Procedimentos estéticos com ênfase na queda capilar / Aesthetic procedures with emphasis on hair loss / Procedimientos estéticos con énfasis en la caída del cabello

A beleza está diretamente ligada ao aspecto dos cabelos, em todos os tempos e todas as culturas. O cabelo ao longo da vida é sujeito a vários tipos de mudanças, sejam elas naturais ou artificiais, conduzidas por uma vontade de mudar, muitas vezes, seja por representar uma nova fase, como também é símbolo de autocuidado, vaidade, sucesso, possuem significativa importância na aparência e autoestima das pessoas e, por isso, a queda capilar pode atingir a qualidade de vida do indivíduo. Neste sentido, o objetivo deste estudo foi avaliar procedimentos estéticos minimamente invasivos e não cirúrgicos com ênfase na queda capilar. Para tanto, foi realizada uma revisão bibliográfica integrativa, de caráter descritivo nas principais bases de dados em saúde: SciELO, Google Acadêmico, PubMed e livros de medicina, nos idiomas português, inglês e espanhol, considerando o período de 2007 a 2022. De acordo com o último censo da Sociedade Brasileira de Dermatologia, a queixa de alopecia está entre as dez mais frequentes nos consultórios dermatológicos. As doenças capilares mais importantes estão divididas em dois grupos, as cicatriciais quando a perda de cabelo é acompanhada por cicatrizes resultando em calvície permanente, e as não cicatriciais onde a calvície não é permanente levando a diminuição e o afinamento gradual do cabelo. A alopecia não cicatricial é a mais frequente e as mais comuns entre elas são a alopecia androgenética e o eflúvio telógeno. Muitos pacientes procuram tratamento para melhorar a aparência e a autoestima, que podem estar relacionados a quadros de ansiedade e depressão. Esses tratamentos devem ser individualizados, onde se deve avaliar as características individuais de cada paciente. Os tratamentos capilares estéticos podem contribuir de forma significativa para a redução da baixa autoestima, contribuindo para recuperação da autoconfiança através do crescimento capilar proporcionado pela estética. Sendo assim, conclui-se que os resultados coletados na revisão de literatura foram satisfatórios, de forma onde mostra que os medicamentos, suplementos e tratamentos estéticos na queda capilar vem evoluindo cada vez mais. Contudo, mais estudos acerca do assunto são necessários.

Beauty is directly linked to the appearance of hair, in all times and all cultures. Hair throughout life is subject to various types of changes, whether natural or artificial, driven by a desire to change, often because it represents a new phase, as it is also a symbol of self-care, vanity, success, they have significant importance in people's appearance and self-esteem and, therefore, hair loss can affect the individual's quality of life. In this sense, the objective of this study was to evaluate minimally invasive and non- surgical aesthetic procedures with an emphasis on hair loss. To this end, an integrative bibliographic review was carried out, of a descriptive nature, in the main health databases: SciELO, Google Scholar, PubMed and medical books, in Portuguese, English and Spanish, considering the period from 2007 to 2022. According to the latest census by the Brazilian Society of Dermatology, the complaint of alopecia is among the ten most frequent complaints in dermatological offices. The most important hair diseases are divided into two groups, scarring when hair loss is accompanied by scars resulting in permanent baldness, and non-scarring where baldness is not permanent leading to gradual thinning and thinning of the hair. Non-scarring alopecia is the most frequent and the most common among them are androgenetic alopecia and telogen effluvium. Many patients seek treatment to improve their appearance and self-esteem, which may be related to anxiety and depression. These treatments must be individualized, where the individual characteristics of each patient must be evaluated. Aesthetic hair treatments can contribute significantly to reducing low self-esteem, contributing to the recovery of self-confidence through hair growth provided by aesthetics. Therefore, it is concluded that the results collected in the literature review were satisfactory, in a way that shows that medicines, supplements and aesthetic treatments in hair loss have been evolving more and more. However, more studies on the subject are needed.

