Synthesis of Analogues of Thyroid Hormones: Nuclear Receptor Modulators

Thyroid hormones are essential for the development and differentiation of all cells of the human body. This work reports the synthesis of some synthetic structural analogues of thyroid hormones, which may be modulators of the thyroid hormone receptor. The known compounds GC-1 (Sobetirome) and CG-24 were successfully prepared and two novel analogous molecules were also synthesized by a new and efficient synthetic methodology. DOI: http://dx.doi.org/10.17807/orbital.v7i3.73

Synthesis of Analogues of Thyroid Hormones: Nuclear Receptor Modulators

Thyroid hormones are essential for the development and differentiation of all cells of the human body. This work reports the synthesis of some synthetic structural analogues of thyroid hormones, which may be modulators of the thyroid hormone receptor. The known compounds GC-1 (Sobetirome) and CG-24 were successfully prepared and two novel analogous molecules were also synthesized by a new and efficient synthetic methodology. DOI: http://dx.doi.org/10.17807/orbital.v7i3.73

Synthesis of 4-azo-butenolides

<p>An efficient, catalyst-free, microwave-assisted approach has been developed for the synthesis of 4-azo-butyenolides derivatives by condensing tetronic acid with various anilines. This approach exhibited good functional group compatibility and produced the desired products in good to excellent yields in just 30–40 min. This approach can be seen as a better alternative to protocols with long reaction times used for the synthesis of these compounds, which are synthons for the obtaining of quinolines.</p

Effects of mycotoxin adsorbents in aflatoxin B 1 - and fumonisin B 1 -contaminated broiler diet on performance and blood metabolite

ABSTRACT The present study examined the effect of aflatoxin (AFB1) and fumonisin (FB1) at the levels of 2 mg kg&#8722;1 AFB1 and 100 mg kg&#8722;1 FB1 and the efficiency of use of different levels of adsorbent based on sodium and calcium aluminosilicate on growth performance, hematological parameters, and biochemical parameters of broilers. A total of 1,440 Cobb broilers were distributed into the following treatments: positive control (PC) - no mycotoxin and adsorbent (AD); PC+3AD - no mycotoxin, with 3 g kg&#8722;1 adsorbent in feed; negative control (NC) - only mycotoxin; NC+1AD - with mycotoxin and 1 g kg&#8722;1 adsorbent in feed; NC+2AD - with mycotoxin and 2 g kg&#8722;1 adsorbent in feed; and NC+3AD - with mycotoxin and 3 g kg&#8722;1 adsorbent in feed. The amounts of AFB1 and FB1 added to NC reduced weight gain (35%) and feed intake (50%) compared with PC; however, inclusion of 2 or 3 g kg&#8722;1 adsorbent to NC alleviated such losses. Birds fed NC showed anemia, immunosuppression, and impaired liver function, observed by reduced cholesterol and increased gamma glutamyl-transferase activity compared with PC; values returned to normal levels when 2 or 3 g kg&#8722;1 of the adsorbent (as fed) were used. Mycotoxins cause adverse effects on most of the parameters studied, and the use of adsorbent at the levels of 2 and 3 g kg&#8722;1 of the adsorbent as fed partially negates the adverse effect of mycotoxicosis

Efeito da redução dos níveis de fósforo nas dietas de poedeiras utilizando enzima fitase na fase de pós-pico de postura

A avicultura de postura tem evoluído muito nos últimos anos por ser um segmento importante na produção de alimento humano de alto valor biológico. Assim, tem se adequado técnicas que possibilitam a melhoria da eficiência de utilização dos nutrientes das rações pelas aves, reduzindo custos e aumentando a produção em quantidade e com qualidade. O experimento teve por objetivo estudar o efeito da adição da enzima fitase em rações com diferentes níveis de fósforo disponível, sobre as características de desempenho, qualidade da casca dos ovos e características dos dejetos de poedeiras comerciais. Foram utilizadas 384 poedeiras comerciais da linhagem Hy-Line White, com 46 semanas de idade. Foi utilizado um delineamento inteiramente casualizado em esquema fatorial 4x3 com quatro repetições de oito aves cada. Os tratamentos foram constituídos de quatro níveis de fósforo disponível (Pd) (0,40; 0,30; 0,20 e 0,10 %) e três níveis de inclusão da enzima fitase (0; 500 e 1000 FTU/Kg de ração) e as rações foram isonutritivas exceto para os níveis de Pd. Utilizou-se quatro ciclos de 28 dias para avaliação dos parâmetros de desempenho e das características de qualidade da casca do ovo. O menor nível de Pd proporcionou menor consumo e produção de ovos, diferindo (p<0,05) dos demais tratamentos e ao adicionar fitase neste nível de Pd houve interação (p<0,01), verificando resultado semelhante aos demais níveis de fósforo disponível

