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At least 73 records · Page 4Linked to original sources
PubMed1975

Lipogenesis and glyceride synthesis in the rat: response to diet and exercise.

The responses of hepatic and adipose tissue malic enzyme (ME), citrate cleavage enzyme (CCE), glucose-6-phosphate dehydrogenase (G6PD), and glyceride synthetase (GS) to exercise training and exhaustive exercies and the potential of a high fat or high carbohydrate diet to modify these responses were studied in male Carworth rats. Characteristic elevation and depression of ME, CCE, and G6PD were decreased in skeletal muscle, liver, and adipose tissues of high carbohydrate-fed rats. A significant two-way diet-training interaction was indicated for hepatic ME and G6PD. This interaction resulted from an apparent training modulation of ME and C6PD responses to the high fat and high carbohydrate diets. Adipose tissue G6PD was significantly decreased by training. Exhaustive exercise performed immediately prior to sacrifice did not significantly alter ME or CCE activities in either liver or adipose tissues, but decreased adipose tissue G6PD in untrained rats. Exhaustion was also associated with decreased GS activity in muscle and liver. Physical training was associated with a significant increase in GS in muscle and adipose tissues. In contrast to glyceride synthesis, no increase in adipose tissue lipogenic potential was noted in response to training, indicating that the physically trianed rat may have an enhanced ability to store but not synthesize fatty acids.

ATP Citrate (pro-S)-Lyase↗
PubMed1976

The influence of dietary inositol on glyceride composition and synthesis in livers of rats fed different fats.

The effect of inositol supplementation on the composition and biosynthesis of glycerides in the livers of rats fed diets containing fats with differing fatty acid composition was investigated. The dietary fats employed in these studies included corn oil, Tower rapeseed oil (RSO), partially hydrogenated soybean oil (SBO), and tallow. No significant influence of inositol on hepatic triglyceride levels was found in animals fed corn oil and SBO whereas inositol deficiency caused a two-and four-fold elevation in triglyceride concentrations in the RSO and tallow groups, respectively. The level of total fatty acids in phospholipid (mg/g liver) was slightly decreased in all fat groups and included a notable decrease in the concentration of monoenoic (18:1) and dienoic (18:2) acids in the RSO and tallow groups. Dietary inositol had a minor effect on the weight % of individual fatty acids in hepatic triglycerides. Inositol-deficient animals showed an increased rate of glyceride synthesis from glycerol-3-phosphate (glycerol-3-P) regardless of the type of fat that was fed. The results indicate that triglyceride accumulation in liver under conditions of inositol deficiency is not only produced with highly saturated fats since the most unsaturated of all the fats tested, Tower RSO, also gave the syndrome. The results further suggested that the accumulation of hepatic lipid due to the feeding of inositol-deficient diets likely arises from their effect on specific metabolic site(s) other than the conversion of glycerol-3-P into lipid.

Animals↗
PubMed1978

Effects of diet on swine glyceride lipid metabolism.

Swine were fed equal amounts of isoenergetic-isonitrogenous diets with low-fat or high-fat content. The high-fat diet, as well as starvation, suppressed the synthesis of fatty acid from glucose in adipose tissue. Diet had no effect on adipose tissue enzymes associated with glyceride synthesis; whereas starvation caused all activities expressed per g tissue to decrease. The hepatic enzyme activities associated with glyceride synthesis tended to be greater in swine fed the the high-fat diet compared to the low-fat diet. Starvation lowered the hepatic esterification of glycerol-3-phosphate but did not influence other enzymes.

Acyltransferases↗
PubMed1988

Influence of different dietary fats on the incorporation of exogenous fatty acids into rat adipose glycerides.

Male Wistar rats were fed for 6 wk either a control low fat diet (1.5% sunflower seed oil) or a diet containing 10% fat: either saturated (coconut oil, cocoa butter) or unsaturated (olive oil, sunflower seed oil). In each dietary condition, in vitro incorporation of exogenously added fatty acids (ranging from capric to oleic acid) was studied in epididymal adipose glycerides. Analysis of variance of data revealed that there was a significant effect of the diet x substrate interaction. When results were expressed per cell lipid weight medium-chain fatty acids (capric and lauric) were esterified to a lesser extent than long-chain fatty acids regardless of the nature of dietary fat (saturated vs. unsaturated). The nature of dietary fat was found to have no effect on the incorporation of medium-chain fatty acids. Feeding saturated fats resulted in an increase of incorporation of long-chain fatty acids into adipose glycerides whereas feeding unsaturated fats did not modify fatty acid incorporation. Modifications of mean fat cell size by dietary fat could not account for all the observed variations.

