紫茉莉根化学成分及其生物活性研究

Studies on the chemical constituents and their bioactivity of the root of Mirabilis jalapa L

    摘要
  • 摘要: 研究紫茉莉根的化学成分及其生物活性. 采用凝胶柱色谱、正相硅胶柱色谱、半制备高效液相色谱等系统分离方法对紫茉莉根乙酸乙酯萃取部位进行分离纯化，通过现代波谱解析技术、理化性质及已知文献鉴定化合物结构，随后采用CCK-8方法检测化合物对5株肿瘤细胞系的抑制活性；并利用LPS诱导RAW 264.7巨噬细胞构建炎症模型，评价化合物抗NO生成活性. 从乙酸乙酯部位中分离并鉴定14个化合物，分别为硫磺菊素 (1)、davidigenin (2)、3,4,2′,4′-四羟基二氢查尔酮 (3)、confusoside (4)、紫铆亭 (5)、3,4-dihydro-7,8-dihydroxy-l(2H)-isoquinolinone (6)、iseluxine (7)、丁香酸甲酯 (8)、香草酸甲酯 (9)、1H-indole-3-carbaldehyde (10)、阿魏酸甲酯 (11)、香草酸 (12)、uridine (13)、桦木酸 (14)，以上化合物均首次从该种植物中分离到，其中化合物6为新的天然产物，本文首次报道其波谱数据. 活性筛选表明，化合物14具有较好的抗肿瘤细胞毒活性，对HGC27、PANC-1、Hela-60、SY5Y、AGS细胞显示出较好的毒性，其IC50值分别为（37.4±1.5），（10.2±1.6），（44.3±1.6），（8.5±0.5），（50.3±1.5 ）μmol/L；化合物1抑制LPS诱导RAW 264.7细胞中NO生成活性较强，IC50值达（20.12±1.01）μmol/L.

     

    Abstract: To study the chemical constituents and bioactivity of Mirabilis jalapa L. Fourteen compounds were isolated from the EtOAc extract of the root of this plant by silica gel, Sephadex LH-20, and CCK-8 method were used to test the antitumor activity in five cell lines, and the anti-inflammatory activities of compounds were evaluated by LPS induced RAW 264.7 inflammatory cell model. They were identified as sulfuretin (1), davidigenin (2), 3,4,2′,4′-tetrahydroxydihydro-chalcone (3), confusoside (4), butin (5), 3,4-dihydro-7,8-dihydroxy-l(2H)-isoquinolinone (6), iseluxine (7), methyl syringate (8), methyl vanillate (9), 1H-indole-3-carbaldehyde (10), ferulic acid methyl ester (11), vanillic acid (12), uridine (13), betulinic acid (14) on the basis of physicochemical properties and spectral data. Compound 14 have significant activity against to the cell lines HGC27, PANC-1, Hela-60, SY5Y, AGS, with IC50 values of (37.4±1.5), (10.2±1.6), (44.3±1.6), (8.5±0.5), and (50.3±1.5) μmol/L, respectively. Compound 1 showed significant activity, the IC50 value of compound 1 was (20.12±1.01)μmol/L．

     

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