European Journal of Medicinal Chemistry, 2013, 9(6):812-8.

Synthesis of genistein coupled with sugar derivatives and their inhibitory effect on nitric oxide production in macrophages

Caio Cesar S Alves, Cristiane F Da Costa, Sandra B R De Castro, et al

Department of Parasitology, Microbiology and Immunology, Federal University of Juiz de Fora, Juiz de Fora, Brazil; et al

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.

法国《欧洲药物化学杂志》，2014年9月

金雀异黄素耦合糖类衍生物的制备及其在巨噬细胞中对一氧化氮产物的抑制作用

卡伊奥 塞萨尔 S 阿尔维斯，克莉斯婷 F 达 科斯塔，桑德拉 B R 德卡斯特罗，等

巴西迪福联邦大学寄生虫学、 微生物学和免疫学学院等

米托蒽醌是一种蒽环类抗癌药物，其治疗自身免疫性疾病的疗效被认为是由于细胞毒性和对细胞增殖的抑制作用。设计并合成了几种新型蒽醌类衍生物，米托蒽醌的同构异形体。通过一种简单的方法制备了亲脂性和官能团化米托蒽醌类似物，并在体外测试这些化合物对巨噬细胞 J774A.1的细胞毒性和对一氧化氮释放的抑制作用。有趣的是与NG-n-甲基-精氨酸治疗对照相比，化合物 3、 4、 5、 6、 7和 8 表现出NO释放减少 (分别为62.4%、 92.6%、 73.4%、 58.4%、 57.8%和 53.4%)，无细胞毒性。总之，制备出产量较好的蒽醌衍生物，并表现出承诺的抗炎性能。