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Chikungunya virus (CHIKV) is a re-emerging disease caused by an alphavirus of the Togaviridae family. Since its first description in 1952, the disease has spread worldwide, affecting populations in both tropical and temperate countries. To date, there is no licensed vaccine or specific pharmacological treatment. Therefore, there is an increasing urgency in developing new antiviral drugs capable of specifically inhibiting viral replication. In the present work, we report the synthesis and antiviral activity evaluation of nineteen naphthoquinone derivatives, containing a sulfonamide or sulfonate group. Cell viability assays indicated a low toxic potential for all tested compounds and inhibitory assays against CHIKV identified five compounds with potent activity. The compounds were also evaluated for their virucidal potential, and the results demonstrated that compound 11a exhibited a virucidal effect higher than 70% in the treatment with 20 µM. Furthermore, in silico studies were performed to predict the antiviral drug targets.

https://doi.org/10.21577/0103-5053.20220010

A New Strategy for the Synthesis of Nonsymmetrical 3,3’-(Aryl/alkyl-methylene)bis-2-hydroxy-1,4-naphthoquinones and Their Cytotoxic Effects in PC3 Prostate Cancer Cells
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Ribeiro, Ruan Carlos B.

; Freitas, Paula Priscilla de

; Moreira, Caroline S.

; Moraes, Leonardo G. C. de

; Moraes, Matheus G. de

; Silva, Fernando de C. da

; Rocha, David R.

; Gimba, Etel R. Pereira

; Ferreira, Vitor F.

Journal of the Brazilian Chemical Society

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feb 2020, Volume 31 N. 2 Pages 288 - 297

Abstract: En | Text: En | PDF: En

A novel method for the synthesis of nonsymmetrical 3,3’-(aryl/alkyl-methylene)bis-2-hydroxy-1,4-naphthoquinones was developed by using the Mannich adduct of naphthoquinone and the reaction with another moiety of 2-hydroxy-1,4-naphthoquinone. This novel method produces for the first time nonsymmetrical 3,3’-(aryl/alkyl-methylene)bis-2-hydroxy-1,4-naphthoquinones. In a preliminary study, these compounds (15c, 15f and 15h) were evaluated regarding their effect over the viability of PC3 metastatic prostate cancer cell using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assays at 100 µM. Three of these compounds presented relevant cytotoxic effects at 72 h posttreatment.

https://doi.org/10.21577/0103-5053.20190172 392 downloads

Brazilian recommendations on the safety and effectiveness of the yellow fever vaccination in patients with chronic immune-mediated inflammatory diseases
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Pileggi, Gecilmara Salviato

; Mota, Licia Maria Henrique Da

; Kakehasi, Adriana Maria

; Souza, Alexandre Wagner De

; Rocha, Aline

; Melo, Ana Karla Guedes de

; Fonte, Caroline Araujo M. da

; Bortoletto, Cecilia

; Brenol, Claiton Viegas

; Marques, Claudia Diniz Lopes

; Zaltman, Cyrla

; Borba, Eduardo Ferreira

; Reis, Enio Ribeiro

; Freire, Eutilia Andrade Medeiros

; Klumb, Evandro Mendes

; Christopoulos, Georges Basile

; Laurindo, Ieda Maria M.

; Ballalai, Isabella

; Costa, Izaias Pereira Da

; Michelin, Lessandra

; Valadares, Lilian David de Azevêdo

; Chebli, Liliana Andrade

; Lacerda, Marcus

; Toscano, Maria Amazile Ferreira

; Yazbek, Michel Alexandre

; Vieira, Rejane Maria R. De Abreu

; Magalhães, Renata

; Kfouri, Renato

; Richtmann, Rosana

; Merenlender, Selma Da Costa Silva

; Valim, Valeria

; Assis, Marcos Renato De

; Kowalski, Sergio Candido

; Trevisani, Virginia Fernandes Moça

Advances in Rheumatology

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2019, Volume 59 elocation 17

