Publications

in vitro activity of the antifungal azoles itraconazole and posaconazole against leishmania amazonensis.	leishmaniasis, caused by protozoan parasites of the leishmania genus, is one of the most prevalent neglected tropical diseases. it is endemic in 98 countries, causing considerable morbidity and mortality. pentavalent antimonials are the first line of treatment for leishmaniasis except in india. in resistant cases, miltefosine, amphotericin b and pentamidine are used. these treatments are unsatisfactory due to toxicity, limited efficacy, high cost and difficult administration. thus, there is an u ...	2013	24376670
cross-protective effect of a combined l5 plus l3 leishmania major ribosomal protein based vaccine combined with a th1 adjuvant in murine cutaneous and visceral leishmaniasis.	two leishmania major ribosomal proteins l3 (lml3) and l5 (lml5) have been described as protective molecules against cutaneous leishmaniasis due to infection with l. major and leishmania braziliensis in balb/c mice when immunized with a th1 adjuvant (non-methylated cpg-oligodeoxynucleotides; cpg-odn). in the present study we analyzed the cross-protective efficacy of an lml3-lml5-cpg odn combined vaccine against infection with leishmania amazonensis and leishmania chagasi (syn. leishmania infantum ...	2014	24382098
unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents.	in this work the synthesis and antiparasitical activity of new 1,5-diaryl-3-oxo-1,4-pentadienyl derivatives are described. first, compounds 1a, 1b, 1c and 1d were prepared by acid-catalyzed aldol reaction between 2-butanone and benzaldehyde, anisaldehyde, p-n,n-dimethylaminobenzaldehyde and p-nitrobenzaldehyde. reacting each of the methyl ketones 1a, 1b, 1c and 1d with the p-substituted benzaldehydes under basic-catalyzed aldol reaction, we further prepared compounds 2a-2p. all twenty compounds ...	2014	24398381
in vitro interaction between surfacen® and surfactant protein a against leishmania amazonensis.	leishmaniasis is caused by a parasite of the leishmania genus, affecting more than 12 million people in 98 countries. the control of leishmaniasis remains a serious problem. there are currently no vaccines for leishmaniasis. the drugs available are toxic, expensive and frequently ineffective. the in vitro activity of surfacen® and sp-a against leishmania amazonensis was evaluated. the combination of both products resulted in a synergic pharmacology effect, demonstrated by a fractional inhibitory ...	2013	24401208
complexes of different nitrogen donor heterocyclic ligands with sbcl3 and phsbcl2 as potential antileishmanial agents against sb(iii)-sensitive and -resistant parasites.	novel trivalent antimony complexes with the nitrogen donor heterocyclic ligand 2,2'-bipyridine (bipy), 1,10-phenanthroline (phen) or dipyrido[3,2-d:2',3'-f]quinoxaline (dpq) have been synthesized by the reaction with sbcl3 or phsbcl2. the crystal structures of [sb(phen)cl3] and [phsb(phen)cl2]ch3cooh were determined and shown to adopt a distorted square pyramid geometry with a five-coordinated sb center. surprisingly, all the complexes, the ligands and phsbcl2 showed very high antileishmanial ac ...	2014	24412095
dynamic identification of h2 epitopes from leishmania (leishmania) amazonensis cysteine proteinase b with potential immune activity during murine infection.	peptides from the cooh-terminal extension of cysteine proteinase b from leishmania (leishmania) amazonensis (cyspep) can modulate immune responses in vertebrate hosts. with this hypothesis as base, we used the online analysis tool syfpeithi to predict seven epitopes from this region with potential to bind h2 proteins. we performed proliferation tests and quantified reactive t lymphocytes applying a cytometry analysis, using samples from draining lymph node of lesions from l. (l.) amazonensis-inf ...	2014	24436127
excreted leishmania peruviana and leishmania amazonensis iron-superoxide dismutase purification: specific antibody detection in colombian patients with cutaneous leishmaniasis.	leishmania sp. survival in the vertebrate host depends on the host macrophage immune response as well as on the parasite's defense against free radicals. iron-superoxide dismutase (fe-sod) is a key antioxidant enzyme that contributes to radical superoxide dismutation, preventing the disease from surging and propagating itself. leishmania sp. has various fe-sod isoforms, one of which (fe-sode) is excreted into the medium and, being highly immunogenic, can be considered a very good molecular marke ...	2014	24440468
