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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.

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    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.

  4. Antifungal Compounds Produced by Colletotrichum gloeosporioides, an Endophytic Fungus from Michelia champaca

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    Vanessa Mara Chapla

    2014-11-01

    Full Text Available In this study, eight endophytic fungi were isolated from the leaves, stems and roots of Michelia champaca. The isolates were screened and evaluated for their antifungal, anticancer and acetylcholinesterase (AChE inhibitory activities. All of the extracts exhibited potent activity against two evaluated phytopathogenic fungi. Chemical investigation of EtOAc extracts of the endophytic fungus Colletotrichum gloeosporioides resulted in the isolation of one new compound, 2-phenylethyl 1H-indol-3-yl-acetate (1, and seven known compounds: uracil (2, cyclo-(S*-Pro-S*-Tyr (3, cyclo-(S*-Pro-S*-Val (4, 2(2-aminophenylacetic acid (5, 2(4-hydroxyphenylacetic acid (6, 4-hydroxy- benzamide (7 and 2(2-hydroxyphenylacetic acid (8. All of the compound structures were elucidated using 1D and 2D NMR and MS analyses. The antifungal and AChE inhibitory activities of compounds 1–8 were evaluated in vitro. Compound 1 exhibited promising activity against Cladosporium cladosporioides and C. sphaerospermum that was comparable to that of the positive control nystatin.

  5. Characterization of an antifungal compound produced by Bacillus sp. strain A(5) F that inhibits Sclerotinia sclerotiorum.

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    Kumar, Ankit; Saini, Sandeep; Wray, Victor; Nimtz, Manfred; Prakash, Anil; Johri, B N

    2012-12-01

    A potential antagonist, Bacillus sp. strain A(5) F was isolated from soybean rhizosphere following in vitro dual plate screening. The bacterium displayed strong inhibitory activity in vitro against soybean stem rot pathogen, Sclerotinia sclerotiorum. The culture supernatant of strain A(5) F completely suppressed the mycelial growth of the pathogen, indicating that suppression was due to the presence of antifungal compounds in the culture filtrate. The culture filtrate also suppressed other phytopathogenic fungi including Fusarium oxysporum and Macrophomina phaseolina, in vitro suggesting a broad spectrum antagonistic activity against fungal pathogens. Chemical extraction followed by chromatographic analysis resulted in two antifungal fractions. The high resolution-electron spin ionization-mass spectrometry (HR-ESI-MS) and Nuclear Magnetic Resonance (1D and 2D(1) H) spectra of these antifungal fractions revealed the presence of antifungal compounds, one of which showed similarity to bacillomycin D.

  6. 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

  7. 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.

  8. Macrocyclic trichothecenes as antifungal and anticancer compounds.

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    de Carvalho, Maira Peres; Weich, Herbert; Abraham, Wolf-Rainer

    2016-01-01

    Trichothecenes are sesquiterpenoid metabolites produced by fungi and species of the plant genus Baccharis, family Asteraceae. They comprise a tricyclic core with an epoxide at C-12 and C-13 and can be grouped into non-macrocyclic and macrocyclic compounds. While many of these compounds are of concern in agriculture, the macrocyclic metabolites have been evaluated as antiviral, anti-cancer, antimalarial and antifungal compounds. Some known cytotoxic responses on eukaryotic cells include inhibition of protein, DNA and RNA syntheses, interference with mitochondrial function, effects on cell division and membranes. These targets however have been elucidated essentially employing non-macrocyclic trichothecenes and only one or two closely related macrocyclic compounds. For several macrocyclic trichothecenes high selectivity against fungal species and against cancer cell lines have been reported suggesting that the macrocycle and its stereochemistry are of crucial importance regarding biological activity and selectivity. This review is focused on compounds belonging to the macrocyclic type, where a cyclic diester or triester ring binds to the trichothecane moiety at C-4 and C- 15 leading to natural products belonging to the groups of satratoxins, verrucarins, roridins, myrotoxins and baccharinoids. Their biological activities, cytotoxic mechanisms and structure-activity relationships (SAR) are discussed. From the reported data it becomes evident that even small changes in the molecules can lead to pronounced effects on biological activity or selectivity against cancer cells lines. Understanding the underlying mechanisms may help to design highly specific drugs for cancer therapy.

  9. Synthesis of Novel Antifungal Triazole Compounds

    Institute of Scientific and Technical Information of China (English)

    Yong CHU; Ming Xia XU; Ding LU

    2004-01-01

    Based on our previous studies of 3D-QSAR, 38 novel objective compounds belonging to 4 series were designed and successfully synthesized directed by the idea of reconstructing the structure of non-pharmacophores while reserving essential ones in triazoles. In vitro pilot studies on their antifungal activities showed that most compounds have inhibitory effects on C.albicans and some inhibit S.cerevisiae also. The effects on C.albicans of 5 compounds are more potent than or equal to that of fluconazole or itraconazole.

  10. 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.

    krusei GO3FlucR 0.78 - 1.56 0.313 - 0.625 64 NT: Not Tested. 4. Discussion The global antifungal market was estimated at $9.4 billion in 2010 and is expected to grow at a rate of 1.9% during 2010-2017. The major class of antifungal compound includes... Genetics Analysis Using Maximum Likelihood, Evolutionary Distance and Maximum Parsimony Methods. Molecular Biology and Evolution, 28, 2731-2739. http://dx.doi.org/10.1093/molbev/msr121 [24] Antifungals Market to 2017—Generic Erosion of Major Polyenes...

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

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    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.

  12. 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.

  13. 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.

  14. Antifungal compounds from the rhizome and roots of Ferula hermonis.

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    Al-Ja'fari, Abdel-Hadi; Vila, Roser; Freixa, Blanca; Costa, Joan; Cañigueral, Salvador

    2013-06-01

    The antifungal activity of hexane, dichloromethane, methanol and aqueous extracts from the rhizome and root of Ferula hermonis was assayed in vitro by the agar disk diffusion method against a panel of human opportunistic and pathogenic fungi. Among them, the hexane and dichloromethane extracts showed the highest activity particularly against the dermatophytes Microsporum gypseum and Tricophyton mentagrophytes as well as the yeast Candida lactis-condensi. Activity-guided fractionation of both extracts using an agar overlay bioautographic method led to the isolation of two antifungal compounds which were identified as the daucane aryl esters jaeschkeanadiol p-hydroxybenzoate (ferutinin) and jaeschkeanadiol benzoate (teferidin). Determination of minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) values of both compounds evidenced a stronger antifungal activity for ferutinin than for teferidin. Particularly, T. mentagrophytes was the most sensitive strain with MIC and MFC values ranging from 8 to 256 µg/mL.

  15. Anticancer and Antifungal Compounds from Aspergillus, Penicillium and Other Filamentous Fungi

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    Peter Boldsen Knudsen

    2013-09-01

    Full Text Available 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 based on substantial previous in-house chemotaxonomic studies.

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

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    Bladt, Tanja Thorskov; Frisvad, Jens Christian; Knudsen, Peter Boldsen; Larsen, Thomas Ostenfeld

    2013-09-13

    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 based on substantial previous in-house chemotaxonomic studies.

  17. 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

  18. Gluconic acid: an antifungal agent produced by Pseudomonas species in biological control of take-all.

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    Kaur, Rajvinder; Macleod, John; Foley, William; Nayudu, Murali

    2006-03-01

    Pseudomonas strain AN5 (Ps. str. AN5), a non-fluorescent Australian bacterial isolate, is an effective biological control (biocontrol) agent of the take-all disease of wheat caused by the fungus Gaeumannomyces graminis var. tritici (Ggt). Ps. str. AN5 controls Ggt by producing an antifungal compound which was purified by thin layer and column chromatography, and identified by NMR and mass spectroscopic analysis to be d-gluconic acid. Commercially bought pure gluconic acid strongly inhibited Ggt. Two different transposon mutants of Ps. str. AN5 which had lost take-all biocontrol did not produce d-gluconic acid. Gluconic acid production was restored, along with take-all biocontrol, when one of these transposon mutants was complemented with the corresponding open reading frame from wild-type genomic DNA. Gluconic acid was detected in the rhizosphere of wheat roots treated with the wild-type Ps. str. AN5, but not in untreated wheat or wheat treated with a transposon mutant strain which had lost biocontrol. The antifungal compounds phenazine-1-carboxylic acid and 2,4-diacetylphloroglucinol, produced by other Pseudomonads and previously shown to be effective in suppressing the take-all disease, were not detected in Ps. str. AN5 extracts. These results suggest that d-gluconic acid is the most significant antifungal agent produced by Ps. str. AN5 in biocontrol of take-all on wheat roots.

  19. An endophytic fungus isolated from finger millet (Eleucine coracona produces anti-fungal natural products

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    Walaa Kamel Mousa

    2015-10-01

    Full Text Available Finger millet is an ancient African cereal crop, domesticated 7000 years ago in Ethiopia, reaching India at 3000 BC. Finger millet is reported to be resistant to various fungal pathogens including Fusarium sp. We hypothesized that finger millet may host beneficial endophytes (plant-colonizing microbes that contribute to the antifungal activity. Here we report the first isolation of endophyte(s from finger millet. Five distinct fungal species were isolated from roots and predicted taxonomically based on 18S rDNA sequencing. Extracts from three putative endophytes inhibited growth of F. graminearum and three other pathogenic Fusarium species. The most potent anti-Fusarium strain (WF4, predicted to be a Phoma sp. was confirmed to behave as an endophyte using pathogenicity and confocal microscopy experiments. Bioassay-guided fractionation of the WF4 extract identified four anti-fungal compounds, viridicatol, tenuazonic acid, alternariol and alternariol monomethyl ether. All the purified compounds caused dramatic breakage of F. graminearum hyphae in vitro. These compounds have not previously been reported to have anti-Fusarium activity. None of the compounds, except for tenuazonic acid, have previously been reported to be produced by Phoma. We conclude that the ancient, disease-tolerant crop, finger millet, is a novel source of endophytic anti-fungal natural products. This paper suggests the value of the crops grown by subsistence farmers as sources of endophytes and their natural products. Application of these natural chemicals to solve real world problems will require further validation.

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

    OpenAIRE

    Peter Boldsen Knudsen; Jens Christian Frisvad; Tanja Thorskov Bladt; Thomas Ostenfeld Larsen

    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 based on substantial previous in-house chemotaxonomic studies.

  1. 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...... based on substantial previous in-house chemotaxonomic studies....

  2. Purification and characterization of antifungal compounds from Lactobacillus plantarum HD1 isolated from kimchi.

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    Ryu, Eun Hye; Yang, Eun Ju; Woo, Eun Rhan; Chang, Hae Choon

    2014-08-01

    Strain HD1 with antifungal activity was isolated from kimchi and identified as Lactobacillus plantarum. Antifungal compounds from Lb. plantarum HD1 were active against food- and feed-borne filamentous fungi and yeasts in a spot-on-the-lawn assay. Antifungal activity of Lb. plantarum HD1 was stronger against filamentous fungi than yeast. Antifungal compounds were purified using solid phase extraction (SPE) and recycling preparative-HPLC. Structures of the antifungal compounds were elucidated by electrospray ionization-mass spectrometry and nuclear magnetic resonance. Active compounds from Lb. plantarum HD1 were identified as 5-oxododecanoic acid (MW 214), 3-hydroxy decanoic acid (MW 188), and 3-hydroxy-5-dodecenoic acid (MW 214). To investigate the potential application of these antifungal compounds for reduction of fungal spoilage in foods, Korean draft rice wine was used as a food model. White film-forming yeasts were observed in control draft rice wine after 11 days of incubation. However, film-forming yeasts were not observed in draft rice wine treated with SPE-prepared culture supernatant of Lb. plantarum HD1 (equivalent to 2.5% addition of culture supernatant) until 27 days of incubation. The addition of antifungal compounds to Korean draft rice wine extended shelf-life up to 27 days at 10 °C without any sterilization process. Therefore, the antifungal activity of Lb. plantarum HD1 may lead to the development of powerful biopreservative systems capable of preventing food- and feed-borne fungal spoilage.

  3. Antifungal hydroxy fatty acids produced during sourdough fermentation: microbial and enzymatic pathways, and antifungal activity in bread.

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    Black, Brenna A; Zannini, Emanuele; Curtis, Jonathan M; Gänzle, Michael G

    2013-03-01

    Lactobacilli convert linoleic acid to hydroxy fatty acids; however, this conversion has not been demonstrated in food fermentations and it remains unknown whether hydroxy fatty acids produced by lactobacilli have antifungal activity. This study aimed to determine whether lactobacilli convert linoleic acid to metabolites with antifungal activity and to assess whether this conversion can be employed to delay fungal growth on bread. Aqueous and organic extracts from seven strains of lactobacilli grown in modified De Man Rogosa Sharpe medium or sourdough were assayed for antifungal activity. Lactobacillus hammesii exhibited increased antifungal activity upon the addition of linoleic acid as a substrate. Bioassay-guided fractionation attributed the antifungal activity of L. hammesii to a monohydroxy C(18:1) fatty acid. Comparison of its antifungal activity to those of other hydroxy fatty acids revealed that the monohydroxy fraction from L. hammesii and coriolic (13-hydroxy-9,11-octadecadienoic) acid were the most active, with MICs of 0.1 to 0.7 g liter(-1). Ricinoleic (12-hydroxy-9-octadecenoic) acid was active at a MIC of 2.4 g liter(-1). L. hammesii accumulated the monohydroxy C(18:1) fatty acid in sourdough to a concentration of 0.73 ± 0.03 g liter(-1) (mean ± standard deviation). Generation of hydroxy fatty acids in sourdough also occurred through enzymatic oxidation of linoleic acid to coriolic acid. The use of 20% sourdough fermented with L. hammesii or the use of 0.15% coriolic acid in bread making increased the mold-free shelf life by 2 to 3 days or from 2 to more than 6 days, respectively. In conclusion, L. hammesii converts linoleic acid in sourdough and the resulting monohydroxy octadecenoic acid exerts antifungal activity in bread.

  4. Antifungal and Antiaflatoxigenic Methylenedioxy-Containing Compounds and Piperine-Like Synthetic Compounds

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    Young-Sun Moon

    2016-08-01

    Full Text Available Twelve methylenedioxy-containing compounds including piperine and 10 piperine-like synthetic compounds were assessed to determine their antifungal and antiaflatoxigenic activities against Aspergillus flavus ATCC 22546 in terms of their structure–activity relationships. Piperonal and 1,3-benzodioxole had inhibitory effects against A. flavus mycelial growth and aflatoxin B1 production up to a concentration of 1000 μg/mL. Ten piperine-like synthetic compounds were synthesized that differed in terms of the carbon length in the hydrocarbon backbone and the presence of the methylenedioxy moiety. In particular, 1-(2-methylpiperidin-1-yl-3-phenylprop-2-en-1-one had potent antifungal and antiaflatoxigenic effects against A. flavus up to a concentration of 1 μg/mL. This synthetic compound was remarkable because the positive control thiabendazole had no inhibitory effect at this concentration. Reverse transcription-PCR analysis showed that five genes involved in aflatoxin biosynthesis pathways were down-regulated in A. flavus, i.e., aflD, aflK, aflQ, aflR, and aflS; therefore, the synthetic compound inhibited aflatoxin production by down-regulating these genes.

  5. Antifungal and Antiaflatoxigenic Methylenedioxy-Containing Compounds and Piperine-Like Synthetic Compounds

    Science.gov (United States)

    Moon, Young-Sun; Choi, Won-Sik; Park, Eun-Sil; Bae, In Kyung; Choi, Sung-Deuk; Paek, Ockjin; Kim, Sheen-Hee; Chun, Hyang Sook; Lee, Sung-Eun

    2016-01-01

    Twelve methylenedioxy-containing compounds including piperine and 10 piperine-like synthetic compounds were assessed to determine their antifungal and antiaflatoxigenic activities against Aspergillus flavus ATCC 22546 in terms of their structure–activity relationships. Piperonal and 1,3-benzodioxole had inhibitory effects against A. flavus mycelial growth and aflatoxin B1 production up to a concentration of 1000 μg/mL. Ten piperine-like synthetic compounds were synthesized that differed in terms of the carbon length in the hydrocarbon backbone and the presence of the methylenedioxy moiety. In particular, 1-(2-methylpiperidin-1-yl)-3-phenylprop-2-en-1-one had potent antifungal and antiaflatoxigenic effects against A. flavus up to a concentration of 1 μg/mL. This synthetic compound was remarkable because the positive control thiabendazole had no inhibitory effect at this concentration. Reverse transcription-PCR analysis showed that five genes involved in aflatoxin biosynthesis pathways were down-regulated in A. flavus, i.e., aflD, aflK, aflQ, aflR, and aflS; therefore, the synthetic compound inhibited aflatoxin production by down-regulating these genes. PMID:27537912

  6. Malettinin E, an antibacterial and antifungal tropolone produced by a marine Cladosporium strain

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    Johanna eSilber

    2014-08-01

    Full Text Available The isolation and structure elucidation of malettinins A–C (1–3 along with the new malettinin E (4 are described. The compounds were produced by the fungus Cladosporium sp. strain KF501, which was isolated from the German Wadden Sea. The malettinins are built up of tropolone/dihydropyran ring structures linked to a furan ring. The structure elucidation of the isolated compounds was achieved by means of one- and two-dimensional NMR spectroscopy supported by mass and UV data. The relative configuration of 4 was determined on the basis of single-crystal X-ray diffraction analysis. 1–4 exhibited antibacterial and antifungal activities when profiled against Xanthomonas campestris and Trichophyton rubrum. The influence of the chemical structure of the furan ring and of configurational changes on biological activities was observed.

  7. 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

  8. Design, synthesis and molecular docking studies of novel triazole antifungal compounds

    Institute of Scientific and Technical Information of China (English)

    Qiu Qin He; Ke Li; Yong Bing Cao; Huan Wen Dong; Li Hua Zhao; Chao Mei Liu; Chun Quan Sheng

    2007-01-01

    Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized.In vitro antifungal activities showed that compounds 10,11,16 and 20 exhibited strong activities.In addition, compounds 10,11 and 16 also displayed certain activities against fluconazole-resistant fungi.

  9. Isolation, Purification, and Structural Identification of an Antifungal Compound from a Trichoderma Strain.

    Science.gov (United States)

    Li, Chong-Wei; Song, Rui-Qing; Yang, Li-Bin; Deng, Xun

    2015-08-01

    Trichoderma strain T-33 has been demonstrated to have inhibitory effect on the fungus species Cytospora chrysosperma. Here, an active antifungal compound was obtained from Trichoderma strain T-33 extract via combined separation technologies, including organic solvent extraction, liquid chromatography, and thin-layer chromatography. The purified compound was further characterized by advanced analytical technologies to elucidate its chemical structure. Results indicated that the active antifungal compound in Trichoderma strain T-33 extract is 2,5- cyclohexadiene-1,4-dione-2,6-bis (1,1-dimethylethyl).

  10. An antifungal compound involved in symbiotic germination of Cypripedium macranthos var. rebunense (Orchidaceae).

    Science.gov (United States)

    Shimura, Hanako; Matsuura, Mayumi; Takada, Noboru; Koda, Yasunori

    2007-05-01

    Germination of orchid seeds fully depends on a symbiotic association with soil-borne fungi, usually Rhizoctonia spp. In contrast to the peaceful symbiotic associations between many other terrestrial plants and mycorrhizal fungi, this association is a life-and-death struggle. The fungi always try to invade the cytoplasm of orchid cells to obtain nutritional compounds. On the other hand, the orchid cells restrict the growth of the infecting hyphae and obtain nutrition by digesting them. It is likely that antifungal compounds are involved in the restriction of fungal growth. Two antifungal compounds, lusianthrin and chrysin, were isolated from the seedlings of Cypripedium macranthos var. rebunense that had developed shoots. The former had a slightly stronger antifungal activity than the latter, and the antifungal spectra of these compounds were relatively specific to the nonpathogenic Rhizoctonia spp. The level of lusianthrin, which was very low in aseptic protocorm-like bodies, dramatically increased following infection with the symbiotic fungus. In contrast, chrysin was not detected in infected protocorm-like bodies. These results suggest that orchid plants equip multiple antifungal compounds and use them at specific developmental stages; lusianthrin maintains the perilous symbiotic association for germination and chrysin helps to protect adult plants.

  11. Control of postharvest fungal pathogens by antifungal compounds from Penicillium expansum.

    Science.gov (United States)

    Rouissi, Wafa; Ugolini, Luisa; Martini, Camilla; Lazzeri, Luca; Mari, Marta

    2013-11-01

    The fungicidal effects of secondary metabolites produced by a strain of Penicillium expansum (R82) in culture filtrate and in a double petri dish assay were tested against one isolate each of Botrytis cinerea, Colletotrichum acutatum, and Monilinia laxa and six isolates of P. expansum, revealing inhibitory activity against every pathogen tested. The characterization of volatile organic compounds released by the R82 strain was performed by solid-phase microextraction-gas chromatographic techniques, and several compounds were detected, one of them identified as phenethyl alcohol (PEA). Synthetic PEA, tested in vitro on fungal pathogens, showed strong inhibition at a concentration of 1,230 μg/ml of airspace, and mycelium appeared more sensitive than conidia; nevertheless, at the concentration naturally emitted by the fungus (0.726 ± 0.16 m g/ml), commercial PEA did not show any antifungal activity. Therefore, a combined effect between different volatile organic compounds produced collectively by R82 can be hypothesized. This aspect suggests further investigation into the possibility of exploiting R82 as a nonchemical alternative in the control of some plant pathogenic fungi.

  12. In vitro antifungal potentials of bioactive compound oleic acid, 3-(octadecyloxy) propyl ester isolated from Lepidagathis cristata Willd. (Acanthaceae) inflorescence

    Institute of Scientific and Technical Information of China (English)

    Maghdu Nainamohamed Abubacker; Palaniyappan Kamala Devi

    2014-01-01

    Objective: To identify bioactive compound oleic acid, 3-(octadecyloxy) propyl ester from Lepidagathis cristata Willd. (L. cristata) and to assess antifungal potentials of the isolated compound. Methods: Aqueous extracts of L. cristata inflorescence were used for this study. The major bioactive compound isolated was tested for antifungal activities. Results: The major bioactive compound oleic acid, 3-(octadecyloxy) propyl ester was isolated from the inflorescence of L. cristata. The bioactive compound was tested for antifungal potentials and found to be highly effective to plant pathogenic fungi Colletotrichum fulcatum NCBT 146, Fusarium oxysporum NCBT 156 and Rhizoctonia solani NCBT 196 as well as for the human pathogenic fungi Curvularia lunata MTCC 2030 and Microsporum canis MTCC 2820. Conclusions: The results justify the antifungal potentials of both plant and human pathogenic fungi. The plant bioactive compound will be helpful in herbal antifungal formulations.

  13. Two small molecule lead compounds as new antifungal agents effective against Candida albicans and Saccharomyces cerevisiae

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    Yones Pilehvar-Soltanahmadi

    2014-06-01

    Full Text Available  Background: Antifungal drug resistance and few numbers of available drugs limit therapeutic options against fungal infections. The present study was designed to discover new antifungal drugs. Materials and Methods: This study was carried out in two separate steps, that is, in silico lead identification and in vitro assaying of antifungal potential. A structural data file of a ternary complex of fusicuccin (legend, C terminus of H+-ATPase and 14-3-3 regulatory protein (1o9F.pdb file was used as a model. Computational screening of a virtual 3D database of drug-like molecules was performed and selected small molecules, resembling the functional part of the ligand performing ligand docking, were tested using ArgusLab (4.0.1. Two lead compounds, 3-Cyclohexan propionic acid (CXP and 4-phenyl butyric acid (PBA were selected according to their ligation scores. Standard Strains of Candida albicans and Saccharomyces cerevisiae were used to measure the antifungal potential of the two identified lead compounds against the fungi using micro-well plate dilution assay. Results: Ligation scores for CXP and PBA were -9.33744 and -10.7259 kcal/mol, respectively, and MIC and MFC of CXP and PBA against the two yeasts were promising. Conclusion: The evidence from the present study suggests that CXP and PBA possess potentially antifungals properties. 

  14. Antifungal activity of extracts from Atacama Desert fungi againstParacoccidioides brasiliensis and identification ofAspergillus felis as a promising source of natural bioactive compounds

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    Graziele Mendes

    2016-03-01

    Full Text Available Fungi of the genus Paracoccidioides are responsible for paracoccidioidomycosis. The occurrence of drug toxicity and relapse in this disease justify the development of new antifungal agents. Compounds extracted from fungal extract have showing antifungal activity. Extracts of 78 fungi isolated from rocks of the Atacama Desert were tested in a microdilution assay against Paracoccidioides brasiliensis Pb18. Approximately 18% (5 of the extracts showed minimum inhibitory concentration (MIC values≤ 125.0 µg/mL. Among these, extract from the fungus UFMGCB 8030 demonstrated the best results, with an MIC of 15.6 µg/mL. This isolate was identified as Aspergillus felis (by macro and micromorphologies, and internal transcribed spacer, β-tubulin, and ribosomal polymerase II gene analyses and was grown in five different culture media and extracted with various solvents to optimise its antifungal activity. Potato dextrose agar culture and dichloromethane extraction resulted in an MIC of 1.9 µg/mL against P. brasiliensis and did not show cytotoxicity at the concentrations tested in normal mammalian cell (Vero. This extract was subjected to bioassay-guided fractionation using analytical C18RP-high-performance liquid chromatography (HPLC and an antifungal assay using P. brasiliensis. Analysis of the active fractions by HPLC-high resolution mass spectrometry allowed us to identify the antifungal agents present in the A. felis extracts cytochalasins. These results reveal the potential of A. felis as a producer of bioactive compounds with antifungal activity.

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

    Science.gov (United States)

    Kumar, Sasidharan Nishanth; Sreekala, Sreerag Ravikumar; Chandrasekaran, Dileep; Nambisan, Bala; Anto, Ruby John

    2014-01-01

    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.

  16. Purification and characterisation of an acidic and antifungal chitinase produced by a Streptomyces sp.

    Science.gov (United States)

    Karthik, Narayanan; Binod, Parameswaran; Pandey, Ashok

    2015-01-01

    An extremely acidic extracellular chitinase produced by a Streptomyces sp. was purified 12.44-fold by ammonium sulphate precipitation, ion-exchange chromatography and gel-permeation chromatography and further characterised. The molecular mass of the enzyme was estimated to be about 40 kDa by SDS-PAGE. The optimum pH and temperature of the purified enzyme were pH 2 and 6, and 50 °C respectively. The enzyme showed high stability in the acidic pH range of 2-6 and temperature stability of up to 50 °C. Additionally, the effect of some cations and other chemical compounds on the chitinase activity was studied. The activity of the enzyme was considerably retained under salinity conditions of up to 3%. The Km and Vmax values of the enzyme were determined to be 6.74 mg mL(-1) and 61.3 U mg(-1) respectively using colloidal chitin. This enzyme exhibited antifungal activity against phytopathogens revealing a potential biocontrol application in agriculture.

  17. Antifungal activity of natural compounds against Candida species isolated from HIV-positive patients

    Institute of Scientific and Technical Information of China (English)

    Dbora Oro; Andria Heissler; Eliandra Mirlei Rossi; Diane Scapin; Patrcia da Silva Malheiros; Everton Boff

    2015-01-01

    To evaluate the antifungal effect of Cinnamomum zeylanicum (C. zeylanicum) and Melaleuca alternifolia essential oils and honey against strains of Candida sp. from HIV-positive patients in order to subsidize new therapeutic strategies for candidiasis. Methods: The study evaluated the antifungal effect of natural antimicrobials against 30 strains of Candida sp. isolated from oral cavities in HIV-infected patients. Then, they were compared to the action of fluconazole and amphotericin B. Antifungal susceptibility was evaluated by the broth macrodilution technique and the minimum inhibitory concentration and the minimum fungicidal concentration were determined. Results: Among all antifungals evaluated in this study, amphotericin B was the one showing the best results; however, all compounds studied here showed inhibitory activities against isolates of Candida sp. Honey (0.031 3 to 64 μg/mL) demonstrated fungistatic activity inhibiting 70% of the isolates. C. zeylanicum essential oil (0.0313 to 64 μg/mL) inhibited 93.3% of the Candida strains and Melaleuca alternifolia essential oil (0.0313 to 64 μg/mL) was able to inhibit 73.3% of them. Conclusions: Therefore, all natural compounds evaluated in this study, especially C. zeylanicum essential oil, may become promising agents for oral candidiasis therapy including in HIV-positive patients.

  18. The Anti-helminthic Compound Mebendazole Has Multiple Antifungal Effects against Cryptococcus neoformans

    Science.gov (United States)

    Joffe, Luna S.; Schneider, Rafael; Lopes, William; Azevedo, Renata; Staats, Charley C.; Kmetzsch, Lívia; Schrank, Augusto; Del Poeta, Maurizio; Vainstein, Marilene H.; Rodrigues, Marcio L.

    2017-01-01

    Cryptococcus neoformans is the most lethal pathogen of the central nervous system. The gold standard treatment of cryptococcosis, a combination of amphotericin B with 5-fluorocytosine, involves broad toxicity, high costs, low efficacy, and limited worldwide availability. Although the need for new antifungals is clear, drug research and development (R&D) is costly and time-consuming. Thus, drug repurposing is an alternative to R&D and to the currently available tools for treating fungal diseases. Here we screened a collection of compounds approved for use in humans seeking for those with anti-cryptococcal activity. We found that benzimidazoles consist of a broad class of chemicals inhibiting C. neoformans growth. Mebendazole and fenbendazole were the most efficient antifungals showing in vitro fungicidal activity. Since previous studies showed that mebendazole reaches the brain in biologically active concentrations, this compound was selected for further studies. Mebendazole showed antifungal activity against phagocytized C. neoformans, affected cryptococcal biofilms profoundly and caused marked morphological alterations in C. neoformans, including reduction of capsular dimensions. Amphotericin B and mebendazole had additive anti-cryptococcal effects. Mebendazole was also active against the C. neoformans sibling species, C. gattii. To further characterize the effects of the drug a random C. gattii mutant library was screened and indicated that the antifungal activity of mebendazole requires previously unknown cryptococcal targets. Our results indicate that mebendazole is as a promising prototype for the future development of anti-cryptococcal drugs.

  19. Antifungal activity of natural compounds against Candida species isolated from HIV-positive patients

    Institute of Scientific and Technical Information of China (English)

    Débora; Oro; Andréia; Heissler; Eliandra; Mirlei; Rossi; Diane; Scapin; Patrícia; da; Silva; Malheiros; Everton; Boff

    2015-01-01

    Objective: To evaluate the antifungal effect of Cinnamomum zeylanicum(C. zeylanicum) and Melaleuca alternifolia essential oils and honey against strains of Candida sp. from HIV-positive patients in order to subsidize new therapeutic strategies for candidiasis.Methods: The study evaluated the antifungal effect of natural antimicrobials against 30 strains of Candida sp. isolated from oral cavities in HIV-infected patients. Then, they were compared to the action of fl uconazole and amphotericin B. Antifungal susceptibility was evaluated by the broth macrodilution technique and the minimum inhibitory concentration and the minimum fungicidal concentration were determined.Results: Among all antifungals evaluated in this study, amphotericin B was the one showing the best results; however, all compounds studied here showed inhibitory activities against isolates of Candida sp. Honey(0.031 3 to 64 μg/m L) demonstrated fungistatic activity inhibiting 70% of the isolates. C. zeylanicum essential oil(0.031 3 to 64 μg/m L) inhibited 93.3% of the Candida strains and Melaleuca alternifolia essential oil(0.031 3 to 64 μg/m L) was able to inhibit 73.3% of them.Conclusions: Therefore, all natural compounds evaluated in this study, especially C. zeylanicum essential oil, may become promising agents for oral candidiasis therapy including in HIV-positive patients.

  20. 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.

  1. NEW ANTIFUNGAL AROMATIC COMPOUNDS FROM THE SEEDS OF RHUS CORIARIA L.

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    Singh Onkar

    2011-01-01

    Full Text Available Phytochemical investigation of the ethanolic extract of the seeds of Rhus coriaria L. (Anacardiaceae afforded three new aromatic compounds identified as 1-methoxy-4-hydroxy-methylene naphthalene (coriarianaphthyl ether, 7-methoxy-5-methyl benzen-4-al-1-oic acid (coriariaoic acid and 1-dodecanoxy-2,8-dihydroxy-anthracene-15-oic acid (coriarianthracenyl ester along with known phytoconstituents n-tetracosane, n-pentacosane, anise alcohol, p-hydroxybenzyl alcohol, methyl lawsone and 2-hydroxymethylene naphthaquinone. The structures of all the isolated compounds have been identified on the basis of spectral data analysis and chemical reactions. All the new compounds showed antifungal activity.

  2. 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.

  3. Anti-Candida and anti-Cryptococcus antifungal produced by marine microorganisms.

    Science.gov (United States)

    El Amraoui, B; El Amraoui, M; Cohen, N; Fassouane, A

    2014-12-01

    In order to search for antifungal from biological origin, we performed a screening of marine microorganisms isolated from seawater, seaweed, sediment and marine invertebrates collected from different coastal areas of the Moroccan Atlantic Ocean. The antifungal activities of these isolates were investigated against the pathogenic yeasts involved in medical mycology. Whole cultures of 34 marine microorganisms were screened for antifungal activities using the method of agar diffusion against four yeasts. The results showed that among the 34 isolates studied, 13 (38%) strains have antifungal activity against at least one out of four yeast species, 11 isolates have anti-Candida albicans CIP 48.72 activity, 12 isolates have anti-C. albicans CIP 884.65 activity, 13 isolates have anti-Cryptococcus neoformans activity and only 6 isolates are actives against Candida tropicalis R2 resistant to nystatin and amphotericin B. Nine isolates showed strong fungicidal activity. Fourteen microorganisms were identified and assigned to the genera Acinetobacter, Aeromonas, Alcaligenes, Bacillus, Chromobacterium, Enterococcus, Pantoea, and Pseudomonas. Due to a competitive role for space and nutrient, the marine microorganisms could produce more antimicrobials; therefore these marine microorganisms were expected to be potential resources of natural products such as those we research: anti-Candida and anti-Cryptococcus fungicides.

  4. Study of the Cytotoxic and Antifungal Activities of Neolignans 8.O.4´ and Structurally Related Compounds

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    P. Matyus

    2000-03-01

    Full Text Available In the present work we report the antifungal and cytotoxic activities of a neolignan 8.O.4´series. The most active antifungal compounds show a significant cytotoxic effect which might be related.

  5. 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.

  6. Novel Antifungal Peptides Produced by Leuconostoc mesenteroides DU15 Effectively Inhibit Growth of Aspergillus niger.

    Science.gov (United States)

    Muhialdin, Belal J; Hassan, Zaiton; Abu Bakar, Fatimah; Algboory, Hussein L; Saari, Nazamid

    2015-05-01

    The ability of Leuconostoc mesenteroides DU15 to produce antifungal peptides that inhibit growth of Aspergillus niger was evaluated under optimum growth conditions of 30 °C for 48 h. The cell-free supernatant showed inhibitory activity against A. niger. Five novel peptides were isolated with the sequences GPFPL, YVPLF, LLHGVPLP, GPFPLEMTLGPT, and TVYPFPGPL as identified by de novo sequencing using PEAKS 6 software. Peptide LLHGVPLP was the only positively charged (cationic peptides) and peptide GPFPLEMTLGPT negatively charged (anionic), whereas the rest are neutral. The identified peptides had high hydrophobicity ratio and low molecular weights with amino acids sequences ranging from 5 to 12 residues. The mode of action of these peptides is observed under the scanning electron microscope and is due to cell lysis of fungi. This work reveals the potential of peptides from L. mesenteroides DU15 as natural antifungal preservatives in inhibiting the growth of A. niger that is implicated to the spoilage during storage.

  7. 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.

  8. EVALUATION OF STRUCTURAL AND BIOCHEMICAL ALTERATIONS IN ASPERGILLUS TERREUS BY THE ACTION OF ANTIFUNGAL ANTIBIOTIC COMPOUND FROM STREPTOMYCES SP. JF714876

    Directory of Open Access Journals (Sweden)

    Babanagare Shankaravva S.

    2011-11-01

    Full Text Available Antifungal compound obtained by Streptomyces sp. JF714876 was examined for its effect on morphological and biochemical alteration in Aspergillus terreus. Microscopic observation revealed swelling of hyphae with deformation and distortion in mycelial structure in presence of moderate concentration of antifungal compound. At high concentration, the compound exhibited fungicidal action. Antifungal treated Aspergillus terreus showed changes in its biochemical content such as, protein, carbohydrates, peroxidase, catalase and amylase as compared to untreated.

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

    Energy Technology Data Exchange (ETDEWEB)

    Luciano, Joao Henrique S.; Lima, Mary Anne S.; Silveira, Edilberto Rocha [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Centro de Ciencias. Dept. de Quimica Organica e Inorganica; Vasconcelos, Ilka Maria; Fernandes, Georgia Sampaio [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Bioquimica e Biologia Molecular; Souza, Elnatan Bezerra de [Universidade do Vale do Acarau, Sobral, CE (Brazil). Coord. de Biologia

    2010-07-01

    The new iridoid glucoside 10-O-vanilloyl-geniposidic acid has been isolated from the aerial parts of Alibertia myrciifolia along with hydroxyhopanone, 3{alpha},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)

  10. [Ajoene the main active compound of garlic (Allium sativum): a new antifungal agent].

    Science.gov (United States)

    Ledezma, Eliades; Apitz-Castro, Rafael

    2006-06-01

    The curative properties of garlic in medicine have been known for a long time. But, it was only in the last three decades when garlic properties were seriously investigated confirming its potential as therapeutic agent. Allicin, ajoene, thiosulfinates and a wide range of other organosulphurate compounds, are known to be the constituents linked to the garlic properties. Regarding the biochemical properties of these compounds, ajoene [(E,Z)-4,5,9 Trithiadodeca 1,6,11 Triene 9-oxide] is stable in water, and it can be obtained by chemical synthesis. There is evidence that some of the garlic constituents exert a wide variety of effects on different biological systems. However, ajoene is the garlic compound related to more biological activities, as showed in in vitro and in vivo systems. Those studies found that ajoene has antithrombotic, anti-tumoral,antifungal, and antiparasitic effects. This study deals with a recently described antifungal property of ajoene, and its potential use in clinical trails to treat several fungal infections.

  11. Antibacterial, Antifungal, and Insecticidal Potentials of Oxalis corniculata and Its Isolated Compounds

    Directory of Open Access Journals (Sweden)

    Azizur Rehman

    2015-01-01

    Full Text Available Oxalis corniculata is a common medicinal plant widely used against numerous infectious diseases. The agrochemical potential of methanolic extract, n-hexane, chloroform, ethyl acetate, and n-butanol fractions were assessed to measure the antibacterial, antifungal, and insecticidal activities of the plant. The crude, chloroform, and n-butanol soluble fractions showed excellent activities against Escherichia coli, Shigella dysenteriae, Salmonella typhi, and Bacillus subtilis but have no activity against Staphylococcus aureus. Similarly the crude, n-hexane, and chloroform fractions were also found to have significant activity against fungal strains including Fusarium solani, Aspergillus flexneri, and Aspergillus flavus and have no activity against Aspergillus niger. Chemical pesticides have shown very good results at the beginning, but with the passage of time the need was realized to use the natural plant sources for the safe control of insects. The current study will provide minor contribution towards it. High mortality rate was recorded for the crude extract and chloroform fraction against Tribolium castaneum. The two isolated compounds 5-hydroxy-6,7,8,4′-tetramethoxyflavone (1 and 5,7,4′-trihydroxy-6,8-dimethoxyflavone (2 were evaluated for antibacterial, antifungal, and insecticidal activities. The results showed that compound 2 was more active than compound 1 against the tested bacterial strains and insects.

  12. 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

  13. Isolation and characterization of antifungal peptides produced by Bacillus amyloliquefaciens LBM5006.

    Science.gov (United States)

    Benitez, Lisianne Brittes; Velho, Renata Voltolini; Lisboa, Marcia Pagno; Medina, Luis Fernando da Costa; Brandelli, Adriano

    2010-12-01

    Bacillus amyloliquefaciens LBM 5006 produces antagonistic activity against pathogenic bacteria and phytopathogenic fungi, including Aspergillus spp., Fusarium spp., and Bipolaris sorokiniana. PCR analysis revealed the presence of ituD, but not sfp genes, coding for iturin and surfactin, respectively. The antimicrobial substance produced by this strain was isolated by ammonium sulfate precipitation, gel filtration chromatography and 1-butanol extraction. The ultraviolet spectrum was typical of a polypeptide and the infrared spectrum indicates the presence of peptide bonds and acyl group(s). The antimicrobial substance was resistant to proteolytic enzymes and heat treatment, and was reactive with ninhydrin. Mass spectroscopy analysis indicated that B. amyloliquefaciens LBM 5006 produces two antimicrobial peptides, with main peaks at m/z 1,058 Da and 1,464 Da, corresponding to iturin-like and fengycin-like peptides, respectively. B. amyloliquefaciens LBM 5006 showed significant activity against phytopatogenic fungi, showing potential for use as a biocontrol agent or production of antifungal preparations.

  14. Antifungal activity of oregano extract against A. Versicolor, E. Nidulans and Eurotium spp.: Producers of sterigmatocystin

    Directory of Open Access Journals (Sweden)

    Kocić-Tanackov Sunčica D.

    2011-01-01

    Full Text Available The paper presents the influence of oregano extract (Origanum vulgare L. on growth of Aspergillus versicolor, Emericella nidulans, Eurotium herbariorum, E. amstelodami, E. chevalieri and E. rubrum - producers of sterigmatocystin (STC isolated from salads. Antifungal tests were performed by agar plates method. The composition of the active component of extract was determined by GC-MS method and the major components were: carvacrol (34.20%, triacetin (22.91%, carvone (18.05%, p-cymene (8.05% and thymol (3.74%. The examined extract showed the ability to reduce mold growth at all applied concentrations. Minimum inhibitory concentrations (MIC for E. nidulans, E. chevalieri and E. amstelodami were 2.5% (v/v and over 2.5% (v/v for A. versicolor. At 1.5% (v/v concentration the extract completely inhibited the growth of E. rubrum, whereas higher dose of 2.5% (v/v was fungicidal against E. herbariorum. Besides its sensory role in food products, the examined oregano extract also exhibits antifungal activities against producers of STC.

  15. Cabanillasin, a new antifungal metabolite, produced by entomopathogenic Xenorhabdus cabanillasii JM26.

    Science.gov (United States)

    Houard, Jessica; Aumelas, André; Noël, Thierry; Pages, Sylvie; Givaudan, Alain; Fitton-Ouhabi, Valérie; Villain-Guillot, Philippe; Gualtieri, Maxime

    2013-10-01

    Since the early 1980s, fungi have emerged as a major cause of human disease. Fungal infections are associated with high levels of morbidity and mortality, and are now recognized as an important public health problem. Gram-negative bacterial strains of genus Xenorhabdus are known to form symbiotic associations with soil-dwelling nematodes of the Steinernematidae family. We describe here the discovery of a new antifungal metabolite, cabanillasin, produced by Xenorhabdus cabanillasii. We purified this molecule by cation-exchange chromatography and reverse-phase chromatography. We then determined the chemical structure of cabanillasin by homo- and heteronuclear NMR and MS-MS. Cabanillasin was found to be active against yeasts and filamentous fungi involved in opportunistic infections.

  16. 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.

  17. Antifungal properties of 2-bromo-3-fluorosuccinic acid esters and related compounds.

    Science.gov (United States)

    Gershon, H; Shanks, L

    1977-04-01

    Twelve esters (C1-C6) of erythro- and threo-2-bromo-3-fluorosuccinic acid and related compounds were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.7 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. At pH 7.0 in the presence of 10% beef serum, no consistent pattern in the fungitoxicity of the erythro- and threo-2-bromo-3-fluorosuccinate esters was seen. Increasing the length of the ester function affects fungitoxicity as follows: C2 greater than C1 greater than C3 greater than C4 greater than C5 greater than C6. The most fungitoxic compound in this study was threo-ethyl 2-bromo-3-fluorosuccinate (C. albicans, 14 mug/ml; A. niger, 30 mug/ml; M. mucedo, 9 mug/ml; T. mentagrophytes, 5 mug/ml). Due to the ease of dehydrohalogenation, the fungitoxicity of 2-bromo-3-fluorosuccinic acid esters may be the result of a mixture composed of the parent compound, the bromo- and fluorofumaric acid esters, and HF and HBr of which part may be formed extracellularly and part within the cell.

  18. 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 ...

  19. 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.

  20. Synthesis, characterisation and antifungal activity of chemically and fungal-produced silver nanoparticles against Trichophyton rubrum

    OpenAIRE

    Pereira, Leonel; Dias, Nicolina; Carvalho,Juliana de; Fernandes, Sara; Santos, Cledir; Lima, Nelson

    2014-01-01

    Aims To characterise and explore the potential in extracellular biosynthesis of silver nanoparticles (AgNPs) by Penicillium chrysogenum and Aspergillus oryzae and to investigate the antifungal effect of chemically vs. biologically synthesised AgNPs comparing with conventional antifungal drugs against Trichophyton rubrum. Methods and Results Chemically synthesised AgNPs (Chem-AgNPs) coated with polyvinylpyrrolidone (PVP) were synthesised by chemical reduction method with glucose in PV...

  1. 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.

  2. Trichosporon inkin biofilms produce extracellular proteases and exhibit resistance to antifungals.

    Science.gov (United States)

    de Aguiar Cordeiro, Rossana; Serpa, Rosana; Flávia Uchoa Alexandre, Camila; de Farias Marques, Francisca Jakelyne; Vladia Silva de Melo, Charlline; da Silva Franco, Jônatas; José de Jesus Evangelista, Antonio; Pires de Camargo, Zoilo; Samia Nogueira Brilhante, Raimunda; Fabio Gadelha Rocha, Marcos; Luciano Bezerra Moreira, José; de Jesus Pinheiro Gomes Bandeira, Tereza; Júlio Costa Sidrim, José

    2015-11-01

    The aim of this study was to determine experimental conditions for in vitro biofilm formation of clinical isolates of Trichosporon inkin, an important opportunistic pathogen in immunocompromised patients. Biofilms were formed in microtitre plates in three different media (RPMI, Sabouraud and CLED), with inocula of 104, 105 or 106 cells ml- 1, at pH 5.5 and 7.0, and at 35 and 28 °C, under static and shaking conditions for 72 h. Growth kinetics of biofilms were evaluated at 6, 24, 48 and 72 h. Biofilm milieu analysis were assessed by counting viable cells and quantification of nucleic acids released into biofilm supernatants. Biofilms were also analysed for proteolytic activity and antifungal resistance against amphotericin B, caspofungin, fluconazole, itraconazole and voriconazole. Finally, ultrastructural characterization of biofilms formed in microtitre plates and catheter disks was performed by scanning electron microscopy. Greater biofilm formation was observed with a starter inoculum of 106 cells ml- 1, at pH 7.0 at 35 °C and 80 r.p.m., in both RPMI and Sabouraud media. Growth kinetics showed an increase in both viable cells and biomass with increasing incubation time, with maximum production at 48 h. Biofilms were able to disperse viable cells and nucleic acids into the supernatant throughout the developmental cycle. T. inkin biofilms produced more protease than planktonic cells and showed high tolerance to amphotericin B, caspofungin and azole derivatives. Mature biofilms were formed by different morphotypes, such as blastoconidia, arthroconidia and hyphae, in a strain-specific manner. The present article details the multicellular lifestyle of T. inkin and provides perspectives for further research.

  3. Method of producing purified carotenoid compounds

    Science.gov (United States)

    Eggink, Laura (Inventor)

    2007-01-01

    A method of producing a carotenoid in solid form includes culturing a strain of Chlorophyta algae cells in a minimal inorganic medium and separating the algae comprising a solid form of carotenoid. In one embodiment f the invention, the strain of Chlorophyta algae cells includes a strain f Chlamydomonas algae cells.

  4. 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 C9 H15 NO3 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.

  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 speciesUlva lactuca,Sargassum tenerrimum andLaurencia obtusa collected from Okha coast, Western India

    Institute of Scientific and Technical Information of China (English)

    Megha Barot; Nirmal Kumar J.I.; Rita N. Kumar

    2016-01-01

    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 ofUlva 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. Use of the Aspergillus oryzae actin gene promoter in a novel reporter system for exploring antifungal compounds and their target genes.

    Science.gov (United States)

    Marui, Junichiro; Yoshimi, Akira; Hagiwara, Daisuke; Fujii-Watanabe, Yoshimi; Oda, Ken; Koike, Hideaki; Tamano, Koichi; Ishii, Tomoko; Sano, Motoaki; Machida, Masayuki; Abe, Keietsu

    2010-08-01

    Demand for novel antifungal drugs for medical and agricultural uses has been increasing because of the diversity of pathogenic fungi and the emergence of drug-resistant strains. Genomic resources for various living species, including pathogenic fungi, can be utilized to develop novel and effective antifungal compounds. We used Aspergillus oryzae as a model to construct a reporter system for exploring novel antifungal compounds and their target genes. The comprehensive gene expression analysis showed that the actin-encoding actB gene was transcriptionally highly induced by benomyl treatment. We therefore used the actB gene to construct a novel reporter system for monitoring responses to cytoskeletal stress in A. oryzae by introducing the actB promoter::EGFP fusion gene. Distinct fluorescence was observed in the reporter strain with minimum background noise in response to not only benomyl but also compounds inhibiting lipid metabolism that is closely related to cell membrane integrity. The fluorescent responses indicated that the reporter strain can be used to screen for lead compounds affecting fungal microtubule and cell membrane integrity, both of which are attractive antifungal targets. Furthermore, the reporter strain was shown to be technically applicable for identifying novel target genes of antifungal drugs triggering perturbation of fungal microtubules or membrane integrity.

  8. Early State Research on Antifungal Natural Products

    Directory of Open Access Journals (Sweden)

    Melyssa Negri

    2014-03-01

    Full Text Available Nosocomial infections caused by fungi have increased greatly in recent years, mainly due to the rising number of immunocompromised patients. However, the available antifungal therapeutic arsenal is limited, and the development of new drugs has been slow. Therefore, the search for alternative drugs with low resistance rates and fewer side effects remains a major challenge. Plants produce a variety of medicinal components that can inhibit pathogen growth. Studies of plant species have been conducted to evaluate the characteristics of natural drug products, including their sustainability, affordability, and antimicrobial activity. A considerable number of studies of medicinal plants and alternative compounds, such as secondary metabolites, phenolic compounds, essential oils and extracts, have been performed. Thus, this review discusses the history of the antifungal arsenal, surveys natural products with potential antifungal activity, discusses strategies to develop derivatives of natural products, and presents perspectives on the development of novel antifungal drug candidates.

  9. 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.

  10. Antifungal compounds of Xylaria sp., an endophytic fungus isolated from Palicourea marcgravii (Rubiaceae); Substancias antifungicas de Xylaria sp., um fungo endofitico isolado de Palicourea marcgravii (Rubiaceae)

    Energy Technology Data Exchange (ETDEWEB)

    Cafeu, Mariana C.; Silva, Geraldo H.; Teles, Helder L.; Bolzani, Vanderlan da S.; Araujo, Angela R. [UNESP, Araraquara, SP (Brazil). Inst. de Quimica]. E-mail: araujoar@iq.unesp.br; Young, Maria Claudia M. [Instituto de Botanica, Sao Paulo, SP (Brazil). Secao de Fisiologia e Bioquimica de Plantas; Pfenning, Ludwig H. [Universidade Federal de Lavras, MG (Brazil). Dept. de Fitopatologia

    2005-11-15

    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. (author)

  11. 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.

  12. Identification and antifungal activity of novel organic compounds found in cuticular and internal lipids of medically important flies.

    Science.gov (United States)

    Gołębiowski, Marek; Cerkowniak, Magdalena; Urbanek, Aleksandra; Dawgul, Małgorzata; Kamysz, Wojciech; Boguś, Mieczysława I; Stepnowski, Piotr

    2015-01-01

    Novel organic compounds found in the cuticular and internal lipids of medically important flies were identified. Uracil, 9-tricosene, 1-oleoyl glycerol, dimethyl suberate and butyl stearate were tested for their potential antifungal activity. Minimal inhibitory concentrations of the compounds against reference strains of fungi were determined. Uracil and dimethyl suberate slightly inhibited the growth of entomopathogenic fungi. The cuticular and internal lipids of Calliphora vicina, Calliphora vomitoria, Sarcophaga carnaria and Musca domestica were studied by gas chromatography (GC) combined with mass spectrometry (GC/MS). A comparison of the lipid extracts between the preimaginal and mature stages showed adults flies contained a higher total content of the identified components. Furthermore, their amounts distinctly predominated in the internal lipids of all the species. The amount of 9-tricosene was the highest in adults of C. vicina, while the larvae and pupae had a definitively lower amount of this compound. Uracil was found to be the most abundant component in extracts obtained from C. vomitoria especially in the internal lipids of adults. 1-oleoyl glycerol was detected in all of the examined species of flies. It was most abundant in the internal extracts isolated from the larvae of C. vicina and the pupae of C. vomitoria. Suberic acid dimethyl ester was found in the larval and pupal internal lipids of C. vicina and S. carnaria in low amounts. Butyl stearate was identified only in the internal lipids of the larvae and adults of houseflies.

  13. 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...

  14. 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.

  15. Methods and systems for producing compounded ultrasound images

    DEFF Research Database (Denmark)

    2012-01-01

    Disclosed is a method for producing compounded ultrasound images by beamforming a first and a second low-resolution image using data from a first ultrasound emission, beamforming a third and a fourth low-resolution image using data from a second ultrasound emission, summing said first and said...

