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The worrisome emergence of pathogens resistant to conventional drugs has stimulated the search for new classes of antimicrobial and antiparasitic agents from natural sources. Antimicrobial peptides (AMPs), acting through mechanisms that do not rely on the interaction with a specific receptor, provide new possibilities for the development of drugs against resistant organisms. This study sought to purify and proteomically characterize the antimicrobial and antiparasitic peptidomes of B. atrox and B. jararacussu snake venoms against Gram-positive (Staphylococcus aureus, Methicillin-resistant Staphylococcus aureus-MRSA), Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) bacteria, and the protozoan parasites Leishmania amazonensis and Plasmodium falciparum (clone W2, resistant to chloroquine). To this end, B. atrox and B. jararacussu venom peptides were purified by combination of 3 kDa cut-off Amicon® ultracentrifugal filters and reverse-phase high-performance liquid chromatography, and then identified by electrospray-ionization Ion-Trap/Time-of-Flight mass spectrometry. Fourteen distinct peptides, with masses ranging from 443.17 to 1383.73 Da and primary structure between 3 and 13 amino acid residues, were sequenced. Among them, 13 contained unique sequences, including 4 novel bradykinin-potentiating-like peptides (BPPs), and a snake venom metalloproteinase tripeptide inhibitor (SVMPi). Although commonly found in Viperidae venoms, except for Bax-12, the BPPs and SVMPi here reported had not been described in B. atrox and B. jararacussu venoms. Among the novel peptides, some exhibited bactericidal activity towards P. aeruginosa and S. aureus, had low hemolytic effect, and were devoid of antiparasitic activity. The identified novel antimicrobial peptides may be relevant in the development of new drugs for the management of multidrug-resistant Gram-negative and Gram-positive bacteria.
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Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Venenos de Crotalídeos/química , Peptídeos/farmacologia , Animais , Antibacterianos/química , Antibacterianos/farmacologia , Antimaláricos/química , Antimaláricos/farmacologia , Bothrops , Venenos de Crotalídeos/isolamento & purificação , Hemolíticos/química , Hemolíticos/farmacologia , Humanos , Leishmania/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Peptídeos/química , Peptídeos/isolamento & purificação , Plasmodium falciparum/efeitos dos fármacos , Pseudomonas aeruginosa/efeitos dos fármacos , Espectrometria de Massas por Ionização por Electrospray , Staphylococcus aureus/efeitos dos fármacosRESUMO
Furazolidone (FZD) is a widely used drug in human and veterinary medicine, and has antibacterial and antiprotozoal action. Although it is widely used as a therapy in various pathological conditions, studies on the efficacy of FZD associated with immune responses are still limited. In this review, we seek to describe which immunopharmacological responses are caused by the administration of FZD. The study followed the recommendations of the Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA). A systematic review of clinical trials and in vitro and in vivo experimental studies was carried out, which resulted in 943 papers, of which 35 were considered eligible and, of these 35, 4 were selected for analysis. The studies listed indicated that administration of FZD can modulate pro- or anti-inflammatory pathways, with a probable increase in the expression of reactive oxygen species and a modulation of apoptotic pathways.
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Imunidade Adaptativa/imunologia , Anti-Infecciosos Locais/farmacologia , Apoptose/imunologia , Furazolidona/farmacologia , Imunidade Inata/imunologia , Imunidade Adaptativa/efeitos dos fármacos , Animais , Apoptose/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Sobrevivência Celular/imunologia , Humanos , Imunidade Inata/efeitos dos fármacos , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/imunologia , Espécies Reativas de Oxigênio/metabolismoRESUMO
The original version of the article above contained an error in the text.
