川牛膝化学成分及其舒张子宫平滑肌活性研究  

Chemical constituents from Cyathulae Radix and their relaxant effects on uterine smooth muscle

作　　者：文敏 赵芮 孙美记 彭成[1,3] 刘娟 熊亮[1,2,3] WEN Min;ZHAO Rui;SUN Mei-ji;PENG Cheng;LIU Juan;XIONG Liang(State Key Laboratory of Southwestern Chinese Medicine Resources,School of Pharmacy,Chengdu University of Traditional Chi nese Medicine;College of Medical Technology,Chengdu University of Traditional Chinese Medicine;Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院西南特色中药资源国家重点实验室 [2]成都中医药大学医学技术学院 [3]成都中医药大学西南特色药材创新药物成分研究所,成都611137

出　　处：《天然产物研究与开发》2025年第2期252-261,共10页Natural Product Research and Development

基　　金：国家自然科学基金青年基金(82104371);国家中医药管理局中医药创新团队及人才支持计划(ZYYCXTD-D-202209);四川省科技创新人才计划(2023JDRC0041)。

摘　　要：本文旨在探究川牛膝提取物及其化学成分的舒张子宫平滑肌活性。利用离体子宫收缩模型对川牛膝乙醇提取物及其乙酸乙酯萃取部位和正丁醇萃取部位的舒张子宫平滑肌活性进行评价,确定最佳活性部位。采用硅胶柱层析、制备薄层层析和半制备高效液相色谱等方法对活性部位进行分离纯化,运用多种现代波谱学技术对分离得到的化合物进行结构鉴定,并对其舒张子宫平滑肌活性进行测定分析。结果显示:与对照组比较,0.4 mg/mL的乙酸乙酯萃取部位能显著(P<0.01)抑制大鼠子宫平滑肌的收缩张力和收缩活力并表现出最佳活性,其抑制率分别为(67.09±5.37)%和(79.27±2.49)%。此外,在累计给药下,川牛膝乙酸乙酯萃取物的最大张力抑制率可达(77.45±12.12)%,EC 50为(0.10±0.01)mg/mL。从川牛膝乙酸乙酯部位分离鉴定出9个化合物,即irilin A(1)、irilin B(2)、2′-羟基-5,6,7-三甲氧基异黄酮(3)、β-谷甾醇葡萄糖苷(4)、滨蒿内酯(5)、N-顺式-阿魏酰-3-甲氧基酪胺(6)、N-反式-阿魏酰甲氧基酪胺(7)、N-顺式-阿魏酰酪胺(8)、N-反式-阿魏酰酪胺(9),化合物2、3、6、7、8、9为首次从川牛膝中分离得到。与对照组比较,化合物1~3、5~9在50μmol/L时均能抑制子宫平滑肌的收缩张力及收缩活力(P<0.05或P<0.01),其中化合物2在50μmol/L时,张力抑制率可达(36.16±2.75)%,活力抑制率可达(47.03±5.84)%。本文通过现代分离纯化技术和离体子宫收缩模型,发现了具有舒张子宫平滑肌活性的川牛膝提取物及化学成分,为阐明川牛膝治疗痛经的物质基础提供了依据。In this study,the relaxant activity on uterine smooth muscle of the extracts and chemical components from Cyathulae Radix was investigated.The uterine contraction model in vitro was used to evaluate the uterine smooth muscle relaxant activity of the 70%EtOH extract and its EtOAc and n-BuOH fractions of Cyathulae Radix.Silica gel column chromatography,preparative thin layer chromatography,and semi-preparative high performance liquid chromatography were used to isolate the compounds from the best active portion,then the structures of isolated compounds were determined by various modern spectroscopic techniques.Finally,the relaxant effects of these compounds on uterine smooth muscle was screened.The results showed that the EtOAc fraction(0.4 mg/mL)could significantly inhibited the contractile tension and contractile activity inhibition on rat uterine smooth muscle and exhibited the best activity,with inhibition rates at(67.09±5.37)%and(79.27±2.49)%.In addition,under the cumulative dosing,the maximum tension inhibition rate was(77.45±12.12)%,and the EC 50 was 0.10±0.01 mg/mL.Nine compounds were isolated from the EtOAc fraction of Cyathulae Radix and were identified as irilin A(1),irilin B(2),2′-hydroxy-5,6,7-trimethoxyisoflavone(3),betavulgarin(4),scoparone(5),N-cis-feruloyl-3-methoxytyramine(6),N-trans-feruloylmethoxytyramine(7),N-cis-fruloyltyramine(8),and N-trans-feruloyltyramine(9).Among them,compounds 2,3,6,7,8 and 9 were isolated from this plant for the first time.Compared with control,compounds 1-3,5-9 inhibited the contractile tension and activity on uterine smooth muscle at 50μmol/L(P<0.05 or P<0.01),among which compound 2 had the best activity,with an tension inhibition rate of(36.16±2.75)%and the activity inhibition rate of(47.03±5.84)%at 50μmol/L.In this study,the relaxant activity on the uterine smooth muscle of Cyathulae Radix extract and its chemical components were found,which provided a scientific basis for clarifying the material basis of Cyathulae Radix in the treatment of dysmenorrhea.

关 键 词：川牛膝 提取物 化学成分 舒张子宫平滑肌 

分 类 号：R284.2[医药卫生—中药学] R285.5[医药卫生—中医学]