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Chloroquine is still the antimalarial drug which is the most utilized. Nevertheless the molecular mode of action of this drug is not very well understood. When mouse erythrocytes injected with Plasmodium berghei are exposed to chloroquine, the first biochemical event is rapid accumulation of the drug. This process is energy dependent, saturable and competively inhibited by drugs of the same therapeutic class (Quinine, Amodiaquine, Mefloquine). Receptors for chloroquine have been proposed for the process of accumulation. The nature of the chloroquine receptor is presently the subject of debates. The latest hypothesis proposed by Chou and coll. [12], is that ferriprotoporphyrin IX, formed by the degradation of hemoglobin by the parasite, binds to chloroquine with a dissociation constant of 3.5.10−9 M. We studied here the molecular interactions between these two species by Proton Nuclear Magnetic Resonance in order to elucidate the nature and the geometry of were undertaken.The perturbations of the NMR spectra of chloroquine (10−2 M) induced by addition of hematin or hemin were measured. Two types of measures were indertaken.The first study carried out in organic solvent (DMSO) has shown that the interaction occured between the acidic functions of hemin and the sidechain nitrogen of chloroquine. The iron atom was not implicated in this process.The second study carried out in aqueous medium (phosphate buffer; 0.1 M; pH = 7) allowed us to demonstrate that chloroquine is able to intercalate into a polymer of hematin. The quinoleic nucleus of chloroquine was intercalated between two dimers of hematin as shown by the broadening of the signal of the quinoleic protons due to very large increase in the correlation time.Finally it was shown that chloroquine is associated as a dimer in aqueous medium by hydrophobic interactions. The association constant is 5.5 M−1. 相似文献
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Nicole Raynaud Brigitte Moreteau Nicole Chaminade et Gérard Nicolas 《Entomologia Experimentalis et Applicata》1985,39(1):43-46
Un apport unique de 10 g d'hormone juvénile 1, réalisé chez des criquets du dernier stade larvaire à corpora allata intacts ou préalablement soumis à une application de precocène 2, provoque, à la mue suivante, l'apparition d'individus dont les caractéristiques sont intermédiaires entre celles du dernier stade larvaire et celles de l'imago. Cependant, les criquets traités par le précocène 2 présentent des variations phénotypiques plus prononcées, se traduisant par un maintien accru des caractéristiques larvaires. Les études ultrastructurales montrent que les corpora allata dégénèrent rapidement sous l'action des 400 g de précocène 2.
Summary In fifth instar locusts, with intact corpora allata or previously subjected to precocene 2 action, a single injection of 10 g juvenile hormone 1 leads, at the next molt, to the appearance of individuals displaying characters ranging from the typical larval to the typical imaginal ones. But, unexpectedly, the phenotypic variations are more marked in the precocene 2 treated locusts, and are typified by an increased retention of larval characters. Electron microscopic studies indicate that the use of 400 g of precocene 2 rapidly leads to the degeneration of the corpora allata.相似文献
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Pierre Fradette Edwin Bourget 《Journal of experimental marine biology and ecology》1981,50(2-3):133-152
Forty-seven navigation buoys were used to collect quantitative samples of epibenthic fauna in the Lower Estuary and Gulf of St. Lawrence. Stations, as described by their sessile species and biomass composition, were grouped using multivariate analysis. A Gower similarity index, modified to take into account the importance of each species in the ecosystem, was used to compare stations. Results obtained by cluster and principal coordinate analyses showed comparable relations between stations. North Shore and Gaspé Coast stations were separated from those of the Lower North Shore, the Mingan Island sector and the Lower Estuary. Stations from the Lower North Shore were also separated from those of the Mingan Island region and of the Lower Estuary, but at a higher level of similarity. All animal assemblages consisted of the following sessile species: Obelia longissima (Pallas), Hiatella arctica (L.), Mytilus edulis L., Balanus balanoides (L.) and B. crenatus (Bruguière). These species formed over 95% of biomass of all sessile species. Differences between the various station assemblages were mainly due to changes in the relative abundance of these species. The geographical gradient of summer surface water temperature best explains the observed clusters. In the Lower Estuary, the spatio-temporal variations of physico-chemical factors and the surface circulation may influence the number of species and their abundance. The circulation systems of the Lower Estuary and near the Mingan Islands might account for the similarity between their assemblages. The same dominant species, Obelia longissima, characterizes the fauna of these two regions. 相似文献
