bluuebunny/crossref_metadata_2025_split huggingface dataset:
The pharmacokinetics of water‐in‐oil‐in‐water‐type multiple emulsion of a new tacrolimus formulation
Authors: Uno Takeji , Yamaguchi Takaji , Li Xiao Kang , Suzuki Yoshinari , Hashimoto Hisakuni , Harada Yukio , Kimura Taizou , Kazui Teruhisa 
Published: November 2006

AbstractWe developed a water‐in‐oil‐in‐water (W/O/W)‐type multiple emulsion of a new tacrolimus formulation. A potential approach to avoid the complications of systemic immunosuppression and simultaneously enhance immunosuppressive efficacy is to deliver immunosuppressive agents locally to the site of the target organs. The W/O/W emulsion is dispersed oil drops containing smaller water droplets that allow the delivery of drugs preferentially to the reticuloendothelial system (RES). Since the liver and the spleen are primary components of the RES, and the brain and the kidney have a poor RES, we hypothesized that a W/O/W emulsion of tacrolimus would prossess the pharmacokinetic benefits of local immunosuppression. We evaluated this hypothesis in a rat model. The tacrolimus levels of whole blood, the liver, spleen, brain, and kidney in rats given intravenous emulsions of tacrolimus (W/O/W group) were compared with a group administered tacrolimus alone (T group). There were no significant differences between the pharmacokinetic parameters of W/O/W group and T group based on whole blood data. However, the W/O/W group had significantly decreased tacrolimus levels in the brain and kidney, and significantly increased levels in the liver and spleen compared with the T group. These data suggest that the W/O/W emulsion is applicable as an intravenous drug carrier for local immunosuppression.
Structure analysis of an allene‐containing estolide tetraester triglyceride in the seed oil of Sebastiana commersoniana (Euphorbiaceae)
Authors: Spitzer Volker , Tomberg Werner , Pohlentz Gottfried 
Published: November 2006

AbstractThe seed oil of Sebastiana commersoniana (Euphorbiaceae) was separated into a triglyceride and an estolide fraction by preparative thin‐layer chromatography. The triglyceride band was characterized by spectroscopic methods, and its fatty acids have been analyzed by gas chromatography (GC) and GC‐mass spectrometry (MS) and their methyl esters. Linolenic acid was the main fatty acid (65%). The estolide band was examined by a combination of spectroscopic and chromatographic methods (ultraviolet, infrared, nuclear magnetic resonance, fast atom bombardment‐MS, GC‐MS of the fatty acids before and after silylation) and was identified as a tetraglyceride, where on α‐carbon of the glyceride backbone was esterfied with 8‐hydroxy‐5,6‐octadienoic acid, which itself was esterfied with trans‐2,cis‐4‐decadienoic acid. The remaining positions of the glyceride backbone were occupied by common fatty acids.
Thermotropic phase behavior of in vivo extracted human stratum corneum lipids
Authors: Bonté Frédéric , Pinguet Patrick , Saunois Alex , Meybeck Alain , Beugin Sophie , Ollivon Michel , Lesieur Sylviane 
Published: November 2006

AbstractThe thermotropic phase behavior of lipids extracted either in vivo from inner forearm (SCLE) or plantar callus (PC) was investigated by differential scanning calorimetry and small angle X‐ray diffraction. PC composition was chromatographically modified (MPC) by eliminating the more polar lipids in order to evaluate their role. Analysis of composition confirms the potential use of PC as a source of stratum corneum lipids. MPC and SCLE exhibit similar differential scanning calorimetry (DSC) profiles with a main transition around 50°C attributed to the solid‐to‐liquid phase transition of the ceramides. The absence of a transition around 50°C for PC suggests the possible perturbation of ceramide packing by the significantly high proportion of phospholipids. X‐ray data suggest a high miscibility of sebum components in stratum corneum lipids with possible modification of chain packing. The MPC patterns show a lipid phase separation which underscores the role of polar lipids in cholesterol/free fatty acids/sterol esters/ceramides structural cohesion.
Heneicosapentaenoate (21:5n−3): Its incorporation into lipids and its effects on arachidonic acid and eicosanoid synthesis
Authors: Larsen L. N. , Høvik K. , Bremer J. , Holm K. H. , Myhren F. , Børretzen B. 
Published: November 2006

