Cimanga K, De Bruyne T, Lasure A, Van Poel B, Pieters L, Vanden Berghe D, Vlietinck A, Kambu K, Tona L
Department of Pharmaceutical Sciences, University of Antwerp, Belgium.
J Nat Prod. 1995 Mar;58(3):372-8. doi: 10.1021/np50117a005.
In a screening program for complement classical pathway modulation, an 80% MeOH extract of the leaves of Morinda morindoides showed potent dose-dependent anticomplementary activity. Bioassay-guided chromatographic separation of the active constituents led to the isolation of ten flavonoids of which two were aglycones. The compounds were tested in vitro for their putative complement-inhibiting properties on the classical (CP) and the alternative (AP) pathways of the complement system. The results indicated that quercetin [1], quercetin 3-O-rhamnoside (quercitrin) [5], and quercetin 3-O-rutinoside (rutin) [7] showed similar anticomplementary activities (inhibition) on the CP of complement. A mixture of two kaempferol triglycosides isolated and denoted as M(015), also had a good inhibitory effect. The effects of these compounds were dose-dependent for this pathway. On the AP of complement, quercetin [1] and M(015) had, respectively, more pronounced inhibitory and activatory effects than the other tested flavonoids, but their effects were not dose-dependent for this pathway. The other isolated flavonoids showed weak effects or were inactive for both pathways.
在一项补体经典途径调节筛选计划中，巴戟天叶片的80%甲醇提取物显示出强大的剂量依赖性抗补体活性。通过生物测定指导的色谱分离法对活性成分进行分离，得到了10种黄酮类化合物，其中两种为苷元。对这些化合物进行体外测试，以检测它们对补体系统经典途径（CP）和替代途径（AP）的假定补体抑制特性。结果表明，槲皮素[1]、槲皮素3 - O - 鼠李糖苷（芦丁）[5]和槲皮素3 - O - 芸香糖苷（芸香苷）[7]对补体经典途径表现出相似的抗补体活性（抑制作用）。分离得到的两种山奈酚三糖苷混合物（记为M(015)）也具有良好的抑制作用。这些化合物对该途径的作用呈剂量依赖性。在补体替代途径上，槲皮素[1]和M(015)分别比其他测试的黄酮类化合物具有更明显的抑制和激活作用，但它们对该途径的作用不呈剂量依赖性。其他分离得到的黄酮类化合物对两种途径均显示出微弱作用或无活性。