Adipose Tissue↗
PubMed1969

Oral glucose tolerance and related factors in a normal population sample. I. Blood sugar, plasma insulin, glyceride, and cholesterol measurements and the effects of age and sex.

Oral glucose tolerance tests were performed on 220 people, a representative sample of the employees of a large pharmaceutical company. Blood sugar and plasma immunoreactive insulin levels were measured on each sample of venous blood obtained before and at half-hourly intervals for two hours after 50 g. of glucose by mouth; plasma cholesterol and glycerides were measured on the fasting sample only.Women had higher mean insulin levels throughout the test, though their mean blood sugar levels were higher only at 90 and 120 minutes. In both sexes there were positive correlations between age and the levels of blood sugar, plasma cholesterol, and plasma glycerides. Though the levels of glucose rose with age, those of insulin did not.

Adult↗
PubMed1969

Oral glucose tolerance and related factors in a normal population sample. II. Interrelationship of glycerides, cholesterol, and other factors with the glucose and insulin response.

The data available from the previous paper have been analysed to determine the interaction between the blood sugar and plasma insulin responses to oral glucose and a number of other biological variables. The total sugar and insulin responses were derived by calculating the total area and the incremental area under the curves.The blood sugar area was significantly correlated with age in both men and women, particularly the former. A striking degree of correlation was found in men between the level of fasting glycerides and the blood sugar area. There was a significant correlation also in women, but this was entirely due to the presence of the older, postmenopausal individuals. A lower degree of correlation was found in both sexes between fasting glycerides and the insulin area.Obesity, as defined by three interrelated factors-ponderal index, triceps fat-fold thickness, and arm girth -was significantly correlated with the insulin area (the association being stronger in the men) and with the blood sugar area only in men.The fasting cholesterol level was correlated with obesity in both sexes but with the blood sugar area and the insulin area only in men.

Adult↗
PubMed1988

Adipose tissue glyceride synthesis in patients with hyperapobetalipoproteinemia.

Adipose tissue was obtained at thoracotomy in five control patients with valvular heart disease, all of whom were free of coronary artery disease and all of whom were normolipidemic with normal low density lipoprotein apolipoprotein B levels, and eight patients with coronary artery disease, all of whom had hyperapobetalipoproteinemia. In both groups, the rates at which linoleic acid and palmitic acid were incorporated into diglyceride and triglyceride were determined in vitro. The data indicate that fatty acid incorporation into adipose tissue glycerides was twice as rapid in controls as in patients with hyperapobetalipoproteinemia. By contrast there was no difference between the groups in the rate of net lipolysis of adipocyte glyceride. The data at hand do not establish the mechanism responsible for the difference in synthesis between normal subjects and patients with hyperapobetalipoproteinemia, but this may explain the delayed chylomicron triglyceride clearance previously observed in the disorder.

Adipose Tissue↗
PubMed2005

Etoposide-loaded nanoparticles made from glyceride lipids: formulation, characterization, in vitro drug release, and stability evaluation.

The aim of the study was to prepare etoposide-loaded nanoparticles with glyceride lipids and then characterize and evaluate the in vitro steric stability and drug release characteristics and stability. The nanoparticles were prepared by melt emulsification and homogenization followed by spray drying of nanodispersion. Spray drying created powder nanoparticles with excellent redispersibility and a minimal increase in particle size (20-40 nm). Experimental variables, such as homogenization pressure, number of homogenization cycles, and surfactant concentration, showed a profound influence on the particle size and distribution. Spray drying of Poloxamer 407-stabilized nanodispersion lead to the formation of matrix-like structures surrounding the nanoparticles, resulting in particle growth. The in vitro steric stability test revealed that the lipid nanoparticles stabilized by sodium tauroglycocholate exhibit excellent steric stability compared with Poloxamer 407. All 3 glyceride nanoparticle formulations exhibited sustained release characteristics, and the release pattern followed the Higuchi equation. The spray-dried lipid nanoparticles stored in black polypropylene containers exhibited excellent long-term stability at 25 degrees C and room light conditions. Such stable lipid nanoparticles with in vitro steric stability can be a beneficial delivery system for intravenous administration as long circulating carriers for controlled and targeted drug delivery.

