Advances in drug design based on the amino acid approach: Taurine analogues for the treatment of CNS diseases

Amino acids are well known to be an important class of compounds for the maintenance of body homeostasis and their deficit, even for the polar neuroactive aminoacids, can be controlled by supplementation. However, for the amino acid taurine (2-aminoethanesulfonic acid) this is not true. Due its special physicochemical properties, taurine is unable to cross the blood-brain barrier. In addition of injured taurine transport systems under pathological conditions, CNS supplementation of taurine is almost null. Taurine is a potent antioxidant and anti-inflammatory semi-essential amino acid extensively involved in neurological activities, acting as neurotrophic factor, binding to GABA A/glycine receptors and blocking the excitotoxicity glutamate-induced pathway leading to be a neuroprotective effect and neuromodulation. Taurine deficits have been implicated in several CNS diseases, such as Alzheimer's, Parkinson's, epilepsy and in the damage of retinal neurons. This review describes the CNS physiological functions of taurine and the development of new derivatives based on its structure useful in CNS disease treatment.&; 2012 by the authors; licensee MDPI, Basel, Switzerland.

Biosolid soil application: Toxicity tests under laboratory conditions

A large volume of generated sewage sludge makes its disposal a problem. The usage of sludge in agriculture is highlighted by a number of advantages. However, heavy metals and other toxic compounds may exercise harmful effects to soil organisms. This study evaluated the possible toxic effects of a biosolid sample, under laboratory conditions, for 30 days, using diplopods Rhinocricus padbergi and plants Allium cepa (onion) as test organisms. The data obtained demonstrated that the biosolid raw sample had genotoxic potential for Allium cepa root tip cells. In the diplopods exposed to biosolid sample, epithelium disorganization in the midgut and a reduction of the volume of the hepatic cells were observed after 7 days of exposure. After 30 days, the animals still showed a reduction of the volume of the hepatic cells, but in minor intensity. Allium cepa analysis showed genotoxicity, but this effect was reduced after 30 days of bioprocessing by diplopods. This study was important to know the effects as well as to determine how this waste could be applied concerning the soil living organisms and plants. © 2012 Cintya Ap. Christofoletti et al.

Pre-harvest sugarcane burning: Determination of emission factors through laboratory measurements

Sugarcane is an important crop for the Brazilian economy and roughly 50% of its production is used to produce ethanol. However, the common practice of pre-harvest burning of sugarcane straw emits particulate material, greenhouse gases, and tropospheric ozone precursors to the atmosphere. Even with policies to eliminate the practice of pre-harvest sugarcane burning in the near future, there is still significant environmental damage. Thus, the generation of reliable inventories of emissions due to this activity is crucial in order to assess their environmental impact. Nevertheless, the official Brazilian emissions inventory does not presently include the contribution from pre-harvest sugarcane burning. In this context, this work aims to determine sugarcane straw burning emission factors for some trace gases and particulate material smaller than 2.5μm in the laboratory. Excess mixing ratios for CO2, CO, NOX, UHC (unburned hydrocarbons), and PM2.5 were measured, allowing the estimation of their respective emission factors. Average estimated values for emission factors (g kg-1 of burned dry biomass) were 1,303 ± 218 for CO2, 65 ± 14 for CO, 1.5 ± 0.4 for NOX, 16 ± 6 for UHC, and 2.6 ± 1.6 for PM2.5. These emission factors can be used to generate more realistic emission inventories and therefore improve the results of air quality models. © 2012 by the authors; licensee MDPI, Basel, Switzerland.

In vitro evaluation of the safety profile of cosmeceuticals containing growth factors and their analogues

Introduction: Aging skin is a condition that affects (or will affect) all people, and its treatment is considered a clinical challenge. Growth factors and their analogues are emerging as a promising therapeutic option. Objectives: To evaluate the safety profile of some dermocosmetic products with formulations based on growth factors - or their analogs intended for that purpose - using in vitro human skin cell culture models. Methods: Two types of cell cultures were studied, and the effects of the study products on the proliferation of melanoma cells and normal human fibroblasts were evaluated. Results: No significant morphological alterations were found in the cultured human melanoma, and no significant decrease in the number of healthy cells was verified in the normal fibroblasts culture. In some cases there was even a proliferation of those cells. Conclusions: These preliminary data demonstrate that cosmeceutical products containing growth factors as an active principle can be considered safe for topical application.

