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impact of reactive oxygen species (ros) on the control of parasite loads and inflammation in leishmania amazonensis infection.reactive oxygen species (ros) protect the host against a large number of pathogenic microorganisms. ros have different effects on parasites of the genus leishmania: some parasites are susceptible to their action, while others seem to be resistant. the role of ros in l. amazonensis infection in vivo has not been addressed to date.201627056545
imipramine alters the sterol profile in leishmania amazonensis and increases its sensitivity to miconazole.imipramine, a tricyclic antidepressant widely used clinically, has other pharmacological effects, such as antileishmanial activity. tricyclic antidepressants interact with lipid bilayers, and some studies have shown that imipramine inhibits methyltransferases. leishmania spp. produces compounds with an ergostane skeleton instead of a cholesterol skeleton, and the inhibition of enzymes of the sterol biosynthesis pathway is an interesting therapeutic target. among these enzymes, c-24 methyltransfe ...201627036654
a new 5-alkylresorcinol glucoside derivative from cybianthus magnus.one new 5-alkylresorcinol glucoside (1) was isolated from leaves of cybianthus magnus, along with 12 known compounds (2-13), isolated from four plants belonging to myrsinaceae family. their structures were determined on the basis of spectroscopic analysis and by comparison of their spectral data with those reported in the literature. among the tested molecules, only compound 2 displayed a strong cytotoxic activity with ic50 values ranging between 22 and 100 μm for all cell lines tested. one new ...201626181307
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 ...201626407073
evaluation of leishmanicidal and trypanocidal activities of phenolic compounds from calea uniflora less.the phytochemical study of calea uniflora led to the isolation of nine phenolic compounds identified as noreugenin (1), ethyl caffeate (2), a mixture of butein (3) + orobol (4), α-hydroxy-butein (5), caffeic acid (6), butein 4'-o-glucopyranosyl (7), quercetin 3-o-glucopyranosyl (8) and 3,5-di-o-caffeoylquinic acid (9). the chemical identity of the isolates was established on the basis of nmr and physical data. the chemical shifts of 5 and 7 have been reassigned and all the isolates were tested a ...201625880257
[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 ...201625418662
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 ...201624856420
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.201624662018
structural and dynamic insights into the c-terminal extension of cysteine proteinase b from leishmania amazonensis.cysteine proteinase b (cpb) is a significant virulence factor for leishmania infections. upon processing from its zymogen form, it happens a release of the immunomodulatory cpb c-terminal extension (cyspep) into the cytoplasm of the macrophage. epitopes derived from this fragment were shown to influence the proportion of lymphocytes cd8+ upon infection, favoring the parasite escaping from the host́s immune system. at present, there is no available structural data of cyspep, which impairs a prope ...201627649549
in vitro and in vivo miltefosine susceptibility of a leishmania amazonensis isolate from a patient with diffuse cutaneous leishmaniasis: follow-up. 201627416021
risk assessment of soulatrolide and mammea (a/ba+a/bb) coumarins from calophyllum brasiliense by a toxicogenomic and toxicological approach.calophyllum brasiliense (calophyllaceae) is a tropical rain forest tree distributed in central and south america. it is an important source of tetracyclic dipyrano coumarins (soulatrolide) and mammea type coumarins. soulatrolide is a potent inhibitor of hiv-1 reverse transcriptase and displays activity against mycobacterium tuberculosis. meanwhile, mammea a/ba and a/bb, pure or as a mixture, are highly active against several human leukemia cell lines, trypanosoma cruzi and leishmania amazonensis ...201626995226
exploiting death: apoptotic immunity in microbial pathogenesis.innate immunity typically is responsible for initial host responses against infections. independently, nucleated cells that die normally as part of the physiological process of homeostasis in mammals (including humans) suppress immunity. specifically, the physiological process of cell death (apoptosis) generates cells that are recognized specifically by viable cells of all types and elicit a profound transient suppression of host immunity (termed 'innate apoptotic immunity' (iai)). iai appears t ...201626943319
synthesis and antileishmanial activity of natural dehydrodieugenol and its mono- and dimethyl ethers.the study of chemistry of naturally occurring compounds and the synthesis of their derivatives is fundamentally important for the development of new drugs. in this work, dehydrodieugenol (dhde) was obtained through oxidative coupling of eugenol, promoted by an aqueous mixture of potassium ferricyanide (k3 [fe(cn)6 ]) and nh3  · h2 o. the partial methoxylation of dhde with mei and k2 co3 mainly resulted in the molecular-shaped monomethyl ether (dhde-1meo) and its dimethyl ether derivative (dhde-2 ...201627251851
the antifungal compound butenafine eliminates promastigote and amastigote forms of leishmania (leishmania) amazonensis and leishmania (viannia) braziliensis.the production of ergosterol lipid, important for the leishmania membrane homeostasis, involves different enzymes. this pathway can be blocked to azoles and allylamines drugs, such as butenafine. the aim of the present work was to evaluate the anti-leishmanicidal activity of this drug in 2 major species of leishmania responsible for causing the american tegumentar leishmaniasis (l. (l.) amazonensis and l. (v.) braziliensis). butenafine eliminated promastigote forms of l. amazonensis and l. brazi ...201627546158
