Influence of Lithium Triflate Salt Concentration on Structural, Thermal, Electrochemical, and Ionic Conductivity Properties of Cassava Starch Solid Biopolymer Electrolytes.

Cassava starch solid biopolymer electrolyte (SBPE) films were prepared by a thermochemical method with different concentrations of lithium triflate (LiTFT) as a dopant salt. The process began with dispersing cassava starch in water, followed by heating to facilitate gelatinization; subsequently, plasticizers and LiTFT were added at differing concentrations. The infrared spectroscopy analysis (FTIR-ATR) showed variations in the wavenumber of some characteristic bands of starch, thus evidencing the interaction between the LiTFT salt and biopolymeric matrix. The short-range crystallinity index, determined by the ratio of COH to COC bands, exhibited the highest crystallinity in the salt-free SBPEs and the lowest in the SBPEs with a concentration ratio (Xm) of 0.17. The thermogravimetric analysis demonstrated that the salt addition increased the dehydration process temperature by 5 °C. Additionally, the thermal decomposition processes were shown at lower temperatures after the addition of the LiTFT salt into the SBPEs. The differential scanning calorimetry showed that the addition of the salt affected the endothermic process related to the degradation of the packing of the starch molecules, which occurred at 70 °C in the salt-free SBPEs and at lower temperatures (2 or 3 °C less) in the films that contained the LiTFT salt at different concentrations. The cyclic voltammetry analysis of the SBPE films identified the redox processes of the glucose units in all the samples, with observed differences in peak potentials (Ep) and peak currents (Ip) across various salt concentrations. Electrochemical impedance spectroscopy was used to establish the equivalent circuit model Rf-(Cdl/(Rct-(CPE/Rre))) and determine the electrochemical parameters, revealing a higher conduction value of 2.72 × 10-3 S cm-1 for the SBPEs with Xm = 17 and a lower conduction of 5.80 × 10-4 S cm-1 in the salt-free SBPEs. It was concluded that the concentration of LiTFT salt in the cassava starch SBPE films influences their morphology and slightly reduces their thermal stability. Furthermore, the electrochemical behavior is affected in terms of variations in the redox potentials of the glucose units of the biopolymer and in their ionic conductivity.

Enantioselective inhibition of human CYP2C19 by the chiral pesticide ethofumesate: Prediction of pesticide-drug interactions in humans.

Ethofumesate is a chiral herbicide that may display enantioselective behavior in humans. For this reason, the enantioselective potential of ethofumesate and its main metabolite ethofumesate-2-hydroxy to cause pesticide-drug interactions on cytochrome P450 forms (CYPs) has been evaluated by using human liver microsomes. Among the evaluated CYPs, CYP2C19 had its activity decreased by the ethofumesate racemic mixture (rac-ETO), (+)-ethofumesate ((+)-ETO), and (-)-ethofumesate ((-)-ETO). CYP2C19 inhibition was not time-dependent, but a strong inhibition potential was observed for rac-ETO (IC50 = 5 ± 1 µmol L-1), (+)-ETO (IC50 = 1.6 ± 0.4 µmol L-1), and (-)-ETO (IC50 = 1.8 ± 0.4 µmol L-1). The reversible inhibition mechanism was competitive, and the inhibition constant (Ki) values for rac-ETO (2.6 ± 0.4 µmol L-1), (+)-ETO (1.5 ± 0.2 µmol L-1), and (-)-ETO (0.7 ± 0.1 µmol L-1) were comparable to the Ki values of strong CYP2C19 inhibitors. Inhibition of CYP2C19 by ethofumesate was enantioselective, being almost twice higher for (-)-ETO than for (+)-ETO, which indicates that this enantiomer may be a more potent inhibitor of this CYP form. For an in vitro-in vivo correlation, the Food and Drug Administration's (FDA) guideline on the assessment of drug-drug interactions used in the early stages of drug development was used. The FDA's R1 values were estimated on the basis of the obtained ethofumesate Ki and distribution volume, metabolism, unbound plasma fraction, gastrointestinal and dermal absorption data available in the literature. The correlation revealed that ethofumesate probably inhibits CYP2C19 in vivo for both chronic (oral) and occupational (dermal) exposure scenarios.