Abstract: En | Text: En | PDF: En

Abstract Background: In Brazil, we are facing an alarming epidemic scenario of Yellow fever (YF), which is reaching the most populous areas of the country in unvaccinated people. Vaccination is the only effective tool to prevent YF. In special situations, such as patients with chronic immune-mediated inflammatory diseases (CIMID), undergoing immunosuppressive therapy, as a higher risk of severe adverse events may occur, assessment of the risk-benefit ratio of the yellow fever vaccine (YFV) should be performed on an individual level. Main body of the abstract: Faced with the scarcity of specific orientation on YFV for this special group of patients, the Brazilian Rheumatology Society (BRS) endorsed a project aiming the development of individualized YFV recommendations for patients with CIMID, guided by questions addressed by both medical professionals and patients, followed an internationally validated methodology (GIN-McMaster Guideline Development). Firstly, a systematic review was carried out and an expert panel formed to take part of the decision process, comprising BRS clinical practitioners, as well as individuals from the Brazilian Dermatology Society (BDS), Brazilian Inflammatory Bowel Diseases Study Group (GEDIIB), and specialists on infectious diseases and vaccination (from Tropical Medicine, Infectious Diseases and Immunizations National Societies); in addition, two representatives of patient groups were included as members of the panel. When the quality of the evidence was low or there was a lack of evidence to determine the recommendations, the decisions were based on the expert opinion panel and a Delphi approach was performed. A recommendation was accepted upon achieving ≥80% agreement among the panel, including the patient representatives. As a result, eight recommendations were developed regarding the safety of YFV in patients with CIMID, considering the immunosuppression degree conferred by the treatment used. It was not possible to establish recommendations on the effectiveness of YFV in these patients as there is no consistent evidence to support these recommendations. Conclusion: This paper approaches a real need, assessed by clinicians and patient care groups, to address specific questions on the management of YFV in patients with CIMID living or traveling to YF endemic areas, involving specialists from many areas together with patients, and might have global applicability, contributing to and supporting vaccination practices. We recommended a shared decision-making approach on taking or not the YFV.

https://doi.org/10.1186/s42358-019-0056-x 1111 downloads

Testing a new surgical instrument to obtain bovine hoof biopsy samples
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Mendes, Heloisa M.F.

; Rocha Júnior, Sérgio S.

; Paz, Cahuê F.R.

; Valadares, Rodrigo C.

; Ribeiro, Rodrigo M.

; Azevedo, David S.D.

; Vasconcelos, Anilton C.

; Faleiros, Rafael R.

Pesquisa Veterinária Brasileira

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jun 2018, Volume 38 N. 6 Pages 1077 - 1084

Abstract: Pt En | Text: Pt En | PDF: Pt | PDF: En

RESUMO: A avaliação das propriedades histológicas e da expressão de genes e proteínas em biópsias tem sido determinante para o entendimento da fisiopatologia, o diagnóstico e o prognóstico das enfermidades. Entretanto, a obtenção de biópsias do casco é um procedimento com limitações devido à ausência de técnicas e instrumentos específicos. O objetivo foi desenvolver e testar, na espécie bovina, um instrumento cirúrgico especificamente desenvolvido para realização de biópsias de casco nominado lamelótomo de Falcão-Faleiros (INPI, BR102013018765-8). Utilizaram-se cinco bovinos adultos que foram sedados, contidos em decúbito lateral e tiveram dois dígitos anestesiados. Em seguida, uma serra circular acoplada a uma microretífica foi usada para o desgaste do estrato córneo na parede dorsal até próximo do estrato lamelar. Após incisões retilíneas delimitando a borda interna da área desgastada, utilizou-se o lamelótomo para obtenção da amostra. Os fragmentos de 16mm de comprimento e 6mm de profundidade foram fixados em formalina e processados para histologia com colorações HE, PAS, Shorr e tricrômico de Masson. Nenhum dos animais apresentou claudicação ou complicação relevantes no período pós-opertório. As amostras foram consideradas adequadas quanto à integridade das lâminas e à preservação de sua arquitetura. Obtiveram-se média de 85 lâminas epidérmicas viáveis por biópsia. Conclui-se que o lamelótomo de Falcão-Faleiros é apropriado e seguro para a obtenção de biópsias de casco em bovinos, se mostrando promissor para uso em estudos clínicos e na rotina de diagnóstico de problemas podais em bovinos.

