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为研究华中枸骨中多个黄烷类成分(1~6)体外抗炎与自由基清除活性,并初步分析其构效关系。采用脂多糖诱导小鼠RAW264.7巨噬细胞炎症模型,MTT法测定细胞毒性作用,Griess法测定NO生成量,ELISA法检测细胞上清液中TNF-α,IL-1β,IL-6,PGE_2的含量;体外测定清除DPPH自由基,超氧阴离子自由基和羟自由基活性。结果表明黄烷1,3,4,6体外显示很强的抗炎活性,能显著抑制NO,TNF-α,IL-1β和IL-6的分泌,化合物1的抑制作用最强,黄烷2和5显示相对较弱的抑制活性,体外自由基清除活性顺序与抗炎活性相似。因此,黄烷1,3,4,6是华中枸骨抗炎和自由基清除活性的活性成分,构效关系初步分析表明4′-羟基为黄烷类化合物显示抗炎和自由基清除活性的主要结构部位。
In order to study the anti-inflammatory and free radical scavenging activities of several flavanoids (1 ~ 6) in the root of Chrysopa sinica, the structure-activity relationship was preliminary analyzed. The model of RAW264.7 macrophage inflammation was induced by lipopolysaccharide. The cytotoxicity was determined by MTT assay. The production of NO was measured by Griess method. The levels of TNF-α, IL-1β, IL-6 and PGE_2 The activity of scavenging DPPH radical, superoxide anion radical and hydroxyl radical were measured in vitro. The results showed that 1,3,4,6 showed strong anti-inflammatory activity in vitro and could significantly inhibit the secretion of NO, TNF-α, IL-1β and IL-6. The inhibitory effect of compound 1 was the strongest. And 5 showed relatively weaker inhibitory activity, and the order of free radical scavenging activity in vitro was similar to that of anti-inflammatory activity. Therefore, flavanone 1,3,4,6 is the active ingredient of the anti-inflammatory and free radical scavenging activities of the stems and leaves of Chrysanthemum morifolium, and preliminary analysis of the structure-activity relationship shows that the 4’-hydroxyl group is an anti-inflammatory and radical scavenging activity of the flavanoids Main structural parts.