Search results for "acids"
showing 10 items of 3520 documents
Core-shell functionalized zirconium-pemetrexed coordination nanoparticles as carriers with a high drug content
2019
Selected drug molecules with Lewis base functions can be assembled into coordinative nanoparticles (NPs) by linking them with suitable metal ions. Such nanomaterials exhibit a high material economy due to high drug contents and minor amounts of inactive additives. The antifolate pemetrexed (PMX) which is used for the treatment of lung cancers contains two carboxy functions that are able to undergo coordinative binding of metal ions. This study presents the development of a multilayer PMX NP system where each layer serves a distinct purpose. The metal-drug NP core is assembled in a bottom-up approach by coordinative interactions between zirconium (IV) ions and PMX molecules. Since the NP cor…
Up-regulation of cholesterol associated genes as novel resistance mechanism in glioblastoma cells in response to archazolid B
2014
Treatment of glioblastoma multiforme (GBM), the most common and aggressive lethal brain tumor, represents a great challenge. Despite decades of research, the survival prognosis of GBM patients is unfavorable and more effective therapeutics are sorely required. Archazolid B, a potent vacuolar H(+)-ATPase inhibitor influencing cellular pH values, is a promising new compound exerting cytotoxicity in the nanomolar range on wild-type U87MG glioblastoma cells and U87MG.∆EGFR cells transfected with a mutant epidermal growth factor receptor (EGFR) gene. Gene expression profiling using microarray technology showed that archazolid B caused drastic disturbances in cholesterol homeostasis. Cholesterol,…
Eight-week consumption of milk enriched with omega 3 fatty acids raises their blood concentrations yet does not affect lipids and cardiovascular dise…
2014
Adequate concentrations of omega 3 fatty acids (FA) may be maintained by consuming foods naturally rich in or functional foods enriched with those essential FA. We assessed the effects of an 8-week consumption of milk enriched with 400. mg of omega 3 FA on blood lipid levels and selected cardiovascular risk factors in adult healthy volunteers. Participants (n= 157) were randomized to consume - for eight weeks - either 500. mL/day of 1% fat milk providing 150. mg of eicosapentaenoic (EPA), 150. mg of docosahexaenoic (DHA), and 100. mg of α-linolenic (ALA) acids or 500. mL/day of non-enriched 1% fat milk. At week 8, we observed significant increments of blood EPA and DHA in the intervention g…
Über die Wirkung von Prostaglandin E1 auf den Ca-Haushalt isolierter Meerschweinchenherzen
1967
The stimulatory effect of PGE1 on different functions of isolated guinea-pig hearts (Langendorff method, Tyrode solution) was coupled with an increase in the rate of45Ca uptake from the perfusion medium. The total myocardial Ca content and the amount of exchangeable cellular Ca were not affected. This action of PGE1 on the myocardial Ca metabolism seems to be related to the positive inotropic action of PGE1 and can most probably be explained by an increase in the membrane permeability to Ca ions (similar to the action of epinephrine).
Phenylalanine Hydroxylase Participation in the Synthesis of Serotonin and Pteridines in Drosophila melanogaster
1997
Abstract Phenylalanine hydroxylase is involved in the synthesis of serotonin and pteridines, probably catalysing the hydroxylation of tryptophan and a tetrahydropterin oxidase reaction, respectively. Supplementation of the wild-type Drosophila diet with either L-Phe or L-Trp induced a significant increase in the phenylalanine hydroxylase concentration, while L-Tyr supplementation had no effect. The level of serotonin in adult heads of the PAH-defective mutant Henna recessive-3 was significantly lower than that obtained for the wild-type strain. A 4-fold increase in the concentration of phenylalanine hydroxylase is observed during the pharate adult head development. It occurs in parallel wit…
Hepatic steatosis and peroxisomal fatty acid beta-oxidation.
2012
Three subhepatocellular compartments concur for fatty acids degradation including ω-oxidation in endoplasmic reticulum and β-oxidation in both mitochondria and peroxisomes. Deficits affecting the peroxisomal physiology may be associated with multiple metabolic disturbances. Nowadays, a growing body of evidence underlines the key role of peroxisomal β-oxidation in the sensing of lipid metabolism through the production/degradation of some essential metabolites. Lessons from several mice models strengthen the link between fatty acid β-oxidation in peroxisomes and the nuclear hormone receptor Peroxisome Proliferator-Activated Receptor (PPAR)-α with an additional level of coregualtor complexity,…
Differential incorporation of labeled amino acids in the territories of the sea urchin blastula
1962
Blastule con mesenchima primario diParacentrotus lividus esposte a un trattamento di 30 min con S35-metionina, leucina-C14 e alanina-C14 mostrano nel territorio vegetativo una densita di tracce considerevolmente minore che in quello animale. Se gli embrioni sono invece esposti all'aminoacido radioattivo durante tutto lo sviluppo o durante le prime ore dopo la fecondazione, tale differenza tra territori animale e vegetativo non si osserva. Si discute il significato di questi reperti.
PPARα/HNF4α Interplay on Diversified Responsive Elements. Relevance in the Regulation of Liver Peroxisomal Fatty Acid Catabolism
2012
In mammals, the liver is the major organ of fatty acid catabolism. This pathway is involved in both mitochondria and peroxisome. While mitochondria breaks down fatty acids with short, medium and long carbon chains, peroxisomes are involved in the catabolism of very long and branched chain fatty acids, which are degraded by three enzymes: acyl-CoA oxidase, multifunctional enzyme and thiolase enzyme. The active pathway results mainly from a tight transcriptional control of these gene-encoding enzymes. Two major nuclear receptors that are highly expressed in this organ are involved in this control, e.g. PPARα (peroxisome proliferator-activated receptor, α isoform) and HNF4α (hepatic nuclear fa…
Toward the Discovery of New Agents Able to Inhibit the Expression of Microsomal Prostaglandin E Synthase-1 Enzyme as Promising Tools in Drug Developm…
2010
In our recent studies, we focused our attention on the synthesis of several γ-hydroxybutenolides designed on the basis of petrosaspongiolide M 1 (PM) structure that has been recognized to potently inhibit the inflammatory process through the selective PLA2 enzyme inhibition. By means of a combination of computational methods and efficient synthetic strategies, we generated small collections of PM modified analogs to identify new potent PLA2 inhibitors, suitable for clinical development. In the course of the biological screening of our compounds, we discovered a potent and selective inhibitor of mPGES-1 expression, the benzothiophene γ-hydroxybutenolide 2, which so far represents the only pr…
Docosahexaenoic acid and other fatty acids induce a decrease in pHiin Jurkat T-cells
2003
Docosahexaenoic acid (DHA) induced rapid (t1/2=33 s) and dose-dependent decreases in pHi in BCECF-loaded human (Jurkat) T-cells. Addition of 5-(N,N-dimethyl)-amiloride, an inhibitor of Na+/H+ exchanger, prolonged DHA-induced acidification as a function of time, indicating that the exchanger is implicated in pHi recovery. Other fatty acids like oleic acid, arachidonic acid, eicosapentaenoic acid, but not palmitic acid, also induced a fall in pHi in these cells. To assess the role of calcium in the DHA-induced acidification, we conducted experiments in Ca2+-free (0% Ca2+) and Ca2+-containing (100% Ca2+) buffer. We observed that there was no difference in the degree of DHA-induced transient ac…