La belleza está directamente ligada al aspecto del cabello, en todos los tiempos y en todas las culturas. El cabello a lo largo de la vida está sujeto a diversos tipos de cambios, ya sean naturales o artificiales, impulsados por un deseo de cambio, a menudo, ya sea para representar una nueva etapa, como también es un símbolo de auto- cuidado, la vanidad, el éxito, tienen una importancia significativa en la apariencia y la autoestima de las personas y, por lo tanto, la pérdida del cabello puede afectar la calidad de vida del individuo. En este sentido, el objetivo de este estudio fue evaluar los procedimientos estéticos mínimamente invasivos y no quirúrgicos con énfasis en la pérdida de cabello. Para ello, se realizó una revisión bibliográfica descriptiva integradora en las principales bases de datos de salud: SciELO, Google Scholar, PubMed y libros de medicina, en portugués, inglés y español, considerando el período de 2007 a 2022. Según el último censo de la Sociedad Brasileña de Dermatología, la queja de alopecia está entre las diez más frecuentes en las consultas de dermatología. Las enfermedades capilares más importantes se dividen en dos grupos, las cicatriciales, cuando la caída del cabello va acompañada de cicatrices que dan lugar a una calvicie permanente, y las no cicatriciales, cuando la calvicie no es permanente, dando lugar a un adelgazamiento y reducción gradual del cabello. Las alopecias no cicatriciales son las más frecuentes y entre ellas destacan la alopecia androgenética y el efluvio telógeno. Muchos pacientes buscan tratamiento para mejorar su aspecto y autoestima, que pueden estar relacionados con la ansiedad y la depresión. Estos tratamientos deben ser individualizados, donde se deben evaluar las características individuales de cada paciente. Los tratamientos capilares estéticos pueden contribuir significativamente a la reducción de la baja autoestima, contribuyendo a la recuperación de la confianza en uno mismo gracias al crecimiento del cabello que proporciona la estética. Por lo tanto, se concluye que los resultados recogidos en la revisión bibliográfica fueron satisfactorios, mostrando que los medicamentos, suplementos y tratamientos estéticos para la caída del cabello están evolucionando cada vez más. Sin embargo, son necesarios más estudios sobre el tema.

Análise da dispensação de pílula do dia seguinte em uma farmácia do município no oeste do estado do Paraná / Analysis of the dispension of the pill of the following day in a pharmacy in the municipality in the west of the state of Paraná / Análisis de la dispensación de la píldora del día siguiente en una farmacia del municipio del oeste del estado de Paraná

pílula contraceptiva de emergência (CE) é chamada pelos médicos de pílula anticoncepcional pós-coito. É um método anticoncepcional de emergência e deve ser tomada até 72 horas após a relação sexual. É adequado para casos de abuso sexual, preservativos rompidos ou falha de outros métodos anticoncepcionais. Sendo assim, o objetivo do presente estudo foi avaliar o perfil da dispensação do contraceptivo de emergência (CE) em uma farmácia comercial localizada em um distrito do município de Assis Chateaubriand no oeste do estado do Paraná. Para o desenvolvimento da pesquisa, foi avaliado a quantidade do medicamento dispensado com o princípio ativo levonorgestrel no período de três meses em uma farmácia de dispensação de medicamentos no distrito de Bragantina, assim como a faixa etária da paciente que utilizou, o seu estado civil e o motivo da compra da pílula. O projeto foi aprovado pelo Comitê de ética sob o número do CAAE: 60509322.3.0000.0109. Os resultados mostraram que no período do desenvolvimento da pesquisa, 10 pacientes fizeram uso da CE, sendo 5 solteiras e 5 casadas, sendo 50%. Quando relatado a idade das pacientes que fazem uso do CE, os resultados foram entre 19 até 41 anos. Quando perguntado para as pacientes se elas faziam uso de outro método contraceptivo e se presente, qual seria este método, os resultados encontrados foram: 40% das mulheres não utilizam outro método contraceptivo e 60% fazem o uso de outro contraceptivo, destes, o percentual foi de 66% que faziam o uso de preservativo e 34% faziam o uso de anticoncepcional. Em relação ao horário pós-coito, isto é, quantas horas após o coito elas procuraram a farmácia para comprar a CE, os resultados encontrados foram de 08 horas até 52 horas. Sendo assim, conclui-se que o estudo possui relevância frente à procura da PDS, no entanto, é de suma importância não esquecer de que a PDS deve ser utilizada somente em casos de emergências e não como uso rotineiro, para isso, existem outros métodos de contraceptivos que podem ser de recurso rotineiro. Neste sentido, mais estudos são necessários para avaliar se a população tem conhecimento sobre o tema, se o farmacêutico está preparado para atendê-los e o porquê da população não se programar melhor para evitar os possíveis "acidentes".

