Han Ah-Reum, Kim Hye Jeoung, Shin Minkyu, Hong Moochang, Kim Yang Seok, Bae Hyunsu
BK21 Oriental Medical Science Center, College of Oriental Medicine, Kyung Hee University, 1 Hoeki-dong, Dongdaemun-gu, Seoul 130-701, Korea.
Chem Biodivers. 2008 Feb;5(2):346-51. doi: 10.1002/cbdv.200890033.
Bioassay-guided fractionation of the root extract of Asarum sieboldii led to the isolation of the four active compounds (-)-sesamin (1), (2E,4E,8Z,10E)-N-(2-methylpropyl)dodeca-2,4,8,10-tetraenamide (2), kakuol (3), and '3,4,5-trimethoxytoluene' (=1,2,3-trimethoxy-5-methylbenzene; 4), in terms of inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production. Compounds 1-4 showed potent inhibition of NO production, with IC(50) values in the low nanomolar-to-micromolar range. Also isolated were the known compounds methylkakuol (5), '3,5-dimethoxytoluene', safrole, asaricin, methyleugenol, and (-)-asarinin, which were found to be inactive in the above assay. Among the ten known isolates, compounds 1, 2, and 5 were found for the first time in this plant.
通过生物活性测定指导对细辛根提取物进行分离，得到了四种活性化合物：（-）-芝麻素（1）、（2E,4E,8Z,10E）-N-（2-甲基丙基）十二碳-2,4,8,10-四烯酰胺（2）、卡枯醇（3）和“3,4,5-三甲氧基甲苯”（=1,2,3-三甲氧基-5-甲基苯；4），这些化合物能够抑制脂多糖（LPS）诱导的一氧化氮（NO）生成。化合物1-4对NO生成表现出强效抑制作用，其半数抑制浓度（IC50）值在低纳摩尔至微摩尔范围内。还分离出了已知化合物甲基卡枯醇（5）、“3,5-二甲氧基甲苯”、黄樟素、细辛醚、甲基丁香酚和（-）-细辛脂素，发现它们在上述测定中无活性。在这十种已知分离物中，化合物1、2和5首次在该植物中被发现。