inhibitory effects promoted by 5'-nucleotides on the ecto-3'-nucleotidase activity of leishmania amazonensis.the protozoan parasite leishmania amazonensis is the etiological agent of cutaneous leishmaniasis. during its life cycle, the flagellated metacyclic promastigote forms are transmitted to vertebrate hosts by sandfly bites, and they develop into amastigotes inside macrophages, where they multiply. l. amazonensis possesses a bifunctional enzyme, called 3'-nucleotidase/nuclease (3'nt/nu), which is able to hydrolyze extracellular 3'-monophosphorylated nucleosides and nucleic acids. 3'nt/nu plays an i ...201627531705
antiparasitic effect of dinoponera quadriceps giant ant venom.neglected tropical diseases (ntd) are treated with toxic therapy of limited efficacy. previously, we studied the antimicrobial effect of dinoponera quadriceps venom (dqv) against bacteria. to continue the study, we report in this short communication the antimicrobial effect of dqv against leishmania amazonensis and trypanosoma cruzi. dqv inhibits the promastigote forms of l. amazonensis and all t. cruzi developmental forms, with low toxicity in host cells. dqv causes cell death in t. cruzi throu ...201627530664
in vitro antileishmanial activity of sterols from trametes versicolor (bres. rivarden).two ergostanes, 5α,8α-epidioxy-22e-ergosta-6,22-dien-3β-ol (1) and 5α-ergost-7,22-dien-3β-ol (2), and a lanostane, 3β-hydroxylanostan-8,24-diene-21-oic acid (trametenolic acid) (3), were isolated from an n-hexane extract prepared from the fruiting body of trametes versicolor (bres. rivarden). the activity of the isolated sterols was evaluated against promastigotes and amastigotes of leishmania amazonensis lainson and shaw, 1972. the lanostane, compound (3), showed the best inhibitory response (i ...201627517895
antileishmanial activity of new thiophene-indole hybrids: design, synthesis, biological and cytotoxic evaluation, and chemometric studies.in the present work, thirty-two hybrid compounds containing cycloalka[b]thiophene and indole moieties (tn5, tn5 1-7, tn6, tn6 1-7, tn7, tn7 1-7, tn8, tn8 1-7) were designed, synthesized and evaluated for their cytotoxic and antileishmanial activity against leishmania amazonensis promastigotes. more than half of the compounds (18 compounds) exhibited significant antileishmanial activity (ic50 lower than 10.0μg/l), showing better performance than the reference drugs (tri- and penta-valent antimoni ...201627515718
recombinant forms of leishmania amazonensis excreted/secreted promastigote surface antigen (psa) induce protective immune responses in dogs.preventive vaccination is a highly promising strategy for interrupting leishmaniasis transmission that can, additionally, contribute to elimination. a vaccine formulation based on naturally excreted secreted (es) antigens was prepared from l. infantum promastigote culture supernatant. this vaccine achieved successful results in phase iii trials and was licensed and marketed as canileish. we recently showed that newly identified es promastigote surface antigen (psa), from both viable promastigote ...201627223609
immunoproteomic and bioinformatic approaches to identify secreted leishmania amazonensis, l. braziliensis, and l. infantum proteins with specific reactivity using canine serum.leishmania spp have a wide range of hosts, and each host can harbor several leishmania species. dogs, for example, are frequently infected by leishmania infantum, where they constitute its main reservoir, but they also serve as hosts for l. braziliensis and l. amazonensis. serological tests for antibody detection are valuable tools for diagnosis of l. infantum infection due to the high levels of antibodies induced, unlike what is observed in l. amazonensis and l. braziliensis infections. likewis ...201627198787
sodium nitroprusside has leishmanicidal activity independent of inos.leishmaniasis is a zoonotic disease caused by protozoa of the genus leishmania . cutaneous leishmaniasis is the most common form, with millions of new cases worldwide each year. treatments are ineffective due to the toxicity of existing drugs and the resistance acquired by certain strains of the parasite.201627163566
neutrophil extracellular traps release induced by leishmania: role of pi3kγ, erk, pi3kσ, pkc, and [ca2+].upon in vitro stimulation, neutrophils undergo a cell death named netosis. this process is characterized by extracellular release of chromatin scaffold associated with granular and cytoplasmic proteins, which together, ensnare and kill microbes. we have previously described that interaction of leishmania amazonensis with human neutrophils leads to the release of neutrophil extracellular traps, which trap and kill the parasite. however, the signaling leading to leishmania induced netosis is still ...201627154356
poloxamer 407 (pluronic(®) f127)-based polymeric micelles for amphotericin b: in vitro biological activity, toxicity and in vivo therapeutic efficacy against murine tegumentary leishmaniasis.in the present study, a poloxamer 407-based amphotericin b (ampb)-containing polymeric micelles system (ampb/m) was employed in the treatment of leishmania amazonensis-infected balb/c mice. initially, the in vitro antileishmanial activity (ic50 value) of ampb/m and b-ampb/m (empty micelles) against stationary promastigotes and amastigotes-like forms of the parasites was determined, and results were of 1.83 ± 0.4 and 22.1 ± 0.7 μm, respectively, for the promastigotes, and of 2.27 ± 0.5 and 33.98  ...201627427166
