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Sample records for acid ascorbyl palmitate

  1. 21 CFR 182.3149 - Ascorbyl palmitate.

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Ascorbyl palmitate. 182.3149 Section 182.3149 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) FOOD FOR... Ascorbyl palmitate. (a) Product. Ascorbyl palmitate. (b) Conditions of use. This substance is...

  2. 21 CFR 582.3149 - Ascorbyl palmitate.

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ascorbyl palmitate. 582.3149 Section 582.3149 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL....3149 Ascorbyl palmitate. (a) Product. Ascorbyl palmitate. (b) Conditions of use. This substance...

  3. Additions of caffeic acid, ascorbyl palmitate or gamma-tocopherol to fish oil-enriched energy bars affect lipid oxidation differently

    Horn, Anna Frisenfeldt; Nielsen, Nina Skall; Jacobsen, Charlotte

    2009-01-01

    The objectives of the study were to investigate the effects of caffeic acid, ascorbyl palmitate and gamma-tocopherol on protection of fish oil-enriched energy bars against lipid oxidation during storage for 10 weeks at room temperature. The lipophilic gamma-tocopherol reduced lipid oxidation during......, or the hydrophilic caffeic acid, or the amphiphilic ascorbyl palmitate at concentrations of 75, 150 and 300 mu g/g fish oil. Prooxidative effects were observed as an increase in the formation of lipid hydroperoxides and volatile secondary oxidation products, as well as the development of rancid off...

  4. Scientific Opinion on the safety and efficacy of vitamin C (ascorbic acid, sodium ascorbate, calcium ascorbate, ascorbyl palmitate, sodium calcium ascorbyl phosphate and sodium ascorbyl phosphate) as a feed additive for all animal species based on a dossier submitted by DSM Nutritional Products Ltd

    EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP)

    2013-01-01

    Vitamin C is essential for primates, guinea pigs and fish. Vitamin C, in the form of ascorbic acid and its calcium and sodium salts, ascorbyl palmitate, sodium calcium ascorbyl phosphate and sodium ascorbyl phosphate, is safe for all animal species. Setting a maximum content in feed and water for drinking is not considered necessary. Data on the vitamin C consumption of consumers are based on the levels of vitamin C in foodstuffs, including food of animal origin, produced in accordance with c...

  5. Inhibition of collagen synthesis by select calcium and sodium channel blockers can be mitigated by ascorbic acid and ascorbyl palmitate.

    Ivanov, Vadim; Ivanova, Svetlana; Kalinovsky, Tatiana; Niedzwiecki, Aleksandra; Rath, Matthias

    2016-01-01

    Calcium, sodium and potassium channel blockers are widely prescribed medications for a variety of health problems, most frequently for cardiac arrhythmias, hypertension, angina pectoris and other disorders. However, chronic application of channel blockers is associated with numerous side effects, including worsening cardiac pathology. For example, nifedipine, a calcium-channel blocker was found to be associated with increased mortality and increased risk for myocardial infarction. In addition to the side effects mentioned above by different channel blockers, these drugs can cause arterial wall damage, thereby contributing to vascular wall structure destabilization and promoting events facilitating rupture of plaques. Collagen synthesis is regulated by ascorbic acid, which is also essential for its optimum structure as a cofactor in lysine and proline hydroxylation, a precondition for optimum crosslinking of collagen and elastin. Therefore, the main objective in this study was to evaluate effects of various types of channel blockers on intracellular accumulation and cellular functions of ascorbate, specifically in relation to formation and extracellular deposition of major collagen types relevant for vascular function. Effects of select Na- and Ca- channel blockers on collagen synthesis and deposition were evaluated in cultured human dermal fibroblasts and aortic smooth muscle cells by immunoassay. All channel blockers tested demonstrated inhibitory effects on collagen type I deposition to the ECM by fibroblasts, each to a different degree. Ascorbic acid significantly increased collagen I ECM deposition. Nifedipine (50 µM), a representative of channel blockers tested, significantly reduced ascorbic acid and ascorbyl palmitate-dependent ECM deposition of collagen type l and collagen type lV by cultured aortic smooth muscle cells. In addition, nifedipine (50 µM) significantly reduced ascorbate-dependent collagen type l and type lV synthesis by cultured aortic smooth

  6. Inhibition of collagen synthesis by select calcium and sodium channel blockers can be mitigated by ascorbic acid and ascorbyl palmitate

    Ivanov, Vadim; Ivanova, Svetlana; Kalinovsky, Tatiana; Niedzwiecki, Aleksandra; Rath, Matthias

    2016-01-01

    Calcium, sodium and potassium channel blockers are widely prescribed medications for a variety of health problems, most frequently for cardiac arrhythmias, hypertension, angina pectoris and other disorders. However, chronic application of channel blockers is associated with numerous side effects, including worsening cardiac pathology. For example, nifedipine, a calcium-channel blocker was found to be associated with increased mortality and increased risk for myocardial infarction. In addition to the side effects mentioned above by different channel blockers, these drugs can cause arterial wall damage, thereby contributing to vascular wall structure destabilization and promoting events facilitating rupture of plaques. Collagen synthesis is regulated by ascorbic acid, which is also essential for its optimum structure as a cofactor in lysine and proline hydroxylation, a precondition for optimum crosslinking of collagen and elastin. Therefore, the main objective in this study was to evaluate effects of various types of channel blockers on intracellular accumulation and cellular functions of ascorbate, specifically in relation to formation and extracellular deposition of major collagen types relevant for vascular function. Effects of select Na- and Ca- channel blockers on collagen synthesis and deposition were evaluated in cultured human dermal fibroblasts and aortic smooth muscle cells by immunoassay. All channel blockers tested demonstrated inhibitory effects on collagen type I deposition to the ECM by fibroblasts, each to a different degree. Ascorbic acid significantly increased collagen I ECM deposition. Nifedipine (50 µM), a representative of channel blockers tested, significantly reduced ascorbic acid and ascorbyl palmitate-dependent ECM deposition of collagen type l and collagen type lV by cultured aortic smooth muscle cells. In addition, nifedipine (50 µM) significantly reduced ascorbate-dependent collagen type l and type lV synthesis by cultured aortic smooth

  7. Scientific Opinion on the safety and efficacy of vitamin C (ascorbic acid, sodium ascorbate, calcium ascorbate, ascorbyl palmitate, sodium calcium ascorbyl phosphate and sodium ascorbyl phosphate as a feed additive for all animal species based on a dossier submitted by DSM Nutritional Products Ltd

    EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP

    2013-02-01

    Full Text Available Vitamin C is essential for primates, guinea pigs and fish. Vitamin C, in the form of ascorbic acid and its calcium and sodium salts, ascorbyl palmitate, sodium calcium ascorbyl phosphate and sodium ascorbyl phosphate, is safe for all animal species. Setting a maximum content in feed and water for drinking is not considered necessary. Data on the vitamin C consumption of consumers are based on the levels of vitamin C in foodstuffs, including food of animal origin, produced in accordance with current EU legislation on the supplementation of feed with vitamin C. The exposure is far below the guidance level. Any potential contribution of the use of vitamin C in feed is therefore already considered in the above data. Consequently, the use of vitamin C in animal nutrition is not of concern for consumer safety. In the absence of inhalation toxicity studies it would be prudent to assume that inhalation of dust from the additives presents a health hazard to workers. Sodium calcium ascorbyl phosphate is not an irritant to skin and eyes and is unlikely to be a skin sensitiser. This conclusion is extrapolated to sodium ascorbyl phosphate. In the absence of data, ascorbic acid, sodium ascorbate, calcium ascorbate and ascorbyl palmitate should be considered as irritant to skin and eyes and as dermal sensitisers. The supplementation of feed with vitamin C does not pose a risk to the environment. Ascorbic acid, sodium calcium ascorbyl phosphate and sodium ascorbyl phosphate are regarded as effective sources of vitamin C when added to feed or water for drinking. Since ascorbic acid, sodium ascorbate, calcium ascorbate and ascorbyl palmitate are authorised for use as antioxidants in food and their function in feed is essentially the same as that in food, no further demonstration of efficacy is considered necessary.

  8. Optimization of α-tocopherol and ascorbyl palmitate addition for the stabilization of sardine oil

    Morales-Medina, R.; García-Moreno, P. J.; Muñío, M. M.; Guadix, A.; Guadix, E. M.

    2015-01-01

    The purpose of the present work was to optimize the addition of natural antioxidants (α- tocopherol and ascorbyl palmitate) for the stabilization of sardine oil rich in omega-3 PUFA. The optimal values for peroxide value (PV), which minimizes primary oxidation products, were obtained at low concentrations of α-tocopherol (50–207 ppm), high content of ascorbyl palmitate (450 ppm) and 50 ppm citric acid. On the other hand, optimal values for p-anisidine value (AV), which minimizes secondary oxi...

  9. Effect of ascorbyl palmitate on oxidative stability of chemically interesterified cottonseed and olive oils

    Javidipour, Issa; Tüfenk, Remzi; Baştürk, Ayhan

    2013-01-01

    The effects of 400 ppm ascorbyl palmitate (AP) on fatty acids composition, tocopherol, peroxide value (PV) and malonaldehyde (MAD) contents of refined cottonseed oil (CO) and virgin olive oil (OO) during chemical interesterification (CI), and storage at 60 °C for 28 days were investigated. CI significantly decreased (p 

  10. Lecithin based lamellar liquid crystals as a physiologically acceptable dermal delivery system for ascorbyl palmitate

    GAŠPERLIN, MIRJANA; Gosenca, Mirjam; Bešter-Rogač, Marija

    2015-01-01

    Liquid crystalline systems with a lamellar structure have been extensively studied as dermal delivery systems. Ascorbyl palmitate (AP) is one of the most studied and used ascorbic acid derivatives and is employed as an antioxidant to prevent skin aging. The aim of this study was to develop and characterize skin-compliant dermal delivery systems with a liquid crystalline structure for AP. First, a pseudoternary phase diagram was constructed using Tween 80/lecithin/isopropyl myristate/water at ...

  11. Ascorbyl palmitate interaction with phospholipid monolayers: electrostatic and rheological preponderancy.

    Mottola, Milagro; Wilke, Natalia; Benedini, Luciano; Oliveira, Rafael Gustavo; Fanani, Maria Laura

    2013-11-01

    Ascorbyl palmitate (ASC16) is an anionic amphiphilic molecule of pharmacological interest due to its antioxidant properties. We found that ASC16 strongly interacted with model membranes. ASC16 penetrated phospholipid monolayers, with a cutoff near the theoretical surface pressure limit. The presence of a lipid film at the interface favored ASC16 insertion compared with a bare air/water surface. The adsorption and penetration time curves showed a biphasic behavior: the first rapid peak evidenced a fast adsorption of charged ASC16 molecules to the interface that promoted a lowering of surface pH, thus partially neutralizing and compacting the film. The second rise represented an approach to the equilibrium between the ASC16 molecules in the subphase and the surface monolayer, whose kinetics depended on the ionization state of the film. Based on the Langmuir dimiristoylphosphatidylcholine+ASC16 monolayer data, we estimated an ASC16 partition coefficient to dimiristoylphosphatidylcholine monolayers of 1.5×10(5) and a ΔGp=-6.7kcal·mol(-1). The rheological properties of the host membrane were determinant for ASC16 penetration kinetics: a fluid membrane, as provided by cholesterol, disrupted the liquid-condensed ASC16-enriched domains and favored ASC16 penetration. Subphase pH conditions affected ASC16 aggregation in bulk: the smaller structures at acidic pHs showed a faster equilibrium with the surface film than large lamellar ones. Our results revealed that the ASC16 interaction with model membranes has a highly complex regulation. The polymorphism in the ASC16 bulk aggregation added complexity to the equilibrium between the surface and subphase form of ASC16, whose understanding may shed light on the pharmacological function of this drug. PMID:23806650

  12. Ascorbyl palmitate-loaded chitosan nanoparticles: characteristic and polyphenol oxidase inhibitory activity.

    Kim, Mi Kyung; Lee, Ji-Soo; Kim, Kwang Yup; Lee, Hyeon Gyu

    2013-03-01

    The aim of this study was to produce ascorbyl palmitate (AP)-loaded nanoparticles in order to inhibit polyphenol oxidase (PPO) in bananas. AP-loaded chitosan nanoparticles were prepared using acetic acid and citric acid (denoted as CS/AA and CS/CA nanoparticles, respectively). As the initial AP concentration increases, the particle size significantly decreases, and the zeta potential, entrapment and loading efficiency significantly increases. The PPO inhibitory activity of AP was effectively improved when AP was nano-encapsulated by chitosan compared to no encapsulation. These results suggest that chitosan nano-encapsulation can be used to enhance the PPO inhibitory activity of AP. PMID:23247266

  13. Electrochemical assay of the antioxidant ascorbyl palmitate in mixed medium.

    Teneva, Olga; Dimcheva, Nina

    2016-07-15

    Electrooxidation of ascorbyl palmitate (AP) over gold screen-printed electrode (AuSPE) and gold nanoparticles modified graphite (AuNPs/gr) was examined in mixed water-alcohol medium. Voltammetric and amperometric studies showed that: (i) AP oxidation on the AuSPE proceeds at higher potential than on AuNPs/gr; (ii) the current density on AuNPs/gr was 2.4 times higher than on AuSPE; (iii) the linear dynamic range for AuNPs/gr doubled that for AuSPE. At the optimal for AuNPs/gr operating potential (250 mV) the following operational parameters were determined: sensitivity 1.627 ± 0.138 μA mM(-1) mm(-2); linearity up to 500 μM; LOD=5.8 μM. Quantification of the AP content in a real sample - stabilised flaxseed oil, was performed. PMID:26948586

  14. Ascorbyl palmitate/DSPE-PEG nanocarriers for oral iron delivery: preparation, characterisation and in vitro evaluation.

    Zariwala, M Gulrez; Farnaud, Sebastien; Merchant, Zahra; Somavarapu, Satyanarayana; Renshaw, Derek

    2014-03-01

    The objective of this study was to encapsulate iron in nanocarriers formulated with ascorbyl palmitate and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine polyethylene glycol (DSPE-PEG) for oral delivery. Blank and iron (Fe) loaded nanocarriers were prepared by a modified thin film method using ascorbyl palmitate and DSPE-PEG. Surface charge of the nanocarriers was modified by the inclusion of chitosan (CHI) during the formulation process. Blank and iron loaded ascorbyl palmitate/DSPE nanocarriers were visualised by transmission electron microscopy (TEM) and physiochemical characterisations of the nanocarriers carried out to determine the mean particle size and zeta potential. Inclusion of chitosan imparted a net positive charge on the nanocarrier surface and also led to an increase in mean particle size. Iron entrapment in ascorbyl palmitate-Fe and ascorbyl palmitate-CHI-Fe nanocarriers was 67% and 76% respectively, suggesting a beneficial effect of chitosan on nanocarrier Fe entrapment. Iron absorption was estimated by measuring Caco-2 cell ferritin formation using ferrous sulphate as a reference standard. Iron absorption from ascorbyl palmitate-Fe (592.17±21.12 ng/mg cell protein) and ascorbyl palmitate-CHI-Fe (800.12±47.6 ng/mg, cell protein) nanocarriers was 1.35-fold and 1.5-fold higher than that from free ferrous sulphate, respectively (505.74±23.73 ng/mg cell protein) (n=6, p<0.05). This study demonstrates for the first time preparation and characterisation of iron loaded ascorbyl palmitate/DSPE PEG nanocarriers, and that engineering of the nanocarriers with chitosan leads to a significant augmentation of iron absorption. PMID:24333557

  15. Optimization of α-tocopherol and ascorbyl palmitate addition for the stabilization of sardine oil

    Morales-Medina, R.

    2015-06-01

    Full Text Available The purpose of the present work was to optimize the addition of natural antioxidants (α- tocopherol and ascorbyl palmitate for the stabilization of sardine oil rich in omega-3 PUFA. The optimal values for peroxide value (PV, which minimizes primary oxidation products, were obtained at low concentrations of α-tocopherol (50–207 ppm, high content of ascorbyl palmitate (450 ppm and 50 ppm citric acid. On the other hand, optimal values for p-anisidine value (AV, which minimizes secondary oxidation products, were found at medium concentrations of α-tocopherol (478–493 ppm, high contents of ascorbyl palmitate (390–450 ppm and 50 ppm citric acid. The conflicting effect of α-tocopherol on the individual optimization of PV and AV motivated the generation of a Pareto front (set of non inferior solutions employing the weighted-sum multi-objective optimization technique.El objetivo de este trabajo fue optimizar la adición de antioxidantes naturales (α-tocoferol y palmitato de ascorbilo para la estabilización de aceite de sardina rico en omega-3 PUFA. Bajas concentraciones de α-tocoferol (50–207 ppm combinadas con la adicción de antioxidantes secundarios como palmitato de ascorbilo (450 ppm y ácido cítrico (50 ppm, minimizaron la formación de hidroperóxidos en el aceite de sardina estudiado. Sin embargo, los productos secundarios de oxidación se redujeron para concentraciones medias de α-tocoferol (478–493 ppm, altas de palmitato de ascorbilo (390–450 ppm y 50 ppm de ácido cítrico. El efecto contradictorio de la concentración de α-tocoferol en la optimización individual del índice de peróxidos e índice de p-anisidina motivó la realización de una optimización simultánea que permite satisfacer la optimización de cada una de las variables individuales en el grado deseado.

  16. A New Approach for Increasing Ascorbyl Palmitate Stability by Addition of Non-irritant Co-antioxidant

    Obreza, Aleš; Pečar, Slavko; Gosenca, Mirjam; GAŠPERLIN, MIRJANA

    2010-01-01

    The aim of this work was to test innovative approach for enhancing ascorbyl palmitate stability in microemulsions for topical application by addition of newly synthesized co-antioxidant 4-(tridecyloxy)benzaldehyde oxime (TDBO) and to investigate its antioxidant activity and finally to evaluate cytotoxicity of TDBO-loaded microemulsions on keratinocyte cells. TDBO significantly increased ascorbyl palmitate stability in oil-dispersed-in-water (o/w) microemulsions, most presumably due to reducti...

  17. Stability of potato chip fried in vegetable oils with different degree of unsaturation. Effect of ascorbyl palmitate during storage

    TORRES R.; Salam, M.; Pérez, P.; Goicoechea, E.; Ortiz, J; Romero, N; Urra, C.; Dobarganes, M. C.; Robert, P.; Masson, L

    2002-01-01

    Four vegetable oils with different polyunsaturated/saturated fatty acid ratio (P/S): 5.2 for sunflower oil, 3.,4 for canola rapeseed oil, 0.4 for a blend of palm oleic and canola rapeseed oil (80:20), and 0.3 for palm olein were assayed for stability of crisps fried in these oils during storage at 60º C. The action of ascorbyl palmitate with special attention to its synergistic effect on the natural antioxidants was also tested. by addition to the fried potatoes. The evolution of ...

  18. Dermal delivery of ascorbyl palmitate: the potential of colloidal delivery systems

    Gosenca, Mirjam; GAŠPERLIN, MIRJANA

    2015-01-01

    This study examined the suitability of various colloidal systems for ascorbyl palmitate (AP) skin delivery. First, a pseudoternary phase diagram for Tween 80/lecithin/butanol, isopropyl myristate (IPM), and water was constructed and regions of lipophilic (w/o) or hydrophilic (o/w) microemulsions (MEs), and emulsions (EMs) were identified. Afterwards, various phase transition systems on the selected dilution line, as well as liquid crystal (LC) as a delivery system on the same dilution line (b...

  19. Effect of ascorbyl palmitate on oxidative stability of chemically interesterified cottonseed and olive oils.

    Javidipour, Issa; Tüfenk, Remzi; Baştürk, Ayhan

    2015-02-01

    The effects of 400 ppm ascorbyl palmitate (AP) on fatty acids composition, tocopherol, peroxide value (PV) and malonaldehyde (MAD) contents of refined cottonseed oil (CO) and virgin olive oil (OO) during chemical interesterification (CI), and storage at 60 °C for 28 days were investigated. CI significantly decreased (p < 0.05) the tocopherol contents of CO and OO. PVs and MAD contents of oil samples considerably increased up to 20 min of CI, followed by a reduction at 30 min. The unsaturated fatty acids/saturated fatty acids (UFA/SFA) ratios of the samples showed slight but significant (p < 0.05) reduction during accelerated oxidation process. Oils with added 400 ppm AP had higher tocopherol, and lower PVs and MAD contents than their counterparts without AP during CI, and storage at 60 °C. AP increased the oxidative stability of interesterified and non-interesterified CO and OO. PMID:25694696

  20. 抗坏血酸及抗坏血酸棕榈酸酯的稳定性研究%Study on stability of ascorbic acid and ascorbyl palmitate

    刘奕博; 任国谱

    2012-01-01

    The effects of light, temperature, pH, oxidant, antioxidant, metal ions, saccharides on stabilities of ascorbic acid(AA) and ascorbyl palmitate(AP) were studied.Results showed that they were destroyed by sunlight, high temperature, oxidant in different extent and sensitive in neutral and alkaline conditions and AP was more stable than AA.Vitamin E (VE) could protect AP effectively.Cu^2 + , Fe^3+ and Mn^2 + could lead to large loss of AA, Mn^2+ had obvious effect on AP.They were stable when glucose and sucrose existed.%研究了光照、温度、pH、氧化剂、抗氧化剂、金属离子、糖类对抗坏血酸(AA)及抗坏血酸棕榈酸酯(AP)稳定性的影响。结果表明:目光、高温、氧化剂、中性及碱性环境都会不同程度地对两者造成损失,其中抗坏血酸棕榈酸酯的稳定性要强于抗坏血酸。维生素E可以有效保护AP。铜离子、铁离子、锰离子会引起AA较大的损失,锰离子对AP稳定性有显著影响。糖类对两者稳定性基本没有影响。

  1. Lecithin based lamellar liquid crystals as a physiologically acceptable dermal delivery system for ascorbyl palmitate.

    Gosenca, Mirjam; Bešter-Rogač, Marija; Gašperlin, Mirjana

    2013-09-27

    Liquid crystalline systems with a lamellar structure have been extensively studied as dermal delivery systems. Ascorbyl palmitate (AP) is one of the most studied and used ascorbic acid derivatives and is employed as an antioxidant to prevent skin aging. The aim of this study was to develop and characterize skin-compliant dermal delivery systems with a liquid crystalline structure for AP. First, a pseudoternary phase diagram was constructed using Tween 80/lecithin/isopropyl myristate/water at a Tween 80/lecithin mass ratio of 1/1, and the region of lamellar liquid crystals was identified. Second, selected unloaded and AP-loaded lamellar liquid crystal systems were physicochemically characterized with polarizing optical microscopy, small-angle X-ray scattering, differential scanning calorimetry, and rheology techniques. The interlayer spacing and rheological parameters differ regarding quantitative composition, whereas the microstructure of the lamellar phase was affected by the AP incorporation, resulting either in additional micellar structures (at 25 and 32 °C) or being completely destroyed at higher temperature (37°C). After this, the study was oriented towards in vitro cytotoxicity evaluation of lamellar liquid crystal systems on a keratinocyte cell line. The results suggest that the lamellar liquid crystals that were developed could be used as a physiologically acceptable dermal delivery system. PMID:23643736

  2. Ascorbyl palmitate, gamma-tocopherol, and EDTA affect lipid oxidation in fish oil enriched salad dressing differently

    Let, M.B.; Jacobsen, Charlotte; Meyer, Anne S.

    2007-01-01

    The aim of the study was to investigate the ability of γ-tocopherol, ethylenediaminetetraacetate (EDTA), and ascorbyl palmitate to protect fish oil enriched salad dressing against oxidation during a 6 week storage period at room temperature. The lipid-soluble γ-tocopherol (220 and 880 µg g-1 of...... antioxidant, and overall peroxide values and volatiles were reduced by approximately 70 and 77-86%, respectively. Conversely, prooxidant effects were observed with a high concentration of ascorbyl palmitate (300 µg g-1 of fish oil), whereas a low concentration was slightly antioxidative (50 µg/g of fish oil......). Finally, a combination of all three antioxidants completely inhibited oxidation during storage, indicating that the prooxidant effects of ascorbyl palmitate were reverted or overshadowed by EDTA and γ-tocopherol....

  3. Palmitato de ascorbil e acetato de tocoferol como antioxidantes metabólicos em larvas de dourado Ascorbyl palmitate and tocopherol acetate as metabolic antioxidants in dourado larvae

    Daniel Okamura

    2008-08-01

    palmitate, ascorbic acid and dehydroascorbic acid, total length, weight and height of the head. Ascorbyl palmitate provided an increase in the total length and in the weight of the larvae after 15 days of feeding. For head height, differences were observed among the three doses of tested ascorbyl palmitate. The supplementation of ascorbyl palmitate increased the vitamin C concentrations. Although vitamin E has not influenced the development sizes, it acted as a metabolic pro-oxidant, which increased the dehydroascorbic acid.

  4. Multivariate optimization of a synergistic blend of oleoresin sage (Salvia officinalis L.) and ascorbyl palmitate to stabilize sunflower oil.

    Upadhyay, Rohit; Mishra, Hari Niwas

    2016-04-01

    The simultaneous optimization of a synergistic blend of oleoresin sage (SAG) and ascorbyl palmitate (AP) in sunflower oil (SO) was performed using central composite and rotatable design coupled with principal component analysis (PCA) and response surface methodology (RSM). The physicochemical parameters viz., peroxide value, anisidine value, free fatty acids, induction period, total polar matter, antioxidant capacity and conjugated diene value were considered as response variables. PCA reduced the original set of correlated responses to few uncorrelated principal components (PC). The PC1 (eigen value, 5.78; data variance explained, 82.53 %) was selected for optimization using RSM. The quadratic model adequately described the data (R (2) = 0. 91, p  0.05). The contour plot of PC 1 score indicated the optimal synergistic combination of 1289.19 and 218.06 ppm for SAG and AP, respectively. This combination of SAG and AP resulted in shelf life of 320 days at 25 °C estimated using linear shelf life prediction model. In conclusion, the versatility of PCA-RSM approach has resulted in an easy interpretation in multiple response optimizations. This approach can be considered as a useful guide to develop new oil blends stabilized with food additives from natural sources. PMID:27413218

  5. Molecular encapsulation of ascorbyl palmitate in preformed V-type starch and amylose.

    Kong, Lingyan; Ziegler, Gregory R

    2014-10-13

    In the present study, we introduce a simple method to prepare inclusion complexes by "inserting" guest molecules into preformed "empty" V-type amylose helices. Ascorbyl palmitate (AscP) was used as a model guest material to investigate the effect of solvent environment, complexation temperature, annealing and guest concentration on inclusion complex formation. High complexation temperature was not necessary for encapsulating guest molecules in amylose helices, avoiding thermal degradation of guest compounds. This method would also avoid the wasting of guest materials because uncomplexed guest can be reused. It was found in the study that intermediate ethanol and acetone concentrations (generally 40-60%, v/v) at room temperature were appropriate for the complexation between V-amylose and AscP. Annealing, i.e. heat treatment in ethanol solutions at elevated temperatures (45-70 °C), was able to significantly increase the crystallinity of V-amylose and V-starch to as high as 65% and facilitate greater complexation evidenced from higher enthalpies, probably due to more regularly arranged helical cavities in larger crystalline phase. The complexation between V-amylose and AscP was also found to be enhanced with AscP concentration, while the dissociation temperature experienced a slight decrease. PMID:25037350

  6. Study of the influence of ascorbyl palmitate and amiodarone in the stability of unilamellar liposomes.

    Benedini, Luciano; Antollini, Silvia; Fanani, Maria Laura; Palma, Santiago; Messina, Paula; Schulz, Pablo

    2014-01-01

    Amiodarone (AMI) is a low water-solubility drug, which is very useful in the treatment of severe cardiac disease. Its adverse effects are associated with toxicity in different tissues. Several antioxidants have been shown to reduce, and prevent AMI toxicity. The aim of this work was to develop and characterize Dimyristoylphosphatidylcholine (DMPC) liposomal carriers doped with ascorbyl palmitate (Asc16) as antioxidant, in order to either minimize or avoid the adverse effects produced by AMI. The employment of liposomes would avoid the use of cosolvents in AMI formulations, and Asc16 could minimize the adverse effects of AMI. To evaluate the partition and integration of AMI and Asc16 in lipid membranes, penetration studies into DMPC monolayers were carried out. The disturbance of the liposomes membranes was studied by generalized polarization (GP). The stability of liposomes was evaluated experimentally and by means of the Derjaguin-Landau-Verwey-Overbeek (DLVO) theory. The size particle and zeta potential (ζ) values of the liposomes were used for application in calculations for attractive and repulsive forces in DLVO theory. In experimental conditions all of these vesicles showed stability at time 0, but only DMPC + Asc16 10% + AMI 10% liposomes kept their size stable and ζ during 28 days. These results are encouraging and suggest that such systems could be suitable for AMI delivery formulations. PMID:24650150

  7. Nanocarrier with self-antioxidative property for stabilizing and delivering ascorbyl palmitate into skin.

    Janesirisakule, Sirinapa; Sinthusake, Tarit; Wanichwecharungruang, Supason

    2013-08-01

    The concept of a nanocarrier with a self-antioxidative property to deliver and stabilize a labile drug while at the same time providing a free radical scavenging activity is demonstrated. Curcumin was grafted onto a poly(vinyl alcohol) [PV(OH)] chain, and the nanocarriers fabricated from the obtained curcumin-grafted PV(OH) polymer [CUR-PV(OH)] showed a good free radical scavenging activity. Ascorbyl palmitate (AP) could be effectively loaded into the CUR-PV(OH) at 29% by weight. The CUR-PV(OH)-encapsulated AP was 77% more stable than the free (unencapsulated) AP, and 47% more stable than AP encapsulated in the control nanocarrier with no antioxidative property [cinnamoyl-grafted PV(OH); CIN-PV(OH)]. Although coencapsulation of curcumin and AP into CIN-PV(OH) showed some improvement on the AP stability, AP was more stable when encapsulated in CUR-PV(OH). Compared with the free AP, encapsulated AP within the CUR-PV(OH) nanocarriers showed not only a better penetration into pig skin dermis via hair follicle pathway followed by the release and diffusion of the AP, but also a greater AP stability after skin application. Although a proof of principle is shown for CUR-PV(OH) and AP, it is likely that other carriers of the same principal could be designed and applied to different oxidation-sensitive drugs. PMID:23775704

  8. L-抗坏血酸棕榈酸酯的酶法合成%Synthesis of L-ascorbyl palmitate catalyzed by lipase

    李红; 陶静; 李颖

    2011-01-01

    The synthesis of L-ascorbyl palmitate catalyzed by lipase in organic phase was studied.The optimized process conditions,such as enzyme,solvent,temperature,reactants and additive were determined.In the presence of 0.05g Novozyme435 as catalyst,0.3g of 4A molecular sieve and 0.3g of n-Bu4NBr as additive in 3mL tert-amyl alcohol at 50℃,16.6mg/mL of L-ascorbyl palmitate was obtained in the reaction of palmitic acid and VC with the molar ratio of 3:1 after 72h.%详细研究了脂肪酶在有机溶剂中催化合成L-抗坏血酸棕榈酸酯的反应,并且对影响产物浓度的几种主要因素进行讨论(如脂肪酶、溶剂、温度、底物比、添加剂),首次通过加入相转移剂提高反应产物浓度,确定了合成L-抗坏血酸棕榈酸酯的最适反应条件:3mL叔戊醇为溶剂,催化剂为Novozyme435,其最佳用量为0.05g,底物棕榈酸与抗坏血酸摩尔比3:1,0.3g4A分子筛作为吸水剂,0.3g四丁基溴化铵作为相转移剂,反应温度50℃,反应时间72h,得到产物浓度为16.6mg/mL。

  9. HPLC法快速测定乳粉中VC棕榈酸酯的含量%Rapid Determination of Content of Ascorbyl Palmitate in Milk Powder by HPLC

    杜淑霞; 徐丽; 廖延智; 司徒满泉; 李文清

    2015-01-01

    建立了利用高效液相色谱仪快速测定乳粉中Vc棕榈酸酯含量的方法。以含0.1%草酸的乙醇溶液为提取剂,以甲醇和0.15%草酸(体积比为90∶10)为流动相,经Inertsil ODS-SP色谱柱分离,采用二极管阵列检测器,在245 nm波长下进行测定。VC棕榈酸酯的质量浓度在0.5μg/mL~100μg/mL浓度范围内与峰面积呈良好的线性关系。以3倍基线噪声所对应的浓度计算VC棕榈酸酯的检出限为2μg/g。加标回收率在92.01%~105.84%之间,相对标准偏差(n=6)在1.02%~2.70%之间。%The method for rapid determination of the content of ascorbyl palmitate in milk powder by high performance liquid chromatograph (HPLC) was established. It was separated through Inertsil ODS-SP chromatographic column with ethanol containing 0.1%oxalic acid as extraction agent and with methanol and 0.15%oxalic acid ( vol/vol=90∶10) as mobile phase, and then was measured under 245 nm wavelength with a diode array detector. There was a good linear relationship between mass concentration of ascorbyl palmitate and peak area when the mass concentration was from 0.5 μg/mL to 100 μg/mL. Detection limit of ascorbyl palmitate was calculated as 2μg/g by the concentration which corresponded to 3 times baseline noise. Standard addition recovery was 92.01%-105.84%, and relative standard deviation (n=6) was 1.02%-2.70%.

  10. Palmitic Acid and Health: Introduction.

    Agostoni, Carlo; Moreno, Luis; Shamir, Raanan

    2016-09-01

    Interest in the dietary role and metabolic effect of saturated fatty acids has been recently renewed on the basis of epidemiologic observations and economical approach to health and well-being. Saturated fats may favorably increase blood HDL-Cholesterol levels without significant changes of the total cholesterol/HDL-Cholesterol ratio. Also, the negative effect of saturated fat on cardiovascular diseases risk has recently been challenged. Palmitic acid, among all, may have special structural and functional roles in utero and in infancy, and indeed is it is being delivered in a unique form in human milk. Future research should include objective cost-benefit analyses when disentangling the role of saturated fats in dietary recommendations. PMID:25764181

  11. 棕榈酸维生素C酯的酶催化合成%Enzymatic Synthesis of Ascorbyl Palmitate by Transesterification in Non-Aqueous Medium

    安庆大; 董晓丽; 王少君; 马金辉

    2001-01-01

    The synthesis of ascorbyl palmitate from methyl palmitate and ascorbic acid was studied. The reaction was carried out in non-aqueous medium with an immobilized Lipase-LIPOZYM IM as biocatalyst. The influence of the initial molar ratio of substrates, the amount of Lipase, reaction temperature and time was investigated, the optimum of reaction conditions were established. The reaction product has perfectly regioselective.%以棕榈酸甲酯和维生素C为原料,以脂肪酶(LIPOZYM IM)为催化剂,催化合成了棕榈酸维生素C酯.详细研究了几种因素(维生素C与棕榈酸甲酯的摩尔比,反应温度,反应时间及脂肪酶用量)对合成反应的影响,确立了棕榈酸维生素C酯的较佳合成条件:底物摩尔比为3:1,反应温度55℃,反应时间8h,脂肪酶用量为反应体系的3%(重量),产品一次收率为68.2%.

  12. Enzymatic synthesis and application of fatty acid ascorbyl esters

    Stojanović Marija M.; Carević Milica B.; Mihailović Mladen D.; Knežević-Jugović Zorica D.; Petrović Slobodan D.; Bezbradica Dejan I.

    2013-01-01

    Fatty acid ascorbyl esters are liposoluble substances that possess good antioxidative properties. These compounds could be synthesized by using various acyl donors for acylation of vitamin C in reaction catalyzed by chemical means or lipases. Enzymatic process is preferred since it is regioselective, performed under mild reaction conditions, with the obtained product being environmentally friendly. Polar organic solvents, ionic liquids, and supercritical fluids has been successfully use...

  13. Oxidative stability of a heme iron-fortified bakery product: Effectiveness of ascorbyl palmitate and co-spray-drying of heme iron with calcium caseinate.

    Alemán, Mercedes; Bou, Ricard; Tres, Alba; Polo, Javier; Codony, Rafael; Guardiola, Francesc

    2016-04-01

    Fortification of food products with iron is a common strategy to prevent or overcome iron deficiency. However, any form of iron is a pro-oxidant and its addition will cause off-flavours and reduce a product's shelf life. A highly bioavailable heme iron ingredient was selected to fortify a chocolate cream used to fill sandwich-type cookies. Two different strategies were assessed for avoiding the heme iron catalytic effect on lipid oxidation: ascorbyl palmitate addition and co-spray-drying of heme iron with calcium caseinate. Oxidation development and sensory acceptability were monitored in the cookies over one-year of storage at room temperature in the dark. The addition of ascorbyl palmitate provided protection against oxidation and loss of tocopherols and tocotrienols during the preparation of cookies. In general, ascorbyl palmitate, either alone or in combination with the co-spray-dried heme iron, prevented primary oxidation and hexanal formation during storage. The combination of both strategies resulted in cookies that were acceptable from a sensory point of view after 1year of storage. PMID:26593529

  14. Stability of potato chip fried in vegetable oils with different degree of unsaturation. Effect of ascorbyl palmitate during storage

    Torres, R.

    2002-06-01

    Full Text Available Four vegetable oils with different polyunsaturated/saturated fatty acid ratio (P/S: 5.2 for sunflower oil, 3.,4 for canola rapeseed oil, 0.4 for a blend of palm oleic and canola rapeseed oil (80:20, and 0.3 for palm olein were assayed for stability of crisps fried in these oils during storage at 60º C. The action of ascorbyl palmitate with special attention to its synergistic effect on the natural antioxidants was also tested. by addition to the fried potatoes. The evolution of the oxidative stability was measured through peroxide value, quantitation of tocopherols and tocotrienols, and induction time (IT by means of Rancimat. Oil degradation during frying was very low as both polar compound percentages and natural antioxidant had similar levels to those present in refined oils. Evolution of analytical parameters during storage results indicated that oil unsaturation degree or P/S had a much more importance on stability of the product than had the content and type of natural antioxidants and the addition of AP. Nevertheless, addition of AP to the fried potatoes had a significant effect resulting in higher retention of natural antioxidants, higher IT and lower PV at any storage timeSe estudia la evolución de la oxidación a 60º C en patatas fritas con cuatro aceites vegetales de distinta relación ácidos grasos poliinsaturados/saturados (P/S: 5,4 para el aceite de girasol, 3,4 para el aceite de canola, 0,4 para una mezcla de oleína de palma (80 % y aceite de canola (20 % y 0,3 para la oleína de palma. Se estudia igualmente la influencia de la adición de palmitato de ascorbilo (AP durante la conservación del producto frito con especial atención a su efecto sinergista sobre los antioxidantes naturales. La evolución de la oxidación en lotes de patatas, con y sin adición de AP, se determinó mediante las siguientes determinaciones analíticas: índice de peróxidos (PV, cuantificación de tocoferoles y tocotrienoles, y periodos de

  15. 1-丁基-3-甲基咪唑三氟甲磺酸盐催化合成L-抗坏血酸棕榈酸酯%Chemical synthesis of L-ascorbyl palmitate in [ BMIM] OTF

    刘瑞瑾; 纪俊敏

    2011-01-01

    L-抗坏血酸棕榈酸酯是一种高效安全的脂溶性抗氧化剂,是近几年被国际上认可的一种新型食品添加剂,广泛地用于粮油、食品、医药、保健品化妆品等领域.1 -丁基-3-甲基咪唑三氟甲磺酸盐( [BMIM] OTF)是一种常用的室温离子液体催化剂,可有效催化乙酰化反应,具有高效、底物普适性好和对水稳定的特点,本文研究了 [BMIM] OTF催化棕榈酸与L-抗坏血酸合成L-抗坏血酸棕榈酸酯,考察了[BMIM] OTF的用量、反应物摩尔比、反应温度、反应时间、对反应转化率的影响.采用正交设计实验法优化工艺条件,得到较佳工艺条件,离子液体用量为反应物质量的3%,棕榈酸∶维生素C为1∶1.2,反应温度为30℃,反应时间为24h,产率达到66.44%.产品质量符合GB16314 - 1996标准.%L - ascorbyl palmitate is a safe and highly efficient lipophilic antioxidant. It is an widely accepted new food antioxidant in recent years and can be used in oil, food, medicine, health protection and cosmetics. 1 - butyl - 3 -methylimidazolium trifluoromethanesulfonate ( [ BMIM] OTF) is a versatile ionic liquid promoter in the room temperature. It can effectively improve acetylization and has the advantage on substrate universality and water soluble stability. In this paper we use [ BMIM ] OTF as a promoter to synthesise L - ascorbyl palmitate. We discussed the impact of dosage of ionic liquid, mole ratio of reaction, temperature and time on the conversion rate. The optimized conditions by orthogonal experiment was: the amount of ionic liquids for the quality of reactant was 3% , the ratio of palmitic acid : VC was 1 : 1. 2, the reaction temperature was 30℃ , and the reaction time was 24h. Under the above condition, L - ascorbyl palmitate conversion rate was 66. 44% . The product was met the requirement of GB16314 - 1996.

  16. Enzymatic synthesis and application of fatty acid ascorbyl esters

    Stojanović Marija M.

    2013-01-01

    Full Text Available Fatty acid ascorbyl esters are liposoluble substances that possess good antioxidative properties. These compounds could be synthesized by using various acyl donors for acylation of vitamin C in reaction catalyzed by chemical means or lipases. Enzymatic process is preferred since it is regioselective, performed under mild reaction conditions, with the obtained product being environmentally friendly. Polar organic solvents, ionic liquids, and supercritical fluids has been successfully used as a reaction medium, since commonly used solvents with high Log P values are inapplicable due to ascorbic acid high polarity. Acylation of vitamin C using fatty acids, their methyl-, ethyl-, and vinyl esters, as well as triglycerides has been performed, whereas application of the activated acyl donors enabled higher molar conversions. In each case, majority of authors reported that using excessive amount of the acyl donor had positive effect on yield of product. Furthermore, several strategies have been employed for shifting the equilibrium towards the product by water content control. These include adjusting the initial water activity by pre-equilibration of reaction mixture, enzyme preparation with water vapor of saturated salt solutions, and the removal of formed water by the addition of molecular sieves or salt hydrate pairs. The aim of this article is to provide a brief overview of the procedures described so far for the lipase-catalyzed synthesis of fatty acid ascorbyl esters with emphasis on the potential application in food, cosmetics, and pharmaceutics. Furthermore, it has been pointed out that the main obstacles for process commercialization are long reaction times, lack of adequate purification methods, and high costs of lipases. Thus, future challenges in this area are testing new catalysts, developing continuous processes for esters production, finding cheaper acyl donors and reaction mediums, as well as identifying standard procedures for

  17. Coating of peanuts with edible whey protein film containing alpha-tocopherol and ascorbyl palmitate.

    Han, J H; Hwang, H-M; Min, S; Krochta, J M

    2008-10-01

    Physical properties of whey protein isolate (WPI) coating solution incorporating ascorbic palmitate (AP) and alpha-tocopherol (tocopherol) were characterized, and the antioxidant activity of dried WPI coatings against lipid oxidation in roasted peanuts were investigated. The AP and tocopherol were mixed into a 10% (w/w) WPI solution containing 6.7% glycerol. Process 1 (P1) blended an AP and tocopherol mixture directly into the WPI solution using a high-speed homogenizer. Process 2 (P2) used ethanol as a solvent for dissolving AP and tocopherol into the WPI solution. The viscosity and turbidity of the WPI coating solution showed the Newtonian fluid behavior, and 0.25% of critical concentration of AP in WPI solution rheology. After peanuts were coated with WPI solutions, color changes of peanuts were measured during 16 wk of storage at 25 degrees C, and the oxidation of peanuts was determined by hexanal analysis using solid-phase micro-extraction samplers and GC-MS. Regardless of the presence of antioxidants in the coating layer, the formation of hexanal from the oxidation of peanut lipids was reduced by WPI coatings, which indicates WPI coatings protected the peanuts from oxygen permeation and oxidation. However, the incorporation of antioxidants in the WPI coating layer did not show a significant difference in hexanal production from that of WPI coating treatment without incorporation of antioxidants. PMID:19019105

  18. Adsorption and inhibition effect of Ascorbyl palmitate on corrosion of carbon steel in ethanol blended gasoline containing water as a contaminant

    Graphical abstract: -- Highlights: •Inhibition performance was studied using weight loss and EIS methods. •The addition of ethanol and water to gasoline increase the corrosion rate of C-steel. •Ascorbyl palmitate has good inhibition efficiency for C-steel in blend fuel. •Efficiency more than 96% was obtained with 120 mg l−1 AP at 298 K. •The adsorption of AP on C-steel surface obeys Langmuir adsorption isotherm. -- Abstract: The adsorption and inhibition effect of Ascorbyl palmitate (AP) on carbon steel in ethanol blended gasoline containing water as a contaminant (GE10 + 1%water) was studied by weight loss and electrochemical impedance spectroscopic (EIS) techniques. The results showed that the addition of ethanol and water to gasoline increase the corrosion rate of carbon steel. AP inhibits the corrosion of carbon steel in (GE10 + 1% water) solution to a remarkable extent. The adsorption of AP on the carbon steel surface was found to obey the Langmuir adsorption isotherm model. The values of activation energy (Ea) and various thermodynamic parameters were calculated and discussed

  19. Final report of the safety assessment of L-Ascorbic Acid, Calcium Ascorbate, Magnesium Ascorbate, Magnesium Ascorbyl Phosphate, Sodium Ascorbate, and Sodium Ascorbyl Phosphate as used in cosmetics.

    Elmore, Amy R

    2005-01-01

    L-Ascorbic Acid, Calcium Ascorbate, Magnesium Ascorbate, Magnesium Ascorbyl Phosphate, Sodium Ascorbate, and Sodium Ascorbyl Phosphate function in cosmetic formulations primarily as antioxidants. Ascorbic Acid is commonly called Vitamin C. Ascorbic Acid is used as an antioxidant and pH adjuster in a large variety of cosmetic formulations, over 3/4 of which were hair dyes and colors at concentrations between 0.3% and 0.6%. For other uses, the reported concentrations were either very low (Ascorbate and Magnesium Ascorbate are described as antioxidants and skin conditioning agents--miscellaneous for use in cosmetics, but are not currently used. Sodium Ascorbyl Phosphate functions as an antioxidant in cosmetic products and is used at concentrations ranging from 0.01% to 3%. Magnesium Ascorbyl Phosphate functions as an antioxidant in cosmetics and was reported being used at concentrations from 0.001% to 3%. Sodium Ascorbate also functions as an antioxidant in cosmetics at concentrations from 0.0003% to 0.3%. Related ingredients (Ascorbyl Palmitate, Ascorbyl Dipalmitate, Ascorbyl Stearate, Erythorbic Acid, and Sodium Erythorbate) have been previously reviewed by the Cosmetic Ingredient Review (CIR) Expert Panel and found "to be safe for use as cosmetic ingredients in the present practices of good use." Ascorbic Acid is a generally recognized as safe (GRAS) substance for use as a chemical preservative in foods and as a nutrient and/or dietary supplement. Calcium Ascorbate and Sodium Ascorbate are listed as GRAS substances for use as chemical preservatives. L-Ascorbic Acid is readily and reversibly oxidized to L-dehydroascorbic acid and both forms exist in equilibrium in the body. Permeation rates of Ascorbic Acid through whole and stripped mouse skin were 3.43 +/- 0.74 microg/cm(2)/h and 33.2 +/- 5.2 microg/cm(2)/h. Acute oral and parenteral studies in mice, rats, rabbits, guinea pigs, dogs, and cats demonstrated little toxicity. Ascorbic Acid and Sodium Ascorbate acted

  20. L-抗坏血酸脂肪酸酯抗氧化活性%Study on the Antioxidant Activities of L-ascorbyl Fatty Acid Esters

    刘建伟; 赵海珍; 吕凤霞; 别小妹; 张充; 陆兆新; 彭杨

    2011-01-01

    In vitro antioxidant activities of L-ascorbyl fatty acid esters were studied by the items of hydroxyl radical system, superoxide anion free radical system, system of DPPH · , and reducing power.Its antioxidant effects was further evaluated by adding into the lard and bead oil.The results indicated that L-ascorbyl fatty acid esters within the given concentration range in doseeffect relationship showed good antioxidant activities on both the clearance of hydroxyl radical,superoxide anion free radical and DPPH · and the reducing power.Furthermore, the antioxidant activities of L-ascorbyl fatty acid esters were comparable with that of L-ascorbyl palmitate.When 0.2% (w/w) of L-ascorbyl fatty acid esters were added in the lard for a 20 h forced oxidation at 100 ℃, the POV of lard was 42.8 meq/kg, which illustrated L-ascorbyl fatty acid esters had significant antioxidant activities.When 0.2% (w/w) of L-ascorbyl fatty acid esters were added in the soybean oil for a 14 h forced oxidation at 100 ℃, the POV of soybean oil was 11.9 meq/ kg.The antioxidant ability of L-ascorbyl fatty acid esters for soybean oil was higher than that of TBHQ, but was close with that of L-ascorbyl palmitate.Thus, L-ascorbyl fatty acid esters were demonstrated to be potential food antioxidants.%从羟基自由基体系、超氧阴离子自由基体系、二苯苦味肼基自由基体系及还原力测试等方面研究L-抗坏血酸脂肪酸酯(VC脂肪酸酯)体外抗氧化活性,并将其添加到猪油和大豆油当中,评价其抗氧化效果.结果表明,在一定的质量浓度范围内,VC脂肪酸酯对羟自由基、超氧阴离子自由基、DPPH自由基均有较好的清除效果,还原能力也较强,并呈一定量效关系,其抗氧化活性与L-抗坏血酸棕榈酸酯相当.VC脂肪酸酯在猪油中的添加质量分数为0.2%,100℃下强制氧化20h时,猪油的过氧化值为42.8 meq/kg,具有明显的抗氧化活性;在大豆油中添加质量分数0.2%,

  1. Enzymatic Synthesis of l-Ascorbyl Fatty Acid Esters Under Ultrasonic Irradiation and Comparison of Their Antioxidant Activity and Stability.

    Jiang, Chen; Lu, Yuyun; Li, Zhuo; Li, Cunzhi; Yan, Rian

    2016-06-01

    A series of novel l-ascorbyl fatty acid esters were synthesized by catalization of Novozym(®) 435 under ultrasonic irradiation and characterized by infrared spectroscopy, electrospray ionization mass spectra, and nuclear magnetic resonance. Their properties especially antioxidant activity and stability were investigated. The results showed that the reducing power, the scavenging activity of hydroxyl radical and 2,2-diphenyl-1-picrylhydrazyl radical were decreased with the increase of the number of carbon atoms in fatty acid. The hydroxyl radical scavenging activity and reducing power of l-ascorbyl saturated fatty acid esters were better than that of tert-butylhydroquinone. The induction period in lipid oxidation of l-ascorbyl saturated fatty acid esters and tert-butylhydroquinone were longer than that of l-ascorbyl unsaturated fatty acid esters and l-ascorbic acid both in soybean oil and lard. Besides, the l-ascorbyl fatty acid esters showed different stabilities in different conditions by comparing with l-ascorbic acid, and the l-ascorbyl saturated fatty acid esters were more stable than l-ascorbyl unsaturated fatty acid esters in ethanol solution. PMID:27100741

  2. Uptake of palmitic acid by rabbit alveolar type II cells

    Alveolar type II cells require a source of palmitic acid for synthesis of dipalmitoyl phosphatidylcholine (DPPC), a major constituent of pulmonary surfactant. Previous studies indicated that maximal rates of DPPC synthesis are achieved only if exogenous palmitate is available to the type II cell. Little is known of the mechanisms by which fatty acids enter type II cells. To determine if uptake is mediated by a membrane carrier system, as described in other cell types, we examined the kinetics of palmitate uptake. Using freshly isolated rabbit type II cells, we demonstrated that radiolabeled palmitate uptake was maximal and linear for 45 s; after 1 min the apparent rate of uptake declined. The initial uptake phase was taken as a measure of cellular fatty acid influx because intracellular radiolabeled palmitate remained 80% nonesterified at this time but was 55% esterified by 2 min. Cellular influx of palmitate showed saturation kinetics with increasing concentration of nonalbumin bound palmitate. Michaelis constant was 52.6 nM, and maximum velocity was 152 pmol.10(6) cells-1.min-1. The hypothesis that saturable cellular influx of palmitate is likely linked to the previously identified membrane fatty acid binding protein (MFABP) was supported by Western-blot analysis of rat lung tissue with an antibody to MFABP that demonstrated the presence of this carrier protein in lung tissue. These data suggest that palmitate uptake by type II cells is saturable and may be mediated by a membrane-associated carrier as described in other cell types

  3. Palmitic Acid in Early Human Development.

    Innis, Sheila M

    2016-09-01

    Palmitic acid (16:0) is a saturated fatty acid present in the diet and synthesized endogenously. Although often considered to have adverse effects on chronic disease in adults, 16:0 is an essential component of membrane, secretory, and transport lipids, with crucial roles in protein palmitoylation and signal molecules. At birth, the term infant is 13-15% body fat, with 45-50% 16:0, much of which is derived from endogenous synthesis in the fetus. After birth, the infant accumulates adipose tissue at high rates, reaching 25% body weight as fat by 4-5 months age. Over this time, human milk provides 10% dietary energy as 16:0, but in unusual triglycerides with 16:0 on the glycerol center carbon. This paper reviews the synthesis and oxidation of 16:0 and possible reasons why the infant is endowed with large amounts of fat and 16:0. The marked deviations in tissues with displacement of 16:0 that can occur in infants fed vegetable oil formulas is introduced. Assuming fetal fatty acid synthesis and the unusual delivery of 16:0 in human milk evolved to afford survival advantage to the neonate, it is timely to question if 16:0 is an essential component of tissue lipids whereby both deficiency and excess are detrimental. PMID:25764297

  4. Application of l-ascorbic acid and its derivatives (sodium ascorbyl phosphate and magnesium ascorbyl phosphate) in topical cosmetic formulations: stability studies

    The present study aimed to formulate and subsequently evaluate a topical skin-care cream (o/w emulsion) from l-ascorbic acid and its derivatives (sodium ascorbyl phosphate and magnesium ascorbyl phosphate) at 2% versus its vehicle (Control). Formulations were developed by entrapping it in the oily phase of o/w emulsion and were stored at 8 degree C, 25 degree C and 40 degree C (in incubator) for a period of four weeks to investigate their stability. In the physical analysis, the evaluation parameters consisted of color, smell, phase separation, centrifugation, and liquefaction. Chemical stability of both derivatives was established by HPLC analysis. In the chemical analysis, the formulation with sodium ascorbyl phosphate was more stable than those with magnesium ascorbyl phosphate and l-ascorbic acid. The microbiological stability of the formulations was also evaluated. The findings indicated that the formulations with l-ascorbic acid and its derivatives were efficient against the proliferation of various spoilage microorganisms, including aerobic plate counts as well as Pseudomonas aeruginosa, Staphylococcus aureus, and yeast and mold counts. The results presented in this work showed good stability throughout the experimental period. Newly formulated emulsion proved to exhibit a number of promising properties and attributes that might open new opportunities for the construction of more efficient, safe, and cost-effective skin-care, cosmetic, and pharmaceutical products. (author)

  5. Protective effects of equimolar mixtures of monomer and dimer of dehydrozingerone with α-tocopherol and/or ascorbyl palmitate during bulk lipid autoxidation.

    Kancheva, Vessela; Slavova-Kazakova, Adriana; Fabbri, Davide; Dettori, Maria Antonietta; Delogu, Giovanna; Janiak, Michał; Amarowicz, Ryszard

    2014-08-15

    Protective effects of recently synthesised dehydrozingerone, M1OH (which is one half of the molecule of curcumin) and dimer of dehydrozingerone, D1(OH)2, as individual compounds (1 mM) and as equimolar binary (1:1) and ternary (1:1:1) mixtures with α-tocopherol (TOH) and/or ascorbyl palmitate (AscPH), were studied during bulk lipid autoxidation at 80 °C. The highest oxidation stability of lipid substrate, in the presence of individual compounds, was found for TOH, followed by D1(OH)2 and M1OH, determined from the main kinetic parameters (antioxidant efficiency, reactivity and capacity). AscPH did not show any protective effect. Synergism was obtained for the binary mixtures of (TOH+AscPH) [42.4%], (M1OH+TOH) [32.4%] and (M1OH+AscPH) [35.6%] and for the ternary mixture of (M1OH+TOH+AscPH) [28.7%]. Different protective effects observed were explained on the basis (of results) of TOH regeneration and its content determined by HPLC. These antioxidant binary and ternary mixtures can be used as functional components of foods with health-promoting effects. PMID:24679780

  6. Defective [U-14 C] palmitic acid oxidation in Duchenne muscular dystrophy

    Compared with normal skeletal muscle, muscle from patients with Duchenne dystrophy had decreased [U-14 C] palmitic acid oxidation. [1-14 C] palmitic acid oxidation was normal. These results may indicate a defect in intramitochondrial fatty acid oxidation

  7. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

    Kunikazu Moribe

    2011-01-01

    Full Text Available Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs or carrier components. Ascorbyl n-alkyl fatty acid derivatives have been formulated as antioxidants or anticancer drugs for nanoparticle formulations such as micelles, microemulsions, and liposomes. ASC-P vesicles called aspasomes are submicron-sized particles that can encapsulate hydrophilic drugs. Several transdermal and injectable formulations of ascorbyl n-alkyl fatty acid derivatives were used, including ascorbyl palmitate.

  8. Highly efficient enzymatic synthesis of an ascorbyl unstaturated fatty acid ester with ecofriendly biomass-derived 2-methyltetrahydrofuran as cosolvent.

    Hu, Ying-Dan; Qin, Ye-Zhi; Li, Ning; Zong, Min-Hua

    2014-01-01

    Enzymatic synthesis of ascorbyl undecylenate, an unsaturated fatty acid ester of ascorbic acid, was reported with biomass-derived 2-methyltetrahydrofuran (MeTHF) as the cosolvent. Of the immobilized lipases tested, Candida antarctica lipase B (CAL-B) showed the highest activity for enzymatic synthesis of ascorbyl undecylenate. Effect of reaction media on the enzymatic reaction was studied. The cosolvent mixture, t-butanol-MeTHF (1:4, v/v) proved to be the optimal medium, in which not only ascorbic acid had moderate solubility, but also CAL-B showed a high activity, thus addressing the major problem of the solvent conflict for dissolving substrate and keeping satisfactory enzyme activity. In addition, the enzyme was much more stable in MeTHF and t-butanol-MeTHF (1:4) than in previously widely used organic solvents, t-butanol, 2-methyl-2-butanol, and acetone. The much higher initial reaction rate in this cosolvent mixture may be rationalized by the much lower apparent activation energy of this enzymatic reaction (26.6 vs. 38.1-39.1 kJ/mol) and higher enzyme catalytic efficiency (Vmax /Km , 8.4 vs. 1.3-1.4 h(-1) ). Ascorbyl undecylenate was obtained with the yields of 84-89% and 6-regioselectivity of >99% in t-butanol-MeTHF (1:4) at supersaturated substrate concentrations (60 and 100 mM) after 5-8 h. PMID:24891225

  9. Synthesis of ascorbyl oleate by transesterification of olive oil with ascorbic acid in polar organic media catalyzed by immobilized lipases.

    Moreno-Perez, Sonia; Filice, Marco; Guisan, Jose M; Fernandez-Lorente, Gloria

    2013-09-01

    The reaction of transesterification between oils (e.g., olive oil) and ascorbic acid in polar anhydrous media (e.g., tert-amyl alcohol) catalyzed by immobilized lipases for the preparation of natural liposoluble antioxidants (e.g., ascorbyl oleate) was studied. Three commercial lipases were tested: Candida antarctica B lipase (CALB), Thermomyces lanuginosus lipase (TLL) and Rhizomucor miehei lipase (RML). Each lipase was immobilized by three different protocols: hydrophobic adsorption, anionic exchange and multipoint covalent attachment. The highest synthetic yields were obtained with CALB adsorbed on hydrophobic supports (e.g., the commercial derivative Novozym 435). The rates and yields of the synthesis of ascorbyl oleate were higher when using the solvent dried with molecular sieves, at high temperatures (e.g. 45°C) and with a small excess of oil (2 mol of oil per mol of ascorbic acid). The coating of CALB derivatives with polyethyleneimine (PEI) improved its catalytic behavior and allowed the achievement of yields of up to 80% of ascorbyl oleate in less than 24h. CALB adsorbed on a hydrophobic support and coated with PEI was 2-fold more stable than a non-coated derivative and one hundred-fold more stable than the best TLL derivative. The best CALB derivative exhibited a half-life of 3 days at 75°C in fully anhydrous media, and this derivative maintained full activity after 28 days at 45°C in dried tert-amyl alcohol. PMID:23891831

  10. Influence of Palmitic Acid and Amino Acids Addition on Iturin A Productivity by Bacillus subtilis RB14-CS

    YULIAR

    2005-01-01

    The aim of this study was to observe the influence of palmitic acid and amino acids on enhancement of iturin A productivity using Bacillus subtilis RB14-CS. The concentrations of palmitic acid examined were 0.8%, 1.6%, and 3.2%. A good yield was observed when 1.6% palmitic acid was added to Polypepton S medium. The production of iturin A increased about 18% than the control. Addition of 3.2% palmitic acid was not effective on iturin A production. It gave lower pH and slightly higher viable ce...

  11. Studies on Lipase-catalyzed Synthesis of L-ascorbyl Palmitate in Non-aqueous Phase%非水相脂肪酶催化合成L-抗坏血酸棕榈酸酯的研究Ⅰ

    汤鲁宏; 张浩

    2000-01-01

    The investigation on the reaction media and lipases (NOVO435、MML、LIPOLASE、PPL) for enzymatic synthesis of L-ascorbyl palmitate as well as the factors effecting initial rate of synthesis reaction (rotation speed, temperature, water content,enzyme concentration,and substrate concentration) is presented. Among these investigated solvents and lipases, amyl alcohol and NOVO435 is the optimum pair. The reaction conditions have been optimized:200r/min, 55℃ , water content = 0, the amount of enzyme= 12.5 % of the substrate' s quantity.%对催化合成L-抗坏血酸棕榈酸酯反应的脂肪酶(NOVO435、MML、LIPOLASE、PPL)和反应介质进行比较,得出最佳酶种为NOVO435,最佳介质为叔戊醇;同时对影响合成L-抗坏血酸棕榈酸酯反应的初速度的因素(转速、温度、水分含量、酶浓度和底物浓度)进行了探讨,确定了最适反应条件:转速为200r/min,温度为55℃,水分含量为0,酶浓度为12.5%。

  12. Biological and Nutritional Properties of Palm Oil and Palmitic Acid: Effects on Health

    Annamaria Mancini

    2015-09-01

    Full Text Available A growing body of evidence highlights the close association between nutrition and human health. Fat is an essential macronutrient, and vegetable oils, such as palm oil, are widely used in the food industry and highly represented in the human diet. Palmitic acid, a saturated fatty acid, is the principal constituent of refined palm oil. In the last few decades, controversial studies have reported potential unhealthy effects of palm oil due to the high palmitic acid content. In this review we provide a concise and comprehensive update on the functional role of palm oil and palmitic acid in the development of obesity, type 2 diabetes mellitus, cardiovascular diseases and cancer. The atherogenic potential of palmitic acid and its stereospecific position in triacylglycerols are also discussed.

  13. System Development from Organic Solvents to Ionic Liquids for Synthesiz-ing Ascorbyl Esters with Conjugated Linoleic Acids

    Yang, Zhiyong; Schultz, Lise; Guo, Zheng;

    2012-01-01

    The aim of this paper is to screen suitable reaction systems for the modification of antioxidants through enzy-matic synthesis. Enzymatic esterification of ascorbic acid with conjugated linoleic acid (CLA) was investigated as a mod-el. Four organic solvents and five different enzymes were evaluated....... Results show that only Novozym® 435 turned out to be a useful enzymatic preparation for the production of ascorbyl-CLA ester. The optimum reaction conditions in the or-ganic solvent system were 4 h at 55°C and at a molar ratio of 5 (CLA/ascorbic acid). The esterification reaction was trans-ferred to an...... ascorbyl-CLA ester when using Novozym® 435 as biocatalyst. It was possible to significantly increase the productivity (150 g/l) through the increase of ascorbic acid sol-ubility in ionic liquids by super saturation together with the increase of reaction temperature to 70°C, far beyond than that in organic...

  14. Influence of fatty acid on lipase-catalyzed synthesis of ascorbyl esters and their free radical scavenging capacity.

    Stojanović, Marija; Carević, Milica; Mihailović, Mladen; Veličković, Dušan; Dimitrijević, Aleksandra; Milosavić, Nenad; Bezbradica, Dejan

    2015-01-01

    Fatty acid (FA) ascorbyl esters are recently emerging food, cosmetic, and pharmaceutical additives, which can be prepared in an eco-friendly way by using lipases as catalysts. Because they are amphiphilic molecules, which possess high free radical scavenging capacity, they can be applied as liposoluble antioxidants as well as emulsifiers and biosurfactants. In this study, the influence of a wide range of acyl donors on ester yield in lipase-catalyzed synthesis and ester antioxidant activity was examined. Among saturated acyl donors, higher yields and antioxidant activities of esters were achieved when short-chain FAs were used. Oleic acid gave the highest yield overall and its ester exhibited a high antioxidant activity. Optimization of experimental factors showed that the highest conversion (60.5%) in acetone was achieved with 5 g L(-1) of lipase, 50 mM of vitamin C, 10-fold molar excess of oleic acid, and 0.7 mL L(-1) of initial water. Obtained results showed that even short- and medium-chain ascorbyl esters could be synthesized with high yields and retained (or even exceeded) free radical scavenging capacity of l-ascorbic acid, indicating prospects of broadening their application in emulsions and liposomes. PMID:25224149

  15. Phase equilibrium measurements and modelling of ternary system (carbon dioxide + ethanol + palmitic acid)

    This work reports phase equilibrium measurements for the ternary system (palmitic acid + ethanol + CO2). The motivation of this research relies on the fact that palmitic acid is the major compound of several vegetable oils. Besides, equilibrium data for palmitic acid in carbon dioxide using ethanol as co-solvent are scarce in the literature. Phase equilibrium experiments were performed using a high-pressure variable-volume view cell over the temperature range of (303 to 343) K and pressures up to 20 MPa and mole fraction of palmitic acid from 0.0199 to 0.2930. Vapour-liquid and solid-fluid transitions were visually observed for the system studied. The Peng-Robinson equation of state, with the classical van der Waals quadratic mixing rule was employed for thermodynamic modelling of the system investigated with a satisfactory agreement between experimental and calculated values.

  16. The mechanism of downregulation of apolipoprotein M mediated by palmitic acid

    施媛萍

    2014-01-01

    Objective To examine whether palmitic acid downregulates ApoM expression and further to investigate its mechanism.Methods Human hepatoma cell line,HepG2 cells were treated with the media containing palmitic acid(1 mmol/L)and/or PI-3K inhibitor LY294002(10μmol/L),protein kinase C inhibitor GF109203X(GFX,2μmol/L)and/or PARβ/δantagonist GSK3787

  17. A liquid crystal of ascorbyl palmitate, used as vaccine platform, provides sustained release of antigen and has intrinsic pro-inflammatory and adjuvant activities which are dependent on MyD88 adaptor protein.

    Sánchez Vallecillo, María F; Minguito de la Escalera, María M; Aguirre, María V; Ullio Gamboa, Gabriela V; Palma, Santiago D; González-Cintado, Leticia; Chiodetti, Ana L; Soldano, Germán; Morón, Gabriel; Allemandi, Daniel A; Ardavín, Carlos; Pistoresi-Palencia, María C; Maletto, Belkys A

    2015-09-28

    Modern subunit vaccines require the development of new adjuvant strategies. Recently, we showed that CpG-ODN formulated with a liquid crystal nanostructure formed by self-assembly of 6-O-ascorbyl palmitate (Coa-ASC16) is an attractive system for promoting an antigen-specific immune response to weak antigens. Here, we showed that after subcutaneous injection of mice with near-infrared fluorescent dye-labeled OVA antigen formulated with Coa-ASC16, the dye-OVA was retained at the injection site for a longer period than when soluble dye-OVA was administered. Coa-ASC16 alone elicited a local inflammation, but how this material triggers this response has not been described yet. Although it is known that some materials used as a platform are not immunologically inert, very few studies have directly focused on this topic. In this study, we explored the underlying mechanisms concerning the interaction between Coa-ASC16 and the immune system and we found that the whole inflammatory response elicited by Coa-ASC16 (leukocyte recruitment and IL-1β, IL-6 and IL-12 production) was dependent on the MyD88 protein. TLR2, TLR4, TLR7 and NLRP3-inflammasome signaling were not required for induction of this inflammatory response. Coa-ASC16 induced local release of self-DNA, and in TLR9-deficient mice IL-6 production was absent. In addition, Coa-ASC16 revealed an intrinsic adjuvant activity which was affected by MyD88 and IL-6 absence. Taken together these results indicate that Coa-ASC16 used as a vaccine platform is effective due to the combination of the controlled release of antigen and its intrinsic pro-inflammatory activity. Understanding how Coa-ASC16 works might have significant implications for rational vaccine design. PMID:26188153

  18. Cyclosporine A and palmitic acid treatment synergistically induce cytotoxicity in HepG2 cells

    Luo, Yi, E-mail: yi.luo@pfizer.com; Rana, Payal; Will, Yvonne

    2012-06-01

    Immunosuppressant cyclosporine A (CsA) treatment can cause severe side effects. Patients taking immunosuppressant after organ transplantation often display hyperlipidemia and obesity. Elevated levels of free fatty acids have been linked to the etiology of metabolic syndromes, nonalcoholic fatty liver and steatohepatitis. The contribution of free fatty acids to CsA-induced toxicity is not known. In this study we explored the effect of palmitic acid on CsA-induced toxicity in HepG2 cells. CsA by itself at therapeutic exposure levels did not induce detectible cytotoxicity in HepG2 cells. Co-treatment of palmitic acid and CsA resulted in a dose dependent increase in cytotoxicity, suggesting that fatty acid could sensitize cells to CsA-induced cytotoxicity at the therapeutic doses of CsA. A synergized induction of caspase-3/7 activity was also observed, indicating that apoptosis may contribute to the cytotoxicity. We demonstrated that CsA reduced cellular oxygen consumption which was further exacerbated by palmitic acid, implicating that impaired mitochondrial respiration might be an underlying mechanism for the enhanced toxicity. Inhibition of c-Jun N-terminal kinase (JNK) attenuated palmitic acid and CsA induced toxicity, suggesting that JNK activation plays an important role in mediating the enhanced palmitic acid/CsA-induced toxicity. Our data suggest that elevated FFA levels, especially saturated FFA such as palmitic acid, may be predisposing factors for CsA toxicity, and patients with underlying diseases that would elevate free fatty acids may be susceptible to CsA-induced toxicity. Furthermore, hyperlipidemia/obesity resulting from immunosuppressive therapy may aggravate CsA-induced toxicity and worsen the outcome in transplant patients. -- Highlights: ► Palmitic acid and cyclosporine (CsA) synergistically increased cytotoxicity. ► The impairment of mitochondrial functions may contribute to the enhanced toxicity. ► Inhibition of JNK activity attenuated

  19. Cyclosporine A and palmitic acid treatment synergistically induce cytotoxicity in HepG2 cells

    Immunosuppressant cyclosporine A (CsA) treatment can cause severe side effects. Patients taking immunosuppressant after organ transplantation often display hyperlipidemia and obesity. Elevated levels of free fatty acids have been linked to the etiology of metabolic syndromes, nonalcoholic fatty liver and steatohepatitis. The contribution of free fatty acids to CsA-induced toxicity is not known. In this study we explored the effect of palmitic acid on CsA-induced toxicity in HepG2 cells. CsA by itself at therapeutic exposure levels did not induce detectible cytotoxicity in HepG2 cells. Co-treatment of palmitic acid and CsA resulted in a dose dependent increase in cytotoxicity, suggesting that fatty acid could sensitize cells to CsA-induced cytotoxicity at the therapeutic doses of CsA. A synergized induction of caspase-3/7 activity was also observed, indicating that apoptosis may contribute to the cytotoxicity. We demonstrated that CsA reduced cellular oxygen consumption which was further exacerbated by palmitic acid, implicating that impaired mitochondrial respiration might be an underlying mechanism for the enhanced toxicity. Inhibition of c-Jun N-terminal kinase (JNK) attenuated palmitic acid and CsA induced toxicity, suggesting that JNK activation plays an important role in mediating the enhanced palmitic acid/CsA-induced toxicity. Our data suggest that elevated FFA levels, especially saturated FFA such as palmitic acid, may be predisposing factors for CsA toxicity, and patients with underlying diseases that would elevate free fatty acids may be susceptible to CsA-induced toxicity. Furthermore, hyperlipidemia/obesity resulting from immunosuppressive therapy may aggravate CsA-induced toxicity and worsen the outcome in transplant patients. -- Highlights: ► Palmitic acid and cyclosporine (CsA) synergistically increased cytotoxicity. ► The impairment of mitochondrial functions may contribute to the enhanced toxicity. ► Inhibition of JNK activity attenuated

  20. Interaction of Palmitic Acid with Metoprolol Succinate at the Binding Sites of Bovine Serum Albumin

    Mashiur Rahman

    2014-12-01

    Full Text Available Purpose: The aim of this study was to characterize the binding profile as well as to notify the interaction of palmitic acid with metoprolol succinate at its binding site on albumin. Methods: The binding of metoprolol succinate to bovine serum albumin (BSA was studied by equilibrium dialysis method (ED at 27°C and pH 7.4, in order to have an insight in the binding chemistry of the drug to BSA in presence and absence of palmitic acid. The study was carried out using ranitidine as site-1 and diazepam as site-2 specific probe. Results: Different analysis of binding of metoprolol succinate to bovine serum albumin suggested two sets of association constants: high affinity association constant (k1 = 11.0 x 105 M-1 with low capacity (n1 = 2 and low affinity association (k2 = 4.0×105 M-1 constant with high capacity (n2 = 8 at pH 7.4 and 27°C. During concurrent administration of palmitic acid and metoprolol succinate in presence or absence of ranitidine or diazepam, it was found that palmitic acid displaced metoprolol succinate from its binding site on BSA resulting reduced binding of metoprolol succinate to BSA. The increment in free fraction of metoprolol succinate was from 26.27% to 55.08% upon the addition of increased concentration of palmitic acid at a concentration of 0×10-5 M to 16×10-5 M. In presence of ranitidine and diazepam, palmitic acid further increases the free fraction of metoprolol succinate from 33.05% to 66.95% and 40.68% to 72.88%, respectively. Conclusion: This data provided the evidence of interaction at higher concentration of palmitic acid at the binding sites on BSA, which might change the pharmacokinetic properties of metoprolol succinate.

  1. Palmitic acid analogs exhibit nanomolar binding affinity for the HIV-1 CD4 receptor and nanomolar inhibition of gp120-to-CD4 fusion.

    Elena E Paskaleva

    Full Text Available BACKGROUND: We recently reported that palmitic acid (PA is a novel and efficient CD4 fusion inhibitor to HIV-1 entry and infection. In the present report, based on in silico modeling of the novel CD4 pocket that binds PA, we describe discovery of highly potent PA analogs with increased CD4 receptor binding affinities (K(d and gp120-to-CD4 inhibition constants (K(i. The PA analogs were selected to satisfy Lipinski's rule of drug-likeness, increased solubility, and to avoid potential cytotoxicity. PRINCIPAL FINDINGS: PA analog 2-bromopalmitate (2-BP was most efficacious with K(d approximately 74 nM and K(i approximately 122 nM, ascorbyl palmitate (6-AP exhibited slightly higher K(d approximately 140 nM and K(i approximately 354 nM, and sucrose palmitate (SP was least efficacious binding to CD4 with K(d approximately 364 nM and inhibiting gp120-to-CD4 binding with K(i approximately 1486 nM. Importantly, PA and its analogs specifically bound to the CD4 receptor with the one to one stoichiometry. SIGNIFICANCE: Considering observed differences between K(i and K(d values indicates clear and rational direction for improving inhibition efficacy to HIV-1 entry and infection. Taken together this report introduces a novel class of natural small molecules fusion inhibitors with nanomolar efficacy of CD4 receptor binding and inhibition of HIV-1 entry.

