Aryl benzofuran derivatives from the stem bark of Calpocalyx dinklagei attenuate inflammation
Aryl benzofuran derivatives from the stem bark of Calpocalyx dinklagei attenuate inflammation
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DOI：
10.1016/j.phytochem.2017.05.007
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发表时间：
2017-09-01
期刊：
影响因子：
3.8
通讯作者：
Tumer, Tugba B.
中科院分区：
文献类型：
--
作者：
Kapche, Deccaux W. F. G.;Lekane, Nadege M.;Tumer, Tugba B.
Calpocalyx dinklagei Harms（豆科）是一种热带药用树，原产于西非。对这种当地植物的茎皮进行植物化学研究，分离出两种以前未描述过的芳基苯并呋喃衍生物，命名为丁克拉金A和B，以及八种已知化合物。利用红外光谱、高分辨质谱、核磁共振等波谱学方法对化合物的结构进行了鉴定。在所有的分离物中，丁克拉格因A对脂多糖（LPS）诱导的RAW 264.7巨噬细胞中一氧化氮（NO）的产生显示出显著的抑制活性。对iNOS和以前未描述的化合物（丁克拉吉因A和B）的SAR和分子对接研究支持实验数据。此外，Dinklagein A在mRNA和蛋白水平上剂量依赖性地抑制LPS刺激的iNOS表达。在低剂量下，它还减弱了IL-1 β的释放、IL-1 β和考克斯-2的mRNA表达。这些结果表明，Dinklagein A可以开发为天然的，多靶点的药物，用于治疗多种炎症性疾病。(C)2017爱思唯尔有限公司版权所有
Calpocalyx dinklagei Harms (Fabaceae) is a tropical medicinal tree, which is indigenous to Western Africa. A phytochemical study of this local plant species from its stem bark has led to the isolation of two previously undescribed aryl benzofuran derivatives, named dinklagein A and B, together with eight known compounds. Their chemical structures were elucidated by use of extensive spectroscopic methods (IR, HREI-MS and 1D and 2D NMR). Among all isolates, dinklagein A displayed remarkably potent inhibitory activity against the production of nitric oxide (NO) in the lipopolysaccharide (LPS) induced RAW264.7 macrophages. SAR and molecular docking investigations on iNOS and previously undescribed compounds (dinklagein A and B) supported experimental data. Furthermore, dinklagein A dose dependently suppressed the LPS-stimulated iNOS expression at both mRNA and protein level. It also attenuated IL-1 beta release, mRNA expressions of IL-1 beta and COX-2 at low doses. These results suggest that dinklagein A can be developed as natural, multi-target agent against several inflammatory diseases. (C) 2017 Elsevier Ltd. All rights reserved.