School of Traditional Chinese Materia Medica, Key Laboratory of Computational Chemistry-Based Natural Antitumor Drug, Shenyang Pharmaceutical University, Wenhua Road 103, Shenyang 110016, PR China.
College of Life and Health Sciences, Northeastern University, Shenyang 110819, PR China.
Bioorg Chem. 2020 Apr;97:103715. doi: 10.1016/j.bioorg.2020.103715. Epub 2020 Feb 28.
Neuroinflammation are involved in the pathogenesis of many neurodegenerative disorders. In our screening of natural effective neuroinflammatory inhibitors from natural products, stilbenes, such as resveratrol and its analogues, have received considerable attention over the last several decades as anti-neuroinflammatory agents. Then, Bletilla striata attracted our attention due to its abundant stilbenes portion, PE fraction. So, three new stilbenes: dusuanlansin E1 (23a), dusuanlansin E2 (23b), 3-hydroxy-5-methoxybibenzyl-3'-O-β-d-glucopyranoside (27), and 30 known stilbene compounds were isolated from B. striata. These structures of the compounds were established on the basis of extensive spectroscopic analysis including 1D and 2D NMR and circular dichroism (CD) data. Furthermore, all the isolated components were tested in vitro for their inhibitory effects on the nitric oxide generation in LPS-stimulated BV2 cells. As a result, compounds 2, 5, 6, 16, 17 can greatly inhibit the NO production without cytotoxicity. In addition, SARs between stilbenes and anti-neuroinflammation effects were discussed briefly. In conclusion, stilbenes were characteristic constituents of the tubers of B. striata with potential anti- neuroinflammatory effects.
神经炎症参与了许多神经退行性疾病的发病机制。在我们从天然产物中筛选天然有效的神经炎症抑制剂的过程中,过去几十年间,白藜芦醇及其类似物等芪类化合物作为抗神经炎症药物受到了相当多的关注。然后,由于白及中富含芪类成分的 PE 部分,白及引起了我们的注意。因此,我们从白及中分离得到了三个新的芪类化合物:独蒜兰素 E1(23a)、独蒜兰素 E2(23b)、3-羟基-5-甲氧基联苯-3'-O-β-D-吡喃葡萄糖苷(27)和 30 种已知的芪类化合物。这些化合物的结构是基于广泛的光谱分析建立的,包括 1D 和 2D NMR 和圆二色性(CD)数据。此外,所有分离得到的成分都在体外进行了测试,以检测它们对 LPS 刺激的 BV2 细胞中一氧化氮生成的抑制作用。结果表明,化合物 2、5、6、16、17 可以在没有细胞毒性的情况下极大地抑制 NO 的产生。此外,还简要讨论了芪类化合物与抗神经炎症作用之间的构效关系。总之,芪类化合物是白及块茎的特征成分,具有潜在的抗神经炎症作用。