28%). Boscalid, a carboxamide fungicide registered for use in the US in 2003, was detected more frequently than atrazine and metolachlor, two herbicides that are typically the most frequently occurring pesticides in many large-scale water quality studies. Fungicide concentrations ranged from less than the method detection limit to approximately 2000 ngL(-1). Currently, limited toxicological data for non-target species exists and the environmental impacts are largely unknown. The results of this study indicate the importance of including fungicides in pesticide monitoring programs, particularly in areas where crops are grown that require frequent treatments to prevent fungal diseases. Published by Elsevier Ltd.

Analysis of Fungicide Sensitivity and Genetic Diversity among Colletotrichum Species in Sweet Persimmon.

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Gang, Geun-Hye; Cho, Hyun Ji; Kim, Hye Sun; Kwack, Yong-Bum; Kwak, Youn-Sig

2015-06-01

Anthracnose, caused by Colletotrichum gloeosporioides (C. gloeosporioides; Teleomorph: Glomerella cingulata), is the most destructive disease that affects sweet persimmon production worldwide. However, the biology, ecology, and genetic variations of C. gloeosporioides remain largely unknown. Therefore, in this study, the development of fungicide resistance and genetic diversity among an anthracnose pathogen population with different geographical origins and the exposure of this population to different cultivation strategies were investigated. A total of 150 pathogen isolates were tested in fungicide sensitivity assays. Five of the tested fungicides suppressed mycelial pathogen growth effectively. However, there were significant differences in the sensitivities exhibited by the pathogen isolates examined. Interestingly, the isolates obtained from practical management orchards versus organic cultivation orchards showed no differences in sensitivity to the same fungicide. PCR-restriction fragment length polymorphism (RFLP) analyses were performed to detect internal transcribed spacer regions and the β-tubulin and glutamine synthetase genes of the pathogens examined. Both the glutamine synthetase and β-tubulin genes contained a complex set of polymorphisms. Based on these results, the pathogens isolated from organic cultivation orchards were found to have more diversity than the isolates obtained from the practical management orchards.

Analysis of Fungicide Sensitivity and Genetic Diversity among Colletotrichum Species in Sweet Persimmon

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Geun-Hye Gang

2015-06-01

Full Text Available Anthracnose, caused by Colletotrichum gloeosporioides (C. gloeosporioides; Teleomorph: Glomerella cingulata, is the most destructive disease that affects sweet persimmon production worldwide. However, the biology, ecology, and genetic variations of C. gloeosporioides remain largely unknown. Therefore, in this study, the development of fungicide resistance and genetic diversity among an anthracnose pathogen population with different geographical origins and the exposure of this population to different cultivation strategies were investigated. A total of 150 pathogen isolates were tested in fungicide sensitivity assays. Five of the tested fungicides suppressed mycelial pathogen growth effectively. However, there were significant differences in the sensitivities exhibited by the pathogen isolates examined. Interestingly, the isolates obtained from practical management orchards versus organic cultivation orchards showed no differences in sensitivity to the same fungicide. PCR-restriction fragment length polymorphism (RFLP analyses were performed to detect internal transcribed spacer regions and the β-tubulin and glutamine synthetase genes of the pathogens examined. Both the glutamine synthetase and β-tubulin genes contained a complex set of polymorphisms. Based on these results, the pathogens isolated from organic cultivation orchards were found to have more diversity than the isolates obtained from the practical management orchards.

Reaction kinetics and mechanisms of organosilicon fungicide flusilazole with sulfate and hydroxyl radicals.

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Mercado, D Fabio; Bracco, Larisa L B; Arques, Antonio; Gonzalez, Mónica C; Caregnato, Paula

2018-01-01

Flusilazole is an organosilane fungicide used for treatments in agriculture and horticulture for control of diseases. The reaction kinetics and mechanism of flusilazole with sulfate and hydroxyl radicals were studied. The rate constant of the radicals with the fungicide were determined by laser flash photolysis of peroxodisulfate and hydrogen peroxide. The results were 2.0 × 10 9 s -1 M -1 for the reaction of the fungicide with HO and 4.6 × 10 8  s -1  M -1 for the same reaction with SO 4 - radicals. The absorption spectra of organic intermediates detected by laser flash photolysis of S 2 O 8 2- with flusilazole, were identified as α-aminoalkyl and siloxyl radicals and agree very well with those estimated employing the time-dependent density functional theory with explicit account for bulk solvent effects. In the continuous photolysis experiments, performed by photo-Fenton reaction of the fungicide, the main degradation products were: (bis(4-fluorophenyl)-hydroxy-methylsilane) and the non-toxic silicic acid, diethyl bis(trimethylsilyl) ester, in ten and twenty minutes of reaction, respectively. Copyright © 2017. Published by Elsevier Ltd.

Interactive Role of Fungicides and Plant Growth Regulator (Trinexapac on Seed Yield and Oil Quality of Winter Rapeseed

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Muhammad Ijaz

2015-09-01

Full Text Available This study was designed to evaluate the role of growth regulator trinexapac and fungicides on growth, yield, and quality of winter rapeseed (Brassica napus L.. The experiment was conducted simultaneously at different locations in Germany using two cultivars of rapeseed. Five different fungicides belonging to the triazole and strobilurin groups, as well as a growth regulator trinexapac, were tested in this study. A total of seven combinations of these fungicides and growth regulator trinexapac were applied at two growth stages of rapeseed. These two stages include green floral bud stage (BBCH 53 and the course of pod development stage (BBCH 65. The results showed that plant height and leaf area index were affected significantly by the application of fungicides. Treatments exhibited induced photosynthetic ability and delayed senescence, which improved the morphological characters and yield components of rape plants at both locations. Triazole, in combination with strobilurin, led to the highest seed yield over other treatments at both experimental locations. Significant effects of fungicides on unsaturated fatty acids of rapeseed oil were observed. Fungicides did not cause any apparent variation in the values of free fatty acids and peroxide of rapeseed oil. Results of our study demonstrate that judicious use of fungicides in rapeseed may help to achieve sustainable farming to obtain higher yield and better quality of rapeseed.

Signum, a new fungicide for control of leaf diseases in outdoor vegetables.

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Callens, D; Sarrazyn, R; Evens, W

2005-01-01

During three years, the new fungicide Signum, containing 6.7% pyraclostrobine + 26.7 % boscalid and developed by BASF. has been evaluated in leek, carrots and cabbages in several outdoor field experiments under practical conditions and during one year in outdoor lettuce. In leek, Phytophthora porri is one of the major leaf diseases causing lesions on differ ent places on the leaves, resulting in at least extra labour costs for trimming or even worse sometimes resulting in complete crop loss. So far, crop protection consists of repeated applications of fungicides especially during autumn and winter. Pyraclostrobin + boscalid has been evaluated in comparison with the fungicides mancozeb, mancozeb + metalaxyl-M and azoxystrobin. The progress of the disease during the growth season is discussed. For all parameters evaluated, pyraclostrobin + boscalid gave comparable or even better results than reference products. Especially during 2003, a small drop of the activity of benalaxyl against P. porri has been observed after repeated applications. In carrots, Erisiphe heraclei and Alternaria dauci are both the most common leaf diseases causing yield and quality loss. During periods of very high pressure of A. dauci, pyraclostrobin + boscalid, applied in a three weeks interval, revealed a superior activity compared with triazole references or compared with azoxystrobin. Against E. heraclei, a good control but also a clear dose response activity have been observed with pyraclostrobin + boscalid. Yield gain was approximately 30 ton /ha compared wih untreated. In Brussels sprouts, good efficacy was obtained against Mycosphaerella spp., Albugo candida and Alternaria spp. In outdoor lettuce Botrytis cinerea and Sclerotinia sclerotiorum are the most important diseases causing crop damage and reducing the quality of the heads. Pyraclostrobin + boscalid was evaluated in comparison with the standard fungicide iprodione. The plant protection was better with the new fungicide

Probabilities for profitable fungicide use against gray leaf spot in hybrid maize.

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Munkvold, G P; Martinson, C A; Shriver, J M; Dixon, P M

2001-05-01

ABSTRACT Gray leaf spot, caused by the fungus Cercospora zeae-maydis, causes considerable yield losses in hybrid maize grown in the north-central United States and elsewhere. Nonchemical management tactics have not adequately prevented these losses. The probability of profitably using fungicide application as a management tool for gray leaf spot was evaluated in 10 field experiments under conditions of natural inoculum in Iowa. Gray leaf spot severity in untreated control plots ranged from 2.6 to 72.8% for the ear leaf and from 3.0 to 7.7 (1 to 9 scale) for whole-plot ratings. In each experiment, fungicide applications with propiconazole or mancozeb significantly reduced gray leaf spot severity. Fungicide treatment significantly (P fungicide applications. For one application, the probability ranged from approximately 0.06 to more than 0.99, and exceeded 0.50 in six of nine scenarios (specific experiment/hybrid). The highest probabilities occurred in the 1995 experiments with the most susceptible hybrid. Probabilities were almost always higher for a single application of propiconazole than for two applications. These results indicate that a single application of propiconazole frequently can be profitable for gray leaf spot management in Iowa, but the probability of a profitable application is strongly influenced by hybrid susceptibility. The calculation of probabilities for positive net returns was more informative than mean separation in terms of assessing the economic success of the fungicide applications.

Synthesis and fungicidal activity of pyrazole derivatives containing 1,2,3,4-tetrahydroquinoline.

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Lei, Peng; Zhang, Xuebo; Xu, Yan; Xu, Gaofei; Liu, Xili; Yang, Xinling; Zhang, Xiaohe; Ling, Yun

2016-01-01

Take-all of wheat, caused by the soil-borne fungus Gaeumannomyces graminis var. tritici, is one of the most important and widespread root diseases. Given that take-all is still hard to control, it is necessary to develop new effective agrochemicals. Pyrazole derivatives have been often reported for their favorable bioactivities. In order to discover compounds with high fungicidal activity and simple structures, 1,2,3,4-tetrahydroquinoline, a biologically active group of natural products, was introduced to pyrazole structure. A series of pyrazole derivatives containing 1,2,3,4-tetrahydroquinoline were synthesized, and their fungicidal activities were evaluated. The bioassay results demonstrated that the title compounds displayed obvious fungicidal activities at a concentration of 50 μg/mL, especially against V. mali, S. sclerotiorum and G. graminis var. tritici. The inhibition rates of compounds 10d, 10e, 10h, 10i and 10j against G. graminis var. tritici were all above 90 %. Even at a lower concentration of 16.7 μg/mL, compounds 10d and 10e exhibited satisfied activities of 100 % and 94.0 %, respectively. It is comparable to that of the positive control pyraclostrobin with 100 % inhibition rate. A series of pyrazole derivatives containing 1,2,3,4-tetrahydroquinoline were synthesized and their structures were confirmed by (1)H NMR, (13)C NMR, IR spectrum and HRMS or elemental analysis. The crystal structure of compound 10g was confirmed by X-ray diffraction. Bioassay results indicated that all title compounds exhibited obvious fungicidal activities. In particular, compounds 10d and 10e showed comparable activities against G. graminis var. tritici with the commercial fungicide pyraclostrobin at the concentration of 16.7 μg/mL.Graphical abstractA series of pyrazole derivatives containing 1,2,3,4-tetrahydroquinoline were designed and synthesized. Bioassay results indicated that all these compounds exhibited obvious fungicidal activities.

Effects of current-use fungicides and their mixtures on the feeding and survival of the key shredder Gammarus fossarum.

Science.gov (United States)

Zubrod, J P; Baudy, P; Schulz, R; Bundschuh, M

2014-05-01

Fungicides are frequently applied in agriculture and are subsequently detected in surface waters in total concentrations of up to several tens of micrograms per liter. These concentrations imply potential effects on aquatic communities and fundamental ecosystem functions such as leaf litter breakdown. In this context, the present study investigates sublethal and lethal effects of organic (azoxystrobin, carbendazim, cyprodinil, quinoxyfen, and tebuconazole) and inorganic (three copper (Cu)-based substances and sulfur) current-use fungicides and their mixtures on the key leaf-shredding invertebrate Gammarus fossarum. The feeding activity of fungicide-exposed gammarids was quantified as sublethal endpoint using a static (organic fungicides; 7 d test duration) or a semi-static (inorganic fungicides; 6 d test duration with a water exchange after 3 d) approach (n=30). EC50-values of organic fungicides were generally observed at concentrations resulting in less than 20% mortality, with the exception of carbendazim. With regard to feeding, quinoxyfen was the most toxic organic fungicide, followed by cyprodinil, carbendazim, azoxystrobin, and tebuconazole. Although all tested organic fungicides have dissimilar (intended) modes of action, a mixture experiment revealed a synergistic effect on gammarids' feeding at high concentrations when using "independent action" as the reference model (∼35% deviation between predicted and observed effect). This may be explained by the presence of a synergizing azole fungicide (i.e. tebuconazole) in this mixture. Furthermore, lethal concentrations of all Cu-based fungicides assessed in this study were comparable amongst one another. However, they differed markedly in their effective concentrations when using feeding activity as the endpoint, with Cu-sulfate being most toxic, followed by Cu-hydroxide and Cu-octanoate. In contrast, sulfur neither affected survival nor the feeding activity of gammarids (up to ∼5 mg/L) but reduced Cu

The Synergistic Effects of Almond Protection Fungicides on Honey Bee (Hymenoptera: Apidae) Forager Survival.

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Fisher, Adrian; Coleman, Chet; Hoffmann, Clint; Fritz, Brad; Rangel, Juliana

2017-06-01

The honey bee (Apis mellifera L.) contributes ∼$17 billion annually to the United States economy, primarily by pollinating major agricultural crops including almond, which is completely dependent on honey bee pollination for nut set. Almond growers face constant challenges to crop productivity owing to pests and pathogens, which are often controlled with a multitude of agrochemicals. For example, fungicides are often applied in combination with other products to control fungal pathogens during almond bloom. However, the effects of fungicides on honey bee health have been so far understudied. To assess the effects of some of the top fungicides used during the 2012 California almond bloom on honey bee forager mortality, we collected foragers from a local apiary and exposed them to fungicides (alone and in various combinations) at the label dose, or at doses ranging from 0.25 to 2 times the label dose rate. These fungicides were Iprodione 2SE Select, Pristine, and Quadris. We utilized a wind tunnel and atomizer set up with a wind speed of 2.9 m/s to simulate field-relevant exposure of honey bees to these agrochemicals during aerial application in almond fields. Groups of 40-50 foragers exposed to either untreated controls or fungicide-laden treatments were monitored daily over a 10-d period. Our results showed a significant decrease in forager survival resulting from exposure to simulated tank mixes of Iprodione 2SE Select, as well as synergistic detrimental effects of Iprodione 2SE Select in combination with Pristine and Quadris on forager survival. © The Authors 2017. Published by Oxford University Press on behalf of Entomological Society of America. All rights reserved. For Permissions, please email: journals.permissions@oup.com.

Potential of Cerbera odollam as a bio-fungicide for post-harvest pathogen Penicilium digitatum

Science.gov (United States)

Singh, Harbant; Yin-Chu, Sue; Al-Samarrai, Ghassan; Syarhabil, Muhammad

2015-05-01

Postharvest diseases due to fungal infection contribute to economic losses in agriculture industry during storage, transportation or in the market. Penicillium digitatum is one of the common pathogen responsible for the postharvest rot in fruits. This disease is currently being controlled by synthetic fungicides such as Guazatine and Imazalil. However, heavy use of fungicides has resulted in environmental pollution, such as residue in fruit that expose a significant risk to human health. Therefore, there is a strong need to develop alternatives to synthetic fungicide to raise customer confidence. In the current research, different concentrations (500 to 3000 ppm) of ethanol extract of Cerbera odollam or commonly known as Pong-pong were compared with Neem and the controls (Positive control/Guazatine; Negative control/DMSO) for the anti-fungicide activity in PDA media contained in 10 cm diameter Petri dishes, using a modification of Ruch and Worf's method. The toxicity (Lc50) of the C.odollam extract was determined by Brine-shrimp test (BST). The results of the research indicated that crude extraction from C.odollam showed the highest inhibition rate (93%) and smallest colony diameter (0.63 cm) at 3000 ppm in vitro compared with Neem (inhibition rate: 88%; colony diameter: 1.33 cm) and control (Positive control/Guazatine inhibition rate: 79%, colony diameter: 1.9 cm; Negative control/DMSO inhibition rate: 0%, colony diameter: 9.2 cm). C.odollam recorded Lc50 value of 5 µg/ml which is safe but to be used with caution (unsafe level: below 2 µg/ml). The above anti-microbial activity and toxicity value results indicate that C.odollam has a potential of being a future bio-fungicide that could be employed as an alternative to synthetic fungicide.

Cytoplasmic fungal lipases release fungicides from ultra-deformable vesicular drug carriers.

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Gero Steinberg

Full Text Available The Transfersome® is a lipid vesicle that contains membrane softeners, such as Tween 80, to make it ultra-deformable. This feature makes the Transfersome® an efficient carrier for delivery of therapeutic drugs across the skin barrier. It was reported that TDT 067 (a topical formulation of 15 mg/ml terbinafine in Transfersome® vesicles has a much more potent antifungal activity in vitro compared with conventional terbinafine, which is a water-insoluble fungicide. Here we use ultra-structural studies and live imaging in a model fungus to describe the underlying mode of action. We show that terbinafine causes local collapse of the fungal endoplasmic reticulum, which was more efficient when terbinafine was delivered in Transfersome® vesicles (TFVs. When applied in liquid culture, fluorescently labeled TFVs rapidly entered the fungal cells (T(1/2~2 min. Entry was F-actin- and ATP-independent, indicating that it is a passive process. Ultra-structural studies showed that passage through the cell wall involves significant deformation of the vesicles, and depends on a high concentration of the surfactant Tween 80 in their membrane. Surprisingly, the TFVs collapsed into lipid droplets after entry into the cell and the terbinafine was released from their interior. With time, the lipid bodies were metabolized in an ATP-dependent fashion, suggesting that cytosolic lipases attack and degrade intruding TFVs. Indeed, the specific monoacylglycerol lipase inhibitor URB602 prevented Transfersome® degradation and neutralized the cytotoxic effect of Transfersome®-delivered terbinafine. These data suggest that (a Transfersomes deliver the lipophilic fungicide Terbinafine to the fungal cell wall, (b the membrane softener Tween 80 allows the passage of the Transfersomes into the fungal cell, and (c fungal lipases digest the invading Transfersome® vesicles thereby releasing their cytotoxic content. As this mode of action of Transfersomes is independent of the

Federal Insecticide, Fungicide, and Rodenticide Act Section 18 Database

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U.S. Environmental Protection Agency — Section 18 of Federal Insecticide, Fungicide, and Rodenticide Act (FIFRA) authorizes EPA to allow an unregistered use of a pesticide for a limited time if EPA...

2-Fluoro-L-Fucose Is a Metabolically Incorporated Inhibitor of Plant Cell Wall Polysaccharide Fucosylation.

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Jose A Villalobos

Full Text Available The monosaccharide L-fucose (L-Fuc is a common component of plant cell wall polysaccharides and other plant glycans, including the hemicellulose xyloglucan, pectic rhamnogalacturonan-I (RG-I and rhamnogalacturonan-II (RG-II, arabinogalactan proteins, and N-linked glycans. Mutations compromising the biosynthesis of many plant cell wall polysaccharides are lethal, and as a result, small molecule inhibitors of plant cell wall polysaccharide biosynthesis have been developed because these molecules can be applied at defined concentrations and developmental stages. In this study, we characterize novel small molecule inhibitors of plant fucosylation. 2-fluoro-L-fucose (2F-Fuc analogs caused severe growth phenotypes when applied to Arabidopsis seedlings, including reduced root growth and altered root morphology. These phenotypic defects were dependent upon the L-Fuc salvage pathway enzyme L-Fucose Kinase/ GDP-L-Fucose Pyrophosphorylase (FKGP, suggesting that 2F-Fuc is metabolically converted to the sugar nucleotide GDP-2F-Fuc, which serves as the active inhibitory molecule. The L-Fuc content of cell wall matrix polysaccharides was reduced in plants treated with 2F-Fuc, suggesting that this molecule inhibits the incorporation of L-Fuc into these polysaccharides. Additionally, phenotypic defects induced by 2F-Fuc treatment could be partially relieved by the exogenous application of boric acid, suggesting that 2F-Fuc inhibits RG-II biosynthesis. Overall, the results presented here suggest that 2F-Fuc is a metabolically incorporated inhibitor of plant cellular fucosylation events, and potentially suggest that other 2-fluorinated monosaccharides could serve as useful chemical probes for the inhibition of cell wall polysaccharide biosynthesis.

Non-target effects of fungicides on nectar-inhabiting fungi of almond flowers.

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Schaeffer, Robert N; Vannette, Rachel L; Brittain, Claire; Williams, Neal M; Fukami, Tadashi

2017-04-01

Nectar mediates interactions between plants and pollinators in natural and agricultural systems. Specialized microorganisms are common nectar inhabitants, and potentially important mediators of plant-pollinator interactions. However, their diversity and role in mediating pollination services in agricultural systems are poorly characterized. Moreover, agrochemicals are commonly applied to minimize crop damage, but may present ecological consequences for non-target organisms. Assessment of ecological risk has tended to focus on beneficial macroorganisms such as pollinators, with less attention paid to microorganisms. Here, using culture-independent methods, we assess the impact of two widely-used fungicides on nectar microbial community structure in the mass-flowering crop almond (Prunus dulcis). We predicted that fungicide application would reduce fungal richness and diversity, whereas competing bacterial richness would increase, benefitting from negative effects on fungi. We found that fungicides reduced fungal richness and diversity in exposed flowers, but did not significantly affect bacterial richness, diversity, or community composition. The relative abundance of Metschnikowia OTUs, nectar specialists that can impact pollination, was reduced by both fungicides. Given growing recognition of the importance of nectar microorganisms as mediators of plant-pollinator mutualisms, future research should consider the impact of management practices on plant-associated microorganisms and consequences for pollination services in agricultural landscapes. © 2016 Society for Applied Microbiology and John Wiley & Sons Ltd.

Low-airflow drying of fungicide-treated shelled corn

International Nuclear Information System (INIS)

Peterson, W.H.; Benson, P.W.

1993-02-01

Approved fungicides inhibit mold growth in shelled corn and allow for longer, natural-air drying. The longer drying periods permit lower than-normal airflows and smaller power units, thus reducing electrical demands on utilities in corn-producing states. Researchers placed approximately 67 m 3 (1900 bu) of one variety of shelled corn at approximately 24% moisture in each of five equally sized storage bins. They partitioned each bin vertically and filled one half of each bin with fungicide-treated corn and one half with untreated corn. Each of four bins used a different airflow. A fifth bin used the lowest of the four airflows but was equipped to capture and use solar energy. All corn dried rapidly with resulting good quality. The percentage of damaged kernels was significantly higher for untreated than for treated corn. The energy required for the lowest airflow system was approximately one half of that required for the higher, more traditional airflows. Because of lower-than-normal airflows, the electrical demand on the utility is approximately one fourth as great as that imposed when the higher, more traditional natural-air systems are used. The 1991 corn growing and drying seasons were unusual in central Illinois, the site of the study. Both harvest and drying occurred several weeks ahead of schedule. Additional work is needed to verify that findings hold true during more-normal Midwest corn growing and drying seasons; the investigators predict that they will. It should be noted that the fungicide used in this study has not yet been approved for widespread use in drying corn

Elucidation and chemical modulation of sulfolipid-1 biosynthesis in Mycobacterium tuberculosis.

Science.gov (United States)

Seeliger, Jessica C; Holsclaw, Cynthia M; Schelle, Michael W; Botyanszki, Zsofia; Gilmore, Sarah A; Tully, Sarah E; Niederweis, Michael; Cravatt, Benjamin F; Leary, Julie A; Bertozzi, Carolyn R

2012-03-09

Mycobacterium tuberculosis possesses unique cell-surface lipids that have been implicated in virulence. One of the most abundant is sulfolipid-1 (SL-1), a tetraacyl-sulfotrehalose glycolipid. Although the early steps in SL-1 biosynthesis are known, the machinery underlying the final acylation reactions is not understood. We provide genetic and biochemical evidence for the activities of two proteins, Chp1 and Sap (corresponding to gene loci rv3822 and rv3821), that complete this pathway. The membrane-associated acyltransferase Chp1 accepts a synthetic diacyl sulfolipid and transfers an acyl group regioselectively from one donor substrate molecule to a second acceptor molecule in two successive reactions to yield a tetraacylated product. Chp1 is fully active in vitro, but in M. tuberculosis, its function is potentiated by the previously identified sulfolipid transporter MmpL8. We also show that the integral membrane protein Sap and MmpL8 are both essential for sulfolipid transport. Finally, the lipase inhibitor tetrahydrolipstatin disrupts Chp1 activity in M. tuberculosis, suggesting an avenue for perturbing SL-1 biosynthesis in vivo. These data complete the SL-1 biosynthetic pathway and corroborate a model in which lipid biosynthesis and transmembrane transport are coupled at the membrane-cytosol interface through the activity of multiple proteins, possibly as a macromolecular complex.

The presence of bromuconazole fungicide pollutant in organic waste anaerobic fermentation

Science.gov (United States)

Hariyadi, H. R.

2017-03-01

The presence of bromuconazole fungicide pollutant in organic waste anaerobic fermentation was carried out as well as the influence phenol and benzoate, and biodegradation of bromuconazole. Bromuconazole is a fungicide effective against Ascomycetes, Basidiomycetes and fungi imperfecti in cereals, grapes, top fruits and vegetables. It is also effective against Alternaria and Fusarium sp. The remaining fungicide in leaves might contaminates landfill. One month of organic waste added with bromuconazole was anaerobically incubated in 500 mL bottles at 30°C without shaking in dark room. High-Performance Liquid Chromatography (HPLC) with UV detector and a 100 RP 185μm Lichrosphere column was used to determine bromuconazole concentration. Methane content was determined by Gas Chromatography (GC) method equipped with a flame ionization detector and a metal column packed with 5% neopentyl glycol sebacate and 1% H3PO4 on Chromosorb W-AW (mesh 80-100). After incubation for 225 days, bromuconazole of 200 mg/L inhibited the production of methane (99.5 mM) significantly, but did not inhibit the production of volatile fatty acids. The addition of 100 mg/L phenol or 146 mg/L benzoate increased the production of methane, 143 mM and 135.2 mM, respectively compared with control (121.8 mM). In anaerobic conditions, the presence of toxic pollutants such as fungicide bromuconazole in landfills sites may cause further problems with the accumulation of volatile fatty acids in leachate. Further study to determine the threshold, the presence of bromconazole in low concentration (less than 200 mg/L) on the methane production is recommended.

Toxicity evaluation of new agricultural fungicides in primary cultured cortical neurons.

Science.gov (United States)

Regueiro, Jorge; Olguín, Nair; Simal-Gándara, Jesús; Suñol, Cristina

2015-07-01

Fungicides are crucial for food protection as well as for the production of crops of suitable quality and quantity to provide a viable economic return. Like other pesticides, fungicides are widely sprayed on agricultural land, especially in wine-growing areas, from where they can move-off after application. Furthermore, residues of these agrochemicals can remain on crops after harvest and even after some food processing operations, being a major exposure pathway. Although a relatively low toxicity has been claimed for this kind of compounds, information about their neurotoxicity is still scarce. In the present study, nine fungicides recently approved for agricultural uses in the EU - ametoctradin, boscalid, cyazofamid, dimethomorph, fenhexamid, kresoxim-methyl, mepanipyrim, metrafenone and pyraclostrobin - have been evaluated for their toxicity in primary cultured mouse cortical neurons. Exposure to 0.1-100µM for 7 days in vitro resulted in a dose-dependent toxicity in the MTT cell viability assay. Strobilurin fungicides kresoxim-methyl (KR) and pyraclostrobin (PY) were the most neurotoxic compounds (lethal concentration 50 were in the low micromolar and nanomolar levels, respectively) causing a rapid raise in intracellular calcium [Ca(2+)]i and strong depolarization of mitochondrial membrane potential. KR- and PY-induced cell death was reversed by the calcium channels blockers MK-801 and verapamil, suggesting that calcium entry through NMDA receptors and voltage-operated calcium channels are involved in KR- and PY-induced neurotoxicity. These results highlight the need for further evaluation of their neurotoxic effects in vivo. Copyright © 2015 Elsevier Inc. All rights reserved.

Fate and activity of fungal BCAs delivered to strawberry flowers and their potential for integration with fungicides

DEFF Research Database (Denmark)

Jensen, Birgit; Andersen, Birgitte; Thrane, Ulf

2013-01-01

Grey mold caused by Botrytis cinerea is a serious strawberry disease. Yield loss is prevented by repeated fungicide treatments during flowering which increases the risk of pesticide residues in berries. Fruit lesions are typically initiated from B. cinerea infected stamens or from dead infected......) the interaction between BCAs and B. cinerea on strawberry flowers, 2) the sensitivity of BCAs to strawberry fungicides, and 3) the effect of combined BCA+fungicide treatment on BCAs and on the indigenous mycobiota....

Biological activity of triazole fungicides towards Botrytis cinerea

NARCIS (Netherlands)

Stehmann, C.

1995-01-01

Botrytis cinerea Pers. ex Fr., the causal agent of grey mould, is one of the most ubiquitous plant pathogens. The fungus is of high economic importance in various major crops and during transport and storage of agricultural products. Protectant fungicides such as

CONTROL OF BAGRAS (Eucalyptus deglupta DAMPING-OFF BY FUNGICIDES

Directory of Open Access Journals (Sweden)

EMILIO O. ANINO

2000-01-01

Full Text Available Selected fungicides were tested to control damp ing-off affecting bagras seedlings in the Central Nursery of the Paper Industries Corporation of the Philippines (PICOP, Surigao del Sur, Philippines. The fungicides, at three concentrations each, were applie d once before seed sowing to control pre-emergence damping-off and applied again after germination to cont rol post-emergence damping-off. Ajax detergent (2g/l H2O, Benlate (0.5 g/1 H2O, Brassicol (1.5 gv'l H 2O, and Fungitox (1.0 g/1 H2O provided the best level of control against the disease. Ajax detergent is the most practical among the best chemicals because it is cheap, locally available, not a heal th hazard, and less polluting.

Insecticidal and fungicidal compounds from Isatis tinctoria.

Science.gov (United States)

Seifert, K; Unger, W

1994-01-01

Tryptanthrin (1), indole-3-acetonitrile (2) and p-coumaric acid methylester (3) were isolated from the aerial parts of Isatis tinctoria L. The compounds show insecticidal and anti-feedant activity against termites (Reticulitermis santonensis), insect preventive and control activity against larvae of the house longhorn beetle (Hylotrupes bajulus) and fungicidal activity against the brown-rot fungus (Coniophora puteana).

48 CFR 1552.235-73 - Access to Federal Insecticide, Fungicide, and Rodenticide Act Confidential Business Information...

Science.gov (United States)

2010-10-01

... Insecticide, Fungicide, and Rodenticide Act Confidential Business Information (APR 1996). 1552.235-73 Section... Insecticide, Fungicide, and Rodenticide Act Confidential Business Information (APR 1996). As prescribed in... Act Confidential Business Information (APR 1996) In order to perform duties under the contract, the...

Chronic aquatic effect assessment for the fungicide azoxystrobin

NARCIS (Netherlands)

Wijngaarden, van R.P.A.; Belgers, J.D.M.; Zafar, M.I.; Matser, A.M.; Boerwinkel, M.C.; Arts, G.H.P.

2014-01-01

This study examined ecological effects of a range of chronic exposure concentrations of the fungicide azoxystrobin in freshwater experimental systems (1270 L outdoor microcosms). Intended and environmentally relevant test concentrations of azoxystrobin were 0, 0.33, 1, 3.3, 10, 33 µg ai/L, kept at

Efficacy of Combined Formulations of Fungicides with Different Modes of Action in Controlling Botrytis Gray Mold Disease in Chickpea

Science.gov (United States)

Rashid, M. H.; Hossain, M. Ashraf; Kashem, M. A.; Kumar, Shiv; Rafii, M. Y.; Latif, M. A.

2014-01-01

Botrytis gray mold (BGM) caused by Botrytis cinerea Pers. Ex. Fr. is an extremely devastating disease of chickpea (Cicer arietinum L.) and has a regional as well as an international perspective. Unfortunately, nonchemical methods for its control are weak and ineffective. In order to identify an effective control measure, six fungicides with different modes of action were evaluated on a BGM susceptible chickpea variety BARIchhola-1 at a high BGM incidence location (Madaripur) in Bangladesh for three years (2008, 2009, and 2010). Among the six fungicides tested, one was protectant [Vondozeb 42SC, a.i. mancozeb (0.2%)], two systemic [Bavistin 50 WP, a.i. carbendazim (0.2%), and Protaf 250EC, propiconazole (0.05%)], and three combination formulations [Acrobat MZ690, dimethomorph 9% + mancozeb 60%, (0.2%); Secure 600 WG, phenomadone + mancozeb (0.2%); and Companion, mancozeb 63% + carbendazim 12% (0.2%)]. The results showed superiority of combination formulations involving both protectant and systemic fungicides over the sole application of either fungicide separately. Among the combination fungicides, Companion was most effective, resulting in the lowest disease severity (3.33 score on 1–9 scale) and the highest increase (38%) of grain yield in chickpea. Therefore, this product could be preferred over the sole application of either solo protectant or systemic fungicides to reduce yield losses and avoid fungicide resistance. PMID:24723819

Efficacy of Combined Formulations of Fungicides with Different Modes of Action in Controlling Botrytis Gray Mold Disease in Chickpea

Directory of Open Access Journals (Sweden)

M. H. Rashid

2014-01-01

Full Text Available Botrytis gray mold (BGM caused by Botrytis cinerea Pers. Ex. Fr. is an extremely devastating disease of chickpea (Cicer arietinum L. and has a regional as well as an international perspective. Unfortunately, nonchemical methods for its control are weak and ineffective. In order to identify an effective control measure, six fungicides with different modes of action were evaluated on a BGM susceptible chickpea variety BARIchhola-1 at a high BGM incidence location (Madaripur in Bangladesh for three years (2008, 2009, and 2010. Among the six fungicides tested, one was protectant [Vondozeb 42SC, a.i. mancozeb (0.2%], two systemic [Bavistin 50 WP, a.i. carbendazim (0.2%, and Protaf 250EC, propiconazole (0.05%], and three combination formulations [Acrobat MZ690, dimethomorph 9% + mancozeb 60%, (0.2%; Secure 600 WG, phenomadone + mancozeb (0.2%; and Companion, mancozeb 63% + carbendazim 12% (0.2%]. The results showed superiority of combination formulations involving both protectant and systemic fungicides over the sole application of either fungicide separately. Among the combination fungicides, Companion was most effective, resulting in the lowest disease severity (3.33 score on 1–9 scale and the highest increase (38% of grain yield in chickpea. Therefore, this product could be preferred over the sole application of either solo protectant or systemic fungicides to reduce yield losses and avoid fungicide resistance.

Evaluation of some fungicides on mycorrhizal symbiosis between two Glomus species from commercial inocula and Allium porrum L. seedlings

Energy Technology Data Exchange (ETDEWEB)

Hernandez-Dorrego, A.; Mestre Pares, J.

2010-07-01

This paper reports the effect of twenty-five commonly used fungicides in agriculture on two arbuscular mycorrhizal fungi (AMF) present in commercial products of ATENS, S.L.: Glomus intra radices (Schenck and Smith) and Glomus mosseae [(Nicol. and Gerd.) Gerdemann and Trappe], forming the symbiosis with leek plants. Systemic fungicides (Aliette, Beltanol, Caddy 10, Forum, Moncut, Ortiva, Previcur, Ridomil Gold MZ, Ridomil Gold SL, Rubigan, Sinthane, Stroby, Swich, Tachigarem, Teldor, Topas 10 EC, Frupica) and non systemic fungicides (Daconil 75%, Ditiver, Euparem, INACOP, Octagon, Parmex, Terrazole and Metaram), started to be applied to soil and leaves at recommended concentrations and frequencies 4 weeks after transplant and AMF inoculation. The effect of the fungicides was assessed by comparing treated and untreated plants that were inoculated with the AMF through quantification of root mycorrhizal colonization. Among the fungicides applied to the soil, Octagon, Ditiver, Parmex and Metaram virtually eliminated the mycorrhizal symbiosis in treated plants, while the mycorrhizal colonization was not affected by the soil treatment with Beltanol, INACOP and Previcur. Three fungicides of foliar recommended application: Rubigan, Frupica, and Sinthane, strongly inhibited mycorrhizal colonization, but Aliette, Forum, Teldor, Swich and Ortiva, did not seem to reduce it substantially. In addition, the work describes the individual effect of each fungicide applied on both, foliage and soil. (Author) 29 refs.

How polyamine synthesis inhibitors and cinnamic acid affect tropane alkaloid production.

Science.gov (United States)

Marconi, Patricia L; Alvarez, María A; Pitta-Alvarez, Sandra I

2007-01-01

Hairy roots of Brugmansia candida produce the tropane alkaloids scopolamine and hyoscyamine. In an attempt to divert the carbon flux from competing pathways and thus enhance productivity, the polyamine biosynthesis inhibitors cyclohexylamine (CHA) and methylglyoxal-bis-guanylhydrazone (MGBG) and the phenylalanine-ammonia-lyase inhibitor cinnamic acid were used. CHA decreased the specific productivity of both alkaloids but increased significantly the release of scopolamine (approx 500%) when it was added in the mid-exponential phase. However, when CHA was added for only 48 h during the exponential phase, the specific productivity of both alkaloids increased (approx 200%), favoring scopolamine. Treatment with MGBG was detrimental to growth but promoted release into the medium of both alkaloids. However, when it was added for 48 h during the exponential phase, MGBG increased the specific productivity (approx 200%) and release (250- 1800%) of both alkaloids. Cinnamic acid alone also favored release but not specific productivity. When a combination of CHA or MGBG with cinnamic acid was used, the results obtained were approximately the same as with each polyamine biosynthesis inhibitor alone, although to a lesser extent. Regarding root morphology, CHA inhibited growth of primary roots and ramification. However, it had a positive effect on elongation of lateral roots.

