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积雪草酸苷 I,一种植物来源的双达玛烷型糖苷皂甙,在体外能诱导人肝癌细胞凋亡,并能抑制体内肿瘤生长。

Segetoside I, a plant-derived bisdesmosidic saponin, induces apoptosis in human hepatoma cells in vitro and inhibits tumor growth in vivo.

机构信息

Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, PR China; Department of Biochemistry and Biotechnology, College of Science, KwameNkrumah University of Science and Technology, Kumasi-Ghana.

Department of Pharmaceutics, School of Pharmacy, Center for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, PR China.

出版信息

Pharmacol Res. 2016 Aug;110:101-110. doi: 10.1016/j.phrs.2016.04.032. Epub 2016 May 12.

DOI:10.1016/j.phrs.2016.04.032
PMID:27180010
Abstract

Segetoside I is a plant-derived bisdesmosidic saponin from Vaccaria segetalis (Neck) with reported anticancer activities. This development has raised an interest in the therapeutic potential of segetoside I. Here, we report the in vitro and in vivo antitumor activities of segetoside I against some selected cancer cell lines (HepG2, human hepatoma; H22, mouse hepatoma; MCF-7, breast cancer; U251, gliocoma; BGC, HGC & SGC, gastric cancinoma; Lovo-1,colon cancer). MTT bioassay analysis showed that HepG2 cells were the most sensitive to segetoside I compared with other cancer cell lines, with lower toxicity in healthy mouse embryonic fibroblast cells. Segetoside I pretreatment of HepG2 resulted in apoptotic induction, dose-dependent DNA fragmentation, inhibition of cell migration, up-regulation of Bax and down-regulation of Bcl-2, which indicated that an apoptotic signaling event could have been initiated. The segetoside I also suppressed hepato-tumour growth in mice with virtually no cytotoxicity and prolonged animal survival, making it a strong oncology drug agent. These findings showed that segetoside I exhibited its antitumor activity via apoptotic induction and significantly support the possible application of the antitumor agent as a potential chemotherapeutic candidate worthy of further investigations.

摘要

獐牙菜苦苷 I 是一种从獐牙菜(Neck)中提取的植物源性双糖苷甾体皂甙,具有抗癌活性。这一发现引起了人们对獐牙菜苦苷 I 治疗潜力的兴趣。在这里,我们报告了獐牙菜苦苷 I 对一些选定的癌细胞系(HepG2,人肝癌;H22,鼠肝癌;MCF-7,乳腺癌;U251,神经胶质瘤;BGC、HGC 和 SGC,胃癌;Lovo-1,结肠癌)的体外和体内抗肿瘤活性。MTT 生物测定分析表明,与其他癌细胞系相比,HepG2 细胞对獐牙菜苦苷 I 最敏感,而对健康的小鼠胚胎成纤维细胞的毒性较低。獐牙菜苦苷 I 预处理 HepG2 导致细胞凋亡诱导、剂量依赖性 DNA 片段化、细胞迁移抑制、Bax 上调和 Bcl-2 下调,这表明可能已经启动了凋亡信号事件。獐牙菜苦苷 I 还抑制了荷瘤小鼠的肝肿瘤生长,几乎没有细胞毒性,并延长了动物的存活时间,使其成为一种强大的肿瘤药物。这些发现表明,獐牙菜苦苷 I 通过诱导细胞凋亡发挥其抗肿瘤活性,并为该抗肿瘤药物作为一种有潜力的化疗候选药物的可能应用提供了有力支持,值得进一步研究。

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