targeted extracellular signal-regulated kinase activation mediated by leishmania amazonensis requires mp1 scaffold.	leishmania amazonensis infection promotes alteration of host cellular signaling and intracellular parasite survival, but specific mechanisms are poorly understood. we previously demonstrated that l. amazonensis infection of dendritic cells (dc) activated extracellular signal-regulated kinase (erk), an map-kinase kinase kinase, leading to altered dc maturation and non-healing cutaneous leishmaniasis. studies using growth factors and cell lines have shown that targeted, robust, intracellular phosp ...	2014	24463270
leishmania braziliensis and leishmania amazonensis amastigote extracts differ in their enhancement effect on leishmania infection when injected intradermally.	it has been reported that repeated intravenous injections of a relatively large amount of leishmania amazonensis amastigote extract (lae) in balb/c mice exacerbates the infection of these mice by leishmania braziliensis. the identification of the extract active principle(s) through physicochemical purification often involves dilution and losses of protein in the course of successive purification procedures. the large amount of the extract required to induce the phenomenon, therefore, hinders the ...	2014	24484604
leishmania-mediated inhibition of iron export promotes parasite replication in macrophages.	leishmania parasites infect macrophages, cells that play an important role in organismal iron homeostasis. by expressing ferroportin, a membrane protein specialized in iron export, macrophages release iron stored intracellularly into the circulation. iron is essential for the intracellular replication of leishmania, but how the parasites compete with the iron export function of their host cell is unknown. here, we show that infection with leishmania amazonensis inhibits ferroportin expression in ...	2014	24497831
the calpain inhibitor mdl28170 induces the expression of apoptotic markers in leishmania amazonensis promastigotes.	human cutaneous leishmaniasis is caused by distinct species, including leishmania amazonensis. treatment of cutaneous leishmaniasis is far from satisfactory due to increases in drug resistance and relapses, and toxicity of compounds to the host. as a consequence for this situation, the development of new leishmanicidal drugs and the search of new targets in the parasite biology are important goals.	2014	24498160
sod1 plasma level as a biomarker for therapeutic failure in cutaneous leishmaniasis.	we show that increased plasma superoxide dismutase 1 (sod1) levels are statistically significant predictors of the failure of pentavalent antimony treatment for cutaneous leishmaniasis caused by leishmania braziliensis. in leishmania amazonensis-infected patients, host sod1 levels can be used to discriminate between localized and drug-resistant diffuse cutaneous leishmaniasis. using in situ transcriptomics (ncounter), we demonstrate a significant positive correlation between host sod1 and interf ...	2014	24511100
isolation of arginase inhibitors from the bioactivity-guided fractionation of byrsonima coccolobifolia leaves and stems.	byrsonima coccolobifolia leaf and stem extracts were studied in the search for possible leishmanicidal compounds using arginase (arg) from leishmania amazonensis as a molecular target. flavonoids 1b, 1e-1g, 2a, 2b, and 2d-2f showed significant inhibitory activity, with ic50 values ranging from 0.9 to 4.8 μm. the kinetics of the most active compounds were determined. flavonoids 1e, 1f, 2a, 2b, and 2e were characterized as noncompetitive inhibitors of arg with dissociation constants (ki) ranging f ...	2014	24521209
2-acylamino-5-nitro-1,3-thiazoles: preparation and in vitro bioevaluation against four neglected protozoan parasites.	the 2-acylamino-5-nitro-1,3-thiazole derivatives (1-14) were prepared using a one step reaction. all compounds were tested in vitro against four neglected protozoan parasites (giardia intestinalis, trichomonas vaginalis, leishmania amazonensis and trypanosoma cruzi). acetamide (9), valeroylamide (10), benzamide (12), methylcarbamate (13) and ethyloxamate (14) derivatives were the most active compounds against g. intestinalis and t. vaginalis, showing nanomolar inhibition. compound 13 (ic50=10nm) ...	2014	24529307
molecular characterization of the mrpa transporter and antimony uptake in four new world leishmania spp. susceptible and resistant to antimony.	atp-binding cassette (abc) transporters have been associated with drug resistance in various diseases. the mrpa gene, a transporter of abcc subfamily, is involved in the resistance by sequestering metal-thiol conjugates in intracellular vesicles of leishmania parasite. in this study, we performed the molecular characterization of the mrpa transporter, analysis of p-glycoprotein (pgp) and aquaglyceroporin-1 (aqp1) expression, and determination of antimony level in antimony-susceptible and -resist ...	2013	24533304
