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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 (diterpene) components of Shanxi Huang Yuanhua (Wikstroemia chamaedaphne flower buds). Methods The compounds were separated and purified by chromatography. The structures of compounds were identified by spectral data and single crystal diffraction. The cytotoxicity and anti-HBV activity were tested by MTT assay. Results Nine compounds were isolated and identified from Daphne genkwa, including six diterpene diterpenes: pimelotide A (2), pimelotide C (3), wikstroelide E (4) and pimelea factor S6 5), pimelea factor S7 (6); 1 tigaton type diterpene: 6α, 7α-epoxy-5β-hydroxy-12-deoxyphorbol-13-decanoate (7) and two flavonoid compounds: luteolin- 4’-O-β-D-glucoside (8) and isoquercetin (9). Compounds 1 to 4 and 7 showed strong cytotoxic activity with TC50 value of 3.24-7.30μg / m L, and compound 3 showed significant inhibition of HBsAg production with IC50 of 0.016μg / m L, therapeutic index (TI) value of 355.63. Conclusion Compounds 7 and 8 were isolated from this genus for the first time. The crystal structure of compound 2 was reported for the first time. It was firstly found that compound 3 had a significant inhibitory effect on the production of HBsAg.