CAJ | 학술논문

目的：应用高通量药物筛选技术发现山豆根乙醇提取物具有较强的抑制丁酰胆碱酯酶（BuChE）活性。采用超高效液相色谱与串联四级杆飞行时间质谱仪联用技术（UPLC-Q-TOF-MS）对其活性部位组分进行分析和鉴定。方法：药材经石油醚渗滤、乙醇提取、乙酸乙酯萃取和水煎煮后，得到4个提取部位。采用5，5′-二硫双硝基苯甲酸（DTNB）法检测 BuChE 活性，并应用 UPLC-Q-TOF-MS 对其活性部位组分进行分析和鉴定。结果：山豆根的乙醇部位显示较强的 BuChE 抑制活性，并从其活性部位中分析鉴定了9个化合物，其中7个化合物主要成分为苦参碱类生物碱，属于喹诺里西啶类生物碱，分别是槐醇、苦参碱、氧化苦参碱、槐定碱、9a-羟基苦参碱、14β-羟基氧化苦参碱、Lamprolobine；2个黄酮类成分分别是 Kushenol O、Kushenol I ／N。山豆根乙醇提取部位 IC50为15.169μg·mL －1。结论：首次发现山豆根乙醇提取部位具有较强的 BuChE 抑制活性，其主要化学成分为苦参碱类生物碱，研究表明山豆根具有延缓老年痴呆的作用，为研发延缓老年痴呆新药提供科学依据。
목적：응용고통량약물사선기술발현산두근을순제취물구유교강적억제정선담감지매（BuChE）활성。채용초고효액상색보여천련사급간비행시간질보의련용기술（UPLC-Q-TOF-MS）대기활성부위조분진행분석화감정。방법：약재경석유미삼려、을순제취、을산을지췌취화수전자후，득도4개제취부위。채용5，5′-이류쌍초기분갑산（DTNB）법검측 BuChE 활성，병응용 UPLC-Q-TOF-MS 대기활성부위조분진행분석화감정。결과：산두근적을순부위현시교강적 BuChE 억제활성，병종기활성부위중분석감정료9개화합물，기중7개화합물주요성분위고삼감류생물감，속우규낙리서정류생물감，분별시괴순、고삼감、양화고삼감、괴정감、9a-간기고삼감、14β-간기양화고삼감、Lamprolobine；2개황동류성분분별시 Kushenol O、Kushenol I ／N。산두근을순제취부위 IC50위15.169μg·mL －1。결론：수차발현산두근을순제취부위구유교강적 BuChE 억제활성，기주요화학성분위고삼감류생물감，연구표명산두근구유연완노년치태적작용，위연발연완노년치태신약제공과학의거。
Objective:Alzheimer’s disease (AD),is a common old age chronic degenerative nerve disease.Using cholinesterase inhibitor to improve AD patients choline levels,is currently the only acknowledged drug treatments.Methods:High-throughput drug screening was applied to screen butyrylcholinesterase inhibitory activity of Sophora tonkinensis extracts, and analyzed the active ingredients,The constituents in S.tonkinensis were determined by UPLC /Q-TOF-MS.Herbs were percolated with petroleum ether,ethanol,ethyl acetate and water,and the corresponding parts of the four extraction were obtained.BuChE inhibitory activity of the candidate compounds was assayed based on thionitrobenzoication (DTNB ) method.The mass spectrometer equipped with electrospray ionization source was used as defector and operated in data collected under the positive ion modes.Results:The ethanol extraction part of S.tonkinensis showed a strong activity.9 kinds compounds were analyzed and identified,among them 7 mainly were matrine type alkaloids,including sophoranol,sophoridine,matrine, oxymatrine,9a-Hydroxymatrine, lamprolobine, 14β-Hydroxyoxymatrine, 2 flavonoids were kushenol I /N, kushenol O.Conclusion:The study indicated that extracted with ethanol of S.tonkinensis has significant butyrylcholinesterase inhibition activity for the first time,and IC50 values is 15.169 μg·mL -1 ,the main compounds mainly is alkaloids of matrine,that indicated that S.tonkinensis,has a certain effect on BuChE,which will provide scientific basis for AD drug resistance research.