New antitumoral agents I: In vitro anticancer activity and in vivo acute toxicity of synthetic 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one and derivatives

This paper describes a new method for the preparation of 1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadien-3-one 1 and its derivatives 2-5. This set of synthetic compounds exhibited high antitumoral activities regarding in vitro screening against several human tumor cell lines as lung carcinoma NCI-460, melanoma UACC-62, breast MCF-7, colon HT-29, renal 786-O, ovarian OVCAR-03 and ovarian expressing the resistance phenotype for adriamycin NCI-ADR/ RES, prostate PC-3, and leukemia K-562. Compounds were also tested against murine tumor cell line B16F10 melanoma and lymphocytic leukemia L1210 as well as to their effect toward normal macrophages. Specific activity against colon cancer cells HT-29 was observed for all tested compounds and suggests further studies with models of colon cancer. Compounds 1, 2, and 4 showed significant cytotoxic activity with IC(50) values <= 2.3 mu M for all human cancer cell lines. Intraperitoneal acute administration of compound 1 and 2 showed very low toxicity rate. (C) 2010 Elsevier Ltd. All rights reserved.

Constituents and antiproliferative activity of extracts from leaves of Croton macrobothrys

Croton macrobothrys Baill, Euphorbiaceae, is a tree from the Atlantic Forest in Southern Brazil, used in traditional medicine and popularly known as "dragon's blood" and "pau-sangue". Leaf n-hexane, dichloromethane and methanol extracts were analyzed by GC/MS and evaluated for their in vitro antiproliferative activity on cell lines 786-0 (kidney), HT-29 (colon), K562 (leukemia), NCI-ADR/RES (drug resistant ovary), NCI-H460 (lung), MCF-7 (mammary), PC-3 (prostate), OVCAR-3 (ovary), U251 (glioma) and UACC-62 (melanoma). The dicloromethane extract exhibited activity against all cell lines at the concentration 25 µg/mL, in particular on cell lines NCI-H460 (GI50 0.33 μg/mL) and K5662 (GI50 0.91 μg/mL). Relevant constituents in dichloromethane extract are the alkaloids corydine and salutaridine, as well as the diterpenes geranylgeraniol and crotonin-derived clerodanes.

Calorimetric investigations of luminescent films polycarbonate (PC) doped with europium complex [Eu(TTA)(3)(H(2)O)(2)]

Polymers doped with rare earth complexes are advantaged in film production for many applications in the luminescent field. In this luminescent polycarbonate (PC) films doped with diaquatris(thenoyltrifluoroacetonate)europium(III) complex [Eu(TTA)(3)(H(2)O)(2)] were prepared and their calorimetric and luminescent properties in the solid state are reported. The thermal behavior was investigated by utilization of differential scanning calorimetry (DSC) and thermogravimetry (TG). Due of the addition of rare earth [Eu(TTA)(3)(H(2)O)(2)] into PC matrix, changes were observed in the thermal behavior concerning the glass transition and thermal stability. Characteristic broadened narrow bands arising from the (5)D(0) -> (7)F(J) transitions (J = 4-0) of Eu(3+) ion indicate the incorporation of the Eu(3+) ions in the polymer. The luminescent films show enhancement emission intensity with an increase of rare earth concentration in polymeric matrix accompanied by decrease in thermal stability.

Analysis of peptides in prohormone convertase 1/3 null mouse brain using quantitative peptidomics

