A cultura do arroz e uma atividade de importância cada vez maior pela sua utilizacao na alimentac... more A cultura do arroz e uma atividade de importância cada vez maior pela sua utilizacao na alimentacao humana, garantindo alimento suficiente e de qualidade para a populacao. A grande preocupacao e o uso intensivo de pesticidas; principal estrategia no campo para o combate e a prevencao de pragas, e os residuos decorrentes desta pratica. Neste trabalho, desenvolveu-se e validou-se um procedimento analitico, utilizando o metodo de extracao QuEChERS modificado e Cromatografia Gasosa com Deteccao por Captura de Eletrons (GC-ECD) para a determinacao residual dos inseticidas bifentrina e lambda-cialotrina e dos fungicidas azoxistrobina e trifloxistrobina em plantas de arroz. O metodo QuEChERS modificado consistiu em uma etapa de extracao inicial utilizando 3,0 g de plantas de arroz na qual foi adicionado 15 mL de acetonitrila contendo 1% (v/v) de acido acetico, seguida por uma etapa de particao apos a adicao de uma mistura de sais anidros (3 g de sulfato de magnesio e 1,7 g de acetato de so...
Nesta nota e apresentada detalhadamente a metodologia (preparacao dos extratos, adaptacao dos car... more Nesta nota e apresentada detalhadamente a metodologia (preparacao dos extratos, adaptacao dos caramujos, ensaio de atividade, destino dos caramujos) usada para a avaliacao da atividade moluscicida de extratos de plantas frente a caramujos da especie Biomphalaria glabrata. A adaptacao desta metodologia tem o proposito de avaliar extratos naturais para a busca de produtos alternativos mais baratos, biodegradaveis, seguros e disponiveis localmente, para o controle das populacoes de caramujos.
With the advancement of medicine, the vaccine against human papillomavirus (HPV) was developed. H... more With the advancement of medicine, the vaccine against human papillomavirus (HPV) was developed. HPV is a sexually transmitted virus and the vaccine is a skillful means of preventing transmission. However, the vaccine needs to be applied to the at-risk population, young women and men. Therefore, the objective of the present study is to highlight comprehensive studies on the applicability of the vaccine to the population in an efficient manner. The research will approach a wide review of scientific articles published in recent years, the collection will be carried out in the Google Scholar Database, MEDLINE and SciELO, allowing a discourse analysis of the selected works, and thus, building a critical analysis resulting from the information gathered about the population at risk, effectiveness and stigmas of non-vaccination. In a critical analysis, it was corroborated that although vaccination has proven to be effective, the population at risk is not totally immune to the virus, since t...
Currently the accelerated and troubled routine ends up also affecting children and adolescents, w... more Currently the accelerated and troubled routine ends up also affecting children and adolescents, who are still unable to develop, express and assimilate what happens to them, internally and externally, understand their pains and suffering; thus, they end up developing mental disorders, such as depression. Given the importance of seeking more information about depression, this study aimed to produce a bibliographic review article on depression in childhood and adolescence and its characteristics. The databases Pubmed (US National Library of Medicine), Scielo (Scientific Electronic Library Online), and Google ScholarⓇ were used in the present study, using the descriptors: depression, psychotropic drugs, mental disorders and psychotherapy. The articles analyzed were written in Portuguese, English and Spanish, for the past 22 years. For the diagnosis of children or adolescents, the clinical investigation has its particularities, the anamnesis must be more in-depth and it must go beyond t...
According to the World Health Organization, researchers estimate that the spread of vaccines has ... more According to the World Health Organization, researchers estimate that the spread of vaccines has allowed worldwide life expectancy to increase by 30 years in the past two centuries. Despite these advances, there are major challenges to be overcome to expand immunization coverage. Currently, the Unified Health System (SUS) offers a total of 19 vaccines that protect against more than 40 diseases free of charge. Therefore, the objective of the study was to study and analyze the current state of Brazilian vaccination in relation to infectious diseases eradicated in the country. For the development of the work, data from the Ministry of Health, published scientific articles in the Google academic, SCIELO and PubMed databases, epidemiological bulletins, as well as relevant studies and reports published on websites and internet portals through the descriptors, vaccination in Brazil, vaccination delay in Brazil, vaccines available in the single system were used (SUS). Through this work, it ...
Revista do Instituto de Medicina Tropical de São Paulo
This is an open-access article distributed under the terms of the Creative Commons Attribution Li... more This is an open-access article distributed under the terms of the Creative Commons Attribution License.