propolis reduces leishmania amazonensis-induced inflammation in the liver of balb/c mice.experimental models of mouse paw infection with l. amazonensis show an induction of a strong inflammatory response in the skin, and parasitic migration may occur to secondary organs with consequent tissue injury. there are few studies focusing on the resolution of damage in secondary organs caused by leishmania species-related cutaneous leishmaniasis. we investigated the propolis treatment effect on liver inflammation induced by leishmania amazonensis infection in the mouse paw. balb/c mice were ...201626711452
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 - corrigendum. 201626521984
antileishmanial activity and mechanism of action from a purified fraction of zingiber officinalis roscoe against leishmania amazonensis.in recent years, considerable attention has been given to identify new antileishmanial products derived from medicinal plants, although, to date, no new effective compound has been recently applied to treat leishmaniasis. in the present study, the antileishmanial activity of a water extract from zingiber officinalis roscoe (ginger) was investigated and a purified fraction, named f10, was identified as responsible by this biological activity. the chemical characterization performed for this fract ...201627013260
transient superdiffusion and long-range correlations in the motility patterns of trypanosomatid flagellate protozoa.we report on a diffusive analysis of the motion of flagellate protozoa species. these parasites are the etiological agents of neglected tropical diseases: leishmaniasis caused by leishmania amazonensis and leishmania braziliensis, african sleeping sickness caused by trypanosoma brucei, and chagas disease caused by trypanosoma cruzi. by tracking the positions of these parasites and evaluating the variance related to the radial positions, we find that their motions are characterized by a short-tim ...201627007779
in vitro and in vivo activities of 2,3-diarylsubstituted quinoxaline derivatives against leishmania amazonensis.leishmaniasis is endemic in 98 countries and territories worldwide. the therapies available for leishmaniasis have serious side effects, thus prompting the search for new therapies. the present study investigated the antileishmanial activities of 2,3-diarylsubstituted quinoxaline derivatives against leishmania amazonensis the antiproliferative activities of 6,7-dichloro-2,3-diphenylquinoxaline (lspn329) and 2,3-di-(4-methoxyphenyl)-quinoxaline (lspn331) against promastigotes and intracellular am ...201627001812
in vivo antileishmanial activity and chemical profile of polar extract from selaginella sellowii.the polar hydroethanolic extract from selaginella sellowii(ssphe) has been previously proven active on intracellular amastigotes (in vitro test) and now was tested on hamsters infected with leishmania (leishmania) amazonensis (in vivo test). ssphe suppressed a 100% of the parasite load in the infection site and draining lymph nodes at an intralesional dose of 50 mg/kg/day × 5, which was similar to the results observed in hamsters treated with n-methylglucamine antimonate (sb) (28 mg/kg/day × 5). ...201626910353
individual and combined antiparasitic effect of six plant metabolites against leishmania amazonensis and trypanosoma cruzi.six plant metabolites including isobavachalcone (1), 4-hydroxylonchocarpine (2), and (e)-1-(2,2-dimethyl-2h-chromen-6-yl)-3-(4-hydroxyphenyl)prop-2-en-1-one (3), 6,8-(di-3-methyl-but-2-enyl)eriodictyol (4), damnacanthal (5), and buesgenine (6) were evaluated for their leishmanicidal and trypanocidal activities against intracellular amastigotes of leishmania amazonensis and trypanosoma cruzi. compounds 2-4 and 6 displayed antileishmanial activity while 3 and 5 showed trypanocidal effect. the leis ...201626906638
oral efficacy of apigenin against cutaneous leishmaniasis: involvement of reactive oxygen species and autophagy as a mechanism of action.the treatment for leishmaniasis is currently based on pentavalent antimonials and amphotericin b; however, these drugs result in numerous adverse side effects. the lack of affordable therapy has necessitated the urgent development of new drugs that are efficacious, safe, and more accessible to patients. natural products are a major source for the discovery of new and selective molecules for neglected diseases. in this paper, we evaluated the effect of apigenin on leishmania amazonensis in vitro ...201626862901
efficacy of tamoxifen and miltefosine combined therapy for cutaneous leishmaniasis in the murine model of infection with leishmania amazonensis.the objective of this study was to characterize in vitro interactions and evaluate the antileishmanial activity of tamoxifen and miltefosine combinations.201626851606
an effective in vitro and in vivo antileishmanial activity and mechanism of action of 8-hydroxyquinoline against leishmania species causing visceral and tegumentary leishmaniasis.the development of new therapeutic strategies to treat leishmaniasis has become a priority. in the present study, the antileishmanial activity of 8-hydroxyquinoline (8-hqn) was investigated against in vitro promastigotes and in vivo intra-macrophage amastigotes of three leishmania species: leishmania amazonensis, leishmania infantum and leishmania braziliensis. studies were performed to establish the 50% leishmania inhibitory concentration (ic50) of 8-hqn, as well as its 50% cytotoxic concentrat ...201626827866