Evaluation of fungicides to protect pruning wounds from Botryosphaeriaceae species infections on almond trees

Directory of Open Access Journals (Sweden)

Diego OLMO

2017-05-01

Full Text Available In vitro efficacy of ten fungicides was evaluated against four Botryosphaeriaceae spp. (Diplodia seriata, Neofusicoccum luteum, N. mediterraneum and N. parvum associated with branch cankers on almond trees. Cyproconazole, pyraclostrobin, tebuconazole, and thiophanate-methyl were effective for the inhibition of mycelial growth of most of these fungi. An experiment on 3-year-old almond trees evaluated boscalid, mancozeb, thiophanate-methyl, pyraclostrobin and tebuconazole for preventative ability against infections caused by the four pathogens. Five months after pruning and fungicide application, lesion length measurements and isolation percentages showed no significant differences among the four pathogens after they were inoculated onto the trees, and also between the two inoculation times tested (1 or 7 d after fungicide application. Thiophanate-methyl was the most effective fungicide, resulting in the shortest lesion lengths and the lowest isolation percentages from artificially inoculated pruning wounds. This chemical is therefore a candidate for inclusion in integrated disease management, to protect pruning wounds from infections caused by species of Botryosphaeriaceae. This study represents the first approach to development of chemical control strategies for the management of canker diseases caused by Botryosphaeriaceae fungi on almond trees. 

Effect of Maize Hybrid and Foliar Fungicides on Yield Under Low Foliar Disease Severity Conditions.

Science.gov (United States)

Mallowa, Sally O; Esker, Paul D; Paul, Pierce A; Bradley, Carl A; Chapara, Venkata R; Conley, Shawn P; Robertson, Alison E

2015-08-01

Foliar fungicide use in the U.S. Corn Belt increased in the last decade; however, questions persist pertaining to its value and sustainability. Multistate field trials were established from 2010 to 2012 in Illinois, Iowa, Ohio, and Wisconsin to examine how hybrid and foliar fungicide influenced disease intensity and yield. The experimental design was in a split-split plot with main plots consisting of hybrids varying in resistance to gray leaf spot (caused by Cercospora zeae-maydis) and northern corn leaf blight (caused by Setosphaera turcica), subplots corresponding to four application timings of the fungicide pyraclostrobin, and sub-subplots represented by inoculations with either C. zeae-maydis, S. turcica, or both at two vegetative growth stages. Fungicide application (VT/R1) significantly reduced total disease severity relative to the control in five of eight site-years (P<0.05). Disease was reduced by approximately 30% at Wisconsin in 2011, 20% at Illinois in 2010, 29% at Iowa in 2010, and 32 and 30% at Ohio in 2010 and 2012, respectively. These disease severities ranged from 0.2 to 0.3% in Wisconsin in 2011 to 16.7 to 22.1% in Illinois in 2010. The untreated control had significantly lower yield (P<0.05) than the fungicide-treated in three site-years. Fungicide application increased the yield by approximately 6% at Ohio in 2010, 5% at Wisconsin in 2010 and 6% in 2011. Yield differences ranged from 8,403 to 8,890 kg/ha in Wisconsin 2011 to 11,362 to 11,919 kg/ha in Wisconsin 2010. Results suggest susceptibility to disease and prevailing environment are important drivers of observed differences. Yield increases as a result of the physiological benefits of plant health benefits under low disease were not consistent.

Activity of two strobilurin fungicides against three species of decay fungi in agar plate tests

Science.gov (United States)

Juliet D. Tang; Tina Ciaramitaro; Maria Tomaso-Peterson; Susan V. Diehl

2017-01-01

The objective of this study was to examine the toxicity of strobilurin fungicides against wood decay fungi in order to assess their potential to act as a co-biocide for copper-based wood protection. Two strobilurin fungicides, Heritage (50% azoxystrobin active ingredient) and Insignia (20% pyraclostrobin active ingredients), and copper sulfate pentahydrate were tested...

Colonies of Bumble Bees (Bombus impatiens Produce Fewer Workers, Less Bee Biomass, and Have Smaller Mother Queens Following Fungicide Exposure

Directory of Open Access Journals (Sweden)

Olivia M. Bernauer

2015-06-01

Full Text Available Bees provide vital pollination services to the majority of flowering plants in both natural and agricultural systems. Unfortunately, both native and managed bee populations are experiencing declines, threatening the persistence of these plants and crops. Agricultural chemicals are one possible culprit contributing to bee declines. Even fungicides, generally considered safe for bees, have been shown to disrupt honey bee development and impair bumble bee behavior. Little is known, however, how fungicides may affect bumble bee colony growth. We conducted a controlled cage study to determine the effects of fungicide exposure on colonies of a native bumble bee species (Bombus impatiens. Colonies of B. impatiens were exposed to flowers treated with field-relevant levels of the fungicide chlorothalonil over the course of one month. Colony success was assessed by the number and biomass of larvae, pupae, and adult bumble bees. Bumble bee colonies exposed to fungicide produced fewer workers, lower total bee biomass, and had lighter mother queens than control colonies. Our results suggest that fungicides negatively affect the colony success of a native bumble bee species and that the use of fungicides during bloom has the potential to severely impact the success of native bumble bee populations foraging in agroecosystems.

Amino Acid Precursor Supply in the Biosynthesis of the RNA Polymerase Inhibitor Streptolydigin by Streptomyces lydicus▿†

Science.gov (United States)

Gómez, Cristina; Horna, Dina H.; Olano, Carlos; Palomino-Schätzlein, Martina; Pineda-Lucena, Antonio; Carbajo, Rodrigo J.; Braña, Alfredo F.; Méndez, Carmen; Salas, José A.

2011-01-01

Biosynthesis of the hybrid polyketide-nonribosomal peptide antibiotic streptolydigin, 3-methylaspartate, is utilized as precursor of the tetramic acid moiety. The three genes from the Streptomyces lydicus streptolydigin gene cluster slgE1-slgE2-slgE3 are involved in 3-methylaspartate supply. SlgE3, a ferredoxin-dependent glutamate synthase, is responsible for the biosynthesis of glutamate from glutamine and 2-oxoglutarate. In addition to slgE3, housekeeping NADPH- and ferredoxin-dependent glutamate synthase genes have been identified in S. lydicus. The expression of slgE3 is increased up to 9-fold at the onset of streptolydigin biosynthesis and later decreases to ∼2-fold over the basal level. In contrast, the expression of housekeeping glutamate synthases decreases when streptolydigin begins to be synthesized. SlgE1 and SlgE2 are the two subunits of a glutamate mutase that would convert glutamate into 3-methylaspartate. Deletion of slgE1-slgE2 led to the production of two compounds containing a lateral side chain derived from glutamate instead of 3-methylaspartate. Expression of this glutamate mutase also reaches a peak increase of up to 5.5-fold coinciding with the onset of antibiotic production. Overexpression of either slgE3 or slgE1-slgE2 in S. lydicus led to an increase in the yield of streptolydigin. PMID:21665968

The toxicity of the fungicide Propiconazole to soil flagellates

DEFF Research Database (Denmark)

Ekelund, Flemming; Westergaard, Kamma; Søe, Dorthe

2000-01-01

We investigated the effects of the ergosterol-inhibiting fungicide, propiconazole {1-[[2-(2,4-dichlorphenyl) - 4 - propyl - 1,3 - dioxolan - 2 - yl]methyl] - 1H - 1,2,4 triazole; Tilt}, on mixed natural populations of bacterivorous and fungivorous flagellates in soil and on single species...... of bacterivorous flagellates in liquid culture. The fungicide affected a mixed natural population of fungivorous flagellates less than the population of bacterivorous flagellates. Our results indicated that the effects of propiconazole on flagellates are direct toxic effects and not effects mediated via their food....... All tested types of flagellates were significantly harmed when exposed to the concentration of propiconazole normally applied to agricultural fields (625¿mg l-1). However, when exposed to the concentration of propiconazole which we expect in the soil water phase after application (ca. 0.6¿mg l-1...

Conversion of the fungicide, ziram in rice plants

International Nuclear Information System (INIS)

Kumarasamy, R.; Raghu, K.

1976-01-01

Zinc dimethyldithiocarbamate (ziram) is a toliar fungicide used for the control of the blast disease of rice caused by Pyricularia oryzae, and is also used for the control of the plant diseases in crops like groundnut, cotton, etc. Since there is lack of data on the conversion products of this fungicide. This investigation was carried out. The results of the author's recent studies with 35 S-labelled ziram in rice seedlings were reported. The 35 S-Labelled ziram (specific activity 1.5 m Ci/m mole) was sprayed on the rice seedlings of 25 days old. At different intervals of time, the seedlings were removed, washed thoroughly, cut into pieces, and extracted with 80% ethanol. By the method described in ''K. Raghu et al., Origin and fate of chemical residents in food, agriculture and fisheries, I.A.E.A., Vienna, 1975, pp. 137-148,'' the segments corresponding to the standards of dimethyl dithio carbamate-alanine (DDCA), DDC-glucoside (DDCG), thiazolidine-2-thione-4-carbamic acid (TTCA), unidentified divolent fungicide (X), and ziram were cut out and the radioactivity was counted in cocktail D scintillation fluid using an LS-100 Beckmann liquid scintillation counter. It is indeed interesting to note that ziram is converted in plant tissues into dimethyldithiocarbamate derivatives like DDCG, DDCA, TTCA and X within 24 hr after spraying. The amounts of these derivatives varied in the course of sampling up to 8 days after spraying. Further studies are needed as to the quantitative nature of these products, but the present report clearly demonstrates the formation of these conversion products in the rice leaves treated with ziram. (Kobatake, H.)

Retention of copper originating from different fungicides in contrasting soil types.

Science.gov (United States)

Komárek, Michael; Vanek, Ales; Chrastný, Vladislav; Száková, Jirina; Kubová, Karolina; Drahota, Petr; Balík, Jirí

2009-07-30

This work described the retention of Cu from two different commonly used pesticides, the Bordeaux mixture (CuSO(4)+Ca(OH)(2)) and Cu-oxychloride (3Cu(OH)(2).CuCl(2)), and from Cu(NO(3))(2) in contrasting soil types (Leptosol, Chernozem, Cambisol). Thermodynamic modeling showed that Cu speciation was similar in all fungicide solutions. However, the retention of Cu differed with the fungicide used (maximum retention from the Bordeaux mixture) which indicates that different retention processes occurred in the studied soils. The suggested mechanisms include: specific and non-specific adsorption (especially on soil organic matter), precipitation of newly formed phases, such as CuO, Cu(OH)(2), Cu(2)(OH)(3)NO(3), CuCO(3)/Cu(2)(OH)(2)CO(3) and in the case of the Bordeaux mixture, precipitation of various Cu-hydroxysulfates. These phases were identified by the speciation model. The retention of fungicide-derived Cu in the studied soil types followed well the Freundlich isotherm and was directly controlled by the chemical form of Cu. This fact should be taken into account for both environmental and practical applications.

Retention of copper originating from different fungicides in contrasting soil types

Energy Technology Data Exchange (ETDEWEB)

Komarek, Michael, E-mail: komarek@af.czu.cz [Department of Agro-Environmental Chemistry and Plant Nutrition, Czech University of Life Sciences Prague, Kamycka 129, 165 21, Prague 6 (Czech Republic); Vanek, Ales [Department of Soil Science and Soil Protection, Czech University of Life Sciences Prague, Kamycka 129, 165 21, Prague 6 (Czech Republic); Chrastny, Vladislav [Department of Applied Chemistry, University of South Bohemia, Studentska 13, 370 05, Ceske Budejovice (Czech Republic); Szakova, Jirina; Kubova, Karolina [Department of Agro-Environmental Chemistry and Plant Nutrition, Czech University of Life Sciences Prague, Kamycka 129, 165 21, Prague 6 (Czech Republic); Drahota, Petr [Institute of Geochemistry, Mineralogy and Mineral Resources, Charles University Prague, Albertov 6, 128 43, Prague 2 (Czech Republic); Balik, Jiri [Department of Agro-Environmental Chemistry and Plant Nutrition, Czech University of Life Sciences Prague, Kamycka 129, 165 21, Prague 6 (Czech Republic)

2009-07-30

This work described the retention of Cu from two different commonly used pesticides, the Bordeaux mixture (CuSO{sub 4} + Ca(OH){sub 2}) and Cu-oxychloride (3Cu(OH){sub 2}.CuCl{sub 2}), and from Cu(NO{sub 3}){sub 2} in contrasting soil types (Leptosol, Chernozem, Cambisol). Thermodynamic modeling showed that Cu speciation was similar in all fungicide solutions. However, the retention of Cu differed with the fungicide used (maximum retention from the Bordeaux mixture) which indicates that different retention processes occurred in the studied soils. The suggested mechanisms include: specific and non-specific adsorption (especially on soil organic matter), precipitation of newly formed phases, such as CuO, Cu(OH){sub 2}, Cu{sub 2}(OH){sub 3}NO{sub 3}, CuCO{sub 3}/Cu{sub 2}(OH){sub 2}CO{sub 3} and in the case of the Bordeaux mixture, precipitation of various Cu-hydroxysulfates. These phases were identified by the speciation model. The retention of fungicide-derived Cu in the studied soil types followed well the Freundlich isotherm and was directly controlled by the chemical form of Cu. This fact should be taken into account for both environmental and practical applications.

Retention of copper originating from different fungicides in contrasting soil types

International Nuclear Information System (INIS)

Komarek, Michael; Vanek, Ales; Chrastny, Vladislav; Szakova, Jirina; Kubova, Karolina; Drahota, Petr; Balik, Jiri

2009-01-01

This work described the retention of Cu from two different commonly used pesticides, the Bordeaux mixture (CuSO 4 + Ca(OH) 2 ) and Cu-oxychloride (3Cu(OH) 2 .CuCl 2 ), and from Cu(NO 3 ) 2 in contrasting soil types (Leptosol, Chernozem, Cambisol). Thermodynamic modeling showed that Cu speciation was similar in all fungicide solutions. However, the retention of Cu differed with the fungicide used (maximum retention from the Bordeaux mixture) which indicates that different retention processes occurred in the studied soils. The suggested mechanisms include: specific and non-specific adsorption (especially on soil organic matter), precipitation of newly formed phases, such as CuO, Cu(OH) 2 , Cu 2 (OH) 3 NO 3 , CuCO 3 /Cu 2 (OH) 2 CO 3 and in the case of the Bordeaux mixture, precipitation of various Cu-hydroxysulfates. These phases were identified by the speciation model. The retention of fungicide-derived Cu in the studied soil types followed well the Freundlich isotherm and was directly controlled by the chemical form of Cu. This fact should be taken into account for both environmental and practical applications.

Fungicide contamination reduces beneficial fungi in bee bread based on an area-wide field study in honey bee, Apis mellifera, colonies.

Science.gov (United States)

Yoder, Jay A; Jajack, Andrew J; Rosselot, Andrew E; Smith, Terrance J; Yerke, Mary Clare; Sammataro, Diana

2013-01-01

Fermentation by fungi converts stored pollen into bee bread that is fed to honey bee larvae, Apis mellifera, so the diversity of fungi in bee bread may be related to its food value. To explore the relationship between fungicide exposure and bee bread fungi, samples of bee bread collected from bee colonies pollinating orchards from 7 locations over 2 years were analyzed for fungicide residues and fungus composition. There were detectable levels of fungicides from regions that were sprayed before bloom. An organic orchard had the highest quantity and variety of fungicides, likely due to the presence of treated orchards within bees' flight range. Aspergillus, Penicillium, Rhizopus, and Cladosporium (beneficial fungi) were the primary fungal isolates found, regardless of habitat differences. There was some variation in fungal components amongst colonies, even within the same apiary. The variable components were Absidia, Alternaria, Aureobasidium, Bipolaris, Fusarium, Geotrichum, Mucor, Nigrospora, Paecilomyces, Scopulariopsis, and Trichoderma. The number of fungal isolates was reduced as an effect of fungicide contamination. Aspergillus abundance was particularly affected by increased fungicide levels, as indicated by Simpson's diversity index. Bee bread showing fungicide contamination originated from colonies, many of which showed chalkbrood symptoms.

Peptides of the constant region of antibodies display fungicidal activity.

Directory of Open Access Journals (Sweden)

Luciano Polonelli

Full Text Available Synthetic peptides with sequences identical to fragments of the constant region of different classes (IgG, IgM, IgA of antibodies (Fc-peptides exerted a fungicidal activity in vitro against pathogenic yeasts, such as Candida albicans, Candida glabrata, Cryptococcus neoformans, and Malassezia furfur, including caspofungin and triazole resistant strains. Alanine-substituted derivatives of fungicidal Fc-peptides, tested to evaluate the critical role of each residue, displayed unaltered, increased or decreased candidacidal activity in vitro. An Fc-peptide, included in all human IgGs, displayed a therapeutic effect against experimental mucosal and systemic candidiasis in mouse models. It is intriguing to hypothesize that some Fc-peptides may influence the antifungal immune response and constitute the basis for devising new antifungal agents.

Peptides of the Constant Region of Antibodies Display Fungicidal Activity

Science.gov (United States)

Polonelli, Luciano; Ciociola, Tecla; Magliani, Walter; Zanello, Pier Paolo; D'Adda, Tiziana; Galati, Serena; De Bernardis, Flavia; Arancia, Silvia; Gabrielli, Elena; Pericolini, Eva; Vecchiarelli, Anna; Arruda, Denise C.; Pinto, Marcia R.; Travassos, Luiz R.; Pertinhez, Thelma A.; Spisni, Alberto; Conti, Stefania

2012-01-01

Synthetic peptides with sequences identical to fragments of the constant region of different classes (IgG, IgM, IgA) of antibodies (Fc-peptides) exerted a fungicidal activity in vitro against pathogenic yeasts, such as Candida albicans, Candida glabrata, Cryptococcus neoformans, and Malassezia furfur, including caspofungin and triazole resistant strains. Alanine-substituted derivatives of fungicidal Fc-peptides, tested to evaluate the critical role of each residue, displayed unaltered, increased or decreased candidacidal activity in vitro. An Fc-peptide, included in all human IgGs, displayed a therapeutic effect against experimental mucosal and systemic candidiasis in mouse models. It is intriguing to hypothesize that some Fc-peptides may influence the antifungal immune response and constitute the basis for devising new antifungal agents. PMID:22470523

Conservation of the 2-keto-3-deoxymanno-octulosonic acid (Kdo) biosynthesis pathway between plants and bacteria.

Science.gov (United States)

Smyth, Kevin M; Marchant, Alan

2013-10-18

The increasing prevalence of multi-drug resistant bacteria is driving efforts in the development of new antibacterial agents. This includes a resurgence of interest in the Gram-negative bacteria lipopolysaccharide (LPS) biosynthesis enzymes as drug targets. The six carbon acidic sugar 2-keto-3-deoxymanno-octulosonic acid (Kdo) is a component of the lipid A moiety of the LPS in Gram-negative bacteria. In most cases the lipid A substituted by Kdo is the minimum requirement for cell growth, thus presenting the possibility of targeting either the synthesis or incorporation of Kdo for the development of antibacterial agents. Indeed, potent in vitro inhibitors of Kdo biosynthesis enzymes have been reported but have so far failed to show sufficient in vivo action against Gram-negative bacteria. As part of an effort to design more potent antibacterial agents targeting Kdo biosynthesis, the crystal structures of the key Kdo biosynthesis enzymes from Escherichia coli have been solved and their structure based mechanisms characterized. In eukaryotes, Kdo is found as a component of the pectic polysaccharide rhamnogalacturonan II in the plant primary cell wall. Interestingly, despite incorporating Kdo into very different macromolecules the Kdo biosynthesis and activation pathway is almost completely conserved between plants and bacteria. This raises the possibility for plant research to exploit the increasingly detailed knowledge and resources being generated by the microbiology community. Likewise, insights into Kdo biosynthesis in plants will be potentially useful in efforts to produce new antimicrobial compounds. Copyright © 2013 Elsevier Ltd. All rights reserved.

Brain modulation of Dufour's gland ester biosynthesis in vitro in the honeybee ( Apis mellifera)

Science.gov (United States)

Katzav-Gozansky, Tamar; Hefetz, Abraham; Soroker, Victoria

2007-05-01

Caste-specific pheromone biosynthesis is a prerequisite for reproductive skew in the honeybee. Nonetheless, this process is not hardwired but plastic, in that egg-laying workers produce a queen-like pheromone. Studies with Dufour’s gland pheromone revealed that, in vivo, workers’ gland biosynthesis matches the social status of the worker, i.e., sterile workers showed a worker-like pattern whereas fertile workers showed a queen-like pattern (production of the queen-specific esters). However, when incubated in vitro, the gland spontaneously exhibits the queen-like pattern, irrespective of its original worker type, prompting the notion that ester production in workers is under inhibitory control that is queen-dependent. We tested this hypothesis by exposing queen or worker Dufour’s glands in vitro to brain extracts of queens, queenright (sterile) workers and males. Unexpectedly, worker brain extracts activated the queen-like esters biosynthesis in workers’ Dufour’s gland. This stimulation was gender-specific; queen or worker brains demonstrated a stimulatory activity, but male brains did not. Queen gland could not be further stimulated. Bioassays with heated and filtered extracts indicate that the stimulatory brain factor is below 3,000 Da. We suggest that pheromone production in Dufour’s gland is under dual, negative positive control. Under queenright conditions, the inhibitor is released and blocks ester biosynthesis, whereas under queenless conditions, the activator is released, activating ester biosynthesis in the gland. This is consistent with the hypothesis that queenright workers are unequivocally recognized as non-fertile, whereas queenless workers try to become “false queens” as part of the reproductive competition.

Systemic fungicidal activity of 1,4-oxathiin derivatives.

Science.gov (United States)

Schmeling, B V; Kulka, M

1966-04-29

Treatment of pinto bean and barley seed with 1,4-oxathiin derivatives gave disease control by systemic fungicidal action of such pathogenic fungi as Uromyces phaseoli and Ustilago nuda. The two chemicals, D735 and F461, were highly specific and selective against the pathogens without injury of the hosts.

Growth of Cucurbita maxima L. plants in the presence of the cycloartenol synthase inhibitor U18666A.

Science.gov (United States)

Fenner, G P; Raphiou, I

1995-03-01

Squash, like other Cucurbitaceae, have unique sterol profiles that offer an excellent opportunity to examine the relationship between sterol biosynthesis and plant growth. To determine the effect of sterol biosynthesis inhibition on squash growth, Cucurbita maxima seedlings with and without cotyledons were subjected to increasing concentrations of the cycloarternol synthase (EC 5.4.99.8) inhibitor 3 beta-(2-diethylaminoethoxy)androstenone (U18666A). Inhibition of shoot growth was concentration-dependent (from 0, 2, 5, 10, and 20 microM); plants with intact cotyledons grew to 26.4, 23.7, 21.6, 20.0, and 15.6 cm, respectively, at the above inhibitor concentrations, compared to 25.5, 19.4, 17.0, 12.0, and 11 cm for plants with severed cotyledons. In plants with severed cotyledons, 10 and 20 microM U18666A caused rapid necrosis of the first two, newly emerged, primary leaves, and halted new leaf formation. Secondary root formation was initially affected at all inhibitor concentrations regardless of whether cotyledons were present or not. Vegetative tissue showed a decrease in the accumulation of the major squash sterol, 7,22-stigmastadienol, accompanied by increased accumulation of minor sterol components. Sterol profiles in cotyledons were unaltered. The data show that sterols are crucial for maintaining plant growth and viability, but do not address the cotyledonary effect on growth with respect to sterol biosynthesis.

Effect of Furfural, Vanillin and Syringaldehyde on Candida guilliermondii Growth and Xylitol Biosynthesis

Science.gov (United States)

Kelly, Christine; Jones, Opal; Barnhart, Christopher; Lajoie, Curtis

Xylitol is a five-carbon sugar alcohol with established commercial use as an alternative sweetener and can be produced from hemicellulose hydrolysate. However, there are difficulties with microbiological growth and xylitol biosynthesis on hydrolysate because of the inhibitors formed from hydrolysis of hemicellulose. This research focused on the effect of furfural, vanillin, and syringaldehyde on growth of Candida guilliermondii and xylitol accumulation from xylose in a semi-synthetic medium in microwell plate and bioreactor cultivations. All three compounds reduced specific growth rate, increased lag time, and reduced xylitol production rate. In general, increasing concentration of inhibitor increased the severity of inhibition, except in the case of 0.5 g vanillin per liter, which resulted in a faster late batch phase growth rate and increased biomass yield. At concentrations of 1 g/1 or higher, furfural was the least inhibitory to growth, followed by syringaldehyde. Vanillin most severely reduced specific growth rate. All three inhibitors reduced xylitol production rate approximately to the same degree.

Effect of benzimidazole fungicides and calcium chloride on ...

African Journals Online (AJOL)

SERVER

2007-06-04

Jun 4, 2007 ... Botrytis cinerea (Besri and Diatta, 1985; Hmouni et al.,. 1996). It is very likely that the repetitive uses of these systemic fungicides and their persistence during long periods of conservation (Ben Arie, 1975; Prusky, 1985) have led to considerable selective pressure on both species. Moreover, the single site ...

Oral Toxicity of Agro-Fungicides: Tilt (Propiconazole), Bayleton ...

African Journals Online (AJOL)

Methods: Twelve Nubian goats were used in these experiments; they were grouped into three groups (and one control group) and dosed orally with two fungicides [Propiconazole (100mg/kg/day), Triadimefon (100mg/kg/day)] and their mixture (50:50 mg/kg/day). Animals were closely observed for clinical signs and behavior ...

Inhibitors of steroidal cytochrome p450 enzymes as targets for drug development.

Science.gov (United States)

Baston, Eckhard; Leroux, Frédéric R

2007-01-01

Cytochrome P450's are enzymes which catalyze a large number of biological reactions, for example hydroxylation, N-, O-, S- dealkylation, epoxidation or desamination. Their substrates include fatty acids, steroids or prostaglandins. In addition, a high number of various xenobiotics are metabolized by these enzymes. The enzyme 17alpha-hydroxylase-C17,20-lyase (P450(17), CYP 17, androgen synthase), a cytochrome P450 monooxygenase, is the key enzyme for androgen biosynthesis. It catalyzes the last step of the androgen biosynthesis in the testes and adrenal glands and produces androstenedione and dehydroepiandrosterone from progesterone and pregnenolone. The microsomal enzyme aromatase (CYP19) transforms these androgens to estrone and estradiol. Estrogens stimulate tumor growth in hormone dependent breast cancer. In addition, about 80 percent of prostate cancers are androgen dependent. Selective inhibitors of these enzymes are thus important alternatives to treatment options like antiandrogens or antiestrogens. The present article deals with recent patents (focus on publications from 2000 - 2006) concerning P450 inhibitor design where steroidal substrates are involved. In this context a special focus is provided for CYP17 and CYP19. Mechanisms of action will also be discussed. Inhibitors of CYP11B2 (aldosterone synthase) will also be dealt with.

Sorption-desorption characteristics of benzimidazole based fungicide 2-(4-fluorophenyl)-1h-benzimidazole on physicochemical properties of selected pakistani soils

International Nuclear Information System (INIS)

Ahmad, K.S.

2014-01-01

A batch equilibrium method has been utilized to investigate the sorption-desorption behavior of a versatile cost-effective fungicide2-(4-fluorophenyl)-1H-benzimidazole) FBNZ on four Pakistani soils geographically distant, from hilly to desert areas. FBNZ is a newly synthesized fungicide prepared in the laboratory and is cost effective than the commercially available fungicides. The adsorption and desorption data were fitted to the Freundlich equation, with values of na = 1, which points to a C-type isotherm. Sorption increases with soil organic carbon content, with greater degree of adsorption for hilly soil and least adsorption on sandy soil of Multan, Punjab. Desorption studies reveal that the adsorbed fungicide are firmly retained by soil particles and present a certain degree of irreversibility. The results indicate that the soil organic matters followed by clay content are the most important soil properties governing the fungicide sorption capacity. (author)

Fungicide sensitivity in the wild rice pathogen Bipolaris oryzae

Science.gov (United States)

In recent years the occurrence of fungal brown spot, caused by Bipolaris oryzae has increased in cultivated wild rice (Zizania palustris) paddies in spite of the use of fungicides. To implement an efficient integrated disease management system, we are exploring whether field isolates have developed ...

Influence of fungicides on gas exchange of pecan foliage

Science.gov (United States)

There are several fungicide chemistries used for disease control on pecan (Carya illinoinensis), but there is little or no knowledge of subtle short- or long-term side-effects of these chemistries on host physiological processes, including photosynthesis (Pn). This study quantifies the impact of se...

The Effect of Fungicides for Seed Treatment on Germination of Barley

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Vesna Stevanović

2009-01-01

Full Text Available The application of chemicals, such as fungicides for seed treatment, is one of the most reliable and perhaps most efficient measures for integrated preservation of crops, and its practicing has become a legal obligation for all seed producers. This investigation was carried out in the laboratory for seed quality and phytopathology of the Small Grains Research Center in Kragujevac. The objective was to establish the effect of fungicides on germination energy and seed germinability (determined after treatments. Two varieties were tested due to a possibility of specific sensitivities of some varieties, so that the results acquired on one variety would not necessarily be valid for another one. Fungicides based on active ingredients from the triasol chemical group had different effects on the energy of germination of barley seeds. Applying Raxil S040-FS, the average germination of barley seeds was 79.3% for the variety Record, and 91.3% for the Grand variety. The variety Record achieved a lower value than the minimum for barley seed germination (88% stipulated by the Rules on Seed Quality of Agricultural Crops.Regardless of barley type, the product Raxil S040-FS showed a statistically significant effect on the number of atypical seedlings and increase in the number of non-germinated seeds, compared to the control.

Comparative assessment of the effect of synthetic and natural fungicides on soil respiration.

Science.gov (United States)

Stefani, Angelo; Felício, Joanna D'Arc; de Andréa, Mara M

2012-01-01

As toxic pesticide residues may persist in agricultural soils and cause environmental pollution, research on natural fungicides to replace the synthetic compounds is currently increasing. The effect of the synthetic fungicide chlorothalonil and a natural potential fungicide on the soil microbial activity was evaluated here by the substrate-induced respiration by addition of glucose (SIR), as bioindicator in two soils (Eutrophic Humic Gley-GHE and Typic Eutroferric Chernosol-AVEC). The induced soil respiration parameter was followed during 28 days after soil treatment either with chlorathalonil (11 μg·g(-1)), or the methanolic fraction from Polymnia sonchifolia extraction (300 μg·g(-1)), and (14)C-glucose (4.0 mg and 5.18 Bq of (14)C-glucose g(-1)). The (14)C-CO(2) produced by the microbial respiration was trapped in NaOH (0.1 M) which was changed each two hours during the first 10 h, and 1, 3, 5, 7, 14 and 28 days after the treatments. The methanolic fraction of the plant extract inhibited (2.2%) and stimulated (1.8%) the respiration of GHE and AVEC, respectively, but the synthetic chlorothalonil caused 16.4% and 2.6% inhibition of the respiration, respectively of the GHE and AVEC soils. As the effects of the natural product were statistically small, this bioindicator indicates that the methanolic fraction of the Polymnia sonchifolia extract, which has fungicide properties, has no environmental effects.

Evaluating the combined efficacy of polymers with fungicides for protection of museum textiles against fungal deterioration in Egypt.

Science.gov (United States)

Abdel-Kareem, Omar

2010-01-01

Fungal deterioration is one of the highest risk factors for damage of historical textile objects in Egypt. This paper represents both a study case about the fungal microflora deteriorating historical textiles in the Egyptian Museum and the Coptic museum in Cairo, and evaluation of the efficacy of several combinations of polymers with fungicides for the reinforcement of textiles and their prevention against fungal deterioration. Both cotton swab technique and biodeteriorated textile part technique were used for isolation of fungi from historical textile objects. The plate method with the manual key was used for identification of fungi. The results show that the most dominant fungi isolated from the tested textile samples belong to Alternaria, Aspergillus, Chaetomium, Penicillium and Trichoderma species. Microbiological testing was used for evaluating the usefulness of the suggested conservation materials (polymers combined with fungicides) in prevention of the fungal deterioration of ancient Egyptian textiles. Textile samples were treated with 4 selected polymers combined with two selected fungicides. Untreated and treated textile samples were deteriorated by 3 selected active fungal strains isolated from ancient Egyptian textiles. This study reports that most of the tested polymers combined with the tested fungicides prevented the fungal deterioration of textiles. Treatment of ancient textiles by suggested polymers combined with the suggested fungicides not only reinforces these textiles, but also prevents fungal deterioration and increases the durability of these textiles. The tested polymers without fungicides reduce the fungal deterioration of textiles but do not prevent it completely.

Tricholin, a new antifungal agent from Trichoderma viride, and its action in biological control of Rhizoctonia solani.

Science.gov (United States)

Lin, A; Lee, T M; Rern, J C

1994-07-01

Tricholin, a ribosome-inactivating protein isolated from the culture broth of Trichoderma viride, has been shown to exert fungicidal effects on Rhizoctonia solani through a multi-hit kinetic interaction. Tricholin causes a parallel cessation of growth, uptake of amino acids, and protein biosynthesis. The in vivo mode of action of tricholin on protein synthesis and cell growth appears to be attributed to the diminishing of the polysome formation in R. solani through damage to large ribosomal subunits. These results concur with previous data and prove that tricholin is an effective inhibitor of protein synthesis. The efficacy of tricholin as an antibiotic agent was estimated to have a duration of approximately 42 hours.

A turn-on supramolecular fluorescent probe for sensing benzimidazole fungicides and its application in living cell imaging

Science.gov (United States)

Tang, Qing; Zhang, Jing; Sun, Tao; Wang, Cheng-Hui; Huang, Ying; Zhou, Qingdi; Wei, Gang

2018-02-01

A cucurbit[8]uril-based turn-on supramolecular fluorescent probe between cucurbit[8]uril (Q[8]) and pyronine Y (PyY) (designated 2PyY@Q[8]) in acidic aqueous solution showed a remarkable fluorescence 'turn-on' response to benzimidazole fungicides such as thiabendazole, fuberidazole and carbendazim. The 2PyY@Q[8] fluorescent probe can be used to detect benzimidazole fungicides with high sensitivity and selectivity with a detection limit of 10- 8 mol/L. A good linear relationship of emission intensity at 580 nm for benzimidazole fungicides at concentrations of 0.4-5.0 μmol/L was observed. The proposed sensing mechanism was investigated using 1H NMR spectroscopy combined with density functional theory calculations at the B3LYP/6-31G(d) level. The cell imaging study showed that the 2PyY@Q[8] complex could be used to image benzimidazole fungicide in prostate cancer (PC3) cells, which may help to elucidate relevant biological processes at the molecular level.

Sensitivity of some nitrogen fixers and the target pest Fusarium oxysporum to fungicide thiram

OpenAIRE

Osman, Awad G.; Sherif, Ashraf M.; Elhussein, Adil A.; Mohamed, Afrah T.

2012-01-01

This study was carried out to investigate the toxic effects of the fungicide thiram (TMTD) against five nitrogen fixers and the thiram target pest Fusarium oxysporum under laboratory conditions. Nitrogen fixing bacteria Falvobacterium showed the highest values of LD50 and proved to be the most resistant to the fungicide followed by Fusarium oxysporum, while Pseudomonas aurentiaca was the most affected microorganism. LD50 values for these microorganisms were in 2–5 orders of magnitude lower in...

Botrytis cinerea Control and the Problem of Fungicide Resistance

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Brankica Tanović

2011-01-01

Full Text Available Botrytis cinerea, the causal agent of grey mould, greatly affects fruit, grapevine, vegetable and ornamental crops production. It is a common causal agent of diseases in plants grown in protected areas, as well as fruit decay during storage and transport. The fungusinvades almost all parts of the plant in all developmental stages, and the symptoms are usually described as grey mould, grey mildew, brown rot and seedling blight. The paper reviews the current knowledge on control possibilities of this necrotrophic pathogen. Theattention is particularly paid to the mode of action of novel fungicides and to the problem of resistance. It is pointed out that by limiting the number of treatments in the growing season, avoiding the use of only one fungicide with a high risk for resistance development,appropriate application rate and timing, using mixtures of pesticides with different modes of action, as well as by alternative use of pesticides from different resistance groups, a longterm preservation of pesticide efficacy is provided.

Late Blight of Potato (Phytophthora infestans I: Fungicides Application and Associated Challenges

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Abdul Majeed

2017-03-01

Full Text Available Potato (Solanum tuberosum L. has been remained an important agricultural crop in resolving global food issues through decades. The crop has experienced enormous growth in terms of production throughout the world in recent decades because of improvement in agricultural mechanization, fertilizers application and irrigation practices. Nevertheless, a significant proportion of this valuable crop is still vulnerable to losses due to prevalence of different viral, bacterial, fungal and nematodes infestations. Late blight, caused by Phytophthora infestans (Mont. de Bary, is one of the most threatening pathogenic diseases which not only results in direct crop losses but also cause farmers to embrace huge monetary expenses for disease control and preventive measures. The disease is well known for notorious ‘Irish Famine’ which resulted in drop of Irish population by more than 20% as result of hunger and potato starvation. Globally, annual losses of crop and money spend on fungicides for late blight control exceeds one trillion US dollars. This paper reviews the significance of late blight of potato and controlling strategies adopted for minimizing yield losses incurred by this disease by the use of synthetic fungicides. Advantages and disadvantages of fungicides application are discussed.

Resistance mutation conserved between insects and mites unravels the benzoylurea insecticide mode of action on chitin biosynthesis.

Science.gov (United States)

Douris, Vassilis; Steinbach, Denise; Panteleri, Rafaela; Livadaras, Ioannis; Pickett, John Anthony; Van Leeuwen, Thomas; Nauen, Ralf; Vontas, John

2016-12-20

Despite the major role of chitin biosynthesis inhibitors such as benzoylureas (BPUs) in the control of pests in agricultural and public health for almost four decades, their molecular mode of action (MoA) has in most cases remained elusive. BPUs interfere with chitin biosynthesis and were thought to interact with sulfonylurea receptors that mediate chitin vesicle transport. Here, we uncover a mutation (I1042M) in the chitin synthase 1 (CHS1) gene of BPU-resistant Plutella xylostella at the same position as the I1017F mutation reported in spider mites that confers etoxazole resistance. Using a genome-editing CRISPR/Cas9 approach coupled with homology-directed repair (HDR) in Drosophila melanogaster, we introduced both substitutions (I1056M/F) in the corresponding fly CHS1 gene (kkv). Homozygous lines bearing either of these mutations were highly resistant to etoxazole and all tested BPUs, as well as buprofezin-an important hemipteran chitin biosynthesis inhibitor. This provides compelling evidence that BPUs, etoxazole, and buprofezin share in fact the same molecular MoA and directly interact with CHS. This finding has immediate effects on resistance management strategies of major agricultural pests but also on mosquito vectors of serious human diseases such as Dengue and Zika, as diflubenzuron, the standard BPU, is one of the few effective larvicides in use. The study elaborates on how genome editing can directly, rapidly, and convincingly elucidate the MoA of bioactive molecules, especially when target sites are complex and hard to reconstitute in vitro.

Coating with fungicide and different doses of fertilizer in vinhatico ...

African Journals Online (AJOL)

Lucas

2016-09-21

Sep 21, 2016 ... The treatments were: seed coating with sand + lime + fungicide with different doses of .... The index was calculated based on the formula of Maguire (1962). ..... Ludwig EJ, Nunes UR, Mertz LM, Silva JR, Nunes SCP (2014).

