The effect of aging on the accuracy of marginal adaptation and fracture resistance of CAD/CAM PEEK single crown restoration

Aim: In recent years, great advances have been made in the use of CAD/CAM to prepare fixed restorations. The marginal and internal fit of these restorations is a principal determinant for their clinical success. In addition, the nature of the oral environment affects the mechanical properties of these restorations. Therefore, this study aimed to investigate the effect of aging process under conditions that simulate the oral environment on the marginal adaptation, and, fracture resistance of crowns fabricated from polyether ether ketone (PEEK) using CAD/CAM methods. Methods: Twenty identical crown restorations were fabricated by using CAD/CAM methods to mill polyether ether ketone (PEEK) material. These crowns were produced by using a software design of an epoxy resin replica of the prepared maxillary first premolar tooth. All PEEK crowns were cemented and randomly divided into two equal groups (A, B). Each group was divided into subgroups (A1, A2 and B1, B2). Group A1 and A2 were used to measure marginal adaptation and fracture resistance, respectively, before aging, while group (B1 and B2) were measured after aging. The cemented crowns were mounted in resin molds to facilitate the sectioning process. The measurements of the marginal gap were performed after sectioning at four points using a stereomicroscope. The fracture resistance of the crowns was investigated using a universal testing machine. A statistical analysis was performed using the GraphPad Prism® software version and unpaired Student's t-test. Results: The results revealed that aging affected the marginal gap, and the fracture resistance of the PEEK crowns. While aging, negatively affected the conditions under investigation, however the least significant difference of marginal gap was found in the margin region. Conclusions: PEEK-CAD/CAM is considered as a good alternative prosthodontic material for fixed prostheses. The CAD/CAM technique used to make PEEK crown restorations in our study offers the advantages of high marginal accuracy and fracture resistance for long-term performance in the oral environment

Comparative study between Plate-Graff, Plate-Cage and PEEK cage in cervical spine fusion / Estudio comparativo entre Plate-Graff, Plate-Cage y Peek cage en la fusión de la columna cervical

Abstract: Objective: To compare results of Plate-Graff, Plate-Cage and PEEK cage in patients with cervical stenosis. Material and methods: Prospective, with before and after intervention and comparative study. From January 2005 to October 2011 we included 37 patients (male: 48.6%, female: 51.4%) post-surgery by anterior approach; 3 groups via: Group I, arthrodesis with Plate-Graff n = 12 (M 41.7%, F 58.3%) with 22 levels, group II, Plate-Cage n = 11 (M 63.6% 36.4% F) 19 levels, group III, PEEK cage, n = 14 (M 0% F 50%) with 25 levels. Functional assessment pre- and postoperative with neck disability index (NDI) and visual analogue scale for pain (VAS). The radiological assessment with X-rays only. Descriptive statistics were obtained. Wilcoxon method use according to data distribution, non parametric tests of ranges with sign of Kruskal-Wallis for comparison between more than two groups, and significance level with p < 0.05. We used the statistical package SPSS version 15. Results: The majority of patients was found between the sixth and eighth decade of life. At one year of follow up the NDI and pain with VAS shown improvement with statistical difference in three groups (p = 0.001). However, the radiographic measurements per year of follow-up showed a significant improvement of segmental lordosis (p = 0.02) only in patients with Plate-Graff. Conclusions: Using the graft offers best clinical and radiographic results compared with the Plate Cage and box peek to one year of follow-up.

Resumen: Objetivo: Comparar resultados de placa-injerto, caja-placa y caja-PEEK, en pacientes con conducto cervical estrecho. Material y métodos: Estudio prospectivo, en panel antes y después, de intervención y comparativo. De Enero de 2005 a Octubre de 2011, muestra de 37 pacientes (masculino: 48.6%, femenino: 51.4%) postoperados por vía anterior; formando tres grupos: grupo I, artrodesis con placa-injerto n = 12 (M 41.7%, F 58.3%) con 22 niveles; grupo II, caja-placa n = 11 (M 63.6%, F 36.4%) con 19 niveles; grupo III, caja-PEEK, n = 14 (M 50%, F 50%) con 25 niveles. La evaluación funcional pre- y postoperatoria mediante la escala de discapacidad cervical y escala visual análoga de dolor. La evaluación radiológica con radiografías de columna cervical. Se obtuvo estadística descriptiva. De acuerdo con la distribución de los datos se usaron pruebas no paramétricas de rangos con signo de Wilcoxon, y Kruskal-Wallis para comparación entre más de dos grupos. Con nivel de significancia de p<0.05. Se utilizó el paquete estadístico SPSS versión 15. Resultados: La mayoría de los pacientes se encontró entre la sexta y octava década de la vida. Al año de postoperados el índice de discapacidad cervical y mejoría del dolor con EVA mostraron mejoría con diferencia estadística en los tres grupos (p = 0.001). Sin embargo, las mediciones radiográficas al año de seguimiento mostraron una mejoría significativa de la lordosis segmentaria (p = 0.02) sólo en pacientes operados con placa-injerto. Conclusiones: El uso de la placa-injerto ofrece mejores resultados clínicos y radiográficos en comparación con la caja-placa y caja-PEEK, al año de seguimiento.

