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Sample records for antifungal compound produced

  1. Production and characterization of antifungal compounds produced by Lactobacillus plantarum IMAU10014.

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    HaiKuan Wang

    Full Text Available Lactobacillus plantarum IMAU10014 was isolated from koumiss that produces a broad spectrum of antifungal compounds, all of which were active against plant pathogenic fungi in an agar plate assay. Two major antifungal compounds were extracted from the cell-free supernatant broth of L. plantarum IMAU10014. 3-phenyllactic acid and Benzeneacetic acid, 2-propenyl ester were carried out by HPLC, LC-MS, GC-MS, NMR analysis. It is the first report that lactic acid bacteria produce antifungal Benzeneacetic acid, 2-propenyl ester. Of these, the antifungal products also have a broad spectrum of antifungal activity, namely against Botrytis cinerea, Glomerella cingulate, Phytophthora drechsleri Tucker, Penicillium citrinum, Penicillium digitatum and Fusarium oxysporum, which was identified by the overlay and well-diffusion assay. F. oxysporum, P. citrinum and P. drechsleri Tucker were the most sensitive among molds.

  2. Antifungal compounds from cyanobacteria.

    Science.gov (United States)

    Shishido, Tânia K; Humisto, Anu; Jokela, Jouni; Liu, Liwei; Wahlsten, Matti; Tamrakar, Anisha; Fewer, David P; Permi, Perttu; Andreote, Ana P D; Fiore, Marli F; Sivonen, Kaarina

    2015-04-13

    Cyanobacteria are photosynthetic prokaryotes found in a range of environments. They are infamous for the production of toxins, as well as bioactive compounds, which exhibit anticancer, antimicrobial and protease inhibition activities. Cyanobacteria produce a broad range of antifungals belonging to structural classes, such as peptides, polyketides and alkaloids. Here, we tested cyanobacteria from a wide variety of environments for antifungal activity. The potent antifungal macrolide scytophycin was detected in Anabaena sp. HAN21/1, Anabaena cf. cylindrica PH133, Nostoc sp. HAN11/1 and Scytonema sp. HAN3/2. To our knowledge, this is the first description of Anabaena strains that produce scytophycins. We detected antifungal glycolipopeptide hassallidin production in Anabaena spp. BIR JV1 and HAN7/1 and in Nostoc spp. 6sf Calc and CENA 219. These strains were isolated from brackish and freshwater samples collected in Brazil, the Czech Republic and Finland. In addition, three cyanobacterial strains, Fischerella sp. CENA 298, Scytonema hofmanni PCC 7110 and Nostoc sp. N107.3, produced unidentified antifungal compounds that warrant further characterization. Interestingly, all of the strains shown to produce antifungal compounds in this study belong to Nostocales or Stigonematales cyanobacterial orders.

  3. Identification and quantification of antifungal compounds produced by lactic acid bacteria and propionibacteria.

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    Le Lay, Céline; Coton, Emmanuel; Le Blay, Gwenaëlle; Chobert, Jean-Marc; Haertlé, Thomas; Choiset, Yvan; Van Long, Nicolas Nguyen; Meslet-Cladière, Laurence; Mounier, Jérôme

    2016-12-19

    Fungal growth in bakery products represents the most frequent cause of spoilage and leads to economic losses for industrials and consumers. Bacteria, such as lactic acid bacteria and propionibacteria, are commonly known to play an active role in preservation of fermented food, producing a large range of antifungal metabolites. In a previous study (Le Lay et al., 2016), an extensive screening performed both in vitro and in situ allowed for the selection of bacteria exhibiting an antifungal activity. In the present study, active supernatants against Penicillium corylophilum and Aspergillus niger were analyzed to identify and quantify the antifungal compounds associated with the observed activity. Supernatant treatments (pH neutralization, heating and addition of proteinase K) suggested that organic acids played the most important role in the antifungal activity of each tested supernatant. Different methods (HPLC, mass spectrometry, colorimetric and enzymatic assays) were then applied to analyze the supernatants and it was shown that the main antifungal compounds corresponded to lactic, acetic and propionic acids, ethanol and hydrogen peroxide, as well as other compounds present at low levels such as phenyllactic, hydroxyphenyllactic, azelaic and caproic acids. Based on these results, various combinations of the identified compounds were used to evaluate their effect on conidial germination and fungal growth of P. corylophilum and Eurotium repens. Some combinations presented the same activity than the bacterial culture supernatant thus confirming the involvement of the identified molecules in the antifungal activity. The obtained results suggested that acetic acid was mainly responsible for the antifungal activity against P. corylophilum and played an important role in E. repens inhibition. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Purification of a new antifungal compound produced by Lactobacillus plantarum AF1 isolated from kimchi.

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    Yang, E J; Chang, H C

    2010-04-30

    The aim of this study was to purify and to identify an antifungal compound of Lactobacillus plantarum AF1, which was isolated from kimchi, and to determine if Lb. plantarum AF1 can prevent fungal growth in a particular food model system. The antifungal compound was purified using SPE and recycling prep-HPLC and its structure was elucidated using NMR and ESI-MS. The active compound from Lb. plantarum AF1 is C(12)H(22)N(2)O(2), 3,6-bis(2-methylpropyl)-2,5-piperazinedion has a molecular mass of 226. This is a new antifungal compound produced by lactic acid bacteria (LAB). To investigate the potential application of the antifungal compound to eliminate fungal spoilage in food and feed, soybean was used as a model. White mycelia and dark green spores of Aspergillus flavus ATCC 22546 were observed in the control soybeans after 1 to 2days incubation. However, fungal growth was not observed in the soybeans treated with a 4-fold concentrated supernatant of Lb. plantarum AF1 culture, even after 2days. The end products produced from kimchi LAB, like 3,6-bis(2-methylpropyl)-2,5-piperazinedion identified in this study, may be a promising alternative to chemical preservatives as a potential biopreservative which prevent fungal spoilage and mycotoxin formation in food and feed. Copyright 2010 Elsevier B.V. All rights reserved.

  5. Diffusible and Volatile Antifungal Compounds Produced by an Antagonistic Bacillus velezensis G341 against Various Phytopathogenic Fungi

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    Seong Mi Lim

    2017-10-01

    Full Text Available The aim of this study was to identify volatile and agar-diffusible antifungal metabolites produced by Bacillus sp. G341 with strong antifungal activity against various phytopathogenic fungi. Strain G341 isolated from four-year-old roots of Korean ginseng with rot symptoms was identified as Bacillus velezensis based on 16S rDNA and gyrA sequences. Strain G341 inhibited mycelial growth of all phytopathogenic fungi tested. In vivo experiment results revealed that n-butanol extract of fermentation broth effectively controlled the development of rice sheath blight, tomato gray mold, tomato late blight, wheat leaf rust, barley powdery mildew, and red pepper anthracnose. Two antifungal compounds were isolated from strain G341 and identified as bacillomycin L and fengycin A by MS/MS analysis. Moreover, volatile compounds emitted from strain G341 were found to be able to inhibit mycelial growth of various phytopathogenic fungi. Based on volatile compound profiles of strain G341 obtained through headspace collection and analysis on GC-MS, dimethylsulfoxide, 1-butanol, and 3-hydroxy-2-butanone (acetoin were identified. Taken together, these results suggest that B. valezensis G341 can be used as a biocontrol agent for various plant diseases caused by phytopathogenic fungi.

  6. Diffusible and Volatile Antifungal Compounds Produced by an Antagonistic Bacillus velezensis G341 against Various Phytopathogenic Fungi.

    Science.gov (United States)

    Lim, Seong Mi; Yoon, Mi-Young; Choi, Gyung Ja; Choi, Yong Ho; Jang, Kyoung Soo; Shin, Teak Soo; Park, Hae Woong; Yu, Nan Hee; Kim, Young Ho; Kim, Jin-Cheol

    2017-10-01

    The aim of this study was to identify volatile and agar-diffusible antifungal metabolites produced by Bacillus sp. G341 with strong antifungal activity against various phytopathogenic fungi. Strain G341 isolated from four-year-old roots of Korean ginseng with rot symptoms was identified as Bacillus velezensis based on 16S rDNA and gyrA sequences. Strain G341 inhibited mycelial growth of all phytopathogenic fungi tested. In vivo experiment results revealed that n -butanol extract of fermentation broth effectively controlled the development of rice sheath blight, tomato gray mold, tomato late blight, wheat leaf rust, barley powdery mildew, and red pepper anthracnose. Two antifungal compounds were isolated from strain G341 and identified as bacillomycin L and fengycin A by MS/MS analysis. Moreover, volatile compounds emitted from strain G341 were found to be able to inhibit mycelial growth of various phytopathogenic fungi. Based on volatile compound profiles of strain G341 obtained through headspace collection and analysis on GC-MS, dimethylsulfoxide, 1-butanol, and 3-hydroxy-2-butanone (acetoin) were identified. Taken together, these results suggest that B. valezensis G341 can be used as a biocontrol agent for various plant diseases caused by phytopathogenic fungi.

  7. Antifungal effect of volatile organic compounds produced by Bacillus amyloliquefaciens CPA-8 against fruit pathogen decays of cherry.

    Science.gov (United States)

    Gotor-Vila, A; Teixidó, N; Di Francesco, A; Usall, J; Ugolini, L; Torres, R; Mari, M

    2017-06-01

    The present work focuses on the antifungal effect of volatile organic compounds (VOCs) produced by Bacillus amyloliquefaciens CPA-8 against Monilinia laxa, M. fructicola and Botrytis cinera, three postharvest fruit pathogens of sweet cherry fruit. VOCs were evaluated with a double petri dish assay against mycelial and colony growth of target pathogens. For this purpose, CPA-8 was grown on different media and cultured for 24 and 48 h at 30 °C before assays. Data showed that mycelial growth inhibition was higher when CPA-8 was grown on Tryptone Soya Agar (TSA) while no differences were generally observed when CPA-8 was cultured for either, 24 and 48 h. Moreover, no effects were observed on colony growth. The main volatile compounds emitted by CPA-8 were identified by solid-phase microextraction (SPME)-gas chromatography as 1,3 pentadiene, acetoin (3-hydroxy-2-butanone) and thiophene. Pure compounds were also tested in vitro on mycelial growth inhibition and their EC 50 values against the three pathogens were estimated. Thiophene was the most effective VOC, showing more than 82% suppression of mycelial growth at the highest concentration (1.35 μL/mL headspace) and EC 50 values ranging from 0.06 to 6.67 μL/mL headspace. Finally, the effectiveness of thiophene and CPA-8 VOCs was evaluated against artificially inoculated cherry fruits. Among the target pathogens, M. fructicola was clearly controlled by CPA-8 with less than 25% of rotten fruits compared to the control (65% disease incidence) and for all pathogens, less than 37.5% of CPA-8 treated decayed fruits produced spores (disease sporulation). Otherwise, pure thiophene showed no effect against any pathogen on disease incidence and disease sporulation. The results indicated that VOCs produced by B. amyloliquefaciens CPA-8 could develop an additive antifungal effect against postharvest fruit pathogens on stone fruit. Copyright © 2017 Elsevier Ltd. All rights reserved.

  8. Epicoccum nigrum P16, a sugarcane endophyte, produces antifungal compounds and induces root growth.

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    Léia Cecilia de Lima Fávaro

    Full Text Available BACKGROUND: Sugarcane is one of the most important crops in Brazil, mainly because of its use in biofuel production. Recent studies have sought to determine the role of sugarcane endophytic microbial diversity in microorganism-plant interactions, and their biotechnological potential. Epicoccum nigrum is an important sugarcane endophytic fungus that has been associated with the biological control of phytopathogens, and the production of secondary metabolites. In spite of several studies carried out to define the better conditions to use E. nigrum in different crops, little is known about the establishment of an endophytic interaction, and its potential effects on plant physiology. METHODOLOGY/PRINCIPAL FINDINGS: We report an approach based on inoculation followed by re-isolation, molecular monitoring, microscopic analysis, plant growth responses to fungal colonization, and antimicrobial activity tests to study the basic aspects of the E. nigrum endophytic interaction with sugarcane, and the effects of colonization on plant physiology. The results indicate that E. nigrum was capable of increasing the root system biomass and producing compounds that inhibit the in vitro growth of sugarcane pathogens Fusarium verticillioides, Colletotrichum falcatum, Ceratocystis paradoxa, and Xanthomomas albilineans. In addition, E. nigrum preferentially colonizes the sugarcane surface and, occasionally, the endophytic environment. CONCLUSIONS/SIGNIFICANCE: Our work demonstrates that E. nigrum has great potential for sugarcane crop application because it is capable of increasing the root system biomass and controlling pathogens. The study of the basic aspects of the interaction of E. nigrum with sugarcane demonstrated the facultative endophytism of E. nigrum and its preference for the phylloplane environment, which should be considered in future studies of biocontrol using this species. In addition, this work contributes to the knowledge of the interaction of this

  9. Cytotoxic and Antifungal Activities of 5-Hydroxyramulosin, a Compound Produced by an Endophytic Fungus Isolated from Cinnamomum mollisimum

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    Carolina Santiago

    2012-01-01

    Full Text Available An endophytic fungus isolated from the plant Cinnamomum mollissimum was investigated for the bioactivity of its metabolites. The fungus, similar to a Phoma sp., was cultured in potato dextrose broth for two weeks, followed by extraction with ethyl acetate. The crude extract obtained was fractionated by high-performance liquid chromatography. Both crude extract and fractions were assayed for cytotoxicity against P388 murine leukemic cells and inhibition of bacterial and fungal pathogens. The bioactive extract fraction was purified further and characterized by nuclear magnetic resonance, mass spectral and X-ray crystallography analysis. A polyketide compound, 5-hydroxyramulosin, was identified as the constituent of the bioactive fungal extract fraction. This compound inhibited the fungal pathogen Aspergillus niger (IC50 1.56 μg/mL and was cytotoxic against murine leukemia cells (IC50 2.10 μg/mL. 5-Hydroxyramulosin was the major compound produced by the endophytic fungus. This research suggests that fungal endophytes are a good source of bioactive metabolites which have potential applications in medicine.

  10. Antifungal compounds from cultures of dairy propionibacteria type strains.

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    Lind, Helena; Sjögren, Jörgen; Gohil, Suresh; Kenne, Lennart; Schnürer, Johan; Broberg, Anders

    2007-06-01

    Antifungal compounds from cultures of five type strains of dairy propionibacteria, as well as from the cultivation medium, were studied. Cell-free supernatants and medium were fractionated by C(18) solid phase extraction. The aqueous 95% acetonitrile fractions were analyzed by GC-MS or subjected to reversed-phase HPLC, to identify, quantify or isolate antifungal substances. The resulting HPLC fractions were screened for antifungal activity against the mold Aspergillus fumigatus and the yeast Rhodotorula mucilaginosa. Active fractions were further separated by HPLC and the structures of the compounds were determined by spectroscopic and chromatographic methods. All five strains produced 3-phenyllactic acid, at concentrations ranging from 1.0 microg mL(-1) (Propionibacterium freudenreichii ssp. shermanii) to 15.1 microg mL(-1) (Propionibacterium thoenii), and at L/D -ratios ranging from 2 : 3 (Propionibacterium acidipropionici) to 9 : 1 (Propionibacterium freudenreichii). A number of active compounds found in cultures of propionibacteria were also present in noninoculated growth medium: two antifungal diketopiperazines, cyclo(L-Phe-L-Pro) and cyclo(L-Ile-L-Pro), and seven antifungal linear peptides. Three of the linear peptides corresponded to sequences found in the medium component casein, suggesting their origin from this component, whereas the diketopiperazines were suggested to be formed from medium peptides by heat treatment.

  11. Antifungal activity of extracts and phenolic compounds from ...

    African Journals Online (AJOL)

    Antifungal activity of extracts and phenolic compounds from Barringtonia racemosa L. (Lecythidaceae). NM Hussin, R Muse, S Ahmad, J Ramli, M Mahmood, MR Sulaiman, MYA Shukor, MFA Rahman, KNK Aziz ...

  12. Cryptic antifungal compounds active by synergism with polyene antibiotics.

    Science.gov (United States)

    Kinoshita, Hiroshi; Yoshioka, Mariko; Ihara, Fumio; Nihira, Takuya

    2016-04-01

    The majority of antifungal compounds reported so far target the cell wall or cell membrane of fungi, suggesting that other types of antibiotics cannot exert their activity because they cannot penetrate into the cells. Therefore, if the permeability of the cell membrane could be enhanced, many antibiotics might be found to have antifungal activity. We here used the polyene antibiotic nystatin, which binds to ergosterol and forms pores at the cell membrane, to enhance the cellular permeability. In the presence of nystatin, many culture extracts from entomopathogenic fungi displayed antifungal activity. Among all the active extracts, two active components were purified and identified as helvolic acid and terramide A. Because the minimum inhibitory concentration of either compound was reduced four-fold in the presence of nystatin, it can be concluded that this screening method is useful for detecting novel antifungal activity. Copyright © 2015 The Society for Biotechnology, Japan. Published by Elsevier B.V. All rights reserved.

  13. Antifungal chemical compounds identified using a C. elegans pathogenicity assay.

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    Julia Breger

    2007-02-01

    Full Text Available There is an urgent need for the development of new antifungal agents. A facile in vivo model that evaluates libraries of chemical compounds could solve some of the main obstacles in current antifungal discovery. We show that Candida albicans, as well as other Candida species, are ingested by Caenorhabditis elegans and establish a persistent lethal infection in the C. elegans intestinal track. Importantly, key components of Candida pathogenesis in mammals, such as filament formation, are also involved in nematode killing. We devised a Candida-mediated C. elegans assay that allows high-throughput in vivo screening of chemical libraries for antifungal activities, while synchronously screening against toxic compounds. The assay is performed in liquid media using standard 96-well plate technology and allows the study of C. albicans in non-planktonic form. A screen of 1,266 compounds with known pharmaceutical activities identified 15 (approximately 1.2% that prolonged survival of C. albicans-infected nematodes and inhibited in vivo filamentation of C. albicans. Two compounds identified in the screen, caffeic acid phenethyl ester, a major active component of honeybee propolis, and the fluoroquinolone agent enoxacin exhibited antifungal activity in a murine model of candidiasis. The whole-animal C. elegans assay may help to study the molecular basis of C. albicans pathogenesis and identify antifungal compounds that most likely would not be identified by in vitro screens that target fungal growth. Compounds identified in the screen that affect the virulence of Candida in vivo can potentially be used as "probe compounds" and may have antifungal activity against other fungi.

  14. Mosquitocidal, nematicidal, and antifungal compounds from Apium graveolens L. seeds.

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    Momin, R A; Nair, M G

    2001-01-01

    The methanolic extract of Apium graveolens seeds was investigated for bioactive compounds and resulted in the isolation and characterization of mosquitocidal, nematicidal, and antifungal compounds sedanolide (1), senkyunolide-N (2), and senkyunolide-J (3). Their structures were determined by 1H and 13C NMR spectral methods. Compounds 1-3 gave 100% mortality at 25, 100, and 100 microg mL(-1), respectively, on the nematode, Panagrellus redivivus. Compound 1 showed 100% mortality at 50 microg mL(-1) on nematode, Caenorhabditis elegans, and fourth-instar mosquito larvae, Aedes aegyptii. Also, it inhibited the growth of Candida albicans and Candida parapsilasis at 100 microg mL(-1). Compounds 2 and 3 were isolated for the first time from A. graveolens. This is the first report of the mosquitocidal, nematicidal, and antifungal activities of compounds 1-3.

  15. Avocado roots treated with salicylic acid produce phenol-2,4-bis (1,1-dimethylethyl), a compound with antifungal activity.

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    Rangel-Sánchez, Gerardo; Castro-Mercado, Elda; García-Pineda, Ernesto

    2014-02-15

    We demonstrated the ability of salicylic acid (SA) to induce a compound in avocado roots that strengthens their defense against Phytophthora cinnamomi. The SA content of avocado roots, before and after the application of exogenous SA, was determined by High-Performance Liquid Chromatography (HPLC). After 4h of SA feeding, the endogenous level in the roots increased to 223 μg g(-1) FW, which was 15 times the amount found in control roots. The methanolic extract obtained from SA-treated avocado roots inhibited the radial growth of P. cinnamomi. A thin layer chromatographic bioassay with the methanolic extract and spores of Aspergillus showed a distinct inhibition zone. The compound responsible for the inhibition was identified as phenol-2,4-bis (1,1-dimethylethyl) by gas chromatography and mass spectrometry. At a concentration of 100 μg/mL, the substance reduced germinative tube length in Aspergillus and radial growth of P. cinnamomi. A commercial preparation of phenol-2,4-bis (1,1-dimethylethyl) caused the same effects on mycelium morphology and radial growth as our isolate, confirming the presence of this compound in the root extracts. This is the first report of the induction of this compound in plants by SA, and the results suggest that it plays an important role in the defense response of avocado. Copyright © 2013 Elsevier GmbH. All rights reserved.

  16. Anticancer and antifungal compounds from Aspergillus, Penicillium and other filamentous fungi

    DEFF Research Database (Denmark)

    Bladt, Tanja Thorskov; Frisvad, Jens Christian; Knudsen, Peter Boldsen

    2013-01-01

    This review covers important anticancer and antifungal compounds reported from filamentous fungi and in particular from Aspergillus, Penicillium and Talaromyces. The taxonomy of these fungi is not trivial, so a focus of this review has been to report the correct identity of the producing organisms...

  17. Bioautography indicates the multiplicity of antifungal compounds ...

    African Journals Online (AJOL)

    AJB SERVER

    2006-09-18

    Sep 18, 2006 ... 199 active compounds, followed by methanol (189) and hexane (73). This difference is apparently not related to the sectional division of the species (Carr, 1988). Comparison of eluent systems. Lastly we determined which TLC solvent system separa- ted the highest number of active compounds (Table 27).

  18. Laccase catalyzed synthesis of iodinated phenolic compounds with antifungal activity.

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    Julian Ihssen

    Full Text Available Iodine is a well known antimicrobial compound. Laccase, an oxidoreductase which couples the one electron oxidation of diverse phenolic and non-phenolic substrates to the reduction of oxygen to water, is capable of oxidizing unreactive iodide to reactive iodine. We have shown previously that laccase-iodide treatment of spruce wood results in a wash-out resistant antimicrobial surface. In this study, we investigated whether phenolic compounds such as vanillin, which resembles sub-structures of softwood lignin, can be directly iodinated by reacting with laccase and iodide, resulting in compounds with antifungal activity. HPLC-MS analysis showed that vanillin was converted to iodovanillin by laccase catalysis at an excess of potassium iodide. No conversion of vanillin occurred in the absence of enzyme. The addition of redox mediators in catalytic concentrations increased the rate of iodide oxidation ten-fold and the yield of iodovanillin by 50%. Iodinated phenolic products were also detected when o-vanillin, ethyl vanillin, acetovanillone and methyl vanillate were incubated with laccase and iodide. At an increased educt concentration of 0.1 M an almost one to one molar ratio of iodide to vanillin could be used without compromising conversion rate, and the insoluble iodovanillin product could be recovered by simple centrifugation. The novel enzymatic synthesis procedure fulfills key criteria of green chemistry. Biocatalytically produced iodovanillin and iodo-ethyl vanillin had significant growth inhibitory effects on several wood degrading fungal species. For Trametes versicolor, a species causing white rot of wood, almost complete growth inhibition and a partial biocidal effect was observed on agar plates. Enzymatic tests indicated that the iodinated compounds acted as enzyme responsive, antimicrobial materials.

  19. Antifungal and antibacterial compounds from Streptomyces strains ...

    African Journals Online (AJOL)

    In addition, antibacterial activity of this strain was determined against human pathogenic bacteria such as. Staphylococcus aureus, Klebsiella pneumoniae, Kocuria ... aureus (MRSA). The present results indicate that isolate KEH23 is a potential antibiotic producer agent for the biocontrol of plant and human pathogens.

  20. Antifungal compound produced by the cassava endophyte Bacillus pumilus MAIIIM4a Composto antifúngico produzido pelo endófito de mandioca Bacillus pumilus MAIIIM4a

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    Flávia Mandolesi Pereira de Melo

    2009-10-01

    Full Text Available In the search for new organisms and new secondary metabolites, a study was conducted to evaluate the diversity of endophytic bacteria from ethnovarieties of cassava cultivated by Brazilian Amazon Indian tribes and also to study the secondary metabolites produced by a Bacillus pumilus strain. Sixty seven cassava endophytic bacteria were subjected to 16S rRNA sequencing and FAME analysis. The bacterial profile revealed that 25% of all endophytic isolates belonged to the genus Bacillus. The isolate B. pumilus MAIIIM4a showed a strong inhibitory activity against the fungi Rhizoctonia solani, Pythium aphanidermatum and Sclerotium rolfsii. Secondary metabolites of this strain were extracted using hexane, dichloromethane and ethyl acetate. Extracts were subjected to bioautography and LC/MS analysis, which allowed the identification of pumilacidin, an antifungal compound produced by B. pumilus MAIIIM4a. The bacterial endophytic localization was confirmed by cassava cell tissue examination using scanning electron microscopy.Na busca de novos organismos e novos metabólitos secundários, um estudo foi conduzido visando avaliar a diversidade de bactérias endofíticas de etnovariedades de mandioca cultivadas por tribos indígenas da Amazônia brasileira e também para estudar metabólitos secundários produzidos por Bacillus pumilus. Sessenta e sete bactérias endofíticas de mandioca foram identificadas através do seqüenciamento do gene 16S rRNA e por meio da análise de ácidos graxos (FAME. Essas análises revelaram que 25% de todos os endofíticos pertenciam ao gênero Bacillus. O isolado Bacillus pumilus MAIIIM4a apresentou forte ação inibitória contra os fitopatógenos Rhizoctonia solani, Pythium aphanidermatum e Sclerotium rolfsii. Os metabólitos secundários deste isolado foram extraídos do sobrenadante usando-se hexano, diclorometano e acetato de etila. Esses extratos foram utilizados nas análises de bioautografia e LC-MS, as quais

  1. Natural antifungal compounds from the peels of Ipomoea batatas Lam.

    Science.gov (United States)

    Oluyori, Abimbola P; Shaw, Arun Kumar; Preeti, Rastogi; Reddy, Sammajay; Atolani, Olubunmi; Olatunji, Gabriel A; Fabiyi, Oluwatoyin A

    2016-09-01

    Three antifungal compounds have been isolated for the first time from the peels of Ipomoea batatas Lam. Their structures were established on the basis of 1D and 2D NMR spectra data as well as ESI-MS and IR analysis. Urs-13(18)-ene-3β-yl acetate was found to possess a weak activity against Sporothrix schenckii and Trichophyton metagrophytes fungi with an MIC value of 50 μg/mL each. Stigmasterol and 3-friedelanol were equally active against T. metagrophytes.

  2. Novel Antifungal Compounds Discovered in Medicines for Malaria Venture's Malaria Box.

    Science.gov (United States)

    Jung, Eric H; Meyers, David J; Bosch, Jürgen; Casadevall, Arturo

    2018-01-01

    Similarities in fungal and animal cells make antifungal discovery efforts more difficult than those for other classes of antimicrobial drugs. Currently, there are only three major classes of antifungal drugs used for the treatment of systemic fungal diseases: polyenes, azoles, and echinocandins. Even in situations where the offending fungal organism is susceptible to the available drugs, treatment courses can be lengthy and unsatisfactory, since eradication of infection is often very difficult, especially in individuals with impaired immunity. Consequently, there is a need for new and more effective antifungal drugs. We have identified compounds with significant antifungal activity in the Malaria Box (Medicines for Malaria Ventures, Geneva, Switzerland) that have higher efficacy than some of the currently used antifungal drugs. Our best candidate, MMV665943 (IUPAC name 4-[6-[[2-(4-aminophenyl)-3H-benzimidazol-5-yl]methyl]-1H-benzimidazol-2-yl]aniline), here referred to as DM262, showed 16- to 32-fold-higher activity than fluconazole against Cryptococcus neoformans . There was also significant antifungal activity in other fungal species with known antifungal resistance, such as Lomentospora prolificans and Cryptococcus gattii . Antifungal activity was also observed against a common fungus, Candida albicans . These results are important because they offer a potentially new class of antifungal drugs and the repurposing of currently available therapeutics. IMPORTANCE Much like the recent increase in drug-resistant bacteria, there is a rise in antifungal-resistant strains of pathogenic fungi. There is a need for novel and more potent antifungal therapeutics. Consequently, we investigated a mixed library of drug-like and probe-like compounds with activity in Plasmodium spp. for activity against two common fungal pathogens, Cryptococcus neoformans and Candida albicans , along with two less common pathogenic species, Lomentospora prolificans and Cryptococcus gattii . We

  3. Antifungal activity of extracts and phenolic compounds from ...

    African Journals Online (AJOL)

    STORAGESEVER

    2009-06-17

    Jun 17, 2009 ... (naringin, rutin, luteolin and kaempferol). The results of present study provide scientific basis for the use of the plant extract in the future development as antifungal, antibacterial, antioxidant and anti- inflammatory agent. Key words: Barringtonia racemosa, antifungal, HPLC, phenolic acids, flavonoids.

  4. Screening of pharmacologically active small molecule compounds identifies antifungal agents against Candida biofilms

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    Takao eWatamoto

    2015-12-01

    Full Text Available Candida species have emerged as important and common opportunistic human pathogens, particularly in immunocompromised individuals. The current antifungal therapies either have toxic side effects or are insufficiently effect. The aim of this study is develop new small-molecule antifungal compounds by library screening methods using C. albicans, and to evaluate their antifungal effects on Candida biofilms and cytotoxic effects on human cells. Wild-type C. albicans strain SC5314 was used in library screening. To identify antifungal compounds, we screened a small-molecule library of 1,280 pharmacologically active compounds (LOPAC1280TM using an antifungal susceptibility test (AST. To investigate the antifungal effects of the hit compounds, ASTs were conducted using Candida strains in various growth modes, including biofilms. We tested the cytotoxicity of the hit compounds using human gingival fibroblast (hGF cells to evaluate their clinical safety. Only 35 compounds were identified by screening, which inhibited the metabolic activity of C. albicans by >50%. Of these, 26 compounds had fungistatic effects and 9 compounds had fungicidal effects on C. albicans. Five compounds, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate, ellipticine and CV-3988, had strong fungicidal effects and could inhibit the metabolic activity of Candida biofilms. However, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine were cytotoxic to hGF cells at low concentrations. CV-3988 showed no cytotoxicity at a fungicidal concentration.Four of the compounds identified, BAY11-7082, BAY11-7085, sanguinarine chloride hydrate and ellipticine, had toxic effects on Candida strains and hGF cells. In contrast, CV-3988 had fungicidal effects on Candida strains, but low cytotoxic effects on hGF cells. Therefore, this screening reveals agent, CV-3988 that was previously unknown to be antifungal agent, which could be a novel therapies for superficial mucosal

  5. VOLATILE COMPOUNDS IN THE AROMA OF THREE SPECIES OF WOOD-ROTTING BASIDIOMYCETES AND THEIR ANTIFUNGAL POTENTIAL

    Directory of Open Access Journals (Sweden)

    Cristiana Virginia PETRE

    2017-12-01

    Full Text Available This study aims to determine the volatile organic compounds synthesized by three species of wood-rotting basidiomycetes: Coriolopsis gallica, Megacollybia platyphylla and Lentinus arcularius and test their antifungal potential. The species were cultivated on liquid media and kept for 25 days at 25 °C. The surface cultures were then homogenized, filtrated and extracted using solid-phase extraction and analyzed by GC-MS. The volatile compounds identified were mainly alcohols, ketones, aldehydes and terpenes. The most common volatiles identified in the experiment are: 1-octen-3-ol, 3-hexanol, 3-methyl-1-butanol, 3-octanone, 2-hexanone, benzaldehyde, and limonene. The volatiles metabolites of these species were tested for their antifungal activity using the bi-compartmented Petri dishes method against two species of plant pathogenic fungi: Fusarium solani and Sclerotinia sclerotiorum, on three media. The volatiles produced by Coriolopsis gallica showed the highest antifungal potential against the phytopathogens. The results revealed the importance of media composition in the synthesis of antifungal volatile compounds.

  6. Purification and Identification of Two Antifungal Cyclic Peptides Produced by Bacillus amyloliquefaciens L-H15.

    Science.gov (United States)

    Han, Yuzhu; Zhang, Bao; Shen, Qian; You, Chengzhen; Yu, Yaqiong; Li, Pinglan; Shang, Qingmao

    2015-08-01

    Bacillus amyloliquefaciens L-H15 with broad spectrum antifungal activity was used as a biocontrol agent to suppress Fusarium oxysporum and other soil-borne fungal plant pathogens. Two antifungal fractions were isolated by bioactivity-guided reversed-phase high-performance liquid chromatography. The two compounds were identified by tandem Q-TOF mass spectroscopy as C15 Iturin A (1) and a novel cyclic peptide with a molecular weight of 852.4 Da (2). Both compounds showed good inhibitory activities against three plant fungal pathogens in cylinder-plate diffusion assay. To our best knowledge, this is the first report on a cyclic antifungal peptide with a molecular weight of 852.4 Da. The strong antifungal activity suggests that the B. amyloliquefaciens L-H15 and its bioactive components might provide an alternative resource for the biocontrol of plant diseases and sustainable agriculture.

  7. Antifungal activity of extracts and isolated compounds from Buchenavia tomentosa on Candida albicans and non-albicans.

    Science.gov (United States)

    Teodoro, Guilherme R; Brighenti, Fernanda L; Delbem, Alberto C Botazzo; Delbem, Ádina Cléia B; Khouri, Sonia; Gontijo, Aline Vidal L; Pascoal, Aislan Crf; Salvador, Marcos J; Koga-Ito, Cristiane Y

    2015-01-01

    This study aimed to evaluate the antifungal activity of Buchenavia tomentosa extract and bioactive compounds on six Candida species. The antimicrobial activity of extract was evaluated using standard strains and clinical isolates. Cytotoxicity was tested in order to evaluate cell damage caused by the extract. Extract was chemically characterized and the antifungal activity of its compounds was evaluated. Extract showed antifungal activity on Candida species. Candida non-albicans were more susceptible than Candida albicans. Low cytotoxicity for extract was observed. The isolated compounds presented antifungal activity at least against one Candida spp. and all compounds presented antifungal effect on Candida glabrata. Extracts from Buchenavia tomentosa showed promising antifungal activity on Candida species with low cytotoxicity. Gallic acid, corilagin and ellagic acid showed promising inhibitory activity on Candida glabrata.

  8. A non-polyenic antifungal produced by a Streptomyces yatensis strain isolated from Mellah Lake in El Kala, North-East of Algeria.

    Science.gov (United States)

    Benouagueni, S; Ranque, S; Gacemi Kirane, D

    2015-03-01

    This study aimed at describing one actinomycete strain E65 that was isolated from the water of Mellah Lake in El Kala, North-East of Algeria that produces a non-polyenic antifungal. Actinomycetes were isolated from Mellah Lake water and screened for antimicrobial activity. Antimicrobial assays were performed on ISP2 agar. The taxonomic position of the strain E65 was determined regarding phenotypic and 16S DNA sequences features. Time course of antifungal metabolites production was evaluated against Candida albicans on ISP2, ISP1 and GYEA broth. The active antifungal compound was extracted using dichloromethane and revealed by a thin layer of chromatography, chemical reagents, UV-visible and infrared spectroscopy. A total of 104 actinomycetes were isolated and screened for antimicrobial activity; 21 strains were active against Staphylococcus aureus, Escherichia coli and Candida albicans. The strain E65 showed a high in vitro activity against S. aureus and C. albicans and a good antifungal activity against a clinical C. albicans strain resistant to 5-fluorocytosine. Its 16S rRNA sequence shared 99% similarity with the Streptomyces yatensis type strain within the Streptomyces violaceusniger subclade of the Streptomyces hygroscopicus clade. It produced a non-polyenic antifungal, the IR spectrum of the antifungal extract corresponded to none of the antimicrobials compounds known to be produced by actinomycete of the S. hygroscopicus clade. The wetlands of El Kala, Algeria are a potential source of bioactive actinomycete that deserves to be explored and exploited. The Streptomyces yatensis E65 strain isolated from Mellah Lake brackish water produces a remarkable antifungal compound which original non-polyenic structure warrants further characterization. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  9. Isolation and identification of an antifungal compound from endophytic Streptomyces sp. CEN26 active against Alternaria brassicicola.

    Science.gov (United States)

    Phuakjaiphaeo, C; Chang, C I; Ruangwong, O; Kunasakdakul, K

    2016-07-01

    2,5-Bis(hydroxymethyl)furan monoacetate (BHMF-OAc) compound was isolated from the culture filtrate secreted by Streptomyces sp. CEN26, an endophytic actinomycete found in the root nodes of Centella asiatica (L.) Urban. The compound was purified using various chromatographic techniques and bioassay-guided fractionation. The compound was then identified through a structural characterization using (1) H, (13) C-NMR and MS analysis. After the purification and identification process, a series of experiments were conducted in order to test whether the compound affected conidial germination of Alternaria brassicicola. Findings show that the compound inhibited and deformed the conidial germination of A. brassicicola. Its minimal inhibitory concentrations of MIC90 and MIC50 were found to be 100 and 25 ppm respectively. Further experimentation show that the aforementioned concentrations of MIC90 and MIC50 completely suppressed the appressorium formation of the fungal pathogen. Therefore, the BHMF-OAc compound does have antifungal properties that help protect plants from infection by A. brassicicola. Endophytic Streptomyces sp. CEN26 produces 2,5-bis(hydroxymethyl)furan monoacetate (BHMF-OAc), which is a compound that inhibits the infection process of Alternaria brassicicola in cabbage. Such an antifungal property would allow for the use of the BHMF-OAc as an alternative to chemical fungicides. © 2016 The Society for Applied Microbiology.

  10. Lipopeptides, a novel protein, and volatile compounds contribute to the antifungal activity of the biocontrol agent Bacillus atrophaeus CAB-1.

    Science.gov (United States)

    Zhang, Xiaoyun; Li, Baoqing; Wang, Ye; Guo, Qinggang; Lu, Xiuyun; Li, Shezeng; Ma, Ping

    2013-11-01

    Bacillus atrophaeus CAB-1 displays a high inhibitory activity against various fungal pathogens and suppresses cucumber powdery mildew and tomato gray mold. We extracted and identified lipopeptides and secreted proteins and volatile compounds produced by strain CAB-1 to investigate the mechanisms involved in its biocontrol performance. In vitro assays indicated all three types of products contributed to the antagonistic activity against the fungal pathogen Botrytis cinerea. Each of these components also effectively prevented the occurrence of the cucumber powdery mildew caused by Sphaerotheca fuliginea under greenhouse conditions. Matrix-assisted laser desorption ionization time-of-flight mass spectrometry revealed that the major bioactive lipopeptide was fengycin A (C15-C17). We isolated the crude-secreted proteins of CAB-1 and purified a fraction with antifungal activity. This protein sequence shared a high identity with a putative phage-related pre-neck appendage protein, which has not been reported as an antifungal factor. The volatile compounds produced by CAB-1 were complex, including a range of alcohols, phenols, amines, and alkane amides. O-anisaldehyde represented one of the most abundant volatiles with the highest inhibition on the mycelial growth of B. cinerea. To our knowledge, this is the first report on profiling three types of antifungal substances in Bacilli and demonstrating their contributions to plant disease control.

  11. The Sesamum indicum rhizosphere associated bacterium: A source of Antifungal compound.

    Science.gov (United States)

    Chaudhary, Renu; Balhara, Meenakshi; Jangir, Deepak; Dangi, Mrridula; Dangi, Mehak; Khatri, Savita; Chhillar, Anil K

    2018-02-05

    The impact of fungal infections on human health has increased considerably within a past few decades. Although drugs with antifungal properties are available, but they are less effective and are associated with side effects. Screening of bacterial isolates from Sesamum indicum and to investigate the antifungal activity of the screened bacterial isolates against Aspergillus sp. Co-culture assay and agar overlay were used to scrutinize the anti-Aspergillus activity. Furthermore, optimization ofmedia and growth conditions to enhance the production of anti-Aspergillus compound. Several bacterial cultures were isolated from Sesamum indicum rhizosphere collected from Mandi (H.P.) India. These bacterial cultures were assayed for antifungal activity against Aspergillus species i.e. A. fumigatus and A. niger. Two most potent strains were chosen for more detailed analyses. The biochemical characterization and 16S ribosomal RNA sequencing revealed that Burkholderia sp. strain RC1 and Acinetobacter pittii strain RC2 exhibits strong similarity (100%) with Burkholderia sp. SR2-07 and Acinetobacter sp. strain 3-59. Additionally, it was also validated that RC1 and RC2 showed significant difference in the production of anti-Aspergillusactivity under altered growth conditions. Results from this study recommends that plant rhizosphere remains a rich hotspot for delivering a novel antifungal compounds. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  12. Antifungal compounds from turmeric and nutmeg with activity against plant pathogens.

    Science.gov (United States)

    Radwan, Mohamed M; Tabanca, Nurhayat; Wedge, David E; Tarawneh, Amer H; Cutler, Stephen J

    2014-12-01

    The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides. Among the active extracts, turmeric and nutmeg were the most active and were chosen for further investigation. The bioassay-guided fractionation led to the isolation of three compounds from turmeric (1-3) and three compounds from nutmeg (4-6). Their chemical structures were elucidated by spectroscopic analysis including HR-MS, 1D, and 2D NMR as curcumin (1), demethoxycurcumin (2) and bisdemethoxy-curcumin (3), erythro-(7R,8R)-Δ(8')-4,7-dihydroxy-3,3',5'-trimethoxy-8-O-4'-neolignan (4), erythro-(7R,8R)-Δ8'-7-acetoxy-3,4,3',5'-tetra-methoxy-8-O-4'-neolignan (5), and 5-hydroxy-eugenol (6). The isolated compounds were subsequently evaluated using a 96-well microbioassay against plant pathogens. At 30 μM, compounds 2 and 3 possessed the most antifungal activity against Phomopsis obscurans and Phomopsis viticola, respectively. Copyright © 2014. Published by Elsevier B.V.

  13. The diversity of antifungal compounds of six South African ...

    African Journals Online (AJOL)

    sambesiaca) were tested against five fungal animal pathogens (Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus, Microsporum canis and Sporothrix schenkii). The Rf values and relative activities of separated compounds were determined. Hexane and dichloromethane extracts had at least three times ...

  14. Antibacterial and antifungal activity of sulfur-containing compounds from Petiveria alliacea L.

    Science.gov (United States)

    Kim, Seokwon; Kubec, Roman; Musah, Rabi A

    2006-03-08

    A total of 18 organosulfur compounds originating from Petiveria alliacea L. roots have been tested for their antibacterial and antifungal activities. These represent compounds occurring in fresh homogenates as well as those present in various macerates, extracts and other preparations made from Petiveria alliacea. Of the compounds assayed, the thiosulfinates, trisulfides and benzylsulfinic acid were observed to be the most active, with the benzyl-containing thiosulfinates exhibiting the broadest spectrum of antimicrobial activity. The effect of plant sample preparation conditions on the antimicrobial activity of the extract is discussed.

  15. Synthesis and preliminary evaluation of N-acylhydrazone compounds as antibacterial and antifungal agents

    International Nuclear Information System (INIS)

    Cachiba, Thomas Haruo; Carvalho, Bruno Demartini; Carvalho, Diogo Teixeira; Cusinato, Marina; Prado, Clara Gaviao; Dias, Amanda Latercia Tranches

    2012-01-01

    We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC 50 values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 μM), C. krusei (34 μM) and C. tropicalis (17 μM). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents. (author)

  16. Candidacidal Action of CF66I, an Antifungal Compound Produced ...

    African Journals Online (AJOL)

    Erah

    fungal cell wall components, and then affected the normal structure of fungal cell wall and induced cell wall thickening, which was confirmed by transmission electron microscopy (TEM) CF66I also exerted its candidacidal activity against cell membrane, eventually induced K+ release from C. albicans and PI uptake.

  17. Candidacidal Action of CF66I, an Antifungal Compound Produced ...

    African Journals Online (AJOL)

    -1,6-glucan, one of fungal cell wall components, and then affected the normal structure of fungal cell wall and induced cell wall thickening, which was confirmed by transmission electron microscopy (TEM) CF66I also exerted its candidacidal ...

  18. Discovery of a Novel Dibromoquinoline Compound Exhibiting Potent Antifungal and Antivirulence Activity That Targets Metal Ion Homeostasis.

    Science.gov (United States)

    Mohammad, Haroon; Elghazawy, Nehal H; Eldesouky, Hassan E; Hegazy, Youssef A; Younis, Waleed; Avrimova, Larisa; Hazbun, Tony; Arafa, Reem K; Seleem, Mohamed N

    2018-03-09

    Globally, invasive fungal infections pose a significant challenge to modern human medicine due to the limited number of antifungal drugs and the rise in resistance to current antifungal agents. A vast majority of invasive fungal infections are caused by species of Candida, Cryptococcus, and Aspergillus. Novel antifungal molecules consisting of unexploited chemical scaffolds with a unique mechanism are a pressing need. The present study identifies a dibromoquinoline compound (4b) with broad-spectrum antifungal activity that inhibits the growth of pertinent species of Candida (chiefly C. albicans), Cryptococcus, and Aspergillus at a concentration of as low as 0.5 μg/mL. Furthermore, 4b, at a subinhibitory concentration, interfered with the expression of two key virulence factors (hyphae and biofilm formation) involved in C. albicans pathogenesis. Three yeast deletion strains ( cox17Δ, ssa1Δ, and aft2Δ) related to metal ion homeostasis were found to be highly sensitive to 4b in growth assays, indicating that the compound exerts its antifungal effect through a unique, previously unexploited mechanism. Supplementing the media with either copper or iron ions reversed the strain sensitivity to 4b, further corroborating that the compound targets metal ion homeostasis. 4b's potent antifungal activity was validated in vivo, as the compound enhanced the survival of Caenorhabditis elegans infected with fluconazole-resistant C. albicans. The present study indicates that 4b warrants further investigation as a novel antifungal agent.

  19. Radiation-induced mutagenesis of antifungal metabolite producing bacillus sp. HKA-17

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Young Keun; Senthilkumar, M. [Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of)

    2009-09-15

    Bacillus sp. Strain HKA-17, isolated from the surface sterilized root nodule of Glycine max, inhibited several fungal plant pathogens. It produced a diffusible extracellular antifungal metabolite that was extracted with n-butanol. The crude extract was purified through Superdex{sup TM} 75 10/300 GL FPLC column. FT-IR spectrum of the FPLC purified-antifungal metabolite confirmed the presence of peptide and glycosidic bonds in its structure. Gamma induced mutagenesis of HKA-17 was carried out at an LD{sub 99} dose (8.46 kGy) to generate a mutant library. By screening the mutant library through a duel plate assay with Alternaria alternata, we selected one mutant with enhanced biocontrol activity (HKA-17e1) and two defective mutants (HKA-17d1 and HKA-17d2). Overproducing mutant recorded the largest inhibition zone (16.25 {+-} 0.86 mm) compared to any other mutant clone as well as wild type, and could be used as a potential biocontrol agent for plant disease suppression. The effect of HKA-17 antifungal metabolite on hyphal morphology was clearly demonstrated through scanning electron microscopy. The crude extract of defective mutant HKA-17 d1 did not induce any changes in hyphal morphology of A. alternata. However, antifungal metabolites of HKA-17 induced abnormal hyphal structures such as hyphal shrivelling, the bulging and swelling of intercalary cells, fragmentation, and cell lysis.

  20. Rapid identification of antifungal compounds against Exserohilum rostratum using high throughput drug repurposing screens.

    Directory of Open Access Journals (Sweden)

    Wei Sun

    Full Text Available A recent large outbreak of fungal infections by Exserohilum rostratum from contaminated compounding solutions has highlighted the need to rapidly screen available pharmaceuticals that could be useful in therapy. The present study utilized two newly-developed high throughput assays to screen approved drugs and pharmaceutically active compounds for identification of potential antifungal agents. Several known drugs were found that have potent effects against E. rostratum including the triazole antifungal posaconazole. Posaconazole is likely to be effective against infections involving septic joints and may provide an alternative for refractory central nervous system infections. The anti-E. rostratum activities of several other drugs including bithionol (an anti-parasitic drug, tacrolimus (an immunosuppressive agent and floxuridine (an antimetabolite were also identified from the drug repurposing screens. In addition, activities of other potential antifungal agents against E. rostratum were excluded, which may avoid unnecessary therapeutic trials and reveals the limited therapeutic alternatives for this outbreak. In summary, this study has demonstrated that drug repurposing screens can be quickly conducted within a useful time-frame. This would allow clinical implementation of identified alternative therapeutics and should be considered as part of the initial public health response to new outbreaks or rapidly-emerging microbial pathogens.

  1. In vitro antifungal activity of organic compounds derived from amino alcohols against onychomycosis

    Directory of Open Access Journals (Sweden)

    César Augusto Caneschi

    Full Text Available Abstract Onychomycosis is a fungal infection of the nail caused by high densities of filamentous fungi and yeasts. Treatment for this illness is long-term, and recurrences are frequently detected. This study evaluated in vitro antifungal activities of 12 organic compounds derived from amino alcohols against standard fungal strains, such as Trichophyton rubrum CCT 5507 URM 1666, Trichophyton mentagrophytes ATCC 11481, and Candida albicans ATCC 10231. The antifungal compounds were synthesized from p-hydroxybenzaldehyde (4a-4f and p-hydroxybenzoic acid (9a-9f. Minimum inhibitory concentrations and minimum fungicidal concentrations were determined according to Clinical and Laboratory Standards Institute protocols M38-A2, M27-A3, and M27-S4. The amine series 4b-4e, mainly 4c and 4e compounds, were effective against filamentous fungi and yeast (MIC from 7.8 to 312 µg/mL. On the other hand, the amide series (9a-9f did not present inhibitory effect against fungi, except amide 9c, which demonstrated activity only against C. albicans. This allowed us to infer that the presence of amine group and intermediate carbon number (8C-11C in its aliphatic side chain seems to be important for antifungal activity. Although these compounds present cytotoxic activity on macrophages J774, our results suggest that these aromatic compounds might constitute potential as leader molecules in the development of more effective and less toxic analogs that could have considerable implications for future therapies of onychomycosis.

  2. Bioactivity-guided isolation and structural characterization of the antifungal compound, plumbagin, from Nepenthes gracilis.

    Science.gov (United States)

    Gwee, Pei Shing; Khoo, Kong Soo; Ong, Hean Chooi; Sit, Nam Weng

    2014-12-01

    Despite several phytochemical studies of Nepenthes gracilis Korth (Nepenthaceae), the biological activities of this pitcher plant remain to be explored. This study evaluates the antifungal activity of N. gracilis extracts, isolates, and characterizes its bioactive compound and evaluates the cytotoxicity of the isolated compound. Fresh leaves of N. gracilis were sequentially extracted. The fungistatic and fungicidal activities of the extracts were evaluated against six species of fungi of medical importance using a colorimetric broth microdilution method. The most active extract was fractionated by liquid-liquid partitioning and further purified by a preparative thin layer chromatography. Structural elucidation was carried out using FT-IR, GC-MS, and NMR. Cytotoxicity testing against rhesus monkey kidney epithelial cells (LLC-MK2) was assessed by a neutral red uptake (NRU) assay. The hexane extract, which showed the lowest minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC), both at 20 μg/mL against Candida albicans, Issatchenkia orientalis, and Trichophyton mentagrophytes, was subjected to bioactivity-guided fractionation. The isolated compound exhibited potent activity with the MIC values ranging from 2 to 31 μg/mL against all the fungi. The active compound was identified as plumbagin (5-hydroxy-2-methyl-naphthalene-1,4-dione). The 50% cytotoxicity concentration (CC50) of plumbagin was 0.60 μg/mL. The selectivity indices of plumbagin against all the fungi were less than 1.0, indicating that plumbagin is more toxic to mammalian than fungal cells. This study provides information on the antifungal properties of N. gracilis leaf extracts, as well as the antifungal and cytotoxicity properties of plumbagin.

  3. Biocontrol of Aspergillus species on peanut kernels by antifungal diketopiperazine producing Bacillus cereus associated with entomopathogenic nematode.

    Directory of Open Access Journals (Sweden)

    Sasidharan Nishanth Kumar

    Full Text Available The rhabditid entomopathogenic nematode associated Bacillus cereus and the antifungal compounds produced by this bacterium were evaluated for their activity in reducing postharvest decay of peanut kernels caused by Aspergillus species in in vitro and in vivo tests. The results showed that B. cereus had a significant effect on biocontrol effectiveness in in vitro and in vivo conditions. The antifungal compounds produced by the B. cereus were purified using silica gel column chromatography and their structure was elucidated using extensive spectral analyses. The compounds were identified as diketopiperazines (DKPs [cyclo-(L-Pro-Gly, cyclo(L-Tyr-L-Tyr, cyclo-(L-Phe-Gly and cyclo(4-hydroxy-L-Pro-L-Trp]. The antifungal activities of diketopiperazines were studied against five Aspergillus species and best MIC of 2 µg/ml was recorded against A. flavus by cyclo(4-hydroxy-L-Pro-L-Trp. To investigate the potential application of cyclo(4-hydroxy-L-Pro-L-Trp to eliminate fungal spoilage in food and feed, peanut kernels was used as a food model system. White mycelia and dark/pale green spores of Aspergillus species were observed in the control peanut kernels after 2 days incubation. However the fungal growth was not observed in peanut kernels treated with cyclo(4-hydroxy-L-Pro-L-Trp. The cyclo(4-hydroxy-L-Pro-L-Trp was nontoxic to two normal cell lines [fore skin (FS normal fibroblast and African green monkey kidney (VERO] up to 200 µg/ml in MTT assay. Thus the cyclo(4-hydroxy-L-Pro-L-Trp identified in this study may be a promising alternative to chemical preservatives as a potential biopreservative agent which prevent fungal growth in food and feed. To the best of our knowledge, this is the first report demonstrating that the entomopathogenic nematode associated B. cereus and cyclo(4-hydroxy-L-Pro-L-Trp could be used as a biocontrol agents against postharvest fungal disease caused by Aspergillus species.

  4. Selection of antifungal protein-producing molds from dry-cured meat products.

    Science.gov (United States)

    Acosta, Raquel; Rodríguez-Martín, Andrea; Martín, Alberto; Núñez, Félix; Asensio, Miguel A

    2009-09-30

    To control unwanted molds in dry-cured meats it is necessary to allow the fungal development essential for the desired characteristics of the final product. Molds producing antifungal proteins could be useful to prevent hazards due to the growth of mycotoxigenic molds. The objective has been to select Penicillium spp. that produce antifungal proteins against toxigenic molds. To obtain strains adapted to these products, molds were isolated from dry-cured ham. A first screening with 281 isolates by the radial inhibition assay revealed that 166 were active against some of the toxigenic P. echinulatum, P. commune, and Aspergillusniger used as reference molds. The activity of different extracts from cultured medium was evaluated by a microspectroscopic assay. Molds producing active chloroform extracts were eliminated from further consideration. A total of 16 Penicillium isolates were screened for antifungal activity from both cell-free media and the aqueous residues obtained after chloroform extraction. The cell-free media of 10 isolates that produced a strong inhibition of the three reference molds were fractionated by FPLC on a cationic column. For protein purification, the fractions of the three molds that showed high inhibitory activity were further chromatographed on a gel filtration column, and the subfractions containing the highest absorbance peaks were assayed against the most sensitive reference molds. One subfraction each from strains AS51D and RP42C from Penicilliumchrysogenum confirmed the inhibitory activity against the reference molds. SDS-PAGE revealed a single band from each subfraction, with estimated molecular masses of 37kDa for AS51D and 9kDa for RP42C. Although further characterisation is required, both these proteins and the producing strains can be of interest to control unwanted molds on foods.

  5. Antifungal iridoids, triterpenes and phenol compounds from Alibertia myrciifolia Sprunge Ex. Schum

    International Nuclear Information System (INIS)

    Luciano, Joao Henrique S.; Lima, Mary Anne S.; Silveira, Edilberto Rocha; Vasconcelos, Ilka Maria; Fernandes, Georgia Sampaio; Souza, Elnatan Bezerra de

    2010-01-01

    The new iridoid glucoside 10-O-vanilloyl-geniposidic acid has been isolated from the aerial parts of Alibertia myrciifolia along with hydroxyhopanone, 3α,22-dihydroxyhopane, ursolic acid, luteolin-3',4'-dimethyl ether, caffeic acid and geniposidic acid. The structures of the isolated compounds were determined by means of mass spectrometry and nuclear magnetic resonance spectral analyses. The antifungal activities of the iridoids 10-O-vanilloyl-geniposidic acid and geniposidic acid were evaluated against the phytopathogenic fungi strains Colletotrichum gloeosporioides, Fusarium solani and Aspergillus niger. (author)

  6. Identification of cyclic lipopeptides produced by Bacillus vallismortis R2 and their antifungal activity against Alternaria alternata.

    Science.gov (United States)

    Kaur, P K; Joshi, N; Singh, I P; Saini, H S

    2017-01-01

    To identify the different antifungal biomolecules produced by isolate Bacillus vallismortis R2 and analyse their effect on Alternaria alternata, a common pathogen causing black point disease of wheat. The different antifungal molecules produced by isolate R2 were purified by column chromatography. The liquid chromatography-mass spectrometry of purified fractions confirmed the ability of R2 to produce biomolecules putatively similar to three different families of cyclic lipopeptides (CLPs) viz. surfactins, iturins and fengycins. The synergistic interaction among CLPs was evident from significant increase in the antifungal activity of mixture of purified fractions as compared to that of the individual fractions by agar well diffusion assay. The evaluation of antifungal activity of purified fractions by 96-well microtitre plate assay showed that the fengycin-like molecules supported significantly higher antifungal activity against A. alternata than iturin A and no antifungal activity was supported by surfactin. The isolate R2, producing different CLPs, can be used as an environmental friendly alternative to chemical fungicides. Among the three different CLPs viz. surfactin, iturin A and fengycin produced by R2, the fengycins were the most active lipopeptides. This is the first report on co-production of three different types of CLPs by the cells of B. vallismortis. © 2016 The Society for Applied Microbiology.

  7. Identification of antifungal compounds active against Candida albicans using an improved high-throughput Caenorhabditis elegans assay.

    Directory of Open Access Journals (Sweden)

    Ikechukwu Okoli

    2009-09-01

    Full Text Available Candida albicans, the most common human pathogenic fungus, can establish a persistent lethal infection in the intestine of the microscopic nematode Caenorhabditis elegans. The C. elegans-C. albicans infection model was previously adapted to screen for antifungal compounds. Modifications to this screen have been made to facilitate a high-throughput assay including co-inoculation of nematodes with C. albicans and instrumentation allowing precise dispensing of worms into assay wells, eliminating two labor-intensive steps. This high-throughput method was utilized to screen a library of 3,228 compounds represented by 1,948 bioactive compounds and 1,280 small molecules derived via diversity-oriented synthesis. Nineteen compounds were identified that conferred an increase in C. elegans survival, including most known antifungal compounds within the chemical library. In addition to seven clinically used antifungal compounds, twelve compounds were identified which are not primarily used as antifungal agents, including three immunosuppressive drugs. This assay also allowed the assessment of the relative minimal inhibitory concentration, the effective concentration in vivo, and the toxicity of the compound in a single assay.

  8. Motile zoospores of Batrachochytrium dendrobatidis move away from antifungal metabolites produced by amphibian skin bacteria.

    Science.gov (United States)

    Lam, Brianna A; Walton, D Brian; Harris, Reid N

    2011-03-01

    Chytridiomycosis is an amphibian skin disease that threatens amphibian biodiversity worldwide. The fungal agent of chytridiomycosis is Batrachochytrium dendrobatidis. There is considerable variation in disease outcomes such that some individuals and populations co-exist with the fungus and others quickly succumb to disease. Amphibians in populations that co-exist with the B. dendrobatidis have sublethal infections on their skins. Symbiotic skin bacteria have been shown in experiments and surveys to play a role in protecting amphibians from chytridiomycosis. Little is known about the mechanisms that antifungal skin bacteria use to ameliorate the effects of B. dendrobatidis. In this study, we identified that B. dendrobatidis isolate JEL 310 zoospores display chemotaxis, in the presence of two bacterially-produced metabolites (2,4-diacetylphloroglucinol and indole-3-carboxaldehyde). In the presence of either metabolite, B. dendrobatidis zoospores move more frequently away from the metabolite. Using parameters estimated from this study, a simple stochastic model of a random walk on a lattice was evaluated. The model shows that these individual behaviors over short time-scales directly lead to population behaviors over long time-scales, such that most zoospores will escape, or not infect a tryptone substrate containing the bacterially-produced metabolite, whereas many zoospores will infect the tryptone substrate containing no metabolite. These results suggest that amphibians that have skin bacteria produce antifungal metabolites that might be able to keep B. dendrobatidis infections below the lethal threshold and thus are able to co-exist with the fungus.

  9. Antifungal activity of low molecular weight chitosan produced from non-traditional marine resources

    Directory of Open Access Journals (Sweden)

    Francisco Pires Avelelas

    2014-06-01

    Full Text Available The four plants pathogens, Botrytis cinerea, Phytophthora cinnamomi, Cryphonectria parasitica and Heterobasidion annosum are responsible for several diseases affecting different plant species in Portugal, such as pines (H. annosum, chestnuts (P. cinnamomi and C. parasitica and eucalyptus (B. cinerea. These pathogens incurs in large economic losses, and ultimately causes the death of these plants. The use of biopolymers as antimicrobial agents, such as chitosan (derived from chitin, is increasing, in order to reduce the negative impact of conventional chemical treatments on the environment, avoiding health risks. Therefore, eco-friendly polymers were produced through (1 N-acetylation with addition of acetic anhydride and (2 hydrogen peroxide of chitosan samples, obtained from two different sources: shrimp (commercial chitosan and swimming crab bycatch specie Polybius henslowii. The chemical structure and molecular weight of the prepared chitosan derivatives, water soluble chitosan (WSC and chitooligosaccharides (COS, was confirmed by Fourier Transform Infrared (FT-IR and Gel Permeation Chromatography (GPC and their antifungal activity evaluated against Botrytis cinerea, Phytophthora cinnamomi, Cryphonectria parasitica and Heterobasidion annosum. The concentration range varied from 0.0125 to 0.1 mg/mL and inhibition percentages were determined by differences in radial growth on the agar plates for all species. Although not all species tested exhibited equal vulnerability towards the concentrations range, antifungal activity of chitosan samples proved to be dependent, increasing the inhibitory capacity with lower concentrations. The results obtained support the use of chitosan fromPolybius henslowii when compared with commercial chitosan with shrimp towards antifungal approaches, suggesting that chitin producers can rely on this crab waste as a raw material for chitin extraction, adding value to this bycatch specie. Financial support was obtained

  10. Synthesis and anti-fungal activity of some new 1,2,4-Triazole and Furan containing compounds

    International Nuclear Information System (INIS)

    Shehata, Ihsan A.

    2003-01-01

    Several new 1, 2, 4-triazole analogs attached to substituted phenyl pyrrole or furan 5-membered heterocycles were synthesized and screened for their antifungal activity. Compounds 5, 6-dihydro-4-oxo-5-phenyl--4ph-furo[2, 3-c] pyrrole (11) and 3-(1-methyl-2-pyrrole methyl)-4-phenyl-5-(4-chlorophenylcarbamoyl methylthio)-1, 2, 4-triazole(16) showed a prominent activity against C.albicans and S.cerevisiae.The detailed synthesis and the antifungal screening are reported. (author)

  11. VOLATILE COMPOUNDS IN THE AROMA OF THREE SPECIES OF WOOD-ROTTING BASIDIOMYCETES AND THEIR ANTIFUNGAL POTENTIAL

    OpenAIRE

    Cristiana Virginia PETRE; Alin Constantin DÎRȚU; Marius NICULAUA; Cătălin TĂNASE

    2017-01-01

    This study aims to determine the volatile organic compounds synthesized by three species of wood-rotting basidiomycetes: Coriolopsis gallica, Megacollybia platyphylla and Lentinus arcularius and test their antifungal potential. The species were cultivated on liquid media and kept for 25 days at 25 °C. The surface cultures were then homogenized, filtrated and extracted using solid-phase extraction and analyzed by GC-MS. The volatile compounds identified were mainly alcohols, ketones, aldehydes...

  12. Antifungal and Cytotoxic Assessment of Lapachol Derivatives Produced by Fungal Biotransformation.

    Science.gov (United States)

    Silva, Eliane O; Ruano-González, Antonio; dos Santos, Raquel A; Sánchez-Maestre, Rosario; Furtado, Niege A J C; Collado, Isidro G; Aleu, Josefina

    2016-01-01

    In the screening for biological active compounds, the biotransformation processes catalyzed by filamentous fungi are useful because they can provide information about the possible appearance of toxic metabolites after oral administration and also generate new leads. In this paper, biotransformation of lapachol (1) by three fungal strains, Mucor circinelloides NRRL3631, Botrytis cinerea UCA992 and Botrytis cinerea 2100, has been investigated for the first time. Lapachol (1) was biotransformed into avicequinone-A (2) by M circinelloides, 3'-hydroxylapachol (3) by B. cinerea, and into dehydro-α-lapachone (4) by both fungi. All these compounds were evaluated for their cytotoxic activities. The metabolite 2 displayed non-selective cytotoxicity against tumor and normal cell lines, 3 did not show cytotoxicity against the same cells, while 4 showed higher cytotoxicity against cancer cell lines than lapachol (1). The transformation of 1 into harmless and reactive metabolites evidences the importance of the evaluation of drug metabolism in the drug discovery process. Antifungal potential of lapachol (1) and its metabolites 2 and 4 against B. cinerea has also been evaluated. Dehydro-α-lapachone (4) has been shown to be less toxic to fungal growth than lapachol (1), which indicates a detoxification mechanism of the phytopathogen.

  13. In vitro antifungal activity of bioactive peptides produced by Lactobacillus plantarum against Aspergillus parasiticus and Penicillium expansum

    OpenAIRE

    C.LuzaF.SaladinoaF.B.LucianobJ.MañesaG.Mecaa

    2017-01-01

    Food spoilage caused by mycotoxigenic moulds represents an important problem in food security. The antimicrobial peptides are compounds of natural origin constituted by a variable number (5–100) of amino acids held together through peptide bonds. In this work, the cell free supernatants (CFSs) containing peptides obtained from four strains of LAB were lyophilized, filtered and tested to determine the antifungal activity against Aspergillus Parasiticus and Penicillium expansum. CFS obtained by...

  14. Antifungal compounds from turmeric and nutmeg with activity against plant pathogens

    Science.gov (United States)

    The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant ...

  15. Potent antifouling compounds produced by marine Streptomyces

    KAUST Repository

    Xu, Ying

    2010-02-01

    Biofouling causes huge economic loss and a recent global ban on organotin compounds as antifouling agents has increased the need for safe and effective antifouling compounds. Five structurally similar compounds were isolated from the crude extract of a marine Streptomyces strain obtained from deep-sea sediments. Antifouling activities of these five compounds and four other structurally-related compounds isolated from a North Sea Streptomyces strain against major fouling organisms were compared to probe structure-activity relationships of compounds. The functional moiety responsible for antifouling activity lies in the 2-furanone ring and that the lipophilicity of compounds substantially affects their antifouling activities. Based on these findings, a compound with a straight alkyl side-chain was synthesized and proved itself as a very effective non-toxic, anti-larval settlement agent against three major fouling organisms. The strong antifouling activity, relatively low toxicity, and simple structures of these compounds make them promising candidates for new antifouling additives. © 2009 Elsevier Ltd. All rights reserved.

  16. In Vitro Evaluation of Sub-Lethal Concentrations of Plant-Derived Antifungal Compounds on FUSARIA Growth and Mycotoxin Production

    Directory of Open Access Journals (Sweden)

    Caterina Morcia

    2017-07-01

    Full Text Available Phytopathogenic fungi can lead to significant cereal yield losses, also producing mycotoxins dangerous for human and animal health. The fungal control based on the use of synthetic fungicides can be complemented by "green" methods for crop protection, based on the use of natural products. In this frame, the antifungal activities of bergamot and lemon essential oils and of five natural compounds recurrent in essential oils (citronellal, citral, cinnamaldehyde, cuminaldehyde and limonene have been evaluated against three species of mycotoxigenic fungi (Fusarium sporotrichioides, F. graminearum and F. langsethiae responsible for Fusarium Head Blight in small-grain cereals. The natural products concentrations effective for reducing or inhibiting the in vitro fungal growth were determined for each fungal species and the following scale of potency was found: cinnamaldehyde > cuminaldehyde > citral > citronellal > bergamot oil > limonene > lemon oil. Moreover, the in vitro mycotoxin productions of the three Fusaria strains exposed to sub-lethal concentrations of the seven products was evaluated. The three fungal species showed variability in response to the treatments, both in terms of inhibition of mycelial growth and in terms of modulation of mycotoxin production that can be enhanced by sub-lethal concentrations of some natural products. This last finding must be taken into account in the frame of an open field application of some plant-derived fungicides.

  17. Design and synthesis of novel complexes containing N-phenyl-1H-pyrazole moiety: Ni complex as potential antifungal and antiproliferative compound

    Science.gov (United States)

    El-Gamel, Nadia E. A.; Farghaly, Thoraya A.

    2013-11-01

    Cu(II) (1), Ni(II) (2), Cr(III) (3) and Fe(III) (4) complexes with 3-acetyl-4-benzoyl-1-phenyl-1H-pyrazole (L1) were prepared and structurally characterized. Usual coordination of L1 was achieved through nitrogen of pyrazole moiety and carbonyl acetyl group. Electronic spectra of the complexes indicate that the geometry of the metal center was six coordinate octahedral. In vitro antimicrobial activity of the ligand and complex compounds was screened in terms of antibacterial effect on Staphylococcus aureus (Gram-positive), Escherichia coli (Gram-negative) and antifungal effect on the fungi Aspergillus flavus and candida albicans using the modified Kirby-Bauer disc diffusion and minimum inhibitory concentrations (MIC) methods. Ni(II) complex (2) exhibited remarkable antifungal inhibition against Candida albicans equal to the standard antifungal agent. To continue our study some structural modifications are formed by adding 4-fluoro-benzoyl moiety to L1 in different forms to produce different ligands, 3-acetyl-4-(4-flourobenzoyl)-1-phenyl-1H-pyrazole (L2) and 3-[(3-acetyl-1-phenyl-1H-4-pyrazolyl)carbonyl]-1-phenyl-4-(4-flourobenzoyl)-1H-pyrazole (L3), Ni complexes (5 and 6) are prepared and comparable in vitro antimicrobial study is evaluated. In vitro cytotoxicity of the Ni(II) complex (2) is studied using MTT assay. The analysis of the cell test showed that (2) displayed quite small cytotoxic response at the higher concentration level which indeed would further enable us for more opportunities in therapeutic and biomedical challenges. Both of the capability as a potent in vitro antifungal agent and the cell test analysis show Ni(II) complex (2) as a promising material in the translation of observed in vitro biological phenomenon into clinical therapies settings.

  18. Another point of view on side effects of antifungal compounds used in veterinary medicine

    Directory of Open Access Journals (Sweden)

    Carmen Lidia Chitescu,

    2011-06-01

    Full Text Available The release of pharmaceuticals into environment has become an increasing concern in recent years. Fungi are part of the microbial flora of many animals, humans and foodstuffs, and some species can cause disease. An antimycotic or antifungal product is one that is used in the treatment of fungal infections. Even at low concentrations, antifungals exert an action against micro-organisms and exhibit selective toxicity towards them. The use of antimicrobials selects for resistant populations of micro-organisms. Development of resistance to antifungals is an increasing problem in veterinary and human medicine.

  19. Methods of producing compounds from plant materials

    Science.gov (United States)

    Werpy, Todd A [West Richland, WA; Schmidt, Andrew J [Richland, WA; Frye, Jr., John G.; Zacher, Alan H. , Franz; James A. , Alnajjar; Mikhail S. , Neuenschwander; Gary G. , Alderson; Eric V. , Orth; Rick J. , Abbas; Charles A. , Beery; Kyle E. , Rammelsberg; Anne M. , Kim; Catherine, J [Decatur, IL

    2010-01-26

    The invention includes methods of processing plant material by adding water to form a mixture, heating the mixture, and separating a liquid component from a solid-comprising component. At least one of the liquid component and the solid-comprising component undergoes additional processing. Processing of the solid-comprising component produces oils, and processing of the liquid component produces one or more of glycerol, ethylene glycol, lactic acid and propylene glycol. The invention includes a process of forming glycerol, ethylene glycol, lactic acid and propylene glycol from plant matter by adding water, heating and filtering the plant matter. The filtrate containing starch, starch fragments, hemicellulose and fragments of hemicellulose is treated to form linear poly-alcohols which are then cleaved to produce one or more of glycerol, ethylene glycol, lactic acid and propylene glycol. The invention also includes a method of producing free and/or complexed sterols and stanols from plant material.

  20. Methods of producing compounds from plant material

    Energy Technology Data Exchange (ETDEWEB)

    Werpy, Todd A.; Schmidt, Andrew J.; Frye, Jr., John G.; Zacher, Alan H.; Franz, James A.; Alnajjar, Mikhail S.; Neuenschwander, Gary G.; Alderson, Eric V.; Orth, Rick J.; Abbas, Charles A.; Beery, Kyle E.; Rammelsberg, Anne M.; Kim, Catherine J.

    2006-01-03

    The invention includes methods of processing plant material by adding water to form a mixture, heating the mixture, and separating a liquid component from a solid-comprising component. At least one of the liquid component and the solid-comprising component undergoes additional processing. Processing of the solid-comprising component produces oils, and processing of the liquid component produces one or more of glycerol, ethylene glycol, lactic acid and propylene glycol. The invention includes a process of forming glycerol, ethylene glycol, lactic acid and propylene glycol from plant matter by adding water, heating and filtering the plant matter. The filtrate containing starch, starch fragments, hemicellulose and fragments of hemicellulose is treated to form linear poly-alcohols which are then cleaved to produce one or more of glycerol, ethylene glycol, lactic acid and propylene glycol. The invention also includes a method of producing free and/or complexed sterols and stanols from plant material.

  1. KB425796-A, a novel antifungal antibiotic produced by Paenibacillus sp. 530603.

    Science.gov (United States)

    Kai, Hirohito; Yamashita, Midori; Takase, Shigehiro; Hashimoto, Michizane; Muramatsu, Hideyuki; Nakamura, Ikuko; Yoshikawa, Koji; Ezaki, Masami; Nitta, Kumiko; Watanabe, Masato; Inamura, Noriaki; Fujie, Akihiko

    2013-08-01

    The novel antifungal macrocyclic lipopeptidolactone, KB425796-A (1), was isolated from the fermentation broth of bacterial strain 530603, which was identified as a new Paenibacillus species based on morphological and physiological characteristics, and 16S rRNA sequences. KB425796-A (1) was isolated as white powder by solvent extraction, HP-20 and ODS-B column chromatography, and lyophilization, and was determined to have the molecular formula C79H115N19O18. KB425796-A (1) showed antifungal activities against Aspergillus fumigatus and the micafungin-resistant infectious fungi Trichosporon asahii, Rhizopus oryzae, Pseudallescheria boydii and Cryptococcus neoformans.

  2. Antifungal activity of schinol and a new biphenyl compound isolated from Schinus terebinthifolius against the pathogenic fungus Paracoccidioides brasiliensis

    Directory of Open Access Journals (Sweden)

    Cota Betania B

    2010-10-01

    Full Text Available Abstract Background The aim of this study was to isolate and identify the antifungal compounds from the extracts of Schinus terebinthifolius (Anacardiaceae against clinical isolates of the pathogenic fungus Paracoccidioides brasiliensis. Methods The hexane and dichlomethane fractions from leaves and stems of S. terebinthifolius were fractionated using several chromatography techniques to afford four compounds. Results The compounds isolated from S. terebinthifolius were identified as schinol (1, a new biphenyl compound, namely, 4'-ethyl-4-methyl-2,2',6,6'-tetrahydroxy[1,1'-biphenyl]-4,4'-dicarboxylate (2, quercetin (3, and kaempferol (4. Compounds 1 and 2 were active against different strains of P. brasiliensis, showing a minimal inhibitory concentration value against the isolate Pb B339 of 15.6 μg/ml. The isolate Pb 1578 was more sensitive to compound 1 with a MIC value of 7.5 μg/ml. Schinol presented synergistic effect only when combined with itraconazole. The compounds isolated from S. terebinthifolius were not able to inhibit cell wall synthesis or assembly using the sorbitol assay. Conclusion This work reveals for the first time the occurrence of compound 2 and discloses activity of compounds 1 and 2 against several clinical isolates of P. brasiliensis. These results justify further studies to clarify the mechanisms of action of these compounds.