  16. 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

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

    Science.gov (United States)

    Cline, Andrew R; Skelley, Paul E; Kinnee, Scott A; Rooney-Latham, Suzanne; Winterton, Shaun L; Borkent, Christopher J; Audisio, Paolo

    2014-01-01

    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 on Fusarium

  18. Identification of volatile compounds produced by the bacterium Burkholderia tropica that inhibit the growth of fungal pathogens

    Science.gov (United States)

    Tenorio-Salgado, Silvia; Tinoco, Raunel; Vazquez-Duhalt, Rafael; Caballero-Mellado, Jesus; Perez-Rueda, Ernesto

    2013-01-01

    It has been documented that bacteria from the Burkholderia genera produce different kinds of compounds that inhibit plant pathogens, however in Burkholderia tropica, an endophytic diazotrophic and phosphate-solubilizing bacterium isolated from a wide diversity of plants, the capacity to produce antifungal compounds has not been evaluated. In order to expand our knowledge about Burkholderia tropica as a potential biological control agent, we analyzed 15 different strains of this bacterium to evaluate their capacities to inhibit the growth of four phytopathogenic fungi, Colletotrichum gloeosporioides, Fusarium culmorum, Fusarium oxysporum and Sclerotium rolffsi. Diverse analytical techniques, including plant root protection and dish plate growth assays and gas chromatography-mass spectroscopy showed that the fungal growth inhibition was intimately associated with the volatile compounds produced by B. tropica and, in particular, two bacterial strains (MTo293 and TTe203) exhibited the highest radial mycelial growth inhibition. Morphological changes associated with these compounds, such as disruption of fungal hyphae, were identified by using photomicrographic analysis. By using gas chromatography-mass spectroscopy technique, 18 volatile compounds involved in the growth inhibition mechanism were identified, including α-pinene and limonene. In addition, we found a high proportion of bacterial strains that produced siderophores during growth with different carbon sources, such as alanine and glutamic acid; however, their roles in the antagonism mechanism remain unclear. PMID:23680857

  19. Preparative Scale MS-Guided Isolation of Bioactive Compounds Using High-Resolution Flash Chromatography: Antifungals from Chiloscyphus polyanthos as a Case Study.

    Science.gov (United States)

    Azzollini, Antonio; Favre-Godal, Quentin; Zhang, Jiaozhen; Marcourt, Laurence; Ebrahimi, Samad Nejad; Wang, Shuqi; Fan, Peihong; Lou, Hongxiang; Guillarme, Davy; Queiroz, Emerson Ferreira; Wolfender, Jean-Luc

    2016-07-01

    In natural product research, the efficient purification of molecules from large amounts of complex extracts is a key element. In this regard, an integrative strategy for efficient MS-guided isolation of antifungal compounds has been developed. First, off-line HPLC antifungal activity-based profiling and HPLC-PDA-MS profiling were used to localize the compounds of interest on the analytical scale. Then, the analytical gradient was geometrically transferred to the flash chromatographic level. Finally, an MS-triggered isolation of the localized bioactive molecules was realized using high-resolution flash chromatographic columns (15 µm spherical particles) coupled to a single quadrupole mass spectrometer via a splitter system. This isolation strategy was applied for the MS-targeted purification of antifungal principles from the liverwort Chiloscyphus polyanthos. This rational methodology has high potential for the targeted large-scale purification of bioactive compounds, avoiding the need to repeat a given bioassay at each isolation step. Seven sesquiterpene lactones were isolated, of which five were found to be bioactive and one was reported as a new compound. The absolute configuration of some compounds was established for the first time by electronic circular dichroism spectroscopy.

  20. Diversity and functions of volatile organic compounds produced by Streptomyces from a disease-suppressive soil

    Directory of Open Access Journals (Sweden)

    Viviane eCordovez

    2015-10-01

    Full Text Available In disease-suppressive soils, plants are protected from infections by specific root pathogens due to the antagonistic activities of soil and rhizosphere microorganisms. For most disease-suppressive soils, however, the microorganisms and mechanisms involved in pathogen control are largely unknown. Our recent studies identified Actinobacteria as the most dynamic phylum in a soil suppressive to the fungal root pathogen Rhizoctonia solani. Here we isolated and characterized 300 isolates of rhizospheric Actinobacteria from the Rhizoctonia-suppressive soil. Streptomyces species were the most abundant, representing approximately 70% of the isolates. Streptomyces are renowned for the production of an exceptionally large number of secondary metabolites, including volatile organic compounds (VOCs. VOC profiling of 12 representative Streptomyces isolates by SPME-GC-MS allowed a more refined phylogenetic delineation of the Streptomyces isolates than the sequencing of 16S rRNA and the house-keeping genes atpD and recA only. VOCs of several Streptomyces isolates inhibited hyphal growth of R. solani and significantly enhanced plant shoot and root biomass. Coupling of Streptomyces VOC profiles with their effects on fungal growth, pointed to VOCs potentially involved in antifungal activity. Subsequent assays with five synthetic analogues of the identified VOCs showed that methyl 2-methylpentanoate, 1,3,5-trichloro-2-methoxy benzene and the VOCs mixture have antifungal activity. In conclusion, our results point to a potential role of VOC-producing Streptomyces in disease suppressive soils and show that VOC profiling of rhizospheric Streptomyces can be used as a complementary identification tool to construct strain-specific metabolic signatures.

  1. Diversity and functions of volatile organic compounds produced by Streptomyces from a disease-suppressive soil

    Science.gov (United States)

    Cordovez, Viviane; Carrion, Victor J.; Etalo, Desalegn W.; Mumm, Roland; Zhu, Hua; van Wezel, Gilles P.; Raaijmakers, Jos M.

    2015-01-01

    In disease-suppressive soils, plants are protected from infections by specific root pathogens due to the antagonistic activities of soil and rhizosphere microorganisms. For most disease-suppressive soils, however, the microorganisms and mechanisms involved in pathogen control are largely unknown. Our recent studies identified Actinobacteria as the most dynamic phylum in a soil suppressive to the fungal root pathogen Rhizoctonia solani. Here we isolated and characterized 300 isolates of rhizospheric Actinobacteria from the Rhizoctonia-suppressive soil. Streptomyces species were the most abundant, representing approximately 70% of the isolates. Streptomyces are renowned for the production of an exceptionally large number of secondary metabolites, including volatile organic compounds (VOCs). VOC profiling of 12 representative Streptomyces isolates by SPME-GC-MS allowed a more refined phylogenetic delineation of the Streptomyces isolates than the sequencing of 16S rRNA and the house-keeping genes atpD and recA only. VOCs of several Streptomyces isolates inhibited hyphal growth of R. solani and significantly enhanced plant shoot and root biomass. Coupling of Streptomyces VOC profiles with their effects on fungal growth, pointed to VOCs potentially involved in antifungal activity. Subsequent assays with five synthetic analogs of the identified VOCs showed that methyl 2-methylpentanoate, 1,3,5-trichloro-2-methoxy benzene and the VOCs mixture have antifungal activity. In conclusion, our results point to a potential role of VOC-producing Streptomyces in disease suppressive soils and show that VOC profiling of rhizospheric Streptomyces can be used as a complementary identification tool to construct strain-specific metabolic signatures. PMID:26500626

  2. Antifungal activity of natural compounds against Candida species isolated from HIV-positive patients

    Directory of Open Access Journals (Sweden)

    Débora Oro

    2015-09-01

    Conclusions: Therefore, all natural compounds evaluated in this study, especially C. zeylanicum essential oil, may become promising agents for oral candidiasis therapy including in HIV-positive patients.

  3. Biocide effects of volatile organic compounds produced by potential biocontrol rhizobacteria on Sclerotinia sclerotiorum

    Directory of Open Access Journals (Sweden)

    Annalisa eGiorgio

    2015-10-01

    Full Text Available Six rhizobacteria isolated from common bean and able to protect bean plants from the common bacterial blight causal agent, were in vitro evaluated for their potential antifungal effects toward different plant pathogenic fungi, mostly soil-borne. By dual culture assays, the above bacteria resulted producing diffusible and volatile metabolites which inhibited the growth of the majority of the pathogens under study. In particular, the latter substances highly affected the mycelium growth of Sclerotinia sclerotiorum strains, one of which was selected for further studies either on mycelium or sclerotia.Gas chromatographic analysis of the bacterial volatiles led to the identification of an array of volatile organic compounds (VOCs. Time course studies showed the modification of the VOCs profile along a period of 5 days. In order to evaluate the single detected VOC effects on fungal growth, some of the pure compounds were tested on S. sclerotiorum mycelium and their minimal inhibitory quantities were determined. Similarly, the minimal inhibitory quantities on sclerotia germination were also defined. Moreover, observations by light and transmission electron microscopes highlighted hyphae cytoplasm granulation and ultrastructural alterations at cell organelles, mostly membranes, mitochondria and endoplasmic reticulum. The membranes appeared one of the primary targets of bacterial volatiles, as confirmed by haemolytic activity observed for the majority of pure VOCs. However, of interest is the alteration observed on mitochondria as well.

  4. Functional assignment of YvgO, a novel set of purified and chemically characterized proteinaceous antifungal variants produced by Bacillus thuringiensis SF361.

    Science.gov (United States)

    Manns, David C; Churey, John J; Worobo, Randy W

    2012-04-01

    This study reports a novel class of antifungal protein derived from bacterial origin. Bacillus thuringiensis SF361, the strain also responsible for producing the novel bacteriocin thurincin H, exhibits broad antifungal activity against select members of several fungal genera, including Aspergillus, Byssochlamys, and Penicillium, as well as the pathogenic yeast Candida albicans. Optimal antifungal production and secretion were observed after-log phase growth when incubated at 37°C in a carbohydrate-free growth medium. High-performance liquid chromatography purification was performed after pH-selective ammonium sulfate precipitation and size-exclusion chromatography. Intact mass analysis and peptide mass fingerprinting identified the 13,484-Da protein to be a mass homolog to the YvgO protein construct sequenced from Bacillus cereus AH 1134. Further analysis via amino-terminal sequencing also revealed the existence of four distinct yet equally efficacious YvgO variants differing only within the first four N-terminal residues. YvgO was found to be remarkably stable, maintaining its antifungal activity under a wide pH and temperature range. When assayed against the toxigenic species Byssochlamys fulva H25, the selected primary filamentous fungal indicator, the MIC was estimated to be 1.5 ppm. Candida albicans 3153 was more resistant, exhibiting MICs between 25 and 800 ppm, depending on growth conditions. YvgO is unique among antifungals, showing no known sequential or functional homology to the typical classes of antifungal proteins, including common membrane-acting agents such as cellulases and glucanases. Due to its activity against an array of pathogenic and spoilage fungi, the potentials for clinical, agricultural, and food-processing applications are encouraging.

  5. 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)

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

    DEFF Research Database (Denmark)

    Valsaraj, R; Pushpangadan, P; Smitt, U W;

    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...

  7. Antifungal activity of extracts and select compounds in heartwood of seven western conifers toward Phytophthora ramorum

    Science.gov (United States)

    Individual compounds and ethyl acetate extracts from heartwood of seven conifer species were tested for fungicidal activity against Phytophthora ramorum. Extracts from incense and western red cedar exhibited the strongest activity (EC50 589 and 646 ppm, respectively), yellow-cedar, western juniper,...

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

    Science.gov (United States)

    Bills, Gerald F; Yue, Qun; Chen, Li; Li, Yan; An, Zhiqiang; Frisvad, Jens C

    2016-03-01

    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 that it is a distinct and novel species of Aspergillus sect. Nidulantes. The taxonomic novelty, Aspergillus mulundensis, is introduced for this historically important echinocandin-producing strain. The closely related A. nidulans FGSC A4 has one of the most extensively characterized secondary metabolomes of any filamentous fungus. Comparison of the full-genome sequences of DSMZ 5745 and FGSC A4 indicated that the two strains share 33 secondary metabolite biosynthetic gene clusters. These shared gene clusters represent ~45% of the total secondary metabolome of each strain, thus indicating a high level intraspecific divergence in terms of secondary metabolism.

  9. 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)

  10. 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.

  11. Identification of a naturally produced antifungal compound with activity against pecan scab

    Science.gov (United States)

    Pecan scab limits the productivity of pecan in the southeastern United States. Alternatives to conventional fungicides are needed, and ideally should be biorational, of low environmental risk with a reduced risk for fungicide resistance. Extracts of a bacterial symbiont (Photorhabdus luminescens) fr...

  12. Triazole antifungals: a review.

    Science.gov (United States)

    Peyton, L R; Gallagher, S; Hashemzadeh, M

    2015-12-01

    Invasive fungal infections and systemic mycosis, whether from nosocomial infection or immunodeficiency, have been on an upward trend for numerous years. Despite advancements in antifungal medication, treatment in certain patients can still be difficult for reasons such as impaired organ function, limited administration routes or poor safety profiles of the available antifungal medications. The growing number of invasive fungal species becoming resistant to current antifungal medications is of appreciable concern. Triazole compounds containing one or more 1,2,4-triazole rings have been shown to contain some of the most potent antifungal properties. Itracon-azole and fluconazole were some of the first triazoles synthesized, but had limitations associated with their use. Second-generation triazoles such as voriconazole, posa-conazole, albaconazole, efinaconazole, ravuconazole and isavuconazole are all derivatives of either itraconazole or fluconazole, and designed to overcome the deficiencies of their parent drugs. The goal of this manuscript is to review antifungal agents derived from triazole.

  13. Antifungal testing and high-throughput screening of compound library against Geomyces destructans, the etiologic agent of geomycosis (WNS in bats.

    Directory of Open Access Journals (Sweden)

    Sudha Chaturvedi

    Full Text Available Bats in the northeastern U.S. are affected by geomycosis caused by the fungus Geomyces destructans (Gd. This infection is commonly referred to as White Nose Syndrome (WNS. Over a million hibernating bats have died since the fungus was first discovered in 2006 in a cave near Albany, New York. A population viability analysis conducted on little brown bats (Myotis lucifugus, one of six bat species infected with Gd, suggests regional extinction of this species within 20 years. The fungus Gd is a psychrophile ("cold loving", but nothing is known about how it thrives at low temperatures and what pathogenic attributes allow it to infect bats. This study aimed to determine if currently available antifungal drugs and biocides are effective against Gd. We tested five Gd strains for their susceptibility to antifungal drugs and high-throughput screened (HTS one representative strain with SpectrumPlus compound library containing 1,920 compounds. The results indicated that Gd is susceptible to a number of antifungal drugs at concentrations similar to the susceptibility range of human pathogenic fungi. Strains of Gd were susceptible to amphotericin B, fluconazole, itraconazole, ketoconazole and voriconazole. In contrast, very high MICs (minimum inhibitory concentrations of flucytosine and echinocandins were needed for growth inhibition, which were suggestive of fungal resistance to these drugs. Of the 1,920 compounds in the library, a few caused 50%--to greater than 90% inhibition of Gd growth. A number of azole antifungals, a fungicide, and some biocides caused prominent growth inhibition. Our results could provide a theoretical basis for future strategies aimed at the rehabilitation of most affected bat species and for decontamination of Gd in the cave environment.

  14. In Vitro evaluation of antifungal activity of Bioactive Compound 2H-FURO [2,3-H]-1-Benzopyran-2-one against seed borne fungi of maize

    Directory of Open Access Journals (Sweden)

    B. Kiran

    2012-03-01

    Full Text Available Antifungal activity of bioactive compound 2HFuro[ 2,3-H]-1-benzopyran-2-one recorded a significant activity at 100-1000 ppm concentration against all the ten Aspergillus species tested. A. flavus recorded complete inhibition at 100 ppm concentration, A. niger at 500 ppm, A. fumigates at 600 ppm, A. flavus oryzae and A. flavus columnaris at 700 ppm respectively. A. ochraceous and A. flavipes recorded complete inhibition at 900 ppm concentration. Compared to synthetic fungicide Captan and Thiram at 2000ppm concentration. Minimum Inhibitory Concentration (MIC of bioactive compound was in the range of 100- 900ppm concentration against all the test fungi.

  15. Alternative method to detect compounds produced by Gambierdiscus spp.

    Directory of Open Access Journals (Sweden)

    Jon Andoni Sánchez

    2014-06-01

    Full Text Available Ciguatoxins (CTXs and CTX precursors are produced by several Gambierdiscus spp. These polyether toxins are associated to ciguatera fish poisoning (CFP. In addition to CTX, maitotoxins (MTX and gambierol are also produced by these dinoflagellates. MTX mechanism of action is strictly Ca2+ dependent, since the toxin induces a massive cytoplasmatic Ca2+ entrance. However, CTX activates the voltage-dependent sodium channels and no relation with calcium fluxes has been showed. The aim of this work was to study the effect of both toxins in the cytoplasmic calcium levels in the SH-SY5Y neuroblastoma cell line by using the fluorescent probe Fura-2 AM. Two completely different calcium profiles were obtained. While, MTX induces a sustained dose-dependent increase in Fura-2 ratio, CTX produces a light increase in dye ratio. From MTX results a calibration curve concentration versus Fura-2 ratio was obtained where the toxin concentration of an unknown sample can be calculated. Then, the effect of four samples from Gambierdiscus cultures was studied and different calcium profiles were obtained. A high increase in Fura-2 ratio was observed in two samples. The calcium profile was similar to MTX and by using the calibration curve the amount of toxin was calculated (4.9 and 1.8 nM of MTX. In the other samples, from the Fura-2 results the presence of CTX like compounds can be established.

  16. Algicidal and antifungal compounds from the roots of Ruta graveolens and synthesis of their analogs.

    Science.gov (United States)

    Meepagala, Kumudini M; Schrader, Kevin K; Wedge, David E; Duke, Stephen O

    2005-11-01

    Bioassay-guided fractionation of the ethyl acetate extract of Ruta graveolens roots yielded rutacridone epoxide with potent selective algicidal activity towards the 2-methyl-isoborneol (MIB)-producing blue-green alga Oscillatoria perornata, with relatively little effect on the green alga Selenastrum capricornutum. The diol-analog of rutacridone epoxide, gravacridondiol, which was also present in the same extract, had significantly less activity towards O. perornata. Rutacridone epoxide also showed significantly higher activity than commercial fungicides captan and benomyl in our micro-bioassay against the agriculturally important pathogenic fungi Colletotrichum fragariae, C. gloeosporioides, C. acutatum, and Botrytis cineara and Fusarium oxysporium. Rutacridone epoxide is reported as a direct-acting mutagen, precluding its use as an agrochemical. In order to understand the structure-activity relationships and to develop new potential biocides without toxicity and mutagenicity, some analogs containing the (2-methyloxiranyl)-dihydrobenzofuran moiety with an epoxide were synthesized and tested. None of the synthetic analogs showed comparable activities to rutacridone epoxide. The absolute stereochemistry of rutacridone was determined to be 2'(R) and that of rutacridone epoxide to be 2'(R), 3'(R) by CD and NMR analysis.

  17. Compounds produced by motor burnouts of refrigeration systems

    Energy Technology Data Exchange (ETDEWEB)

    Koester, C.; Hawley-Fedder, R.; Foiles, L.

    1995-05-24

    The phase-out of chlorofluorocarbons has necessitated the introduction of alternate refrigerants. R22 (CF{sub 2}ClH), R134a (CF{sub 3}CH{sub 2}F), and R507 (50/50 CHF{sub 2}CF{sub 3}/CF{sub 3}CH{sub 3}) are newer fluids which are used in cooling systems. Recently, concern over the possible formation of toxic compounds during electrical arcing through these fluids has prompted us to identify their electrical breakdown products by electron ionization GC/MS. For example, it is known that perfluoroisobutylene (PFIB), which have an threshold limit value of 10 ppb (set by the American Conference of Government Industrial Hygienists), is produced from the thermal and electrical breakdown of some refrigerants. We have used specially designed test cells, equipped with electrodes, to simulate the electrical breakdown of R22, R134a, and R507 in refrigeration systems.

  18. 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.

  19. Bioactivity of volatile organic compounds produced by Pseudomonas tolaasii

    Directory of Open Access Journals (Sweden)

    Pietro eLo Cantore

    2015-10-01

    Full Text Available Pseudomonas tolaasii is the main bacterial pathogen of several mushroom species. In this paper we report that strains of P. tolaasii produce volatile substances inducing in vitro mycelia growth inhibition of Pleurotus ostreatus and P. eryngii, and Agaricus bisporus and P. ostreatus basidiome tissue blocks brown discoloration. P. tolaasii strains produced the volatile ammonia but not hydrogen cyanide. Among the volatiles detected by GC-MS, methanethiol, dimethyl disulfide, and 1-undecene were identified. The latter, when assayed individually as pure compounds, led to similar effects noticed when P. tolaasii volatiles natural blend was used on mushrooms mycelia and basidiome tissue blocks. Furthermore, the natural volatile mixture, resulted toxic toward lettuce and broccoli seedling growth. In contrast, pure volatiles showed different activity according to their nature and/or doses applied. Indeed, methanethiol resulted toxic at all the doses used, while dimethyl disulfide toxicity was assessed till a quantity of 1.25 µg, below which it caused, together with 1-undecene ( 10 µg, broccoli growth increase.

  20. Antifungal activity of Wickerhamomyces anomalus and Lactobacillus plantarum during sourdough fermentation: identification of novel compounds and long-term effect during storage of wheat bread.

    Science.gov (United States)

    Coda, Rossana; Cassone, Angela; Rizzello, Carlo G; Nionelli, Luana; Cardinali, Gianluigi; Gobbetti, Marco

    2011-05-01

    This study aimed at investigating the antifungal activity of Wickerhamomyces anomalus and sourdough lactic acid bacteria to extend the shelf life of wheat flour bread. The antifungal activity was assayed by agar diffusion, growth rate inhibition, and conidial germination assays, using Penicillium roqueforti DPPMAF1 as the indicator fungus. Sourdough fermented by Lactobacillus plantarum 1A7 (S1A7) and dough fermented by W. anomalus LCF1695 (D1695) were selected and characterized. The water/salt-soluble extract of S1A7 was partially purified, and several novel antifungal peptides, encrypted into sequences of Oryza sativa proteins, were identified. The water/salt-soluble extract of D1695 contained ethanol and, especially, ethyl acetate as inhibitory compounds. As shown by growth inhibition assays, both water/salt-soluble extracts had a large inhibitory spectrum, with some differences, toward the most common fungi isolated from bakeries. Bread making at a pilot plant was carried out with S1A7, D1695, or a sourdough started with a combination of both strains (S1A7-1695). Slices of the bread manufactured with S1A7-1695 did not show contamination by fungi until 28 days of storage in polyethylene bags at room temperature, a level of protection comparable to that afforded by 0.3% (wt/wt) calcium propionate. The effect of sourdough fermentation with W. anomalus LCF1695 was also assessed based on rheology and sensory properties.

  1. Quantification of the Triazole Antifungal Compounds Voriconazole and Posaconazole in Human Serum or Plasma Using Liquid Chromatography Electrospray Tandem Mass Spectrometry (HPLC-ESI-MS/MS).

    Science.gov (United States)

    Molinelli, Alejandro R; Rose, Charles H

    2016-01-01

    Voriconazole and posaconazole are triazole antifungal compounds used in the treatment of fungal infections. Therapeutic drug monitoring of both compounds is recommended in order to guide drug dosing to achieve optimal blood concentrations. In this chapter we describe an HPLC-ESI-MS/MS method for the quantification of both compounds in human plasma or serum following a simple specimen preparation procedure. Specimen preparation consists of protein precipitation using methanol and acetonitrile followed by a cleanup step that involves filtration through a cellulose acetate membrane. The specimen is then injected into an HPLC-ESI-MS/MS equipped with a C18 column and separated over an acetonitrile gradient. Quantification of the drugs in the specimen is achieved by comparing the response of the unknown specimen to that of the calibrators in the standard curve using multiple reaction monitoring.

  2. Design, synthesis, and biological evaluation of 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones and related compounds as antifungal and antibacterial agents.

    Science.gov (United States)

    Tandon, Vishnu K; Yadav, Dharmendra B; Maurya, Hardesh K; Chaturvedi, Ashok K; Shukla, Praveen K

    2006-09-01

    A series of (S)-N-(3-chloro-1,4-naphthoquinon-2-yl)-alpha-amino acid ethyl esters 3 and 1,2,3-trisubstituted-1,4-dihydrobenzo[g]quinoxaline-5,10-diones 6-23 were synthesized and evaluated for antifungal and antibacterial activities. The structure-activity relationship of these compounds was studied and the results show that the compounds 3a and 3b exhibited in vitro antifungal activity against Candida albicans, Cryptococcus neoformans, and Sporothrix schenckii whereas compounds 12 and 22 showed in vitro antibacterial activity against Klebsiella pneumoniae and Escherichia coli.

  3. Development of Radiolabeled compounds using reactor-produced radionuclides

    Energy Technology Data Exchange (ETDEWEB)

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

    2007-06-15

    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 {sup 166}Ho, {sup 131}I, {sup 90}Y and {sup 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 {sup 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 {sup 99m}Tc(CO){sub 3

  4. Synthesis and In Vitro Biological Evaluation of Aminonaphthoquinones and Benzo[b]phenazine-6,11-dione Derivatives as Potential Antibacterial and Antifungal Compounds

    Directory of Open Access Journals (Sweden)

    Amaç Fatih Tuyun

    2015-01-01

    Full Text Available A series of 2-arylamino-3-chloro-1,4-naphthoquinone derivatives (3a–h by the reaction of 2,3-dichloro-1,4-naphthoquinone with aryl amines (2a–h and benzo[b]phenazine-6,11-dione derivatives (4a–c by the treatment of 2-arylamino-3-chloro-1,4-naphthoquinone derivatives (3a–h with sodium azide were synthesized and tested for their in vitro antibacterial and antifungal activities. The results suggest that compounds 3d and 3g had potent antifungal activity against Candida albicans (MIC = 78.12 μg/mL. All synthesized compounds (3a–h, 4a–c possessed activity against E. faecalis with MIC values of between 312.5 and 1250 μg/mL. Benzo[b]phenazine-6,11-dione derivatives (4a–c were mostly active against Gram-positive bacteria. The structures of the new members of the series were established on the basis of their spectral properties (IR, 1H NMR, 13C NMR, and mass spectrometry.

  5. Synthesis of new 4-methyl-2-(4-pyridyl)-1,2,3,4-tetrahydroquinolines as potent antifungal compounds

    Energy Technology Data Exchange (ETDEWEB)

    Mendez, Leonor Y. Vargas [Universidad Santo Tomas, Bucaramanga (Colombia). Grupo de Investigaciones Ambientales; Zacchino, Susana A. [Universidad Nacional del Rosario, (Argentina). Lab. de Farmacognosia; Kouznetsov, Vladimir V. [Universidad Industrial de Santander, Bucaramanga (Colombia). Lab. de Quimica Organica y Biomolecular

    2010-07-01

    Synthesis, spectral characterization and biological results of new series of 2-(4-pyridyl)- 1,2,3,4-tetrahydroquinolines and their closer precursors, -N-aryl-N-[1-(4-pyridyl)but-3-enyl] amines are reported. It was found that both g-pyridyl substituted precursors and final products, tetrahydroquinolines, showed very good antifungal activities against Aspergillus fumigatus, Aspergillus flavus, Aspergillus niger, Microsporum gypseun, Trichophyton rubrum and Trichophyton mentagrophytes. (author)

  6. Isolation and physico-chemical characterization of an antifungal and antibacterial peptide produced by Bacillus licheniformis A12.

    Science.gov (United States)

    Gálvez, A; Maqueda, M; Martínez-Bueno, M; Lebbadi, M; Valdivia, E

    1993-07-01

    An antifungal substance named peptide A12-C has been purified to homogeneity from supernatants of sporulated cultures of Bacillus licheniformis A12. It consists of a 0.77-kDa hydrophilic peptide containing two residues of Glu and one of Arg, Ala, Pro, Tyr and Orn. No fatty acids, phosphorus or carbohydrates have been detected. Peptide A12-C is active on several fungi (Microsporum canis CECT 2797, Mucor mucedo CECT 2653, M. plumbeus (CCM F 443, Sporothrix schenckii CECT 2799 and Trichophyton mentagrophytes CECT 2793) and bacteria (Bacillus megaterium, Corynebacterium glutamicum, Sarcina and Mycobacterium), although the latter are less sensitive.

  7. 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.

  8. Study of nonvolatile degradation compounds produced by radiosterilization of cefotaxime

    Science.gov (United States)

    Barbarin, N.; Tilquin, B.

    2001-01-01

    The effects of radiosterilization on the purity profile of cefotaxime were evaluated by a liquid chromatography-diode array method. Numerous new radiolytic compounds were detected in very small amount. They were quantified and it appeared that none was present above the level of 0.1% of the main compound and the total amount was only of 0.72%. Despite the low quantities present, some radiolytic compounds had UV spectra which could justify the apparition of a yellow coloration detected after irradiation. Others had UV spectra similar to that of cefotaxime, suggesting similarity in the molecular structures. Finally, some mechanisms of formation were proposed for four radiolytic compounds which were identified by mass spectrometry in a former study.

  9. Study of nonvolatile degradation compounds produced by radiosterilization of cefotaxime

    Energy Technology Data Exchange (ETDEWEB)

    Barbarin, N.; Tilquin, B. E-mail: tilquin@cham.ucl.ac.be

    2001-07-01

    The effects of radiosterilization on the purity profile of cefotaxime were evaluated by a liquid chromatography-diode array method. Numerous new radiolytic compounds were detected in very small amount. They were quantified and it appeared that none was present above the level of 0.1% of the main compound and the total amount was only of 0.72%. Despite the low quantities present, some radiolytic compounds had UV spectra which could justify the apparition of a yellow coloration detected after irradiation. Others had UV spectra similar to that of cefotaxime, suggesting similarity in the molecular structures. Finally, some mechanisms of formation were proposed for four radiolytic compounds which were identified by mass spectrometry in a former study. (author)

  10. Biochemical and immunological characterization of a recombinantly-produced antifungal cysteine proteinase inhibitor from green kiwifruit (Actinidia deliciosa).

    Science.gov (United States)

    Popovic, Milica; Andjelkovic, Uros; Burazer, Lidija; Lindner, Buko; Petersen, Arnd; Gavrovic-Jankulovic, Marija

    2013-10-01

    Plant proteinase inhibitors are considered important defense molecules against insect and pathogen attack. The cysteine proteinase inhibitor (CPI) from green kiwifruit (Actinidia deliciosa) belongs to the cystatin family and shows potent antifungal activity (in vitro and in vivo). However, the low abundance of this molecule in fruit (6μg/g of fresh fruit) seems to limit further investigations on the interaction between phytocystatin and photopathogenic fungi. In this paper the cDNA of the kiwi CPI was expressed in Escherichia coli. Fifteen N-terminal amino acids were identified by Edman degradation, and 77% of the rCPI primary structure was confirmed by mass fingerprint. The structural homology of recombinant CPI (rCPI) to its natural counterpart has been clearly demonstrated in immunological assays (immunoblot and ELISA inhibition). Biological activity of rCPI was demonstrated in inhibition assay with cysteine proteinase papain (EC50 2.78nM). In addition, rCPI reveals antifungal properties toward pathogenic fungi (Alternaria radicina and Botrytis cinerea), which designates it as an interesting model protein for the exploration of plant phytocystatins - pathogen interactions. Understanding the molecular mechanisms of natural plant resistance could lead to the development of ecologically safe fungicides for controlling post-harvest diseases and maintaining food quality.

  11. 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.

  12. DEB-2菌株抗真菌活性物质对半夏组培生长的影响%Effects of DEB-2 Antifungal Compound to Tissue Culture of Pinellia ternate

    Institute of Scientific and Technical Information of China (English)

    吴璇; 康冀川; 雷帮星; 何劲; 杨秀超; 吴定基

    2011-01-01

    In order to develop the DEB-2 antifungal compound to become antifungal additive of tissue, the inhibition activity to common contaminated fungi of tissue culture of DEB-2 antifungal compound and the effects of the growth of P. ternate were studied. The results showed that the antifungal compound of DEB-2 had strong inhibition activity to contaminated fungi of tissue culture. At the concentration of 20mL/L, the antifungal compound could obviously restrain the growth of contaminated fungi, but had no effects to the growth of P. ternate. However, the antifungal compound could restrain the regeneration rate of P. ternate' s adventitious buds at 30mL/L of antifungal compound. The height of P. ternate' s adventitious buds was strongly restrained at 40mL/L of antifungal compound, but the growth vigor of P. ternate was not obviously inhibited.%为了开发DEB-2菌株抗真菌活性物质成为组培抗真菌添加剂,采用生长速率法研究了DEB-2菌株抗真菌活性物质对12株组培常见污染菌的抑制作用,并将该抗真菌活性物质添加到组培培养基中,观察其对半夏组培苗生长的影响.结果表明,DEB-2菌株抗真菌物质对组培常见污染菌有较强的抑制作用,在20 mL/L浓度下能明显抑制大多数常见组培污染真菌的生长,但对半夏的生长无显著影响;在30 mL/L浓度下能显著抑制半夏不定芽的再生率;在40 mL/L浓度下对不定芽生长高度的抑制作用极显著,对半夏的生长势有明显的抑制作用.

  13. Effect of preharvest anti-fungal compounds on Aspergillus steynii and A. carbonarius under fluctuating and extreme environmental conditions

    OpenAIRE

    García Cela, Esther; Gil-Serna, J.; Marín Sillué, Sònia; Acevedo, H. (Horacio); B. Patiño; Ramos Girona, Antonio J.

    2012-01-01

    Ochratoxin A (OTA) has been found in pre-harvest and freshly harvested wheat. Spanish climatic conditions point to Aspergillus species as probably responsible for this OTA. In this study the effectiveness of 5 non-specific antifungal chemicals used on wheat fields (25.9% tebuconazole + 60.0% N,N-capramide dimethyl; 12.70% tebuconazole + 12.7% prothioconazole + 59.5% N,N‐amide dimethyldecane; 12.5% epoxiconazole; 12.5% tetraconazole; and 70% thiophanate methyl) and an extract from Equisetum ar...

  14. 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.

  15. Varietal flavour compounds of four grape varieties producing Madeira wines

    OpenAIRE

    Câmara, José de Sousa; Herbert, Paulo; Marques, José Carlos; Alves, Maria Arminda

    2004-01-01

    Boal, Malvasia, Sercial and Verdelho are the main white grape varieties used in Madeira wine production. To estimate the free fraction of varietal aroma compounds of these varieties, 39 samples of musts were analysed to determine their content of monoterpenols and C13 norisoprenoids (terpenoids), using dynamic headspace solid-phase microextraction coupled with gas chromatography–mass spectrometry. The r-values for linearity studies of the analytical method used, varied between 0.977 (nerolido...

  16. Antifungal adjuvants: Preserving and extending the antifungal arsenal.

    Science.gov (United States)

    Butts, Arielle; Palmer, Glen E; Rogers, P David

    2017-02-17

    As the rates of systemic fungal infections continue to rise and antifungal drug resistance becomes more prevalent, there is an urgent need for new therapeutic options. This issue is exacerbated by the limited number of systemic antifungal drug classes. However, the discovery, development, and approval of novel antifungals is an extensive process that often takes decades. For this reason, there is growing interest and research into the possibility of combining existing therapies with various adjuvants that either enhance activity or overcome existing mechanisms of resistance. Reports of antifungal adjuvants range from plant extracts to repurposed compounds, to synthetic peptides. This approach would potentially prolong the utility of currently approved antifungals and mitigate the ongoing development of resistance.

  17. In vitro antifungal activity of 2-(2'-hydroxy-5'-aminophenyl)benzoxazole in Candida spp. strains.

    Science.gov (United States)

    Daboit, Tatiane Caroline; Stopiglia, Cheila Denise Ottonelli; Carissimi, Mariana; Corbellini, Valeriano Antonio; Stefani, Valter; Scroferneker, Maria Lúcia

    2009-11-01

    The development of azole antifungals has allowed for the treatment of several fungal infections. However, the use of these compounds is restricted because of their hepatotoxicity or because they need to be administered together with other drugs in order to prevent resistance to monotherapy. Benzoxazole derivatives are among the most thriving molecular prototypes for the development of antifungal agents. 2-(2'-hydroxyphenyl) benzoxazoles are versatile molecules that emit fluorescence and have antibacterial, antiviral and antifungal properties. 2-(2'-hydroxy-5'-aminophenyl) benzoxazole (HAMBO) was tested against Candida yeast. The inhibition provided by HAMBO was lower than that of fluconazole, showing low antifungal activity against Candida spp., but equivalent to that of benzoxazoles tested in similar studies. HAMBO showed fungistatic activity against all analysed strains. This class of novel benzoxazole compounds may be used as template to produce better antifungal drugs.

  18. Study on Antifungal Substance Produced by Bacillus amylolique f aciens%解淀粉芽孢杆菌抑菌活性初步研究

    Institute of Scientific and Technical Information of China (English)

    杨帆; 李新民; 刘春来; 王爽; 夏吉星; 王克勤; 刘兴龙

    2015-01-01

    In order to isolate and purify the antifungal proteins and lipopeptides products ,and promote the devel‐opment and utilization of antagonistic bacteria ,two strains of Bacillus amylolique f aciens which showed obvi‐ous antifungal activity against plant pathogens were selected .Antifungal proteins of two strains were prelimina‐ry separated ,using the methods of ammonium sulfate precipitation ,and tested on plant pathogens .Antifungal activity of lipopeptides products which extracted with methanol from hydrochloric acid precipitate were tested plant pathogens .Two strains were also tested wether could produce cellulose ,protease and siderophore .The re‐sults showed that the strongest antifungal proteins inhibition activity of strain BQD1 was under the ammonium sulfate condition of 20% ~ 30% ,its diameter of inhibition zone to Setosphaeria turcica was 31 .48 mm .Anti‐fungal proteins inhibition activity of strain TY was under the ammonium sulfate condition of 30% ~ 40% ,its diameter of inhibition zone to Setosphaeria turcica was 34 .20 mm .Lipopeptides products of two strains had stronger antagonism effect on target plant pathogens than its ferfentation .two strains could both produce cellu‐lose ,protease and siderophore .%为了进一步分离纯化抑菌蛋白和脂肽类物质,促进拮抗菌的开发和利用,选取2株对多种植物病原真菌具有良好拮抗作用的解淀粉芽孢杆菌,利用硫酸铵沉淀法粗提2株菌株的抑菌蛋白,酸沉淀法粗提脂态类抑菌物质,分别测定粗提物对多种植物病原真菌的抑制效果。初步检测2株菌株是否具有产纤维素酶、蛋白酶和嗜铁素活性。结果表明:BQD1菌株20%~30%的蛋白粗提液对玉米大斑病菌拮抗作用最强,抑菌直径达31.48 mm 。 TY 菌株30%~40%的蛋白粗提液对玉米大斑病菌抑菌直径最高达34.20 mm 。2株菌株脂态类粗提液对靶标病原菌株的拮抗作用均高于其发酵液,且

  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. Iridate compound produces extraordinarily high coercive magnetic field

    Science.gov (United States)

    Zapf, Vivien; Topping, Craig; Kim, Jae-Wook; Mun, Eun-Deok; Goddard, Paul; Ghannadzadeh, Saman; Luo, Xuan; Cheong, Sang-Wook; Singleton, John

    2014-03-01

    We present a data on an iridate compound that shows an extraordinarily large magnetic hysteresis loop. The coercive magnetic field exceeds 40 Tesla in single-crystal samples. The hysteresis coexists with a linear background, and the total remanent magnetization is about half a Bohr magneton. We will discuss the emergence of these properties from the interplay of spin-orbit coupling, magnetic exchange and possible frustration. The single crystalline material exhibits a magnetic hysteresis loop for one orientation of the magnetic field and a smooth linear increase in the magnetization with field for the other. Measurements were conducted in 65 T short-pulse magnets and the 60 Tesla shaped-pulse magnet at the National High Magnetic Field Lab in Los Alamos. We do not observe any dependence of the magnetic hysteresis on magnetic field sweep rate. Compounds containing Ir4 + have attracted attention recently due to strong spin-orbit coupling that competes with crystal-electric field and exchange interactions. This competition can result in non-Hund's-rule ground states with unusual properties.

  1. 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.

  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.

    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.

  3. 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.

  4. 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 ga

  5. Compound cast product and method for producing a compound cast product

    Science.gov (United States)

    Meyer, Thomas N.; Viswanathan, Srinath

    2002-09-17

    A compound cast product is formed in a casting mold (14) having a mold cavity (16) sized and shaped to form the cast product. A plurality of injectors (24) is supported from a bottom side (26) of the casting mold (14). The injectors (24) are in fluid communication with the mold cavity (16) through the bottom side (26) of the casting mold (14). A molten material holder furnace (12) is located beneath the casting mold (14). The holder furnace (12) defines molten material receiving chambers (36) configured to separately contain supplies of two different molten materials (37, 38). The holder furnace (12) is positioned such that the injectors (24) extend downward into the receiving chamber (36). The receiving chamber (36) is separated into at least two different flow circuits (51, 52). A first molten material (37) is received in a first flow circuit (51), and a second molten material (38) is received into a second flow circuit (52). The first and second molten materials (37, 38) are injected into the mold cavity (16) by the injectors (24) acting against the force of gravity. The injectors (24) are positioned such that the first and second molten materials (37, 38) are injected into different areas of the mold cavity (16). The molten materials (37, 38) are allowed to solidify and the resulting compound cast product is removed from the mold cavity (16).

  6. Antifungal antibiotic CA1189 produced by a Mangrove endophyte Streptomyces sp.A1626%红树林内生链霉菌A1626产生的抗真菌抗生素CA1189

    Institute of Scientific and Technical Information of China (English)

    褚以文; 李进军; 王辂; 余蓉

    2011-01-01

    Objective To purify and to identify an antifungal compound of an endophytic isolate Streptomyces sp. A1626, which was isolated from stems of Kandelia candel(Linn.) Druce, and to determine its antifungal activity. Methods Compound CA 1189 was separated and purified by solvent extraction, silica gel, RP-18 column chromatography. Its structure was elucidated on the basis of extensive spectroscopic analysis including UV, IR, MS,1D and 2D NMR experiments. Its in vitro antifungal activity was determined with micro-broth dilution assay. Results and Conclusion The potent antifungal compound CA 1189 is identical with benzoxazole derivative AJI9561.%目的 研究秋茄内生链霉菌菌株A1626产生的活性代谢产物.方法 发酵液经有机溶剂萃取、正相硅胶柱层析、C18柱制备色谱分离获得单体,通过紫外光谱、红外光谱、质谱、一维和二维核磁共振谱的测定解析,确证单体化合物的结构,采用微量液体稀释法对单体化合物的抗真菌活性进行测定.结果 与结论活性化合物CA1189属于苯并噁唑类,与文献报道的AYI9561结构一致,其抗真菌活性为首次报道.

  7. Two Streptomyces species producing antibiotic, antitumor, and anti-inflammatory compounds are widespread among intertidal macroalgae and deep-sea coral reef invertebrates from the central Cantabrian Sea.

    Science.gov (United States)

    Braña, Alfredo F; Braña, Afredo F; Fiedler, Hans-Peter; Nava, Herminio; González, Verónica; Sarmiento-Vizcaíno, Aida; Molina, Axayacatl; Acuña, José L; García, Luis A; Blanco, Gloria

    2015-04-01

    Streptomycetes are widely distributed in the marine environment, although only a few studies on their associations to algae and coral ecosystems have been reported. Using a culture-dependent approach, we have isolated antibiotic-active Streptomyces species associated to diverse intertidal marine macroalgae (Phyllum Heterokontophyta, Rhodophyta, and Chlorophyta), from the central Cantabrian Sea. Two strains, with diverse antibiotic and cytotoxic activities, were found to inhabit these coastal environments, being widespread and persistent over a 3-year observation time frame. Based on 16S rRNA sequence analysis, the strains were identified as Streptomyces cyaneofuscatus M-27 and Streptomyces carnosus M-40. Similar isolates to these two strains were also associated to corals and other invertebrates from deep-sea coral reef ecosystem (Phyllum Cnidaria, Echinodermata, Arthropoda, Sipuncula, and Anelida) living up to 4.700-m depth in the submarine Avilés Canyon, thus revealing their barotolerant feature. These two strains were also found to colonize terrestrial lichens and have been repeatedly isolated from precipitations from tropospheric clouds. Compounds with antibiotic and cytotoxic activities produced by these strains were identified by high-performance liquid chromatography (HPLC) and database comparison. Antitumor compounds with antibacterial activities and members of the anthracycline family (daunomycin, cosmomycin B, galtamycin B), antifungals (maltophilins), anti-inflamatory molecules also with antituberculosis properties (lobophorins) were identified in this work. Many other compounds produced by the studied strains still remain unidentified, suggesting that Streptomyces associated to algae and coral ecosystems might represent an underexplored promising source for pharmaceutical drug discovery.

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

    Science.gov (United States)

    Aunsbjerg, S D; Honoré, A H; Marcussen, J; Ebrahimi, P; Vogensen, F K; Benfeldt, C; Skov, T; Knøchel, S

    2015-02-02

    Lactic acid bacteria with antifungal properties can be used to control spoilage of food and feed. Previously, most of the identified metabolites have been isolated from cell-free fermentate of lactic acid bacteria with methods suboptimal for detecting possible contribution from volatiles 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 the contribution of diacetyl in the antifungal effect of L. paracasei DGCC 2132 and indicate that the importance of volatiles may have been previously underestimated.

  9. Antifungal and antiviral products of marine organisms.

    Science.gov (United States)

    Cheung, Randy Chi Fai; Wong, Jack Ho; Pan, Wen Liang; Chan, Yau Sang; Yin, Cui Ming; Dan, Xiu Li; Wang, He Xiang; Fang, Evandro Fei; Lam, Sze Kwan; Ngai, Patrick Hung Kui; Xia, Li Xin; Liu, Fang; Ye, Xiu Yun; Zhang, Guo Qing; Liu, Qing Hong; Sha, Ou; Lin, Peng; Ki, Chan; Bekhit, Adnan A; Bekhit, Alaa El-Din; Wan, David Chi Cheong; Ye, Xiu Juan; Xia, Jiang; Ng, Tzi Bun

    2014-04-01

    Marine organisms including bacteria, fungi, algae, sponges, echinoderms, mollusks, and cephalochordates produce a variety of products with antifungal activity including bacterial chitinases, lipopeptides, and lactones; fungal (-)-sclerotiorin and peptaibols, purpurides B and C, berkedrimane B and purpuride; algal gambieric acids A and B, phlorotannins; 3,5-dibromo-2-(3,5-dibromo-2-methoxyphenoxy)phenol, spongistatin 1, eurysterols A and B, nortetillapyrone, bromotyrosine alkaloids, bis-indole alkaloid, ageloxime B and (-)-ageloxime D, haliscosamine, hamigeran G, hippolachnin A from sponges; echinoderm triterpene glycosides and alkene sulfates; molluscan kahalalide F and a 1485-Da peptide with a sequence SRSELIVHQR; and cepalochordate chitotriosidase and a 5026.9-Da antifungal peptide. The antiviral compounds from marine organisms include bacterial polysaccharide and furan-2-yl acetate; fungal macrolide, purpurester A, purpurquinone B, isoindolone derivatives, alterporriol Q, tetrahydroaltersolanol C and asperterrestide A, algal diterpenes, xylogalactofucan, alginic acid, glycolipid sulfoquinovosyldiacylglycerol, sulfated polysaccharide p-KG03, meroditerpenoids, methyl ester derivative of vatomaric acid, lectins, polysaccharides, tannins, cnidarian zoanthoxanthin alkaloids, norditerpenoid and capilloquinol; crustacean antilipopolysaccharide factors, molluscan hemocyanin; echinoderm triterpenoid glycosides; tunicate didemnin B, tamandarins A and B and; tilapia hepcidin 1-5 (TH 1-5), seabream SauMx1, SauMx2, and SauMx3, and orange-spotted grouper β-defensin. Although the mechanisms of antifungal and antiviral activities of only some of the aforementioned compounds have been elucidated, the possibility to use those known to have distinctly different mechanisms, good bioavailability, and minimal toxicity in combination therapy remains to be investigated. It is also worthwhile to test the marine antimicrobials for possible synergism with existing drugs. The prospects of

  10. 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...

  11. 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....

  12. Antifungal activity of the lipopeptides produced by Bacillus amyloliquefaciens anti-CA against Candida albicans isolated from clinic.

    Science.gov (United States)

    Song, Bo; Rong, Yan-Jun; Zhao, Ming-Xin; Chi, Zhen-Ming

    2013-08-01

    The bacterium Bacillus amyloliquefaciens anti-CA isolated from mangrove system was found to be able to actively kill Candida albicans isolated from clinic. The bacterial strain anti-CA could produce high level of bioactive substance, amylase and protease in the cheap medium containing 2.0 % soybean meal, 2.0 % wheat flour, pH 6.5 within 26 h. After purification, the main bioactive substance was confirmed to be a cyclic lipopeptide containing a heptapeptide, L-Asp→L-Leu→L-Leu→L-Val→L-Val→L-Glu→L-Leu and a 3-OH fatty acid (15 carbons). In addition to C. albicans, the purified lipopeptide can also kill many yeast strains including Metschnikowia bicuspidata, Candida tropicalis, Yarrowia lipolytica and Saccharomyces cerevisiae. After treated by the purified lipopeptide, both the whole cells and protoplasts of C. albicans were destroyed.

  13. Design,Synthesis and Antifungal Activity of Novel Triazole Derivatives

    Institute of Scientific and Technical Information of China (English)

    Chun Quan SHENG; Wan Nian ZHANG; Hai Tao JI; Yun Long SONG; Min ZHANG; You Jun ZHOU; Jia Guo LU; Jü ZHU

    2004-01-01

    Twenty-one 1-(1H-1,2,4-triazolyl)-2-(2,4-diflurophenyl)-3-(4-substituted-1- piperazinyl)-2-propanol derivatives were designed and synthesized,on the basis of the active site of lanosterol 14(-demethylase.In vitro antifungal activities showed that some of the target compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

  14. Identification of the antifungal compound, trans-cinnamic acid, produced by Photorhabdus luminescens, a potential biopesticide against pecan scab

    Science.gov (United States)

    Pecan scab (caused by Fusicladium effusum) is the major disease that limits the productivity and quality of pecan in the southeastern US. Alternatives to conventional fungicides are desirable and should be biorational, of low environmental risk with a reduced risk for fungicide resistance developing...

  15. Volatile compounds in samples of cork and also produced by selected fungi.

    Science.gov (United States)

    Barreto, M C; Vilas Boas, L; Carneiro, L C; San Romão, M V

    2011-06-22

    The production of volatile compounds by microbial communities of cork samples taken during the cork manufacturing process was investigated. The majority of volatiles were found in samples collected at two stages: resting after the first boiling and nontreated cork disks. Volatile profiles produced by microbiota in both stages are similar. The releasable volatile compounds and 2,4,6-trichloroanisole (TCA) produced in cork-based culture medium by five isolated fungal species in pure and mixed cultures were also analyzed by gas chromatography coupled with mass spectrometry (GC-MS).The results showed that 1-octen-3-ol and esters of fatty acids (medium chain length C8-C20) were the main volatile compounds produced by either pure fungal species or their mixture. Apparently, Penicillium glabrum is the main contributor to the overall volatile composition observed in the mixed culture. The production of releasable TCA on cork cannot be attributed to any of the assayed fungal isolates.

  16. Antifungal activity improved by coproduction of cyclodextrins and anabaenolysins in Cyanobacteria.

    Science.gov (United States)

    Shishido, Tania K; Jokela, Jouni; Kolehmainen, Clara-Theresia; Fewer, David P; Wahlsten, Matti; Wang, Hao; Rouhiainen, Leo; Rizzi, Ermanno; De Bellis, Gianluca; Permi, Perttu; Sivonen, Kaarina

    2015-11-03

    Cyclodextrins are cyclic oligosaccharides widely used in the pharmaceutical industry to improve drug delivery and to increase the solubility of hydrophobic compounds. Anabaenolysins are lipopeptides produced by cyanobacteria with potent lytic activity in cholesterol-containing membranes. Here, we identified the 23- to 24-kb gene clusters responsible for the production of the lipopeptide anabaenolysin. The hybrid nonribosomal peptide synthetase and polyketide synthase biosynthetic gene cluster is encoded in the genomes of three anabaenolysin-producing strains of Anabaena. We detected previously unidentified strains producing known anabaenolysins A and B and discovered the production of new variants of anabaenolysins C and D. Bioassays demonstrated that anabaenolysins have weak antifungal activity against Candida albicans. Surprisingly, addition of the hydrophilic fraction of the whole-cell extracts increased the antifungal activity of the hydrophobic anabaenolysins. The fraction contained compounds identified by NMR as α-, β-, and γ-cyclodextrins, which undergo acetylation. Cyclodextrins have been used for decades to improve the solubility and bioavailability of many drugs including antifungal compounds. This study shows a natural example of cyclodextrins improving the solubility and efficacy of an antifungal compound in an ancient lineage of photosynthetic bacteria.

  17. Antifungal constituents of Melicope borbonica

    DEFF Research Database (Denmark)

    Simonsen, Henrik Toft; Adsersen, Anne; Bremner, Paul

    2004-01-01

    , as the major constituents. All three compounds exhibited moderate antifungal activity against Candida albicans and Penicillium expansum, in accordance with the traditional use of the plant. Moreover, 2,4,6-trimethoxyacetophenone (methylxanthoxylin), three other coumarins [7-(3-methyl-2-butenyloxy)-6...

  18. Antifungal Production of a Strain of Actinomycetes spp Isolated from the Rhizosphere of Cajuput Plant: Selection and Detection of Exhibiting Activity Against Tested Fungi

    Directory of Open Access Journals (Sweden)

    Alimuddin A

    2015-11-01

    Full Text Available Actinomycetes are bacteria known to constitute a large part of the rhizosphere microbiota. Their isolation is an important step for screening of new bioactive compounds. Culturable actinomycetes populations from cajuput plant rhizosphere soils in Wanagama I Forest UGM Yogyakarta were collected to study about their antifungal activity. Among 17 of a total 43 isolates that showed activity were screened for producing antifungi substances. Screening for antifungal activity of isolates were performed with dual culture bioassay in vitro. One isolate that was designated as Streptomyces sp.GMR-22 was the strongest against all tested fungi and appeared promising for a sources of antifungal. Culture’s supernatant and mycelia were extracted with chloroform, ethyl acetate and methanol, respectively. Antifungal activity of crude extracts was tested by diffusion method against tested fungi. The result indicates that isolates of actinomycetes from cajuput plant rhizosphere could be an interesting sources of antifungal bioactive substances.