Continuous efforts have been made to discover new drugs for the treatment of Chagas' disease,... more Continuous efforts have been made to discover new drugs for the treatment of Chagas' disease, human African trypanosomiasis, and leishmaniasis. We have previously reported the synthesis and antileishmanial and antitrypanosomal (Y strain) properties of 2,3-disubstituted quinoxalines. Considering their promising antiparasitic potential, the present study was conducted to expand our search and take advantage of high-throughput assays to investigate the effects of quinoxaline derivatives against Leishmania donovani, Trypanosoma brucei, and Trypanosoma cruzi (Tulahuen strain). These compounds were active against the kinetoplastid parasites that were evaluated. The 2-chloro-3-methylsulfoxylsulfonyl and 2-chloro-3-methylsulfinyl quinoxalines were the most potent, and some of these derivatives were even more active than the reference drugs. Although the 2,3-diaryl-substituted quinoxalines were not active against all of the parasites, they were active against T. brucei and intracellular ...
Leishmaniasis is endemic in 98 countries and territories worldwide. The therapies available for l... more Leishmaniasis is endemic in 98 countries and territories worldwide. The therapies available for leishmaniasis have serious side effects, thus prompting the search for new therapies. The present study investigated the antileishmanial activities of 2,3-diarylsubstituted quinoxaline derivatives againstLeishmania amazonensis. The antiproliferative activities of 6,7-dichloro-2,3-diphenylquinoxaline (LSPN329) and 2,3-di-(4-methoxyphenyl)-quinoxaline (LSPN331) against promastigotes and intracellular amastigotes were assessed, and the cytotoxicities of LSPN329 and LSPN331 were determined. Morphological and ultrastructural alterations were examined by electron microscopy, and biochemical alterations, reflected by the mitochondrial membrane potential (ΔΨm), mitochondrial superoxide anion (O2·−) concentration, the intracellular ATP concentration, cell volume, the level of phosphatidylserine exposure on the cell membrane, cell membrane integrity, and lipid inclusions, were evaluated.In vivoanti...
Quinoxalines belong to the N-containing heterocyclic compounds that stand out as having promising... more Quinoxalines belong to the N-containing heterocyclic compounds that stand out as having promising biological activity due to their privileged scaffold. In this work, we report the synthesis, antileishmanial, and antitrypanosomal properties of 46 new 2,3-disubstituted quinoxaline and 40 previously reported derivatives. Among all of the compounds screened for in vitro activity against epimastigotes and trypomastigotes of Trypanosoma cruzi and promastigotes of Leishmania amazonensis as well as mammalian toxicity on LLCMK2 cells and J774 macrophages, analogues from series 5, 6, 7, 9, 12, and 13 displayed high activity at micromolar IC50 and EC50 concentrations. Sixteen quinoxaline derivatives were selected and evaluated on T. cruzi and/or L. amazonensis amastigotes. The most active compounds were 6a-b and 7d-e, on all evolutive forms of L. amazonensis and T. cruzi evaluated with IC50 values 0.1–0.8 μM on promastigotes and epimastigotes 1.4–8.6 on amastigotes. Compounds 5k, 12b and 13a w...
Evidence-Based Complementary and Alternative Medicine, 2013
Leishmaniasis is a disease that affects millions of people worldwide. The drugs that are availabl... more Leishmaniasis is a disease that affects millions of people worldwide. The drugs that are available for the treatment of this infection exhibit high toxicity and various side effects. Several studies have focused on the development of new chemotherapeutic agents that are less toxic and more effective against trypanosomatids. We investigated the effects ofN-butyl-1-(4-dimethylamino)phenyl-1,2,3,4-tetrahydro-β-carboline-3-carboxamide (C4) and its possible targets againstL. amazonensis. The results showed morphological and ultrastructural alterations, depolarization of the mitochondrial membrane, the loss of cell membrane integrity, and an increase in the formation of mitochondrial superoxide anions inL. amazonensistreated withC4. Our results indicate thatC4is a selective antileishmanial agent, and its effects appear to be mediated by mitochondrial dysfunction.