P>Neuropeptides are produced from larger precursors by limited proteolysis, first by endopeptidases and then by carboxypeptidases. Major endopeptidases required for these cleavages include prohormone convertase (PC) 1/3 and PC2. In this study, quantitative peptidomics analysis was used to characterize the specific role PC1/3 plays in this process. Peptides isolated from hypothalamus, amygdala, and striatum of PC1/3 null mice were compared with those from heterozygous and wild-type mice. Extracts were labeled with stable isotopic tags and fractionated by HPLC, after which relative peptide levels were determined using tandem mass spectrometry. In total, 92 peptides were found, of which 35 were known neuropeptides or related peptides derived from 15 distinct secretory pathway proteins: 7B2, chromogranin A and B, cocaine- and amphetamine-regulated transcript, procholecystokinin, proenkephalin, promelanin concentrating hormone, proneurotensin, propituitary adenylate cyclase-activating peptide, proSAAS, prosomatosatin, provasoactive intestinal peptide, provasopressin, secretogranin III, and VGF. Among the peptides derived from these proteins, similar to 1/3 were decreased in the PC1/3 null mice relative to wild-type mice, similar to 1/3 showed no change, and similar to 1/3 increased in PC1/3 null. Cleavage sites were analyzed in peptides that showed no change or that decreased in PC1/3 mice, and these results were compared with peptides that showed no change or decreased in previous peptidomic studies with PC2 null mice. Analysis of these sites showed that while PC1/3 and PC2 have overlapping substrate preferences, there are particular cleavage site residues that distinguish peptides preferred by each PC.

3-manifolds in Euclidean space from a contact viewpoint

We study the geometry of 3-manifolds generically embedded in R(n) by means of the analysis of the singularities of the distance-squared and height functions on them. We describe the local structure of the discriminant (associated to the distribution of asymptotic directions), the ridges and the flat ridges.

The doodle of a finitely determined map germ from R(2) to R(3)

Let f : U subset of R(2) -> R(3) be a representative of a finitely determined map germ f : (R(2), 0) -> (R(3), 0). Consider the curve obtained as the intersection of the image of the mapping f with a sufficiently small sphere s(epsilon)(2) centered at the origin in R(3), call this curve the associated doodle of the map germ f. For a large class of map germs the associated doodle has many transversal self-intersections. The topological classification of such map germs is considered from the point of view of the associated doodles. (C) 2009 Elsevier Inc. All rights reserved.

Pulpotomies with portland cement in human primary molars

Two clinical cases in which Portland cement (PC) was applied as a medicament after pulpotomy of mandibular primary molars in children are presented. Pulpotomy using PC was carried out in two mandibular first molars and one mandibular second molar, which were further followed-up. At the 3, 6 and 12-month follow-up appointments, clinical and radiographic examinations of the pulpotomized teeth and their periradicular area revealed that the treatments were successful in maintaining the teeth asymptomatic and preserving pulpal vitality. Additionally, the formation of a dentin bridge immediately below the PC could be observed in the three molars treated. PC may be considered as an effective alternative for primary molar pulpotomies, at least in a short-term period. Randomized clinical trials with human teeth are required in order to determine the suitability of PC before unlimited clinical use can be recommended.

Oral findings and dental care in a patient with myelomeningocele: case report of a 3-year-old child

Myelomeningocele (MMC) is a congenital malformation of the neural tube that occurs in the first weeks of pregnancy. This malformation refers to the caudal non-closure of the neural tube and neural tissue exposure, which lead to neurological problems, such as hydrocephalus, motor disability, genitourinary tract and skeletal abnormalities and mental retardation. Patients with MMC have an acknowledged predisposition to latex allergy and are usually at a high caries risk and activity due to poor oral hygiene, fermentable carbon hydrate-rich diet and prolonged use of sugar-containing medications. This paper addresses the common oral findings in pediatric patients with MMC, discusses the strategies and precautions to deal with these individuals and reports the dental care to a young child diagnosed with this condition.

Alterações dimensionais do côndilo mandibular em indivíduos de 3 a 20 anos de idade usando tomografia computadorizada de feixe cônico: um estudo preliminar

