Biological activity of the azlactone derivative EPA-35 against Trypanosoma cruzi.

Abstract:

:Chagas disease, caused by Trypanosoma cruzi, affects six to seven million people worldwide. Treatment is based on benznidazole, producing several side effects and debatable efficacy, highlighting the need for new alternative drugs. We investigated the activity of four C-4 functionalized azlactone derivatives (EPA-27, EPA-35, EPA-63 and EPA-91) as potential T. cruzi inhibitors. Screening with epimastigotes indicated EPA-35 as the best compound (IC50/24 h: 33 μM). This compound was 14.1 times more potent against intracellular amastigotes (IC50/24 h: 2.34 μM). Treatment of infected Vero cells for 72 h (up to 30 μM EPA-35) resulted in a dose-dependent decrease in number of trypomastigotes and amastigotes released in the supernatant, but the amastigote/trypomastigote ratio remained constant, indicating that amastigote growth was disturbed, but cell differentiation was unaffected. Analysis of treated epimastigotes by flow cytometry indicated that the plasma membrane remained intact, but there was a significant decrease in mitochondrial membrane potential. The pattern of cell distribution in the cell cycle stages (G1, G2, M) was unaltered in treated epimastigotes, indicating a trypanocidal rather than a trypanostatic activity. Scanning electron microscopy and flow cytometry showed epimastigotes with a round shape and decrease in cell size. Taken together, our data indicate that the EPA-35 is effective against T. cruzi. Synthetic transformation of EPA-35 into other derivatives may provide promising compounds for further evaluation against this parasite.

journal_name

FEMS Microbiol Lett

authors

de Azeredo CM,Ávila EP,Pinheiro DL,Amarante GW,Soares MJ

doi

10.1093/femsle/fnx020

subject

Has Abstract

pub_date

2017-02-01 00:00:00

issue

4

eissn

0378-1097

issn

1574-6968

pii

fnx020

journal_volume

364

pub_type

杂志文章
  • The immune response to Lactococcus lactis: implications for its use as a vaccine delivery vehicle.

    abstract::The development of natural antibodies to Lactococcus lactis in three inbred strains of mice and the effect of inoculating L. lactis into these mice has been investigated. All animals developed detectable levels of natural (systemic and secretory) anti-lactococcal antibodies. Systemic anti-lactococcal antibodies were p...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.1994.tb07041.x

    authors: Norton PM,Brown HW,Le Page RW

    更新日期:1994-07-15 00:00:00

  • Activation of FNR-dependent transcription by iron: an in vitro switch for FNR.

    abstract::FNR is an iron-binding transcriptional regulator of Escherichia coli which controls the expression of target genes in response to anaerobiosis. The mechanism used by FNR to sense and respond to anaerobiosis is unknown but it is thought to involve iron. In vitro transcription analyses have shown that iron-deficient FNR...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.1993.tb06517.x

    authors: Green J,Guest JR

    更新日期:1993-10-15 00:00:00

  • A new pullulan and a branched (1-->3)-, (1-->6)-linked beta-glucan from the lichenised ascomycete Teloschistes flavicans.

    abstract::The polysaccharides formed on hot alkaline extraction of the ascomycetous lichen Teloschistes flavicans were fractionated to give two glucans, which were characterised by methylation analysis and 1D and 2D NMR spectroscopy. One was a branched beta-glucan containing (1-->3) and (1-->6) linkages, a structure which is mo...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2002.tb11152.x

    authors: Reis RA,Tischer CA,Gorin PA,Iacomini M

    更新日期:2002-04-23 00:00:00

  • Immunogenicity of IMS 1113 plus soluble subunit and chimeric proteins containing Mycoplasma hyopneumoniae P97 C-terminal repeat regions.

    abstract::The surface adhesin P97 mediates the adherence of Mycoplasma hyopneumoniae to swine cilia. Two reiterated repeats R1 and R2 are located at the C-terminus of P97. The purpose of this study was to evaluate the immunogenicity of Montanide adjuvant IMS 1113 plus soluble subunit proteins rR1, rR1R2 and their chimeric forms...

