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thiophene derivatives with antileishmanial activity isolated from aerial parts of porophyllum ruderale (jacq.) cass.porophyllum ruderale (jacq.) cass. is a plant native to brazil and in the northwest region of the state of paraná, brazil, aerial parts of p. ruderale have been used popularly in the treatment of lesions caused by leishmania sp.. in this study the antileishmanial and cytotoxic activities of the crude extract, fractions, and isolated compounds from aerial parts of p. ruderale was evaluated. the dichloromethane extract was submitted to chromatography to yield compounds active against leishmania am ...201121522080
effectiveness of the local or oral delivery of the novel naphthopterocarpanquinone lqb-118 against cutaneous leishmaniasis.objectives this paper describes the antileishmanial properties of lqb-118, a new compound designed by molecular hybridization, orally active in leishmania amazonensis-infected balb/c mice. methods in vitro antileishmanial activity was determined in l. amazonensis-infected macrophages. for in vivo studies, lqb-118 was administered intralesionally (15 μg/kg/day, five times a week), intraperitoneally (4.5 mg/kg/day, five times a week) or orally (4.5 mg/kg/day, five times a week) to l. amazonensis-i ...201121531758
protease expression by microorganisms and its relevance to crucial physiological/pathological events.the treatment of infections caused by fungi and trypanosomatids is difficult due to the eukaryotic nature of these microbial cells, which are similar in several biochemical and genetic aspects to host cells. aggravating this scenario, very few antifungal and anti-trypanosomatidal agents are in clinical use and, therefore, therapy is limited by drug safety considerations and their narrow spectrum of activity, efficacy and resistance. the search for new bioactive agents against fungi and trypanoso ...201121537490
correlation of meta 1 expression with culture stage, cell morphology and infectivity in leishmania (leishmania) amazonensis promastigotes.the parasitic protozoan leishmania (leishmania) amazonensis alternates between mammalian and insect hosts. in the insect host, the parasites proliferate as procyclic promastigotes andthen differentiate into metacyclic infective forms. the meta 1 gene is preferentially expressed during metacyclogenesis. meta 1 expression profile determination along parasite growth curves revealed that the meta 1 mrna level peaked at the early stationary phase then decreased to an intermediate level. no correlatio ...201121537679
the lfr1 ferric iron reductase of leishmania amazonensis is essential for the generation of infective parasite forms.the protozoan parasite leishmania is the causative agent of serious human infections worldwide. the parasites alternate between insect and vertebrate hosts, and cause disease by invading macrophages, where they replicate. parasites lacking the ferrous iron transporter lit1 cannot grow intracellularly, indicating that a plasma membrane-associated mechanism for iron uptake is essential for the establishment of infections. here we identify and functionally characterize a second member of the leishm ...201121558274
photodynamic therapy for american cutaneous leishmaniasis: the efficacy of methylene blue in hamsters experimentally infected with leishmania (leishmania) amazonensis.the aim of this study was to investigate the effectiveness of photodynamic therapy (pdt) using methylene blue (mb) as the photosensitizing compound and a light-emitting diode (led) in american cutaneous leishmaniasis (acl). hamsters were experimentally infected with leishmania (leishmania) amazonensis. after the development of the lesions in the footpad, the animals were treated with mb three times a week for 3months. ten minutes after each application of mb, the lesions were irradiated with led ...201121575635
evaluation of the microbicidal activity and cytokines/chemokines profile released by neutrophils from htlv-1 infected individuals.human t-cell lymphotropic virus-type 1 (htlv-1) induces activation and spontaneous proliferation of t cells with production of type-1 pro-inflammatory cytokines. it modifies the immune response to other antigens and increases susceptibility to infectious diseases. however, little is known about innate immunity in htlv-1 infection. htlv-1 infected individuals have higher spontaneous neutrophil activation than htlv-1 seronegative individuals, as shown by the nitroblue tetrazolium (nbt) assay. this ...201121595736
the pharmacological inhibition of sterol biosynthesis in leishmania is counteracted by enhancement of ldl endocytosis.leishmania parasites, despite being able to synthesize their own sterols, acquire and accumulate significant amounts of cholesterol through low density lipoprotein (ldl) particle endocytosis. the role of this system in leishmania amazonensis promastigotes under pharmacological pressure by sterol biosynthesis inhibitors (sbis) was investigated. first, thin layer chromatography demonstrated that l. amazonensis promastigotes, in response to ergosterol biosynthesis inhibition by treatment with 4.0 a ...201121601554
gene expression profiling and molecular characterization of antimony resistance in leishmania amazonensis.drug resistance is a major problem in leishmaniasis chemotherapy. rna expression profiling using dna microarrays is a suitable approach to study simultaneous events leading to a drug-resistance phenotype. genomic analysis has been performed primarily with old world leishmania species and here we investigate molecular alterations in antimony resistance in the new world species l. amazonensis.201121629719
new cassane diterpenes from caesalpinia echinata.an investigation of the ethanolic extract from stems of caesalpinia echinata lam (leguminosae-caesalpinioideae) led to the isolation of five new cassane diterpenes along with known lambertianic acid. their structures were determined based on spectroscopic methods. a preliminary study on leishmanicidal activity demonstrated that compounds 1, 2 and 6 were found to inhibit the growth of amastigote-like forms of leishmania amazonensis without affecting mononuclear cells obtained from human periphera ...201121641971
leishmania promotes its own virulence by inducing expression of the host immune inhibitory ligand cd200.leishmania parasites infect macrophages, cells normally involved in innate defense against pathogens. leishmania amazonensis and leishmania major cause severe or mild disease, respectively, consistent with each parasite's ability to survive within activated macrophages. the mechanisms underlying increased virulence of l. amazonensis are mostly unknown. we show that l. amazonensis promotes its own survival by inducing expression of cd200, an immunoregulatory molecule that inhibits macrophage ac ...201121669395
photodynamic therapy using methylene blue to treat cutaneous leishmaniasis.abstract objective: the purpose of this study was to show the efficiency and underlying mechanism of action of photodynamic therapy (pdt) using methylene blue (mb) and non-coherent light sources to treat cutaneous leishmaniasis (cl). background data: systemic treatment can cause severe side effects, and pdt using porphyrin precursors as sensitizers has been used as an alternative to treat cl. mb has been used under illumination or in the dark to treat a wide range of medical conditions, and it e ...201121671755
