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COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2009-10-20 , DOI: 10.1016/j.bmcl.2009.10.069
Ericsson David Coy , Luis Enrique Cuca , Michael Sefkow

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.



中文翻译:

新月桂科植物的COX,LOX和血小板聚集抑制特性

26个新木脂体的抗炎电位(二环型14和苯并呋喃型的12),从三个樟科物种(隔绝Pleurothyrium cinereum,Ocotea艽Nectandra amazonum),在体外通过抑制COX-1的评价,COX-2、5-LOX和激动剂诱导的兔血小板聚集。发现苯并呋喃新木脂素是选择性的COX-2抑制剂,而双环辛烷新木脂素选择性地抑制PAF作用以及COX-1和5-LOX。发现新木脂体9--7,8-脱氢-异水杨苷B 15和电影蛋白C 7分别是最有效的COX-2抑制剂和PAF拮抗剂。油桃素C 10 表现出双重5-LOX / COX-2抑制作用。

更新日期:2009-10-20
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