  2. The Effects of plasticizers and palmitic acid toward the properties of the carrageenan Film

    Heru Wibowo, Atmanto; Listiyawati, Oktaviana; Purnawan, Candra

    2016-02-01

    Varied plasticizers and palmitic acid additive have been added in the carrageenan film. The film was made by mixing of the carrageenan and plasticizers (glycerol, polyethylene glycol, polyvinyl alcohol) with composition of 92:3, 90:6, 87:9, 84:12, 81:15(%w/w) and in the presence of palmitic acid as additive with 1%, 2%, 3%, 4%, 5% of total weight. Casting method was used for the film molding and drying at 60oC with the oven for 12 hours. To investigate the effects of plasticizers and additive, some mechanical tests on film were performed. The test result concludes that plasticizers in the film decreased the tensile strength and increased the elongation break of the carrageenan film. The additive of palmitic acid decreased the tensile strength of the carrageenan film and also decreased the-the water absorbance of the film. The highest tensile strength of films made was with the formulation of carrageenan: PEG with composition of 92:3 (% w/w). The highest elongation break of the film was for carrageenan:PVA with the composition of 81: 15 (%w/w) and carrageenan:palmitic acid:PEG with the composition of 92: 3: 1 (%w/w). The lowest water absorption of the film was achieved for carrageenan:PVA:palmitic acid with the composition of 87: 3: 5 (%w/w).

  3. Comparison of palmitic acid kinetics during glucose or ketone body infusions

    Birkhahn, R.H.; Block, D.J.; Birkhahn, G.C.; Thomford, N.R.

    1986-03-05

    Ketone body interactions can be observed for extended ketosis by infusion by monoacetoacetin (the monoglyceride of acetoacetic acid). Palmitic acid kinetics were compared on the 5th day of glucose or ketone body-glucose infusions. 20 rats were fed complete diets intravenously at the rate of 50 ml/day. All diets contained vitamins, trace minerals, electrolytes, amino acids and 1 kcal/ml of non-protein energy. Rats were divided by energy source: Group A (n = 10) received energy from glucose and Group B (n = 10) from 72% monoacetoacetin plus 28% glucose. Diets were given at 1/2 and 3/4 rats on days 1 and 2, respectively and at full rate for days 3-5. Urinary nitrogen losses, body weight and dietary intake were measured daily. Palmitate kinetics was measured on day 5 using a continuous infusion of (1-/sup 14/C) palmitate and measuring C-14 in breath and plasma and plasma palmitate by GC. The two groups had similar body weight changes and urinary nitrogen losses over the 3 days of full intake Group A had lower plasma palmitate (88 +/- 7 vs 105 +/- 6 micromol/l) but similar turnover (17.1 +/- 2.4 vs 15.0 +/- 1.9 mmol/hr) and oxidation 2.3 +/- 0.3 vs 2.2 +/- 0.05 mmol/hr) compared to Group B. These data show that feeding monoacetoacetin intravenously does not stimulate fatty acid metabolism in the well nourished rat.

  4. Ameliorative effects of polyunsaturated fatty acids against palmitic acid-induced insulin resistance in L6 skeletal muscle cells

    Sawada Keisuke

    2012-03-01

    Full Text Available Abstract Background Fatty acid-induced insulin resistance and impaired glucose uptake activity in muscle cells are fundamental events in the development of type 2 diabetes and hyperglycemia. There is an increasing demand for compounds including drugs and functional foods that can prevent myocellular insulin resistance. Methods In this study, we established a high-throughput assay to screen for compounds that can improve myocellular insulin resistance, which was based on a previously reported non-radioisotope 2-deoxyglucose (2DG uptake assay. Insulin-resistant muscle cells were prepared by treating rat L6 skeletal muscle cells with 750 μM palmitic acid for 14 h. Using the established assay, the impacts of several fatty acids on myocellular insulin resistance were determined. Results In normal L6 cells, treatment with saturated palmitic or stearic acid alone decreased 2DG uptake, whereas unsaturated fatty acids did not. Moreover, co-treatment with oleic acid canceled the palmitic acid-induced decrease in 2DG uptake activity. Using the developed assay with palmitic acid-induced insulin-resistant L6 cells, we determined the effects of other unsaturated fatty acids. We found that arachidonic, eicosapentaenoic and docosahexaenoic acids improved palmitic acid-decreased 2DG uptake at lower concentrations than the other unsaturated fatty acids, including oleic acid, as 10 μM arachidonic acid showed similar effects to 750 μM oleic acid. Conclusions We have found that polyunsaturated fatty acids, in particular arachidonic and eicosapentaenoic acids prevent palmitic acid-induced myocellular insulin resistance.

  5. Interaction of Palmitic Acid with Metoprolol Succinate at the Binding Sites of Bovine Serum Albumin

    Mashiur Rahman; Farzana Prianka; Mohammad Shohel; Md. Abdul Mazid

    2014-01-01

    Purpose: The aim of this study was to characterize the binding profile as well as to notify the interaction of palmitic acid with metoprolol succinate at its binding site on albumin. Methods: The binding of metoprolol succinate to bovine serum albumin (BSA) was studied by equilibrium dialysis method (ED) at 27°C and pH 7.4, in order to have an insight in the binding chemistry of the drug to BSA in presence and absence of palmitic acid. The study was carried out using ranitidine as site-1 a...

  6. Incorporation of Palmitic Acid or Stearic Acid into Soybean Oils Using Enzymatic Interesterification.

    Teh, Soek Sin; Voon, Phooi Tee; Hock Ong, Augustine Soon; Choo, Yuen May

    2016-09-01

    Incorporations of nature fatty acids which were palmitic acid and stearic acid into the end positions of soybean oils were done using sn-1,3 specific immobilised lipase from Rhizomucor miehei at different ratios in order to produce symmetrical triglycerides without changing the fatty acids at sn-2 position. The optimum ratio for the process was 25:75 w/w. There were 19.2% increase of SFA for P25 and 16% increase for S25 at the sn-1,3 positions. The research findings indicated that the structured lipids produced from enzymatic interesterification possessed a higher oxidative stability than soybean oil. The newly formed structured lipids (SUS type) could be good sources for various applications in food industry. PMID:27477075

  7. Blood contact properties of ascorbyl chitosan.

    Yalinca, Z; Yilmaz, E; Taneri, B; Bullici, F; Tuzmen, S

    2013-01-01

    Ascorbyl chitosan was synthesized by heating chitosan with ascorbic acid in isopropanol. The products were characterized by FTIR and C-13 NMR spectroscopies, SEM, and elemental analysis. Blood contact properties of ascorbyl chitosans were evaluated. The ascorbyl chitosans demonstrated to have increased lipid-lowering activity in comparison to chitosan alone upon contact with human blood serum in in vitro conditions. Furthermore, the total cholesterol/HDL ratio was improved towards the desirable ideal values after three hours contact with ascorbyl chitosan samples. The lipid-lowering activity increased with ascorbyl substitution. The inherent nonspecific adsorption capability of chitosan due to its chelating power with several different functional groups was exhibited by ascorbyl chitosans as well. This behavior was exemplified in a simultaneous decrease in the total iron values of the volunteers together with lower lipid levels. Furthermore, ascorbyl chitosans were observed to have less hemocompatibility but increased anticoagulant activity when compared to chitosan alone. Additional in vivo studies are necessary to support these results and to investigate further the advantages and disadvantages of these materials to prove their safety prior to clinical applications. PMID:23862665

  8. Study on preparation, structure and thermal energy storage property of capric-palmitic acid/attapulgite composite phase change materials

    Highlights: → Capric-palmitic acid/attapulgite composite PCMs are prepared by vacuum method. → The composite PCMs is form-stable. → There is no chemical reaction between the capric-palmitic acid and attapulgite. → The phase change temperature and the latent heat of the composite PCM is 21.71 oC and 48.2 J/g, respectively. - Abstract: Fatty acid phase change materials (PCMs) have some advantages such as less corrosivity, no separation of subcooling phase and low price. In this paper, capric acid and palmitic acid are composited according to a certain mass ratio to prepare binary fatty acid. Capric-palmitic acid are absorbed into attapulgite by vacuum method to prepare capric-palmitic acid/attapulgite composite PCMs. Analysis methods such as differential scanning analysis (DSC), scanning electron microscope (SEM), Fourier transform infrared (FT-IR) and specific surface analysis (BET method) are used to test the thermal properties, structure and composition of the prepared composite PCM. The results indicate that the pore structure of the caplic-paltimic acid/attapulgite composite PCM is open-ended tubular capillary, which is beneficial to the adsorption. Capric acid and palmitic acid can be absorbed uniformly into attapulgite and the optimum absorption ratio of capric-palmitic binary fatty acid is 35%. There is no chemical reaction between the capric-palmitic acid and attapulgite. The phase change temperature of the capric-palmitic acid/attapulgite composite PCM is 21.71 oC and the latent heat is 48.2 J/g.

  9. Histopathological, morphometric and stereological studies of ascorbic acid and magnesium ascorbyl phosphate in a skin care formulation.

    Silva, G M; Maia Campos, P M

    2000-06-01

    Ascorbic acid (vitamin C) has been widely used in cosmetics and dermatological formulations due to its inhibitory effect on melanogenesis by affecting collagen synthesis and scavenger properties. However, ascorbic acid (AA) is quickly oxidized and decomposes in aqueous solution and to solve this problem, vitamin C derivatives were synthesized. In the present investigation, histopathological, morphometric and stereological studies were carried out to investigate the possible alterations caused by formulations containing AA or magnesium ascorbyl phosphate (MAP) in the epidermis. Gel creams either with or without 2% AA or its derivative were selected for investigation. Guinea-pigs were shaved on the back, and four areas of 1.5 cm(2) each were used for the experiments. One untreated area was used for control and the others for the application of gel cream formulations either with or without AA or its derivatives. The formulations were applied daily for 2, 4 and 8 weeks and biopsies were then obtained from each area using a dermatological punch. The material collected was analysed by histopathological, morphometric and stereological techniques. We observed that, under the present experimental conditions, whole formulations acted on the epidermis causing a thickening of the epithelium, with cells of larger volume in the granulose and spinous layers. PMID:18503473

  10. Influence of Palmitic Acid and Amino Acids Addition on Iturin A Productivity by Bacillus subtilis RB14-CS

    YULIAR

    2005-07-01

    Full Text Available The aim of this study was to observe the influence of palmitic acid and amino acids on enhancement of iturin A productivity using Bacillus subtilis RB14-CS. The concentrations of palmitic acid examined were 0.8%, 1.6%, and 3.2%. A good yield was observed when 1.6% palmitic acid was added to Polypepton S medium. The production of iturin A increased about 18% than the control. Addition of 3.2% palmitic acid was not effective on iturin A production. It gave lower pH and slightly higher viable cell number of RB14-CS than control and the others addition concentration. Whereas the addition of 0.8% of each of the following amino acids; L-arg, L-asn , L-gln , L-glu, L-gly, L-leu, L-lys, L-trp, L-tyr, and L-val could not increase iturin A productivity, but changed the proportion of iturin A peaks. L-leu, L-val, and L-asn addition produced the highest proportion of peak 3, 4, and 1 respectively.

  11. Oxidative stability of structured lipids produced from sunflower oil and caprylic acid

    Timm Heinrich, Maike; Xu, Xuebing; Nielsen, Nina Skall;

    2003-01-01

    commercial antioxidant blend Grindox 117 (propyl gallate/citric acid/ascorbyl palmitate) or gallic acid to the SL was investigated. The lipid type affected the oxidative stability: SL was less stable than SO and RL. The reduced stability was most likely caused by both the structure of the lipid and...

  12. Inhibition of collagen synthesis by select calcium and sodium channel blockers can be mitigated by ascorbic acid and ascorbyl palmitate

    Ivanov, Vadim; Ivanova, Svetlana; KALINOVSKY, TATIANA; NIEDZWIECKI, ALEKSANDRA; RATH, MATTHIAS

    2016-01-01

    Calcium, sodium and potassium channel blockers are widely prescribed medications for a variety of health problems, most frequently for cardiac arrhythmias, hypertension, angina pectoris and other disorders. However, chronic application of channel blockers is associated with numerous side effects, including worsening cardiac pathology. For example, nifedipine, a calcium-channel blocker was found to be associated with increased mortality and increased risk for myocardial infarction. In addition...

  13. Enzymatic synthesis of cocoa butter equivalent from olive oil and palmitic-stearic fatty acid mixture.

    Mohamed, Ibrahim O

    2015-01-01

    The main goal of the present research is to restructure olive oil triacylglycerol (TAG) using enzymatic acidolysis reaction to produce structured lipids that is close to cocoa butter in terms of TAG structure and melting characteristics. Lipase-catalyzed acidolysis of refined olive oil with a mixture of palmitic-stearic acids at different substrate ratios was performed in an agitated batch reactor maintained at constant temperature and agitation speed. The reaction attained steady-state conversion in about 5 h with an overall conversion of 92.6 % for the olive oil major triacylglycerol 1-palmitoy-2,3-dioleoyl glycerol (POO). The five major TAGs of the structured lipids produced with substrate mass ratio of 1:3 (olive oil/palmitic-stearic fatty acid mixture) were close to that of the cocoa butter with melting temperature between 32.6 and 37.7 °C. The proposed kinetics model used fits the experimental data very well. PMID:25342261

  14. Inhibition of Receptor Interacting Protein Kinases Attenuates Cardiomyocyte Hypertrophy Induced by Palmitic Acid

    Mingyue Zhao; Lihui Lu; Song Lei; Hua Chai; Siyuan Wu; Xiaoju Tang; Qinxue Bao; Li Chen; Wenchao Wu; Xiaojing Liu

    2016-01-01

    Palmitic acid (PA) is known to cause cardiomyocyte dysfunction. Cardiac hypertrophy is one of the important pathological features of PA-induced lipotoxicity, but the mechanism by which PA induces cardiomyocyte hypertrophy is still unclear. Therefore, our study was to test whether necroptosis, a receptor interacting protein kinase 1 and 3 (RIPK1 and RIPK3-) dependent programmed necrosis, was involved in the PA-induced cardiomyocyte hypertrophy. We used the PA-treated primary neonatal rat cardi...

  15. The kinetics of the solidification of highly supersaturated solutions of palmitic acid in oleic acid: a comparison between two models

    RAMIRO RICO-MARTINEZ; JOSE ALBERTO GALLEGOS-INFANTE

    1999-01-01

    The crystallization of fatty acids is very important in industrial applications and biological systems. A comparison between theoretical models and experimental data helps in clarifying mechanistic aspects of these systems. In this contribution, we compare the performance of two models in fitting data from the crystallization of supersaturated solutions of palmitic acid in oleic acid. One of the models was developed by Avrami and the other is based on considering diffusion as limiting (the D-...

  16. Palmitic acid suppresses apolipoprotein M gene expression via the pathway of PPARβ/δ in HepG2 cells

    Highlights: • Palmitic acid significantly inhibited APOM gene expression in HepG2 cells. • Palmitic acid could obviously increase PPARB/D mRNA levels in HepG2 cells. • PPARβ/δ antagonist, GSK3787, had no effect on APOM expression. • GSK3787 could reverse the palmitic acid-induced down-regulation of APOM expression. • Palmitic acid induced suppression of APOM expression is mediated via the PPARβ/δ pathway. - Abstract: It has been demonstrated that apolipoprotein M (APOM) is a vasculoprotective constituent of high density lipoprotein (HDL), which could be related to the anti-atherosclerotic property of HDL. Investigation of regulation of APOM expression is of important for further exploring its pathophysiological function in vivo. Our previous studies indicated that expression of APOM could be regulated by platelet activating factor (PAF), transforming growth factors (TGF), insulin-like growth factor (IGF), leptin, hyperglycemia and etc., in vivo and/or in vitro. In the present study, we demonstrated that palmitic acid could significantly inhibit APOM gene expression in HepG2 cells. Further study indicated neither PI-3 kinase (PI3K) inhibitor LY294002 nor protein kinase C (PKC) inhibitor GFX could abolish palmitic acid induced down-regulation of APOM expression. In contrast, the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ) antagonist GSK3787 could totally reverse the palmitic acid-induced down-regulation of APOM expression, which clearly demonstrates that down-regulation of APOM expression induced by palmitic acid is mediated via the PPARβ/δ pathway

  17. Docosahexaenoic acid and palmitic acid reciprocally modulate monocyte activation in part through endoplasmic reticulum stress.

    Snodgrass, Ryan G; Huang, Shurong; Namgaladze, Dmitry; Jandali, Ola; Shao, Tiffany; Sama, Spandana; Brüne, Bernhard; Hwang, Daniel H

    2016-06-01

    Palmitic acid (C16:0) and TLR2 ligand induce, but docosahexaenoic acid (DHA) inhibits monocyte activation. C16:0 and TLR2 or TLR4 ligand induce certain ER stress markers; thus, we determined whether ER stress induced by these agonists is sufficient to induce monocyte activation, and whether the ER stress is inhibited by DHA which is known to inhibit C16:0- or ligand-induced TLR activation. Monocyte activation and ER stress were assessed by TLR/inflammasome-induced IL-1β production, and phosphorylation of IRE-1 and eIF2 and expression of CHOP, respectively in THP-1 cells. TLR2 ligand Pam3CSK4 induced phosphorylation of eIF2, but not phosphorylation of IRE-1 and CHOP expression. LPS also induced phosphorylation of both IRE-1 and eIF2 but not CHOP expression suggesting that TLR2 or TLR4 ligand, or C16:0 induces different ER stress responses. C16:0-, Pam3CSK4-, or LPS-induced IL-1β production was inhibited by 4-phenylbutyric acid, an inhibitor of ER stress suggesting that IL-1β production induced by these agonists is partly mediated through ER stress. Among two ER stress-inducing molecules, thapsigargin but not tunicamycin led to the expression of pro-IL-1β and secretion of IL-1β. Thus, not all types of ER stress are sufficient to induce inflammasome-mediated IL-1β secretion in monocytes. Although both C16:0 and thapsigargin-induced IL-1β secretion was inhibited by DHA, only C16:0-mediated ER stress was responsive to DHA. These findings suggest that the anti-inflammatory effects of DHA are at least in part mediated through modulating ER homeostasis and that the propensity of ER stress can be differentially modulated by the types of dietary fat we consume. PMID:27142735

  18. Brain region-specificity of palmitic acid-induced abnormalities associated with Alzheimer's disease

    Melrose Joseph

    2008-06-01

    Full Text Available Abstract Background Alzheimer's disease (AD is a progressive, neurodegenerative disease mostly affecting the basal forebrain, cortex and hippocampus whereas the cerebellum is relatively spared. The reason behind this region-specific brain damage in AD is not well understood. Here, we report our data suggesting "differential free fatty acid metabolism in the different brain areas" as a potentially important factor in causing the region-specific damage observed in AD brain. Findings The astroglia from two different rat brain regions, cortex (region affected in AD and cerebellum (unaffected region, were treated with 0.2 mM of palmitic acid. The conditioned media were then transferred to the cortical neurons to study the possible effects on the two main, AD-associated protein abnormalities, viz. BACE1 upregulation and hyperphosphorylation of tau. The conditioned media from palmitic-acid treated cortical astroglia, but not the cerebellar astroglia, significantly elevated levels of phosphorylated tau and BACE1 in cortical neurons as compared to controls (47 ± 7% and 45 ± 4%, respectively. Conclusion The present data provide an experimental explanation for the region-specific damage observed in AD brain; higher fatty acid-metabolizing capacity of cortical astroglia as compared to cerebellar astroglia, may play a causal role in increasing vulnerability of cortex in AD, while sparing cerebellum.

  19. The kinetics of the solidification of highly supersaturated solutions of palmitic acid in oleic acid: a comparison between two models

    RAMIRO RICO-MARTINEZ

    1999-08-01

    Full Text Available The crystallization of fatty acids is very important in industrial applications and biological systems. A comparison between theoretical models and experimental data helps in clarifying mechanistic aspects of these systems. In this contribution, we compare the performance of two models in fitting data from the crystallization of supersaturated solutions of palmitic acid in oleic acid. One of the models was developed by Avrami and the other is based on considering diffusion as limiting (the D-model. The D-model fitted the data better than the Avrami model in all cases. The D-model has a low value of the regression coefficient (r2, lower than 0.9 in only three cases. For these points, the thermodynamic force was smaller. Differences in the parameter n (an index of dimensionality were observed; these differences indicate that clusters were present previous to the crystallization process. Furthermore, there appears to be a difference in the mechanism of crystallization of pure solutions of palmitic acid and solutions with a small fraction of oleic acid. Thus, one is lead to the conclusion that the rate of crystallization of fatty acids at high concentrations is limited by diffusion.

  20. Palmitic acid induces interleukin-1β secretion via NLRP3 inflammasomes and inflammatory responses through ROS production in human placental cells.

    Shirasuna, Koumei; Takano, Hiroki; Seno, Kotomi; Ohtsu, Ayaka; Karasawa, Tadayoshi; Takahashi, Masafumi; Ohkuchi, Akihide; Suzuki, Hirotada; Matsubara, Shigeki; Iwata, Hisataka; Kuwayama, Takehito

    2016-08-01

    Maternal obesity, a major risk factor for adverse pregnancy complications, results in inflammatory cytokine release in the placenta. Levels of free fatty acids are elevated in the plasma of obese human. These fatty acids include obesity-related palmitic acids, which is a major saturated fatty acid, that promotes inflammatory responses. Increasing evidence indicates that nucleotide-binding oligomerization domain-like receptor pyrin domain-containing 3 (NLRP3) inflammasomes mediate inflammatory responses induced by endogenous danger signals. We hypothesized that inflammatory responses associated with gestational obesity cause inflammation. To test this hypothesis, we investigated the effect of palmitic acid on the activation of NLRP3 inflammasomes and inflammatory responses in a human Sw.71 trophoblast cell line. Palmitic acid stimulated caspase-1 activation and markedly increased interleukin (IL)-1β secretion in Sw.71 cells. Treatment with a caspase-1 inhibitor diminished palmitic acid-induced IL-1β release. In addition, NLRP3 and caspase-1 genome editing using a CRISPR/Cas9 system in Sw.71 cells suppressed IL-1β secretion, which was stimulated by palmitic acid. Moreover, palmitic acid stimulated caspase-3 activation and inflammatory cytokine secretion (e.g., IL-6 and IL-8). Palmitic acid-induced cytokine secretion were dependent on caspase-3 activation. In addition, palmitic acid-induced IL-1β, IL-6, and IL-8 secretion was depended on reactive oxygen species (ROS) generation. In conclusion, palmitic acid caused activation of NLRP3 inflammasomes and inflammatory responses, inducing IL-1β, IL-6, and IL-8 secretion, which is associated with ROS generation, in human Sw.71 placental cells. We suggest that obesity-related palmitic acid induces placental inflammation, resulting in association with pregnancy complications. PMID:27300134

  1. Phase equilibria of oleic, palmitic, stearic, linoleic and linolenic acids in supercritical CO2

    P. L. Penedo

    2009-03-01

    Full Text Available The knowledge of the phase equilibrium is one of the most important factors to study the design of separation processes controlled by the equilibrium. Fatty acids are present in high concentration as by-products in vegetable oils but the equilibrium data involving these components is scarce. The objective of this work is the experimental determination of the liquid-vapor equilibrium of five binary different systems formed by carbon dioxide and palmitic acid (C16:0, stearic acid (C18:0, oleic acid (C18:1, linoleic acid (C18:2 and linolenic acid (C18:3. The equilibrium experimental data was collected at 40, 60 and 80ºC at 60, 90 and 120 bar, at the extract and raffinate phases, using an experimental apparatus containing an extractor, a gas cylinder and pressure and temperature controllers. The data was modeled using the cubic equation of state of Peng-Robinson with the mixing rule of van der Waals with binary interaction parameters. The model was adequate to treat the experimental data at each temperature and at all the temperatures together. The best model that includes the van der Waals mixing rule with two parameters has maximum deviation of 17%. The distribution coefficients were also analyzed and it was concluded that the fractionation of the fatty acids is possible using supercritical carbon dioxide.

  2. PALMITIC AND OLEIC ACIDS AND THEIR ROLE IN PATHOGENESIS OF ATHEROSCLEROSIS

    V. N. Titov

    2014-01-01

    Full Text Available On the basis of phylogenetic theory of general pathology, the cause of a noninfectious disease whose occurrence in a population is more than 5–7% is an impaired biological function or reaction to the environment. From the general biology viewpoint, high mortality rate related to cardio-vascular diseases and atherosclerosis (intercellular deficiency of polyenic fatty acids (PFA is just extinction of the Homo sapiens population upon adaptation to new environmental factors. The biological function of throphology (feeding and biological reaction of exotrophy (external feeding are impaired in several aspects, the major of which is nonphysiologically high dietary content of saturated fatty acids, primarily, of palmitic fatty acid (FA. The lipoprotein system formed at early stages of phylogenesis cannot transport and provide physiological deposition of great amounts of palmitic FA, which leads to the development of an adaption (compensatory and accumulation disease. This results in hypermipidemia, impaired bioavailability of PFA to cells, compesatory production of humoral mediators from ω-9 eicosatrienoic mead FA, disorders in physiological parameters of cell plasma membrane and integral proteins, nonphysiological conformation of apoВ-100 in lipoproteins, formation of ligandless lipoproteins (biological litter and impairments in the biological function of endoecology, utilization of ligandless lipoproteins in arterial intima by phylogenetically early macrophages that do not hydrolyze polyenic cholesterol esters, increase in the intensity of the biological reaction of inflammation, and destructive and inflammatory lesions in arterial intima of an atheromatosis or atherothrombosis type. Atheromatous masses are catabolites of PFA which were not internalized by phylogenetically late cells via receptor-mediated pathway.

  3. Palmitic acid-labeled lipids selectively incorporated into platelet cytoskeleton during aggregation

    Previous experiments showed that during the early stages (20-30 seconds) of aggregation induced by adenosine diphosphate (ADP, 2 microM) or thrombin (0.1 U/mL) of rabbit or human platelets prelabeled with [3H]palmitic acid, labeled lipid became associated with the cytoskeleton isolated after lysis with 1% Triton X-100, 5 mM EGTA [ethylene glycol-bis-(beta-aminoethyl ether)]-N,N,N',N'-tetra-acetic acid. The association appeared to be related to the number of sites of contact and was independent of the release of granule contents. We have now investigated the nature of the labeled lipids by thin-layer and column chromatography and found differences between the distribution of the label in intact platelets (both stimulated and unstimulated) and the isolated cytoskeletons. In both species, and with either ADP or thrombin as aggregating agent, 70-85% of the label in both intact platelets and in the cytoskeletons was in phospholipids. The distribution of label among the phospholipids in the cytoskeletons was similar to that in intact platelets except that the percentage of label in phosphatidylcholine was significantly higher in the cytoskeletons of human platelets than in the intact platelets, and the percentage of label in phosphatidylserine/phosphatidylinositol was significantly lower in the cytoskeletons of rabbit platelets and thrombin-aggregated human platelets than in intact platelets. The cytoskeletons contained a lower percentage of label in triacylglycerol, diacylglycerol, and cholesterol ester than the intact platelets. Contrary to a report in the literature, we found no evidence for the incorporation of diacylglycerol and palmitic acid into the cytoskeleton

  4. Hydrolytic degradation behaviour of sucrose palmitate reinforced poly(lactic acid) nanocomposites.

    Valapa, Ravi Babu; G, Pugazhenthi; Katiyar, Vimal

    2016-08-01

    This work discusses the influence of novel biofiller, "sucrose palmitate" (SP) on the hydrolytic degradation behavior of poly(lactic acid) (PLA) nanocomposites. The influence of temperature and pH of the solution on the hydrolytic degradation behavior of PLA and PLA-SP nanocomposites was investigated. The variation in the crystallinity of PLA and PLA composites subjected to the hydrolytic degradation process is verified by XRD and DSC analysis. The morphological changes that occurred during the degradation process are observed by scanning electron microscopy (SEM). Thermo-gravimetric analysis confirms the loss of thermal stability of the neat PLA as well as composites after hydrolytic degradation process. Transparency measurements support the enhancement in opacity of both the PLA and PLA-SP nanocomposites with progress in hydrolytic degradation period. PMID:27095433

  5. Comparison of microwave processing and excess steam jet cooking for spherulite production of from starch:palmitic acid inclusion complexes

    It was previously shown that toroid and spherical/lobed spherulites were formed upon slow cooling of aqueous dispersions of corn starch and palmitic acid after passing through an excess steam jet cooker. Spherulite yield was 86% based on amylose. In order to determine whether excess steam jet cookin...

  6. Antioxidant effect of mogrosides against oxidative stress induced by palmitic acid in mouse insulinoma NIT-1 cells

    Excessive oxidative stress in pancreatic β cells, caused by glucose and fatty acids, is associated with the pathogenesis of type 2 diabetes. Mogrosides have shown antioxidant and antidiabetic activities in animal models of diabetes, but the underlying mechanisms remain unclear. This study evaluated the antioxidant effect of mogrosides on insulinoma cells under oxidative stress caused by palmitic acid, and investigated the underlying molecular mechanisms. Mouse insulinoma NIT-1 cells were cultured in medium containing 0.75 mM palmitic acid, mimicking oxidative stress. The effects of 1 mM mogrosides were determined with the dichlorodihydrofluorescein diacetate assay for intracellular reactive oxygen species (ROS) and FITC-Annexin V/PI assay for cell apoptosis. Expression of glucose transporter-2 (GLUT2) and pyruvate kinase was determined by semi-quantitative reverse-transcription polymerase chain reaction. Palmitic acid significantly increased intracellular ROS concentration 2-fold (P<0.05), and decreased expression of GLUT2 (by 60%, P<0.05) and pyruvate kinase (by 80%, P<0.05) mRNAs in NIT-1 cells. Compared with palmitic acid, co-treatment with 1 mM mogrosides for 48 h significantly reduced intracellular ROS concentration and restored mRNA expression levels of GLUT2 and pyruvate kinase. However, mogrosides did not reverse palmitic acid-induced apoptosis in NIT-1 cells. Our results indicate that mogrosides might exert their antioxidant effect by reducing intracellular ROS and regulating expression of genes involved in glucose metabolism. Further research is needed to achieve a better understanding of the signaling pathway involved in the antioxidant effect of mogrosides

  7. Antioxidant effect of mogrosides against oxidative stress induced by palmitic acid in mouse insulinoma NIT-1 cells

    Xu, Q.; Chen, S.Y.; Deng, L.D.; Feng, L.P.; Huang, L.Z.; Yu, R.R. [Department of Pharmacy, Guilin Medical University, Guilin (China)

    2013-11-18

    Excessive oxidative stress in pancreatic β cells, caused by glucose and fatty acids, is associated with the pathogenesis of type 2 diabetes. Mogrosides have shown antioxidant and antidiabetic activities in animal models of diabetes, but the underlying mechanisms remain unclear. This study evaluated the antioxidant effect of mogrosides on insulinoma cells under oxidative stress caused by palmitic acid, and investigated the underlying molecular mechanisms. Mouse insulinoma NIT-1 cells were cultured in medium containing 0.75 mM palmitic acid, mimicking oxidative stress. The effects of 1 mM mogrosides were determined with the dichlorodihydrofluorescein diacetate assay for intracellular reactive oxygen species (ROS) and FITC-Annexin V/PI assay for cell apoptosis. Expression of glucose transporter-2 (GLUT2) and pyruvate kinase was determined by semi-quantitative reverse-transcription polymerase chain reaction. Palmitic acid significantly increased intracellular ROS concentration 2-fold (P<0.05), and decreased expression of GLUT2 (by 60%, P<0.05) and pyruvate kinase (by 80%, P<0.05) mRNAs in NIT-1 cells. Compared with palmitic acid, co-treatment with 1 mM mogrosides for 48 h significantly reduced intracellular ROS concentration and restored mRNA expression levels of GLUT2 and pyruvate kinase. However, mogrosides did not reverse palmitic acid-induced apoptosis in NIT-1 cells. Our results indicate that mogrosides might exert their antioxidant effect by reducing intracellular ROS and regulating expression of genes involved in glucose metabolism. Further research is needed to achieve a better understanding of the signaling pathway involved in the antioxidant effect of mogrosides.

  8. Research progress of lipase-catalyzed synthesis of L-ascorbyl organic acid ester%脂肪酶催化合成L-抗坏血酸有机酸酯的研究进展

    蒋相军; 胡燚; 刘维明; 黄和

    2011-01-01

    To broaden the applications of L-ascorbic acid, it is an economical and feasible way to convert L-aseorbic acid into L-ascorbyl organic acid ester. The recent research progress of enzymatic synthesis of L-ascorbyl organic acid ester is summarized, by focusing on enzymatic synthesis of L-ascorbyl saturated fatty acid ester, unsaturated fatty acid ester and mixed fatty acid ester in organic solvents. The types of lipase, organic solvents and methods of separation and purification in the synthesis are discussed. Furthermore, the prospect of enzymatic synthesis of L-ascorbyl organic acid ester is also presented.%为了拓宽L-抗坏血酸酯在维护人体健康中的应用,将L-抗坏血酸转化成L-抗坏血酸酯是经济可行的手段。综述了近年来酶催化L-抗坏血酸有机酸酯的研究进展,重点介绍了有机相中L-抗坏血酸饱和脂肪酸酯、不饱和脂肪酸酯、脂肪酸混合酯的酶促合成,对于酶的种类、有机溶剂的选择及分离纯化方法进行了探讨,并对酶催化L-抗坏血酸有机酸酯合成前景进行了展望。

  9. T cells cooperate with palmitic acid in induction of beta cell apoptosis

    Miljković Djordje

    2009-05-01

    Full Text Available Abstract Background Diabetes is characterized by progressive failure of insulin producing beta cells. It is well known that both saturated fatty acids and various products of immune cells can contribute to the reduction of beta cell viability and functionality during diabetes pathogenesis. However, their joint action on beta cells has not been investigated, so far. Therefore, we explored the possibility that leukocytes and saturated fatty acids cooperate in beta cell destruction. Results Rat pancreatic islets or insulinoma cells (RIN were co-cultivated with concanavalin A (ConA-stimulated rat lymph node cells (LNC, or they were treated with cell-free supernatants (Sn obtained from ConA-stimulated spleen cells or from activated CD3+ cells, in the absence or presence of palmitic acid (PA. ConA-stimulated LNC or Sn and PA cooperated in inducing caspase-3-dependent RIN cell apoptosis. The observed effect of PA and Sn on RIN cell viability was mediated by p38 mitogen-activated protein kinase (MAPK-signaling and was achieved through auto-destructive nitric oxide (NO production. The cooperative effect of Sn was mimicked with the combination of interleukin-1β, interleukin-2, interleukin-6, interleukin-17, interferon-γ and tumor necrosis factor-α. Conclusion These results imply that stimulated T cells produce cytokines that cooperate with saturated free fatty acids in beta cell destruction during diabetes pathogenesis.

  10. Withaferin A protects against palmitic acid-induced endothelial insulin resistance and dysfunction through suppression of oxidative stress and inflammation

    Kalaivani Batumalaie; Muhammad Arif Amin; Dharmani Devi Murugan; Munavvar Zubaid Abdul Sattar; Nor Azizan Abdullah

    2016-01-01

    Activation of inflammatory pathways via reactive oxygen species (ROS) by free fatty acids (FFA) in obesity gives rise to insulin resistance and endothelial dysfunction. Withaferin A (WA), possesses both antioxidant and anti-inflammatory properties and therefore would be a good strategy to suppress palmitic acid (PA)-induced oxidative stress and inflammation and hence, insulin resistance and dysfunction in the endothelium. Effect of WA on PA-induced insulin resistance in human umbilical vein e...

  11. Dietary Triacylglycerols with Palmitic Acid in the sn-2 Position Modulate Levels of N-Acylethanolamides in Rat Tissues

    Carta, Gianfranca; Murru, Elisabetta; Lisai, Sara; Sirigu, Annarita; Piras, Antonio; Collu, Maria; Batetta, Barbara; Gambelli, Luisa; Banni, Sebastiano

    2015-01-01

    Background Several evidences suggest that the position of palmitic acid (PA) in dietary triacylglycerol (TAG) influences different biological functions. We aimed at evaluating whether dietary fat with highly enriched (87%) PA in sn-2 position (Hsn-2 PA), by increasing PA incorporation into tissue phospholipids (PL), modifies fatty acid profile and biosynthesis of fatty acid—derived bioactive lipids, such as endocannabinoids and their congeners. Study Design Rats were fed for 5 weeks diets con...

  12. KINETIC STUDY OF PALMITIC ACID ESTERIFICATION CATALYZED BY Rhizopus oryzae RESTING CELLS

    RAMON CANELA

    2009-04-01

    Full Text Available

    ABSTRACT

    In the present study, a kinetic model for the biocatalytic synthesis of esters using Rhizopus oryzae resting cells is proposed. The kinetic study has been made in a range of 30-50 °C and atmospheric pressure. The Influence of operating variables, water content, pH, amount of mycelium was studied. Different values of temperature, initial mycelium concentration and acid/alcohol molar ratio were tested. Initial rates were estimated from the slope of the concentration of palmitic acid, or their corresponding ester at conversions of less than 10%, versus time and reported as mmol l-1 min -1. The values of kinetic constants were computed using the freeware program SIMFIT (http:\\www.simfit.man.ac.uk.

    Key words: bound lipase, esterification, fungal resting cells, Rhizopus oryzae, palmitic acid, propanol.


    RESUMEN

    En el presente estudio, un modelo cinético para la síntesis de esteres usando Rhizopus oryzae resting cells es propuesto. El estudio cinético fue realizado en un rango de temperatura de 30-50 ºC a presión atmosférica reducida. La influencia de las variables de operación tales como temperatura, pH y contenido de agua fueron estudiadas. Diferentes valores de concentración de micelio y relación molar de ácido/alcohol son ensayadas, Las velocidades iníciales se estimaron de la curva de concentración de acido palmítico, y su correspondiente conversión a ester en menos del 10%, frente a tiempo y reportadas en mmol I-1 min -1. Los valores de las constantes cinéticas fueron calculados usando el programa freeware SIMFIT (http:\\www.simfit.man.ac.uk.

    Palabras clave: Lipasas, esterificación, resting cells, Rhizopus oryzae, acido palmítico, propanol.

  13. Scientific Opinion on the safety and efficacy of vitamin C (ascorbic acid and sodium calcium ascorbyl phosphate) as a feed additive for all animal species based on a dossier submitted by VITAC EEIG

    EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP)

    2013-01-01

    Vitamin C (formerly known as antiscorbutic vitamin) is essential for primates, guinea pigs and fish. Vitamin C, in the form of ascorbic acid and sodium calcium ascorbyl phosphate, is safe for all animal species. Setting a maximum content in feed and water for drinking is not considered necessary. Data on the vitamin C consumption of consumers are based on the levels of vitamin C in foodstuffs, including food of animal origin, produced in accordance with current EU legislation on the supplemen...

  14. Reactivity of chlorine radical with submicron palmitic acid particles: kinetic measurements and products identification

    M. Mendez

    2013-06-01

    Full Text Available The heterogeneous reaction of Cl. radicals with sub-micron palmitic acid (PA particles was studied in an aerosol flow tube in the presence or in the absence of O2. Fine particles were generated by homogeneous condensation of PA vapors and introduced in the reactor where chlorine atoms are produced by photolysis of Cl2 using UV lamps surrounding the reactor. The effective reactive uptake coefficient (γ has been determined from the rate loss of PA measured by GC/MS analysis of reacted particles as a function of the chlorine exposure. In the absence of O2, γ = 14 ± 5 indicates efficient secondary chemistry involving Cl2. GC/MS analyses have shown the formation of monochlorinated and polychlorinated compounds in the oxidized particles. Although, the PA particles are solid, the complete mass can be consumed. In the presence of oxygen, the reaction is still dominated by secondary chemistry but the propagation chain length is smaller than in the absence of O2 which leads to an uptake coefficient γ = 3 ± 1. In the particulate phase, oxocarboxylic acids and dicarboxylic acids are identified by GC/MS. Formation of alcohols and monocarboxylic acids are also suspected. All these results show that solid organic particles could be efficiently oxidized by gas-phase radicals not only on their surface, but also in bulk by mechanisms which are still unclear. Furthermore the identified reaction products are explained by a chemical mechanism showing the pathway of the formation of more functionalized products. They help to understand the aging of primary tropospheric aerosol containing fatty acids.

  15. Scientific Opinion on the safety and efficacy of vitamin C (ascorbic acid and sodium calcium ascorbyl phosphate as a feed additive for all animal species based on a dossier submitted by VITAC EEIG

    EFSA Panel on Additives and Products or Substances used in Animal Feed (FEEDAP

    2013-02-01

    Full Text Available Vitamin C (formerly known as antiscorbutic vitamin is essential for primates, guinea pigs and fish. Vitamin C, in the form of ascorbic acid and sodium calcium ascorbyl phosphate, is safe for all animal species. Setting a maximum content in feed and water for drinking is not considered necessary. Data on the vitamin C consumption of consumers are based on the levels of vitamin C in foodstuffs, including food of animal origin, produced in accordance with current EU legislation on the supplementation of feed with vitamin C. The exposure is far below the guidance level. Any potential contribution of the use of vitamin C in feed is therefore already considered in the above data. Consequently, the use of vitamin C in animal nutrition is not of concern for consumer safety. In the absence of inhalation toxicity studies it would be prudent to assume that inhalation of dust from the additives presents a health hazard to workers and measures should be taken to minimise inhalation exposure. In the absence of data, ascorbic acid and sodium calcium ascorbyl phosphate should be considered as irritant to skin and eyes and as dermal sensitisers. The supplementation of feed with vitamin C does not pose a risk to the environment. Ascorbic acid and sodium calcium ascorbyl phosphate are regarded as effective sources of vitamin C when added to feed or water for drinking.

  16. Palmitic Acid on Salt Subphases and in Mixed Monolayers of Cerebrosides: Application to Atmospheric Aerosol Chemistry

    Ellen M. Adams

    2013-10-01

    Full Text Available Palmitic acid (PA has been found to be a major constituent in marine aerosols, and is commonly used to investigate organic containing atmospheric aerosols, and is therefore used here as a proxy system. Surface pressure-area isotherms (π-A, Brewster angle microscopy (BAM, and vibrational sum frequency generation (VSFG were used to observe a PA monolayer during film compression on subphases of ultrapure water, CaCl2 and MgCl2 aqueous solutions, and artificial seawater (ASW. π-A isotherms indicate that salt subphases alter the phase behavior of PA, and BAM further reveals that a condensation of the monolayer occurs when compared to pure water. VSFG spectra and BAM images show that Mg2+ and Ca2+ induce ordering of the PA acyl chains, and it was determined that the interaction of Mg2+ with the monolayer is weaker than Ca2+. π-A isotherms and BAM were also used to monitor mixed monolayers of PA and cerebroside, a simple glycolipid. Results reveal that PA also has a condensing effect on the cerebroside monolayer. Thermodynamic analysis indicates that attractive interactions between the two components exist; this may be due to hydrogen bonding of the galactose and carbonyl headgroups. BAM images of the collapse structures show that mixed monolayers of PA and cerebroside are miscible at all surface pressures. These results suggest that the surface morphology of organic-coated aerosols is influenced by the chemical composition of the aqueous core and the organic film itself.

  17. Effects of lung surfactant proteins, SP-B and SP-C, and palmitic acid on monolayer stability.

    Ding, J; Takamoto, D Y; von Nahmen, A; Lipp, M M; Lee, K Y; Waring, A J; Zasadzinski, J A

    2001-01-01

    Langmuir isotherms and fluorescence and atomic force microscopy images of synthetic model lung surfactants were used to determine the influence of palmitic acid and synthetic peptides based on the surfactant-specific proteins SP-B and SP-C on the morphology and function of surfactant monolayers. Lung surfactant-specific protein SP-C and peptides based on SP-C eliminate the loss to the subphase of unsaturated lipids necessary for good adsorption and respreading by inducing a transition between...

  18. Phase change material: Optimizing the thermal properties and thermal conductivity of myristic acid/palmitic acid eutectic mixture with acid-based surfactants

    In this study the addition of surfactant to fatty acids as phase change materials (PCMs) for solar thermal applications is proposed. The incorporation of surfactant additives into a eutectic mixture of fatty acids can significantly increase the value of latent heat storage and can suppress undercooling. We report the preparation of myristic acid/palmitic acid (MA/PA) eutectic mixture as Phase Change Material (PCM) with addition of 0, 5, 10, 15, and 20% sodium myristate (SM), sodium palmitate (SP), and sodium stearate (SS), the influence of surfactant additives on thermal properties and thermal conductivity of eutectic mixtures. It was found that the addition of 5% SM, 5% SP, and 5% SS to MA/PA eutectic mixture is very effective in depressing the liquid/solid phase change temperature, reducing the undercooling and increasing the amount of latent heat of fusion as well as thermal conductivity of eutectic PCM compared to eutectic PCM without surfactants. Furthermore MA/PA + 5%SS has the highest latent heat of fusion of 191.85 J g−1, while MA/PA + 5%SM showed the least undercooling of 0.34 °C and the highest thermal conductivity of 0.242 W m−1 K−1. -- Highlights: • Myristic acid (MA) and palmitic acid (PA) are fatty acids component. • The eutectic composition ratio of MA/PA obtained at 70/30, wt.%. • 5% each acid-based surfactants were reduces the melting and undercooling temperature of MA/PA (70/30, wt.%). • Thermal conductivity and ΔHf of MA/PA (70/30, wt.%) were increased by adding 5% surfactants. • MA/PA + 5% acid-based surfactants have a great potential to apply in LHTES applications

  19. Palmitic acid suppresses apolipoprotein M gene expression via the pathway of PPAR{sub β/δ} in HepG2 cells

    Luo, Guanghua; Shi, Yuanping; Zhang, Jun; Mu, Qinfeng; Qin, Li; Zheng, Lu; Feng, Yuehua [Comprehensive Laboratory, The Third Affiliated Hospital of Soochow University, Changzhou 213003 (China); Berggren-Söderlund, Maria; Nilsson-Ehle, Peter [Division of Clinical Chemistry and Pharmacology, Department of Laboratory Medicine, Lund University, S-221 85 Lund (Sweden); Zhang, Xiaoying, E-mail: zhangxy6689996@163.com [Department of Cardiothoracic Surgery, The Third Affiliated Hospital of Soochow University, Changzhou 213003 (China); Xu, Ning, E-mail: ning.xu@med.lu.se [Division of Clinical Chemistry and Pharmacology, Department of Laboratory Medicine, Lund University, S-221 85 Lund (Sweden)

    2014-02-28

    Highlights: • Palmitic acid significantly inhibited APOM gene expression in HepG2 cells. • Palmitic acid could obviously increase PPARB/D mRNA levels in HepG2 cells. • PPAR{sub β/δ} antagonist, GSK3787, had no effect on APOM expression. • GSK3787 could reverse the palmitic acid-induced down-regulation of APOM expression. • Palmitic acid induced suppression of APOM expression is mediated via the PPAR{sub β/δ} pathway. - Abstract: It has been demonstrated that apolipoprotein M (APOM) is a vasculoprotective constituent of high density lipoprotein (HDL), which could be related to the anti-atherosclerotic property of HDL. Investigation of regulation of APOM expression is of important for further exploring its pathophysiological function in vivo. Our previous studies indicated that expression of APOM could be regulated by platelet activating factor (PAF), transforming growth factors (TGF), insulin-like growth factor (IGF), leptin, hyperglycemia and etc., in vivo and/or in vitro. In the present study, we demonstrated that palmitic acid could significantly inhibit APOM gene expression in HepG2 cells. Further study indicated neither PI-3 kinase (PI3K) inhibitor LY294002 nor protein kinase C (PKC) inhibitor GFX could abolish palmitic acid induced down-regulation of APOM expression. In contrast, the peroxisome proliferator-activated receptor beta/delta (PPAR{sub β/δ}) antagonist GSK3787 could totally reverse the palmitic acid-induced down-regulation of APOM expression, which clearly demonstrates that down-regulation of APOM expression induced by palmitic acid is mediated via the PPAR{sub β/δ} pathway.

  20. UPR in palmitate-treated pancreatic beta-cells is not affected by altering oxidation of the fatty acid

    Sol E-ri; Sargsyan Ernest; Bergsten Peter

    2011-01-01

    Abstract Background Elevated levels of lipids are detrimental for beta-cell function and mass. One of the mechanisms of how fatty acids induce apoptosis is development of the unfolded protein response (UPR). It is still far from understood how fatty acids activate the UPR, however. Methods We examined how palmitate-induced activation of the UPR was affected by altering the metabolism of the fatty acid in insulin-secreting INS-1E and MIN6 cell lines and intact human islets. To increase oxidati...

  1. Digestibility of Fatty Acids in the Gastrointestinal Tract of Dairy Cows Fed with Tallow or Saturated Fats Rich in Stearic Acid or Palmitic Acid

    Weisbjerg, Martin Riis; Hvelplund, Torben; Børsting, Christian Friis

    1992-01-01

    Fatty acid digestibility was studied with five lactating cows fed three different fat sources in a 5 × 5 latin square experiment. The treatments were 500 g of tallow, 500 or 1000 g of saturated fat rich in stearic acid (C18:0) (SARF) or 500 or 1000 g of saturated fat rich in palmitic acid (C16......:0) (PARF) per day. The total daily fatty acid intake was about 1100 g in rations with the highest fat inclusion. The fatty acid digestibilities were 76% for tallow, 74 and 64% for 500 and 1000 g SARF, respectively, and 87 and 81% for 500 and 1000 g of PARF, respectively. When compared to fatty acid...... digestibility for tallow predicted from a model based on literature values, PARF had a higher fatty acid digestibility at both fat intakes, and SARF had a lower fatty acid digestibility, especially at high fat intake....

  2. AKTIVITAS DAN STABILITAS RADICAL SCAVENGING L-ASKORBIL PALMITAT HASIL SINTESIS SECARA ENZIMATIK [Activity and Stability of Radical Scavenging of L- Palmitate Synthesized Enzymatically

    Tri Agus Siswoyo1*

    2009-12-01

    Full Text Available L-ascorbyl palmitate (AsA-Pal-Enz was synthesized by using an immobilized lipase from Aspergillus niger. A comparison of antioxidative effects between L-ascorbic acid (AsA and AsA-Pal-Enz was determined in terms of 1,1-diphenyl-2-picrylhydrazyl (DPPH radical–scavenging. The results indicate that the AsA-Pal-Enz was effective in preventing lipid oxidation, while the antioxidative activity in authentic AsA-Pal was lower. The activity of AsA-Pal-Enz was very stable than AsA-Pal standard during heating.

  3. AKTIVITAS DAN STABILITAS RADICAL SCAVENGING L-ASKORBIL PALMITAT HASIL SINTESIS SECARA ENZIMATIK [Activity and Stability of Radical Scavenging of L- Palmitate Synthesized Enzymatically

    Tri Agus Siswoyo; Tri Ardiyati 2)

    2009-01-01

    L-ascorbyl palmitate (AsA-Pal-Enz) was synthesized by using an immobilized lipase from Aspergillus niger. A comparison of antioxidative effects between L-ascorbic acid (AsA) and AsA-Pal-Enz was determined in terms of 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical–scavenging. The results indicate that the AsA-Pal-Enz was effective in preventing lipid oxidation, while the antioxidative activity in authentic AsA-Pal was lower. The activity of AsA-Pal-Enz was very stable than AsA-Pal standard duri...

  4. Preparation and properties of highly conductive palmitic acid/graphene oxide composites as thermal energy storage materials

    PA/GO (palmitic acid/graphene oxide) as PCMs (phase change materials) prepared by vacuum impregnation method, have high thermal conductivity. The GO (graphene oxide) composite was used as supporting material to improve thermal conductivity and shape stabilization of composite PCM (phase change material). SEM (Scanning electronic microscope), FT-IR (Fourier transformation infrared spectroscope) and XRD (X-ray diffractometer) were applied to determine microstructure, chemical structure and crystalloid phase of palmitic acid/GO composites, respectively. DSC (Differential scanning calorimeter) test was done to investigate thermal properties which include melting and solidifying temperatures and latent heat. FT-IR analysis represented that the composite instruction of porous palmitic acid and GO were physical. The temperatures of melting, freezing and latent heats of the composite measured through DSC analysis were 60.45, 60.05 °C, 101.23 and 101.49 kJ/kg, respectively. Thermal cycling test showed that the form-stable composite PCM has good thermal reliability and chemical stability. Thermal conductivity of the composite PCM was improved by more than three times from 0.21 to 1.02. As a result, due to their acceptable thermal properties, good thermal reliability, chemical stability and great thermal conductivities, we can consider the prepared form-stable composites as highly conductive PCMs for thermal energy storage applications. - Highlights: • Novel composite PCM with high thermal conductivity and latent heat storage. • New thermal cycling test for thermal reliability of composite PCMs. • Increasing thermal conductivity of composite PCM with graphene oxide. • Increasing thermal stability of phase change material by adding graphene oxide

  5. Absorption of 14C-stearic acid and 3H-palmitic acid from the intestines of a re-entrant cannulated sheep

    A sheep fitted with a rumen cannula, a simple cannula at the proximal end and a re-entrant cannula at the ileal end of the duodenum, was fed with a normal diet of hay and concentrate. Chromic oxide impregnated on paper and equivalent to 1.5 g, was daily pushed through the rumen during the preliminary feeding period. On the day of the experiment, a mixture of 3H-methyl palmitate and 14C-methyl stearate was introduced into the rumen and the samples of blood, digesta from rumen, upper and lower cannulae were collected at 3 h intervals over a period of 36 hours. The 3H and 14C specific activity time curves of palmitic, stearic and total fatty acids showed a sort of precursor product relationship, in the order of rumen upper and lower cannula, but such a curve for serum lipoprotein fatty acids gave two to three peaks. The percentage absorption between upper and lower cannula was 83.5 for total fatty acids, 85.4 for palmitic acid and 85.2 for stearic acid. (author)

  6. Encapsulating fatty acid esters of bioactive compounds in starch

    Lay Ma, Ursula Vanesa

    Interest in the use of many bioactive compounds in foods is growing in large part because of the apparent health benefits of these molecules. However, many of these compounds can be easily degraded during processing, storage, or their passage through the gastrointestinal tract before reaching the target site. In addition, they can be bitter, acrid, or astringent, which may negatively affect the sensory properties of the product. Encapsulation of these molecules may increase their stability during processing, storage, and in the gastrointestinal tract, while providing controlled release properties. The ability of amylose to form inclusion complexes and spherulites while entrapping certain compounds has been suggested as a potential method for encapsulation of certain molecules. However, complex formation and spherulitic crystallization are greatly affected by the type of inclusion molecules, type of starch, and processing conditions. The objectives of the present investigation were to: (a) study the effect of amylose, amylopectin, and intermediate material on spherulite formation and its microstructure; (b) investigate the formation of amylose and high amylose starch inclusion complexes with ascorbyl palmitate, retinyl palmitate, and phytosterol esters; (c) evaluate the ability of spherulites to form in the presence of fatty acid esters and to entrap ascorbyl palmitate, retinyl palmitate, and phytosterol esters; and (d) evaluate the effect of processing conditions on spherulite formation and fatty acid ester entrapment. Higher ratios of linear to branched molecules resulted in the formation of more and rounder spherulites with higher heat stability. In addition to the presence of branches, it appears that spherulitic crystallization is also affected by other factors, such as degree of branching, chain length, and chain length distribution. Amylose and Hylon VII starch formed inclusion complexes with fatty acid esters of ascorbic acid, retinol, or phytosterols

  7. Dietary interesterified fat enriched with palmitic acid induces atherosclerosis by impairing macrophage cholesterol efflux and eliciting inflammation.

    Afonso, Milessa Silva; Lavrador, Maria Silvia Ferrari; Koike, Marcia Kiyomi; Cintra, Dennys Esper; Ferreira, Fabiana Dias; Nunes, Valeria Sutti; Castilho, Gabriela; Gioielli, Luiz Antonio; Paula Bombo, Renata; Catanozi, Sergio; Caldini, Elia Garcia; Damaceno-Rodrigues, Nilsa Regina; Passarelli, Marisa; Nakandakare, Edna Regina; Lottenberg, Ana Maria

    2016-06-01

    Interesterified fats are currently being used to replace trans fatty acids. However, their impact on biological pathways involved in the atherosclerosis development was not investigated. Weaning male LDLr-KO mice were fed for 16weeks on a high-fat diet (40% energy as fat) containing polyunsaturated (PUFA), TRANS, palmitic (PALM), palmitic interesterified (PALM INTER), stearic (STEAR) or stearic interesterified (STEAR INTER). Plasma lipids, lipoprotein profile, arterial lesion area, macrophage infiltration, collagen content and inflammatory response modulation were determined. Macrophage cholesterol efflux and the arterial expression of cholesterol uptake and efflux receptors were also performed. The interesterification process did not alter plasma lipid concentrations. Although PALM INTER did not increase plasma cholesterol concentration as much as TRANS, the cholesterol enrichment in the LDL particle was similar in both groups. Moreover, PALM INTER induced the highest IL-1β, MCP-1 and IL-6 secretion from peritoneal macrophages as compared to others. This inflammatory response elicited by PALM INTER was confirmed in arterial wall, as compared to PALM. These deleterious effects of PALM INTER culminate in higher atherosclerotic lesion, macrophage infiltration and collagen content than PALM, STEAR, STEAR INTER and PUFA. These events can partially be attributed to a macrophage cholesterol accumulation, promoted by apoAI and HDL2-mediated cholesterol efflux impairment and increased Olr-1 and decreased Abca1 and Nr1h3 expressions in the arterial wall. Interesterified fats containing palmitic acid induce atherosclerosis development by promoting cholesterol accumulation in LDL particles and macrophagic cells, activating the inflammatory process in LDLr-KO mice. PMID:27142741

  8. Dietary ascorbic acid requirements during the hatchery production of turbot larvae

    Merchie, G.; Lavens, P.; Dhert, Ph.; Garcia Ulloa Gómez, M.; Nelis, H.; De leenheer, A P; Sorgeloos, P.

    1996-01-01

    The effect of the high ascorbic acid (AA) levels transferred through enriched live food was evaluated for turbot Scophthalmus maximus larvae in two consecutive feeding experiments. The same feeding strategy was applied to all treatments, except for the AA content in the live food which was manipulated through bioencapsulation with ascorbyl palmitate. This resulted finally in a low, medium and high-AA treatment. The AA incorporation levels in the turbot larvae (up to 1400 µg AA g DW-1) were co...

  9. Endoplasmic reticulum stress involved in high-fat diet and palmitic acid-induced vascular damages and fenofibrate intervention

    Fenofibrate (FF) is widely used to lower blood lipids in clinical practice, but whether its protective effect on endothelium-dependent vasodilatation (EDV) in thoracic aorta is related with endoplasmic reticulum (ER) stress remains unknown. In this study, female Sprauge Dawley rats were divided into standard chow diets (SCD), high-fat diets (HFD) and HFD plus FF treatment group (HFD + FF) randomly. The rats of latter two groups were given HFD feeding for 5 months, then HFD + FF rats were treated with FF (30 mg/kg, once daily) via gavage for another 2 months. The pathological and tensional changes, protein expression of eNOS, and ER stress related genes in thoracic aorta were measured. Then impacts of palmitic acid (PA) and FF on EDV of thoracic aorta from normal female SD rats were observed. Ultimately the expression of ER stress related genes were assessed in primary mouse aortic endothelial cells (MAEC) treated by fenofibric acid (FA) and PA. We found that FF treatment improved serum lipid levels and pathological changes in thoracic aorta, accompanied with decreased ER stress and increased phosphorylation of eNOS. FF pretreatment also improved EDV impaired by different concentrations of PA treatment. The dose- and time-dependent inhibition of cell proliferation by PA were inverted by FA pretreatment. Phosphorylation of eNOS and expression of ER stress related genes were all inverted by FA pretreatment in PA-treated MAEC. Our findings show that fenofibrate recovers damaged EDV by chronic HFD feeding and acute stimulation of PA, this effect is related with decreased ER stress and increased phosphorylation of eNOS. - Highlights: • Fenofibrate treatment improved pathological changes in thoracic aorta by chronic high-fat-diet feeding. • Fenofibrate pretreatment improved endothelium-dependent vasodilation impaired by different concentrations of palmitic acid. • The inhibition of proliferation in endothelial cells by palmitic acid were inverted by fenofibric

  10. Endoplasmic reticulum stress involved in high-fat diet and palmitic acid-induced vascular damages and fenofibrate intervention

    Lu, Yunxia, E-mail: wwwdluyx@sina.com [Department of Biochemistry and Molecular Biology, Anhui Medical University, Hefei, Anhui 230032 (China); The Comprehensive Laboratory, Anhui Medical University, Hefei, Anhui 230032 (China); Cheng, Jingjing [Department of Biochemistry and Molecular Biology, Anhui Medical University, Hefei, Anhui 230032 (China); Chen, Li [Department of Biochemistry and Molecular Biology, Anhui Medical University, Hefei, Anhui 230032 (China); Department of Medical Laboratory, Anhui Provincial Hospital, Hefei, Anhui 230001 (China); Li, Chaofei; Chen, Guanjun [Department of Biochemistry and Molecular Biology, Anhui Medical University, Hefei, Anhui 230032 (China); Gui, Li [The Comprehensive Laboratory, Anhui Medical University, Hefei, Anhui 230032 (China); Shen, Bing [Department of Physiology, Anhui Medical University, Hefei, Anhui 230032 (China); Zhang, Qiu [Department of Endocrinology, First Affiliated Hospital of Anhui Medical University, Hefei, Anhui 230022 (China)

    2015-02-27

    Fenofibrate (FF) is widely used to lower blood lipids in clinical practice, but whether its protective effect on endothelium-dependent vasodilatation (EDV) in thoracic aorta is related with endoplasmic reticulum (ER) stress remains unknown. In this study, female Sprauge Dawley rats were divided into standard chow diets (SCD), high-fat diets (HFD) and HFD plus FF treatment group (HFD + FF) randomly. The rats of latter two groups were given HFD feeding for 5 months, then HFD + FF rats were treated with FF (30 mg/kg, once daily) via gavage for another 2 months. The pathological and tensional changes, protein expression of eNOS, and ER stress related genes in thoracic aorta were measured. Then impacts of palmitic acid (PA) and FF on EDV of thoracic aorta from normal female SD rats were observed. Ultimately the expression of ER stress related genes were assessed in primary mouse aortic endothelial cells (MAEC) treated by fenofibric acid (FA) and PA. We found that FF treatment improved serum lipid levels and pathological changes in thoracic aorta, accompanied with decreased ER stress and increased phosphorylation of eNOS. FF pretreatment also improved EDV impaired by different concentrations of PA treatment. The dose- and time-dependent inhibition of cell proliferation by PA were inverted by FA pretreatment. Phosphorylation of eNOS and expression of ER stress related genes were all inverted by FA pretreatment in PA-treated MAEC. Our findings show that fenofibrate recovers damaged EDV by chronic HFD feeding and acute stimulation of PA, this effect is related with decreased ER stress and increased phosphorylation of eNOS. - Highlights: • Fenofibrate treatment improved pathological changes in thoracic aorta by chronic high-fat-diet feeding. • Fenofibrate pretreatment improved endothelium-dependent vasodilation impaired by different concentrations of palmitic acid. • The inhibition of proliferation in endothelial cells by palmitic acid were inverted by fenofibric

  11. The difluoromethylene (CF2) group in aliphatic chains: Synthesis and conformational preference of palmitic acids and nonadecane containing CF2 groups.

    Wang, Yi; Callejo, Ricardo; Slawin, Alexandra M Z; O'Hagan, David

    2014-01-01

    The syntheses of palmitic acids and a nonadecane are reported with CF2 groups located 1,3 or 1,4 to each other along the aliphatic chain. Specifically 8,8,10,10- and 8,8,11,11-tetrafluorohexadecanoic acids (6b and 6c) are prepared as well as the singly modified analogue 8,8-difluorohexadecanoic acid (6a). Also 8,8,11,11-tetrafluorononadecane (27) is prepared as a pure hydrocarbon containing a 1,4-di-CF2 motif. The modified palmitic acids are characterized by differential scanning calorimetry (DSC) to determine melting points and phase behaviour relative to palmitic acid (62.5 °C). It emerges that 6c, with the CF2 groups placed 1,4- to each other, has a significantly higher melting point (89.9 °C) when compared to the other analogues and palmitic acid itself. It is a crystalline compound and the structure reveals an extended anti-zig-zag chain. Similarly 8,8,11,11-tetrafluorononadecane (27) adopts an extended anti-zig-zag structure. This is rationalized by dipolar relaxation between the two CF2 groups placed 1,4 to each other in the extended anti-zig-zag chain and suggests a design modification for long chain aliphatics which can introduce conformational stability. PMID:24454560

  12. Modelling the influence of palmitic, palmitoleic, stearic and oleic acids on apparent heat resistance of spores of Bacillus cereus NTCC 11145 and Clostridium sporogenes Pasteur 79.3

    Mvou Lekogo, Brice; Coroller, Louis; Mathot, Anne Gabrielle; Mafart, Pierre; Leguérinel, Ivan

    2010-01-01

    Heat resistance of spores is affected by many factors such as temperature, pH, water activity (aw) and others. Previous studies have reported that free fatty acids can affect the germination and growth of bacterial spores. In this study, we investigated the influence of free fatty acids in heating medium or in recovery medium on the heat resistance of spores of Bacillus cereus NTCC 11145 and Clostridium sporogenes Pasteur 79.3. Four free fatty acids were studied: palmitic, palmitoleic, steari...

  13. Formulation and evaluation of hydrous and anhydrous skin whitening products containing sodium ascorbyl phosphate and kojic acid dipalmitate / Marike Ganz

    Ganz, Marike

    2006-01-01

    In Asia skin lightening products have grown to be the best selling skin care products, whereas in the Western hemisphere, including Europe and North America, the main demand is for the treatment of age spots and skin even toning. For African and Asian women, skin lightening is part of their culture, as lighter skin signifies increased wealth and social status. It is believed that blending vitamin C, or its derivates, with kojic acid, or its esters, could synergistically inhibit...

  14. Increase in radioactivity of the trichloroacetic acid-insoluble fraction of the vitamin A-deficient rat retina and its reversal by retinyl palmitate and retinoic acid

    The effect of vitamin A deficiency on body weight of rats, protein content of their retinas and the in vitro incorporation of [3H]leucine, [14C]glucosamine and [3H]fucose into the TCA-insoluble material of these retinas were studied. The results showed that: (1) rats maintained on a vitamin A-deficient diet stopped growing after about 4 weeks on the diet. They maintained a more or less constant weight for about 4 more weeks and then lost weight precipitously. Rats that had been on the vitamin A-deficient diet for 7 weeks resumed growth 2 to 3 weeks after intraperitoneal injection of retinyl palmitate or retinoic acid. (2) Neither vitamin A-deficiency nor its reversal by either retinyl palmitate or retinoic acid had any effect on the protein content of the retinas. (3) The incorporation of [3H]leucine, [14C]glucosamine and [3H]fucose into the TCA-insoluble fraction of the incubated retina was significantly higher in the deficient retina than in the vitamin A-supplemented control. (4) One week after the intraperitoneal injection of deficient rats with retinyl palmitate the incorporation of [14C]glucosamine and [3H]fucose was returned to a level that was not significantly different from that observed in the control. (5) Intraperitoneal injection of deficient rats with retinoic acid decreased the incorporation of [14C]glucosamine into the TCA-insoluble fraction of the retina to a level which was not significantly different from that observed in the control. (author)

  15. Withaferin A protects against palmitic acid-induced endothelial insulin resistance and dysfunction through suppression of oxidative stress and inflammation.

    Batumalaie, Kalaivani; Amin, Muhammad Arif; Murugan, Dharmani Devi; Sattar, Munavvar Zubaid Abdul; Abdullah, Nor Azizan

    2016-01-01

    Activation of inflammatory pathways via reactive oxygen species (ROS) by free fatty acids (FFA) in obesity gives rise to insulin resistance and endothelial dysfunction. Withaferin A (WA), possesses both antioxidant and anti-inflammatory properties and therefore would be a good strategy to suppress palmitic acid (PA)-induced oxidative stress and inflammation and hence, insulin resistance and dysfunction in the endothelium. Effect of WA on PA-induced insulin resistance in human umbilical vein endothelial cells (HUVECs) was determined by evaluating insulin signaling mechanisms whilst effect of this drug on PA-induced endothelial dysfunction was determined in acetylcholine-mediated relaxation in isolated rat aortic preparations. WA significantly inhibited ROS production and inflammation induced by PA. Furthermore, WA significantly decreased TNF-α and IL-6 production in endothelial cells by specifically suppressing IKKβ/NF-κβ phosphorylation. WA inhibited inflammation-stimulated IRS-1 serine phosphorylation and improved the impaired insulin PI3-K signaling, and restored the decreased nitric oxide (NO) production triggered by PA. WA also decreased endothelin-1 and plasminogen activator inhibitor type-1 levels, and restored the impaired endothelium-mediated vasodilation in isolated aortic preparations. These findings suggest that WA inhibited both ROS production and inflammation to restore impaired insulin resistance in cultured endothelial cells and improve endothelial dysfunction in rat aortic rings. PMID:27250532

  16. Diacylglycerol kinase δ phosphorylates phosphatidylcholine-specific phospholipase C-dependent, palmitic acid-containing diacylglycerol species in response to high glucose levels.

    Sakai, Hiromichi; Kado, Sayaka; Taketomi, Akinobu; Sakane, Fumio

    2014-09-19

    Decreased expression of diacylglycerol (DG) kinase (DGK) δ in skeletal muscles is closely related to the pathogenesis of type 2 diabetes. To identify DG species that are phosphorylated by DGKδ in response to high glucose stimulation, we investigated high glucose-dependent changes in phosphatidic acid (PA) molecular species in mouse C2C12 myoblasts using a newly established liquid chromatography/MS method. We found that the suppression of DGKδ2 expression by DGKδ-specific siRNAs significantly inhibited glucose-dependent increases in 30:0-, 32:0-, and 34:0-PA and moderately attenuated 30:1-, 32:1-, and 34:1-PA. Moreover, overexpression of DGKδ2 also enhanced the production of these PA species. MS/MS analysis revealed that these PA species commonly contain palmitic acid (16:0). D609, an inhibitor of phosphatidylcholine-specific phospholipase C (PC-PLC), significantly inhibited the glucose-stimulated production of the palmitic acid-containing PA species. Moreover, PC-PLC was co-immunoprecipitated with DGKδ2. These results strongly suggest that DGKδ preferably metabolizes palmitic acid-containing DG species supplied from the PC-PLC pathway, but not arachidonic acid (20:4)-containing DG species derived from the phosphatidylinositol turnover, in response to high glucose levels. PMID:25112873

  17. Effects of substrate availability and acute ischemia on regional myocardial metabolism demonstrated noninvasively with F-18 deoxyglucose, C-11 palmitic acid and positron computed tomography

    The results indicate that both, F-18 deoxyglucose and C-11 palmitic acid accurately trace different aspects of myocardial metabolism and their changes induced by altered substrate availability and by reduced oxygen supply. Through the pattern of tissue clearance of C-11 palmitic acid, the metabolic fate of Free fatty acids (FFA) can be assessed. Size and turnover rate of the early phase indicate the fraction of C-11 palmitic acid entering immediate oxidation and the rate of oxidation, yet the absence of such a phase does not indicate a metabolic abnormality but merely a shift in myocardial sustrate utilization from FFA to glucose or lactic acid. The normal variability is no longer present when oxygen supply is limited as for example in acute ischemia and this restriction in substrate utilization can be demonstrated with positron computed tomography (PCT). Not only is FFA uptake reduced in proportion to blood flow, but the fraction entering the oxidative pool and its turnover rate are depressed. The regional shift to glucose utilization in acute ischemia is also demonstrated noninvasively by FDG uptake in excess of blood flow and oxygen supply. These studies from the basis for evaluating alternate substrate utilization and tissue viability in myocardial disease

  18. Saturated fatty acid palmitate induces extracellular release of histone H3: A possible mechanistic basis for high-fat diet-induced inflammation and thrombosis

    Highlights: •High-fat diet feeding and palmitate induces the release of nuclear protein histone H3. •ROS production and JNK signaling mediates the release of histone H3. •Extracellular histones induces proinflammatory and procoagulant response. -- Abstract: Chronic low-grade inflammation is a key contributor to high-fat diet (HFD)-related diseases, such as type 2 diabetes, non-alcoholic steatohepatitis, and atherosclerosis. The inflammation is characterized by infiltration of inflammatory cells, particularly macrophages, into obese adipose tissue. However, the molecular mechanisms by which a HFD induces low-grade inflammation are poorly understood. Here, we show that histone H3, a major protein component of chromatin, is released into the extracellular space when mice are fed a HFD or macrophages are stimulated with the saturated fatty acid palmitate. In a murine macrophage cell line, RAW 264.7, palmitate activated reactive oxygen species (ROS) production and JNK signaling. Inhibitors of these pathways dampened palmitate-induced histone H3 release, suggesting that the extracellular release of histone H3 was mediated, in part, through ROS and JNK signaling. Extracellular histone activated endothelial cells toexpress the adhesion molecules ICAM-1 and VCAM-1 and the procoagulant molecule tissue factor, which are known to contribute to inflammatory cell recruitment and thrombosis. These results suggest the possible contribution of extracellular histone to the pathogenesis of HFD-induced inflammation and thrombosis

  19. Saturated fatty acid palmitate induces extracellular release of histone H3: A possible mechanistic basis for high-fat diet-induced inflammation and thrombosis

    Shrestha, Chandan [Department of Systems Biology in Thromboregulation, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima (Japan); Department of Laboratory and Vascular Medicine, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima (Japan); Ito, Takashi [Department of Systems Biology in Thromboregulation, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima (Japan); Kawahara, Ko-ichi [Department of Biomedical Engineering, Osaka Institute of Technology, Osaka (Japan); Shrestha, Binita; Yamakuchi, Munekazu; Hashiguchi, Teruto [Department of Laboratory and Vascular Medicine, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima (Japan); Maruyama, Ikuro, E-mail: rinken@m3.kufm.kagoshima-u.ac.jp [Department of Systems Biology in Thromboregulation, Kagoshima University Graduate School of Medical and Dental Sciences, Kagoshima (Japan)

    2013-08-09

    Highlights: •High-fat diet feeding and palmitate induces the release of nuclear protein histone H3. •ROS production and JNK signaling mediates the release of histone H3. •Extracellular histones induces proinflammatory and procoagulant response. -- Abstract: Chronic low-grade inflammation is a key contributor to high-fat diet (HFD)-related diseases, such as type 2 diabetes, non-alcoholic steatohepatitis, and atherosclerosis. The inflammation is characterized by infiltration of inflammatory cells, particularly macrophages, into obese adipose tissue. However, the molecular mechanisms by which a HFD induces low-grade inflammation are poorly understood. Here, we show that histone H3, a major protein component of chromatin, is released into the extracellular space when mice are fed a HFD or macrophages are stimulated with the saturated fatty acid palmitate. In a murine macrophage cell line, RAW 264.7, palmitate activated reactive oxygen species (ROS) production and JNK signaling. Inhibitors of these pathways dampened palmitate-induced histone H3 release, suggesting that the extracellular release of histone H3 was mediated, in part, through ROS and JNK signaling. Extracellular histone activated endothelial cells toexpress the adhesion molecules ICAM-1 and VCAM-1 and the procoagulant molecule tissue factor, which are known to contribute to inflammatory cell recruitment and thrombosis. These results suggest the possible contribution of extracellular histone to the pathogenesis of HFD-induced inflammation and thrombosis.