copaiba oil: an alternative to development of new drugs against leishmaniasis.leishmaniasis is a neglected disease that is increasing globally at an alarming rate. glucantime has been the therapy of choice for more than 50 years. a recent study reported the antileishmanial activity of copaiba oil against leishmania amazonensis. these results led us to investigate morphological and ultrastructural changes in l. amazonensis treated with copaiba oil, using electron microscopy and flow cytometry to assess specific organelles as targets for copaiba oil. in the promastigote and ...201221716677
dermaseptin 01 as antimicrobial peptide with rich biotechnological potential: study of peptide interaction with membranes containing leishmania amazonensis lipid-rich extract and membrane models.this article addresses the interactions of the synthetic antimicrobial peptide dermaseptin 01 (glwstikqkgkeaaiaaa- kaagqaalgal-nh(2) , ds 01) with phospholipid (pl) monolayers comprising (i) a lipid-rich extract of leishmania amazonensis (lre-la), (ii) zwitterionic pl (dipalmitoylphosphatidylcholine, dppc), and (iii) negatively charged pl (dipalmitoylphosphatidylglycerol, dppg). the degree of interaction of ds 01 with the different biomembrane models was quantified from equilibrium and dynamic l ...201121805539
molecular determinants of ciliary membrane localization of trypanosoma cruzi flagellar calcium-binding protein.the flagellar calcium binding protein (fcabp)(4) of trypanosoma cruzi is localized to the flagellar membrane in all life cycle stages of the parasite. myristoylation and palmitoylation of the n-terminus of fcabp are necessary for flagellar membrane targeting. not all dually acylated proteins in t. cruzi are flagellar, however. other determinants of fcabp therefore likely contribute to flagellar specificity. we generated t. cruzi transfectants expressing the n-terminal 24 or 12 amino acids of fca ...201121784841
synthesis, evaluation against leishmania amazonensis and cytotoxicity assays in macrophages of sixteen new congeners morita-baylis-hillman adducts.we report the design, synthesis, in vitro evaluation against leishmania amazonensis (ic(50)), cytotoxicity assays in macrophages (cc(50)), and selectivity index (sicc(50)/ic(50)) of sixteen new congeners aromatic morita-baylis-hillman adducts 1-16. the 1-16 were prepared in good to excellent yields (58%-97%) from the "one pot" morita-baylis-hillman reaction between the aldehydes 29-36 and the acrylates 27 or 28 under dabco as promoter. the mbha 2-[hydroxy(2-nitrophenyl)propyl] propanoate (1, ic( ...201121775030
antileishmanial sesquiterpene lactones from pseudelephantopus spicatus, a traditional remedy from the chayahuita amerindians (peru). part iii.ethnopharmacological relevance: the study of traditional remedies used by the chayahuita, an ethnic group from the peruvian amazonia, has prompted us to investigate in detail the ethanolic extract of pseudelephantopus spicatus (juss. ex aubl.) c.f. baker, which has demonstrated strong biological activity towards leishmania amazonensis. our goal was to discover the active compound of this plant-based remedy. materials and methods: a bioguided fractionation of the crude extract was undertaken base ...201121771652
leishmania amazonensis: effects of oral treatment with copaiba oil in mice.leishmaniasis is a severe public-health problem, with high rates of morbidity and mortality. efforts to find new, effective and safe oral agents for the treatment of leishmaniasis have been ongoing for several decades, in order to avoid the problems with the currently used antimonials. in the present study, we found that a copaiba oil oral treatment (group iv) caused a significant reduction in the average lesion size (1.1±0.4mm) against leishmania amazonensis lesions compared with untreated mice ...201121771592
the in vitro leishmanicidal activity of hexadecylphosphocholine (miltefosine) against four medically relevant leishmania species of brazil.the in vitro leishmanicidal activity of miltefosine-« (zentaris gmbh) was assessed against four medically relevant leishmania species of brazil: leishmania (leishmania) amazonensis, leishmania (viannia) braziliensis, leishmania (viannia) guyanensis and leishmania (leishmania) chagasi. the activity of miltefosine against these new world species was compared to its activity against the old world strain, leishmania (leishmania) donovani, which is known to be sensitive to the effects of miltefosine. ...201121739037
miltefosine induces programmed cell death in leishmania amazonensis promastigotes.in the current study, we evaluated the mechanism of action of miltefosine, which is the first effective and safe oral treatment for visceral leishmaniasis, in leishmania amazonensis promastigotes. miltefosine induced a process of programmed cell death, which was determined by the externalization of phosphatidylserine, the incorporation of propidium iodide, cell-cycle arrest at the sub-g0/g1 phase and dna fragmentation into oligonucleosome-sized fragments. despite the intrinsic variation that is ...201121739043
design, synthesis and antileishmanial in vitro activity of new series of chalcones-like compounds: a molecular hybridization approach.the chalcone-like series 1a-1g was efficiently synthesized from morita-baylis-hillman reaction (52-74% yields). compounds 1a-1g were designed by molecular hybridization based on the anti-inflammatory drug methyl salicylate (3) and the antileishmanial moiety of the morita-baylis-hillman adducts 2a-2g. the 1a-1g compounds were much more actives than precursor series 2a-2g, for example, ic(50)=7.65 ++m on leishmania amazonensis and 10.14 ++m on leishmania chagasi (compound 1c) when compared to ic(5 ...201121684751
molecular factors governing inhibition of arylimidamides against leishmania: conservative computational modeling to improve chemotherapies.a dataset of 55 compounds with inhibitory activity against leishmania donovani axenic amastigotes and leishmania amazonensis intracellular parasites was examined through three-dimensional quantitative structure-activity relationship modeling employing molecular descriptors from both rigid and flexible compound alignments. for training and testing purposes, the compounds were divided into two datasets of 45 and 10 compounds, respectively. statistically significant models were constructed and vali ...201121741248
in silico predicted epitopes from the cooh-terminal extension of cysteine proteinase b inducing distinct immune responses during leishmania (leishmania) amazonensis experimental murine infection.abstract:201121824434
cratp interferes in the promastigote-macrophage interaction in leishmania amazonensis infection.recent have shown the relationship between ecto-nucleoside-triphosphate-diphosphohydrolases (ecto-ntpdases or ecto-nucleotidases) and virulence and infectivity in trypanosomatids. in this work, the inhibition of the ecto-atpase activities and promastigote growth of leishmania amazonensis by cratp was characterized. furthermore, this compound was used to investigate the role of ecto-nucleotidase in the interaction of l. amazonensis with resident peritoneal macrophages obtained from balb/c mice. c ...201121679488
leishmania amazonensis: characterization of an ecto-3'-nucleotidase activity and its possible role in virulence.ecto-3'-nucleotidase/nuclease (3'nt/nu) is a membrane-bound enzyme that plays a key role in the nutrition of leishmania sp. protozoan parasites. this enzyme generates nucleosides via hydrolyzes of 3'mononucleotides and nucleic acids, which enter the cell by specific transporters. in this work, we identify and characterize leishmania amazonensis ecto-3'-nucleotidase activity (la3'-nucleotidase), report ammonium tetrathiomolybdate (ttm) as a novel la3'-nucleotidase inhibitor and approach the possi ...201121827749