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Malaria, caused by protozoa of the genus Plasmodium, is a disease that infects hundreds of millions of people annually, causing an enormous social burden in many developing countries. Since current antimalarial drugs are starting to face resistance by the parasite, the development of new therapeutic options has been prompted. The enzyme Plasmodium falciparum enoyl-ACP reductase (PfENR) has a determinant role in the fatty acid biosynthesis of this parasite and is absent in humans, making it an ideal target for new antimalarial drugs. In this sense, the present study aimed at evaluating the in silico binding affinity of natural and synthetic amides through molecular docking, in addition to their in vitro activity against P. falciparum by means of the SYBR Green Fluorescence Assay. The in vitro results revealed that the natural amide piplartine (1a) presented partial antiplasmodial activity (20.54 µM), whereas its synthetic derivatives (1m-IC50 104.45 µM), (1b, 1g, 1k, and 14f) and the natural amide piperine (18a) were shown to be inactive (IC50 > 200 µM). The in silico physicochemical analyses demonstrated that compounds 1m and 14f violated the Lipinski's rule of five. The in silico analyses showed that 14f presented the best binding affinity (- 13.047 kcal/mol) to PfENR and was also superior to the reference inhibitor triclosan (- 7.806 kcal/mol). In conclusion, we found that the structural modifications in 1a caused a significant decrease in antiplasmodial activity. Therefore, new modifications are encouraged in order to improve the activity observed.
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Amidas/farmacologia , Antimaláricos/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Amidas/química , Animais , Chlorocebus aethiops , Simulação por Computador , Enoil-(Proteína de Transporte de Acila) Redutase (NADH)/antagonistas & inibidores , Enoil-(Proteína de Transporte de Acila) Redutase (NADH)/metabolismo , Células Hep G2 , Humanos , Malária Falciparum , Simulação de Acoplamento Molecular , Piper nigrum , Plasmodium falciparum/enzimologia , Triclosan/farmacologia , Células VeroRESUMO
The sandfly Trichophoromyia auraensis has recently evolved as a proven vector of Leishmania (Viannia) endemic to state of Acre in the north of Brazil. This note is intended to propose a correction in the report of the first occurrence of natural infection of Leishmania (Viannia) in this species. We and the other scientific groups reinforced that Tr. auraensis is a possible vector involved in the transmission of American cutaneous leishmaniasis in Acre, Brazil.
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Insetos Vetores/classificação , Leishmania/isolamento & purificação , Psychodidae/classificação , Animais , Brasil , Insetos Vetores/parasitologia , Leishmaniose Cutânea/transmissão , Psychodidae/parasitologiaRESUMO
In this study, we identified the phlebotomine sandfly vectors involved in the transmission of American Cutaneous Leishmaniasis (ACL) in Assis Brasil, Acre, Brazil, which is located on the Brazil-Peru-Bolivia frontier. The genotyping of Leishmania in phlebotomines was performed using polymerase chain reaction (PCR) and PCR-restriction fragment length polymorphism. A total of 6,850 sandflies comprising 67 species were captured by using CDC light traps in rural areas of the municipality. Three sandfly species were found in the state of Acre for the first time: Lutzomyia georgii, Lu. complexa and Lu. evangelistai. The predominant species was Lu. auraensis/Lu. ruifreitasi and Lu. davisi (total 59.27%). 32 of 368 pools were positive for the presence of Leishmania DNA (16 pools corresponding to Lu. davisi, and 16 corresponding to Lu. auraensis/Lu. ruifreitasi), with a minimal infection prevalence of 1.85% in Lu. davisi and 2.05% in Lu. auraensis/Lu. ruifreitasi. The Leishmania species found showed maximum identity with L. (Viannia) guyanensis and L. (V.) braziliensis in both phlebotomine species. Based on these results and similar scenarios previously described along the Brazil/Peru/Bolivia tri-border, the studied area must take into consideration the possibility of Lu. davisi and Lu. auraensis/Lu. ruifreitasi as probable vectors of ACL in this municipality.
