| leishmania strains causing self-healing cutaneous leishmaniasis have greater susceptibility towards oxidative stress. | the survival of leishmania parasites within macrophages is influenced by generation of free radicals. to establish whether generation of free radicals influenced chemotherapeutic response, promastigotes from isolates causing self-healing or delayed/non-self-healing cutaneous leishmaniasis (cl) or visceral leishmaniasis (vl) were evaluated for their susceptibility to nitric oxide (no), antimony and miltefosine. in a self-healing cl strain of leishmania major (5askh), susceptibility to no and anti ... | 2012 | 22385212 |
| ldl uptake by leishmania amazonensis: involvement of membrane lipid microdomains. | leishmania amazonensis lacks a de novo mechanism for cholesterol synthesis and therefore must scavenge this lipid from the host environment. in this study we show that the l. amazonensis takes up and metabolizes human ldl(1) particles in both a time and dose-dependent manner. this mechanism implies the presence of a true ldl receptor because the uptake is blocked by both low temperature and by the excess of non-labelled ldl. this receptor is probably associated with specific microdomains in the ... | 2012 | 22381219 |
| infection by leishmania amazonensis in mice: a potential model for chronic hypoxia. | hypoxia is a common feature of injured and infected tissues. hypoxia inducible factors 1α and 2α (hif-1α, hif-2α) are heterodimeric transcription factors mediating the cellular responses to hypoxia and also the vascular endothelial growth factor (vegf). vegf is a cytokine which can be induced by hypoxia, whose pathogenic mechanisms are still unclear and which is the subject of debate. murine cutaneous lesions during leishmania amazonensis parasite infection are chronic, although they are small a ... | 2012 | 22360823 |
| chemical and biological analyses of the essential oils and main constituents of piper species. | the essential oils obtained from leaves of piper duckei and piper demeraranum by hydrodistillation were analyzed by gas chromatography-mass spectrometry. the main constituents found in p. demeraranum oil were limonene (19.3%) and β-elemene (33.1%) and in p. duckei oil the major components found were germacrene d (14.7%) and trans-caryophyllene (27.1%). p. demeraranum and p. duckei oils exhibited biological activity, with ic(50) values between 15 to 76 μg ml(-1) against two leishmania species, p. ... | 2012 | 22330429 |
| the leishmanicidal flavonols quercetin and quercitrin target leishmania (leishmania) amazonensis arginase. | polyamine biosynthesis enzymes are promising drug targets for the treatment of leishmaniasis, chagas' disease and african sleeping sickness. arginase, which is a metallohydrolase, is the first enzyme involved in polyamine biosynthesis and converts arginine into ornithine and urea. ornithine is used in the polyamine pathway that is essential for cell proliferation and ros detoxification by trypanothione. the flavonols quercetin and quercitrin have been described as antitrypanosomal and antileishm ... | 2012 | 22327179 |
| a comparison of two distinct murine macrophage gene expression profiles in response to leishmania amazonensis infection. | the experimental murine model of leishmaniasis has been widely used to characterize the immune response against leishmania. cba mice develop severe lesions, while c57bl/6 present small chronic lesions under l. amazonensis infection. employing a transcriptomic approach combined with biological network analysis, the gene expression profiles of c57bl/6 and cba macrophages, before and after l. amazonensis infection in vitro, were compared. these strains were selected due to their different degrees o ... | 2012 | 22321871 |
| extracellular matrix alterations in experimental leishmania amazonensis infection in susceptible and resistant mice. | leishmania is inoculated, by the bite of an infected sandfly, into the skin of the host, where the promastigotes are phagocyted by dermal macrophages. the dermal region comprises cells and abundant extracellular matrix. studies show that matrix metalloproteinases play an important role in host defense responses against pathogens in mammals and that their activities lead to the production of antimicrobial peptides. the aim of this study is to evaluate the changes in the distribution of fibronecti ... | 2012 | 22316002 |
| leishmania amazonensis impairs dc function by inhibiting cd40 expression via a2b adenosine receptor activation. | dendritic cells (dcs) play an essential role in the modulation of immune responses and several studies have evaluated the interactions between leishmania parasites and dcs. while extracellular atp exhibits proinflammatory properties, adenosine is an important anti-inflammatory mediator. here we investigated the effects of leishmania infection on dc responses and the participation of purinergic signalling in this process. bone marrow-derived dendritic cells (bmdcs) from c57bl/6j mice infected wit ... | 2012 | 22311598 |