Eugenol and tricaine methanesulfonate as anhestesics for the pearl cichlid

Anesthesia reduces the handling process duration and prevent fish injuries. The anesthetic effect and ideal concentrations of eugenol and tricaine methanesulfonate (MS-222) were tested for pearl cichlid (Geophagus brasiliensis) juveniles with an average weight of 4.4 g in water at 24ºC. The criterion for determining the optimal dose considered an induction time of one minute. Experiment 1 tested the concentrations of 25, 75, 150 and 300 mg L-1 of eugenol. The best results were obtained at doses of 150 and 300 mg L-1. Experiment 2 aimed to establish a more accurate result by testing the concentrations of 180, 210, 240 and 270 mg L-1, and led to an estimation of 217 mg L-1 of eugenol to induce anesthesia in one minute. Experiment 3 evaluated 200, 300, 400, 500 and 600 mg L-1 of tricaine, of which the concentration of 294 mg L-1 was estimated to induce anesthesia in one minute. No significant differences were observed for recovery times when using either of the anesthetics. No mortality was observed within 24 hours after the experiments for any concentration of the anesthetics. The present study recommends 217 mg L-1 of eugenol or 394 mg L-1 of tricaine for anesthesia of the pearl cichlid.

Eugenol and tricaine methanesulfonate as anhestesics for the pearl cichlid

Anesthesia reduces the handling process duration and prevent fish injuries. The anesthetic effect and ideal concentrations of eugenol and tricaine methanesulfonate (MS-222) were tested for pearl cichlid (Geophagus brasiliensis) juveniles with an average weight of 4.4 g in water at 24ºC. The criterion for determining the optimal dose considered an induction time of one minute. Experiment 1 tested the concentrations of 25, 75, 150 and 300 mg L-1 of eugenol. The best results were obtained at doses of 150 and 300 mg L-1. Experiment 2 aimed to establish a more accurate result by testing the concentrations of 180, 210, 240 and 270 mg L-1, and led to an estimation of 217 mg L-1 of eugenol to induce anesthesia in one minute. Experiment 3 evaluated 200, 300, 400, 500 and 600 mg L-1 of tricaine, of which the concentration of 294 mg L-1 was estimated to induce anesthesia in one minute. No significant differences were observed for recovery times when using either of the anesthetics. No mortality was observed within 24 hours after the experiments for any concentration of the anesthetics. The present study recommends 217 mg L-1 of eugenol or 394 mg L-1 of tricaine for anesthesia of the pearl cichlid.(AU)

Enantioselective in vitro metabolism and in vitro-in vivo correlation of the herbicide ethofumesate in a human model.

Ethofumesate (ETO) is a chiral herbicide that is marketed as a racemic mixture in the European Union and the United States. The growing consumption of pesticides in the world, along with their presence in water and food, has increased human exposure to these chemicals. Another issue concerning these compounds is that each enantiomer of a chiral pesticide may interact with biomolecules differently. For this reason, this study aimed to investigate the in vitro metabolism of ethofumesate (the racemic mixture as well as the isolated enantiomers) by human liver microsomes (HLM) and to explore the in vitro-in vivo correlation. Before the kinetics was determined, the method was fully validated by evaluating its selectivity, linearity, precision, accuracy, carryover, and stability. All the evaluated parameters agreed with the European Medicines Agency guideline. The enzyme kinetic parameters and the in vitro-in vivo correlation demonstrated that there was no enantioselective difference for the metabolism and bioavailable fraction of each enantiomer. The enzyme kinetics was biphasic; the KM1 values were 15, 5.8, and 5.6 for rac-ETO, (+)-ETO, and (-)-ETO, respectively. The total in vitro intrinsic clearance was 0.10 mg mL min-1 mg-1 for rac-ETO and its enantiomers. The enantiomer (-)-ETO was only metabolized by CYP2C19, while (+)-ETO was metabolized by both CYP2C19 and CYP3A4. CYP2C19 polymorphism and/or inhibition may represent a risk for humans exposed to this pesticide.

