| serodiagnosis of visceral and cutaneous leishmaniasis in human and canine populations living in indigenous reserves in the brazilian amazon region. | leishmaniasis is endemic to the northern, northeastern, central-western, and southeastern regions of brazil. we aimed to assess the epidemiological situation of leishmaniasis in humans and dogs in indigenous villages located in the states of mato grosso and tocantins using a serological survey conducted in may 2011. | 2017 | 28327803 |
| antileishmanial activity of handroanthus serratifolius (vahl) s. grose (bignoniaceae). | this study aimed to evaluate the leishmanicidal activity of ethanol extract, fractions, and isolated substance from handroanthus serratifolius against leishmania amazonensis. furthermore, this activity was related to cytotoxicity, and the selectivity index was determined. the ethanol extract was obtained by maceration of the stem powder, and the extract was subjected to fractionation on chromatographic column. the lapachol was obtained by acid base extraction followed by purification in chromato ... | 2017 | 28286535 |
| a chimera containing cd4+ and cd8+ t-cell epitopes of the leishmania donovani nucleoside hydrolase (nh36) optimizes cross-protection against leishmania amazonesis infection. | the leishmania donovani nucleoside hydrolase (nh36) and nh a34480 of leishmania amazonensis share 93% of sequence identity. in mice, the nh36 induced protection against visceral leishmaniasis is mediated by a cd4+ t cell response against its c-terminal domain (f3). besides this cd4+ th1 response, prevention and cure of l. amazonensis infection require also additional cd8+ and regulatory t-cell responses to the nh36 n-terminal (f1 domain). we investigated if mice vaccination with f1 and f3 domain ... | 2017 | 28280494 |
| leishmania (leishmania) amazonensis induces macrophage mir-294 and mir-721 expression and modulates infection by targeting nos2 and l-arginine metabolism. | leishmania (leishmania) amazonensis is an intracellular protozoan parasite responsible for the cutaneous leishmaniasis. the parasite replicates inside mammalian macrophage to establish infection. host-pathogen interactions result in microrna-mediated post-transcriptional regulation of host genes involved in inflammatory immune response. we analyzed macrophage mirna profiles during l. (l.) amazonensis infection. the regulation of macrophage mirna expression by the parasite correlates with/depends ... | 2017 | 28276497 |
| topical tamoxifen in the therapy of cutaneous leishmaniasis. | the aims of the present work were to test the effect of tamoxifen administered topically and the therapeutic efficacy of tamoxifen and pentavalent antimonial combinations in an experimental model of cutaneous leishmaniasis. balb/c mice infected with a luciferase expressing line of leishmania amazonensis were treated with topical tamoxifen in two different formulations (ethanol or oil-free cream) as monotherapy or in co-administration with pentavalent antimonial. treatment efficacy was evaluated ... | 2017 | 28274283 |
| induction of early autophagic process on leishmania amazonensis by synergistic effect of miltefosine and innovative semi-synthetic thiosemicarbazone. | drug combination therapy is a current trend to treat complex diseases. many benefits are expected from this strategy, such as cytotoxicity decrease, retardation of resistant strains development, and activity increment. this study evaluated in vitro combination between an innovative thiosemicarbazone molecule - bzts with miltefosine, a drug already consolidated in the leishmaniasis treatment, against leishmania amazonensis. cytotoxicity effects were also evaluated on macrophages and erythrocytes. ... | 2017 | 28270805 |
| cutaneous leishmaniasis in french guiana: revising epidemiology with pcr-rflp. | the development of polymerase chain reaction-restriction fragment length polymorphism (pcr-rflp) technique for species identification among patients presenting leishmaniasis allowed to better determine the main circulating species in french guiana. | 2017 | 28265182 |
| chemical composition, antiprotozoal and cytotoxic activities of indole alkaloids and benzofuran neolignan of aristolochia cordigera. | this is a comparative study on the intraspecific chemical variability of aristolochia cordigera species, collected in two different regions of brazil, biome cerrado (semiarid) and biome amazônia (coastal). the use of gc-ms and statistical methods led to the identification of 56 compounds. a higher percentage of palmitone and germacrene-d in the hexanes extracts of the leaves of plants from these respective biomes was observed. phytochemical studies on the extracts led to the isolation and identi ... | 2017 | 28264205 |
| differences in the detection of brdu/edu incorporation assays alter the calculation for g1, s, and g2 phases of the cell cycle in trypanosomatids. | trypanosomatids are the etiologic agents of various infectious diseases in humans. they diverged early during eukaryotic evolution and have attracted attention as peculiar models for evolutionary and comparative studies. here, we show a meticulous study comparing the incorporation and detection of the thymidine analogs brdu and edu in leishmania amazonensis, trypanosoma brucei, and trypanosoma cruzi to monitor their dna replication. we used brdu- and edu-incorporated parasites with the respectiv ... | 2017 | 28258618 |
