川芎化学成分及其抑制子宫平滑肌收缩作用(Ⅱ)  

Chemical constituents from Ligusticum striatum and their inhibitory effects on uterine smooth muscle contraction(Ⅱ)

作　　者：冯芮 彭成[1] 周飞 郭力[1,2] 刘娟 熊亮[1,2] FENG Rui;PENG Cheng;ZHOU Fei;GUO Li;LIU Juan;XIONG Liang(State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China,School of Pharmaceutical,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Institute of Innovative Medicine Ingredients of Southwest Specialty Medicinal Materials,Chengdu University of TCM,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院省部共建西南特色中药资源国家重点实验室,四川成都611137 [2]成都中医药大学西南特色药材创新药物成分研究所,四川成都611137

出　　处：《中成药》2021年第11期3032-3037,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金优秀青年科学基金(82022072);国家自然科学基金区域联合基金项目(U19A2010);霍英东教育基金项目(171037);四川省科技创新苗子工程培育项目(2019046);四川省天府“万人计划”人才计划(168);成都中医药大学西南特色中药资源重点实验室开放研究基金资助项目(2020XSGG015,2020BSH013);成都中医药大学“杏林学者”学科人才提升计划(BSH2019028);四川省卫生和计划生育委员会项目(18PJ555)。

摘　　要：目的研究川芎Ligusticum striatum DC.的化学成分及其抑制子宫平滑肌收缩作用。方法川芎水提物正丁醇萃取部位采用硅胶、ODS、Sephadex LH-20和半制备液相进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。采用缩宫素致大鼠离体子宫平滑肌痉挛模型考察其对子宫平滑肌收缩活动的影响。结果从中分离得到10个化合物,分别鉴定为环(L-苯丙氨酸-L-丝氨酸)(1)、环(D-苯丙氨酸-L-丝氨酸)(2)、环(L-苯丙氨酸-L-谷氨酰胺)(3)、2-isopropyl-5-phenylmethyl-imidazolidinone-4-one(4)、环(L-苯丙氨酸-L-丙氨酸)(5)、环(L-酪氨酸-L-亮氨酸)(6)、环(L-苯丙氨酸-L-酪氨酸)(7)、4(3H)-喹唑酮(8)、3-羟基喹啉(9)、marinoquinoline K(10)。与空白组比较,化合物2和5在高剂量时对子宫收缩张力、收缩活力表现出抑制作用,中、低剂量组无明显作用。结论所有化合物均为首次从该植物和藁本属中分离得到,化合物2、5在50μmol/L时对离体子宫平滑肌收缩活动有抑制作用。AIM To study the chemical constituents from Ligusticum striatum DC.and their inhibitory effects on uterine smooth muscle contraction.METHODS The n-butanol fraction of aqueous extract from L.striatum was isolated and purified by silica,ODS,Sephadex LH-20 and semi preparative liquid chromatography,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their inhibitory effects on uterine smooth muscle contraction were investigated by rat uterine smooth muscle spasm model induced by oxytocin.RESULTS Ten compounds were isolated and identified as cyclo-(L-Phe-L-Ser)(1),cyclo-(D-Phe-L-Ser)(2),cyclo-(L-Phe-L-Gln)(3),2-isopropyl-5-phenylmethyl-imidazolidinone-4-one(4),cyclo-(L-Phe-L-Ala)(5),cyclo-(L-Tyr-L-Leu)(6),cyclo-(L-Phe-L-Tyr)(7),quinazolin-4(3 H)-one(8),3-hydroxyquinoline(9)and marinoquinoline K(10).Compared with the blank group,compounds 2,5 showed the inhibitory effect on uterine contractile tension and contractility activity at the high dose,while the medium and low dose groups had no obvious effect.CONCLUSION All the compounds are isolated from this plant and genus Ligusticum for the first time.Compounds 2,5 have the inhibitory effects on the contractile activity of isolated uterine smooth muscle at 50μmol/L.

关 键 词：川芎 化学成分 分离鉴定 抑制子宫平滑肌收缩 

分 类 号：R284.1[医药卫生—中药学]