17 research outputs found

    Desenvolvimento de uma nanoformulação com alumínio-cloro-ftalocianina e paromomicina para tratamento da leishmaniose

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    Tese (Doutorado) — Universidade de Brasília, Instituto de Ciências Biológicas, Programa de Pós-Graduação em Nanociência e Nanobiotecnologia, 2016.A leishmaniose é um problema de saúde pública em países em desenvolvimento. O tratamento dessa doença baseia-se principalmente no uso de antimoniais pentavalentes, em casos de falha terapêutica drogas como o Pentostam e a Anfotericina B tem sido utilizadas. Entretanto, a elevada toxicidade desses compostos e a geração de resistência a eles tem limitado o tratamento dessa doença, o que sugere o desenvolvimento de terapias mais efetivas. Por isso, realizou-se esta tese cujo objetivo principal consistiu no desenvolvimento de uma nanoformulação contendo o fotossensibilizante Alumínio-Cloro-Ftalocianina e o antibiótico Paromomicina para ser utilizada no tratamento da Leishmaniose Cutânea por meio de Terapia Fotodinâmica. A nanoemulsão O/A de AlClFt e Paromomicina foi preparada por meio do método de emulsificação espontânea, sendo que depois de caracterizada e ter a sua estabilidade determinada, o sistema de nanoemulsão foi testado quanto a capacidade de apresentar efeito antiparasitário em promastigotas, amastigotas intracelulares de L. braziliensis e células THP-1 diferenciadas, antes e depois da Terapia Fotodinâmica (5 joules/cm2) durante 24 horas; os resultados foram expressos como percentagens de inibição e concentração inibitória 50 e 90 (CI50, CI90) e como concentração citotóxica 50 e 90 (CC50 e CC90). Além disso, determinou-se ex vivo, em pele de camundongos Balb/c, a capacidade de permeação e de retenção dos sistemas de nanoemulsão mediante o sistema de células de Franz e tape stripping, respetivamente. Adicionalmente, camundongos Balb/c foram tratados topicamente na base da cauda com os nanoconjugados durante 15 dias usando terapia fotodinâmica, após de seis dias do término do tratamento; fígado, pele, baço e rim foram extraídos para a análise da biodistribuição da AlClFt e PM por espectrofluorometria e cromatografia líquida de alto desempenho, respetivamente. Além disso, medula óssea dos camundongos foi analisada para avaliação de formação de micronúcleos nos eritrócitos policromatófilos; sangue intracardíaca foi extraído para análise hemograma. Os resultados mostraram sistemas de nanoemulsão O/A com diâmetros hidrodinâmicos 90% do crescimento de promastigotas e amastigotas intracelulares de L. braziliensis após da terapia fotodinâmica em concentrações onde não foi observado toxicidade nas células hospedeiras, mostrando seletividade. Por outro lado, em ex vivo e in vivo, a AlClFt não foi capaz de permear a pele de camundongos Balb/c. Já a PM no nanoconjugado, permeou até 86 vezes mais do que a PM livre após de 6 horas em sistemas ex vivo. A PM acumulou-se mais no baço. Os sistemas de nanoemulsão não foram genotóxico, tampouco causaram irritabilidade, vermelhidão e laceração durante e após do tratamento tópico. A análise do hemograma mostrou diminuição na contagem de plaquetas da maioria dos camundongos, as outras células do sangue não foram alteradas. Estes resultados, além de originais, propõem um nanoconjugado promissor para ser utilizado no modelo murino de Leishmaniasis cutânea.Leishmaniasis is still a public health problem in developing countries, which have morbidity on the increase. Pentavalent antimonials are still the mainstay of treatment, although