| metacaspase-binding peptide inhibits heat shock-induced death in leishmania (l.) amazonensis. | leishmania (leishmania) amazonensis is an important agent of cutaneous leishmaniasis in brazil. this parasite faces cell death in some situations during transmission to the vertebrate host, and this process seems to be dependent on the activity of metacaspase (mca), an enzyme bearing trypsin-like activity present in protozoans, plants and fungi. in fact, the association between mca expression and cell death induced by different stimuli has been demonstrated for several leishmania species. regula ... | 2017 | 28252649 |
| cytokines and microbicidal molecules regulated by il-32 in thp-1-derived human macrophages infected with new world leishmania species. | interleukin-32 (il-32) is expressed in lesions of patients with american tegumentary leishmaniasis (atl), but its precise role in the disease remains unknown. | 2017 | 28241012 |
| anti-leishmania activity of essential oil of myracrodruon urundeuva (engl.) fr. all.: composition, cytotoxity and possible mechanisms of action. | myracrodruon urundeuva (engl.) fr. all., commonly known as "aroeira-do-sertão", is a medicinal plant from anacardiaceae family. in this study, the chemical composition of m. urundeuva essential oil (mueo) was evaluated by gas chromatography-mass spectrometry (gc-ms), as well as its anti-leishmania potential, cytotoxicity, and macrophage activation capability as possible antiprotozoal mechanism of action were assessed. fourteen compounds were identified, which constituted 94.87% of total oil comp ... | 2017 | 28189487 |
| n-acetyl-cysteine inhibits liver oxidative stress markers in balb/c mice infected with leishmania amazonensis. | leishmaniasis is a parasitosis caused by several species of the genus leishmania. these parasites present high resistance against oxidative stress generated by inflammatory cells. | 2017 | 28177049 |
| leishmania in synanthropic rodents (rattus rattus): new evidence for the urbanization of leishmania (leishmania) amazonensis. | this study aimed to detect parasites from leishmania genus, to determine the prevalence of anti-leishmania spp. antibodies, to identify circulating species of the parasite, and to determine epidemiological variables associated with infection in rats caught in urban area of londrina, paraná, brazil. animal capture was carried out from may to december 2006, serological and molecular methods were performed. dna was extracted from total blood, and nested-pcr, targeting ssu rrna from leishmania genus ... | 2017 | 28177041 |
| leishmania amazonensis and leishmania chagasi: in vitro leishmanicide activity of virola surinamensis (rol.) warb. | virola species have been used in traditional medicine as healing in skin infections. from v. surinanensis oil were isolated several sesquiterpene as the nerolidol which showed activity against species of leishmania. the current study aimed to evaluate the leishmanicide activity and toxicity of extracts, fractions and surinamesin obtained from leaves of virola surinamensis. hexane, ethyl acetate, and methanol extracts were obtained from powder of dry leaves of v. surinamensis. the hexane and ethy ... | 2017 | 28174103 |
| in vitro and in vivo antimalarial potential of oleoresin obtained from copaifera reticulata ducke (fabaceae) in the brazilian amazon rainforest. | in view of the wide variety of the flora of the amazon region, many plants have been studied in the search for new antimalarial agents. copaifera reticulata is a tree distributed throughout the amazon region which contains an oleoresin rich in sesquiterpenes and diterpenes with β-caryophyllene as the major compound. the oleoresin has demonstrated antiparasitic activity against leishmania amazonensis. because of this previously reported activity, this oleoresin would be expected to also have anti ... | 2017 | 28160850 |
| design and synthesis of a new series of 3,5-disubstituted isoxazoles active against trypanosoma cruzi and leishmania amazonensis. | chagas disease and leishmaniasis are neglected tropical diseases (ntds) endemic in developing countries. although there are drugs available for their treatment, efforts on finding new efficacious therapies are continuous. the natural lignans grandisin (1) and veraguensin (2) show activity against trypomastigote t. cruzi and their scaffold has been used as inspiration to design new derivatives with improved potency and chemical properties. we describe here the planning and microwave-irradiated sy ... | 2017 | 28152426 |
| effect of clinically approved hdac inhibitors on plasmodium, leishmania and schistosoma parasite growth. | malaria, schistosomiasis and leishmaniases are among the most prevalent tropical parasitic diseases and each requires new innovative treatments. targeting essential parasite pathways, such as those that regulate gene expression and cell cycle progression, is a key strategy for discovering new drug leads. in this study, four clinically approved anti-cancer drugs (vorinostat, belinostat, panobinostat and romidepsin) that target histone/lysine deacetylase enzymes were examined for in vitro activity ... | 2017 | 28107750 |
| perifosine mechanisms of action in leishmania species. | here the mechanism by which perifosine induced cell death in leishmania donovani and leishmania amazonensis is described. the drug reduced leishmania mitochondrial membrane potential and decreased cellular atp levels while increasing phosphatidylserine externalization. perifosine did not increase membrane permeabilization. we also found that the drug inhibited the phosphorylation of akt in the parasites. these results highlight the potential use of perifosine as an alternative to miltefosine aga ... | 2017 | 28096161 |
