目的 对仙鹤草Agrimonia pilosa的化学成分进行分离和鉴定，并利用去血清损伤的PC12细胞模型筛选化合物的神经保护活性。方法 利用80%乙醇对仙鹤草进行提取，再通过大孔吸附树脂、ODS、硅胶、Sephadex LH-20凝胶以及半制备型高效液相等柱色谱方法进行分离，然后根据质谱、核磁、圆二色谱等波谱学数据鉴定化合物的结构。结果 从仙鹤草中分离并鉴定了10个木脂素类化合物，分别命名为仙鹤草酸酯（1）、仙鹤草苷A（2）、苦树苷C（3）、长花马先蒿苷B（4）、（7R，8S）-4，7，9，9'-四羟基-3，3'-二甲氧基-8-O-4'-新木脂素-7-O-β-D-葡萄糖苷（5）、（7S，8S）-3-甲氧基-8，4'-氧代新木脂素-3'，4，7，9，9'-五醇（6）、红叶藤苷（7）、（7S，8R）-1-[4-O-（β-D-吡喃葡糖糖基）-3-甲氧基苯基]-2-[4-（3-羟丙基）-2，6-二甲氧基苯氧基]-1，3-丙二醇（8）、密穗马先蒿苷（9）、淫羊藿醇A₂（10）。结论 化合物1 和2 为新化合物，其余化合物均为首次从仙鹤草中分离得到。化合物1a 和1b 为1对互变的葡萄糖端基手性相反的8-O-4'型木脂素酸酯；化合物1 在10 μmol/L对去血清损伤的PC12神经细胞表现出一定的保护作用。

Objective To investigate the chemical constituents of Agrimonia pilosa and evaluate their neuroprotective activities by PC12 cell model. Methods Firstly, the dried plant of A. pilosa were extracted by 80% ethanol aqueous. Then, the compounds were isolated and purified by a variety of chromatographic techniques including HP-20 macroporous resin, ODS, silica gel, Sephadex LH-20, and semi-preparative HPLC. The structures of the isolates were determined by a combination of HR-ESI-MS, NMR, and ECD spectra. Finally, the neuroprotective activities of isolates were tested. Results Ten lignans were isolated and identified as pilosaneolignan ester (1), pilosaneolignanside A (2), picraquassioside C (3), longifloroside B (4), (7R,8S)-4,7,9,9'-tetrahydroxy-3,3'-dimethoxy-8,4'-oxyneolignan-7-O-β-D-glucoside (5), (7S,8S)-3-methoxy-8,4'-oxyneoligna-3',4,7,9,9'-pentol (6), rourinoside (7), (7S,8R)-1-[4-O-(β-D-glucopyranosyl)-3-methoxyphenyl]-2-[4-(3-hydroxy-propyl)-2,6-dimethoxyphenoxy]-1,3-propanediol (8), densispicoside (9), and icariol A₂ (10). Conclusion The structures of 1 and 2 are new compounds, compounds 3-10 are isolated from A. pilosa for the first time. Notably, compounds 1a and 1b represent a pair of interchangeable 8,4'-oxyneolignan glucose ester with the opposite hemiacetal hydroxy. Compound 1 exhibits the moderate protective effect on injury induced by serum deprivation in PC12 cells at 10 μmol/L.

R284.1

中国医学科学院医学与健康科技创新工程（2019-I2M-1-005）