ABSTRACT: The histological and molecular analysis of biopsy samples are fundamental steps for the understanding of physiopathology, diagnosis and prognosis of the diseases. However, harvest of tissue biopsies from hoof lamellar tissue is a procedure with limitations due to lack of effective surgical instruments and techniques. The aim of the current study is to develop and test in vivo a surgical instrument with the specific purpose of harvesting lamellar tissue in cattle. A prototype called Falcão-Faleiros’ lamellotome (INPIBR102013018765-8) was designed, produced and tested. After sedation, five adult cattle were restrained in lateral recumbency and locally anesthetized in two digits. The stratum corneum was worn down using a rotary tool coupled to a 3/8” high-speed cutter until the soft tissue proximity was reached. Next, the inner edge of the worn area was bounded with a scalpel. The lamellotome was introduced to obtain and hold the sample. The histological specimens of 16mm length by 6mm depth were stained with HE, PAS, Masson’s thricome and Shorr. The structures of interest were differentiated in the histological analysis without technical artifacts and a mean number of 85 epidermal laminae per sample were counted. No relevant lameness or wound complication were seen following the procedure. In conclusion the technique using the lamellotme was effective in obtaining lamellar tissue biopsy samples without causing clinical harm in cattle. The procedure showed potential to be used in clinical research or even as a supplementary diagnosis method for routine bovine podiatry.

https://doi.org/10.1590/1678-5150-pvb-5073 881 downloads

Synthesis of New Xanthenes Based on Lawsone and Coumarin via a Tandem Three-Component Reaction
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Cardoso, Mariana F. C.

; Forezi, Luana S. M.

; Cavalcante, Victor G. S.

; Juliani, Cecília S. R.

; Resende, Jackson Antônio L. C.

; Rocha, David R. da

; Silva, Fernando C. da

; Ferreira, Vitor F.

Journal of the Brazilian Chemical Society

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oct 2017, Volume 28 N. 10 Pages 1926 - 1936

Abstract: En | Text: En | PDF: En

The synthesis of several new xanthenes based on the 1,3-dicarbonyl scaffolds lawsone and coumarin was developed using tandem three-component reactions involving the reagents ortho-hydroxybenzaldehyde, as bifunctional reagent, and an appropriate thiol. These reactions generated two series of para- and ortho-naphthoxanthenes that are structurally related to α- and β-pyranaphthoquinones and one series of coumarin-xanthene derivatives.

https://doi.org/10.21577/0103-5053.20170032 913 downloads

MICORRIZAS ARBUSCULARES NO CRESCIMENTO DE LEGUMINOSAS ARBÓREAS EM SUBSTRATO CONTENDO REJEITO DE MINERAÇÃO DE CARVÃO
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Stoffel, Shantau Camargo Gomes

; Armas, Rafael Dutra de

; Giachini, Admir José

; Rossi, Márcio José

; Gonzalez, David

; Meyer, Edenilson

; Nicoleite, Carlos Henrique

; Rocha-Nicoleite, Edilane

; Soares, Claudio Roberto Fonseca Sousa

CERNE

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jun 2016, Volume 22 N. 2 Pages 181 - 188