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DNA/análise , Insetos Vetores/genética , Leishmania/genética , Psychodidae/genética , Animais , Biodiversidade , Bolívia , Brasil , DNA de Cinetoplasto , Feminino , Genótipo , Humanos , Insetos Vetores/classificação , Insetos Vetores/parasitologia , Leishmaniose Cutânea/transmissão , Peru , Reação em Cadeia da Polimerase , Densidade Demográfica , Psychodidae/classificação , Psychodidae/parasitologiaRESUMO
BACKGROUND: 3beta,6beta,16beta-trihydroxylup-20(29)-ene is a lupane triterpene isolated from Combretum leprosum fruit. The lupane group has been extensively used in studies on anticancer effects; however, its possible activity against protozoa parasites is yet poorly known. The high toxicity of the compounds currently used in leishmaniasis chemotherapy stimulates the investigation of new molecules and drug targets for antileishmanial therapy. METHODS: The activity of 3beta,6beta,16beta-trihydroxylup-20(29)-ene was evaluated against Leishmania (L.) amazonensis by determining the cytotoxicity of the compound on murine peritoneal macrophages, as well as its effects on parasite survival inside host cells. To evaluate the effect of this compound on intracellular amastigotes, cultures of infected macrophages were treated for 24, 48 and 96 h and the percentage of infected macrophages and the number of intracellular parasites was scored using light microscopy. RESULTS: Lupane showed significant activity against the intracellular amastigotes of L. (L.) amazonensis. The treatment with 109 µM for 96 h reduced in 80 % the survival index of parasites in BALB/c peritoneal macrophages. At this concentration, the triterpene caused no cytotoxic effects against mouse peritoneal macrophages. Ultrastructural analyses of L. (L.) amazonensis intracellular amastigotes showed that lupane induced some morphological changes in parasites, such as cytosolic vacuolization, lipid body formation and mitochondrial swelling. Bioinformatic analyses through molecular docking suggest that this lupane has high-affinity binding with DNA topoisomerase. CONCLUSION: Taken together, our results have showed that the lupane triterpene from C. leprosum interferes with L. (L.) amazonensis amastigote replication and survival inside vertebrate host cells and bioinformatics analyses strongly indicate that this molecule may be a potential inhibitor of topoisomerase IB. Moreover, this study opens major prospects for the development of novel chemotherapeutic agents with leishmanicidal activity.
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Combretum/química , Leishmania mexicana/efeitos dos fármacos , Leishmaniose/parasitologia , Macrófagos Peritoneais/parasitologia , Extratos Vegetais/farmacologia , Triterpenos/farmacologia , Animais , Citoplasma/parasitologia , DNA Topoisomerases Tipo I/efeitos dos fármacos , Feminino , Frutas/química , Técnicas In Vitro , Leishmaniose/tratamento farmacológico , Camundongos , Camundongos Endogâmicos BALB C , Fitoterapia , Extratos Vegetais/química , Triterpenos/isolamento & purificaçãoRESUMO
Groundbreaking studies of phlebotomine sand fly populations in Assis Brasil, State of Acre, Brazil, resulted in the collection of 13 new records of phlebotomine sand flies and one previously undescribed species. Lutzomyia naiffi sp. nov. is described here. The new species is similar to Lutzomyia columbiana (Ristorcelli & Van Ty) in measurements and other morphological characters.
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Psychodidae/anatomia & histologia , Psychodidae/classificação , Animais , Brasil , MasculinoRESUMO
Traditionally, Ehrlich's tumor is used in experimental oncology to investigate the therapeutic capacity of different synthetic chemotherapeutic agents or to evaluate the antitumoral activity of different substances of natural origin. However, the understanding of immune mechanisms during Ehrlich carcinogenesis is still limited. In this review, we seek to describe the immune response during Ehrlich's tumor growth, and natural response without the influence of pharmacological administration, immunotherapies or concomitant challenges. The study followed the recommendations of the Preferred Reporting Items for Systematic Reviews and Meta-Analysis (PRISMA). A systematic review was carried out that included experimental trials with mice challenged with Ehrlich's tumor. The research was carried out in three databases including MEDLINE/PubMed, Scopus, Latin American and Caribbean Literature in Health Sciences (LILACS). The searches resulted in 913 papers being found, of which 55 articles were considered eligible, and of these 55, 29 were selected for analysis. Findings indicate that there is an increase in the expression of M2 and T Helper (TH2) macrophages and of the cytokines IL-17, IL-1B, IL-6 and PGE in the ascitic form of Ehrlich. These phenotypic expressions are also found in ascitic neoplasms in humans. Ehrlich's solid tumor was characterized by increased expression of CD4, CD8, neutrophils and TNF-a, Foxp3 + and Qa-2 +, and these characteristics are analogous to human breasts cancers. It is our understanding that further studies are needed to assess the immune mechanisms in Ehrlich's tumor, since these findings can be used to improve cancer treatments that are analogous to Ehrlich's tumor.
