Dillapiole as Antileishmanial Agent: Discovery, Cytotoxic Activity and Preliminary SAR Studies of Dillapiole Analogues

In this paper, the isolation of dillapiole (1) from Piper aduncum was reported as well as the semi-synthesis of two phenylpropanoid derivatives [di-hydrodillapiole (2), isodillapiole (3)], via reduction and isomerization reactions. Also, the compounds' molecular properties (structural, electronic, hydrophobic, and steric) were calculated and investigated to establish some preliminary structureactivity relationships (SAR). Compounds were evaluated for in vitro antileishmanial activity and cytotoxic effects on fibroblast cells. Compound 1 presented inhibitory activity against Leishmania amazonensis (IC50?=?69.3 mu M) and Leishmania brasiliensis (IC50?=?59.4 mu M) and induced cytotoxic effects on fibroblast cells mainly in high concentrations. Compounds 2 (IC50?=?99.9 mu M for L. amazonensis and IC50?=?90.5 mu M for L. braziliensis) and 3 (IC50?=?122.9 mu M for L. amazonensis and IC50?=?109.8 mu M for L. brasiliensis) were less active than dillapiole (1). Regarding the molecular properties, the conformational arrangement of the side chain, electronic features, and the hydrophilic/hydrophobic balance seem to be relevant for explaining the antileishmanial activity of dillapiole and its analogues.

Use of ground-penetrating radar to map subsurface features at the Lapa do Santo archaeological site (Brazil)

In this article we present some results of ground-penetrating radar (GPR) studies carried out at the Lapa do Santo archaeological site. This cave is within the Lagoa Santa karstic region, Minas Gerais State, Brazil. Results from 44 GPR profiles obtained with 400 MHz shielded antennas indicated anomalous hyperbolic reflections and areas with high sub-horizontal reflection amplitude suggesting archaeological and geological potential targets, respectively. These results were encouraging and were used to guide excavations at this site. Excavation of test units (metre by metre) allowed identifying an anthropogenic feature, e.g., a fire hearth structure and natural features, such as a stalagmite and top of bedrock. Results also indicated the importance of the GPR survey as a tool for orienting archaeological researches, increasing the probability of finding archaeological interest targets in an excavation program in an area of environmental protection.

Experiments on through-wall imaging using ultra wideband radar

Through-wall imaging (TWI) may provide vital information on interior environment in cases when physically entering such environment would pose danger to the person involved. The concept of ultra wideband radar (UWB radar) is an emerging technology, which offers high spatial resolution, as opposed to narrow band radars. Thus, TWI applications using UWB radar have become a growing field of research with several applications in the civil and defense areas such as rescue and surveillance. For this study, a prototype system of UWB radar to TWI has been built. Analyses and result to several kinds of experiments have been presented, that is, detection and visualization of metallic targets behind wooden board wall and concrete blocks wall. The results are encouraging and show the advantages of using UWB radar for TWI. (C) 2011 Wiley Periodicals, Inc. Microwave Opt Technol Lett, 54:339-344, 2012; View this article online at wileyonlinelibrary.com. DOI 10.1002/mop.26543

Upper Pleistocene to Holocene peatland evolution in Southern Brazilian highlands as depicted by radar stratigraphy, sedimentology and palynology

Paleoenvironmental interpretation of proxy data derived from peatlands is largely based upon an evolutionary model for ombrotrophic bogs, in which peat accumulates in still environments. Reports on proxies obtained from minerotrophic fens, where hydrologic inputs are variable, are less common. In this study, a highland peatland in southern Brazil is presented through ground penetrating radar (GPR) and sedimentological, palynological and geochronologic data. The radar stratigraphic interpretation suggests a relatively complex history of erosion and deposition at the site since the beginning of Marine Isotope Stage 3 (MIS 3) interstadial period. In spite of this, radar stratigraphic and palynologic interpretations converge. Electromagnetic reflections tend to group in clusters that show lateral coherence and correlate with different sediment types, while pollen grains abound and are well preserved. As a result, the study of minerotrophic fens provides a source of proxies. suggesting that ombrotrophic bogs are not the only reliable source of data in wetlands for palynological analysis. (C) 2012 University of Washington. Published by Elsevier Inc. All rights reserved.