  20. Enteric neuropathy can be induced by high fat diet in vivo and palmitic acid exposure in vitro.

    Ulrikke Voss

    Full Text Available OBJECTIVE: Obese and/or diabetic patients have elevated levels of free fatty acids and increased susceptibility to gastrointestinal symptoms. Since the enteric nervous system is pivotal in regulating gastrointestinal functions alterations or neuropathy in the enteric neurons are suspected to occur in these conditions. Lipid induced intestinal changes, in particular on enteric neurons, were investigated in vitro and in vivo using primary cell culture and a high fat diet (HFD mouse model. DESIGN: Mice were fed normal or HFD for 6 months. Intestines were analyzed for neuronal numbers, remodeling and lipid accumulation. Co-cultures of myenteric neurons, glia and muscle cells from rat small intestine, were treated with palmitic acid (PA (0 - 10(-3 M and / or oleic acid (OA (0 - 10(-3 M, with or without modulators of intracellular lipid metabolism. Analyses were by immunocyto- and histochemistry. RESULTS: HFD caused substantial loss of myenteric neurons, leaving submucous neurons unaffected, and intramuscular lipid accumulation in ileum and colon. PA exposure in vitro resulted in neuronal shrinkage, chromatin condensation and a significant and concentration-dependent decrease in neuronal survival; OA exposure was neuroprotective. Carnitine palmitoyltransferase 1 inhibition, L-carnitine- or alpha lipoic acid supplementation all counteracted PA-induced neuronal loss. PA or OA alone both caused a significant and concentration-dependent loss of muscle cells in vitro. Simultaneous exposure of PA and OA promoted survival of muscle cells and increased intramuscular lipid droplet accumulation. PA exposure transformed glia from a stellate to a rounded phenotype but had no effect on their survival. CONCLUSIONS: HFD and PA exposure are detrimental to myenteric neurons. Present results indicate excessive palmitoylcarnitine formation and exhausted L-carnitine stores leading to energy depletion, attenuated acetylcholine synthesis and oxidative stress to be main

  1. EGFR Inhibition Blocks Palmitic Acid-induced inflammation in cardiomyocytes and Prevents Hyperlipidemia-induced Cardiac Injury in Mice.

    Li, Weixin; Fang, Qilu; Zhong, Peng; Chen, Lingfeng; Wang, Lintao; Zhang, Yali; Wang, Jun; Li, Xiaokun; Wang, Yi; Wang, Jingying; Liang, Guang

    2016-01-01

    Obesity is often associated with increased risk of cardiovascular diseases. Previous studies suggest that epidermal growth factor receptor (EGFR) antagonism may be effective for the treatment of angiotensin II-induced cardiac hypertrophy and diabetic cardiomyopathy. This study was performed to demonstrate if EGFR plays a role in the pathogenesis of hyperlipidemia/obesity-related cardiac injuries. The in vivo studies using both wild type (WT) and apolipoprotein E (ApoE) knockout mice fed with high fat diet (HFD) showed the beneficial effects of small-molecule EGFR inhibitors, AG1478 and 542, against obesity-induced myocardial injury. Administration of AG1478 and 542 significantly reduced myocardial inflammation, fibrosis, apoptosis, and dysfunction in both two obese mouse models. In vitro, EGFR signaling was blocked by either siRNA silencing or small-molecule EGFR inhibitors in palmitic acid (PA)-stimulated cardiomyocytes. EGFR inhibition attenuated PA-induced inflammatory response and apoptosis in H9C2 cells. Furthermore, we found that PA-induced EGFR activation was mediated by the upstream TLR4 and c-Src. This study has confirmed the detrimental effect of EGFR activation in the pathogenesis of obesity-induced cardiac inflammatory injuries in experimental mice, and has demonstrated the TLR4/c-Src-mediated mechanisms for PA-induced EGFR activation. Our data suggest that EGFR may be a therapeutic target for obesity-related cardiovascular diseases. PMID:27087279

  2. Study of Enzymatic Synthesis of L-ascorbyl Fatty Acid Esters in Tert-amyl Alcohol%叔戊醇体系中酶法合成L-抗坏血酸脂肪酸酯的研究

    张洪勇; 钱俊青

    2011-01-01

    研究以棕榈油为酰基供体和L-抗坏血酸在有机相中利用脂肪酶催化酯交换反应合成L-抗坏血酸脂肪酸酯.对催化合成L-抗坏血酸脂肪酸酯的反应介质进行了比较,系统考察了底物浓度、溶剂用量、底物摩尔比、温度、水活度、分子筛加入时间和加入量对酶催化反应的影响,确定了最适反应条件:在20 mL用分子筛充分除水的叔戊醇中,0.352g·L-1抗坏血酸和4.535 g棕榈油(L-抗坏血酸和脂肪酸的底物摩尔比为1∶8)在14.2%(w/w,酶/L-抗坏血酸)的脂肪酶Novo435催化作用下,反应初始加入50 g·L-1的分子筛,温度55℃,摇床转速200 r ·min-1,反应24 h后底物转化率可达65%,产物浓度可达22 g·L-1.%The synthesis of L-ascorbyl fatty acid esters through transesterification of ascorbic acid and palm oil in tert-amy\\ alcohol catalyzed by immobilized lipase was studied. A series of solvents used for the reaction were investigated, among them the tert-amyl alcohol was found to be the most suitable reaction media for the enzymatic synthesis of L-ascorbyl fatty acid esters. The addition of the molecular sieves was found to be helpful for reaction system to keep the water activity and to make the equilibrium go to the product. The factors affecting catalytic leaction, such as the substrate concentration, amount of solvent, substrate molar ratio, temperature, water activity and the addition of molecular sieve, were investigated. The results show that, when 0.352 g ascorbic acid and 4.535 g palm oil (the molar ratio of ascorbic acid to fatty acid is 1:8) are catalyzed by 14.2% Novo435 (weight % of ascorbic acid) in 20 mL terf-amyl alcohol with 50 g·L-1 molecular sieve added and rotation speed of 200 r·min-1, the conversion of ascorbic acid can reach 65% and the concentration of L-ascorbyl fatty acid esters is 22 g·L-1 after 24 h reaction at 55℃.

  3. Induction of Gnrh mRNA expression by the ω-3 polyunsaturated fatty acid docosahexaenoic acid and the saturated fatty acid palmitate in a GnRH-synthesizing neuronal cell model, mHypoA-GnRH/GFP.

    Tran, Dean Q; Ramos, Ernesto H; Belsham, Denise D

    2016-05-01

    Gonadotropin-releasing hormone (GnRH) neurons coordinate reproduction. However, whether GnRH neurons directly sense free fatty acids (FFAs) is unknown. We investigated the individual effects of the FFAs docosahexaenoic acid (DHA), palmitate, palmitoleate, and oleate (100 μM each) on Gnrh mRNA expression in the mHypoA-GnRH/GFP neuronal cell model. We report that 2 h exposure to palmitate or DHA increases Gnrh transcription. Using the inhibitors AH7614, K252c, U0126, wortmannin, and LY294002, we demonstrate that the effect of DHA is mediated through GPR120 to downstream PKC/MAPK and PI3K signaling. Our results indicate that the effect of palmitate may depend on palmitoyl-coA synthesis and PI3K signaling. Finally, we demonstrate that both DHA and palmitate increase Gnrh enhancer-derived RNA levels. Overall, these studies provide evidence that GnRH neurons directly sense FFAs. This will advance our understanding of the mechanisms underlying FFA sensing in the brain and provides insight into the links between nutrition and reproductive function. PMID:26923440

  4. CPT1α over-expression increases long-chain fatty acid oxidation and reduces cell viability with incremental palmitic acid concentration in 293T cells

    To test the cellular response to an increased fatty acid oxidation, we generated a vector for an inducible expression of the rate-limiting enzyme carnitine palmitoyl-transferase 1α (CPT1α). Human embryonic 293T kidney cells were transiently transfected and expression of the CPT1α transgene in the tet-on vector was activated with doxycycline. Fatty acid oxidation was measured by determining the conversion of supplemented, synthetic cis-10-heptadecenoic acid (C17:1n-7) to C15:ln-7. CPT1α over-expression increased mitochondrial long-chain fatty acid oxidation about 6-fold. Addition of palmitic acid (PA) decreased viability of CPT1α over-expressing cells in a concentration-dependent manner. Both, PA and CPT1α over-expression increased cell death. Interestingly, PA reduced total cell number only in cells over-expressing CPT1α, suggesting an effect on cell proliferation that requires PA translocation across the mitochondrial inner membrane. This inducible expression system should be well suited to study the roles of CPT1 and fatty acid oxidation in lipotoxicity and metabolism in vivo

  5. Brain region-specificity of palmitic acid-induced abnormalities associated with Alzheimer's disease

    Melrose Joseph; Balu Deebika; Patil Sachin; Chan Christina

    2008-01-01

    Abstract Background Alzheimer's disease (AD) is a progressive, neurodegenerative disease mostly affecting the basal forebrain, cortex and hippocampus whereas the cerebellum is relatively spared. The reason behind this region-specific brain damage in AD is not well understood. Here, we report our data suggesting "differential free fatty acid metabolism in the different brain areas" as a potentially important factor in causing the region-specific damage observed in AD brain. Findings The astrog...

  6. Determination of Fatty Acid Metabolism with Dynamic 11C-Palmitate Positron Emission Tomography of Mouse Heart In Vivo

    Li, Yinlin; Huang, Tao; Zhang, Xinyue; Zhong, Min; Walker, Natalie N.; He, Jiang; Berr, Stuart S.; Keller, Susanna R.; Kundu, Bijoy K.

    2015-01-01

    The goal of this study was to establish a quantitative method for measuring FA metabolism with partial volume (PV) and spill-over (SP) corrections using dynamic 11C-palmitate PET images of mouse heart in vivo. Methods Twenty-minute dynamic 11C-palmitate PET scans of four 18–20 week old male C57BL/6 mice under isoflurane anesthesia were performed using a Focus 120 PET scanner. A model corrected blood input function (MCIF), by which the input function with SP and PV corrections and the metabolic rate constants (k1−k5) are simultaneously estimated from the dynamic 11C-palmitate PET images of mouse hearts in a 4-compartment tracer kinetic model, was used to determine rates of myocardial FA oxidation (MFAO), myocardial FA esterification (MFAE), myocardial FA utilization (MFAU) and myocardial FA uptake (MFAUp). Results The MFAO thus measured in C57BL/6 mice was 375.03±43.83 nmoles/min/g. This compares well with the MFAO measured in perfused working C57BL/6 mouse hearts ex vivo of about 350 nmoles/g/min and 400 nmoles/min/g. Conclusions FA metabolism was measured for the first time in mouse heart in vivo using dynamic 11C-palmitate PET in a 4-compartment tracer kinetic model. MFAO obtained with this model were validated by results previously obtained with mouse hearts ex vivo. PMID:26462138

  7. Chemo-enzymatic synthesis of vinyl and l-ascorbyl phenolates and their inhibitory effects on advanced glycation end products.

    Hwang, Seung Hwan; Wang, Zhiqiang; Lim, Soon Sung

    2017-01-01

    This study successfully established the feasibility of a two-step chemo-enzymatic synthesis of l-ascorbyl phenolates. Intermediate vinyl phenolates were first chemically produced and then underwent trans-esterification with l-ascorbic acid in the presence of Novozyme 435® (Candida Antarctica lipase B) as a catalyst. Twenty vinyl phenolates and 11 ascorbyl phenolates were subjected to in vitro bioassays to investigate their inhibitory activity against advanced glycation end products (AGEs). Among them, vinyl 4-hydroxycinnamate (17VP), vinyl 4-hydroxy-3-methoxycinnamate (18VP), vinyl 4-hydroxy-3,5-dimethoxycinnamate (20VP), ascorbyl 4-hydroxy-3-methoxycinnamate (18AP) and ascorbyl 3,4-dimethoxycinnamate (19AP) showed 2-10 times stronger inhibitory activities than positive control (aminoguanidine and its precursors). These results indicated that chemo-enzymatically synthesized compounds have AGE inhibitory effect and thus are effective in either preventing or retarding glycation protein formation. PMID:27507531

  8. Palmitic Acid Induces Production of Proinflammatory Cytokines Interleukin-6, Interleukin-1β, and Tumor Necrosis Factor-α via a NF-κB-Dependent Mechanism in HaCaT Keratinocytes

    Bing-rong Zhou

    2013-01-01

    Full Text Available To investigate whether palmitic acid can be responsible for the induction of inflammatory processes, HaCaT keratinocytes were treated with palmitic acid at pathophysiologically relevant concentrations. Secretion levels of interleukin-6 (IL-6, tumor necrosis factor-α (TNF-α, interleukin-1β (IL-1β, NF-κB nuclear translocation, NF-κB activation, Stat3 phosphorylation, and peroxisome proliferator-activated receptor alpha (PPARα mRNA and protein levels, as well as the cell proliferation ability were measured at the end of the treatment and after 24 hours of recovery. Pyrrolidine dithiocarbamate (PDTC, a selective chemical inhibitor of NF-κB and goat anti-human IL-6 polyclonal neutralizing antibody were used to inhibit NF-κB activation and IL-6 production, respectively. Our results showed that palmitic acid induced an upregulation of IL-6, TNF-α, IL-1β secretions, accompanied by NF-κB nuclear translocation and activation. Moreover, the effect of palmitic acid was accompanied by PPARα activation and Stat3 phosphorylation. Palmitic acid-induced IL-6, TNF-α, IL-1β productions were attenuated by NF-κB inhibitor PDTC. Palmitic acid was administered in amounts able to elicit significant hyperproliferation and can be attenuated by IL-6 blockage. These data demonstrate for the first time that palmitic acid can stimulate IL-6, TNF-α, IL-1β productions in HaCaT keratinocytes and cell proliferation, thereby potentially contributing to acne inflammation and pilosebaceous duct hyperkeratinization.

  9. Pulmonary lung surfactant synthetic peptide concentration-dependent modulation of DPPC and POPG acyl chain order in a DPPC:POPG:palmitic acid lipid mixture.

    Krill, S L; Gupta, S L; Smith, T

    1994-05-01

    Lung surfactant-associated protein interaction with lipid matrices and the effects on lipid thermotropic phase behavior are areas of active research. Many studies limit the lipids to a single or two-component system. The current investigation utilizes a three-lipid component matrix (DPPC:POPG:palmitic acid) to investigate the impact of a synthetic surfactant protein B fragment (SP-B 53-78 DiACM) on the dynamic surface activity of the lipid admixture as measured by a Wilhelmy surface balance. Also, the modulation of the individual lipid acyl chain order by the peptide within the lipid matrix is studied through the use of thermal perturbation FTIR spectroscopy. The data clearly demonstrate a concentration-dependent effect of the peptide on the surface activity with an improvement in the dynamic surface tension diagram characteristics (decreased surface tension and increased collapse plateau) especially at low, 0.36 M%, peptide concentrations. These effects are diminished upon further addition of the peptide. FTIR spectral data demonstrate that the peptide addition results in a significant increase in the acyl chain order of the DPPC and POPG components as measured by the position of the methylene stretching vibrational bands. DPPC is most sensitive to the peptide presence, while the palmitic acid is least affected. The transition temperatures of the individual lipids are also increased with the addition of the peptide. The presence of POPG in the matrix achieves the surface activity similarly seen with natural lung surfactant relative to a DPPC/palmitic acid lipid matrix alone. Its presence increases the sensitivity of the DPPC acyl chains to the presence of the peptide. These effects on the chain order are most probably related to the increased acyl chain fluidity which POPG imparts to the lipid matrix because of the presence of the cis double bond. The phosphatidylglycerol headgroup also adds a negative charge to the lipid matrix which enhances the peptide

  10. Countercurrent Chromatographic Separation of Lipophilic Ascorbic Acid Derivatives and Extract from Kadsura Coccinea Using Hydrophobic Organic-Aqueous Two-Phase Solvent Systems

    Shinomiya, Kazufusa; Li, Heran; Kitanaka, Susumu; Ito, Yoichiro

    2009-01-01

    Countercurrent chromatographic (CCC) separation of lipophilic ascorbic acid derivatives and the crude extract from Kadsura Coccinea was performed using the type-J multilayer coil planet centrifuge with a hydrophobic organic-aqueous two-phase solvent system composed of n-hexane/ethyl acetate/ethanol/aqueous 0.1% trifluoroacetic acid at the volume ratio of (5 : 5 : 6 : 2). The lipophilic ascorbic acid derivatives were separated in the order of L-ascrobyl 2,6-dibutyrate, L-ascorbyl 6-palmitate a...

  11. Synthesis and preliminary evaluation of 18F-labeled 4-thia palmitate as a PET tracer of myocardial fatty acid oxidation

    Interest remains strong for the development of a noninvasive technique for assessment of regional fatty acid oxidation rate in the myocardium. 18F-labeled 4-thia palmitate (FTP, 16-[18F]fluoro-4-thia-hexadecanoic acid) has been synthesized and preliminarily evaluated as a metabolically trapped probe of myocardial fatty acid oxidation for positron emission tomography (PET). The radiotracer is synthesized by Kryptofix 2.2.2/K2CO3 assisted nucleophilic radiofluorination of an iodo-ester precursor, followed by alkaline hydrolysis and by purification by reverse phase high performance liquid chromatography. Biodistribution studies in rats showed high uptake and long retention of FTP in heart, liver, and kidneys consistent with relatively high fatty acid oxidation rates in these tissues. Inhibition of carnitine palmitoyl-transferase-I caused an 80% reduction in myocardial uptake, suggesting the dependence of trapping on the transport of tracer into the mitochondrion. Experiments with perfused rat hearts showed that the estimates of the fractional metabolic trapping rate (FR) of FTP tracked inhibition of oxidation rate of palmitate with hypoxia, whereas the FR of the 6-thia analog 17-[18F]fluoro-6-thia-heptadecanoic acid was insensitive to hypoxia. In vivo defluorination of FTP in the rat was evidenced by bone uptake of radioactivity. A PET imaging study with FTP in normal swine showed excellent myocardial images, prolonged myocardial retention, and no bone uptake of radioactivity up to 3 h, the last finding suggesting a species dependence for defluorination of the omega-labeled fatty acid. The results support further investigation of FTP as a potential PET tracer for assessing regional fatty acid oxidation rate in the human myocardium

  12. Synthesis and preliminary evaluation of {sup 18}F-labeled 4-thia palmitate as a PET tracer of myocardial fatty acid oxidation

    DeGrado, Timothy R. E-mail: trd@petsparc.mc.duke.edu; Wang Shuyan; Holden, James E.; Nickles, R. Jerome; Taylor, Michael; Stone, Charles K

    2000-04-01

    Interest remains strong for the development of a noninvasive technique for assessment of regional fatty acid oxidation rate in the myocardium. {sup 18}F-labeled 4-thia palmitate (FTP, 16-[{sup 18}F]fluoro-4-thia-hexadecanoic acid) has been synthesized and preliminarily evaluated as a metabolically trapped probe of myocardial fatty acid oxidation for positron emission tomography (PET). The radiotracer is synthesized by Kryptofix 2.2.2/K{sub 2}CO{sub 3} assisted nucleophilic radiofluorination of an iodo-ester precursor, followed by alkaline hydrolysis and by purification by reverse phase high performance liquid chromatography. Biodistribution studies in rats showed high uptake and long retention of FTP in heart, liver, and kidneys consistent with relatively high fatty acid oxidation rates in these tissues. Inhibition of carnitine palmitoyl-transferase-I caused an 80% reduction in myocardial uptake, suggesting the dependence of trapping on the transport of tracer into the mitochondrion. Experiments with perfused rat hearts showed that the estimates of the fractional metabolic trapping rate (FR) of FTP tracked inhibition of oxidation rate of palmitate with hypoxia, whereas the FR of the 6-thia analog 17-[{sup 18}F]fluoro-6-thia-heptadecanoic acid was insensitive to hypoxia. In vivo defluorination of FTP in the rat was evidenced by bone uptake of radioactivity. A PET imaging study with FTP in normal swine showed excellent myocardial images, prolonged myocardial retention, and no bone uptake of radioactivity up to 3 h, the last finding suggesting a species dependence for defluorination of the omega-labeled fatty acid. The results support further investigation of FTP as a potential PET tracer for assessing regional fatty acid oxidation rate in the human myocardium.

  13. Lipidomic-based investigation into the regulatory effect of Schisandrin B on palmitic acid level in non-alcoholic steatotic livers

    Kwan, Hiu Yee; Niu, Xuyan; Dai, Wenlin; Tong, Tiejun; Chao, Xiaojuan; Su, Tao; Chan, Chi Leung; Lee, Kim Chung; Fu, Xiuqiong; Yi, Hua; Yu, Hua; Li, Ting; Tse, Anfernee Kai Wing; Fong, Wang Fun; Pan, Si-Yuan; Lu, Aiping; Yu, Zhi-Ling

    2015-01-01

    Schisandrin B (SchB) is one of the most abundant bioactive dibenzocyclooctadiene derivatives found in the fruit of Schisandra chinensis. Here, we investigated the potential therapeutic effects of SchB on non-alcoholic fatty-liver disease (NAFLD). In lipidomic study, ingenuity pathway analysis highlighted palmitate biosynthesis metabolic pathway in the liver samples of SchB-treated high-fat-diet-fed mice. Further experiments showed that the SchB treatment reduced expression and activity of fatty acid synthase, expressions of hepatic mature sterol regulatory element binding protein-1 and tumor necrosis factor-α, and hepatic level of palmitic acid which is known to promote progression of steatosis to steatohepatitis. Furthermore, the treatment also reduced hepatic fibrosis, activated nuclear factor-erythroid-2-related factor-2 which is known to attenuate the progression of NASH-related fibrosis. Interestingly, in fasting mice, a single high-dose SchB induced transient lipolysis and increased the expressions of adipose triglyceride lipase and phospho-hormone sensitive lipase. The treatment also increased plasma cholesterol levels and 3-hydroxy-3-methylglutaryl-CoA reductase activity, reduced the hepatic low-density-lipoprotein receptor expression in these mice. Our data not only suggest SchB is a potential therapeutic agent for NAFLD, but also provided important information for a safe consumption of SchB because SchB overdosed under fasting condition will have adverse effects on lipid metabolism. PMID:25766252

  14. In Vivo RNAi Efficacy of Palmitic Acid-Conjugated Dicer-Substrate siRNA in a Subcutaneous Tumor Mouse Model.

    Kubo, Takanori; Yanagihara, Kazuyoshi; Seyama, Toshio

    2016-06-01

    Short interfering RNAs are used in RNA interference technology and are powerful tools for target gene silencing in a sequence-specific manner. In this study, we synthesized Dicer-substrate siRNAs consisting of 27-nt double-stranded RNAs conjugated with palmitic acid at the 5'-end of the sense strand and investigated their RNA interference efficacies in vitro and in vivo. The palmitic acid-conjugated 27-nt DsiRNAs (C16-Dsi27RNAs) were prepared by our simple synthesis strategy and achieved a good yield. C16-Dsi27RNAs showed enhanced in vitro RNA interference potency compared with not only non-modified Dsi27RNAs but also cholesterol-conjugated Dsi27RNAs against both an exogenous enhanced green fluorescent protein and the endogenous vascular endothelial growth factor gene in a human scirrhous-type gastric cancer cell line that stably expressed the enhanced green fluorescent protein gene (GCIY-eGFP). Additionally, C16-Dsi27RNAs had potent gene silencing activity against both enhanced green fluorescent protein and vascular endothelial growth factor as target genes in a subcutaneous tumor mouse model generated from GCIY-eGFP cells administered by intratumoral injection. These results suggest that the C16-Dsi27RNAs will be useful next-generation RNA interference molecules that can overcome the problems associated with RNA interference technology. PMID:26800111

  15. Comparison of 11-C-Palmitic Acid (CPA), and 123-I-heptadecanoic acid (IHA) turnover in human heart

    This study was designed to compare the results obtained with IHA in the investigation of myocardial fatty acid metabolism (MFAM) with those obtained by the use of CPA.- 8 patients (pts) without clinical signs of heart or metabolic disease were investigated under rest and fasting condition by dynamic PET following i.v. injection of 3 mCi CPA and by conventional scintigraphy following i.v. injection of 3 mCi IHA. Data were collected over a period of 90 min (frame rate was 1/min) and corrected for blood activity and catabolically released 123-I.-In 6 pts a good agreement between CPA and IHA data was observed. The activity release from the myocardium in these cases was biexponential. The ratio Q ranged between 0.7 and 6.7. -In the remaining 2 pts significant discrepancies between CPA and IHA data were observed. Since these pts were known to have cardiac neurosis and the first measurement was carried out with CPA, the authors assumed that the anxiety of the pt during CPA examination is responsible for the changing of the MFAM. This was confirmed by examination of these pts with IHA under mental stress. In both vases the data obtained by the use of CPA agree closely with those obtained by the use of IHA under mental stress. These data indicate that both CPA and IHa are applicable for studying MFAM and that in external assessment of MFAM, not only the dietary status, but also the mental state of the pts should be considered

  16. Comparison of 11-C-Palmitic Acid (CPA), and 123-I-heptadecanoic acid (IHA) turnover in human heart

    Notohamiprodjo, G.; Schmid, A.; Spohr, G.; Vyska, K.; Feinendegen, L.E.

    1985-05-01

    This study was designed to compare the results obtained with IHA in the investigation of myocardial fatty acid metabolism (MFAM) with those obtained by the use of CPA.- 8 patients (pts) without clinical signs of heart or metabolic disease were investigated under rest and fasting condition by dynamic PET following i.v. injection of 3 mCi CPA and by conventional scintigraphy following i.v. injection of 3 mCi IHA. Data were collected over a period of 90 min (frame rate was 1/min) and corrected for blood activity and catabolically released 123-I.-In 6 pts a good agreement between CPA and IHA data was observed. The activity release from the myocardium in these cases was biexponential. The ratio Q ranged between 0.7 and 6.7. -In the remaining 2 pts significant discrepancies between CPA and IHA data were observed. Since these pts were known to have cardiac neurosis and the first measurement was carried out with CPA, the authors assumed that the anxiety of the pt during CPA examination is responsible for the changing of the MFAM. This was confirmed by examination of these pts with IHA under mental stress. In both vases the data obtained by the use of CPA agree closely with those obtained by the use of IHA under mental stress. These data indicate that both CPA and IHa are applicable for studying MFAM and that in external assessment of MFAM, not only the dietary status, but also the mental state of the pts should be considered.

  17. Effects of Artemia enriched with unsaturated fatty acids and vitamin C on growth, survival and resistance Salmo trutta caspius larvae

    Javaheri baboli, Mehran

    2006-01-01

    This experiment was conducted to investigate the effect of using n-3 HUFA and Vitamin C enriched Artemia urmiana Nauplii Five difference treament were tested: for Caspian salmon (Salmo trutta caspius) larvae compare with artificial food in five treatment: (1) Artificial food, (2) Newly hatched Artemia (3) n-3 HUFA enriched Artemia (4) n-3 HUFA + 10% Ascorbyl Palmitate enriched Artemia (5) n-3 HUFA+20% Ascorbyl palmitate enriched Artemia during 15 days then all treatment were fe...

  18. Monocyte adhesion induced by multi-walled carbon nanotubes and palmitic acid in endothelial cells and alveolar-endothelial co-cultures

    Cao, Yi; Roursgaard, Martin; Jacobsen, Nicklas Raun;

    2016-01-01

    Free palmitic acid (PA) is a potential pro-atherogenic stimulus that may aggravate particle-mediated cardiovascular health effects. We hypothesized that the presence of PA can aggravate oxidative stress and endothelial activation induced by multi-walled carbon nanotube (MWCNT) exposure in vitro. We...... investigated the interaction between direct exposure to MWCNTs and PA on THP-1 monocyte adhesion to human umbilical vein endothelial cells (HUVECs), as well as on indirect exposure in an alveolar-endothelial co-culture model with A549 cells and THP-1-derived macrophages exposed in inserts and the effect...... monocultures. Both effects were found to be independent of the presence of PA. MWCNT exposure significantly increased THP-1 monocyte adhesion to HUVECs, and co-exposure to PA aggravated the NM400-mediated adhesion but decreased the NM402-mediated adhesion. For the co-cultures, the exposure of A549 cells did...

  19. Preparation of carbon-11 labelled acetate and palmitic acid for the study of myocardial metabolism by emission-computerised axial tomography

    Methods have been developed for the labelling of acetate and palmitic acid with the positron-emitting radionuclide, 11C(T=20.4 min). Labelling was achieved via carbonation of the appropriate alkyl magnesium bromide (methyl magnesium bromide or n-pentadecyl magnesium bromide) with 11C-labelled carbon dioxide produced by the 14Np(p,α)11C nuclear reaction. The radiochemical yield and speed of each method of labelling are such that a radiochemically pure product is obtained in injectable form and in activity (>10 mCi) suitable for the study of myocardial metabolism by emission-computerised axial tomography. High pressure liquid chromatography and thin layer chromatography were used to assess the radiochemical purity of each radiopharmaceutical. The specific activity of 11C-labelled acetate was estimated by an enzymic procedure to be greater than 0.5 Ci/μmole. (author)

  20. Ternary Liquid-Liquid Equilibrium for Systems of Fatty Acid Methyl Ester(Methyl Palmitate/Methyl Stearate)+Ethanol+Glycerol at Atmospheric Pressure

    夏淑倩; 罗慧娟; 马沛生

    2015-01-01

    Liquid-liquid equilibrium data of two ternary systems methyl palmitate+ethanol+glycerol and methyl stearate+ethanol+glycerol at(318.2 and 333.2)K and atmospheric pressure were measured. The values of distri-bution coefficient and selectivity were calculated, which indicates that glycerol can be separated from fatty acid ester by using ethanol as an extraction solvent. The consistency of the isothermal tie-line data were checked by the Othmer-Tobias equation. The correlation coefficients R2 are higher than 0.993,9 for all the fitted curves. The NRTL activity coefficient model was applied to the correlation of the measured tie-line data. The root mean square devia-tion(RMSD)values are less than 0.007 for all the systems, which shows a good predictive capability of this model for such systems.

  1. 酶催化合成维生素C脂肪酸酯的反应条件优化%Optimization of the enzymatic synthesis of L-ascorbyl fatty acid esters

    宋秋红; 王熙; 田平芳

    2009-01-01

    以维生素C(Vc)和若干种脂肪酸为底物,采用自制假丝酵母Candida sp. 99-125固定化脂肪酶,催化合成维生素C脂肪酸酯.结果表明,在该酯化反应中,油酸为最佳脂肪酸底物,丙酮为最佳反应介质.同时研究了各反应因素对Vc转化率的影响,优化后的反应条件为:当Vc浓度为0.06mol/L时,温度40*#℃,固定化酶量1.5*#g,油酸与Vc物质的量比为5∶1,反应时间48*#h,分子筛添加量0.5*#g,底物Vc分4次流加,Vc转化率可达91%,批次实验表明该固定化酶在重复使用10次后仍具较高活力.%The enzymatic synthesis of L-ascorbyl fatty acid esters (AFAE) has been studied using a self-made immobilized lipase generated by Candida sp. 99 - 125 as the biocatalyst. Oleic acid was found to be the best source of a fatty acid acyl group in the synthesis of AFAEs. Through screening of different reaction media, ace-tone was found to be the most suitable solvent for the esterification. The effects of various other factors on the synthesis of AFAEs were also investigated. Under the following optimized reaction conditions: initial ascorbic acid (vitamin C) concentration (Vc) of 0.06mol/L at 40℃, 1.5g of immobilized enzyme, substrate molar ratio of 5:1, reaction time of 48 h, content of molecular sieve of 0.5 g and four times fed-batch addition of the sub-strate, an esterification ratio of 91 % was obtained. Furthermore, repeated batch reactions revealed the durabili-ty of the immobilized lipase, which retained high activity after sequential reaction for 10 rounds.

  2. Evaluation of the antiaggregant activity of ascorbyl phenolic esters with antioxidant properties.

    Lopez, Esther; del Carmen Ortega-Liébana, María; Salido, Sofía; Salido, Ginés M; Altarejos, Joaquín; Rosado, Juan A; Redondo, Pedro C

    2015-09-01

    Beneficial effects of the antioxidant L-ascorbic acid (Asc) in human health are well known. Its particular role in hemostasis deserves further consideration, since it has been described a dose-dependent effect of Asc in platelet activity. Contrary, it has been demonstrated that phenolic compounds have inhibitory effects on platelet aggregation stimulated by the physiological agonist thrombin (Thr). Here, we have evaluated the actions of three synthetic phenolic esters of Asc: L-ascorbyl 6-protocatechuate (Prot Asc), L-ascorbyl 6-gallate (Gal Asc), and L-ascorbyl 6-caffeate (Caf Asc). All these Asc derivatives exhibited greater radical scavenging activity than Asc, and in experiments using human platelets from healthy subjects, they do not evoke changes in platelet viability upon their administration. Nevertheless, these compounds altered platelet calcium homeostasis in response to Thr, although Prot Asc induced a smaller effect than Gal Asc, Caf Asc, and Asc. As a consequence, platelet aggregation was also impaired by these compounds, reporting Prot Asc and Caf Asc a weaker antiaggregant action than Gal Asc and Asc. Treatments with Gal Asc and Caf Asc altered in larger extent the phosphorylation pattern of pp60(Src) and mammalian target of rapamycin (mTOR) evoked by stimulating human platelets with Thr. Summarizing, Prot Asc is the ascorbyl phenolic ester with the strongest antioxidant properties and weakest antiaggregant actions, and its use as antioxidant may be safer than the rest of derivatives in order to prevent thrombotic alteration in patients that need treatment with antioxidant therapies. PMID:26081024

  3. The effect of chronic exposure to high palmitic acid concentrations on the aerobic metabolism of human endothelial EA.hy926 cells.

    Broniarek, Izabela; Koziel, Agnieszka; Jarmuszkiewicz, Wieslawa

    2016-09-01

    A chronic elevation of circulating free fatty acids (FFAs) is associated with diseases like obesity or diabetes and can lead to lipotoxicity. The goals of this study were to assess the influence of chronic exposure to high palmitic acid (PAL) levels on mitochondrial respiratory functions in endothelial cells and isolated mitochondria. Human umbilical vein endothelial cells (EA.hy926 line) were grown for 6 days in a medium containing either 100 or 150 μM PAL. Growth at high PAL concentrations induced a considerable increase in fatty acid-supplied respiration and a reduction of mitochondrial respiration during carbohydrate and glutamine oxidation. High PAL levels elevated intracellular and mitochondrial superoxide generation; increased inflammation marker, acyl-coenzyme A (CoA) dehydrogenase, uncoupling protein 2 (UCP2), and superoxide dismutase 2 expression; and decreased hexokinase I and pyruvate dehydrogenase expression. No change in aerobic respiration capacity was observed, while fermentation was decreased. In mitochondria isolated from high PAL-treated cells, an increase in the oxidation of palmitoylcarnitine, a decrease in the oxidation of pyruvate, and an increase in UCP2 activity were observed. Our results demonstrate that exposure to high PAL levels induces a shift in endothelial aerobic metabolism toward the oxidation of fatty acids. Increased levels of PAL caused impairment and uncoupling of the mitochondrial oxidative phosphorylation system. Our data indicate that FFAs significantly affect endothelial oxidative metabolism, reactive oxygen species (ROS) formation, and cell viability and, thus, might contribute to endothelial and vascular dysfunction. PMID:27417103

  4. Drug Nanoparticle Formulation Using Ascorbic Acid Derivatives

    Kunikazu Moribe; Waree Limwikrant; Kenjirou Higashi; Keiji Yamamoto

    2011-01-01

    Drug nanoparticle formulation using ascorbic acid derivatives and its therapeutic uses have recently been introduced. Hydrophilic ascorbic acid derivatives such as ascorbyl glycoside have been used not only as antioxidants but also as food and pharmaceutical excipients. In addition to drug solubilization, drug nanoparticle formation was observed using ascorbyl glycoside. Hydrophobic ascorbic acid derivatives such as ascorbyl mono- and di-n-alkyl fatty acid derivatives are used either as drugs...

  5. Palmitic Acid-Induced Neuron Cell Cycle G2/M Arrest and Endoplasmic Reticular Stress through Protein Palmitoylation in SH-SY5Y Human Neuroblastoma Cells

    Yung-Hsuan Hsiao

    2014-11-01

    Full Text Available Obesity-related neurodegenerative diseases are associated with elevated saturated fatty acids (SFAs in the brain. An increase in SFAs, especially palmitic acid (PA, triggers neuron cell apoptosis, causing cognitive function to deteriorate. In the present study, we focused on the specific mechanism by which PA triggers SH-SY5Y neuron cell apoptosis. We found that PA induces significant neuron cell cycle arrest in the G2/M phase in SH-SY5Y cells. Our data further showed that G2/M arrest is involved in elevation of endoplasmic reticular (ER stress according to an increase in p-eukaryotic translation inhibition factor 2α, an ER stress marker. Chronic exposure to PA also accelerates beta-amyloid accumulation, a pathological characteristic of Alzheimer’s disease. Interestingly, SFA-induced ER stress, G2/M arrest and cell apoptosis were reversed by treatment with 2-bromopalmitate, a protein palmitoylation inhibitor. These findings suggest that protein palmitoylation plays a crucial role in SFA-induced neuron cell cycle G2/M arrest, ER stress and apoptosis; this provides a novel strategy for preventing SFA-induced neuron cell dysfunction.

  6. Lipase-catalyzed synthesis of L-ascorbyl fatty acid esters and D-isoascorbyl fatty acid esters%脂肪酶催化合成L-抗坏血酸脂肪酸酯和D-异抗坏血酸脂肪酸酯

    郑大贵; 祝显虹; 余泗莲; 彭化南; 张小兰

    2012-01-01

    The lipase-catalyzed synthesis of L.-ascorbyl fatty acid esters and D-isoascorbyl fatty acid esters were studied by direct es-terification and transesterification,respectively. The structures of products were confirmed by IR,1H NMR,13C NMR and MS. It was found that the yield of the direct esterification were higher than that of the corresponding transesterification under the similar synthetic conditions. The raw material fatty acids and fatty acid methyl esters could be recycled and reused.%用固定化脂肪酶Lipozyme 435作催化剂,分别用直接酯化法和酯交换法合成L-抗坏血酸脂肪酸酯和D-异抗坏血酸脂肪酸酯.产物结构经IR、1HNMR、13CNMR和MS表征.结果表明,对于同一目标化合物,相似条件下,直接酯化法的效果优于酯交换法,原料脂肪酸和脂肪酸甲酯均可回收循环使用.

  7. Preparation of CLA ascorbyl ester with improved volumetric productivity by an ionic liquid-based reaction system

    Chen, B.L.; Guo, Zheng; Let, M.B.;

    2008-01-01

    A new approach to the enzymatic production Of conjugated linoleic acid (CLA) ascorbyl ester with a remarkably high volumetric productivity (120-200 g L-1) has been developed, in which strong solvation by tOMA-TFA (methyltrioctylammonium trifluoroacetate) enables a high concentration of ascorbic...

  8. Synthesis of lipase-catalyzed L-ascorbyl decanoate in ultrasonic field and determination of its antioxidant activity%超声波强化酶法合成L-抗坏血酸癸酸酯及其抗氧化性研究

    李卓; 晏日安; 曾永青

    2013-01-01

    The esterification of decanoic acid with L-ascorbic acid in the presence of tert-butanol acid as the solvent and immobilized lipase (Novozym(R) 435) as the catalyst by means of ultrasonic irradiation to obtain L-ascorbyl decanoate (L-AD) was studied. By using ultrasound the dissolution rate of the reactants could be accelerated greatly,the reaction time of esterification could be reduced from 48 to 4h. The optimal actual yield was 78.48%.The purity of target product was above 98.6% after recrystallized. The immobilized lipase could be reused 4 times in ultrasonic field. In antioxidant activities of L-ascorbyl decanoate were studied by the items of hydroxyl radical system, system of DPPH· ,and reducing power. Its antioxidant effect were further evaluated by adding into the soybean and sunflower oil. The result indicated that L-ascorbyl decanoate within the given concentration range in dose-effect relationship showed good antioxidant activities on the clearance of hydroxyl radical,superoxide anion free radical and the reducing power of DPPh·.Furthermore,antioxidant activities of L-ascorbyl decanoate were comparable with that of L-ascorbyl palmitate,and the first two indexes were higher than that of TBHQ. Thus,L-ascorbyl decanoate was demonstrated to be a potential food antioxidant.%研究了在超声波场中以固定化脂肪酶(Novozvm(R)435)为催化剂,在叔丁醇中合成L-抗坏血酸癸酸酯.超声波可以显著加速底物的溶解,并使反应时间由48h缩短到4h.产率可达到78.48%,产物纯度为98.6%,超声波处理下固定化脂肪酶可重复利用的次数为4次.抗氧化实验结果表明在一定质量浓度范围内,L-抗坏血酸癸酸酯具有很强的还原力、清除羟自由基、DPPH自由基能力能力,在等质量浓度下与L-抗坏血酸棕榈酸酯相当,且前两个指标优于TBHQ;将L-抗坏血酸癸酸酯添加到油脂中,其抗氧化能力也较优,说明L-抗坏血酸癸酸酯是一种很有潜力的抗氧化剂.

  9. Inhibition of HIV-1 infection in ex vivo cervical tissue model of human vagina by palmitic acid; implications for a microbicide development.

    Xudong Lin

    Full Text Available BACKGROUND: Approximately 80% of all new HIV-1 infections are acquired through sexual contact. Currently, there is no clinically approved microbicide, indicating a clear and urgent therapeutic need. We recently reported that palmitic acid (PA is a novel and specific inhibitor of HIV-1 fusion and entry. Mechanistically, PA inhibits HIV-1 infection by binding to a novel pocket on the CD4 receptor and blocks efficient gp120-to-CD4 attachment. Here, we wanted to assess the ability of PA to inhibit HIV-1 infection in cervical tissue ex vivo model of human vagina, and determine its effect on Lactobacillus (L species of probiotic vaginal flora. PRINCIPAL FINDINGS: Our results show that treatment with 100-200 µM PA inhibited HIV-1 infection in cervical tissue by up to 50%, and this treatment was not toxic to the tissue or to L. crispatus and jensenii species of vaginal flora. In vitro, in a cell free system that is independent of in vivo cell associated CD4 receptor; we determined inhibition constant (Ki to be ∼2.53 µM. SIGNIFICANCE: These results demonstrate utility of PA as a model molecule for further preclinical development of a safe and potent HIV-1 entry microbicide inhibitor.

  10. Effect of a bovine lung surfactant protein isolate (SP-B/C) on egg phosphatidylglycerol acyl chain order in a lipid mixture with dipalmitoylphosphatidylcholine and palmitic acid.

    Krill, S L; Gupta, S L

    1994-04-01

    Dynamic surface tension measurements of films of a d62 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine:L-alpha-phosphatidyl-DL - glycerol:d31 palmitic acid (d62-DPPC:EggPG:d31-PA) lipid matrix in the presence of a bovine pulmonary surfactant protein isolate (SP-B/C) demonstrate the improved surface activity over that of the lipids alone. Thus, significant interaction of the proteins with the lipid matrix is demonstrated. The effect of SP-B/C on the acyl chain order of the negatively charged EggPG within a d62-DPPC:EggPG:d31-PA lipid matrix in D2O saline was investigated in thermal perturbation Fourier transform IR spectroscopic studies. The EggPG thermotropic phase behavior was determined independently of the other lipid components with perdeuterated lipids and D2O. The data demonstrate the high degree of EggPG acyl chain disorder in the absence of the protein isolate. A broad transition occurs between 30 and 40 degrees C. The addition of the protein isolate did not alter the acyl chain order at 0.281 and 1.46 mg/mL of protein. However, alterations in the lipid carbonyl vibrational mode were observed. PMID:8046609

  11. Glycation of bovine serum albumin by ascorbate in vitro: Possible contribution of the ascorbyl radical?

    Sadowska-Bartosz, Izabela; Stefaniuk, Ireneusz; Galiniak, Sabina; Bartosz, Grzegorz

    2015-12-01

    Ascorbic acid (AA) has been reported to be both pro-and antiglycating agent. In vitro, mainly proglycating effects of AA have been observed. We studied the glycation of bovine serum albumin (BSA) induced by AA in vitro. BSA glycation was accompanied by oxidative modifications, in agreement with the idea of glycoxidation. Glycation was inhibited by antioxidants including polyphenols and accelerated by 2,​2'-​azobis-​2-​methyl-​propanimidamide and superoxide dismutase. Nitroxides, known to oxidize AA, did not inhibit BSA glycation. A good correlation was observed between the steady-state level of the ascorbyl radical in BSA samples incubated with AA and additives and the extent of glycation. On this basis we propose that ascorbyl radical, in addition to further products of AA oxidation, may initiate protein glycation. PMID:26202868

  12. An 11-bp insertion in Zea mays FatB reduces the palmitate content of fatty acids in maize grain

    Fatty acids in maize kernels are important for human and livestock health. We combined linkage and association analysis to fine-map the major QTL-Pal9 to a 90-kb region, in which only one candidate gene was identified. The gene was named ZmFatB and is orthologous to FatB in Arabidopsis, with a simil...

  13. Effects of Ghrelin on Triglyceride Accumulation and Glucose Uptake in Primary Cultured Rat Myoblasts under Palmitic Acid-Induced High Fat Conditions

    Lingling Han

    2015-01-01

    Full Text Available This study aimed to study the effects of acylated ghrelin on glucose and triglyceride metabolism in rat myoblasts under palmitic acid- (PA- induced high fat conditions. Rat myoblasts were treated with 0, 10−11, 10−9, or 10−7 M acylated ghrelin and 0.3 mM PA for 12 h. Triglyceride accumulation was determined by Oil-Red-O staining and the glycerol phosphate dehydrogenase-peroxidase enzymatic method, and glucose uptake was determined by isotope tracer. The glucose transporter 4 (GLUT4, AMP-activated protein kinase (AMPK, acetyl-CoA carboxylase (ACC, and uncoupling protein 3 (UCP3 were assessed by RT-PCR and western blot. Compared to 0.3 mM PA, ghrelin at 10−9 and 10−7 M reduced triglyceride content (5.855 ± 0.352 versus 5.030 ± 0.129 and 4.158 ± 0.254 mM, P<0.05 and prevented PA-induced reduction of glucose uptake (1.717 ± 0.264 versus 2.233 ± 0.333 and 2.333 ± 0.273 10−2 pmol/g/min, P<0.05. The relative protein expression of p-AMPKα/AMPKα, UCP3, and p-ACC under 0.3 mM PA was significantly reduced compared to controls (all P<0.05, but those in the 10−9 and 10−7 M ghrelin groups were significantly protected from 0.3 mM PA (all P<0.05. In conclusion, acylated ghrelin reduced PA-induced triglyceride accumulation and prevented the PA-induced decrease in glucose uptake in rat myoblasts. These effects may involve fatty acid oxidation.

  14. Palmitate impairs cytokinesis associated with RhoA inhibition

    Jianhua Zhang; Ying Yang; Jiarui Wu

    2010-01-01

    @@ Dear Editor, Excess fatty acid accumulation in non-adipose tissues results in lipotoxicity, which has been implicated in the pathogenesis of metabolic diseases such as obesity and diabetes [1]. A number of tissue culture systems have been used to study lipotoxicity by supplementation of culture media with palmitate, which is a major saturated free fatty acid in human plasma and has been reported to induce apoptosis in various cell types [2]. Here we report that palmitate causes formation of binucleate cells as a consequence of cytokinetic impairment. Our results reveal a novel toxic effect of palmitate on cell division and extend the implication of lipotoxicity to cytokinetic failure.

  15. Overexpression of steroidogenic acute regulatory protein in rat aortic endothelial cells attenuates palmitic acid-induced inflammation and reduction in nitric oxide bioavailability

    Tian Dai

    2012-11-01

    Full Text Available Abstract Background Endothelial dysfunction is a well documented evidence for the onset of atherosclerosis and other cardiovascular diseases. Lipids disorder is among the main risk factors for endothelial dysfunction in these diseases. Steroidogenic acute regulatory protein (StAR, one of the cholesterol transporters, plays an important role in the maintenance of intracellular lipid homeostasis. However, the effect of StAR on endothelial dysfunction is not well understood. Palmitic acid (PA has been shown to decrease eNOS activity and induce inflammation, both are the causes of endothelial dysfunction, in an endothelial cell culture model. Methods StAR gene was introduced into primary rat aortic endothelial cells by adenovirus infection. Real-time PCR and Western blotting were performed to determine the relative genes and proteins expression level to elucidate the underlying mechanism. The free fatty acid and cholesterol quantification kits were used to detect total cellular free fatty acid and cholesterol. The levels of inflammatory factors and nitric oxide were determined by ELISA and classic Griess reagent methods respectively. Results We successfully overexpressed StAR in primary rat aortic endothelial cells. Following StAR overexpression, mRNA levels of IL-1β, TNFα, IL6 and VCAM-1 and protein levels of IL-1β, , TNFα and IL-6 in culture supernatant were significantly decreased, which duing to blocke NFκB nuclear translocation and activation. Moreover, StAR overexpression attenuated the PA-induced reduction of nitric oxide bioavailability by protecting the bioactivity of pAkt/peNOS/NO pathway. Furthermore, the key genes involved in lipid metabolism were greatly reduced following StAR overexpression. In order to investigate the underlying mechanism, cerulenin and lovastatin, the inhibitor of fatty acid and cholesterol synthase, were added prior to PA treatment. The results showed that both cerulenin and lovastatin had a similar effect as

  16. 2-Dodecylcyclobutanone, a radiolytic product of palmitic acid, is genotoxic in primary human colon cells and in cells from preneoplastic lesions

    Knoll, Nadine [Department of Nutritional Toxicology, Institute for Nutritional Sciences, Friedrich Schiller University, Dornburger Strasse 25, D-07743 Jena (Germany); Weise, Anja [Institute of Human Genetics and Anthropology, Friedrich Schiller University, Kollegiengasse 10, D-07743 Jena (Germany); Claussen, Uwe [Institute of Human Genetics and Anthropology, Friedrich Schiller University, Kollegiengasse 10, D-07743 Jena (Germany); Sendt, Wolfgang [Department of General and Visceral Surgery, Clinic for Surgery, Friedrich Schiller University, Erlanger Allee 101, D-07743 Jena (Germany); Marian, Brigitte [Institute for Cancer Research, University of Vienna, Borschkegasse 8a, A-1090 Vienna (Austria); Glei, Michael [Department of Nutritional Toxicology, Institute for Nutritional Sciences, Friedrich Schiller University, Dornburger Strasse 25, D-07743 Jena (Germany); Pool-Zobel, Beatrice L. [Department of Nutritional Toxicology, Institute for Nutritional Sciences, Friedrich Schiller University, Dornburger Strasse 25, D-07743 Jena (Germany)]. E-mail: b8pobe@uni-jena.de

    2006-02-22

    The irradiation of fat results in the formation of 2-alkylcyclobutanones, a new class of food contaminants. Results of previous in vitro studies with primary human colon cells and in vivo experiments with rats fed with 2-alkylcyclobutanones indicated that these radiolytic derivatives may be genotoxic and enhance the progression of colon tumors. The underlying mechanisms of these effects, however, are not clearly understood. Therefore we performed additional investigations to elucidate the genotoxic potential of 2-dodecylcyclobutanone (2dDCB) that is generated from palmitic acid. In particular, we explored the relative sensitivities of human colon cells, representing different stages of tumor development and healthy colon tissues, respectively. HT29clone19A cells, LT97 adenoma cells and primary human epithelial cells were exposed to 2dDCB (150-2097 {mu}M). We determined cytotoxic effects using trypan blue exclusion. Genotoxicity, reflected as strand breaks, was assessed using the alkaline version of the comet assay and chromosomal abnormalities were investigated by 24-color fluorescence-in-situ-hybridization. 2dDCB was cytotoxic in a time- and dose-dependent manner in LT97 adenoma cells and in freshly isolated primary cells but not in the human colon tumor cell line. Associated with this was a marked induction of DNA damage by 2dDCB in LT97 adenoma cells and in freshly isolated colonocytes, whereas in the HT29clone19A cells no strand breaks were detectable. A long-term incubation of LT97 adenoma cells with lower concentrations of 2dDCB revealed cytogenetic effects. In summary, 2dDCB was clearly genotoxic in healthy human colon epithelial cells and in cells representing preneoplastic colon adenoma. These findings provide additional evidence that this compound may be regarded as a possible risk factor for processes in colon carcinogenesis related to initiation and progression.

  17. Monocyte adhesion induced by multi-walled carbon nanotubes and palmitic acid in endothelial cells and alveolar-endothelial co-cultures.

    Cao, Yi; Roursgaard, Martin; Jacobsen, Nicklas Raun; Møller, Peter; Loft, Steffen

    2016-01-01

    Free palmitic acid (PA) is a potential pro-atherogenic stimulus that may aggravate particle-mediated cardiovascular health effects. We hypothesized that the presence of PA can aggravate oxidative stress and endothelial activation induced by multi-walled carbon nanotube (MWCNT) exposure in vitro. We investigated the interaction between direct exposure to MWCNTs and PA on THP-1 monocyte adhesion to human umbilical vein endothelial cells (HUVECs), as well as on indirect exposure in an alveolar-endothelial co-culture model with A549 cells and THP-1-derived macrophages exposed in inserts and the effect measured in the lower chamber on HUVECs and THP-1 cells. The exposure to MWCNTs, including a short (NM400) and long (NM402) type of entangled fibers, was associated with elevated levels of reactive oxygen species as well as a decrease in the intracellular glutathione concentration in HUVEC and A549 monocultures. Both effects were found to be independent of the presence of PA. MWCNT exposure significantly increased THP-1 monocyte adhesion to HUVECs, and co-exposure to PA aggravated the NM400-mediated adhesion but decreased the NM402-mediated adhesion. For the co-cultures, the exposure of A549 cells did not promote THP-1 adhesion to HUVECs in the lower chamber. When THP-1 macrophages were present on the cell culture inserts, there was a modest increase in the adhesion and an increase in interleukin-6 and interleukin-8 levels in the lower chamber whereas no tumor necrosis factor was detected. Overall, this study showed that direct exposure of HUVECs to MWCNTs was associated with oxidative stress and monocyte adhesion and the presence of PA increased the adhesion when exposed to NM400. PMID:26067756

  18. 2-Dodecylcyclobutanone, a radiolytic product of palmitic acid, is genotoxic in primary human colon cells and in cells from preneoplastic lesions

    The irradiation of fat results in the formation of 2-alkylcyclobutanones, a new class of food contaminants. Results of previous in vitro studies with primary human colon cells and in vivo experiments with rats fed with 2-alkylcyclobutanones indicated that these radiolytic derivatives may be genotoxic and enhance the progression of colon tumors. The underlying mechanisms of these effects, however, are not clearly understood. Therefore we performed additional investigations to elucidate the genotoxic potential of 2-dodecylcyclobutanone (2dDCB) that is generated from palmitic acid. In particular, we explored the relative sensitivities of human colon cells, representing different stages of tumor development and healthy colon tissues, respectively. HT29clone19A cells, LT97 adenoma cells and primary human epithelial cells were exposed to 2dDCB (150-2097 μM). We determined cytotoxic effects using trypan blue exclusion. Genotoxicity, reflected as strand breaks, was assessed using the alkaline version of the comet assay and chromosomal abnormalities were investigated by 24-color fluorescence-in-situ-hybridization. 2dDCB was cytotoxic in a time- and dose-dependent manner in LT97 adenoma cells and in freshly isolated primary cells but not in the human colon tumor cell line. Associated with this was a marked induction of DNA damage by 2dDCB in LT97 adenoma cells and in freshly isolated colonocytes, whereas in the HT29clone19A cells no strand breaks were detectable. A long-term incubation of LT97 adenoma cells with lower concentrations of 2dDCB revealed cytogenetic effects. In summary, 2dDCB was clearly genotoxic in healthy human colon epithelial cells and in cells representing preneoplastic colon adenoma. These findings provide additional evidence that this compound may be regarded as a possible risk factor for processes in colon carcinogenesis related to initiation and progression

  19. Palmitate attenuates osteoblast differentiation of fetal rat calvarial cells

    Yeh, Lee-Chuan C.; Ford, Jeffery J. [Department of Biochemistry, The University of Texas Health Science Center at San Antonio, TX (United States); Lee, John C. [Department of Biochemistry, The University of Texas Health Science Center at San Antonio, TX (United States); The Sam and Ann Barshop Institute for Longevity and Aging Studies, The University of Texas Health Science Center at San Antonio, TX (United States); Adamo, Martin L., E-mail: adamo@biochem.uthscsa.edu [Department of Biochemistry, The University of Texas Health Science Center at San Antonio, TX (United States); The Sam and Ann Barshop Institute for Longevity and Aging Studies, The University of Texas Health Science Center at San Antonio, TX (United States)

    2014-07-18

    Highlights: • Palmitate inhibits osteoblast differentiation. • Fatty acid synthase. • PPARγ. • Acetyl Co-A carboxylase inhibitor TOFA. • Fetal rat calvarial cell culture. - Abstract: Aging is associated with the accumulation of ectopic lipid resulting in the inhibition of normal organ function, a phenomenon known as lipotoxicity. Within the bone marrow microenvironment, elevation in fatty acid levels may produce an increase in osteoclast activity and a decrease in osteoblast number and function, thus contributing to age-related osteoporosis. However, little is known about lipotoxic mechanisms in intramembraneous bone. Previously we reported that the long chain saturated fatty acid palmitate inhibited the expression of the osteogenic markers RUNX2 and osteocalcin in fetal rat calvarial cell (FRC) cultures. Moreover, the acetyl CoA carboxylase inhibitor TOFA blocked the inhibitory effect of palmitate on expression of these two markers. In the current study we have extended these observations to show that palmitate inhibits spontaneous mineralized bone formation in FRC cultures in association with reduced mRNA expression of RUNX2, alkaline phosphatase, osteocalcin, and bone sialoprotein and reduced alkaline phosphatase activity. The effects of palmitate on osteogenic marker expression were inhibited by TOFA. Palmitate also inhibited the mRNA expression of fatty acid synthase and PPARγ in FRC cultures, and as with osteogenic markers, this effect was inhibited by TOFA. Palmitate had no effect on FRC cell proliferation or apoptosis, but inhibited BMP-7-induced alkaline phosphatase activity. We conclude that palmitate accumulation may lead to lipotoxic effects on osteoblast differentiation and mineralization and that increases in fatty acid oxidation may help to prevent these lipotoxic effects.

  20. Palmitate attenuates osteoblast differentiation of fetal rat calvarial cells

    Highlights: • Palmitate inhibits osteoblast differentiation. • Fatty acid synthase. • PPARγ. • Acetyl Co-A carboxylase inhibitor TOFA. • Fetal rat calvarial cell culture. - Abstract: Aging is associated with the accumulation of ectopic lipid resulting in the inhibition of normal organ function, a phenomenon known as lipotoxicity. Within the bone marrow microenvironment, elevation in fatty acid levels may produce an increase in osteoclast activity and a decrease in osteoblast number and function, thus contributing to age-related osteoporosis. However, little is known about lipotoxic mechanisms in intramembraneous bone. Previously we reported that the long chain saturated fatty acid palmitate inhibited the expression of the osteogenic markers RUNX2 and osteocalcin in fetal rat calvarial cell (FRC) cultures. Moreover, the acetyl CoA carboxylase inhibitor TOFA blocked the inhibitory effect of palmitate on expression of these two markers. In the current study we have extended these observations to show that palmitate inhibits spontaneous mineralized bone formation in FRC cultures in association with reduced mRNA expression of RUNX2, alkaline phosphatase, osteocalcin, and bone sialoprotein and reduced alkaline phosphatase activity. The effects of palmitate on osteogenic marker expression were inhibited by TOFA. Palmitate also inhibited the mRNA expression of fatty acid synthase and PPARγ in FRC cultures, and as with osteogenic markers, this effect was inhibited by TOFA. Palmitate had no effect on FRC cell proliferation or apoptosis, but inhibited BMP-7-induced alkaline phosphatase activity. We conclude that palmitate accumulation may lead to lipotoxic effects on osteoblast differentiation and mineralization and that increases in fatty acid oxidation may help to prevent these lipotoxic effects

  1. Hydrophobic interactions between polymeric carrier and palmitic acid-conjugated siRNA improve PEGylated polyplex stability and enhance in vivo pharmacokinetics and tumor gene silencing.

    Sarett, Samantha M; Werfel, Thomas A; Chandra, Irene; Jackson, Meredith A; Kavanaugh, Taylor E; Hattaway, Madison E; Giorgio, Todd D; Duvall, Craig L

    2016-08-01

    Formation of stable, long-circulating siRNA polyplexes is a significant challenge in translation of intravenously-delivered, polymeric RNAi cancer therapies. Here, we report that siRNA hydrophobization through conjugation to palmitic acid (siPA) improves stability, in vivo pharmacokinetics, and tumor gene silencing of PEGylated nanopolyplexes (siPA-NPs) with balanced cationic and hydrophobic content in the core relative to the analogous polyplexes formed with unmodified siRNA, si-NPs. Hydrophobized siPA loaded into the NPs at a lower charge ratio (N(+):P(-)) relative to unmodified siRNA, and siPA-NPs had superior resistance to siRNA cargo unpackaging in comparison to si-NPs upon exposure to the competing polyanion heparin and serum. In vitro, siPA-NPs increased uptake in MDA-MB-231 breast cancer cells (100% positive cells vs. 60% positive cells) but exhibited equivalent silencing of the model gene luciferase relative to si-NPs. In vivo in a murine model, the circulation half-life of intravenously-injected siPA-NPs was double that of si-NPs, resulting in a >2-fold increase in siRNA biodistribution to orthotopic MDA-MB-231 mammary tumors. The increased circulation half-life of siPA-NPs was dependent upon the hydrophobic interactions of the siRNA and the NP core component and not just siRNA hydrophobization, as siPA did not contribute to improved circulation time relative to unmodified siRNA when delivered using polyplexes with a fully cationic core. Intravenous delivery of siPA-NPs also achieved significant silencing of the model gene luciferase in vivo (∼40% at 24 h after one treatment and ∼60% at 48 h after two treatments) in the murine MDA-MB-231 tumor model, while si-NPs only produced a significant silencing effect after two treatments. These data suggest that stabilization of PEGylated siRNA polyplexes through a combination of hydrophobic and electrostatic interactions between siRNA cargo and the polymeric carrier improves in vivo pharmacokinetics and

  2. Enzymatic Synthesis of Ascorbyl Palmitate%酶促反应合成棕榈酸Vc酯

    孙燕; 夏木西 卡玛尔; 吾满江·艾力; 贾殿增

    2006-01-01

    讨论了以黑曲霉脂肪酶为催化剂,以抗坏血酸和棕榈酸甲酯为底物的酯交换反应及其影响因素.考察了在摇床速度为200r/min,叔丁醇为溶剂下,底物的摩尔比、温度、脂肪酶浓度、时间、含水量对转化率的影响.结果表明,底物棕榈酸甲酯与Vc的摩尔比为1.3:1.0、反应温度为36℃、反应时间为24h、脂肪酶浓度为15%、含水量为1%时,Vc的转化率为23%.合成的棕榈酸Vc酯,无需和底物分离,可以直接作为油脂食品的添加剂.

  3. An investigation of the likely role of (O-acyl) ω-hydroxy fatty acids in meibomian lipid films using (O-oleyl) ω-hydroxy palmitic acid as a model.

    Schuett, Burkhardt S; Millar, Thomas J

    2013-10-01

    (O-acyl) ω-hydroxy fatty acids (OAHFAs) are a recently found group of polar lipids in meibum. Since these lipids can potentially serve as a surfactant in the tear film lipid layer, the surface properties of a molecule of this lipid class was investigated and compared with a structurally related wax ester and a fatty acid. (O-oleyl) ω-hydroxy palmitic acid was synthesized and used as the model OAHFA. It was spread either alone or mixed with human meibum on an artificial tear buffer in a Langmuir trough, and pressure-area isocycle profiles were recorded at different temperatures and compared with those of palmityl oleate and oleic acid. These measurements were accompanied by fluorescence microscopy of meibum mixed films during pressure-area isocycles. The pressure area curves indicated that pure films of the model OAHFA are as surface active as oleic acid films, cover a much larger surface area than either palmityl oleate or oleic acid and show a distinct biphasic pressure-area isocycle profile. The OAHFAs appeared to remain on the aqueous surface and show only a minor re-arrangement into multi-layered structures during repetitive pressure area isocycles. All these properties can be explained by OAHFAs binding weakly to the aqueous surface via an ester group and strongly via a carboxyl group. By contrast, the pressure area profiles of palmityl oleate films indicate that they form multi-layers and oleic acid presumably forms micelles and desorbs into the subphase. When mixed with meibum, similar features as for pure films were observed. In addition, meibum-OAHFA films appeared very homogeneous; a feature not seen with other mixtures. In conclusion these data support the notion that the tested OAHFA is a very potent surfactant which is important in spreading and stabilising meibomian lipid films. PMID:23792170

  4. Lipidomic-based investigation into the regulatory effect of Schisandrin B on palmitic acid level in non-alcoholic steatotic livers

    Kwan, Hiu Yee; Niu, Xuyan; Dai, Wenlin; Tong, Tiejun; Chao, Xiaojuan; Su, Tao; Chan, Chi Leung; Lee, Kim Chung; Fu, Xiuqiong; Yi, Hua; Yu, Hua; Li, Ting; Tse, Anfernee Kai Wing; Fong, Wang Fun; Pan, Si-Yuan

    2015-01-01

    Schisandrin B (SchB) is one of the most abundant bioactive dibenzocyclooctadiene derivatives found in the fruit of Schisandra chinensis. Here, we investigated the potential therapeutic effects of SchB on non-alcoholic fatty-liver disease (NAFLD). In lipidomic study, ingenuity pathway analysis highlighted palmitate biosynthesis metabolic pathway in the liver samples of SchB-treated high-fat-diet-fed mice. Further experiments showed that the SchB treatment reduced expression and activity of fat...

  5. Preparation of Solid Phase Microextraction (SPME) Probes through Polyaniline Multiwalled Carbon Nanotubes (PANI/MWCNTs) Coating for the Extraction of Palmitic Acid and Oleic Acid in Organic Solvents

    Khajeamiri, Alireza

    2012-01-01

    A fiber coating from polyaniline (PANI) was electrochemically prepared and employed for Solid phase micreoextraction (SPME). The PANI film was directly electrodeposited on the platinum wire surface using cyclic voltametry (CV) technique. The same method was applied for the preparation of SPME fiber coated by polyaniline multiwalled carbon nanotubes (PANI/MWCNTs) composite. The concentration of sulfuric acid for electropolymerization was 0.1 M in the presence of 0.045 M aniline in aqueous solu...

  6. Palmitic acid interferes with energy metabolism balance by adversely switching the SIRT1-CD36-fatty acid pathway to the PKC zeta-GLUT4-glucose pathway in cardiomyoblasts.

    Chen, Yeh-Peng; Tsai, Chia-Wen; Shen, Chia-Yao; Day, Cecilia-Hsuan; Yeh, Yu-Lan; Chen, Ray-Jade; Ho, Tsung-Jung; Padma, V Vijaya; Kuo, Wei-Wen; Huang, Chih-Yang

    2016-05-01

    Metabolic regulation is inextricably linked with cardiac function. Fatty acid metabolism is a significant mechanism for creating energy for the heart. However, cardiomyocytes are able to switch the fatty acids or glucose, depending on different situations, such as ischemia or anoxia. Lipotoxicity in obesity causes impairments in energy metabolism and apoptosis in cardiomyocytes. We utilized the treatment of H9c2 cardiomyoblast cells palmitic acid (PA) as a model for hyperlipidemia to investigate the signaling mechanisms involved in these processes. Our results show PA induces time- and dose-dependent lipotoxicity in H9c2 cells. Moreover, PA enhances cluster of differentiation 36 (CD36) and reduces glucose transporter type 4 (GLUT4) pathway protein levels following a short period of treatment, but cells switch from CD36 back to the GLUT4 pathway after during long-term exposure to PA. As sirtuin 1 (SIRT1) and protein kinase Cζ (PKCζ) play important roles in CD36 and GLUT4 translocation, we used the SIRT1 activator resveratrol and si-PKCζ to identify the switches in metabolism. Although PA reduced CD36 and increased GLUT4 metabolic pathway proteins, when we pretreated cells with resveratrol to activate SIRT1 or transfected si-PKCζ, both were able to significantly increase CD36 metabolic pathway proteins and reduce GLUT4 pathway proteins. High-fat diets affect energy metabolism pathways in both normal and aging rats and involve switching the energy source from the CD36 pathway to GLUT4. In conclusion, PA and high-fat diets cause lipotoxicity in vivo and in vitro and adversely switch the energy source from the CD36 pathway to the GLUT4 pathway. PMID:27133433

  7. Palmitic acid (16:0) competes with omega-6 linoleic and omega-3 ɑ-linolenic acids for FADS2 mediated Δ6-desaturation.

    Park, Hui Gyu; Kothapalli, Kumar S D; Park, Woo Jung; DeAllie, Christian; Liu, Lei; Liang, Allison; Lawrence, Peter; Brenna, J Thomas

    2016-02-01

    Sapienic acid, 16:1n-10 is the most abundant unsaturated fatty acid on human skin where its synthesis is mediated by FADS2 in the sebaceous glands. The FADS2 product introduces a double bond at the Δ6, Δ4 and Δ8 positions by acting on at least ten substrates, including 16:0, 18:2n-6, and 18:3n-3. Our aim was to characterize the competition for accessing FADS2 mediated Δ6 desaturation between 16:0 and the most abundant polyunsaturated fatty acids (PUFA) in the human diet, 18:2n-6 and 18:3n-3, to evaluate whether competition may be relevant in other tissues and thus linked to metabolic abnormalities associated with FADS2 or fatty acid levels. MCF7 cells stably transformed with FADS2 biosynthesize 16:1n-10 from exogenous 16:0 in preference to 16:1n-7, the immediate product of SCD highly expressed in cancer cell lines, and 16:1n-9 via partial β-oxidation of 18:1n-9. Increasing availability of 18:2n-6 or 18:3n-3 resulted in decreased bioconversion of 16:0 to 16:1n-10, simultaneously increasing the levels of highly unsaturated products. FADS2 cells accumulate the desaturation-elongation products 20:3n-6 and 20:4n-3 in preference to the immediate desaturation products 18:3n-6 and 18:4n-3 implying prompt/coupled elongation of the nascent desaturation products. MCF7 cells incorporate newly synthesized 16:1n-10 into phospholipids. These data suggest that excess 16:0 due to, for instance, de novo lipogenesis from high carbohydrate or alcohol consumption, inhibits synthesis of highly unsaturated fatty acids, and may in part explain why supplemental preformed EPA and DHA in some studies improves insulin resistance and other factors related to diabetes and metabolic syndrome aggravated by excess calorie consumption. PMID:26597785

  8. Investigation of the Interaction of Naringin Palmitate with Bovine Serum Albumin: Spectroscopic Analysis and Molecular Docking

    Zhang, Xia; Li, Lin; Xu, Zhenbo; Liang, Zhili; Su, Jianyu; Huang, Jianrong; Li, Bing

    2013-01-01

    Background Bovine serum albumin (BSA) contains high affinity binding sites for several endogenous and exogenous compounds and has been used to replace human serum albumin (HSA), as these two compounds share a similar structure. Naringin palmitate is a modified product of naringin that is produced by an acylation reaction with palmitic acid, which is considered to be an effective substance for enhancing naringin lipophilicity. In this study, the interaction of naringin palmitate with BSA was c...

  9. Activation of PPARδ up-regulates fatty acid oxidation and energy uncoupling genes of mitochondria and reduces palmitate-induced apoptosis in pancreatic β-cells

    Recent evidence indicates that decreased oxidative capacity, lipotoxicity, and mitochondrial aberrations contribute to the development of insulin resistance and type 2 diabetes. The goal of this study was to investigate the effects of peroxisome proliferator-activated receptor δ (PPARδ) activation on lipid oxidation, mitochondrial function, and insulin secretion in pancreatic β-cells. After HIT-T15 cells (a β-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPARδ), we found that administration of GW increased the expression of PPARδ mRNA. GW-induced activation of PPARδ up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. These results suggest that activation of PPARδ plays an important role in protecting pancreatic β-cells against aberrations caused by lipotoxicity in metabolic syndrome and diabetes.

  10. Activation of PPAR{delta} up-regulates fatty acid oxidation and energy uncoupling genes of mitochondria and reduces palmitate-induced apoptosis in pancreatic {beta}-cells

    Wan, Jun; Jiang, Li; Lue, Qingguo; Ke, Linqiu [Department of Endocrinology, West China Hospital of Sichuan University, 37 Guoxue Lane, Chengdu, Sichuan 610041 (China); Li, Xiaoyu [State Key Laboratory of Oral Diseases, Sichuan University, No. 14, 3rd Section, Renmin South Road, Chengdu, Sichuan 610041 (China); Tong, Nanwei, E-mail: buddyjun@hotmail.com [Department of Endocrinology, West China Hospital of Sichuan University, 37 Guoxue Lane, Chengdu, Sichuan 610041 (China)

    2010-01-15

    Recent evidence indicates that decreased oxidative capacity, lipotoxicity, and mitochondrial aberrations contribute to the development of insulin resistance and type 2 diabetes. The goal of this study was to investigate the effects of peroxisome proliferator-activated receptor {delta} (PPAR{delta}) activation on lipid oxidation, mitochondrial function, and insulin secretion in pancreatic {beta}-cells. After HIT-T15 cells (a {beta}-cell line) were exposed to high concentrations of palmitate and GW501516 (GW; a selective agonist of PPAR{delta}), we found that administration of GW increased the expression of PPAR{delta} mRNA. GW-induced activation of PPAR{delta} up-regulated carnitine palmitoyltransferase 1 (CPT1), long-chain acyl-CoA dehydrogenase (LCAD), pyruvate dehydrogenase kinase 4 (PDK4), and uncoupling protein 2 (UCP2); alleviated mitochondrial swelling; attenuated apoptosis; and reduced basal insulin secretion induced by increased palmitate in HIT cells. These results suggest that activation of PPAR{delta} plays an important role in protecting pancreatic {beta}-cells against aberrations caused by lipotoxicity in metabolic syndrome and diabetes.

  11. Palmitate induces ER calcium depletion and apoptosis in mouse podocytes subsequent to mitochondrial oxidative stress.