Mesilato de desferroxamina como candidato a adjuvante farmacêutico e cosmético / Desferroxamine mesylate as a candidate for pharmaceutical and cosmetic adjuvant

Este trabalho propôs o uso do fármaco quelante mesilato de desferroxamina (DFO) como agente adjuvante para estabilização química e microbiológica de formulações. Soluções de ácido ascórbico (AA) 5,0% (p/v) foram preparadas com sistemas antioxidantes constituídos por diferentes combinações de DFO, ácido etilenodiamino tetra-acético (EDTA) e metabissulfito de sódio, cada adjuvante na concentração máxima de 0,1% (p/v). Os sistemas foram testados previamente quanto à atividade antioxidante, mediante adição de um complexo de ferro (III) redox-ativo e ensaio baseado em fluorescência. Os sistemas também foram associados ao metilparabeno e avaliados quanto à atividade antimicrobiana pelo método turbidimétrico, utilizando-se a técnica de microdiluição em meios líquidos e cepas padrão de bactérias e fungos, incluindo S. aureus (ATCC 6538), E. coli (ATCC 8739), P. aeruginosa (ATCC 9027), C. albicans (ATCC 10231) e A. brasiliensis (ATCC 16404). As soluções de AA foram expostas a condições de teste de estabilidade acelerada e avaliadas quanto à estabilidade química, empregando-se método volumétrico validado para quantificar AA. Verificou-se que o EDTA foi o agente quelante que melhor contribuiu na estabilidade química da solução de AA, entretanto, o DFO apresentou desempenho muito superior ao EDTA para bloquear a atividade pró-oxidante do ferro. Além disso, o DFO foi fator relevante na inibição do crescimento microbiano e demonstrou sinergia com o metilparabeno. A otimização estatística dos resultados indicou que o uso do DFO nos sistemas antioxidante e conservante pode reduzir consideravelmente a concentração dos adjuvantes convencionais, EDTA, metabissulfito e metilparabeno, os quais são muitas vezes associados a reações de hipersensibilidade ou a danos ao meio ambiente

In this work it was proposed the use of the chelating drug desferroxamine mesylate (DFO) as adjuvant for chemical and microbiological stabilization of formulations. Ascorbic acid (AA) solutions 5.0% (w/v) were prepared with antioxidant systems containing different combinations of DFO, ethylenediaminetetraacetic acid (EDTA) and sodium metabisulphite, using a maximum concentration of 0.1% (w/v) for each adjuvant. Previously, the systems were spiked with a redox-active iron (III) complex and tested for antioxidant activity by fluorescence-based assay. The systems also were associated with methylparaben and evaluated for antimicrobial activity by turbidimetric method, using the microdilution technique and standard strains of bacteria and fungi, including S. aureus (ATCC 6538), E. coli (ATCC 8739), P. aeruginosa (ATCC 9027), C. albicans (ATCC 10231) and A. brasiliensis (ATCC 16404). The AA solutions were exposed to accelerated stability test conditions and evaluated for chemical stability, using a volumetric method that was validated to quantify AA. It was found that EDTA was the chelating agent that most contributed to the chemical stability of AA solution, however, DFO demonstrated a much higher performance to EDTA to block the pro-oxidant activity of iron. In addition, DFO was a relevant factor in the inhibition of microbial growth and showed synergy with methylparaben. The statistical optimization of the results indicated that the use of DFO in the antioxidant and preservative systems might considerably reduce the concentration of the conventional adjuvants, EDTA, metabisulphite and methylparaben, which are often associated with hypersensitivity reactions or environmental damage

Larvicidal and residual activity of imidazolium salts against Aedes aegypti (Diptera: Culicidae).

