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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anti-cancer activity studies of dammarane-type triterpenoid derivatives
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Synthesis and anti-cancer activity studies of dammarane-type triterpenoid derivatives

机译：达米甲烷型三萜类衍生物的合成与抗癌活性研究

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摘要

Two series of novel derivatives of AD-2, an active ginsenoside derived from ginseng were designed and synthesized. Five human cancer cell lines (MGC-803, SGC-7901, A549, MCF-7, PC-3 cells) and one normal ovarian cell IOSE144 were employed to evaluate the anti-proliferative activity. Most of derivatives possessed obvious enhanced activity compared with AD-2. Among them, compound 4c displayed the most excellent activity in all tested cancer cell lines, especially A549 cells with an IC50 value of 1.07 +/- 0.05 mu M. The underlying mechanism study suggested that 4c induced S-phase arrest and apoptosis in A549 cells. Increasing the level of ROS and inducing collapse of MMP in cells treated with 4c were also proved. Moreover, Western blot analysis showed that the expression level of p53 and p21 were obviously increased. 4c could remarkably up-regulate the expression of cyt c in cytosol, the ratio of Bax to Bcl-2 and activate caspase-3/9/PARP. Besides, the expression level of MDM2 was remarkably decreased. The results indicated that 4c caused apoptosis through the mitochondrial pathway, which ROS generation was probably involved in, and had the potent to serve as anti-proliferative agent. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：设计和合成了两种ad-2的三种新衍生物，是衍生自人参的活跃的人参皂苷。使用5个人癌细胞系（MgC-803，SGC-7901，A549，MCF-7，PC-3细胞）和一个正常卵巢细胞IOSE144来评估抗增殖活性。与AD-2相比，大多数衍生物具有明显的增强活动。其中，化合物4C在所有测试的癌细胞系中显示出最优异的活性，特别是A549细胞，IC50值为1.07 +/- 0.05 mu M.潜在的机制研究表明，4C诱导的S相停滞和凋亡在A549细胞中。还证明了增加ROS水平并诱导用4C处理的细胞中MMP的塌陷。此外，Western印迹分析表明，P53和P21的表达水平明显增加。 4C可以显着上调CytO醇的Cyt C的表达，BCL-2的比例与BCL-2和活化胱天冬酶-3 / 9 / PARP。此外，MDM2的表达水平显着降低。结果表明，4C引起通过线粒体途径引起的细胞凋亡，该途径可能参与其中，并且具有效力作为抗增殖剂。 （c）2019年Elsevier Masson SAS。版权所有。

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