Publications
| Title | Abstract | Year(sorted ascending) Filter | PMID Filter |
|---|
| 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 ... | 2015 | 25659770 |
| 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. | 2015 | 25636874 |
| 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. | 2015 | 25633844 |
| 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 ... | 2015 | 26169126 |
| 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 ... | 2015 | 26150922 |
| 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 ... | 2015 | 26125921 |
| 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 ... | 2015 | 26116864 |
| 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 ... | 2015 | 26107111 |
| 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 ... | 2015 | 26099574 |
| 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 ... | 2015 | 26095535 |
| 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 ... | 2015 | 26094119 |
| 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 ... | 2015 | 26074677 |
| 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 ... | 2015 | 26070143 |
| 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 ... | 2015 | 26055530 |
| 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 ... | 2015 | 26052723 |
| 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 ... | 2015 | 26040192 |
| 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. ... | 2015 | 26009021 |
| 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 ... | 2015 | 26001191 |
| 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 ... | 2015 | 25973801 |
| 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 ... | 2015 | 25946239 |
| 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 ... | 2015 | 25929728 |
| 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 ... | 2015 | 25917716 |
| 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 ... | 2015 | 25896942 |
| toxicogenomic analysis of pharmacological active coumarins isolated from calophyllum brasiliense. | calophyllum brasiliense (calophyllaceae) is a tropical rain forest tree, mainly distributed in south and central america. it is an important source of bioactive natural products like, for instance soulatrolide, and mammea type coumarins. soulatrolide is a tetracyclic dipyranocoumarins and a potent inhibitor of hiv-1 reverse transcriptase and mycobacterium tuberculosis. mammea a/ba and a/bb coumarins, pure or as a mixture, are highly active against several leukemia cell lines, trypanosoma cruzi a ... | 2015 | 26697389 |
| the effect of ursolic acid on leishmania (leishmania) amazonensis is related to programed cell death and presents therapeutic potential in experimental cutaneous leishmaniasis. | among neglected tropical diseases, leishmaniasis is one of the most important ones, affecting more than 12 million people worldwide. the available treatments are not well tolerated, and present diverse side effects, justifying the search for new therapeutic compounds. in the present study, the activity of ursolic acid (ua) and oleanolic acid (oa) were assayed in experimental cutaneous leishmaniasis (in vitro and in vivo). promastigote forms of l. amazonensis were incubated with oa and ua for 24h ... | 2015 | 26674781 |
| 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 ... | 2015 | 26673780 |
| 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 ... | 2015 | 26608746 |
| 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. | 2015 | 26547537 |
| 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 ... | 2015 | 26528287 |
| 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 ... | 2015 | 26401717 |
| 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 ... | 2015 | 26400473 |
| 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 ... | 2015 | 26396059 |
| 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 ... | 2015 | 26394776 |
| 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 ... | 2015 | 26375353 |
| 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 ... | 2015 | 26372217 |
| 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 ... | 2015 | 26366075 |
| 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 ... | 2015 | 26357662 |
| 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 ... | 2015 | 26349969 |
| 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 ... | 2015 | 26318306 |
| 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/ ... | 2015 | 25606862 |
| 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 ... | 2015 | 26606687 |
| 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 ... | 2015 | 26240156 |
| 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/ ... | 2015 | 25742265 |
| 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 ... | 2015 | 25014011 |
| 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 ... | 2015 | 25124926 |
| 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 ... | 2015 | 25288263 |