potential therapeutic use of herbal extracts in trypanosomiasis.	the aim of the present study was to evaluate the effects of crude extracts from handroanthus impetiginosa, ageratum conyzoides, and ruta graveolens on leishmania amazonensis and trypanosoma cruzi infection in vitro. the results showed that the extracts caused significant toxicity in promastigotes and trypomastigotes. a significant decrease in the rate of cell invasion by pretreated trypomastigotes and promastigotes was also observed. the extracts caused a significant reduction of the multiplicat ...	2014	24548158
combination therapy with tamoxifen and amphotericin b in experimental cutaneous leishmaniasis.	leishmaniasis chemotherapy remains very challenging. the high cost of active drugs, along with the severity of their side effects and the increasing failure rate of the current therapeutic schemes, calls for the discovery of new active drugs and schemes of treatment. the use of combination therapy has gained much attention in recent years as a possible strategy for overcoming the various shortcomings in the present arsenal. we recently described the effectiveness of tamoxifen in murine models of ...	2014	24550333
miltefosine increases lipid and protein dynamics in leishmania amazonensis membranes at concentrations similar to those needed for cytotoxicity activity.	miltefosine (mt) is a membrane-active alkylphospholipid licensed for the topical treatment of breast cancer skin metastases and the oral treatment of leishmaniasis, although its mechanism of action remains unclear. electron paramagnetic resonance (epr) spectroscopy of a spin-labeled lipid and a thiol-specific spin label in the plasma membrane of leishmania promastigotes showed that mt causes dramatic increases in membrane dynamics. although these alterations can be detected using a spin-labeled ...	2014	24614380
identification and characterization of new leishmania promastigote surface antigens, lapsa-38s and lipsa-50s, as major immunodominant excreted/secreted components of l. amazonensis and l. infantum.	we have previously demonstrated that sera from dogs vaccinated with excreted/secreted antigens (esa) of leishmania infantum promastigotes (liesap) mainly recognized an immunodominant antigen of 54 kda. an anti-liesap-specific igg2 humoral response was observed and associated to th1-type response in vaccinated dogs. this response was highly correlated with a long-lasting and strong liesap-vaccine protection toward l. infantum experimental infection. in addition, it was also shown that dogs from t ...	2014	24614507
novel targeting using nanoparticles: an approach to the development of an effective anti-leishmanial drug-delivery system.	the study reported here aimed to develop an optimized nanoparticle delivery system for amphotericin b (ampb) using a polyelectrolyte complexation technique. for this, two oppositely charged polymers presenting anti-leishmanial activity - chitosan (cs) and chondroitin sulfate (chs) - were used: cs as a positively charged polymer and chs as a negatively charged polymer. the chitosan (nq) nanoparticles, chitosan-chondroitin sulfate (nqc) nanoparticles, and chitosan-chondroitin sulfate-amphotericin ...	2014	24627630
understanding the mechanisms controlling leishmania amazonensis infection in vitro: the role of ltb4 derived from human neutrophils.	neutrophils are rapidly recruited to the site of leishmania infection and play an active role in capturing and killing parasites. they are the main source of leukotriene b4 (ltb4), a potent proinflammatory lipid mediator. however, the role of ltb4 in neutrophil infection by leishmania amazonensis is not clear. in this study, we show that l. amazonensis or its lipophosphoglycan can induce neutrophil activation, degranulation, and ltb4 production. using pharmacological inhibitors of leukotriene sy ...	2014	24634497
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
activity of anti-cancer protein kinase inhibitors against leishmania spp.	there is an urgent need to develop new and effective treatments for poverty-related neglected diseases. in light of the time required to bring a new drug to market and the cost involved (10-15 years, >1 billion us$), one approach to identifying new treatments for diseases like leishmaniasis is to evaluate drugs that are already registered for the treatment of other diseases. this paper describes the anti-leishmanial activities of 10 fda-approved protein kinase inhibitors already available for th ...	2014	24668412