  19. Antifungal Activity of Essential Oils from Some Medicinal Plants of Iran against Alternaria alternate

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    I. Hadizadeh

    2009-01-01

    Full Text Available Problem statement: Increasing public concern over the level of pesticide residues in food especially fresh produce has built up adequate pressure for scientists to look for less hazardous and environmentally safer compounds for controlling post harvest diseases. Essential oils as registered food grade materials have the potential to be applied as alternative anti-fungal treatments for fresh fruits and vegetables. Approach: We present in this study, the identification of the essential oils with antifungal activity from some medicinal plants of Iran (nettle (Urtica dioica L., thyme (Thymus vulgaris L., eucalyptus (Eucalyptus spp., Rue (Ruta graveolens L. and common yarrow (Achillea millefolium L., and their potential application as "generally regarded as safe" antifungal compounds against Alternaria alternate on tomato as a model pathosystem. Results: Both the nettle and the thyme oils exhibited antifungal activity against A. alternata. The thyme oil exhibited a lower degree of inhibition 68.5 and 74.8% at 1500 and 2000 ppm, respectively. Spore germination and germ tube elongation of the pathogens in potato dextrose broth was strongly reduced in the presence of 1500 ppm of the nettle oil. The same concentration of this oil reduced the percentage of decayed tomatoes. The experiments on reducing the development of natural tomato rot gave similar results. Conclusions: Application of essential oils for postharvest disease control of fresh produce, as a novel emerging alternative to hazardous anti-fungal treatments will allow a safer and environmentally more acceptable management of postharvest diseases.

  20. 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

  1. 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.

  2. Synthesis and antifungal activity of the novel triazole compounds%新型三唑醇类化合物的合成及抗真菌活性研究

    Institute of Scientific and Technical Information of China (English)

    王曙东; 陈兴东; 赵庆杰; 邹燕; 胡宏岗; 俞世冲; 汪亭; 柴晓云; 任海祥

    2011-01-01

    目的 以氟康唑为先导化合物,设计合成新的三唑醇类化合物,并研究其抗真菌活性.方法 引入较大基团的N,N-二取代侧链结构,合成一系列目标化合物,所有化合物结构均经MS、1H NMR等谱确证;选择8种真菌为实验菌株,测定其体外抗真菌活性.结果 合成了18个未见文献报道的目标化合物,化合物对所选真菌均表现出了一定的抑菌活性.结论 引入较大基团的N,N-二取代侧链结构对抗真菌活性影响较大.%Objective To design the synthesis and evaluate the antifungal active of the novel triazole compounds hased on the structure of fluconazole. Methods The big N,N-disubstituted group was introduced and a series of compounds were synthesized, all of them were confirmed by MS and 'H NMR, et al. The antifungal activity were also evaluated against the eight common pathogenic fungi. Results Eighteen compounds were synthesized,which exhibited activity against fungi tested. Conclusion The big N,N-disubstituted group introduced to the side chain could affected the antifungal activity.

  3. AN OVERVIEW OF AZOLE ANTIFUNGALS

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    Pratibha Shivaji Gavarkar*, Rahul Shivaji Adnaik, and Shrinivas Krishna Mohite

    2013-11-01

    Full Text Available Fungal infections in critically ill or immunosuppressed patients were increasing in incidence in the human population over the last 1-2 decades. There were few advances in antifungal therapy and, until recently, there were few choices from which to select a treatment for systemic mycoses. However, in the past decade, there have been several developments in this area. Antifungal agents are sufficiently diverse in activity, toxicity, and drug interaction potential. Azoles are synthetic and semi-synthetic compounds. They have a broad spectrum of activity. Triazole antifungals are active to treat an array of fungal pathogens, whereas imidazoles are used almost exclusively in the treatment of superficial mycoses and vaginal candidiasis. Despite the advances, serious fungal infections remain difficult to treat, and resistance to the available drugs is emerging. Use of the currently available azoles in combination with other antifungal agents with different mechanisms of action is likely to provide enhanced efficacy. The present review aims to explore the pharmacology, pharmacokinetics, spectrum of activity, safety, toxicity and potential for drug–drug interactions of the azole antifungal agents.

  4. Isolation of an antimicrobial compound produced by bacteria associated with reef-building corals

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    Jean-Baptiste Raina

    2016-08-01

    Full Text Available Bacterial communities associated with healthy corals produce antimicrobial compounds that inhibit the colonization and growth of invasive microbes and potential pathogens. To date, however, bacteria-derived antimicrobial molecules have not been identified in reef-building corals. Here, we report the isolation of an antimicrobial compound produced by Pseudovibrio sp. P12, a common and abundant coral-associated bacterium. This strain was capable of metabolizing dimethylsulfoniopropionate (DMSP, a sulfur molecule produced in high concentrations by reef-building corals and playing a role in structuring their bacterial communities. Bioassay-guided fractionation coupled with nuclear magnetic resonance (NMR and mass spectrometry (MS, identified the antimicrobial as tropodithietic acid (TDA, a sulfur-containing compound likely derived from DMSP catabolism. TDA was produced in large quantities by Pseudovibrio sp., and prevented the growth of two previously identified coral pathogens, Vibrio coralliilyticus and V. owensii, at very low concentrations (0.5 μg/mL in agar diffusion assays. Genome sequencing of Pseudovibrio sp. P12 identified gene homologs likely involved in the metabolism of DMSP and production of TDA. These results provide additional evidence for the integral role of DMSP in structuring coral-associated bacterial communities and underline the potential of these DMSP-metabolizing microbes to contribute to coral disease prevention.

  5. 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

  6. Antifungal activities of three different Lactobacillus species and their production of antifungal carboxylic acids in wheat sourdough.

    Science.gov (United States)

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

    2016-02-01

    This study was undertaken to assess the antifungal performance of three different Lactobacillus species.Experiments were conducted in vitro and in situ to extend the shelf life of wheat bread. Standard sourdough analyses were performed characterising acidity and carbohydrate levels. Overall, the strains showed good inhibition in vitro against the indicator mould Fusarium culmorum TMW4.2043. Sourdough bread fermented with Lactobacillus amylovorus DSM19280 performed best in the in situ shelf life experiment. An average shelf life extension of six more mould-free days was reached when compared to the non-acidified control bread. A range of antifungal-active acids like 3-phenyllactic acid, 4-hydroxyphenyllactic acid and 2-hydroxyisocaproic acid in quantities between 0.1 and 360 mg/kg were present in the freeze-dried sourdoughs. Their concentration differed greatly amongst the species.However, a higher concentration of these compounds could not completely justify the growth inhibition of environmental moulds. In particular, although Lb. reuteri R29 produced the highest total concentration of these active compounds in the sourdough, its addition to bread did not result in a longest shelf life. Nevertheless, when the artificial compounds were spiked into a chemically acidified dough, it succeeded in a longer shelf life (+25 %) than achieved only by acidifying the dough. This provides evidence of their contribution to the antifungal activity and their synergy in concentration levels far below their single minimal inhibition concentrations under acidic conditions.

  7. Organic compounds in produced waters from coalbed natural gas wells in the Powder River Basin, Wyoming, USA

    Science.gov (United States)

    Orem, W.H.; Tatu, C.A.; Lerch, H.E.; Rice, C.A.; Bartos, T.T.; Bates, A.L.; Tewalt, S.; Corum, M.D.

    2007-01-01

    The organic composition of produced water samples from coalbed natural gas (CBNG) wells in the Powder River Basin, WY, sampled in 2001 and 2002 are reported as part of a larger study of the potential health and environmental effects of organic compounds derived from coal. The quality of CBNG produced waters is a potential environmental concern and disposal problem for CBNG producers, and no previous studies of organic compounds in CBNG produced water have been published. Organic compounds identified in the produced water samples included: phenols, biphenyls, N-, O-, and S-containing heterocyclic compounds, polycyclic aromatic hydrocarbons (PAHs), aromatic amines, various non-aromatic compounds, and phthalates. Many of the identified organic compounds (phenols, heterocyclic compounds, PAHs) are probably coal-derived. PAHs represented the group of organic compounds most commonly observed. Concentrations of total PAHs ranged up to 23 ??g/L. Concentrations of individual compounds ranged from about 18 to compound concentrations was documented, as two wells with relatively high organic compound contents in produced water in 2001 had much lower concentrations in 2002. In many areas, including the PRB, coal strata provide aquifers for drinking water wells. Organic compounds observed in produced water are also likely present in drinking water supplied from wells in the coal. Some of the organic compounds identified in the produced water samples are potentially toxic, but at the levels measured in these samples are unlikely to have acute health effects. The human health effects of low-level, chronic exposure to coal-derived organic compounds in drinking water are currently unknown. Continuing studies will evaluate possible toxic effects from low level, chronic exposure to coal-derived organic compounds in drinking water supplies.

  8. 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...... contamination of coffee with the sensory characteristics of the beverage. The aim of this research was to investigate the production of VCs by fungi isolated from coffee and their potential as modifiers of the sensory coffee beverage quality. Three species were isolated from coffee from the southwest of São...... Paulo state and selected for the study: Penicillium brevicompactum, Aspergillus luchuensis (belonging to section Nigri) and Penicillium sp. nov. (related to Penicillium crustosum). VCs produced by the fungal inoculated in raw coffee beans were extracted and tentatively identified by SPME...

  9. Antifungal activity of five species of Polygala

    Directory of Open Access Journals (Sweden)

    Susana Johann

    2011-09-01

    Full Text Available Crude extracts and fractions of five species of Polygala - P. campestris, P. cyparissias, P. paniculata, P. pulchella and P. sabulosa - were investigated for their in vitro antifungal activity against opportunistic Candida species, Cryptococcus gattii and Sporothrix schenckii with bioautographic and microdilution assays. In the bioautographic assays, the major extracts were active against the fungi tested. In the minimal concentration inhibitory (MIC assay, the hexane extract of P. paniculata and EtOAc fraction of P. sabulosa showed the best antifungal activity, with MIC values of 60 and 30 µg/mL, respectively, against C. tropicalis, C. gattii and S. schenckii. The compounds isolated from P. sabulosa prenyloxycoumarin and 1,2,3,4,5,6-hexanehexol displayed antifungal activity against S. schenckii (with MICs of 125 µg/mL and 250 µg/mL, respectively and C. gattii (both with MICs of 250 µg/mL. Rutin and aurapten isolated from P. paniculata showed antifungal activity against C. gattii with MIC values of 60 and 250 µg/mL, respectively. In the antifungal screening, few of the isolated compounds showed good antifungal inhibition. The compound α-spinasterol showed broad activity against the species tested, while rutin had the best activity with the lowest MIC values for the microorganisms tested. These two compounds may be chemically modified by the introduction of a substitute group that would alter several physico-chemical properties of the molecule, such as hydrophobicity, electronic density and steric strain.

  10. The flocculation efficiency of compound bioflocculant by flocculant-producing bacteria

    Institute of Scientific and Technical Information of China (English)

    MA Fang; WANG Qin; MENG Lu; XU Yang; YANG Ji-xian

    2006-01-01

    The flocculation efficiency of compound bioflocculant produced by flocculant-producing bacteria was investigated in this study. Cheap cellulose was selected as the substrate for the production of a lower cost bioflocculant. The end product of cellulose decomposing bacteria was utilized as substrate for flocculant-producing bacteria. The optimum fermentation conditions were determined as follows: the initial fermentation and fermentation time was 5 d and 1 d respectively, the temperature was 30 °C, the rotation speed was 120 r/min, the amount of CaCl2 solution (10%) was 1.5 ml/L. The flocculation test indicated that the bioflocculant had high efficiency in the removal of the turbidity raw water from Songhaa River.

  11. Antifungal Poly(lactic acid Films Containing Thymol and Carvone

    Directory of Open Access Journals (Sweden)

    Boonruang Kanchana

    2016-01-01

    Full Text Available The goal of this study was to develop antifungal poly(lactic acid films for food packaging applications. The antifungal compounds, thymol and R-(--carvone were incorporated into poly(lactic acid (PLA-based polymer at 10, 15 and 20% by weight. Film converting process consists of three steps including melt blending, sheet extrusion and biaxial stretching. The incorporation of antifungal compounds into the polymer matrix resulted in decreased Tg and Tm, increased gas permeabilility, reduced tensile strength and increased elongation at break of the antifungal PLA films.

  12. 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.

  13. Volatile compounds and sensory characteristics of various instant teas produced from black tea.

    Science.gov (United States)

    Kraujalytė, Vilma; Pelvan, Ebru; Alasalvar, Cesarettin

    2016-03-01

    Various instant teas produced differently from black tea [freeze-dried instant tea (FDIT), spray-dried instant tea (SDIT), and decaffeinated instant tea (DCIT)], were compared for their differences in volatile compounds as well as descriptive sensory analysis (DSA). A total of 63 volatile compounds in all tea samples (eight aldehydes, ten alcohols, nine ketones, five esters, eight acids, ten terpenes/terpenoids, ten furans/furanones, two pyrroles, and one miscellaneous compound) were tentatively identified. Black tea, FDIT, SDIT, and DCIT contained 60, 55, 47, and 40 volatile compounds, respectively. Ten flavour attributes such as after taste, astringency, bitter, caramel-like, floral/sweet, green/grassy, hay-like, malty, roasty, and seaweed were identified. Intensities for a number of flavour attributes (except for caramel-like in SDIT and bitter and after taste in DCIT) were not significantly different (p>0.05) among tea samples. The present study suggests that instant teas can also be used as good alternative to black tea.

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

    Directory of Open Access Journals (Sweden)

    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.

  15. Evaluation of Benzophenone-N-ethyl Morpholine Ethers as Antibacterial and Antifungal Activities

    Directory of Open Access Journals (Sweden)

    A. Bushra Begum

    2014-01-01

    Full Text Available Microorganisms are closely associated with the health and welfare of human beings. Whereas some microorganisms are beneficial, others are detrimental. Bacterial infections often produce inflammation and pains and in some instances, infections result in high mortality. Any subtle change in the drug molecule, which may not be detected by chemical methods, can be revealed by a change in the antimicrobial activity and hence microbiological assays are very useful. A series of substituted hydroxy benzophenones and benzophenone-N-ethyl morpholine ethers were screened for their antibacterial and antifungal activities. Antibacterial activity against S. aureus, E. aerogenes, M. luteus, K. pneumonia, and S. typhimurium, S. paratyphi-B and P. vulgaris bacterial strains and antifungal activity against C. albicans, B. cinerea, M. pachydermatis, C. krusei fungal strains were carried out. The bioassays indicated that most of the synthesized compounds showed potential antibacterial and antifungal agents.

  16. Redox Characteristics of Thiol Compounds Using Radicals Produced by Water Vapor Radio Frequency Discharge

    Science.gov (United States)

    Hayashi, Nobuya; Nakahigashi, Akari; Goto, Masaaki; Kitazaki, Satoshi; Koga, Kazunori; Shiratani, Masaharu

    2011-08-01

    The redox reaction between cystein and cystine is observed using radicals produced in water vapor plasma for the control of plant growth. Cystein is oxidized to cystine using the OH radical in the higher-pressure regime and cystine is reduced to cystein by the H radical generated in the lower-pressure regime. Also, the oxidative stress reaction of plants is observed when water vapor plasma is irradiated onto seeds of plants such as radish sprouts. The mechanism of the control of plant growth is explained by the change in thiol compound quantity of the plant cells induced by the radical reaction.

  17. Design, synthesis and antifungal activity of novel triazole derivatives

    Institute of Scientific and Technical Information of China (English)

    Qing lie Zhao; Yan Song; Hong Gang Hu; Shi Chong Yu; Qiu Ye Wu

    2007-01-01

    Twenty-three 1 -(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-cycloproyl-N-substituted-amino)-2-propanols were designed and synthesized on the basis of the active site of lanosterol 14α-demethylase.In vitro antifungal activities showed that some of the title compounds had higher antifungal activity and broader antifungal spectrum than fluconazole.

  18. 农用抗真菌海洋微生物的筛选及放线菌T19-07活性代谢产物的初步研究%Screening of marine microorganisms with agricultural antifungal activities and preliminary study on the bioactive metabolites produced by strain T19-07

    Institute of Scientific and Technical Information of China (English)

    胡杨; 张道敬; 李元广; 陶黎明; 田黎; 李淑兰

    2011-01-01

    Objective To screen the active strains with agricultural antifungal activity from marine microorganisms as well as the bioactive metabolites produced by marine actinomyces Streptomyces nodosus T19-07. Methods Using phytopathogenic fungi as targets, the active strains were screened out by pairing culture assay. Based on the index of antifungal activity, the characteristics of fermentation of strain T19-07 in 5 L fermentor were studied, and the bioactive substances were extracted by macro-porous resin XAD-16, and TLC bioautography combined with HPLC was used to separate the active compound Results Twelve antagonistic strains against phytopathogenic fungi were screened out from 31 marine microorganisms. The main antifungal substance of strain T19-07 was isolated with relative molecular mass of 214 Da, and its antifungal activity in vitro against Alternaria solani was similar with iprodione registrated as a chemical pesticide, MIC below 12. 5 μg · Ml-1. Conclusion Marine microorganisms are important resources to find agricultural antibiotics. The bioactive substances produced by marine actinomyces S. nodosus T19-07 exhibit potent antifungal activity in vitro, and it has the potential for further study.%通过筛选获得具有拮抗植物病原真菌活性的海洋微生物菌株,并对其中一株海洋生境的结节链霉菌(Streptomyces nodosus)T19-07的活性代谢产物进行初步研究.方法 以植物病原真菌为靶标,采用平板对峙培养法筛选出活性菌株;再以抑菌活性为指标,考察较强活性菌株T19-07在5L发酵罐中的培养过程特征,并通过大孔吸附树脂XAD-16柱层析对活性物质进行分离提取,结合TLC生物自显影和HPLC快速确定代谢产物中的活性组分.结果 从31株海洋微生物中筛选出12株对多种植物病原真菌具有拮抗作用的菌株;确定了菌株T19-07的代谢产物中的主要抑菌活性物质,其相对分子质量为214,并且它对茄交链格孢霉的

  19. Effect of diazotrophic bacteria as phosphate solubilizing and indolic compound producers on maize plants

    Directory of Open Access Journals (Sweden)

    Mónica Del Pilar López Ortega

    2013-12-01

    Full Text Available Phosphorus is limiting for growth of maize plants, and because of that use of fertilizers like Rock Phosphate has been proposed. However, direct use of Rock Phosphate is not recommended because of its low availability, so it is necessary to improve it. In this study, a group of diazotrophic bacteria were evaluated as phosphate-solubilizing bacteria, for their production of indolic compounds and for their effects on growth of maize plants. Strains of the genera Azosporillum, Azotobacter, Rhizobium and Klebsiella, were quantitatively evaluated for solubilization of Ca3(PO42 and rock phosphate as a single source of phosphorous in SRS culture media. Additionally, the phosphatase enzyme activity was quantified at pH 5.0, 7.0 and 8.0 using p-nitrophenyl phosphate, and production of indolic compound was determined by colorimetric quantification. The effect of inoculation of bacteria on maize was determined in a completely randomized greenhouse experiment where root and shoot dry weights and phosphorus content were assessed. Results showed that strain C50 produced 107.2 mg .L-1 of available-P after 12 days of fermentation, and AC10 strain had the highest phosphatase activity at pH 8 with 12.7 mg of p-nitrophenol mL .h-1. All strains synthetized indolic compounds, and strain AV5 strain produced the most at 63.03 µg .mL-1. These diazotrophic bacteria increased plant biomass up to 39 % and accumulation of phosphorus by 10%. Hence, use of diazotrphic phosphate-solubilizing bacteria may represent an alternative technology for fertilization systems in maize plants.

  20. 3种芳香植物单方及其复方精油的抗真菌作用%Antifungal Function of Three Pure Essential Oils and Their Compounds from Aromatic Plants

    Institute of Scientific and Technical Information of China (English)

    姚元; 陈全家; 姚雷

    2012-01-01

    In this study, essential oils from lemongrass, thyme and cinnamon were obtained by means of steam distillation. The antimicrobial effects of these essential oils on different athlete foot fungus (Trichophyton rubrum, Trichophyton gypsum and Epidermophyton floccosum ) were investigated and compared in vitro experiments by using different essential oil formulas (pure and mixture) respectively. The results showed that favorite anti-fungal effects were indicated in all pure essential oils and their compounds. The order of the anti-fungal function was listed as follows :cinnamon>thyme>lemongrass. In addition,3μl of blended essential oils (lemongrass, thyme, and cinnamon) with the proportion of 1∶1∶ 1 demonstrated the best anti-fungal effects against 3 dominant fungus strains. The combination of two or three of the pure essential oil showed significantly synergistic anti-fungal effects. The descending order of the fungal susceptibility to the essential oil was as follows: Epidermophyton floccosum > Trichophyton gypsum>Trichophyton rubrum.%探讨柠檬草、百里香和肉桂精油及其它们所组成的复方精油对足癣真菌的抑制作用.通过抑茵圈法,比较单方精油及其组合复方精油对引起足癣的真菌:红色毛癣菌、石膏样毛癣茵和絮状表皮癣茵的抑茵作用.结果表明,单方精油和复方精油对受试真菌均有较好的抑菌效果.单方精油的抑菌效果强弱顺序为:肉桂、百里香、柠檬草,复方精油中柠檬草十百里香十肉桂(1∶1∶1)在3μL时对3种真菌效果最佳.通过两两组合或三者组合的精油复方表现出明显的协同增效的作用.对真菌的抑茵作用大小为:絮状表皮癣菌>石膏样毛癣菌>红色毛癣菌.

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

    Directory of Open Access Journals (Sweden)

    van Loon Joop JA

    2011-02-01

    Full Text Available Abstract Background 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. Methods 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. Results 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%. Conclusions 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.

  2. 解淀粉芽孢杆菌BI2产抑菌物质的新型种衣剂的研制%A Novel Seed Coating Formula with Antifungal Substances Produced by Bacillus amyloliquefaciens BI2

    Institute of Scientific and Technical Information of China (English)

    王亚军; 李昆; 王德培

    2015-01-01

    The antifungal substances produced from Bacillus amyloliquefaciens BI2,were for the first time used asactive ingredients in seed coating. The fermented broth containing antifungal substances was ultrafiltered and freeze-dried to form lyophilized powder,and then mixed with composite film-forming agent solution. Finally,peanut seeds were coated with this kind of seed coating containing antifungal substances. The results showed that the best volume ratio of 4%, polyvinyl alco-hol(PVA)to 1.5%, sodium carboxymethyl cellulose(CMC-Na)was 5:1,which is the best film former recipe in seed coating,and it has no significant effect on seed germination potential and germination rate. The pH stability andthermal stability of the lyophilized powder of the fermentated broth containing antifungal substances are good. The MIC of the pow-der to inhibitAspergillus flavus spore germination is 1.92,mg/mL. When the content of that powder in the film former reaches 4,mg/mL,A. flavuswas completely inhibited.%将解淀粉芽孢杆菌BI2发酵所产抑菌物质作为新型种衣剂的有效成分与研制的复合型成膜剂溶液混合,制成可抑制黄曲霉孢子萌发的花生种子包衣.结果表明,选用 4%,聚乙烯醇(PVA)与 1.5%,羧甲基纤维素钠(CMC-Na)以体积比 5:1 混合作为种子包衣最佳成膜剂配方,经过包衣后对花生种子的发芽势和发芽率没有显著影响.含有抑菌物质的发酵液冻干粉的 pH 稳定性和热稳定性均较好.发酵液冻干粉抑制黄曲霉孢子萌发的最小质量浓度为1.92,mg/mL.在与花生种子混合时,发酵液冻干粉在成膜剂中的含量达到4,mg/mL时,黄曲霉完全被抑制.

  3. 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

  4. Production and characterization of Iturinic lipopeptides as antifungal agents and biosurfactants produced by a marine pinctada martensii-derived Bacillus mojavensis B0621A.

    Science.gov (United States)

    Ma, Zongwang; Hu, Jiangchun

    2014-06-01

    Bacillus mojavensis B0621A was isolated from a pearl oyster Pinctada martensii collected from South China Sea. While screening for cyclic lipopeptides potentially useful as lead compounds for biological control against soil-bone fungal plant pathogens, three lipopeptides were isolated and purified from the fermentation broth of B. mojavensis B0621A via vacuum flash chromatography coupled with reversed-phase high performance liquid chromatography (RP-HPLC). The structural characterization and identification of these cyclic lipopeptides were performed by tandem mass spectrometry (MS/MS) combined with gas chromatography-mass spectrometry (GC-MS) analysis as well as chemical degradation. These lipopeptides were finally characterized as homologues of mojavensins, which contained identical amino acids back bones of asparagine1, tyrosine2, asparagine3, glutamine4, proline5, asparagine6, and asparagine7 and differed from each other by their saturated β-amino fatty acid chain residues, namely, iso-C14 mojavensin, iso-C16 mojavensin, and anteiso-C17 mojavensin, respectively. All lipopeptide isomers, especially iso-C16 mojavensin and anteiso-C17 mojavensin, displayed moderate antagonism and dose-dependent activity against several formae speciales of Fusarium oxysporum and presented surface tension activities. These properties demonstrated that the lipopeptides produced by B. mojavensis B0621A may be useful as biological control agent to fungal plant pathogens.

  5. 产抗真菌蛋白(AFP)巨大曲霉的分离鉴定及AFP的提纯%The Screening of a Antifungal Protein(AFP)-Producing Aspergillus giganteus and Purification of AFP

    Institute of Scientific and Technical Information of China (English)

    元月; 王德良; 郭立芸; 林智平; 江伟

    2012-01-01

    从土壤中分离出1株可产抗真菌蛋白的菌株,通过形态观察和分子生物学实验等方法鉴定其为巨大曲霉,编号AF-11。研究证明,利用纤维素阳离子交换柱层析法和凝胶柱层析法可从该菌的发酵上清液中分离纯化出高活性的抗真菌蛋白(AFP),该蛋白对青霉属、曲霉属和镰刀霉属等产毒丝状真菌的生长具有明显的抑制作用。%A strain which can produce antifungal protein was isolated from soil and was identified as Aspergillus giganteus,numbered AF-11,through morphologic observation and molecular biology experiments.It has been proven that the high activity and purity antifungal protein(AFP) which can obviously inhibit the growth of filamentous fungi such as Penicillium,Aspergillus and Fusarium,can be separated from the fermentation supernatant by using cellulose cation exchange column chromatography and gelatin column chromatography.

  6. 生防菌解淀粉芽孢杆菌抗菌蛋白的研究进展%Research Advances of Antifungal Proteins Produced by Biocontrol Bacterium,Bacillus amyloliquefaciens

    Institute of Scientific and Technical Information of China (English)

    出晓铭; 林毅雄; 张珅; 严芬; 林河通

    2014-01-01

    Bacillus amyloliquefaciens is a kind of biocontrol bacterium which has great ability against fungi and bacteria,thereby it has high research values and potential for development in biological control of posthar-vest diseases of fruits and vegetables.The separation and purification of antifungal proteins produced by Bacil-lus amyloliquefaciens,the disease resistant mechanisms and the application of biocontrol of antifungal proteins were summarized.The future potential application in biocontrol of postharvest diseases of fruits and vegetables was also discussed.%生防解淀粉芽孢杆菌具有强烈抑制真菌和细菌的能力,在果蔬采后病害防治方面具有巨大的应用潜力。该文对解淀粉芽孢杆菌产生的抗菌蛋白、蛋白的分离纯化、抑菌机理和生防应用等方面进行了综述,并对其在果蔬采后病害防治应用前景进行了展望。

  7. Characterisation of the Candida albicans Phosphopantetheinyl Transferase Ppt2 as a Potential Antifungal Drug Target.

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    Katharine S Dobb

    Full Text Available Antifungal drugs acting via new mechanisms of action are urgently needed to combat the increasing numbers of severe fungal infections caused by pathogens such as Candida albicans. The phosphopantetheinyl transferase of Aspergillus fumigatus, encoded by the essential gene pptB, has previously been identified as a potential antifungal target. This study investigated the function of its orthologue in C. albicans, PPT2/C1_09480W by placing one allele under the control of the regulatable MET3 promoter, and deleting the remaining allele. The phenotypes of this conditional null mutant showed that, as in A. fumigatus, the gene PPT2 is essential for growth in C. albicans, thus fulfilling one aspect of an efficient antifungal target. The catalytic activity of Ppt2 as a phosphopantetheinyl transferase and the acyl carrier protein Acp1 as a substrate were demonstrated in a fluorescence transfer assay, using recombinant Ppt2 and Acp1 produced and purified from E.coli. A fluorescence polarisation assay amenable to high-throughput screening was also developed. Therefore we have identified Ppt2 as a broad-spectrum novel antifungal target and developed tools to identify inhibitors as potentially new antifungal compounds.

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

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    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. Metal-Based Antibacterial and Antifungal Agents: Synthesis, Characterization, and In Vitro Biological Evaluation of Co(II, Cu(II, Ni(II, and Zn(II Complexes with Amino Acid-Derived Compounds

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    Zahid H. Chohan

    2006-01-01

    Full Text Available A series of antibacterial and antifungal amino acid-derived compounds and their cobalt(II, copper(II, nickel(II, and zinc(II metal complexes have been synthesized and characterized by their elemental analyses, molar conductances, magnetic moments, and IR, and electronic spectral measurements. Ligands (L1–(L5 were derived by condensation of β-diketones with glycine, phenylalanine, valine, and histidine and act as bidentate towards metal ions (cobalt, copper, nickel, and zinc via the azomethine-N and deprotonated-O of the respective amino acid. The stoichiometric reaction between the metal(II ion and synthesized ligands in molar ratio of M: L (1: 1 resulted in the formation of the metal complexes of type [M(L(H2O4]Cl (where M = Co(II, Cu(II, and Zn(II and of M: L (1: 2 of type [M(L2(H2O2] (where M = Co(II, Cu(II, Ni(II, and Zn(II. The magnetic moment data suggested for the complexes to have an octahedral geometry around the central metal atom. The electronic spectral data also supported the same octahedral geometry of the complexes. Elemental analyses and NMR spectral data of the ligands and their metal(II complexes agree with their proposed structures. The synthesized ligands, along with their metal(II complexes, were screened for their in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexeneri, Pseudomonas aeruginosa, and Salmonella typhi and two Gram-positive (Bacillus subtilis and Staphylococcus aureus bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, and Candida glaberata. The results of these studies show the metal(II complexes to be more antibacterial/antifungal against one or more species as compared to the uncomplexed ligands. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties. Five compounds, (3, (7, (10, (11, and (22, displayed potent cytotoxic

  10. Stark broadening measurements in plasmas produced by laser ablation of hydrogen containing compounds

    Science.gov (United States)

    Burger, Miloš; Hermann, Jörg

    2016-08-01

    We present a method for the measurement of Stark broadening parameters of atomic and ionic spectral lines based on laser ablation of hydrogen containing compounds. Therefore, plume emission spectra, recorded with an echelle spectrometer coupled to a gated detector, were compared to the spectral radiance of a plasma in local thermal equilibrium. Producing material ablation with ultraviolet nanosecond laser pulses in argon at near atmospheric pressure, the recordings take advantage of the spatially uniform distributions of electron density and temperature within the ablated vapor. By changing the delay between laser pulse and detector gate, the electron density could be varied by more than two orders of magnitude while the temperature was altered in the range from 6,000 to 14,000 K. The Stark broadening parameters of transitions were derived from their simultaneous observation with the hydrogen Balmer alpha line. In addition, assuming a linear increase of Stark widths and shifts with electron density for non-hydrogenic lines, our measurements indicate a change of the Stark broadening-dependence of Hα over the considered electron density range. The presented results obtained for hydrated calcium sulfate (CaSO4ṡ2H2O) can be extended to any kind of hydrogen containing compounds.

  11. Synthetic, structural and antifungal studies of coordination compounds of Ru(III, Rh(III and Ir(III with tetradentate Schiff bases

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    ANKITA SRIVASTAVA

    2006-09-01

    Full Text Available A series of octahedral Ru(III, Rh(III and Ir(III complexes have been prepared with tetradentate Schiff bases derived by condensing isatin with 1,2-diaminoethane, 1,3-diaminopropane, 1,4-diaminobutane, 1,2-diaminobenzene and 1,3-diaminobenzene. The obtained complexes were characterized on the basis of their elemental analyses, magnetic moment, conductance, IR, electronic, 1HNMR and FAB mass spectra, as well as thermal analyses. The Ru(III complexes are low spin paramagnetic, while Rh(III and Ir(III behave as diamagnetic complexes. The IR spectral data revealed that all the Schiff bases behave as tetradentate and are coordinated to Ru(III, Rh(III and Ir(III via nitrogen and oxygen. Antifungal studies of the ligands as well as their complexes were carried out by the agar plate method.

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

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    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.

  13. An overview of antifungal peptides derived from insect.

    Science.gov (United States)

    Faruck, Mohammad Omer; Yusof, Faridah; Chowdhury, Silvia

    2016-06-01

    Fungi are not classified as plants or animals. They resemble plants in many ways but do not produce chlorophyll or make their own food photosynthetically like plants. Fungi are useful for the production of beer, bread, medicine, etc. More complex than viruses or bacteria; fungi can be destructive human pathogens responsible for various diseases in humans. Most people have a strong natural immunity against fungal infection. However, fungi can cause diseases when this immunity breaks down. In the last few years, fungal infection has increased strikingly and has been accompanied by a rise in the number of deaths of cancer patients, transplant recipients, and acquired immunodeficiency syndrome (AIDS) patients owing to fungal infections. The growth rate of fungi is very slow and quite difficult to identify. A series of molecules with antifungal activity against different strains of fungi have been found in insects, which can be of great importance to tackle human diseases. Insects secrete such compounds, which can be peptides, as a part of their immune defense reactions. Active antifungal peptides developed by insects to rapidly eliminate infectious pathogens are considered a component of the defense munitions. This review focuses on naturally occurring antifungal peptides from insects and their challenges to be used as armaments against human diseases.

  14. Volatile organic compounds of Thai honeys produced from several floral sources by different honey bee species

    Science.gov (United States)

    Pattamayutanon, Praetinee; Angeli, Sergio; Thakeow, Prodpran; Abraham, John; Disayathanoowat, Terd; Chantawannakul, Panuwan

    2017-01-01

    The volatile organic compounds (VOCs) of four monofloral and one multifloral of Thai honeys produced by Apis cerana, Apis dorsata and Apis mellifera were analyzed by headspace solid-phase microextraction (HS-SPME) followed by gas chromatography and mass spectrometry (GC-MS). The floral sources were longan, sunflower, coffee, wild flowers (wild) and lychee. Honey originating from longan had more VOCs than all other floral sources. Sunflower honey had the least numbers of VOCs. cis-Linalool oxide, trans-linalool oxide, ho-trienol, and furan-2,5-dicarbaldehyde were present in all the honeys studied, independent of their floral origin. Interestingly, 2-phenylacetaldehyde was detected in all honey sample except longan honey produced by A. cerana. Thirty-two VOCs were identified as possible floral markers. After validating differences in honey volatiles from different floral sources and honeybee species, the results suggest that differences in quality and quantity of honey volatiles are influenced by both floral source and honeybee species. The group of honey volatiles detected from A. cerana was completely different from those of A. mellifera and A. dorsata. VOCs could therefore be applied as chemical markers of honeys and may reflect preferences of shared floral sources amongst different honeybee species. PMID:28192487

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

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    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.

  16. Regeneration of insulin-producing pancreatic cells using a volatile bioactive compound and human teeth.

    Science.gov (United States)

    Okada, Mio; Imai, Toshio; Yaegaki, Ken; Ishkitiev, Nikolay; Tanaka, Tomoko

    2014-10-30

    Transplantation of insulin (INS)-secreting cells differentiated in vitro from stem cells promises a safer and easier treatment of severe diabetes mellitus. A volatile bioactive compound, hydrogen sulfide (H2S), promotes cell differentiation; human tooth-pulp stem cells undergo hepatic differentiation. The aim of this study is to develop a novel protocol using H2S to enhance pancreatic differentiation from the CD117(+) cell fraction of human tooth pulp. During the differentiation, the cells were exposed to 0.1 ng ml(-1) H2S. Immunocytochemistry, RT-PCR, determination of INS c-peptide content and flow cytometry of pancreatically related markers were carried out. Expression of WNT and the PI3K/AKT signaling pathway were also determined by PCR array. After differentiation, INS, glucagon (GCG), somatostatin (SST) and pancreatic polypeptide (PPY) were positive when examined by immunofluorescence. INS and GCG were also determined flow-cytometrically. Only the cells expressing INS increased after H2S exposure. The number of cells expressing GCG was significantly decreased. Genes involved in canonical WNT and the WNT/calcium pathways were highly expressed after H2S exposure. H2S accelerated INS synthesis and secretion by regenerated INS-producing cells from human teeth. All signaling pathway functions of the PI3K-AKT pathway were extremely activated by H2S exposure. The matured INS-producing cells originating in human teeth were increased by H2S in order to control blood-glucose level.

  17. 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.

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

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    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.

  19. Plant Growth Promotion by Volatile Organic Compounds Produced by Bacillus subtilis SYST2

    Science.gov (United States)

    Tahir, Hafiz A. S.; Gu, Qin; Wu, Huijun; Raza, Waseem; Hanif, Alwina; Wu, Liming; Colman, Massawe V.; Gao, Xuewen

    2017-01-01

    Bacterial volatiles play a significant role in promoting plant growth by regulating the synthesis or metabolism of phytohormones. In vitro and growth chamber experiments were conducted to investigate the effect of volatile organic compounds (VOCs) produced by the plant growth promoting rhizobacterium Bacillus subtilis strain SYST2 on hormone regulation and growth promotion in tomato plants. We observed a significant increase in plant biomass under both experimental conditions; we observed an increase in photosynthesis and in the endogenous contents of gibberellin, auxin, and cytokinin, while a decrease in ethylene levels was noted. VOCs emitted by SYST2 were identified through gas chromatography-mass spectrometry analysis. Of 11 VOCs tested in glass jars containing plants in test tubes, only two, albuterol and 1,3-propanediole, were found to promote plant growth. Furthermore, tomato plants showed differential expression of genes involved in auxin (SlIAA1. SlIAA3), gibberellin (GA20ox-1), cytokinin (SlCKX1), expansin (Exp2, Exp9. Exp 18), and ethylene (ACO1) biosynthesis or metabolism in roots and leaves in response to B. subtilis SYST2 VOCs. Our findings suggest that SYST2-derived VOCs promote plant growth by triggering growth hormone activity, and provide new insights into the mechanism of plant growth promotion by bacterial VOCs. PMID:28223976

  20. Characterization of total retinoid-like activity of compounds produced by three common phytoplankton species.

    Science.gov (United States)

    Sychrová, Eliška; Priebojová, Jana; Smutná, Marie; Nováková, Kateřina; Kohoutek, Jiří; Hilscherová, Klára

    2016-12-01

    Phytoplankton can produce various bioactive metabolites, which may affect other organisms in the aquatic environment. This study provides the first information on the total retinoid-like activity associated with both intracellular and extracellular metabolites produced by selected phytoplankton species that could play a role in teratogenic effects and developmental disruption in exposed organisms. The studied species included a coccoid cyanobacteria (Microcystis aeruginosa), a filamentous cyanobacteria (Aphanizomenon gracile) and a green alga (Desmodesmus quadricauda), all of which commonly occur in freshwater bodies in Europe. Methanolic extracts from cellular material and extracellular exudates were prepared from cultures cultivated in two light-intensity variants with five replicates for each species. The retinoid-like activity was evaluated by in vitro assays along with chemical analyses of two potent retinoic acids (all-trans retinoic acid (ATRA) and 9cis-RA). The mean total retinoid-like activity of metabolites produced by the three studied species representing different phytoplankton taxonomic groups ranged from 705 to 5572ng ATRA equivalent/g dry matter corresponding to 0.064-0.234ng ATRA/10(6) cells. Retinoid-like activity was found in the cellular extracts of all species, while only the extracellular exudates of cyanobacteria exhibited detectable activity (41-1081ng ATRA/L). The greatest extracellular as well as total (extra- and intra- cellular together) retinoid-like activity was detected for Microcystis aeruginosa. The two potent retinoic acids studied were more frequently detected in cellular extracts than in extracellular exudates of all species. Their contribution to observed in vitro effects was relatively low for all tested samples (<10%), indicating a substantial contribution of other retinoid-like compounds to the overall activity. The results indicate possible influence of light intensity and cell density on the production of metabolites with

  1. Antimicrobial Action of Compounds from Marine Seaweed

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    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.

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

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    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.

  3. Antifungal activity and transdermal permeability in vitro of compound naftifine hydrochloride nanoemulsion%复方盐酸萘替芬纳米乳的体外抑菌活性和透皮性能

    Institute of Scientific and Technical Information of China (English)

    刘凯; 欧阳五庆; 王波臻; 王阳

    2016-01-01

    本研究旨在考察复方盐酸萘替芬纳米乳(NTF-CIN-NE)的体外抑菌活性和透皮性能,为其临床应用提供理论依据.用微量稀释法对NTF-CIN-NE体外抑菌性能进行考察;通过HPLC测定药物含量;利用改良的Franz扩散装置测定其透皮性能.体外抑菌试验表明,NTF-CIN-NE对犬小孢子菌、石膏样小孢子菌、须癣毛癣菌、红色毛癣菌的MIC分别是0.008,0.016,0.008,0.004 mg/L,MBC分别是0.156,0.156,0.039,0.039 mg/L,优于盐酸萘替芬(NTF)和肉桂醛(CIN)原药混合液.建立的HPLC测定NTF-CIN-NE中NTF和CIN的含量,方法的专属性好,准确度高.透皮试验表明NTF-CIN-NE的透皮性能显著优于原药混合液组(P<0.01)和含2%氮酮的原药混合液组(P<0.01).综上表明,以纳米乳为载体的NTF-CIN-NE,提高了抑菌活性和经皮渗透能力,有助于药物经皮给药和药物疗效的发挥.%This study were conducted to investigate the antifungal activity and transdermal speed of compound naftifine hydrochloride nanoemulsion (NTF-CIN-NE) in vitro for purpose of offering theoretical basis for its clinical application.Antifungal activity test of NTF-CIN-NE in vitro was conducted by using the microdilution method and the content of drugs was measured by HPLC.The evaluation of its transdermal permeability was conducted by utilizing modified Franz diffusion device.The results of antifungal activity test in vitro showed the MIC to microsporum canis,microsporum gypseum,trichophyton mentagrophytes and trichophyton rubrum (0.008,0.016,0.008 and 0.016 mg/L,respectively);MBC (0.156,0.156,0.039,0.156 mg/L,respectively),which was better than NTF and CIN technical mixture.The HPLC was a specific,high accuracy method to measure the content of NTF-CIN-NE.Transdermal experiments showed that transdermal performance of NTF-CIN-NE was significantly better than technical mixture group (P<0.01) and technical mixture containing 2% azone group (P<0.01).Overall,nanoemulsion as the carrier

  4. Metal based biologically active compounds: design, synthesis, and antibacterial/antifungal/cytotoxic properties of triazole-derived Schiff bases and their oxovanadium(IV) complexes.

    Science.gov (United States)

    Chohan, Zahid H; Sumrra, Sajjad H; Youssoufi, Moulay H; Hadda, Taibi B

    2010-07-01

    A new series of oxovanadium(IV) complexes have been designed and synthesized with a new class of triazole Schiff bases derived from the reaction of 3,5-diamino-1,2,4-triazole with 2-hydroxy-1-naphthaldehyde, pyrrole-2-carboxaldehyde, pyridine-2-carboxaldehyde and acetyl pyridine-2-carboxaldehyde, respectively. Physical (magnetic susceptibility, molar conductance), spectral (IR, (1)H NMR, (13)C NMR, mass and electronic) and analytical data have established the structures of these synthesized Schiff bases and their oxovanadium(IV) complexes. The Schiff bases, predominantly act as bidentate and coordinate with the vanadium(IV) metal to give a stoichiometric ratio of 1:2 [M:L], forming a general formulae, [M(L-H)(2)] and [M(L)(2)]SO(4) where L = (L(1))-(L(4)) and M = VO(IV) of these complexes in a square-pyramidal geometry. In order to evaluate the biological activity of Schiff bases and to assess the role of vanadium(IV) metal on biological activity, the triazole Schiff bases and their oxovanadium(IV) complexes have been studied for in vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexenari, Pseudomonas aeruginosa, Salmonella typhi) and two Gram-positive (Staphylococcus aureus, Bacillus subtilis) bacterial strains, in vitro antifungal activity against Trichophyton longifucus, Candida albican, Aspergillus flavus, Microscopum canis, Fusarium solani and Candida glaberata. The simple Schiff bases showed weaker to significant activity against one or more bacterial and fungal strains. In most of the cases higher activity was exhibited upon coordination with vanadium(IV) metal. Brine shrimp bioassay was also carried out for in vitro cytotoxic properties against Artemia salina.

  5. Human mycoses and advances in antifungal therapy.

    Science.gov (United States)

    Fromtling, R A

    2001-04-01

    The 11th Focus on Fungal Infections meeting was held in Washington, D.C., U.S.A., March 1416, 2001. At the conference, there were well-attended sessions that focused on the pathogenesis and therapy of fungal disease. This report focuses on new information on fungal incidence and pathogenesis as well as on the in vitro and clinical experience of established antifungal drugs (fluconazole, itraconazole, amphotericin B, liposomal formulations of amphotericin B, terbinafine) and the newer antifungal compounds approved for use (e.g., caspofungin) and in development (the new-generation azoles: voriconazole, posaconazole, ravuconazole, and the candins, micafungin and anidulafungin).

  6. Isolation and Structure Elucidation of Autolytimycin, A New Compound Produced by Streptomyces Autolyticus JX-47

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Autolytimycin 1 was isolated from the culture filtrate ofStreptomyces autolyticus JX-47,together with two known compounds, lebstatin 2 and 17-O-demethyl-geldanamycin 3. These compounds showed the activities of anti-HSV-I. The structure of 1 was determined by spectral analysis.

  7. 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.

  8. A simple, convenient, and one pot synthetic route for the preparation of 1,3,5-thiadiazines-2-thione heterocyclic compounds and their antifungal activity

    Directory of Open Access Journals (Sweden)

    Sohail Saeed

    2015-12-01

    Full Text Available A series of new heterocyclic 1,3,5-thiadiazines-2-thione with aroyl/aryl substituents (3a-c were synthesized by reacting isothiocyanates with N- (propan-2-ylpropan-2- amine in the presence of tetrabutylammonium bromide as phase transfer catalyst. The structures of these novel compounds were characterized by IR, mass spectrometry, and elemental analysis. The crystal structures were determined from single-crystal X-ray diffraction data. The synthesized compounds were tested in vitro against Fusarium solani, A. fumigatus, and Aspergillus flavus using standard drugs.

  9. Identification of geosmin and 2-methylisoborneol in cyanobacteria and molecular detection methods for the producers of these compounds.

    Science.gov (United States)

    Suurnäkki, Suvi; Gomez-Saez, Gonzalo V; Rantala-Ylinen, Anne; Jokela, Jouni; Fewer, David P; Sivonen, Kaarina

    2015-01-01

    Geosmin and 2-methylisoborneol (MIB) are muddy/earthy off-flavor metabolites produced by a range of bacteria. Cyanobacteria are the major producers of the volatile metabolites geosmin and MIB which produce taste and odor problems in drinking water and fish worldwide. Here we detected geosmin and MIB by studying 100 cyanobacteria strains using solid phase microextraction gas chromatography mass spectrometry (SPME GC-MS). A total of 21 geosmin producers were identified from six cyanobacteria genera. Two of the geosmin producers also produced MIB. A PCR protocol for the detection of geoA and MIB synthase genes involved in the biosynthesis of geosmin and MIB was developed. The geoA and MIB synthase genes were detected in all strains shown to produce geosmin and MIB, respectively. Cyanobacterial geoA and MIB synthase sequences showed homology to terpene synthases genes of actinobacteria and proteobacteria. Additional off-flavor compounds, nor-carotenoids β-ionone and β-cyclocitral, were found from 55 strains among the 100 cyanobacterial strains studied; β-ionone was present in 45 and β-cyclocitral in 10 strains. Six of the cyanobacteria which contain off-flavor compounds also produced toxins, anatoxin-a or microcystins. The molecular method developed is a useful tool in monitoring potential cyanobacterial producers of geosmin and MIB.

  10. Active packaging with antifungal activities.

    Science.gov (United States)

    Nguyen Van Long, N; Joly, Catherine; Dantigny, Philippe

    2016-03-01

    There have been many reviews concerned with antimicrobial food packaging, and with the use of antifungal compounds, but none provided an exhaustive picture of the applications of active packaging to control fungal spoilage. Very recently, many studies have been done in these fields, therefore it is timely to review this topic. This article examines the effects of essential oils, preservatives, natural products, chemical fungicides, nanoparticles coated to different films, and chitosan in vitro on the growth of moulds, but also in vivo on the mould free shelf-life of bread, cheese, and fresh fruits and vegetables. A short section is also dedicated to yeasts. All the applications are described from a microbiological point of view, and these were sorted depending on the name of the species. Methods and results obtained are discussed. Essential oils and preservatives were ranked by increased efficacy on mould growth. For all the tested molecules, Penicillium species were shown more sensitive than Aspergillus species. However, comparison between the results was difficult because it appeared that the efficiency of active packaging depended greatly on the environmental factors of food such as water activity, pH, temperature, NaCl concentration, the nature, the size, and the mode of application of the films, in addition to the fact that the amount of released antifungal compounds was not constant with time.

  11. Producing a compound Nucleus via Inelastic Scattering: The 90Zr(alpha,alpha')90Zr* Case

    Energy Technology Data Exchange (ETDEWEB)

    Escher, J E; Dietrich, F S

    2008-05-23

    In a Surrogate reaction a compound nucleus is produced via a direct reaction (pickup, stripping, or inelastic scattering). For a proper application of the Surrogate approach it is necessary to predict the resulting angular momentum and parity distribution in the compound nucleus. A model for determining these distributions is developed for the case of inelastic alpha scattering off a spherical nucleus. The focus is on obtaining a first, simple description of the direct-reaction process that produces the compound nucleus and on providing the basis for a more complete treatment of the problem. The approximations employed in the present description are discussed and the extensions required for a more rigorous treatment of the problem are outlined. To illustrate the formalism, an application to {sup 90}Zr({alpha},{alpha}{prime}){sup 90}Zr* is presented.

  12. Identification and classification of known and putative antimicrobial compounds produced by a wide variety of Bacillales species

    NARCIS (Netherlands)

    Zhao, Xin; Kuipers, Oscar P

    2016-01-01

    BACKGROUND: Gram-positive bacteria of the Bacillales are important producers of antimicrobial compounds that might be utilized for medical, food or agricultural applications. Thanks to the wide availability of whole genome sequence data and the development of specific genome mining tools, novel anti

  13. Antibacterial, antifungal and cytotoxic activity of terrestrial cyanobacterial strains from Serbia

    Institute of Scientific and Technical Information of China (English)

    Zorica SVIRCEV; Dragana CETOJEVIC-SIMIN; Jelica SIMEUNOVIC; Maja KARAMAN; Dejan STOJANOVIC

    2008-01-01

    Cyanobacteria are known to be a rich source of biologically active compounds some of which can have pharmaceutical importance. In this work we present the screening results of cyanobacterial strains for their antibacterial, antifungal, and cytotoxic activity. Cyanobacterial strains were isolated from various soil types in province of Vojvodina and Central Serbia, Republic of Serbia. The screening included 9 strains of Anabaena and 9 strains of Nostoc. Both, extracellular products (from the culture liquid) and cellular crude Iipophilic extracts were tested against 13 bacterial strains and 8 fungal strains. Cytotoxic activity was tested against three human cell lines. Methanol extracts were prepared according to φstensvik. Antibacterial and antifungal activities were determined measuring inhibition zone, 48 h after inoculation. The cytotoxic activity was determined by suIforhodamine B (SRB) colorimetric assay. Of all cyanobacterial strains tested, 52% showed some antifungal and 41% antibacterial activity. Two out of six tested strains possessed cytotoxic activity. The cytotoxic activity of Anabaena strain S12 was found both in culture liquid and crude cell extract. It occurred specifically between the 21st and 42nd day of cultivation against HeLa and MCF7 cells, but had no activity against cell line derived from a healthy tissue. A high percentage of the active strains among the tested strains justify the effort of screening cyanobacteria that are isolated from terrestrial environments. The most promising strains for the fur-ther study are Anabaena strain S12 which showed strong cytotoxic and antibacterial activity and Ana-baena strain S20 which produces a potent antifungal compound. The future work, besides further screening and chemical identification of the active compounds, should also include the development of culture techniques that would lead to more efficient production of biologically active compounds.