Marine drugs for cancer: surfacing biotechnological innovations from the oceans

This review will discuss the contributions of marine natural molecules, a source only recently found to have pharmaceutical prospects, to the development of anticancer drugs. Of the seven clinically utilized compounds with a marine origin, four are used for the treatment of cancer. The development of these drugs has afforded valuable knowledge and crucial insights to meet the most common challenges in this endeavor, such as toxicity and supply. In this context, the development of these compounds will be discussed herein to illustrate, with successful examples provided by cytarabine, trabectedin, eribulin and brentuximab vedotin, the steps involved in this process as well as the scientific advances and technological innovation potential associated with developing a new drug from marine resources.

Asymmetric bioreduction of ketoesters derivatives by Kluyveromyces marxianus: influence of molecular structure on the conversion and enantiomeric excess

ABSTRACT This study presents the bioreduction of six β-ketoesters by whole cells of Kluyveromyces marxianus and molecular investigation of a series of 13 β-ketoesters by hologram quantitative structure-activity relationship (HQSAR) in order to relate with conversion and enantiomeric excess of β-stereogenic-hydroxyesters obtained by the same methodology. Four of these were obtained as (R)-configuration and two (S)-configuration, among them four compounds exhibited >99% enantiomeric excess. The β-ketoesters series LUMO maps showed that the β-carbon of the ketoester scaffold are exposed to undergo nucleophilic attack, suggesting a more favorable β-carbon side to enzymatic reduction based on adopted molecular conformation at the reaction moment. The HQSAR method was performed on the β-ketoesters derivatives separating them into those provided predominantly (R)- or (S)-β-hydroxyesters. The HQSAR models for both (R)- and (S)-configuration showed high predictive capacity. The HQSAR contribution maps suggest the importance of β-ketoesters scaffold as well as the substituents attached therein to asymmetric reduction, showing a possible influence of the ester group carbonyl position on the molecular conformation in the enzyme catalytic site, exposing a β-carbon side to the bioconversion to (S)- and (R)-enantiomers.

Bonding of the Polymer Polyetheretherketone (PEEK) to Human Dentin: Effect of Surface Treatments

Abstract Polyetheretherketone (PEEK) is a material suitable for frameworks of fixed dental prostheses. The effect of different surface treatments on the bond strength of PEEK bonded to human dentin was evaluated. One hundred PEEK cylinders (3 mm×3 mm) were divided into five groups according to surface treatment: silica coating, sandblasting with 45 μm Al2O3 particles, etching with 98% sulfuric acid for 5, 30 and for 60 s. These cylinders were luted with resin cement onto 50 human molars. First, each tooth was embedded in epoxy resin and the buccal dentin surface was exposed. Then, two delimited dentin areas (Æ:3 mm) per tooth were etched with 35% phosphoric acid and bonded with a two-step self-priming adhesive system. After the luting procedure the specimens were stored in water (24 h/37 °C). Shear bond strength (SBS) was tested using a universal testing machine (crosshead speed 0.5 mm/min; load cell 50 kgf) and failure types were assessed. Stress data (MPa) were analyzed using the Kruskal-Wallis test. Comparison of the proportions of different failure types was performed using the Bonferroni method (p<0.05). Kruskal-Wallis demonstrated that differences among groups were not significant (p=0.187). Mean SBS were as follows: silica coating, 2.12±1.12 MPa; sandblasting, 2.37±0.86 MPa; sulfuric acid 5 s, 2.28±1.75 MPa; sulfuric acid 30 s, 1.80±0.85 MPa; sulfuric acid 60 s, 1.67±0.94 MPa. Adhesive and mixed failures were predominant in all groups. Both physical and chemical surface treatments produced adhesion between PEEK, resin cement and dentin.

