青花椒根皮中1个新的香豆素类化合物  

A new coumarin isolated from root barks of Zanthoxylum schinifolium

作　　者：张东博 王征 梁艳妮 于金高 张珍 李铂 刘世军 蔡兴航 宋忠兴 任丽 侯青 谢培 唐志书 ZHANG Dong-bo;WANG Zheng;LIANG Yan-ni;YU Jin-gao;ZHANG Zhen;LI Bo;LIU Shi-jun. CAI Xing-hang;SONG Zhong-xing;REN Li;HOU Qing;XIE Pei;TANG Zhi-shu(Shaanxi Province Key Laboratory of New Drugs and Chinese Medicine Foundation Research/Shaanxi Rheumatism and Tumor Center of TCM Engineering Technology Research,Shaanxi Collaborative In novation Center of Chinese Medici nal Resource Industrialization,Shaanxi University of Chinese Medicine,Xianyang 712083,China)

机构地区：[1]陕西中医药大学/陕西省中药资源产业化协同创新中心/陕西省中药基础与新药研究重点实验室/陕西省风湿与肿瘤类中药制剂工程技术研究中心

出　　处：《中草药》2019年第12期2798-2801,共4页Chinese Traditional and Herbal Drugs

基　　金：陕西省重点研发计划(2017SF-365);陕西省重点研发计划(2017SF-327);陕西省教育厅自然科学专项项目(16JK1196)

摘　　要：目的对青花椒Zanthoxylum schinifolium根皮中抗炎活性成分进行跟踪分离研究。方法采用硅胶、Sephadex LH-20、MCI以及半制备HPLC等色谱方法进行分离纯化,根据理化性质和现代谱学技术鉴定化合物的结构,以脂多糖(LPS)诱导的RAW264.7细胞炎症模型进行抗炎活性评价。结果从青花椒根皮的醋酸乙酯部位中共分离得到4个香豆素类化合物,分别鉴定为青花椒素A(1)、7-甲氧基香豆素(2)、异东莨菪内酯(3)和秦皮乙素(4)。在LPS诱导RAW264.7细胞产生一氧化氮(NO)的模型中,化合物1~4均对NO的产生具有抑制作用,半数抑制浓度(IC50)值分别为(0.21±0.03)、(0.92±0.16)、(0.15±0.02)和(0.26±0.04)μmol/L。结论化合物1为新化合物,是1个罕见的香豆素类化合物,命名为青花椒素A。化合物3为首次从该属植物中分离得到,所有化合物均具有较强的抗NO生成活性。Objective To study the anti-inflammatory components from the root barks of Zanthoxylum schinifolium. Methods The compounds were isolated and purified by silica gel, MCI, Sephadex LH-20 column chromatographies, and semi-preparative HPLC, and their structures were elucidated by physical and spectroscopic analysis. The anti-inf1ammatory activity was evaluated by the levels of NO in LPS-induced RAW264.7 tested by Griess reagent. Results Four coumarins, namely zantholin A (1), 7-methoxycoumarin (2), isoscopoletin (3), and esculetin (4), were isolated from the root barks of Z. schinifolium. Compounds 1-4 exhibited anti-inflammatory activities on inhibition of lipopolysaccharide (LPS)-induced NO production in RAW 264.7 macrophages with IC50 values of (0.21 ±0.03),(0.92 ±0.16),(0.15 ±0.02), and (0.26 ±0.04)μmol/L, respectively. Conclusion Compound 1 is a new compound, a rare terpenylated coumarin named zantholin A, and compounds 3 is obtained from this plant for the first time. All compounds exhibited anti-inflammatory activities.

关 键 词：芸香科 青花椒:青花椒素A:香豆素 抗炎活性 7-甲氧基香豆素 异东莨菪内酯 秦皮乙素 

分 类 号：R284.1[医药卫生—中药学]