Synthesis and in vitro inhibitory activity of matrine derivatives towards pro-inflammatory cytokines
Synthesis and in vitro inhibitory activity of matrine derivatives towards pro-inflammatory cytokines
复制标题
苦参碱衍生物的合成及其对促炎细胞因子的体外抑制活性。
DOI：
10.1016/j.bmcl.2010.09.075
复制
发表时间：
2010-12-15
影响因子：
2.7
通讯作者：
Wu, Qiuye
中科院分区：
文献类型：
--
作者：
Hu, Honggang;Wang, Shaozhan;Wu, Qiuye
苦参碱是一种苦参生物碱，在我们以前的报告中显示了良好的抗炎作用。本研究通过经典的Michael加成反应合成了一系列苦参碱衍生物。生物学研究表明，合成的衍生物对肿瘤坏死因子-α的产生和核因子-kappaB的转录活性均有良好的抑制作用。在酮基上引入不同的氨基可以改善生化图谱，从而鉴定出比苦参碱和苦参碱具有更高抑制活性的更有效的衍生物，如1f。(C)2010年由爱思唯尔有限公司出版。
Matrine, a sophora alkaloid, exhibited good anti-inflammation effects in our previous report. In the present study, a series of matrine derivatives were synthesized via classical Michael addition. Biological studies showed that the synthetic derivatives had good inhibitory effect towards TNF-alpha production and NF kappa B transcriptional activity. The introduction of various amino groups to the keto beta position could improve the biochemical profile, resulting in the identification of more potent derivates, such as 1f, with higher inhibitory activity than both matrine and sophoramine. (C) 2010 Published by Elsevier Ltd.