Co-construction Collaborative Innovation Center for Chinese Medicine Resources Industrialization by Shaanxi & Education Ministry, State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), Shaanxi University of Chinese Medicine, 712083, Xianyang, PR China.
Co-construction Collaborative Innovation Center for Chinese Medicine Resources Industrialization by Shaanxi & Education Ministry, State Key Laboratory of Research & Development of Characteristic Qin Medicine Resources (Cultivation), Shaanxi University of Chinese Medicine, 712083, Xianyang, PR China; China Academy of Chinese Medical Sciences, Beijing, 100700, PR China.
Phytochemistry. 2024 Oct;226:114208. doi: 10.1016/j.phytochem.2024.114208. Epub 2024 Jul 5.
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 IC values from 0.75 to 8.17 μΜ. These findings provide useful information for the search for natural selective COX-2 inhibitors.
刺五加皮（五加科植物无梗五加的干燥根皮）在中国已被用于治疗风湿疾病超过 2000 年。从刺五加皮中分离得到了四个以前未被描述的木脂素（1-4）和 12 个已知的木脂素（5-16）。在这项研究中，报告了化合物 1-16 对中性粒细胞弹性蛋白酶（NE）、环加氧酶-1（COX-1）和环加氧酶-2（COX-2）的抑制活性。结果表明，化合物 1-16 对 NE 和 COX-1 表现出较弱的抑制活性。然而，化合物 2、6-8 和 13-16 对 COX-2 表现出更好的抑制作用，IC 值为 0.75 至 8.17 μΜ。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。
