2-(4-Oxo-1,3-thiazolidin-2-ylidene)acetamid as promising scaffold for designing new antifungal compounds

1,3-Thiazolidin-4-one derivatives with a exocyclic C=C double bond in position 2 of the hetero ring have a wide spectrum of biological activity, but their fungicidal activity has not been studied as much as it should be. This paper presents a simple and convenient approach for obtaining potential antifungal agents based on 2-(4-oxo-1,3-thiazolidin-2-ylidene)acetamides. The first examples of evaluating the fungicidal activity of 8 obtained compounds on 8 strains of phytopathogenic fungi are presented. A highly active compound 4e with EC50 of 0.85 and 2.29 µg/mL against A. solani and P. lingam, respectively, was found to be promising for further study

Butanol production by Clostridium pasteurianum NRRL-598 using corn steep liquor as nutrient source / Produção de butanol por Clostridium pasteurianum NRRL-598 usando licor de maceração de milho como fonte de nutrientes

Butanol has become an interesting substitute for ethanol in additives and fuel applications due to its physical chemical properties. Several Clostridium strains are able to produce ABE (acetone, butanol and ethanol) solvents by fermentation. Efforts have been made to reduce cost of butanol biotechnological production in order to become this route competitive when compared to petrochemical technology. This study aimed to evaluate the use of corn steep liquor, a residue of corn industry, as unique nutrient source in culture medium for butanol production by Clostridium pasteurianum NRRL B-598. The strain is capable of producing butanol using only corn steep liquor as nutrient source. The yield was 0.30 gButanol/gglucose  and the butanol productivity was 0.11 g.L-1.h-1 using 20 g.L-1 of corn steep liquor. 

SiF4 anomalous behaviour reassessed

The Si 1s−1, Si 2s−1, and Si 2p−1 photoelectron spectra of the SiX4 molecules with X = F, Cl, Br, CH3 were measured. From these spectra the Si 1s−1 and Si 2s−1 lifetime broadenings were determined, revealing a significantly larger value for the Si 2s−1 core hole of SiF4 than for the same core hole of the other molecules of the sequence. This finding is in line with the results of the Si 2p−1 core holes of a number of SiX4 molecules, with an exceptionally large broadening for SiF4. For the Si 2s−1 core hole of SiF4 the difference to the other SiX4 molecules can be explained in terms of Interatomic Coulomb Decay (ICD)-like processes. For the Si 2p−1 core hole of SiF4 the estimated values for the sum of the Intraatomic Auger Electron Decay (IAED) and ICD-like processes are too small to explain the observed linewidth. However, the results of the given discussion render for SiF4 significant contributions from Electron Transfer Mediated Decay (ETMD)-like processes at least plausible. On the grounds of our results, some more molecular systems in which similar processes can be observed are identified

Spatio-temporal study and population structure of Daptonema Oxycerca (Nematoda: Xyalidae) in Coroa Grande, Rio de Janeiro, Brazil

Daptonema oxycerca foi descrita originalmente para o Mar do Norte, mas até o momento nada se conhece sobre essa espécie em regiões tropicais. A distribuição espaço-temporal e a estrutura populacional de D. oxycerca foram estudadas durante o período de um ano (de Maio 1998 a Abril 1999) em Coroa Grande, Rio de Janeiro, Brasil. Para a amostragem, dois transectos fixos e perpendiculares à linha d'água foram estabelecidos, e, em cada transecto, quatro níveis foram marcados para representar as zonas superior e inferior do médiolitoral. As menores temperaturas foram observadas no final do inverno e início da primavera e as maiores temperaturas no verão. A densidade de D. oxycerca variou durante o ano, com um pico em agosto. Essa tendência foi observada para os machos, as fêmeas grávidas e as fêmeas não-grávidas. A densidade da espécie correlacionou-se negativamente com a temperatura. A variação da razão sexual não foi significativa. D. oxycerca foi mais abundante no nível superior do médiolitoral em ambos os transectos. Esse trabalho representa o primeiro registro de D. oxycerca no Brasil, assim como, confirma a influência da temperatura na regulação de sua densidade populacional.Daptonema oxycerca was originally described from the North Sea and, up to now, nothing is known of this species in tropical regions. The spatio-temporal distribution and the population structure of this species was studied during one-year period (from May 1998 through April 1999) in Coroa Grande, Rio de Janeiro, Brazil. For sampling, two fixed, parallel transects were established perpendicularly to the shoreline, and at each transect, four, equally spaced levels were marked to represent the upper and the low intertidal zones. The lowest temperatures occurred in the end of the austral winter and first month of the spring and the highest temperatures occurred in the austral summer. The density of D. oxycerca varied during the year, with a peak in August. This tendency was observed for males, ovigerous females, and non-ovigerous females. The species density was negative correlated with temperature. The sex ratio was not statistically significant. D. oxycerca was most abundant at the upper intertidal level in both transects. This work provides the first record of D. oxycerca in Brazil, and confirms the influence of temperature in regulating its population density