    journal_title:FEMS microbiology letters

    pub_type: 信件

    doi:10.1111/1574-6968.12389

    authors: Barate AK,Cho Y,Truong QL,Hahn TW

    更新日期:2014-03-01 00:00:00

  • The genome of the Erwinia amylovora phage PhiEaH1 reveals greater diversity and broadens the applicability of phages for the treatment of fire blight.

    abstract::The enterobacterium Erwinia amylovora is the causal agent of fire blight. This study presents the analysis of the complete genome of phage PhiEaH1, isolated from the soil surrounding an E. amylovora-infected apple tree in Hungary. Its genome is 218 kb in size, containing 244 ORFs. PhiEaH1 is the second E. amylovora in...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/1574-6968.12319

    authors: Meczker K,Dömötör D,Vass J,Rákhely G,Schneider G,Kovács T

    更新日期:2014-01-01 00:00:00

  • Spiroethers of German chamomile inhibit production of aflatoxin G and trichothecene mycotoxin by inhibiting cytochrome P450 monooxygenases involved in their biosynthesis.

    abstract::The essential oil of German chamomile showed specific inhibition toward aflatoxin G(1) (AFG(1)) production, and (E)- and (Z)-spiroethers were isolated as the active compounds from the oil. The (E)- and (Z)-spiroethers inhibited AFG(1) production of Aspergillus parasiticus with inhibitory concentration 50% (IC(50)) val...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2008.01195.x

    authors: Yoshinari T,Yaguchi A,Takahashi-Ando N,Kimura M,Takahashi H,Nakajima T,Sugita-Konishi Y,Nagasawa H,Sakuda S

    更新日期:2008-07-01 00:00:00

  • Cell wall substrate specificity of six different lysozymes and lysozyme inhibitory activity of bacterial extracts.

    abstract::We have investigated the specificity of six different lysozymes for peptidoglycan substrates obtained by extraction of a number of gram-negative bacteria and Micrococcus lysodeikticus with chloroform/Tris-HCl buffer (chloroform/buffer). The lysozymes included two that are commercially available (hen egg white lysozyme...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2006.00240.x

    authors: Nakimbugwe D,Masschalck B,Deckers D,Callewaert L,Aertsen A,Michiels CW

    更新日期:2006-06-01 00:00:00

  • Comparison of transcription of multiple genes at three developmental stages of the plant pathogen Sclerotinia sclerotiorum.

    abstract::The ascomycete Sclerotinia sclerotiorum is a plant pathogen with a very broad host range. In order to identify and characterize genes involved in S. sclerotiorum infection of Brassica napus (canola), expressed sequence tags (ESTs) were examined from libraries prepared from three tissues: complex appressorium (infectio...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2006.00212.x

    authors: Sexton AC,Cozijnsen AJ,Keniry A,Jewell E,Love CG,Batley J,Edwards D,Howlett BJ

    更新日期:2006-05-01 00:00:00

  • Nucleotide sequence of the nfaA gene encoding the antigen 8786 adhesive factor of enterotoxigenic Escherichia coli.

    abstract::The nucleotide sequence of a 714-bp DNA fragment containing the enterotoxic Escherichia coli (ETEC) adhesive factor 8786 structural gene, designated nfaA, revealed an open reading frame of 498 bp encoding a polypeptide of 166 amino acids. Primer-extension experiments showed that the nfaA gene is within a single transc...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1016/0378-1097(92)90169-o

    authors: Aubel D,Darfeuille-Michaud A,Martin C,Joly B

    更新日期:1992-11-01 00:00:00

  • Helicobacter pylori strain ATCC700392 encodes a methyl-accepting chemotaxis receptor protein (MCP) for arginine and sodium bicarbonate.

    abstract::Helicobacter pylori ATCC43504 responds chemotactically to aspartic acid and serine, but not to arginine, nor to sodium bicarbonate. In contrast, H. pylori ATCC700392 (strain 26695) shows chemotaxis to all four attractants. Open reading frame HP0099 from H. pylori 26695 is predicted to encode one of three methyl-accept...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1016/S0378-1097(03)00423-3

    authors: Cerda O,Rivas A,Toledo H

    更新日期:2003-07-29 00:00:00

  • Diversity of endophytic fungi of Paeonia lactiflora Pallas and screening for fungal paeoniflorin producers.

