Hwang B Y, Lee J H, Koo T H, Kim H S, Hong Y S, Ro J S, Lee K S, Lee J J
Anticancer Agents Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Taejon.
Planta Med. 2001 Jul;67(5):406-10. doi: 10.1055/s-2001-15808.
A methanolic extract of the whole plant of Isodon japonicus (Labiatae) showed potent inhibition on the LPS-induced nitric oxide (NO) and prostaglandin E2 (PGE2) production in RAW264.7 cells. Four known kaurane diterpenes were isolated by activity-guided fractionation and their structures were identified as kamebanin (1), kamebacetal A (2), kamebakaurin (3), excisanin A (4). All compounds also inhibited the LPS-induced NF-kappaB activation as assessed by NF-kappaB reporter assay and electrophoretic mobility shift assay (EMSA). Compounds 2-4 showed comparable inhibitory effects on the LPS-induced production of NO and PGE2, and activation of NF-kappaB without affecting cell viability. These results suggest that kaurane diterpenes could exert their inhibitory effects on the production of NO and PGE2 through the suppression of NF-kappaB activation, and be partially responsible for the anti-inflammatory activities of the genus Isodon.
线纹香茶菜（唇形科）全株的甲醇提取物对RAW264.7细胞中脂多糖（LPS）诱导的一氧化氮（NO）和前列腺素E2（PGE2）生成显示出强效抑制作用。通过活性导向分离法分离出4种已知的贝壳杉烷二萜，其结构鉴定为龟甲冬青素（1）、龟甲冬青缩醛A（2）、龟甲冬青苷（3）、延命草素A（4）。通过NF-κB报告基因检测和电泳迁移率变动分析（EMSA）评估，所有化合物还抑制LPS诱导的NF-κB激活。化合物2-4对LPS诱导的NO和PGE2生成以及NF-κB激活显示出相当的抑制作用，且不影响细胞活力。这些结果表明，贝壳杉烷二萜可通过抑制NF-κB激活对NO和PGE2的生成发挥抑制作用，并部分解释了香茶菜属植物的抗炎活性。