  3. Antifungal activity of schinol and a new biphenyl compound isolated from Schinus terebinthifolius against the pathogenic fungus Paracoccidioides brasiliensis.

    Science.gov (United States)

    Johann, Susana; Sá, Nívea P; Lima, Luciana A R S; Cisalpino, Patricia S; Cota, Betania B; Alves, Tânia M A; Siqueira, Ezequias P; Zani, Carlos L

    2010-10-12

    The aim of this study was to isolate and identify the antifungal compounds from the extracts of Schinus terebinthifolius (Anacardiaceae) against clinical isolates of the pathogenic fungus Paracoccidioides brasiliensis. The hexane and dichlomethane fractions from leaves and stems of S. terebinthifolius were fractionated using several chromatography techniques to afford four compounds. The compounds isolated from S. terebinthifolius were identified as schinol (1), a new biphenyl compound, namely, 4'-ethyl-4-methyl-2,2',6,6'-tetrahydroxy[1,1'-biphenyl]-4,4'-dicarboxylate (2), quercetin (3), and kaempferol (4). Compounds 1 and 2 were active against different strains of P. brasiliensis, showing a minimal inhibitory concentration value against the isolate Pb B339 of 15.6 μg/ml. The isolate Pb 1578 was more sensitive to compound 1 with a MIC value of 7.5 μg/ml. Schinol presented synergistic effect only when combined with itraconazole. The compounds isolated from S. terebinthifolius were not able to inhibit cell wall synthesis or assembly using the sorbitol assay. This work reveals for the first time the occurrence of compound 2 and discloses activity of compounds 1 and 2 against several clinical isolates of P. brasiliensis. These results justify further studies to clarify the mechanisms of action of these compounds.

  4. Identification and antifungal activity of Streptomyces sp. S72 isolated ...

    African Journals Online (AJOL)

    The test of antifungal activity for several pathogens fungi causing invasive aspergillosis and systemic candidiasis revealed that the Streptomyces sp. S72 was a good moderate antifungal compound producer against Aspergillus fumigatus and Candida albicans, and had no activity against Aspergillus flavus, Aspergillus ...

  5. 2-(Substituted phenyl-3,4-dihydroisoquinolin-2-iums as Novel Antifungal Lead Compounds: Biological Evaluation and Structure-Activity Relationships

    Directory of Open Access Journals (Sweden)

    Xin-Juan Yang

    2013-08-01

    Full Text Available The title compounds are a class of structurally simple analogues of quaternary benzo[c]phenanthridine alkaloids (QBAs. In order to develop novel QBA-like antifungal drugs, in this study, 24 of the title compounds with various substituents on the N-phenyl ring were evaluated for bioactivity against seven phytopathogenic fungi using the mycelial growth rate method and their SAR discussed. Almost all the compounds showed definite activities in vitro against each of the test fungi at 50 μg/mL and a broad antifungal spectrum. In most cases, the mono-halogenated compounds 2–12 exhibited excellent activities superior to the QBAs sanguinarine and chelerythrine. Compound 8 possessed the strongest activities on each of the fungi with EC50 values of 8.88–19.88 µg/mL and a significant concentration-dependent relationship. The SAR is as follows: the N-phenyl group is a high sensitive structural moiety for the activity and the characteristics and position of substituents intensively influence the activity. Generally, electron-withdrawing substituents remarkably enhance the activity while electron-donating substituents cause a decrease of the activity. In most cases, ortha- and para-halogenated isomers were more active than the corresponding m-halogenated isomers. Thus, the title compounds emerged as promising lead compounds for the development of novel biomimetic antifungal agrochemicals. Compounds 8 and 2 should have great potential as new broad spectrum antifungal agents for plant protection.

  6. Bioactive compounds and antifungal activity of three different seaweed species Ulva lactuca, Sargassum tenerrimum and Laurencia obtusa collected from Okha coast, Western India

    Directory of Open Access Journals (Sweden)

    Megha Barot

    2016-04-01

    Full Text Available Objective: To evaluate bioactive compounds responsible for antifungal activity from seaweeds of Okha coast, Western India. Methods: Each species were extracted with different solvents with increasing polarity: hexane, ethyl acetate, chloroform and methanol using Soxhlet apparatus. The antifungal activity was determined by agar diffusion plate method by using fluconazole, ketoconazole and amphotericin B as standards. Gas chromatography-mass spectrometer analysis was done for identification of bioactive compounds present in crude extract. Results: The gas chromatography-mass spectrometer analysis of all the extracts revealed the presence of steroids, fatty acids and esters compounds. Among the three species, the maximum crude extract yield (53.46% and the largest inhibition zone (36 mm were recorded in methanol extract of Ulva lactuca, whereas the minimum crude extract yield and inhibition zone were recorded in chloroform extract of the same species as 0.5% and 10 mm, respectively. Methanol and ethyl acetate extract showed the maximum antifungal activity and the major important compounds like steroids, fatty acids and esters were detected with higher amount in all the extracts. Conclusions: The present study revealed that the different seaweed extracts showed moderate to significant antifungal activity against the strains tested as compared with the standard fungicides, and polar solvents methanol and ethyl acetate were comparatively efficient for extraction of different metabolites that are responsible for antifungal activity.

  7. A biotechnological approach for the development of new antifungal compounds to protect the environment and the human health

    Directory of Open Access Journals (Sweden)

    Claudia Zani

    2015-11-01

    Full Text Available Background. In the Po Valley aflatoxins play a relevant role: the local food economy is heavily based on cereal cultivations for animal feed and human nutrition. Aims of this project are the identification of new compounds that inhibit Aspergillus proliferation, the development of new inhibitors of aflatoxins production, and the set-up a practical screening procedure to identify the most effective and safe compounds. Design and Methods. New compounds will be synthetized with natural origin molecules as ligands and endogenous metal ions to increase their bioavailability for the fungi as metal complexes. A biotechnological high-throughput screening will be set up to identify efficiently the most powerful substances. The newly synthesized compounds with effective antifungal activities, will be evaluated with battery of tests with different end-points to assess the toxic potential risk for environmental and human health. Expected impact of the study for public health. The fundamental step in the project will be the synthesis of new compounds and the study of their capability to inhibit aflatoxin biosynthesis. A new, simple, inexpensive and high-throughput method to screen the anti-fungine and anti-mycotoxin activity of the new synthesised compounds will be applied. The evaluation of possible risks for humans due to toxic and genotoxic activities of the molecules will be made with a new approach using different types of cells (bacteria, plants and human cells.

  8. GC/MS spectroscopic approach and antifungal potential of bioactive extracts produced by marine macroalgae

    Directory of Open Access Journals (Sweden)

    Aida H. Shobier

    2016-09-01

    Full Text Available The antifungal activity and the chemical constituents of selected macroalgae collected from the Egyptian Mediterranean coast of Alexandria have been investigated. Agar well diffusion assay was used to determine the antifungal potential of the extractable matter against Fusarium solani, Fusarium oxysporum, Tricoderma hamatum, Aspergillus flavipes and Candida albicans. The ethyl acetate and methanolic extracts (ULE2 and ULM5 of Ulva lactuca obtained from Al Selsela exhibited the highest activity with (AI = 1.05 ± 0.053 and 1.03 ± 0.052, respectively, compared with fluconazole. However, the methanolic extract of U. lactuca (ULM1 from Abu Qir Bay showed (AI = 0.73 ± 0.037. This followed by methanolic extracts of Pterocladia capillacea (PCM1: AI = 0.70 ± 0.035 and Ulva fasciata (UFM1: AI = 0.69 ± 0.035. GC/MS analysis of ULM1 and ULM5 indicated the existence of different constituents revealing ecological impacts. The methanolic extract (UFM1 contains six major components including palmitic acid, methylester, trichloromethyloxirane, linolenic acid, ethylester, 3,7,11,15-tetramethyl-2-hexadecen-1-ol, 11-octadecenoic acid, methylester and 12,15-octadecadienoic acid, methylester. High percentages of palmitic acid, n-heptacosane, 2-methylhexadecan-1-ol, methoxy acetic acid, 2-tridecylester and myristic acid are found in the methanolic extract of P. capillacea (PCM1. Most of the identified components have been reported to possess antimicrobial activity that could be responsible for the antifungal potential reported in the present study.

  9. Microorganisms and methods for producing pyruvate, ethanol, and other compounds

    Energy Technology Data Exchange (ETDEWEB)

    Reed, Jennifer L.; Zhang, Xiaolin

    2017-12-26

    Microorganisms comprising modifications for producing pyruvate, ethanol, and other compounds. The microorganisms comprise modifications that reduce or ablate activity of one or more of pyruvate dehydrogenase, 2-oxoglutarate dehydrogenase, phosphate acetyltransferase, acetate kinase, pyruvate oxidase, lactate dehydrogenase, cytochrome terminal oxidase, succinate dehydrogenase, 6-phosphogluconate dehydrogenase, glutamate dehydrogenase, pyruvate formate lyase, pyruvate formate lyase activating enzyme, and isocitrate lyase. The microorganisms optionally comprise modifications that enhance expression or activity of pyruvate decarboxylase and alcohol dehydrogenase. The microorganisms are optionally evolved in defined media to enhance specific production of one or more compounds. Methods of producing compounds with the microorganisms are provided.

  10. Effect of Polymer Micelles on Antifungal Activity of Geranylorcinol Compounds against Botrytis cinerea.

    Science.gov (United States)

    Taborga, Lautaro; Díaz, Katy; Olea, Andrés F; Reyes-Bravo, Paula; Flores, Mario E; Peña-Cortés, Hugo; Espinoza, Luis

    2015-08-12

    Herein, we explore the potential use of two micelle-forming block copolymers, i.e., Pluronic F-127 and poly(ethylene oxide)-b-poly(caprolactone), for application of fungicide agents. The polymer effect on the in vitro fungicide activity of a series of geranyl orcinol derivatives against Botrytis cinerea has been assessed. The results show that, for all test compounds, the incorporation into micelles, formed by Pluronic F-127, produces a great enhancement of the inhibitory effect on the growth of B. cinerea. For some compounds, at the lowest tested concentration (50 ppm), the percentage of inhibition increases significantly (from 0-10 to 80-90%) when the application is made using a polymer solution instead of an ethanol/water mixture. The synthesis and structural determination of a series of eight geranylphenols/diacetates, which were used as fungicide agents, are also discussed. These results suggest that polymer micelles are promising systems for application of crop-protecting agents.

  11. Mixtures of Quaternary Ammonium Compounds and Long-chain Fatty Acids as Antifungal Agents

    Science.gov (United States)

    Kull, F. C.; Eisman, P. C.; Sylwestrowicz, H. D.; Mayer, R. L.

    1961-01-01

    The influence of undecylenic acid on the fungistatic effect of phenoxyethyldimethyldodecylammonium bromide (Domiphen bromide) against Trichophyton mentagrophytes was investigated. The unsaturated fatty acid was found to enhance the fungistatic activity of Domiphen bromide against this organism. The ratio of concentrations of these agents has a marked influence on the results of in vitro tests for antifungal action resulting in a completely different effect than heretofore noted in combination experiments against bacteria. The enhancing phenomenon is not particular to T. mentagrophytes, it was observed also with Candida albicans. PMID:14460466

  12. Rhizoctonia solani and Bacterial Inoculants Stimulate Root Exudation of Antifungal Compounds in Lettuce in a Soil-Type Specific Manner

    Directory of Open Access Journals (Sweden)

    Saskia Windisch

    2017-06-01

    Full Text Available Previous studies conducted on a unique field site comprising three contrasting soils (diluvial sand DS, alluvial loam AL, loess loam LL under identical cropping history, demonstrated soil type-dependent differences in biocontrol efficiency against Rhizoctonia solani-induced bottom rot disease in lettuce by two bacterial inoculants (Pseudomonas jessenii RU47 and Serratia plymuthica 3Re-4-18. Disease severity declined in the order DS > AL > LL. These differences were confirmed under controlled conditions, using the same soils in minirhizotron experiments. Gas chromatography-mass spectrometry (GC-MS profiling of rhizosphere soil solutions revealed benzoic and lauric acids as antifungal compounds; previously identified in root exudates of lettuce. Pathogen inoculation and pre-inoculation with bacterial inoculants significantly increased the release of antifungal root exudates in a soil type-specific manner; with the highest absolute levels detected on the least-affected LL soil. Soil type-dependent differences were also recorded for the biocontrol effects of the two bacterial inoculants; showing the highest efficiency after double-inoculation on the AL soil. However, this was associated with a reduction of shoot growth and root hair development and a limited micronutrient status of the host plants. Obviously, disease severity and the expression of biocontrol effects are influenced by soil properties with potential impact on reproducibility of practical applications.

  13. Penicillium antifungal protein (PAF) is involved in the apoptotic and autophagic processes of the producer Penicillium chrysogenum.

    Science.gov (United States)

    Kovács, Barbara; Hegedűs, Nikoletta; Bálint, Mihály; Szabó, Zsuzsa; Emri, Tamás; Kiss, Gréta; Antal, Miklós; Pócsi, István; Leiter, Eva

    2014-09-01

    PAF, which is produced by the filamentous fungus Pencicillium chrysogenum, is a small antifungal protein, triggering ROS-mediated apoptotic cell death in Aspergillus nidulans. In this work, we provide information on the function of PAF in the host P. chrysogenum considering that carbon-starving cultures of the Δpaf mutant strain showed significantly reduced apoptosis rates in comparison to the wild-type (wt) strain. Moreover, the addition of PAF to the Δpaf strain resulted in a twofold increase in the apoptosis rate. PAF was also involved in the regulation of the autophagy machinery of this fungus, since several Saccharomyces cerevisiae autophagy-related ortholog genes, e.g. those of atg7, atg22 and tipA, were repressed in the deletion strain. This phenomenon was accompanied by the absence of autophagosomes in the Δpaf strain, even in old hyphae.

  14. An antifungal chitinase produced by Bacillus cereus with shrimp and crab shell powder as a carbon source.

    Science.gov (United States)

    Chang, Wen-Teish; Chen, Chin-Shuh; Wang, San-Lang

    2003-08-01

    The production of inexpensive chitinolytic enzymes is an element in the utilization of shellfish processing wastes. In this study, shrimp and crab shell powder prepared by treating shrimp and crab processing wastes with boiling and crushing was used as a substrate for the isolation of an antifungal chitinase-producing microorganism. Bacillus cereus YQ 308, a strain isolated from the soil samples, excreted one chitinase when cultured in a medium containing 2% (wt/vol) shrimp and crab shell powder as major carbon source. The chitinase, purified by sequential chromatography, had an Mr of 48 kDa and pI of 5.2. The purified chitinase (2 mg/ml) inhibited the hyphal extension of the fungi Fusarium oxysporum and Pythium ultimum.

  15. Marine Vibrio Species Produce the Volatile Organic Compound Acetone

    OpenAIRE

    Nemecek-Marshall, M.; Wojciechowski, C.; Kuzma, J.; Silver, G. M.; Fall, R.

    1995-01-01

    While screening aerobic, heterotrophic marine bacteria for production of volatile organic compounds, we found that a group of isolates produced substantial amounts of acetone. Acetone production was confirmed by gas chromatography, gas chromatography-mass spectrometry, and high-performance liquid chromatography. The major acetone producers were identified as nonclinical Vibrio species. Acetone production was maximal in the stationary phase of growth and was stimulated by addition of l-leucine...

  16. Plant-derived bioactive compounds produced by endophytic fungi.

    Science.gov (United States)

    Zhao, J; Shan, T; Mou, Y; Zhou, L

    2011-02-01

    Plant endophytic fungi are an important and novel resource of natural bioactive compounds with their potential applications in agriculture, medicine and food industry. In the past two decades, many valuable bioactive compounds with antimicrobial, insecticidal, cytotoxic, and anticancer activities have been successfully discovered from endophytic fungi. During the long period of co-evolution, a friendly relationship was formed between each endophyte and its host plant. Some endophytes have the ability to produce the same or similar bioactive compounds as those originated from their host plants. This review mainly deals with the research progress on endophytic fungi for producing plant-derived bioactive compounds such as paclitaxel, podophyllotoxin, camptothecine, vinblastine, hypericin, and diosgenin. The relations between endophytic fungi and their host plants, biological activities and action mechanisms of these compounds from endophytic fungi, some available strategies for efficiently promoting production of these bioactive compounds, as well as their potential applications in the future will also be discussed. It is beneficial for us to better understand and take advantage of plant endophytic fungi.

  17. Interactions between a sap beetle, sabal palm, scale insect, filamentous fungi and yeast, with discovery of potential antifungal compounds.

    Directory of Open Access Journals (Sweden)

    Andrew R Cline

    Full Text Available The multi-trophic relationship between insects, yeast, and filamentous fungi is reported on sabal palm (Sabal palmetto (Walter Lodd. ex Schult. & Schult. f.. Gut content analyses and observations of adult and larval feeding of the sap beetle Brachypeplus glaber LeConte indicate that niche partitioning of fungal food substrata occurs between adults and larvae. This is the first report of specific mycophagous niche partitioning among beetle life stages based on gut content analyses. Fungi isolated from the beetle gut of adults, larvae, and pupae include species of Fusarium Link, Cladosporium Link, and Penicillium Link, which were differentially ingested by larvae and adults; Fusarium solani and Penicillium species in larvae, whereas F. oxysoproum, F. verticillioides, and Cladosporium in adults. These data indicate the first species-level host data for Brachypeplus Erichson species. Fusarium proliferatum (Matsush. Nirenberg was the most commonly occurring fungal gut component, being isolated from the palm as well as gut of larvae, pupae, and adults; representing a commonly shared food resource. One species of yeast, Meyerozyma caribbica (Vaughan-Mart. et al. Kurtzman & Suzuki (basionym = Pichia caribbica, was isolated from all life stages and is likely responsible for anti-fungal properties observed in the pupae and represents a promising source of antifungal compounds; rearing and diagnostic protocols are provided to aid biomedical researchers. Feeding and cleaning behaviors are documented using time-lapse video-micrography, and discussed in a behavioral and functional morphological context. Adults spent long periods feeding, often >1/3 of the two-hour observation period. A generic adult body posture was observed during feeding, and included substrate antennation before and after ingestion. Adult grooming behaviors were manifested in distinct antennal and tarsal cleaning mechanisms. Larval behaviors were different from adults, and larvae feeding

  18. Search for antifungal and anticancer compounds from native plant species of Cerrado and Atlantic Forest.

    Science.gov (United States)

    Bolzani, V da S; Young, M C; Furlan, M; Cavalheiro, A J; Araújo, A R; Silva, D H; Lopes, M N

    1999-01-01

    Bioactivity-guided fractionation of several bioactive extracts obtained from Cerrado and Atlantic Forest plant species led to the isolation of potent DNA-damaging piperidine 1-5 and guanidine alkaloids 6-9 from Cassia leptophylla and Pterogyne nitens respectively, two common Leguminosae from Atlantic Forest. By means of biotechnological approach on Maytenus aquifolium, a species from Cerrado, moderate DNA-damaging sesquiterpene pyridine alkaloid 10-11 was isolated. Bioassay-guided fractionation on Casearia sylvestris, a medicinal plant species found in Cerrado and Atlantic Forest, led to the isolation of clerodane diterpenes 12-13 which showed effect on DNA. In addition, we have reported several interesting potent antifungal iridoids: 1 beta-hydroxy-dihydrocornin (14), 1 alpha-hydroxy-dihydrocornin (15), alpha-gardiol (16), beta-gardiol (17), plumericin (18), isoplumericin (19), 11-O-trans-caffeoylteucrein (20); ester derivative: 2-methyl-4-hydroxy-butyl-caffeoate (21), amide N-[7-(3',4'-methylenedioxyphenyl)-2Z, 4Z-heptadienoyl] pyrrolidine (22) and triterpene viburgenin (23).

  19. Aspergillus mulundensis sp. nov., a new species for the fungus producing the antifungal echinocandin lipopeptides, mulundocandins

    DEFF Research Database (Denmark)

    Bills, Gerald F.; Yue, Qun; Chen, Li

    2016-01-01

    The invalidly published name Aspergillus sydowii var. mulundensis was proposed for a strain of Aspergillus that produced new echinocandin metabolites designated as the mulundocadins. Reinvestigation of this strain (Y-30462=DSMZ 5745) using phylogenetic, morphological, and metabolic data indicated...

  20. New anti-HIV-1, antimalarial, and antifungal compounds from Terminalia bellerica

    DEFF Research Database (Denmark)

    Valsaraj, R.; Pushpangadan, P.; Wagner Smitt, U.

    1997-01-01

    A bioactivity-guided fractionation of an extract of Terminalia bellerica fruit rind led to the isolation of two new lignans named termilignan (1) and thannilignan (2), together with 7-hydroxy-3',4'-(methylenedioxy)flavan (3) and anolignan B (4). All four compounds possessed demonstrable anti-HIV-1...

  1. Synthesis and preliminary evaluation of N-acylhydrazone compounds as antibacterial and antifungal agents; Sintese e avaliacao preliminar da atividade antibacteriana e antifungica de derivados N-acilidrazonicos

    Energy Technology Data Exchange (ETDEWEB)

    Cachiba, Thomas Haruo; Carvalho, Bruno Demartini; Carvalho, Diogo Teixeira [Universidade Federal de Alfenas, MG (Brazil). Fac. de Ciencias Farmaceuticas. Dept. de Alimentos e Medicamentos; Cusinato, Marina; Prado, Clara Gaviao; Dias, Amanda Latercia Tranches, E-mail: diogo.carvalho@unifal-mg.edu.br [Universidade Federal de Alfenas, MG (Brazil). Inst. de Ciencias Biomedicas

    2012-07-01

    We describe the synthesis and evaluation of N-acylhydrazone compounds bearing different electron-donating groups in one of its aromatic rings, obtained using a four-step synthetic route. IC{sub 50} values against pathogenic fungi and bacteria were determined by serial microdilution. Compounds showed low activity against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. By contrast, a derivative with a meta-oriented electron-donating group showed significant activity (IC50) against Candida albicans (17 {mu}M), C. krusei (34 {mu}M) and C. tropicalis (17 {mu}M). Results suggest this is a promising lead-compound for synthesis of potent antifungal agents. (author)

  2. Isolation and identification of N-butyl-tetrahydro-5-oxofuran-2-carboxamide produced by Bacillus sp. L60 and its antifungal activity.

    Science.gov (United States)

    Lee, Yong-Seong; Cho, Jeong-Yong; Moon, Jae-Hak; Kim, Kil-Yong

    2017-03-01

    Rhizoctonia solani is the cause of substantial economic loss in many crops. The aim of this study is to investigate biocontrol potential of Bacillus sp. L60 against R. solani and to purify an antifungal compound. In this study, Bacillus sp. L60 demonstrated significant antagonism toward R. solani with the dual culture assay. The antifungal compound was extracted from Bacillus sp. L60 culture supernatant with n-butanol, and identified as N-butyl-tetrahydro-5-oxofuran-2-carboxamide (BT-5O-2C) having molecular weights of 185.1052 Da with the formula C 9 H 15 NO 3 using NMR and HR-ESI-MS analysis. The minimum inhibitory concentration (MIC) value of the antifungal compound was 256 µg ml -1 against R. solani. Therefore, our results clearly demonstrated BT-5O-2C as well as Bacillus sp. L60 as potential biological control agents for the management of R. solani. © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  3. Coumarin Antifungal Lead Compounds from Millettia thonningii and Their Predicted Mechanism of Action

    Directory of Open Access Journals (Sweden)

    Daniel M. Ayine-Tora

    2016-10-01

    Full Text Available Fungal pathogens continue to pose challenges to humans and plants despite efforts to control them. Two coumarins, robustic acid and thonningine-C isolated from Millettia thonningii, show promising activity against the fungus Candida albicans with minimum fungicidal concentration of 1.0 and 0.5 mg/mL, respectively. Molecular modelling against the putative bio-molecular target, lanosterol 14α-demethylase (CYP51, revealed a plausible binding mode for the active compounds, in which the hydroxyl group binds with a methionine backbone carboxylic group blocking access to the iron catalytic site. This binding disrupts the synthesis of several important sterols for the survival of fungi.

  4. Cuticular antifungals in spiders: density- and condition dependence.

    Directory of Open Access Journals (Sweden)

    Daniel González-Tokman

    Full Text Available Animals living in groups face a high risk of disease contagion. In many arthropod species, cuticular antimicrobials constitute the first protective barrier that prevents infections. Here we report that group-living spiders produce cuticular chemicals which inhibit fungal growth. Given that cuticular antifungals may be costly to produce, we explored whether they can be modulated according to the risk of contagion (i.e. under high densities. For this purpose, we quantified cuticular antifungal activity in the subsocial crab spider Diaea ergandros in both natural nests and experimentally manipulated nests of varying density. We quantified the body-condition of spiders to test whether antifungal activity is condition dependent, as well as the effect of spider density on body-condition. We predicted cuticular antifungal activity to increase and body-condition to decrease with high spider densities, and that antifungal activity would be inversely related to body-condition. Contrary to our predictions, antifungal activity was neither density- nor condition-dependent. However, body-condition decreased with density in natural nests, but increased in experimental nests. We suggest that pathogen pressure is so important in nature that it maintains high levels of cuticular antifungal activity in spiders, impacting negatively on individual energetic condition. Future studies should identify the chemical structure of the isolated antifungal compounds in order to understand the physiological basis of a trade-off between disease prevention and energetic condition caused by group living, and its consequences in the evolution of sociality in spiders.

  5. Sesquiterpenes produced by endophytic fungus Phomopsis cassiae with antifungal and acetylcholinesterase inhibition activities; Sesquiterpenos produzidos pelo fungo endofitico Phomopsis cassiae com atividade antifungica e inibidora de acetilcolinesterase

    Energy Technology Data Exchange (ETDEWEB)

    Zanardi, Lisineia M.; Bolzani, Vanderlan da S.; Cavalheiro, Alberto J.; Silva, Dulce H. Siqueira; Trevisan, Henrique C.; Araujo, Angela R. [UNESP, Araraquara, SP (Brazil). Inst. de Quimica; Silva, Geraldo H. [Universidade Federal de Sergipe (UFS), Aracaju, SE (Brazil). Centro de Ciencias Exatas e Tecnologia; Teles, Helder L. [Universidade Federal do Mato Grosso (UFMT), Rondonopolis, MT (Brazil). Dept. de Ciencias Biologicas; Young, Maria Claudia M., E-mail: araujoar@iq.unesp.br [Instituto de Botanica, Sao Paulo, SP (Brazil). Seccao de Fisiologia e Bioquimica de Plantas

    2012-07-01

    Two new diastereoisomeric cadinanes sesquiterpenes 3,9-dihydroxycalamenene (1-2), along with the known 3-hydroxycalamen-8-one (3) and aristelegone-A (4), were isolated from ethyl acetate extract of Phomopsis cassiae, an endophytic fungus in Cassia spectabilis. Their structures, including relative stereochemistry, were determined on the basis of detailed interpretation of 2D NMR spectra and comparison with related known compounds. Compounds 1-4 displayed antifungal activity against the phytopathogenic fungi Cladosporium cladosporioides and C. sphaerospermum, as well as inhibition of acetylcholinesterase. (author)

  6. Potent In Vitro Antifungal Activities of Naturally Occurring Acetylenic Acids▿

    Science.gov (United States)

    Li, Xing-Cong; Jacob, Melissa R.; Khan, Shabana I.; Ashfaq, M. Khalid; Babu, K. Suresh; Agarwal, Ameeta K.; ElSohly, Hala N.; Manly, Susan P.; Clark, Alice M.

    2008-01-01

    Our continuing effort in antifungal natural product discovery has led to the identification of five 6-acetylenic acids with chain lengths from C16 to C20: 6-hexadecynoic acid (compound 1), 6-heptadecynoic acid (compound 2), 6-octadecynoic acid (compound 3), 6-nonadecynoic acid (compound 4), and 6-icosynoic acid (compound 5) from the plant Sommera sabiceoides. Compounds 2 and 5 represent newly isolated fatty acids. The five acetylenic acids were evaluated for their in vitro antifungal activities against Candida albicans, Candida glabrata, Candida krusei, Candida tropicalis, Candida parapsilosis, Cryptococcus neoformans, Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Trichophyton mentagrophytes, and Trichophyton rubrum by comparison with the positive control drugs amphotericin B, fluconazole, ketoconazole, caspofungin, terbinafine, and undecylenic acid. The compounds showed various degrees of antifungal activity against the 21 tested strains. Compound 4 was the most active, in particular against the dermatophytes T. mentagrophytes and T. rubrum and the opportunistic pathogens C. albicans and A. fumigatus, with MICs comparable to several control drugs. Inclusion of two commercially available acetylenic acids, 9-octadecynoic acid (compound 6) and 5,8,11,14-eicosatetraynoic acid (compound 7), in the in vitro antifungal testing further demonstrated that the antifungal activities of the acetylenic acids were associated with their chain lengths and positional triple bonds. In vitro toxicity testing against mammalian cell lines indicated that compounds 1 to 5 were not toxic at concentrations up to 32 μM. Furthermore, compounds 3 and 4 did not produce obvious toxic effects in mice at a dose of 34 μmol/kg of body weight when administered intraperitoneally. Taking into account the low in vitro and in vivo toxicities and significant antifungal potencies, these 6-acetylenic acids may be excellent leads for further preclinical studies. PMID:18458131

  7. Potent in vitro antifungal activities of naturally occurring acetylenic acids.

    Science.gov (United States)

    Li, Xing-Cong; Jacob, Melissa R; Khan, Shabana I; Ashfaq, M Khalid; Babu, K Suresh; Agarwal, Ameeta K; Elsohly, Hala N; Manly, Susan P; Clark, Alice M

    2008-07-01

    Our continuing effort in antifungal natural product discovery has led to the identification of five 6-acetylenic acids with chain lengths from C(16) to C(20): 6-hexadecynoic acid (compound 1), 6-heptadecynoic acid (compound 2), 6-octadecynoic acid (compound 3), 6-nonadecynoic acid (compound 4), and 6-icosynoic acid (compound 5) from the plant Sommera sabiceoides. Compounds 2 and 5 represent newly isolated fatty acids. The five acetylenic acids were evaluated for their in vitro antifungal activities against Candida albicans, Candida glabrata, Candida krusei, Candida tropicalis, Candida parapsilosis, Cryptococcus neoformans, Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Trichophyton mentagrophytes, and Trichophyton rubrum by comparison with the positive control drugs amphotericin B, fluconazole, ketoconazole, caspofungin, terbinafine, and undecylenic acid. The compounds showed various degrees of antifungal activity against the 21 tested strains. Compound 4 was the most active, in particular against the dermatophytes T. mentagrophytes and T. rubrum and the opportunistic pathogens C. albicans and A. fumigatus, with MICs comparable to several control drugs. Inclusion of two commercially available acetylenic acids, 9-octadecynoic acid (compound 6) and 5,8,11,14-eicosatetraynoic acid (compound 7), in the in vitro antifungal testing further demonstrated that the antifungal activities of the acetylenic acids were associated with their chain lengths and positional triple bonds. In vitro toxicity testing against mammalian cell lines indicated that compounds 1 to 5 were not toxic at concentrations up to 32 muM. Furthermore, compounds 3 and 4 did not produce obvious toxic effects in mice at a dose of 34 mumol/kg of body weight when administered intraperitoneally. Taking into account the low in vitro and in vivo toxicities and significant antifungal potencies, these 6-acetylenic acids may be excellent leads for further preclinical studies.

  8. Antifungal activity of naphthoquinoidal compounds in vitro against fluconazole-resistant strains of different Candida species: a special emphasis on mechanisms of action on Candida tropicalis.

    Directory of Open Access Journals (Sweden)

    João B A Neto

    Full Text Available In recent decades, the incidence of candidemia in tertiary hospitals worldwide has substantially increased. These infections are a major cause of morbidity and mortality; in addition, they prolong hospital stays and raise the costs associated with treatment. Studies have reported a significant increase in infections by non-albicans Candida species, especially C. tropicalis. The number of antifungal drugs on the market is small in comparison to the number of antibacterial agents available. The limited number of treatment options, coupled with the increasing frequency of cross-resistance, makes it necessary to develop new therapeutic strategies. The objective of this study was to evaluate and compare the antifungal activities of three semisynthetic naphthofuranquinone molecules against fluconazole-resistant Candida spp. strains. These results allowed to us to evaluate the antifungal effects of three naphthofuranquinones on fluconazole-resistant C. tropicalis. The toxicity of these compounds was manifested as increased intracellular ROS, which resulted in membrane damage and changes in cell size/granularity, mitochondrial membrane depolarization, and DNA damage (including oxidation and strand breakage. In conclusion, the tested naphthofuranquinones (compounds 1-3 exhibited in vitro cytotoxicity against fluconazole-resistant Candida spp. strains.

  9. Development of Radiolabeled compounds using reactor-produced radionuclides

    International Nuclear Information System (INIS)

    Choi, Sun Ju; Park, K. B.; Park, S. H.

    2007-06-01

    To establish a robust technology for radiopharmaceutical development, we focused on the configuration of fundamental development of radiolabeled compounds for radioimmunotherapy and drug delivery as well as the development of bifunctional chelating agents and radiolabeling methods for the radiopharmaceuticals with highly specific activity to deliver sufficient number of radionuclides to the target site. In this project, we aim to improve the quality of life and the public welfare by fostering the medical application of radioisotopes for the effective treatment of malignant diseases and by developing efficient radiolabeling methods of specific bio-active materials with radioisotopes and new candidates for radiopharmaceutical application. We have established the procedure for the preparation of radiolabeled antibody and biotin with radioisotopes such as 166 Ho, 131 I, 90 Y and 111 In for tumour targeting. In the future, these technologies will be applicable to development of radioimmunotherapeutic drug. The combination treatment of radioisotope with anti-cancer agents or chemotherapeutic agents may produce a synergistic static effects in the tumour and this synergism would be exerted via gene level through the activation of a cell death pathway. The combination therapy may be very beneficial for cancer treatment and this can overcome not only the hazards of unnecessary exposure to high radiation level during therapy, but also the tendency for drug resistance caused by chemotherapy. To develop new drug delivery system suitable for CT imaging agent, a chitosan derivative and radiolabed Folate-targeted polymer with 131 I were synthesized. We also carried out the development of DTPA derivatives for CT imaging agent, radiolabeled precursor, and established a highly efficient radiolabeling methodology with lanthanide nuclide. In order to develop neuroreceptor targeting compounds, we synthesized WAY-100635 compound and 99m Tc(CO) 3 precursor from Chrysamine G derivatives

  10. Special Issue: Novel Antifungal Drug Discovery

    Directory of Open Access Journals (Sweden)

    Maurizio Del Poeta

    2016-12-01

    Full Text Available This Special Issue is designed to highlight the latest research and development on new antifungal compounds with mechanisms of action different from the ones of polyenes, azoles, and echinocandins. The papers presented here highlight new pathways and targets that could be exploited for the future development of new antifungal agents to be used alone or in combination with existing antifungals. A computational model for better predicting antifungal drug resistance is also presented.

  11. Substâncias antifúngicas de Xylaria sp., um fungo endofítico isolado de Palicourea marcgravii (Rubiaceae Antifungal compounds of Xylaria sp., an endophytic fungus isolated from Palicourea marcgravii (Rubiaceae

    Directory of Open Access Journals (Sweden)

    Mariana C. Cafêu

    2005-12-01

    Full Text Available Five compounds, 2-hexyl-3-methyl-butanodioic acid (1, cytochalasin D (2, 7-dechlorogriseofulvin (3, cytochalasin B (4 and griseofulvin (5, have been isolated from the endophytic fungus Xylaria sp., and their structures were elucidated on the basis of spectroscopic data. In the bioautography assay against Cladosporium cladosporioides and Cladosporium sphaerospermum, compounds 1 and 2 were found to be active while compounds 3, 4 and 5 did not show antifungal activity.

  12. Effects of disrupting the polyketide synthase gene WdPKS1 in Wangiella [Exophiala] dermatitidis on melanin production and resistance to killing by antifungal compounds, enzymatic degradation, and extremes in temperature

    Directory of Open Access Journals (Sweden)

    Mandal Piyali

    2006-06-01

    Full Text Available Abstract Background Wangiella dermatitidis is a human pathogenic fungus that is an etiologic agent of phaeohyphomycosis. W. dermatitidis produces a black pigment that has been identified as a dihydroxynaphthalene melanin and the production of this pigment is associated with its virulence. Cell wall pigmentation in W. dermatitidis depends on the WdPKS1 gene, which encodes a polyketide synthase required for generating the key precursor for dihydroxynaphthalene melanin biosynthesis. Results We analyzed the effects of disrupting WdPKS1 on dihydroxynaphthalene melanin production and resistance to antifungal compounds. Transmission electron microscopy revealed that wdpks1Δ-1 yeast had thinner cell walls that lacked an electron-opaque layer compared to wild-type cells. However, digestion of the wdpks1Δ-1 yeast revealed small black particles that were consistent with a melanin-like compound, because they were acid-resistant, reacted with melanin-binding antibody, and demonstrated a free radical signature by electron spin resonance analysis. Despite lacking the WdPKS1 gene, the mutant yeast were capable of catalyzing the formation of melanin from L-3,4-dihyroxyphenylalanine. The wdpks1Δ-1 cells were significantly more susceptible to killing by voriconazole, amphotericin B, NP-1 [a microbicidal peptide], heat and cold, and lysing enzymes than the heavily melanized parental or complemented strains. Conclusion In summary, W. dermatitidis makes WdPKS-dependent and -independent melanins, and the WdPKS1-dependent deposition of melanin in the cell wall confers protection against antifungal agents and environmental stresses. The biological role of the WdPKS-independent melanin remains unclear.

  13. Antifungal Compounds Isolated from Smyrnium olusatrum L. Essential Oil, Growing Wild in Cephalonia, Greece. Chemical Analysis and Structure Elucidation

    Directory of Open Access Journals (Sweden)

    Gerasimia Tsasi

    2016-01-01

    Full Text Available The essential oils (EOs from the leaves and the flowers of Smyrnium olusatrum L. , growing wild in the island of Cephalonia (Greece, were analyzed by GC-FID and GC-MS. Fifty nine constituents, which accounted for 90.3% (fl and 97.1% (lvs of the oils, were identified. Furanodiene, g ermacrone and furanoeremophil-1-one were the major constituents in both essential oils; they were also isolated from the flowers essential oil and identified using spectroscopic methods, ie. 1D and 2D NMR, GC-MS . In addition b -myrcene ( 11.7% and b -phellandrene (5.2% were main constituents in the essential oil of the leaves. The essential oils and the pure isolates were evaluated for antifungal activity against Aspergillus fumigatus , A. versicolor, A. ochraceus, A. niger, Trichoderma viride, Penicillium funiculosum, P. ochrochloron, P. verucosum var. cyclopium by using the microdilution method and proved to possess significant antifungal effect. Among them, (+ furanoeremophil-1-one was particularly active with MIC values in the range of 0.0008-0.125 mg/mL and MFC values of 0.025-0.050 mg/mL and proved more effective than the commercial mycotics ketoconazole and bifonazole used as positive controls.

  14. Collapsing aged culture of the cyanobacterium Synechococcus elongatus produces compound(s toxic to photosynthetic organisms.

    Directory of Open Access Journals (Sweden)

    Assaf Cohen

    Full Text Available Phytoplankton mortality allows effective nutrient cycling, and thus plays a pivotal role in driving biogeochemical cycles. A growing body of literature demonstrates the involvement of regulated death programs in the abrupt collapse of phytoplankton populations, and particularly implicates processes that exhibit characteristics of metazoan programmed cell death. Here, we report that the cell-free, extracellular fluid (conditioned medium of a collapsing aged culture of the cyanobacterium Synechococcus elongatus is toxic to exponentially growing cells of this cyanobacterium, as well as to a large variety of photosynthetic organisms, but not to eubacteria. The toxic effect, which is light-dependent, involves oxidative stress, as suggested by damage alleviation by antioxidants, and the very high sensitivity of a catalase-mutant to the conditioned medium. At relatively high cell densities, S. elongatus cells survived the deleterious effect of conditioned medium in a process that required de novo protein synthesis. Application of conditioned medium from a collapsing culture caused severe pigment bleaching not only in S. elongatus cells, but also resulted in bleaching of pigments in a cell free extract. The latter observation indicates that the elicited damage is a direct effect that does not require an intact cell, and therefore, is mechanistically different from the metazoan-like programmed cell death described for phytoplankton. We suggest that S. elongatus in aged cultures are triggered to produce a toxic compound, and thus, this process may be envisaged as a novel regulated death program.

  15. Tioconazole, a new imidazole-antifungal agent for the treatment of dermatomycoses. Antifungal and pharmacologic properties.

    Science.gov (United States)

    Marriott, M S; Baird, J R; Brammer, K W; Faulkner, J K; Halliwell, G; Jevons, S; Tarbit, M H

    1983-01-01

    Tioconazole is a new imidazole antifungal agent with broad-spectrum activity. Its in vitro activity against common dermal pathogens is generally better than miconazole by a factor of 2-8. This activity is paralleled by good topical efficacy in a guinea pig dermatomycosis model. Pharmacokinetic studies in animals have demonstrated minimal systemic exposure following dermal application. Acute general pharmacology studies have shown that the compound is well tolerated in animals and unlikely to produce side-effects in man.

  16. Antifungal Activity of Bacillus coagulans TQ33, Isolated from Skimmed Milk Powder, against Botrytis cinerea

    Directory of Open Access Journals (Sweden)

    Rui Feng Xiao

    2013-01-01

    Full Text Available Bacillus coagulans TQ33 is isolated from the skimmed milk powder and has a broad antifungal activity against pathogens such as Botrytis cinerea, Alternaria solani, Phytophthora drechsleri Tucker, Fusarium oxysporum and Glomerella cingulata. The characteristics of active antifungal substances produced by B. coagulans TQ33 and its antifungal effects against the growth of plant pathogenic fungi has been evaluated. The effect of pH, temperature and protease on the antifungal activity of B. coagulans TQ33 was determined. The results of partial characterization of the antifungal compound indicated that its activity is likely to be due to the production of a proteinaceous substance together with other substances. The greenhouse trials suggest that B. coagulans TQ33 has a great potential for the control of plant pathogenic fungi.

  17. Contribution of volatiles to the antifungal effect of Lactobacillus paracasei in defined medium and yogurt

    DEFF Research Database (Denmark)

    Aunsbjerg, Stina Dissing; Honoré, Anders Hans; Marcussen, J.

    2015-01-01

    to the antifungal activity. The role of volatile compounds in the antifungal activity of Lactobacillus paracasei DGCC 2132 in a chemically defined interaction medium (CDIM) and yogurt was therefore investigated with a sampling technique minimizing volatile loss. Diacetyl was identified as the major volatile...... produced by L. paracasei DGCC 2132 in CDIM. When the strain was added to a yogurt medium diacetyl as well as other volatiles also increased but the metabolome was more complex. Removal of L. paracasei DGCC 2132 cells from CDIM fermentate resulted in loss of both volatiles, including diacetyl......, and the antifungal activity towards two strains of Penicillium spp. When adding diacetyl to CDIM or yogurt without L. paracasei DGCC 2132, marked inhibition was observed. Besides diacetyl, the antifungal properties of acetoin were examined, but no antifungal activity was observed. Overall, the results demonstrate...

  18. Identification of the predominant volatile compounds produced by Aspergillus flavus.

    Science.gov (United States)

    Kamiński, E; Libbey, L M; Stawicki, S; Wasowicz, E

    1972-11-01

    A culture of Aspergillus flavus grown on moistened wheat meal was homogenized with a blendor, and the resulting slurry was vacuum-distilled at 5 mm of Hg and 35 C. The aqueous distillate was collected in traps cooled to -10 to -80 C. The culture volatiles were extracted from the distillate with CH(2)Cl(2), and, after removal of the bulk of the solvent, the concentrated volatiles were examined by packed-column gas chromatography. Nineteen peaks were observed, and coupled gas chromatography-mass spectrometry was employed to identify the larger components. The compounds identified were: 3-methyl-butanol, 3-octanone, 3-octanol, 1-octen-3-ol, 1-octanol, and cis-2-octen-1-ol. The two octenols were the predominant compounds, and sufficient sample was trapped from the gas chromatograph for infrared analyses; this confirmed the mass spectral identifications and permitted the assignment of the cis designation to 2-octen-1-ol. Both oct-1-en-3-ol and cis-2-octen-1-ol are thought to be responsible for the characteristic musty-fungal odor of certain fungi; the latter compound may be a useful chemical index of fungal growth.

  19. Activity of Antifungal Organobismuth(III Compounds Derived from Alkyl Aryl Ketones against S. cerevisiae: Comparison with a Heterocyclic Bismuth Scaffold Consisting of a Diphenyl Sulfone

    Directory of Open Access Journals (Sweden)

    Toshihiro Murafuji

    2014-07-01

    Full Text Available A series of hypervalent organobismuth(III compounds derived from alkyl aryl ketones [XBi(5-R'C6H3-2-COR(Ar] was synthesized to investigate the effect of the compounds’ structural features on their antifungal activity against the yeast Saccharomyces cerevisiae. In contrast to bismuth heterocycles [XBi(5-RC6H3-2-SO2C6H4-1'-] derived from diphenyl sulfones, a systematic quantitative structure-activity relationship study was possible. The activity depended on the Ar group and increased for heavier X atoms, whereas lengthening the alkyl chain (R or introducing a substituent (R' reduced the activity. IBi(C6H4-2-COCH3(4-FC6H4 was the most active. Its activity was superior to that of the related acyclic analogues ClBi[C6H4-2-CH2N(CH32](Ar and ClBi(C6H4-2-SO2 tert-Bu(Ar and also comparable to that of heterocyclic ClBi(C6H4-2-SO2C6H4-1'-, which was the most active compound in our previous studies. Density function theory calculations suggested that hypervalent bismuthanes undergo nucleophilic addition with a biomolecule at the bismuth atom to give an intermediate ate complex. For higher antifungal activity, adjusting the lipophilicity-hydrophilicity balance, modeling the three-dimensional molecular structure around the bismuth atom, and stabilizing the ate complex appear to be more important than tuning the Lewis acidity at the bismuth atom.

  20. Synergistic effects of tacrolimus and azole antifungal compounds in fluconazole-susceptible and fluconazole-resistant Candida glabrata isolates

    Directory of Open Access Journals (Sweden)

    Laura Bedin Denardi

    2015-03-01

    Full Text Available In vitro interaction between tacrolimus (FK506 and four azoles (fluconazole, ketoconazole, itraconazole and voriconazole against thirty clinical isolates of both fluconazole susceptible and -resistant Candida glabrata were evaluated by the checkerboard microdilution method. Synergistic, indifferent or antagonism interactions were found for combinations of the antifungal agents and FK506. A larger synergistic effect was observed for the combinations of FK506 with itraconazole and voriconazole (43%, followed by that of the combination with ketoconazole (37%, against fluconazole-susceptible isolates. For fluconazole-resistant C. glabrata, a higher synergistic effect was obtained from FK506 combined with ketoconazole (77%, itraconazole (73%, voriconazole (63% and fluconazole (60%. The synergisms that we observed in vitro, notably against fluconazole-resistant C. glabrata isolates, are promising and warrant further analysis of their applications in experimental in vivo studies.

  1. Antifungal potential of marine natural products

    OpenAIRE

    El-Hossary, Ebaa M.; Cheng, Cheng; Hamed, Mostafa M.; El-Sayed Hamed, Ashraf Nageeb; Ohlsen, Knut; Hentschel, Ute; Abdelmohsen, Usama Ramadan

    2017-01-01

    Highlights: • Fungal infections represent an increasing threat to human health. • Fungal infections in plants are a worldwide problem to the agricultural industry. • Diverse antifungal compounds were isolated from different marine organisms. • The number of new antifungal marine natural products is rapidly developing. • Marine sponges and bacteria are the predominant sources for antifungal compounds. Abstract: Fungal diseases represent an increasing threat to human healt...

  2. Antifungal activity of the ethanolic extracts of Punica granatum L. and evaluation of the morphological and structural modifications of its compounds upon the cells of Candida spp.

    Directory of Open Access Journals (Sweden)

    Paula Cristina Anibal

    2013-09-01

    Full Text Available Ethanolic crude extracts prepared from the arils and seeds, pericarp, peels and from the whole fruit of Punica granatum, known as pomegranate, had their antifungal activity tested against Candida spp. The ethanolic crude extracts were analyzed by Mass Spectrometry and yielded many compounds such as punicalagin and galladydilacton. The extracts from the pericarp and peel showed activity against Candida spp., with MICs of 125 µg/mL. The effect of pericarp and peel extracts upon the morphological and structure of C. albicans and C. krusei were examined by scanning and transmission electron microscopy, with the visualization of an irregular membrane and hyphae, formation of vacuoles and thickening of the cell wall. The data obtained revealed potential antimicrobial activity against yeasts cells of the Candida genus, and the bioactive compounds could be responsible for changes in cell morphology and structure. The data obtained open new perspectives for future research in continuation to this study, where information such as determination of the site of action of the compounds could contribute to an alternative therapy against these organisms.

  3. Antifungal activity of the ethanolic extracts of Punica granatum L. and evaluation of the morphological and structural modifications of its compounds upon the cells of Candida spp

    Science.gov (United States)

    Anibal, Paula Cristina; Peixoto, Iza Teixeira Alves; Foglio, Mary Ann; Höfling, José Francisco

    2013-01-01

    Ethanolic crude extracts prepared from the arils and seeds, pericarp, peels and from the whole fruit of Punica granatum, known as pomegranate, had their antifungal activity tested against Candida spp. The ethanolic crude extracts were analyzed by Mass Spectrometry and yielded many compounds such as punicalagin and galladydilacton. The extracts from the pericarp and peel showed activity against Candida spp., with MICs of 125 μg/mL. The effect of pericarp and peel extracts upon the morphological and structure of C. albicans and C. krusei were examined by scanning and transmission electron microscopy, with the visualization of an irregular membrane and hyphae, formation of vacuoles and thickening of the cell wall. The data obtained revealed potential antimicrobial activity against yeasts cells of the Candida genus, and the bioactive compounds could be responsible for changes in cell morphology and structure. The data obtained open new perspectives for future research in continuation to this study, where information such as determination of the site of action of the compounds could contribute to an alternative therapy against these organisms. PMID:24516425

  4. Antifungal activity of the ethanolic extracts of Punica granatum L. and evaluation of the morphological and structural modifications of its compounds upon the cells of Candida spp.

    Science.gov (United States)

    Anibal, Paula Cristina; Peixoto, Iza Teixeira Alves; Foglio, Mary Ann; Höfling, José Francisco

    2013-01-01

    Ethanolic crude extracts prepared from the arils and seeds, pericarp, peels and from the whole fruit of Punica granatum, known as pomegranate, had their antifungal activity tested against Candida spp. The ethanolic crude extracts were analyzed by Mass Spectrometry and yielded many compounds such as punicalagin and galladydilacton. The extracts from the pericarp and peel showed activity against Candida spp., with MICs of 125 μg/mL. The effect of pericarp and peel extracts upon the morphological and structure of C. albicans and C. krusei were examined by scanning and transmission electron microscopy, with the visualization of an irregular membrane and hyphae, formation of vacuoles and thickening of the cell wall. The data obtained revealed potential antimicrobial activity against yeasts cells of the Candida genus, and the bioactive compounds could be responsible for changes in cell morphology and structure. The data obtained open new perspectives for future research in continuation to this study, where information such as determination of the site of action of the compounds could contribute to an alternative therapy against these organisms.

  5. Carbonyl Compounds Produced by Vaporizing Cannabis Oil Thinning Agents.

    Science.gov (United States)

    Troutt, William D; DiDonato, Matthew D

    2017-11-01

    Cannabis use has increased in the United States, particularly the use of vaporized cannabis oil, which is often mixed with thinning agents for use in vaporizing devices. E-cigarette research shows that heated thinning agents produce potentially harmful carbonyls; however, similar studies have not been conducted (1) with agents that are commonly used in the cannabis industry and (2) at temperatures that are appropriate for cannabis oil vaporization. The goal of this study was to determine whether thinning agents used in the cannabis industry produce potentially harmful carbonyls when heated to a temperature that is appropriate for cannabis oil vaporization. Four thinning agents (propylene glycol [PG], vegetable glycerin [VG], polyethylene glycol 400 [PEG 400], and medium chain triglycerides [MCT]) were heated to 230°C and the resulting vapors were tested for acetaldehyde, acrolein, and formaldehyde. Each agent was tested three times. Testing was conducted in a smoking laboratory. Carbonyl levels were measured in micrograms per puff block. Analyses showed that PEG 400 produced significantly higher levels of acetaldehyde and formaldehyde than PG, MCT, and VG. Formaldehyde production was also significantly greater in PG compared with MCT and VG. Acrolein production did not differ significantly across the agents. PG and PEG 400 produced high levels of acetaldehyde and formaldehyde when heated to 230°C. Formaldehyde production from PEG 400 isolate was particularly high, with one inhalation accounting for 1.12% of the daily exposure limit, nearly the same exposure as smoking one cigarette. Because PG and PEG 400 are often mixed with cannabis oil, individuals who vaporize cannabis oil products may risk exposure to harmful formaldehyde levels. Although more research is needed, consumers and policy makers should consider these potential health effects before use and when drafting cannabis-related legislation.

  6. Rare earth intermetallic compounds produced by a reduction-diffusion process

    International Nuclear Information System (INIS)

    Cech, R.E.

    1975-01-01

    A reduction-diffusion process is given for producing novel rare earth intermetallic compounds, such as cobalt--rare earth intermetallic compounds, especially compounds useful in preparing permanent magnets. A particulate mixture of rare earth metal halide, cobalt and calcium hydride is heated to effect reduction of the rare earth metal halide and to diffuse the resulting rare earth metal into the cobalt to form the intermetallic compound

  7. Bioactive Compounds Produced by Hypoxylon fragiforme against Staphylococcus aureus Biofilms

    Directory of Open Access Journals (Sweden)

    Kamila Tomoko Yuyama

    2017-12-01

    Full Text Available Treating infections organized in biofilms is a challenge due to the resistance of the pathogens against antibiotics and host immune cells. Many fungi grow in a wet environment, favorable for the growth of bacterial biofilms, and we speculated that fungi possess some strategies to control these bacterial biofilms. A fungus identified as Hypoxylon fragiforme, was collected in the Harz Mountains, Germany, and its mycelial culture was fermented in different culture media for 67 days to test its biological potential against bacterial biofilms. Sclerin, sclerin diacid and its 3-methyl monoester (methyl 1-(5-hydroxy-6-carboxylic-2,3,4-trimethylphenyl propionate are here described for the first time from this fungus. Sclerin and its diacid interfered with the biofilm formation of the pathogen Staphylococcus aureus, inhibiting 86% and 80% of the biofilm at 256 μg mL−1, respectively, but not killing the bacterium. Interestingly, the monomethylester of sclerin diacid was inactive. Although these compounds did not possess any activity against a pre-formed biofilm, they prevented its formation at subtoxic concentrations. Furthermore, sclerin and its diacid displayed a high specificity against Staphylococcus aureus, indicating a good strategy against pathogenic biofilms when combined with antibiotics.

  8. An endophytic/pathogenic Phoma sp. from creosote bush producing biologically active volatile compounds having fuel potential.

    Science.gov (United States)

    Strobel, Gary; Singh, Sanjay K; Riyaz-Ul-Hassan, Syed; Mitchell, Angela M; Geary, Brad; Sears, Joe

    2011-07-01

    A Phoma sp. was isolated and characterized as endophytic and as a pathogen of Larrea tridentata (creosote bush) growing in the desert region of southern Utah, USA. This fungus produces a unique mixture of volatile organic compounds (VOCs), including a series of sesquiterpenoids, some alcohols and several reduced naphthalene derivatives. Trans-caryophyllene, a product in the fungal VOCs, was also noted in the VOCs of this pungent plant. The gases of Phoma sp. possess antifungal properties and is markedly similar to that of a methanolic extract of the host plant. Some of the test organisms with the greatest sensitivity to the Phoma sp. VOCs were Verticillium, Ceratocystis, Cercospora and Sclerotinia while those being the least sensitive were Trichoderma, Colletotrichum and Aspergillus. We discuss the possible involvement of VOC production by the fungus and its role in the biology/ecology of the fungus/plant/environmental relationship with implications for utilization as an energy source. © 2011 Federation of European Microbiological Societies. Published by Blackwell Publishing Ltd. All rights reserved.

  9. Chalcone derivatives as potential antifungal agents: Synthesis, and antifungal activity

    Directory of Open Access Journals (Sweden)

    Deepa Gupta

    2015-01-01

    Full Text Available Much research has been carried out with the aim to discover the therapeutic values of chalcone derivatives. Chalcones possess wide range of pharmacological activity such as antibacterial, antimalarial, antiprotozoal, antitubercular, anticancer, and antifungal agents etc. The presence of reactive α,β-unsaturated keto group in chalcones is found to be responsible for their biological activity. The rapid developments of resistance to antifungal agents, led to design, and synthesize the new antifungal agents. The derivatives of chalcones were prepared using Claisen-Schmidt condensation scheme with appropriate tetralone and aldehyde derivatives. Ten derivatives were synthesized and were biologically screened for antifungal activity. The newly synthesized derivatives of chalcone showed antifungal activity against fungal species, Microsporum gypseum. The results so obtained were superior or comparable to ketoconazole. It was observed that none of the compounds tested showed positive results for fungi Candida albicans nor against fungi Aspergillus niger. Chalcone derivatives showed inhibitory effect against M. gypseum species of fungus. It was found that among the chalcone derivatives so synthesized, two of them, that is, 4-chloro derivative, and unsubstituted derivative of chalcone showed antifungal activity superior to ketoconazole. Thus, these can be the potential new molecule as antifungal agent.

  10. Homology modeling of target proteins and identification novel antifungal compounds against Candida tropicalis through structure based virtual screening.

    Science.gov (United States)

    Ravinarayanan, Haribalaganesh; Paul, Bibhash K; Chakraborty, Angshu; Sundar, Krishnan

    2015-08-01

    Candida tropicalis, the etiological agent of candidiasis evades the immune system and survive in the human host for decades. Currently there are not many drugs available in the market to treat these fungal infections. The increasing number of fungal infections necessitates the need for new drug candidates that can be used to treat fungal infections such as candida. Many natural products available in plants, animals and microorganisms exhibit potent anti-microbial activity; but they are not explored to their potential. Virtual screening of anti-microbials against known targets accelerates the process of drug discovery and development. In the present study, a total of 27 compounds of natural origin such as plants, microbes and marine sponges were evaluated for their ability to interact with four of the new targets. The study revealed the effectiveness of 3 compounds with improved binding affinity against the four target proteins; that could be used as lead compounds in designing new drug candidates.

  11. The influence of iron coordination compounds on producing capacity of some crops

    International Nuclear Information System (INIS)

    Rakhimova, M.M.; Yusupov, Z.N.; Nurmatov, T.M.; Dzhafarov, M.I.

    1993-01-01

    Present article is devoted to influence of iron coordination compounds on producing capacity of some crops. The influence of aqueous solutions of iron coordination compounds with anions of acetic and ethylen diamin disuccinic acids on germinative energy and germination of cotton crops and grapes was studied in laboratory conditions. The conducted researches shown that application of iron coordination compounds improves the growth, fruiting and the quality of studied crops.

  12. Gain and loss of fruit flavour compounds produced by wild and cultivated strawberry species

    NARCIS (Netherlands)

    Aharoni, A.; Giri, A.P.; Verstappen, F.W.A.; Bertea, C.M.; Sevenier, R.E.; Sun, Z.; Jongsma, M.A.; Schwab, W.; Bouwmeester, H.J.

    2004-01-01

    The blends of flavor compounds produced by fruits serve as biological perfumes used to attract living creatures, including humans. They include hundreds of metabolites and vary in their characteristic fruit flavor composition. The molecular mechanisms by which fruit flavor and aroma compounds are

  13. Exposure assessment of cattle via roughages to plants producing compounds of concern

    NARCIS (Netherlands)

    Raamsdonk, van L.W.D.; Ozinga, W.A.; Hoogenboom, L.A.P.; Mulder, P.P.J.; Mol, J.G.J.; Groot, M.J.; Fels, van der H.J.; Nijs, de W.C.M.

    2015-01-01

    Food producing animals are exposed to biologically active plant compounds through feed and roughages, presenting a potential risk to the animal but also consumers of food of animal origin. To evaluate to which plant compounds of concern dairy cows in the Netherlands are exposed, a ranking filter

  14. Potential of volatile compounds produced by fungi to influence sensory quality of coffee beverage

    DEFF Research Database (Denmark)

    Iamanaka, B. T.; Teixeira, A. A.; Teixeira, A. R. R.

    2014-01-01

    Fungi are known producers of a large number of volatile compounds (VCs). Several VCs such as 2,4,6 trichloroanisole (TCA), geosmin and terpenes have been found in coffee beverages, and these compounds can be responsible for off-flavor development. However, few studies have related the fungal...

  15. Antifungal Lipopeptides Produced by Bacillus sp. FJAT-14262 Isolated from Rhizosphere Soil of the Medicinal Plant Anoectochilus roxburghii.

    Science.gov (United States)

    Chen, Qianqian; Liu, Bo; Wang, Jieping; Che, Jianmei; Liu, Guohong; Guan, Xiong

    2017-05-01

    This study aimed to develop biocontrol Bacillus and explore bacterial biocontrol substances. According to the blood agar test, strain FJAT-14262 was screened as a biosurfactant-producer. The biosurfactant-producing ability of FJAT-14262 was further confirmed by the oil spreading tests because of its amphipathic character. Furthermore, its fermentation supernatant could decrease the surface tension from 74.1 to 32.7 mN m -1 . Fourier transform infrared spectroscopy (FT-IR) analysis indicated that the biosurfactant produced by the strain FJAT-14262 was a kind of lipopeptides. Reverse-phase high-performance liquid chromatography (RP-HPLC) and liquid chromatography-mass spectrometry (LC-MS) analysis demonstrated that this lipopeptide contained surfactin with polar amino acids and hydrophobic fatty acid chains. Moreover, bioinformatic analysis revealed that the nonribosomal peptide synthetases genes srfAA, srfAB, and srfAC were structurally conserved in the FJAT-14262 genome. Importantly, the crude surfactant exhibited strong inhibitory activities against Fusarium oxysporum, suggesting that strain FJAT-14262 could be a potential biological control agent against Fusarium wilt.

  16. Exposure assessment of cattle via roughages to plants producing compounds of concern.

    Science.gov (United States)

    van Raamsdonk, L W D; Ozinga, W A; Hoogenboom, L A P; Mulder, P P J; Mol, J G J; Groot, M J; van der Fels-Klerx, H J; de Nijs, M

    2015-12-15

    Food producing animals are exposed to biologically active plant compounds through feed and roughages, presenting a potential risk to the animal but also consumers of food of animal origin. To evaluate to which plant compounds of concern dairy cows in the Netherlands are exposed, a ranking filter model was developed, combining information on abundance of plant species in vegetation plots in the Netherlands (183,905 plots of three different vegetation types) with plant-compound combinations (700), and with consumption data of fresh grass, grass silage and corn silage by cattle. The most abundant plant genera are those producing cyanogenic glycosides, coumarins and benzofuranocoumarins, being predominantly fodder plants (alfalfa, clover and some grasses) considered to be safe. Highest exposures were estimated for plant genera producing piperidine alkaloids (horsetail), furanocoumarins (parsley and relatives), pyrrolizidine alkaloids (Symphytum, Senecio, Leucanthemum, Eupatorium) and essential oils. The current results allow to prioritise future scientific research on these compounds. Copyright © 2015 Elsevier Ltd. All rights reserved.

  17. Antifungal activity of synthetic antiseptics and natural compounds against Candida dubliniensis before and after in vitro fluconazole exposure

    Directory of Open Access Journals (Sweden)

    Cássia Franco Reginato

    Full Text Available ABSTRACT INTRODUCTION: This study evaluated the susceptibilities of oral candidiasis-derived Candida albicans, fluconazole-resistant (FR Candida dubliniensis, and fluconazole-susceptible (FS C. dubliniensis to synthetic antiseptics [chlorhexidine gluconate (CHX, cetylpyridinium chloride (CPC, and triclosan (TRC] and natural compounds (carvacrol, eugenol and thymol. METHODS: Susceptibility tests were performed based on the M27-A3 reference method. The fluconazole-resistant C. dubliniensis strains were obtained after prolonged in vitro exposure to increasing fluconazole concentrations. The geometric mean values for minimum inhibitory concentrations and minimum fungicidal concentrations were compared among the groups. RESULTS: Fluconazole-susceptible C. dubliniensis was more sensitive to CPC and TRC than FR C. dubliniensis and C. albicans were. However, eugenol and thymol were more active against FR C. dubliniensis. The fungicidal activities of CHX and TRC were similar for the three groups, and FR C. dubliniensis and C. albicans had similar sensitivities to CPC. CONCLUSIONS: The resistance of C. dubliniensis to fluconazole affects its sensitivity the synthetic antiseptics and natural compounds that were tested.

  18. Draft Genome Sequence of Hoeflea sp. Strain BAL378, a Potential Producer of Bioactive Compounds

    DEFF Research Database (Denmark)

    Bentzon-Tilia, Mikkel; Riemann, Lasse; Gram, Lone

    2014-01-01

    Some phytoplankton-associated marine bacteria produce bioactive compounds. Members of the genus Hoeflea may be examples of such bacteria; however, data describing their metabolisms are scarce. Here, we report the draft genome sequence of Hoeflea sp. strain BAL378, a putative producer of bacterioc...... of bacteriocins, polyketides, and auxins, as demonstrated by genome mining....

  19. Parasiticidal, antifungal and antibacterial activities of Onosma ...

    African Journals Online (AJOL)

    STORAGESEVER

    2009-10-05

    Oct 5, 2009 ... neubauer counting chamber and IC50 values of compounds pos- sessing antileishmanial activity were calculated by Software Ezfit. 5.03 Perella Scientific. IC50 values of different fractions against the test pathogen are mentioned in Table 1. Antifungal activity. Similarly antifungal activity was evaluated by ...

  20. INVESTIGATION OF ANTIFUNGAL ACTIVITY OF QUINOLINIUM DERIVATIVES

    Directory of Open Access Journals (Sweden)

    G. A. Alexandrova

    2013-01-01

    Full Text Available Abstract. Antifungal activity (Candida albicans, Candida krusei of some substituted quinolinium derivatives has been investigated. It was established that the most perspective compound for detail investigation of antifungal activity by labeled biomarkers method was N-phenylbenzoquinaldinium tetrafluoroborate.

  1. Volatile compounds of Aspergillus strains with different abilities to produce ochratoxin A.

    Science.gov (United States)

    Jeleń, Henryk H; Grabarkiewicz-Szczesna, Jadwiga

    2005-03-09

    Volatile compounds emitted by Aspergillus strains having different abilities to produce ochratoxin A were investigated. Thirteen strains of Aspergillus ochraceus, three belonging to the A. ochraceus group, and eight other species of Aspergillus were examined for their abilities to produce volatile compounds and ochratoxin A on a wheat grain medium. The profiles of volatile compounds, analyzed using SPME, in all A. ochraceus strains, regardless of their toxeginicity, were similar and comprised mainly of 1-octen-3-ol, 3-octanone, 3-octanol, 3-methyl-1-butanol, 1-octene, and limonene. The prevailing compound was always 1-octen-3-ol. Mellein, which forms part of the ochratoxin A molecule, was found in both toxigenic and nontoxigenic strains. Volatile compounds produced by other Aspergillus strains were similar to those of A. ochraceus. Incubation temperatures (20, 24, and 27 degrees C) and water content in the medium (20, 30, and 40%) influenced both volatile compounds formation and ochratoxin A biosynthesis efficiency, although conditions providing the maximum amount of volatiles were different from those providing the maximum amount of ochratoxin A. The pattern of volatiles produced by toxigenic A. ochraceus strains does not facilitate their differentiation from nontoxigenic strains.

  2. Marine Pharmacology in 2012–2013: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti-Inflammatory, Antiprotozoal, Antituberculosis, and Antiviral Activities; Affecting the Immune and Nervous Systems, and Other Miscellaneous Mechanisms of Action

    Directory of Open Access Journals (Sweden)

    Alejandro M. S. Mayer

    2017-08-01

    Full Text Available The peer-reviewed marine pharmacology literature from 2012 to 2013 was systematically reviewed, consistent with the 1998–2011 reviews of this series. Marine pharmacology research from 2012 to 2013, conducted by scientists from 42 countries in addition to the United States, reported findings on the preclinical pharmacology of 257 marine compounds. The preclinical pharmacology of compounds isolated from marine organisms revealed antibacterial, antifungal, antiprotozoal, antituberculosis, antiviral and anthelmitic pharmacological activities for 113 marine natural products. In addition, 75 marine compounds were reported to have antidiabetic and anti-inflammatory activities and affect the immune and nervous system. Finally, 69 marine compounds were shown to display miscellaneous mechanisms of action which could contribute to novel pharmacological classes. Thus, in 2012–2013, the preclinical marine natural product pharmacology pipeline provided novel pharmacology and lead compounds to the clinical marine pharmaceutical pipeline, and contributed significantly to potentially novel therapeutic approaches to several global disease categories.

  3. Nepenthes rafflesiana pitcher liquid has antifungal activity against Candida spp.

    OpenAIRE

    Hanna Yolanda; Ingrid M. Makahinda; Maureen Aprilia; Nikki Sanjaya; Harry Gunawan; Rita Dewi

    2015-01-01

    BACKGROUND To develop new effective antifungals, it is essential to search for antifungal compounds from plants such as Nepenthes spp., which have their greatest diversity in Indonesia. Since chitin-induced liquid (CIL) from Nepenthes khasiana pitchers has antifungal activity, due to their naphthoquinone content, this study aimed to evaluate antifungal activity of Nepenthes rafflesiana pitcher liquids on Candida spp. METHODS Collected pitcher liquids were of 3 types: non-induced l...

  4. Introduction and comparison of measurement methods of antifungal properties of lactic acid bacteria in cheese

    Directory of Open Access Journals (Sweden)

    H Sedaghat

    2014-02-01

    Full Text Available Various laboratory methods have been developed to evaluate the effectiveness of anti-mould effect of lactic acid bacteria. However, most of these investigations have been conducted in culture medium. Due to the occurrence of complex interaction between food components and antimicrobial substances produced by lactic acid bacteria, the result achieved from these studies may be different from those seen in food model. In various studies growth inhibition of molds on the surface of foods are considered as antifungal activity. Consequently, introduction and comparison of efficient methods for evaluation of anti-mould effect of lactic acid bacteria would be helpful. In this study, antifungal activity of lactic acid bacteria inoculated in cheese was estimated using Microdilution method. Pieces of cheese samples were overlaid with molds and the antifungal effect of this bacteria was studied against Aspergillus flavus and Aspergillus parasiticus. All three methods showed the effectiveness of lactic bacteria on mold inhibition. Comparison of the results showed that there was significant positive correlation between antifungal overlay assay and direct growth of mold on cheese, since this two test showed antifungal effect in the same way including interaction between bacteria and mold and also producing antifungal compound.

  5. Use of the Soft-agar Overlay Technique to Screen for Bacterially Produced Inhibitory Compounds.

    Science.gov (United States)

    Hockett, Kevin L; Baltrus, David A

    2017-01-14

    The soft-agar overlay technique was originally developed over 70 years ago and has been widely used in several areas of microbiological research, including work with bacteriophages and bacteriocins, proteinaceous antibacterial agents. This approach is relatively inexpensive, with minimal resource requirements. This technique consists of spotting supernatant from a donor strain (potentially harboring a toxic compound(s)) onto a solidified soft agar overlay that is seeded with a bacterial test strain (potentially sensitive to the toxic compound(s)). We utilized this technique to screen a library of Pseudomonas syringae strains for intraspecific killing. By combining this approach with a precipitation step and targeted gene deletions, multiple toxic compounds produced by the same strain can be differentiated. The two antagonistic agents commonly recovered using this technique are bacteriophages and bacteriocins. These two agents can be differentiated using two simple additional tests. Performing a serial dilution on a supernatant containing bacteriophage will result in individual plaques becoming less in number with greater dilution, whereas serial dilution of a supernatant containing bacteriocin will result a clearing zone that becomes uniformly more turbid with greater dilution. Additionally, a bacteriophage will produce a clearing zone when spotted onto a fresh soft agar overlay seeded with the same strain, whereas a bacteriocin will not produce a clearing zone when transferred to a fresh soft agar lawn, owing to the dilution of the bacteriocin.

  6. The Elements of Antifungal Drug Discovery

    DEFF Research Database (Denmark)

    Kjellerup, Lasse

    compounds (ZACs). Zinc is an important micronutrient and the immune system is known to operate with a similar mechanism to the ZACs by scavenging zinc from the site of infection, thus preventing the growth of pathogens through zinc starvation. In addition to the observations made about the ZAC compounds......In this PhD thesis I will explore the development of antifungal drugs. Fungal infections are estimated to cause the death of 1.5 million patients each year. There is currently a need for new antifungal drugs as the existing drugs are hampered by lack of broad-spectrum antifungal activity...

  7. Degradation of Total Petroleum Hydrocarbon and BTEX Compounds in Produced Water

    Energy Technology Data Exchange (ETDEWEB)

    Jackson, Lorri

    2002-04-01

    Petroleum Environmental Technologies, LLC entered into a Cooperative Research and Development agreement with the Rocky Mountain Oilfield Testing Center to an in-situ pit treatment demonstration and produced water treatment demonstration. The purpose of the test is to demonstrate the degradation of petroleum hydrocarbon compounds in soil and aqueous matrices where ECOSAFE is applied to enhance the degradation of these contaminants.

  8. Method of producing granulates of a semiconductor compound from arsenic selenide

    International Nuclear Information System (INIS)

    Vogel, G.; Preslawski, N.

    1980-01-01

    Granulates are produced from As 2 S 3 , As 2 O 5 , alloys of selenic/tellurium, or compound systems based on chalcogenides. For this purpose the original substance consisting of As and Se is filled as loose material into the reactor of an equipment that has got an electric heating and a mixer-settler for homogenizing the melting phase of the mixture. In this way a product is formed meeting the requirements for a photoconductor compound to be evaporated in high-vacuum. (DG) [de

  9. Production and Recovery of Aroma Compounds Produced by Solid-State Fermentation Using Different Adsorbents

    Directory of Open Access Journals (Sweden)

    Adriane B. P. Medeiros

    2006-01-01

    Full Text Available Volatile compounds with fruity characteristics were produced by Ceratocystis fimbriata in two different bioreactors: columns (laboratory scale and horizontal drum (semi-pilot scale. Coffee husk was used as substrate for the production of volatile compounds by solid-state fermentation. The production of volatile compounds was significantly higher when horizontal drum bioreactor was used than when column bioreactors were used. These results showed that this model of bioreactor presents good perspectives for scale-up and application in an industrial production. Headspace analysis of the solid-state culture detected twelve compounds, among them: ethanol, acetaldehyde, ethyl acetate, ethyl propionate, and isoamyl acetate. Ethyl acetate was the predominant product in the headspace (28.55 µmol/L/g of initial dry matter. Activated carbon, Tenax-TA, and Amberlite XAD-2 were tested to perform the recovery of the compounds. The adsorbent columns were connected to the column-type bioreactor. All compounds present in the headspace of the columns were adsorbed in Amberlite XAD-2. With Tenax-TA, acetaldehyde was adsorbed in higher concentrations. However, the recovery found by using the activated carbon was very low.

  10. Antifungal Streptomyces spp. associated with the infructescences of Protea spp. in South Africa

    Directory of Open Access Journals (Sweden)

    Zander Human

    2016-11-01

    Full Text Available Common saprophytic fungi are seldom present in Protea infructescences, which is strange given the abundance of mainly dead plant tissue in this moist protected environment. We hypothesized that the absence of common saprophytic fungi in Protea infructescences could be due to a special symbiosis where the presence of microbes producing antifungal compounds protect the infructescence. Using a culture based survey, employing selective media and in vitro antifungal assays, we isolated antibiotic producing actinomycetes from infructescences of Protea repens and P. neriifolia from two geographically separated areas. Isolates were grouped into three different morphological groups and appeared to be common in the Protea spp. examined in this study. The three groups were supported in 16S rRNA and multi-locus gene trees and were identified as potentially novel Streptomyces spp. All of the groups had antifungal activity in vitro. Streptomyces sp. Group 1 had inhibitory activity against all tested fungi and the active compound produced by this species was identified as fungichromin. Streptomyces spp. Groups 2 and 3 had lower inhibition against all tested fungi, while Group 3 showed limited inhibition against Candida albicans and Sporothrix isolates. The active compound for Group 2 was also identified as fungichromin even though its production level was much lower than Group 1. The antifungal activity of Group 3 was linked to actiphenol. The observed antifungal activity of the isolated actinomycetes could contribute to protection of the plant material against common saprophytic fungi, as fungichromin was also detected in extracts of the infructescence. The results of this study suggest that the antifungal Streptomyces spp. could play an important role in defining the microbial population associated with Protea infructescences.