The morning after pill (PDS) is called the post-coital birth control pill by doctors. It is an emergency contraceptive method and must be taken within 72 hours of sexual intercourse. It is suitable for cases of sexual abuse, broken condoms or failure of other contraceptive methods. Therefore, the objective of the present study will be to evaluate the profile of the dispensation of emergency contraceptives (EC) in a pharmacy in the western municipality of the state of Paraná. For the development of the research, the amount of medication dispensed in a period of three months in a drug dispensing pharmacy was evaluated, as well as the age group of the patient who will use it, her marital status and the reason for purchasing the pill. The project was approved by the Ethics Committee under CAAE number: 60509322.3.0000.0109. The results showed that during the research development period, 10 patients used PDS, 5 of them single and 5 married, being 50%. When reporting the age of patients using the morning-after pill, the results ranged from 19 to 41 years. When asked to patients if they used another contraceptive method and, if present, which method this would be, the results found were: 40% of women do not use another contraceptive method and 60% use another contraceptive, of these, the percentage 66% used condoms and 34% used contraceptives. Regarding the post-coital time, that is, how many hours after coitus they looked for the pharmacy to buy the PDS, the results found were from 08 hours to 52 hours. Therefore, it is concluded that care with medication intake becomes more important when it comes to EC, due to its potential risks to the female body, which can have consequences, especially when used excessively and without prior knowledge. Thus, more guidance on the use and its adverse effects, as more studies on the subject are necessary, in order to minimize the damage that PDS can cause in the female organism.

La píldora del día después (PDS) es llamada por los médicos píldora anticonceptiva poscoital. Es un método anticonceptivo de emergencia y debe ser tomada dentro de las 72 horas siguientes a la relación sexual. Está indicada en casos de abuso sexual, rotura del preservativo o fracaso de otros métodos anticonceptivos. Por lo tanto, el objetivo del presente estudio será evaluar el perfil de la dispensación de anticonceptivos de emergencia (AE) en una farmacia del municipio oeste del estado de Paraná. Para el desarrollo de la investigación, se evaluó la cantidad de medicación dispensada en un período de tres meses en una farmacia dispensadora de medicamentos, así como el grupo etario de la paciente que la utilizará, su estado civil y el motivo de compra de la píldora. El proyecto fue aprobado por el Comité de Ética con el número CAAE: 60509322.3.0000.0109. Los resultados mostraron que durante el período de desarrollo de la investigación, 10 pacientes utilizaron la PDS, 5 de ellas solteras y 5 casadas, siendo el 50%. Al informar sobre la edad de las pacientes que utilizaban la píldora del día después, los resultados oscilaron entre 19 y 41 años. Cuando se preguntó a las pacientes si utilizaban otro método anticonceptivo y, en caso afirmativo, cuál sería, los resultados encontrados fueron: 40% de las mujeres no utilizan otro método anticonceptivo y 60% utilizan otro anticonceptivo, de estas, el porcentaje 66% utilizó preservativo y 34% anticonceptivos. En cuanto al tiempo post-coital, es decir, cuántas horas después del coito buscaron la farmacia para comprar la PDS, los resultados encontrados fueron de 08 horas a 52 horas. Por lo tanto, se concluye que el cuidado con la ingesta de medicamentos se vuelve más importante cuando se trata de la AE, debido a sus riesgos potenciales para el organismo femenino, que pueden tener consecuencias, especialmente cuando se usa en exceso y sin conocimiento previo. Por lo tanto, son necesarias más orientaciones sobre el uso y sus efectos adversos, así como más estudios sobre el tema, con el fin de minimizar los daños que la PDS puede causar en el organismo femenino.

Mecanismos de expressão de resistência aos antibióticos e saúde pública / Mechanisms of expression of resistance to antibiotics and public health / Mecanismos de expresión de la resistencia a los antibióticos y salud pública