in cases of therapeutic failure, another drugs such as Pentostan, and Amphotericin B, among others, are considered. However, the effectiveness of this therapy is limited due to its high toxicity, the emergence of acquired resistance, route of administration and prolonged lenght of therapy. For the above, the search for new drugs is a focus in investigation, actually. In order to formulate an alternative antileishamanial therapy, in this thesis is proposed the use of nanobiotechnology to optimize the combined effect of photodynamic therapy with aluminiumphthalocyanine chloride (AlClFt) and Paramomycin (PM), an antibiotic used to the treatment of the leishmaniasis in the Old world. If this nanoconjugate is active against the parasite, is not toxic and its nanoconjugated are able to penetrate layers of skin of mices, it could be used as a murine model of cutaneous leishamaniasis, in subsequent studies. According to above, the main objective of this thesis was to develop a nano-formulation of aluminium-phthalocyanine chloride and Paramomicyn for the treatment of cutaneous leishmaniasis using photodynamic therapy.The oil/water (O/W) nanoemulsion of AlClFt and Paramomycin was prepared using the spontaneous emulsification method. Also, nanoemulsions with each individuals compounds and vehicles were prepared. The colloidal characterization of theses nanosystems was made by measuring the hydrodynamic diameter and determining polydispersity index and zeta potential by dynamic light scattering and electrophoretic mobility, respectively. Furthemore, physicochemical caracterization was performed to determine the absorption and emission spectra (excited 350nm) of AlClFt present in the nanosystem. pH, reactive oxygen species and stabylity at 4ºC during four months were also determined. Promastigotes and intracelular amastigotes of Leishamania braziliensis and differentiated tHP-1 cells were treated with each of different nanoemulsion systems, before and after photodynamic therapy (5 joules/cm2), during 24 hours. The results were expressed as inhibition percents and 50 and 90% inhibitory concentration (IC50 and IC90). Permeability and ex vivo retention in skin of Balb/c mice of nanoemulsions were tested by Franz cells and tape stripping systems, respectively. In addition, Balb/c mice were treated topically with the nanoconjugates during 15 days. 6 days after treatment finished, liver, skin, spleen and kidney were extracted in order to analyze the AlClFt and PM biodistribution by spectrophotometry and High performance liquid cromatography (HPLC), respectively. Also, bone marrow of mice was analyzed to detect micronucleous in polychromatic erithrocytes. It was obtained intracardiac blood to hematologic analysis. The O/W nanoemulsion systems showed hydrodynamic diameters 90% of promastigotes and intracellular promastigotes of L. braziliensis after photodynamyc therapy using no toxic concentrations for host cells, showing selectivity. Moreover, In ex vivo and in vivo systems, AlClFt did not able to penetrate a skin of Balb/c mice while PM nanoconjugate penetrate 86 fold more than PM free, after 6 hours in ex vivo systems. In vivo assays, concentrations up 292.96M were detected in spleen of treated animals. The nanoemulsion system did not show genotoxicity neither irritability, redness nor tearing during and after topic treatment. Decreased platelet count was recorded in most of mice. Another blood cells were not altered. These results suggest a promissory nanoconjugate to be used in the murine model of cutaneous Leishmaniasis

