Diazoles y triazoles derivados del extracto de aceite de ricino: síntesis, efecto hipoglucémico, potencial antioxidante y actividad antimicrobiana

The ricinoleate triglyceride was extracted from castor-oil seeds grown in Algeria and isolated by catalytically methanolyse to methyl ricinoleate. Six diazole and triazole derivatives of ricinoleic acid were synthesized and characterized: 1,3,4-oxadiazole-5-thione (4); 1,3,4-thiadiazole-5-thione (5); 4-N-amino-1,2,4-triazole-5-thiol (7); 1,2,4-triazole-5-thione (9); 5-amino-1,3,4-oxadiazole (10) and 5-amino-1,3,4-thiadiazole (11). The antibacterial and antifungal screening data of synthesized compounds showed appreciable inhibition and among them, 5, 7 and 8 showed more inhibition on Gram positive Enterococcus faecalis than reference ampiciline; while compounds 1, 7, 8, 10 and 11 showed competitive antifungal effects compared to reference amphotericin B. In addition, all synthesized compounds (1-11) showed competitive antioxidant properties, particularly compounds 7 at 125, 250, 500 and 1000 μg/mL and compounds 4, 5 and 9 at a concentration of 1000 μg/mL. The intermediate compounds 1, 2 and 8 showed anti-α-amylase activity at various concentrations in the range of IC50 = (120.25 ± 1.17 - 130.42 ± 2.48). Oxadiazole 4 showed the best α-amylase inhibition by 78.5% at a concentration of 1000 μg/mL.Los triglicéridos de ricinoleico se extrajeron de semillas de aceite de ricino cultivadas en Argelia y se sintetizó catalíticamente con metanolisis el ricinoleato de metilo. Seis derivados de diazoles y triazoles de ácido ricinoleico se han sintetizado y caracterizado: 1,3,4-oxadiazol-5-tiona (4), 1,3,4-tiadiazol-5-tiona (5), 4-N-amino-1,2,4-triazol-5-tiol (7), 1,2,4-triazol-5-tiona (9), 5-amino-1,3,4-oxadiazol (10) y 5-amino-1,3,4-tiadiazol (11). Los datos de detección antibacteriana y antifúngica de los compuestos sintetizados mostraron una inhibición apreciable, entre ellos, los compuestos 5, 7 y 8 mostraron más inhibición en Enterococcus faecalis Gram positivo que la ampicilina de referencia. Mientras que los compuestos 1, 7, 8, 10 y 11 mostraron una influencia antifúngica competitiva en comparación con la anfotericina de referencia B. Como todos los compuestos sintetizados (1-11) mostraron propiedades antioxidantes competitivas, particularmente los compuestos 7, a 125, 250, 500 y 1000 μg/mL también compuestos 4, 5 y 9 a una concentración de 1000 μg/mL. Los compuestos intermedios 1, 2 y 8 mostraron actividad anti-α-amilasa a diversas concentraciones en el rango de IC50 = (120.25 ± 1.17 - 130.42 ± 2.48). El oxadiazol 4 mostró la mejor inhibición de la α-amilasa en un 78.5% a una concentración de 1000 μg/mL

The Epistemology of Intentionality: Notional Constituents vs. Direct Grasp

Franz Brentano is well known for highlighting the importance of intentionality, but he said curiously little about the nature of intentionality. According to Mark Textor, there is a deep reason for this: Brentano took intentionality to be a conceptual primitive the nature of which is revealed only in direct grasp. Although there is certainly textual support for this interpretation, it appears in tension with Brentano’s repeated attempts to analyze intentionality in terms of ‘notional constituents’ – aspects of intentionality which cannot come apart in reality but which can be conceptually distinguished. After bringing out this tension, I explore some options for resolving it, ultimately offering my own favored interpretation

Isotopic and velocity distributions of Bi produced in charge-pickup reactions of 208Pb at 1 A GeV

