天然产物研究与开发 ›› 2020, Vol. 32 ›› Issue (12): 2094-2100.doi: 10.16333/j.1001-6880.2020.12.014

• 开发研究 • 上一篇    下一篇

鸦胆子中黄酮及其抗炎、抗补体活性的研究

何潇1,郭文静1,吴佳辉1,熊紫微1,谭婷1,冯育林1,2,杨世林2,温泉1*   

  1. 1江西中医药大学;2创新药物与高效节能降耗制药设备国家重点实验室,南昌 330006

  • 出版日期:2020-12-28 发布日期:2020-12-24
  • 基金资助:
    国家自然科学基金(81860684);国家重点研发计划(2019YFC1712302);江西省教育厅项目(GJJ190689);江西省中药学一流学科建设(JXSYLXKZHYAO016)

Anticomplement and anti-inflammatory flavones from the seeds of Brucea javanica

HE Xiao1,GUO Wen-jing1,WU Jia-hui1, XIONG Zi-wei1,TAN Ting1,FENG Yu-lin1,2,YANG Shi-lin2,WEN Quan1*   

  1. 1Jiangxi University of Traditional Chinese Medicine;2State Key Laboratory of Innovative Drug and Efficient Energy-Saving Pharmaceutical Equipment,Nanchang 330006,China

  • Online:2020-12-28 Published:2020-12-24

摘要:

研究鸦胆子中的黄酮类成分及其抗炎、抗补体的活性。采用正反相硅胶柱色谱、Sephadex LH-20凝胶柱色谱、制备液相及重结晶等方法从鸦胆子中分离纯化出一系列黄酮,利用NMR和质谱解析黄酮类成分的结构。采用Griess法及CCK-8法方法测定黄酮单体的抗炎及细胞毒活性,采用体外溶血方法测定黄酮类成分补体经典途径CH50的活性。从鸦胆子果实乙醇提取物的乙酸乙酯萃取部位分离得到12个骨架类型一致的黄酮类化合物,分别鉴定为:木犀草素(1)、芹菜素(2)、木犀草素7-O-β-D-葡萄糖苷(3)、7-甲氧基木犀草素(4)、槲皮素-3-O-α-L-吡喃鼠李糖苷(5)、木犀草素-3′-O-β-D-葡萄糖苷(6)、山柰酚-3-O-α-L-鼠李糖苷(7)、芹菜素-7-O-β-D-吡喃葡萄糖苷(8)、3′-甲氧基木犀草素(9)、野漆树苷(10)、芦丁(11)、异牡荆素(12),其中化合物1、2、4、6、7、8、11、12首次从鸦胆子中分离得到。活性测试表明,化合物1、2、3、4、5、9、11表现出显著抑制NO生成,除化合物4、9外,其余10个化合物均具有一定程度的抗补体活性,且构效关系明显。

关键词: 鸦胆子, 黄酮, 抗炎活性, 抗补体活性

Abstract:

Flavonoids from the seeds of Brucea javanica and their anti-inflammatory and anticomplement activities were studied.The compounds were isolated and identified by chromatographic and spectroscopic methods.The anti-inflammatory and cytotoxic activities of the compounds were determined by Griess method and CCK-8 method.Determination of CH50 activity of classical complement pathway of flavonoids by hemolysis method.Compounds (1-12) obtained from the ethyl acetate fraction of the ethanol extract were identified as luteolin (1),apigenin (2),luteolin-7-O-β-D-glucoside (3),7-methoxy-luteolin (4),quercetin-3-O-α-L-rhamnoside (5),luteolin-3′-O-β-D-glucoside (6),kaempferol-3-O-α-L-rhamoside (7),apigenin-7-O-β-D-glucoside (8),3′-methoxy-luteolin (9),apigenin-7-O-neohesperidoside (10),rutin (11) and isovitexin (12).Compounds 1,2,4,6,7,8,11 and 12 were obtained from this species for the first time.The results of screening demonstrated that compounds 1,2,3,4,5,9 and 11 showed moderate NO inhibitory effects,while all the compounds,except for compounds 4 and 9,possessed anticomplement activity and exhibited well structure-activity relationship.

Key words: Brucea javanica , (L.) Merr, flavonoid, anti-inflammatory activity, anticomplement activity

中图分类号:  R932