  11. Antifungal Streptomyces spp. Associated with the Infructescences of Protea spp. in South Africa

    Science.gov (United States)

    Human, Zander R.; Moon, Kyuho; Bae, Munhyung; de Beer, Z. Wilhelm; Cha, Sangwon; Wingfield, Michael J.; Slippers, Bernard; Oh, Dong-Chan; Venter, Stephanus N.

    2016-01-01

    Common saprophytic fungi are seldom present in Protea infructescences, which is strange given the abundance of mainly dead plant tissue in this moist protected environment. We hypothesized that the absence of common saprophytic fungi in Protea infructescences could be due to a special symbiosis where the presence of microbes producing antifungal compounds protect the infructescence. Using a culture based survey, employing selective media and in vitro antifungal assays, we isolated antibiotic producing actinomycetes from infructescences of Protea repens and P. neriifolia from two geographically separated areas. Isolates were grouped into three different morphological groups and appeared to be common in the Protea spp. examined in this study. The three groups were supported in 16S rRNA and multi-locus gene trees and were identified as potentially novel Streptomyces spp. All of the groups had antifungal activity in vitro. Streptomyces sp. Group 1 had inhibitory activity against all tested fungi and the active compound produced by this species was identified as fungichromin. Streptomyces spp. Groups 2 and 3 had lower inhibition against all tested fungi, while Group 3 showed limited inhibition against Candida albicans and Sporothrix isolates. The active compound for Group 2 was also identified as fungichromin even though its production level was much lower than Group 1. The antifungal activity of Group 3 was linked to actiphenol. The observed antifungal activity of the isolated actinomycetes could contribute to protection of the plant material against common saprophytic fungi, as fungichromin was also detected in extracts of the infructescence. The results of this study suggest that the antifungal Streptomyces spp. could play an important role in defining the microbial population associated with Protea infructescences. PMID:27853450

  12. Natural and synthetic peptides with antifungal activity.

    Science.gov (United States)

    Ciociola, Tecla; Giovati, Laura; Conti, Stefania; Magliani, Walter; Santinoli, Claudia; Polonelli, Luciano

    2016-08-01

    In recent years, the increase of invasive fungal infections and the emergence of antifungal resistance stressed the need for new antifungal drugs. Peptides have shown to be good candidates for the development of alternative antimicrobial agents through high-throughput screening, and subsequent optimization according to a rational approach. This review presents a brief overview on antifungal natural peptides of different sources (animals, plants, micro-organisms), peptide fragments derived by proteolytic cleavage of precursor physiological proteins (cryptides), synthetic unnatural peptides and peptide derivatives. Antifungal peptides are schematically reported based on their structure, antifungal spectrum and reported effects. Natural or synthetic peptides and their modified derivatives may represent the basis for new compounds active against fungal infections.

  13. Antibióticos antifúngicos produzidos por actinomicetos do Brasil e sua determinação preliminar nos meios experimentais Antifungal antibiotics produced by Brazilian actinomycetes and its preliminary determination in experimental media

    Directory of Open Access Journals (Sweden)

    Keidi Ujikawa

    2003-06-01

    Full Text Available Várias amostras de solo do Brasil foram semeadas em placas de ágar e diversas cepas de actinomicetos produtoras de antibióticos antifúngicos foram isoladas. Foram desenvolvidos meios para eliciação da biossíntese dos antibióticos e métodos para determinação rápida do seu rendimento. Ao todo, foram isoladas 41 cepas de actinomicetos aeróbios produtoras de metabólitos antifúngicos. Destes, 11 (26,8% eram macrolídeos tetraênicos, 13 (31,7% macrolídeos pentaênicos, 1 (2,4%, macrolídeo oxopentaênico, 1 (2,4% macrolídeo hexaênico e 6 (14,6% macrolídeos heptaênicos. Os antibióticos antifúngicos produzidos pelas restantes 9 cepas ativas (21,9% não eram poliênicos. Os poliênicos mais utilizados atualmente na clínica são do tipo tetraênico (nistatina e heptaênico (anfotericina B. Um meio à base de leite de soja favoreceu extraordinariamente a eliciação da biossíntese de polienos por algumas cepas, enquanto que para outras não houve favorecimento e para outras foi prejudicial. Os rendimentos obtidos atingiram cerca de 6000 U de antibióticos poliênicos por mL.Various Brazilian soil samples were seeded in agar plates and several strains of antifungal antibiotic producing actinomycetes were isolated. Antibiotic biosynthesis elicitation media were developed and methods for determination of yields were studied. A total of 41 antifungal antibiotic producing strains of aerobic actinomycetes resulted. Among the antibiotics produced, 11 (26.8% were grouped as macrolide tetraenes, 13 (31.7% as pentaenes, 1 (2.4% as oxo pentaene, 1 (2.4% as hexaene and 6 (14.6% as heptaenes. Several of these strains also produced antibacterial antibiotics, like polyether antibiotics. The remaining 9 active strains (21.9% produced non polyene type of antifungals. A medium based on soybean milk favored extraordinarily the elicitation of polyenes biosynthesis by some native strains, while with other strains, this was not favored, while with

  14. Bioactive Compound Rich Indian Spices Suppresses the Growth of β-lactamase Produced Multidrug Resistant Bacteria

    OpenAIRE

    Eadlapalli Siddhartha; Vemula Sarojamma; Vadde Ramakrishna

    2017-01-01

    Background: Multidrug Resistance (MDR) among bacteria become a global concern due to failure of antibiotics, is drawn attention for best antimicrobials from the spices which have been using ancient days in Indian culinary and traditional medicine. Aim and Objectives: The present study was undertaken to evaluate the bioactive compounds and their antibacterial activity in routinely used culinary Indian spices against β-lactamase produced MDR bacteria. Material and Methods: Ethanolic extracts p...

  15. Improvement of a synthetic lure for Anopheles gambiae using compounds produced by human skin microbiota.

    Science.gov (United States)

    Verhulst, Niels O; Mbadi, Phoebe A; Kiss, Gabriella Bukovinszkiné; Mukabana, Wolfgang R; van Loon, Joop J A; Takken, Willem; Smallegange, Renate C

    2011-02-08

    Anopheles gambiae sensu stricto is considered to be highly anthropophilic and volatiles of human origin provide essential cues during its host-seeking behaviour. A synthetic blend of three human-derived volatiles, ammonia, lactic acid and tetradecanoic acid, attracts A. gambiae. In addition, volatiles produced by human skin bacteria are attractive to this mosquito species. The purpose of the current study was to test the effect of ten compounds present in the headspace of human bacteria on the host-seeking process of A. gambiae. The effect of each of the ten compounds on the attractiveness of a basic blend of ammonia, lactic and tetradecanoic acid to A. gambiae was examined. The host-seeking response of A. gambiae was evaluated in a laboratory set-up using a dual-port olfactometer and in a semi-field facility in Kenya using MM-X traps. Odorants were released from LDPE sachets and placed inside the olfactometer as well as in the MM-X traps. Carbon dioxide was added in the semi-field experiments, provided from pressurized cylinders or fermenting yeast. The olfactometer and semi-field set-up allowed for high-throughput testing of the compounds in blends and in multiple concentrations. Compounds with an attractive or inhibitory effect were identified in both bioassays. 3-Methyl-1-butanol was the best attractant in both set-ups and increased the attractiveness of the basic blend up to three times. 2-Phenylethanol reduced the attractiveness of the basic blend in both bioassays by more than 50%. Identification of volatiles released by human skin bacteria led to the discovery of compounds that have an impact on the host-seeking behaviour of A. gambiae. 3-Methyl-1-butanol may be used to increase mosquito trap catches, whereas 2-phenylethanol has potential as a spatial repellent. These two compounds could be applied in push-pull strategies to reduce mosquito numbers in malaria endemic areas.

  16. Potent Antifungal Activity of Pure Compounds from Traditional Chinese Medicine Extracts against Six Oral Candida Species and the Synergy with Fluconazole against Azole-Resistant Candida albicans

    Directory of Open Access Journals (Sweden)

    Zhimin Yan

    2012-01-01

    Full Text Available This study was designed to evaluate the in vitro antifungal activities of four traditional Chinese medicine (TCM extracts. The inhibitory effects of pseudolaric acid B, gentiopicrin, rhein, and alion were assessed using standard disk diffusion and broth microdilution assays. They were tested against six oral Candida species, Candida albicans, Candida glabrata, Candida tropicalis, Candida krusei, Candida dubliniensis, and Candida guilliermondii, including clinical isolates from HIV-negative, HIV-positive, and Sjögren's syndrome patients. It was found that pseudolaric acid B had the most potent antifungal effect and showed similar antifungal activity to all six Candida spp, and to isolates from HIV-negative, HIV-positive, and Sjögren's syndrome patients. The MIC values ranged from 16 to 128 μg/mL. More interestingly, a synergistic effect of pseudolaric acid B in combination with fluconazole was observed. We suggest that pseudolaric acid B might be a potential therapeutic fungicidal agent in treating oral candidiasis.

  17. Compounds producing an effective combinatorial regimen for disruption of HIV-1 latency.

    Science.gov (United States)

    Hashemi, Pargol; Barreto, Kris; Bernhard, Wendy; Lomness, Adam; Honson, Nicolette; Pfeifer, Tom A; Harrigan, P Richard; Sadowski, Ivan

    2018-02-01

    Highly active antiretroviral therapy (HAART) has improved the outlook for the HIV epidemic, but does not provide a cure. The proposed "shock-and-kill" strategy is directed at inducing latent HIV reservoirs, which may then be purged via boosted immune response or targeting infected cells. We describe five novel compounds that are capable of reversing HIV latency without affecting the general T-cell activation state. The new compounds exhibit synergy for reactivation of latent provirus with other latency-reversing agents (LRAs), in particular ingenol-3-angelate/PEP005. One compound, designated PH02, was efficient at reactivating viral transcription in several cell lines bearing reporter HIV-1 at different integration sites. Furthermore, it was capable of reversing latency in resting CD4 + T lymphocytes from latently infected aviremic patient cells on HAART, while producing minimal cellular toxicity. The combination of PH02 and PEP005 produces a strong synergistic effect for reactivation, as demonstrated through a quantitative viral outgrowth assay (qVOA), on CD4 + T lymphocytes from HIV-1-infected individuals. We propose that the PH02/PEP005 combination may represent an effective novel treatment for abrogating persistent HIV-1 infection. © 2017 The Authors. Published under the terms of the CC BY 4.0 license.

  18. Phenolic compounds and antioxidant activity in red fruits produced in organic farming

    Directory of Open Access Journals (Sweden)

    Susana M. A. Soutinho

    2014-01-01

    Full Text Available In this work were studied three red fruits (raspberry, gooseberry and blueberry produced in organic mode, to evaluate the variations in the content of phenolic compounds and antioxidant capacity along maturation. The phenols were extracted from the fruits with two solvents (methanol and acetone and were quantified by the Folin-Ciocalteu method. The antioxidant activity was determined with two methods (HPPH and ABTS. Furthermore, HPLC was used to identify and quantify some phenolic compounds present in the fruits analyzed. The results showed that the total phenolic compounds in all fruits decreased along maturation, either in the methanol or acetone extracts (23 % and 20 % reduction, on average, for methanol and acetone extracts, respectively, although in methanol extracts the levels of phenolic compounds were always higher (0.54 and 0.21 mg GAE/g. The blueberry showed higher level of total phenolics in methanol extract (average 0.67 mg GAE/g, while in the acetone extract it was gooseberry (average 0.31 mg GAE/g. At the end of maturation, all fruits studied had similar values of antioxidant capacity as determined by DPPH method (0.52 mmol Trolox/g. For the ABTS method, blueberries showed higher values of antioxidant activity (6.01 mmol Trolox/g against 3.01 and 2.66 mmol Trolox/g, for raspberry and gooseberry, respectively. Furthermore, the HPLC analysis allowed to identify monomeric anthocyanins and phenolic acids in the three fruits studied.

  19. Production, optimization, characterization and antifungal activity of ...

    African Journals Online (AJOL)

    SAM

    2014-04-02

    Apr 2, 2014 ... the present study, the antifungal activity of crude A. terrus chitinase was investigated against Apergillus niger, Aspergillus oryzae .... Chitinase activity was determined spectrophotometrically by estimating the amount of ..... characterization of two. Bifunctional chitinases lysozyme extracellularly produced by.

  20. Identification of an antifungal metabolite produced by a potential biocontrol Actinomyces strain A01 Identificação de um metabólito antifúngico produzido pela cepa Actinomyces A01

    Directory of Open Access Journals (Sweden)

    Cai Ge Lu

    2008-12-01

    Full Text Available Actinomyces strain A01 was isolated from soil of a vegetable field in the suburb of Beijing, China. According to the morphological, cultural, physiological and biochemical characteristics, and 16S rDNA sequence analysis, strain A01 was identified as Streptomyces lydicus. In the antimicrobial spectrum test strain A01 presented a stable and strong inhibitory activity against several plant pathogenic fungi such as Fusarium oxysporum, Botrytis cinerea, Monilinia laxa, etc. However, no antibacterial activity was found. In pot experiments in greenhouse, the development of tomato gray mold was markedly suppressed by treatment with the fermentation broth of the strain A01, and the control efficacy was higher than those of Pyrimethanil and Polyoxin. A main antifungal compound (purity 99.503% was obtained from the fermentation broth of strain A01 using column chromatography and HPLC. The chemical structural analysis with UV, IR, MS, and NMR confirmed that the compound produced by the strain A01 is natamycin, a polyene antibiotic produced by S. chattanovgensis, S. natalensis, and S. gilvosporeus, widely used as a natural biological preservative for food according to previous reports. The present study revealed a new producing strain of natamycin and its potential application as a biological control agent for fungal plant diseases.A cepa Actinomyces A01 foi isolada do solo de um campo agrícola no subúrbio de Beijing, China. De acordo com as características morfológicas, culturais, fisiológicas e bioquímicas, e análise da sequência 16S rDNA , a cepa A01 foi identificada como Streptomyces lydicus. Nos testes de espectro antimicrobiano, a cepa A01 apresentou atividade inibitória intensa e estável contra vários fungos patogênicos para plantas, como Fusarium oxysporum, Botrytis cinerea, Monilia laxa, etc. Entretanto, não foi encontrada atividade antibacteriana. Em experimentos em estufas, o desenvolvimento do fungo cinza do tomate foi fortemente

  1. Characterization of the Antibiotic Compound No. 70 Produced by Streptomyces sp. IMV-70

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    Lyudmila P. Trenozhnikova

    2012-01-01

    Full Text Available We describe the actinomycete strain IMV-70 isolated from the soils of Kazakhstan, which produces potent antibiotics with high levels of antibacterial activity. After the research of its morphological, chemotaxonomic, and cultural characteristics, the strain with potential to be developed further as a novel class of antibiotics with chemotherapeutics potential was identified as Streptomyces sp. IMV-70. In the process of fermentation, the strain Streptomyces spp. IMV-70 produces the antibiotic no. 70, which was isolated from the culture broth by extraction with organic solvents. Antibiotic compound no. 70 was purified and separated into individual components by HPLC, TLC, and column chromatography methods. The main component of the compound is the antibiotic 70-A, which was found to be identical to the peptolide etamycin A. Two other antibiotics 70-B and 70-C have never been described and therefore are new antibiotics. The physical-chemical and biological characteristics of these preparations were described and further researched. Determination of the optimal growth conditions to cultivate actinomycete-producer strain IMV-70 and development of methods to isolate, purify, and accumulate preparations of the new antibiotic no. 70 enable us to research further the potential of this new class of antibiotics.

  2. Characterization of the Antibiotic Compound No. 70 Produced by Streptomyces sp. IMV-70

    Science.gov (United States)

    Trenozhnikova, Lyudmila P.; Khasenova, Almagul K.; Balgimbaeva, Assya S.; Fedorova, Galina B.; Katrukha, Genrikh S.; Tokareva, Nina L.; Kwa, Boo H.; Azizan, Azliyati

    2012-01-01

    We describe the actinomycete strain IMV-70 isolated from the soils of Kazakhstan, which produces potent antibiotics with high levels of antibacterial activity. After the research of its morphological, chemotaxonomic, and cultural characteristics, the strain with potential to be developed further as a novel class of antibiotics with chemotherapeutics potential was identified as Streptomyces sp. IMV-70. In the process of fermentation, the strain Streptomyces spp. IMV-70 produces the antibiotic no. 70, which was isolated from the culture broth by extraction with organic solvents. Antibiotic compound no. 70 was purified and separated into individual components by HPLC, TLC, and column chromatography methods. The main component of the compound is the antibiotic 70-A, which was found to be identical to the peptolide etamycin A. Two other antibiotics 70-B and 70-C have never been described and therefore are new antibiotics. The physical-chemical and biological characteristics of these preparations were described and further researched. Determination of the optimal growth conditions to cultivate actinomycete-producer strain IMV-70 and development of methods to isolate, purify, and accumulate preparations of the new antibiotic no. 70 enable us to research further the potential of this new class of antibiotics. PMID:22536145

  3. Evaluation of various ions and compounds on nitrilase produced from Streptomyces sp.

    Science.gov (United States)

    Khandelwal, Amit Kumar; Nigam, Vinod Kumar; Vidyarthi, Ambarish S; Ghosh, Purnendu

    2010-01-01

    The nitrilase produced from a new isolate is evaluated for its activity in presence of a number of different ions and compounds at optimal conditions. It was found that the activity of nitrilase increased up to 10-20% in presence of most of the divalent ions at a concentration of 5 mM relative to the control. Silver, mercury, tin, DTT, ascorbic acid and thiourea, respectively, were observed as potential inhibitors of the enzyme catalysis. The investigation on storage stability of whole cells in presence of a number of stabilizers showed that the enzyme is stable (relative activity 50%) for more than 120 days at various temperatures.

  4. Complete genome sequence of a natural compounds producer, Streptomyces violaceus S21

    Directory of Open Access Journals (Sweden)

    Jiafang Fu

    2017-06-01

    Full Text Available The complete genome sequence of Streptomyces violaceus strain S21, a valuable natural compounds producer isolated from the forest soil, is firstly presented here. The genome comprised 7.91M bp, with a G+C content of 72.65%. A range of genes involved in pathways of secondary product biosynthesis were predicted. The genome sequence is available at DDBJ/EMBL/Genbank under the accession number CP020570. This genome is annotated with 6856 predicted genes identifying the natural product biosynthetic gene clusters in S. violaceus.

  5. Lateralization of spike and wave complexes produced by hallucinogenic compounds in the cat.

    Science.gov (United States)

    Contreras, C M; Dorantes, M E; Mexicano, G; Guzmán-Flores, C

    1986-06-01

    The ability of four hallucinogenic compounds--ketamine, phencyclidine, quipazine, and SKF-10 047--to produce some specific electrical pattern in portions of the limbic system and the hemispheric lateralization of such effects were studied in cats with permanently implanted electrodes. Electronic frequency and area integrators were used to analyze the results, and the percentage change in electrographic alterations was calculated. All compounds studied produced trains of spike and wave complexes in the cingulum, rapid discharges in the amygdala complex, and slow-wave synchronous activity in the septal nucleus. Those changes predominated in the left hemisphere. At small but hallucinatory concentrations of these drugs, the cortical EEG was not affected. Exploratory movements directed toward nonexistent objects, classified as hallucinatory-like behavior, appeared simultaneous with these changes in the EEG recordings. We concluded that there could exist a relationship between the appearance of spike and wave complexes in the limbic system without epileptic signs (twitching or myoclonus) and the presence of hallucinations, and that there is a left side hemispheric lateralization of the electrographic effects, viewing cerebral dominance phenomena as a functional and fluctuating state.

  6. Catalytic Synthesis and Antifungal Activity of New Polychlorinated Natural Terpenes

    Directory of Open Access Journals (Sweden)

    Hana Ighachane

    2017-01-01

    Full Text Available Various unsaturated natural terpenes were selectively converted to the corresponding polychlorinated products in good yields using iron acetylacetonate in combination with nucleophilic cocatalyst. The synthesized compounds were evaluated for their in vitro antifungal activity. The antifungal bioassays showed that 2c and 2d possessed significant antifungal activity against Fusarium oxysporum f. sp. albedinis (Foa, Fusarium oxysporum f. sp. canariensis (Foc, and Verticillium dahliae (Vd.

  7. Pilot scale test of a produced water-treatment system for initial removal of organic compounds

    Energy Technology Data Exchange (ETDEWEB)

    Sullivan, Enid J [Los Alamos National Laboratory; Kwon, Soondong [UT-AUSTIN; Katz, Lynn [UT-AUSTIN; Kinney, Kerry [UT-AUSTIN

    2008-01-01

    A pilot-scale test to remove polar and non-polar organics from produced water was performed at a disposal facility in Farmington NM. We used surfactant-modified zeolite (SMZ) adsorbent beds and a membrane bioreactor (MBR) in combination to reduce the organic carbon content of produced water prior to reverse osmosis (RO). Reduction of total influent organic carbon (TOC) to 5 mg/L or less is desirable for efficient RO system operation. Most water disposed at the facility is from coal-bed gas production, with oil production waters intermixed. Up to 20 gal/d of produced water was cycled through two SMZ adsorbent units to remove volatile organic compounds (BTEX, acetone) and semivolatile organic compounds (e.g., napthalene). Output water from the SMZ units was sent to the MBR for removal of the organic acid component of TOC. Removal of inorganic (Mn and Fe oxide) particulates by the SMZ system was observed. The SMZ columns removed up to 40% of the influent TOC (600 mg/L). BTEX concentrations were reduced from the initial input of 70 mg/L to 5 mg/L by the SMZ and to an average of 2 mg/L after the MBR. Removal rates of acetate (input 120-170 mg/L) and TOC (input up to 45 mg/L) were up to 100% and 92%, respectively. The water pH rose from 8.5 to 8.8 following organic acid removal in the MBR; this relatively high pH was likely responsible for observed scaling of the MBR internal membrane. Additional laboratory studies showed the scaling can be reduced by metered addition of acid to reduce the pH. Significantly, organic removal in the MBR was accomplished with a very low biomass concentration of 1 g/L throughout the field trial. An earlier engineering evaluation shows produced water treatment by the SMZ/MBR/RO system would cost from $0.13 to $0.20 per bbl at up to 40 gpm. Current estimated disposal costs for produced water are $1.75 to $4.91 per bbl when transportation costs are included, with even higher rates in some regions. Our results suggest that treatment by an SMZ

  8. Production of Bioactive Compounds by Bacillus subtilis against Sclerotium rolfsii

    Directory of Open Access Journals (Sweden)

    Nalisha, I.

    2006-01-01

    Full Text Available This study aims to investigate the characteristic of bioactive compound produced by Bacillus subtilis against Sclerotium rolfsii and the influence of additive supplements on the antagonistic activity of B. subtilis. The fact that B. subtilis produced an antifungal substance which has inhibitory effect on wide range of fungi, including S. rolfsii, is well known. To learn the effect of pH, temperature and light condition on the production of antifungal compound, B. subtilis was inoculated in Potato Dextrose Broth at various initial pH, temperatures and light conditions, respectively. This antagonist was found to produce antifungal compound that stable at 80C with 58.3 % inhibition on S. rolfsii. The activity was constant within a wide range of pH (3–11. However, treatment with pH11 lead to higher antifungal activity (31.57 % inhibition and it was also found to produce substance that can endure dark condition (46.24 % inhibition with fungicidal effect on S. rolfsii. A series of experiments also been carried out to enhance the antifungal production by supplementing different carbon source preparation into bacterial liquid culture. B. subtilis were grown in minimal medium containing 1 % of oil palm root, Ganoderma lucidum or chitin, respectively prior to bioassay. Crude culture from oil palm root supplemented culture shown significantly reduction in S. rolfsii growth compared to other carbon source crude culture or the antagonism alone, suggesting that this approach may provide improved biocontrol efficiency.

  9. An Insecticidal Compound Produced by an Insect-Pathogenic Bacterium Suppresses Host Defenses through Phenoloxidase Inhibition

    Directory of Open Access Journals (Sweden)

    Ihsan Ullah

    2014-12-01

    Full Text Available A bioassay-guided column chromatographic strategy was adopted in the present study to fractionate the culture extract of Photorhabdus temperata M1021 to identify potential insecticidal and antimicrobial compounds. An ethyl acetate (EtOAc culture extract of P. temperata was assayed against Galleria mellonella larvae through intra-hemocoel injection and exhibited 100% insect mortality within 60 h. The EtOAc fraction and an isolated compound exhibited phenoloxidase (PO inhibition of up to 60% and 63%, respectively. The compound was identified as 1,2-benzenedicarboxylic acid (phthalic acid, PA by gas chromatography-mass spectrometry and nuclear magnetic resonance. PA exhibited insecticidal activity against G. mellonella in a dose-dependent manner, and 100% insect mortality was observed at 108 h after injection of 1 M PA. In a PO inhibition assay, 0.5 and 1 M concentrations of PA were found to inhibit PO activity by 74% and 82%, respectively; and in a melanotic nodule formation assay, nodule formation was significantly inhibited (27 and 10 nodules by PA (0.5 and 1 M, respectively. PA was furthermore found to have substantial antioxidant activity and maximum antioxidant activity was 64.7% for 0.5 M PA as compare to control. Antibacterial activity was assessed by The MIC values ranged from 0.1 M to 0.5 M of PA. This study reports a multifunctional PA, a potential insecticidal agent, could a factor of insect mortality along with other toxins produced by P. temperata M1021.

  10. Trophic transfer of naturally produced brominated aromatic compounds in a Baltic Sea food chain.

    Science.gov (United States)

    Dahlgren, Elin; Lindqvist, Dennis; Dahlgren, Henrik; Asplund, Lillemor; Lehtilä, Kari

    2016-02-01

    Brominated aromatic compounds (BACs) are widely distributed in the marine environment. Some of these compounds are highly toxic, such as certain hydroxylated polybrominated diphenyl ethers (OH-PBDEs). In addition to anthropogenic emissions through use of BACs as e.g. flame retardants, BACs are natural products formed by marine organisms such as algae, sponges, and cyanobacteria. Little is known of the transfer of BACs from natural producers and further up in the trophic food chain. In this study it was observed that total sum of methoxylated polybrominated diphenyl ethers (MeO-PBDEs) and OH-PBDEs increased in concentration from the filamentous red alga Ceramium tenuicorne, via Gammarus sp. and three-spined stickleback (Gasterosteus aculeatus) to perch (Perca fluviatilis). The MeO-PBDEs, which were expected to bioaccumulate, increased in concentration accordingly up to perch, where the levels suddenly dropped dramatically. The opposite pattern was observed for OH-PBDEs, where the concentration exhibited a general trend of decline up the food web, but increased in perch, indicating metabolic demethylation of MeO-PBDEs. Debromination was also indicated to occur when progressing through the food chain resulting in high levels of tetra-brominated MeO-PBDE and OH-PBDE congeners in fish, while some penta- and hexa-brominated congeners were observed to be the dominant products in the alga. As it has been shown that OH-PBDEs are potent disruptors of oxidative phosphorylation and that mixtures of different congener may act synergistically in terms of this toxic mode of action, the high levels of OH-PBDEs detected in perch in this study warrants further investigation into potential effects of these compounds on Baltic wildlife, and monitoring of their levels. Copyright © 2015 Elsevier Ltd. All rights reserved.

  11. Suitability of a cytotoxicity assay for detection of potentially harmful compounds produced by freshwater bloom-forming algae.

    Science.gov (United States)

    Sorichetti, Ryan J; McLaughlin, Jace T; Creed, Irena F; Trick, Charles G

    2014-01-01

    Detecting harmful bioactive compounds produced by bloom-forming pelagic algae is important to assess potential risks to public health. We investigated the application of a cell-based bioassay: the rainbow trout gill-w1 cytotoxicity assay (RCA) that detects changes in cell metabolism. The RCA was used to evaluate the cytotoxic effects of (1) six natural freshwater lake samples from cyanobacteria-rich lakes in central Ontario, Canada; (2) analytical standards of toxins and noxious compounds likely to be produced by the algal communities in these lakes; and (3) complex mixtures of compounds produced by cyanobacterial and chrysophyte cultures. RCA provided a measure of lake water toxicity that could not be reproduced using toxin or noxious compound standards. RCA was not sensitive to toxins and only sensitive to noxious compounds at concentrations higher than reported environmental averages (EC 50 ≥10 3 nM). Cultured algae produced bioactive compounds that had recognizable dose dependent and toxic effects as indicated by RCA. Toxicity of these bioactive compounds depended on taxa (cyanobacteria, not chrysophytes), growth stage (stationary phase more toxic than exponential phase), location (intracellular more toxic than extracellular) and iron status (cells in high-iron treatment more toxic than cells in low-iron treatment). The RCA provides a new avenue of exploration and potential for the detection of natural lake algal toxic and noxious compounds. Copyright © 2013 Elsevier B.V. All rights reserved.

  12. Direct observation of defects in A15 compounds produced by fast neutron irradiation

    International Nuclear Information System (INIS)

    Pande, C.S.

    1979-01-01

    The nature of defect or defect complexes produced in superconducting compounds Nb 3 Sn, Nb 3 Pt, and V 3 Si by high energy (E greater than or equal to 1 MeV) neutron irradiation is investigated by transmission electron microscopy. The newly developed technique of superlattice reflection imaging is used whereby the regions of reduced long range order are directly imaged. Unlike metals these regions were found in general not to collapse into dislocation loops. The size and the volume fraction of these disordered regions are obtained for fluences ranging from 10 17 neutrons/cm 2 to 3 x 10 19 neutrons/cm 2 . The size ranges from 20A to 60A. Typical volume fraction for 10 18 neutrons/cm 2 is over 1%

  13. Purification and characterization of two new cell-bound bioactive compounds produced by wild Lactococcus lactis strain.

    Science.gov (United States)

    Saraiva, Margarete Alice Fontes; Brede, Dag Anders; Nes, Ingolf Figved; Baracat-Pereira, Maria Cristina; de Queiroz, Marisa Vieira; de Moraes, Célia Alencar

    2017-07-03

    Novel compounds and innovative methods are required considering that antibiotic resistance has reached a crisis point. In the study, two cell-bound antimicrobial compounds produced by Lactococcus lactis ID1.5 were isolated and partially characterized. Following purification by cationic exchange and a solid-phase C18 column, antimicrobial activity was recovered after three runs of RPC using 60% (v/v) and 100% (v/v) of 2-propanol for elution, suggesting that more than one antimicrobial compound were produced by L. lactis ID1.5, which were in this study called compounds AI and AII. The mass spectrum of AI and AII showed major intensity ions at m/z 1070.05 and 955.9 Da, respectively. The compound AI showed a spectrum of antimicrobial activity mainly against L. lactis species, while the organisms most sensitive to compound AII were Bacillus subtilis, Listeria innocua, Streptococcus pneumoniae and Pseudomonas aeruginosa. The antimicrobial activity of both compounds was suppressed by treatment with Tween 80. Nevertheless, both compounds showed high stability to heat and proteases treatments. The isolated compounds, AI and AII, showed distinct properties from other antimicrobial substances already reported as produced by L. lactis, and have a significant inhibitory effect against two clinically important respiratory pathogens. © FEMS 2017. All rights reserved. For permissions, please e-mail: journals.permissions@oup.com.

  14. Antibacterial and antifungal properties of guanylhydrazones

    Directory of Open Access Journals (Sweden)

    Ajdačić Vladimir

    2017-01-01

    Full Text Available A series of novel guanylhydrazones were designed, synthesized and characterized. All the compounds were screened for their antibacterial and antifungal activity. Compounds 26 and 27 showed excellent antibacterial activities against Staphylococcus aureus ATCC 25923 and Micrococcus luteus ATCC 379 with minimal inhibitory concentrations of 4 μg mL-1, and good antifungal activity against Candida parapsilosis ATCC 22019. These results suggested that the selected guanylhydrazones could serve as promising leads for improved antimicrobial development. [Project of the Ministry of Education, Science and Technological Development of the Republic of Serbia, Grant No. 172008 and Grant No. 173048

  15. [Derivatives of 4-nitroso-aminopyrazole as antifungal agents].

    Science.gov (United States)

    Giori, P; Mazzotta, D; Vertuani, G; Guarneri, M; Pancaldi, D; Brunelli, A

    1981-12-01

    The synthesis of 4-nitroso-5-amminopyrazoles and of 4-nitroso-5-pyrazolylurethans and -ureas is described. The chemicals were tested for antifungal activity against Erysiphe graminis, Erysiphe cichoracearum, Puccinia recondita, Septoria apii and Rhizoctonia solani. A number of the described compounds showed some antifungal activity.

  16. Marine Pharmacology in 2009–2011: Marine Compounds with Antibacterial, Antidiabetic, Antifungal, Anti-Inflammatory, Antiprotozoal, Antituberculosis, and Antiviral Activities; Affecting the Immune and Nervous Systems, and other Miscellaneous Mechanisms of Action †

    Science.gov (United States)

    Mayer, Alejandro M. S.; Rodríguez, Abimael D.; Taglialatela-Scafati, Orazio; Fusetani, Nobuhiro

    2013-01-01

    The peer-reviewed marine pharmacology literature from 2009 to 2011 is presented in this review, following the format used in the 1998–2008 reviews of this series. The pharmacology of structurally-characterized compounds isolated from marine animals, algae, fungi and bacteria is discussed in a comprehensive manner. Antibacterial, antifungal, antiprotozoal, antituberculosis, and antiviral pharmacological activities were reported for 102 marine natural products. Additionally, 60 marine compounds were observed to affect the immune and nervous system as well as possess antidiabetic and anti-inflammatory effects. Finally, 68 marine metabolites were shown to interact with a variety of receptors and molecular targets, and thus will probably contribute to multiple pharmacological classes upon further mechanism of action studies. Marine pharmacology during 2009–2011 remained a global enterprise, with researchers from 35 countries, and the United States, contributing to the preclinical pharmacology of 262 marine compounds which are part of the preclinical pharmaceutical pipeline. Continued pharmacological research with marine natural products will contribute to enhance the marine pharmaceutical clinical pipeline, which in 2013 consisted of 17 marine natural products, analogs or derivatives targeting a limited number of disease categories. PMID:23880931

  17. In Vitro Antifungal Activity of Burkholderia gladioli pv. agaricicola against Some Phytopathogenic Fungi

    Directory of Open Access Journals (Sweden)

    Hazem S. Elshafie

    2012-12-01

    Full Text Available The trend to search novel microbial natural biocides has recently been increasing in order to avoid the environmental pollution from use of synthetic pesticides. Among these novel natural biocides are the bioactive secondary metabolites of Burkholderia gladioli pv. agaricicola (Bga. The aim of this study is to determine antifungal activity of Bga strains against some phytopathogenic fungi. The fungicidal tests were carried out using cultures and cell-free culture filtrates against Botrytis cinerea, Aspergillus flavus, Aspergillus niger, Penicillium digitatum, Penicillium expansum, Sclerotinia sclerotiorum and Phytophthora cactorum. Results demonstrated that all tested strains exert antifungal activity against all studied fungi by producing diffusible metabolites which are correlated with their ability to produce extracellular hydrolytic enzymes. All strains significantly reduced the growth of studied fungi and the bacterial cells were more bioactive than bacterial filtrates. All tested Bulkholderia strains produced volatile organic compounds (VOCs, which inhibited the fungal growth and reduced the growth rate of Fusarium oxysporum and Rhizoctonia solani. GC/MS analysis of VOCs emitted by strain Bga 11096 indicated the presence of a compound that was identified as 1-methyl-4-(1-methylethenyl-cyclohexene, a liquid hydrocarbon classified as cyclic terpene. This compound could be responsible for the antifungal activity, which is also in agreement with the work of other authors.

  18. Molecular characterization of antimicrobial compound produced by Lactobacillus acidophilus AA11.

    Science.gov (United States)

    Abo-Amer, Aly E

    2007-06-01

    Approximately 63 strains of Lactobacillus acidophilus were isolated from Egyptian home-made cheese and examined for production of antagonism. Only eight strains demonstrated inhibitory activity against spoilage microorganisms (i.e. Staphylococcus aureus and Bacillus cereus) and pathogens (i.e. E. coli, Salmonella sp. and Shigella sp.). Lactobacillus acidophilus AA11 produced higher antimicrobial activity with a wide range of inhibition. The agent AA11 was sensitive to proteolytic enzymes and retained full activity after 30 min at 100 degrees C. Activity against sensitive cells was bactericidal but not bacteriolytic. The compound was produced during growth phase and could be extracted from the culture supernatant fluids with n-butanol. 12% SDS-PAGE analysis of 40% ammonium sulphate precipitated agent showed two peptides with molecular weights of approximately 36 kDa and approximately 29 kDa. No plasmid was identified in Lactobacillus acidophilus AA11 indicating that the genes encoding the inhibitory agent were located on the chromosome. These characteristics identify the inhibitory substance as a bacteriocin, designated acidocin AA11 and confer the agent an application potential as a biopreservative.

  19. Bioactive Compound Rich Indian Spices Suppresses the Growth of β-lactamase Produced Multidrug Resistant Bacteria

    Directory of Open Access Journals (Sweden)

    Eadlapalli Siddhartha

    2017-01-01

    Full Text Available Background: Multidrug Resistance (MDR among bacteria become a global concern due to failure of antibiotics, is drawn attention for best antimicrobials from the spices which have been using ancient days in Indian culinary and traditional medicine. Aim and Objectives: The present study was undertaken to evaluate the bioactive compounds and their antibacterial activity in routinely used culinary Indian spices against β-lactamase produced MDR bacteria. Material and Methods: Ethanolic extracts prepared from twenty spices and were evaluated for total phenolics, flavonoids, alkaloids, terpenoids, antioxidant properties, and also assayed their antibacterial activities against β-lactamase producing MDR bacteria (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa and Staphylococcus aureus. β-Lactamase and cell viability assays were performed in MDR bacteria. Results: Among twenty spices, cinnamon and clove exhibited highest levels of phenolics and terpenoids with elevated antioxidant potential and also showing greater reducing potential at lower concentrations of extract (2.3 and 4.06 µg GAE/gm, respectively. Further, the spices extracts were assessed for antimicrobial activity against β-lactamase produced tested MDR bacteria and observed higher antimicrobial activity with cinnamon, garlic, tamarind and clove at lowest concentrations of MIC and MBC at 16 - 32 µg GAE/ml, as compared to standard drug, amoxiclav (16/8 µg/ml. Spices significantly inhibited the β-lactamase activity (80–94% and also cell viability in tested MDR bacteria. Conclusion: Indian spices consist of rich bioactive profile and antioxidant activity inhibited the bacterial growth effectively by suppressing β-lactamase production in MDR bacteria. Results indicating the spices as functional foods and could be used in prevention of antibiotic resistance.

  20. A marine sponge associated strain of Bacillus subtilis and other marine bacteria can produce anticholinesterase compounds.

    Science.gov (United States)

    Pandey, Sony; Sree, Ayinampudi; Sethi, Dipti Priya; Kumar, Chityal Ganesh; Kakollu, Sudha; Chowdhury, Lipsa; Dash, Soumya Suchismita

    2014-02-15

    Acetylcholinesterase (AChE) inhibitors or anticholinesterases reduce the activity of enzyme acetylcholinesterase that degrades the neurotransmitter acetylcholine in the brain. The inhibitors have a significant pharmacological role in neurodegenerative diseases like Alzheimer's and Parkinson's etc. Although plants have been a significant source of these compounds, there are very few sporadic reports of microorganisms producing such inhibitors. Anticholinesterase activity in bacterial associates of marine soft corals and sponges were not previously reported. We screened 887 marine bacteria for the presence of acetylcholinesterase inhibitors, in a microplate based assay, and found that 140 (15.8%) of them inhibit the electric eel enzyme, acetylcholinesterase. Majority of the active isolates were bacterial associates of soft corals followed by sediment isolates while most of the potent inhibitors belonged to the bacterial associates of marine sponges. Maximum inhibition (54%) was exhibited by a bacterial strain M18SP4P (ii), isolated from the marine sponge Fasciospongia cavernosa. Based on phenotypic characterization and 16S rDNA sequencing, the strain was identified as Bacillus subtilis - revealing yet another activity in a strain of the model organism that is considered to be a cell factory. TLC bioautography of the methanol extract of this culture, showed the presence of two major components having this activity, when compared to Galanthamine, the positive control. From the results of our study, we conclude that acetylcholinesterase inhibitors are quite prevalent in marine bacteria, particularly the bacterial associates of marine invertebrates. Several potential AChE inhibitors in marine bacteria are waiting to be discovered to provide easily manipulable natural sources for the mass production of these therapeutic compounds.

  1. A marine sponge associated strain of Bacillus subtilis and other marine bacteria can produce anticholinesterase compounds

    Science.gov (United States)

    2014-01-01

    Background Acetylcholinesterase (AChE) inhibitors or anticholinesterases reduce the activity of enzyme acetylcholinesterase that degrades the neurotransmitter acetylcholine in the brain. The inhibitors have a significant pharmacological role in neurodegenerative diseases like Alzheimer’s and Parkinson’s etc. Although plants have been a significant source of these compounds, there are very few sporadic reports of microorganisms producing such inhibitors. Anticholinesterase activity in bacterial associates of marine soft corals and sponges were not previously reported. Results We screened 887 marine bacteria for the presence of acetylcholinesterase inhibitors, in a microplate based assay, and found that 140 (15.8%) of them inhibit the electric eel enzyme, acetylcholinesterase. Majority of the active isolates were bacterial associates of soft corals followed by sediment isolates while most of the potent inhibitors belonged to the bacterial associates of marine sponges. Maximum inhibition (54%) was exhibited by a bacterial strain M18SP4P (ii), isolated from the marine sponge Fasciospongia cavernosa. Based on phenotypic characterization and 16S rDNA sequencing, the strain was identified as Bacillus subtilis - revealing yet another activity in a strain of the model organism that is considered to be a cell factory. TLC bioautography of the methanol extract of this culture, showed the presence of two major components having this activity, when compared to Galanthamine, the positive control. Conclusion From the results of our study, we conclude that acetylcholinesterase inhibitors are quite prevalent in marine bacteria, particularly the bacterial associates of marine invertebrates. Several potential AChE inhibitors in marine bacteria are waiting to be discovered to provide easily manipulable natural sources for the mass production of these therapeutic compounds. PMID:24528673

  2. Characterization of an Antibacterial Compound, 2-Hydroxyl Indole-3-Propanamide, Produced by Lactic Acid Bacteria Isolated from Fermented Batter.

    Science.gov (United States)

    Jeevaratnam, Kadirvelu; Vidhyasagar, Venkatasubramanian; Agaliya, Perumal Jayaprabha; Saraniya, Appukuttan; Umaiyaparvathy, Muthukandan

    2015-09-01

    Lactic acid bacteria are known to produce numerous antimicrobial compounds that are active against various pathogens. Here, we have purified and characterized a novel low-molecular-weight (LMW) antimicrobial compound produced by Lactobacillus and Pediococcus isolated from fermented idly and uttapam batter. The LMW compound was extracted from cell-free supernatant using ice-cold acetone, purified by gel permeation and hydrophobic interaction chromatography. It exhibited antimicrobial activity against Gram-positive and Gram-negative pathogenic bacteria sparing the probiotic strains like Lactobacillus rhamnosus. The molecular weight of the LMW compound was identified as 204 Da using LC-MS-ESI. In addition, the structure of the compound was predicted using spectroscopic methods like FTIR and NMR and identified as 2-hydroxyl indole-3-propanamide. The LMW compound was differentiated from its related compound, tryptophan, by Salkowski reaction and thin-layer chromatography. This novel LMW compound, 2-hydroxyl indole-3-propanamide, may have an effective application as an antibiotic which can spare prevailing probiotic organisms but target only the pathogenic strains.

  3. Actinomycetes of Orthosipon stamineus rhizosphere as producer of antibacterial compound against multidrug resistant bacteria

    Science.gov (United States)

    Rante, H.; Yulianty, R.; Usmar; Djide, N.; Subehan; Burhamzah, R.; Prasad, M. B.

    2017-11-01

    The increasing case of antibiotic resistence has become an important problem to be faced in treating the infection diseases. The diversities of microbia, especially actinomycetes bacteria which originated from rizosphere soil of medicinal plant, has opened a chance for discovering the metabolites which can be used in solving the antibiotic resistant pathogenic bacteria problems. The aim of this research was to isolate the actinobacteria originated from medicinal plant rizosphere of Orthosipon stamineus as the producer of anti-multidrug resistances bacteria compounds. Three isolates of actinomycetes has been isolated from Orthosipon stamineus rhizosphere named KC3-1, KC3-2 and KC3-3. One isolate (KC3-3) showed big activity in inhibiting the test microbes by antagonistic test of actinomycetes isolates against Staphylococcus aureus and Eschericia coli antibiotic resistant bacteria. Furthermore, the KC3-3 isolate was fermented in Starch Nitrate Broth (SNB) medium for 14 days. The supernatant and the biomass of the fermentation yield were separated. The supernatant were extracted using ethyl acetate as the solvent and the biomass were extracted using methanol. The antibacterial activity test of ethyl acetate and methanol extract revealed that the extracts can inhibit the bacteria test up to 5% concentration. The ethyl acetate and methanol extracts can inhibit the bacteria test up to 5% concentration.

  4. Producing surfactant-synthesized nanomaterials in situ on a building substrate, without volatile organic compounds.

    Science.gov (United States)

    Illescas, Juan F; Mosquera, Maria J

    2012-08-01

    This article describes a sol-gel route for nanomaterials production, without volatile organic compounds (VOCs). These materials are simply obtained by mixing a silica oligomer with a non-ionic surfactant under ultrasonic agitation. The surfactant acts as sol-gel transition catalyst and also as an agent that directs the pore structure of the material, reducing capillary pressure during drying. Thus, a crack-free monolithic material is produced. We also synthesize a novel product with hydrophobic properties by adding OH terminal-polydimethylsiloxane to the starting sol. Importantly, since our synthesis does not require calcination or other additional procedures, the sol can be applied directly onto substrates, particularly the external surface of buildings. Thus, an application of these nanomaterials is to restore and to protect building substrates. Our in-depth investigation of the structure of these materials, using several techniques (physisorption, scanning electron microscopy, transmission electron microscopy, atomic force microscopy, nuclear resonance magnetic spectroscopy), reveals that they are composed of silica particles as a result of the role played by n-octylamine. In the hybrid materials, polydimethylsiloxane acts to form bridges linking the silica particles. Finally, we demonstrate the effectiveness of these products for consolidating one particular building stone and making it hydrophobic.

  5. Current state and perspectives of producing biodiesel‐like compounds by biotechnology

    Science.gov (United States)

    Uthoff, Stefan; Bröker, Daniel; Steinbüchel, Alexander

    2009-01-01

    Summary The global demand for crude oil is expected to continue to rise in future while simultaneously oil production is currently reaching its peak. Subsequently, rising oil prices and their negative impacts on economy, together with an increased environmental awareness of our society, directed the focus also on the biotechnological production of fuels. Although a wide variety of such fuels has been suggested, only the production of ethanol and biodiesel has reached a certain economic feasibility and volume, yet. This review focuses on the current state and perspectives of biotechnological production of biodiesel‐like compounds. At present by far most of the produced biodiesel is obtained by chemical transesterification reactions, which cannot meet the demands of a totally ‘green’ fuel production. Therefore, also several biotechnological biodiesel production processes are currently being developed. Biotechnological production can be achieved by purified enzymes in the soluble state, which requires cost‐intensive protein preparation. Alternatively, enzymes could be immobilized on an appropriate matrix, enabling a reuse of the enzyme, although the formation of by‐products may provide difficulties to maintain the enzyme activity. Processes in presence of organic solvents like t‐butanol have been developed, which enhance by‐product solubility and therefore prevent loss of enzyme activity. As another approach the application of whole‐cell catalysis for the production of fatty acid ethyl esters, which is also referred to as ‘microdiesel’, by recombinant microorganisms has recently been suggested. PMID:21255288

  6. Current state and perspectives of producing biodiesel-like compounds by biotechnology.

    Science.gov (United States)

    Uthoff, Stefan; Bröker, Daniel; Steinbüchel, Alexander

    2009-09-01

    The global demand for crude oil is expected to continue to rise in future while simultaneously oil production is currently reaching its peak. Subsequently, rising oil prices and their negative impacts on economy, together with an increased environmental awareness of our society, directed the focus also on the biotechnological production of fuels. Although a wide variety of such fuels has been suggested, only the production of ethanol and biodiesel has reached a certain economic feasibility and volume, yet. This review focuses on the current state and perspectives of biotechnological production of biodiesel-like compounds. At present by far most of the produced biodiesel is obtained by chemical transesterification reactions, which cannot meet the demands of a totally 'green' fuel production. Therefore, also several biotechnological biodiesel production processes are currently being developed. Biotechnological production can be achieved by purified enzymes in the soluble state, which requires cost-intensive protein preparation. Alternatively, enzymes could be immobilized on an appropriate matrix, enabling a reuse of the enzyme, although the formation of by-products may provide difficulties to maintain the enzyme activity. Processes in presence of organic solvents like t-butanol have been developed, which enhance by-product solubility and therefore prevent loss of enzyme activity. As another approach the application of whole-cell catalysis for the production of fatty acid ethyl esters, which is also referred to as 'microdiesel', by recombinant microorganisms has recently been suggested. © 2009 The Authors. Journal compilation © 2009 Society for Applied Microbiology and Blackwell Publishing Ltd.

  7. Diversity of Micromonospora strains from the deep Mediterranean Sea and their potential to produce bioactive compounds

    Directory of Open Access Journals (Sweden)

    Andrea Gärtner

    2016-06-01

    Full Text Available During studies on bacteria from the Eastern Mediterranean deep-sea, incubation under in situ conditions (salinity, temperature and pressure and heat treatment were used to selectively enrich representatives of Micromonospora. From sediments of the Ierapetra Basin (4400 m depth and the Herodotos Plain (2800 m depth, 21 isolates were identified as members of the genus Micromonospora. According to phylogenetic analysis of 16S rRNA gene sequences, the Micromonospora isolates could be assigned to 14 different phylotypes with an exclusion limit of ≥ 99.5% sequence similarity. They formed 7 phylogenetic clusters. Two of these clusters, which contain isolates obtained after enrichment under pressure incubation and phylogenetically are distinct from representative reference organism, could represent bacteria specifically adapted to the conditions in situ and to life in these deep-sea sediments. The majority of the Micromonospora isolates (90% contained at least one gene cluster for biosynthesis of secondary metabolites for non-ribosomal polypeptides and polyketides (polyketide synthases type I and type II. The determination of biological activities of culture extracts revealed that almost half of the strains produced substances inhibitory to the growth of Gram-positive bacteria. Chemical analyses of culture extracts demonstrated the presence of different metabolite profiles also in closely related strains. Therefore, deep-sea Micromonospora isolates are considered to have a large potential for the production of new antibiotic compounds.

  8. Marine pharmacology in 2001--2002: marine compounds with anthelmintic, antibacterial, anticoagulant, antidiabetic, antifungal, anti-inflammatory, antimalarial, antiplatelet, antiprotozoal, antituberculosis, and antiviral activities; affecting the cardiovascular, immune and nervous systems and other miscellaneous mechanisms of action.

    Science.gov (United States)

    Mayer, Alejandro M S; Hamann, Mark T

    2005-01-01

    During 2001--2002, research on the pharmacology of marine chemicals continued to be global in nature involving investigators from Argentina, Australia, Brazil, Canada, China, Denmark, France, Germany, India, Indonesia, Israel, Italy, Japan, Mexico, Netherlands, New Zealand, Pakistan, the Philippines, Russia, Singapore, Slovenia, South Africa, South Korea, Spain, Sweden, Switzerland, Thailand, United Kingdom, and the United States. This current article, a sequel to the authors' 1998, 1999 and 2000 marine pharmacology reviews, classifies 106 marine chemicals derived from a diverse group of marine animals, algae, fungi and bacteria, on the basis of peer-reviewed preclinical pharmacology. Anthelmintic, antibacterial, anticoagulant, antifungal, antimalarial, antiplatelet, antiprotozoal, antituberculosis or antiviral activities were reported for 56 marine chemicals. An additional 19 marine compounds were shown to have significant effects on the cardiovascular, immune and nervous system as well as to possess anti-inflammatory and antidiabetic effects. Finally, 31 marine compounds were reported to act on a variety of molecular targets and thus may potentially contribute to several pharmacological classes. Thus, during 2001--2002 pharmacological research with marine chemicals continued to contribute potentially novel chemical leads for the ongoing global search for therapeutic agents for the treatment of multiple disease categories.

  9. Volatile compounds profile and sensory evaluation of Beninese condiments produced by inocula of Bacillus subtilis

    DEFF Research Database (Denmark)

    Azokpota, Paulin; Hounhouigan, Joseph D.; Annan, Nana T.

    2010-01-01

    identified in relatively high concentrations and were subdivided into seven main groups with the predominance of four major groups: pyrazines, aldehydes, ketones and alcohols. Compared to the spontaneously fermented condiments, volatile compounds identified in controlled fermented condiments have been found......BACKGROUND: Three Beninese food condiments (ABS124h, IBS248h and SBS348h) were produced by controlled fermentation of African locust beans using inocula of pure cultures of Bacillus subtilis, BS1, BS2 and BS3, respectively. Quantitative and qualitative assessments of the volatile compounds...... in the condiments produced have been performed using the Likens-Nickerson simultaneous distillation-extraction method and GC-MS analysis, followed by a sensory evaluation in comparison with the spontaneously fermented condiments. RESULTS: A total of 94 volatile compounds have been found including 53 compounds...

  10. Antimicrobial Action of Compounds from Marine Seaweed

    Directory of Open Access Journals (Sweden)

    María José Pérez

    2016-03-01

    Full Text Available Seaweed produces metabolites aiding in the protection against different environmental stresses. These compounds show antiviral, antiprotozoal, antifungal, and antibacterial properties. Macroalgae can be cultured in high volumes and would represent an attractive source of potential compounds useful for unconventional drugs able to control new diseases or multiresistant strains of pathogenic microorganisms. The substances isolated from green, brown and red algae showing potent antimicrobial activity belong to polysaccharides, fatty acids, phlorotannins, pigments, lectins, alkaloids, terpenoids and halogenated compounds. This review presents the major compounds found in macroalga showing antimicrobial activities and their most promising applications.

  11. Antimicrobial Action of Compounds from Marine Seaweed.

    Science.gov (United States)

    Pérez, María José; Falqué, Elena; Domínguez, Herminia

    2016-03-09

    Seaweed produces metabolites aiding in the protection against different environmental stresses. These compounds show antiviral, antiprotozoal, antifungal, and antibacterial properties. Macroalgae can be cultured in high volumes and would represent an attractive source of potential compounds useful for unconventional drugs able to control new diseases or multiresistant strains of pathogenic microorganisms. The substances isolated from green, brown and red algae showing potent antimicrobial activity belong to polysaccharides, fatty acids, phlorotannins, pigments, lectins, alkaloids, terpenoids and halogenated compounds. This review presents the major compounds found in macroalga showing antimicrobial activities and their most promising applications.

  12. Antimicrobial Action of Compounds from Marine Seaweed

    Science.gov (United States)

    Pérez, María José; Falqué, Elena; Domínguez, Herminia

    2016-01-01

    Seaweed produces metabolites aiding in the protection against different environmental stresses. These compounds show antiviral, antiprotozoal, antifungal, and antibacterial properties. Macroalgae can be cultured in high volumes and would represent an attractive source of potential compounds useful for unconventional drugs able to control new diseases or multiresistant strains of pathogenic microorganisms. The substances isolated from green, brown and red algae showing potent antimicrobial activity belong to polysaccharides, fatty acids, phlorotannins, pigments, lectins, alkaloids, terpenoids and halogenated compounds. This review presents the major compounds found in macroalga showing antimicrobial activities and their most promising applications. PMID:27005637

  13. Reactivity Of Radiolytically-Produced Nitrogen Oxide Radicals Toward Aromatic Compounds

    International Nuclear Information System (INIS)

    Elias, Gracy

    2010-01-01

    radiolysis of the modifier (Cs-7SB), which solvates both metal complexes, is responsible for this change. These reactions presumably occur due to reactions with radiolytically-produced nitrogen-centered radicals like (sm b ullet)NO, (sm b ullet)NO 2 and (sm b ullet)NO 3 . Anisole (C 6 H 5 -OCH 3 ) was used in this study as a surrogate for Cs-7SB, since both are aryl ethers. Toluene was used as a surrogate for Cs-7SB because of the alkyl group on the benzene ring in both molecules. Anisole, highly reactive in acids, is a small molecule compared to Cs-7SB and the nitration products are easier to identify compared to those for the larger Cs-7SB molecule. Toluene is less reactive than anisole. Therefore, the highly reactive anisole and the less reactive toluene were considered in this study as model compounds to compare the reaction mechanisms and the nitrated products in acidic media under irradiation. Experiments were designed to elucidate the mechanism of the nitration of aromatic rings in γ-irradiated aqueous nitric acid. Since a suite of radical and ionic reactive species are produced in this condensed-phase system, solutions of nitric acid, neutral nitrate and neutral nitrite were irradiated in separate experiments to isolate selected reactive species. Product nitration species were assessed by high performance liquid chromatography (HPLC) with a reversed phase C-18 column and photodiode array detector. The nitrated anisole product distributions were the same with and without radiation in acidic solution, although more products were formed with radiation. In the irradiated acidic condensed phase, radiation-enhanced nitrous acid-catalyzed nitrosonium ion electrophilic aromatic substitution followed by oxidation reactions dominated over radical addition reactions. In contrast, the distribution of nitrated derivatives for toluene showed nitronium ion electrophilic substitution in the unirradiated acidic medium as a result of thermal nitration only at elevated temperatures

  14. Design, Synthesis, DFT Study and Antifungal Activity of Pyrazolecarboxamide Derivatives

    Directory of Open Access Journals (Sweden)

    Jin-Xia Mu

    2016-01-01

    Full Text Available A series of novel pyrazole amide derivatives were designed and synthesized by multi-step reactions from phenylhydrazine and ethyl 3-oxobutanoate as starting materials, and their structures were characterized by NMR, MS and elemental analysis. The antifungal activity of the title compounds was determined. The results indicated that some of title compounds exhibited moderate antifungal activity. Furthermore, DFT calculations were used to study the structure-activity relationships (SAR.

  15. Organic Compounds Produced by Photolysis of Realistic Interstellar and Cometary Ice Analogs Containing Methanol

    Science.gov (United States)

    Bernstein, Max P.; Sandford, Scott A.; Allamandola, Louis J.; Chang, Sherwood; Scharberg, Maureen A.

    1995-01-01

    The InfraRed (IR) spectra of UltraViolet (UV) and thermally processed, methanol-containing interstellar / cometary ice analogs at temperatures from 12 to 300 K are presented. Infrared spectroscopy, H-1 and C-13 Nuclear Magnetic Resonance (NMR) spectroscopy, and gas chromatography-mass spectrometry indicate that CO (carbon monoxide), CO2 (carbon dioxide), CH4 (methane), HCO (the formyl radical), H2CO (formaldehyde), CH3CH2OH (ethanol), HC([double bond]O)NH2 (formamide), CH3C([double bond]O)NH2 (acetamide), and R[single bond]C[triple bond]N (nitriles) are formed. In addition, the organic materials remaining after photolyzed ice analogs have been warmed to room temperature contain (in rough order of decreasing abundance), (1) hexamethylenetetramine (HMT, C6H12N4), (2) ethers, alcohols, and compounds related to PolyOxyMethylene (POM, ([single bond]CH2O[single bond](sub n)), and (3) ketones (R[single bond]C([double bond]O)[single bond]R') and amides (H2NC([double bond]O)[single bond]R). Most of the carbon in these residues is thought to come from the methanol in the original ice. Deuterium and C-13 isotopic labeling demonstrates that methanol is definitely the source of carbon in HMT. High concentrations of HMT in interstellar and cometary ices could have important astrophysical consequences. The ultraviolet photolysis of HMT frozen in H2O ice readily produces the 'XCN' band observed in the spectra of protostellar objects and laboratory ices, as well as other nitriles. Thus, HMT may be a precursor of XCN and a source of CN in comets and the interstellar medium. Also, HMT is known to hydrolyze under acidic conditions to yield ammonia, formaldehyde, and amino acids. Thus, HMT may be a significant source of prebiogenic compounds on asteroidal parent bodies. A potential mechanism for the radiative formation of HMT in cosmic ices is outlined.

  16. Design, synthesis, and in vitro evaluation of novel antifungal triazoles.

    Science.gov (United States)

    Xie, Fei; Ni, Tingjunhong; Zhao, Jing; Pang, Lei; Li, Ran; Cai, Zhan; Ding, Zichao; Wang, Ting; Yu, Shichong; Jin, Yongsheng; Zhang, Dazhi; Jiang, Yuanying

    2017-05-15

    Twenty-nine novel triazole analogues of ravuconazole and isavuconazole were designed and synthesized. Most of the compounds exhibited potent in vitro antifungal activities against 8 fungal isolates. Especially, compounds a10, a13, and a14 exhibited superior or comparable antifungal activity to ravuconazole against all the tested fungi. Structure-activity relationship study indicated that replacing 4-cyanophenylthioazole moiety of ravuconazole with fluorophenylisoxazole resulted in novel antifungal triazoles with more effectiveness and a broader-spectrum. Copyright © 2017 Elsevier Ltd. All rights reserved.

  17. Synthesis and Biological Evaluation of Norcantharidin Derivatives Possessing an Aromatic Amine Moiety as Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Yang Wang

    2015-12-01

    Full Text Available Based on the structure of naturally produced cantharidin, different arylamine groups were linked to the norcantharidin scaffold to provide thirty six compounds. Their structures were confirmed by melting point, 1H-NMR, 13C-NMR and HRMS-ESI studies. These synthetic compounds were tested as fungistatic agents against eight phytopathogenic fungi using the mycelium growth rate method. Of these thirty six derivatives, seven displayed stronger antifungal activity than did norcantharidin, seven showed higher activity than did cantharidin and three exhibited more significant activity than that of thiabendazole. In particular, 3-(3′-chloro-phenylcarbamoyl norcantharidate II-8 showed the most significant fungicidal activity against Sclerotinia fructigena and S. sclerotiorum, with IC50 values of 0.88 and 0.97 μg/mL, respectively. The preliminary structure-activity relationship data of these compounds revealed that: (1 the benzene ring is critical for the improvement of the spectrum of antifungal activity (3-phenylcarbamoyl norcantharidate II-1 vs norcantharidin and cantharidin; (2 among the three sites, including the C-2′, C-3′ and C-4′ positions of the phenyl ring, the presence of a halogen atom at the C-3′position of the benzene ring caused the most significant increase in antifungal activity; (3 compounds with strongly electron-drawing or electron-donating groups substitutions were found to have a poor antifungal activity; and (4 compared with fluorine, bromine and iodine, chlorine substituted at the C-3′ position of the benzene ring most greatly promoted fungistatic activity. Thus, compound II-8 has emerged as new lead structure for the development of new fungicides.

  18. Retinoid-like compounds produced by phytoplankton affect embryonic development of Xenopus laevis.

    Science.gov (United States)

    Smutná, M; Priebojová, J; Večerková, J; Hilscherová, K

    2017-04-01

    Teratogenic effects, which were remarkably similar to those induced by retinoic acids, have been seen in wild frogs indicating possible source of retinoids in the environment. Recent studies indicate that some cyanobacterial species can contain teratogenic retinoic acids (RAs) and their analogues. Retinoids are known to regulate important processes such as differentiation, development, and embryogenesis. The study investigated the effects of exudates (extracellular compounds) of two cyanobacteria species with retinoic-like activity and one algae species on embryonic development of amphibians. The retinoid-like activity determined by in vitro reporter gene assay reached 528ng retinoid equivalents (REQ)/L and 1000ng REQ/L in exudates of Cylindrospermopsis raciborskii and Microcystis aeruginosa, respectively, while algal exudates showed no detectable activity. Total mean of retinoid-like copounds into exudate was 35.6ng ATRA/mil.cells for M.aeruginosa and 6.71ng ATRA/mil.cells for C.raciborskii, respectively. Toxicity tests with amphibian embryos up to 96h of development were carried out according to the standard guide for the Frog Embryo Teratogenesis Assay Xenopus. Lowest observed effect concentrations (LOEC) of malformations (2.5-2.6µg/L REQ) were two times lower than LOEC for ATRA (5µg/L). The exudates of both cyanobacteria were indeed provoking diverse teratogenic effects (e.g. tail, gut and eyes deformation) and interference with growth in frogs embryos, while such effects were not observed for the algae. Xenopus embryos were also exposed to all-trans retinoic acid (ATRA) in concentration range (1-40µg/L) equivalent to the REQs detected in cyanobacterial exudates. ATRA (10µg/L) caused similar teratogenic phenotypes at corresponding REQs as cyanobacterial exudates. The study confirms the ability of some species of cyanobacteria to produce retinoids naturally and excrete them directly into the environment at concentrations which might have adverse influence on

  19. Aroma-Active Compounds in Jinhua Ham Produced With Different Fermentation Periods

    Directory of Open Access Journals (Sweden)

    Xiao-Sheng Liu

    2014-11-01

    Full Text Available The aroma-active compounds in Jinhua ham processed and stored for 9, 12, 15 and 18 months were extracted by dynamic headspace sampling (DHS and solvent-assisted flavor evaporation (SAFE and analyzed by gas chromatography-olfactometry-mass spectrometry (GC-O-MS. In GC-O-MS, volatile compounds were identified based on their mass spectrum, linear retention index (LRI, odor properties, or reference compound comparisons. The results showed that a total number of 81 aroma-active compounds were identified by GC-O-MS. Among them, acids (such as acetic acid, butanoic acid and 3-methylbutanoic acid, saturated aldehydes (such as hexanal, heptanal, octanal and 3-methylbutanal, benzene derivatives (such as benzeneacetic acid, ester and lactone (such as γ-nonalactone and γ-decalactone were identified as critical compounds in Jinhua ham aroma. The results also indicated that the type and content of the odorants increased significantly with the duration of the fermentation period.

  20. IIn vitro antifungal evaluation of various plant extracts against early ...

    African Journals Online (AJOL)

    Antifungal activities of 27 plant extracts were tested against Alternaria solani (E. & M.) Jones and Grout using radial growth technique. While all tested plant extracts produced some antifungal activities, the results revealed that Circium arvense, Humulus lupulus, Lauris nobilis and Salvia officinalis showed significant ...

  1. Optimization for the Production of Surfactin with a New Synergistic Antifungal Activity

    Science.gov (United States)

    Liu, Mei; Dai, Huanqin; Song, Fuhang; Yu, Zhenyan; Wang, Shujin; Hu, Jiangchun; Kokare, Chandrakant R.; Zhang, Lixin

    2012-01-01

    Background Two of our long term efforts are to discover compounds with synergistic antifungal activity from metabolites of marine derived microbes and to optimize the production of the interesting compounds produced by microorganisms. In this respect, new applications or mechanisms of already known compounds with a high production yield could be continually identified. Surfactin is a well-known lipopeptide biosurfactant with a broad spectrum of antimicrobial and antiviral activity; however, there is less knowledge on surfactin’s antifungal activity. In this study, we investigated the synergistic antifungal activity of C15-surfactin and the optimization of its production by the response surface method. Methodology/Principal Findings Using a synergistic antifungal screening model, we found that the combination of C15-surfactin and ketoconazole (KTC) showed synergistic antifungal effect on Candida albicans SC5314 when the concentrations of C15-surfactin and KTC were 6.25 µg/mL and 0.004 µg/mL, respectively. These concentrations were lower than their own efficient antifungal concentrations, which are >100 µg/mL and 0.016 µg/mL, respectively. The production of C15-surfactin from Bacillus amyloliquefaciens was optimized by the response surface methodology in shaker flask cultivation. The Plackett-Burman design found sucrose, ammonium nitrate and NaH2PO4.2H2O to have significant effects on C15-surfactin production. The optimum values of the tested variables were 21.17 g/L sucrose, 2.50 g/L ammonium nitrate and 11.56 g/L NaH2PO4·2H2O. A production of 134.2 mg/L, which were in agreement with the prediction, was observed in a verification experiment. In comparison to the production of original level (88.6 mg/L), a 1.52-fold increase had been obtained. Conclusion/Significance This work first found that C15-surfactin was an efficient synergistic antifungal agent, and demonstrated that response surface methodology was an effective method to improve the production of C15

  2. Optimization for the production of surfactin with a new synergistic antifungal activity.

    Directory of Open Access Journals (Sweden)

    Xiangyang Liu

    Full Text Available Two of our long term efforts are to discover compounds with synergistic antifungal activity from metabolites of marine derived microbes and to optimize the production of the interesting compounds produced by microorganisms. In this respect, new applications or mechanisms of already known compounds with a high production yield could be continually identified. Surfactin is a well-known lipopeptide biosurfactant with a broad spectrum of antimicrobial and antiviral activity; however, there is less knowledge on surfactin's antifungal activity. In this study, we investigated the synergistic antifungal activity of C(15-surfactin and the optimization of its production by the response surface method.Using a synergistic antifungal screening model, we found that the combination of C(15-surfactin and ketoconazole (KTC showed synergistic antifungal effect on Candida albicans SC5314 when the concentrations of C(15-surfactin and KTC were 6.25 µg/mL and 0.004 µg/mL, respectively. These concentrations were lower than their own efficient antifungal concentrations, which are >100 µg/mL and 0.016 µg/mL, respectively. The production of C(15-surfactin from Bacillus amyloliquefaciens was optimized by the response surface methodology in shaker flask cultivation. The Plackett-Burman design found sucrose, ammonium nitrate and NaH(2PO(4 x 2H(2O to have significant effects on C(15-surfactin production. The optimum values of the tested variables were 21.17 g/L sucrose, 2.50 g/L ammonium nitrate and 11.56 g/L NaH(2PO(4·2H(2O. A production of 134.2 mg/L, which were in agreement with the prediction, was observed in a verification experiment. In comparison to the production of original level (88.6 mg/L, a 1.52-fold increase had been obtained.This work first found that C(15-surfactin was an efficient synergistic antifungal agent, and demonstrated that response surface methodology was an effective method to improve the production of C(15-surfactin.

  3. Carbon dioxide absorbents containing potassium hydroxide produce much larger concentrations of compound A from sevoflurane in clinical practice.

    Science.gov (United States)

    Yamakage, M; Yamada, S; Chen, X; Iwasaki, S; Tsujiguchi, N; Namiki, A

    2000-07-01

    We investigated the concentrations of degraded sevoflurane Compound A during low-flow anesthesia with four carbon dioxide (CO(2)) absorbents. The concentrations of Compound A, obtained from the inspiratory limb of the circle system, were measured by using a gas chromatograph. In the groups administered 2 L/min fresh gas flow with 1% sevoflurane, when the conventional CO(2) absorbents, Wakolime(TM) (Wako, Tokyo, Japan) and Drägersorb(TM) (Dräger, Lübeck, Germany), were used, the concentrations of Compound A increased steadily from a baseline to 14.3 ppm (mean) and 13.2 ppm, respectively, at 2 h after exposure to sevoflurane. In contrast, when the other novel types of absorbents containing decreased or no potassium hydroxide/sodium hydroxide, Medisorb(TM) (Datex-Ohmeda, Louisville, CO) and Amsorb(TM) (Armstrong, Coleraine, Northern Ireland), were used, Compound A remained at baseline (potassium hydroxide/sodium hydroxide produce much larger concentrations of Compound A from sevoflurane in clinical practice. An absorbent containing neither potassium hydroxide nor sodium hydroxide produces the smallest concentrations of Compound A.

  4. In vitro antifungal activities of 26 plant extracts on mycelial growth of ...

    African Journals Online (AJOL)

    Antifungal activities of 26 plant extracts were tested against Phytophthora infestans using radial growth technique. While all tested plant extracts produced some antifungal activities Xanthium strumarium, Lauris nobilis, Salvia officinalis and Styrax officinalis were the most active plants that showed potent antifungal activity.

  5. Antifungal Activity of Bacillus coagulans TQ33, Isolated from Skimmed Milk Powder, against Botrytis cinerea

    OpenAIRE

    Wang, Hai Kuan; Xiao, Rui Feng; Qi†, Wei

    2013-01-01

    Bacillus coagulans TQ33 is isolated from the skimmed milk powder and has a broad antifungal activity against pathogens such as Botrytis cinerea, Alternaria solani, Phytophthora drechsleri Tucker, Fusarium oxysporum and Glomerella cingulata. The characteristics of active antifungal substances produced by B. coagulans TQ33 and its antifungal effects against the growth of plant pathogenic fungi has been evaluated. The effect of pH, temperature and protease on the antifungal activity of B. coagul...

  6. Anti-Fungal activity of essential oil from Baeckea frutescens L against Pleuratus ostreatus

    Science.gov (United States)

    Jemi, Renhart; Barus, Ade Irma; Nuwa, Sarinah, Luhan, Gimson

    2017-11-01

    Ujung Atap is an herb that have distinctive odor on its leaves. The plant's essential oil contains bioactive compounds but has not been investigated its anti-fungal activity against Pleurotus ostreatus. Essential oil from Ujung Atap leaves is one environmentally friendly natural preservative. This study consisted of distillation Ujung Atap leaves with boiled method, determining the number of acid, essential oil ester, and anti-fungal activity against Pleurotus ostreatus. Analysis of the data to calculate anti-fungal activity used probit analysis method to determine the IC50. Results for the distillation of leaves Ujung Atap produce essential oil yield of 0.071% and the average yield of the acid number and the ester of essential oils Ujung Atap leaves are 5.24 and 12.15. Anti-fungal activity Pleurotus ostreatus at a concentration of 1000 µg/mL, 100 µg/mL, 75 µg/mL, 50 µg/mL and 100 µg/mL BA defunct or fungi was declared dead, while at a concentration of 25 µg/mL, 10 µg/mL and 5 µg/mL still occur inhibitory processes. Results obtained probit analysis method IC50 of 35.48 mg/mL; means the essential oil of Ujung Atap leaf can inhibit fungal growth by 50 percent to 35.48 µg/mL concentration.

  7. Antifungal isopimaranes from Hypoestes serpens.

    Science.gov (United States)

    Rasoamiaranjanahary, L; Guilet, D; Marston, A; Randimbivololona, F; Hostettmann, K

    2003-09-01

    Five isopimarane diterpenes (7beta-hydroxyisopimara-8,15-dien-14-one, 14alpha-hydroxyisopimara-7,15-dien-1-one, 1beta,14alpha-dihydroxyisopimara-7,15-diene, 7beta-hydroxyisopimara-8(14),15-dien-1-one and 7beta-acetoxyisopimara-8(14),15-dien-1-one) have been isolated from the leaves of Hypoestes serpens (Acanthaceae). All compounds exhibited antifungal activity against both the plant pathogenic fungus Cladosporium cucumerinum and the yeast Candida albicans; two of them also displayed an acetylcholinesterase inhibition. The structures of the compounds were determined by means of spectrometric methods, including 1D and 2D NMR experiments and MS analysis.

  8. Antifungal metabolites of lactobacilli

    Science.gov (United States)

    Vina A. Yang; Carol A. Clausen

    2004-01-01

    In recent years, public concern about indoor mold growth has increased dramatically in the United States. In this study, lactic acid bacteria, which are known to produce antimicrobial compounds important in the biopreservation of food, were evaluated to determine if the same antimicrobial properties can be used to protect wood from mold establishment. Based on biomass...

  9. Comparison of EUCAST and CLSI Reference Microdilution MICs of Eight Antifungal Compounds for Candida auris and Associated Tentative Epidemiological Cutoff Values

    DEFF Research Database (Denmark)

    Arendrup, M. C.; Prakash, Anupam; Meletiadis, Joseph

    2017-01-01

    , with several peaks for all compounds except amphotericin B, suggesting possible acquired resistance. Modal MIC, geometric MIC, MIC50, and MIC90values were ≤1 2-fold dilutions apart, and no significant differences were found. The quantitative agreement was best for amphotericin B (80%/97% within ±1/±2 dilutions......, the estimated ECOFFs were dependent on the method applied for voriconazole (1 to 32) and isavuconazole (0.125 to 4). CLSI and EUCAST MICs were remarkably similar and confirmed uniform fluconazole resistance and variable acquired resistance to the other agents....

  10. TLR2, TLR4 and Dectin-1 signalling in hematopoietic stem and progenitor cells determines the antifungal phenotype of the macrophages they produce.