degranulating neutrophils promote leukotriene b4 production by infected macrophages to kill leishmania amazonensis parasites.neutrophils mediate early responses against pathogens, and they become activated during endothelial transmigration toward the inflammatory site. in the current study, human neutrophils were activated in vitro with immobilized extracellular matrix proteins, such as fibronectin (fn), collagen, and laminin. neutrophil activation by fn, but not other extracellular matrix proteins, induces the release of the granules' contents, measured as matrix metalloproteinase 9 and neutrophil elastase activity i ...201626800873
exploring the unbinding of leishmania (l.) amazonensis cpb derived-epitopes from h2 mhc class i proteins.new strategies to control leishmania disease demand an extensive knowledge about several aspects of infection including the understanding of its molecular events. in murine models, cysteine proteinase b from leishmania amazonensis promotes regulation of immune response, and fragments from its c-terminus extension (cyspep) can play a decisive role in the host-parasite interaction. the interaction between cyspep-derived peptides and major histocompatibility complex (mhc) proteins is a crucial fact ...201626798994
physalis angulata induces death of promastigotes and amastigotes of leishmania (leishmania) amazonensis via the generation of reactive oxygen species.leishmaniasis are a neglected group of emerging diseases that have been found in 98 countries and are caused by protozoa of the genus leishmania. the therapy for leishmaniasis causes several side effects and leads to drug-resistant strains. natural products from plants have exhibited activities against leishmania in various experimental models. physalis angulata is a widely used plant in popular medicine, and in the literature it has well-documented leishmanicidal activity. however, its mechanis ...201626765293
active sesquiterpene lactones against leishmania amazonensis and leishmania braziliensis.seventeen sesquiterpene lactones (sls) isolated from five species of the tribe vernonieae were evaluated for their in vitro activity against promastigotes of leishmania amazonensis and leishmania braziliensis. additionally, a quantitative structure activity relationship has been made, since all these natural compounds were found to have potent to mild antileishmanial properties. the most active compounds against l. braziliensis were 16 and 17 (ic50 values 1.45 and 1.34 μm, respectively), followe ...201626755152
antibacterial and leishmanicidal activity of bolivian propolis.the antimicrobial activity of bolivian propolis was assessed for the first time on a panel of bacteria and two endemic parasitic protozoa. ten samples of bolivian propolis and their main constituents were tested using the micro-broth dilution method against 11 bacterial pathogenic strains as well as against promastigotes of leishmania amazonensis and l. braziliensis using the xtt-based colorimetric method. the methanolic extracts showed antibacterial effect ranging from inactive (mics > 1000 μg  ...201626743801
a trypanosomatid iron transporter that regulates mitochondrial function is required for leishmania amazonensis virulence.iron, an essential co-factor of respiratory chain proteins, is critical for mitochondrial function and maintenance of its redox balance. we previously reported a role for iron uptake in differentiation of leishmania amazonensis into virulent amastigotes, by a mechanism that involves reactive oxygen species (ros) production and is independent of the classical ph and temperature cues. iron import into mitochondria was proposed to be essential for this process, but evidence supporting this hypothes ...201626741360
leishmanicidal, cytotoxicity and wound healing potential of arrabidaea chica verlot.leishmaniasis includes a wide complex of diseases that affect humans and other mammals, and can range from a mild cutaneous form to a severe visceral type. the safety of the standard treatment using pentavalent antimony is a concern due to its toxic effects. the search for alternative, effective and less toxic treatments has led to the testing of natural products. the present study aimed to evaluate the cytotoxic, leishmanicidal and healing potential of arrabidaea chica.201626729470
molecular characterization and functional analysis of pteridine reductase in wild-type and antimony-resistant leishmania lines.pteridine reductase (ptr1) is an nadph-dependent reductase that participates in the salvage of pteridines, which are essential to maintain growth of leishmania. in this study, we performed the molecular characterization of ptr1 gene in wild-type (wts) and sbiii-resistant (sbr) lines from leishmania guyanensis (lg), leishmania amazonensis (la), leishmania braziliensis (lb) and leishmania infantum (li), evaluating the chromosomal location, mrna levels of the ptr1 gene and ptr1 protein expression. ...201626689884
the integrated endoplasmic reticulum stress response in leishmania amazonensis macrophage infection: the role of x-box binding protein 1 transcription factor.endoplasmic reticulum (er) stress triggers the integrated er-stress response (iersr) that ensures cellular survival of er stress and represents a primordial form of innate immunity. we investigated the role of iersr duringleishmania amazonensisinfection. treatment of raw 264.7 infected macrophages with the er stress-inducing agent thapsigargin (tg; 1 μm) increasedl. amazonensisinfectivity in an ifn1-α receptor (ifnar)-dependent manner. in western blot assays, we showed thatl. amazonensisactivate ...201626678450