leishmanicidal activity of the agaricus blazei murill in different leishmania species.leishmaniasis is a major public health problem, and the alarming spread of parasite resistance underlines the importance of discovering new therapeutic products. the present study aims to investigate the in vitro leishmanicidal activity of an agaricus blazei murill mushroom extract as compared to different leishmania species and stages. the water extract proved to be effective against promastigote and amastigote-like stages of leishmania amazonensis, l. chagasi, and l. major, with ic(50) (50% in ...201121723957
new salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-n-oxide with antileishmanial and antimalarial activities.continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-n-oxide quinoxaline-2-carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against plasmodium falciparum colombian fcr-3 strain and leishmania amazonensis strain mhom/br/76/ltb-012a. further computational studies were carried out in order to analyze graphic sar and adme properties. the results obtained indicate that ...201121724395
activity of cuban propolis extracts on leishmania amazonensis and trichomonas vaginalis.in this paper we analyzed the antiprotozoal effects of eighteen cuban propolis extracts (brown, red and yellow type) collected in different geographic areas, using leishmania amazonensis (as a model of intracellular protozoa) and trichomonas vaginalis (as a model of extracellular protozoa). all evaluated propolis extracts caused inhibitory effect on intracellular amastigotes of l. amazonensis. however, cytotoxicity on peritoneal macrophages from balb/c mice was observed. only five samples decrea ...201121834236
Sir2-Related Protein 1 from Leishmania amazonensis is a glycosylated NAD+-dependent deacetylase.SUMMARYSirtuin proteins form a family of NAD+-dependent protein deacetylases that are considered potential drug targets against parasites. Here, we present the first characterization of a sirtuin orthologue from Leishmania amazonensis, an aetiological agent of American tegumentary leishmaniasis that has been the subject of many studies focused in the development of therapeutic approaches. The protein has high sequence identity with other Kinetoplastid Silent information regulator 2 Related Prote ...201121819639
Infection with Leishmania amazonensis upregulates purinergic receptor expression and induces host-cell susceptibility to UTP-mediated apoptosis.Nucleotides are released into the extracellular milieu from infected cells and cells at inflammatory sites. The extracellular nucleotides bind to specific purinergic (P2) receptors and thereby induce a variety of cellular responses including anti-parasitic effects. Here we investigated whether extracellular nucleotides affect leishmanial infection in macrophages, and found that UTP reduces strongly the parasite load in peritoneal macrophages. Ultrastructural analysis of infected cells revealed t ...201121740498
in vitro activity of the clinical pulmonary surfactant surfacen® against leishmania amazonensis.surfacen® is an exogenous natural lung surfactant, composed by phospholipids and hydrophobic proteins, which is applied successfully in newborn respiratory distress syndrome. in this paper, in vitro activity of surfacen® against leishmania amazonensis is described. the product showed activity against the amastigote form found in peritoneal macrophages from balb/c mice, with an ic50 value of 17.9 ± 3.0 µg/ml; while no toxic effect on host cell was observed up to 200 µg/ml. this is the first repor ...201121915470
HPLC Analysis of Supercritical Carbon Dioxide and Compressed Propane Extracts from Piper amalago L. with Antileishmanial Activity.Piper amalago L. leaves were extracted with supercritical carbon dioxide and compressed propane under different conditions, and with chloroform by the conventional maceration method. These methods were compared for the pyrrolidine alkaloid content. Supercritical carbon dioxide (SFE-CO(2)) at 313 K and 12.55 MPa showed the highest selectivity for the main compound (600.53 mg/g of extract). A gradient high-performance liquid chromatography (HPLC) method was developed and validated to quantify the ...201122193211
Leishmanicidal effects of piperine, its derivatives, and analogues on Leishmania amazonensis.Leishmaniasis is a tropical disease caused by protozoan parasites of the genus Leishmania which affects 12 million people worldwide. The discovery of drugs for the treatment of leishmaniasis is a pressing concern in global health programs. The aim of this study aim was to evaluate the leishmanicidal effect of piperine and its derivatives/analogues on Leishmania amazonensis. Our results showed that piperine and phenylamide are active against promastigotes and amastigotes in infected macrophages. ...201121885074
Expression of infection-related genes in parasites and host during murine experimental infection with Leishmania (Leishmania) amazonensis.Leishmania parasites are able to interfere with host immune responses on many levels, as T cell responses balance, as observed in the murine model of infection. In the present study, we analyzed genes expression in both host and parasite during the progression of infection. Host genes associated to T-lymphocytes responses, MHC classes I and II, as well as parasite enzymes genes, cysteine-proteinases(CP) B and C, were examined in mice along evolution of infection by Leishmania (Leishmania) amazon ...201222178713
Effect of Bixa orellana against Leishmania amazonensis.Background: In the present study, an activity of Bixa orellana extract against Leishmania amazonensis was demonstrated. Result: Experimentally infected BALB/c mice were treated with B. orellana extract which showed a significant activity against promastigote and amastigote forms of L. amazonensis. Conclusion: This study supports the importance of natural sources as antileishmanial drugs.201122189367
Pterocarpanquinones, aza-pterocarpanquinone and derivatives: synthesis, antineoplasic activity on human malignant cell lines and antileishmanial activity on Leishmania amazonensis.Pterocarpanquinones (1a-e) and the aza-pterocarpanquinone (2) were synthesized through palladium catalyzed oxyarylation and azaarylation of conjugate olefins, and showed antineoplasic effect on leukemic cell lines (K562 and HL-60) as well as colon cancer (HCT-8), gliobastoma (SF-295) and melanoma (MDA-MB435) cell lines. Some derivatives were prepared (3-8) and evaluated, allowing establishing the structural requirements for the antineoplasic activity in each series. Compound 1a showed the best s ...201122000949
the in vivo activity of 1,3,4-thiadiazolium-2-aminide compounds in the treatment of cutaneous and visceral leishmaniasis.researchers have recently investigated the biological activities of mesoionic (mi) compounds, which have shown in vitro activity against many species of leishmania, as well as trypanosoma cruzi. the main goal of this study was to evaluate and compare the activity of three mi compounds against leishmania amazonensis and leishmania infantum infection in vivo.201221987238
Differential modulation of ATP-induced P2X7-associated permeabilities to cations and anions of macrophages by infection with Leishmania amazonensis.Leishmania and other parasites display several mechanisms to subvert host immune cell function in order to achieve successful infection. The ATP receptor P2X7, an agonist-gated cation channel widely expressed in macrophages and other cells of the immune system, is also coupled to inflammasome activation, IL-1 beta secretion, production of reactive oxygen species, cell death and the induction of the permeabilization of the plasma membrane to molecules of up to 900 Da. P2X7 receptors can function ...201121966508
