Yoon Mi-Ae, Jeong Tae-Sook, Park Doo-Sang, Xu Ming-Zhe, Oh Hyun-Woo, Song Kyoung-Bin, Lee Woo Song, Park Ho-Yong
Insect Resources Laboratory, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Korea.
Biol Pharm Bull. 2006 Apr;29(4):735-9. doi: 10.1248/bpb.29.735.
The oxidized low-density lipoprotein (ox-LDL) plays a critical role at the early stages of atherosclerosis. Thus, the prevention of LDL-oxidation by antioxidants may arrest the progression of atherosclerosis. Two quinoline alkaloids, 3,8-dihydroxyquinoline (1) and 2,8-dihydroxy-3,4-dimethoxyquinoline (3), and 2,4-di-tert-butylphenol (2) were isolated from the dried body of Scolopendra subspinipes. Compounds 1-3 exhibited antioxidant activities on copper-mediated (1: IC50=2.6 microM, 2: IC50=8.2 microM, 3: IC50=63.0 microM), AAPH-mediated oxidation (1: IC50=3.9 microM, 2: IC50=9.9 microM, 3: IC50=71.8 microM), and SIN-1-mediated oxidation (1: 70%, 2: 52%, 3: 29% at 5.0 microM) in the TBARS assay. The antioxidant activities of compounds 1-3 were tested with respect to other parameters, such as the lag time of conjugated diene fromation, relative electrophoretic mobility (REM) of ox-LDL, and apoB-100 fragmentation on copper-mediated LDL-oxidation. In addition, compounds 1-3 showed 1,1-diphenyl-2-picrylhydrasyl (DPPH) radical scavenging activity and compound 1 also exhibited metal chelating activity.
氧化型低密度脂蛋白（ox-LDL）在动脉粥样硬化早期起着关键作用。因此，抗氧化剂预防低密度脂蛋白氧化可能会阻止动脉粥样硬化的进展。从少棘蜈蚣干燥体中分离出两种喹啉生物碱，3,8 - 二羟基喹啉（1）和2,8 - 二羟基 - 3,4 - 二甲氧基喹啉（3），以及2,4 - 二叔丁基苯酚（2）。在硫代巴比妥酸反应物（TBARS）测定中，化合物1 - 3对铜介导的氧化（1：IC50 = 2.6 microM，2：IC50 = 8.2 microM，3：IC50 = 63.0 microM）、偶氮二异丁腈（AAPH）介导的氧化（1：IC50 = 3.9 microM，2：IC50 = 9.9 microM，3：IC50 = 71.8 microM）和过氧亚硝基阴离子（SIN - 1）介导的氧化（在5.0 microM时，1：70%，2：52%，3：29%）表现出抗氧化活性。针对其他参数测试了化合物1 - 3的抗氧化活性，如共轭二烯形成的延迟时间、氧化型低密度脂蛋白的相对电泳迁移率（REM）以及铜介导的低密度脂蛋白氧化时载脂蛋白B - 100的片段化。此外，化合物1 - 3表现出1,1 - 二苯基 - 2 - 苦基肼基（DPPH）自由基清除活性，化合物1还表现出金属螯合活性。