Abstract: Pt En | Text: Pt En | PDF: Pt | PDF: En

RESUMO O objetivo desse trabalho foi avaliar o efeito da inoculação de fungos micorrízicos arbusculares (FMA) no crescimento, colonização micorrízica e absorção de P e elementos-traço em leguminosas arbóreas expostas a rejeito de mineração de carvão. Ensaios independentes para as leguminosas Mimosa scabrella Benth. (bracatinga), Mimosa bimucronata (DC.) Kuntze (maricá) e Parapiptadenia rigida (Benth.) Brenan (angico-vermelho) foram conduzidos em casa de vegetação em delineamento inteiramente casualizado com seis tratamentos. Foram avaliados cinco isolados de FMA autóctones de áreas de mineração (Acaulospora colombiana, Acaulospora morrowiae, Dentiscutata heterogama, Rhizophagus clarus e Rhizophagus irregularis), além de um tratamento controle não inoculado, com quatro repetições. Verificou-se que a colonização micorrízica foi superior a 60% para a bracatinga e o maricá, enquanto que, para o angico-vermelho, foi de no máximo 26%. De maneira geral, a inoculação de FMA favoreceu o crescimento das leguminosas arbóreas, atingindo incrementos de até 1430%. A absorção de fósforo foi beneficiada principalmente pela inoculação de A. colombiana, R. irregularis e A. morrowiae. Apesar de se verificar redução nos teores de elementos-traço na parte aérea das plantas, a inoculação de FMA ocasionou incrementos significativos no acúmulo de As, Cu, Zn e Cr para todas as leguminosas avaliadas. Desta forma, os FMA desempenham papel importante para o crescimento de espécies arbóreas em áreas de mineração de carvão, as quais apresentam ambientes pobres, degradados e muitas vezes contaminados.

ABSTRACT The objective of this work was to evaluate the effects of arbuscular mycorrhizal inoculation in the growth, colonization and absorption of P and trace elements of leguminous trees on coal mine wastes. Independent assays for Mimosa scabrella Benth. (common name bracatinga), Mimosa bimucronata (DC.) Kuntze (maricá) and Parapiptadenia rigida (Benth.) Brenan (angico-vermelho) were carried out in a greenhouse on an entirely casualized experimental delineation composed of six treatments. Five coal mine autochthonous arbuscular mycorrhizal fungal isolates were tested, including Acaulospora colombiana, Acaulospora morrowiae, Dentiscutata heterogama, Rhizophagus clarus and Rhizophagus irregulars, aside from a control treatment, with four replications each. Results show that arbuscular mycorrhizal colonization was greater than 60% for Mimosa species, and up to 26% for Parapiptadenia. Overall, the fungal inoculation promoted better plant growth, with increments of up to 1430%. Phosphorous absorption was favored, especially when inoculation was done with A. colombiana, R. irregularis and A. morrowiae. Even though there was a conclusive reduction in the levels of trace elements in the plant´s shoots, the inoculation with those species of fungi promoted significant increments in the accumulated levels of As, Cu, Zn and Cr for all plant species tested. Therefore, arbuscular mycorrhizal fungi play important roles in these poor, degraded and often contaminated environments.

https://doi.org/10.1590/01047760201622021969 2530 downloads

Perfil hematológico de cabras Saanen e mestiças (1/2 Saanen e 1/2 Anglo-nubiana) criadas em clima tropical do Ceará
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Souza, Priscila T.

; Salles, Maria Gorete F.

; Costa, Antônio Nélson L.

; Carneiro, Hilton A.V.

; Souza, Leonardo P.

; Rocha, David R.

; Araújo, Airton A.

Pesquisa Veterinária Brasileira

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jan 2015, Volume 35 N. 1 Pages 99 - 104

