Synthesis and biological evaluation of trifluralin analogues as antileishmanial agents

A series of new analogues of trifluralin (TFL) were synthesized and characterized in view of changing the unfavorable properties that limits its use as antileishmanial agent. Some of the TFL analogues display more activity than a standard drug (miltefosine) against the promastigote forms of Leishmania infantum and Leishmania donovani and the intracellular form (THP-1 infected with L. infantum). All analogues showed a clear advantage over miltefosine, as they are not hemolytic. Some analogues can conjugate these characteristics with reduced cell toxicity and improved intracellular activity.     

Synergy of fatty acid and reactive alkenal activation of proton conductance through uncoupling protein 1 in mitochondria

The kinetics of proton transport through mammalian UCP1 (uncoupling protein 1) expressed in yeast mitochondria were measured. There was little or no UCP1 activity in the absence of added palmitate, but significant activity in its presence. The activator 4-HNE (4-hydroxy-2-nonenal) had little effect when added alone, but significantly enhanced proton conductance in the presence of added palmitate. Activation of the proton conductance of UCP1 was synergistic: proton conductance in the presence of both palmitate and 4-HNE was significantly greater than the sum of the individual effects. Mitochondria from control yeast transformed with empty vector showed no such synergy, showing that synergy is a property of UCP1. Activation by the 4-HNE analogue trans-cinnamate showed essentially the same characteristics as activation by 4-HNE. Mitochondria from brown adipose tissue also showed synergistic activation of GDP-sensitive proton conductance by palmitate and 4-HNE. These results show that reactive alkenals activate the proton conductance of UCP1 more strongly when fatty acids are also added, with implications for both mechanistic and physiological models of UCP1 activation.     

Influence of Hydrological Pulse on Bacterial Growth and DOC Uptake in a Clear-Water Amazonian Lake

This study was conducted to evaluate: (1) the bacterial growth and the dissolved organic carbon (DOC) uptake in an Amazonian lake (Lake Batata) at high-water and low-water periods of the flood pulse; (2) the influence of nitrogen and phosphorus (NP) additions on bacterial growth and DOC uptake in Lake Batata at two flood pulse periods; and (3) the bioavailability of the main DOC sources in Lake Batata. Lake Batata is a typical clear-water Amazonian lake, located in the watershed of Trombetas River, Central Amazon, Brazil. Bacterial batch cultures were set up with 90% 0.2-μm filtered water and 10% inoculum from Lake Batata. N-NH₄NO₃ and P-KH₂PO₄, with final concentrations of 50 and 5 μM, respectively, were added to the cultures, except for controls. Extra sources of DOC (e.g., algal lysate, plant leachates) were added to constitute six distinct treatments. Bacterial response was measured by maximum bacterial abundance and rates of bacterial production, respiration, DOC uptake, and bacterial growth efficiency (BGE). Bacterial growth and DOC uptake were higher in NP treatments than in controls, indicating a consistent nutrient limitation in Lake Batata. The composition of DOC also seems to be an important regulating factor of bacterial growth in Lake Batata. Seasonally, bacterial growth and DOC bioavailability were higher at low-water period, when the phytoplankton is a significant extra source of DOC, than at high-water period, when the forest is the main source of DOC. DOC bioavailability was better estimated based on the diversity and the diagenetic stage of carbon compounds than on single classes of labile compounds. Changes in BGE were better related to CNP stoichiometry in the water, and the “excess” of organic substrates was oxidized in catabolism, despite the quality of these compounds for bacterial growth. Finally, we conclude that bacterial growth and DOC uptake vary throughout the flood pulse in clear-water Amazonian ecosystems as a result of changes in nutrient concentration and in DOC composition.     

Changes in the allocation of some chemical compounds in structures of Oryza glumaepatula (Steud) in an Amazonian lake subjected to an anthropic impact (Lake Batata, Porto Trombetas)

Lake Batata is a typical clear water lake of the Amazon, located at the right margin of the Trombetas River, at the town of Porto Trombetas (PA). It is subjected to a large and predictable variation of the water level, greater than 6 m, being in the floodplain of the Trombetas River. For 10 years (1979–1989) Lake Batata has received the tailings of bauxite processing from the activities of Mineração Rio do Norte S.A. These tailings impacted about 30% of its total area with an effluent of fine granulometry. Nowadays, two different areas can be observed at Lake Batata, one impacted by the bauxite tailings and one where the natural characteristics have been preserved. The aquatic macrophyte Oryza glumaepatula (Steud), known as wild rice, is one of the species found in the two areas, impacted and natural. The goal of this research was to evaluate the concentration of organic matter, organic carbon, N, P, lipids, soluble carbohydrates, and cell-wall fraction in three structures of O. glumaepatula (leaves and culm, adventitious roots, and basal roots), as well as to identify the possible differences in the allocation of these compounds between individuals in the natural and impacted areas. While the differences between the different structures of the plant are preliminary data for studies on the detritus chain and herbivory, the differences between the natural and impacted areas show the probable impact of the tailings on O. glumaepatula.     