correlation between glucose uptake and membrane potential in leishmania parasites isolated from dcl patients with therapeutic failure: a proof of concept.	besides infection with drug-resistant parasites, therapeutic failure in leishmaniasis may be caused by altered drug pharmacokinetics, re-infection, and host immunologic compromise. our aim has been to evaluate if relapses that occur in patients suffering from diffuse cutaneous leishmaniasis (dcl) associate with changes in the fitness of infecting organisms. therefore, in isolates from patients suffering dcl, we correlated glucose uptake and plasma membrane potential and compared the results with ...	2014	24671239
in vitro and in vivo efficacy of novel flavonoid dimers against cutaneous leishmaniasis.	treatment of leishmaniasis by chemotherapy remains a challenge because of limited efficacy, toxic side effects, and drug resistance. we previously reported that synthetic flavonoid dimers have potent antipromastigote and antiamastigote activity against leishmania donovani, the causative agent of visceral leishmaniasis. here, we further investigate their leishmanicidal activities against cutaneous leishmania species. one of the flavonoid dimers (compound 39) has marked antipromastigote (50% inhib ...	2014	24687505
identification of differentially expressed proteins from leishmania amazonensis associated with the loss of virulence of the parasites.	the present study analyzed whether or not the in vitro cultivation for long periods of time of pre-isolated leishmania amazonensis from lesions of chronically infected balb/c mice was able to interfere in the parasites' infectivity using in vivo and in vitro experiments. in addition, the proteins that presented a significant decrease or increase in their protein expression content were identified applying a proteomic approach.	2014	24699271
in vitro cytokines profile and ultrastructural changes of microglia and macrophages following interaction with leishmania.	in the present study, we assessed morphological changes and cytokine production after in vitro interaction with causative agents of american cutaneous leishmaniasis and compared the microglia and macrophage immune responses. cultures of microglia and macrophages infected with stationary-phase promastigotes of leishmania (viannia) shawi, leishmania (viannia) braziliensis or leishmania (leishmania) amazonensis were evaluated 24, 48 and 72 h after interaction. macrophages only presented the classic ...	2014	24717447
purification and biochemical characterization of three myotoxins from bothrops mattogrossensis snake venom with toxicity against leishmania and tumor cells.	bothrops mattogrossensis snake is widely distributed throughout eastern south america and is responsible for snakebites in this region. this paper reports the purification and biochemical characterization of three new phospholipases a2 (pla2s), one of which is presumably an enzymatically active asp49 and two are very likely enzymatically inactive lys49 pla2 homologues. the purification was obtained after two chromatographic steps on ion exchange and reverse phase column. the 2d sds-page analysis ...	2014	24724078
antiparasitic activities of novel ruthenium/lapachol complexes.	the present study describes the synthesis, characterization, antileishmanial and antiplasmodial activities of novel diimine/(2,2'-bipyridine (bipy), 1,10-phenanthroline (phen), 4,4'-methylbipyridine (me-bipy) and 4,4'-methoxybipyridine (meo-bipy)/phosphine/ruthenium(ii) complexes containing lapachol (lap, 2-hydroxy-3-(3-33 methyl-2-buthenyl)-1,4-naphthoquinone) as bidentate ligand. the [ru(lap)(pph3)2(bipy)]pf6 (1), [ru(lap)(pph3)2(me-bipy)]pf6 (2), [ru(lap)(pph3)2(meo-bipy)]pf6(3) and[ru(lap)(p ...	2014	24727183
leukotriene b4 modulates p2x7 receptor-mediated leishmania amazonensis elimination in murine macrophages.	atp is an important signaling molecule in the immune system, and it is able to bind the p2x7 purinergic receptor. recently, our group showed that atp-treated macrophages eliminate leishmania amazonensis. it has been reported that leukotriene b4 (ltb4) reduces the parasitic load of infected macrophages. additionally, it has been demonstrated that the p2x7 receptor can induce pla2 activation and arachidonic acid mobilization. based on these findings, we investigated whether ltb4 is produced upon p ...	2014	24729618
role of protein kinase r in the killing of leishmania major by macrophages in response to neutrophil elastase and tlr4 via tnfα and ifnβ.	in cutaneous leishmaniasis, leishmania amazonensis activates macrophage double-stranded, rna-activated protein kinase r (pkr) to promote parasite growth. in our study, leishmania major grew normally in raw cells, raw-expressing dominant-negative pkr (pkr-dn) cells, and macrophages of pkr-knockout mice, revealing that pkr is dispensable for l. major growth in macrophages. pkr activation in infected macrophages with poly i:c resulted in parasite death. fifty percent of l. major-knockout lines for ...	2014	24732131
