黄芫花化学成分及其抗乙肝病毒作用  

Chemical constituents from flowers of Wikstroemia chamaedaphne and their anti-hepatitis B virus activity

作　　者：张志强 李石飞[1] 张立伟[1] 钞建宾[2] 

机构地区：[1]化学生物学与分子工程教育部重点实验室,山西大学分子科学研究所,山西太原030006 [2]山西大学大型仪器中心,山西太原030006

出　　处：《中草药》2017年第7期1292-1297,共6页Chinese Traditional and Herbal Drugs

基　　金：山西省重点研发计划项目(201603D321024);山西省面上青年基金项目(201601D021157)

摘　　要：目的研究山西黄芫花(河朔荛花Wikstroemia chamaedaphne的花蕾)中具有抗乙肝病毒(HBV)作用的二萜成分。方法采用色谱方法分离纯化,经波谱数据和单晶衍射技术鉴定化合物结构,采用MTT法进行体外细胞毒和抗HBV活性测试。结果从黄芫花中分离鉴定9个化合物,包括6个瑞香烷型二萜:河朔荛花素(1)、pimelotide A(2)、pimelotide C(3)、wikstroelide E(4)、pimelea factor S6(5)、pimelea factor S7(6);1个惕各烷型二萜:6α,7α-epoxy-5β-hydroxy-12-deoxyphorbol-13-decanoate(7)和2个黄酮苷化合物:木犀草素-4′-O-β-D-葡萄糖苷(8)和异槲皮苷(9)。化合物1~4和7均显示较强的细胞毒活性,其半数毒性浓度(TC50)值为3.24~7.30μg/m L,且化合物3显示出显著的抑制HBsAg产生的作用,其IC50为0.016μg/m L,治疗指数(therapeutic index,TI)值为355.63。结论化合物7和8为首次从该属植物中分离得到,首次报道了化合物2的晶体结构,首次发现了化合物3具有显著的抑制HBsAg产生的作用。Objective To study the anti-hepatitis B virus diterpenoids from flowers of Wikstroemia chamaedaphne. Methods The chemical constituents of the plant were isolated and purified by column chromatography and their structures were elucidated on the basis of physicochemical properties, X-ray, and spectral data. The antivirus assay was tested by MTT and ELISA methods. Results Six daphnane-type diterpenoids and one tigliane-type diterpenoid were obtained and determined as simplexin （1）, pimelotide A （2）, pimelotide C （3）, wikstroelide E （4）, pimelea factor $6 （5）, pimelea factor S7 （6）, and 6α,Tct-epoxy-515-hydroxy-12- deoxyphorbol-13-decanoate （7）, along with two flavonoid glycosides luteolin-4＇-O-β-D-glucoside （8） and isoquercitrin （9）. Compounds 1-4 and 7 showed certain cytotoxicity on HepG2.2.15 and compound 3 exhibited strong anti-hepatitis B virus activities with IC50 value of 0.016μg/mL against HBV surface antigen （HBsAg）, with TI （Therapeutic Index） value of 355.63. Conclusion Compounds 7 and 8 are isolated from the genus for the first time. And it is the first time to report the X-ray structure of compound 2 and the anti-hepatitis B virus activity of compound 3 （pimelotide C）.

关 键 词：黄芫花 瑞香烷型二萜 惕各烷型二萜 河朔荛花素 pimelotide C 抗乙肝病毒 

分 类 号：R284.1[医药卫生—中药学]