Chemistry, Pharmaceutical↗
PubMed2006

Acidolysis and glyceride synthesis reactions using fatty acids with two Pseudomonas lipases having different substrate specificities.

Enzymatic acidolysis and glyceride synthesis using polyunsaturated fatty acids (PUFAs) with lipases from Pseudomonas fluorescens HU380 (HU-lipase), P. fluorescens AK102 (AK-lipase), and Candida rugosa (CR-lipase) were studied. The acidolysis of triolein with eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA) in n-hexane was evaluated with lipases immobilized on Celite 545. HU-lipase showed the highest incorporation rate at a low temperature (10 degrees C) with either EPA or DHA as the acyl donor, and the rate decreased with increasing reaction temperature. At 45 degrees C, the rates for EPA and DHA were 7.1 and 0.5 relative to those at 10 degrees C, respectively. The EPA incorporation rate was even higher at a low temperature (10 degrees C), and the DHA incorporation rate increased with decreasing temperature. Although AK-lipase showed the reverse tendency for incorporation rate, the DHA incorporation rate increased with increasing reaction temperature with both PUFAs. HU-lipase reacted well with PUFAs such as DHA, EPA, arachidonic acid (AA), mead acid (MA), and dihomo-gamma-linolenic acid (DGLA) on acidolysis and glyceride synthesis. The reactivities of AK-lipase toward these PUFAs except for DGLA, i.e., MA, AA, EPA, and DHA, were low for both reactions. The unique substrate specificities of the lipases from the Pseudomonas strains will enable us to use these lipases for the modification of fats and oils containing PUFAs such as fish oil.

Bacterial Proteins↗
PubMed2005

Effects of glycerides on the intestinal absorption of cyclosporine a using the in-situ mesenteric vein cannulated rat model.

The purpose of this study was to evaluate and compare the effect of glycerides with different fatty acid distributions (e.g. Arlacel 186, Capmul GMO and Captex 350) on Cyclosporine absorption in rat ileum segment using the modified single-pass intestinal perfusion with mesenteric vein cannulation. Drug concentration in the perfusate and blood plasma was analyzed by HPLC; and permeability coefficients were calculated from drug appearance in blood (P(blood)) and disappearance from perfusate (P(lumen)). Particle size was measured using Malvern Zetasaizer 1000HSA. Rheologic properties were measured using Brookfield viscometer. The results show that the average particle sizes after dilution (100 folds) of formulae containing Arlacel 186, Capmul GMO and Captex 350 and containing 0.8 mM CsA were 260+/-35.8, 130+/-11.4 and 37.5+/-6.0 nm, respectively. The polydispersity index was 0.6, 0.7 and 0.108 for formulations with Arlacel 186, Capmul GMO and Captex 350, respectively. CsA permeability coefficients (P(blood)) calculated from drug appearance in the blood in presence of Arlacel 186, Capmul GMO and Captex 350 were 0.3x10(-6), 1.0x10(-6) and 1.7x10(-6) cm2/sec, respectively. Phenol red was used as a water marker to determine net water absorption and secretion. Its constant concentration suggested that formulation did not alter intestinal water flux. From the results we can conclude that degree of glyceride esterification has a potential impact on the average particle size distribution and polydispersity of the formed micelles on dilution, which on turn contribute to the interaction between membrane and drug.

Animals↗
PubMed1975

Sustained release of naltrexone from glyceride implants.