Isotopically resolved cross sections and velocity distributions have been measured in charge-pickup reactions of 1 A GeV 208Pb with proton, deuterium and titanium target. The total and partial charge-pickup cross sections in the reactions 208Pb + 1H and 208Pb + 2H are measured to be the same in the limits of the error bars. A weak increase in the total charge-pickup cross section is seen in the reaction of 208Pb with the titanium target. The measured velocity distributions show different contributions - quasi-elastic scattering and Delta-resonance excitation - to the charge-pickup production. Data on total and partial charge-pickup cross sections from these three reactions are compared with other existing data and also with model calculations based on the coupling of different intra-nuclear cascade codes and an evaporation code.Comment: 20 pages, 12 figures, background information on http://www-w2k.gsi.de/kschmidt

Duration of adjuvant chemotherapy for stage III colon cancer

BACKGROUND Since 2004, a regimen of 6 months of treatment with oxaliplatin plus a fluoropyrimidine has been standard adjuvant therapy in patients with stage III colon cancer. However, since oxaliplatin is associated with cumulative neurotoxicity, a shorter duration of therapy could spare toxic effects and health expenditures. METHODS We performed a prospective, preplanned, pooled analysis of six randomized, phase 3 trials that were conducted concurrently to evaluate the noninferiority of adjuvant therapy with either FOLFOX (fluorouracil, leucovorin, and oxaliplatin) or CAPOX (capecitabine and oxaliplatin) administered for 3 months, as compared with 6 months. The primary end point was the rate of disease-free survival at 3 years. Noninferiority of 3 months versus 6 months of therapy could be claimed if the upper limit of the two-sided 95% confidence interval of the hazard ratio did not exceed 1.12. RESULTS After 3263 events of disease recurrence or death had been reported in 12,834 patients, the noninferiority of 3 months of treatment versus 6 months was not confirmed in the overall study population (hazard ratio, 1.07; 95% confidence interval [CI], 1.00 to 1.15). Noninferiority of the shorter regimen was seen for CAPOX (hazard ratio, 0.95; 95% CI, 0.85 to 1.06) but not for FOLFOX (hazard ratio, 1.16; 95% CI, 1.06 to 1.26). In an exploratory analysis of the combined regimens, among the patients with T1, T2, or T3 and N1 cancers, 3 months of therapy was noninferior to 6 months, with a 3-year rate of disease-free survival of 83.1% and 83.3%, respectively (hazard ratio, 1.01; 95% CI, 0.90 to 1.12). Among patients with cancers that were classified as T4, N2, or both, the disease-free survival rate for a 6-month duration of therapy was superior to that for a 3-month duration (64.4% vs. 62.7%) for the combined treatments (hazard ratio, 1.12; 95% CI, 1.03 to 1.23; P=0.01 for superiority). CONCLUSIONS Among patients with stage III colon cancer receiving adjuvant therapy with FOLFOX or CAPOX, noninferiority of 3 months of therapy, as compared with 6 months, was not confirmed in the overall population. However, in patients treated with CAPOX, 3 months of therapy was as effective as 6 months, particularly in the lower-risk subgroup. (Funded by the National Cancer Institute and others.

Evaporation residues produced in spallation of 208Pb by protons at 500A MeV

The production cross sections of fragmentation-evaporation residues in the reaction Pb+p at 500A MeV have been measured using the inverse-kinematics method and the FRS spectrometer (GSI). Fragments were identified in nuclear charge using ionisation chambers. The mass identification was performed event-by-event using the B-rho - TOF - Delta-E technique. Although partially-unresolved ionic charge states induced an ambiguity on the mass of some heavy fragments, production rates could be obtained with a high accuracy by systematically accounting for the polluting ionic charge states. The contribution of multiple reactions in the target was subtracted using a new, partly self-consistent code. The isobaric distributions are found to have a shape very close to the one observed in experiments at higher energy. Kinematic properties of the fragments were also measured. The total and the isotopic cross sections, including charge-pickup cross sections, are in good agreement with previous measurements. The data are discussed in the light of previous spallation measurements, especially on lead at 1 GeV