Increasing the activity of copper(II) complexes against Leishmania through lipophilicity and pro-oxidant ability.Copper complexes with fluorinated ß-diketones were synthesized and characterized in terms of lipophilicity and peroxide-assisted oxidation of dihydrorhodamine as an indicator of redox activity. The biological activity of the complexes was tested against promastigotes of Leishmania amazonensis. Inhibition of trypanosomatid-specific trypanothione reductase was also tested. It was found that the highly lipophilic and redox-active bis(trifluoroacetylacetonate) derivative had increased toxicity towar ...201221866394
Lack of signaling by IL-4 or by IL-4/IL-13 has more attenuating effects on Leishmania amazonensis dorsal skin - than on footpad-infected mice.Lesion development in tegumentary leishmaniasis is markedly influenced by the inoculation site and the type and number of injected infective forms. This and the yet unclear contribution of Th2 cytokines as susceptibility factors to Leishmania amazonensis infection prompted us to investigate the roles of IL-4, IL-13 and IL-10 on C57BL/6 and BALB/c mice infected in the footpad (paw) or rump with low-dose L. amazonensis purified-metacyclics. Wild-type (WT) mice of either strain developed, in the ru ...201222019418
synthesis, cytotoxicity, and in vitro antileishmanial activity of mono-t-butyloxycarbonyl-protected diamines.leishmania amazonensis is the etiologic agent of the cutaneous and diffuse leishmaniasis. this species is often associated with drug resistance, and the conventional treatments exhibit high toxicity for patients. therefore, the search for new antileishmanial compounds is urgently needed since there is no vaccine available. in this study, using the in vitro traditional drug screening test, we have analyzed the effects of a series of diaminoalkanes monoprotected with t-butyloxycarbonyl (boc) again ...201121907525
intranasal immunization with lack-dna promotes protective immunity in hamsters challenged with leishmania chagasi.summarylack (leishmania analogue of the receptor kinase c) is a conserved protein in protozoans of the genus leishmania which is associated with the immunopathogenesis and susceptibility of balb/c mice to l. major infection. previously, we demonstrated that intranasal immunization with a plasmid carrying the lack gene of leishmania infantum (lack-dna) promotes protective immunity in balb/c mice against leishmania amazonensis and leishmania chagasi. in the present study, we investigated the prote ...201121867591
axenic leishmania amazonensis promastigotes sense both the external and internal arginine pool distinctly regulating the two transporter-coding genes.leishmania (l.) amazonensis uses arginine to synthesize polyamines to support its growth and survival. here we describe the presence of two gene copies, arranged in tandem, that code for the arginine transporter. both copies show similar open reading frames (orfs), which are 93% similar to the l. (l.) donovani aap3 gene, but their 5' and 3' utr's have distinct regions. according to quantitative rt-pcr, the 5.1 aap3 mrna amount was increased more than 3 times that of the 4.7 aap3 mrna along the p ...201122114701
potential utility of hyperbaric oxygen therapy and propolis in enhancing the leishmanicidal activity of glucantime.in this study we investigated the efficacy of hyperbaric oxygen (hbo) therapy, alone or combined with the pentavalent antimonial glucantime on leishmania amazonensis infection. in parallel, the effect of brazilian red propolis gel (propain) alone or combined with glucantime on l. amazonensis infection was evaluated. the inhibition of the infection in macrophages treated with glucantime in combination with hbo exposition was greater than that of macrophages treated with glucantime alone or hbo al ...201122183457
Leishmanicidal and antitumoral activities of endophytic fungi associated with the Antarctic angiosperms Deschampsia antarctica Desv. and Colobanthus quitensis (Kunth) Bartl.A total of 564 isolates of endophytic fungi were recovered from the plants Deschampsia antarctica and Colobanthus quitensis collected from Antarctica. The isolates were screened against parasites Leishmania amazonensis and Trypanosoma cruzi and against the human tumour cell lines. Of the 313 fungal isolates obtained from D. antarctica and 251 from C. quitensis, 25 displayed biological activity. Nineteen extracts displayed leishmanicidal activity, and six inhibited the growth of at least one tumo ...201222072308
dot/icm type ivb secretion system requirements for coxiella burnetii growth in human macrophages.central to q fever pathogenesis is replication of the causative agent, coxiella burnetii, within a phagolysosome-like parasitophorous vacuole (pv) in mononuclear phagocytes. c. burnetii modulates pv biogenesis and other host cell functions, such as apoptotic signaling, presumably via the activity of proteins delivered to the host cytosol by a dot/icm type ivb secretion system (t4bss). in this study, we utilized a c. burnetii strain carrying icmd inactivated by the himar1 transposon to investigat ...201121862628
antiproliferative, ultrastructural, and physiological effects of amiodarone on promastigote and amastigote forms of leishmania amazonensis.amiodarone (amio), the most frequently antiarrhythmic drug used for the symptomatic treatment of chronic chagas' disease patients with cardiac compromise, has recently been shown to have also specific activity against fungi, trypanosoma cruzi and leishmania. in this work, we characterized the effects of amio on proliferation, mitochondrial physiology, and ultrastructure of leishmania amazonensis promastigotes and intracellular amastigotes. the ic(50) values were 4.21 and 0.46 μm against promasti ...201122091415
the coxiella burnetii dot/icm system creates a comfortable home through lysosomal renovation.understanding the molecular pathogenesis of coxiella burnetii, the causative agent of human q fever, has historically been hindered by the technical difficulties of genetically manipulating obligate intracellular bacteria. the recent development of culture conditions suitable for axenic propagation of c. burnetii has paved the way for the application of a range of genetic techniques to address key questions within the field. recent studies using mutational analysis have revealed that the c. burn ...201122010216
human cutaneous leishmaniasis: interferon-dependent expression of double-stranded rna-dependent protein kinase (pkr) via tlr2.we investigated the type i interferon (ifn-1)/pkr axis in the outcome of the leishmania (leishmania) amazonensis infection, along with the underlying mechanisms that trigger and sustain this signaling pathway. reporter assays of cell extracts from raw-264.7 macrophages infected with l. (l.) amazonensis or hek-293t cells cotransfected with tlr2 and pkr promoter constructions were employed. primary macrophages of tlr2-knockout (ko) or ifnr-ko mice were infected, and the levels of pkr, ifn-1, and s ...201121846836
A new type of pterocarpanquinone that affects Toxoplasma gondii tachyzoites in vitro.Toxoplasma gondii, the agent of Toxoplasmosis, is an obligate intracellular protozoan able to infect a wide range of vertebrate cells, including nonprofessional and professional phagocytes. Therefore, drugs must have intracellular activities in order to control this parasite. The most common therapy for Toxoplasmosis is the combination of sulfadiazine and pyrimethamine. This treatment is associated with adverse reactions, thus, the development of new drugs is necessary. In previous studies, naph ...201122177332
