Publications

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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
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
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
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
in vitro and in vivo miltefosine susceptibility of a leishmania amazonensis isolate from a patient with diffuse cutaneous leishmaniasis: follow-up. 201627416021
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
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 ...201627150963
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 ...201627096224
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 ...201627084328
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 ...201627073297
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 ...201627058234
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
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
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
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
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
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
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
monitoring the response of patients with cutaneous leishmaniasis to treatment with pentamidine isethionate by quantitative real-time pcr, and identification of leishmania parasites not responding to therapy.leishmania (viannia) guyanensis is believed to be the principal cause of cutaneous leishmaniasis (cl) in suriname. this disease is treated with pentamidine isethionate (pi), but treatment failure has increasingly been reported.201626648589
antileishmanial and immunomodulatory effects of the essential oil from tetradenia riparia (hochstetter) codd.cutaneous leishmaniasis usually presents therapeutic resistance to antimonials, and the existing therapies for leishmaniasis have many adverse effects and toxicity. natural products may be regarded as possible candidates for alternative leishmaniasis treatment. the plant tetradenia riparia has shown promise for the treatment of infectious diseases in folk medicine. we evaluated the antileishmanial activity of an essential oil from t. riparia (treo) and the modulatory effects of treo on cytokine ...201626615004
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
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
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
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
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
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
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
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
phosphatidylserine exposure on the surface of leishmania amazonensis amastigotes modulates in vivo infection and dendritic cell function.leishmania amazonensis parasites can cause diverse forms of leishmaniasis in humans and persistent lesions in most inbred strains of mice. in both cases, the infection is characterized by a marked immunosuppression of the host. we previously showed that amastigote forms of the parasite make use of surface-exposed phosphatidylserine (ps) molecules to infect host cells and promote alternative macrophage activation, leading to uncontrolled intracellular proliferation of the parasites. in this study ...201623163958
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
leishmania infection in bats from a non-endemic region of leishmaniasis in brazil.leishmaniasis is a complex of zoonotic diseases caused by parasites of the genus leishmania, which can develop in domestic as well as wild animals and humans throughout the world. currently, this disease is spreading in rural and urban areas of non-endemic regions in brazil. recently, bats have gained epidemiological significance in leishmaniasis due to its close relationship with human settlements. in this study, we investigated the presence of leishmania spp. dna in blood samples from 448 bats ...201728831941
synthesis, in vitro and in vivo giardicidal activity of nitrothiazole-nsaid chimeras displaying broad antiprotozoal spectrum.we designed and synthesized five new 5-nitrothiazole-nsaid chimeras as analogues of nitazoxanide, using a dcc-activated amidation. compounds 1-5 were tested in vitro against a panel of five protozoa: 2 amitochondriates (giardia intestinalis, trichomonas vaginalis) and 3 kinetoplastids (leishmania mexicana, leishmania amazonensis and trypanosoma cruzi). all chimeras showed broad spectrum and potent antiprotozoal activities, with ic50 values ranging from the low micromolar to nanomolar order. comp ...201728645659
platonia insignis mart., a brazilian amazonian plant: the stem barks extract and its main constituent lupeol exert antileishmanial effects involving macrophages activation.platonia insignis mart., popularly known as "bacurizeiro," is used in traditional medical practices based on its diverse biological properties. this study was aimed at evaluating the antileishmanial effects of the ethanol extract (etoh-ext), hexane fraction (hex-f), and its main isolated lupeol obtained from stem barks of p. insignis against leishmania (leishmania) amazonensis, as well as their cytotoxicity and possible mechanisms of action. the etoh-ext, hex-f, and lupeol inhibited the growth o ...201728852412
