摘要
目的研究川芎Ligusticum chuanxiong茎叶醇提物具有舒张血管活性的苯酞类成分。方法采用MCI、硅胶、Sephadex LH-20、中压液相色谱、半制备高效液相色谱等方法进行研究。并比较了苯酞和苯酞二聚体对离体大鼠胸主动脉环的舒张作用。结果从川芎茎叶中分离出10个苯酞化合物,分别鉴定为Z-3-丁烯基苯酞(1)、洋川芎内酯-E(2)、Z-洋川芎内酯-H(3)、(3Z,7β)-3-丁烯基-7-羟基-4,5,6,7-四氢苯酞(4)、新藁本内酯(5)、Z,Z′-3.3′a,7.7′a-双藁本内酯(6)、3Z,3Z′-6,8′,7,3′-双藁本内酯(7)、Z-东当归内酯A(8)、(3′Z)-(3S,8R,3a′S,6′R)-4,5-去氢-3.3′a,8.6′-双藁本内酯(9)、(3Z)-(3a R,6S,3′R,8′S)-3a.8′,6.3′-双藁本内酯(10)。化合物1、6~9能显著降低氯化钾预收缩大鼠胸主动脉环的张力。其中化合物6~8最高浓度(12μmol/L)舒张率分别为60%、52%、70%,半数有效浓度(EC50)分别为9.46、11.86、8.73μmol/L。结论所有化合物均为首次从川芎茎叶中分离得到,化合物6和8为首次从川芎中分离。受试化合物均有舒张血管活性,且二聚体的活性优于单苯酞。
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),(3 Z,7β)-3-butenyl-7-hydroxy-4,5,6,7-tetrahydrophthalide(4),neoligustilide(5);Z,Z′-3.3′a,7.7′a-diligustilide(6),3 Z,3 Z′-6,8′,7,3′-diligustilide(7),Z-tokinolide A(8),(3′Z)-(3 S,8 R,3 a′S,6′R)-4,5-dehydro-3.3′a,8.6′-diligustilide(9),and(3 Z)-(3 a R,6 S,3′R,8′S)-3 a.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(12μmol/L),respectively.The EC50 was 9.46,11.86 and 8.73μmol/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.
作者
唐飞
谭玉柱
敖慧
闫洪玲
罗巍
杨琴
胡昌江
彭成
TANG Fei;TAN Yu-zhu;AO Hui;YAN Hong-ling;LUO Wei;YANG Qin;HU Chang-jiang;PENG Cheng(State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China,College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Innovation Institute of Chinese Medicine and Pharmacy,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Key Laboratory of Quality Control and Efficacy Evaluation of Traditional Chinese Medicine Formula Granules,Sichuan New Green Medicine Science and Technology Development Co.,Ltd.,Pengzhou 610031,China)
出处
《中草药》
CAS
CSCD
北大核心
2020年第5期1190-1195,共6页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金青年基金项目(81703693)
“杏林学者”学科人才科研提升计划(QNXZ2018009)
第65批中国博士后基金面上项目(2019M653363)
四川省科技创新(苗子工程)培育项目(2019052).
作者简介
唐飞(1996—),男,硕士研究生,主要从事中药药效与物质基础研究。E-mail:1428921639@qq.com;通信作者:胡昌江,博士生导师,教授,研究方向为中药炮制原理及饮片质量标准研究。E-mail:hhccjj@hotmail.com;通信作者:彭成,博士生导师,教授,研究方向为中药药效与毒理研究。Tel:(028)61800232 E-mail:pengchengchengdu@126.com;并列第一作者:谭玉柱(1985—),男,实验师,从事中药药效物质基础研究。Tel:(028)61800231 E-mail:tanyuzhu@cdutcm.edu.cn