| high dilutions of antimony modulate cytokines production and macrophage - leishmania (l.) amazonensis interaction in vitro. | in previous results mice treated with high dilutions of antimony presented reduction of monocyte migration to the site of infection with increase in b lymphocytes population in the local lymph node. | 2017 | 28092793 |
| vector competence of lutzomyia cruzi naturally demonstrated for leishmania infantum and suspected for leishmania amazonensis. | corumbá city is one of the oldest visceral leishmaniasis-endemic foci in the state of mato grosso do sul, brazil, where the transmission of leishmania infantum has been attributed to lutzomyia cruzi aiming at investigating the parameters of the vectorial capacity of lu. cruzi for l. infantum, a project was undertaken in this city. among these parameters, vector competence was investigated and the results obtained are reported herein. of the 12 hamsters exposed to feed wild-caught female sandflie ... | 2017 | 28077746 |
| phenotypic diversity and selection maintain leishmania amazonensis infectivity in balb/c mouse model. | leishmania are protozoan parasites that show remarkable diversity, as revealed by the various clinical forms of leishmaniasis, which can range from mild skin lesions to severe metastatic cutaneous/mucosal lesions. the exact nature and extent of leishmania phenotypic diversity in establishing infection is not fully understood. in order to try to understand some aspects of this diversity, we subcutaneously infected balb/c mice with first and second generation subclones of a l. amazonensis strain i ... | 2017 | 28076468 |
| development and evaluation of zinc phthalocyanine nanoemulsions for use in photodynamic therapy for leishmania spp. | photodynamic therapy (pdt) combines light with photosensitizers (ps) for production of reactive oxygen species (ros) that can kill infectious microorganisms such as bacteria, fungi and protozoa. the application of nanotechnology has enabled the advancement of pdt because many ps are insoluble in water, necessitating a nanocarrier as a physiologically acceptable carrier. nanoemulsions are efficient nanocarriers for solubilizing liposoluble drugs, like the ps, in water. cutaneous (cl) and mucocuta ... | 2017 | 28071592 |
| in vitro antiprotozoal activity of (s)-cis-verbenol against leishmania spp. and trypanosoma cruzi. | (s)-cis-verbenol, a monoterpene frequently found as a component of essential oils, was assayed against leishmania amazonensis, leishmania infantum, leishmania brasiliensis and against two strains of trypanosoma cruzi. the cytotoxicity of the compound was also assayed against human fibroblast cells using a colorimetric method. benznidazole was used as reference drug against t. cruzi and amphotericin b was used against leishmania spp. the compound showed good activity against the trypanosomes, bei ... | 2017 | 28062234 |
| a recombinant fusion protein displaying murine and human mhc class i- and ii-specific epitopes protects against leishmania amazonensis infection. | tegumentary leishmaniasis (tl) constitutes a major public health problem with significant morbidity worldwide. synthetic peptide-based vaccines are attractive candidates to protect against leishmaniasis, since t cell-specific epitopes can be delivery to antigen-presenting cells, leading to the generation of a th1 cell-mediated immunity. in this context, the present study aims to evaluate the immunogenicity and protective efficacy of a vaccine composed of major histocompatibility complex class i ... | 2017 | 28049560 |
| oligopeptidase b and b2: comparative modelling and virtual screening as searching tools for new antileishmanial compounds. | leishmaniasis are diseases caused by parasites of the genus leishmania and transmitted to humans by the bite of infected insects of the subfamily phlebotominae. current drug therapy shows high toxicity and severe adverse effects. recently, two oligopeptidases (opbs) were identified in leishmania amazonensis, namely oligopeptidase b (opb) and oligopeptidase b2 (opb2). these opbs could be ideal targets, since both enzymes are expressed in all parasite lifecycle and were not identified in human. th ... | 2017 | 28031079 |
| antileishmanial activity of verbascoside: selective arginase inhibition of intracellular amastigotes of leishmania (leishmania) amazonensis with resistance induced by lps plus ifn-γ. | verbascoside is the main component of the traditional medicinal plants that were used against protozoa parasites that cause malaria and leishmaniasis. previously, we have described verbascoside inhibition of leishmania amazonensis arginase as well as its antileishmanial action against extracellular promastigotes. in this study, we have assessed arginase parasite inhibition in intracellular amastigotes. in addition, we verified whether verbascoside can influence the host defense against the paras ... | 2017 | 28017773 |
| leishmanicidal activity of the alkaloid-rich fraction from guatteria latifolia. | leishmaniasis is caused by protozoan parasites belonging to the genus leishmania and includes cutaneous, mucocutaneous and visceral clinical forms. the drugs currently available for leishmaniasis treatment are pentavalent antimonials, amphotericin b and miltefosine, which present high toxicity, elevated cost and development of parasite resistance. the natural products constitute an important source of substances with leishmanicidal potential. here we evaluated in vitro the anti-leishmania amazon ... | 2017 | 28011169 |
