Biological activities of novel derivatives of DIF-1 isolated from Dictyostelium
Biological activities of novel derivatives of DIF-1 isolated from Dictyostelium
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DOI：
10.1016/j.bbrc.2008.10.105
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发表时间：
2008-12-19
影响因子：
3.1
通讯作者：
Kubohara, Yuzuru
中科院分区：
文献类型：
--
作者：
Kikuchi, Haruhisa;Ishiko, Shinya;Kubohara, Yuzuru
分化诱导因子-1（DIF-1）是一种亲脂性信号分子（氯化烷基苯酮），可诱导细胞黏菌盘状网柄菌柄细胞分化。此外，DIF-1及其衍生物在体外哺乳动物细胞中显示出具有抗白血病活性和葡萄糖消耗促进活性。本研究为了评价DIF-1的化学构效关系，我们合成了8个DIF-1衍生物，并研究了它们在Dictyosteoplasty细胞中的柄细胞诱导活性和在哺乳动物细胞中的药理活性。在衍生物中，DIF-1的两个酰胺衍生物，其疏水指数接近于DIF-1的疏水指数。诱导柄细胞分化的DIF-1一样强烈的Dictyosteoblastoma细胞。还发现某些衍生物抑制人K562白血病细胞的生长，促进小鼠3 T3-L1细胞的葡萄糖消耗。这些结果为LIS提供了关于DIF-1的化学结构-效应关系的有价值的信息。(C)2008年爱思唯尔公司All rights reserved.
The differentiation-inducing factor-1 (DIF-1) is a lipophilic signal molecule (chlorinated alkylphenone) that induces stalk cell differentiation in the cellular slime mold Dictyostelium discoideum. in addition, DIF-1 and its derivatives have been shown to possess anti-leukemic activity and glucose Consumption-promoting activity in vitro in mammalian cells. In this study. to assess the chemical structure-effect relationship of DIF-1, we synthesized eight derivatives of DIF-1 and investigated their stalk cell-inducing activity in Dictyostelium cells and pharmacological activities in mammalian cells. Of the derivatives, two amide derivatives of DIF-1, whose hydrophobic indexes are close to that of DIF-1. induced stalk cell differentiation as strongly as DIF-1 in Dictyostelium cells. It Was also found that some derivatives Suppressed cell growth in human K562 leukemia cells and promoted glucose consumption in mouse 3T3-L1 cells. These results give LIS valuable information as to the chemical structure-effect relationship of DIF-1. (C) 2008 Elsevier Inc. All rights reserved.