  14. Antibacterial, antifungal and cytotoxic activity of terrestrial cyanobacterial strains from Serbia

    Institute of Scientific and Technical Information of China (English)

    Zorica; SVIRCEV; Dragana; CETOJEVIC-SIMIN; Jelica; SIMEUNOVIC; Maja; KARAMAN; Dejan; STOJANOVIC

    2008-01-01

    Cyanobacteria are known to be a rich source of biologically active compounds some of which can have pharmaceutical importance. In this work we present the screening results of cyanobacterial strains for their antibacterial, antifungal, and cytotoxic activity. Cyanobacterial strains were isolated from various soil types in province of Vojvodina and Central Serbia, Republic of Serbia. The screening included 9 strains of Anabaena and 9 strains of Nostoc. Both, extracellular products (from the culture liquid) and cellular crude lipophilic extracts were tested against 13 bacterial strains and 8 fungal strains. Cytotoxic activity was tested against three human cell lines. Methanol extracts were prepared according to ?stensvik. Antibacterial and antifungal activities were determined measuring inhibition zone, 48 h after inoculation. The cytotoxic activity was determined by sulforhodamine B (SRB) colorimetric assay. Of all cyanobacterial strains tested, 52% showed some antifungal and 41% antibacterial activity. Two out of six tested strains possessed cytotoxic activity. The cytotoxic activity of Anabaena strain S12 was found both in culture liquid and crude cell extract. It occurred specifically between the 21st and 42nd day of cultivation against HeLa and MCF7 cells, but had no activity against cell line derived from a healthy tissue. A high percentage of the active strains among the tested strains justify the effort of screening cyanobacteria that are isolated from terrestrial environments. The most promising strains for the fur- ther study are Anabaena strain S12 which showed strong cytotoxic and antibacterial activity and Ana- baena strain S20 which produces a potent antifungal compound. The future work, besides further screening and chemical identification of the active compounds, should also include the development of culture techniques that would lead to more efficient production of biologically active compounds.

  15. Antifungal properties of halofumarate esters.

    Science.gov (United States)

    Gershon, H; Shanks, L

    1978-04-01

    Alkyl esters (C1--C4) of the four halofumaric acids were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes at pH 5.6 and 7.0 in the absence and presence of 10% beef serum in Sabouraud dextrose agar. The most toxic compound to each organism was: C. albicans, ethyl iodofumarate (0.054 mmole/liter); A. niger, methyl bromofumarate (0.090 mmole/liter); M. mucedo, methyl fluorofumarate (0.037 mmole/liter); and T. mentagrophytes, ethyl iodofumarate (0.020 mmole/liter). The order of overall activity of the six most toxic compounds was: ethyl iodofumarate greater than ethyl chlorofumarate greater than methyl iodofumarate = methyl bromofumarate greater than methyl chlorofumarate greater than bromofumarate.

  16. Synthesis of quarternary ammonium salts with dithiocarbamate moiety and their antifungal activities against Helminthosporium oryzae

    Indian Academy of Sciences (India)

    Mandeep Singh; Anita Garg; Anjali Sidhu; Vineet Kumar

    2013-05-01

    Quaternary ammonium salts containing dithiocarbamate moiety were synthesized and evaluated for their antifungal activities against Helminthosporium oryzae. All the synthesized compounds showed moderate to promising fungitoxicity against the test. Some of the synthesized compounds inflicted antifungal activity greater than the standard fungicide.

  17. Structure identification for compound I separated and purified from taxoids-produced endophytic fungi (Alternaria. alternata var. taxi 1011)

    Institute of Scientific and Technical Information of China (English)

    XIANG Yong; LIU Jun; LU An-guo; CUI Jing-xia

    2003-01-01

    Endophytic fungi are widely found in almost all kinds of plants. Many endophytic fungi can produce some physiological active compounds, which are same to or analog to those isolated from their hosts. Producing physiological active compounds through microbial fermentation can give a new way to resolve resource limitation and to find out alternative source. Through the methods of organic solvent extraction, thin layer chromatography (TLC) and column chromatography, compound I was isolated, purified from the liquid fermentation metabolites of the taxoids-produced endophytic fungi (Alternaria. alternata var. taxi 1011 Y. Xiang et LU An-guo) that was screened from the bark of Taxus. cuspidata Sieb.et Zucc.. Compound I was identified as one kind of taxoids type III, based on the analyzing results by using the methods of ultraviolet spectroscopy (UV), infrared spectroscopy (IR), mass spectrometry (MS) and nuclear magnetic resonance spectroscopy (NMR). This study provides a completed method for separation and purification of the endophytic fungi as well as structure identification of its fermentation metabolite

  18. Odorant receptors from the light brown apple moth (Epiphyas postvittana) recognize important volatile compounds produced by plants.

    Science.gov (United States)

    Jordan, Melissa D; Anderson, Alisha; Begum, Doreen; Carraher, Colm; Authier, Astrid; Marshall, Sean D G; Kiely, Aidan; Gatehouse, Laurence N; Greenwood, David R; Christie, David L; Kralicek, Andrew V; Trowell, Stephen C; Newcomb, Richard D

    2009-06-01

    Moths recognize a wide range of volatile compounds, which they use to locate mates, food sources, and oviposition sites. These compounds are recognized by odorant receptors (OR) located within the dendritic membrane of sensory neurons that extend into the lymph of sensilla, covering the surface of insect antennae. We have identified 3 genes encoding ORs from the tortricid moth, Epiphyas postvittana, a pest of horticulture. Like Drosophila melanogaster ORs, they contain 7 transmembrane helices with an intracellular N-terminus, an orientation in the plasma membrane opposite to that of classical GPCRs. EpOR2 is orthologous to the coreceptor Or83b from D. melanogaster. EpOR1 and EpOR3 both recognize a range of terpenoids and benzoates produced by plants. Of the compounds tested, EpOR1 shows the best sensitivity to methyl salicylate [EC(50) = 1.8 x 10(-12) M], a common constituent of floral scents and an important signaling compound produced by plants when under attack from insects and pathogens. EpOR3 best recognizes the monoterpene citral to low concentrations [EC(50) = 1.1 x 10(-13) M]. Citral produces the largest amplitude electrophysiological responses in E. postvittana antennae and elicits repellent activity against ovipositing female moths. Orthologues of EpOR3 were found across 6 families within the Lepidoptera, suggesting that the ability to recognize citral may underpin an important behavior.

  19. Can agricultural fungicides accelerate the discovery of human antifungal drugs?

    Science.gov (United States)

    Myung, Kyung; Klittich, Carla J R

    2015-01-01

    Twelve drugs from four chemical classes are currently available for treatment of systemic fungal infections in humans. By contrast, more than 100 structurally distinct compounds from over 30 chemical classes have been developed as agricultural fungicides, and these fungicides target many modes of action not represented among human antifungal drugs. In this article we introduce the diverse aspects of agricultural fungicides and compare them with human antifungal drugs. We propose that the information gained from the development of agricultural fungicides can be applied to the discovery of new mechanisms of action and new antifungal agents for the management of human fungal infections.

  20. Benzaldehyde as an insecticidal, antimicrobial, and antioxidant compound produced by Photorhabdus temperata M1021.

    Science.gov (United States)

    Ullah, Ihsan; Khan, Abdul Latif; Ali, Liaqat; Khan, Abdur Rahim; Waqas, Muhammad; Hussain, Javid; Lee, In-Jung; Shin, Jae-Ho

    2015-02-01

    The Photorhabdus temperata M1021 secretes toxic compounds that kill their insect hosts by arresting immune responses. Present study was aimed to purify the insecticidal and antimicrobial compound(s) from the culture extract of P. temperata M1021 through bioassay guided fractionation. An ethyl acetate (EtOAc) extract of the P. temperata M1021 exhibited 100% mortality in Galleria mellonella larvae within 72 h. In addition, EtOAc extract and bioactive compound 1 purified form the extract through to column chromatography, showed phenol oxidase inhibition up to 60% and 80% respectively. The analysis of (1)H and (13)C NMR spectra revealed the identity of pure compound as "benzaldehyde". The benzaldehyde showed insecticidal activity against G. mellonella in a dose-dependent manner and 100% insect mortality was observed at 108 h after injection of 8 mM benzaldehyde. In a PO inhibition assay, 4, 6, and 8 mM concentrations of benzaldehyde were found to inhibit PO activity about 15%, 42%, and 80% respectively. In addition, nodule formation was significantly (P benzaldehyde as compare to control. Moreover, benzaldehyde was found to have great antioxidant activity and maximum antioxidant activity was 52.9% at 8 mM benzaldehyde as compare to control. Antimicrobial activity was assessed by MIC values ranged from 6 mM 10 mM for bacterial strains and 8 mM to 10 mM for fungal strains. The results suggest that benzaldehyde could be applicable for developing novel insecticide for agriculture use.

  1. Evaluation of Antifungal and Antibacterial Activity and Analysis of Bioactive Phytochemical Compounds of Cinnamomum Zeylanicum (Cinnamon Bark using Gas Chromatography-Mass Spectrometry

    Directory of Open Access Journals (Sweden)

    Imad Hadi Hameed

    2016-08-01

    Full Text Available Phytochemicals are chemical compounds often referred to as secondary metabolites. Thirty nine bioactive phytochemical compounds were identified in the methanolic extract of Cinnamon bark. The identification of phytochemical compounds is based on the peak area, retention time molecular weight and molecular formula. GC-MS analysis of Cinnamomum zeylanicum revealed the existence of the 6 -Oxa-bicyclo[3.1.0]hexan-3-one, Benzaldehyde, Cyclohexene,4-isopropenyl-1-methoxymethoxymethyl, Benzoic acid- methyl ester, Benzaldehyde dimethyl acetal, Benzenepropanal, Benzylidenemalonaldehyde, 3-Phenylpropanol, Cinnamaldehyde, (E, 2-Propen- 1- ol,3-phenyl, 9-Methoxybicyclo[6.1.0]nona – 2,4,6- triene , 1,3-Bis(cinnamoyloxymethyladamantine, Alfa.– Copaene, Naphthalene , 1,2,3,5,6,7,8,8a-octahydro-1,8a-dimethyl-7-(1-methyl, Cis – 2-Methoxycinnamic acid, Bicyclo[3.1.1]hept-2-ene,2,6- dimethyl-6-(4-methyl-3-pentenyl, Trans-2-Hydroxycinnamic acid , methyl ester, y-Muurolene, ß-Guaiene, Cadala-1(10,3,8-triene, Isolongifolene,4,5,9,10-dehydro, Cubenol, Tau-Muurolol, Α-Cadinol , Spiro[tricyclo[4.4.0.0(5.9]decane-10.2oxirane],1-methyl-4-isoprol, 6-Isopropenyl-4,8q-dimethyl-1,2,3,5,6,7,8,8a-octahydronaphthalen, Ethyl9,9-difomylnona-2,4,6,8-tetraenoate, Trans-13-Octadecenoic acid, Tributyl acetylcitrate, 9,12,15-Octadecatrienoic acid ,2,3-dihydroxypropyl ester, 9-Octadecenamide, 17.alfa.-21ß-28,30-Bisnorhopane, 17.alfa.-21ß-28,30-Bisnorhopane, Androstan-3-one,cyclic 1,2-ethanediyl mercaptole , (5α, (4H4a,5,6,7,8,8a-Hexahydrobenzopyran-5-one-3-carboxamide,2, 4H-Cyclopropa[5´,6´]benz [1´,2´,7,8]azuleno[5,6]oxiren-4-one,8,8a, (22S-21-Acetoxy-6α,11ß-dihydroxy-16α,17α-propylmethylenediox, (+-γ-Tocopherol,O-methyl and Stigmasterol. Cinnamomum zeylanicum contain chemical constitutions which may be useful for various herbal formulation as anti-inflammatory, analgesic, antipyretic, cardiac tonic and antiasthamatic. Cinnamomum zeylanicum was highly active against

  2. Synthesis and antifungal activity of derivatives of 2- and 3-benzofurancarboxylic acids.

    Science.gov (United States)

    Hejchman, Elzbieta; Ostrowska, Kinga; Maciejewska, Dorota; Kossakowski, Jerzy; Courchesne, William E

    2012-11-01

    We found that amiodarone has potent antifungal activity against a broad range of fungi, potentially defining a new class of antimycotics. Investigations into its molecular mechanisms showed amiodarone mobilized intracellular Ca2+, which is thought to be an important antifungal characteristic of its fungicidal activity. Amiodarone is a synthetic drug based on the benzofuran ring system, which is contained in numerous compounds that are both synthetic and isolated from natural sources with antifungal activity. To define the structural components responsible for antifungal activity, we synthesized a series of benzofuran derivatives and tested them for the inhibition of growth of two pathogenic fungi, Cryptococcus neoformans and Aspergillus fumigatus, to find new compounds with antifungal activity. We found several derivatives that inhibited fungal growth, two of which had significant antifungal activity. We were surprised to find that calcium fluxes in cells treated with these derivatives did not correlate directly with their antifungal effects; however, the derivatives did augment the amiodarone-elicited calcium flux into the cytoplasm. We conclude that antifungal activity of these new compounds includes changes in cytoplasmic calcium concentration. Analyses of these benzofuran derivatives suggest that certain structural features are important for antifungal activity. Antifungal activity drastically increased on converting methyl 7-acetyl-6-hydroxy-3-methyl-2-benzofurancarboxylate (2b) into its dibromo derivative, methyl 7-acetyl-5-bromo-6-hydroxy-3-bromomethyl-2-benzofurancarboxylate (4).

  3. Antileishmanial, antimicrobial and antifungal activities of some new aryl azomethines.

    Science.gov (United States)

    Al-Kahraman, Yasser M S A; Madkour, Hassan M F; Ali, Dildar; Yasinzai, Masoom

    2010-01-28

    A series of eighteen azomethines has been synthesized by the reaction of appropriate primary aromatic amines with aryl and/or heteroaryl carboxaldehydes. The synthesized azomethines have been evaluated for their in vitro antileishmanial, antibacterial and antifungal activities. The results revealed some antifungal activity of most of the synthesized compounds, whereas the antileishmaniasis activity results highlighted that all synthesized azomethines inhibited parasite growth and most of them showed highly potent action towards Leishmania major promastigotes. No remarkable bactericidal activities were observed.

  4. 7-Chloroquinolin-4-yl Arylhydrazone Derivatives: Synthesis and Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Auri R. Duval

    2011-01-01

    Full Text Available Fifteen 7-chloro-4-arylhydrazonequinolines have been evaluated for their in vitro antifungal activity against eight oral fungi: Candida albicans, C. parapsilosis, C. lipolytica, C. tropicalis, C. famata, C. glabrata, Rhodutorula mucilaginosa, and R. glutinis. Several compounds exhibited minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC activities comparable with the first-line drug fluconazole. These results could be considered as an important starting point for the rational design of new antifungal agents.

  5. Inter- and intraspecific variation in defensive compounds produced by five neotropical stink bug species (Hemiptera: Pentatomidae).

    Science.gov (United States)

    Pareja, Martín; Borges, Miguel; Laumann, Raúl A; Moraes, Maria C B

    2007-07-01

    The differences in composition of defensive secretions between nymphs, adult males and adult females of Chinavia impicticornis (=Acrosternum impicticorne), Chinavia ubica (=Acrosternum ubicum), Euschistus heros, Dichelops melacanthus and Piezodorus guildinii (Hemiptera, Pentatomidae) were analysed within and between species using compositional log-ratio statistics and canonical variates analysis. Differences in composition between nymphs, males and females were found for all species, as well as when all species were pooled. In particular, tetradecanal appears to be a predominantly nymphal compound in D. melacanthus, E. heros and P. guildinii. In the two Chinavia species 4-oxo-(E)-2-hexenal and an unknown compound were more dominant in nymphs. The interspecific analysis revealed a good separation of defensive compounds according to their taxonomic relationship. Thus, the two Chinavia species grouped together, with (E)-2-decenal and (E)-2-hexenyl acetate, contributing to this separation. The other three species also differed from each other, with (E)-2-octenal associated to D. melacanthus, (E)-2-hexenal to P. guildinii and (E,E)-2,4-decadienal and tetradecanal to E. heros. The pooled analysis of stage ignoring species revealed tetradecanal and 4-oxo-(E)-2-decenal (tentative identification) strongly associated to nymphs. Thus, there are predictable differences between stages, and many of the differences are conserved between species. Consideration of these differences could prove to be important in understanding stink bug-natural enemy interactions, and in optimising biocontrol efforts.

  6. Study on a method for loading a Li compound to produce tritium using high-temperature gas-cooled reactor

    Energy Technology Data Exchange (ETDEWEB)

    Nakaya, Hiroyuki, E-mail: nakaya@nucl.kyushu-u.ac.jp [Department of Applied Quantum Physics and Nuclear Engineering, Kyushu University, 744 Motooka, Fukuoka 8190395 (Japan); Matsuura, Hideaki [Department of Applied Quantum Physics and Nuclear Engineering, Kyushu University, 744 Motooka, Fukuoka 8190395 (Japan); Katayama, Kazunari [Department of Advanced Energy Engineering Science, Kyushu University, 6-1 Kasuga-koen, Kasuga 8168580 (Japan); Goto, Minoru; Nakagawa, Shigeaki [Japan Atomic Energy Agency, 4002 Oarai, Ibaraki (Japan)

    2015-10-15

    Highlights: • Tritium production by a high-temperature gas-cooled reactor was studied. • The loading method considering tritium outflow suppression was estimated. • A reactor with 600 MWt produced 400–600 g of tritium for 180 days. • A possibility that tritium outflow can be sufficiently suppressed was shown. - Abstract: Tritium production using high-temperature gas-cooled reactors and its outflow from the region loading Li compound into the helium coolant are estimated when considering the suppression of tritium outflow. A Li rod containing a cylindrical Li compound placed in an Al{sub 2}O{sub 3} cladding tube is assumed as a method for loading Li compound. A gas turbine high-temperature reactor of 300 MW electrical nominal capacity (GTHTR300) with 600 MW thermal output power is considered and modeled using the continuous-energy Monte Carlo transport code MVP-BURN, where burn-up simulations are carried out. Tritium outflow is estimated from equilibrium solution for the tritium diffusion equation in the cladding tube. A GTHTR300 can produce 400–600 g of tritium over a 180-day operation using the chosen method of loading the Li compound while minimizing tritium outflow from the cladding tube. Optimizing tritium production while suppressing tritium outflow is discussed.

  7. A methodological approach to screen diverse cheese-related bacteria for their ability to produce aroma compounds.

    Science.gov (United States)

    Pogačić, Tomislav; Maillard, Marie-Bernadette; Leclerc, Aurélie; Hervé, Christophe; Chuat, Victoria; Yee, Alyson L; Valence, Florence; Thierry, Anne

    2015-04-01

    Microorganisms play an important role in the development of cheese flavor. The aim of this study was to develop an approach to facilitate screening of various cheese-related bacteria for their ability to produce aroma compounds. We combined i) curd-based slurry medium incubated under conditions mimicking cheese manufacturing and ripening, ii) powerful method of extraction of volatiles, headspace trap, coupled to gas chromatography-mass spectrometry (HS-trap-GC-MS), and iii) metabolomics-based method of data processing using the XCMS package of R software and multivariate analysis. This approach was applied to eleven species: five lactic acid bacteria (Leuconostoc lactis, Lactobacillus sakei, Lactobacillus paracasei, Lactobacillus fermentum, and Lactobacillus helveticus), four actinobacteria (Brachybacterium articum, Brachybacterium tyrofermentans, Brevibacterium aurantiacum, and Microbacterium gubbeenense), Propionibacterium freudenreichii, and Hafnia alvei. All the strains grew, with maximal populations ranging from 7.4 to 9.2 log (CFU/mL). In total, 52 volatile aroma compounds were identified, of which 49 varied significantly in abundance between bacteria. Principal component analysis of volatile profiles differentiated species by their ability to produce ethyl esters (associated with Brachybacteria), sulfur compounds and branched-chain alcohols (H. alvei), branched-chain acids (H. alvei, P. freudenreichii and L. paracasei), diacetyl and related carbonyl compounds (M. gubbeenense and L. paracasei), among others.

  8. 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

    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...... was similar.   CONCLUSION: The investigated B. subtilis, BS1, BS2 and BS3 can be considered as potential starter cultures for the fermentation of African locust beans to produce good quality of Beninese food condiments. Copyright © 2009 Society of Chemical Industry...

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

    Science.gov (United States)

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

    2016-07-05

    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-phosphate and/or ribulose 5-phosphate to DXP, or (b) a YajO, or functional variant thereof, and a XylB, or functional variant thereof.

  10. Short-term and long-term behavior of PP-polymer nanocomposites produced by injection molding compounding

    Science.gov (United States)

    Battisti, M. G.; Guttmann, P.; Chitu, L.; Friesenbichler, W.

    2015-05-01

    There are only few investigations considering the impact of nanoscale fillers on the mechanical und thermo-mechanical properties of polymers. Particularly there is a lack of results regarding long term creep behavior of Polypropylene-based polymer nanocomposites (PNCs). Therefore, the objective of this study is to determine the influence of nanofiller content on the mechanical and thermo-mechanical behavior of Polypropylene-based PNCs. Processing of the test specimens was carried out using the Polymer NanoComposite Injection Molding Compounder (PNC-IMC). In comparison to the conventional compounding process, in which the compound must be pelletized and fed into the injection molding machine for the second plasticizing process, injection molding compounding combines these two processing steps. Material compounding and subsequent injection molding are done directly with only one plasticizing process, using a heated melt pipe and a melt accumulator for melt transfer from the compounder to the injection molding machine. The PNCs were produced in the 3-in-1 process at the PNC-IMC, where all components (polymer, compatibilizer, nanofiller) were added simultaneously into the compounder. Furthermore, the polymer melt was treated using elongational flow generating devices for better intercalation and exfoliation of the nanofillers. Tensile tests were made to characterize the short-term-mechanical properties. Tensile creep tests show the influence of nanofillers on the long-term-creep-performance and dynamic mechanical tests (DMA) were performed to investigate the thermo-mechanical behavior. Both, the improvements in the mechanical and thermo-mechanical properties in comparison to the pure polypropylene are shown and give an excellent overview of possibilities and limitations of the PNCs. Further research will focus on the detailed understanding of the different mechanisms of property improvement of layered silicates in polymer. By using small angle X-ray scattering

  11. Antifungal pharmacokinetics and pharmacodynamics.

    Science.gov (United States)

    Lepak, Alexander J; Andes, David R

    2014-11-10

    Successful treatment of infectious diseases requires choice of the most suitable antimicrobial agent, comprising consideration of drug pharmacokinetics (PK), including penetration into infection site, pathogen susceptibility, optimal route of drug administration, drug dose, frequency of administration, duration of therapy, and drug toxicity. Antimicrobial pharmacokinetic/pharmacodynamic (PK/PD) studies consider these variables and have been useful in drug development, optimizing dosing regimens, determining susceptibility breakpoints, and limiting toxicity of antifungal therapy. Here the concepts of antifungal PK/PD studies are reviewed, with emphasis on methodology and application. The initial sections of this review focus on principles and methodology. Then the pharmacodynamics of each major antifungal drug class (polyenes, flucytosine, azoles, and echinocandins) is discussed. Finally, the review discusses novel areas of pharmacodynamic investigation in the study and application of combination therapy.

  12. 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.

  13. 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.

  14. Marine bacteria producing antibacterial compounds isolated from inter-tidal invertebrates

    OpenAIRE

    León, Jorge; Laboratorio de Microbiología Ambiental y Biotecnología, Facultad de Ciencias Biológicas, Universidad Nacional Mayor de San Marcos, Apartado 110058, Lima Perú.; Liza, Libia; Laboratorio de Microbiología Ambiental y Biotecnología, facultad de Ciencias Biológicas,Universidad Nacional Mayor de San Marcos, Lima, Perú. Biólogo. Microbiólogo.; Soto, Isela; Laboratorio de Microbiología Ambiental y Biotecnología, Facultad de Ciencias Biológicas, Universidad Nacional Mayor de San Marcos, Apartado 110058, Lima Perú.; Torres, Magali; Laboratorio de Microbiología Ambiental y Biotecnología, facultad de Ciencias Biológicas,Universidad Nacional Mayor de San Marcos, Lima, Perú. Biólogo. Microbiólogo; Orosco, Andrés; Laboratorio de Microbiología Ambiental y Biotecnología, facultad de Ciencias Biológicas,Universidad Nacional Mayor de San Marcos, Lima, Perú. Biólogo. Microbiólogo

    2010-01-01

    Prospective sampling activities of intertidal invertebrates in the Ancon Bay (Lima, Peru) were done in order to select marine bacteria producing antimicrobial substances. The study included the isolation of bacteria in marine agar, in vitro antimicrobial susceptibility testing and electronic microscopic observations. We report the isolation, phenotypical characterization and antimicrobial properties of 10 strains of marine bacteria including the genus Vibrio, Pseudomonas, and Flavobacteri...

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

    Science.gov (United States)

    Frisvad, Jens C; Houbraken, Jos; Popma, Suuske; Samson, Robert A

    2013-02-01

    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 conidiophores with echinulate thick-walled conidia and produce the extrolites asperphenamate, citreoisocoumarin, communesin A and B, asperentin and 5'-hydroxy-asperentin. Penicillium spathulatum is unique in having restricted colonies on Czapek yeast agar (CYA) with an olive grey reverse, good growth on CYA supplemented with 5% NaCl, terverticillate bi- and ter-ramulate conidiophores and consistently produces the extrolites benzomalvin A and D and asperphenamate. The two new species belong to Penicillium section Brevicompacta and are phylogenetically closely related to Penicillium tularense. With exception of Penicillium fennelliae, asperphenamate is also produced by all other species in section Brevicompacta (P. tularense, Penicillium brevicompactum, Penicillium bialowiezense, Penicillium olsonii, Penicillium astrolabium and Penicillium neocrassum). Both new species have a worldwide distribution. The new species 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.

  16. 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...... supplemented with 5% NaCl, terverticillate bi- and ter-ramulate conidiophores and consistently produces the extrolites benzomalvin A and D and asperphenamate. The two new species belong to Penicillium section Brevicompacta and are phylogenetically closely related to Penicillium tularense. With exception...... of Penicillium fennelliae, asperphenamate is also produced by all other species in section Brevicompacta (P. tularense, Penicillium brevicompactum, Penicillium bialowiezense, Penicillium olsonii, Penicillium astrolabium and Penicillium neocrassum). Both new species have a worldwide distribution. The new species...

  17. 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...

  18. Use of pervaporation process for the recovery of aroma compounds produced by P. fermentans in sugarcane molasses.

    Science.gov (United States)

    Rossi, Suzan Cristina; Medeiros, Adriane Bianchi Pedroni; Weschenfelder, Thiago André; de Paula Scheer, Agnes; Soccol, Carlos Ricardo

    2017-03-17

    Natural fruity aroma was produced during submerged fermentation by Pichia fermentans using sugarcane molasses as a cultivation broth. The aroma compounds were recovered from the fermentation by a pervaporation process using a polydimethylsiloxane membrane (Pervap 4060-Sulzer). Isoamyl acetate, a characteristic compound associated with fruity aromas, was the major compound produced. The pervaporation module was fed at three different temperatures to test the best conditions to recover the natural fruity aroma. The total flux (J T), partial fluxes of each component (J i), and enrichment factors (β) were determined within the tested ranges. The process was performed at 45 °C, a feed flow of 1.5 mL/min and 0.1 kPa, for a duration of 13 h to concentrate the natural flavor. The pervaporation process can concentrate the isoamyl acetate from fermented broth from 9 to 61.8 mg/L in the first hour of pervaporation. As a single step of downstream operation, pervaporation was efficient for recovering and concentrating the natural fruity aroma. The obtained product was colorless and had a characteristic banana flavor.

  19. Antifungal activity of diethyldithiocarbamate.

    Science.gov (United States)

    Allerberger, F; Reisinger, E C; Söldner, B; Dierich, M P

    1989-10-01

    Sodium diethyldithiocarbamate (DTC) was evaluated for its ability to combat four different species of fungi in vitro. Using a microtiter-broth-dilution method we were able to demonstrate an antifungal activity against Candida albicans, Cryptococcus neoformans, Aspergillus fumigatus and Mucor mucedo in doses achievable by intravenous administration in man.

  20. Identification of the toxic compounds produced by Sargassum thunbergii to red tide microalgae

    Institute of Scientific and Technical Information of China (English)

    WANG Renjun; WANG You; TANG Xuexi

    2012-01-01

    The inhibitory effects of methanol extracts from the tissues of three macroalgal species on the growths of three marine red tide microalgae were assessed under laboratory conditions.Extracts of Sargassum thunbergii(Mertens ex Roth)Kuntz tissue had stronger inhibitory effects than those of either Sargassum pallidum(Turner)C.Agardh or Sargassum kjellmanianum Yendo on the growths of Heterosigrna akashiwo(Hada)Hada,Skeletonema costatum(Grey.)Grey,and Prorocentrum micans Ehrenberg.Methanol extracts of S.thunbergii were further divided into petroleum ether,ethyl acetate,butanol,and distilled water phases by liquid-liquid fractionation.The petroleum ether and ethyl acetate fractions had strong algicidal effects on the microalgae.Gas chromatography-mass spectrometry analyses of these two phases identified nine fatty acids,most of which were unsaturated fatty acids.In addition,pure compounds of four of the nine unsaturated fatty acids had effective concentrations below 5 mg/L.Therefore,unsaturated fatty acids are a component of the allelochemicals in S.thunbergii tissue.

  1. Recent Advances in the Application of Metabolomics to Studies of Biogenic Volatile Organic Compounds (BVOC Produced by Plant

    Directory of Open Access Journals (Sweden)

    Yoko Iijima

    2014-08-01

    Full Text Available In many plants, biogenic volatile organic compounds (BVOCs are produced as specialized metabolites that contribute to the characteristics of each plant. The varieties and composition of BVOCs are chemically diverse by plant species and the circumstances in which the plants grow, and also influenced by herbivory damage and pathogen infection. Plant-produced BVOCs are receptive to many organisms, from microorganisms to human, as both airborne attractants and repellants. In addition, it is known that some BVOCs act as signals to prime a plant for the defense response in plant-to-plant communications. The compositional profiles of BVOCs can, thus, have profound influences in the physiological and ecological aspects of living organisms. Apart from that, some of them are commercially valuable as aroma/flavor compounds for human. Metabolomic technologies have recently revealed new insights in biological systems through metabolic dynamics. Here, the recent advances in metabolomics technologies focusing on plant-produced BVOC analyses are overviewed. Their application markedly improves our knowledge of the role of BVOCs in chemosystematics, ecological influences, and aroma research, as well as being useful to prove the biosynthetic mechanisms of BVOCs.

  2. 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.

  3. Antifungal Effect of (+-Pinoresinol Isolated from Sambucus williamsii

    Directory of Open Access Journals (Sweden)

    Bomi Hwang

    2010-05-01

    Full Text Available In this study, we investigated the antifungal activity and mechanism of action of (+-pinoresinol, a biphenolic compound isolated from the herb Sambucus williamsii,used in traditional medicine. (+-Pinoresinol displays potent antifungal properties without hemolytic effects on human erythrocytes. To understand the antifungal mechanism of (+-pinoresinol, we conducted fluorescence experiments on the human pathogen Candida albicans. Fluorescence analysis using 1,6-diphenyl-1,3,5-hexatriene (DPH indicated that the (+-pinoresinol caused damage to the fungal plasma membrane. This result was confirmed by using rhodamine-labeled giant unilamellar vesicle (GUV experiments. Therefore, the present study indicates that (+-pinoresinol possesses fungicidal activities and therapeutic potential as an antifungal agent for the treatment of fungal infectious diseases in humans.

  4. Antifungal effect of (+)-pinoresinol isolated from Sambucus williamsii.

    Science.gov (United States)

    Hwang, Bomi; Lee, Juneyoung; Liu, Qing-He; Woo, Eun-Rhan; Lee, Dong Gun

    2010-05-14

    In this study, we investigated the antifungal activity and mechanism of action of (+)-pinoresinol, a biphenolic compound isolated from the herb Sambucus williamsii,used in traditional medicine. (+)-Pinoresinol displays potent antifungal properties without hemolytic effects on human erythrocytes. To understand the antifungal mechanism of (+)-pinoresinol, we conducted fluorescence experiments on the human pathogen Candida albicans. Fluorescence analysis using 1,6-diphenyl-1,3,5-hexatriene (DPH) indicated that the (+)-pinoresinol caused damage to the fungal plasma membrane. This result was confirmed by using rhodamine-labeled giant unilamellar vesicle (GUV) experiments. Therefore, the present study indicates that (+)-pinoresinol possesses fungicidal activities and therapeutic potential as an antifungal agent for the treatment of fungal infectious diseases in humans.

  5. 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.

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

    Science.gov (United States)

    Lu, Yan-Yang; Lin, Yi; Zhang, Han; Ding, Dongxiao; Sun, Xia; Huang, Qiansheng; Lin, Lifeng; Chen, Ya-Jie; Chi, Yu-Lang; Dong, Sijun

    2016-01-01

    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. PMID:27314375

  7. Moisture resistant and anti-reflection optical coatings produced by plasma polymerization of organic compounds

    Science.gov (United States)

    Hollahan, J. R.; Wydeven, T.

    1975-01-01

    The need for protective coatings on critical optical surfaces, such as halide crystal windows or lenses used in spectroscopy, has long been recognized. It has been demonstrated that thin, one micron, organic coatings produced by polymerization of flourinated monomers in low temperature gas discharge (plasma) exhibit very high degrees of moisture resistence, e.g., hundreds of hours protection for cesium iodide vs. minutes before degradation sets in for untreated surfaces. The index of refraction of these coatings is intermediate between that of the halide substrate and air, a condition for anti-reflection, another desirable property of optical coatings. Thus, the organic coatings not only offer protection, but improved transmittance as well. The polymer coating is non-absorbing over the range 0.4 to 40 microns with an exception at 8.0 microns, the expected absorption for C-F bonds.

  8. Bioactivities of Ketones Terpenes: Antifungal Effect on F. verticillioides and Repellents to Control Insect Fungal Vector, S. zeamais

    Directory of Open Access Journals (Sweden)

    Romina P. Pizzolitto

    2015-11-01

    Full Text Available Maize is one the most important staple foods in the world. However, numerous pests, such as fungal pathogens, e.g., Fusarium verticillioides, and insects, such as Sitophlilus zeamais, attack maize grains during storage. Many F. verticillioides strains produce fumonisins, one of the most important mycotoxin that causes toxic effects on human and animal health. This situation is aggravated by the insect fungal vector, Sitophlilus zeamais, which contributes to the dispersal of fungal spores, and through feeding damage, provide entry points for fungal infections. The aim of this study was to evaluate in vitro bioassays, the antifungal activity on F. verticillioides M3125 and repellent effects against S. zeamais of ketone terpenes. In addition, we performed Quantitative structure–activity relationship (Q-SAR studies between physico-chemical properties of ketone terpenes and the antifungal effect. Thymoquinone was the most active compound against F. verticillioides (Minimum Inhibitory Concentration, MIC: 0.87 affecting the lag phase and the growth rate showing a total inhibition of growth at concentration higher than 2 mM (p < 0.05. The Q-SAR model revealed that the antifungal activity of ketone compounds is related to the electronic descriptor, Pi energy. Thymoquinone showed a strong repellent effect (−77.8 ± 8.5, p < 0.001 against S. zeamais. These findings make an important contribution to the search for new compounds to control two stored pests of maize.

  9. Antifungal activity of Terminalia superba (combretaceae

    Directory of Open Access Journals (Sweden)

    SIAKA Sohro

    2015-04-01

    Full Text Available The aim of the present study was to optimize the anticandidosic activities of Terminalia superba (TEKAM4 and the identification of major compounds present in the most active chromatographic fraction. The hydroethanolic extract TEKAM4-X0 was prepared by homogenization employing a blender. Two derivatives extracts of TEKAM4-X0 (X1-1 and X1-2 were obtained by a liquid/liquid partition of TEKAM4-X0 in a mixture of hexane and water (v/v. Three chromatographic fractions (F1, F2 and F3 from X1-2 were separated by means of Sephadex-LH20 gel filtration chromatography. All the extracts were incorporated to Sabouraud according to the agar slanted double dilution method. Ketoconazole was used as standards for antifungal assay. The entire fractions were tested on the previously prepared medium culture containing 1000 cells of C. albicans. Antifungal activity was determined by evaluating antifungal parameters values (MFC and IC50. Lastly, the structures of 2 isolated compounds were elucidated by combination of Flash chromatography and spectroscopic methods, including MS, and multiple stage RMN experiments.

  10. A direct pre-screen for marine bacteria producing compounds inhibiting quorum sensing reveals diverse planktonic bacteria that are bioactive.

    Science.gov (United States)

    Linthorne, Jamie S; Chang, Barbara J; Flematti, Gavin R; Ghisalberti, Emilio L; Sutton, David C

    2015-02-01

    A promising new strategy in antibacterial research is inhibition of the bacterial communication system termed quorum sensing. In this study, a novel and rapid pre-screening method was developed to detect the production of chemical inhibitors of this system (quorum-quenching compounds) by bacteria isolated from marine and estuarine waters. This method involves direct screening of mixed populations on an agar plate, facilitating specific isolation of bioactive colonies. The assay showed that between 4 and 46 % of culturable bacteria from various samples were bioactive, and of the 95 selectively isolated bacteria, 93.7 % inhibited Vibrio harveyi bioluminescence without inhibiting growth, indicating potential production of quorum-quenching compounds. Of the active isolates, 21 % showed further activity against quorum-sensing-regulated pigment production by Serratia marcescens. The majority of bioactive isolates were identified by 16S ribosomal DNA (rDNA) amplification and sequencing as belonging to the genera Vibrio and Pseudoalteromonas. Extracts of two strongly bioactive Pseudoalteromonas isolates (K1 and B2) were quantitatively assessed for inhibition of growth and quorum-sensing-regulated processes in V. harveyi, S. marcescens and Chromobacterium violaceum. Extracts of the isolates reduced V. harveyi bioluminescence by as much as 98 % and C. violaceum pigment production by 36 % at concentrations which had no adverse effect on growth. The activity found in the extracts indicated that the isolates may produce quorum-quenching compounds. This study further supports the suggestion that quorum quenching may be a common attribute among culturable planktonic marine and estuarine bacteria.

  11. The application of phenotypic microarray analysis to anti-fungal drug development.

    Science.gov (United States)

    Greetham, Darren; Lappin, David F; Rajendran, Ranjith; O'Donnell, Lindsay; Sherry, Leighann; Ramage, Gordon; Nile, Christopher

    2017-03-01

    Candida albicans metabolic activity in the presence and absence of acetylcholine was measured using phenotypic microarray analysis. Acetylcholine inhibited C. albicans biofilm formation by slowing metabolism independent of biofilm forming capabilities. Phenotypic microarray analysis can therefore be used for screening compound libraries for novel anti-fungal drugs and measuring antifungal resistance.

  12. Head Space Solid Phase Micro-Extraction (HS - SPME of volatile organic compounds produced by Sporidiobolus salmonicolor (CBS 2636

    Directory of Open Access Journals (Sweden)

    Eunice Valduga

    2010-12-01

    Full Text Available The aim of the present study was the assessment of volatile organic compounds produced by Sporidiobolus salmonicolor (CBS 2636 using methyl and ethyl ricinoleate, ricinoleic acid and castor oil as precursors. The analysis of the volatile organic compounds was carried out using Head Space Solid Phase Micro-Extraction (HS - SPME. Factorial experimental design was used for investigating extraction conditions, verifying stirring rate (0-400 rpm, temperature (25-60 ºC, extraction time (10-30 minutes, and sample volume (2-3 mL. The identification of volatile organic compounds was carried out by Gas Chromatography with Mass Spectrum Detector (GC/MSD. The conditions that resulted in maximum extraction were: 60 ºC, 10 minutes extraction, no stirring, sample volume of 2.0 mL, and addition of saturated KCl (1:10 v/v. In the bio-production of volatile organic compounds the effect of stirring rate (120-200 rpm, temperature (23-33 ºC, pH (4.0-8.0, precursor concentration (0.02-0.1%, mannitol (0-6%, and asparagine concentration (0-0.2% was investigated. The bio-production at 28 ºC, 160 rpm, pH 6,0 and with the addition of 0.02% ricinoleic acid to the medium yielded the highest production of VOCs, identified as 1,4-butanediol, 1,2,2-trimethylciclopropilamine, beta-ionone; 2,3-butanodione, pentanal, tetradecane, 2-isononenal, 4-octen-3-one, propanoic acid, and octadecane.

  13. Antibacterial and antifungal activities of benzimidazole and benzoxazole derivatives.

    OpenAIRE

    Elnima, E I; Zubair, M U; Al-Badr, A A

    1981-01-01

    The in vitro antibacterial and antifungal activities of six benzimidazole and benzoxazole derivatives were tested against standard strains and 59 clinical isolates. Of the six compounds, only compounds II and III (both benzoxazoles) were active, whereas the rest were devoid of any activity. Considerable growth inhibition of all of the standard strains, including fungi and gram-positive and gram-negative bacteria, resulted when they were treated with these compounds. Fifty-nine clinical isolat...

  14. Characterization of Linoleate 10-Hydratase of Lactobacillus plantarum and Novel Antifungal Metabolites

    Science.gov (United States)

    Chen, Yuan Y.; Liang, Nuan Y.; Curtis, Jonathan M.; Gänzle, Michael G.

    2016-01-01

    Lactobacilli convert linoleic acid to the antifungal compound 10-hydroxy-12-octadecenoic acid (10-HOE) by linoleate 10-hydratase (10-LAH). However, the effect of this conversion on cellular membrane physiology and properties of the cell surface have not been demonstrated. Moreover, Lactobacillus plantarum produces 13-hydroxy-9-octadecenoic acid (13-HOE) in addition to 10-HOE, but the antifungal activity of 13-HOE was unknown. Phylogenetic analyses conducted in this study did not differentiate between 10-LAH and linoleate 13-hydratase (13-LAH). Thus, linoleate hydratases (LAHs) must be characterized through their differences in their activities of linoleate conversion. Four genes encoding putative LAHs from lactobacilli were cloned, heterologous expressed, purified and identified as FAD-dependent 10-LAH. The unsaturated fatty acid substrates stimulated the growth of lactobacilli. We also investigated the role of 10-LAH in ethanol tolerance, membrane fluidity and hydrophobicity of cell surfaces in lactobacilli by disruption of lah. Compared with the L. plantarum lah deficient strain, 10-LAH in wild-type strain did not exert effect on cell survival and membrane fluidity under ethanol stress, but influenced the cell surface hydrophobicity. Moreover, deletion of 10-LAH in L. plantarum facilitated purification of 13-HOE and demonstration of its antifungal activity against Penicillium roqueforti and Aspergillus niger. PMID:27757104

  15. Antifungal Constituents from the Roots of Piper dilatatum Rich.

    Directory of Open Access Journals (Sweden)

    Ruilan Alves dos Santos

    2013-01-01

    Full Text Available The compounds (+-(7S,8R-epoxy-5,6-didehydrokavain (1, flavokavain B (2, β-sitosterol (3, and stigmasterol (4 are reported here as chemical constituents of Piper dilatatum Rich. (Piperaceae. Their structures were determined on the basis of their spectroscopic data (1H and 13C NMR, MS, and IR. The antifungal activities of pyrone 1 (1 μg and chalcone 2 (100 μg were determined by means of direct bioautography against Cladosporium cladosporioides and C. sphaerospermum. Results indicate P. dilatatum as a candidate for the development of novel antifungal phytotherapic products as well as point out pyrone 1 as a promising hit compound in the quest for novel antifungal agents.

  16. Targeting efflux pumps to overcome antifungal drug resistance.

    Science.gov (United States)

    Holmes, Ann R; Cardno, Tony S; Strouse, J Jacob; Ivnitski-Steele, Irena; Keniya, Mikhail V; Lackovic, Kurt; Monk, Brian C; Sklar, Larry A; Cannon, Richard D

    2016-08-01

    Resistance to antifungal drugs is an increasingly significant clinical problem. The most common antifungal resistance encountered is efflux pump-mediated resistance of Candida species to azole drugs. One approach to overcome this resistance is to inhibit the pumps and chemosensitize resistant strains to azole drugs. Drug discovery targeting fungal efflux pumps could thus result in the development of azole-enhancing combination therapy. Heterologous expression of fungal efflux pumps in Saccharomyces cerevisiae provides a versatile system for screening for pump inhibitors. Fungal efflux pumps transport a range of xenobiotics including fluorescent compounds. This enables the use of fluorescence-based detection, as well as growth inhibition assays, in screens to discover compounds targeting efflux-mediated antifungal drug resistance. A variety of medium- and high-throughput screens have been used to identify a number of chemical entities that inhibit fungal efflux pumps.

  17. 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.

  18. 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.

  19. An expert system for process planning of sheet metal parts produced on compound die for use in stamping industries

    Indian Academy of Sciences (India)

    SACHIN SALUNKHE; DEEPAK PANGHAL; SHAILENDRA KUMAR; H M A HUSSEIN

    2016-08-01

    Process planning of sheet metal part is an important activity in the design of compound die. Traditional methods of carrying out this task are manual, tedious, time-consuming, error-prone and experiencebased. This paper describes the research work involved in the development of an expert system for process planning of sheet metal parts produced on compound die. The proposed system is organized in six modules. For development of system modules, domain knowledge acquired from various sources of knowledge acquisition is refined and then framed in form of ‘IF-Then’ variety of production rules. System modules are coded in AutoLISP language and user interface is created using visual basic (VB). The system is capable to automate various activities of process planning including blank modeling, blank nesting, determining punch force required, election of clearance between punch and die, identifying sheet metal operations, and determining proper sequence of operations for manufacturing the part. The proposed system can be implemented on a PC having VB and AutoCAD software, therefore its low cost of implementation makes it affordable even for small scale sheet metal industries.

  20. 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.

  1. Characterisation of volatile compounds produced by bacteria isolated from the spoilage flora of cold-smoked salmon.

    Science.gov (United States)

    Joffraud, J J; Leroi, F; Roy, C; Berdagué, J L

    2001-06-15

    This study investigated the volatile compounds produced by bacteria belonging to nine different bacterial groups: Lactobacillus sake, L. farciminis, L. alimentarius, Carnobacterium piscicola, Aeromonas sp., Shewanella putrefaciens, Brochothrix thermosphacta, Photobacterium phosphoreum and Enterobacteriaceae isolated from cold-smoked salmon. Each bacterial group was represented by several strains. In addition, combinations of the groups were examined as well. Sterile blocks of cold-smoked salmon were inoculated, vacuum-packed and stored at 6 degrees C. After 40 days of storage at 6 degrees C, aerobic viable count and pH were recorded, the volatile fraction of the samples was analysed by gas chromatography-mass spectrometry (GC-MS), and spoilage was assessed by sensory evaluation. Among the 81 volatile compounds identified by GC-MS, 30 appeared to be released as a result of bacterial metabolism. Some of the effects of inoculated bacterial strains on the composition of the volatile fraction seemed to be characteristic of certain bacterial species. Sensory analysis showed relationships between bacteria, the composition of the volatile fraction and the organoleptic quality of smoked salmon.

  2. Male Phyllotreta striolata (F.) produce an aggregation pheromone: identification of male-specific compounds and interaction with host plant volatiles.

    Science.gov (United States)

    Beran, Franziska; Mewis, Inga; Srinivasan, Ramasamy; Svoboda, Jiří; Vial, Christian; Mosimann, Hervé; Boland, Wilhelm; Büttner, Carmen; Ulrichs, Christian; Hansson, Bill S; Reinecke, Andreas

    2011-01-01

    The chrysomelid beetle Phyllotreta striolata is an important pest of Brassicaceae in Southeast Asia and North America. Here, we identified the aggregation pheromone of a population of P. striolata from Taiwan, and host plant volatiles that interact with the pheromone. Volatiles emitted by feeding male P. striolata attracted males and females in the field. Headspace volatile analyses revealed that six sesquiterpenes were emitted specifically by feeding males. Only one of these, however, elicited an electrophysiological response from antennae of both sexes. A number of host plant volatiles, e.g., 1-hexanol, (Z)-3-hexen-1-ol, and the glucosinolate hydrolysis products allyl isothiocyanate (AITC), 3-butenyl isothiocyanate, and 4-pentenyl isothiocyanate also elicited clear responses from the antenna. The active male-specific compound was identified as (+)-(6R,7S)-himachala-9,11-diene by chiral stationary phase gas-chromatography with coupled mass spectrometry, and by comparison with reference samples from Abies nordmanniana, which is known to produce the corresponding enantiomer. The pheromone compound was synthesized starting from (-)-α-himachalene isolated from Cedrus atlantica. Under field conditions, the activity of the synthetic pheromone required concomitant presence of the host plant volatile allyl isothiocyanate. However, both synthetic (+)-(6R,7S)-himachala-9,11-diene alone and in combination with AITC were attractive in a two-choice laboratory assay devoid of other natural olfactory stimuli. We hypothesize that P. striolata adults respond to the pheromone only if specific host volatiles are present. In the same laboratory set up, more beetles were attracted by feeding males than by the synthetic stimuli. Thus, further research will be necessary to reveal the components of a more complex blend of host or male-produced semiochemicals that might enhance trap attractiveness in the field.

  3. 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

  4. [Expression of N domain of chromogranin A in Bacillus subtilis and its antifungal activity].

    Science.gov (United States)

    Li, Rui-Fang; Lou, Jin-Xian; Zhang, Tian-Yuan

    2004-03-01

    Chromogranin A (CGA) is a soluble protein existed in most secreted cells and neurons. It was recently found that the bovine CGA N terminal region has vasoinhibitory, antibacterial and antifungal activities. Since the need for effective antifungal agents increases in parallel with the expanding number of immunocompromised patients at risk for fungal infections, it becomes imperative to find antifungal compounds with low toxicity toward mammalian cells. To study the antifungal activity of CGA N terminal region, the DNA fragment encoding for the N terminal 1-76 amino acid sequence (CGA1-76) of human CGA was amplified by PCR technique. After DNA sequence analysis, the amplified DNA fragment was cloned into the Bacillus subtilis inducible and expression vector pSBPTQ constructed in this study and the resultant plasmid pSVTQ was then transformed into triple-protease deficient Bacillus subtilis strain DB403 competent cells. The transformants was screened on LB plates containing 10 microg/mL kanamycin. The positive transformant DB403 (pSVTQ) was grown on kanmycin containing 2 x MSR medium and sucrose was added to 2% final concentration for induction after 2h cultivation. The culture supernatant was used to run SDS-PAGE. The result of SDS-PAGE showed that the CGA1-76 was expressed by sucrose induction and the expressed product secreted into the medium with a yield of 5 mg/L. The expressed product reacts specifically with mouse anti CGA47-68 monoclonal antibody. The antifungal activity of the expressed product was examined by adding the culture supernatant to the fungal spore or Candida albican suspensions at appropriate proportion and found that the recombinant human CGA1-76 produced in Bacillus subtilis inhibits the growth of Fusarium sp. Alternaria sp. and Candida albican at the concerntration of 4 micromol/L. These results demonstrate that human CGA1-76 has expressed in Bacillus subtilis and the expressed product is immunogenic and has the antifungal activity.

  5. Antifungal Activity of Lactic Acid Bacteria Strains Isolated from Natural Honey against Pathogenic Candida Species

    Science.gov (United States)

    Bulgasem, Bulgasem Y.; Lani, Mohd Nizam; Wan Yusoff, Wan Mohtar; Fnaish, Sumaya G.

    2016-01-01

    The role of lactic acid bacteria (LAB) in honey as antifungal activity has received little attention and their mechanism of inhibitory of fungi is not fully understood. In this study, LAB were isolated from honey samples from Malaysia, Libya, Saudi Arabia, and Yemen. Twenty-five isolates were confirmed LAB by catalase test and Gram staining, and were screened for antifungal activity. Four LAB showed inhibitory activity against Candida spp. using the dual agar overlay method. And they were identified as Lactobacillus plantarum HS isolated from Al-Seder honey, Lactobacillus curvatus HH isolated from Al-Hanon honey, Pediococcus acidilactici HC isolated from Tualang honey and Pediococcus pentosaceus HM isolated from Al-Maray honey by the 16S rDNA sequence. The growth of Candida glabrata ATCC 2001 was strongly inhibited (>15.0 mm) and (10~15 mm) by the isolates of L. curvatus HH and P. pentosaceus HM, respectively. The antifungal activity of the crude supernatant (cell free supernatant, CFS) was evaluated using well diffusion method. The CFS showed high antifungal activity against Candida spp. especially The CFS of L. curvatus HH was significantly (p < 0.05) inhibited growth of C. glabrata ATCC 2001, C. parapsilosis ATCC 2201, and C. tropicalis ATCC 750 with inhibitory zone 22.0, 15.6, and 14.7 mm, respectively. While CFS of P. pentosaceus HM was significantly (p < 0.05) effective against C. krusei, C. glabrata, and C. albicans with inhibition zone 17.2, 16.0, and 13.3 mm, respectively. The results indicated that LAB isolated from honey produced compounds which can be used to inhibit the growth of the pathogenic Candida species. PMID:28154488

  6. "Green preservatives": combating fungi in the food and feed industry by applying antifungal lactic acid bacteria.

    Science.gov (United States)

    Pawlowska, Agata M; Zannini, Emanuele; Coffey, Aidan; Arendt, Elke K

    2012-01-01

    Fungal food spoilage plays a pivotal role in the deterioration of food and feed systems and some of them are also able to produce toxic compounds for humans and animals. The mycotoxins produced by fungi can cause serious health hazards, including cancerogenic, immunotoxic, teratogenic, neurotoxic, nephrotoxic and hepatotoxic effects, and Kashin-Beck disease. In addition to this, fungal spoilage/pathogens are causing losses of marketable quality and hygiene of foodstuffs, resulting in major economic problem throughout the world. Nowadays, food spoilage can be prevented using physical and chemical methods, but no efficient strategy has been proposed so far to reduce the microbial growth ensuring public health. Therefore, lactic acid bacteria (LAB) can play an important role as natural preservatives. The protection of food products using LAB is mainly due to the production of antifungal compounds such as carboxylic acids, fatty acids, ethanol, carbon dioxide, hydrogen peroxide, and bacteriocins. In addition to this, LAB can also positively contribute to the flavor, texture, and nutritional value of food products. This review mainly focuses on the use of LAB for food preservation given their extensive industrial application in a wide range of foods and feeds. The attention points out the several industrial patents concerning the use of antifungal LAB as biocontrol agent against spoilage organisms in different fermented foods and feeds.

