Search results for " activity"
showing 10 items of 4540 documents
“Click” on PLGA-PEG and hyaluronic acid: Gaining access to anti-leishmanial pentamidine bioconjugates
2017
Pentamidine (Pent), an antiparasitic drug used for the treatment of visceral leishmaniasis, has been modified with terminal azide groups and conjugated to two different polymer backbones (PLGA-PEG [PP] copolymer and hyaluronic acid [HA]) armed with alkyne end-groups. The conjugation has been performed by Copper Catalyzed Azido Alkyne Cycloaddition (CuAAC) using CuSO4 /sodium ascorbate as metal source. The novel PP-Pent and HA-Pent bioconjugates are proposed, respectively, as non-targeted and targeted drug delivery systems against Leishmania infections. Moreover, Pent has been encapsulated into PP nanoparticles by the oil-in-water emulsion method, with the aim to compare the biological activ…
Reciprocal Enzymatic Interference of Carnitine Palmitoyltransferase I and Glycerol-3-Phosphate Acyltransferase in Purified Liver Mitochondria
2006
(i) Highly purified mitochondrial fractions were practically devoid of microsomal contamination and of acyl-CoA ligase activity. (ii) In mitochondria, glycerol-3-phosphate acyltransferase (GPAT) activity was supported by two enzymes, the first being very active at low palmitoyl-CoA / albumin ratios and sensitive to external agents (external form), the second being detected only at higher palmitoyl-CoA / albumin ratios and insensitive to external agents (internal form). (iii) Carnitine palmitoyltransferase I (CPT I) activity was shown to inhibit external GPAT activity only. (iv) Glycerol-3-phosphate exerted an inhibitory effect on CPT I, even when GPAT was inactive. Reciprocal interaction of…
Role of Parenchymal Versus Non-Parenchymal Cells on the Control of Biologically Reactive Intermediates
1986
The non-parenchymal cells (NPC) of the liver have the potential to significantly influence the formation of reactive intermediates in the liver because of their critical location along the sinusoids where they are the first cells to encounter blood borne xenobiotics. To study the possible role of the NPC in the metabolism of xenobiotics, populations of NPC and parenchymal cells (PC) were prepared from rats and various xenobiotic metabolizing enzyme activities investigated. The specific activity of every enzyme studied was 12 to 1000% higher in the PC than in the NPC populations and the pattern of activities between the 2 populations was remarkably different. The NPC also displayed a more dr…
Novel Terphenyls and 3,5-Diaryl Isoxazole Derivatives Endowed with Growth Supporting and Antiapoptotic Properties
2008
A new study on terphenyl and diaryl-isoxazole and -isoxazoline derivatives, maintaining a common 3-adamantyl-4-hydroxyphenyl moiety, has been conducted to find compounds with growth supporting and antiapoptotic properties. Unexpectedly, diphenyisoxazole derivatives bearing a nitro group replacing the carboxylic function have been found with the highest cell protective activity within the series, in complete and in serum-free conditions. Inhibition of apoptosis induced by daunorubicin has also been observed for the most active compound.
Molecular and kinetic properties of lactate dehydrogenase in the degenerating peripheral nerve
1966
Abstract Electrophoretic and catalytic studies have been carried out on lactate dehydrogenase of normal and transected sciatic nerves of the rat. Lactate dehydrogenase of the intact nerve exhibits an almost even distribution of activity among its component iso-enzymes. The complete transection of the nerve is responsible for a deep and immediate shift of the enzyme towards the so-called muscle type pattern. Seven days after the nerve section the percentage activity of iso-enzyme 5 is almost three times higher than in the intact nerve. After a short lag period lactate dehydrogenase specific activity (activity/mg protein) undergoes a sharp decrease in transected nerves. The return of the elec…
Biological effects of short-chain fatty acids in nonruminant mammals.
1993
propionate, volatile fatty acids (VFAs), cholesterol, cell prolifera tion, human gastric lipase
Staphylococcal NreB: an O2-sensing histidine protein kinase with an O2-labile iron-sulphur cluster of the FNR type
2004
Summary The nreABC ( n itrogen re gulation) operon encodes a new staphylococcal two-component regulatory sys- tem that controls dissimilatory nitrate/nitrite reduc- tion in response to oxygen. Unlike other two- component sensors NreB is a cytosolic protein with four N-terminal cysteine residues. It was shown that both the NreB-cysteine cluster and Fe ions are required for function. Isolated NreB was converted to the active form by incubation with cysteine desul- phurase, ferrous ions and cysteine. This activation is typical for FeS-containing proteins and was reversed by oxygen. During reconstitution an absorption band at 420 nm and a yellow-brownish colour (typical for an FNR-type iron-sul…
Anti-/Pro-Oxidant Behavior of Naturally Occurring Molecules in Polymers and Biopolymers: A Brief Review
2019
Polymers and biopolymers are continuously subjected to the action of different stress factors, such as oxygen, heat, UV light, mechanical stress, humidity, etc., during their processing and service life, undergoing overall oxidative degradation, that causes performance and property deterioration. To improve the resistance at high temperatures and long-term weatherability of the polymers and biopolymers, usually, during their manufacturing, synthetic antioxidants and UV-light stabilizers are added. In the past decade, several concerns related to the impact of the synthetic stabilizers have emerged, and to reduce their negative effect on human health and the environment, their replacement wit…
Localization and Activity of a Carboxypeptidase in Germinating Seeds of Scots Pine, Pinus sylvestris
1976
Extracts prepared from the endosperm of germinating seeds of Scots pine, Pinus sylvestris L., hydrolysed two typical carboxypeptidase substrates, Z-Phe-Ala and Z-Phe-Phe, with pH optima at 4.2 and 5.0. The activities were completely destroyed by diisopropylfluorophosphate. Identical heat inactivation curves and elution patterns in gel chromatography on Sephadex G-200 suggest that the two activities are due to a single enzyme. In resting seeds very low carboxypeptidase activity was present in both the endosperm and the embryo. During germination on agar gel at 20°C in the dark the activities, expressed as enzyme units per seed, increased in the seedling and particularly in the endosperm up t…
Antioxidation and the Hypoxic Ventilatory Response
2012
Reactive oxygen species favor the reductive state of iron. Antioxidation, by depleting biologically active ferrous iron, could then have a stabilizing effect, akin to hypoxia, on HIF-1α; the process which controls the genetic responses to hypoxia. However, the influence of antioxidation on the hypoxic ventilatory responses (HVR) is unclear. In this study we set out to determine the influence of mangiferin, a natural polyphenolic compound present in mango trees, with strong antioxidant and iron chelating properties, on the HVR. The study was performed in awake Wistar rats. Acute HVR to 12% and 8% FiO2 before and 40 min after mangiferin (300 mg/kg, i.p.) pretreatment were recorded plethysmogr…