Translocation and metabolism of the fungicide Metalaxyl in rangpur lime seedlings

Energy Technology Data Exchange (ETDEWEB)

Musumeci, M.R.; Ruegg, E.F. (Instituto Biologico, Sao Paulo (Brazil). Centro de Radioisotopos)

1984-08-01

The application of /sup 14/C-metalaxyl to leaves of two and six month-old Rangpur lime (Citrus limonia Osb.) seedlings is studied. In a basal foliar application, 85% of the fungicide remained in the applied leaves, though translocation was verified to upper leaves, stems and roots. When metalaxyl was applied in upper leaves only traces of radiocarbon were detected in roots and stems. After 30 days in the two-and six-month old plants, 70% of the radiocarbon corresponded to the applied fungicide Metalaxyl was degraded in leave tissues to N-(2-methoxyacetil)-N-(2,6-xylyl)-DL-alanine and two others unidentified metabolites. Polar compounds were also detected. Only 1.5% of the radiocarbon was detected as bound residue, not extracted by the acetone extraction.

Effect of Fungicide Applications on Grain Sorghum (Sorghum bicolor L. Growth and Yield

Directory of Open Access Journals (Sweden)

Dan D. Fromme

2017-01-01

Full Text Available Field studies were conducted in the upper Texas Gulf Coast and in central Louisiana during the 2013 through 2015 growing seasons to evaluate the effects of fungicides on grain sorghum growth and development when disease pressure was low or nonexistent. Azoxystrobin and flutriafol at 1.0 L/ha and pyraclostrobin at 0.78 L/ha were applied to the plants of two grain sorghum hybrids (DKS 54-00, DKS 53-67 at 25% bloom and compared with the nontreated check for leaf chlorophyll content, leaf temperature, and plant lodging during the growing season as well as grain mold, test weight, yield, and nitrogen and protein content of the harvested grain. The application of a fungicide had no effect on any of the variables tested with grain sorghum hybrid responses noted. DKS 53-67 produced higher yield, greater test weight, higher percent protein, and N than DKS 54-00. Results of this study indicate that the application of a fungicide when little or no disease is present does not promote overall plant health or increase yield.

Soybean (Glycine max L. Response to Fungicides in the Absence of Disease Pressure

Directory of Open Access Journals (Sweden)

W. James Grichar

2013-01-01

Full Text Available Field studies were conducted during the 2010 and 2011 growing seasons along the Texas Upper Gulf Coast region to study the effects of fungicides on soybean disease development and to evaluate the response of four soybean cultivars to prothioconazole plus trifloxystrobin and pyraclostrobin. In neither year did any soybean diseases develop enough to be an issue. Only NKS 51-T8 responded to a fungicide treatment in 2010 while HBK 5025 responded in 2011. Prothioconazole plus trifloxystrobin increased NKS 51-T8 yield by 23% in 2010 while in 2011 the yield of HBK 5025 was increased 14% over the unsprayed check. No yield response was noted with pyraclostrobin on any soybean cultivar. Only prothioconazole + trifloxystrobin applied to either NKS 51-T8 or DP5335 in 2010 resulted in a net increase in dollars per hectare over the unsprayed check of the respective cultivar. In 2011, under extremely dry conditions, all fungicides with the exception of prothioconazole + trifloxystrobin applied to HBK 5025 resulted in a net decrease in returns over the unsprayed check.

Effect of the spray volume adjustment model on the efficiency of fungicides and residues in processing tomato

Energy Technology Data Exchange (ETDEWEB)

Ratajkiewicz, H.; Kierzek, R.; Raczkowski, M.; Hołodyńska-Kulas, A.; Łacka, A.; Wójtowicz, A.; Wachowiak, M.

2016-11-01

This study compared the effects of a proportionate spray volume (PSV) adjustment model and a fixed model (300 L/ha) on the infestation of processing tomato with potato late blight (Phytophthora infestans (Mont.) de Bary) (PLB) and azoxystrobin and chlorothalonil residues in fruits in three consecutive seasons. The fungicides were applied in alternating system with or without two spreader adjuvants. The proportionate spray volume adjustment model was based on the number of leaves on plants and spray volume index. The modified Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) method was optimized and validated for extraction of azoxystrobin and chlorothalonil residue. Gas chromatography with a nitrogen and phosphorus detector and an electron capture detector were used for the analysis of fungicides. The results showed that higher fungicidal residues were connected with lower infestation of tomato with PLB. PSV adjustment model resulted in lower infestation of tomato than the fixed model (300 L/ha) when fungicides were applied at half the dose without adjuvants. Higher expected spray interception into the tomato canopy with the PSV system was recognized as the reasons of better control of PLB. The spreader adjuvants did not have positive effect on the biological efficacy of spray volume application systems. The results suggest that PSV adjustment model can be used to determine the spray volume for fungicide application for processing tomato crop. (Author)

Effect of the spray volume adjustment model on the efficiency of fungicides and residues in processing tomato

Directory of Open Access Journals (Sweden)

Henryk Ratajkiewicz

2016-08-01

Full Text Available This study compared the effects of a proportionate spray volume (PSV adjustment model and a fixed model (300 L/ha on the infestation of processing tomato with potato late blight (Phytophthora infestans (Mont. de Bary (PLB and azoxystrobin and chlorothalonil residues in fruits in three consecutive seasons. The fungicides were applied in alternating system with or without two spreader adjuvants. The proportionate spray volume adjustment model was based on the number of leaves on plants and spray volume index. The modified Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS method was optimized and validated for extraction of azoxystrobin and chlorothalonil residue. Gas chromatography with a nitrogen and phosphorus detector and an electron capture detector were used for the analysis of fungicides. The results showed that higher fungicidal residues were connected with lower infestation of tomato with PLB. PSV adjustment model resulted in lower infestation of tomato than the fixed model (300 L/ha when fungicides were applied at half the dose without adjuvants. Higher expected spray interception into the tomato canopy with the PSV system was recognized as the reasons of better control of PLB. The spreader adjuvants did not have positive effect on the biological efficacy of spray volume application systems. The results suggest that PSV adjustment model can be used to determine the spray volume for fungicide application for processing tomato crop.

Fungicide application practices and personal protective equipment use among orchard farmers in the agricultural health study.

Science.gov (United States)

Hines, C J; Deddens, J A; Coble, J; Alavanja, M C R

2007-04-01

Fungicides are routinely applied to deciduous tree fruits for disease management. Seventy-four private orchard applicators enrolled in the Agricultural Health Study participated in the Orchard Fungicide Exposure Study in 2002-2003. During 144 days of observation, information was obtained on chemicals applied and applicator mixing, application, personal protective, and hygiene practices. At least half of the applicators had orchards with orchard applicators.

Everybody needs sphingolipids, right! Mining for new drug targets in protozoan sphingolipid biosynthesis.

Science.gov (United States)

Mina, John G M; Denny, P W

2018-02-01

Sphingolipids (SLs) are an integral part of all eukaryotic cellular membranes. In addition, they have indispensable functions as signalling molecules controlling a myriad of cellular events. Disruption of either the de novo synthesis or the degradation pathways has been shown to have detrimental effects. The earlier identification of selective inhibitors of fungal SL biosynthesis promised potent broad-spectrum anti-fungal agents, which later encouraged testing some of those agents against protozoan parasites. In this review we focus on the key enzymes of the SL de novo biosynthetic pathway in protozoan parasites of the Apicomplexa and Kinetoplastidae, outlining the divergence and interconnection between host and pathogen metabolism. The druggability of the SL biosynthesis is considered, alongside recent technology advances that will enable the dissection and analyses of this pathway in the parasitic protozoa. The future impact of these advances for the development of new therapeutics for both globally threatening and neglected infectious diseases is potentially profound.

Fungicides efficiency on wheat diseases control in response to the application with different spray nozzles

Directory of Open Access Journals (Sweden)

Felipe Rafael Garcés Fiallos

2011-12-01

Full Text Available This study aimed to evaluate the efficiency of fungicides to leaf control diseases of wheat, when applied to different models of spray nozzles. The experiment was conducted in a randomized block design with four replicates of factorial (4 x 3+1. Data were subjected to analysis of variance and means compared by Tukey test at 5% probability. The fungicides used were: Opera® (pyraclostrobin+epoxiconazole 0.75 L.ha-1 , Opera® 0.75 L.ha-1 +Folicur® (tebuconazole 0.3 L.ha-1 , Priori Xtra® (azoxystrobin+cyproconazole 0.3 L.ha-1 , Priori Xtra® 0.3 L.ha-1 +Tilt® (propiconazole 0.3 L.ha-1 . These fungicides were applied with three models of spray nozzles jet planes: XR 11 001 (fine drop, AIRMIX 11,001 (average drop and AVI 11,001 (coarse drop. We evaluated the incidence and severity (damage per plant leaf of yellow spot (Drechslera tritici-repentis, spot blotch (Bipolaris sorokiniana, leaf rust (Puccinia triticina and grain yield (kg.ha-1 culture. The results show that the application of fungicides for control of leaf diseases in wheat resulted in increases in grain yield, and yield higher values were observed with the application of Opera®, using the XR 11001.

Environmental fate of fungicides and other current-use pesticides in a central California estuary

Science.gov (United States)

Smalling, Kelly L.; Kuivila, Kathryn; Orlando, James L.; Phillips, Bryn M.; Anderson, Brian S.; Siegler, Katie; Hunt, John W.; Hamilton, Mary

2013-01-01

The current study documents the fate of current-use pesticides in an agriculturally-dominated central California coastal estuary by focusing on the occurrence in water, sediment and tissue of resident aquatic organisms. Three fungicides (azoxystrobin, boscalid, and pyraclostrobin), one herbicide (propyzamide) and two organophosphate insecticides (chlorpyrifos and diazinon) were detected frequently. Dissolved pesticide concentrations in the estuary corresponded to the timing of application while bed sediment pesticide concentrations correlated with the distance from potential sources. Fungicides and insecticides were detected frequently in fish and invertebrates collected near the mouth of the estuary and the contaminant profiles differed from the sediment and water collected. This is the first study to document the occurrence of many current-use pesticides, including fungicides, in tissue. Limited information is available on the uptake, accumulation and effects of current-use pesticides on non-target organisms. Additional data are needed to understand the impacts of pesticides, especially in small agriculturally-dominated estuaries.

RAMAN SPECTROSCOPY-BASED METABOLOMICS FOR DIFFERENTIATING TOXICITIES OF TRIAZOLE FUNGICIDES

Science.gov (United States)

Conazole fungicides are widely used both agriculturally for the protection of crops, and pharmaceutically in the treatment of topical and systemic infections. Heavy usage has created concern over the impact these compounds may have through environmental exposure to humans and ot...

RAMAN SPECTROSCOPY-BASED METABOLOMICS FOR DIFFERENTIATING TOXICITIES OF CONAZOLE FUNGICIDES

Science.gov (United States)

Conazole fungicides are widely used both agriculturally for the protection of crops, and pharmaceutically in the treatment of topical and systemic infections. Heavy usage has created concern over the impact these compounds may have through environmental exposure to humans and ot...

AmcA - a putative mitochondrial ornithine transporter supporting fungal siderophore biosynthesis

Directory of Open Access Journals (Sweden)

Lukas eSchafferer

2015-04-01

Full Text Available Iron is an essential nutrient required for a wide range of cellular processes. The opportunistic fungal pathogen Aspergillus fumigatus employs low-molecular mass iron-specific chelators, termed siderophores, for uptake, storage and intracellular iron distribution, which play a crucial role in the pathogenicity of this fungus. Siderophore biosynthesis depends on coordination with the supply of its precursor ornithine, produced mitochondrially from glutamate or cytosolically via hydrolysis of arginine. In this study, we demonstrate a role of the putative mitochondrial transporter AmcA (AFUA_8G02760 in siderophore biosynthesis of A. fumigatus.Consistent with a role in cellular ornithine handling, AmcA-deficiency resulted in decreased cellular ornithine and arginine contents as well as decreased siderophore production on medium containing glutamine as the sole nitrogen source. In support, arginine and ornithine as nitrogen sources did not impact siderophore biosynthesis due to cytosolic ornithine availability. As revealed by Northern blot analysis, transcript levels of siderophore biosynthetic genes were unresponsive to the cellular ornithine level. In contrast to siderophore production, AmcA deficiency did only mildly decrease the cellular polyamine content, demonstrating cellular prioritization of ornithine use. Nevertheless, AmcA-deficiency increased the susceptibility of A. fumigatus to the polyamine biosynthesis inhibitor eflornithine, most likely due to the decreased ornithine pool. AmcA-deficiency decreased the growth rate particularly on ornithine as the sole nitrogen source during iron starvation and sufficiency, indicating an additional role in the metabolism and fitness of A. fumigatus, possibly in mitochondrial ornithine import. In the Galleria mellonella infection model, AmcA-deficiency did not affect virulence of A. fumigatus, most likely due to the residual siderophore production and arginine availability in this host niche.

FUNGICIDAL PROPERTIES OF ARTEMISIA AROMATIC PLANTS TOWARDS FUSARIUM OXYSPORUM

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Ivashchenko Iryna Vіctorovna

2015-08-01

Full Text Available The article establishes the fungicidal activity of water extracts of Artemisia maritimа L., Artemisia austriaca Jacq., under the concentration of 100, 50 and 25 mg/ml on dry matter with regard to the phytopathogenic mushroom Fusarium oxysporum. It also shows the fungistatic influence of extract of Artemisia dracunculus L. under concentration 25 and 50 mg/ml, fungicidal – under 100 mg/ml. Concerning Artemisia abrotanum L., the slow growth of mushroom is observed under the concentration 25 mg/ml, fungicidal effect – under 50 and 100 mg/ml. The paper provides the information on the component composition of ethereal oil and phenolic compounds of Artemisia maritimа, Artemisia austriaca, Artemisia abrotanum, Artemisia dracunculus, cultivated in Zhytomyr Polissya. The chief ingredients of ethereal oil which is synthesized by the plant of Artemisia abrotanum are 1,8-cineole (30.44% and camphor (31.92%. A high 1,8-cineole and camphor content determines antimicrobial properties of the plants. Amount of phenolic compounds in the air-dry raw Artemisia abrotanum is 2.98 percent. By the method of highly efficient solution chromatography (HESChr in the grass of Artemisia abrotanum we have detected 23 phenolic compounds, of which we identified such flavonoids as rutin, luteolin-7-glycoside as well as caffeic, chlorogenic and isochlorogenic acids. The main compounds of ethereal oil of Artemisia austriaca are trans-verbenole (30.77 %, pinocarvone (10.77 % and sabinilacetate (18.16 %. In the grass of Artemisia austriaca we have detected 31 phenolic compounds, of which we identified such flavonoids as rutin, apigenin, quercetin-bioside and the following acids: caffeic, chlorogenic, and isochlorogenic. Amount of phenolic compounds in the air-dry raw Austrian wormwood is 27.25 mg / g (2.73 %. The main component of ethereal oil of Artemisia dracunculus is methyleugenol (94.65 %. We have discovered 31 phenolic compounds in the grass of linear-leaved wormwood

Development of biodegradable fungicide by radiation

Energy Technology Data Exchange (ETDEWEB)

Lee, Young Keun; Kim, Dong Sub [KAERI, Daejeon (Korea, Republic of)

2011-01-15

To develop the fungicide which is biodegradable and alternative to chemical pesticide that has an side effect of environmental pollution, Mutant induction of the enhanced antifungal activity was studied by using radiation. Characteristics and structure of antifungal biomaterials derived from these mutants were analysed. Two biomaterials related to the antifungal activity from the above mutant were isolated and purified. Microbial pesticide were manufactured in combination of various additives. Antiphytopathogenic effects were proven by pot experiment and It was promising to prevent pepper, Chinese cabbage and radish from anthrax, phytophthora and root rot

Development of biodegradable fungicide by radiation

Energy Technology Data Exchange (ETDEWEB)

Lee, Youngkeun; Kim, Dongsub

2012-03-15

To develop the fungicide which is biodegradable and alternative to chemical pesticide that has an side effect of environmental pollution, Mutant induction of the enhanced antifungal activity was studied by using radiation. Characteristics and structure of antifungal biomaterials derived from these mutants were analysed. Two biomaterials related to the antifungal activity from the above mutant were isolated and purified. Microbial pesticide were manufactured in combination of various additives. Antiphytopathogenic effects were proven by field test and it was promising to prevent Chinese cabbage and radish from phytophthora and root rot.

Development of biodegradable fungicide by radiation

International Nuclear Information System (INIS)

Lee, Young Keun; Kim, Dong Sub

2011-01-01

To develop the fungicide which is biodegradable and alternative to chemical pesticide that has an side effect of environmental pollution, Mutant induction of the enhanced antifungal activity was studied by using radiation. Characteristics and structure of antifungal biomaterials derived from these mutants were analysed. Two biomaterials related to the antifungal activity from the above mutant were isolated and purified. Microbial pesticide were manufactured in combination of various additives. Antiphytopathogenic effects were proven by pot experiment and It was promising to prevent pepper, Chinese cabbage and radish from anthrax, phytophthora and root rot

Development of biodegradable fungicide by radiation

International Nuclear Information System (INIS)

Lee, Young Jeun; Kim, Dong Sub

2010-01-01

To develop the fungicide which is biodegradable and alternative to chemical pesticide that has an side effect of environmental pollution, Mutant induction of the enhanced antifungal activity was studied by using radiation. Characteristics and structure of antifungal biomaterials derived from these mutants were analysed. Sixteen antifungal microbes were isolated and 4 antifungal activity enhanced mutants were induced by using radiation. P. lentimorbus WJ5a17 had 41% higher antifungal activity than the wild type. Two biomaterials related to the antifungal activity from the above mutant were isolated and purified

Development of biodegradable fungicide by radiation

International Nuclear Information System (INIS)

Lee, Youngkeun; Kim, Dongsub

2012-03-01

To develop the fungicide which is biodegradable and alternative to chemical pesticide that has an side effect of environmental pollution, Mutant induction of the enhanced antifungal activity was studied by using radiation. Characteristics and structure of antifungal biomaterials derived from these mutants were analysed. Two biomaterials related to the antifungal activity from the above mutant were isolated and purified. Microbial pesticide were manufactured in combination of various additives. Antiphytopathogenic effects were proven by field test and it was promising to prevent Chinese cabbage and radish from phytophthora and root rot

Discovering Novel Alternaria solani Succinate Dehydrogenase Inhibitors by in Silico Modeling and Virtual Screening Strategies to Combat Early Blight

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Sehrish Iftikhar

2017-11-01

Full Text Available Alternaria blight is an important foliage disease caused by Alternaria solani. The enzyme Succinate dehydrogenase (SDH is a potential drug target because of its role in tricarboxylic acid cycle. Hence targeting Alternaria solani SDH enzyme could be efficient tool to design novel fungicides against A. solani. We employed computational methodologies to design new SDH inhibitors using homology modeling; pharmacophore modeling and structure based virtual screening. The three dimensional SDH model showed good stereo-chemical and structural properties. Based on virtual screening results twelve commercially available compounds were purchased and tested in vitro and in vivo. The compounds were found to inhibit mycelial growth of A. solani. Moreover in vitro trials showed that inhibitory effects were enhanced with increase in concentrations. Similarly increased disease control was observed in pre-treated potato tubers. Hence the applied in silico strategy led us to identify novel fungicides.

Inhibitory effects of azole-type fungicides on interleukin-17 gene expression via retinoic acid receptor-related orphan receptors α and γ

Energy Technology Data Exchange (ETDEWEB)

Kojima, Hiroyuki, E-mail: kojima@iph.pref.hokkaido.jp [Hokkaido Institute of Public Health, Kita-19, Nishi-12, Kita-ku, Sapporo 060-0819 (Japan); Muromoto, Ryuta; Takahashi, Miki [Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812 (Japan); Takeuchi, Shinji [Hokkaido Institute of Public Health, Kita-19, Nishi-12, Kita-ku, Sapporo 060-0819 (Japan); Takeda, Yukimasa; Jetten, Anton M. [National Institute of Environmental Health Sciences, National Institutes of Health, 111 T. W. Alexander Drive, Research Triangle Park, NC 27709 (United States); Matsuda, Tadashi [Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812 (Japan)

2012-03-15

The retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ), are key regulators of helper T (Th)17 cell differentiation, which is involved in the innate immune system and autoimmune disorders. However, it remains unclear whether environmental chemicals, including pesticides, have agonistic and/or antagonistic activity against RORα/γ. In this study, we investigated the RORα/γ activity of several azole-type fungicides, and the effects of these fungicides on the gene expression of interleukin (IL)-17, which mediates the function of Th17 cells. In the ROR-reporter gene assays, five azole-type fungicides (imibenconazole, triflumizole, hexaconazole, tetraconazole and imazalil) suppressed RORα- and/or RORγ-mediated transcriptional activity as did benzenesulphonamide T0901317, a ROR inverse agonist and a liver X receptor (LXR) agonist. In particular, imibenconazole, triflumizole and hexaconazole showed RORγ inverse agonistic activity at concentrations of 10{sup −6} M. However, unlike T0901317, these fungicides failed to show any LXRα/β agonistic activity. Next, five azole-type fungicides, showing ROR inverse agonist activity, were tested on IL-17 mRNA expression in mouse T lymphoma EL4 cells treated with phorbol myristate acetate and ionomycin. The quantitative RT-PCR analysis revealed that these fungicides suppressed the expression of IL-17 mRNA without effecting RORα and RORγ mRNA levels. In addition, the inhibitory effect of imibenconazole as well as that of T0901317 was absorbed in RORα/γ-knocked down EL4 cells. Taken together, these results suggest that some azole-type fungicides inhibit IL-17 production via RORα/γ. This also provides the first evidence that environmental chemicals can act as modulators of IL-17 expression in immune cells. -- Highlights: ► Nuclear receptors, RORα and RORγ, are key regulators of Th17 cell differentiation. ► Five azole-type fungicides act as RORα/γ inverse agonists. ► These fungicides

Inhibitory effects of azole-type fungicides on interleukin-17 gene expression via retinoic acid receptor-related orphan receptors α and γ

International Nuclear Information System (INIS)

Kojima, Hiroyuki; Muromoto, Ryuta; Takahashi, Miki; Takeuchi, Shinji; Takeda, Yukimasa; Jetten, Anton M.; Matsuda, Tadashi

2012-01-01

The retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ), are key regulators of helper T (Th)17 cell differentiation, which is involved in the innate immune system and autoimmune disorders. However, it remains unclear whether environmental chemicals, including pesticides, have agonistic and/or antagonistic activity against RORα/γ. In this study, we investigated the RORα/γ activity of several azole-type fungicides, and the effects of these fungicides on the gene expression of interleukin (IL)-17, which mediates the function of Th17 cells. In the ROR-reporter gene assays, five azole-type fungicides (imibenconazole, triflumizole, hexaconazole, tetraconazole and imazalil) suppressed RORα- and/or RORγ-mediated transcriptional activity as did benzenesulphonamide T0901317, a ROR inverse agonist and a liver X receptor (LXR) agonist. In particular, imibenconazole, triflumizole and hexaconazole showed RORγ inverse agonistic activity at concentrations of 10 −6 M. However, unlike T0901317, these fungicides failed to show any LXRα/β agonistic activity. Next, five azole-type fungicides, showing ROR inverse agonist activity, were tested on IL-17 mRNA expression in mouse T lymphoma EL4 cells treated with phorbol myristate acetate and ionomycin. The quantitative RT-PCR analysis revealed that these fungicides suppressed the expression of IL-17 mRNA without effecting RORα and RORγ mRNA levels. In addition, the inhibitory effect of imibenconazole as well as that of T0901317 was absorbed in RORα/γ-knocked down EL4 cells. Taken together, these results suggest that some azole-type fungicides inhibit IL-17 production via RORα/γ. This also provides the first evidence that environmental chemicals can act as modulators of IL-17 expression in immune cells. -- Highlights: ► Nuclear receptors, RORα and RORγ, are key regulators of Th17 cell differentiation. ► Five azole-type fungicides act as RORα/γ inverse agonists. ► These fungicides suppress

The effect of nitrogen fertilizing and fungicide application on the yield and selected parameters of grain quality of winter wheat

Directory of Open Access Journals (Sweden)

Alena Bezdíčková

2007-01-01

Full Text Available In 2001–2004 an influence of gradually increased portions of nitrogen (100–130–160 kg/N.ha–1 applied on the wheat variety Ebi in combination with the modified fungicidal protection in the yield and the selected quality grain parameters were observed within the small-plot field trials. Nitrogenous fertilizers according to the amount of nitrogen contained were applied in 2–4 terms during vegetation in regeneration (55kg/N.ha–1, 1st production (45kg/N.ha–1, 2nd production (30kg/N.ha–1 and qualitative portion (30kg/N.ha–1. The fungicidal protection was based on the equal treatment in the phase of BBCH 37 and with regard to the varieties different treatment in the phase of BBCH 55. The dependence on the year was proved at all observed parameters. Higher intensity of nitrogenous fertilization had no decisive impact on the yields. From the point of view of increased yields, the second production nitrogenous fertilization had the strongest impact; it increased the grain yields by 0.084–0.461 t./ha–1. Higher intensity of nitrogenous fertilization positively influenced the baker’s grain quality. The increased portions of nitrogen decisively increased the volume of N-substances in all trial years. The second production nitrogenous fertilization increased the N-substances volume from 0.1 to 0.8%. Qualitative additional fertilization increased their volume from 0.26 to 1.38%. Higher N portions increased sedimentation in most cases. The falling number was not considerably influenced. The mechanical grain qualities (volume weight, number full grains, and GTW were relatively less influenced than the baker’s quality by the nitrogenous fertilization. The application of fungicides positively influenced not only the yields but also mechanical qualities of the grain, i.e. volume weight, thousand grains weight and portion of Full grains. On the contrary the baker’s quality was not decisively influenced. It was proved that the decisive

field tolerance of selected varieties to and fungicide efficacy against ...

African Journals Online (AJOL)

ACSS

and median temperatures of 28°C (Osiru et al.,. 2007), it has the potential ... this study was to evaluate a wide range of sweet ... following each fungicide application to reduce wash-off. ..... specific mode of action (Avenot and Michailides,. 2007 ...

Effects of four fungicides on nine non-target submersed macrophytes

NARCIS (Netherlands)

Belgers, J.D.M.; Aalderink, G.H.; Brink, van den P.J.

2009-01-01

We tested the sensitivity of nine submersed macrophyte species to the fungicides chlorothalonil, pentachlorophenol, fluazinam, and carbendazim. Endpoints determined 3 weeks after the start of the treatment were based on shoot and root growth in water. Carbendazim proved not or only moderately toxic

High glucose suppresses human islet insulin biosynthesis by inducing miR-133a leading to decreased polypyrimidine tract binding protein-expression.

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Rikard G Fred

Full Text Available BACKGROUND: Prolonged periods of high glucose exposure results in human islet dysfunction in vitro. The underlying mechanisms behind this effect of high glucose are, however, unknown. The polypyrimidine tract binding protein (PTB is required for stabilization of insulin mRNA and the PTB mRNA 3'-UTR contains binding sites for the microRNA molecules miR-133a, miR-124a and miR-146. The aim of this study was therefore to investigate whether high glucose increased the levels of these three miRNAs in association with lower PTB levels and lower insulin biosynthesis rates. METHODOLOGY/PRINCIPAL FINDINGS: Human islets were cultured for 24 hours in the presence of low (5.6 mM or high glucose (20 mM. Islets were also exposed to sodium palmitate or the proinflammatory cytokines IL-1beta and IFN-gamma, since saturated free fatty acids and cytokines also cause islet dysfunction. RNA was then isolated for real-time RT-PCR analysis of miR-133a, miR-124a, miR-146, insulin mRNA and PTB mRNA contents. Insulin biosynthesis rates were determined by radioactive labeling and immunoprecipitation. Synthetic miR-133a precursor and inhibitor were delivered to dispersed islet cells by lipofection, and PTB was analyzed by immunoblotting following culture at low or high glucose. Culture in high glucose resulted in increased islet contents of miR-133a and reduced contents of miR-146. Cytokines increased the contents of miR-146. The insulin and PTB mRNA contents were unaffected by high glucose. However, both PTB protein levels and insulin biosynthesis rates were decreased in response to high glucose. The miR-133a inhibitor prevented the high glucose-induced decrease in PTB and insulin biosynthesis, and the miR-133a precursor decreased PTB levels and insulin biosynthesis similarly to high glucose. CONCLUSION: Prolonged high-glucose exposure down-regulates PTB levels and insulin biosynthesis rates in human islets by increasing miR-133a levels. We propose that this mechanism

Translocation and metabolism of the fungicide Metalaxyl in rangpur lime seedlings

International Nuclear Information System (INIS)

Musumeci, M.R.; Ruegg, E.F.

1984-01-01

The application of 14 C-metalaxyl to leaves of two and six month-old Rangpur lime (Citrus limonia Osb.) seedlings is studied. In a basal foliar application, 85% of the fungicide remained in the applied leaves, though translocation was verified to upper leaves, stems and roots. When metalaxyl was applied in upper leaves only traces of radiocarbon were detected in roots and stems. After 30 days in the two-and six-month old plants, 70% of the radiocarbon corresponded to the applied fungicide Metalaxyl was degraded in leave tissues to N-(2-methoxyacetil)-N-(2,6-xylyl)-DL-alanine and two others unidentified metabolites. Polar compounds were also detected. Only 1.5% of the radiocarbon was detected as bound residue, not extracted by the acetone extraction. (Author) [pt

Phytotoxicity of the combination of some insecticides and fungicides on the ornamental species Petunia sp.

Directory of Open Access Journals (Sweden)

Renata Bažok

2016-12-01

Full Text Available In the production of ornamental plants, it is often necessary to combine plant protection products (PPPs for simultaneous pest control. The use of a combination of PPPs often leads to phytotoxicity. The aim of this study was to determine the phytotoxicity of the combination of fungicides (azoxystrobin and cyprodinil + fludioxonil and insecticides based on abamectin and thiomethoxam on the ornamental plant Petunia sp. The PPPs are used at recommended and double doses. Based on the damage, phytotoxicity indices were calculated. Petunia plants are sensitive even when PPPs are used in recommended doses. Combinations of the both insecticides with the combined fungicide based on cyprodinil and fludioxinil can be advised to protect petunias only if one applies the recommended doses. All combinations of insecticides with a fungicide based on azoxystrobin should not be applied because there is a serious risk of phytotoxicity.

FUNGICIDES IN SECOND HARVEST CORN: CERCOSPORIOSE CONTROL AND BLOTCH, PRODUCTIVITY, ECONOMIC RETURN AND GRAIN QUALITY

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P. Rezende

2017-10-01

Full Text Available Os objetivos desse trabalho foram avaliar a eficiência de The aim of this study was evaluate efficacy fungicides to control cercospora leaf spot (Cercospora zeae-maydis and helminthosporium leaf blight (Exserohilumturcicum, productivity, economic returns and quality of grain of corn culture of second crop in Farm Bandeirantes at Feliz Natal/MT. The treatments evaluated were: pyraclostrobina+epoxiconazol (0,7 L ha-1, trifloxistrobina+protioconazol (0,3L ha-1, azoxistrobina+cyproconazol(0,3 L ha-1, azoxystrobina (0,25 L ha-1, trifloxistrobina+ciproconazol (0,2 L ha-1 and control. Theapplicationof products occurred when corn was with 55 days, with a high propelled sprayer. The experimental design was a randomized block, with 6 treatments and 3 replications. The severity of each disease was visually determined through periodic analyses and ten plants were marked in each repetition, which were evaluated during the entire crop cycle. The data of severity obtained were used to calculate the area under disease progress curve (AUDPC. It was also obtained the production per ha, the economic return (R$ ha-1 and physiological quality of grain was evaluated by germination tests and accelerated aging of the grains. All treatments had significant difference compared to the control sample in controlling cercospora leaf spot about the control of helminthosporiumleat blight, the fungicides trifloxystrobin+prothioconazol and trifloxystrobin+cyproconazol were not efficient, and the fungicides pyraclostrobina+epoxiconazol, azoxystrobina, azoxistrobina+cyproconazol were efficient. The treatments that had major production are from the group of triazoles+strobilurine and the fungicide pyraclostrobin+epoxyconazol showed greater economic viability. Not were differences among fungicides, and neither of the treatments compared to control, in germination and accelerated aging tests, showing that the grains have good quality characteristics

Effects of Artea, a systemic fungicide, on the antioxidant system and ...

African Journals Online (AJOL)

Effects of Artea, a systemic fungicide, on the antioxidant system and the respiratory activity of durum wheat ( Triticum durum L .). ... African Journal of Biotechnology ... Root respiratory activity was also determined using a polarographic method ...

Rainfall thresholds as support for timing fungicide applications in the control of potato late blight in Ecuador and Peru

DEFF Research Database (Denmark)

Kromann, Peter; Taipe, Arturo; Perez, Willmer G.

2009-01-01

Accumulated rainfall thresholds were studied in seven field experiments conducted in Ecuador and Peru for their value in timing applications of fungicide to control potato late blight, caused by Phytophthora infestans. Fungicide regimes based on accumulated rainfall thresholds ranging from 10 to 70...

Sustained release of fungicide metalaxyl by mesoporous silica nanospheres

Energy Technology Data Exchange (ETDEWEB)

Wanyika, Harrison, E-mail: hwanyika@gmail.com [Jomo Kenyatta University of Agriculture and Technology, Department of Chemistry (Kenya)

2013-08-15

The use of nanomaterials for the controlled delivery of pesticides is nascent technology that has the potential to increase the efficiency of food production and decrease pollution. In this work, the prospect of mesoporous silica nanoparticles (MSN) for storage and controlled release of metalaxyl fungicide has been investigated. Mesoporous silica nanospheres with average particle diameters of 162 nm and average pore sizes of 3.2 nm were prepared by a sol-gel process. Metalaxyl molecules were loaded into MSN pores from an aqueous solution by a rotary evaporation method. The loaded amount of metalaxyl as evaluated by thermogravimetric analysis was about 14 wt%. Release of the fungicide entrapped in the MSN matrix revealed sustained release behavior. About 76 % of the free metalaxyl was released in soil within a period of 30 days while only 11.5 and 47 % of the metalaxyl contained in the MSN carrier was released in soil and water, respectively, within the same period. The study showed that MSN can be used to successfully store metalaxyl molecules in its mesoporous framework and significantly delay their release in soil.

Sustained release of fungicide metalaxyl by mesoporous silica nanospheres

International Nuclear Information System (INIS)

Wanyika, Harrison

2013-01-01

The use of nanomaterials for the controlled delivery of pesticides is nascent technology that has the potential to increase the efficiency of food production and decrease pollution. In this work, the prospect of mesoporous silica nanoparticles (MSN) for storage and controlled release of metalaxyl fungicide has been investigated. Mesoporous silica nanospheres with average particle diameters of 162 nm and average pore sizes of 3.2 nm were prepared by a sol–gel process. Metalaxyl molecules were loaded into MSN pores from an aqueous solution by a rotary evaporation method. The loaded amount of metalaxyl as evaluated by thermogravimetric analysis was about 14 wt%. Release of the fungicide entrapped in the MSN matrix revealed sustained release behavior. About 76 % of the free metalaxyl was released in soil within a period of 30 days while only 11.5 and 47 % of the metalaxyl contained in the MSN carrier was released in soil and water, respectively, within the same period. The study showed that MSN can be used to successfully store metalaxyl molecules in its mesoporous framework and significantly delay their release in soil

Joint use of fungicides, insecticides and inoculants in the treatment of soybean seeds

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Yara Cristiane Buhl Gomes

Full Text Available ABSTRACT The interference of the joint application of pesticides with seed inoculation on the survival of Bradyrhizobium has been reported in the last years. So, the objective of this study was to evaluate the joint use of fungicides, insecticides and inoculant in the treatment of soybean seeds on various parameters of Bradyrhizobium nodulation in soybean as well as on crop productivity parameters. The experiment was conducted during the 2013/2014 crop in the experimental field of the Instituto Federal de Educação, Ciência e Tecnologia de Mato Grosso - Campo Novo do Parecis Campus. The seeds of TMG 133 RR variety were sown in pots. It was used a randomized block design in a 4 x 4 + 1 factorial, four fungicides (1: fludioxonil + metalaxyl-M, 2: carboxine + thiram, 3: difeconazole and 4: carbendazim + thiram, four insecticides (1: fipronil 250 SC, 2: thiamethoxam, 3: imidacloprid + thiodicarpe and 4: imodacloprid 600 FC and an inoculant (SEMIA 5079 and SEMIA 5080, common to all treatments, with three replications. The experiment was not repeated. The joint application of fungicide and insecticide with inoculant does not affect nodulation, foliar N content and vegetative growth of the plants as well as the masses of grains per plant and 100-grain mass. The use of the carbendazim + thiram mixed with fipronil and carbendazim + thiram mixed with imidacloprid provides less number of pods per plant and grains per plant, reflecting in reductions in the production of soybean grains. In this way, the fungicide carbendazim + thiram, regardless of the combined applied insecticide, is the most harmful to Bradyrhizobium spp.

Observations on the Behaviour of Different Populations of Plasmopara viticola Resistant to QoI Fungicides in Italian Vineyards

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M.L. Gullino

2004-12-01

Full Text Available Grapevine downy mildew, caused by Plasmopara viticola, is probably the most damaging fungal disease of grapevine world-wide. Among the fungicides recently developed for downy mildew control is the QoI class of fungicides, which inhibits mitochondrial respiration. Since 1999, selected P. viticola populations in northern Italy have been monitored for resistance to QoI fungicides. Detached leaf discs and whole potted plants were used under controlled conditions to test the sampled populations. QoI-resistant populations of P. viticola were found in all the vineyards sampled in 2001 and 2002 in Trentino Alto Adige and Friuli Venezia Giulia, where failure in QoI control was reported. Many of the populations had minimum inhibition concentration (MIC values 3– 30 times higher than those of sensitive reference populations. Populations of P. viticola sampled from vineyards in Piedmont, where no QoI fungicides had previously been used, showed MIC values equal to, or lower than those of the reference populations. Most of the P. viticola populations collected in Trentino Alto Adige in 2001 showed high virulence in leaf disc test and were not controlled by QoI fungicides, applied both at field and double field rates in the whole plant test. Most of these populations retained their virulence in the subsequent leaf disc test in water.

Combinations of fungicide and cultural practices influence the incidence and impact of fusiform rust in slash pine plantations

Science.gov (United States)

James D. Haywood; Allan E. Tiarks

1994-01-01

Slash pine was grown in central Louisiana under four levels of culture with or without repeated sprayings of the systematic fungicide triadimefon for protection against fusiform rust. The eight treatment combinations were: (1)no fungicide, weed control, or fertilizer; (2)weeded; (3)weeded, applied inorganic fertilizer, and bedded before planting; (4)weeded, bedded,...