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Imunidade Adaptativa/fisiologia , Carcinoma de Ehrlich/imunologia , Carcinoma de Ehrlich/patologia , Imunidade Inata/fisiologia , Imunidade Adaptativa/efeitos dos fármacos , Animais , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Carcinoma de Ehrlich/tratamento farmacológico , Humanos , Imunidade Celular/efeitos dos fármacos , Imunidade Celular/fisiologia , Imunidade Inata/efeitos dos fármacos , Camundongos , Carga Tumoral/efeitos dos fármacos , Carga Tumoral/fisiologiaRESUMO
In 2019, 229 million cases of malaria were recorded worldwide. For epidemiologic surveillance and proper treatment of persons infected with Plasmodium spp., rapid detection of infections by Plasmodium spp. is critical. Thus, Plasmodium spp. diagnosis is one of the indispensable measures for malaria control. Although microscopy is the gold standard for diagnosis, it has restrictions related mainly to the lack of qualified human resources, which is a problem in many regions. Thus, this review presents major innovations in diagnostic methods as alternatives to or complementary to microscopy. Detection platforms in lateral flow systems, electrochemical immunosensors, molecular biology and, more recently, those integrated with smartphones, are highlighted, among others. The advanced improvement of these tests aims to provide techniques that are sensitive and specific, but also quick, easy to handle and free from the laboratory environment. In this way, the tracking of malaria cases can become increasingly effective and contribute to controlling the disease.
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The discovery of new drugs and dosage forms for the treatment of neglected tropical diseases, such as human and animal leishmaniasis, is gaining interest in the chemical, biological, pharmaceutical, and medical fields. Many pharmaceutical companies are exploring the use of old drugs to establishing new drug dosage forms and drug delivery systems, in particular for use in neglected diseases. The formation of complexes with cyclodextrins is widely used to improve the stability, solubility, and bioavailability of pharmaceutical drugs, as well as reduce both the toxicity and side effects of many of these drugs. The aim of this study was to characterize solid compounds obtained from the association between furazolidone (FZD) and ß-cyclodextrin (ß-CD) or hydroxypropyl-ß-cyclodextrin (HP-ß-CD). The solid compounds were prepared in molar ratios of 1:1 and 1:2 (drug:CD) by kneading and lyophilization. Molecular docking was used to predict the preferred relative orientation of FZD when bound in both studied cyclodextrins. The resulting solid compounds were qualitatively characterized by scanning electron microscopy (SEM), thermal analysis (DSC and TG/DTG), X-ray diffraction (XRD), Raman spectroscopy with image mapping (Raman mapping), and 13C nuclear magnetic resonance spectroscopy (13C NMR) in the solid state. The cytotoxicity of the compounds against THP-1 macrophages and the 50% growth inhibition (IC50) against Leishmania amazonensis promastigote forms were subsequently investigated using in vitro techniques. For all of the solid compounds obtained, the existence of an association between FZD and CD were confirmed by one or more characterization techniques (TG/DTG, DSC, SEM, XRD, RAMAN, and 13C NMR), particularly by a significant decrease in the crystallinity of these materials and a reduction in the melting enthalpy associated with furazolidone thermal events. The formation of more effective interactions occurred in the compounds prepared by lyophilization, in a 1:2 molar ratio of the two CDs studied. However, the formation of an inclusion complex was confirmed only for the solid compound obtained from HP-ß-CD prepared by lyophilization (LHFZD1:2). The absence of cytotoxicity on the THP-1 macrophage lineages and the leishmanicidal activity were confirmed for all compounds. MHFZD1:2 and LHFZD1:2 were found to be very active against promastigote forms of L. amazonensis, while all others were considered only active. These results are in line with the literature, demonstrating the existence of biological activity for associations between drugs and CDs in the form of complexes and non-complexes. All solid compounds obtained were found to be promising for use as leishmanicidal agents against promastigote forms of L. amazonensis.
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Antiprotozoários/farmacologia , Furazolidona , beta-Ciclodextrinas , 2-Hidroxipropil-beta-Ciclodextrina , Varredura Diferencial de Calorimetria , Leishmania/efeitos dos fármacos , Simulação de Acoplamento Molecular , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios XRESUMO
INTRODUCTION: Leishmaniasis, Chagas disease, and malaria cause morbidity globally. The drugs currently used for treatment have limitations. Activity of cinnamic acid analogs against Leishmania spp., Trypanosoma cruzi, and Plasmodium falciparum was evaluated in the interest of identifying new antiprotozoal compounds. METHODS: In vitro effects of analogs against L. braziliensis, L. infantum chagasi, T. cruzi, and P. falciparum, and hemolytic and cytotoxic activities on NCTC 929 were determined. RESULTS: Three analogs showed leishmanicidal and tripanocidal activity. No antiplasmodial, hemolytic, or cytotoxic activity was observed. CONCLUSIONS: Antiprotozoal activity of analogs against L. infantum braziliensis, L. infantum chagasi, and T. cruzi was demonstrated.
