Design And Synthesis Of N-acylated Aza-goniothalamin Derivatives And Evaluation Of Their In Vitro And In Vivo Antitumor Activity.

Herein we describe the synthesis of a focused library of compounds based on the structure of goniothalamin (1) and the evaluation of the potential antitumor activity of the compounds. N-Acylation of aza-goniothalamin (2) restored the in vitro antiproliferative activity of this family of compounds. 1-(E)-But-2-enoyl-6-styryl-5,6-dihydropyridin-2(1H)-one (18) displayed enhanced antiproliferative activity. Both goniothalamin (1) and derivative 18 led to reactive oxygen species generation in PC-3 cells, which was probably a signal for caspase-dependent apoptosis. Treatment with derivative 18 promoted Annexin V/7-aminoactinomycin D double staining, which indicated apoptosis, and also led to G2 /M cell-cycle arrest. In vivo studies in Ehrlich ascitic and solid tumor models confirmed the antitumor activity of goniothalamin (1), without signs of toxicity. However, derivative 18 exhibited an unexpectedly lower in vivo antitumor activity, despite the treatments being administered at the same site of inoculation. Contrary to its in vitro profile, aza-goniothalamin (2) inhibited Ehrlich tumor growth, both on the ascitic and solid forms. Our findings highlight the importance of in vivo studies in the search for new candidates for cancer treatment.

Use Of Experimental Design To Optimize A Triple-potential Waveform To Develop A Method For The Determination Of Streptomycin And Dihydrostreptomycin In Pharmaceutical Veterinary Dosage Forms By Hplc-pad.

An HPLC-PAD method using a gold working electrode and a triple-potential waveform was developed for the simultaneous determination of streptomycin and dihydrostreptomycin in veterinary drugs. Glucose was used as the internal standard, and the triple-potential waveform was optimized using a factorial and a central composite design. The optimum potentials were as follows: amperometric detection, E1=-0.15V; cleaning potential, E2=+0.85V; and reactivation of the electrode surface, E3=-0.65V. For the separation of the aminoglycosides and the internal standard of glucose, a CarboPac™ PA1 anion exchange column was used together with a mobile phase consisting of a 0.070 mol L(-1) sodium hydroxide solution in the isocratic elution mode with a flow rate of 0.8 mL min(-1). The method was validated and applied to the determination of streptomycin and dihydrostreptomycin in veterinary formulations (injection, suspension and ointment) without any previous sample pretreatment, except for the ointments, for which a liquid-liquid extraction was required before HPLC-PAD analysis. The method showed adequate selectivity, with an accuracy of 98-107% and a precision of less than 3.9%.

Ecological Literacy And Beyond: Problem-based Learning For Future Professionals.

Ecological science contributes to solving a broad range of environmental problems. However, lack of ecological literacy in practice often limits application of this knowledge. In this paper, we highlight a critical but often overlooked demand on ecological literacy: to enable professionals of various careers to apply scientific knowledge when faced with environmental problems. Current university courses on ecology often fail to persuade students that ecological science provides important tools for environmental problem solving. We propose problem-based learning to improve the understanding of ecological science and its usefulness for real-world environmental issues that professionals in careers as diverse as engineering, public health, architecture, social sciences, or management will address. Courses should set clear learning objectives for cognitive skills they expect students to acquire. Thus, professionals in different fields will be enabled to improve environmental decision-making processes and to participate effectively in multidisciplinary work groups charged with tackling environmental issues.

Effectiveness of a new toothbrush design versus a conventional tongue scraper in improving breath odor and reducing tongue microbiota

For centuries, specific instruments or regular toothbrushes have routinely been used to remove tongue biofilm and improve breath odor. Toothbrushes with a tongue scraper on the back of their head have recently been introduced to the market. The present study compared the effectiveness of a manual toothbrush with this new design, i.e., possessing a tongue scraper, and a commercial tongue scraper in improving breath odor and reducing the aerobic and anaerobic microbiota of tongue surface. The evaluations occurred at 4 moments, when the participants (n=30) had their halitosis quantified with a halimeter and scored according to a 4-point scoring system corresponding to different levels of intensity. Saliva was collected for counts of aerobic and anaerobic microorganisms. Data were analyzed statistically by Friedman's test (p<0.05). When differences were detected, the Wilcoxon test adjusted for Bonferroni correction was used for multiple comparisons (group to group). The results confirmed the importance of mechanical cleaning of the tongue, since this procedure provided an improvement in halitosis and reduction of aerobe and anaerobe counts. Regarding the evaluated methods, the toothbrush's tongue scraper and conventional tongue scraper had a similar performance in terms of breath improvement and reduction of tongue microbiota, and may be indicated as effective methods for tongue cleaning.

