Abstract:
:5 alpha-Cholest-8(14)-en-3 beta-ol-15-one is a potent inhibitor of cholesterol biosynthesis which has significant hypocholesterolemic activity upon oral administration to rodents and nonhuman primates. In the present study the metabolism of the 15-ketosterol has been investigated after the oral administration of a mixture of [2,4-3H]5 alpha-cholest-8(14)-en-3 beta-ol-15-one and [4-14C]cholesterol to 8 baboons. Blood samples were obtained at 4, 8, 12, 16, and 24 h after administration of the labeled sterols. Clear differences in the time courses of the levels of 3H and 14C in plasma were observed. 3H in plasma showed maximum values at 4 to 8 h, whereas maximum values for the levels of 14C were observed much later. 3H in plasma was shown to be primarily in the form of its metabolites, i.e. esters of the 15-ketosterol, cholesterol, and cholesteryl esters. The levels of the 15-ketosterol and of each of these metabolites showed different changes with time. The labeled cholesterol (and the cholesterol moiety of the cholesteryl esters), formed from the [2,4-3H]-15-ketosterol, was characterized by chromatography and by purification by way of its dibromide derivative. At 24 h after the administration of the labeled sterols, the distribution of 3H in plasma lipoprotein fractions paralleled that of 14C, with most of the 3H and 14C in high density lipoprotiens (HDL) and low density lipoproteins (LDL). Almost all of the 3H in HDL and in LDL was found as cholesterol, cholesteryl esters and esters of the 15-ketosterol. The distribution of 3H in HDL and in LDL of the free 15-ketosterol, esters of the 15-ketosterol, cholesterol, and cholesteryl esters was similar to that of plasma, thereby indicating no unusual concentration of any of the 3H labeled components in HDL or LDL.
journal_name
Chem Phys Lipidsjournal_title
Chemistry and physics of lipidsauthors
Pajewski TN,Brabson JS,Kisic A,Wang KS,Hylarides MD,Jackson EM,Schroepfer GJ Jrdoi
10.1016/0009-3084(89)90072-8subject
Has Abstractpub_date
1989-03-01 00:00:00pages
243-63issue
4eissn
0009-3084issn
1873-2941pii
0009-3084(89)90072-8journal_volume
49pub_type
杂志文章abstract::The dicyclohexylborane-mediated addition of allene 1 to (E)-2-tridecenal affords a quaternary protected 2-amino-2-vinyl-1,3-diol in good yield as a single diastereomer. This compound is readily transformed into the four stereoisomers of the quaternary (E)-2-vinyl analogs of sphingosine. The metabolic fate and the effe...
journal_title:Chemistry and physics of lipids
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journal_title:Chemistry and physics of lipids
pub_type: 临床试验,杂志文章,多中心研究
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abstract::Infarcted porcine heart tissue and surrounding tissue were investigated for the content of plasmalogens and oxidatively derived corresponding alpha-hydroxyaldehydes as well as for products of lipid peroxidation, e.g. malondialdehyde, glyoxal, 2-hydroxyheptanal and oxygenated fatty acids. Oxidation products of unsatura...
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abstract::Racemic 1-O-(2-methyloctadecyl)-2-O-acetyl-glycero-3-phosphocholine, a branched chain PAF species, was prepared by chemical synthesis and investigated for biological activity on human blood platelets in vitro. The synthesis started from 2-O-benzylglycerol and 2-methyloctadecyl-1-methyl sulfonate and was accomplished i...
journal_title:Chemistry and physics of lipids
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journal_title:Chemistry and physics of lipids
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doi:10.1016/s0009-3084(99)00101-2
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journal_title:Chemistry and physics of lipids
pub_type: 杂志文章
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更新日期:2002-05-01 00:00:00
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journal_title:Chemistry and physics of lipids
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journal_title:Chemistry and physics of lipids
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