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Antiprotozoários/farmacologia , Cinamatos/farmacologia , Leishmania/efeitos dos fármacos , Plasmodium falciparum/efeitos dos fármacos , Trypanosoma cruzi/efeitos dos fármacos , Antiprotozoários/química , Cinamatos/química , Testes de Sensibilidade ParasitáriaRESUMO
INTRODUCTION: This study assessed the activity of compounds from Piper tuberculatum against Plasmodium falciparum and Leishmania guyanensis. METHODS: The effects of compounds from P. tuberculatum fruits on P. falciparum and L. guyanensis promastigote growth in vitro were determined. Hemolytic action and cytotoxicity in HepG2 and J774 cells were measured. RESULTS: Three compounds showed strong antiplasmodial activity and one compound showed strong antileishmanial activity. Two compounds were non-toxic to HepG2 cells and all were toxic to J774 cells. The compounds showed no hemolytic activity. CONCLUSIONS: The tested compounds from P. tuberculatum exhibited antiparasitic and cytotoxic effects.
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Antiprotozoários/farmacologia , Frutas/química , Leishmania guyanensis/efeitos dos fármacos , Piper/química , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Antiprotozoários/isolamento & purificação , Células Hep G2/efeitos dos fármacos , Humanos , Concentração Inibidora 50 , Testes de ToxicidadeRESUMO
This study evaluated the species composition of sand flies and identified potential vectors of Leishmania Ross species in rural areas of Porto Velho, Rondônia State, Brazil. American cutaneous leishmaniasis (ACL) is one of the gravest threats to public health in this state. Sand flies were collected over the course of 2014 and 2015 using HP light traps. Polymerase chain reaction was performed by targeting the Leishmania mkDNA region. In total, 2,344 sand flies were collected, from which 45 species, nine subgenera, and five species group were identified. The most abundant species were Lutzomyia antunesi (Coutinho) (n = 597, 25.47%), Lutzomyia ubiquitalis (Mangabeira) (n = 496, 21.16%), and Lutzomyia octavioi (Vargas) (n = 199, 8.49%). The greatest diversity occurred in the forest environment where the most abundant species were L. antunesi (n = 588, 25.07%), L. ubiquitalis (n = 493, 21.02%), L. octavioi (n = 199, 8.49%), and Lutzomyia flaviscutellata (Mangabeira) (n = 132, 5.63%). Two pools of L. ubiquitalis were positive for Leishmania DNA, which suggests that L. ubiquitalis is a putative vector of leishmaniasis in the municipality of Porto Velho.
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Biota , Insetos Vetores/fisiologia , Insetos Vetores/parasitologia , Leishmania/isolamento & purificação , Psychodidae/fisiologia , Psychodidae/parasitologia , Animais , Brasil , DNA de Protozoário/genética , Feminino , Florestas , Pradaria , Masculino , Reação em Cadeia da Polimerase , Dinâmica PopulacionalRESUMO
Abstract Malaria is a disease caused by Plasmodium spp. protozoa. The ability of Plasmodium to develop resistance to current antimalarial drugs makes the study of chemotherapeutic alternatives extremely important. This study aimed to evaluate the antimalarial activity of compound 3286938 (1-(3-benzyloxy-4-methoxy-phenyl)-3-(3,4,5-trimethoxy-phenyl)-propan-1-one), which presents in its structure a 3,4,5-trimethoxyphenyl group, in vitro, using the W2 strain of P. falciparum and against circulating strains of P. vivax and P. falciparum from the state of Rondônia. The compound 3286938 obtained an IC50 of 24.4 µM against the W2 strain of P. falciparum, and against the circulating strains, it presented a median (MD)=38.7 µM for P. vivax and MD=6.7 µM for P. falciparum. As for toxicity, 3286938 showed CC50 > 500 µM for VERO and HepG2 strains with a selectivity index greater than 12.9, a ratio calculated for P. falciparum and P. vivax regarding Vero and HepG2 cells. The compound was not considered hemolytic in in vitro assays, thus indicating the specificity of its antiplasmodial action. Based on the results presented, and considering the unprecedented character of the compound, it can be concluded that 3286938 was shown to be promising for complementary in vitro and in vivo studies aiming to produce effective antiplasmodial action.