INTRODUÇÃO: o exame de tomografia computadorizada de feixe cônico (TCFC) oferece excelente representação dos tecidos duros da articulação temporomandibular (ATM). OBJETIVO: investigar as alterações morfológicas do côndilo mandibular, da infância à idade adulta, utilizando a TCFC. MÉTODOS: um estudo transversal foi conduzido envolvendo 36 côndilos de 18 indivíduos com idades variando entre 3 e 20 anos. As imagens dos côndilos foram obtidas por meio do sistema i-CAT e medidas com uma ferramenta do programa específica para ATM, que permite cortes perpendiculares à cabeça do côndilo, com correção individual em função das diferenças angulares de cada um. As maiores distâncias nas vistas lateral e frontal foram consideradas tanto para os côndilos do lado direto como para os do lado esquerdo. RESULTADOS: a dimensão lateral do côndilo mandibular parece ser estabelecida de maneira precoce, sofrendo poucas alterações com o passar dos anos, enquanto a dimensão frontal tende a aumentar. Assimetrias entre o côndilo esquerdo e o direito foram comumente observadas; no entanto, tais diferenças não apresentaram significância estatística para as vistas lateral (P=0,815) e frontal (P=0,374). CONCLUSÕES: os côndilos apresentaram simetria com relação ao tamanho, sendo observado crescimento apenas na dimensão frontal Os resultados sugerem que a TCFC constitui-se numa ferramenta útil na mensuração e avaliação das dimensões condilares.

Immediate implants placed into infected sockets: a case report with 3-year follow-up

The esthetics and functional integrity of the periodontal tissue may be compromised by dental loss. Immediate implants became a viable option to maintain the periodontal architecture because of their anatomic compatibility with the dental socket and the possibility of eliminating local contamination. This article describes the procedure of immediate implant placement in the anterior maxilla replacing teeth with chronic periapical lesions, which were condemned due to endodontic lesions persisting after failed endodontic treatment and endodontic surgery, and discusses the relationship between the procedure and periapical lesions. Surgical removal of hopeless teeth 11, 12 and 21 was performed conservatively in such a way to preserve the anatomy and gingival esthetics. A second surgical access was gained at the apical level, allowing the debridement of the surgical chamber for elimination of the periapical lesion, visual orientation for setting of the implants and filling of the surgical chamber with xenogenous bovine bone graft. After this procedure, the bone chamber was covered with an absorbent membrane and the healing screws were positioned on the implants. Later, a provisional partial removable denture was installed and the implants were inserted after 6 months. After 3 years of rehabilitation, the implants present satisfactory functional and esthetic conditions, suggesting that immediate implant placement combined with guided bone regeneration may be indicated for replacing teeth lost due to chronic periapical lesions with endodontic failure history in the anterior maxilla.

Utilização de levedura íntegra e seus derivados em dietas para juvenis de tilápia do Nilo

Neste trabalho, avaliou-se a adição de células íntegras de levedura e seus derivados em dietas para juvenis de tilápia do Nilo. Foram utilizados 144 juvenis machos de tilápia (peso médio de 52,1g) distribuídos em 12 tanques de fibra de vidro (250L), em delineamento inteiramente casualizado, composto por quatro tratamentos e três repetições. Os peixes foram alimentados ad libitum, duas vezes ao dia durante 60 dias, com dietas isoproteicas (28% PB) e isocalóricas (2.900kcal de ED kg-1) contendo levedura íntegra de cana-de-açúcar (LI), levedura autolisada (LA) e parede celular (PC) adicionados na proporção de 25% da proteína bruta total, comparadas com uma dieta controle (CO), sem adição de levedura. Não foram observadas diferenças significativas para conversão alimentar aparente e taxa de eficiência protéica. No entanto, o ganho em peso foi melhor nos peixes alimentados com as dietas LA (114,70g) e PC (131,03g), assim como em relação à taxa de crescimento específico (LA=1,79 e PC=1,93%), à proteína bruta no ganho de peso (LA=14,45 e PC=15,62%) e ao conteúdo corporal proteico (LA=14,89 e PC=15,67g 100g-1). As frações, a parede celular e a levedura autolisada de cana-de-açúcar podem ser utilizadas em dietas para juvenis de tilápia.