Crystal structures of Leishmania mexicana arginase complexed with α,α-disubstituted boronic amino-acid inhibitors

Energy Technology Data Exchange (ETDEWEB)

Hai, Yang; Christianson, David W.

2016-03-16

Leishmaniaarginase is a potential drug target for the treatment of leishmaniasis because this binuclear manganese metalloenzyme initiatesde novopolyamine biosynthesis by catalyzing the hydrolysis of L-arginine to generate L-ornithine and urea. The product L-ornithine subsequently undergoes decarboxylation to yield putrescine, which in turn is utilized for spermidine biosynthesis. Polyamines such as spermidine are essential for the growth and survival of the parasite, so inhibition of enzymes in the polyamine-biosynthetic pathway comprises an effective strategy for treating parasitic infections. To this end, two X-ray crystal structures ofL. mexicanaarginase complexed with α,α-disubstituted boronic amino-acid inhibitors based on the molecular scaffold of 2-(S)-amino-6-boronohexanoic acid are now reported. Structural comparisons with human and parasitic arginase complexes reveal interesting differences in the binding modes of the additional α-substituents,i.e.the D side chains, of these inhibitors. Subtle differences in the three-dimensional contours of the outer active-site rims among arginases from different species lead to different conformations of the D side chains and thus different inhibitor-affinity trends. The structures suggest that it is possible to maintain affinity while fine-tuning intermolecular interactions of the D side chain of α,α-disubstituted boronic amino-acid inhibitors in the search for isozyme-specific and species-specific arginase inhibitors.

Disease control by chemical and biological fungicides in cultivated mushrooms: button mushroom, oyster mushroom and shiitake

Directory of Open Access Journals (Sweden)

Ivana Potočnik

2015-12-01

Full Text Available The most commonly cultivated basidiomycetes worldwide and in Serbia are button mushroom (Agaricus bisporus, oyster mushroom (Pleurotus sp. and shiitake (Lentinus edodes. Production of their fruiting bodies is severely afflicted by fungal, bacterial, and viral pathogens that are able to cause diseases which affect yield and quality. Major A. bisporus fungal pathogens include Mycogone perniciosa, Lecanicillium fungicola, and Cladobotryum spp., the causal agents of dry bubble, wet bubble, and cobweb disease, respectively. Various Trichoderma species, the causal agents of green mould, also affect all three kinds of edible mushrooms. Over the past two decades, green mould caused by T. aggressivum has been the most serious disease of button mushroom. Oyster mushroom is susceptible to T. pleurotum and shiitake to T. harzianum. The bacterial brawn blotch disease, caused by Pseudomonas tolaasii, is distributed globally. Disease control on mushroom farms worldwide is commonly based on the use of fungicides. However, evolution of pathogen resistance to fungicides after frequent application, and host sensitivity to fungicides are serious problems. Only a few fungicides are officially recommended in mushroom production: chlorothalonil and thiabendazol in North America and prochloraz in the EU and some other countries. Even though decreased sensitivity levels of L. fungicola and Cladobotryum mycophilum to prochloraz have been detected, disease control is still mainly provided by that chemical fungicide. Considering such resistance evolution, harmful impact to the environment and human health, special attention should be focused on biofungicides, both microbiological products based on Bacillus species and various natural substances of biological origin, together with good programs of hygiene. Introduction of biofungicides has created new possibilities for crop protection with reduced application of chemicals.

Investigations on the isoprenoid biosynthesis in the green alga Scenedesmus obliquus by using the 13C-labelling technique

International Nuclear Information System (INIS)

Schwender, J.

1995-01-01

The biosynthesis of several prenyllipids (isoprenoid lipids) of the green alga Scendesmus obliquus was investigated. The aim was to verify, whether the biosynthesis of isopentenyl diphosphate (IPP) in Scenedesmus proceeds according to the classical acetate mevalonate pathway or to an alternative pathway. An alternative pathway for IPP formation has recently been detected in some eubacteria by the group of Prof. M. Rohmer. Some inhibition tests were performed with mevinolin, a specific inhibitor of HMG-CoA reductase which yields mevalonic acid. Mevinolin should block the biosynthesis of such isoprenoids which are formed via the acetate mevalonate pathway. Scenedesmus was grown heterotrophically on 13 C-labelled glucose or acetate. After isolation and purification of 13 C-labelled phytol (side chains of chlorophylls), β-carotene, lutein, plastoquinone-9 and three sterol compounds, the enrichment of 13 C at different carbon-positions of the labelled compounds was determined. This was achieved by the 13 C-NMR technique in cooperation with Miriam Seemann of the group of Prof. M. Rohmer in Mullhouse/France. (orig.) [de

POMICS: A Simulation Disease Model for Timing Fungicide Applications in Management of Powdery Mildew of Cucurbits.

Science.gov (United States)

Sapak, Z; Salam, M U; Minchinton, E J; MacManus, G P V; Joyce, D C; Galea, V J

2017-09-01

A weather-based simulation model, called Powdery Mildew of Cucurbits Simulation (POMICS), was constructed to predict fungicide application scheduling to manage powdery mildew of cucurbits. The model was developed on the principle that conditions favorable for Podosphaera xanthii, a causal pathogen of this crop disease, generate a number of infection cycles in a single growing season. The model consists of two components that (i) simulate the disease progression of P. xanthii in secondary infection cycles under natural conditions and (ii) predict the disease severity with application of fungicides at any recurrent disease cycles. The underlying environmental factors associated with P. xanthii infection were quantified from laboratory and field studies, and also gathered from literature. The performance of the POMICS model when validated with two datasets of uncontrolled natural infection was good (the mean difference between simulated and observed disease severity on a scale of 0 to 5 was 0.02 and 0.05). In simulations, POMICS was able to predict high- and low-risk disease alerts. Furthermore, the predicted disease severity was responsive to the number of fungicide applications. Such responsiveness indicates that the model has the potential to be used as a tool to guide the scheduling of judicious fungicide applications.

Assessment of Total Risk on Non-Target Organisms in Fungicide Application for Agricultural Sustainability

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Ali Musa Bozdogan

2014-02-01

Full Text Available In Turkey, in 2010, the amount of pesticide (active ingredient; a.i. used in agriculture was about 23,000 metric tons, of which approximately 32% was fungicides. In 2012, 14 a.i. were used for fungus control in wheat cultivation areas in Adana province, Turkey. These a.i. were: azoxystrobin, carbendazim, difenoconazole, epoxiconazole, fluquinconazole, prochloraz, propiconazole, prothioconazole, pyraclostrobin, spiroxamine, tebuconazole, thiophanate-methyl, triadimenol, and trifloxystrobin. In this study, the potential risk of a.i. on non-target organisms in fungicide application of wheat cultivation was assessed by The Pesticide Occupational and Environmental Risk (POCER indicators. In this study, the highest human health risk was for fluquinconazole (Exceedence Factor (EF 1.798 for human health, whereas the fungicide with the highest environmental risk was propiconazole (EF 2.000 for the environment. For non-target organisms, the highest potential risk was determined for propiconazole when applied at 0.1250 kg a.i. ha-1 (EF 2.897. The lowest total risk was for azoxystrobin when applied at  0.0650 kg a.i. ha-1 (EF 0.625.

Comparative hygienic assessment of active ingredients content in the air environment after treatment of cereal spiked crops by combined fungicides.

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Kondratiuk, Mykola; Blagaia, Anna; Pelo, Ihor

2018-01-01

Introduction: The quality of the air environment significantly affects the health of the population. Chemical plant protection products in the spring and summer time may be the main pollutants of the air environment in rural areas. Chemical plant protection products are dangerous substances of anthropogenic origin. If applying pesticides in high concentrations, the risk of poisoning by active ingredients of pesticide preparations in workers directly contacting with it increases. The aim: Comparative hygienic assessment of active ingredients content in the air environment after treatment of cereal spiked crops by combined fungicides was the aim of the work. Materials and methods: Active ingredients of the studied combined fungicides, samples of air, and swabs from workers' skin and stripes from overalls were materials of the research. Methods of full-scale in-field hygienic experiment, gas-liquid chromatography, high-performance liquid chromatography, as well as statistical and bibliographic methods were used in the research. Results and conclusions: Active ingredients of the studied combined fungicides were not detected in the working zone air and atmospheric air at the levels exceeding the limits of its detection by appropriate chromatography methods. Findings confirmed the air environment safety for agricultural workers and rural population if studied combined fungicides are applied following the hygienically approved suggested application rates and in accordance of good agricultural practice rules. However the possible complex risk for workers after certain studied fungicides application may be higher than acceptable due to the elevated values for dermal effects. The complex risk was higher than acceptable in еру case of aerial spraying of both studied fungicides, meanwhile only one combination of active ingredients revealed possible risk for workers applying fungicides by rod method of cereal spiked crops treatment.

Reaction Intermediate Analogues as Bisubstrate Inhibitors of Pantothenate Synthetase

OpenAIRE

Xu, Zhixiang; Yin, Wei; Martinelli, Leonardo K.; Evans, Joanna; Chen, Jinglei; Yu, Yang; Wilson, Daniel J.; Mizrahi, Valerie; Qiao, Chunhua; Aldrich, Courtney C.

2014-01-01

The biosynthesis of pantothenate, the core of coenzyme A (CoA), has been considered an attractive target for the development of antimicrobial agents since this pathway is essential in prokaryotes, but absent in mammals. Pantothenate synthetase, encoded by the gene panC, catalyzes the final condensation of pantoic acid with β–alanine to afford pantothenate via an intermediate pantoyl adenylate. We describe the synthesis and biochemical characterization of five PanC inhibitors that mimic the in...

Computational discovery of picomolar Q(o) site inhibitors of cytochrome bc1 complex.

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Hao, Ge-Fei; Wang, Fu; Li, Hui; Zhu, Xiao-Lei; Yang, Wen-Chao; Huang, Li-Shar; Wu, Jia-Wei; Berry, Edward A; Yang, Guang-Fu

2012-07-11

A critical challenge to the fragment-based drug discovery (FBDD) is its low-throughput nature due to the necessity of biophysical method-based fragment screening. Herein, a method of pharmacophore-linked fragment virtual screening (PFVS) was successfully developed. Its application yielded the first picomolar-range Q(o) site inhibitors of the cytochrome bc(1) complex, an important membrane protein for drug and fungicide discovery. Compared with the original hit compound 4 (K(i) = 881.80 nM, porcine bc(1)), the most potent compound 4f displayed 20 507-fold improved binding affinity (K(i) = 43.00 pM). Compound 4f was proved to be a noncompetitive inhibitor with respect to the substrate cytochrome c, but a competitive inhibitor with respect to the substrate ubiquinol. Additionally, we determined the crystal structure of compound 4e (K(i) = 83.00 pM) bound to the chicken bc(1) at 2.70 Å resolution, providing a molecular basis for understanding its ultrapotency. To our knowledge, this study is the first application of the FBDD method in the discovery of picomolar inhibitors of a membrane protein. This work demonstrates that the novel PFVS approach is a high-throughput drug discovery method, independent of biophysical screening techniques.

Fungicide sensitivity of Trichoderma spp. from Agaricus bisporus farms in Serbia.

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Kosanović, Dejana; Potočnik, Ivana; Vukojević, Jelena; Stajić, Mirjana; Rekanović, Emil; Stepanović, Miloš; Todorović, Biljana

2015-01-01

Trichoderma species, the causal agents of green mould disease, induce great losses in Agaricus bisporus farms. Fungicides are widely used to control mushroom diseases although green mould control is encumbered with difficulties. The aims of this study were, therefore, to research in vitro toxicity of several commercial fungicides to Trichoderma isolates originating from Serbian and Bosnia-Herzegovina farms, and to evaluate the effects of pH and light on their growth. The majority of isolates demonstrated optimal growth at pH 5.0, and the rest at pH 6.0. A few isolates also grew well at pH 7. The weakest mycelial growth was noted at pH 8.0-9.0. Generally, light had an inhibitory effect on the growth of tested isolates. The isolates showed the highest susceptibility to chlorothalonil and carbendazim (ED50 less than 1 mg L(-1)), and were less sensitive to iprodione (ED50 ranged 0.84-6.72 mg L(-1)), weakly resistant to thiophanate-methyl (ED50 = 3.75-24.13 mg L(-1)), and resistant to trifloxystrobin (ED50 = 10.25-178.23 mg L(-1)). Considering the toxicity of fungicides to A. bisporus, carbendazim showed the best selective toxicity (0.02), iprodione and chlorothalonil moderate (0.16), and thiophanate-methyl the lowest (1.24), while trifloxystrobin toxicity to A. bisporus was not tested because of its inefficiency against Trichoderma isolates.

Serine biosynthesis and transport defects.

Science.gov (United States)

El-Hattab, Ayman W

2016-07-01

l-serine is a non-essential amino acid that is biosynthesized via the enzymes phosphoglycerate dehydrogenase (PGDH), phosphoserine aminotransferase (PSAT), and phosphoserine phosphatase (PSP). Besides its role in protein synthesis, l-serine is a potent neurotrophic factor and a precursor of a number of essential compounds including phosphatidylserine, sphingomyelin, glycine, and d-serine. Serine biosynthesis defects result from impairments of PGDH, PSAT, or PSP leading to systemic serine deficiency. Serine biosynthesis defects present in a broad phenotypic spectrum that includes, at the severe end, Neu-Laxova syndrome, a lethal multiple congenital anomaly disease, intermediately, infantile serine biosynthesis defects with severe neurological manifestations and growth deficiency, and at the mild end, the childhood disease with intellectual disability. A serine transport defect resulting from deficiency of the ASCT1, the main transporter for serine in the central nervous system, has been recently described in children with neurological manifestations that overlap with those observed in serine biosynthesis defects. l-serine therapy may be beneficial in preventing or ameliorating symptoms in serine biosynthesis and transport defects, if started before neurological damage occurs. Herein, we review serine metabolism and transport, the clinical, biochemical, and molecular aspects of serine biosynthesis and transport defects, the mechanisms of these diseases, and the potential role of serine therapy. Copyright © 2016 Elsevier Inc. All rights reserved.

Sensitivity of Septoria pyricola isolates to carbendazim, DMI and QoI based fungicides and to boscalid, in Greece

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Athanassios Christos PAPPAS

2010-09-01

Full Text Available The sensitivity of 36 Septoria pyricola single spore isolates, obtained from isolated pear orchards, to carbendazim, bitertanol, flusilazole, myclobutanil, azoxystrobin, kresoxim-methyl, pyraclostrobin, trifloxystrobin and boscalid, was studied in vitro. Spore suspensions were point-inoculated on media amended with various concentrations of fungicides and the minimum inhibitory concentration (MICs of the fungicides was determined. Most isolates were highly resistant to carbendazim, forming colonies even at concentrations of 100 mg L-1 of the fungicide. A few isolates failed to form colonies with carbendazim concentrations of 0.1 and 10 mg L-1; these isolates were designated carbendazim-sensitive and moderately carbendazim-resistant respectively.The MIC of DMI fungicides was up to 1 mg L-1 with some isolates, and the mean MICs of bitertanol, flusilazole and myclobutanil were 0.133±0.036, 0.075±0.044 and 0.230±0.038 mg L-1 respectively. The MIC of the QoI fungicides was up to 0.1 mg L-1 with most isolates, but some isolates were 100-fold less sensitive to azoxystrobin. The mean MICs of azoxystrobin, kresoxim-methyl, pyraclostrobin and trifloxystrobin were 0.177±0.040, 0.075±0.035, 0.067±0.063, and 0.073±0.065 mg L-1 respectively. Overall, the MIC of boscalid was 1 mg L-1, and the mean MIC was 0.111±0.044 mg L-1. The ED50 values of representative isolates are also presented, as determined by colony formation with dispersed spore inoculation on a medium amended with fungicides. The results show that the benzimidazoles are ineffective against S. pyricola isolates in Greece and suggest that the future effectiveness of the DMIs is at risk.

Induction of dopamine biosynthesis by l-DOPA in PC12 cells: implications of L-DOPA influx and cyclic AMP.

Science.gov (United States)

Jin, Chun Mei; Yang, Yoo Jung; Huang, Hai Shan; Lim, Sung Cil; Kai, Masaaki; Lee, Myung Koo

2008-09-04

The effects of 3,4-dihydroxyphenylalanine (l-DOPA) on dopamine biosynthesis and cytotoxicity were investigated in PC12 cells. l-DOPA treatment (20-200 microM) increased the levels of dopamine by 226%-504% after 3-6 h of treatment and enhanced the activities of tyrosine hydroxylase (TH) and aromatic l-amino acid decarboxylase (AADC). l-DOPA (20-200 muM) treatment led to a 562%-937% increase in l-DOPA influx at 1 h, which inhibited the activity of TH, but not AADC, during the same period. The extracellular releases of dopamine were also increased by 231%-570% after treatment with 20 and 200 microM l-DOPA for 0.5-3 h. l-DOPA at a concentration of 100-200 microM, but not 20 microM, exerted apoptotic cytotoxicity towards PC12 cells for 24-48 h. l-DOPA (20-200 microM) increased the intracellular cyclic AMP levels by 318%-557% after 0.5-1 h in a concentration-dependent manner. However, the elevated cyclic AMP levels by l-DOPA could not protect against l-DOPA (100-200 microM)-induced cytotoxicity after 24-48 h. In addition, l-DOPA (20-200 microM)-induced increases in cyclic AMP and dopamine were significantly reduced by treatment with SCH23390 (dopamine D(1) receptor antagonist). The increased levels of dopamine by l-DOPA were also reduced by H89 (protein kinase A, PKA, inhibitor) and GF109203X (protein kinase C inhibitor); however, the reduction by GF109203X was not significant. l-DOPA at 20-200 microM stimulated the phosphorylation of PKA and cyclic AMP-response element binding protein and induced the biosynthesis of the TH protein. These results indicate that 20-200 microM l-DOPA induces dopamine biosynthesis by two pathways. One pathway involves l-DOPA directly entering the cells to convert dopamine through AADC activity (l-DOPA decarboxylation). The other pathway involves l-DOPA and/or released dopamine activating TH to enhance dopamine biosynthesis by the dopamine D(1) receptor-cyclic AMP-PKA signaling system (dopamine biosynthesis by TH).

SEARCH OF NEW SYNTHETIC INHIBITORS OF TYROSINASE

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Yu. Shesterenko

2017-11-01

Full Text Available Melanin pigmentation of skin plays the most important role in the protection of organism against UV-irradiation, but the excessive accumulation of melanin brings to toxic melanodermia, melasma, lentigo and other skin lesions. Tyrosinase is the key enzyme of skin melanin pigment biosynthesis. In spite of certain progress in investigation of natural and synthetic tyrosinase inhibitors, actuality of such studies is of a high level, because the existing inhibitors are in some cases unstable, expensive, toxic, requires complex methods of synthesis or isolation from natural sources. The aim of the work is screening of new tyrosinase inhibitors, using the enzyme, isolated from Agaricus bisporus. Tyrosinase was isolated from Agaricus bisporus mushrooms by a modified method. It was found, that the introduction of polyethylene glycol 4000 in the extraction process promotes 3-fold reduction of polyphenol content, which leads to increase purity of enzyme with an increase in its activity by 25%. A search for new tyrosinase inhibitors among a wide range of compounds, including derivatives of 3-chloro-1,4-naphthoquinone, isatin, 3-hydroxy-2-naphthoic acid, etc was conducted. The studied substances did not displayed inhibitory effect at concentration of 0,1-0,5 mmol/dm3.

In-vitro evaluation of fungicides, plant extracts and bio-control agents against rice blast pathogen magnaporthe oryzae couch

International Nuclear Information System (INIS)

Hajano, J.U.D.; Lodhi, M.; Pathan, M.A.; Khanzada, A.; Shah, G.S.

2012-01-01

Among 5 fungicides viz., Thiophanate-methyl, Carbendazim, Fosetyl-aluminium, Mancozeb and Copper oxychloride, used against the Magnaporthe oryzae, only Mancozeb appeared as the highly effective fungicide that completely inhibited the mycelial growth of the fungus. All other fungicides showed little effect at higher concentrations. The extracts of garlic (Allium sativum L.), neem (Azadirachta indica L.) and calatropis (Calotropis procera L.) when used against M. oryzae by food poisoning method, only higher dose of garlic completely inhibited the mycelial growth of the test fungus. Six bio-control agents viz., Trichoderma harzianum, Trichoderma polysporum, Trichoderma pseudokoningii, Gliocladium virens, Paecilomyces variotii and Paecilomyces lilacinus were used. Maximum mycelial inhibition of M. oryzae was provided by P. lilacinus followed by Trichoderma spp. (author)

Synergistic effect of the combined bio-fungicides ε-poly-l-lysine and chitooligosaccharide in controlling grey mould (Botrytis cinerea) in tomatoes.

Science.gov (United States)

Sun, Guangzheng; Yang, Qichao; Zhang, Ancheng; Guo, Jia; Liu, Xinjie; Wang, Yang; Ma, Qing

2018-07-02

The antifungal properties and the induction of resistance by ε-poly-l-lysine (ε-PL) and chitooligosaccharide (COS) were examined to find an alternative to synthetic fungicides currently used in the control of the devastating fungal pathogen Botrytis cinerea, the causal agent of grey mould disease of tomatoes. As presented herein, this combined treatment (200 mg/L ε-PL + 400 mg/L COS) was found to have optimal in vitro antifungal activities, achieving an inhibition rate of 90.22%. In vivo assays with these combined bio-fungicides, under greenhouse conditions using susceptible tomato plants, demonstrated good protection against severe grey mould. In field tests, the combined bio-fungicides had a control effect of up to 66.67% against tomato grey mould. To elucidate the mechanisms of the combined bio-fungicide-induced resistance in the tomato, plants were subjected to three treatments: 1) inoculation with B. cinerea after spraying with 200 mg/L ε-PL alone, 2) inoculation with the combined bio-fungicides, and 3) inoculation with 400 mg/L COS alone. Compared to the control (sterile water), increases in salicylic acid (SA) and jasmonic acid (JA) levels and increased phenylalanine ammonia lyase (PAL), peroxidase (POD), and superoxide dismutase (SOD) activities were observed. Catalase (CAT) activity and abscisic acid (ABA) and gibberellin (GA) levels decreased, particularly in the combined bio-fungicide-treated plants. Altogether, these findings reveal that the combined bio-fungicides (200 mg/L ε-PL + 400 mg/L COS) should be an excellent biocontrol agent candidate that combines direct antifungal activity against B. cinerea with plant resistance. Copyright © 2018. Published by Elsevier B.V.

DIFFERENTIATING TOXICITIES OF CONAZOLE FUNGICIDES THROUGH METABONOMIC ANALYSES OF MULTIPLE TISSUES

Science.gov (United States)

The conazole fungicides represent a large group of compounds widely used agriculturally for the protection of crop plants (Hutson 1998) and pharmaceutically in the treatment of topical and systemic infections(Sheehan 1999). In 1999, the latest period for which agricultural usage...

Fatty acid biosynthesis is involved in the production of hepatitis B virus particles

International Nuclear Information System (INIS)

Okamura, Hitomi; Nio, Yasunori; Akahori, Yuichi; Kim, Sulyi; Watashi, Koichi; Wakita, Takaji; Hijikata, Makoto

2016-01-01

Hepatitis B virus (HBV) proliferates in hepatocytes after infection, but the host factors that contribute to the HBV lifecycle are poorly understood at the molecular level. We investigated whether fatty acid biosynthesis (FABS), which was recently reported to contribute to the genomic replication of hepatitis C virus, plays a role in HBV proliferation. We examined the effects of inhibitors of the enzymes in the FABS pathway on the HBV lifecycle by using recombinant HBV-producing cultured cells and found that the extracellular HBV DNA level, reflecting HBV particle production, was decreased by treatment with inhibitors suppressed the synthesis of long-chain saturated fatty acids with little cytotoxicity. The reduced HBV DNA level was reversed when palmitic acid, which is the product of fatty acid synthase (FAS) during FABS, was used simultaneously with the inhibitor. We also observed that the amount of intracellular HBV DNA in the cells was increased by FAS inhibitor treatment, suggesting that FABS is associated with HBV particle production but not its genome replication. This suggests that FABS might be a potent target for anti-HBV drug with a mode of action different from current HBV therapy. -- Highlights: •Inhibitors of ACC1 and FAS but not SCD1 decreased production of extracellular HBV DNA. •Products of FABS, long chain fatty acids, increased production of extracellular HBV DNA. •FAS inhibitor increased intracellular levels of HBV DNA and HBcAg. •FABS was suggested to contribute to HBV particle production without significant relation with secretory pathway of the cells.

Fatty acid biosynthesis is involved in the production of hepatitis B virus particles

Energy Technology Data Exchange (ETDEWEB)

Okamura, Hitomi [Laboratory of Human Tumor Viruses, Institute for Virus Research, Kyoto University, 53 Kawaharacho, Shogoin, Sakyoku, Kyoto 606-8507 (Japan); Graduate School of Biostudies, Kyoto University, Yoshida-Konoecho, Sakyoku, Kyoto 606-8501 (Japan); Nio, Yasunori, E-mail: yasunori.nio@takeda.com [Takeda Pharmaceutical Company Limited, Pharmaceutical Research Division, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555 (Japan); Akahori, Yuichi [Laboratory of Human Tumor Viruses, Institute for Virus Research, Kyoto University, 53 Kawaharacho, Shogoin, Sakyoku, Kyoto 606-8507 (Japan); Graduate School of Biostudies, Kyoto University, Yoshida-Konoecho, Sakyoku, Kyoto 606-8501 (Japan); Kim, Sulyi [Laboratory of Human Tumor Viruses, Institute for Virus Research, Kyoto University, 53 Kawaharacho, Shogoin, Sakyoku, Kyoto 606-8507 (Japan); Watashi, Koichi [Department of Virology II, National Institute of Infectious Diseases, Tokyo 162-8640 (Japan); Department of Applied Biological Science, Tokyo University of Sciences, Noda 278-8510 (Japan); CREST, Japan Science and Technology Agency (JST), Saitama 332-0012 (Japan); Wakita, Takaji [Department of Virology II, National Institute of Infectious Diseases, Tokyo 162-8640 (Japan); Hijikata, Makoto, E-mail: mhijikat@virus.kyoto-u.ac.jp [Laboratory of Human Tumor Viruses, Institute for Virus Research, Kyoto University, 53 Kawaharacho, Shogoin, Sakyoku, Kyoto 606-8507 (Japan); Graduate School of Biostudies, Kyoto University, Yoshida-Konoecho, Sakyoku, Kyoto 606-8501 (Japan)

2016-06-17

Hepatitis B virus (HBV) proliferates in hepatocytes after infection, but the host factors that contribute to the HBV lifecycle are poorly understood at the molecular level. We investigated whether fatty acid biosynthesis (FABS), which was recently reported to contribute to the genomic replication of hepatitis C virus, plays a role in HBV proliferation. We examined the effects of inhibitors of the enzymes in the FABS pathway on the HBV lifecycle by using recombinant HBV-producing cultured cells and found that the extracellular HBV DNA level, reflecting HBV particle production, was decreased by treatment with inhibitors suppressed the synthesis of long-chain saturated fatty acids with little cytotoxicity. The reduced HBV DNA level was reversed when palmitic acid, which is the product of fatty acid synthase (FAS) during FABS, was used simultaneously with the inhibitor. We also observed that the amount of intracellular HBV DNA in the cells was increased by FAS inhibitor treatment, suggesting that FABS is associated with HBV particle production but not its genome replication. This suggests that FABS might be a potent target for anti-HBV drug with a mode of action different from current HBV therapy. -- Highlights: •Inhibitors of ACC1 and FAS but not SCD1 decreased production of extracellular HBV DNA. •Products of FABS, long chain fatty acids, increased production of extracellular HBV DNA. •FAS inhibitor increased intracellular levels of HBV DNA and HBcAg. •FABS was suggested to contribute to HBV particle production without significant relation with secretory pathway of the cells.

Regulation of cell wall biosynthesis.

Science.gov (United States)

Zhong, Ruiqin; Ye, Zheng-Hua

2007-12-01

Plant cell walls differ in their amount and composition among various cell types and even in different microdomains of the wall of a given cell. Plants must have evolved regulatory mechanisms controlling biosynthesis, targeted secretion, and assembly of wall components to achieve the heterogeneity in cell walls. A number of factors, including hormones, the cytoskeleton, glycosylphosphatidylinositol-anchored proteins, phosphoinositides, and sugar nucleotide supply, have been implicated in the regulation of cell wall biosynthesis or deposition. In the past two years, there have been important discoveries in transcriptional regulation of secondary wall biosynthesis. Several transcription factors in the NAC and MYB families have been shown to be the key switches for activation of secondary wall biosynthesis. These studies suggest a transcriptional network comprised of a hierarchy of transcription factors is involved in regulating secondary wall biosynthesis. Further investigation and integration of the regulatory players participating in the making of cell walls will certainly lead to our understanding of how wall amounts and composition are controlled in a given cell type. This may eventually allow custom design of plant cell walls on the basis of our needs.

Phytopharmacology of the rice diseases. I. In vitro tests on application of the dust fungicides to the important pathogenic fungi

Energy Technology Data Exchange (ETDEWEB)

Hashioka, Y; Saito, T

1953-01-01

In this paper, the results of experiments on the repressing effect of selected fungicides on the growth of pathogenic fungi of rice are reported. Organic mercury compounds were tested and found to be more effective fungicides than copper. Their use in agriculture is recommended.

Discovery of inhibitors of Leishmania β-1,2-mannosyltransferases using a click-chemistry-derived guanosine monophosphate library.

Directory of Open Access Journals (Sweden)

Phillip van der Peet

Full Text Available Leishmania spp. are a medically important group of protozoan parasites that synthesize a novel intracellular carbohydrate reserve polymer termed mannogen. Mannogen is a soluble homopolymer of β-1,2-linked mannose residues that accumulates in the major pathogenic stages in the sandfly vector and mammalian host. While several steps in mannogen biosynthesis have been defined, none of the enzymes have been isolated or characterized. We report the development of a simple assay for the GDP-mannose-dependent β-1,2-mannosyltransferases involved in mannogen synthesis. This assay utilizes octyl α-D-mannopyranoside to prime the formation of short mannogen oligomers up to 5 mannose residues. This assay was used to screen a focussed library of 44 GMP-triazole adducts for inhibitors. Several compounds provided effective inhibition of mannogen β-1,2-mannosyltransferases in a cell-free membrane preparation. This assay and inhibitor compounds will be useful for dissecting the role of different mannosyltransferases in regulating de novo biosynthesis and elongation reactions in mannogen metabolism.

The Antibiotic CJ-15,801 is an Antimetabolite which Hijacks and then Inhibits CoA Biosynthesis

Science.gov (United States)

van der Westhuyzen, Renier; Hammons, Justin C.; Meier, Jordan L.; Dahesh, Samira; Moolman, Wessel J. A.; Pelly, Stephen C.; Nizet, Victor; Burkart, Michael D.; Strauss, Erick

2012-01-01

SUMMARY The natural product CJ-15,801 is an inhibitor of Staphylococcus aureus, but not other bacteria. Its close structural resemblance to pantothenic acid, the vitamin precursor of coenzyme A (CoA), and its Michael acceptor moiety suggest that it irreversibly inhibits an enzyme involved in CoA biosynthesis or utilization. However, its mode of action and the basis for its specificity have not been elucidated to date. We demonstrate that CJ-15,801 is transformed by the uniquely selective S. aureus pantothenate kinase, the first CoA biosynthetic enzyme, into a substrate for the next enzyme, phosphopantothenoylcysteine synthetase, which is inhibited through formation of a tight-binding structural mimic of its native reaction intermediate. These findings reveal CJ-15,801 as a vitamin biosynthetic pathway antimetabolite with a mechanism similar to that of the sulfonamide antibiotics, and highlight CoA biosynthesis as a viable antimicrobial drug target. PMID:22633408

The fungicidal properties of the carbon materials obtained from chitin and chitosan promoted by copper salts

Energy Technology Data Exchange (ETDEWEB)

Ilnicka, Anna, E-mail: annakucinska@o2.pl; Walczyk, Mariusz; Lukaszewicz, Jerzy P.

2015-07-01

Renewable raw materials chitin and chitosan (N-deacetylated derivative of chitin) were subjected to action of different copper modifiers that were carbonized in the atmosphere of the N{sub 2} inert gas. As a result of the novel manufacturing procedure, a series of carbon materials was obtained with developed surface area and containing copper derivatives of differentiated form, size, and dispersion. The copper modifier and manufacturing procedure (concentration, carbonization temperature) influence the physical–chemical and fungicide properties of the carbons. The received carbons were chemically characterized using several methods like low-temperature adsorption of nitrogen, X-ray diffraction analysis, scanning electron microscopy, cyclic voltammetry, elemental analysis, and bioassay. Besides chemical testing, some biological tests were performed and let to select carbons with the highest fungicidal activity. Such carbons were characteristic of the specific form of copper derivatives occurring in them, i.e., nanocrystallites of Cu{sup 0} and/or Cu{sub 2}O of high dispersion on the surface of carbon. The carbons may find an application as effective contact fungistatic agents in cosmetology, medicine, food industry, etc. - Highlights: • The novel manufacturing procedure yields new functional carbon materials. • Two biopolymers chitin and chitosan can undergo copper(II) ion modification. • The Cu-modified carbon materials exhibit high fungicidal activity. • The fungicidal activity results from the presence of Cu{sup 0} and Cu{sub 2}O nano-crystallites.

Ranking of fungicides according to risk assessments for health and environment

DEFF Research Database (Denmark)

Jørgensen, Lise Nistrup; Ørum, Jens Erik

2014-01-01

PL varies for fungicide standard rates by a factor of 10. Products including epoxiconazole generally have higher PL's due to the human health profile of this active. PL's per area, crop or product will supplement the previous pesticide statistics based on treatment frequency index (TFI). PL has also......Denmark has introduced a new indicator for ranking the potential impact of pesticides on health and environment. The new Pesticide Load (PL) makes it possible for farmers to choose the least harmful fungicides and substitute between products which have an equally good efficacy profile. In practice...... been introduced as the basis for a new tax system for pesticides from 1 July 2013, replacing the old value based tax. The Government has asked for a 40% reduction in the PL per ha by 2015, based on substitutions to less harmfull products. As certain pesticide groups will be favoured by the new tax...

Foliar Application of the Fungicide Pyraclostrobin Reduced Bacterial Spot Disease of Pepper

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Beom Ryong Kang

2018-03-01

Full Text Available Pyraclostrobin is a broad-spectrum fungicide that inhibits mitochondrial respiration. However, it may also induce systemic resistance effective against bacterial and viral diseases. In this study, we evaluated whether pyraclostrobin enhanced resistance against the bacterial spot pathogen, Xanthomonas euvesicatora on pepper (Capsicum annuum. Although pyraclostrobin alone did not suppressed the in vitro growth of X. euvesicatoria, disease severity in pepper was significantly lower by 69% after treatments with pyraclostrobin alone. A combination of pyraclostrobin with streptomycin reduced disease by over 90% that of the control plants. The preventive control of the pyraclostrobin against bacterial spot was required application 1-3 days before pathogen inoculation. Our findings suggest that the fungicide pyraclostrobin can be used with a chemical pesticide to control bacterial leaf spot diseases in pepper.

In vitro and in vivo screening of azole fungicides for antiandrogenic effects

DEFF Research Database (Denmark)

Taxvig, Camilla; Vinggaard, Anne; Hass, Ulla

signs of feminization of the male offspring were investigated. Tebuconazole caused an increase in testicular 17alfa-hydroxyprogesterone and progesterone levels, and a decrease in testosterone levels in male fetuses. Epoxiconazole had no effect on any of the mesured hormonelevels. Furthermore...... and antiandrogenic effects both in vitro and in vivo. Two other azole fungicides, tebuconazole and epoxiconazole, have now been investigated for antiandrogenic effects in vitro and in vivo as well. The fungicides were screened in two well-established cell assays, including testing for agonistic and antagonistic...... effects on AR in transfected CHO cells, using an AR reporter gene assay. The compounds were also analyzed for effects on steroidogenesis in H295R cells, a human adrenocorticocarcinoma cell line, used to detect effects on steroid production. In vitro tebuconazole and epoxiconazole proved to be antagonists...

Inhibitory effects of azole-type fungicides on interleukin-17 gene expression via retinoic acid receptor-related orphan receptors α and γ

Science.gov (United States)

Kojima, Hiroyuki; Muromoto, Ryuta; Takahashi, Miki; Takeuchi, Shinji; Takeda, Yukimasa; Jetten, Anton M.; Matsuda, Tadashi

2013-01-01

The retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ), are key regulators of helper T (Th)17 cell differentiation, which is involved in the innate immune system and autoimmune disorders. However, it remains unclear whether environmental chemicals, including pesticides, have agonistic and/or antagonistic activity against RORα/γ. In this study, we investigated the RORα/γ activity of several azole-type fungicides, and the effects of these fungicides on the gene expression of interleukin (IL)-17, which mediates the function of Th17 cells. In the ROR-reporter gene assays, five azole-type fungicides (imibenconazole, triflumizole, hexaconazole, tetraconazole and imazalil) suppressed RORα- and/or RORγ-mediated transcriptional activity as did benzenesulphonamide T0901317, a ROR inverse agonist and a liver X receptor (LXR) agonist. In particular, imibenconazole, triflumizole and hexaconazole showed RORγ inverse agonistic activity at concentrations of 10−6 M. However, unlike T0901317, these fungicides failed to show any LXRα/β agonistic activity. Next, five azole-type fungicides, showing ROR inverse agonist activity, were tested on IL-17 mRNA expression in mouse T lymphoma EL4 cells treated with phorbol myristate acetate and ionomycin. The quantitative RT-PCR analysis revealed that these fungicides suppressed the expression of IL-17 mRNA without effecting RORα and RORγ mRNA levels. In addition, the inhibitory effect of imibenconazole as well as that of T0901317 was absorbed in RORα/γ-knocked down EL4 cells. Taken together, these results suggest that some azole-type fungicides inhibit IL-17 production via RORα/γ. This also provides the first evidence that environmental chemicals can act as modulators of IL-17 expression in immune cells. PMID:22289359

Biosynthesis of tylophora alkaloids

International Nuclear Information System (INIS)

Mulchandani, N.B.; Iyer, S.S.; Badheka, L.P.

1974-01-01

Using labelled precursors, biosynthesis of the tylophora alkaloids, tylophorine, tylophorinidine and tylophorinide has been investigated in Tylophora asthmatica plants. The radioactive precursors, phenylalanine-2- 14 C, benzoic acid-1- 14 C, benzoic acid-ring 14 C, acetate-2- 14 C, ornithine-5- 14 C, acetate-2- 14 C, ornithine-5- 14 C and cinnamic acid-2- 14 C were administered to the plants individually by wick technique. Tylophorine was isolated in each case and assayed for its radioactivity to find out the incorporation of the label into it. The results indicate that: (1) phenylalanine via cinnamic acid is an important precursor in the biosynthesis of tylophorine (2) orinithine participates in tylophorine biosynthesis via pyrroline and (3) tylophorinidine may be a direct precursor of tylophorine. (M.G.B.)

