Publications

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classical ros-dependent and early/rapid ros-independent release of neutrophil extracellular traps triggered by leishmania parasites.neutrophil extracellular traps (nets) extruded from neutrophils upon activation are composed of chromatin associated with cytosolic and granular proteins, which ensnare and kill microorganisms. this microbicidal mechanism named classical netosis has been shown to dependent on reactive oxygen species (ros) generation by nadph oxidase and also chromatin decondensation dependent upon the enzymes (pad4), neutrophil elastase (ne) and myeloperoxidase (mpo). net release also occurs through an early/rap ...201526673780
il-27 enhances leishmania amazonensis infection via ds-rna dependent kinase (pkr) and il-10 signaling.the protozoan parasite leishmania infects and replicates in macrophages, causing a spectrum of diseases in the human host, varying from cutaneous to visceral clinical forms. it is known that cytokines modulate the immunological response against leishmania and are relevant for infection resolution. here, we report that interleukin (il)-27 increases leishmania amazonensis replication in human and murine macrophages and that the blockage of the il-10 receptor on the surface of infected cells abolis ...201525466588
synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents.quinoxalines belong to the n-containing heterocyclic compounds that stand out as having promising biological activity due to their privileged scaffold. in this work, we report the synthesis, antileishmanial, and antitrypanosomal properties of 46 new 2,3-disubstituted quinoxaline and 40 previously reported derivatives. among all of the compounds screened for in vitro activity against epimastigotes and trypomastigotes of trypanosoma cruzi and promastigotes of leishmania amazonensis as well as mamm ...201525461316
syzygium cumini (l.) skeels essential oil and its major constituent α-pinene exhibit anti-leishmania activity through immunomodulation in vitro.syzygium cumini (l.) skeels (myrtaceae), commonly known as "jambolão" in brazil is widely used in folk medicine against leishmaniasis, inflammation, chronic diarrhea, and ulcers. it is one of the most commonly used plants for the treatment of diabetes worldwide. in previous studies, syzygium cumini was shown to possess antihyperlipidemic and anti-allergic properties, and to exhibit good performance as an antimicrobial agent against bacteria, fungi, and protozoa parasites of the genus leishmania ...201525460590
a putative role for inosine 5' monophosphate dehydrogenase (impdh) in leishmania amazonensis programmed cell death.leishmania amazonensis undergoes apoptosis-like programmed cell death (pcd) under heat shock conditions. we identified a potential role for inosine 5' monophosphate dehydrogenase (impdh) in l. amazonensis pcd. trypanosomatids do not have a "de novo" purine synthesis pathway, relying on the salvage pathway for survival. impdh, a key enzyme in the purine nucleotide pathway, is related to cell growth and apoptosis. since guanine nucleotide depletion triggers cell cycle arrest and apoptosis in sever ...201525499513
in vitro evaluation of (-)α-bisabolol as a promising agent against leishmania amazonensis.current treatments for leishmaniasis present some difficulties due to their toxicity, the use of the intravenous route for administration and therapy duration, which may lead to treatment discontinuation. the aim of this study is to investigate new treatment alternatives to improve patients well being. therefore, we evaluated the inhibitory effect of (-)α-bisabolol, a sesquiterpene alcohol found in various essential oils of different plant species, against the promastigotes and intracellular ama ...201525448354
photodynamic effects of zinc phthalocyanines on intracellular amastigotes of leishmania amazonensis and leishmania braziliensis.this study investigated the photoactivity of four zinc phthalocyanines (pczns) on a murine macrophage cell line infected with leishmania amazonensis or leishmania braziliensis. infected and uninfected cells were incubated with pczns at different concentrations (1-10 μm) for 3 h and then exposed to an led device in continuous wave mode at 660 nm with a fluency of 50 j/cm(2) (25 mv). enzymatic activity was determined by mtt assay 24 h after light treatment. the results demonstrated that all pczns ...201525288263
nanobiotechnologic approach to a promising vaccine prototype for immunisation against leishmaniasis: a fast and effective method to incorporate gpi-anchored proteins of leishmania amazonensis into liposomes.liposomes are known to be a potent adjuvant for a wide range of antigens, as well as appropriate antigen carriers for antibody generation response in vivo. in addition, liposomes are effective vehicles for peptides and proteins, thus enhancing their immunogenicity. considering these properties of liposomes and the antigenicity of the leishmania membrane proteins, we evaluated if liposomes carrying glycosylphosphatidylinositol (gpi)-anchored proteins of leishmania amazonensis promastigotes could ...201525265060
arginase i, polyamine, and prostaglandin e2 pathways suppress the inflammatory response and contribute to diffuse cutaneous leishmaniasis.diffuse cutaneous leishmaniasis (dcl) is a rare clinical manifestation of tegumentary leishmaniasis. the molecular mechanisms underlying dcl pathogenesis remain unclear, and there is no efficient treatment available. this study investigated the systemic and in situ expression of the inflammatory response that might contribute to suppression in dcl. the plasma levels of arginase i, ornithine decarboxylase (odc), transforming growth factor β (tgf-β), and prostaglandin e2 (pge2) were higher in pati ...201525124926
increased tau phosphorylation and receptor for advanced glycation endproducts (rage) in the brain of mice infected with leishmania amazonensis.leishmaniasis is a parasitosis caused by several species of the genus leishmania, an obligate intramacrophagic parasite. although neurologic symptoms have been observed in human cases of leishmaniasis, the manifestation of neurodegenerative processes is poorly studied. the aim of the present work was to investigate if peripheral infection of balb/c mice with leishmania amazonensis affects tau phosphorylation and rage protein content in the brain, which represent biochemical markers of neurodegen ...201525014011
the 2',4'-dihydroxychalcone could be explored to develop new inhibitors against the glycerol-3-phosphate dehydrogenase from leishmania species.the enzyme glycerol-3-phosphate dehydrogenase (g3pdh) from leishmania species is considered as an attractive target to design new antileishmanial drugs and a previous in silico study reported on the importance of chalcones to achieve its inhibition. here, we report the identification of a synthetic chalcone in our in vitro assays with promastigote cells from leishmania amazonensis, its biological activity in animal models, and docking followed by molecular dynamics simulation to investigate the ...201526169126
leishmania is not prone to develop resistance to tamoxifen.tamoxifen, an antineoplastic agent, is active in vitro and in vivo against the parasitic protozoa leishmania. as part of our efforts to unravel this drug's mechanisms of action against the parasite and understand how resistance could arise, we tried to select tamoxifen-resistant leishmania amazonensis. three different strategies to generate tamoxifen resistant mutants were used: stepwise increase in drug concentration applied to promastigote cultures, chemical mutagenesis followed by drug select ...201526150922