    Actividad antiparasitaria de nuevas dihidrodibenzo[c,f]tiazolo[3,2-a] azepin-3(2H)-onas contra Leishmania chagasi y Trypanosoma cruzi

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    RESUMEN INTRODUCCIÓN: La leishmaniasis y la enfermedad de Chagas son consideradas como problemas de salud pública en varios países, y nuevas estrategias quimioterapéuticas son necesarias para el control de estas enfermedades. OBJETIVO: El objetivo de este trabajo fue evaluar in vitro la actividad antiparasitaria de 7 nuevas dihidrodibenzo[c,f]tiazolo[3,2-a]azepin-3(2H)-onas contra Leishmania chagasi, Trypanosoma cruzi, y la citotoxicidad sobre las células de mamìfero Vero y THP-1. MATERIALES Y MÉTODOS: La actividad antiparasitaria se determinó microscópicamente por conteo directo de parásitos vivos en comparación con el control no tratado, y la citotoxicidad en células de mamífero por el método colorimétrico de MTT. Las formas extracelulares e intracelulares de los parásitos utilizados así como las células de mamífero, fueron tratadas con diferentes concentraciones de los compuestos (0,3-600 µM) por 3-5 días. Los resultados de actividad de los compuestos fueron expresados en concentración inhibitoria (CI50) y concentración citotóxica (CC50). RESULTADOS: En T. cruzi, 4 compuestos (4a, 4b, 4d, 4g) fueron activos contra epimastigotes con rangos de actividad de CI50 entre 11,28-32,66 µM, y tres (4a, 4c, 4g) contra la forma intracelular (CI50= 18,42-23,62 µM), sin presentar toxicidad en células de mamífero. En L. chagasi, seis compuestos (4a-d, 4g) fueron activos contra promastigotes con CI50 entre 8,27-28,59 µM. El compuesto 4d fue parcialmente activo contra amastigotes intracelulares de L. chagasi (CI50= 59,36 µM). CONCLUSIONES: Los compuestos 4a y 4g presentaron actividad in vitro contra L. chagasi y T. cruzi y baja toxicidad en células de mamífero. Estudios posteriores con los compuestos activos encontrados, de genotoxicidad, mecanismos de acción y de evaluación de su actividad en modelos experimentales, son necesarios para establecer su posible uso como antiparasitarios. Palabras clave: Leishmania chagasi, Trypanosoma cruzi, toxicidad, dihidrodibenzo[c,f]tiazolo[3,2-a] azepin-3(2H)-onas, células Vero y células THP-1 ABSTRACT INTRODUCTION: Leishmaniasis and Chagas disease are considered public health problems in several countries and new chemotherapeutic approaches are needed to control these diseases. OBJETIVE: The aim of this study was to evaluate the antiparasitic activity of 7 new dihydrodibenzo[c,f]thiazolo[3.2-a]azepin-3(2H)-ones on Leishmania chagasi, Trypanosoma cruzi, and the cytotoxicity on Vero and THP-1 cells.  MATERIALS AND METHODS: The antiparasitic activities were determined microscopically counting living parasites compared with untreated control, and the mammalian cell toxicities using the MTT colorimetric test. (Extracellular and intracellular forms of the parasites used and mammalian cells were treated with different concentrations (0.3-600 µM) of compounds for 3-5 days). The activities of the compounds were expressed as the concentration to inhibit 50% percent of parasites (IC50) and the concentration to kill 50% of the mammalian cells (CC50). RESULTS: 4 compounds (4a, 4b, 4d, 4g) were active against T. cruzi epimastigotes with ranges of IC50 from 11.28 to 32.66 μM, and three (4a, 4c, 4g) inhibited the intracellular form (IC50 = 18.42-23.62 μM), with low toxicity on mammalian cells. In L. chagasi, 6 compounds (4a-d, 4g) were active against promastigote forms (IC50= 8.27-28.59 μM). Compound 4d was partially active against intracellular amastigotes of L. chagasi (IC50= 59.36 μM). CONCLUSIONS: The compounds 4a and 4g were actives on both T. cruzi and L. chagasi parasites with low toxicity on mammalian cells. Further studies of genotoxicity, mechanisms of action and evaluation of its activity in experimental models are necessaries.  Keywords: Leishmania chagasi, Trypanosoma cruzi, toxicity, dihydrodibenzo[c,f]-thiazolo[3,2-a]azepin-3(2H)-ones, Vero and THP-1 cell

    Actividad antiparasitaria de nuevas dihidrodibenzo[c,f]tiazolo[3,2-a] azepin-3(2H)-onas contra Leishmania chagasi y Trypanosoma cruzi

