Ryu Jae-Ha, Ahn Hanna, Kim Ji Yeon, Kim Young-Kyoon
College of Pharmacy, Sookmyung Women's University, Seoul, Korea.
Phytother Res. 2003 May;17(5):485-9. doi: 10.1002/ptr.1180.
Nitric oxide (NO) produced in large amounts by inducible nitric oxide synthase (iNOS) is known to be responsible for the vasodilation and hypotension observed in septic shock and inflammation. Inhibitors of iNOS, thus, may be useful candidates for the treatment of inflammatory diseases accompanied by overproduction of NO. We prepared alcoholic extracts of woody plants and screened the inhibitory activity of NO production in lipopolysaccharide (LPS)-activated macrophages after the treatment of these extracts. Among 83 kinds of plant extracts, 23 kinds of extracts showed potent inhibitory activity of NO production above 60% at the concentration of 80 micro g/ml. Some of potent extracts showed dose dependent inhibition of NO production of LPS-activated macrophages at the concentration of 80, 40, 20 micro g/ml. Especially, Artemisia iwayomogi, Machilus thunbergii, Populus davidiana and Populus maximowiczii showed the most potent inhibition (above 70%) at the concentration of 40 micro g/ml. Inhibitory activity of NO production was concentrated to nonpolar solvent fractions (ethyl ether and/or ethyl acetate soluble fractions) of Artemisia iwayomogi, Machilus thunbergii and Morus bombycis. These plants are promising candidates for the study of the activity-guided purification of active compounds and would be useful for the treatment of inflammatory diseases and endotoxemia accompanying overproduction of NO.
诱导型一氧化氮合酶(iNOS)大量产生的一氧化氮(NO)已知是导致脓毒症休克和炎症中出现血管舒张和低血压的原因。因此,iNOS抑制剂可能是治疗伴有NO过量产生的炎症性疾病的有用候选药物。我们制备了木本植物的醇提取物,并在处理这些提取物后,筛选了其对脂多糖(LPS)激活的巨噬细胞中NO产生的抑制活性。在83种植物提取物中,有23种提取物在80微克/毫升的浓度下显示出高于60%的有效NO产生抑制活性。一些有效提取物在80、40、20微克/毫升的浓度下对LPS激活的巨噬细胞的NO产生表现出剂量依赖性抑制。特别是,艾蒿、黑壳楠、山杨和大青杨在40微克/毫升的浓度下显示出最强的抑制作用(高于70%)。艾蒿、黑壳楠和桑的NO产生抑制活性集中在非极性溶剂部分(乙醚和/或乙酸乙酯可溶部分)。这些植物是活性化合物活性导向纯化研究的有前途的候选植物,对治疗伴有NO过量产生的炎症性疾病和内毒素血症将是有用的。