Resumo O poli-éter-éter-cetona (PEEK) é um material indicado para as estruturas de próteses parciais fixas. O efeito de diferentes tratamentos de superfície na resistência de união entre PEEK e dentina humana foi avaliado. Cem cilindros de PEEK (3 mm×3 mm) foram divididos em cinco grupos de acordo com tratamento de superfície: silicatização, jateamento com partículas de Al2O3 45 µm, condicionamento com ácido sulfúrico 98% por 5, 30 e 60 s. Esses cilindros foram cimentados com cimento resinoso em cinquenta molares humanos. Primeiro, cada dente foi incluído em resina epóxica e a superfície dentinária vestibular foi exposta. Depois, duas áreas (Æ:3 mm) em dentina/por dente foram delimitadas, condicionadas com ácido fosfórico a 35% e receberam aplicação de um sistema adesivo de dois passos. Após o procedimento de cimentação, as amostras foram armazenadas em água (24 h/37 °C). A resistência da união ao cisalhamento (SBS) foi testada em uma máquina universal de ensaios (velocidade 0,5 mm/min; célula de carga 50 kgf), e foram avaliados os tipos de falha. Os dados de tensão (MPa) foram analisados pelo teste de Kruskal-Wallis. A comparação das percentagens de diferentes tipos de falha foi realizada utilizando o método de Bonferroni (p<0,05). O teste de Kruskal-Wallis demonstrou que as diferenças entre os grupos não foram significantes (p=0,187). As médias de SBS foram: silicatização, 2,12±1,12 MPa; jateamento, 2,37±0,86 MPa; ácido sulfúrico por 5 s, de 2,28±1,75 MPa; ácido sulfúrico por 30 s, 1,80±0,85 MPa, ácido sulfúrico por 60 s, 1,67±0,94 MPa. Falhas adesivas e mistas foram predominantes em todos os grupos. Ambos tratamentos de superfície, físicos e químicos, promoveram adesão entre PEEK, cimento resinoso e dentina.

Comparative in vitro evaluation of CAD/CAM vs conventional provisional crowns

ABSTRACT Objective This study compared the marginal gap, internal fit, fracture strength, and mode of fracture of CAD/CAM provisional crowns with that of direct provisional crowns. Material and Methods An upper right first premolar phantom tooth was prepared for full ceramic crown following tooth preparation guidelines. The materials tested were: VITA CAD-Temp®, Polyetheretherketone “PEEK”, Telio CAD-Temp, and Protemp™4 (control group). The crowns were divided into four groups (n=10), Group1: VITA CAD-Temp®, Group 2: PEEK, Group 3: Telio CAD-Temp, and Group 4: Protemp™4. Each crown was investigated for marginal and internal fit, fracture strength, and mode of fracture. Statistical analysis was performed using GraphPad Prism software version 6.0. Results The average marginal gap was: VITA CAD-Temp® 60.61 (±9.99) µm, PEEK 46.75 (±8.26) µm, Telio CAD-Temp 56.10 (±5.65) µm, and Protemp™4 193.07(±35.96) µm (P<0.001). The average internal fit was: VITA CAD-Temp® 124.94 (±22.96) µm, PEEK 113.14 (±23.55) µm, Telio CAD-Temp 110.95 (±11.64) µm, and Protemp™4 143.48(±26.74) µm. The average fracture strength was: VITA CAD-Temp® 361.01 (±21.61) N, PEEK 802.23 (±111.29) N, Telio CAD-Temp 719.24 (±95.17) N, and Protemp™4 416.40 (±69.14) N. One-way ANOVA test showed a statistically significant difference for marginal gap, internal gap, and fracture strength between all groups (p<0.001). However, the mode of fracture showed no differences between the groups (p>0.05). Conclusions CAD/CAM fabricated provisional crowns demonstrated superior fit and better strength than direct provisional crowns.

Frequent users of emergency services: associated factors and reasons for seeking care / Usuários frequentes de serviço de emergência: fatores associados e motivos de busca por atendimento / Usuarios frecuentes de servicios de emergencia: factores asociados y motivos de la búsqueda de atención

Aim: to identify the profile of frequent users of emergency services, to verify the associated factors and to analyze the reasons for the frequent use of the services. METHOD: An explanatory sequential type mixed method was adopted. Quantitative data were collected from the electronic medical records, with a sample of 385 users attended four or more times in an emergency service, during the year 2011. Qualitative data were collected through semi-structured interviews with 18 users, intentionally selected from the results of the quantitative stage. Quantitative data were analyzed using descriptive and inferential statistics and qualitative data using thematic analysis. RESULTS: It was found that 42.9% were elderly, 84.9% had chronic diseases, 63.5% were classified as urgent, 42.1% stayed for more than 24 hours in the service and 46.5% were discharged. Scheduled follow-up appointment, risk classification, length of stay and outcome were factors associated with frequent use. The reasons for seeking the services were mainly related to the exacerbation of chronic diseases, to easier access and concentration of technology, to the bond, and to the scheduled appointments. CONCLUSIONS: The results contribute to comprehending the repeated use of emergency services and provide additional data to plan alternatives to reduce frequent use. .