    Science.gov (United States)

    Megías, Javier; Martínez, Alba; Yáñez, Alberto; Goodridge, Helen S; Gozalbo, Daniel; Gil, M Luisa

    2016-05-01

    TLRs represent an attractive target for the stimulation of myeloid cell production by HSPCs. We have previously demonstrated that HSPCs use TLR2 to sense Candida albicans in vivo and induce the production of macrophages. In this work, we used an in vitro model of HSPCs differentiation to investigate the functional consequences for macrophages of exposure of HSPCs to various PAMPs and C. albicans cells. Mouse HSPCs (Lin(-) cells) were cultured with M-CSF to induce macrophage differentiation, in the presence or absence of the following PRR agonists: Pam3CSK4 (TLR2 ligand), LPS (TLR4 ligand), depleted zymosan (which only activates Dectin-1), or C. albicans yeasts (which activate several PRRs, but principally TLR2 and Dectin-1). Our data show that these PAMPs differentially impact the anti-microbial function of the macrophages produced by the exposed HSPCs. Pure TLR2 and TLR4 ligands generate macrophages with a diminished ability to produce inflammatory cytokines. In contrast, HSPCs activation in response to C. albicans leads to the generation of macrophages that are better prepared to deal with the infection, as they produce higher amounts of inflammatory cytokines and have higher fungicidal capacity than control macrophages. Therefore, the tailored manipulation of the differentiation process may help to boost the innate immune response to infection. Copyright © 2016 Institut Pasteur. Published by Elsevier Masson SAS. All rights reserved.

  11. Two generators to produce SI-traceable reference gas mixtures for reactive compounds at atmospheric levels

    Science.gov (United States)

    Pascale, C.; Guillevic, M.; Ackermann, A.; Leuenberger, D.; Niederhauser, B.

    2017-12-01

    To answer the needs of air quality and climate monitoring networks, two new gas generators were developed and manufactured at METAS in order to dynamically generate SI-traceable reference gas mixtures for reactive compounds at atmospheric concentrations. The technical features of the transportable generators allow for the realization of such gas standards for reactive compounds (e.g. NO2, volatile organic compounds) in the nmol · mol-1 range (ReGaS2), and fluorinated gases in the pmol ṡ mol-1 range (ReGaS3). The generation method is based on permeation and dynamic dilution. The transportable generators have multiple individual permeation chambers allowing for the generation of mixtures containing up to five different compounds. This mixture is then diluted using mass flow controllers, thus making the production process adaptable to generate the required amount of substance fraction. All parts of ReGaS2 in contact with the gas mixture are coated to reduce adsorption/desorption processes. Each input parameter required to calculate the generated amount of substance fraction is calibrated with SI-primary standards. The stability and reproducibility of the generated amount of substance fractions were tested with NO2 for ReGaS2 and HFC-125 for ReGaS3. They demonstrate stability over 1-4 d better than 0.4% and 0.8%, respectively, and reproducibility better than 0.7% and 1%, respectively. Finally, the relative expanded uncertainty of the generated amount of substance fraction is smaller than 3% with the major contributions coming from the uncertainty of the permeation rate and/or of the purity of the matrix gas. These relative expanded uncertainties meet then the needs of the data quality objectives fixed by the World Meteorological Organization.

  12. Influence of Technological Processes on Biologically Active Compounds of Produced Grapes Juices

    Czech Academy of Sciences Publication Activity Database

    Tříska, Jan; Balík, J.; Strohalm, J.; Novotná, P.; Vrchotová, Naděžda; Lefnerová, D.; Landfeld, A.; Híc, P.; Tománková, E.; Veverka, J.; Houška, M.

    2016-01-01

    Roč. 9, č. 3 (2016), s. 421-429 ISSN 1935-5130 R&D Projects: GA MŠk(CZ) LO1415; GA MZe QJ1210258; GA MZe QI91B094 Institutional support: RVO:67179843 Keywords : Grapevine juices * Thermomaceration * Biologically active compounds * Antioxidative capacity * Total polyphenols * Antimutagenic activity Subject RIV: GM - Food Processing Impact factor: 2.576, year: 2016

  13. Water-soluble phenolic compounds produced from extractive ammonia pretreatment exerted binary inhibitory effects on yeast fermentation using synthetic hydrolysate

    Science.gov (United States)

    Xue, Saisi; Jones, A. Daniel; Sousa, Leonardo; Piotrowski, Jeff; Jin, Mingjie; Sarks, Cory; Dale, Bruce E.

    2018-01-01

    Biochemical conversion of lignocellulosic biomass to liquid fuels requires pretreatment and enzymatic hydrolysis of the biomass to produce fermentable sugars. Degradation products produced during thermochemical pretreatment, however, inhibit the microbes with regard to both ethanol yield and cell growth. In this work, we used synthetic hydrolysates (SynH) to study the inhibition of yeast fermentation by water-soluble components (WSC) isolated from lignin streams obtained after extractive ammonia pretreatment (EA). We found that SynH with 20g/L WSC mimics real hydrolysate in cell growth, sugar consumption and ethanol production. However, a long lag phase was observed in the first 48 h of fermentation of SynH, which is not observed during fermentation with the crude extraction mixture. Ethyl acetate extraction was conducted to separate phenolic compounds from other water-soluble components. These phenolic compounds play a key inhibitory role during ethanol fermentation. The most abundant compounds were identified by Liquid Chromatography followed by Mass Spectrometry (LC-MS) and Gas Chromatography followed by Mass Spectrometry (GC-MS), including coumaroyl amide, feruloyl amide and coumaroyl glycerol. Chemical genomics profiling was employed to fingerprint the gene deletion response of yeast to different groups of inhibitors in WSC and AFEX-Pretreated Corn Stover Hydrolysate (ACSH). The sensitive/resistant genes cluster patterns for different fermentation media revealed their similarities and differences with regard to degradation compounds. PMID:29543873

  14. Rhodotorula taiwanensis MD1149 produces hypoacetylated PEFA compounds with increased surface activity compared to Rhodotorula babjevae MD1169

    Science.gov (United States)

    Rubinfeld, Bonnee; Leif, Roald; Mulcahy, Heather; Dugan, Lawrence; Souza, Brian

    2018-01-01

    Biosurfactants have several desirable characteristics in the industrial sector: detergency, antimicrobial effects, skin hydration, and emulsibility. Several yeast glycolipids are currently being utilized in these capacities: sophorolipids, ustilagic acid, and mannosylerythritol lipids (MELs). An emerging class of glycolipids, termed polyol esters of fatty acids (PEFA), have recently been reported for Rhodotorula babjevae, a basidiomycetous yeast species that secretes hyperacetylated congeners of PEFA (typically with 3–6 acetylation modifications). While screening Rhodotorula species for surfactant production, we identified a new environmental isolate identified as Rhodotorula taiwanensis MD1149 that dropped the surface tension of the liquid medium, indicating that it produced a potent biosurfactant. Acid depolymerization of the purified biosurfactants, followed by gas chromatography-mass spectrometry (GC-MS) analysis revealed that the biosurfactants were composed of PEFA compounds composed mainly of mannitol and arabitol esters of 3-hydroxy fatty acid, 3-methoxy fatty acid, and fatty acids with a single double bond; chain lengths were mainly C16 and C18. Liquid chromatography-mass spectrometry (LC-MS) confirmed the predicted accurate mass of these compounds. Interestingly, PEFA compounds produced by Rhodotorula taiwanensis MD1149 were more surface active due to their hypoacetylation profile (0–4 acetylation modifications) compared to Rhodotorula babjevae MD1169. These disparate surface active properties, based on acetylation, change the hydrophilic-lipophilic balance (HLB) of these compounds, and their potential utility within industrial applications. PMID:29293588

  15. Rhodotorula taiwanensis MD1149 produces hypoacetylated PEFA compounds with increased surface activity compared to Rhodotorula babjevae MD1169.

    Science.gov (United States)

    Lyman, Mathew; Rubinfeld, Bonnee; Leif, Roald; Mulcahy, Heather; Dugan, Lawrence; Souza, Brian

    2018-01-01

    Biosurfactants have several desirable characteristics in the industrial sector: detergency, antimicrobial effects, skin hydration, and emulsibility. Several yeast glycolipids are currently being utilized in these capacities: sophorolipids, ustilagic acid, and mannosylerythritol lipids (MELs). An emerging class of glycolipids, termed polyol esters of fatty acids (PEFA), have recently been reported for Rhodotorula babjevae, a basidiomycetous yeast species that secretes hyperacetylated congeners of PEFA (typically with 3-6 acetylation modifications). While screening Rhodotorula species for surfactant production, we identified a new environmental isolate identified as Rhodotorula taiwanensis MD1149 that dropped the surface tension of the liquid medium, indicating that it produced a potent biosurfactant. Acid depolymerization of the purified biosurfactants, followed by gas chromatography-mass spectrometry (GC-MS) analysis revealed that the biosurfactants were composed of PEFA compounds composed mainly of mannitol and arabitol esters of 3-hydroxy fatty acid, 3-methoxy fatty acid, and fatty acids with a single double bond; chain lengths were mainly C16 and C18. Liquid chromatography-mass spectrometry (LC-MS) confirmed the predicted accurate mass of these compounds. Interestingly, PEFA compounds produced by Rhodotorula taiwanensis MD1149 were more surface active due to their hypoacetylation profile (0-4 acetylation modifications) compared to Rhodotorula babjevae MD1169. These disparate surface active properties, based on acetylation, change the hydrophilic-lipophilic balance (HLB) of these compounds, and their potential utility within industrial applications.

  16. [Amides of amino acids and peptides as antifungal agents].

    Science.gov (United States)

    Giori, P; Vertuani, G; Mazzotta, D; Guarneri, M; Pancaldi, D; Brunelli, A

    1982-07-01

    The synthesis of pyrazolyl-amides of aminoacids and peptides is described. The chemicals were tested for antifungal activity against wheat powdery mildew (Erysiphe graminis DC.), cucumber powdery mildew (Erysiphe cichoracearum DC.), wheat brown rust (Puccinia recondita Rob. ex Desm. f. sp. tritici Erikss et Henn.), celery leaf spot (Septoria Apii Briosi ed Cav. Chest.) and collar rot (Rhizoctonia solani Kuhn). Some of these compounds showed antifungal activity.

  17. Zygosaccharomyces bailii Is a Potential Producer of Various Flavor Compounds in Chinese Maotai-Flavor Liquor Fermentation

    OpenAIRE

    Yan Xu; Yan Zhi; Qun Wu; Rubing Du; Yan Xu

    2017-01-01

    Zygosaccharomyces bailii is a common yeast in various food fermentations. Understanding the metabolic properties and genetic mechanisms of Z. bailii is important for its industrial applications. Fermentation characteristics of Z. bailii MT15 from Chinese Maotai-flavor liquor fermentation were studied. Z. bailii MT15 produced various flavor compounds, including 19 alcohols, six acids, three esters, three ketones, and two aldehydes. Moreover, production of acids and aldehydes were increased by ...

  18. Host cells and methods for producing 1-deoxyxylulose 5-phosphate (DXP) and/or a DXP derived compound

    Energy Technology Data Exchange (ETDEWEB)

    Kirby, James; Fortman, Jeffrey L.; Nishimoto, Minobu; Keasling, Jay D.

    2017-05-02

    The present invention provides for a genetically modified host cell capable of producing 1-deoxyxylulose 5-phosphate or 1-deoxy-D-xylulose 5-phosphate (DXP) (12), and optionally one or more DXP derived compounds, comprising: (a) a mutant RibB, or functional variant thereof, capable of catalyzing xylulose 5-phoshpate and/or ribulose 5-phospate to DXP, or (b) a YajO, or functional variant thereof, and a XylB, or functional variant thereof.

  19. Antifungal Activity of Homoaconitate and Homoisocitrate Analogs

    Directory of Open Access Journals (Sweden)

    Sławomir Milewski

    2012-11-01

    Full Text Available Thirteen structural analogs of two initial intermediates of the L-a-aminoadipate pathway of L-lysine biosynthesis in fungi have been designed and synthesized, including fluoro- and epoxy-derivatives of homoaconitate and homoisocitrate. Some of the obtained compounds exhibited at milimolar range moderate enzyme inhibitory properties against homoaconitase and/or homoisocitrate dehydrogenase of Candida albicans. The structural basis for homoisocitrate dehydrogenase inhibition was revealed by molecular modeling of the enzyme-inhibitor complex. On the other hand, the trimethyl ester forms of some of the novel compounds exhibited antifungal effects. The highest antifungal activity was found for trimethyl trans-homoaconitate, which inhibited growth of some human pathogenic yeasts with minimal inhibitory concentration (MIC values of 16–32 mg/mL.

  20. Metabolite and Mechanistic Basis of Antifungal Property Exhibited by Endophytic Bacillus amyloliquefaciens BmB 1.

    Science.gov (United States)

    Jasim, B; Benny, Rosemin; Sabu, Rohini; Mathew, Jyothis; Radhakrishnan, E K

    2016-07-01

    Plants are ubiquitously colonized by endophytic microorganisms which contribute significantly to plant health through production of plant growth regulators or disease suppression. In the present study, an endophytic bacterial isolate designated as BmB 1 with significant antifungal and plant growth promoting properties was isolated from the stem tissue of Bacopa monnieri (L.) Pennell. The isolate was studied in detail for the molecular and chemical basis of its bioactivity which proved it to have the presence of surfactin, iturin, and type I polyketide synthase (PKS) genes. For the analysis of the chemical basis of antifungal property, extract of the isolate was initially checked for its activity on test pathogens and LC-MS/MS based analysis further confirmed the presence of bacillomycin (m/z (M+H(+)) 1031.8) and surfactin (m/z (M+H(+)) 1008.6 and 1022.6) in the extract prepared. The light microscopic and SEM analysis of the treated and untreated mycelia of the pathogens clearly revealed the hypal destruction caused by the compounds produced by the selected isolate. This confirms the ability of the organism to directly inhibit the growth of the tested pathogens. The GC-MS analysis also confirmed the isolate to have the presence of volatile compounds with the expected role to induce induced systemic resistance (ISR) of the plant. Because of the multitargeted antifungal property, the isolate which was identified as Bacillus amyloliquefaciens can have potential biocontrol applications.

  1. Aluminium Foam and Magnesium Compound Casting Produced by High-Pressure Die Casting

    Directory of Open Access Journals (Sweden)

    Iban Vicario

    2016-01-01

    Full Text Available Nowadays, fuel consumption and carbon dioxide emissions are two of the main focal points in vehicle design, promoting the reduction in the weight of vehicles by using lighter materials. The aim of the work is to evaluate the influence of different aluminium foams and injection parameters in order to obtain compound castings with a compromise between the obtained properties and weight by high-pressure die cast (HPDC using aluminium foams as cores into a magnesium cast part. To evaluate the influence of the different aluminium foams and injection parameters on the final casting products quality, the type and density of the aluminium foam, metal temperature, plunger speed, and multiplication pressure have been varied within a range of suitable values. The obtained compound HPDC castings have been studied by performing visual and RX inspections, obtaining sound composite castings with aluminium foam cores. The presence of an external continuous layer on the foam surface and the correct placement of the foam to support injection conditions permit obtaining good quality parts. A HPDC processed magnesium-aluminium foam composite has been developed for a bicycle application obtaining a suitable combination of mechanical properties and, especially, a reduced weight in the demonstration part.

  2. Galacto-oligosaccharide hydrolysis by genetically-engineered alpha-galactosidase-producing Pseudomonas chlororaphis strains

    Science.gov (United States)

    Various Pseudomonas chlororaphis strains have been shown to produce rhamnolipid (a biosurfactant), poly(hydroxyalkanoate) (PHA; a biopolymer), and/or antifungal compounds for plants. An ability to metabolize galacto-oligosaccharides in soy molasses would allow P. chlororaphis to use the byproduct as...

  3. The dar genes of Pseudomonas chlororaphis PCL1606 are crucial for biocontrol activity via production of the antifungal compound 2-hexyl, 5-propyl resorcinol.

    Science.gov (United States)

    Calderón, Claudia E; Pérez-García, Alejandro; de Vicente, Antonio; Cazorla, Francisco M

    2013-05-01

    To determine the genetic basis by which 2-hexyl, 5-propyl resorcinol (HPR) is produced by the biocontrol rhizobacterium Pseudomonas chlororaphis (formerly known as P. fluorescens) PCL1606, the presence and role of dar genes were investigated. To accomplish this aim, the pCGNOV-1 plasmid was isolated from a PCL1606 genomic library and was shown to hybridize to various dar probes by Southern blot. An analysis of the pCGNOV-1 genomic DNA revealed the presence of five open reading frames that were homologous to dar genes and had an organization that resembled the arrangement of previously described P. chlororaphis strains. Phylogenetic studies resulted in the clustering of PCL1606 with the P. chlororaphis subgroup, which supported the renaming of this strain from P. fluorescens to P. chlororaphis PCL1606. The construction of insertional mutants for each homologous dar gene in P. chlororaphis PCL1606 along with their corresponding complemented derivative strains restored HPR production and confirmed the key role of the dar A and darB genes in HPR production and in the antagonistic phenotype. Finally, biocontrol assays were performed on avocado-Rosellinia and tomato-Fusarium test systems using the HPR-defective and -complemented derivative strains generated here and demonstrated the crucial role of the biosynthetic dar genes in the biocontrol phenotype of P. chlororaphis PCL1606. This biocontrol phenotype is dependent on the dar genes via their production of the HPR antibiotic. Some of the dar genes not directly involved in the biosynthesis of HPR, such as darS or darR, might contribute to regulatory features of HPR production.

  4. Structural Basis of Human CYP51 Inhibition by Antifungal Azoles

    Energy Technology Data Exchange (ETDEWEB)

    Strushkevich, Natallia; Usanov, Sergey A.; Park, Hee-Won (Toronto); (IBC-Belarus)

    2010-09-22

    The obligatory step in sterol biosynthesis in eukaryotes is demethylation of sterol precursors at the C14-position, which is catalyzed by CYP51 (sterol 14-alpha demethylase) in three sequential reactions. In mammals, the final product of the pathway is cholesterol, while important intermediates, meiosis-activating sterols, are produced by CYP51. Three crystal structures of human CYP51, ligand-free and complexed with antifungal drugs ketoconazole and econazole, were determined, allowing analysis of the molecular basis for functional conservation within the CYP51 family. Azole binding occurs mostly through hydrophobic interactions with conservative residues of the active site. The substantial conformational changes in the B{prime} helix and F-G loop regions are induced upon ligand binding, consistent with the membrane nature of the protein and its substrate. The access channel is typical for mammalian sterol-metabolizing P450 enzymes, but is different from that observed in Mycobacterium tuberculosis CYP51. Comparison of the azole-bound structures provides insight into the relative binding affinities of human and bacterial P450 enzymes to ketoconazole and fluconazole, which can be useful for the rational design of antifungal compounds and specific modulators of human CYP51.

  5. In vitro antifungal activity of topical and systemic antifungal drugs against Malassezia species.

    Science.gov (United States)

    Carrillo-Muñoz, Alfonso Javier; Rojas, Florencia; Tur-Tur, Cristina; de Los Ángeles Sosa, María; Diez, Gustavo Ortiz; Espada, Carmen Martín; Payá, María Jesús; Giusiano, Gustavo

    2013-09-01

    The strict nutritional requirements of Malassezia species make it difficult to test the antifungal susceptibility. Treatments of the chronic and recurrent infections associated with Malassezia spp. are usually ineffective. The objective of this study was to obtain in vitro susceptibility profile of 76 clinical isolates of Malassezia species against 16 antifungal drugs used for topical or systemic treatment. Isolates were identified by restriction fragment length polymorphism. Minimal inhibitory concentrations (MIC) were obtained by a modified microdilution method based on the Clinical Laboratory Standards Institute reference document M27-A3. The modifications allowed a good growth of all tested species. High in vitro antifungal activity of most tested drugs was observed, especially triazole derivatives, except for fluconazole which presented the highest MICs and widest range of concentrations. Ketoconazole and itraconazole demonstrated a great activity. Higher MICs values were obtained with Malassezia furfur indicating a low susceptibility to most of the antifungal agents tested. Malassezia sympodialis and Malassezia pachydermatis were found to be more-susceptible species than M. furfur, Malassezia globosa, Malassezia slooffiae and Malassezia restricta. Topical substances were also active but provide higher MICs than the compounds for systemic use. The differences observed in the antifungals activity and interspecies variability demonstrated the importance to studying the susceptibility profile of each species to obtain reliable information for defining an effective treatment regimen. © 2013 Blackwell Verlag GmbH.

  6. Broad spectrum anti-microbial compounds producing bacteria from coast of Qingdao bays.

    Science.gov (United States)

    Khan, Muhammad Naseem; Li, Meng; Mirani, Zulfiqar Ali; Wang, Jingxue; Lin, Hong; Buzdar, Muhammad Aslam

    2015-03-01

    Anti-microbial resistance burden and hazard associated with chemical treatment of infections demanded for new anti-microbial natural products. Marine associated microorganisms are the enormous source of bioactive compounds. In this study we have isolated 272 marine bacteria among them 136 (50%) were antagonistic to at least one of the four pathogenic strains Listeria monocytogenes, Vibrio cholerae, E. coli and S. aureus. Only two strains exhibited antibacterial activity against all four test strains, which were identified by 16S rDNA sequencing as Bacillus sp. DK1-SA11 and Vibrio sp. DK6-SH8. Marine isolate DK1-SA11 has potential to resist boiling temperature and pH 2-12. Furthermore cell free extract (CFE) inhibited all test organisms including superbug MRSA and pathogenic yeast Candida albicans. Marine isolate Bacillus sp. DK1-SA11 could be a potential combatant for the battle of drugs and bugs.

  7. Characterization of aerosols from RDD surrogate compounds produced by fast thermal transients

    International Nuclear Information System (INIS)

    Di Lemma, Fidelma Giulia; Colle, Jean-Yves; Ernstberger, Markus; Konings, Rudy J.M.

    2016-01-01

    Experimental tests have been performed to characterize the aerosols representative of radiological dispersion devices (RDDs, a.k.a. “dirty bombs”) by applying to chosen surrogate compound rapid high temperature transients, vaporizing the sample and forming aerosols mainly by rapid cooling of the vapour. The materials, which were tested in their non-radioactive form, had been chosen from the radioactive sources widely used in industries and nuclear medicine applications, Co, CsCl, Ir and SrTiO 3 . Our analyses permitted the characterization of the inhalable fraction of the aerosols released, and the study of the influence of cladding materials on the aerosol release and on its characteristics. (author)

  8. POTENTIAL IN VITRO ANTI-HELICOBACTER ACTIVITY OF BACTERIOCIN AND BACTERIOCIN-LIKE COMPOUNDS PRODUCED BY LACTOBACILLI

    Directory of Open Access Journals (Sweden)

    Mohammed A. Ramadan

    2014-10-01

    Full Text Available The study was designed for screening of the potential activity of lactic acid bacteria against Helicobacter pylori and other enteropathogenic organisms. A total of 40 samples including natural cow milk and fresh infant stools were tested for the presence of lactic acid bacteria. Of these samples, 73 lactic acid bacterial isolates were recovered on MRS agar medium using the streak-plate method. Isolates inducing probiotic effect were tested under microaerophilic conditions against standard cultures of H. pylori, Esherichia coli and Salmonella enteritidis. The data obtained showed that five isolates of lactic acid bacteria were able to produce bacteriocin or bacteriocin-like compounds. Sequencing of 16S rRNA gene revealed that five isolates belonged to Lactobacillus rhamnosus and Lactobacillus plantarum in addition to other lactic acid bacteria. The most effective isolate (LAB1 showed a marked large inhibition zone against H. pylori. The bacteriocin or bacteriocin like compound(s produced by lactobacilli were further analyzed and characterized. We can conclude that probiotics might be useful in the prophylaxis or as co-therapy for treatment of H. pylori infections.

  9. Development of Phenol-Enriched Olive Oil with Phenolic Compounds Extracted from Wastewater Produced by Physical Refining.

    Science.gov (United States)

    Venturi, Francesca; Sanmartin, Chiara; Taglieri, Isabella; Nari, Anita; Andrich, Gianpaolo; Terzuoli, Erika; Donnini, Sandra; Nicolella, Cristiano; Zinnai, Angela

    2017-08-22

    While in the last few years the use of olive cake and mill wastewater as natural sources of phenolic compounds has been widely considered and several studies have focused on the development of new extraction methods and on the production of functional foods enriched with natural antioxidants, no data has been available on the production of a phenol-enriched refined olive oil with its own phenolic compounds extracted from wastewater produced during physical refining. In this study; we aimed to: (i) verify the effectiveness of a multi-step extraction process to recover the high-added-value phenolic compounds contained in wastewater derived from the preliminary washing degumming step of the physical refining of vegetal oils; (ii) evaluate their potential application for the stabilization of olive oil obtained with refined olive oils; and (iii) evaluate their antioxidant activity in an in vitro model of endothelial cells. The results obtained demonstrate the potential of using the refining wastewater as a source of bioactive compounds to improve the nutraceutical value as well as the antioxidant capacity of commercial olive oils. In the conditions adopted, the phenolic content significantly increased in the prototypes of phenol-enriched olive oils when compared with the control oil.

  10. Determination of unique microbial volatile organic compounds produced by five Aspergillus species commonly found in problem buildings.

    Science.gov (United States)

    Gao, Pengfei; Korley, Frederick; Martin, Jennifer; Chen, Bean T

    2002-01-01

    This study identified unique microbial volatile organic compounds (UMVOCs) produced by five Aspergillus species (A. fumigatus, A. versicolor, A. sydowi, A. flavus, and A. niger) cultivated on malt extract agar and gypsum board. The hypothesis was that UMVOCs can be used to predict the presence of Aspergillus species. During the cultivation humidified air was continually supplied and evenly distributed through each of the culture flasks. Volatile metabolites were collected using Tenax TA tubes on Days 8, 16, and 30 after inoculation. The volatile metabolites were determined by gas chromatography/mass spectroscopy after thermal desorption. Nine compounds recognized as UMVOCs--3-methyl-1-butanol; 2-methyl-1-propanol; terpineol; 2-heptanone; 1-octen-3-ol; dimethyl disulfide; 2-hexanone; 3-octanone; and 2-pentylfuran--were found on the cultures in detectable amounts. The first two compounds were detected at the highest frequency when combining both media. The first four compounds were found to be the dominant UMVOCs on gypsum board, which could be used as chemical markers of the common Aspergillus species grown indoors.

  11. The preparation of organic radiopharmaceuticals and labelled compounds using short-lived cyclotron-produced radionuclides

    International Nuclear Information System (INIS)

    Uhlenhut, G.J.; Koch, H.

    1982-01-01

    Accelerator-produced nuclides and radiopharmaceutical production are discussed with examples of pertinent methods of isotope production, methods of incorporation into organic molecules, and the general problems attandant on the production and use of these materials in this new and interdisciplinary effort. The literature is surveyed with stress being given to the use of 11 C, 13 N and 15 O. 205 references are included. (author)

  12. Two new Penicillium species Penicillium buchwaldii and Penicillium spathulatum, producing the anticancer compound asperphenamate

    DEFF Research Database (Denmark)

    Frisvad, Jens Christian; Houbraken, Jos; Popma, Suuske

    2013-01-01

    Penicillium buchwaldii sp. nov. (type strain CBS 117181(T) = IBT 6005(T) = IMI 30428(T) ) and Penicillium spathulatum sp. nov. (CBS 117192(T) = IBT 22220(T) ) are described as new species based on a polyphasic taxonomic approach. Isolates of P. buchwaldii typically have terverticillate conidiopho...... were mainly isolated from indoor environments and food and feedstuffs. The fact that asperphenamate has been found in many widely different plants may indicate that endophytic fungi rather than the plants are the actual producers....

  13. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms

    OpenAIRE

    Seleem, Dalia; Chen, Emily; Benso, Bruna; Pardi, Vanessa; Murata, Ramiro M.

    2016-01-01

    Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent, The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876) in vitro and investigate whether monolaurin can alter gene expressio...

  14. Haliscosamine: a new antifungal sphingosine derivative from the Moroccan marine sponge Haliclona viscosa

    OpenAIRE

    El-Amraoui, Belkassem; Biard, Jean-Fan?ois; Fassouane, Aziz

    2013-01-01

    In the aim of searching for new antifungal products from marine origin, we have isolated a sphingosine derivative, (9Z)-2-amino-docos-9-ene-1,3,13,14-tetraol (Haliscosamine) from the Moroccan sea sponge Haliclona viscosa using bio-guided (antifungal) HPLC methods. The molecular structure of this compound was elucidated by spectrometric techniques IR, UV, MS and NMR. The isolated metabolite showed a significant antifungal activity against Cryptococcus and Candida species and a weak general tox...

  15. Alteration of oxidative phosphorylation as a possible mechanism of the antifungal action of p-coumaric acid against Botrytis cinerea.

    Science.gov (United States)

    Morales, J; Mendoza, L; Cotoras, M

    2017-10-01

    The aim of this study was to analyse the mechanism of action of p-coumaric acid against isolate B05·10 of Botrytis cinerea. For this purpose, the effect of this compound on cell membrane, cell wall and oxidative phosphorylation was determined. Induction of oxidative stress triggered by this compound was also studied. p-coumaric acid showed antifungal effect on the mycelial growth. Additionally, the compound was able to retard the germination of Botrytis cinerea conidia. The mechanism of action of this compound was analysed using fluorescent probes. p-Coumaric acid did not affect the integrity of cell wall and plasmatic membrane and neither produced oxidative stress. Finally, it was shown that the compound produced an increase in oxygen consumption. p-coumaric acid performs as a mitochondrial uncoupler in B. cinerea. Its role as an uncoupler of oxidative phosphorylation could be explained to its acidic, nonpolar and planar characteristics. These structural and chemical characteristics would favour ability of p-coumaric acid to pass through cellular membranes. Plant secondary metabolites can be used as an alternative way to control phytopathogenic fungi. The knowledge of the action mechanism of these compounds can contribute to design modified molecules with higher antifungal activity. © 2017 The Society for Applied Microbiology.

  16. Anthropogenic and naturally-produced organobrominated compounds in marine mammals from Brazil.

    Science.gov (United States)

    Dorneles, Paulo R; Lailson-Brito, José; Dirtu, Alin C; Weijs, Liesbeth; Azevedo, Alexandre F; Torres, João P M; Malm, Olaf; Neels, Hugo; Blust, Ronny; Das, Krishna; Covaci, Adrian

    2010-01-01

    Liver samples from 51 cetaceans, comprising 10 species, stranded between 1994 and 2006 in a highly industrialized and urbanized region in Southeast Brazil, were analyzed for polybrominated diphenyl ethers (PBDEs) and methoxylated-PBDEs (MeO-PBDEs). A concentration range of PBDEs (3-5960ng/g lw) similar to that observed in Northern Hemisphere dolphins was found. MeO-PBDE concentrations in continental shelf (CS) dolphins from Brazil are among the highest detected to date in cetaceans (up to 250microg/g lw). Higher SigmaMeO-PBDE concentrations were measured in CS and oceanic dolphins than in estuarine dolphins. The SigmaPBDE/SigmaMeO-PBDE ratio varied significantly ranging from a mean value of 7.12 to 0.08 and 0.01 for estuarine, CS and oceanic species, respectively. A positive correlation was observed between SigmaPBDE and year of stranding of male estuarine dolphins (Sotalia guianensis), which suggests temporal variation in the exposure. Placental transfer of organobrominated compounds was also evidenced in S. guianensis.

  17. Evaluation of Volatile Organic Compounds and Carbonyl Compounds Present in the Cabins of Newly Produced, Medium- and Large-Size Coaches in China

    Directory of Open Access Journals (Sweden)

    Yan-Yang Lu

    2016-06-01

    Full Text Available An air-conditioned coach is an important form of transportation in modern motorized society; as a result, there is an increasing concern of in-vehicle air pollution. In this study, we aimed to identify and quantify the levels of volatile organic compounds (VOCs and carbonyl compounds (CCs in air samples collected from the cabins of newly produced, medium- and large-size coaches. Among the identified VOCs and CCs, toluene, ethylbenzene, xylene, formaldehyde, acetaldehyde, acrolein/acetone, and isovaleraldehyde were relatively abundant in the cabins. Time was found to affect the emissions of the contaminants in the coaches. Except for benzaldehyde, valeraldehyde and benzene, the highest in-vehicle concentrations of VOCs and CCs were observed on the 15th day after coming off the assembly line, and the concentrations exhibited an approximately inverted U-shaped pattern as a function of time. Interestingly, this study also showed that the interior temperature of the coaches significantly affected the VOCs emissions from the interior materials, whereas the levels of CCs were mainly influenced by the relative humidity within the coaches. In China, guidelines and regulations for the in-vehicle air quality assessment of the coaches have not yet been issued. The results of this study provide further understanding of the in-vehicle air quality of air-conditioned coaches and can be used in the development of both specific and general rules regarding medium- and large-size coaches.

  18. Is the lower atmosphere a readily accessible reservoir of culturable, antimicrobial compound-producing Actinomycetales?

    Directory of Open Access Journals (Sweden)

    Carolyn F. Weber

    2015-08-01

    Full Text Available Recent metagenomic studies have revealed that microbial diversity in the atmosphere rivals that of surface environments. This indicates that the atmosphere may be worth bioprospecting in for novel microorganisms, especially those selected for by harsh atmospheric conditions. This is interesting in light of the antibiotic resistance crisis and renewed interests in bioprospecting for members of the Actinomycetales, which harbor novel secondary metabolite-producing pathways and produce spores that make them well suited for atmospheric travel. The latter leads to the hypothesis that the atmosphere may be a promising environment in which to search for novel Actinomycetales. Although ubiquitous in soils, where bioprospecting efforts for Actinomycetales have been and are largely still focused, we present novel data indicating that culturable members of this taxonomic order are 3 to 5.6 times more abundant in air samples collected at 1.5, 4.5, 7.5 and 18 m above the ground, than in the underlying soil. These results support the hypothesis that mining the vast and readily accessible lower atmosphere for novel Actinomycetales in the search for undescribed secondary metabolites, could prove fruitful.

  19. Lactobacillus amylovorus DSM 19280 as a novel food-grade antifungal agent for bakery products.

    Science.gov (United States)

    Ryan, Liam A M; Zannini, Emanuele; Dal Bello, Fabio; Pawlowska, Agata; Koehler, Peter; Arendt, Elke K

    2011-04-29

    Mould spoilage is the main cause of substantial economic loss in bakery industry and might also cause public health problems due to the production of mycotoxins. The reduction of mould growth in bakery products is thus of crucial importance and there is great interest to develop safe and efficient strategies for this purpose. In this study Lactobacillus amylovorus DSM19280 has been shown to produce a wide spectrum of antifungal compounds active against common bread spoilage fungi. Among the indicator moulds, Aspergillus fumigatus and Fusarium culmorum were the most sensitive organisms. Several antifungal compounds were found to be present in synthetic medium inoculated with L. amylovorus DSM19280 strain, some of them being reported here for the first time. Wheat doughs fermented with L. amylovorus DSM19280 had good rheological properties and the breads thereof were of high quality as shown by rheofermentometer and texture analyser measurements. The results were compared with those obtained with a control non-antifungal L. amylovorus DSM20531(T) strain, a non-acidified and a chemically acidified dough. The quality of sourdough and bread fermented with L. amylovorus DSM 19280 was comparable to that obtained by using L. amylovorus DSM20531 (T). Additionally, breads were evaluated for the ability to retard the growth of Fusarium culmorum FST 4.05, Aspergillus niger FST4.21, Penicillium expansum FST 4.22, Penicillium roqueforti FST 4.11 and fungal flora from the bakery environment. The biological preservation of bread with L. amylovorus DSM 19280 was also compared to the most commonly used antifungal agent Calcium propionate. Breads containing sourdough fermented with L. amylovorus DSM 19280 were more effective in extending the shelf life of bread than the calcium propionate. Copyright © 2011 Elsevier B.V. All rights reserved.

  20. Hydrogen peroxide as a new defensive compound in "benzoyl cyanide" producing polydesmid millipedes.

    Science.gov (United States)

    Kuwahara, Yasumasa; Yamaguchi, Takuya; Ichiki, Yayoi; Tanabe, Tsutomu; Asano, Yasuhisa

    2017-04-01

    Hydrogen peroxide was newly and simultaneously demonstrated with well-known hydrogen cyanide as a component of defensive secretions of "benzoyl cyanide" producing polydesmid millipedes. Presence of hydrogen peroxide was successively evidenced by Trinder reagent's spray with colorless as well as oily smears of defensive secretions containing benzoyl cyanide and hydrogen cyanide by alkaline picrate paper treatment. Linear correlation was demonstrated between quantities of hydrogen peroxide and benzoyl cyanide. By qualitative assay, seven benzoyl cyanide containing polydesmidans (six species of adults and one species of a nymph at stadium I) tested positive to Trinder reagent, indicative of the presence of hydrogen peroxide (together with hydrogen cyanide), while two cyanogenic species without benzoyl cyanide exhibited negative responses to the reagent. Two types of millipedes were elucidated as species of cyanogenic Polydesmida.

  1. Antifungal and antibacterial compounds from Streptomyces strains ...

    African Journals Online (AJOL)

    African Journal of Biotechnology. Journal Home · ABOUT THIS JOURNAL · Advanced Search · Current Issue · Archives · Journal Home > Vol 8, No 13 (2009) >. Log in or Register to get access to full text downloads.

  2. Antifungal proteins and peptides of leguminous and non-leguminous origins.

    Science.gov (United States)

    Ng, T B

    2004-07-01

    Antifungal proteins and peptides, as their names imply, serve a protective function against fungal invasion. They are produced by a multitude of organisms including leguminous flowering plants, non-leguminous flowering plants, gymnosperms, fungi, bacteria, insects and mammals. The intent of the present review is to focus on the structural and functional characteristics of leguminous, as well as non-leguminous, antifungal proteins and peptides. A spectacular diversity of amino acid sequences has been reported. Some of the antifungal proteins and peptides are classified, based on their structures and/or functions, into groups including chitinases, glucanases, thaumatin-like proteins, thionins, and cyclophilin-like proteins. Some of the well-known proteins such as lectins, ribosome inactivating proteins, ribonucleases, deoxyribonucleases, peroxidases, and protease inhibitors exhibit antifungal activity. Different antifungal proteins may demonstrate different fungal specificities. The mechanisms of antifungal action of only some antifungal proteins including thaumatin-like proteins and chitinases have been elucidated.

  3. Prospective Source of Antimicrobial Compounds From Pigment Produced by Bacteria associated with Brown Alga ( Phaeophyceae ) Isolated from Karimunjawa island, Indonesia

    Science.gov (United States)

    Lunggani, A. T.; Darmanto, Y. S.; Radjasa, O. K.; Sabdono, A.

    2018-02-01

    Brown algae or Phaeophyceae characterized by their natural pigments that differ from other important algal classes. Several publications proves that brown algae - associated bacteria have great potential in developing marine pharmaceutical industry since they are capable to synthesized numerous bioactive metabolite compounds. However the potency of marine pigmented microbes associated with brown alga to produce natural pigments and antimicrobials has been less studied. Marine pigmented bacteria associated with brown algae collected from Karimunjawa Island were successfully isolated and screened for antimicrobial activity. The aim of this research was evaluated of the antimicrobial activity of pigments extracted from culturable marine pigmented bacteria on some pathogenic bacteria and yeast. The results showed that all isolates had antimicrobial activity and could be prospectively developed as antimicrobial agent producing pigments. The 6 marine pigmented bacteria was identified to genus level as Pseudoalteromonas, Sphingomonas, Serratia, Paracoccus, Vibrio.

  4. High-Speed Counter-Current Chromatography (HSCCC) Purification of Antifungal Hydroxy Unsaturated Fatty Acids from Plant-Seed Oil and Lactobacillus Cultures.

    Science.gov (United States)

    Liang, Nuanyi; Cai, Pengfei; Wu, Datong; Pan, Yuanjiang; Curtis, Jonathan M; Gänzle, Michael G

    2017-12-27

    Hydroxy unsaturated fatty acids (HUFA) can function as antifungal agents. To investigate the antifungal spectrum, that is, the scope of the in vitro fungal-inhibition activities of HUFA and their potential applications, three HUFA were produced by microbial transformation or extracted from plant-seed oils; these compounds included coriolic acid (13-hydroxy-9,11-octadecadienoic acid) from Coriaria seed oil, 10-hydroxy-12-octadecenoic acid from cultures of Lactobacillus hammesii, and 13-hydroxy-9-octadecenoic acid from cultures of Lactobacillus plantarum TMW1.460Δlah. HUFA were purified by high-speed counter-current chromatography (HSCCC), characterized by LC-MS and MS/MS, and their antifungal activities were evaluated with 15 indicator fungal strains. The HUFA had different antifungal spectra when compared with unsaturated fatty acids with comparable structures but without hydroxy groups. The inhibitory effects of HUFA specifically targeted filamentous fungi, including Aspergillus niger and Penicillium roqueforti, whereas yeasts, including Candida spp. and Saccharomyces spp., were resistant to HUFA. The findings here support the development of food applications for antifungal HUFA.

  5. Volatile Flavor Compounds Produced by Molds of Aspergillus, Penicillium, and Fungi imperfecti.

    Science.gov (United States)

    Kaminski, E; Stawicki, S; Wasowicz, E

    1974-06-01

    Strains of molds Aspergillus niger, A. ochraceus, A. oryzae, A. parasiticus, Penicillium chrysogenum, P. citrinum, P. funiculosum, P. raistrickii, P. viridicatum, Alternaria, Cephalosporium, and Fusarium sp. were grown on sterile coarse wheat meal at 26 to 28 C for 120 h. The volatiles from mature cultures were distilled at low temperature under reduced pressure. The distillates from traps -40 and -78 C were extracted with methylene chloride and subsequently concentrated. All the concentrates thus obtained were analyzed by gas-liquid chromatography, mass spectrometry, chemical reactions of functional groups, and olfactory evaluation. Six components detected in the culture distillates were identified positively: 3-methylbutanol, 3-octanone, 3-octanol, 1-octen-3-ol, 1-octanol, and 2-octen-1-ol. They represented 67 to 97% of all the volatiles occurring in the concentrated distillate. The following 14 components were identified tentatively: octane, isobutyl alcohol, butyl alcohol, butyl acetate, amyl acetate, octyl acetate, pyridine, hexanol, nonanone, dimethylpyrazine, tetramethylpyrazine, benzaldehyde, propylbenzene, and phenethyl alcohol. Among the volatiles produced by molds, 1-octen-3-ol yielding a characteristic fungal odor was found predominant.

  6. Antifungal Activity of Selected Lactic Acid Bacteria and Propionic Acid Bacteria against Dairy-Associated Spoilage Fungi

    DEFF Research Database (Denmark)

    Aunsbjerg, Stina Dissing

    Bacterial cultures of lactic and propionic acid bacteria are widely used in fermented products including dairy products. Spoilage fungi may constitute a quality and safety issue in these products. The antifungal properties of some lactic and propionic acid bacteria make them potential candidates...... diacetyl and lactic acid, 6 antifungal hydroxy acids were identified. Of these, 3 have previously been reported from antifungal lactic acid bacteria, whereas the other 3 hydroxy acids have not previously been reported produced by antifungal lactic acid bacteria....

  7. Zygosaccharomyces bailii Is a Potential Producer of Various Flavor Compounds in Chinese Maotai-Flavor Liquor Fermentation

    Directory of Open Access Journals (Sweden)

    Yan Xu

    2017-12-01

    Full Text Available Zygosaccharomyces bailii is a common yeast in various food fermentations. Understanding the metabolic properties and genetic mechanisms of Z. bailii is important for its industrial applications. Fermentation characteristics of Z. bailii MT15 from Chinese Maotai-flavor liquor fermentation were studied. Z. bailii MT15 produced various flavor compounds, including 19 alcohols, six acids, three esters, three ketones, and two aldehydes. Moreover, production of acids and aldehydes were increased by 110 and 41%, respectively, at 37°C (the maximum temperature in liquor fermentation compared with that at 30°C, indicating its excellent flavor productivity. Z. bailii MT15 is a diploid with genome size of 20.19 Mb. Comparative transcriptome analysis revealed that 12 genes related to amino acid transport were significantly up-regulated (2.41- to 5.11-fold at 37°C. Moreover, genes ARO8, ARO9, and ALDH4 involved in amino acid metabolism also showed higher expression levels (>1.71-fold at 37°C. Increased substrate supply and a vigorous metabolism might be beneficial for the increased production of acids and aldehydes at 37°C. This work revealed the potential contribution of Z. bailii to various flavor compounds in food fermentation, and produced insights into the metabolic mechanisms of Z. bailii in flavor production.

  8. Stand-off detection of plant-produced volatile organic compounds using short-range Raman LIDAR

    Science.gov (United States)

    Johnson, Lewis; Barnett, Cleon; Brown, Christopher; Crawford, Devron; Tumlinson, James

    2004-03-01

    Several plant species release volatile organic compounds (VOCs) when under stresses such as herbivore feeding attack. The release of these plant-produced VOCs (i.e. terpenes) triggers the release of active biochemical defenses, which target the attacker. In some cases, the VOCs send cues to nearby carnivorous predators to attract them to the feeding herbivore. Volatile compounds are released both locally by damaged leaves and systemically by the rest of the plant. These compounds are released in large quantities, which facilitate detection of pests in the field by parasitoids. Detecting the plant"s VOC emissions as a function of various parameters (e.g. ambient temperature, atmospheric nitrogen levels, etc.) is essential to designing effective biological control systems. In addition these VOC releases may serve as early warning indicator of chemo-bio attacks. By combining Raman spectroscopy techniques with Laser Remote Sensing (LIDAR) systems, we are developing a Standoff detection system. Initial results indicate that is it possible to detect and differentiate between various terpenes, plant species, and other chemical compounds at distances greater than 12 meters. Currently, the system uses the 2nd harmonic of a Nd:YAG; however plans are underway to improve the Raman signal by moving the illumination wavelength into the solar-blind UV region. We report on our initial efforts of designing and characterizing this in a laboratory proof of concept system. We envision that this effort will lead to the design of a portable field-deployable system to rapidly characterize, with a high spatial resolution, large crops and other fields.

  9. Antifungal activity of cinnamaldehyde and eugenol congeners against wood-rot fungi.

    Science.gov (United States)

    Cheng, Sen-Sung; Liu, Ju-Yun; Chang, Ed-Haun; Chang, Shang-Tzen

    2008-07-01

    In this study, the antifungal activities of cinnamaldehyde and eugenol congeners against white-rot fungus Lenzites betulina and brown-rot fungus Laetiporus sulphureus were evaluated and the relationships between the antifungal activity and the chemical structures were also examined. Results from antifungal tests revealed that cinnamaldehyde, alpha-methyl cinnamaldehyde, (E)-2-methylcinnamic acid, eugenol and isoeugenol exhibited strong antifungal activity against all fungi tested. Results derived from the chemical structure-antifungal activity relationship study suggested that compounds with an aldehyde group or an acid group, a conjugated double bond and a length of CH chain outside the ring affect their antifungal properties. Furthermore, the presence of the methyl moiety in the ortho position may have a considerable influence on the inhibitory action against L. betulina and L. sulphureus. In addition, the lipophilicity may play, in part, a crucial role in determining the toxicity of phenylpropenes.

  10. Significance of volatile compounds produced by spoilage bacteria in vacuum-packed cold-smoked salmon ( Salmo salar ) analyzed by GC-MS and multivariate regression

    DEFF Research Database (Denmark)

    Jørgensen, Lasse Vigel; Huss, Hans Henrik; Dalgaard, Paw

    2001-01-01

    , 1- penten-3-ol, and 1-propanol. The potency and importance of these compounds was confirmed by gas chromatography- olfactometry. The present study provides valuable information on the bacterial reactions responsible for spoilage off-flavors of cold-smoked salmon, which can be used to develop......Changes were studied in the concentration of 38 volatile compounds during chilled storage at 5 degreesC of six lots of commercially produced vacuum-packed cold-smoked salmon and sterile cold-smoked salmon. The majority of volatile compounds produced during spoilage of cold-smoked salmon were...... alcohols, which were produced by microbial activity. Partial least- squares regression of volatile compounds and sensory results allowed for a multiple compound quality index to be developed. This index was based on volatile bacterial metabolites, 1- propanol and 2-butanone, and 2-furan...

  11. Antifungal Quinoline Alkaloids from Waltheria indica.

    Science.gov (United States)

    Cretton, Sylvian; Dorsaz, Stéphane; Azzollini, Antonio; Favre-Godal, Quentin; Marcourt, Laurence; Ebrahimi, Samad Nejad; Voinesco, Francine; Michellod, Emilie; Sanglard, Dominique; Gindro, Katia; Wolfender, Jean-Luc; Cuendet, Muriel; Christen, Philippe

    2016-02-26

    Chemical investigation of a dichloromethane extract of the aerial parts of Waltheria indica led to the isolation and characterization of five polyhydroxymethoxyflavonoids, namely, oxyanin A (1), vitexicarpin (3), chrysosplenol E (4), flindulatin (5), 5-hydroxy-3,7,4'-trimethoxyflavone (6), and six quinolone alkaloids, waltheriones M-Q (2, 7, 8, 10, 11) and 5(R)-vanessine (9). Among these, compounds 2, 7, 8, 10, and 11 have not yet been described in the literature. Their chemical structures were established by means of spectroscopic data interpretation including (1)H and (13)C, HSQC, HMBC, COSY, and NOESY NMR experiments and UV, IR, and HRESIMS. The absolute configurations of the compounds were established by ECD. The isolated constituents and 10 additional quinoline alkaloids previously isolated from the roots of the plant were evaluated for their in vitro antifungal activity against the human fungal pathogen Candida albicans, and 10 compounds (7, 9, 11-16, 18, 21) showed growth inhibitory activity on both planktonic cells and biofilms (MIC ≤ 32 μg/mL). Their spectrum of activity against other pathogenic Candida species and their cytotoxicity against human HeLa cells were also determined. In addition, the cytological effect of the antifungal isolated compounds on the ultrastructure of C. albicans was evaluated by transmission electron microscopy.

  12. A comparative study on the potential of epiphytic yeasts isolated from tropical fruits to produce flavoring compounds.

    Science.gov (United States)

    Grondin, Eric; Shum Cheong Sing, Alain; Caro, Yanis; Raherimandimby, Marson; Randrianierenana, Ando Lalaniaina; James, Steve; Nueno-Palop, Carmen; François, Jean Marie; Petit, Thomas

    2015-06-16

    In recent years, there has been an increasing interest in identifying and characterizing the yeast flora associated with diverse types of habitat because of the many potential desirable technological properties of these microorganisms, especially in food applications. In this study, a total of 101 yeast strains were isolated from the skins of tropical fruits collected in several locations in the South West Indian Ocean. Sequence analysis of the D1/D2 domains of the large subunit (LSU) ribosomal RNA gene identified 26 different species. Among them, two species isolated from the skins of Cape gooseberry and cocoa beans appeared to represent putative new yeast species, as their LSU D1/D2 sequence was only 97.1% and 97.4% identical to that of the yeasts Rhodotorula mucilaginosa and Candida pararugosa, respectively. A total of 52 Volatile Organic Compounds (VOCs) were detected by Head Space Solid Phase Micro Extraction coupled to Gas Chromatography and Mass Spectroscopy (HS-SPME-GC/MS) from the 26 yeast species cultivated on a glucose rich medium. Among these VOCs, 6 uncommon compounds were identified, namely ethyl but-2-enoate, ethyl 2-methylbut-2-enoate (ethyl tiglate), ethyl 3-methylbut-2-enoate, 2-methylpropyl 2-methylbut-2-enoate, butyl 2-methylbut-2-enoate and 3-methylbutyl 2-methylbut-2-enoate, making them possible yeast species-specific markers. In addition, statistical methods such as Principal Component Analysis allowed to associate each yeast species with a specific flavor profile. Among them, Saprochaete suaveolens (syn: Geotrichum fragrans) turned to be the best producer of flavor compounds, with a total of 32 out of the 52 identified VOCs in its flavor profile. Copyright © 2015 Elsevier B.V. All rights reserved.

  13. Environmental feedbacks and engineered nanoparticles: mitigation of silver nanoparticle toxicity to Chlamydomonas reinhardtii by algal-produced organic compounds.

    Directory of Open Access Journals (Sweden)

    Louise M Stevenson

    Full Text Available The vast majority of nanotoxicity studies measures the effect of exposure to a toxicant on an organism and ignores the potentially important effects of the organism on the toxicant. We investigated the effect of citrate-coated silver nanoparticles (AgNPs on populations of the freshwater alga Chlamydomonas reinhardtii at different phases of batch culture growth and show that the AgNPs are most toxic to cultures in the early phases of growth. We offer strong evidence that reduced toxicity occurs because extracellular dissolved organic carbon (DOC compounds produced by the algal cells themselves mitigate the toxicity of AgNPs. We analyzed this feedback with a dynamic model incorporating algal growth, nanoparticle dissolution, bioaccumulation of silver, DOC production and DOC-mediated inactivation of nanoparticles and ionic silver. Our findings demonstrate how the feedback between aquatic organisms and their environment may impact the toxicity and ecological effects of engineered nanoparticles.

  14. Compounds used to produce cloned animals are genotoxic and mutagenic in mammalian assays in vitro and in vivo

    Directory of Open Access Journals (Sweden)

    R.J. Oliveira

    2014-04-01

    Full Text Available The compounds 6-dimethylaminopurine and cycloheximide promote the successful production of cloned mammals and have been used in the development of embryos produced by somatic cell nuclear transfer. This study investigated the effects of 6-dimethylaminopurine and cycloheximide in vitro, using the thiazolyl blue tetrazolium bromide colorimetric assay to assess cytotoxicity, the trypan blue exclusion assay to assess cell viability, the comet assay to assess genotoxicity, and the micronucleus test with cytokinesis block to test mutagenicity. In addition, the comet assay and the micronucleus test were also performed on peripheral blood cells of 54 male Swiss mice, 35 g each, to assess the effects of the compounds in vivo. The results indicated that both 6-dimethylaminopurine and cycloheximide, at the concentrations and doses tested, were cytotoxic in vitro and genotoxic and mutagenic in vitro and in vivo, altered the nuclear division index in vitro, but did not diminish cell viability in vitro. Considering that alterations in DNA play important roles in mutagenesis, carcinogenesis, and morphofunctional teratogenesis and reduce embryonic viability, this study indicated that 6-dimethylaminopurine and cycloheximide utilized in the process of mammalian cloning may be responsible for the low embryo viability commonly seen in nuclear transfer after implantation in utero.

  15. Screening for Endophytic Fungi from Turmeric Plant (Curcuma longa L.) of Sukabumi and Cibinong with Potency as Antioxidant Compounds Producer.

    Science.gov (United States)

    Bustanussalam; Rachman, Fauzy; Septiana, Eris; Lekatompessy, Sylvia J R; Widowati, Tiwit; Sukiman, Harmastini I; Simanjuntak, Partomuan

    2015-01-01

    Potency of medicinal plant is related to microorganisms lived in the plant tissue. Those microorganisms are known as endophytic microbes that live and form colonies in the plant tissue without harming its host. Each plant may contains several endophytic microbes that produce biological compounds or secondary metabolites due to co-evolution or genetic transfer from the host plant to endophytic microbes. Endophytic fungi research done for turmeric plant (Curcuma longa L.) gave 44 isolated fungi as results. Those 44 fungi isolated were fermented in Potato Dextrose Broth (PDB) media, filtered, extracted with ethylacetate and then were analyzed by Thin Layer Chromatography (TLC) method and tested for their antioxidant activity by radical scavenging method. The antioxidant activity of the ethylacetate filtrate extracts either from Sukabumi or Cibinong were higher than the biomass extracts. There were 6 fungi that showed antioxidant activities over 65%, i.e., with code name K.Cl.Sb.R9 (93.58%), K.Cl.Sb.A11 (81.49%), KCl.Sb.B1 (78.81%), KCl.Sb.R11 (71.67%) and K.Cl.Sb.A12 (67.76%) from Sukabumi and K.Cl.Cb.U1 (69.27%) from Cibinong. These results showed that bioproduction by endophytic microbes can gave potential antioxidant compounds.

  16. Compounds used to produce cloned animals are genotoxic and mutagenic in mammalian assays in vitro and in vivo

    Energy Technology Data Exchange (ETDEWEB)

    Oliveira, R.J. [Programa de Pós-Graduação em Biologia Celular e Molecular, Instituto de Biociências de Rio Claro, Universidade Estadual Paulista, Rio Claro, SP (Brazil); Centro de Estudos em Células Tronco, Terapia Celular e Genética Toxicológica, Núcleo de Hospital Universitário, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Programa de Pós-Graduação em Saúde em Desenvolvimento na Região Centro-Oeste, Faculdade de Medicina “Dr. Hélio Mandetta”, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Programa de Mestrado em Farmácia, Centro de Ciências Biológicas e da Saúde, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Mantovani, M.S.; Silva, A.F. da [Departamento de Biologia Geral, Universidade Estadual de Londrina, Londrina, PR (Brazil); Pesarini, J.R. [Centro de Estudos em Células Tronco, Terapia Celular e Genética Toxicológica, Núcleo de Hospital Universitário, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Programa de Pós-Graduação em Saúde em Desenvolvimento na Região Centro-Oeste, Faculdade de Medicina “Dr. Hélio Mandetta”, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Mauro, M.O. [Centro de Estudos em Células Tronco, Terapia Celular e Genética Toxicológica, Núcleo de Hospital Universitário, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Programa de Doutorado em Biotecnologia e Biodiversidade - Rede Pró Centro-Oeste, Universidade Federal de Mato Grosso do Sul, Campo Grande, MS (Brazil); Ribeiro, L.R. [Programa de Pós-Graduação em Biologia Celular e Molecular, Instituto de Biociências de Rio Claro, Universidade Estadual Paulista, Rio Claro, SP (Brazil); Programa de Pós-Graduação em Patologia, Faculdade de Medicina de Botucatu, Universidade Estadual Paulista, Botucatu, SP (Brazil)

    2014-03-28

    The compounds 6-dimethylaminopurine and cycloheximide promote the successful production of cloned mammals and have been used in the development of embryos produced by somatic cell nuclear transfer. This study investigated the effects of 6-dimethylaminopurine and cycloheximide in vitro, using the thiazolyl blue tetrazolium bromide colorimetric assay to assess cytotoxicity, the trypan blue exclusion assay to assess cell viability, the comet assay to assess genotoxicity, and the micronucleus test with cytokinesis block to test mutagenicity. In addition, the comet assay and the micronucleus test were also performed on peripheral blood cells of 54 male Swiss mice, 35 g each, to assess the effects of the compounds in vivo. The results indicated that both 6-dimethylaminopurine and cycloheximide, at the concentrations and doses tested, were cytotoxic in vitro and genotoxic and mutagenic in vitro and in vivo, altered the nuclear division index in vitro, but did not diminish cell viability in vitro. Considering that alterations in DNA play important roles in mutagenesis, carcinogenesis, and morphofunctional teratogenesis and reduce embryonic viability, this study indicated that 6-dimethylaminopurine and cycloheximide utilized in the process of mammalian cloning may be responsible for the low embryo viability commonly seen in nuclear transfer after implantation in utero.

  17. Antifungal Activity from Leaves of Acacia Nilotica against Pythium Aphanidermatum

    Directory of Open Access Journals (Sweden)

    A. J. Khan

    1996-01-01

    Full Text Available Gallic acid and methyl ester of gallic acid has been identified as antifungal compounds against the mycelial growth of Pythium aphanidermatum from acetone-water extracts of Acacia nilotica leaves. The growth of fungus was completely ceased by gallic acid and its methyl ester at 1000 ppm and 750 ppm, respectively. Antifungal properties of both compounds were found to be higher in combination than alone. The minimum inhibitory concentration for both compounds was 1000 ppm. No phytotoxic effect of the compounds was observed on watermelon seed germination. The growth of roots and shoots of watermelon seedlings was promoted by gallic acid but decreased with methyl ester of gallic acid. Nitrate reductase activity of the fungus was significantly inhibited by both compounds.

  18. Antifungal sourdough lactic acid bacteria as biopreservation tool in quinoa and rice bread.

    Science.gov (United States)

    Axel, Claudia; Brosnan, Brid; Zannini, Emanuele; Furey, Ambrose; Coffey, Aidan; Arendt, Elke K

    2016-12-19

    The use of sourdough fermented with specific strains of antifungal lactic acid bacteria can reduce chemical preservatives in bakery products. The main objective of this study was to investigate the production of antifungal carboxylic acids after sourdough fermentation of quinoa and rice flour using the antifungal strains Lactobacillus reuteri R29 and Lactobacillus brevis R2Δ as bioprotective cultures and the non-antifungal L. brevis L1105 as a negative control strain. The impact of the fermentation substrate was evaluated in terms of metabolic activity, acidification pattern and quantity of antifungal carboxylic acids. These in situ produced compounds (n=20) were extracted from the sourdough using a QuEChERS method and detected by a new UHPLC-MS/MS chromatography. Furthermore, the sourdough was applied in situ using durability tests against environmental moulds to investigate the biopreservative potential to prolong the shelf life of bread. Organic acid production and TTA values were lowest in rice sourdough. The sourdough fermentation of the different flour substrates generated a complex and significantly different profile of carboxylic acids. Extracted quinoa sourdough detected the greatest number of carboxylic acids (n=11) at a much higher concentration than what was detected from rice sourdough (n=9). Comparing the lactic acid bacteria strains, L. reuteri R29 fermented sourdoughs contained generally higher concentrations of acetic and lactic acid but also the carboxylic acids. Among them, 3-phenyllactic acid and 2-hydroxyisocaproic acid were present at a significant concentration. This was correlated with the superior protein content of quinoa flour and its high protease activity. With the addition of L. reuteri R29 inoculated sourdough, the shelf life was extended by 2 days for quinoa (+100%) and rice bread (+67%) when compared to the non-acidified controls. The L. brevis R2Δ fermented sourdough bread reached a shelf life of 4 days for quinoa (+100%) and

  19. Antifungal activities and active ingredients of Melodinus suaveolens Champ. ex Benth.

    Science.gov (United States)

    Xu, Yanan; Ling, Siquan; Zeng, Dongqiang; Tang, Wenwei

    2017-07-16

    Four Melodinus species with antifungal activity were found in survey of the floral resources, in Shiwan Mountain Natural Reserve, Guangxi Province, China. Crude methanolic extracts of the twigs and leaves of Melodinus suaveolens exhibited potent antifungal activities against the plant pathogenic fungi Colletotrichum musae, Colletotrichum graminicola, Colletotrichum gloeosporioides and Alternaria musae, and the ethyl acetate fraction inhibited these pathogens at rates of 85.37, 91.47, 72.77 and 89.87%, respectively (5 mg/mL). A new compound, (2R, 3S, 5S, 6R)-1-O-methyl- chiro-inositol was isolated from the ethyl acetate fraction, along with 15 known compounds. The antifungal activities of compounds (1-16) were evaluated for the first time. Compound (4) had potent antifungal activity against C. gloeosporioides, C. graminicola and A. musae.

  20. Antifungal activity of rice straw extract on some phytopathogenic fungi

    African Journals Online (AJOL)

    user

    2012-09-04

    Sep 4, 2012 ... Key words: Rice straw, allelochemicals, antifungal, Aspergillus flavus, Alternaria alternata, Botrytis cinerea, amylase, protease ..... Identification and quantification of compounds in a series of allelopathic and non- allelopathic rice root exudates. J. Chem. Ecol. 30:1647-1662. Timmer LW, Peever TL, Solel Z, ...

  1. Antifungal metabolites from fungal endophytes of Pinus strobus

    DEFF Research Database (Denmark)

    Sumarah, Mark W; Kesting, Julie R; Sørensen, Dan

    2011-01-01

    The extracts of five foliar fungal endophytes isolated from Pinus strobus (eastern white pine) that showed antifungal activity in disc diffusion assays were selected for further study. From these strains, the aliphatic polyketide compound 1 and three related sesquiterpenes 2-4 were isolated and c...

  2. Synthesis and Antifungal Activities of Some Novel Pyrimidine Derivatives

    Directory of Open Access Journals (Sweden)

    Dequn Sun

    2011-06-01

    Full Text Available Three series of new pyrimidine derivatives were synthesized and their antifungal activities were evaluated in vitro against fourteen phytopathogenic fungi. The results indicated that most of the synthesized compounds possessed fungicidal activities and some of them are more potent than the control fungicides. Preliminary SAR was also discussed.

  3. Combinatorial effect of mutagenesis and medium component optimization on Bacillus amyloliquefaciens antifungal activity and efficacy in eradicating Botrytis cinerea.

    Science.gov (United States)

    Masmoudi, Fatma; Ben Khedher, Saoussen; Kamoun, Amel; Zouari, Nabil; Tounsi, Slim; Trigui, Mohamed

    2017-04-01

    This work is directed towards Bacillus amyloliquefaciens strain BLB371 metabolite production for biocontrol of fungal phytopathogens. In order to maximise antifungal metabolite production by this strain, two approaches were combined: random mutagenesis and medium component optimization. After three rounds of mutagenesis, a hyper active mutant, named M3-7, was obtained. It produces 7 fold more antifungal metabolites (1800AU/mL) than the wild strain in MC medium. A hybrid design was applied to optimise a new medium to enhance antifungal metabolite production by M3-7. The new optimized medium (35g/L of peptone, 32.5g/L of sucrose, 10.5g/L of yeast extract, 2.4g/L of KH 2 PO 4 , 1.3g/L of MgSO 4 and 23mg/L of MnSO 4 ) achieved 1.62 fold enhancement in antifungal compound production (3000AU/mL) by this mutant, compared to that achieved in MC medium. Therefore, combinatory effect of these two approaches (mutagenesis and medium component optimization) allowed 12 fold improvement in antifungal activity (from 250UA/mL to 3000UA/mL). This improvement was confirmed against several phytopathogenic fungi with an increase of MIC and MFC over than 50%. More interestingly, a total eradication of gray mold was obtained on tomato fruits infected by Botrytis cinerea and treated by M3-7, compared to those treated by BLB371. From the practical point of view, combining random mutagenesis and medium optimization could be considered as an excellent tool for obtaining promising biological products useful against phytopathogenic fungi. Copyright © 2017 Elsevier GmbH. All rights reserved.

  4. Antifungal therapy in European hospitals

    DEFF Research Database (Denmark)

    Zarb, P; Amadeo, B; Muller, A

    2012-01-01

    The study aimed to identify targets for quality improvement in antifungal use in European hospitals and determine the variability of such prescribing. Hospitals that participated in the European Surveillance of Antimicrobial Consumption Point Prevalence Surveys (ESAC-PPS) were included. The WHO...... of 40,878 (3.7%) antimicrobials. Antifungals were mainly (54.2%) administered orally. Hospital-acquired infections represented 44.5% of indications for antifungals followed by medical prophylaxis at 31.2%. The site of infection was not defined in 36.0% of cases but the most commonly targeted sites were...... respiratory (19.2%) and gastrointestinal (18.8%). The most used antifungal was fluconazole (60.5%) followed by caspofungin (10.5%). Antifungal-antibacterial combinations were frequently used (77.5%). The predominance of fluconazole use in participating hospitals could result in an increase in prevalence...

  5. Naturally occurring antifungal aromatic esters and amides

    International Nuclear Information System (INIS)

    Ali, M.S.; Shahnaz; Tabassum, S.; Ogunwande, I.A.; Pervez, M.K.

    2010-01-01

    During the search of antifungal natural products from terrestrial plants, a new long chained aromatic ester named grandiflorate along with spatazoate from Portulaca grandiflora and N-[2-methoxy-2-(4-methoxyphenyl) ethyl]-trans-cinnamide and aegeline from Solanum erianthum of Nigeria were isolated and tested against six fungal species. The known constituents have not been reported so far from mentioned investigated plants. Structures of the isolated compounds were elucidated with the aid of spectroscopic techniques including two dimensional NMR experiments. Among the compounds, the esters found more potent than amides against Candida albicans and Aspergillus flavus. The new compound grandiflorate gave response against all tested fungal species while aegeline was found to give lowest inhibition during this study. (author)

  6. Mode of Antifungal Drugs Interaction with Cytochrome P- 450

    Directory of Open Access Journals (Sweden)

    M- Mahmodian

    1991-07-01

    Full Text Available Computer was used to identify the interactions of substrates and antifungal drugs with the enzyme, Cytochrome P-450; and then Molplot.bas computer program was applied to get three dimensional figures of 5-hydroxy camphor.oxidation products of camphor analogues, and antifungal drugs.Cartesian characteristics of atoms building molecules, are taken from Buildz. for program, which can calculate X,Y,Z coordinates of atoms by Zmatrix data. The other program which can calculate X,Y,Z coordinates, using fractional characteristics, is the Coord, for program that, gives our cartesian characteristics of the atoms of molecule, then by using these data, we obtain three dimensional figures and distance between active atoms in compounds under consideration. Results show that distance between two oxygen atoms in 5-exo-hydroxy- camphor and the other compounds obtained from oxidation of camphor analogues, with the distance of two oxygen atoms in antifungal compounds under discussion are equal. Therefore, we can conclude that, the antifungal molecule also interacts with enzyme's active site, by its own sites, in a similar manner to the 5-hydroxy camphor molecule, which is:"n1. Nitrogen atom (N of Imidazole and Triazole ring in antifungal molecule with Iron atom in heam molecule belonging to Cytochrome P-450 enzyme, are coordinated."n2. The other atoms such as : 0,S or N in structure of the antifungal drug are coordinated with hydrogen atom of hydroxyl group belong ing to Tyr-96 in the structure of enzyme, forming hydrogen bonding.

  7. Synthesis and antifungal evaluation of PCA amide analogues.

    Science.gov (United States)

    Qin, Chuan; Yu, Di-Ya; Zhou, Xu-Dong; Zhang, Min; Wu, Qing-Lai; Li, Jun-Kai

    2018-04-18

    To improve the physical and chemical properties of phenazine-1-carboxylic acid (PCA) and find higher antifungal compounds, a series of PCA amide analogues were designed and synthesized and their structures were confirmed by 1 H NMR, HRMS, and X-ray. Most compounds showed some antifungal activities in vitro. Particularly, compound 3d exhibited inhibition effect against Pyriculariaoryzac Cavgra with EC 50 value of 28.7 μM and compound 3q exhibited effect against Rhizoctonia solani with EC 50 value of 24.5 μM, more potently active than that of the positive control PCA with its EC 50 values of 37.3 μM (Pyriculariaoryzac Cavgra) and 33.2 μM (Rhizoctonia solani), respectively.

  8. Antifungal activity of streptomycetes isolated bentonite clay

    Directory of Open Access Journals (Sweden)

    V. P. Shirobokov

    2016-12-01

    Full Text Available Aim. To investigate the biological activity of streptomycetes, isolated from Ukrainian bentonite clay. Methods. For identification of the investigated microorganisms there were used generally accepted methods for study of morpho-cultural and biochemical properties and sequencing of 16Ѕ rRNA producer. Antagonistic activity of the strain was determined by agar diffusion and agar block method using gram-positive, gram-negative microorganisms and fungi. Results. Research of autochthonous flora from bentonite clay of Ukrainian various deposits proved the existence of stable politaxonomic prokaryotic-eukaryotic consortia there. It was particularly interesting that the isolated microorganisms had demonstrated clearly expressed antagonistic properties against fungi. During bacteriological investigation this bacterial culture was identified like representative of the genus Streptomyces. Bentonite streptomycetes, named as Streptomyces SVP-71, inagar mediums (agar block method inhibited the growth of fungi (yeast and mold; zones of growth retardation constituted of 11-36 mm, and did not affect the growth of bacteria. There were investigated the inhibitory effects of supernatant culture fluid, ethanol and butanol extracts of biomass streptomycetes on museum and clinical strains of fungi that are pathogenic for humans (Candida albicans, C. krusei, C. utilis, C. parapsilosis, C. tropicalis, C. kefir, S. glabrata, C. lusitaniae, Aspergillus niger, Mucor pusillus, Fusarium sporotrichioides. It has been shown that research antifungal factor had 100% of inhibitory effect against all fungi used in experiments in vitro. In parallel, it was found that alcohol extracts hadn’t influence to the growth of gram-positive and gram-negative bacteria absolutely. It was shown that the cultural fluid supernatant and alcoholic extracts of biomass had the same antagonistic effect, but with different manifestation. This evidenced about identity of antifungal substances

  9. Aroma Compounds Prevision using Artificial Neural Networks Influence of Newly Indigenous Saccharomyces SPP in White Wine Produced with Vitis Vinifera Cv Siria

    OpenAIRE

    Caldeira, A. Teresa; Martins, M. Rosário; Cabrita, Maria João; Ambrósio, Cristina; Arteiro, José; Neves, José; Vicente, Henrique

    2010-01-01

    Commercial yeasts strains of Saccharomyces cerevisae are frequently used in white wine production as starters in fermentation process, however, these strains can affect the wine characteristics. The aim of this study was to evaluate the effect of three strains of Saccharomyces spp. (var. 1, 2 and 3) on wine aroma compounds produced in microvinification assays. Microvinification assays were carried out with Vitis vinifera cv Síria grapes using the strains in study as starters. Aroma compounds ...

  10. Antifungal pharmacodynamics: Latin America's perspective.

    Science.gov (United States)

    Gonzalez, Javier M; Rodriguez, Carlos A; Agudelo, Maria; Zuluaga, Andres F; Vesga, Omar

    The current increment of invasive fungal infections and the availability of new broad-spectrum antifungal agents has increased the use of these agents by non-expert practitioners, without an impact on mortality. To improve efficacy while minimizing prescription errors and to reduce the high monetary cost to the health systems, the principles of pharmacokinetics (PK) and pharmacodynamics (PD) are necessary. A systematic review of the PD of antifungals agents was performed aiming at the practicing physician without expertise in this field. The initial section of this review focuses on the general concepts of antimicrobial PD. In vitro studies, fungal susceptibility and antifungal serum concentrations are related with different doses and dosing schedules, determining the PD indices and the magnitude required to obtain a specific outcome. Herein the PD of the most used antifungal drug classes in Latin America (polyenes, azoles, and echinocandins) is discussed. Copyright © 2016 Sociedade Brasileira de Infectologia. Published by Elsevier Editora Ltda. All rights reserved.

  11. Antifungal pharmacodynamics: Latin America's perspective

    Directory of Open Access Journals (Sweden)

    Javier M. Gonzalez

    2017-01-01

    Full Text Available The current increment of invasive fungal infections and the availability of new broad-spectrum antifungal agents has increased the use of these agents by non-expert practitioners, without an impact on mortality. To improve efficacy while minimizing prescription errors and to reduce the high monetary cost to the health systems, the principles of pharmacokinetics (PK and pharmacodynamics (PD are necessary. A systematic review of the PD of antifungals agents was performed aiming at the practicing physician without expertise in this field. The initial section of this review focuses on the general concepts of antimicrobial PD. In vitro studies, fungal susceptibility and antifungal serum concentrations are related with different doses and dosing schedules, determining the PD indices and the magnitude required to obtain a specific outcome. Herein the PD of the most used antifungal drug classes in Latin America (polyenes, azoles, and echinocandins is discussed.

  12. Significance of volatile compounds produced by spoilage bacteria in vacuum-packed cold-smoked salmon ( Salmo salar ) analyzed by GC-MS and multivariate regression

    DEFF Research Database (Denmark)

    Jørgensen, Lasse Vigel; Huss, Hans Henrik; Dalgaard, Paw

    2001-01-01

    -carboxaldehyde produced by autolytic activity. Only a few of the volatile compounds produced during spoilage of cold-smoked salmon had an aroma value high enough to indicate contribution to the spoilage off- flavor of cold-smoked salmon. These were trimethylamine, 3- methylbutanal, 2-methyl-1-butanol, 3-methyl-1-butanol......, 1- penten-3-ol, and 1-propanol. The potency and importance of these compounds was confirmed by gas chromatography- olfactometry. The present study provides valuable information on the bacterial reactions responsible for spoilage off-flavors of cold-smoked salmon, which can be used to develop...

  13. Synthesis of heterocycle-attached methylidenebenzenesulfonohydrazones as antifungal agents.

    Science.gov (United States)

    Gao, Zhinan; Lv, Min; Li, Qin; Xu, Hui

    2015-11-15

    A series of heterocycle-attached methylidenebenzenesulfonohydrazone derivatives were synthesized and evaluated for their antifungal activities against seven phytopathogenic fungi such as Fusarium graminearum, Alternaria solani, Valsa mali, Phytophthora capsici, Fusarium solani, Botrytis cinerea, and Glomerella cingulata. Compounds 7b, 8d, 9a, 9b and 9d exhibited a good and broad-spectrum of antifungal activities against at least five phytopathogenic fungi at the concentration of 100 μg/mL. It demonstrated that addition of one double bond between the phenylsulfonylhydrazone fragment and the furan ring of 6a,b,d could afford more active compounds 9a,b,d; however, introduction of the nitro group on the phenyl ring of 6a-9a gave less potent compounds 6e-9e. Copyright © 2015 Elsevier Ltd. All rights reserved.

