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Uptake Efficiency (uptake + efficiency)
Selected AbstractsNovel Guanidine-Containing Molecular Transporters Based on Lactose Scaffolds: Lipophilicity Effect on the Intracellular Organellar SelectivityCHEMISTRY - A EUROPEAN JOURNAL, Issue 30 2008Goutam Biswas Dr. Abstract We have synthesized two lactose-based molecular transporters, each containing seven guanidine residues attached to the lactose scaffold through ,-aminocarboxylate linker chains of two different lengths, and have examined their cellular uptakes and intracellular and organellar localizations in HeLa cells, as well as their tissue distributions in mice. Both molecular transporters showed higher cellular uptake efficiencies than Arg8, and wide tissue distributions including the brain. Mitochondrial localization is of special interest because of its potential relevance to "mitochondrial diseases". Interestingly, it has been found that the intracellular localization sites of the G7 molecular transporters,namely either mitochondria or lysosomes and endocytic vesicles,are largely determined by the linker chain lengths, or their associated lipophilicities. [source] PRECLINICAL STUDY: Effect of cannabinoids on platelet serotonin uptakeADDICTION BIOLOGY, Issue 2 2007Marie Velenovská ABSTRACT Serotonin is involved in many of the same processes affected by cannabinoids; therefore, we investigated in vitro and in vivo effects of these drugs on the function of serotonin transporter. The effect of ,9 -tetrahydrocannabinol (,9 -THC), endocannabinoid anandamide and synthetic cannabinoid receptor agonist WIN 55,212-2 on platelet serotonin uptake and membrane microviscosity was examined in 19 marijuana smokers and 20 controls. (1) Serotonin uptake was inhibited at higher doses of ,9 -THC (IC50 = 139 µmol/l), anandamide (IC50 = 201 µmol/l) or WIN 55,212-2 (IC50 = 17.4 µmol/l); the inhibition was found non-competitive. ,9 -THC, anandamide and WIN 55,212-2 produced different effects on the membrane microviscosity. (2) Maximal velocity of platelet serotonin uptake was significantly increased in a group of chronic marijuana smokers suffering impairment of cognitive functions when compared with controls. Opposite effect of marijuana smoking on the serotonin uptake efficiency was observed in males beside females. In summary, this study provides evidence that (1) Activity of serotonin transporter is acutely affected by cannabinoids at relatively high drug concentrations; this effect is indirect and can be partially accounted for the changes in the membrane microviscosity. (2) Increase of maximal velocity of the serotonin uptake could be understood as adaptation change in the serotonergic system induced by chronic cannabis use. A hypothesis was supported that lowered serotonin uptake may reflect a gender-related differences in effects of psychoactive cannabinoids. [source] In vitro Studies of Functionalized Mesoporous Silica Nanoparticles for Photodynamic TherapyADVANCED MATERIALS, Issue 2 2009Hsiung-Lin Tu A versatile platform for photodynamic therapy (PDT), mesoporous silica nanoparticles functionalized with protoporphyrin IX (PpIX-MSNs), has been developed. In vitro studies on HeLa cells show high uptake efficiency. Phototoxicity results give both irradiation time- and dosage-dependent cell death events. Because of the ease of incorporating other biomedical functional groups, we believe MSNs would be an ideal platform for biomedical applications. [source] Body Distribution of Poly- DL -lactide-poly(ethylene glycol) Microspheres with Entrapped Leptospira interrogans Antigens Following Intravenous and Oral Administration to Guinea-pigsJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 7 2000XIAOHONG LI Poly- DL -lactide-poly(ethylene glycol) (PELA) microspheres with entrapped antigens were administered intravenously and orally into guinea-pigs to quantitatively determine the in-vivo distribution and release profiles. PELA microspheres containing 125I-labelled outer-membrane protein Leptospira interrogans antigens (125I-OMP) were prepared by double-emulsion solvent extraction procedure, and characterized with respect to size, morphology and in-vitro release profiles. The fractured sections of liver and spleen were inspected by scanning electron microscopy, which indicated that microspheres had successfully been entrapped within the above tissues after intravenous injection and oral administration. At predetermined intervals, the blood and such tissues as the liver, spleen, kidney, thyroid, small intestine and mesentery were collected, and the radioactivity was measured by gamma scintillation counting. Following intravenous administration, 56.7% of administered microspheres were accumulated in immunization-related tissues, and 40.1% of microspheres were located in the liver and spleen. However, there was limited uptake efficiency (8.33%) following oral administration, and 49.5% of the absorbed microspheres were located in the intestinal