The Key Laboratory of Chinese Medicine Research and Development in Hebei Province, Traditional Chinese Medicine Institute, Chengde Medical University, Chengde 067000, China.
Experiment Center for Science and Technology, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai 201203, China.
Molecules. 2024 Aug 10;29(16):3799. doi: 10.3390/molecules29163799.
Allergies are one of the diseases whose incidence rates have increased in recent years due to the greenhouse effect and extreme climate change. Therefore, the development of new antiallergic drugs has attracted the interest of researchers in chemistry and pharmacy fields. Dicoumarin is a coumarin derivative with various biological activities, but its antiallergic activity has not been evaluated. In this study, 14 different dicoumarin derivatives were synthesized by diethylamine-catalyzed condensation reactions of 4-hydroxycoumarin with 14 different aldehydes, and they were identified on the basis of their spectral data. The dicoumarin derivatives were subjected to studies on the degranulation of rat basophilic leukemia cells (RBL-2H3 cells) and mouse bone-marrow-derived mast cells (mBMMCs), and some of them showed good inhibitory effects on the degranulation of the two types of mast cells, demonstrating their good antiallergic activity. This study presents a new method of developing new antiallergic drugs.
过敏是近年来由于温室效应和极端气候变化导致发病率上升的疾病之一。因此，新型抗过敏药物的开发引起了化学和药学领域研究人员的兴趣。二苯并吡喃酮是一种具有多种生物活性的香豆素衍生物，但它的抗过敏活性尚未得到评估。在这项研究中，通过 4-羟基香豆素与 14 种不同的醛在二乙胺催化缩合反应中合成了 14 种不同的二苯并吡喃酮衍生物，并根据其光谱数据进行了鉴定。对二苯并吡喃酮衍生物进行了大鼠嗜碱性白血病细胞 (RBL-2H3 细胞) 和鼠骨髓来源肥大细胞 (mBMMCs) 的脱颗粒研究，其中一些对两种类型的肥大细胞的脱颗粒具有良好的抑制作用，表明它们具有良好的抗过敏活性。这项研究提出了开发新型抗过敏药物的新方法。