expression of glyceraldehyde 3-phosphate dehydrogenase is enhanced in leishmania spp naturally resistant to nitric oxide.leishmania spp are the causative agents of a spectrum of diseases termed leishmaniasis that affect mammals, including humans and dogs. although reactive nitrogen species are employed in the control of parasitism by the immune system, it is known that leishmania can withstand this oxidative stress. as the mechanism by which these species are resistant to nitric oxide (no) is poorly understood, the main objective of this study was to evaluate the expression of glyceraldehyde 3-phosphate dehydrogen ...201526125921
antileishmanial activity of essential oil and 6,7-dehydroroyleanone isolated from tetradenia riparia.tetradenia riparia plant is used as a traditional medicine in africa for the treatment of inflammatory and infectious diseases as like parasitic. therapy for leishmaniasis caused by leishmania (leishmania) amazonensis specie often fails, and the conventional drugs are toxic, expensive, require a long period of treatment, and adverse effects are common. the alternative therapies using natural products are inexpensive and have few or any adverse reaction. these reasons are sufficient to investigat ...201526116864
novel dialkylphosphorylhydrazones: synthesis, leishmanicidal evaluation and theoretical investigation of the proposed mechanism of action.as part of a program to develop new drugs for the treatment of neglected diseases, new dialkylphosphorylhydrazones were synthesized and evaluated against the trypanosomatid parasites leishmania braziliensis and leishmania amazonensis. the synthesis of these compounds proved satisfactory with yields ranging from moderate to good. the most active compounds against l. braziliensis presented ic50 values in the 10(-2) μm range, similar to that of the reference drug pentamidine. two compounds, 4m and ...201526107111
phage-fused epitopes from leishmania infantum used as immunogenic vaccines confer partial protection against leishmania amazonensis infection.two mimotopes of leishmania infantum identified by phage display were evaluated as vaccine candidates in balb/c mice against leishmania amazonensis infection. the epitope-based immunogens, namely b10 and c01, presented as phage-fused peptides; were used without association of a th1 adjuvant, and they were administered isolated or in combination into animals. both clones showed a specific production of interferon-gamma (ifn-γ), interleukin-12 (il-12) and granulocyte/macrophage colony-stimulating ...201526099574
biological characterization of the amazon coral micrurus spixii snake venom: isolation of a new neurotoxic phospholipase a2.the micrurus genus is the american representative of elapidae family. micrurus spixii is endemic of south america and northern states of brazil. elapidic venoms contain neurotoxins that promote curare-mimetic neuromuscular blockage. in this study, biochemical and functional characterizations of m. spixii crude venom were performed and a new neurotoxic phospholipase a2 called mspla2-i was isolated. m. spixii crude venom caused severe swelling in the legs of tested mice and significant release of ...201526095535
synthesis and biological evaluation of novel piperidine-benzodioxole derivatives designed as potential leishmanicidal drug candidates.a novel series of ester and carbamate derivatives was synthesized and evaluated its activities against leishmania amazonensis. all compounds exhibited weaker leishmanicidal activity than amphotericin b. however, results indicated that substituents on the aryl-acyl subunit are important for modulation of the leishmanicidal effect. the nitro derivative showed the highest activity of the series with an ic50 = 17.24 μm, and comparable potency to the 3,4-benzodioxole ester and n-hexyl carbamate deriv ...201526094119
kaurenoic acid possesses leishmanicidal activity by triggering a nlrp12/il-1β/cnos/no pathway.leishmania amazonensis (l. amazonensis) infection can cause severe local and diffuse injuries in humans, a condition clinically known as american cutaneous leishmaniasis (acl). currently, the therapeutic approach for acl is based on glucantime, which shows high toxicity and poor effectiveness. therefore, acl remains a neglected disease with limited options for treatment. herein, the in vitro antiprotozoal effect and mechanisms of the diterpene kaurenoic acid [ent-kaur-16-en-19-oic acid] (ka) aga ...201526074677
modulation of na+/k+ atpase activity by hydrogen peroxide generated through heme in l. amazonensis.leishmania amazonensis is a protozoan parasite that occurs in many areas of brazil and causes skin lesions. using this parasite, our group showed the activation of na+/k+ atpase through a signaling cascade that involves the presence of heme and protein kinase c (pkc) activity. heme is an important biomolecule that has pro-oxidant activity and signaling capacity. reactive oxygen species (ros) can act as second messengers, which are required in various signaling cascades. our goal in this work is ...201526070143
synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.chalcones form a class of compounds that belong to the flavonoid family and are widely distributed in plants. their simple structure and the ease of preparation make chalcones attractive scaffolds for the synthesis of a large number of derivatives enabling the evaluation of the effects of different functional groups on biological activities. in this letter, we report the successful synthesis of a series of novel prenylated chalcones via claisen-schmidt condensation and the evaluation of their ef ...201526055530
cinnamic acid derived compounds loaded into liposomes: antileishmanial activity, production standardisation and characterisation.synthetic compounds derived from cinnamic acid were tested in cultures containing the promastigote form of leishmania amazonensis and the dimethylsulphoxide solution of b2 compound (2.0 mg/ml) led to a 92% decrease of leishmania in 96 h of treatment. then, different liposomal systems (diameters ∼200 nm) were prepared by the extrusion method in the presence and absence of compounds studied. dsc thermograms of the liposomes in the presence of these compounds caused changes in δh, tm and δt1/2, com ...201526052723
analysis of iron superoxide dismutase-encoding dna vaccine on the evolution of the leishmania amazonensis experimental infection.the present work aimed to evaluate the immunogenicity of leishmania amazonensis iron superoxide dismutase (sod)-encoding dna experimental vaccine and the protective properties of this dna vaccine during infection. the sod gene was subcloned into the pvax1 plasmid, and it was used to immunize balb/c mice. twenty-one days after the last immunization, mice were sacrificed (immunogenicity studies) or subcutaneously challenged with l. amazonensis (studies of protection), and alterations in cellular a ...201526040192
il-18 contributes to susceptibility to leishmania amazonensis infection by macrophage-independent mechanisms.we evaluated the role of il-18 during leishmania amazonensis infection in c57bl/6 mice, using il-18ko mice. we showed that il-18 is involved in susceptibility to l. amazonensis, since il-18ko mice presented reduced lesions and parasite loads. because macrophages are the host cells of the parasite, we investigated if macrophages were involved in il-18-mediated susceptibility to l. amazonensis. we showed that macrophages obtained from wt or il-18ko responded similarly to l. amazonensis infection. ...201526009021