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    RESUMEN INTRODUCCIÓN: La leishmaniasis y la enfermedad de Chagas son consideradas como problemas de salud pública en varios países, y nuevas estrategias quimioterapéuticas son necesarias para el control de estas enfermedades. OBJETIVO: El objetivo de este trabajo fue evaluar in vitro la actividad antiparasitaria de 7 nuevas dihidrodibenzo[c,f]tiazolo[3,2-a]azepin-3(2H)-onas contra Leishmania chagasi, Trypanosoma cruzi, y la citotoxicidad sobre las células de mamìfero Vero y THP-1. MATERIALES Y MÉTODOS: La actividad antiparasitaria se determinó microscópicamente por conteo directo de parásitos vivos en comparación con el control no tratado, y la citotoxicidad en células de mamífero por el método colorimétrico de MTT. Las formas extracelulares e intracelulares de los parásitos utilizados así como las células de mamífero, fueron tratadas con diferentes concentraciones de los compuestos (0,3-600 µM) por 3-5 días. Los resultados de actividad de los compuestos fueron expresados en concentración inhibitoria (CI50) y concentración citotóxica (CC50). RESULTADOS: En T. cruzi, 4 compuestos (4a, 4b, 4d, 4g) fueron activos contra epimastigotes con rangos de actividad de CI50 entre 11,28-32,66 µM, y tres (4a, 4c, 4g) contra la forma intracelular (CI50= 18,42-23,62 µM), sin presentar toxicidad en células de mamífero. En L. chagasi, seis compuestos (4a-d, 4g) fueron activos contra promastigotes con CI50 entre 8,27-28,59 µM. El compuesto 4d fue parcialmente activo contra amastigotes intracelulares de L. chagasi (CI50= 59,36 µM). CONCLUSIONES: Los compuestos 4a y 4g presentaron actividad in vitro contra L. chagasi y T. cruzi y baja toxicidad en células de mamífero. Estudios posteriores con los compuestos activos encontrados, de genotoxicidad, mecanismos de acción y de evaluación de su actividad en modelos experimentales, son necesarios para establecer su posible uso como antiparasitarios. Palabras clave: Leishmania chagasi, Trypanosoma cruzi, toxicidad, dihidrodibenzo[c,f]tiazolo[3,2-a] azepin-3(2H)-onas, células Vero y células THP-1 ABSTRACT INTRODUCTION: Leishmaniasis and Chagas disease are considered public health problems in several countries and new chemotherapeutic approaches are needed to control these diseases. OBJETIVE: The aim of this study was to evaluate the antiparasitic activity of 7 new dihydrodibenzo[c,f]thiazolo[3.2-a]azepin-3(2H)-ones on Leishmania chagasi, Trypanosoma cruzi, and the cytotoxicity on Vero and THP-1 cells.  MATERIALS AND METHODS: The antiparasitic activities were determined microscopically counting living parasites compared with untreated control, and the mammalian cell toxicities using the MTT colorimetric test. (Extracellular and intracellular forms of the parasites used and mammalian cells were treated with different concentrations (0.3-600 µM) of compounds for 3-5 days). The activities of the compounds were expressed as the concentration to inhibit 50% percent of parasites (IC50) and the concentration to kill 50% of the mammalian cells (CC50). RESULTS: 4 compounds (4a, 4b, 4d, 4g) were active against T. cruzi epimastigotes with ranges of IC50 from 11.28 to 32.66 μM, and three (4a, 4c, 4g) inhibited the intracellular form (IC50 = 18.42-23.62 μM), with low toxicity on mammalian cells. In L. chagasi, 6 compounds (4a-d, 4g) were active against promastigote forms (IC50= 8.27-28.59 μM). Compound 4d was partially active against intracellular amastigotes of L. chagasi (IC50= 59.36 μM). CONCLUSIONS: The compounds 4a and 4g were actives on both T. cruzi and L. chagasi parasites with low toxicity on mammalian cells. Further studies of genotoxicity, mechanisms of action and evaluation of its activity in experimental models are necessaries.  Keywords: Leishmania chagasi, Trypanosoma cruzi, toxicity, dihydrodibenzo[c,f]-thiazolo[3,2-a]azepin-3(2H)-ones, Vero and THP-1 cell

