Abstract:
:Epidemiological studies support an inverse correlation between HDL-C and cardiovascular disease. However, low HDL-C levels do not always segregate with premature disease. These include, LCAT deficiency and the apolipoproteinA-IMilano (AIM) variant. AIM has a cysteine for arginine at position 173 in the otherwise cysteine free protein permitting AIM homodimerization and apoA-II heterodimerization. We relate the biochemical characteristics of low HDL-C phenotype AIM carriers to lipoprotein changes in humans administered recombinant dimeric AIM/palmitoyl-oleoyl phosphatidyl choline (ETC-216). Pharmacokinetic analysis of infused ETC-216 suggest a slow distribution of AIM into peripheral tissue and an extremely long terminal half-life in plasma. Following ETC-216 administration to normal human volunteers, an initial dose-dependent HDL-C elevation was observed. Thereafter, subjects transiently acquired a lipoprotein profile similar to that of AIM carriers, including reduced HDL-C and mild hypertriglyceridemia. The time-dependent changes in plasma lipids/lipoproteins may support an increased tissue cholesterol removing capacity of ETC-216. These findings provide mechanistic insight into the rapid removal of atheromatous plaques observed in humans, possibly linked to enhanced cholesterol removal capacity of ETC-216.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Bisgaier CL,Ackermann R,Rea T,Rodrigueza WV,Hartman Ddoi
10.1016/j.phrs.2016.05.001subject
Has Abstractpub_date
2016-09-01 00:00:00pages
86-99eissn
1043-6618issn
1096-1186pii
S1043-6618(15)30189-4journal_volume
111pub_type
杂志文章,随机对照试验abstract::The objective of this study was to investigate the effects of 3-aminobenzamide (3-AB) on tissue damage in lung after hind limb ischemia-reperfusion (I/R), by assessing blood biochemical assay and histopathological analysis. Thirty-five adult Wistar rats were divided into five groups. After application of anaesthesia b...
journal_title:Pharmacological research
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pub_type: 杂志文章,评审
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journal_title:Pharmacological research
pub_type: 杂志文章
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pub_type: 临床试验,杂志文章
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journal_title:Pharmacological research
pub_type: 杂志文章
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更新日期:1996-04-01 00:00:00
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