Com o avanço da medicina e o aumento do uso de antimicrobianos, a resistência microbiana vem se tornando um problema sério na saúde pública. Para que uma bactéria se torne resistente, são necessários vários fatores, entre eles, o uso indiscriminado e prolongado de antimicrobianos e as resistências intrínsecas e adquiridas. Nesse contexto, o objetivo do trabalho foi explorar os mecanismos de ação dos antimicrobianos, de resistência e a sua importância na saúde pública. Foram utilizadas para a presente pesquisa, as bases de dados Pubmed, Google acadêmico e Scielo. Segundo a Organização Mundial da Saúde define-se resistência ao antibiótico quando o mesmo não produz mais efeito. A inserção cada vez mais frequente de antimicrobianos favorece a resistência, onde provocam uma pressão seletiva sobre os microrganismos, tornando-os resistentes a diversas drogas. O uso indiscriminado de antimicrobianos é o principal fator de resistência microbiana, assim como o uso de antimicrobianos sem exame de cultura e teste de sensibilidade. Neste sentido, conclui-se que é de suma importância a atualização de protocolos que contenham os mecanismos de resistência bacteriana a fim de minimizar o uso indiscriminado de antimicrobianos, assim como capacitar os profissionais da saúde para este problema na saúde pública.

With the advance of medicine and the increase in the use of antimicrobials, microbial resistance has become a serious problem in public health. For a bacterium to become resistant, several factors are necessary, among them, the indiscriminate and prolonged use of antimicrobials and the intrinsic and acquired resistance. In this context, the objective of the work was to explore the mechanisms of action of antimicrobials, resistance and their importance in public health. Pubmed, Google academic and Scielo databases were used for this research. According to the World Health Organization, resistance to antibiotics is defined when it no longer has an effect. The increasingly frequent insertion of antimicrobials favors resistance, where they put selective pressure on microorganisms, making them resistant to various drugs. The indiscriminate use of antimicrobials is the main factor of microbial resistance, as well as the use of antimicrobials without culture examination and sensitivity test. In this sense, it is concluded that it is extremely important to update protocols that contain the mechanisms of bacterial resistance in order to minimize the indiscriminate use of antimicrobials, as well as to train health professionals for this problem in public health.

Con los avances de la medicina y el mayor uso de antimicrobianos, la resistencia microbiana se ha convertido en un grave problema de salud pública. Para que una bacteria se vuelva resistente son necesarios varios factores, entre ellos, el uso indiscriminado y prolongado de antimicrobianos y la resistencia intrínseca y adquirida. En este contexto, el objetivo de este trabajo fue explorar los mecanismos de acción de los antimicrobianos, la resistencia y su importancia en la salud pública. Para esta investigación se utilizaron las bases de datos Pubmed, Google Scholar y Scielo. Según la Organización Mundial de la Salud, la resistencia a un antibiótico se define cuando deja de producir efecto. El uso cada vez más frecuente de antimicrobianos favorece la resistencia, ya que provocan una presión selectiva sobre los microorganismos, haciéndolos resistentes a varios fármacos. El uso indiscriminado de antimicrobianos es el principal factor de resistencia microbiana, así como el uso de antimicrobianos sin pruebas de cultivo y sensibilidad. En este sentido, se concluye que es de suma importancia actualizar los protocolos que contienen los mecanismos de resistencia bacteriana para minimizar el uso indiscriminado de antimicrobianos, así como capacitar a los profesionales de la salud para este problema en la salud pública.

Review Covid-19 (sars-cov-2) and medicinal plants ­ literature / Revisão Covid-19 (sars-cov-2) e plantas medicinais - literatura / Revisión Covid-19 (sars-cov-2) y plantas medicinales - bibliografía

In December 2019, a new coronavirus originating from the city of Wuhan in China started an epidemic that brought many countries into chaos and despair. SARS-CoV-2, as identified, gave rise to the severe acute respiratory syndrome called COVID-19. Its transmission happens through droplets of saliva, hand or contaminated surfaces. Since its discovery, COVID-19 has led many to death, therefore, researchers from around the world have joined efforts to develop strategies to contain the virus. In this race, drugs such as Chloroquine and Hydroxychloroquine have become possible options for showing an antiviral effect, however, studies contest their efficiency, generating uncertainties. Therefore, other alternatives have been investigated in this context, and the study of medicinal plants has been the target of research for the treatment of COVID-19 in search of bioactive natural products that can exert an antiviral action. The study aimed to analyze the published literature on COVID-19 (SARS-CoV-2) and its relationship with medicinal plants. Bibliographical survey. So far, no specific treatment against the disease has been found, only supportive, with drugs that aim to improve the individual's immune system and ensure that the virus does not replicate, for example, there are options such as chloroquine, hydroxychloroquine, remdesivir and convalescent plasma. On the other hand, studies have revealed that medicinal plants such as garlic, among others, showed efficiency in modulating proteins with a view to preventing viral replication and improving immunity against COVID-19. So far, there are no drugs that are completely safe and have been shown to have activity against the new coronavirus (SARS-CoV-2). However, medicinal plants can contribute to the development of specific therapies against SARS-CoV-2 in a safe and effective way.

