Soybean (Glycine max) as a versatile biocatalyst for organic synthesis

A series of aliphatic and aromatic aldehydes and ketones were reduced using plant cell preparations of Glycine max seeds (soybean). The biotransformation of five aromatic aldehydes in water, at room temperature afforded the corresponding alcohols in excellent yields varying from 89 to 100%. Two prochiral aromatic ketones yielded the alcohol in very low conversion, 1% and to 4%; however with good enantiomeric excess (ee) of 99 and 79%, respectively. Additionally, three prochiral and one cyclic aliphatic ketones produced the corresponding alcohols in moderate yields varying from 10 to 58% and ee varying from 73 to 99%. Hydrolysis of two aromatic esters yielded the expected carboxylic acids in 49 and 66%. Most of the obtained alcohols have commercial value as cosmetic fragrances. Although, the enzymes present in soybean (reductase/lipase) has not been defined, the reaction is an important route for the preparation of pure alcohols and carboxylic acid, with low cost and environmental impact.Keywords: Glycine max, biocatalysis, bioreduction, aldehydes and ketones, ester hydrolysi

Magnetic nanosystem for cancer therapy using oncocalyxone A, an antitomour secondary metabolite isolated from a Brazilian plant

none14siThis paper describes the investigation and development of a novel magnetic drug delivery nanosystem (labeled as MO-20) for cancer therapy. The drug employed was oncocalyxone A (onco A), which was isolated from Auxemma oncocalyx, an endemic Brazilian plant. It has a series of pharmacological properties: antioxidant, cytotoxic, analgesic, anti-inflammatory, antitumor and antiplatelet. Onco A was associated with magnetite nanoparticles in order to obtain magnetic properties. The components of MO-20 were characterized by XRD, FTIR, TGA, TEM and Magnetization curves. The MO-20 presented a size of about 30 nm and globular morphology. In addition, drug releasing experiments were performed, where it was observed the presence of the anomalous transport. The results found in this work showed the potential of onco A for future applications of the MO-20 as a new magnetic drug release nanosystem for cancer treatment.openBarreto, Antônio C.H.; Santiago, Vivian R.; Freire, Rafael M.; Mazzetto, Selma E.; Denardin, Juliano C.; Mele, Giuseppe; Cavalcante, Igor M.; Ribeiro, Maria E.N.P.; Ricardo, Nágila M.P.S.; Gonçalves, Tamara; Carbone, Luigi; Lemos, Telma L.G.; Pessoa, Otília D.L.; Fechine, Pierre B.A.*Barreto, Antônio C. H.; Santiago, Vivian R.; Freire, Rafael M.; Mazzetto, Selma E.; Denardin, Juliano C.; Mele, Giuseppe; Cavalcante, Igor M.; Ribeiro, Maria E. N. P.; Ricardo, Nágila M. P. S.; Gonçalves, Tamara; Carbone, Luigi; Lemos, Telma L. G.; Pessoa, Otília D. L.; Fechine, Pierre B. A

Predicting progression of mild cognitive impairment to dementia using neuropsychological data: a supervised learning approach using time windows

Background: Predicting progression from a stage of Mild Cognitive Impairment to dementia is a major pursuit in current research. It is broadly accepted that cognition declines with a continuum between MCI and dementia. As such, cohorts of MCI patients are usually heterogeneous, containing patients at different stages of the neurodegenerative process. This hampers the prognostic task. Nevertheless, when learning prognostic models, most studies use the entire cohort of MCI patients regardless of their disease stages. In this paper, we propose a Time Windows approach to predict conversion to dementia, learning with patients stratified using time windows, thus fine-tuning the prognosis regarding the time to conversion. Methods: In the proposed Time Windows approach, we grouped patients based on the clinical information of whether they converted (converter MCI) or remained MCI (stable MCI) within a specific time window. We tested time windows of 2, 3, 4 and 5 years. We developed a prognostic model for each time window using clinical and neuropsychological data and compared this approach with the commonly used in the literature, where all patients are used to learn the models, named as First Last approach. This enables to move from the traditional question "Will a MCI patient convert to dementia somewhere in the future" to the question "Will a MCI patient convert to dementia in a specific time window". Results: The proposed Time Windows approach outperformed the First Last approach. The results showed that we can predict conversion to dementia as early as 5 years before the event with an AUC of 0.88 in the cross-validation set and 0.76 in an independent validation set. Conclusions: Prognostic models using time windows have higher performance when predicting progression from MCI to dementia, when compared to the prognostic approach commonly used in the literature. Furthermore, the proposed Time Windows approach is more relevant from a clinical point of view, predicting conversion within a temporal interval rather than sometime in the future and allowing clinicians to timely adjust treatments and clinical appointments.FCT under the Neuroclinomics2 project [PTDC/EEI-SII/1937/2014, SFRH/BD/95846/2013]; INESC-ID plurianual [UID/CEC/50021/2013]; LASIGE Research Unit [UID/CEC/00408/2013

