目的 研究川芎Ligusticum chuanxiong莖葉醇提物具有舒張血管活性的苯酞類成分。方法 采用MCI、硅膠、Sephadex LH-20、中壓液相色譜、半制備高效液相色譜等方法進行研究。并比較了苯酞和苯酞二聚體對離體大鼠胸主動脈環(huán)的舒張作用。結(jié)果 從川芎莖葉中分離出10個苯酞化合物，分別鑒定為Z-3-丁烯基苯酞（1）、洋川芎內(nèi)酯-E（2）、Z-洋川芎內(nèi)酯-H（3）、（3Z，7β）-3-丁烯基-7-羥基-4，5，6，7-四氫苯酞（4）、新藁本內(nèi)酯（5）、Z，Z'-3.3'a，7.7'a-雙藁本內(nèi)酯（6）、3Z，3Z'-6，8'，7，3'-雙藁本內(nèi)酯（7）、Z-東當歸內(nèi)酯A（8）、（3'Z）-（3S，8R，3a'S，6'R）-4，5-去氫-3.3'a，8.6'-雙藁本內(nèi)酯（9）、（3Z）-（3aR，6S，3'R，8'S）-3a.8'，6.3'-雙藁本內(nèi)酯（10）?；衔?b>1、6～9能顯著降低氯化鉀預(yù)收縮大鼠胸主動脈環(huán)的張力。其中化合物6～8最高濃度（12 μmol/L）舒張率分別為60%、52%、70%，半數(shù)有效濃度（EC₅₀）分別為9.46、11.86、8.73 μmol/L。結(jié)論 所有化合物均為首次從川芎莖葉中分離得到，化合物6和8為首次從川芎中分離。受試化合物均有舒張血管活性，且二聚體的活性優(yōu)于單苯酞。

Objective To study the phthalides with vasodilating activity of alcohol extracts from stems and leaves of Ligusticum chuanxiong. Methods Compounds were isolated by extensive chromatographic techniques including MCI, silica gel, Sephadex LH-20, ODS, and semi-preparative HPLC. The vasodilating effect of phthalide and dimer phthalide on thoracic aortic ring in vitro was investigated. Results Ten phthalides were isolated and identified, and their structures were elucidated as Z-3-butylidenephthalide (1), senkyunolide-E (2), Z-senkyunolide-H (3), (3Z,7β)-3-butenyl-7-hydroxy-4,5,6,7-tetrahydrophthalide (4), neoligustilide (5); Z,Z'-3.3'a,7.7'a-diligustilide (6), 3Z,3Z'-6,8',7,3'-diligustilide (7), Z-tokinolide A (8), (3'Z)-(3S,8R,3a'S,6'R)-4,5-dehydro- 3.3'a,8.6'-diligustilide (9), and (3Z)-(3aR,6S,3'R,8'S)-3a.8',6.3'-diligustilide (10). Compound 1, 6-9 significantly reduced the strain of thoracic aortic ring in KCl preconstricted rats. The diastolic rate of compounds 6-8 were 60%, 52% and 70% at the highest concentrations (12 μmol/L), respectively. The EC₅₀ was 9.46, 11.86 and 8.73 μmol/L, respectively. Conclusion All compounds are firstly isolated from the stems and leaves of L. chuanxiong. Compounds 6, 8 are firstly isolated from L. chuanxiong. The test compounds could dilate blood vessels, and the activity of dimer phthalide was better than that of phthalide.

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國家自然科學基金青年基金項目（81703693）；“杏林學者”學科人才科研提升計劃（QNXZ2018009）；第65批中國博士后基金面上項目（2019M653363）；四川省科技創(chuàng)新（苗子工程）培育項目（2019052）