Polarimetric X-band weather radar measurements in the tropics: radome and rain attenuation correction

A polarimetric X-band radar has been deployed during one month (April 2011) for a field campaign in Fortaleza, Brazil, together with three additional laser disdrometers. The disdrometers are capable of measuring the raindrop size distributions (DSDs), hence making it possible to forward-model theoretical polarimetric X-band radar observables at the point where the instruments are located. This setup allows to thoroughly test the accuracy of the X-band radar measurements as well as the algorithms that are used to correct the radar data for radome and rain attenuation. For the campaign in Fortaleza it was found that radome attenuation dominantly affects the measurements. With an algorithm that is based on the self-consistency of the polarimetric observables, the radome induced reflectivity offset was estimated. Offset corrected measurements were then further corrected for rain attenuation with two different schemes. The performance of the post-processing steps was analyzed by comparing the data with disdrometer-inferred polarimetric variables that were measured at a distance of 20 km from the radar. Radome attenuation reached values up to 14 dB which was found to be consistent with an empirical radome attenuation vs. rain intensity relation that was previously developed for the same radar type. In contrast to previous work, our results suggest that radome attenuation should be estimated individually for every view direction of the radar in order to obtain homogenous reflectivity fields.

Enhancement of blood-tumor barrier permeability by Sar-[D-Phe8]des-Arg9BK, a metabolically resistant bradykinin B1 agonist, in a rat C6 glioma model

Abstract Background While it is well known that bradykinin B2 agonists increase plasma protein extravasation (PPE) in brain tumors, the bradykinin B1 agonists tested thus far are unable to produce this effect. Here we examine the effect of the selective B1 agonist bradykinin (BK) Sar-[D-Phe8]des-Arg9BK (SAR), a compound resistant to enzymatic degradation with prolonged activity on PPE in the blood circulation in the C6 rat glioma model. Results SAR administration significantly enhanced PPE in C6 rat brain glioma compared to saline or BK (p < 0.01). Pre-administration of the bradykinin B1 antagonist [Leu8]-des-Arg (100 nmol/Kg) blocked the SAR-induced PPE in the tumor area. Conclusions Our data suggest that the B1 receptor modulates PPE in the blood tumor barrier of C6 glioma. A possible role for the use of SAR in the chemotherapy of gliomas deserves further study.

O efeito da abertura do valo grande na sedimentação do sistema estuarino-lagunar de Cananéia-Iguape (SE Brasil)

Devido às suas propriedades geomorfológicas e físico‐químicas, estuários e as lagunas estão entre os ambientes mais sensíveis à ação humana, e o número de trabalhos que trata deste tema tem aumentado rapidamente. O sistema Cananéia‐Iguape (SE Brasil) consiste em um complexo de canais estuarinos e lagunares, localizados no chamado Lagamar, uma Reserva da Biosfera da UNESCO. Esses canais são bordejados por uma vegetação de mangue exuberante, na qual desenvolvem‐se extensos bancos de ostras e mexilhões e que constitui um criadouro natural para espécies de importância econômica, tais como camarões, manjubas, robalos, pescadas, entre outros. Não obstanbte, sua importância ambiental, o sistema vem sofrendo modificações dramáticas nos últimos 150 anos, em função da abertura, em 1852, de um canal artificial, o Valo Grande, conectando o Rio Ribeira de Iguape ao sistema estuarino‐lagunar, afetando as características físico‐químicas e o processo deposicional. Um fator agravante diz respeito ao fato de que atividades de mineração realizadas pela Plumbum S/A entre 1945 e 1995 no Vale do Ribeira.