  14. Chemical Constituents and Antifungal Activity of Ficus hirta Vahl. Fruits

    Directory of Open Access Journals (Sweden)

    Chunpeng Wan

    2017-09-01

    Full Text Available Phytochemical investigation of Ficus hirta Vahl. (Moraceae fruits led to isolate two carboline alkaloids (1 and 2, five sesquiterpenoids/norsesquiterpenoids (3–7, three flavonoids (8–10, and one phenylpropane-1,2-diol (11. Their structures were elucidated by the analysis of their 1D and 2D NMR, and HR-ESI-MS data. All of the isolates were isolated from this species for the first time, while compounds 2, 4–6, and 8–11 were firstly reported from the genus Ficus. Antifungal assay revealed that compound 8 (namely pinocembrin-7-O-β-d-glucoside, a major flavonoid compound present in the ethanol extract of F. hirta fruits, showed good antifungal activity against Penicillium italicum, the phytopathogen of citrus blue mold caused the majority rotten of citrus fruits.

  15. Failure of Serial Taste-Taste Compound Presentations to Produce Overshadowing of Extinction of Conditioned Taste Aversion

    Science.gov (United States)

    Pineno, Oskar

    2010-01-01

    Two experiments were conducted to study overshadowing of extinction in a conditioned taste aversion preparation. In both experiments, aversive conditioning with sucrose was followed by extinction treatment with either sucrose alone or in compound with another taste, citric acid. Experiment 1 employed a simultaneous compound extinction treatment…

  16. Design, Synthesis, and Antifungal Activity of New α-Aminophosphonates

    Directory of Open Access Journals (Sweden)

    Zahra Rezaei

    2011-01-01

    Full Text Available α-Aminophosphonates are bioisosteres of amino acids and have several pharmacological activities. These compounds have been synthesized by various routes from reaction between amine, aldehyde, and phosphite compounds. In order to synthesize α-aminophosphonates, catalytic effect of CuCl2 was compared with FeCl3. Also all designed structures as well as griseofulvin were docked into the active site of microtubule (1JFF, using Autodock program. The results showed that the reactions were carried out in the presence of CuCl2 in lower yields, and also the time of reaction was longer in comparison with FeCl3. The chemical structures of the new compounds were confirmed by spectral analyses. The compounds were investigated for antifungal activity against several fungi in comparison with griseofulvin. An indole-derived bis(α-aminophosphonates with the best negative ΔG in docking study showed maximum antifungal activity against Microsporum canis, and other investigated compounds did not have a good antifungal activity.

  17. Synthesis and Antifungal Activity of Novel 3-Caren-5-One Oxime Esters

    Directory of Open Access Journals (Sweden)

    Min Huang

    2017-09-01

    Full Text Available A series of novel 3-caren-5-one oxime esters were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Two E-Z stereoisomers of the intermediate 3-caren-5-one oxime were separated by column chromatography for the first time. The structures of all the intermediates and target compounds were confirmed by UV-Vis, FTIR, NMR, ESI-MS, and elemental analysis. The antifungal activity of the target compounds was preliminarily evaluated by the in vitro method against Fusarium oxysporum f. sp. cucumerinum, Physalospora piricola, Alternaria solani, Cercospora arachidicola, Gibberella zeae, Rhizoeotnia solani, Bipolaris maydis, and Colleterichum orbicalare at 50 µg/mL. The target compounds exhibited best antifungal activity against P. piricola, in which compounds (Z-4r (R = β-pyridyl, (Z-4q (R = α-thienyl, (E-4f′ (R = p-F Ph, (Z-4i (R = m-Me Ph, (Z-4j (R = p-Me Ph, and (Z-4p (R = α-furyl had inhibition rates of 97.1%, 87.4%, 87.4%, 85.0%, 81.9%, and 77.7%, respectively, showing better antifungal activity than that of the commercial fungicide chlorothanil. Also, compound (Z-4r (R = β-pyridyl displayed remarkable antifungal activity against all the tested fungi, with inhibition rates of 76.7%, 82.7%, 97.1%, 66.3%, 74.7%, 93.9%, 76.7% and 93.3%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide chlorothanil. Besides, the E-Z isomers of the target oxime esters were found to show obvious differences in antifungal activity. These results provide an encouraging framework that could lead to the development of potent novel antifungal agents.

  18. Synthesis and Antifungal Activity of Novel 3-Caren-5-One Oxime Esters.

    Science.gov (United States)

    Huang, Min; Duan, Wen-Gui; Lin, Gui-Shan; Li, Kun; Hu, Qiong

    2017-09-12

    A series of novel 3-caren-5-one oxime esters were designed and synthesized by multi-step reactions in an attempt to develop potent antifungal agents. Two E - Z stereoisomers of the intermediate 3-caren-5-one oxime were separated by column chromatography for the first time. The structures of all the intermediates and target compounds were confirmed by UV-Vis, FTIR, NMR, ESI-MS, and elemental analysis. The antifungal activity of the target compounds was preliminarily evaluated by the in vitro method against Fusarium oxysporum f. sp. cucumerinum , Physalospora piricola , Alternaria solani , Cercospora arachidicola , Gibberella zeae, Rhizoeotnia solani , Bipolaris maydis , and Colleterichum orbicalare at 50 µg/mL. The target compounds exhibited best antifungal activity against P. piricola , in which compounds ( Z )- 4r (R = β -pyridyl), ( Z )- 4q (R = α -thienyl), ( E )- 4f' (R = p -F Ph), ( Z )- 4i (R = m -Me Ph), ( Z )- 4j (R = p -Me Ph), and ( Z )- 4p (R = α -furyl) had inhibition rates of 97.1%, 87.4%, 87.4%, 85.0%, 81.9%, and 77.7%, respectively, showing better antifungal activity than that of the commercial fungicide chlorothanil. Also, compound ( Z )- 4r (R = β -pyridyl) displayed remarkable antifungal activity against all the tested fungi, with inhibition rates of 76.7%, 82.7%, 97.1%, 66.3%, 74.7%, 93.9%, 76.7% and 93.3%, respectively, showing better or comparable antifungal activity than that of the commercial fungicide chlorothanil. Besides, the E-Z isomers of the target oxime esters were found to show obvious differences in antifungal activity. These results provide an encouraging framework that could lead to the development of potent novel antifungal agents.

  19. Essential oil of Algerian Eucalyptus citriodora: Chemical composition, antifungal activity.

    Science.gov (United States)

    Tolba, H; Moghrani, H; Benelmouffok, A; Kellou, D; Maachi, R

    2015-12-01

    Essential oil of Eucalyptus citriodora is a natural product which has been attributed for various medicinal uses. In the present investigation, E. citriodora essential oil was used to evaluate its antifungal effect against medically important dermatophytes. Essential oil from the Algerian E. citriodora leaves was analyzed by GC and GC/MS. The antifungal effect of E. citriodora essential oil was evaluated against four dermatophytes: Microsporum canis, Microsporum gypseum, Trichophyton mentagrophytes, Trichophyton rubrum using disc diffusion method, disc volatilization method, and agar dilution method. The chemical composition of the oil revealed the presence of 22 compounds accounting for 95.27% of the oil. The dominant compounds were citronellal (69.77%), citronellol (10.63%) and isopulegol (4.66%). The disc diffusion method, MIC and MFC determination, indicated that E. citriodora essential oil had a higher antifungal potential against the tested strains with inhibition zone diameter which varied from (12 to 90mm) and MIC and MFC values ranged from (0.6 to 5μL/mL and 1.25 to 5μL/mL) respectively. The M. gypseum was the most resistant to the oil. The results of the present study indicated that E. citriodora essential oil may be used as a new antifungal agent recommended by the pharmaceutical industries. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  20. Mass spectrometry identification of antifungal lipopeptides from Bacillus sp. BCLRB2 against Rhizoctonia solani and Sclerotinia sclerotiorum.

    Science.gov (United States)

    Elkahoui, S; Djébali, N; Karkouch, I; Ibrahim, A Hadj; Kalai, L; Bachkovel, S; Tabbene, O; Limam, F

    2014-01-01

    This work aims to characterize the bioactive molecules produced by an antagonistic Bacillus sp. strain BCLRB2 isolated from healthy leaves of olive tree against Rhizoctonia solani and Sclerotinia sclerotiorum. The bacterial strain isolated showed a high and persistent antifungal activity against the two pathogens. The free-cell supernatant showed also a high antifungal activity against R. solani and at a lower extent against S. sclerotiorum. The partial purification of the antifungal substances with methanol gradient applied to C18 column binding the Bacillus BCLRB2 culture supernatant showed that the 20% and 60% methanol fractions had a high and specific activity against S. sclerotiorum and R. solani, respectively. The mass spectrometry identification of the compounds in the fraction specifically active against S. sclerotiorum revealed the presence of bacillomycin D C16 as a major lipopeptide. The fraction specifically active against R. solani contained bacillomycin D C15 and 2 unknown lipopeptides. The 80% methanol fraction had a moderate and a broad spectrum activity against the two pathogens and consisted from two iturin D (C13 and C14) as a major lipopeptides.

  1. Antifungal activity of the pygidial gland secretion of Laemostenus punctatus (Coleoptera: Carabidae) against cave-dwelling micromycetes

    Science.gov (United States)

    Nenadić, Marija; Ljaljević-Grbić, Milica; Stupar, Miloš; Vukojević, Jelena; Ćirić, Ana; Tešević, Vele; Vujisić, Ljubodrag; Todosijević, Marina; Vesović, Nikola; Živković, Nemanja; Ćurčić, Srećko

    2017-06-01

    The antifungal potential of the pygidial gland secretion of the troglophilic ground beetle Laemostenus punctatus from a cave in Southeastern Serbia against cave-dwelling micromycetes, isolated from the same habitat, has been investigated. Eleven collected samples were analyzed and 32 isolates of cave-dwelling fungi were documented. A total of 14 fungal species were identified as members of the genera Aspergillus, Penicillium, Alternaria, Cladosporium, Rhizopus, Trichoderma, Arthrinium, Aureobasidium, Epicoccum, Talaromyces, and Fusarium. Five isolates were selected for testing the antifungal activity of the pygidial gland secretion: Talaromyces duclauxi, Aspergillus brunneouniseriatus, Penicillium sp., Rhizopus stolonifer, and Trichoderma viride. The microdilution method has been applied to detect minimal inhibitory concentrations (MICs) and minimal fungicidal concentrations (MFCs). The most sensitive isolate was Penicillium sp., while the other isolates demonstrated a high level of resistance to the tested agent. L. punctatus has developed a special mechanism of producing specific compounds that act synergistically within the secretion mixture, which are responsible for the antifungal action against pathogens from the cave. The results open opportunities for further research in the field of ground beetle defense against pathogens, which could have an important application in human medicine, in addition to the environmental impact, primarily.

  2. Mapping and Identification of Antifungal Peptides in the Putative Antifungal Protein AfpB from the Filamentous Fungus Penicillium digitatum.

    Science.gov (United States)

    Garrigues, Sandra; Gandía, Mónica; Borics, Attila; Marx, Florentine; Manzanares, Paloma; Marcos, Jose F

    2017-01-01

    Antifungal proteins (AFPs) from Ascomycetes are small cysteine-rich proteins that are abundantly secreted and show antifungal activity against non-producer fungi. A gene coding for a class B AFP (AfpB) was previously identified in the genome of the plant pathogen Penicillium digitatum . However, previous attempts to detect the AfpB protein were not successful despite the high expression of the corresponding afpB gene. In this work, the structure of the putative AfpB was modeled. Based on this model, four synthetic cysteine-containing peptides, PAF109, PAF112, PAF118, and PAF119, were designed and their antimicrobial activity was tested and characterized. PAF109 that corresponds to the γ-core motif present in defensin-like antimicrobial proteins did not show antimicrobial activity. On the contrary, PAF112 and PAF118, which are cationic peptides derived from two surface-exposed loops in AfpB, showed moderate antifungal activity against P. digitatum and other filamentous fungi. It was also confirmed that cyclization through a disulfide bridge prevented peptide degradation. PAF116, which is a peptide analogous to PAF112 but derived from the Penicillium chrysogenum antifungal protein PAF, showed activity against P. digitatum similar to PAF112, but was less active than the native PAF protein. The two AfpB-derived antifungal peptides PAF112 and PAF118 showed positive synergistic interaction when combined against P. digitatum . Furthermore, the synthetic hexapeptide PAF26 previously described in our laboratory also exhibited synergistic interaction with the peptides PAF112, PAF118, and PAF116, as well as with the PAF protein. This study is an important contribution to the mapping of antifungal motifs within the AfpB and other AFPs, and opens up new strategies for the rational design and application of antifungal peptides and proteins.

  3. Antifungal activity of bacterial strains from the rhizosphere of ...

    African Journals Online (AJOL)

    user

    2011-06-08

    Jun 8, 2011 ... This study evaluated the antifungal action of biomolecules produced from the secondary metabolism of bacterial strains found in the rhizosphere of semi arid plants against human pathogenic Candida albicans. Crude extracts were obtained using ethyl acetate as an organic solvent and the bioactivity was.

  4. Antifungal activity of bacterial strains from the rhizosphere of ...

    African Journals Online (AJOL)

    This study evaluated the antifungal action of biomolecules produced from the secondary metabolism of bacterial strains found in the rhizosphere of semi arid plants against human pathogenic Candida albicans. Crude extracts were obtained using ethyl acetate as an organic solvent and the bioactivity was assessed with a ...

  5. Nepenthes rafflesiana pitcher liquid has antifungal activity against Candida spp.

    Directory of Open Access Journals (Sweden)

    Hanna Yolanda

    2014-08-01

    Full Text Available Background To develop new effective antifungals, it is essential to search for antifungal compounds from plants such as Nepenthes spp., which have their greatest diversity in Indonesia. Since chitin-induced liquid (CIL from Nepenthes khasiana pitchers has antifungal activity, due to their naphthoquinone content, this study aimed to evaluate antifungal activity of Nepenthes rafflesiana pitcher liquids on Candida spp. Methods Collected pitcher liquids were of 3 types: non-induced liquid (NIL, prey-induced liquid (PIL, and chitin-induced liquid (CIL. Non-induced liquid (NIL was collected from fresh naturally opened pitchers, PIL from opened pitchers after 3 hours of induction with Zophobas morio larvae, and CIL from closed pitchers after 5 days of chitin solution injection. The antifungal activity of the liquids against C. albicans, C. glabrata, C. krusei, and C. tropicalis were detected by disc diffusion and macrodilution methods. Results Inhibition zone diameters of NIL, PIL, and CIL against C. albicans were 35.00 (35.00 – 39.33 mm, 26.33 (23.00 – 40.00 mm, and 30.00 ( 28.00 – 32.00 mm, respectively, while for C. glabrata the zone diameters were 22.22 ± 3.66 mm, 29.89 ± 2.79 mm, and 28.89 ± 1.17 mm, respectively. No inhibition zones were found for NIL, PIL, and CIL against C. krusei and C. tropicalis. At concentrations of 80%, almost all samples showed visually apparent inhibition of fungal growth. Conclusion The pitcher liquid of N. rafflesiana has antifungal properties, presumably due to the presence of many potentially active substances, such as naphthoquinones, as has been proven in other studies.

  6. Nepenthes rafflesiana pitcher liquid has antifungal activity against Candida spp.

    Directory of Open Access Journals (Sweden)

    Hanna Yolanda

    2015-12-01

    Full Text Available BACKGROUND To develop new effective antifungals, it is essential to search for antifungal compounds from plants such as Nepenthes spp., which have their greatest diversity in Indonesia. Since chitin-induced liquid (CIL from Nepenthes khasiana pitchers has antifungal activity, due to their naphthoquinone content, this study aimed to evaluate antifungal activity of Nepenthes rafflesiana pitcher liquids on Candida spp. METHODS Collected pitcher liquids were of 3 types: non-induced liquid (NIL, prey-induced liquid (PIL, and chitin-induced liquid (CIL. Non-induced liquid (NIL was collected from fresh naturally opened pitchers, PIL from opened pitchers after 3 hours of induction with Zophobas morio larvae, and CIL from closed pitchers after 5 days of chitin solution injection. The antifungal activity of the liquids against C. albicans, C. glabrata, C. krusei, and C. tropicalis were detected by disc diffusion and macrodilution methods. RESULTS Inhibition zone diameters of NIL, PIL, and CIL against C. albicans were 35.00 (35.00 – 39.33 mm, 26.33 (23.00 – 40.00 mm, and 30.00 ( 28.00 – 32.00 mm, respectively, while for C. glabrata the zone diameters were 22.22 ± 3.66 mm, 29.89 ± 2.79 mm, and 28.89 ± 1.17 mm, respectively. No inhibition zones were found for NIL, PIL, and CIL against C. krusei and C. tropicalis. At concentrations of 80%, almost all samples showed visually apparent inhibition of fungal growth. CONCLUSION The pitcher liquid of N. rafflesiana has antifungal properties, presumably due to the presence of many potentially active substances, such as naphthoquinones, as has been proven in other studies.

  7. Candida Species Biofilms’ Antifungal Resistance

    Science.gov (United States)

    Silva, Sónia; Rodrigues, Célia F.; Araújo, Daniela; Rodrigues, Maria Elisa; Henriques, Mariana

    2017-01-01

    Candida infections (candidiasis) are the most prevalent opportunistic fungal infection on humans and, as such, a major public health problem. In recent decades, candidiasis has been associated to Candida species other than Candida albicans. Moreover, biofilms have been considered the most prevalent growth form of Candida cells and a strong causative agent of the intensification of antifungal resistance. As yet, no specific resistance factor has been identified as the sole responsible for the increased recalcitrance to antifungal agents exhibited by biofilms. Instead, biofilm antifungal resistance is a complex multifactorial phenomenon, which still remains to be fully elucidated and understood. The different mechanisms, which may be responsible for the intrinsic resistance of Candida species biofilms, include the high density of cells within the biofilm, the growth and nutrient limitation, the effects of the biofilm matrix, the presence of persister cells, the antifungal resistance gene expression and the increase of sterols on the membrane of biofilm cells. Thus, this review intends to provide information on the recent advances about Candida species biofilm antifungal resistance and its implication on intensification of the candidiasis. PMID:29371527

  8. Mapping and Identification of Antifungal Peptides in the Putative Antifungal Protein AfpB from the Filamentous Fungus Penicillium digitatum

    OpenAIRE

    Garrigues, Sandra; Gandía Gómez, Mónica; Borics, Attila; Marx, Florentine; Manzanares, Paloma; Marcos López, José Francisco

    2017-01-01

    Antifungal proteins (AFPs) from Ascomycetes are small cysteine-rich proteins that are abundantly secreted and show antifungal activity against non-producer fungi. A gene coding for a class B AFP (AfpB) was previously identified in the genome of the plant pathogen Penicillium digitatum. However, previous attempts to detect the AfpB protein were not successful despite the high expression of the corresponding afpB gene. In this work, the structure of the putative AfpB was modeled. Based on this ...

  9. DYSREGULATION OF ION HOMEOSTASIS BY ANTIFUNGAL AGENTS

    Directory of Open Access Journals (Sweden)

    Yongqiang eZhang

    2012-04-01

    Full Text Available Ion signaling and transduction networks are central to fungal development and virulence because they regulate gene expression, filamentation, host association and invasion, pathogen stress response and survival. Dysregulation of ion homeostasis rapidly mediates cell death, forming the mechanistic basis by which a growing number of amphipathic but structurally unrelated compounds elicit antifungal activity. Included in this group is carvacrol, a terpenoid phenol that is a prominent component of oregano and other plant essential oils. Carvacrol triggers an early dose dependent Ca2+ burst and long lasting pH changes in the model yeast S. cerevisiae. The distinct phases of ionic transients and a robust transcriptional response that overlaps with Ca2+ stress and nutrient starvation point to specific signaling events elicited by plant terpenoid phenols, rather than a non-specific lesion of the membrane as was previously considered. We discuss the potential use of plant essential oils and other agents that disrupt ion signaling pathways as chemosensitizers to augment conventional antifungal therapy, and to convert fungistatic drugs with strong safety profiles into fungicides.

  10. Antifungal Activity of Eucalyptus Urophylla Oil Against Aspergillus Niger and Fusarium Oxysporum

    OpenAIRE

    Pujiarti, Rini; Hadi Nurjanto, Handojo; Sunarta, Sigit

    2018-01-01

    Essential oils obtained from Eucalyptus posses many bioactivities as fungicidal, antimicrobial, insecticidal and other activities. This study elucidated chemical compounds and antifungal activity of Eucalyptus urophylla leaves oil. Effectiveness of E. urophylla leaves oil were evaluated as antifungal against pathogenic fungi of A. Niger and F. oxysporum. Eucalyptus urophylla oil was obtained by hydrodistillation method from fresh leaves of E. urophylla. Gas chromatography-mass spectrometry (G...

  11. An on-line post-column detection system for the detection of reactive-oxygen-species-producing compounds and antioxidants in mixtures

    Science.gov (United States)

    Kool, Jeroen; Van Liempd, Sebastiaan M.; Harmsen, Stefan; Schenk, Tim; Irth, Hubertus; Commandeur, Jan N. M.

    2007-01-01

    Reactive oxygen species (ROS) can damage proteins, cause lipid peroxidation, and react with DNA, ultimately resulting in harmful effects. Antioxidants constitute one of the defense systems used to neutralize pro-oxidants. Since pro-oxidants and antioxidants are found ubiquitously in nature, pro-and antioxidant effects of individual compounds and of mixtures receive much attention in scientific research. A major bottleneck in these studies, however, is the identification of the individual pro-oxidants and antioxidants in mixtures. Here, we describe the development and validation of an on-line post-column biochemical detection system for ROS-producing compounds and antioxidants in mixtures. Inclusion of cytochrome P450s and cytochrome P450 reductase also permitted the screening of compounds that need bioactivation to exert their ROS-producing properties. This pro-oxidant and antioxidant detection system was integrated on-line with gradient HPLC. The resulting high-resolution screening technology was able to separate mixtures of ROS-producing compounds and antioxidants, allowing each species to be characterized rapidly and sensitively. PMID:17468853

  12. Slowly biodegradable organic compounds impact the biostability of non-chlorinated drinking water produced from surface water.

    Science.gov (United States)

    Hijnen, W A M; Schurer, R; Bahlman, J A; Ketelaars, H A M; Italiaander, R; van der Wal, A; van der Wielen, P W J J

    2018-02-01

    It is possible to distribute drinking water without a disinfectant residual when the treated water is biologically stable. The objective of this study was to determine the impact of easily and slowly biodegradable compounds on the biostability of the drinking water at three full-scale production plants which use the same surface water, and on the regrowth conditions in the related distribution systems. Easily biodegradable compounds in the drinking water were determined with AOC-P17/Nox during 2012-2015. Slowly biodegradable organic compounds measured as particulate and/or high-molecular organic carbon (PHMOC), were monitored at the inlet and after the different treatment stages of the three treatments during the same period. The results show that PHMOC (300-470 μg C L -1 ) was approximately 10% of the TOC in the surface water and was removed to 50-100 μg C L -1 . The PHMOC in the water consisted of 40-60% of carbohydrates and 10% of proteins. A significant and strong positive correlation was observed for PHMOC concentrations and two recently introduced bioassay methods for slowly biodegradable compounds (AOC-A3 and biomass production potential, BPC 14 ). Moreover, these three parameters in the biological active carbon effluent (BACF) of the three plants showed a positive correlation with regrowth in the drinking water distribution system, which was assessed with Aeromonas, heterotrophic plate counts, coliforms and large invertebrates. In contrast, the AOC-P17/Nox concentrations did not correlate with these regrowth parameters. We therefore conclude that slowly biodegradable compounds in the treated water from these treatment plants seem to have a greater impact on regrowth in the distribution system than easily biodegradable compounds. Copyright © 2017 Elsevier Ltd. All rights reserved.

  13. Penetratin and derivatives acting as antifungal agents

    NARCIS (Netherlands)

    Masman, Marcelo F.; Rodriguez, Ana M.; Raimondi, Marcela; Zacchino, Susana A.; Luiten, Paul G. M.; Somlai, Csaba; Kortvelyesi, Tamas; Penke, Botond; Enriz, Ricardo D.

    The synthesis, in vitro evaluation, and conformational study of RQIKTWFQNRRMKWKK-NH(2) (penetratin) and related derivatives acting as antifungal agents are reported. Penetratin and some of its derivatives displayed antifungal activity against the human opportunistic pathogenic standardized ATCC

  14. SHORT COMMUNICATION EVALUATION OF ANTIFUNGAL AND ...

    African Journals Online (AJOL)

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    Pakistan) and chloramphenicol from Sigma St. Louis. (USA) was used as standard. Antifungal activity of monoesters. The antifungal activities of the monoesters (1-29) were determined by employing hanging drop method considering ketoconazole ...

  15. Oxylipin studies expose aspirin as antifungal.

    Science.gov (United States)

    Kock, Johan L F; Sebolai, Olihile M; Pohl, Carolina H; van Wyk, Pieter W J; Lodolo, Elizabeth J

    2007-12-01

    The presence of aspirin-sensitive 3-hydroxy fatty acids (i.e. 3-OH oxylipins) in yeasts was first reported in the early 1990s. Since then, these oxidized fatty acids have been found to be widely distributed in yeasts. 3-OH oxylipins may: (1) have potent biological activity in mammalian cells; (2) act as antifungals; and (3) assist during forced spore release from enclosed sexual cells (asci). A link between 3-OH oxylipin production, mitochondria and aspirin sensitivity exists. Research suggests that: (1) 3-OH oxylipins in some yeasts are probably also produced by mitochondria through incomplete beta-oxidation; (2) aspirin inhibits mitochondrial beta-oxidation and 3-OH oxylipin production; (3) yeast sexual stages, which are probably more dependent on mitochondrial activity, are also characterized by higher 3-OH oxylipin levels as compared to asexual stages; (4) yeast sexual developmental stages as well as cell adherence/flocculation are more sensitive to aspirin than corresponding asexual growth stages; and (5) mitochondrion-dependent asexual yeast cells with a strict aerobic metabolism are more sensitive to aspirin than those that can also produce energy through an alternative anaerobic glycolytic fermentative pathway in which mitochondria are not involved. This review interprets a wide network of studies that reveal aspirin to be a novel antifungal.

  16. Candidiasis and the impact of flow cytometry on antifungal drug discovery.

    Science.gov (United States)

    Ku, Tsun Sheng N; Bernardo, Stella; Walraven, Carla J; Lee, Samuel A

    2017-11-01

    Invasive candidiasis continues to be associated with significant morbidity and mortality as well as substantial health care costs nationally and globally. One of the contributing factors is the development of resistance to antifungal agents that are already in clinical use. Moreover, there are known treatment limitations with all of the available antifungal agents. Since traditional techniques in novel drug discovery are time consuming, high-throughput screening using flow cytometry presents as a potential tool to identify new antifungal agents that would be useful in the management of these patients. Areas covered: In this review, the authors discuss the use of automated high-throughput screening assays based upon flow cytometry to identify potential antifungals from a library comprised of a large number of bioactive compounds. They also review studies that employed the use of this research methodology that has identified compounds with antifungal activity. Expert opinion: High-throughput screening using flow cytometry has substantially decreased the processing time necessary for screening thousands of compounds, and has helped enhance our understanding of fungal pathogenesis. Indeed, the authors see this technology as a powerful tool to help scientists identify new antifungal agents that can be added to the clinician's arsenal in their fight against invasive candidiasis.

  17. Acylated Flavone Glycosides from the Roots of Saussurea lappa and Their Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Yemireddy Venkata Ramnareddy

    2007-03-01

    Full Text Available The isolation of four novel acylated flavonoid glycosides from the roots of Saussurea lappa and their identification using a combination of 1D and 2D NMR and mass spectrometry is described. The in vitro antifungal and antibacterial activities of the isolated compounds and their mixture were tested on nine fungal and four bacterial strains, using the microdilution method. The compounds and mixture showed moderate to high antifungal activity against most of the fungi tested, compared to a miconazole standard, while only one compound and the mixture showed antibacterial activity against all strains tested.

  18. Synthesis, Anti-Bacterial and Anti-Fungal Evaluation of Pyrazoline Derivatives

    Directory of Open Access Journals (Sweden)

    Ashvin D. Panchal

    2012-01-01

    Full Text Available The Series of N-(5-(Substituted phenyl-4,5-dihydro-1H-pyrazol-3-yl-4H-1,2,4-triazol-4-amine compounds were prepared by reaction of 4-amino-1,2,4-Triazole with Acetyl Chloride followed by different aromatic aldehydes and cyclization with hydrazine hydrate. The structures of new compounds were confirmed by IR and 1H-NMR spectral data. Anti-bacterial and Anti-fungal activities were evaluated and compared with the standard drugs, some compounds of the series exhibited promising anti-microbial and anti-fungal activity compared to standard drugs.

  19. Prediction of bioactive compounds activity against wood contaminant fungi using artificial neural networks

    OpenAIRE

    Vicente, Henrique; Roseiro, José C.; Arteiro, José M.; Neves, José; Caldeira, A. Teresa

    2013-01-01

    Biopesticides based on natural endophytic bacteria to control plant diseases are an ecological alternative to the chemical treatments. Bacillus species produce a wide variety of metabolites with biological activity like iturinic lipopeptides. This work addresses the production of biopesticides based on natural endophytic bacteria, isolated from Quercus suber. Artificial Neural Networks were used to maximize the percentage of inhibition triggered by antifungal activity of bioactive compounds p...

  20. In vitro and in vivo activity of a novel antifungal small molecule against Candida infections.

    Directory of Open Access Journals (Sweden)

    Sarah Sze Wah Wong

    Full Text Available Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistant Candida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity against Candida spp. both in vitro and in vivo. We screened a library of 50,240 small molecules for inhibitors of yeast-to-hypha transition, a major virulence attribute of Candida albicans. This screening identified 20 active compounds. Further examination of the in vitro antifungal and anti-biofilm properties of these compounds, using a range of Candida spp., led to the discovery of SM21, a highly potent antifungal molecule (minimum inhibitory concentration (MIC 0.2-1.6 µg/ml. In vitro, SM21 was toxic to fungi but not to various human cell lines or bacterial species and was active against Candida isolates that are resistant to existing antifungal agents. Moreover, SM21 was relatively more effective against biofilms of Candida spp. than the current antifungal agents. In vivo, SM21 prevented the death of mice in a systemic candidiasis model and was also more effective than the common antifungal nystatin at reducing the extent of tongue lesions in a mouse model of oral candidiasis. Propidium iodide uptake assay showed that SM21 affected the integrity of the cell membrane. Taken together, our results indicate that SM21 has the potential to be developed as a novel antifungal agent for clinical use.

  1. 75 FR 79320 - Animal Drugs, Feeds, and Related Products; Regulation of Carcinogenic Compounds in Food-Producing...

    Science.gov (United States)

    2010-12-20

    ... is calculated from tumor data of the cancer bioassays using a statistical extrapolation procedure... the presence of the marker residue of the sponsored compound in the target tissue of the target animal... detectable (that is, the marker residue is below the limit of detection) using the approved regulatory...

  2. Slowly biodegradable organic compounds impact the biostability of non-chlorinated drinking water produced from surface water

    NARCIS (Netherlands)

    Hijnen, W.A.M.; Schurer, R.; Bahlman, J.A.; Ketelaars, H.A.M.; Italiaander, R.; Wal, van der A.; Wielen, van der P.W.J.J.

    2018-01-01

    It is possible to distribute drinking water without a disinfectant residual when the treated water is biologically stable. The objective of this study was to determine the impact of easily and slowly biodegradable compounds on the biostability of the drinking water at three full-scale production

  3. Evaluation of phenolic compounds content and in vitro antioxidant activity of red wines produced from Vitis labrusca grapes

    Directory of Open Access Journals (Sweden)

    Daniel Braga de Lima

    2011-09-01

    Full Text Available Wine production in the northern Curitiba, Paraná, Brazil, specifically the communes of Colombo and Almirante Tamandaré, is based mainly on the utilization of Vitis labrusca grapes var. Bordô (Ives. Total sugar content, pH, and total acidity were analyzed in red wine samples from 2007 and 2008 vintages following official methods of analysis. Moreover, total phenolic, flavonoid, and tannin contents were analyzed by colorimetric methodologies and the antioxidant activity was determined using the 2,2-diphenyl-1-picrylhydrazyl (DPPH radical methodology. Phenolic compounds were identified by high performance liquid chromatography. The total phenolic content of wine samples presented concentrations varying between 1582.35 and 2896.08 mg gallic acid.L-1 since the major part corresponds to flavonoid content. In these compounds' concentration range, a direct relationship between phenolic compounds content and levels of antioxidant activity was not observed. Among the identified phenolic compounds, chlorogenic, caffeic, and syringic acids were found to be the major components. Using three principal components, it was possible to explain 81.36% of total variance of the studied samples. Principal Components Analysis does not differentiate between vintages.

  4. Contribution of phenolic compounds to food flavors: Strecker-type degradation of amines and amino acids produced by o- and p-diphenols.

    Science.gov (United States)

    Delgado, Rosa M; Zamora, Rosario; Hidalgo, Francisco J

    2015-01-14

    The ability of 20 phenolic derivatives to produce the Strecker-type degradation of phenylalanine and phenylglycine methyl ester was studied to investigate both the direct degradation of amino acids and amines by phenolic compounds in the absence of added oxidants and the effect of the number and positions of hydroxyl groups in the aromatic ring of the phenolic compound in relation to its ability to produce carbonyl derivatives from amino compounds. The obtained results showed that polyphenols can produce the Strecker degradation of amino acids and amines in the absence of added oxidants. The only requisite for producing the reaction is the presence of two hydroxyl groups in ortho or para positions. However, the presence of two hydroxyl groups in meta position in an additional aromatic ring can inhibit the Strecker-degrading ability of the hydroxyl groups in ortho or para positions. A reaction pathway that explains all of these findings is proposed. In addition, the effect of reaction conditions on the obtained reaction yields was studied. Activation energies (Ea) for phenylacetaldehyde formation from phenylalanine in the presence of hydroquinone, 1,2,4-trihydroxybenzene, and benzoquinone were 32.9, 31.5, and 28.8 kJ/mol, respectively.

  5. Conformational restriction of aryl thiosemicarbazones produces potent and selective anti-Trypanosoma cruzi compounds which induce apoptotic parasite death.

    Science.gov (United States)

    Magalhaes Moreira, Diogo Rodrigo; de Oliveira, Ana Daura Travassos; Teixeira de Moraes Gomes, Paulo André; de Simone, Carlos Alberto; Villela, Filipe Silva; Ferreira, Rafaela Salgado; da Silva, Aline Caroline; dos Santos, Thiago André Ramos; Brelaz de Castro, Maria Carolina Accioly; Pereira, Valéria Rego Alves; Leite, Ana Cristina Lima

    2014-03-21

    Chagas disease, caused by Trypanosoma cruzi, is a life-threatening infection leading to approximately 12,000 deaths per year. T. cruzi is susceptible to thiosemicarbazones, making this class of compounds appealing for drug development. Previously, the homologation of aryl thiosemicarbazones resulted in an increase in anti-T. cruzi activity in comparison to aryl thiosemicarbazones without a spacer group. Here, we report the structural planning, synthesis and anti-T. cruzi evaluation of new aryl thiosemicarbazones (9a-x), designed as more conformationally restricted compounds. By varying substituents attached to the phenyl ring, substituents were observed to retain, enhance or greatly increase the anti-T. cruzi activity, in comparison to the nonsubstituted derivative. In most cases, hydrophobic and bulky substituents, such as bromo, biphenyl and phenoxyl groups, greatly increased antiparasitic activity. Specifically, thiosemicarbazones were identified that inhibit the epimastigote proliferation and were toxic for trypomastigotes without affecting mouse splenocytes viability. The most potent anti-T. cruzi thiosemicarbazones were evaluated against cruzain. However, inhibition of this enzyme was not observed, suggesting that the compounds work through another mechanism. In addition, examination of T. cruzi cell death showed that these thiosemicarbazones induce apoptosis. In conclusion, the structural design executed within the series of aryl thiosemicarbazones (9a-x) led to the identification of new potent anti-T. cruzi agents, such as compounds (9h) and (9r), which greatly inhibited epimastigote proliferation, and demonstrated a toxicity for trypomastigotes, but not for splenocytes. Mechanistically, these compounds do not inhibit the cruzain, but induce T. cruzi cell death by an apoptotic process. Copyright © 2014 Elsevier Masson SAS. All rights reserved.

  6. Correlations and adsorption mechanisms of aromatic compounds on biochars produced from various biomass at 700 °C.

    Science.gov (United States)

    Yang, Kun; Jiang, Yuan; Yang, Jingjing; Lin, Daohui

    2018-02-01

    Knowledge of adsorption behavior of organic contaminants on high heat temperature treated biochars is essential for application of biochars as adsorbents in wastewater treatment and soil remediation. In this study, isotherms of 25 aromatic compounds adsorption on biochars pyrolyzed at 700 °C from biomass including wood chips, rice straw, bamboo chips, cellulose, lignin and chitin were investigated to establish correlations between adsorption behavior and physicochemical properties of biochars. Isotherms were well fitted by Polanyi theory-based Dubinin-Ashtakhov (DA) model with three parameters, i.e., adsorption capacity (Q 0 ) and adsorption affinity (E and b). Besides the negative correlation of Q 0 with molecular maximum cross-sectional areas (σ) of organic compounds, positive correlations of Q 0 with total pore volume (V total ) and average diameter of micropore (D) of biochars were observed, indicating that adsorption by biochars is captured by the pore-filling mechanism with molecular sieving effect in biochar pores. Linear solvation energy relationships (LSERs) of adsorption affinity (E) with solvatochromic parameters of organic compounds (i. e., α m and π ∗ ) were established, suggesting that hydrophobic effect, π-π interaction and hydrogen-bonding interaction are the main forces responsible for adsorption. The regression coefficient (π 1 ) and intercept (C) of obtained LSERs are correlated with biochar H/C and R micro , respectively, implying that biochars with higher aromaticity and more micropores have stronger π-π bonding potential and hydrophobic effect potential with aromatic molecule, respectively. However, hydrogen-bonding potential of biochars for organic molecules is not changed significantly with properties of biochars. A negative correlation of b with biochar H/C is also obtained. These correlations could be used to predict the adsorption behavior of organic compounds on high heat temperature treated biochars from various biomass for

  7. Contribution of phlA and some metabolites of fluorescent pseudomonads to antifungal activity.

    Science.gov (United States)

    Afsharmanesh, H; Ahmadzadeh, M; Sharifi-Tehrani, A; Javan-Nikkhah, M; Ghazanfari, K

    2005-01-01

    Fluorescent Pseudomonas species are an important group of PGPR that suppress fungal root and seedling disease by production of antifungal metabolites such as 2,4-diacetylphloroglucinol (2,4-DAPG), pyoluteorin, pyrolinitrin, siderophores and HCN. The compound 2,4-DAPG is a major determinant in biocontrol of plant pathogens. A 7.2 kbp chromosomal DNA region, carrying DAPG biosynthetic genes (phlA, phlC, phlB, phlD, phIE and phlF). Detecting the ph1 genes make them an ideal marker gene for 2,4-DAPG-producing fluorescent pseudomonad's. In this study we detected ph1A gene (that convert MAPG to 2,4-DAPG) using PCR assay with primers phlA-1r and phlA- f that enabled amplification of phlA sequences from fluorescent pseudomonad's from ARDRA group 1 and 3. We could detect phlA gene in P. fluorescens strains CHAO, Pf-44, Pf-1, Pf-2, Pf-3, Pf-17, Pf-62 and Pf-64, native isolates of Iran. The efficacy of this method for rapid assay characterizing rhizosphere population of 2,4-DAPG producing bacteria from soil of different area of Iran is in progress. We used a collection of 48 fluorescent pseudomonas strains in vitro, with known biological control activity against some soil born phytopathogenic fungi such as, Macrophomina phaseoli, Rhizoctonia solani Vericillium dahlia, Phytophthora nicotiana, Pythium spp. and Fusarium spp. and the potential to produce known secondary metabolites such as protease. Strains Pf-1, Pf-2, Pf-3, Pf-17, Pf-33 and Pf-44 showed the best antifungal activity against all fungi used in this study. Thirty-eight of 48 strains produced protease. The ability to rapidly characterize populations of 2,4-DAPG producers will greatly enhance our understanding of their role in the suppression of root disease.

  8. Microwave-Assisted Synthesis and Antifungal Activity of Some Novel Thioethers Containing 1,2,4-Triazole Moiety

    Directory of Open Access Journals (Sweden)

    Li-Jing Min

    2015-11-01

    Full Text Available A series of novel thioether derivatives containing 1,2,4-triazole moiety were designed and synthesized from 4-chlorophenol and ethyl 2-chloroacetate as starting materials by multi-step reactions under microwave irradiation, and their structures were characterized by 1H-NMR, MS and elemental analysis. The antifungal activity of title compounds was determined. The results indicated that some of title compounds exhibited moderate antifungal activity.

  9. Synthesis of 1H-1,2,3-triazoles and study of their antifungal and cytotoxicity activities.

    Science.gov (United States)

    da Silva, Iara F; Martins, Prisicila R C; da Silva, Emanuelly G; Ferreira, Sabrina B; Ferreira, Vitor F; da Costa, Karen Regina C; de Vasconcellos, Marne C; Lima, Emerson S; da Silva, Fernando de C

    2013-12-01

    We report herein the results of antifungal activity of fifteen 1,2,3-triazoles against Candida albicans, Candida krusei, Candida parapsilosis, Candida kefyr, Candida tropicalis, Candida dubliniensis, Tricophyton rubrum, Microporum canis and Aspergillus niger. All of the 1,2,3-triazoles were prepared from 1,3-dipolar cyclizations between aryl azides and alkynes catalyzed by Cu(I), and several of the compounds exhibited antifungal activity with low cytotoxicity. The results demonstrated the potential and importance of developing new 1,2,3-triazoles compounds with antifungal activity.

  10. Antifungal Activity of Brazilian Propolis Microparticles against Yeasts Isolated from Vulvovaginal Candidiasis

    Directory of Open Access Journals (Sweden)

    Kelen Fátima Dalben Dota

    2011-01-01

    Full Text Available Propolis, a resinous compound produced by Apis mellifera L. bees, is known to possess a variety of biological activities and is applied in the therapy of various infectious diseases. The aim of this study was to evaluate the in vitro antifungal activity of propolis ethanol extract (PE and propolis microparticles (PMs obtained from a sample of Brazilian propolis against clinical yeast isolates of importance in the vulvovaginal candidiasis (VVC. PE was used to prepare the microparticles. Yeast isolates (n=89, obtained from vaginal exudates of patients with VVC, were exposed to the PE and the PMs. Moreover, the main antifungal drugs used in the treatment of VVC (Fluconazole, Voriconazole, Itraconazole, Ketoconazole, Miconazole and Amphotericin B were also tested. Minimum inhibitory concentration (MIC was determined according to the standard broth microdilution method. Some Candida albicans isolates showed resistance or dose-dependent susceptibility for the azolic drugs and Amphotericin B. Non-C. albicans isolates showed more resistance and dose-dependent susceptibility for the azolic drugs than C. albicans. However, all of them were sensitive or dose-dependent susceptible for Amphotericin B. All yeasts were inhibited by PE and PMs, with small variation, independent of the species of yeast. The overall results provided important information for the potential application of PMs in the therapy of VVC and the possible prevention of the occurrence of new symptomatic episodes.

  11. Phenolic compounds, organic acids and antioxidant activity of grape juices produced in industrial scale by different processes of maceration.

    Science.gov (United States)

    Lima, Marcos dos Santos; da Conceição Prudêncio Dutra, Maria; Toaldo, Isabela Maia; Corrêa, Luiz Claudio; Pereira, Giuliano Elias; de Oliveira, Débora; Bordignon-Luiz, Marilde Terezinha; Ninow, Jorge Luiz

    2015-12-01

    The effect of maceration process on the profile of phenolic compounds, organic acids composition and antioxidant activity of grape juices from new varieties of Vitis labrusca L. obtained in industrial scale was investigated. The extraction process presented a high yield without pressing the grapes. The use of a commercial pectinase resulted in an increase on extraction yield and procyanidins B1 and B2 concentrations and a decrease on turbidity and concentration of catechins. The combination of 60 °C and 3.0 mL 100 kg(-1) of enzyme resulted in the highest extraction of phenolic compounds, reducing the content of acetic acid. The juices presented high antioxidant activity, related to the great concentration of malvidin, cyanidin, catechin and caffeic, cinnamic and gallic acids. Among the bioactive compounds, the juices presented high concentration of procyanidin B1, caffeic acid and trans-resveratrol, with higher levels compared to those reported in the literature. Copyright © 2015 Elsevier Ltd. All rights reserved.

  12. Separation, determination and antifungal activity test of the products from a new Bacillus amyloliquefaciens.

    Science.gov (United States)

    Wang, Tao; Wu, Mian-Bin; Chen, Zheng-Jie; Lin, Jian-Pin; Yang, Li-Rong

    2016-01-01

    A new Bacillus amyloliquefaciens named ZJU-2011 was discovered, and the culture supernatant showed a strong inhibitory effect against Candida albicans. In this study, a novel method was developed to purify the antifungal compounds in high purity. The obtained products were analysed by high performance liquid chromatography and proven to be of high purity. Mass spectrometry showed that the molecular weights of the two bioactive components were 270 and 288, respectively, and their structures were determined to be bacilysin and chlorotetaine by using (1)H and (13)C nuclear magnetic resonance spectroscopy. To the best of our knowledge, this is the first time that B. amyloliquefaciens has been reported to produce bacilysin and chlorotetaine simultaneously. The minimum inhibitory concentration of chlorotetaine against six common fungal pathogens were determined to be in the range of 1.8-7.8 μg/mL.

  13. Occurrence, production, and export of lipophilic compounds by hydrocarbonoclastic marine bacteria and their potential use to produce bulk chemicals from hydrocarbons.

    Science.gov (United States)

    Manilla-Pérez, Efraín; Lange, Alvin Brian; Hetzler, Stephan; Steinbüchel, Alexander

    2010-05-01

    Petroleum (or crude oil) is a complex mixture of hydrocarbons. Annually, millions of tons of crude petroleum oil enter the marine environment from either natural or anthropogenic sources. Hydrocarbon-degrading bacteria (HDB) are able to assimilate and metabolize hydrocarbons present in petroleum. Crude oil pollution constitutes a temporary condition of carbon excess coupled to a limited availability of nitrogen that prompts marine oil-degrading bacteria to accumulate storage compounds. Storage lipid compounds such as polyhydroxyalkanoates (PHAs), triacylglycerols (TAGs), or wax esters (WEs) constitute the main accumulated lipophilic substances by bacteria under such unbalanced growth conditions. The importance of these compounds as end-products or precursors to produce interesting biotechnologically relevant chemicals has already been recognized. In this review, we analyze the occurrence and accumulation of lipid storage in marine hydrocarbonoclastic bacteria. We further discuss briefly the production and export of lipophilic compounds by bacteria belonging to the Alcanivorax genus, which became a model strain of an unusual group of obligate hydrocarbonoclastic bacteria (OHCB) and discuss the possibility to produce neutral lipids using A. borkumensis SK2.

  14. Characterization of Compounds with Tumor–Cell Proliferation Inhibition Activity from Mushroom (Phellinus baumii Mycelia Produced by Solid-State Fermentation

    Directory of Open Access Journals (Sweden)

    Henan Zhang

    2017-04-01

    Full Text Available The inhibition of tumor-cell proliferationbyan organicsolvent extract from the solid-state fermentation of Phellinus baumii mycelia inoculated in rice medium was investigated in vitro. The active compounds inhibiting tumor-cell proliferation were characterized. Results revealed that all (petroleum ether, chloroform, ethyl acetate, and butanol fractions inhibited tumor-cell proliferation in a dose-dependent fashion. The ethyl acetate extract had the highest inhibitory effecton tumor-cell proliferation, and the butanol fraction had the lowest. Six compounds were isolated and purified from the ethyl acetate extract of P. baumii mycelia by the tandem application of silica-gel column chromatography (SGCC, high-speed countercurrent chromatography (HSCCC, and preparative HPLC. These compounds were identified by NMR and electrospray ionization-mass spectrometry (ESI-MS spectroscopic methods as ergosterol (RF1, ergosta-7,22-dien-3β-yl pentadecanoate (RF3, 3,4-dihydroxy benzaldehyde(RF6, inoscavinA (RF7, baicalein(RF10, and 24-ethylcholesta-5,22-dien-3β-ol (RF13. To further clarify the activity of these compounds, the cell-proliferation-inhibition tests of these compounds on various tumor cells were carried out and evaluatedin vitro. Results suggested that compounds RF6, RF7, and RF10 had potent inhibition effects on the proliferation of a series of tumor cell lines, including K562, L1210, SW620, HepG2, LNCaP, and MCF-7cells. These findings indicated that P. baumii mycelia produced by solid-state fermentation in rice canbe used to obtain active compounds with the ability to inhibittumor-cell proliferation.

  15. Characterization of Compounds with Tumor-Cell Proliferation Inhibition Activity from Mushroom (Phellinus baumii) Mycelia Produced by Solid-State Fermentation.

    Science.gov (United States)

    Zhang, Henan; Shao, Qian; Wang, Wenhan; Zhang, Jingsong; Zhang, Zhong; Liu, Yanfang; Yang, Yan

    2017-04-27

    The inhibition of tumor-cell proliferationbyan organicsolvent extract from the solid-state fermentation of Phellinus baumii mycelia inoculated in rice medium was investigated in vitro. The active compounds inhibiting tumor-cell proliferation were characterized. Results revealed that all (petroleum ether, chloroform, ethyl acetate, and butanol) fractions inhibited tumor-cell proliferation in a dose-dependent fashion. The ethyl acetate extract had the highest inhibitory effecton tumor-cell proliferation, and the butanol fraction had the lowest. Six compounds were isolated and purified from the ethyl acetate extract of P. baumii mycelia by the tandem application of silica-gel column chromatography (SGCC), high-speed countercurrent chromatography (HSCCC), and preparative HPLC. These compounds were identified by NMR and electrospray ionization-mass spectrometry (ESI-MS) spectroscopic methods as ergosterol (RF1), ergosta-7,22-dien-3β-yl pentadecanoate (RF3), 3,4-dihydroxy benzaldehyde(RF6), inoscavinA (RF7), baicalein(RF10), and 24-ethylcholesta-5,22-dien-3β-ol (RF13). To further clarify the activity of these compounds, the cell-proliferation-inhibition tests of these compounds on various tumor cells were carried out and evaluatedin vitro. Results suggested that compounds RF6, RF7, and RF10 had potent inhibition effects on the proliferation of a series of tumor cell lines, including K562, L1210, SW620, HepG2, LNCaP, and MCF-7cells. These findings indicated that P. baumii mycelia produced by solid-state fermentation in rice canbe used to obtain active compounds with the ability to inhibittumor-cell proliferation.

  16. Antifungal Treatment for Pityriasis Versicolor.

    Science.gov (United States)

    Gupta, Aditya K; Foley, Kelly A

    2015-03-12

    Pityriasis versicolor (PV), also known as tinea versicolor, is caused by Malassezia species. This condition is one of the most common superficial fungal infections worldwide, particularly in tropical climates. PV is difficult to cure and the chances for relapse or recurrent infections are high due to the presence of Malassezia in the normal skin flora. This review focuses on the clinical evidence supporting the efficacy of antifungal treatment for PV. A systematic review of literature from the PubMed database was conducted up to 30 September 2014. The search criteria were "(pityriasis versicolor OR tinea versicolor) AND treatment", with full text available and English language required. Topical antifungal medications are the first-line treatment for PV, including zinc pyrithione, ketoconazole, and terbinafine. In cases of severe or recalcitrant PV, the oral antifungal medications itraconazole and fluconazole may be more appropriate, with pramiconazole a possible future option. Oral terbinafine is not effective in treating PV and oral ketoconazole should no longer be prescribed. Maintenance, or prophylactic, therapy may be useful in preventing recurrent infection; however, at this time, there is limited research evaluating the efficacy of prophylactic antifungal treatment.

  17. Microbial biotransformation to obtain new antifungals

    Directory of Open Access Journals (Sweden)

    Luiz Fernando Bianchini

    2015-12-01

    Full Text Available Antifungal drugs belong to few chemical groups and such low diversity limits the therapeutic choices. The urgent need of innovative options has pushed researchers to search new bioactive molecules. Literature regarding the last 15 years reveals that different research groups have used different approaches to achieve such goal. However, the discovery of molecules with different mechanisms of action still demands considerable time and efforts. This review was conceived to present how Pharmaceutical Biotechnology might contribute to the discovery of molecules with antifungal properties by microbial biotransformation procedures. Authors present some aspects of (1 microbial biotransformation of herbal medicines and food; (2 possibility of major and minor molecular amendments in existing molecules by biocatalysis; (3 methodological improvements in processes involving whole cells and immobilized enzymes; (4 potential of endophytic fungi to produce antimicrobials by bioconversions; and (5 in silico research driving to the improvement of molecules. All these issues belong to a new conception of transformation procedures, so-called green chemistry, which aims the highest possible efficiency with reduced production of waste and the smallest environmental impact.

  18. Microbial Biotransformation to Obtain New Antifungals

    Science.gov (United States)

    Bianchini, Luiz F.; Arruda, Maria F. C.; Vieira, Sergio R.; Campelo, Patrícia M. S.; Grégio, Ana M. T.; Rosa, Edvaldo A. R.

    2015-01-01

    Antifungal drugs belong to few chemical groups and such low diversity limits the therapeutic choices. The urgent need of innovative options has pushed researchers to search new bioactive molecules. Literature regarding the last 15 years reveals that different research groups have used different approaches to achieve such goal. However, the discovery of molecules with different mechanisms of action still demands considerable time and efforts. This review was conceived to present how Pharmaceutical Biotechnology might contribute to the discovery of molecules with antifungal properties by microbial biotransformation procedures. Authors present some aspects of (1) microbial biotransformation of herbal medicines and food; (2) possibility of major and minor molecular amendments in existing molecules by biocatalysis; (3) methodological improvements in processes involving whole cells and immobilized enzymes; (4) potential of endophytic fungi to produce antimicrobials by bioconversions; and (5) in silico research driving to the improvement of molecules. All these issues belong to a new conception of transformation procedures, so-called “green chemistry,” which aims the highest possible efficiency with reduced production of waste and the smallest environmental impact. PMID:26733974

  19. Role of lone-pair electrons in producing minimum thermal conductivity in nitrogen-group chalcogenide compounds.

    Science.gov (United States)

    Skoug, Eric J; Morelli, Donald T

    2011-12-02

    Fully dense crystalline solids with extremely low lattice thermal conductivity (κ(L)) are of practical importance for applications including thermoelectric energy conversion and thermal barrier coatings. Here we show that lone-pair electrons can give rise to minimum κ(L) in chalcogenide compounds that contain a nominally trivalent group VA element. Electrostatic repulsion between the lone-pair electrons and neighboring chalcogen ions creates anharmonicity in the lattice, the strength of which is determined by the morphology of the lone-pair orbital and the coordination number of the group VA atom. © 2011 American Physical Society

  20. Bioprospecting Sponge-Associated Microbes for Antimicrobial Compounds.

    Science.gov (United States)

    Indraningrat, Anak Agung Gede; Smidt, Hauke; Sipkema, Detmer

    2016-05-02

    Sponges are the most prolific marine organisms with respect to their arsenal of bioactive compounds including antimicrobials. However, the majority of these substances are probably not produced by the sponge itself, but rather by bacteria or fungi that are associated with their host. This review for the first time provides a comprehensive overview of antimicrobial compounds that are known to be produced by sponge-associated microbes. We discuss the current state-of-the-art by grouping the bioactive compounds produced by sponge-associated microorganisms in four categories: antiviral, antibacterial, antifungal and antiprotozoal compounds. Based on in vitro activity tests, identified targets of potent antimicrobial substances derived from sponge-associated microbes include: human immunodeficiency virus 1 (HIV-1) (2-undecyl-4-quinolone, sorbicillactone A and chartarutine B); influenza A (H1N1) virus (truncateol M); nosocomial Gram positive bacteria (thiopeptide YM-266183, YM-266184, mayamycin and kocurin); Escherichia coli (sydonic acid), Chlamydia trachomatis (naphthacene glycoside SF2446A2); Plasmodium spp. (manzamine A and quinolone 1); Leishmania donovani (manzamine A and valinomycin); Trypanosoma brucei (valinomycin and staurosporine); Candida albicans and dermatophytic fungi (saadamycin, 5,7-dimethoxy-4-p-methoxylphenylcoumarin and YM-202204). Thirty-five bacterial and 12 fungal genera associated with sponges that produce antimicrobials were identified, with Streptomyces, Pseudovibrio, Bacillus, Aspergillus and Penicillium as the prominent producers of antimicrobial compounds. Furthemore culture-independent approaches to more comprehensively exploit the genetic richness of antimicrobial compound-producing pathways from sponge-associated bacteria are addressed.

  1. Bioprospecting Sponge-Associated Microbes for Antimicrobial Compounds

    Directory of Open Access Journals (Sweden)

    Anak Agung Gede Indraningrat

    2016-05-01

    Full Text Available Sponges are the most prolific marine organisms with respect to their arsenal of bioactive compounds including antimicrobials. However, the majority of these substances are probably not produced by the sponge itself, but rather by bacteria or fungi that are associated with their host. This review for the first time provides a comprehensive overview of antimicrobial compounds that are known to be produced by sponge-associated microbes. We discuss the current state-of-the-art by grouping the bioactive compounds produced by sponge-associated microorganisms in four categories: antiviral, antibacterial, antifungal and antiprotozoal compounds. Based on in vitro activity tests, identified targets of potent antimicrobial substances derived from sponge-associated microbes include: human immunodeficiency virus 1 (HIV-1 (2-undecyl-4-quinolone, sorbicillactone A and chartarutine B; influenza A (H1N1 virus (truncateol M; nosocomial Gram positive bacteria (thiopeptide YM-266183, YM-266184, mayamycin and kocurin; Escherichia coli (sydonic acid, Chlamydia trachomatis (naphthacene glycoside SF2446A2; Plasmodium spp. (manzamine A and quinolone 1; Leishmania donovani (manzamine A and valinomycin; Trypanosoma brucei (valinomycin and staurosporine; Candida albicans and dermatophytic fungi (saadamycin, 5,7-dimethoxy-4-p-methoxylphenylcoumarin and YM-202204. Thirty-five bacterial and 12 fungal genera associated with sponges that produce antimicrobials were identified, with Streptomyces, Pseudovibrio, Bacillus, Aspergillus and Penicillium as the prominent producers of antimicrobial compounds. Furthemore culture-independent approaches to more comprehensively exploit the genetic richness of antimicrobial compound-producing pathways from sponge-associated bacteria are addressed.

  2. Radiation application for upgrading of bioresources - Development of antifungal and/or nitrogen fixative microbes

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Ki Sung; Ko, Dong Kyu; Han, Gab Jin [Paichai University, Taejon (Korea)

    2000-04-01

    (1) In this study, the antifungal bacteria six strains were isolated from various environment located in Chung-cheong area, Korea. These isolates were identified the genera Bacillus sp, Pseudomonas sp. through morphological, physiological and biochemical analysis. Strains KL3362 and KL3397 were identified as Pseudomonas aurantiaca and Alcaligenes faecalis, respectively. Considering antifungal(AF) spectrum, strain KL3303, 3334, and 3341 show the broad range, KL3362 and KL3397 the narrow range of AF activity on a number of pathogenic fungi. Therefore, strains KL3341 and KL3362 were selected as the strong candidate of antifungal bacteria on every purpose and usage related with our research goal. (2) KL3341 producing-antifungal substances were consisted of five different kinds of low molecular weight polypeptides (3) Optimal conditions for the production of antifungal substances were analyzed under various environmental conditions. Growth rates were different according to carbon and nitrogen source, antifungal substance production yields were not different, however. Product of antifungal substances according t phosphate is proportional to the concentration. And productivity of antifungal substances was generally high in the range 30 {approx} 37 deg. C at pH 7. In case of adding vitamin B1 or lysine to medium, the antifungal activity was enhanced. (4) Mutants with enhanced antifungal activities were constructed by radiation of {gamma}-ray. (5) AF strains were screened and selected from this research can be used in the microbial biocides as well as multifunctional bio-controllers in order to remove plant pathogenic fungi and to clarify the polluted environment. Due to their excellent degradation capability for agricultural and/or organic substances, they also can be used to improve soil quality, to ferment compost and to clean up the environment. 35 refs., 17 figs., 15 tabs. (Author)

  3. Correlation between Plant Secondary Metabolites and Their Antifungal Mechanisms–A Review

    DEFF Research Database (Denmark)

    Freiesleben, Sara; Jäger, Anna

    2014-01-01

    The search for new antifungal drugs often involves secondary metabolites from plants because of their pharmacological activity against foreign pathogens. Among the modern drugs in use today about 40% are of natural origin. To distinguish the secondary metabolites they can be divided into groups b...... biosynthetic groups of secondary metabolites; the phenolic compounds and the nitrogen containing compounds. Despite this there are correlations between some of the subgroups and their antifungal mechanism of actions....... it is interesting to investigate a relation between the biosynthetic origin of the antifungal compound and it’s mode of action against fungi. This correlation could limit the search to those natural compounds, which only interferes with the target of interest. This review is based on a comprehensive literature...... the biosynthetic group of terpenes and their antifungal mechanisms of action, all of them exhibiting their antifungal action through cell membrane disruption, although some of the terpenes also seemed to work through mitochondrial dysfunction. A clear correlation has not been demonstrated between the two other...

  4. Fumigant antifungal activity of Myrtaceae essential oils and constituents from Leptospermum petersonii against three Aspergillus species.

    Science.gov (United States)

    Kim, Eunae; Park, Il-Kwon

    2012-09-03

    Commercial plant essential oils obtained from 11 Myrtaceae plant species were tested for their fumigant antifungal activity against Aspergillus ochraceus, A. flavus, and A. niger. Essential oils extracted from Leptospermum petersonii at air concentrations of 56 × 10(-3) mg/mL and 28 × 10(-3) mg/mL completely inhibited the growth of the three Aspergillus species. However, at an air concentration of 14 × 10(-3) mg/mL, inhibition rates of L. petersonii essential oils were reduced to 20.2% and 18.8% in the case of A. flavus and A. niger, respectively. The other Myrtaceae essential oils (56 × 10(-3) mg/mL) only weakly inhibited the fungi or had no detectable affect. Gas chromatography-mass spectrometry analysis identified 16 compounds in L. petersonii essential oil. The antifungal activity of the identified compounds was tested individually by using standard or synthesized compounds. Of these, neral and geranial inhibited growth by 100%, at an air concentration of 56 × 10(-3) mg/mL, whereas the activity of citronellol was somewhat lover (80%). The other compounds exhibited only moderate or weak antifungal activity. The antifungal activities of blends of constituents identified in L. petersonii oil indicated that neral and geranial were the major contributors to the fumigant and antifungal activities.

  5. Antifungal and antioxidant activity of fatty acid methyl esters from vegetable oils

    Directory of Open Access Journals (Sweden)

    MARIA E.A. PINTO

    2017-08-01

    Full Text Available ABSTRACT Fatty acid methyl esters (FAMEs were obtained from vegetable oils of soybean, corn and sunflower. The current study was focused on evaluating the antifungal activity of FAMEs mainly against Paracoccidioides spp., as well as testing the interaction of these compounds with commercial antifungal drugs and also their antioxidant potential. FAMEs presented small IC50 values (1.86-9.42 μg/mL. All three FAMEs tested showed antifungal activity against isolates of Paracoccidioides spp. with MIC values ranging from 15.6-500 µg/mL. Sunflower FAMEs exhibited antifungal activity that extended also to other genera, with an MIC of 15.6 μg/mL against Candida glabrata and C. krusei and 31.2 μg/mL against C. parapsilosis. FAMEs exhibited a synergetic effect with itraconazole. The antifungal activity of the FAMEs against isolates of Paracoccidioides spp. is likely due to the presence of methyl linoleate, the major compound present in all three FAMEs. The results obtained indicate the potential of FAMEs as sources for antifungal and antioxidant activity.

  6. Method to produce biomass-derived compounds using a co-solvent system containing gamma-valerolactone

    Science.gov (United States)

    Dumesic, James A.; Motagamwala, Ali Hussain

    2017-06-27

    A method to produce an aqueous solution of carbohydrates containing C5- and/or C6-sugar-containing oligomers and/or C5- and/or C6-sugar monomers in which biomass or a biomass-derived reactant is reacted with a solvent system having an organic solvent, and organic co-solvent, and water, in the presence of an acid. The method produces the desired product, while a substantial portion of any lignin present in the reactant appears as a precipitate in the product mixture.

  7. Synthesis, In Vitro Biological Evaluation, and Molecular Docking of New Triazoles as Potent Antifungal Agents.

    Science.gov (United States)

    Li, Xiang; Liu, Chao; Tang, Sheng; Wu, Qiuye; Hu, Honggang; Zhao, Qingjie; Zou, Yan

    2016-01-01

    Based on the structure of the active site of CYP51 and the structure-activity relationships of azole antifungal compounds that we designed in a previous study, a series of 1-{1-[2-(substitutedbenzyloxy)ethyl]-1H-1,2,3-triazol-4-yl}-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ols (6a-n) were designed and synthesized utilizing copper-catalyzed azide-alkyne cycloaddition. Preliminary antifungal tests against eight human pathogenic fungi in vitro showed that all the title compounds exhibited excellent antifungal activities with a broad spectrum in vitro. Molecular docking results indicated that the interaction between the title compounds and CYP51 comprised π-π interactions, hydrophobic interactions, and the narrow hydrophobic cleft. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

  8. Antifungal activity of fabrics knitted by metalized Silver/Polyester composite yarn

    Science.gov (United States)

    Özkan, İ.; Duru Baykal, P.

    2017-10-01

    In this study, antifungal properties of fabric knitted from metalized silver/polyester composite yarn were investigated. Intermingling is an alternative technique for yarn blending process. Yarns having different features can be combined by feeding the same intermingling jet. This process is defined as commingling. In the study, intermingling process was used to produce metalized silver/polyester composite yarn. Commingled yarns were knitted to single jersey fabrics by IPM brand sample type circular knitting machine. Antifungal activity test was applied to samples against Aspergillus Niger according to AATCC 30 test procedure. It has been identified that the application provides antifungal activity to fabric.

  9. 77 FR 50591 - Animal Drugs, Feeds, and Related Products; Regulation of Carcinogenic Compounds in Food-Producing...

    Science.gov (United States)

    2012-08-22

    ... corresponding to no significant increase in the risk of cancer to the human consumer. However, the definition of... used in food- producing animals. Specifically, the Agency is clarifying the definition of ``S o '' and revising the definition of ``S m '' so that it conforms to the clarified definition of S o . Other...

  10. Synthesis and Antifungal Evaluation of 1-Aryl-2-dimethyl-aminomethyl-2-propen-1-one Hydrochlorides

    Directory of Open Access Journals (Sweden)

    Mehmet Emin Topaloglu

    2011-06-01

    Full Text Available The development of resistance to current antifungal therapeutics drives the search for new effective agents. The fact that several acetophenone-derived Mannich bases had shown remarkable antifungal activities in our previous studies led us to design and synthesize some acetophenone-derived Mannich bases, 1-8 and 2-acetylthiophene-derived Mannich base 9, 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochloride, to evaluate their antifungal activities. The designed chemical structures have α,β-unsaturated ketone moieties, which are responsible for the bioactivities of the Mannich bases. The aryl part was C6H5 (1; 4-CH3C6H4 (2; 4-CH3OC6H4 (3; 4-ClC6H4 (4; 4-FC6H4 (5; 4-BrC6H4 (6; 4-HOC6H4 (7; 4-NO2C6H4 (8; and C4H3S(2-yl (9. In this study the designed compounds were synthesized by the conventional heating method and also by the microwave irradiation method to compare these methods in terms of reaction times and yields to find an optimum synthetic method, which can be applied for the synthesis of Mannich bases in further studies. Since there are limited number of studies reporting the synthesis of Mannich bases by microwave irradiation, this study may also contribute to the general literature on Mannich bases. Compound 7 was reported for the first time. Antifungal activities of all compounds and synthesis of the compounds by microwave irradiation were also reported for the first time by this study. Fungi (15 species were used for antifungal activity test. Amphotericin B was tested as an antifungal reference compound. In conclusion, compounds 1-6, and 9, which had more potent (2–16 times antifungal activity than the reference compound amphotericin B against some fungi, can be model compounds for further studies to develop new antifungal agents. In addition, microwave irradiation can be considered to reduce reaction period, while the conventional method can still be considered to obtain compounds with higher reaction yields in the synthesis of

  11. Identification and growth optimization of a Marine Bacillus DK1-SA11 having potential of producing broad spectrum antimicrobial compounds.

    Science.gov (United States)

    Khan, Muhammad Naseem; Lin, Hong; Li, Meng; Wang, Jingxue; Mirani, Zulfiqar Ali; Khan, Seema Ismat; Buzdar, Muhammad Aslam; Ali, Imran; Jamil, Khalid

    2017-05-01

    Control of harmful bacteria in food, aquaculture, pharmaceuticals, agriculture, hospitals and recreation water pools are of great global concern. Marine bacteria are an enormous source of bio-controlling agents. The aim of this study was to identify and optimize the growth conditions including effect of different biotic and abiotic factors on antimicrobial activity of strain DK1-SA11 isolated from Qingdao Bay of China Yellow Sea. Microscopic characterization, API® 20E and 50 CHB kit base carbohydrates utilization, 16S rDNA and DNA gyrB gene sequencing studies identified the bacterium as Bacillus subtilis subsp. spizizenii DK1-SA11. Antimicrobial spectrum of cell free supernatant (CFS) has shown antimicrobial activities against all test strains including methicillin-resistant Staphylococcus aureus, E. coli O157:H7, Candida albicans, Klebsiella pneumoniae, Listeria monocytogenes, Vibrio parahaemolyticus, E. coli, Pseudomonas fluorescens, Salmonella typhimurium and Vibrio cholerae. Among all the media tested, Marine Broth 2216 was found to be the best medium for bacterial growth and production of antibacterial compounds. The other optimum conditions for growth were pH:7 and incubation temperature: 25°C with < 180 rpm for 60-72 h. Out of 49 different carbohydrates tested, D-mannose increases the antibacterial activity by 33.3% while D-arabitol decreases it by 44.4%. Crude CFS showed activity even after three months of storage below -20°C and boiling for 10 min, whereas it loses 100% of its antimicrobial activity after enzymatic treatments of lipase, trypsin and papain. The production of antimicrobial compounds and broad spectrum of antimicrobial activity against all tested pathogens suggested that the strain DK1-SA11 can be used as a source for probiotics, synbiotics and antibiotics.

  12. Natural and anthropogenically-produced brominated compounds in endemic dolphins from Western South Atlantic: Another risk to a vulnerable species

    International Nuclear Information System (INIS)

    Alonso, Mariana B.; Eljarrat, Ethel; Gorga, Marina; Secchi, Eduardo R.; Bassoi, Manuela; Barbosa, Lupércio; Bertozzi, Carolina P.; Marigo, Juliana; Cremer, Marta; Domit, Camila; Azevedo, Alexandre F.; Dorneles, Paulo R.; Torres, João Paulo M.

    2012-01-01

    Liver samples from 53 Franciscana dolphins along the Brazilian coast were analyzed for organobrominated compounds. Target substances included the following anthropogenic pollutants: polybrominated diphenyl ethers (PBDEs), polybrominated biphenyls (PBBs), pentabromoethylbenzene (PBEB), hexabromobenzene (HBB), decabromodiphenylethane (DBDPE), as well as the naturally-generated methoxylated-PBDEs (MeO-PBDEs). PBDE concentrations ranged from 6 to 1797 ng/g lw (mean 166 ± 298 ng/g lw) and were similar to those observed in cetaceans from Northern Hemisphere. PBBs were found in all sampling locations (< LOQ to 57 ng/g lw). DBDPE was detected in 42% of the dolphins from the most industrialized Brazilian state and the concentrations ranging from < LOQ to 352 ng/g lw. Franciscana dolphins from the tropical Brazilian shore presented the highest MeO-PBDE concentrations ever reported for coastal cetaceans (up to 14 μg/g lw). Eight MeO-PBDE congeners were detected and the present investigation constituted the first record of occurrence of six of them in marine mammal livers. - Highlights: ► PBDE, emerging BFR and MeO-PBDE levels in Franciscana dolphin from Brazil were reported. ► Six MeO-PBDEs were detected for the first time in marine mammals. ► PBDE contamination was similar than those from other industrialized areas around the world. ► MeO-PBDEs presented the higher concentrations found in coastal biota worldwide. - Concentrations and accumulation profiles of PBDEs, MeO-PBDEs and emerging brominated compounds in livers of dolphins from South Atlantic.

  13. Study on Mutagenic Breeding of Bacillus Subtilis and Properties of Its Antifungal Substances

    Science.gov (United States)

    Liu, Jing; Yao, Jianming

    2004-08-01

    Bacillus subtitles JA isolated by our laboratory produced a large amount of antifungal substances, which had strong inhibitory activity against various plant pathogenic fungi, such as Rhizoctonia solani, Fusarium graminearum and so on. Ion beam implantation as a new mutagenic methods was applied in our studay. After B. subtitles JA was implanted by N+ ions, a strain designated as B. subtitles JA-026 was screened and obtained, which had a higher ability to produce those antifungal substances. A series of experiments indicated that the antifungal substances were thermostable and partially sensitive to proteinases K and tryproteinase. When the fermentating broth was fractionated with ammonium sulphate of a final saturation of 70%, the precipitate-enhanced inhibitory activity while the supernatant lost this activity. It appeared that the antifungal substances were likely to be protein.

  14. Synthesis and DFT study on Hantzsch reaction to produce asymmetrical compounds of 1,4-dihydropyridine derivatives for P-glycoprotein inhibition as anticancer agent.

    Science.gov (United States)

    Mollazadeh, Shirin; Moosavi, Fatemeh; Hadizadeh, Farzin; Seifi, Mahmoud; Behravan, Javad; Iman, Maryam

    2018-02-19

    P-glycoprotein (P-gp) causes the efflux of cancer chemotherapy drugs from tumor cells, so it's inhibition can be one target for design and synthesis of new anticancer drugs. In this study new compounds of 1,4-dihydropyridine (DHP) were recommended as inhibitors of P-gp. We synthesized new symmetrical DHP with 36% - 43% yield by the reaction of new reactants. In biological studies, these compounds have high lipophilicity, and thus low water solubility. Four reactants I with different reactivity was computed and compared using DFT study. The LUMO-map was differently distributed on each reactant. Amine intermediate underwent tautomerism as atransition state and it seems to play important role in reaction progress. Calculations were performed to select suitable reactants. Two different reactants I, including one polar group and a non-polar group, were used to produce asymmetric compounds with 49%-60% yield. These asymmetric DHPs were more soluble than symmetric DHPs. In the final step another selected symmetric product (by elimination of chlorine atom) was synthesized with high yield (74%) with using DFT study. In this study, selected reactants by DFT calculation have increased yield of reaction from 36% to 74% without any catalyst. Diversity of products is noticeable topic. Racemic asymmetric compounds with R and S enantiomers have potential for enantiomeric separation. Each of these enantiomers could have different physiological effect. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  15. Fengycin produced by Bacillus subtilis 9407 plays a major role in the biocontrol of apple ring rot disease.

    Science.gov (United States)

    Fan, Haiyan; Ru, Jinjiang; Zhang, Yuanyuan; Wang, Qi; Li, Yan

    2017-06-01

    Apple ring rot, caused by Botryosphaeria dothidea, is a serious apple disease in China. Bacillus subtilis 9407 was isolated from healthy apples and showed strong antifungal activity against B. dothidea. To identify the primary antifungal compound of B. subtilis 9407 and determine its role in controlling apple ring rot, a transposon mutant library was constructed using TnYLB-1, and a mutant completely defective in antifungal activity was obtained. The gene inactivated in the antifungal activity mutant had 98.5% similarity to ppsB in B. subtilis subsp. subtilis str. 168, which encodes one of the five synthetases responsible for synthesizing fengycin. A markerless ppsB deletion mutant was constructed. Compared with the wild-type strain, lipopeptide crude extracts from ΔppsB showed almost no inhibition of B. dothidea mycelial growth. Furthermore, fengycin-like lipopeptides (retention factor 0.1-0.2) that exhibited antifungal activity against B. dothidea were observed in the wild-type strain by thin-layer chromatography (TLC)-bioautography analysis, but not in ΔppsB. Semipreparative reverse-phase high performance liquid chromatography (RP-HPLC) detection revealed that ΔppsB lost the ability to synthesize fengycin. These results suggest that ppsB is responsible for synthesizing fengycin and that fengycin is the major antifungal compound produced by B. subtilis 9407 against B. dothidea. Moreover, a biocontrol assay showed that the control efficacy of ΔppsB was reduced by half compared with the wild-type strain, indicating that fengycin plays a major role in controlling apple ring rot disease. This is the first report on the use of a B. subtilis strain as a potential biological control agent to control apple ring rot disease by the production of fengycin. Copyright © 2017 Elsevier GmbH. All rights reserved.