Abstract: Pt En | Text: Pt En | PDF: Pt | PDF: En

Objetivou-se verificar a influência das condições climáticas sobre o perfil hematológico de cabras Saanen e mestiça (1/2 Saanen x 1/2 Anglo-nubiana), bem como determinar valores de referência para esses animais criados no Ceará. Foram utilizadas 30 cabras que tiveram o sangue coletado mensalmente durante a época chuvosa (fevereiro a maio) e seca (agosto a novembro) para realização do eritrograma e leucograma. As médias foram comparadas pelo teste t-Student e Mann Whitney, quando constatada distribuição paramétrica e não paramétrica dos dados, respectivamente, com significância quando p<0,05. Procedeu-se ainda um estudo de correlações simples de Pearson dos parâmetros hematológicos com variáveis ambientais e fisiológicas. O número de hemácias foi maior em cabras Saanen e na época chuvosa, enquanto que o hematócrito foi maior na época seca (p<0,05). Os leucócitos e linfócitos foram maiores em cabras mestiças nas duas épocas (p<0,05). Nos dois genótipos, os leucócitos e linfócitos foram maiores na época seca e os neutrófilos segmentados maiores na época chuvosa (p<0,05). Os demais parâmetros não diferiram (p>0,05). As hemácias e neutrófilos segmentados apresentaram uma correlação negativa com a temperatura ambiente, porém positiva com a umidade do ar e a temperatura retal (p<0,05). O hematócrito correlacionou-se positivamente com a temperatura ambiente e frequência respiratória (p<0,05). Os leucócitos e linfócitos mostraram uma correlação negativa com a temperatura retal (p<0,05). Conclui-se, portanto, que fêmeas Saanen sofrem mais influência das variações climáticas e a época chuvosa tem maior impacto negativo sobre os parâmetros hematológicos. Os valores obtidos poderão servir como referência para esses genótipos no Ceará.

The aim of this study was to determine the influence of climatic conditions on the hematological profile of Saanen and mixed-breed (1/2 Saanen x 1/2 Anglo-Nubian) goats, as well as to define reference values for these animals bred in Ceará, Brazil. Thirty goats were utilized and blood samples were collected monthly during the rainy (February to May) and dry (August to November) periods to obtain an erythrogram a leukogram. The averange were compared by the t-Student test and Mann Whitney test, with parametric and non-parametric distribution of the data, respectively, where p<0.05 was considered significant. A study was carried out of simple Pearson correlations of the hematological parameters with environmental and physiological variables. The number of red blood cells (RBCs) was higher in the Saanen goats and in the rainy period, while the hematocrit was higher in the dry period (p<0.05). The leukocytes and lymphocytes were higher in the 1/2S1/2AN goats in the two periods (p<0.05). In the two genotypes, the leukocytes and lymphocytes were higher in the dry season and the segmented neutrophils higher in the rainy season (p<0.05). The other parameters did not differ (p>0.05). The RBCs and segmented neutrophils displayed a negative correlation with air temperature, but positive with relative humidity and rectal temperature (p<0.05). The hematocrit positively correlated with air temperature and respiratory rate (p<0.05). The leukocytes and lymphocytes showed a negative correlation with rectal temperature (p<0.05). It was therefore concluded that Saanen females are more affected by climatic variations and that the rainy season has a greater negative impact on hematological parameters. The values obtained could serve as a reference for these genotypes in Ceará.

https://doi.org/10.1590/S0100-736X2015000100019 2037 downloads

Morphological and morphometric evaluation of prepubertal gilt ovaries, uterine tubes and uterus at different oestrus cycle stages
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Oberlender, Guilherme

; Pontelo, Thais P.

; Miranda, José R.

; Miranda, David R.

; Zangeronimo, Márcio G.

; Silva, Adriana C.

; Menezes, Tila A.

; Rocha, Luiz G. P.

Pesquisa Veterinária Brasileira

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jan 2014, Volume 34 N. 1 Pages 83 - 90