BACKGROUND: Aedes aegypti is an important mosquito species that can transmit several arboviruses such as dengue fever, yellow fever, chikungunya and zika. Because these mosquitoes are becoming resistant to most chemical insecticides used around the world, studies with new larvicides should be prioritized. Based on the known biological profile of imidazolium salts (IS), the objective of this study was to evaluate the potential of six IS as larvicides against Ae. aegypti, as tested against Ae. aegypti larvae. Larval mortality was measured after 24 and 48 h, and residual larvicidal activity was also evaluated. RESULTS: Promising results were obtained with aqueous solutions of two IS: 1-n-octadecyl-3-methylimidazolium chloride (C18 MImCl) and 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C16 MImMeS), showing up to 90% larval mortality after 48 h exposure. C18 MImCl was more effective than C16 mIMeS, causing mortality until day 15 after exposure. An application of C18 MImCl left to dry under ambient conditions for at least 2 months and then dissolved in water showed a more pronounced residual effect (36 days with 95% mortality and 80% mortality up to 78 days). CONCLUSION: This is the first study to show the potential of IS in the control of Ae. aegypti. Further studies are needed to understand the mode of action of these compounds in the biological development of this mosquito species. © 2017 Society of Chemical Industry.

L-tyrosine induces the production of a pyomelanin-like pigment by the parasitic yeast-form of Histoplasma capsulatum.

Melanization of Histoplasma capsulatum remains poorly described, particularly in regards to the forms of melanin produced. In the present study, 30 clinical and environmental H. capsulatum strains were grown in culture media with or without L-tyrosine under conditions that produced either mycelial or yeast forms. Mycelial cultures were not melanized under the studied conditions. However, all strains cultivated under yeast conditions produced a brownish to black soluble pigment compatible with pyomelanin when grew in presence of L-tyrosine. Sulcotrione inhibited pigment production in yeast cultures, strengthening the hyphothesis that H. capsulatum yeast forms produce pyomelanin. Since pyomelanin is produced by the fungal parasitic form, this pigment may be involved in H. capsulatum virulence.

Tumor estromal gastrointestinal de origem gástrica: relato de caso / Gastrointestinal stromal tumor of gastric origin: case report

Os tumores estromais gastrintestinais (GIST) são raros, de comportamento imprevisível, sendo a maioria assintomática ou com sintomas inespecíficos. Podem acometer qualquer local do tubo digestivo, sendo o tratamento padrão a ressecção cirúrgica completa, porém são frequentes as recidivas e metástases. O presente caso é um relato de uma paciente idosa com massa abdominal crescente e dolorosa ao exame físico, com resultado de exames complementares de imagem que sugerem tratar-se de GIST. Submetida à terapia cirúrgica para ressecção da lesão e seguimento com mesilato de imatinibe (Glivec®). (AU)

Gastrointestinal stromal tumors (GIST) are rare, with unpredictable behavior, most of them asymptomatic or nonspecific symptoms. They may arise in any place of digestive tube, and the standard treatment is the complete surgical resection, however recurrences and metastases are frequent. The following case is a report from an elderly patient with growing and painful abdominal mass on physical examination, and the result of complementary imaging tests suggests that this is GIST. Submitted to surgical therapy for resection of the lesion and follow-up with imatinib mesylate (Glivec®). (AU)

Sulfonate salts of the therapeutic agent dapsone: 4-[(4-aminophenyl)sulfonyl]anilinium benzenesulfonate monohydrate and 4-[(4-aminophenyl)sulfonyl]anilinium methanesulfonate monohydrate.

Dapsone, formerly used to treat leprosy, now has wider therapeutic applications. As is the case for many therapeutic agents, low aqueous solubility and high toxicity are the main problems associated with its use. Derivatization of its amino groups has been widely explored but shows no significant therapeutic improvements. Cocrystals have been prepared to understand not only its structural properties, but also its solubility and dissolution rate. Few salts of dapsone have been described. The title salts, C12H13N2O2S(+)·C6H5O3S(-)·H2O and C12H13N2O2S(+)·CH3SO3(-)·H2O, crystallize as hydrates and both compounds exhibit the same space group (monoclinic, P21/n). The asymmetric unit of each salt consists of a 4-[(4-aminophenyl)sulfonyl]anilinium monocation, the corresponding sulfonate anion and a water molecule. The cation, anion and water molecule form hydrogen-bonded networks through N-H...O=S, N-H...Owater and Owater-H...O=S hydrogen bonds. For both salts, the water molecules interact with one sulfonate anion and two anilinium cations. The benzenesulfonate salt forms a two-dimensional network, while the hydrogen bonding within the methanesulfonate salt results in a three-dimensional network.

