Abstract:
:Various derivatives and isosteres of neolignans of the 2,5-diaryl tetrahydrofuran type have been synthesized as antagonists of platelet-activating factor (PAF). A detailed analysis of their structure-activity relationship (SAR) has revealed a clear preference for an asymmetrical molecular configuration with a high degree of stereo and chiral specificity associated with greater potency. The trans-2S,5S enantiomers are generally 10-200 times more potent in vitro than their corresponding cis or trans-2R,5R isomers. A similar stereochemical preference is indicated by the recently reported PAF antagonist MK-287 which has undergone clinical evaluation. An azido derivative L-662,025 has been characterized as a photolabile irreversible antagonist of PAF for the investigation of solubilized and partially purified PAF binding proteins from cell membranes. The biological justification for concomitant inhibition of both PAF receptor and 5-lipoxygenase in inflammation is well recognized. The feasibility of developing such dual-functional agents has been demonstrated by a group of dithiolane analogs of neolignans and several derivatives of futoenone.
journal_name
Lipidsjournal_title
Lipidsauthors
Shen TYdoi
10.1007/BF02536521subject
Has Abstractpub_date
1991-12-01 00:00:00pages
1154-6issue
12eissn
0024-4201issn
1558-9307journal_volume
26pub_type
杂志文章,评审相关文献
LIPIDS文献大全abstract::Conjugated linoleic acid (CLA) has been shown to cause a reduction in obesity in several species. CLA-induced body fat loss is enhanced when mice are fed coconut oil (CO) and involves increased lipolysis. The objective of this paper was to determine if the CLA-induced lipolysis in mice fed with different oil sources w...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-013-3835-x
更新日期:2013-11-01 00:00:00
abstract::We have studied the effect of various diets on the phospholipid fatty acid composition and in vitro delta 5 desaturase activity of hepatic microsomes derived either from the normal or streptozotocin-induced diabetic rat. The diets studied were the standard rat chow diet and a basal fat-free diet supplemented either wi...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02535763
更新日期:1989-10-01 00:00:00
abstract::During germination of seeds of the gymnosperm, Pinus pinea, radioactivity from [2-14C]-mevalonate proceeded principally through the anaerobic reactions leading to squalene in the first 24 hr in both the haploid endosperm and the diploid embryo, and only with succeeding time (3-9 days) in both cases was label transferr...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02533642
更新日期:1977-04-01 00:00:00
abstract::Recent reports show that a fatty meal can substantially increase the concentration of oxidized lipids in low density lipoprotein (LDL). Knowing the LDL-specific antioxidant effects of high density lipoprotein (HDL), we aimed to investigate whether HDL can modify the postprandial oxidative stress after a fatty meal. Su...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-014-3963-y
更新日期:2014-12-01 00:00:00
abstract::In experiments with 4 different types of cells, we evaluated the cholesterogenic activity by incorporation of 14C-acetic acid into cholesterol and digitonin-precipitable sterols. In every case, the cholesterogenesis appeared considerably faster when expressed as digitonid than when expressed as real cholesterol produc...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02534676
更新日期:1983-09-01 00:00:00
abstract::The monoazaaromatics, pyridine (1), hexyl nicotinate (2), and quinoline (3) and diazaaromatics, pyrimidine (4) and purine (5), readily act as photo-initiators for the peroxidation of methyl linoleate in 0.50 M SDS at 37 degrees C giving free radical chain oxidations of linoleate. Quantitative kinetic runs on the order...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-997-0030-3
更新日期:1997-03-01 00:00:00
abstract::The conversion of [14C]-labeled compounds such as acetate, glucose, pyruvate and palmitate into CO2, glyceride-glycerol, glyceride fatty acids and total lipids was monitored in the average and matching adipocyte (with respect to size) preparations from young (6-9 wk) and old (age 56-60 wk) male Sprague-Dawley rats. Th...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02536404
更新日期:1986-07-01 00:00:00
abstract::Orally administered dihomo-gamma-linolenic acid (DHLA) is well absorbed in man; it appears in blood after ca. 4 hr first as triglyceride ester and later as phospholipid. After sustained-dosing, DHLA penetrated membrane pools and all phospholipid components but, depending on the dosage, reached a metabolic equilibrium ...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02533869