    Xu, S; Nam, S M; Kim, J-H; Das, R; Choi, S-K; Nguyen, T T; Quan, X; Choi, S J; Chung, C H; Lee, E Y; Lee, I-K; Wiederkehr, A; Wollheim, C B; Cha, S-K; Park, K-S

    2015-01-01

    Pathologic alterations in podocytes lead to failure of an essential component of the glomerular filtration barrier and proteinuria in chronic kidney diseases. Elevated levels of saturated free fatty acid (FFA) are harmful to various tissues, implemented in the progression of diabetes and its complications such as proteinuria in diabetic nephropathy. Here, we investigated the molecular mechanism of palmitate cytotoxicity in cultured mouse podocytes. Incubation with palmitate dose-dependently increased cytosolic and mitochondrial reactive oxygen species, depolarized the mitochondrial membrane potential, impaired ATP synthesis and elicited apoptotic cell death. Palmitate not only evoked mitochondrial fragmentation but also caused marked dilation of the endoplasmic reticulum (ER). Consistently, palmitate upregulated ER stress proteins, oligomerized stromal interaction molecule 1 (STIM1) in the subplasmalemmal ER membrane, abolished the cyclopiazonic acid-induced cytosolic Ca(2+) increase due to depletion of luminal ER Ca(2+). Palmitate-induced ER Ca(2+) depletion and cytotoxicity were blocked by a selective inhibitor of the fatty-acid transporter FAT/CD36. Loss of the ER Ca(2+) pool induced by palmitate was reverted by the phospholipase C (PLC) inhibitor edelfosine. Palmitate-dependent activation of PLC was further demonstrated by following cytosolic translocation of the pleckstrin homology domain of PLC in palmitate-treated podocytes. An inhibitor of diacylglycerol (DAG) kinase, which elevates cytosolic DAG, strongly promoted ER Ca(2+) depletion by low-dose palmitate. GF109203X, a PKC inhibitor, partially prevented palmitate-induced ER Ca(2+) loss. Remarkably, the mitochondrial antioxidant mitoTEMPO inhibited palmitate-induced PLC activation, ER Ca(2+) depletion and cytotoxicity. Palmitate elicited cytoskeletal changes in podocytes and increased albumin permeability, which was also blocked by mitoTEMPO. These data suggest that oxidative stress caused by saturated FFA

  12. Possible Involvement of Palmitate in Pathogenesis of Periodontitis.

    Shikama, Yosuke; Kudo, Yasusei; Ishimaru, Naozumi; Funaki, Makoto

    2015-12-01

    Type 2 diabetes (T2D) is characterized by decreased insulin sensitivity and higher concentrations of free fatty acids (FFAs) in plasma. Among FFAs, saturated fatty acids (SFAs), such as palmitate, have been suggested to promote inflammatory responses. Although many epidemiological studies have shown a link between periodontitis and T2D, little is known about the clinical significance of SFAs in periodontitis. In this study, we showed that gingival fibroblasts have cell-surface expression of CD36, which is also known as FAT/fatty acid translocase. Moreover, CD36 expression was increased in gingival fibroblasts of high-fat diet-induced T2D model mice, compared with gingival fibroblasts of mice fed a normal diet. DNA microarray analysis revealed that palmitate increased mRNA expression of pro-inflammatory cytokines and chemokines in human gingival fibroblasts (HGF). Consistent with these results, we confirmed that palmitate-induced interleukin (IL)-6, IL-8, and CXCL1 secretion in HGF, using a cytokine array and ELISA. SFAs, but not an unsaturated fatty acid, oleate, induced IL-8 production. Docosahexaenoic acid (DHA), which is one of the omega-3 polyunsaturated fatty acids, significantly suppressed palmitate-induced IL-6 and IL-8 production. Treatment of HGF with a CD36 inhibitor also inhibited palmitate-induced pro-inflammatory responses. Finally, we demonstrated that Porphyromonas gingivalis (P.g.) lipopolysaccharide and heat-killed P.g. augmented palmitate-induced chemokine secretion in HGF. These results suggest a potential link between SFAs in plasma and the pathogenesis of periodontitis. PMID:25921577

  13. Uptake of palmitate by hepatocyte suspensions: facilitation by albumin?

    Pond, S M; Davis, C K; Bogoyevitch, M A; Gordon, R A; Weisiger, R A; Bass, L

    1992-05-01

    Albumin-dependent uptake of unbound [3H]palmitic acid by hepatocytes isolated from female rat livers was studied and the experimental results compared with the predictions of a noncompartmental diffusion-reaction theory for the cellular uptake of protein-bound ligands. The outright theoretical predictions involve values for the parameters of the system, some newly measured (hepatocyte radii and the rate constant for the dissociation of palmitate-albumin complex) and some taken from the literature (diffusion coefficients and the equilibrium association constant for the palmitate-albumin complex). The measured unbound clearance of [3H]palmitic acid, defined as the initial uptake velocity divided by the unbound [3H]palmitic acid concentration in the medium, was enhanced 6.6-fold as the concentration of human serum albumin was increased from approximately 5 to 480 microM. This enhancement factor was predicted by the theory, according to which the enhancement reflects codiffusion of bound ligand across the unstirred layer adjacent to the cell membrane and, therefore, an increased delivery of unbound ligand to the cell surface. In contrast, the absolute magnitude of the unbound clearance was consistent with the theory only for the lowest published value for the equilibrium association constant, 15 microM-1. For higher published values (62 and 94 microM-1), the magnitude of the unbound clearance observed experimentally was severalfold higher than that predicted by the theory. If in fact the association constant exceeds 30 microM-1, the data would imply that an albumin-dependent facilitation mechanism exists which enhances the availability of palmitate to the cell over and above the enhancement predicted by the diffusion-reaction theory. PMID:1590397

  14. Biosysthesis of Corn Starch Palmitate by Lipase Novozym 435

    Kai Lin

    2012-06-01

    Full Text Available Esterification of starch was carried out to expand the usefulness of starch for a myriad of industrial applications. Lipase B from Candida antarctica, immobilized on macroporous acrylic resin (Novozym 435, was used for starch esterification in two reaction systems: micro-solvent system and solvent-free system. The esterification of corn starch with palmitic acid in the solvent-free system and micro-solvent system gave a degree of substitution (DS of 1.04 and 0.0072 respectively. Esterification of corn starch with palmitic acid was confirmed by UV spectroscopy and IR spectroscopy. The results of emulsifying property analysis showed that the starch palmitate with higher DS contributes to the higher emulsifying property (67.6% and emulsion stability (79.6% than the native starch (5.3% and 3.9%. Modified starch obtained by esterification that possesses emulsifying properties and has long chain fatty acids, like palmitic acid, has been widely used in the food, pharmaceutical and biomedical applications industries.

  15. Effect of dl-ethionine on the intestinal absorption and transport of palmitic acid-1-14C and tripalmitin-14C. Role of intramucosal factors in the uptake of luminal lipids

    Kessler, Jacques I.; Mishkin, S.; Stein, J.

    1969-01-01

    The effect of DL-ethionine on the uptake and transport of lipid by the rat small intestine was investigated. A cottonseed oil emulsion containing 14C-labeled tripalmitin or palmitic acid was administered intragastrically to rats pretreated with DL-ethionine, DL-ethionine plus methionine, or saline, and the rats were sacrificed 2, 4, and 6 hr later. Lipids from the plasma, the stomach, the colon, the luminal contents of the small intestine, and the wall of the small intestine were extracted, fractionated, and their radioactivity assayed. Ethionine markedly inhibited the uptake of lipids by the small intestine. This inhibition was not related to impairment of intraluminal lipolysis since analagous inhibitions were observed when palmitic acid or predigested triglyceride (TG), obtained through a jejunal fistula from normal animals, was administered instead of tripalmitin. Ethionine also inhibited the transport of lipid from the wall of the small intestine. A significant fraction of the administered lipid remained in the wall of the small intestine, and only a small fraction was transported to the blood stream. Although most of the wall radioactivity was in the form of TG, significant proportions were also found in the free fatty acid (FFA) and partial glyceride fractions, indicating a marked inhibition of mucosal reesterification to TG. The degree of inhibition of mucosal reesterification and the degree of inhibition of transport of wall lipids were directly related to the degree of inhibition of uptake of luminal radioactivity. This relationship suggests that the rate of reesterification, the level of mucosal FFA, and the rate of transport of intramucosal TG may be of importance in determining the extent of uptake of intraluminal lipid by the mucosal cells. Since a significant fraction of the wall radioactivity was in the form of TG, the decreased transport of wall lipids was attributed to an impairment of chylomicron completion due to inhibition of either the

  16. Sequence-specific {sup 1}H, {sup 13}C, and {sup 15}N resonance assignments for intestinal fatty-acid-binding protein complexed with palmitate (15.4 kDA)

    Hodsdon, M.E.; Toner, J.J.; Cistola, D.P. [Washington Univ. School of Medicine, St. Louis, MO (United States)

    1994-12-01

    Intestinal fatty-acid-binding protein (I-FABP) belongs to a family of soluble, cytoplasmic proteins that are thought to function in the intracellular transport and trafficking of polar lipids. Individual members of this protein family have distinct specificities and affinities for fatty acids, cholesterol, bile salts, and retinoids. We are comparing several retinol- and fatty-acid-binding proteins from intestine in order to define the factors that control molecular recognition in this family of proteins. We have established sequential resonance assignments for uniformly {sup 13}C/{sup 15}N-enriched I-FABP complexed with perdeuterated palmitate at pH7.2 and 37{degrees}C. The assignment strategy was similar to that introduced for calmodulin. We employed seven three-dimensional NMR experiments to establish scalar couplings between backbone and sidechain atoms. Backbone atoms were correlated using triple-resonance HNCO, HNCA, TOCSY-HMQC, HCACO, and HCA(CO)N experiments. Sidechain atoms were correlated using CC-TOCSY, HCCH-TOCSY, and TOCSY-HMQC. The correlations of peaks between three-dimensional spectra were established in a computer-assisted manner using NMR COMPASS (Molecular Simulations, Inc.) Using this approach, {sup 1}H, {sup 13}C, and {sup 15}N resonance assignments have been established for 120 of the 131 residues of I-FABP. For 18 residues, amide {sup 1}H and {sup 15}N resonances were unobservable, apparently because of the rapid exchange of amide protons with bulk water at pH 7.2. The missing amide protons correspond to distinct amino acid patterns in the protein sequence, which will be discussed. During the assignment process, several sources of ambiguity in spin correlations were observed. To overcome this ambiguity, the additional inter-residue correlations often observed in the HNCA experiment were used as cross-checks for the sequential backbone assignments.

  17. Improved production of postlarval white shrimp through supplementation of L-ascorbyl-2-polyphosphate in their diet

    Kontara, E.K.M.; Merchie, G.; Lavens, P.; Robles, R; Nelis, H.; De leenheer, A P; Sorgeloos, P.

    1997-01-01

    L-ascorbyl-2-polyphosphate (ApP) was used as a vitamin C source to study the ascorbic acid (AA) requirements for the early postlarval stages of white shrimp (Penaeus vannamei). First the stability of ApP in the diets was determined: ApP losses after pelletizing and 10 min immersion in seawater were 25-35% and 30%, respectively. Semipurified diets with five levels of ApP (0, 20, 40, 100 and 200 mg kg-1 expressed as active AA were fed ad libitum to P. vannamei (PL-14 stage, mean dry weight 0.73...

  18. Surfactantlipid biosynthesis: Regulation of transmembrane transport of palmitate

    Guthmann, Florian

    2010-01-01

    Considering the mechanisms by which antenatal maturation of lung can be induced, the role of long chain fatty acids as precursors of surfactant lipid synthesis has not been thoroughly investigated. To specifically increase surfactant synthesis during the fetal and/or neonatal period we studied the regulation of de novo phosphatidyl synthesis in type II pneumocytes. First, we characterised the transmembrane transport of palmitate, a long chain fatty acid prevalent in surfactant lipids, with...

  19. Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin.

    Suh, Dong-Churl; Kim, Yeongseok; Kim, Hyeongmin; Ro, Jieun; Cho, Seong-Wan; Yun, Gyiae; Choi, Sung-Up; Lee, Jaehwi

    2014-01-01

    The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin demonstrated significantly increased RP distributions in the epidermis. Furthermore, it was found that skin distribution of RP could be further improved by combined use of pectin and ascorbyl palmitate (AP), due largely to their anti-oxidative effect. These results clearly demonstrate that the skin deposition properties of RP can be improved by stabilizing RP with pectin. Therefore, it is strongly suggested that pectin could be used in the pharmaceutical and cosmetic formulations as an efficient stabilizing agent and as skin penetration modulator. PMID:24596625

  20. Ascorbyl coumarates as multifunctional cosmeceutical agents that inhibit melanogenesis and enhance collagen synthesis.

    Kwak, Jun Yup; Park, Soojin; Seok, Jin Kyung; Liu, Kwang-Hyeon; Boo, Yong Chool

    2015-09-01

    L-Ascorbic acid (AA) and p-coumaric acid (p-CA) are naturally occurring antioxidants that are known to enhance collagen synthesis and inhibit melanin synthesis, respectively. The purpose of this study was to examine hybrid compounds between AA and p-CA as multifunctional cosmeceutical agents. Ascorbyl 3-p-coumarate (A-3-p-C), ascorbyl 2-p-coumarate (A-2-p-C), and their parent compounds were tested for their effects on cellular melanin synthesis and collagen synthesis. At 100 μM, A-3-p-C and A-2-p-C decreased melanin content of human dermal melanocytes stimulated by L-tyrosine, by 65 and 59%, respectively, compared to 11% inhibition of AA and 70% inhibition of p-CA. A-3-p-C and A-2-p-C were less effective than p-CA but more effective than AA at inhibiting tyrosinase activity. A-3-p-C and A-2-p-C were more effective than p-CA at inhibiting the autoxidation of L-3,4-dihydroxyphenylalanine. At 100-300 μM, A-3-p-C and A-2-p-C augmented collagen release from human dermal fibroblasts by 120-144% and 125-191%, respectively, compared to 126-133% increase of AA and 120-146% increase of p-CA. They increased procollagen type I C-peptide release (A-3-p-C, and A-2-p-C) like AA, and decreased matrix metalloproteinase 1 level (A-2-p-C) like p-CA, implicating that they might regulate collagen metabolism by multiple mechanisms. This study suggests that A-3-p-C and A-2-p-C could be used as multifunctional cosmeceutical agents for the attenuation of certain aspects of skin aging. PMID:26078014

  1. Study on the antioxidation activity of D-isoascorbyl camellia oil fatty acid esters%异VC山茶油脂肪酸酯的抗氧化性能研究

    余泗莲; 余彬; 祝显虹; 毛刘量; 郑大贵

    2012-01-01

    新鲜猪油中添加异VC山茶油脂肪酸酯和对照的抗氧化剂,按照GB/T5009.37-2003的方法,进行强氧化试验,测定过氧化值(POV);二苯代苦味肼基自由基(DPPH.)无水乙醇溶液中添加异VC山茶油脂肪酸酯和对照的抗氧化剂,用分光光度法测定DPPH.清除率(SA).POV数据表明,参照中国规定的最高允许浓度往猪油中分别添加抗氧化剂,异VC山茶油脂肪酸酯抗氧化能力与异VC棕榈酸酯和TBHQ相当,但比维生素C棕榈酸酯强.SA数据表明,在受试物浓度高于1.666710-4mol·L-1,并且浓度相同时,异VC山茶油脂肪酸酯表现出比异VC棕榈酸酯、VC棕榈酸酯和TBHQ更强的清除能力.%D - isoascorbyl camellia oil fatty acid esters was added in lard and peroxide value ( POV) in lard sample was tested according to GB/T5009. 37-2003. The scavenging activity (SA) of D - isoascorbyl camellia oil fatty acid esters on DPPH free - radical was tested by spectrophotometry. The POV data showed that the antioxidation activity of D - isoascorbyl camellia oil fatty acid esters was better than that of L - ascorbyl palmitate, and was almost the same as that of D - isoascorbyl palmitate and TBHQ at the highest permitted amount by China food additives regulation. The SA data showed that when the concentration of samples was higher than 1. 666710 -4mol · L-1, the activity of scavenging DPPH of D - isoascorbyl camellia oil fatty acid esters was higher than that of D - isoascorbyl palmitate, L - ascorbyl palmitate and TBHQ.

  2. Short Term Palmitate Supply Impairs Intestinal Insulin Signaling via Ceramide Production.

    Tran, Thi Thu Trang; Postal, Bárbara Graziela; Demignot, Sylvie; Ribeiro, Agnès; Osinski, Céline; Pais de Barros, Jean-Paul; Blachnio-Zabielska, Agnieszka; Leturque, Armelle; Rousset, Monique; Ferré, Pascal; Hajduch, Eric; Carrière, Véronique

    2016-07-29

    The worldwide prevalence of metabolic diseases is increasing, and there are global recommendations to limit consumption of certain nutrients, especially saturated lipids. Insulin resistance, a common trait occurring in obesity and type 2 diabetes, is associated with intestinal lipoprotein overproduction. However, the mechanisms by which the intestine develops insulin resistance in response to lipid overload remain unknown. Here, we show that insulin inhibits triglyceride secretion and intestinal microsomal triglyceride transfer protein expression in vivo in healthy mice force-fed monounsaturated fatty acid-rich olive oil but not in mice force-fed saturated fatty acid-rich palm oil. Moreover, when mouse intestine and human Caco-2/TC7 enterocytes were treated with the saturated fatty acid, palmitic acid, the insulin-signaling pathway was impaired. We show that palmitic acid or palm oil increases ceramide production in intestinal cells and that treatment with a ceramide analogue partially reproduces the effects of palmitic acid on insulin signaling. In Caco-2/TC7 enterocytes, ceramide effects on insulin-dependent AKT phosphorylation are mediated by protein kinase C but not by protein phosphatase 2A. Finally, inhibiting de novo ceramide synthesis improves the response of palmitic acid-treated Caco-2/TC7 enterocytes to insulin. These results demonstrate that a palmitic acid-ceramide pathway accounts for impaired intestinal insulin sensitivity, which occurs within several hours following initial lipid exposure. PMID:27255710

  3. Palmitate induces ER calcium depletion and apoptosis in mouse podocytes subsequent to mitochondrial oxidative stress

    Xu, S; Nam, S M; Kim, J-H; Das, R.; Choi, S-K; T.T. Nguyen; Quan, X.; Choi, S. J.; Chung, C H; Lee, E Y; Lee, I-K; Wiederkehr, A; Wollheim, C. B.; Cha, S-K; Park, K-S.

    2015-01-01

    Pathologic alterations in podocytes lead to failure of an essential component of the glomerular filtration barrier and proteinuria in chronic kidney diseases. Elevated levels of saturated free fatty acid (FFA) are harmful to various tissues, implemented in the progression of diabetes and its complications such as proteinuria in diabetic nephropathy. Here, we investigated the molecular mechanism of palmitate cytotoxicity in cultured mouse podocytes. Incubation with palmitate dose-dependently i...

  4. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models. -- Highlights: ► Efficacy of MP and EP in combating inflammation was displayed in several models. ► MP and EP reduced carrageenan-induced rat paw edema and prostaglandin E2 level. ► MP and EP decreased TNF-α and IL-6 levels in experimental endotoxemia. ► MP and EP reduced NF-κB expression and histological changes in rat liver and lung. ► MP and EP reduced croton oil-induced ear edema and neutrophil infiltration.

  5. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models

    Saeed, Noha M. [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Egyptian Russian University, Cairo (Egypt); El-Demerdash, Ebtehal [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo (Egypt); Abdel-Rahman, Hanaa M. [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Egyptian Russian University, Cairo (Egypt); Algandaby, Mardi M. [Department of Biology (Botany), Faculty of Science, King Abdulaziz University, Jeddah (Saudi Arabia); Al-Abbasi, Fahad A. [Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah (Saudi Arabia); Abdel-Naim, Ashraf B., E-mail: abnaim@pharma.asu.edu.eg [Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo (Egypt)

    2012-10-01

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models. -- Highlights: ► Efficacy of MP and EP in combating inflammation was displayed in several models. ► MP and EP reduced carrageenan-induced rat paw edema and prostaglandin E2 level. ► MP and EP decreased TNF-α and IL-6 levels in experimental endotoxemia. ► MP and EP reduced NF-κB expression and histological changes in rat liver and lung. ► MP and EP reduced croton oil-induced ear edema and neutrophil infiltration.

  6. Anti-inflammatory activity of methyl palmitate and ethyl palmitate in different experimental rat models.

    Saeed, Noha M; El-Demerdash, Ebtehal; Abdel-Rahman, Hanaa M; Algandaby, Mardi M; Al-Abbasi, Fahad A; Abdel-Naim, Ashraf B

    2012-10-01

    Methyl palmitate (MP) and ethyl palmitate (EP) are naturally occurring fatty acid esters reported as inflammatory cell inhibitors. In the current study, the potential anti-inflammatory activity of MP and EP was evaluated in different experimental rat models. Results showed that MP and EP caused reduction of carrageenan-induced rat paw edema in addition to diminishing prostaglandin E2 (PGE2) level in the inflammatory exudates. In lipopolysaccharide (LPS)-induced endotoxemia in rats, MP and EP reduced plasma levels of tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). MP and EP decreased NF-κB expression in liver and lung tissues and ameliorated histopathological changes caused by LPS. Topical application of MP and EP reduced ear edema induced by croton oil in rats. In the same animal model, MP and EP reduced neutrophil infiltration, as indicated by decreased myeloperoxidase (MPO) activity. In conclusion, this study demonstrates the effectiveness of MP and EP in combating inflammation in several experimental models. PMID:22842335

  7. Síntese, caracterização e análise térmica dos sais de lítio, sódio e potássio do ácido palmítico e do seu éster etílico Synthesis, characterization and thermal analysis of lithium, sodium and potassium salts of the palmitic acid and its ethyl ester

    André Luis Castro de Sales

    2008-01-01

    Full Text Available Alkaline salts of the palmitic acid were synthesized and characterized from aqueous and ethanolic medium. The salts were characterized by elemental analysis (EA and infrared spectroscopy (IR. EA and IR, being its synthesis comproved, also characterized the ethyl palmitate. All the salts and the ester were submitted to thermal analysis using thermogravimetry (TG, and differential thermal analysis (DTA in the temperature ranging from room to 700 ºC under air dynamic atmosphere. Differential scanning calorimetry (DSC measurements were taken from -90 ºC up to temperatures close to the starting of the decomposition temperature, determined by thermogravimetry, using heating and cooling cycles.

  8. 生物法合成维生素C棕榈酸酯%Biological Synthesis of L-ascorbyl Palmitate

    徐凤杰; 谭天伟

    2005-01-01

    研究了不同的脂肪酶在有机溶剂体系中催化合成L-维生素C棕榈酸酯的反应.针对维生素C在有机溶剂中溶解度较低这一问题,对催化合成维生素C棕榈酸酯反应的脂肪酶和反应介质进行比较,同时对影响合成维生素C棕榈酸酯反应的因素(温度、底物浓度、底物摩尔比、反应时间和酶量等)进行探讨,优化了反应条件:在10mL的丙酮中,1.094g棕榈酸与0.107g维生素C在酶量为20%(W/W,固定化酶/维生素C)的固定化脂肪酶催化下,初始含0.4nm分子筛20%,温度为60℃,转速为200r/min,反应48h转化率可以达到80%,产物维生素C棕榈酸酯的浓度可达20g/L.

  9. Electron Spin Resonance of Ascorbyl (Vitamin C) Radicals in Synthetic CaCO3 by UV Irradiation

    Sato, Hideo; Tani, Atsushi; Ikeya, Motoji

    2003-02-01

    Free radicals ascribed to ascorbic acid (AscH2), vitamin C, in the solid matrix of synthetic calcium carbonate have been studied using electron spin resonance (ESR) after UV irradiation. A new ESR signal with g-factors of g\\|=2.0024 and g\\bot=2.0053 was found together with a broad singlet signal around g=2.005 and a doublet signal at g=2.0053 separated by 0.18 mT due to the ascorbyl radical (Asc•-). The molecular orbitals of Asc•- and two other types of ascorbyl radical (AscH•-) were calculated using the semi-empirical PM3 unrestricted Hartree-Fock (UHF) method, which indicated that the hyperfine splitting due to hydrogen bonded to one of the carbons in the pentagonal ring was dominant. The axial signal was ascribed to AscH•-, while the doublet signal was ascribed to Asc•- in CaCO3. Possible pharmaceutical and nutritional applications of embedding unstable active molecules into the crystalline lattice of CaCO3 and a new nondestructive method for determination of vitamin C contents are discussed because the vitamin C has higher thermal stability in the carbonate than that in aqueous solution.

  10. Investigation of the interaction of naringin palmitate with bovine serum albumin: spectroscopic analysis and molecular docking.

    Xia Zhang

    Full Text Available BACKGROUND: Bovine serum albumin (BSA contains high affinity binding sites for several endogenous and exogenous compounds and has been used to replace human serum albumin (HSA, as these two compounds share a similar structure. Naringin palmitate is a modified product of naringin that is produced by an acylation reaction with palmitic acid, which is considered to be an effective substance for enhancing naringin lipophilicity. In this study, the interaction of naringin palmitate with BSA was characterised by spectroscopic and molecular docking techniques. METHODOLOGY/PRINCIPAL FINDINGS: The goal of this study was to investigate the interactions between naringin palmitate and BSA under physiological conditions, and differences in naringin and naringin palmitate affinities for BSA were further compared and analysed. The formation of naringin palmitate-BSA was revealed by fluorescence quenching, and the Stern-Volmer quenching constant (KSV was found to decrease with increasing temperature, suggesting that a static quenching mechanism was involved. The changes in enthalpy (ΔH and entropy (ΔS for the interaction were detected at -4.11 ± 0.18 kJ·mol(-1 and -76.59 ± 0.32 J·mol(-1·K(-1, respectively, which indicated that the naringin palmitate-BSA interaction occurred mainly through van der Waals forces and hydrogen bond formation. The negative free energy change (ΔG values of naringin palmitate at different temperatures suggested a spontaneous interaction. Circular dichroism studies revealed that the α-helical content of BSA decreased after interacting with naringin palmitate. Displacement studies suggested that naringin palmitate was partially bound to site I (subdomain IIA of the BSA, which was also substantiated by the molecular docking studies. CONCLUSIONS/SIGNIFICANCE: In conclusion, naringin palmitate was transported by BSA and was easily removed afterwards. As a consequence, an extension of naringin applications for use in food, cosmetic

  11. Isosteviol has beneficial effects on palmitate-induced α-cell dysfunction and gene expression.

    Xiaoping Chen

    Full Text Available BACKGROUND: Long-term exposure to high levels of fatty acids impairs insulin secretion and exaggerates glucagon secretion. The aim of this study was to explore if the antihyperglycemic agent, Isosteviol (ISV, is able to counteract palmitate-induced α-cell dysfunction and to influence α-cell gene expression. METHODOLOGY/PRINCIPAL FINDINGS: Long-term incubation studies with clonal α-TC1-6 cells were performed in the presence of 0.5 mM palmitate with or without ISV. We investigated effects on glucagon secretion, glucagon content, cellular triglyceride (TG content, cell proliferation, and expression of genes involved in controlling glucagon synthesis, fatty acid metabolism, and insulin signal transduction. Furthermore, we studied effects of ISV on palmitate-induced glucagon secretion from isolated mouse islets. Culturing α-cells for 72-h with 0.5 mM palmitate in the presence of 18 mM glucose resulted in a 56% (p<0.01 increase in glucagon secretion. Concomitantly, the TG content of α-cells increased by 78% (p<0.01 and cell proliferation decreased by 19% (p<0.05. At 18 mM glucose, ISV (10(-8 and 10(-6 M reduced palmitate-stimulated glucagon release by 27% (p<0.05 and 27% (p<0.05, respectively. ISV (10(-6 M also counteracted the palmitate-induced hypersecretion of glucagon in mouse islets. ISV (10(-6 M reduced α-TC1-6 cell proliferation rate by 25% (p<0.05, but ISV (10(-8 and 10(-6 M had no effect on TG content in the presence of palmitate. Palmitate (0.5 mM increased Pcsk2 (p<0.001, Irs2 (p<0.001, Fasn (p<0.001, Srebf2 (p<0.001, Acaca (p<0.01, Pax6 (p<0.05 and Gcg mRNA expression (p<0.05. ISV significantly (p<0.05 up-regulated Insr, Irs1, Irs2, Pik3r1 and Akt1 gene expression in the presence of palmitate. CONCLUSIONS/SIGNIFICANCE: ISV counteracts α-cell hypersecretion and apparently contributes to changes in expression of key genes resulting from long-term exposure to palmitate. ISV apparently acts as a glucagonostatic drug with potential as a

  12. Signaling dynamics of palmitate-induced ER stress responses mediated by ATF4 in HepG2 cells

    Cho Hyunju

    2013-01-01

    Full Text Available Abstract Background Palmitic acid, the most common saturated free fatty acid, has been implicated in ER (endoplasmic reticulum stress-mediated apoptosis. This lipoapotosis is dependent, in part, on the upregulation of the activating transcription factor-4 (ATF4. To better understand the mechanisms by which palmitate upregulates the expression level of ATF4, we integrated literature information on palmitate-induced ER stress signaling into a discrete dynamic model. The model provides an in silico framework that enables simulations and predictions. The model predictions were confirmed through further experiments in human hepatocellular carcinoma (HepG2 cells and the results were used to update the model and our current understanding of the signaling induced by palmitate. Results The three key things from the in silico simulation and experimental results are: 1 palmitate induces different signaling pathways (PKR (double-stranded RNA-activated protein kinase, PERK (PKR-like ER kinase, PKA (cyclic AMP (cAMP-dependent protein kinase A in a time dependent-manner, 2 both ATF4 and CREB1 (cAMP-responsive element-binding protein 1 interact with the Atf4 promoter to contribute to a prolonged accumulation of ATF4, and 3 CREB1 is involved in ER-stress induced apoptosis upon palmitate treatment, by regulating ATF4 expression and possibly Ca2+ dependent-CaM (calmodulin signaling pathway. Conclusion The in silico model helped to delineate the essential signaling pathways in palmitate-mediated apoptosis.

  13. Biosysthesis of Corn Starch Palmitate by Lipase Novozym 435

    Kai Lin; Le Chang; Chun-Gu Xia; Yan Wang; Tie Liu; Jia-Ying Xin

    2012-01-01

    Esterification of starch was carried out to expand the usefulness of starch for a myriad of industrial applications. Lipase B from Candida antarctica, immobilized on macroporous acrylic resin (Novozym 435), was used for starch esterification in two reaction systems: micro-solvent system and solvent-free system. The esterification of corn starch with palmitic acid in the solvent-free system and micro-solvent system gave a degree of substitution (DS) of 1.04 and 0.0072 resp...

  14. Reaction kinetics of isopropyl palmitate synthesis

    Lili Fu; Yinge Bai; Gaozhi L; Denggao Jiang

    2015-01-01

    In this study, the kinetics of isopropyl palmitate synthesis including the reaction mechanism was studied based on the two-step noncatalytic method. The liquid-phase diffusion effect on the reaction process was eliminated by adjusting the stirring rate. The results showed that the two-step reaction followed a tetrahedral mechanism and conformed to second-order reaction kinetics. Nucleophilic attack on the carbonyl carbon afforded an intermedi-ate, containing a tetrahedral carbon center. The intermediate ultimately decomposed by elimination of the leav-ing group, affording isopropyl palmitate. The experimental data were analyzed at different temperatures by the integral method. The kinetic equations of the each step were deduced, and the activation energy and frequency factor were obtained. Experiments were performed to verify the feasibility of kinetic equations, and the result showed that the kinetic equations were reliable. This study could be very significant to both industrial application and determining the continuous production of isopropyl palmitate.

  15. 维生素C衍生物的制备及其在化妆品中的应用%Preparation of L-ascorbic acid derivatives and their application in cosmetics

    谷雪贤

    2011-01-01

    维生素C衍牛物克服了维生素C易被氧化不稳定的缺点,被广泛用于化妆品中.阐述了维生素C衍生物围内外的研究情况,主要对维生素C的磷酸酯盐、糖苷、棕榈酸酯、乙基醚、甲基硅基等衍生物的制备方法进行了总结.介绍了其在化妆品中的应用情况,指出了维生素C衍生物的发展趋势.%The L-ascorbic acid derivatives overcomes the shortcoming of L-ascorbic acid which is easy to be oxidized,and has been broadly applied in cosmetics.The recent development situation of L-ascorbic acid derivatives is reviewed,and the preparation methods and the application on cosmetics of the L-ascorbic acid derivatives such as L-ascorbic acid-2-phosphate, ascorbic acid glucoside, ascorbyl palmitate were summarized.The trendency of the L-ascorbic acid derivatives is proposed also.

  16. Effects of antioxidants on the lipase-catalyzed acidolysis during production of structured lipids

    Xu, Xuebing; Timm Heinrich, Maike; Nielsen, Nina Skall;

    2005-01-01

    In the production process of structured lipids, the influence of the addition of antioxidants before enzymatic acidolysis was investigated. Eight different antioxidants were screened: butylated hydroxyanisole, butylated hydroxytoluene, propyl gallate, ascorbyl palmitate, citric acid, EDTA, a...

  17. Efficacy and safety of disodium ascorbyl phytostanol phosphates in men with moderate dyslipidemia

    Vissers, Maud N; Trip, Mieke D; Pritchard, P. Haydn; Tam, Patrick; Lukic, Tatjana; de Sain-van der Velden, Monique G.; de Barse, Martina; Kastelein, John J. P.

    2008-01-01

    Objective This study investigated the efficacy, safety, tolerability, and pharmacokinetics of a novel cholesterol absorption inhibitor, FM-VP4, comprising disodium ascorbyl sitostanol phosphate (DASP) and disodium ascorbyl campestanol phosphate (DACP). Methods In phase 1, 30 men received a single dose of 100, 200, 400, 800, 1,600, or 2,000 mg FM-VP4 or placebo. In phase 2, 100 men were treated with 100, 200, 400, or 800 mg/day of FM-VP4 or placebo for 4 weeks. Results The drug was well tolera...

  18. Surprisingly Long-Lived Ascorbyl Radicals in Acetonitrile: Concerted Proton-Electron Transfer Reactions and Thermochemistry

    Warren, Jeffrey J.; Mayer, James M.

    2008-01-01

    Proton-coupled electron transfer (PCET) reactions and thermochemistry of 5,6-isopropylidene ascorbate (iAscH−) have been examined in acetonitrile solvent.iAscH− is oxidized by 2,4,6-tBu3C6H2O• and by excess TEMPO• to give the corresponding 5,6-isopropylidene ascorbyl radical anion (iAsc•−), which persists for hours at 298 K in dry MeCN solution. The stability of iAsc•− is surprising in light of the transience of the ascorbyl radical in aqueous solutions, and is due to the lack of the protons ...

  19. 棕榈酸在三酰甘油中的位置分布对大鼠营养吸收的影响%Effect of positional distribution of palmitic acid in triglycerides on the absorption of the nutrition in rats

    宋秋; 刘亚东; 李晓敏; 杨丽杰

    2012-01-01

    The impacts of the position of palmitic acid in triglyceride on the absorption of fatty acids and mineral were studied. Feeding experiment was performed by using four groups of young male Wistar rats. Fat raw materials with different proportions of sn-2 position palmitic acid were added into fat-free diets which were the OPO ( 1,3- dioleoyl- 2- palmitoyl triglyceride ) structural fat, the vegetable oil mixture with imitating the composition of OPO,the infant formula containing OPO and the common infant formula. The proportions of the experimental fat in each groups were all 10% ,as for the sn-2 position palmitic acid in four groups were respectively 45.40% ,13.29% ,48.04% ,and 28.66%. After 2 weeks feeding,the contents of lipid,calcium and magnesium in the fecal were analyzed. The results showed that the fat absorption after intake of OPO and the infant formula containing OPO were higher than the other two groups significantly with much less calcium excreting. In conclusion,high content of sn-2 position palmitic acid could promote the absorption of fat in rats, reduce the formation of fatty acid soap and improve the calcium absorption.%研究了棕榈酸在三酰甘油中的不同位置分布对脂肪酸及矿质元素吸收的影响。以幼龄雄性Wistar大鼠为动物模型,将含不同比例sn-2位棕榈酸的脂肪原料添加到无脂饲料中,分别为:OPO(1,3-二油酸-2-棕榈酸甘油酯)结构脂肪,组成模拟OPO的混合植物油,含OPO的婴儿配方奶粉以及常规婴儿配方奶粉。饲料实验脂肪含量均为10%,各组sn-2位棕榈酸相对含量分别为45.40%、13.29%、48.04%、28.66%。喂养两周后,分析大鼠粪便中的脂质及钙、镁元素。结果显示,OPO组和OPO婴儿配方奶粉组的大鼠对脂肪的吸收显著高于另外两组,并且钙排泄较少。由此可得出结论:高含量的sn-2位棕榈酸可以促进大鼠对脂肪的吸收,减少脂肪酸皂的形成,并能改善对钙的吸收。

  20. The flux control coefficient of carnitine palmitoyltransferase I on palmitate beta-oxidation in rat hepatocyte cultures.

    Spurway, T D; Sherratt, H A; Pogson, C I; Agius, L

    1997-01-01

    Two important factors that determine the flux of hepatic beta-oxidation of long-chain fatty acids are the availability of fatty acid and the activity of carnitine palmitoyltransferase I (CPT I). Using Metabolic Control Analysis, the flux control coefficient of CPT I in rat hepatocyte monolayers was determined by titration with 2-[6-(4-chlorophenoxy)hexyl]oxirane-2-carboxylate (Etomoxir), which is converted to Etomoxir-CoA, an irreversible inhibitor of CPT I. We measured CPT I activity and flux through beta-oxidation at 0.2 mM and 1.0 mM palmitate to simulate substrate concentrations in fed and fasted states. Rates of beta-oxidation were 4.5-fold higher at 1. 0 mM palmitate compared with 0.2 mM palmitate. Flux control coefficients of CPT I, estimated by two independent methods, were similar: 0.67 and 0.79 for 0.2 mM palmitate, and 0.68 and 0.77 for 1 mM palmitate. It is concluded that the regulatory potential of CPT I is similar at low and high physiological concentrations of palmitate. PMID:9173869

  1. High beta-palmitate fat controls the intestinal inflammatory response and limits intestinal damage in mucin Muc2 deficient mice.

    Peng Lu

    Full Text Available BACKGROUND: Palmitic-acid esterified to the sn-1,3 positions of the glycerol backbone (alpha, alpha'-palmitate, the predominant palmitate conformation in regular infant formula fat, is poorly absorbed and might cause abdominal discomfort. In contrast, palmitic-acid esterified to the sn-2 position (beta-palmitate, the main palmitate conformation in human milk fat, is well absorbed. The aim of the present study was to examine the influence of high alpha, alpha'-palmitate fat (HAPF diet and high beta-palmitate fat (HBPF diet on colitis development in Muc2 deficient (Muc2(-/- mice, a well-described animal model for spontaneous enterocolitis due to the lack of a protective mucus layer. METHODS: Muc2(-/- mice received AIN-93G reference diet, HAPF diet or HBPF diet for 5 weeks after weaning. Clinical symptoms, intestinal morphology and inflammation in the distal colon were analyzed. RESULTS: Both HBPF diet and AIN-93G diet limited the extent of intestinal erosions and morphological damage in Muc2(-/- mice compared with HAPF diet. In addition, the immunosuppressive regulatory T (Treg cell response as demonstrated by the up-regulation of Foxp3, Tgfb1 and Ebi3 gene expression levels was enhanced by HBPF diet compared with AIN-93G and HAPF diets. HBPF diet also increased the gene expression of Pparg and enzymatic antioxidants (Sod1, Sod3 and Gpx1, genes all reported to be involved in promoting an immunosuppressive Treg cell response and to protect against colitis. CONCLUSIONS: This study shows for the first time that HBPF diet limits the intestinal mucosal damage and controls the inflammatory response in Muc2(-/- mice by inducing an immunosuppressive Treg cell response.

  2. Increased incorporation of 14C-palmitate into tissue lipids by isolated heart myocytes in endotoxic shock

    The incorporation of 14C-palmitate into various classes of tissue lipids by isolated adult dog heart myocytes was studied in an attempt to understand the pathophysiology of myocardial dysfunction during endotoxic shock. The results showed that the incorporation of 14C-palmitate into phospholipids was increased by 85.3% and 108.8% at 0.5 hours and two hours, respectively, following endotoxin (0.5 mg Escherichia coli lipopolysaccharide B per kg body weight) administration. Incorporation of radioactive palmitate into triglycerides was increased by 50.9% and 107.2% at 0.5 and two hours, respectively, postendotoxin. Incorporation of 14C-palmitate into diglycerides was stimulated by 51.9% and 64.5% at 0.5 and two hours, respectively, after endotoxin injection. The incorporation of 14C-palmitate into tissue-free fatty acids and unaltered at 0.5 hours but it was increased by 211.7% at two hours postendotoxin. These data demonstrated that myocardial membrane lipid profile was greatly altered by increased incorporation of 14C-palmitate into phospholipids and neutral lipids after endotoxin administration. An alteration in myocardial lipid profile, as reported in this study, may contribute to the development of myocardial dysfunction during shock

  3. A single prior bout of exercise protects against palmitate-induced insulin resistance despite an increase in total ceramide content.

    Thrush, A Brianne; Harasim, Ewa; Chabowski, Adrian; Gulli, Roberto; Stefanyk, Leslie; Dyck, David J

    2011-05-01

    Ceramide accumulation has been implicated in the impairment of insulin-stimulated glucose transport in skeletal muscle following saturated fatty acid (FA) exposure. Importantly, a single bout of exercise can protect against acute lipid-induced insulin resistance. The mechanism by which exercise protects against lipid-induced insulin resistance is not completely known but may occur through a redirection of FA toward triacylglycerol (TAG) and away from ceramide and diacylglycerol (DAG). Therefore, in the current study, an in vitro preparation was used to examine whether a prior bout of exercise could confer protection against palmitate-induced insulin resistance and whether the pharmacological [50 μM fumonisin B(1) (FB1)] inhibition of ceramide synthesis in the presence of palmitate could mimic the protective effect of exercise. Soleus muscle of sedentary (SED), exercised (EX), and SED in the presence of FB1 (SED+FB1) were incubated with or without 2 mM palmitate for 4 h. This 2-mM palmitate exposure impaired insulin-stimulated glucose transport (-28%, P TAG accumulation in the SED group (P TAG (P net increase in ceramide content in response to palmitate exposure in the EX group was not different compared with SED, despite the maintenance of insulin sensitivity. The incubation of soleus from SED rats with FB1 (SED+FB1) prevented the detrimental effects of palmitate and caused a redirection of FA toward TAG accumulation (P < 0.05). Therefore, this research suggests that although inhibiting ceramide accumulation can prevent the detrimental effects of palmitate, a single prior bout of exercise appears to protect against palmitate-induced insulin resistance, which may be independent of changes in ceramide content. PMID:21325642

  4. Gas chromatography-mass spectrometry of ethyl palmitate calibration and resolution with ethyl oleate as biomarker ethanol sub acute in urine application study

    Suaniti, Ni Made; Manurung, Manuntun

    2016-03-01

    Gas Chromatography-Mass Spectrometry is used to separate two and more compounds and identify fragment ion specific of biomarker ethanol such as palmitic acid ethyl ester (PAEE), as one of the fatty acid ethyl esters as early detection through conyugated reaction. This study aims to calibrate ethyl palmitate and develop analysis with oleate acid. This methode can be used analysis ethanol and its chemistry biomarker in ethanol sub-acute consumption as analytical forensic toxicology. The result show that ethanol level in urine rats Wistar were 9.21 and decreased 6.59 ppm after 48 hours consumption. Calibration curve of ethyl palmitate was y = 0.2035 x + 1.0465 and R2 = 0.9886. Resolution between ethyl palmitate and oleate were >1.5 as good separation with fragment ion specific was 88 and the retention time was 18 minutes.

  5. Palmitate-induced inflammatory pathways in human adipose microvascular endothelial cells promote monocyte adhesion and impair insulin transcytosis.

    Pillon, Nicolas J; Azizi, Paymon M; Li, Yujin E; Liu, Jun; Wang, Changsen; Chan, Kenny L; Hopperton, Kathryn E; Bazinet, Richard P; Heit, Bryan; Bilan, Philip J; Lee, Warren L; Klip, Amira

    2015-07-01

    Obesity is associated with inflammation and immune cell recruitment to adipose tissue, muscle and intima of atherosclerotic blood vessels. Obesity and hyperlipidemia are also associated with tissue insulin resistance and can compromise insulin delivery to muscle. The muscle/fat microvascular endothelium mediates insulin delivery and facilitates monocyte transmigration, yet its contribution to the consequences of hyperlipidemia is poorly understood. Using primary endothelial cells from human adipose tissue microvasculature (HAMEC), we investigated the effects of physiological levels of fatty acids on endothelial inflammation and function. Expression of cytokines and adhesion molecules was measured by RT-qPCR. Signaling pathways were evaluated by pharmacological manipulation and immunoblotting. Surface expression of adhesion molecules was determined by immunohistochemistry. THP1 monocyte interaction with HAMEC was measured by cell adhesion and migration across transwells. Insulin transcytosis was measured by total internal reflection fluorescence microscopy. Palmitate, but not palmitoleate, elevated the expression of IL-6, IL-8, TLR2 (Toll-like receptor 2), and intercellular adhesion molecule 1 (ICAM-1). HAMEC had markedly low fatty acid uptake and oxidation, and CD36 inhibition did not reverse the palmitate-induced expression of adhesion molecules, suggesting that inflammation did not arise from palmitate uptake/metabolism. Instead, inhibition of TLR4 to NF-κB signaling blunted palmitate-induced ICAM-1 expression. Importantly, palmitate-induced surface expression of ICAM-1 promoted monocyte binding and transmigration. Conversely, palmitate reduced insulin transcytosis, an effect reversed by TLR4 inhibition. In summary, palmitate activates inflammatory pathways in primary microvascular endothelial cells, impairing insulin transport and increasing monocyte transmigration. This behavior may contribute in vivo to reduced tissue insulin action and enhanced tissue

  6. Retinyl Palmitate Supplementation Modulates T-bet and Interferon Gamma Gene Expression in Multiple Sclerosis Patients.

    Mohammadzadeh Honarvar, Niyaz; Harirchian, Mohammad Hossein; Abdolahi, Mina; Abedi, Elahe; Bitarafan, Sama; Koohdani, Fariba; Siassi, Feridoun; Sahraian, Mohammad Ali; Chahardoli, Reza; Zareei, Mahnaz; Salehi, Eisa; Geranmehr, Maziyar; Saboor-Yaraghi, Ali Akbar

    2016-07-01

    Vitamin A derivatives such as retinoic acid may improve the impaired balance of CD4+ T cells in autoimmune and inflammatory diseases. This study is a double-blind randomized trial to evaluate the effect of vitamin A (as form of retinyl palmitate) supplementation on multiple sclerosis (MS) patients. Thirty-nine patients were enrolled and randomly assigned to two groups. Both groups were followed for 6 months. The experimental group received 25,000 IU of retinyl palmitate daily, while the control group received a placebo. Before and after the study, the expression of interferon gamma (IFN-γ) and T-bet genes was evaluated in peripheral blood mononuclear cells of patients by RT-PCR. The results showed that after 6 months of supplementation, expression of IFN-γ and T-bet was significantly decreased. These data suggest that retinyl palmitate supplementation can modulate the impaired balance of Th1 and Th2 cells and vitamin A products that may be involved in the therapeutic mechanism of vitamin A in MS patients. This study provides information regarding the decreased gene expression of IFN-γ and T-bet in MS by retinyl palmitate supplementation. PMID:27122150

  7. Sheep erythrocyte membrane binding and transfer of long-chain fatty acids

    Bojesen, Inge Norby; Bojesen, Eigil

    1999-01-01

    Palmitic acid, oleic acid, linoleic acid, arachidonic acid, sheep erythrocyte ghosts, transporting elements, transport kinetics, fatty acid transport, transport rate constants......Palmitic acid, oleic acid, linoleic acid, arachidonic acid, sheep erythrocyte ghosts, transporting elements, transport kinetics, fatty acid transport, transport rate constants...

  8. Inhibition of uncoupling protein 2 with genipin exacerbates palmitate-induced hepatic steatosis

    Ma Shuangtao; Yang Dachun; Li; Tan Yan; Tang Bing; Yang Yongjian

    2012-01-01

    Abstract Background Uncoupling protein 2 (UCP2) was reported to be involved in lipid metabolism through regulating the production of superoxide anion. However, the role of UCP2 in hepatocytes steatosis has not been determined. We hypothesized that UCP2 might regulate hepatic steatosis via suppressing oxidative stress. Results We tested this hypothesis in an in vitro model of hepatocytic steatosis in HepG2 cell lines induced by palmitic acid (PA). We found that treatment with PA induced an obv...

  9. 维生素C多聚磷酸酯合成工艺研究%Synthesis of Ascorbyl Polyphosphate

    王敬臣; 崔凤霞; 曹琳青; 郑利宇; 曹晓伟

    2011-01-01

    采用单因素及正交试验研究了在敞开系统中,各种因素对以维生素C为原料在水溶液体系中直接酰化反应生成维生素C多聚磷酸酯的影响,结果表明,最佳反应条件:维生素C含量95%~100%,三偏磷酸钠含量70%,维生素C与三偏磷酸钠的质量比1∶1∶1,维生素C与氯化钙的摩尔比1∶0.075,反应温度40—50℃,反应溶液pH=10维生素C多聚磷酸酯的效价可达到36.87%,收率达96.84%.%Taking the ascorbic acid as raw material, through single factor and orthogonal experiment in the open systems, various factors is disscussed in aqueous solution of ascorbic acid directly acylation reaction of polyphosphate, the results show that the optimum reaction conditions: the ascorbic acid content is 95% ~100%, the sodium trimetaphosphat content is 70%, ascorbic acid and sodium trimetaphosphatin in the mass ratio of 1 : 1, ascorbic acid and calcium chloride in the molar ratio of 1 : 0. 075, the reaction temperature is 40~50 ℃ , the reaction solution pH of 10, the content of ascorbyl polyphosphate is up to 36. 87% and the yield is up to 96. 84%.

  10. Magnesium Ascorbyl Phosphate Regulates the Expression of Inflammatory Biomarkers in Cultured Sebocytes

    Lee, Weon Ju; Kim, Sang Lim; Choe, Yoon Seok; Jang, Yong Hyun; Lee, Seok-Jong; Kim, Do Won

    2015-01-01

    Background Acne is an inflammatory skin disorder caused by inflammatory biomarkers. Magnesium ascorbyl phosphate (MAP) is a stable precursor of vitamin C. It achieves a constant delivery of vitamin C into the skin and has antioxidative effects. Objective We performed this study to evaluate the effect of MAP on the expression of inflammatory biomarkers in cultured sebocytes. Methods Reverse transcription-polymerase chain reaction (RT-PCR) and enzyme-linked immunosorbent assay were performed fo...

  11. Mechanisms of Ascorbyl Radical Formation in Human Platelet-Rich Plasma

    Kou-Gi Shyu; Chao-Chien Chang; Yu-Chieh Yeh; Joen-Rong Sheu; Duen-Suey Chou

    2014-01-01

    Recently, many clinical reports have suggested that the ascorbyl free radical (Asc∙) can be treated as a noninvasive, reliable, real-time marker of oxidative stress, but its generation mechanisms in human blood have rarely been discussed. In this study, we used upstream substances, enzyme inhibitors, and free radical scavengers to delineate the mechanisms of Asc∙ formation in human platelet-rich plasma (PRP). Our results show that the doublet signal was detected in PRP samples by using electr...

  12. Determination of the antioxidant activity based on the content changes in fatty acid methyl esters in vegetable oils

    Housam Haj Hamdo; Zaid Al-Assaf; Warid Khayata

    2014-01-01

    Free radicals,which are generated in several biochemical reactions in the body,have been implicated as mediators of many diseases,including cancer,atherosclerosis and heart diseases.Although the endogenous antioxidants can scavenge these free radicals,they are often insufficient to maintain the in vivo redox balance.The antioxidant activity (AOA) was examined by addition of each tested antioxidants [alpha-tocopherol (a-T),beta-tocopherol (β-T),gamma-tocopherol (γ-T),delta-tocopherol (δ-T),butylated hydroxyanisole (BHA),2,6-di-tert-butyl-4-methylphenol (BHT),and ascorbyle palmitate (AP)] to four types of different vegetable oils (sunflower oil,soybean oil,corn oil and olive oil).Moreover,content changes in fatty acids were then investigated every 3 months during the storage period.The results showed that the AOA was different among the tested antioxidants.The AOA for BHA was the most for different types of oil compared with other antioxidants,whereas the δ-T possessed the lowest AOA.

  13. Palmitate stimulates glucose transport in rat adipocytes by a mechanism involving translocation of the insulin sensitive glucose transporter (GLUT4)

    Hardy, R. W.; Ladenson, J. H.; Henriksen, E. J.; Holloszy, J. O.; McDonald, J. M.

    1991-01-01

    In rat adipocytes, palmitate: a) increases basal 2-deoxyglucose transport 129 +/- 27% (p less than 0.02), b) decreases the insulin sensitive glucose transporter (GLUT4) in low density microsomes and increases GLUT4 in plasma membranes and c) increases the activity of the insulin receptor tyrosine kinase. Palmitate-stimulated glucose transport is not additive with the effect of insulin and is not inhibited by the protein kinase C inhibitors staurosporine and sphingosine. In rat muscle, palmitate: a) does not affect basal glucose transport in either the soleus or epitrochlearis and b) inhibits insulin-stimulated glucose transport by 28% (p less than 0.005) in soleus but not in epitrochlearis muscle. These studies demonstrate a potentially important differential role for fatty acids in the regulation of glucose transport in different insulin target tissues.

  14. In Vitro Palmitate Treatment of Myotubes from Postmenopausal Women Leads to Ceramide Accumulation, Inflammation and Affected Insulin Signaling

    Abildgaard, Julie; Henstridge, Darren C; Pedersen, Anette Tønnes;

    2014-01-01

    Menopause is associated with an increased incidence of insulin resistance and metabolic diseases. In a chronic palmitate treatment model, we investigated the role of skeletal muscle fatty acid exposure in relation to the metabolic deterioration observed with menopause. Human skeletal muscle...... satellite cells were isolated from premenopausal (n = 6) and postmenopausal (n = 5) women. In an in vitro model, the myotubes were treated with palmitate (300 µM) for one-, two- or three days during differentiation. Effects on lipid accumulation, inflammation and insulin signaling were studied. Palmitate......, post-myotubes showed a blunted insulin stimulated phosphorylation of AS160 in response to chronic palmitate treatment compared with pre-myotubes (p = 0.02). The increased intramyocellular ceramide content in the post-myotubes was associated with a significantly higher mRNA expression of Serine...

  15. Cystic fibrosis bronchial epithelial cells are lipointoxicated by membrane palmitate accumulation.

    Laurie-Anne Payet

    Full Text Available The F508del-CFTR mutation, responsible for Cystic Fibrosis (CF, leads to the retention of the protein in the endoplasmic reticulum (ER. The mistrafficking of this mutant form can be corrected by pharmacological chaperones, but these molecules showed limitations in clinical trials. We therefore hypothesized that important factors in CF patients may have not been considered in the in vitro assays. CF has also been associated with an altered lipid homeostasis, i. e. a decrease in polyunsaturated fatty acid levels in plasma and tissues. However, the precise fatty acyl content of membrane phospholipids from human CF bronchial epithelial cells had not been studied to date. Since the saturation level of phospholipids can modulate crucial membrane properties, with potential impacts on membrane protein folding/trafficking, we analyzed this parameter for freshly isolated bronchial epithelial cells from CF patients. Interestingly, we could show that Palmitate, a saturated fatty acid, accumulates within Phosphatidylcholine (PC in CF freshly isolated cells, in a process that could result from hypoxia. The observed PC pattern can be recapitulated in the CFBE41o(- cell line by incubation with 100 µM Palmitate. At this concentration, Palmitate induces an ER stress, impacts calcium homeostasis and leads to a decrease in the activity of the corrected F508del-CFTR. Overall, these data suggest that bronchial epithelial cells are lipointoxicated by hypoxia-related Palmitate accumulation in CF patients. We propose that this phenomenon could be an important bottleneck for F508del-CFTR trafficking correction by pharmacological agents in clinical trials.

  16. Fatty acid induced remodeling within the human liver fatty acid-binding protein.

    Sharma, Ashwani; Sharma, Amit

    2011-09-01

    We crystallized human liver fatty acid-binding protein (LFABP) in apo, holo, and intermediate states of palmitic acid engagement. Structural snapshots of fatty acid recognition, entry, and docking within LFABP support a heads-in mechanism for ligand entry. Apo-LFABP undergoes structural remodeling, where the first palmitate ingress creates the atomic environment for placement of the second palmitate. These new mechanistic insights will facilitate development of pharmacological agents against LFABP. PMID:21757748

  17. Fatty Acid Induced Remodeling within the Human Liver Fatty Acid-binding Protein*

    Sharma, Ashwani; Sharma, Amit

    2011-01-01

    We crystallized human liver fatty acid-binding protein (LFABP) in apo, holo, and intermediate states of palmitic acid engagement. Structural snapshots of fatty acid recognition, entry, and docking within LFABP support a heads-in mechanism for ligand entry. Apo-LFABP undergoes structural remodeling, where the first palmitate ingress creates the atomic environment for placement of the second palmitate. These new mechanistic insights will facilitate development of pharmacological agents against ...

  18. KINETIC STUDY OF PALMITIC ACID ESTERIFICATION CATALYZED BY Rhizopus oryzae RESTING CELLS Estudio cinético de la esterificación del ácido palmítico catalizado por células en reposo de Rhizopus oryzae

    JONH J MÉNDEZ

    Full Text Available In the present study, a kinetic model for the biocatalytic synthesis of esters using Rhizopus oryzae resting cells is proposed. The kinetic study has been made in a range of 30-50 °C and atmospheric pressure. The Influence of operating variables, water content, pH, amount of mycelium was studied. Different values of temperature, initial mycelium concentration and acid/alcohol molar ratio were tested. Initial rates were estimated from the slope of the concentration of palmitic acid, or their corresponding ester at conversions of less than 10%, versus time and reported as mmol l-1 min -1. The values of kinetic constants were computed using the freeware program SIMFIT (http:\\www.simfit.man.ac.uk.En el presente estudio, un modelo cinético para la síntesis de esteres usando Rhizopus oryzae resting cells es propuesto. El estudio cinético fue realizado en un rango de temperatura de 30-50 ºC a presión atmosférica reducida. La influencia de las variables de operación tales como temperatura, pH y contenido de agua fueron estudiadas. Diferentes valores de concentración de micelio y relación molar de ácido/alcohol son ensayadas, Las velocidades iníciales se estimaron de la curva de concentración de acido palmítico, y su correspondiente conversión a ester en menos del 10%, frente a tiempo y reportadas en mmol I-1 min -1. Los valores de las constantes cinéticas fueron calculados usando el programa freeware SIMFIT (http:\\www.simfit.man.ac.uk

  19. Study on lipase-catalytic synthesis of ascorbyl palmitate%脂肪酶催化合成棕榈酸维生素C酯的研究

    夏木西卡玛尔; 吾满江·艾力

    2007-01-01

    在溶剂相中,用固定化脂肪酶催化合成棕榈酸维生素C酯.研究了反应体系含水量、溶剂、反应温度、加酶量、加入分子筛等因素对反应的影响.结果表明,最佳反应条件为:Novo 435脂肪酶用量为反应物质量的4%,叔丁醇作溶剂,反应温度55℃,摇床转速200 r/min,反应时间36 h,转化率52%,产品纯度95%.

  20. 酰氯法合成L-抗坏血酸棕榈酸酯的研究%Synthesis of L-ascorbyl Palmitate with Acyl Chloride Method

    许肇成; 何松; 陈永恒; 林富强

    2010-01-01

    本文对酰氯法反应制备L-抗坏血酸棕榈酸酯的反应介质、提取液和催化剂进行初步探讨,结果表明甲基乙酰胺和二氯甲烷为反应介质、以氯化亚砜或氯化氢作催化剂对产率有较大提高,氯仿为提取液可以提高产品纯度.

  1. Study on Antioxidation Effect of Ascorbyl Palmitate%L-抗坏血酸棕榈酸酯的抗氧化效果研究

    高荫榆; 雷占兰; 谢何融; 郭磊

    2007-01-01

    L-抗坏血酸棕榈酸酯(AP)是具有功能性、营养性、无毒、高效的抗氧化剂,应用范围广泛.本实验以乌桕脂棕榈酸甲酯为原料,采用化学法将其与抗坏血酸合成AP,并将其应用到大豆油与菜籽油当中,与BHA、TBHQ、VE及AP/VE效果相比较,评价其抗氧化效率.结果表明,AP具有显著的抗氧化性,是一种安全、高效的抗氧化剂和增效剂.

  2. HPLC Determination of Ascorbyl Palmitate in Foods%高效液相色谱法测定食品中抗坏血酸棕榈酸酯

    陆志芸; 张辉; 赵敏; 葛宇; 林毅侃; 周耀斌

    2010-01-01

    提出了快速测定油脂食品、焙烤食品和方便米面食品中抗坏血酸棕榈酸酯的高效液相色谱法.以柠檬酸和异抗坏血酸为稳定剂,甲醇为样品提取剂,以甲醇-乙腈(1+1)及磷酸(1+99)溶液为流动相,经反相C18色谱柱梯度洗脱,在243 nm波长处,用光电二极管阵列检测器进行测定.抗坏血酸棕榈酸酯的质量浓度在0.50~100.0 mg·L-1范围内与其峰面积呈线性关系,测定下限(10S/N)为0.005 g·kg-1.加标回收率在85%~104%之间,相对标准偏差(n=6)在1.1%~3.9%之间.

  3. Study on the antioxidation of L-ascorbyl palmitate%L-抗坏血酸棕榈酸酯的抗氧化性研究

    雷琳

    2009-01-01

    目的:研究L-抗坏血酸棕榈酸酯(L-AP)的抗氧化性.方法:将L-AP应用到猪油、大豆油与菜籽油当中,与CMG、BHA、TSHQ、维生素E及AP/维生素E效果比较.评价其抗氧化效率.结果:L-AP的加入对油脂的各种品质有明显的改善作用.结论:L-AP具有显著的抗氧化性,是一种安全、高效的抗氧化剂和增效剂.

  4. L-抗坏血酸棕榈酸酯的合成及应用%Synthesis and application of L-ascorbyl palmitate

    曹会兰; 杨建武

    2003-01-01

    研究了一种以L-抗坏血酸和棕榈酸为原料,合成出L-抗坏血酸棕榈酸酯(AP)的改进方法,产率为86%.并探讨了AP作为抗氧剂在棉籽油中的应用,结果表明AP的抗氧效果优于BHA和BHT.

  5. Advances in Research on Synthesis of L-Ascorbyl Palmitate%L-抗坏血酸棕榈酸酯的合成研究进展

    刘长波; 高瑞昶

    2003-01-01

    L-抗坏血酸棕榈酸酯是优良的天然抗氧化剂.综述了L-抗坏血酸棕榈酸酯合成研究进展,归纳了L-抗坏血酸棕榈酸酯的几种合成方法,如化学合成法和酶催化法,为其合成研究提供一些线索.

  6. Palmitato de ascorbil e acetato de tocoferol como antioxidantes metabólicos em larvas de dourado Ascorbyl palmitate and tocopherol acetate as metabolic antioxidants in dourado larvae

    Daniel Okamura; Felipe Guedes de Araújo; Priscila Viera Rosa Logato; Ulisses Simon da Silveira; Luis David Solis Murgas; Rilke Tadeu Fonseca de Freitas

    2008-01-01

    O objetivo deste trabalho foi avaliar o efeito e a interação entre a suplementação de palmitato de ascorbil e acetato de tocoferol, na alimentação de larvas de dourado (Salminus brasiliensis), durante o seu desenvolvimento inicial. Foi utilizado o delineamento experimental inteiramente ao acaso, com parcelas subdivididas: nas parcelas, em arranjo fatorial (2x3) com seis rações constituídas pela combinação de duas concentrações de acetato de tocoferol (0 e 250 mg kg-1) e três concentrações de ...

  7. Effect of surface-potential modulators on the opening of lipid pores in liposomal and mitochondrial inner membranes induced by palmitate and calcium ions.

    Belosludtsev, Konstantin N; Belosludtseva, Natalia V; Agafonov, Alexey V; Penkov, Nikita V; Samartsev, Victor N; Lemasters, John J; Mironova, Galina D

    2015-10-01

    The effect of surface-potential modulators on palmitate/Ca2+-induced formation of lipid pores was studied in liposomal and inner mitochondrial membranes. Pore formation was monitored by sulforhodamine B release from liposomes and swelling of mitochondria. ζ-potential in liposomes was determined from electrophoretic mobility. Replacement of sucrose as the osmotic agent with KCl decreased negative ζ-potential in liposomes and increased resistance of both mitochondria and liposomes to the pore inducers, palmitic acid, and Ca2+. Micromolar Mg2+ also inhibited palmitate/Ca2+-induced permeabilization of liposomes. The rate of palmitate/Ca2+-induced, cyclosporin A-insensitive swelling of mitochondria increased 22% upon increasing pH from 7.0 to 7.8. At below the critical micelle concentration, the cationic detergent cetyltrimethylammonium bromide (10 μM) and the anionic surfactant sodium dodecylsulfate (10-50 μM) made the ζ-potential less and more negative, respectively, and inhibited and stimulated opening of mitochondrial palmitate/Ca2+-induced lipid pores. Taken together, the findings indicate that surface potential regulates palmitate/Ca2+-induced lipid pore opening. PMID:26014488

  8. Dynamic nuclear polarization-magnetic resonance imaging at low ESR irradiation frequency for ascorbyl free radicals

    Shinji Ito; Fuminori Hyodo

    2016-01-01

    Highly water-soluble ubiquinone-0 (CoQ0) reacts with ascorbate monoanion (Asc) to mediate the production of ascorbyl free radicals (AFR). Using aqueous reaction mixture of CoQ0 and Asc, we obtained positively enhanced dynamic nuclear polarization (DNP)-magnetic resonance (MR) images of the AFR at low frequency (ranging from 515 to 530 MHz) of electron spin resonance (ESR) irradiation. The shape of the determined DNP spectrum was similar to ESR absorption spectra with doublet spectral peaks. T...

  9. Associations between hepatic metabolism of propionate and palmitate in liver slices from transition dairy cows.

    McCarthy, M M; Piepenbrink, M S; Overton, T R

    2015-10-01

    Multiparous Holstein cows (n=95) were used to evaluate changes in hepatic propionate and palmitate metabolism and liver composition over time during the transition period, along with the relationships of these variables with cumulative increases in nonesterified fatty acids and β-hydroxybutyrate during the periparturient period. Data from 3 previous experiments were used to address the study objectives, accounting for a total of 95 multiparous Holstein cows. Liver slices from biopsies on d -21, 1, and 21 relative to parturition were used to determine conversion of [1-(14)C]palmitate to CO2 and esterified products (EP) and the conversion of [1-(14)C]propionate to CO2 and glucose. Hepatic glycogen content was highest on d -21 and was 26.9 and 36.5% of prepartum values on d 1 and 21, respectively. Liver triglyceride content was lowest at d -21 and was 271 and 446% of prepartum values on d 1 and 21, respectively. We detected no difference in the capacity for the liver to oxidize [1-(14)C]palmitate to CO2 between d -21 and d 1; however, on d 21, oxidation was 84% of prepartum values. The capacity of the liver to convert [1-(14)C]palmitate to EP was 148 and 139% of prepartum values on d 1 and 21, respectively. The capacity of liver to convert [1-(14)C]propionate to CO2 was 127 and 83% of prepartum values on d 1 and 21, and the capacity of liver to convert [1-(14)C]propionate to glucose was 126 and 85% of prepartum values on d 1 and 21, respectively. Correlation relationships suggest that overall, cows with elevated prepartum liver triglyceride content had elevated triglycerides throughout the transition period along with increased [1-(14)C]palmitate oxidation and conversion to EP and a decreased propensity to convert [1-(14)C]propionate to glucose. Cows with increased [1-(14)C]propionate oxidation had increased conversion of [1-(14)C]propionate to glucose throughout the transition period. Overall, conditions that lead to impairments in fatty acid metabolism during the

  10. Lipophilization of ascorbic acid: a monolayer study and biological and antileishmanial activities.

    Kharrat, Nadia; Aissa, Imen; Sghaier, Manel; Bouaziz, Mohamed; Sellami, Mohamed; Laouini, Dhafer; Gargouri, Youssef

    2014-09-17

    Ascorbyl lipophilic derivatives (Asc-C2 to Asc-C(18:1)) were synthesized in a good yield using lipase from Staphylococcus xylosus produced in our laboratory and immobilized onto silica aerogel. Results showed that esterification had little effect on radical-scavenging capacity of purified ascorbyl esters using DPPH assay in ethanol. However, long chain fatty acid esters displayed higher protection of target lipids from oxidation. Moreover, compared to ascorbic acid, synthesized derivatives exhibited an antibacterial effect. Furthermore, ascorbyl derivatives were evaluated, for the first time, for their antileishmanial effects against visceral (Leishmania infantum) and cutaneous parasites (Leishmania major). Among all the tested compounds, only Asc-C10, Asc-C12, and Asc-C(18:1) exhibited antileishmanial activities. The interaction of ascorbyl esters with a phospholipid monolayer showed that only medium and unsaturated long chain (Asc-C10 to Asc-C(18:1)) derivative esters were found to interact efficiently with mimetic membrane of leishmania. These properties would make ascorbyl derivatives good candidates to be used in cosmetic and pharmaceutical lipophilic formulations. PMID:25148258

  11. Palmitate-induced changes in energy demand cause reallocation of ATP supply in rat and human skeletal muscle cells.

    Nisr, Raid B; Affourtit, Charles

    2016-09-01

    Mitochondrial dysfunction has been associated with obesity-related muscle insulin resistance, but the causality of this association is controversial. The notion that mitochondrial oxidative capacity may be insufficient to deal appropriately with excessive nutrient loads is for example disputed. Effective mitochondrial capacity is indirectly, but largely determined by ATP-consuming processes because skeletal muscle energy metabolism is mostly controlled by ATP demand. Probing the bioenergetics of rat and human myoblasts in real time we show here that the saturated fatty acid palmitate lowers the rate and coupling efficiency of oxidative phosphorylation under conditions it causes insulin resistance. Stearate affects the bioenergetic parameters similarly, whereas oleate and linoleate tend to decrease the rate but not the efficiency of ATP synthesis. Importantly, we reveal that palmitate influences how oxidative ATP supply is used to fuel ATP-consuming processes. Direct measurement of newly made protein demonstrates that palmitate lowers the rate of de novo protein synthesis by more than 30%. The anticipated decrease of energy demand linked to protein synthesis is confirmed by attenuated cycloheximide-sensitivity of mitochondrial respiratory activity used to make ATP. This indirect measure of ATP turnover indicates that palmitate lowers ATP supply reserved for protein synthesis by at least 40%. This decrease is also provoked by stearate, oleate and linoleate, albeit to a lesser extent. Moreover, palmitate lowers ATP supply for sodium pump activity by 60-70% and, in human cells, decreases ATP supply for DNA/RNA synthesis by almost three-quarters. These novel fatty acid effects on energy expenditure inform the 'mitochondrial insufficiency' debate. PMID:27154056

  12. Lipase-catalyzed synthesis of ascorbyl oleate in acetone: optimization of reaction conditions and lipase reusability.

    Stojanović, Marija; Velićković, Dušan; Dimitrijević, Aleksandra; Milosavić, Nenad; Knežević-Jugović, Zorica; Bezbradica, Dejan

    2013-01-01

    Lipase-catalyzed ascorbyl oleate synthesis is eco-friendly and selective way of production of liposoluble biocompatible antioxidants, but still not present on an industrial level due to the high biocatalyst costs. In this study, response surface methodology was applied in order to estimate influence of individual experimental factors, identify interactions among them, and to determine optimum conditions for enzymatic synthesis of ascorbyl oleate in acetone, in terms of limiting substrate conversion, product yield, and yield per mass of consumed enzyme. As a biocatalyst, commercial immobilized preparation of lipase B from Candida antarctica, Novozym 435, was used. In order to develop cost-effective process, at reaction conditions at which maximum amount of product per mass of biocatalyst was produced (60°C, 0.018 % (v/v) of water, 0.135 M of vitamin C, substrates molar ratio 1:8, and 0.2 % (w/v) of lipase), possibilities for further increase of ester yield were investigated. Addition of molecular sieves at 4(th) hour of reaction enabled increase of yield from 16.7 mmol g⁻¹ to 19.3 mmol g⁻¹. Operational stability study revealed that after ten reaction cycles enzyme retained 48 % of its initial activity. Optimized synthesis with well-timed molecular sieves addition and repeated use of lipase provided production of 153 mmol per gram of enzyme. Further improvement of productivity was achieved using procedure for the enzyme reactivation. PMID:23985489

  13. Insulin Resistance Is Correlated with Palmitic Acid Uptake in Skeletal Muscle Cells%棕榈酸的组织吸收分布及对骨骼肌胰岛素抵抗的影响

    彭恭; 刘延波; 李凌海; 刘平生

    2012-01-01

    Retinoids (vitamin A and its derivatives) play important roles in the maintenance of various tissues in the adult vertebrate and are essential for diverse embryological processes. As a member of retinoids (vitamin A and its derivatives), retinoic acid (RA) has been extensively investigated in embryopathology. However, the mechanisms by which RA influences these processes are not completely understood. In the present study, we found that embryonic RA exposure via maternal treatment with gavage-fed 3 successive doses of RA on day 8 of gestation led to a high incidence (96.77%, 30/31) of rachischisis with myeloschisis, I.e., spina bifida aperta, among the surviving day 18 fetuses. Using microarray technology, we identified 134 genes in the spinal cords of mice that exhibit at least a 1.5-fold change between mice with spina bifida and control samples. Several downstream genes of RA signaling involved in lipid metabolism were regulated at the transcriptional level after maternal RA exposure. Furthermore, a gene set enrichment analysis (GSEA) implicate many altered expression of genes, involved in pro- or anti-apoptosis, cell proliferation, migration, cytoskeleton components, and cell or focal adhesion, which are associated which the spina bifida induced by the maternal RA exposure. This indicates that defective functions of these cell components and biological processes preceded the abnormal development of neural tube. Our study provides a global analysis of gene expression patterns in spina bifida and will help the understanding of the etiology and pathology of neural tube defects.%脂肪酸代谢紊乱是Ⅱ型糖尿病的主要致病因素之一.棕榈酸是血液中含量最高的游离脂肪酸.我们建立了大鼠颈静脉置管输注棕榈酸的模型,发现血液中的大部分棕榈酸被骨骼肌组织所吸收.以棕榈酸处理的C2C12骨骼肌细胞为实验模型发现,棕榈酸进入骨骼肌细胞后的中间代谢产物(磷脂和甘油二酯)的累

  14. Effect of the alkyl chains and of the headgroups on the thermal behavior of ascorbic acid surfactants mixtures.

    Venturini, Chiara; Pomposi, Cristina; Ambrosi, Moira; Carretti, Emiliano; Fratini, Emiliano; Lo Nostro, Pierandrea; Baglioni, Piero

    2014-03-20

    The role of the alkyl chain length and of the headgroup on the thermal behavior of mixtures of ASC8 (ascorbyl octanoate) and ASC16 (ascorbyl hexadecanoate) was investigated through differential scanning calorimetry, small- and wide-angle X-ray scattering, and Fourier transform infrared spectroscopy experiments. The formation of two eutectics and of a peritectic point was found from the phase diagram, and their structural properties were studied. The results were compared by investigating the thermal behavior of mixtures of octanoic acid and hexadecanoic acid. The findings provide insights into the role of the ascorbyl headgroups on the intermolecular interactions that determine the phase behavior of the two ascorbic acid based surfactants in the solid state. PMID:24555769

  15. Molecular Dynamics Simulation of Palmitate Ester Self-Assembly with Diclofenac

    Abu Bakar Salleh

    2012-07-01

    Full Text Available Palm oil-based esters (POEs are unsaturated and non-ionic esters with a great potential to act as chemical penetration enhancers and drug carriers for transdermal drug nano-delivery. A ratio of palmitate ester and nonionic Tween80 with and without diclofenac acid was chosen from an experimentally determined phase diagram. Molecular dynamics simulations were performed for selected compositions over a period of 15 ns. Both micelles showed a prolate-like shape, while adding the drug produced a more compact micellar structure. Our results proposed that the drug could behave as a co-surfactant in our simulated model.

  16. VC复合脂肪酸酯的合成及抗氧化性能%SYNTHESIS AND ANTIOXIDANT EFFECTS OF ASCORBYL COMPOSITE ALIPHATIC ESTER

    冯光炷; 谢文磊

    2001-01-01

    猪油与甲醇进行酯交换制备复合脂肪酸甲酯,得率97.2%.再以浓硫酸为溶剂和催化剂,VC和复合脂肪酸甲酯进行酯交换合成VC复合脂肪酸酯.考察了反应时间、反应物配比及浓硫酸用量对酯交换反应的影响,结果表明,最适宜的反应条件为:n(VC)∶n(复合脂肪酸酯)为1∶1.2,反应时间为26h,n(浓H2SO4)∶n(VC+复合脂肪酸酯)为1∶0.15,反应温度为25℃,产率达76%.产品的抗氧化性能测试表明VC复合脂肪酸酯是一种优良的无毒抗氧化剂.%Ascorbyl composite aliphatic ester was synyhesized by transesterificantion of L-ascorbic acid with methyl composite aliphatic ester which is synthesized from lard and methyl alcohol using concentrated sulfuric acid as sol ve nt and catalyst. The yield was up to 76%. The effects of reaction temperature, r atio of reactant, amount of concentrated sulfuric acid on transesterification ha ve been investigated. The optimum synthetic conditions are that the ratio of Vc to composite aliphatic ester is 1∶1.2,reaction time is 26 h, the ratio of conce ntrated H2SO4 to composite aliphatic ester is 1∶0.15,reaction temperatur e is 25 ℃ .The test of antioxidant shows that Ascorbyl composite aliphatic ester is a good oxidant without poison.

  17. Levels of retinyl palmitate and retinol in the skin of SKH-1 mice topically treated with retinyl palmitate and concomitant exposure to simulated solar light for thirteen weeks.