Ornato e despojamento no mundo fabril

O artigo investiga algumas das tendências da arquitetura gerada por fábricas - galpões industriais, moradias, igrejas, escolas, clubes etc. -, erguida no Brasil entre as duas últimas décadas do século XIX e as primeiras do XX. Apoia-se em amplo inventário, como base para um esforço de análise que se propõe a identificar os temas e usos predominantes dos ornatos aplicados a construções geradas por fábricas, as referências historicistas mobilizadas e eventuais rupturas de signos arquitetônicos tipológicos, e, no limite, a abolição de ornatos e dos referidos signos. Assim, de um lado, trata da penetração da linguagem eclética nessas construções, investigando o repertório formal utilizado em diferentes tipologias. De outro, trata da simultânea difusão de uma estética tipicamente fabril, fundamentada em noções de economia, eficiência, utilidade e funcionalidade. Mostra como tais noções se expressam ora em uma simplificação ou ausência de ornatos, ora no uso de ornatos cujos temas remetem ao mundo das máquinas; às vezes, no distanciamento ou abandono de signos arquitetônicos tipológicos consagrados; ou, ainda, no emprego de materiais produzidos industrialmente e que se difundiram a partir, sobretudo, da arquitetura de fábricas.The article examines some aspects of the architecture created for factories - warehouses, houses, churches, schools, clubs etc. -, built in Brazil between the two last decades of the nineteenth century and early of the twentieth century. The research relies on extensive inventory, the basis on which an analysis effort is realized that aims to identify the themes and predominant use of ornament applied to constructions produced by factories, the historicist references mobilized and eventual disruption of typological architectural signs, and, ultimately, the elimination of ornament and of those signs. Therefore, on one side, it deals with the penetration of the eclectic language in these buildings, by examining the formal repertoire used in different typologies. On the other side, it deals with simultaneous diffusion of a typical manufacturing aesthetic, based on notions of economy, efficiency, utility and functionality. It shows how such notions are expressed in either a simplification or the lack of ornament, sometimes in the use of ornament whose themes relate to the world of machines, sometimes in the detachment or abandonment of embodied architectural typological signs, or even the use of industrially produced materials that have spread from mainly the architecture of factories

ytotoxicity of dehydrocrotonin (a nor-clerodane from Croton cajucara) on human lymphocytes

Trans-Dehydrocrotonin, a 19-nor-clerodane, is the major norditerpene obtained from Croton cajucara, a Brazilian medicinal plant which presents important biological effects, such as antineoplastic and antiulcerogenic activities. In this work, we analyzed the effect of this sesquiterpene lactone on normal human lymphocytes. The cell viability was verified after treatment for 24 and 72 h with trans-dehydrocrotonin, in the presence and absence of phytohemagglutin (specific mitogen for this cell), through three endpoints to assess cytotoxicity in vitro: MTT reduction (mitochondrial function), protein quantification (cell number) and phosphatase activity (cell metabolism). When the cells were treated with dehydrocrotonin in the presence of mitogen, no toxic effect was observed. Nevertheless, in the absence of mitogen, the IC50 was 450 μM for MTT reduction and phosphatase activity. Moreover, in this condition, trans-dehydrocrotonin caused stimulation of protein content from 100 μM. Our results suggest that phytohemagglutin protects human lymphocytes against the trans-dehydrocrotonin toxic effect.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Kinetic characterization and flavonoid effect on human lymphocyte protein tyrosine phosphatase

