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橘叶化学成分及其抗炎活性研究

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目的 研究橘Citrus reticulata Blanco叶化学成分及其抗炎活性.方法 橘叶85%乙醇提取物采用硅胶、D101 大孔树脂、MCI、ODS、Sephadex LH-20 进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构.采用Griess法测定化合物对脂多糖诱导RAW 264.7 细胞产生NO的抑制活性.建立角叉菜胶致小鼠足肿胀炎症模型,检测IL-1β、TNF-α水平.结果 从中分离得到 12 个化合物,分别鉴定为川陈皮素(1)、橘红素(2)、5-去甲川陈皮素(3)、5,4'-二羟基-6,7,8,3'-四甲氧基黄酮(4)、5-羟基-7,8,3',4'-四甲氧基黄酮(5)、3,5,6,7,8,3',4'-七甲氧基黄酮(6)、橙皮素(7)、5-羟基-6,7,3',4'-四甲氧基黄酮(8)、β-香树脂醇(9)、豆甾-5-烯-3β-醇(10)、对羟基苯甲醛(11)、香草醛(12).化合物 1~4、6~7、10、12 对脂多糖诱导RAW 264.7 细胞释放NO有较强抑制活性,IC50值分别为(25.21±2.10)、(37.77±0.50)、(38.19±1.58)、(21.89±1.73)、(43.81±1.18)、(47.98±2.55)、(41.23±1.11)、(43.80±1.43)μmol/mL.化合物 2~3 可降低IL-1β、TNF-α水平(P<0.05,P<0.01).结论 化合物6~7、9 为首次从该植物中分离得到.化合物1~4、8 有较强的体外抗炎活性,化合物2~3 有明显的体内抗炎活性.
Chemical constituents from the leaves of Citrus reticulata and their anti-inflammatory activities
AIM To study the chemical constituents from the leaves of Citrus reticulata Blanco and their anti-inflammatory activities.METHODS The 85%ethanol extract from the leaves of C.reticulata was isolated and purified by silica gel,D101 macroporous resin,MCI,ODS and Sephadex LH-20,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The Griess method was used to determine their inhibitory activities on lipopolysaccharide-induced NO production in macrophages RAW 264.7 cells.The mice foot swelling inflammation model induced by carrageenan was established,and the levels of IL-1β,TNF-α were detected.RESULTS Twelve compounds were isolated and identified as nobiletin(1),tangeretin(2),5-demethylinoblitin(3),5,4'-dihydroxy-6,7,8,3'-tetramethoxy flavone(4),5-hydroxy-7,8,3',4'-trimethoxyflavanone(5),3,5,6,7,8,3',4'-heptamethoxyflavanone(6),hesperetin(7),5-hydroxy-6,7,3',4'-tetramethoxyphenone(8),β-balsam alcohol(9),stigmaster-5-en-3β-alcohol(10),p-hydroxybenzaldehyde(11),vanillin(12).Compounds 1,4,6,7,10 and 12 had strong inhibitory activites on NO release in LPS-induced RAW 264.7 cells,and the IC50 values were(25.21±2.10),(37.77±0.50),(38.19±1.58),(21.89±1.73),(43.81±1.18),(47.98±2.55),(41.23±1.11),(43.80±1.43)μmol/mL,respectively.Compounds 2-3 reduced IL-1β and TNF-α levels(P<0.05,P<0.01).CONCLUSION Compounds 6-7,9 are isolated from this plant for the first time.Compounds 1-4,8 exhibit strong in vitro anti-inflammatory activities,and compounds 2-3 exhibit significant in vivo anti-inflammatory activities.

Citrus reticulata Blancoleaveschemical constituentsisolation and identificationanti-inflammatory activities

杨发科、杨兴、张志毕、尹蕊、张洪川、邓徐丽、董维茂、王一谋、何红平、董发武

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云南中医药大学中药学院,云南省南药可持续利用重点实验室,云南 昆明 650500

昆明医科大学第三附属医院,云南 昆明 650500

昆明医科大学生物医学工程研究院,云南 昆明 650500

化学成分 分离鉴定 抗炎活性

国家自然科学基金资助项目国家自然科学基金资助项目云南省高层次人才培养支持计划"青年拔尖人才"专项云南省基础研究计划面上项目云南省南药可持续利用研究重点实验室开放课题重点项目

3186009282260758YNWR-QNBJ-2020-255202101AT070254202105AG070012ZD2201

2024

中成药
国家食品药品监督管理局,信息中心中成药信息站,上海中药行业协会

中成药

CSTPCD北大核心
影响因子:1.217
ISSN:1001-1528
年,卷(期):2024.46(9)
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