Three Minor Diterpenoids with Three Carbon Skeletons from Euphorbia peplus
Three Minor Diterpenoids with Three Carbon Skeletons from Euphorbia peplus
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大戟中具有三个碳骨架的三种次要二萜
DOI：
10.1021/acs.orglett.6b00787
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发表时间：
2016-05-06
期刊：
影响因子：
5.2
通讯作者：
Qiu, Ming-Hua
中科院分区：
文献类型：
--
作者：
Wan, Luo-Sheng;Nian, Yin;Qiu, Ming-Hua
大戟在传统医学中被用于治疗哮喘和牛皮癣。从该植物中分离并鉴定了三个高度修饰的二萜类化合物，即pepluacetal（1）和pepluanol A-B（2-3）。化合物1-3分别表现出前所未有的5/4/7/3、5/6/7/3和5/5/8/3环系统。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对新化合物的反应。所有三种化合物都抑制Kv1.3，其中化合物3最有效，IC 50值为9.50 μ m。
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 mu m.