In the present study, we evaluated the in vitro antiprotozoal activity of a guaianolide (11,13-de... more In the present study, we evaluated the in vitro antiprotozoal activity of a guaianolide (11,13-dehydrocompressanolide) isolated from Tanacetum parthenium against Trypanosoma cruzi and investigated the possible combinational effect of guaianolide and benznidazole. The isolated compound was shown to be effective against T. cruzi, with IC₅₀ values of 18.1±0.8 and 66.6±1.3 μM against the multiplicative epimastigote and amastigote forms, respectively. The best results were obtained against trypomastigotes, with an EC₅₀ of 5.7±0.7 μM. The guaianolide presented no toxicity in LLCMK₂ cells (CC₅₀ of 93.5 μM) and was 16.4-fold more selective for trypomastigotes. The study of the combinational effect of benznidazole and guaianolide revealed the presence of a synergistic effect against the epimastigote form and marginal additive effect against the trypomastigote form. Striking morphological changes were observed in epimastigotes treated with guaianolide, such as thinning and stretching of the cell body and flagellum and changes in the format of the cell body with apparent leakage of the cytoplasmic content in trypomastigote forms. The ultrastructural analysis of epimastigotes revealed the presence of membranes that involved organelles and formation of myelin-like figures. Flow cytometry revealed a cell volume reduction and decrease in mitochondrial membrane potential. However, no major changes in cell membrane integrity were found in the epimastigote form treated with guaianolide.
The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation o... more The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation of its leishmanicidal potential are reported here for the first time. The oil obtained by hydrodistillation was analysed by combination of GC and GC/MS. Thirty-five compounds were identified, representing 91.8% of the oil composition. The oil consists primarily of monoterpenes (37.1%), sesquiterpenes (26.3%) and oxygenated sesquiterpenes (23.9%), myrcene (34.3%), zerumbone (15.8%), bicyclogermacrene (8.9%), α-humulene (4.8%) and germacrene D (4.3%) being the major constituents. Activity against Leishmania infantum was determined using the tetrazolium dye (MTT) colorimetric method. The oil, as well as zerumbone, one of its major constituents, showed significant leishmanicidal activity, with IC 50 values of 19.4 and 9.0 μg/ml, respectively. Cytotoxicity in macrophages cells was evaluated using the MTT colorimetric assay. The EO showed the CC 50 < 10 μg/ml to macrophages cells.
A cultura do arroz e uma atividade de importância cada vez maior pela sua utilizacao na alimentac... more A cultura do arroz e uma atividade de importância cada vez maior pela sua utilizacao na alimentacao humana, garantindo alimento suficiente e de qualidade para a populacao. A grande preocupacao e o uso intensivo de pesticidas; principal estrategia no campo para o combate e a prevencao de pragas, e os residuos decorrentes desta pratica. Neste trabalho, desenvolveu-se e validou-se um procedimento analitico, utilizando o metodo de extracao QuEChERS modificado e Cromatografia Gasosa com Deteccao por Captura de Eletrons (GC-ECD) para a determinacao residual dos inseticidas bifentrina e lambda-cialotrina e dos fungicidas azoxistrobina e trifloxistrobina em plantas de arroz. O metodo QuEChERS modificado consistiu em uma etapa de extracao inicial utilizando 3,0 g de plantas de arroz na qual foi adicionado 15 mL de acetonitrila contendo 1% (v/v) de acido acetico, seguida por uma etapa de particao apos a adicao de uma mistura de sais anidros (3 g de sulfato de magnesio e 1,7 g de acetato de so...
Nesta nota e apresentada detalhadamente a metodologia (preparacao dos extratos, adaptacao dos car... more Nesta nota e apresentada detalhadamente a metodologia (preparacao dos extratos, adaptacao dos caramujos, ensaio de atividade, destino dos caramujos) usada para a avaliacao da atividade moluscicida de extratos de plantas frente a caramujos da especie Biomphalaria glabrata. A adaptacao desta metodologia tem o proposito de avaliar extratos naturais para a busca de produtos alternativos mais baratos, biodegradaveis, seguros e disponiveis localmente, para o controle das populacoes de caramujos.
With the advancement of medicine, the vaccine against human papillomavirus (HPV) was developed. H... more With the advancement of medicine, the vaccine against human papillomavirus (HPV) was developed. HPV is a sexually transmitted virus and the vaccine is a skillful means of preventing transmission. However, the vaccine needs to be applied to the at-risk population, young women and men. Therefore, the objective of the present study is to highlight comprehensive studies on the applicability of the vaccine to the population in an efficient manner. The research will approach a wide review of scientific articles published in recent years, the collection will be carried out in the Google Scholar Database, MEDLINE and SciELO, allowing a discourse analysis of the selected works, and thus, building a critical analysis resulting from the information gathered about the population at risk, effectiveness and stigmas of non-vaccination. In a critical analysis, it was corroborated that although vaccination has proven to be effective, the population at risk is not totally immune to the virus, since t...
