Abstract

Juncus effusus L. (J. effusus) is a Traditional Chinese Medicine (TCM) that has long been used for dealing with gynaecological disorders, such as relieving insomnia, preventing tinnitus, reducing edema with diuretic effect. In our course of evidence-based medical research focused on this herb, one new phenanthrene, Junfusol B (2), together with seventeen known compounds were isolated and identified. All the structures of these compounds were elucidated by spectroscopic methods. The absolute stereochemistry of compounds 1 and 2 was further determined by comparing their calculated and experimental Electronic Circular Dichroism (ECD) spectra and optical rotation (OR) values. The isolates were evaluated for their estrogenic and anti-inflammatory activities which were considered as relevant etiological factors of insomnia, tinnitus and edema in the ancient TCM theory. The results revealed that most of the obtained phenanthrenes in this work were found exerting agonistic effects on estrogen receptor. This is the first report to declare the exact estrogen-regulating potential among this type of compounds from J. effusus. Moreover, phenanthrenes 3 − 7 exhibited significant inhibitions on superoxide anion generation and elastase release in fMLP/CB-induced human neutrophilic inflammation model. J. effusus may be developed as a complementary agent utilized in menopausal multiple syndromes.

摘要

Juncus effusus L. ( J. effusus ) 是一种中药 (TCM)，长期以来一直用于治疗妇科疾病，如缓解失眠、预防耳鸣、减轻水肿并具有利尿作用。在我们以这种草药为重点的循证医学研究过程中，分离和鉴定了一种新的菲，君富索 B ( 2 ) 以及 17 种已知化合物。这些化合物的所有结构均通过光谱方法进行了阐明。化合物1和2的绝对立体化学通过比较他们的计算和实验电子圆二色性（ECD）光谱和旋光度（OR）值进一步确定。对分离物的雌激素和抗炎活性进行了评价，这些活性在古代中医理论中被认为是失眠、耳鸣和水肿的相关病因。结果表明，在这项工作中获得的大部分菲被发现对雌激素受体具有激动作用。这是第一份在J. effusus的这类化合物中宣布确切的雌激素调节潜力的报告。此外，菲3  -  7在 fMLP/CB 诱导的人中性粒细胞炎症模型中，对超氧阴离子的产生和弹性蛋白酶的释放表现出显着的抑制作用。J. effusus可开发为用于更年期多发性综合征的补充剂。