Semisynthesis and pharmacological investigation of lipo-alkaloids prepared from aconitine

Processed aconite drugs are widely used in Eastern medicine as painkillers and antirheumatic agents. It is known that the traditional processing of aconite drugs increases the amount of lipo-alkaloids. In order to obtain information about the pharmacological potential of these compounds, semisynthesis of 9 aconitine-derived lipo-alkaloids was carried out and their COX-1, COX-2 and LTB₄ formation inhibitory activities were investigated. It was found that compounds esterified with unsaturated fatty acids demonstrated significant COX-2 inhibitory effects, while in the COX-1 assay only 14-benzoylaconine-8-O-eicosapentaenoate exerted remarkable activity. The inhibition of LTB₄ formation was pronounced in cases of long chain fatty acid derivatives.     

Characterization of suspended particulate matter in the Moselle River (Lorraine,France): evolution along the course of the river and in different hydrologic regimes

Purpose

Suspended particulate matter (SPM) plays an important role in the transport and fate of contaminants in the environment. To better understand the relationships between contaminants and SPM, SPM properties, and their variations with flow regime, river size, land use, and season should be considered.

Materials and methods

The grain size distribution, elemental composition, and mineralogy of SPM from different stations along the Moselle River (Lorraine, France) were investigated at the particle scale during different flow regimes. The resulting data were compared with the elemental composition of the dissolved compartment to understand the role of particles in element transport.

Results and discussion

The grain size distribution, elemental composition, and mineralogy of SPM along the Moselle River and during different flow regimes showed only slight variations, except for the Fensch and Orne tributaries, two rivers that were impacted by inherited steel-making industrialization and different land use. In the Moselle River, SPM mainly consisted of clay minerals, while in Fensch and Orne Rivers, SPM mainly consisted of multiple types of anthropogenic particles. The diffuse urbanization gradient was hardly recognized based on the Trace Metal Element (TMEs) content in the river SPM, while the rivers impacted by the steel industries had greater TME contents. Finally, the TME content in the Moselle SPM was more strongly influenced by water flow than by the position of sampling on the linear reach of the Moselle River. The partitioning of TMEs in the particles and water at the main Moselle station (Frouard) revealed that SPM predominantly contributed to TMEs transport.

Conclusions

This study confirmed that catchment geology greatly contributed to the SPM composition in the mean-sized rivers. In addition, the high anthropogenic pressure could be deciphered for small tributaries. Furthermore, this study allowed us to observe the high contribution of particles to TMEs and Rare Earth Element (REEs) transportation.

     

Occurrence of zearalenone-4-beta-D-glucopyranoside in wheat

An LC-MS method was developed for the analysis of zearalenone-4-beta-D-glucopyranoside and zearalenone in wheat (Triticum aestivum). The limit of determination for zearalenone-4-beta-D-glucopyranoside and zearalenone was 10 microg/kg. The recovery rates were calculated to be 69% and 89% at a concentration of 100 microg/kg for zearalenone-4-beta-D-glucopyranoside and zearalenone, respectively. Twenty-four Bavarian wheat samples from a 1999 harvest were analyzed. Zearalenone was present in 22 of 24 field samples, the levels ranged from 11 to 860 microg/kg. Zearalenone-4-beta-D-glucopyranoside was found in 10 of the zearalenone positive samples (42%) at levels ranging from 17 to 104 microg/kg. The amounts of zearalenone-4-beta-D-glucopyranoside were correlated to those of zearalenone (r2 = 0.86, b = 0.10). After gastrointestinal hydrolyzation, zearalenone-4-beta-glucopyranoside might be implicated in the development of a zearalenone-syndrome. Therefore, more attention should be focused on conjugated mycotoxins in food and feed.     