| 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 ... | 2015 | 25265060 |
| 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 ... | 2015 | 25448354 |
| 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 ... | 2015 | 25466588 |
| 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 ... | 2015 | 25461316 |
| 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 ... | 2015 | 25460590 |
| 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 ... | 2015 | 25499513 |
| 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 ... | 2015 | 26424529 |
| 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 ... | 2015 | 26422160 |
| 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 ... | 2015 | 25583728 |
| 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 ... | 2015 | 25569338 |
| 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 ... | 2015 | 25554487 |
| 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. | 2015 | 26517558 |
| 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 ... | 2015 | 26513640 |
| 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 ... | 2015 | 26513474 |
| 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 ... | 2015 | 26463637 |
| 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) ... | 2015 | 25971623 |
| 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 ... | 2015 | 26602870 |
| 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 ... | 2015 | 26619186 |
| 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. | 2015 | 26435708 |
| 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. | 2015 | 25849562 |
| 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 ... | 2015 | 26602873 |
| 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 ... | 2015 | 26415499 |
| 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 ... | 2016 | 27148270 |
| 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 ... | 2016 | 27508930 |
| 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 ... | 2016 | 26975994 |
| lysosomal trafficking regulator (lyst). | regulation of vesicle trafficking to lysosomes and lysosome-related organelles (lros) as well as regulation of the size of these organelles are critical to maintain their functions. disruption of the lysosomal trafficking regulator (lyst) results in chediak-higashi syndrome (chs), a rare autosomal recessive disorder characterized by oculocutaneous albinism, prolonged bleeding, severe immunodeficiency, recurrent bacterial infection, neurologic dysfunction and hemophagocytic lympohistiocytosis (hl ... | 2016 | 26427484 |
| indigenous microbiota and leishmaniasis. | animals are colonized by their indigenous microbiota from the early days of life. the estimated number of associated bacterial cells in humans is around of 10(14) per individual, most of them in the gut. several studies have investigated the microbiota-host relationship, and the use of germfree animals has been an important tool in these studies. these animals, when infected with a pathogen, have shown to be sometimes more resistant and other times more susceptible than conventional animals. lei ... | 2016 | 26407073 |
| [cutaneous leishmaniosis: unusual clinical manifestation]. | clinical manifestations of leishmaniasis are diverse and related to the infecting species, its relationship with the environment and the host immune response. a case of late andean cutaneous leishmaniasis with extensive manifestation is presented. the case was confirmed through microbiological and immunological studies; identification was performed by cytochrome b gene sequencing and the species was determined as leishmania (leishmania) amazonensis. the patient was treated with sodium stibogluco ... | 2016 | 25418662 |
| impact of tumor necrosis factor receptor p55 deficiency in susceptibility of c57bl/6 mice to infection with leishmania (leishmania) amazonensis. | tumor necrosis factor (tnf) is involved in host resistance to several intracellular pathogens. although the critical role of tnf receptor (tnfr)p55 in leishmania (leishmania) major infection has been demonstrated, the impact of tnfrp55 deficiency on l. (l.) amazonensis infection has not been explored. l. (l.) amazonensis-infected tnfrp55(-/-) mice failed to resolve lesions, whereas c57bl/6 wild-type mice completely healed. the susceptibility of the tnfrp55(-/-) mice was characterized by higher l ... | 2016 | 24856420 |
| immunization with antigenic extracts of leishmania associated with montanide isa 763 adjuvant induces partial protection in balb/c mice against leishmania (leishmania) amazonensis infection. | a proper adjuvant has a relevant role in vaccine formulations to generate an effective immune response. in this study, total leishmania antigen (tla) formulated with montanide isa 763 or r848 as adjuvants were evaluated as a first generation leishmania vaccine in a murine model. | 2016 | 24662018 |