effects of bone marrow mesenchymal stromal cell therapy in experimental cutaneous leishmaniasis in balb/c mice induced by leishmania amazonensis.cutaneous leishmaniasis remains both a public health and a therapeutic challenge. to date, no ideal therapy for cutaneous leishmaniasis has been identified, and no universally accepted therapeutic regimen and approved vaccines are available. due to the mesenchymal stromal cell (msc) immunomodulatory capacity, they have been applied in a wide variety of disorders, including infectious, inflammatory, and allergic diseases. we evaluated the potential effects of bone marrow msc therapy in a murine m ...201728848541
a calmodulin-like protein (lcala) is a new leishmania amazonesis candidate for telomere end-binding protein.leishmania spp. telomeres are composed of 5'-ttaggg-3' repeats associated with proteins. we have previously identified larbp38 and larpa-1 as proteins that bind the g-rich telomeric strand. at that time, we had also partially characterized a protein:dna complex, named lagt1, but we could not identify its protein component.201728844976
the photodynamic action of pheophorbide a induces cell death through oxidative stress in leishmania amazonensis.leishmaniasis is a disease caused by hemoflagellate protozoa, affecting millions of people worldwide. the difficulties of treating patients with this parasitosis include the limited efficacy and many side effects of the currently available drugs. therefore, the search for new compounds with leishmanicidal action is necessary. photodynamic therapy has been studied in the medical field because of its selectivity, utilizing a combination of visible light, a photosensitizer compound, and singlet oxy ...201728821011
synthesis and in vitro evaluation of ca(2+) channel blockers 1,4-dihydropyridines analogues against trypanosoma cruzi and leishmania amazonensis: sar analysis.drugs containing the1,4-dihydropyridine (dhp) core have recently attracted attention concerning their antiparasitic effect against various species of leishmania and trypanosoma. this approach named drugs repositioning led to interesting results, which have prompted us to prepare 21 dhp's analogues. the 1,4-dhp scaffold was decorated with different function groups at tree points including the nitrogen atom (nh and n-phenyl), the aryl group attached to c-4 (various substituted aryl residues) and t ...201728801098
leishmania amazonensis-induced camp triggered by adenosine a2b receptor is important to inhibit dendritic cell activation and evade immune response in infected mice.differently from others leishmania species, infection by the protozoan parasite l. amazonensis is associated with a lack of antigen-specific t-cell responses. dendritic cells (dc) are essential for the innate immune response and for directing the differentiation of t-helper lymphocytes. previously, we showed that l. amazonensis infection impairs dc activation through the activation of adenosine a2b receptor, and here, we evaluated the intracellular events triggered by this receptor in infected c ...201728791011
morita-baylis-hillman adducts display anti-inflammatory effects by modulating inflammatory mediator expression in raw264.7 cells.inflammatory response plays an important role not only in the normal physiology but also in pathologies such as cancers. the morita-baylis-hillman adducts (mbha) are a novel group of synthetic molecules that have demonstrated many biological activities against some parasitic cells such as plasmodium falciparum, leishmania amazonensis, and leishmania chagasi, and antimitotic activity against sea urchin embryonic cells was also related. however, little is known about the mechanisms induced by mbha ...201728785138
dectin-1 activation during leishmania amazonensis phagocytosis prompts syk-dependent reactive oxygen species production to trigger inflammasome assembly and restriction of parasite replication.protozoan parasites of the genus leishmania are the causative agents of leishmaniasis, a disease that can be lethal and affects 12 million people worldwide. leishmania replicates intracellularly in macrophages, a process that is essential for disease progression. although the production of reactive oxygen species (ros) accounts for restriction of parasite replication, leishmania is known to induce ros upon macrophage infection. we have recently demonstrated nlrp3 inflammasome activation in infec ...201728784846
anti-leishmania activity of new ruthenium(ii) complexes: effect on parasite-host interaction.leishmaniasis is a parasitic disease caused by protozoa of the genus leishmania. the many complications presented by the current treatment - including high toxicity, high cost and parasite resistance - make the development of new therapeutic agents indispensable. the present study aims to evaluate the anti-leishmania potential of new ruthenium(ii) complexes, cis‑[ru(ii)(η(2)-o2cr)(dppm)2]pf6, with dppm=bis(diphenylphosphino)methane and r=4-butylbenzoate (bbato) 1, 4-(methylthio)benzoate (mtbato) ...201728783554