HST and VLT investigations of the fragments of comet C/1999 S4 (LINEAR)

At least 16 fragments were detected in images of comet C/1999 S4 (LINEAR) taken on 5 August 2000 with the Hubble Space Telescope (HST) and on 6 August with the Very Large Telescope (VLT). Photometric analysis of the fragments indicates that the largest ones have effective spherical diameters of about 100 meters, which implies that the total mass in the observed fragments was about 2 x 10(9) kilograms. The comet's dust tail, which was the most prominent optical feature in August, was produced during a major fragmentation event, whose activity peaked on UT 22.8 +/- 0.2 July 2000. The mass of small particles (diameters less than about 230 micrometers) in the tail was about 4 x 10(8) kilograms, which is comparable to the mass contained in a large fragment and to the total mass lost from water sublimation after 21 July 2000 (about 3 x 10(8) kilograms). HST spectroscopic observations during 5 and 6 July 2000 demonstrate that the nucleus contained little carbon monoxide ice (ratio of carbon monoxide to water is less than or equal to 0.4%), which suggests that this volatile species did not play a role in the fragmentation of C/1999 S4 (LINEAR).     

Diminished response of Werner's syndrome fibroblasts to growth factors PDGF and FGF

Patients with Werner's syndrome, an autosomal recessive disorder, undergo an accelerated aging process that leads to premature death. Fibroblasts from such patients typically grow poorly in culture. Here it is shown that fibroblasts from a patient with Werner's syndrome have a markedly attenuated mitogenic response to platelet-derived growth factor (PDGF) and fibroblast growth factor (FGF). In contrast, they have a full mitogenic response to fetal bovine serum. Both PDGF binding and receptor numbers per cell are unaltered. The Werner's syndrome cells express high constitutive levels of collagenase in vitro. Although PDGF enhances collagenase expression through increased levels of hybridizable collagenase messenger RNA in normal skin fibroblasts, no induction of collagenase occurs in the Werner's syndrome fibroblasts. Moreover, the failure to respond to this agonist effect of PDGF is not restored by fetal bovine serum. The data suggest that failure of one or more PDGF-mediated pathways in Werner's syndrome cells may contribute to the phenotypic expression of the disorder.     

Vascular smooth muscle: aerobic glycolysis linked to sodium and potassium transport processes

Under aerobic conditions, glucose is primarily catabolized by vascular smooth muscle to lactate, in spite of an adequate oxidative capacity. Although this is often considered to be indicative of some nonspecific metabolic insufficiency, there is evidence that aerobic glycolysis is specifically coupled to sodium and potassium transport processes, whereas oxidative metabolism is couple to contracticle energy requirements.     

Ionosphere of venus: first observations of the effects of dynamics on the dayside ion composition

Bennett radio-frequency ion mass spectrometers have returned the first in situ measurements of the Venus dayside ion composition, including evidence of pronounced structural variability resulting from a dynamic interaction with the solar wind. The ionospheric envelope, dominated above 200 kilometers by O(+), responds dramatically to variations in the solar wind pressure, Which is observed to compress the thermal ion distributions from heights as great as 1800 kilometers inward to 280 kilometers. At the thermal ion boundary, or ionopause, the ambient ions are swept away by the solar wind, such that a zone of accelerated suprathermnal plasma is encountered. At higher altitudes, extending outward on some orbits for thousands of kilometers to the bows shock, energetic ion currents are detected, apparently originating from the shocked solar wind plasma. Within the ionosphere, observations of pass-to-pass differences in the ion scale heights are indicative of the effects of ion convection stimlulated by the solar wind interaction.     

DNA rearrangement and altered RNA expression of the c-myb oncogene in mouse plasmacytoid lymphosarcomas

Three types of tumors termed plasmacytomas (ABPC's), lymphosarcomas (ABLS's), and plasmacytoid lymphosarcomas (ABPL's) arise in BALB/c mice treated with pristane and Abelson murine leukemia virus (A-MuLV). While most ABPC's and BLS's contain integrated A-MuLV proviral genome and synthesize the v-abl RNA, most ABPL's do not. The ABPL tumors were examined for the expression of other oncogenes that may be associated with their transformed state, in the absence of transforming virus. These tumors expressed abundant c-myb RNA of unusually large size and showed DNA rearrangements of the c-myb locus.