Influence of specimens' design and manufacturing process on microtensile bond strength to enamel: laboratory and FEA comparison

This study evaluated the effect of specimens' design and manufacturing process on microtensile bond strength, internal stress distributions (Finite Element Analysis - FEA) and specimens' integrity by means of Scanning Electron Microscopy (SEM) and Laser Scanning Confocal Microscopy (LCM). Excite was applied to flat enamel surface and a resin composite build-ups were made incrementally with 1-mm increments of Tetric Ceram. Teeth were cut using a diamond disc or a diamond wire, obtaining 0.8 mm² stick-shaped specimens, or were shaped with a Micro Specimen Former, obtaining dumbbell-shaped specimens (n = 10). Samples were randomly selected for SEM and LCM analysis. Remaining samples underwent microtensile test, and results were analyzed with ANOVA and Tukey test. FEA dumbbell-shaped model resulted in a more homogeneous stress distribution. Nonetheless, they failed under lower bond strengths (21.83 ± 5.44 MPa)c than stick-shaped specimens (sectioned with wire: 42.93 ± 4.77 MPaª; sectioned with disc: 36.62 ± 3.63 MPa b), due to geometric irregularities related to manufacturing process, as noted in microscopic analyzes. It could be concluded that stick-shaped, nontrimmed specimens, sectioned with diamond wire, are preferred for enamel specimens as they can be prepared in a less destructive, easier, and more precise way.

Cultivares de batata para sistemas orgânicos de produção

Informações a respeito de cultivares adaptadas ao sistema de cultivo orgânico são escassas. O objetivo deste estudo foi avaliar, sob sistema de cultivo orgânico, genótipos nacionais e estrangeiros desenvolvidos para o cultivo convencional, quanto ao potencial produtivo, em condições de campo. O experimento foi conduzido em 2008, no Pólo APTA Leste Paulista, em Monte Alegre do Sul-SP. O delineamento experimental foi em blocos ao acaso, com 18 tratamentos e quatro repetições. Cada parcela foi constituída por 80 batatas-semente, dispostas em quatro linhas de 5 m de comprimento, espaçadas de 80 cm, com 25 cm entre tubérculos. Os genótipos avaliados foram Agata, Asterix, Caesar, Cupido, Éden, Melody, Novella e Vivaldi, de origem estrangeira; e Apuã, Aracy, Catucha, IAC Aracy Ruiva, Itararé, Monte Alegre 172, IAC 6090, APTA 16.5, APTA 15.20 e APTA 21.54, nacionais. Foram avaliadas as características de produtividade total e comercial de tubérculos, massa média total e comercial de tubérculos, teor de matéria seca e severidade da pinta-preta (Alternaria solani). Os clones APTA 16.5, APTA 21.54 e IAC 6090, e as cultivares Cupido, Apuã, Itararé e Monte Alegre 172 foram os mais produtivos. 'APTA 21.54' superou os demais em relação a produtividade comercial (18,07 t ha-1), sendo que 'APTA 16.5', 'Cupido', 'IAC 6090' e 'Itararé' formaram o segundo grupo. As maiores massas médias de tubérculos foram apresentadas pelas cultivares Itararé e Cupido. O clone IAC 6090 e as cultivares Aracy e Aracy Ruiva foram as que apresentaram maiores teores de matéria seca, com valor médio de 22,91%. 'APTA 16.5', 'Apuã', 'Aracy', 'Aracy Ruiva', 'Éden', 'Ibituaçú' e 'Monte Alegre 172' apresentaram alto nível de resistência à pinta-preta. As cultivares Itararé, Apuã e Cupido são adaptadas ao cultivo orgânico, e os clones avançados APTA 16.5, APTA 21.54 e IAC 6090 apresentam potencial de cultivo no sistema orgânico.