Morphology of the male genital organs and cloaca of Rhea americana americana

As características morfológicas, macroscópicas e microscópicas, dos órgãos genitais masculinos e da cloaca foram analisados em 23 emas, quatro filhotes (duas semanas), sete jovens (de três a oito meses) e doze adultos (três anos), provenientes da Cooperativa Emas do Brasil, RS, e do CEMAS, Mossoró, RN. Os testículos da ema possuem formato alongado e localizam-se na cavidade celomática, na região intra-abdominal dorsal, com comprimento e larguras médias de 7,6±1,2cm e 2,6± 0,7cm nos adultos; 4,5±1,5cm e 0,9±0,4cm nos jovens; e 0,8±0,3cm, e 0,2±0,1cm nos filhotes. O testículo está envolto pela túnica albugínea e seu parênquima possui túbulos seminíferos irregulares, compostos por epitélio espermatogênico e por células de sustentação, e pelo tecido intersticial, com as células endócrinas intersticiais, tecido conjuntivo frouxo e vasos. Nos adultos observaram-se todas as células da linhagem espermatogênica, enquanto nos jovens com 3 meses, os testículos apresentaram túbulos seminíferos com luz reduzidas, espermatogônias e células de sustentação indiferenciadas. Os ductos eferentes possuem um epitélio cúbico ciliado, enquanto no ducto epididimário o epitélio é columnar. O epidídimo apresentou-se alongado e fusiforme junto a margem medial do testículo. O ducto deferentes apresentou trajeto sinuoso nos adultos, retilíneo nos jovens, convoluto na sua porção média, diminuindo seu formato sigmóide em sua porção caudal, próximo à cloaca. O epitélio é pseudoestratificado e reveste a luz irregular nos adultos e circular nos jovens, mantendo proximidade com o ureter. A cloaca dividiu-se em três segmentos: o coprodeu, o urodeo e o proctodeo. No urodeu os ductos deferentes desembocaram em papilas na parede ventro-lateral, próximo a inserção do falo fibroso. O falo é um órgão fibroso linfático, localizado na parede ventral, no assoalho da cloaca, e apresentou duas porções: uma rígida bifurcada e contorcida, e outra simples espiralada e flexível, a qual normalmente esteve invertida. Em exposição forçada, o falo teve 14 cm de comprimento. De forma geral os órgãos reprodutores das emas compartilharam da morfologia de outras aves, principalmente aquelas descritas para os avestruzes.The rhea (Rhea americana americana) is a bird that belongs to the group of the Ratitas, order Rheiforme and family Rheidae. Macroscopic and microscopic morphology of the male genital organ (testes, epididymis, deferent ducts, and phallus) and the cloaca were analyzed in 23 emas, four chicken (2 weeks old), young (3 to 10 months old), and twelve adult ones (3 years old), from Cooperativa Emas do Brasil, RS and from CEMAS, Mossoró, RN. The testis of rhea had elongated shape and were located inside coelomatic cavity, in dorsal region of abdominal cavity, with medium length and width of 7.6±1.2cm and 2.6±0.7cm at adult animals; 4.5±1.5cm and 0.9±0.4cm at young animals; and 0.8±0.3cm, and 0.2±0.1cm at chicken. The testis were recovered by the tunica albuginea and its parenchyma had seminiferous tubules composed by spermatogenic epithelium and by sustentation cells, and also interstitial tissue, with interstitial endocrine cells, connective tissue and vessels. At the adult animals were observed all the cells from spermatogenic lineage, whilst at the youngs with 3 months the seminiferous tubules had a smale lumen with spermatogonia and undifferentiated sustentacular cells. The efferents ductus were composed by a cubic ciliated epithelium, while the epididimydis duct had a columnar epithelium. The epididymis was elongated and fusiform closely to medial testis board. The deferent duct had sinuous stretch at adult animals, rectilineae at young animal, convolute at its medium portion, decreasing its sigmoid shape at caudal portion, next to cloaca. The epithelium was pseudostratified ciliated, irregular lumen at adult animal, and circular at young animal, closely with urether. The cloaca was divided into three segments: coprodeum, urodeum and proctodeum. At urodeum the deferent ducts discharged into papillas at the ventral side wall, next to fibrous phallus's insertion. The phallus was a lymphatic fibrous organ, located at ventral wall, at the cloaca floor, and was composed by two portions: one rigid forked and twisted, and another simple spiraled and flexible, which normally was inverted. In forced exposition, the phallus had 14 cm in length. In a general way the Rhea genital organs shared the morphology from others birds, mainly those described to the ostrich

Current State-of-Art and New Trends on Lipid Nanoparticles (SLN and NLC) for Oral Drug Delivery