OBJETIVO: identificar o perfil de usuários frequentes de serviço de emergência, verificar fatores associados e analisar os motivos para utilização frequente do serviço. MÉTODO: adotou-se método misto, do tipo sequencial explanatório. Os dados quantitativos foram coletados em registros de prontuários eletrônicos, com amostra de 385 usuários, atendidos quatro vezes ou mais em um serviço de emergência, durante o ano de 2011. Os dados qualitativos foram obtidos por meio de entrevistas semiestruturadas, com 18 usuários, selecionados intencionalmente a partir dos resultados da etapa quantitativa. Os dados quantitativos foram analisados com estatística descritiva e inferencial e os qualitativos com análise temática. RESULTADOS: identificou-se que 42,9% eram idosos, 84,9% tinham doenças crônicas, 63,5% foram classificados como urgentes, 42,1% permaneceram mais de 24 horas no serviço e 46,5% tiveram alta. Os fatores associados à utilização frequente são retorno agendado, classificação de risco, tempo de permanência e desfecho. Os motivos da busca pelo serviço são relacionados, principalmente, à agudização de doenças crônicas, maior facilidade de acesso, concentração de tecnologia, vínculo e retornos agendados. CONCLUSÕES: os resultados contribuem para compreensão do uso repetido de serviços de emergência e oferecem subsídios para planejamento de alternativas para redução da utilização frequente. .

OBJETIVO: identificar el perfil de usuarios frecuentes de servicios de emergencia, verificar los factores asociados y analizar los motivos para utilización frecuente de ese servicio. MÉTODO: se adoptó un método mixto del tipo secuencial explicativo. Los datos cuantitativos fueron recolectados en registros de fichas electrónicas, con muestra de 385 usuarios atendidos cuatro veces o más, en un servicio de emergencia, durante el año de 2011. Los datos cualitativos fueron obtenidos por medio de entrevistas semiestructuradas con 18 usuarios, seleccionados intencionalmente a partir de los resultados de la etapa cuantitativa. Los datos cuantitativos fueron analizados con estadística descriptiva e inferencial y los cualitativos con análisis temático. RESULTADOS: se identificó que 42,9% eran ancianos, 84,9% tenían enfermedades crónicas, 63,5% fueron clasificados como urgentes, 42,1% permanecieron más de 24 horas en el servicio y 46,5% tuvieron alta para el domicilio. El retorno programado, la clasificación de riesgo, el tiempo de permanencia y el resultado, son factores asociados a la utilización frecuente. Los motivos de la búsqueda por el servicio son relacionados, principalmente a: la agudización de enfermedades crónicas, la mayor facilidad de acceso y concentración de tecnología, los vínculos, y a los retornos programados. CONCLUSIONES: los resultados contribuyen para la comprensión del uso repetido de servicios de emergencia y ofrecen informaciones para planificar alternativas para reducción de la utilización frecuente. .

Volatile composition of peppermint (Mentha piperita L.) commercial teas through solid phase extraction

Volatiles from aqueous extract of peppermint commercial sachets were investigated through gas chromatography/flame ionization detection (GC/FID) and GC/mass spectrometry (MS). Samples were prepared under similar conditions as in homemade tea. Volatiles were isolated using solid phase extraction method (SPE) with Porapak Q trap followed by desorption with acetone. Estimated mean values for short and medium chain carboxylic acids (C2- C12) and ketones lay in the range of 50-64 μg kg-1 whilst aliphatic alcohols and acyclic hydrocarbons had values lower than 6 μg kg-1. The major volatiles were terpenes (275-382 μg kg-1) that reached 89 % of the total composition. A total of 16 compounds, among them dodecane, acetoin, acetol, citral, geraniol and octanoic acid have been described by the first time in peppermint tea. These findings could be attributed to the different analytical approach employed, mainly to the use of different extraction/pre-concentration techniques. Given the apparently lower proportion of terpenes in the aqueous extract it may be that the chemical properties of the peppermint essential oil are not entirely reproduced with homemade tea.