Abstract6,9,12,15,18‐Heneicosapentaenoic acid (21:5n‐3) (HPA), present in small amounts in fish oils, has been prepared by chemical elongation of eicosapentaenoic acid (EPA) and its biological properties compared with EPA and docosahexaenoic acid (DHA). All the double bonds of HPA are displaced one carbon away from the carboxyl group when compared to EPA. HPA is incorporated into phospholipids and into triacylglycerol in cell culture to a similar extent as EPA and DHA. HPA is a stronger inhibitor of the conversion of α‐linoleic acid and dihomo‐γ‐linolenic acid to arachidonic acid (AA) in hepatoma cells than are EPA, DHA, and AA. HPA is a poor substrate for prostaglandin H synthase and for 5‐lipoxygenase, but it inactivates prostaglandin H synthase as rapidly as do AA, EPA, and DHA. HPA inhibits thromboxane synthesis in isolated platelets as efficiently as EPA. EPA, HPA, and DHA are all weak inducers of acyl‐CoA oxidase in hepatoma cells. Therefore, since fish oils contain only small amounts of HPA, it is unlikely that this fatty acid is of particular significance for the biological effects of these oils, possibly with the exception that it is a strong inhibitor of AA synthesis.
Characterization of an HL‐60 cell variant resistant to the antineoplastic ether lipid 1‐O‐octadecyl‐2‐o‐methyl‐rac‐glycero‐3‐phosphocholine
Authors: Small George W. , Strum Jay C. , Daniel Larry W. 
Published: November 2006

AbstractA resistant cell line (HL‐60R) was selected by incubating HL‐60 cells with increasing concentrations of 1‐O‐octadecyl‐2‐O‐methyl‐rac‐glycero‐3‐phosphocholine (ET‐18‐OCH3) and used to examine the mechanism of resistance to the antineoplastic ether‐linked lipid. The HL‐60R cells exhibited a>10‐fold increase in resistance when measured by [3H]‐thymidine incorporation in comparison to the HL‐60 cell line. ET‐18‐OCH3 binding occurred at 4°C and was not saturable at the concentrations tested (1–100 μM), indicating that the binding was receptor‐independent. At 4°C, association of ET‐18‐OCH3 was low for each cell line. At 37°C, uptake in the HL‐60 cells was approximately 5‐fold greater in comparison to HL‐60R cells at each concentration tested. However, when the cellular content of ET‐18‐OCH3 was equal, both cell lines experienced similar declines in cell growth. Cellular incorporation of ether lipid was determined using serum‐free media and in the presence of serum albumin or lipoproteins. Reduced uptake by the resistant cell line was observed only in the presence of albumin. A greater proportion of ether lipid could be removed from prelabeled HL‐60R cells than from HL‐60 cells, by an albumin wash procedure, indicating an increased rate of internalization and retention by the sensitive cell line. ET‐18‐OCH3 uptake in the HL‐60 cell line was also more sensitive to treatment with endocytic (chloroquine, monensin) or metabolic (NaF, KCN) inhibitors. These results suggest that uptake is the principal determinant influencing sensitivity of the resistant cell line and consists of receptor‐independent binding followed by internalization. Differential uptake requires the presence of serum albumin and is dependent on the energy‐dependent endocytosis of the ether lipid.
Conjugated linoleic acid modulation of phorbol ester‐induced events in murine keratinocytes
Authors: Liu Kai‐Li , Belury Martha A. 
Published: November 2006

AbstractRecent work in our lab has shown that the chemoprotective fatty acid, conjugated linoleic acid (CLA), inhibits phorbol ester skin tumor promotion in mice. Because little is known about the deposition of CLA into tissues as well as its biological activity, this study compared the incorporation and biological activity of CLA to linoleic acid (LA; 18:2, c9, c12) and arachidonic acid (AA; 20:4 c5, c8, c11, c14) in cultured keratinocytes. When keratinocytes (HEL‐30) were grown in media containing 14C‐CLA for various periods, more than 50% of the 14C‐CLA was incorporated into cellular lipids by 9 h. The distribution of CLA in phospholipid classes was similar to LA. Approximately 50% of 14C‐LA and 14C‐CLA were incorporated into phosphatidylcholine (PC), while the remainder was taken up by phosphatidylethanolamine (PE) and phosphatidyl‐serine/phosphatidylinositol (PS/PI). In contrast, 14C‐AA was more equitably distributed into PC, PE, or PS/PI (27, 30, or 38%, respectively). When keratinocytes were prelabeled with radiolabeled fatty acids, phorbol ester‐induced release of 14C‐CLA was 1.5 times higher than 14C‐LA and 14C‐AA. However, 14C‐prostaglandin E (PGE) release in 14C‐CLA prelabeled cultures was 6 and 13 times lower than cultures treated with 14C‐LA and 14C‐AA, respectively. Moreover, the ability of nonradiolabeled CLA to support ornithine decarboxylase activity, a hallmark event of tumor promotion, was significantly lower than in LA‐ and AA‐treated cultures. These studies suggest that CLA inhibits skin tumor promotion, in part, through a PGE‐de‐pendent mechanism.
Unusual effects of some vegetable oils on the survival time of stroke‐prone spontaneously hypertensive rats
Authors: Huang Min‐Zhao , Watanabe Shiro , Kobayashi Tetsuyuki , Nagatsu Akito , Sakakibara Jinsaku , Okuyama Harumi 
Published: November 2006