1-n-Hexadecyl-3-methylimidazolium methanesulfonate and chloride salts with effective activities against Candida tropicalis biofilms.

UNLABELLED: Although the use of catheters in critically ill patients is mostly inevitable, this invasive procedure comes together with several health risks. Within this context, the contamination with Candida tropicalis is a primary concern as this highly prevalent pathogenic yeast can develop an extensive polymeric matrix that hinders the drugs' penetration and its effective treatment. This study addresses the potential for the 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C16 MImMeS) and chloride (C16 MImCl) salts for eliminating the viable cells of biofilms of Candida tropicalis, compared to the performance of chlorhexidine (CHX) and fluconazole (FLZ). The minimum concentration required of C16 MImMeS, C16 MImCl, CHX and FLZ for elimination of the biofilm's viable cells (MBEC) was evaluated through microtitre plate biofilm exposure with different concentrations of these substances. These concentrations were determined at 80% of effective activity against the biofilm's viable cells by using the MTT reduction assay. C16 MImMeS and C16 MImCl were able to eliminate the viable cells at much lower concentrations (15·6 and 0·45 µg ml(-1) respectively) than CHX (1250 µg ml(-1) ) and FLZ (resistance of the viable cells). This demonstrates the high potential of these substances for nosocomial infections control. SIGNIFICANCE AND IMPACT OF THE STUDY: The 1-n-hexadecyl-3-methylimidazolium methanesulfonate (C16 MImMeS) and chloride (C16 MImCl) salts are extremely effective in eliminating the viable cells of Candida tropicalis biofilms, which allows the use of much lower concentrations than with the antimicrobial of choice (chlorhexidine) in hospital practices. These findings indicate these imidazolium salts as high-potential candidates for asepsis of medical environments and materials, including implants.

Guarda responsável de animais de estimação na área urbana do município de Pelotas, RS, Brasil / Responsible pet animal guardianship in the urban area of the municipality of Pelotas in the state of Rio Grande do Sul, Brazil

O presente estudo teve por objetivo estimar a presença de cães e gatos em domicílios da zona urbana do município e avaliar a guarda responsável e seus fatores associados. Foi realizado um estudo transversal, de base populacional com processo de amostragem em múltiplos estágios e com os setores censitários do censo demográfico do ano de 2010, realizado pelo IBGE, utilizados como conglomerados. A unidade em estudo foi o domicílio. O desfecho foi a guarda responsável, definida por um escore que levou em consideração as seguintes variáveis: esterilização, vacinação antirrábica, consulta médica veterinária, controle de endoparasitas, acesso dos animais às áreas públicas e o recolhimento das fezes nestes locais e controle de ectoparasitas. Entre os 1.558 domicílios investigados, 58,9% possuíam animais de estimação (cão e/ou gato). O estudo revela que o escore de posse responsável aumenta com a escolaridade do chefe da família e é maior entre os moradores de apartamento. A maioria dos domicílios investigados atendeu apenas a metade dos critérios. Os resultados deste estudo apontam para a necessidade de políticas públicas que orientem a população sobre a guarda responsável e que ofertem serviços de imunizações e esterilização para os animais.

The study sought to estimate the presence of cats and dogs in households in the urban area of the city and assess responsible guardianship and associated factors. A population-based, cross-sectional study was conducted using the multi-stage sampling process and the census sectors of the demographic census of the year 2010 carried out by IBGE were used as conglomerates. The unit under study was the household. The outcome was responsible guardianship, defined by a score that took into account the following variables: sterilization, anti-rabies vaccination, veterinary medical consultation, control of endoparasites, access of animals to public areas, control of ectoparasites and the collection of feces of animals in public areas. Of the 1,558 households investigated, 58.9% had pets (cat or dog). The study reveals that the score of responsible guardianship increases with the education level of the head of the household and is highest among apartment dwellers. The majority of the households investigated met only half of the criteria. The results of this study point to the need for public policies that instruct the population on responsible guardianship, and that offer immunizations and sterilization services for animals.

