Cytotoxicity and Anti-inflammatory Properties of Apigenin-Derived Isolaxifolin
Cytotoxicity and Anti-inflammatory Properties of Apigenin-Derived Isolaxifolin
复制标题
芹菜素衍生的异茄叶甙的细胞毒性和抗炎特性
DOI：
10.1021/acs.jnatprod.9b00113
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发表时间：
2019-09-01
影响因子：
5.1
通讯作者：
Lan, Ping
中科院分区：
文献类型：
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作者：
Chen, Yongsheng;Chen, Wan-Na;Lan, Ping
稀有的黄酮类异恶福林是一种有效的杀虫剂，被吹捧为潜在的谷物保护剂。为了评估这种天然产物对人类健康的任何影响，并探索其各种其他生物学性质，我们从结构上更简单、含量更丰富的天然产物芹菜素中建立了半合成方法。五步反应序列首次为深入评价标题天然产物的细胞毒性性质提供了足够的材料。还检测了异恶福林对小鼠巨噬细胞RAW 264.7细胞中某些促炎细胞因子的影响。这类研究表明，异恶福林对正常细胞没有毒性作用，而对某些癌细胞株的细胞毒作用强于其合成前体芹菜素。此外，与芹菜素不同的是，异烟福林仅以一种相当温和且剂量无关的方式减少了脂多糖诱导的RAW 264.7细胞中NO、肿瘤坏死因子-α和IL-6的分泌。
The rare flavonoid isolaxifolin, a potent insecticide, has been touted as a potential grain-protecting agent. In order to assess any impact of this natural product on human health and to explore its various other biological properties, we have established a semisynthesis from the simpler but structurally related and more abundant natural product apigenin. The five-step reaction sequence has provided, for the first time, sufficient material for an in-depth evaluation of the cytotoxic properties of the title natural product. The impact of isolaxifolin on certain pro-inflammatory cytokines in murine macrophage RAW 264.7 cells has also been examined. Such studies have revealed that isolaxifolin displays no toxic effects toward normal cells while displaying greater cytotoxicities against certain cancer cell lines than its synthetic precursor apigenin. Furthermore, unlike apigenin, isolaxifolin only reduced NO, TNF-alpha, and IL-6 secretions in LPS-induced RAW 264.7 cells in a rather modest and dose-independent manner.