leishmania amazonensis promastigotes in 3d collagen i culture: an in vitro physiological environment for the study of extracellular matrix and host cell interactions.	leishmania amazonensis is the causative agent of american cutaneous leishmaniasis, an important neglected tropical disease. once leishmania amazonensis is inoculated into the human host, promastigotes are exposed to the extracellular matrix (ecm) of the dermis. however, little is known about the interaction between the ecm and leishmania promastigotes. in this study we established l. amazonensis promastigote culture in a three-dimensional (3d) environment mainly composed of collagen i (col i). t ...	2014	24765565
antileishmanial activity of essential oil from chenopodium ambrosioides and its main components against experimental cutaneous leishmaniasis in balb/c mice.	chenopodium ambrosioides have been used during centuries by native people to treat parasitic diseases.	2014	24768411
leishmanicidal evaluation of tetrahydroprotoberberine and spirocyclic erythrina-alkaloids.	leishmaniasis is one of the world's most problematic diseases in developing countries. traditional medicines to treat leishmaniasis have serious side effects, as well as significant parasite resistance problems. in this work, two alkaloids 1 and 2 were obtained from corydalis govaniana wall and seven alkaloids 3-9, were obtained from erythrina verna. the structures of the compounds were confirmed by mass spectrometry and 1d- and 2d-nmr spectroscopy. the leishmanicidal activity of compounds 1-9 a ...	2014	24802983
periodate-oxidized atp modulates macrophage functions during infection with leishmania amazonensis.	previously, we showed that treating macrophages with atp impairs the intracellular growth of leishmania amazonensis, and that the p2x7 purinergic receptor is overexpressed during leishmaniasis. in the present study, we directly evaluated the effect of periodate-oxidized atp (oatp) on parasite control in leishmania-infected macrophages. we found that oatp impaired the attachment/entrance of l. amazonensis promastigotes to c57bl/6 mouse macrophages in a p2x7 receptor-independent manner, as macroph ...	2014	24804957
in vitro and in vivo antileishmania activity of sesquiterpene lactone-rich dichloromethane fraction obtained from tanacetum parthenium (l.) schultz-bip.	the discovery of new treatments for neglected diseases, including leishmaniasis, is a substantial challenge for scientific research. plant extracts have shown potential in the selective treatment of tropical diseases. the present study evaluated the in vitro and in vivo antileishmania effects of a sesquiterpene lactone-rich dichloromethane fraction (df) obtained from the aerial parts of tanacetum parthenium (l.) schultz-bip. in vitro studies of the df indicated an ic50 of 2.40±0.76 μg ml(-1) aga ...	2014	24810433
antileishmanial activity of the estrogen receptor modulator raloxifene.	the treatment of leishmaniasis relies mostly on parenteral drugs with potentially serious adverse effects. additionally, parasite resistance in the treatment of leishmaniasis has been demonstrated for the majority of drugs available, making the search for more effective and less toxic drugs and treatment regimens a priority for the control of leishmaniasis. the aims of this study were to evaluate the antileishmanial activity of raloxifene in vitro and in vivo and to investigate its mechanism of ...	2014	24810565
arrabidaea chica hexanic extract induces mitochondrion damage and peptidase inhibition on leishmania spp.	currently available leishmaniasis treatments are limited due to severe side effects. arrabidaea chica is a medicinal plant used in brazil against several diseases. in this study, we investigated the effects of 5 fractions obtained from the crude hexanic extract of a. chica against leishmania amazonensis and l. infantum, as well as on the interaction of these parasites with host cells. promastigotes were treated with several concentrations of the fractions obtained from a. chica for determination ...	2014	24818162
cross-protective immunity to leishmania amazonensis is mediated by cd4+ and cd8+ epitopes of leishmania donovani nucleoside hydrolase terminal domains.	the nucleoside hydrolase (nh) of leishmania donovani (nh36) is a phylogenetic marker of high homology among leishmania parasites. in mice and dog vaccination, nh36 induces a cd4+ t cell-driven protective response against leishmania chagasi infection directed against its c-terminal domain (f3). the c-terminal and n-terminal domain vaccines also decreased the footpad lesion caused by leishmania amazonensis. we studied the basis of the crossed immune response using recombinant generated peptides co ...	2014	24822054