Mechanistic aspects of superacid mediated condensation of polyphenols with ketones. Implications for polymer synthesis.

A detailed computational study of possible reaction paths for methanesulfonic and triflic acid mediated polyhydroxyalkylation reaction between resorcinol and trifluoracetone accompanied by cyclodehydration to give 9H-xanthene containing polymers has been carried out at M06-2X/6-311+G level of theory. A cluster solvation model was used for the calculations. The calculations revealed that the most kinetically favorable reaction path involves the cyclodehydration occurring during the polymer forming step. In this case 9H-xanthene formation is promoted by the activated phenyl ring in Wheland intermediate assisting the aromatic nucleophilic substitution of OH group which leads to the cyclization. It has been demonstrated that the inability of methanesulfonic acid to catalyze the formation of 9H-xanthene containing polymers is due to the very high barrier of the rate limiting step of the polymer forming reaction and not the cyclodehydration process.

Synthesis of pharmacologically active 1-amino-isoquinolines prepared via silver triflate-catalyzed cyclization of o-alkynylbenzaldoximes with isocyanates.

The synthesis of a series of 1-amino-isoquinolines prepared via electrophilic cyclization [3+2] cycloaddition/rearrangement reactions of o-alkynylbenzaldoxime 1 with isocyanates 2 in the presence of catalytic amount of AgOTf was demonstrated. The cyclized products were obtained in good yields under an air atmosphere. 1-Amino-isoquinoline derivatives 3a, 3b, 3j and 3t were screened in vitro for the antioxidant potential and efficacy to inhibit cerebral monoamine oxidase (MAO) activity. The antidepressant-like action of some 1-amino-isoquinolines was performed in the mouse forced swimming test (FST). The pharmacological screening of 1-amino-isoquinoline derivatives indicated that 3a, 3b, 3j and 3t were antioxidants and inhibited cerebral MAO-A and B activities at low concentrations. Although at different doses 3a, 3b, 3j and 3t were effective antidepressant-like drugs in the mouse FST. None of 1-amino-isoquinolines tested caused acute cerebral, hepatic or renal toxicity in mice.

Leucemia mieloide crónica: respuesta de los pacientes al tratamiento con imatinib en el Hospital PNP Luis N. Sáenz del 2006 al 2011 / Chronic myeloid leukemia: patient response to treatment with Imatinib in the Hospital PNP Luis N. Saenz from 2006 to 2011

Objetivos: Conocer el comportamiento de la LMC y su respuesta al tratamiento con Imatinib en pacientes tratados en el HN-PNP-LNS entre el 2006 y 2011 respectivamente. Material y métodos: Estudio de tipo retrospectivo y metodología observacional, transversal y descriptivo en 34 pacientes con LMC, siendo el instrumento principal de estudio la Ficha de Datos, previamente validada. Resultados: En el servicio de Hematología del HN-PNP-LNS entre Enero del 2006 a Diciembre del 2011, se reservaron 34 historias clínicas de pacientes con Leucemia Mieloide Crónica. La edad promedio fue de 46.4±10.3 años, observándose que igual o menos de 50 años tenían 23 pacientes (67.65 por ciento). Predominó el sexo masculino en una relación de 1.42/1. Observamos que 30 pacientes (88.25 por ciento) debutaron en fase crónica. El comportamiento hematológico promedio en sangre periférica al momento del diagnóstico (n=30), el porcentaje promedio de blastos, fue de 1.8 entre 0-5 por ciento. El porcentaje de eosinófilos fue de 2.5 entre 0.7, al diagnóstico. El porcentaje promedio de basófilos al diagnóstico fue de 8.8 entre 1-20 por ciento, presentamos la respuesta hematológica a los 06 meses de tratamiento en las diferentes fases de la enfermedad; así, en la fase crónica el 70 por ciento obtuvo una respuesta hematológica completa (RHC). Dicho de otra forma, el 100 por ciento de pacientes en fase crónica logra algún grado de respuesta hematológica, mientras que en la fase acelerada, ninguno logró respuesta hematológica completa. A los 12 meses, observamos que la mayoría de los pacientes mantiene la respuesta hematológica alcanzada a los 06 meses; esto es, el 75.85 por ciento en fase crónica mantiene su RHC y el 100 por ciento 04 casos en fase acelerada mantiene su RHP. En relación a la respuesta citogenética a los 12 meses de tratamiento con Imatinib, sólo en 3 casos (9.30 por ciento) se lograron respuesta citogenética completa (RCC); el 48.40 por ciento obtuvieron respuesta mayor...