| evaluation of chemical composition and antileishmanial and antituberculosis activities of essential oils of piper species. | essential oils from fresh piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (gc-ms), and a total of 68 components were identified. principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. the composition of the essential oil of piper mosenii was described for the first time. the cytotoxicity of the essential oils was evaluated in peri ... | 2016 | 28009804 |
| nanoscaled hydrated antimony (v) oxide as a new approach to first-line antileishmanial drugs. | coordination compounds of pentavalent antimony have been, and remain, the first-line drugs in leishmaniasis treatment for >70 years. molecular forms of sb (v) complexes are commercialized as sodium stibogluconate (pentostam(®)) and meglumine antimoniate (ma) (glucantime(®)). ever-increasing drug resistance in the parasites limits the use of antimonials, due to the low drug concentrations being administered against high parasitic counts. sb(5+) toxicity provokes severe side effects during treatme ... | 2017 | 28008252 |
| evaluation of chemical composition and antileishmanial and antituberculosis activities of essential oils of piper species. | essential oils from fresh piperaceae leaves were obtained by hydrodistillation and analyzed by gas chromatography mass spectrometry (gc-ms), and a total of 68 components were identified. principal components analysis results showed a chemical variability between species, with sesquiterpene compounds predominating in the majority of species analyzed. the composition of the essential oil of piper mosenii was described for the first time. the cytotoxicity of the essential oils was evaluated in peri ... | 2016 | 27973453 |
| the antileishmanial activity of xanthohumol is mediated by mitochondrial inhibition. | xanthohumol (xan) is a natural constituent of human nutrition. little is known about its actions on leishmanial parasites and their mitochondria as putative target. therefore, we determined the antileishmanial activity of xan and resveratrol (res, as alternative compound with antileishmanial activity) with respect to mitochondria in leishmania amazonensis promastigotes/amastigotes (lap/laa) in comparison with their activity in peritoneal macrophages from mouse (pmm) and macrophage cell line j774 ... | 2016 | 27938439 |
| use of recombinant antigens for sensitive serodiagnosis of american tegumentary leishmaniasis caused by different leishmania species. | american tegumentary leishmaniasis (atl) (also known as cutaneous leishmaniasis [cl]) is caused by various species of protozoa of the genus leishmania the diagnosis is achieved on a clinical, epidemiological, and pathological basis, supported by positive parasitological exams and demonstration of leishmanin delayed-type hypersensitivity. serological assays are not routinely used in the diagnosis because many are considered to have low sensitivity and the particular leishmania species causing the ... | 2017 | 27927927 |
| natural canine infection by leishmania infantum and leishmania amazonensis and their implications for disease control. | leishmaniasis is a major public health problem worldwide. because leishmania can adapt to new hosts or vectors, knowledge concerning the current etiological agent in dogs is important in endemic areas. this study aimed to identify the leishmania species detected in 103 samples of peripheral blood from dogs that were naturally infected with these protozoa. the diagnosis of leishmaniasis was determined through parasitological examination, the indirect enzyme-linked immunosorbent assay (elisa) and ... | 2016 | 27925065 |
| antiprotozoal and antioxidant alkaloids from alternanthera littoralis. | five alkaloids, in addition to hydroxytyrosol and uridine, were isolated from aerial parts of alternanthera littoralis p. beauv. among the isolated compounds, alternamide a was an unusual tricyclic alkaloid with a bridged benzoazepine core. all isolated alkaloids have a catechol moiety, indicating a possible common biosynthetic route. their structures were established by 1d and 2d nmr spectroscopy in combination with extensive tandem ms experiments by collisional induced dissociation (cid). the ... | 2017 | 27889243 |
| leishmania amazonensis infection induces behavioral alterations and modulates cytokine and neurotrophin production in the murine cerebral cortex. | neurological symptoms have been associated with leishmania infection, however little is known about how the nervous system is affected in leishmaniasis. this work aimed to analyze parasitic load, production of cytokines/neurotrophins in the prefrontal cortex and behavioral changes in balb/c mice infected with leishmania amazonensis. at 2 and 4months post-infection, infected mice showed a decrease in ifn-γ, il-1, il-6, il-4, il-10 cytokines and bdnf and ngf neurotrophins in prefrontal cortex asso ... | 2016 | 27876366 |
| synthesis and biological evaluation against mycobacterium tuberculosis and leishmania amazonensis of a series of diaminated terpenoids. | we report the synthesis of a series of diaminated terpenoids containing, as side-chain of the diamine core, the "head-to-tail" prenyl derivatives, with amino amino spacers of variable length. in vitro biological activity of these compounds was evaluated against mycobacterium tuberculosis and leishmania amazonensis, and the structure-activity relationships are discussed. different biological results were observed depending on the terpenic side-chain length. the best results were obtained for tran ... | 2016 | 27876209 |