cell-to-cell transfer of leishmania amazonensis amastigotes is mediated by immunomodulatory lamp-rich parasitophorous extrusions.	the last step of leishmania intracellular life cycle is the egress of amastigotes from the host cell and their uptake by adjacent cells. using multidimensional live imaging of long-term-infected macrophage cultures we observed that leishmania amazonensis amastigotes were transferred from cell to cell when the donor host macrophage delivers warning signs of imminent apoptosis. they were extruded from the macrophage within zeiotic structures (membrane blebs, an apoptotic feature) rich in phagolyso ...	2014	24824158
chronic infection by leishmania amazonensis mediated through mapk erk mechanisms.	leishmania amazonensis is an intracellular protozoan parasite responsible for chronic cutaneous leishmaniasis (cl). cl is a neglected tropical disease responsible for infecting millions of people worldwide. l. amazonensis promotes alteration of various signaling pathways that are essential for host cell survival. specifically, through parasite-mediated phosphorylation of extracellular signal regulated kinase (erk), l. amazonensis inhibits cell-mediated parasite killing and promotes its own survi ...	0	24838145
antileishmanial activity and cytotoxicity of brazilian plants.	leishmaniasis is a major public health problem, and the alarming spread of parasite resistance has increased the importance of discovering new therapeutic products. the present study aimed to investigate the in vitro leishmanicidal activity from 16 different brazilian medicinal plants. stationary-phase promastigotes of leishmania amazonensis and murine macrophages were exposed to 44 plant extracts or fractions for 48 h at 37°c, in order to evaluate their antileishmanial activity and cytotoxicity ...	2014	24846006
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
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 = ...	2014	24906989
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 ...	2014	24913171
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.	2014	24913205
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 ...	2014	24956553
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 ...	2014	24966857
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 ...	2014	24989828
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 ...	2014	24996348
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
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 ...	2014	25014108
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 ...	2014	25029171
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 ...	2014	25033218
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 ...	2014	25033301
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 ...	2014	25045693
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 ...	2014	25092697
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 ...	2014	25101672
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. ...	2014	25102355
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 ...	2014	25114129
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
antileishmanial activity of medicinal plants used in endemic areas in northeastern brazil.	this study investigates the leishmanicidal activity of five species of plants used in folk medicine in endemic areas of the state of alagoas, brazil. data were collected in the cities of colonia leopoldina, novo lino, and união dos palmares, alagoas state, from patients with cutaneous leishmaniasis (leishmania amazonensis) who use medicinal plants to treat this disease. plants extracts were tested at a concentration of 1-100 μg/ml in all experiments, except in an assay to evaluate activity again ...	2014	25126099
leishmania amazonensis infection impairs dendritic cell migration from the inflammatory site to the draining lymph node.	in vitro studies show that leishmania infection decreases the adhesion of inflammatory phagocytes to connective tissue by a mechanism dependent on the modulation of integrin function. however, we know little about the influence of this reduction in leukocyte adhesion on parasite dissemination from the infection site.	2014	25142021
leishmania amazonensis: increase in ecto-atpase activity and parasite burden of vinblastine-resistant protozoa.	leishmania amazonensis is a protozoan parasite that induces mucocutaneous and diffuse cutaneous lesions upon infection. an important component in treatment failure is the emergence of drug-resistant parasites. it is necessary to clarify the mechanism of resistance that occurs in these parasites to develop effective drugs for leishmaniasis treatment. promastigote forms of l. amazonensis were selected by gradually increasing concentrations of vinblastine and were maintained under continuous drug p ...	2014	25176449