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 ...201627618071
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 ...201627612813
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 ...201627600041
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 ...201627597410
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 ...201627579922
antiprotozoal screening of the cuban native plant scutellaria havanensis.scutellaria havanensis jacq. (lamiaceae) is a native medicinal herb with a history of use in cuba.201627564587
inhibitory effects of zanthoxylum rhoifolium lam. (rutaceae) against the infection and infectivity of macrophages by leishmania amazonensis.zanthoxylum rhoifolium lam. (rutaceae) has been traditionally used in the treatment of microbial infections and parasitic diseases. in the present study, the antileishmanial effect induced by the ethanol extract of stem barks from z. rhoifolium (zr-eetoh) and its n-hexane fraction (zr-fhex) on infection and infectivity of murine macrophages by promastigote forms of leishmania amazonensis were investigated. in different set of experiments, macrophages or promastigotes were pretreated with zr-eeto ...201627556219
unveiling the role of the integrated endoplasmic reticulum stress response in leishmania infection - future perspectives.the integrated endoplasmic reticulum stress response (iersr) is an evolutionarily conserved adaptive mechanism that ensures endoplasmic reticulum (er) homeostasis and cellular survival in the presence of stress including nutrient deprivation, hypoxia, and imbalance of ca(+) homeostasis, toxins, and microbial infection. three transmembrane proteins regulate integrated signaling pathways that comprise the iersr, namely, ire-1 that activates xbp-1, the pancreatic er kinase (perk) that phosphorylate ...201627499755
in vivo near-infrared fluorescence imaging of leishmania amazonensis expressing infrared fluorescence protein (irfp) for real-time monitoring of cutaneous leishmaniasis in mice.the use of leishmania amazonensis-infected balb/c mice is an important model for the study of experimental cutaneous leishmaniasis. here we report the development of a non-invasive method to directly evaluate and measure parasite burden during the course of the infection, based on the near-infrared fluorescence detection of a recombinant l. amazonensis strain. so, we generated a l. amazonensis strain that stably expresses the near-infrared protein (irfp) gene and compared the maintenance of its ...201627498229
malaria-cutaneous leishmaniasis co-infection: influence on disease outcomes and immune response.malaria and cutaneous leishmaniasis (cl) are co-endemic throughout large regions in tropical countries and co-infection may impact the evolution of host-parasite interactions. in the present study, we evaluate malaria/leishmaniasis disease outcome, th1/th2 cytokine levels and the cd4 and cd8 t-cell profiles in a co-infection murine model (balb/c) of plasmodium yoelii 17xnl (py) and leishmania amazonensis (la) or l. braziliensis (lb). malaria parasitaemia was assessed through blood strains staine ...201627446022
stachytarpheta cayennensis extract inhibits promastigote and amastigote growth in leishmania amazonensis via parasite arginase inhibition.stachytarpheta cayennensis is a plant that is traditionally used to treat tegumentary leishmaniasis and as an anti-inflammatory agent.201627432217
an 8-hydroxyquinoline-containing polymeric micelle system is effective for the treatment of murine tegumentary leishmaniasis.the current treatment of leishmaniasis has been hampered due to the high toxicity of the available drugs and long duration protocols, which often lead to its abandonment. in the present study, a poloxamer 407-based delivery system was developed, and a molecule, 8-hydroxyquinoline (8-hqn), was incorporated with it, leading to an 8-hqn/micelle (8-hqn/m) composition. assays were performed to evaluate the in vitro antileishmanial activity of 8-hqn/m against leishmania amazonensis stationary promasti ...201627365053
calmodulin polymerase chain reaction-restriction fragment length polymorphism for leishmania identification and typing.a precise identification of leishmania species involved in human infections has epidemiological and clinical importance. herein, we describe a preliminary validation of a restriction fragment length polymorphism assay, based on the calmodulin intergenic spacer region, as a tool for detecting and typing leishmania species. after calmodulin amplification, the enzyme haeiii yielded a clear distinction between reference strains of leishmania mexicana, leishmania amazonensis, leishmania infantum, lei ...201627352873
antileishmanial activity and structure-activity relationship of triazolic compounds derived from the neolignans grandisin, veraguensin, and machilin g.sixteen 1,4-diaryl-1,2,3-triazole compounds 4-19 derived from the tetrahydrofuran neolignans veraguensin 1, grandisin 2, and machilin g 3 were tested against leishmania (leishmania) amazonensis intracellular amastigotes. triazole compounds 4-19 were synthetized via click chemistry strategy by 1,3-dipolar cycloaddition between terminal acetylenes and aryl azides containing methoxy and methylenedioxy groups as substituents. our results suggest that most derivatives were active against intracellula ...201627331807
