Kapche Deccaux W F G, Lekane Nadège M, Kulabas Seda S, Ipek Hande, Tok Tugba T, Ngadjui Bonaventure T, Demirtas Ibrahim, Tumer Tugba B
University of Yaoundé I, P. O. Box +(237) 47, Yaoundé, Cameroon; Çankırı Karatekin University, Faculty of Sciences, Department of Chemistry, 18200, Çankırı, Turkey.
Department of Organic Chemistry, Faculty of Science, University of Yaoundé I, P. O. Box +(237) 812, Yaoundé, Cameroon.
Phytochemistry. 2017 Sep;141:70-79. doi: 10.1016/j.phytochem.2017.05.007. Epub 2017 Jun 1.
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-1β release, mRNA expressions of IL-1β and COX-2 at low doses. These results suggest that dinklagein A can be developed as natural, multi-target agent against several inflammatory diseases.
丁氏豆茶决明（豆科）是一种热带药用树，原产于西非。对这种来自其茎皮的本地植物物种进行的植物化学研究已导致分离出两种先前未描述的芳基苯并呋喃衍生物，命名为丁氏豆茶决明素A和B，以及八种已知化合物。通过使用广泛的光谱方法（红外光谱、高分辨电子轰击质谱以及一维和二维核磁共振）阐明了它们的化学结构。在所有分离物中，丁氏豆茶决明素A对脂多糖（LPS）诱导的RAW264.7巨噬细胞中一氧化氮（NO）的产生显示出显著的抑制活性。对诱导型一氧化氮合酶（iNOS）和先前未描述的化合物（丁氏豆茶决明素A和B）的构效关系及分子对接研究支持了实验数据。此外，丁氏豆茶决明素A在mRNA和蛋白质水平上均剂量依赖性地抑制LPS刺激的iNOS表达。它在低剂量时还减弱了白细胞介素-1β（IL-1β）的释放、IL-1β和环氧化酶-2（COX-2）的mRNA表达。这些结果表明，丁氏豆茶决明素A可被开发成一种针对多种炎症性疾病的天然多靶点药物。