the heme transport capacity of lhr1 determines the extent of virulence in leishmania amazonensis.leishmania spp. are trypanosomatid parasites that replicate intracellularly in macrophages, causing serious human morbidity and mortality throughout the world. trypanosomatid protozoa cannot synthesize heme, so must acquire this essential cofactor from their environment. earlier studies identified lhr1 as a leishmania amazonensis transmembrane protein that mediates heme uptake. null mutants of lhr1 are not viable and single knockout strains have reduced virulence, but very little is known about ...201526001191
nitric oxide and brazilian propolis combined accelerates tissue repair by modulating cell migration, cytokine production and collagen deposition in experimental leishmaniasis.the fact that drugs currently used in the treatment of leishmania are highly toxic and associated with acquired resistance has promoted the search for new therapies for treating american tegumentary leishmaniasis (atl). in this study, balb/c mice were injected in the hind paw with leishmania (leishmania) amazonensis and subsequently treated with a combination of nitric oxide (no) donor (cis-[ru(bpy) 2imn(no)](pf6)3) (ru-no), given by intraperitoneal injection, and oral brazilian propolis for 30 ...201525973801
the efficacy of 2-nitrovinylfuran derivatives against leishmania in vitro and in vivo.despite recent advances in the treatment of some forms of leishmaniasis, the available drugs are still far from ideal due to inefficacy, parasite resistance, toxicity and cost. the wide-spectrum antimicrobial activity of 2-nitrovinylfuran compounds has been described, as has their activity against trichomonas vaginalis and other protozoa. thus, the aim of this study was to test the antileishmanial activities of six 2-nitrovinylfurans in vitro and in a murine model of leishmaniasis. minimum paras ...201525946239
synthesis and characterization of bismuth(iii) and antimony(v) porphyrins: high antileishmanial activity against antimony-resistant parasite.two bismuth(iii) porphyrins-5,10,15,20-tetrakis(phenyl)porphyrinatobismuth(iii) nitrate, [bi(iii)(tpp)]no3, and the unprecedent 5,10,15,20-tetrakis(4-carbomethoxyphenyl)porphyrinatobismuth(iii) nitrate, [bi(iii)(t4cmpp)]no3, and two unprecedented antimony(v) porphyrins dichlorido(5,10,15,20-tetrakis(phenyl)porphyrinato)antimony(v) bromide, [sb(v)(tpp)cl2]br, and dibromido(5,10,15,20-tetrakis(4-carbomethoxyphenyl)porphyrinato)antimony(v) bromide, [sb(v)(t4cmpp)br2]br,-were synthesized by reacting ...201525929728
high selective antileishmanial activity of vanadium complex with stilbene derivative.leishmaniasis is a group of disease caused by different species of the parasite leishmania affecting millions of people worldwide. conventional therapy relies on multiple parenteral injections with pentavalent antimonials which exhibit high toxicity and various side effects have been reported. hence, the research for an effective and low toxic effect drug is necessary. in the present work, the synthesis, spectroscopic and analytical characterizations of stilbene derivative (h2salophen) and its v ...201525917716
immunohistochemical evidence of stress and inflammatory markers in mouse models of cutaneous leishmaniosis.leishmanioses are chronic parasitic diseases and host responses are associated with pro- or anti-inflammatory cytokines involved, respectively, in the control or exacerbation of infection. the relevance of other inflammatory mediators and stress markers has not been widely studied and there is a need to search for biomarkers to leishmaniasis. in this work, the stress and inflammatory molecules p38 mitogen-activated protein kinase, cyclooxygenase-2, migration inhibitory factor, macrophage inflamm ...201525896942
ifn-γ-dependent recruitment of cd4(+) t cells and macrophages contributes to pathogenesis during leishmania amazonensis infection.interferon gamma (ifn-γ) is a key factor in the protection of hosts against intracellular parasites. this cytokine induces parasite killing through nitric oxide and reactive oxygen species production by phagocytes. surprisingly, during leishmania amazonensis infection, ifn-γ plays controversial roles. during in vitro infections, ifn-γ induces the proliferation of the amastigote forms of l. amazonensis. however, this cytokine is not essential at the beginning of an in vivo infection. it is not cl ...201526401717
the human parasite leishmania amazonensis downregulates inos expression via nf-κb p50/p50 homodimer: role of the pi3k/akt pathway.leishmania amazonensis activates the nf-κb transcriptional repressor homodimer (p50/p50) and promotes nitric oxide synthase (inos) downregulation. we investigated the role of pi3k/akt in p50/p50 nf-κb activation and the effect on inos expression in l. amazonensis infection. the increased occupancy of p50/p50 on the inos promoter of infected macrophages was observed and we demonstrated that both p50/p50 nf-κb induction and inos downregulation in infected macrophages depended on pi3k/akt activatio ...201526400473
effect of aliphatic, monocarboxylic, dicarboxylic, heterocyclic and sulphur-containing amino acids on leishmania spp. chemotaxis.in the sand-fly mid gut, leishmania promastigotes are exposed to acute changes in nutrients, e.g. amino acids (aas). these metabolites are the main energy sources for the parasite, crucial for its differentiation and motility. we analysed the migratory behaviour and morphological changes produced by aliphatic, monocarboxylic, dicarboxylic, heterocyclic and sulphur-containing aas in leishmania amazonensis and leishmania braziliensis and demonstrated that l-methionine (10-12 m), l-tryptophan (10-1 ...201526396059
intranasal vaccination with killed leishmania amazonensis promastigotes antigen (laag) associated with caf01 adjuvant induces partial protection in balb/c mice challenged with leishmania (infantum) chagasi.the caf01 adjuvant has previously been shown to be safe for human use and to be a potent adjuvant for several vaccine antigens. in the present work, we sought to optimize the leishmania amazonensis antigens (laag) intranasal vaccine in an attempt to enhance the protective immune responses against leishmania (infantum) chagasi by using the caf01 association. laag/caf01 vaccinated mice that were challenged 15 days after booster dose with l. (infantum) chagasi showed a significant reduction in thei ...201526394776
novel 3,4-methylenedioxyde-6-x-benzaldehyde-thiosemicarbazones: synthesis and antileishmanial effects against leishmania amazonensis.a series of eleven 3,4-methylenedioxyde-6-x-benzaldehyde-thiosemicarbazones (16-27) was synthesised as part of a study to search for potential new drugs with a leishmanicidal effect. the thiosemicarbazones, ten of which are new compounds, were prepared in good yields (85-98%) by the reaction of 3,4-methylenedioxyde-6-benzaldehydes (6-x-piperonal), previously synthesised for this work by several methodologies, and thiosemicarbazide in ethanol with a few drops of h2so4. these compounds were evalua ...201526375353
further evidence of an association between the presence of leishmania rna virus 1 and the mucosal manifestations in tegumentary leishmaniasis patients.tegumentary leishmaniasis (tl) is endemic in latin america, and brazil contributes approximately 20 thousand cases per year. the pathogenesis of tl, however, is still not fully understood. clinical manifestations vary from cutaneous leishmaniasis (cl) to more severe outcomes, such as disseminated leishmaniasis (dl), mucosal leishmaniasis (ml) and diffuse cutaneous leishmaniasis (dcl). many factors have been associated with the severity of the disease and the development of lesions. recent studie ...201526372217
nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (cl). in this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for cl treatment using a 2(2) full factorial design. the formulations were prepared b ...201526366075
evaluation of antileishmanial activity of albaha medicinal plants against leishmania amazonensis.sixteen methanolic extracts obtained from thirteen plant species, selected either from ethnobotanical or chemotaxonomical data, were screened for their antileishmanial activity against leishmania amazonensis. the cytotoxic activity against normal peritoneal macrophages from normal balb/c mice was also determined. eight extracts had ic50 values ranging from <12.5 to 37.8 µg/ml against promastigotes. achillea biebersteinii flower, euphorbia helioscopia, and solanum incanum leaf extracts showed ant ...201526357662
evaluation of the leishmanicidal and cytotoxic effects of inhibitors for microorganism metabolic pathway enzymes.chemotherapy for leishmaniosis a neglected parasitic disease, is based on few drugs, which are toxic and present resistance issues. efforts for the development of new therapies are essential for the control of leishmaniasis. metabolic pathway enzymes are promising targets for new drugs against parasites. the search for effective drugs against key enzymes can take advantage of the similarities between metabolic pathways in different microorganisms trypanosomatids trypanosoma cruzi and leishmania ...201526349969
antileishmanial activity of compounds produced by endophytic fungi derived from medicinal plant vernonia polyanthes and their potential as source of bioactive substances.the purpose of this work was to evaluate the antileishmanial activity of endophytic fungi isolated from leaves of vernonia polyanthes plant and their prospective use in the discovery of bioactive compounds. sixteen endophytes were isolated by using potato dextrose agar medium and submitted to cultivation in rice medium. the fungal cultures were extracted with ethanol and used as crude extracts for testing their antileishmanial activity. the most active ethanol extract was obtained from p2-f3 str ...201526318306
leishmanicidal effect of synthetic trans-resveratrol analogs.stilbene-based compounds show antitumoral, antioxidant, antihistaminic, anti-inflammatory and antimicrobial activities. here, we evaluated the effect of the trans-resveratrol analogs, pterostilbene, piceatannol, polydatin and oxyresveratrol, against leishmania amazonensis.201526517558
2-amino-thiophene derivatives present antileishmanial activity mediated by apoptosis and immunomodulation in vitro.this study evaluated the effects of 2-amino-thiophene derivatives on the promastigote and amastigote forms of leishmania (leishmania) amazonensis and their possible mechanisms of action. initially, we evaluated the antileishmanial activity of ten 2-amino-thiophene derivatives on promastigote and axenic amastigote forms of leishmania amazonensis and their cytotoxicity against murine macrophages and human red blood cells. three promising compounds were selected for studies of the cell death proces ...201526513640
distinct macrophage fates after in vitro infection with different species of leishmania: induction of apoptosis by leishmania (leishmania) amazonensis, but not by leishmania (viannia) guyanensis.leishmania is an intracellular parasite in vertebrate hosts, including man. during infection, amastigotes replicate inside macrophages and are transmitted to healthy cells, leading to amplification of the infection. although transfer of amastigotes from infected to healthy cells is a crucial step that may shape the outcome of the infection, it is not fully understood. here we compare l. amazonensis and l. guyanensis infection in c57bl/6 and balb/c mice and investigate the fate of macrophages whe ...201526513474
benzophenone derivatives as cysteine protease inhibitors and biological activity against leishmania(l.) amazonensis amastigotes.the leishmanicidal potential of benzophenones has been described, some of them highlighting their potential as cysteine protease inhibitors. therefore, this work described leishmanicidal activity of nine benzophenone derivatives (1a-c;2a-c;3a-c) against intramacrophage amastigote forms of leishmania(l.)amazonensis (ic50) and the cytotoxic effect on murine peritoneal macrophages (cc50). the derivative 1c exhibited a selectivity index si (cc50/ic50) of 6.7, besides cytotoxicity lower than amphoter ...201526463637
hiv-1 tat protein enhances the intracellular growth of leishmania amazonensis via the ds-rna induced protein pkr.hiv-1 co-infection with human parasitic diseases is a growing public health problem worldwide. leishmania parasites infect and replicate inside macrophages, thereby subverting host signaling pathways, including the response mediated by pkr. the hiv-1 tat protein interacts with pkr and plays a pivotal role in hiv-1 replication. this study shows that tat increases both the expression and activation of pkr in leishmania-infected macrophages. importantly, the positive effect of tat addition on paras ...201526608746
novel selective inhibitor of leishmania (leishmania) amazonensis arginase.arginase is a glycosomal enzyme in leishmania that is involved in polyamine and trypanothione biosynthesis. the central role of arginase in leishmania (leishmania) amazonensis was demonstrated by the generation of two mutants: one with an arginase lacking the glycosomal addressing signal and one in which the arginase-coding gene was knocked out. both of these mutants exhibited decreased infectivity. thus, arginase seems to be a potential drug target for leishmania treatment. in an attempt to sea ...201525845502
the efficacy of 2-nitrovinylfuran derivatives against leishmania in vitro and in vivo.despite recent advances in the treatment of some forms of leishmaniasis, the available drugs are still far from ideal due to inefficacy, parasite resistance, toxicity and cost. the wide-spectrum antimicrobial activity of 2-nitrovinylfuran compounds has been described, as has their activity against trichomonas vaginalis and other protozoa. thus, the aim of this study was to test the antileishmanial activities of six 2-nitrovinylfurans in vitro and in a murine model of leishmaniasis. minimum paras ...201525807467
effect of apigenin on leishmania amazonensis is associated with reactive oxygen species production followed by mitochondrial dysfunction.leishmaniasis is an important neglected disease caused by protozoa of the genus leishmania that affects more than 12 million people worldwide. leishmaniasis treatment requires the administration of toxic and poorly tolerated drugs, and parasite resistance greatly reduces the efficacy of conventional medications. apigenin (1), a naturally occurring plant flavone, has a wide range of reported biological effects. in this study, antileishmanial activity of 1 in vitro was investigated, and its mechan ...201525768915
interactions between neutrophils and leishmania braziliensis amastigotes facilitate cell activation and parasite clearance.leishmania braziliensis and leishmania amazonensis are both causative agents of cutaneous leishmaniasis in south america. however, patient prognosis and the host immune response differ considerably depending on the infecting parasite species. the mechanisms underlying these differences appear to be multifactorial, with both host and parasite components contributing to disease outcome. as neutrophils are a prominent component of the inflammatory infiltrate in chronic cutaneous, diffuse cutaneous ...201525766649