morinda citrifolia linn. fruit (noni) juice induces an increase in no production and death of leishmania amazonensis amastigotes in peritoneal macrophages from balb/c.leishmaniasis is a complex disease that is considered a serious public health problem. due to the absence of an effective vaccine and debilitating chemotherapy better therapies are urgently needed. this situation has stimulated the search for alternative treatments such as the use of herbal medicines. several studies conducted with morinda citrifolia linn. have shown various biological activities such as antitumor, immunomodulation and antileishmanial activity, however its mechanisms of action a ...201627328771
synthesis and antileishmanial activity of c7- and c12-functionalized dehydroabietylamine derivatives.abietane-type diterpenoids, either naturally occurring or synthetic, have shown a wide range of pharmacological actions, including antiprotozoal properties. in this study, we report on the antileishmanial evaluation of a series of (+)-dehydroabietylamine derivatives functionalized at c7 and/or c12. thus, the activity in vitro against leishmania infantum, leishmania donovani, leishmania amazonensis and leishmania guyanensis, was studied. most of the benzamide derivatives showed activities at low ...201627318121
c5 induces different cell death pathways in promastigotes of leishmania amazonensis.leishmaniasis is a neglected infection that is caused by leishmania protozoa, affecting millions of people worldwide, mainly in tropical and subtropical regions. this disease has different clinical forms: cutaneous, mucocutaneous, and visceral. the drugs that are currently available for the treatment of this infection have limitations, such as high toxicity, long-term treatment, and leads to drug-resistant strains. numerous studies, in various experimental models, have sought to develop more eff ...201627317947
polarity-sensitive nanocarrier for oral delivery of sb(v) and treatment of cutaneous leishmaniasis.there is a great need for orally active drugs for the treatment of the neglected tropical disease leishmaniasis. amphiphilic sb(v) complexes, such as 1:3 sb-n-octanoyl-n-methylglucamide complex (sbl8), are promising drug candidates. it has been previously reported that sbl8 forms kinetically stabilized nanoassemblies in water and that this simple dispersion exhibits antileishmanial activity when given by oral route to a murine model of visceral leishmaniasis. the main objective of the present wo ...201627307731
synthesis and pharmacological evaluation of mono-arylimidamides as antileishmanial agents.arylimidamide (aia) compounds containing two pyridylimidamide terminal groups (bis-aias) possess outstanding in vitro antileishmanial activity, and the frontrunner bis-aia db766 (2,5-bis[2-(2-isopropoxy)-4-(2-pyridylimino)aminophenyl]furan) is active in visceral leishmaniasis models when given orally. eighteen compounds containing a single pyridylimidamide terminal group (mono-aias) were synthesized and evaluated for their antileishmanial potential. six of these compounds exhibited sub-micromola ...201627048943
hsp70 of leishmania amazonensis alters resistance to different stresses and mitochondrial bioenergetics.the 70 kda heat shock protein (hsp70) is a molecular chaperone that assists the parasite leishmania in returning to homeostasis after being subjected to different types of stress during its life cycle. in the present study, we evaluated the effects of hsp70 transfection of l. amazonensis promastigotes (ptex-hsp70) in terms of morphology, resistance, infectivity and mitochondrial bioenergetics. the ptex-hsp70 promastigotes showed no ultrastructural morphological changes compared to control parasi ...201627304024
leishmania amazonensis engages cd36 to drive parasitophorous vacuole maturation.leishmania amastigotes manipulate the activity of macrophages to favor their own success. however, very little is known about the role of innate recognition and signaling triggered by amastigotes in this host-parasite interaction. in this work we developed a new infection model in adult drosophila to take advantage of its superior genetic resources to identify novel host factors limiting leishmania amazonensis infection. the model is based on the capacity of macrophage-like cells, plasmatocytes, ...201627280707
comparative analysis of carbohydrate residues in the midgut of phlebotomines (diptera: psychodidae) from colony and field populations from amazon, brazil.leishmaniasis are worldwide diseases that occur in 98 countries including brazil, transmitted by the bite of female phlebotomines during blood feeding. in brazil it is known that some species of sand flies as lutzomyia longipalpis sensun latum (vector of leishmania infantum chagasi), lutzomyia flaviscutellata (vector of leishmania (leishmania) amazonensis) and lutzomyia antunesi [suspected vector of leishmania (viannia) lindenbergi] are incriminated of transmitting the parasite leishmania for th ...201627264642
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 ...201627776144
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 ...201627876366
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 ...201627480800
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 ...201627795620
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 ...201627743972
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 ...201627725158
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, ...201627834831
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 ...201627825341
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 ...201627812653
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.201627812652
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 ...201627925065