    Yan, J; Xia, Q; Wamer, W G; Boudreau, M D; Warbritton, A; Howard, P C; Fu, P P

    2007-11-01

    Retinyl esters account for more than 70% of the endogenous vitamin A found in human skin, and retinyl palmitate is one of the retinyl esters in this pool. Human skin is also exposed to retinyl palmitate exogenously through the topical application of cosmetic and skin care products that contain retinyl palmitate. To date, there is limited information on the penetration and distribution of retinyl palmitate and vitamin A within in the skin. In this study, the accumulation of retinyl palmitate and generation of retinol in the skin of male and female SKH-1 mice that received repeated topical applications of creams containing 0.0%, 0.1%, 0.5%, 1.0%, 5.0%, 10%, or 13% of retinyl palmitate 5 days a week for a period of 13 weeks were studied. Because products containing retinyl palmitate are frequently applied to sun-exposed skin, and because it is well established that exposure to sunlight and UV light can alter cutaneous levels of retinoids, mice in this study were additionally exposed 5 days a week to simulated solar light. The results showed that retinyl palmitate diffused into the skin and was partially hydrolyzed to retinol. The levels of retinyl palmitate in the skin of mice that were administered retinyl palmitate cream were higher than control values, and levels of both retinyl palmitate and retinol increased with the application of higher concentrations of retinyl palmitate in the cream. Our results indicate that topically applied retinyl palmitate may alter the normal physiological levels of retinyl palmitate and retinol in the skin of SKH-1 mice and may have a significant impact on vitamin A homeostasis in the skin. PMID:18717516

  18. Application of antioxidants during short-path distillation of structured lipids

    Timm-Heinrich, Maike; Xu, Xuebing; Nielsen, Nina Skall;

    2007-01-01

    A specific structured lipid was produced from sunflower oil and caprylic acid. The antioxidative effect of adding alpha-tocopherol, ascorbyl palmitate or citric acid (each in three different concentrations) was investigated before and after the purification process (short-path distillation), and...... was compared with a control without addition of antioxidant. The oxidative status and stability were characterized by peroxide and anisidine values, secondary volatile oxidation products and induction period. The antioxidants affected the oxidative status compared with the control: citric acid was...... prooxidative at low concentrations, but antioxidative at high concentrations. Addition of ascorbyl palmitate had an antioxidative effect at all concentrations employed. alpha-Tocopherol showed less antioxidative activity compared with ascorbyl palmitate and citric acid, and its efficacy was slightly decreased...

  19. Effects of Paliperidone Palmitate on Coagulation: An Experimental Study

    Enver Demirel Yılmaz; Sedat Motor; Fatih Sefil; Neslihan Pınar; Hanifi Kokacya; Mustafa Kisa; Suleyman Oktar

    2014-01-01

    Objective. The aim of the present study was to examine the effects of a new antipsychotic drug paliperidone palmitate on hemogram and coagulation parameters in rats. Materials and Methods. Experiments were performed on 22 female albino Wistar rats (8–12 weeks old). Control group was given drinking water as vehicle (0.3 mL). PAL-1 rats were given 1 mg/kg paliperidone palmitate (in 0.3 mL drinking water) by oral gavage once a day for ten days and PAL-3 rats received 3 mg/kg paliperidone palmita...

  20. Effect of exogenous fatty acids on biotin deprived death of Saccharomyces cerevisiae

    The effect of exogeneous fatty acids on cell growth and death of the biotin-requiring yeast Saccharomyces cerevisiae BA-1 was examined with respect to the mechanism of synthetic pathway of fatty acid under biotin starvation. At a growth temperature of 300C, exogeneous unsaturated fatty acids, such as palmitoleic, oleic, linoleic, and linolenic acids which promote the cell growth and suppress death effectively, were incorporated intactly into the cellular fatty acids, whereas the saturated fatty acid, palmitic acid, which supports growth but some what inhibits death, was once incorporated, and about 60% of incorporated palmitic acid was found to be desaturated. However, at an elevated temperature of 360C, even palmitic acid showed similar effects to unsaturated fatty acids in cell growth and death; following by an increased desaturation of palmitic acid. Thus the data indicate that palmitic aicd, as well as unsaturated fatty acids directly compensate for the deficiency of endogenously synthesized fatty acids caused by biotin starvation. (auth.)

  1. The efficacy of compounds with different polarities as antioxidant in emulsions with omega-3 lipids

    Sørensen, Ann-Dorit Moltke; Nielsen, Nina Skall; Decker, Eric A.;

    2011-01-01

    evaluate the efficacy of antioxidants [ascorbic acid, ascorbyl palmitate, ascorbyl CLA and CLA (conjugated linoleic acid)] with different polarities in two different emulsion systems: o/w emulsion (5% oil) and w/o emulsion (98% oil) stabilized with citrem and PGPR, respectively. The efficacy of the...... antioxidants was compared to their partitioning in an o/w emulsion system and to results obtained from different antioxidant assays: iron reducing power, chelating activity and radical scavenging activity. For the w/o emulsions the efficacy of the antioxidants followed the polar paradox hypothesis: ascorbyl...

  2. Enhancement of stress resistance of the guppy Poecilia reticulata through feeding with vitamin C supplement

    Lim, L C; Dhert, P.; Chew, W.Y.; Dermaux, V.; Nelis, H.; Sorgeloos, P.

    2002-01-01

    This study investigated the use of vitamin C supplement in formulated diets and live Artemia juveniles to enhance the stress resistance of the guppy Poecilia reticulata. To evaluate the stress resistance, fish were subjected to osmotic shock in pre-aerated water containing 35 ppt sodium chloride. Ascorbyl acid-poly phosphate and ascorbyl palmitate were used as vitamin C sources for formulated diets and live Artemia juveniles, respectively. Results showed that guppies fed moist formulated diet...

  3. Preparation of starch-stabilized silver nanoparticles from amylose-sodium palmitate inclusion complexes

    Starch-stabilized silver nanoparticles were prepared from amylose-sodium palmitate complexes by first converting sodium palmitate to silver palmitate by reaction with silver nitrate and then reducing the silver ion to metallic silver. This process produced water solutions that could be dried and the...

  4. Radiolytical oxidation of ascorbic acid in aqueous solutions

    Complete text of publication follows. Ascorbic acid, AsA (vitamin c), has been widely studied as an antioxidant or as an initiator of some technological processes, for example polymerization or nanoparticles formation. AsA can be easily oxidized to ascorbyl radical, in the first stage, and to dehydroascorbic acid, DHA, in the second stage. It has been found that several different ascorbyl radicals are formed during AsA oxidation but the main radical exists as the anion with the unpaired electron delocalized on a highly conjugated tricarbonyl system. Absorption spectrum of ascorbyl radical shows two bands with maxima at 300 and 360 nm, however only that at 360 nm is proportional to the dose and thus this wavelength was chosen for observations. We studied the oxidation of AsA by the following oxidizing radicals generated by the pulse radiolysis method ·OH, (SCN)2-·, Cl2-·, N3· and NO2·. The observed dependence of the yield and the formation rate of the AsA radical on the reduction potential of the oxidizing radical is discussed. The results obtained in water are compared with those obtained with AsA enclosed in the water pools of reverse micelles formed by AOT in n-heptane or by Igepal CO-520 in c-hexane. Somewhat surprising observation of different ascorbyl radical in pulse irradiated reverse micelles containing DHA is also commented.

  5. Palmitate binding to serum albumin, measured by rate of dialysis

    Brodersen, R; Honoré, B; Andersen, S

    1988-01-01

    Dialysis experiments were performed with an acetylcellulose membrane between two identical sample solutions; a trace amount of radiolabelled palmitate was added on one side and the rate of dialytic equilibration of the label was measured. By comparison with rates measured in standard experiments...

  6. Stability evaluation of tocopheryl acetate and ascorbyl tetraisopalmitate in isolation and incorporated in cosmetic formulations using thermal analysis

    Mariana Mandelli de Almeida; Cibele Rosana Ribeiro de Castro Lima; Joyce Santos Quenca-Guillen; Elder Moscardini Filho; Lucildes Pita Mercuri; Maria Inês Rocha Miritello Santoro; Erika Rosa Maria Kedor-Hackmann

    2010-01-01

    In view of the increase in the number of cosmetic preparations containing antioxidant vitamins, chiefly, due to their action in preventing the process of skin aging, there is a need to develop pre-formulation studies and to validate analytical methods in order to obtain high quality products. Thus, the objective of this research was to evaluate and compare the thermal behavior of tocopheryl acetate and ascorbyl tetraisopalmitate as raw materials, and incorporated into a base cream. Thermograv...

  7. Enzyme-controlled scavenging of ascorbyl and 2,6-dimethoxy-semiquinone free radicals in Ehrlich ascites tumor cells.

    Pethig, R; Gascoyne, P R; McLaughlin, J. A.; Szent-Györgyi, A

    1985-01-01

    The rate of scavenging by Ehrlich ascites cells of anionic ascorbyl and 2,6-dimethoxy-p-semiquinone free radicals has been investigated by electron spin resonance spectroscopy both for viable cells and for subcellular fractions obtained by differential centrifugation. The scavenging activity is concluded to be associated with an NAD(P)H enzyme containing an active sulfhydryl group. Attempts to identify the enzyme with the reported properties of either semi-dehydro-ascorbate reductase or DT-di...

  8. Study on stability of L-ascorbyl decanoate, L-ascorbyl laurate and L-ascorbyl palmitate%抗坏血酸癸酸酯、抗坏血酸月桂酸酯和抗坏血酸棕榈酸酯的稳定性研究

    江晨; 刘柳; 黄才欢; 汪勇; 晏日安

    2015-01-01

    利用碘量法测定含量,探究了光照、温度、pH及金属离子对抗坏血酸癸酸酯、抗坏血酸月桂酸酯和抗坏血酸棕榈酸酯乙醇溶液稳定性的影响.结果表明:光照、高温和碱性条件都会不同程度地对三者的稳定性造成影响,而酸性、中性条件以及体系中添加的金属离子Mg2+、Ca2+、Na+、Fe2+对三者稳定性的影响均不大.除光照条件外,其他条件下三者稳定性差异并不大.

  9. Physical activity is associated with retained muscle metabolism in human myotubes challenged with palmitate

    Green, C J; Bunprajun, T; Pedersen, B K;

    2013-01-01

    in satellite cells challenged with palmitate. Although the benefits of physical activity on whole body physiology have been well investigated, this paper presents novel findings that both diet and exercise impact satellite cells directly. Given the fact that satellite cells are important for muscle......  The aim of this study was to investigate whether physical activity is associated with preserved muscle metabolism in human myotubes challenged with saturated fatty acids. Human muscle satellite cells were isolated from sedentary or active individuals and differentiated into myocytes in culture...... and correlated positively to JNK phosphorylation. In conclusion, muscle satellite cells retain metabolic differences associated with physical activity. Physical activity partially protects myocytes from fatty acid-induced insulin resistance and inactivity is associated with dysregulation of metabolism...

  10. Control of bovine hepatic fatty acid oxidation

    Jesse, B.W.; Emery, R.S.; Thomas, J.W.

    1986-09-01

    Fatty acid oxidation by bovine liver slices and mitochondria was examined to determine potential regulatory sites of fatty acid oxidation. Conversion of 1-(/sup 14/C)palmitate to /sup 14/CO/sub 2/ and total (/sup 14/C)acid-soluble metabolites was used to measure fatty acid oxidation. Oxidation of palmitate (1 mM) was linear in both liver slice weight and incubation time. Carnitine stimulated palmitate oxidation; 2 mM dl-carnitine produced maximal stimulation of palmitate oxidation to both CO/sup 2/ and acid-soluble metabolites. Propionate (10 mM) inhibited palmitate oxidation by bovine liver slices. Propionate (.5 to 10 mM) had no effect on palmitate oxidation by mitochondria, but malonyl Coenzyme A, the first committed intermediate of fatty acid synthesis, inhibited mitochondrial palmitate oxidation (inhibition constant = .3 ..mu..M). Liver mitochonndrial carnitine palmitoyltransferase exhibited Michaelis constants for palmitoyl Coenzyme A and l-carnitine of 11.5 ..mu..M and .59 mM, respectively. Long-chain fatty acid oxidation in bovine liver is regulated by mechanisms similar to those in rats but adapted to the unique digestive physiology of the bovine.

  11. Control of bovine hepatic fatty acid oxidation

    Fatty acid oxidation by bovine liver slices and mitochondria was examined to determine potential regulatory sites of fatty acid oxidation. Conversion of 1-[14C]palmitate to 14CO2 and total [14C]acid-soluble metabolites was used to measure fatty acid oxidation. Oxidation of palmitate (1 mM) was linear in both liver slice weight and incubation time. Carnitine stimulated palmitate oxidation; 2 mM dl-carnitine produced maximal stimulation of palmitate oxidation to both CO2 and acid-soluble metabolites. Propionate (10 mM) inhibited palmitate oxidation by bovine liver slices. Propionate (.5 to 10 mM) had no effect on palmitate oxidation by mitochondria, but malonyl Coenzyme A, the first committed intermediate of fatty acid synthesis, inhibited mitochondrial palmitate oxidation (inhibition constant = .3 μM). Liver mitochonndrial carnitine palmitoyltransferase exhibited Michaelis constants for palmitoyl Coenzyme A and l-carnitine of 11.5 μM and .59 mM, respectively. Long-chain fatty acid oxidation in bovine liver is regulated by mechanisms similar to those in rats but adapted to the unique digestive physiology of the bovine

  12. A case of paliperidone-palmitate-induced tardive dyskinesia.

    Lally, John

    2012-06-13

    OBJECTIVES: This is one of the first cases reported in the literature of paliperidone-palmitate-induced prolonged dyskinesia. METHOD: Case report. RESULTS: We report the case of a 49-year-old woman with paranoid schizophrenia who developed orofacial dyskinesia some 4 months after the commencement of paliperidone long-acting injection. CONCLUSION: This case serves as a clinical reminder that dyskinesia can occur with all antipsychotic medications.

  13. Pharmacoeconomic analysis of paliperidone palmitate for treating schizophrenia in Greece

    Einarson Thomas R; Geitona Maria; Chaidemenos Alexandros; Karpouza Vasiliki; Mougiakos Theodoros; Paterakis Periklis; Ploumpidis Dimitrios; Potamitis-Komis Dionyssios; Zilbershtein Roman; Vicente Colin; Piwko Charles; Kakkavas Panagiotis; Paparouni Konstantina; Jensen Rasmus C D; Hemels Michiel E H

    2012-01-01

    Abstract Background Patients having chronic schizophrenia with frequent relapses and hospitalizations represent a great challenge, both clinically and financially. Risperidone long-acting injection (RIS-LAI) has been the main LAI atypical antipsychotic treatment in Greece. Paliperidone palmitate (PP-LAI) has recently been approved. It is dosed monthly, as opposed to biweekly for RIS-LAI, but such advantages have not yet been analysed in terms of economic evaluation. Purpose To compare costs a...

  14. Effects of Paliperidone Palmitate on Coagulation: An Experimental Study

    Yılmaz, Enver Demirel; Motor, Sedat; Pınar, Neslihan; Kokacya, Hanifi; Kisa, Mustafa; Oktar, Suleyman

    2014-01-01

    Objective. The aim of the present study was to examine the effects of a new antipsychotic drug paliperidone palmitate on hemogram and coagulation parameters in rats. Materials and Methods. Experiments were performed on 22 female albino Wistar rats (8–12 weeks old). Control group was given drinking water as vehicle (0.3 mL). PAL-1 rats were given 1 mg/kg paliperidone palmitate (in 0.3 mL drinking water) by oral gavage once a day for ten days and PAL-3 rats received 3 mg/kg paliperidone palmitate (in 0.3 mL drinking water) by oral gavage for ten days. Blood samples were drawn from the heart 24 hours after the last drug dose, and hemogram and coagulation parameters were measured with automated analyzers. Results. Hemogram did not change in the paliperidone treated groups compared to the controls. Factor VIII levels decreased in the PAL-1 and PAL-3 groups; and this decrease was significantly greater in the PAL-3. Factor IX levels decreased in PAL-3 rats, but its levels also increased in PAL-1 rats compared to the control. Discussion. Paliperidone has led to changes in the serum levels of coagulation factors VIII and IX in rats. As a result, paliperidone may be causing thromboembolism or bleeding in a dose-independent manner. PMID:24764772

  15. Effects of Paliperidone Palmitate on Coagulation: An Experimental Study

    Enver Demirel Yılmaz

    2014-01-01

    Full Text Available Objective. The aim of the present study was to examine the effects of a new antipsychotic drug paliperidone palmitate on hemogram and coagulation parameters in rats. Materials and Methods. Experiments were performed on 22 female albino Wistar rats (8–12 weeks old. Control group was given drinking water as vehicle (0.3 mL. PAL-1 rats were given 1 mg/kg paliperidone palmitate (in 0.3 mL drinking water by oral gavage once a day for ten days and PAL-3 rats received 3 mg/kg paliperidone palmitate (in 0.3 mL drinking water by oral gavage for ten days. Blood samples were drawn from the heart 24 hours after the last drug dose, and hemogram and coagulation parameters were measured with automated analyzers. Results. Hemogram did not change in the paliperidone treated groups compared to the controls. Factor VIII levels decreased in the PAL-1 and PAL-3 groups; and this decrease was significantly greater in the PAL-3. Factor IX levels decreased in PAL-3 rats, but its levels also increased in PAL-1 rats compared to the control. Discussion. Paliperidone has led to changes in the serum levels of coagulation factors VIII and IX in rats. As a result, paliperidone may be causing thromboembolism or bleeding in a dose-independent manner.

  16. Hibiscus sabdariffa polyphenols prevent palmitate-induced renal epithelial mesenchymal transition by alleviating dipeptidyl peptidase-4-mediated insulin resistance.

    Huang, Chien-Ning; Wang, Chau-Jong; Yang, Yi-Sun; Lin, Chih-Li; Peng, Chiung-Huei

    2016-01-01

    Diabetic nephropathy has a significant socioeconomic impact, but its mechanism is unclear and needs to be examined. Hibiscus sabdariffa polyphenols (HPE) inhibited high glucose-induced angiotensin II receptor-1 (AT-1), thus attenuating renal epithelial mesenchymal transition (EMT). Recently, we reported HPE inhibited dipeptidyl-peptidase-4 (DPP-4, the enzyme degrades type 1 glucagon-like peptide (GLP-1)), which mediated insulin resistance signals leading to EMT. Since free fatty acids can realistically bring about insulin resistance, using the palmitate-stimulated cell model in contrast with type 2 diabetic rats, in this study we examined if insulin resistance causes renal EMT, and the preventive effect of HPE. Our findings reveal that palmitate hindered 30% of glucose uptake. Treatment with 1 mg mL(-1) of HPE and the DPP-4 inhibitor linagliptin completely recovered insulin sensitivity and palmitate-induced signal cascades. HPE inhibited DPP-4 activity without altering the levels of DPP-4 and the GLP-1 receptor (GLP-1R). HPE decreased palmitate-induced phosphorylation of Ser307 of insulin receptor substrate-1 (pIRS-1 (S307)), AT-1 and vimentin, while increasing phosphorylation of phosphatidylinositol 3-kinase (pPI3K). IRS-1 knockdown revealed its essential role in mediating downstream AT-1 and EMT. In type 2 diabetic rats, it suggests that HPE concomitantly decreased the protein levels of DPP-4, AT-1, vimentin, and fibronectin, but reversed the in vivo compensation of GLP-1R. In conclusion, HPE improves insulin sensitivity by attenuating DPP-4 and the downstream signals, thus decreasing AT-1-mediated tubular-interstitial EMT. HPE could be an adjuvant to prevent diabetic nephropathy. PMID:26514092

  17. Formulation and evaluation of sodium ascorbyl phosphate and kojic acid containing products / Anita van Rensburg

    Van Rensburg, Anita

    2004-01-01

    The skin, our main defence against harmful substances such as wind, dirt, bacteria and ultraviolet radiation has also the important functions of preventing water loss, regulating temperature and receiving external stimuli. Skin colour varies depending on racial background, sex and the season of the year due to the exposure to sunlight. Skin colour is primarily determined by the amount of melanin produced by the melanocytes. For this reason, research for the development of white...

  18. Lauroyl/palmitoyl glycol chitosan gels enhance skin delivery of magnesium ascorbyl phosphate.

    Wang, Po-Chun; Huang, Yan-Ling; Hou, Sheng-Shu; Chou, Chen-Hsi; Tsai, Jui-Chen

    2013-01-01

    Palmitoyl glycol chitosan (GCP) hydrogel has been reported as erodible controlled-release systems for the delivery of both hydrophilic and hydrophobic molecules. In this study we prepared lauroyl/palmitoyl glycol chitosan (GCL/GCP) in gel form and evaluated their application for skin delivery of the hydrophilic compound, magnesium ascorbyl phosphate (MAP), which is widely used in cosmetic formulations. Release of MAP from the polymer gels was significantly decreased with increasing concentration of GCL/GCP in the formulations in comparison with glycol chitosan (GC). In both aqueous and 10% ethanol vehicles, MAP flux was increased 1.58- to 3.96-fold of 1% GC from 1% GCL/GCP. Increase in MAP flux was correlated to the increase in GCL/GCP concentration prepared in 10% ethanol vehicle. GCL/GCP, in either water or 10% ethanol vehicles, increased the skin penetration and skin deposition of MAP in comparison with GC, hydroxypropylmethylcellulose, and carbopol, while sustaining its release from the polymer gels. Both the enhancement in skin penetration/deposition and sustained release of MAP were depended on polymer concentration. Also, with increase in polymer concentration, epidermal to dermal drug deposition ratio tended to increase, which will be beneficial to its activity in the epidermis, such as inhibition of tyrosinase and protection from UV damage. These data suggested both GCL and GCP can be applied as delivery vehicles to improve percutaneous absorption of MAP. PMID:23931090

  19. Mechanisms of ascorbyl radical formation in human platelet-rich plasma.

    Shyu, Kou-Gi; Chang, Chao-Chien; Yeh, Yu-Chieh; Sheu, Joen-Rong; Chou, Duen-Suey

    2014-01-01

    Recently, many clinical reports have suggested that the ascorbyl free radical (Asc(∙)) can be treated as a noninvasive, reliable, real-time marker of oxidative stress, but its generation mechanisms in human blood have rarely been discussed. In this study, we used upstream substances, enzyme inhibitors, and free radical scavengers to delineate the mechanisms of Asc(∙) formation in human platelet-rich plasma (PRP). Our results show that the doublet signal was detected in PRP samples by using electron spin resonance, and the hyperfine splitting of the doublet signal was a(H) = 1.88 gauss and g-factor = 2.00627, which was determined to be the Asc(∙). We observed that the inhibitors of NADPH oxidase (NOX), cyclooxygenase (COX), lipoxygenase (LOX), cytochrome P450 (CYP450), mitochondria complex III, and nitric oxide synthase (NOS), but not xanthine oxidase, diminished the intensity of the Asc(∙) signal dose dependently. All enzyme inhibitors showed no obvious antioxidant activity during a Fenton reaction assay. In summary, the obtained data suggest that Asc(∙) formation is associated with NOX, COX, LOX, CYP450, eNOS, and mitochondria in human PRP. PMID:24696859

  20. Electronic paramagnetic resonance (EPR) for the study of ascorbyl radical and lipid radicals in marine organisms.

    González, Paula Mariela; Aguiar, María Belén; Malanga, Gabriela; Puntarulo, Susana

    2013-08-01

    Electron paramagnetic resonance (EPR) spectroscopy detects the presence of radicals of biological interest, such as ascorbyl radical (A(•)) and lipid radicals. A(•) is easily detectable by EPR even in aqueous solution at room-temperature. Under oxidative conditions leading to changes in total ascorbate (AH(-)) content, the A(•)/AH(-) ratio could be used to estimate early oxidative stress in the hydrophilic milieu. This methodology was applied to a wide range of aquatic systems including algae, sea urchin, limpets, bivalves and fish, under physiological and oxidative stress conditions as well. The A(•)/AH(-) ratio reflected the state of one part of the oxidative defense system and provided an early and simple diagnosis of environmental stressing conditions. Oxidative damage to lipids was assessed by the EPR-sensitive adduct formation that correlates well with cell membrane damage with no interference from other biological compounds. Probe instability, tissue metabolism, and lack of spin specificity are drawback factors for employing EPR for in vivo determination of free radicals. However, the dependability of this technique, mostly by combining it with other biochemical strategies, enhances the value of these procedures as contributors to the knowledge of oxidative condition in aquatic organisms. PMID:23485428

  1. Dynamic nuclear polarization-magnetic resonance imaging at low ESR irradiation frequency for ascorbyl free radicals

    Ito, Shinji; Hyodo, Fuminori

    2016-02-01

    Highly water-soluble ubiquinone-0 (CoQ0) reacts with ascorbate monoanion (Asc) to mediate the production of ascorbyl free radicals (AFR). Using aqueous reaction mixture of CoQ0 and Asc, we obtained positively enhanced dynamic nuclear polarization (DNP)-magnetic resonance (MR) images of the AFR at low frequency (ranging from 515 to 530 MHz) of electron spin resonance (ESR) irradiation. The shape of the determined DNP spectrum was similar to ESR absorption spectra with doublet spectral peaks. The relative locational relationship of spectral peaks in the DNP spectra between the AFR (520 and 525 MHz), 14N-labeled carbamoyl-PROXYL (14N-CmP) (526.5 MHz), and Oxo63 (522 MHz) was different from that in the X-band ESR spectra, but were similar to that in the 300-MHz ESR spectra. The ratio of DNP enhancement to radical concentration for the AFR was higher than those for 14N-CmP, Oxo63, and flavin semiquinone radicals. The spectroscopic DNP properties observed for the AFR were essentially the same as those for AFR mediated by pyrroloquinoline quinone. Moreover, we made a success of in vivo DNP-MR imaging of the CoQ0-mediated AFR which was administered by the subcutaneous and oral injections as an imaging probe.

  2. Mechanisms of Ascorbyl Radical Formation in Human Platelet-Rich Plasma

    Kou-Gi Shyu

    2014-01-01

    Full Text Available Recently, many clinical reports have suggested that the ascorbyl free radical (Asc∙ can be treated as a noninvasive, reliable, real-time marker of oxidative stress, but its generation mechanisms in human blood have rarely been discussed. In this study, we used upstream substances, enzyme inhibitors, and free radical scavengers to delineate the mechanisms of Asc∙ formation in human platelet-rich plasma (PRP. Our results show that the doublet signal was detected in PRP samples by using electron spin resonance, and the hyperfine splitting of the doublet signal was aH=1.88 gauss and g-factor = 2.00627, which was determined to be the Asc∙. We observed that the inhibitors of NADPH oxidase (NOX, cyclooxygenase (COX, lipoxygenase (LOX, cytochrome P450 (CYP450, mitochondria complex III, and nitric oxide synthase (NOS, but not xanthine oxidase, diminished the intensity of the Asc∙ signal dose dependently. All enzyme inhibitors showed no obvious antioxidant activity during a Fenton reaction assay. In summary, the obtained data suggest that Asc∙ formation is associated with NOX, COX, LOX, CYP450, eNOS, and mitochondria in human PRP.

  3. Assessment of penetration of Ascorbyl Tetraisopalmitate into biological membranes by molecular dynamics.

    Machado, N C F; Dos Santos, L; Carvalho, B G; Singh, P; Téllez Soto, C A; Azoia, N G; Cavaco-Paulo, A; Martin, A A; Favero, P P

    2016-08-01

    The present work, involves the simulation of the transport of a vitamin C derivative, Ascorbyl Tetraisopalmitate (ATI), through human skin by molecular dynamics. Percutaneous absorption of the ATI molecule through the infundibulum, an important route of absorption into the hair follicle of the human skin, has been modeled and compared with the stratum corneum membrane. The comparative study was done using molecular dynamics with Martini force field. In infundibulum, a single ATI molecule require more time to penetrate, and the data obtained suggested that a high concentration of ATI molecule accelerated the process of penetration. In conclusion, the ATI molecule was found to have more affinity towards the stratum corneum as compared with the infundibulum, and it followed a straight pathway to penetrate (until 600ns of simulation). In the infundibulum, it showed less affinity, more mobility and followed a lateral pathway. Thus, this work contributes to a better understanding of the different molecular interactions during percutaneous absorption of active molecules in these two different types of biological membranes. PMID:27289538

  4. 77 FR 59287 - National Organic Program (NOP); Sunset Review (2012) for Nutrient Vitamins and Minerals

    2012-09-27

    ... oil, arachidonic acid (ARA) single-cell oil, taurine, inositol, choline, ascorbyl palmitate, synthetic... organic. Arachidonic Acid (ARA) single- Yes NOSB recommended the cell oil \\b\\. addition to Sec. 205.605(a... handling should be continued (75 FR 14500).\\1\\ The ANPR indicated that the exemption for the use...

  5. Serotonin- and Dopamine-Related Gene Expression in db/db Mice Islets and in MIN6 β-Cells Treated with Palmitate and Oleate

    Cataldo, L. R.; Olmos, P.; Galgani, J. E.; Valenzuela, R.; Aranda, E.; Cortés, V. A.; Santos, J. L.

    2016-01-01

    High circulating nonesterified fatty acids (NEFAs) concentration, often reported in diabetes, leads to impaired glucose-stimulated insulin secretion (GSIS) through not yet well-defined mechanisms. Serotonin and dopamine might contribute to NEFA-dependent β-cell dysfunction, since extracellular signal of these monoamines decreases GSIS. Moreover, palmitate-treated β-cells may enhance the expression of the serotonin receptor Htr2c, affecting insulin secretion. Additionally, the expression of monoamine-oxidase type B (Maob) seems to be lower in islets from humans and mice with diabetes compared to nondiabetic islets, which may lead to increased monoamine concentrations. We assessed the expression of serotonin- and dopamine-related genes in islets from db/db and wild-type (WT) mice. In addition, the effect of palmitate and oleate on the expression of such genes, 5HT content, and GSIS in MIN6 β-cell was determined. Lower Maob expression was found in islets from db/db versus WT mice and in MIN6 β-cells in response to palmitate and oleate treatment compared to vehicle. Reduced 5HT content and impaired GSIS in response to palmitate (−25%; p < 0.0001) and oleate (−43%; p < 0.0001) were detected in MIN6 β-cells. In conclusion, known defects of GSIS in islets from db/db mice and MIN6 β-cells treated with NEFAs are accompanied by reduced Maob expression and reduced 5HT content. PMID:27366756

  6. Paliperidone palmitate use in pregnancy in a woman with schizophrenia.

    Özdemir, Aslı Karadağ; Pak, Şima Ceren; Canan, Fatih; Geçici, Ömer; Kuloğlu, Murat; Gücer, Mustafa Kadri

    2015-10-01

    Long-acting antipsychotic use in schizophrenia has become an advantage for treatment compliance and convenient administration of the drugs. There is no data on paliperidone palmitate (PP) use in pregnancy, which is the longest-acting (i.e., 1 month) atypical antipsychotic. In this case report, we aim to present a patient diagnosed with schizophrenia who had been using PP before and during her pregnancy until week 28 of gestation and gave birth to a male baby that weighed 3000 g at 39 weeks. As far as we know, this is the first case report on PP use during pregnancy. PMID:25599999

  7. Successful therapy of macrophage activation syndrome with dexamethasone palmitate.

    Nakagishi, Yasuo; Shimizu, Masaki; Kasai, Kazuko; Miyoshi, Mari; Yachie, Akihiro

    2016-07-01

    Macrophage activation syndrome (MAS) is a severe and potential life-threatening complication of childhood systemic inflammatory disorders. Corticosteroids are commonly used as the first-line therapy for MAS. We report four patients with MAS who were successfully treated with dexamethasone palmitate (DexP), a liposome-incorporated dexamethasone, much more efficient than free corticosteroids. DexP effectively inhibited inflammation in MAS patients in whom the response to pulse methylprednisolone was not sufficient to manage their diseases. DexP was also effective as the first-line therapy for MAS. Based on these findings, DexP is an effective therapy in treating MAS patients. PMID:24754272

  8. EPR characterization of ascorbyl and sulfur dioxide anion radicals trapped during the reaction of bovine Cytochrome c Oxidase with molecular oxygen

    Yu, Michelle A.; Egawa, Tsuyoshi; Yeh, Syun-Ru; Rousseau, Denis L.; Gerfen, Gary J.

    2010-04-01

    The reaction intermediates of reduced bovine Cytochrome c Oxidase (C cO) were trapped following its reaction with oxygen at 50 μs-6 ms by innovative freeze-quenching methods and studied by EPR. When the enzyme was reduced with either ascorbate or dithionite, distinct radicals were generated; X-band (9 GHz) and D-band (130 GHz) CW-EPR measurements support the assignments of these radicals to ascorbyl and sulfur dioxide anion radical ( SO2-rad ), respectively. The X-band spectra show a linewidth of 12 G for the ascorbyl radical and 11 G for the SO2-rad radical and an isotropic g-value of 2.005 for both species. The D-band spectra reveal clear distinctions in the g-tensors and powder patterns of the two species. The ascorbyl radical spectrum displays approximate axial symmetry with g-values of g x = 2.0068, g y = 2.0066, and g z = 2.0023. The SO2-rad radical has rhombic symmetry with g-values of g x = 2.0089, g y = 2.0052, and g z = 2.0017. When the contributions from the ascorbyl and SO2-rad radicals were removed, no protein-based radical on C cO could be identified in the EPR spectra.

  9. Protection from Palmitate-Induced Mitochondrial DNA Damage Prevents from Mitochondrial Oxidative Stress, Mitochondrial Dysfunction, Apoptosis, and Impaired Insulin Signaling in Rat L6 Skeletal Muscle Cells

    Yuzefovych, Larysa V.; Solodushko, Viktoriya A.; Wilson, Glenn L.; Rachek, Lyudmila I.

    2011-01-01

    Saturated free fatty acids have been implicated in the increase of oxidative stress, mitochondrial dysfunction, apoptosis, and insulin resistance seen in type 2 diabetes. The purpose of this study was to determine whether palmitate-induced mitochondrial DNA (mtDNA) damage contributed to increased oxidative stress, mitochondrial dysfunction, apoptosis, impaired insulin signaling, and reduced glucose uptake in skeletal muscle cells. Adenoviral vectors were used to deliver the DNA repair enzyme ...

  10. Preparation of Vegetable Oil Emulsions from Amylose-Sodium Palmitate Inclusion Complexes

    Aqueous dispersions of high amylose starch were steam jet cooked and blended with aqueous solutions of sodium palmitate to generate amylose sodium palmitate helical inclusion complexes. This preparative method allows sufficient quantities of these complexes to be prepared to examine their propertie...

  11. Stevioside counteracts the alpha-cell hypersecretion caused by long-term palmitate exposure

    Hong, J; Chen, L; Jeppesen, P B; Nordentoft, I; Hermansen, K

    2006-01-01

    -stimulated glucagon release by 22 and 45%, respectively (P< 0.01). There was no significant change in glucagon content after 72-h culture with palmitate and/or stevioside. Palmitate increased carnitine palmitoyltransferase I (CPT I) mRNA level, whereas stevioside enhanced CPT I, peroxisome proliferator...

  12. 78 FR 73200 - Draft Guidance for Industry on Bioequivalence Recommendations for Paliperidone Palmitate Extended...

    2013-12-05

    ... the Federal Register of June 11, 2010 (75 FR 33311), FDA announced the availability of a guidance for... Recommendations for Paliperidone Palmitate Extended-Release Injectable Suspension; Availability AGENCY: Food and... for Paliperidone Palmitate.'' The guidance provides specific recommendations on the design...

  13. Mechanism of long chain monoenoic fatty acids acting on the energy metabolism of heart

    The oxidation of 1-14C-erucic (Csub(22:1)) and 1-14C-nervonic (Csub(24:1)) acid was studied compared to 1-14C-palmitic and -oleic acid in isolated rat and pig heart mitochondria. After mitochondrial incubation with the albumin-bound fatty acids only small amounts of 14CO2 developed from the oxidation of the long chain monoenoic acids as compared to palmitic or oleic acid. The slow down of the oxidation rate was more pronounced in rat than in pig heart mitochondria. The oxidation of palmitic or oleic acid was not found to be inhibited by the C20-C24-monoeneic acids, whereas palmitic or oleic acid inhibited the oxidation of erucic acid competitively. From present findings an idea may be developed of the interference on fatty acid metabolism in heart muscle by erucic and other long chain monenoic acids. (orig.)

  14. Fatty Acid Composition of Agaricus bisporus (Lange) Sing.

    Aktümsek, Abdurrahman; ÖZTÜRK, Celâleddin; KAŞIK, Giyasettin

    1998-01-01

    Fatty acid compositions of fruit body, stem, lamellae and total of Agaricus bisporus were seperately analysed by GLC. In the all fatty acid compositions of A. bisporus, linoleic acid were predominant. Percentages of linoleic acid were varied between 53.45 - 68.78%. It was showed that the other major fatty acids were palmitic, oleic and stearic acid in the fatty acid compositions.

  15. Inhibition of uncoupling protein 2 with genipin exacerbates palmitate-induced hepatic steatosis

    Ma Shuangtao

    2012-11-01

    Full Text Available Abstract Background Uncoupling protein 2 (UCP2 was reported to be involved in lipid metabolism through regulating the production of superoxide anion. However, the role of UCP2 in hepatocytes steatosis has not been determined. We hypothesized that UCP2 might regulate hepatic steatosis via suppressing oxidative stress. Results We tested this hypothesis in an in vitro model of hepatocytic steatosis in HepG2 cell lines induced by palmitic acid (PA. We found that treatment with PA induced an obvious lipid accumulation in HepG2 cells and a significant increase in intracellular triglyceride content. Moreover, the specific inhibition of UCP2 by genipin remarkably exacerbated PA-induced hepatocytes steatosis. Interestingly, the PA-induced superoxide overproduction can also be enhanced by incubation with genipin. In addition, administration with the antioxidant tempol abolished genipin-induced increase in intracellular lipid deposition. We further found that genipin significantly increased the protein expression of fatty acid translocase (FAT/CD36. Conclusions These findings suggest that UCP2 plays a protective role in PA-induced hepatocytic steatosis through ameliorating oxidative stress.

  16. Paliperidone palmitate injection for the acute and maintenance treatment of schizophrenia in adults

    Kim, Shiyun; Solari, Hugo; Weiden, Peter J; Bishop, Jeffrey R

    2012-01-01

    Purpose To review the use of paliperidone palmitate in treatment of patients with schizophrenia. Methods Published clinical trial data for the development and utilization of paliperidone palmitate for the treatment of schizophrenia were assessed in this review. Four short-term, randomized, double-blind, placebo-controlled trials investigated the efficacy of paliperidone palmitate in acute exacerbation of schizophrenia. Paliperidone palmitate was also studied as a maintenance treatment to prevent or delay relapse in stable schizophrenia. In addition, paliperidone palmitate was compared to risperidone long-acting injection for noninferiority in three studies. Results Paliperidone palmitate has been shown to be effective in reducing symptoms as measured by the Positive and Negative Syndrome Scale total scores in the four acute treatment studies. In the maintenance treatment studies, paliperidone palmitate was found to be more effective than placebo in preventing or delaying the time to first relapse in stable schizophrenia patients. In addition, paliperidone palmitate was shown to be noninferior to risperidone long-acting injection in two studies. It was shown to be reasonably well tolerated in all clinical trials. Acute treatment phase should be initiated with a dose of 234 mg on day one and 156 mg on day eight, followed by a recommended monthly maintenance dose of 39–234 mg based on efficacy and tolerability results from the clinical studies. Conclusion Providing an optimal long-term treatment can be challenging. Paliperidone palmitate can be used as an acute treatment even in outpatient setting, and it has shown to be well tolerated by patients. Also, it does not require overlapping oral antipsychotic supplementation while being initiated, and is dosed once per month. PMID:22879739

  17. Paliperidone palmitate injection for the acute and maintenance treatment of schizophrenia in adults

    Kim S

    2012-07-01

    Full Text Available Shiyun Kim,1 Hugo Solari,2 Peter J Weiden,2 Jeffrey R Bishop11Department of Pharmacy Practice, University of Illinois at Chicago College of Pharmacy, 2Department of Psychiatry, University of Illinois at Chicago College of Medicine, Chicago, IL, USAPurpose: To review the use of paliperidone palmitate in treatment of patients with schizophrenia.Methods: Published clinical trial data for the development and utilization of paliperidone palmitate for the treatment of schizophrenia were assessed in this review. Four short-term, randomized, double-blind, placebo-controlled trials investigated the efficacy of paliperidone palmitate in acute exacerbation of schizophrenia. Paliperidone palmitate was also studied as a maintenance treatment to prevent or delay relapse in stable schizophrenia. In addition, paliperidone palmitate was compared to risperidone long-acting injection for noninferiority in three studies.Results: Paliperidone palmitate has been shown to be effective in reducing symptoms as measured by the Positive and Negative Syndrome Scale total scores in the four acute treatment studies. In the maintenance treatment studies, paliperidone palmitate was found to be more effective than placebo in preventing or delaying the time to first relapse in stable schizophrenia patients. In addition, paliperidone palmitate was shown to be noninferior to risperidone long-acting injection in two studies. It was shown to be reasonably well tolerated in all clinical trials. Acute treatment phase should be initiated with a dose of 234 mg on day one and 156 mg on day eight, followed by a recommended monthly maintenance dose of 39–234 mg based on efficacy and tolerability results from the clinical studies.Conclusion: Providing an optimal long-term treatment can be challenging. Paliperidone palmitate can be used as an acute treatment even in outpatient setting, and it has shown to be well tolerated by patients. Also, it does not require overlapping oral

  18. Amelioration of palmitate-induced metabolic dysfunction in L6 muscle cells expressing low levels of receptor-interacting protein 140.

    Constantinescu, Silvana; Turcotte, Lorraine P

    2015-11-01

    We have shown that reduced expression of receptor-interacting protein 140 (RIP140) alters the regulation of fatty-acid (FA) oxidation in muscle. To determine whether a high level of FA availability alters the effects of RIP140 on metabolic regulation, L6 myotubes were transfected with or without RNA interference oligonucleotide sequences to reduce RIP140 expression, and then incubated with high levels of palmitic acid, with or without insulin. High levels of palmitate reduced basal (53%-58%) and insulin-treated (24%-44%) FA uptake and oxidation, and increased basal glucose uptake (88%). In cells incubated with high levels of palmitate, low RIP140 increased basal FA uptake and insulin-treated FA oxidation and glucose uptake, and decreased basal glucose uptake and insulin-treated FA uptake. Under basal conditions, low RIP140 increased the mRNA content of FAT/CD36 (159%) and COX4 (61%), as well as the protein content of Nur77 (68%), whereas the mRNA expression of FGF21 (50%) was decreased, as was the protein content of CPT1b (35%) and FGF21 (44%). Under insulin-treated conditions, low RIP140 expression increased the mRNA content of MCAD (84%) and Nur77 (84%), as well as the protein content of Nur77 (23%). Thus, a low level of RIP140 restores the rates of FA uptake in the basal state, in part via a reduction in upstream insulin signaling. Our data also indicate that the protein expression of Nur77 may be modulated by RIP140 when muscle cells are metabolically challenged by high levels of palmitate. PMID:26406163

  19. A New Simple UV Spectrophotometric Determination of Paliperidone Palmitate in Tablets

    Satya.T*

    2014-01-01

    Full Text Available simple ultra violet spectrophotometric method for the analysis of paliperidone palmitate. The chemicals and reagents were prepared for DDQ and WFB methods. Paliperidone Palmitate obeys Beer’s law between the range of 0-200µg/ml. Paliperidone Palmitate chemically named as, (9RS-3-[2-[4-(6-fluoro-1,2,benzisoxazol ylpiperidin-1-yl]ethyl]-2-methyl4-oxo-6,7,8,9-tetrahydro-4H-pyridol [1,2-a] pyrimadin-9-ylhexadecanoate is an antipsychotic drug used in the treatment of schizophrenia. It works by helping to restore the balance of certain natural chemicals (neurotransmitters in the brain.

  20. A New Simple UV Spectrophotometric Determination of Paliperidone Palmitate in Tablets

    Satya.T*

    2014-01-01

    simple ultra violet spectrophotometric method for the analysis of paliperidone palmitate. The chemicals and reagents were prepared for DDQ and WFB methods. Paliperidone Palmitate obeys Beer’s law between the range of 0-200µg/ml. Paliperidone Palmitate chemically named as, (9RS)-3-[2-[4-(6-fluoro-1,2,benzisoxazol yl)piperidin-1-yl]ethyl]-2-methyl4-oxo-6,7,8,9-tetrahydro-4H-pyridol [1,2-a] pyrimadin-9-ylhexadecanoate is an antipsychotic drug used in the treatment of schizophrenia. I...

  1. Inhibitory effect of added adenosine diphosphate on palmitate oxidation in mitochondria from rat brain

    Kawamura, N.

    1986-05-01

    It is generally accepted that fatty acids are poor substrates for the oxidation in brain because plasma fatty acids do not traverse the blood-brain barrier. However, a regional difference in the barrier suggests that fatty acids are available for oxidation. Why most of fatty acids are not oxidized is not certain. For this reason, regulation of oxidation of (1-/sup 14/C)palmitate (pal) in rat brain has been studied in nonsynaptic mitochondria (mit) prepared by use of Ficoll/sucrose density gradient. The authors found two contrasting oxidations with respect to ATP concentration; Type A at 2 mM and Type B at 0.5 mM. The rate of Type A was 50% of the level of B. Type A was inhibited by high levels of L-carnitine (car) and Mg/sup 2 +/. Added ADP inhibited Type A, but stimulated B. Addition of carboxyatractyloside was stimulatory for Type A, but inhibitory for B. The rate of Type A showed a downward curvature with increasing protein concentration while that of B showed a linear relationship. Addition of NH/sub 4//sup +/ to Type A stimulated the rate and reduced the inhibitory effects of both added ADP and high levels of car. These results suggest that under the normal level of ATP, the carnitine-dependent transport of pal is inhibited (thereby resulting in the inhibition in pal oxidation) by the transport of ADP into mit mediated by the ATP-ADP translocase, but that the inhibition is not observed under the specified conditions or regions where ATP levels are low or ammonia levels are high.

  2. Inhibitory effect of added adenosine diphosphate on palmitate oxidation in mitochondria from rat brain

    It is generally accepted that fatty acids are poor substrates for the oxidation in brain because plasma fatty acids do not traverse the blood-brain barrier. However, a regional difference in the barrier suggests that fatty acids are available for oxidation. Why most of fatty acids are not oxidized is not certain. For this reason, regulation of oxidation of [1-14C]palmitate (pal) in rat brain has been studied in nonsynaptic mitochondria (mit) prepared by use of Ficoll/sucrose density gradient. The authors found two contrasting oxidations with respect to ATP concentration; Type A at 2 mM and Type B at 0.5 mM. The rate of Type A was 50% of the level of B. Type A was inhibited by high levels of L-carnitine (car) and Mg2+. Added ADP inhibited Type A, but stimulated B. Addition of carboxyatractyloside was stimulatory for Type A, but inhibitory for B. The rate of Type A showed a downward curvature with increasing protein concentration while that of B showed a linear relationship. Addition of NH4+ to Type A stimulated the rate and reduced the inhibitory effects of both added ADP and high levels of car. These results suggest that under the normal level of ATP, the carnitine-dependent transport of pal is inhibited (thereby resulting in the inhibition in pal oxidation) by the transport of ADP into mit mediated by the ATP-ADP translocase, but that the inhibition is not observed under the specified conditions or regions where ATP levels are low or ammonia levels are high

  3. Sodium orthovanadate suppresses palmitate-induced cardiomyocyte apoptosis by regulation of the JAK2/STAT3 signaling pathway.

    Liu, Jing; Fu, Hui; Chang, Fen; Wang, Jinlan; Zhang, Shangli; Caudle, Yi; Zhao, Jing; Yin, Deling

    2016-05-01

    Elevated circulatory free fatty acids (FFAs) especially saturated FFAs, such as palmitate (PA), are detrimental to the heart. However, mechanisms responsible for this phenomenon remain unknown. Here, the role of JAK2/STAT3 in PA-induced cytotoxicity was investigated in cardiomyocytes. We demonstrate that PA suppressed the JAK2/STAT3 pathway by dephosphorylation of JAK2 (Y1007/1008) and STAT3 (Y705), and thus blocked the translocation of STAT3 into the nucleus. Conversely, phosphorylation of S727, another phosphorylated site of STAT3, was increased in response to PA treatment. Pretreatment of JNK inhibitor, but not p38 MAPK inhibitor, inhibited STAT3 (S727) activation induced by PA and rescued the phosphorylation of STAT3 (Y705). The data suggested that JNK may be another upstream factor regulating STAT3, and verified the important function of P-STAT3 (Y705) in PA-induced cardiomyocyte apoptosis. Sodium orthovanadate (SOV), a protein tyrosine phosphatase inhibitor, obviously inhibited PA-induced apoptosis by restoring JAK2/STAT3 pathways. This effect was diminished by STAT3 inhibitor Stattic. Collectively, our data suggested a novel mechanism that the inhibition of JAK2/STAT3 activation was responsible for palmitic lipotoxicity and SOV may act as a potential therapeutic agent by targeting JAK2/STAT3 in lipotoxic cardiomyopathy treatment. PMID:26921179

  4. Lipase-catalyzed synthesis of L-ascorbyl octanoate in non-aqueous phase and its structural characterization%非水相酶促合成L-抗坏血酸辛酸酯及其结构表征

    张淑青; 潘丽军; 姜绍通; 操丽丽

    2015-01-01

    L-ascorbyl octanoate was synthesized through lipase-catalyzed esterification in organic sys-tem with mid-chain fatty acid n-octanoic acid as acyl donor. The reaction parameters that highly influ-enced the conversion rate of L-ascorbic acid were selected as main variables to design the response sur-face experiment on the basis of preliminary experiments, then a regression model was established and the optimal synthesis conditions were obtained. The results indicated that reaction time, reaction tempera-ture, interaction between reaction time and reaction temperature and interaction between reaction time and substrate concentration had significant effects on the conversion rate of L-ascorbic acid ( p<0 . 05 ) , and the regression model could be used to predict the conversion rate of L-ascorbic acid. The optimal enzymatic synthesis conditions of L-ascorbyl octanoate were obtained as follows:reaction time 11. 45 h, substrate(L-ascorbic acid) concentration 0. 24 mol/L, reaction temperature 55. 3℃, dosage of lipase ( based on the mass of L-ascorbic acid) 19. 18%. Under these conditions,the conversion rate of L-ascor-bic acid reached 83. 31%. In addition, the product was characterized by IR, MS, 1 H NMR and 13 C NMR, and the result showed that n-octanoic acid was introduced into the sixth hydroxyl of L-ascorbic acid.%以中链脂肪酸正辛酸为酰基供体,在有机相体系中利用脂肪酶催化酯化反应合成L-抗坏血酸辛酸酯。根据初步试验结果,选取对L-抗坏血酸酯化转化率影响显著的因素,进行响应面试验设计,建立回归模型,得到最优参数组合。结果表明:反应时间、反应温度、反应时间和反应温度的交互作用以及反应时间和底物浓度的交互作用对 L -抗坏血酸酯化转化率均有显著影响(p <0.05),回归模型可用。 L-抗坏血酸辛酸酯酶法合成最优工艺条件为反应时间11.45 h、底物(L-抗坏血酸)浓度0.24 mol/L、反应温度55.3℃、脂

  5. Anti-inflammatory and antifibrotic effects of methyl palmitate

    Methyl palmitate (MP) has been shown earlier to inhibit Kupffer cells and rat peritoneal macrophages. To evaluate the potential of MP to inhibit the activation of other macrophages, RAW cells (macrophages of alveolar origin) were treated with varying concentrations of MP (0.25, 0.5, 1 mM). Assessment of cytotoxicity using MTT assay revealed that 0.25 and 0.5 mM are not toxic to RAW cells. MP was able to inhibit the phagocytic function of RAW cells. Treatment of cells with MP 24 hours prior to LPS stimulation significantly decreased nitric oxide release and altered the pattern of cytokines release; there was a significant decrease in TNF-α and a significant increase in IL-10 compared to the controls. However, there is a non-significant change in IL-6 level. Furthermore, phosphorylation of inhibitory kappa B (IκBα) protein was significantly decreased in RAW cells treated with 0.5 mM MP after LPS stimulation. Based upon the in-vitro results, it was examined whether MP treatment will be effective in preventing bleomycin-induced lung inflammation and fibrosis in-vivo. Bleomycin given by itself caused destruction of the lung architecture characterized by pulmonary fibrosis with collapse of air alveoli and emphysematous. Bleomycin induced a significant increase in hydroxyproline level and activated NF-κB, p65 expression in the lung. MP co-treatment significantly ameliorated bleomycin effects. These results suggest that MP has a potential of inhibiting macrophages in general. The present study demonstrated for the first time that MP has anti-inflammatory and antifibrotic effect that could be through NF-kB inhibition. Thus MP like molecule could be a promising anti-inflammatory and antifibrotic drug. - Research highlights: →Methyl palmitate is a universal macrophage inhibitor. →It could be a promising nucleus of anti-inflammatory and antifibrotic drugs. →The underlying mechanism of these effects could be through NF-kB inhibition.

  6. Berberine treatment attenuates the palmitate-mediated inhibition of glucose uptake and consumption through increased 1,2,3-triacyl-sn-glycerol synthesis and accumulation in H9c2 cardiomyocytes.

    Chang, Wenguang; Chen, Li; Hatch, Grant M

    2016-04-01

    Dysfunction of lipid metabolism and accumulation of 1,2-diacyl-sn-glycerol (DAG) may be a key factor in the development of insulin resistance in type 2 diabetes. Berberine (BBR) is an isoquinoline alkaloid extract that has shown promise as a hypoglycemic agent in the management of diabetes in animal and human studies. However, its mechanism of action is not well understood. To determine the effect of BBR on lipid synthesis and its relationship to insulin resistance in H9c2 cardiomyocytes, we measured neutral lipid and phospholipid synthesis and their relationship to glucose uptake. Compared with controls, BBR treatment stimulated 2-[1,2-(3)H(N)]deoxy-D-glucose uptake and consumption in palmitate-mediated insulin resistant H9c2 cells. The mechanism was though an increase in protein kinase B (AKT) activity and GLUT-4 glucose transporter expression. DAG accumulated in palmitate-mediated insulin resistant H9c2 cells and treatment with BBR reduced this DAG accumulation and increased accumulation of 1,2,3-triacyl-sn-glycerol (TAG) compared to controls. Treatment of palmitate-mediated insulin resistant H9c2 cells with BBR increased [1,3-(3)H]glycerol and [1-(14)C]glucose incorporation into TAG and reduced their incorporation into DAG compared to control. In addition, BBR treatment of these cells increased [1-(14)C]palmitic acid incorporation into TAG and decreased its incorporation into DAG compared to controls. BBR treatment did not alter phosphatidylcholine or phosphatidylethanolamine synthesis. The mechanism for the BBR-mediated decreased precursor incorporation into DAG and increased incorporation into TAG in palmitate-incubated cells was an increase in DAG acyltransferase-2 activity and its expression and a decrease in TAG hydrolysis. Thus, BBR treatment attenuates palmitate-induced reduction in glucose uptake and consumption, in part, through reduction in cellular DAG levels and accumulation of TAG in H9c2 cells. PMID:26774040

  7. Manic Symptoms during a Switch from Paliperidone ER to Paliperidone Palmitate in a Patient with Schizophrenia

    Demirci, Kadir; Keleş, Süleyman; Demirdaş, Arif; Korucu, Cafer Çağrı

    2015-01-01

    Some antipsychotic drugs have treatment efficacy for mania and bipolar disorder. However, these drugs may rarely cause manic symptoms in some schizophrenic patients. We hereby report a 22-year-old female patient with schizophrenia who experienced a manic episode during a switch from paliperidone ER to paliperidone palmitate. This case is an important reminder that an abrupt switch from oral paliperidone to paliperidone palmitate may predispose certain patients to hypomanic or manic symptoms. PMID:26539300

  8. Paliperidone palmitate injection for the acute and maintenance treatment of schizophrenia in adults

    Bishop, Jeffrey

    2012-01-01

    Shiyun Kim,1 Hugo Solari,2 Peter J Weiden,2 Jeffrey R Bishop11Department of Pharmacy Practice, University of Illinois at Chicago College of Pharmacy, 2Department of Psychiatry, University of Illinois at Chicago College of Medicine, Chicago, IL, USAPurpose: To review the use of paliperidone palmitate in treatment of patients with schizophrenia.Methods: Published clinical trial data for the development and utilization of paliperidone palmitate for the treatment of schizophrenia were assessed in...

  9. Manic Symptoms during a Switch from Paliperidone ER to Paliperidone Palmitate in a Patient with Schizophrenia

    Kadir Demirci; Süleyman Keleş; Arif Demirdaş; Cafer Çağrı Korucu

    2015-01-01

    Some antipsychotic drugs have treatment efficacy for mania and bipolar disorder. However, these drugs may rarely cause manic symptoms in some schizophrenic patients. We hereby report a 22-year-old female patient with schizophrenia who experienced a manic episode during a switch from paliperidone ER to paliperidone palmitate. This case is an important reminder that an abrupt switch from oral paliperidone to paliperidone palmitate may predispose certain patients to hypomanic or manic symptoms.

  10. Manic Symptoms during a Switch from Paliperidone ER to Paliperidone Palmitate in a Patient with Schizophrenia

    Kadir Demirci

    2015-01-01

    Full Text Available Some antipsychotic drugs have treatment efficacy for mania and bipolar disorder. However, these drugs may rarely cause manic symptoms in some schizophrenic patients. We hereby report a 22-year-old female patient with schizophrenia who experienced a manic episode during a switch from paliperidone ER to paliperidone palmitate. This case is an important reminder that an abrupt switch from oral paliperidone to paliperidone palmitate may predispose certain patients to hypomanic or manic symptoms.

  11. Comparative Evaluation of Diagnostic Tools for Oxidative Deterioration of Polyunsaturated Fatty Acid-Enriched Infant Formulas during Storage

    Caroline Siefarth

    2013-12-01

    than achievable via conventional methods. In detail, oxidative variances between the formulations revealed that lipid oxidation was low when copper was administered in an encapsulated form and when antioxidants (vitamin E, ascorbyl palmitate were present.

  12. The Production of Nitric Oxide, IL-6, and TNF-Alpha in Palmitate-Stimulated PBMNCs Is Enhanced through Hyperglycemia in Diabetes

    Caroline Maria Oliveira Volpe

    2014-01-01

    Full Text Available We examined nitric oxide (NO, IL-6, and TNF-α secretion from cultured palmitate-stimulated PBMNCs or in the plasma from type 2 diabetes mellitus (T2MD patients or nondiabetic (ND controls. Free fatty acids (FFA have been suggested to induce chronic low-grade inflammation, activate the innate immune system, and cause deleterious effects on vascular cells and other tissues through inflammatory processes. The levels of NO, IL-6, TNF-α, and MDA were higher in supernatant of palmitate stimulated blood cells (PBMNC or from plasma from patients. The results obtained in the present study demonstrated that hyperglycemia in diabetes exacerbates in vitro inflammatory responses in PBMNCs stimulated with high levels of SFA (palmitate. These results suggest that hyperglycemia primes PBMNCs for NO, IL-6, and TNF-alpha secretion under in vitro FFA stimulation are associated with the secretion of inflammatory biomarkers in diabetes. A combined therapy targeting signaling pathways activated by hyperglycemia in conjunction with simultaneous control of hyperglycemia and hypertriglyceridemia would be suggested for controlling the progress of diabetic complications.

  13. Autocrine effects of transgenic resistin reduce palmitate and glucose oxidation in brown adipose tissue.

    Pravenec, Michal; Mlejnek, Petr; Zídek, Václav; Landa, Vladimír; Šimáková, Miroslava; Šilhavý, Jan; Strnad, Hynek; Eigner, Sebastian; Eigner Henke, Kateřina; Škop, Vojtěch; Malínská, Hana; Trnovská, Jaroslava; Kazdová, Ludmila; Drahota, Zdeněk; Mráček, Tomáš; Houštěk, Josef

    2016-06-01

    Resistin has been originally identified as an adipokine that links obesity to insulin resistance in mice. In our previous studies in spontaneously hypertensive rats (SHR) expressing a nonsecreted form of mouse resistin (Retn) transgene specifically in adipose tissue (SHR-Retn), we have observed an increased lipolysis and serum free fatty acids, ectopic fat accumulation in muscles, and insulin resistance. Recently, brown adipose tissue (BAT) has been suggested to play an important role in the pathogenesis of metabolic disturbances. In the current study, we have analyzed autocrine effects of transgenic resistin on BAT glucose and lipid metabolism and mitochondrial function in the SHR-Retn vs. nontransgenic SHR controls. We observed that interscapular BAT isolated from SHR-Retn transgenic rats compared with SHR controls showed a lower relative weight (0.71 ± 0.05 vs. 0.91 ± 0.08 g/100 g body wt, P < 0.05), significantly reduced both basal and insulin stimulated incorporation of palmitate into BAT lipids (658 ± 50 vs. 856 ± 45 and 864 ± 47 vs. 1,086 ± 35 nmol/g/2 h, P ≤ 0.01, respectively), and significantly decreased palmitate oxidation (37.6 ± 4.5 vs. 57 ± 4.1 nmol/g/2 h, P = 0.007) and glucose oxidation (277 ± 34 vs. 458 ± 38 nmol/g/2 h, P = 0.001). In addition, in vivo microPET imaging revealed significantly reduced (18)F-FDG uptake in BAT induced by exposure to cold in SHR-Retn vs. control SHR (232 ± 19 vs. 334 ± 22 kBq/ml, P < 0.05). Gene expression profiles in BAT identified differentially expressed genes involved in skeletal muscle and connective tissue development, inflammation and MAPK and insulin signaling. These results provide evidence that autocrine effects of resistin attenuate differentiation and activity of BAT and thus may play a role in the pathogenesis of insulin resistance in the rat. PMID:27113533

  14. Retinyl palmitate polymeric nanocapsules as carriers of bioactives.

    Teixeira, Zaine; Dreiss, Cécile A; Lawrence, M J; Heenan, Richard K; Machado, Daisy; Justo, Giselle Z; Guterres, Sílvia S; Durán, Nelson

    2012-09-15

    Nanocapsules containing poly(d,l-lactide) shell and retinyl palmitate core have been prepared by the pre-formed polymer interfacial deposition method. Dynamic light scattering measurements yielded an average hydrodynamic diameter of ∼220nm and a polydispersity index of ∼0.12. Small-angle neutron scattering experiments revealed the presence of two populations of nanocapsules of core diameters ∼192 and 65nm. Freeze fracture transmission electron microscopy showed a polydisperse population of nanocapsules (NC), with a poly(d,l-lactide) shell thickness between 11 and 3nm. For comparison purposes, nanoemulsions (NE, no polymer) and nanospheres (NS, polymer matrix) were also prepared. Each type of nanoparticles exhibited a different morphology (when examined by electron microscopy), in particular NC showed deformability by capillary adhesion. All three types of nanoparticles successfully encapsulated the poorly water-soluble molecules baicalein and benzophenone-3. The thermal behavior of the various nanoparticles was different to a physical mixture of its individual components. Cytotoxicity and phototoxicity assays, performed in human keratinocytes (HaCaT) and murine fibroblasts (BALB/c 3T3), showed that the NC were only cytotoxic at high concentrations. In vitro release studies of benzophenone-3, by the dialysis bag method using NC and NS, showed a sustained release; however, permeation studies using plastic surgery human abdominal skin in Franz diffusion cells showed that a higher amount of benzophenone-3 from NC penetrated into the skin, most probably due to the deformable nature of these nanoparticles. PMID:22738849

  15. Paliperidone Palmitate-induced Urinary Incontinence: A Case Report.

    Karslıoǧlu, Ersin Hatice; Özalp, Elvan; Çayköylü, Ali

    2016-02-29

    Urinary incontinence, although rarely reported, is one of the most important adverse effects of antipsychotic medication. It can be an embarrassing, distressing, and potentially treatment-limiting. Several antipsychotics, including both typical and atypical varieties, are known to induce urinary incontinence. Many antipsychotic drugs target the neural pathways controlling continence by binding to receptors of some neurotransmitters such as serotonin, dopamine, acetylcholine, and adrenaline. Pharmacological management of incontinence should be considered if there is a risk of cessation of the antipsychotic therapy or any decline in patients' compliance. Amitriptyline, desmopressin, ephedrine, and anticholinergics such as oxybutynin and trihexyphenidyl are the most frequently used agents to treat incontinence. We think that the frequency of incontinence is higher than reported in the literature, and that follow-up routines should include a form of standardized screening for all possible adverse effects, including incontinence, of any given antipsychotic. In this article, we report a case of urinary incontinence as an adverse effect of paliperidone palmitate use during maintenance therapy in a patient with schizophrenia. PMID:26792046

  16. Tea Flavanols Block Advanced Glycation of Lens Crystallins Induced by Dehydroascorbic Acid.

    Zhu, Yingdong; Zhao, Yantao; Wang, Pei; Ahmedna, Mohamed; Ho, Chi-Tang; Sang, Shengmin

    2015-01-20

    Growing evidence has shown that ascorbic acid (ASA) can contribute to protein glycation and the formation of advanced glycation end products (AGEs), especially in the lens. The mechanism by which ascorbic acid can cause protein glycation probably originates from its oxidized form, dehydroascorbic acid (DASA), which is a reactive dicarbonyl species. In the present study, we demonstrated for the first time that four tea flavanols, (-)-epigallocatechin 3-O-gallate (EGCG), (-)-epigallocatechin (EGC), (-)-epicatechin 3-O-gallate (ECG), and (-)-epicatechin (EC), could significantly trap DASA and consequently form 6C- or 8C-ascorbyl conjugates. Among these four flavanols, EGCG exerted the strongest trapping efficacy by capturing approximate 80% of DASA within 60 min. We successfully purified and identified seven 6C- or 8C-ascorbyl conjugates of flavanols from the chemical reaction between tea flavanols and DASA under slightly basic conditions. Of which, five ascorbyl conjugates, EGCGDASA-2, EGCDASA-2, ECGDASA-1, ECGDASA-2 and ECDASA-1, were recognized as novel compounds. The NMR data showed that positions 6 and 8 of the ring A of flavanols were the major active sites for trapping DASA. We further demonstrated that tea flavanols could effectively inhibit the formation of DASA-induced AGEs via trapping DASA in the bovine lens crystallin-DASA assay. In this assay, 8C-ascorbyl conjugates of flavanols were detected as the major adducts using LC-MS. This study suggests that daily consumption of beverages containing tea flavanols may prevent protein glycation in the lens induced by ascorbic acid and its oxidized products. PMID:25437149

  17. Effect of L-ascorbyl Palmitate on the Stability of Frying Oil%L-抗坏血酸棕榈酸酯在煎炸油中应用研究

    何松; 林富强; 陈永恒

    2010-01-01

    油炸食品用油随着煎炸时间的延长,油脂的品质逐渐劣变,其对人体的健康存在危害.由L-抗坏血酸棕榈酸酯复配而成的复合稳定剂,能明显延长煎炸用油的使用寿命,效果好于其他单体抗氧化剂.

  18. 非水相中脂肪酶催化合成L-抗坏血酸棕榈酸酯%Lipase-catalyzed synthesis of L-ascorbyl palmitate in non-aqueous medium

    姜新慧; 晏日安; 曾永青

    2010-01-01

    研究了洋葱伯克霍尔德菌脂肪酶在非水相中催化合成L-抗坏血酸棕榈酸酯(L-AP).酶用量固定为L-抗坏血酸质量的18.7%,底物L-抗坏血酸与棕榈酸的摩尔比限定在1:2,对影响酶催化合成的因素如溶剂、反应时间、温度、棕榈酸浓度、分子筛用量和摇床转速进行研究.L-AP的最佳合成条件:6.08 mmol L-抗坏血酸、12.19 mmol棕榈酸,0.20 g脂肪酶,40 mL叔丁醇,4A分子筛用量4 g,恒温55℃,摇床转速为150 r/min,反应时间48 h,L-AP产率达87.6%.电动搅拌下酶催化合成L-AP,酶重复使用10次,最高产率为89.5%.

  19. 非水相酶促L-抗坏血酸棕榈酸酯合成的动力学%Kinetic Study on Lipase Catalyzed Synthesis of L-ascorbyl Palmitate in 2-methyl-2-butanol

    汤鲁宏; 张浩; 孙云飞

    2000-01-01

    对叔戊醇中酶法合成L-抗坏血酸棕榈酸酯(L-AP)的反应动力学进行了研究,对影响其反应动力学的因素(转速、温度、水分活度、酶质量分数和底物浓度)进行了探讨,确定了最有效的酶促反应环境.即转速为200 r/min,温度为55 ℃,水分活度为0,加酶量为20%.并对底物进行了比较,得到了对酶亲和力最大的底物--棕榈酸甲酯.

  20. 食用油中L-抗坏血酸棕榈酸酯含量测定方法研究%A Determination Method of Ascorbyl Palmitate in Edible Oil

    黄少强; 刘志同

    2006-01-01

    研究了直接滴定法测定食用油中L-抗坏血酸棕榈酸酯的方法.用甲醇对油样中L-抗坏血酸棕榈酸酯进行提取,对提取物在酸性条件下水解,用水解产物对2,6-二氯酚靛酚钠溶液进行滴定.该方法灵敏性高、准确可靠.

  1. The Determination of L-ascorbyl Palmitate in Cosmetic by Thin Layer Chromatography Fluorometry%化妆品中L-抗坏血酸棕榈酸酯的薄层色谱分析

    胡波年; 谢华林; 胡汉祥; 李爱阳

    2004-01-01

    应用荧光薄层扫描法测定了化妆品中L-抗坏血酸棕榈酸酯(AP)的含量.选用高效硅胶G薄层板,以三氯甲烷-甲醇-乙酸-水(体积比:80∶20∶8∶2)为展开剂,激发波长λ=365 nm,AP在1.0~16.0 μg范围内呈良好的线性关系,回收率为96.4%~105.0%,RSD(相对标准偏差)=1.31%,该法简单、灵敏、结果准确、重现性好,明显优于目前的其它各种分析方法,可用于化妆品的质量控制.

  2. Spectrophotometric Determination of L-Ascorbyl Palmitate with Silicamolybdenum Heteropoly Blue%硅钼兰分光光度法测定微量L-抗坏血酸棕榈酸酯

    汤鲁宏; 张浩

    2000-01-01

    论证了硅钼杂多兰反应在有机介质中进行的可行性,研究了L-抗坏血酸棕榈酸酯(L-AP)在有机介质中对硅钼杂多兰形成的影响,优选了测定条件,建立了测定其含量的硅钼兰分光光度法.该法显色体系的最大吸收波长在720nm,检测范围为0.25-2.0mg/50ml,相对标准偏差为0.43%,回收率为99.4%~100.4%.

  3. L-抗坏血酸-6-榈酸脂的抗氧化性及其合成%Antioxidation and Preparation of L-ascorbyl 6-palmitate

    孙涛; 赵红丽; 王大力; 琚行松

    2005-01-01

    L-抗坏血酸-6-棕榈酸脂是一种新型的脂溶性抗氧化剂,因其具有安全、高效、无毒的特点,所以受到普遍关注.本文对L-抗坏血酸-6-棕榈酸脂的功能、合成等方面进行了综述.

  4. Selection of Suitable Reaction Media and Lipase:Synthesize of L-ascorbyl Palmitate Catalyzed by Lipase%催化合成L-抗坏血酸棕榈酸酯的反应媒体和脂肪酶

    汤鲁宏; 张浩

    2000-01-01

    对水、庚烷和叔戊醇等几种反应媒体和NOVO435(Candida antartica), MML(Mucor miehei), LIPOLASE , PPL(Porcine pancreas)等数种脂肪酶对L-抗坏血酸棕榈酸酯合成反应的影响进行了系统的研究.结果表明,反应媒体及脂肪酶品种对反应影响极大.所研究的几种反应媒体中,叔戊醇是唯一适用于该反应的反应媒体.在所研究的几种脂肪酶中,NOVO 435表现出了良好的催化活性;MML也有一定活性,但不如NOVO 435,其相对活力只有NOVO 435的20%,其余酶种则无催化活性.

  5. Study on Synthesis Technology of L-ascorbyl-2-phosphate-6-palmitate%L-抗坏血酸-2-磷酸-6-棕榈酸酯的合成工艺研究

    刘建平; 欧阳克氙; 罗晓燕; 蔡力创; 郭雄昌

    2013-01-01

    以L-抗坏血酸-2-磷酸酯和棕榈酰氯为原料,DMAP为催化剂,酰氯化法合成L、抗坏血酸-2-磷酸石-棕榈酸酯.研究了L-抗坏血酸-2-磷酸酯与棕榈酰氯的摩尔比、反应温度、反应时间等工艺条件对收率的影响.工艺条件优化后,收率达到85%.

  6. Pharmacoeconomic analysis of paliperidone palmitate for treating schizophrenia in Greece

    2012-01-01

    Background Patients having chronic schizophrenia with frequent relapses and hospitalizations represent a great challenge, both clinically and financially. Risperidone long-acting injection (RIS-LAI) has been the main LAI atypical antipsychotic treatment in Greece. Paliperidone palmitate (PP-LAI) has recently been approved. It is dosed monthly, as opposed to biweekly for RIS-LAI, but such advantages have not yet been analysed in terms of economic evaluation. Purpose To compare costs and outcomes of PP-LAI versus RIS-LAI in Greece. Methods A cost-utility analysis was performed using a previously validated decision tree to model clinical pathways and costs over 1 year for stable patients started on either medication. Rates were taken from the literature. A local expert panel provided feedback on treatment patterns. All direct costs incurred by the national healthcare system were obtained from the literature and standard price lists; all were inflated to 2011 costs. Patient outcomes analyzed included average days with stable disease, numbers of hospitalizations, emergency room visits, and quality-adjusted life-years (QALYs). Results The total annual healthcare cost with PP-LAI was €3529; patients experienced 325 days in remission and 0.840 QALY; 28% were hospitalized and 15% received emergency room treatment. With RIS-LAI, the cost was €3695, patients experienced 318.6 days in remission and 0.815 QALY; 33% were hospitalized and 17% received emergency room treatment. Thus, PP-LAI dominated RIS-LAI. Results were generally robust in sensitivity analyses with PP-LAI dominating in 74.6% of simulations. Results were sensitive to the price of PP-LAI. Conclusions PP-LAI appears to be a cost-effective option for treating chronic schizophrenia in Greece compared with RIS-LAI since it results in savings to the health care system along with better patient outcomes. PMID:22747533

  7. Pharmacoeconomic analysis of paliperidone palmitate for treating schizophrenia in Greece

    Einarson Thomas R

    2012-07-01

    Full Text Available Abstract Background Patients having chronic schizophrenia with frequent relapses and hospitalizations represent a great challenge, both clinically and financially. Risperidone long-acting injection (RIS-LAI has been the main LAI atypical antipsychotic treatment in Greece. Paliperidone palmitate (PP-LAI has recently been approved. It is dosed monthly, as opposed to biweekly for RIS-LAI, but such advantages have not yet been analysed in terms of economic evaluation. Purpose To compare costs and outcomes of PP-LAI versus RIS-LAI in Greece. Methods A cost-utility analysis was performed using a previously validated decision tree to model clinical pathways and costs over 1 year for stable patients started on either medication. Rates were taken from the literature. A local expert panel provided feedback on treatment patterns. All direct costs incurred by the national healthcare system were obtained from the literature and standard price lists; all were inflated to 2011 costs. Patient outcomes analyzed included average days with stable disease, numbers of hospitalizations, emergency room visits, and quality-adjusted life-years (QALYs. Results The total annual healthcare cost with PP-LAI was €3529; patients experienced 325 days in remission and 0.840 QALY; 28% were hospitalized and 15% received emergency room treatment. With RIS-LAI, the cost was €3695, patients experienced 318.6 days in remission and 0.815 QALY; 33% were hospitalized and 17% received emergency room treatment. Thus, PP-LAI dominated RIS-LAI. Results were generally robust in sensitivity analyses with PP-LAI dominating in 74.6% of simulations. Results were sensitive to the price of PP-LAI. Conclusions PP-LAI appears to be a cost-effective option for treating chronic schizophrenia in Greece compared with RIS-LAI since it results in savings to the health care system along with better patient outcomes.