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INTRODUCTION:: Malaria and leishmaniasis are prevalent in tropical regions, which have environmental characteristics that are highly favorable to protozoa and vectors of these diseases; the transmission of these infections in sub-tropical regions, although recognized, represents only a small fraction of cases. Plants are constantly being used in the search for and acquisition of new drugs, and many compounds derived from them have been used to combat various diseases. In this study, we evaluated the action of the dichloromethanolic extract of Myrciaria dubia leaves against the protozoa Plasmodium falciparum, Leishmania amazonensis, Leishmania braziliensis, and Leishmania chagasi through bioassays. METHODS: The extract from M. dubia was tested for its anti-P. falciparum activity in an anti-histidine-rich protein II immunosorbent assay. The antileishmanial assays were performed using the resazurin method, while cytotoxicity against human hepatoma (HepG2) strain was determined using the colorimetric MTT [3-(4, 5-dimethyl-2- thiazolyl)-2, 5-diphenyl-2H tetrazolium bromide] method. RESULTS: The M. dubia extract presented a half-maximal inhibitory concentration equal to 2.35 (1.05)µg/mL for P. falciparum, 190.73 (6.41) µg/mL for L. amazonensis, and greater than equal to 200µg/mL for L. chagasi and L. braziliensis strains. The cytotoxic concentration for 50% of the cells was above 500µg/mL for HepG2, indicating no toxicity and greater selectivity against parasites. CONCLUSIONS: The results obtained indicate the presence of antiplasmodial and leishmanicidal bioactive compounds in the dichloromethanolic extracts of M. dubia leaves, and point towards future studies to elucidate the mechanism of action for each physiological effect.
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Antimaláricos/farmacologia , Antiprotozoários/farmacologia , Leishmania/efeitos dos fármacos , Myrtaceae/química , Extratos Vegetais/farmacologia , Plasmodium falciparum/efeitos dos fármacos , Antimaláricos/isolamento & purificação , Antimaláricos/toxicidade , Antiprotozoários/isolamento & purificação , Antiprotozoários/toxicidade , Colorimetria , Células Hep G2/efeitos dos fármacos , Humanos , Técnicas Imunoenzimáticas , Concentração Inibidora 50 , Leishmania/classificação , Testes de Sensibilidade Parasitária , Extratos Vegetais/toxicidadeRESUMO
Trichophoromyia ruifreitasi sp. n. is described as a new species of sand fly from the genus Trichophoromyia Barretto. This description is supported with illustrations and photographs that detail the morphological characteristics of male specimens collected in the municipality of Assis Brasil, Acre State, Brazilian Amazon. This species is similar to Trichophoromyia auraensis (Mangabeira), but the two species can be easily differentiated by the distribution of setae on their parameres, and by the presence of a dorsal lobe in the parameres of the new species.
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BACKGROUND: Phlebotomine sand flies (Diptera: Psychodidae) are insects of medical importance due to the role that some species play in the transmission of leishmaniasis. This work aimed to study some ecological aspects among sand flies fauna inhabiting two different environments: the várzea (lowland Amazonian forest) and terra firme (upland Amazonian forest), both located in Tefé Municipality, Amazonas State, Braziland to detect Leishmania infection in those phlebotomine populations. METHODS: Sand flies were collected using HP light traps. Collection took place over the course of six months: January, February, April, August, September, and October of 2013. To detect natural infection by Leishmania, DNA samples were extracted from female sand flies and submitted to Polymerase Chain Reaction (PCR) targeting the kDNA gene; Leishmania species were identified by PCR-RFLP targeting the hsp70 gene and genetic sequencing. RESULTS: In all, 5,716 individuals were collected, and 46 species were identified. Trichophoromyia ubiquitalis (3,330 - 58.26%) and Nyssomyia antunesi (661 - 11.26%) were the most abundant species. Species richness was greater in terra firme environments (42 species) than in the várzea environments (22 species), and forests ecotopes (43 species) were richer than peridomiciles (28 species). DNA of Leishmania was found in Th. ubiquitalis and Psychodopygus davisi, both of which inhabit the terra firme environment and sequencing analysis confirmed the presence of Leishmania (Viannia) lainsoni DNA in Th. ubiquitalis in Tefé Municipality. CONCLUSIONS: The high abundance of Th. ubiquitalis and Ps. davisi and detection of DNA of Leishmania sp. may indicate that both species could be putative vectors for American Cutaneous Leishmaniasis (ACL) in the terra firme environment of Tefé. The sand fly fauna found in várzea is rich and diverse, exhibiting several species, nevertheless the seasonal hydric stress during part of the year that could influence the local diversity, if compared with other studies. This is the first report in Amazonas State of Th. ubiquitalis with presence of L. (V.) lainsoni DNA.