AbstractPreliminary experiments have shown that a diet containing 10% rapeseed oil (low‐erucic acid) markedly shortens the survival time of stroke‐prone spontaneously hypertensive (SHRSP) rats under 1% NaCl loading as compared with diets containing perilla oil or soybean oil. High‐oleate safflower oil and high‐oleate sunflower oil were found to have survival time‐shortening activities comparable to that of rapeseed oil; olive oil had slightly less activity. A mixture was made of soybean oil, perilla oil, and triolein partially purified from high‐oleate sunflower oil to adjust the fatty acid composition to that of rapeseed oil. The survival time of this triolein/mixed oil group was between those of the rapessed oil and soybean oil groups. When 1% NaCl was replaced with tap water, the survival time was prolonged by ∼80%. Under these conditions, the rapeseed oil and evening primrose oil shortened the survival time by ∼40% as compared with n‐3 fatty acid‐rich perilla and fish oil; lard, soybean oil, and safflower oil with relatively high n‐6/n‐3 ratios shortened the survival time by roughly 10%. The observed unusual survival time‐shortening activities of some vegetable oils (rapeseed, high‐oleate safflower, high‐oleate sunflower, olive, and evening primrose oil) may not be due to their unique fatty acid compositions, but these results suggest that these vegetable oils contain factor(s) which are detrimental to SHRSP rats.
γ‐linolenic acid‐containing diet attenuates bleomycin‐induced lung fibrosis in hamsters
Authors: Ziboh Vincent A. , Yun Monica , Hyde Dallas M. , Giri Shri N. 
Published: November 2006

AbstractAlthough bleomycin (BLM), an antineoplastic drug, is used in the treatment of a variety of tumors, the mechanism(s) that contribute to its induced lung injury and fibrosis are not fully elucidated. Since alterations in the levels of certain fatty acid metabolites have been associated with BLM‐induced lung injury, we tested the effects of dietary γ‐linolenic acid (GLA)‐containing evening primrose oil on BLM‐induced morphological alterations in the hamster lung, the marked elevation of tissue hydroxyproline (a marker for collagen synthesis), and elevated generation of arachidonic acid metabolites (marker of inflammatory mediators). Our data revealed that after 14 d of dietary GLA‐containing oil (i) BLM‐induced elevation of lung hydroxyproline was suppressed (P<0.05), (ii) the marked BLM‐induced elevation of lung leukotriene B4 (LTB4) (a marker of polymorphonuclear generation of proinflammatory LTB4) was significantly suppressed (P<0.05). The decrease in LTB4 was accompanied by marked elevations (P<0.05) of lung prostaglandin E1 (PGE1) and 15‐hydroxyeicosatrienoic acid (15‐HETrE), both with known antiinflammatory properties. Taken together, data from these studies suggest that dietary GLA‐containing oil contributes to tissue elevation of PGE1 and 15‐HETrE, which in vivo may attenuate lung inflammation and fibrosis.
Oleanolic acid and ursolic acid stabilize liposomal membranes
Authors: Han Suk Kyu , Ko Young Ill , Park Soo Jung , Jin In Jung , Kim Young Mi 
Published: November 2006

AbstractThe effects of oleanolic acid (OA) and ursolic acid (UA) on the fluidity and stability of dipalmitoyl phosphatidylcholine (DPPC) liposomal membrane were monitored by measuring the fluorescence polarization of 1,6‐diphenyl‐1,3,5‐hexatriene labeled in the liposomal membrane and the leakage of calcein from the probe‐encapsulated liposomes. The experiments with the liposomes made of DPPC and OA or UA showed that OA and UA exhibited a moderate fluidity‐modulating effect for the liquid‐crystalline liposomal membrane, and a strong condensing effect for both crystalline and liquid‐crystalline liposomal membranes. Their effects were comparable to those of cholesterol. These results suggest that their fluidity‐modulating and condensing effects might have some implications in their biological functions.
Structural characterization of a “Signature” phosphatidylethanolamine as the major 10‐hydroxy stearic acid‐containing lipid of Cryptosporidium parvum oocysts
Authors: Schrum David P. , Alugupalli Srinivas , Kelly Sean T. , White David C. , Fayer Ronald 
Published: November 2006