Dynamics and Conformational Studies of TOAC Spin Labeled Analogues of Ctx(Ile21)-Ha Peptide from Hypsiboas albopunctatus

Antimicrobial peptides (AMPs) isolated from several organisms have been receiving much attention due to some specific features that allow them to interact with, bind to, and disrupt cell membranes. The aim of this paper was to study the interactions between a membrane mimetic and the cationic AMP Ctx(Ile21)-Ha as well as analogues containing the paramagnetic amino acid 2,2,6,6-tetramethylpiperidine-1-oxyl-4-amino-4-carboxylic acid (TOAC) incorporated at residue positions n = 0, 2, and 13. Circular dichroism studies showed that the peptides, except for [TOAC13]Ctx(Ile21)-Ha, are unstructured in aqueous solution but acquire different amounts of α-helical secondary structure in the presence of trifluorethanol and lysophosphocholine micelles. Fluorescence experiments indicated that all peptides were able to interact with LPC micelles. In addition, Ctx(Ile21)-Ha and [TOAC13]Ctx(Ile21)-Ha peptides presented similar water accessibility for the Trp residue located near the N-terminal sequence. Electron spin resonance experiments showed two spectral components for [TOAC0]Ctx(Ile21)-Ha, which are most likely due to two membrane-bound peptide conformations. In contrast, TOAC2 and TOAC13 derivatives presented a single spectral component corresponding to a strong immobilization of the probe. Thus, our findings allowed the description of the peptide topology in the membrane mimetic, where the N-terminal region is in dynamic equilibrium between an ordered, membrane-bound conformation and a disordered, mobile conformation; position 2 is most likely situated in the lipid polar head group region, and residue 13 is fully inserted into the hydrophobic core of the membrane. © 2013 Vicente et al.

One-nucleon-induced nonmesonic hypernuclear decay in laboratory coordinates

We present a formalism for the computation of one-nucleon-induced nonmesonic weak hypernuclear decay rates in laboratory coordinates, within an independent-particle shell model framework, with a view to its generalization to the case of two-nucleon-induced transitions. © 2013 AIP Publishing LLC.

Identification of Candida species in the clinical laboratory: A review of conventional, commercial, and molecular techniques

In healthy individuals, Candida species are considered commensal yeasts of the oral cavity. However, these microorganisms can also act as opportunist pathogens, particularly the so-called non-albicans Candida species that are increasingly recognized as important agents of human infection. Several surveys have documented increased rates of C. glabrata, C. tropicalis, C. guilliermondii, C. dubliniensis, C. parapsilosis, and C. krusei in local and systemic fungal infections. Some of these species are resistant to antifungal agents. Consequently, rapid and correct identification of species can play an important role in the management of candidiasis. Conventional methods for identification of Candida species are based on morphological and physiological attributes. However, accurate identification of all isolates from clinical samples is often complex and time-consuming. Hence, several manual and automated rapid commercial systems for identifying these organisms have been developed, some of which may have significant sensitivity issues. To overcome these limitations, newer molecular typing techniques have been developed that allow accurate and rapid identification of Candida species. This study reviewed the current state of identification methods for yeasts, particularly Candida species. © 2013 John Wiley & Sons A/S.

The licensing of a laboratory for manipulating radionuclides in Brazil

Radionuclides take a major role in guidelines of environmental agencies/national organizations of countries worldwide. In Brazil, CNEN-Comissão Nacional de Energia Nuclear is responsible for managing all subjects related to nuclear energy in the country. Thus, laboratories employing radionuclides for the development of their activities must submit a Radioprotection Plan to CNEN in order to get an operation license. Such plan must indicate that the laboratory is exempt of risks to the people involved and designed to fit all related environmental aspects. This was the case of LABIDRO-Hydrochemical and Isotopes Laboratory that belongs to IGCE-Geosciences and Exact Sciences Institute from UNESP - the University of the State of São Paulo Júlio de Mesquita Filho, located at Rio Claro city, São Paulo State, Brazil. The total monthly activity of the radionuclides utilized during the laboratorial activities held at LABIDRO corresponds to 0.01 μCi. This paper describes all information provided by LABIDRO in order to get the CNEN license. The LABIDRO plan also showed the expected radioactive waste released when the experiments take place and CNEN decided that it fits the guidelines established by Brazilian legislation. Therefore, LABIDRO received its license for utilizing radionuclides, which is valid until September 2016. © 2013 WIT Press.

Synthesis, X-ray crystal structure and theoretical calculations of antileishmanial neolignan analogues

A síntese e a estrutura cristalina por difração de raios-X de dois análogos de neolignanas, 2-(4-clorofenil)-1-feniletanona (20) e 2-[tio(4-clorofenil)]-1-(3,4-dimetoxifenil)propan-1-ona (12) são descritas. O composto 12 apresenta atividade intracelular contra Leishmania donovani e Leishmania amazonensis de amastigotas que causam a leishmaniose tegumentar e visceral. Além disso, a teoria do funcional de densidade (DFT) com o funcional híbrido B3LYP foi empregado para calcular um conjunto de descritores moleculares para dezenove análogos sintéticos de neolignanas com atividades antileishmaniose. Posteriormente, a análise discriminante stepwise foi realizada para investigar possíveis relações entre a estrutura molecular e atividades biológicas. Por meio dessa análise os compostos foram classificados em dois grupos ativos e inativos de acordo com seu grau de atividade biológica, e as propriedades mais importantes foram as cargas de alguns átomos, a afinidade eletrônica e o ClogP.