Lipids and lipid nanoparticles are extensively employed as oral-delivery systems for drugs and other active ingredients. These have been exploited for many features in the field of pharmaceutical technology. Lipids usually enhance drug absorption in the gastrointestinal tract (GIT), and when formulated as nanoparticles, these molecules improve mucosal adhesion due to small particle size and increasing their GIT residence time. In addition, lipid nanoparticles may also protect the loaded drugs from chemical and enzymatic degradation and gradually release drug molecules from the lipid matrix into blood, resulting in improved therapeutic profiles compared to free drug. Therefore, due to their physiological and biodegradable properties, lipid molecules may decrease adverse side effects and chronic toxicity of the drug-delivery systems when compared to other of polymeric nature. This paper highlights the importance of lipid nanoparticles to modify the release profile and the pharmacokinetic parameters of drugs when administrated through oral route

Modified silicas covalently bounded to 5,10,15,20-tetrakis(2-hydroxy-5-nitrophenyl)porphyrinato iron(III): synthesis, spectroscopic and EPR characterization. Catalytic studies

In this work we have studied cyclooctene epoxidation with PhIO, using a new iron porphyrin, 5,10,15,20-tetrakis(2-hydroxy-5-nitrophenyl)porphyrinato iron(III), supported on silica matrices via eletrostatic interaction and / or covalent bonds as catalyst. These catalysts were obtained and immobilized on the solid supports propyltrimethylammonium silica (SiN+); propyltrimethylammonium and propylimidazole silica [SiN+(IPG)] and chloropropylsilica (CPS) via elestrostatic interactions and covalent binding. Characterization of the supported catalysts by UV-Vis spectroscopy and EPR (Electron paramagnetic resonance) indicated the presence of a mixture of FeII and FeIII species in all of the three obtained catalysts. In the case of (Z)-cyclooctene epoxidation by PhIO the yields observed for cis-epoxycyclooctane were satisfactory for the reactions catalyzed by the three materials (ranging from 68% to 85%). Such results indicate that immobilization of metalloporphyrins onto solid supports via groups localized on the ortho positions of their mesophenyl rings can lead to efficient catalysts for epoxidation reactions. The catalyst 1-CPS is less active than 1-SiN and 1-SiN(IPG), this argues in favour of the immobilization of this metalloporphyrin onto solids via electrostatic interactions, which is easier to achieve and results in more active oxidation catalysts. Interestingly, the activity of the supported catalysts remained the same even after three successive recyclings; therefore, they are stable under the oxidizing conditions.Neste trabalho estudamos a epoxidação do cicloocteno com PhIO utilizando uma nova porfirina 5,10,15,20-tetraquis(2-hidroxi-5-nitrofenil)porfirinato de ferro(III), suportada em matrizes de sílica via interação eletrostática e / ou ligações covalentes, como catalisador. Estes catalisadores foram obtidos e imobilizados em suporte sólido (sílica propiltrimetilamônio (SiN+); sílica propiltrimetilamônio e propilimidazol [SiN+(IPG)] e cloropropilsílica (CPS)) via interações eletrostáticas e ligações covalentes. A caracterização do catalisador suportado por UV-Vis e EPR (ressonância eletrônica paramagnética) indicou a presença de uma mistura de espécies de FeII e FeIII em todos os catalisadores obtidos. No caso da epoxidação do (Z)-cicloocteno por PhIO, os rendimentos observados para o cis-epoxiciclooctano foram satisfatórios para as reações catalisadas pelos três materiais (entre 65 e 85%). Estes resultados indicam que a imobilização de metaloporfirinas em suportes sólidos via grupos localizados na posição orto de seus anéis mesofenil pode promover a catálise eficiente das reações de epoxidação. O catalisador 1-CPS é menos ativo que 1-SiN e 1-SiN(IPG), o que está em acordo com a imobilização destas metaloporfirinas em suportes sólidos via interações eletrostáticas, o que é mais fácil de ocorrer e resulta em um catalisador mais ativo. A atividade do catalisador suportado permaneceu a inalterada, mesmo após três reciclos sucessivos, mostrando que eles são estáveis sob condições oxidantes

Cymoxanil inhibits respiration through inhibition of mitochondrial complex IV

Cymoxanil is a synthetic acetamide fungicide, used against oomycetes. It was first introduced in 1977 and can be used against downy mildew diseases induced by Plasmopara viticola in grapevine cultures and late blight diseases caused by Phytophthora infestans, in tomatoes and potatoes cultures. This fungicide is used in mixed formulations and its higher solubility enables a relatively widespread occurrence in toxic concentrations in aquatic environments. Although it has been used over the years, its biochemical mode of action is not yet known. Some studies reported that cymoxanil affects growth, respiration, DNA, RNA and protein synthesis and RNA polymerase activity of Phytophthora infestans, and it was reported to inhibit cell growth and biomass production and decrease the respiration rate of S. cerevisiae. Using yeast S. cerevisiae as model, we further characterized its effect on mitochondria. We found that whole cells treated with cymoxanil present a higher inhibition of oxygen consumption after 3 h of treatment that remains over time. Using isolated mitochondria, we observe that cymoxanil inhibits respiratory rate of yeast cells by inhibiting oxidative phosphorylation, through inhibition of complex IV activity. Although other targets cannot be excluded, our data provide new information about mode of action of cymoxanil that can be instrumental to drive informed management regarding the use of this fungicide.info:eu-repo/semantics/publishedVersio