Solid dispersions of naltrexone in natural glycerides were used to form injectable implants which continously release narcotic antagonists in vivo. The dispersions were formed and tested either as small cylindrical pellets, e.g. 1x3.0 mm in size, or as particles with diameters in size ranges between 125-250 mu, that are suspended in an aqueous methyl cellulose solution. Both types of implants delivered naltrexone to mice at rates that were effective in blocking the antiociceptive action of morphine for at least one month. The rate of naltrexone release was controlled by altering its concentration in the dispersion and by varying the glyceride composition. Degradation and absorption of the implants were found to depend on their composition, dimensions and location in the body. No appreciable tissue incompatibility was seen in mice, rats, rabbits, monkeys and swine, even when long-lasting preparations were removed a year after treatment.

Animals↗
PubMed2004

Synthesis, biological evaluation and kinetic studies of glyceride prodrugs of diclofenac.

The prodrugs (glyceride derivatives) 3a and 3b of diclofenac were prepared by reacting 1, 2, 3-trihydroxy propane-1,3-dipalmitate/stearate with the acid chloride of diclofenac as potential prodrugs to reduce the gastrointestinal toxicity associated with them. These prodrugs were evaluated for their ulcerogenicity, anti-inflammatory and analgesic activity. It was found that the prodrugs were significantly less irritating to the gastric mucosa as indicated by severity index of 0.86, 0.78 compared to 1.6 of diclofenac. The prodrugs 3a and 3b showed better anti-inflammatory and analgesic activity than the parent drugs. The hydrolysis of prodrugs 3a and 3b were studied at pH 3, 4, 5 and 7.4. The HPLC analysis showed that the prodrugs were resistant to hydrolysis at pH 3, 4 and 5 indicating that they did not hydrolyze in acidic environment, whereas at pH 7.4 the prodrugs readily released the parent drug in significant quantities. The plasma levels of diclofenac were also analyzed by HPLC in rats after single oral dose of the prodrugs. The results indicated that the parent drugs were readily released. The concentration of diclofenac during the study was found higher in animals treated with prodrugs 3a and 3b compared with animals treated with diclofenac. The concentration of diclofenac was found to be 38.59, 33.6 and 30.36 microg/ml in animals treated with prodrugs 3a, 3b and diclofenac respectively. In conclusion, all these studies indicated that the glyceride prodrugs of diclofenac might be considered as potential biolabile prodrugs of diclofenac.

Acetic Acid↗
PubMed1995

Isotope dilution mass spectrometry as a candidate definitive method for determining total glycerides and triglycerides in serum.

A new isotope dilution mass spectrometric method for total glycerides and triglycerides in human serum is described. Total glycerides are defined as the sum of tri-, di-, and monoglycerides plus free glycerol; triglycerides are defined as the pure triglyceride species. In both determinations, serum samples are supplemented by addition of [13C3]tripalmitin, processed, derivatized, and the abundance ratios of selected ions are determined. Bias is investigated by quantifying the analyte in the same samples under different chromatographic and ionization conditions. The analytes were determined in two human serum pools. The CV for a single measurement ranged from 0.35% to 0.72%, and the relative SEM ranged from 0.10% to 0.34%; there was no significant bias in the measurements. The combination of high precision and absence of significant bias in the results qualify this method for consideration as a Definitive Method as defined by the National Committee for Clinical Laboratory Standards.

Carbon Isotopes↗
PubMed1997

Enhancing effects of monohexanoin and two other medium-chain glyceride vehicles on intestinal absorption of desmopressin (dDAVP).

The intestinal absorption enhancement of the nonapeptide [Mpa1,D-Arg8]vasopressin (dDAVP) by medium-chain glyceride vehicles was studied using an in vivo rat model. Rats were gavaged with dDAVP formulated with three different lipid vehicles: (1) monohexanoin, (2) mixed monoglycerides, diglycerides and triglycerides of hexanoic acid and (3) monoglycerides, diglycerides and triglycerides of octanoic and decanoic acids, and with saline as control. The marker absorption into blood and urine was followed for 24 hr. All lipid vehicles enhanced the oral bioavailability of dDAVP, but monohexanoin gave the highest increase, approximately 10 times that of control. In contrast to dDAVP, the stable and more lipophilic nonapeptide analog [Mpa1,D-Tyr(ethyl)2,Val4,D-Arg8]oxytocin did not show increased urine recovery when formulated with monohexanoin. A 2-fold increase in urine recovery of the inert low-molecular-weight marker [51Cr]EDTA was observed when formulated with monohexanoin. With use of the fluorescent marker Evans blue formulated with monohexanoin, an elevated accumulation of Evans blue in the mucus layer was observed after incubation in in situ loops. No mucosal damage after lipid vehicle gavage was observed by light microscopic evaluation. Medium-chain glycerides functioned well as oral absorption enhancers of the model peptide dDAVP, and monohexanoin showed the highest enhancement capacity. The mechanisms of this enhancement appear to be related to a protection against luminal dDAVP degradation, mucoadhesive properties of the vehicle and, possibly, an altered epithelial absorption pathway.