Early larval development in the laboratory of Alpheus estuariensis (Crustacea: Caridea) from the Amazon Region

O presente estudo descreve e ilustra em detalhes os quatro primeiros estágios de Alpheus estuariensis Christoffersen, 1984 a partir de larvas cultivadas em laboratório. Duas fêmeas ovígeras foram coletadas no canal de maré do estuário de Bragança, estado do Pará, nordeste do Brasil. Após a eclosão, as larvas foram colocadas em pequenos recipientes (com 10 larvas em cada). As fêmeas foram depositadas no Museu Paraense Emilio Goeldi (MPEG 0803) e as larvas de cada estágio larval no Museu zoológico da Universidade de São Paulo (MUSP18452). Foram dissecadas 10 larvas e exúvias com finas agulhas sob um microscópio ocular. Comparações morfológicas com outros estudos reportados sobre o desenvolvimento larval de espécies de Alpheus são brevemente discutidas.

The larval development of Pinnixa gracilipes Coelho (Decapoda, Pinnotheridae) reared in the laboratory

Pinnixa gracilipes Coelho, 1997 é um pequeno caranguejo pinoterídeo que vive em associação com Lepidophthalmus siriboia Felder & Rodrigues, 1993 no nordeste do Estado do Pará, Brasil. Larvas de P. gracilipes foram cultivadas em laboratório desde o nascimento ao estágio megalopa. O desenvolvimento completo durou cerca de 24 dias. O período médio de cada estágio foi 5, 4, 4, 5 e 6 dias, respectivamente. No presente trabalho, os cinco estágios zoeae e megalopa são descritos e ilustrados em detalhes. Comparações morfológicas com estudos anteriores sobre larvas da família Pinnotheridae são brevemente discutidas.

The complete larval development of Armases benedicti (Rathbun) (Decapoda, Sesarmidae), from the Amazon region, reared in the laboratory

São descritos e ilustrados em detalhes, os quatro estágios de zoea e um de megalopa do caranguejo Armases benedicti (Rathbun, 1897), a partir de larvas obtidas em laboratório. A média de duração de cada estágio larval foi 3, 2, 4, 4 e 13 dias, respectivamente. O período compreendido desde a eclosão até o surgimento do primeiro juvenil foi de 26 dias. Morfologicamente A. benedicti é muito similar às outras espécies do gênero, contudo, um pequeno espinho lateral é claramente observado na carapaça das zoeas desta espécie. Esta característica aparenta ser única dentre os Sesarmidae. Outra característica distinta desta espécie é a distribuição das cerdas do endópodo da maxila (2+2), o qual difere dos demais sesarmídeos que apresentam a distribuição (2+3), exceto para Sesarma tetragonum (Fabricius, 1798) o qual apresenta (2+2). Outras comparações morfológicas com trabalhos anteriores relacionados a larvas do gênero Armases Abele, 1992 são brevemente discutidas.

The early phyllosoma stages of spiny lobster Panulirus echinatus Smith, 1869 (Decapoda: Palinuridae) reared in the laboratory

Os estágios iniciais de lagosta tropical Panulirus echinatus eclodiram e foram cultivados em laboratório. Fêmeas ovígeras foram capturadas em seu habitat e cuidadosamente transportadas para o laboratório. As larvas foram cultivadas em tanques de recirculação de água e alimentadas com náuplios de Artemia e gônadas mexilhão Brachydonts sp. Microalga Dunaliella viridis foi adicionada em cada tanque de cultivo na concentração de 150 x 10⁴ cel.mL^–1. Os filosomas mudaram oito vezes e o período de intermuda de cada instar foi de cerca de 7 a 10 dias. As principais mudanças morfológicas de cada apêndice foram descritas, ilustradas e comparadas com trabalhos anteriores.

Redescription of megalopa and juvenile development of Pachygrapsus gracilis (Decapoda: Grapsidae) from the Amazon region, reared in the laboratory

ABSTRACT: This present study re-describes the megalopa stage and provides detailed morphological descriptions and main growth changes observed in stages I through VII of the juvenile instars of the dark shore crab Pachygrapsus gracilis (Saussure, 1858), from the Amazon region. The specimens in this study were reared in the laboratory and the megalopae were collected at Ajuruteua beach in northeastern Pará, Brazil. Previous studies had described the megalopa of P. gracilis from Mexican waters, as well as those of Pachygrapsus transversus (Gibbes, 1850) and Pachygrapsus marmoratus (Fabricius, 1787). A comparison between the Mexican and Amazonian populations of P. gracilis revealed significant morphological differences. The main difference is the presence of 3 elongated setae on the 5th pereiopods of individuals of the Amazonian population. The setal number and their arrangement in the appendages also differed. In P. gracilis, the male and female genital openings are observed from the juvenile instar III, whereas differentiation in male pleopods is observed only in juvenile instar V. In females, the pleopods undergo rapid differentiation during juvenile instar VI. These morphological comparisons and other observations on development are briefly compared and discussed with reports for other species.