    abstract::Endophytic fungi from Paeonia lactiflora Pallas, which is mainly distributed in China, were characterized and screened to identify those capable of producing paeoniflorin. A total of 101 isolates obtained from the roots, stems and leaves of P. lactiflora were grouped into 16 fungal taxa based on morphological traits a...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1093/femsle/fny263

    authors: Cheng X,Wei Z,Pu S,Xiang M,Yan A,Zhang Y,Wang X

    更新日期:2018-12-01 00:00:00

  • Examination of Serpulina pilosicoli for attachment and invasion determinants of Enterobacteria.

    abstract::The spirochaete, Serpulina pilosicoli, is the agent of intestinal spirochaetosis, a diarrhoeal disease of humans and other species. By mechanisms as yet unknown, large numbers of these spirochaetes intimately attach to the colonic mucosa by one cell end. In some infected individuals, the spirochaetes may invade the la...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.1998.tb13127.x

    authors: Hartland EL,Mikosza AS,Robins-Browne RM,Hampson DJ

    更新日期:1998-08-01 00:00:00

  • MHYT, a new integral membrane sensor domain.

    abstract::MHYT, a new conserved protein domain with a likely signaling function, is described. This domain consists of six transmembrane segments, three of which contain conserved methionine, histidine, and tyrosine residues that are projected to lie near the outer face of the cytoplasmic membrane. In Synechocystis sp. PCC6803,...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2001.tb10919.x

    authors: Galperin MY,Gaidenko TA,Mulkidjanian AY,Nakano M,Price CW

    更新日期:2001-11-27 00:00:00

  • Molecular characterization of benzimidazole-resistant isolates of Cladosporium fulvum.

    abstract::The benzimidazole fungicide thiophanate-methyl is commonly applied to control leaf mould of tomato caused by Cladosporium fulvum in China. In this study, 32 isolates of C. fulvum were examined for their sensitivities to thiophanate-methyl, and two benzimidazole-resistant (BenR) phenotypes BenR1 and BenR2 were identifi...

    journal_title:FEMS microbiology letters

    pub_type: 信件

    doi:10.1111/j.1574-6968.2007.00999.x

    authors: Yan L,Chen J,Zhang C,Ma Z

    更新日期:2008-01-01 00:00:00

  • Induction of baroresistance by hydrogen peroxide, ethanol and cold-shock in Saccharomyces cerevisiae.

    abstract::The acquisition of tolerance to high hydrostatic pressure of 220 MPa (HHP) in response to a 0.4 mM hydrogen peroxide, 6% ethanol and cold-shock (10 degrees C) pretreatment for different lengths of times was studied in the yeast Saccharomyces cerevisiae. The protection conferred by these different treatments was simila...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1016/j.femsle.2004.02.002

    authors: Palhano FL,Orlando MT,Fernandes PM

    更新日期:2004-04-01 00:00:00

  • Characterization of Xanthomonas oryzae pv. oryzae recX, a gene that is required for high-level expression of recA.

    abstract::Analysis of the nucleotide sequence downstream from the Xanthomonas oryzae pv. oryzae recA gene reveals two orfs designated orfX and recX. The former has the potential to code for a 5.6 kDa protein of unknown function while the latter encodes for a putative 14.6 kDa protein with homology to RecX from various bacteria....