therapeutic switching: from antidermatophytic essential oils to new leishmanicidal products.this study examined whether the antidermatophytic activity of essential oils (eos) can be used as an indicator for the discovery of active natural products against leishmania amazonensis. the aerial parts of seven plants were hydrodistilled. using broth microdilution techniques, the obtained eos were tested against three strains of dermatophytes (trichophyton mentagrophytes, microsporum gypseum and microsporum canis). to compare the eos antifungal and antiparasitic effects, the eos activities ag ...201525742270
antileishmanial activity of standardized fractions of stryphnodendron obovatum (barbatimão) extract and constituent compounds.stryphnodendron obovatum benth. is a brazilian tree used to treat skin ulceration, promote wound healing, and inhibit the growth of protozoa, including trypanosoma and leishmania species. bioguided fractionation of the ethanol extract of s. obovatum stem bark was performed, and antileishmanial and antioxidant activities of the standardized fractions were analyzed.201525732835
therapeutic switching: from antidermatophytic essential oils to new leishmanicidal products.this study examined whether the antidermatophytic activity of essential oils (eos) can be used as an indicator for the discovery of active natural products against leishmania amazonensis. the aerial parts of seven plants were hydrodistilled. using broth microdilution techniques, the obtained eos were tested against three strains of dermatophytes (trichophyton mentagrophytes, microsporum gypseum and microsporum canis). to compare the eos antifungal and antiparasitic effects, the eos activities ag ...201525714080
combinations of ascaridole, carvacrol, and caryophyllene oxide against leishmania.to date there are no vaccines against leishmania and chemotherapy remains the mainstay for the control of leishmaniasis. the drugs currently used for leishmaniasis therapy are significantly toxic, expensive, and result in a growing frequency of refractory infections. in this study, we evaluated the effect of combinations of the main components of essential oil from chenopodium ambrosioides (ascaridole, carvacrol, and caryophyllene oxide) against leishmaniaamazonensis. anti-leishmanial effects of ...201525697866
in vitro metacyclogenesis of leishmania (viannia) braziliensis and leishmania (leishmania) amazonensis clinical field isolates, as evaluated by morphology, complement resistance, and infectivity to human macrophages.this study was designed to assess in vitro metacyclogenesis of leishmania (viannia) braziliensis and leishmania (leishmania) amazonensis clinical field isolates obtained from patient lesions (l. braziliensis img3 and pps6m; l. amazonensis mab6). metacyclogenesis was evaluated by different criteria, namely, promastigote size (morphometric analysis and flow cytometry), surface modifications (loss of lectin or monoclonal antibody (mab) binding, complement resistance), and infectivity to human macro ...201525695070
regulation of leishmania (l.) amazonensis protein expression by host t cell dependent responses: differential expression of oligopeptidase b, tryparedoxin peroxidase and hsp70 isoforms in amastigotes isolated from balb/c and balb/c nude mice.leishmaniasis is an important disease that affects 12 million people in 88 countries, with 2 million new cases every year. leishmania amazonensis is an important agent in brazil, leading to clinical forms varying from localized (lcl) to diffuse cutaneous leishmaniasis (dcl). one interesting issue rarely analyzed is how host immune response affects leishmania phenotype and virulence. aiming to study the effect of host immune system on leishmania proteins we compared proteomes of amastigotes isola ...201525692783
4-aminoquinoline derivatives as potential antileishmanial agents.the leishmanicidal activity of a series of 4-aminoquinoline (amq) derivatives was assayed against leishmania amazonensis. this activity against the intracellular parasite was found stronger than for l. amazonensis promastigotes. neither compound was cytotoxic against macrophages. the compound amq-j, which exhibited a strong activity against promastigotes and amastigotes of l. amazonensis (ic50 values of 5.9 and 2.4 μg/ml, respectively) and similar leishmanicidal activity to reference drugs, was ...201525682728
antivascular and anti-parasite activities of natural and hemisynthetic flavonoids from new caledonian gardenia species (rubiaceae).a series of 16 flavonoids were isolated and prepared from bud exudate of gardenia urvillei and gardenia oudiepe, endemic to new caledonia. most of them are rare polymethoxylated flavones. some of these compounds showed noticeable activity against leishmania (leishmania) amazonensis, plasmodium falciparum and trypanosoma brucei gambiense, in addition to tubulin polymerization inhibition at low micromolar concentration. we also provide a full set of nmr data as some of the flavones were incomplete ...201525659770
leishmanicidal activity of lipophilic extracts of some hypericum species.leishmaniasis has emerged as the third most prevalent parasite-borne disease worldwide after malaria and filariasis, with about 350 million people at risk of infection. antileishmanial drugs currently available have various limitations, mainly because of the parasite resistance and side effects. the search of new antileishmanial drugs is ventured throughout the world.201525636874
biodegradable microparticles containing crotamine isolated from crotalus durissus terrificus display antileishmanial activity in vitro.to evaluate antileishmanial activity of crotamine, a toxin isolated from crotalus durissus terrificus, in solution form and encapsulated in biodegradable microparticles in vitro.201525633844
the effect of the phytol-rich fraction from lacistema pubescens against leishmania amazonensis is mediated by mitochondrial dysfunction.leishmaniasis is a complex disease caused by protozoan parasite leishmania and the treatment remains a serious problem since the available drugs exhibited high toxicity and side effects. plant-derived natural products are promising leads for the development of novel chemotherapeutics. in this work the phytol-rich hexane fraction (prf) from the leaves of lacistema pubescens was obtained and identified by gc-ms analysis. when assayed for antileishmanial effects, prf was active against promastigote ...201526424529
molecular characterization of american cutaneous leishmaniasis in the tri‑border area of assis brasil, acre state, brazil.in this study, leishmania species were identified by polymerase chain reaction (pcr). the epidemiology of patients suspected of having american cutaneous leishmaniasis in the municipality of assis brasil, acre state, located in the brazil/peru/bolivia tri-border was also investigated. by pcr, the dna of leishmania was detected in 100% of the cases (37 samples) and a pcr-restriction fragment length polymorphism (rflp) of the hsp 70 gene identified the species in 32 samples: leishmania (viannia) b ...201526422160
antileishmanial activity and trypanothione reductase effects of terpenes from the amazonian species croton cajucara benth (euphorbiaceae).leishmaniasis comprises several infectious diseases caused by protozoa parasites of leishmania genus. in recent years, there has been a growing interest in the therapeutic use of natural products to treat parasitic diseases. among them croton cajucara benth. (euphorbiaceae) is a plant found in the amazonian region with a history of safe use in folk medicine.201526547537