Animals↗
PubMed1976

Sustained release of naltrexone from glyceride implants.

Solid dispersions of naltrexone in natural glycerides were used to form injectable implants which continuously release narcotic antagonists in vivo. The dispersions were formed and tested either as small cylindrical pellets, e.g. l x 3.0 mm in size, or as particles with diameters in size ranges between 125-250 mu, that are suspended in an aqueous methyl cellulose solution. Both types of implants delivered naltrexone to mice at rates that were effective in blocking the antiociceptive action of morphine for at least one month. The rate of naltrexone release was controlled by altering its concentration in the dispersion and by varying the glyceride composition. Degradation and absorption of the implants were found to depend on their composition, dimensions and location in the body. No appreciable tissue incompatibility was seen in mice, rats, rabbits, monkeys and swine, even when long-lasting preparations were removed a year after treatment.

Animals↗
PubMed2005

Preparation and evaluation of glibenclamide-polyglycolized glycerides solid dispersions with silicon dioxide by spray drying technique.

Solid dispersions (SDs) of glibenclamide (GBM); a poorly water-soluble drug and polyglycolized glycerides (Gelucire with the aid of silicon dioxide (Aerosil 200); as an adsorbent, were prepared by spray drying technique. SDs and spray dried GBM in comparison with pure GBM and corresponding physical mixtures (PMs) were initially characterized and then subjected to ageing study up to 3 months. Initial characterization of SDs and spray dried GBM by DSC and XRPD showed that GBM was present in its amorphous form (AGBM). Improvement in the solubility and dissolution rate was observed for all samples. DRIFT spectroscopy revealed presence of hydrogen bonding in SDs. During ageing study, almost no decrease of in vitro drug dissolution was observed, over the period of 3 months as compare with freshly prepared SDs. Slight crystallinity in SDs was observed in the DSC and XRPD studies during ageing. Moreover in vivo study in Swiss Albino mice also justified the improvement in the therapeutic efficacy of amorphous GBM in SDs over pure GBM. Thus, present study demonstrated the high potential of spray drying technique for obtaining stable free flowing SDs of poorly water-soluble drugs using polyglycolized glycerides carriers with the aid of silicon dioxide as an adsorbent.

Animals↗
PubMed2001

Dietary oils high in oleic acid, but with different non-glyceride contents, have different effects on lipid profiles and peroxidation in rabbit hepatic mitochondria.

The influence on the lipid profile and lipid peroxidation in rabbit-liver mitochondria exerted by different edible oils high in oleic acid but different non-glyceride phenolic fractions was studied. High-phenolic virgin olive oil from the variety "Picual", the same oil submitted to an exhaustive process of washing to eliminate the phenolic fraction without altering the lipid profile and high-oleic sunflower oil (poor in phenolic compounds) were added to rabbit diets. The results reveal the importance of the different oleic: linoleic ratio of the lipid sources on the lipid profile of mitochondrial membranes. This is highlighted by the greater proportion of saturated fatty acids and the lower content in oleic acid (p < 0.05) shown by the rabbits fed on high-oleic sunflower oil. The group fed on the fat rich in phenolics exhibited the highest level of antioxidants (alpha-tocopherol, ubiquinone 10) and the highest activity of glutathione peroxidase as well as the lowest content in hydroperoxides and TBARS. The study provides evidences in vivo about the considerable antioxidant capacity of the phenolic fraction of virgin olive oil in rabbit-liver mitochondria and the important role that this non-glyceride fraction can play in the overall antioxidant benefits attributed to this oil.

Journal Article↗