State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences , 132 Lanhei Road, Kunming 650201, P. R. China.
Key Laboratory of Animal Models and Human Diease Mechanisms, and Ion Channel Research and Drug Development Center, Kunming Institute of Zoology, Chinese Academy of Sciences , Kunming 650223, P. R. China.
Org Lett. 2016 May 6;18(9):2166-9. doi: 10.1021/acs.orglett.6b00787. Epub 2016 Apr 14.
Euphorbia peplus has been used in traditional medicine to treat asthma and psoriasis. Three highly modified diterpenoids, namely, pepluacetal (1) and pepluanol A-B (2-3), have been isolated and identified from this plant. Compounds 1-3 exhibit unprecedented 5/4/7/3, 5/6/7/3, and 5/5/8/3 ring systems, respectively. Their structures with absolute configurations were determined by spectroscopic analyses, X-ray crystallography, and electronic circular dichroism calculations. Since Kv1.3 is a validated target for the treatment of autoimmune diseases, such as multiple sclerosis, type-1 diabetes, asthma, and psoriasis, Kv1.3 was studied in terms of its response to the new compounds. All three compounds inhibit Kv1.3, with compound 3 being the most effective with an IC50 value of 9.50 μM.
绵毛大戟被用于传统医学中以治疗哮喘和银屑病。从这种植物中分离并鉴定出三种高度修饰的二萜类化合物，分别为绵毛醇 A-B（2-3）和绵毛醇 A-B（1）。化合物 1-3 分别呈现出前所未有的 5/4/7/3、5/6/7/3 和 5/5/8/3 环系。通过光谱分析、X 射线晶体学和电子圆二色性计算确定了它们的结构和绝对构型。由于 Kv1.3 是治疗自身免疫性疾病（如多发性硬化症、1 型糖尿病、哮喘和银屑病）的有效靶点，因此研究了 Kv1.3 对这些新化合物的反应。这三种化合物均抑制 Kv1.3，其中化合物 3 的抑制作用最强，IC50 值为 9.50 μM。