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Ecossistema , Leishmania/fisiologia , Psychodidae/parasitologia , Animais , Brasil , DNA de Protozoário/genética , Feminino , Regulação da Expressão Gênica , Proteínas de Choque Térmico HSP72/genética , Proteínas de Choque Térmico HSP72/metabolismo , Insetos Vetores/parasitologia , Leishmania/genética , Reação em Cadeia da Polimerase , Polimorfismo de Fragmento de Restrição , Especificidade da EspécieRESUMO
In this study, Leishmania species were identified by Polymerase Chain Reaction (PCR). The epidemiology of patients suspected of having American Cutaneous Leishmaniasis in the municipality of Assis Brasil, Acre State, located in the Brazil/Peru/Bolivia tri-border was also investigated. By PCR, the DNA of Leishmania was detected in 100% of the cases (37 samples) and a PCR-Restriction Fragment Length Polymorphism (RFLP) of the hsp 70 gene identified the species in 32 samples: Leishmania (Viannia) braziliensis (65.6%) , L. (V.) shawi (28.1%) , L. (V.) guyanensis (3.1%) and mixed infection L. (V.) guyanensis and L. (Leishmania) amazonensis(3.1%)This is the first report of L. (V.) shawi and L. (L.) amazonensis in Acre. The two predominant species were found in patients living in urban and rural areas. Most cases were found in males living in rural areas for at least three years and involved in rural work. This suggests, in most cases, a possible transmission of the disease from a rural/forest source, although some patients had not engaged in activities associated with permanence in forestall areas, which indicate a possible sandflies adaptation to the periurban setting.
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Leishmania/classificação , Leishmaniose Cutânea/parasitologia , Leishmaniose Mucocutânea/parasitologia , Adolescente , Adulto , Animais , Brasil/epidemiologia , Criança , Pré-Escolar , Feminino , Humanos , Lactente , Recém-Nascido , Leishmania/genética , Leishmania/isolamento & purificação , Leishmaniose Cutânea/diagnóstico , Leishmaniose Cutânea/epidemiologia , Leishmaniose Mucocutânea/diagnóstico , Leishmaniose Mucocutânea/epidemiologia , Masculino , Reação em Cadeia da Polimerase , Polimorfismo de Fragmento de Restrição , Fatores de Risco , População Rural , População Urbana , Adulto JovemRESUMO
Trichomonas vaginalis and Leishmania spp. are protozoal species responsible for millions of cases of parasitic diseases worldwide. Considering the potential of natural products and the need for more effective and less toxic alternatives to treat trichomoniasis and leishmaniasis, this study aimed to evaluate the effect of two series of triterpenes derivatives with different modifications at C-3 and C-28 positions of the ursolic acid (UA) and betulinic acid (BA) against trophozoites of Trichomonas vaginalis and promastigotes forms of Leishmania (L.) amazonensis. The compounds modified just at C-3 were the most active. The 3β-acetyl betulinic acid (1b) reduced the trophozoites viability of T. vaginalis at 74%, followed by the 3-oxo ursolic acid and 3-oxo betulinic acid (3a and 3b) compounds (55% of reduction). The compound 3β-isobutyl ursolic acid (7a) inhibited the viability of L. amazonensis promastigotes by 55%. Therefore, analyzing the structure-activity relationship and the data of literature, it is possible to suppose that the inclusion of polar groups in the skeletons could improve the antiprotozoal activity. Overall, further studies are necessary to develop triterpenic derivatives with more powerful trichomonicidal and leishmanicidal properties.