| proteomic analysis reveals differentially expressed proteins in macrophages infected with leishmania amazonensis or leishmania major. | cba macrophages effectively control leishmania major infection, yet are permissive to leishmania amazonensis. employing a transcriptomic approach, we previously showed the up-regulation of the genes involved in the classical pathway of macrophage activation in resistant mice. however, microarray analyses do not evaluate changes in gene expression that occur after translation. to circumvent this analytical limitation, we employed a proteomics approach to increase our understanding of the modulati ... | 2016 | 23628411 |
| 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. | 2016 | 27041867 |
| evaluation of chemical composition and antileishmanial and antituberculosis activities of essential oils of piper species. | essential oils from fresh piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (gc-ms), and a total of 68 components were identified. principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. the composition of the essential oil of piper mosenii was described for the first time. the cytotoxicity of the essential oils was evaluated in peri ... | 2016 | 28009804 |
| evaluation of chemical composition and antileishmanial and antituberculosis activities of essential oils of piper species. | essential oils from fresh piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (gc-ms), and a total of 68 components were identified. principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. the composition of the essential oil of piper mosenii was described for the first time. the cytotoxicity of the essential oils was evaluated in peri ... | 2016 | 27973453 |
| the antileishmanial activity of xanthohumol is mediated by mitochondrial inhibition. | xanthohumol (xan) is a natural constituent of human nutrition. little is known about its actions on leishmanial parasites and their mitochondria as putative target. therefore, we determined the antileishmanial activity of xan and resveratrol (res, as alternative compound with antileishmanial activity) with respect to mitochondria in leishmania amazonensis promastigotes/amastigotes (lap/laa) in comparison with their activity in peritoneal macrophages from mouse (pmm) and macrophage cell line j774 ... | 2016 | 27938439 |
| leishmania amazonensis infection induces behavioral alterations and modulates cytokine and neurotrophin production in the murine cerebral cortex. | neurological symptoms have been associated with leishmania infection, however little is known about how the nervous system is affected in leishmaniasis. this work aimed to analyze parasitic load, production of cytokines/neurotrophins in the prefrontal cortex and behavioral changes in balb/c mice infected with leishmania amazonensis. at 2 and 4months post-infection, infected mice showed a decrease in ifn-γ, il-1, il-6, il-4, il-10 cytokines and bdnf and ngf neurotrophins in prefrontal cortex asso ... | 2016 | 27876366 |
| synthesis and biological evaluation against mycobacterium tuberculosis and leishmania amazonensis of a series of diaminated terpenoids. | we report the synthesis of a series of diaminated terpenoids containing, as side-chain of the diamine core, the "head-to-tail" prenyl derivatives, with amino amino spacers of variable length. in vitro biological activity of these compounds was evaluated against mycobacterium tuberculosis and leishmania amazonensis, and the structure-activity relationships are discussed. different biological results were observed depending on the terpenic side-chain length. the best results were obtained for tran ... | 2016 | 27876209 |
| the role of the p2x7 receptor in murine cutaneous leishmaniasis: aspects of inflammation and parasite control. | leishmania amazonensis is the etiological agent of diffuse cutaneous leishmaniasis. the immunopathology of leishmaniasis caused by l. amazonensis infection is dependent on the pathogenic role of effector cd4(+) t cells. purinergic signalling has been implicated in resistance to infection by different intracellular parasites. in this study, we evaluated the role of the p2x7 receptor in modulating the immune response and susceptibility to infection by l. amazonensis. we found that p2x7-deficient m ... | 2016 | 27866341 |
| detection of leishmania amazonensis and leishmania braziliensis in culicoides (diptera, ceratopogonidae) in an endemic area of cutaneous leishmaniasis in the brazilian amazonia. | biting midges in the genus culicoides act as vectors of arboviruses throughout the world and as vectors of filariasis in latin america, the caribbean, and parts of africa. although culicoides spp. are currently not considered to be vectors of leishmania protozoa, the high abundance of biting midges in areas with active cutaneous leishmaniasis transmission points to the possibility of culicoides infection by these pathogens. we used pcr to test captured culicoides species for natural infection wi ... | 2016 | 27860021 |