Molecular mapping of soybean rust (Phakopsora pachyrhizi) resistance genes: discovery of a novel locus and alleles

Soybean production in South and North America has recently been threatened by the widespread dissemination of soybean rust (SBR) caused by the fungus Phakopsora pachyrhizi. Currently, chemical spray containing fungicides is the only effective method to control the disease. This strategy increases production costs and exposes the environment to higher levels of fungicides. As a first step towards the development of SBR resistant cultivars, we studied the genetic basis of SBR resistance in five F(2) populations derived from crossing the Brazilian-adapted susceptible cultivar CD 208 to each of five different plant introductions (PI 200487, PI 200526, PI 230970, PI 459025, PI 471904) carrying SBR-resistant genes (Rpp). Molecular mapping of SBR-resistance genes was performed in three of these PIs (PI 459025, PI 200526, PI 471904), and also in two other PIs (PI 200456 and 224270). The strategy mapped two genes present in PI 230970 and PI 459025, the original sources of Rpp2 and Rpp4, to linkage groups (LG) J and G, respectively. A new SBR resistance locus, rpp5 was mapped in the LG-N. Together, the genetic and molecular analysis suggested multiple alleles or closely linked genes that govern SBR resistance in soybean.     

Mitochondrial function in Parkinson's disease cybrids containing an nt2 neuron-like nuclear background

Mitochondria likely play a role in Parkinson's disease (PD) neurodegeneration. We modelled PD by creating cytoplasmic hybrid (cybrid) cell lines in which endogenous mitochondrial DNA (mtDNA) from PD or control subject platelets was expressed within human teratocarcinoma (NT2) cells previously depleted of endogenous mtDNA. Complex I activity was reduced in both PD cybrid lines and in the platelet mitochondria used to generate them. Under basal conditions PD cybrids had less ATP, more LDH release, depolarized mitochondria, less mitochondrial cytochrome c, and higher caspase 3 activity. Equivalent MPP+ exposures are more likely to trigger programmed cell death in PD cybrid cells than in control cybrid cells. Our data support a relatively upstream role for mitochondrial dysfunction in idiopathic PD.     

Macroinvertebrates associated with Chara in a tropical coastal lagoon (Imboassica lagoon,Rio de Janeiro,Brazil)

Imboassica lagoon is an urban coastal lagoon located in the municipality of Macaé (RJ), which has been exposed to a process of artificial eutrophication through the inflow of untreated sewage, as well as artificial openings of the sandbar that separates it from the ocean, provoking drastic modifications in this ecosystem. The sampling for the analysis of the community of macroinvertebrates associated with Charopyceae (Chara angolensis e C. fibrosa) were performed between October 1995 and October 1997, with a total of 9 samplings at two sampling stations: one located in the innermost area of the lagoon and another at the mouth of the main sewage channel, close to the sandbar. Throughout this period, four artificial sandbar-opening events were recorded, resulting in changes in the biomass of the macroalgae and in the densities of the macroinvertebrate populations. Through the analysis of the density of organisms per square meter, and density of organisms per 100 g dry weight of Chara, it was established that the biomass of the macroalgae has a direct influence on the density of the associated macrofauna. The greater development of the periphytic community in the area close to the inflow of sewage allows for the development of a community of macroinvertebrates with high densities, composed mainly of scraping organisms, such as the mollusc Heleobia australis (Hidrobiidae).     

Secondary productivity (3H-Leucine and 3H-Thymidine incorporation), abundance and biomass of the epiphytic bacteria attached to detritus of Typha domingensis pers. in a tropical coastal lagoon

Senescent, naturally dried leaves of Typha domingensis were incubated inthe littoral region of a coastal lagoon and epiphytic bacterial volume,abundance, biomass and secondary productivity were measured during 127 daysof decomposition. The peak of cell abundance was registered at t =127 days when expressed per leaf surface area (10.07×10⁷cells cm^-2; 7.26 µgC cm^-2), and at t= 26 days when expressed per biofilm dry mass (38.10 ×10⁷ cells (mgDM biofilm)^-1, 30.52 µgC(mgDM biofilm)^-1). The highest values of bacterial biovolumesand lower turnover time were usually obtained in the beginning of thecolonization. Leu:Tdr ratios were also higher in the beginning of thecolonization, when bacterial community presented unbalanced metabolism.Consequently, the highest discrepancies between the bacterial secondaryproduction estimated by leu and Tdr incorporation were observed in the first2 days of decomposition. On average, the bacterial secondary productivityestimated by leu incorporation was 2.1 times higher than the valuesestimated by Tdr incorporation when the empirical factor for Tdr wasobtained from the relationship between Tdr and biomass increment. Thisdifference increased to 4.2 when the empirical factor was obtained from therelationship between Tdr and cell numbers increment. An average of bothmethods (0.0037 to 0.1397 µgC cm^-2 h^-1)produced results that fall within the range reported in the literature forepiphytic bacteria of freshwater ecosystems.     

Effects of disturbance on phosphorus turnover and plankton dynamics

In coastal lagoons, one common type of anthropogenic disturbanceis opening of the sand barriers that isolate these lagoons fromthe sea. We investigated how a disturbance caused by an artificialopening of the sand barrier affects phytoplankton and bacterioplanktondynamics and alkaline phosphatase activities (APA) in a Braziliancoastal lagoon. We propose an index of potential phosphorusturnover time (PPTT) calculated as the ratio of total phosphorus(TP) and APA in an attempt to quantify the effect of disturbanceson phosphorus recycling within the plankton community. Openingthe barrier caused increased phytoplankton biomass, TP concentrations,APA and PPTT, and decreased bacteria to phytoplankton biomassratio. PPTT is easily calculated and may be used to detect planktonresponses to anthropogenic disturbances.