an in vitro model of antibody-enhanced killing of the intracellular parasite leishmania amazonensis.	footpad infection of c3heb/fej mice with leishmania amazonensis leads to chronic lesions accompanied by large parasite loads. co-infecting these animals with l. major leads to induction of an effective th1 immune response that can resolve these lesions. this cross-protection can be recapitulated in vitro by using immune cells from l. major-infected animals to effectively activate l. amazonensis-infected macrophages to kill the parasite. we have shown previously that the b cell population and the ...	2014	25191842
furofuran lignans display schistosomicidal and trypanocidal activities.	parasitic diseases continue to be a major worldwide health problem, and there is an urgent need for development of therapeutic drugs. this paper describes synthesis of dehydrodiferulic acid dilactone 1 and dehydrodisinapic acid dilactone 2 furofuran lignans by oxidative coupling of ferulic and sinapic acids, respectively. their schistosomicidal, trypanocidal, and leishmanicidal activities were evaluated in vitro against schistosoma mansoni adult worms, trypomastigote and amastigotes forms of try ...	2014	25200100
the in vitro biological activity of the brazilian brown seaweed dictyota mertensii against leishmania amazonensis.	seaweeds present a wide variety of interesting bioactive molecules. in the present work we evaluated the biological activity of the dichloromethane/methanol (2:1) extract (dme) from the brown seaweed dictyota mertensii against leishmania amazonensis and its cytotoxic potential on mammalian cells. the extract showed significant inhibitory effect on the growth of promastigote forms (ic50=71.60 μg/ml) and low toxicity against mammalian cells (cc50=233.10 μg/ml). the dme was also efficient in inhibi ...	2014	25207712
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 ...	2014	25224005
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.	2014	25229296
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- ...	2014	25232947
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.	2014	25239157
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 ...	2014	25247686
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.	2014	25251262
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 ...	2014	25253283
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
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
insulin-like growth factor-i induces arginase activity in leishmania amazonensis amastigote-infected macrophages through a cytokine-independent mechanism.	leishmania (leishmania) amazonensis exhibits peculiarities in its interactions with hosts. because amastigotes are the primary form associated with the progression of infection, we studied the effect of insulin-like growth factor (igf)-i on interactions between l. (l.) amazonensis amastigotes and macrophages. upon stimulation of infected macrophages with igf-i, we observed decreased nitric oxide production but increased arginase expression and activity, which lead to increased parasitism. howeve ...	2014	25294956
evidences for leishmanicidal activity of the naphthoquinone derivative epoxy-α-lapachone.	in this work, we analyze the leishmanicidal effects of epoxy-α-lapachone on leishmania (viannia) braziliensis and leishmania (leishmania) amazonensis. promasigotes and amastigotes (inhabiting human macrophages) from both species were assayed to verify the compound's activity over the distinct morphological stages. the incubation with epoxy-α-lapachone led to a significant decrease in the numbers of promastigotes from both species in the cultures, in a dose-and time-dependent fashion. the surviva ...	2014	25307687
the comparative genomics and phylogenomics of leishmania amazonensis parasite.	leishmaniasis is an infectious disease caused by leishmania species. leishmania amazonensis is a new world leishmania species belonging to the mexicana complex, which is able to cause all types of leishmaniasis infections. the l. amazonensis reference strain mhom/br/1973/m2269 was sequenced identifying 8,802 codifying sequences (cds), most of them of hypothetical function. comparative analysis using six leishmania species showed a core set of 7,016 orthologs. l. amazonensis and leishmania mexica ...	2014	25336895