Objectives: To determine the behavior of the LMC and its response to treatment with Imatinib in patients in the HN-PNP-LNS between 2006 and 2011, respectively. Material and methods: retrospective and observational, transversal and descriptive method in 34 patients with CML, the main survey instrument data sheet, previously validated. Results: In the Service of Hematology HN-PNP-LNS between January 2006 to December 2011, 34 case histories of patients with chronic myeloid leukemia reserved. The average age was 46.4±10.3 years, with equal or less than 50 years were 23 patients (67.65 per cent). Males predominated in a ratio of 1.42/1. We note that 30 patients (88.25 per cent) debuted in chronic phase. The average peripheral blood hematological behavior at diagnosis (n=30), the average blast percentage was 1.8 per cent 0-5. The percentage of eosinophils was 2.5 from 0.7, to diagnosis. The average percentage of basophils at diagnosis was 1-20 per cent 8.8, we present the hematologic response to the 06 months of treatment at different stages of the disease; so, in the chronic phase 70 per cent obtained a complete hematologic response (CHR). In other words, 100 per cent of patients in chronic phase achieved some degree of hematologic response, while in the accelerated phase, none achieved complete hematologic response. At 12 months, we found that most patients achieved hematologic response remains to the 06 months; that is, 75.85 per cent in chronic phase remains RHC and 100 per cent 04 cases in accelerated phase remains RHP. In relation to the cytogenetic response at 12 months of treatment with Imatinib, only in 3 cases (9.30 per cent) complete cytogenetic response (CCyR) was achieved; 48.40 per cent obtained the highest response (complete plus partial response). Conclusions: Treatment with Imatinib in the initial dose of 400 mg / day, is currently the treatment of choice for Ph+ CML in FC, cytogenetic and molecular...

Dielectric relaxation spectroscopy shows a sparingly hydrated interface and low counterion mobility in triflate micelles.

The properties of ionic micelles are affected by the nature of the counterion. Specific ion effects can be dramatic, inducing even shape and phase changes in micellar solutions, transitions apparently related to micellar hydration and counterion binding at the micellar interface. Thus, determining the hydration and dynamics of ions in micellar systems capable of undergoing such transitions is a crucial step in understanding shape and phase changes. For cationic micelles, such transitions are common with large organic anions as counterions. Interestingly, however, phase separation also occurs for dodecyltrimethylammonium triflate (DTATf) micelles in the presence of sodium triflate (NaTf). Specific ion effects for micellar solutions of dodecyltrimethylammonium chloride (DTAC), bromide (DTAB), methanesulfonate (DTAMs), and triflate (DTATf) were studied with dielectric relaxation spectroscopy (DRS), a technique capable of monitoring hydration and counterion dynamics of micellar aggregates. In comparison to DTAB, DTAC, and DTAMs, DTATf micelles were found to be considerably less hydrated and showed reduced counterion mobility at the micellar interface. The obtained DTATf and DTAMs data support the reported central role of the anion's -CF3 moiety with respect to the properties of DTATf micelles. The reduced hydration observed for DTATf micelles was rationalized in terms of the higher packing of this surfactant compared to that of other DTA-based systems. The decreased mobility of Tf(-) anions condensed at the DTATf interface strongly suggests the insertion of Tf(-) in the micellar interface, which is apparently driven by the strong hydrophobicity of -CF3.

Mebendazole mesylate monohydrate: a new route to improve the solubility of mebendazole polymorphs.