  8. Trimetazidine prevents palmitate-induced mitochondrial fission and dysfunction in cultured cardiomyocytes.

    Kuzmicic, Jovan; Parra, Valentina; Verdejo, Hugo E; López-Crisosto, Camila; Chiong, Mario; García, Lorena; Jensen, Michael D; Bernlohr, David A; Castro, Pablo F; Lavandero, Sergio

    2014-10-01

    Metabolic and cardiovascular disease patients have increased plasma levels of lipids and, specifically, of palmitate, which can be toxic for several tissues. Trimetazidine (TMZ), a partial inhibitor of lipid oxidation, has been proposed as a metabolic modulator for several cardiovascular pathologies. However, its mechanism of action is controversial. Given the fact that TMZ is able to alter mitochondrial metabolism, we evaluated the protective role of TMZ on mitochondrial morphology and function in an in vitro model of lipotoxicity induced by palmitate. We treated cultured rat cardiomyocytes with BSA-conjugated palmitate (25 nM free), TMZ (0.1-100 μM), or a combination of both. We evaluated mitochondrial morphology and lipid accumulation by confocal fluorescence microscopy, parameters of mitochondrial metabolism (mitochondrial membrane potential, oxygen consumption rate [OCR], and ATP levels), and ceramide production by mass spectrometry and indirect immunofluorescence. Palmitate promoted mitochondrial fission evidenced by a decrease in mitochondrial volume (50%) and an increase in the number of mitochondria per cell (80%), whereas TMZ increased mitochondrial volume (39%), and decreased mitochondrial number (56%), suggesting mitochondrial fusion. Palmitate also decreased mitochondrial metabolism (ATP levels and OCR), while TMZ potentiated all the metabolic parameters assessed. Moreover, pretreatment with TMZ protected the cardiomyocytes from palmitate-induced mitochondrial fission and dysfunction. TMZ also increased lipid accumulation in cardiomyocytes, and prevented palmitate-induced ceramide production. Our data show that TMZ protects cardiomyocytes by changing intracellular lipid management. Thus, the beneficial effects of TMZ on patients with different cardiovascular pathologies can be related to modulation of the mitochondrial morphology and function. PMID:25091560

  9. An automated SPE-based high-yield synthesis of [11C]acetate and [11C]palmitate: no liquid–liquid extraction, solvent evaporation or distillation required

    Introduction: An automated method is described for the rapid and high-yield synthesis of two of the most commonly used radioactive fatty acids: [11C]acetate and [11C]palmitate. Methods: Reaction of [11C]CO2 with the respective Grignard reagents in diethyl ether solution proceeded for 2 min at 40°C. Quenching of the reaction and liberation of nonreacted [11C]CO2 occurred upon addition of a fourfold molar excess of aqueous 0.1 M HCl (acetate) or nonaqueous HCl/Et2O (palmitate). Labeled products were then purified by adsorption to an Alumina-N Sep-Pak Plus cartridge and eluted with either aqueous NaH2PO4 solution (acetate) or 100% ethanol (palmitate). Results: High-performance liquid chromatography analysis confirmed that the radiochemical purity of each product was >98%, and decay-corrected radiochemical yields averaged 33% for [11C]palmitate and 40% for [11C]acetate. Conclusion: The method requires no liquid–liquid extraction, solvent evaporation or distillation capabilities and can be readily adapted to existing radiosynthesis modules.

  10. Uncoupling effect of fatty acids on heart muscle mitochondria and submitochondrial particles.

    Dedukhova, V I; Mokhova, E N; Skulachev, V P; Starkov, A A; Arrigoni-Martelli, E; Bobyleva, V A

    1991-12-16

    The effect of ATP/ADP-antiporter inhibitors on palmitate-induced uncoupling was studied in heart muscle mitochondria and inside-out submitochondrial particles. In both systems palmitate is found to decrease the respiration-generated membrane potential. In mitochondria, this effect is specifically abolished by carboxyatractylate (CAtr) a non-penetrating inhibitor of antiporter. In submitochondrial particles, CAtr does not abolish the palmitate-induced potential decrease. At the same time, bongkrekic acid, a penetrating inhibitor of the antiporter, suppresses the palmitate effect on the potential both in mitochondria and particles. Palmitoyl-CoA which is known to inhibit the antiporter in mitochondria as well as in particles decreases the palmitate uncoupling efficiency in both these systems. These data are in agreement with the hypothesis that the ATP/ADP-antiporter is involved in the action of free fatty acids as natural uncouplers of oxidative phosphorylation. PMID:1765167

  11. Effect of 6 dietary fatty acids on the postprandial lipid profile, plasma fatty acids, lipoprotein lipase, and cholesterol ester transfer activities in healthy young men

    Tholstrup, T.; Sandstrøm, B.; Bysted, Anette;

    2001-01-01

    , plasma fatty acids, and preheparin lipoprotein lipase and cholesterol ester transfer protein (CETP) activities. Design: Six test fats high (approximate to 43% by wt) in stearic acid, palmitic acid, palmitic + myristic acid, oleic acid, elaidic acid (trans 18:1), and linoleic acid were produced by......Background: There is increasing evidence that postprandial triacylglycerol-rich lipoproteins may be related to atherogenic risk. Objective: The objective was to investigate the effect of individual fatty acid intakes on postprandial plasma lipoprotein triacylglycerol and cholesterol concentrations...... to the test-fat meals were observed for plasma lipoprotein triacylglycerol and cholesterol concentrations, plasma fatty acid concentrations, and lipoprotein lipase and CETP activities (diet x time interaction: 0.001

    acids stearic and palmitic acids...

  12. Efficacy of transdermal magnesium ascorbyl phosphate delivery after ultrasound treatment with microbubbles in gel-type surrounding medium in mice.

    Liao, Ai-Ho; Lu, Ying-Jui; Hung, Chi-Ray; Yang, Meng-Yu

    2016-04-01

    Liquid microemulsions appropriate for topical application were obtained by increasing their viscosity through the addition of thickening agents. The present study first assessed the usefulness of ultrasound (US) plus US contrast agent, microbubbles (MBs), in agarose gel for enhancing transdermal drug delivery. The effect of US plus MBs in agarose gel on the penetration of the skin by magnesium ascorbyl phosphate (MAP) was explored both in vitro and in vivo. In the in vitro experiments, the stability of MBs was investigated by examining the penetration of MAP by the model drug, Evans blue, in two media: an agarose phantom and pig skin. The penetration depth in the agarose phantom and pig skin increased by 40% and 195%, respectively, when treated with US plus MBs in 0.1% agarose solution combined with MAP (UMB1), and by 48% and 206%, respectively, when treated with US plus MBs in 0.15% agarose solution and MAP (UMB2). The skin-whitening effects in C57BL/6J mice in the UMB1 and UMB2 groups over a 4-week experimental period were significantly increased by 63% and 70%, respectively, in the fourth week. The findings of this study suggest that the survival of MBs with US is affected by the viscosity of the surrounding medium, and that in mice, treatment with US plus MBs in a suitable agarose gel can increase skin permeability and enhance transdermal MAP delivery. PMID:26838887

  13. Alpha-synuclein gene deletion decreases brain palmitate uptake and alters the palmitate metabolism in the absence of alpha-synuclein palmitate binding

    Golovko, Mikhail Y; Færgeman, Nils J.; Cole, Nelson B;

    2005-01-01

    Alpha-synuclein is an abundant protein in the central nervous system that is associated with a number of neurodegenerative disorders, including Parkinson's disease. Its physiological function is poorly understood, although recently it was proposed to function as a fatty acid binding protein. To b....... Thus, alpha-synuclein has effects on 16:0 uptake and metabolism similar to those of an FABP, but unlike FABP, it does not directly bind 16:0; hence, the mechanism underlying these effects is different from that of a classical FABP....

  14. Interaction of the 2,6-dimethoxysemiquinone and ascorbyl free radicals with Ehrlich ascites cells: a probe of cell-surface charge.

    Pethig, R; Gascoyne, P R; McLaughlin, J. A.; Szent-Györgyi, A

    1984-01-01

    The rate of quenching by Ehrlich ascites cells of anionic 2,6-dimethoxy-p-semiquinone and ascorbyl free radicals is investigated as a function of cell concentration, the blocking of cell-surface sulfhydryl groups by N-ethylmaleimide, and the reduction of cell-surface charge by neuraminidase. The rate of quenching is found to be proportional to cell viability and to the number of free cell-surface sulfhydryl groups. The enzymatic action of neuraminidase results in an increase of the free radic...

  15. l-Ascorbyl-2-phosphate attenuates NF-κB signaling in SZ95 sebocytes without affecting IL-6 and IL-8 secretion

    Ikeno, Hiroshi; Apel, Mara; Zouboulis, Christos; Luger, Thomas A; Böhm, Markus

    2015-01-01

    Acne is the most common inflammatory skin disease. Interleukin-1 (IL-1) is at the beginning of the cytokine signaling cascade and may be involved in the pathogenesis of this disorder. It activates redox-sensitive transcription factors, which induce IL-6 and IL-8 expression. Interestingly, l-ascorbyl-2-phosphate (APS) was shown to have beneficial effects in patients with acne vulgaris. The mechanism of action of this agent remains unknown. Here, we investigated if APS attenuates IL-1β- or TNF-...

  16. Re-evaluation of the Optimum Dietary Vitamin C Requirement in Juvenile Eel, Anguilla japonica by Using L-ascorbyl-2-monophosphate

    Bae, Jun-Young; Park, Gun-Hyun; Yoo, Kwang-Yeol; Lee, Jeong-Yeol; Kim, Dae-Jung; Bai, Sungchul C.

    2012-01-01

    This study was conducted to re-evaluate the dietary vitamin C requirement in juvenile eel, Anguilla japonica by using L-ascorbyl-2-monophosphate (AMP) as the vitamin C source. Five semi-purified experimental diets were formulated to contain 0 (AMP0), 30 (AMP24), 60 (AMP52), 120 (AMP108) and 1,200 (AMP1137) mg AMP kg-1 diet on a dry matter basis. Casein and defatted fish meal were used as the main protein sources in the semi-purified experimental diets. After a 4-week conditioning period, fish...

  17. Effect of amino acids on the interaction between cobalamin(II) and dehydroascorbic acid

    Dereven'kov, I. A.; Thi, Thu Thuy Bui; Salnikov, D. S.; Makarov, S. V.

    2016-03-01

    The kinetics of the reaction between one-electron-reduced cobalamin (cobalamin(II), Cb(II)) and the two-electron-oxidized form of vitamin C (dehydroascorbic acid, DHA) with amino acids in an acidic medium is studied by conventional UV-Vis spectroscopy. It is shown that the oxidation of Cbl(II) by dehydroascorbic acid proceeds only in the presence of sulfur-containing amino acids (cysteine, acetylcysteine). A proposed reaction mechanism includes the step of amino acid coordination on the Co(II)-center through the sulfur atom, along with that of the interaction between this complex and DHA molecules, which results in the formation of ascorbyl radical and the corresponding Co(III) thiolate complex.

  18. Palmitate and stearate binding to human serum albumin. Determination of relative binding constants

    Vorum, H; Fisker, K; Honoré, B

    1997-01-01

    Multiple binding equilibria of two apparently insoluble ligands, palmitate and stearate, to defatted human serum albumin were studied in a 66 mM sodium phosphate buffer (pH 7.4) at 37 degrees C, by determination of dialytic exchange rates of ligands among identical equilibrium solutions. The expe...

  19. Differential effects of the ascorbyl and tocopheryl derivative on the methamphetamine-induced toxic behavior and toxicity

    A previous study showed that high doses of methamphetamine induce self-injurious behavior (SIB) in rodents. Furthermore, the combination of methamphetamine and morphine increased lethality in mice. We recently surmised that the rise in SIB and mortality induced by methamphetamine and/or morphine may be related to oxidative stress. The present study was designed to determine whether an antioxidant could inhibit SIB or mortality directly induced by methamphetamine and/or morphine. The SIB induced by 20 mg/kg of methamphetamine was abolished by the administration of Na L-ascorbyl-2-phosphate (APS: 300 mg/kg), but not Na DL-α-tocopheryl phosphate (TPNa: 200 mg/kg). In contrast, APS (300 mg/kg) and TPNa (200 mg/kg) each significantly attenuated the lethality induced by methamphetamine and morphine. The present study showed that the signal intensity of superoxide adduct was increased by 20 mg/kg of methamphetamine in the heart and lungs, and methamphetamine plus morphine tended to increase superoxide adduct in all of the tissues measured by ESR spin trap methods. Adduct signal induced in brain by methamphetamine administration increased in significance, but in mouse administrated methamphetamine plus morphine. There are differential effects of administration of methamphetamine and coadministration of methamphetamine plus morphine on adduct signal. These results suggest that APS and TPNa are effective for reducing methamphetamine-induced toxicity and/or toxicological behavior. While APS and TPNa each affected methamphetamine- and/or morphine-induced toxicology and/or toxicological behavior, indicating that both drugs have antioxidative effects, their effects differed

  20. Kinetic and thermodynamic investigation of enzymatic L-ascorbyl acetate synthesis.

    Zhang, Dong-Hao; Li, Chao; Zhi, Gao-Ying

    2013-12-01

    Kinetics and thermodynamics of lipase-catalyzed esterification of l-ascorbic acid in acetone were investigated by using vinyl acetate as acyl donor. The results showed that l-ascorbic acid could generate inhibition effect on lipase activity. A suitable model, Ping-Pong Bi-Bi mechanism having substrate inhibition, was thus introduced to describe the enzymatic kinetics. Furthermore, the kinetic and thermodynamic parameters were calculated from a series of experimental data according to the kinetic model. The inhibition constant of L-ascorbic acid was also obtained, which seemed to imply that enhancing reaction temperature could depress the substrate inhibition. Besides, the activation energy values of the first-step and the second-step reaction were estimated to be 37.31 and 4.94 kJ/mol, respectively, demonstrating that the first-step reaction was the rate-limiting reaction and could be easily improved by enhancing temperature. PMID:24211407

  1. Qualitative and quantitative assessment of fatty acids of buddleja asiatica by GC-MS

    To analyze the fatty acid contents of Buddleja asiatica Lour,both the non-volatile oil and fat obtained from the n-hexane soluble sub- fraction were subjected to GC/MS using BSTFA (N,O-bis(trimethylsilyl) trifloroacetamide) derivatization. The oil showed the presence of six fatty acids including palmitic acid (46.75 %), linoleic acid (37.80 %), stearic acid (10.98 %), arachidic acid, margaric acid and lignoceric acid (< 3 %) . Analysis of the fat revealed nine fatty acids including lignoceric acid (43.12 %), behenic acid (26.39 %), arachidic acid (9.29 %) and stearic acid (5.3 %). Cerotic acid, montanic acid, melissic acid and palmitic acid were found in low amounts (< 5 %) while trycosylic acid (4.83 %) was the only fatty acid with odd number of carbon atoms. The oil showed a low thermal stability. (author)

  2. Macrophage polarisation by fatty acids is PPARgamma-dependent.

    Pararasa, Chatyan; Bailey, Clifford; Griffiths, Helen

    2014-10-01

    Elevated plasma free fatty acids (FAs) are associated with increased risk of cardiovascular disease. We investigated the effects of the saturated FA palmitate and unsaturated FA oleate on monocyte phenotype and function. Palmitate increased cell surface expression of integrin CD11b and scavenger receptor CD36 in a concentration-dependent manner with some decrease in mitochondrial reducing capacity at high concentration (300µM). Monocytes incubated with palmitate, but not oleate, showed increased uptake of oxidized LDL and increased adhesion to rat aortic endothelium, particularly at bifurcations. The palmitate-induced increase in CD11b and CD36 expression was associated with increased cellular C16 ceramide and sphingomyelin, loss of reduced glutathione, and increased reactive oxygen species (ROS). Increased monocyte surface CD11b and CD36 was inhibited by fumonisin B1, an inhibitor of de novo ceramide synthesis, but not by the superoxide dismutase mimetic MnTBap. In contrast, MnTBap prevented the mitochondrial ROS increase and metabolic inhibition due to 300µM palmitate. This study demonstrates that in viable monocytes, palmitate but not oleate increases expression of surface CD11b and CD36. Palmitate increases monocyte adhesion to the aortic wall and promotes uptake of oxidized LDL and this involves de novo ceramide synthesis. We have also explored whether specific dietary fatty acids drive monocyte to macrophage polarisation via metabolic pathways. Here we show that monocytes pre-incubated with the saturated fatty acid palmitate increase production of inflammatory cytokines such as TNFa and IL-6 in response to a phorbol myristate differentiation trigger. This increases mitochondrial superoxide production, reduces dependency on oxidative phosphorylation through ceramide-dependent inhibition of PPARgamma activity and increases TNFa production, again via a mechanism that requires ceramide production. PMID:26461339

  3. Direct incorporation of fatty acids into microbial phospholipids in soils: Position-specific labeling tells the story

    Dippold, Michaela A.; Kuzyakov, Yakov

    2016-02-01

    Fatty acids have been used as plant and microbial biomarkers, and knowledge about their transformation pathways in soils and sediments is crucial for interpreting fatty acid signatures, especially because the formation, recycling and decomposition processes are concurrent. We analyzed the incorporation of free fatty acids into microbial fatty acids in soil by coupling position-specific 13C labeling with compound-specific 13C analysis. Position-specifically and uniformly 13C labeled palmitate were applied in an agricultural Luvisol. Pathways of fatty acids were traced by analyzing microbial utilization of 13C from individual molecule positions of palmitate and their incorporation into phospholipid fatty acids (PLFA). The fate of palmitate 13C in the soil was characterized by the main pathways of microbial fatty acid metabolism: Odd positions (C-1) were preferentially oxidized to CO2 in the citric acid cycle, whereas even positions (C-2) were preferentially incorporated into microbial biomass. This pattern is a result of palmitate cleavage to acetyl-CoA and its further use in the main pathways of C metabolism. We observed a direct, intact incorporation of more than 4% of the added palmitate into the PLFA of microbial cell membranes, indicating the important role of palmitate as direct precursor for microbial fatty acids. Palmitate 13C was incorporated into PLFA as intact alkyl chain, i.e. the C backbone of palmitate was not cleaved, but palmitate was incorporated either intact or modified (e.g. desaturated, elongated or branched) according to the fatty acid demand of the microbial community. These modifications of the incorporated palmitate increased with time. Future PLFA studies must therefore consider the recycling of existing plant and microbial-derived fatty acids. This study demonstrates the intact uptake and recycling of free fatty acids such as palmitate in soils, as well as the high turnover and transformation of cellular PLFA. Knowledge about the intact

  4. Glycation of bovine serum albumin by ascorbate in vitro: Possible contribution of the ascorbyl radical?

    Sadowska-Bartosz, Izabela; Stefaniuk, Ireneusz; Galiniak, Sabina; Bartosz, Grzegorz

    2015-01-01

    Ascorbic acid (AA) has been reported to be both pro-and antiglycating agent. In vitro, mainly proglycating effects of AA have been observed. We studied the glycation of bovine serum albumin (BSA) induced by AA in vitro. BSA glycation was accompanied by oxidative modifications, in agreement with the idea of glycoxidation. Glycation was inhibited by antioxidants including polyphenols and accelerated by 2,​2′-​azobis-​2-​methyl-​propanimidamide and superoxide dismutase. Nitroxides, known to oxid...

  5. Incorporation of l-14C-leucine in rat liver and spleen tissue after methyl palmitate action on RES

    In rats, Wistar strain, after i.v. injection of an emulsion of methyl palmitate (0.4 g methyl palmitate per animal), using 740 kBq l-14C-leucine, proteosynthesis in liver and spleen homogenates and trichloroacetate precipitates was investigated. After 2-hour and 24-hour intervals following methyl palmitate administration an insignificantly raised leucine incorporation was observed in the liver and spleen. In the liver it can be explained by increased formation of enzymes needed for more intensive metabolic processes associated with the breakdown of palmitate. In the spleen it could be due to a more rapid replication of lymphocytes or enhanced formation of specific proteins, i.e., immunoglobulins. The return of these values to normal during subsequent intervals suggests, however, that only temporary changes are involved. (author)

  6. Paliperidone Palmitate Long-Acting Injectable Given Intramuscularly in the Deltoid Versus the Gluteal Muscle: Are They Therapeutically Equivalent?

    Yin, John; Collier, Abby C; Barr, Alasdair M; Honer, William G; Procyshyn, Ric M

    2015-08-01

    Paliperidone palmitate long-acting injectable is a second-generation antipsychotic indicated for the treatment of schizophrenia. According to the product monograph, the monthly maintenance dose of paliperidone palmitate can be given in either the deltoid or gluteal muscle. Unfortunately, many clinicians may misinterpret these directions to mean that these intramuscular sites are interchangeable, and thus therapeutically equivalent. Currently, the literature on this topic is sparse, but the published pharmacokinetic studies and Food and Drug Administration submission data on paliperidone palmitate show discrepancies in the elimination half-life, peak plasma concentration, and absorption rate that are dependent on the site of injection. The degree of shifts in pharmacokinetic parameters suggests that paliperidone palmitate injections via the deltoid and gluteal muscle are not bioequivalent and therefore are not therapeutically equivalent. Thus, using the same maintenance dosing regimen at both sites or switching between sites of injection may result in unforeseen consequences in patient outcomes. PMID:26061612

  7. Downregulation of Bcl-2 Expression by miR-34a Mediates Palmitate-Induced Min6 Cells Apoptosis

    Lin, Xiaojie; Huang, Zhimin; Liu, Juan; Li, Hai; Wei, Guohong; Cao, Xiaopei; Li, Yanbing

    2014-01-01

    Recent studies have demonstrated that the expression of miR-34a is significantly upregulated and associated with cell apoptosis in pancreatic β-cell treated with palmitate. Nevertheless, the underlying detailed mechanism is largely unknown. Here, we showed that miR-34a was significantly induced in Min6 pancreatic β-cell upon palmitate treatment. Elevated miR-34a promoted Min6 cell apoptosis. Intriguingly, ectopic expression of miR-34a lowered the expression of Bcl-2, an antiapoptotic protein. Luciferase reporter assay indicated the direct interaction of miR-34a with the Bcl-2 3′-UTR. Moreover, downregulated expression of Bcl-2 induced by palmitate could be restored by inhibition of miR-34a. We conclude that direct suppression of Bcl-2 by miR-34a accounts for palmitate-induced increased apoptosis rate in pancreatic β-cell. PMID:24829923

  8. Stability evaluation of tocopheryl acetate and ascorbyl tetraisopalmitate in isolation and incorporated in cosmetic formulations using thermal analysis

    Mariana Mandelli de Almeida

    2010-03-01

    Full Text Available In view of the increase in the number of cosmetic preparations containing antioxidant vitamins, chiefly, due to their action in preventing the process of skin aging, there is a need to develop pre-formulation studies and to validate analytical methods in order to obtain high quality products. Thus, the objective of this research was to evaluate and compare the thermal behavior of tocopheryl acetate and ascorbyl tetraisopalmitate as raw materials, and incorporated into a base cream. Thermogravimetry (TG / DTG and differential scanning calorimetry (DSC were used for this purpose. Both vitamins were found to be stable up to 250ºC. The base cream (placebo and the sample (base cream containing the vitamins presented different weight loss. Thermal analysis has shown itself to be an excellent tool for the characterization of these vitamins and can be used in routine analysis for quality control of this type of cosmetic formulation.Considerando o potencial antioxidante das vitaminas utilizadas em produtos cosméticos, seu uso na prevenção do processo de envelhecimento da pele e a necessidade de estudos de pré-formulação que garantam o desenvolvimento de cosméticos de qualidade, foi objetivo deste trabalho avaliar e comparar o comportamento térmico dos ativos acetato de tocoferila e tetraisopalmitato de ascorbila, matérias-primas, isoladamente e incorporados em creme base. As técnicas termogravimetria/termogravimetria derivada (TG/DTG e calorimetria exploratória diferencial (DSC foram utilizadas para tal finalidade. Verificou-se que as vitaminas mantiveram-se estáveis até a temperatura de, aproximadamente, 250 ºC, observando-se diferença na perda de massa entre o creme base e o creme base associado às vitaminas. Assim sendo, a análise térmica mostrou-se como excelente ferramenta para caracterização das vitaminas e do creme base, podendo ser empregada em análises de rotina no controle de qualidade deste tipo de formulação cosmética.

  9. Apolipoprotein E polymorphism influences postprandial retinyl palmitate but not triglyceride concentrations

    Boerwinkle, E. (Univ. of Texas Health Science Center, Houston, TX (United States)); Brown, S.; Patsch, W. (Methodist Hospital and Baylor College of Medicine, Houston, TX (United States)); Sharrett, A.R. (National Heart, Lung, and Blood Institute, Bethesda, MD (United States)); Heiss, G. (Univ. of North Carolina, Chapel Hill, NC (United States))

    1994-02-01

    To quantify the effect of the apolipoprotein (apo) E polymorphism on the magnitude of postprandial lipemia, the authors have defined its role in determining the response to a single high-fat meal in a large sample of (N = 474) individuals taking part in the biethnic Atherosclerosis Risk in Communities Study. The profile of postprandial response in plasma was monitored over 8 h by triglyceride, triglyceride-rich lipoprotein (TGRL)-triglyceride, apo B-48/apo B-100 ratio, and retinyl palmitate concentrations, and the apo E polymorphism was determined by DNA amplification and digestion. The frequency of the apo E alleles and their effects on fasting lipid levels in this sample with vitamin A was significantly different among apo E genotypes, with delayed clearance in individuals with an [var epsilon]2 allele, compared with [var epsilon]3/3 and [var epsilon]3/4 individuals. In the sample of 397 Caucasians, average retinyl palmitate response was 1,489 [mu]g/dl in [var epsilon]2/3 individuals, compared with 1,037 [mu]g/dl in [var epsilon]3/3 individuals and 1,108 [mu]g/dl in [var epsilon]3/4 individuals. The apo E polymorphism accounted for 7.1% of the interindividual variation in postprandial retinyl palmitate response, a contribution proportionally greater than its well-known effect on fasting LDL-cholesterol. However, despite this effect on postprandial retinyl palmitate, the profile of postprandial triglyceride response was not significantly different among apo E genotypes. The profile of postprandial response was consistent between the sample of Caucasians and a smaller sample of black subjects. While these data indicate that the removal of remnant particles from circulation is delayed in subjects with the [var epsilon]2/3 genotype, there is no reported evidence that the [var epsilon]2 allele predisposes to coronary artery disease (CAD). 82 refs., 6 figs., 4 tabs.

  10. Anti-Oxidative Activity of Pectin and Its Stabilizing Effect on Retinyl Palmitate

    Ro, Jieun; Kim, Yeongseok; Kim, Hyeongmin; Jang, Soung Baek; Lee, Hyun Joo; Chakma, Suharto; Jeong, Ji Hoon; Lee, Jaehwi

    2013-01-01

    The purpose of this study was to examine the anti-oxidative activity of pectin and other polysaccharides in order to develop a cosmeceutical base having anti-oxidative effects towards retinyl palmitate (RP). The anti-oxidative stabilizing effects of pectin and other polysaccharides on RP were evaluated by DPPH assay and then the stabilizing effect of pectin on RP was examined as a function of time. Among the polysaccharides we examined, pectin exhibited a considerably higher anti-oxidative ac...

  11. A retrospective observational study of the effectiveness of paliperidone palmitate on acute inpatient hospitalization rates

    Bressington, Daniel; Stock, Jon; Hulbert, Sabina; MacInnes, Douglas

    2015-01-01

    This retrospective mirror-image observational study aimed to establish the effects of the long-acting antipsychotic injection paliperidone palmitate (PP) on acute inpatient hospitalization rates. We utilized routinely collected clinical data to compare the number and length of acute patient admissions 1 year before and 1 year after initiation of PP. A single cohort of 66 patients with a diagnosis of schizophrenia and who had received monthly injections of PP for at least 1 year were included ...

  12. Cerebral metabolism of plasma [14C]palmitate in awake, adult rat: subcellular localization

    Following intravenous injection of [U-14C]palmitate in awake adult rats, whole brain radioactivity reached a broad maximum between 15-60 min, then declined rapidly to reach a relatively stable level between 4 hr and 20 hr. At 44 hr total radioactivity was 57% of the 4 hr value (p less than 0.05). About 50% of palmitate which entered the brain from the blood was oxidized rapidly, producing 14C-labeled water-soluble components which later left the cytosol. Radioactivity in the cytosolic fraction peaked at 45 min and then declined, coincident with the decline in total brain radioactivity. Membrane fractions were rapidly labeled to levels which remained relatively stable from 1 to 44 hr. Increases in the relative distributions of radioactivity were seen between 1 and 4 hr for the microsomal and mitochondrial fractions, and beyond 4 hr for the synaptic and myelin membrane fractions (p less than 0.05). Radioactivity in membrane fractions was 80-90% lipid, 5-13% water-soluble components and 3-17% protein. The proportion of label in membrane-associated protein increased with time. Proportions of radioactivity in the combined membrane fractions increased from 65% to 76% to 80% at 4, 20 and 44 hr, respectively. The results show that plasma-derived palmitate enters oxidative and synthetic pathways to an equal extent, immediately after entry into the brain. At and after 4 hr, the radiolabel resides predominantly in stable membrane lipids and protein. Brain radioactivity at 4 hr can be used therefore, to examine incorporation of palmitate into lipids in vivo, in different experimental conditions

  13. Enhanced In Vitro Skin Deposition Properties of Retinyl Palmitate through Its Stabilization by Pectin

    Suh, Dong-Churl; Kim, Yeongseok; Kim, Hyeongmin; Ro, Jieun; Cho, Seong-Wan; Yun, Gyiae; Choi, Sung-Up; Lee, Jaehwi

    2014-01-01

    The purpose of this study was to examine the effect of stabilization of retinyl palmitate (RP) on its skin permeation and distribution profiles. Skin permeation and distribution study were performed using Franz diffusion cells along with rat dorsal skin, and the effect of drug concentration and the addition of pectin on skin deposition profiles of RP was observed. The skin distribution of RP increased in a concentration dependent manner and the formulations containing 0.5 and 1 mg of pectin d...

  14. Identification of sitosteryl glucoside palmitate in a chloroform-derived fraction of Phyllanthus niruri with antiplasmodial and peripheral antinociceptive properties

    Ezenyi; Ifeoma; Chinwude; Kulkarni; Roshan; Joshi; Swati; Salawu; Oluwakanyinsola; Adeola; Emeje; Martins

    2014-01-01

    Objective:To evaluate the antiplasmodial properties of fractions of chloroform portion of Phyllanthus niruri(P.niruri) methanol extract and identify a suitable chemical marker present therein.Methods:Chloroform portion of P.niruri methanol extract was separated from silica gel using gradient systems of hexane,ethylacetate and methanol.The fractions were screened for antiplasmodial activity against Plasmodium falciparum HB3 and FcM29.Fractions with IC50<10μg/ml.against parasites were further screened for peripheral analgesic activity,while cytotoxicity was evaluated using THP-1 cells.Results:Fractions 12-14 were very active(IC50<10 μg/mL) against Plasmodium falciparum and showed no significant cytotoxicity.Fractions 12 and 13 exhibited significant(P<0.01) reduction in acetic acid-induced writhing in mice,decreasing the number of writhes by 66.67% and 65.22% respectively and comparable with 100 mg/kg aspirin(65.22%).From fraction 12,a compound was isolated and identified as sitosteryl-6-β-D-glucoside-6’-palmitate by 1H,13C nuclear magnetic resonance and mass spectroscopies.Conclusions:Our findings illustrate antiplasmodial column fractions of P.niruri with analgesic activity and identify sitosteryl glucoside pahmitate as a chemical marker of activity.

  15. PINK1 alleviates palmitate induced insulin resistance in HepG2 cells by suppressing ROS mediated MAPK pathways.

    Cang, Xiaomin; Wang, Xiaohua; Liu, Pingli; Wu, Xue; Yan, Jin; Chen, Jinfeng; Wu, Gang; Jin, Yan; Xu, Feng; Su, Jianbin; Wan, Chunhua; Wang, Xueqin

    2016-09-01

    Oxidative stress is an important pathogenesis of insulin resistance (IR) and Type 2 diabetes mellitus (T2DM). Studies have shown that knockdown of PTEN-induced putative kinase 1 (PINK1) causes oxidative stress and mitophagy. In db/db mice, PINK1 protein level is down-regulated. However, little is known regarding the mechanism by which PINK1 modulates IR in response to reactive oxygen species (ROS) induced stress. In our study, PINK1 expression decreased during palmitate (PA) induced IR in HepG2 cells and the hepatic tissues of high fat diet (HFD) fed mice. Additionally, free fatty acids (FFAs) could increase ROS and suppress insulin signaling pathway, which was indicated by reduced phosphorylation of protein kinase B (AKT) and glycogen synthase kinase 3β (GSK-3β). In addition, insulin induced glucose uptake decreased and the expression of phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase), two key gluconeogenic enzymes, was up-regulated after PA treatment. Intriguingly, PINK1 overexpression could lead to opposite results. Moreover, PA induced hepatic IR through C-Jun N-terminal kinase (JNK) and extracellular signal-regulated kinase (ERK) pathways, which were rescued by PINK1 overexpression. In summary, our results demonstrate that PINK1 promoted hepatic IR via JNK and ERK pathway in PA treated HepG2 cells, implying a novel molecular target for the therapy of diabetes. PMID:27423393

  16. Fortification of fried potato chips with antioxidant vitamins to enhance their nutritional value and storage ability

    Edress El-Sayed, Fyka; Mahmoud Allam, Samah Said

    2004-01-01

    The frying shelf life of commercial frying oil was increased by the addition of synthetic and natural antioxidants, e.g. TBHQ, retinyl palmitate and ascorbyl palmitate (antioxidant vitamins).The results revealed that TBHQ had the best effect in retarding the deteriorative effect of frying conditions throughout 24h of frying potato chips at 180±10 ºC followed by the effect of retinyl palmitate and the effect of ascorbyl palmitate compared to the control without any additives. Fried...

  17. Live food mediated vitamin C transfer to Dicentrarchus labraxand Clarias gariepinus

    Merchie, G.; Lavens, P.; Dhert, Ph.; Pector, R.; Mai Soni, A.F.; Nelis, H.; Ollevier, F.P.; De leenheer, A P; Sorgeloos, P.

    1995-01-01

    Live food enrichment techniques, using formulated diets and emulsions for improving the nutritional quality of Brachionus and Artemia , were studied as a tool for transferring ascorbic acid (AA) to fish larvae. Artemia nauplii enriched for 24h with an experimental emulsion containing 20% HUFA and 0%, 10% and 20% ascorbyl palmitate (AP) were administered to catfish larvae in a 20-day feeding trial. Survival was not affected by the dietary AA, but from day 7 onwards a significantly positive eff...

  18. Effects of dietary vitamin C on fish and crustacean larvae

    Merchie, G.; Lavens, P.; Sorgeloos, P.

    1995-01-01

    In order to assess the dietary needs for ascorbic acid (AA) at startfeeding, the AA content in the various live diets currently applied in aquaculture (algae, rotifers, Artemia ) was studied. Application of boosting techniques using ascorbyl palmitate (AP) as the vitamin C source enabled the transfer of elevated levels of bioactive vitamin C (up to 2500µg AA.g DW-1) via the live food chain into larvae of fish (Clarias gariepinus, Dicentrarchus labrax, Scophthalmus maximus), shrimp (Pennaeus v...

  19. Optimization of dietary vitamin C in fish and crustacean larvae: a review

    Merchie, G.; Lavens, P.; Sorgeloos, P.

    1997-01-01

    HPLC techniques were adapted and standardized for quantification of ascorbic acid (AA) and its derivates in both diets and target organisms. To assess the dietary needs for AA at start of exogenous feeding, the AA content in the various live diets currently used in aquaculture (algae, rotifers, Artemia ) was analyzed. Application of techniques for boosting vitamin C using ascorbyl palmitate as the source enabled the transfer of elevated levels (up to 2,500 µg AA/g DW) of bioactive vitamin C. ...

  20. Equilibrium spreading pressure and Langmuir–Blodgett film formation of omega-substituted palmitic acids

    Snow, Arthur W., E-mail: arthur.snow@nrl.navy.mil; Jernigan, Glenn G.; Ancona, Mario G.

    2014-04-01

    Langmuir–Blodgett isotherms and equilibrium spreading pressures were measured for compounds of the series X–(CH{sub 2}){sub 15}COOH, X = CH{sub 3}, SH, OH, F, Cl, Br. Only the CH{sub 3} and F terminated compounds formed monolayers with sufficient stability for accurate isotherm measurement, film transfer and X-ray photoelectron spectroscopic analysis. The presence of the terminal heteroatom substituents significantly diminished the stability of the L–B film and depressed the equilibrium spreading pressures (20 °C) from 15.4 mN/m for the CH{sub 3} terminated compound to a range of 0.95 to 0.08 mN/m for the other members of the series. These characteristics are attributed to the monolayer film being in a metastable state and the dipole moment of the heteroatom terminal group increasing the monolayer film kinetic instability by facilitating the formation of three-dimensional structures. - Highlights: • Compound series X–(CH{sub 2}){sub 15}COOH, X = CH{sub 3}, SH, OH, F, Cl, Br was analyzed. • Only-CH{sub 3} and-F terminated compounds form stable Langmuir–Blodgett films. • Heteroatom terminal groups promote kinetic instability in Langmuir–Blodgett films. • X-ray photoelectron spectra analyzed for molecular orientation and packing density.

  1. Protection provided by phytoestrogens against cardiac lipotoxicity induced by palmitic acid

    Couto, Renata Lopes Familiar

    2014-01-01

    A menopausa é um processo biológico natural caracterizado pela redução dos níveis hormonais, nomeadamente, o estrogénio e progesterona. A perda de estrogénios parece desencadear uma cascata de eventos, levando ao aumento do risco para doenças cardiovasculares. A conjugação do processo de envelhecimento e perda de estrogénio durante a menopausa tem um impacto negativo no metabolismo dos lípidos no coração, o que resulta no aumento da lipotoxicidade e portanto do risco de doenças cardiovascular...

  2. Equilibrium spreading pressure and Langmuir–Blodgett film formation of omega-substituted palmitic acids

    Langmuir–Blodgett isotherms and equilibrium spreading pressures were measured for compounds of the series X–(CH2)15COOH, X = CH3, SH, OH, F, Cl, Br. Only the CH3 and F terminated compounds formed monolayers with sufficient stability for accurate isotherm measurement, film transfer and X-ray photoelectron spectroscopic analysis. The presence of the terminal heteroatom substituents significantly diminished the stability of the L–B film and depressed the equilibrium spreading pressures (20 °C) from 15.4 mN/m for the CH3 terminated compound to a range of 0.95 to 0.08 mN/m for the other members of the series. These characteristics are attributed to the monolayer film being in a metastable state and the dipole moment of the heteroatom terminal group increasing the monolayer film kinetic instability by facilitating the formation of three-dimensional structures. - Highlights: • Compound series X–(CH2)15COOH, X = CH3, SH, OH, F, Cl, Br was analyzed. • Only-CH3 and-F terminated compounds form stable Langmuir–Blodgett films. • Heteroatom terminal groups promote kinetic instability in Langmuir–Blodgett films. • X-ray photoelectron spectra analyzed for molecular orientation and packing density

  3. 维生素C糖苷类衍生物的研究进展%Research progress of ascorbyl glucoside derivates

    饶建华; 韩璐; 张自萍

    2012-01-01

    Vitamin C is listed in the essential nutrition elements of human beings or animals, and plays an important role in protecting human health and animal growth. The well-known susceptibility of vitamin C to oxida-tive degradation has led to great interest in its derivatives with increased stability in recent years. The vitamin C derivatives can be classified as salt, ester and saccharide derivatives. Ascorbyl glucoside derivates represent a kind of important vitamin C derivatives. Many domestic and overseas research papers have reported various saccharide derivatives of vitamin C. Therefore, in this review we summarized the latest research progress of ascorbyl glucoside derivates with chemical modification of hydroxyl group at the C2-, C5- and C6-position of vitamin C.%维生素C( vitamin C,VC)是人体的必需营养元素,在保护人类健康和动物生长过程中起到不可代替的重要作用.由于VC自身易被氧化降解,开发稳定的高附加值VC衍生物就成为人们研究的热点.目前,VC衍生物主要有VC盐、VC酯和VC糖苷3种形式,其中VC糖苷类衍生物稳定性高,生理活性与VC 最接近,近年来备受国内外学者的关注.因此,本文就VC上的C2-,C5-及C6-糖苷类衍生物的国内外研究进展进行了归纳总结.

  4. Quantitation of fatty acids by GLC and separation of omega-6 nutraceutical fatty acid from carthamus tinctorius L. seed oil cultivated in Pakistan

    The GLC analysis of carthamus tinctorius (safflower) yielded average hexane extracted oil content of 28% (25-30%); the oil contained high level of linoleic acid (74%). Monounsaturated fatty acid, oleic acid amounted 12.94%, while the saturated fatty acids like palmitic acid and stearic acid were 9.43 and 1.81%, respectively. Iodine value of linoleic acid was found to be 160:1 while its purity was 93.1%. (author)

  5. Synthesis and structural analysis of 13C-fatty acids

    2000-01-01

    The 13C-labeled fatty acids octanoic-1-13C acid and palmitic-l-13C acid were synthetically prepared from Ba 13CO3. The yield of the former was more than 90% and that of the latter was above 85%. MS, IR, 1H-NMR and 13NMR were performed to analyze the structures of the two 13C-fatty acids, compared with their unlabeled fatty acids.

  6. The effect of two novel cholesterol-lowering agents, disodium ascorbyl phytostanol phosphate (DAPP) and nanostructured aluminosilicate (NSAS) on the expression and activity of P-glycoprotein within Caco-2 cells

    Sachs-Barrable, Kristina; Darlington, Jerald W; Wasan, Kishor M.

    2014-01-01

    Background Many drugs are substrates for P-glycoprotein (P-gp) and interactions involving P-gp may be relevant to clinical practice. Co-administration with P-gp inhibitors or inducers changes the absorption profile as well as the risk for drug toxicity, therefore it is important to evaluate possible P-gp alterations. The purpose of this study was to investigate the effect of two novel cholesterol-lowering agents, disodium ascorbyl phytostanol phosphate (DAPP) and nanostructured aluminium sili...

  7. Solubilized delivery of paliperidone palmitate by D-alpha-tocopheryl polyethylene glycol 1000 succinate micelles for improved short-term psychotic management.

    Muthu, Madaswamy S; Sahu, Ashish K; Sonali; Abdulla, Allabakshi; Kaklotar, Dhansukh; Rajesh, Chellappa V; Singh, Sanjay; Pandey, Bajarangprasad L

    2016-01-01

    The objective of this work was to formulate paliperidone palmitate-loaded d-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS or TPGS) micelles for improved antipsychotic effect during short-term management of psychotic disorders. Vitamin E TPGS micelles containing paliperidone palmitate were prepared by the solvent casting method and control paliperidone palmitate formulations were prepared by simple sonication method. The prepared micelles and control paliperidone palmitate formulations were evaluated for different parameters. Particle sizes of prepared micelles, control paliperidone palmitate formulations were determined at 25 °C by dynamic light scattering technique and external surface morphology was determined by transmission electron microscopy analysis. The encapsulation efficiency was determined by spectrophotometery. In-vitro release studies of micelles and control formulations were carried out by dialysis bag diffusion method. The particle sizes of the paliperidone palmitate-loaded TPGS micelles were 26.5 nm. About 92% of drug encapsulation efficiency was achieved with micelles. The drug release from paliperidone palmitate-loaded TPGS micelles was sustained for more than 24 h with 40% of drug release. The TPGS product, i.e. paliperidone palmitate-loaded micelles, resulted in nano-sized delivery, solubility enhancement and permeability of the micelles which provided an improved and prolonged anti-psychotic effect in comparison to control paliperidone palmitate formulation. PMID:24853962

  8. Fatty acids composition of fruits of selected Central European sedges (Carex L. Cyperaceae)

    Bogucka-Kocka, A.; Janyszek, M.

    2010-07-01

    Fatty acids in the fruits of 13 sedge species (Ca rex L., Cyperaceae) were analyzed. The oil contents in the fruits of the studied sedges ranged from 3.73 and 46.52%. In the studied fruit oils 14 different fatty acids were identified. The main unsaturated fatty acids were: linoleic, a-linolenic, oleic, oleo palmitic n-7; oleo palmitic n-9, octadecenic, and eicosenoic acids. The following acids were found in the greatest quantities: linoleic, oleic, a-linolenic and palmitic acids. Based on the fatty acid composition, studied taxa can be divided in two groups. The first group (C. flava, C. pseudocyperus, C. riparia, C. leporina) is a very good source of linoleic acid. The second group, including the remaining species, is a good source of a-linolenic acid. The highest oleic acid contents were observed in C. vulpina. The studied material has shown a low concentration of saturated fatty acids, among which palmitic acid was the main one.Results of the analyses allow for the inclusion of the studied species among plants whose fruits are characterized by a high content of unsaturated fatty acids. (Author)

  9. Nuclear factor-κB is a common upstream signal for growth differentiation factor-5 expression in brown adipocytes exposed to pro-inflammatory cytokines and palmitate

    Highlights: • GDF5 expression is up-regulated by IL-1β, TNF-α and palmitate in brown pre-adipocytes. • NF-κB stimulates promoter activity and expression of GDF5 in brown pre-adipocytes. • Recruitment of NF-κB to the GDF5 promoter is facilitated in BAT from ob/ob mice. • An NF-κB inhibitor prevents upregulation of GDF5 expression in brown pre-adipocytes. - Abstract: We have previously demonstrated that genetic and acquired obesity similarly led to drastic upregulation in brown adipose tissue (BAT), rather than white adipose tissue, of expression of both mRNA and corresponding protein for the bone morphogenic protein/growth differentiation factor (GDF) member GDF5 capable of promoting brown adipogenesis. In this study, we evaluated expression profiles of GDF5 in cultured murine brown pre-adipocytes exposed to pro-inflammatory cytokines and free fatty acids (FFAs), which are all shown to play a role in the pathogenesis of obesity. Both interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) were effective in up-regulating GDF5 expression in a concentration-dependent manner, while similar upregulation was seen in cells exposed to the saturated FFA palmitate, but not to the unsaturated FFA oleate. In silico analysis revealed existence of the putative nuclear factor-κB (NF-κB) binding site in the 5′-flanking region of mouse GDF5, whereas introduction of NF-κB subunits drastically facilitated both promoter activity and expression of GDF5 in brown pre-adipocytes. Chromatin immunoprecipitation analysis confirmed significant facilitation of the recruitment of NF-κB to the GDF5 promoter in lysed extracts of BAT from leptin-deficient ob/ob obese mice. Upregulation o GDF5 expression was invariably inhibited by an NF-κB inhibitor in cultured brown pre-adipocytes exposed to IL-1β, TNF-α and palmitate. These results suggest that obesity leads to upregulation of GDF5 expression responsible for the promotion of brown adipogenesis through a mechanism

  10. Nuclear factor-κB is a common upstream signal for growth differentiation factor-5 expression in brown adipocytes exposed to pro-inflammatory cytokines and palmitate

    Hinoi, Eiichi; Iezaki, Takashi; Ozaki, Kakeru; Yoneda, Yukio, E-mail: yyoneda@p.kanazawa-u.ac.jp

    2014-10-03

    Highlights: • GDF5 expression is up-regulated by IL-1β, TNF-α and palmitate in brown pre-adipocytes. • NF-κB stimulates promoter activity and expression of GDF5 in brown pre-adipocytes. • Recruitment of NF-κB to the GDF5 promoter is facilitated in BAT from ob/ob mice. • An NF-κB inhibitor prevents upregulation of GDF5 expression in brown pre-adipocytes. - Abstract: We have previously demonstrated that genetic and acquired obesity similarly led to drastic upregulation in brown adipose tissue (BAT), rather than white adipose tissue, of expression of both mRNA and corresponding protein for the bone morphogenic protein/growth differentiation factor (GDF) member GDF5 capable of promoting brown adipogenesis. In this study, we evaluated expression profiles of GDF5 in cultured murine brown pre-adipocytes exposed to pro-inflammatory cytokines and free fatty acids (FFAs), which are all shown to play a role in the pathogenesis of obesity. Both interleukin-1β (IL-1β) and tumor necrosis factor-α (TNF-α) were effective in up-regulating GDF5 expression in a concentration-dependent manner, while similar upregulation was seen in cells exposed to the saturated FFA palmitate, but not to the unsaturated FFA oleate. In silico analysis revealed existence of the putative nuclear factor-κB (NF-κB) binding site in the 5′-flanking region of mouse GDF5, whereas introduction of NF-κB subunits drastically facilitated both promoter activity and expression of GDF5 in brown pre-adipocytes. Chromatin immunoprecipitation analysis confirmed significant facilitation of the recruitment of NF-κB to the GDF5 promoter in lysed extracts of BAT from leptin-deficient ob/ob obese mice. Upregulation o GDF5 expression was invariably inhibited by an NF-κB inhibitor in cultured brown pre-adipocytes exposed to IL-1β, TNF-α and palmitate. These results suggest that obesity leads to upregulation of GDF5 expression responsible for the promotion of brown adipogenesis through a mechanism

  11. Tectorigenin Attenuates Palmitate-Induced Endothelial Insulin Resistance via Targeting ROS-Associated Inflammation and IRS-1 Pathway.

    Qi Wang

    Full Text Available Tectorigenin is a plant isoflavonoid originally isolated from the dried flower of Pueraria thomsonii Benth. Although its anti-inflammatory and anti-hyperglycosemia effects have been well documented, the effect of tectorigenin on endothelial dysfunction insulin resistance involved has not yet been reported. Herein, this study aims to investigate the action of tectorigenin on amelioration of insulin resistance in the endothelium. Palmitic acid (PA was chosen as a stimulant to induce ROS production in endothelial cells and successfully established insulin resistance evidenced by the specific impairment of insulin PI3K signaling. Tectorigenin effectively inhibited the ability of PA to induce the production of reactive oxygen species and collapse of mitochondrial membrane potential. Moreover, tectorigenin presented strong inhibition effect on ROS-associated inflammation, as TNF-α and IL-6 production in endothelial cells was greatly reduced with suppression of IKKβ/NF-κB phosphorylation and JNK activation. Tectorigenin also can inhibit inflammation-stimulated IRS-1 serine phosphorylation and restore the impaired insulin PI3K signaling, leading to a decreased NO production. These results demonstrated its positive regulation of insulin action in the endothelium. Meanwhile, tectorigenin down-regulated endothelin-1 and vascular cell adhesion molecule-1 overexpression, and restored the loss of insulin-mediated vasodilation in rat aorta. These findings suggested that tectorigenin could inhibit ROS-associated inflammation and ameliorated endothelial dysfunction implicated in insulin resistance through regulating IRS-1 function. Tectorigenin might have potential to be applied for the management of cardiovascular diseases involved in diabetes and insulin resistance.

  12. High-Fat Diet and Palmitate Alter the Rhythmic Secretion of Glucagon-Like Peptide-1 by the Rodent L-cell.

    Gil-Lozano, Manuel; Wu, W Kelly; Martchenko, Alexandre; Brubaker, Patricia L

    2016-02-01

    Secretion of the incretin hormone, glucagon-like peptide-1 (GLP-1), by the intestinal L-cell is rhythmically regulated by an independent molecular clock. However, the impact of factors known to affect the activity of similar cell-autonomous clocks, such as circulating glucocorticoids and high-fat feeding, on GLP-1 secretory patterns remains to be elucidated. Herein the role of the endogenous corticosterone rhythm on the pattern of GLP-1 and insulin nutrient-induced responses was examined in corticosterone pellet-implanted rats. Moreover, the impact of nutrient excess on the time-dependent secretion of both hormones was assessed in rats fed a high-fat, high-sucrose diet. Finally, the effects of the saturated fatty acid, palmitate, on the L-cell molecular clock and GLP-1 secretion were investigated in vitro using murine GLUTag L-cells. Diurnal variations in GLP-1 and insulin nutrient-induced responses were maintained in animals lacking an endogenous corticosterone rhythm, suggesting that glucocorticoids are not the predominant entrainment factor for L-cell rhythmic activity. In addition to hyperglycemia, hyperinsulinemia, insulin resistance, and disorganization of feeding behavior, high-fat high-sucrose-fed rats showed a total abrogation of the diurnal variation in GLP-1 and insulin nutrient-induced responses, with comparable levels of both hormones at the normal peak (5:00 pm) and trough (5:00 am) of their daily pattern. Finally, palmitate incubation induced profound derangements in the rhythmic expression of circadian oscillators in GLUTag L-cells and severely impaired the secretory activity of these cells. Collectively our findings demonstrate that obesogenic diets disrupt the rhythmic activity of the L-cell, partially through a direct effect of specific nutritional components. PMID:26646204

  13. A Novel Liposomal Dexamethasone Palmitate Formulation and Anti-inflammatory Effects on Mice

    LI, Ji; YANG, Jing; WANG, Wenxin; YU, Jichen; FU, Jingguo; WANG, Xiaolai

    2009-01-01

    A novel dexamethasone palmitate liposomal long-circulating (DPL long-circulating) drug delivery system was established. The DPL long-circulating and DPL (dexamethasone palmitate liposomal) systems were prepared by film-distributed extrusion with phospholipid and cholesterol. The formulation stability of DPL long-circulating and DPL were investigated. The anti-inflammatory activity and acute toxicity of DPL long-circulating, DPL and dexa- methasone sodium phosphate injection (DSP) were evaluated with mice. The DPL long-circulating systems were successfully prepared by film-distributed extrusion methods. The experimental results showed that the DPL long-circulating had uniform particle size and stable property. The DPL long-circulating and DPL showed stronger anti-inflammatory effect than DSP in an anti-inflammatory test. Acute toxicity tests showed that DSP injection had lower toxicity than the DPL long-circulating and DPL, which suggested that DPL long-circulating and DPL had higher bioavailability with passive targeting efficacy of liposomes. The DPL long-circulating formulation product can meet quality requirement. This formulation had stronger anti-inflammatory effect and higher acute toxicity.

  14. Effectiveness of long-acting paliperidone palmitate in borderline personality disorder.

    Palomares, Nerea; Montes, Ana; Díaz-Marsá, Marina; Carrasco, José L

    2015-11-01

    The aim of the present study is to test the efficacy of palmitate paliperidone long-acting injection for patients with borderline personality disorder (BPD). A total of 16 patients with BPD were treated with intramuscular paliperidone palmitate (IMPP) over 12 weeks. Effectiveness measures included the CGI-BPD, HARS, MADRS, BIS-11, and STAXI-2. Functional improvement was assessed using the Global Assessment of Functioning scale. A list of adverse events was provided to clinicians and patients. Treatment with IMPP was associated with a significant average reduction of 1.6 (95% confidence interval: 1192-2008; P>0.01) in CGI-BPD scores and an average increase of psychosocial functioning as scored by the Global Assessment of Functioning scale of 13.3 (95% confidence interval: 8.35-18.31; P>0.01) was obtained. The treatment decreased impulsive-disruptive behaviors and improved general functioning. An acceptable tolerance was observed. The average weight gain was clinically irrelevant despite being statistically significant. No other relevant adverse side effects were reported, with the exception of galactorrhea, which required suspension of treatment in three patients. IMPP seems to be a well-tolerated alternative to other second-generation antipsychotics in the treatment of BPD. More controlled studies replicating these results should be proposed in the future. PMID:26230268

  15. A Controlled, Evidence-Based Trial of Paliperidone Palmitate, A Long-Acting Injectable Antipsychotic, in Schizophrenia

    Nasrallah, Henry A.; Gopal, Srihari; Gassmann-Mayer, Cristiana; Quiroz, Jorge A.; Lim, Pilar; Eerdekens, Mariëlle; Yuen, Eric; Hough, David

    2010-01-01

    Paliperidone palmitate is a long-acting injectable antipsychotic agent. This 13-week, multicenter, randomized (1 : 1 : 1 : 1), double-blind, parallel-group study evaluated the efficacy, safety, and tolerability of fixed 25, 50, and 100 milligram equivalent (mg equiv.) doses of paliperidone palmitate vs placebo administered as gluteal injections on days 1 and 8, then every 4 weeks (days 36 and 64) in 518 adult patients with schizophrenia. The intent-to-treat analysis set (N=514) was 67% men an...

  16. In Vitro Evaluation of the Antiviral Activity of the Synthetic Epigallocatechin Gallate Analog-Epigallocatechin Gallate (EGCG Palmitate against Porcine Reproductive and Respiratory Syndrome Virus

    Chunjian Zhao

    2014-02-01

    Full Text Available In this study, epigallocatechin gallate (EGCG palmitate was synthesized and its anti-porcine reproductive and respiratory syndrome virus (PRRSV activity was studied. Specifically, EGCG palmitate was evaluated for its ability to inhibit PRRSV infection in MARC-145 cells when administered as pre-, post-, or co-treatment. EGCG and ribavirin were used as controls. The results showed that a 50% cytotoxic concentration (CC50 of EGCG, EGCG palmitate, and ribavirin was achieved at 2,359.71, 431.42, and 94.06 μM, respectively. All three drugs inhibited PRRSV in a dose-dependent manner regardless of the treatment protocol. EGCG palmitate exhibited higher cytotoxicity than EGCG, but lower cytotoxicity than ribavirin. EGCG palmitate anti-PRRSV activity was significantly higher than that of EGCG and ribavirin, both as pre-treatment and post-treatment. Under the former conditions and a tissue culture infectious dose of 10 and 100, the selectivity index (SI of EGCG palmitate in the inhibition of PRRSV was 3.8 and 2.9 times higher than that of ribavirin when administered as a pre-treatment, while the SI of EGCG palmitate in the inhibition of PRRSV was 3.0 and 1.9 times higher than ribavirin when administered as a post-treatment. Therefore, EGCG palmitate is potentially effective as an anti-PRRSV agent and thus of interest to the pharmaceutical industry.

  17. The crystallization of metal soaps and fatty acids in oil paint model systems.

    Hermans, Joen J; Keune, Katrien; Loon, Annelies van; Iedema, Piet D

    2016-04-20

    The formation and crystallization of metal soaps in oil paint layers is an important issue in the conservation of oil paintings. The chemical reactions and physical processes that are involved in releasing metal ions from pigments and fatty acids from the oil binder to form crystalline metal soap deposits have so far remained poorly understood. We have used a combination of differential scanning calorimetry (DSC) and attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) on model mixtures of palmitic acid, lead palmitate or zinc palmitate and linseed oil to study the transition from amorphous material to crystalline fatty acid or metal soap. This transition forms the final stage in the cascade of processes leading to metal soap-related oil paint degradation. Palmitic acid as well as the metal soaps showed nearly ideal solubility behavior. However, it was found that, near room temperature, both lead and zinc palmitate are practically insoluble in both liquid and partially polymerized linseed oil. Interestingly, the rate of metal soap and fatty acid crystallization decreased rapidly with the degree of linseed oil polymerization, possibly leading to systems where metal soaps are kinetically trapped in a semi-crystalline state. To explain the various morphologies of metal soap aggregates observed in oil paint layers, it is proposed that factors affecting the probability of crystal nucleation and the rate of crystal growth play a crucial role, like exposure to heat or cleaning solvents and the presence of microcracks. PMID:27039879

  18. Enzymatic Hydrolysis of Magnesium Ascorbyl Phosphate and Kinetic Analysis%酶法水解VC磷酸酯镁及其动力学分析

    郎爱花; 刘惠青; 车影; 闫果兰; 靳利娥

    2012-01-01

    In order to investigate the process of enzymatic hydrolysis of magnesium ascorbyl phosphate (MAP), the best hydrolysis condition was chosen and the kinetics was analyzed through the experiments. With phosphoesterase complex (PC) as catalyst, the effect on the degree of MAP hydrolysis by some influenced factors such as substrate concentration, reaction time, pH, temperature, enzyme content was investigated and the hydrolysis kinetics was studied. The results show that hydrolysis degree of MAP reached the largest, to (32. 64 + 0. 42) % under the conditions of 1. 72g/L substrate concentration by 5% enzyme, 37 °C , pH 5. 5,hydrolysis time 4h. The established kinetics followed the equation of Michealis-Menten, km and vmax of which were 25. 82 g/L and 126. 26 g/(L · h), respectively.%考察酶法水解Vc磷酸酯镁(Magnesium Ascorbyl Phosphate,MAP)过程,采用复合磷酸酯酶( Phosphoesterase Complex,PC)为催化剂,以水解产物Vc的含量(水解率)为指标考察底物浓度、反应时间、pH值、反应温度、酶用量等因素对MAP水解程度的影响,选择最佳水解条件并对其进行动力学分析.结果表明,在底物MAP的质量浓度为1.72 g/L、酶和底物的体积分数为5%、温度37℃、pH5.5条件下水解4h,水解率最大,可达(32.64 ±0.42)%.动力学分析表明:水解动力学符合米氏方程,其中km=25.82 g/L,vmax=126.26 g/(L·h).

  19. Vitamin C derivatives as new coreactants for tris(2,2'-bipyridine)ruthenium(II) electrochemiluminescence

    Highlights: → Ru(bpy)32+ electrochemiluminescence of vitamin C derivatives have been investigated. → Ascorbyl phosphate and ascorbyl palmitate show intense electrochemiluminescence. → Ascorbyl 2-phosphate was detected with high sensitivity. → This study provides a new way to detect vitamin C derivatives. - Abstract: Vitamin C derivatives (VCDs) have been widely used as the alternative and stable sources of vitamin C, and accordingly exhibit many new applications, such as anti-tumor and central nervous system drug delivery. In this study, their Ru(bpy)32+ electrochemiluminescence (ECL) properties have been investigated for the first time using well-known ascorbyl phosphate and ascorbyl palmitate as representative VCDs. Ascorbyl phosphate and ascorbyl palmitate are VCDs with different substituted positions. Both of them increase Ru(bpy)32+ ECL, indicating that other VCDs may also enhance Ru(bpy)32+ ECL signal. The calibration plot for ascorbyl phosphate is linear from 3 x 10-6 to 1.0 x 10-3 M with a detection limit of 1.4 x 10-6 M at a signal-to-noise ratio of 3. The relative standard deviation is 3.6% for six replicate measurements of 0.01 mM ascorbyl 2-phosphate solution. The proposed method is about one order of magnitude more sensitive than electrochemical and UV-vis methods for the determination of ascorbyl phosphate, and is used successfully for the determination of ascorbyl phosphate in whitening and moisturising body wash.

  20. Modulation of Swarming and Virulence by Fatty Acids through the RsbA Protein in Proteus mirabilis

    Liaw, Shwu-Jen; Lai, Hsin-Chih; Wang, Won-Bo

    2005-01-01

    After sensing external signals, Proteus mirabilis undergoes a multicellular behavior called swarming which is coordinately regulated with the expression of virulence factors. Here we report that exogenously added fatty acids could act as signals to regulate swarming in P. mirabilis. Specifically, while oleic acid enhanced swarming, some saturated fatty acids, such as lauric acid, myristic acid, palmitic acid, and stearic acid, inhibited swarming. We also found that expression of hemolysin, wh...

  1. Synergy analysis reveals association between insulin signaling and desmoplakin expression in palmitate treated HepG2 cells.

    Xuewei Wang

    Full Text Available The regulation of complex cellular activities in palmitate treated HepG2 cells, and the ensuing cytotoxic phenotype, involves cooperative interactions between genes. While previous approaches have largely focused on identifying individual target genes, elucidating interacting genes has thus far remained elusive. We applied the concept of information synergy to reconstruct a "gene-cooperativity" network for palmititate-induced cytotoxicity in liver cells. Our approach integrated gene expression data with metabolic profiles to select a subset of genes for network reconstruction. Subsequent analysis of the network revealed insulin signaling as the most significantly enriched pathway, and desmoplakin (DSP as its top neighbor. We determined that palmitate significantly reduces DSP expression, and treatment with insulin restores the lost expression of DSP. Insulin resistance is a common pathological feature of fatty liver and related ailments, whereas loss of DSP has been noted in liver carcinoma. Reduced DSP expression can lead to loss of cell-cell adhesion via desmosomes, and disrupt the keratin intermediate filament network. Our findings suggest that DSP expression may be perturbed by palmitate and, along with insulin resistance, may play a role in palmitate induced cytotoxicity, and serve as potential targets for further studies on non-alcoholic fatty liver disease (NAFLD.

  2. Quantitative analysis of retinol and retinol palmitate in vitamin tablets using 1H-nuclear magnetic resonance spectroscopy

    1H-NMR spectrometry was applied to the quantitative analysis of Vitamin A in four different types of vitamin tablets without any chromatographic purification or saponification. The experiment was performed analysing the H-15 resonance, which appears at δ 4.32 for retinol and δ 4.69 for retinol palmitate, well separated from other resonances in the 1H-NMR spectrum. Compounds were quantified using the relative ratio of the integral of the H-15 signal to that of a known amount of internal standard (200 μg/ml), anthracene. In order to evaluate the feasibility of avoiding the saponification of retinol palmitate in the preparation of samples, several solvents such as dimethylsulfoxide, n-hexane, methanol, water, and 0.1 M of HCl were tested as possible extraction solvents. Among these, dimethylsulfoxide showed the best yield of retinol palmitate. This method, using dimethylsulfoxide extraction and 1H-NMR, allows rapid and simple quantitation of retinol palmitate in tablets avoiding tedious saponification

  3. Automated production of [11C]acetate and [11C]palmitate using a modified GE Tracerlab FXC-Pro

    As researchers explore new applications for positron emission tomography radiopharmaceuticals, the demand for effective and readily available radiopharmaceuticals continues to increase. The syntheses of two such radiopharmaceuticals, [11C]acetate and [11C]palmitate, can be automated on the GE Tracerlab FXC-Pro by utilizing Grignard reactions. Radiochemical purities of the [11C]acetate and the [11C]palmitate products were high (>98% and >99.9%, respectively) with average non-corrected yields of 18% (n=3) and 10% (n=5), respectively. These data comprise the validation trials for site qualification of clinical production of both radiopharmaceuticals. -- Graphical abstract: Automated syntheses of [11C]acetate and [11C]palmitate using a modified GE Tracerlab FXC-Pro are reported. Radiochemical purities of the [11C]acetate and the [11C]palmitate products were high (>98% and >99.9%, respectively) with average non-corrected yields of 18% (n=3) and 10% (n=5), respectively.

  4. Clean synthesis of biodiesel over solid acid catalysts of sulfonated mesopolymers

    2010-01-01

    FDU-15-SO3H,a solid acid material prepared from the sulfonation of FDU-15 mesoporous polymer,has been demonstrated to serve as an efficient catalyst in the esterification of palmitic acid with methanol as well as in the transesterification of fatty acid-edible oil mixture.FDU-15-SO3H achieved an acid conversion of 99.0% when the esterification was carried out at 343 K with a methanol/palmitic acid molar ratio of 6:1 and 5 wt% catalyst loading.It was capable of giving 99.0% yield of fatty acid methyl esters (FAME) when the transesterification of soybean oil was performed at 413 K and the methanol/oil weight ratio of 1:1.FDU-15-SO3H was further applied to the transesterification/esterification of the oil mixtures with a varying ratio of soybean oil to palmitic acid,which simulated the feedstock with a high content of free fatty acids.The yield of FAME reached 95% for the oil mixtures containing 30 wt% palmitic acid.This indicated the sulfonated mesopolymer was a potential catalyst for clean synthesis of fuel alternative of biodiesel from the waste oil without further purification.

  5. Paliperidone Palmitate Associated with Necrotizing Deep Tissue Infection and Sepsis Requiring Surgical Intervention

    Jonathan G. Leung

    2015-01-01

    Full Text Available Long-acting injectable antipsychotics provide the delivery of medication over an extended period of time requiring administration typically only every 2 to 4 weeks. The side effect profile of a long-acting injectable antipsychotic is predictable and similar to the oral formulation. However, injection site reactions may occur with this novel delivery system. The risk of an injection site reaction may be greater with the repeated administration of a lipophilic decanoate formulation and include pain, development of indurations, and fibrosis. Severe complications from injection site reactions have rarely been described in the literature with newer agents. We report the first case of a patient prescribed paliperidone palmitate every 3 weeks that developed severe sepsis requiring vasopressors and intubation due to delayed relayed recognition of a necrotizing infection at an injection site. Clinicians should be alerted to screen for injection site reactions when there is an unknown source infection in a patient receiving a long-acting injectable antipsychotic.

  6. Paliperidone Palmitate Associated with Necrotizing Deep Tissue Infection and Sepsis Requiring Surgical Intervention

    Leung, Jonathan G.; Kooda, Kirstin J.; Frazee, Erin N.; Nelson, Sarah; Moore, Katherine M.

    2015-01-01

    Long-acting injectable antipsychotics provide the delivery of medication over an extended period of time requiring administration typically only every 2 to 4 weeks. The side effect profile of a long-acting injectable antipsychotic is predictable and similar to the oral formulation. However, injection site reactions may occur with this novel delivery system. The risk of an injection site reaction may be greater with the repeated administration of a lipophilic decanoate formulation and include pain, development of indurations, and fibrosis. Severe complications from injection site reactions have rarely been described in the literature with newer agents. We report the first case of a patient prescribed paliperidone palmitate every 3 weeks that developed severe sepsis requiring vasopressors and intubation due to delayed relayed recognition of a necrotizing infection at an injection site. Clinicians should be alerted to screen for injection site reactions when there is an unknown source infection in a patient receiving a long-acting injectable antipsychotic. PMID:26843999

  7. Changes in lipid composition, fatty acid profile and lipid oxidative stability during Cantonese sausage processing.

    Qiu, Chaoying; Zhao, Mouming; Sun, Weizheng; Zhou, Feibai; Cui, Chun

    2013-03-01

    Lipid composition, fatty acid profile and lipid oxidative stability were evaluated during Cantonese sausage processing. Free fatty acids increased with concomitant decrease of phospholipids. Total content of free fatty acids at 72 h in muscle and adipose tissue was 7.341 mg/g and 3.067 mg/g, respectively. Total amount of saturated, monounsaturated and polyunsaturated fatty acids (SFA, MUFA, and PUFA) in neutral lipid exhibited a little change during processing, while the proportion of PUFA significantly decreased in the PL fraction. The main triacylglycerols were POO+SLO+OOO, PSO (P = palmitic acid, O = oleic acid, L = linoleic acid, S = stearic acid), and a preferential hydrolysis of palmitic, oleic and linoleic acid was observed. Phosphatidylcholines (PC) and phosphatidylethanolamines (PE) were the main components of phospholipids and PE exhibited the most significant degradation during processing. Thiobarbituric acid values (TBARS) increased while peroxide values and hexanal contents varied during processing. PMID:23273460

  8. Molar extinction coefficients of some fatty acids

    Sandhu, G.K.; Singh, K.; Lark, B.S.;

    2002-01-01

    ) and stearic acid (C18H36O2), has been measured at the photon energies 81, 356, 511, 662, 1173 and 1332 keV. Experimental values for the molar extinction coefficient, the effective atomic number and the electron density have been derived and compared with theoretical calculations. There is good......The attenuation of gamma rays in some fatty acids, viz. formic acid (CH2O2), acetic acid (C2H4O2), propionic acid (C3H6O2), butyric acid (C4H8O2), n-hexanoic acid (C6H12O2), n-caprylic acid (C8H16O2), lauric acid (C12H24O2), myristic acid (C14H28O2), palmitic acid (C16H32O2), oleic acid (C18H34O2...

  9. Fatty acid chemistry of Atrichum undulatum and Hypnum andoi

    Pejin Boris

    2012-01-01

    Full Text Available The fatty acid composition of the moss species Atrichum undulatum (Hedw. P. Beauv. (Polytrichaceae and Hypnum andoi A.J.E. Sm. (Hypnaceae collected in winter time were analyzed by gas chromatography (GC and gas chromatography-mass spectrometry (GC-MS as a contribution to their chemistry. Eight fatty acids were identified in the chloroform/methanol extract 1:1 of A. undulatum (linoleic acid 26.80%, palmitic acid 22.17%, α-linolenic acid 20.50%, oleic acid 18.49%, arachidonic acid 6.21%, stearic acid 3.34%, cis-5,8,11,14,17-eicosapentaenoic acid 1.52% and behenic acid 1.01%, while six fatty acids were found in the same type of extract of H. andoi (palmitic acid 63.48%, erucic acid 12.38%, stearic acid 8.08%, behenic acid 6.26%, lignoceric acid 5.16% and arachidic acid 4.64%. According to this study, the moss A. undulatum can be considered as a good source of both essential fatty acids for humans (linoleic acid and α-linolenic acid during the winter.

  10. Development of Fatty Acid-Producing Corynebacterium glutamicum Strains

    Takeno, Seiki; Takasaki, Manami; Urabayashi, Akinobu; Mimura, Akinori; Muramatsu, Tetsuhiro; Mitsuhashi, Satoshi; Ikeda, Masato

    2013-01-01

    To date, no information has been made available on the genetic traits that lead to increased carbon flow into the fatty acid biosynthetic pathway of Corynebacterium glutamicum. To develop basic technologies for engineering, we employed an approach that begins by isolating a fatty acid-secreting mutant without depending on mutagenic treatment. This was followed by genome analysis to characterize its genetic background. The selection of spontaneous mutants resistant to the palmitic acid ester s...

  11. Analysis of fatty acids in selected Macedonian edible oils

    Ivanova, Violeta; Mitrev, Sasa; Leitner, Erich; Lankmayr, Ernst; Siegmund, Barbara; Stafilov, Trajče

    2015-01-01

    The fatty acid composition of few Macedonian edible oils, including sunflower, pumpkin seed, flax, rapeseed and sesame seeds, was determined using GC-FID analysis after derivatisation with BF3-methanolic solution. Six different types of fatty acids (FAs) were found in the oils samples. Palmitic acid (C16:0) and stearic acid (C18:0) were common in all saturates. Myristic acid (C14:0) was present in the sunflower and pumpkin seed oil. Oleic acid (C18:1), linoleic acid (C18:2) and -linolenic (C...

  12. Total Oil Content and Fatty Acid Profile of some Almond (Amygdalus Communis L. Cultivars

    Yildirim Adnan Nurhan

    2016-07-01

    Full Text Available This study was conducted to determine the total oil contents and fatty acid compositions of some commercial almond cultivars. The total oil contents changed significantly (p<0.05 by year in all cultivars with the exception of cultivar Ferrastar. Total oil contents were changed from 50.90% (Picantili to 62.01% (Supernova in 2008 and from 52.44% (Lauranne to 63.18% (Cristomorto in 2009. While predominant unsaturated fatty acids were oleic and linoleic acids, predominant saturated fatty acid was palmitic acid. The highest amount of oleic acid was obtained in Glorieta in both 2008 (83.35% and 2009 (72.74%. Linoleic acid content varied by year and the highest content was recorded in Picantili (26.08% in 2008 and Yaltinski (30.01% in 2009. The highest amount of palmitic acid was detected in cultivar Sonora in both years, i.e. as 7.76% in 2008 and 10.11% in 2009. The mean UFA:SFA ratio was 11.73 in 2008 but 7.59 in 2009. Principal component (PC analysis indicated that palmitic acid, palmitoleic acid, stearic acid, oleic acid, arachidic acid, unsaturated fatty acid (UFA, saturated fatty acid (SFA and UFA:SFA ratio were primarily responsible for the separation on PC1

  13. Caveolar fatty acids and acylation of caveolin-1.

    Qian Cai

    Full Text Available PURPOSE: Caveolae are cholesterol and sphingolipids rich subcellular domains on plasma membrane. Caveolae contain a variety of signaling proteins which provide platforms for signaling transduction. In addition to enriched with cholesterol and sphingolipids, caveolae also contain a variety of fatty acids. It has been well-established that acylation of protein plays a pivotal role in subcellular location including targeting to caveolae. However, the fatty acid compositions of caveolae and the type of acylation of caveolar proteins remain largely unknown. In this study, we investigated the fatty acids in caveolae and caveolin-1 bound fatty acids. METHODS: Caveolae were isolated from Chinese hamster ovary (CHO cells. The caveolar fatty acids were extracted with Folch reagent, methyl esterificated with BF3, and analyzed by gas chromatograph-mass spectrometer (GC/MS. The caveolin-1 bound fatty acids were immunoprecipitated by anti-caveolin-1 IgG and analyzed with GC/MS. RESULTS: In contrast to the whole CHO cell lysate which contained a variety of fatty acids, caveolae mainly contained three types of fatty acids, 0.48 µg palmitic acid, 0.61 µg stearic acid and 0.83 µg oleic acid/caveolae preparation/5 × 10(7 cells. Unexpectedly, GC/MS analysis indicated that caveolin-1 was not acylated by myristic acid; instead, it was acylated by palmitic acid and stearic acid. CONCLUSION: Caveolae contained a special set of fatty acids, highly enriched with saturated fatty acids, and caveolin-1 was acylated by palmitic acid and stearic acid. The unique fatty acid compositions of caveolae and acylation of caveolin-1 may be important for caveolae formation and for maintaining the function of caveolae.