Selective effects of two systemic fungicides on soil fungi.

Science.gov (United States)

Abdel-Fattah, H M; Abdel-Kader, M I; Hamida, S

1982-08-20

BAS 317 00F was not toxic to the total count of fungi after 2 days but was regularly significantly toxic at the three doses after 5, 20 and 40 days and toxic at the low and the high doses after 80 days. In the agar medium, it was toxic to the counts of total fungi. Aspergillus, A. terreus, Rhizopus oryzae and Mucor racemosus at the high dose. Only the mycelial growth of Trichoderma viride which was significantly inhibited by the three doses when this fungicide was added to the liquid medium. Polyram-Combi induced two effects on the total population of soil fungi. One inhibitory and this was demonstrated almost regularly after 2, 10 and 40 days and the other stimulatory after 80 days of treatment with the low and the high doses. In the agar medium, this fungicide was very toxic to total fungi and to almost all fungal genera and species at the three doses. Several fungi could survive the high dose. In liquid medium, the test fungi showed variable degree of sensitivity and the most sensitive was Gliocladium roseum which was completely eradicated by the three doses.

Synthesis, Fungicidal Activity and Mode of Action of 4-Phenyl-6-trifluoromethyl-2-aminopyrimidines against Botrytis cinerea

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Chunhui Liu

2016-06-01

Full Text Available Anilinopyrimidines are the main chemical agents for management of Botrytis cinerea. However, the drug resistance in fungi against this kind of compounds is very serious. To explore new potential fungicides against B. cinerea, a series of 4-phenyl-6-trifluoromethyl-2-amino-pyrimidine compounds (compounds III-1 to III-22 were synthesized, and their structures were confirmed by 1H-NMR, IR and MS. Most of these compounds possessed excellent fungicidal activity. The compounds III-3 and III-13 showed higher fungicidal activity than the positive control pyrimethanil on fructose gelatin agar (FGA, and compound III-3 on potato dextrose agar (PDA indicated high activity compared to the positive control cyprodinil. In vivo greenhouse results indicated that the activity of compounds III-3, III-8, and III-11 was significantly higher than that of the fungicide pyrimethanil. Scanning electron micrography (SEM and transmission electron micrography (TEM were applied to illustrate the mechanism of title compounds against B. cinerea. The title compounds, especially those containing a fluorine atom at the ortho-position on the benzene ring, could maintain the antifungal activity against B. cinerea, but their mechanism of action is different from that of cyprodinil. The present study lays a good foundation for us to find more efficient reagents against B. cinerea.

Fungicides transport in runoff from vineyard plot and catchment: contribution of non-target areas.

Science.gov (United States)

Lefrancq, Marie; Payraudeau, Sylvain; García Verdú, Antonio Joaquín; Maillard, Elodie; Millet, Maurice; Imfeld, Gwenaël

2014-04-01

Surface runoff and erosion during the course of rainfall events are major processes of pesticides transport from agricultural land to aquatic ecosystem. These processes are generally evaluated either at the plot or the catchment scale. Here, we compared at both scales the transport and partitioning in runoff water of two widely used fungicides, i.e., kresoxim-methyl (KM) and cyazofamid (CY). The objective was to evaluate the relationship between fungicides runoff from the plot and from the vineyard catchment. The results show that seasonal exports for KM and CY at the catchment were larger than those obtained at the plot. This underlines that non-target areas within the catchment largely contribute to the overall load of runoff-associated fungicides. Estimations show that 85 and 62 % of the loads observed for KM and CY at the catchment outlet cannot be explained by the vineyard plots. However, the partitioning of KM and CY between three fractions, i.e., the suspended solids (>0.7 μm) and two dissolved fractions (i.e., between 0.22 and 0.7 µm and plot scales enable to evaluate the sources areas of pesticide off-site transport.

Effect of foliar fertilizer and fungicidal protection against leaf spot diseases on winter wheat

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Agnieszka Mączyńska

2012-12-01

Full Text Available Field experiments were carried out in the seasons 2000/2001 and 2001/2002 in Plant Protection Institute, Sooenicowice Branch to assess the influence of foliar fertilizers such as Ekolist PK 1, Ekolist Mg, Mikrosol Z and Urea on healthiness of winter wheat. Foliar fertilizers were mixed with fungicides. The fungicides were applied at full or half recommended doses. The effect of the disease on wheat leaves was evaluated three times in each vegetation season. Remaining green leaf area (GLA of leaves was also determined. GLA of the leaves F-1 was not significantly different for each combination with different fertilization and different levels of chemical treatment. The application of foliar fertilizer only had no effect on green leaf area (GLA. The results indicate that foliar fertilization of all experimental plots improved leaf condition and therefore halted the development of wheat leaf diseases. The increases of 1000 grain mass and yield was high for each plot where a fertilizer and a full or half dose of a fungicide was applied. Foliar fertilizing with no chemical control had no proven effect on studied parameters.

A long term field study of the effect of fungicides penconazole and sulfur on yeasts in the vineyard.

Science.gov (United States)

Cordero-Bueso, Gustavo; Arroyo, Teresa; Valero, Eva

2014-10-17

This research deals with how two fungicide treatments against powdery mildew, penconazole as a systematic fungicide and sulfur as an inorganic broad-spectrum fungicide, affect the diversity and density of wine yeasts associated with grape berry surfaces and subsequent spontaneous fermentations. Unlike other studies in this area, this work aims to evaluate this effect on the population dynamics in the environment, the conditions of which are not reproducible in the laboratory. A long term (three year) sampling plan was thus devised. A minimum inhibitory concentration assay was also carried out in the laboratory in order to prove the influence of these antifungals on yeast populations. While both antifungal treatments (penconazole and sulfur) were similarly effective against powdery mildew, each had a very different effect on yeast populations. Penconazole showed the most negative effect on biodiversity in the vineyard and was the fungicide to which the isolated yeasts showed the greatest sensitivity. This study therefore evidences the suitability of treatment with sulfur, in both conventional and organic viticulture, to preserve the yeast population associated with grape berries, in particular the Saccharomyces cerevisiae species. Copyright © 2014 Elsevier B.V. All rights reserved.

Occurrence of fungicides and other pesticides in surface water, groundwater, and sediment from three targeted-use areas in the United States, 2009

Science.gov (United States)

Orlando, James L.; Smalling, Kelly L.; Reilly, Timothy J.; Boehlke, Adam; Meyer, Michael T.; Kuivila, Kathryn

2013-01-01

Surface-water, groundwater, and suspended- and bedsediment samples were collected in three targeted-use areas in the United States where potatoes were grown during 2009 and analyzed for an extensive suite of fungicides and other pesticides by gas chromatograph/mass spectrometry and liquid chromatography with tandem mass spectrometry. Fungicides were detected in all environmental matrices sampled during the study. The most frequently detected fungicides were azoxystrobin, boscalid, chlorothalonil, and pyraclostrobin. Other pesticides that were detected frequently included amino phosphonic acid (AMPA), atrazine, metolaclor, and the organochlorine insecticide p,p’-DDT and its degradates p,p’-DDD and p,p’-DDE. A greater number of pesticides were detected in surface water relative to the other environmental matrices sampled, and at least one pesticide was detected in 62 of the 63 surfacewater samples. The greatest numbers of pesticides and the maximum observed concentrations for most pesticides were measured in surface-water samples from Idaho. In eight surface- water samples (six from Idaho and two from Wisconsin), concentrations of bifenthrin, metolachlor, or malathion exceeded U.S. Environmental Protection Agency freshwater aquatic-life benchmarks for chronic toxicity to invertebrates. Thirteen pesticides, including seven fungicides, were detected in groundwater samples. Shallow groundwater samples collected beneath recently harvested potato fields contained more pesticides and had higher concentrations of pesticides than samples collected from other groundwater sources sampled during the study. Generally, pesticide concentrations were lower in groundwater samples than in surfacewater or sediment samples, with the exception of the fungicide boscalid, which was found to have its highest concentration in a shallow groundwater sample collected in Wisconsin. Thirteen pesticides, including four fungicides, were detected in suspended-sediment samples. The most

Application of Fungicides and Microalgal Phenolic Extracts for the Direct Control of Fumonisin Contamination in Maize.

Science.gov (United States)

Scaglioni, Priscila Tessmer; Blandino, Massimo; Scarpino, Valentina; Giordano, Debora; Testa, Giulio; Badiale-Furlong, Eliana

2018-05-16

Fungicides and, for the first time, microalgal phenolic extracts (MPE) from Spirulina sp. and Nannochloropsis sp. were applied on maize culture media under field conditions to evaluate their ability to minimize Fusarium species development and fumonisin production. An in vitro assay against F. verticillioides was carried out using maize grains as the culture medium. An open-field experiment was carried out in Northwest Italy under natural infection conditions. The compared treatments were factorial combinations of two insecticide treatments (an untreated control and pyrethroid, used against European Corn Borer), four antifungal treatments (an untreated control, MPE from Spirulina sp., MPE from Nannochloropsis sp., and a synthetic fungicide), and two timings of the application of the antifungal compounds (at maize flowering and at the milk stage). The MPE compounds were capable of inhibiting fumonisin production in vitro more efficiently than tebuconazole. Insecticide application reduced the infection by Fusarium species and subsequent fumonisin contamination. However, fumonisins in maize fields were not significantly controlled by either fungicide or MPE application.

Fungicidal effect of 15 disinfectants against 25 fungal contaminants commonly found in bread and cheese manufacturing.

Science.gov (United States)

Bundgaard-Nielsen, K; Nielsen, P V

1996-03-01

Resistance of 19 mold and 6 yeast species to 15 commercial disinfectants was investigated by using a suspension method in which the fungicidal effect and germination time were determined at 20 degrees C. Disinfectants containing 0.5% dodecyldiethylentriaminacetic acid, 10 g of chloramine-T per 1, 2.0% formaldehyde, 0.1% potassium hydroxide, 3.0% hydrogen peroxide, or 0.3% peracetic acid were ineffective as fungicides. The fungicidal effect of quaternary ammonium compounds and chlorine compounds showed great variability between species and among the six isolates of Penicillium roqueforti var. roqueforti tested. The isolates of P roqueforti var. carneum, P. discolor, Aspergillus versicolor, and Eurotium repens examined were resistant to different quaternary ammonium compounds. Conidia and vegetative cells were killed by alcohols, whereas ascospores were resistant. Resistance of ascospores to 70% ethanol increased with age. Both P. roqueforti var. roqueforti and E. repens showed great variability of resistance within isolates of each species.

Influence of the fungicide Folcidin on the distribution and metabolism of /sup 32/P in gherkin plants

Energy Technology Data Exchange (ETDEWEB)

Hanker, I; Kudelova, A; Taimr, L [Vyzkumne Ustavy Rostlinne Vyroby, Prague (Czechoslovakia). Ustav Ochrany Rostlin; Friedrich, A [Ceskoslovenska Akademie Ved, Prague. Ustav Experimentalni Botaniky

1976-01-01

A high accumulation of /sup 32/P was observed in the leaves of intact gherkin plants 9 days after their roots had been treated with a 0.005% suspension of the systemic fungicide Folcidin 50WP (cypendazole), and 8 days after the roots had been exposed to labelled phosphate. Folcidin also affected phosphorus metabolism in the plants. A high biological cytokinin-like activity of the fungicide was established using a callus cytokinin bioassay.

Estimation of modern range of fungicides and scope of their application in agriculture of Ukraine as component of state social and hygienic monitoring

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Vavrinevych O.P.

2013-12-01

Full Text Available The analysis of the range of pesticides, including fungicides, authorized for use in Ukraine and the scope of their application during 1999 - 2012 years was carried out. Statistical research methods were used in the analysis, evaluation of the results was car¬ried out in terms of the rate of growth and increase. It was determined that in the range structure of pesticides, authorized for use in Ukraine the largest share accounted for herbicides. Part of the herbicides was 43,8±0,95% on average over the period from 1999 to 2012. The share of fungicides was 28,6±1,1%, insecticides - 20,3±0,78%, plant growth regulators - 7,4±0,59%. Mixed fungicides are the largest part of fungicides in the structure of the range (26,3-39,3%, the number of its had increased by 542% over 13-year period. Prior to 2003 there was a slight increase in the number of mixed fungicides, growth rate was 0-8,3% since 2006, its rate of increase has averaged 53% every 2 years. Triazoles and conazoles (14,9-31,4%, benzimidazoles, imidazoles (9,8-14,7%, carbamates, dithiocarbamates (3,1-13,8%, inorganic compounds (6,1-11,1% containing one active ingredient in formulation were the most common among the fungicides. The growth rate of strobilurin fungicides was 900%, triazoles – 550%, benzimidazoles, imidazoles – 400%, inorganic compounds – 243%, aniline-pyrimidines – 200%, pyrimidines, pyridines, pyrroles – 67%, dithiocarbamic and carbamic acid derivatives – 50%, phthalimides, phenylsulfamides, amides – 43%.

Design, Synthesis and Fungicidal Activities of Some Novel Pyrazole Derivatives

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Xue-Ru Liu

2014-09-01

Full Text Available In order to discover new compounds with good fungicidal activities, 32 pyrazole derivatives were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR, 13C-NMR, and high-resolution electrospray ionization mass spectrometry (HR-ESI-MS, and their fungicidal activities against Botrytis cinerea, Rhizoctonia solani Kuhn, Valsa mali Miyabe et Yamada, Thanatephorus cucumeris (Frank Donk, Fusarium oxysporum (S-chl f.sp. cucumerinum Owen, and Fusarium graminearum Schw were tested. The bioassay results indicated that most of the derivatives exhibited considerable antifungal activities, especially compound 26 containing a p-trifluoromethyl- phenyl moiety showed the highest activity, with EC50 values of 2.432, 2.182, 1.787, 1.638, 6.986, and 6.043 μg/mL against B. cinerea, R. solani, V. mali, T. cucumeris, F. oxysporum, and F. graminearum, respectively. Moreover, the activities of compounds such as compounds 27–32 were enhanced by introducing isothiocyanate and carboxamide moieties to the 5-position of the pyrazole ring.

Borrelidin B: isolation, biological activity, and implications for nitrile biosynthesis.

Science.gov (United States)

Schulze, Christopher J; Bray, Walter M; Loganzo, Frank; Lam, My-Hanh; Szal, Teresa; Villalobos, Anabella; Koehn, Frank E; Linington, Roger G

2014-11-26

Borrelidin (1) is a nitrile-containing bacterially derived polyketide that is a potent inhibitor of bacterial and eukaryotic threonyl-tRNA synthetases. We now report the discovery of borrelidin B (2), a tetrahydro-borrelidin derivative containing an aminomethyl group in place of the nitrile functionality in borrelidin. The discovery of this new metabolite has implications for both the biosynthesis of the nitrile group and the bioactivity of the borrelidin compound class. Screening in the SToPS assay for tRNA synthetase inhibition revealed that the nitrile moiety is essential for activity, while profiling using our in-house image-based cytological profiling assay demonstrated that 2 retains biological activity by causing a mitotic stall, even in the absence of the nitrile motif.

PHENOTYPIC CHARACTERISATION AND GENETIC ANALYSIS OF MUTANTS OF ASPERGILLUS NIDULANS RESISTANT TO THE FUNGICIDE TOLCLOFOS-METHYL

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A CHIBANI

2000-12-01

Full Text Available Spontaneous mutants of Aspergillus nidulans were recovered from 0,55.10+7  conidia incubated on synthetic medium supplemented with 100 mg tolclofos-methyl/ml. They differed considerably in morphology, growth rate, and level of resistance to two other fungicides. All mutants tested were cross-resistant to quintozene and vinclozolin; they produced fewer conidia than their wild-type parent. Some mutants required fungicides for maximum growth. Genetic analysis revealed that the mutants carried mutations in one gene located on linkage group III.

Grape berry bacterial inhibition by different copper fungicides

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Martins Guilherme

2016-01-01

Full Text Available Copper fungicides are widely used in viticulture. Due to its large spectrum of action, copper provides an efficient control over a great number of vine pathogens. Previous studies showed that, high levels of cupric residues can impact grape-berry microbiota, in terms of the size and population structure, reducing the diversity and the abundance. Due to the importance of grape-berry bacterial in crop health, and the potential impact of copper fungicides over the microbiota, we determined Minimum Inhibitory Concentration (MIC of different copper formulations for bacterial species isolated from grape berries. We study the Minimum Inhibitory Concentration (MIC of different copper formulations (copper sulphate (CuSO4 pure, Bordeaux mixture (CuSO4 + Ca(OH2, copper oxide (Cu2O, copper hydroxide (Cu(OH2 over 92 bacterial strains isolated from grape berries in different stages of the ripening process. The results of MIC measurements revealed that the different copper formulations have a variable inhibitory effect and among the different isolates, some species are the most resistant to all copper formulations than others. This study confirm that usage of cupric phytosanitary products should be reasonable independently of the farming system; they also provide evidence of the importance of the choice of which copper formulations are to be used regarding their impact on the grape berry bacterial microbiota.

Combination Effects of (TriAzole Fungicides on Hormone Production and Xenobiotic Metabolism in a Human Placental Cell Line

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Svenja Rieke

2014-09-01

Full Text Available Consumers are exposed to multiple residues of different pesticides via the diet. Therefore, EU legislation for pesticides requires the evaluation of single active substances as well as the consideration of combination effects. Hence the analysis of combined effects of substances in a broad dose range represents a key challenge to current experimental and regulatory toxicology. Here we report evidence for additive effects for (triazole fungicides, a widely used group of antifungal agents, in the human placental cell line Jeg-3. In addition to the triazoles cyproconazole, epoxiconazole, flusilazole and tebuconazole and the azole fungicide prochloraz also pesticides from other chemical classes assumed to act via different modes of action (i.e., the organophosphate chlorpyrifos and the triazinylsulfonylurea herbicide triflusulfuron-methyl were investigated. Endpoints analysed include synthesis of steroid hormone production (progesterone and estradiol and gene expression of steroidogenic and non-steroidogenic cytochrome-P-450 (CYP enzymes. For the triazoles and prochloraz, a dose dependent inhibition of progesterone production was observed and additive effects could be confirmed for several combinations of these substances in vitro. The non-triazoles chlorpyrifos and triflusulfuron-methyl did not affect this endpoint and, in line with this finding, no additivity was observed when these substances were applied in mixtures with prochloraz. While prochloraz slightly increased aromatase expression and estradiol production and triflusulfuron-methyl decreased estradiol production, none of the other substances had effects on the expression levels of steroidogenic CYP-enzymes in Jeg-3 cells. For some triazoles, prochloraz and chlorpyrifos a significant induction of CYP1A1 mRNA expression and potential combination effects for this endpoint were observed. Inhibition of CYP1A1 mRNA induction by the AhR inhibitor CH223191 indicated AhR receptor dependence this

Profitability of fungicide use decisions among cocoa farmers in south ...

African Journals Online (AJOL)

A decision theoretic approach and regression method were used to analyze the data collected. The results indicated that (i) expected crop loss should be taken into account when deciding on the amount of fungicides to apply in the study area and (ii) the use rate recommended by CRIN could not be used in all situations – it ...

Effect of amino acids on tannase biosynthesis by Bacillus licheniformis KBR6.

Science.gov (United States)

Mohapatra, Pradeep K Das; Pati, Bikas R; Mondal, Keshab C

2009-04-01

Microbial tannase (tannin acyl hydrolase, EC 3.1.1.20), a hydrolysable tannin-degrading enzyme, has gained importance in various industrial processes, and is used extensively in the manufacture of instant tea, beer, wine, and gallic acid. Tannase is an inducible enzyme, and hydrolysable tannin, especially tannic acid, is the sole inducer. This study is of the effect of various amino acids and their analogues on tannase biosynthesis by Bacillus licheniformis KBR6 to ascertain the mode of action of these growth factors on tannase biosynthesis from microbial origin. Enzyme production was carried out in enriched tannic acid medium through submerged fermentation for 20 h at 35 degrees C. Different amino acids at a concentration of 0.05 g% (w/v) were added to the culture medium immediately after sterilization. Culture supernatant was used as the source of the enzyme and the quantity of tannase was estimated by the colorimetric assay method. Growth of the organism was estimated according to biomass dry weight. Maximum tannase (2.87-fold that of the control) was synthesized by B. licheniformis KBR6 when alanine was added to the culture medium. Other amino acids, such as DL-serine, L-cystine, glycine, L-ornithine, aspartic acid, L-glutamic acid, DL-valine, L-leucine and L-lysine, also induced tannase synthesis. L-Cysteine monohydrochloride and DL-threonine were the most potent inhibitors. Regulation of tannase biosynthesis by B. licheniformis in the presence of various amino acids is shown. This information will be helpful for formulating an enriched culture medium for industrial-scale tannase production.

Effects of a Squalene Epoxidase Inhibitor, Terbinafine, on Ether Lipid Biosyntheses in a Thermoacidophilic Archaeon, Thermoplasma acidophilum

Science.gov (United States)

Kon, Takahide; Nemoto, Naoki; Oshima, Tairo; Yamagishi, Akihiko

2002-01-01

The archaeal plasma membrane consists mainly of diether lipids and tetraether lipids instead of the usual ester lipids found in other organisms. Although a molecule of tetraether lipid is thought to be synthesized from two molecules of diether lipids, there is no direct information about the biosynthetic pathway(s) or intermediates of tetraether lipid biosynthesis. In this study, we examined the effects of the fungal squalene epoxidase inhibitor terbinafine on the growth and ether lipid biosyntheses in the thermoacidophilic archaeon Thermoplasma acidophilum. Terbinafine was found to inhibit the growth of T. acidophilum in a concentration-dependent manner. When growing T. acidophilum cells were pulse-labeled with [2-14C]mevalonic acid in the presence of terbinafine, incorporation of radioactivity into the tetraether lipid fraction was strongly suppressed, while accumulation of radioactivity was noted at the position corresponding to diether lipids, depending on the concentration of terbinafine. After the cells were washed with fresh medium and incubated further without the radiolabeled substrate and the inhibitor, the accumulated radioactivity in the diether lipid fraction decreased quickly while that in the tetraether lipids increased simultaneously, without significant changes in the total radioactivity of ether lipids. These results strongly suggest that terbinafine inhibits the biosynthesis of tetraether lipids from a diether-type precursor lipid(s). The terbinafine treatment will be a tool for dissecting tetraether lipid biosynthesis in T. acidophilum. PMID:11844769

Differences Among Commonly Sprayed Orchard Fungicides in Targeting the Beneficial Fungi Associated with Honey Bee Colony and Bee Bread Provisions (In Vitro)

Science.gov (United States)

Our studies evaluated the effects of representative fungicides, boscalid and pyraclostrobin, propiconazole, and chlorothalonil, alone and in combination, on 12 fungi species isolated from bee bread. Chlorothalonil was fungicidal (slowed growth without killing) and was least effective on Aspergillus...

Assessing effects of the fungicide tebuconazole to heterotrophic microbes in aquatic microcosms

NARCIS (Netherlands)

Dimitrov, M.R.; Kosol, Sujitra; Smidt, H.; Brink, van den P.J.; Wijngaarden, van R.P.A.; Brock, T.C.M.; Maltby, L.

2014-01-01

Aquatic ecological risk assessment of fungicides in Europe under Regulation 1107/2009/EC does not currently assess risk to non-target bacteria and fungi. Rather, regulatory acceptable concentrations based on ecotoxicological data obtained from studies with fish, invertebrates and primary producers

Expression of the insect metalloproteinase inhibitor IMPI in the fat body of Galleria mellonella exposed to infection with Beauveria bassiana.

Science.gov (United States)

Vertyporokh, Lidiia; Wojda, Iwona

2017-01-01

The inducible metalloproteinase inhibitor (IMPI) discovered in Galleria mellonella is currently the only specific inhibitor of metalloproteinases found in animals. Its role is to inhibit the activity of metalloproteinases secreted by pathogenic organisms as virulence factors to degrade immune-relevant polypeptides of the infected host. This is a good example of an evolutionary arms race between the insect hosts and their natural pathogens. In this report, we analyze the expression of a gene encoding an inducible metalloproteinase inhibitor (IMPI) in fat bodies of the greater wax moth larvae Galleria mellonella infected with an entomopathogenic fungus Beauveria bassiana. We have used a natural infection, i.e. covering larval integument with fungal aerospores, as well as injection of fungal blastospores directly into the larval hemocel. We compare the expression of IMPI with the expression of genes encoding proteins with fungicidal activity, gallerimycin and galiomycin, whose expression reflects the stimulation of Galleria mellonella defense mechanisms. Also, gene expression is analyzed in the light of survival of animals after spore injection.

The Spatial Organization of Glucosinolate Biosynthesis

DEFF Research Database (Denmark)

Nintemann, Sebastian

cells is an open question. Likewise, it is not known how glucosinolate biosynthesis is orchestrated at the subcellular level. These open questions were addressed with several approaches in this project, with the aim of shedding light on the spatial organization of glucosinolate biosynthesis from...... between the individual classes of glucosinolates under constitutive and induced conditions and identified the source tissues of these defense compounds. Protein-protein interaction studies were carried out to investigate the subcellular organization of glucosinolate biosynthesis. We identified a family...

Preliminary Trials on Treatment of Esca-Infected Grapevines with Trunk Injection of Fungicides

Directory of Open Access Journals (Sweden)

T. Dula

2007-04-01

Full Text Available An increase in trunk diseases (due to esca, Agrobacterium, rugose wood virus, leaf roll viruses, phytoplasma etc. leading to young vines death is a very serious worry in vineyards in Hungary, as it is in other countries. In response to a demand expressed by grapevine growers, a method was tested for the direct treatment of pathogens in wood tissue. An experiment based on trunk injection was carried out in an esca infected vineyard. The various fungicides (propiconazole, difenoconazole, thiabendazole; propiconazole+ thiabendazole were injected into the trunk before the beginning of the xylem sap flow at high pressure. As a result the number of symptomatic plants was decreased, and the vigour of the plants was not impaired by the fungicide ingredients. The combination difenoconazole+ thiabendazole showed the best result.

Tentative identification of 2-imidazoline as a transformation product of ethylenebisdithiocarbamate fungicides

NARCIS (Netherlands)

Vonk, J.W.; Kaars Sijpesteijn, A.

2-Imidazoline has been identified tentatively as a minor conversion product of ethylenethiourea in seedlings of cucumber and wheat. As ethylenethiourea is known to be present in plants after root treatment with ethylenebisdithiocarbamate fungicides, 2-imidazoline is assumed to be a terminal residue

Signum, a new fungicide with interesting properties in resistance management of fungal diseases in strawberries.

Science.gov (United States)

Hauke, K; Creemers, P; Brugmans, W; Van Laer, S

2004-01-01

Signum, a new fungicide developed by BASF, was applied during 6 successive years against fungal diseases in strawberries. The product is formulated as a water dispersible granule, containing 6.7 % pyraclostrobin and 26.7 % boscalid. Pyraclostrobin is similar in chemistry to other strobilurin fungicides like kresoxim-methyl and trifloxystrobin, registered for fruit disease control. Boscalid belongs to the class of carboxyanilides. Both components in the premix formulation combine two different biochemical modes of action in the fungal cell respiration. Therefore, this co-formulation gives a broad-spectrum activity and also a reduced resistance risk for different target pathogens. Botrytis cinerea is the most important disease on strawberry-fruits and thus the control of fruit rot is mainly focused on this fungus. In average over 6 years, Signum has not only given a very good control against Botrytis fruit rot, but it has also shown a high performance in the control of Colletotrichum. Besides, Signum provides good control of powdery mildew (Podosphaera aphanis) and limits the shift to other fruit rots like leather rot (Phytophthora cactorum and leak (Rhizopus, Mucor). The availability of several categories of fungicide families with a different mode of action gives opportunities in alternating different fungicides and is the best guarantee for a sustainable control of fruit rot in all kinds of strawberry production methods. Signum should be integrated in an overall disease management program. Trials, in which the applications of Signum were timed on disease forecasting, based on environmental factors favorable for Botrytis development, were very promising. This tool can also help in establishing the IPM-concept in the production of strawberries.

Treatment and Prevention of Breast Cancer Using Multifunctional Inhibitors of Cholesterol Biosynthesis

Science.gov (United States)

2015-08-01

suggesting an allosteric modification of estrogen receptor  RO blocks the production of an estrogen regulated gene ( progesterone receptor) in...alternative targets in the pathway leading to the production of cholesterol, which might be regulated with less toxic inhibitors to control the progression of...to effectively treat and prevent cancers of the breast. Our goal was to identify alternative targets in the pathway leading to the production of

Fungicide-driven evolution and molecular basis of multidrug resistance in field populations of the grey mould fungus Botrytis cinerea.

Directory of Open Access Journals (Sweden)

Matthias Kretschmer

2009-12-01

Full Text Available The grey mould fungus Botrytis cinerea causes losses of commercially important fruits, vegetables and ornamentals worldwide. Fungicide treatments are effective for disease control, but bear the risk of resistance development. The major resistance mechanism in fungi is target protein modification resulting in reduced drug binding. Multiple drug resistance (MDR caused by increased efflux activity is common in human pathogenic microbes, but rarely described for plant pathogens. Annual monitoring for fungicide resistance in field isolates from fungicide-treated vineyards in France and Germany revealed a rapidly increasing appearance of B. cinerea field populations with three distinct MDR phenotypes. All MDR strains showed increased fungicide efflux activity and overexpression of efflux transporter genes. Similar to clinical MDR isolates of Candida yeasts that are due to transcription factor mutations, all MDR1 strains were shown to harbor activating mutations in a transcription factor (Mrr1 that controls the gene encoding ABC transporter AtrB. MDR2 strains had undergone a unique rearrangement in the promoter region of the major facilitator superfamily transporter gene mfsM2, induced by insertion of a retrotransposon-derived sequence. MDR2 strains carrying the same rearranged mfsM2 allele have probably migrated from French to German wine-growing regions. The roles of atrB, mrr1 and mfsM2 were proven by the phenotypes of knock-out and overexpression mutants. As confirmed by sexual crosses, combinations of mrr1 and mfsM2 mutations lead to MDR3 strains with higher broad-spectrum resistance. An MDR3 strain was shown in field experiments to be selected against sensitive strains by fungicide treatments. Our data document for the first time the rising prevalence, spread and molecular basis of MDR populations in a major plant pathogen in agricultural environments. These populations will increase the risk of grey mould rot and hamper the effectiveness of

Identification of isolates of the plant pathogen Leptosphaeria maculans with resistance to the triazole fungicide fluquinconazole using a novel In Planta assay.

Directory of Open Access Journals (Sweden)

Angela P Van de Wouw

Full Text Available Leptosphaeria maculans is the major pathogen of canola (oilseed rape, Brassica napus worldwide. In Australia, the use of azole fungicides has contributed to the 50-fold increase in canola production in the last 25 years. However, extensive application of fungicides sets the stage for the selection of fungal populations with resistance. A high-throughput in planta assay was developed to allow screening of thousands of isolates from multiple populations. Using this screen, isolates were identified with decreased sensitivity to the fungicide fluquinconazole when applied at field rates as a protective seed dressing: these isolates cause significantly larger lesions on cotyledons and true leaves and increased disease severity at plant maturity. This increased in planta resistance was specific to fluquinconazole, with no cross resistance to flutriafol or tebuconazole/prothioconazole. In a limited set of 22 progeny from a cross between resistant and susceptible parents, resistance segregated in a 1:1 ratio, suggesting a single gene is responsible. A survey of 200 populations from across canola growing regions of Australia revealed fungicide resistance was present in 15% of the populations. Although in vitro analysis of the fungicide resistant isolates showed a significant shift in the average EC50 compared to the sensitive isolates, this was not as evident as the in planta assays. The development of this novel, high-throughput in planta assay has led to the identification of the first fungicide resistant L. maculans isolates, which may pose a threat to the productivity of the Australian canola industry.

Synthesis and fungicidal properties of 2,4-diaza-1,3,5 ...

African Journals Online (AJOL)

The preparation of 2,4-diaza-1,3,5-pentanetrione compounds were described. The fungicidal effects of these compounds on the mycelial growth of the isolate, Phoma eupyrena were carried out by in vitro experiment. The results show that the response to treatment depended not only on the concentration of the compounds ...

Application of Copper Solid Amalgam Electrode for Determination of Fungicide Tebuconazole

Czech Academy of Sciences Publication Activity Database

Nováková, Kateřina; Navrátil, Tomáš; Jaklová Dytrtová, Jana; Chýlková, J.

2013-01-01

Roč. 8, č. 1 (2013), s. 1-16 ISSN 1452-3981 R&D Projects: GA ČR GAP206/11/1638; GA ČR(CZ) GAP208/12/1645 Institutional support: RVO:61388955 ; RVO:61388963 Keywords : tebuconazole * fungicide * copper solid amalgam electrode Subject RIV: CG - Electrochemistry Impact factor: 1.956, year: 2013

Effects of artea, a systemic fungicide, on the antioxidant system and ...

African Journals Online (AJOL)

STORAGESEVER

2009-09-01

Sep 1, 2009 ... from oxygen metabolism in mitochondria (Alscher et al.,. 2002). Plants have well ... effects on plant in the sense they may induce a decrease in growth as well as modulating the metabolic balance. Morphological effects of ... with fungicide concentration (about 150% at 100 ppm). At. 25 ppm, the increase in ...

Strobilurin fungicides induce changes in photosynthetic gas exchange that do not improve water use efficiency of plants grown under conditions of water stress.

Science.gov (United States)

Nason, Mark A; Farrar, John; Bartlett, David

2007-12-01

The effects of five strobilurin (beta-methoxyacrylate) fungicides and one triazole fungicide on the physiological parameters of well-watered or water-stressed wheat (Triticum aestivum L.), barley (Hordeum vulgare L.) and soya (Glycine max Merr.) plants were compared. Water use efficiency (WUE) (the ratio of rate of transpiration, E, to net rate of photosynthesis, A(n)) of well-watered wheat plants was improved slightly by strobilurin fungicides, but was reduced in water-stressed plants, so there is limited scope for using strobilurins to improve the water status of crops grown under conditions of drought. The different strobilurin fungicides had similar effects on plant physiology but differed in persistence and potency. When applied to whole plants using a spray gun, they reduced the conductance of water through the epidermis (stomatal and cuticular transpiration), g(sw), of leaves. Concomitantly, leaves of treated plants had a lower rate of transpiration, E, a lower intercellular carbon dioxide concentration, c(i), and a lower net rate of photosynthesis, A(n), compared with leaves of control plants or plants treated with the triazole. The mechanism for the photosynthetic effects is not known, but it is hypothesised that they are caused either by strobilurin fungicides acting directly on ATP production in guard cell mitochondria or by stomata responding to strobilurin-induced changes in mesophyll photosynthesis. The latter may be important since, for leaves of soya plants, the chlorophyll fluorescence parameter F(v)/F(m) (an indication of the potential quantum efficiency of PSII photochemistry) was reduced by strobilurin fungicides. It is likely that the response of stomata to strobilurin fungicides is complex, and further research is required to elucidate the different biochemical pathways involved. Copyright (c) 2007 Society of Chemical Industry.

Comparison of the Fungicide Sensitivity of Alberta and Prince Edward Island Isolates of Fusarium graminearum Producing Either 3- or 15-acetyl Deoxynivalenol

Science.gov (United States)

Fusarium graminearum Schwabe of the ‘3ADON’ chemotype is now displacing ‘15ADON’ isolates in Canada. One concern regarding this shift in chemotypes is related to potential differences in fungicide sensitivity. This could have significant implications as fungicide application is an important strate...

Dipping Strawberry Plants in Fungicides before Planting to Control Anthracnose

Directory of Open Access Journals (Sweden)

Myeong Hyeon Nam

2014-03-01

Full Text Available Anthracnose crown rot (ACR, caused by Colletotrichum fructicola, is a serious disease of strawberry in Korea. The primary inoculums of ACR were symptomless strawberry plants, plant debris, and other host plants. To effectively control anthracnose in symptomless transplanted strawberries, it is necessary to use diseasefree plants, detect the disease early, and apply a fungicide. Therefore, in 2010 and 2011, we evaluated the efficacy of pre-plant fungicide dips by using strawberry transplants infected by C. fructicola for the control of anthracnose. Dipping plants in prochloraz-Mn for 10 min before planting was most effective for controlling anthracnose in symptomless strawberry plants and resulted in more than 76% control efficacy. Azoxystrobin showed a control efficacy of over 40%, but plants treated with pyraclostrobin, mancozeb and iminoctadine tris showed high disease severity. The control efficacy of the dip treatment with prochloraz-Mn did not differ with temperature and time. Treatment with prochloraz-Mn for more than an hour caused growth suppression in strawberry plants. Therefore, the development of anthracnose can be effectively reduced by dipping strawberry plants for 10 min in prochloraz-Mn before planting.

Synthesis and study on biological activity of nitrogen-containing heterocyclic compounds – regulators of enzymes of nucleic acid biosynthesis

Directory of Open Access Journals (Sweden)

Alexeeva I. V.

2013-07-01

Full Text Available Results of investigations on the development of new regulators of functional activity of nucleic acid biosynthesis enzymes based on polycyclic nitrogen-containing heterosystems are summarized. Computer design and molecular docking in the catalytic site of target enzyme (T7pol allowed to perform the directed optimization of basic structures. Several series of compounds were obtained and efficient inhibitors of herpes family (simple herpes virus type 2, Epstein-Barr virus, influenza A and hepatitis C viruses were identified, as well as compounds with potent antitumor, antibacterial and antifungal activity. It was established that the use of model test systems based on enzymes participating in nucleic acids synthesis is a promising approach to the primary screening of potential inhibitors in vitro.

