State Key Laboratory of Medicinal Chemical Biology, College of Pharmacy, and Tianjin Key Laboratory of Molecular Drug Research, Nankai University, Tianjin 300050, People's Republic of China.
School of Medicine, Nankai University, Tianjin 300071, People's Republic of China.
Bioorg Chem. 2020 Nov;104:104331. doi: 10.1016/j.bioorg.2020.104331. Epub 2020 Oct 1.
Inflammation, especially chronic inflammation, has been found to be closely related to the pathology of many diseases and the discovery of bioactive natural products to inhibit NO production is one of strategies to treat inflammation. In our continuous search for bioactive natural substances as potential anti-inflammatory agents, five new compounds (1-5) were extracted and purified from Patrinia heterophylla. The NMR and MS data analysis, along with electronic circular dichroism (ECD) calculations, led to the identification of these isolates, which were new iridoids. Using cell and zebrafish models, the in vitro and in vivo anti-inflammatory effects were conducted to evaluate the potency of anti-inflammation of these compounds. The preliminary mechanism was explored using molecular docking and Western blotting experiments.
炎症，尤其是慢性炎症，与许多疾病的病理学密切相关，发现具有抑制 NO 产生的生物活性天然产物是治疗炎症的策略之一。在我们不断寻找生物活性天然物质作为潜在抗炎剂的过程中，从苦菜中提取和纯化了五种新化合物（1-5）。通过 NMR 和 MS 数据分析以及电子圆二色性（ECD）计算，确定了这些分离物为新的环烯醚萜类化合物。利用细胞和斑马鱼模型，进行了体外和体内抗炎作用评估，以评价这些化合物的抗炎效力。通过分子对接和 Western blot 实验探讨了初步的作用机制。