Currently the accelerated and troubled routine ends up also affecting children and adolescents, w... more Currently the accelerated and troubled routine ends up also affecting children and adolescents, who are still unable to develop, express and assimilate what happens to them, internally and externally, understand their pains and suffering; thus, they end up developing mental disorders, such as depression. Given the importance of seeking more information about depression, this study aimed to produce a bibliographic review article on depression in childhood and adolescence and its characteristics. The databases Pubmed (US National Library of Medicine), Scielo (Scientific Electronic Library Online), and Google ScholarⓇ were used in the present study, using the descriptors: depression, psychotropic drugs, mental disorders and psychotherapy. The articles analyzed were written in Portuguese, English and Spanish, for the past 22 years. For the diagnosis of children or adolescents, the clinical investigation has its particularities, the anamnesis must be more in-depth and it must go beyond t...
According to the World Health Organization, researchers estimate that the spread of vaccines has ... more According to the World Health Organization, researchers estimate that the spread of vaccines has allowed worldwide life expectancy to increase by 30 years in the past two centuries. Despite these advances, there are major challenges to be overcome to expand immunization coverage. Currently, the Unified Health System (SUS) offers a total of 19 vaccines that protect against more than 40 diseases free of charge. Therefore, the objective of the study was to study and analyze the current state of Brazilian vaccination in relation to infectious diseases eradicated in the country. For the development of the work, data from the Ministry of Health, published scientific articles in the Google academic, SCIELO and PubMed databases, epidemiological bulletins, as well as relevant studies and reports published on websites and internet portals through the descriptors, vaccination in Brazil, vaccination delay in Brazil, vaccines available in the single system were used (SUS). Through this work, it ...
Revista do Instituto de Medicina Tropical de São Paulo
This is an open-access article distributed under the terms of the Creative Commons Attribution Li... more This is an open-access article distributed under the terms of the Creative Commons Attribution License.
Continuous efforts have been made to discover new drugs for the treatment of Chagas' disease,... more Continuous efforts have been made to discover new drugs for the treatment of Chagas' disease, human African trypanosomiasis, and leishmaniasis. We have previously reported the synthesis and antileishmanial and antitrypanosomal (Y strain) properties of 2,3-disubstituted quinoxalines. Considering their promising antiparasitic potential, the present study was conducted to expand our search and take advantage of high-throughput assays to investigate the effects of quinoxaline derivatives against Leishmania donovani, Trypanosoma brucei, and Trypanosoma cruzi (Tulahuen strain). These compounds were active against the kinetoplastid parasites that were evaluated. The 2-chloro-3-methylsulfoxylsulfonyl and 2-chloro-3-methylsulfinyl quinoxalines were the most potent, and some of these derivatives were even more active than the reference drugs. Although the 2,3-diaryl-substituted quinoxalines were not active against all of the parasites, they were active against T. brucei and intracellular ...
Leishmaniasis is endemic in 98 countries and territories worldwide. The therapies available for l... more Leishmaniasis is endemic in 98 countries and territories worldwide. The therapies available for leishmaniasis have serious side effects, thus prompting the search for new therapies. The present study investigated the antileishmanial activities of 2,3-diarylsubstituted quinoxaline derivatives againstLeishmania amazonensis. The antiproliferative activities of 6,7-dichloro-2,3-diphenylquinoxaline (LSPN329) and 2,3-di-(4-methoxyphenyl)-quinoxaline (LSPN331) against promastigotes and intracellular amastigotes were assessed, and the cytotoxicities of LSPN329 and LSPN331 were determined. Morphological and ultrastructural alterations were examined by electron microscopy, and biochemical alterations, reflected by the mitochondrial membrane potential (ΔΨm), mitochondrial superoxide anion (O2·−) concentration, the intracellular ATP concentration, cell volume, the level of phosphatidylserine exposure on the cell membrane, cell membrane integrity, and lipid inclusions, were evaluated.In vivoanti...