  14. Effectiveness of Paliperidone Palmitate vs. Haloperidol Decanoate for Maintenance Treatment of Schizophrenia: A Randomized Clinical Trial

    McEvoy, Joseph P.; Byerly, Matthew; Hamer, Robert M.; Dominik, Rosalie; Swartz, Marvin S.; Rosenheck, Robert A.; Ray, Neepa; Lamberti, J. Steven; Buckley, Peter F.; Wilkins, Tania M.; Stroup, T. Scott

    2014-01-01

    Importance Long-acting injectable (LAI) antipsychotics are used to reduce medication non-adherence and subsequent relapse in schizophrenia-spectrum disorders. The relative effectiveness of LAI versions of second-generation (atypical) and older antipsychotics has not been assessed. Objective To compare the effectiveness of the second-generation LAI antipsychotic paliperidone palmitate (PP) to the older LAI antipsychotic haloperidol decanoate (HD). Design, Setting, and Participants Multisite, double-blind, randomized clinical trial conducted at 22 clinical research sites in the U.S. The 311 randomized patients (PP=157, HD=154) were adults diagnosed with schizophrenia or schizoaffective disorder who were clinically assessed to be at risk of relapse and likely to benefit from a LAI antipsychotic. Interventions Intramuscular injections of HD 25–200 mg or PP 39–234 mg every month for up to 24 months. Main Outcome Measures Efficacy failure, which reflected inadequate control of psychopathology by the study medication, as determined by a blinded adjudication committee. Key secondary outcomes were common adverse effects of antipsychotic medications. Results There was no statistically significant difference in the rate of efficacy failure for PP compared to HD (adjusted hazard ratio 0.98, 95% confidence interval [CI] 0.65–1.47). On average, patients on PP gained and those on HD lost weight; after six months the least squares mean weight change on PP was +2.17 kg (1.25 to 3.09) and on HD was −0.96 kg (−1.88 to −0.04). Patients taking PP had significantly greater increases in serum prolactin (men 34.56 µg/L (29.75 to 39.37) vs. 15.41 (10.73 to 20.08), p<0.001; women 75.19 (63.03 to 87.36) vs. 26.84 (13.29 to 40.40), p<0.001). Patients taking HD had significantly larger increases in global ratings of akathisia (0.73 [0.59 to 0.87] vs. 0.45 [0.31 to 0.59], p=0.006). Conclusions and Relevance Among adults with schizophrenia or schizoaffective disorder, treatment with

  15. CD36 Mediated Fatty Acid-Induced Podocyte Apoptosis via Oxidative Stress.

    Wei Hua

    Full Text Available Hyperlipidemia-induced apoptosis mediated by fatty acid translocase CD36 is associated with increased uptake of ox-LDL or fatty acid in macrophages, hepatocytes and proximal tubular epithelial cells, leading to atherosclerosis, liver damage and fibrosis in obese patients, and diabetic nephropathy (DN, respectively. However, the specific role of CD36 in podocyte apoptosis in DN with hyperlipidemia remains poorly investigated.The expression of CD36 was measured in paraffin-embedded kidney tissue samples (Ctr = 18, DN = 20 by immunohistochemistry and immunofluorescence staining. We cultured conditionally immortalized mouse podocytes (MPC5 and treated cells with palmitic acid, and measured CD36 expression by real-time PCR, Western blot analysis and immunofluorescence; lipid uptake by Oil red O staining and BODIPY staining; apoptosis by flow cytometry assay, TUNEL assay and Western blot analysis; and ROS production by DCFH-DA fluorescence staining. All statistical analyses were performed using SPSS 21.0 statistical software.CD36 expression was increased in kidney tissue from DN patients with hyperlipidemia. Palmitic acid upregulated CD36 expression and promoted its translocation from cytoplasm to plasma membrane in podocytes. Furthermore, palmitic acid increased lipid uptake, ROS production and apoptosis in podocytes, Sulfo-N-succinimidyloleate (SSO, the specific inhibitor of the fatty acid binding site on CD36, decreased palmitic acid-induced fatty acid accumulation, ROS production, and apoptosis in podocytes. Antioxidant 4-hydroxy-2,2,6,6- tetramethylpiperidine -1-oxyl (tempol inhibited the overproduction of ROS and apoptosis in podocytes induced by palmitic acid.CD36 mediated fatty acid-induced podocyte apoptosis via oxidative stress might participate in the process of DN.

  16. Effect of Whole-Body X-Irradiation of the Synthesis of Individual Fatty Acids in Liver Slices from Normal and Fasted Rats

    Hansen, Heinz Johs. Max; Hansen, Lisbeth Grænge; Faber, M.

    1965-01-01

    (1) Using (2-14C) acetate and (1-14C) butyrate as precursors, rat-liver fatty acids were synthesized in vitro and assayed by paper chromatography. (2) Whole-body x-irradiation induced a change in the synthetic pattern of hepatic fatty acids towards a relatively enhanced synthesis of palmitic acid...

  17. (Vapor + liquid) equilibrium for the binary systems {water + glycerol} and {ethanol + glycerol, ethyl stearate, and ethyl palmitate} at low pressures

    Highlights: → We measured VLE for the binary system {ethyl stearate and palmitate + ethanol}. → The boiling temperatures were obtained using Othmer-type ebuliometer. → The experimental data were modeled using NRTL, UNIQUAC, and UNIFAC models. - Abstract: This work reports the experimental measurements {(vapor + liquid) equilibrium} for the systems {water(1) + glycerol(2)}, {ethanol(1) + glycerol(2)}, {ethanol(1) + ethyl stearate(2)}, and {ethanol(1) + ethyl palmitate(2)}. Boiling temperatures were measured using an Othmer-type ebulliometer over a pressure range of 14 kPa to 96 kPa. The experimental data were well correlated using the NRTL and UNIQUAC models. The performance of the UNIFAC-Dortmund model in relation to predicting the phase equilibrium of the systems was also studied.

  18. The significance of electron spin resonance of the ascorbic acid radical in freeze dried human brain tumours and oedematous or normal periphery.

    Mueller, H. W.; Tannert, S.

    1986-01-01

    The ESR spectrum, attributed to the ascorbic acid (ascorbyl) radical and obtained by exposing freeze dried material to air, can not be used as proof for the occurrence of in vivo free radical reactions. Depending on the method of freeze drying, the content of blood or hemolyzed blood is the dominant factor in creating higher than normal ESR signals in brain or related tissue. These findings explain why the signal, though larger in many human brain tumours than in their surroundings, is not in...

  19. General oxidative stress during doxorubicin-induced cardiotoxicity in rats: absence of cardioprotection and low antioxidant efficiency of alpha-lipoic acid.

    Ghibu, Steliana; Delemasure, Stéphanie; Richard, Carole; Guilland, Jean-Claude; Martin, Laurent; Gambert, Ségolène; Rochette, Luc; Vergely, Catherine

    2012-01-01

    To evaluate the effects of alpha-lipoic acid (AL) in a model of doxorubicin (DOX)-induced cardiotoxicity, male Wistar rats were treated with DOX (1 mg/kg/d; 10 d) in combination or not with AL (50 mg/kg/d; 15 d). Plasma oxidative stress was determined by hydroperoxides (ROOH) and the ascorbyl radical/ascorbate ratio. One and two months later, the functional parameters of the hearts were determined in vivo by catheterization and cardiac oxidative stress was assessed by malonedialdehyde (MDA) a...

  20. Long-acting paliperidone palmitate – interim results of an observational study of its effect on hospitalization

    Taylor, David; Olofinjana, Olubanke

    2014-01-01

    Paliperidone palmitate (PP) is a recently introduced long-acting atypical, or second-generation, antipsychotic. Published data on PP are currently limited to controlled trials and case reports. In this observational study, we followed up 200 consecutive patients prescribed PP in normal practice. After 1 year, 65% of patients were still receiving PP. The number of admissions to hospital in the year following PP initiation was 0.49/patient compared with 0.69/patient/year, 3 years before initiat...

  1. Body mass index and metabolic parameters in patients with schizophrenia during long-term treatment with paliperidone palmitate

    Sliwa, Jennifer Kern; Fu, Dong-Jing; Bossie, Cynthia A.; Turkoz, Ibrahim; Alphs, Larry

    2014-01-01

    Background There is a strong association between weight gain and metabolic events in patients with schizophrenia receiving many of the second-generation antipsychotic agents. We explored the relationship between body mass index (BMI) and metabolic events in patients with schizophrenia receiving long-acting injectable paliperidone palmitate (PP) in a long-term trial. Methods We conducted a post hoc analysis of data from a PP study that included a 33-week open-label transition (TR) and maintena...

  2. Methylphenidate for the treatment of erectile dysfunction induced by long acting injectable paliperidone palmitate: a case report

    ng chong guan; koh ong hui; jesjeet singh gill

    2013-01-01

    Erectile dysfunction is one of the common sexual adverse effects encountered in male patients treated with antipsychotics. It is associated with prolactin secretion secondary to dopamine antagonism by the antipsychotics. Methylphenidate is a psychostimulant that inhibits the reuptake of dopamine. In this case, we report a 42 year old schizophrenic male, who developed erectile dysfunction after administration of a long acting injectable antipsychotic, namely paliperidone palmitate. The erectil...

  3. Long-term tolerability of once-monthly injectable paliperidone palmitate in subjects with recently diagnosed schizophrenia

    Sliwa, Jennifer Kern; Bossie, Cynthia A.; Fu, Dong-Jing; Turkoz, Ibrahim; Alphs, Larry

    2012-01-01

    Background A post hoc analysis from a multiphase trial with open-label transition and maintenance phases, a double-blind relapse prevention phase, and an optional open-label extension examined the long-term tolerability with continuous once-monthly injectable paliperidone palmitate 39, 78, 117, or 156 mg (25, 50, 75, or 100 mg equivalents [mg eq] of paliperidone) in subjects with recently diagnosed (≤5 years; n = 216) versus chronic illness (>5 years; n = 429) schizophrenia. Methods Adverse e...

  4. Expansion of guidance for the day 8 initiation dose of paliperidone palmitate to avoid a missed dose

    Samtani MN; Nuamah I; Gopal S; Remmerie B; Sliwa JK; Alphs L

    2013-01-01

    Mahesh N Samtani,1 Isaac Nuamah,1 Srihari Gopal,1 Bart Remmerie,2 Jennifer Kern Sliwa,3 Larry Alphs31Janssen Research and Development, LLC, NJ, USA; 2Janssen Research and Development, LLC, Division of Janssen Pharmaceutica NV, Beerse, Belgium; 3Janssen Scientific Affairs, LLC, NJ, USABackground: Paliperidone palmitate (PP) is a long-acting injectable formulation of an atypical antipsychotic, paliperidone. Its dose can be expressed in milligram or milligram equivalents (mg eq) of active palipe...

  5. Number needed to treat and number needed to harm with paliperidone palmitate relative to long-acting haloperidol, bromperidol, and fluphenazine decanoate for treatment of patients with schizophrenia

    Srihari Gopal

    2011-03-01

    Full Text Available Srihari Gopal1, Joris Berwaerts1, Isaac Nuamah1, Kasem Akhras2, Danielle Coppola1, Ella Daly1, David Hough1, Joseph Palumbo11Johnson & Johnson Pharmaceutical Research & Development, LLC, Raritan, NJ, USA; 2Johnson & Johnson Pharmaceutical Services, LLC, Raritan, NJ, USABackground: We analyzed data retrieved through a PubMed search of randomized, placebo-controlled trials of first-generation antipsychotic long-acting injectables (haloperidol decanoate, bromperidol decanoate, and fluphenazine decanoate, and a company database of paliperidone palmitate, to compare the benefit-risk ratio in patients with schizophrenia.Methods: From the eight studies that met our selection criteria, two efficacy and six safety parameters were selected for calculation of number needed to treat (NNT, number needed to harm (NNH, and the likelihood of being helped or harmed (LHH using comparisons of active drug relative to placebo. NNTs for prevention of relapse ranged from 2 to 5 for paliperidone palmitate, haloperidol decanoate, and fluphenazine decanoate, indicating a moderate to large effect size.Results: Among the selected maintenance studies, NNH varied considerably, but indicated a lower likelihood of encountering extrapyramidal side effects, such as akathisia, tremor, and tardive dyskinesia, with paliperidone palmitate versus placebo than with first-generation antipsychotic depot agents versus placebo. This was further supported by an overall higher NNH for paliperidone palmitate versus placebo with respect to anticholinergic use and Abnormal Involuntary Movement Scale positive score. LHH for preventing relapse versus use of anticholinergics was 15 for paliperidone palmitate and 3 for fluphenazine decanoate, favoring paliperidone palmitate.Conclusion: Overall, paliperidone palmitate had a similar NNT and a more favorable NNH compared with the first-generation long-acting injectables assessed.Keywords: long-acting injectables, first-generation antipsychotics

  6. Palmitate Luciferin: A molecular design for the second harmonic generation study of ion complexation at the air-water interface

    A molecular organic chromophore, Palmitate-Luciferin, has been synthesized for studying ion complexation at the air-water interface using second harmonic generation (SHG). This molecule was designed through the addition of a long hydrophobic palmitoyl alkyl chain to the aromatic π-electron system of Luciferin. We first demonstrate that this organic chromophore is a potential candidate for SHG studies of ion complexation with the measurement of its first hyper-polarizability in aqueous solutions by hyper Rayleigh scattering (HRS) with and without calcium ions. Then, we characterize the Palmitate-Luciferin surfactant properties at the air-water interface combining surface tension measurements with a surface SHG study and Brewster angle imaging. These results allow us to build a molecular description of the chromophore at the interface and observe its molecular reorganization during the monolayer compression leading to the formation of aggregates. Finally, we show that the initial goal of the designing work is achieved since Palmitate-Luciferin indeed exhibits a higher SHG response in the presence of calcium ions in the aqueous sub-phase as expected. (authors)

  7. Satisfaction of immediate or delayed switch to paliperidone palmitate in patients unsatisfied with current oral atypical antipsychotics.

    Kwon, Jun Soo; Kim, Sung Nyun; Han, Jaewook; Lee, Sang Ick; Chang, Jae Seung; Choi, Jung-Seok; Lee, Heon-Jeong; Cho, Seong Jin; Jun, Tae-Youn; Lee, Seung-Hwan; Han, Changsu; Lee, Kyoung-Uk; Lee, Kyung Kyu; Lee, EunJung

    2015-11-01

    Patient satisfaction with treatment is an important clinical index associated with the efficacy and adherence of treatment in schizophrenia. Although switching from oral antipsychotics to the long-acting injectable formulation may improve convenience, patient satisfaction has not been studied extensively. We carried out a 21-week, multicenter, randomized, open-label comparative study. A total of 154 patients with schizophrenia unsatisfied with current oral atypical antipsychotics were assigned randomly to either immediate or delayed switching to paliperidone palmitate, the long-acting injectable formulation of paliperidone. The Medication Satisfaction Questionnaire (MSQ) and the Treatment Satisfaction Questionnaire for Medication (TSQM) were used to evaluate patient satisfaction with treatment, whereas the Positive and Negative Syndrome Scale (PANSS) and the Personal and Social Performance (PSP) scale were used to evaluate efficacy. From baseline to the final assessment, the MSQ score increased significantly in both groups, and the increase was greatest after the first administration of paliperidone palmitate in the immediate switch group. The scores of TSQM effectiveness, convenience, and global satisfaction as well as the PSP total score increased significantly, whereas the PANSS total score decreased significantly in both groups. The immediate switch group showed a significant improvement in the TSQM convenience score compared with the delayed switch group on oral antipsychotics during the comparison period. Most adverse events were minor and tolerable. In short, switching from oral atypical antipsychotics to paliperidone palmitate because of poor satisfaction significantly improved patient satisfaction, with comparable efficacy and tolerability. PMID:26196188

  8. Glucose and Palmitate Differentially Regulate PFKFB3/iPFK2 and Inflammatory Responses in Mouse Intestinal Epithelial Cells

    Botchlett, Rachel; Li, Honggui; Guo, Xin; Qi, Ting; Zhao, JiaJia; Zheng, Juan; Woo, Shih-Lung; Pei, Ya; Liu, Mengyang; Hu, Xiang; Chen, Guang; Guo, Ting; Yang, Sijun; Li, Qifu; Xiao, Xiaoqiu; Huo, Yuqing; Wu, Chaodong

    2016-01-01

    The gene PFKFB3 encodes for inducible 6-phosphofructo-2-kinase, a glycolysis-regulatory enzyme that protects against diet-induced intestine inflammation. However, it is unclear how nutrient overload regulates PFKFB3 expression and inflammatory responses in intestinal epithelial cells (IECs). In the present study, primary IECs were isolated from small intestine of C57BL/6J mice fed a low-fat diet (LFD) or high-fat diet (HFD) for 12 weeks. Additionally, CMT-93 cells, a cell line for IECs, were cultured in low glucose (LG, 5.5 mmol/L) or high glucose (HG, 27.5 mmol/L) medium and treated with palmitate (50 μmol/L) or bovine serum albumin (BSA) for 24 hr. These cells were analyzed for PFKFB3 and inflammatory markers. Compared with LFD, HFD feeding decreased IEC PFKFB3 expression and increased IEC proinflammatory responses. In CMT-93 cells, HG significantly increased PFKFB3 expression and proinflammatory responses compared with LG. Interestingly, palmitate decreased PFKFB3 expression and increased proinflammatory responses compared with BSA, regardless of glucose concentrations. Furthermore, HG significantly increased PFKFB3 promoter transcription activity compared with LG. Upon PFKFB3 overexpression, proinflammatory responses in CMT-93 cells were decreased. Taken together, these results indicate that in IECs glucose stimulates PFKFB3 expression and palmitate contributes to increased proinflammatory responses. Therefore, PFKFB3 regulates IEC inflammatory status in response to macronutrients. PMID:27387960

  9. A comparison of retinyl palmitate and red palm oil β-carotene as strategies to address Vitamin A deficiency.

    Souganidis, Ellie; Laillou, Arnaud; Leyvraz, Magali; Moench-Pfanner, Regina

    2013-08-01

    Vitamin A deficiency continues to be an international public health problem with several important health consequences including blindness and overall increased rates of morbidity and mortality. To address this widespread issue, a series of strategies have been put into place from dietary diversification to supplementation and fortification programs. Retinyl palmitate has been used successfully for decades as a supplement as well as a way to fortify numerous foods, including vegetable oil, rice, monosodium glutamate, cereal flours and sugar. Recently, there has been rising interest in using a natural source of carotenoids, β-carotene from red palm oil (RPO), for fortification. Although RPO interventions have also been shown to effectively prevent Vitamin A deficiency, there are numerous challenges in using beta-carotene from RPO as a fortification technique. β-Carotene can induce significant changes in appearance and taste of the fortified product. Moreover, costs of fortifying with beta-carotene are higher than with retinyl palmitate. Therefore, RPO should only be used as a source of Vitamin A if it is produced and used in its crude form and regularly consumed without frying. Furthermore, refined RPO should be fortified with retinyl palmitate, not β-carotene, to ensure that there is adequate Vitamin A content. PMID:23955382

  10. A Comparison of Retinyl Palmitate and Red Palm Oil β-Carotene as Strategies to Address Vitamin A Deficiency

    Regina Moench-Pfanner

    2013-08-01

    Full Text Available Vitamin A deficiency continues to be an international public health problem with several important health consequences including blindness and overall increased rates of morbidity and mortality. To address this widespread issue, a series of strategies have been put into place from dietary diversification to supplementation and fortification programs. Retinyl palmitate has been used successfully for decades as a supplement as well as a way to fortify numerous foods, including vegetable oil, rice, monosodium glutamate, cereal flours and sugar. Recently, there has been rising interest in using a natural source of carotenoids, β-carotene from red palm oil (RPO, for fortification. Although RPO interventions have also been shown to effectively prevent Vitamin A deficiency, there are numerous challenges in using beta-carotene from RPO as a fortification technique. β-Carotene can induce significant changes in appearance and taste of the fortified product. Moreover, costs of fortifying with beta-carotene are higher than with retinyl palmitate. Therefore, RPO should only be used as a source of Vitamin A if it is produced and used in its crude form and regularly consumed without frying. Furthermore, refined RPO should be fortified with retinyl palmitate, not β-carotene, to ensure that there is adequate Vitamin A content.

  11. Paliperidone Palmitate Once-Monthly Injectable Treatment for Acute Exacerbations of Schizoaffective Disorder.

    Fu, Dong-Jing; Turkoz, Ibrahim; Simonson, R Bruce; Walling, David; Schooler, Nina; Lindenmayer, Jean-Pierre; Canuso, Carla; Alphs, Larry

    2016-08-01

    The optimal treatment for schizoaffective disorder (SCA) is not well established. In this initial 6-month open-label treatment period of a large, multiphase, relapse-prevention study, the efficacy and safety of paliperidone palmitate once-monthly (PP1M) injectable were evaluated in subjects with symptomatic SCA. Subjects with acute exacerbation of SCA (ie, with psychotic and either depressive and/or manic symptoms) were enrolled and treated with PP1M either as monotherapy or in combination with antidepressants or mood stabilizers (combination therapy group). After flexible-dose treatment with PP1M for 13 weeks, stabilized subjects continued into a 12-week fixed-dose PP1M treatment period. A total of 667 subjects were enrolled; 320 received monotherapy and 347 received PP1M as combination therapy; 334 subjects completed the entire 25-week treatment. Statistically significant and clinically meaningful improvements from baseline were observed for all efficacy measures in psychosis (per Positive and Negative Syndrome Scale), mood symptoms (per Young Mania Rating Scale and Hamilton Depression Rating Scale-21 items), and functioning (per Personal and Social Performance Scale) from week 1 to all time points during the 25-week treatment period (P acute exacerbation of SCA provided rapid, broad, and persistent reduction in psychotic, depressive, and manic symptoms, as well as improved functioning. PMID:27322760

  12. Pharmacokinetic profile after multiple deltoid or gluteal intramuscular injections of paliperidone palmitate in patients with schizophrenia.

    Rossenu, Stefaan; Cleton, Adriaan; Hough, David; Crauwels, Herta; Vandebosch, An; Berwaerts, Joris; Eerdekens, Marielle; Herben, Virginie; De Meulder, Marc; Remmerie, Bart; Francetic, Igor

    2015-07-01

    Paliperidone palmitate (PP) is a once-monthly long-acting injectable antipsychotic approved for the treatment of schizophrenia in many countries. To evaluate the different injection-site options, we compared the pharmacokinetic profile of paliperidone after multiple injections of PP 100 mg eq. (156 mg of PP, equivalent to 100 mg of paliperidone) on days 1, 8, 36, and 64 into the deltoid (n = 24) or gluteal muscle (n = 25) in patients with schizophrenia. After four injections in the deltoid muscle, paliperidone exposure was higher for AUCτ and Cmax , compared with the gluteal muscle (geometric mean AUCτ -based ratio: 120% [90% CI: 93.1-154.7%], and geometric mean Cmax -based ratio: 130% [90% CI: 100.6-168.9%]). The mean [SD] fluctuation index was higher, with a larger interpatient variability, after deltoid-injections (75.9% [30.9%]) than gluteal-injections (58.5% [14.3%]). The median tmax was similar for both sites. PP was generally tolerable in patients, with more favorable local-site tolerability for gluteal-injection. In conclusion, to achieve therapeutic-concentrations quickly, the first-two injections of PP are best administered into the deltoid muscle, whereas thereafter maintenance-injections can be administered either in the deltoid or gluteal muscle. PMID:27136907

  13. A retrospective observational study of the effectiveness of paliperidone palmitate on acute inpatient hospitalization rates.

    Bressington, Daniel; Stock, Jon; Hulbert, Sabina; MacInnes, Douglas

    2015-07-01

    This retrospective mirror-image observational study aimed to establish the effects of the long-acting antipsychotic injection paliperidone palmitate (PP) on acute inpatient hospitalization rates. We utilized routinely collected clinical data to compare the number and length of acute patient admissions 1 year before and 1 year after initiation of PP. A single cohort of 66 patients with a diagnosis of schizophrenia and who had received monthly injections of PP for at least 1 year were included in the analysis. The mean number of acute inpatient admissions fell from 0.86 in the year before PP initiation to 0.23 in the following year (P = 0.001), and there was a numerical but nonsignificant decrease in the number of bed days from 32.48 to 31.22 over the study duration. The median number of bed days in the year before PP initiation was 20, and in the year after initiation it was 0. The median number of admissions also fell from 1 to 0 during the same period. The results of the study should be treated cautiously because of the limitations of the study design but suggest that patients with a diagnosis of schizophrenia who continue treatment with PP over 12 months experience a significant reduction in hospital admissions compared with the previous year. PMID:25882381

  14. Anti-Oxidative Activity of Pectin and Its Stabilizing Effect on Retinyl Palmitate

    Ro, Jieun; Kim, Yeongseok; Kim, Hyeongmin; Jang, Soung Baek; Lee, Hyun Joo; Chakma, Suharto

    2013-01-01

    The purpose of this study was to examine the anti-oxidative activity of pectin and other polysaccharides in order to develop a cosmeceutical base having anti-oxidative effects towards retinyl palmitate (RP). The anti-oxidative stabilizing effects of pectin and other polysaccharides on RP were evaluated by DPPH assay and then the stabilizing effect of pectin on RP was examined as a function of time. Among the polysaccharides we examined, pectin exhibited a considerably higher anti-oxidative activity, with an approximately 5-fold greater DPPH radical scavenging effect compared to other polysaccharides. The DPPH radical scavenging effect of pectin increased gradually with increasing concentrations of pectin. At two different RP concentrations, 0.01 and 0.1% in ethanol, addition of pectin improved the stability of RP in a concentration dependent manner. The stabilizing effect of pectin on RP was more effective for the lower concentration of RP (0.01%, v/v). Further, degradation of RP was reduced following the addition of pectin as measured over 8 hours. From the results obtained, it can be suggested that pectin may be a promising ingredient for cosmeceutical bases designed to stabilize RP or other pharmacological agents subject to degradation by oxidation. PMID:23776395

  15. Encapsulation of Vitamin A palmitate for animal supplementation: Formulation, manufacturing and stability implications.

    Albertini, Beatrice; Di Sabatino, Marcello; Calogerà, Giacomo; Passerini, Nadia; Rodriguez, Lorenzo

    2010-01-01

    Two manufacturing methods and numerous formulative approaches have been evaluated to obtain a stable oral pharmaceutical form of Vitamin A palmitate (VAP), a substance very sensitive to light, temperature, humidity and metal ions. The best results were obtained by formulating VAP, stabilized with butylated hydroxytoluene (BHT), in double layer microcapsules constituted by a core of chitosan, Tween 20, CaCl(2) and EDTA surrounded by a first chitosan-alginate membrane and an outer membrane of calcium-alginate. This formulation design enabled the production of beads with high drug loading (42% w/w) and high encapsulation efficiency (94%). The stability of VAP-loaded microcapsules was assessed according to EMEA guidelines. This formulation design showed the best performance in terms of VAP recovery (t(50%) > 360 days) after 1 year of storage at room conditions. This is a very important result considering the poor shelf-life (45 days) of pure VAP stabilized with BHT stored at the same conditions. PMID:19538031

  16. Analysis of embryo, cytoplasm and maternal effects on fatty acid components in soybean (Glycine max Merill.)

    NING Hailong; LI Wenxia; LI Wenbin

    2007-01-01

    The quality of oil determined by the constituents and proportion of fatty acid components,and the understanding of heredity of fatty acid components are of importance to breeding good quality soybean varieties.Embryo,cytoplasmic and maternal effects and genotype×environment interaction effects for quality traits of soybean [Glycine max (L.) Merrill.] seeds were analyzed using a general genetic model for quantitative traits of seeds with parents,F1 and F2,of 20 crosses from a diallel mating design of five parents planted in the field in 2003 and 2004 in Harbin,China.The interaction effects of palmitic,stearic,and linoleic acid contents were larger than the genetic main effects,while the genetic main effects were equal to interaction effects for linolenic and oleic acid content.Among all kinds of genetic main effects,the embryo effects were the largest for palmitic,stearic,and linoleic acids,while the cytoplasm effects were the largest for oleic and linolenic acids.Among all kinds of interaction effects,the embryo interaction effects were the largest for fatty acids.The sum of additive and additive× environment effects were larger than that of dominance and dominance×environment effects for the linolenic acid content,but not for other quality traits.The general heritabilities were the main parts of heritabilities for palmitic and oleic acid contents,but the interaction was more important for stearic,linoleic,and linolenic acid contents.For the general heritability,maternal and cytoplasm heritabilities were the main components for palmitic,oleic,and linolenic acid contents.It was shown for the interaction heritabilities that the embryo interaction heritabilities were more important for oleic and linolenic acid contents,while the maternal interaction heritabilities were more important for linoleic acid content.Among selection response components,the maternal and cytoplasm general responses and/or interaction responses were more important for palmitic

  17. Study of the Synthesis of L - ascorbyl - 2 - triphosphate with Asscorbic Acid and Hexmetaphosphate%六偏磷酸钠与Vc合成Vc多聚磷酸酯

    金显春; 赵敏; 王锦堂

    2003-01-01

    报导了Vc与六偏磷酸钠在水介质中合成Vc多聚磷酸酯(LAPP)的方法,研究了不同反应条件对LAPP产率与质量的影响.当Vc/六偏磷酸钠/催化剂(物质的量比)=1:1.30:0.15,溶液pH=9时LAPP的收率为85.6%.

  18. Efficacy, safety, and impact on hospitalizations of paliperidone palmitate in recent-onset schizophrenia

    Zhang F

    2015-03-01

    Full Text Available Fan Zhang,1 Tianmei Si,2,3 Chiun-Fang Chiou,4 Anthony WF Harris,5 Chang Yoon Kim,6 Padmashree Jahagirdar,7 Steve Ascher8 1Xian Janssen Pharmaceuticals, Beijing, People’s Republic of China; 2Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Beijing, People’s Republic of China; 3Key Laboratory of Mental Health, Ministry of Health (Peking University, Beijing, People’s Republic of China; 4Janssen Asia-Pacific, Singapore; 5Discipline of Psychiatry, Sydney Medical School, University of Sydney, Australia and Brian Dynamics Center, Westmead Millennium Institute for Medical Research, Westmead, NSW, Australia; 6Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea; 7Theorem Clinical Research, Bangalore, India; 8Janssen Research and Development, LLC, Titusville, NJ, USA Objective: To evaluate the efficacy, safety, and impact on hospitalizations of long-acting injectable paliperidone palmitate (PP treatment, in patients with recent-onset schizophrenia who had not responded satisfactorily to oral antipsychotics.Methods: In this 18-month, open-label, Phase-IIIb study from Asia-Pacific region, patients (18–50 years with recent-onset (≤5 years schizophrenia unsatisfactorily treated with previous oral antipsychotics were initiated on PP 150 mg eq on day 1, 100 mg eq on day 8, followed by flexible once monthly maintenance doses of 50–150 mg eq. The number and duration of hospitalizations were compared using a mirror analysis method between two periods: retrospective (12 months before PP initiation and prospective (12 and 18 months after PP treatment periods.Results: A total of 303 out of 521 (58% patients (mean age, 28.7 years; 65.5% men, 92.5% Asian completed the study. Positive and Negative Syndrome Scale (PANSS total score improved significantly from baseline to month 18 (mean [standard deviation, SD] change: -11.3 [21.38], P<0.0001, primary endpoint. Subgroup analysis revealed

  19. Paliperidone Palmitate and Metabolic Syndrome in Patients With Schizophrenia: A 12-Month Observational Prospective Cohort Study.

    Rosso, Gianluca; Pessina, Enrico; Martini, Azzurra; Di Salvo, Gabriele; Maina, Giuseppe

    2016-06-01

    Oral and long-acting injectable second-generation antipsychotics are known to be associated with a high risk of metabolic adverse effects. Together with other drug treatments, poor lifestyle choices, and genetic liability, they contribute to development of metabolic syndrome (MetS), which occurs in nearly one third of patients with schizophrenia.The primary objective of this multicenter prospective observational study was to explore the prevalence of MetS in a sample of 60 real-world patients treated with paliperidone palmitate (PP) over a period of 12 months. The secondary objectives were to assess other tolerability aspects and the efficacy of PP on schizophrenic symptoms.The proportion of patients with MetS at baseline (33%) did not significantly change neither at 6 (39.0%) nor at 12 months (29.5%) of PP treatment. The same applies to each individual component of MetS. We found a slight but statistically significant increase in body mass index (26.3 ± 6.0 vs 27.1 ± 4.6, P = 0.031) and of waist circumference (98.2 ± 17.9 vs 100.3 ± 15.9, P = 0.021) from baseline to end point. Weight gain was detected in approximately 15% of patients.At least 1 mild or moderate adverse event was found in 71.3%, 88.0%, and 52.1% of patients, respectively, at baseline, 6 months, and 12 months. A significant improvement in schizophrenic symptoms emerged by means of Positive and Negative Syndrome Scale total and subscale scores.Together with previous literature findings, our results seem to indicate that PP could be a valid therapeutic option for patients with a severe disorder and with a high metabolic risk profile. PMID:27043122

  20. Photomutagenicity of retinyl palmitate by ultraviolet a irradiation in mouse lymphoma cells.

    Mei, Nan; Xia, Qingsu; Chen, Ling; Moore, Martha M; Fu, Peter P; Chen, Tao

    2005-11-01

    Retinyl palmitate (RP), a storage form of vitamin A, is frequently used as a cosmetic ingredient, with more than 700 RP-containing cosmetic products on the U.S. market in 2004. There are concerns for the possible genotoxicity and carcinogenicity of RP when it is exposed to sunlight. To evaluate the photomutagenicity of RP in cells when exposed to ultraviolet A (UVA) light, L5178Y/Tk+/- mouse lymphoma cells were treated with different doses of RP alone/or in the presence of UVA light. Treatment of the cells with RP alone at the dose range of 25-100 microg/ml did not increase mutant frequencies (MFs) over the negative control, whereas treatment of cells with 1-25 microg/ml RP under UVA light (82.8 mJ/cm2/min for 30 min) produced a dose-dependent mutation induction. The mean induced MF (392 x 10(-6)) for treatment with 25 microg/ml RP under UVA exposure was about threefold higher than that for UVA alone (122 x 10(-6)), a synergistic effect. To elucidate the underlying mechanism of action, we examined the mutants for loss of heterozygosity (LOH) at four microsatellite loci spanning the entire chromosome 11, on which the Tk gene is located. The mutational spectrum for the RP + UVA treatment was significantly different from the negative control, but not significantly different from UVA exposure alone. Ninety four percent of the mutants from RP + UVA treatment lost the Tk+ allele, and 91% of the deleted sequences extended more than 6 cM in chromosome length, indicating clastogenic events affecting a large segment of the chromosome. These results suggest that RP is photomutagenic in combination with UVA exposure in mouse lymphoma cells, with a clastogenic mode-of-action. PMID:16107546

  1. L-Ascorbyl-2-phosphate attenuates NF-κB signaling in SZ95 sebocytes without affecting IL-6 and IL-8 secretion.

    Ikeno, Hiroshi; Apel, Mara; Zouboulis, Christos; Luger, Thomas A; Böhm, Markus

    2015-09-01

    Acne is the most common inflammatory skin disease. Interleukin-1 (IL-1) is at the beginning of the cytokine signaling cascade and may be involved in the pathogenesis of this disorder. It activates redox-sensitive transcription factors, which induce IL-6 and IL-8 expression. Interestingly, L-ascorbyl-2-phosphate (APS) was shown to have beneficial effects in patients with acne vulgaris. The mechanism of action of this agent remains unknown. Here, we investigated if APS attenuates IL-1β- or TNF-α-mediated IL-6 and IL-8 expression in SZ95 sebocytes, whereas TNF-α was used as control. We also explored NF-κB activation which is known to orchestrate IL-1β- and TNF-α-mediated cytokine expression in many cell types. Both IL-1β and TNF-α increased IL-6 and IL-8 mRNA expression in SZ95 sebocytes. However, only IL-1β induced IL-6 and IL-8 secretion. IL-1β but not TNF-α activated NF-κB canonical signaling as demonstrated by Iκ-Bα phosphorylation and degradation as well as by nuclear accumulation of NF-κB/p65. Concomitant treatment of SZ95 sebocytes with APS attenuated the effect of IL-1β and TNF-α on IL-6 and IL-8 gene expression as well as on IL-1β-mediated NF-κB signaling. In contrast, APS failed to reduce IL-1β-mediated IL-6 and IL-8 secretion, presumably by maintained IL-1β-mediated p38 activation, which is known to control IL-8 secretion. Our findings shed light into the impact of IL-1β on the inflammatory cytokine response and its molecular mechanisms in human sebocytes. Our data further suggest that the beneficial effect of APS in acne patients involves attenuation of NF-κB signaling but not reduction of IL-6 or IL-8 secretion. PMID:25894228

  2. 抗坏血酸磷酸酯镁及熊果苷的检测方法进展%Advances in detection method of magnesium ascorbyl phosphate and arbutin

    杨园园; 郁荣华; 李勤; 周泽琳

    2014-01-01

    Whitening mechanism and effects on the human body of magnesium ascorbyl phosphate and arbutin are introduced in this paper. The various detection methods currently used for magnesium ascorbyl phosphate and arbutin were summarized, compared and analyzed. The common detection method is liquid chromatography, which can detect five whitening ingredients containing magnesium ascorbyl phosphate and arbutin;in addition, GC/MS and LC/MS/MS method can also detect arbutin, and the detection limit and recov-ery are better than HPLC. The mass spectrometry and simultaneous detection of multiple components will be the mainstream in the future.%本文简要介绍了近年应用十分广泛的美白成分抗坏血酸磷酸酯镁及熊果苷的作用机制以及对人体的影响,综述了目前采用的多种检测方法,并对各种检测方法进行比较及分析。目前较为常用的检测方法为液相色谱法,可以同时检测包含抗坏血酸磷酸酯镁及熊果苷在内的五种美白成分;另外,气相色谱-质谱联用法以及液相色谱-质谱联用法也能够检测熊果苷,而且能得到更低的检出限和较高的回收率,灵敏度高,能提高分析效率。但是由于方法中流动相、检测基质等因素,仍需进一步完善改进检测方法。综合上述方法考虑,质谱联用以及同时检测多种成分是今后美白成分检测的主要发展方向。

  3. Variation in fatty acids composition including trans fat in different brands of potato chips by GC-MS

    Twelve different brands of potato chips were analyzed for their fatty acid compositions with eminence on trans fatty acid (TFA) using GC-MS. Results of the present study showed that the dominant fatty acids were saturated fatty acids. Among the saturated fatty acids, palmitic acid (23.91.42.64 %) was found in greater amount in all analyzed chips samples. The amount of TFA's determined was ranged between (4.91.14.13 %). Although there was significant variation in the fatty acid profile of all analyzed chips samples but high amount of palmitic acid and trans fat was commonly observed. The results of present study clearly indicated fat used in the manufacturing of chips was partially hydrogenated and palm oil had major contribution. The high level of trans as well as saturated fat is startling issue for the health of consumers. (author)

  4. Variation in Fatty Acids Composition Including Trans Fat in Different Brands of Potato Chips by GC-MS

    Aftab A. Kandhro

    2010-06-01

    Full Text Available Twelve different brands of potato chips were analyzed for their fatty acid compositions with eminence on trans fatty acid (TFA using GC-MS. Results of the present study showed that the dominant fatty acids were saturated fatty acids. Among the saturated fatty acids, palmitic acid (23.91–42.64 % was found in greater amount in all analyzed chips samples. The amount of TFA’s determined was ranged between (4.91–14.13 %. Although there was significant variation in the fatty acid profile of all analyzed chips samples but high amount of palmitic acid and trans fat was commonly observed. The results of present study clearly indicated fat used in the manufacturing of chips was partially hydrogenated and palm oil had major contribution. The high level of trans as well as saturated fat is startling issue for the health of consumers.

  5. Propylenated fatty acids as emulsifiers

    El-Shattory, Y.; Aly, Saadia M.; Megahed, M. G.

    1999-01-01

    Hydroxy propylenyl stéarate, palmitate, laurate, oléate and linoleate were prepared by reaction of propylene oxide with fatty acid at 160 °C for five hours stirring in presence of potassium hydroxide as a catalyst. Physico-chemical properties of the five products, regarding their use as emulsifiers, were determined.

    Se prepararon estearato, palmitato, laurato, oleato y linoleato de hidroxipropilenilos mediante reacción de oxido de propileno con ácido graso a 160 °C durante ...

  6. Direct Free Fatty Acid Storage in Different Sized Adipocytes from the Same Depot

    Rajjo, Tamim I.; Harteneck, Debra A.; Jensen, Michael D.

    2014-01-01

    Objective Human adipocytes take up free fatty acids (FFA) directly from the circulation, even at times of high lipolytic activity. Whether these processes occurs simultaneously within the same cells or are partitioned between different cells, for example large and small cells, is unknown. Design and Methods We measured direct FFA storage in subcutaneous fat in 13 adults using a continuous infusion of [U-13C]palmitate and a bolus of [1-14C]palmitate followed 30 min later by abdominal and femor...

  7. High levels of fatty acids increase contractile function of neonatal rabbit hearts during reperfusion following ischemia.

    Ito, Masayoshi; Jaswal, Jagdip S; Lam, Victoria H; Oka, Tatsujiro; Zhang, Liyan; Beker, Donna L; Lopaschuk, Gary D; Rebeyka, Ivan M

    2010-05-01

    In the neonatal heart the transition from using carbohydrates to using fatty acids has not fully matured and oxidative metabolism/ATP generation may be limiting contractile function after ischemia. This study tested the hypothesis that increasing fatty acid availability increases recovery of left ventricular (LV) work by increasing palmitate oxidation, tricarboxylic acid (TCA) cycle activity, and ATP generation. Isolated working hearts from 7-day-old rabbits were perfused with Krebs solution containing low (0.4 mM) or high (2.4 mM) palmitate and 5.5 mM glucose. Hearts were subjected to 35-min global ischemia before 40-min reperfusion, and rates of glycolysis, glucose oxidation, and palmitate oxidation were assessed. LV work was similar before ischemia but was greater during reperfusion in hearts perfused with 2.4 mM palmitate compared with hearts perfused with 0.4 mM palmitate [6.98 +/- 0.14 (n = 15) vs. 3.01 +/- 0.23 (n = 16) mJ.beat(-1).g dry wt(-1); P < 0.05]. This was accompanied by increased LV energy expenditure during reperfusion [35.98 +/- 0.16 (n = 8) vs. 19.92 +/- 0.18 (n = 6) mJ.beat(-1).g dry wt(-1); P < 0.05]. During reperfusion the rates of palmitate oxidation [237.5 +/- 28.10 (n = 7) vs. 86.0 +/- 9.7 (n = 6) nmol.g dry wt(-1).min(-1); P < 0.05], total TCA cycle activity [2.65 +/- 0.39 (n = 7) vs. 1.36 +/- 0.14 (n = 6) micromol acetyl-CoA.g dry wt(-1).min(-1); P < 0.05], and ATP generation attributable to palmitate oxidation [26.6 +/- 3.1 (n = 7) vs. 12.6 +/- 1.7 (n = 6) micromol.g dry wt(-1).min(-1); P < 0.05] were greater in hearts perfused with 2.4 mM palmitate. These data indicate that the neonatal heart has decreased energy reserve, and, in contrast to the mature heart, increasing availability of fatty acid substrate increases energy production and improves recovery of function after ischemia. PMID:20154256

  8. Micro method for determination of nonesterified fatty acid in whole blood obtained by fingertip puncture

    Hansen, Jesper Søndergaard; Munk, Jens; Gaster, Michael;

    2006-01-01

    background fluorescence reading, NEFAs were converted to acyl-CoA by the acyl-CoA synthetase and the NEFA content was calculated from fluorescence emission changes using palmitic acid as external standard. The FACI-50 NEFA method was compared with two commercially available methods for quantification of NEFA....

  9. The effect of carbohydrate and fat variation in euenergetic diets on postabsorptive free fatty acid release

    Bisschop, PH; Ackermans, MT; Endert, E; Ruiter, AFC; Meijer, AJ; Kuipers, F; Sauerwein, HP; Romijn, JA

    2002-01-01

    Diet composition and energy content modulate free fatty acid (FFA) release. The aim of this study was to evaluate the dose-response effects of euenergetic variations in dietary carbohydrate and fat content on postabsorptive FFA release. The rate of appearance (R-a) of palmitate was measured by infus

  10. The stereospecific triacylglycerol structures and fatty acid profiles of human milk and infant formulas

    Straarup, Ellen Marie; Lauritzen, L.; Færk, Jan;

    2006-01-01

    Background: The stereospecific structures of the triacylglycerol molecules in human milk differ from that of cow's milk and vegetable oils, which are the fat sources used in infant formula. In human milk, palmitic acid (16:0) is predominantly esterified in the sn2 position, whereas vegetable oils...

  11. Survey of SSC12 regions affecting fatty acid composition of intramuscular fat using high density SNP data

    María eMuñoz

    2012-01-01

    Full Text Available Fatty acid composition is a critical aspect of pork because it affects sensorial and technological aspects of meat quality and it is relevant for human health. Previous studies identified significant QTLs in porcine chromosome 12 for fatty acid profile of backfat and intramuscular fat. In the present study, 374 SNPs mapped in SSC12 from the 60K Porcine SNP Beadchip were used. We have combined linkage and association analyses with expression data analysis in order to identify regions of SSC12 that could affect fatty acid composition of intramuscular fat in longissimus muscle. The QTL scan showed a region around the 60 cM position that significantly affects palmitic fatty acid and two related fatty acid indexes. The Iberian QTL allele increased the palmitic content (+2.6% of mean trait. This QTL does not match any of those reported in the previous study on fatty acid composition of backfat, suggesting different genetic control acting at both tissues. The SNP association analyses showed significant associations with linolenic and palmitic acids besides several indexes. Among the polymorphisms that affect palmitic fatty acid and match the QTL region at 60 cM, there were three that mapped in the Phosphatidylcholine Transfer Protein (PCTP gene and one in the Acetyl-CoA Carboxylase  gene (ACACA. Interestingly one of the PCTP SNPs also affected significantly unsaturated and double bound indexes and the ratio between polyunsaturated/monounsaturated fatty acids. Differential expression was assessed on longissimus muscle conditional on the genotype of the QTL and on the most significant SNPs, according to the results obtained in the former analyses. Results from the microarray expression analyses, validated by RT-qPCR, showed that PCTP expression levels significantly vary depending on the QTL as well as on the own PCTP genotype. The results obtained with the different approaches point out the PCTP gene as a powerful candidate underlying the QTL for

  12. Comparative Transcriptome Analysis of Three Oil Palm Fruit and Seed Tissues That Differ in Oil Content and Fatty Acid Composition

    Dussert, Stéphane; Guerin, Chloe; Andersson, Mariette; JOET, THIERRY; Tranbarger, Timothy J.; Pizot, Maxime; Gautier, Sarah; Omore, Alphonse; Durand-Gasselin, Tristan; Morcillo, Fabienne

    2013-01-01

    Oil palm (Elaeis guineensis) produces two oils of major economic importance, commonly referred to as palm oil and palm kernel oil, extracted from the mesocarp and the endosperm, respectively. While lauric acid predominates in endosperm oil, the major fatty acids (FAs) of mesocarp oil are palmitic and oleic acids. The oil palm embryo also stores oil, which contains a significant proportion of linoleic acid. In addition, the three tissues display high variation for oil content at maturity. To g...

  13. Long-term tolerability of once-monthly injectable paliperidone palmitate in subjects with recently diagnosed schizophrenia

    Sliwa JK; Bossie CA; Fu D-J; Turkoz I; Alphs L

    2012-01-01

    Jennifer Kern Sliwa,1 Cynthia A Bossie,1 Dong-Jing Fu,1 Ibrahim Turkoz,2 Larry Alphs11Janssen Scientific Affairs LLC, 2Janssen Research and Development, LLC, Titusville, NJ, USABackground: A post hoc analysis from a multiphase trial with open-label transition and maintenance phases, a double-blind relapse prevention phase, and an optional open-label extension examined the long-term tolerability with continuous once-monthly injectable paliperidone palmitate 39, 78, 117, or 156 mg (25, 50, 75, ...

  14. The fatty acids and alkanes of Satureja adamovicii Silic and Satureja fukarekii Silic (NOTE

    DUSANKA KITIC

    1999-05-01

    Full Text Available The content and composition of fatty acids and alkanes of Satureja adamovicii Silic and Satureja fukarekii Silic were analized by GC. It was found that unsaturated acids prevailed and that the major components were palmitic, oleic, linoleic and linolenic acids. The hydrocarbon fractions of pentane extracts were shown to consist of the alkane homologues (C17 to C34 with nonacosane and hentriacontane being prevailing compounds.

  15. Solder Flux Residues and Humidity-Related Failures in Electronics: Relative Effects of Weak Organic Acids Used in No-Clean Flux Systems

    Verdingovas, Vadimas; Jellesen, Morten Stendahl; Ambat, Rajan

    2015-01-01

    This paper presents the results of humidity testing of weak organic acids (WOAs), namely adipic, succinic, glutaric, dl-malic, and palmitic acids, which are commonly used as activators in no-clean solder fluxes. The study was performed under humidity conditions varying from 60% relative humidity...

  16. Cross linkage studies with the membranes of the vesicular stomatitis virus using radioactive 4-acido and 5-acido palmitic acid

    In the study described here the spatial arrangement of lipids and proteins in the VS virus was investigated on the basis of the covalent cross linkage technique. The formation of such cross linkages is brought about by the action of photosensitive acidosubstituted lipids, which permit acido functions to be introduced into a membrane in a previously defined position. Subsequently, photolysis helps to trigger the generation of radioactive nitrenes that react with the proteins and lipids in their immediate vicinity in a direct and non-selective way. The findings revealed by this study have raised questions as to the possibility of lipid-protein and lipid-lipid interactions, which is also discussed. (orig./MG)

  17. 硬脂酸中棕榈酸和硬脂酸的GC法测定%Determination of Palmitic Acid and Stearic Acid in Stearic Acid by GC

    邱颖姮

    2010-01-01

    建立了GC法测定硬脂酸中的棕榈酸和硬脂酸.以聚乙二醇(PEG)为固定相,采用程序升温,进样口温度250℃,检测器温度260℃,分流比30:1,载气为氮气.棕榈酸和硬脂酸在0.5~4 mg/ml浓度范围内与峰面积线性关系良好;回收率为100.3%和100.2%,RSD均为0.9%.

  18. 维A酸维生素C棕榈酸酯泡囊的体外释放、经皮渗透和皮肤贮留研究%Study on the Release Rate, in Vitro Skin Penetration and Retention of Tretinoin Ascorbyl Palmitate Vesicles

    陈正明; 龙晓英; 丁钢; 袁飞

    2010-01-01

    目的 研究维生素C棕榈酸酯泡囊作为维A酸载体时,主药的体外释放、经皮渗透和皮肤贮留情况.方法 采用Franz扩散池测定维A酸从载体中的释放速度,扩散池与供给池之间为纤维素膜(截留分子量8 000~14 000),扩散池面积为2.92 cm2.体外透皮试验用小鼠、大鼠或兔子背部皮肤替代半透膜.在体外透皮试验完结后,取下皮肤,剪碎匀浆,用50%异丙醇-生理盐水提取,提取液处理后用HPLC测定药物浓度.结果 结果 表明维A酸释放速率和累积经皮渗透量大于市售乳膏,同时具有较高的皮肤贮留量.结论 维生素C棕榈酸酯泡囊作为维A酸载体有助于增加局部药物浓度.

  19. Incorporation of [14C]-palmitate into lipids of Brassica cells during the induction of freezing tolerance

    Changes in plasma membrane lipid composition have been causally related to increased freezing tolerance. Studies of lipid metabolism during ABA induction of freezing tolerance in Brassica napus suspension cultures were undertaken. Cells were labeled with [14C]-palmitate four days after transfer to fresh medium (control) or medium containing ABA (which increases freezing tolerance). At times between one and 20 hrs after labeling, ABA-treated cells incorporated almost twice the amount of label as controls cells. Approximately 80% of the radioactivity was associated with neutral lipids in ABA-treated cells and controls. Incorporation of label into total cellular polar lipids was 4.9 x 105 dpm/mg protein for control cells and 1 x 106 dpm/mg protein for cells transferred to medium containing ABA. Analysis of lipids following alkaline hydrolysis indicated that incorporation of [14C]-palmitate into glucosylceramide of ABA-treated cells was less than 60% of control values when expressed relative to that of the total polar lipids. Incorporation into ceramides was also depressed in ABA-treated cells

  20. Modeling the budget impact of long-acting injectable paliperidone palmitate in the treatment of schizophrenia in Japan

    Mahlich J

    2015-05-01

    Full Text Available Jörg Mahlich,1,2 Masamichi Nishi,3 Yoshimichi Saito11Health Economics, Janssen Pharmaceutical KK, Tokyo, Japan; 2Düsseldorf Institute for Competition Economics, University of Düsseldorf, Düsseldorf, Germany; 3Pricing, Janssen Pharmaceutical KK, Tokyo, JapanBackground: The cost of schizophrenia in Japan is high and new long-acting injectable (LAI antipsychotics might be able to reduce costs by causing a reduction of hospital stays. We aim to estimate budget effects of the introduction of a new 1-month LAI, paliperidone palmitate, in Japan.Methods: A budget impact analysis was conducted from a payer perspective. The model took direct costs of illness into account (ie, costs for inpatient and outpatient services, as well as drug costs. The robustness of the model was checked using a sensitivity analysis.Results: According to our calculations, direct total costs of schizophrenia reach 710,500 million yen a year (US$6 billion. These costs decrease to 691,000 million yen (US$5.9 billion 3 years after the introduction of paliperidone palmitate.Conclusion: From a payer point of view, the introduction of a new treatment for schizophrenia in Japan helps to save resources and is not associated with a higher financial burden.Keywords: budget impact, schizophrenia, long-acting injectables, paliperidone, Japan

  1. Study on Synergies of Natural Antioxidants and their Antioxidation Functions on Peanut Oil%天然抗氧化剂的增效作用及其对花生油抗氧化效果研究

    黄克; 崔春; 赵谋明; 马浩

    2012-01-01

    Rosmarinus officinalis extract, tea polyphenol, phytic acid, ascorbyl palmitate and vitamin E were selected to prepare natural antioxidant compound for peanut oil due to their antioxidant capacities. The induction time of peanut oil added various antioxidant was tested by Rancimat method. According to the range analysis of orthogonal test design results, the contributions of 4 natural antioxidants to antioxidation were ranked in turn as : Rosmarinus officinalis extract>tea polyphenol >phytic acid>ascorbyl palmitate, and the optimum formula of the natural antioxidant compound was as follows: Rosmarinus officinalis extract 0.07%,tea polyphenol 0.03%,phytic acid 0.02% and ascorbyl palmitate 0.02%. The antioxidant capacity of this compound was higher than that of TBHQ.%对迷迭香提取物、荼多酚、植酸、VE、抗坏血酸棕榈酸酯在花生油中的抗氧化性能和五种天然抗氧化剂相互之间的增效作用进行了研究.通过Rancimat法测定了添加各种抗氧剂的花生油的诱导时间,根据正交实验结果,各种天然抗氧化剂在组分中的主次因素为迷迭香提取物>茶多酚>植酸>抗坏血酸棕榈酸酯,优化得出天然抗氧化剂的复配配方为迷迭香提取物0.07%、茶多酚0.03%、植酸0.02%、抗坏血酸棕榈酸酯0.02%.此配方对花生油的抗氧化能力优于TBHQ.

  2. Fatty Acids Composition of Vegetable Oils and Its Contribution to Dietary Energy Intake and Dependence of Cardiovascular Mortality on Dietary Intake of Fatty Acids

    Jana Orsavova; Ladislava Misurcova; Jarmila Vavra Ambrozova; Robert Vicha; Jiri Mlcek

    2015-01-01

    Characterizations of fatty acids composition in % of total methylester of fatty acids (FAMEs) of fourteen vegetable oils—safflower, grape, silybum marianum, hemp, sunflower, wheat germ, pumpkin seed, sesame, rice bran, almond, rapeseed, peanut, olive, and coconut oil—were obtained by using gas chromatography (GC). Saturated (SFA), monounsaturated (MUFA) and polyunsaturated fatty acids (PUFA), palmitic acid (C16:0; 4.6%–20.0%), oleic acid (C18:1; 6.2%–71.1%) and linoleic acid (C18:2; 1.6%–79%)...

  3. Tolerability of initiation doses of once-monthly paliperidone palmitate in patients with recently diagnosed schizophrenia in an acute treatment trial

    Bossie, Cynthia A; Fu, Dong-Jing; Sliwa, Jennifer Kern; Alphs, Larry; Ma, Yi-Wen

    2011-01-01

    Objective: To examine the tolerability of the recommended initiation doses for once-monthly injectable paliperidone palmitate in patients who have recently been diagnosed with schizophrenia and for whom high doses may pose tolerability concerns. Methods: A post hoc analysis from a 13-week double-blind study of patients with schizophrenia randomized 1:1:1:1 to placebo or paliperidone palmitate at 25, 100, or 150 mg equivalents (mg eq) of paliperidone (corresponding to 39, 156, or 234 mg respec...

  4. Amino acid peroxyl radicals. Formation and reaction with ascorbate

    Complete text of publication follows. Proteins are significant targets for partly reduced oxygen species in vivo. This results in random formation of radicals on the amino acid residues (AA·) of the protein, which in turn, in the presence of oxygen, can yield the corresponding peroxyl radicals (AAOO·). Both radical types can cause further biological damage. We studied the N-acetylamide derivatives of the amino acids glycine, alanine and proline as models of these residues in proteins. We generated the amino acid radicals specifically by reaction with hydroxyl radicals produced in solutions irradiated with 2 MeV electrons in the presence of N2O. In the absence of oxygen the amino acid radicals decayed with rate constants in the narrow range (0.9-1.3) x 109 M-1s-1, while in the presence of oxygen they were converted very rapidly to the corresponding peroxyl radicals with rate constants that vary between 6.3 x 108 and 5.5 x 109 M-1s-1, depending on the amino acid. The corresponding N-acetylated amino acids were also studied and showed similar behaviour but with slightly smaller rate constants. Antioxidants are able to repair tyrosyl and tryptophanyl radicals in various proteins in vitro. For ascorbate, the principal endogenous biological antioxidant, we have measured rate constants in the range 105-108 M-1s-1. The peroxyl radicals of all amino acids studied here were reduced by oxidizing ascorbate to the ascorbyl radical. The reaction was followed at 360 nm, where ascorbyl radical has an absorption coefficient of 3300 M-1cm-1, and the derived rate constants were all close to 107 M-1s-1. However, the spontaneous decay of peroxyl radicals is also fast and competes with the reaction with ascorbate. It is to be stressed that reaction of AAOO· and ascorbate gives rise to hydroperoxides (AAOOH) that are also reactive molecules. Our study suggests that reaction with protein radicals may be responsible for the ascorbate loss reported in organisms exposed to oxidative

  5. Comparison of fatty acid composition in total lipid of diapause and non-diapause larvae of Cydia pomonella (Lepidoptera: Tortricidae)

    ABBAS KHANI; SAEID MOHARRAMIPOUR; MOHSEN BARZEGAR; HOSSEIN NADERI-MANESH

    2007-01-01

    Seasonal changes in the fatty acid composition of the total lipid extracted from the whole body of Cydia pomonella L. larvae were determined by gas chromatography. The six most abundant fatty acids in both non-diapause and diapause larvae of codling moth were oleic (35%-39%), palmitic (23%-33%), linoleic (16%-30%), palmitoleic (5%-10%),stearic (1.5%-3.0%) and linolenic acids (1.0%-2.5%). This represents a typical complement of Lepidopteran fatty acids. The fatty acid composition of total lipid of C. pomonella larvae was related to diapause. In similarity to most other reports, the proportion of unsaturated fatty acids increased in diapause initiation state. The total lipid of diapause larvae contained more linoleic acid (25.8% vs. 16.1%) and less palmitic acid (24.7% vs. 33.4%),than that ofnon-diapause larvae. The weight percentage of linoleic acid (C18:2) increased from 16% to 26% from early-August through early-September during transition to diapause,while palmitic acid (C16:0) decreased from 33% to 25% at the same time. These changes resulted in an increase in the ratio of unsaturated to saturated fatty acids (UFA/SFA) from 1.72 in non-diapause larvae to 2.63 in diapause larvae.

  6. Influence of dietary vitamin C dosage on turbot (Scophthalmus maximus) and European sea bass (Dicentrarchus labrax) nursery stages

    Merchie, G.; Lavens, P.; Storch, V.; Übel, U.; Nelis, H.; De leenheer, A P; Sorgeloos, P.

    1996-01-01

    Stable forms of vitamin C were verified as dietary sources of ascorbic acid (AA) for the nursery stages of European sea bass and turbot. In a first experiment, various concentrations of ascorbyl palmitate (AP) and one level of AA 2-polyphosphate (ApP) were evaluated in a semi purified diet for European sea bass, Dicentrarchus labrax. A significantly lower AA concentration was detected in the fry fed the AP-supplemented diets compared to the ApP-fed group, providing evidence that AP is an infe...

  7. Activity and viability of methanogens in anaerobic digestion of unsaturated and saturated long-chain fatty acids

    Sousa, D.Z.; Salvador, A.F.; Ramos, J.; Guedes, A.P.; Barbosa, S.; Stams, A.J.M.; Alves, M.M.; Pereira, M.A.

    2013-01-01

    Lipids can be anaerobically digested to methane, but methanogens are often considered to be highly sensitive to the long-chain fatty acids (LCFA) deriving from lipids hydrolysis. In this study, the effect of unsaturated (oleate [C18:1]) and saturated (stearate [C18:0] and palmitate [C16:0]) LCFA tow

  8. Amino and Fatty Acids of Wild Edible Mushrooms of the Genus Boletus

    Dmitri O. Levitsky

    2010-10-01

    Full Text Available A comparative study on the free amino acids of 15 wild edible mushroom species belonging to the genus Boletus (phylum Basidiomycota was developed. The major amino acids in the fruit bodies were arginine , alanine, glutamine, and glutamic acid. The most abundant fatty acids were oleic ( 9- 18:1, linoleic acid (9,12-18:2 , and palmitic acid (16:0, but a great variation of the ester composition from one to another one was found. Chemical constituents were characterized by GC-MS, and other chemical methods.

  9. Fatty Acids Analysis, Antioxidant and Biological Activity of Fixed Oil of Annona muricata L. Seeds

    Elagbar, Zaha A.; Rajashri R. Naik; Ashok K. Shakya; Bardaweel, Sanaa K

    2016-01-01

    The total oil yield and the fatty acid composition were determined in the Annona muricata L. fixed oil using organic solvent extraction and GC-FID. The seeds were found to contain about ~21.5% of crude fixed oil on a dry weight basis. The crude oil containing fatty acid was converted into methyl esters and analysed by GC-FID. Fourteen fatty acids were identified using GC-FID. The major monounsaturated and saturated fatty acids were oleic acid (39.2%) and palmitic acid (19.1–19.2%), respective...

  10. Adaptation of anaerobically grown Thauera aromatica, Geobacter sulfurreducens and Desulfococcus multivorans to organic solvents on the level of membrane fatty acid composition

    Duldhardt, Ilka; Gaebel, Julia; Chrzanowski, Lukasz; Nijenhuis, Ivonne; Härtig, Claus; Schauer, Frieder; Heipieper, Hermann J.

    2010-01-01

    Summary The effect of different solvents and pollutants on the cellular fatty acid composition of three bacterial strains: Thauera aromatica, Geobacter sulfurreducens and Desulfococcus multivorans, representatives of diverse predominant anaerobic metabolisms was investigated. As the prevailing adaptive mechanism in cells of T. aromatica and G. sulfurreducens whose cellular fatty acids patterns were dominated by palmitic acid (C16:0) and palmitoleic acid (C16:1cis), the cells reacted by an inc...

  11. Fatty acid composition, antioxidant and antibacterial properties of the microwave aqueous extract of three varieties of Labisia pumila Benth

    Karimi, Ehsan; Jaafar, Hawa ZE; Ghasemzadeh, Ali; Ebrahimi, Mahdi

    2015-01-01

    Background The present study was conducted in order to evaluate the fatty acid profile, anti-oxidant and anti-bacterial activities from the microwave aqueous extract of the leaves of three different varieties of Labisia pumila Benth. Results The chemical analysis of the extract showed that fatty acids (palmitic, palmitoleic, stearic, oleic, linoleic and α-linolenic) acid as the main components in three varieties of L. pumila leaves. Furthermore, the obtained results of the anti-oxidant reveal...

  12. Temperature induced modulation of lipid oxidation and lipid accumulation in palmitate-mediated 3T3-L1 adipocytes and 3T3-L1 adipocytes.

    Lin, Xiaofen; Li, Yi; Leung, Polly Hangmei; Li, Jiashen; Hu, Junyan; Liu, Xuan; Li, Zhi

    2016-05-01

    Human skin temperature can vary widely depending on anatomical location and ambient temperature. It is also known that local changes in skin and subcutaneous temperature can affect fat metabolism. This study aimed to explore the potential effects of surrounding thermal environment on fat by investigating cell viability, lipid oxidation, and lipid accumulation in 3T3-L1 adipocytes and palmitate-treated adipocytes after 4h incubation. No significant differences of viability in 3T3-L1 adipocytes were detected under different temperature conditions. Despite no significant increase being observed under warm temperature (39°C) conditions, a similarly significant suppression of intracellular reactive oxygen species (ROS) and lipid peroxidation were found in 3T3-L1 adipocytes and palmitate-treated adipocytes under 4h exposure to cooler temperatures of 31-33°C (Psize of lipid droplets in 3T3-L1 adipocytes (Padipocytes. In the palmitate-induced adiposity model, although excessive ROS and lipid peroxidation has been attenuated by temperature decrease (Psize (P>0.05) and remedy the palmitate damage induced cell death (Padipocytes. PMID:27157327

  13. Analysis of all-rac-alpha-tocopheryl acetate and retinyl palmitate in medical foods using a zero control reference material (ZRM) as a method development tool.

    Chase, G W; Eitenmiller, R R; Long, A R

    1999-01-01

    A liquid chromatographic method is described for analysis of all- rac-alpha-tocopheryl acetate and retinyl palmitate in medical food. The vitamins are extracted in isopropyl alcohol and hexane-ethyl acetate without saponification and quantitated by normal-phase chromatography with fluorescence detection. All rac-alpha-tocopheryl acetate and retinyl palmitate are chromatographed isocratically with a mobile phase of 0.5% (v/v) and 0.125% (v/v) isopropyl alcohol in hexane, respectively. Recovery studies performed on a medical food zero control reference material (ZRM) fortified with the analytes averaged 99.7% (n = 25) for retinyl palmitate and 101% (n = 25) for all- rac-alpha-tocopheryl acetate. Coefficients of variation were 0.87-2.63% for retinyl palmitate and 1.42-3.20% for all-rac-alpha-tocopheryl acetate. The method provides a rapid, specific, and easily controlled assay for analysis of vitamin A and vitamin E in medical foods. Use of chlorinated solvents is avoided. PMID:10232898

  14. Red palm oil-supplemented and biofortified gari on the carotenoid and retinyl palmitate concentrations of triacylglycerol-rich plasma of women

    Boiled biofortified cassava containing ß-carotene (BC) can increase retinyl palmitate (RP) in triacylglycerol (TAG)-rich plasma. Thus, it might alleviate vitamin A deficiency. Cassava requires extensive preparation to decrease its level of cyanogenic glucosides, which can be fatal. Garification ...

  15. SIRT1 attenuates palmitate-induced endoplasmic reticulum stress and insulin resistance in HepG2 cells via induction of oxygen-regulated protein 150

    Jung, T.W.; Lee, K.T.; Lee, M.W.; Ka, K.H.

    2012-01-01

    Endoplasmic reticulum (ER) stress has been implicated in the pathology of type 2 diabetes mellitus (T2DM). Although SIRT1 has a therapeutic effect on T2DM, the mechanisms by which SIRT1 ameliorates insulin resistance (IR) remain unclear. In this study, we investigated the impact of SIRT1 on palmitate-induced ER stress in HepG2 cells and its underlying signal pathway. Treatment with resveratrol, a SIRT1 activator significantly inhibited palmitate-induced ER stress, leading to the protection against palmitate-induced ER stress and insulin resistance. Resveratrol and SIRT1 overexpression induced the expression of oxygen-regulated protein (ORP) 150 in HepG2 cells. Forkhead box O1 (FOXO1) was involved in the regulation of ORP150 expression because suppression of FOXO1 inhibited the induction of ORP150 by SIRT1. Our results indicate a novel mechanism by which SIRT1 regulates ER stress by overexpression of ORP150, and suggest that SIRT1 ameliorates palmitate-induced insulin resistance in HepG2 cells via regulation of ER stress.

  16. [Lipid synthesis by an acidic acid tolerant Rhodotorula glutinis].

    Lin, Zhangnan; Liu, Hongjuan; Zhang, Jian'an; Wang, Gehua

    2016-03-01

    Acetic acid, as a main by-product generated in the pretreatment process of lignocellulose hydrolysis, significantly affects cell growth and lipid synthesis of oleaginous microorganisms. Therefore, we studied the tolerance of Rhodotorula glutinis to acetic acid and its lipid synthesis from substrate containing acetic acid. In the mixed sugar medium containing 6 g/L glucose and 44 g/L xylose, and supplemented with acetic acid, the cell growth was not:inhibited when the acetic acid concentration was below 10 g/L. Compared with the control, the biomass, lipid concentration and lipid content of R. glutinis increased 21.5%, 171% and 122% respectively when acetic acid concentration was 10 g/L. Furthermore, R. glutinis could accumulate lipid with acetate as the sole carbon source. Lipid concentration and lipid yield reached 3.20 g/L and 13% respectively with the initial acetic acid concentration of 25 g/L. The lipid composition was analyzed by gas chromatograph. The main composition of lipid produced with acetic acid was palmitic acid, stearic acid, oleic acid, linoleic acid and linolenic acid, including 40.9% saturated fatty acids and 59.1% unsaturated fatty acids. The lipid composition was similar to that of plant oil, indicating that lipid from oleaginous yeast R. glutinis had potential as the feedstock of biodiesel production. These results demonstrated that a certain concentration of acetic acid need not to be removed in the detoxification process when using lignocelluloses hydrolysate to produce microbial lipid by R. glutinis. PMID:27349116

  17. Paliperidone palmitate and risperidone long-acting injectable in subjects with schizophrenia recently treated with oral risperidone or other oral antipsychotics

    Alphs L

    2013-03-01

    Full Text Available Larry Alphs,1 Cynthia A Bossie,1 Jennifer Kern Sliwa,2 Dong-Jing Fu,1 Yi-Wen Ma,3 Joseph Hulihan11CNS Medical Affairs, 2Medical Information, Janssen Scientific Affairs, LLC, Titusville, NJ, USA; 3Biostatistics, B&P, Janssen Research & Development LLC, Titusville, NJ, USABackground: This post hoc subgroup analysis of a randomized, double-blind trial evaluated the response to treatment with two long-acting injectable atypical antipsychotics, ie, paliperidone palmitate and risperidone long-acting injectable (RLAI, in subjects with schizophrenia experiencing clinically significant symptoms despite recent treatment with oral risperidone only or other oral antipsychotics.Methods: Adult subjects were eligible for the 13-week, double-blind, double-dummy trial (NCT00589914 if they had an established diagnosis of schizophrenia for at least one year and a Positive and Negative Syndrome Scale (PANSS total score of 60–120 inclusive at screening. Subjects received either paliperidone palmitate (234 mg, day 1; 156 mg, day 8; then once-monthly flexible dosing or RLAI (25–50 mg biweekly, with oral risperidone supplementation on days 1–28, plus matched placebo injections/tablets.Results: This post hoc analysis reports data on 747 subjects who, within 2 weeks of starting double-blind study medication, had reportedly received oral risperidone only (paliperidone palmitate group, n = 126; RLAI group, n = 107, other oral antipsychotics (paliperidone palmitate group, n = 199; RLAI group, n = 203, or no antipsychotic (paliperidone palmitate group, n = 56; RLAI group, n = 56. Mean PANSS total scores improved significantly at end point across all subgroups (mean change from baseline ranged from −17.5 to −19.5, all P < 0.0001. Clinical Global Impression-Severity and Personal and Social Performance scale measures also significantly improved from baseline (all P < 0.0001.Conclusion: Treatment with paliperidone palmitate or RLAI resulted in a significant reduction

  18. Effect of modern milking technologies and psyhrotrophic microorganisms on fatty acid in milk

    Александра Николаевна Бергилевич

    2014-12-01

    Full Text Available It was found that the milking of cows with robotics has a greater influence on formation of free fatty acids (FFA in milk than automatic milking "Carousel." Among all researched FFA, the largest concentrations in milk were palmitic, oleic and stearic fatty acids. Pseudomonas spp in milk during refrigerated storage secrete lipase, promoting the FFA formation. Adding a solution of H2O2 to raw milk stops the formation of bacterial lipases.

  19. Effect of dietary fatty acids on the postprandial fatty acid composition of triacylglycerol-rich lipoproteins in healthy male subjects

    Bysted, Anette; Holmer, G.; Lund, Pia;

    2005-01-01

    interesterified test fats with equal amounts of palmitic acid ( P fat), stearic acid (S fat), trans-18: 1 isomers (T fat), oleic acid (O fat), or linoleic acid (L fat) were tested. Subjects: A total of 16 healthy, normolipidaemic males ( age 23 +/- 2 y) were recruited. Interventions: The participants ingested fat......Objective: The aim of the present study was to investigate the effect of trans-18: 1 isomers compared to other fatty acids, especially saturates, on the postprandial fatty acid composition of triacylglycerols ( TAG) in chylomicrons and VLDL. Design: A randomised crossover experiment where five......-rich test meals ( 1 g fat per kg body weight) and the fatty acid profiles of chylomicron and VLDL TAG were followed for 8 h. Results: The postprandial fatty acid composition of chylomicron TAG resembled that of the ingested fats. The fatty acids in chylomicron TAG were randomly distributed among the three...

  20. Effect of dietary fatty acids on the postprandial fatty acid composition of triacylglycerol-rich lipoproteins in healthy male subjects

    Bysted, Anette; Holmer, G.; Lund, Pia; Sandstrom, B.; Tholstrup, T.

    2005-01-01

    Objective: The aim of the present study was to investigate the effect of trans-18: 1 isomers compared to other fatty acids, especially saturates, on the postprandial fatty acid composition of triacylglycerols ( TAG) in chylomicrons and VLDL. Design: A randomised crossover experiment where five...... interesterified test fats with equal amounts of palmitic acid ( P fat), stearic acid (S fat), trans-18: 1 isomers (T fat), oleic acid (O fat), or linoleic acid (L fat) were tested. Subjects: A total of 16 healthy, normolipidaemic males ( age 23 +/- 2 y) were recruited. Interventions: The participants ingested fat......-rich test meals ( 1 g fat per kg body weight) and the fatty acid profiles of chylomicron and VLDL TAG were followed for 8 h. Results: The postprandial fatty acid composition of chylomicron TAG resembled that of the ingested fats. The fatty acids in chylomicron TAG were randomly distributed among the three...

  1. Variation in Fatty Acids Composition Including Trans Fat in Different Brands of Potato Chips by GC-MS

    Kandhro, Aftab A.; S.T.H. Sherazi; S.A. Mahesar; M. Younis Talpur; Yawar Latif

    2010-01-01

    Twelve different brands of potato chips were analyzed for their fatty acid compositions with eminence on trans fatty acid (TFA) using GC-MS. Results of the present study showed that the dominant fatty acids were saturated fatty acids. Among the saturated fatty acids, palmitic acid (23.91–42.64 %) was found in greater amount in all analyzed chips samples. The amount of TFA’s determined was ranged between (4.91–14.13 %). Although there was significant variation in the fatty acid profile of all ...