Abstract: Pt En | Text: Pt En | PDF: Pt | PDF: En

Pesquisas são realizadas no desenvolvimento de técnicas/procedimentos que propiciem maior eficiência reprodutiva em animais de produção, dentre esses, os suínos. Nesse sentido, o estudo dos órgãos reprodutivos das fêmeas suínas em diferentes fases do ciclo estral é importante para avaliação da presença de anomalias e/ou demais parâmetros que possam afetar a fertilidade futura do animal. Objetivando-se avaliar as características morfológicas, morfométricas e histomorfométricas dos ovários, útero e tubas uterinas (TUs) de fêmeas suínas pré-púberes em diferentes fases do ciclo estral, tratos reprodutivos foram obtidos de 48 animais imediatamente após o abate. Posteriormente, as estruturas foram dissecadas e retiradas, sendo os ovários utilizados para a classificação da fase do ciclo estral de cada fêmea em fase folicular (FF) e fase luteínica (FL). Em seguida, foram realizadas avaliações morfométricas dos ovários, TUs, cornos uterinos e corpo uterino. Após, segmentos mediais das TUs e útero foram fixados em solução de Bouin, processados e incluídos rotineiramente em parafina, quando cortes histológicos de 5,0 micrômetros (µm) foram obtidos e corados com Hematoxilina e Eosina. Análises histomorfométricas foram realizadas utilizando sistema de captura de imagens e software específico. Posteriormente, os dados obtidos foram submetidos ao teste t de Student para a avaliação de diferenças estatísticas (P<0,05) entre as diferentes fases do ciclo estral (FF × FL) e entre a localização das estruturas reprodutivas (antímero direito × esquerdo). Dentre as fêmeas avaliadas, 35 encontravam-se na FF e 13 na FL. Não houve diferença (P>0,05) entre os parâmetros morfométricos dos ovários, TUs e útero das fêmeas nas FF e FL. Da mesma forma, em relação à localização das estruturas reprodutivas, tanto nas duas fases do ciclo estral, como na média geral, não houve diferença (P>0,05). Em relação às variáveis histomorfométricas, as fêmeas classificadas na FF apresentaram maior (P<0,05) altura do epitélio glandular e da TU em comparação com os animais na FL. Por outro lado, o diâmetro das glândulas endometriais foi maior (P<0,05) nas fêmeas classificadas na FL em comparação com a FF. Além disso, as fêmeas na FL apresentaram maior (P<0,05) proporção do endométrio ocupada por glândulas, enquanto que as fêmeas da FF apresentaram maior (P<0,05) proporção de tecido conjuntivo e vasos sanguíneos. Em conclusão, em fêmeas suínas pré-púberes, os parâmetros histomorfométricos, o diâmetro das glândulas endometriais, a altura do epitélio glandular e da TU e a proporção do endométrio ocupada por tecido conjuntivo, além das glândulas e vasos sanguíneos variam ao longo do ciclo estral, possivelmente devido à influência dos esteróides ovarianos.

Studies are performed in developing techniques/procedures that provide greater reproductive performance in farm animals, including pigs. In this sense, the study of gilts reproductive organs at different oestrus cycle stages for assessing the presence of abnormalities and/or other parameters that may affect the future animal fertility is important. In order to evaluate the morphological, morphometric and histomorphometric features of ovaries, uterus and uterine tubes (UTs) characteristics of prepubertal gilts at different oestrus cycle stages, reproductive tracts from 48 animals immediately after slaughter were obtained. After, the structures were dissected and removed, and the ovaries were used for classification of oestrus cycle stage of each gilt in follicular phase (FP) and luteal phase (FL). Then, morphometric evaluations of ovaries, UTs, uterine horns and uterine body were performed. Besides that, medial segments of UTs and uterus were fixed in Bouin solution, processed and included in paraffin, when histological sections of 5.0 micrometers (µm) were obtained and stained with Hematoxylin and Eosin. Histomorphometric analyzes using image capture system and specific software were performed. Afterwards, data were submitted to Student's t test for assessment the statistical differences (P<0.05) between the two different oestrus cycle stages (FP × LP) and between the placement of reproductive structures (right × left antimer). Among the gilts evaluated, 35 were in the FP and 13 in LP. There was no difference (P>0.05) between morphometric parameters of ovaries, UTs and uterus of gilts in FP and LP. Likewise, in respect to the placement of reproductive structures, both in the oestrus cycle stages, as in the general average, there was no difference (P>0.05). Regarding the histomorphometric variables, gilts classified in FP presented a higher (P<0.05) height of glandular and UT epithelium compared to animals in LP. On the other hand, the diameter of endometrial glands was higher (P<0.05) in gilts at LP compared to FP. Furthermore, gilts in LP presented a higher (P<0.05) proportion of endometrium occupied by glands, whereas animals in FP had a higher (P<0.05) proportion of connective tissue and blood vessels. In conclusion, in prepubertal gilts, the histomorphometric parameters as endometrial glands diameter, the height of glandular epithelium and of UT epithelium and the proportion of endometrium occupied by connective tissue, besides the glands and blood vessels varies through the oestrus cycle, possibly under the influence of ovarian steroids.