kinetoplastid membrane protein-11 as a vaccine candidate and a virulence factor in leishmania.kinetoplastid membrane protein-11 (kmp-11), a protein present in all kinetoplastid protozoa, is considered a potential candidate for a leishmaniasis vaccine. in leishmania amazonensis, kmp-11 is expressed in promastigotes and amastigotes. in both stages, the protein was found in association with membrane structures at the cell surface, flagellar pocket, and intracellular vesicles. more importantly, its surface expression is higher in amastigotes than in promastigotes and increases during metacyc ...201526528287
epoxy-α-lapachone has in vitro and in vivo anti-leishmania (leishmania) amazonensis effects and inhibits serine proteinase activity in this parasite.leishmania (leishmania) amazonensis is a protozoan that causes infections with a broad spectrum of clinical manifestations. the currently available chemotherapeutic treatments present many problems, such as several adverse side effects and the development of resistant strains. natural compounds have been investigated as potential antileishmanial agents, and the effects of epoxy-α-lapachone on l. (l.) amazonensis were analyzed in the present study. this compound was able to cause measurable effec ...201525583728
intranasal vaccination with leishmanial antigens protects golden hamsters (mesocricetus auratus) against leishmania (viannia) braziliensis infection.previous results have shown that oral and intranasal administration of particulate leishmania (leishmania) amazonensis antigens (laag) partially protects mice against l. amazonensis infection. however, vaccination studies on species of the subgenus viannia, the main causative agent of cutaneous and mucosal leishmaniasis in the americas, have been hampered by the lack of easy-to-handle bio-models that accurately mimic the human disease. recently, we demonstrated that the golden hamster is an appr ...201525569338
e-ntpdase (ecto-nucleoside triphosphate diphosphohydrolase) of leishmania amazonensis inhibits macrophage activation.leishmania amazonensis, the causal agent of diffuse cutaneous leishmaniasis, is known for its ability to modulate the host immune response. because a relationship between ectonucleotidase activity and the ability of leishmania to generate injury in c57bl/6 mice has been demonstrated, in this study we evaluated the involvement of ecto-nucleoside triphosphate diphosphohydrolase (e-ntpdase) activity of l. amazonensis in the process of infection of j774-macrophages. our results show that high-activi ...201525554487
pvd1 defensin, a plant antimicrobial peptide with inhibitory activity against leishmania amazonensis.plant defensins are small cysteine-rich peptides and exhibit antimicrobial activity against a variety of both plant and human pathogens. despite the broad inhibitory activity that plant defensins exhibit against different micro-organisms, little is known about their activity against protozoa. in a previous study, we isolated a plant defensin named pvd1 from phaseolus vulgaris (cv. pérola) seeds, which was seen to be deleterious against different yeast cells and filamentous fungi. it exerted its ...201526285803
characterization of the b cell response to leishmania infection after anti-cd20 b cell depletion.anti-cd20 depletion therapies targeting b cells are commonly used in malignant b cell disease and autoimmune diseases. there are concerns about the ability of b cells to respond to infectious diseases acquired either before or after b cell depletion. there is evidence that the b cell response to existing or acquired viral infections is compromised during treatment, as well as the antibody response to vaccination. our laboratory has an experimental system using co-infection of c3h mice with both ...201526261496
potent in vitro antiproliferative synergism of combinations of ergosterol biosynthesis inhibitors against leishmania amazonensis.leishmaniases comprise a spectrum of diseases caused by protozoan parasites of the leishmania genus. treatments available have limited safety and efficacy, high costs, and difficult administration. thus, there is an urgent need for safer and more-effective therapies. most trypanosomatids have an essential requirement for ergosterol and other 24-alkyl sterols, which are absent in mammalian cells. in previous studies, we showed that leishmania amazonensis is highly susceptible to aryl-quinuclidine ...201526239973
hairless mice as an experimental model of infection with leishmania (leishmania) amazonensis.hrs/j hairless mice have been investigated as an experimental model in cutaneous leishmaniasis induced by leishmania (leishmania) amazonensis. the animals were inoculated with 10(6) promastigotes into the right hind footpad and the course of infection was followed up for 30, 60 and 90 days. balb/c mice were infected and used as control. hairless mice were susceptible to l. (l.) amazonensis infection and a progressive increase in number of parasites and footpad thickness was detected over time. s ...201526234915
the pentavalent antimonial therapy against experimental leishmania amazonensis infection is more effective under the inhibition of the nf-κb pathway.during leishmania infection, host immune response is important to prevent the growth/survival of intracellular amastigotes. in this study, we evaluated in vitro and in vivo whether or not during leishmania amazonensis infection, pentavalent antimonial treatment/therapy could be more effective under tnf-α inhibition. both l. amazonensis-infected macrophages (in vitro model) and mice (in vivo model) were treated with a nuclear factor-κb (nf-κb) inhibitor and with glucantime®, alone and in combined ...201526218282
first detection of leishmania spp. dna in brazilian bats captured strictly in urban areas.leishmania spp. is a protozoan that maintains its life cycle in domestic and wild animals and it may include bats, a population that has increased in urban environments. this study aimed to investigate the presence of leishmania spp. in bats captured strictly in urban areas that are endemic for visceral leishmaniasis. the spleen and skin samples of 488 bats from 21 endemic cities in northwestern são paulo state, brazil, were tested for the presence of leishmania kdna using real-time pcr. differe ...201526209107
in vitro biological action of aqueous extract from roots of physalis angulata against leishmania (leishmania) amazonensis.leishmaniasis is an infectious disease caused by various species of the protozoan parasites of the leishmania genus and transmitted by phlebotomine sandflies. the protozoa multiply in phagocytic cells, mainly macrophages, which play an important role defending the organism from pathogens. the most effective treatment for leishmaniasis is the chemotherapy and besides the high cost, these drugs are toxic and require a long period of treatment. currently, some herbal products are considered an impo ...201526205771
capillary electrophoresis reveals polyamine metabolism modulation in leishmania (leishmania) amazonensis wild type and arginase knockout mutants under arginine starvation.l-arginine is an essential amino acid in leishmania (leishmania) amazonensis metabolism. a key enzyme for parasite l-arginine metabolism is arginase (arg) that uses arginine to produce urea and ornithine, a precursor of polyamine pathway guaranteeing parasite replication in both insect and mammal hosts. there is an alternative pathway to produce ornithine via l-proline and glutamate, but this mechanism is not described in leishmania. in the mammal host, two enzymes can use l-arginine as substrat ...201526202519