  16. Cultivation of entomopathogenic fungi for the search of antibacterial compounds.

    Science.gov (United States)

    Lee, Si-Young; Nakajima, Ikuo; Ihara, Fumio; Kinoshita, Hiroshi; Nihira, Takuya

    2005-11-01

    Entomopathogenic fungi are a rich source of natural bioactive compounds. To establish cultivation conditions which facilitate the production of bioactive compounds and to select good genera among entomopathogenic fungi as the producer, 47 typical entomopathogenic fungi were tested for their ability to produce antibiotic activity. Thirty-eight strains (81%) and 30 strains (64%) of these fungi produced either anti-Bacillus compounds or anti-Staphylococcus compounds, respectively, indicating that the majority of the entomopathogenic fungi tested possessed the ability to produce antibacterial compounds. Using 9 representative strains (Aschersonia sp. HF724, Beauveria bassiana HF338, Cordyceps ramosopulvinata HF746, Metarhizium anisopliae HF293, Metarhizium flavoviride HF698, Nomuraea rileyi HF588, Paecilomyces fumosoroseus HF254, Paecilomyces tenuipes HF419, and Verticillium lecanii HF238), the cultivation conditions in liquid medium were surveyed with respect to the cultivation procedure and medium composition, particularly in terms of the presence or absence of insect-derived materials. At 26 degrees C, M. anisopliae HF293, N. rileyi HF588, and V. lecanii HF238 strains produced clear antibiotic activity against Bacillus and Saccharomyces, but only in the presence of insect-derived materials, suggesting that the production of antibacterial/antifungal compounds by entomopathogenic fungi is triggered by the presence of insect-derived materials.

  17. Characterization of Antifungal Natural Products Isolated from Endophytic Fungi of Finger Millet (Eleusine coracana

    Directory of Open Access Journals (Sweden)

    Walaa Kamel Mousa

    2016-09-01

    Full Text Available Finger millet is an ancient African-Indian crop that is resistant to many pathogens including the fungus, Fusarium graminearum. We previously reported the first isolation of putative fungal endophytes from finger millet and showed that the crude extracts of four strains had anti-Fusarium activity. However, active compounds were isolated from only one strain. The objectives of this study were to confirm the endophytic lifestyle of the three remaining anti-Fusarium isolates, to identify the major underlying antifungal compounds, and to initially characterize the mode(s of action of each compound. Results of confocal microscopy and a plant disease assay were consistent with the three fungal strains behaving as endophytes. Using bio-assay guided fractionation and spectroscopic structural elucidation, three anti-Fusarium secondary metabolites were purified and characterized. These molecules were not previously reported to derive from fungi nor have antifungal activity. The purified antifungal compounds were: 5-hydroxy 2(3H-benzofuranone, dehydrocostus lactone (guaianolide sesquiterpene lactone, and harpagoside (an iridoide glycoside. Light microscopy and vitality staining were used to visualize the in vitro interactions between each compound and Fusarium; the results suggested a mixed fungicidal/fungistatic mode of action. We conclude that finger millet possesses fungal endophytes that can synthesize anti-fungal compounds not previously reported as bio-fungicides against F. graminearum.

  18. Isolation of chrysophanic acid-9-anthrone, the major antifungal principle of Cassia tora.

    Science.gov (United States)

    Acharya, T K; Chatterjee, I B

    1975-01-01

    An antifungal principle of defatted seed power of Cassia tora Linn. was isolated by extraction of an aqueous paste of the powder with benzene, followed by column chromatography over activated silica gel C using chloroform as the developing solvent. Besides chrysophanic acid and other hydroxyanthraquinone derivatives, the major antifungal compound was identified as chrysophanic acid-9-anthrone, the structure of which was assigned on the basis of its chemical properties and uv, ir, nmr and mass spectral analysis. The compound was active against Trichophyton rubrum, T. mentagrophytes, Microsporum canis, M. gypseum and Geotrichum candidum in broth in the presence of 100 mug/ml L-ascorbic acid as antioxidant.

  19. Melanins Protect Sporothrix brasiliensis and Sporothrix schenckii from the Antifungal Effects of Terbinafine

    OpenAIRE

    Almeida-Paes, Rodrigo; Figueiredo-Carvalho, Maria Helena Galdino; Brito-Santos, F?bio; Almeida-Silva, Fernando; Oliveira, Manoel Marques Evangelista; Zancop?-Oliveira, Rosely Maria

    2016-01-01

    Terbinafine is a recommended therapeutic alternative for patients with sporotrichosis who cannot use itraconazole due to drug interactions or side effects. Melanins are involved in resistance to antifungal drugs and Sporothrix species produce three different types of melanin. Therefore, in this study we evaluated whether Sporothrix melanins impact the efficacy of antifungal drugs. Minimal inhibitory concentrations (MIC) and minimal fungicidal concentrations (MFC) of two Sporothrix brasiliensi...

  20. Synthesis and in vitro antibacterial and antifungal activities of benzoxazole derivatives

    International Nuclear Information System (INIS)

    Khan, K.M.; Ambreen, N.; Ahmad, A.; Amyn, A.

    2013-01-01

    The in vitro antibacterial and antifungal activities of twenty-nine (29) benzoxazole derivatives were tested against fifteen Gram-positive and sixteen Gram-negative strains. Out of the twenty-nine compounds, eighteen compounds 3-5, 7-9, 11-13, 15-25 showed a broad range of activity against tested Gram-positive microorganisms, whereas rest of the compounds 6, 10, 14 and 26-31 were found to be completely inactive against all the tested strains of Gram-positive bacteria. Five compounds 8, 11-13, and 15 showed activities against Gram-negative strains whereas the rest were devoid of any activity. Twenty-one (21) out of twenty-nine (29) compounds possessed antifungal activity. The structures of the synthetic compounds were confirmed by IR, EIMS and /sup 1/H-NMR spectral data. (author)

  1. Inhibitors of amino acids biosynthesis as antifungal agents.

    Science.gov (United States)

    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.

  2. Accumulation of a bioactive benzoisochromanequinone compound kalafungin by a wild type antitumor-medermycin-producing streptomycete strain.

    Directory of Open Access Journals (Sweden)

    Jin Lü

    Full Text Available Medermycin and kalafungin, two antibacterial and antitumor antibiotics isolated from different streptomycetes, share an identical polyketide skeleton core. The present study reported the discovery of kalafungin in a medermycin-producing streptomycete strain for the first time. A mutant strain obtained through UV mutagenesis showed a 3-fold increase in the production of this antibiotic, compared to the wild type strain. Heterologous expression experiments suggested that its production was severely controlled by the gene cluster for medermycin biosynthesis. In all, these findings suggested that kalafungin and medermycin could be accumulated by the same streptomycete and share their biosynthetic pathway to some extent in this strain.

  3. Matrix assisted ionization: new aromatic and nonaromatic matrix compounds producing multiply charged lipid, peptide, and protein ions in the positive and negative mode observed directly from surfaces.

    Science.gov (United States)

    Li, Jing; Inutan, Ellen D; Wang, Beixi; Lietz, Christopher B; Green, Daniel R; Manly, Cory D; Richards, Alicia L; Marshall, Darrell D; Lingenfelter, Steven; Ren, Yue; Trimpin, Sarah

    2012-10-01

    Matrix assisted inlet ionization (MAII) is a method in which a matrix:analyte mixture produces mass spectra nearly identical to electrospray ionization without the application of a voltage or the use of a laser as is required in laserspray ionization (LSI), a subset of MAII. In MAII, the sample is introduced by, for example, tapping particles of dried matrix:analyte into the inlet of the mass spectrometer and, therefore, permits the study of conditions pertinent to the formation of multiply charged ions without the need of absorption at a laser wavelength. Crucial for the production of highly charged ions are desolvation conditions to remove matrix molecules from charged matrix:analyte clusters. Important factors affecting desolvation include heat, vacuum, collisions with gases and surfaces, and even radio frequency fields. Other parameters affecting multiply charged ion production is sample preparation, including pH and solvent composition. Here, findings from over 100 compounds found to produce multiply charged analyte ions using MAII with the inlet tube set at 450 °C are presented. Of the compounds tested, many have -OH or -NH(2) functionality, but several have neither (e.g., anthracene), nor aromaticity or conjugation. Binary matrices are shown to be applicable for LSI and solvent-free sample preparation can be applied to solubility restricted compounds, and matrix compounds too volatile to allow drying from common solvents. Our findings suggest that the physical properties of the matrix such as its morphology after evaporation of the solvent, its propensity to evaporate/sublime, and its acidity are more important than its structure and functional groups.

  4. Matrix Assisted Ionization: New Aromatic and Nonaromatic Matrix Compounds Producing Multiply Charged Lipid, Peptide, and Protein Ions in the Positive and Negative Mode Observed Directly from Surfaces

    Science.gov (United States)

    Li, Jing; Inutan, Ellen D.; Wang, Beixi; Lietz, Christopher B.; Green, Daniel R.; Manly, Cory D.; Richards, Alicia L.; Marshall, Darrell D.; Lingenfelter, Steven; Ren, Yue; Trimpin, Sarah

    2012-10-01

    Matrix assisted inlet ionization (MAII) is a method in which a matrix:analyte mixture produces mass spectra nearly identical to electrospray ionization without the application of a voltage or the use of a laser as is required in laserspray ionization (LSI), a subset of MAII. In MAII, the sample is introduced by, for example, tapping particles of dried matrix:analyte into the inlet of the mass spectrometer and, therefore, permits the study of conditions pertinent to the formation of multiply charged ions without the need of absorption at a laser wavelength. Crucial for the production of highly charged ions are desolvation conditions to remove matrix molecules from charged matrix:analyte clusters. Important factors affecting desolvation include heat, vacuum, collisions with gases and surfaces, and even radio frequency fields. Other parameters affecting multiply charged ion production is sample preparation, including pH and solvent composition. Here, findings from over 100 compounds found to produce multiply charged analyte ions using MAII with the inlet tube set at 450 °C are presented. Of the compounds tested, many have -OH or -NH2 functionality, but several have neither (e.g., anthracene), nor aromaticity or conjugation. Binary matrices are shown to be applicable for LSI and solvent-free sample preparation can be applied to solubility restricted compounds, and matrix compounds too volatile to allow drying from common solvents. Our findings suggest that the physical properties of the matrix such as its morphology after evaporation of the solvent, its propensity to evaporate/sublime, and its acidity are more important than its structure and functional groups.

  5. Synthesis and Antifungal Activities of 5-(o-Hydroxy phenyl-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole

    Directory of Open Access Journals (Sweden)

    Shiv K. Gupta

    2011-01-01

    Full Text Available New series of 5-(o-hydroxy phenyl-2-[4'aryl-3'chloro-2'azetidinon-1-yl]-1,3,4-thiadiazole have been synthesized and the structures of the new compounds were established on the basis of IR, 1H NMR spectral data. In vitro antifungal activity (MIC activity was evaluated and compared with standard drugs of ketoconazole. Compounds 3c in the series has shown interesting antifungal activity against both C. albicans and A. niger fungus. In the gratifying result, most of the compounds were found to have moderate antifungal activity.

  6. Investigations on the production of labelled organic compounds by recoil labelling with gamma,n-produced 11-C-atoms

    International Nuclear Information System (INIS)

    Wagenbach, U.

    1981-01-01

    ''Hot'' 11 C atoms are produced from 12 C(γ,n) 11 C nuclear reactions by bremsstrahlung at the 65 MeV electron linear accelerator in Giessen. The relative retention in various C-atoms of the amino acid, methionine, is determined by splitting of the terminal C-atoms of the molecule and by independent determination of the content of 11 C in the isolated and derived fragments. The terminal groups (thiomethyl or carboxyl groups) each carry approx. 25% of the total retained radioactivity, the remaining 50% being spread over the three inner carbon atoms. The activation of alkylamines, crystallised as hydrochlorides, hydrofluorides, oxalates and sulphates, leads to similar yields of direct labelling from 5 to 15%. Amines activated in the liquid state show a retention of less than 5%. The yields for labelled synthetic products are between 10 and 15% for amino acids and are often higher for crystallised amines. Amines activated in the liquid state produced greater yields of synthesis products but at the same time an increase in the product range. The labelled synthesis products can be separated faster by suitable methods such as preparative HPLC and are then available for carrier-free studies in the life sciences. (orig./EF) [de

  7. Perfluorinated Compounds in Greenhouse and Open Agricultural Producing Areas of Three Provinces of China: Levels, Sources and Risk Assessment.

    Science.gov (United States)

    Zhang, Yanwei; Tan, Dongfei; Geng, Yue; Wang, Lu; Peng, Yi; He, Zeying; Xu, Yaping; Liu, Xiaowei

    2016-12-10

    Field investigations on perfluoroalkyl acid (PFAA) levels in various environmental matrixes were reported, but there is still a lack of PFAA level data for agricultural environments, especially agricultural producing areas, so we collected soil, irrigation water and agricultural product samples from agricultural producing areas in the provinces of Liaoning, Shandong and Sichuan in China. The background pollution from instruments was removed and C₄-C 18 PFAAs were detected by LC-MS/MS. The concentrations of PFAAs in the top and deep layers of soil were compared, and the levels of PFAAs in different agricultural environments (greenhouses and open agriculture) were analyzed. We found the order of PFAA levels by province was Shandong > Liaoning > Sichuan. A descending trend of PFAA levels from top to deep soil and open to greenhouse agriculture was shown and perfluorobutanoic acid (PFBA) was considered as a marker for source analysis. Bean vegetables contribute highly to the overall PFAA load in vegetables. A significant correlation was shown between irrigation water and agricultural products. The EDI (estimated daily intake) from vegetables should be of concern in China.

  8. Perfluorinated Compounds in Greenhouse and Open Agricultural Producing Areas of Three Provinces of China: Levels, Sources and Risk Assessment

    Directory of Open Access Journals (Sweden)

    Yanwei Zhang

    2016-12-01

    Full Text Available Field investigations on perfluoroalkyl acid (PFAA levels in various environmental matrixes were reported, but there is still a lack of PFAA level data for agricultural environments, especially agricultural producing areas, so we collected soil, irrigation water and agricultural product samples from agricultural producing areas in the provinces of Liaoning, Shandong and Sichuan in China. The background pollution from instruments was removed and C4–C18 PFAAs were detected by LC-MS/MS. The concentrations of PFAAs in the top and deep layers of soil were compared, and the levels of PFAAs in different agricultural environments (greenhouses and open agriculture were analyzed. We found the order of PFAA levels by province was Shandong > Liaoning > Sichuan. A descending trend of PFAA levels from top to deep soil and open to greenhouse agriculture was shown and perfluorobutanoic acid (PFBA was considered as a marker for source analysis. Bean vegetables contribute highly to the overall PFAA load in vegetables. A significant correlation was shown between irrigation water and agricultural products. The EDI (estimated daily intake from vegetables should be of concern in China.

  9. Antifungal activity of some tetranortriterpenoids.

    Science.gov (United States)

    Govindachari, T R; Suresh, G; Gopalakrishnan, G; Masilamani, S; Banumathi, B

    2000-06-01

    Natural tetranortriterpenoids such as cedrelone from Toona ciliata, azadiradione from Azadirachta indica, limonin, limonol and nomilinic acid from Citrus medica, along with some cedrelone derivatives were tested for their antifungal activity against Puccinia arachidis, a groundnut rust pathogen. Results show that cedrelone was the most effective in reducing rust pustule emergence. Replacement of functional groups or modification of the A or the B ring in cedrelone reduced the effectiveness indicating the importance of specific structural features for activity.

  10. Studies of the yields of 57Fe(II)-species produced after the EC-decay and of 60Co(II)-species produced in the (n, γ) reaction in cobalt(III) coordination compounds

    International Nuclear Information System (INIS)

    Sano, Hirotoshi; Harada, Masayuki; Endo, Kazutoyo

    1978-01-01

    The yields of 57 Fe(II)-species produced after EC-decay were compared with those of 60 Co(II)-species produced in the 59 Co(n, γ) 60 Co reaction for twelve cobalt(III) coordination compounds. The results indicate that the radiochemical yield of 60 Co(II)-species correlates with the yield of 57 Fe(II)-species except in the case of [Co(NH 3 ) 6 ] 2 (CrO 4 ) 3 . The anomalously low yield of 57 Fe(II)-species in [Co(NH 3 ) 6 ] 2 (CrO 4 ) 3 is ascribed to the reaction of chromate anions with ammine ligands initiated by the nuclear transformation in a solid. (author)

  11. Defensins: antifungal lessons from eukaryotes

    Directory of Open Access Journals (Sweden)

    Patrícia M. Silva

    2014-03-01

    Full Text Available Over the last years, antimicrobial peptides (AMPs have been the focus of intense research towards the finding of a viable alternative to current antifungal drugs. Defensins are one of the major families of AMPs and the most represented among all eukaryotic groups, providing an important first line of host defense against pathogenic microorganisms. Several of these cysteine-stabilized peptides present a relevant effect against fungi. Defensins are the AMPs with the broader distribution across all eukaryotic kingdoms, namely, Fungi, Plantæ and Animalia, and were recently shown to have an ancestor in a bacterial organism. As a part of the host defense, defensins act as an important vehicle of information between innate and adaptive immune system and have a role in immunomodulation. This multidimensionality represents a powerful host shield, hard for microorganisms to overcome using single approach resistance strategies. Pathogenic fungi resistance to conventional antimycotic drugs is becoming a major problem. Defensins, as other AMPs, have shown to be an effective alternative to the current antimycotic therapies, demonstrating potential as novel therapeutic agents or drug leads. In this review, we summarize the current knowledge on some eukaryotic defensins with antifungal action. An overview of the main targets in the fungal cell and the mechanism of action of these AMPs (namely, the selectivity for some fungal membrane components are presented. Additionally, recent works on antifungal defensins structure, activity and citotoxicity are also reviewed.

  12. Fumigant antifungal activity of essential oil components from Acorus gramineus against three phytopathogenic fungi.

    Science.gov (United States)

    Lee, Yeon-Suk; Kim, Junheon; Lee, Sang-Gil; Shin, Sang-Chul; Park, Il-Kwon

    2008-01-01

    Analysis by gas chromatography-mass spectrometry led to the identification of 26 compounds in Acorus gramineus essential oil. The antifungal activity of the identified compounds was tested singularly by using standard compounds. Allyl isothiocyanate and cis-asarone showed inhibition rates of 100% against P. cactorum at 28 mg/l air. In a test with C. parasitica and E. circinatum, allyl isothiocyante and cis-asarone showed moderate activity at 28 mg/l air.

  13. Effects on perceived air quality and symptoms of exposure to microbially produced metabolites and compounds emitted from damp building materials.

    Science.gov (United States)

    Claeson, A-S; Nordin, S; Sunesson, A-L

    2009-04-01

    This work investigated perceived air quality and health effects from exposure to low to high levels of volatile organic compounds (VOCs) emitted from damp building materials and a mixture of molds growing on the materials. A mixture of Wallemia sebi, Fusarium culmorum, Penicillium chrysogenum, Ulocladium botrytis, and Aspergillus versicolor was inoculated on pine wood and particle board. In Study 1, each of 27 participants took part in two exposure conditions, one with air from molds growing on building materials (low levels of emissions from the building materials and the mold mixture) and one with blank air, both conditions during 60 min. In Study 2, each of 24 participants was exposed (10 min) four times in a 2 x 2 design randomly to air from moldy building materials (high levels) and blank, with and without nose-clip. The participants rated air quality and symptoms before, during, and after each exposure. Self-reported tear-film break-up time and attention and processing speed (Study 1) was also measured. Exposure to high VOC levels increased the reports of perceived poor air quality, and in the condition without nose-clip enhanced skin symptoms were also noted. No such outcome was observed when exposing the participants to low VOC levels. Emissions from building materials caused by dampness and microbial growth may be involved in indoor air health problems. This study showed that exposure to high levels of VOC emitted from damp building materials and a mixture of mold may cause perceived poor air quality. It also indicated that stimulation of chemical warning systems (the nasal chemosensory part of the trigeminal system and the olfactory system) may enhance skin symptoms.

  14. The Impact of the Antimicrobial Compounds Produced by Lactic Acid Bacteria on the Growth Performance of Mycobacterium avium subsp. paratuberculosis

    Directory of Open Access Journals (Sweden)

    Petr Kralik

    2018-04-01

    Full Text Available Cell-free supernatants (CFSs extracted from various lactic acid bacteria (LAB cultures were applied to Mycobacterium avium subsp. paratuberculosis (MAP cells to determine their effect on MAP viability. In addition, 5% lactic acid (LA; pH 3 and commercially synthetized nisin bacteriocin were also tested. This procedure was chosen in order to mimic the influence of LAB compounds during the production and storage of fermented milk products, which can be contaminated by MAP. Its presence in milk and milk products is of public concern due to the possible ingestion of MAP by consumers and the discussed role of MAP in Crohn’s disease. Propidium monoazide real-time PCR (PMA qPCR was used for viability determination. Although all CFS showed significant effects on MAP viability, two distinct groups of CFS – effective and less effective – could be distinguished. The effective CFSs were extracted from various lactobacilli cultures, their pH values were mostly lower than 4.5, and their application resulted in >2 log10 reductions in MAP viability. The group of less effective CFS were filtered from Lactococcus and enterococci cultures, their pH values were higher than 4.5, and their effect on MAP viability was <2 log10. LA elicited a reduction in MAP viability that was similar to that of the group of less effective CFS. Almost no effect was found when using commercially synthetized nisin at concentrations of 0.1–1000 μg/ml. A combination of the influence of the type of bacteriocin, the length of its action, bacteriocin production strain, and pH are all probably required for a successful reduction in MAP viability. However, certain bacteriocins and their respective LAB strains (Lactobacillus sp. appear to play a greater role in reducing the viability of MAP than pH.

  15. The influence of extracellular compounds produced by selected Baltic cyanobacteria, diatoms and dinoflagellates on growth of green algae Chlorella vulgaris

    Science.gov (United States)

    Żak, Adam; Kosakowska, Alicja

    2015-12-01

    Secondary metabolites produced by bacteria, fungi, algae and plants could affect the growth and development of biological and agricultural systems. This natural process that occurs worldwide is known as allelopathy. The main goal of this work was to investigate the influence of metabolites obtained from phytoplankton monocultures on the growth of green algae Chlorella vulgaris. We selected 6 species occurring in the Baltic Sea from 3 different taxonomic groups: cyanobacteria (Aphanizomenon flos-aquae; Planktothrix agardhii), diatoms (Thalassiosira pseudonana; Chaetoceros wighamii) and dinoflagellates (Alexandrium ostenfeldii; Prorocentrum minimum). In this study we have demonstrated that some of selected organisms caused allelopathic effects against microalgae. Both the negative and positive effects of collected cell-free filtrates on C. vulgaris growth, chlorophyll a concentration and fluorescence parameters (OJIP, QY, NPQ) have been observed. No evidence has been found for the impact on morphology and viability of C. vulgaris cells.

  16. Antifungal activity of extracts from endophytic fungi associated with Smallanthus maintained in vitro as autotrophic cultures and as pot plants in the greenhouse.

    Science.gov (United States)

    Rosa, Luiz H; Tabanca, Nurhayat; Techen, Natascha; Pan, Zhiqiang; Wedge, David E; Moraes, Rita M

    2012-10-01

    The endophytic fungal assemblages associated with Smallanthus sonchifolius (Poepp.) H. Rob. and Smallanthus uvedalius (L.) Mack. ex Small growing in vitro autotrophic cultures and in the greenhouse were identified and evaluated for their ability to produce bioactive compounds. A total of 25 isolates were recovered that were genetically closely related to species of the genera Bionectria , Cladosporium , Colletotrichum , Fusarium , Gibberella , Hypocrea , Lecythophora , Nigrospora , Plectosphaerella , and Trichoderma . The endophytic assemblages of S. sonchifolius presented a greater diversity than the group isolated from S. uvedalius and demonstrated the presence of dominant generalist fungi. Extracts of all fungi were screened against the fungal plant pathogens. Ten extracts (41.6%) displayed antifungal activities; some of them had a broad antifungal activity. The phylotypes Lecythophora sp. 1, Lecythophora sp. 2, and Fusarium oxysporum were isolated from in vitro autotrophic cultures and displayed antifungal activity. The presence of bioactive endophytic fungi within S. sonchifolius and S. uvedalius suggests an ecological advantage against pathogenic attacks. This study revealed reduced numbers of endophytes in association with both Smallanthus species in controlled cultivation conditions compared with the endophytic communities of hosts collected in the wild environments. Even as reduced endophytic communities, these fungi continue to provide chemical protection for the host.

  17. Antifungal activities of secondary metabolites isolated from liquid fermentations of Stereum hirsutum (Sh134-11) against Botrytis cinerea (grey mould agent).

    Science.gov (United States)

    Aqueveque, Pedro; Céspedes, Carlos L; Becerra, José; Aranda, Mario; Sterner, Olov

    2017-11-01

    Extracts obtained from liquid mycelial fermentations of the Chilean fungus Stereum hirsutum (Sh134-11) showed antifungal activity against Botrytis cinerea. Two types of extracts were obtained: EtOAc-extract (liquid phase) and MeOH-extract (mycelial phase). Plate diffusion assay showed that EtOAc-extracts were more active than MeOH-extracts. A large-scale fermentation of Sh134-11 and chromatographic methods allowed to isolated four compounds: MS-3, Vibralactone, Vibralactone B and Sterenin D. Only Sterenin D showed antifungal activity against B. cinerea in the tests performed. Effects on the mycelial growth of B. cinerea showed that Sterenin D showed inhibition at 1000-2000 μg/mL reaching 67% and 76% respectively. Sterenin D was more effective to control the sporogenesis, inhibiting in 96% the sporulation at 500 μg/mL. Assays showed that Sterenin D exhibited a minimal fungicidal concentration (MFC) of 50 μg/mL and minimal inhibitory concentration (MIC) at 20 μg/mL. Our study indicated that submerged fermentations of Chilean S. hirsutum (Sh134-11) produced extracts with antifungal activity and Sterenin D is responsible for this activity, which could be used as possible biofungicides alternative to synthetic fungicides. Copyright © 2017 Elsevier Ltd. All rights reserved.

  18. Study of the behaviour of P-oxides produced in the combustion of phosphorus-bearing organic compounds and their absorption on suitable substances by means of compounds labelled with 32P. I

    International Nuclear Information System (INIS)

    Binkowski, J.; Gizinski, S.; Kaminski, R.; Reimschuessel, W.

    1976-01-01

    During the pyrolytic reaction of phosphorus-bearing compounds in an atmosphere of oxygen, there are produced P-oxides, which interfere in the determination of carbon and hydrogen. The behaviour of these P-oxides was studied intensively in the empty combustion tube in dependence on temperature, velocity of the carrier gas, the nature of the combustion and the positioning of the tube. The P-oxides were determined by the employment of 32 P-labelled aniline phosphate and by activation measurement of the 32 P directly through the tube walls as well as in the finely divided material. In conventional combustions the P-oxides separate abundantly on the walls of the tube provided that the gas velocity is low, especially in those zones of the tube where there is marked temperature lowering, or where very high temperature prevail. Deposited P-oxides are swept out of the tube only in the course of a very long time. Consequently a tube in which the P-bearing compounds have been burned will interfere because of the eluted P-oxides and hence will interfere also if P-free compounds are burned in this same tube

  19. Evaluation of radio-activated compounds produced in the walls and adjacent areas of a small medical cyclotron

    International Nuclear Information System (INIS)

    Saito, Kyoko; Takahashi, Yasuyuki; Yamaguchi, Ichiro; Kimura, Ken-ichi; Kanzaki, Takao; Shimada, Hirotaka; Otake, Hidenori; Oriuchi, Noboru; Endo, Keigo

    2009-01-01

    According to the 18 O(p, n) 18 F reaction, fast neutrons produced in the target will cause residual radioactivity in a cyclotron itself and in the concrete walls mainly after thermalization of neutrons. As exploratory work prior to decommissioning of a medical cyclotron facility, surface and core samples of the facility's concrete walls were collected after confirming the external radiation was at a low level based on hollow ionization chamber-type survey meter and glass dosimeter measurements. The residual radioactivity in these samples was measured by gamma-spectrometry. Residual radioactivity was detected in all of the components of the cyclotron. In the concrete, eight residual radioactive nuclides were identified. However, radioactivity concentrations of these radionuclides were less than that of 40 K which may exist generally in a natural environment. A clearance level for radioactive solid waste has not been defined nor implemented at present in Japan, and reliable evaluation will be required to minimize radioactive waste at the time of decommissioning. The present results provide basic data for establishment of regulatory guidelines for decommissioning of medical cyclotrons. (author)

  20. Pollen types and levels of total phenolic compounds in propolis produced by Apis mellifera L. (Apidae in an area of the Semiarid Region of Bahia, Brazil

    Directory of Open Access Journals (Sweden)

    VANESSA R. MATOS

    2014-03-01

    Full Text Available Twenty-two propolis samples produced by Apis mellifera L. in an area of the Semiarid region the the State of Bahia (Agreste of Alagoinhas, Brazil, were palynologically analyzed and quantified regarding their levels of total phenolic compounds. These samples were processed using the acetolysis technique with the changes suggested for use with propolis. We found 59 pollen types belonging to 19 families and 36 genera. The family Fabaceae was the most representative in this study with nine pollen types, followed by the family Asteraceae with seven types. The types Mikania and Mimosa pudica occurred in all samples analyzed. The types Mimosa pudica and Eucalyptus had frequency of occurrence above 50% in at least one sample. The highest similarity index (c. 72% occurred between the samples ER1 and ER2, belonging to the municipality of Entre Rios. Samples from the municipality of Inhambupe displayed the highest (36.78±1.52 mg/g EqAG and lowest (7.68 ± 2.58 mg/g EqAG levels of total phenolic compounds. Through the Spearman Correlation Coefficient we noticed that there was a negative linear correlation between the types Mimosa pudica (rs = -0.0419 and Eucalyptus (rs = -0.7090 with the profile of the levels of total phenolic compounds of the samples.

  1. Mangrove rare actinobacteria: taxonomy, natural compound, and discovery of bioactivity

    Science.gov (United States)

    Azman, Adzzie-Shazleen; Othman, Iekhsan; Velu, Saraswati S.; Chan, Kok-Gan; Lee, Learn-Han

    2015-01-01

    Actinobacteria are one of the most important and efficient groups of natural metabolite producers. The genus Streptomyces have been recognized as prolific producers of useful natural compounds as they produced more than half of the naturally-occurring antibiotics isolated to-date and continue as the primary source of new bioactive compounds. Lately, Streptomyces groups isolated from different environments produced the same types of compound, possibly due to frequent genetic exchanges between species. As a result, there is a dramatic increase in demand to look for new compounds which have pharmacological properties from another group of Actinobacteria, known as rare actinobacteria; which is isolated from special environments such as mangrove. Recently, mangrove ecosystem is becoming a hot spot for studies of bioactivities and the discovery of natural products. Many novel compounds discovered from the novel rare actinobacteria have been proven as potential new drugs in medical and pharmaceutical industries such as antibiotics, antimicrobials, antibacterials, anticancer, and antifungals. This review article highlights the latest studies on the discovery of natural compounds from the novel mangrove rare actinobacteria and provides insight on the impact of these findings. PMID:26347734

  2. Correlation between Plant Secondary Metabolites and Their Antifungal Mechanisms–A Review

    DEFF Research Database (Denmark)

    Freiesleben, Sara; Jäger, Anna

    2014-01-01

    The search for new antifungal drugs often involves secondary metabolites from plants because of their pharmacological activity against foreign pathogens. Among the modern drugs in use today about 40% are of natural origin. To distinguish the secondary metabolites they can be divided into groups...... search for existing knowledge about antifungal mechanisms of different secondary metabolites from plants. The secondary metabolites have been grouped into three major groups according to their biosynthetic origin, and into subgroups according to their structure. There seems to be a correlation between...... biosynthetic groups of secondary metabolites; the phenolic compounds and the nitrogen containing compounds. Despite this there are correlations between some of the subgroups and their antifungal mechanism of actions....

  3. Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group

    Directory of Open Access Journals (Sweden)

    Xu K

    2015-03-01

    Full Text Available Kehan Xu,1,* Lei Huang,1,* Zheng Xu,2 Yanwei Wang,1,3 Guojing Bai,1 Qiuye Wu,1 Xiaoyan Wang,1 Shichong Yu,1 Yuanying Jiang1 1School of Pharmacy, Second Military Medical University, Shanghai, 2Shanghai Changzheng Hospital, Second Military Medical University, Shanghai, 3Number 422 Hospital of PLA, Zhanjiang, People’s Republic of China *These authors contributed equally to this work Abstract: In previous studies undertaken by our group, a series of 1-(1H-1,2,4-triazole-1-yl-2-(2,4-difluorophenyl-3-substituted-2-propanols (1a–r, which were analogs of fluconazole, was designed and synthesized by click chemistry. In the study reported here, the in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. Compounds 1a, 1q, and 1r showed the more antifungal activity than the others. Keywords: triazole, synthesis, antifungal activity, CYP51

  4. Antifungal effects of Allium ascalonicum, Marticaria chamomilla and Stachys lavandulifolia extracts on Candida albicans

    Directory of Open Access Journals (Sweden)

    Moghim Hassan

    2014-01-01

    Full Text Available Introduction: Due to increased risk for opportunistic fungal infections and increasing prevalence of hospital infections caused by pathogenic yeasts and fungus resistance to antifungal drugs, discovery of antifungal compounds with high efficiency is necessary. This study was aimed to evaluate and compare the antifungal activities of Allium ascalonicum, Marticaria chamomilla and Stachys lavandulifolia on Candida albians. Methods: In this study the plants extracts were prepared with macerated method using ethanol 70%. Antifungal activities of the extracts were performed according to microbroth dilution method in 96 well microdilution plates. The amount of Minimum Inhibitory Concentration (MIC and Minimum Fungicidal Concentration (MFC based on counting the number of fungal colonies (CFU were evaluated for each of Allium ascalonicum, Chamomile and Stachys lavandulifolia extracts compared with the control group. Results: MIC of Allium ascalonicum, Marticaria chamomilla and Stachys lavandulifolia were respectively 0.31, 3.75 and 15.13 mg/ml and also MIC50% of Allium ascalonicum, Marticaria chamomilla and Stachys lavandulifolia were respectively 0.93, 10.59 and 41.32 mg/ml and MIC 90% of them were respectively 8.65, 16.88 and 60.55 mg/ml and their MFC were respectively 20, 20 and 65 mg/ml. Conclusion: The results indicate that all three extracts are effective, but Allium ascalonicum possesses the highest antifungal activity on Candida albicans. If clinical trials approve these findings, this plant may represent a new source of antifungal agent for control of Candida albicans.

  5. Role of Modular Polyketide Synthases in the Production of Polyether Ladder Compounds in Ciguatoxin-Producing Gambierdiscus polynesiensis and G. excentricus (Dinophyceae).

    Science.gov (United States)

    Kohli, Gurjeet S; Campbell, Katrina; John, Uwe; Smith, Kirsty F; Fraga, Santiago; Rhodes, Lesley L; Murray, Shauna A

    2017-09-01

    Gambierdiscus, a benthic dinoflagellate, produces ciguatoxins that cause the human illness Ciguatera. Ciguatoxins are polyether ladder compounds that have a polyketide origin, indicating that polyketide synthases (PKS) are involved in their production. We sequenced transcriptomes of Gambierdiscus excentricus and Gambierdiscus polynesiensis and found 264 contigs encoding single domain ketoacyl synthases (KS; G. excentricus: 106, G. polynesiensis: 143) and ketoreductases (KR; G. excentricus: 7, G. polynesiensis: 8) with sequence similarity to type I PKSs, as reported in other dinoflagellates. In addition, 24 contigs (G. excentricus: 3, G. polynesiensis: 21) encoding multiple PKS domains (forming typical type I PKSs modules) were found. The proposed structure produced by one of these megasynthases resembles a partial carbon backbone of a polyether ladder compound. Seventeen contigs encoding single domain KS, KR, s-malonyltransacylase, dehydratase and enoyl reductase with sequence similarity to type II fatty acid synthases (FAS) in plants were found. Type I PKS and type II FAS genes were distinguished based on the arrangement of domains on the contigs and their sequence similarity and phylogenetic clustering with known PKS/FAS genes in other organisms. This differentiation of PKS and FAS pathways in Gambierdiscus is important, as it will facilitate approaches to investigating toxin biosynthesis pathways in dinoflagellates. © 2017 The Author(s) Journal of Eukaryotic Microbiology © 2017 International Society of Protistologists.

  6. Analytical and sensorial characterization of the aroma of wines produced with sour rotten grapes using GC-O and GC-MS: identification of key aroma compounds.

    Science.gov (United States)

    Barata, André; Campo, Eva; Malfeito-Ferreira, Manuel; Loureiro, Virgílio; Cacho, Juan; Ferreira, Vicente

    2011-03-23

    In the present work, the aroma profiles of wines elaborated from sound and sour rot-infected grapes as raw material have been studied by sensory analysis, gas chromatography-olfactometry (GC-O), and gas chromatography-mass spectrometry (GC-MS), with the aim of determining the odor volatiles most likely associated with this disease. The effect of sour rot was tested in monovarietal wines produced with the Portuguese red grape variety Trincadeira and in blends of Cabernet Sauvignon and sour rotten Trincadeira grapes. Wines produced from damaged berries exhibited clear honey-like notes not evoked by healthy samples. Ethyl phenylacetate (EPhA) and phenylacetic acid (PAA), both exhibiting sweet honey-like aromas, emerged as key aroma compounds of sour rotten wines. Their levels were 1 order of magnitude above those found in controls and reached 304 and 1668 μg L(-1) of EPhA and PAA, respectively, well above the corresponding odor thresholds. Levels of γ-nonalactone also increased by a factor 3 in sour rot samples. Results also suggest that sour rot exerts a great effect on the secondary metabolism of yeast, decreasing the levels of volatiles related to fatty acids and amino acid synthesis. The highest levels of γ-decalactone of up to 405 μg L(-1) were also found in all of the samples, suggesting that this could be a relevant aroma compound in Trincadeira wine aroma.

  7. Strains of the genus Serratia as beneficial rhizobacteria of oilseed rape with antifungal properties.

    Science.gov (United States)

    Kalbe, C; Marten, P; Berg, G

    1996-12-01

    Isolates of Serratia have been isolated from the rhizosphere of oilseed rape. The percentage of Serratia in this microenvironment was determined as 12.4% of the total antifungal bacteria. Serratia liquefaciens, S. plymuthica and S. rubidaea were found. All of the isolates showed an antifungal activity against different phytopathogenic fungi in vitro but the efficiency of strains was different. The antifungal mechanisms of 18 selected strains were investigated. Direct antifungal effect may be based on antibiosis (production of prodigiosin and pyrrolnitrin) and production of lytic enzymes (chitinases and beta-1,3-glucanases). Potent siderophores were secreted by the strains to improve the availability of iron. No strain was able to produce cyanide. Most of the strains secrete the plant growth hormone indole-acetic-acid which can directly promote the growth of roots. The mechanisms were specific for each isolate.

  8. Antifungal activity of redox-active benzaldehydes that target cellular antioxidation

    Directory of Open Access Journals (Sweden)

    Mahoney Noreen

    2011-05-01

    Full Text Available Abstract Background Disruption of cellular antioxidation systems should be an effective method for control of fungal pathogens. Such disruption can be achieved with redox-active compounds. Natural phenolic compounds can serve as potent redox cyclers that inhibit microbial growth through destabilization of cellular redox homeostasis and/or antioxidation systems. The aim of this study was to identify benzaldehydes that disrupt the fungal antioxidation system. These compounds could then function as chemosensitizing agents in concert with conventional drugs or fungicides to improve antifungal efficacy. Methods Benzaldehydes were tested as natural antifungal agents against strains of Aspergillus fumigatus, A. flavus, A. terreus and Penicillium expansum, fungi that are causative agents of human invasive aspergillosis and/or are mycotoxigenic. The yeast Saccharomyces cerevisiae was also used as a model system for identifying gene targets of benzaldehydes. The efficacy of screened compounds as effective chemosensitizers or as antifungal agents in formulations was tested with methods outlined by the Clinical Laboratory Standards Institute (CLSI. Results Several benzaldehydes are identified having potent antifungal activity. Structure-activity analysis reveals that antifungal activity increases by the presence of an ortho-hydroxyl group in the aromatic ring. Use of deletion mutants in the oxidative stress-response pathway of S. cerevisiae (sod1Δ, sod2Δ, glr1Δ and two mitogen-activated protein kinase (MAPK mutants of A. fumigatus (sakAΔ, mpkCΔ, indicates antifungal activity of the benzaldehydes is through disruption of cellular antioxidation. Certain benzaldehydes, in combination with phenylpyrroles, overcome tolerance of A. fumigatus MAPK mutants to this agent and/or increase sensitivity of fungal pathogens to mitochondrial respiration inhibitory agents. Synergistic chemosensitization greatly lowers minimum inhibitory (MIC or fungicidal (MFC

  9. Synthesis and Antifungal Activity of Novel Sulfone Derivatives Containing 1,3,4-Oxadiazole Moieties

    Directory of Open Access Journals (Sweden)

    Maoguo Tong

    2011-11-01

    Full Text Available A series of new sulfone compounds containing 1,3,4-oxadiazole moieties were synthesized. The structures of these compounds were confirmed by spectroscopic data (IR, 1H- and 13C-NMR and elemental analyses. Antifungal tests indicated that all the title compounds exhibited good antifungal activities against eight kinds of plant pathogenic fungi, and some showed superiority over the commercial fungicide hymexazol. Among them, compounds 5d, 5e, 5f, and 5i showed prominent activity against B. cinerea, with determined EC50 values of 5.21 μg/mL, 8.25 µg/mL, 8.03 µg/mL, and 21.00 µg/mL, respectively. The present work demonstrates that sulfone derivatives such as 5d containing a 1,3,4-oxadiazole moiety can be used as possible lead compounds for the development of potential agrochemicals.

  10. Antifungal stewardship in a tertiary hospital.

    Science.gov (United States)

    Ramos, Antonio; Pérez-Velilla, Claudia; Asensio, Angel; Ruiz-Antorán, Belén; Folguera, Carlos; Cantero, Mireia; Orden, Beatriz; Muñez, Elena

    2015-01-01

    The inappropriate use of antifungals is an important health problem related to increasing adverse effects, unnecessary cost and promotion of resistant and emerging fungal infections. Despite its relevance, many health institutions assign few resources to improve prescribing practices. To evaluate the efficiency of an antifungal stewardship programme (ASP) centered on restricted antifungal agents. The main activity during the eight-month study was to perform a programmed review of restricted antifungals (lipid formulations of amphotericin B, echinocandins and voriconazole) prescribed in hospitalized patients. In the case of amendable antifungal treatment, a recommendation was included in the electronic medical record. A total of 280 antifungal prescriptions for 262 patients were revised during the study period. The indications were prophylactic in 85 cases (30.4%), pre-emptive in 10 cases (3.5%), empiric in 122 cases (43.6%), and directed in 63 cases (22.5%). A total of 70 prescriptions (25%) in 61 patients were considered to be amendable. In most of these cases, treatment could have been reduced considering the patient's clinical improvement and microbiological results. The most common advice was antifungals change (70%), antifungal withdrawal (21%), removal of one antifungal drug in cases of combined therapy (7%), and switching to oral route (1%). Proposed recommendations were addressed in 28 cases (40%). There was no significant difference in adherence with respect to the type of recommendation (p=0.554). There was a 42% lower use of antifungals during the period of the study compared to that observed during a similar previous period. Mortality among patients who were treated according to the recommendations of the ASP was 17% and in whom treatment was not modified it was 30% (p=0.393). ASPs centered on hospitalized patients may be an efficient strategy to ameliorate antifungal use in hospitals. Copyright © 2014 Revista Iberoamericana de Micología. Published by

  11. Outbreak of Extended-Spectrum Beta-Lactamase Producing Enterobacter cloacae with High MICs of Quaternary Ammonium Compounds in a Hematology Ward Associated with Contaminated Sinks

    Science.gov (United States)

    Chapuis, Angélique; Amoureux, Lucie; Bador, Julien; Gavalas, Arthur; Siebor, Eliane; Chrétien, Marie-Lorraine; Caillot, Denis; Janin, Marion; de Curraize, Claire; Neuwirth, Catherine

    2016-01-01

    Objective: To investigate an outbreak of extended-spectrum beta-lactamase (ESBL) producing Enterobacter cloacae that occurred in the Hematology ward (24-bed unit) of the François Mitterrand University Hospital (Dijon, France) between January 2011 and December 2013. The outbreak involved 43 patients (10 infected and 33 colonized). Design: We performed environmental analysis to detect multiresistant E. cloacae for comparison with clinical isolates (genotyping by pulsed-field gel electrophoresis and MLST as well as ESBL-typing) and determined the MICs of the quaternary ammonium compounds (QACs) alkyldimethylbenzylammonium chloride (ADBAC) and didecyldimethylammonium chloride (DDAC). A bleach-based cleaning-disinfection program was implemented in December 2012 after mechanical removal of the biofilm in all sinks. Results: We have detected 17 ESBL-producing E. cloacae in patients sink drains, shower drains and medical sink drains. Sequencing of the bla genes performed on 60 strains recovered from patients and environment (n = 43 clinical and n = 17 environmental) revealed that bla CTX−M15 was predominant (37 isolates) followed by bla CTX−M9 plus bla SHV−12 (20 isolates). We observed a great diversity among the isolates: 14 pulsotypes (11 STs) in clinical isolates and 9 pulsotypes (7 STs) in environmental isolates. Six pulsotypes were identical between clinical and environmental isolates. MICs of the quaternary ammonium compounds widely used for disinfection were very high in clinical and environmental isolates. Immediately after the implementation of the disinfection program we noticed a substantial fall in cases number. Our findings demonstrate the role of drains as important reservoir of ESBL-producing E. cloacae and highlight the necessity to settle drains accessible to achieve correct cleaning as well as to use disinfectant with proved activity against nosocomial pathogens. PMID:27462306

  12. Outbreak of extended-spectrum beta-lactamase producing Enterobacter cloacae with high MICs of quaternary ammonium compounds in a Hematology ward associated with contaminated sinks

    Directory of Open Access Journals (Sweden)

    Angelique Chapuis

    2016-07-01

    Full Text Available ObjectiveTo investigate an outbreak of extended-spectrum beta-lactamase (ESBL producing Enterobacter cloacae that occurred in the Hematology ward (24-bed unit of the François Mitterrand University Hospital (Dijon, France between January 2011 and December 2013. The outbreak involved 43 patients (10 infected and 33 colonized. DesignWe performed environmental analysis to detect multiresistant E. cloacae for comparison with clinical isolates (genotyping by pulsed-field gel electrophoresis and MLST as well as ESBL-typing and determined the MICs of the quaternary ammonium compounds (QACs alkyldimethylbenzylammonium chloride (ADBAC and didecyldimethylammonium chloride (DDAC. A bleach-based cleaning-disinfection program was implemented in December 2012 after mechanical removal of the biofilm in all sinks. ResultsWe have detected 17 ESBL-producing E. cloacae in patients sink drains, shower drains and medical sink drains. Sequencing of the bla genes performed on 60 strains recovered from patients and environment (n=43 clinical and n=17 environmental revealed that bla CTX-M15 was predominant (37 isolates followed by bla CTX-M9 plus bla SHV-12 (20 isolates. We observed a great diversity among the isolates: 14 pulsotypes (11 STs in clinical isolates and 9 pulsotypes (7 STs in environmental isolates. Six pulsotypes were identical between clinical and environmental isolates. MICs of the quaternary ammonium compounds widely used for disinfection were very high in clinical and environmental isolates. Immediately after the implementation of the disinfection program we noticed a substantial fall in cases number. Our findings demonstrate the role of drains as important reservoir of ESBL-producing E. cloacae and highlight the necessity to settle drains accessible to achieve correct cleaning as well as to use disinfectant with proved activity against nosocomial pathogens.

  13. Outbreak of Extended-Spectrum Beta-Lactamase Producing Enterobacter cloacae with High MICs of Quaternary Ammonium Compounds in a Hematology Ward Associated with Contaminated Sinks.

    Science.gov (United States)

    Chapuis, Angélique; Amoureux, Lucie; Bador, Julien; Gavalas, Arthur; Siebor, Eliane; Chrétien, Marie-Lorraine; Caillot, Denis; Janin, Marion; de Curraize, Claire; Neuwirth, Catherine

    2016-01-01

    To investigate an outbreak of extended-spectrum beta-lactamase (ESBL) producing Enterobacter cloacae that occurred in the Hematology ward (24-bed unit) of the François Mitterrand University Hospital (Dijon, France) between January 2011 and December 2013. The outbreak involved 43 patients (10 infected and 33 colonized). We performed environmental analysis to detect multiresistant E. cloacae for comparison with clinical isolates (genotyping by pulsed-field gel electrophoresis and MLST as well as ESBL-typing) and determined the MICs of the quaternary ammonium compounds (QACs) alkyldimethylbenzylammonium chloride (ADBAC) and didecyldimethylammonium chloride (DDAC). A bleach-based cleaning-disinfection program was implemented in December 2012 after mechanical removal of the biofilm in all sinks. We have detected 17 ESBL-producing E. cloacae in patients sink drains, shower drains and medical sink drains. Sequencing of the bla genes performed on 60 strains recovered from patients and environment (n = 43 clinical and n = 17 environmental) revealed that bla CTX-M15 was predominant (37 isolates) followed by bla CTX-M9 plus bla SHV-12 (20 isolates). We observed a great diversity among the isolates: 14 pulsotypes (11 STs) in clinical isolates and 9 pulsotypes (7 STs) in environmental isolates. Six pulsotypes were identical between clinical and environmental isolates. MICs of the quaternary ammonium compounds widely used for disinfection were very high in clinical and environmental isolates. Immediately after the implementation of the disinfection program we noticed a substantial fall in cases number. Our findings demonstrate the role of drains as important reservoir of ESBL-producing E. cloacae and highlight the necessity to settle drains accessible to achieve correct cleaning as well as to use disinfectant with proved activity against nosocomial pathogens.

  14. Antifungal Microbial Agents for Food Biopreservation-A Review.

    Science.gov (United States)

    Leyva Salas, Marcia; Mounier, Jérôme; Valence, Florence; Coton, Monika; Thierry, Anne; Coton, Emmanuel

    2017-07-08

    Food spoilage is a major issue for the food industry, leading to food waste, substantial economic losses for manufacturers and consumers, and a negative impact on brand names. Among causes, fungal contamination can be encountered at various stages of the food chain (e.g., post-harvest, during processing or storage). Fungal development leads to food sensory defects varying from visual deterioration to noticeable odor, flavor, or texture changes but can also have negative health impacts via mycotoxin production by some molds. In order to avoid microbial spoilage and thus extend product shelf life, different treatments-including fungicides and chemical preservatives-are used. In parallel, public authorities encourage the food industry to limit the use of these chemical compounds and develop natural methods for food preservation. This is accompanied by a strong societal demand for 'clean label' food products, as consumers are looking for more natural, less severely processed and safer products. In this context, microbial agents corresponding to bioprotective cultures, fermentates, culture-free supernatant or purified molecules, exhibiting antifungal activities represent a growing interest as an alternative to chemical preservation. This review presents the main fungal spoilers encountered in food products, the antifungal microorganisms tested for food bioprotection, and their mechanisms of action. A focus is made in particular on the recent in situ studies and the constraints associated with the use of antifungal microbial agents for food biopreservation.

  15. Antifungal activity of polycyclic aromatic hydrocarbons against Ligninolytic fungi

    Directory of Open Access Journals (Sweden)

    Memić Mustafa

    2011-01-01

    Full Text Available Environmental contamination by polycyclic aromatic hydrocarbons (PAHs has caused increasing concern because of their known, or suspected, carcinogenic and mutagenic effects. Polycyclic aromatic hydrocarbons occurring in the environment are usually the result of the incomplete combustion of carbon containing materials. The main sources of severe PAHs contamination in soil come from fossil fuels, i.e. production or use of fossil fuels or their products, such as coal tar and creosote. Creosote is used as a wood preservation for railway ties, bridge timbers, pilling and large-sized lumber. It consists mainly of PAHs, phenol and cresol compounds that cause harmful health effects. Research on biodegradation has shown that a special group of microorganisms, the white-rot fungi and brown-rot fungi, has a remarkable potential to degrade PAHs. This paper presents a study of the antifungal activity of 12 selected PAHs against two ligninolytic fungi Hypoxylon fragiforme (white rot and Coniophora puteana (brown rot. The antifungal activity of PAHs was determined by the disc-diffusion method by measuring the diameter of the zone of inhibition. The results showed that the antifungal activity of the tested PAHs (concentration of 2.5 mmol/L depends on the their properties such as molar mass, solubility in water, values of log Kow, ionization potential and Henry’s Law constant as well as number of aromatic rings, molecule topology or pattern of ring linkage. Among the 12 investigated PAHs, benzo(k fluoranthene with five rings, and pyrene with four cyclic condensed benzene rings showed the highest antifungal activity.

  16. Essential oil of Psidium cattleianum leaves: antioxidant and antifungal activity.

    Science.gov (United States)

    Castro, Micheli R; Victoria, Francine N; Oliveira, Daniela H; Jacob, Raquel G; Savegnago, Lucielli; Alves, Diego

    2015-02-01

    Psidium cattleianum Sabine (Myrtacea) is rich in vitamin C and phenolic compounds, including epicatechin and gallic acid as the main components. To evaluate the antifungal and antioxidant capacity in vitro of the essential oil of araçá (EOA). The acute toxicity of the EOA also was evaluated in mice. The leaves of the P. cattleianum were extracted by steam distillation. The antioxidant capacity was evaluated by in vitro tests [1,1-diphenyl-2-picryl-hydrazyl (DPPH), 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonate) (ABTS), ferric ion reducing antioxidant power (FRAP), linoleic acid oxidation, thiobarbituric acid reactive species (TBARS)], and ex vivo analysis [TBARS, δ-aminulevunilate dehydratase (δ-Ala-D) and catalase activity, non-protein thiols (NPSH), and ascorbic acid levels]. The toxicity was studied in mice by a single oral administration of EOA; and the antifungal activity was performed with five strains of fungi. The EOA exhibited antioxidant activity in the FRAP assay and reduced lipid peroxidation in the cortex (Imax = 32.90 ± 2.62%), hippocampus (IC50 = 48.00 ± 3.00 µg/ml and Imax = 32.90 ± 2.62%), and cerebellum (Imax = 45.40 ± 14.04%) of mice. Acute administration of the EOA by the oral route did not cause toxicological effects in mice (LD50 > 500 µg/ml). The EOA also showed antifungal activity through of the determination minimum inhibitory concentration (MIC) values ranging from 41.67 ± 18.04 to 166.70 ± 72.17 µg/ml for tested strains. The results of present study indicate that EOA possess antioxidant properties, antifungal and not cause toxicity at tested doses.

  17. Characterization of four new antifungal yanuthones from Aspergillus niger

    DEFF Research Database (Denmark)

    Petersen, Lene Maj; Holm, Dorte Koefoed; Knudsen, Peter Boldsen

    2015-01-01

    identified three class I yanuthones originating from the polyketide 6-methylsalicylic acid (yanuthone K, L and M (1–3)) and a class II yanuthone, which was named yanuthone X2 (4). The four new compounds were tested toward the pathogenic yeast Candida albicans and all displayed antifungal activity. Yanuthone...

  18. Antifungal potential of marine sponge extract against plant and fish pathogenic fungi

    Digital Repository Service at National Institute of Oceanography (India)

    PrabhaDevi; Ravichandran, S.; Ribeiro, M.; Ciavatta, M.L.

    of the active compound as latrunculin B on the basis of spectroscopic data. This finding suggests that latrunculin B, could be considered as a lead molecule for the design of new antifungals for managing common fungal diseases in aquaculture. Toxicity testing...

  19. Antibacterial and antifungal activities of 5-arylidene-n,n-dimethylbarbiturates derivatives

    International Nuclear Information System (INIS)

    Rahim, F.; Haider, S.M.

    2014-01-01

    A series of N,N-dimethyl-arylidene barbiturates 1-22 has been re-synthesized and evaluated against a number of Gram-positive, Gram-negative bacteria and some fungal strains. Most of the compounds were found to be active against a number of Gram-positive, Gram-negative and also displayed anti-fungal activities. (author)

  20. Draft Genome Sequence of Bacillus velezensis OSY-S3, a Producer of Potent Antimicrobial Agents Active against Bacteria and Fungi.

    Science.gov (United States)

    Gerst, Michelle M; Yesil, Mustafa; Yousef, Ahmed E

    2018-01-18

    Bacillus velezensis OSY-S3 produces anti- Listeria , anti- Escherichia coli , and antifungal compounds. Additionally, fermentate of B. velezensis OSY-S3 culture removes Staphylococcus aureus biofilms effectively. The draft genome sequence of B. velezensis OSY-S3 reported here had a genome size of ~3.90 Mb and a G+C content of 46.5%. Copyright © 2018 Gerst et al.

  1. Draft Genome Sequence of Bacillus velezensis OSY-S3, a Producer of Potent Antimicrobial Agents Active against Bacteria and Fungi

    OpenAIRE

    Gerst, Michelle M.; Yesil, Mustafa; Yousef, Ahmed E.

    2018-01-01

    ABSTRACT Bacillus velezensis OSY-S3 produces anti-Listeria, anti-Escherichia coli, and antifungal compounds. Additionally, fermentate of B. velezensis OSY-S3 culture removes Staphylococcus aureus biofilms effectively. The draft genome sequence of B. velezensis OSY-S3 reported here had a genome size of ~3.90 Mb and a G+C content of 46.5%.

  2. Biologically active compounds of semi-metals.

    Science.gov (United States)

    Rezanka, Tomás; Sigler, Karel

    2008-02-01

    Semi-metals (boron, silicon, arsenic and selenium) form organo-metal compounds, some of which are found in nature and affect the physiology of living organisms. They include, e.g., the boron-containing antibiotics aplasmomycin, borophycin, boromycin, and tartrolon or the silicon compounds present in "silicate" bacteria, relatives of the genus Bacillus, which release silicon from aluminosilicates through the secretion of organic acids. Arsenic is incorporated into arsenosugars and arsenobetaines by marine algae and invertebrates, and fungi and bacteria can produce volatile methylated arsenic compounds. Some prokaryotes can use arsenate as a terminal electron acceptor while others can utilize arsenite as an electron donor to generate energy. Selenium is incorporated into selenocysteine that is found in some proteins. Biomethylation of selenide produces methylselenide and dimethylselenide. Selenium analogues of amino acids, antitumor, antibacterial, antifungal, antiviral, anti-infective drugs are often used as analogues of important pharmacological sulfur compounds. Other metalloids, i.e. the rare and toxic tellurium and the radioactive short-lived astatine, have no biological significance.

  3. Antifungal saponins from Swartzia langsdorffii; Saponinas antifungicas de Swartzia langsdorffii

    Energy Technology Data Exchange (ETDEWEB)

    Marqui, Sara Regina de; Lemos, Renata Brionizio; Santos, Luciana Avila; Castro-Gamboa, Ian; Cavalheiro, Alberto Jose; Bolzani, Vanderlan da Silva; Silva, Dulce Helena Siqueira [Universidade Estadual Paulista (UNESP), Araraquara, SP (Brazil). Inst. de Quimica]. E-mail: dhsilva@iq.unesp.br; Scorzoni, Liliana; Fusco-Almeida, Ana Maria; Mendes-Giannini, Maria Jose Soares [Universidade Estadual Paulista (UNESP), Araraquara, SP (Brazil). Faculdade de Ciencias Farmaceuticas; Young, Maria Claudia Marx; Torres, Luce Maria Brandao [Inst. de Botanica, SP (Brazil). Secao de Fisiologia e Bioquimica de Plantas

    2008-07-01

    Chromatographic fractionation of the EtOH extract from the leaves of Swartzia langsdorffii afforded the pentacyclic triterpenes oleanolic acid and lupeol, and two saponins: oleanolic acid 3-sophoroside and the new ester 3-O-{beta}-D-(6'-methyl)-glucopyranosyl-28-O-{beta}-D-glucopyranosyl-oleanate. Their structures were elucidated from spectral data, including 2D NMR and HRESIMS experiments. Antifungal activity of all isolated compounds was evaluated, using phytopathogens Cladosporium cladosporioides and C. sphaerospermum, and human pathogens Candida albicans, C. krusei, C. parapsilosis and Cryptococcus neoformans. (author)

  4. Enhancement of downy mildew disease resistance in pearl millet by the G_app7 bioactive compound produced by Ganoderma applanatum.

    Science.gov (United States)

    Jogaiah, Sudisha; Shetty, Hunthrike Shekar; Ito, Shin-Ichi; Tran, Lam-Son Phan

    2016-08-01

    Pearl millet (Pennisetum glaucum) stands sixth among the most important cereal crops grown in the semi-arid and arid regions of the world. The downy mildew disease caused by Sclerospora graminicola, an oomycete pathogen, has been recognized as a major biotic constraint in pearl millet production. On the other hand, basidiomycetes are known to produce a large number of antimicrobial metabolites, providing a good source of anti-oomycete agrochemicals. Here, we report the discovery and efficacy of a compound, named G_app7, purified from Ganoderma applanatum on inhibition of growth and development of S. graminicola, as well as the effects of seed treatment with G_app7 on protection of pearl millet from downy mildew. G_app7 consistently demonstrated remarkable effects against S. graminicola by recording significant inhibition of sporangium formation (41.4%), zoospore release (77.5%) and zoospore motility (91%). Analyses of G_app7 compound using two-dimensional nuclear magnetic resonance spectroscopy and liquid chromatography-mass spectrometry revealed its close resemblance to metominostrobin, a derivative of strobilurin group of fungicides. Furthermore, the G_app7 was shown to stably maintain the inhibitory effects at different temperatures between 25 and 80 °C. In addition, the anti-oomycete activity of G_app7 was fairly stable for a period of at least 12 months at 4 °C and was only completely lost after being autoclaved. Seed treatment with G_app7 resulted in a significant increase in disease protection (63%) under greenhouse conditions compared with water control. The identification and isolation of this novel and functional anti-oomycete compound from G. applanatum provide a considerable agrochemical importance for plant protection against downy mildew in an environmentally safe and economical manner. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  5. Chemical composition and antifungal activity of thyme (Thymus vulgaris essential oil

    Directory of Open Access Journals (Sweden)

    S. Farsaraei*

    2017-11-01

    Full Text Available Background and objectives: The antifungal activity of the essential oils and their constituents against some phytopathogenic fungi has been reported. Thymus vulgaris (Lamiaceae is one of the Thymus species.  A large number of studies have concerned the chemical compositions and antifungal activity of thyme’s oil. In order to reduce the use of synthetic fungicides, recently considerable attention has been given to search for naturally occurring compounds. The aim of the present work was to determine the chemical composition and antifungal activity of T. vulgaris oil cultivated in Iran. Methods: The essential oil from aerial parts of the plant at full flowering stage was subjected to hydrodistillation and chemical compounds were analyzed by GC/GC-MS. The in vitro antifungal activity against three phytopathogenic fungi (Drechslera spicifera, Fusarium oxysporum f.sp. ciceris and Macrophomina phaseolinaby of the oil was evaluated by agar dilution method. The data were subjected to ANOVA according to the SPSS 21 software. Results: Totally 45 compounds representing 96.75% of the oil were found. Thymol (36.81% and ρ-cymene (30.90% were the main components of thyme oil. According to the results, the antifungal activity of the oil increased with a rising in concentration. All of the tested fungi growth was completely inhibited on 1600 µL/L. In this study fungicidal activity was only observed on F. oxysporum and D. spicifera at concentrations higher than 800 µL/L.  Conclusion: The antifungal activity of T. vulgaris essential oil could be probably due to the high concentration of oxygenated monoterpenes (thymol and monoterpene hydrocarbons (ρ-cymene.

  6. Total bremsstrahlung spectra of thick lead compounds produced by {sup 90}Sr beta emitter in photon energy region of 10–100 keV

    Energy Technology Data Exchange (ETDEWEB)

    Sharma, Suhansar Jit [Department of Physics, B.B.S.B Polytechnic, Fatehgarh Sahib, Punjab (India); Singh, Tajinder, E-mail: tajindersingh2k9@gmail.com [Department of Physics, Mata Gujri College, Fatehgarh Sahib, Punjab (India); Singh, Doordarshi [Department of Mechanical Engineering, B.B.S.B Engineering College, Fatehgarh Sahib, Punjab (India); Singh, Amrit [Department of Physics, Baba Ajay Singh Khalsa College, Gurdas Nangal, Gurdaspur, Punjab (India); Dhaliwal, A.S. [Department of Physics, Sant Longowal Institute of Engineering & Technology, Longowal (Sangrur), Punjab (India)

    2017-06-15

    Highlights: • Total bremsstrahlung spectra in thick targets of Pb compounds by {sup 90}Sr in energy range 10–100 keV. • Experimental results show better agreement with the model which includes PB in SA up to 30 keV. • At higher photon energy region 30–100 keV the model which describes OB is more accurate. • Experimental results show positive deviations from the entire models at higher energy end spectrum. - Abstract: The total bremsstrahlung spectra in the thick targets of lead acetate trihydrate (Pb(CH{sub 3}COO){sub 2}·3H{sub 2}O), lead nitrate Pb(NO{sub 3}){sub 2} and lead chloride (PbCl{sub 2}) produced by {sup 90}Sr beta particles have been investigated in the photon energy region of 10–100 keV. The experimental bremsstrahlung spectra have been compared with the theoretical models Elwert corrected (non relativistic) Bethe Heitler theory, modified Elwert factor (relativistic) Bethe Heitler theory for ordinary bremsstrahlung and modified Elwert factor (relativistic) Bethe Heitler theory which includes polarization bremsstrahlung in the stripped atom approximation. The experimental results show better agreement with theoretical model that includes polarization bremsstrahlung in stripped approximation in the photon energy region below 30 keV. However, at higher photon energy region 30–100 keV, the theoretical model which describes ordinary bremsstrahlung is more accurate to describe the experimental bremsstrahlung spectra. The experimental results show positive deviations from the entire theoretical models at higher energy end of the spectrum. The results indicate that polarization bremsstrahlung plays important role in the formation of total bremsstrahlung spectra in lead compounds produced by continuous beta particles at low photon energy region of 10–30 keV.

  7. Antifungal actinomycetes associated with the pine bark beetle, Orthotomicus erosus, in South Africa

    Directory of Open Access Journals (Sweden)

    Zander R. Human

    2017-01-01

    Full Text Available Actinomycete bacteria are often associated with insects that have a mutualistic association with fungi. These bacteria are believed to be important to this insect–fungus association as they produce antibiotics that exclude other saprophytic fungi from the immediate environment. The aim of this study was to investigate the presence of potentially protective actinomycetes associated with Orthotomicus erosus, an alien invasive pine bark beetle, in South Africa. This bark beetle and its relatives have an association with Ophiostomatales species which are often the only fungi found in the bark beetle galleries. We hypothesised that antibiotic-producing actinomycetes could be responsible for the paucity of other fungi in the galleries by producing compounds to which the Ophiostoma spp. are tolerant. Several actinomycetes in the genus Streptomyces and one Gordonia sp. were isolated from the beetle. Interestingly, most isolates were from the same species as actinomycetes associated with other pine-infesting insects from other parts of the world, including bark beetles and the woodwasp Sirex noctilio. Most actinomycetes isolated had strong antifungal properties against the selected test fungi, including Ophiostoma ips, which is the most common fungal symbiont of Orthotomicus erosus. Although the actinomycetes did not benefit Ophiostoma ips and the hypothesis was not supported, their sporadic association with Orthotomicus erosus suggests that they could have some impact on the composition of the fungal communities present in the bark beetle galleries, which is at present poorly understood.

  8. Synthesis, Single Crystal X-ray Analysis, and Antifungal Profiling of Certain New Oximino Ethers Bearing Imidazole Nuclei

    Directory of Open Access Journals (Sweden)

    Reem I. Al-Wabli

    2017-11-01

    Full Text Available Fungal infections threaten human health, particularly in immune-compromised patients worldwide. Although there are a large number of antifungal agents available, the desired clinical attributes for the treatment of fungal infections have not yet been achieved. Azoles are the mainstay class of the clinically used antifungal agents. In the current study, the synthesis, spectroscopic characterization, and antifungal activity of certain new oximino ethers Va–n bearing imidazole nuclei are reported. The (E-configuration of the imine double bond of the synthesized compounds Va–n has been confirmed via single crystal X-ray analysis of compound Vi as a representative example of this class of compounds. The molecular structure of compound Vi was crystallized in the monoclinic, P21/c, a = 18.7879(14 Å, b = 5.8944(4 Å, c = 16.7621(12 Å, β = 93.063(3°, V = 1855.5(2 Å3, Z = 4. The in vitro antifungal activity of the synthesized compounds Va–n were evaluated using diameter of the inhibition zone (DIZ and minimum inhibitory concentration (MIC assays against different fungal strains. Compound Ve manifested anti-Candida albicans activity with an MIC value of 0.050 µmol/mL, being almost equipotent with the reference antifungal drug fluconazole (FLC,while compounds Vi and Vn are the most active congeners against Candida parapsilosis, being equipotent and about twenty-three times more potent than FLC with an MIC value of 0.002 µmol/mL. The results of the current report might support the development of new potent and safer antifungal azoles.

  9. Biosynthesis of components with antifungal activity against Aspergillus spp. using Streptomyces hygroscopicus

    Directory of Open Access Journals (Sweden)

    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.

  10. USE OF A MICRO TITLE PLATE DILUTION ASSAY TO MEASURE ACTIVITY OF ANTIFUNGAL COMPOUNDS AGAINST Mycosphaerella Fijiensis, MORELET. UTILIZACIÓN DE UN ENSAYO DE DILUCIÓN EN MICROPLATOS PARA MEDIR LA ACTIVIDAD ANTIFÚNGICA DE SUSTANCIAS CONTRA Mycosphaerella fijiensis, MORELET.

    Directory of Open Access Journals (Sweden)

    Jorge Enrique Peláez Montoya

    2006-12-01

    Full Text Available Black Sigatoka, caused by the fungus Mycosphaerella fijiensis is the most important disease in banana plantations. The fungus is controlled mainly by fungicide applications with an annual cost of about 350 million dollars in Latin and Central America. Due to the appearance of resistant strains and to the economical and environmental impact caused by the extensive use of fungicides, accurate methods are necessary for monitoring the fungal sensitivity to these agents. In this paper we describe the standarization of a method based on microplate dilutions that measures IC50 of different antifungal compounds against single ascospore cultures of M. fijiensis. The method was used to measure the sensitivity of 30 strains collected from different regions in Colombia against Propiconazol, Benomyl and Azoxystrobin. Used at a larger scale, this method could be useful to monitor M. fijiensis sensitivity against fungicides and to search for new compounds with activity against the fungus.La Sigatoka negra, causada por el hongo Mycosphaerella fijiensis, es la enfermedad más importante que afecta plantaciones de banano y plátano. El hongo es controlado principalmente mediante fungicidas químicos con un costo anual de cerca de 350 millones de dólares para América latina y 25 millones de dólares para Colombia. Debido al desarrollo de cepas del hongo resistentes a los fungicidas y a las consecuencias que para el medio ambiente tiene su uso intensivo, es importante el desarrollo de métodos que permitan monitorear de una manera precisa la aparición de resistencia. También es de gran utilidad disponer de un método que permita evaluar en forma sencilla la actividad de nuevas sustancias contra el hongo. En este artículo describimos la estandarización de un método basado en diluciones en microplatos que permite determinar la IC50 de diversos compuestos antifungicos contra cultivos monospóricos de M. fijiensis. Para su validación, el método fue utilizado

  11. Aaptamine Derivatives with Antifungal and Anti-HIV-1 Activities from the South China Sea Sponge Aaptos aaptos

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    Hao-Bing Yu

    2014-12-01

    Full Text Available Five new alkaloids of aaptamine family, compounds (1–5 and three known derivatives (6–8, have been isolated from the South China Sea sponge Aaptos aaptos. The structures of all compounds were unambiguously elucidated by spectroscopic analyses, as well as by comparison with the literature data. Compounds 1–2 are characterized with triazapyrene lactam skeleton, whereas compounds 4–5 share an imidazole-fused aaptamine moiety. These compounds were evaluated in antifungal and anti-HIV-1 assays. Compounds 3, 7, and 8 showed antifungal activity against six fungi, with MIC values in the range of 4 to 64 μg/mL. Compounds 7–8 exhibited anti-HIV-1 activity, with inhibitory rates of 88.0% and 72.3%, respectively, at a concentration of 10 μM.

  12. An Interspecies Signaling System Mediated by Fusaric Acid Has Parallel Effects on Antifungal Metabolite Production by Pseudomonas protegens Strain Pf-5 and Antibiosis of Fusarium spp.

    Science.gov (United States)

    Quecine, Maria Carolina; Kidarsa, Teresa A; Goebel, Neal C; Shaffer, Brenda T; Henkels, Marcella D; Zabriskie, T Mark; Loper, Joyce E

    2015-12-11

    Pseudomonas protegens strain Pf-5 is a rhizosphere bacterium that suppresses soilborne plant diseases and produces at least seven different secondary metabolites with antifungal properties. We derived mutants of Pf-5 with single and multiple mutations in biosynthesis genes for seven antifungal metabolites: 2,4-diacetylphoroglucinol (DAPG), pyrrolnitrin, pyoluteorin, hydrogen cyanide, rhizoxin, orfamide A, and toxoflavin. These mutants were tested for inhibition of the pathogens Fusarium verticillioides and Fusarium oxysporum f. sp. pisi. Rhizoxin, pyrrolnitrin, and DAPG were found to be primarily responsible for fungal antagonism by Pf-5. Previously, other workers showed that the mycotoxin fusaric acid, which is produced by many Fusarium species, including F. verticillioides, inhibited the production of DAPG by Pseudomonas spp. In this study, amendment of culture media with fusaric acid decreased DAPG production, increased pyoluteorin production, and had no consistent influence on pyrrolnitrin or orfamide A production by Pf-5. Fusaric acid also altered the transcription of biosynthetic genes, indicating that the mycotoxin influenced antibiotic production by Pf-5 at the transcriptional level. Addition of fusaric acid to the culture medium reduced antibiosis of F. verticillioides by Pf-5 and derivative strains that produce DAPG but had no effect on antibiosis by Pf-5 derivatives that suppressed F. verticillioides due to pyrrolnitrin or rhizoxin production. Our results demonstrated the importance of three compounds, rhizoxin, pyrrolnitrin, and DAPG, in suppression of Fusarium spp. by Pf-5 and confirmed that an interspecies signaling system mediated by fusaric acid had parallel effects on antifungal metabolite production and antibiosis by the bacterial biological control organism. Copyright © 2016, American Society for Microbiology. All Rights Reserved.

  13. Analysis of phenolic compounds for poultry feeds

    Science.gov (United States)

    Phenolic compounds have generated significant interest recently as feed additives that can impart bioactive characteristics such as anti-oxidant, anti-microbial, and anti-fungal properties to a feed formulation [1-2]. Such natural compounds may offer some preventive benefit to the routine administra...

  14. Antibacterial and cytotoxic compounds from the bark of Cananga odorata.

    Science.gov (United States)

    Rahman, M Mukhlesur; Lopa, Simin S; Sadik, Golam; Harun-Or-Rashid; Islam, Robiul; Khondkar, Proma; Alam, A H M Khurshid; Rashid, Mohammad A

    2005-12-01

    O-Methylmoschatoline, liriodenine and 3,4-dihydroxybenzoic acid isolated from the barks of Cananga odorata showed antibacterial activities against a number of Gram (+) and Gram (-) bacteria. The compounds also showed antifungal and cytotoxic activities.