Estudo da composição da fração volátil do extrato aquoso de sachês de hortelã pimenta (Mentha piperita L.) através da extração em fase sólida. O princípio desse trabalho foi investigar a fração volátil do extrato aquoso de sachês comerciais de hortelã pimenta usando cromatografia gasosa com detectores de ionização em chama e de massas. As amostras foram preparadas em condições similares às usadas para o preparo do chá caseiro. Os compostos voláteis foram isolados via método de extração em fase sólida com adsorvente Porapak Q e eluídos com acetona. Uma estimativa dos valores médios dos ácidos carboxílicos de cadeias média e curta ficou na faixa de 50-64 μg kg-1, enquanto alcoóis alifáticos e hidrocarbonetos acíclicos tiveram valores menores do que 6 μg kg-1. Os terpenos (275-382 μg kg-1) foram os compostos majoritários alcançando 89 % dos sólidos totais. Um total de 16 compostos voláteis, entre eles, dodecano, acetoína, acetol, citral, geraniol e ácido octanóico foram descritos pela primeira vez no chá de hortelã pimenta. Esses resultados poderiam ser atribuídos aos diferentes métodos analíticos empregados, principalmente devido ao uso de diferentes técnicas de extração e pré-concentração. Em função da proporção menor de terpenos no extrato aquoso é razoável especular que as propriedades químicas do óleo essencial da hortelã pimenta não sejam totalmente reproduzidas com o consumo do chá caseiro.

Reconstrucción de la bóveda craneana con implante de poli-éter-éter-cetona diseñado por computadora: informe de un caso / Cranial vault reconstruction using computer-designed polyetheretherketone (PEEK) implant: case report

Introducción: La reconstrucción de los huesos del cráneo es un procedimiento complejo y representa un reto para el grupo médico tratante; generalmente se realiza en pacientes con pérdida de la bóveda craneana secundaria a procesos infecciosos crónicos no controlados o por osteorradionecrosis, lo que implica mayor posibilidad de fracaso o rechazo de los materiales utilizados para la reparación del defecto. La selección del material para sustituir la bóveda craneana es difícil debido a la diversidad de productos existentes; el material debe ser inerte, ligero, fácil de colocar y adaptable al defecto, con lo cual se ofrece mejores resultados estéticos y funcionales. Con el diseño por computadora del implante es posible ofrecer un implante individual y específico para cada defecto y paciente. Caso clínico: Mujer con diagnóstico de estesioneuroblastoma tratada con resección craneofacial anterior y radioterapia; como complicación presentó osteomielitis y osteorradionecrosis y, consecuentemente, pérdida de la bóveda craneana en la región frontal; este defecto fue reconstruido con un implante de poli-éter-éter-cetona diseñado por computadora con base en el defecto evaluado por tomografía computarizada. Se muestran los resultados obtenidos. Conclusiones: El implante diseñado por computadora realizado con poli-éter-éter-cetona es una alternativa segura, fácil de usar y con gran adaptabilidad a los defectos de la bóveda craneana.

BACKGROUND: Reconstruction of the bones of the skull is a complex procedure and represents a challenge for the surgical team. It is generally performed in patients who have loss of the cranial vault secondary to chronic infection or uncontrolled osteoradionecrosis, indicating a greater chance of failure or rejection of the materials used for repair of the defect. Selection of material to replace the cranial vault is complex due to the diversity of existing products. The ideal material is inert, lightweight, easy to fit and adaptable to the defect, offering the best aesthetic and functional results. Computer design of the implant makes this process easier by providing an implant specific to each individual patient and defect. CLINICAL CASE: We report the case of a patient who was diagnosed with esthesioneuroblastoma and was treated with anterior craniofacial resection and radiotherapy. Osteomyelitis and osteoradionecrosis were consequent complications with loss of the cranial vault in the frontal region. The defect was reconstructed with a polyetheretherketone (PEEK) computer-designed implant based on the defect evaluated by computed tomography. Results obtained are shown below. CONCLUSIONS: The PEEK computer-designed implant is a safe and easy to use alternative with great adaptability to cranial vault defects.