murine cutaneous leishmaniasis investigated by maldi mass spectrometry imaging.imaging mass spectrometry (ims) is recognized as a powerful tool to investigate the spatial distribution of untargeted or targeted molecules of a wide variety of samples including tissue sections. leishmania is a protozoan parasite that causes different clinical manifestations in mammalian hosts. leishmaniasis is a major public health risk in different continents and represents one of the most important neglected diseases. cutaneous lesions from mice experimentally infected with leishmania spp. ...201728783195
evaluation of boldine activity against intracellular amastigotes of leishmania amazonensis.leishmaniasis is a neglected and endemic disease that affects poorest population mainly in developing countries. a lack of adequate and definitive chemotherapeutic agents to fight against this infection has led to the investigation of numerous compounds. the aim of this study was to investigate in vitro activity of boldine against leishmania amazonensis murine cell infection. boldine ((s)-2,9-dihydroxy-1,10-dimethoxy-aporphine) is an aporphine alkaloid found abundantly in the leaves/bark of bold ...201728719960
il-32γ promotes the healing of murine cutaneous lesions caused by leishmania braziliensis infection in contrast to leishmania amazonensis.interleukin 32 (il-32) is a pro-inflammatory cytokine induced in patients with american tegumentary leishmaniasis (atl) caused by leishmania braziliensis. here, we investigated whether il-32 is also expressed in patient lesions caused by l. amazonensis. in addition, we evaluated experimental l. amazonensis and l. braziliensis infections in c57bl/6 transgenic mice for human il-32γ (il-32γtg) in comparison with wild-type (wt) mice that do not express the il-32 gene.201728709468
chemical characterization, antileishmanial activity, and cytotoxicity effects of the essential oil from leaves of pluchea carolinensis (jacq.) g. don. (asteraceae).current strategies to control leishmaniasis are mainly based on chemotherapy. however, none of the available drugs can be considered to be ideal to treat this disease. because of the hydrophobic nature and bioactivities of their components, essential oils (eos) can be considered as important sources for developing agents against intracellular pathogens, such as leishmania parasites. in this study, we report the chemical characterization, antileishmanial activities, and cytotoxicity effect of the ...201728703380
kh-tfmdi, a novel sirtuin inhibitor, alters the cytoskeleton and mitochondrial metabolism promoting cell death in leishmania amazonensis.treatment of leishmaniasis involves the use of antimonials, miltefosine, amphotericin b or pentamidine. however, the side effects of these drugs and the reports of drug-resistant parasites demonstrate the need for new treatments that are safer and more efficacious. histone deacetylase inhibitors are a new class of compounds with potential to treat leishmaniasis. herein, we evaluated the effects of kh-tfmdi, a novel histone deacetylase inhibitor, on leishmania amazonensis promastigotes and intrac ...201728685254
amiodarone and itraconazole improve the activity of pentavalent antimonial in the treatment of experimental cutaneous leishmaniasis.leishmaniasis affect millions of people, causing morbidity and mortality, especially in developing tropical and subtropical countries. unfortunately, the possibilities of treatment for these infections are still quite limited and most of the available drugs present serious side effects. the objective of this paper was to evaluate the therapeutic role of amiodarone and itraconazole in the treatment of cutaneous leishmaniasis caused by leishmania (leishmania) amazonensis. in order to perform this ...201728668672
the potent cell permeable calpain inhibitor mdl28170 affects the interaction of leishmania amazonensis with macrophages and shows anti-amastigote activity.since the discovery of the28 first drugs used in leishmaniasis treatment up to now, the search for compounds with anti-leishmania activity without toxic effects and able to overcome the emergency of resistant strains remains a major goal to combat this neglected disease. with this in mind, in the present work, we evaluated the effects of the calpain inhibitor mdl28170 on the interaction process of leishmania amazonensis promastigote forms with murine peritoneal macrophages and on the intracellul ...201728663009
in vitro additive interaction between ketoconazole and antimony against intramacrophage leishmania (leishmania) amazonensis amastigotes.leishmaniasis is a group of diseases caused by protozoa of leishmania genus. the currently available treatments for this disease are expensive, present high toxicity and are associated to difficulties of healing and parasite resistance. therefore, the development of strategies for leishmaniasis treatment is indispensable and includes reposition of existing drugs, as well as drug combination therapy. the aim of this study was to assess the nature of ketoconazole and antimony association on the cy ...201728662149