  7. New targets and delivery systems for antifungal therapy.

    Science.gov (United States)

    Walsh, T J; Viviani, M A; Arathoon, E; Chiou, C; Ghannoum, M; Groll, A H; Odds, F C

    2000-01-01

    Development of new approaches for treatment of invasive fungal infections encompasses new delivery systems for approved and investigational compounds, as well as exploiting the cell membrane, cell wall and virulence factors as putative antifungal targets. Novel delivery systems consisting of cyclodextrins, cochleates, nanoparticles/nanospheres and long circulating ('stealth') liposomes, substantially modulate the pharmacokinetics of existing compounds, and may also be useful to enhance the delivery of antifungal agents to sites of infection. Further insights into the structure-activity relationship of the antifungal triazoles that target the biosynthesis of ergosterol in the fungal cell membrane have led to the development of highly potent broad spectrum agents, including posaconazole, ravuconazole and voriconazole. Similarly, a novel generation of cell-wall active semisynthetic echinocandin 1,3 beta-glucan inhibitors (caspofungin, FK463, and VER-002) has entered clinical development. These agents have potent and broad-spectrum activity against Candida spp, and potentially useful activity against Aspergillus spp. and Pneumocystis carinii. The ongoing convergence of the fields of molecular pathogenesis, antifungal pharmacology and vaccine development will afford the opportunity to develop novel targets to complement the existing antifungal armamentarium.

  8. Antifungal activity of resveratrol against Botrytis cinerea is improved using 2-furyl derivatives.

    Directory of Open Access Journals (Sweden)

    Francesco Caruso

    Full Text Available The antifungal effect of three furyl compounds closely related to resveratrol, (E-3,4,5-trimethoxy-β-(2-furyl-styrene (1, (E-4-methoxy-β-(2-furyl-styrene (2 and (E-3,5-dimethoxy-β-(2-furyl-styrene (3 against Botrytis cinerea was analyzed. The inhibitory effect, at 100 µg ml(-1 of compounds 1, 2, 3 and resveratrol on conidia germination, was determined to be about 70%, while at the same concentration pterostilbene (a dimethoxyl derivative of resveratrol produced complete inhibition. The title compounds were more fungitoxic towards in vitro mycelial growth than resveratrol and pterostilbene. Compound 3 was the most active and a potential explanation of this feature is given using density functional theory (DFT calculations on the demethoxylation/demethylation process. Compound 3 was further evaluated for its effects on laccase production, oxygen consumption and membrane integrity of B. cinerea. An increase of the laccase activity was observed in the presence of compound 3 and, using Sytox Green nucleic acid stain, it was demonstrated that this compound altered B. cinerea membrane. Finally, compound 3 partially affected conidia respiration.

  9. Bacillus isolates from the spermosphere of peas and dwarf French beans with antifungal activity against Botrytis cinerea and Pythium species.

    Science.gov (United States)

    Walker, R; Powell, A A; Seddon, B

    1998-05-01

    A range of isolation procedures including washing, sonication and incubation in nutrient broth were used separately and in combination to obtain potential bacterial antagonists to Botrytis cinerea and Pythium mamillatum from the testae and cotyledons of peas and dwarf French beans. Heat treatment was also used to bias this selection towards spore-forming bacteria. Ninety-two bacterial isolates were obtained, 72 of which were provisionally characterized as species of Bacillus. Four of these Bacillus isolates (B3, C1, D4 and J7) displayed distinct antagonism in vitro against Botrytis cinerea and P. mamillatum when screened using dual culture analysis. Further characterization of these antagonists using API 50CHB biochemical profiling identified isolate D4 as Bacillus polymyxa and isolates B3, C1 and J7 as strains of B. subtilis. In vitro screening techniques, using cell-free and heat-killed extracts of liquid cultures against Botrytis cinerea, demonstrated the production of antifungal compounds by these four Bacillus antagonists. With each isolate the antifungal activity was found not to be either exclusively spore-bound nor released entirely into the medium but present in both fractions. The antifungal compounds produced by these isolates were shown to be heat-stable. Their identification, production and release require further study for exploitation as biocontrol systems.

  10. Antifungal therapy in European hospitals

    DEFF Research Database (Denmark)

    Zarb, P; Amadeo, B; Muller, A;

    2012-01-01

    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...

  11. 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

    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......, 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...

  12. Primary Analysis of Antifungal Proteins Produced by Bacillus amylolique faciens X-278 against Verticillium dahliae%解淀粉芽孢杆菌X-278菌株抗菌蛋白初步分析

    Institute of Scientific and Technical Information of China (English)

    黎波; 魏学军; 李亚宁; 孟庆芳; 张汀; 刘大群; 赤国彤

    2013-01-01

    为研究解淀粉芽孢杆菌X-278菌株所产抗菌蛋白的性质,通过饱和硫酸铵沉淀法提取X-278菌株蛋白粗提液,并对蛋白粗提液进行蛋白酶稳定性试验和热稳定性试验.结果表明,当硫酸铵饱和度为50%时,沉淀得到的X-278菌株蛋白粗提液对棉花黄萎病菌的押菌作用最强,抑菌圈直径迭18.9 mm.蛋白粗提液对蛋白酶K敏感性最差,对胰蛋白酶最敏感;蛋白粗提液经40℃处理后押菌活性最高,而121℃处理后抑菌活性最低,抑菌圈直径为13.6 mm,为对照(常温处理)的72%.以上结果表明,X-278菌株粗蛋白的部分抗菌成分属于耐热物质,并且抗菌成分间存在性质上的差异.%In order to study the characteristics of antifungal proteins isolated from Bacillus amyloliquefaciens X-278,crude proteins were extracted via precipitation of the cell culture of strain X-278 with ammonium sulphate,and the protease stability and thermal stability were determined.The result showed that the crude proteins of strain X-278 had strongest control effect on cotton Verticillium wilt using ammonium sulphate at 50% saturation,with the inhibition zone diameter of 18.9 mm.The crude protein extracts were relatively insensitive to proteinase K,but more sensitive to trypsin.The activity of the antifungal substrates was investigated under different temperatures,and the result showed that the antifungal activity at 40 ℃ was the highest,while it decreased most at 121 ℃ and showed significant difference from the control.However,the crude protein extracts still retained 72 % of the antifungal activity compared to the control and the diameter of inhibition zone was 13.6 mm after heat treatment for 30 min under 121 ℃.The results above indicated that part of the antifungal extracts of Bacillus amyloliquefaciens X-278 were heat-resistant substance and the antifungal extracts were several substrates with different traits.

  13. 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....

  14. 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...... by spectroscopic analyses including 2D NMR, HRMS and by comparison to literature data where available. The isolated compounds 1, 2, and 5 were antifungal against both the rust Microbotryum violaceum and Saccharomyces cerevisae....

  15. Synthesis, antibacterial and antifungal activity of some derivatives of 2-phenyl-chromen-4-one

    Indian Academy of Sciences (India)

    Sayed Alam

    2004-11-01

    Some derivatives of 2-phenyl-chromen-4-one (flavone ring) have been synthesized and tested for antibacterial and antifungal activities along with their chalcone precursors against four human pathogenic bacteria and five plant mould fungi. The structures of the synthesized compounds were elucidated by UV, IR and 1H NMR spectroscopic techniques, and elemental analysis. The antibacterial and antifungal screens of the synthesized compounds were performed in vitro by the filter paper disc diffusion method and the poisoned food technique.

  16. 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.

  17. Antifungal activity of two Lactobacillus strains with potential probiotic properties.

    Science.gov (United States)

    Gerbaldo, Gisela A; Barberis, Carla; Pascual, Liliana; Dalcero, Ana; Barberis, Lucila

    2012-07-01

    Aflatoxin (highly toxic and carcinogenic secondary metabolites produced by fungi) contamination is a serious problem worldwide. Modern agriculture and animal production systems need to use high-quality and mycotoxin-free feedstuffs. The use of microorganisms to preserve food has gained importance in recent years due to the demand for reduced use of chemical preservatives by consumers. Lactic acid bacteria are known to produce various antimicrobial compounds that are considered to be important in the biopreservation of food and feed. Lactobacillus rhamnosus L60 and Lactobacillus fermentum L23 are producers of secondary metabolites, such as organic acids, bacteriocins and, in the case of L60, hydrogen peroxide. The antifungal activity of lactobacilli strains was determined by coculture with Aspergillus section Flavi strains by two qualitative and one quantitative methods. Both L23 and L60 completely inhibited the fungal growth of all aflatoxicogenic strains assayed. Aflatoxin B (1) production was reduced 95.7-99.8% with L60 and 27.5-100% with L23. Statistical analysis of the data revealed the influence of L60 and L23 on growth parameters and aflatoxin B (1) production. These results are important given that these aflatoxicogenic fungi are natural contaminants of feed used for animal production, and could be effectively controlled by Lactobacillus L60 and L23 strains with probiotic properties.

  18. Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis

    Science.gov (United States)

    Scorzoni, Liliana; de Paula e Silva, Ana C. A.; Marcos, Caroline M.; Assato, Patrícia A.; de Melo, Wanessa C. M. A.; de Oliveira, Haroldo C.; Costa-Orlandi, Caroline B.; Mendes-Giannini, Maria J. S.; Fusco-Almeida, Ana M.

    2017-01-01

    The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins and biofilm formation, emphasizing the importance of understanding these mechanisms. To address these problems, different approaches to preventing and treating fungal diseases are described in this review, with a focus on the resistance mechanisms of fungi, with the goal of developing efficient strategies to overcoming and preventing resistance as well as new advances in antifungal therapy. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, and the synergistic effect obtained by the combination of antifungals contributes to reducing toxicity and could be an alternative for treatment. Another important issue is the development of new formulations for antifungal agents, and interest in nanoparticles as new types of carriers of antifungal drugs has increased. In addition, modifications to the chemical structures of traditional antifungals have improved their activity and pharmacokinetic parameters. Moreover, a different approach to preventing and treating fungal diseases is immunotherapy, which involves different mechanisms, such as vaccines, activation of the immune response and inducing the production of host antimicrobial molecules. Finally, the use of a mini-host has been encouraging for in vivo testing because these animal models demonstrate a good correlation with the mammalian model; they also increase the speediness of as well as facilitate the

  19. Antifungal Therapy: New Advances in the Understanding and Treatment of Mycosis.

    Science.gov (United States)

    Scorzoni, Liliana; de Paula E Silva, Ana C A; Marcos, Caroline M; Assato, Patrícia A; de Melo, Wanessa C M A; de Oliveira, Haroldo C; Costa-Orlandi, Caroline B; Mendes-Giannini, Maria J S; Fusco-Almeida, Ana M

    2017-01-01

    The high rates of morbidity and mortality caused by fungal infections are associated with the current limited antifungal arsenal and the high toxicity of the compounds. Additionally, identifying novel drug targets is challenging because there are many similarities between fungal and human cells. The most common antifungal targets include fungal RNA synthesis and cell wall and membrane components, though new antifungal targets are being investigated. Nonetheless, fungi have developed resistance mechanisms, such as overexpression of efflux pump proteins and biofilm formation, emphasizing the importance of understanding these mechanisms. To address these problems, different approaches to preventing and treating fungal diseases are described in this review, with a focus on the resistance mechanisms of fungi, with the goal of developing efficient strategies to overcoming and preventing resistance as well as new advances in antifungal therapy. Due to the limited antifungal arsenal, researchers have sought to improve treatment via different approaches, and the synergistic effect obtained by the combination of antifungals contributes to reducing toxicity and could be an alternative for treatment. Another important issue is the development of new formulations for antifungal agents, and interest in nanoparticles as new types of carriers of antifungal drugs has increased. In addition, modifications to the chemical structures of traditional antifungals have improved their activity and pharmacokinetic parameters. Moreover, a different approach to preventing and treating fungal diseases is immunotherapy, which involves different mechanisms, such as vaccines, activation of the immune response and inducing the production of host antimicrobial molecules. Finally, the use of a mini-host has been encouraging for in vivo testing because these animal models demonstrate a good correlation with the mammalian model; they also increase the speediness of as well as facilitate the

  20. Antileishmanial, Antimicrobial and Antifungal Activities of Some New Aryl Azomethines

    Directory of Open Access Journals (Sweden)

    Masoom Yasinzai

    2010-01-01

    Full Text Available A series of eighteen azomethines has been synthesized by the reaction of appropriate primary aromatic amines with aryl and/or heteroaryl carboxaldehydes. The synthesized azomethines have been evaluated for their in vitro antileishmanial, antibacterial and antifungal activities. The results revealed some antifungal activity of most of the synthesized compounds, whereas the antileishmaniasis activity results highlighted that all synthesized azomethines inhibited parasite growth and most of them showed highly potent action towards Leishmania major promastigotes. No remarkable bactericidal activities were observed.

  1. Trichoharzianol, a new antifungal from Trichoderma harzianum F031.

    Science.gov (United States)

    Jeerapong, Chotika; Phupong, Worrapong; Bangrak, Phuwadol; Intana, Warin; Tuchinda, Patoomratana

    2015-04-15

    A new decalin derivative, trichoharzianol (1), together with three known compounds, eujavanicol A (2), 5-hydroxy-3-hydroxymethyl-2-methyl-7-methoxychromone (3), and 4,6-dihydroxy-5-methylphthalide (4), were isolated from Trichoderma harzianum F031. For the first time, compounds 2-4 were reported from the Trichoderma species. Their structures were characterized by spectroscopic methods. Trichoharzianol (1) showed the highest antifungal activity against Colletotrichum gloeosporioides, with a minimum inhibitory concentration (MIC) of 128 μg/mL.

  2. A single Streptomyces symbiont makes multiple antifungals to support the fungus farming ant Acromyrmex octospinosus.

    Directory of Open Access Journals (Sweden)

    Ryan F Seipke

    Full Text Available Attine ants are dependent on a cultivated fungus for food and use antibiotics produced by symbiotic Actinobacteria as weedkillers in their fungus gardens. Actinobacterial species belonging to the genera Pseudonocardia, Streptomyces and Amycolatopsis have been isolated from attine ant nests and shown to confer protection against a range of microfungal weeds. In previous work on the higher attine Acromyrmex octospinosus we isolated a Streptomyces strain that produces candicidin, consistent with another report that attine ants use Streptomyces-produced candicidin in their fungiculture. Here we report the genome analysis of this Streptomyces strain and identify multiple antibiotic biosynthetic pathways. We demonstrate, using gene disruptions and mass spectrometry, that this single strain has the capacity to make candicidin and multiple antimycin compounds. Although antimycins have been known for >60 years we report the sequence of the biosynthetic gene cluster for the first time. Crucially, disrupting the candicidin and antimycin gene clusters in the same strain had no effect on bioactivity against a co-evolved nest pathogen called Escovopsis that has been identified in ∼30% of attine ant nests. Since the Streptomyces strain has strong bioactivity against Escovopsis we conclude that it must make additional antifungal(s to inhibit Escovopsis. However, candicidin and antimycins likely offer protection against other microfungal weeds that infect the attine fungal gardens. Thus, we propose that the selection of this biosynthetically prolific strain from the natural environment provides A. octospinosus with broad spectrum activity against Escovopsis and other microfungal weeds.

  3. A single Streptomyces symbiont makes multiple antifungals to support the fungus farming ant Acromyrmex octospinosus.

    Science.gov (United States)

    Seipke, Ryan F; Barke, Jörg; Brearley, Charles; Hill, Lionel; Yu, Douglas W; Goss, Rebecca J M; Hutchings, Matthew I

    2011-01-01

    Attine ants are dependent on a cultivated fungus for food and use antibiotics produced by symbiotic Actinobacteria as weedkillers in their fungus gardens. Actinobacterial species belonging to the genera Pseudonocardia, Streptomyces and Amycolatopsis have been isolated from attine ant nests and shown to confer protection against a range of microfungal weeds. In previous work on the higher attine Acromyrmex octospinosus we isolated a Streptomyces strain that produces candicidin, consistent with another report that attine ants use Streptomyces-produced candicidin in their fungiculture. Here we report the genome analysis of this Streptomyces strain and identify multiple antibiotic biosynthetic pathways. We demonstrate, using gene disruptions and mass spectrometry, that this single strain has the capacity to make candicidin and multiple antimycin compounds. Although antimycins have been known for >60 years we report the sequence of the biosynthetic gene cluster for the first time. Crucially, disrupting the candicidin and antimycin gene clusters in the same strain had no effect on bioactivity against a co-evolved nest pathogen called Escovopsis that has been identified in ∼30% of attine ant nests. Since the Streptomyces strain has strong bioactivity against Escovopsis we conclude that it must make additional antifungal(s) to inhibit Escovopsis. However, candicidin and antimycins likely offer protection against other microfungal weeds that infect the attine fungal gardens. Thus, we propose that the selection of this biosynthetically prolific strain from the natural environment provides A. octospinosus with broad spectrum activity against Escovopsis and other microfungal weeds.

  4. Suppression of bacterial wilt of tomato by bioorganic fertilizer made from the antibacterial compound producing strain Bacillus amyloliquefaciens HR62.

    Science.gov (United States)

    Huang, Jianfeng; Wei, Zhong; Tan, Shiyong; Mei, Xinlan; Shen, Qirong; Xu, Yangchun

    2014-11-05

    Ralstonia solanacearum (Smith) is an important soil-borne pathogen worldwide. We investigated the effects of a new bioorganic fertilizer, BIO62, which was made from organic fertilizer and antagonist Bacillus amyloliquefaciens HR62, on the control of bacterial wilt of tomato in greenhouse condition. The results showed that the application of BIO62 significantly decreased disease incidence by 65% and strongly reduced R. solanacearum populations both in the rhizosphere soil (8.04 log cfu g(-1) dry soil) and crown sections (5.63 log cfu g(-1) fresh plant section) at 28 days after pathogen challenge. Antibacterial compounds produced by HR62 were purified by silica gel, Sephadex LH-20, and HPLC and then identified using HPLC/electrospray ionization mass spectrometry analysis. Macrolactin A and 7-O-malonyl macrolactin A (molecular weights of 402 and 488 Da, respectively), along with surfactin B (molecular weights of 994, 1008, 1022, and 1036 Da), were observed to inhibit the growth of R. solanacearum.

  5. Giant dipole resonance built on hot rotating nuclei produced during evaporation of light particles from the 88Mo compound nucleus

    Science.gov (United States)

    Ciemała, M.; Kmiecik, M.; Maj, A.; Mazurek, K.; Bracco, A.; Kravchuk, V. L.; Casini, G.; Barlini, S.; Baiocco, G.; Bardelli, L.; Bednarczyk, P.; Benzoni, G.; Bini, M.; Blasi, N.; Brambilla, S.; Bruno, M.; Camera, F.; Carboni, S.; Cinausero, M.; Chbihi, A.; Chiari, M.; Corsi, A.; Crespi, F. C. L.; D'Agostino, M.; Degerlier, M.; Fornal, B.; Giaz, A.; Gramegna, F.; Krzysiek, M.; Leoni, S.; Marchi, T.; Matejska-Minda, M.; Mazumdar, I.; Meczyński, W.; Million, B.; Montanari, D.; Morelli, L.; Myalski, S.; Nannini, A.; Nicolini, R.; Pasquali, G.; Piantelli, S.; Prete, G.; Roberts, O. J.; Schmitt, Ch.; Styczeń, J.; Szpak, B.; Valdré, S.; Wasilewska, B.; Wieland, O.; Wieleczko, J. P.; Ziebliński, M.; Dudek, J.; Dinh Dang, N.

    2015-05-01

    High-energy giant dipole resonance (GDR) γ rays were measured following the decay of the hot, rotating compound nucleus of 88Mo, produced at excitation energies of 124 and 261 MeV. The reaction 48Ti + 40Ca at 300 and 600 MeV bombarding energies has been used. The data were analyzed using the statistical model Monte Carlo code gemini++. It allowed extracting the giant dipole resonance parameters by fitting the high-energy γ -ray spectra. The extracted GDR widths were compared with the available data at lower excitation energy and with theoretical predictions based on (i) The Lublin-Strasbourg drop macroscopic model, supplemented with thermal shape fluctuations analysis, and (ii) The phonon damping model. The theoretical predictions were convoluted with the population matrices of evaporated nuclei from the statistical model gemini++. Also a comparison with the results of a phenomenological expression based on the existing systematics, mainly for lower temperature data, is presented and discussed. A possible onset of a saturation of the GDR width was observed around T =3 MeV.

  6. Nanofilled and/or toughened POM composites produced by water-mediated melt compounding: Structure and mechanical properties

    Directory of Open Access Journals (Sweden)

    2008-10-01

    Full Text Available Binary and ternary composites composed of polyoxymethylene (POM, polyurethane (PU and synthetic boehmite alumina (AlO(OH were produced by water-mediated melt compounding technique. PU latex and/or aqueous alumina suspension were injected into the molten POM in a twin-screw extruder to prepare toughened and/or reinforced polymer composites. The dispersion of the alumina and PU was studied by transmission- and scanning electron microcopy techniques (TEM and SEM, respectively, and discussed. The crystallization of the POM-based systems was inspected by polarized optical microscopy (PLM. The mechanical and thermomechanical properties of the composites were determined in dynamic-mechanical thermal analysis (DMTA, short-time creep tests (performed at various temperatures, uniaxial static tensile and notched Charpy impact tests. Incorporation of alumina increased the stiffness and resistance to creep and reduced the tensile strength, elongation at break and impact toughness. The change in the above parameters was opposite for the POM/PU binary blends. Additional incorporation of alumina in the POM/PU blend enhanced the resistance to creep, elongation at break and maintained the impact toughness compared to the POM/PU blend.

  7. Self-assembled cardanol azo derivatives as antifungal agent with chitin-binding ability.

    Science.gov (United States)

    Mahata, Denial; Mandal, Santi M; Bharti, Rashmi; Gupta, Vinay Krishna; Mandal, Mahitosh; Nag, Ahindra; Nando, Golok B

    2014-08-01

    Cardanol is a non-isoprenoic phenolic lipid-mixture of distilled cashew nut shell liquid obtained from Anacardium occidentale. Herein, cardanol is purified from cashew nut shell liquid (CNSL) and synthesized to new compounds with different azo amphiphiles. These synthesized compounds are allowed to self-assembled in hydrophobic environment and checked antifungal activity against Candida albicans. Self-assembled structure of CABA showed higher antifungal activity (16μg/mL) and chitin-binding ability in comparison to CAP and CANB. Furthermore, the self-assembled azo amphiphiles are immobilized with silver ions to prepare hydrogel which showed eight folds enhanced antifungal activity. Toxicity is reduced by several folds of self-assembled or hydrogel structure in comparison to pure compounds. Thus, the self-assembled structure of amphiphiles and their hydrogels have been found to be new macromolecules of interest with potential use as antifungal drugs.

  8. Design, synthesis of novel antifungal triazole derivatives with high activities against Aspergillus fumigatus

    Institute of Scientific and Technical Information of China (English)

    Qiu Qin He; Chao Mei Liu; Ke Li; Yong Bing Cao

    2007-01-01

    Based on the active site of Aspergillusfumigatus lanosterol 14α-demethylase (AF-CYP51), novel triazole compounds were designed. Their chemical synthesis and the antifungal activities were reported. The results showed that all the target compounds exhibited excellent activities with broad spectrum; in which compounds 4, 12 and 15 showed comparable activities against A.fumigatus to the control drug itraconazole.

  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; José NEVES; 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. Novel approaches to antifungal prophylaxis.

    Science.gov (United States)

    Ostrosky-Zeichner, Luis

    2004-06-01

    Antifungal prophylaxis represents a significant advance in the management of patients at risk from fungal infections in a variety of settings. Identification of patients at the highest risk and the utilisation of safe and effective drugs maximises the benefits of prophylaxis. Situations in which antifungal prophylaxis has been shown to be useful are bone marrow transplantation, liver and lung transplantation, surgical and neonatal intensive care units, secondary prophylaxis of fungal infections associated with HIV and neutropenia associated haematological malignancies and their treatment. New antifungal agents, such as the echinocandins and the new azoles, are available and have a potential role in antifungal prophylaxis. Future studies should evaluate which strategy is more useful; prophylaxis or pre-emptive therapy.

  11. New production process of the antifungal chaetoglobosin A using cornstalks.

    Science.gov (United States)

    Jiang, Cheng; Song, Jinzhu; Zhang, Junzheng; Yang, Qian

    2017-02-04

    Chaetoglobosin A is an antibacterial compound produced by Chaetomium globosum, with potential application as a biopesticide and cancer treatment drug. The aim of this study was to evaluate the feasibility of utilizing cornstalks to produce chaetoglobosin A by C. globosum W7 in solid-batch fermentation and to determine an optimal method for purification of the products. The output of chaetoglobosin A from the cornstalks was 0.34mg/g, and its content in the crude extract was 4.80%. Purification conditions were optimized to increase the content of chaetoglobosin A in the crude extract, including the extract solvent, temperature, and pH value. The optimum process conditions were found to be acetone as the extractant, under room temperature, and at a pH value of 13. Under these conditions, a production process of the antifungal chaetoglobosin A was established, and the content reached 19.17%. Through further verification, cornstalks could replace crops for the production of chaetoglobosin A using this new production process. Moreover, the purified products showed great inhibition against Rhizoctonia solani, with chaetoglobosin A confirmed as the main effective constituent (IC50=3.88μg/mL). Collectively, these results demonstrate the feasibility of using cornstalks to synthesize chaetoglobosin A and that the production process established in this study was effective.

  12. AN OVERVIEW ON ANTIFUNGAL THERAPY

    OpenAIRE

    Karki, Nirmal K.; Ahmed, Azhar; Charde, Rita; Charde, Manoj; Gandhare, Bhushan

    2011-01-01

    The number of fungi causing systemic disease is growing and the number of systemic diseases caused by fungi is increasing. The currently available antifungal agents for the treatment of systemic mycoses include polyene antibiotics (Amphotericin B), fluoropyrimidine (Flu cytosine), and Nystatin andazole group of drugs (Ketoconazole, Fluconazole, and Itraconazole). Novel drug delivery systems for antifungal therapy, based on the type of formulation are classified as Liposomes Nanocochleates, Na...

  13. 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…

  14. Sphaeropsidones, phytotoxic dimedone methyl ethers produced by Diplodia cupressi: a structure-activity relationship study.

    Science.gov (United States)

    Evidente, Antonio; Maddau, Lucia; Scanu, Bruno; Andolfi, Anna; Masi, Marco; Motta, Andrea; Tuzi, Angela

    2011-04-25

    Sphaeropsidone and episphaeropsidone are two phytotoxic dimedone methyl ethers produced by Diplodia cupressi, the causal agent of a canker disease of cypress in the Mediterranean area. In this study, eight derivatives obtained by chemical modifications and two natural analogues were assayed for phytotoxic and antifungal activities, and a structure-activity relationship was examined. Each compound was tested on nonhost plants and on five fungal pathogenic species belonging to the genus Phytophthora. The results provide insights into structure-activity relationships within these compounds. It was found that the hydroxy group at C-5, the absolute C-5 configuration, the epoxy group, and the C-2 carbonyl group appear to be structural features important in conferring biological activity. The conversion of sphaeropsidone into the corresponding 1,4-dione derivative led to a compound showing greater antifungal activity than its precursor. This finding could be useful in devising new natural fungicides for practical application in agriculture.

  15. The ultrasound-assisted extraction and identification of antifungal substances from B. amyloliquefaciens strain NJN-6 suppressing Fusarium oxysporum.

    Science.gov (United States)

    Yuan, Jun; Raza, Waseem; Huang, Qiwei; Shen, Qirong

    2012-12-01

    The primary mechanism underlying antagonism among microorganisms is the production of antagonistic substances called antibiotics that inhibit the growth of pathogens. In this study, the antagonistic substances produced by the Bacillus amyloliquefaciens strain NJN-6 that had antifungal activity against Fusarium oxysporum were extracted and identified. The active antifungal substance was extracted from dried leavening with ultrasound-assisted extraction (UAE), using n -butanol as the extractant. HPLC/ESI-MS was performed to investigate the components of the extracts. The results of the study showed that the antimicrobial substances consisted of three homologues of the iturin A family with molecular weights of 1043, 1057 and 1071 Da and of two homologues of the fengycin family with molecular weights of 1477 and 1491 Da. The effects of ultrasonic treatment time, extraction time and extractant volume, three major methodological parameters, were also studied to determine the optimal conditions for extraction. Compared with traditional extraction techniques, UAE is a simple, cheap and environmentally friendly method that represents a new option for the isolation and identification of lipopeptides and other active compounds. These antifungal substances extracted and identified from Bacillus amyloliquefaciens NJN-6 will help us to understand its biocontrol mechanism against Fusarium oxysporum.

  16. On the Ideal Quality Control Specification of Compound Prescription -- Taking thought for the New Ingredients Produced in the Single Drugs Combining Process in Compound Prescription

    Institute of Scientific and Technical Information of China (English)

    刘建利

    2002-01-01

    @@ Effectiveness, safety and quality controllability are the three basic and most important premises for evaluating the quality of drugs. Having undergone clinical tests and been verified in thousands of years, the effectiveness and safety of compound prescription, the chief form of medication in TCM, have been proved reliable. Sometimes due to the lack of quality controllability, incorrect drug or method of preparing being used, so poor therapeutic effect can be seen, though diagnosis and prescription are correct. Quality uncontrollability is also one of the important reasons that causes difficulty for TCM preparation to enter international market. In order to ensure the effectiveness and safety of TCM compound prescription and the entering of TCM preparation into international market, strict quality control specifications should be defined. Although wide attention has been paid to this task, how to define the specifications is still under discussion.

  17. 细辛对番茄早疫病菌的抑制作用及其活性成分的分离%Antifungal activities and active compounds of the extracts from Asarum himalaicum against Alternaria solani

    Institute of Scientific and Technical Information of China (English)

    李少华

    2011-01-01

    The purpose is to explore the fungicide properties of Asarum himalaicum with active chemicals in its extract as a fungicide. The disc diffusion assay was used to test the antifungal activity of the extract of A. himalaicum against Alternaria solani and the pot experiments was used to evaluated the activities of extract. The result indicated that the crude chloroform extract of A. himalaicum had strong antifungal activity and on mycelium growth and spores germination when treated in 48 and 96 h. The EC50of mycelium growth and spores germination of Alteraria solani were 1.69 and 0.41 mg/mL respectively. The bioassay result showed that petroleum ether fraction had strong antifungal activity on inhibiting the spores germination which was 100% in 48 h but had weak inhibition ability on mycelium growth which was about 40% in 96 h. The chloroform fraction had strong inhibiting activities both on the mycelium growth and spores germination which were 72.27 % (in 96 h) and 83.42% (in 48 h), respectively. The bioassay result showed that four sub-fractions had strong antifungal activities and the inhibition rates on mycelium growth were all higher than 85% in 96 h. The results of pot tests showed that the crude extract exhibited a protective efficacy and therapeutic efficacy over than 70% against the Alternaria solani with the extract concentration at 4 mg/mL. A. himalaicum could be a potential pesticide against Alternaria solanl.%以番茄早疫病茼为供试植物病原茼,采用生物活性追踪法和活体盆栽试验法评价了细辛提取物的抑茵活性,并探索了细辛的杀菌活性成分.结果表明:细辛氯仿粗提取物在96和48 h对供试茵的菌丝生长和孢子萌发都有较强的抑制作用.其中对茵丝生长和孢子萌发的半效应浓度EC50分别为1.69和0.41 mg/mL.细辛氯仿粗提取物经萃取分离得到的石油醚、氯仿和甲醇组分中,石油醚组分对供试茵孢子萌发具有强抑制作用,处理48 h

  18. IPC synthase as a useful target for antifungal drugs.

    Science.gov (United States)

    Sugimoto, Yuichi; Sakoh, Hiroki; Yamada, Koji

    2004-12-01

    Inositol phosphorylceramide (IPC) synthase is a common and essential enzyme in fungi and plants, which catalyzes the transfer of phosphoinositol to the C-1 hydroxy of ceramide to produce IPC. This reaction is a key step in fungal sphingolipid biosynthesis, therefore the enzyme is a potential target for the development of nontoxic therapeutic antifungal agents. Natural products with a desired biological activity, aureobasidin A (AbA), khafrefungin, and galbonolide A, have been reported. AbA, a cyclic depsipeptide containing 8 amino acids and a hydroxyl acid, is a broad spectrum antifungal with strong activity against many pathogenic fungi such as Candida spp., Cryptococcus neoformans, and some Aspergillus spp. Khafrefungin, an aldonic acid ester with a C22 long alkyl chain, has antifungal activity against C. albicans, Cr. Neoformans, and Saccharomyces cerevisiae. Galbonolide A is a 14-membered macrolide with fungicidal activity against clinically important strains, and is especially potent against Cr. neoformans. These classes of natural products are potent and specific antifungal agents. We review current progress in the development of IPC synthase inhibitors with antifungal activities, and present structure-activity relationships (SAR), physicochemical and structural properties, and synthetic methodology for chemical modification.

  19. 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

    Lactic acid bacteria with antifungal properties can be used to control spoilage of food and feed. Previously, most of the identified metabolites have been isolated from cell-free fermentate of lactic acid bacteria with methods suboptimal for detecting possible contribution from volatiles...... 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...

  20. Synthesis and Biological Evaluation of Hydrazone Derivatives as Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Bruna B. Casanova

    2015-05-01

    Full Text Available Emerging yeasts are among the most prevalent causes of systemic infections with high mortality rates and there is an urgent need to develop specific, effective and non-toxic antifungal agents to respond to this issue. In this study 35 aldehydes, hydrazones and hydrazines were obtained and their antifungal activity was evaluated against Candida species (C. parapsilosis, C. tropicalis, C. krusei, C. albicans, C. glabrata and C. lusitaneae and Trichosporon asahii, in an in vitro screening. The minimum inhibitory concentrations (MICs of the active compounds in the screening was determined against 10 clinical isolates of C. parapsilosis and 10 of T. asahii. The compounds 4-pyridin-2-ylbenzaldehyde] (13a and tert-butyl-(2Z-2-(3,4,5-trihydroxybenzylidinehydrazine carboxylate (7b showed the most promising MIC values in the range of 16–32 μg/mL and 8–16 μg/mL, respectively. The compounds’ action on the stability of the cell membrane and cell wall was evaluated, which suggested the action of the compounds on the fungal cell membrane. Cell viability of leukocytes and an alkaline comet assay were performed to evaluate the cytotoxicity. Compound 13a was not cytotoxic at the active concentrations. These results support the discovery of promising candidates for the development of new antifungal agents.

  1. Antibiotics from basidiomycetes. 26. Phlebiakauranol aldehyde an antifungal and cytotoxic metabolite from Punctularia atropurpurascens.

    Science.gov (United States)

    Anke, H; Casser, I; Steglich, W; Pommer, E H

    1987-04-01

    Phlebiakauranol aldehyde and the corresponding alcohol were isolated from cultures of Punctularia atropurpurascens. The aldehyde but not the alcohol exhibited strong antifungal activity against several phytopathogens as well as antibacterial and cytotoxic activities. Two acetylated derivatives prepared from the aldehyde showed only very weak antifungal and antibacterial and moderate cytotoxic activities. We therefore assume, that the aldehyde group together with the high number of hydroxyl groups are responsible for the biological activity of the compound.

  2. Chemistry and antifungal potential of Alantolides from Inula racemosa H

    Indian Academy of Sciences (India)

    Dalvir Kataria; K K Chahal

    2013-01-01

    Alantolactone and isoalantolactone were isolated from powdered roots of Inula racemosa H. using Soxhlet extraction followed by the column chromatography. Pyrazolines of alantolactone and isoalantolactone were synthesized using diazomethane, diazoethane and diazopropane. The structure elucidation of the compounds were carried out using IR and 1H NMR spectroscopic techniques. All the compounds were screened in vitro for their antifungal potential at various concentrations against Alternaria brassicae and Penicillium italicum using spore germination inhibition technique and against Rhizoctonia solani by poisoned food technique. All the compounds exhibited fairly good fungitoxicity against the test fungi with ED50 values of less than 500 g mL-1.

  3. 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.

  4. 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.

    2009-01-01

    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 stra

  5. 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.

  6. NOVEL BIOACTIVE COMPOUNDS FROM MANGROVE DERIVED ACTINOMYCETES

    Directory of Open Access Journals (Sweden)

    Kumari Amrita

    2012-09-01

    Full Text Available Mangrove is most productive and unexplored ecosystem that approximately covers one fourth of world coastline with high diversity of thriving organism. Recently the rate of isolation of novel bioactive compounds from microorganism living in mangrove forest has tremendously increased which is reflected in significant hasten for exploration of mangrove actinomycetes. Actinomycetes are group of bacteria which are extremely interesting as active producers of many primary and secondary metabolites. Many survey reports has depicted that the biologically active compounds which have been obtained so far from microbes, 45 percent are produced by actinomycetes, 38 percent by fungi and 17 percent by unicellular bacteria. Actinomycetes from mangrove environment provide diverse and are potential rich source of antibiotics, anticancer, antifungal and antiviral agent, enzyme and enzyme inhibitor. Mangrove actinomycetes are a prolific but underexploited source for the discovery of novel secondary metabolites.

  7. 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.

  8. Treating chromoblastomycosis with systemic antifungals.

    Science.gov (United States)

    Bonifaz, Alexandro; Paredes-Solís, Vanessa; Saúl, Amado

    2004-02-01

    Chromoblastomycosis is a subcutaneous mycosis for which there is no treatment of choice but rather, several treatment options, with low cure rates and many relapses. The choice of treatment should consider several conditions, such as the causal agent (the most common one being Fonsecaea pedrosoi ), extension of the lesions, clinical topography and health status of the patient. Most oral and systemic antifungals have been used; the best results have been obtained with itraconazole and terbinafine at high doses, for a mean of 6 - 12 months. In extensive and refractory cases, chemotherapy with oral antifungals may be associated with thermotherapy (local heat and/or cryosurgery). Limited or early cases may be managed with surgical methods, always associated with oral antifungal agents. It is important to determine the in vitro sensitivity of the major causal agents to the various drugs, by estimating the minimum inhibitory concentration, as well as drug tolerability and drug interactions.

  9. ANTIFUNGAL PROPHYLAXIS IN IMMUNOCOMPROMISED PATIENTS

    Directory of Open Access Journals (Sweden)

    Lourdes Vazquez

    2016-09-01

    Full Text Available Invasive fungal infections (IFIs represent significant complications in patients with hematological malignancies. Chemoprevention of IFIs may be important in this setting, but most antifungal drugs have demonstrated poor efficacy, particularly in the prevention of invasive aspergillosis. Antifungal prophylaxis in hematological patients is currently regarded as the gold standard in situations with a high risk of infection, such as acute leukemia, myelodysplastic syndromes, and autologous or allogeneic hematopoietic stem cell transplantation. Over the years, various scientific societies have established a series of recommendations for antifungal prophylaxis based on prospective studies performed with different drugs. However, the prescription of each agent must be personalized, adapting its administration to the characteristics of individual patients and taking into account possible interactions with concomitant medication.

  10. 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...

  11. 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.

  12. 抗菌蛋白磷酸盐结合蛋白前体的分离及其产生菌的鉴定%Isolation of antifungal protein phosphate-binding protein precursor and identification of its producing strain

    Institute of Scientific and Technical Information of China (English)

    范丽霞; 李红兵; 宗兆锋; 辛红梅; 祁志军; 魏少鹏; 吴文君

    2012-01-01

    Guided by the results of the bioassay against Bacillus cereus, a protein that the antimicrobial activity was not reported in the literature was isolated from the fermentation broth of actinomycete GXW1 which was collected from the soil of Guangxi province by ammonium sulfate precipitation, ion-exchange chromatography, gel column chromatography and SDS-PAGE in turn. According to the analysis of protein mass spectroscopy by a BLASTn search in NCBInr database, the antifungal protein was identified as phosphate-binding protein precursor with the molecular weight of 39.18 ku. The strain GXW1 was characterized as Streptomyces rubiginosohelvolus based on the morphological characteristics, cultural characteristics, physiological and biochemical characteristics, as well as phylogenetic analysis of 16S rDNA sequence.%以抑菌活性生物测定结果为指导,采用硫酸铵沉淀、离子交换柱层析、凝胶柱层析和SDS-聚丙烯酰胺凝胶电泳等方法,从采自广西土壤的1株放线菌菌株GXW1发酵液中分离到1种未见文献报道具有抑菌活性的蛋白,经质谱鉴定并与NCBInr蛋白数据库比对,认为其应为磷酸盐结合蛋白前体(phosphate-binding protein precursor,pre-PBP),分子质量为39.18 ku.根据其形态特征、培养特征、生理生化特性及16S rDNA序列分析,将菌株GXW1归入链霉菌属,并鉴定为锈赤蜡黄链霉菌Streptomyces rubiginosohelvolus.

  13. Ultraviolet and visible complex refractive indices of secondary organic material produced by photooxidation of the aromatic compounds toluene and m-Xylene

    Directory of Open Access Journals (Sweden)

    P. F. Liu

    2014-08-01

    Full Text Available Secondary organic material (SOM produced by the oxidation of anthropogenic volatile organic compounds is light-absorbing (i.e., brown carbon. Spectral data of the optical properties, however, are scarce. The present study obtained the continuous spectra of the real and imaginary refractive indices (m = n − i k in the ultraviolet (UV-visible region using spectroscopic ellipsometry for n and UV-visible spectrometry for k. Several different types of SOM were produced in an oxidation flow reactor by photooxidation of toluene and m-xylene for variable concentrations of nitrogen oxides (NOx. The results show that the k values of the anthropogenically derived material were at least ten times greater than those of biogenically derived material. The presence of NOx produced organonitrogen compounds, such as nitro-aromatics and organonitrates, which enhanced light absorption. Compared with the SOM derived from m-xylene, the toluene-derived SOM had larger k values, as well as greater NOx induced enhancement, suggesting different brown-carbon-forming potentials of different aromatic precursor compounds. The results imply that anthropogenic SOM produced around urban environments can have an important influence in affecting ultraviolet irradiance, which might consequently influence photochemical cycles of urban pollution.

  14. 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.

  15. 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.

  16. 植物内生枯草芽孢杆菌E1R-j脂肽类化合物的分离鉴定及抑菌作用%Isolation and identification of lipopeptides produced by endophytic bacteria Bacillus subtilis E1 R-j and its anti-fungal mechanism studies

    Institute of Scientific and Technical Information of China (English)

    姬婧媛; 杨洁; 高小宁; 黄丽丽; 康振生

    2015-01-01

    The entophytic Bacillus subtilis E1R-j was isolated from wheat roots. The objective of this study was to isolate and identify the lipopeptides produced by B. subtilis strain E1R-j using acid precipitation, FPLC and MALDI-TOF/TOF-MS techniques. Four antifungal fractions, P1, P2, P3 and P4, were separated from the lipopeptides, and the P3 fraction has been shown to bear the major antifungal activity. According to the mass spectra analysis, P3 consisted of fengycins. The further experiments demonstrated that P3 was stable to high temperature, and even remained antifungal activity at 121 ℃ for 30 min. Microscope observation revealed that the P3 strongly inhibited the growth of mycelial. Furthermore, it can also cause deformities of mycelial cells, disintegration of the cell wall,the leakage of cytoplasm and so on.%植物内生枯草芽孢杆菌Bacillus subtilis菌株E1 R-j分离自小麦根部。以小麦全蚀病菌作为靶标菌,采用酸沉淀、快速蛋白液相色谱( FPLC)和基质辅助激光解吸附飞行时间质谱( MALDI-TOF/TOF-MS)技术,对该菌发酵液中的抗真菌活性物质进行分离鉴定和抑菌活性研究。结果表明:菌株E1 R-j产生的抗菌活性物质由P1、P2、P3和P44类组分组成,其中P3起主要抑菌作用。MALDI-TOF/TOF-MS分析结果显示,P3为fengycins。经试验发现,P3对温度稳定,121℃下放置30 min仍可保持抑菌活性。电子显微境观察发现,P3对小麦全蚀病菌菌丝生长有强烈的抑制作用,同时还可造成菌丝细胞畸形、细胞壁溃解、细胞质外渗等。

  17. Antifungal Activity of Essential Oil of Eucalyptus camaldulensis Dehnh. against Selected Fusarium spp.

    Science.gov (United States)

    Maina, Angeline W.; Wagacha, John M.

    2017-01-01

    The objective of this study was to evaluate the antifungal activity of essential oil (EO) of Eucalyptus camaldulensis Dehnh. against five Fusarium spp. commonly associated with maize. The essential oil had been extracted by steam distillation in a modified Clevenger-type apparatus from leaves of E. camaldulensis and their chemical composition characterized by gas chromatography mass spectrometry. Poisoned food technique was used to determine the percentage inhibition of mycelial growth, minimum inhibitory concentration, and minimum fungicidal concentration of the EO on the test pathogens. Antifungal activity of different concentrations of the EO was evaluated using disc diffusion method. The most abundant compounds identified in the EO were 1,8-cineole (16.2%), α-pinene (15.6%), α-phellandrene (10.0%), and p-cymene (8.1%). The EO produced complete mycelial growth inhibition in all the test pathogens at a concentration of 7-8 μL/mL after five days of incubation. The minimum inhibitory concentration and minimum fungicidal concentration of the EO on the test fungi were in the range of 7-8 μL/mL and 8–10 μL/mL, respectively. These findings confirm the fungicidal properties of E. camaldulensis essential oils and their potential use in the management of economically important Fusarium spp. and as possible alternatives to synthetic fungicides. PMID:28127308

  18. 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.

  19. 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.

  20. Biochemical approaches to selective antifungal activity. Focus on azole antifungals.

    Science.gov (United States)

    Vanden Bossche, H; Marichal, P; Gorrens, J; Coene, M C; Willemsens, G; Bellens, D; Roels, I; Moereels, H; Janssen, P A

    1989-01-01

    Azole antifungals (e.g. the imidazoles: miconazole, clotrimazole, bifonazole, imazalil, ketoconazole, and the triazoles: diniconazole, triadimenol, propiconazole, fluconazole and itraconazole) inhibit in fungal cells the 14 alpha-demethylation of lanosterol or 24-methylenedihydrolanosterol. The consequent inhibition of ergosterol synthesis originates from binding of the unsubstituted nitrogen (N-3 or N-4) of their imidazole or triazole moiety to the heme iron and from binding of their N-1 substituent to the apoprotein of a cytochrome P-450 (P-450(14)DM) of the endoplasmic reticulum. Great differences in both potency and selectivity are found between the different azole antifungals. For example, after 16h of growth of Candida albicans in medium supplemented with [14C]-acetate and increasing concentrations of itraconazole, 100% inhibition of ergosterol synthesis is achieved at 3 x 10(-8) M. Complete inhibition of this synthesis by fluconazole is obtained at 10(-5) M only. The agrochemical imidazole derivative, imazalil, shows high selectivity, it has almost 80 and 98 times more affinity for the Candida P-450(s) than for those of the piglet testes microsomes and bovine adrenal mitochondria, respectively. However, the topically active imidazole antifungal, bifonazole, has the highest affinity for P-450(s) of the testicular microsomes. The triazole antifungal itraconazole inhibits at 10(-5) M the P-450-dependent aromatase by 17.9, whereas 50% inhibition of this enzyme is obtained at about 7.5 x 10(-6)M of the bistriazole derivative fluconazole. The overall results show that both the affinity for the fungal P-450(14)DM and the selectivity are determined by the nitrogen heterocycle and the hydrophobic N-1 substituent of the azole antifungals. The latter has certainly a greater impact. The presence of a triazole and a long hypdrophobic nonligating portion form the basis for itraconazole's potency and selectivity.

  1. Variation in Scent Compounds of Oil-Bearing Rose (Rosa damascena Mill. Produced by Headspace Solid Phase Microextraction, Hydrodistillation and Solvent Extraction

    Directory of Open Access Journals (Sweden)

    Sabri Erbaş

    2016-03-01

    Full Text Available In this research, rose oil and rose water were hydro-distilled from the fresh oil-bearing rose flowers (Rosa damascena Mill. using Clevenger-type apparatus. Rose concretes were extracted from the fresh rose flowers by using non-polar solvents, e.g. diethyl ether, petroleum ether, cyclo-hexane, chloroform and n-hexane, and subsequently by evaporation of the solvents under vacuum. Absolutes were produced from the concretes with ethyl alcohol extraction at -20°C, leaving behind the wax and other paraffinic substances. Scent compounds of all these products detected by gas chromatography (GC-FID/GC-MS were compared with the natural scent compounds of fresh rose flower detected by using headspace solid phase microextraction (HS-SPME with carboxen/polydimethylsiloxane (CAR/PDMS fiber. A total of 46 compounds analysis were identified by HS-SPME-GC-MS in the fresh flower, and a total of 15 compounds were identified by GC-MS in the hydrodistilled rose oil. While main compounds in rose oil were geraniol (35.4%, citronellol (31.6%, and nerol (15.3%, major compound in fresh rose flower, rose water and residue water was phenylethyl alcohol (43.2, 35.6 and 98.2%, respectively. While the highest concrete yield (0.7% was obtained from diethyl ether extraction, the highest absolute yield (70.9% was obtained from the n-hexane concrete. The diethyl ether concrete gave the highest productivity of absolute, as 249.7 kg of fresh rose flowers was needed to produce 1 kg of absolute.

  2. Detection of volatile compounds produced by microbial growth in urine by selected ion flow tube mass spectrometry (SIFT-MS).

    Science.gov (United States)

    Storer, Malina K; Hibbard-Melles, Kim; Davis, Brett; Scotter, Jenny

    2011-10-01

    Selected ion flow tube-mass spectrometry has been used to measure the volatile compounds occurring in the headspace of urine samples inoculated with common urinary tract infection (UTI)-causing microbes Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Klebsiella pneumoniae, Enterococcus faecalis, or Candida albicans. This technique has the potential to offer rapid and simple diagnosis of the causative agent of UTIs.

  3. Male-produced aggregation pheromone compounds from the eggplant flea beetle (Epitrix fuscula): identification, synthesis, and field biossays.

    Science.gov (United States)

    Zilkowski, Bruce W; Bartelt, Robert J; Cossé, Allard A; Petroski, Richard J

    2006-11-01

    Volatiles from the eggplant flea beetle, Epitrix fuscula Crotch (Coleoptera: Chrysomelidae), feeding on host foliage, were investigated. Six male-specific compounds were detected and were identified through the use of mass spectrometry, nuclear magnetic resonance (NMR) spectrometry, chiral and achiral gas chromatography, high-performance liquid chromatography, electrophysiology (gas chromatography-electroantennography, GC-EAD), and microchemical tests. The two most abundant of the six compounds were (2E,4E,6Z)-2,4,6-nonatrienal (1) and (2E,4E,6E)-2,4,6-nonatrienal (2). The other four compounds, present in minor amounts, were identified as himachalene sesquiterpenes; two of these, 3 and 4, were hydrocarbons and two, 5 and 6, were alcohols. All four sesquiterpenes were previously encountered from male flea beetles of Aphthona spp. and Phyllotreta cruciferae. Synthetic 1 and 2 matched the natural products by GC retention times, mass spectra, and NMR spectra. Sesquiterpenes 3-6 similarly matched synthetic standards and natural samples from the previously studied species in all ways, including chirality. Both natural and synthetic 1 and 2 gave positive GC-EAD responses, as did sesquiterpenes 3, 5, and 6. Field trials were conducted with a mixture of 1 and 2, and the baited traps were significantly more attractive than control traps to both male and female E. fuscula. The E. fuscula pheromone has potential for monitoring or controlling these pests in eggplants.

  4. Potential allelopathic indole diketopiperazines produced by the plant endophytic Aspergillus fumigatus using the one strain-many compounds method.

    Science.gov (United States)

    Zhang, Qiang; Wang, Shi-Qiong; Tang, Hao-Yu; Li, Xiao-Jun; Zhang, Lu; Xiao, Jian; Gao, Yu-Qi; Zhang, An-Ling; Gao, Jin-Ming

    2013-11-27

    On the basis of the OSMAC (one strain-many compounds) strategy, 14 indole diketopiperazine (DKP) alkaloids, including spirotryprostatins (1-3), tryprostatins (4-6), and cyclotryprostatins (7-14), were isolated from the endophyte Aspergillus fumigatus associated with Melia azedarach L. Their structures were identified by nuclear magnetic resonance and electrospray ionization mass spectrometry data. All the indole DKPs were evaluated for plant growth regulation using the lettuce (Lactuca sativa) seedling growth bioassay, which showed the plant growth influence of the seedling. Among these compounds tested, a tryprostatin-type compound, brevianamide F (6), was identified as a new type of natural potential plant growth inhibitor with a response index (RI) higher than that of the positive control glyphosate, a broad-spectrum systemic herbicide. 6 can also inhibit turnip (Raphanus sativus) shoot and root elongation with RIs of -0.76 and -0.70, respectively, at 120 ppm, and it strongly inhibits amaranth (Amaranthus mangostanus) seedling growth with a high RI of -0.9 at 40 ppm. The structure-allelopathic activity relationship analysis of these isolated alkaloids indicates that tryprostatin-type alkaloids without the C5 prenyl and methoxy group give the most potent inhibition of seedling growth. Brevianamide F (6) could be used to develop a natural eco-friendly herbicide.