El objetivo del trabajo fue determinar las propiedades cinéticas y evaluar el efecto de algunos bioflavonoides sobre la proteína humana linfocitaria tirosina fosfatasa. Tirosina-, serina- y treonina-fosfato fueron hidrolizadas por esta fosfatasa en un 60%, 20% y 10%, respectivamente. En los estudios cinéticos la actividad enzimática fue determinada usando p-nitrofenilfosfato (pNPP) como sustrato. La enzima presentó un pH optimo cercano a 5.0 y fue inhibida por p-cloromercuribenzoato (pCMB) 100 (M (80%), fluoruro 10 mM (35%), vanadato 10 mM (100%), y Cu+2 5 mM (85%). La enzima fue también fuertemente inhibida por un cóctel de inhibidores de tirosina fosfatasa, pero fue insensible al ácido okadaico. Estos resultados confirman que la mayor actividad fosfatasa en los linfocitos humanos es una proteína tirosina fosfatasa. Entre los bioflavonoides ensayados solamente la fisetina presentó un efecto inhibitorio en el orden del 80% sobre la actividad enzimática.The aim of this work was to determine the kinetic properties and evaluate the effect of some flavonoids on human lymphocyte protein tyrosine phosphatase. Tyrosine-, serine- and threonine-phosphate were hydrolyzed by this phosphatase 60%, 20% and 10%, respectively. In the kinetic studies the enzymatic activity was determined by using p-nitrophenylphosphate (pNPP) as substrate. The enzyme presented optimum pH around 5.0 and was inhibited by 100 μM p-chloromercuribenzoate (pCMB) (80%), 10 mM fluoride (35%), 10 mM vanadate (100%), and 5mM Cu+2 (85%). The enzyme was also strongly inhibited by a tyrosine phosphatase inhibitor cocktail, but was unaffected by okadaic acid. These results confirm that the major phosphatase activity in human lymphocytes is a protein tyrosine phosphatase. Among the bioflavonoids tested only fisetin showed an inhibitory effect in order of 80% on the enzymatic activity.Colegio de Farmacéuticos de la Provincia de Buenos Aire

The effect of carbohydrate mouth rinse on performance, biochemical and psychophysiological variables during a cycling time trial: a crossover randomized trial

Abstract Background The hypothesis of the central effect of carbohydrate mouth rinse (CMR) on performance improvement in a fed state has not been established, and its psychophysiological responses have not yet been described. The aim of this study was to evaluate the effect of CMR in athletes fed state on performance, biochemical and psychophysiological responses compared to ad libitum water intake. Methods Eleven trained male cyclists completed a randomized, crossover trial, which consisted of a 30 km cycle ergometer at self-selected intensity and in a fed state. Subjects were under random influence of the following interventions: CMR with a 6% unflavored maltodextrin solution; mouth rinsing with a placebo solution (PMR); drinking “ad libitum” (DAL). The time for completion of the test (min), heart rate (bpm) and power (watts), rating of perceived exertion (RPE), affective response, blood glucose (mg/dL) and lactate (mmol/DL), were evaluated before, during and immediately after the test, while insulin (uIL/mL), cortisol (μg/dL) and creatine kinase (U/L) levels were measured before, immediately after the test and 30 min after the test. Results Time for completion of the 30 km trial did not differ significantly among CMR, PMR and DAL interventions (means = 54.5 ± 2.9, 54.7 ± 2.9 and 54.5 ± 2.5 min, respectively; p = 0.82). RPE and affective response were higher in DAL intervention (p < 0.01). Glucose, insulin, cortisol and creatine kinase responses showed no significant difference among interventions. Conclusions In a fed state, CMR has not caused metabolic changes, and it has not improved physical performance compared to ad libitum water intake, but demonstrated a possible central effect. ReBec registration number: RBR-4vpwkg. Available in http://www.ensaiosclinicos.gov.br/rg/?q=RBR-4vpwkg