lulo cell line derived from lutzomyia longipalpis (diptera: psychodidae): a novel model to assay leishmania spp. and vector interaction.leishmania (vianna) braziliensis, leishmania (leishmania) amazonensis and leishmania (leishmania) chagasi are important parasites in the scenario of leishmaniasis in brazil. during the life cycle of these parasites, the promastigote forms adhere to the midgut epithelial microvillii of phlebotomine insects to avoid being secreted along with digestive products. lulo cells are a potential model that will help to understand the features of this adhesion phenomenon. here, we analyze the interaction b ...201122082050
4-acetoxydolastane diterpene from the brazilian brown alga canistrocarpus cervicornis as antileishmanial agent.natural marine products have shown an interesting array of diverse and novel chemical structures with potent biological activities. our study reports the antiproliferative assays of crude extracts, fraction and pure compound (4r,9s,14s)-4α-acetoxy-9β,14α-dihydroxydolast-1(15),7-diene (1) obtained from brown alga canistrocarpus cervicornis showing the antileishmanial activity. we showed that 1 had a dose-dependent activity during 72 h of treatment, exhibiting ic(50) of 2.0 μg/ml, 12.0 μg/ml, and ...201122163190
immunological correlates of cure in the first american cutaneous leishmaniasis patient treated by immunotherapy in argentina. a case report.a patient with localized cutaneous leishmaniasis due to leishmania (leishmania) amazonensis infection was treated with an antigen containing heat-killed l. (l.) amazonensis promastigotes plus bcg. expression of t-cell differentiation, memory and senescence receptors markers were analyzed on t cell subpopulations, in order to establish the correlation between the percentages of expression of these receptors and his clinical status, at different stages of his follow up. the following case reports ...201122523846
use of in vivo and in vitro systems to select leishmania amazonensis expressing green fluorescent protein.various leishmania species were engineered with green fluorescent protein (gfp) using episomal vectors that encoded an antibiotic resistance gene, such as aminoglycoside geneticin sulphate (g418). most reports of gfp-leishmania have used the flagellated extracellular promastigote, the stage of parasite detected in the midgut of the sandfly vector; fewer studies have been performed with amastigotes, the stage of parasite detected in mammals. in this study, comparisons were made regarding the effi ...201122355202
in vitro antileishmanial, trypanocidal, and mammalian cell activities of diverse n,n' -dihetaryl substituted diamines and related compounds.the leishmaniasis and chagas diseases constitute a serious public health problem worldwide with few and ineffective treatment options. the search for new antiparasitic candidates at the initial steps of drug discovery and development is still necessary. the synthesis of 22 de novo synthetized n,n'-dihetaryl-alkyldiamine derivatives and in vitro antiparasitic activity were evaluated for the first time against intracellular and extracellular forms of leishmania (leishmania) infantum, l. (viannia) ...201223641328
[antileishmanial activity of six extracts from marine organisms].infections caused by protozoa of the genus leishmania are a global health problem with a high prevalence in underdeveloped countries. there is no vaccine against this disease at present and the treatment used is poor, so the search for more effective and safe medicines is an urgent need.201223444628
mitochondria superoxide anion production contributes to geranylgeraniol-induced death in leishmania amazonensis.here we demonstrate the activity of geranylgeraniol, the major bioactive constituent from seeds of bixa orellana, against leishmania amazonensis. geranylgeraniol was identified through (1)h and (13)c nuclear magnetic resonance imaging and dept. the compound inhibited the promastigote and intracellular amastigote forms, with ic(50) of 11 ± 1.0 and 17.5 ± 0.7 μg/ml, respectively. this compound was also more toxic to parasites than to macrophages and did not cause lysis in human blood cells. morpho ...201223304195
identification of sl addition trans-splicing acceptor sites in the internal transcribed spacer i region of pre-rrna in leishmania (leishmania) amazonensis.trypanosomatidae is a family of early branching eukaryotes harbouring a distinctive repertoire of gene expression strategies. functional mature messenger rna is generated via the trans-splicing and polyadenylation processing of constitutively transcribed polycistronic units. recently, trans-splicing of pre-small subunit ribosomal rna in the 5' external transcribed spacer region and of precursor trnasec have been described. here, we used a previously validated semi-nested reverse transcription-po ...201223295762
sphingolipid degradation in leishmania (leishmania) amazonensis.human leishmaniasis is caused by more than 20 leishmania species and has a wide range of symptoms. our recent studies have demonstrated the essential role of sphingolipid degradation in the virulence of leishmania (leishmania) major, a species responsible for localized cutaneous leishmaniasis in the old world. in this study, we investigated the function of sphingolipid degradation in leishmania (leishmania) amazonensis, an etiological agent of localized and diffuse cutaneous leishmaniasis in sou ...201223285302
molecular diagnosis of leishmania amazonensis in a captive spider monkey in bauru, são paulo, brazil.the municipality of bauru, são paulo, brazil, is an area endemic for leishmaniasis. at the zoo, a spider monkey (ateles paniscus) showed nonpathognomonic symptoms, such as weight loss and pale mucous membranes. blood was collected from the jugular vein and investigated for the presence of leishmania spp. dna by polymerase chain reaction and restriction fragment length polymorphism. parasite dna was detected, and the pattern observed was identical to leishmania amazonensis. this study presents mo ...201223272368
distinct transcriptional signatures of bone marrow-derived c57bl/6 and dba/2 dendritic leucocytes hosting live leishmania amazonensis amastigotes.the inoculation of a low number (10(4)) of l. amazonensis metacyclic promastigotes into the dermis of c57bl/6 and dba/2 mouse ear pinna results in distinct outcome as assessed by the parasite load values and ear pinna macroscopic features monitored from days 4 to 22-phase 1 and from days 22 to 80/100-phase 2. while in c57bl/6 mice, the amastigote population size was increasing progressively, in dba/2 mice, it was rapidly controlled. this latter rapid control did not prevent intracellular amastig ...201223272268
the immunomodulatory effect of plant lectins: a review with emphasis on artinm properties.advances in the glycobiology and immunology fields have provided many insights into the role of carbohydrate-protein interactions in the immune system. we aim to present a comprehensive review of the effects that some plant lectins exert as immunomodulatory agents, showing that they are able to positively modify the immune response to certain pathological conditions, such as cancer and infections. the present review comprises four main themes: (1) an overview of plant lectins that exert immunomo ...201323299509