Design, construction and evaluation of a simple pressurized solvent extraction system

This work describes the construction and testing of a simple pressurized solvent extraction (PSE) system. A mixture of acetone:water (80:20), 80 ºC and 103.5 bar, was used to extract two herbicides (Diuron and Bromacil) from a sample of polluted soil, followed by identification and quantification by high-performance liquid chromatography coupled with diode array detector (HPLC-DAD). The system was also used to extract soybean oil (70 ºC and 69 bar) using pentane. The extracted oil was weighed and characterized through the fatty acid methyl ester analysis (myristic (< 0.3%), palmitic (16.3%), stearic (2.8%), oleic (24.5%), linoleic (46.3%), linolenic (9.6%), araquidic (0.3%), gadoleic (< 0.3%), and behenic (0.3%) acids) using high-resolution gas chromatography with flame ionization detection (HRGC-FID). PSE results were compared with those obtained using classical procedures: Soxhlet extraction for the soybean oil and solid-liquid extraction followed by solid-phase extraction (SLE-SPE) for the herbicides. The results showed: 21.25 ± 0.36% (m/m) of oil in the soybeans using the PSE system and 21.55 ± 0.65% (m/m) using the soxhlet extraction system; extraction efficiency (recovery) of herbicides Diuron and Bromacil of 88.7 ± 4.5% and 106.6 ± 8.1%, respectively, using the PSE system, and 96.8 ± 1.0% and 94.2 ± 3.9%, respectively, with the SLP-SPE system; limit of detection (LOD) and limit of quantification (LOQ) for Diuron of 0.012 mg kg-1 and 0.040 mg kg-1, respectively; LOD and LOQ for Bromacil of 0.025 mg kg-1 and 0.083 mg kg-1, respectively. The linearity used ranged from 0.04 to 1.50 mg L-1 for Diuron and from 0.08 to 1.50 mg L-1 for Bromacil. In conclusion, using the PSE system, due to high pressure and temperature, it is possible to make efficient, fast extractions with reduced solvent consumption in an inert atmosphere, which prevents sample and analyte decomposition.

Atherinella blackburni (Schultz, 1949) at Itamambuca Beach, Ubatuba, SP: ecological characterization and distribution on the Brazilian coast (Teleostei: Atheriniformes: Atherinopsidae)

Atherinella blackburni is a silverside species whose occurrence on the Brazilian coast was not properly registered until recently. So far, records of its distribution along the Brazilian shore were limited to Itaparica Island, Bahia State, and Porto Inhaúma, Rio de Janeiro State. In a recent survey of the ichthyofauna of Itamambuca Beach, Ubatuba, São Paulo State, 100 specimens of this species were collected, yielding a considerable source of information regarding its ecology and a new southern limit of its distribution. A detailed survey of an ichthyological collection revealed lots of this species from regions of the Brazilian Northeast, resulting in a northward expansion of the occurrence of A. blackburni in Brazilian waters. Besides the populations found on the Brazilian coast, the species also occurs discontinuously in the Atlantic coasts of Costa Rica, Panama and Venezuela. Meristic and morphometric analysis showed overlapped values between Brazilian populations and the ones closer to the Caribbean. An ecological study of A. blackburni at Itamambuca Beach revealed that it is a predominantly diurnal species with preference for warm and salty waters, often occurring in sandy-bottom environments. It was more abundant in Summer and Winter, when individuals with smaller values of length and weight also occurred.

Ecological aspects of the surf-zone ichthyofauna of Itamambuca Beach, Ubatuba, SP

Sandy beaches are among the most extensive environments in Brazil and are generally threatened by disorderly urban growth due to their location along the coast, where human populations tend to concentrate. This is especially true in southeastern Brazil, where the largest urban areas are located. Thus, better knowledge regarding these natural resources is of considerable importance. The surf zone of sandy beaches is inhabited by a number of fish species, including juveniles seeking both food and shelter from predators. An ecological survey was conducted in the surf zone of Itamambuca beach in the city of Ubatuba, São Paulo State, Brazil, in order to evaluate the composition, structure and dynamics of the fish fauna using community descriptors. Diurnal and nocturnal samples were taken with a beach seine at five oceanographic stations over a 12-month period. Water temperature and salinity were also recorded. A total of 2,147 individuals representing 34 species and 18 families were sampled. The main variation in fish fauna was detected on the diel level, followed by a spatial repartition possibly related to salinity. Seasonal variation was also observed. The five most important species in the overall context were Atherinella brasiliensis, Eucinostomus melanopterus, Mugil sp., Trachinotus goodei and Atherinella blackburni.

Culicidae (Diptera, Culicomorpha) from the western Brazilian Amazon: Juami-Japurá Ecological Station

With 312 trap-hours of sampling effort, 1554 specimens of Culicidae (Diptera) were collected, using CDC and Malaise traps, in nine different locations along the Juami River, within the Juami-Japurá Ecological Station, Amazonas State, Brazil. A list of mosquito species with 54 taxa is presented, which includes three new distributional records for the state of Amazonas. The species found belong to the genera Anopheles, Aedeomyia, Aedes, Psorophora, Culex, Coquillettidia, Sabethes, Wyeomyia and Uranotaenia.