  15. Two new cyclopeptides from the co-culture broth of two marine mangrove fungi and their antifungal activity.

    Science.gov (United States)

    Huang, Song; Ding, Weijia; Li, Chunyuan; Cox, Daniel G

    2014-10-01

    The strategy that co-cultivation two microorganisms in a single confined environment were recently developed to generate new active natural products. In the study, two new cyclic tetrapeptides, cyclo (D-Pro-L-Tyr-L-Pro-L-Tyr) (1) and cyclo (Gly-L-Phe-L-Pro-L-Tyr) (2) were isolated from the co-culture broth of two mangrove fungi Phomopsis sp. K38 and Alternaria sp. E33. Their antifungal activity against Candida albicans, Gaeumannomyces graminis, Rhzioctonia cerealis, Helminthosporium sativum and Fusarium graminearum was evaluated. Different column chromatographic techniques with different solvent systems were used to separate the constituents of the n-butyl alcohol extract of the culture broth. The structures of compounds 1 and 2 were identified by analysis of spectroscopic data (one-dimensional, two-dimensional - nuclear magnetic resonance, mass spectrometry) and Marfey's analytic method. Dilution method was used for the evaluation of antifungal activity. Compounds 1 and 2 were identified as cyclo (D-Pro-L-Tyr-L-Pro-L-Tyr) and cyclo (Gly-L-Phe-L-Pro-L-Tyr), respectively. Compounds 1 and 2 showed moderate to high antifungal activities as compared with the positive control. Compounds 1 and 2 are new cyclopeptides with moderate antifungal activity being worthy of consideration for the development and research of antifungal agents.

  16. Inhibitors of the glyoxylate cycle enzyme ICL1 in Candida albicans for potential use as antifungal agents.

    Directory of Open Access Journals (Sweden)

    Hong-Leong Cheah

    Full Text Available Candida albicans is an opportunistic pathogen that causes candidiasis in humans. In recent years, metabolic pathways in C. albicans have been explored as potential antifungal targets to treat candidiasis. The glyoxylate cycle, which enables C. albicans to survive in nutrient-limited host niches and its. Key enzymes (e.g., isocitrate lyase (ICL1, are particularly attractive antifungal targets for C. albicans. In this study, we used a new screening approach that better reflects the physiological environment that C. albicans cells experience during infection to identify potential inhibitors of ICL. Three compounds (caffeic acid (CAFF, rosmarinic acid (ROS, and apigenin (API were found to have antifungal activity against C. albicans when tested under glucose-depleted conditions. We further confirmed the inhibitory potential of these compounds against ICL using the ICL enzyme assay. Lastly, we assessed the bioavailability and toxicity of these compounds using Lipinski's rule-of-five and ADMET analysis.

  17. In vitro antifungal activities of leaf extracts of Lippia alba (Verbenaceae against clinically important yeast species

    Directory of Open Access Journals (Sweden)

    Graziela Teixeira de Oliveira

    2014-04-01

    Full Text Available Introduction There are few studies reporting the antifungal activities of Lippia alba extracts. Methods A broth microdilution assay was used to evaluate the antifungal effects of Lippia alba extracts against seven yeast species of Candida and Cryptococcus. The butanol fraction was investigated by gas chromatography-mass spectrometry. Results The butanol fraction showed the highest activity against Candida glabrata. The fraction also acted synergistically with itraconazole and fluconazole against C. glabrata. The dominant compounds in the butanol fraction were 2,2,5-trimethyl-3,4-hexanedione, 3,5-dimethyl-4-octanone and hexadecane. Conclusions The butanol fraction may be a good candidate in the search for new drugs from natural products with antifungal activity.

  18. DAYA ANTIFUNGAL DEKOK KAYU MANIS (Cinnamomum burmanni TERHADAP Candida Albicans SECARA IN VITRO

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    Lailia Nur Rachma

    2012-09-01

    Full Text Available Candida albicans is the most oportunis fungi that cause flour albus. Cinnamomum burmanni have been widely known as therapy for flour albus. This efect caused by its chemical compound such as cinnamaldehyde, eugenol, cinnamic acid, limonene, cathecin, coumarin, linalool, and tannin. This research aims was to know the comparison of antifungal potency of Cinnamomum burmanni on Candida albicans in vitro. The design was true experimental. The decoction concentrations of Cinnamomum burmanni that were used were 8%, 4%, 2%, 1%, 0.5%, 0.25%, and 0.125% with three time repetition. The data was analized with One-way ANOVA test with convidence interval 95% (p < 0.05. One-way ANOVA test gave result Cinnamomum burmanni had antifungal potency against Candida albicans. Minimum Inhibitory Concentration (MIC of Cinnamomum burmanni was 1%. Minimum Fungicidal Concentration (MFC of Cinnamomum burmanni was 2%. The conclusion was Cinnamomum burmanni had antifungal potency against Candida albicans in vitro.

  19. Haliscosamine: a new antifungal sphingosine derivative from the Moroccan marine sponge Haliclona viscosa.

    Science.gov (United States)

    El-Amraoui, Belkassem; Biard, Jean-Fançois; Fassouane, Aziz

    2013-01-01

    In the aim of searching for new antifungal products from marine origin, we have isolated a sphingosine derivative, (9Z)-2-amino-docos-9-ene-1,3,13,14-tetraol (Haliscosamine) from the Moroccan sea sponge Haliclona viscosa using bio-guided (antifungal) HPLC methods. The molecular structure of this compound was elucidated by spectrometric techniques IR, UV, MS and NMR. The isolated metabolite showed a significant antifungal activity against Cryptococcus and Candida species and a weak general toxicity in the brine shrimp lethality test. Further research is needed to study its in vivo activity, as well as to elucidate the mechanism underlying its activity in the hope of a future use in medical mycology.

  20. Triterpenoid glycosides from Medicago sativa as antifungal agents against Pyricularia oryzae.

    Science.gov (United States)

    Abbruscato, Pamela; Tosi, Solveig; Crispino, Laura; Biazzi, Elisa; Menin, Barbara; Picco, Anna M; Pecetti, Luciano; Avato, Pinarosa; Tava, Aldo

    2014-11-19

    The antifungal properties of saponin mixtures from alfalfa (Medicago sativa L.) tops and roots, the corresponding mixtures of prosapogenins from tops, and purified saponins and sapogenins against the causal agent of rice blast Pyricularia oryzae isolates are presented. In vitro experiments highlighted a range of activities, depending upon the assayed metabolite. The antifungal effects of the most promising prosapogenin mixture from alfalfa tops were confirmed by means of in planta tests using three different Italian cultivars of rice (Oryza sativa L. ssp. japonica), known to possess high, medium, and low blast resistance. The evidenced antifungal properties of the tested metabolites allowed some considerations on their structure-activity relationship. Results indicate that prosapogenins are active compounds to prevent the fungal attack of P. oryzae on different rice cultivars. Therefore, if properly formulated, these substances could represent a promising and environmentally friendly treatment to control rice blast.

  1. Correlation between the lipophilicity and antifungal activity of some benzoxazole derivatives

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2010-01-01

    Full Text Available In the present work, a quantitative relationship between the lipophilicity and antifungal activity of some benzoxazole derivatives against Candida albicans was investigated by using QSAR (quantitative structure-activity relationship analyses. The descriptors which describe numerically the lipophilicity, logP, were calculated using Chem-Office Software version 7.0. The linear correlation between the minimal inhibitory concentration (log1/cMIC and lipophilicity descriptors was investigated. The best QSAR model predicting the antifungal activity of the investigated series of benzoxazole was developed. The results are discussed on the basis of statistical data. High agreement between theoretical and experimental inhibitory values was obtained. The results of this study indicate that the lipophilicity parameter has a significant effect on antifungal activity of this class of compounds, which can be very useful in the design of new biologically active molecules.

  2. A chemometric approach for prediction of antifungal activity of some benzoxazole derivatives against Candida albicans

    Directory of Open Access Journals (Sweden)

    Podunavac-Kuzmanović Sanja O.

    2012-01-01

    Full Text Available The purpose of the article is to promote and facilitate prediction of antifungal activity of the investigated series of benzoxazoles against Candida albicans. The clinical importance of this investigation is to simplify design of new antifungal agents against the fungi which can cause serious illnesses in humans. Quantitative structure activity relationship analysis was applied on nineteen benzoxazole derivatives. A multiple linear regression (MLR procedure was used to model the relationships between the molecular descriptors and the antifungal activity of benzoxazole derivatives. Two mathematical models have been developed as a calibration models for predicting the inhibitory activity of this class of compounds against Candida albicans. The quality of the models was validated by the leave-one-out technique, as well as by the calculation of statistical parameters for the established model. [Projekat Ministarstva nauke Republike Srbije, br. 172012 i br. 172014

  3. Characterization of volatile constituents of Haplopappus greenei and studies on the antifungal activity against phytopathogens.

    Science.gov (United States)

    Demirci, Betul; Baser, Kemal Husnu Can; Tabanca, Nurhayat; Wedge, David E

    2006-04-19

    Essential oil of Haplopappus greenei A. Gray was obtained by hydrodistillation of aerial parts, which were subsequently analyzed by gas chromatography and gas chromatography-mass spectrometry. Major components were identified as carvacrol (8.7%), beta-pinene (7.6%), trans-pinocarveol (6.2%), and caryophyllene oxide (5.8%), respectively. In total, 104 components representing 84.9% of the investigated essential oil were characterized. Furthermore, the essential oil was evaluated for antimalarial, antimicrobial, and antifungal activities. However, only antifungal activity was observed against the strawberry anthracnose-causing fungal plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides using the direct overlay bioautography assay. Major essential oil components were also evaluated for antifungal activity; the carvacrol standard demonstrated nonselective activity against the three Colletotrichum species and the other compounds were inactive.

  4. Antifungal Edible Coatings for Fresh Citrus Fruit: A Review

    Directory of Open Access Journals (Sweden)

    Lluís Palou

    2015-12-01

    Full Text Available According to their origin, major postharvest losses of citrus fruit are caused by weight loss, fungal diseases, physiological disorders, and quarantine pests. Cold storage and postharvest treatments with conventional chemical fungicides, synthetic waxes, or combinations of them are commonly used to minimize postharvest losses. However, the repeated application of these treatments has led to important problems such as health and environmental issues associated with fungicide residues or waxes containing ammoniacal compounds, or the proliferation of resistant pathogenic fungal strains. There is, therefore, an increasing need to find non-polluting alternatives to be used as part of integrated disease management (IDM programs for preservation of fresh citrus fruit. Among them, the development of novel natural edible films and coatings with antimicrobial properties is a technological challenge for the industry and a very active research field worldwide. Chitosan and other edible coatings formulated by adding antifungal agents to composite emulsions based on polysaccharides or proteins and lipids are reviewed in this article. The most important antifungal ingredients are selected for their ability to control major citrus postharvest diseases like green and blue molds, caused by Penicillium digitatum and Penicillium italicum, respectively, and include low-toxicity or natural chemicals such as food additives, generally recognized as safe (GRAS compounds, plant extracts, or essential oils, and biological control agents such as some antagonistic strains of yeasts or bacteria.

  5. Hydrolysate from a mixture of legume flours with antifungal activity as an ingredient for prolonging the shelf-life of wheat bread.

    Science.gov (United States)

    Rizzello, Carlo Giuseppe; Verni, Michela; Bordignon, Stefano; Gramaglia, Valerio; Gobbetti, Marco

    2017-06-01

    Aiming at identifying antifungal compounds from plant matrices to be used as ingredients in the bakery industry, a water/salt-soluble extract (WSE) was produced from a legume enzyme hydrolysate, consisting of a mixture of pea, lentil, and faba bean flours, and assayed towards Penicillium roqueforti DPPMAF1. Agar diffusion assays allowed the selection of the optimal processing conditions for hydrolysis. As shown by hyphal radial growth rate, the inhibition was observed towards several fungi, including Aspergillus parasiticus CBS971.97, Penicillium carneum CBS 112297, Penicillium paneum CBS 101032, Penicillium polonicum 112490. A multi-step purification was carried out to identify the active compounds. The antifungal activity was attributed to native proteins (nsLTP, ubiquitin, lectin alpha-1 chain, wound-induced basic protein, defensin-1, defensin-2) and a mixture of peptides, which were released during hydrolysis. Nine peptides were purified and identified as sequences encrypted in legume vicilins, lectins and chitinases. WSE was used as ingredient for making bread under pilot plant conditions. Chemical, structural and sensory characterization of bread showed the lack of significant changes compared to control. The bread made with the legume hydrolysate had a longer shelf-life than that of the control. Copyright © 2016 Elsevier Ltd. All rights reserved.

  6. Isolation and biochemical characterization of a novel leguminous defense peptide with antifungal and antiproliferative potency.

    Science.gov (United States)

    Wang, Shaoyun; Rao, Pingfan; Ye, Xiuyun

    2009-02-01

    Leguminous plants have formed a popular subject of research owing to the abundance of proteins and peptides with important biological activities that they produce. The antifungal proteins and peptides have been purified from a number of leguminous species. However, research continues to discover novel antifungal plant-produced peptides and proteins are being needed, specially those novel ones with both antifungal activity and other significant bioactivities. The objective of this study was to isolate a novel peptide from Phaseolus limensis. A 6.8 kDa peptide designated Limyin, with both antifungal and antiproliferative activity, was isolated from the large lima bean (P. limensis) legumes. The isolation procedure consisted of extraction, precipitation, affinity chromatography on Affi-gel blue gel, ion chromatography on SP-Toyopearl, and gel filtration on Superdex 75. Its N-terminal sequence was determined to be KTCENLATYYRGPCF, showing high homology to defensin and defensin precursors from plants. It potently suppressed mycelial growth in Alternaria alternata, Fusarium solani, and Botrytis cinerea. Its antifungal activity was stable up to 80 degrees C. It showed antiproliferative activity towards tumor cells including human liver hepatoma cells Bel-7402 and neuroblastoma cells SHSY5Y. However, it had no effect on bacteria Staphylococcus aureus and Salmonella. The present findings make a significant addition of the research on leguminous plants.

  7. Antifungal dimeric chalcone derivative kamalachalcone E from Mallotus philippinensis.

    Science.gov (United States)

    Kulkarni, Roshan R; Tupe, Santosh G; Gample, Suwarna P; Chandgude, Macchindra G; Sarkar, Dhiman; Deshpande, Mukund V; Joshi, Swati P

    2014-01-01

    From the red coloured extract (Kamala) prepared through acetone extraction of the fresh whole uncrushed fruits of Mallotus philippinensis, one new dimeric chalcone (1) along with three known compounds 1-(5,7-dihydroxy-2,2,6-trimethyl-2H-1-benzopyran-8-yl)-3-phenyl-2-propen-1-one (2), rottlerin (3) and 4'-hydroxyrottlerin (4) were isolated. The structure of compound 1 was elucidated by 1D and 2D NMR analyses that included HSQC, HMBC, COSY and ROESY experiments along with the literature comparison. Compounds 1-4 were evaluated for antifungal activity against different human pathogenic yeasts and filamentous fungi. The antiproliferative activity of the compounds was evaluated against Thp-1 cell lines. Compounds 1 and 2 both exhibited IC50 of 8, 4 and 16 μg/mL against Cryptococcus neoformans PRL518, C. neoformans ATCC32045 and Aspergillus fumigatus, respectively. Compound 4, at 100 μg/mL, showed 54% growth inhibition of Thp-1 cell lines.

  8. Synthesis and antifungal activity of two novel spermidine analogues.

    Science.gov (United States)

    Mackintosh, C A; Slater, L A; McClintock, C A; Walters, D R; Havis, N D; Robins, D J

    1997-03-01

    Two spermidine analogues were synthesised and examined for antifungal activity. Both compounds used as 1 mM post-inoculation sprays reduced infection of barley seedlings by the powdery mildew fungus, Erysiphe graminis f.sp. hordei, infection of broad bean seedlings by the rust fungus, Uromyces viciae-fabae, and infection of apple seedlings by the powdery mildew fungus, Podosphaera leucotricha. Since these fungal pathogens cannot be cultured axenically, the effects of the two spermidine analogues on mycelial growth in vitro, as well as preliminary investigations on polyamine biosynthesis, were undertaken using the oat stripe pathogen, Pyrenophora avenae. Although neither compound affected radial growth of the fungus on plates, both analogues reduced fungal biomass in liquid culture substantially. The two spermidine analogues, used at a concentration of 1 mM, had no significant effect on the conversion of labelled ornithine into polyamines in P. avenae.

  9. Eco-friendly synthesis and potent antifungal activity of 2-substituted coumaran-3-ones

    Directory of Open Access Journals (Sweden)

    PRABHA SOLANKI

    2012-11-01

    Full Text Available Solanki P, Shekhawat P. 2012. Eco-friendly synthesis and potent antifungal activity of 2-substituted coumaran-3-ones. Nusantara Bioscience 4: 101-104. 3-halochromones (IIa-c and IIIa-c have been synthesized by treating 1- (2-hydroxyphenyl-3-methyl-1,3-propanediones (Ia-c with bromine or sulphuryl chloride in dioxane respectively. These chromones were employed in the synthesis of 2-acetyl-coumaran-3-ones (IVa-f. These were subjected to Knoevenagel condensation to give 2-cinnamoyl coumaran-3-ones. In vitro assay and field trials of these compounds against Fusarium oxysporum were carried out to study the antifungal effect of target compounds. Compound Va was the most effective growth inhibitor of the pathogen, whereas Vc showd a little tendency and Vb, Vd, Ve and Vf hardly inhibits the growth

  10. Design, synthesis and antifungal activities of novel strobilurin derivatives containing pyrimidine moieties

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, Xiang; Geo, Yongxin; Liu, Huijun; Guo, Baoyuan; Wang, Huili [Research Center for Eco-Environmental Sciences/Chinese Academy of Sciences, Beijing (China)

    2012-04-15

    Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel β-methoxy acrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, {sup 1}H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbicular, Botrytis cinerea Pers and Protoporphyria caps ici Leon ian at the concentration of 50 μg/mL. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial stilbenetriol fungicide azoxystrobin.

  11. Design, synthesis and antifungal activities of novel strobilurin derivatives containing pyrimidine moieties

    International Nuclear Information System (INIS)

    Zhang, Xiang; Geo, Yongxin; Liu, Huijun; Guo, Baoyuan; Wang, Huili

    2012-01-01

    Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel β-methoxy acrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1 H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbicular, Botrytis cinerea Pers and Protoporphyria caps ici Leon ian at the concentration of 50 μg/mL. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial stilbenetriol fungicide azoxystrobin

  12. Chemical markers and antifungal activity of red propolis from Sergipe, Brazil

    Directory of Open Access Journals (Sweden)

    Lucyana Santos de Mendonça

    2015-06-01

    Full Text Available The aim of this study was to analyze the physicochemical properties and antifungal activities of the red propolis samples from Sergipe, Brazil, and also evaluate their variability throughout the year. The characterization of the hydroalcoholic extract (HPE of the red propolis samples was performed monthly from October 2009 to September 2010. The concentrations of the bioactive compounds varied during the year, but their chromatographic profiles were similar. Four compounds were identified by comparison with authentic standards. Formononetin was one of the predominant compounds in all propolis extracts. In our study, it was observed that all the propolis samples inhibited the growth of Candida species. Multivariate analysis confirmed the variations in chemical composition and color of the HPEs throughout the year. The biological activities of the HPEs were statistically significant (p<0.05, and all samples exhibited antifungal properties.

  13. Microwave Assisted Synthesis, Antifungal Activity, and DFT Study of Some Novel Triazolinone Derivatives

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    Na-Bo Sun

    2015-01-01

    Full Text Available A series of some novel 1,2,4-triazol-5(4H-one derivatives were designed and synthesized under microwave irradiation via multistep reaction. The structures of 1,2,4-triazoles were confirmed by 1H NMR, MS, FTIR, and elemental analysis. The antifungal activities of 1,2,4-triazoles were determined. The antifungal activity results indicated that the compounds 5c, 5f, and 5h exhibited good activity against Pythium ultimum, and the compounds 5b and 5c displayed good activity against Corynespora cassiicola. Theoretical calculation of the compound 5c was carried out with B3LYP/6-31G (d. The full geometry optimization was carried out using 6-31G(d basis set, and the frontier orbital energy and electrostatic potential were discussed, and the structure-activity relationship was also studied.

  14. Antifungal and toxicological activities of compounds from traveller's ...

    African Journals Online (AJOL)

    Different concentrations (i.e. 25 - 200 mg/ml) of the extracts prepared using ethanol; n-Hexane, hot water and cold water were tested against some selected human ... The in vivo effects of the extracts on vital organs such as liver, kidney and some haematological parameters (Pack cell volume, Erythrocyte sedimentation rate, ...

  15. Alternative testing strategies for predicting developmental toxicity of antifungal compound

    NARCIS (Netherlands)

    Li, H.

    2016-01-01

    Determination of safe human exposure levels of chemicals in toxicological risk assessments largely relies on animal toxicity data. In these toxicity studies, the highest number of animals are used for reproductive and developmental toxicity testing. Because of economic and ethical reasons, there

  16. Caerulomycin A- An antifungal compound isolated from marine actinomycetes.

    Digital Repository Service at National Institute of Oceanography (India)

    Ambavane, V.; Tokdar, P.; Parab, R.; Sreekumar, E.S.; Mahajan, G.B.; Mishra, P.D.; DeSouza, L.; Ranadive, P.

    -vitro activity against pa- N N N OH O 1' 2' 6' 1 2 6 7 V. Ambavane et al. 576 thogenic and drug resistant Candida strains. Caerulomycin A was first isolated from S. caeruleus [25] [26] as an antibiotic. Later it was reported to have anti-cancer activity...

  17. Cytotoxic and Antifungal Constituents Isolated from the Metabolites of Endophytic Fungus DO14 from Dendrobium officinale

    Directory of Open Access Journals (Sweden)

    Ling-Shang Wu

    2015-12-01

    Full Text Available Two novel cytotoxic and antifungal constituents, (4S,6S-6-[(1S,2R-1, 2-dihydroxybutyl]-4-hydroxy-4-methoxytetrahydro-2H-pyran-2-one (1, (6S,2E-6-hydroxy-3-methoxy-5-oxodec-2-enoic acid (2, together with three known compounds, LL-P880γ (3, LL-P880α (4, and Ergosta-5,7,22-trien-3b-ol (5 were isolated from the metabolites of endophytic fungi from Dendrobium officinale. The chemical structures were determined based on spectroscopic methods. All the isolated compounds 1–5 were evaluated by cytotoxicity and antifungal effects. Our present results indicated that compounds 1–4 showed notable anti-fungal activities (minimal inhibitory concentration (MIC ≤ 50 μg/mL for all the tested pathogens including Candida albicans, Cryptococcus neoformans, Trichophyton rubrum, Aspergillus fumigatus. In addition, compounds 1–4 possessed notable cytotoxcities against human cancer cell lines of HL-60 cells with the IC50 values of below 100 μM. Besides, compounds 1, 2, 4 and 5 showed strong cytotoxities on the LOVO cell line with the IC50 values were lower than 100 μM. In conclusion, our study suggested that endophytic fungi of D. officinale are great potential resources to discover novel agents for preventing or treating pathogens and tumors.

  18. Production of Volatile Compounds in Reconstituted Milk Reduced-Fat Cheese and the Physicochemical Properties as Affected by Exopolysaccharide-Producing Strain

    Directory of Open Access Journals (Sweden)

    Weijun Wang

    2012-12-01

    Full Text Available The application of the exopolysaccharide-producing strains for improving the texture and technical properties of reduced-fat cheese looks very promising. Streptococcus thermophilus TM11 was evaluated for production of reduced-fat cheese using reconstituted milk powder (CRMP. The physicochemical analysis of fresh and stored cheeses showed that this strain slightly increased moisture content resulting in cheese with higher yield and lower protein content compared to the direct acidified cheese. The volatiles of cheese were determined by SPME and GC equipped with a mass spectrometer. The results indicated that the major compounds included aldehydes, ketones and acids, whereas, alcohols and branched-chain aldehydes that contribute to exciting and harsh flavors were not found in CRMP. By the textural profile analysis, we found the cheese made with S. thermophilus TM11 had lower cohesiveness, resilience and higher adhesiveness than the direct acidified cheese, and had similar hardness. Further, S. thermophilus TM11 greatly changed the protein matrix with more opened cavities according to observation by scanning electron microscopy. Consequently, use of S. thermophilus TM11 could endow CRMP with the novel and suitable flavor properties and improved texture quality.

  19. Isolation of Saccharomyces cerevisiae strains producing higher levels of flavoring compounds for production of "cachaça" the Brazilian sugarcane spirit.

    Science.gov (United States)

    Vicente, Maristela de Araújo; Fietto, Luciano Gomes; Castro, Ieso de Miranda; dos Santos, Ana Nery Gonçalves; Coutrim, Maurício Xavier; Brandão, Rogelio Lopes

    2006-04-15

    In Brazil, spontaneous fermentation and open vessels are still used to produce cachaça (the Brazilian sugarcane spirit) and this fermentation is characterized by mixed cultures with continuous succession of yeast species. This work shows the development of a methodology for isolation of yeasts, particularly Saccharomyces cerevisiae, used in the production of cachaça. According to the proposed strategy, the strains were selected for their ability to adapt to stress conditions encountered during fermentation of the sugarcane juice such as high sucrose concentration; high temperatures and high alcohol concentration; for their capacity to flocculate; and for their higher fermentative ability. For strains with such characteristics, specific procedures were employed to select for 5,5,5-trifluoro-DL-leucine (TFL) and cerulenin-resistant strains, since these characteristics are related to a higher capacity of production of the flavoring compounds isoamyl alcohol and caproic acid, respectively. The effectiveness of such a selection strategy was documented. Taken together, the results obtained present the development of a new strategy to isolate yeast strains with appropriated characteristics to be used in the cachaça industry. Moreover, the results obtained offer an explanation for the great variability in terms of chemical composition found in products obtained even in a single distillery.

  20. Production of volatile compounds in reconstituted milk reduced-fat cheese and the physicochemical properties as affected by exopolysaccharide-producing strain.

    Science.gov (United States)

    Wang, Weijun; Zhang, Lanwei; Li, Yanhua

    2012-12-05

    The application of the exopolysaccharide-producing strains for improving the texture and technical properties of reduced-fat cheese looks very promising. Streptococcus thermophilus TM11 was evaluated for production of reduced-fat cheese using reconstituted milk powder (CRMP). The physicochemical analysis of fresh and stored cheeses showed that this strain slightly increased moisture content resulting in cheese with higher yield and lower protein content compared to the direct acidified cheese. The volatiles of cheese were determined by SPME and GC equipped with a mass spectrometer. The results indicated that the major compounds included aldehydes, ketones and acids, whereas, alcohols and branched-chain aldehydes that contribute to exciting and harsh flavors were not found in CRMP. By the textural profile analysis, we found the cheese made with S. thermophilus TM11 had lower cohesiveness, resilience and higher adhesiveness than the direct acidified cheese, and had similar hardness. Further, S. thermophilus TM11 greatly changed the protein matrix with more opened cavities according to observation by scanning electron microscopy. Consequently, use of S. thermophilus TM11 could endow CRMP with the novel and suitable flavor properties and improved texture quality.

  1. Chemical Variability, Antioxidant and Antifungal Activities of Essential Oils and Hydrosol Extract of Calendula arvensis L. from Western Algeria.

    Science.gov (United States)

    Belabbes, Rania; Dib, Mohammed El Amine; Djabou, Nassim; Ilias, Faiza; Tabti, Boufeldja; Costa, Jean; Muselli, Alain

    2017-05-01

    The chemical composition of the essential oils and hydrosol extract from aerial parts of Calendula arvensis L. was investigated using GC-FID and GC/MS. Intra-species variations of the chemical compositions of essential oils from 18 Algerian sample locations were investigated using statistical analysis. Chemical analysis allowed the identification of 53 compounds amounting to 92.3 - 98.5% with yields varied of 0.09 - 0.36% and the main compounds were zingiberenol 1 (8.7 - 29.8%), eremoligenol (4.2 - 12.5%), β-curcumene (2.1 - 12.5%), zingiberenol 2 (4.6 - 19.8%) and (E,Z)-farnesol (3.5 - 23.4%). The study of the chemical variability of essential oils allowed the discrimination of two main clusters confirming that there is a relation between the essential oil compositions and the harvest locations. Different concentrations of essential oil and hydrosol extract were prepared and their antioxidant activity were assessed using three methods (2,2-diphenyl-1-picrylhydrazyl, Ferric-Reducing Antioxidant Power Assay and β-carotene). The results showed that hydrosol extract presented an interesting antioxidant activity. The in vitro antifungal activity of hydrosol extract produced the best antifungal inhibition against Penicillium expansum and Aspergillus niger, while, essential oil was inhibitory at relatively higher concentrations. Results showed that the treatments of pear fruits with essential oil and hydrosol extract presented a very interesting protective activity on disease severity of pears caused by P. expansum. © 2017 Wiley-VHCA AG, Zurich, Switzerland.

  2. Anti-Candida albicans natural products, sources of new antifungal drugs: A review.

    Science.gov (United States)

    Zida, A; Bamba, S; Yacouba, A; Ouedraogo-Traore, R; Guiguemdé, R T

    2017-03-01

    Candida albicans is the most prevalent fungal pathogen in humans. Due to the development of drug resistance, there is today a need for new antifungal agents for the efficient management of C. albicans infections. Therefore, we reviewed antifungal activity, mechanisms of action, possible synergism with antifungal drugs of all natural substances experimented to be efficient against C. albicans for future. An extensive and systematic review of the literature was undertaken and all relevant abstracts and full-text articles analyzed and included in the review. A total of 111 documents were published and highlighted 142 anti-C. albicans natural products. These products are mostly are reported in Asia (44.37%) and America (28.17%). According to in vitro model criteria, from the 142 natural substances, antifungal activity can be considered as important for 40 (28.20%) and moderate for 24 (16.90%). Sixteen products have their antifungal activity confirmed by in vivo gold standard experimentation. Microbial natural products, source of antifungals, have their antifungal mechanism well described in the literature: interaction with ergosterol (polyenes), inhibition 1,3-β-d-glucan synthase (Echinocandins), inhibition of the synthesis of cell wall components (chitin and mannoproteins), inhibition of sphingolipid synthesis (serine palmitoyltransferase, ceramide synthase, inositol phosphoceramide synthase) and inhibition of protein synthesis (sordarins). Natural products from plants mostly exert their antifungal effects by membrane-active mechanism. Some substances from arthropods are also explored to act on the fungal membrane. Interestingly, synergistic effects were found between different classes of natural products as well as between natural products and azoles. Search for anti-C. albicans new drugs is promising since the list of natural substances, which disclose activity against this yeast is today long. Investigations must be pursued not only to found more new anti

  3. Screening of Azotobacter isolates for PGP properties and antifungal activity

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    Bjelić Dragana Đ.

    2015-01-01

    Full Text Available Аmong 50 bacterial isolates obtained from maize rhizospherе, 13 isolates belonged to the genus Azotobacter. Isolates were biochemically characterized and estimated for pH and halo tolerance ability and antibiotic resistance. According to characterization, the six representative isolates were selected and further screened in vitro for plant growth promoting properties: production of indole-3-acetic acid (IAA, siderophores, hydrogen cyanide (HCN, exopolysaccharides, phosphate solubilization and antifungal activity (vs. Helminthosporium sp., Macrophomina sp., Fusarium sp.. Beside HCN production, PGP properties were detected for all isolates except Azt7. All isolates produced IAA in the medium without L-tryptophan and the amount of produced IAA increased with concentration of precursor in medium. The highest amount of IAA was produced by isolates Azt4 (37.69 and 45.86 μg ml-1 and Azt5 (29.44 and 50.38 μg ml-1 in the medium with addition of L-tryptophan (2.5 and 5 mM. The isolates showed the highest antifungal activity against Helminthosporium sp. and the smallest antagonistic effect on Macrophomina sp. Radial Growth Inhibition (RGI obtained by the confrontation of isolates with tested phytopathogenic fungi, ranged from 10 to 48%. [Projekat Ministarstva nauke Republike Srbije, br. TR 31073

  4. In vitro antifungal activity of four chemotypes of Lippia alba (Verbenaceae essential oils against Alternaria solani (Pleosporeaceae isolates

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    ELISA Z. TOMAZONI

    2016-06-01

    Full Text Available Several volatile natural compounds produced by plant secondary metabolism have been proven to present antimicrobial action, enabling their use in phytopathogen control. They also present low environmental impact when compared to conventional pesticides. Essential oils contain these compounds and can be found in several plant species, such as Lippia alba (Mill. N.E. Brown (Verbenaceae. Essential oils of four chemotypes of L. alba, characterized by their major compounds, namely camphor, citral, linalool and camphor/1,8-cineole, were tested against the phytopathogen Alternaria solani Sorauer (Pleosporaceae, which causes early blight on tomatoes and is responsible for great economic losses regarding production. Essential oils antifungal action was tested in vitro using potato dextrose agar medium with essential oil concentrations at 0.1, 0.5, 1.0, 1.5 and 2.0 µL mL-1. The chemotype that had the best performance was citral, showing significant inhibition compared to the others, starting at the 0.5 µL mL-1 concentration. The essential oil belonging to the linalool chemotype was efficient starting at the 1.5 µL mL-1 concentration. Conversely, the camphor chemotype did not show any action against the phytopathogen. Moreover, the essential oils had no remarkable effect on tomato germination and growth. In conclusion, these essential oils presented fungicidal action against A. solani.

  5. Production of a defensin-like antifungal protein NFAP from Neosartorya fischeri in Pichia pastoris and its antifungal activity against filamentous fungal isolates from human infections.

    Science.gov (United States)

    Virágh, Máté; Vörös, Dóra; Kele, Zoltán; Kovács, Laura; Fizil, Ádám; Lakatos, Gergely; Maróti, Gergely; Batta, Gyula; Vágvölgyi, Csaba; Galgóczy, László

    2014-02-01

    Neosartorya fischeri NRRL 181 isolate secretes a defensin-like antifungal protein (NFAP) which has a remarkable antifungal effect against ascomycetous filamentous fungi. This protein is a promising antifungal agent of biotechnological value; however in spite of the available knowledge of the nature of its 5'-upstream transcriptional regulation elements, the bulk production of NFAP has not been resolved yet. In this study we carried out its heterologous expression in the yeast Pichia pastoris and investigated the growth inhibition effect exerted by the heterologous NFAP (hNFAP) on filamentous fungal isolates from human infections compared with what was caused by the native NFAP. P. pastoris KM71H transformant strain harboring the pPICZαA plasmid with the mature NFAP encoding gene produced the protein. The final yield of the hNFAP was sixfold compared to the NFAP produced by N. fischeri NRRL 181. Based on the signal dispersion of the amide region, it was proven that the hNFAP exists in folded state. The purified hNFAP effectively inhibited the growth of fungal isolates belonging to the Aspergillus and to the Fusarium genus, but all investigated zygomycetous strain proved to be insusceptible. There was no significant difference between the growth inhibition effect exerted by the native and the heterologous NFAP. These data indicated that P. pastoris KM71H can produce the NFAP in an antifungally active folded state. Our results provide a base for further research, e.g., investigation the connection between the protein structure and the antifungal activity using site directed mutagenesis. Copyright © 2013 Elsevier Inc. All rights reserved.

  6. An in vitro study of the antifungal activity of Trichoderma virens 7b and a profile of its non-polar antifungal components released against Ganoderma boninense.

    Science.gov (United States)

    Angel, Lee Pei Lee; Yusof, Mohd Termizi; Ismail, Intan Safinar; Ping, Bonnie Tay Yen; Mohamed Azni, Intan Nur Ainni; Kamarudin, Norman Hj; Sundram, Shamala

    2016-11-01

    Ganoderma boninense is the causal agent of a devastating disease affecting oil palm in Southeast Asian countries. Basal stem rot (BSR) disease slowly rots the base of palms, which radically reduces productive lifespan of this lucrative crop. Previous reports have indicated the successful use of Trichoderma as biological control agent (BCA) against G. boninense and isolate T. virens 7b was selected based on its initial screening. This study attempts to decipher the mechanisms responsible for the inhibition of G. boninense by identifying and characterizing the chemical compounds as well as the physical mechanisms by T. virens 7b. Hexane extract of the isolate gave 62.60% ± 6.41 inhibition against G. boninense and observation under scanning electron microscope (SEM) detected severe mycelial deformation of the pathogen at the region of inhibition. Similar mycelia deformation of G. boninense was observed with a fungicide treatment, Benlate ® indicating comparable fungicidal effect by T. virens 7b. Fraction 4 and 5 of hexane active fractions through preparative thin layer chromatography (P-TLC) was identified giving the best inhibition of the pathogen. These fractions comprised of ketones, alcohols, aldehydes, lactones, sesquiterpenes, monoterpenes, sulphides, and free fatty acids profiled through gas chromatography mass spectrometry detector (GC/MSD). A novel antifungal compound discovery of phenylethyl alcohol (PEA) by T. virens 7b is reported through this study. T. virens 7b also proved to be an active siderophore producer through chrome azurol S (CAS) agar assay. The study demonstrated the possible mechanisms involved and responsible in the successful inhibition of G. boninense.

  7. Structure-Antifungal Activity Relationship of Fluorinated Dihydroguaiaretic Acid Derivatives and Preventive Activity against Alternaria alternata Japanese Pear Pathotype.

    Science.gov (United States)

    Nishiwaki, Hisashi; Nakazaki, Shoko; Akiyama, Koichi; Yamauchi, Satoshi

    2017-08-09

    The structure-activity relationship of the antifungal fluorinated dihydroguaiaretic acid derivatives was evaluated. Some of the newly synthesized lignan compounds were found to show higher antifungal activity against phytopathogenic fungi such as Alternaria alternata (Japanese pear and apple pathotypes) and A. citri than the lead compound, 3-fluoro-3'-methoxylignan-4'-ol (3). The broad antifungal spectrum of 3'-hydroxyphenyl derivative 16 was observed, and the 3'-fluoro-4'-hydroxyphenyl derivative 38 was found to show the highest activity against the A. alternata Japanese pear pathotype, with an EC 50 value of 11 μM. The preventive effect of the potent lignan on the infection of A. alternata in the Japanese pear's leaves was also shown.

  8. Gene Expression Response of Trichophyton rubrum during Coculture on Keratinocytes Exposed to Antifungal Agents

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    Tatiana Takahasi Komoto

    2015-01-01

    Full Text Available Trichophyton rubrum is the most common causative agent of dermatomycoses worldwide, causing infection in the stratum corneum, nails, and hair. Despite the high prevalence of these infections, little is known about the molecular mechanisms involved in the fungal-host interaction, particularly during antifungal treatment. The aim of this work was to evaluate the gene expression of T. rubrum cocultured with keratinocytes and treated with the flavonoid trans-chalcone and the glycoalkaloid α-solanine. Both substances showed a marked antifungal activity against T. rubrum strain CBS (MIC = 1.15 and 17.8 µg/mL, resp.. Cytotoxicity assay against HaCaT cells produced IC50 values of 44.18 to trans-chalcone and 61.60 µM to α-solanine. The interaction of keratinocytes with T. rubrum conidia upregulated the expression of genes involved in the glyoxylate cycle, ergosterol synthesis, and genes encoding proteases but downregulated the ABC transporter TruMDR2 gene. However, both antifungals downregulated the ERG1 and ERG11, metalloprotease 4, serine proteinase, and TruMDR2 genes. Furthermore, the trans-chalcone downregulated the genes involved in the glyoxylate pathway, isocitrate lyase, and citrate synthase. Considering the urgent need for more efficient and safer antifungals, these results contribute to a better understanding of fungal-host interactions and to the discovery of new antifungal targets.

  9. Quantitative and qualitative analysis of the antifungal activity of allicin alone and in combination with antifungal drugs.

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    Young-Sun Kim

    Full Text Available The antifungal activity of allicin and its synergistic effects with the antifungal agents flucytosine and amphotericin B (AmB were investigated in Candida albicans (C. albicans. C. albicans was treated with different conditions of compounds alone and in combination (allicin, AmB, flucytosine, allicin + AmB, allicin + flucytosine, allicin + AmB + flucytosine. After a 24-hour treatment, cells were examined by scanning electron microscopy (SEM and atomic force microscopy (AFM to measure morphological and biophysical properties associated with cell death. The clearing assay was conducted to confirm the effects of allicin. The viability of C. albicans treated by allicin alone or with one antifungal drug (AmB, flucytosine in addition was more than 40% after a 24-hr treatment, but the viability of groups treated with combinations of more than two drugs was less than 32%. When the cells were treated with allicin alone or one type of drug, the morphology of the cells did not change noticeably, but when cells were treated with combinations of drugs, there were noticeable morphological changes. In particular, cells treated with allicin + AmB had significant membrane damage (burst or collapsed membranes. Classification of cells according to their cell death phase (CDP allowed us to determine the relationship between cell viability and treatment conditions in detail. The adhesive force was decreased by the treatment in all groups compare to the control. Cells treated with AmB + allicin had a greater adhesive force than cells treated with AmB alone because of the secretion of molecules due to collapsed membranes. All cells treated with allicin or drugs were softer than the control cells. These results suggest that allicin can reduce MIC of AmB while keeping the same efficacy.

  10. Screening of antifungal agents using ethanol precipitation and bioautography of medicinal and food plants.

    Science.gov (United States)

    Schmourlo, Gracilene; Mendonça-Filho, Ricardo R; Alviano, Celuta Sales; Costa, Sônia S

    2005-01-15

    In the search for bioactive compounds, bioautography and ethanol precipitation of macromolecules (proteins, polysaccharides, etc.) of plant aqueous extracts were associated in an antifungal screening. Thus, the supernatants, precipitates (obtained by ethanol precipitation) and aqueous extracts were investigated of medicinal and fruit bearing plants used against skin diseases by the Brazilian population. The agar diffusion and broth dilution methods were used to assess the activity against three fungi: Candida albicans, Trichophyton rubrum and Cryptococcus neoformans. The results, evaluated by the diameter of the inhibition zone of fungal growth, indicate that six plant species, among the 16 investigated, showed significant antifungal activity. The minimal inhibitory concentration (MIC) was determined on plant extracts that showed high efficacy against the tested microorganisms. The most susceptible yeast was Trichophyton rubrum and the best antifungal activity was shown by Xanthosoma sagittifolium supernatant. The bioautography was performed only for the aqueous extracts and supernatants of those plants that showed antifungal activity against Candida albicans and Cryptococcus neoformans, using n-butanol/acetic acid/water (BAW) 8:1:1 to develop silica gel TLC plates. Clear inhibition zones were observed for aqueous extracts of Schinus molle (R(f) 0.89) and Schinus terebinthifolius (R(f) 0.80) against Candida albicans, as for supernatant of Anacardium occidentale (R(f) 0.31) against Cryptococcus neoformans. The separation of macromolecules from metabolites, as in the case of Anacardium occidentale, Solanum sp. and Xanthosoma sagittifolium, enhances antifungal activity. In other cases, the antifungal activity is destroyed, as observed for Momordica charantia, Schinus molle and Schinus terebinthifolius.

  11. Efficacy of antimicrobial compounds on surface decontamination of seven shiga toxin-producing Escherichia coli (STEC) and Salmonella inoculated onto fresh beef

    Science.gov (United States)

    Several antimicrobial compounds have been implemented in commercial meat processing plants for decontamination of pathogens on beef carcasses, but there are many commercially available, novel antimicrobial compounds that may be more effective and suitable to be implemented in beef processing pathoge...

  12. Synthesis and antifungal activity of halogenated aromatic bis-γ-lactones analogous to avenaciolide

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    Pedro A. Castelo-Branco

    2012-01-01

    Full Text Available Here we describe the total syntheses and characterization by elemental analyses, infrared and NMR spectroscopy of three new compounds analogous to avenaciolide, a bis-γ-lactone isolated from Aspergillus avenaceus that possesses antifungal activity, where the octyl group of the natural product was replaced by aromatic groups containing chlorine and fluorine atoms. The effects of the avenaciolide, the novel compounds and their synthetic precursors on mycelia development and conidia germination of Colletotrichum gloeosporioides and Fusarium solani were evaluated in vitro. The title compounds were almost as active as avenaciolide. The absolute structures of the chlorinated analogs were determined by X-ray diffraction analysis.

  13. Synthesis and antifungal activity of new bis-{gamma}-lactones analogous to avenaciolide

    Energy Technology Data Exchange (ETDEWEB)

    Magaton, Andreia da Silva; Rubinger, Mayura M. M.; Macedo Junior, Fernando C. de [Vicosa Univ., MG (Brazil). Dept. de Quimica]. E-mail: mayura@ufv.br; Zambolim, Laercio [Vicosa Univ., MG (Brazil). Dept. de Fitopatologia

    2007-03-15

    In a study of the antifungal activity of selected compounds as potentials agrochemicals, we have prepared and characterized by elemental analyses, infrared and NMR spectroscopies three new bis-{gamma}-lactones analogous to avenaciolide, where the octyl group of this natural product was replaced by heptyl, hexyl and pentyl groups. The effects on the mycelia development and conidia germination of Colletotrichum gloesporioides of these compounds and their synthetic precursors were evaluated in vitro. The title compounds were active in the tested conditions, while all the synthetic precursors were inactive. The preparation and characterization of 15 new synthetic intermediates are also described. (author)

  14. The effect of pH on the formation of volatile compounds produced by heating a model system containing 5?-Imp and cysteine

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    Madruga Marta Suely

    1998-01-01

    Full Text Available The identification of volatile compounds formed from the reactions of Inosine-5?-Monophosphate (5?-IMP with Cysteine at three different pH (3.0; 4.5; 6.0 and 140 °C were performed using dynamic headspace analysis. The results gave over 90 volatile compounds, mainly heterocyclic compounds, including sulphur containing furans, thiophenes, thiazoles, furans, alkyl sulphides, bicyclic compounds and cyclic sulphides. The studies showed that sulphur-substituted furans, mercaptoketones and alkylfurans were formed mainly at acidic pH, while pyrazines were completely inhibited at high pH. These findings support an earleir observation that pH has a great influence on volatile compounds formed in Maillard type reactions.

  15. Antifungal agents. 10. New derivatives of 1-[(aryl)[4-aryl-1H-pyrrol-3-yl]methyl]-1H-imidazole, synthesis, anti-candida activity, and quantitative structure-analysis relationship studies.

    Science.gov (United States)

    Tafi, Andrea; Costi, Roberta; Botta, Maurizio; Di Santo, Roberto; Corelli, Federico; Massa, Silvio; Ciacci, Andrea; Manetti, Fabrizio; Artico, Marino

    2002-06-20

    The synthesis, anti-Candida activity, and quantitative structure-activity relationship (QSAR) studies of a series of 2,4-dichlorobenzylimidazole derivatives having a phenylpyrrole moiety (related to the antibiotic pyrrolnitrin) in the alpha-position are reported. A number of substituents on the phenyl ring, ranging from hydrophobic (tert-butyl, phenyl, or 1-pyrrolyl moiety) to basic (NH(2)), polar (CF(3), CN, SCH(3), NO(2)), or hydrogen bond donors and acceptor (OH) groups, were chosen to better understand the interaction of these compounds with cytochrome P450 14-alpha-lanosterol demethylase (P450(14DM)). Finally, the triazole counterpart of one of the imidazole compounds was synthesized and tested to investigate influence of the heterocyclic ring on biological activity. The in vitro antifungal activities of the newly synthesized azoles 10p-v,x-c' were tested against Candida albicans and Candida spp. at pH 7.2 and pH 5.6. A CoMFA model, previously derived for a series of antifungal agents belonging to chemically diverse families related to bifonazole, was applied to the new products. Because the results produced by this approach were not encouraging, Catalyst software was chosen to perform a new 3D-QSAR study. Catalyst was preferred this time because of the possibility of considering each compound as a collection of energetically reasonable conformations and of considering alternative stereoisomers. The pharmacophore model developed by Catalyst, named HYPO1, showed good performances in predicting the biological activity data, although it did not exhibit an unequivocal preference for one enantiomeric series of inhibitors relative to the other. One aromatic nitrogen with a lone pair in the ring plane (mapped by all of the considered compounds) and three aromatic ring features were recognized to have pharmacophoric relevance, whereas neither hydrogen bond acceptor nor hydrophobic features were found. These findings confirmed that the key interaction of azole

  16. Screening of antifungal azole drugs and agrochemicals with an adapted alamarBlue-based assay demonstrates antibacterial activity of croconazole against Mycobacterium ulcerans.

    Science.gov (United States)

    Scherr, Nicole; Röltgen, Katharina; Witschel, Matthias; Pluschke, Gerd

    2012-12-01

    An alamarBlue-based growth inhibition assay has been adapted for the thermosensitive and slow-growing pathogen Mycobacterium ulcerans. The standardized test procedure enables medium-throughput screening of preselected compound libraries. Testing of a set of 48 azoles with known antifungal activity led to the identification of an imidazole antifungal displaying an inhibitory dose (ID) of 9 μM for M. ulcerans.

  17. Study of antimicrobial effect of novel Quaternary Ammonium Compounds on bacteria and fungi

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    Maryam Sadrnia

    2014-10-01

    Full Text Available Background: Quarterly Ammonium Compounds (QuAC are the more effective antimicrobial agents in medicine and industry. It needs to produce the new compounds with the wider spectrum and less toxicity, because of microbial resistance. Aim of this study was microbiological Evaluation of the new Quarterly Ammonium Compounds produced by Structural modifications on some bacteria, yeast and fungi. Material and Methods: 16 Quat salts were designed and made in Ethanol or Aceto Nitril. Minimum Inhibitory Concentration (MIC was determined by standard method on Nutrient Broth and Minimal agar culture media for bacteria , Potato Dextrose Agar (PDA for fungi and Nutrient Agar and Saboro Dextrose Agar (SDA for yeasts . Results: Compounds 2,7,8,9,12,13 has the more antimicrobial effect ( minimum of MIC. Furthermore, it was shown that MIC was unrelated to culture compounds. In yeast culture it must to increases the concentration in enriched media. Compounds 9,12 and 13 has the more antibacterial effect as well as antifungal effect. Conclusion: In comparison of structure of produced compounds and results of the study, it was revealed that radical R3 has the most important role in antimicrobial properties of Quats and it could to be substitute any suitable group related to increasing anti microbial effects.

  18. Bioactive compounds from northern plants.

    Science.gov (United States)

    Hohtola, Anja

    2010-01-01

    Northern conditions are characterised by long days with much light and low temperatures during the growing season. It has been chimed that herbs and berries grown in the north are stronger tasting compared to those of southern origin. The compounds imparting aroma and color to berries and herbs are secondary metabolites which in plants mostly act as chemical means of defense. Recently, the production of secondary metabolites using plant cells has been the subject of expanding research. Light intensity, photoperiod and temperature have been reported to influence the biosynthesis of many secondary metabolites. Native wild aromatic and medicinal plant species of different families are being studied to meet the needs of raw material for the expanding industry of e.g., health-promoting food products known as nutraceutics. There are already a large number of known secondary compounds produced by plants, but the recent advances in modern extraction and analysis should enable many more as yet unknown compounds to be found, characterised and utilised. Rose root (Rhodiola rosea) is a perennial herbaceous plant which inhabits mountain regions throughout Europe, Asia and east coastal regions of North America. The extract made from the rhizomes acts as a stimulant like the Ginseng root. Roseroot has been categorized as an adaptogen and is reported to have many pharmacological properties. The biologically active components of the extract are salitroside tyrosol and cinnamic acid glycosides (rosavin, rosarin, rosin). Round-leaved sundew (Drosera rotundifolia L.) has circumboreal distribution. It inhabits nutrient-poor, moist and sunny areas such as peat bogs and wetlands. Sundew leaves are collected from the wild-type for various medicinal preparations and can be utilized in treating e.g., as an important "cough-medicine" for different respiratory diseases. The antimicrobial activity of extracts of aerial parts against various bacteria has been investigated. Drosera produces

  19. In vitro antifungal activity of bacteria against Mycosphaerella fijiensis mediated by diffused and volatile metabolites

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    Mileidy Cruz-Martín

    2012-07-01

    Full Text Available Antagonistic microorganisms do not have a unique mode of action. Multiplicity of these is an important feature for selection as biological control agents. Black Sigatoka is considered the foliar disease with most economic impact for the banana industry worldwide. New strategies to control it are required to reduce the use of fungicides. That is why an increasing interest to find biological alternatives, such as the use of antagonistic bacteria, has risen. Assays wer e carr ied ou t to determine whether in v it r o ant if ungal ac ti vity of 20 bacterial str ai ns against My cosphaer ella fijiensis was caused by metabolites diffused into the culture medium or volatile. Results demonstrated that 80.0% of bacterial strains tested showed in vitro antifungal activity by diffused metabolites in the culture medium and 60.0% by producing volatile metabolites. The 55.0% of strains showed both mechanisms. This feature makes these bacteria the best candidate for its selection as biological control agent. Keywords: antagonistic, biocontrol, volatile compounds, diffused metabolites.

  20. Augmenting the activity of antifungal agents against aspergilli using structural analogues of benzoic acid as chemosensitizing agents.

    Science.gov (United States)

    Kim, Jong H; Campbell, Bruce C; Mahoney, Noreen; Chan, Kathleen L; Molyneux, Russell J; Balajee, Arunmozhi

    2010-10-01

    A number of benzoic acid analogues showed antifungal activity against strains of Aspergillus flavus, Aspergillus fumigatus and Aspergillus terreus, causative agents of human aspergillosis, in in vitro bioassays. Structure-activity analysis revealed that antifungal activities of benzoic and gallic acids were increased by addition of a methyl, methoxyl or chloro group at position 4 of the aromatic ring, or by esterification of the carboxylic acid with an alkyl group, respectively. Thymol, a natural phenolic compound, was a potent chemosensitizing agent when co-applied with the antifungal azole drugs fluconazole and ketoconazole. The thymol-azole drug combination demonstrated complete inhibition of fungal growth at dosages far lower than the drugs alone. Co-application of thymol with amphotericin B had an additive effect on all strains of aspergilli tested with the exception of two of three strains of A. terreus, where there was an antagonistic effect. Use of two mitogen-activated protein kinase (MAPK) mutants of A. fumigatus, sakAΔ and mpkCΔ, having gene deletions in the oxidative stress response pathway, indicated antifungal and/or chemosensitization activity of the benzo analogues was by disruption of the oxidative stress response system. Results showed that both these genes play overlapping roles in the MAPK system in this fungus. The potential of safe, natural compounds or analogues to serve as chemosensitizing agents to enhance efficacy of commercial antifungal agents is discussed. Published by Elsevier Ltd.

  1. Drug-drug interactions of antifungal agents and implications for patient care.

    Science.gov (United States)

    Gubbins, Paul O; Amsden, Jarrett R

    2005-10-01

    Drug interactions in the gastrointestinal tract, liver and kidneys result from alterations in pH, ionic complexation, and interference with membrane transport proteins and enzymatic processes involved in intestinal absorption, enteric and hepatic metabolism, renal filtration and excretion. Azole antifungals can be involved in drug interactions at all the sites, by one or more of the above mechanisms. Consequently, azoles interact with a vast array of compounds. Drug-drug interactions associated with amphotericin B formulations are predictable and result from the renal toxicity and electrolyte disturbances associated with these compounds. The echinocandins are unknown cytochrome P450 substrates and to date are relatively devoid of significant drug-drug interactions. This article reviews drug interactions involving antifungal agents that affect other agents and implications for patient care are highlighted.

  2. A new antifungal phenolic glycoside derivative, iridoids and lignans from Alibertia sessilis (vell.) K. Schum. (Rubiaceae)

    Energy Technology Data Exchange (ETDEWEB)

    Silva, Viviane C. da; Bolzani, Vanderlan da S.; Lopes, Marcia N. [UNESP, Araraquara, SP (Brazil). Inst. de Quimica. Dept. de Quimica Organica]. E-mail: mnlopes@iq.unesp.br; Young, Maria C.M. [Instituto de Botanica, Sao Paulo, SP (Brazil). Secao de Fisiologia e Bioquimica de Plantas

    2007-07-01

    A new antifungal phenolic glycoside, 3,4,5-trimethoxyphenyl-1-O-{beta}-D-(5-O-syringoyl)apiofuranosyl-(1 {yields} 6)-{beta}-D-glucopyranoside (1), together with four known iridoids, geniposidic acid (2), geniposide (3), 6{alpha}-hydroxygeniposide (4) and 6{beta}-hydroxygeniposide (5); two lignans, (+)-lyoniresinol-3{alpha}-O-{beta}-D-glucopyranoside (6), (-)-lyoniresinol-3{alpha}-O-{beta}-D-glucopyranoside (7); and two phenolic acids, chlorogenic (8) and salicylic acids (9) and D-manitol (10), were isolated from the ethanolic extract of the stems of Alibertia sessilis. Structures of 1 and of the known compounds were determined by spectroscopic analysis. All compounds isolated were evaluated for their antifungal activities against two phytopathogenic fungi strains Cladosporium cladosporioides and C. sphaerospermum by direct bioautography. (author)

  3. A new antifungal phenolic glycoside derivative, iridoids and lignans from Alibertia sessilis (vell.) K. Schum. (Rubiaceae)

    International Nuclear Information System (INIS)

    Silva, Viviane C. da; Bolzani, Vanderlan da S.; Lopes, Marcia N.; Young, Maria C.M.

    2007-01-01

    A new antifungal phenolic glycoside, 3,4,5-trimethoxyphenyl-1-O-β-D-(5-O-syringoyl)apiofuranosyl-(1 → 6)-β-D-glucopyranoside (1), together with four known iridoids, geniposidic acid (2), geniposide (3), 6α-hydroxygeniposide (4) and 6β-hydroxygeniposide (5); two lignans, (+)-lyoniresinol-3α-O-β-D-glucopyranoside (6), (-)-lyoniresinol-3α-O-β-D-glucopyranoside (7); and two phenolic acids, chlorogenic (8) and salicylic acids (9) and D-manitol (10), were isolated from the ethanolic extract of the stems of Alibertia sessilis. Structures of 1 and of the known compounds were determined by spectroscopic analysis. All compounds isolated were evaluated for their antifungal activities against two phytopathogenic fungi strains Cladosporium cladosporioides and C. sphaerospermum by direct bioautography. (author)

  4. Synergistic activity of antifungal drugs and lipopeptide AC7 against Candida albicans biofilm on silicone

    Directory of Open Access Journals (Sweden)

    Chiara Ceresa

    2017-04-01

    Full Text Available The occurrence of Candida albicans device-associated infections is tightly correlated to the ability of this fungus to form biofilms. The presence of this three-dimensional structure protects cells from host defenses, and significantly increases their resistance to antifungal agents. Lipopeptide biosurfactants are microbial products with interesting antibacterial, antifungal and anti-adhesive properties. Aim of the present study was to investigate a possible synergistic effect of lipopeptide AC7BS in combination with amphotericin B or fluconazole against C. albicans planktonic cells, biofilm formation and 24 h-old biofilms on medical-grade silicone elastomer disks, in simulated physiological conditions. In co-incubation experiments, AC7BS alone was not effective. However, the combination of AC7BS with the antifungal compounds resulted in a synergistic increase in the efficacy of the drugs against planktonic cells and biofilm, leading to a reduction of MICs and SMICs50. In pre-coating conditions, amphotericin B alone and AC7BS alone significantly inhibited C. albicans biofilms. When the two molecules were tested in association, a synergistic effect was observed on different phases of biofilm formation and a lower SMIC50 was detected. The observed synergism could be related to the combination of the AC7BS anti-adhesive activity and the AMB antifungal effect, but also to the ability of the biosurfactant to affect membranes, thus facilitating AMB entry in the cells. These results suggest that AC7BS can be considered a potential inhibitor of C. albicans biofilm on medical insertional materials and its use as coating agent may potentiate the effect of antifungal compounds such as AMB, when applied in combination.

  5. Antifungal potential of Avicennia schaueriana Stapf & Leech. (Acanthaceae) against Cladosporium and Colletotrichum species.

    Science.gov (United States)

    Fardin, K M; Young, M C M

    2015-07-01

    There is significant interest in research to develop plant extracts with fungicidal activities that are less harmful to the environment and human health than synthetic fungicides. This study aimed to evaluate the antifungal activity of the extracts of Avicennia schaueriana against Colletotrichum and Cladosporium species and to identify the compounds responsible for the activity. Leaves and stems of A. schaueriana were extracted with ethanol and partitioned with petroleum ether, chloroform and ethyl acetate. The antifungal activity of such extracts was tested by bioautography against Cladosporium sphaerospermum, Cladosporium cladosporioides and Colletotrichum lagenarium. Ethanolic extracts, petroleum ether and chloroform fractions of stems had the highest antifungal activity with several active bands (Rf = 0·72 and Rf = 0·55). In the agar dilution assay, ethanolic extract, petroleum ether and chloroform fractions of stems were the most efficacious, presenting 85, 62 and 63% growth inhibition of Colletotrichum gloeopsporioides and minimum inhibitory concentration values between 1 and 1·5 mg ml(-1) , respectively. Analysis carried out using gas chromatography coupled to a mass spectrometry of petroleum ether and chloroform fractions allowed the identification of fatty acids methyl esters, lupeol and naphthoquinones such as lapachol, α-lapachone, naphtho[2,3-b]furan-4,9-dione, 2-isopropyl- and avicenol-C. We may infer that the antifungal activity of A. schaueriana is due to the abundance of these compounds. This study shows that Avicennia schaueriana extracts have a high potential for the growth inhibition of Colletotrichum and Cladosporium ssp. and will provide a starting point for discovering new natural products with antifungal activity. Their development is of particular interest to organic production systems where synthetic fungicides cannot be used. © 2015 The Society for Applied Microbiology.

  6. Syntheses, in vitro antibacterial and antifungal activities of a series of N-alkyl, 1,4-dithiines.

    Science.gov (United States)

    Zentz, F; Labia, R; Sirot, D; Faure, O; Grillot, R; Valla, A

    2005-01-01

    A series of dithiines were synthesized by cyclization of 4-(alkylamino)-4-oxobutanoic acids under the action of SOCl2. Their in vitro antibacterial and antifungal activities have been evaluated against reference strains and versus reference compounds. The so-called 'isoimides' 2a, 2b were totally inactive whereas some imides had low MICs for few bacteria and for few fungal microorganisms.

  7. Antifungal activity of gold nanoparticles prepared by solvothermal method

    Energy Technology Data Exchange (ETDEWEB)

    Ahmad, Tokeer, E-mail: tahmad3@jmi.ac.in [Nanochemistry Laboratory, Department of Chemistry, Jamia Millia Islamia, New Delhi 110025 (India); Wani, Irshad A.; Lone, Irfan H.; Ganguly, Aparna [Nanochemistry Laboratory, Department of Chemistry, Jamia Millia Islamia, New Delhi 110025 (India); Manzoor, Nikhat; Ahmad, Aijaz [Department of Biosciences, Jamia Millia Islamia, New Delhi 110025 (India); Ahmed, Jahangeer [Department of Chemistry, Michigan State University, East Lansing, MI 48824 (United States); Al-Shihri, Ayed S. [Department of Chemistry, Faculty of Science, King Khalid University, Abha 61413, P.O. Box 9004 (Saudi Arabia)

    2013-01-15

    Graphical abstract: Gold nanoparticles (7 and 15 nm) of very high surface area (329 and 269 m{sup 2}/g) have been successfully synthesized through solvothermal method by using tin chloride and sodium borohydride as reducing agents. As-prepared gold nanoparticles shows very excellent antifungal activity against Candida isolates and activity increases with decrease in the particle size. Display Omitted Highlights: ► Effect of reducing agents on the morphology of gold nanoparticles. ► Highly uniform and monodisperse gold nanoparticles (7 nm). ► Highest surface area of gold nanoparticles (329 m{sup 2/}g). ► Excellent antifungal activity of gold nanoparticles against Candida strains. -- Abstract: Gold nanoparticles have been successfully synthesized by solvothermal method using SnCl{sub 2} and NaBH{sub 4} as reducing agents. X-ray diffraction studies show highly crystalline and monophasic nature of the gold nanoparticles with face centred cubic structure. The transmission electron microscopic studies show the formation of nearly spherical gold nanoparticles of average size of 15 nm using SnCl{sub 2}, however, NaBH{sub 4} produced highly uniform, monodispersed and spherical gold nanoparticles of average grain size of 7 nm. A high surface area of 329 m{sup 2}/g for 7 nm and 269 m{sup 2}/g for 15 nm gold nanoparticles was observed. UV–vis studies assert the excitations over the visible region due to transverse and longitudinal surface plasmon modes. The gold nanoparticles exhibit excellent size dependant antifungal activity and greater biocidal action against Candida isolates for 7 nm sized gold nanoparticles restricting the transmembrane H{sup +} efflux of the Candida species than 15 nm sized gold nanoparticles.

  8. New constitutive latex osmotin-like proteins lacking antifungal activity.

    Science.gov (United States)

    Freitas, Cleverson D T; Silva, Maria Z R; Bruno-Moreno, Frederico; Monteiro-Moreira, Ana C O; Moreira, Renato A; Ramos, Márcio V

    2015-11-01

    Proteins that share similar primary sequences to the protein originally described in salt-stressed tobacco cells have been named osmotins. So far, only two osmotin-like proteins were purified and characterized of latex fluids. Osmotin from Carica papaya latex is an inducible protein lacking antifungal activity, whereas the Calotropis procera latex osmotin is a constitutive antifungal protein. To get additional insights into this subject, we investigated osmotins in latex fluids of five species. Two potential osmotin-like proteins in Cryptostegia grandiflora and Plumeria rubra latex were detected by immunological cross-reactivity with polyclonal antibodies produced against the C. procera latex osmotin (CpOsm) by ELISA, Dot Blot and Western Blot assays. Osmotin-like proteins were not detected in the latex of Thevetia peruviana, Himatanthus drasticus and healthy Carica papaya fruits. Later, the two new osmotin-like proteins were purified through immunoaffinity chromatography with anti-CpOsm immobilized antibodies. Worth noting the chromatographic efficiency allowed for the purification of the osmotin-like protein belonging to H. drasticus latex, which was not detectable by immunoassays. The identification of the purified proteins was confirmed after MS/MS analyses of their tryptic digests. It is concluded that the constitutive osmotin-like proteins reported here share structural similarities to CpOsm. However, unlike CpOsm, they did not exhibit antifungal activity against Fusarium solani and Colletotrichum gloeosporioides. These results suggest that osmotins of different latex sources may be involved in distinct physiological or defensive events. Copyright © 2015 Elsevier Masson SAS. All rights reserved.

  9. Antifungal activity of gold nanoparticles prepared by solvothermal method

    International Nuclear Information System (INIS)

    Ahmad, Tokeer; Wani, Irshad A.; Lone, Irfan H.; Ganguly, Aparna; Manzoor, Nikhat; Ahmad, Aijaz; Ahmed, Jahangeer; Al-Shihri, Ayed S.

    2013-01-01

    Graphical abstract: Gold nanoparticles (7 and 15 nm) of very high surface area (329 and 269 m 2 /g) have been successfully synthesized through solvothermal method by using tin chloride and sodium borohydride as reducing agents. As-prepared gold nanoparticles shows very excellent antifungal activity against Candida isolates and activity increases with decrease in the particle size. Display Omitted Highlights: ► Effect of reducing agents on the morphology of gold nanoparticles. ► Highly uniform and monodisperse gold nanoparticles (7 nm). ► Highest surface area of gold nanoparticles (329 m 2/ g). ► Excellent antifungal activity of gold nanoparticles against Candida strains. -- Abstract: Gold nanoparticles have been successfully synthesized by solvothermal method using SnCl 2 and NaBH 4 as reducing agents. X-ray diffraction studies show highly crystalline and monophasic nature of the gold nanoparticles with face centred cubic structure. The transmission electron microscopic studies show the formation of nearly spherical gold nanoparticles of average size of 15 nm using SnCl 2 , however, NaBH 4 produced highly uniform, monodispersed and spherical gold nanoparticles of average grain size of 7 nm. A high surface area of 329 m 2 /g for 7 nm and 269 m 2 /g for 15 nm gold nanoparticles was observed. UV–vis studies assert the excitations over the visible region due to transverse and longitudinal surface plasmon modes. The gold nanoparticles exhibit excellent size dependant antifungal activity and greater biocidal action against Candida isolates for 7 nm sized gold nanoparticles restricting the transmembrane H + efflux of the Candida species than 15 nm sized gold nanoparticles.

  10. The importance of extremophile cyanobacteria in the production of biologically active compounds

    Directory of Open Access Journals (Sweden)

    Drobac-Čik Aleksandra V.

    2007-01-01

    Full Text Available Due to their ability to endure extreme conditions, terrestrial cyanobacteria belong to a group of organisms known as "extremophiles". Research so far has shown that these organisms posses a great capacity for producing biologically active compounds (BAC. The antibacterial and antifungal activities of methanol extracts of 21 cyanobacterial strains belonging to Anabaena and Nostoc genera, previously isolated from different soil types and water resources in Serbia, were evaluated. In general, larger number of cyanobacterial strains showed antifungal activity. In contrast to Nostoc, Anabaena strains showed greater diversity of antibacterial activity (mean value of percentages of sensitive targeted bacterial strains 3% and 25.9% respectively. Larger number of targeted fungi was sensitive to cultural liquid extract (CL, while crude cell extract (CE affected more bacterial strains. According to this investigation, the higher biological activity of terrestrial strains as representatives of extremophiles may present them as significant BAC producers. This kind of investigation creates very general view of cyanobacterial possibility to produce biologically active compounds but it points out the necessity of exploring terrestrial cyanobacterial extremophiles as potentially excellent sources of these substances and reveals the most prospective strains for further investigations.

  11. Antimicrobial and allelopathic metabolites produced by Penicillium brasilianum.

    Science.gov (United States)

    Tang, Hao-Yu; Zhang, Qiang; Li, He; Gao, Jin-Ming

    2015-01-01

    Six known compounds, isoroquefortine C (1), griseofulvin (2), ergosterol peroxide (3), 3β-hydroxy-(22E,24R)-ergosta-5,8,22-trien-7-one (4), cerevisterol (5) and (22E,24R)-6β-methoxyergosta-7,22-diene-3β,5α-diol (6), were produced by the fungus Penicillium brasilianum, and their structures were elucidated by spectroscopic methods. This is the first report on isoroquefortine C as naturally occurring compound. Their bioactivities against five phytopathogenic fungi (Gibeberalla saubinetti, Fusarium solani, Botrytis cinerea, Colletotrichum gloeosporioides and Alternaria solani) and four pathogenic bacteria (Escherichia coli, Bacillus subtilis, Staphyloccocus aureus and Bacillus cereus), as well as allelopathic activities on Raphanus sativus were tested. Compound 1 exhibited a remarkable antifungal activity with minimum inhibitory concentration (MIC) of 12.5 μM against C. gloeosporioides, in comparison with positive control hymexazol (MIC 25 μM). Compound 2 displayed strong inhibitory effects on the growth of A. solani and S. aureus with MIC of 3.13 μM for each. Compounds 2 and 3 displayed a significant growth-inhibition activity on R. sativus.

  12. Facile Syntheses and Molecular-Docking of Novel Substituted 3,4-Dimethyl-1H-pyrrole-2-carboxamide/carbohydrazide Analogues with Antimicrobial and Antifungal Properties

    Directory of Open Access Journals (Sweden)

    Jitendra D. Bhosale

    2018-04-01

    Full Text Available The article describes the use of facile one-pot, high-yielding reactions to synthesize substituted 3,4-dimethyl-1H-pyrrole-2-carboxamides 3a–m and carbohydrazide analogues 5a–l as potential antifungal and antimicrobial agents. The structural identity and purity of the synthesized compounds were assigned based on appropriate spectroscopic techniques. Synthesized compounds were assessed in vitro for antifungal and antibacterial activity. The compounds 5h, 5i and 5j were found to be the most potent against Aspergillus fumigatus, with MIC values of 0.039 mg/mL. The compound 5f bearing a 2, 6-dichloro group on the phenyl ring was found to be the most active broad spectrum antibacterial agent with a MIC value of 0.039 mg/mL. The mode of action of the most promising antifungal compounds (one representative from each series; 3j and 5h was established by their molecular docking with the active site of sterol 14α-demethylase. Molecular docking studies revealed a highly spontaneous binding ability of the tested compounds in the access channel away from catalytic heme iron of the enzyme, which suggested that the tested compounds inhibit this enzyme and would avoid heme iron-related deleterious side effects observed with many existing antifungal compounds.

  13. Triterpenes as Potentially Cytotoxic Compounds

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    Malwina Chudzik

    2015-01-01

    Full Text Available Triterpenes are compounds of natural origin, which have numerously biological activities: anti-cancer properties, anti-inflammatory, anti-oxidative, anti-viral, anti-bacterial and anti-fungal. These substances can be isolated from plants, animals or fungi. Nowadays, when neoplasms are main cause of death, triterpenes can become an alternative method for treating cancer because of their cytotoxic properties and chemopreventive activities.

  14. Synergistic antifungal activity of KB425796-C in combination with micafungin against Aspergillus fumigatus and its efficacy in murine infection models.

    Science.gov (United States)

    Kai, Hirohito; Yamashita, Midori; Nakamura, Ikuko; Yoshikawa, Koji; Nitta, Kumiko; Watanabe, Masato; Inamura, Noriaki; Fujie, Akihiko

    2013-08-01

    KB425796-C is a novel antifungal metabolite produced by the newly isolated bacterial strain Paenibacillus sp. No. 530603. This compound is a 40-membered macrocyclic lipopeptidolactone consisting of 12 amino acids and a 3-hydroxy-15-methylpalmitoyl moiety. KB425796-C displayed antifungal activity against micafungin-resistant fungi and was fungicidal to Trichosporon asahii in vitro. In a murine systemic infection model of T. asahii, KB425796-C showed excellent efficacy upon i.p. administration at 32 mg kg(-1). In addition, KB425796-C induced morphological changes in the hyphae of Aspergillus fumigatus and had fungicidal effects in combination with micafungin. In a mouse model of septic A. fumigatus infection, although non-treated mice survived for a maximum of only 6 days, the survival rate of micafungin-treated mice (0.1 mg kg(-1)) increased to 20%, while the survival rate of mice treated with a combination of micafungin (0.1 mg kg(-1)) and KB425796-C (32 mg kg(-1)) increased to 100% during the 31-day post-infection period. Our findings suggest that KB425796-C is a good candidate for the treatment of aspergillosis in combination with micafungin.

  15. Synthesis of Oxylipin Mimics and Their Antifungal Activity against the Citrus Postharvest Pathogens

    Directory of Open Access Journals (Sweden)

    Jimei Ma

    2016-02-01

    Full Text Available Nine oxylipin mimics were designed and synthesized starting from d-mannose. Their antifungal activity against three citrus postharvest pathogens was evaluated by spore germination assay. The results indicated that all the compounds significantly inhibited the growth of Penicillium digitatum, Penicillium italicum and Aspergillus niger. The compound (3Z,6Z,8S,9R,10R-octadeca-3,6-diene-8,9,10-triol (3 exhibited excellent inhibitory effect on both Penicillium digitatum (IC50 = 34 ppm and Penicillium italicum (IC50 = 94 ppm. Their in vivo antifungal activities against citrus postharvest blue mold were tested with fruit inoculated with the pathogen Penicillium italicum. The compound (3R,4S-methyl 3,4-dihydroxy-5-octyltetrahydrofuran-2-carboxylate (9 demonstrated significant efficacy by reducing the disease severity to 60%. The antifungal mechanism of these oxylipin mimics was postulated in which both inhibition of pathogenic mycelium and stimuli of the host oxylipin-mediated defense response played important roles.

  16. Synthesis of Oxylipin Mimics and Their Antifungal Activity against the Citrus Postharvest Pathogens.

    Science.gov (United States)

    Ma, Jimei; Li, Yupeng; Chen, Hangwei; Zeng, Zhen; Li, Zi-Long; Jiang, Hong

    2016-02-22

    Nine oxylipin mimics were designed and synthesized starting from d-mannose. Their antifungal activity against three citrus postharvest pathogens was evaluated by spore germination assay. The results indicated that all the compounds significantly inhibited the growth of Penicillium digitatum, Penicillium italicum and Aspergillus niger. The compound (3Z,6Z,8S,9R,10R)-octadeca-3,6-diene-8,9,10-triol (3) exhibited excellent inhibitory effect on both Penicillium digitatum (IC50 = 34 ppm) and Penicillium italicum (IC50 = 94 ppm). Their in vivo antifungal activities against citrus postharvest blue mold were tested with fruit inoculated with the pathogen Penicillium italicum. The compound (3R,4S)-methyl 3,4-dihydroxy-5-octyltetrahydrofuran-2-carboxylate (9) demonstrated significant efficacy by reducing the disease severity to 60%. The antifungal mechanism of these oxylipin mimics was postulated in which both inhibition of pathogenic mycelium and stimuli of the host oxylipin-mediated defense response played important roles.