3769 downloads

A new approach for the synthesis of 3-substituted cytotoxic nor-β-lapachones
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Cardoso, Mariana F. C.

; Silva, Illana M. C. B. da

; Santos Júnior, Helvécio M. dos

; Rocha, David R.

; Araújo, Ana Jérsia

; Pessoa, Claudia

; Moraes, Manoel O. de

; Lotufo, Letícia V. C.

; Silva, Fernando de C. da

; Santos, Wilson C.

; Ferreira, Vitor F.

Journal of the Brazilian Chemical Society

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jan 2013, Volume 24 N. 1 Pages 12 - 16

Abstract: Pt En | Text: Pt En | PDF: Pt | PDF: En

Vários estudos têm mostrado o potencial citotóxico de derivados da nor-β-lapachona contra células tumorais. Considerando a nor-β-lapachona um importante protótipo, uma série inédita de nor-β-lapachonas substituídas em C-3 foi sintetizada através de uma nova metodologia sintética envolvendo intermediário sintético 3-hidróxi-nor-β-lapachona para o acoplamento de alguns nucleófilos contendo núcleos derivados de carboidratos ou 2H-pirazóis. Todos os derivados foram avaliados frente a quatro linhagens de células tumorais. Duas das substâncias apresentaram moderada citotoxicidade, enquanto as demais inibiram fortemente todas as linhagens tumorais testadas.

Several studies have demonstrated the cytotoxic potential of nor-β-lapachone derivative against cancer cells. Considering nor-β-lapachone as an important prototype, a set of new 3-substituted nor-β-lapachones was synthesized by a new synthetic route that involves the use of synthetic intermediate generated for coupling with several nucleophiles containing the carbohydrate and 2H-pyrazole substituent moieties. All the compounds were screened against four tumor cell lines. Two of the compounds showed moderate cytotoxicity, while the other compounds strongly inhibit all tested cancer cell lines.

2637 downloads

10.

Augmentation of catecholamine release elicited by an Eugenia punicifolia extract in chromaffin cells
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Pascual, Ricardo de

; Colmena, Inés

; Rios, Cristobal de los

; Rosa, Juliana M.

; Correa-Leite, Paulo E.

; Lima-Araújo, Kátia G.

; Ferreira, Vitor F.

; Rocha, David R.

; Gonzaga, Daniel T. G.

; García, Antonio G.

; Santos, Wilson C.

; Gandía, Luis

Revista Brasileira de Farmacognosia

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feb 2012, Volume 22 N. 1 Pages 1 - 12

Abstract: En | Text: En | PDF: En

Plant extracts of Eugenia punicifolia (Kunth) DC., Myrtaceae, are used in Amazon region of Brazil to treat diarrhea and stomach disturbances, and as hypoglycemic medicine. We have recently shown that an aqueous extract of E. punicifolia augmented cholinergic neurotransmission in a rat phrenic nerve-diaphragm preparation. In this study, we investigated the effects of an E. punicifolia dichloromethane extract (EPEX) in a neuronal model of cholinergic neurotransmission, the bovine adrenal chromaffin cell. EPEX augmented the release of catecholamine triggered by acetylcholine (ACh) pulses but did not enhance ACh-evoked inward currents, which were inhibited by 30%. Since EPEX did not cause a blockade of acetylcholinesterase or butyrylcholinesterase, it seems that EPEX is not directly activating the cholinergic system. EPEX also augmented K+-elicited secretion without enhancing the whole-cell inward calcium current. This novel and potent effect of EPEX in enhancing exocytosis might help to identify the active component responsible for augmenting exocytosis. When elucidated, the molecular structure of this active principle could serve as a template to synthesise novel compounds to regulate the exocytotic release of neurotransmitters.

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