| multifunctional cd4⁺ t cells in patients with american cutaneous leishmaniasis. | leishmaniasis is a group of important parasitic diseases affecting millions worldwide. to understand more clearly the quality of t helper type 1 (th1) response stimulated after leishmania infection, we applied a multiparametric flow cytometry protocol to evaluate multifunctional t cells induced by crude antigen extracts obtained from promastigotes of leishmania braziliensis (lbag) and leishmania amazonensis (laag) in peripheral blood mononuclear cells from healed cutaneous leishmaniasis patients ... | 2012 | 22288594 |
| effects of (-) mammea a/bb isolated from calophyllum brasiliense leaves and derivatives on mitochondrial membrane of leishmania amazonensis. | we have previously demonstrated antileishmanial activity on leishmania amazonensis of the natural (1-2), synthetic (7) and derivatives of coumarin (-) mammea a/bb (3-6) isolated from the dichloromethane extract of calophyllum brasiliense leaves. the aim of the present study was to evaluate morphological and ultrastructural alterations in leishmania amazonensis induced by these compounds. in promastigote forms, all seven compounds produced significant morphological and ultrastructural alterations ... | 2012 | 22285848 |
| efficacy of miltefosine treatment in leishmania amazonensis-infected balb/c mice. | leishmaniasis is one of the most serious worldwide diseases caused by protozoan parasites of the leishmania genus, affecting millions of people around the world. all currently available treatments present severe toxic side effects, require long-term compliance, cause serious side effects and are uncomfortable for patients. leishmania amazonensis, a species endemic to brazil, causes severe localised or diffuse skin lesions in humans. owing to the unsatisfactory nature of the currently available c ... | 2012 | 22226653 |
| modeling of leishmaniasis infection dynamics: novel application to the design of effective therapies. | the who considers leishmaniasis as one of the six most important tropical diseases worldwide. it is caused by parasites of the genus leishmania that are passed on to humans and animals by the phlebotomine sandfly. despite all of the research, there is still a lack of understanding on the metabolism of the parasite and the progression of the disease. in this study, a mathematical model of disease progression was developed based on experimental data of clinical symptoms, immunological responses, a ... | 2012 | 22222070 |
| leishmanicidal, trypanocidal, and cytotoxic activities of endophytic fungi associated with bioactive plants in brazil. | one hundred and twenty-one isolates of endophytic fungi were recovered from leaves of the bioactive brazilian plant species ageratum myriadenia , palicourea tetraphylla , piptadenia adiantoides, and trixis vauthieri. all fungal isolates were cultivated in liquid media and crude extracts were obtained with ethyl acetate. the crude extracts were tested in bioassay panels using leishmania amazonensis , trypanosoma cruzi, the enzyme trypanothione reductase (tryr) from trypanosoma cruzi, and three hu ... | 2010 | 24031513 |
| in vitro and in vivo leishmanicidal studies of peperomia galioides (piperaceae). | petroleum ether and methylene chloride extracts of peperomia galioides and three prenylated diphenols, grifolic acid, grifolin and piperogalin exhibited in vitro antileishmanial activity. during the course of infection of balb/c mice with leishmania amazonensis, the treatments with each of these compounds did not influence the progression of the disease. | 1996 | 23195082 |
| leishmanicidal activity of peroxynitrite. | nitric oxide reacts with superoxide to produce peroxynitrite which has been reported to be highly microbicidal to trypanosoma cruzi in phosphate buffer but ineffective against leishmania major in culture medium. this contradiction and the potential importance of peroxynitrite as a cytotoxic effector molecule of both macrophages and neutrophils led us to re-examine its leishmanicidal effects. our results demonstrate that peroxynitrite inhibits growth of leishmania amazonensis promastigotes in a c ... | 1995 | 27405713 |
| 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 ... | 2017 | 28831941 |
| 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 ... | 2017 | 28645659 |
| 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 ... | 2017 | 28852412 |
| 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 ... | 2017 | 28848541 |
| 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. | 2017 | 28844976 |
| 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 ... | 2017 | 28821011 |
| 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 ... | 2017 | 28801098 |
| 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 ... | 2017 | 28791011 |