  2. Effect of individual dietary fatty acids on postprandial activation of blood coagulation factor VII and fibrinolysis in healthy young men

    Tholstrup, T.; Miller, G.J.; Bysted, Anette;

    2003-01-01

    Background: Hypertriglyceridemia may represent a procoagulant state involving disturbances to the hemostatic system. Plasminogen activator inhibitor type 1 (PAI-1) is increased in the presence of hypertriglyceridemia. Free fatty acids (FFAs) in plasma may promote factor VII (FVII) activation....... Objective: We tested the hypothesis that FVII activation would be less after consumption of saturated fatty acids than after other fatty acids. Design: The effects of 6 matching dietary test fats, rich in stearic (S), palmitic (P), palmitic + myristic (M), oleic (O), trans 18:1 (T), and linoleic (L) acid......, respectively, on the postprandial lipid and hemostatic profile (after 2, 4, 6, and 8 h) were investigated in 16 young men. High-fat meals (1 g fat/kg body wt; 43% from the test fatty acid) were served in the morning on 6 separate days. Results: All fats increased FVII activation. The S fat resulted in a lower...

  3. Effects of intravenous methyl palmoxirate on the turnover and oxidation of fatty acids in conscious dogs

    Bailey, J.W.; Jensen, M.D.; Miles, J.M. (Mayo Medical School, Rochester, MN (USA))

    1991-04-01

    Methyl palmoxirate (MP) is a member of a class of hypoglycemic agents that inhibit fatty acid oxidation in vitro. The studies presented here were undertaken to determine the effects of intravenous (IV) MP on tracer-determined rates of fatty acid oxidation and systemic adipose tissue lipolysis in dogs. MP (40 mg/kg) was administered IV to five mongrel dogs using a primed continuous infusion of (1-{sup 14}C)palmitate to determine palmitate kinetics. Palmitate concentration and rate of appearance decreased rapidly (from 155 +/- 25 to 47 +/- 6 mumol/L and 2.9 +/- 0.5 to 0.9 +/- 0.2 mumol.kg-1.min-1, respectively, at 15 minutes, both P less than .05). Palmitate oxidation also decreased, from 1.5 +/- 0.4 to 0.3 +/- 0.1 mumol.kg-1.min-1, P less than .05. Oxidative clearance decreased by approximately 50% 90 minutes after MP administration (P less than .05). Fractional oxidation of palmitate also decreased by approximately 40% (P less than .05). Plasma insulin increased from 45 +/- 6 to 240 +/- 93 pmol/L at 15 minutes (P less than .05). Plasma glucose decreased over the course of study by approximately 20% (P less than .05). In summary, MP has a specific inhibitory effect on plasma free fatty acid (FFA) oxidation in dogs, confirming previous in vitro observations in an in vivo model. In addition, it has a potent antilipolytic effect when administered IV, an effect likely mediated by stimulation of insulin secretion. The observation that systemic FFA oxidation was only partially suppressed at this relatively high dose of MP is consistent with previous studies suggesting that MP may exert its major effect in the liver, and may be less potent in extrahepatic tissues.

  4. Effects of intravenous methyl palmoxirate on the turnover and oxidation of fatty acids in conscious dogs

    Methyl palmoxirate (MP) is a member of a class of hypoglycemic agents that inhibit fatty acid oxidation in vitro. The studies presented here were undertaken to determine the effects of intravenous (IV) MP on tracer-determined rates of fatty acid oxidation and systemic adipose tissue lipolysis in dogs. MP (40 mg/kg) was administered IV to five mongrel dogs using a primed continuous infusion of [1-14C]palmitate to determine palmitate kinetics. Palmitate concentration and rate of appearance decreased rapidly (from 155 +/- 25 to 47 +/- 6 mumol/L and 2.9 +/- 0.5 to 0.9 +/- 0.2 mumol.kg-1.min-1, respectively, at 15 minutes, both P less than .05). Palmitate oxidation also decreased, from 1.5 +/- 0.4 to 0.3 +/- 0.1 mumol.kg-1.min-1, P less than .05. Oxidative clearance decreased by approximately 50% 90 minutes after MP administration (P less than .05). Fractional oxidation of palmitate also decreased by approximately 40% (P less than .05). Plasma insulin increased from 45 +/- 6 to 240 +/- 93 pmol/L at 15 minutes (P less than .05). Plasma glucose decreased over the course of study by approximately 20% (P less than .05). In summary, MP has a specific inhibitory effect on plasma free fatty acid (FFA) oxidation in dogs, confirming previous in vitro observations in an in vivo model. In addition, it has a potent antilipolytic effect when administered IV, an effect likely mediated by stimulation of insulin secretion. The observation that systemic FFA oxidation was only partially suppressed at this relatively high dose of MP is consistent with previous studies suggesting that MP may exert its major effect in the liver, and may be less potent in extrahepatic tissues

  5. Starch aerogel beads obtained from inclusion complexes prepared from high amylose starch and sodium palmitate

    Starch aerogels are a class of low density highly porous renewable materials currently prepared from retrograded starch gels and are of interest for their good surface area, porosity, biocompatibility, and biodegradability. Recently, we have reported on starches containing amylose-fatty acid salt h...

  6. Oxidative stability of structured lipid-based infant formula emulsion: effect of antioxidants.

    Zou, Long; Akoh, Casimir C

    2015-07-01

    The effect of permitted antioxidants, including α-tocopherol, β-carotene, ascorbyl palmitate, ascorbic acid, citric acid, and their combinations, on the lipid oxidation of structured lipid (SL)-based infant formula (IF) was evaluated. The 3.5% oil-in-water IF emulsion was formulated with a human milk fat analogue enriched with docosahexaenoic acid and stearidonic acid, and the antioxidants were added at 0.005% and 0.02% of the oil. The peroxide value, anisidine value, and hexanal concentration of emulsion samples were measured over a 28-day period. The results showed that whether a compound exhibited antioxidant behavior depended on its mechanism of action, polarity, concentration, and environmental conditions. The most effective antioxidant was ascorbyl palmitate at 0.005%, and a synergistic antioxidant effect was found between α-tocopherol and β-carotene. A high correlation was observed between anisidine value and hexanal content. Our findings have important implications for the successful incorporation of SL into IF products for infant nutrition and health. PMID:25704676

  7. 一锅法合成反-β-正烷氧羰基丙烯酸-6-L-抗坏血酸酯及其性能研究%One-pot synthesis of 6-L-ascorbyl trans-β-n-alkoxycarbonyl acrylates and their properties

    郑大贵; 祝显虹; 周安西; 张勇

    2014-01-01

    A general one-pot procedure was described that converted trans-β-n-alkoxycarbonyl( C1-C8 n-alkoxycarbonyl) acrylic acid (1a-1h)to 6-L-ascorbyl trans-β-n-alkoxycarbonyl acrylates(2a-2h) upon sequential treatment of the acid in N,N-dimethylacet-amide(DMAc)with thionyl chloride and L-ascorbic acid. The structures of 2a-2h were confirmed by 1H NMR、13C NMR、MS and IR. The scavenging activity of 2f on DPPH free-radical was tested by UV-Vis spectrophotometry,and the anti-microbial activities of 2a-2h were tested by peptide-agarose diffusion assay. It was fond that when the molar concentration of the tested samples was the same,the scavenging activity on DPPH radical(1,1-Diphenyl-2-picrylhydrazyl radical)of 2f was a little higher than that of L-ascor-bic acid and TBHQ(Tertiary butylhydroquinone)at higher concentration range. The diameters of antibacterial active ring of 2a-2h against Staphyloccocus aureus,Escherichia coli and Bacillus subtilis were between 5. 00-6. 25 mm,and those of 2a-2h against Streptomyces microflavus were between 15. 50-17. 25 mm,when the concentration of tested samples were in 2 mg·mL-1 .%在N,N-二甲基乙酰胺(DMAc)中,反-β-正烷氧羰基丙烯酸(1a-1h,a-h分别对应于C1-C8正烷氧羰基)与SOCl2在0℃下反应,生成的酰氯不经分离,采用一锅法,直接与L-抗坏血酸反应得到反-β-正烷氧羰基丙烯酸-6-L-抗坏血酸酯(2a-2h)。2a-2h的结构经1 H NMR、13 C NMR、MS和IR确证。用分光光度法测试了2f清除二苯代苦味肼基自由基(DPPH·)的活性,用孔穴扩散法测试了2a-2h的抗菌活性。结果表明,受试物摩尔浓度相等时,在较高浓度范围内,2f对DPPH·的清除率略高于L-抗坏血酸和叔丁基对苯二酚(TBHQ);在给药量2 mg·mL-1时,2a-2h对金黄葡萄球菌、大肠杆菌、枯草芽孢杆菌的抑菌圈直径在5.00-6.25 mm之间,对细黄链霉菌的抑菌圈直径在15.50-17.25 mm之间。

  8. Vitamin C derivatives as new coreactants for tris(2,2'-bipyridine)ruthenium(II) electrochemiluminescence

    Yuan Yali; Li Haijuan; Han Shuang; Hu Lianzhe [State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin 130022 (China); Graduate University of the Chinese Academy of Sciences, Beijing 100864 (China); Parveen, Saima [State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin 130022 (China); Graduate University of the Chinese Academy of Sciences, Beijing 100864 (China); Department of Chemistry, Baghdad-ul-Jadeed Campus, The Islamia University of Bahawalpur, Bahawalpur (Pakistan); Xu Guobao, E-mail: guobaoxu@ciac.jl.cn [State Key Laboratory of Electroanalytical Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun, Jilin 130022 (China)

    2011-09-09

    Highlights: {yields} Ru(bpy){sub 3}{sup 2+} electrochemiluminescence of vitamin C derivatives have been investigated. {yields} Ascorbyl phosphate and ascorbyl palmitate show intense electrochemiluminescence. {yields} Ascorbyl 2-phosphate was detected with high sensitivity. {yields} This study provides a new way to detect vitamin C derivatives. - Abstract: Vitamin C derivatives (VCDs) have been widely used as the alternative and stable sources of vitamin C, and accordingly exhibit many new applications, such as anti-tumor and central nervous system drug delivery. In this study, their Ru(bpy){sub 3}{sup 2+} electrochemiluminescence (ECL) properties have been investigated for the first time using well-known ascorbyl phosphate and ascorbyl palmitate as representative VCDs. Ascorbyl phosphate and ascorbyl palmitate are VCDs with different substituted positions. Both of them increase Ru(bpy){sub 3}{sup 2+} ECL, indicating that other VCDs may also enhance Ru(bpy){sub 3}{sup 2+} ECL signal. The calibration plot for ascorbyl phosphate is linear from 3 x 10{sup -6} to 1.0 x 10{sup -3} M with a detection limit of 1.4 x 10{sup -6} M at a signal-to-noise ratio of 3. The relative standard deviation is 3.6% for six replicate measurements of 0.01 mM ascorbyl 2-phosphate solution. The proposed method is about one order of magnitude more sensitive than electrochemical and UV-vis methods for the determination of ascorbyl phosphate, and is used successfully for the determination of ascorbyl phosphate in whitening and moisturising body wash.

  9. Comparative structure analysis of non-polar organic ferrofluids stabilized by saturated mono-carboxylic acids.

    Avdeev, M V; Bica, D; Vékás, L; Aksenov, V L; Feoktystov, A V; Marinica, O; Rosta, L; Garamus, V M; Willumeit, R

    2009-06-01

    The structure of ferrofluids (magnetite in decahydronaphtalene) stabilized with saturated mono-carboxylic acids of different chain lengths (lauric, myristic, palmitic and stearic acids) is studied by means of magnetization analysis and small-angle neutron scattering. It is shown that in case of saturated acid surfactants, magnetite nanoparticles are dispersed in the carrier approximately with the same size distribution whose mean value and width are significantly less as compared to the classical stabilization with non-saturated oleic acid. The found thickness of the surfactant shell around magnetite is analyzed with respect to stabilizing properties of mono-carboxylic acids. PMID:19376524

  10. Paliperidone palmitate and risperidone long-acting injectable in subjects with schizophrenia recently treated with oral risperidone or other oral antipsychotics

    Alphs, Larry; Bossie, Cynthia A; Sliwa, Jennifer Kern; Fu, Dong-Jing; Ma, Yi-Wen; Hulihan, Joseph

    2013-01-01

    Background This post hoc subgroup analysis of a randomized, double-blind trial evaluated the response to treatment with two long-acting injectable atypical antipsychotics, ie, paliperidone palmitate and risperidone long-acting injectable (RLAI), in subjects with schizophrenia experiencing clinically significant symptoms despite recent treatment with oral risperidone only or other oral antipsychotics. Methods Adult subjects were eligible for the 13-week, double-blind, double-dummy trial (NCT00589914) if they had an established diagnosis of schizophrenia for at least one year and a Positive and Negative Syndrome Scale (PANSS) total score of 60–120 inclusive at screening. Subjects received either paliperidone palmitate (234 mg, day 1; 156 mg, day 8; then once-monthly flexible dosing) or RLAI (25–50 mg biweekly, with oral risperidone supplementation on days 1–28), plus matched placebo injections/tablets. Results This post hoc analysis reports data on 747 subjects who, within 2 weeks of starting double-blind study medication, had reportedly received oral risperidone only (paliperidone palmitate group, n = 126; RLAI group, n = 107), other oral antipsychotics (paliperidone palmitate group, n = 199; RLAI group, n = 203), or no antipsychotic (paliperidone palmitate group, n = 56; RLAI group, n = 56). Mean PANSS total scores improved significantly at end point across all subgroups (mean change from baseline ranged from −17.5 to −19.5, all P < 0.0001). Clinical Global Impression-Severity and Personal and Social Performance scale measures also significantly improved from baseline (all P < 0.0001). Conclusion Treatment with paliperidone palmitate or RLAI resulted in a significant reduction in the symptoms of schizophrenia irrespective of previous recent treatment with oral risperidone only or other oral antipsychotics. For subjects who had previously received oral risperidone only, the difference in formulation was the main change in the intervention because the

  11. Onset of efficacy and tolerability following the initiation dosing of long-acting paliperidone palmitate: post-hoc analyses of a randomized, double-blind clinical trial

    Fu Dong-Jing

    2011-05-01

    Full Text Available Abstract Background Paliperidone palmitate is a long-acting injectable atypical antipsychotic for the acute and maintenance treatment of adults with schizophrenia. The recommended initiation dosing regimen is 234 mg on Day 1 and 156 mg on Day 8 via intramuscular (deltoid injection; followed by 39 to 234 mg once-monthly thereafter (deltoid or gluteal. These post-hoc analyses addressed two commonly encountered clinical issues regarding the initiation dosing: the time to onset of efficacy and the associated tolerability. Methods In a 13-week double-blind trial, 652 subjects with schizophrenia were randomized to paliperidone palmitate 39, 156, or 234 mg (corresponding to 25, 100, or 150 mg equivalents of paliperidone, respectively or placebo (NCT#00590577. Subjects randomized to paliperidone palmitate received 234 mg on Day 1, followed by their randomized fixed dose on Day 8, and monthly thereafter, with no oral antipsychotic supplementation. The onset of efficacy was defined as the first timepoint where the paliperidone palmitate group showed significant improvement in the Positive and Negative Syndrome Scale (PANSS score compared to placebo (Analysis of Covariance [ANCOVA] models and Last Observation Carried Forward [LOCF] methodology without adjusting for multiplicity using data from the Days 4, 8, 22, and 36 assessments. Adverse event (AE rates and relative risks (RR with 95% confidence intervals (CI versus placebo were determined. Results Paliperidone palmitate 234 mg on Day 1 was associated with greater improvement than placebo on Least Squares (LS mean PANSS total score at Day 8 (p = 0.037. After the Day 8 injection of 156 mg, there was continued PANSS improvement at Day 22 (p ≤ 0.007 vs. placebo and Day 36 (p Conclusions Significantly greater symptom improvement was observed by Day 8 with paliperidone palmitate (234 mg on Day 1 compared to placebo; this effect was maintained after the 156 mg Day 8 injection, with a trend towards a dose

  12. Active ingredients fatty acids as antibacterial agent from the brown algae Padina pavonica and Hormophysa triquetra

    Gihan Ahmed El Shoubaky; Essam Abd El Rahman Salem

    2014-01-01

    Objective: To estimate the fatty acids content in the brown algae Padina pavonica (P. pavonica) and Hormophysa triquetra (H. triquetra) and evaluate their potential antimicrobial activity as bioactive compounds.Methods:The fatty acid compositions of the examined species were analyzed using gas chromatography-mass spectrometry. The antimicrobial activity of crude and fatty acids was assessed using the agar plug technique.Results:The fatty acids profile ranged from C8:0 to C20:4. Concentration of saturated fatty acids in P. pavonica was in the order palmitic>myristic>stearic whereas concentration of the unsaturated fatty acids was oleic acid>palmitoleic>9-cis-hexadecenoic>linoleic acid>α-linolenic>arachidonic> elaidic acid. H. triquetra contained high concentration of saturated fatty acids than those of P. pavonica which was in the order as follows: palmitic>margaric>myristic>nonadecyclic>stearic>caprylic>tridecylic>pentadecylic>lauric while the unsaturated fatty acids consisted of oleic>nonadecenoic>non adecadienoate>margaroleic. The crude and fatty acid extracts of H. triquetra and P. pavonica were biologically active on the tested pathogens. H.triquetra exhibited a larger inhibitory zone than P. pavonica. Conclusions: The brown algae P. pavonica and H. triquetra have high efficient amount of fatty acids and showed strong antibacterial activity, especially H. triquetra.

  13. Deoxygenation of Plant Fatty Acid using NiSnK/ SiO2 as Catalyst

    Environmental friendly bio-oil which offers supply reliability as a potential alternative fuel, has spurred to rapid development of bio fuels technology. Palm oil is a potential renewable energy source for bio fuels production in the future and Malaysia is one of the world largest palm oil producers. However, undesired oxygen content in the plant fatty acid that contributes to low energy density, high viscosity, and low stability, makes the palm oil not effective to be used as bio fuels directly. In the present study, the performance of silica supported trimetal catalyst, NiSnK/ SiO2, on deoxygenation of used palm oil was evaluated. In addition, the effects of operating parameters, such as reaction temperature and weight hourly space velocity were investigated. Conversion of palmitic acid as high as 90 % was achieved in deoxygenation of used palm oil at reaction temperature 350 degree Celsius. In order to have a better understanding on the deoxygenation reaction, model compound system using the major saturated fatty acid in the used palm oil, palmitic acid was also carried out. Palmitic acid was found mainly decarboxylated into n-pentadecane with some decarboxylation and isomerization products. (author)

  14. Long-term tolerability of once-monthly injectable paliperidone palmitate in subjects with recently diagnosed schizophrenia

    Sliwa JK

    2012-08-01

    Full Text Available Jennifer Kern Sliwa,1 Cynthia A Bossie,1 Dong-Jing Fu,1 Ibrahim Turkoz,2 Larry Alphs11Janssen Scientific Affairs LLC, 2Janssen Research and Development, LLC, Titusville, NJ, USABackground: A post hoc analysis from a multiphase trial with open-label transition and maintenance phases, a double-blind relapse prevention phase, and an optional open-label extension examined the long-term tolerability with continuous once-monthly injectable paliperidone palmitate 39, 78, 117, or 156 mg (25, 50, 75, or 100 mg equivalents [mg eq] of paliperidone in subjects with recently diagnosed (≤5 years; n = 216 versus chronic illness (>5 years; n = 429 schizophrenia.Methods: Adverse events reported at a ≥2% margin between subgroups were identified. Relative risks (in the recently diagnosed compared with the chronically ill and 95% confidence intervals (CI were determined, and CI not including 1 were considered potentially significant.Results: In both subgroups, the mean monthly dose was 109 mg (69.9 mg eq. Continuous mean exposures were 333.9 ± 271.9 and 308.7 ± 278.3 days in the recently diagnosed and chronic illness subgroups, respectively. Using the criteria outlined in the methods, nasopharyngitis was a potentially significant event reported in more chronically ill than recently diagnosed subjects at months 6, 9, 12, and endpoint (7.2% versus 2.8%; relative risk 0.384; 95% CI 0.163–0.907. Influenza (2.8% versus 0.7%; relative risk 3.9; 95% CI 1.003–15.730 and amenorrhea (3.2% versus 0.9%; relative risk 3.476; 95% CI 1.029–11.744 at endpoint were potentially significant events in more recently diagnosed than chronically ill subjects. Mean weight changes, sedation/somnolence, any extrapyramidal symptom-related or glucose-related events were generally similar between the groups. The mean prolactin level increased in both sexes in both subgroups (changes from baseline of +41.8 ng/mL and +26.5 ng/mL in recently diagnosed and chronic illness females and

  15. Electrochemical examination of the ascorbic acid radical anion in non-aqueous electrolytes

    Yoshimura, M.; Honda, K.; Kondo, T.; Rao, T.N.; Tryk, D.A.; Fujishima, A

    2002-10-15

    A quasi-reversible redox reaction involving ascorbic acid was observed in non-aqueous electrolytes at conductive diamond electrode. The chemical reversibility of these reactions is consistent with ascorbic acid being reduced to the ascorbic acid radical anion in a one-electron process, with subsequent reoxidation to ascorbic acid. This is the first report on the electrochemical production of the ascorbic acid radical anion in non-aqueous electrolytes. Ascorbyl 6-stearate and 4-hydroxy 2(5H)-furanone, which have somewhat similar structures as ascorbic acid, also showed one-electron transfer reduction reaction producing radicals with a single negative charge, suggesting that these compounds follow the same electrochemical behavior as ascorbic acid. The double bond and hydroxyl substituent on the five-membered ring are shown to be necessary for the stabilization of the radical anions. It was confirmed by the calculation of the total energy using molecular orbital methods that resonance structures involving the double-bond and hydroxyl group provide significant stabilization of the radical anions. Electrochemical preparation may be a useful method for the detailed study of radicals, their molecular structure and reactivity.

  16. Electrochemical examination of the ascorbic acid radical anion in non-aqueous electrolytes

    A quasi-reversible redox reaction involving ascorbic acid was observed in non-aqueous electrolytes at conductive diamond electrode. The chemical reversibility of these reactions is consistent with ascorbic acid being reduced to the ascorbic acid radical anion in a one-electron process, with subsequent reoxidation to ascorbic acid. This is the first report on the electrochemical production of the ascorbic acid radical anion in non-aqueous electrolytes. Ascorbyl 6-stearate and 4-hydroxy 2(5H)-furanone, which have somewhat similar structures as ascorbic acid, also showed one-electron transfer reduction reaction producing radicals with a single negative charge, suggesting that these compounds follow the same electrochemical behavior as ascorbic acid. The double bond and hydroxyl substituent on the five-membered ring are shown to be necessary for the stabilization of the radical anions. It was confirmed by the calculation of the total energy using molecular orbital methods that resonance structures involving the double-bond and hydroxyl group provide significant stabilization of the radical anions. Electrochemical preparation may be a useful method for the detailed study of radicals, their molecular structure and reactivity

  17. Anaerobic biodegradation of long chain fatty acids : biomethanisation of biomass-associated LCFA as a challenge for the anaerobic treatment of effluents with high lipid/LCFA content

    Pereira, M.A.

    2003-01-01

    Tese de doutoramento em Engenharia Biológica e Química. This work was focused on the anaerobic biodegradation of Long Chain Fatty Acids, especially those that are associated to anaerobic sludge by mechanisms of adsorption, precipitation or entrapment. When continuously fed with oleic acid (EGSB reactors, influent concentrations between 2 and 8 g COD/l and HRT=1 day), suspended and granular anaerobic sludge accumulated palmitic acid. This LCFA was efficiently biomethanised in batch assays, ...

  18. Sterols and fatty acids extraction process from the cactus Opuntia ficus-indica [(L.) Miller] by means of supercritical CO2

    Bermejo Acosta, Gerardo

    2009-01-01

    After 120 years of Supercritical Fluids (SCF) discovering, practical applications began to be developed. The SCF extraction (SCFE) of sterol fraction and fatty acids from the prickly pear seeds' oil, considered sub-product from sweets processing, is compared to traditional extraction methods varying extraction time, modifier influence, temperature and pressure of supercritical CO2 as main solvent. The main substances found were β-sitosterol (BS), Linoleic Acid (LA) and Palmitic Acid (PA). Low...

  19. Evaluation of Fatty Acid and Amino Acid Compositions in Okra (Abelmoschus esculentus Grown in Different Geographical Locations

    Rokayya Sami

    2013-01-01

    Full Text Available Okra has different uses as a food and a remedy in traditional medicine. Since it produces many seeds, distribution of the plant is also quite easy. Although seed oil yield is low (4.7%, since the linoleic acid composition of the seed oil is quiet high (67.5%, it can still be used as a source of (UNSAT unsaturated fatty acids. In this study, samples of okra grown in four different locations were analyzed to measure fatty acid and amino acid compositions. The content of the lipid extraction ranged from 4.34% to 4.52% on a dry weight basis. Quantitatively, the main okra fatty acids were palmitic acid (29.18–43.26%, linoleic acid (32.22–43.07%, linolenic acid (6.79–12.34%, stearic acid (6.36–7.73%, oleic acid (4.31–6.98%, arachidic acid (ND–3.48%, margaric acid (1.44–2.16%, pentadecylic acid (0.63–0.92%, and myristic acid (0.21–0.49%. Aspartic acid, proline, and glutamic acids were the main amino acids in okra pods, while cysteine and tyrosine were the minor amino acids. Statistical methods revealed how the fatty acid and amino acid contents in okra may be affected by the sampling location.

  20. Muscle cells challenged with saturated fatty acids mount an autonomous inflammatory response that activates macrophages

    Pillon Nicolas J

    2012-10-01

    Full Text Available Abstract Obesity is associated with chronic low-grade inflammation. Within adipose tissue of mice fed a high fat diet, resident and infiltrating macrophages assume a pro-inflammatory phenotype characterized by the production of cytokines which in turn impact on the surrounding tissue. However, inflammation is not restricted to adipose tissue and high fat-feeding is responsible for a significant increase in pro-inflammatory cytokine expression in muscle. Although skeletal muscle is the major disposer of dietary glucose and a major determinant of glycemia, the origin and consequence of muscle inflammation in the development of insulin resistance are poorly understood. We used a cell culture approach to investigate the vectorial crosstalk between muscle cells and macrophages upon exposure to physiological, low levels of saturated and unsaturated fatty acids. Inflammatory pathway activation and cytokine expression were analyzed in L6 muscle cells expressing myc-tagged GLUT4 (L6GLUT4myc exposed to 0.2 mM palmitate or palmitoleate. Conditioned media thereof, free of fatty acids, were then tested for their ability to activate RAW264.7 macrophages. Palmitate -but not palmitoleate- induced IL-6, TNFα and CCL2 expression in muscle cells, through activation of the NF-κB pathway. Palmitate (0.2 mM alone did not induce insulin resistance in muscle cells, yet conditioned media from palmitate-challenged muscle cells selectively activated macrophages towards a pro-inflammatory phenotype. These results demonstrate that low concentrations of palmitate activate autonomous inflammation in muscle cells to release factors that turn macrophages pro-inflammatory. We hypothesize that saturated fat-induced, low-grade muscle cell inflammation may trigger resident skeletal muscle macrophage polarization, possibly contributing to insulin resistance in vivo.

  1. Expansion of guidance for the day 8 initiation dose of paliperidone palmitate to avoid a missed dose

    Samtani MN

    2013-05-01

    Full Text Available Mahesh N Samtani,1 Isaac Nuamah,1 Srihari Gopal,1 Bart Remmerie,2 Jennifer Kern Sliwa,3 Larry Alphs31Janssen Research and Development, LLC, NJ, USA; 2Janssen Research and Development, LLC, Division of Janssen Pharmaceutica NV, Beerse, Belgium; 3Janssen Scientific Affairs, LLC, NJ, USABackground: Paliperidone palmitate (PP is a long-acting injectable formulation of an atypical antipsychotic, paliperidone. Its dose can be expressed in milligram or milligram equivalents (mg eq of active paliperidone (39, 78, 117, 156, and 234 mg of PP correspond to 25, 50, 75, 100, and 150 mg eq of paliperidone. The recommended initiation dosing regimen for PP is 150 [day 1]/100[day 8] mg eq. Labeling guidance allowed a ± 2 day window for the day 8 injection that provides more flexibility with patient scheduling and avoids missing the day 8 initiation dose. Recently, expansion of the day 8 dosing window from ±2 to ±4 days has been approved in the United States based on results obtained from the model-based simulations and review of safety data presented here.Methods: The predicted exposure for the recommended initiation regimen of PP was compared with day 1/day 4, and day 1/day 12 dosing scenarios; each scenario was compared with the highest clinically evaluated initiation regimen (150[day 1]/150[day 8] mg eq and to the recommended 6 mg/day oral dose of extended-release paliperidone.Results: Simulated exposures with PP 150 mg eq on day 1 and 100 mg eq on days 4, 8, or 12 overlap considerably, with ±3 ng/mL variation in median maximum plasma concentrations. Based upon pharmacokinetic bridging/bracketing, the peak concentration with PP 150/100 mg eq [days 1/4] was lower than that with the highest initiation regimen. Exposures for PP 150 mg eq on day 1 and 100 mg eq on days 4, 8, or 12 were maintained close to those of 6 mg of paliperidone extended-release.Conclusion: These simulations indicate that using the expanded dosing window of ±4 days has little effect on

  2. Radiolytic products of irradiated authentic fatty acids and triacylglycerides

    Kim, K.-S. E-mail: kskim@mail.chosun.ac.kr; Lee, Jeong-Min; Seo, Hye-Young; Kim, Jun-Hyoung; Song, Hyun-Pa; Byun, Myung-Woo; Kwon, Joong-Ho

    2004-10-01

    Radiolytic products of authentic fatty acids (palmitic, stearic, oleic, linoleic and linolenic acids) and triacylglycerides (tripalmitin, tristearin, triolein, trilinolein and trilinolenin) were determined. Concentrations of hydrocarbons from the saturated fatty acids were higher than the unsaturated fatty acids. Authentic fatty acids were mainly decomposed in the {alpha}-carbon position and C{sub n-1} hydrocarbons occurred in higher than C{sub n-2} hydrocarbons. Concentrations of 2-alkylcyclobutanones from the saturated fatty acids were lower than the unsaturated fatty acids. Concentrations of hydrocarbons from tripalmitin and tristearin were not a significant change compared with triolein, trilinolein and trilinolenin. For all triacylglycerides except triolein, C{sub n-1} hydrocarbons were higher than C{sub n-2} hydrocarbons. Radioproduction rates of 2-alkylcyclobutanones from tripalmitin and tristearin were higher than triolein, trilinolein and trilinolenin.

  3. Toxicity of long chain fatty acids towards acetate conversion by Methanosaeta concilii and Methanosarcina mazei.

    Silva, Sérgio A; Salvador, Andreia F; Cavaleiro, Ana J; Pereira, M Alcina; Stams, Alfons J M; Alves, M Madalena; Sousa, Diana Z

    2016-07-01

    Long-chain fatty acids (LCFA) can inhibit methane production by methanogenic archaea. The effect of oleate and palmitate on pure cultures of Methanosaeta concilii and Methanosarcina mazei was assessed by comparing methane production rates from acetate before and after LCFA addition. For both methanogens, a sharp decrease in methane production (> 50%) was observed at 0.5 mmol L(-1) oleate, and no methane was formed at concentrations higher than 2 mmol L(-1) oleate. Palmitate was less inhibitory than oleate, and M. concilii was more tolerant to palmitate than M. mazei, with 2 mmol L(-1) palmitate causing 11% and 64% methanogenic inhibition respectively. This study indicates that M. concilii and M. mazei tolerate LCFA concentrations similar to those previously described for hydrogenotrophic methanogens. In particular, the robustness of M. concilii might contribute to the observed prevalence of Methanosaeta species in anaerobic bioreactors used to treat LCFA-rich wastewater. PMID:27273786

  4. Influence of free fatty acids on glucose uptake in prostate cancer cells

    Introduction: The study focuses on the interaction between glucose and free fatty acids (FFA) in malignant human prostate cancer cell lines by an in vitro observation of uptake of fluoro-2-deoxy-D-glucose (FDG) and acetate. Methods: Human prostate cancer cell lines (PC3, CWR22Rv1, LNCaP, and DU145) were incubated for 2 h and 24 h in glucose-containing (5.5 mM) Dulbecco’s Modified Eagle’s Medium (DMEM) with varying concentrations of the free fatty acid palmitate (0–1.0 mM). Then the cells were incubated with [18 F]-FDG (1 μCi/mL; 0.037 MBq/mL) in DMEM either in presence or absence of glucose and in presence of varying concentrations of palmitate for 1 h. Standardized procedures regarding cell counting and measuring for 18 F radioactivity were applied. Cell uptake studies with 14C-1-acetate under the same conditions were performed on PC3 cells. Results: In glucose containing media there was significantly increased FDG uptake after 24 h incubation in all cell lines, except DU145, when upper physiological levels of palmitate were added. A 4-fold increase of FDG uptake in PC3 cells (15.11% vs. 3.94%/106 cells) was observed in media with 1.0 mM palmitate compared to media with no palmitate. The same tendency was observed in PC3 and CWR22Rv1 cells after 2 h incubation. In glucose-free media no significant differences in FDG uptake after 24 h incubation were observed. The significant differences after 2 h incubation all pointed in the direction of increased FDG uptake when palmitate was added. Acetate uptake in PC3 cells was significantly lower when palmitate was added in glucose-free DMEM. No clear tendency when comparing FDG or acetate uptake in the same media at different time points of incubation was observed. Conclusions: Our results indicate a FFA dependent metabolic boost/switch of glucose uptake in PCa, with patterns reflecting the true heterogeneity of the disease

  5. Influence of free fatty acids on glucose uptake in prostate cancer cells☆

    Andersen, Kim Francis; Divilov, Vadim; Sevak, Kuntalkumar; Koziorowski, Jacek; Lewis, Jason S.; Pillarsetty, NagaVaraKishore

    2016-01-01

    Introduction The study focuses on the interaction between glucose and free fatty acids (FFA) in malignant human prostate cancer cell lines by an in vitro observation of uptake of fluoro-2-deoxy-d-glucose (FDG) and acetate. Methods Human prostate cancer cell lines (PC3, CWR22Rv1, LNCaP, and DU145) were incubated for 2 h and 24 h in glucose-containing (5.5 mM) Dulbecco’s Modified Eagle’s Medium (DMEM) with varying concentrations of the free fatty acid palmitate (0–1.0 mM). Then the cells were incubated with [18 F]-FDG (1 µCi/mL; 0.037 MBq/mL) in DMEM either in presence or absence of glucose and in presence of varying concentrations of palmitate for 1 h. Standardized procedures regarding cell counting and measuring for 18F radioactivity were applied. Cell uptake studies with 14C-1-acetate under the same conditions were performed on PC3 cells. Results In glucose containing media there was significantly increased FDG uptake after 24 h incubation in all cell lines, except DU145, when upper physiological levels of palmitate were added. A 4-fold increase of FDG uptake in PC3 cells (15.11% vs. 3.94%/106 cells) was observed in media with 1.0 mM palmitate compared to media with no palmitate. The same tendency was observed in PC3 and CWR22Rv1 cells after 2 h incubation. In glucose-free media no significant differences in FDG uptake after 24 h incubation were observed. The significant differences after 2 h incubation all pointed in the direction of increased FDG uptake when palmitate was added. Acetate uptake in PC3 cells was significantly lower when palmitate was added in glucose-free DMEM. No clear tendency when comparing FDG or acetate uptake in the same media at different time points of incubation was observed. Conclusions Our results indicate a FFA dependent metabolic boost/switch of glucose uptake in PCa, with patterns reflecting the true heterogeneity of the disease. PMID:24440212

  6. Effects of fatty acid regulation on visfatin gene expression in adipocytes

    WEN Yu; WANG Hong-wei; WU Jing; LU Hui-ling; HU Xiu-fen; Katherine Cianflone

    2006-01-01

    Background The levels of long-term elevated serum or intracellular free fatty acid (FFA) induce insulin resistance associated with central obesity. The insulin-mimetic protein visfatin is preferentially produced by visceral adipose tissues and has been implicated in obesity and insulin resistance. To identify that FFA is capable of inducing insulin resistance and to clarify the role of FFA on visfatin, we examined the effect of monounsaturated FFA oleate (C18:1) and saturated FFA palmitate (C16:0) on glucose transport and visfatin gene expression in cultured 3T3-L1 adipocytes or preadipocytes.Methods FFA-free DMEM/F12, 0.125 mmol/L, 0.5 mmol/1 and 1.0 mmol/L oleate or palmitate was added to cultured 3T3-L1 adipocytes or preadipocytes and incubated overnight. Glucose transport was assessed as 3H-2-deoxy-glucose uptake. Total RNA was extracted and subjected to RT-PCR for the measurement of visfatin mRNA levels. Statistical comparisons between control group and other groups were performed with the two-tailed paired t test, and one-way ANOVA was used to compare the mean values among the groups.Results Insulin increased specific membrane glucose transport in 3T3-L1 preadipocytes. Upregulation was evident from 15 minutes to 1 hour exposure to insulin. However, after 6-hour exposure to insulin, there was a downregulation in the response to insulin. Dose response studies demonstrated that 2-deoxy glucose transport was increased by 336% at 50 nmol/L insulin (P<0.01), and reached a maximal effect at 100 nmol/L insulin(P<0.01). Oleate and palmitate treatment did not influence basal glucose transport (without insulin stimulation),whereas insulin-stimulated glucose transport was inhibited after overnight oleate and palmitate treatment in preadipocytes and adipocytes. In 3T3-L1 preadipocytes, insulin resistance could be achieved at 0.125 mmol/L oleate or palmitate (P<0.05, respectively), and the inhibition was dose dependent. In adipocytes, the inhibition was noted at 0

  7. Efficacy and safety of once-monthly injection of paliperidone palmitate in hospitalized Asian patients with acute exacerbated schizophrenia: an open-label, prospective, noncomparative study

    Li HF; Turkoz I; Zhang F

    2015-01-01

    HuaFang Li,1 Ibrahim Turkoz,2 Fan Zhang3 1Shanghai Mental Health Center, Shanghai Jiao Tong University School of Medicine, Shanghai, People’s Republic of China; 2Janssen Research & Development, LLC, Titusville, NJ, USA; 3Xi’an Janssen Pharmaceutical Ltd., Beijing, People’s Republic of China Introduction: This single-group, open-label, prospective, noncomparative, multicenter, Phase IV study explored the efficacy and tolerability of paliperidone palmitate (PP)...

  8. A one-year prospective study of the safety, tolerability and pharmacokinetics of the highest available dose of paliperidone palmitate in patients with schizophrenia

    Coppola Danielle; Liu Yanning; Gopal Srihari; Remmerie Bart; Samtani Mahesh N; Hough David W; Nuamah Isaac; Sulaiman Ahmad; Pandina Gahan

    2012-01-01

    Abstract Background There are no previous reports of paliperidone palmitate's (PP) long term tolerability or pharmacokinetics of the highest dose in patients with schizophrenia. This study evaluates safety and tolerability, as well as pharmacokinetics, of the highest marketed dose of PP (150 mg eq. [234 mg]) in stable patients with schizophrenia over a 1-year period. Methods In this 1-year prospective study, eligible patients (aged 18-65 years; Positive and Negative Syndrome Scale's total sco...

  9. Changes in prolactin levels and sexual functioning after switching from long-acting injectable risperidone to paliperidone palmitate in young psychotic patients: a case series

    Itziar Montalvo; Laura Ortega; Xavi López; Montse Solé; Rosa Monseny; Joan Franch; Javier Labad

    2012-01-01

    Statement of the problem : Long-acting injectable (LAI) antipsychotics have been developed to increase compliance in schizophrenia. Risperidone-LAI was the first LAI atypical antipsychotic, as a biweekly injection. Paliperidone Palmitate (PP) is a recently developed LAI atypical antipsychotic that is administered monthly. PP is hydrolized to paliperidone (9-hydroxyrisperidone), the primary active metabolite of risperidone. Although both risperidone and paliperidone are associated with increas...

  10. Onset of efficacy and tolerability following the initiation dosing of long-acting paliperidone palmitate: post-hoc analyses of a randomized, double-blind clinical trial

    Fu Dong-Jing; Ma Yi-Wen; Sliwa Jennifer K; Bossie Cynthia A; Alphs Larry

    2011-01-01

    Abstract Background Paliperidone palmitate is a long-acting injectable atypical antipsychotic for the acute and maintenance treatment of adults with schizophrenia. The recommended initiation dosing regimen is 234 mg on Day 1 and 156 mg on Day 8 via intramuscular (deltoid) injection; followed by 39 to 234 mg once-monthly thereafter (deltoid or gluteal). These post-hoc analyses addressed two commonly encountered clinical issues regarding the initiation dosing: the time to onset of efficacy and ...

  11. Oligonol suppresses lipid accumulation and improves insulin resistance in a palmitate-induced in HepG2 hepatocytes as a cellular steatosis model

    Park, Jae-Yeo; Kim, Younghwa; Im, Jee Ae; Lee, Hyangkyu

    2015-01-01

    Background Oligonol is a low molecular weight form of polyphenol polymers derived from lychee fruits. Several studies suggest that Oligonol has an anti-obesity effect. Since obesity is tightly associated with insulin resistance, we investigated a possible remission effect of Oligonol on lipid accumulation and insulin resistance in human hepatic HepG2 cells. Methods HepG2 cells were treated with palmitate for 24 h to induce cellular hepatic steatosis and insulin resistance. The cells were then...

  12. Are the Long-Acting Intramuscular Formulations of Risperidone or Paliperidone Palmitate Associated with Post-Injection Delirium/Sedation Syndrome? An Assessment of Safety Databases

    Alphs, Larry; Gopal, Srihari; Karcher, Keith; Kent, Justine; Kern Sliwa, Jennifer; Kushner, Stuart; Nuamah, Isaac; Singh, Jaskaran

    2011-01-01

    Long-acting injectable (LAI) formulations of antipsychotics are valuable treatment alternatives for patients with psychotic disorders, and understanding their safe use is critical. Post-injection delirium/sedation syndrome (PDSS) has been reported following treatment with one atypical antipsychotic LAI. Clinical databases of risperidone LAI and paliperidone palmitate were explored to identify if cases of PDSS had been observed. No cases of PDSS were identified in 15 completed trials of 3,164 ...

  13. Paliperidone palmitate and risperidone long-acting injectable in subjects with schizophrenia recently treated with oral risperidone or other oral antipsychotics

    Alphs L; Bossie CA; Sliwa JK; Fu DJ; Ma YW; Hulihan J

    2013-01-01

    Larry Alphs,1 Cynthia A Bossie,1 Jennifer Kern Sliwa,2 Dong-Jing Fu,1 Yi-Wen Ma,3 Joseph Hulihan11CNS Medical Affairs, 2Medical Information, Janssen Scientific Affairs, LLC, Titusville, NJ, USA; 3Biostatistics, B&P, Janssen Research & Development LLC, Titusville, NJ, USABackground: This post hoc subgroup analysis of a randomized, double-blind trial evaluated the response to treatment with two long-acting injectable atypical antipsychotics, ie, paliperidone palmitate and risper...

  14. Number needed to treat and number needed to harm with paliperidone palmitate relative to long-acting haloperidol, bromperidol, and fluphenazine decanoate for treatment of patients with schizophrenia

    Gopal, Srihari; Berwaerts, Joris; Nuamah, Isaac; Akhras, Kasem; Coppola, Danielle; Daly, Ella; Hough, David; Palumbo, Joseph

    2011-01-01

    Background: We analyzed data retrieved through a PubMed search of randomized, placebo-controlled trials of first-generation antipsychotic long-acting injectables (haloperidol decanoate, bromperidol decanoate, and fluphenazine decanoate), and a company database of paliperidone palmitate, to compare the benefit-risk ratio in patients with schizophrenia. Methods: From the eight studies that met our selection criteria, two efficacy and six safety parameters were selected for calculation of number...

  15. Long-acting injectable paliperidone palmitate versus oral paliperidone extended release: a comparative analysis from two placebo-controlled relapse prevention studies

    Markowitz, Michael; Fu, Dong-Jing; Levitan, Bennett; Gopal, Srihari; Turkoz, Ibrahim; Alphs, Larry

    2013-01-01

    Background Increasing availability and use of long-acting injectable antipsychotics have generated a need to compare these formulations with their oral equivalents; however, a paucity of relevant data is available. Methods This post hoc comparison of the long-term efficacy, safety and tolerability of maintenance treatment with paliperidone palmitate (PP) versus oral paliperidone extended release (ER) used data from two similarly designed, randomised, double-blind (DB), placebo-controlled schi...

  16. The enhancing effect of excess retinol palmitate on induction of odontogenic tumors and inhibitory effect on squamous cell carcinoma of the gingiva in hamsters treated with N-methylnitrosourea

    Kohgo, T.; Mezawa, F.; lizuka, T.; Shindoh, M

    1999-01-01

    The influence of excess retinol palmitate on induction of tumors in the oral region was examined histopathologically. Sixty-three weanling Syrian golden hamsters were divided into five groups and received either 0.2% N-methylnitrosourea (MNU) (lmg1100g body weight) or retinol palmitate (RP) (25,000 IU/100g body weight) twice a week for 16 weeks, singly or in combination. Animals received RP intraperitoneally or intragastrically and then, 6 hours later, the anim...

  17. Effectiveness and Predictors of Continuation of Paliperidone Palmitate Long-Acting Injection Treatment: A 12-Month Naturalistic Cohort Study.

    Whale, Richard; Pereira, Marco; Cuthbert, Sharon; Fialho, Renata

    2015-10-01

    Antipsychotic long-acting injectable (LAI) medication has an important place as a treatment option in schizophrenia with evolving evidence to support clinical benefit over oral medication. Paliperidone palmitate is recently licensed as an LAI. We studied a naturalistic cohort of all identifiable patients who initiated paliperidone LAI in a specific United Kingdom region (Sussex) from first availability up to January 2013 (n = 179). Favorably, 60% of the cohort continued paliperidone LAI beyond 12 months from initiation. Schizophrenia diagnosis was significantly associated with 12-month continuation on univariate analysis (65% continuation rate at 12 months in this diagnostic subgroup). No baseline variables were identified as independently associated with 12-month continuation. However, fewer inpatient days after initiation (odds ratio [OR], 1.01; 95% confidence interval [CI], 1.003-1.011; P = 0.002), dose adjustment up or down (OR, 3.46; 95% CI, 1.26-9.51; P = 0.016), and a higher maintenance dose (OR, 8.31; 95% CI, 1.84-37.51; P = 0.006) during treatment course were all independently associated with continuation on multivariate analysis. Our findings support the importance of a collaborative approach with the LAI recipient in treatment decision making to enhance treatment effectiveness. PMID:26267419

  18. Long-acting paliperidone palmitate – interim results of an observational study of its effect on hospitalization

    Olofinjana, Olubanke

    2014-01-01

    Paliperidone palmitate (PP) is a recently introduced long-acting atypical, or second-generation, antipsychotic. Published data on PP are currently limited to controlled trials and case reports. In this observational study, we followed up 200 consecutive patients prescribed PP in normal practice. After 1 year, 65% of patients were still receiving PP. The number of admissions to hospital in the year following PP initiation was 0.49/patient compared with 0.69/patient/year, 3 years before initiation (P=0.0001). The mean number of bed days fell from 38.78 to 23.09/patient/year over the corresponding period (P=0.0001). The median number of bed days 3 years before PP initiation was 21.50/year and in the year following PP initiation, it was 0. Outcomes were numerically but not statistically better in those continuing PP than in those who ceased PP within a year of initiation. PP was effective and well-tolerated and, given its positive effect on hospital bed days, broadly cost-effective. PMID:24419004

  19. Topical Application of Retinyl Palmitate-Loaded Nanotechnology-Based Drug Delivery Systems for the Treatment of Skin Aging

    Marcela B. Oliveira

    2014-01-01

    Full Text Available The objective of this study was to perform a structural characterization and evaluate the in vitro safety profile and in vitro antioxidant activity of liquid crystalline systems (LCS with and without retinyl palmitate (RP. LCS containing polyether functional siloxane (PFS as a surfactant, silicon glycol copolymer (SGC as oil phase, and water in the ratios 30 : 25 : 45 and 40 : 50 : 10 with (OLSv = RP-loaded opaque liquid system and TLSv = RP-loaded transparent liquid system, respectively and without (OLS and TLS, respectively RP were studied. Samples were characterized using polarized light microscopy (PLM and rheology analysis. In vitro safety profile was evaluated using red cell hemolysis and in vitro cytotoxicity assays. In vitro antioxidant activity was performed by the DPPH method. PLM analysis showed the presence of lamellar LCS just to TLS. Regardless of the presence of RP, the rheological studies showed the pseudoplastic behavior of the formulations. The results showed that the incorporation of RP in LCS improved the safety profile of the drug. In vitro antioxidant activity suggests that LCS presented a higher capacity to maintain the antioxidant activity of RP. PFS-based systems may be a promising platform for RP topical application for the treatment of skin aging.

  20. Photoirradiation of Retinyl Palmitate in Ethanol with Ultraviolet Light - Formation of Photodecomposition Products, Reactive Oxygen Species, and Lipid Peroxides

    Peter P. Fu

    2006-06-01

    Full Text Available We have previously reported that photoirradiation of retinyl palmitate (RP, a storage and ester form of vitamin A (retinol, with UVA light resulted in the formation of photodecomposition products, generation of reactive oxygen species, and induction of lipid peroxidation. In this paper, we report our results following the photoirradiation of RP in ethanol by an UV lamp with approximately equal UVA and UVB light. The photodecomposition products were separated by reversed-phase HPLC and characterized spectroscopically by comparison with authentic standards. The identified products include: 4-keto-RP, 11-ethoxy-12-hydroxy-RP, 13-ethoxy-14-hydroxy-RP, anhydroretinol (AR, and trans- and cis-15-ethoxy-AR. Photoirradiation of RP in the presence of a lipid, methyl linoleate, resulted in induction of lipid peroxidation. Lipid peroxidation was inhibited when sodium azide was present during photoirradiation which suggests free radicals were formed. Our results demonstrate that, similar to irradiation with UVA light, RP can act as a photosensitizer leading to free radical formation and induction of lipid peroxidation following irradiation with UVB light.

  1. Scientific Opinion on the substantiation of a health claim related to beta-palmitate and contribution to softening of stools pursuant to Article 14 of Regulation (EC No 1924/2006

    EFSA Panel on Dietetic Products, Nutrition and Allergies (NDA

    2014-02-01

    Full Text Available Following an application from Specialised Nutrition Europe (formerly IDACE, submitted for authorisation of a health claim pursuant to Article 14 of Regulation (EC No 1924/2006 via the Competent Authority of France, the EFSA Panel on Dietetic Products, Nutrition and Allergies (NDA was asked to deliver an opinion on the scientific substantiation of a health claim related to beta-palmitate and contribution to softening of stools. The food constituent, beta-palmitate, that is the subject of the health claim, is sufficiently characterised. Contribution to softening of stools is a beneficial physiological effect for infants. In weighing the evidence the Panel took into account that, out of two human intervention studies with important methodological limitations, one suggested a stool-softening effect of beta-palmitate whereas the second did not, that one animal study did not support a stool-softening effect of beta-palmitate, and that the evidence provided for a mechanism by which beta-palmitate could contribute to the softening of stools is weak. The Panel concludes that a cause and effect relationship has not been established between the consumption of beta-palmitate and softening of stools.

  2. The Synthesis of 6-L-ascorbyl Trans-β-alkoxycarbonylacrylate and Study of Its Antimicrobial Activity%反丁烯二酸-6-L-抗坏血酸甲酯的合成及抑菌性能的研究

    吴亚凉; 宁正祥

    2009-01-01

    A new asymmetrical ester,6-L-ascorbyl trans-β-alkoxycarbonylacrylate,containing α,β-unsaturated carbonyl group structure was prepared via esterification. The antimicrobial activity of 6-L-ascorbyl trans-β-alkoxycar-bonylacrylate was studied. Results showed that 53.45% yield could be obtained. The minimum inhibition concentration and inhibition rate of 6-L-ascorbyl trans-β-alkoxycarbonylacrylate to Escherichia coli,Bacillus subtilis,Saccharo-myces cerevisiae was 1.0 g/L,88. 83% ; 0. 75 g/L,80. 47% ; 0. 75 g/L,82. 12% respectively. Its antimicrobial activity was much better than sodium benzoate and postassium benzoate,besides the antimicrobial activity did not changed obviously under heat treatment. It was also seen that 6-L-ascorbyl trans-β-alkoxycarbonylacrylate had strong antimicrobial effects for bacteria and yeasts. It is worth the exploration of further development and application.%采用直接酯化法合成了一种新型抗坏血酸衍生物并具有α,β-不饱和羰基结构的化学防腐剂--反丁烯二酸-6-L-抗坏血酸甲酯(V_c酯),合成产率可达53.45%,并对其抑菌效果进行了研究.结果表明,V_c酯对大肠杆菌、枯草杆菌、啤酒酵母的最低抑菌浓度及抑菌率分别为1.0g/L,88.83%;0.75g/L,80.47%;0.75g/L,82.12%;其抑菌效果显著优于常用防腐剂苯甲酸钠及山梨酸钾,且高温处理对其抑菌效果无明显影响,表明V_c酯对细菌、酵母均具有较强的抑制作用.

  3. Oils of insects and larvae consumed in Africa: potential sources of polyunsaturated fatty acids

    Womeni Hilaire Macaire

    2009-07-01

    Full Text Available The objective of this paper is to present the beneficial aspects of some insects consumed in sub-Saharan Africa, based on examples of insects consumed in Cameroon, to present their potential as sources of lipids and essential fatty acids. In Africa, termites, larvae of raphia weevil, caterpillars, crickets, bees, maggots, butterflies, weevil, etc. are significant sources of food. These insects belong mainly to the orders of : Isoptera, Orthoptera, Dictyoptera, Coleoptera, Hymenoptera, Lepidoptera and Diptera. Depending on the species, insects are rich in proteins, minerals (K, Ca, Mg, Zn, P, Fe and/or vitamins (thiamine/B1, riboflavine/B2, pyridoxine/B6, acid pantothenic, niacin. The composition of oils extracted from the following six insects consumed in Cameroon was investigated : larvaes of raphia weevil (Rhynchophorus phoenicis, crickets (Homorocoryphus nitidulus, grasshopper (Zonocerus variegates, termites (Macrotermes sp., a variety of caterpillars (Imbrasia sp. and an unidentified caterpillar from the forest (UI carterpillar. The extraction yields of oil were 53.75%, 67.25%, 9.12%, 49.35%, 24.44% and 20.17% respectively for raphia weevil larvae, crickets, devastating crickets, termites, Imbrasia and UI caterpillar. The oil from raphia weevil mainly contains 37.60% of palmitoleic acid and 45.46% of linoleic acid. The oil from crickets is principally made up of palmitoleic acid (27.59%, linoleic acid (45.63% and α-linolenic acid (16.19%. The oil from grasshoppers is composed of palmitoleic acid (23.83%, oleic acid (10.71%, linoleic acid (21.07%, α-linolenic acid (14.76% and γ-linolenic acid (22.54%. The main components of termite oil are : palmitic acid (30.47%, oleic acid (47.52% and linoleic acid (8.79%. Palmitic acid (36.08% and linolenic acid (38.01% are the two dominant fatty acids of Imbrasia oil. As Imbrasia oil, UI caterpillar oil is composed of palmitic acid (30.80% and linolenic acid (41.79%. Stearic acid (7.04%, oleic acid

  4. A Post-hoc Comparison of Paliperidone Palmitate to Oral Risperidone During Initiation of Long-acting Risperidone Injection in Patients with Acute Schizophrenia

    Pandina, Gahan; Lane, Rosanne; Nuamah, Isaac; Remmerie, Bart; Coppola, Danielle; Hough, David

    2011-01-01

    Objective: First-month data of a 13-week acute schizophrenia study were used to compare paliperidone palmitate to oral risperidone during initiation of long-acting injectable risperidone. Design: Double-blind, randomized study. Setting: Outpatient or inpatient. Participants: Adults with established (≥1 year) schizophrenia. Those assigned to risperidone long-acting injectable (n=460) received 25mg on Days 8 and 22 with oral risperidone (l–6mg) supplementation for the first 28 days. The paliperidone palmitate group (n=453) received 150mg eq. on Day 1, l00mg eq. on Day 8, and oral placebo supplementation for the first 28 days. Measurements: Positive and Negative Syndrome Scale, Personal and Social Performance Scale, Clinical Global Impression-Severity score, and responder rate (percentage of patients with ≥30% reduction in PANSS total score). An analysis of covariance model estimated least-square mean differences between treatment groups. A post-hoc analysis of efficacy data for the period of interest, i.e., at the time points before and after the first 28 days, was conducted. Results: Positive and Negative Syndrome Scale, Personal and Social Performance Scale, Clinical global Impression-Severity scores showed similar efficacy between the treatment groups during the first weeks of treatment, corresponding to the risperidone long-acting injection initiation period. Mean Positive and Negative Syndrome Scale total score at baseline was 84.7 for paliperidone palmitate and 84.4 for oral risperidone, on Day 22 was 73.6 and 74.1, respectively, and on Day 36 was 71.8 and 72.8, respectively. Overall incidence of adverse events in the first 28 days was generally similar (45% for paliperidone palmitate vs. 35% for oral risperidone), except for injection site pain (4.6% vs. 0.7%). Similar active moiety plasma concentrations were obtained during this period. Conclusion: During the first month, paliperidone palmitate without oral supplementation has similar efficacy and

  5. Synergistic permeability enhancing effect of lysophospholipids and fatty acids on lipid membranes

    Davidsen, Jesper; Mouritsen, O.G.; Jørgensen, K.

    2002-01-01

    The permeability-enhancing effects of the two surfactants, 1-paltnitoyl-2-lyso-sn-gycero-3-pllosplloclloline (lysoPPC) and palmitic acid (PA), on lipid membranes that at physiological temperatures are in the gel, fluid, and liquid-ordered phases were determined using the concentration-dependent s......The permeability-enhancing effects of the two surfactants, 1-paltnitoyl-2-lyso-sn-gycero-3-pllosplloclloline (lysoPPC) and palmitic acid (PA), on lipid membranes that at physiological temperatures are in the gel, fluid, and liquid-ordered phases were determined using the concentration......-dependent self-quenching properties of the hydrophilic marker, calcein. Adding lysoPPC to lipid membranes in the gel-phase induced a time-dependent calcein release curve that can be described by the sum of two exponentials, whereas RA induces a considerably more complex release curve. However, when lysoPPC and...

  6. Analysis of fatty acids by graphite plate laser desorption/ionization time-of-flight mass spectrometry.

    Park, K H; Kim, H J

    2001-01-01

    Fatty acids obtained from triglycerides (trioelin, tripalmitin), foods (milk, corn oil), and phospholipids (phosphotidylcholine, phosphotidylserine, phosphatidic acid) upon alkaline hydrolysis were observed directly without derivatization by graphite plate laser desorption/ionization time-of-flight mass spectrometry (GPLDI-TOFMS). Mass-to-charge ratios predicted for sodium adducts of expected fatty acids (e.g. palmitic, oleic, linoleic and arachidonic acids) were observed without interference. Although at present no quantitation is possible, the graphite plate method enables a simple and rapid qualitative analysis of fatty acids. PMID:11507764

  7. Surface and interlayer base-characters in lepidocrocite titanate: The adsorption and intercalation of fatty acid

    Maluangnont, Tosapol; Arsa, Pornanan; Limsakul, Kanokporn; Juntarachairot, Songsit; Sangsan, Saithong; Gotoh, Kazuma; Sooknoi, Tawan

    2016-06-01

    While layered double hydroxides (LDHs) with positively-charged sheets are well known as basic materials, layered metal oxides having negatively-charged sheets are not generally recognized so. In this article, the surface and interlayer base-characters of O2- sites in layered metal oxides have been demonstrated, taking lepidocrocite titanate K0.8Zn0.4Ti1.6O4 as an example. The low basicity (0.04 mmol CO2/g) and low desorption temperature (50-300 °C) shown by CO2- TPD suggests that O2- sites at the external surfaces is weakly basic, while those at the interlayer space are mostly inaccessible to CO2. The liquid-phase adsorption study, however, revealed the uptake as much as 37% by mass of the bulky palmitic acid (C16 acid). The accompanying expansion of the interlayer space by ~0.1 nm was detected by PXRD and TEM. In an opposite manner to the external surfaces, the interlayer O2- sites can deprotonate palmitic acid, forming the salt (i.e., potassium palmitate) occluded between the sheets. Two types of basic sites are proposed based on ultrafast 1H MAS NMR and FTIR results. The interlayer basic sites in lepidocrocite titanate leads to an application of this material as a selective and stable two-dimensional (2D) basic catalyst, as demonstrated by the ketonization of palmitic acid into palmitone (C31 ketone). Tuning of the catalytic activity by varying the type of metal (Zn, Mg, and Li) substituting at TiIV sites was also illustrated.

  8. Molecular assessment of complex microbial communities degrading long chain fatty acids in methanogenic bioreactors

    Sousa, D.Z.; Pereira, M.A.; Smidt, Hauke; Stams, A.J.M.; Alves, M. M.

    2007-01-01

    Microbial diversity of anaerobic sludge after extended contact with long chain fatty acids (LCFA) was studied using molecular approaches. Samples containing high amounts of accumulated LCFA were obtained after continuous loading of two bioreactors with oleate or with palmitate. These sludge samples were then incubated in batch assays to allow degradation of the biomass-associated LCFA. In addition, sludge used as inoculum for the reactors was also characterized. Predominant ...

  9. Microbial communities involved in anaerobic degradation of unsaturated or saturated long chain fatty acids

    Sousa, D.Z.; Pereira, M.A.; Stams, A.J.M.; Alves, M. M.; Smidt, H.

    2007-01-01

    Anaerobic long-chain fatty acid (LCFA)-degrading bacteria were identified by combining selective enrichment studies with molecular approaches. Two distinct enrichment cultures growing on unsaturated and saturated LCFAs were obtained by successive transfers in medium containing oleate and palmitate, respectively, as the sole carbon and energy sources. Changes in the microbial composition during enrichment were analyzed by denaturing gradient gel electrophoresis (DGGE) profiling of PCR...

  10. Separation and characterization of the acid lipase and neutral esterases from human liver.

    Warner, T G; Dambach, L M; Shin, J H; O'Brien, J S

    1980-01-01

    Electrophoresis of human liver homogenates followed by reaction with 4-methylumbelliferyl palmitate reveals the presence of two major electrophoretic forms with esterase (lipase) activity toward this substrate. The two enzymes were isolated and partially purified based on their solubility differences and their relative affinities for the lectin column concanavalin A-Sepharose 4B. Lipase A was particulate with an acidic pH optimum (5.2) and could be solubilized with the non-ionic surfactant Tr...

  11. Thermal characteristic reliability of fatty acid binary mixtures as phase change materials (PCMs) for thermal energy storage applications

    The thermal characteristic reliability of two binary mixtures of fatty acid, myristic acid/palmitic acid/sodium myristate (MA/PA/SM) and myristic acid/palmitic acid/sodium palmitate (MA/PA/SP), were investigated using a thermal cycling test setup for 0, 1000, 2000, 3000, and 3600 heating/cooling cycles. The changes in thermal properties and chemical bonding of both eutectic PCMs were measured using Differential Scanning Calorimetric (DSC) and Fourier Transform Infrared Spectroscopy (FT-IR) analyzer, respectively. MA/PA/SM and MA/PA/SP eutectic mixtures shows only minor changes in phase transition temperature (Tm, Ts) and in latent heat of fusion (ΔHf). Moreover, the chemical bonding structures of these eutectic PCMs show no degradation and the thermal performance of those PCMs shows a good stability after 3600 thermal cycles. Therefore, it is found that the thermal characteristic stability of prepared MA/PA/SM and MA/PA/SP eutectic mixtures were acceptable for long term performance and economic feasibilities used as a phase change material (PCM) for thermal energy storage (TES) application. - Highlights: • The MA/PA/SM and MA/PA/SP were used as eutectic phase change materials (PCM). • Thermal reliability of eutectic PCMs evaluated using a thermal cycling test. • MA/PA/SP has a great thermal characteristic than MA/PA/SM after 3600 thermal cycles. • The eutectic PCMs did not show change of appearance after 3600 thermal cycles

  12. Aortic drug delivery of dexamethasone palmitate incorporated into lipid microspheres and its antiatherosclerotic effect in atherogenic mice.

    Chono, Sumio; Tauchi, Yoshihiko; Morimoto, Kazuhiro

    2005-08-01

    In order to confirm the efficacy of dexamethasone (DXM) palmitate incorporated into lipid microspheres (d-lipo) on atherosclerosis, the aortic drug delivery by d-lipo and its antiatherosclerotic effect were investigated. In an in vitro uptake experiment, d-lipo or DXM was added to macrophages and foam cells, and then incubated for 1, 4, 8 and 24 h at 37 degrees C. The uptake of drug by these cells after addition of d-lipo was higher than that of DXM at each time point. In an in vitro pharmacological experiment, the macrophages and foam cells were incubated with d-lipo or DXM for 24 h at 37 degrees C. The inhibitory effect of d-lipo on cellular cholesterol ester (CE) accumulation in these cells was significantly more potent than that of DXM. In an in vivo pharmacokinetic experiment, d-lipo or DXM was intravenously administered to atherogenic mice, and then aorta was collected at 1, 8, and 24 h after administration. The aortic drug concentration after administration of d-lipo to atherogenic mice was higher than that of DXM at each time point. In an in vivo pharmacological experiment, d-lipo or DXM was intravenously administered to atherogenic mice once a week for 7 weeks. The inhibitory effect of d-lipo on the aortic CE accumulation in atherogenic mice was significantly more potent than that of DXM. These findings suggest that efficient drug delivery to the atherosclerotic lesions by d-lipo produces an excellent antiatherosclerotic effect at a lower dose. Therefore, d-lipo may be useful for the development of drug delivery systems for atherosclerotic therapy. PMID:16308209

  13. Determination of Fatty Acid in Asparagus by Gas Chromatography

    Zehra HAJRULAI-MUSLIU

    2016-05-01

    Full Text Available Asparagus contain a lot of macronutrients and micronutrients including folate, dietary fibre (soluble and insoluble and phenolic compounds. Also asparagus is a good source of unsaturated linoleic and linolenic fatty acids which are precursors for Eicosapentanoic acid (EPA and Docosahexanoic acid (DHA. Unsaturated fatty acids have important biological effects and they have important role in human health. The objective of this study was to analyze fatty acid composition of asparagus as a potential source of linoleic and linolenic acid - a precursor for EPA and DHA. For this reason we analyzed fifty seven samples of asparagus collected from the local market. We used AOAC 996.06 method and analyses were performed with gas chromatograph with flame-ionization detector (GC-FID. The highest concentration of fatty acid in the asparagus was linoleic acid (C18:2n6 which content in asparagus is 25.620±1.0%. Also, asparagus is good source of -linolenic fatty acid (C18:3n3 and content of this fatty acid in asparagus is 8.840±0.3%. The omega-6 to omega-3 (n6/n3 ratio in asparagus was 3.19. Polyunsaturated fatty acids (PUFAs were higher than monounsaturated fatty acids (MUFAs, and from saturated fatty acids, palmitic acid was most frequent with 24.324±1.0%. From our study we can conclude that asparagus is very good source of unsaturated fatty acids, especially linoleic and linolenic fatty acids.

  14. Susceptibility of pancreatic beta cells to fatty acids is regulated by LXR/PPARalpha-dependent stearoyl-coenzyme A desaturase.

    Karine H Hellemans

    Full Text Available Chronically elevated levels of fatty acids-FA can cause beta cell death in vitro. Beta cells vary in their individual susceptibility to FA-toxicity. Rat beta cells were previously shown to better resist FA-toxicity in conditions that increased triglyceride formation or mitochondrial and peroxisomal FA-oxidation, possibly reducing cytoplasmic levels of toxic FA-moieties. We now show that stearoyl-CoA desaturase-SCD is involved in this cytoprotective mechanism through its ability to transfer saturated FA into monounsaturated FA that are incorporated in lipids. In purified beta cells, SCD expression was induced by LXR- and PPARalpha-agonists, which were found to protect rat, mouse and human beta cells against palmitate toxicity. When their SCD was inhibited or silenced, the agonist-induced protection was also suppressed. A correlation between beta cell-SCD expression and susceptibility to palmitate was also found in beta cell preparations isolated from different rodent models. In mice with LXR-deletion (LXRbeta(-/- and LXRalphabeta(-/-, beta cells presented a reduced SCD-expression as well as an increased susceptibility to palmitate-toxicity, which could not be counteracted by LXR or PPARalpha agonists. In Zucker fatty rats and in rats treated with the LXR-agonist TO1317, beta cells show an increased SCD-expression and lower palmitate-toxicity. In the normal rat beta cell population, the subpopulation with lower metabolic responsiveness to glucose exhibits a lower SCD1 expression and a higher susceptibility to palmitate toxicity. These data demonstrate that the beta cell susceptibility to saturated fatty acids can be reduced by stearoyl-coA desaturase, which upon stimulation by LXR and PPARalpha agonists favors their desaturation and subsequent incorporation in neutral lipids.

  15. Anticancer effects of 6-o-palmitoyl-ascorbate combined with a capacitive-resistive electric transfer hyperthermic apparatus as compared with ascorbate in relation to ascorbyl radical generation

    Kato, Shinya; ASADA, RYOKO; KAGEYAMA, KATSUHIRO; SAITOH, YASUKAZU; Miwa, Nobuhiko

    2011-01-01

    The aim of the present study is to determine the anti-proliferative activity of 6-o-palmitoyl-l-ascorbic acid (Asc6Palm) that is a lipophilic derivative of l-ascorbic acid (Asc), on human tongue squamous carcinoma HSC-4 cells by combined use of hyperthermia in comparison to Asc. Asc6Palm or Asc were administered to HSC-4 cells for 1 h, to which hyperthermia at 42 °C was applied for initial 15 min. After further 1–72 h incubation at 37 °C, cell proliferation was determined with Crystal Violet ...

  16. The application of hydrogen-palladium electrode for potentiometric acid-base determinations in tetrahydrofuran

    Jokić Anja B.

    2013-01-01

    Full Text Available The application of the hydrogen-palladium electrode (H2/Pd as the indicator electrode for the determination of relative acidity scale (Es, mV of tetrahydrofuran (THF and the potentiometric titrations of acids in this solvent was investigated. The relative acidity scale tetrahydrofuran was determined from the difference half-neutralization potentials of perchloric acid and tetrabutylammonium hydroxide (TBAH, which were measured by using both H2/Pd-SCE and glass-SCE electrode pairs. The experimentally obtained value of Es scale THF with a H2/Pd-SCE electrode pair was 1155 mV, and those obtained with glass-SCE electrode pair 880 mV. By using a H2/Pd indicator electrode, the individual acids (benzoic acid, palmitic acid, maleic acid, acetyl acetone, α-naphthol and two component acid mixtures (benzoic acid + α-naphthol, palmitic acid + α-naphthol, maleic acid + α-naphthol and maleic acid + ftalic acid were titrated with a standard solution of TBAH. In addition, sodium methylate and potassium hydroxide proved to be very suitable titrating agents for titrating of the individual acids and the acids in mixtures, respectively. The relative error of the determination of acids in mixture was less than 3%. The results are in agreement with those obtained by a conventional glass electrode. The advantages of H2/Pd electrode over a glass electrode in potentiometric acid-base determinations in tetrahydrofuran lie in the following: this electrode gives wider relative acidity scale THF, higher the potential jumps at the titration end-point and relatively fast response time; furthermore, it is very durable, simple to prepare and can be used in the titrations of small volumes. [Projekat Ministarstva nauke Republike Srbije, br.172051

  17. Fatty acids composition of Spanish black (Morus nigra L.) and white (Morus alba L.) mulberries.

    Sánchez-Salcedo, Eva M; Sendra, Esther; Carbonell-Barrachina, Ángel A; Martínez, Juan José; Hernández, Francisca

    2016-01-01

    This research has determined qualitatively and quantitatively the fatty acids composition of white (Morus alba) and black (Morus nigra) fruits grown in Spain, in 2013 and 2014. Four clones of each species were studied. Fourteen fatty acids were identified and quantified in mulberry fruits. The most abundant fatty acids were linoleic (C18:2), palmitic (C16:0), oleic (C18:1), and stearic (C18:0) acids in both species. The main fatty acid in all clones was linoleic (C18:2), that ranged from 69.66% (MN2) to 78.02% (MA1) of the total fatty acid content; consequently Spanish mulberry fruits were found to be rich in linoleic acid, which is an essential fatty acid. The fatty acid composition of mulberries highlights the nutritional and health benefits of their consumption. PMID:26213011

  18. Identification of rapeseed oil fatty acid esters in transesterification reactions by gas chromatography - mass spectrometry method

    Rapeseed oil transesterification with different alcohols - methyl, ethyl, n-propyl and isopropyl alcohol - has been carried out. Yields of fatty acid alkyl esters obtained from rapeseed oil were determined using the internal standard method. Results of interpretation of the obtained ester mass spectra are reported. The specimen of Latvian rape oil contains: 57.6% of oleic acid, 18.2% of linoleic acid, 8.2% linolenic acid, 3.3% palmitic acid, 2% of stearic acid and less than 1% of arachidic acid. Values of Kovats retention indices of the rapeseed oil fatty acid esters on the capillary columns DB-5 MS and DB-17 MS have been compared. More selective separation of fatty acid alkyl esters has been achieved on the stationary phase with higher content of phenyl groups (DB-17 MS). (authors)

  19. Oil and fatty acid accumulation during coriander (Coriandrum sativum L. fruit ripening under organic cultivation

    Quang-Hung Nguyen

    2015-08-01

    Full Text Available To evaluate the accumulation of oil and fatty acids in coriander during fruit ripening, a field experiment was conducted under organic cultivation conditions in Auch (near Toulouse, southwestern France during the 2009 cropping season. The percentage and composition of the fatty acids of coriander were determined by gas chromatography. Our results showed that rapid oil accumulation started in early stages (two days after flowering, DAF. Twelve fatty acids were identified. Saturated and polyunsaturated acids were the dominant fatty acids at earlier stages (2–12 DAF, but decreased after this date. After this stage, petroselinic acid increased to its highest amount at 18 DAF. In contrast, palmitic acid followed the opposite trend. Saturated and polyunsaturated fatty acids decreased markedly and monounsaturated fatty acids increased during fruit maturation. It appears that the fruit of coriander may be harvested before full maturity.

  20. Deficits in docosahexaenoic acid and associated elevations in the metabolism of arachidonic acid and saturated fatty acids in the postmortem orbitofrontal cortex of patients with bipolar disorder.

    McNamara, Robert K; Jandacek, Ronald; Rider, Therese; Tso, Patrick; Stanford, Kevin E; Hahn, Chang-Gyu; Richtand, Neil M

    2008-09-30

    Previous antemortem and postmortem tissue fatty acid composition studies have observed significant deficits in the omega-3 fatty acid docosahexaenoic acid (DHA, 22:6n-3) in red blood cell (RBC) and postmortem cortical membranes of patients with unipolar depression. In the present study, we determined the fatty acid composition of postmortem orbitofrontal cortex (OFC, Brodmann area 10) of patients with bipolar disorder (n=18) and age-matched normal controls (n=19) by gas chromatography. After correction for multiple comparisons, DHA (-24%), arachidonic acid (-14%), and stearic acid (C18:0) (-4.5%) compositions were significantly lower, and cis-vaccenic acid (18:1n-7) (+12.5%) composition significantly higher, in the OFC of bipolar patients relative to normal controls. Based on metabolite:precursor ratios, significant elevations in arachidonic acid, stearic acid, and palmitic acid conversion/metabolism were observed in the OFC of bipolar patients, and were inversely correlated with DHA composition. Deficits in OFC DHA and arachidonic acid composition, and elevations in arachidonic acid metabolism, were numerically (but not significantly) greater in drug-free bipolar patients relative to patients treated with mood-stabilizer or antipsychotic medications. OFC DHA and arachidonic acid deficits were greater in patients plus normal controls with high vs. low alcohol abuse severity. These results add to a growing body of evidence implicating omega-3 fatty acid deficiency as well as the OFC in the pathoaetiology of bipolar disorder. PMID:18715653