Lipoxygenase inhibitory tetraketones: potential Remedial source for inflammation and asthma / Las tetracetonas inhibidoras de la lipoxigenasa: fuente potencial Remedial para la inflamación y el asma

OBJETIVE: A series of tetraketones has been synthesized by way of a one pot synthesis and screened for inhibitory activity against the enzyme lipoxygenase. METHOD: An efficient and high yielding one pot synthesis to tetraketones [2-22] has been developed by way of tetraethyl ammonium bromide (Et4N+Br-) mediated condensation of cyclohexane-1, 3-dione [1] with a variety of aldehydes. Lipoxygenase enzyme solution was prepared so that enzyme concentration in reaction mixture was adjusted to give rates of 0.05 absorbance/minute. The test compounds were prepared in methanol of concentrations 50, 25, 12.5, 6.25 and 3.125 µM. The reaction mixture contained 160 µL (100 mM) sodium phosphate buffer (pH 8.0), 10µL of test-compound solution and 20µL of lipoxygenase solution. The contents were mixed and incubated for 10 minutes at 25ºC. The reaction was then initiated by the addition of 10µL substrate solution (linoleic acid, 0.5 mM, 0.12% w/v tween 20 in the ratio of 1:2), with the formation of (9Z,11E)-(13S)-13-hydroperoxyoctadeca-9,11-dienoate, the change of absorbance at 234 nm was followed for 6 minutes. The concentrations of the test compounds that inhibited the lipoxygenase activity by 50% (IC50) were determined by monitoring the effect of increasing concentrations of these compounds in the assays on the degree of inhibition. The IC50 values were calculated by means of the EZ-Fit Enzyme-Kinetics Program (Perrella Scientific Inc., Amherst, USA). RESULT: The tetraketones [2-22] were synthesized in high yields (91-98%) using mild reaction conditions. Most of these compounds showed significant inhibitory activity against the enzyme lipoxygenase. It was found that the presence of substituents which increase delocalization of electrons enhances the inhibitory activity. CONCLUSION: It is concluded that the study is likely to lead to the discovery of therapeutically efficient agents against important disorders such as inflammation and asthma.

OBJETIVO: Una serie de tetracetonas han sido sintetizadas mediante síntesis de varios pasos en un solo reactor (one-pot), y examinadas en relación con su actividad inhibitoria frente a la enzima lipoxigenasa. MÉTODO: Una síntesis one-pot de un rendimiento alto y eficiente para la obtención de tetracetonas (2-22) ha sido desarrollada mediante bromuro amónico tetraetílico (Et4N+Br-) - de ciclohexano-1,3-diona, con una variedad de aldehídos. La solución de enzima lipoxigenasa fue preparada de modo que la concentración de la enzima en las mezcla de la reacción fue ajustada para que diera tasas de 0.05 absorbancia/minuto. Los compuestos de la prueba fueron preparados en metanol de concentraciones (50, 25, 12.5, 6.25 y 3.125 µM). La mezcla de reacción contenía 160 µL (100 mM) de un tampón (buffer) de fosfato de sodio (pH 8.0), 10µL de solución de compuesto de prueba, y 20µL de solución de lipoxigenasa. Los contenidos fueron mezclados e incubados por 10 minutos a 25ºC. La reacción fue iniciada entonces por la adición de 10µL de solución substrato (ácido linoleico, 0.5 mM, 0.12% p/v tween 20 en proporción de 1:2), con la formación de (9Z, 11E)-(13S)-13-hidroperoxioctadeca-9,11-dienoato, el cambio de absorbancia a 234 nm fue seguido por 6 minutos. Las concentraciones de los compuestos de prueba que inhibían la actividad de la lipoxigenasa en un 50% (IC50) fueron determinadas monitoreando el efecto del aumento de las concentraciones de estos compuestos en los ensayos sobre el grado de inhibición. Los valores IC50 fueron calculados mediante el Programa Cinética de la Enzima EZ-Fit (Perrella Scientific Inc., Amherst, USA). RESULTADOS: Las tetracetonas (2-22) se sintetizaron con elevados rendimientos (91-98%) usando condiciones de reacción leve. La mayoría de estos compuestos mostraron una actividad inhibitoria significativa frente a la enzima lipoxigenasa. Se halló que la presencia de sustituyentes que aumentan la deslocalización de los electrones contribuye a mejorar la actividad inhibitoria. CONCLUSIÓN: Se concluye que es probable que el estudio conduzca al descubrimiento de agentes terapéuticamente eficientes frente a trastornos importantes tales como la inflamación y el asma.