leishmania amazonensis amastigotes trigger neutrophil activation but resist neutrophil microbicidal mechanisms.neutrophils are the first cells to infiltrate to the site of leishmania promastigote infection, and these cells help to reduce parasite burden shortly after infection is initiated. several clinical reports indicate that neutrophil recruitment is sustained over the course of leishmaniasis, and amastigote-laden neutrophils have been isolated from chronically infected patients and experimentally infected animals. the goal of this study was to compare how thioglycolate-elicited murine neutrophils re ...201323918780
trypanosoma cruzi differentiates and multiplies within chimeric parasitophorous vacuoles in macrophages coinfected with leishmania amazonensis.the trypanosomatids leishmania amazonensis and trypanosoma cruzi are excellent models for the study of the cell biology of intracellular protozoan infections. after their uptake by mammalian cells, the parasitic protozoan flagellates l. amazonensis and t. cruzi lodge within acidified parasitophorous vacuoles (pvs). however, whereas l. amazonensis develops in spacious, phagolysosome-like pvs that may enclose numerous parasites, t. cruzi is transiently hosted within smaller vacuoles from which it ...201626975994
identification of differentially expressed proteins from leishmania amazonensis associated with the loss of virulence of the parasites.the present study analyzed whether or not the in vitro cultivation for long periods of time of pre-isolated leishmania amazonensis from lesions of chronically infected balb/c mice was able to interfere in the parasites' infectivity using in vivo and in vitro experiments. in addition, the proteins that presented a significant decrease or increase in their protein expression content were identified applying a proteomic approach.201424699271
cell-to-cell transfer of leishmania amazonensis amastigotes is mediated by immunomodulatory lamp-rich parasitophorous extrusions.the last step of leishmania intracellular life cycle is the egress of amastigotes from the host cell and their uptake by adjacent cells. using multidimensional live imaging of long-term-infected macrophage cultures we observed that leishmania amazonensis amastigotes were transferred from cell to cell when the donor host macrophage delivers warning signs of imminent apoptosis. they were extruded from the macrophage within zeiotic structures (membrane blebs, an apoptotic feature) rich in phagolyso ...201424824158
leishmania-mediated inhibition of iron export promotes parasite replication in macrophages.leishmania parasites infect macrophages, cells that play an important role in organismal iron homeostasis. by expressing ferroportin, a membrane protein specialized in iron export, macrophages release iron stored intracellularly into the circulation. iron is essential for the intracellular replication of leishmania, but how the parasites compete with the iron export function of their host cell is unknown. here, we show that infection with leishmania amazonensis inhibits ferroportin expression in ...201424497831
enhancement of experimental cutaneous leishmaniasis by leishmania extract: identification of a disease-associated antibody specificity.both leishmania braziliensis and leishmania amazonensis induce cutaneous disease when injected in the skin of balb/c mice. however, l. amazonensis may also visceralize in that strain of mice, infecting mainly the liver and spleen. in addition, whereas balb/c mice die with a progressive cutaneous disease when infected by l. amazonensis, the infection by l. braziliensis is spontaneously cured. in a previous work, we have found that intravenous injections of l. amazonensis amastigote extract (lae) ...201525971623
lipophosphoglycans from leishmania amazonensis strains display immunomodulatory properties via tlr4 and do not affect sand fly infection.the immunomodulatory properties of lipophosphoglycans (lpg) from new world species of leishmania have been assessed in leishmania infantum and leishmania braziliensis, the causative agents of visceral and cutaneous leishmaniasis, respectively. this glycoconjugate is highly polymorphic among species with variation in sugars that branch off the conserved gal(β1,4)man(α1)-po4 backbone of repeat units. here, the immunomodulatory activity of lpgs from leishmania amazonensis, the causative agent of di ...201627508930
leishmania amazonensis dna in wild females of lutzomyia cruzi (diptera: psychodidae) in the state of mato grosso do sul, brazil.studies on natural infection by leishmania spp of sandflies collected in endemic and nonendemic areas can provide important information on the distribution and intensity of the transmission of these parasites. this study sought to investigate the natural infection by leishmaniain wild female sandflies. the specimens were caught in the city of corumbá, state of mato grosso do sul (brazil) between october 2012-march 2014, and dissected to investigate flagellates and/or submitted to molecular analy ...201526602870
ecological niche modelling predicts southward expansion of lutzomyia (nyssomyia) flaviscutellata (diptera: psychodidae: phlebotominae), vector of leishmania (leishmania) amazonensis in south america, under climate change.vector borne diseases are susceptible to climate change because distributions and densities of many vectors are climate driven. the amazon region is endemic for cutaneous leishmaniasis and is predicted to be severely impacted by climate change. recent records suggest that the distributions of lutzomyia (nyssomyia) flaviscutellata and the parasite it transmits, leishmania (leishmania) amazonensis, are expanding southward, possibly due to climate change, and sometimes associated with new human inf ...201526619186
natural infection of phlebotomines (diptera: psychodidae) by leishmania (leishmania) amazonensis in an area of ecotourism in central-western brazil.bonito municipality, known as an area of ecoturism, in mato grosso do sul state, brazil, is also a focus of visceral and cutaneous leishmaniases, with cases registered in both human and canine populations. this study sought to investigate natural infection by flagellate forms of leishmania in phlebotomines of the urban area of bonito.201526435708
divergent profile of emerging cutaneous leishmaniasis in subtropical brazil: new endemic areas in the southern frontier.although known to be highly endemic in the amazon regions of brazil, the presence of cutaneous leishmaniasis (cl) in the subtropical southern part of the country has largely been ignored. this study was conducted to demonstrate cl is emerging in the brazilian state of santa catarina, as well as to characterize the epidemiological profile and leishmania species involved.201323457521
nucleosides present on phlebotomine saliva induce immunossuppression and promote the infection establishment.sand fly saliva plays a crucial role in establishing leishmania infection. we identified adenosine (ado) and adenosine monophosphate (amp) as active pharmacologic compounds present in phlebotomus papatasi saliva that inhibit dendritic cell (dc) functions through a pge2/il 10-dependent mechanism.201525849562
salivary gland homogenates from wild-caught sand flies lutzomyia flaviscutellata and lutzomyia (psychodopygus) complexus showed inhibitory effects on leishmania (leishmania) amazonensis and leishmania (viannia) braziliensis infection in balb/c mice.during the natural transmission of leishmania parasites, the infected sand fly female regurgitates promastigotes into the host's skin together with its saliva. it has been reported that vector saliva contains immunomodulatory molecules that facilitate the establishment of infection. thus, the main objective of this study was to evaluate the specificity of lutzomyia (lu.) flaviscutellata and lu. (psychodopygus) complexus salivas on the infectivity of leishmania (l.) (leishmania) amazonensis and l ...201425476864
