Synthesis and anti-metastatic effects of novel chiral ionone alkaloid derivatives
Synthesis and anti-metastatic effects of novel chiral ionone alkaloid derivatives
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DOI：
10.1016/j.ejmech.2015.06.037
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发表时间：
2015-08-28
影响因子：
6.7
通讯作者：
Qin, Nan
中科院分区：
文献类型：
--
作者：
Fang, Hai-Jun;Shou, Xiao-Ai;Qin, Nan
合成了一种新的手性离子生物碱衍生物，并评价了其在人MDA-MB-231乳腺癌细胞中的抗转移作用。衍生物的手性中心C-6在抗转移活性中发挥了重要作用。与阳性对照LY294002相比，化合物17b和19a对egf诱导的MDA-MB-231细胞侵袭表现出较强的抑制作用，IC50值分别为0.026 +/- 0.003和0.016 +/- 0.002 μ M。此外，化合物17b和19a对MDA-MB-231细胞中p-PKC zeta和p-整合素β 1的表达呈剂量依赖性抑制作用。因此，化合物17b和19a具有开发新型抗转移药物的潜力。(C) 2015 Elsevier Masson SAS。版权所有。
Novel chiral ionone alkaloid derivatives were synthesized and evaluated their anti-metastatic effects in human MDA-MB-231 breast cancer cells. The chiral center C-6 of derivatives exerted an important role in response to the anti-metastatic activity. Comparing with a positive control of LY294002, compounds 17b and 19a exhibited potent inhibitory effects on the EGF-induced invasion of MDA-MB-231 cells with IC50 values of 0.026 +/- 0.003 and 0.016 +/- 0.002 mu M, respectively. Moreover, compounds 17b and 19a showed inhibitory effects on the expressions of p-PKC zeta and p-integrin beta 1 in MDA-MB-231 cells in a dose-dependent manner. Thus, compounds 17b and 19a offer potential to be developed as novel anti-metastasis agents. (C) 2015 Elsevier Masson SAS. All rights reserved.