Arzanol, a prenylated heterodimeric phloroglucinyl pyrone, inhibits eicosanoid biosynthesis and exhibits anti-inflammatory efficacy in vivo.

Based on its capacity to inhibit in vitro HIV-1 replication in T cells and the release of pro-inflammatory cytokines in monocytes, the prenylated heterodimeric phloroglucinyl α-pyrone arzanol was identified as the major anti-inflammatory and anti-viral constituent from Helichrysum italicum. We have now investigated the activity of arzanol on the biosynthesis of pro-inflammatory eicosanoids, evaluating its anti-inflammatory efficacy in vitro and in vivo. Arzanol inhibited 5-lipoxygenase (EC 7.13.11.34) activity and related leukotriene formation in neutrophils, as well as the activity of cyclooxygenase (COX)-1 (EC 1.14.99.1) and the formation of COX-2-derived prostaglandin (PG)E(2)in vitro (IC(50)=2.3-9μM). Detailed studies revealed that arzanol primarily inhibits microsomal PGE(2) synthase (mPGES)-1 (EC 5.3.99.3, IC(50)=0.4μM) rather than COX-2. In fact, arzanol could block COX-2/mPGES-1-mediated PGE(2) biosynthesis in lipopolysaccharide-stimulated human monocytes and human whole blood, but not the concomitant COX-2-derived biosynthesis of thromboxane B(2) or of 6-keto PGF(1α), and the expression of COX-2 or mPGES-1 protein was not affected. Arzanol potently suppressed the inflammatory response of the carrageenan-induced pleurisy in rats (3.6mg/kg, i.p.), with significantly reduced levels of PGE(2) in the pleural exudates. Taken together, our data show that arzanol potently inhibits the biosynthesis of pro-inflammatory lipid mediators like PGE(2)in vitro and in vivo, providing a mechanistic rationale for the anti-inflammatory activity of H. italicum, and a rationale for further pre-clinical evaluation of this novel anti-inflammatory lead

Application of Hansch’s Model to Capsaicinoids and Capsinoids: A Study Using the Quantitative Structure−Activity Relationship. A Novel Method for the Synthesis of Capsinoids

We describe a synthetic approach for two families of compounds, the capsaicinoids and capsinoids, as part of a study of the quantitative relationship between structure and activity

Ações de integração da zootecnia UDESC com a comunidade rural e urbana do oeste de Santa Catarina

Trabalho apresentado no 31º SEURS - Seminário de Extensão Universitária da Região Sul, realizado em Florianópolis, SC, no período de 04 a 07 de agosto de 2013 - Universidade Federal de Santa Catarina.Este trabalho apresenta as principais ações de extensão desenvolvidas pelo Curso de Zootecnia da UDESC, por meio dos dois programas de extensão universitária em execução no referido curso. Os dois programas têm como foco principal possibilitar intercâmbio de conhecimentos entre os meios rural e urbano e a Universidade, com foco em áreas variadas do conhecimento. As ações descritas neste trabalho fazem parte dos Programas “Interação UDESC - comunidade: Construção do conhecimento no meio rural e urbano” e “Conexão Zootecnia - UDESC e a Produção Animal”. O público-alvo envolve acadêmicos, população urbana, produtores rurais, técnicos do setor agropecuário e alunos de cursos do ensino fundamental, médio e superior da Região Oeste do Estado de Santa Catariana. Nestas ações, estão sendo realizadas abordagens sobre bem-estar de animais de rua e de companhia, manejo da bovinocultura de Leite, noções de geodésia e navegação com receptores de sinal de satélite, controle zootécnico de rebanhos e orientações sobre o controle parasitário, assim como realização de diagnóstico parasitológico animal. Como estratégias centrais das ações destacam-se parcerias com ONGs e sociedade visando minimizar a problemática de animais sob guarda não responsável e abandonados, capacitações para o uso de novas tecnologias, com curso sobre Noções Básicas e promoção de eventos integrativos sobre diferentes áreas da produção animal, com a promoção de cinco edições do 'CONECTA ZOO’. As ações realizadas em ambos os programas estão sendo desenvolvidas em municípios da região Oeste do Estado de Santa Catarina. A metodologia adotada visa o diálogo entre os participantes, de forma que os mesmos sintam-se a vontade para emitir opiniões, facilitando a troca de experiências e o aprendizado

SAR Studies on Curcumin's Pro-inflammatory Targets: Discovery of Prenylated Pyrazolocurcuminoids as Potent and Selective Novel Inhibitors of 5-Lipoxygenase.