  5. A search for pure compounds suitable for use as matrix in spectroscopic studies of radiation-produced radical cations. III. A selection of compounds based on the thermochemistry of hydrogen and proton transfer reactions between neutral molecules and their cations

    Science.gov (United States)

    Van den Bosch, Ann; Ceulemans, Jan

    A systematic investigation is made of the thermochemistry of hydrogen and proton transfer between neutral molecules and their cations covering the entire organic chemistry, with the aim of selecting those compounds that are suitable for use as matrices in spectroscopic studies of radiation-produced radical cations. Compounds that are characterized by positive reaction enthalpies may be considered promising for use as matrices in such studies. Calculations are based on experimentally determined ionization energies and proton affinities and on carbon-hydrogen bond strengths that are arbitrarily taken as 418 kJ.mol -1 (100 kcal.mol -1). Effects of actual deviations from this value are considered. In the aliphatic series of compounds, reaction enthalpies depend strongly on functional groups present. Marked positive reaction enthalpies are obtained for alkenes, alkadienes, thioethers, mercaptans, iodoalkanes and tertiary amines. Non-aromatic cyclic compounds generally behave as their aliphatic counterparts. Thus, positive reaction enthalpies are generally obtained for unsaturated alicyclic hydrocarbons and cyclic thioethers. Positive reaction enthalpies are also obtained for piperidine, quinuclidine, manxine and derivatives. In the homocyclic aromatic series of compounds, reaction enthalpies are generally positive. Thus, positive reaction enthalpies are obtained for aromatic hydrocarbons, fluoro- and chlorobenzenes, aromatic amines (amino group attached directly to the ring) and halo- and methoxyanilines. In the heterocyclic aromatic series of compounds reaction enthalpies are generally negative. This is for instance the case for a large number of pyridine derivatives, di- and triazines and a number of bi- and tricyclic compounds. Positive reaction enthalpies are however obtained for furan and pyrrole.

  6. Novel whole-cell Reporter Assay for Stress-Based Classification of Antibacterial Compounds Produced by Locally Isolated Bacillus spp.

    OpenAIRE

    Nithya, Vadakedath; Halami, Prakash M.

    2012-01-01

    Reporter bacteria are beneficial for the rapid and sensitive screening of cultures producing peptide antibiotics, which can be an addition or alternative to the established antibiotics. This study was carried out to validate the usability of specific reporter strains for the target mediated identification of antibiotics produced by native Bacillus spp. isolated from different food sources. During preliminary classification, cell wall stress causing Bacillus isolates were screened by using rep...

  7. Impact of brief exposure to antifungal agents on the post-antifungal effect and hemolysin activity of oral Candida albicans

    Directory of Open Access Journals (Sweden)

    Arjuna Nishantha ELLEPOLA

    2015-08-01

    Full Text Available AbstractPost-antifungal effect (PAFE of Candida and its production of hemolysin are determinants of candidal pathogenicity. Candida albicans is the foremost aetiological agent of oral candidosis, which can be treated with polyene, azole, and echinocandin antifungals. However, once administered, the intraoral concentrations of these drugs tend to be subtherapeutic and transient due to the diluent effect of saliva and cleansing effect of the oral musculature. Hence, intra-orally, Candidamay undergo a brief exposure to antifungal drugs.Objective Therefore, the PAFE and hemolysin production of oral C. albicans isolates following brief exposure to sublethal concentrations of the foregoing antifungals were evaluated.Material and Methods A total of 50 C. albicans oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to sublethal concentrations of nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole for 60 min. Thereafter, the drugs were removed and the PAFE and hemolysin production were determined by previously described turbidometric and plate assays, respectively.Results Nystatin, amphotericin B, caspofungin and ketoconazole induced mean PAFE (hours of 2.2, 2.18, 2.2 and 0.62, respectively. Fluconazole failed to produce a PAFE. Hemolysin production of these isolates was suppressed with a percentage reduction of 12.27, 13.47, 13.33, 8.53 and 4.93 following exposure to nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole, respectively.Conclusions Brief exposure to sublethal concentrations of antifungal drugs appears to exert an antifungal effect by interfering with the growth as well as hemolysin production of C. albicans.

  8. 多粘类芽孢杆菌HY96-2产脂肽类抗真菌物质的研究%Antifungal Lipopeptide Produced by Paenibacillus polymyxa HY96-2

    Institute of Scientific and Technical Information of China (English)

    范磊; 张道敬; 刘振华; 陶黎明; 罗远婵; 魏鸿刚; 李淑兰; 李元广

    2012-01-01

    对一株已经商业化的可防治植物枯萎病的生防菌-多粘类芽孢杆菌HY96-2发酵液中抗真菌活性物质进行了分离纯化,采用酸化、正丁醇萃取、乙酸乙酯沉淀、硅胶柱层析、Sephadex LH-20柱层析、高效液相色谱( HPLC)等方法分离得到了一个抗真菌活性化合物6B,经NMR、MS、MS/MS等光谱学方法鉴定其为Fusaricidin A.琼脂扩散法抑菌试验结果表明,6B对西瓜枯萎病菌、水稻纹枯病菌、灰霉病菌等15种植物病原真菌的最小抑菌浓度为12.5 ~ 50 μg/mL.盆栽实验结果表明,6B对黄瓜灰霉病具有明显的防治效果,当6B的浓度达到250 μg/mL时,防治效果高达95%.%Isolation and purification of antifungal substance from Paenibacillus polymyxa HY96-2,a commercial biocon-trol strain used in control of fusarium wilt disease, was studied in this paper. By means of acidification,n-BuOH extraction, ethyl acetate precipitation, silica gel column chromatography, sephadex LH-20 column chromatography and HPLC preparation ,6B was isolated and purified. Its structure was elucidated as fusaricidin A by means of spectroscopic analysis including NMR,MS and ESI-MS/MS. Results of two-fold serial agar dilution method showed that the minimum inhibition concentrations of 6B against 15 phytopathogenic fungi were 12.5 -50 μg/mL. Greenhouse results showed that 6B had better control effect on Botrytis cinerea of cucumber. The control effect could reach ;5% when its concentration was set at 250 μg/mL.

  9. 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)

  10. NATURAL ANTIFUNGAL COMPOUNDS FROM Syzygium aromaticum (L.) MERR.ET PERRY%丁香[Syzygium aromaticum (L.) Merr.et Perry]挥发油中天然抗菌成分研究

    Institute of Scientific and Technical Information of China (English)

    孔秋莲; 宋义忠; 章丽丽; 陈留勇; 李清芳

    2004-01-01

    Essential oil from clove [Syzygium aromaticum (L.) Merr. Et Perry] buds was analyzed by GC-MS, and 20 components were identified. The main one was eugenol, which absolute content was 91.197mg/g. Antifungal activity assays showed that the oil and its derivant both inhibited the growth of Aspergillus niger and Penicillium expansun. The minimum inhibition concentration (MIC) of the oil was 50% for Aspergillus niger and 25% for Penicillium expansun, while that of the derivant was 25% for Aspergillus niger and 20% for Penicillium expansun. Both eugenol and its derivant also inhibited the growth of Aspergillus niger and Penicillium expansun, and the MIC of the eugenol was 1% for Aspergillus niger and 0.5% for Penicillium expansun, while that of the eugenol derivant was 5% for both Aspergillus niger and Penicillium expansun.%研究结果表明,丁香[Syzygium aromaticum (L.) Merr. et Perry]挥发油及其衍生物均可抑制黑曲霉(Aspergillus niger)和扩展青霉(Penicillium expansun)的生长,丁香挥发油对黑曲霉的最小抑菌浓度为50%,对扩展青霉的最小抑菌浓度为25%;丁香挥发油衍生物对黑曲霉的最小抑菌浓度为25%,对扩展青霉的最小抑菌浓度为20%.用GC-MS详细分析了丁香挥发油的化学成分,共鉴定了20个化合物,其中主要成分为丁香酚,含量占挥发油成分总量的68.0278%.

  11. 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.

  12. Study on Influencing Factors of the Antifungal Activity on the Main Postharvest Disease -producing Fungus of Apricot Fruit by Oligochitosan%壳寡糖对杏果实采后主要病原菌抑菌作用的研究

    Institute of Scientific and Technical Information of China (English)

    贾盼盼; 刘晓丹; 吝晨晨; 朱璇

    2012-01-01

    [目的]研究壳寡糖对引起杏果实采后病害主要病原真菌抑菌作用的影响因素.[方法]将供试菌种扩展青霉(Penicillium expansum)、胶孢链格孢(Alternaria alternata)和匍枝根霉(Rhizopus stolonifer)活化培养后接种到含有壳寡糖的PDA培养基上,观察不同分子量及不同浓度的壳寡糖对不同病原菌菌落生长的影响.[结果]壳寡糖对3种供试菌均有较好的抑制作用.不同分子量的壳寡糖抑菌效果不同,分子量5000和10000壳寡糖的抑菌率显著高于分子量3 000的壳寡糖.在供试壳寡糖浓度中,处理效果表现为剂量依赖关系,三种分子量的壳寡糖均以2.0%浓度对三种供试菌的抑菌效果最好.不同病原菌对壳寡糖的敏感性不同,供试壳寡糖对胶孢链格孢(A.alternata)和匍枝根霉(R.stolonifer)的抑制率明显高于扩展青霉(P.expansu).[结论]不同分子量的壳寡糖对病原菌的菌落生长均有较好的抑制作用,抑制作用的大小因壳寡糖分子量、浓度、病原菌的不同而有差异.%[Objective] The influencing factors of the antifungal activity on the main postharvest disease -producing fungus of apricot fruit by oligochitosan were studied. [Method] Penicillium expansum, Alternaria alternate and Rhizopus stolonifer were inoculated on the potato dextrose agar containing oligochitosan. The effects of oligochitosan of different molecular weight and concentration on the colony growth were evaluated. [Result]The results from the experiment showed that the oligochitosan had good antifungal activity on the three tested fungi strains. The antifungal activity of 10,000 Da was higher than that of the oligochitosan with molecular weight 3, 000 Da. The antifungal activity of the tested oligochitosan concentration has a concentration dependent manner. Among them, 2.0% oligochitosan was the most effective. Different strains had different sensitivities to the oligochitosan. A. Alternata and R. Stolonifer were more

  13. 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.

  14. Antifungal activity of mango peel and seed extracts against clinically pathogenic and food spoilage yeasts.

    Science.gov (United States)

    Dorta, E; González, M; Lobo, M G; Laich, F

    2015-11-26

    The antioxidant and antifungal (antiyeast) properties of mango (Mangifera indica) peel and seed by-products were investigated. Nine extracts were obtained using three cultivars and two extraction methods. Significant differences between cultivars and extraction methods were detected in their bioactive compounds and antioxidant activity. The antifungal property was determined using agar diffusion and broth micro-dilution assays against 18 yeast species of the genera Candida, Dekkera, Hanseniaspora, Lodderomyces, Metschnikowia, Pichia, Schizosaccharomyces, Saccharomycodes and Zygosaccharomyces. All mango extracts showed antifungal activity. The minimum inhibitory concentration (MIC) and the minimum fungicidal concentration (MFC) values were lower for seed than for peel extracts. MICs and MFCs ranged from values 30 mgGAE/mL, respectively. The multivariate analysis showed a relationship between antifungal activity, the capacity to inhibit lipid peroxidation and total phenol content. These properties were associated with high levels of proanthocyanidins, gallates and gallotannins in the extracts.

  15. A Copper Coordination Compound Produced by a Marine Fungus Fusarium sp. ZZF51 with Biosorption of Cu(Ⅱ) Ions

    Institute of Scientific and Technical Information of China (English)

    TAN Ni; PAN Jia-Hui; PENG Guang-Tian; MOU Cheng-Bo; TAO Yi-Wen; SHE Zhi-Gang; YANG Ze-Liang; ZHOU Shi-Ning; LIN Yong-Cheng

    2008-01-01

    A copper coordination compound ZZF51 (A) named bis(5-butyl-2-pyridinecarboxylato-N1,O2)-copper, the first time found in the nature, was isolated from a marine endophytic fungus Fusarium sp. ZZF51 from the South China Sea coast. Its structure was elucidated using spectroscopic methods and single crystal X-ray diffraction analysis.The antimicrobial cytotoxicity experiments exhibited that ZZF51(A) had mutagenicity activities against four aerobic reference strains Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Salmonella enteritidis with respective MIC values of 12.5, 25, 12.5, and 50 μg/mL. The anti-cancer tests showed that the compound had strong inhibitory activities against three human cancer lines KB, KBv200, and HepG2 with IC50 values of 3.54, 3.68 and 25.12 μg/mL respectively. In the course of investigating the source of ZZF51(A) in biomass, it was found that the output of ZZF51(A) was largely influenced by the amount of CuCl2 in the liquid medium, and the fungus (No.ZZF51) had two notable characteristics: endurance of high concentration Cu(Ⅱ) ions and biosorption of Cu(Ⅱ) ions.

  16. In Situ Visualization of the Local Photothermal Effect Produced on α-Cyclodextrin Inclusion Compound Associated with Gold Nanoparticles

    Science.gov (United States)

    Silva, Nataly; Muñoz, Camila; Diaz-Marcos, Jordi; Samitier, Josep; Yutronic, Nicolás; Kogan, Marcelo J.; Jara, Paul

    2016-04-01

    Evidence of guest migration in α-cyclodextrin-octylamine (α-CD-OA) inclusion compound (IC) generated via plasmonic heating of gold nanoparticles (AuNPs) has been studied. In this report, we demonstrate local effects generated by laser-mediated irradiation of a sample of AuNPs covered with inclusion compounds on surface-derivatized glass under liquid conditions by atomic force microscopy (AFM). Functionalized AuNPs on the glass and covered by the ICs were monitored by recording images by AFM during 5 h of irradiation, and images showed that after irradiation, a drastic decrease in the height of the AuNPs occurred. The absorption spectrum of the irradiated sample showed a hypsochromic shift from 542 to 536 nm, evidence suggesting that much of the population of nanoparticles lost all of the parts of the overlay of ICs due to the plasmonic heat generated by the irradiation. Mass spectrometry matrix-assisted laser desorption/ionization-time-of-flight (MALDI-TOF) performed on a sample containing a collection of drops obtained from the surface of the functionalized glass provided evidence that the irradiation lead to disintegration of the ICs and therefore exit of the octylamine molecule (the guest) from the cyclodextrin cavity (the matrix).

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

    Institute of Scientific and Technical Information of China (English)

    刘静; 姚建铭

    2004-01-01

    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.

  18. Production of sensory compounds by means of the yeast Dekkera bruxellensis in different nitrogen sources with the prospect of producing cachaça.

    Science.gov (United States)

    Castro Parente, Denise; Vidal, Esteban Espinosa; Leite, Fernanda Cristina Bezerra; de Barros Pita, Will; de Morais, Marcos Antonio

    2015-01-01

    The distilled spirit made from sugar cane juice, also known as cachaça, is a traditional Brazilian beverage that in recent years has increased its market share among international distilled beverages. Several volatile compounds produced by yeast cells during the fermentation process are responsible for the unique taste and aroma of this drink. The yeast Dekkera bruxellensis has acquired increasing importance in the fermented beverage production, as the different metabolites produced by this yeast may be either beneficial or harmful to the end-product. Since D. bruxellensis is often found in the fermentation processes carried out in ethanol fuel distillation in Brazil, we employed this yeast to analyse the physiological profile and production of aromatic compounds and to examine whether it is feasible to regard it as a cachaça-producing microorganism. The assays were performed on a small scale and simulated the conditions for the production of handmade cachaça. The results showed that the presence of aromatic and branched-chain amino acids in the medium has a strong influence on the metabolism and production of flavours by D. bruxellensis. The assimilation of these alternative nitrogen sources led to different fermentation yields and the production of flavouring compounds. The influence of the nitrogen source on the metabolism of fusel alcohols and esters in D. bruxellensis highlights the need for further studies of the nitrogen requirements to obtain the desired level of sensory compounds in the fermentation. Our results suggest that D. bruxellensis has the potential to play a role in the production of cachaça.

  19. Bioautography-guided isolation of antibacterial compounds of essential oils from Thai spices against histamine-producing bacteria.

    Science.gov (United States)

    Lomarat, Pattamapan; Phanthong, Phanida; Wongsariya, Karn; Chomnawang, Mullika Traidej; Bunyapraphatsara, Nuntavan

    2013-05-01

    The outbreak of histamine fish poisoning has been being an issue in food safety and international trade. The growth of contaminated bacterial species including Morganella morganii which produce histidine decarboxylase causes histamine formation in fish during storage. Histamine, the main toxin, causes mild to severe allergic reaction. At present, there is no well-established solution for histamine fish poisoning. This study was performed to determine the antibacterial activity of essential oils from Thai spices against histamine-producing bacteria. Among the essential oils tested, clove, lemongrass and sweet basil oils were found to possess the antibacterial activity. Clove oil showed the strongest inhibitory activity against Morganella morganii, followed by lemongrass and sweet basil oils. The results indicated that clove, lemongrass and sweet basil oils could be useful for the control of histamine-producing bacteria. The attempt to identify the active components using preparative TLC and GC/MS found eugenol, citral and methyl chavicol as the active components of clove, lemongrass and sweet basil oils, respectively. The information from this study would be useful in the research and development for the control of histamine-producing bacteria in fish or seafood products to reduce the incidence of histamine fish poisoning.

  20. Amphotericin B-copper(II) complex as a potential agent with higher antifungal activity against Candida albicans.

    Science.gov (United States)

    Chudzik, Barbara; Tracz, Izabela B; Czernel, Grzegorz; Fiołka, Marta J; Borsuk, Grzegorz; Gagoś, Mariusz

    2013-08-16

    Amphotericin B (AmB) is a polyene antibiotic produced by Streptomyces nodosus used for more than 50 years in the treatment of acute systemic fungal infections. It exhibits a broad spectrum of activity against fungal and protozoan pathogens with relatively rare resistance. The aim of this study was to prepare and evaluate the utility of the AmB-Cu(2+) complex as a potential compound with a high fungicidal activity at lower concentrations, compared with conventional AmB. It was hypothesized that insertion of copper ions into fungal cell membranes, together with the AmB-Cu(2+) complex bypassing the natural homeostatic mechanisms of this element, may contribute to the increased fungicidal activity of AmB. The analysis of results indicates the increased antifungal activity of the AmB-Cu(2+) complex against Candida albicans in comparison with the pure AmB and Fungizone. Additionally, it was stated that the increased antifungal activity of the AmB-Cu(2+) complex is not the sum of the toxic effects of AmB and Cu(2+) ions, but is a result of the unique structure of this compound.

  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

    2017-01-21

    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 fifty-three 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 (DPPH, FRAP 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. This article is protected by copyright. All rights reserved.

  2. Activation of Melanin Synthesis in Alternaria infectoria by Antifungal Drugs.

    Science.gov (United States)

    Fernandes, Chantal; Prados-Rosales, Rafael; Silva, Branca M A; Nakouzi-Naranjo, Antonio; Zuzarte, Mónica; Chatterjee, Subhasish; Stark, Ruth E; Casadevall, Arturo; Gonçalves, Teresa

    2015-12-28

    The importance of Alternaria species fungi to human health ranges from their role as etiological agents of serious infections with poor prognoses in immunosuppressed individuals to their association with respiratory allergic diseases. The present work focuses on Alternaria infectoria, which was used as a model organism of the genus, and was designed to unravel melanin production in response to antifungals. After we characterized the pigment produced by A. infectoria, we studied the dynamics of 1,8-dihydroxynaphthalene (DHN)-melanin production during growth, the degree of melanization in response to antifungals, and how melanization affected susceptibility to several classes of therapeutic drugs. We demonstrate that A. infectoria increased melanin deposition in cell walls in response to nikkomycin Z, caspofungin, and itraconazole but not in response to fluconazole or amphotericin B. These results indicate that A. infectoria activates DHN-melanin synthesis in response to certain antifungal drugs, possibly as a protective mechanism against these drugs. Inhibition of DHN-melanin synthesis by pyroquilon resulted in a lower minimum effective concentration (MEC) of caspofungin and enhanced morphological changes (increased hyphal balloon size), characterized by thinner and less organized A. infectoria cell walls. In summary, A. infectoria synthesizes melanin in response to certain antifungal drugs, and its susceptibility is influenced by melanization, suggesting the therapeutic potential of drug combinations that affect melanin synthesis.

  3. Endophytic fungi found in association with Bacopa monnieri as potential producers of industrial enzymes and antimicrobial bioactive compounds

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    Meenu Katoch

    2014-10-01

    Full Text Available This study aimed to screen the endophytic fungal species of ethano-medicinal plant Bacopa monnieri (L. Pennell for their ability to produce antimicrobial substances against Bacillus subtilis, Pseudomonas aeroginosa, Salmonella typhimurium, Escherichia coli, Klebsiella pneumonia, Staphylococcus aureus, and Candida albicans. Endophytes were also screened for their ability to produce amylase, cellulase, protease and lipase to evaluate their ecological role within the host plant. Twenty-six endophytes were isolated and seventeen were identified. All the isolated endophytes exhibited amylolytic activity. Lipolytic, cellulolytic, proteolytic activity was shown by 98, 28 and 31% isolates, respectively. Similarly, all the endophytes (100% exhibited significant antimicrobial activity against K. pneumonia, while seventeen endophytes (89.5% were active against S. aureus. Fourteen endophytes (78.9% showed significant antimicrobial activity against B. subtilis and C. albicans. Eleven (57.8%, nine (50%, four (21% endophytes were active against S. typhimurium, E. coli and P. aeruginosa, respectively.

  4. Phenolic compounds, organic acids and antioxidant activity of grape juices produced from new Brazilian varieties planted in the Northeast Region of Brazil.

    Science.gov (United States)

    Lima, Marcos Dos Santos; Silani, Igor de Souza Veras; Toaldo, Isabela Maia; Corrêa, Luiz Claudio; Biasoto, Aline Camarão Telles; Pereira, Giuliano Elias; Bordignon-Luiz, Marilde T; Ninow, Jorge Luiz

    2014-10-15

    The phenolic compounds, organic acids and the antioxidant activity were determined for grape juice samples from new Brazilian varieties grown in the Sub-middle São Francisco Valley in the Northeast Region of Brazil. The results showed that the Brazilian grape juices have high antioxidant activity, which was significantly correlated with the phenolic compounds catechin, epicatechin gallate, procyanidin B1, rutin, gallic acid, caffeic acid, p-coumaric acid, pelargonidin-3-glucoside, cyanidin-3-glucoside, cyaniding-3,5-diglucoside and delphinidin-3-glucoside. The produced juice samples showed higher concentrations of trans-resveratrol than those observed in juices made from different varieties of grapes from traditional growing regions. Organic acids concentrations were similar to those of juices produced from other classical varieties. It was demonstrated that it is possible to prepare juices from grapes of new varieties grown in the Northeast of Brazil containing a high content of bioactive compounds and typical characteristics of the tropical viticulture practised in the Sub-middle São Francisco Valley.

  5. Sporobacterium olearium gen. nov., sp. nov., a new methanethiol-producing bacterium that degrades aromatic compounds, isolated from an olive mill wastewater treatment digester.

    Science.gov (United States)

    Mechichi, T; Labat, M; Garcia, J L; Thomas, P; Patel, B K

    1999-10-01

    A strictly chemo-organotrophic, anaerobic bacterium was isolated from an olive mill wastewater treatment digester on syringate and designated strain SR1T. The cells were slightly curved rods, stained Gram-positive and possessed terminal spores. Strain SR1T utilized crotonate, methanol and a wide range of aromatic compounds including 3,4,5-trimethoxybenzoate (TMB), 3,4,5-trimethoxycinnamate (TMC), syringate, 3,4,5-trimethoxyphenylacetate (TMPA), 3,4,5-trimethoxyphenylpropionate (TMPP), ferulate, sinapate, vanillate, 3,4-dimethoxybenzoate, 2,3-dimethoxybenzoate, gallate, 2,4,6-trihydroxybenzoate (THB), pyrogallol, phloroglucinol and quercetin as carbon and energy sources. Acetate and butyrate were produced from aromatic compounds, methanol and crotonate whereas methanethiol (MT) was produced from methoxylated aromatic compounds and methanol. Strain SR1T had a G + C content of 38 mol% and grew optimally between 37 and 40 degrees C at pH 7.2 on a crotonate-containing medium. Phylogenetically, strain SR1T was a member of cluster XIVa of the Clostridiales group and shared a sequence similarity of 90% with Clostridum aminovalericum and Eubacterium fissicatena. Consequently, its precise neighbourliness to any one of them depended on the selection of strains of the cluster. On the basis of the phylogenetic and phenotypic evidence presented in this paper, the designation of strain SR1T as Sporobacterium olearium gen. nov., sp. nov. is proposed. The type strain is SR1T (= DSM 12504T).

  6. Design, synthesis, and antifungal activities of novel triazole derivatives containing the benzyl group.

    Science.gov (United States)

    Xu, Kehan; Huang, Lei; Xu, Zheng; Wang, Yanwei; Bai, Guojing; Wu, Qiuye; Wang, Xiaoyan; Yu, Shichong; Jiang, Yuanying

    2015-01-01

    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.

  7. Antifungal bis[bibenzyls] from the Chinese liverwort Marchantia polymorpha L.

    Science.gov (United States)

    Niu, Chong; Qu, Jian-Bo; Lou, Hong-Xiang

    2006-01-01

    Bioassay-guided separation of the antifungal constituents of the Chinese liverwort Marchantia polymorpha L. (Marchantiaceae) led to the isolation of seven bis[bibenzyl]-type macrocycles. On the basis of NMR and MS analyses, the three new compounds plagiochin E (1), 13,13'-O-isoproylidenericcardin D (4), and riccardin H (7) were identified, together with four known compounds: marchantin E (2), neomarchantin A (3), marchantin A (5), and marchantin B (6). Their antifungal activities against Candida albicans were determined by TLC bioautography.

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

    Science.gov (United States)

    Mousa, Walaa Kamel; Schwan, Adrian L; Raizada, Manish N

    2016-09-03

    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.

  9. 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.

  10. 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.

  11. 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.

  12. Medicago truncatula increases its iron-uptake mechanisms in response to volatile organic compounds produced by Sinorhizobium meliloti.

    Science.gov (United States)

    Orozco-Mosqueda, Maria del Carmen; Macías-Rodríguez, Lourdes I; Santoyo, Gustavo; Farías-Rodríguez, Rodolfo; Valencia-Cantero, Eduardo

    2013-11-01

    Medicago truncatula represents a model plant species for understanding legume-bacteria interactions. M. truncatula roots form a specific root-nodule symbiosis with the nitrogen-fixing bacterium Sinorhizobium meliloti. Symbiotic nitrogen fixation generates high iron (Fe) demands for bacterial nitrogenase holoenzyme and plant leghemoglobin proteins. Leguminous plants acquire Fe via "Strategy I," which includes mechanisms such as rhizosphere acidification and enhanced ferric reductase activity. In the present work, we analyzed the effect of S. meliloti volatile organic compounds (VOCs) on the Fe-uptake mechanisms of M. truncatula seedlings under Fe-deficient and Fe-rich conditions. Axenic cultures showed that both plant and bacterium modified VOC synthesis in the presence of the respective symbiotic partner. Importantly, in both Fe-rich and -deficient experiments, bacterial VOCs increased the generation of plant biomass, rhizosphere acidification, ferric reductase activity, and chlorophyll content in plants. On the basis of our results, we propose that M. truncatula perceives its symbiont through VOC emissions, and in response, increases Fe-uptake mechanisms to facilitate symbiosis.

  13. Cladosporium cladosporioides LPSC 1088 produces the 1,8-dihydroxynaphthalene-melanin-like compound and carries a putative pks gene.

    Science.gov (United States)

    Llorente, Carla; Bárcena, Alejandra; Vera Bahima, José; Saparrat, Mario C N; Arambarri, Angélica M; Rozas, M Fernanda; Mirífico, María V; Balatti, Pedro A

    2012-12-01

    Cladosporium cladosporioides is a dematiaceous fungus with coloured mycelia and conidia due to the presence of dark pigments. The purpose of this study was to characterize the dark pigments synthetized by Cladosporium sp. LPSC no. 1088 and also to identify the putative polyketide synthase (pks) gene that might be involved in the pigment biosynthesis. Morphological as well as molecular features like the ITS sequence confirmed that LPSC 1088 is Cladosporium cladosporioides. UV-visible, Fourier Transform Infrared (FTIR) and Electron Spin Resonance (ESR) spectroscopy analysis as well as melanin inhibitors suggest that the main dark pigment of the isolate was 1,8 dihydroxynaphthalene (DHN)-melanin-type compound. Two commercial fungicides, Difenoconazole and Chlorothalonil, inhibited fungal growth as well as increased pigmentation of the colonies suggesting that melanin might protect the fungus against chemical stress. The pigment is most probably synthetized by means of a pentaketide pathway since the sequence of a 651 bp fragment, coding for a putative polyketide synthase, is highly homologous to pks sequences from other fungi.

  14. 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.

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

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    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.

  16. Defensins: antifungal lessons from eukaryotes

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    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.

  17. 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.

  18. Exogenous glycine and serine promote growth and antifungal activity of Penicillium citrinum W1 from the south-west Indian Ocean.

    Science.gov (United States)

    Wu, Chang-wen; Zhao, Xian-liang; Wu, Xiao-jun; Wen, Chao; Li, Hui; Chen, Xin-hua; Peng, Xuan-xian

    2015-04-01

    PcPAF is a novel antifungal protein identified by our recent study, which is produced by a fungal strain Penicillium citrinum W1 isolated from a south-west Indian Ocean sediment sample. The present study identified glycine as a potential metabolite which increased the fungal growth and promoted antifungal activity. Then, GC/MS based metabolomics was used to disclose the metabolic mechanism manipulated by glycine. With the aid of unsupervised hierarchical clustering analysis and supervised orthogonal partial least-squares-discriminant analysis, the intracellular metabolite profiles were distinguished among two glycine-treated groups and control. 43 and 47 significantly varied metabolites were detected in 2.5 mM or 5 mM glycine-treated groups and involved in seven and eight pathways, respectively. Furthermore, exogenous serine, which is converted from glycine, showed the same potential as glycine did. Our findings not only identify glycine and serine as nutrients which promoted P. citrinum W1 growth and increased antifungal activity, but also highlight the way to utilize metabolomics for an understanding of metabolic mechanism manipulated by an exogenous compound.

  19. 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.

  20. Antagonism of antifungal metabolites from Streptomyces griseus H7602 against Phytophthora capsici.

    Science.gov (United States)

    Nguyen, Xuan Hoa; Naing, Kyaw Wai; Lee, Young Seong; Kim, Yong Hwan; Moon, Jae Hak; Kim, Kil Yong

    2015-01-01

    In this study, evidences for antagonism were established by production of antifungal metabolites from Streptomyces griseus H7602, which were active to inhibit mycelial growth of Phytophthora capsici in the in vitro assays. Mycelial growth and zoosporangia formation of P. capsici was strongly inhibited in the medium containing the cell free culture filtrate of S. griseus H7602. Antifungal metabolites from the cell free culture filtrate of S. griseus H7602 showed substantial antagonistic effects on P. capsici. In addition, a purified antifungal compound was separated from the antifungal metabolites of S. griseus H7602 and identified to be 1H-pyrrole-2-carboxylic acid (PCA) by spectra analyses. PCA showed strong antifungal activity and was evaluated for the first time for its antagonism against P. capsici under in vitro conditions. Minimum inhibitory concentration (MIC) value of PCA was low (4 µg ml(-1)), and the mycelial growth of P. capsici was almost inhibited at concentration of 64 µg ml(-1). This study suggests that the PCA may be useful as biofungicides against P. capsici, and the prominent antagonism of antifungal metabolites from S. griseus H7602 highlights it as a candidate for biocontrol of P. capsici.

  1. Production of peptide antifungal antibiotic and biocontrol activity of Bacillus subtilis.

    Science.gov (United States)

    Kumar, Ajay; Saini, Pragati; Shrivastava, J N

    2009-01-01

    Among different bacterial cultures, a potent Bacillus subtilis MTCC-8114 was isolated from garden soil samples which showed 16 and 14 mm inhibition zones by spot inoculation method and 24 and 22 mm inhibition zones by well agar diffusion method against test fungi i.e. Microsporum fulvum and Trichophyton species. Among four media tested, the maximum growth and antibiotic production was found in trypticase soya broth (TSB) medium at 37 degrees C, pH-7 and 48 h of incubation. The Rf value (0.64) by Thin Layer Chromatography (TLC) technique and UV and FTIR spectral data of the active antifungal compound, indicated that the isolated compound belongs to peptide antifungal antibiotic group. MIC value of antifungal antibiotic was 135 and 145 microg/ml.

  2. 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

  3. Effects of volatile organic compounds produced by Bacillus amyloliquefaciens on the growth and virulence traits of tomato bacterial wilt pathogen Ralstonia solanacearum.

    Science.gov (United States)

    Raza, Waseem; Wang, Jichen; Wu, Yuncheng; Ling, Ning; Wei, Zhong; Huang, Qiwei; Shen, Qirong

    2016-09-01

    The production of volatile organic compounds (VOCs) by microbes is an important characteristic for their selection as biocontrol agents against plant pathogens. In this study, we identified the VOCs produced by the biocontrol strain Bacillus amyloliquefaciens T-5 and evaluated their impact on the growth and virulence traits of tomato bacterial wilt pathogen Ralstonia solanacearum. The results showed that the VOCs of strain T-5 significantly inhibited the growth of R. solanacearum in agar medium and in soil. In addition, VOCs significantly inhibited the motility traits, root colonization, biofilm formation, and production of antioxidant enzymes and exopolysaccharides by R. solanacearum. However, no effect of VOCs on the production of hydrolytic enzymes by R. solanacearum was observed. The strain T-5 produced VOCs, including benzenes, ketones, aldehydes, alkanes, acids, and one furan and naphthalene compound; among those, 13 VOCs showed 1-10 % antibacterial activity against R. solanacearum in their produced amounts by T-5; however, the consortium of all VOCs produced on agar medium, in sterilized soil, and in natural soil showed 75, 62, and 85 % growth inhibition of R. solanacearum, respectively. The real-time PCR analysis further confirmed the results when the expression of different virulence- and metabolism-related genes in R. solanacearum cells was decreased after exposure to the VOCs of strain T-5. The results of this study clearly revealed the significance of VOCs in the control of plant pathogens. This information would help to better comprehend the microbial interactions mediated by VOCs in nature and to develop safer strategies to control plant disease.

  4. Antifungal activity of redox-active benzaldehydes that target cellular antioxidation

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    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

  5. Identification of urolithin a as a metabolite produced by human colon microflora from ellagic acid and related compounds.

    Science.gov (United States)

    Cerdá, Begoña; Periago, Paula; Espín, Juan Carlos; Tomás-Barberán, Francisco A

    2005-07-13

    Dietary ellagic acid and related polyphenols are metabolized in humans to dibenzopyran-6-one derivatives, and the microbial origin of these metabolites has been suggested. However, this has not been demonstrated so far. Fecal samples donated by six volunteers were incubated under anaerobic conditions, and aliquots were used to evaluate the fecal metabolism of ellagic acid, the ellagitannin punicalagin, and an ellagitannin rich extract from walnuts. The isoflavone daidzein was also incubated with the same fecal samples to follow the production of the microbial metabolites previously reported (dihydrogenistein, O-demethylangolensin, and equol) as a positive control of the system and to evaluate similarities between isoflavone and ellagic acid fecal flora metabolism. After fermentation the metabolite "urolithin A" (3,8-dihydroxy-6H-dibenzo[b,d]pyran-6-one) was produced from ellagic acid, punicalagin, and the ellagitannin extract in all the fecal cultures from different volunteers, but with very different production rates and concentrations. This large variability in the concentration of metabolite and kinetics of metabolite production is consistent with the large variability found in the excretion of these metabolites in urine in vivo after human consumption of ellagitannins, and with differences in the composition of the fecal microflora. No correlation between isoflavone and ellagic acid metabolism by fecal microflora was observed. The present study confirms the microbial origin of the recently reported in vivo generated hydroxy-6H-dibenzo[b,d]pyran-6-one derivatives in humans and is a further step in the study of the bioavailability and metabolism of ellagic acid and ellagitannins.

  6. Characterization of a biosurfactant produced by Pseudomonas cepacia CCT6659 in the presence of industrial wastes and its application in the biodegradation of hydrophobic compounds in soil.

    Science.gov (United States)

    Silva, Elias J; Rocha e Silva, Nathália Maria P; Rufino, Raquel D; Luna, Juliana M; Silva, Ricardo O; Sarubbo, Leonie A

    2014-05-01

    The bacterium Pseudomonas cepacia CCT6659 cultivated with 2% soybean waste frying oil and 2% corn steep liquor as substrates produced a biosurfactant with potential application in the bioremediation of soils. The biosurfactant was classified as an anionic biomolecule composed of 75% lipids and 25% carbohydrates. Characterization by proton nuclear magnetic resonance ((1)H and (13)C NMR) revealed the presence of carbonyl, olefinic and aliphatic groups, with typical spectra of lipids. Four sets of biodegradation experiments were carried out with soil contaminated by hydrophobic organic compounds amended with molasses in the presence of an indigenous consortium, as follows: Set 1-soil+bacterial cells; Set 2-soil+biosurfactant; Set 3-soil+bacterial cells+biosurfactant; and Set 4-soil without bacterial cells or biosurfactant (control). Significant oil biodegradation activity (83%) occurred in the first 10 days of the experiments when the biosurfactant and bacterial cells were used together (Set 3), while maximum degradation of the organic compounds (above 95%) was found in Sets 1-3 between 35 and 60 days. It is evident from the results that the biosurfactant alone and its producer species are both capable of promoting biodegradation to a large extent.

  7. 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

    2017-02-17

    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 G. excentricus and G. 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. Additionally, 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. This article is protected by copyright. All rights reserved.

  8. An endophyte of Picrorhiza kurroa Royle ex. Benth, producing menthol, phenylethyl alcohol and 3-hydroxypropionic acid, and other volatile organic compounds.

    Science.gov (United States)

    Qadri, Masroor; Deshidi, Ramesh; Shah, Bhawal Ali; Bindu, Kushal; Vishwakarma, Ram A; Riyaz-Ul-Hassan, Syed

    2015-10-01

    An endophytic fungus, PR4 was found in nature associated with the rhizome of Picrorhiza kurroa, a high altitude medicinal plant of Kashmir Himalayas. The fungus was found to inhibit the growth of several phyto-pathogens by virtue of its volatile organic compounds (VOCs). Molecular phylogeny, based on its ITS1-5.8S-ITS2 ribosomal gene sequence, revealed the identity of the fungus as Phomopsis/Diaporthe sp. This endophyte was found to produce a unique array of VOCs, particularly, menthol, phenylethyl alcohol, (+)-isomenthol, β-phellandrene, β-bisabolene, limonene, 3-pentanone and 1-pentanol. The purification of compounds from the culture broth of PR4 led to the isolation of 3-hydroxypropionic acid (3-HPA) as a major metabolite. This is the first report of a fungal culture producing a combination of biologically and industrially important metabolites—menthol, phenylethyl alcohol, and 3-HPA. The investigation into the monoterpene biosynthetic pathway of PR4 led to the partial characterization of isopiperitenone reductase (ipr) gene, which seems to be significantly distinct from the plant homologue. The biosynthesis of plant-like-metabolites, such as menthol, is of significant academic and industrial significance. This study indicates that PR4 is a potential candidate for upscaling of menthol, phenylethyl alcohol, and 3-HPA, as well as for understanding the menthol/monoterpene biosynthetic pathway in fungi.

  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. Research Antifungal Activity on Bacteriocin Produced by Lactic Acid Bacteria from Traditional Sour Cabbage%传统酸菜中具有抗真菌特性乳酸菌素的研究

    Institute of Scientific and Technical Information of China (English)

    李传娟; 双全; 栗永乐; 萨如拉; 桑木信辅; 琢田爱

    2012-01-01

    The antibacterial ability of lactic acid bacteria (LAB), which isolated from the sour cabbage juice prepared by herdsman in the east Inner Mogolia Region, were determined by Plate punch diffusion method, and the extracellulary bacteriocins of one screening strain was partial purified by gel filtration Sephadex G-15, and its biochemical characteristics were assessed in vitro. The results showed that strain S1-4 of LAB, which was screened out from 84 tested strains, had a broad spectrum antibacterial fungi property. Purified extracellulary bacteriocins from strain S1-4 was characterised as a proteinaceous substance. This bacteriocins compound, molecular mass ranged from 6.5 kDa to 8 kDa, has thermal stability and acid tolerance with an optimum antibacterial ability at pH 4.0.%通过平板打孔扩散法测定从内蒙古东部地区传统酸菜汁中分离的乳酸菌(LAB)的抑菌能力,再用葡聚糖凝胶G-15对筛选乳酸菌的胞外细菌素进行分离及特性研究。结果显示,84株供试乳酸菌中筛选出1株具有广谱抗真菌能力的乳酸菌S1-4。该乳酸菌所产生的胞外抑菌素属蛋白类物质,具有热稳定和耐酸特性,在pH4.0时抑菌效果最佳,其分子量约为6.5KDa~8kDa。

  11. 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....... factors thereby facilitating development of new protective cultures. The aim of the current thesis was to determine and study metabolites involved in antifungal activity of protective Lactobacillus paracasei and Propionibacterium freudenreichii subsp. shermanii. This involved development of a suitable...

  12. Antifungal activity of ibuprofen against aspergillus species and its interaction with common antifungal drugs

    Institute of Scientific and Technical Information of China (English)

    LI Li-juan; CHEN Wei; XU Hui; WAN Zhe; LI Ruo-yu; LIU Wei

    2010-01-01

    Background The incidence of invasive aspergillosis (IA) has increased in frequency in immunocompromised patients with a variety of diseases. The poor prognosis might be due to limited treatment option. This study aimed to evaluate antifungal activity of ibuprofen against clinical isolates of aspergillus species, as well as its interaction with azoles or with amphotericin B or with micafungin.Methods Antifungal activity of ibuprofen against 10 strains of Aspergillus fumigatus, Aspergillus flavus, and Aspergillus terreus were tested with both disk diffusion assay and standard broth microdilution method. To determine whether ibuprofen combined with itraconazole, voriconazole, amphotericin B, or micafungin had interactive effects on aspergillus spp., we used both disk diffusion assay and Chequerboard method.Results As for disk diffusion method, ibuprofen produced a zone of growth inhibition with diameters of (20.1±3.9) mm at 48 hours of incubation. As for broth microdilution method, the minimal inhibitory concentration (MIC) ranges of ibuprofen against aspergillus spp. were 1000-2000 μg/ml, and the minimal fungicidal concentration (MFC) ranges of that was 2000-8000 μg/ml. For 2 of 5 isolates, when ibuprofen combined with itraconazole or voriconazole, the zones of growth inhibition were larger than those of the individual drug. The results of Chequerboard method showed that fractional inhibitory concentration index (FICI) ranges were 1.125-2.500.Conclusions Ibuprofen is active against aspergillus spp.. And ibuprofen does not affect the in vitro activity of itraconazole, voriconazole, amphotericin B or micafungin against aspergillus spp..

  13. Synthesis, Structure-Activity Relationships (SAR and in Silico Studies of Coumarin Derivatives with Antifungal Activity

    Directory of Open Access Journals (Sweden)

    José M. Barbosa-Filho

    2013-01-01

    Full Text Available The increased incidence of opportunistic fungal infections, associated with greater resistance to the antifungal drugs currently in use has highlighted the need for new solutions. In this study twenty four coumarin derivatives were screened in vitro for antifungal activity against strains of Aspergillus. Some of the compounds exhibited significant antifungal activity with MICs values ranging between 16 and 32 µg/mL. The structure-activity relationships (SAR study demonstrated that O-substitutions are essential for antifungal activity. It also showed that the presence of a short aliphatic chain and/or electron withdrawing groups (NO2 and/or acetate favor activity. These findings were confirmed using density functional theory (DFT, when calculating the LUMO density. In Principal Component Analysis (PCA, two significant principal components (PCs explained more than 60% of the total variance. The best Partial Least Squares Regression (PLS model showed an r2 of 0.86 and q2cv of 0.64 corroborating the SAR observations as well as demonstrating a greater probe N1 interaction for active compounds. Descriptors generated by TIP correlogram demonstrated the importance of the molecular shape for antifungal activity.

  14. Eupatorium capillifolium essential oil: chemical composition antifungal activity and insecticidal activity

    Science.gov (United States)

    Natural plant extracts often contain compounds that are useful in pest management applications. The essential oil of Eupatorium capillifolium (dog-fennel) was investigated for antifungal and insecticidal activities. Essential oil obtained by hydrodistillation of aerial parts was analyzed by gas chro...

  15. Response of tomato wilt pathogen Ralstonia solanacearum to the volatile organic compounds produced by a biocontrol strain Bacillus amyloliquefaciens SQR-9.

    Science.gov (United States)

    Raza, Waseem; Ling, Ning; Yang, Liudong; Huang, Qiwei; Shen, Qirong

    2016-04-22

    It is important to study the response of plant pathogens to the antibiosis traits of biocontrol microbes to design the efficient biocontrol strategies. In this study, we evaluated the role of volatile organic compounds (VOCs) produced by a biocontrol strain Bacillus amyloliquefaciens SQR-9 on the growth and virulence traits of tomato wilt pathogen Ralstonia solanacearum (RS). The VOCs of SQR-9 significantly inhibited the growth of RS on agar medium and in soil. In addition, the VOCs significantly inhibited the motility traits, production of antioxidant enzymes and exopolysaccharides, biofilm formation and tomato root colonization by RS. The strain SQR-9 produced 22 VOCs, but only nine VOCs showed 1-11% antibacterial activity against RS in their corresponding amounts; however, the consortium of all VOCs showed 70% growth inhibition of RS. The proteomics analysis showed that the VOCs of SQR-9 downregulated RS proteins related to the antioxidant activity, virulence, carbohydrate and amino acid metabolism, protein folding and translation, while the proteins involved in the ABC transporter system, amino acid synthesis, detoxification of aldehydes and ketones, methylation, protein translation and folding, and energy transfer were upregulated. This study describes the significance and effectiveness of VOCs produced by a biocontrol strain against tomato wilt pathogen.

  16. 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)

  17. Synthesis and antifungal evaluation of imines derived from 3-Amino-2-isopropyl-3H-quinazolin-4-one

    Directory of Open Access Journals (Sweden)

    Idris Karakaya

    2013-12-01

    Full Text Available Novel Schiff bases were synthesised using 3-aminoquinazolinone (1 and a variety of aldehydes in the presence of acetic acid as solvent. Antifungal evaluation of the compounds was carried out by the agar dilution method. Among the all compounds prepared, quinazolinone itself showed the best fungiostatic activity against all filamentous fungi.

  18. Antifungal, anti-biofilm and adhesion activity of the essential oil of Myrtus communis L. against Candida species.

    Science.gov (United States)

    Cannas, Sara; Molicotti, Paola; Usai, Donatella; Maxia, Andrea; Zanetti, Stefania

    2014-01-01

    Candida species belong to the normal microbiota of the oral cavity, gastrointestinal tract and vagina. The increasing incidence of drug-resistant pathogens and the toxicity of the antifungal compounds have drawn the attention towards the antimicrobial activity of natural products, an inexpensive alternative. The aim of this work was to evaluate the adhesion activity, the biofilm formation and the action of the Myrtus communis L. essential oil (EO) on the biofilm formation towards three species isolated from clinical samples: Candida albicans, Candida parapsilosis and Candida tropicalis. Furthermore, we evaluated the antimycotic activity of the EO towards the three species, and the results were compared with the minimum inhibitory concentration of six antimycotics. The activity of the EO against C. albicans and C. parapsilosis was better than that obtained against C. tropicalis; moreover, the strains used in the assay were adhesive and biofilm producer, and the effect of myrtle EO on the biofilm formation yielded encouraging results.

  19. Antifungal effect of cumin essential oil alone and in combination with antifungal drugs

    Directory of Open Access Journals (Sweden)

    SAHADEO PATIL

    2015-05-01

    Full Text Available Abstract. Patil S, Maknikar P, Wankhade S, Ukesh C, Rai M. 2015. Antifungal effect of cumin essential oil alone and in combination with antifungal drugs. Nusantara Bioscience 7: 55-59. We report evaluation of antifungal activity of cumin seed oil and its pharmacological interactions when used in combination with some of the widely used conventional antifungal drugs using CLSI broth microdilution, agar disc diffusion and checkerboard microtitre assay against Candida. The essential oil was obtained from cumin seeds using hydrodistillation technique and was later evaluated for the presence of major chemical constituents present in it using gas chromatography and mass spectrometry (GC-MS assay. The GC-MS assay revealed the abundance of γ-terpinene (35.42% followed by p-cymene (30.72%. The agar disc diffusion assay demonstrated highly potent antifungal effect against Candida species. Moreover, the combination of cumin essential oil (CEO with conventional antifungal drugs was found to reduce the individual MIC of antifungal drug suggesting the occurrence of synergistic interactions. Therefore, the therapy involving combinations of CEO and conventional antifungal drugs can be used for reducing the toxicity induced by antifungal drugs and at the same time enhancing their antifungal efficacy in controlling the infections caused due to Candida species.

  20. Econazole nitrate-loaded MCM-41 for an antifungal topical powder formulation.

    Science.gov (United States)

    Ambrogi, Valeria; Perioli, Luana; Pagano, Cinzia; Marmottini, Fabio; Moretti, Massimo; Mizzi, Fabiola; Rossi, Carlo

    2010-11-01

    The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM-41 1/3) and the resulting inclusion compound was characterized by X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). The drug loading was confirmed by the decrease of specific surface area and pore volume between MCM-41 and the inclusion compound. Formulations containing the inclusion compound were prepared and submitted to in vitro dissolution test and in vitro antifungal activity. A remarkable dissolution rate improvement as well as a higher antifungal activity was observed for the inclusion compound if compared to a commercial product. Moisture sorption properties for MCM-41 and formulations were evaluated as well.

  1. Identification of antifungal natural products via Saccharomyces cerevisiae bioassay: insights into macrotetrolide drug spectrum, potency and mode of action.

    Science.gov (United States)

    Tebbets, Brad; Yu, Zhiguo; Stewart, Douglas; Zhao, Li-Xing; Jiang, Yi; Xu, Li-Hua; Andes, David; Shen, Ben; Klein, Bruce

    2013-04-01

    Since current antifungal drugs have not kept pace with the escalating medical demands of fungal infections, new, effective medications are required. However, antifungal drug discovery is hindered by the evolutionary similarity of mammalian and fungal cells, which results in fungal drug targets having human homologs and drug non-selectivity. The group III hybrid histidine kinases (HHKs) are an attractive drug target since they are conserved in fungi and absent in mammals. We used a Saccharomyces cerevisiae reporter strain that conditionally expresses HHK to establish a high-throughput bioassay to screen microbial extracts natural products for antifungals. We identified macrotetrolides, a group of related ionophores thought to exhibit restricted antifungal activity. In addition to confirming the use of this bioassay for the discovery of antifungal natural products, we demonstrated broader, more potent fungistatic activity of the macrotetrolides against multiple Candida spp., Cryptococcus spp., and Candida albicans in biofilms. Macrotetrolides were also active in an animal model of C. albicans biofilm, but were found to have inconsistent activity against fluconazole-resistant C. albicans, with most isolates resistant to this natural product. The macrotetrolides do not directly target HHKs, but their selective activity against S. cerevisiae grown in galactose (regardless of Drk1 expression) revealed potential new insight into the role of ion transport in the mode of action of these promising antifungal compounds. Thus, this simple, high-throughput bioassay permitted us to screen microbial extracts, identify natural products as antifungal drugs, and expand our understanding of the activity of macrotetrolides.

  2. Augmenting the Antifungal Activity of an Oxidizing Agent with Kojic Acid: Control of Penicillium Strains Infecting Crops

    Directory of Open Access Journals (Sweden)

    Jong H. Kim

    2014-11-01

    Full Text Available Oxidative treatment is one of the strategies for preventing Penicillium contamination in crops/foods. The antifungal efficacy of hydrogen peroxide (H2O2; oxidant was investigated in Penicillium strains by using kojic acid (KA as a chemosensitizing agent, which can enhance the susceptibility of pathogens to antifungal agents. Co-application of KA with H2O2 (chemosensitization resulted in the enhancement of antifungal activity of either compound, when compared to the independent application of each agent alone. Of note, heat enhanced the activity of H2O2 to a greater extent during chemosensitization, whereby the minimum inhibitory or minimum fungicidal concentrations of H2O2 was decreased up to 4 or 13 fold, respectively, at 35–45 °C (heat, when compared to that at 28 °C (normal growth temperature. However, heat didn’t increase the antifungal activity of KA, indicating specificity exists between heat and types of antifungals applied. The effect of chemosensitization was also strain-specific, where P. expansum (both parental and fludioxonil-resistant mutants or P. italicum 983 exhibited relatively higher susceptibility to the chemosensitization, comparing to other Penicillium strains tested. Collectively, chemosensitization can serve as a potent antifungal strategy to lower effective dosages of toxic antifungal substances, such as H2O2. This can lead to coincidental lowering of environmental and health risks.

  3. Antifungal activity of some metabolites of higher fungi (Basidiomycetes - an overview

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    Teresa Florianowicz

    2014-01-01

    Full Text Available A series of compounds of different chemical structures showing antifungal activity were isolated from higher fungi (Basidiomycetes fruit bodies. Among the microflora against which the examined metabolites showed effective activity, there are pathogenic organisms for people as well as for animals: Candida albicans, Candida tropicalis, Rhodotorula rubra, Aspergillus fumigatus and pathogens attacking plants: Penicillium chrysogenum, Botrytis cinerea, Alternaria solani, Fusarium culmorum, Trichoderma lignorum and Verticillium dahlae. Searching for fungal metabolites having antifungal activity creates possibilities of using them against a range of fungal pathogens of clinical, agronomic and environmental significance.

  4. Antifungal drug resistance to azoles and polyenes.

    Science.gov (United States)

    Masiá Canuto, Mar; Gutiérrez Rodero, Félix

    2002-09-01

    There is an increased awareness of the morbidity and mortality associated with fungal infections caused by resistant fungi in various groups of patients. Epidemiological studies have identified risk factors associated with antifungal drug resistance. Selection pressure due to the continuous exposure to azoles seems to have an essential role in developing resistance to fluconazole in Candida species. Haematological malignancies, especially acute leukaemia with severe and prolonged neutropenia, seem to be the main risk factors for acquiring deep-seated mycosis caused by resistant filamentous fungi, such us Fusarium species, Scedosporium prolificans, and Aspergillus terreus. The still unacceptably high mortality rate associated with some resistant mycosis indicates that alternatives to existing therapeutic options are needed. Potential measures to overcome antifungal resistance ranges from the development of new drugs with better antifungal activity to improving current therapeutic strategies with the present antifungal agents. Among the new antifungal drugs, inhibitors of beta glucan synthesis and second-generation azole and triazole derivatives have characteristics that render them potentially suitable agents against some resistant fungi. Other strategies including the use of high doses of lipid formulations of amphotericin B, combination therapy, and adjunctive immune therapy with cytokines are under investigation. In addition, antifungal control programmes to prevent extensive and inappropriate use of antifungals may be needed.