efficacy of intranasal laag vaccine against leishmania amazonensis infection in partially resistant c57bl/6 mice.we have previously demonstrated that intranasal vaccination of highly susceptible balb/c mice with whole leishmania amazonensis antigens (laag) leads to protection against murine cutaneous leishmaniasis. here, we evaluate the response of partially resistant c57bl/6 mice to vaccination as a more representative experimental model of human cutaneous leishmaniasis.201627716449
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 ...201627938439
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 ...201627876209
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 ...201627866341
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 ...201627860021
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 ...201627973453
functional complementation of leishmania (leishmania) amazonensis ap endonuclease gene (lamap) in escherichia coli mutant strains challenged with dna damage agents.during its life cycle leishmania spp. face several stress conditions that can cause dna damages. base excision repair plays an important role in dna maintenance and it is one of the most conserved mechanisms in all living organisms. dna repair in trypanosomatids has been reported only for old world leishmania species. here the ap endonuclease from leishmania (l.) amazonensis was cloned, expressed in escherichia coli mutants defective on the dna repair machinery, that were submitted to different ...201627223868
biological activities of croton palanostigma klotzsch.different species of croton are used in traditional amazonian medicine. among the popular uses are treatment of bacterial diseases, poorly healing wounds and fevers.201627041867
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 ...201628009804
cutaneous leishmaniasis vaccination: a matter of quality.there have been exhaustive efforts to develop an efficient vaccine against leishmaniasis. factors like host and parasite genetic characteristics, virulence, epidemiological scenarios, and, mainly, diverse immune responses triggered by leishmania species make the achievement of this aim a complex task. it is already clear that the induction of a th1, pro-inflammatory response, is important in the protection against leishmania infection. however, many questions must still be answered to fully unde ...201627148270
lipophosphoglycans from leishmania amazonensis strains display immunomodulatory properties via tlr4 and do not affect sand fly infection.the immunomodulatory properties of lipophosphoglycans (lpg) from new world species of leishmania have been assessed in leishmania infantum and leishmania braziliensis, the causative agents of visceral and cutaneous leishmaniasis, respectively. this glycoconjugate is highly polymorphic among species with variation in sugars that branch off the conserved gal(β1,4)man(α1)-po4 backbone of repeat units. here, the immunomodulatory activity of lpgs from leishmania amazonensis, the causative agent of di ...201627508930
trypanosoma cruzi differentiates and multiplies within chimeric parasitophorous vacuoles in macrophages coinfected with leishmania amazonensis.the trypanosomatids leishmania amazonensis and trypanosoma cruzi are excellent models for the study of the cell biology of intracellular protozoan infections. after their uptake by mammalian cells, the parasitic protozoan flagellates l. amazonensis and t. cruzi lodge within acidified parasitophorous vacuoles (pvs). however, whereas l. amazonensis develops in spacious, phagolysosome-like pvs that may enclose numerous parasites, t. cruzi is transiently hosted within smaller vacuoles from which it ...201626975994
antileishmanial activity of the essential oil from tetradenia riparia obtained in different seasons.the herbaceous shrub tetradenia riparia has been traditionally used to treat inflammatory and infectious diseases. recently, a study showed that t. riparia essential oil (treo) obtained in summer has antileishmanial effects, although these results could be influenced by seasonal variation. this study evaluated the activity of the treo obtained in different seasons against leishmania (leishmania) amazonensis, in vitro and in vivo. the compounds in the treo were analysed by gas chromatography-mass ...201526602873
expression of calpain-like proteins and effects of calpain inhibitors on the growth rate of angomonas deanei wild type and aposymbiotic strains.angomonas deanei is a trypanosomatid parasite of insects that has a bacterial endosymbiont, which supplies amino acids and other nutrients to its host. bacterium loss induced by antibiotic treatment of the protozoan leads to an aposymbiotic strain with increased need for amino acids and results in increased production of extracellular peptidases. in this work, a more detailed examination of a. deanei was conducted to determine the effects of endosymbiont loss on the host calpain-like proteins (c ...201526415499
nucleosides present on phlebotomine saliva induce immunossuppression and promote the infection establishment.sand fly saliva plays a crucial role in establishing leishmania infection. we identified adenosine (ado) and adenosine monophosphate (amp) as active pharmacologic compounds present in phlebotomus papatasi saliva that inhibit dendritic cell (dc) functions through a pge2/il 10-dependent mechanism.201525849562