The anticarcinogenic and anti-inflammatory properties of curcumin have been extensively investigated, identifying prostaglandin E2 synthase (mPGES)-1 and 5-lipoxygenase (5-LO), key enzymes linking inflammation with cancer, as high affinity targets. A comparative structure-activity study revealed three modifications dissecting mPGES-1/5-LO inhibition, namely (i) truncation of the acidic, enolized dicarbonyl moiety and/or replacement by pyrazole, (ii) hydrogenation of the interaryl linker, and (iii) (dihydro)prenylation. The prenylated pyrazole analogue 11 selectively inhibited 5-LO, outperforming curcumin by a factor of up to 50, and impaired zymosan-induced mouse peritonitis along with reduced 5-LO product levels. Other pro-inflammatory targets of curcumin (i.e., mPGES-1, cyclooxygenases, 12/15-LOs, nuclear factor-κB, nuclear factor-erythroid 2-related factor-2, and signal transducer and activator of transcription 3) were hardly affected by 11. The strict structural requirements for mPGES-1 and 5-LO inhibition strongly suggest that specific interactions rather than redox or membrane effects underlie the inhibition of mPGES-1 and 5-LO by curcumin

Broccoli, PTEN deletion and prostate cancer: where is the link?

The concept that vegetables and fruits are relevant sources of cancer-preventive substances is strongly supported by population studies. Among others, cruciferous vegetables like broccoli, cabbage, cauliflower and Brussels sprouts are thought to affect the development of various types of cancers and especially prostate tumors. Yet, the identification of the molecular mechanisms by which the 'active' compounds contained in these vegetables mediate their anticancer activity has historically lagged behind. Accordingly, direct laboratory evidence of how individual nutrients affect cancer genes and the pathways they control remains the major obstacle to progress in this research field. Here we review a recent report investigating the interaction between sulforaphane, a dietary isothiocyanate derived from broccoli, and expression of the PTEN tumor suppressor gene in pre malignant prostate tissue

Developmental patterns of a large set of barley (Hordeum vulgare) cultivars in response to ambient temperature

Ambient temperature plays an important role in plant development. In cereals, little is known about the exact effects of ambient temperature in the range between it being a vernalising agent and an abiotic stress factor; thus the genetic determinants involved in the registering and response to ambient temperature, and their natural variation has not been dissected either. Principally, we wished to establish the level of natural variation in response to ambient temperature in barley via studying plant phenological development. The responses to temperature of 168 barley genotypes of different provenances and seasonal growth habit groups were observed in controlled environments. The effects of four temperature regimes (13◦C, 16.5◦C, 18◦C and 23◦C) on the duration of plant phenophases were examined. The plant development was characterised in a series of consecutive phenophases that span the plant life cycle from germination through flowering to attainment of maximum plant height. Ambient temperature affected significantly plant development, with substantial variation in responses among the genotypes. Six major types of responses were identified, which depended strongly on seasonal growth habit, with only a small degree of overlap. Although the differences in the timing of development among clusters were significant under each temperature regime, the 23◦C treatment resulted in the largest diversity of responses, with significant changes in the ranking of the six clusters compared to other treatments. Two clusters showed particularly unusual responses to 23C: the development of one winter barley cluster was extremely accelerated by the 23C treatment, whereas the development of one spring barley cluster was significantly delayed. Ambient temperature assumes importance as a regulatory cue in the intricate and complex temporal and spatial regulation network of plant development in cereals and acts mostly through its regulatory effect on certain developmental phases such as the onset and duration of the intensive stem elongation