chronic infection by leishmania amazonensis mediated through mapk erk mechanisms.leishmania amazonensis is an intracellular protozoan parasite responsible for chronic cutaneous leishmaniasis (cl). cl is a neglected tropical disease responsible for infecting millions of people worldwide. l. amazonensis promotes alteration of various signaling pathways that are essential for host cell survival. specifically, through parasite-mediated phosphorylation of extracellular signal regulated kinase (erk), l. amazonensis inhibits cell-mediated parasite killing and promotes its own survi ...024838145
comparative genomics of canine-isolated leishmania (leishmania) amazonensis from an endemic focus of visceral leishmaniasis in governador valadares, southeastern brazil.leishmaniasis is a highly diverse group of diseases caused by kinetoplastid of the genus leishmania. these parasites are taxonomically diverse, with human pathogenic species separated into two subgenera according to their development site inside the alimentary tract of the sand fly insect vector. the disease encompasses a variable spectrum of clinical manifestations with tegumentary or visceral symptoms. among the causative species in brazil, leishmania (leishmania) amazonensis is an important e ...201728091623
antileishmanial activity of the essential oil from tetradenia riparia obtained in different seasons.the herbaceous shrub tetradenia riparia has been traditionally used to treat inflammatory and infectious diseases. recently, a study showed that t. riparia essential oil (treo) obtained in summer has antileishmanial effects, although these results could be influenced by seasonal variation. this study evaluated the activity of the treo obtained in different seasons against leishmania (leishmania) amazonensis, in vitro and in vivo. the compounds in the treo were analysed by gas chromatography-mass ...201526602873
expression of calpain-like proteins and effects of calpain inhibitors on the growth rate of angomonas deanei wild type and aposymbiotic strains.angomonas deanei is a trypanosomatid parasite of insects that has a bacterial endosymbiont, which supplies amino acids and other nutrients to its host. bacterium loss induced by antibiotic treatment of the protozoan leads to an aposymbiotic strain with increased need for amino acids and results in increased production of extracellular peptidases. in this work, a more detailed examination of a. deanei was conducted to determine the effects of endosymbiont loss on the host calpain-like proteins (c ...201526415499
leishmania amazonensis exhibits phosphatidylserine-dependent procoagulant activity, a process that is counteracted by sandfly saliva.leishmania parasites expose phosphatidylserine (ps) on their surface, a process that has been associated with regulation of host's immune responses. in this study we demonstrate that ps exposure by metacyclic promastigotes of leishmania amazonensis favours blood coagulation. l. amazonensis accelerates in vitro coagulation of human plasma. in addition, l. amazonensis supports the assembly of the prothrombinase complex, thus promoting thrombin formation. this process was reversed by annexin v whic ...024037188
leishmania metacyclogenesis is promoted in the absence of purines.leishmania parasites, the causative agent of leishmaniasis, are transmitted through the bite of an infected sand fly. leishmania parasites present two basic forms known as promastigote and amastigote which, respectively, parasitizes the vector and the mammalian hosts. infection of the vertebrate host is dependent on the development, in the vector, of metacyclic promastigotes, however, little is known about the factors that trigger metacyclogenesis in leishmania parasites. it has been generally s ...201223050028
cutaneous leishmaniasis vaccination: a matter of quality.there have been exhaustive efforts to develop an efficient vaccine against leishmaniasis. factors like host and parasite genetic characteristics, virulence, epidemiological scenarios, and, mainly, diverse immune responses triggered by leishmania species make the achievement of this aim a complex task. it is already clear that the induction of a th1, pro-inflammatory response, is important in the protection against leishmania infection. however, many questions must still be answered to fully unde ...201627148270
a novel molecular test to diagnose canine visceral leishmaniasis at the point of care.dogs are the principal reservoir hosts of zoonotic visceral leishmaniasis (vl) but current serological methods are not sensitive enough to detect all subclinically infected animals, which is crucial to vl control programs. polymerase chain reaction (pcr) methods have greater sensitivity but require expensive equipment and trained personnel, impairing its implementation in endemic areas. we developed a diagnostic test that uses isothermal recombinase polymerase amplification (rpa) to detect leish ...201526240156
bioactive endophytic fungi isolated from caesalpinia echinata lam. (brazilwood) and identification of beauvericin as a trypanocidal metabolite from fusarium sp.aiming to identify new sources of bioactive secondary metabolites, we isolated 82 endophytic fungi from stems and barks of the native brazilian tree caesalpinia echinata lam. (fabaceae). we tested their ethyl acetate extracts in several in vitro assays. the organic extracts from three isolates showed antibacterial activity against staphylococcus aureus and escherichia coli [minimal inhibitory concentration (mic) 32-64 μg/ml]. one isolate inhibited the growth of salmonella typhimurium (mic 64 μg/ ...201525742265
antibacterial, antifungal and antileishmanial activities of indolone-n-oxide derivatives.an alarming increase in microbial resistance to traditional drugs and classical pharmacophores has spurred the search for new antimicrobial compounds. indolone-n-oxides (inods) possess a redox pharmacophore with promising, recently established, antimalarial activities. in this study, the anti-infectious properties of a series of inods were investigated. the antibacterial activity was evaluated against five bacterial strains gram-positive (staphylococcus aureus, enterococcus hirae), gram-negative ...201222828966
bioactive compounds of aspergillus terreus-f7, an endophytic fungus from hyptis suaveolens (l.) poit.the compounds terrein (1), butyrolactone i (2), and butyrolactone v (3) were isolated from the ethyl acetate extract (etoac) of the endophytic fungus aspergillus terreus-f7 obtained from hyptis suaveolens (l.) poit. the extract and the compounds presented schistosomicidal activity against schistosoma mansoni; at 100 µg/ml for etoac extract, 1297.3 µm for compound 1, 235.6 µm for compound 2, and 454.1 µm for compound 3, they killed 100% of the parasites after 72 h of treatment. compounds 1, 2, an ...201728243983
antimicrobial activity of plants used as medicinals on an indigenous reserve in rio das cobras, paraná, brazil.a considerable percentage of global biodiversity is located in brazil, a country that also has rich cultural and ethnic diversity. in the community of rio das cobras, paraná, plants are still widely used in the health care not only by indigenous people but also by the non-indigenous population that inhabits the region. the investigation of the efficacy and safety of these plants in the treatment of infectious diseases provides insights for future studies of these species allowing the appropriate ...201222867638