leishmania amazonensis dna in wild females of lutzomyia cruzi (diptera: psychodidae) in the state of mato grosso do sul, brazil.studies on natural infection by leishmania spp of sandflies collected in endemic and nonendemic areas can provide important information on the distribution and intensity of the transmission of these parasites. this study sought to investigate the natural infection by leishmaniain wild female sandflies. the specimens were caught in the city of corumbá, state of mato grosso do sul (brazil) between october 2012-march 2014, and dissected to investigate flagellates and/or submitted to molecular analy ...201526602870
ecological niche modelling predicts southward expansion of lutzomyia (nyssomyia) flaviscutellata (diptera: psychodidae: phlebotominae), vector of leishmania (leishmania) amazonensis in south america, under climate change.vector borne diseases are susceptible to climate change because distributions and densities of many vectors are climate driven. the amazon region is endemic for cutaneous leishmaniasis and is predicted to be severely impacted by climate change. recent records suggest that the distributions of lutzomyia (nyssomyia) flaviscutellata and the parasite it transmits, leishmania (leishmania) amazonensis, are expanding southward, possibly due to climate change, and sometimes associated with new human inf ...201526619186
natural infection of phlebotomines (diptera: psychodidae) by leishmania (leishmania) amazonensis in an area of ecotourism in central-western brazil.bonito municipality, known as an area of ecoturism, in mato grosso do sul state, brazil, is also a focus of visceral and cutaneous leishmaniases, with cases registered in both human and canine populations. this study sought to investigate natural infection by flagellate forms of leishmania in phlebotomines of the urban area of bonito.201526435708
a novel molecular test to diagnose canine visceral leishmaniasis at the point of care.dogs are the principal reservoir hosts of zoonotic visceral leishmaniasis (vl) but current serological methods are not sensitive enough to detect all subclinically infected animals, which is crucial to vl control programs. polymerase chain reaction (pcr) methods have greater sensitivity but require expensive equipment and trained personnel, impairing its implementation in endemic areas. we developed a diagnostic test that uses isothermal recombinase polymerase amplification (rpa) to detect leish ...201526240156
bioactive endophytic fungi isolated from caesalpinia echinata lam. (brazilwood) and identification of beauvericin as a trypanocidal metabolite from fusarium sp.aiming to identify new sources of bioactive secondary metabolites, we isolated 82 endophytic fungi from stems and barks of the native brazilian tree caesalpinia echinata lam. (fabaceae). we tested their ethyl acetate extracts in several in vitro assays. the organic extracts from three isolates showed antibacterial activity against staphylococcus aureus and escherichia coli [minimal inhibitory concentration (mic) 32-64 μg/ml]. one isolate inhibited the growth of salmonella typhimurium (mic 64 μg/ ...201525742265
enhancement of experimental cutaneous leishmaniasis by leishmania extract: identification of a disease-associated antibody specificity.both leishmania braziliensis and leishmania amazonensis induce cutaneous disease when injected in the skin of balb/c mice. however, l. amazonensis may also visceralize in that strain of mice, infecting mainly the liver and spleen. in addition, whereas balb/c mice die with a progressive cutaneous disease when infected by l. amazonensis, the infection by l. braziliensis is spontaneously cured. in a previous work, we have found that intravenous injections of l. amazonensis amastigote extract (lae) ...201525971623
anti-infective assessment of senecio smithioides (asteraceae) and isolation of 9-oxoeuryopsin, a furanoeremophilane-type sesquiterpene with antiplasmodial activity.the search for anti-infective activity in the antipyretic plant senecio smithioides was conducted. petroleum ether (pe), dichloromethane (ch2cl2), ethyl acetate (etoac) and hydroethanolic (96% etoh) extracts, and compounds 9-oxoeuryopsin (1), epoxydecompostin (2) and senecionine (3) were obtained from the aerial parts. all extracts and 1 were tested against chloroquine-resistant strain of plasmodium falciparum (ref. chloroquine), trypanosoma cruzi (ref. nifurtimox), leishmania braziliensis, leis ...201526606687
bioactive endophytic fungi isolated from caesalpinia echinata lam. (brazilwood) and identification of beauvericin as a trypanocidal metabolite from fusarium sp.aiming to identify new sources of bioactive secondary metabolites, we isolated 82 endophytic fungi from stems and barks of the native brazilian tree caesalpinia echinata lam. (fabaceae). we tested their ethyl acetate extracts in several in vitro assays. the organic extracts from three isolates showed antibacterial activity against staphylococcus aureus and escherichia coli [minimal inhibitory concentration (mic) 32-64 μg/ml]. one isolate inhibited the growth of salmonella typhimurium (mic 64 μg/ ...201525606862
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 ...201526674781
classical ros-dependent and early/rapid ros-independent release of neutrophil extracellular traps triggered by leishmania parasites.neutrophil extracellular traps (nets) extruded from neutrophils upon activation are composed of chromatin associated with cytosolic and granular proteins, which ensnare and kill microorganisms. this microbicidal mechanism named classical netosis has been shown to dependent on reactive oxygen species (ros) generation by nadph oxidase and also chromatin decondensation dependent upon the enzymes (pad4), neutrophil elastase (ne) and myeloperoxidase (mpo). net release also occurs through an early/rap ...201526673780
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