| the role of the p2x7 receptor in murine cutaneous leishmaniasis: aspects of inflammation and parasite control. | leishmania amazonensis is the etiological agent of diffuse cutaneous leishmaniasis. the immunopathology of leishmaniasis caused by l. amazonensis infection is dependent on the pathogenic role of effector cd4(+) t cells. purinergic signalling has been implicated in resistance to infection by different intracellular parasites. in this study, we evaluated the role of the p2x7 receptor in modulating the immune response and susceptibility to infection by l. amazonensis. we found that p2x7-deficient m ... | 2016 | 27866341 |
| detection of leishmania amazonensis and leishmania braziliensis in culicoides (diptera, ceratopogonidae) in an endemic area of cutaneous leishmaniasis in the brazilian amazonia. | biting midges in the genus culicoides act as vectors of arboviruses throughout the world and as vectors of filariasis in latin america, the caribbean, and parts of africa. although culicoides spp. are currently not considered to be vectors of leishmania protozoa, the high abundance of biting midges in areas with active cutaneous leishmaniasis transmission points to the possibility of culicoides infection by these pathogens. we used pcr to test captured culicoides species for natural infection wi ... | 2016 | 27860021 |
| consequences of acute oxidative stress in leishmania amazonensis: from telomere shortening to the selection of the fittest parasites. | leishmaniasis is a spectrum of diseases caused by parasites of the genus leishmania that affects millions of people around the world. during infection, the parasites use different strategies to survive the host's defenses, including overcoming exposure to reactive oxidant species (ros), responsible for causing damage to lipids, proteins and dna. this damage especially affects telomeres, which frequently results in genome instability, senescence and cell death. telomeres are the physical ends of ... | 2017 | 27836509 |
| synthesis and in vitro anti leishmania amazonensis biological screening of morita-baylis-hillman adducts prepared from eugenol, thymol and carvacrol. | leishmaniasis represents a series of severe neglected tropical diseases caused by protozoa of the genus leishmania and is widely distributed around the world. here, we present the syntheses of morita-baylis-hillman adducts (mbhas) prepared from eugenol, thymol and carvacrol, and their bioevaluation against promastigotes of leishmania amazonensis. the new mbhas are prepared in two steps from essential oils in moderate to good yields and present ic50 values in the range of 22.30-4.71 μm. moreover, ... | 2016 | 27834831 |
| essential oils: in vitro activity against leishmania amazonensis, cytotoxicity and chemical composition. | the current chemotherapy for cutaneous leishmaniosis (cl) has a series of drug limitations such as toxic side effects, long duration, high costs and drug resistance, which requires the development of new drugs or effective alternatives to the cl treatment. essential oils (eos) are complex mixtures of secondary metabolites from various plants. it has been shown that several eos, or their constituents, have inhibitory activity against protozoa. thus, this study aims to evaluate the biological acti ... | 2016 | 27825341 |
| evaluation of the antiplasmodial and leishmanicidal potential of myrciaria dubia (myrtaceae) extract. | malaria and leishmaniasis are prevalent in tropical regions, which have environmental characteristics that are highly favorable to protozoa and vectors of these diseases; the transmission of these infections in sub-tropical regions, although recognized, represents only a small fraction of cases. plants are constantly being used in the search for and acquisition of new drugs, and many compounds derived from them have been used to combat various diseases. in this study, we evaluated the action of ... | 2016 | 27812653 |
| screening of the in vitro antileishmanial activities of compounds and secondary metabolites isolated from maytenus guianensis klotzsch ex reissek (celastraceae) chichuá amazon. | maytenus guianensis is a member of the celastraceae family that is used in traditional medicine, particularly for its anti-parasitic and anti-cancer effects. to explore the ethnopharmacological potential of this plant, the present study was designed to screen the in vitro antileishmanial activities of extracts and compounds isolated from m. guianensis. | 2016 | 27812652 |
| anti-leishmania amazonensis activity of serjania lethalis a. st.-hil. | extracts of serjania lethalis a. st.-hil leaves and stems were tested in order to identify potential agents against leishmania amazonensis. the hexane fraction (hf) and dichloromethane subfractions (ddf and mdf) showed leishmanicidal effect. the anti-promastigote ic50 values were 10.29 (hf), 11.41 (ddf) and 28.33μg⁄ml (mdf); whereas those against amastigote were 7.2 (hf), 8.1 (ddf) and 6.5μg⁄ml (mdf). among the fractions and subfractions assayed, only hf altered the cell cycle of the parasite, i ... | 2017 | 27793725 |
| in vitro assessment of plants growing in cuba belonging to solanaceae family against leishmania amazonensis. | in this study, an in vitro antileishmanial assessment of plant extracts from 12 genera and 46 species growing in cuba belonging to solanaceae family was performed. a total of 226 extracts were screened against promastigotes of leishmania amazonensis, and cytotoxicity of active extracts [median inhibitory concentration (ic50 ) promastigotes <100 µg/ml] was determined on peritoneal macrophage from balb/c mice. extracts that showed selective index >5 were then assayed against intracellular amastigo ... | 2016 | 27480800 |
