COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans

COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans
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DOI:
10.1016/j.bmcl.2009.10.069
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发表时间:
2009-12-15
影响因子:
2.7
通讯作者:
Sefkow, Michael
Sefkow, Michael
中科院分区:
医学4区
文献类型:
--
作者:
David Coy, Ericsson;Enrique Cuca, Luis;Sefkow, Michael

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通过体外抑制考克斯-1、考克斯-2、5-LOX和激动剂诱导的兔血小板聚集,评价了从三种樟科植物(Pleurostyrum cinereum、Ocotea macrophylla和Nectandra amazonum)中分离的26种新木脂素(14种双环辛烷型和12种苯并呋喃型)的抗炎潜力。发现苯并呋喃新木脂素是选择性考克斯-2抑制剂,而双环辛烷新木脂素选择性抑制PAF作用以及考克斯-1和5-LOX。新木脂素9-去甲-7,8-脱氢异淫羊藿苷B 15和cinerin C7分别是最强的考克斯-2抑制剂和PAF拮抗剂。Nectamazin C10表现出双重5-LOX/考克斯-2抑制作用。(C)2009爱思唯尔有限公司保留所有权利。
The anti-inflammatory potential of 26 neolignans (14 of the bicyclooctane-type and 12 of the benzofuran-type), isolated from three Lauraceae species (Pleurothyrium cinereum, Ocotea macrophylla and Nectandra amazonum), was evaluated in vitro through inhibition of COX-1, COX-2, 5-LOX and agonist-induced aggregation of rabbit platelets. Benzofuran neolignans were found to be selective COX-2 inhibitors, whereas bicyclooctane neolignans inhibit selectively the PAF-action as well as COX-1 and 5-LOX. The neolignan 9-nor-7,8-dehydro-isolicarin B 15 and cinerin C 7 were found to be the most potent COX-2 inhibitor and PAF-antagonist, respectively. Nectamazin C 10 exhibited dual 5-LOX/COX-2 inhibition. (C) 2009 Elsevier Ltd. All rights reserved.