Mebendazole mesylate monohydrate, a new stable salt of mebendazole (MBZ), has been synthesized and fully characterized. It was obtained from recrystallization of MBZ forms A, B, or C in diverse solvents with the addition of methyl sulfonic acid solution. The crystal packing is first organized as a two-dimensional array consisting of rows of alternating MBZ molecules linked to columns of mesylate ions by hydrogen bonds. The three-dimensional structure is further developed by classical intermolecular interactions involving water molecules. In addition, nonclassical contacts are also found. The vibrational behavior is consistent with the crystal structure, the most important functional groups showing shifts to lower or higher frequencies in relation to the MBZ polymorphs. Thermal analysis indicates that the compound is stable up to 50°C. Decomposition occurs in five steps. Solubility studies show that the title compound presents a significant higher performance than polymorph C. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 102:3528-3538, 2013.

Effect of counterions on the shape, hydration, and degree of order at the interface of cationic micelles: the triflate case.

Specific ion effects in surfactant solutions affect the properties of micelles. Dodecyltrimethylammonium chloride (DTAC), bromide (DTAB), and methanesulfonate (DTAMs) micelles are typically spherical, but some organic anions can induce shape or phase transitions in DTA(+) micelles. Above a defined concentration, sodium triflate (NaTf) induces a phase separation in dodecyltrimethylammonium triflate (DTATf) micelles, a phenomenon rarely observed in cationic micelles. This unexpected behavior of the DTATf/NaTf system suggests that DTATf aggregates have unusual properties. The structural properties of DTATf micelles were analyzed by time-resolved fluorescence quenching, small-angle X-ray scattering, nuclear magnetic resonance, and electron paramagnetic resonance and compared with those of DTAC, DTAB, and DTAMs micelles. Compared to the other micelle types, the DTATf micelles had a higher average number of monomers per aggregate, an uncommon disk-like shape, smaller interfacial hydration, and restricted monomer chain mobility. Molecular dynamic simulations supported these observations. Even small water-soluble salts can profoundly affect micellar properties; our data demonstrate that the -CF3 group in Tf(-) was directly responsible for the observed shape changes by decreasing interfacial hydration and increasing the degree of order of the surfactant chains in the DTATf micelles.

Ocorrência de múltiplas neoplasias em paciente portador de leucemia mieloide crônica: relato de caso / Occurence of multiple neoplasms in patient with chronic myeloid leukemia: case report

Introdução: A leucemia mieloide crônica é um distúrbio mieloproliferativo clonal com uma anormalidade citogenética específica, resultante da translocação entre os cromossomos 9 e 22 com consequente produção de uma proteína com atividade tirosina quinase alterada. Tratamentos históricos com drogas como bussulfan, hidroxiureia e interferon passaram a ser pouco utilizados devido ao surgimento dos inibidores de tirosina quinase, cujo principal representante é o mesilato de imatinibe. Esse fármaco é a terapia de primeira linha, sendo bem tolerado pelos pacientes e com baixo risco de eventos adversos severos. Entretanto, com cerca de dez anos de uso, ainda há preocupação com efeitos colaterais em longo prazo, tais como o desenvolvimento de segunda neoplasia. Objetivo: Descrever a ocorrência de múltiplas neoplasias em um portador de leucemia mieloide crônica. Método: Relata-se o caso de um paciente com leucemia mieloide crônica há 13 anos, tendo utilizado hidroxiureia e interferon como terapias prévias e em uso de mesilato de imatinibe há nove anos. Resultados: Há dois anos, o paciente apresentou dois nódulos em coxa esquerda que foram totalmente ressecados. Diagnosticou-se lipossarcoma mixoide e o paciente foi submetido à radioterapia. A tomografia computadorizada do abdomên de controle aos seis meses detectou nódulo espiculado na gordura mesenquimal adjacente ao jejuno/íleo. Feita laparotomia exploradora e ressecção, o anatomopatológico demonstrou fibromatose desmoide. Conclusão: O portador de tumor maligno tem risco aumentado de desenvolver uma segunda neoplasia, que pode dessa forma ocorrer nos portadores de leucemia mieloide crônica. Essa associação pode estar relacionada aos fármacos usados no tratamento da mesma.