Desempenho produtivo, características de carcaça e avaliação econômica de bovinos cruzados, castrados e não-castrados, terminados em pastagens de Brachiaria decumbens

Avaliou-se o efeito da castração sobre o desempenho produtivo e sobre as características de carcaça e realizou-se a avaliação econômica de bovinos terminados em pastagens de Brachiaria decumbens. Foram utilizados oito novilhos Canchim-Nelore com 14 meses de idade, sendo quatro animais castrados e quatro não-castrados, com média de peso corporal de 273,2kg. O delineamento foi inteiramente ao acaso com quatro repetições por tratamento. Os animais receberam, diariamente, 0,7% do PC de suplemento proteíco-energético e foram abatidos aos 26 meses de idade. O peso de abate e o ganho médio diário (GMD) diferiram entre castrados e não-castrados, com médias de 441,0 e 482,2kg e 0,6 e 0,7kg/dia, respectivamente. Não houve efeito da castração sobre as características avaliadas, com exceção do peso de abate, do peso da carcaça quente, 252,3 versus 229,9kg, da cor da carne, 3,25 versus 4,50 pontos e da espessura da gordura subcutânea, 0,6 versus 1,4mm, respectivamente, para não-castrados e castrados. A lucratividade por animal e por hectare foi de 14,5 e 15,8% para não-castrados e 4,5 e 5,8% para castrados, respectivamente. Sugere-se a utilização de bovinos não-castrados suplementados em pastagens de Brachiaria decumbens.

Modulation of peritoneal macrophage activity by the saturation state of the fatty acid moiety of phosphatidylcholine

To determine the effects of saturated and unsaturated fatty acids in phosphatidylcholine (PC) on macrophage activity, peritoneal lavage cells were cultured in the presence of phosphatidylcholine rich in saturated or unsaturated fatty acids (sat PC and unsat PC, respectively), both used at concentrations of 32 and 64 µM. The treatment of peritoneal macrophages with 64 µM unsat PC increased the production of hydrogen peroxide by 48.3% compared to control (148.3 ± 16.3 vs 100.0 ± 1.8%, N = 15), and both doses of unsat PC increased adhesion capacity by nearly 50%. Moreover, 64 µM unsat PC decreased neutral red uptake by lysosomes by 32.5% compared to the untreated group (67.5 ± 6.8 vs 100.0 ± 5.5%, N = 15), while both 32 and 64 µM unsat PC decreased the production of lipopolysaccharide-elicited nitric oxide by 30.4% (13.5 ± 2.6 vs 19.4 ± 2.5 µM) and 46.4% (10.4 ± 3.1 vs 19.4 ± 2.5 µM), respectively. Unsat PC did not affect anion production in non-stimulated cells or phagocytosis of unopsonized zymosan particles. A different result pattern was obtained for macrophages treated with sat PC. Phorbol 12-miristate 13-acetate-elicited superoxide production and neutral red uptake were decreased by nearly 25% by 32 and 64 µM sat PC, respectively. Sat PC did not affect nitric oxide or hydrogen peroxide production, adhesion capacity or zymosan phagocytosis. Thus, PC modifies macrophage activity, but this effect depends on cell activation state, fatty acid saturation and esterification to PC molecule and PC concentration. Taken together, these results indicate that the fatty acid moiety of PC modulates macrophage activity and, consequently, is likely to affect immune system regulation in vivo.

A new bianthron glycoside as inhibitor of Trypanosoma cruzi glyceraldehyde 3-phosphate dehydrogenase activity

A phytochemical investigation of the ethanolic extract of stalks of Senna martiana Benth. (Leguminoseae), native specie of northeast Brazil, resulted in the isolation and spectroscopic characterization of a new bianthrone glycoside, martianine 1 (10,10'-il-chrysophanol-10-oxi10,10'-bi-glucosyl). Its identification was established by HRMS, IR and 2D NMR experiments. The evaluation of martianine trypanocidal activity was carried out against gliceraldehyde 3-phosphate dehydrogenase enzyme from Trypanosoma cruzi. Its inhibitory constant (Ki) is in the low micromolar concentration and it was determined by isothermal titration calorimetry to be 27.3 ± 2.47 µmol L-1. The non-competitive mechanism is asserted to be putative of the mode of action martianine displays against T. cruzi GAPDH. Results show that martianine has a great potential to become new lead molecule by inhibiting this key enzyme and for the development of new drugs against Chagas disease.