Cytotoxic and Pro-apoptotic Activities of Sesquiterpene Lactones from Inula Britannica
Cytotoxic and Pro-apoptotic Activities of Sesquiterpene Lactones from Inula Britannica
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DOI：
10.1177/1934578x1601100103
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发表时间：
2016-01
影响因子：
1.8
通讯作者：
Ping Xiang;Xin Guo;Yangyang Han;Jin-Ming Gao;Jiangjiang Tang
中科院分区：
文献类型：
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作者：
Ping Xiang;Xin Guo;Yangyang Han;Jin-Ming Gao;Jiangjiang Tang
本研究从药用植物不列颠旋覆花的花冠中分离得到5个具有α-亚甲基-γ-内酯结构的倍半萜内酯，其中包括2个桉树内酯，1个β-羟基马蹄内酯(1)和2个伊万古斯汀(2)，以及3个1，10-二乙基马蹄内酯(3)，1，6-O，O-二乙酰基巴丁内酯(4)和6个α-O(2-甲基丁基)巴丹内酯(5)。用波谱方法对它们的结构进行了表征。首次报道了2的X射线数据。其中，桉内酯1和2对HEp2、SGC-7901和HCT116人癌细胞具有显著的细胞毒作用，与以依托泊苷(VP-16)为参照物的细胞毒作用相当。此外，1诱导HEp2细胞凋亡与裂解原天冬氨酸酶-3和PARP有关。用正常细胞(CHO)进行的生物测定表明，所有倍半萜对所测试的癌细胞株都具有弱的选择性。
In this study, five known sesquiterpene lactones (STL) with an α-methylene-γ-lactone motif, including two eudesmanolides, 1β-hydroxyalantolactone (1) and ivangustin (2), and three 1,10-seco-eudesmanolides, 1-O-acetylbritannilactone (3), 1,6-O, O-diacetylbritannilactone (4), and 6α-O(2-methylbutyryl)britannilactone (5) were isolated from the flower heads of the medicinal plant Inula britannica. Their structures were characterized by spectroscopic methods. X-ray data of 2 is reported for the first time. Among them, eudesmanolides 1 and 2 exhibited remarkable cytotoxicity against HEp2, SGC-7901 and HCT116 human cancer cell lines, comparable with etoposide (Vp-16) used as reference drug. Furthermore, treatment of HEp2 cells with 1 induced apoptosis associated with cleaved procaspase-3 and PARP. The biological assays carried out with normal cells (CHO) revealed that all sesquiterpenes were weakly selective against the cancer cell lines tested.