| 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 ... | 2017 | 28785138 |
| 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 ... | 2017 | 28784846 |
| 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) ... | 2017 | 28783554 |
| 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. ... | 2017 | 28783195 |
| 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 ... | 2017 | 28719960 |
| 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. | 2017 | 28709468 |
| 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 ... | 2017 | 28703380 |
| 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 ... | 2017 | 28685254 |
| 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 ... | 2017 | 28668672 |
| 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 ... | 2017 | 28663009 |
| 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 ... | 2017 | 28662149 |
| 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%, ... | 2017 | 28653597 |
| 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 ... | 2017 | 28642199 |
| 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 ... | 2017 | 28641584 |
| 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 ... | 2017 | 28597089 |
| 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). ... | 2017 | 28590516 |
| 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 ... | 2017 | 28583224 |
| 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 ... | 2017 | 28551817 |
| 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 ... | 2017 | 28550086 |
| 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. | 2017 | 28524774 |
| 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 ... | 2017 | 28509873 |
| 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 ... | 2017 | 28507113 |
| 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 ... | 2017 | 28505157 |
| 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 ... | 2017 | 28495622 |
| 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 ... | 2017 | 28487000 |
| 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 ... | 2017 | 28483460 |
| 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 ... | 2017 | 28454918 |
| evaluation of vaccinal effectiveness of preparations containing membrane antigens of leishmania (l.) amazonensis in experimental cutaneous leishmaniasis model. | american tegumentary leishmaniasis (atl) is considered a neglected disease, for which an effective vaccine or an efficient diagnosis is not yet available and whose chemotherapeutic arsenal is threatened by the emergence of resistance by etiological agents such as leishmania amazonensis. atl is endemic in poor countries and has a high incidence in brazil. vaccines developed from native parasite fractions have led to the identification of defined antigenic subunits and the development of vaccine a ... | 2017 | 28433944 |
| effect of 1,2,3-triazole salts, non-classical bioisosteres of miltefosine, on leishmania amazonensis. | here, we report the effect of new non-classical bioisosteres of miltefosine on leishmania amazonensis. fifteen compounds were synthesized and the compound dhmtac, containing an acetate anion, a side chain of 10 carbon atoms linked to n-1 and a methyl group linked to n-3, showed high and selective biological activity against l. amazonensis. on the intracellular amastigotes, stages of the parasite related to human disease, the ic50 values were near or similar to the 1.0μm (0.9, 0.8 and 1.0μm on l. ... | 2017 | 28433512 |
| pcr-based identification of trypanosoma lewisi and trypanosoma musculi using maxicircle kinetoplast dna. | trypanosoma lewisi, transmitted by rat fleas, is a widespread pathogen specific to rats with records of human infection cases. its closely related species with global distribution, trypanosoma musculi, is transmitted between mice by ingestion of infected fleas. these trypanosomes are of similar morphology, making it difficult to distinguish them by microscopy. in this study, we have developed a rapid, sensitive and reliable pcr method for the diagnosis of t. lewisi and t. musculi. the t. lewisi- ... | 2017 | 28427957 |
| effect of piplartine and cinnamides on leishmania amazonensis, plasmodium falciparum and on peritoneal cells of swiss mice. | plants of the piperaceae family produce piplartine that was used to synthesize the cinnamides. | 2017 | 28415906 |
| resolvin d1 drives establishment of leishmania amazonensis infection. | previous studies have indicated that the balance between different eicosanoids reflect the intensity of the inflammatory profile in patients with tegumentary leishmaniasis. more recently, pro-resolution lipid mediators have been shown to play critical roles in dampening pathological inflammatory processes to reestablish homeostasis in a diverse range of experimental settings. among these lipid mediator, resolvins from d series have been described as potent anti-inflammatory and immunomodulatory ... | 2017 | 28393908 |