| antileishmanial activity and inducible nitric oxide synthase activation by runo complex. | parasites of the genus leishmania are capable of inhibiting effector functions of macrophages. these parasites have developed the adaptive ability to escape host defenses; for example, they inactivate the nf-κb complex and suppress inos expression in infected macrophages, which are responsible for the production of the major antileishmanial substance nitric oxide (no), favoring then its replication and successful infection. metal complexes with no have been studied as potential compounds for the ... | 2016 | 27795620 |
| aminoquinoline compounds: effect of 7-chloro-4-quinolinylhydrazone derivatives against leishmania amazonensis. | in this study, we have investigated the antileishmanial activity of ten 7-chloro-4-quinolinylhydrazone derivatives. among the compounds tested, compounds 2a and 2j presented activity against promastigotes (ic50 values of 52.5 and 21.1 μm, respectively) and compounds 2a and 2c were active against intracellular amastigotes (ic50 of 8.1 and 15.6 μm, respectively) of leishmania amazonensis. the majority of compounds did not show toxicity against murine macrophages. compound 2a exhibited low cytotoxi ... | 2016 | 27743972 |
| optimization of extraction method and evaluation of antileishmanial activity of oil and nanoemulsions of pterodon pubescens benth. fruit extracts. | currently, leishmaniasis is difficult to manage owing to the limited choice and high toxicity of available drugs, and emergence of drug-resistant protozoa. medicinal plants, which produce various bioactive molecules, can help counter this global shortage. in this study, we prepared pterodon pubescens fruit extracts, which show antileishmanial activity, and developed a nanoemulsion of the optimized extract to improve its performance. the extracts were prepared using conventional methods and a sup ... | 2016 | 27725158 |
| the cytotoxic activity of miltefosine against leishmania and macrophages is associated with dynamic changes in plasma membrane proteins. | in this study, we combined electron paramagnetic resonance (epr) spectroscopy with an analysis of biophysical cellular parameters to study the mechanisms underlying the in vitro anti-leishmanial activity of miltefosine (mt). a thiol-specific spin label attached to membrane-bound proteins of leishmania amazonensis and peritoneal macrophages indicated that mt may bind to plasma membrane proteins in large quantities via a detergent-like action and cause structural changes associated with a marked i ... | 2017 | 27773565 |
| increased abundance of proteins involved in resistance to oxidative and nitrosative stress at the last stages of growth and development of leishmania amazonensis promastigotes revealed by proteome analysis. | leishmania amazonensis is one of the major etiological agents of the neglected, stigmatizing disease termed american cutaneous leishmaniasis (acl). acl is a zoonosis and rodents are the main reservoirs. most cases of acl are reported in brazil, bolivia, colombia and peru. the biological cycle of the parasite is digenetic because sand fly vectors transmit the motile promastigote stage to the mammalian host dermis during blood meal intakes. the amastigote stage survives within phagocytes of the ma ... | 2016 | 27776144 |
| a3k2a3-induced apoptotic cell death of leishmania amazonensis occurs through caspase- and atp-dependent mitochondrial dysfunction. | leishmaniasis is a neglected tropical disease that affects millions of people worldwide. current therapies mainly rely on antimonial drugs that are inadequate because of their high toxicity and increased drug resistance. an urgent need exists to discover new, more effective, more affordable, and more target-specific drugs. pathways that are associated with apoptosis-like cell death have been identified in unicellular eukaryotes, including protozoan parasites. in the present study, we studied the ... | 2017 | 27761752 |
| exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor. | 3,6-disubstituted imidazo[1,2-b]pyridazine derivatives were synthesized to identify new inhibitors of various eukaryotic kinases, including mammalian and protozoan kinases. among the imidazo[1,2-b]pyridazines tested as kinase inhibitors, several derivatives were selective for dyrks and clks, with ic50 < 100 nm. the characterization of the kinome of several parasites, such as plasmodium and leishmania, has pointed out profound divergences between protein kinases of the parasites and those of the ... | 2017 | 27721154 |
| 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. | 2016 | 27716449 |
| a vaccine composed of a hypothetical protein and the eukaryotic initiation factor 5a from leishmania braziliensis cross-protection against leishmania amazonensis infection. | in the present study, two proteins cloned from leishmania braziliensis species, a hypothetical protein (lbhyp) and the eukaryotic initiation factor 5a (eif5a), were evaluated to protect balb/c mice against l. amazonensis infection. the animals were immunized with the antigens, either separately or in combination, using saponin as an immune adjuvant in both cases. spleen cells from vaccinated and later infected mice produced significantly higher levels of protein and parasite-specific ifn-γ, il-1 ... | 2017 | 27693018 |
| 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 ... | 2016 | 27649549 |