Síndrome de deficiencia del transportador de glucosa tipo 1 (SDGLUT-1) tratado con dieta cetogénica: Caso clínico / Glucose transponer type 7 deficiency síndrome (GLUT-1 SD) treated with ketogenic diet: Report of one case

The glucose transporter type 1 deficiency syndrome (GLUT-1 SD) (OMIM 606777) is an inborn error of metabolism of brain glucose transport. The characteristic clinical manifestations are seizures, hypotonia, developmental delay, microcephaly and hypoglycorrhachia. We report a girl with normal weight and height at birth. At 6 weeks of age she started with convulsions reaching up to 20 myoclonic seizures a day. She was treated with valproate, phenobarbital and carbamazepine without response. Blood analysis including aminoacids and acylcarnitines were all normal. The brain MRI showed frontal atrophy with an increased subarachnoidal space and Electroencephalography was abnormal. Blood glucose was 84 mg/dl and spinal fluid glucose 26 mg/dl with a ratio of 0.31 (Normal Ratio >0.65+00.1). These results suggested the diagnosis of GLUT-1 SD, and was confirmed with erythrocyte glucose uptake of 44 percent (Normal range 80-100 percent). A molecular study found the mutation 969del, C971T in exon 6 of the gene Glut-1. Treatment with a ketogenic diet was started immediately and after 7 days with this diet seizures ceased. Anticonvulsants were progressively suspended. At present, the patient is 6 years old, she continues on a ketogenic diet and supplements with L-carnitine, lipoic acid, vitamins and minerals. Growth and development are normal with an intelligence quotient of 103. It is concluded that it is necessary to include GLUT-1 SD in the differential diagnosis of children with early seizures that are non responsive to pharmacological treatment.

Insecticidal activity of 2-tridecanone against the cowpea weevil Callosobruchus maculatus (Coleoptera: Bruchidae)

The effect of 2-tridecanone vapor on the cowpea weevil (Callosobruchus maculatus) development was determined. Seeds of cowpea were infested with adults and exposed to different doses of 2-tridecanone isolated from Pilocarpus microphyllus Stapf ex Holm, a plant species native from northeastern Brazil. The pure monoterpene was evaluated both undiluted as well as in the dilutions 1:10, 1:100 and 1:1,000 (v/v). The following parameters of the cowpea weevil life cycle were analyzed in response to decreasing doses of 2-tridecanone: number of eggs laid, percentage of egg hatching on seeds, percentage of adult emergence, adult weight at emergence, mean developmental time and number of adults emerged. Vapor of 2-tridecanone caused a significant (P < 0.05) reduction in the number of eggs laid, in the percentage of eggs hatched and in the number of emerged adults in infested seeds. The fumigant insecticidal effect of 2-tridecanone was mainly due to its ovicidal activity.

O efeito dos vapores da 2-tridecanona sobre o caruncho do feijão-de-corda (Callosobruchus maculatus) foi avaliado. Sementes de feijão-de-corda infestados com insetos adultos foram expostas a diferentes doses de 2-tridecanona isolada de Pilocarpus microphyllus, uma espécie nativa do Nordeste do Brasil. O monoterpeno puro foi utilizado nas diluições 1:10, 1:100 e 1:1000 (v/v). Os parâmetros da biologia do inseto foram analisados em função da resposta a doses decrescentes de 2-tridecanona: número de ovos postos por fêmea, percentagem de eclosão de ovos, percentagem de emergência de adultos, peso dos adultos recém-emergidos, tempo médio de desenvolvimento e número total de ovos emergidos. Diferenças significativas (P < 0.05) entre as doses de 2-tridecanona testadas foram observadas, para quatro dos seis parâmetros biológicos analisados. Os resultados obtidos indicaram que a 2-tridecanona é tóxica para C. maculatus, reduzindo significativamente (P < 0.05) o número de insetos emergidos após a infestação. Esse efeito foi causado principalmente pela significativa redução observada na eclosão dos ovos expostos ao vapor da substância.

Effects of L-alanyl-glutamine upon the blood and kidney biochemical parameters in the rat hind limb model of ischemia/reperfusion