    Actividad contra Trypanosoma cruzi, Leishmania chagasi y células de mamífero de nuevas N-bencil (2-furilmetil) cinamamidas

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    RESUMENINTRODUCCIÓN: La quimioterapia contra la leishmaniasis y la enfermedad de Chagas es inefectiva, condición que agrava el problema de salud pública que estas enfermedades tropicales representan.OBJETIVO: Determinar la actividad de nuevas N-bencil (2-furilmetil) cinamamidas en las formas libres e intracelulares de Leismania chagasi y Trypanosoma cruzi y en células Vero y THP-1.MATERIALES Y MÉTODOS: Los parásitos y las células fueron tratados con diferentes concentraciones de los compuestos y su actividad fue determinada microscópicamente y por la prueba colorimétrica de MTT en el caso de los parásitos y células de mamífero, respectivamente. Los resultados de actividad fueron expresados como la concentración que inhibe o destruye 50% o 90% de los parásitos o células.RESULTADOS: Las N-arilalquilamidas 1, 2 y 5 fueron activos en epimastigotes de T. cruzi con actividades entre CI50 3,71-38,81 µM y CI90 entre 50,87-59,87 µM. El compuesto 2 presentó actividad en amastigotes intracelulares de L. chagasi con CI50 77,76 µM. Las amidas preparadas no presentaron toxicidad en células THP-1 y solo el compuesto 4 fue parcialmente tóxico en células Vero (CC50 65,90 ± 5,71 µM).CONCLUSIONES: La baja toxicidad presentada por los compuestos 1, 2 y 5 y la actividad antiparasitaria mostrada soportan el diseño de nuevas moléculas relacionadas para ser evaluadas en sistemas in vitro e in vivo contra estas enfermedades parasitarias.Palabras clave: Leishmaniasis, enfermedad de Chagas, amastigotes intracelulares, citotoxicidad, cinamamidas N-sustituidasABSTRACTINTRODUCTION: The chemotherapy against leishmaniasis and Chagas disease is ineffective, a condition that is aggravating the public health problem caused by these tropical diseases.OBJECTIVE: To determine the activity of new 7V-benzyl(2-furylmethyl) cinnamamides in the free and intracellular forms of Leishmania chagasi and Trypanosoma cruzi and Vero and THP-1 cells.MATERIALS AND METHODS: The parasites and cells were treated with different concentrations of the compounds and the activity was determined microscopically and MTT colorimetric test in the case of parasites and mammalian cells. Antiparasitic activity of tested compounds was expressed as the concentration that inhibits or destroys 50% or 90% of parasites and cells.RESULTS: The 7V-arylalkylamides 1, 2 and 5 were active against T. cruzi epimastigotes with a range of activities between IC50 3.71-38.81 μM and IC90 between 50.87-59.87 μM. The compound 2 was active on intracellular amastigotes of L. chagasi with IC50 77.76 μM. The tested amides were not toxic to THP-1 cells; just only compound 4 resulted partially toxic on Vero cells (CC50 65.9 ± 5.71 μM).CONCLUSIONS: The low toxicity and the antiparasitic activity showed by the cinnamanide compounds 1, 2 and 5 support the design of new related molecules in order to be evaluated on in vitro and in vivo systems for these parasitic diseases.Keywords: Leishmaniasis, Chagas disease, intracellular amastigote, cytotoxicity, N-substituted cinnamamide

    Actividad contra Trypanosoma cruzi, Leishmania chagasi y células de mamífero de nuevas N-bencil (2-furilmetil) cinamamidas