| leishmania infection inhibits macrophage motility by altering f-actin dynamics and the expression of adhesion complex proteins. | leishmania is an intracellular protozoan parasite that causes a broad spectrum of clinical manifestations, ranging from self-healing skin lesions to fatal visceralizing disease. as the host cells of choice for all species of leishmania, macrophages are critical for the establishment of infections. how macrophages contribute to parasite homing to specific tissues and how parasites modulate macrophage function are still poorly understood. in this study, we show that leishmania amazonensis infectio ... | 2017 | 27641840 |
| the brown alga stypopodium zonale (dictyotaceae): a potential source of anti-leishmania drugs. | this study evaluated the anti-leishmania amazonensis activity of a lipophilic extract from the brown alga stypopodium zonale and atomaric acid, its major compound. our initial results revealed high inhibitory activity for intracellular amastigotes in a dose-dependent manner and an ic50 of 0.27 μg/ml. due to its high anti-leishmania activity and low toxicity toward host cells, we fractionated the lipophilic extract. a major meroditerpene in this extract, atomaric acid, and its methyl ester deriva ... | 2016 | 27618071 |
| generating nanoparticles containing a new 4-nitrobenzaldehyde thiosemicarbazone compound with antileishmanial activity. | thiosemicarbazones are an important class of compounds that have been extensively studied in recent years, mainly because of their broad profile of pharmacological activity. a new 4-nitrobenzaldehyde thiosemicarbazone compound (bzts) that was derived from s-limonene has been demonstrated to have significant antiprotozoan activity. however, the hydrophobic characteristic of bzts limits its administration and results in low oral bioavailability. in the present study, we proposed the synthesis of n ... | 2016 | 27612813 |
| antileishmanial activity of ezetimibe: inhibition of sterol biosynthesis, in vitro synergy with azoles, and efficacy in experimental cutaneous leishmaniasis. | leishmaniasis affects mainly low-income populations in tropical regions. radical innovation in drug discovery is time-consuming and expensive, imposing severe restrictions on the ability to launch new chemical entities for the treatment of neglected diseases. drug repositioning is an attractive strategy for addressing a specific demand more easily. in this project, we have evaluated the antileishmanial activities of 30 drugs currently in clinical use for various morbidities. ezetimibe, clinicall ... | 2016 | 27600041 |
| synthesis and evaluation against leishmania amazonensis of novel pyrazolo[3,4-d]pyridazinone-n-acylhydrazone-(bi)thiophene hybrids. | a new series of pyrazolo[3,4-d]pyridazin-7-one derivatives were synthesised and evaluated for their in vitro antileishmanial activity against leishmania amazonensis promastigote and axenic amastigote forms. the results showed that the pyrazolo[3,4-d]-pyridazin-7-one-n-acylhydrazone-(bi)thiophene hybrids 5b, 6b and 6d exhibit better antileishmanial activity with ic50 84.96, 3.63 and 10.79 μm, against the promastigote form and ic50 32.71, 2.32 and >100 μm against the axenic amastigote form, respec ... | 2016 | 27597410 |
| morinda citrifolia linn. reduces parasite load and modulates cytokines and extracellular matrix proteins in c57bl/6 mice infected with leishmania (leishmania) amazonensis. | the absence of an effective vaccine and the debilitating chemotherapy for leishmaniasis demonstrate the need for developing alternative treatments. several studies conducted with morinda citrifolia have shown various biological activities, including antileishmanial activity, however its mechanisms of action are unknown. this study aimed to analyze the in vivo activity of m. citrifolia fruit juice (noni) against leishmania (leishmania) amazonensis in c57bl/6 mice. m. citrifolia fruit juice from t ... | 2016 | 27579922 |
| 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. | 2016 | 27564587 |
| 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 ... | 2016 | 27556219 |
| 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 ... | 2016 | 27546158 |
| 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 ... | 2016 | 27531705 |
| 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 ... | 2016 | 27530664 |
| 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 ... | 2016 | 27517895 |
| 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 ... | 2016 | 27515718 |
| 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 ... | 2016 | 27499755 |
| 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 ... | 2016 | 27498229 |
| 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 ... | 2016 | 27446022 |
| 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. | 2016 | 27432217 |
| 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 ... | 2016 | 27427166 |
| in vitro and in vivo miltefosine susceptibility of a leishmania amazonensis isolate from a patient with diffuse cutaneous leishmaniasis: follow-up. | | 2016 | 27416021 |
| in vitro effects of the neolignan 2,3-dihydrobenzofuran against leishmania amazonensis. | leishmaniasis is an infectious disease complex caused by protozoa from the leishmania genus, which presents a broad spectrum of clinical manifestations: cutaneous, mucocutaneous and visceral forms. the current treatments are unsatisfactory considering that few drugs are available and present some level of toxicity. many lignans and neolignans have been used for the development of new antileishmania drugs. the capability in vitro of the neolignan 2,3-dihydrobenzofuran (2,3-dbf), a commonly found ... | 2017 | 27398818 |
| 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 ... | 2016 | 27365053 |
| 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 ... | 2016 | 27352873 |
| 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 ... | 2016 | 27331807 |
