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两种樟科植物中天然化合物的体外抗炎作用

In vitro anti-inflammatory effects of naturally-occurring compounds from two Lauraceae plants.

作者信息

Coy-Barrera Ericsson D, Cuca-Suarez Luis E

机构信息

Laboratorio de Investigación en Productos Naturales Vegetales, Departamento de Química, Facultad de Ciencias, Universidad Nacional de Colombia, Bogotá DC, Colombia.

出版信息

An Acad Bras Cienc. 2011 Dec;83(4):1397-402. doi: 10.1590/s0001-37652011005000044. Epub 2011 Oct 21.

DOI:10.1590/s0001-37652011005000044
PMID:22011769
Abstract

The in vitro anti-inflammatory effects of seven known lignans and one dihydrochalcone isolated from the leaves of two Lauraceae species (Pleurothyrium cinereum and Ocotea macrophylla), were evaluated through the inhibition of COX-1, COX-2, 5-LOX and the aggregation of rabbit platelets induced by PAF, AA and ADP. (+)-de-4"-O-methylmagnolin 4 was found to be a potent COX-2/5-LOX dual inhibitor and PAF-antagonist (COX-2 IC(50) 2.27 µM; 5-LOX IC(50) 5.05 µM; PAF IC(50) 2.51 µM). However, all compounds exhibited an activity at different levels, indicating good anti-inflammatory properties to be considered in further structural optimization studies.

摘要

从两种樟科植物(灰叶赛楠和大叶楠)的叶子中分离出的七种已知木脂素和一种二氢查耳酮的体外抗炎作用,通过抑制COX-1、COX-2、5-LOX以及PAF、AA和ADP诱导的兔血小板聚集来进行评估。发现(+)-去-4”-O-甲基厚朴酚4是一种有效的COX-2/5-LOX双重抑制剂和PAF拮抗剂(COX-2 IC(50) 2.27 µM;5-LOX IC(50) 5.05 µM;PAF IC(50) 2.51 µM)。然而,所有化合物都表现出不同程度的活性,表明在进一步的结构优化研究中应考虑其良好的抗炎特性。

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