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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Fangchinoline derivatives induce cell cycle arrest and apoptosis in human leukemia cell lines via suppression of the PI3K/AKT and MAPK signaling pathway
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Fangchinoline derivatives induce cell cycle arrest and apoptosis in human leukemia cell lines via suppression of the PI3K/AKT and MAPK signaling pathway

机译：芳樟醇衍生物通过抑制PI3K / AKT和MAPK信号通路诱导人白血病细胞系中的细胞周期停滞和细胞凋亡

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摘要

Fangchinoline, a bisbenzylisoquinoline alkaloid extracted from Stephania tetrandra S. Moore, is known to exert anti-cancer activity. A series of new fangchinoline derivatives have been synthesized and evaluated for their anti-cancer activity. In cell viability assay, these fangchinoline derivatives displayed higher proliferation inhibitory activity on leukemia and breast cancer cell lines than the parental compound. Among them, 3e exhibited strongest cell growth inhibitory activity in a dose- and time-dependent manner on leukemia cell line HEL through induction of G0/G1 cell cycle arrest and apoptosis. Treatment of HEL cells with 3e also resulted in significant suppression of the MAPK and PI3K/AKT pathway as well as c-MYC downregulation, which may responsible for induction of apoptosis and cell cycle arrest. In docking analysis, high affinity interaction between 3e and Aktl was responsible for drastic kinase inhibition by the compound. This derivative compound may be useful as a potent anti-cancer agent for treatment of leukemia. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：从Stephania Tetrandra S. Moore提取的双苄基异喹啉生物碱，已知从Stephania Tetrandra S. Moore中提取的芳香素碱。已经合成了一系列新的芳藻胺衍生物，并评估其抗癌活动。在细胞活力测定中，这些芳香碱衍生物在白血病和乳腺癌细胞系上显示出比亲本化合物更高的增殖抑制活性。其中，通过诱导G0 / G1细胞循环骤停和凋亡，在白血病细胞系HeL上以剂量和时间依赖性方式表现出最强的细胞生长抑制活性。 Hel细胞的HE1细胞的处理也导致MAPK和PI3K / AKT途径以及C-MYC下调，这可能负责诱导细胞凋亡和细胞周期骤停。在对接分析中，3E和AKT1之间的高亲和力相互作用负责化合物的激烈激酶抑制。该衍生物化合物可用作治疗白血病的有效抗癌剂。 （c）2019年Elsevier Masson SAS。版权所有。

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