  17. Antifungal and antiaflatoxigenic activities of coumarinyl thiosemicarbazides against Aspergillus flavus NRRL 3251.

    Science.gov (United States)

    Kovač, Tihomir; Kovač, Marija; Strelec, Ivica; Nevistić, Ante; Molnar, Maja

    2017-03-01

    The antifungal and antiaflatoxigenic effects of two series of coumarinyl thiosemicarbazides on Aspergillus flavus NRRL 3251 were studied. Fungi were grown in YES medium for 72 h at 29 °C in the presence of 0, 0.1, 1, and 10 μg mL-1 of coumarinyl thiosemicarbazides: one series with substitution in position 7 and another with substitution in position 4 of the coumarin core. Dry mycelia weight determination was used for antifungal activity estimation, while the aflatoxin B1 content in YES media, determined by the dilute and shoot LC-MS/MS technique, was used for the antiaflatoxigenic effect estimation. Standard biochemical assays were used for oxidative status marker (TBARS, SOD, CAT, and GPX) determination in A. flavus NRRL 3251 mycelia. Results show that 7-substituted-coumarinyl thiosemicarbazides possess a better antifungal and antiaflatoxigenic activity than 4-substituted ones. The most prominent substituted compound was the compound 3, N-(4-chlorophenyl)-2-(2-((4-methyl-2-oxo-2H-chromen-7-yl)oxy)acetyl)hydrazine-1-carbothioamide, which completely inhibited aflatoxin production at the concentration of 10 μg mL-1. Oxidative stress response of A. flavus exposed to the selected compounds points to the modulation of oxidative stress as a possible reason of aflatoxin production inhibition.

  18. Chemical Composition and in Vitro Antifungal Activity Screening of the Allium ursinum L. (Liliaceae)

    Science.gov (United States)

    Bagiu, Radu Vasile; Vlaicu, Brigitha; Butnariu, Monica

    2012-01-01

    The objective of the study was to summarize the methods for isolating and identifying natural sulfur compounds from Allium ursinum (ramson) and to discuss the active constituents with regard to antifungal action. Using chromatographic techniques, the active constituents were isolated and subsequently identified. Analyses by high-performance liquid chromatography (HPLC) suggested that these compounds were sulfur constituents, with a characteristic absorbance at 250 nm. Gas chromatography-mass spectrometry (GC-MS) analyses allowed the chemical structures of the isolated constituents to be postulated. We adopted the same methods to identify the health-giving profiling of ramsons and the effects are thought to be primarily derived from the presence and breakdown of the alk(en)ylcysteine sulphoxide, alliin and its subsequent breakdown to allicin (sulfur-compounds of ramson) in connection with antifungal action. The aim of the study was the characterization of the chemical composition of ramsons and the testing of the action of the in vitro extracts, on different strains of Candida albicans. The main goal was to highlight the most efficient extracts of Allium ursinum that can provide long-term antifungal activity without remissions. The extracts from Allium ursinum plants, inhibited growth of Candida spp. cells at concentrations ranging from 0.5 to 4.0 mg/mL, while that of adherent cells at concentrations ranging from 1.0 to > 4.0 mg/mL, depending on the yeast and plant species. PMID:22408399

  19. Antifungal Activity of Commercial Essential Oils and Biocides against Candida Albicans.

    Science.gov (United States)

    Serra, Elisa; Hidalgo-Bastida, Lilia Araida; Verran, Joanna; Williams, David; Malic, Sladjana

    2018-01-25

    Management of oral candidosis, most frequently caused by Candida albicans , is limited due to the relatively low number of antifungal drugs and the emergence of antifungal tolerance. In this study, the antifungal activity of a range of commercial essential oils, two terpenes, chlorhexidine and triclosan was evaluated against C. albicans in planktonic and biofilm form. In addition, cytotoxicity of the most promising compounds was assessed using murine fibroblasts and expressed as half maximal inhibitory concentrations (IC50). Antifungal activity was determined using a broth microdilution assay. The minimum inhibitory concentration (MIC) was established against planktonic cells cultured in a range of concentrations of the test agents. The minimal biofilm eradication concentration (MBEC) was determined by measuring re-growth of cells after pre-formed biofilm was treated for 24 h with the test agents. All tested commercial essential oils demonstrated anticandidal activity (MICs from 0.06% ( v / v ) to 0.4% ( v / v )) against planktonic cultures, with a noticeable increase in resistance exhibited by biofilms (MBECs > 1.5% ( v / v )). The IC50s of the commercial essential oils were lower than the MICs, while a one hour application of chlorhexidine was not cytotoxic at concentrations lower than the MIC. In conclusion, the tested commercial essential oils exhibit potential as therapeutic agents against C. albicans , although host cell cytotoxicity is a consideration when developing these new treatments.

  20. Propolis from the northwest of Argentina as a source of antifungal principles.

    Science.gov (United States)

    Quiroga, E N; Sampietro, D A; Soberón, J R; Sgariglia, M A; Vattuone, M A

    2006-07-01

    To determine the antimycotic and cytotoxic activities of partially purified propolis extract on yeasts, xylophagous and phytopathogenic fungi. To compare these activities with pinocembrin and galangin isolated from this propolis and with the synthetic drugs ketoconazole and clortrimazole. Ethanolic propolis extract was partially purified by cooling at -20 degrees C. Two of its components were isolated by HPLC and identified as pinocembrin and galangin. The antifungal activity was assayed by bioautography, hyphal radial growth, hyphal extent and microdilution in liquid medium. Cytotoxicity was studied with the lethality assay of Artemia salina. The obtained results were compared with the actions of ketoconazole and clortrimazole. The results showed that the antifungal potency of ketoconazole and clortrimazole is higher than pinocembrin, galangin and the partially purified propolis extract in this order. Otherwise, the cytotoxicity of the synthetic drugs is also the highest. Partially purified propolis extract inhibits fungal growth. The comparison of its relative biocide potency and cytotoxicity with synthetic drugs and two components of this propolis (pinocembrin and galangin) showed that the propolis from 'El Siambón', Tucumán, Argentina, is a suitable source of antifungal products. The partially purified propolis extract and its isolated compounds, pinocembrin and galangin, have the capacity of being used as antifungals without detriment to the equilibrium of agroecosystems. The impact of this study is that the preparation of agrochemicals with reduced economic costs using a partially purified preparation as the active principle is possible.

  1. Phytochemistry, antioxidant potential and antifungal of Byrsonima crassifolia on soil phytopathogen control

    Directory of Open Access Journals (Sweden)

    B. S. Andrade

    2017-07-01

    Full Text Available Abstract The use of chemical defensives to control fungal diseases has by consequence to impact negatively over the environment and human health, this way, the use of plant extracts with antifungal properties along with proper cultural management makes viable an alternative plant production control, specially for familiar and organic cultures. The objective of this study was to perform phytochemical and antioxidant analysis of Byrsonima crassifolia (canjiqueira barks and evaluate its antifungal potential over Fusarium solani and Sclerotinia sclerotiorum mycelial growth. The ethanol extract from plants collected in Pantanal, Mato Grosso do Sul, Brazil was submitted to phytochemical prospection, total phenol and flavonoids quantification and antioxidant activiy determination (DPPH. To evaluate antifungal activity concentrations of 800, 1200, 1600, 2000 and 2400 µg 100 mL-1 of ethanol extract were used. Which concentration was separately incorporated in agar (PDA and shed in Petri dishes, followed by the fungi mycelial disc where the colonies diameter was measured daily. Negatives control with agar without extract and agar with an ethanol solution were used. The B. crassifolia ethanol extract presented inhibitory activity over the fungi studied where concentrations of 800 and 1600 µg 100 mL-1, inhibited 38% of the mycelial growth of F. solani; to S. sclerotiorum the best concentration was 2400 µg 100 mL1, reducing 37.5%. The antifungal bark extract potential of this specie is attributed to phenolic compounds and to triterpenes derivatives.

  2. Antifungal Activity of Commercial Essential Oils and Biocides against Candida Albicans

    Directory of Open Access Journals (Sweden)

    Elisa Serra

    2018-01-01

    Full Text Available Management of oral candidosis, most frequently caused by Candida albicans, is limited due to the relatively low number of antifungal drugs and the emergence of antifungal tolerance. In this study, the antifungal activity of a range of commercial essential oils, two terpenes, chlorhexidine and triclosan was evaluated against C. albicans in planktonic and biofilm form. In addition, cytotoxicity of the most promising compounds was assessed using murine fibroblasts and expressed as half maximal inhibitory concentrations (IC50. Antifungal activity was determined using a broth microdilution assay. The minimum inhibitory concentration (MIC was established against planktonic cells cultured in a range of concentrations of the test agents. The minimal biofilm eradication concentration (MBEC was determined by measuring re-growth of cells after pre-formed biofilm was treated for 24 h with the test agents. All tested commercial essential oils demonstrated anticandidal activity (MICs from 0.06% (v/v to 0.4% (v/v against planktonic cultures, with a noticeable increase in resistance exhibited by biofilms (MBECs > 1.5% (v/v. The IC50s of the commercial essential oils were lower than the MICs, while a one hour application of chlorhexidine was not cytotoxic at concentrations lower than the MIC. In conclusion, the tested commercial essential oils exhibit potential as therapeutic agents against C. albicans, although host cell cytotoxicity is a consideration when developing these new treatments.

  3. Antifungal activity, main active components and mechanism of Curcuma longa extract against Fusarium graminearum

    Science.gov (United States)

    Zhang, Fusheng; Chen, Qin; Chen, Cheng; Yu, Xiaorui; Liu, Qingya; Bao, Jinku

    2018-01-01

    Curcuma longa possesses powerful antifungal activity, as demonstrated in many studies. In this study, the antifungal spectrum of Curcuma longa alcohol extract was determined, and the resulting EC50 values (mg/mL) of its extract on eleven fungi, including Fusarium graminearum, Fusarium chlamydosporum, Alternaria alternate, Fusarium tricinctum, Sclerotinia sclerotiorum, Botrytis cinerea, Fusarium culmorum, Rhizopus oryzae, Cladosporium cladosporioides, Fusarium oxysporum and Colletotrichum higginsianum, were 0.1088, 0.1742, 0.1888, 0.2547, 0.3135, 0.3825, 0.4229, 1.2086, 4.5176, 3.8833 and 5.0183, respectively. Among them, F. graminearum was selected to determine the inhibitory effects of the compounds (including curdione, isocurcumenol, curcumenol, curzerene, β-elemene, curcumin, germacrone and curcumol) derived from Curcuma longa. In addition, the antifungal activities of curdione, curcumenol, curzerene, curcumol and isocurcumenol and the synergies of the complexes of curdione and seven other chemicals were investigated. Differential proteomics of F. graminearum was also compared, and at least 2021 reproducible protein spots were identified. Among these spots, 46 were classified as differentially expressed proteins, and these proteins are involved in energy metabolism, tRNA synthesis and glucose metabolism. Furthermore, several fungal physiological differences were also analysed. The antifungal effect included fungal cell membrane disruption and inhibition of ergosterol synthesis, respiration, succinate dehydrogenase (SDH) and NADH oxidase. PMID:29543859

  4. Chemical Composition, Antifungal and Antioxidant Activities of Hedyosmum brasiliense Mart. ex Miq. (Chloranthaceae) Essential Oils

    Science.gov (United States)

    Murakami, Cynthia; Cordeiro, Inês; Young, Maria Cláudia M.

    2017-01-01

    Background: Hedyosmum brasiliense Mart. ex Miq. (Chloranthaceae) is a dioecious shrub popularly used in Brazil to treat foot fungi and rheumatism. This work investigated the chemical composition, antifungal, and antioxidant activities of flowers and leaves of H. brasiliense essential oils; Methods: H. brasiliense male and female flowers and leaves were collected at Ilha do Cardoso (São Paulo) and the essential oils were extracted by hydrodistillation and analyzed by GC/MS and their similarity compared by Principal Component Analysis. Antifungal activity was performed by bioautography and antioxidant potential by 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH) free radical scavenging and β-carotene/linoleic acid system; Results: The major compounds for all oils were sabinene, curzerene, and carotol, but some differences in their chemical composition were discriminated by Principal Component Analysis (PCA) analysis. Bioautography showed two antifungal bands at Rf’s 0.67 and 0.12 in all samples, the first one was identified as curzerene. The oils presented stronger antioxidant potential in β-carotene/linoleic acid bioassay, with IC50’s from 80 to 180 μg/mL, than in DPPH assay, with IC50’s from 2516.18 to 3783.49 μg/mL; Conclusions: These results suggested that curzerene might be responsible for the antifungal activity of H. brasiliense essential oils. Besides, these essential oils exhibited potential to prevent lipoperoxidation, but they have a weak radical scavenger activity. PMID:28930269

  5. Phytochemistry, antioxidant potential and antifungal of Byrsonima crassifolia on soil phytopathogen control.

    Science.gov (United States)

    Andrade, B S; Matias, R; Corrêa, B O; Oliveira, A K M; Guidolin, D G F; Roel, A R

    2018-02-01

    The use of chemical defensives to control fungal diseases has by consequence to impact negatively over the environment and human health, this way, the use of plant extracts with antifungal properties along with proper cultural management makes viable an alternative plant production control, specially for familiar and organic cultures. The objective of this study was to perform phytochemical and antioxidant analysis of Byrsonima crassifolia (canjiqueira) barks and evaluate its antifungal potential over Fusarium solani and Sclerotinia sclerotiorum mycelial growth. The ethanol extract from plants collected in Pantanal, Mato Grosso do Sul, Brazil was submitted to phytochemical prospection, total phenol and flavonoids quantification and antioxidant activiy determination (DPPH). To evaluate antifungal activity concentrations of 800, 1200, 1600, 2000 and 2400 µg 100 mL-1 of ethanol extract were used. Which concentration was separately incorporated in agar (PDA) and shed in Petri dishes, followed by the fungi mycelial disc where the colonies diameter was measured daily. Negatives control with agar without extract and agar with an ethanol solution were used. The B. crassifolia ethanol extract presented inhibitory activity over the fungi studied where concentrations of 800 and 1600 µg 100 mL-1, inhibited 38% of the mycelial growth of F. solani; to S. sclerotiorum the best concentration was 2400 µg 100 mL1, reducing 37.5%. The antifungal bark extract potential of this specie is attributed to phenolic compounds and to triterpenes derivatives.

  6. ANTIFUNGAL POTENTIAL OF LEAF EXTRACTS OF LEGUMINOUS TREES AGAINSTSCLEROTIUM ROLFSII.

    Science.gov (United States)

    Sana, Nighat; Shoaib, Amna; Javaid, Arshad

    2016-01-01

    Sclerotium rolfsii Sacc. is a destructive soil-borne plant pathogen that infects over 500 plant species and causes significant yield losses in many economically important plant species. Synthetic fungicides used to combat the menace also pollute the environment and cause health hazards. In order to search environmental friendly alternatives from natural resources, methanolic extracts of three leguminous tree species namely Acacia nilotica (L.) Willd. ex Delile subsp. indica (Benth.) Brenan, Prosopis juliflora (Sw.) DC. and Albizia lebbeck (L.) Benth. were evaluated for their antifungal activity against S. rolfsii and A. nilotica subsp. indica exhibited the maximum fungicidal potential. Two hundred grams dried leaf material of each of the three test plant species were extracted with methanol for two weeks. After filtration, methanol was evaporated on a rotary evaporator. Malt extract broth was used to make various concentrations of the crude methanolic extracts and their antifungal potential was determined by comparing the fungal biomass in various treatments with control. Chemical composition of methanolic leaf extract of A. nilotica subsp. indica was determined through GC-MS analysis. Methanolic leaf extract of A. nilotica subsp. indica showed the highest fungicidal activity. Fungal biomass was decreased by 17-55% due to various concentrations of this extract over control. Different concentrations of P. juliflora reduced fungal biomass by 3-52%. Fourteen compounds were identified in methanolic extract of A. nilotica subsp. indica . 9,12,15-octadecatrienoic acid, methyl ester, (Z,Z,Z,)- (16.59%) was the most abundant compound followed by 1-pentanol, 2 methyl-, acetate (14.80%); hexanedioic acid, dimethyl ester (13.10%) and cyclotriaconta- 1, 7, 16, 22-tetraone (10.28%). This study concludes that methanolic leaf extract of A. nilotica subsp. indica can be used for management of S. rolfsii .

  7. Synthesis, Characterization and Antifungal Evaluation of 5-Substituted-4-Amino-1,2,4-Triazole-3-Thioesters

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    Aurangzeb Hasan

    2011-01-01

    Full Text Available A series of 5-substituted-4-amino-1,2,4-triazole-3-thioesters was synthesized by converting variously substituted organic acids successively into the corresponding esters, hydrazides, 5-substituted-1,3,4-oxadiazole-2-thiols, 5-substituted-1,2,4-triazole-2-thiols and 5-substituted-1,3,4-oxadiazole-2-thioesters. Finally the target compounds were obtained by refluxing 5-substituted-1,3,4-oxadiazole-2-thioesters in the presence of hydrazine hydrate and absolute alcohol. The structures of the synthesized compounds were established by physicochemical and spectroscopic methods. The synthesized compounds were evaluated for their in vitro antifungal activity. Some of the evaluated compounds possessed significant antifungal activity as compared to a terbinafine standard.

  8. Genetic engineering of crop plants for fungal resistance: role of antifungal genes.

    Science.gov (United States)

    Ceasar, S Antony; Ignacimuthu, S

    2012-06-01

    Fungal diseases damage crop plants and affect agricultural production. Transgenic plants have been produced by inserting antifungal genes to confer resistance against fungal pathogens. Genes of fungal cell wall-degrading enzymes, such as chitinase and glucanase, are frequently used to produce fungal-resistant transgenic crop plants. In this review, we summarize the details of various transformation studies to develop fungal resistance in crop plants.

  9. Cloning, Overexpression andin vitroAntifungal Activity ofZea MaysPR10 Protein.

    Science.gov (United States)

    Zandvakili, Niloofar; Zamani, Mohammadreza; Motallebi, Mostafa; Moghaddassi Jahromi, Zahra

    2017-03-01

    Plants have various defense mechanisms such as production of antimicrobial peptides, particularly pathogenesis related proteins (PR proteins). PR10 family is an essential member of this group, with antifungal, antibacterial and antiviral activities. The goal of this study is to assess the antifungal activity of maize PR10 against some of fungal phytopathogens. Zea mays PR10 gene (TN-05-147) was cloned from genomic DNA and cDNA and overexpressed in Escherichia coli . The existence of a 77- bp intron and two exons in PR10 was confi rmed by comparing the genomic and cDNA sequences. The PR10 cDNA was cloned in pET26b (+) expression vector and transformed into E. coli strain Rosetta DE3 in order to express PR10 recombinant protein. Expression of the recombinant protein was checked by western analysis. Recombinant PR10 appeared as insoluble inclusion bodies and thus solubilized and refolded. PR10 was isolated using Ni- NTA column. The activity of the refolded protein was confi rmed by DNA degradation test. The antifungal activity of PR10 was assessed using radial diff usion, disc diff usion and spore germination. The hemolytic assay was performed to investigate the biosafety of recombinant PR10. Recombinant maize PR10 exerted broad spectrum antifungal activity against Botrytis cinerea, Sclerotinia sclerotiorum, Fusarium oxysporum, Verticillium dahlia and Alternaria solani . Hemolysis biosafety test indicated that the protein is not poisonous to mammalian cells. Maize PR10 has the potential to be used as the antifungal agent against diff erent fungal phytopathogens. Therefore, this protein can be used in order to produce antifungal agents and fungi resistance transgenic plants.

  10. Synthetic multivalent antifungal peptides effective against fungi.

    Directory of Open Access Journals (Sweden)

    Rajamani Lakshminarayanan

    Full Text Available Taking advantage of the cluster effect observed in multivalent peptides, this work describes antifungal activity and possible mechanism of action of tetravalent peptide (B4010 which carries 4 copies of the sequence RGRKVVRR through a branched lysine core. B4010 displayed better antifungal properties than natamycin and amphotericin B. The peptide retained significant activity in the presence of monovalent/divalent cations, trypsin and serum and tear fluid. Moreover, B4010 is non-haemolytic and non-toxic to mice by intraperitoneal (200 mg/kg or intravenous (100 mg/kg routes. S. cerevisiae mutant strains with altered membrane sterol structures and composition showed hyper senstivity to B4010. The peptide had no affinity for cell wall polysaccharides and caused rapid dissipation of membrane potential and release of vital ions and ATP when treated with C. albicans. We demonstrate that additives which alter the membrane potential or membrane rigidity protect C. albicans from B4010-induced lethality. Calcein release assay and molecular dynamics simulations showed that the peptide preferentially binds to mixed bilayer containing ergosterol over phophotidylcholine-cholesterol bilayers. The studies further suggested that the first arginine is important for mediating peptide-bilayer interactions. Replacing the first arginine led to a 2-4 fold decrease in antifungal activities and reduced membrane disruption properties. The combined in silico and in vitro approach should facilitate rational design of new tetravalent antifungal peptides.

  11. Prevalence and Antifungal Susceptibility of Candida Species ...

    African Journals Online (AJOL)

    Candidal vulvovaginitis causes extreme discomfort and affects the well being of women. The aim of this study was to determine the prevalence of Candida infections among women attending gynaecological clinic at the Komfo Anokye Teaching Hospital (KATH) in Kumasi and the antifungal susceptibility patterns of the ...

  12. Interactions between antifungal and antiretroviral agents.

    Science.gov (United States)

    Hughes, Christine A; Foisy, Michelle; Tseng, Alice

    2010-09-01

    Since the advent of combination antiretroviral therapy, the incidence of opportunistic infections has declined and the life expectancy of HIV-infected people has significantly increased. However, opportunistic infections, including fungal diseases, remain a leading cause of hospitalizations and mortality in HIV-infected people. With the availability of several new antiretroviral and antifungal agents, drug-drug interactions emerge as a potential safety concern. Relevant literature was identified using a Medline search of articles published up to March 2010 and a review of conference abstracts. Search terms included HIV, antifungal agents and drug interactions. Original papers and relevant citations were considered for this review. Readers will gain an understanding of the pharmacokinetic properties of antiretroviral and antifungal agents, and insight into significant drug-drug interactions which may require dosage adjustments or a change in therapy. Azole antifungal drugs, with the exception of fluconazole, pose the greatest risk of two-way interactions with antiretroviral drugs through CYP450 enzymes effects. Limited studies suggest the risk of interactions between antiretroviral drugs and echinocandins is much lower. The combination of tenofovir and amphotericin B should be used with caution and close monitoring of renal function is required.

  13. Antifungal diterpenes from Hypoestes serpens (Acanthaceae).

    Science.gov (United States)

    Rasoamiaranjanahary, Lalao; Marston, Andrew; Guilet, David; Schenk, Kurt; Randimbivololona, Fanantenanirainy; Hostettmann, Kurt

    2003-02-01

    Two new diterpenes, fusicoserpenol A and dolabeserpenoic acid A, with antifungal activity, were isolated from leaves of Hypoestes serpens (Acanthaceae). Their structures were elucidated by means of spectrometric methods including 1D and 2D NMR experiments and MS analysis. X-ray crystallographic analysis confirmed the structure of fusicoserpenol A and established the relative configuration.

  14. Species identification and antifungal susceptibility pattern of ...

    African Journals Online (AJOL)

    Dalia Saad ElFeky

    2015-10-23

    Oct 23, 2015 ... Abstract Vulvovaginal candidiasis (VVC) remains one of the most common infections of the female genital tract. Correct identification of the isolated Candida species is essential to direct the empirical antifungal therapy. Objectives: This local study was conducted to identify the spectrum of Candida species ...

  15. Antimycotoxigenic and antifungal activities of Citrullus colocynthis ...

    African Journals Online (AJOL)

    user

    2013-10-23

    Oct 23, 2013 ... 2Laboratory of Technology and Animal Production, University of Abdelhamid Ibn Badis, Mostaganem (27000), Algeria. 3Laboratory of ... results suggest that the extracts showed a very good antifungal activity against A. ochraceus, but for A. ..... activity of essential oil and its constituents from Calocedrus.

  16. Chemical constituents, antibacterial, antifungal and antioxidant ...

    African Journals Online (AJOL)

    ... penicillium notatum and Rhizopus stolonifer) at different concentrations, except ethyl acetate extract which showed no antifungal property on Rhizopus stolonifer. Ethyl acetate and methanol extracts exhibited significant antioxidant activities by scavenging DPPH free radicals with IC of 12.14 and 93.85 μg/ml respectively.

  17. Antifungal potentials of Azardirachta indica and Ocimum ...

    African Journals Online (AJOL)

    Antifungal potentials of Azardirachta indica and Ocimum grattissimum leaf extracts in the control of yam rot. ... Fusarium oxysporium, Botryodiplodia theobromae, Rhizopus stolonifer, Penicilluim notatum and Aspergillus niger were isolated from the rotted yams. Both fresh and dry extracts of the leaves had significant effects ...

  18. Studies on Buddleja asiatica antibacterial, antifungal, antispasmodic ...

    African Journals Online (AJOL)

    Jane

    2011-07-27

    Jul 27, 2011 ... Crude extract of Buddleja asiatica Lour and its fractions, chloroform (F1), ethyl acetate (F2) and n- butanol (F3) were evaluated for antibacterial, antifungal, antispasmodic and Ca++ antagonist activities. The antibacterial activity was performed against 11 types of bacteria. The crude extract and fractions F2.

  19. Species identification and antifungal susceptibility pattern of ...

    African Journals Online (AJOL)

    Species identification of Candida isolates was done using phenotypic methods including germ tube test, Rice Tween-80 agar, Chrom ID (CAN2) agar and API 20C AUX, while PCR-RFLP was used as the gold standard method. Antifungal susceptibility testing was done using the disk diffusion method. Results: Vaginal swab ...

  20. Antifungal evaluation and phytochemical screening of methanolic ...

    African Journals Online (AJOL)

    The objective of the study was to further examine the medicinal value of Boswellia dalzielii plant by evaluating the antifungal activity and carrying out phytochemical screening of methanolic extract, hexane, ethyl acetate, aqueous fractions and the sub-fractions of the stem bark of the plant. Standard methods were used for ...

  1. Novel, Synergistic Antifungal Combinations that Target Translation Fidelity

    Science.gov (United States)

    Moreno-Martinez, Elena; Vallieres, Cindy; Holland, Sara L.; Avery, Simon V.

    2015-01-01

    There is an unmet need for new antifungal or fungicide treatments, as resistance to existing treatments grows. Combination treatments help to combat resistance. Here we develop a novel, effective target for combination antifungal therapy. Different aminoglycoside antibiotics combined with different sulphate-transport inhibitors produced strong, synergistic growth-inhibition of several fungi. Combinations decreased the respective MICs by ≥8-fold. Synergy was suppressed in yeast mutants resistant to effects of sulphate-mimetics (like chromate or molybdate) on sulphate transport. By different mechanisms, aminoglycosides and inhibition of sulphate transport cause errors in mRNA translation. The mistranslation rate was stimulated up to 10-fold when the agents were used in combination, consistent with this being the mode of synergistic action. A range of undesirable fungi were susceptible to synergistic inhibition by the combinations, including the human pathogens Candida albicans, C. glabrata and Cryptococcus neoformans, the food spoilage organism Zygosaccharomyces bailii and the phytopathogens Rhizoctonia solani and Zymoseptoria tritici. There was some specificity as certain fungi were unaffected. There was no synergy against bacterial or mammalian cells. The results indicate that translation fidelity is a promising new target for combinatorial treatment of undesirable fungi, the combinations requiring substantially decreased doses of active components compared to each agent alone. PMID:26573415

  2. Antifungal activity of indigenous Bacillus spp. isolated from soil

    Directory of Open Access Journals (Sweden)

    Bjelić Dragana Đ.

    2017-01-01

    Full Text Available Biocontrol using plant growth-promoting rhizobacteria (PGPR represents an alternative approach to disease management, since PGPR are known to promote growth and reduce diseases in various crops. Among the different PGPR, members of the genus Bacillus are prefered for most biotechnological uses due to their capability to form extremely resistant spores and produce a wide variety of metabolites with antimicrobial activity. The objective of this research was to identify antagonistic bacteria for management of the plant diseases. Eleven isolates of Bacillus spp. were obtained from the soil samples collected from different localities in the Province of Vojvodina. The antifungal activity of bacterial isolates against five fungal species was examined using a dual plate assay. Bacillus isolates exhibited the highest antifungal activity against Fusarium proliferatum, Fusarium oxysporum f. sp. cepae and Alternaria padwickii, while they had the least antagonistic effect on Fusarium verticillioides and Fusarium graminearum. Molecular identification showed that effective bacterial isolates were identified as Bacillus safensis (B2, Bacillus pumilus (B3, B11, Bacillus subtilis (B5, B7 and Bacillus megaterium (B8, B9. The highest antagonistic activity was exhibited by isolates B5 (from 39% to 62% reduction in fungal growth and B7 (from 40% to 71% reduction in fungal growth. These isolates of B. subtilis could be used as potential biocontrol agents of plant diseases. [Project of the Serbian Ministry of Education, Science and Technological Development, Grant no. TR-31073

  3. SB-224289 Antagonizes the Antifungal Mechanism of the Marine Depsipeptide Papuamide A.

    Directory of Open Access Journals (Sweden)

    Chelsi D Cassilly

    Full Text Available In order to expand the repertoire of antifungal compounds a novel, high-throughput phenotypic drug screen targeting fungal phosphatidylserine (PS synthase (Cho1p was developed based on antagonism of the toxin papuamide A (Pap-A. Pap-A is a cyclic depsipeptide that binds to PS in the membrane of wild-type Candida albicans, and permeabilizes its plasma membrane, ultimately causing cell death. Organisms with a homozygous deletion of the CHO1 gene (cho1ΔΔ do not produce PS and are able to survive in the presence of Pap-A. Using this phenotype (i.e. resistance to Pap-A as an indicator of Cho1p inhibition, we screened over 5,600 small molecules for Pap-A resistance and identified SB-224289 as a positive hit. SB-224289, previously reported as a selective human 5-HT1B receptor antagonist, also confers resistance to the similar toxin theopapuamide (TPap-A, but not to other cytotoxic depsipeptides tested. Structurally similar molecules and truncated variants of SB-224289 do not confer resistance to Pap-A, suggesting that the toxin-blocking ability of SB-224289 is very specific. Further biochemical characterization revealed that SB-224289 does not inhibit Cho1p, indicating that Pap-A resistance is conferred by another undetermined mechanism. Although the mode of resistance is unclear, interaction between SB-224289 and Pap-A or TPap-A suggests this screening assay could be adapted for discovering other compounds which could antagonize the effects of other environmentally- or medically-relevant depsipeptide toxins.

  4. Characterization ofBacillus amyloliquefaciensDA12 Showing Potent Antifungal Activity against MycotoxigenicFusariumSpecies.

    Science.gov (United States)

    Lee, Theresa; Park, Dami; Kim, Kihyun; Lim, Seong Mi; Yu, Nan Hee; Kim, Sosoo; Kim, Hwang-Yong; Jung, Kyu Seok; Jang, Ja Yeong; Park, Jong-Chul; Ham, Hyeonheui; Lee, Soohyung; Hong, Sung Kee; Kim, Jin-Cheol

    2017-10-01

    In an attempt to develop a biological control agent against mycotoxigenic Fusarium species, we isolated Bacillus amyloliquefaciens strain DA12 from soil and explored its antimicrobial activities. DA12 was active against the growth of mycotoxigenic F. asiaticum , F. graminearum , F. proliferatum , and F. verticillioides both in vitro and in planta (maize). Further screening using dual culture extended the activity range of strain DA12 against other fungal pathogens including Botrytis cinerea , Colletotrichum coccodes , Endothia parasitica , Fusarium oxysporum , Raffaelea quercus-mongolicae , and Rhizoctonia solani . The butanol extract of the culture filtrate of B. amyloliquefaciens DA12 highly inhibited the germination of F. graminearum macroconidia with inhibition rate 83% at a concentration of 31.3 μg/ml and 100% at a concentration of 250 μg/ml. The antifungal metabolite from the butanol extract was identified as iturin A by thin layer chromatography-bioautography. In addition, volatile organic compounds produced by DA12 were able to inhibit mycelial growth of various phytopathogenic fungi. The volatile compounds were identified as 2-heptanone, 5-methyl heptanone and 6-methyl heptanone by gas chromatography-mass spectrometry (GC-MS) analysis. These results indicate that the antagonistic activity of Bacillus amyloliquefaciens DA12 was attributable to iturin A and volatile heptanones, and the strain could be used as a biocontrol agent to reduce the development of Fusarium diseases and mycotoxin contamination of crops.

  5. In vitro antifungal activity of allyl isothiocyanate (AITC) against Aspergillus parasiticus and Penicillium expansum and evaluation of the AITC estimated daily intake.

    Science.gov (United States)

    Manyes, L; Luciano, F B; Mañes, J; Meca, G

    2015-09-01

    Isothiocyanates (ITCs) are natural compounds derived from cruciferous vegetables produced by enzymatic conversion of metabolites called glucosinolates. They are potentially useful antimicrobial compounds for food applications have been shown to be promising agents against cancer in human cell culture, animal models, and in epidemiological studies. In this study, the antifungal activity of the allyl isothiocyanate (AITC) was evaluated on two mycotoxigenic fungi as Aspergillus parasiticus and Penicillium expnsum, aflatoxins (AFs) and patulin (PAT) producers, employing an assay on solid medium. Also an approximation of the risk evaluation associated to the intake of food treated with the AITC to reduce the risk of fungi spoilage has been evaluated. On solid medium and after 20 days incubation the strain of Penicillium expansum was inhibited with AITC quantities highest than 50 mg, whereas the strain of A. parasiticus was sensible to AITC doses highest than 5 mg. The analysis of the risk assessment associated to the intake of several food classes treated with the bioactive compound AITC to prevent fungi spoilage evidenced that this product can be considered as safe due that the estimated daily intakes (EDIs) are always lower than the AITC Admissible Daily intake (ADI). Copyright © 2015 Elsevier Ltd. All rights reserved.

  6. Synthesis, Antiproliferative and Antifungal Activities of 1,2,3-Triazole-Substituted Carnosic Acid and Carnosol Derivatives

    Directory of Open Access Journals (Sweden)

    Mariano Walter Pertino

    2015-05-01

    Full Text Available Abietane diterpenes exhibit an array of interesting biological activities, which have generated significant interest among the pharmacological community. Starting from the abietane diterpenes carnosic acid and carnosol, twenty four new triazole derivatives were synthesized using click chemistry. The compounds differ in the length of the linker and the substituent on the triazole moiety. The compounds were assessed as antiproliferative and antifungal agents. The antiproliferative activity was determined on normal lung fibroblasts (MRC-5, gastric epithelial adenocarcinoma (AGS, lung cancer (SK-MES-1 and bladder carcinoma (J82 cells while the antifungal activity was assessed against Candida albicans ATCC 10231 and Cryptococcus neoformans ATCC 32264. The carnosic acid γ-lactone derivatives 1–3 were the most active antiproliferative compounds of the series, with IC50 values in the range of 43.4–46.9 μM and 39.2–48.9 μM for MRC-5 and AGS cells, respectively. Regarding antifungal activity, C. neoformans was the most sensitive fungus, with nine compounds inhibiting more than 50% of its fungal growth at concentrations ≤250 µg∙mL−1. Compound 22, possessing a p-Br-benzyl substituent on the triazole ring, showed the best activity (91% growth inhibition at 250 µg∙mL−1 In turn, six compounds inhibited 50% C. albicans growth at concentrations lower than 250 µg∙mL−1.

  7. Synthesis and antifungal activities of pradimicin derivatives, modification at C4'-position.

    Science.gov (United States)

    Kamachi, H; Iimura, S; Okuyama, S; Hoshi, H; Tamura, S; Shinoda, M; Saitoh, K; Konishi, M; Oki, T

    1992-09-01

    The 4'-N-alkyl(1 approximately 10) and 4'-N-acyl derivatives (11 approximately 21) of pradimicins (PRMs) were synthesized by trimethylsilylation of PRMs A, C and FA-1 followed by condensation with appropriate alkylating and acylating agents. The 4'-hydroxy derivatives (23 and 24) were synthesized from PRM FA-2 in a 3-step sequence. Among these compounds, the 4'-N-carboxyl substituted alkyl (1, 5, 8 and 10), 4'-N-formyl (11) and 4'-axial-hydroxy (23) derivatives retained the antifungal activity of the parent compounds and showed great improvement in water solubility.

  8. COMPARISON OF POTENCY OF ANTIFUNGAL ACTION OF DANDRUFF SHAMPOOS AND DIFFERENT PLANT EXTRACTS

    Directory of Open Access Journals (Sweden)

    Naga Padma P, Anuradha K, Divya K

    2015-04-01

    Full Text Available Context: Dandruff a very common scalp disorder with high prevalence in population is caused by numerous host factors in conjunction with Malassezia furfur. Most of the commercially available anti-dandruff hair shampoos contain some form of antifungal agent(s that appear to reduce the incidence of the disease. There are no good scientific studies done to prove the antifungal activity of commercially available hair shampoos. Aim: In this study commercially available shampoos were assessed for antifungal activity against a human dandruff isolate of M. furfur. The shampoos were Head & Shoulders, Clinic All Clear, and Pantene etc. The results demonstrated that all six of the assayed hair shampoos have some antifungal effect on growth of M. furfur. These products have poor efficacies, more side effects and give scope for recurrence of symptoms. Methods and Materials: Therefore different plant extracts that possess various active compounds which have antifungal activity could help to overcome the incidence of the disease and also avoid the emergence of resistance in the pathogen. The plant extracts were tested in different concentrations like 1:5, 1:10, 1:20 and they were hibiscus, neem, soap nut, etc. The inhibitory action was studied using agar well assay and disc diffusion method and the results indicated in percentage of inhibition. Conclusion: The study was significant as not only efficient known plant products with anti-dandruff activity could be compared with commercially available shampoos but also their better efficacies at minimum concentrations could be identified. This can help make a polyherbal mixture that could be incorporated in hair oil or shampoos for better anti-dandruff activity.

  9. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms

    Directory of Open Access Journals (Sweden)

    Dalia Seleem

    2016-06-01

    Full Text Available Monolaurin (also known as glycerol monolaurate is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876 in vitro and investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1α and IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously with C. albicans for 24 hrs followed by the exposure to treatments of monolaurin (3.9–2,500 µM, positive control fluconazole (32.2 µM, and vehicle control group (1% ethanol, which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5–125 µM and 125–250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1α and IL-1β in the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the pro-inflammatory response of the host.

  10. In vitro evaluation of antifungal activity of monolaurin against Candida albicans biofilms.

    Science.gov (United States)

    Seleem, Dalia; Chen, Emily; Benso, Bruna; Pardi, Vanessa; Murata, Ramiro M

    2016-01-01

    Monolaurin (also known as glycerol monolaurate) is a natural compound found in coconut oil and is known for its protective biological activities as an antimicrobial agent. The nature of oral candidiasis and the increased antifungal resistance demand the search for novel antifungal therapeutic agents. In this study, we examine the antifungal activity of monolaurin against Candida albicans biofilms (strain ATCC:SC5314/MYA2876) in vitro and investigate whether monolaurin can alter gene expression of host inflammatory cytokines, IL-1α and IL-1β. In a co-culture model, oral fibroblast cells were cultured simultaneously with C. albicans for 24 hrs followed by the exposure to treatments of monolaurin (3.9-2,500 µM), positive control fluconazole (32.2 µM), and vehicle control group (1% ethanol), which was a model used to evaluate the cytotoxicity of monolaurin on fibroblasts as well as to analyze morphological characteristics of biofilms through fluorescence microscopy. In addition, the co-culture model was used for RNA extraction of oral fibroblasts to assess gene expression of host inflammatory cytokines, using quantitative real-time PCR. Our results showed the MIC and MFC of monolaurin were in the range 62.5-125 µM and 125-250 µM, respectively. Biofilm antifungal assay showed significant reduction in Log (CFU/ml) of biofilms treated with 1,250 and 2,500 µM of 1-monolaurin when compared to the control groups . There was also a significant down-regulation of IL-1α and IL-1β in the co-culture treated with monolaurin. It can be concluded that monolaurin has a potential antifungal activity against C. albicans and can modulate the pro-inflammatory response of the host.

  11. Anti-inflammatory activity of Vismia guianensis (Aubl.) Pers. extracts and antifungal activity against Sporothrix schenckii.

    Science.gov (United States)

    Oliveira, A H; de Oliveira, G G; Carnevale Neto, F; Portuondo, D F; Batista-Duharte, A; Carlos, I Z

    2017-01-04

    Vismia guianensis (Aubl.) Pers. is traditionally used in North and Northeast of Brazil for the treatment of dermatomycoses. Since the strategy associating immunomodulators with antifungal drugs seems to be promissory to improve the treatment efficacy in fungal infections, we aimed to investigate the antifungal activity of V. guianensis ethanolic extract of leaves (VGL) and bark (VGB) against Sporothrix schenckii ATCC 16345 and their antinflammatory activities. The extracts were analyzed by HPLC-DAD-IT MS/MS for in situ identification of major compounds. Antifungal activity was evaluated in vitro (microdilution test) and in vivo using a murine model of S. schenckii infection. The production of TNF-α, IFN-γ, IL-4, IL-10 and IL-12 by measured by ELISA, as well as measured the production and inhibition of the NO after treatment with the plant extracts or itraconazole (ITR). Two O-glucosyl-flavonoids and 16 prenylated benzophenone derivatives already described for Vismia were detected. Both VGL and VGB showed significant antifungal activity either in in vitro assay of microdilution (MIC=3.9µg/mL) and in vivo model of infection with reduction of S. schenckii load in spleen. It was also observed a predominance of reduction in the production of NO and the proinflammatory cytokines evaluated except TNFα, but with stimulation of IL-10, as evidence of a potential anti-inflammatory effect associated. The results showed that both VGL and VGB have a significant antifungal against S. schenckii and an anti-inflammatory activity. These results can support the use of these extracts for alternative treatment of sporotrichosis. Copyright © 2016 Elsevier B.V. All rights reserved.

  12. Investigation of the effect of base strength on the antifungal activity and chemical composition of the fish scales hydrolyzates

    International Nuclear Information System (INIS)

    Niaz, S.; Dil, S.

    2016-01-01

    The effect of base strength on the antifungal activity of the fish scale hydrolyzate was investigated for six types of samples prepared from the scales of Cyprinus carpio using sodium hydroxide in the range of 1-11 percent strength in the aqueous solution. Each of the sample was analyzed for its acid-base content using titration against HCl in addition to the spot test analysis for phenolic compounds. Each of these samples was analyzed using FTIR spectroscopy. Variation in chemical composition and functional group were observed with variation in the base strength. The in vitro antifungal activity of the fish scale hydrolyzates was tested against four pathogenic fungi including Acremonium, Pythium, Verticillium, and Alternaria. The antifungal assay was carried out using agar well diffusion methods. The sterilization was carried out using streptomycin while ketoconazole was used as the standard antifungal agent. Minimum inhibitory concentration was determined for the most active hydrolyzate which was obtained by 9 percent base solution. The cause of this antifungal activity was also discussed in this communication. (author)

  13. Antifungal Activity of Isoliquiritin and Its Inhibitory Effect against Peronophythora litchi Chen through a Membrane Damage Mechanism

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    Jianjun Luo

    2016-02-01

    Full Text Available This study investigated the antifungal activity and potential antifungal mechanism(s of isoliquiritin against P. litchi Chen, one of the main litchi pathogens. The antifungal activity of isoliquiritin against P. litchi Chen had been proven in a dose-dependent manner through in vitro (mycelial growth and sporangia germination and in vivo (detached leaf tests. Results revealed that isoliquiritin exhibited significant antifungal activity against the tested pathogens, especially, P. litchi Chen, with a minimum inhibitory concentration of 27.33 mg/L. The morphology of P. litchi Chen was apparently changed by isoliquiritin through cytoplasm leakage and distortion of mycelia. The cell membrane permeability of the P. litchi Chen increased with the increasing concentration of isoliquiritin, as evidenced by a rise in relative electric conductivity and a decrease in reducing sugar contents. These results indicated that the antifungal effects of isoliquiritin could be explained by a membrane lesion mechanism causing damage to the cell membrane integrity leading to the death of mycelial cells. Taken together, isoliquiritin may be used as a natural alternative to commercial fungicides or a lead compound to develop new fungicides for the control of litchi downy blight.

  14. Characterization and geographical discrimination of commercial Citrus spp. honeys produced in different Mediterranean countries based on minerals, volatile compounds and physicochemical parameters, using chemometrics.

    Science.gov (United States)

    Karabagias, Ioannis K; Louppis, Artemis P; Karabournioti, Sofia; Kontakos, Stavros; Papastephanou, Chara; Kontominas, Michael G

    2017-02-15

    The objective of the present study was: i) to characterize Mediterranean citrus honeys based on conventional physicochemical parameter values, volatile compounds, and mineral content ii) to investigate the potential of above parameters to differentiate citrus honeys according to geographical origin using chemometrics. Thus, 37 citrus honey samples were collected during harvesting periods 2013 and 2014 from Greece, Egypt, Morocco, and Spain. Conventional physicochemical and CIELAB colour parameters were determined using official methods of analysis and the Commission Internationale de l' Eclairage recommendations, respectively. Minerals were determined using ICP-OES and volatiles using SPME-GC/MS. Results showed that honey samples analyzed, met the standard quality criteria set by the EU and were successfully classified according to geographical origin. Correct classification rates were 97.3% using 8 physicochemical parameter values, 86.5% using 15 volatile compound data and 83.8% using 13 minerals. Copyright © 2016 Elsevier Ltd. All rights reserved.

  15. Spectroscopic analysis of phenolic compounds for food and feed formulations

    Science.gov (United States)

    Phenolic compounds exhibit several bioactive properties including anti-oxidant, anti-microbial, and anti-fungal characteristics with potential applications as additives in functional food and feed formulations. Phenolic compounds occur in plants as secondary metabolites and may be recovered as a co-...

  16. Synthesis and antifungal activity of nicotinamide derivatives as succinate dehydrogenase inhibitors.

    Science.gov (United States)

    Ye, Yong-Hao; Ma, Liang; Dai, Zhi-Cheng; Xiao, Yu; Zhang, Ying-Ying; Li, Dong-Dong; Wang, Jian-Xin; Zhu, Hai-Liang

    2014-05-07

    Thirty-eight nicotinamide derivatives were designed and synthesized as potential succinate dehydrogenase inhibitors (SDHI) and precisely characterized by (1)H NMR, ESI-MS, and elemental analysis. The compounds were evaluated against two phytopathogenic fungi, Rhizoctonia solani and Sclerotinia sclerotiorum, by mycelia growth inhibition assay in vitro. Most of the compounds displayed moderate activity, in which, 3a-17 exhibited the most potent antifungal activity against R. solani and S. sclerotiorum with IC50 values of 15.8 and 20.3 μM, respectively, comparable to those of the commonly used fungicides boscalid and carbendazim. The structure-activity relationship (SAR) of nicotinamide derivatives demonstrated that the meta-position of aniline was a key position contributing to the antifungal activity. Inhibition activities against two fungal SDHs were tested and achieved the same tendency with the data acquired from in vitro antifungal assay. Significantly, 3a-17 was demonstrated to successfully suppress disease development in S. sclerotiorum infected cole in vivo. In the molecular docking simulation, sulfur and chlorine of 3a-17 were bound with PHE291 and PRO150 of the SDH homology model, respectively, which could explain the probable mechanism of action between the inhibitory and target protein.

  17. Semisynthetic modifications of hemiaminal function at ornithine unit of mulundocandin, towards chemical stability and antifungal activity.

    Science.gov (United States)

    Lal, Bansi; Gund, Vitthal Genbhau; Gangopadhyay, Ashok Kumar; Nadkarni, S R; Dikshit, Vidula; Chatterjee, D K; Shirvaikar, R

    2003-11-17

    Mulundocandin (1), is an echinocandin class of lipopeptide. It has wide spectrum of antifungal activity against Candida and Aspergillus species. Semisynthetic modification at Ornithine-5-hydroxyl (hemiaminal function) of 1 was carried out to improve solution stability and hence in vivo activity. Synthesis of ether (C-OR), thioether (C-SR) and C-N linkage at hemiaminal function have been described. All synthetic analogues were evaluated for their stability in aqueous solution and found to be more stable than mulundocandin. Antifungal activity of Orn-5 analogues was evaluated both in vitro against Candida albicans and Aspergillus fumigatus by agar well method and in vivo (oral and intraperitoneal) in C. albicans infected Swiss mice. Results of in vivo assays of analogues 2-9 by the oral route suggests that the introduction of either oxygen nucleophiles (-OR) or sulphur nucleophiles (-SR), at either Orn-5 or at both Orn-5 and HTyr-4 positions, results in retaining the activity of the parent compound with improved aqueous stability in most cases. Compound 9 has shown improved antifungal activity in comparison to mulundocandin by oral application in Swiss mice.

  18. Synthesis, Antifungal Evaluation and In Silico Study of N-(4-Halobenzylamides

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    Ricardo Carneiro Montes

    2016-12-01

    Full Text Available A collection of 32 structurally related N-(4-halobenzylamides were synthesized from cinnamic and benzoic acids through coupling reactions with 4-halobenzylamines, using (benzotriazol-1-yloxytris(dimethylaminophosphonium hexafluorophosphate (BOP as a coupling agent. The compounds were identified by spectroscopic methods such as infrared, 1H- and 13C- Nuclear Magnetic Resonance (NMR and high-resolution mass spectrometry. The compounds were then submitted to antimicrobial tests by the minimum inhibitory concentration method (MIC and nystatin was used as a control in the antifungal assays. The purpose of the tests was to evaluate the influence of structural changes in the cinnamic and benzoic acid substructures on the inhibitory activity against strains of Candida albicans, Candida tropicalis, and Candida krusei. A quantitative structure-activity relationship (QSAR study with KNIME v. 3.1.0 and Volsurf v. 1.0.7 softwares were realized, showing that descriptors DRDRDR, DRDRAC, L4LgS, IW4 and DD2 influence the antifungal activity of the haloamides. In general, 10 benzamides revealed fungal sensitivity, especially a vanillic amide which enjoyed the lowest MIC. The results demonstrate that a hydroxyl group in the para position, and a methoxyl at the meta position enhance antifungal activity for the amide skeletal structure. In addition, the double bond as a spacer group appears to be important for the activity of amide structures.

  19. In vitro antifungal activity of Ocimum selloi essential oil and methylchavicol against phytopathogenic fungi1

    Directory of Open Access Journals (Sweden)

    Larissa Corrêa Bomfim Costa

    Full Text Available The efficacy of Ocimum selloi essential oil was evaluated for controlling the growth of mycelia and spores germination Moniliophthora perniciosa. Six compounds (99.89% of the total oil were identified by GC-MS, of which methyl chavicol, methyl eugenol, β-caryophyllene, germacrene-D, bicyclogermacrene and spathulenol. Essential oil was tested for antifungal activity, which was determined by disc diffusion and minimum inhibitory concentration (MIC determination methods. Application of the oil reduced mycelial growth in a dose dependent manner, with maximum inhibition being observed at concentration of 1,000 ppm. Such antifungal activity could be attributed to methyl chavicol since the pure compound was shown to be similarly effective against Moniliophthora perniciosa at 1,000 ppm. The oil when applied at a concentration of 1,000 ppm, reduced the spore germination of Colletotrichum gloeosporioides and M. perniciosa by 93 and 87%, respectively, but had no effect on the Alternaria alternata. It is concluded that the oil from O. selloi and its major constituent, methyl chavicol, are efficient in inhibiting M. perniciosa, but less effective against C. gloeosporioides and A. alternata. The results obtained from this work may contribute to the development of alternative anti-fungal agents to protect the cacao crop from fungal disease.

  20. Antibacterial and Antifungal Activities of Cyanobacterial Strains Isolated from Hot Springs in Oman

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    Neelam Sherwani1

    2015-06-01

    Full Text Available In this study, cyanobacterial microbial mats from five hot springs in Oman, namely Al Kasfah Rustaq, Al Thwara Nakhl, Al–Ali Hammam, Gala and Bowsher, were characterized using direct microscopy. Nine monoclonal cyanobacterial cultures were obtained and their extracts in butanol, dichloromethane (DCM and hexane were screened for antibacterial and antifungal activities. Direct microscopy revealed the presence of 12 different unicellular and filamentous morphotypes, with different distribution in the various mats. Temperature seems to be one of the most important parameters that accounts for the differences in cyanobacterial composition of the mats. Cells of the nine isolates and their aqueous supernatants were subsequently extracted with butanol, DCM and hexane. Dried extracts were tested against nine bacterial (i.e. gram +ve Staphylococcus aureus, Bacillus subtilis and gram –ve, Escherichia coli, Klebsiella pneumoniae, Salmonella choleraesuis, S. enterica, Psuedomonas aeruginosa, Providencia stuartii, and  Acinetobacter calcoaceticus and two fungal pathogens (Rhizoctonia solani and Pythium sp.. All isolates exhibited antibacterial and antifungal activities, which depended mainly on the type of cyanobacterial culture, type of solvent used and the pathogen tested. The highest antibacterial activity was observed in Phormidium species, and butanol was found to be the most appropriate solvent to extract bioactivity from these cyanobacterial species. The results of this study suggest that thermal springs in Oman harbor diverse types of cyanobacteria, which may constitute an important source of antibacterial and antifungal compounds. Further investigation is needed to purify these compounds and find their chemical compositions and modes of action.

  1. The In Vitro Efficacy of Essential Oils and Antifungal Drugs Against Prototheca zopfii.

    Science.gov (United States)

    Grzesiak, Barbara; Głowacka, Anna; Krukowski, Henryk; Lisowski, Andrzej; Lassa, Henryka; Sienkiewicz, Monika

    2016-08-01

    The algae of the genus Prototheca are environmental pathogens whose main reservoir is the habitat of cows. They can cause protothecosis in domestic and wild animals, as well as human beings, with the main etiological agents being Prototheca zopfii in animals and Prototheca wickerhamii in humans. The aim of the study was to evaluate the in vitro activity of selected essential oils and antifungal antibiotics against P. zopfii isolates. The material consisted of nine P. zopfii strains isolated from the milk of cows suffering from mastitis. Eight essential oils produced by POLLENA-AROMA, Poland, and nine antifungal agents were tested. The effects of essential oils on P. zopfii were evaluated by microdilution with liquid Sabouraud dextrose broth, and susceptibility to antifungal agents was tested using the disk-diffusion method. All used essential oils inhibited the activity of P. zopfii isolates, with MIC values ranging from 0.2 to 10.5 μl/ml. Cinnamon, clove, and thyme demonstrated the highest activity against the tested P. zopfii strains at concentrations ranging from 0.6 to 1.0 μl/ml. Of the antifungal agents, the tested strains were the most sensitive to nystatin (100 %). The tested essential oils can be used to complement protothecosis therapy in animals and human beings.

  2. Whey permeate fermented with kefir grains shows antifungal effect against Fusarium graminearum.

    Science.gov (United States)

    Gamba, Raúl Ricardo; De Antoni, Graciela; Peláez, Angela León

    2016-05-01

    The objective of the work reported here was to study the antifungal capability of cell-free supernatants obtained from whey permeates after fermentation by the kefir grains CIDCA AGK1 against Fusarium graminearum growth and zearalenone (ZEA) production. The assays were performed in order to study the conidial germination inhibition -in liquid media- and the effect on fungal growth rate and the Latency phase -in solid media. We observed that fermented supernatants of pH 3·5 produced the highest percentages of inhibition of conidial germination. The dilution and, particularly, alkalinisation of them led to the gradual loss of antifungal activity. In the fungal inhibition assays on plates we found that only the highest proportion of supernatant within solid medium had significant antifungal activity, which was determined as fungicidal. There was no ZEA biosynthesis in the medium with the highest proportion of supernatant, whereas at lower concentrations, the mycotoxin production was strain-dependent. From the results obtained we concluded that kefir supernatants had antifungal activity on the F. graminearum strains investigated and inhibited mycotoxin production as well, but in a strain-dependent fashion. The present work constitutes the first report of the effect of the products obtained from the kefir-grain fermentation of whey permeates - a readily available by-product of the dairy industry - on F. graminearum germination, growth, and toxin production.

  3. Melanins Protect Sporothrix brasiliensis and Sporothrix schenckii from the Antifungal Effects of Terbinafine.

    Directory of Open Access Journals (Sweden)

    Rodrigo Almeida-Paes

    Full Text Available Terbinafine is a recommended therapeutic alternative for patients with sporotrichosis who cannot use itraconazole due to drug interactions or side effects. Melanins are involved in resistance to antifungal drugs and Sporothrix species produce three different types of melanin. Therefore, in this study we evaluated whether Sporothrix melanins impact the efficacy of antifungal drugs. Minimal inhibitory concentrations (MIC and minimal fungicidal concentrations (MFC of two Sporothrix brasiliensis and four Sporothrix schenckii strains grown in the presence of the melanin precursors L-DOPA and L-tyrosine were similar to the MIC determined by the CLSI standard protocol for S. schenckii susceptibility to amphotericin B, ketoconazole, itraconazole or terbinafine. When MICs were determined in the presence of inhibitors to three pathways of melanin synthesis, we observed, in four strains, an increase in terbinafine susceptibility in the presence of tricyclazole, a DHN-melanin inhibitor. In addition, one S. schenckii strain grown in the presence of L-DOPA had a higher MFC value when compared to the control. Growth curves in presence of 2×MIC concentrations of terbinafine showed that pyomelanin and, to a lesser extent, eumelanin were able to protect the fungi against the fungicidal effect of this antifungal drug. Our results suggest that melanin protects the major pathogenic species of the Sporothrix complex from the effects of terbinafine and that the development of new antifungal drugs targeting melanin synthesis may improve sporotrichosis therapies.

  4. Melanins Protect Sporothrix brasiliensis and Sporothrix schenckii from the Antifungal Effects of Terbinafine.

    Science.gov (United States)

    Almeida-Paes, Rodrigo; Figueiredo-Carvalho, Maria Helena Galdino; Brito-Santos, Fábio; Almeida-Silva, Fernando; Oliveira, Manoel Marques Evangelista; Zancopé-Oliveira, Rosely Maria

    2016-01-01

    Terbinafine is a recommended therapeutic alternative for patients with sporotrichosis who cannot use itraconazole due to drug interactions or side effects. Melanins are involved in resistance to antifungal drugs and Sporothrix species produce three different types of melanin. Therefore, in this study we evaluated whether Sporothrix melanins impact the efficacy of antifungal drugs. Minimal inhibitory concentrations (MIC) and minimal fungicidal concentrations (MFC) of two Sporothrix brasiliensis and four Sporothrix schenckii strains grown in the presence of the melanin precursors L-DOPA and L-tyrosine were similar to the MIC determined by the CLSI standard protocol for S. schenckii susceptibility to amphotericin B, ketoconazole, itraconazole or terbinafine. When MICs were determined in the presence of inhibitors to three pathways of melanin synthesis, we observed, in four strains, an increase in terbinafine susceptibility in the presence of tricyclazole, a DHN-melanin inhibitor. In addition, one S. schenckii strain grown in the presence of L-DOPA had a higher MFC value when compared to the control. Growth curves in presence of 2×MIC concentrations of terbinafine showed that pyomelanin and, to a lesser extent, eumelanin were able to protect the fungi against the fungicidal effect of this antifungal drug. Our results suggest that melanin protects the major pathogenic species of the Sporothrix complex from the effects of terbinafine and that the development of new antifungal drugs targeting melanin synthesis may improve sporotrichosis therapies.

  5. Antifungal activity of essential oils on Aspergillus parasiticus isolated from peanuts

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    Yooussef Mina M.

    2016-04-01

    Full Text Available Aspergillus parasiticus is one of the most common fungi which contaminates peanuts by destroying peanut shells before they are harvested and the fungus produces aflatoxins. The aim of this study was to evaluate the antifungal activities of seventeen essential oils on the growth of the aflatoxigenic form of A. parasiticus in contaminated peanuts from commercial outlets in Georgia. The agar dilution method was used to test the antifungal activity of essential oils against this form of A. parasiticus at various concentrations: 500; 1,000; 1,500; 2,000; 2,500 ppm. Among the seventeen essential oils tested, the antifungal effect of cinnamon, lemongrass, clove and thyme resulted in complete inhibition of mycelial growth. Cinnamon oil inhibited mycelial growth at ≥ 1,000 ppm, lemongrass and clove oils at ≥ 1,500 ppm and thyme at 2,500 ppm. However, cedar wood, citronella, cumin and peppermint oils showed partial inhibition of mycelial growth. Eucalyptus oil, on the other hand, had less antifungal properties against growth of A. parasiticus, irrespective of its concentration. Our results indicate that the aflatoxigenic form of A. parasiticus is sensitive to selected essential oils, especially cinnamon. These findings clearly indicate that essential oils may find a practical application in controlling the growth of A. parasiticus in stored peanuts.

  6. Known and novel terpenes from Buddleja globosa displaying selective antifungal activity against dermatophytes.

    Science.gov (United States)

    Mensah, A Y; Houghton, P J; Bloomfield, S; Vlietinck, A; Vanden Berghe, D

    2000-09-01

    Lipophilic extracts of the stembark of Buddleja globosa were found to have antifungal activity at 125 microg/mL against three dermatophytic fungal species but had no activity at 1000 microg/mL against four other fungal species or two yeast species. Bioassay-guided fractionation of Si gel column eluates using the sensitive fungal species resulted in active fractions from which were isolated five compounds that were characterized by spectroscopic methods as one novel and four known compounds. The known compounds were the diterpene buddlejone (1), the bisditerpene maytenone, and the two sesquiterpenes buddledin A and buddledin B, while the novel compound was characterized as the diterpene deoxybuddlejone (2). The minimum inhibitory concentration of all the compounds was determined against all the microorganisms under test, and buddledins A and B were shown to exhibit the greatest antifungal activity, with values of 43 microM and 51 microM, respectively, against the sensitive fungi Trichophyton rubrum, Tricophyton interdigitale, and Epidermophyton floccosum.

  7. Characterisation of two novel bacteriocin-like substances produced by Bacillus amyloliquefaciens ELI149 with broad-spectrum antimicrobial activity.

    Science.gov (United States)

    Salazar, Francisco; Ortiz, Aurelio; Sansinenea, Estibaliz

    2017-12-01

    The aim of this study was to isolate and characterise antifungal and bactericidal compounds from Bacillus amyloliquefaciens strain ELI149. An absorbent resin (Amberlite ® XAD-16) and silica gel column chromatography were used for isolation and purification purposes, respectively. Antibacterial and antifungal assays were performed by the well diffusion method to demonstrate the biological activity of each compound. Cell damage of the tested fungi was evaluated for fengycin under phase-contrast microscopy. Sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) and mass spectroscopy techniques were performed to estimate the approximate molecular mass of each compound. Two bacteriocin-like substances (BLSs) with different physical properties and inhibitory activities were isolated along with two known antifungal compounds. The two BLSs were heat stable and were not sensitive to acid or alkaline conditions (pH 2-10), with broad-spectrum antimicrobial activity. The antifungal compounds were identified as surfactin and fengycin. Only fengycin showed marked antifungal properties against several phytopathogens. The two isolated BLSs were partially characterised and their bactericidal properties were analysed. The antifungals compounds were identified as surfactin and fengycin, this latter being mainly responsible for the antifungal activity. Copyright © 2017 International Society for Chemotherapy of Infection and Cancer. Published by Elsevier Ltd. All rights reserved.

  8. Microwave-Assisted Synthesis of Some 1,3,4-Oxadiazole Derivatives and Evaluation of Their Antibacterial and Antifungal Activity

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    Deepak Swarnkar

    2014-01-01

    Full Text Available A series of substituted 1,3,4-oxadiazole derivatives (3a–f and (6a–f have been synthesized from diphenylacetic acid hydrazide under microwave irradiation in various reaction conditions. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, and 1H NMR. These targeted compounds have been tested for their antibacterial and antifungal activities compared to ampicillin and griseofulvin as standard drug. Compounds 3a, 3e, 3f, 6c, 6d, 6e, and 6d exhibited the maximum antibacterial activities while 3b, 3c, 3d, 3e, 6a, 6d, and 6e exhibited the maximum antifungal activities.

  9. Antibacterial, Antifungal and antioxidant activities of some medicinal plants.

    Science.gov (United States)

    Wazir, Asma; Mehjabeen, -; Jahan, Noor; Sherwani, Sikander Khan; Ahmad, Mansoor

    2014-11-01

    The purpose of this study was to evaluate the antibacterial, antifungal and antioxidant activities of medicinal plants. The antibacterial activity of methanolic extracts of three medicinal plants (Swertia chirata, Terminalia bellerica and Zanthoxylum armatum) were tested against Gentamicin (standard drug) on eleven gram positive and seventeen gram negative bacteria by agar well method. It was revealed that seven-gram negative and six gram positive bacterial species were inhibited by these plant extracts. Minimum inhibitory concentrations (MIC) of the extracts were determined by broth micro-dilution method. The significant MIC value of Swertia chirata was 20mg/ml against Serratia marcesens, Zanthoxylum armatum was 10 mg/ml against Aeromonas hydrophila and Terminali bellerica was 20mg/ml against Acinetobacter baumanii as well as Serratia marcesens. Antifungal screening was done for methanolic extracts of these plants by agar well method with the 6 saprophytic, 5 dermatophytic and 6 yeasts. In this case Griseofulvin was used as a standard. All saprophytes and dermatophytes were showed resistance by these plants extracts except Microsporum canis, which was inhibited by Z. armatum and S. chirata extracts. The significant MIC value of Zanthoxylum armatum was 10mg/ml against Microsporum canis and Swertia chirata was 10mg/ml against Candida tropicalis. The anti-oxidant study was performed by DPPH free radical scavenging assay using ascorbic acid as a reference standard. Significant antioxidant activities were observed by Swertia chirata and Zanthoxylum armatum at concentration 200μg/ml was 70% DPPH scavenging activity (EC50=937.5μg/ml) while Terminalia bellerica showed 55.6% DPPH scavenging activity (EC50=100μg/ml). This study has shown that these plants could provide potent antibacterial compounds and may possible preventive agents in ROS related ailments.

  10. Phylogenetic Diversity and Antifungal Activity of Endophytic Fungi Associated with Tephrosia purpurea

    Science.gov (United States)

    Luo, Ze-Ping; Lin, Hai-Yan; Ding, Wen-Bing; He, Hua-Liang

    2015-01-01

    Sixty-one endophytic fungus strains with different colony morphologies were isolated from the leaves, stems and roots of Tephrosia purpurea with colonization rates of 66.95%, 37.50%, and 26.92%, respectively. Based on internal transcribed spacer sequence analysis, 61 isolates were classified into 16 genera belonging to 3 classes under the phylum Ascomycota. Of the 61 isolates, 6 (9.84%) exhibited antifungal activity against one or more indicator plant pathogenic fungi according to the dual culture test. Isolate TPL25 had the broadest antifungal spectrum of activity, and isolate TPL35 was active against 5 plant pathogenic fungi. Furthermore, culture filtrates of TPL25 and TPL35 exhibited greater than 80% growth inhibition against Sclerotinia sclerotiorum. We conclude that the endophytic fungal strains TPL25 and TPL35 are promising sources of bioactive compounds. PMID:26839503

  11. Lipase-Catalyzed Kinetic Resolution of Novel Antifungal N-Substituted Benzimidazole Derivatives.

    Science.gov (United States)

    Łukowska-Chojnacka, Edyta; Staniszewska, Monika; Bondaryk, Małgorzata; Maurin, Jan K; Bretner, Maria

    2016-04-01

    A series of new N-substituted benzimidazole derivatives was synthesized and their antifungal activity against Candida albicans was evaluated. The chemical step included synthesis of appropriate ketones containing benzimidazole ring, reduction of ketones to the racemic alcohols, and acetylation of alcohols to the esters. All benzimidazole derivatives were obtained with satisfactory yields and in relatively short times. All synthesized compounds exhibit significant antifungal activity against Candida albicans 900028 ATCC (% cell inhibition at 0.25 μg concentration > 98%). Additionally, racemic mixtures of alcohols were separated by lipase-catalyzed kinetic resolution. In the enzymatic step a transesterification reaction was applied and the influence of a lipase type and solvent on the enantioselectivity of the reaction was studied. The most selective enzymes were Novozyme SP 435 and lipase Amano AK from Pseudomonas fluorescens (E > 100). © 2016 Wiley Periodicals, Inc.

  12. Isotryptophan from Antarctic Bacillus amyloliquefaciens Pc3: purification, identification, characterization, and antifungal activity.

    Science.gov (United States)

    Cui, Pengfei; Guo, Wenbin; Chen, Xinhua

    2017-09-01

    Strain Pc3 was isolated from Antarctic seawater and identified as Bacillus amyloliquefaciens. A compound with antifungal activity was purified from the fermentation supernatant of B. amyloliquefaciens Pc3. Its structure was determined to be (S)-2-amino-3-(1H-indol-2-yl) propanoic acid, named as isotryptophan, based on detailed analysis of its nuclear magnetic resonance (NMR) and high-resolution electrospray ionisation mass spectrometry (HR-ESI-MS). Isotryptophan exhibited good thermal stability and antifungal activity against several plant-pathogenic fungi with low minimum inhibitory concentrations. Therefore, the characterisation of isotryptophan from the Antarctic B. amyloliquefaciens Pc3 will facilitate its potential application in the control of plant-pathogenic fungal infection.

  13. Synthesis, Spectral Characterization, and Antibacterial and Antifungal Studies of PANI/V2O5 Nanocomposites

    Directory of Open Access Journals (Sweden)

    Chakradhar Sridhar

    2016-01-01

    Full Text Available The present study deals with the synthesis and characterization of nanocrystalline vanadium pentoxide (V2O5 nanoparticles and their antibacterial and antifungal activity on Staphylococcus aureus and Aspergillus niger, respectively, by agar diffusion method. The metal oxide has been synthesized by employing the sol-gel method, polyaniline (PANI has been synthesized by chemical oxidation, and PANI/V2O5 composites have been synthesized by in situ polymerization method with different ratios (10, 20, 30, 40, and 50 weight% of V2O5 in PANI. The newly prepared composites were characterized by FTIR and powder X-ray diffraction (P-XRD techniques and are found to be formed of PANI/V2O5 nanocomposites, and also the compounds showed moderate antibacterial and antifungal activity.

  14. Amphotericin B, an Anti-Fungal Medication, Directly Increases the Cytotoxicity of NK Cells

    Science.gov (United States)

    Kim, Nayoung; Choi, Ji-Wan; Park, Hye-Ran; Kim, Inki; Kim, Hun Sik

    2017-01-01

    Immunomodulatory drugs (IMiDs) present one example of immunomodulatory agents that improve cancer immunotherapy. Based on the cytotoxic activity of natural killer (NK) cells against cancer cells, a high throughput screening method for the identification of novel immunomodulatory molecules with the potential to stimulate NK cell cytotoxicity against cancer cells was designed and tested using an approved drug library. Among the primary hit compounds, the anti-fungal drug amphotericin B (AMP-B) increased the cytotoxicity of NK cell line and human primary NK cells in a direct manner. The increase in NK cell activity was related to increased formation of NK-target cell conjugates and the subsequent granule polarization toward target cells. The results of the present study indicate that AMP-B could serve a dual function as an anti-fungal and immunomodulatory drug. PMID:28608807

  15. Exploiting mitochondria as targets for the development of new antifungals.

    Science.gov (United States)

    Li, Dongmei; Calderone, Richard

    2017-02-17

    Mitochondria are essential for cell growth and survival of most fungal pathogens. Energy (ATP) produced during oxidation/reduction reactions of the electron transport chain (ETC) Complexes I, III and IV (CI, CIII, CIV) fuel cell synthesis. The mitochondria of fungal pathogens are understudied even though more recent published data suggest critical functional assignments to fungal-specific proteins. Proteins of mammalian mitochondria are grouped into 16 functional categories. In this review, we focus upon 11 proteins from 5 of these categories in fungal pathogens, OXPHOS, protein import, stress response, carbon source metabolism, and fission/fusion morphology. As these proteins also are fungal-specific, we hypothesize that they may be exploited as targets in antifungal drug discovery. We also discuss published transcriptional profiling data of mitochondrial CI subunit protein mutants, in which we advance a novel concept those CI subunit proteins have both shared as well as specific responsibilities for providing ATP to cell processes.

  16. Antifungal activity of 10 Guadeloupean plants.

    Science.gov (United States)

    Biabiany, Murielle; Roumy, Vincent; Hennebelle, Thierry; François, Nadine; Sendid, Boualem; Pottier, Muriel; Aliouat, El Moukhtar; Rouaud, Isabelle; Lohézic-Le Dévéhat, Françoise; Joseph, Henry; Bourgeois, Paul; Sahpaz, Sevser; Bailleul, François

    2013-11-01

    Screening of the antifungal activities of ten Guadeloupean plants was undertaken to find new extracts and formulations against superficial mycoses such as onychomycosis, athlete's foot, Pityriasis versicolor, as well as the deep fungal infection Pneumocystis pneumonia. For the first time, the CMI of these plant extracts [cyclohexane, ethanol and ethanol/water (1:1, v/v)] was determined against five dermatophytes, five Candida species, Scytalidium dimidiatum, a Malassezia sp. strain and Pneumocystis carinii. Cytotoxicity tests of the most active extracts were also performed on an HaCat keratinocyte cell line. Results suggest that the extracts of Bursera simaruba, Cedrela odorata, Enterolobium cyclocarpum and Pluchea carolinensis have interesting activities and could be good candidates for developing antifungal formulations. Copyright © 2012 John Wiley & Sons, Ltd.

  17. Tolerability and safety of antifungal drugs

    Directory of Open Access Journals (Sweden)

    Francesco Scaglione

    2013-08-01

    Full Text Available When treating critically ill patients, as those with fungal infections, attention should be focused on the appropriate use of drugs, especially in terms of dose, safety, and tolerability. The fungal infection itself and the concomitant physiological disorders concur to increase the risk of mortality in these patients, therefore the use of any antifungal agent should be carefully evaluated, considering both the direct action on the target fungus and the adverse effects eventually caused. Among antifungal drugs, echinocandins have the greatest tolerability. In fact, unlike amphotericin B, showing nephrotoxicity, and azoles, which are hepatotoxic, the use of echinocandins doesn’t result in major adverse events.http://dx.doi.org/10.7175/rhc.v4i2s.873

  18. Antibacterial and Antifungal Activities of Spices.

    Science.gov (United States)

    Liu, Qing; Meng, Xiao; Li, Ya; Zhao, Cai-Ning; Tang, Guo-Yi; Li, Hua-Bin

    2017-06-16

    Infectious diseases caused by pathogens and food poisoning caused by spoilage microorganisms are threatening human health all over the world. The efficacies of some antimicrobial agents, which are currently used to extend shelf-life and increase the safety of food products in food industry and to inhibit disease-causing microorganisms in medicine, have been weakened by microbial resistance. Therefore, new antimicrobial agents that could overcome this resistance need to be discovered. Many spices-such as clove, oregano, thyme, cinnamon, and cumin-possessed significant antibacterial and antifungal activities against food spoilage bacteria like Bacillus subtilis and Pseudomonas fluorescens , pathogens like Staphylococcus aureus and Vibrio parahaemolyticus, harmful fungi like Aspergillus flavus, even antibiotic resistant microorganisms such as methicillin resistant Staphylococcus aureus. Therefore, spices have a great potential to be developed as new and safe antimicrobial agents. This review summarizes scientific studies on the antibacterial and antifungal activities of several spices and their derivatives.

  19. Combination Antifungal Therapy for Cryptococcal Meningitis

    OpenAIRE

    Day, Jeremy N.; Chau, Tran T.H.; Wolbers, Marcel; Mai, Pham P.; Dung, Nguyen T.; Mai, Nguyen H.; Phu, Nguyen H.; Nghia, Ho D.; Phong, Nguyen D.; Thai, Cao Q.; Thai, Le H.; Chuong, Ly V.; Sinh, Dinh X.; Duong, Van A.; Hoang, Thu N.

    2013-01-01

    Background\\ud Combination antifungal therapy (amphotericin B deoxycholate and flucytosine) is the recommended treatment for cryptococcal meningitis but has not been shown to reduce mortality, as compared with amphotericin B alone. We performed a randomized, controlled trial to determine whether combining flucytosine or high-dose fluconazole with high-dose amphotericin B improved survival at 14 and 70 days.\\ud Methods\\ud We conducted a randomized, three-group, open-label trial of induction the...

  20. Antifungal Efficacy of Myrtus communis Linn

    OpenAIRE

    Sadeghi Nejad; Erfani Nejad; Yusef Naanaie; Zarrin

    2014-01-01

    Background The ethanolic extract of Myrtus communis Linn. leaves was assayed in vitro as a growth inhibitor against opportunistic fungi such as Candida and Aspergillus species. Myrtus communis Linn. (Family, Myrtaceae) is an aromatic evergreen shrub or small tree. It is native to the Mediterranean region. Objectives This study aimed to assess antifungal activity (in vitro) of the ethanolic extracts of Myrtus communis leaves as a g...