OBJETIVO: Investigar alterações dos parâmetros metabólicos no sangue e rim de ratos submetidos à isquemia/reperfusão do membro pélvico. MÉTODOS: Quarenta e oito ratos machos foram distribuídos aleatoriamente em 2 grupos pré-tratados com administração intragástrica de solução salina 2,0 mL (G-1) ou L-alanil-glutamina 0,75 mgKg-1(G-2), uma vez ao dia (7:00h) durante 7 dias. Uma hora após a última gavagem todos os ratos foram anestesiados com éter dietílico, laparotomizados e submetidos ao pinçamento da artéria de ilíaca esquerda, durante 3 horas. Amostras foram coletadas ao término de isquemia e durante a reperfusão (1-3-6h) para determinação das concentrações in vivo de piruvato, lactato, glicose e corpos cetônicos (rim e sangue) e ATP (rim). RESULTADOS: Lactacemia e cetonemia aumentaram no grupo G-2 quando comparadas às aferidas em ratos não-tratados, durante a reperfusão. As concentrações de piruvato diminuíram e de lactato aumentaram significativamente no rim, durante a reperfusão (1h, 3h) em ratos do G-2 comparados aos respectivos controles. Houve um aumento significante nas concentrações renais de glicose, ATP e corpos cetônicos nos ratos tratados com L-alanil-glutamina durante a reperfusão (3h). CONCLUSÕES: A isquemia do membro pélvico em ratos pré-tratados com L-alanil-glutamina induz aumento da lactacemia e da concentração de lactato renal, indicando atividade glicolítica aumentada na medula renal. A hipercetonemia induzida pela oferta do dipeptídeo sugere cetogênese elevada, sinalizada por possível queda nas concentrações plasmáticas de insulina resultante da maior oxidação de glicose e utilização desse hormônio em tecidos periféricos.

Estudos para a síntese do petrosinol e da amamistatina B / Studies on the synthesis of petrosinol and of amamistatin B

O petrosinol é um produto natural obtido a partir de esponjas do gênero Petrosia sp. Trata-se de um poliacetileno que posui atividade anti-HIV. A síntese deste composto, ainda não descrita na literatura, mostrou-se difícil. No presente trabalho são descritas as rotas sintéticas testadas para a obtenção do petrosinol. Foram feitas abordagens, totalizando sete, que consistiram na síntese de sistemas dicarbonílicos `alfa´, ß-insaturados, os quais se mostraram pouco reativos, que não permitiram a continuidade das rotas com esta abordagem, ou tentativas de construção de álcoois propargílicos, que neste caso, os intermediários de síntese se mostraram muito instáveis. A síntese do petrosinol necessita de mais estudos visando novas tentativas para se obter o sistema diol insaturado central presente na molécula, chave para a síntese total da mesma

El segundo bienio del Programa de Evaluación Externa de Calidad en Uroanálisis (PEECU) / The second biennial of the External Quality Evaluation Program in Urinalysis (PEECU)

OBJECTIVE: To characterize the participation of clinical laboratories in the second biennial of an external quality assurance scheme for urinalysis in Mexico. METHODS: The participants received 32 control samples in 8 shipments of 4 controls each during the biennial 1999-2000. The controls were in the form of tablets to be dissolved in 12 mL of water to mimic urine. The participants performed dipstick assays of pH, specific gravity (SG) and 8 analytes (proteins, glucose, ketones, blood, bilirubin, nitrites, urobilinogen, leukocytes) in the controls. Expected control values were assigned by 10-15 replicate automated assays using dipsticks and apparatus of a single provider (Bayer). Participants' results were transformed to scores ranging from zero (perfect result) to 400 (worst possible). Score differences were analyzed using nonparametric methods (Kruskal-Wallis and Mann-Whitney). RESULTS: The best results were seen for nitrites, ketones and proteins (mean global scores = 3-5) and the worst for SG (score = 45) with intermediate scores of 10-13 for the other six. CONCLUSIONS: The scores improved for the second biennial from a grand mean of 17 in the first significantly down to 12 in the second. The number of participants has been increasing yearly and there has been a decrease of participants who do not report at least 3 out of 4 yearly shipments. We confirmed that automated readings yield better scores than visual readings.

Effects of piperitenone oxide on the intestinal smooth muscle of the guinea pig

We investigated the effects of piperitenone oxide (PO), a major constituent of the essential oil of Mentha x villosa, on the guinea pig ileum. PO (30 to 740 mug/ml) relaxed basal tonus without significantly alterating the resting membrane potential. In addition, PO relaxed preparations precontracted with either 60 mM K+ or 5 mM tetraethyl-ammonium in a concentration-dependent manner. At concentrations from 0.1 to 10 mug/ml PO potentiated acetylcholine-induced contractions, while higher concentrations (>30 mug/ml) blocked this response. These higher PO concentrations also inhibited contractions induced by 60 mM K+. PO also blocked the components of acetylcholine contraction which are not sensitive to nifedipine or to solutions with nominal zero Ca2+ and EGTA. These results show that PO is a relaxant of intestinal smooth muscle and suggest that this activity may be mediated at least in part by an intracellular effect.