  5. Separation of antifungal chiral drugs by SFC and HPLC: a comparative study.

    Science.gov (United States)

    Bernal, J L; Toribio, L; del Nozal, M J; Nieto, E M; Montequi, M I

    2002-12-31

    The enantiomeric separation of several compounds, including an antifungal drug and several of its precursors, using HPLC and SFC is described in this work. The columns employed were based on polysaccharide derivatives and the results show that most of the separations obtained by SFC are better, in terms of high resolution and short analysis time, than those obtained by HPLC. Only one compound could not be resolved using SFC but, in this case, HPLC provided baseline resolution.

  6. Antifungal and cytotoxic substances from the stem barks of Desmos chinensis

    Institute of Scientific and Technical Information of China (English)

    Monchanok Tuntipaleepun; Suda Chakthong; Chanita Ponglimanont; Patimaporn Plodpai; Supayang P. Voravuthikunchai

    2012-01-01

    Isounonal-7-methyl ether (1) and chinendihydrochalcone (2) together with 8 known compounds were isolated from the stem barks of Desmos chinensis.Their structures were determined on the basis of spectroscopic data.Compound 2 exhibited cytotoxic activity against MOLT-3 cancer cell line (ICso 7.16 μg/mL) and antifungal activity against Pyricularia oryzae and Rhizoctonia solani with MIC values of 15.6 and 31.2 μg/mL,respectively.

  7. 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.

  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.

  9. 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.

  10. Encapsulation of Antifungals in Micelles Protects Candida albicans during Gall-Bladder Infection

    Science.gov (United States)

    Hsieh, Shih-Hung; Brunke, Sascha; Brock, Matthias

    2017-01-01

    Candida albicans is a dimorphic fungus that colonizes human mucosal surfaces with the potential to cause life-threatening invasive candidiasis. Studies on systemic candidiasis in a murine infection model using in vivo real-time bioluminescence imaging revealed persistence of C. albicans in the gall bladder under antifungal therapy. Preliminary analyses showed that bile conferred resistance against a wide variety of antifungals enabling survival in this cryptic host niche. Here, bile and its components were studied for their ability to reduce antifungal efficacy in order to elucidate the underlying mechanism of protection. While unconjugated bile salts were toxic to C. albicans, taurine, or glycine conjugated bile salts were well tolerated and protective against caspofungin and amphotericin B when exceeding their critical micellar concentration. Microarray experiments indicated that upregulation of genes generally known to mediate antifungal protection is not involved in the protection process. In contrast, rhodamine 6G and crystal violet in- and efflux experiments indicated encapsulation of antifungals in micelles, thereby reducing their bioavailability. Furthermore, farnesol sensing was abolished in the presence of conjugated bile salts trapping C. albicans cells in the hyphal morphology. This suggests that bioavailability of amphiphilic and hydrophobic compounds is reduced in the presence of bile. In contrast, small and hydrophilic molecules, such as cycloheximide, flucytosine, or sodium azide kept their antifungal properties. We therefore conclude that treatment of gall bladder and bile duct infections is hampered by the ability of bile salts to encapsulate antifungals in micelles. As a consequence, treatment of gall bladder or bile duct infections should favor the use of small hydrophilic drugs that are not solubilised in micelles. PMID:28203228

  11. 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.

    2014-01-01

    Background: 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. Materials and Methods: 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. Results: 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. Conclusions: Compounds 1 and 2 are new cyclopeptides with moderate antifungal activity being worthy of consideration for the development and research of antifungal agents. PMID:25422539

  12. Design and Synthesis of Some New 1,3,4-Thiadiazines with Coumarin Moieties and Their Antioxidative and Antifungal Activity

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    Milan Čačić

    2014-01-01

    Full Text Available A series of newly disubstituted (compounds 4a,b and trisubstituted 1,3,4-thiadiazines 5a–l with various substituents was prepared utilizing different thiosemicarbazides and 3-α-bromoacetylcoumarins as starting compounds. The structures of the synthesized 1,3,4-thiadiazines are elucidated and confirmed utilizing the corresponding analytical and spectroscopic data. All of the new thiadiazine derivatives were tested for their antioxidant activity, employing different antioxidant assays (DPPH scavenging activity, iron chelating activity, power reducing activity. Compounds 5b, 5f, 5j and 4b were proven to be the best DPPH radical scavengers, while compounds 5h and 5j have shown the best iron chelating activity. Thiadiazine derivatives were also tested on their antifungal activity against four mycotoxicogenic fungi, Aspergillus flavus, A. ochraceus, Fusarium graminearum and F. verticillioides. The best antifungal against A. flavus was proven to be compound 5e, while compounds 4a and 5c were the best antifungals on A. ochraceus, and compound 5g showed the best antifungal activity on F. verticillioides.

  13. 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

  14. Type I methionine aminopeptidase from Saccharomyces cerevisiae is a potential target for antifungal drug screening

    Institute of Scientific and Technical Information of China (English)

    Ling-ling CHEN; Jia LI; Jing-ya LI; Qun-li LUO; Wei-feng MAO; Qiang SHEN; Fa-jun NAN; Qi-zhuang YE

    2004-01-01

    AIM: To screen antifungal drug candidates using in vitro and in vivo assays based on type I methionine aminopeptidase from Saccharomyces cerevisiae (ScMetAP1). METHODS: A colorimetric assay suitable for high throughput screening (HTS) using recombinant ScMetAP1 protein expressed in Escherichia coli was established for antifungal lead discovery. A series of pyridine-2-carboxylic acid derivatives were characterized and a chemical library of 12 800 pure organic compounds was screened with the in vitro ScMetAP1 assay. Active compounds from the in vitro assay were further evaluated by a growth inhibition assay on yeast strain with deletion of ScMetAP1 gene mapl in comparison with the wild-type yeast strain and the yeast strain with deletion of type II enzyme (ScMetAP2)gene map2. RESULTS: Active ScMetAP1 inhibitors were identified from HTS. Some of the pyridine-2-carboxylic acid derivatives (compound 2 and 3) had selective inhibition of the growth of map2 deletion yeast and weak inhibition on wild-type yeast growth, while no inhibition on mapl deletion yeast. CONCLUSION: ScMetAP1 is a novel potential target for developing antifungal drugs. The in vitro and in vivo ScMetAP1 assays can serve as tools in discovering antifungal drug candidates.

  15. Antifungal quinazolinones from marine-derived Bacillus cereus and their preparation.

    Science.gov (United States)

    Xu, Zhihong; Zhang, Yapeng; Fu, Haichao; Zhong, Huimin; Hong, Kui; Zhu, Weiming

    2011-07-01

    Two new quinazolinones alkaloids, R(+)-2-(heptan-3-yl)quinazolin-4(3H)-one (1) and (2R,3'R)+(2S,3'R)-2-(heptan-3-yl)-2,3-dihydroquinazolin-4(1H)-one (2) (a pair of epimers), as well as seven known analogues, 2-methylquinazolin-4(3H)-one (3), 2-benzylquinazolin-4(3H)-one (4), cyclo-(Pro-Ile), cyclo-(Pro-Leu), cyclo-(Pro-Val), cyclo-(Pro-Phe), and cyclo-(Tyr-Pro) were isolated from the n-butyl alcohol extract of the marine-derived bacterium Bacillus cereus 041381. The new compounds were identified by spectroscopic analysis and chemical synthesis. Four optical isomers 5-8 were also synthesized. Compounds 1-8 all showed moderate antifungal activity against Candida albicans with MIC values of 1.3-15.6 μM. Compound 5 exhibits the most powerful antifungal activity, which may reveal that S-configuration and 2,3-double bond were necessary for antifungal activity, and the racemization at C-2 and C-3' reduced the antifungal activity.

  16. An antifungal protein from ginger rhizomes.

    Science.gov (United States)

    Wang, Hexiang; Ng, Tzi Bun

    2005-10-14

    There are very few reports on antifungal proteins from rhizomes and there is none from the family of Zingiberaceae. An antifungal protein with a novel N-terminal sequence was isolated from ginger rhizomes utilizing a protocol that involved ion exchange chromatography on DEAE-cellulose, affinity chromatography on Affi-gel blue gel, and fast protein liquid chromatography on Superdex 75. The protein was unadsorbed on DEAE-cellulose and adsorbed on Affi-gel blue gel. It exhibited an apparent molecular mass of 32kDa and exerted antifungal activity toward various fungi including Botrytis cinerea, Fusarium oxysporum, Mycosphaerella arachidicola, and Physalospora piricola.

  17. Design, synthesis and antifungal activity of novel triazole derivatives containing substituted 1,2,3-triazole-piperdine side chains.

    Science.gov (United States)

    Jiang, Zhigan; Gu, Julin; Wang, Chen; Wang, Shengzheng; Liu, Na; Jiang, Yan; Dong, Guoqiang; Wang, Yan; Liu, Yang; Yao, Jianzhong; Miao, Zhenyuan; Zhang, Wannian; Sheng, Chunquan

    2014-07-23

    Due to increasing incidence of invasive fungal infections and severe drug resistance to triazole antifungal agents, a series of novel antifungal triazoles with substituted triazole-piperidine side chains were designed and synthesized. Most of the target compounds showed good inhibitory activity against a variety of clinically important fungal pathogens. In particular, compounds 8t and 8v were highly active against Candida albicans and Cryptococcus neoformans with MIC values in the range of 0.125 μg/mL to 0.0125 μg/mL. They represent promising leads for the development of new generation of triazole antifungal agents. Molecular docking studies revealed that the target compounds interacted with CACYP51 mainly through hydrophobic and Van der Waals interactions.

  18. Antifungal activity of essential oil from fruits of Indian Cuminum cyminum.

    Science.gov (United States)

    Romagnoli, Carlo; Andreotti, Elisa; Maietti, Silvia; Mahendra, Rai; Mares, Donatella

    2010-07-01

    The essential oil of fruits of Cuminum cyminum L. (Apiaceae), from India, was analyzed by GC and GC-MS, and its antifungal activity was tested on dermatophytes and phytopathogens, fungi, yeasts and some new Aspergilli. The most abundant components were cumin aldehyde, pinenes, and p-cymene, and a fraction of oxygenate compounds such as alcohol and epoxides. Because of the large amount of the highly volatile components in the cumin extract, we used a modified recent technique to evaluate the antifungal activity only of the volatile parts at doses from 5 to 20 microL of pure essential oil. Antifungal testing showed that Cuminum cyminum is active in general on all fungi but in particular on the dermatophytes, where Trichophyton rubrum was the most inhibited fungus also at the lowest dose of 5 microL. Less sensitive to treatment were the phytopathogens.

  19. 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.

  20. In-vitro antibacterial, antifungal and cytotoxic activities of some coumarins and their metal complexes.

    Science.gov (United States)

    Rehman, Saeed U; Chohan, Zahid H; Gulnaz, Farzana; Supuran, Claudiu T

    2005-08-01

    A series of new antibacterial and antifungal coumarin-derived compounds and their transition metal complexes [cobalt (II), copper (II), nickel (II) and zinc (II)] have been synthesized, characterized and screened for their in vitro antibacterial activity against Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Pseudomonas aeruginosa, Salmonella typhi, Shigella dysenteriae, Bacillus cereus, Corynebacterium diphtheriae, Staphylococcus aureus and Streptococcus pyogenes bacterial strains and for in vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani, Candida glaberata. The results of these studies show the metal complexes to be more antibacterial and antifungal as compared to the uncomplexed coumarins. The brine shrimp bioassay was also carried out to study their in vitro cytotoxic properties.

  1. Correlation between the lipophilicity and antifungal activity of some benzoxazole derivatives

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    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

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    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. Preliminary phytochemical analysis, antibacterial, antifungal and anticandidal activities of successive extracts of Crossandra infundibuliformis

    Institute of Scientific and Technical Information of China (English)

    MadhumithaG; SaralAM

    2011-01-01

    Objective:To investigate the phytochemical, antibacterial, antifungal and anticandidal activity of successive extracts of Crossandra infundibuliformis (Acanthaceae) leaves. Methods:Preliminary screening on the presence of alkaloids, saponins, phytosterols, phenolic compounds, flavanoids, tannins, carbohydrates, terpenoids, oils and fats were carried out by phytochemical analysis. The antibacterial, antifungal and anticandidal activities were done by agar well diffusion technique. Results:The successive extracts have an array of chemical constituents and the MIC values of antibacterial activity ranges from 0.007 8 to 0.015 0μg/mL. In case of antifungal and anticandidal activities the MIC values were between 0.125 and 0.250μg/mL. Conclusions:These findings demonstrate that the leaf extracts of C. infundibuliformis presents excellent antimicrobial activities and thus have great potential as a source for natural health care products.

  4. 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...

  5. Antifungal Activity of Lavandula Angustifolia and Quergues Infectoria Extracts in Comparison with Nystatin on Candida Albicans

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    F. Nouri

    2016-07-01

    Full Text Available Introduction & Objective: Nowadays,herbal extracts are used to treat diseases, especially infec-tious ones. Candida albicans is the most common causes of oral opportunistic infections.In this study, antifungal effects of two herbal extracts were evaluated on an oral pathogen i.e. Candida albicans. Materials & Methods: In this descriptive- analytic study, the Department of Prosthodontics, ,Tehran University of Medical Sciences, school of Dentistry the oral samples of 25 patients with denture stomatitis were collected using sterile swabs. Then the isolated candida albicans and standard candida albicans PTCC 5027 were cultured. The antifungal effect was evaluated with disk plate method. Nystatin and methanol were used as positive and negative control groups, respectively. The power of antifungal activity was evaluated with the inhibition zone diameter of each of the extracts. At the end, the data were analyzed by ANOVA and Fried-man statistical tests. Results: Results showed that extracts of Querques infectoria had great antifungal effects. There was not statistically significant difference between nystatine and Querques infectoria extract (P>0.05 however , Querques infectoria was statistically more effective than lavender extract and nystatin showed the highest antifungal activity (P <0.001. Conclusion: This study showed that plant extracts had positive effects on Candida albicans as compared to nystatin. Thus, we hope to find new herbal medicines and compounds to treat candidiasis in the future. (Sci J Hamadan Univ Med Sci 2016; 23 (2:172-178

  6. Synthesis and antifungal activities of glycosylated derivatives of the cyclic peptide fungicide caspofungin.

    Science.gov (United States)

    Guo, Junxiang; Hu, Honggang; Zhao, Qingjie; Wang, Ting; Zou, Yan; Yu, Shichong; Wu, Qiuye; Guo, Zhongwu

    2012-08-01

    Diseases caused by systemic fungal infections have become a significant clinical problem in recent decades. A series of glycosyl derivatives of the approved cyclic peptide antifungal drug caspofungin conjugated with β-D-glucopyranose, β-D-galactopyranose, β-D-xylopyranose, β-L-rhamnopyranose, β-maltose and β-lactose units were designed, synthesized, and evaluated as new potential antifungal drugs. The compounds were obtained by coupling the corresponding glycosyl amines to the free primary amino groups of caspofungin through a bifunctional glutaryl linker. In contrast to caspofungin, these glycosylated derivatives are soluble in water, but are not hygroscopic and moreover, are more stable than caspofungin under high humidity and temperature. CD studies showed that glycosylation has very little impact on the conformation of the cyclic peptide of caspofungin. In vitro antifungal tests against seven human pathogenic fungi revealed that the caspofungin-monosaccharide conjugates, but not the disaccharide conjugates, have increased antifungal activities against the majority of tested fungus species relative to caspofungin. The β-D-glucopyranosyl derivative 2 a showed the strongest and broadest antifungal activity, providing a lead for further studies.

  7. Treatment of dermatophytosis by a new antifungal agent 'apigenin'.

    Science.gov (United States)

    Singh, Geeta; Kumar, Padma; Joshi, Suresh Chandra

    2014-08-01

    Dermatophytes are the most common causative agents of cutaneous mycosis and remain a major public health problem in spite of the availability of an increasing number of antifungal drugs. It was, therefore considered necessary to pursue the screening of different extracts (compounds) of selected traditional medicinal plants reportedly having antidermatophyte potential. The aim of this study was to isolate and identify specific compound from the most active extract (free flavonoid) of stem of Terminalia chebula of the selected plants to treat dermatophytosis induced on experimental mice. Mice which were experimentally induced with Trichophyton mentagrophytes were grouped in six of five animals each. To treat the lesions on infected mice, two concentrations of isolated apigenin ointment, i.e. 2.5 mg g(-1) (Api I) and 5 mg g(-1) (Api II), and terbinafine (standard) of concentration 5 mg g(-1) were used. Complete recovery from the infection was recorded on 12th day of treatment for reference drug Terbinafine and Api II (5 mg g(-1) ) concentration of ointment, whereas Api I (2.5 mg g(-1) ) ointment showed complete cure on 16th day of treatment. Fungal burden was also calculated by culturing skin scraping from infected mice's of different groups. Apigenin has shown potency as the infected animals recover completely by Api II comparable to the standard drug in 12th day. So Apigenin can be explored as an antifungal agent in the clinical treatment of dermatophytosis in future.

  8. 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.

  9. HPTLC fingerprint profile, in vitro antioxidant and evaluation of antimicrobial compound produced from Brevibacillus brevis-EGS9 against multidrug resistant Staphylococcus aureus.

    Science.gov (United States)

    Arumugam, T; Senthil Kumar, P; Gopinath, K P

    2017-01-01

    In the present study, in vitro antimicrobial activity of Brevibacillus brevis EGS9 against multi drug resistant Staphylococcus aureus (MDRSA) and to investigate the antimicrobial, antioxidant activity and HPTLC finger print profile of Brevibacillus brevis EGS9. Primary screening was done using by cross streak method against multi drug resistant Staphylococcus aureus. The bioactive metabolites were extracted from Brevibacillus brevis EGS9 using ethyl acetate extraction. Ethyl acetate extract showed significant antimicrobial activity against Escherichia coli (20.2 ± 0.1) mm, Candida albicans (19.2 ± 0.3) mm and Bacillus cereus (18.6 ± 0.2) mm respectively. Forty three UTI bacterial strains were isolated from mid-urine samples of 50 males and 50 females. Escherichia coli were more predominant (48%) followed by Klebsilla pneumonia (29%), Pseudomonas aeruginosa (17%), Staphylococcus aureus (4%) and Enterobacter faecalis (6%). The ethyl acetate extract was examined to evaluate antibacterial properties against isolated UTIs bacterial pathogens. The results were revealed that the maximum zone was measured in Escherichia coli (18.1 ± 0.4) mm and minimum zone of inhibition was shown against Pseudomonas aeruginosa (10.6 ± 0.3) mm. Based on the results obtained, the extract of Brevibacillus brevis EGS9 exhibited dose dependent manner of antioxidant activity. The DPPH scavenging activity of lowest concentration at 25 μg/ml and high concentration at 1000 μg/ml was measured at 2.4% and 39.5% respectively. HPTLC finger print profile was showed the active compounds present in crude extract, which may responsible for the antioxidant prospective. These results showed that, the significant antimicrobial properties against pathogen; this work will be helpful to explore the active compound identification in the field of pharmaceutical research and able to produce new drug molecules against pathogens.

  10. Analysis of Volatile Metabolites Released by Staphylococcus Aureus using Gas Chromatography-Mass Spectrometry and Determination of its Antifungal Activity

    Directory of Open Access Journals (Sweden)

    Hayfaa Hussein Jaddoa

    2016-08-01

    , Glycyl-D-asparagine, Actinomycin C2, 12-Octadecenoic acid , methyl ester, 6-Octadecenoic acid , methyl ester ,(z-, 2,5-Piperazinedione , 3,6-bis(2-methylpropyl-, l-Leucyl-d-leucine and Methyl 12-hydroxy-9-octadecenoate. Gramineae poaceae was very highly active (6.71±0.13 mm. The results of anti-fungal activity produced by Staphylococcus aureus showed that the volatile compounds were highly effective to suppress the growth of Aspergillus terreus. Staphylococcus aureus produce many important secondary metabolites with high biological activities. Based on the significance of employing bioactive compounds in pharmacy to produce drugs for the treatment of many diseases, the purification of compounds produced by Staphylococcus aureus can be useful.

  11. 五株土壤细菌所产抑菌挥发性物质的生物活性评估及其应用%Bioactive evaluation and application of antifungal volatiles generated by five soil bacteria

    Institute of Scientific and Technical Information of China (English)

    刘玮玮; 赵丽静; 王超; 慕卫; 刘峰

    2009-01-01

    To study the bioactivity and application potential of antifungal volatile organic compounds (VOCs)from soil bacteria,the volatiles generated by five bacteria were determined by SPME-GC-MS (Solid Phase Microextraction-Gas Chromatography-Mass Spectrometry)and their bioactivity was given further confirmation with commercially available compounds in sealed plates.Further,the application of these volatile-producing bacteria for the biological control of two main diseases on cucumber caused by Sclerotinia sclerrotium and Sphaerotheca fuliginea,respectively treated by soil and direct fumigation,was investigated in greenhouse.In total,21-31 and 12 compounds were detected from bacterial TSB-YE cultures and TSB-YE medium controls,respectively,which covered a wide range of alkyl,aldehyde,alcohol,ketone,fatty acid,amine,oxime,phenol and heterocyclics.Of the 20 candidate compounds assayed for antifungal activity in sealed plates,furfural,benzaldehyde,1-octanol,1-octen-3-ol,3,7-dimethyl-1,6-octadien-3-ol,2-ethyl-1-hexanol exhibited complete inhibition against S.sclerotiorum at a lowest treatment dosage of 0.01 g.Mixing the autoclaved soil with bacteria caused a higher control effect (28.57%-71.43%)on S.sclerrotium than those of bottom layer treatments,and an obvious growth promotion of cucumber seedlings was shown.When applied directly as fumigation,these volatiles could significantly inhibit the disease severity of powdery mildew on the fumigating seedlings.

  12. Response Surface Methodology: Optimisation of Antifungal Bioemulsifier from Novel Bacillus thuringiensis

    Science.gov (United States)

    Venkatachalam, Ponnusami

    2014-01-01

    An antifungal bioemulsifier compound was produced from a novel strain of Bacillus thuringiensis pak2310. To accentuate the production and as the first step to improve the yield, a central composite design (CCD) was used to study the effect of various factors like minimal salts (1X and 3X), glycerol concentration (2% and 4%), beef extract concentration (1% and 3%), and sunflower oil concentration (2% and 4%) on the production of bioemulsifier molecule and to optimize the conditions to increase the production. The E24 emulsification index was used as the response variable as the increase in surfactant production was seen to be proportional to increased emulsification. A quadratic equation was employed to express the response variable in terms of the independent variables. Statistical tools like student's t-test, F-test, and ANOVA were employed to identify the important factors and to test the adequacy of the model. Under optimum conditions (1X concentration of minimal salts (MS), 2.6% glycerol (v/v), 1% beef extract (w/v), and 2% sunflower oil (v/v)) a 65% increase in yield was produced. PMID:25379529

  13. Response surface methodology: optimisation of antifungal bioemulsifier from novel Bacillus thuringiensis.

    Science.gov (United States)

    Rajendran, Deepak; Venkatachalam, Ponnusami; Ramakrishnan, Jayapradha

    2014-01-01

    An antifungal bioemulsifier compound was produced from a novel strain of Bacillus thuringiensis pak2310. To accentuate the production and as the first step to improve the yield, a central composite design (CCD) was used to study the effect of various factors like minimal salts (1X and 3X), glycerol concentration (2% and 4%), beef extract concentration (1% and 3%), and sunflower oil concentration (2% and 4%) on the production of bioemulsifier molecule and to optimize the conditions to increase the production. The E 24 emulsification index was used as the response variable as the increase in surfactant production was seen to be proportional to increased emulsification. A quadratic equation was employed to express the response variable in terms of the independent variables. Statistical tools like student's t-test, F-test, and ANOVA were employed to identify the important factors and to test the adequacy of the model. Under optimum conditions (1X concentration of minimal salts (MS), 2.6% glycerol (v/v), 1% beef extract (w/v), and 2% sunflower oil (v/v)) a 65% increase in yield was produced.

  14. Response Surface Methodology: Optimisation of Antifungal Bioemulsifier from Novel Bacillus thuringiensis

    Directory of Open Access Journals (Sweden)

    Deepak Rajendran

    2014-01-01

    Full Text Available An antifungal bioemulsifier compound was produced from a novel strain of Bacillus thuringiensis pak2310. To accentuate the production and as the first step to improve the yield, a central composite design (CCD was used to study the effect of various factors like minimal salts (1X and 3X, glycerol concentration (2% and 4%, beef extract concentration (1% and 3%, and sunflower oil concentration (2% and 4% on the production of bioemulsifier molecule and to optimize the conditions to increase the production. The E24 emulsification index was used as the response variable as the increase in surfactant production was seen to be proportional to increased emulsification. A quadratic equation was employed to express the response variable in terms of the independent variables. Statistical tools like student’s t-test, F-test, and ANOVA were employed to identify the important factors and to test the adequacy of the model. Under optimum conditions (1X concentration of minimal salts (MS, 2.6% glycerol (v/v, 1% beef extract (w/v, and 2% sunflower oil (v/v a 65% increase in yield was produced.

  15. Antifungal properties of Brazilian cerrado plants

    Directory of Open Access Journals (Sweden)

    Souza Lúcia Kioko Hasimoto e

    2002-01-01

    Full Text Available Ethanolic extracts from leaves of Hyptis ovalifolia, H. suaveolens, H. saxatilis, Hyptidendrum canum, Eugenia uniflora, E. dysenterica, Caryocar brasiliensis and Lafoensia pacari were investigated for their antifungal activity against dermatophytes. The most effective plants were H. ovalifolia and E. uniflora, while Trichophyton rubrum was the most sensitive among the four dermatophytes species evaluated. This study has demonstrated antifungal properties of Brazilian Cerrado plant extracts in "in vitro" assays.

  16. 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.

  17. Prenylated flavonoids from the roots of Desmodium caudatum and evaluation of their antifungal activity.

    Science.gov (United States)

    Sasaki, Hisako; Kashiwada, Yoshiki; Shibatav, Hirofumi; Takaishi, Yoshihisa

    2012-11-01

    Two new prenylated flavonoids (1, 4) and two new prenylated C-methyl-flavonoids (6, 7), together with four known flavonoids (2, 3, 5, 8), were isolated from the roots of Desmodium caudatum. The structures of the new compounds were elucidated by extensive spectroscopic analyses including 1D-, 2D-NMR and MS. The antifungal activities of five compounds (1, 2, 4, 6, 8) as well as nine flavonoids (9-17) previously isolated from this plant against Aspergillus niger, Penicillium sp., Rhizopus sp., and Trichophyton sp. were evaluated. Compound 6 showed potent antifungal activity against Trichophyton sp. with a minimum inhibitory concentration (MIC) value of 1.95 µg/mL.

  18. Synthesis and Antifungal Activities of New Type β-Methoxyacrylate-Based StrobUurin Analogues

    Institute of Scientific and Technical Information of China (English)

    张翔; 刘慧君; 高永鑫; 王会利; 郭宝元; 李建中

    2012-01-01

    Strobilurins have become one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel fl-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, 1H nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activity against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 μg/mL. Exhilaratingly, compound 1 a (R= methyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

  19. 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.

  20. 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.

  1. Antifungal Activity of the Volatiles of High Potency Cannabis sativa L. Against Cryptococcus neoformans

    Directory of Open Access Journals (Sweden)

    Amira S. Wanas

    2016-03-01

    Full Text Available The n-hexane extracted volatile fraction of high potency Cannabis sativa L (Cannabaceae . was assessed in vitro for antifungal, antibacterial and antileishmanial activities. The oil exhibited selective albeit modest, antifungal activity against Cryptococcus neoformans with an IC 50 value of 33.1 µg/mL. Biologically-guided fractionation of the volatile fraction resulted in the isolation of three major compounds (1-3 using various chromatographic techniques. The chemical structures of the isolated compounds were identified as α-humulene (1, b -caryophyllene (2 and caryophyllene oxide (3 using GC/FID, GC/MS, 1D- and 2D-NMR analyses, respectively. Compound 1 showed potent and selective antifungal activity against Cryptococcus neoformans with IC 50 and MIC values of 1.18 m g/mL and 5.0 m g/mL respectively. Whereas compound 2 showed weak activity (IC 50 19.4 µg/mL, while compound 3 was inactive against C. neoformans.

  2. Leaf-associated bacteria from transgenic white poplar producing resveratrol-like compounds: isolation, molecular characterization, and evaluation of oxidative stress tolerance.

    Science.gov (United States)

    Balestrazzi, Alma; Bonadei, Martina; Calvio, Cinzia; Mattivi, Fulvio; Carbonera, Daniela

    2009-07-01

    The aim of this study was the isolation and characterization of the culturable bacteria inhabiting the leaves of transgenic white poplars (Populus alba L. 'Villafranca') engineered with the StSy gene for the production of resveratrol-like compounds. Resveratrol glucosides are available in small amounts from natural sources or by expensive chemical synthesis procedures. An alternative approach for the large-scale production of these relevant pharmaceuticals is the use of transgenic plants as bioreactors, although the occurrence of novel molecules in plants growing under field conditions might interfere, to some extent, with the associated microbial population. Both epiphytes and endophytes were isolated from the leaves of 2 StSy transgenic lines producing resveratrol glucosides and from an untransformed plant line grown in a greenhouse. Eleven isolates were recovered and classified as members of the genus Bacillus by 16S rDNA-based analysis. In addition, 2 isolates were classified as members of the Curtobacterium and Kocuria genera, respectively. Tolerance to hydrogen peroxide, UV-C, and paraquat was evaluated, as were the swimming and swarming motility of the leaf-associated bacteria. Interestingly, the isolates recovered from transgenic tissues showed the ability to withstand oxidative stress compared with isolates recovered from the untransformed poplar line. In vitro bioassays showed that trans-resveratrol inhibited both the swarming and swimming motilities in all the tested bacteria. The effects of trans-resveratrol on flagellin production, required for motility, were also investigated by immunoblot analysis.

  3. Isolation of an extremely halophilic arhaeon Natrialba sp. C21 able to degrade aromatic compounds and to produce stable biosurfactant at high salinity.

    Science.gov (United States)

    Khemili-Talbi, Souad; Kebbouche-Gana, Salima; Akmoussi-Toumi, Siham; Angar, Yassmina; Gana, Mohamed Lamine

    2015-11-01

    Natrialba sp. strain C21 was isolated from oil contaminated saline water in Ain Salah (Algeria) and has exhibited a good potential for degrading phenol (3% v/v), naphthalene (3% v/v), and pyrene (3% v/v) at high salinity with high growth, enzymatic activity and biosurfactant production. Successful metabolism of aromatic hydrocarbon compounds of the strain Natrialba sp. C21 appears to require the ortho-cleavage pathway. Indeed, assays of the key enzymes involved in the ring cleavage of catechol 1, 2-dioxygenase indicated that degradation of the phenol, naphthalene and pyrene by strain Natrialba sp. C21 was via the ortho-cleavage pathway. Cells grown on aromatic hydrocarbons displayed greater ortho-activities mainly towards catechol, while the meta-activity was very low. Besides, biosurfactants derived from the strain C21 were capable of effectively emulsifying both aromatic and aliphatic hydrocarbons and seem to be particularly promising since they have particular adaptations like the increased stability at high temperature and salinity conditions. This study clearly demonstrates for the first time that strain belonging to the genera Natrialba is able to grow at 25% (w/v) NaCl, utilizing phenol, naphthalene, and pyrene as the sole carbon sources. The results suggest that the isolated halophilic archaeon could be a good candidate for the remediation process in extreme environments polluted by aromatic hydrocarbons. Moreover, the produced biosurfactant offers a multitude of interesting potential applications in various fields of biotechnology.

  4. Polyphenol compounds and anti-inflammatory activities of Korean black raspberry ( Rubus coreanus Miquel) wines produced from juice supplemented with pulp and seed.

    Science.gov (United States)

    Lim, Jae Woong; Hwang, Hyun Joo; Shin, Chul Soo

    2012-05-23

    Three types of Korean black raspberry wine were produced via alcoholic fermentation from juice, juice-pulp, and juice-pulp-seed, respectively. These wines were compared in terms of their anti-inflammatory activities and polyphenol contents. The total content of polyphenol compounds in wines was increased by 22.4% after supplementation with pulp and by 56.7% after supplementation with both pulp and seed. The reduction rate of NO evolution was highest in the order juice-pulp-seed wine, juice-pulp wine, and juice wine. Addition of the juice-pulp-seed wine at a level of 62.5-500 mg/L decreased the NO evolution rate by 40.5-94.2%. Eight fractions were obtained from juice-pulp-seed wine via ethyl acetate extraction and silica gel chromatography. Of these, the AF fraction, which exhibited the highest in vitro anti-inflammatory activity, exerted inhibitory effects on ear edema, writhing response, and vein membrane vascular permeability in mice. 3,4-Dihydroxybenzoic acid accounted for 37.6% of the total polyphenol content in the AF fraction.

  5. 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 is

  6. Isolation, Molecular Identification and Evaluation of Antifungal Effects of the Bacilli Isolated from Rhizospheric Soil of Gorgan Region against Tricophyton Mentagrophytes

    Directory of Open Access Journals (Sweden)

    Pordeli, HR. (PhD

    2013-01-01

    Full Text Available Background and Objective: Soil bacteria, particularly Bacillus genus have thepotential of producing a range of bioactive substances with antimicrobial andantifungal properties. They have the ability to produce hundreds of active andeffective biologic compound against microorganisms. Therefore, it seems to be aproper candidate in the biocontrol of fungal pathogenesis.Material and Methods: In this study, soil samples were collected from differentparts of Gorgan in order to isolate Bacillus and to determine their antifungalactivity against T.mentagrophytes. The Isolates that had the highest antifungaleffects were analyzed by PCR and 16s rRNA sequencing.Results: Of 54 strains, 14 have antifungal activity. The Isolates, S4 and S12,identified as B.cereus and B.thuringiensis respectively show the highestantidermatofit effect. These isolates based on 16s rRNA sequence analysis show97% homology with Bacillus cereusstrain KU4 and Bacillus thuringiensisstrainucsc27.Conclusion: According to the results, it seems that the soil Bacilli have biocontrolpotential against dermatophytic agents such as T.mentagrophytes.Keywords: Antifungal effects; Bacillus; Rhizospheric soil; T.mentagrophytes

  7. Screening of Azotobacter isolates for PGP properties and antifungal activity

    Directory of Open Access Journals (Sweden)

    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

  8. Characterization of an antifungal chitinase from Bacillus sp.SL-13

    Institute of Scientific and Technical Information of China (English)

    Chen; Shan

    2014-01-01

    Bacillus sp.SL-13 produced antifungal proteins.The growth of the plant-pathogenic fungi Rhizoctonia solani was considerably inhibited by the presence of the SL-13 culture supernatant.It is very suitable for the use in a relatively unstable environment,exhibiting effective biological control.

  9. In vitro antifungal activity of four chemotypes of Lippia alba (Verbenaceae essential oils against Alternaria solani (Pleosporeaceae isolates

    Directory of Open Access Journals (Sweden)

    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.

  10. In vitro antifungal activity of four chemotypes of Lippia alba (Verbenaceae) essential oils against Alternaria solani (Pleosporeaceae) isolates.

    Science.gov (United States)

    Tomazoni, Elisa Z; Pansera, Márcia R; Pauletti, Gabriel F; Moura, Sidnei; Ribeiro, Rute T S; Schwambach, Joséli

    2016-05-31

    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.

  11. Gene Expression Response of Trichophyton rubrum during Coculture on Keratinocytes Exposed to Antifungal Agents

    Science.gov (United States)

    Komoto, Tatiana Takahasi; Bitencourt, Tamires Aparecida; Silva, Gabriel; Beleboni, Rene Oliveira; Marins, Mozart; Fachin, Ana Lúcia

    2015-01-01

    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. PMID:26257814

  12. Gene Expression Response of Trichophyton rubrum during Coculture on Keratinocytes Exposed to Antifungal Agents

    Directory of Open Access Journals (Sweden)

    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.

  13. Hassallidins, antifungal glycolipopeptides, are widespread among cyanobacteria and are the end-product of a nonribosomal pathway.

    Science.gov (United States)

    Vestola, Johanna; Shishido, Tania K; Jokela, Jouni; Fewer, David P; Aitio, Olli; Permi, Perttu; Wahlsten, Matti; Wang, Hao; Rouhiainen, Leo; Sivonen, Kaarina

    2014-05-06

    Cyanobacteria produce a wide variety of cyclic peptides, including the widespread hepatotoxins microcystins and nodularins. Another class of peptides, cyclic glycosylated lipopeptides called hassallidins, show antifungal activity. Previously, two hassallidins (A and B) were reported from an epilithic cyanobacterium Hassallia sp. and found to be active against opportunistic human pathogenic fungi. Bioinformatic analysis of the Anabaena sp. 90 genome identified a 59-kb cryptic inactive nonribosomal peptide synthetase gene cluster proposed to be responsible for hassallidin biosynthesis. Here we describe the hassallidin biosynthetic pathway from Anabaena sp. SYKE748A, as well as the large chemical variation and common occurrence of hassallidins in filamentous cyanobacteria. Analysis demonstrated that 20 strains of the genus Anabaena carry hassallidin synthetase genes and produce a multitude of hassallidin variants that exhibit activity against Candida albicans. The compounds discovered here were distinct from previously reported hassallidins A and B. The IC50 of hassallidin D was 0.29-1.0 µM against Candida strains. A large variation in amino acids, sugars, their degree of acetylation, and fatty acid side chain length was detected. In addition, hassallidins were detected in other cyanobacteria including Aphanizomenon, Cylindrospermopsis raciborskii, Nostoc, and Tolypothrix. These compounds may protect some of the most important bloom-forming and globally distributed cyanobacteria against attacks by parasitic fungi.

  14. 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.

  15. Evaluation of antifungal potential of selected medicinal plants against human pathogenic fungi

    Directory of Open Access Journals (Sweden)

    Hayat Sakander

    2015-01-01

    Full Text Available Context: Evaluation of medicinal plants used in traditional medicine lead to novel bioactive compounds with antifungal activity that could be exploited as therapeutic agents. Aims: The aim was to screen selected medicinal plants for antifungal activity against three important human pathogenic fungi and to identify the broad group of phytochemicals responsible for the activity. Materials and Methods: A total of 8 medicinal plants were screened for antifungal activity against three human pathogenic fungi. Aqueous and the solvent extracts of the plant materials were prepared by polarity based solvent extraction. Antifungal activity was tested by well and disc diffusion methods. Minimum inhibitory concentration (MIC of the active extract was determined by micro-broth dilution technique. Phytochemical analysis of the active extract was done. Statistical Analysis Used: The results were statistically analysed by One-Way analysis of variance with Post-hoc Tukey′s B test at P < 0.05 using the  Software SPSS version 20 (IBM Corp. Armonk, NY Released 2011. Results: Significant antifungal activity was observed in the aqueous extracts of the fruits of Terminalia chebula (47.75 mm against Microsporum gypseum and the mesocarp of Persea americana (40.5 mm against Microsporum canis. Candida albicans was inhibited by the ethyl acetate (20 mm and aqueous extracts (16 mm of T. chebula fruits and aqueous extract of the seeds of Syzygium jambos (16 mm. The aqueous extract of mesocarp of P. americana showed lowest MIC value (312.5 μg/ml against M. canis and M. gypseum. Phytochemical analysis of the active extracts revealed the presence of phenols, tannins, alkaloids and flavonoids. Conclusions: The study validates the use of the plants in the treatment of fungal infections and has provided important leads for the discovery of new plant-based antifungal agents.

  16. Antinociception produced by Thalassia testudinum extract BM-21 is mediated by the inhibition of acid sensing ionic channels by the phenolic compound thalassiolin B

    Directory of Open Access Journals (Sweden)

    Thomas Olivier P

    2011-01-01

    Full Text Available Abstract Background Acid-sensing ion channels (ASICs have a significant role in the sensation of pain and constitute an important target for the search of new antinociceptive drugs. In this work we studied the antinociceptive properties of the BM-21 extract, obtained from the sea grass Thalassia testudinum, in chemical and thermal models of nociception in mice. The action of the BM-21 extract and the major phenolic component isolated from this extract, a sulphated flavone glycoside named thalassiolin B, was studied in the chemical nociception test and in the ASIC currents of the dorsal root ganglion (DRG neurons obtained from Wistar rats. Results Behavioral antinociceptive experiments were made on male OF-1 mice. Single oral administration of BM-21 produced a significant inhibition of chemical nociception caused by acetic acid and formalin (specifically during its second phase, and increased the reaction time in the hot plate test. Thalassiolin B reduced the licking behavior during both the phasic and tonic phases in the formalin test. It was also found that BM-21 and thalassiolin B selectively inhibited the fast desensitizing (τ Conclusions To our knowledge, this is the first report of an ASIC-current inhibitor derived of a marine-plant extract, and in a phenolic compound. The antinociceptive effects of BM-21 and thalassiolin B may be partially because of this action on the ASICs. That the active components of the extract are able to cross the blood-brain barrier gives them an additional advantage for future uses as tools to study pain mechanisms with a potential therapeutic application.

  17. Antifungal, Cytotoxic, and Immunomodulatory Properties of Tea Tree Oil and Its Derivative Components: Potential Role in Management of Oral Candidosis in Cancer Patients

    OpenAIRE

    Ramage, Gordon; Milligan, Steven; Lappin, David F; Sherry, Leighann; Sweeney, Petrina; Williams, Craig; Bagg, Jeremy; Culshaw, Shauna

    2012-01-01

    Candida albicans forms oral biofilms that cause disease and are difficult to treat with conventional antifungal agents. Tea tree oil (TTO) is a natural compound with reported antimicrobial and immunomodulatory activities. The aims of the study were to evaluate the antifungal efficacy of TTO and key derivatives against C. albicans biofilms, to assess the toxicological effects of TTO on a clinically relevant oral cell line, and to investigate its impact on inflammation. TTO and its derivatives ...

  18. Antifungal, cytotoxic and immunomodulatory properties of tea tree oil and its derivative components: potential role in management of oral candidosis in cancer patients

    OpenAIRE

    Gordon eRamage; Steven eMilligan; Lappin, David F; Leighann eSherry; Petrina eSweeney; Craig eWilliams; Jeremy eBagg; Shauna eCulshaw

    2012-01-01

    Candida albicans forms oral biofilms that cause disease and are difficult to treat with conventional antifungal agents. Tea tree oil (TTO) is a natural compound with reported antimicrobial and immunomodulatory activities. The aims of the study were to evaluate the antifungal efficacy of TTO and key derivatives against C. albicans biofilms, to assess the toxicological effects of TTO on a clinically relevant oral cell line, and to investigate its impact on inflammation. TTO and its derivatives ...

  19. New ikarugamycin derivatives with antifungal and antibacterial properties from Streptomyces zhaozhouensis.

    Science.gov (United States)

    Lacret, Rodney; Oves-Costales, Daniel; Gómez, Cristina; Díaz, Caridad; de la Cruz, Mercedes; Pérez-Victoria, Ignacio; Vicente, Francisca; Genilloud, Olga; Reyes, Fernando

    2014-12-29

    A bioassay guided fractionation of the ethyl acetate extract from culture broths of the strain Streptomyces zhaozhouensis CA-185989 led to the isolation of three new polycyclic tetramic acid macrolactams (1-3) and four known compounds. All the new compounds were structurally related to the known Streptomyces metabolite ikarugamycin (4). Their structural elucidation was accomplished using a combination of electrospray-time of flight mass spectrometry (ESI-TOF MS) and 1D and 2D NMR analyses. Compounds 1-3 showed antifungal activity against Aspergillus fumigatus, Candida albicans and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).

  20. New Ikarugamycin Derivatives with Antifungal and Antibacterial Properties from Streptomyces zhaozhouensis

    Directory of Open Access Journals (Sweden)

    Rodney Lacret

    2014-12-01

    Full Text Available A bioassay guided fractionation of the ethyl acetate extract from culture broths of the strain Streptomyces zhaozhouensis CA-185989 led to the isolation of three new polycyclic tetramic acid macrolactams (1–3 and four known compounds. All the new compounds were structurally related to the known Streptomyces metabolite ikarugamycin (4. Their structural elucidation was accomplished using a combination of electrospray-time of flight mass spectrometry (ESI-TOF MS and 1D and 2D NMR analyses. Compounds 1–3 showed antifungal activity against Aspergillus fumigatus, Candida albicans and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA.

  1. Characterization of a New Sesquiterpene and Antifungal Activities of Chemical Constituents from Dryopteris fragrans (L. Schott

    Directory of Open Access Journals (Sweden)

    Yu-Hong Huang

    2014-01-01

    Full Text Available One new sesquiterpene and six known compounds were isolated from Dryopteris fragrans (L. Schot. They were identified as 3-O-β-D-glucopyranosylalbicanol- 11-O-β-D-glucopyranoside (1, dihydroconiferylalcohol (2, (E-3-(4-hydroxyphenylacrylic acid (3, esculetin (4, 5,7-dihydroxy-2-hydroxymethylchromone (5, eriodictyol (6 and isoorientin (7 by UV, MS, 1D-NMR and 2D-NMR spectroscopy. The antifungal activities of the seven isolated compounds were screened. Compounds 2, 3, 4 and 5 showed obvious activities against Microsporum canis and Epidermophyton floccosum.

  2. 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)

  3. Synthesis, antimicrobial and antifungal activities of novel 1H-1,4-diazepines containing pyrazolopyrimidinone moiety

    Indian Academy of Sciences (India)

    Rajesh Kumar; Yogesh Chandra Joshi

    2009-07-01

    Acylation of 5-(2-ethoxyphenyl)-1-methyl-3-propyl-1,6-dihydro-7-pyrazolo [4,3-d) pyrimidin-7-one 1 with chloroacetylchloride in the presence of anyhydrous aluminium chloride affords 5-[(5-chloroacetyl-2-ethoxy)phenyl]-1-methyl-3-propyl-1,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one 2. The compound 2 condensed with various -diketones/-ketoesters compound, to obtain new -diketones/-ketoesters 4a-i treated with ethylenediamine (EDA) gives 1H-1,4-diazepines. The compounds 5a-i has been screened for antimicrobial, antifungal and anthelmintic activities.

  4. New Ikarugamycin Derivatives with Antifungal and Antibacterial Properties from Streptomyces zhaozhouensis

    Science.gov (United States)

    Lacret, Rodney; Oves-Costales, Daniel; Gómez, Cristina; Díaz, Caridad; de la Cruz, Mercedes; Pérez-Victoria, Ignacio; Vicente, Francisca; Genilloud, Olga; Reyes, Fernando

    2014-01-01

    A bioassay guided fractionation of the ethyl acetate extract from culture broths of the strain Streptomyces zhaozhouensis CA-185989 led to the isolation of three new polycyclic tetramic acid macrolactams (1–3) and four known compounds. All the new compounds were structurally related to the known Streptomyces metabolite ikarugamycin (4). Their structural elucidation was accomplished using a combination of electrospray-time of flight mass spectrometry (ESI-TOF MS) and 1D and 2D NMR analyses. Compounds 1–3 showed antifungal activity against Aspergillus fumigatus, Candida albicans and antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA). PMID:25551780

  5. Antifungal Substances from Streptomyces sp. A3265 Antagonistic to Plant Pathogenic Fungi.

    Science.gov (United States)

    Van Minh, Nguyen; Woo, E-Eum; Kim, Ji-Yul; Kim, Dae-Won; Hwang, Byung Soon; Lee, Yoon-Ju; Lee, In-Kyoung; Yun, Bong-Sik

    2015-09-01

    In a previous study, we identified a Streptomyces sp., A3265, as exhibiting potent antifungal activity against various plant pathogenic fungi, including Botrytis cinerea, Colletotrichum gloeosporioides, and Rhizoctonia solani. This strain also exhibited a biocontrolling effect against ginseng root rot and damping-off disease, common diseases of ginseng and other crops. In this study, we isolated two antifungal substances responsible for this biocontrolling effect via Diaion HP-20 and Sephadex LH-20 column chromatography, medium pressure liquid chromatography, and high-performance liquid chromatography. These compounds were identified as guanidylfungin A and methyl guanidylfungin A by spectroscopic methods. These compounds exhibited potent antimicrobial activity against various plant pathogenic fungi as well as against bacteria.

  6. New synthesis and biological evaluation of benzothiazole derivates as antifungal agents.

    Science.gov (United States)

    Herrera Cano, Natividad; Ballari, María S; López, Abel G; Santiago, Ana N

    2015-04-15

    In search of new antifungal agrochemicals that could replace commercially available, aryl-2-mercaptobenzothiazoles were synthesized. They were prepared by two methodologies, using both photostimulated reaction and microwave assisted reaction. These reactions took place without the use of metallic catalyst by a one-pot procedure with excellent yields (70-98%). Synthesized compounds were evaluated for fungal growth inhibition against Botrytis cinerea. Most of the compounds have an excellent antifungal activity, and three of these showed a superior inhibitory effect to commercial fungicide Triadimefon. IC50 values observed for 2-(phenylthio)benzothiazole, 2-(2-chlorophenylthio)benzothiazole, and 2-(3-chlorophenyl thio)benzothiazole were 0.75, 0.69, and 0.65 μg mL(-1), respectively.

  7. Anti-fungal activities of constituents from Uvaria scheffleri and Artabotrys brachypetalus

    Directory of Open Access Journals (Sweden)

    Odebode A.C.

    2006-01-01

    Full Text Available The anti-fungal activity of schefflone, a mixture of dimmer, 3,5 dimethoxy carvacrol and annonaceous acetogenin, extracted from stem-bark and root of Uvaria scheffleri and Artabotrys bruchypetalus against Fusarium solani, Botryodiplodia theobromae, Asperillus niger and Aspergillus flavus was determined. An in-vitro bioassay showed that the minimum inhibitory effect of the compounds to the fungal pathogens occurred at 200 ppm in both radial growth and mycelia dry weight measurements. Acetogenin from A brachypetalus had a very strong anti-fungal effect on all the test fungi. The effects of the compounds were more pronounced on F solani than on the other. The bioassay methods also play a significant role in the sensitivity of the samples on the pathogens. .

  8. 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)

  9. Synthesis and biological evaluation of fluconazole analogs with triazole-modified scaffold as potent antifungal agents.

    Science.gov (United States)

    Hashemi, Seyedeh Mahdieh; Badali, Hamid; Irannejad, Hamid; Shokrzadeh, Mohammad; Emami, Saeed

    2015-04-01

    In order to find new azole antifungals, we have recently designed a series of triazole alcohols in which one of the 1,2,4-triazol-1-yl group in fluconazole structure has been replaced with 4-amino-5-aryl-3-mercapto-1,2,4-triazole motif. In this paper, we focused on the structural refinement of the primary lead, by removing the amino group from the structure to achieve 5-aryl-3-mercapto-1,2,4-triazole derivatives 10a-i and 11a-i. The in vitro antifungal susceptibility testing of title compounds demonstrated that most compounds had potent inhibitory activity against Candida species. Among them, 5-(2,4-dichlorophenyl)triazole analogs 10h and 11h with MIC values of fluconazole against Candida species.

  10. Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate.

    Science.gov (United States)

    Sun, Jialong; Zhou, Yuanming

    2015-03-09

    A series of pyrazole carboxamide and isoxazolol pyrazole carboxylate derivatives were designed and synthesized in this study. The structures of the compounds were elucidated based on spectral data (infrared, proton nuclear magnetic resonance and mass spectroscopy). Then, all of the compounds were bioassayed in vitro against four types of phytopathogenic fungi (Alternaria porri, Marssonina coronaria, Cercospora petroselini and Rhizoctonia solani) using the mycelium growth inhibition method. The results showed that some of the synthesized pyrazole carboxamides displayed notable antifungal activity. The isoxazole pyrazole carboxylate 7ai exhibited significant antifungal activity against R. solani, with an EC50 value of 0.37 μg/mL. Nonetheless, this value was lower than that of the commercial fungicide, carbendazol.

  11. Epidemiology and antifungal resistance in invasive candidiasis

    Directory of Open Access Journals (Sweden)

    Rodloff AC

    2011-04-01

    Full Text Available Abstract The epidemiology of Candida infections has changed over the last two decades: The number of patients suffering from such infections has increased dramatically and the Candida species involved have become more numerous as Candida albicans is replaced as an infecting agent by various non-C. albicans species (NAC. At the same time, additional antifungal agents have become available. The different Candida species may vary in their susceptibility for these various antifungals. This draws more attention to in vitro susceptibility testing. Unfortunately, several different test methods exist that may deliver different results. Moreover, clinical breakpoints (CBP that classify test results into susceptible, intermediate and resistant are controver- sial between CLSI and EUCAST. Therefore, clinicians should be aware that interpretations may vary with the test system being followed by the microbiological laboratory. Thus, knowledge of actual MIC values and pharmacokinetic properties of individual antifungal agents is important in delivering appropriate therapy to patients

  12. The SRAP based molecular diversity related to antifungal and antioxidant bioactive constituents for biocontrol potentials of Trichoderma against Sclerotium rolfsii Scc.