lipid-core nanocapsules increase the oral efficacy of quercetin in cutaneous leishmaniasis.new oral treatments are needed for all forms of leishmaniasis. here, the improved oral efficacy of quercetin (qc) and its penta-acetylated derivative (pqc) was evaluated in cutaneous leishmaniasis after encapsulation in lipid-core nanocapsules (lncs) of poly(ε-caprolactone). leishmania amazonensis-infected balb/c mice were given 51 daily oral doses of free drugs (16 mg kg-1) or lnc-loaded drugs (0·4 mg kg-1). while treatment with free qc reduced the lesion sizes and parasite loads by 38 and 71%, ...201728653597
chemical profile and anti-leishmanial activity of three ecuadorian propolis samples from quito, guayaquil and cotacachi regions.three propolis samples were collected from different regions of ecuador (quito, guayaquil and cotacachi) and their methanolic extracts were prepared. preliminary information supplied by tlc and nmr data, allowed us to define two main types of propolis: cotacachi propoli sample (cps), rich in flavonoids and quito and guayaquil samples (qps and gps) containing triterpenic alcohols and acetyl triterpenes as the main constituents. two different approaches based on rp-hplc preparative procedure and n ...201728642199
crotoxin stimulates an m1 activation profile in murine macrophages during leishmania amazonensis infection.american tegumentary leishmaniasis is caused by different species of leishmania. this protozoan employs several mechanisms to subvert the microbicidal activity of macrophages and, given the limited efficacy of current therapies, the development of alternative treatments is essential. animal venoms are known to exhibit a variety of pharmacological activities, including antiparasitic effects. crotoxin (ctx) is the main component of crotalus durissus terrificus venom, and it has several biological ...201728641584
vosalophen: a vanadium complex with a stilbene derivative-induction of apoptosis, autophagy, and efficiency in experimental cutaneous leishmaniasis.in our previous work, we demonstrated the promising in vitro effect of vosalophen, a vanadium complex with a stilbene derivative, against leishmania amazonensis. its antileishmanial activity has been associated with oxidative stress in l. amazonensis promastigotes and l. amazonensis-infected macrophages. in the present study, the mechanism involved in the death of parasites after treatment with vosalophen, as well as in vivo effect in the murine model cutaneous leishmaniasis, has been investigat ...201728597089
1,3-bis(aryloxy)propan-2-ols as potential antileishmanial agents.we describe herein the synthesis and antileishmanial activity of 1,3-bis(aryloxy)propan-2-ols. five compounds (2, 3, 13, 17, and 18) exhibited an effective antileishmanial activity against stationary promastigote forms of leishmania amazonensis (ic50  < 15.0 μm), and an influence of compound lipophilicity on activity was suggested. most of the compounds were poorly selective, as they showed toxicity toward murine macrophages, except 17 and 18, which presented good selective indexes (si ≥ 10.0). ...201728590516
anti-parasitic effect of the diuretic and na+-atpase inhibitor furosemide in cutaneous leishmaniasis.leishmania amazonensis promastigotes are known to express furosemide (lasix®)-sensitive p-type membrane na+-atpase. in the present study, furosemide activity was studied in intracellular amastigotes and infected balb/c mice to investigate its efficacy in cutaneous leishmaniasis (cl). intracellular parasites, but not macrophages, were found to be sensitive to killing by furosemide (ic50 = 87 µ m vs cc50 ≫ 1000 µ m, respectively). although furosemide did not induce nitric oxide production or intra ...201728583224
discovery of novel inhibitors for leishmania nucleoside diphosphatase kinase (ndk) based on its structural and functional characterization.nucleoside diphosphate kinases (ndks) are ubiquitous enzymes that catalyze the transfer of the γ-phosphate moiety from an ntp donor to an ndp acceptor, crucial for maintaining the cellular level of nucleoside triphosphates (ntps). the inability of trypanosomatids to synthesize purines de novo and their dependence on the salvage pathway makes ndk an attractive target to develop drugs for the diseases they cause. here we report the discovery of novel inhibitors for leishmania ndk based on the stru ...201728551817
the iron-dependent mitochondrial superoxide dismutase soda promotes leishmania virulence.leishmaniasis is one of the leading globally neglected diseases, affecting millions of people worldwide. leishmania infection depends on the ability of insect-transmitted metacyclic promastigotes to invade mammalian hosts, differentiate into amastigotes, and replicate inside macrophages. to counter the hostile oxidative environment inside macrophages, these protozoans contain anti-oxidant systems that include iron-dependent superoxide dismutases (sods) in mitochondria and glycosomes. increasing ...201728550086
