牛角瓜强心苷成分的抗肿瘤活性研究  

Anti-tumor activity of cardiac glycosides from Calotropis gigantea

作　　者：宫正 王磊[1] 樊成武 靳云奥 沈彤[1] GONG Zheng;WANG Lei;FAN Cheng-wu;JIN Yun-ao;SHEN Tong(Lanzhou Jiaotong University,Lanzhou 730070,China)

机构地区：[1]兰州交通大学,兰州730070

出　　处：《天然产物研究与开发》2025年第2期271-277,391,共8页Natural Product Research and Development

基　　金：甘肃省农业科技支撑项目(KJZC-2024-16)。

摘　　要：研究牛角瓜(Calotropis gigantea(L.)W.T.Aiton)甲醇提取物的强心苷类化学成分及其对癌细胞的抑制作用。采用多种柱色谱技术和高效液相制备技术对牛角瓜的甲醇提取物进行分离纯化,分离所得的化合物运用NMR、MS等技术进行结构鉴定,并研究这些化合物对人宫颈癌细胞HeLa、人非小细胞肺癌细胞A549和人肝癌细胞HepG2的抗肿瘤作用。最终分离得到6个化合物,分别鉴定为克罗甙元(1)、乌沙甙元(2)、3-O-β-allopyranosyluzarigenin(3)、frugoside(4)、牛角瓜甙(5)、glucocoroglaucigenin(6)。活性研究结果表明,化合物1~6对HeLa、A549和HepG2细胞都具有抑制作用。化合物5能够诱导人宫颈癌细胞HeLa细胞内氧化应激,抑制硫氧还蛋白还原酶1(thioredoxin reductase 1,TrxR1)的活性,并促进细胞凋亡。This study aims to investigate the cardiac glycoside components in the methanol extract of Calotropis gigantea(L.)W.T.Aiton and their inhibitory effect on cancer cells.Various column chromatography techniques and preparative HPLC were used to separate and purify the methanol extract of C.gigantea.The structures of the isolated compounds were identified by NMR,MS techniques.The anti-tumor effects of these compounds on human cervical cancer cells HeLa,human non-small cell lung cancer cells A549 and human hepatocellular carcinoma cells HepG2 were studied.Eventually,six compounds were isolated and identified as coroglaucigenin(1),uzarigenine(2),3-O-β-allopyranosyluzarigenin(3),frugoside(4),calotropin(5),and glucocoroglaucigenin(6).Compounds 1-6 had inhibitory effects on HeLa,A549 and HepG2 cells.Compound 5 could induce intracellular oxidative stress in human cervical cancer cells HeLa,inhibit the activity of thioredoxin reductase 1(TrxR1)and promote apoptosis.

关 键 词：牛角瓜 强心苷 抗肿瘤活性 

分 类 号：O629.2[理学—有机化学]