Synthesis and Evaluation of Cytotoxicity and Inhibitory Effect on Nitric Oxide Production by J774A.1 Macrophages of New Anthraquinone Derivatives
作者:Caio Cesar Alves、Cristiane F. Costa、Sandra B. R. Castro、Tais Correa、Gabriele Santiago、Renata Diniz、Ana Ferreira、Mauro De Almeida
DOI:10.2174/1573406411309060005
日期:2013.7.1
Mitoxantrone is an anthracene-based anticancer agent whose efficacy in treating autoimmune diseases is believed
to be due to cytotoxicity and inhibition of proliferation of cells. Several novel anthraquinone derivatives, analogs of
mitoxantrone, were designed and synthesized. Lipophilic and functionalized mitoxantrone analogs were prepared by a
simple methodology and the cytotoxicity and the inhibitory effect on nitric oxide release of these compounds were demonstrated
in vitro on J774A.1 macrophages. Interestingly compounds 3, 4, 5, 6, 7, and 8 exhibited reduction in NO release
(62.4%, 92.6%, 73.4%, 58.4%, 57.8% and 53.4%, respectively) in comparison to NG-n-methyl-arginine treated control,
without cytotoxicity. In conclusion, anthraquinone derivatives were prepared in a good yield and showed promissory antiinflammatory
properties.
米托蒽醌是一种基于蒽的抗癌药物,其治疗自身免疫性疾病的功效被认为
是由于细胞毒性和抑制细胞增殖所致。几种新型蒽醌衍生物、类似物
设计并合成了米托蒽醌。亲脂性和功能化的米托蒽醌类似物是通过
方法简单,并且证明了这些化合物的细胞毒性和对一氧化氮释放的抑制作用
体外 J774A.1 巨噬细胞。有趣的是,化合物 3、4、5、6、7 和 8 表现出 NO 释放减少
与 NG-n-甲基-精氨酸处理的对照相比(分别为 62.4%、92.6%、73.4%、58.4%、57.8% 和 53.4%),
无细胞毒性。总之,以良好的产率制备了蒽醌衍生物,并显示出良好的抗炎作用
特性。