cytotoxicity and anti-leishmania amazonensis activity of citrus sinensis leaf extracts.leishmania amazonensis is the main agent of diffuse cutaneous leishmaniasis, a disease characterized by lesional polymorphism and the commitment of skin surface. previous reports demonstrated that the citrus genus possess antimicrobial activity.201728524774
leishmanicidal activity and structure-activity relationships of essential oil constituents.several constituents of essential oils have been shown to be active against pathogens such as bacteria, fungi, and protozoa. this study demonstrated the in vitro action of ten compounds present in essential oils against leishmania amazonensis promastigotes. with the exception of p-cymene, all evaluated compounds presented leishmanicidal activity, exhibiting ic50 between 25.4 and 568.1 μg ml(-1). compounds with the best leishmanicidal activity presented a phenolic moiety (ic50 between 25.4 and 82 ...201728509873
efficacy of a binuclear cyclopalladated compound therapy for cutaneous leishmaniasis in the murine model of infection with leishmania amazonensis and its inhibitory effect on topoisomerase 1b.leishmaniasis is a disease found throughout the (sub)tropical parts of the world caused by protozoan parasites of the leishmania genus. despite the numerous problems associated with existing treatments, pharmaceutical companies continue to neglect the development of better ones. the high toxicity of current drugs combined with emerging resistance makes the discovery of new therapeutic alternatives urgent. we report here the evaluation of a binuclear cyclopalladated complex containing pd(ii) and ...201728507113
structurally optimized analogs of the retrograde trafficking inhibitor retro-2cycl limit leishmania infections.in infected mammalian cells, leishmania parasites reside within specialized compartments called parasitophorous vacuoles (lpvs). we have previously shown that retro-2, a member of a novel class of small retrograde pathway inhibitors caused reduced lpv sizes and lower parasite numbers during experimental l. mexicana sp. infections. the purpose of this study was to determine if structural analogs of retro-2cycl reported to have superior potency in the inhibition of retrograde pathway-dependent phe ...201728505157
a new l-amino acid oxidase from bothrops jararacussu snake venom: isolation, partial characterization, and assessment of pro-apoptotic and antiprotozoal activities.a new l-amino acid oxidase (laao) from bothrops jararacussu venom (bjussulaao-ii) was isolated by using a three-step chromatographic procedure based on molecular exclusion, hydrophobicity, and affinity. bjussulaao-ii is an acidic enzyme with pi=3.9 and molecular mass=60.36kda that represents 0.3% of the venom proteins and exhibits high enzymatic activity (4884.53u/mg/mim). we determined part of the primary sequence of bjussulaao-ii by identifying 96 amino acids, from which 34 compose the n-termi ...201728495622
experimental mixed infection of leishmania (leishmania) amazonensis and leishmania (l.) infantum in hamsters (mesocricetus auratus).in south america, visceral leishmaniasis is frequently caused by leishmania infantum and, at an unknown frequency, by leishmania amazonensis. therefore, mixed infections with these organisms are possible. mixed infections might affect the clinical course, immune response, diagnosis, treatment and epidemiology of the disease. here we describe the clinical course of mixed infections with l. amazonensis and l. infantum in a hamster model. we show that mixed infections are associated with more sever ...201728487000
voacamine alters leishmania ultrastructure and kills parasite by poisoning unusual bi-subunit topoisomerase ib.indole alkaloids possess a large spectrum of biological activities including anti-protozoal action. here we report for the first time that voacamine, isolated from the plant tabernaemontana coronaria, is an antiprotozoal agent effective against a large array of trypanosomatid parasites including indian strain of leishmania donovani and brazilian strains of leishmania amazonensis and trypanosoma cruzi. it inhibits the relaxation activity of topoisomerase ib of l. donovani (ldtop1b) and stabilizes ...201728483460
targeting leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system.dextran-coated poly (n-butyl cyanoacrylate) nanoparticles (pbca-nps) were prepared and were evaluated for enhanced delivery of a promising anti-leishmania drug candidate, hydroxymethylnitrofurazone (nfoh), to phagocytic cells. currently available chemotherapy for leishmaniasis, such as pentavalent antimonials, presents low safety and efficacy. furthermore, widespread drug resistance in leishmaniasis is rapidly emerging. to overcome these drawbacks, the use of nanosized delivery systems can reduc ...201728454918
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