Convenient synthesis of ketal derivatives from cubebin using amberlite as heterogeneous catalyst

Eleven ketal derivatives were prepared from the natural product cubebin using Amberlite IR-120AR as heterogeneous catalyst and ROH as the source of the alkyl group.Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq

Atividade antimicrobiana in vitro das folhas de araçá (Psidium cattleianum Sabine) contra micro-organismos da mucosa oral

Resumo Introdução A espécie Psidium cattleianum Sabine tem despertado o interesse dos pesquisadores por apresentar, além de atividade cicatrizante, analgésica e antioxidante, propriedades antimicrobianas frente a micro-organismos da mucosa oral que podem atuar como agentes cariogênicos. Objetivo Foi avaliada, neste trabalho, a atividade antimicrobiana de extratos bruto e fracionados das folhas do araçá, além do seu perfil cromatográfico. Material e método Para avaliação da atividade antimicrobiana, foi utilizada a técnica de microdiluição, para determinação da Concentração Inibitória Mínima (CIM), e repique do inóculo em Ágar Muller Hinton (Himedia), para averiguação da Concentração Bactericida Mínima (CBM). O extrato foi testado nas concentrações entre 10 e 500 µg/mL. O perfil cromatográfico foi realizado pelo método de Cromatografia Líquida de Alta Eficiência (CLAE). Resultado Os resultados obtidos foram submetidos a uma análise descritiva e foi possível observar a atividade inibitória dos extratos do P. cattleianum contra S. mutans e S. oralis. Conclusão A atividade antimicrobiana dos extratos de P. cattleianum contra micro-organismos orais justifica maiores estudos para a utilização medicinal dessa espécie, como, por exemplo, sua utilização em enxaguantes bucais

In vitro efficacy of the essential oil of Piper cubeba L. (Piperaceae) against Schistosoma mansoni

In this paper, cercariae, schistosomula, and adult Schistosoma mansoni worms were incubated in vitro with the essential oil of Piper cubeba (PC-EO) at concentrations from 12.5 to 200 mu g/mL, and the viability was evaluated using an inverted microscopy. The effects of PC-EO at 100 and 200 mu g/mL on the stages of S. mansoni were similar to those of the positive control (PZQ at 12.5 mu g/mL), with total absence of mobility after 120 h. However, at concentrations from 12.5 to 50 mu g/mL, PC-EO caused a reduction in the viability of cercariae and schistosomula when compared with the negative control groups (RPMI 1640 or dechlorinated water) or (RPMI 1640 + 0.1% DMSO or dechlorinated water + 0.1% DMSO). On the other hand, adult S. mansoni worms remained normally active when incubated with PC-EO at concentrations of 12.5 and 25 mu g/mL, and their viabilities were similar to those of the negative control groups. In addition, at concentrations ranging from 50 to 200 mu g/mL, separation of all the coupled adult worms was observed after 24 h of incubation, which is related to the fact of the reduction in egg production at this concentration. The main chemical constituents of PC-EO were identified by gas chromatography-mass spectrometry as being sabinene (19.99%), eucalyptol (11.87%), 4-terpineol (6.36%), beta-pinene (5.81%), camphor (5.61%), and delta-3-carene (5.34%). The cytotoxicity of the PC-EO was determined, and a significant cytotoxicity was only obtained in the concentration of 200 mu g/mL after 24 h treatment. The results suggest that PC-EO possesses an effect against cercariae, schistosomula, and adult worms of the S. mansoni.CNPqCNPqFAPESPFAPESPFAPESPFAPESP [2009/15207-4, 2007/54241-8