Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure-activity relationships

Piperazine and pyrrolidine derivatives were synthesised and evaluated for their capacity to inhibit the growth of Plasmodium falciparum chloroquine-resistant (FCR-3) strain in culture. The combined presence of a hydroxyl group, a propane chain and a fluor were shown to be crucial for the antiplasmodial activity. Five compounds of the aryl-alcohol series inhibited 50% of parasite growth at doses ?10 μM. The most active compound 1-(4-fluoronaphthyl)-3-[4-(4-nitro-2-trifluoromethylphenyl)piperazin-1-yl] propan-1-ol was almost 20–40 times more active on P. falciparum (IC₅₀: 0.5 μM) than on tumorogenic and non-tumorogenic cells. In vivo it has a very weak effect; inhibiting 35% of parasite growth only, at 10 mg/kg/day against Plasmodium berghei infected mice without any impact on survival time. In silico molecular docking study and molecular electrostatic potential calculation revealed that this compound bound to the active site of Plasmodium plasmepsin II enzyme.     

STUDIES IN THE PHYSICAL CHEMISTRY OF THE PROTEINS : VI. THE ACTIVITY COEFFICIENTS OF THE IONS IN CERTAIN OXYHEMOGLOBIN SOLUTIONS.

1. The solvent action of a neutral salt upon a protein, oxyhemoglobin, has been found identical to the solvent action of a neutral salt upon a bi-bivalent or uni-quadrivalent compound. 2. The solubility of oxyhemoglobin in phosphate solutions of varying ionic strength has been defined by the equation: log See PDF for Equation in which µ is the ionic strength, and S ₀ is the solubility in the absence of salt. 3. The values of S ₀ have been calculated to be 12.2, 11.2, and 13.1 gm. per liter respectively at pH 6.4, 6.6, and 6.8. 4. The relatively great solubility of oxyhemoglobin in water has been ascribed to the strong affinity constants for acid and base of certain groups in oxyhemoglobin. 5. The small change in the solubility of oxyhemoglobin effected by neutral salts suggests that but few such groups are dissociated in oxyhemoglobin in the state in which it crystallizes near its isoelectric point. 6. Certain of the other properties of oxyhemoglobin, such as its low viscosity, are considered in the light of its molecular weight and its valence type.     

Can water responses in Stipa tenacissima L. during the summer season be promoted by non-rainfall water gains in soil?

This article reports on quantified soil water gains and their possible effects on summer water relationships in a semiarid Stipa tenacissima L. grasslands located in SE Spain. We believe that the net soil water gains detected using minilysimeters could be from soil water vapour adsorption (WVA). Our study of high water-stress showed stomatal conductance (21.8–43.1 mmol H₂O m⁻² s⁻¹) in S. tenacissima leaves unusual for the summer season, and the evapotranspiration from S. tenacissima grassland, estimated by a multi-source sparse evapotranspiration model, closely corresponding to total WVA. This highlights the importance of summer soil WVA to stomatal conductance and vital transpiration in S. tenacissima. This study measured pre-dawn leaf water potential (ψ) response to sporadic light rainfall, finding that a light summer rainfall (1.59 mm day⁻¹) was sufficient to vary ψ in S. tenacissima from −3.8 (close to the turgour loss point) to −2.7 MPa. We hypothesize that soil WVA can supply vegetation with water vital to its survival in seasons with a severe water deficit, giving rise to a close relationship between soil water dynamics and plant water response.     

Patterns in size and shedding of Fasciola hepatica eggs by naturally and experimentally infected murid rodents

Using samples collected on the island of Corsica, a comparative study was done of the morphometry of Fasciola hepatica eggs shed by cattle and by naturally and experimentally infected murid rodents (wild Mus musculus and Rattus rattus and Rattus norvegicus Wistar laboratory strain). Eggs shed by murids are smaller in size than those shed by naturally infected cattle. A second study analyzed the number of F. hepatica eggs shed in murid feces at different time intervals, i.e., months, days, and 6-hr periods, by the Kato-Katz technique. Both experimentally and naturally infected black rats (R. rattus) were used, and Wistar rats were experimentally infected and included for comparison. The present studies prove that black rats R. rattus are able to shed eggs independently from the liver fluke isolate and that egg shedding occurs throughout the life of this host species, uninterrupted during all the months analyzed in a 2-yr period. Moreover, the results suggest that this shedding is continuous, with eggs appearing in the feces daily. The results on egg shedding by wild black rats R. rattus reach their maximum shedding in spring and autumn and a maximum during twilight hr. These chronobiological patterns appear to favor parasite transmission, both seasonally and daily.     

Oxidation of dibenzothiophene (DBT) by Serratia marcescens UCP 1549 formed biphenyl as final product

ABSTRACT: BACKGROUND: The desulphurization of dibenzothiophene (DBT), a recalcitrant thiophenic fossil fuel component by Serratia marcescens (UCP 1549) in order for reducing the sulphur content was investigated. The study was carried out establishing the growth profile using Luria Bertani medium to different concentrations of DBT during 120hours at 28oC, and orbital shaker at 150rpm. RESULTS: The results indicated that concentrations of DBT 0.5, 1.0 and 2.0 mM do not affected the growth of the bacterium. The DBT showed similar Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MCB) (3.68 mM). The desulphurization of DBT by S. marcescens was used with 96 hours of growth on 2mM of DBT, and was determined by gas chromatography (GC) and GC-mass spectrometry. In order to study the desulphurization process by S. marcescens was observed the presence of a sulfur-free product at 16 hours of cultivation The results show that S. marcescens oxidizes DBT to its corresponding DBT-5 oxide and then to DBT-sulfone, without the formation of any biphenyl. CONCLUSIONS: The data suggests the use of metabolic pathway "4S" by S. marcescens (UCP 1549) and formed biphenyl. The microbial desulphurization process by S. Serratia can be suggest significant reducing sulphur content in DBT, and showed promising potential for reduction of the sulfur content in diesel oil.     

Effects of ungulates on epigeal arthropods in Sierra Nevada National Park (southeast Spain)

This paper examines the effect of ungulates on epigeal arthropod communities in two common plant communities of the high mountains of the Sierra Nevada (southeast Spain). We have compared the abundance, biomass, diversity and specific composition of arthropod communities in grazed and ungrazed plots experimentally excluded from ungulates. In general, we found that arthropods were more abundant and diverse in grazed than in ungrazed plots. However, the effect of ungulates depended on the variable considered (diversity versus abundance versus biomass). Moreover, ungulates also affected species composition. This means that without affecting diversity, ungulates can still have a strong effect on arthropod communities by changing species composition. Also, the relationship between ungulates and arthropods differed depending on the year of study and the sampling period. In conclusion, our study indicates that to extrapolate the results obtained for a group of insects, a habitat or a sampling period is not appropriate for the conservation of arthropod communities.     

Biological pH sensing based on surface enhanced Raman scattering through a 2-aminothiophenol-silver probe

We report pH sensing for biological applications based on surface enhanced Raman scattering (SERS) from silver nanoparticles functionalized with 2-aminothiophenol (2-aminobenzenethiol, 2-ABT). pH-dependent SERS spectra of the attached 2-ABT molecules enable one to sense the pH over the range of 3.0-8.0. We have performed the first demonstration of SERS detection in living cells kept in different pH buffer solutions and show that the pH sensitivity is retained in that case. Thus, the nanoparticles can be used as probes delivering spatially localized chemical information from biological environments and provide a new way to monitor chemical changes at cellular level.