Interaction of membrane mimetic vesicles with the antimicrobial peptide gomesin and its analogues

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Detection of Mycoplasma pulmonis in laboratory rats and technicians

Five species of mycoplasma are associated with several rat diseases. Mycoplasma pulmonis is the most important and most studied, possibly causing disease in rats and undermining the validity of laboratory experiments. M. pulmonis was isolated in 144/240 laboratory rats and identified by PCR in 155/240. This species was also detected in 12 human individuals (technicians of a laboratory animal house hold) in contact with these rats. The results were confirmed by sequencing of DNA products. Mycoplasma species are host specific; however, M. pulmonis was identified in humans, suggesting a case of unspecific colonization. Statistical analysis shows a greater risk for M. pulmonis colonizing individuals who are exposed to infected rats in animal facilities than individuals who do not. The detection of M. pulmonis in humans indicates a new status for this mollicute mycoplasmas in animal-holding facilities.

Structural and thermodynamic analysis of thrombin:suramin interaction in solution and crystal phases

Suramin is a hexasulfonated naphthylurea which has been recently characterized as a non-competitive inhibitor of human alpha-thrombin activity over fibrinogen, although its binding site and mode of interaction with the enzyme remain elusive. Here, we determined two X-ray structure of the thrombin: suramin complex, refined at 2.4 angstrom resolution. While a single thrombin: suramin complex was found in the asymmetric unit cell of the crystal, some of the crystallographic contacts with symmetrically related molecules are mediated by both the enzyme and the ligand. Molecular dynamics simulations with the 1:1 complex demonstrate a large rearrangement of suramin in the complex, but with the protein scaffold and the more extensive protein-ligand regions keep unchanged. Small-angle X-ray scattering measurements at high micromolar concentration demonstrate a suramin-induced dimerization of the enzyme. These data indicating a dissimilar binding mode in the monomeric and oligomeric states, with a monomeric, 1:1 complex to be more likely to exist at the thrombin physiological, nanomolar concentration range. Collectively, close understanding on the structural basis for interaction is given which might establish a basis for design of suramin analogues targeting thrombin. Crown Copyright (C) 2009 Published by Elsevier B.V. All rights reserved.

Synthesis of the Macrolactone of Migrastatin and Analogues with Potent Cell-Migration Inhibitory Activity

The synthesis of the macrolactone core of migrastatin 2, its potent anti-metastasis analogue 34, and ester derivatives 35 and 38 are reported. The approach involves the use of a dihydroxylation reaction to establish the desired C-8 stereocenter followed by a metathesis cyclization reaction. The effects of the compounds on the migration and invasion of human breast cancer cells were evaluated by using the wound-healing and the Boyden-chamber cell-migration and cell-invasion assays. The results revealed a high potency of the macrolactones 2 and 34 and the ester analogues 35 and 38, which suggests they have potential as antimetastatic agents.

Synthesis and analgesic profile of conformationally constrained N-acylhydrazone analogues: Discovery of novel N-arylideneamino quinazolin-4(3H)-one compounds derived from natural safrole

In this work we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and platelet anti-aggregating properties of new 3-(arylideneamino)-2-methyl-6,7-methylenedioxy-quinazolin-4 (3H)-one derivatives (3a-j), designed as conformationally constrained analogues of analgesic 1,3- benzodioxolyl-N- acylhydrazones (1) previously developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (2) as starting material. The pharmacological assays lead us to identify compounds LASSBio-1240 (3b) and LASSBio-1272 (3d) as new analgesic prototypes, presenting an antinociceptive pro. le more potent and effective than dipyrone and indomethacin used, respectively, as standards in AcOH-induced abdominal constrictions assay and in the formalin test. These results confirmed the success in the exploitation of conformation restriction strategy for identification of novel cyclic N-acylhydrazone analogues with optimized analgesic profile (C) 2009 Elsevier Ltd. All rights reserved.

Have Biofuel, Will Travel: A Colorful Experiment and a Different Approach To Teach the Undergraduate Laboratory

The substitution of petroleum-based fuels with those from renewable sources has gained momentum worldwide. A UV-vis experiment for the quantitative analysis of biofuels (bioethanol or biodiesel) in (petroleum-based) diesel oil has been developed. Before the experiment, students were given a quiz on biofuels, and then they were asked to suggest a suitable UV-vis experiment for the quantification of biofuels in diesel oil. After discussing the results of the quiz, the experiment was conducted. This included the determination of lambda(max) of the medium-dependent, that is, solvatochromic, visible absorption band of the probe 2,6-bis[4-(tert-butyl)phenyl]-4-{2,4,6-tris[4-(tert-butyl)phenyl]pyridinium-1-yl}phenolate as a function of fuel composition. The students appreciated that the subject was linked to a daily situation and that they were asked to suggest the experiment. This experiment served to introduce the phenomena of solvation and solvatochromism.