| synthesis and in vitro anti leishmania amazonensis biological screening of morita-baylis-hillman adducts prepared from eugenol, thymol and carvacrol. | leishmaniasis represents a series of severe neglected tropical diseases caused by protozoa of the genus leishmania and is widely distributed around the world. here, we present the syntheses of morita-baylis-hillman adducts (mbhas) prepared from eugenol, thymol and carvacrol, and their bioevaluation against promastigotes of leishmania amazonensis. the new mbhas are prepared in two steps from essential oils in moderate to good yields and present ic50 values in the range of 22.30-4.71 μm. moreover, ... | 2016 | 27834831 |
| essential oils: in vitro activity against leishmania amazonensis, cytotoxicity and chemical composition. | the current chemotherapy for cutaneous leishmaniosis (cl) has a series of drug limitations such as toxic side effects, long duration, high costs and drug resistance, which requires the development of new drugs or effective alternatives to the cl treatment. essential oils (eos) are complex mixtures of secondary metabolites from various plants. it has been shown that several eos, or their constituents, have inhibitory activity against protozoa. thus, this study aims to evaluate the biological acti ... | 2016 | 27825341 |
| evaluation of the antiplasmodial and leishmanicidal potential of myrciaria dubia (myrtaceae) extract. | malaria and leishmaniasis are prevalent in tropical regions, which have environmental characteristics that are highly favorable to protozoa and vectors of these diseases; the transmission of these infections in sub-tropical regions, although recognized, represents only a small fraction of cases. plants are constantly being used in the search for and acquisition of new drugs, and many compounds derived from them have been used to combat various diseases. in this study, we evaluated the action of ... | 2016 | 27812653 |
| screening of the in vitro antileishmanial activities of compounds and secondary metabolites isolated from maytenus guianensis klotzsch ex reissek (celastraceae) chichuá amazon. | maytenus guianensis is a member of the celastraceae family that is used in traditional medicine, particularly for its anti-parasitic and anti-cancer effects. to explore the ethnopharmacological potential of this plant, the present study was designed to screen the in vitro antileishmanial activities of extracts and compounds isolated from m. guianensis. | 2016 | 27812652 |
| in vitro assessment of plants growing in cuba belonging to solanaceae family against leishmania amazonensis. | in this study, an in vitro antileishmanial assessment of plant extracts from 12 genera and 46 species growing in cuba belonging to solanaceae family was performed. a total of 226 extracts were screened against promastigotes of leishmania amazonensis, and cytotoxicity of active extracts [median inhibitory concentration (ic50 ) promastigotes <100 µg/ml] was determined on peritoneal macrophage from balb/c mice. extracts that showed selective index >5 were then assayed against intracellular amastigo ... | 2016 | 27480800 |
| antileishmanial activity and inducible nitric oxide synthase activation by runo complex. | parasites of the genus leishmania are capable of inhibiting effector functions of macrophages. these parasites have developed the adaptive ability to escape host defenses; for example, they inactivate the nf-κb complex and suppress inos expression in infected macrophages, which are responsible for the production of the major antileishmanial substance nitric oxide (no), favoring then its replication and successful infection. metal complexes with no have been studied as potential compounds for the ... | 2016 | 27795620 |
| aminoquinoline compounds: effect of 7-chloro-4-quinolinylhydrazone derivatives against leishmania amazonensis. | in this study, we have investigated the antileishmanial activity of ten 7-chloro-4-quinolinylhydrazone derivatives. among the compounds tested, compounds 2a and 2j presented activity against promastigotes (ic50 values of 52.5 and 21.1 μm, respectively) and compounds 2a and 2c were active against intracellular amastigotes (ic50 of 8.1 and 15.6 μm, respectively) of leishmania amazonensis. the majority of compounds did not show toxicity against murine macrophages. compound 2a exhibited low cytotoxi ... | 2016 | 27743972 |
| optimization of extraction method and evaluation of antileishmanial activity of oil and nanoemulsions of pterodon pubescens benth. fruit extracts. | currently, leishmaniasis is difficult to manage owing to the limited choice and high toxicity of available drugs, and emergence of drug-resistant protozoa. medicinal plants, which produce various bioactive molecules, can help counter this global shortage. in this study, we prepared pterodon pubescens fruit extracts, which show antileishmanial activity, and developed a nanoemulsion of the optimized extract to improve its performance. the extracts were prepared using conventional methods and a sup ... | 2016 | 27725158 |