    Science.gov (United States)

    Hirpara, Darshna G; Gajera, H P; Bhimani, R D; Golakiya, B A

    2016-08-01

    The study was performed to examine 11 isolates of Trichoderma for their bio-control potentials against Sclerotium rolfsii Sacc. causing stem rot in groundnut. The antagonists Trichoderma were subjected to sequence related amplified polymorphism (SRAP) based molecular diversity analysis and compared with their hardness to S. rolfsii with respect to secretary antifungal and antioxidant profile. T. virens NBAII Tvs 12 evident highest (87.91 %) growth inhibition of test pathogen followed by T. koningii MTCC 796 (67.03 %) at 7 days after inoculation (DAI). Microscopic study confirmed biocontrol mechanism as mycoparasitism for Tvs 12 and antibiosis for MTCC 796. The growth inhibition of test pathogen was significantly negatively correlated with sclerotia formation and lipid peroxidation during antagonism due to release of secretary bioactive antioxidants by antagonists to terminate oxidative burst generated by S. rolfsii and causing inhibition of sclerotium formation. The GC-MS profile identified antifungal and antioxidant constituents hexadecane, 1,2-benzenedicarboxylic acid, mono (2-ethylhexyl) ester, 1-hexadecanesulfonyl chloride, and octadecane in potent antagonists Tvs 12; and nonacosane and octadecane in MTCC 796 along with two novel compounds 1-pentadecene and 1-heneicosyl formate for biocontrol activity. Molecular diversity of Trichoderma isolates associated with antagonistic activity was assessed by SRAP markers. The 115 primer combinations generate total 1328 amplified products of which, 1095 are shared polymorphic and 199 are unique polymorphic. The 15 SRAP combinations produced 18 bands to diagnose best antagonist Tvs 12 and 13 SRAP combinations generated 19 unique bands for identification of MTCC 796. The mycoparasitic antagonist Tvs 12 would be the best antagonist and released unique antifungal and antioxidant constituents to combat pathogen infection. The SRAP based genetic diversity indicates Tvs12 strain clustered with T. viride NBAII Tv23 and shared

  13. Synthesis, Antifungal Activities and Qualitative Structure Activity Relationship of Carabrone Hydrazone Derivatives as Potential Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Hao Wang

    2014-03-01

    Full Text Available Aimed at developing novel fungicides for relieving the ever-increasing pressure of agricultural production caused by phytopathogenic fungi, 28 new hydrazone derivatives of carabrone, a natural bioactive sesquisterpene, in three types were designed, synthesized and their antifungal activities against Botrytis cinerea and Colletotrichum lagenarium were evaluated. The result revealed that all the derivatives synthesized exhibited considerable antifungal activities in vitro and in vivo, which led to the improved activities for carabrone and its analogues and further confirmed their potential as antifungal agents.

  14. Optimization of Medium for Lactobacillus plantarum IMAU10116 Producing Active Compound against Penicillium roqueforti%植物乳杆菌IMAU10116产生抗娄地青霉活性物质培养基的优化

    Institute of Scientific and Technical Information of China (English)

    戚薇; 石景; 尹娅凤; 王海宽

    2011-01-01

    [ Objective ] The study aimed to screen out Lactobacillus plantarum possessing higher inhibitory activity against Penicillium roqueforti and enhance its antifungal activity. [ Method] The activated L. plantarum IMAU10116 was innoculated MRS liquid medium for culturing and double-layer plate point inoculation was used to evaluate its activity against P. roqueforti. [ Result] The single-factor experiments showed that when glucose was used as carbon source, the inhibitory effect of L. plantarum 1MAUl0116 against P. roqueforti was best; when malt extract powder was used as nitrogen source, its inhibitory effect was best; the optimum growth factor for antifungal lactobacillus producing antifungal substance was powder of corn steep liquor. The optimum medium composition of L. plantarum IMAU10116 was 20 g/L glucose + 20 g/L malt extract powder + 7 g/L powder of corn steep liquor + quantum sufficit mineral salt. The diameter of inhibition zone of L. plantarum IMAU10116 cultured with optimized medium against P. roqueforti was 18.6 mm and that of L. plantarum IMAU10116 cultured with MRS medium was 15.0 mm. [Conclusion] L. plantarum IMAU10116 had very good inhibition activity against P. roquefoni and it was hopeful to get better application in food and forage additive domain.%[目的]筛选对娄地青霉有较强抑菌活性的植物乳杆菌并提高其抗真菌活性.[方法]将活化后的植物乳杆菌IMAU10116接种到MRS液体培养基中培养,采用双层平板点接法评价其杭娄地青霉菌的活性.[结果]单因素试验表明,以葡萄糖为碳源时,植物乳杆菌IMAU10116对娄地青霉的抑制效果最好;植物乳杆菌以麦芽浸粉为氮源时,抑菌效果最好;抗真菌乳酸菌产生杭菌物质的最佳生长因子为玉米浆粉植物乳杆菌IMAU10116最佳培养基组成为:葡萄糖20 g/L+麦芽浸粉20 g/L+玉米浆粉7 g/L+适量无机盐.用优化培养基培养的植物乳杆菌IMAU10116抑制娄地青霉菌产生的抑菌圈为18.6 mm

  15. Characteristic spectral studies and in vitro antifungal activity of some Schiff bases and their organotin (Ⅳ) complexes

    Institute of Scientific and Technical Information of China (English)

    Wajid Rehman; Musa Kaleem Baloch; Bakhtiar Muhammad; Amin Badshah; Khalid M. Khan

    2004-01-01

    The synthesis and in vitro antifungal activity of some Schiff bases and their Sn (Ⅳ) complexes has been tested against plant pathogenic fungi and it is found that they possess excellent fungicidal activity. On the basis of 1H-, 13C-, 119Sn NMR-, 119Sn Mossbauer, IR and Elemental analysis the tetrahedral geometry is proposed for the synthesized compounds.

  16. Microwave-Assisted Synthesis and Biological Evaluation of Dihydropyrimidinone Derivatives as Anti-Inflammatory, Antibacterial, and Antifungal Agents

    Directory of Open Access Journals (Sweden)

    Anjna Bhatewara

    2013-01-01

    Full Text Available A simple protocol for the efficient preparation of aryl and heteroaryl substituted dihydropyrimidinone has been achieved via initial Knoevenagel, subsequent addition, and final cyclization of aldehyde, ethylcyanoacetate, and guanidine nitrate in the presence of piperidine as a catalyst in solvent-free under microwave irradiation. The synthesized compounds showed a good anti-inflammatory, antibacterial, and antifungal activity.

  17. 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.

  18. Antifungal agents in neonates: issues and recommendations.

    Science.gov (United States)

    Almirante, Benito; Rodríguez, Dolors

    2007-01-01

    Fungal infections are responsible for considerable morbidity and mortality in the neonatal period, particularly among premature neonates. Four classes of antifungal agents are commonly used in the treatment of fungal infections in pediatric patients: polyene macrolides, fluorinated pyrimidines, triazoles, and echinocandins. Due to the paucity of pediatric data, many recommendations for the use of antifungal agents in this population are derived from the experience in adults. The purpose of this article was to review the published data on fungal infections and antifungal agents, with a focus on neonatal patients, and to provide an overview of the differences in antifungal pharmacology in neonates compared with adults. Pharmacokinetic data suggest dosing differences in children versus adult patients with some antifungals, but not all agents have been fully evaluated. The available pharmacokinetic data on the amphotericin B deoxycholate formulation in neonates exhibit considerable variability; nevertheless, the dosage regimen suggested in the neonatal population is similar to that used in adults. More pharmacokinetic information is available on the liposomal and lipid complex preparations of amphotericin B and fluconazole, and it supports their use in neonates; however, the optimal dosage and duration of therapy is difficult to establish. All amphotericin-B formulations, frequently used in combination with flucytosine, are useful for treating disseminated fungal infections and Candida meningitis in neonates. Fluconazole, with potent in vitro activity against Cryptococcus neoformans and almost all Candida spp., has been used in neonates with invasive candidiasis at dosages of 6 mg/kg/day, and for antifungal prophylaxis in high-risk neonates. There are limited data on itraconazole, voriconazole, and posaconazole use in neonates. Caspofungin, which is active against Candida spp. and Aspergillus spp., requires higher doses in children relative to adults, and dosing is

  19. New aminoporphyrins bearing urea derivative substituents: synthesis, characterization, antibacterial and antifungal activity

    Directory of Open Access Journals (Sweden)

    Gholamreza Karimipour

    2015-06-01

    Full Text Available This work studied the synthesis of 5,10,15-tris(4-aminophenyl-20-(N,N-dialkyl/diaryl-N-phenylurea porphyrins (P1-P4 with alkyl or aryl groups of Ph, iPr, Et and Me, respectively and also the preparation of their manganese (III and cobalt (II complexes (MnP and CoP. The P1-P4 ligands were characterized by different spectroscopic techniques (1H NMR, FTIR, UV-Vis and elemental analysis, and metalated with Mn and Co acetate salts. The antibacterial and antifungal activities of these compounds in vitro were investigated by agar-disc diffusion method against Escherichia coli (-, Pseudomonas aeruginosa (-, Staphylococcus aureus(+, Bacillus subtilis (+ and Aspergillus oryzae and Candida albicans. Results showed that antibacterial and antifungal activity of the test samples increased with increase of their concentrations and the highest activity was obtained when the concentration of porphyrin compounds was 100 µg/mL. The activity for the porphyrin ligands depended on the nature of the urea derivative substituents and increased in the order P1 > P2 > P3 >P4, which was consistent with the order of their liposolubility. MnP and CoP complexes exhibited much higher antibacterial and antifungal activity than P1-P4ligands. Further, the growth inhibitory effects of these compounds was generally in the order CoP complexes > MnP complexes > P1-P4 ligands. Among these porphyrin compounds, CoP1displayed the highest antibacterial and antifungal activity, especially with a concentration of 100 µg/mL, against all the four tested bacteria and two fungi, and therefore it could be potential to be used as drug.

  20. Anti-fungal activity of crude extracts and essential oil of Moringa oleifera Lam.

    Science.gov (United States)

    Chuang, Ping-Hsien; Lee, Chi-Wei; Chou, Jia-Ying; Murugan, M; Shieh, Bor-Jinn; Chen, Hueih-Min

    2007-01-01

    Investigations were carried out to evaluate the therapeutic properties of the seeds and leaves of Moringa oleifera Lam as herbal medicines. Ethanol extracts showed anti-fungal activities in vitro against dermatophytes such as Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis. GC-MS analysis of the chemical composition of the essential oil from leaves showed a total of 44 compounds. Isolated extracts could be of use for the future development of anti-skin disease agents.

  1. Characterization of Antifungal Activity and Nail Penetration of ME1111, a New Antifungal Agent for Topical Treatment of Onychomycosis

    OpenAIRE

    Tabata, Yuji; Takei-Masuda, Naomi; Kubota, Natsuki; Takahata, Sho; Ohyama, Makoto; Kaneda, Kaori; Iida, Maiko; Maebashi, Kazunori

    2016-01-01

    Fungal nail infection (onychomycosis) is a prevalent disease in many areas of the world, with a high incidence approaching 23%. Available antifungals to treat the disease suffer from a number of disadvantages, necessitating the discovery of new efficacious and safe antifungals. Here, we evaluate the in vitro antifungal activity and nail penetration ability of ME1111, a novel antifungal agent, along with comparator drugs, including ciclopirox, amorolfine, terbinafine, and itraconazole. ME1111 ...

  2. Bioautography Guided Identification of Anticandidal Compounds from A. terreus st. 1

    Directory of Open Access Journals (Sweden)

    B. K. Nagaraja

    2011-01-01

    Full Text Available Problem statement: Saprophytic and soil inhabiting microorganisms are prolific producers of secondary metabolites with wide range of structural and functional diversity. The objective of the current study was to screen and evaluate the anti-candidal properties of soil inhabiting fungi. Approach: Preliminary dual culture assay and bioautography was used to screen the fungi with potential anti-fungal activity and direct detection of antifungal compound/fraction in microbial extract on thin layer chromatograms, respectively. Disk diffusion, broth dilution and germ tube inhibitory assay were used to evaluate and confirm the anticandidal activity. Partial characterization of purified extract was carried out using High Performance Liquid Chromatography (HPLC and Fast Performance Liquid Chromatography (FPLC techniques. Result and Discussion: A. terreus was found to produce compound with anti-candidal and germ tube inhibitory activity against human pathogen Candida albicans at 200 mg ml-1. Further proteinase inhibitory activity of the extract, tested using plate assay and SDS-PAGE ensures the anti-candidal activity of the extract. Present study identified and confirmed the potential anticandidal activity, interms of germ tube and proteinase inhibititory activity, of metabolites produced by A. terreus st.1. Conclusion: The bio-assay guided fractionation and purification resulted in identification of unique fraction with active anti-candidal activity. Thus this fraction may serve as one of the lead to develop novel anti-candidal therapeutics.

  3. 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.

  4. Antifungal Activity of Eugenol against Penicillium, Aspergillus, and Fusarium Species.

    Science.gov (United States)

    Campaniello, Daniela; Corbo, Maria Rosaria; Sinigaglia, Milena

    2010-06-01

    The antifungal activity of eugenol in a model system against aspergilli (Aspergillus niger, Aspergillus terreus, and Emericella nidulans), penicilli (Penicillium expansum, Penicillium glabrum, and Penicillium italicum), and fusaria (Fusarium oxysporum and Fusarium avenaceum) was investigated. Minimum detection time (time to attain a colony diameter of 1 cm) and the kinetic parameters were evaluated. The effectiveness of the active compound seemed to be strain or genus dependent; 100 mg/liter represented a critical value for P. expansum, P. glabrum, P. italicum, A. niger, and E. nidulans because a further increase of eugenol resulted in fungistatic activity. The radial growth of A. terreus and F. avenaceum was inhibited at 140 mg/liter, and growth of F. oxysporum was completely inhibited at 150 mg/liter.

  5. A non-polyene antifungal antibiotic from Streptomyces albidoflavus PU 23

    Indian Academy of Sciences (India)

    S K Augustine; S P Bhavsar; B P Kapadnis

    2005-03-01

    In all 312 actinomycete strains were isolated from water and soil samples from different regions. All these isolates were purified and screened for their antifungal activity against pathogenic fungi. Out of these, 22% of the isolates exhibited activity against fungi. One promising strain, Streptomyces albidoflavus PU 23 with strong antifungal activity against pathogenic fungi was selected for further studies. Antibiotic was extracted and purified from the isolate. Aspergillus spp. was most sensitive to the antibiotic followed by other molds and yeasts. The antibiotic was stable at different temperatures and pH tested and there was no significant loss of the antifungal activity after treatment with various detergents and enzymes. Synergistic effect was observed when the antibiotic was used in combination with hamycin. The antibiotic was fairly stable for a period of 12 months at 4°C. The mode of action of the antibiotic seems to be by binding to the ergosterol present in the fungal cell membrane resulting in the leakage of intracellular material and eventually death of the cell. The structure of the antibiotic was determined by elemental analysis and by ultraviolet (UV), Fourier transform infrared (FTIR), nuclear magnetic resonance (NMR) and liquid chromatography mass spectra (LCMS). The antibiotic was found to be a straight chain polyhydroxy, polyether, non-proteinic compound with a single double bond, indicating a nonpolyene antifungal antibiotic.

  6. Plant latex: a promising antifungal agent for post harvest disease control.

    Science.gov (United States)

    Sibi, G; Wadhavan, Rashmi; Singh, Sneha; Shukla, Abhilasha; Dhananjaya, K; Ravikumar, K R; Mallesha, H

    2013-12-01

    Bioactive compounds from plant latex are potential source of antifungic against post harvest pathogens. Latex from a total of seven plant species was investigated for its phytochemical and antifungal properties. Six fungi namely Aspergillus fumigatus, A. niger, A. terreus, F. solani, P. digitatum and R. arrhizus were isolated from infected fruits and vegetables and tested against various solvent extracts of latex. Analysis of latex extracts with phytochemical tests showed the presence of alkaloids, flavonoids, glycosides, phenols, saponins, steroids, tannins and terpenoids. Antifungal assay revealed the potential inhibitory activity of petroleum ether extracts against the postharvest fungal isolates. Various degree of sensitivity was observed irrespective of plant species studied with A. terreus and P. digitatum as the most susceptible ones. F. solani and A. fumigatus were moderately sensitive to the latex extracts tested. Among the plants, latex of Thevetia peruviana (75.2%) and Artocarpus heterophyllus (64.8%) were having potential antifungal activity against the isolates followed by Manilkara zapota (51.1%). In conclusion, use of plant latex makes interest to control postharvest fungal diseases and is fitting well with the concept of safety for human health and environment.

  7. Investigation on mechanism of antifungal activity of eugenol against Trichophyton rubrum.

    Science.gov (United States)

    de Oliveira Pereira, Fillipe; Mendes, Juliana Moura; de Oliveira Lima, Edeltrudes

    2013-07-01

    Trichophyton rubrum is a worldwide agent responsible for chronic cases of dermatophytosis which have high rates of resistance to antifungal drugs. Attention has been drawn to the antimicrobial activity of aromatic compounds because of their promising biological properties. Therefore, we investigated the antifungal activity of eugenol against 14 strains of T. rubrum which involved determining its minimum inhibitory concentration (MIC) and effects on mycelial growth (dry weight), conidial germination and morphogenesis. The effects of eugenol on the cell wall (sorbitol protect effect) and the cell membrane (release of intracellular material, complex with ergosterol, ergosterol synthesis) were investigated. Eugenol inhibited the growth of 50% of T. rubrum strains employed in this study at an MIC = 256 μg/ml, as well as mycelial growth and conidia germination. It also caused abnormalities in the morphology of the dermatophyte in that we found wide, short, twisted hyphae and decreased conidiogenesis. The results of these studies on the mechanisms of action suggested that eugenol exerts antifungal effects on the cell wall and cell membrane of T. rubrum. Eugenol act on cell membrane by a mechanism that seems to involve the inhibition of ergosterol biosynthesis. The lower ergosterol content interferes with the integrity and functionality of the cell membrane. Finally, our studies support the potential use of the eugenol as an antifungal agent against T. rubrum.

  8. In Vitro Antifungal Activity of Sanguinarine and Chelerythrine Derivatives against Phytopathogenic Fungi

    Directory of Open Access Journals (Sweden)

    Yan-Ni Ma

    2012-11-01

    Full Text Available In order to understand the antifungal activity of some derivatives of sanguinarine (S and chelerythrine (C and their structure-activity relationships, sixteen derivatives of S and C were prepared and evaluated for in vitro antifungal activity against seven phytopathogenic fungi by the mycelial growth rate method. The results showed that S, C and their 6-alkoxy dihydro derivatives S1–S4, C1–C4 and 6-cyanodihydro derivatives S5, C5 showed significant antifungal activity at 100 µg/mL against all the tested fungi. For most tested fungi, the median effective concentrations of S, S1, C and C1 were in a range of 14–50 µg/mL. The structure-activity relationship showed that the C=N+ moiety was the determinant for the antifungal activity of S and C. S1–S5 and C1–C5 could be considered as the precursors of S and C, respectively. Thus, the present results strongly suggested that S and C or their derivatives S1–S5 and C1–C5 should be considered as good lead compounds or model molecules to develop new anti-phytopathogenic fungal agents.

  9. 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.

  10. In-vitro antibacterial, antifungal and cytotoxic properties of metal-based furanyl derived sulfonamides.

    Science.gov (United States)

    Chohan, Zahid H; Shaikh, Ali U; Naseer, Muhammad M; Supuran, Claudiu T

    2006-12-01

    A new series of antibacterial and antifungal furanyl-derived sulfonamides and their cobalt (II), copper (II), nickel (II) and zinc (II) metal complexes have been synthesized, characterized and screened for their in-vitro antibacterial activity against four Gram-negative (Escherichia coli, Shigella flexneri, Pseudomonas aeruginosa and Salmonella typhi) and two Gram-positive (Bacillus subtilis and Staphylococcus aureus) bacterial strains and, for in-vitro antifungal activity against Trichophyton longifusus, Candida albicans, Aspergillus flavus, Microsporum canis, Fusarium solani and Candida glaberata. The results of these studies revealed that all compounds showed significant to moderate antibacterial activity. However, the zinc (II) complexes were found to be comparatively much more active as compared to the others. For antifungal activity generally, compounds (22) and (24) showed significant activity against Escherichia coli (a), (6) against Shigella flexeneri (b), (16) and (22) against Pseudomonas aeruginosa (c), (14) and (16) against Salmonella typhi (d), (9) against Staphylococcus aureus (e) and, (14) and (16) against Bacillus subtilis (f) fungal strains. The brine shrimp (Artemia salina) bioassay was also carried out to study their in-vitro cytotoxic properties. Only three compounds, (6), (10) and (23) displayed potent cytotoxic activity with LD50 = 1.8535 x 10(-4), 1.8173 x 10(-4) and 1.9291 x 10(-4) respectively.

  11. Antifungal activity of diketopiperazines and stilbenes against plant pathogenic fungi in vitro.

    Science.gov (United States)

    Kumar, S Nishanth; Nambisan, Bala

    2014-01-01

    The present study aimed to investigate antifungal activity of a stilbene and diketopiperazine compounds against plant pathogenic fungi, including Phytophthora capsici, P. colocasiae, Botrytis cinerea and Colletotrichum gloeosporioides. Minimal inhibition concentrations (MIC) and minimal fungicidal concentrations (MFC) of stilbenes and diketopiperazines for each fungus were determined using microplate method. Best activity was recorded by stilbenes against P. capsici and P. colocasiae. All four test compounds were effective in inhibiting different stages of the life cycle of test fungi. Stilbenes were more effective than diketopiperazines in inhibiting mycelial growth and inhibiting different stages of the life cycle of P. capsici and P. colocasiae. Rupture of released zoospores induced by stilbenes was reduced by addition of 100 mM glucose. The effects of stilbenes on mycelial growth and zoospore release, but not zoospore rupture, were reduced largely when pH value was above 7. In addition, stilbenes were investigated for its antifungal stability against Phytophthora sp. The results showed that stilbenes maintained strong fungistatic activity over a wide pH range (pH 4–9) and temperature range (70–120 °C). The compound stilbenes exhibited strong and stable broad-spectrum antifungal activity, and had a significant fungicidal effect on fungal cells. Results from prebiocontrol evaluations performed to date are probably useful in the search for alternative approaches to controlling serious plant pathogens.

  12. NATURAL POLYACETYLENE COMPOUNDS

    Directory of Open Access Journals (Sweden)

    D. A. Konovalov

    2014-01-01

    Full Text Available Polyacetylenes (polyynes are compounds which contain two or more triple bonds in its structure. About 2 000 different polyacetylenes and biogenetically related substances were identified in 24 families of higher plants. However, most of these compounds were found in seven families of flowering plants: Apiaceae (Umbelliferae, Araliaceae, Asteraceae (Compositae, Campanulaceae, Olacaceae, Pittosporaceae and Santalaceae. Polyacetylenes are relatively unstable, chemically and biologically active compounds, and present in fungi, microorganisms, marine invertebrates and other organisms except for plants. Acetylenes form distinct specialized group of chemically active natural compounds, which are biosynthesized in plants of unsaturated fatty acids. In addition to widespread aliphatic polyacetylenes thiophenes dithiacyclohexadienes (thiarubrines, thioethers, sulphoxides, sulphones, alkamides, chlorohydrins, lactones, spiroacetal enol ethers, furans, pyrans, tetrahydropyrans, isocoumarins, aromatic acetylenes were also found in plant species. Polyacetylenes are localized in different plant organs, and can be found both individually and as a compound with carbohydrates, terpene, phenolic and other compounds. Many polyacetylenes are found in the composition of the essential oils of plants and it confirms their strongly marked ecological functions. From biological point of view these compounds are often synthesized by plants as toxic or bitter antifeedants, allelopathic compounds, phytoalexins or broadly antibiotic components. Polyynes are strong photosensitizers. They exhibit anti-inflammatory, anti-coagulant, anti-bacterial, antituberculosis, anti-fungal, anti-viral, neuroprotective and neurotoxic activity. Immunostimulatory influence associated with certain allergenicity of some of these substances was established. Therefore, without a doubt polyacetylenes are of interest for the modern pharmacy and medicine.

  13. Antifungal membranolytic activity of the tyrocidines against filamentous plant fungi.

    Science.gov (United States)

    Rautenbach, Marina; Troskie, Anscha M; Vosloo, Johan A; Dathe, Margitta E

    2016-11-01

    The tyrocidines and analogues are cyclic decapeptides produced by Brevibacillus parabrevis with a conserved sequence of cyclo(D-Phe(1)-Pro(2)-X(3)-x(4)-Asn(5)-Gln(6)-X(7)-Val(8)-X(9)-Leu(10)) with Trp(3,4)/Phe(3,4) in the aromatic dipeptide unit, Lys(9)/Orn(9) as their cationic residue and Tyr (tyrocidines), Trp (tryptocidines) or Phe (phenicidines) in position 7. Previous studies indicated they have a broad antifungal spectrum with the peptides containing a Tyr residue in position 7 being more active than those with a Phe or Trp residue in this position. Detailed analysis of antifungal inhibition parameters revealed that Phe(3)-D-Phe(4) in the aromatic dipeptide unit lead to more consistent activity against the three filamentous fungi in this study. These peptides exhibited high membrane activity and fast leakage kinetics against model membranes emulating fungal membranes, with selectivity towards ergosterol containing membranes. More fluid membranes and doping of liposomes with the sphingolipid, glucosylceramide, led to a decreased permeabilising activity. Peptide-induced uptake of membrane impermeable dyes was observed in hyphae of both Fusarium solani and Botrytis cinerea, with uptake more pronounced at the hyphal growth tips that are known to contain ergosterol-sphigolipid rich lipid rafts. Tyrocidine interaction with these rafts may lead to the previously observed fungal hyperbranching. However, the leakage of model membranes and Bot. cinerea did not correlate directly with the antifungal inhibition parameters, indicating another target or mode of action. Proteinase K treatment of target fungi had a minimal influence or even improved the tyrocidine activity, ruling out a mannoprotein target in the fungal cell wall. β-glucanase treatment of Bot. cinerea did not significantly affect the tyrocidine activity, but there was a significant loss in activity towards the β-glucanase treated F. solani. This study showed the tyrocidine antifungal membrane activity is

  14. Synthesis, Characterization and Antifungal Evaluation of 5-Substituted-4-Amino-1,2,4-Triazole-3-Thioesters

    Directory of Open Access Journals (Sweden)

    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.

  15. Polyketide and benzopyran compounds of an endophytic fungus isolated from Cinnamomum mollissimum:biological activity and structure

    Institute of Scientific and Technical Information of China (English)

    Carolina Santiago; Lin Sun; Murray Herbert Gibson Munro; Jacinta Santhanam

    2014-01-01

    Objective:To study bioactivity and compounds produced by an endophytic Phoma sp. fungus isolated from the medicinal plant Cinnamomum mollissimum. Methods: Compounds produced by the fungus were extracted from fungal broth culture with ethyl acetate. This was followed by bioactivity profiling of the crude extract fractions obtained via high performance liquid chromatography. The fractions were tested for cytotoxicity to P388 murine leukemic cells and antimicrobial activity against bacteria and pathogenic fungi. Compounds purified from active fractions which showed antibacterial, antifungal and cytotoxic activities were identified using capillary nuclear magnetic resonance analysis, mass spectrometry and admission to AntiMarin database. Results: Three known compounds, namely 4-hydroxymellein, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one and 1-(2,6-dihydroxyphenyl) ethanone, were isolated from the fungus. The polyketide compound 4-hydroxymellein showed high inhibitory activity against P388 murine leukemic cells (94.6%) and the bacteria Bacillus subtilis (97.3%). Meanwhile, 4,8-dihydroxy-6-methoxy-3-methyl-3,4-dihydro-1H-isochromen-1-one, a benzopyran compound, demonstrated moderate inhibitory activity against P388 murine leukemic cells (48.8%) and the fungus Aspergillus niger (56.1%). The second polyketide compound, 1 (2,6-dihydroxyphenyl) ethanone was inactive against the tested targets. Conclusions: These findings demonstrate the potential of endophytes as producers of pharmacologically important compounds, including polyketides which are major secondary metabolites in fungi.

  16. Lipid-based antifungal agents: current status.

    Science.gov (United States)

    Arikan, S; Rex, J H

    2001-03-01

    Immunocompromised patients are well known to be predisposed to developing invasive fungal infections. These infections are usually difficult to diagnose and more importantly, the resulting mortality rate is high. The limited number of antifungal agents available and their high rate of toxicity are the major factors complicating the issue. However, the development of lipid-based formulations of existing antifungal agents has opened a new era in antifungal therapy. The best examples are the lipid-based amphotericin B preparations, amphotericin B lipid complex (ABLC; Abelcet), amphotericin B colloidal dispersion (ABCD; Amphotec or Amphocil), and liposomal amphotericin B (AmBisome). These formulations have shown that antifungal activity is maintained while toxicity is reduced. This progress is followed by the incorporation of nystatin into liposomes. Liposomal nystatin formulation is under development and studies of it have provided encouraging data. Finally, lipid-based formulations of hamycin, miconazole, and ketoconazole have been developed but remain experimental. Advances in technology of liposomes and other lipid formulations have provided promising new tools for management of fungal infections.

  17. 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

  18. Tin(IV) complexes of pyrrolidinedithiocarbamate: synthesis, characterisation and antifungal activity.

    Science.gov (United States)

    Menezes, D C; Vieira, F T; de Lima, G M; Porto, A O; Cortés, M E; Ardisson, J D; Albrecht-Schmitt, T E

    2005-12-01

    The reaction of ammonium pyrrolidinedithiocarbamate, [NH4{S2CN(CH2)4}], with SnCl2, [Sn(C6H5)2Cl2], [Sn(C6H5)3Cl], [Sn(C4H9)2Cl2] and [Sn(C6H11)3Cl] produced in good yield the compounds [Sn{S2CN(CH2)4}2Cl2] (1), [Sn{S2CN(CH2)4}2Ph2] (2), [Sn{S2CN(CH2)4}Ph3] (3), [Sn{S2CN(CH2)4}2 n-Bu2] (4) and [Sn{S2CN(CH2)4}Cy3] (5). The complexes were characterised by infrared, multinuclear NMR (1H, 13C{1H} and 119Sn{1H}) and 119Sn Mössbauer spectroscopies. In addition, the crystal structure of 4 was determined by X-ray crystallography. The in vitro antifungal activity of the tin(IV) complexes as well of the ligand was performed on human pathogenic fungi, Candida albicans, in concentrations of 0.025; 0.050; 0.100; 0.200; 0.400; 0.800; 1.600 and 3.200 mM. The microorganism presented resistance to the dithiocarbamate ligand and all tin(IV) complexes tested were actives. The highest activity was found for compounds 1 and 4.

  19. 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).

  20. Determination of antifungal susceptibility patterns among the environmental isolates of Aspergillus fumigatus in Iran

    Science.gov (United States)

    Mohammadi, Faezeh; Dehghan, Parvin; Nekoeian, Shahram; Hashemi, Seyed Jamal

    2016-01-01

    Background: In recent years, triazole-resistant environmental isolates of Aspergillus fumigatus have emerged in Europe and Asia. Azole resistance has been reported in patients who are treated with long-term azole therapy or exposure of the fungus spores to the azole fungicides used in agriculture. To date, a wide range of mutations in A. fumigatus have been described conferring azole-resistance, which commonly involves modifications in the cyp51A gene. We investigated antifungal susceptibility pattern of environmental isolates of A. fumigatus. Materials and Methods: In this study, 170 environmental samples collected from indoors surfaces of three hospitals in Iran. It was used β-tubulin gene to confirm the all of A. fumigatus isolates, which was identified by conventional methods. Furthermore, the antifungal susceptibility of itraconazole, voriconazole, and posaconazole was investigated using broth microdilution test, according to European Committee on Antimicrobial Susceptibility testing reference method. Results: From a total of 158 environmental molds fungi obtained from the hospitals, 58 isolates were identified as A. fumigatus by amplification of expected size of β-tubulin gene (~500 bp). In this study, in vitro antifungal susceptibility testing has shown that there were not high minimum inhibitory concentration values of triazole antifungals in all of the 58 environmental isolates of A. fumigatus. Conclusion: Our findings demonstrated that there was not azole-resistant among environmental isolates of A. fumigatus. Medical triazoles compounds have structural similarity with triazole fungicide compounds in agriculture, therefore, resistance development through exposure to triazole fungicide compounds in the environment is important but it sounds there is not a serious health problem in drug resistance in environmental isolates in Iran. PMID:27656605

  1. Antifungal activity of 4-substituted crotonic acid esters.

    Science.gov (United States)

    Gershon, H; Shanks, L; Gawiak, D E

    1976-08-01

    Twenty-three 4-substituted crotonic acid esters were tested for antifungal activity against Candida albicans, Aspergillus niger, Mucor mucedo, and Trichophyton mentagrophytes. For the analogues of the methyl ester containing substituents in the 4 position, the following order of fungitoxicity was observed: I greater than Br greater than Cl greater than CH3S greater than CH3O greater than F=H. Of the homologues of the esters of the 4-iodo and 4-bromo compounds which included methyl, ethyl, n-propyl, n-butyl, n-pentyl, and n-hexyl, ethyl 4-iodocrotonate was most toxic to the four fungi at pH 7.0 in the presence of 10% beef serum (C. albicans, 18mug/ml, A. niger, 40 mug/ml, M. mucedo, 5 mug/ml, T. mentagrophytes, 4 mug/ml). It is believed that the mechanism of fungitoxicity is due, in part, to a nucleophilic reaction involving SH-containing compounds. This is based on the correlation of fungitoxicity with the order of leaving groups in the nucleophilic reaction and the protection against the toxicity of the test compounds to the fungi by cysteine and glutathione.

  2. 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.

  3. Comments on 'Organic sulphur compounds produced by flash pyrolysis of Timhadit oil shale' by M. Ishiwatari, H. Sakashita, T. Tatsumi and H-O. Tominaga

    NARCIS (Netherlands)

    Sinninghe Damsté, J.S.

    1991-01-01

    Since we have analysed three different stratigraphic units of the Timhadit oil shale for sulphur compounds by means of pyrolysis-gas chromatography (Eglinton and Sinninghe DamstC, unpublished results), we believe that the identification by Ishiwatari et al. is not correct. In a recent paper we demon

  4. Antitumor and antifungal activities of organic extracts of seacucumber Holothuria atra from the southeast coast of India

    Science.gov (United States)

    Dhinakaran, Devaraj Isaac; Lipton, Aaron Premnath

    2015-02-01

    In phylum Echinodermata, the family Holothuridae is distinguished by its capacity of bioactive compounds. Sea cucumber Holothuria atra is commonly known as the lollyfish. The antifungal activity was detected using agar well diffusion method against the various fungal strains such as Trichoderma viride, Aspergillus niger, Aspergillus flavis, Candida albicans and Penicillium chrysogenum. Relatively high antifungal activity was seen against Candida albicans at 100 μL-1 concentration of extracts. Zone of inhibition was measured at 18 mm of diameter. The anti-tumor activities were detected against the Vero and Hep2 cell lines using MTT assay. The cells were treated with H. atra extract at concentrations 0.078-10mg mL-1. The extract showed high proliferative activity against the Hep2 cells. The body wall extracts of sea cucumber ( H. atra) showed effective antifungal and antitumor activities. All these findings suggest that the extracts could be used for the development of drugs.

  5. 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.

  6. 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.

  7. In vitro antifungal activity of hydroxychavicol isolated from Piper betle L

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    Afrin Farhat

    2010-02-01

    Full Text Available Abstract Background Hydroxychavicol, isolated from the chloroform extraction of the aqueous leaf extract of Piper betle L., (Piperaceae was investigated for its antifungal activity against 124 strains of selected fungi. The leaves of this plant have been long in use tropical countries for the preparation of traditional herbal remedies. Methods The minimum inhibitory concentration (MIC and minimum fungicidal concentration (MFC of hydroxychavicol were determined by using broth microdilution method following CLSI guidelines. Time kill curve studies, post-antifungal effects and mutation prevention concentrations were determined against Candida species and Aspergillus species "respectively". Hydroxychavicol was also tested for its potential to inhibit and reduce the formation of Candida albicans biofilms. The membrane permeability was measured by the uptake of propidium iodide. Results Hydroxychavicol exhibited inhibitory effect on fungal species of clinical significance, with the MICs ranging from 15.62 to 500 μg/ml for yeasts, 125 to 500 μg/ml for Aspergillus species, and 7.81 to 62.5 μg/ml for dermatophytes where as the MFCs were found to be similar or two fold greater than the MICs. There was concentration-dependent killing of Candida albicans and Candida glabrata up to 8 × MIC. Hydroxychavicol also exhibited an extended post antifungal effect of 6.25 to 8.70 h at 4 × MIC for Candida species and suppressed the emergence of mutants of the fungal species tested at 2 × to 8 × MIC concentration. Furthermore, it also inhibited the growth of biofilm generated by C. albicans and reduced the preformed biofilms. There was increased uptake of propidium iodide by C. albicans cells when exposed to hydroxychavicol thus indicating that the membrane disruption could be the probable mode of action of hydroxychavicol. Conclusions The antifungal activity exhibited by this compound warrants its use as an antifungal agent particularly for treating topical

  8. In Vitro and In Vivo Antifungal Activity of Lichochalcone-A against Candida albicans Biofilms

    Science.gov (United States)

    Seleem, Dalia; Benso, Bruna; Noguti, Juliana; Pardi, Vanessa; Murata, Ramiro Mendonça

    2016-01-01

    Oral candidiasis (OC) is an opportunistic fungal infection with high prevalence among immunocompromised patients. Candida albicans is the most common fungal pathogen responsible for OC, often manifested in denture stomatitis and oral thrush. Virulence factors, such as biofilms formation and secretion of proteolytic enzymes, are key components in the pathogenicity of C. albicans. Given the limited number of available antifungal therapies and the increase in antifungal resistance, demand the search for new safe and effective antifungal treatments. Lichochalcone-A is a polyphenol natural compound, known for its broad protective activities, as an antimicrobial agent. In this study, we investigated the antifungal activity of lichochalcone-A against C. albicans biofilms both in vitro and in vivo. Lichochalcone-A (625 μM; equivalent to 10x MIC) significantly reduced C. albicans (MYA 2876) biofilm growth compared to the vehicle control group (1% ethanol), as indicated by the reduction in the colony formation unit (CFU)/ml/g of biofilm dry weight. Furthermore, proteolytic enzymatic activities of proteinases and phospholipases, secreted by C. albicans were significantly decreased in the lichochalcone-A treated biofilms. In vivo model utilized longitudinal imaging of OC fungal load using a bioluminescent-engineered C. albicans (SKCa23-ActgLUC) and coelenterazine substrate. Mice treated with lichochalcone-A topical treatments exhibited a significant reduction in total photon flux over 4 and 5 days post-infection. Similarly, ex vivo analysis of tongue samples, showed a significant decrease in CFU/ml/mg in tongue tissue sample of lichochalcone-A treated group, which suggest the potential of lichochalcone-A as a novel antifungal agent for future clinical use. PMID:27284694

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

    Science.gov (United States)

    Benso, Bruna; Pardi, Vanessa

    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. PMID:27366648

  10. PHYTOCHEMICAL SCREENING AND IN-VITRO ANTIFUNGAL INVESTIGATION OF PARTHENIUM HYSTEROPHORUS EXTRACTS AGAINST ALTERNARIA ALTERNATA

    Directory of Open Access Journals (Sweden)

    Singh Padma

    2013-07-01

    Full Text Available The extensive use of fungicides are polluting the environment and giving rise to undesirable biological effects on animal and human beings. Therefore use of plant extracts as biological control agents is being popularized in recent years. Alternaria alternata is reported for causing foliage disease in several important vegetables and crops. In an approach towards the development of eco friendly antifungal compound for controlling plant diseases caused by Alternaria alternata different extracts of Parthenium hysterophorus were tested for their antifungal potential. Parthenium hysterophorus is considered as an obnoxious weed, growing on waste land. The four different solvent extracts viz., aqueous, methanol, acetone and ethanol extracts of leaves of Parthenium hysterophorus was evaluated from antifungal potential against four different isolates of Alternaria alternata isolated from potato (Solanum tuberosum, onion (Allium cepa, tomato (Lycopersicon esculentum and mustard (Brassica compestris by food poison technique. The ethanolic extract showed complete inhibition against the four isolates i.e. 100 % followed by acetone and methanol extracts which was approximately 96 % and 76 % respectively, while aqueous extract do not showed any antifungal activity. Thus the result showed that the ethanolic extract was the best extract to be used. The phytochemical analysis revealed the presence of alkaloid, glycoside, steroid, saponin in varying concentration in different extracts which might be the cause of antifungal potential. The present study supports the use of leaf extract of Parthenium hysterophorus as biofungicides for the disease caused by Alternaria alternata. This will help to save the environment from chemical hazards as most of the synthetic fungicide constitute mercury, zinc etc which are toxic for nature.

  11. Antifungal New Oxepine-Containing Alkaloids and Xanthones from the Deep-Sea-Derived Fungus Aspergillus versicolor SCSIO 05879.

    Science.gov (United States)

    Wang, Junfeng; He, Weijun; Huang, Xiaolong; Tian, Xinpeng; Liao, Shengrong; Yang, Bin; Wang, Fazuo; Zhou, Xiaojiang; Liu, Yonghong

    2016-04-13

    Phytopathogenic fungi remain a continuous and huge threat in the agricultural fields. The agrochemical industry has made great development of the use of microbial natural products, which has been regarded as an effective strategy against phytopathogenic fungi. Antifungal bioassay-directed fractionation was used to isolate two new oxepine-containing alkaloids (1 and 2), two new 4-aryl-quinolin-2-one alkaloids (3 and 4), and four new prenylated xanthones (5-8) from the deep-sea-derived fungus Aspergillus versicolor SCSIO 05879. Extensive NMR spectroscopic analysis, quantum mechanical calculations, and X-ray single-crystal diffraction were used to elucidate their structures, including their absolute configurations. Versicoloids A and B, versicone A, and cottoquinazoline A showed antifungal activities against three phytopathogenic fungi. The antifungal activities of these bioactive compounds strongly depend on the fungal species. Especially versicoloids A and B showed strong fungicidal effect (MIC of 1.6 μg/mL) against Colletotrichum acutatum, compared with that of the positive control cycloheximide (MIC of 6.4 μg/mL). The results of antifungal experiments indicated that versicoloids A and B may be regarded as candidate agents of antifungal agrochemicals.

  12. 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.

  13. Identification of a New Class of Antifungals Targeting the Synthesis of Fungal Sphingolipids

    Science.gov (United States)

    Mor, Visesato; Rella, Antonella; Farnoud, Amir M.; Singh, Ashutosh; Munshi, Mansa; Bryan, Arielle; Naseem, Shamoon; Konopka, James B.; Ojima, Iwao; Bullesbach, Erika; Ashbaugh, Alan; Linke, Michael J.; Cushion, Melanie; Collins, Margaret; Ananthula, Hari Krishna; Sallans, Larry; Desai, Pankaj B.; Wiederhold, Nathan P.; Fothergill, Annette W.; Kirkpatrick, William R.; Patterson, Thomas; Wong, Lai Hong; Sinha, Sunita; Giaever, Guri; Nislow, Corey; Flaherty, Patrick; Pan, Xuewen; Cesar, Gabriele Vargas; de Melo Tavares, Patricia; Frases, Susana; Miranda, Kildare; Rodrigues, Marcio L.; Luberto, Chiara; Nimrichter, Leonardo

    2015-01-01

    ABSTRACT Recent estimates suggest that >300 million people are afflicted by serious fungal infections worldwide. Current antifungal drugs are static and toxic and/or have a narrow spectrum of activity. Thus, there is an urgent need for the development of new antifungal drugs. The fungal sphingolipid glucosylceramide (GlcCer) is critical in promoting virulence of a variety of human-pathogenic fungi. In this study, we screened a synthetic drug library for compounds that target the synthesis of fungal, but not mammalian, GlcCer and found two compounds [N′-(3-bromo-4-hydroxybenzylidene)-2-methylbenzohydrazide (BHBM) and its derivative, 3-bromo-N′-(3-bromo-4-hydroxybenzylidene) benzohydrazide (D0)] that were highly effective in vitro and in vivo against several pathogenic fungi. BHBM and D0 were well tolerated in animals and are highly synergistic or additive to current antifungals. BHBM and D0 significantly affected fungal cell morphology and resulted in the accumulation of intracellular vesicles. Deep-sequencing analysis of drug-resistant mutants revealed that four protein products, encoded by genes APL5, COS111, MKK1, and STE2, which are involved in vesicular transport and cell cycle progression, are targeted by BHBM. PMID:26106079

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

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    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.

  15. 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.

  16. 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.

  17. 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.

  18. 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. PMID:27031728

  19. OTYPIC CHARACTERIZATION AND ANTIFUNGAL SUSCEPTIBILITY PATTERN OF CANDIDA SP ISOLATED FROM A TERTIARY CARE CENTER

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    Rudramurthy

    2014-02-01

    Full Text Available ACT: Candida , a yeast like ubiquitous fungus , is an endogenous species which produces commonest fungal infection; Candidiasis. Resistance to antifungal agents is an alarming sign for the emerging common nosocomial candidiasis. MATERIALS AND METHODS: Various types of specimens we re collected from the c linically suspected cases of candidiasis. Isolation and characterization of candida sp . was done by standard procedures. Antifungal susceptibility was done by disc diffusion method. RESULT: The candida was isolated from various clinical specimens , vaginal swab (24.66% , skin scraping (13.33% oral swabs (12.66% , ear swabs ( 11.33% , nail scraping (10% , and pus from diabetes foot ulcer and post - operative wound infection ( 8% , sputum ( 6% , urine (4.66% , stool ( 4% , blood ( 2.66% , and eye swabs ( 2.66%. Amon g different species of candida isolated C.albicans was the predominant species (79.33% followed by C tropicalis (19.33% and C.Guilliermondii (1.33%. Antifungal resistance of different species of candida was higher to fluconazole . The least resistance wa s seen with amphotericin - B (1.33%. CONCLUSION: The increased isolation of candida species and development of resistance to commonly used antifungal drugs requires careful interpretation and the in vitro susceptibility testing. This facilitates better pat ient care.

  20. 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-...

  1. Synthesis,Characterization and Biological Activities of Novel Acrylamide Compounds

    Institute of Scientific and Technical Information of China (English)

    XU Liang-zhong; XU Zhong-jie; ZHANG Gong-sheng; ZHOU Kai; ZHAI Zhi-wei

    2008-01-01

    With dimethomorph and flumorph as the leading compounds,four novel acrylamide compounds with two types of structure were designed and synthesized by means of the method of"me too chemistry".The target compounds were characterized by 1H NMR,IR,MS,and elemental analysis.The influences of solvent and raw material on the yield were investigated and optimum processing conditions were determined.The results of preliminary biological tests show that all those compounds exhibit certain antifungal activities.

  2. Azide-enolate 1,3-dipolar cycloaddition in the synthesis of novel triazole-based miconazole analogues as promising antifungal agents.

    Science.gov (United States)

    González-Calderón, Davir; Mejía-Dionicio, María G; Morales-Reza, Marco A; Ramírez-Villalva, Alejandra; Morales-Rodríguez, Macario; Jauregui-Rodríguez, Bertha; Díaz-Torres, Eduardo; González-Romero, Carlos; Fuentes-Benítes, Aydeé

    2016-04-13

    Seven miconazole analogs involving 1,4,5-tri and 1,5-disubstituted triazole moieties were synthesized by azide-enolate 1,3-dipolar cycloaddition. The antifungal activity of these compounds was evaluated in vitro against four filamentous fungi, including Aspergillus fumigatus, Trichosporon cutaneum, Rhizopus oryzae, and Mucor hiemalis as well as three species of Candida spp. as yeast specimens. These pre-clinical studies suggest that compounds 4b, 4d and 7b can be considered as drug candidates for future complementary biological studies due to their good/excellent antifungal activities.

  3. 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.

  4. A new furoquinoline alkaloid with antifungal activity from the leaves of Ruta chalepensis L.

    Science.gov (United States)

    Emam, A; Eweis, M; Elbadry, M

    2010-12-01

    Bioassay-guided separation with an eye toward antifungal activity led to the isolation of the new alkaloid 5-(1̀,1̀-dimethylallyl)-8-hydroxyfuro[2-3-b] quinoline (1) and the known biscoumarin daphnoretin (2) as the active constituents of the chloroform extract obtained from the leaves of Ruta chalepensis. The structures of the metabolites were elucidated on the basis of their spectral characteristics (NMR, UV, and MS) and were compared with the literature. The antifungal activity of the isolated compounds was evaluated against the phytopathogenic fungi Rhizoctonia solani, Sclerotium rolfsii, and Fusarium solani, which cause root-rot and wilt diseases in several economically important food crops such as potato, sugar beet, and tomato.

  5. Antifungal Depsidone Metabolites from Cordyceps dipterigena, an Endophytic Fungus Antagonistic to the Phytopathogen Gibberella fujikuroi

    Science.gov (United States)

    Varughese, Titto; Riosa, Nivia; Higginbotham, Sarah; Arnold, A. Elizabeth; Coley, Phyllis D.; Kursar, Thomas A.; Gerwick, William H.; Cubilla Rios, L.

    2012-01-01

    Among thirty four endophytic fungal strains screened for in vitro antagonism, the endophytic fungus Cordyceps dipterigena was found to strongly inhibit mycelial growth of the plant pathogenic fungus Gibberella fujikuroi. Two new depsidone metabolites, cordycepsidone A (1) and cordycepsidone B (2), were isolated from the PDA culture extract of C. dipterigena and identified as being responsible for the antifungal activity. Elucidation of their chemical structures was carried out using 1D and 2D NMR spectroscopy in combination with IR and MS spectroscopic data. Cordycepsidone A displayed strong and dose-dependent antifungal activity against the plant pathogenic fungus Gibberella fujikuroi. The isolates were inactive in bioassays for malaria (Plasmodium falciparum), leishmaniasis (Leishmania donovani), Chagas’s disease (Trypanosoma cruzi), and cytotoxicity at 10 μg/mL. The compounds were also found to be inactive against several bacterial strains at 50 μg/mL. PMID:22707798

  6. In vitro antioxidant, antifungal and cytotoxic activity of methanolic extract of Calligonum polygonoides

    Directory of Open Access Journals (Sweden)

    Arif Khan

    2015-06-01

    Full Text Available Present study is aimed at the pharmacological characterization of methanol extract of Calligonum polygonoides from District Bannu. Dried plant was grounded and extracted with methanol to prepare methanol crud extract. In vitro biological assays were conducted using this methanolic extract according to standard protocol. Cytotoxic activity of plant methanolic extract against brine shrimps while antifungal activity was also measured. Eighty percent death rate of brine shrimp was observed at 1,000 μg/mL of plant extract. 70 ± 0.0% growth inhibition of Aspergillus niger was measured during the present study. Significant scavenging results were observed during scavenging of free radicles viz; 78.1% against DPPH, 83.1% to ABTS and 36% against superoxide at 500 μg/mL were obtained. The results obtained in this study indicate that C. polygonoides possess significant antioxidant, antifungal and cytotoxic bioactive compounds.

  7. Synthesis, Spectral Characterization, and Antibacterial and Antifungal Studies of PANI/V2O5 Nanocomposites

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    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.

  8. Antifungal Activity of Coumarin from Ageratum conyzoides L. Leaves on Candida albicans cells

    Directory of Open Access Journals (Sweden)

    Gunawan Pamudji Widodo

    2012-07-01

    Full Text Available The aim of this study was to identify the antifungal activity of coumarin isolated from Ageratum conyzoides L. leaves and to observe its influence on Candida albicans cells by scanning electron microscope (SEM and transmission electron microscope (TEM. Antifungal activity testing by disk diffusion method showed coumarin was active toward pathogenic fungus, Candida albicans with the MIC value of coumarin of 125 g mL-1. The influence of this substance on C. albicans cells was observed by scanning and transmission electron microscopies. The result showed that this compound damaged the cell by pores formation on the cell wall. The death of cells occurred due to leakage and necrotic of cytoplasmic content.

  9. Antibacterial, antifungal and antiviral activity of propolis of different geographic origin.

    Science.gov (United States)

    Kujumgiev, A; Tsvetkova, I; Serkedjieva, Y; Bankova, V; Christov, R; Popov, S

    1999-03-01

    Propolis samples from different geographic origins were investigated for their antibacterial (against Staphylococcus aureus and Escherichia coli), antifungal (against Candida albicans) and antiviral (against Avian influenza virus) activities. All samples were active against the fungal and Gram-positive bacterial test strains, and most showed antiviral activity. The activities of all samples were similar in spite of the differences in their chemical composition. In samples from the temperate zone, flavonoids and esters of phenolic acids are known to be responsible for the above mentioned activities of bee glue; tropical samples did not contain such substances but showed similar activities. Obviously, in different samples, different substance combinations are essential for the biological activity of the bee glue. It seems that propolis has general pharmacological value as a natural mixture and not as a source of new powerful antimicrobial, antifungal and antiviral compounds.

  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; Li, You-Zhi

    2015-12-01

    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.

  11. Antifungal activity of amphotericin B conjugated to carbon nanotubes.

    Science.gov (United States)

    Benincasa, Monica; Pacor, Sabrina; Wu, Wei; Prato, Maurizio; Bianco, Alberto; Gennaro, Renato

    2011-01-25

    Amphotericin B (AMB) has long been considered the most effective drug in the treatment of serious invasive fungal infections. There are, however, major limitations to its use, due to several adverse effects, including acute infusional reactions and, most relevant, a dose-dependent nephrotoxicity. At least some of these effects are attributed to the aggregation of AMB as a result of its poor water solubility. To overcome this problem, reformulated versions of the drug have been developed, including a micellar dispersion of AMB with sodium deoxycholate (AMBD), its encapsulation into liposomes, or its incorporation into lipidic complexes. The development of nanobiotechnologies provides novel potential drug delivery systems that make use of nanomaterials such as functionalized carbon nanotubes (f-CNTs), which are emerging as an innovative and efficient tool for the transport and cellular translocation of therapeutic molecules. In this study, we prepared two conjugates between f-CNTs and AMB. The an