Stereoselective synthesis of azetidine-derived glutamate and aspartate analogues from chiral azetidin-3-ones

The stereoselective syntheses of cis conformationally constrained glutamate and aspartate analogues, containing an azetidine framework were accomplished from (S)-N-tosyl-2-phenylglycine in moderate overall yields. The key steps in these syntheses involved an efficient Wittig olefination of an azetidin-3-one, followed by a highly stereoselective rhodium catalyzed hydrogenation. The route could also be applied to the synthesis of a trans glutamate analogue, since epimerization of cis to trans isomer could be performed using DBU in toluene at reflux. (C) 2008 Elsevier Ltd. All rights reserved.

Immobilized analogues of sunflower trypsin inhibitor-1 constitute a versatile group of affinity sorbents for selective isolation of serine proteases

Sunflower trypsin inhibitor-1 (SFI-1), a natural 14-residue cyclic peptide, and some of its synthetic acyclic variants are potent protease inhibitors displaying peculiar inhibitory profiles. Here we describe the synthesis and use of affinity sorbents prepared by coupling SFTI-1 analogues to agarose resin. Chymotrypsinand trypsin-like proteases could then be selectively isolated from pancreatin; similarly, other proteases were obtained from distinct biological sources. The binding capacity of [Lys5]-SFTI-1-agarose for trypsin was estimated at over 10 mg/mL of packed gel. SFTI-1-based resins could find application either to improve the performance of current purification protocols or as novel protease-discovery tools in different areas of biological investigation. (C) 2009 Elsevier B.V. All rights reserved.

Section of Television Laboratory at the New York Trade School

Several students are shown working in a section of the Television Laboratory at the New York Trade School. Black and white photograph with some damage due to writing in red ink along the long edges.

Experiencing Science in Action: The Use of Exhibition Techniques in Guided Tours to a Scientific Laboratory

The current paper presents a study conducted at CERN, Switzerland, to investigate visitors' and tour guides' use and appreciation of existing panels at visit itinerary points. The results were used to develop a set of recommendations for constructing optimal panels to assist the guides' explanation.

Science is Primary - Children Thinking and Learning in theChemistry Laboratory

The goal of primary science education is to foster children’s interest, develop positive science attitudes and promote science process skills development. Learning by playing and discovering provides several opportunities for children to inquiry and understand science based on the first–hand experience. The current research was conducted in the children’s laboratory in Heureka, the Finnish science centre. Young children (aged 7 years) which came from 4 international schools did a set of chemistry experiments in the laboratory. From the results of the cognitive test, the pre-test, the post-test, supported by observation and interview, we could make the conclusion that children enjoyed studying in the laboratory. Chemistry science was interesting and fascinating for young children; no major gender differences were found between boys and girls learning in the science laboratory. Lab work not only encouraged children to explore and investigate science, but also stimulated children’s cognitive development.

Comparison of learning between Digital gallery and Hands-on Laboratory

This thesis has been done in ROM (Royal Ontario Museum) located in Toronto Canada. It focuses on learning in two parts of the museum. It tries to find out how much each part is effective in terms of learning. Studies have been done in the Digital gallery, which has been equipped with digital video projector and workstation that allows visitors to interact with the collections in 2 or 3 dimensional spaces while they are watching the presenting film. The rest of the study was in Hands-on laboratory, which allows students to examine artifacts and discuss their findings .The method was used in this research is Concept mapping .In Digital gallery, 24 schools surveys in the form of pre-post- test by help of the concept mapping method has been done. In Hands-on laboratory, 12 schools have been studied by using the combination of interviewing and written pre post-test of concept mapping.

Print quality study of a laboratory offset press

PAPRO operates within the Forest Research company and their mission is to develop value-addingindustry solutions. At present there are no good ways for mills to easily test the printing quality on newsprintpaper. There is a great need for a fast way to do this on different paper qualities; with a laboratory-offset press this can be both a time and money saving method. At PAPRO Forest Research, NewZealand, a laboratory offset press has been developed and designed, during the past seven years, concerningthis issue. Earlier projects were made concerning the press, e.g. to establish the optimal settings.The mission with this project was to partly determine the present variability of the print quality andto evaluate if the fountain solution, distilled water and 2% Diol green concentrate, used at the momentmixed with different percentages of Isopropanol could decrease the variability and contribute to morestabile results. Throughout the whole project the print quality showed a high variation and was evenmore variable when the Isopropanol was added. All in all 50 print rounds times twelve printed paperstrips was carried out through the project divided into three parts. To analyse the print quality, amicroscope with an image capture camera has been used. Data from the taken images was analysedand inserted into charts to see the variations.The conclusions of the whole project are not satisfying because no final evaluations were possible tomake. Main conclusions are that the additive of Isopropanol to the ordinary fountain solution, used atpresent, only contributed to more unstable results of the print quality. And it seems to be difficult toget some stable results from the lab press as long as the room where it is placed is not fully conditionedas required for the process of offset printing. And the fact that the airbrush which applies theamount of fountain solution is also variable, as shown in earlier projects, which contributes to unstableresults as well. For further work more exact parameters as a conditioned room are required and thepossibility to further design the laboratory press to use waterless offset printing instead.

Lithography Laboratory 3

Photograph of students at the Voorhees Technical Institute.