Search results for "Activity"
showing 10 items of 7178 documents
Revisiting delta-6 desaturase regulation by C18 unsaturated fatty acids, depending on the nutritional status.
2009
Dietary polyunsaturated fatty acids (PUFA) play a key role in regulating delta-6 desaturase (D6D), the key enzyme for long-chain PUFA biosynthesis. Nevertheless, the extent of their effects on this enzyme remains controversial and difficult to assess. It has been generally admitted that C18 unsaturated fatty acids (UFAs) regulate negatively delta-6 desaturase (D6D). This inhibition has been evidenced in regard to a high glucose/fat free (HG/FF) diet used in reference. However, several nutritional investigations did not evidence any inhibition of desaturases when feeding fatty acids. Because the choice of the basal diet appeared to be of primary importance in such experiments, our goal was t…
Herbicidally Active Derivatives of Aminomethylenebis-Phosphonic Acid-Mode of Action and Structure - Activity Relationship
1996
Abstract: (N-pyridylamino)methylenebisphosphonates exhibit strong herbicidal activity which may be reversed by supplementation of the growth media with aromatic amino acids. They appeare to be the inhibitors of aromatic amino acids biosynthesis acting as inhibitors of DAHP synthase the first enzyme of shikimate pathway. Over 40 analogues of these acids were synthesized in order to determine the structure-activity relationship.
Biological Activities of Natural Sesquiterpene Lactones and the Effect of Synthetic Sesquiterpene Derivatives on Insect Juvenile Hormone Biosynthesis
1998
Three natural sesquiterpene lactones have been assayed for their biological activity on locust (Locusta migratoria) nymphs. Since results obtained in vivo pointed to disruptions on juvenile hormone (JH)-regulated physiology, we tested the sesquiterpene lactones and a family of synthetic sesquiterpene derivatives for their ability to disturb the rate of JH biosynthesis by locust corpora allata (CA) in vitro. All the active compounds in vitro share a basic sesquiterpene double-ring structure as well as substituents with different chemical complexities. Compounds that shared an eudesmane base with different oxidation states on C3 and C12 carbon atoms were tested as JH biosynthesis inhibitors. …
On the biochemical classification of yeast trehalases: Candida albicans contains two enzymes with mixed features of neutral and acid trehalase activi…
2009
Abstract Two enzymes endowed with trehalase activity are present in Candida albicans . The cytosolic trehalase (Ntc1p), displayed high activity in exponential phase regardless of the carbon source (glucose, trehalose or glycerol). Ntc1p activity was similar in neutral (pH 7.1) or acid (pH 4.5) conditions, strongly inhibited by ATP, weakly stimulated by divalent cations (Ca 2+ or Mn 2+ ) and unaffected in the presence of cyclic AMP. The Ntc1p activity decreased in stationary phase, except in glycerol-grown cultures, but the catalytic properties did not change. In turn, the cell wall-linked trehalase (Atc1p) showed elevated activity in resting cells or in cultures growing on trehalose or glyc…
Mannosyl transferases inSaccharomyces cerevisiae: Evidence for the occurrence of ectomannosyltransferase activity
1981
The subcellular distribution of mannosyltransferases inSaccharomyces cerevisiae was studied following the separation of the plasma membrane from other intracellular membranous systems. Most of the activity was linked to internal membranes, and the rest was located at the level of the plasma membrane. Yeast plasma membranes coated on their external face with concanavalin A when incubated with GDP-[U-14C]mannose incorporated 20% less [U-14C]mannose in glycoproteins and 110% more in glycolipids than plasma membranes alone. This suggested that part of the total mannosyltransferase activity of the plasma membrane is located on its outer surface. A significant incorporation of radioactive mannose…
Novel Sortase A Inhibitors to Counteract Gram-Positive Bacterial Biofilms
2019
Sortase A (SrtA) is a membrane enzyme responsible for the covalent anchoring of surface proteins on the cell wall of Gram-positive bacteria. Nowadays it is considered an interesting target for the development of new anti-infective drugs which aim to interfere with important Gram-positive virulence mechanisms. Along the years, we studied the anti-staphylococcal and anti-biofilm activity of some natural and synthetic polyhalogenated pyrrolic compounds, called pyrrolomycins. Some of them were active on Gram-positive pathogens at a μg/mL range of concentration (1.5-0.045 μg/mL) and showed a biofilm inhibition in the range of 50-80%. [1-3] In light of these encouraging results, herein we present…
Novel Stilbene-Based Antileukemic Agents Active in P-Glycoprotein Expressing and Apoptosis-Resistant Acute Leukaemia Cell Lines.
2005
Abstract The stilbene scaffold is a basic element for a number of biologically active natural and synthetic compounds and in accordance with Evans’ definition it can be considered as a privileged structure. One of the most relevant and studied stilbenes is Resveratrol, a phytoalexin present in grapes, endowed with chemopreventive and chemotherapeutic properties and able to induce apoptosis in different cancer cell lines. Since reduced apoptosis has been implicated in the development and progression of malignant tumors and in the occurrence of chemoresistant phenotypes, resveratrol-induced apoptosis might therefore contribute to its antitumor activity. However, resveratrol is a not potent cy…
Endogenous Role of Microsomal Epoxide Hydrolase
2005
The specific activities of microsomal epoxide hydrolase with 16α,17α-epoxyandrosten-3-one (androstene oxide) as substrate were measured in various metabolically important and in various steroidogenic organs of the male and female rat and compared with the activities of 16α,17α-epoxyestratrienol (estroxide) and benzo[a]pyrene 4,5-oxide. Androstene oxide was an exceptionally good substrate. The specific activities differed widely between organs but the ratio of the activities towards these substrates was constant in all organs investigated. The ratios compared to benzo[a]pyrene 4,5-oxide were 2.5 for estroxide, and 8.6 for androstene oxide. The ontogenetic development of specific epoxide hydr…
Rollimembrin, a novel acetogenin inhibitor of mammalian mitochondrial complex I
1997
Abstract Rollimembrin (3), is a new adjacent bis-tetrahydrofuranic acetogenin with a scarce relative configuration, threo/cis/threo/cis/erythro, isolated from Rollinia membranacea seeds. The mechanism of cytotoxic activity, determined by NADH-oxidase experiments, establish that rollimembrin (3) is the most potent inhibitor of mammalian mitochondrial complex I.
Saponin with antibacterial activity from the roots of Albizia adianthifolia
2019
AbstractAn unprecedented saponin is being reported herein together with five known compounds from the methanol extract of the roots of Albizia adianthifolia. The metabolites were obtained over repe...