Metallothionein induction, antioxidative responses, glycogen and growth changes in Tubifex tubifex (Oligochaete) exposed to the fungicide, fenhexamid

International Nuclear Information System (INIS)

Mosleh, Yahia Y.; Paris-Palacios, Severine; Couderchet, Michel; Biagianti-Risbourg, Sylvie; Vernet, Guy

2005-01-01

Laboratory studies were conducted to determine the effects of different concentrations of fenhexamid (0.1, 1, and 10 mg L -1 ) on growth, oxidative stress, protein, glycogen, and metallothionein (MT) contents in Tubifex tubifex after an exposure of 2, 4, and 7 days. In addition, residues of the fungicide were followed in water and in the worms. In water, fenhexamid concentration decreased slowly (maximum - 2±0.03% after 2 days for 1 mg L -1 ). In the worms, it increased after 4 days and decreased thereafter, confirming that the worms were exposed to the fungicide and not to a degradation product. LC 50 values were between 95.22±5.36 and 32.11±1.8 mg L -1 depending on exposure time. Exposure to fenhexamid had a negative effect on T. tubifex growth (maximum effect -12.2±0.8% after 7 days with 10 mg L -1 ) demonstrating the toxic effect of the pesticide. This growth rate decrease was accompanied by a reduction in protein and glycogen contents. The activity of catalase (CAT), and glutathione reductase (GR) increased in response to the fungicide demonstrating an oxidative stress in the worms. In contrast glutathion-S-transferase activity (GST) decreased. Exposure to fenhexamid also induced synthesis of MT (maximum +78±8% after 2 days for 10 mg L -1 ). The specificity of MT concentration increase in response to metals is discussed. - Exposure to the fungicide fenhexamid increased metallothionein levels in Tubifex tubifex

Detachment of sprayed colloidal copper oxychloride-metalaxyl fungicides by a shallow water flow.

Science.gov (United States)

Pose-Juan, Eva; Paradelo-Pérez, Marcos; Rial-Otero, Raquel; Simal-Gándara, Jesus; López-Periago, José E

2009-06-01

Flow shear stress induced by rainfall promotes the loss of the pesticides sprayed on crops. Some of the factors influencing the losses of colloidal-size particulate fungicides are quantified by using a rotating shear system model. With this device it was possible to analyse the flow shear influencing washoff of a commercial fungicide formulation based on a copper oxychloride-metalaxyl mixture that was sprayed on a polypropylene surface. A factor plan with four variables, i.e. water speed and volume (both variables determining flow boundary stress in the shear device), formulation dosage and drying temperature, was set up to monitor colloid detachment. This experimental design, together with sorption experiments of metalaxyl on copper oxychloride, and the study of the dynamics of metalaxyl and copper oxychloride washoff, made it possible to prove that metalaxyl washoff from a polypropylene surface is controlled by transport in solution, whereas that of copper oxychloride occurs by particle detachment and transport of particles. Average losses for metalaxyl and copper oxychloride were, respectively, 29 and 50% of the quantity applied at the usual recommended dosage for crops. The key factors affecting losses were flow shear and the applied dosage. Empirical models using these factors provided good estimates of the percentage of fungicide loss. From the factor analysis, the main mechanism for metalaxyl loss induced by a shallow water flow is solubilisation, whereas copper loss is controlled by erosion of copper oxychloride particles.

RAMAN SPECTROSCOPY-BASED METABOLOMICS FOR DIFFERENTIATING EXPOSURES TO TRIAZOLE FUNGICIDES USING RAT URINE

Science.gov (United States)

Normal Raman spectroscopy was evaluated as a metabolomic tool for assessing the impacts of exposure to environmental contaminants, using rat urine collected during the course of a toxicological study. Specifically, one of three triazole fungicides, myclobutanil, propiconazole or ...

Radioisotopes and fungicide research- present status and future prospects

International Nuclear Information System (INIS)

Chatrath, M.S.

1996-01-01

The developments in pesticides and radioisotopes fields were so near to each other that at a very early stage in this history, both became linked together and their usefulness was recognised for faster development. The purpose of this communication is to illustrate the present status these techniques in fungicide research by drawing suitable examples and also to bring out the directions in which future research will be going with the aid of these tools. 72 refs

In silico approach towards identification of potential inhibitors of Helicobacter pylori DapE.

Science.gov (United States)

Mandal, Rahul Shubhra; Das, Santasabuj

2015-01-01

Helicobacter pylori is a gastric mucosal pathogen and is associated with diseases like peptic ulcer and gastric cancer. To combat H. pylori infection, there is an urgent need for new class of antibiotics due to the emergence of drug-resistant strains. Enzymes involved in bacterial lysine biosynthetic pathways may be potential targets for antibacterial drug development, since lysine is an essential component of the bacterial peptidoglycan cell wall. No pathway exists for lysine biosynthesis in humans; hence, the inhibitors targeting bacterial enzymes may have selective toxicity. dapE-encoded N-succinyl-L,L-diaminopimelic acid desuccinylase (DapE) is a critical enzyme of this pathway and deletion of DapE gene is lethal to H. pylori, since the organism has no alternative pathway for lysine biosynthesis. In this study, we reported a 3D model structure of H. pylorie DapE, which consisted of a catalytic domain and a dimerization domain generated by MODELLER software. We also confirmed the stability of the modeled structure through 10 ns molecular dynamics simulation using GROMACS software. Next, to identify potential small molecule inhibitors of DapE, drug-like small molecule-screening library was generated. This was performed by Tanimoto-based similarity searching in the PubChem Database with DapE substrate L,L-SDAP as a query molecule, followed by fragment-based docking approach using GLIDE XP. This approach identified two potential substrate-competitive small molecule inhibitors of DapE. These new molecules may provide a starting point to search for novel therapeutics.

Phytopharmacological studies on the rice diseases. III. Fungitoxicity of the different dust fungicides evaluated by protoplasm coagulation in conidia of Cochliobolus miyabeanus

Energy Technology Data Exchange (ETDEWEB)

Hashioka, Y; Ikegami, H

1956-01-01

The modes of reaction of fungal conidia to fungicides (mercury and copper compounds) varied with the concentration of fungicide. At lower fugicide concentrations, restriction of elongation of germ-tubes was noted. At high concentrations, there was no germination accompanied by vacuolation. At the highest concentrations, conidia protoplasm was coagulated.

[Determination of seven strobilurin fungicide residues in Chinese herbs by liquid chromatography-tandem mass spectrometry coupled with solid phase extraction].

Science.gov (United States)

Zhang, Yule; Huang, Chaoqun; Zhu, Xiaoyu; Chen, Xiaomei; Mo, Weimin

2013-03-01

An LC-MS/MS method was developed for the simultaneously determination of seven strobilurin fungicide residues in Chinese herbs. The strobilurin fungicides include Z-metominostrobin, kresoxim-methyl, dimoxystrobin, picoxystrobin, pyraclostrobin, azoxystrobin and trifloxystrobin. The sample was extracted with ethyl acetate and cleaned-up by an amino SPE column. The seven strobilurin fungicide residues were separated on a C18 column with gradient elution of 1.0 per thousand formic acid and methanol as mobile phases, and detected by ESI-MS in positive ion and selective reaction monitoring (SRM) mode. External standard method was used to the quantification with good linear relationships (r > or = 0. 996). The LOQs were 2 micro g/kg for dimoxystrobin, picoxystrobin and trifloxystrobin, 4 mciro g/kg for pyraclostrobin and azoxystrobin, 10 micro g/kg for Z-metominostrobin and kresoxim-methyl. The recoveries were from 60.4% to 110% with the RSDs between 1.2% and 17%. The developed method is suitable for the determination and confirmation of the seven strobilurin fungicide residues in the three of Eight Zhes ( Ophiopogon japonicus (Thunb.), Scrophularia ningpoensis Hemsl. and Corydalis yanhusuo W T Wang).

Effects of selected herbicides and fungicides on growth, sporulation and conidial germination of entomopathogenic fungus Beauveria bassiana.

Science.gov (United States)

Celar, Franci A; Kos, Katarina

2016-11-01

The in vitro fungicidal effects of six commonly used fungicides, namely fluazinam, propineb, copper(II) hydroxide, metiram, chlorothalonil and mancozeb, and herbicides, namely isoxaflutole, fluazifop-P-butyl, flurochloridone, foramsulfuron, pendimethalin and prosulfocarb, on mycelial growth, sporulation and conidial germination of entomopathogenic fungus Beauveria bassiana (ATCC 74040) were investigated. Mycelial growth rates and sporulation at 15 and 25 °C were evaluated on PDA plates containing 100, 75, 50, 25, 12.5, 6.25 and 0% of the recommended application rate of each pesticide. The tested pesticides were classified in four scoring categories based on reduction in mycelial growth and sporulation. All pesticides, herbicides and fungicides tested had fungistatic effects of varying intensity, depending on their rate in the medium, on B. bassiana. The most inhibitory herbicides were flurochloridone and prosulfocarb, and fluazinam and copper(II) hydroxide were most inhibitory among the fungicides, while the least inhibitory were isoxaflutole and chlorothalonil. Sporulation and conidial germination of B. bassiana were significantly inhibited by all tested pesticides compared with the control treatment. Flurochloridone, foramsulfuron, prosulfocarb and copper(II) hydroxide inhibited sporulation entirely at 100% rate (99-100% inhibition), and the lowest inhibition was shown by fluazifop-P-butyl (22%) and metiram (33%). At 100% dosage, all herbicides in the test showed a high inhibitory effect on conidial germination. Conidial germination inhibition ranged from 82% with isoxaflutole to 100% with fluorochloridone, pendimethalin and prosulfocarb. At 200% dosage, inhibition rates even increased (96-100%). All 12 pesticides tested had a fungistatic effect on B. bassiana of varying intensity, depending on the pesticide and its concentration. B. bassiana is highly affected by some herbicides and fungicides even at very low rates. Flurochloridone, foramsulfuron

Effect of the vigour and of the fungicide treatment in the germination and sanity tests of soybean seeds

OpenAIRE

Gomes, Delineide Pereira; Barrozo, Leandra Matos; Souza, Apolyana Lorraine; Sader, Rubens [UNESP; Silva, Gilvania Campos [UNESP

2009-01-01

Soybeans seeds with different levels of vigour, treated and or no with fungicide were submitted to the test of germination in the sand and roll substrates of paper and the test of sanity. In test of germination, there were only significant differences between treatments that used soybeans with high vigour and with low vigour, regardless of the presence or absence of fungicide treatment, in the two substrates. The soybeans with low vigour no treated provided the largest percentages of seed con...

Effects of artea, a systemic fungicide, on the antioxidant system and ...

African Journals Online (AJOL)

The present work aimed at the study of the effects of Artea, a systemic azole fungicide, on durum Wheat (Triticum durum L. cv. GTA dur). Seeds were grown in a medium containing respectively 25, 50, 75 and 100 ppm of Artea under controlled conditions. Roots of eight-day-old plants were used to determine catalase, ...

Glycopeptide antibiotic biosynthesis.

Science.gov (United States)

Yim, Grace; Thaker, Maulik N; Koteva, Kalinka; Wright, Gerard

2014-01-01

Glycopeptides such as vancomycin, teicoplanin and telavancin are essential for treating infections caused by Gram-positive bacteria. Unfortunately, the dwindled pipeline of new antibiotics into the market and the emergence of glycopeptide-resistant enterococci and other resistant bacteria are increasingly making effective antibiotic treatment difficult. We have now learned a great deal about how bacteria produce antibiotics. This information can be exploited to develop the next generation of antimicrobials. The biosynthesis of glycopeptides via nonribosomal peptide assembly and unusual amino acid synthesis, crosslinking and tailoring enzymes gives rise to intricate chemical structures that target the bacterial cell wall. This review seeks to describe recent advances in our understanding of both biosynthesis and resistance of these important antibiotics.

The effect of treating wheat with Ethrel in conjunction with some fungicides on the susceptibility to fungal diseases and on the root zone mycoflora of this plant

Directory of Open Access Journals (Sweden)

Marian Michniewicz

2013-12-01

Full Text Available Wheat cv. Grana grown under field conditions, in the early phase of the first node formation, was sprayed with Ethrel (0.35 ml/m2 and with the fungicides: Sportak 45 EC (0.1 ml/m2 and Bayleton Triple (0.2 g/m2 - separately and in conjunction with Ethrel. It was found that Ethrel reduced the plant's susceptibility to infection by Cercosporella herpotrichoides and by species of the genus Fusarium. The fungicides were more active and also reduced the susceptibility to infection by Erysiphe graminis and Puccinia triticina. The fungistatic effect of Ethrel and Sportak was synergistic only in the case of Cercosporella herpotrichoides. Other interactions between Ethrel and fungicides were not found. Ethrel and fungicides only slightly affected the mycoflora of the root but they completely eliminated the fungi of the genus Mucor from the rhizosphere and reduced the participation of isolates of the genus Alternaria and Cladosporium in the rhizosphere and rhizoplane of wheat. The fungicides were more active than Ethrel. An interaction between Ethrel and fungicides in the reduction of fungi of the genus Fusarium in the rhizosphere was shown.

Identification of Multiple Cryptococcal Fungicidal Drug Targets by Combined Gene Dosing and Drug Affinity Responsive Target Stability Screening

Directory of Open Access Journals (Sweden)

Yoon-Dong Park

2016-08-01

Full Text Available Cryptococcus neoformans is a pathogenic fungus that is responsible for up to half a million cases of meningitis globally, especially in immunocompromised individuals. Common fungistatic drugs, such as fluconazole, are less toxic for patients but have low efficacy for initial therapy of the disease. Effective therapy against the disease is provided by the fungicidal drug amphotericin B; however, due to its high toxicity and the difficulty in administering its intravenous formulation, it is imperative to find new therapies targeting the fungus. The antiparasitic drug bithionol has been recently identified as having potent fungicidal activity. In this study, we used a combined gene dosing and drug affinity responsive target stability (GD-DARTS screen as well as protein modeling to identify a common drug binding site of bithionol within multiple NAD-dependent dehydrogenase drug targets. This combination genetic and proteomic method thus provides a powerful method for identifying novel fungicidal drug targets for further development.

Changes in Sensitivity Levels of Botrytis spp. Population Isolated from Lily to Fungicides and Control under Field Condition

Directory of Open Access Journals (Sweden)

Soosang Hahm

2013-03-01

Full Text Available Forty eight isolates of Botrytis elliptica and 23 isolates of B. cinerea from several locations in Korea were tested for resistance to fungicides used in the farmer's fields. Isolation frequency of B. elliptica having EC50 (effective concentration of 50% value 500−1000 μg/ml to benomyl and mancozeb appeared highly, suggesting that the two fungicides are not effective in controlling leaf blight of lily in the field. The isolates were tested for resistance to fungicides procymidone and iprodione which were most commonly used in the farmer's fields. The rates of EC50 value 5−50 μg/ml to procymidome and iprodione were 93.7% and 100%, respectively, and those of 0−0.1 μg/ml to diethofencarb+carbendazim and fludioxonil were 98.0% and 93.8%, respectively. In the rain-protected cultivation, control of leaf blight of lily was the most effective when iprodine, diethofencarb+ carbendazim, and fludioxonil were sprayed alternately four times during the growing season.

Determination of neonicotinoid insecticides and strobilurin fungicides in particle phase atmospheric samples by liquid chromatography-tandem mass spectrometry.

Science.gov (United States)

Raina-Fulton, Renata

2015-06-03

A liquid chromatography-tandem mass spectrometry method has been developed for the determination of neonicotinoids and strobilurin fungicides in the particle phase fraction of atmosphere samples. Filter samples were extracted with pressurized solvent extraction, followed by a cleanup step with solid phase extraction. Method detection limits for the seven neonicotinoid insecticides and six strobilurin fungicides were in the range of 1.0-4.0 pg/m(3). Samples were collected from June to September 2013 at two locations (Osoyoos and Oliver) in the southern Okanagan Valley Agricultural Region of British Columbia, where these insecticides and fungicides are recommended for use on tree fruit crops (apples, pears, cherries, peaches, apricots) and vineyards. This work represents the first detection of acetamiprid, imidacloprid, clothianidin, kresoxim-methyl, pyraclostrobin, and trifloxystrobin in particle phase atmospheric samples collected in the Okanagan Valley in Canada. The highest particle phase atmospheric concentrations were observed for imidacloprid, pyraclostrobin, and trifloxystrobin at 360.0, 655.6, and 1908.2 pg/m(3), respectively.

The calcineurin pathway inhibitor tacrolimus enhances the in vitro activity of azoles against Mucorales via apoptosis.

Science.gov (United States)

Shirazi, F; Kontoyiannis, D P

2013-09-01

The calcineurin pathway regulates antifungal drug resistance and the virulence of several major human-pathogenic fungi, including the recalcitrant Mucorales. We hypothesized that the fungistatic triazoles posaconazole (PCZ) and itraconazole (ICZ) become fungicidal in the setting of the calcineurin inhibitor tacrolimus (TCR) and that such an effect is mediated through apoptosis. Fungicidal activity and apoptosis were studied using standard microbiological techniques and hyphal metabolic and vital dye reduction assays at 37°C in RPMI 1640. Apoptosis was characterized by detecting intracellular Ca(2+), phosphatidylserine (PS) externalization, DNA fragmentation, plasma membrane integrity, chromatin condensation, reactive oxygen species (ROS) generation, caspase-like activity, ATP, and cytochrome c release. MICs for PCZ and ICZ alone were significantly higher (8 to 128 μg/ml) than those of PCZ or ICZ plus TCR (0.25 to 4 μg/ml) for Rhizopus oryzae, Cunninghamella bertholletiae, and Mucor circinelloides. Both PCZ and ICZ in combination with TCR became fungicidal, and their activity was mediated through increased apoptotic cell death of R. oryzae (10 to 50%), C. bertholletiae (5 to 50%), and M. circinelloides (5 to 55%) germlings, with morphological apoptotic changes characterized by externalization of PS, nuclear condensation, and DNA fragmentation. Moreover, activation of the caspase-like activity was correlated with cell death induced by TCR plus PCZ or ICZ. These changes correlated with elevated intracellular Ca(2+) and ROS levels and disturbance of mitochondrial potential. We found that PCZ or ICZ in combination with TCR renders Mucorales sensitive to triazoles via apoptotic death. These observations could serve as a new paradigm for the development of new therapeutic strategies.

Off-site transport of fungicides with runoff: A comparison of flutolanil and pentachloronitrobeneze applied to creeping bentgrass managed as a golf course fairway

Science.gov (United States)

Flutolanil and pentachloronitrobenzene (PCNB) are fungicides used to control or suppress foliar and soil borne diseases in turf and ornamental crops. On golf courses, sports fields, sod farms and commercial lawns these fungicides are used as preventive treatments to combat snow mold, brown patch an...

Impact of Fungicide Residues on Polymerase Chain Reaction and on Yeast Metabolism

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Gildo Almeida da Silva

Full Text Available ABSTRACT The indiscriminate use of pesticides on grape crops is harmful for consumers´ healthin “in natura” consumption and in the ingestion of wine and grape juice. During winemaking, a rapid and efficient fermentation stage is critical to avoid proliferation of contaminating microorganisms and to guarantee the product´s quality. Polymerase chain reaction (PCR has the advantage of detecting these contaminants in the early stages of fermentation. However,this enzymatic reaction may also be susceptible to specific problems, reducing its efficiency. Agricultural practices, such as fungicide treatments, may be a source of PCR inhibiting factors and may also interfere in the normal course of fermentation.The action of the pesticides captan and folpet on PCR and on yeast metabolism was evaluated, once these phthalimide compounds are widely employed in Brazilian vineyards. DNA amplification was only observed at 75 and 37.5 µg/mL of captan concentrations, whereas with folpet, amplification was observed only in the two lowest concentrations tested (42.2 and 21.1µg/mL.Besides the strong inhibition on Taq polymerase activity, phthalimides also inhibited yeast metabolism at all concentrations analyzed.Grape must containing captan and folpet residues could not be transformed into wine due to stuck fermentation caused by the inhibition of yeast metabolism. Non-compliance with the waiting period for phthalimide fungicides may result in financial liabilities to the viticulture sector.The use of yeasts with high fungicide sensitivity should be selected for must fermentation as a strategy for sustainable wine production and to assure that products comply with health and food safety standards.

Interactions between crop biomass and development of foliar diseases in winter wheat and the potential to graduate the fungicide dose according to crop biomass

DEFF Research Database (Denmark)

Jensen, Peter Kryger; Jørgensen, Lise Nistrup

2016-01-01

dose. The study was carried out investigating fungicide dose response controlling foliar diseases in winter wheat at three biomass densities obtained growing the crop at three nitrogen levels and using variable seed rates. Further the field experiments included three fungicide dose rates at each...... biomass level, an untreated control, and 75%, 50% and 33% of the recommended fungicide dose rate and the experiments were replicated for three years. Crop biomass had a significant influence on occurrence of septoria and yellow rust with greater disease severity at increasing crop biomass. In two of three...... years, the interaction of crop biomass and fungicide dose rate had a significant influence on disease severity indicating a biomassdependent dose response. The interaction occurred in the two years with high yield potential in combination with severe disease attack. If the variation in crop density...

Fungicidal and anti-aflatoxigenic effects of the essential oil of Cymbopogon citratus (DC.) Stapf. (lemongrass) against Aspergillus flavus Link. isolated from stored rice.

Science.gov (United States)

Paranagama, P A; Abeysekera, K H T; Abeywickrama, K; Nugaliyadde, L

2003-01-01

To develop a natural fungicide against aflatoxigenic fungi, to protect stored rice, using the essential oil of lemongrass. Aspergillus flavus Link. was isolated from stored rice and identified as an aflatoxigenic strain. Lemongrass oil was tested against A. flavus and the test oil was fungistatic and fungicidal against the test pathogen at 0.6 and 1.0 mg ml(-1), respectively. Aflatoxin production was completely inhibited at 0.1 mg ml(-1). The results obtained from the thin layer chromatographic bioassay and gas chromatography indicated citral a and b as the fungicidal constituents in lemongrass oil. During the fumigant toxicity assay of lemongrass oil, the sporulation and the mycelial growth of the test pathogen were inhibited at the concentrations of 2.80 and 3.46 mg ml(-1), respectively. Lemongrass oil could be used to manage aflatoxin formation and fungal growth of A. flavus in stored rice. Currently, fungicides are not used to control fungal pests or mycotoxin production on stored rice. Rice treated with the essential oil of lemongrass could be used to manage fungal pests as well as the insect pests in stored rice. The essential oil is chemically safe and acceptable to consumers, as synthetic chemical fungicides can cause adverse health effects to consumers.

Dual-Targeting Small-Molecule Inhibitors of the Staphylococcus aureus FMN Riboswitch Disrupt Riboflavin Homeostasis in an Infectious Setting.

Science.gov (United States)

Wang, Hao; Mann, Paul A; Xiao, Li; Gill, Charles; Galgoci, Andrew M; Howe, John A; Villafania, Artjohn; Barbieri, Christopher M; Malinverni, Juliana C; Sher, Xinwei; Mayhood, Todd; McCurry, Megan D; Murgolo, Nicholas; Flattery, Amy; Mack, Matthias; Roemer, Terry

2017-05-18

Riboswitches are bacterial-specific, broadly conserved, non-coding RNA structural elements that control gene expression of numerous metabolic pathways and transport functions essential for cell growth. As such, riboswitch inhibitors represent a new class of potential antibacterial agents. Recently, we identified ribocil-C, a highly selective inhibitor of the flavin mononucleotide (FMN) riboswitch that controls expression of de novo riboflavin (RF, vitamin B2) biosynthesis in Escherichia coli. Here, we provide a mechanistic characterization of the antibacterial effects of ribocil-C as well as of roseoflavin (RoF), an antimetabolite analog of RF, among medically significant Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus (MRSA) and Enterococcus faecalis. We provide genetic, biophysical, computational, biochemical, and pharmacological evidence that ribocil-C and RoF specifically inhibit dual FMN riboswitches, separately controlling RF biosynthesis and uptake processes essential for MRSA growth and pathogenesis. Such a dual-targeting mechanism is specifically required to develop broad-spectrum Gram-positive antibacterial agents targeting RF metabolism. Copyright © 2017 Elsevier Ltd. All rights reserved.

Biosynthesis of silver nanoparticles synthesized by Aspergillus ...

Indian Academy of Sciences (India)

Biotechnology Division, Applied Science Department, University of ... Abstract. In the present study, biosynthesis of silver nanoparticles and its antioxidant, antimicrobial and cytotoxic ... example of the biosynthesis using fungi was that the cell-.

Evaluation of fungicides for the control of false smut of rice caused ...

African Journals Online (AJOL)

Benomyl, Copper Oxychloride, Iprodione, Thiabendazole (TBZ) and Mancozeb were evaluated both in the laboratory and field study in 1994, for the control of false smut of rice caused by Ustilaginoidea virens (Cooke) Tak. in upland rice in Edo State, Nigeria. In the laboratory the fungicides were evaluated at three ...

Discovery and quantitative structure-activity relationship study of lepidopteran HMG-CoA reductase inhibitors as selective insecticides.

Science.gov (United States)

Zang, Yang-Yang; Li, Yuan-Mei; Yin, Yue; Chen, Shan-Shan; Kai, Zhen-Peng

2017-09-01

In a previous study we have demonstrated that insect 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) can be a potential selective insecticide target. Three series of inhibitors were designed on the basis of the difference in HMGR structures from Homo sapiens and Manduca sexta, with the aim of discovering potent selective insecticide candidates. An in vitro bioassay showed that gem-difluoromethylenated statin analogues have potent effects on JH biosynthesis of M. sexta and high selectivity between H. sapiens and M. sexta. All series II compounds {1,3,5-trisubstituted [4-tert-butyl 2-(5,5-difluoro-2,2-dimethyl-6-vinyl-4-yl) acetate] pyrazoles} have some effect on JH biosynthesis, whereas most of them are inactive on human HMGR. In particular, the IC 50 value of compound II-12 (37.8 nm) is lower than that of lovastatin (99.5 nm) and similar to that of rosuvastatin (24.2 nm). An in vivo bioassay showed that I-1, I-2, I-3 and II-12 are potential selective insecticides, especially for lepidopteran pest control. A predictable and statistically meaningful CoMFA model of 23 inhibitors (20 as training sets and three as test sets) was obtained with a value of q 2 and r 2 of 0.66 and 0.996 respectively. The final model suggested that a potent insect HMGR inhibitor should contain suitable small and non-electronegative groups in the ring part, and electronegative groups in the side chain. Four analogues were discovered as potent selective lepidopteran HMGR inhibitors, which can specifically be used for lepidopteran pest control. The CoMFA model will be useful for the design of new selective insect HMGR inhibitors that are structurally related to the training set compounds. © 2017 Society of Chemical Industry. © 2017 Society of Chemical Industry.

Enzymatic basis for fungicide removal by Elodea canadensis.

Science.gov (United States)

Dosnon-Olette, Rachel; Schröder, Peter; Bartha, Bernadett; Aziz, Aziz; Couderchet, Michel; Eullaffroy, Philippe

2011-07-01

Plants can absorb a diversity of natural and man-made toxic compounds for which they have developed diverse detoxification mechanisms. Plants are able to metabolize and detoxify a wide array of xenobiotics by oxidation, sugar conjugation, glutathione conjugation, and more complex reactions. In this study, detoxification mechanisms of dimethomorph, a fungicide currently found in aquatic media were investigated in Elodea canadensis. Cytochrome P450 (P450) activity was measured by an oxygen biosensor system, glucosyltransferases (GTs) by HPLC, glutathione S-transferases (GSTs), and ascorbate peroxidase (APOX) were assayed spectrophotometrically. Incubation of Elodea with dimethomorph induced an increase of the P450 activity. GST activity was not stimulated by dimethomorph suggesting that GST does not participate in dimethomorph detoxification. In plants exposed to dimethomorph, comparable responses were observed for GST and APOX activities showing that the GST was more likely to play a role in response to oxidative stress. Preincubation with dimethomorph induced a high activity of O- and N-GT, it is therefore likely that both enzymes participate in the phase II (conjugation) of dimethomorph detoxification process. For the first time in aquatic plants, P450 activity was shown to be induced by a fungicide suggesting a role in the metabolization of dimethomorph. Moreover, our finding is the first evidence of dimethomorph and isoproturon activation of cytochrome P450 multienzyme family in an aquatic plant, i.e., Elodea (isoproturon was taken here as a reference molecule). The detoxification of dimetomorph seems to proceed via hydroxylation, and subsequent glucosylation, and might yield soluble as well as cell wall bound residues.

Effects of Fungicide and Adjuvant Sprays on Nesting Behavior in Two Managed Solitary Bees, Osmia lignaria and Megachile rotundata.

Science.gov (United States)

Artz, Derek R; Pitts-Singer, Theresa L

2015-01-01

There is a growing body of empirical evidence showing that wild and managed bees are negatively impacted by various pesticides that are applied in agroecosystems around the world. The lethal and sublethal effects of two widely used fungicides and one adjuvant were assessed in cage studies in California on blue orchard bees, Osmia lignaria, and in cage studies in Utah on alfalfa leafcutting bees, Megachile rotundata. The fungicides tested were Rovral 4F (iprodione) and Pristine (mixture of pyraclostrobin + boscalid), and the adjuvant tested was N-90, a non-ionic wetting agent (90% polyethoxylated nonylphenol) added to certain tank mixtures of fungicides to improve the distribution and contact of sprays to plants. In separate trials, we erected screened cages and released 20 paint-marked females plus 30-50 males per cage to document the behavior of nesting bees under treated and control conditions. For all females in each cage, we recorded pollen-collecting trip times, nest substrate-collecting trip times (i.e., mud for O. lignaria and cut leaf pieces for M. rotundata), cell production rate, and the number of attempts each female made to enter her own or to enter other nest entrances upon returning from a foraging trip. No lethal effects of treatments were observed on adults, nor were there effects on time spent foraging for pollen and nest substrates and on cell production rate. However, Rovral 4F, Pristine, and N-90 disrupted the nest recognition abilities of O. lignaria females. Pristine, N-90, and Pristine + N-90 disrupted nest recognition ability of M. rotundata females. Electroantennogram responses of antennae of O. lignaria females maintained in the laboratory did not differ significantly between the fungicide-exposed and control bees. Our results provide the first empirical evidence that two commonly used fungicides and a non-ionic adjuvant can disrupt nest recognition in two managed solitary bee species.

The regulation and biosynthesis of antimycins

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Ryan F. Seipke

2013-11-01

Full Text Available Antimycins (>40 members were discovered nearly 65 years ago but the discovery of the gene cluster encoding antimycin biosynthesis in 2011 has facilitated rapid progress in understanding the unusual biosynthetic pathway. Antimycin A is widely used as a piscicide in the catfish farming industry and also has potent killing activity against insects, nematodes and fungi. The mode of action of antimycins is to inhibit cytochrome c reductase in the electron transport chain and halt respiration. However, more recently, antimycin A has attracted attention as a potent and selective inhibitor of the mitochondrial anti-apoptotic proteins Bcl-2 and Bcl-xL. Remarkably, this inhibition is independent of the main mode of action of antimycins such that an artificial derivative named 2-methoxyantimycin A inhibits Bcl-xL but does not inhibit respiration. The Bcl-2/Bcl-xL family of proteins are over-produced in cancer cells that are resistant to apoptosis-inducing chemotherapy agents, so antimycins have great potential as anticancer drugs used in combination with existing chemotherapeutics. Here we review what is known about antimycins, the regulation of the ant gene cluster and the unusual biosynthetic pathway.

Revealing fosfomycin primary effect on Staphylococcus aureus transcriptome: modulation of cell envelope biosynthesis and phosphoenolpyruvate induced starvation

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Gruden Kristina

2010-06-01

Full Text Available Abstract Background Staphylococcus aureus is a highly adaptable human pathogen and there is a constant search for effective antibiotics. Fosfomycin is a potent irreversible inhibitor of MurA, an enolpyruvyl transferase that uses phosphoenolpyruvate as substrate. The goal of this study was to identify the pathways and processes primarily affected by fosfomycin at the genome-wide transcriptome level to aid development of new drugs. Results S. aureus ATCC 29213 cells were treated with sub-MIC concentrations of fosfomycin and harvested at 10, 20 and 40 minutes after treatment. S. aureus GeneChip statistical data analysis was complemented by gene set enrichment analysis. A visualization tool for mapping gene expression data into biological pathways was developed in order to identify the metabolic processes affected by fosfomycin. We have shown that the number of significantly differentially expressed genes in treated cultures increased with time and with increasing fosfomycin concentration. The target pathway - peptidoglycan biosynthesis - was upregulated following fosfomycin treatment. Modulation of transport processes, cofactor biosynthesis, energy metabolism and nucleic acid biosynthesis was also observed. Conclusions Several pathways and genes downregulated by fosfomycin have been identified, in contrast to previously described cell wall active antibiotics, and was explained by starvation response induced by phosphoenolpyruvate accumulation. Transcriptomic profiling, in combination with meta-analysis, has been shown to be a valuable tool in determining bacterial response to a specific antibiotic.

Comparative study of the fungicide Benomyl toxicity on some plant growth promoting bacteria and some fungi in pure cultures

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Elslahi Randa H.

2014-03-01

Full Text Available Six laboratory experiments were carried out to investigate the effect of the fungicide Benomyl on pure cultures of some plant growth promoting bacteria (PGPB and some fungi. The highest LD50 was recorded for Bacillus circulans and proved to be the most resistant to the fungicide, followed by Azospirillum braziliense, while Penicillium sp. was the most affected microorganism. LD50 values for the affected microorganisms were in 21-240 orders of magnitude lower in comparison with the LD50 value for Azospirillum braziliense. The results indicate a strong selectivity for Benomyl against Rhizobium meliloti and Penicillium sp. when compared to other microorganisms tested. The highest safety coefficient was recorded for Bacillus circulans followed by Azospirillum braziliense, while Rhizobium meliloti, showed the lowest safety coefficient value compared to other bacteria. The lowest toxicity index was recorded for Bacillus circulans and Azospirillum braziliense. The slope of the curves for Bacillus sp. and Rhizobium meliloti was steeper than that of the other curves, suggesting that even a slight increase of the dose of the fungicide can cause a very strong negative effect. In conclusion, Benomyl could be applied without restriction when using inocula based on growth promoting bacteria such as symbiotic nitrogen fixers (Rhizobium meliloti, non-symbiotic nitrogen fixers (Azospirillum braziliense or potassium solibilizers (Bacillus circulans, given that the fungicide is applied within the range of the recommended field dose.

Comparative study of the fungicide Benomyl toxicity on some plant growth promoting bacteria and some fungi in pure cultures.

Science.gov (United States)

Elslahi, Randa H; Osman, Awad G; Sherif, Ashraf M; Elhussein, Adil A

2014-03-01

Six laboratory experiments were carried out to investigate the effect of the fungicide Benomyl on pure cultures of some plant growth promoting bacteria (PGPB) and some fungi. The highest LD50 was recorded for Bacillus circulans and proved to be the most resistant to the fungicide, followed by Azospirillum braziliense, while Penicillium sp. was the most affected microorganism. LD50 values for the affected microorganisms were in 21-240 orders of magnitude lower in comparison with the LD50 value for Azospirillum braziliense. The results indicate a strong selectivity for Benomyl against Rhizobium meliloti and Penicillium sp. when compared to other microorganisms tested. The highest safety coefficient was recorded for Bacillus circulans followed by Azospirillum braziliense, while Rhizobium meliloti, showed the lowest safety coefficient value compared to other bacteria. The lowest toxicity index was recorded for Bacillus circulans and Azospirillum braziliense. The slope of the curves for Bacillus sp. and Rhizobium meliloti was steeper than that of the other curves, suggesting that even a slight increase of the dose of the fungicide can cause a very strong negative effect. In conclusion, Benomyl could be applied without restriction when using inocula based on growth promoting bacteria such as symbiotic nitrogen fixers (Rhizobium meliloti), non-symbiotic nitrogen fixers (Azospirillum braziliense) or potassium solibilizers (Bacillus circulans), given that the fungicide is applied within the range of the recommended field dose.

Predictive value of cell assays for developmental toxicity and embryotoxicity of conazole fungicides

DEFF Research Database (Denmark)

Sørensen, Karin Dreisig; Taxvig, Camilla; Kjærstad, Mia Birkhøj

2013-01-01

in reasonably good agreement with available in vivo effects. Ketoconazole and epoxiconazole are the most potent embryotoxic compounds, whereas prochloraz belongs to the most potent developmental toxicants. In conclusion, a rough prediction of the ranking of these conazole fungicides for in vivo toxicity data...

Management of resistance to the fungicide fenpropimorph in Erysiphe graminis f.sp tritici

NARCIS (Netherlands)

Engels, A.J.G.

1998-01-01

In the last three decades, plant disease control has become heavily dependent on fungicides. This practice increased yield significantly but had also negative side-effects on the environment. In many countries, integrated control programs have been initiated in order to reduce pesticide use

Combination of Trichoderma harzianum endochitinase and a membrane-affecting fungicide on control of Alternaria leaf spot in transgenic broccoli plants.

Science.gov (United States)

Mora, A; Earle, E D

2001-04-01

Progeny from transgenic broccoli (cv. Green Comet) expressing a Trichoderma harzianum endochitinase gene were used to assess the interaction between endochitinase and the fungicide Bayleton in the control of Alternaria brassicicola. In vitro assays have shown synergistic effects of endochitinase and fungicides on fungal pathogens. Our study examined the in planta effects of endochitinase and Bayleton, individually and in combination. Two month old transgenic and non-transgenic plants were sprayed with ED50 levels of Bayleton and/or inoculated with an A. brassicicola spore suspension. Disease levels in non-sprayed transgenic plants were not statistically different from sprayed transgenic plants nor from sprayed non-transgenic controls. Thus endochitinase-transgenic plants alone provided a significant reduction of disease severity, comparable to the protection by fungicide on non-transgenic plants. Comparison of the expected additive and observed effects revealed no synergism between endochitinase and Bayleton (at ED50 level), and usually less than an additive effect. Some transgenic lines sprayed with fungicide at doses higher than ED50 showed resistance similar to the non-sprayed transgenic lines, again suggesting no synergistic effect. Lack of synergism may be due to incomplete digestion of the cell wall by endochitinase, so that the effect of Bayleton at the cell membrane is not enhanced.

Effects of powdery mildew fungicide programs on twospotted spider mite (Acari: Tetranychidae), hop aphid (Hemiptera: Aphididae), and their natural enemies in hop yards.

Science.gov (United States)

Gent, D H; James, D G; Wright, L C; Brooks, D J; Barbour, J D; Dreves, A J; Fisher, G C; Walton, V M

2009-02-01

Twospotted spider mite, Tetranychus urticae Koch (Acari: Tetranychidae), and hop aphid, Phorodon humuli (Schrank) (Hemiptera: Aphididae), are the most important arthropod pests of hop (Humulus lupulus L.) in the Northern Hemisphere. A potential barrier for greater adoption of conservation biological control strategies for spider mites and hop aphid is the extensive use of fungicides for management of hop powdery mildew, Podosphaera macularis (Wallr.:Fr.) U. Braun & S. Takamatsu. Field studies conducted in experimental plots in Oregon and Washington in 2005 and 2006 quantified the effects of powdery mildew fungicide programs (i.e., sulfur, paraffinic oil, and synthetic fungicides) on arthropod pests and natural enemies on hop. Fungicide treatment significantly affected spider mite populations in all four studies. Multiple applications of sulfur fungicides applied before burr development resulted in 1.4-3.3-fold greater spider mite populations during summer. Near the cessation of the sulfur applications, or after a lag of 20-30 d, spider mite populations increased significantly faster on sulfur treated plants compared with water-treated plants in three of four experiments. The effect of paraffinic oil on spider mites was varied, leading to exacerbation of spider mites in Oregon and Washington in 2005, suppression of mites in Oregon in 2006, and no significant effect compared with water in Washington in 2006. Significant relative treatment effects for cone damage due to spider mite feeding were detected in Oregon in 2005 in plots treated with sulfur and paraffinic oil compared with water and synthetic fungicides. Mean populations of hop aphids were similar among treatments in Oregon, although sulfur treatment suppressed hop aphid populations in Washington in 2005 and 2006. Populations of individual predacious insect species and cumulative abundance of macropredators were not consistently suppressed or stimulated by treatments in all trials. However, predatory mite

The guanylhydrazone CNI-1493: an inhibitor with dual activity against malaria-inhibition of host cell pro-inflammatory cytokine release and parasitic deoxyhypusine synthase.