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2001.tb10929.x

    authors: Sukchawalit R,Vattanaviboon P,Utamapongchai S,Vaughn G,Mongkolsuk S

    更新日期:2001-11-27 00:00:00

  • Helicobacter pylori HopQ outer membrane protein attenuates bacterial adherence to gastric epithelial cells.

    abstract::Helicobacter pylori genomes contain about 30 hop genes that encode outer membrane proteins. Helicobacter pylori hopQ alleles exhibit a high level of genetic diversity, and two families of hopQ alleles have been described. Type I hopQ alleles are found more commonly in cag-positive H. pylori strains from patients with ...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2008.01368.x

    authors: Loh JT,Torres VJ,Algood HM,McClain MS,Cover TL

    更新日期:2008-12-01 00:00:00

  • In silico analysis of trypanosomatids' helicases.

    abstract::Trypanosomatids are unicellular protozoan parasites that cause many diseases in animals, including humans, and plants. These early divergent eukaryotes have many singular structures and processes, including the hyper-modified 'base J', a mitochondrial DNA network, RNA editing, and trans-splicing; all of these unique f...

    journal_title:FEMS microbiology letters

    pub_type: 信件

    doi:10.1111/j.1574-6968.2012.02644.x

    authors: Gargantini PR,Lujan HD,Pereira CA

    更新日期:2012-10-01 00:00:00

  • Sensitivity of bacteria to diamond nanoparticles of various size differs in gram-positive and gram-negative cells.

    abstract::In this study, the influence of the size and surface termination of diamond nanoparticles (DNPs) on their antibacterial activity against Escherichia coli and Bacillus subtilis was assessed. The average size and distribution of DNPs were determined by dynamic light scattering and X-ray diffraction techniques. The chemi...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/1574-6968.12373

    authors: Beranová J,Seydlová G,Kozak H,Benada O,Fišer R,Artemenko A,Konopásek I,Kromka A

    更新日期:2014-02-01 00:00:00

  • Existence and characterization of allelic variants of Sao, a newly identified surface protein from Streptococcus suis.

    abstract::Surface antigen one (Sao) is a newly identified protein from the major zoonotic pathogen, Streptococcus suis. In search of functional proteins related to the pathogenesis of Chinese S. suis 2 (SS2), unexpectedly, a variant of Sao protein was obtained. To test its prevalence in S. suis, PCR assay was adopted to address...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2007.00859.x

    authors: Feng Y,Zheng F,Pan X,Sun W,Wang C,Dong Y,Ju AP,Ge J,Liu D,Liu C,Yan J,Tang J,Gao GF

    更新日期:2007-10-01 00:00:00

  • Inactivation of the fis gene leads to reduced growth rate.

    abstract::The FIS protein (factor for inversion stimulation) is known to activate the transcription of rRNA and tRNA operons in Escherichia coli. In this report the growth behaviour of a fis bacterium was studied under steady-state conditions and in competition experiments with a wild-type bacterium in a chemostat. The growth r...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1016/0378-1097(92)90292-v

    authors: Nilsson L,Verbeek H,Hoffmann U,Haupt M,Bosch L

    更新日期:1992-11-15 00:00:00

  • Conversion of methionine to methional by Lactococcus lactis.

    abstract::Lactic acid bacteria were screened for methional production from 4-methylthio-2-ketobutanoate. Only Lactococcus lactis IFPL730 produced high amounts of methional. It was demonstrated that production of this compound was an exclusively enzymatic reaction. The present work describes for the first time that L. lactis can...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2001.tb10884.x

    authors: Amárita F,Fernández-Esplá D,Requena T,Pelaez C

    更新日期:2001-10-16 00:00:00

  • Molecular characterization of a new acetyl xylan esterase (AXEII) from edible straw mushroom Volvariella volvacea with both de-O-acetylation and de-N-acetylation activity.

    abstract::A new Volvariella volvacea gene encoding a carbohydrate esterase (CE) family 4 acetyl xylan esterase (AXE) (designated as VvaxeII) was cloned and characterized. The coded polypeptide had 253 amino acid residues, with the first 19 serving as a secretion signal peptide. The VvaxeII transcript levels were high when the f...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2009.01585.x

    authors: Liu X,Ding S

    更新日期:2009-06-01 00:00:00

  • Mice immunization with live lactococci displaying a surface anchored HPV-16 E7 oncoprotein.

