Abstract：
Acanthopanacis cortex (the dried root bark of Acanthopanax gracilistylus W. W. Smith) has been used for the treatment of rheumatic diseases in China for over 2000 years. Four previously undescribed lignans (1-4) and 12 known lignans (5-16) were isolated from Acanthopanacis cortex. In this study, the inhibitory activities of compounds 1-16 against neutrophil elastase (NE), cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) are reported. The results show that compounds 1-16 exhibit weak inhibitory activities against NE and COX-1. However, compounds 2, 6-8 and 13-16 demonstrate better COX-2 inhibitory effects with IC50 values from 0.75 to 8.17 μΜ. These findings provide useful information for the search for natural selective COX-2 inhibitors.
摘要：
刺五加皮层（刺五加的干根皮）已在中国用于治疗风湿性疾病已有2000多年的历史。从刺五加皮层中分离出四种先前未描述的木酚素（1-4）和12种已知的木酚素（5-16）。在这项研究中,化合物1-16对中性粒细胞弹性蛋白酶(NE)的抑制活性,报道了环氧合酶-1(COX-1)和环氧合酶-2(COX-2)。结果表明,化合物1-16对NE和COX-1表现出弱的抑制活性。然而,化合物2、6~8和13~16显示出更好的COX-2抑制作用，IC50值为0.75至8.17μM。这些发现为寻找天然选择性COX-2抑制剂提供了有用的信息。