mucosa. Compared with in-vitro release, the in-vivo release profiles of 125I-OMP from PELA microspheres, determined from the decreasing radioactivity in the above tissues, were much faster and the burst effect was higher. Antigen-loaded PELA microspheres were efficiently entrapped within immunization-related tissues after intravenous administration, but orally administered PELA microspheres showed limited uptake efficiency. Further investigation is needed to improve intestinal absorption. [source] Combined effects of arbuscular mycorrhizas and light on water uptake of the neotropical understory shrubs, Piper and PsychotriaNEW PHYTOLOGIST, Issue 2 2003Damond A. Kyllo Summary ,,Root hydraulic conductance (Kr) was measured for five understory shrub species of the neotropical moist forest to determine the effects of arbuscular mycorrhizas (AM) for both carbon-rich and carbon-limited host plants. ,,Kr was measured using a high pressure flow meter (HPFM) for potted plants grown in a factorial combination of AM fungi (presence/absence) and light (3.5 and 30% of full sun, low/high). ,,AM colonization improved Kr for the more shade-tolerant species plants when growing in low light. By contrast, water uptake efficiency of the light-demanding species was significantly decreased by AM fungi in high light. Regardless of AM colonization, light-demanding species had a lower capacity than shade-tolerant species to meet transpirational demands, and they allocated substantially more to fine root production relative to leaf area when colonized. ,,The differential effects of AM colonization and light on a species' root hydraulic conductance in relation to phylogeny and light adaptation demonstrate that AM fungi may be critical in determining early plant succession and community composition not only due to effects on nutrient uptake, but on water uptake as well. [source] Crops and genotypes differ in efficiency of potassium uptake and usePHYSIOLOGIA PLANTARUM, Issue 4 2008Zed Rengel Cultivars with increased efficiency of uptake and utilization of soil nutrients are likely to have positive environmental effects through reduced usage of chemicals in agriculture. This review assesses the available literature on differential uptake and utilization efficiency of K in farming systems. Large areas of agricultural land in the world are deficient in K (e.g. 3/4 of paddy soils in China, 2/3 of the wheatbelt in Southern Australia), with export in agricultural produce (especially hay) and leaching (especially in sandy soils) contributing to lowering of K content in the soil. The capacity of a genotype to grow and yield well in soils low in available K is K efficiency. Genotypic differences in efficiency of K uptake and utilization have been reported for all major economically important plants. The K-efficient phenotype is a complex one comprising a mixture of uptake and utilization efficiency mechanisms. Differential exudation of organic compounds to facilitate release of non-exchangeable K is one of the mechanisms of differential K uptake efficiency. Genotypes efficient in K uptake may have a larger surface area of contact between roots and soil and increased uptake at the root,soil interface to maintain a larger diffusive gradient towards roots. Better translocation of K into different organs, greater capacity to maintain cytosolic K+ concentration within optimal ranges and increased capacity to substitute Na+ for K+ are the main mechanisms underlying K utilization efficiency. Further breeding for increased K efficiency will be dependent on identification of suitable markers and compounding of efficiency mechanisms into locally adapted germplasm. [source] Optimal Conditions for Labelling of 3T3 Fibroblasts with Magnetoliposomes without Affecting Cellular ViabilityCHEMBIOCHEM, Issue 17 2007Stefaan J. H. Soenen Drs. Abstract A comparative study that deals with the internalisation of different types of magnetoliposomes (MLs) by 3T3 fibroblasts revealed that cationic MLs proved to be superior to neutral and anionic ones. Internalisation was visualised both by optical light and transmission electron microscopy. The latter showed that the cationic MLs ultimately ended up in lysosomal structures. The effect of increasing 1,2-dioleoyl-3-trimethylammonium propane (DOTAP) concentrations in the cationic ML coat has been elucidated. High uptake efficiency was only achieved with MLs that carry a high DOTAP payload. However, these structures also demonstrated toxic effects. The use of the saturated distearoyl analogue (DSTAP) at identical concentrations led to improved uptake efficiency and lower toxicity. By using iron-oxide-free vesicles, it was shown that the toxicity was due to lipid bilayer constituents and not the iron oxide. In conclusion, the use of DMPC,DSTAP (96.67:3.33; molar ratio) MLs results in an extremely high labelling of 3T3 fibroblasts with iron oxides (47.66 pg Fe per cell) without evoking any influence on cell viability. [source] | |||||||||||||