    abstract::E7 oncoprotein of human papillomavirus-16 (HPV-16) is constitutively produced in cervical cancer (CxCa) and is a good candidate for the design of therapeutic vaccines. In this work, the nisin-controlled expression system was used to display the E7 protein at the cell surface of the food-grade Gram-positive bacterium L...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1016/S0378-1097(03)00778-X

    authors: Cortes-Perez NG,Bermúdez-Humarán LG,Le Loir Y,Rodriguez-Padilla C,Gruss A,Saucedo-Cárdenas O,Langella P,Montes-de-Oca-Luna R

    更新日期:2003-12-05 00:00:00

  • Analysis of the role of the two flagella of Bradyrhizobium japonicum in competition for nodulation of soybean.

    abstract::Bradyrhizobium japonicum has two types of flagella. One has thin filaments consisting of the 33-kDa flagellins FliCI and FliCII (FliCI-II) and the other has thick filaments consisting of the 65-kDa flagellins FliC1, FliC2, FliC3, and FliC4 (FliC1-4). To investigate the roles of each flagellum in competition for nodula...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2011.02280.x

    authors: Althabegoiti MJ,Covelli JM,Pérez-Giménez J,Quelas JI,Mongiardini EJ,López MF,López-García SL,Lodeiro AR

    更新日期:2011-06-01 00:00:00

  • The rfaH gene, which affects lipopolysaccharide synthesis in Salmonella enterica serovar Typhi, is differentially expressed during the bacterial growth phase.

    abstract::We have cloned and sequenced the rfaH gene from Salmonella enterica serovar Typhi strain Ty2. The gene showed a high degree of similarity to the rfaH genes from Escherichia coli K-12 and S. enterica serovar Typhimurium. A rfaH mutant was constructed by site-directed mutagenesis. This mutant produced a rough lipopolysa...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2001.tb10874.x

    authors: Rojas G,Saldías S,Bittner M,Zaldívar M,Contreras I

    更新日期:2001-10-16 00:00:00

  • Identification of beta-oxidation and thioesterase activities in Staphylococcus carnosus 833 strain.

    abstract::Staphylococcus carnosus 833, inoculated into sausage meat, increased the level of methyl ketones, which contributed to the cured aroma. These ketones can arise from incomplete beta-oxidation followed by two enzymatic activities: a thioesterase and a decarboxylase. In this study we identified the beta-oxidative pathway...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2000.tb09272.x

    authors: Engelvin G,Feron G,Perrin C,Mollé D,Talon R

    更新日期:2000-09-01 00:00:00

  • The expression of the flagellum of Legionella pneumophila is modulated by different environmental factors.

    abstract::Legionella pneumophila, the aetiologic agent of legionnaires' disease, contains a single, monopolar flagellum which is composed of one major subunit, the FlaA protein. Expression studies using a reporter gene fusion of the flaA promoter with the luxAB gene revealed that the flaA expression is not only temperature regu...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.1999.tb13603.x

    authors: Heuner K,Brand BC,Hacker J

    更新日期:1999-06-01 00:00:00

  • Identification of in vivo essential genes from Pseudomonas aeruginosa by PCR-based signature-tagged mutagenesis.

    abstract::We adapted PCR-based signature-tagged mutagenesis (STM) to Pseudomonas aeruginosa. A collection of 1056 mutants was screened in a chronic lung infection rat model. Thirteen mutants were confirmed to be attenuated. Analysis revealed that these STM mutants represented transposon insertions into eight genes previously de...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2002.tb11162.x

    authors: Lehoux DE,Sanschagrin F,Levesque RC

    更新日期:2002-04-23 00:00:00

  • The Serratia-type hemolysin of Chromobacterium violaceum.

    abstract::Chromobacterium violaceum is a Gram-negative opportunistic human pathogen and an inhabitant of tropical soils and waterways. Although known primarily for the synthesis of the pigment violacein, and more recently as a reporter strain for quorum sensing, clinical reports of chromobacteriosis comprise the largest block o...

    journal_title:FEMS microbiology letters

    pub_type: 杂志文章

    doi:10.1111/j.1574-6968.2006.00566.x

    authors: Brumbach KC,Eason BD,Anderson LK

    更新日期:2007-02-01 00:00:00