AbstractA 10‐hydroxy stearic acid‐containing lipid from Cryptosporidium parvum was purified by thin‐layer chromatography and analyzed by infrared spectroscopy, fast‐atom bombardment mass spectrometry, 1H and 31P nuclear magnetic resonance spectroscopy, and was identified as phosphatidylethanolamine.
Capillary supercritical fluid chromatography‐atmospheric pressure chemical ionization mass spectrometry of γ‐ and α‐linolenic acid containing triacylglycerols in berry oils
Authors: Manninen Pekka , Laakso Päivi 
Published: November 2006

AbstractThe effect of the γ‐linolenic acid (18:3n‐6) residue on the elution of triacylglycerols on a 25% cyanopropyl‐25% phenyl‐50% methylpolysiloxane stationary phase was confirmed by using capillary supercritical fluid chromatography‐atmospheric pressure chemical ionization mass spectrometry [cSFC‐(APCI)MS]. The general elution rule on this stationary phase is that triacylglycerols having the same ACN+2n value coeluted (ACN‐acyl carbon number and n=combined number of double bonds in the acyl chains). The different effect of γ‐ and α‐linolenic acid residues on the retention of triacylglycerols and the use of cSFC‐(APCI)MS allowed the study of the number of different linolenic acid residue isomer combinations in triacylglycerols with an identical ACN and degree of unsaturation. Stearidonic acid (18:4n‐3) residue was found to have a similar effect on the retention behavior of triacylglycerols as that of γ‐linolenic acid residue. The abundance of the [M‐RCOO]+ ion, formed by the loss of one fatty acid moiety of a triacylglycerol, was found to be clearly higher in the case of γ‐isomer of the linolenic acid than that of α‐isomer in the identical regiospecific position. This indicates that the distance of the double bonds from the glycerol backbone in the acyl chain affects the stability of a triacylglycerol molecule in the (APCI)MS system. The triacylglycerol composition and the fatty acid combinations of triacylglycerols were found to be almost identical in black currant (Ribes nigrum) and alpine currant (R. alpinum) seed oils.
Correlation of suppressed linoleic acid metabolism with the hypocholesterolemic action of eritadenine in rats
Authors: Sugiyama Kimio , Yamakawa Akihiro , Saeki Shigeru 
Published: November 2006

AbstractThe dose‐dependent effects of dietary eritadenine on the metabolism of linoleic acid and on the plasma cholesterol concentration were investigated to clarify the mechanism of the hypocholesterolemic action of eritadenine in rats. Rats were fed control or eritadenine‐supplemented (2 to 20 mg/kg) diets for 14 d. Eritadenine supplementation significantly decreased both the plasma cholesterol concentration and the 20∶4n−6/18∶2n−6 ratio of liver microsomal and plasma phosphatidylcholine (PC) in a dose‐dependent manner. Eritadenine was also found to decrease the activity of Δ6 desaturase in liver microsomes; these was significant correlation between the Δ6‐desaturase activity and the 20∶4n−6/18∶2n−6 ratio in the PC of liver microsomes (r=0.989, P<0.001) or plasma (r=0.986, P<0.001). Certain plasma PC molecular species, as represented by 16:0‐18:2, were increased by eritadenine in a dose‐dependent manner, and certain plasma PC molecular species, as represented by 18:0‐20:4, were conversely decreased by eritadenine. There was a significant correlation between the plasma total cholesterol concentration and the proportion of the sum of plasma PC molecular species which contain 18:1 or 18:2 in the sn‐2 position. These results support the idea that the suppression of linoleic acid metabolism by eritadenine might be associated with the hypocholesterolemic action of eritadenine.
Effect of trifluoperazine on certain arterial wall lipid‐metabolizing enzymes inducing atherosclerosis in rhesus monkeys
Authors: Mohindroo A. , Ahluwalia P. 
Published: November 2006

AbstractThe effect of trifluoperazine (TFP) was investigated on arterial wall lipid‐metabolizing enzymes like acyl‐CoA:cholesterol acyltransferase (ACAT) and cholesterol ester hydrolase (CEH) in rhesus monkeys. The activity was determined in aortic wall homogenates obtained from rhesus monkeys fed an atherogenic diet coupled with intramuscular injections of adrenaline and TFP. Although TFP had no significant effect on serum cholesterol and triglycerides, it decreased significantly the formation of atherosclerotic lesions by decreasing the esterification of cholesterol, by inhibiting ACAT and enhancing its utilization by activating CEH. Hence, the preventive effect of TFP on the development of atherosclerosis in rhesus monkeys is mediated through its ability to influence the activities of arterial wall lipid‐metabolizing enzymes like ACAT and CEH.
Facile and general method for preparation of (E)‐4‐hydroxy‐2‐alkenals
Authors: Sugamoto Kazuhiro , Matsushita Yoh‐ichi , Matsui Takanao 
Published: November 2006

