荷叶中的生物碱及其对5-HT 2A和5-HT 2C受体的激动作用研究  

Alkaloids from leaves of Nelumbo nucifera Gaertn.and their agonistic activities on 5-HT 2A and 5-HT 2C receptors

作　　者：王豪 刘艳芳 王委 芮海云[1] 董好岩 WANG Hao;LIU Yan-fang;WANG Wei;RUI Hai-yun;DONG Hao-yan(Jiangsu Key Laboratory of Chiral Pharmaceuticals Biosynthesis,Taizhou University;Center for Novel Drug Development of Taizhou,Taizhou 225300,China;Dalian Institute of Chemical Physics,Chinese Academy of Sciences,Dalian 116023,China)

机构地区：[1]泰州学院江苏省手性医药化学品生物制造重点实验室 [2]泰州新药创制服务中心,泰州225300 [3]中国科学院大连化学物理研究所,大连116023

出　　处：《天然产物研究与开发》2023年第4期656-661,721,共7页Natural Product Research and Development

基　　金：江苏省高校自然科学基金面上项目(18KJB350011)。

摘　　要：对荷叶中的生物碱进行了分离、鉴定和调脂减肥活性研究。本研究结合传统酸提碱沉法与现代高效液相色谱制备技术,从荷叶中分离、纯化到11个生物碱,分别被鉴定为N-氧基原荷叶碱(1)、原荷叶碱(2)、莲碱(3)、降氧化北美黄连次碱(4)、荜茇宁(5)、巴婆碱(6)、O-去甲基荷叶碱(7)、N-去甲基荷叶碱(8)、荷叶碱(9)、衡州乌药碱(10)和亚美罂粟碱(11),其中,化合物1、4和5为首次从荷叶中分得。测试所得化合物对5-HT_(2A)和5-HT_(2C)受体的激动作用,结果表明11个生物碱对5-HT_(2A)受体均具有一定的激动作用,进一步揭示了荷叶调脂减肥的可能药效基础和作用机理。The alkaloids in leaves of Nelumbo nucifera Gaertn.were isolated,identified and evaluated for their lipid-regulating activities on receptors 5-HT 2A and 5-HT 2C in this study.Eleven alkaloids were isolated and purified from lotus leaves by combining the traditional acid extraction and alkali precipitation method with modern high-performance liquid chromatography techniques,and were identified as pronuciferine N-oxide(1),pronuciferine(2),roemerine(3),noroxyhydrastinine(4),piperlonguminine(5),asimilobine(6),O-nornuciferine(7),N-nornuciferine(8),nuciferine(9),coclaurine(10)and armepavine(11),respectively.Among them,compounds 1,4 and 5 were obtained from the title plant for the first time.It is revealed that all alkaloids possessed interesting agonistic activities on 5-HT_(2A)receptor by an MTT assay on HEK 293 cell lines,which implied the potential chemical substance and pharmacological mechanism of the lipid-regulating activities of lotus leaves.

关 键 词：荷叶 生物碱 5-羟色胺受体 调脂 减肥 

分 类 号：R284.1[医药卫生—中药学]