Em dezembro de 2019, um novo coronavírus originário da cidade de Wuhan, na China, iniciou uma epidemia que levou muitos países ao caos e ao desespero. O SARS-CoV-2, conforme identificado, deu origem à síndrome respiratória aguda grave chamada COVID-19. Sua transmissão acontece através de gotículas de saliva, mãos ou superfícies contaminadas. Desde sua descoberta, o COVID-19 levou muitos à morte, por isso, pesquisadores de todo o mundo uniram esforços para desenvolver estratégias para conter o vírus. Nesta corrida, medicamentos como Cloroquina e Hidroxicloroquina tornaram-se opções possíveis por apresentarem efeito antiviral, porém, estudos contestam sua eficiência, gerando incertezas. Portanto, outras alternativas têm sido investigadas nesse contexto, e o estudo de plantas medicinais tem sido alvo de pesquisas para o tratamento da COVID- 19 em busca de produtos naturais bioativos que possam exercer ação antiviral. O estudo teve como objetivo analisar a literatura publicada sobre COVID-19 (SARS-CoV-2) e sua relação com plantas medicinais. Levantamento bibliográfico. Até o momento, não foi encontrado nenhum tratamento específico contra a doença, apenas de suporte, com medicamentos que visam melhorar o sistema imunológico do indivíduo e garantir que o vírus não se replique, por exemplo, há opções como cloroquina, hidroxicloroquina, remdesivir e convalescença plasma. Por outro lado, estudos revelaram que plantas medicinais como o alho, entre outras, mostraram eficiência na modulação de proteínas visando prevenir a replicação viral e melhorar a imunidade contra a COVID-19. Até o momento, não existem medicamentos completamente seguros e que tenham demonstrado atividade contra o novo coronavírus (SARS-CoV-2). No entanto, as plantas medicinais podem contribuir para o desenvolvimento de terapias específicas contra o SARS-CoV-2 de forma segura e eficaz.

En diciembre de 2019, un nuevo coronavirus originario de la ciudad de Wuhan, en China, inició una epidemia que sumió a muchos países en el caos y la desesperación. El SARS-CoV- 2, tal y como fue identificado, dio lugar al síndrome respiratorio agudo severo denominado COVID-19. Su transmisión se produce a través de gotitas de saliva, de las manos o de superficies contaminadas. Desde su descubrimiento, el COVID-19 ha llevado a muchos a la muerte, por lo que investigadores de todo el mundo han aunado esfuerzos para desarrollar estrategias de contención del virus. En esta carrera, fármacos como la Cloroquina y la Hidroxicloroquina se han convertido en posibles opciones por mostrar un efecto antiviral, sin embargo, los estudios refutan su eficacia, generando incertidumbres. Por lo tanto, otras alternativas han sido investigadas en este contexto, y el estudio de las plantas medicinales ha sido el objetivo de la investigación para el tratamiento de COVID-19 en busca de productos naturales bioactivos que puedan ejercer una acción antiviral. El estudio tuvo como objetivo analizar la literatura publicada sobre el COVID-19 (SARS-CoV-2) y su relación con las plantas medicinales. Estudio bibliográfico. Hasta el momento, no se ha encontrado un tratamiento específico contra la enfermedad, sólo de soporte, con fármacos que buscan mejorar el sistema inmunológico del individuo y asegurar que el virus no se replique, por ejemplo, existen opciones como la cloroquina, hidroxicloroquina, remdesivir y plasma convaleciente. Por otro lado, estudios han revelado que plantas medicinales como el ajo, entre otras, mostraron eficacia en la modulación de proteínas con vistas a impedir la replicación viral y mejorar la inmunidad contra el COVID-19. Hasta el momento, no existen medicamentos que sean completamente seguros y que hayan demostrado tener actividad contra el nuevo coronavirus (SARS-CoV-2). Sin embargo, las plantas medicinales pueden contribuir al desarrollo de terapias específicas contra el SARS-CoV-2 de forma segura y eficaz.

