Xu Guang-Hua, Ryoo In-Ja, Kim Young-Hee, Choo Soo-Jin, Yoo Ick-Dong
Functional Metabolite Research Center, Korea Research Institute of Bioscience and Biotechnology, Daejeon 305-806, Republic of Korea.
Arch Pharm Res. 2009 Feb;32(2):275-82. doi: 10.1007/s12272-009-1233-y. Epub 2009 Mar 13.
Bioassay-guided fractionation of the MeOH extract of Thuja orientalis fruits using a DPPH (2,2-diphenyl-1-picrylhydrazyl) assay led to the isolation of 9 flavonoids: cupressuflavone (1), amentoflavone (2), robustaflavone (3), afzelin (4), (+)-catechin (5), quercitrin (6), hypolaetin 7-O-beta-xylopyranoside (7), isoquercitrin (8) and myricitrin (9). Their chemical structures were determined by spectroscopic analyses. The free radical scavenging and human neutrophil elastase (HNE) inhibitory activities were evaluated for the isolated compounds. By DPPH scavenging assay, compounds 5, 6, 7, 8 and 9 showed anti-oxidant activities with IC(50) values of 28.66, 31.19, 18.30, 26.63 and 15.10 microM, respectively. By ABTS [2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt] scavenging assay, these compounds also exhibited potent anti-oxidant activities with IC(50) values of 6.77, 13.96, 6.97, 22.79 and 9.96 microM, respectively. Of note, compounds 1, 2 and 3 showed significant HNE inhibitory activities with IC(50) values of 8.09, 1.27 and 1.33 microM, respectively.
采用DPPH（2,2-二苯基-1-苦基肼）法对侧柏果实甲醇提取物进行生物活性导向分离，得到9种黄酮类化合物：扁柏黄酮（1）、穗花杉双黄酮（2）、粗榧黄酮（3）、杨梅苷（4）、（+）-儿茶素（5）、槲皮苷（6）、次亚麻素7-O-β-木糖苷（7）、异槲皮苷（8）和杨梅素（9）。通过光谱分析确定了它们的化学结构。对分离得到的化合物进行了自由基清除和人中性粒细胞弹性蛋白酶（HNE）抑制活性评价。通过DPPH清除试验，化合物5、6、7、8和9表现出抗氧化活性，IC50值分别为28.66、31.19、18.30、26.63和15.10μM。通过ABTS[2,2'-偶氮二（3-乙基苯并噻唑啉-6-磺酸）二铵盐]清除试验，这些化合物也表现出较强的抗氧化活性，IC50值分别为6.77、13.96、6.97、22.79和9.96μM。值得注意的是，化合物1、2和3表现出显著的HNE抑制活性，IC50值分别为8.09、1.27和1.33μM。