更新日期:1979-02-01 00:00:00
abstract::Using primary rat hepatocyte cultures, the potency of several garlic-derived organosulfur compounds to inhibit cholesterol biosynthesis in toto as well as at early and late steps of this metabolic pathway was compared. Concerning early steps, allicin significantly inhibited incorporation of [14C]acetate into nonsaponi...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02587912
更新日期:1996-12-01 00:00:00
abstract::U-57,908 (RHC 80267) was shown to inhibit lipoprotein lipase (LPL) activity in cardiac myocytes from rat hearts; the concentrations required for inhibition to 50% of control activity were 1.1 microM and 2.5 microM for myocyte homogenates and a post-heparin medium preparation, respectively. The inhibition of LPL activi...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02536481
更新日期:1992-04-01 00:00:00
abstract::Inflammatory disorders are associated with a decrease in iron absorption because of the blockade of iron in storage organs. Fish oils, rich in n-3 PUFA, are used to prevent and treat inflammatory disorders and increase iron absorption in noninflamed rats. Here we examine whether n-3 PUFA prevent inflammation-related h...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-003-1131-8
更新日期:2003-08-01 00:00:00
abstract::The effects of aging on the hepatic metabolism of cholesterol were studied in 1-, 6- and 24-month-old male Sprague-Dawley rats. Microsomal 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase activity, which regulates cholesterol biosynthesis, decreased from 835 +/- 144 (SEM) pmol/min/mg protein in the youngest g...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02537197
更新日期:1991-05-01 00:00:00
abstract::A patient with classic Zellweger syndrome was treated with docosahexaenoic acid ethyl ester (DHA-EE) for three months. Five other patients with Zellweger variants (four of them less than one-year-old and a five-year-old) were treated with DHA-EE until normalization of the DHA levels in erythrocytes. When arachidonic a...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02637067
更新日期:1996-03-01 00:00:00
abstract::The purpose of the present investigation was to test whether permanent skeletal muscle cells (rat L6 cells) could serve as an in vitro model for alpha-tocopherol (alphaTocH) biodiscrimination studies. L6 cells were incubated in the presence of high density lipoprotein (HDL), low density lipoprotein (LDL), and very low...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-998-0298-3
更新日期:1998-10-01 00:00:00
abstract::It has been shown that different lysophosphatidylcholines (LPC) possess relaxing properties in vascular strips. We report on the effect of intraatrial injection of LPC micelles into white New Zealand rabbits. Changes in renal and coronary flow were determined by radioactive microspheres. Coronary blood flow increased ...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02543975
更新日期:1991-03-01 00:00:00
abstract::The effects of droplet size and emulsifiers on oxidative stability of polyunsaturated TAG in oil-in-water (o/w) emulsions with droplet sizes of 0.806 +/- 0.0690, 3.28 +/- 0.0660, or 10.7 +/- 0.106 microm (mean +/- SD) were investigated. Hydroperoxide contents in the emulsion with a mean droplet size of 0.831 microm we...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-005-1410-4
更新日期:2005-05-01 00:00:00
abstract::Phospholipids are integral constituents of the milk fat globule membranes and they play a central role in infants' immune and inflammatory responses. A methodology employing liquid chromatography coupled with evaporative light scattering detector has been optimized and validated to quantify the major phospholipids cla...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-013-3825-z
更新日期:2013-10-01 00:00:00
abstract::Various physical fractions of the barley kernel were fed to one-day-old female and male chickens to determine their effect on hepatic beta-hydroxy-beta-methylglutaryl coenzyme A (HMG-CoA) reductase, cholesterol 7 alpha-hydroxylase and the lipogenic enzymes, acetyl-CoA carboxylase (ACX), malic enzyme (ME), citrate-clea...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02534592
更新日期:1982-12-01 00:00:00
abstract::Apolipoprotein E (apo E) plays an essential role in lipoprotein metabolism, where it is involved in the clearance of chylomicrons and very low density lipoproteins. Apart from some rare variants, apo E exists in three common isoforms (E2, E3, and E4). The different isoforms have not only been associated with different...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-000-0500-7