| 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 ... | 2016 | 27328771 |
| 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 ... | 2016 | 27318121 |
| 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 ... | 2016 | 27317947 |
| 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 ... | 2016 | 27307731 |
| 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 ... | 2016 | 27304024 |
| 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, ... | 2016 | 27280707 |
| 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 ... | 2016 | 27264642 |
| a proteomic road to acquire an accurate serological diagnosis for human tegumentary leishmaniasis. | diagnostic tools are important for clinical management and epidemiological evaluation of tegumentary (tl) and visceral (vl) leishmaniasis. serology is not frequently used for the diagnosis of the tl form because low antibody titers and cross-reaction with vl. therefore, it is crucial to identify specific and immunogenic antigens from species associated with the tl form. here we employed a proteomic approach coupled to an in silico analysis and identified the most abundant and immunogenic protein ... | 2017 | 27262223 |
| 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 ... | 2016 | 27251851 |
| antileishmanial activity of a calophyllum brasiliense leaf extract. | calophyllum brasiliense (clusiaceae) is a tree that grows mainly in the atlantic forest in brazil. its leaves possess antibacterial activity, cytotoxic activity against certain tumor cell lines, and antimicrobial activity in balb/c mice infected with leishmania (leishmania) amazonensis.aiming to identify ultrastructural changes and dna fragmentation in leishmania (viannia) braziliensis, promastigotes were treated with a concentration of the dichloromethane extract and coumarin (-) mammea a/bb fr ... | 2017 | 27224267 |
| 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 ... | 2016 | 27223609 |
| 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 ... | 2016 | 27198787 |
| 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. | 2016 | 27163566 |
| 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 ... | 2016 | 27154356 |
| synthesis, cytotoxic activity on leukemia cell lines and quantitative structure-activity relationships (qsar) studies of morita-baylis-hillman adducts. | the morita-baylis-hillman reaction is an organocatalyzed chemical transformation that allows access to small poly-functionalized molecules and has considerable synthetic potential and promising biological profiles. the morita-baylis-hillman adducts (mbha) are a new class of bioactive compounds and highlight its potentialities to the discovery of new cheaper and efficient drugs, e.g. as anti-leishmania chagasi and leishmania amazonensis, anti- trypanosoma cruzi, anti-plasmodium falciparum and pla ... | 2016 | 27150963 |
| verbascoside inhibits promastigote growth and arginase activity of leishmania amazonensis. | verbascoside (1) is a phenylethanoid glycoside that has antileishmanial activity against leishmania infantum and leishmania donovani. in this study, we verified the activity of 1 on leishmania amazonensis and arginase inhibition. compound 1 showed an ec50 of 19 μm against l. amazonensis promastigotes and is a competitive arginase inhibitor (ki = 0.7 μm). docking studies were performed to assess the interaction of 1 with arginase at the molecular level. arginase is an enzyme of the polyamine bios ... | 2016 | 27096224 |
| in vivo and in vitro phagocytosis of leishmania (leishmania) amazonensis promastigotes by b-1 cells. | leishmaniasis is caused by leishmania parasites that infect several cell types. the promastigote stage of leishmania is internalized by phagocytic cells and transformed into the obligate intracellular amastigote form. b-1 cells are a subpopulation of b cells that are able to differentiate in vitro and in vivo into mononuclear phagocyte-like cells with phagocytic properties. b-1 cells use several receptors for phagocytosis, such as the mannose receptor and third complement receptor. leishmania bi ... | 2016 | 27084328 |
| differential recruitment of dendritic cells subsets to lymph nodes correlates with a protective or permissive t-cell response during leishmania (viannia) braziliensis or leishmania (leishmania) amazonensis infection. | leishmania (l.) amazonensis (la) and l. (v.) braziliensis (lb) are responsible for a large clinical and immunopathological spectrum in human disease; while la may be responsible for anergic disease, lb infection leads to cellular hypersensitivity. to better understand the dichotomy in the immune response caused by these leishmania species, we evaluated subsets of dendritic cells (dcs) and t lymphocyte in draining lymph nodes during the course of la and lb infection in balb/c mice. our results de ... | 2016 | 27073297 |
| neutrophils contribute to the protection conferred by artinm against intracellular pathogens: a study on leishmania major. | artinm, a d-mannose binding lectin from artocarpus heterophyllus, has immunomodulatory activities through its interaction with n-glycans of immune cells, culminating with the establishment of t helper type 1 (th1) immunity. this interaction protects mice against intracellular pathogens, including leishmania major and leishmania amazonensis. artinm induces neutrophils activation, which is known to account for both resistance to pathogens and host tissue injury. although exacerbated inflammation w ... | 2016 | 27058234 |
| 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. | 2016 | 27056545 |
| 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 ... | 2016 | 27048943 |