广西地不容块根化学成分及其酪氨酸酶抑制、杀虫活性研究  

Chemical constituents from the root tubers of Stephania kwangsiensis and their tyrosinase inhibition and insecticidal activities

作　　者：农艳婷 邹碧群[3] 曾思文 王亚凤[2] 阳丙媛 黄永林[2] 郭伦发[2] 杨克迪 何瑞杰[2] 葛利 NONG Yan-ting;ZOU Bi-qun;ZENG Si-wen;WANG Ya-feng;YANG Bing-yuan;HUANG Yong-lin;GUO Lun-fa;YANG Ke-di;HE Rui-jie;GE Li(Medical College of Guangxi University,Nanning 530004,China;Guangxi Key Laboratory for Functional Phytochemicals and Continuous Utilization of Resources,Guangxi Institute of Botany,Guangxi Zhuang Autonomous Region and Chinese Academy of Sciences,Guilin 541006,China;Department of Chemistry and Pharmaceutical Science,Guilin Normal College,Guilin 541199,China;School of Chemistry&Chemical Engineering,Guangxi University,Nanning 530004,China)

机构地区：[1]广西大学医学院,广西南宁530004 [2]广西壮族自治区中国科学院广西植物研究所,广西植物功能物质与资源持续利用重点实验室,广西桂林541006 [3]桂林师范高等专科学校化学与药学系,广西桂林541199 [4]广西大学化学化工学院,广西南宁530004

出　　处：《中成药》2024年第10期3310-3315,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(32060108,82060764);广西自然科学基金(2018GXNSFAA294033,2023GXNSFAA02642);广西重点研发计划(桂科AB23026013);广西植物功能物质与资源持续利用重点实验室开放基金(FPRU2022-5);广西药物分子发现与成药性优化重点实验室开放课题(GKLDDO-2023-B01);桂北特色药资源研究中心科研项目(YJZX202104);桂林市创新平台和人才计划(20210102-3)。

摘　　要：目的研究广西地不容块根化学成分及其酪氨酸酶抑制、杀虫活性。方法广西地不容块根70%乙醇提取物采用Sephadex LH-20、MCI、ODS、半制备HPLC、HSCCC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。以左旋多巴为底物,测定酪氨酸酶抑制活性。以柑橘木虱防治效果为指标,评价杀虫活性。结果从中分离得到12个化合物,分别鉴定为延胡索乙素(1)、去氢克班宁(2)、crebanine(3)、stephanine(4)、liriodenine(5)、piperumbellactam A(6)、sinoacutine(7)、(+)-salutaridine N-oxide(8)、bisnorargemonine(9)、(+)-corytuberine(10)、sebiferine(11)、palmatrubine(12)。化合物5~7对酪氨酸酶IC 50值分别为(0.1702±0.0101)、(0.7663±0.0331)、(0.5193±0.0075)mg/mL。化合物2~5、7、8、10~12对柑橘木虱的防治效果在(19.33±0.57)%~(77.15±0.45)%之间。结论化合物2、5、6、8~12为首次从该植物块根中分离得到,6、9为首次从千金藤属植物中分离得到。化合物5~7具有较强的酪氨酸酶抑制活性,7、8、10具有较强的杀虫活性。AIM To study the chemical constituents from the root tubers of Stephania kwangsiensis H.S.Lo and their tyrosinase inhibition and insecticidal activities.METHODS The 70%ethanol extract from root tubers of S.kwangsiensis was isolated and purified by Sephadex LH-20,MCI,ODS,semi-prepative HPLC and HSCCC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The tyrosinase inhibitory activities were determined by using levodopa as substrate,and the insecticidal activities were evaluated by the control effect of Diaphorina citri.RESULTS Twelve compounds were isolated and identified as tetrahydropalmatine(1),dehydrocrebanine(2),crebanine(3),stephanine(4),liriodenine(5),piperumbellactam A(6),sinoacutine(7),(+)-salutaridine N-oxide(8),bisnorargemonine(9),(+)-corytuberine(10),sebiferine(11)and palmatrubine(12).The IC 50 values of compounds 5-7 to tyrosinase were(0.1702±0.0101),(0.7663±0.0331)and(0.5193±0.0075)mg/mL,respectively.The control effects of compounds 2-5,7,8,10-12 against D.citri ranged from(19.33±0.57)%to(77.15±0.45)%.CONCLUSION Compounds 2,5,6,and 8-12 are isolated from this plant for the first time,6 and 9 are first obtained from genus Stephania.Compounds 5-7 displayed significant tyrosinase inhibition activities.Compounds 7,8 and 10 show strong insecticidal activities.

关 键 词：广西地不容 块根 化学成分 分离鉴定 酪氨酸酶 杀虫活性 

分 类 号：R284.1[医药卫生—中药学]