AbstractA facile one‐pot synthesis of (E)‐4‐hydroxy‐2‐alkenals such as (E)‐4‐hydroxy‐2‐nonenal, (E)‐4‐hydroxy‐2‐heptenal, and (E)‐4‐hydroxy‐2‐hexenal was achieved from the corresponding (2E,4E)‐2,4‐alkadienals by reduction‐oxygenation with molecular oxygen and triethylsilane in the presence of cobalt(II) porphyrin as a catalyst followed by treatment with trimethylphosphite.
Effects of oxidative stress on glycerolipid acyl turnover in rat hepatocytes
Authors: Girón‐Calle Julio , Schmid Patricia C. , Schmid Harald H. O. 
Published: November 2006

AbstractLipid peroxidation was induced in freshly isolated rat hepatocytes by incubation in the presence of Fe3+, resulting in accumulation of thiobarbituric acid reactive substances. Analysis of lipid classes revealed that the levels and fatty acid compositions of the two major phospholipids, phosphatidylcholine (PC) and phosphatidylethanolamine (PE), remained unchanged but the levels of triacylglycerols (TAG) were significantly reduced, and some of their polyunsaturated fatty acids were selectively lost as the result of oxidant treatment. Acyl turnover in PC and PE as determined by 18O incorporation from H218O‐containing media remained largely unchanged during oxidant treatment, while some increased turnover of the saturated fatty acids in TAG was observed. We hypothesize that constitutive recycling of membrane phospholipids rather than selective in situ repair eliminates peroxidized species of PC and PE, TAG could serve as an expendable fatty acid reserve, providing a limited but very dynamic pool of polyunsaturated fatty acids for the resynthesis of phospholipids.
The effects of cyclic fatty acid monomers on cultured porcine endothelial cells
Authors: Flickinger Brent D. , McCusker Robert H. , Perkins Edward G. 
Published: November 2006

AbstractThe popularity of polyunsaturated oils used in food applications and preparation continues to appreciate as a result of positive health claims. With polyunsaturated oils inherently more susceptible to oxidative and thermal degradation, the formation of new fatty acid species increases considerably. The presence of one species known as cyclic fatty acid monomers (CFAM) has been detected as a component of many oils subjected to various thermal processes including deep‐fat frying. The effect of CFAM on metabolic processes has not been fully characterized. In this study, confluent porcine aortic endothelial cells incorporated CFAM into their polar and nonpolar lipid fractions following a 48‐h exposure to 31 and 62 ppm CFAM in the culture medium. Subsequently, the influence of CFAM incorporation on various membrane‐dependent physical properties and biochemical processes was investigated. CFAM decreased the lipid packing order of the membrane bilayer core but did not alter the lipid packing order of lipid chain segments at or near the lipid‐water interface of the membrane. CFAM led to significant reductions in Ca2+ ATPase activity and monolayer integrity while eliciting a significant increase of prostacyclin synthesis and secretion.
Failure of the nonselective β‐blocker propranolol to affect lipoprotein lipase gene expression in the rat
Authors: Gouni‐Berthold I. , Oka K. , Berthold H. K. , Chan L. 
Published: November 2006

AbstractTreatment with β‐blockers has been reported to be associated with the development of hypertriglyceridemia. The etiology, even the existence, of this phenomenon is controlverisal. The purpose of our study was to examine whether the nonselective β‐blocker propranolol causes hypertriglyceridemia in the rat and whether its action is mediated by the modulation of lipoprotein lipase (LPL) messenger RNA (mRNA) accumulation or activity. LPL activity was assayed in fresh tissue by incubation with tritiated triglycerides. LPL mRNA was quantified in total RNA by slot‐blot analysis using a mouse LPL complementary DNA probe. We have conducted three series of experiments in unanaesthetized rats in order to study the effects of different single doses of propranolol (1.5 to 6 mg i.p.) and different durations of treatment (15 min to 4 wk). We measured triglyceride and cholesterol levels in plasma as well as the LPL activity and mRNA levels in the heart and adipose tissue before and after propranolol administration. In these experiments we did not find any significant decrease in either the activity or the amount of mRNA of lipoprotein lipase nor was there any change in plasma lipids following treatment. Our results lead us to the conclusion that the nonselective β‐blocker propranolol affects neither the activity nor, the mRNA level of LPL in the rat.