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    RESUMENINTRODUCCIÓN: La quimioterapia contra la leishmaniasis y la enfermedad de Chagas es inefectiva, condición que agrava el problema de salud pública que estas enfermedades tropicales representan.OBJETIVO: Determinar la actividad de nuevas N-bencil (2-furilmetil) cinamamidas en las formas libres e intracelulares de Leismania chagasi y Trypanosoma cruzi y en células Vero y THP-1.MATERIALES Y MÉTODOS: Los parásitos y las células fueron tratados con diferentes concentraciones de los compuestos y su actividad fue determinada microscópicamente y por la prueba colorimétrica de MTT en el caso de los parásitos y células de mamífero, respectivamente. Los resultados de actividad fueron expresados como la concentración que inhibe o destruye 50% o 90% de los parásitos o células.RESULTADOS: Las N-arilalquilamidas 1, 2 y 5 fueron activos en epimastigotes de T. cruzi con actividades entre CI50 3,71-38,81 µM y CI90 entre 50,87-59,87 µM. El compuesto 2 presentó actividad en amastigotes intracelulares de L. chagasi con CI50 77,76 µM. Las amidas preparadas no presentaron toxicidad en células THP-1 y solo el compuesto 4 fue parcialmente tóxico en células Vero (CC50 65,90 ± 5,71 µM).CONCLUSIONES: La baja toxicidad presentada por los compuestos 1, 2 y 5 y la actividad antiparasitaria mostrada soportan el diseño de nuevas moléculas relacionadas para ser evaluadas en sistemas in vitro e in vivo contra estas enfermedades parasitarias.Palabras clave: Leishmaniasis, enfermedad de Chagas, amastigotes intracelulares, citotoxicidad, cinamamidas N-sustituidasABSTRACTINTRODUCTION: The chemotherapy against leishmaniasis and Chagas disease is ineffective, a condition that is aggravating the public health problem caused by these tropical diseases.OBJECTIVE: To determine the activity of new 7V-benzyl(2-furylmethyl) cinnamamides in the free and intracellular forms of Leishmania chagasi and Trypanosoma cruzi and Vero and THP-1 cells.MATERIALS AND METHODS: The parasites and cells were treated with different concentrations of the compounds and the activity was determined microscopically and MTT colorimetric test in the case of parasites and mammalian cells. Antiparasitic activity of tested compounds was expressed as the concentration that inhibits or destroys 50% or 90% of parasites and cells.RESULTS: The 7V-arylalkylamides 1, 2 and 5 were active against T. cruzi epimastigotes with a range of activities between IC50 3.71-38.81 μM and IC90 between 50.87-59.87 μM. The compound 2 was active on intracellular amastigotes of L. chagasi with IC50 77.76 μM. The tested amides were not toxic to THP-1 cells; just only compound 4 resulted partially toxic on Vero cells (CC50 65.9 ± 5.71 μM).CONCLUSIONS: The low toxicity and the antiparasitic activity showed by the cinnamanide compounds 1, 2 and 5 support the design of new related molecules in order to be evaluated on in vitro and in vivo systems for these parasitic diseases.Keywords: Leishmaniasis, Chagas disease, intracellular amastigote, cytotoxicity, N-substituted cinnamamide

    Educomunicação, Transformação Social e Desenvolvimento Sustentável

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    Esta publicação apresenta os principais trabalhos dos GTs do II Congresso Internacional de Comunicação e Educação nos temas Transformação social, com os artigos que abordam principalmente Educomunicação e/ou Mídia-Educação, no contexto de políticas de diversidade, inclusão e equidade; e, em Desenvolvimento Sustentável os artigos que abordam os avanços da relação comunicação/educação no contexto da educação ambiental e desenvolvimento sustentável

    A multi-country test of brief reappraisal interventions on emotions during the COVID-19 pandemic.