Science.gov (United States)

Specht, Sabine; Sarite, Salem Ramadan; Hauber, Ilona; Hauber, Joachim; Görbig, Ulf F; Meier, Chris; Bevec, Dorian; Hoerauf, Achim; Kaiser, Annette

2008-05-01

Malaria is still a major cause of death in the tropics. There is an urgent need for new anti-malarial drugs because drug-resistant plasmodia frequently occur. Over recent years, we elucidated the biosynthesis of hypusine, a novel amino acid contained in eukaryotic initiation factor 5A (eIF-5A) in Plasmodium. Hypusine biosynthesis involves catalysis of deoxyhypusine synthase (DHS) in the first step of post-translational modification. In a screen for new inhibitors of purified plasmodium DHS, CNI-1493, a novel selective pro-inflammatory cytokine inhibitor used in clinical phase II for the treatment of Crohn's disease, inhibited the enzyme of the parasite 3-fold at a concentration of 2 microM. In vitro experiments with 200 microM CNI-1493 in Plasmodium-infected erythrocytes, which lack nuclei and DHS protein, showed a parasite clearance within 2 days. This can presumably be attributed to an anti-proliferating effect because of the inhibition of DHS by the parasite. The determined IC50 of CNI-1493 was 135.79 microM after 72 h. In vivo application of this substance in Plasmodium berghei ANKA-infected C57BL/6 mice significantly reduced parasitemia after dosage of 1 mg/kg or 4 mg/kg/body weight and prevented death of mice with cerebral malaria. This effect was paralleled by a decrease in serum TNF levels of the mice. We suggest that the new mechanism of CNI-1493 is caused by a decrease in modified eIF-5A biosynthesis with a downstream effect on the TNF synthesis of the host. From the current data, we consider CNI-1493 to be a promising drug for anti-malarial therapy because of its combined action, i.e., the decrease in eIF-5A biosynthesis of the parasite and host cell TNF biosynthesis.

The influence of particle size and AgNO3 concentration in the ionic exchange process on the fungicidal action of antimicrobial glass

International Nuclear Information System (INIS)

Mendes, E.; Piletti, R.; Barichello, T.; Oliveira, C.M.; Kniess, C.T.; Angioletto, E.; Riella, H.G.

2012-01-01

Antimicrobial materials have long been used as an effective means of reducing the risks posed to humans by fungi, bacteria and other microorganisms. These materials are essential in environments where cleanliness, comfort and hygiene are the predominate concerns. This work presents preliminary results for the development of a fungicidal vitreous material that is produced by the incorporation of a silver ionic specimen through ionic exchange reactions. Silver ions were incorporated into powdered glass via ionic exchange in an ionic medium containing silver species with different concentrations of AgNO 3 . The fungicidal efficiency of the samples was studied as a function of the AgNO 3 concentration and the particle size of the glass using the agar diffusion test for the microbiological analysis of the fungus species Candida albicans. The samples were examined by scanning electron microscopy (SEM), energy dispersive spectroscopy (EDS) and X-ray diffraction (XRD). The experimental results showed that the fungicidal effect was dependent on the AgNO 3 concentration in the ionic exchange medium but was not dependent on the particle size of the glass. - Highlights: ► The fungicidal powder glass presents high potential for application as polymeric additive and others application in the medical area. ► The fungicidal effect was dependent on AgNO3 concentration, but was not dependent on the particle size of the glass. ► The XRD results show that the ionic exchange process promotes the formation of silver crystalline phases with cubic cells.

Photodegradation of multiclass fungicides in the aquatic environment and determination by liquid chromatography-tandem mass spectrometry.

Science.gov (United States)

Celeiro, Maria; Facorro, Rocio; Dagnac, Thierry; Vilar, Vítor J P; Llompart, Maria

2017-08-01

The photodegradation behaviour for nine widespread fungicides (benalaxyl, cyprodinil, dimethomorph, fenhexamide, iprovalicarb, kresoxim-methyl, metalaxyl, myclobutanil and tebuconazole) was evaluated in different types of water. Two different systems, direct UV photolysis and UVC/H 2 O 2 advanced oxidation process (AOP), were applied for the photodegradation tests. For the monitoring of the target compound degradation, a method based on direct injection liquid chromatography-tandem mass spectrometry (LC-MS/MS) was developed. Several fungicide photodegradation by-products were tentatively identified by high-resolution mass spectrometry (HRMS) as well. For the photolysis studies, the efficiency of different types of radiation, UVC (λ = 254 nm) and UVA (λ = 365 nm), was compared. UVC photolysis provided the highest removal with a complete degradation for fenhexamide and kresoxim-methyl, and percentages between 48 and 78% for the other compounds, excluding iprovalicarb and myclobutanil with removals <35%, after 30 min of irradiation. Besides, the photodegradation tests were performed with different initial concentrations of fungicides, and the efficiency of two photoreactor systems was compared. In all cases, the kinetics followed pseudo-first order, and the half-life times could also be calculated. The addition of H 2 O 2 under UVC light allowed an improvement of the reaction kinetics, especially for the most recalcitrant fungicides, obtaining in all cases removals higher than 82% in less than 6 min. Finally, in order to evaluate the suitability of the proposed systems, both UVC photolysis and UVC/H 2 O 2 system were tested in different real water matrices (wastewater, tap water, swimming pool water and river water), showing that the UVC/H 2 O 2 system had the highest removal efficiency in less than 6 min, for all water samples.

Genome wide association mapping for the tolerance to the polyamine oxidase inhibitor guazatine in Arabidopsis thaliana

Directory of Open Access Journals (Sweden)

Kostadin Evgeniev eAtanasov

2016-04-01

Full Text Available Guazatine is a potent inhibitor of polyamine oxidase (PAO activity. In agriculture, guazatine is used as non-systemic contact fungicide efficient in the protection of cereals and citrus fruits against disease. The composition of guazatine is complex, mainly constituted by a mixture of synthetic guanidated polyamines (polyaminoguanidines. Here we have studied the effects from exposure to guazatine in the weed Arabidopsis thaliana. We report that micromolar concentrations of guazatine are sufficient to inhibit growth of Arabidopsis seedlings and induce chlorosis, whereas germination is barely affected. We observed the occurrence of quantitative variation in the response to guazatine between 107 randomly chosen Arabidopsis accessions. This enabled us to undertake genome-wide association (GWA mapping that identified a locus on chromosome one associated with guazatine tolerance. CHLOROPHYLLASE 1 (CLH1 within this locus was studied as candidate gene, together with its paralog (CLH2. The analysis of independent clh1-2, clh1-3, clh2-3, clh2-2 and double clh1-2 clh2-3 mutant alleles indicated that CLH1 and/or CLH2 loss-of-function or expression down-regulation promote guazatine tolerance in Arabidopsis. We report a natural mechanism by which Arabidopsis populations can overcome toxicity by the fungicide guazatine.

Design and Synthesis of New Peptidomimetics as Potential Inhibitors of MurE.

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Zivec, Matej; Turk, Samo; Blanot, Didier; Gobec, Stanislav

2011-03-01

With the continuing emergence and spread of multidrug-resistant bacteria, there is an urgent need for the development of new antimicrobial agents. One possible source of new antibacterial targets is the biosynthesis of the bacterial cell-wall peptidoglycan. The assembly of the peptide stem is carried out by four essential enzymes, known as the Mur ligases (MurC, D, E and F). We have designed and synthesised a focused library of compounds as potential inhibitors of UDP-N-acetylmuramoyl-L-alanyl-D-glutamate:L-lysine ligase (MurE) from Staphylococcus aureus. This was achieved using two approaches: (i) synthesis of transition-state analogues based on the methyleneamino core; and (ii) synthesis of MurE reaction product analogues. Two methyleneamino-based compounds are identified as initial hits for inhibitors of MurE.

Amelioration of irradiation injury to Florida grapefruit by pretreatment with vapor heat or fungicides

International Nuclear Information System (INIS)

Miller, W.R.; McDonald, R.E.

1998-01-01

Grapefruit shipped to certain markets must be certified free of Caribbean fruit fly (Anastrepha suspensa Loew) (CFF) infestation. Low-dose irradiation is effective for the control of CFF by sterilization. This treatment is expected to be approved for industry usage in the near future. 'Marsh' grapefruit (Citrus paradisi Macf.) was treated with vapor heat (2 hours at 38 degrees C), and fungicidal treatments of thiabendazole (TBZ) (4 gm.L-1) and TBZ (1 gm.L-1) plus imazalil (1 gm.L-1) prior to irradiation at 0.5 or 1.0 kGy. Vapor heat reduced the severity and incidence of peel injury by approximately 50% without adversely affecting other quality attributes. The fungicide did not reduce peel injury. The use of vapor heat before low-dose irradiation quarantine treatment of grapefruit may ameliorate or eliminate peel injury caused by irradiation

Effect of fungicide on the development of wheat stem rust and yield ...

African Journals Online (AJOL)

Stem rust caused by Puccinia graminis f.sp tritici Erik. & E. Henn. is a highly destructive disease of wheat (Triticum aestivum L.). The effects of fungicide application on stem rust (Puccinia graminis tritici) epidemics and yield of three bread wheat varieties varying in reaction to the disease were studied in two major wheat ...

Evaluation of fungicidal and fungistatic activity of plant essential oils towards plant pathogenic and saprophytic fungi

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Zia BANIHASHEMI

2011-09-01

Full Text Available   The contact and vapor effects of essential oils from different plants were studied in vitro for fungicidal and fungistatic activity towards different Basidiomycete, Ascomycete, Zygomycete and Oomycete taxa. Of nine essential oils tested, most were fungicidal at very low concentrations to most of the fungi. Hyphae were more sensitive than spores to the formulations. The essential oils citral, β-citronellol, geraniol and oil of lavender, at 1 μL mL-1 medium or 12 μL L-1 of air, inhibited growth and germination in the fungal species examined. Different species of fungal genera reacted differently to the formulations. Some of the formulations were fungistatic to spore germination.

Fungicidal seed coatings exert minor effects on arbuscular mycorrhizal fungi and plant nutrient content

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Aims: Determine if contemporary, seed-applied fungicidal formulations inhibit colonization of plant roots by arbuscular mycorrhizal (AM) fungi, plant development, or plant nutrient content during early vegetative stages of several commodity crops. Methods: We evaluated seed-applied commercial fungic...

Fungicidal control of Lophodermium seditiosum on Pinus sylvestris seedlings in Swedish forest nurseries

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Stenstroem, Elna [Swedish Univ. of Agricultural Sciences, Uppsala (Sweden). Dept. of Forest Mycology and Pathology; Arvidsson, Bernt [Svenska Skogsplantor AB, Joenkoeping (Sweden)

2001-07-01

During the 1990s, there were serious outbreaks of the pathogen Lophodermium seditiosum on pine seedlings in Swedish forest nurseries, even though the seedlings had been treated with the fungicide propiconazole. The present experiment was carried out to evaluate two other fungicides, fluazinam and azoxystrobin, as possible alternatives to propiconazole. In the tests, which were all carried out in the same forest nursery, seedlings were treated with either propiconazole, fluazinam. or azoxystrobin, and the proportion of needles with ascocarps of L. seditiosum and the number of ascocarps per needle were recorded over the following 2 yrs. Seedlings treated with azoxystrobin already appeared healthier than control seedlings in September of the first year, and by November all azoxystrobin-treated seedlings had fewer ascocarps per needle compared with control seedlings. In autumn of the second year, there were no ascocarps on seedlings treated with fluazinam or azoxystrobin, whereas seedlings treated with propiconazole had similar numbers of ascocarps to non-treated control seedlings.

FLO11 expression and lipid biosynthesis are required for air-liquid biofilm formation in a Saccharomyces cerevisiae flor strain.

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Zara, Giacomo; Goffrini, Paola; Lodi, Tiziana; Zara, Severino; Mannazzu, Ilaria; Budroni, Marilena

2012-11-01

Air-liquid biofilm formation is largely dependent on Flo11p and seems related to cell lipid content and composition. Here, it is shown that in the presence of cerulenin, a known inhibitor of the fatty acid synthase complex, biofilm formation is inhibited together with FLO11 transcription in a flor strain of Saccharomyces cerevisiae, while the administration of saturated fatty acids to cerulenin-containing medium restores biofilm formation and FLO11 transcription. It is also shown that, in biofilm cells, the FLO11 transcription is accompanied by the transcription of ACC1, ACS1 and INO1 key genes in lipid biosynthesis and that biofilm formation is affected by the lack of inositol in flor medium. These results are compatible with the hypothesis that the air-liquid biofilm formation depends on FLO11 transcription levels as well as on fatty acids biosynthesis. © 2012 Federation of European Microbiological Societies. Published by Blackwell Publishing Ltd. All rights reserved.

Methyl Salicylate-Based Vortex-Assisted Surfactant-Enhanced Emulsification Microextraction and HPLC for Determination of Fungicides in Honey Samples.

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Santaladchaiyakit, Yanawath; Bunchamnan, Jutamas; Tongsa, Darunee; Srijaranai, Supalax

2017-12-01

Methyl salicylate based vortex-assisted surfactant-enhanced emulsification microextraction (MeSA-VASEME) has been developed and applied for rapid preconcentration of fungicides (i.e., carbendazim, thiabendazole, and fluberidazole) in honey samples followed by high performance liquid chromatographic analysis. MeSA was used as an extraction solvent, while surfactant was used to enhance the extraction performance under the dispersion by vortex agitation. The optimum MeSA-VASEME conditions were 100 μL MeSA, 2.0 mmol L‒1 sodium dodecyl sulfate, and vortex agitation at 1200 rpm for 90 s. Preconcentration factors were obtained in the range of 32-40. The limit of detection in the studied honey samples was 0.5 μg L‒1. The recovery of the spiked target fungicides at 20, 50, and 100 μg L‒1 were 81.5-116.8 % with the relative standard deviation below 11%. The proposed method is simple, sensitive, less organic solvent consuming, inexpensive, and a rapid procedure for the residue analysis of fungicides in honey samples.

A porphodimethene chemical inhibitor of uroporphyrinogen decarboxylase.

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Kenneth W Yip

Full Text Available Uroporphyrinogen decarboxylase (UROD catalyzes the conversion of uroporphyrinogen to coproporphyrinogen during heme biosynthesis. This enzyme was recently identified as a potential anticancer target; its inhibition leads to an increase in reactive oxygen species, likely mediated by the Fenton reaction, thereby decreasing cancer cell viability and working in cooperation with radiation and/or cisplatin. Because there is no known chemical UROD inhibitor suitable for use in translational studies, we aimed to design, synthesize, and characterize such a compound. Initial in silico-based design and docking analyses identified a potential porphyrin analogue that was subsequently synthesized. This species, a porphodimethene (named PI-16, was found to inhibit UROD in an enzymatic assay (IC50 = 9.9 µM, but did not affect porphobilinogen deaminase (at 62.5 µM, thereby exhibiting specificity. In cellular assays, PI-16 reduced the viability of FaDu and ME-180 cancer cells with half maximal effective concentrations of 22.7 µM and 26.9 µM, respectively, and only minimally affected normal oral epithelial (NOE cells. PI-16 also combined effectively with radiation and cisplatin, with potent synergy being observed in the case of cisplatin in FaDu cells (Chou-Talalay combination index <1. This work presents the first known synthetic UROD inhibitor, and sets the foundation for the design, synthesis, and characterization of higher affinity and more effective UROD inhibitors.

Inhibitors of polyamine metabolism: review article.

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Wallace, H M; Fraser, A V

2004-07-01

The identification of increased polyamine concentrations in a variety of diseases from cancer and psoriasis to parasitic infections has led to the hypothesis that manipulation of polyamine metabolism is a realistic target for therapeutic or preventative intervention in the treatment of certain diseases. The early development of polyamine biosynthetic single enzyme inhibitors such as alpha-difluoromethylornithine (DFMO) and methylglyoxal bis(guanylhydrazone) showed some interesting early promise as anticancer drugs, but ultimately failed in vivo. Despite this, DFMO is currently in use as an effective anti-parasitic agent and has recently also been shown to have further potential as a chemopreventative agent in colorectal cancer. The initial promise in vitro led to the development and testing of other potential inhibitors of the pathway namely the polyamine analogues. The analogues have met with greater success than the single enzyme inhibitors possibly due to their multiple targets. These include down regulation of polyamine biosynthesis through inhibition of ornithine decarboxylase and S-adenosylmethionine decarboxylase and decreased polyamine uptake. This coupled with increased activity of the catabolic enzymes, polyamine oxidase and spermidine/spermine N1-acetyltransferase, and increased polyamine export has made the analogues more effective in depleting polyamine pools. Recently, the identification of a new oxidase (PAO-h1/SMO) in polyamine catabolism and evidence of induction of both PAO and PAO-h1/SMO in response to polyamine analogue treatment, suggests the analogues may become an important part of future chemotherapeutic and/or chemopreventative regimens.

Action of mercury as a soil fungicide

Energy Technology Data Exchange (ETDEWEB)

Booer, J R

1951-01-01

Metallic mercury and mercury compounds in the soil retard the growth of plants. The development of mosses and lichens is inhibited, and experimental evidence shows that the growth of toadstools on turf and the activity of ascomycetes is retarded by mercury. In vitro, mercury has no fungicidal action but the rate of growth of hyphae is reduced by mercury vapour. The lack of fungicial properties of mercury and its good performance in controlling certain soil-borne diseases are reconciled by assuming that a differential retardation disturbs the relationships necessary for infection. This assumption is supported by diagrams which treat the rates of growth of the parasite and the host as population characteristics normally distributed. 21 references, 10 figures, 5 tables.

A comparative modeling and molecular docking study on Mycobacterium tuberculosis targets involved in peptidoglycan biosynthesis.

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Fakhar, Zeynab; Naiker, Suhashni; Alves, Claudio N; Govender, Thavendran; Maguire, Glenn E M; Lameira, Jeronimo; Lamichhane, Gyanu; Kruger, Hendrik G; Honarparvar, Bahareh

2016-11-01

An alarming rise of multidrug-resistant Mycobacterium tuberculosis strains and the continuous high global morbidity of tuberculosis have reinvigorated the need to identify novel targets to combat the disease. The enzymes that catalyze the biosynthesis of peptidoglycan in M. tuberculosis are essential and noteworthy therapeutic targets. In this study, the biochemical function and homology modeling of MurI, MurG, MraY, DapE, DapA, Alr, and Ddl enzymes of the CDC1551 M. tuberculosis strain involved in the biosynthesis of peptidoglycan cell wall are reported. Generation of the 3D structures was achieved with Modeller 9.13. To assess the structural quality of the obtained homology modeled targets, the models were validated using PROCHECK, PDBsum, QMEAN, and ERRAT scores. Molecular dynamics simulations were performed to calculate root mean square deviation (RMSD) and radius of gyration (Rg) of MurI and MurG target proteins and their corresponding templates. For further model validation, RMSD and Rg for selected targets/templates were investigated to compare the close proximity of their dynamic behavior in terms of protein stability and average distances. To identify the potential binding mode required for molecular docking, binding site information of all modeled targets was obtained using two prediction algorithms. A docking study was performed for MurI to determine the potential mode of interaction between the inhibitor and the active site residues. This study presents the first accounts of the 3D structural information for the selected M. tuberculosis targets involved in peptidoglycan biosynthesis.

Extracellular biosynthesis of silver nanoparticles using Bacillus sp. GP-23 and evaluation of their antifungal activity towards Fusarium oxysporum

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Gopinath, V.; Velusamy, P.

2013-04-01

In last few decades nanoparticles have attracted and emerged as a field in biomedical research due to their incredible applications. The current research was focused on extracellular synthesis of silver nanoparticles (AgNPs) using cell free culture supernatant of strain GP-23. It was found that the strain GP-23 belonged to Bacillus species by 16S rRNA sequence analysis. Biosynthesis of AgNPs was achieved by addition of culture supernatant with aqueous silver nitrate solution, after 24 h it turned to brown color solution with a peak at 420 nm corresponding to the Plasmon absorbance of AgNPs by UV-Vis Spectroscopy. The nanoparticles were characterized by FTIR, XRD, HRTEM, EDX and AFM. The synthesized nanoparticles were found to be spherical in shape with size in the range of 7-21 nm. It was stable in aqueous solution for five months period of storage at room temperature under dark condition. The biosynthesized AgNPs exhibited strong antifungal activity against plant pathogenic fungus, Fusarium oxysporum at the concentration of 8 μg ml-1. The results suggest that the synthesized AgNPs act as an effective antifungal agent/fungicide.

In vitro metabolism of the anti-androgenic fungicide vinclozolin by rat liver microsomes

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Vinclozolin (V) is a fungicide used in agricultural settings. V administered to rats is hydrolyzed to 2-[[(3,5-dichlorophenyl)-carbamoyl]oxy]-2-methyl-3-butenoic acid (Ml) and 3',5'-dichloro-2-hydroxy-2-methylbut-3-enanilide (M2). V, Ml and M2 have antiandrogenic properties by in...

Modeling the influence of raindrop size on the wash-off losses of copper-based fungicides sprayed on potato (Solanum tuberosum L.) leaves.

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Pérez-Rodríguez, Paula; Paradelo, Marcos; Rodríguez-Salgado, Isabel; Fernández-Calviño, David; López-Periago, José Eugenio

2013-01-01

Modeling the pesticide wash-off by raindrops is important for predicting pesticide losses and the subsequent transport of pesticides to soil and in soil run-off. Three foliar-applied copper-based fungicide formulations, specifically the Bordeaux mixture (BM), copper oxychloride (CO), and a mixture of copper oxychloride and propylene glycol (CO-PG), were tested on potato (Solanum tuberosum L.) leaves using a laboratory raindrop simulator. The losses in the wash-off were quantified as both copper in-solution loss and copper as particles detached by the raindrops. The efficiency of the raindrop impact on the wash-off was modeled using a stochastic model based on the pesticide release by raindrops. In addition, the influence of the raindrop size, drop falling height, and fungicide dose was analyzed using a full factorial experimental design. The average losses per dose after 14 mm of dripped water for a crop with a leaf area index equal to 1 were 0.08 kg Cu ha(-1) (BM), 0.3 kg Cu ha(-1) (CO) and 0.47 kg Cu ha(-1) (CO-PG). The stochastic model was able to simulate the time course of the wash-off losses and to estimate the losses of both Cu in solution and as particles by the raindrop impacts. For the Cu-oxychloride fungicides, the majority of the Cu was lost as particles that detached from the potato leaves. The percentage of Cu lost increased with the decreasing raindrop size in the three fungicides for the same amount of dripped water. This result suggested that the impact energy is not a limiting factor in the particle detachment rate of high doses. The dosage of the fungicide was the most influential factor in the losses of Cu for the three formulations studied. The results allowed us to quantify the factors that should be considered when estimating the losses by the wash-off of copper-based fungicides and the inputs of copper to the soil by raindrop wash-off.

Contamination of apple orchard soils and fruit trees with copper-based fungicides: sampling aspects.

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Wang, Quanying; Liu, Jingshuang; Liu, Qiang

2015-01-01

Accumulations of copper in orchard soils and fruit trees due to the application of Cu-based fungicides have become research hotspots. However, information about the sampling strategies, which can affect the accuracy of the following research results, is lacking. This study aimed to determine some sampling considerations when Cu accumulations in the soils and fruit trees of apple orchards are studied. The study was conducted in three apple orchards from different sites. Each orchard included two different histories of Cu-based fungicides usage, varying from 3 to 28 years. Soil samples were collected from different locations varying with the distances from tree trunk to the canopy drip line. Fruits and leaves from the middle heights of tree canopy at two locations (outer canopy and inner canopy) were collected. The variation in total soil Cu concentrations between orchards was much greater than the variation within orchards. Total soil Cu concentrations had a tendency to increase with the increasing history of Cu-based fungicides usage. Moreover, total soil Cu concentrations had the lowest values at the canopy drip line, while the highest values were found at the half distances between the trunk and the canopy drip line. Additionally, Cu concentrations of leaves and fruits from the outer parts of the canopy were significantly higher than from the inner parts. Depending on the findings of this study, not only the between-orchard variation but also the within-orchard variation should be taken into consideration when conducting future soil and tree samplings in apple orchards.

Jasmonate-induced biosynthesis of andrographolide in Andrographis paniculata.

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Sharma, Shiv Narayan; Jha, Zenu; Sinha, Rakesh Kumar; Geda, Arvind Kumar

2015-02-01

Andrographolide is a prominent secondary metabolite found in Andrographis paniculata that exhibits enormous pharmacological effects. In spite of immense value, the normal biosynthesis of andrographolide results in low amount of the metabolite. To induce the biosynthesis of andrographolide, we attempted elicitor-induced activation of andrographolide biosynthesis in cell cultures of A. paniculata. This was carried out by using methyl jasmonate (MeJA) as an elicitor. Among the various concentrations of MeJA tested at different time periods, 5 µM MeJA yielded 5.25 times more andrographolide content after 24 h of treatment. The accumulation of andrographolide was correlated with the expression level of known regulatory genes (hmgs, hmgr, dxs, dxr, isph and ggps) of mevalonic acid (MVA) and 2-C-methyl-d-erythritol-4-phosphate (MEP) pathways. These results established the involvement of MeJA in andrographolide biosynthesis by inducing the transcription of its biosynthetic pathways genes. The coordination of isph, ggps and hmgs expression highly influenced the andrographolide biosynthesis. © 2014 Scandinavian Plant Physiology Society.

Effects of Fungicide and Adjuvant Sprays on Nesting Behavior in Two Managed Solitary Bees, Osmia lignaria and Megachile rotundata.

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Derek R Artz

Full Text Available There is a growing body of empirical evidence showing that wild and managed bees are negatively impacted by various pesticides that are applied in agroecosystems around the world. The lethal and sublethal effects of two widely used fungicides and one adjuvant were assessed in cage studies in California on blue orchard bees, Osmia lignaria, and in cage studies in Utah on alfalfa leafcutting bees, Megachile rotundata. The fungicides tested were Rovral 4F (iprodione and Pristine (mixture of pyraclostrobin + boscalid, and the adjuvant tested was N-90, a non-ionic wetting agent (90% polyethoxylated nonylphenol added to certain tank mixtures of fungicides to improve the distribution and contact of sprays to plants. In separate trials, we erected screened cages and released 20 paint-marked females plus 30-50 males per cage to document the behavior of nesting bees under treated and control conditions. For all females in each cage, we recorded pollen-collecting trip times, nest substrate-collecting trip times (i.e., mud for O. lignaria and cut leaf pieces for M. rotundata, cell production rate, and the number of attempts each female made to enter her own or to enter other nest entrances upon returning from a foraging trip. No lethal effects of treatments were observed on adults, nor were there effects on time spent foraging for pollen and nest substrates and on cell production rate. However, Rovral 4F, Pristine, and N-90 disrupted the nest recognition abilities of O. lignaria females. Pristine, N-90, and Pristine + N-90 disrupted nest recognition ability of M. rotundata females. Electroantennogram responses of antennae of O. lignaria females maintained in the laboratory did not differ significantly between the fungicide-exposed and control bees. Our results provide the first empirical evidence that two commonly used fungicides and a non-ionic adjuvant can disrupt nest recognition in two managed solitary bee species.

QSAR study on the antimalarial activity of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors.

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Hou, X; Chen, X; Zhang, M; Yan, A

2016-01-01

Plasmodium falciparum, the most fatal parasite that causes malaria, is responsible for over one million deaths per year. P. falciparum dihydroorotate dehydrogenase (PfDHODH) has been validated as a promising drug development target for antimalarial therapy since it catalyzes the rate-limiting step for DNA and RNA biosynthesis. In this study, we investigated the quantitative structure-activity relationships (QSAR) of the antimalarial activity of PfDHODH inhibitors by generating four computational models using a multilinear regression (MLR) and a support vector machine (SVM) based on a dataset of 255 PfDHODH inhibitors. All the models display good prediction quality with a leave-one-out q(2) >0.66, a correlation coefficient (r) >0.85 on both training sets and test sets, and a mean square error (MSE) antimalarial activity. The models are capable of predicting inhibitors' antimalarial activity and the molecular descriptors for building the models could be helpful in the development of new antimalarial drugs.

Cummulative and antagonistic effects of a mixture of the antiandrogrens vinclozolin and iprodione in the pubertal male rat:

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Vinclozolin and iprodione are dicarboximide fungicides that display anti-androgenic effects in the male rat, which suggests co-exposure to these fungicides would lead to cumulative effects on androgen-sensitive endpoints. Iprodione is a steroid synthesis inhibitor, but AR antagon...

Sensitivities of baseline isolates and boscalid-resistant mutants of Alternaria alternata from pistachio to fluopyram, penthiopyrad, and fluxapyroxad

NARCIS (Netherlands)

Avenot, H.F.; Biggelaar, van den H.; Morgan, D.P.; Moral, J.; Joosten, M.H.A.J.; Michailides, T.J.

2014-01-01

Resistance of Alternaria alternata to boscalid, the first succinate dehydrogenase inhibitor (SDHI) fungicide labeled on pistachio, has become a common occurrence in California pistachio orchards and affects the performance of this fungicide. In this study, we established the baseline sensitivities

Comparisons of Prostate Cancer Inhibitors Abiraterone and TOK-001 Binding with CYP17A1 through Molecular Dynamics.

Science.gov (United States)

Xiao, Fei; Yang, Maohua; Xu, Youjun; Vongsangnak, Wanwipa

2015-01-01

Cytochrome P450 17A1 (CYP17A1) is associated in the steroid hormone biosynthesis in human. As cell proliferation of prostate cancer in response to androgen steroid, an inhibition of CYP17A1 becomes an alternative approach to inhibit biosynthesis of androgen and support treatment of prostate cancer. However, biology-driven inhibitor development of prostate cancer is poorly elucidated. The aims of this study are to address structural differences at atomic-level between CYP17A1 and inhibitors i.e., abiraterone and TOK-001, and further investigate the effect of point mutation of CYP17A1 on the active site stability and the local interactions that are hydrophobic interaction and hydrogen bonding throughout molecular dynamics (MD) simulation. After performing multiple comparisons among four different complexes across CYP17A1 and inhibitors, interestingly TOK-001 oriented toward the active pocket and formed larger volume with I-helix of CYP17A1 than abiraterone, whereas abiraterone showed tighter binding and more active site stability. Considering on the effect of hydrophobic interaction and hydrogen bonding between abiraterone and CYP17A1, the key residues of Phe114, Ile371, Val482, and Asn202 were identified. This contributes into tight binding interactions; however abiraterone is effectively weakened along with the global conformation mobility increased in A105L mutation. Surprisingly, overall conformation of the CYP17A1 remained stable when bound to TOK-001. This basic knowledge can guide future experiments on design of efficient inhibitors for CYP17A1, which provides theoretical basis of androgen-dependent disease therapy.

Endogenous sterol biosynthesis is important for mitochondrial function and cell morphology in procyclic forms of Trypanosoma brucei.

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Pérez-Moreno, Guiomar; Sealey-Cardona, Marco; Rodrigues-Poveda, Carlos; Gelb, Michael H; Ruiz-Pérez, Luis Miguel; Castillo-Acosta, Víctor; Urbina, Julio A; González-Pacanowska, Dolores

2012-10-01

Sterol biosynthesis inhibitors are promising entities for the treatment of trypanosomal diseases. Insect forms of Trypanosoma brucei, the causative agent of sleeping sickness, synthesize ergosterol and other 24-alkylated sterols, yet also incorporate cholesterol from the medium. While sterol function has been investigated by pharmacological manipulation of sterol biosynthesis, molecular mechanisms by which endogenous sterols influence cellular processes remain largely unknown in trypanosomes. Here we analyse by RNA interference, the effects of a perturbation of three specific steps of endogenous sterol biosynthesis in order to dissect the role of specific intermediates in proliferation, mitochondrial function and cellular morphology in procyclic cells. A decrease in the levels of squalene synthase and squalene epoxidase resulted in a depletion of cellular sterol intermediates and end products, impaired cell growth and led to aberrant morphologies, DNA fragmentation and a profound modification of mitochondrial structure and function. In contrast, cells deficient in sterol methyl transferase, the enzyme involved in 24-alkylation, exhibited a normal growth phenotype in spite of a complete abolition of the synthesis and content of 24-alkyl sterols. Thus, the data provided indicates that while the depletion of squalene and post-squalene endogenous sterol metabolites results in profound cellular defects, bulk 24-alkyl sterols are not strictly required to support growth in insect forms of T. brucei in vitro. Copyright © 2012 Australian Society for Parasitology Inc. Published by Elsevier Ltd. All rights reserved.

The role of peroxisomal fatty acyl-CoA beta-oxidation in bile acid biosynthesis

International Nuclear Information System (INIS)

Hayashi, H.; Miwa, A.

1989-01-01

The physiological role of the peroxisomal fatty acyl-CoA beta-oxidizing system (FAOS) is not yet established. We speculated that there might be a relationship between peroxisomal degradation of long-chain fatty acids in the liver and the biosynthesis of bile acids. This was investigated using [1- 14 C]butyric acid and [1- 14 C]lignoceric acid as substrates of FAOS in mitochondria and peroxisomes, respectively. The incorporation of [ 14 C]lignoceric acid into primary bile acids was approximately four times higher than that of [ 14 C]butyric acid (in terms of C-2 units). The pools of these two fatty acids in the liver were exceedingly small. The incorporations of radioactivity into the primary bile acids were strongly inhibited by administration of aminotriazole, which is a specific inhibitor of peroxisomal FAOS in vivo. Aminotriazole inhibited preferentially the formation of cholate, the major primary bile acid, from both [ 14 C]lignoceric acid and [ 14 C]butyric acid, rather than the formation of chenodeoxycholate. The former inhibition was about 70% and the latter was approximately 40-50%. In view of reports that cholate is biosynthesized from endogenous cholesterol, the above results indicate that peroxisomal FAOS may have an anabolic function, supplying acetyl CoA for bile acid biosynthesis

The role of peroxisomal fatty acyl-CoA beta-oxidation in bile acid biosynthesis

Energy Technology Data Exchange (ETDEWEB)

Hayashi, H.; Miwa, A. (Josai Univ., Saitama (Japan))

1989-11-01

The physiological role of the peroxisomal fatty acyl-CoA beta-oxidizing system (FAOS) is not yet established. We speculated that there might be a relationship between peroxisomal degradation of long-chain fatty acids in the liver and the biosynthesis of bile acids. This was investigated using (1-{sup 14}C)butyric acid and (1-{sup 14}C)lignoceric acid as substrates of FAOS in mitochondria and peroxisomes, respectively. The incorporation of ({sup 14}C)lignoceric acid into primary bile acids was approximately four times higher than that of ({sup 14}C)butyric acid (in terms of C-2 units). The pools of these two fatty acids in the liver were exceedingly small. The incorporations of radioactivity into the primary bile acids were strongly inhibited by administration of aminotriazole, which is a specific inhibitor of peroxisomal FAOS in vivo. Aminotriazole inhibited preferentially the formation of cholate, the major primary bile acid, from both ({sup 14}C)lignoceric acid and ({sup 14}C)butyric acid, rather than the formation of chenodeoxycholate. The former inhibition was about 70% and the latter was approximately 40-50%. In view of reports that cholate is biosynthesized from endogenous cholesterol, the above results indicate that peroxisomal FAOS may have an anabolic function, supplying acetyl CoA for bile acid biosynthesis.

Tomato strigolactones are derived from carotenoids and their biosynthesis is promoted by phosphate starvation.

Science.gov (United States)

López-Ráez, Juan Antonio; Charnikhova, Tatsiana; Gómez-Roldán, Victoria; Matusova, Radoslava; Kohlen, Wouter; De Vos, Ric; Verstappen, Francel; Puech-Pages, Virginie; Bécard, Guillaume; Mulder, Patrick; Bouwmeester, Harro

2008-01-01

* Strigolactones are rhizosphere signalling compounds that mediate host location in arbuscular mycorrhizal (AM) fungi and parasitic plants. Here, the regulation of the biosynthesis of strigolactones is studied in tomato (Solanum lycopersicum). * Strigolactone production under phosphate starvation, in the presence of the carotenoid biosynthesis inhibitor fluridone and in the abscisic acid (ABA) mutant notabilis were assessed using a germination bioassay with seeds of Orobanche ramosa; a hyphal branching assay with Gigaspora spp; and by liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) analysis. * The root exudates of tomato cv. MoneyMaker induced O. ramosa seed germination and hyphal branching in AM fungi. Phosphate starvation markedly increased, and fluridone strongly decreased, this activity. Exudates of notabilis induced approx. 40% less germination than the wild-type. The LC-MS/MS analysis confirmed that the biological activity and changes therein were due to the presence of several strigolactones; orobanchol, solanacol and two or three didehydro-orobanchol isomers. * These results show that the AM branching factors and parasitic plant germination stimulants in tomato root exudate are strigolactones and that they are biosynthetically derived from carotenoids. The dual activity of these signalling compounds in attracting beneficial AM fungi and detrimental parasitic plants is further strengthened by environmental conditions such as phosphate availability.

Influence of light, UV-B radiation, and herbicides on wax biosynthesis of cucumber seedlings

International Nuclear Information System (INIS)

Tevini, M.; Steinmüller, D.

1987-01-01

The behavior of cuticular alkane-1-ols and alkanes were studied in different developmental stages of cucumber seedlings grown in the dark or under white light, with or without UV-B radiation or in presence of wax biosynthesis inhibitors, trichloroacetic acid and metolachlor. Accumulation of alkane-1-ols increased light independently with seedling age. Synthesis of alkanes was strictly light and dose dependent. Addition of UV-B radiation did not alter the amounts of alkanes or alcohols, however, the distribution of homologues was shifted towards shorter chain homologues. Treatments with Cl 3 AcOH resulted in strong inhibition of alkane accumulation, whereas the amount of alkane-1-ols was changed neither at low nor at moderate concentrations of Cl 3 AcOH but their homologue distribution shifted towards longer chain lengths. This shifting was depressed in the presence of UV-B. At high concentrations of Cl 3 Ac0H similar homologue distributions as produced by UV-B (shift to shorter homologues) were observed. Metolachlor treatment resulted in an inhibition of alkane-1-ol production connected with rising amounts of alkanes, predominantly of short chain species. A simple model of wax biosynthesis is proposed which describes the interactions with white light, UV-B radiation and herbicides. (author)

Inhibition of the Flavin-Dependent Monooxygenase Siderophore A (SidA) Blocks Siderophore Biosynthesis and Aspergillus fumigatus Growth.