| natural canine infection by leishmania infantum and leishmania amazonensis and their implications for disease control. | leishmaniasis is a major public health problem worldwide. because leishmania can adapt to new hosts or vectors, knowledge concerning the current etiological agent in dogs is important in endemic areas. this study aimed to identify the leishmania species detected in 103 samples of peripheral blood from dogs that were naturally infected with these protozoa. the diagnosis of leishmaniasis was determined through parasitological examination, the indirect enzyme-linked immunosorbent assay (elisa) and ... | 2016 | 27925065 |
| increased abundance of proteins involved in resistance to oxidative and nitrosative stress at the last stages of growth and development of leishmania amazonensis promastigotes revealed by proteome analysis. | leishmania amazonensis is one of the major etiological agents of the neglected, stigmatizing disease termed american cutaneous leishmaniasis (acl). acl is a zoonosis and rodents are the main reservoirs. most cases of acl are reported in brazil, bolivia, colombia and peru. the biological cycle of the parasite is digenetic because sand fly vectors transmit the motile promastigote stage to the mammalian host dermis during blood meal intakes. the amastigote stage survives within phagocytes of the ma ... | 2016 | 27776144 |
| the brown alga stypopodium zonale (dictyotaceae): a potential source of anti-leishmania drugs. | this study evaluated the anti-leishmania amazonensis activity of a lipophilic extract from the brown alga stypopodium zonale and atomaric acid, its major compound. our initial results revealed high inhibitory activity for intracellular amastigotes in a dose-dependent manner and an ic50 of 0.27 μg/ml. due to its high anti-leishmania activity and low toxicity toward host cells, we fractionated the lipophilic extract. a major meroditerpene in this extract, atomaric acid, and its methyl ester deriva ... | 2016 | 27618071 |
| generating nanoparticles containing a new 4-nitrobenzaldehyde thiosemicarbazone compound with antileishmanial activity. | thiosemicarbazones are an important class of compounds that have been extensively studied in recent years, mainly because of their broad profile of pharmacological activity. a new 4-nitrobenzaldehyde thiosemicarbazone compound (bzts) that was derived from s-limonene has been demonstrated to have significant antiprotozoan activity. however, the hydrophobic characteristic of bzts limits its administration and results in low oral bioavailability. in the present study, we proposed the synthesis of n ... | 2016 | 27612813 |
| antileishmanial activity of ezetimibe: inhibition of sterol biosynthesis, in vitro synergy with azoles, and efficacy in experimental cutaneous leishmaniasis. | leishmaniasis affects mainly low-income populations in tropical regions. radical innovation in drug discovery is time-consuming and expensive, imposing severe restrictions on the ability to launch new chemical entities for the treatment of neglected diseases. drug repositioning is an attractive strategy for addressing a specific demand more easily. in this project, we have evaluated the antileishmanial activities of 30 drugs currently in clinical use for various morbidities. ezetimibe, clinicall ... | 2016 | 27600041 |
| synthesis and evaluation against leishmania amazonensis of novel pyrazolo[3,4-d]pyridazinone-n-acylhydrazone-(bi)thiophene hybrids. | a new series of pyrazolo[3,4-d]pyridazin-7-one derivatives were synthesised and evaluated for their in vitro antileishmanial activity against leishmania amazonensis promastigote and axenic amastigote forms. the results showed that the pyrazolo[3,4-d]-pyridazin-7-one-n-acylhydrazone-(bi)thiophene hybrids 5b, 6b and 6d exhibit better antileishmanial activity with ic50 84.96, 3.63 and 10.79 μm, against the promastigote form and ic50 32.71, 2.32 and >100 μm against the axenic amastigote form, respec ... | 2016 | 27597410 |
| morinda citrifolia linn. reduces parasite load and modulates cytokines and extracellular matrix proteins in c57bl/6 mice infected with leishmania (leishmania) amazonensis. | the absence of an effective vaccine and the debilitating chemotherapy for leishmaniasis demonstrate the need for developing alternative treatments. several studies conducted with morinda citrifolia have shown various biological activities, including antileishmanial activity, however its mechanisms of action are unknown. this study aimed to analyze the in vivo activity of m. citrifolia fruit juice (noni) against leishmania (leishmania) amazonensis in c57bl/6 mice. m. citrifolia fruit juice from t ... | 2016 | 27579922 |