Quinoxalines belong to the N-containing heterocyclic compounds that stand out as having promising... more Quinoxalines belong to the N-containing heterocyclic compounds that stand out as having promising biological activity due to their privileged scaffold. In this work, we report the synthesis, antileishmanial, and antitrypanosomal properties of 46 new 2,3-disubstituted quinoxaline and 40 previously reported derivatives. Among all of the compounds screened for in vitro activity against epimastigotes and trypomastigotes of Trypanosoma cruzi and promastigotes of Leishmania amazonensis as well as mammalian toxicity on LLCMK2 cells and J774 macrophages, analogues from series 5, 6, 7, 9, 12, and 13 displayed high activity at micromolar IC50 and EC50 concentrations. Sixteen quinoxaline derivatives were selected and evaluated on T. cruzi and/or L. amazonensis amastigotes. The most active compounds were 6a-b and 7d-e, on all evolutive forms of L. amazonensis and T. cruzi evaluated with IC50 values 0.1–0.8 μM on promastigotes and epimastigotes 1.4–8.6 on amastigotes. Compounds 5k, 12b and 13a w...
Evidence-Based Complementary and Alternative Medicine, 2013
Leishmaniasis is a disease that affects millions of people worldwide. The drugs that are availabl... more Leishmaniasis is a disease that affects millions of people worldwide. The drugs that are available for the treatment of this infection exhibit high toxicity and various side effects. Several studies have focused on the development of new chemotherapeutic agents that are less toxic and more effective against trypanosomatids. We investigated the effects ofN-butyl-1-(4-dimethylamino)phenyl-1,2,3,4-tetrahydro-β-carboline-3-carboxamide (C4) and its possible targets againstL. amazonensis. The results showed morphological and ultrastructural alterations, depolarization of the mitochondrial membrane, the loss of cell membrane integrity, and an increase in the formation of mitochondrial superoxide anions inL. amazonensistreated withC4. Our results indicate thatC4is a selective antileishmanial agent, and its effects appear to be mediated by mitochondrial dysfunction.
In the present study, we evaluated the in vitro antiprotozoal activity of a guaianolide (11,13-de... more In the present study, we evaluated the in vitro antiprotozoal activity of a guaianolide (11,13-dehydrocompressanolide) isolated from Tanacetum parthenium against Trypanosoma cruzi and investigated the possible combinational effect of guaianolide and benznidazole. The isolated compound was shown to be effective against T. cruzi, with IC₅₀ values of 18.1±0.8 and 66.6±1.3 μM against the multiplicative epimastigote and amastigote forms, respectively. The best results were obtained against trypomastigotes, with an EC₅₀ of 5.7±0.7 μM. The guaianolide presented no toxicity in LLCMK₂ cells (CC₅₀ of 93.5 μM) and was 16.4-fold more selective for trypomastigotes. The study of the combinational effect of benznidazole and guaianolide revealed the presence of a synergistic effect against the epimastigote form and marginal additive effect against the trypomastigote form. Striking morphological changes were observed in epimastigotes treated with guaianolide, such as thinning and stretching of the cell body and flagellum and changes in the format of the cell body with apparent leakage of the cytoplasmic content in trypomastigote forms. The ultrastructural analysis of epimastigotes revealed the presence of membranes that involved organelles and formation of myelin-like figures. Flow cytometry revealed a cell volume reduction and decrease in mitochondrial membrane potential. However, no major changes in cell membrane integrity were found in the epimastigote form treated with guaianolide.
The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation o... more The composition of the essential oil (EO) from leaves of Vernonia polyanthes and the evaluation of its leishmanicidal potential are reported here for the first time. The oil obtained by hydrodistillation was analysed by combination of GC and GC/MS. Thirty-five compounds were identified, representing 91.8% of the oil composition. The oil consists primarily of monoterpenes (37.1%), sesquiterpenes (26.3%) and oxygenated sesquiterpenes (23.9%), myrcene (34.3%), zerumbone (15.8%), bicyclogermacrene (8.9%), α-humulene (4.8%) and germacrene D (4.3%) being the major constituents. Activity against Leishmania infantum was determined using the tetrazolium dye (MTT) colorimetric method. The oil, as well as zerumbone, one of its major constituents, showed significant leishmanicidal activity, with IC 50 values of 19.4 and 9.0 μg/ml, respectively. Cytotoxicity in macrophages cells was evaluated using the MTT colorimetric assay. The EO showed the CC 50 < 10 μg/ml to macrophages cells.
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