Ryu Jae-Ha, Son Haeng Ja, Lee Sook Hyun, Sohn Dong Hwan
College of Pharmacy, Sookmyung Women's University, 140-742, Seoul, Republic of Korea.
Bioorg Med Chem Lett. 2002 Feb 25;12(4):649-51. doi: 10.1016/s0960-894x(01)00812-5.
Two neolignans were isolated from leaves of Perilla frutescens (Labiatae) as inhibitors of nitric oxide syntheses (IC50 5.9 microM and 53.5 microM, respectively) and tumor necrosis factor-alpha in lipopolysaccharide-activated RAW 264.7 cells. Their structures were identified as 1beta,2alpha,3beta,4alpha-1,2-dimethyl-3,4-bis-(2,4,5-trimethoxyphenyl)-cyclobutane (magnosalin), and 1alpha,2beta,3beta,4alpha-1,2-dimethyl-3,4-bis-(2,4,5-trimethoxyphenyl)-cyclobutane (andamanicin), and their activities were confirmed as resulted from the suppressed expression of inducible nitric oxide synthase enzyme and from the secretion of tumor necrosis factor-alpha from activated macrophages.
从紫苏(唇形科)叶中分离出两种新木脂素,它们是一氧化氮合成的抑制剂(IC50分别为5.9微摩尔和53.5微摩尔),并能抑制脂多糖激活的RAW 264.7细胞中肿瘤坏死因子-α的产生。它们的结构被鉴定为1β,2α,3β,4α-1,2-二甲基-3,4-双-(2,4,5-三甲氧基苯基)-环丁烷(厚朴酚)和1α,2β,3β,4α-1,2-二甲基-3,4-双-(2,4,5-三甲氧基苯基)-环丁烷(和厚朴酚),其活性经证实是由于诱导型一氧化氮合酶的表达受到抑制以及活化巨噬细胞分泌肿瘤坏死因子-α所致。