oral effectiveness of pmic4, a novel hydroxyethylpiperazine analogue, in leishmania amazonensis.pentavalent antimonials have saved the lives of thousands of leishmania-infected patients more than seventy years but, unfortunately, they are highly toxic and require parenteral delivery. therefore, the search for safer and orally delivered alternative is a need. this paper describes the antileishmanial properties of pmic4, a novel hydroxyethylpiperazine analogue. pmic4 showed potent activity against intracellular amastigotes of leishmania amazonensis, with ic50 of 1.8 μm and selectivity index ...201425516829
in vitro activity of the hydroethanolic extract and biflavonoids isolated from selaginella sellowii on leishmania (leishmania) amazonensis.this study is the first phytochemical investigation of selaginella sellowii and demonstrates the antileishmanial activity of the hydroethanolic extract from this plant (sshe), as well as of the biflavonoids amentoflavone and robustaflavone, isolated from this species. the effects of these substances were evaluated on intracellular amastigotes of leishmania (leishmania) amazonensis, an aetiological agent of american cutaneous leishmaniasis. sshe was highly active against intracellular amastigotes ...201425591109
molecular detection of leishmania in sand flies (diptera: psychodidae: phlebotominae) collected in the caititu indigenous reserve of the municipality of lábrea, state of amazonas, brazil.phlebotominae sand flies are of medical importance because they are vectors of human pathogens, such as protozoa of the genus leishmania ross, etiological agent of american cutaneous leishmaniasis (acl). in lábrea, a municipality in the state of amazonas, brazil, acl is primarily associated with subsistence activities, such as collection and extraction of forest products, undertaken by both indigenous and nonindigenous people. data on acl in indigenous populations are scarce, such that there is ...201426309318
functional properties and stability of spray-dried pigments from bordo grape (vitis labrusca) winemaking pomace.the stability of anthocyanin and phenolic compounds, the antioxidant capacity, the antimicrobial activity and the capacity to inhibit arginase from leishmania were evaluated in spray-dried powders from bordo grape winemaking pomace extract. the pigments were produced using maltodextrin as the carrier agent at concentrations varying from 10% to 30% and air entrance temperatures varying from 130 to 170°c. a sample of freeze-dried extract without the carrier was also evaluated. the anthocyanins in ...201424996348
nlr proteins and parasitic disease.parasitic diseases are a serious global health concern. many of the most common and most severe parasitic diseases, including chagas' disease, leishmaniasis, and schistosomiasis, are also classified as neglected tropical diseases and are comparatively less studied than infectious diseases prevalent in high income nations. the nlrs (nucleotide-binding domain leucine-rich-repeat-containing proteins) are cytosolic proteins known to be involved in pathogen detection and host response. the role of nl ...201424989828
leishmania donovani nucleoside hydrolase terminal domains in cross-protective immunotherapy against leishmania amazonensis murine infection.nucleoside hydrolases of the leishmania genus are vital enzymes for the replication of the dna and conserved phylogenetic markers of the parasites. leishmania donovani nucleoside hydrolase (nh36) induced a main cd4(+) t cell driven protective response against l. chagasi infection in mice which is directed against its c-terminal domain. in this study, we used the three recombinant domains of nh36: n-terminal domain (f1, amino acids 1-103), central domain (f2 aminoacids 104-198), and c-terminal do ...201424966857
synthesis and antiparasitic activity of new bis-arylimidamides: db766 analogs modified in the terminal groups.fifteen novel bis-arylimidamide derivatives with various 6-membered (7a-c) and 5-membered (7d-o) heterocyclic rings replacing the terminal pyridyl rings of the lead compound db766{(2,5-bis[2-i-propoxy-4-(2-pyridylimino)aminophenylfuran]}, were prepared and evaluated versus trypanosoma cruzi, leishmania amazonensis, trypanosoma brucei rhodesiense and plasmodium falciparum. compound 7a with pyrimidine replacing the pyridine rings showed good activity versus t. cruzi, t. brucei rhodesiense and p. f ...201424956553
cell death in amastigote forms of leishmania amazonensis induced by parthenolide.leishmania amazonensis infection results in diverse clinical manifestations: cutaneous, mucocutaneous or visceral leishmaniasis. the arsenal of drugs available for treating leishmania infections is limited. therefore, new, effective, and less toxic leishmaniasis treatments are still needed. we verified cell death in amastigote forms of leishmania amazonensis induced by the sesquiterpene lactone parthenolide.201424913205
leishmanicidal activities of novel synthetic furoxan and benzofuroxan derivatives.a novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5]oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of leishmania amazonensis. the furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). the benzofuroxan derivative 8a was able to ...201424913171
in vitro and in vivo activity of major constituents from pluchea carolinensis against leishmania amazonensis.the search for new therapeutic agents from natural sources has been a constant for the treatment of diseases such as leishmaniasis. herein, in vitro and in vivo pharmacological activities of pure major phenolic constituents (caffeic acid, chlorogenic acid, ferulic acid, quercetin, and rosmarinic acid) from pluchea carolinensis against leishmania amazonensis are presented. pure compounds showed inhibitory activity against promastigotes (ic50 = 0.2-0.9 μg/ml) and intracellular amastigotes (ic50 =  ...201424906989
resveratrol is active against leishmania amazonensis: in vitro effect of its association with amphotericin b.resveratrol is a polyphenol found in black grapes and red wine and has many biological activities. in this study, we evaluated the effect of resveratrol alone and in association with amphotericin b (amb) against leishmania amazonensis. our results demonstrate that resveratrol possesses both antipromastigote and antiamastigote effects, with 50% inhibitory concentrations (ic50s) of 27 and 42 μm, respectively. the association of resveratrol with amb showed synergy for l. amazonensis amastigotes, as ...201425114129
short-term protection conferred by leishvacin® against experimental leishmania amazonensis infection in c57bl/6 mice.to date, there is no vaccine available against human leishmaniasis. although some vaccination protocols can induce immunity in murine models, they fail to induce protection in humans. the reasons for that remain unclear. the aim of the present study was to characterize the changes in the pattern of the immune response during subcutaneous vaccination with leishvacin® in mice. we also investigated whether ifn-γ and nitric oxide synthase are indispensable for the protection elicited by the vaccine. ...201425102355
terpenes increase the lipid dynamics in the leishmania plasma membrane at concentrations similar to their ic50 values.although many terpenes have shown antitumor, antibacterial, antifungal, and antiparasitic activity, the mechanism of action is not well established. electron paramagnetic resonance (epr) spectroscopy of the spin-labeled 5-doxyl stearic acid revealed remarkable fluidity increases in the plasma membrane of terpene-treated leishmania amazonensis promastigotes. for an antiproliferative activity assay using 5×10(6) parasites/ml, the sesquiterpene nerolidol and the monoterpenes (+)-limonene, α-terpine ...201425101672