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Résumé L'analyse (acides aminés et sucres) d'extrait de feuille, de 5 variétés de manioc (Manihot esculenta), du Faux caoutchouc (Hybride deM. esculenta x M.glaziovii), du Poinsettia (Euphorbia pulcherrina) et du Talinum (Talinum triangularae), caractérisés par différents degrés de résistance par antibiose à la cochenille du manioc (Phenacoccus manihoti (Mat. Ferr.)) (Homoptera: Pseudococcidae), a été réalisée sur des extraits obtenus par centrifugation du matériel foliaire. Les teneurs en acids aminés, très différentes d'une plante à l'autre, apparaissent aussi importantes entre les variétés de l'espèce manioc qu'entre les différentes espèces végétales avec respectivement un rapport de variation de 4,5 et 5,5. De même, les teneurs en sucres (exprimées en équivalent saccharose), sont très différentes d'une plante à l'autre avec un rapport de variation de 1 à 33 entre les deux extrêmes, si l'on ne considère que l'espèceM. esculenta, il n'est plus que de 3,5.Des différences dans les proportions relatives des acids aminés libres d'extrait de feuille sont observées aussi bien entre les variétés de manioc qu'entre les espèces végétales. Cependant pour toutes les plantes étudiées l'acide glutamique, la glutamine, l'ethanolamine, et l'alanine représentent près de 50% des acides aminés de l'extrait de feuille; l'acide aspertique, l'asparagine et la sérine près de 20% tandis que la tyrosine, la méthionine, l'isoleucine, la leucine et la lysine sont présents en très faibles pourcentages.Le degré de résistance à la cochenille du manioc des différentes plantes-hôtes n'a pu être relié, ni à la teneur de leur extrait de feuille en acides aminés et en sucres, ni à leur composition relative en acides aminés. Il n'a pu être non plus relié au rapport Sucres/Acides aminés Nos résultats suggèrent que des caractéristiques biochimiques autres que celles étudiées dans ce travail interviennent dans les mécanismes de résistance vis-à-vis de la cochenille du manioc.
Summary The levels of sugars and amino acids were determined in leaf extracts from a number of plants showing different levels of resistance to the cassava mealybug,Phenacoccus manihoti (Homoptera: Pseudococcidae). There were five varieties of cassava (Manihot esculenta), as well as a hybrid obtained by crossingM. esculenta andM. glaziovii, poinsettia (Euphorbia pulcherrina) and talinum (Talinum triangularae). The variability in the total concentration of amino acid concentrations was as great between varieties of cassava as at the species level. In contrast, there was much less variability in the concentration of sugars at the intervarietal that at the interspecies level.While there were both intervarietal and interspecific differences in the amino acid composition, glutamic acid, glutamine, ethanolamine and alanine represented nearly 50% of the total in all plants examined. Aspartic acid, asparagine and serine accounted for approximately 20%, while tyrosine, methionine, isoleucine, leucine and lysine are present at low levels.The different levels of resistance noted in the different plants were not associated with the concentrations of either amino acids or sugars, the ratios of sugar/amino concentrations or the amino acid compositions obtained from leaf extracts. This suggests that other aspects of plant chemistry confer resistance to cassava mealybugs.相似文献
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D-glucose specifically deuterated at C-6 was prepared and used for the biosynthesis of bacterial cellulose with Acetobacter xylinum. The material obtained was converted into glucitol hexaacetate and analyzed by 250 MHz n.m.r. and mass spectrometry. These spectra indicated that about 70% of the starting D-glucose was incorporated without modification of deuteriation at the C-6 position. However an explanation is required of the finding that deuterium was also incorporated at the C-2 and C-1 positions of the cellulose, arising respectively from the 6 pro-R and 6 pro-S positions of the initial D-glucose. 相似文献
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As a preliminary to the study of the metabolism of erucic acid by beating heart cells of post natal rats in culture, the activity of lipoprotein lipase and the oxidation of palmitic acid have been studied. The results have led us to use 14 day cultures as the material of choice for experiments on the incorporation of erucic acid into cardiac cells, and on its subsequent distribution into different classes of lipid. Work on fatty acid oxidation has been carried out on 5–8 day cultures.We have shown that erucic acid enters cardiac muscle cells, but that the cells are not capable of oxidizing it directly.We have suggested two independent mechanisms by which this is done, namely shortening of the chain followed by the complete utilization of this smaller molecules by β-oxidation. The delay which this implies would explain the accumulation of erucic acid in the heart cells.We have also proposed that the accumulation of large quantities of erucic acid in phospholipids and esters of cholesterol may modify the structure of cellular and mitochondrial membranes, thus explaining the pathological effects of erucic acid. 相似文献
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Denise Viale 《Journal of experimental marine biology and ecology》1979,40(3):201-221
