Phan Minh Giang, Do Thi Thao, Nguyen Thi Nga, Do Thi Viet Huong, Dong Ngoc Phuc, Vu Minh Trang
Faculty of Chemistry, VNU University of Science, Vietnam National University, 19 Le Thanh Tong Street, Hanoi, Vietnam.
Institute of Biotechnology, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet Road, Hanoi, Vietnam.
Evid Based Complement Alternat Med. 2021 May 18;2021:6610347. doi: 10.1155/2021/6610347. eCollection 2021.
Thunb. of the plant family Asteraceae is a popular traditional herb in Vietnam. However, its chemical constituents as well as bioactive principles have not been investigated yet. We investigated the phytochemistry of in Vietnam and isolated seventeen compounds including phytosterols, terpenoids, phenolic acids, flavonoids, fatty alcohols, and fatty acids. They were structurally determined by MS and NMR analysis. Except for compounds and , all the other compounds were identified for the first time from . Since many sesquiterpene lactones with -methylene -lactone ring are reported as anti-inflammatory and anticancer agents, eupatoriopicrin , 1-hydroxy-8-(4,5-dihydroxytigloyloxy)eudesma-4(15),11(13)-dien-6,12-olide were selected among the isolates for biological assays. Compound was identified as the main bioactive sesquiterpene lactone of showing its potent anti-inflammatory and cytotoxic activity through inhibiting NO production and the growth of HepG2 and MCF-7 human cancer cell lines. For the first time, eupatoriopicrin was demonstrated to strongly inhibit NTERA-2 human cancer stem cell (CSC) line . It is noticeable that the cytotoxicity of eupatoriopicrin against NTERA-2 cells is mediated by its apoptosis-inducing capability of as demonstrated by the results of Hoechst 33342 staining, flow cytometry apoptosis analysis, and caspase-3 activity assays. The biological activities of the main bioactive constituents -, , , and supported the reported anti-inflammatory and anticancer properties of extracts from .
菊科植物的 Thunb. 是越南一种受欢迎的传统草药。然而，其化学成分以及生物活性成分尚未得到研究。我们对越南的 进行了植物化学研究，分离出 17 种化合物，包括植物甾醇、萜类化合物、酚酸、黄酮类化合物、脂肪醇和脂肪酸。通过质谱和核磁共振分析确定了它们的结构。除化合物 和 外，所有其他化合物均首次从 中鉴定出来。由于许多具有 -亚甲基 -内酯环的倍半萜内酯被报道为抗炎和抗癌剂，因此从分离物中选择了泽兰苦内酯、1-羟基-8-(4,5-二羟基惕各酰氧基)桉叶-4(15),11(13)-二烯-6,12-内酯进行生物测定。化合物 被鉴定为 的主要生物活性倍半萜内酯，通过抑制一氧化氮生成以及 HepG2 和 MCF-7 人癌细胞系的生长显示出其强大的抗炎和细胞毒性活性。首次证明泽兰苦内酯能强烈抑制 NTERA-2 人癌干细胞 (CSC) 系 。值得注意的是，如 Hoechst 33342 染色、流式细胞术凋亡分析和 caspase-3 活性测定结果所示，泽兰苦内酯对 NTERA-2 细胞的细胞毒性是由其诱导凋亡的能力介导的。主要生物活性成分 -、、、和 的生物活性支持了报道的 的提取物的抗炎和抗癌特性。