the new pyrazolyltetrazole derivative msn20 is effective via oral delivery against cutaneous leishmaniasis.an orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-(4'-methoxyphenyl)1h-pyrazole-4-yl]1h-tetrazole (msn20). msn20 showed a 50% inhibitory concentration (ic50) of 22.3 μm against amastigotes of leishmania amazonensis and reduced significantly the paras ...201425092697
liposomal formulation of turmerone-rich hexane fractions from curcuma longa enhances their antileishmanial activity.promastigote forms of leishmania amazonensis were treated with different concentrations of two fractions of curcuma longa cortex rich in turmerones and their respective liposomal formulations in order to evaluate growth inhibition and the minimal inhibitory concentration (mic). in addition, cellular alterations of treated promastigotes were investigated under transmission and scanning electron microscopies. liporhic and liporhiwc presented lower mic, 5.5 and 12.5 μg/ml, when compared to nonencap ...201425045693
leishmania amazonensis amastigotes highly express a tryparedoxin peroxidase isoform that increases parasite resistance to macrophage antimicrobial defenses and fosters parasite virulence.professional phagocytes generate a myriad of antimicrobial molecules to kill invading microorganisms, of which nitrogen oxides are integral in controlling the obligate intracellular pathogen leishmania. although reactive nitrogen species produced by the inducible nitric oxide synthase (inos) can promote the clearance of intracellular parasites, some leishmania species/stages are relatively resistant to inos-mediated antimicrobial activity. the underlying mechanism for this resistance remains lar ...201425033301
in vitro and in vivo miltefosine susceptibility of a leishmania amazonensis isolate from a patient with diffuse cutaneous leishmaniasis.miltefosine was the first oral compound approved for visceral leishmaniasis chemotherapy, and its efficacy against leishmania donovani has been well documented. leishmania amazonensis is the second most prevalent species causing cutaneous leishmaniasis and the main etiological agent of diffuse cutaneous leishmaniasis in brazil. driven by the necessity of finding alternative therapeutic strategies for a chronic diffuse cutaneous leishmaniasis patient, we evaluated the susceptibility to miltefosin ...201425033218
in vitro and in vivo activity of benzo[c]phenanthridines against leishmania amazonensis.seven benzo[c]phenanthridines, synthetic or isolated from zanthoxylum rhoifolium root bark, were evaluated against leishmania amazonensis axenic amastigotes. five of them were considered leishmanicidal, with ic50 values ranging from 0.03 to 0.54 µm, and were evaluated on intramacrophagic amastigotes of l. amazonensis. chelerythrine displayed the best activity (ic50=0.5 µm), which was in the same range as the reference compound amphotericin b (ic50=0.4 µm). in vivo studies with chelerythrine, avi ...201425029171
in vivo antileishmanial efficacy of miltefosine against leishmania (leishmania) amazonensis.leishmaniasis, a disease caused by parasites of the leishmania genus, constitutes a significant health and social problem in many countries and is increasing worldwide. the conventional treatment, meglumine antimoniate (ma), presents numerous disadvantages, including invasiveness, toxicity, and frequent therapeutic failure, justifying the attempts at finding alternatives to the first-line therapy. we have studied the comparative long-term efficacy of ma against miltefosine (mf) in leishmania inf ...201425014108
cell death and ultrastructural alterations in leishmania amazonensis caused by new compound 4-nitrobenzaldehyde thiosemicarbazone derived from s-limonene.the treatment of leishmaniasis with pentavalent antimonials is problematic because of their toxicity. investigations of potentially active molecules are important to discover less toxic drugs that are viable economic alternatives for the treatment of leishmaniasis. thiosemicarbazones are a group of molecules that are known for their wide versatility and biological activity. in the present study, we examined the antileishmania activity, mechanism of action, and biochemical alterations produced by ...201425253283
leishmanicidal compounds and potent pparγ activators from renealmia thyrsoidea (ruiz & pav.) poepp. & endl.leaves and rhizomes of renealmia thyrsoidea (ruiz & pav.) poepp. & endl. traditionally used in the yanesha pharmacopoeia to treat skin infections such as leishmaniasis ulcers, or to reduce fever were chemically investigated to identify leishmanicidal compounds, as well as pparγ activators.201425251262
synthesis, leishmanicidal activity and theoretical evaluations of a series of substituted bis-2-hydroxy-1,4-naphthoquinones.a series of eight substituted bis-2-hydroxy-1,4-naphthoquinone derivatives was synthesized through lawsone condensation with various aromatic and aliphatic aldehydes under mild acidic conditions. the title compounds were evaluated for antileishmanial activity in vitro against leishmania amazonensis and leishmania braziliensis promastigotes; six compounds showed good activity without significant toxic effects. the compound with the highest activity was used for an in vivo assay with leishmania am ...201425247686
intranasal vaccination with extracellular serine proteases of leishmania amazonensis confers protective immunity to balb/c mice against infection.previously, we demonstrated that unlike subcutaneous or intramuscular vaccination, intranasal vaccination of balb/c mice with whole leishmania amazonensis antigens leads to protection against cutaneous leishmaniasis. here, the role of parasite serine proteases in the protective immunity was investigated.201425239157
extracellular vesicles from leishmania-infected macrophages confer an anti-infection cytokine-production profile to naïve macrophages.extracellular vesicles (evs) are structures with phospholipid bilayer membranes and 100-1000 nm diameters. these vesicles are released from cells upon activation of surface receptors and/or apoptosis. the production of evs by dendritic cells, mast cells, macrophages, and b and t lymphocytes has been extensively reported in the literature. evs may express mhc class ii and other membrane surface molecules and carry antigens. the aim of this study was to investigate the role of evs from leishmania- ...201425232947
effectiveness of miltefosine-pentoxifylline compared to miltefosine in the treatment of cutaneous leishmaniasis in c57bl/6 mice.the treatment of leishmaniasis ischallenging, given the difficulties in drug administration and resistance. therefore, we chose to test the efficacy of miltefosine combined with pentoxifylline.201425229296
n-butyl-[1-(4-methoxy)phenyl-9h-β-carboline]-3-carboxamide prevents cytokinesis in leishmania amazonensis.leishmaniasis, a complex of diseases caused by protozoa of the genus leishmania, is endemic in 98 countries, affecting approximately 12 million people worldwide. current treatments for leishmaniasis have many disadvantages, such as toxicity, high costs, and prolonged treatment, making the development of new treatment alternatives highly relevant. several studies have verified the antileishmanial activity of β-carboline compounds. in the present study, we investigated the in vitro antileishmanial ...201425224005
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