Up to the present there was not believed to be any excretion in the skin of cetaceans because of the absence of sweat and sebaceous glands. It has now been shown that concentrated salty excretion is produced in various cetaceans by numerous epidermal cells dispersed in the whole epidermis. They are not aggregated into glands. Other epidermal cells, likewise scattered in the epidermis, synthetize lipids; this function seems homologous to the sebaceous function of other mammals. 相似文献
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The study of polyelectrolytes in solution by small-angle x-ray scattering techniques involves special problems, raised by the presence of several species: solvent, macroions, counterions, and possibly the ions of an additional electrolyte. A theoretical treatment of this problem is developed, based upon geometric concepts; the treatment applies to globular and to rodlike particles for the case of x-ray experiments carried out on an absolute scale. The equation obtained involves several parameters: mass and radius of gyration for globular particles; mass per unit length and axial radius of gyration for rodlike particles; partial specific volumes of the neutral macromolecular component of the counterions and of the added electrolyte; solvation of the macromolecular species; fraction of the counterions osmotically free. The equation is used to interpret a series of experiments performed with the Li, Na, and Cs salts of DNA in solution in water containing variable amounts of the chlorides of each cation. The effects of concentration are first eliminated by extrapolating to infinite dilution the experiments carried out at different concentrations; then the effects of the solvation are eliminated by extrapolating to pure water the results obtained at different electrolyte concentration. The parameters still involved at this stage are the mass per unit length, the partial specific volumes of the DNA and of the counterions, and the fraction of the counterions osmotically free. If the partial specific volumes are chosen in agreement with other data of the literature, and if the fraction of the counterions osmotically free is assumed to be 0.30 for the three salts, as suggested by other workers, the structure of the DNA molecules turns out to be the same for three cations, and to agree with the Watson-Crick model. These results are confirmed by the study of the liquid–crystalline gels, obtained at higher concentration, that lead to a direct determination of the mass per unit length of the rods. Moreover the solvation of the DNA molecules is determined as is shown to be different for each of the three cations. These results are in excellent agreement with those obtained by other techniques. 相似文献
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Glycerol specifically deuterated at C-1, C-2, or C-3 was prepared and used for the biosynthesis of bacterial cellulose with Acetobacter xylinum.The material obtained were converted into glucitol hexaacetate and analyzed by 250-MHz nuclear magnetic resonance and mass spectrometry. The spectra indicated that the protons of the C-3 position of the starting glycerol were incorporated as substituents of the C-6 and C-1 positions of the cellulose. Similarly, protons of the C-2 and C-5 positions of the cellulose came essentially from water and the protons bonded at the C-3 and C-4 positions of the cellulose from protons bonded to C-1 of the starting glycerol. 相似文献
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B. Frérot M. Renou C. Malosse et C. Descoins 《Entomologia Experimentalis et Applicata》1988,46(3):281-289
Les analyses physico-chimiques d'extraits hexaniques de glandes à phéromone de femelles vierges de T. jacobaeae, associées à des études du comportement sexuel et à l'électroantennographie, ont permis d'identifier le composé majoritaire (98%) comme étant l'époxy-9S,10R-(Cis)-hénéicosadiène-3Z,6Z (no 1) et de déterminer sa configuration absolue. Les analogies entre les spectres du composé no 2 (1,5%) et ceux de l'époxy-9S,10R éicosadiène-3Z,6Z de synthèse nous conduisent à proposer cette structure pour ce constituant minoritaire. Le troisième produit (0,5%) possède les caractéristiques physico-chimiques de l'hénéicosatriène-3Z,6Z,9Z (no 3). Les produits 1 et 3 ont déjà été identifiés comme constituants de phéromones d'Arctiidae tandis que le produit 2 est décrit ici pour la première fois dans une sécrétion phéromonale de Lépidoptère. 相似文献
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Patrick Masson Philippe Vallin 《Journal of chromatography. B, Analytical technologies in the biomedical and life sciences》1983,273(2)
Affinity electrophoresis has been applied to the study of the multiple molecular forms of three human plasma cholinesterase phenotypes (usual enzyme U, atypical enzyme A and intermediate UA). Electrophoreses were carried out in polyacrylamide gels containing a water-soluble macromolecular derivative of m-amino-(substituted)-phenyltrimethylammonium immobilized within the gel network.Apparent dissociation constants (KD app) were estimated from the mobilities of the enzymes versus ligand concentration.The ratio of KD app values of the molecular forms of phenotypes A and U which is approximately 2 is consistent with the hypothesis that the anionic site is altered in atypical enzyme. 相似文献