东北延胡索块茎中的生物碱及其抗肿瘤活性研究  

Alkaloids from the tubers of Corydalis ambigua var. amurensis and their antitumor activities

作　　者：常生 刘志惠[2] 韩娜[2] 杨志友[2] 王盼盼 李凡 殷军[2] CHANG Sheng;LIU Zhi-hui;HAN Na;YANG Zhi-you;WANG Pan-pan;LI Fan;YIN Jun(Heping Hospital Affiliated to Changzhi Medical College,Changzhi Medical College,Changzhi 046000,China;School of Traditional Chinese Medicine,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]长治医学院,长治医学院附属和平医院,山西长治046000 [2]沈阳药科大学中药学院,辽宁沈阳110016

出　　处：《中成药》2022年第11期3507-3513,共7页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(81573628,81872982);辽宁省重点实验室项目[2011(20)];辽宁省教育厅科技规划项目(L2014381)。

摘　　要：目的研究东北延胡索Corydalis ambigua Cham.et Schlecht.var.amurensis Maxim.块茎中生物碱类成分及其体外抗肿瘤活性。方法对东北延胡索80%乙醇提取物采用硅胶、Sephadex LH-20、薄层制备色谱等方法进行分离纯化,根据理化性质及波谱数据鉴定所得化合物的结构。MTT法测定化合物体外抗HepG2、HCT116、A549、HL60细胞活性。结果从中分离得到16个化合物,分别鉴定为华尖碱(1)、紫堇达明碱(2)、卡维丁(3)、紫堇碱(4)、11-去甲氧基白元胡碱(5)、3-去甲基白元胡碱(6)、2-去甲基白元胡碱(7)、8-羟甲基白元胡碱(8)、6-乙酰基-14-羟基-8-羟甲基白元胡碱(9)、6-乙酰基-N-去甲基白元胡碱(10)、11-去甲基白元胡碱(11)、6-乙酰基白元胡碱(12)、白元胡碱(13)、2,11-二去甲基白元胡碱(14)、去氢卡维丁(15)、药根碱(16)。化合物6对HCT116细胞的IC_(50)为(9.30±1.06)μmol/L,化合物1对A549细胞的IC_(50)为(20.89±3.13)μmol/L。结论化合物4、14~16为首次从块茎中分离得到,化合物15、16首次从该植物中分离得到。化合物6可抑制HCT116细胞增殖。AIM To study the alkaloids of the tubers of Corydalis ambigua Cham.et Schlecht.var.amurensis Maxim.and their antitumor activities in vitro.METHODS The 80%ethanol extract from the tubers were isolated and purified by silica gel column chromatography,Sephadex LH-20 column chromatography and PTLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The antitumor activities of compounds against HepG2,HCT116,A549 and HL-60 cells in vitro were evaluated by MTT method.RESULTS Sixteen compounds were isolated and identified as sinactine(1),corydalmine(2),cavidine(3),corydaline(4),11-demethoxyambinine(5),3-demethylambinine(6),2-demethylambinine(7),8-hydroxymethyl-ambinine(8),6-acetyl-14-hydroxy-8-hydroxymethyl-ambinine(9),6-acetyl-N-demethylambinine(10),11-demethylambinine(11),6-acetylambinine(12),ambinine(13),2,11-didemethylambinine(14),dehydrocavidine(15)and jatrorrhizine(16).Compound 6 exhibited inhibitory activity on the proliferation of HCT116 cells with IC_(50) values of(9.30±1.06)μmol/L.Compound 1 exhibited inhibitory activity on the proliferation of A549 cells with IC_(50) values of(20.89±3.13)μmol/L.CONCLUSION Compunds 4,14-16 are isolated from the tubers for the first time,while compounds 15 and 16 are isolated from C.ambigua var.amurensis for the first time.Compound 6 shows good inhibitory activity against HCT116 cells.

关 键 词：东北延胡索 块茎 生物碱类成分 化学成分 分离鉴定 抗肿瘤活性 

分 类 号：R284.1[医药卫生—中药学]