pterocarpanquinone lqb-118 induces apoptosis in leishmania (viannia) braziliensis and controls lesions in infected hamsters.	previous results demonstrate that the hybrid synthetic pterocarpanquinone lqb-118 presents antileishmanial activity against leishmania amazonensis in a mouse model. the aim of the present study was to use a hamster model to investigate whether lqb-118 presents antileishmanial activity against leishmania (viannia) braziliensis, which is the major leishmania species related to american tegumentary leishmaniasis. the in vitro antileishmanial activity of lqb-118 on l. braziliensis was tested on the ...	2014	25340550
protective effects of the antileishmanial extract of tephrosia cinerea (l.) pers. (fabaceae) against cyclophosphamide-induced damage.	tephrosia cinerea l. (pers.) is a tropical species that exhibits antileishmanial activity in leishmania amazonensis promastigote cultures and is commonly used to treat infections, inflammations, ulcers, nervous conditions, and diarrhea. however, no studies have investigated its effects on genetic material. therefore, we evaluated the genotoxic potential, antigenotoxic potential, and cytotoxic effects of hydroalcoholic extracts of t. cinerea leaves. in an in vitro genotoxicity study, human periph ...	2014	25366795
[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
an optimized nanoparticle delivery system based on chitosan and chondroitin sulfate molecules reduces the toxicity of amphotericin b and is effective in treating tegumentary leishmaniasis.	amphotericin b (ampb) is active against leishmaniasis, but its use is hampered due to its high toxicity observed in patients. in this study, a nanoparticles-delivery system for ampb (nqc-ampb), containing chitosan and chondroitin sulfate molecules, was evaluated in balb/c mice against leishmania amazonensis. an in vivo biodistribution study, including biochemical and toxicological evaluations, was performed to evaluate the toxicity of ampb. nanoparticles were radiolabeled with technetium-99m and ...	2014	25429219
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
rpa-1 from leishmania amazonensis (larpa-1) structurally differs from other eukaryote rpa-1 and interacts with telomeric dna via its n-terminal ob-fold domain.	replication protein a-1 (rpa-1) is a single-stranded dna-binding protein involved in dna metabolism. we previously demonstrated the interaction between larpa-1 and telomeric dna. here, we expressed and purified truncated mutants of larpa-1 and used circular dichroism measurements and molecular dynamics simulations to demonstrate that the tertiary structure of larpa-1 differs from human and yeast rpa-1. larpa-1 interacts with telomeric ssdna via its n-terminal ob-fold domain, whereas rpa from hig ...	2014	25451229
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
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
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
salivary gland homogenates from wild-caught sand flies lutzomyia flaviscutellata and lutzomyia (psychodopygus) complexus showed inhibitory effects on leishmania (leishmania) amazonensis and leishmania (viannia) braziliensis infection in balb/c mice.	during the natural transmission of leishmania parasites, the infected sand fly female regurgitates promastigotes into the host's skin together with its saliva. it has been reported that vector saliva contains immunomodulatory molecules that facilitate the establishment of infection. thus, the main objective of this study was to evaluate the specificity of lutzomyia (lu.) flaviscutellata and lu. (psychodopygus) complexus salivas on the infectivity of leishmania (l.) (leishmania) amazonensis and l ...	2014	25476864
leishmania braziliensis replication protein a subunit 1: molecular modelling, protein expression and analysis of its affinity for both dna and rna.	replication factor a (rpa) is a single-strand dna binding protein involved in dna replication, recombination and repair processes. it is composed by the subunits rpa-1, rpa-2 and rpa-3; the major dna-binding activity resides in the subunit 1 of the heterotrimeric rpa complex. in yeast and higher eukaryotes, besides the three basic structural dna-binding domains, the rpa-1 subunit contains an n-terminal region involved in protein-protein interactions with a fourth dna-binding domain. remarkably, ...	2014	25498946
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
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 ...	2014	25516829
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
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
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
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 ...	2014	25591109
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
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
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
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