Science.gov (United States)

Martín Del Campo, Julia S; Vogelaar, Nancy; Tolani, Karishma; Kizjakina, Karina; Harich, Kim; Sobrado, Pablo

2016-11-18

Aspergillus fumigatus is an opportunistic fungal pathogen and the most common causative agent of fatal invasive mycoses. The flavin-dependent monooxygenase siderophore A (SidA) catalyzes the oxygen and NADPH dependent hydroxylation of l-ornithine (l-Orn) to N 5 -l-hydroxyornithine in the biosynthetic pathway of hydroxamate-containing siderophores in A. fumigatus. Deletion of the gene that codes for SidA has shown that it is essential in establishing infection in mice models. Here, a fluorescence polarization high-throughput assay was used to screen a 2320 compound library for inhibitors of SidA. Celastrol, a natural quinone methide, was identified as a noncompetitive inhibitor of SidA with a MIC value of 2 μM. Docking experiments suggest that celastrol binds across the NADPH and l-Orn pocket. Celastrol prevents A. fumigatus growth in blood agar. The addition of purified ferric-siderophore abolished the inhibitory effect of celastrol. Thus, celastrol inhibits A. fumigatus growth by blocking siderophore biosynthesis through SidA inhibiton.

Paralytic shellfish toxin biosynthesis in cyanobacteria and dinoflagellates: A molecular overview.

Science.gov (United States)

Wang, Da-Zhi; Zhang, Shu-Fei; Zhang, Yong; Lin, Lin

2016-03-01

Paralytic shellfish toxins (PSTs) are a group of water soluble neurotoxic alkaloids produced by two different kingdoms of life, prokaryotic cyanobacteria and eukaryotic dinoflagellates. Owing to the wide distribution of these organisms, these toxic secondary metabolites account for paralytic shellfish poisonings around the world. On the other hand, their specific binding to voltage-gated sodium channels makes these toxins potentially useful in pharmacological and toxicological applications. Much effort has been devoted to the biosynthetic mechanism of PSTs, and gene clusters encoding 26 proteins involved in PST biosynthesis have been unveiled in several cyanobacterial species. Functional analysis of toxin genes indicates that PST biosynthesis in cyanobacteria is a complex process including biosynthesis, regulation, modification and export. However, less is known about the toxin biosynthesis in dinoflagellates owing to our poor understanding of the massive genome and unique chromosomal characteristics [1]. So far, few genes involved in PST biosynthesis have been identified from dinoflagellates. Moreover, the proteins involved in PST production are far from being totally explored. Thus, the origin and evolution of PST biosynthesis in these two kingdoms are still controversial. In this review, we summarize the recent progress on the characterization of genes and proteins involved in PST biosynthesis in cyanobacteria and dinoflagellates, and discuss the standing evolutionary hypotheses concerning the origin of toxin biosynthesis as well as future perspectives in PST biosynthesis. Paralytic shellfish toxins (PSTs) are a group of potent neurotoxins which specifically block voltage-gated sodium channels in excitable cells and result in paralytic shellfish poisonings (PSPs) around the world. Two different kingdoms of life, cyanobacteria and dinoflagellates are able to produce PSTs. However, in contrast with cyanobacteria, our understanding of PST biosynthesis in

Influence of fungicides on occurence of Fusarium spp. and other stem base diseases on winter wheat

Directory of Open Access Journals (Sweden)

Václav Sklenář

2008-01-01

Full Text Available From 1999 to 2004 the occurence of fungi: Pseudocercosporella herpotrichoides (Fron. and Fusarium spp. was evaluated in small plot field trials on seven varieties of winter wheat. The efficacy of fungicide protection against stem base diseases and influence on yields was monitored in field conditions in Velká Bystřice near Olomouc.For diagnostic of casual fungi two methods were used: 1. Method of coloring mycelium in stems, 2. Method of cultivation of mycelim on agar.Results from detection of casual fungi are following: Pseudocercosporella herpotrichoides (Fron., Fusarium culmorum (W. G. Sm. Sacc. and Fusarium graminearum Schwabe.For high efficacy of protection against roots and stem base disease the following fungicide variants should be applied: Sportak Alpha 1.5 l . ha−1 (BBCH 30/Cerelux Plus 0.7 l . ha−1 (BBCH 51, Sportak HF 1 l . ha−1 (BBCH 30/Cerelux Plus 0.7 l . ha−1, Alert S 1.0 l . ha−1 (BBCH 30/Cerelux Plus 0.7 l . ha−1 (BBCH 51. The application of fungicides positively influenced yields. Yield increased at average by10–20 % after the aplication but the rise in yields was not in total correlation with the efficacy. These results can be possibly used in the system of integral control of winter wheat against stem base disease in wheat.

ENVIRONMENTAL RISK ASSESSMENT OF SOME COPPER BASED FUNGICIDES ACCORDING TO THE REQUIREMENTS OF GOOD LABORATORY PRACTICE

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Marga GRĂDILĂ

2015-10-01

Full Text Available The paper presents data demonstrating the functionality of biological systems reconstituted with aquatic organisms developed under Good Laboratory Practice testing facility within Research - Development Institute for Plant Protection Bucharest for environmental risk assessment of four fungicides based on copper, according to Good Laboratory Practice requirements. For risk assessment, according to GLP were made the following steps: Good Laboratory Practice test facility was established, we have ensured adequate space for growth, acclimatization and testing for each test species, it was installed a complex water production instalation needed to perform tests, it was achieved control system for checking environmental conditions and have developed specific operating procedures that have been accredited according to Good Laboratory Practice.The results showed that biological systems model of the Good Laboratory Practice test facility in Research - Development Institute for Plant Protection meet the requirements of Organisation for Economic Co-operation and Development Guidelines regarding GLP, and after testing copper-based fungicides in terms of acute toxicity Cyprinus carpio and to Daphnia magna revealed that three of them (copper oxychloride, copper hydroxide and copper sulphate showed ecological efficiency, ie low toxicity. Metallic copper based fungicides showed a higher toxicity, resulting in fish toxicity symptoms: sleep, sudden immersion, faded, weakness, swimming in spiral, lack of balance, breathing slow and cumbersome, spasms and mortality.

Elucidating the structural basis for differing enzyme inhibitor potency by cryo-EM.

Science.gov (United States)

Rawson, Shaun; Bisson, Claudine; Hurdiss, Daniel L; Fazal, Asif; McPhillie, Martin J; Sedelnikova, Svetlana E; Baker, Patrick J; Rice, David W; Muench, Stephen P

2018-02-20

Histidine biosynthesis is an essential process in plants and microorganisms, making it an attractive target for the development of herbicides and antibacterial agents. Imidazoleglycerol-phosphate dehydratase (IGPD), a key enzyme within this pathway, has been biochemically characterized in both Saccharomyces cerevisiae ( Sc_ IGPD) and Arabidopsis thaliana ( At_ IGPD). The plant enzyme, having been the focus of in-depth structural analysis as part of an inhibitor development program, has revealed details about the reaction mechanism of IGPD, whereas the yeast enzyme has proven intractable to crystallography studies. The structure-activity relationship of potent triazole-phosphonate inhibitors of IGPD has been determined in both homologs, revealing that the lead inhibitor (C348) is an order of magnitude more potent against Sc_ IGPD than At_ IGPD; however, the molecular basis of this difference has not been established. Here we have used single-particle electron microscopy (EM) to study structural differences between the At and Sc_ IGPD homologs, which could influence the difference in inhibitor potency. The resulting EM maps at ∼3 Å are sufficient to de novo build the protein structure and identify the inhibitor binding site, which has been validated against the crystal structure of the At_ IGPD/C348 complex. The structure of Sc _IGPD reveals that a 24-amino acid insertion forms an extended loop region on the enzyme surface that lies adjacent to the active site, forming interactions with the substrate/inhibitor binding loop that may influence inhibitor potency. Overall, this study provides insights into the IGPD family and demonstrates the power of using an EM approach to study inhibitor binding. Copyright © 2018 the Author(s). Published by PNAS.

Using airborne imagery to monitor cotton root rot infection before and after fungicide treatment

Science.gov (United States)

Cotton root rot is a severe soilborne disease that has affected cotton production for over a century. Recent research has shown that a commercial fungicide, flutriafol, has potential for the control of this disease. To effectively and economically control this disease, it is necessary to identify in...

Elimination of fungicides in biopurification systems: Effect of fungal bioaugmentation on removal performance and microbial community structure.

Science.gov (United States)

Murillo-Zamora, Sergio; Castro-Gutiérrez, Víctor; Masís-Mora, Mario; Lizano-Fallas, Verónica; Rodríguez-Rodríguez, Carlos E

2017-11-01

Bioaugmentation with ligninolytic fungi represents a potential way to improve the performance of biomixtures used in biopurification systems for the treatment of pesticide-containing agricultural wastewater. The fungus Trametes versicolor was employed in the bioaugmentation of a biomixture to be used in the simultaneous removal of seven fungicides. Liquid cultures of the fungus were able to remove tebuconazole, while no evidence of carbendazim, metalaxyl and triadimenol depletion was found. When applied in the biomixture, the bioaugmented matrix failed to remove all the triazole fungicides (including tebuconazole) under the assayed conditions, but was efficient to eliminate carbendazim, edifenphos and metalaxyl (the latter only after a second pesticide application). The re-addition of pesticides markedly increased the elimination of carbendazim and metalaxyl; nonetheless, no clear enhancement of the biomixture performance could be ascribed to fungal bioaugmentation, not even after the re-inoculation of fungal biomass. Detoxification efficiently took place in the biomixture (9 d after pesticide applications) according to acute tests on Daphnia magna. DGGE-analysis revealed only moderate time-divergence in bacterial and fungal communities, and a weak establishment of T. versicolor in the matrix. Data suggest that the non-bioaugmented biomixture is useful for the treatment of fungicides other than triazoles. Copyright © 2017 Elsevier Ltd. All rights reserved.

Richness and density of aquatic benthic macroinvertebrates after exposure to fungicides and insecticides in rice paddy fields

Directory of Open Access Journals (Sweden)

ALANA C.D. WANDSCHEER

Full Text Available ABSTRACT The objective of this study was to verify the richness and density of aquatic benthic macroinvertebrates after exposure to fungicides and insecticides of the rice paddy fields. In the crop seasons of 2012/13 and 2013/14, field experiments were performed, which consisted of single-dose applications of the fungicides trifloxystrobin + tebuconazole and tricyclazole, and the insecticides lambda-cyhalothrin + thiamethoxam and diflubenzuron, in 10 m2 experimental plots, over rice plants in the R3 stage. Control plots with and without rice plants were maintained in order to simulate a natural environment. Soil samples were collected during rice cultivation for assessment of the macroinvertebrate fauna. Chemical-physical parameters assessed in the experiments included temperature, pH and oxygen dissolved in the water and pesticide persistence in the water and in the soil. The application of a single dose of the pesticides and fungicides in the recommended period does not cause significant negative effects over the richness and density of the macroinvertebrates. Tebuconazole, tricyclazole and thiamethoxam showed high persistence in the irrigation water of rice paddy fields. Thus, the doses and number of applications of these products in crops should be carefully handled in order to avoid contamination of the environment.

Richness and density of aquatic benthic macroinvertebrates after exposure to fungicides and insecticides in rice paddy fields.

Science.gov (United States)

Wandscheer, Alana C D; Marchesan, Enio; Santos, Sandro; Zanella, Renato; Silva, Marília F; Londero, Guilherme P; Donato, Gabriel

2017-01-01

The objective of this study was to verify the richness and density of aquatic benthic macroinvertebrates after exposure to fungicides and insecticides of the rice paddy fields. In the crop seasons of 2012/13 and 2013/14, field experiments were performed, which consisted of single-dose applications of the fungicides trifloxystrobin + tebuconazole and tricyclazole, and the insecticides lambda-cyhalothrin + thiamethoxam and diflubenzuron, in 10 m2 experimental plots, over rice plants in the R3 stage. Control plots with and without rice plants were maintained in order to simulate a natural environment. Soil samples were collected during rice cultivation for assessment of the macroinvertebrate fauna. Chemical-physical parameters assessed in the experiments included temperature, pH and oxygen dissolved in the water and pesticide persistence in the water and in the soil. The application of a single dose of the pesticides and fungicides in the recommended period does not cause significant negative effects over the richness and density of the macroinvertebrates. Tebuconazole, tricyclazole and thiamethoxam showed high persistence in the irrigation water of rice paddy fields. Thus, the doses and number of applications of these products in crops should be carefully handled in order to avoid contamination of the environment.

Insecticidal, Repellent and Fungicidal Properties of Novel Trifluoromethylphenyl Amides

Science.gov (United States)

2013-01-01

inhibition even at the higher concentration of 30.0 lM. Captan is an excellent fungicide with a multisite mode of action that is ap- plied to crops such as...trifluoroacetamide (1c) was most active (24 h LD50 19.182 nM, 0.5 lL/insect). However, the 24 h LC50 and LD50 values of fipronil against Ae. aegypti...adults with 24 h LC50 values of 5.6 and 4.9 lg/cm2 for the Oregon- R and 1675 strains, respectively. Fipronil had LC50 values of 0.004 and 0.017 lg/cm2

Elaboration of a fragment library hit produces potent and selective aspartate semialdehyde dehydrogenase inhibitors.

Science.gov (United States)

Thangavelu, Bharani; Bhansali, Pravin; Viola, Ronald E

2015-10-15

Aspartate-β-semialdehyde dehydrogenase (ASADH) lies at the first branch point in the aspartate metabolic pathway which leads to the biosynthesis of several essential amino acids and some important metabolites. This pathway is crucial for many metabolic processes in plants and microbes like bacteria and fungi, but is absent in mammals. Therefore, the key microbial enzymes involved in this pathway are attractive potential targets for development of new antibiotics with novel modes of action. The ASADH enzyme family shares the same substrate binding and active site catalytic groups; however, the enzymes from representative bacterial and fungal species show different inhibition patterns when previously screened against low molecular weight inhibitors identified from fragment library screening. In the present study several approaches, including fragment based drug discovery (FBDD), inhibitor docking, kinetic, and structure-activity relationship (SAR) studies have been used to guide ASADH inhibitor development. Elaboration of a core structure identified by FBDD has led to the synthesis of low micromolar inhibitors of the target enzyme, with high selectivity introduced between the Gram-negative and Gram-positive orthologs of ASADH. This new set of structures open a novel direction for the development of inhibitors against this validated drug-target enzyme. Copyright © 2015 Elsevier Ltd. All rights reserved.

In Vivo Roles of Fatty Acid Biosynthesis Enzymes in Biosynthesis of Biotin and α-Lipoic Acid in Corynebacterium glutamicum.

Science.gov (United States)

Ikeda, Masato; Nagashima, Takashi; Nakamura, Eri; Kato, Ryosuke; Ohshita, Masakazu; Hayashi, Mikiro; Takeno, Seiki

2017-10-01

For fatty acid biosynthesis, Corynebacterium glutamicum uses two type I fatty acid synthases (FAS-I), FasA and FasB, in addition to acetyl-coenzyme A (CoA) carboxylase (ACC) consisting of AccBC, AccD1, and AccE. The in vivo roles of the enzymes in supplying precursors for biotin and α-lipoic acid remain unclear. Here, we report genetic evidence demonstrating that the biosynthesis of these cofactors is linked to fatty acid biosynthesis through the FAS-I pathway. For this study, we used wild-type C. glutamicum and its derived biotin vitamer producer BFI-5, which was engineered to express Escherichia coli bioBF and Bacillus subtilis bioI Disruption of either fasA or fasB in strain BFI-5 led to decreased production of biotin vitamers, whereas its amplification contributed to increased production, with a larger impact of fasA in both cases. Double disruptions of fasA and fasB resulted in no biotin vitamer production. The acc genes showed a positive effect on production when amplified simultaneously. Augmented fatty acid biosynthesis was also reflected in pimelic acid production when carbon flow was blocked at the BioF reaction. These results indicate that carbon flow down the FAS-I pathway is destined for channeling into the biotin biosynthesis pathway, and that FasA in particular has a significant impact on precursor supply. In contrast, fasB disruption resulted in auxotrophy for lipoic acid or its precursor octanoic acid in both wild-type and BFI-5 strains. The phenotypes were fully complemented by plasmid-mediated expression of fasB but not fasA These results reveal that FasB plays a specific physiological role in lipoic acid biosynthesis in C. glutamicum IMPORTANCE For the de novo biosynthesis of fatty acids, C. glutamicum exceptionally uses a eukaryotic multifunctional type I fatty acid synthase (FAS-I) system comprising FasA and FasB, in contrast to most bacteria, such as E. coli and B. subtilis , which use an individual nonaggregating type II fatty acid synthase

Comparison of dielectric barrier discharge modes fungicidal effect on candida albicans growth

International Nuclear Information System (INIS)

Slama, J.; Kriha, V.; Fantova, V.; Julak, J.

2013-01-01

Filamentary and quasi-homogeneous mode of dielectric barrier discharge (DBD) was investigated as a plasma source with fungicidal effect on Candida albicans yeast inoculated on Sabouraud agar wafers. As compared with the filamentary DBD mode, the quasi-homogeneous mode had significantly better results: shorter exposition time needed for inhibiting C. albicans yeast, moreover the quasi-homogeneous mode had gentle influence on the agar surface structure.

Foliar Application of the Fungicide Pyraclostrobin Reduced Bacterial Spot Disease of Pepper

OpenAIRE

Beom Ryong Kang; Jang Hoon Lee; Young Cheol Kim

2018-01-01

Pyraclostrobin is a broad-spectrum fungicide that inhibits mitochondrial respiration. However, it may also induce systemic resistance effective against bacterial and viral diseases. In this study, we evaluated whether pyraclostrobin enhanced resistance against the bacterial spot pathogen, Xanthomonas euvesicatora on pepper (Capsicum annuum). Although pyraclostrobin alone did not suppressed the in vitro growth of X. euvesicatoria, disease severity in pepper was significantly lower by 69% after...

Biosynthesis of silver nanoparticles by Aspergillus niger , Fusarium ...

African Journals Online (AJOL)

... scanning electron microscope (SEM). Results indicate the synthesis of silver nanoparticles in the reaction mixture. The synthesis of nanoparticles would be suitable for developing a microbial nanotechnology biosynthesis process for mass scale production. Keywords: Silver nanoparticles, biosynthesis, fungi, Aspergillus.

Increased sesquiterpenoid biosynthesis and an apparent decrease in sterol biosynthesis in elicitor-treated tobacco cell suspension cultures

International Nuclear Information System (INIS)

Voegeli, U.; Bhatt, P.N.; Chappell, J.

1987-01-01

Addition of fungel elicitor prepared from Phytophthora parasitica to tobacco cell suspension cultures leads to an increased production of the phytoalexin capsidiol. Capsidiol is a sesquiterpenoid which is most likely synthesized from farnesylpyrophosphat (FPP) by a bicyclic cyclase reaction. Because FPP is also a substrate for squalene synthetase and therefore a precursor of sterol biosynthesis, the question arises whether or not the accumulation of capsidiol in elicitor-treated cells occurs at the expense of sterol biosynthesis. ( 14 C]-acetate was given to elicitor-treated and control (no treatment) cell cultures and incorporation into sterols and capsidiol determined. No labeled capsidiol was detected in control cells. In elicitor-treated cells about 12-15% of the radioactivity taken up by the cells was incorporated into capsidiol. In contrast, control cells incorporated 4 times more radioactivity into sterols than elicitor-treated cells. Similar results were obtained using ( 3 H)-mevalonate as a precursor of capsidiol and sterol biosynthesis. Likely explanations for the apparently decline in sterol biosynthesis in elicitor-treated cells include: (1) inhibition of squalene synthetase; (2) induction of capsidiol synthesizing enzymes; and (3) metabolic channeling of FPP into capsidiol versus sterols. These possibilities will be discussed further together with other results

High glucose suppresses human islet insulin biosynthesis by inducing miR-133a leading to decreased polypyrimidine tract binding protein-expression

DEFF Research Database (Denmark)

Fred, Rikard G; Bang-Berthelsen, Claus H; Mandrup-Poulsen, Thomas

2010-01-01

BACKGROUND: Prolonged periods of high glucose exposure results in human islet dysfunction in vitro. The underlying mechanisms behind this effect of high glucose are, however, unknown. The polypyrimidine tract binding protein (PTB) is required for stabilization of insulin mRNA and the PTB mRNA 3......'-UTR contains binding sites for the microRNA molecules miR-133a, miR-124a and miR-146. The aim of this study was therefore to investigate whether high glucose increased the levels of these three miRNAs in association with lower PTB levels and lower insulin biosynthesis rates. METHODOLOGY...... for real-time RT-PCR analysis of miR-133a, miR-124a, miR-146, insulin mRNA and PTB mRNA contents. Insulin biosynthesis rates were determined by radioactive labeling and immunoprecipitation. Synthetic miR-133a precursor and inhibitor were delivered to dispersed islet cells by lipofection, and PTB...

Determination of acid dissociation constants of triazole fungicides by pressure assisted capillary electrophoresis

Czech Academy of Sciences Publication Activity Database

Konášová, Renáta; Jaklová Dytrtová, Jana; Kašička, Václav

2015-01-01

Roč. 1408, Aug 21 (2015), s. 243-249 ISSN 0021-9673 R&D Projects: GA ČR(CZ) GA13-17224S; GA ČR GP13-21409P Institutional support: RVO:61388963 Keywords : triazole fungicides * acid dissociation constant * pK(a) * capillary electrophoresis * ionic mobility Subject RIV: CB - Analytical Chemistry , Separation Impact factor: 3.926, year: 2015

Probing the Influence of Linker Length and Flexibility in the Design and Synthesis of New Trehalase Inhibitors

Directory of Open Access Journals (Sweden)

Giampiero D’Adamio

2018-02-01

Full Text Available This work aims to synthesize new trehalase inhibitors selective towards the insect trehalase versus the porcine trehalase, in view of their application as potentially non-toxic insecticides and fungicides. The synthesis of a new pseudodisaccharide mimetic 8, by means of a stereoselective α-glucosylation of the key pyrrolizidine intermediate 13, was accomplished. The activity of compound 8 as trehalase inhibitor towards C. riparius trehalase was evaluated and the results showed that 8 was active in the μM range and showed a good selectivity towards the insect trehalase. To reduce the overall number of synthetic steps, simpler and more flexible disaccharide mimetics 9–11 bearing a pyrrolidine nucleus instead of the pyrrolizidine core were synthesized. The biological data showed the key role of the linker chain’s length in inducing inhibitory properties, since only compounds 9 (α,β-mixture, bearing a two-carbon atom linker chain, maintained activity as trehalase inhibitors. A proper change in the glucosyl donor-protecting groups allowed the stereoselective synthesis of the β-glucoside 9β, which was active in the low micromolar range (IC50 = 0.78 μM and 12-fold more potent (and more selective than 9α towards the insect trehalase.

Impact of three different fungicides on fungal epi- and endophytic communities of common bean (Phaseolus vulgaris) and broad bean (Vicia faba).

Science.gov (United States)

Prior, René; Mittelbach, Moritz; Begerow, Dominik

2017-06-03

In this study, the impacts of three different fungicides to fungal phyllosphere communities on broad bean (Vicia faba, Fabaceae) and common bean (Phaseolus vulgaris, Fabaceae) were analyzed. The fungicides included copper, sulfur, and azoxystrobin. The plants were sowed, grown, and treated under conditions occurring in conventional and organic farming. A culture-based approach was used to identify changes in the phyllosphere fungal community after the treatment. Different effects on species richness and growth index of the epiphytic and endophytic communities for common bean and broad bean could be shown. Treatments with sulfur showed the weakest effect, followed by those based on copper and the systemic azoxystrobin, which showed the strongest effect especially on endophytic communities. The epiphytic fungal community took five weeks to recover after treatment with azoxystrobin. However, the effect of azoxystrobin on the endophytic community lasted more than five weeks. Finally, the data suggest that the surface structure of the host leaves have a huge impact on the mode of action that the fungicides exert.

Evidence for a cytoplasmic pathway of oxalate biosynthesis in Aspergillus niger

International Nuclear Information System (INIS)

Kubicek, C.P.; Schreferl-Kunar, G.; Woehrer, W.; Roehr, M.

1988-01-01

Oxalate accumulation of up to 8 g/liter was induced in Aspergillus niger by shifting the pH from 6 to 8. This required the presence of P/sub i/ and a nitrogen source and was inhibited by the protein synthesis inhibitor cycloheximide. Exogenously added 14 CO 2 was not incorporated into oxalate, but was incorporated into acetate and malate, thus indicating the biosynthesis of oxalate by hydrolytic cleavage of oxaloacetate. Inhibition of mitochondrial citrate metabolism by fluorocitrate did not significantly decrease the oxalate yield. The putative enzyme that was responsible for this oxaloacetate hydrolase (EC 3.7.1.1), which was induced de novo during the pH shift. Subcellular fractionation of oxalic acid-forming mycelia of A. niger showed that this enzyme is located in the cytoplasm of A. niger. The results are consistent with a cytoplasmic pathway of oxalate formation which does not involve the tricarboxylic acid cycle

Mycobacterium tuberculosis phosphoribosylpyrophosphate synthetase: biochemical features of a crucial enzyme for mycobacterial cell wall biosynthesis.

Directory of Open Access Journals (Sweden)

Anna P Lucarelli

Full Text Available The selection and soaring spread of Mycobacterium tuberculosis multidrug-resistant (MDR-TB and extensively drug-resistant strains (XDR-TB is a severe public health problem. Currently, there is an urgent need for new drugs for tuberculosis treatment, with novel mechanisms of action and, moreover, the necessity to identify new drug targets. Mycobacterial phosphoribosylpyrophosphate synthetase (MtbPRPPase is a crucial enzyme involved in the biosynthesis of decaprenylphosphoryl-arabinose, an essential precursor for the mycobacterial cell wall biosynthesis. Moreover, phosphoribosylpyrophosphate, which is the product of the PRPPase catalyzed reaction, is the precursor for the biosynthesis of nucleotides and of some amino acids such as histidine and tryptophan. In this context, the elucidation of the molecular and functional features of MtbPRPPase is mandatory. MtbPRPPase was obtained as a recombinant form, purified to homogeneity and characterized. According to its hexameric form, substrate specificity and requirement of phosphate for activity, the enzyme proved to belong to the class I of PRPPases. Although the sulfate mimicked the phosphate, it was less effective and required higher concentrations for the enzyme activation. MtbPRPPase showed hyperbolic response to ribose 5-phosphate, but sigmoidal behaviour towards Mg-ATP. The enzyme resulted to be allosterically activated by Mg(2+ or Mn(2+ and inhibited by Ca(2+ and Cu(2+ but, differently from other characterized PRPPases, it showed a better affinity for the Mn(2+ and Cu(2+ ions, indicating a different cation binding site geometry. Moreover, the enzyme from M. tuberculosis was allosterically inhibited by ADP, but less sensitive to inhibition by GDP. The characterization of M. tuberculosis PRPPase provides the starting point for the development of inhibitors for antitubercular drug design.

Mechanisms of action underlying the antiandrogenic effects of the fungicide prochloraz

DEFF Research Database (Denmark)

Laier, Peter; Metzdorff, Stine Broeng; Boberg, Julie

2006-01-01

The fungicide prochloraz has got multiple mechanisms of action that may influence the demasculinizing and reproductive toxic effects of the compound. In the present study, Wistar rats were dosed perinatally with prochloraz (50 and 150 mg/kg/day) from gestational day (GD) 7 to postnatal day (PND) ...... acts directly on the fetal testis to inhibit steroidogenesis and that this effect is exhibited at protein, and not at genomic, level. (c) 2005 Elsevier Inc. All rights reserved....

The effect of stereochemistry on the biological activity of natural phytotoxins, fungicides, insecticides and herbicides.

Science.gov (United States)

Evidente, Antonio; Cimmino, Alessio; Andolfi, Anna

2013-02-01

Phytotoxins are secondary microbial metabolites that play an essential role in the development of disease symptoms induced by fungi on host plants. Although phytotoxins can cause extensive-and in some cases devastating-damage to agricultural crops, they can also represent an important tool to develop natural herbicides when produced by fungi and plants to inhibit the growth and spread of weeds. An alternative strategy to biologically control parasitic plants is based on the use of plant and fungal metabolites, which stimulate seed germination in the absence of the host plant. Nontoxigenic fungi also produce bioactive metabolites with potential fungicide and insecticide activity, and could be applied for crop protection. All these metabolites represent important tools to develop eco-friendly pesticides. This review deals with the relationships between the biological activity of some phytotoxins, seed germination stimulants, fungicides and insecticides, and their stereochemistry. Copyright © 2012 Wiley Periodicals, Inc.

Comparison of human health risks resulting from exposure to fungicides and mycotoxins via food

NARCIS (Netherlands)

Muri, S.D.; Voet, van der H.; Boon, P.E.; Klaveren, van J.D.; Bruschweiler, B.

2009-01-01

The interest in holistic considerations in the area of food safety is increasing. Risk managers may face the problem that reducing the risk of one compound may increase the risk of another compound. An example is the potential increase in mycotoxin levels due to a reduced use of fungicides in crop

Jasmonate mediates salt-induced nicotine biosynthesis in tobacco (Nicotiana tabacum L.

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Xiaodong Chen

2016-04-01

Full Text Available Jasmonate (JA, as an important signal, plays a key role in multiple processes of plant growth, development and stress response. Nicotine and related pyridine alkaloids in tobacco (Nicotiana tabacum L. are essential secondary metabolites. Whether environmental factors control nicotine biosynthesis and the underlying mechanism remains previously unreported. Here, we applied physiological and biochemical approaches to investigate how salt stress affects nicotine biosynthesis in tobacco. We found that salt stress induced the biosynthesis of JA, which subsequently triggered the activation of JA-responsive gene expression and, ultimately, nicotine synthesis. Bioinformatics analysis revealed the existence of many NtMYC2a-recognized G-box motifs in the promoter regions of NtLOX, NtAOS, NtAOC and NtOPR genes. Applying exogenous JA increased nicotine content, while suppressing JA biosynthesis reduced nicotine biosynthesis. Salt treatment could not efficiently induce nicotine biosynthesis in transgenic anti-COI1 tobacco plants. These results demonstrate that JA acts as the essential signal which triggers nicotine biosynthesis in tobacco after salt stress.

Biosynthesis of components with antifungal activity against Aspergillus spp. using Streptomyces hygroscopicus

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Dodić Jelena M.

2015-01-01

Full Text Available Losses of apple fruit during storage are mainly caused by fungal phytopathogens. Traditionally, postharvest fungal disease is controlled by the application of synthetic fungicides. However, the harmful impact on environment as well as human health largely limits their application. To reduce these problems in agrochemicals usage, new compounds for plant protection, which are eco-friendly, should be developed. The aim of this study is optimization of medium composition in terms of glucose, soybean meal and phosphates content, by applying response surface methodology, for the production of agents with antifungal activity against Aspergillus spp. For biosynthesis was used strain of Streptomyces hygroscopicus isolated from the environment. Experiments were carried out in accordance with Box-Behnken design with three factors on three levels and three repetitions in the central point. Antifungal activity of the obtained cultivation mediums against Aspergillus oryzae and Aspergillus niger was determined, in vitro, using the diffusion - disc method. For determination optimal medium components desirability function was used. Achieved model predicts that the maximum inhibition zone diameter (40.93 mm against test microorganisms is produced when the initial content of glucose, soybean meal and phosphates are 47.77 g/l, 24.54 g/l and 0.98 g/l, respectively. To minimize the consumption of medium components and costs of effluents processing, additional three sets of optimization were made. The chosen method for optimization of medium components was efficient, relatively simple and time and material saving. Obtained results can be used for the further techno-economic analysis of the process to select optimal medium composition for industrial application.

Non-target impact of fungicide tetraconazole on microbial communities in soils with different agricultural management.

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Sułowicz, Sławomir; Cycoń, Mariusz; Piotrowska-Seget, Zofia

2016-08-01

Effect of the fungicide tetraconazole on microbial community in silt loam soils from orchard with long history of triazole application and from grassland with no known history of fungicide usage was investigated. Triazole tetraconazole that had never been used on these soils before was applied at the field rate and at tenfold the FR. Response of microbial communities to tetraconazole was investigated during 28-day laboratory experiment by determination of changes in their biomass and structure (phospholipid fatty acids method-PLFA), activity (fluorescein diacetate hydrolysis-FDA) as well as changes in genetic (DGGE) and functional (Biolog) diversity. Obtained results indicated that the response of soil microorganisms to tetraconazole depended on the management of the soils. DGGE patterns revealed that both dosages of fungicide affected the structure of bacterial community and the impact on genetic diversity and richness was more prominent in orchard soil. Values of stress indices-the saturated/monounsaturated PLFAs ratio and the cyclo/monounsaturated precursors ratio, were almost twice as high and the Gram-negative/Gram-positive ratio was significantly lower in the orchard soil compared with the grassland soil. Results of principal component analysis of PLFA and Biolog profiles revealed significant impact of tetraconazole in orchard soil on day 28, whereas changes in these profiles obtained for grassland soil were insignificant or transient. Obtained results indicated that orchards soil seems to be more vulnerable to tetraconazole application compared to grassland soil. History of pesticide application and agricultural management should be taken into account in assessing of environmental impact of studied pesticides.

Relationship of Resistance to Benzimidazole Fungicides with Mutation of β-Tubulin Gene in Venturia nashicola

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Yeonsoo Kwak

2017-06-01

Full Text Available Pear scab caused by Venturia nashicola has been reported as an important disease of pear resulting in lowering the quality of pear fruits. In this study, it was conducted to investigate the relationship between resistance of V. nashicola and mutation of β-tubulin gene and the fungicide resistance in field isolate group in benzimidazole fungicides. Responce of V. nashicola to carbendazim could be classified into 3 groups as sensitive that does not grow at all on PDA amended with 0.16 μg/ml of carbendazim, low resistance that could not grow in 4.0 μg/ml medium, and high resistance that can grow even at 100 μg/ml. Thirty isolates of V. nashicola collected from 3 regions as Wonju, Naju, and Okcheon were highly resistant to carbendazim. Analysis of the nucleotide sequence of β-tubulin gene of V. nashicola showed that there was no difference in the nucleotide sequence between the sensitive and the low-resistant isolate, but GAG at codon 198 (glutamic acid was replaced with GCG (alanine in the high-resistant isolate. Among 10 isolates obtained from the Okcheon, 5 isolates showed the substitution of glycine for glutamic acid, which were resistant to carbendazim, but more sensitive to the mixture of carbendazim and diethofencarb than others. Through these results, all isolates of V. nashicola isolated in pear orchard were found to be resistant to benzimidazoles. Also, mutants E198A and E198G at β-tubulin were found to be important mechanisms of V. nashicola resistance against benzimidazole fungicides.

Infectivity of the conidia of the rice blast fungus treated with the different fungicidal solutions

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Hashioka, Y; Ikegami, H

1959-01-01

Infectivity of the conidia of Piricularia oryzae (rice blast fungus) which had been treated with different fungicides was examined. Germination of conidia treated with phenylmercuric acetate was severely repressed. Copper sulfate had a mild inhibitory effect. Organosulfur compounds also had a slight inhibitory effect.

Widespread contamination of wildflower and bee-collected pollen with complex mixtures of neonicotinoids and fungicides commonly applied to crops.

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David, Arthur; Botías, Cristina; Abdul-Sada, Alaa; Nicholls, Elizabeth; Rotheray, Ellen L; Hill, Elizabeth M; Goulson, Dave

2016-03-01

There is considerable and ongoing debate as to the harm inflicted on bees by exposure to agricultural pesticides. In part, the lack of consensus reflects a shortage of information on field-realistic levels of exposure. Here, we quantify concentrations of neonicotinoid insecticides and fungicides in the pollen of oilseed rape, and in pollen of wildflowers growing near arable fields. We then compare this to concentrations of these pesticides found in pollen collected by honey bees and in pollen and adult bees sampled from bumble bee colonies placed on arable farms. We also compared this with levels found in bumble bee colonies placed in urban areas. Pollen of oilseed rape was heavily contaminated with a broad range of pesticides, as was the pollen of wildflowers growing nearby. Consequently, pollen collected by both bee species also contained a wide range of pesticides, notably including the fungicides carbendazim, boscalid, flusilazole, metconazole, tebuconazole and trifloxystrobin and the neonicotinoids thiamethoxam, thiacloprid and imidacloprid. In bumble bees, the fungicides carbendazim, boscalid, tebuconazole, flusilazole and metconazole were present at concentrations up to 73nanogram/gram (ng/g). It is notable that pollen collected by bumble bees in rural areas contained high levels of the neonicotinoids thiamethoxam (mean 18ng/g) and thiacloprid (mean 2.9ng/g), along with a range of fungicides, some of which are known to act synergistically with neonicotinoids. Pesticide exposure of bumble bee colonies in urban areas was much lower than in rural areas. Understanding the effects of simultaneous exposure of bees to complex mixtures of pesticides remains a major challenge. Copyright © 2015 Elsevier Ltd. All rights reserved.

Impact of non-selective fungicides on the growth and production of ochratoxin A by Aspergillus ochraceus and A. carbonarius in barley-based medium.

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Mateo, Eva M; Valle-Algarra, F M; Mateo-Castro, R; Jimenez, M

2011-01-01

The aim of this study was to assess the influence of the non-selective fungicides mancozeb, copper oxychloride, and sulfur on the growth and capability for producing ochratoxin A (OTA) of ochratoxigenic isolates of Aspergillus carbonarius and A. ochraceus in barley-based medium. Lag phases and growth rates were determined for each fungicide at different doses, at 15°C and 25°C and at 0.97 a(w). Mancozeb at 40 mg l(-1 )inhibited fungal growth and provided lag phases >24 days at 10-20 mg l(-1) and 15°C. OTA was observed only at 25°C and doses Sulfur was inhibitory or provided large lag phases at 5-8 g l(-1) (at 15°C) while at 25°C growth took place even at 8 g l(-1), although OTA levels were low or undetectable. The antifungal activity decreased in the order mancozeb > copper oxychloride > sulfur, and was lower at 25°C than at 15°C. OTA accumulation was affected by the type of fungicide, dose, temperature and time. The efficacy of these fungicides on the growth of A. carbonarius and A. ochraceus and OTA production in barley-based medium is assessed for the first time.