WITHDRAWN: Main Diagnostic Methods for COVID-19: Integrative Review

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Antileishmanial activity of Melampodium divaricatum and Casearia sylvestris essential oils on Leishmania amazonensis.

Leishmaniasis is a disease that affects millions of people and it is an important public health problem. The drugs currently used for the treatment of leishmaniasis present undesirable side effects and low efficacy. In this study, we evaluated the in vitro activity of Melampodium divaricatum (MD-EO) and Casearia sylvestris (CS-EO) essential oils (EO) against promastigote and amastigote forms of Leishmania amazonensis. Sesquiterpenes E-caryophyllene (56.0%), germacrene D (12.7%) and bicyclogermacrene (9.2%) were identified as the main components of MD-EO, whereas E-caryophyllene (22.2%), germacrene D (19.6%) and bicyclogermacrene (12.2%) were the main constituents of CS-EO. CS-EO and E-caryophyllene were active against promastigote forms of L. amazonensis (IC50 24.2, 29.8 and 49.9 µg/mL, respectively). However, MD-EO, CS-EO and E-caryophyllene were more active against amastigote forms, with IC50 values of 10.7, 14.0, and 10.7 µg/mL, respectively. E-caryophyllene presented lower cytotoxicity against macrophages J774-A1 (CC50 of 62.1 µg/mL) than the EO. The EOs and E-caryophyllene should be further studied for the development of new antileishmanial drugs.

Quinoxaline derivatives as potential antitrypanosomal and antileishmanial agents.

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 amastigotes of T. cruzi, without interfering with mammalian cell viability. These compounds presented encouraging results that will guide our future studies on in vivo bioassays towards the mode of action.

Composition and leishmanicidal activity of the essential oil of Vernonia polyanthes Less (Asteraceae).

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 IC50 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 CC50 < 10 µg/ml to macrophages cells.

In Vitro and In Vivo Activities of 2,3-Diarylsubstituted Quinoxaline Derivatives against Leishmania amazonensis.

Leishmaniasis is endemic in 98 countries and territories worldwide. The therapies available for leishmaniasis have serious side effects, thus prompting the search for new therapies. The present study investigated the antileishmanial activities of 2,3-diarylsubstituted quinoxaline derivatives against Leishmania amazonensis The antiproliferative activities of 6,7-dichloro-2,3-diphenylquinoxaline (LSPN329) and 2,3-di-(4-methoxyphenyl)-quinoxaline (LSPN331) against promastigotes and intracellular 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 vivo antileishmanial activity was evaluated in a murine cutaneous leishmaniasis model. Compounds LSPN329 and LSPN331 showed significant selectivity for promastigotes and intracellular amastigotes and low cytotoxicity. In promastigotes, ultrastructural alterations were observed, including an increase in lipid inclusions, concentric membranes, and intense mitochondrial swelling, which were associated with hyperpolarization of ΔΨm, an increase in the O2·(-) concentration, decreased intracellular ATP levels, and a decrease in cell volume. Phosphatidylserine exposure and DNA fragmentation were not observed. The cellular membrane remained intact after treatment. Thus, the multifactorial response that was responsible for the cellular collapse of promastigotes was based on intense mitochondrial alterations. BALB/c mice treated with LSPN329 or LSPN331 showed a significant decrease in lesion thickness in the infected footpad. Therefore, the antileishmanial activity and mitochondrial mechanism of action of LSPN329 and LSPN331 and the decrease in lesion thickness in vivo brought about by LSPN329 and LSPN331 make them potential candidates for new drug development for the treatment of leishmaniasis.

Synthesis and biological evaluation of novel 2,3-disubstituted quinoxaline derivatives as antileishmanial and antitrypanosomal agents.

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 were the most selective (SI = 19.5-38.4) on amastigotes of T. cruzi. In general their activity was directly related to the methylsulfoxyl, methylsulfonyl, and amine groups as well as the presence of chorine or bromine in the molecules. The current results indicate that these quinoxaline derivatives are novel and promising agents for further development towards a treatment for Chagas' disease and leishmaniasis.

The Effects of N-Butyl-1-(4-dimethylamino)phenyl-1,2,3,4-tetrahydro- ß -carboline-3-carboxamide against Leishmania amazonensis Are Mediated by Mitochondrial Dysfunction.