American cutaneous leishmaniasis in the Pontal of Paranapanema - SP, Brazil: ecological and entomological aspects

American cutaneous leishmaniasis (ACL) occurs in epidemic outbreaks and in sporadic cases with small annual variation in the Pontal of Paranapanema, SP. There is little research on the sandfly fauna of this region. The last outbreaks were related to the Movement of the Landless Workers (MST) and with the ecological tourism in preserved forest of the Parque Estadual do Morro do Diabo (PEMD). AIM: identification of the sandfly fauna within the PEMD, mainly anthropophilic species already incriminated as vectors of ACL, as well as their seasonality, hourly frequency and data of the behavior. M&M: The captures were undertaken with CDC light and Shannon traps from 6:00 pm to 10:00 pm, monthly from May 2000 to December 2001. The temperature and relative humidity data were registered at hourly intervals. RESULTS: The captured species were: Brumptomyia brumpti, Nyssomyia neivai, Nyssomyia whitmani, Pintomyia fischeri and Pintomyia pessoai. The P. pessoai predominated (34.39%) and N. neivai was less found (0.74%), only being captured in CDC traps. Shannon trap captured more sandflies (63.01%) than the CDC traps (36.99%). Despite the environmental degradation anthropophilic species, indicates favorable bioecological conditions for persistence of vectors and potential transmission of leishmaniasis.

Epidemiological and ecological aspects related to malaria in the area of influence of the lake at Porto Primavera dam, in western São Paulo State, Brazil

A study was carried out in the area of influence of the Porto Primavera Hydroelectric Power Station, in western São Paulo State, to investigate ecological and epidemiological aspects of malaria in the area and monitor the profile of the anopheline populations following the environmental changes brought about by the construction of the lake. Mosquitoes captured were analyzed by standardized indicator species analysis (ISA) before and during different flooding phases (253 m and 257 m elevations). The local human population was studied by means of parasitological (thin/thick blood smears), molecular (PCR) and serological tests. Serological tests consisted of Enzyme Linked Immunosorbent Assay (ELISA) with synthetic peptides of the circumsporozoite protein (CSP) from classic Plasmodium vivax, P. vivax variants (VK247 and "vivax-like"), P. malariae and P. falciparum and Indirect Immunofluorescence Assay (IFA) with asexual forms of P. vivax, P. malariae and P. falciparum. The results of the entomological survey indicated that, although the Anopheles darlingi population increased after the flooding, the population density remained very low. No malaria, parasite infection or DNA was detected in the inhabitants of the study area. However, there was a low frequency of antibodies against asexual forms and a significant prevalence of antibodies against P. vivax, P. vivax variants, P. falciparum and P. malariae; the presence of these antibodies may result from recent or less recent contact with human or simian Plasmodium (a parallel study in the same area revealed the existence of a sylvatic cycle). Nevertheless, these results suggest that, as in other places where malaria is present and potential vectors circulate, the local epidemiological conditions observed could potentially support the transmission of malaria in Porto Primavera Lake if infected individuals are introduced in sufficient numbers. Further studies are required to elucidate the phenomena described in this paper.

Discrepancies among ecological, household, and individual data on fruits and vegetables consumption in Brazil

Information on fruits and vegetables consumption in Brazil in the three levels of dietary data was analyzed and compared. Data about national supply came from Food Balance Sheets compiled by the FAO; household availability information was obtained from the Brazilian National Household Budget Survey (HBS); and actual intake information came from a large individual dietary intake survey that was representative of the adult population of São Paulo city. All sources of information were collected between 2002 and 2003. A subset of the HBS, representative of São Paulo city, was used in our analysis in order to improve the quality of the comparison with actual intake data. The ratio of national supply to household availability of fruits and vegetables was 2.6 while the ratio of national supply to actual intake was 4.0. The discrepancy ratio in the comparison between household availability and actual intake was smaller, 1.6. While the use of supply and availability data has advantages, as lower cost, must be taken into account that these sources tend to overestimate actual intake of fruits and vegetables.

Design and characterization of bridged loop-gap resonators for use in electron paramagnetic resonance measurements

This paper revisits the design of L and S band bridged loop-gap resonators (BLGRs) for electron paramagnetic resonance applications. A novel configuration is described and extensively characterized for resonance frequency and quality factor as a function of the geometrical parameters of the device. The obtained experimental results indicate higher values of the quality factor (Q) than previously reported in the literature, and the experimental analysis data should provide useful guidelines for BLGR design.