更新日期:2000-01-01 00:00:00
abstract::Tissue and blood fatty acid compositions are used as biological markers of fatty acid intakes to improve dietary assessments. These approaches are invasive and not well accepted, particularly in infants and young children. We developed a sensitive method for the analysis of fatty acids in cheek cell glycerophospholipi...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-011-3576-7
更新日期:2011-10-01 00:00:00
abstract::The effect of ethanol on the fatty acid desaturation by rat liver has been studied using liquid diets of different composition. Acute ethanol administration increased triacylglycerols of total liver lipids, but did not modify significantly the lipidic composition of microsomes. The delta 6 and delta 5 desaturases were...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02535837
更新日期:1980-04-01 00:00:00
abstract::Lipid-enriched diets have been related to a high cancer incidence in experimental animals for many years, and more recently, to assorted defects on the immune response. We investigated the effect of incubating human or murine (C3H/HEJ) lymphocytes with saturated (16:0) and unsaturated (18:1, 18:2, 18:3, 20:4) fatty ac...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02534659
更新日期:1982-10-01 00:00:00
abstract::The effects of SMP-500, a novel ACAT inhibitor, on serum lipid levels, hepatic lipid secretion rate, and hepatic lipid disposition in rats were studied to clarify its lipid-lowering action. SMP-500 reduced the serum cholesterol level in a dose-dependent manner in rats fed a hypercholesterolemic diet. SMP-500 also redu...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s1145-002-0907-1
更新日期:2002-04-01 00:00:00
abstract::We describe a method for the quantitative analysis of molecular species of diacylglycerol and alkylacylglycerol as their diradylglycerobenzoate derivatives. Synthetic internal standards were used to provide quantitative determinations of the low levels of diacylglycerol and alkylacylglycerol and their individual molec...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02544045
更新日期:1990-11-01 00:00:00
abstract::The effect of various physicochemical forms of substrate on the activity of acid cholesteryl ester hydrolase isolated from rat liver lysosomes was studied. The amount of sodium taurocholate was varied in the substrate mixture which contained constant amounts of egg phosphatidylcholine (PC) and cholesteryl oleate. The ...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02535632
更新日期:1986-08-01 00:00:00
abstract::A method for the simultaneous quantitative analysis of prostaglandin E2 (PGE2) and PGE3 is described. The PG were analyzed by selected ion monitoring as the methyl ester-TMS ether derivatives of PGB2 and PGB3, respectively. The internal standard for the quantification of both species was [3,3,4,4-2H4]PGE2. A linear re...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02535360
更新日期:1982-11-01 00:00:00
abstract::An effective resolution of intact phosphatidylserines on the basis of unsaturation has been achieved by conventional argentation thin layer chromatography (TLC) following trifluoracetylaction. The trifluoroacetamides are prepared by treatment with trifluoroacetic anhydride or N-methyl-bis-trifluoroacetamide. The aceta...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02533377
更新日期:1977-07-01 00:00:00
abstract::The physiological role of long-chain fatty acyl-CoA is thought to be primarily in intermediary metabolism of fatty acids. However, recent data show that nM to microM levels of these lipophilic molecules are potent regulators of cell functions in vitro. Although long-chain fatty acyl-CoA are present at several hundred ...
journal_title:Lipids
pub_type: 杂志文章,评审
doi:10.1007/BF02522684
更新日期:1996-09-01 00:00:00
abstract::The influence of dietary TAG source (fish oil, triolein, and coconut oil) and level (7.5 and 15% of the diet) on growth, lipase activity, and mRNA level was studied in sea bass larvae, from mouth opening until day 24 and from day 37 to 52. Fish oil and triolein induced better growth in both experiments, this being sig...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/s11745-004-1250-2
更新日期:2004-05-01 00:00:00
abstract::Acid cholesteryl ester hydrolase (CEH) activity was assayed in mononuclear cells of patients with symptomatic atherosclerosis (transient ischemic attacks, TIA) and in age-matched controls showing no evidence of atherosclerosis. The acid CEH level of TIA patients was significantly lower than that of controls (1074 +/- ...
journal_title:Lipids
pub_type: 杂志文章
doi:10.1007/BF02534317
更新日期:1980-12-01 00:00:00