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 of N-butyl-1-(4-dimethylamino)phenyl-1,2,3,4-tetrahydro-ß-carboline-3-carboxamide (C4) and its possible targets against L. 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 in L. amazonensis treated with C4. Our results indicate that C4 is a selective antileishmanial agent, and its effects appear to be mediated by mitochondrial dysfunction.

Trypanocidal activity of guaianolide obtained from Tanacetum parthenium (L.) Schultz-Bip. and its combinational effect with benznidazole.

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.

Qualidade de água dos rios Vacacaí e Vacacaí-Mirim no Estado do Rio Grande do Sul, Brasil / Water quality of the Vacacaí and Vacacaí-Mirim rivers in the Rio Grande do Sul State, Brazil

A água é um dos recursos naturais fundamentais para a vida. Neste trabalho, foi avaliada a qualidade da água dos rios Vacacaí e Vacacaí-Mirim no Rio Grande do Sul (RS), Brasil, com base nos parâmetros N-nitrato (N-NO3), N-amônia (N-NH3), fósforo (P), potássio (K) e sódio (Na) e também na variação do pH e da condutividade elétrica (CE) da água. As coletas de água foram realizadas a cada 15 dias, de outubro a março de 2002/03 a 2006/07. Os resultados foram comparados com as legislações do RS (Secretaria da Saúde e Meio Ambiente), do Brasil (CONAMA e Ministério da Saúde) e dos Estados Unidos (EPA). O pH variou de 5,71 a 7,50, e a CE, de 33,33 a 118,88µS cm-1. Para N-nitrato, as amostras de água estiveram dentro de limites aceitáveis estabelecidos pelas legislações. A concentração de P oscilou de 0,00 a 0,18mg L-1. Os níveis de N-amônia variaram de 0,02 a 0,39mg L-1, o K, de 2,05 a 3,66mg L-1 e o Na, de 1,84 a 16,8mg L-1.

Water is an important natural resource for preserving the life in the planet. In this survey, it was evaluated water quality in the Vacacaí and Vacacaí-Mirim basins in Rio Grande do Sul State, Brazil. The water samples were evaluated for N-nitrate (N-NO3), phosphorus (P), potassium (K) and sodium (Na), pH and electric conductivity (EC). The results were compared to the values suggested by the resolutions of the State Environmental Agency (Secretaria da Saúde e Meio Ambiente), the Brazilian Agencies (CONAMA e Ministério da Saúde) and the United States Environmental Protection Agency (EPA). The water pH varied between 5.71 and 7.5 and de EC between 33.33 and 118.88µS cm-1. For N-nitrate 100 percent samples were in the settled limits by environmental legislation. The P levels were between 0.00 to 0.18mg L-1. The N-ammonia levels varied between 0.02 and 0.39mg L-1, the K levels remained between 2.05 and 3.66mg L-1 and the Na levels between 1.84 and 16.8mg L-1.

Bioensaio de atividade moluscicida adaptado para a avaliação de extratos de plantas medicinais / Bioensayo de actividad moluscicida adaptado para evaluación de extractos de plantas medicinales / Bioassay of molluscicidal activity adapted for the evaluation of medicinal plant extracts

Nesta nota é apresentada detalhadamente a metodologia (preparação dos extratos, adaptação dos caramujos, ensaio de atividade, destino dos caramujos) usada para a avaliação da atividade moluscicida de extratos de plantas frente a caramujos da espécie Biomphalaria glabrata. A adaptação desta metodologia tem o propósito de avaliar extratos naturais para a busca de produtos alternativos mais baratos, biodegradáveis, seguros e disponíveis localmente, para o controle das populações de caramujos.

The methodology (extract preparation, adaptation of the snails, activity test, destiny of the snails) used for the evaluation of the molluscicidal activity of plant extracts in relation to snails from the Biomphalaria glabrata species appears in detail in this note. The adaptation of this methodology has the purpose of evaluating natural extracts in order to find cheaper, biodegradable, safe and easily available alternative products for the control of the populations of snails.

En este apunte se presenta detalladamente la metodología (preparación de los extractos, adaptación de los caracoles, ensayo de actividad, destino de los caracoles) utilizada para la evaluación de la actividad moluscicida de extractos de plantas frente a caracoles de la especie Biomphalaria glabrata. La adaptación de esta metodología tiene el propósito de evaluar extractos naturales para la búsqueda de productos alternativos más baratos, biodegradables, seguros y disponibles localmente, para el control de las poblaciones de caracoles.