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    The COVID-19 pandemic has increased negative emotions and decreased positive emotions globally. Left unchecked, these emotional changes might have a wide array of adverse impacts. To reduce negative emotions and increase positive emotions, we tested the effectiveness of reappraisal, an emotion-regulation strategy that modifies how one thinks about a situation. Participants from 87 countries and regions (n = 21,644) were randomly assigned to one of two brief reappraisal interventions (reconstrual or repurposing) or one of two control conditions (active or passive). Results revealed that both reappraisal interventions (vesus both control conditions) consistently reduced negative emotions and increased positive emotions across different measures. Reconstrual and repurposing interventions had similar effects. Importantly, planned exploratory analyses indicated that reappraisal interventions did not reduce intentions to practice preventive health behaviours. The findings demonstrate the viability of creating scalable, low-cost interventions for use around the world

    Actividad contra Trypanosoma cruzi, Leishmania chagasi y células de mamífero de nuevas N-bencil (2-furilmetil) cinamamidas Activity against Trypanosoma cruzi, Leishmania chagasi and mammalian cells of new N-benzyl (2-furylmethyl) cinnamamides

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    Introducción: La quimioterapia contra la leishmaniasis y la enfermedad de Chagas es inefectiva, condición que agrava el problema de salud pública que estas enfermedades tropicales representan. Objetivo: Determinar la actividad de nuevas N-bencil (2-furilmetil) cinamamidas en las formas libres e intracelulares de Leismania chagasi y Trypanosoma cruzi y en células Vero y THP-1. Materiales y métodos: Los parásitos y las células fueron tratados con diferentes concentraciones de los compuestos y su actividad fue determinada microscópicamente y por la prueba colorimétrica de MTT en el caso de los parásitos y células de mamífero, respectivamente. Los resultados de actividad fueron expresados como la concentración que inhibe o destruye 50% o 90% de los parásitos o células. Resultados: Las N-arilalquilamidas 1, 2 y 5 fueron activos en epimastigotes de T. cruzi con actividades entre IC50 3,71-38,81 μM y IC90 entre 50,87-59,87 μM. El compuesto 2 presentó actividad en amastigotes intracelulares de L. chagasi con IC50 77,76 μM. Las amidas preparadas no presentaron toxicidad en células THP-1 y solo el compuesto 4 fue parcialmente tóxico en células Vero (CC50 65,90 ± 5,71 μM). Conclusiones: La baja toxicidad presentada por los compuestos 1, 2 y 5 y la actividad antiparasitaria mostrada soportan el diseño de nuevas moléculas relacionadas para ser evaluadas en sistemas in vitro e in vivo contra estas enfermedades parasitarias. Salud UIS 2009; 41: 275-279Introduction: The chemotherapy against leishmaniasis and Chagas disease is ineffective, a condition that is aggravating the public health problem caused by these tropical diseases. Objective: To determine the activity of new N-benzyl(2-furylmethyl) cinnamamides in the free and intracellular forms of Leishmania chagasi and Trypanosoma cruzi and Vero and THP-1 cells. Materials and methods: The parasites and cells were treated with different concentrations of the compounds and the activity was determined microscopically and MTT colorimetric test in the case of parasites and mammalian cells. Antiparasitic activity of tested compounds was expressed as the concentration that inhibits or destroys 50% or 90% of parasites and cells. Results: The N-arylalkylamides 1, 2 and 5 were active against T. cruzi epimastigotes with a range of activities between IC50 3.71-38.81 μM and IC90 between 50.87-59.87 μM. The compound 2 was active on intracellular amastigotes of L. chagasi with IC50 77.76 μM. The tested amides were not toxic to THP-1 cells; just only compound 4 resulted partially toxic on Vero cells (CC50 65.9 ± 5.71 μM). Conclusions: The low toxicity and the antiparasitic activity showed by the cinnamanide compounds 1, 2 and 5 support the design of new related molecules in order to be evaluated on in vitro and in vivo systems for these parasitic diseases. Salud UIS 2009; 41: 275-279
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