biological activities of croton palanostigma klotzsch.different species of croton are used in traditional amazonian medicine. among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers.201627041867
anti-infective assessment of senecio smithioides (asteraceae) and isolation of 9-oxoeuryopsin, a furanoeremophilane-type sesquiterpene with antiplasmodial activity.the search for anti-infective activity in the antipyretic plant senecio smithioides was conducted. petroleum ether (pe), dichloromethane (ch2cl2), ethyl acetate (etoac) and hydroethanolic (96% etoh) extracts, and compounds 9-oxoeuryopsin (1), epoxydecompostin (2) and senecionine (3) were obtained from the aerial parts. all extracts and 1 were tested against chloroquine-resistant strain of plasmodium falciparum (ref. chloroquine), trypanosoma cruzi (ref. nifurtimox), leishmania braziliensis, leis ...201526606687
biological activities of croton palanostigma klotzsch.different species of croton are used in traditional amazonian medicine. among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers.201726246738
bioactive endophytic fungi isolated from caesalpinia echinata lam. (brazilwood) and identification of beauvericin as a trypanocidal metabolite from fusarium sp.aiming to identify new sources of bioactive secondary metabolites, we isolated 82 endophytic fungi from stems and barks of the native brazilian tree caesalpinia echinata lam. (fabaceae). we tested their ethyl acetate extracts in several in vitro assays. the organic extracts from three isolates showed antibacterial activity against staphylococcus aureus and escherichia coli [minimal inhibitory concentration (mic) 32-64 μg/ml]. one isolate inhibited the growth of salmonella typhimurium (mic 64 μg/ ...201525606862
discovery of the rapanone and suberonone mixture as a motif for leishmanicidal and antifungal applications.leishmaniasis and fungal infections are significant diseases impacting worldwide public health. treatments have developed greatly over time, however, there is a necessity to discover less toxic drugs, which have greater efficacy and are more economically accessible. this work conducted a screening of cerrado species extracts: connarus suberosus planch. (connaraceae), neea theifera oerst. (nyctaginaceae) and myrcia linearifolia cambess. (myrtaceae) against leishmania (leishmania) amazonensis, der ...201424331757
treatment of leishmania (leishmania) amazonensis-infected mice with a combination of a palladacycle complex and heat-killed propionibacterium acnes triggers protective cellular immune responses.palladacycle complex dppe 1.2 was previously reported to inhibit the in vitro and in vivo infection by leishmania (leishmania) amazonensis. the aim of the present study was to compare the effect of dppe 1.2, in association with heat-killed propionibacterium acnes, on l. (l.) amazonensis infection in two mouse strains, balb/c and c57bl/6, and to evaluate the immune responses of the treated animals. foot lesions of l. (l.) amazonensis-infected mice were injected with dppe 1.2 alone, or associated ...201728321209
functional complementation of leishmania (leishmania) amazonensis ap endonuclease gene (lamap) in escherichia coli mutant strains challenged with dna damage agents.during its life cycle leishmania spp. face several stress conditions that can cause dna damages. base excision repair plays an important role in dna maintenance and it is one of the most conserved mechanisms in all living organisms. dna repair in trypanosomatids has been reported only for old world leishmania species. here the ap endonuclease from leishmania (l.) amazonensis was cloned, expressed in escherichia coli mutants defective on the dna repair machinery, that were submitted to different ...201627223868
characterization and optimization of artinm lectin expression in escherichia coli.artinm is a d-mannose-specific lectin from artocarpus integrifolia seeds that induces neutrophil migration and activation, degranulation of mast cells, acceleration of wound healing, induction of interleukin-12 production by macrophages and dendritic cells, and protective t helper 1 immune response against leishmania major, leishmania amazonensis and paracoccidioides brasiliensis infections. considering the important biological properties of artinm and its therapeutic applicability, this study w ...201222857259
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.the 2-acylamino-5-nitro-1,3-thiazole derivatives (1-14) were prepared using a one step reaction. all compounds were tested in vitro against four neglected protozoan parasites (giardia intestinalis, trichomonas vaginalis, leishmania amazonensis and trypanosoma cruzi). acetamide (9), valeroylamide (10), benzamide (12), methylcarbamate (13) and ethyloxamate (14) derivatives were the most active compounds against g. intestinalis and t. vaginalis, showing nanomolar inhibition. compound 13 (ic50=10nm) ...201424529307
leishmaniasis recidivans in ethiopia: cutaneous and mucocutaneous features.cutaneous leishmaniasis (cl) is endemic in ethiopia. an unusual clinical form of this disease is leishmaniasis recidivans (lr), a prolonged, relapsing form of cutaneous leishmaniasis resembling tuberculosis of the skin that may persist for many years with a chronic and relapsing course. this rare variant has been shown to be caused by leishmania tropica species in the old world and by leishmania braziliensis, leishmania amazonensis, leishmania panamensis, and leishmania guyanensis in the new wor ...201728141598
the anti-trichomonas vaginalis phloroglucinol derivative isoaustrobrasilol b modulates extracellular nucleotides hydrolysis.trichomonas vaginalis causes trichomoniasis, a neglected sexually transmitted disease. due to severe health consequences and treatment failure, new therapeutic alternatives are crucial. phloroglucinols from southern brazilian hypericum species demonstrated anti-t. vaginalis and anti-leishmania amazonensis activities. the modulation of biochemical pathways involved in the control of inflammatory response by ectonucleotidases, ntpdase and ecto-5'-nucleotidase, represents new targets for combating ...201728390095
glycosylated metal chelators as anti-parasitic agents with tunable selectivity.trypanosoma cruzi and leishmania amazonensis are the causative agents of chagas' disease and leishmaniasis, respectively. these conditions affect millions of people worldwide, especially in developing countries. as such, there is an urgent need for novel, efficient and cost-effective treatments for these diseases, given the growing resistance and side-effects of current therapies. this work details the synthesis and evaluation of the anti-parasitic activity of novel amino- and iminopyridyl metal ...201728382355
exploring the association of surface plasmon resonance with recombinant mhc:ig hybrid protein as a tool for detecting t lymphocytes in mice infected with leishmania (leishmania) amazonensis.a surface plasmon resonance- (spr-) based recognition method applying h-2 l(d):ig/peptides complexes for ex vivo monitoring cellular immune responses during murine infection with leishmania (leishmania) amazonensis is described. lymphocytes from lesion-draining popliteal lymph nodes were captured on a carboxylated sensor chip surface previously functionalized with h-2 l(d):ig (dimerx) protein bound to synthetic peptides derived from the cooh-terminal region of cysteine proteinase b of l. (l.) am ...201728373990
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