Three Minor Diterpenoids with Three Carbon Skeletons from Euphorbia peplus

• DOI: 10.1021/acs.orglett.6b00787
• Publication Date: 2016-04-14T16:02:29Z
• Authors: Luo-Sheng Wan; Yin Nian; Chen-Jun Ye; Li-Dong Shao; Xing-Rong Peng; Chang-An Geng; Zhi-Li Zuo; Xiao-Nian Li; Jian Yang; Ming Zhou; Ming-Hua Qiu
• Keywords: Minor (academic); Euphorbiaceae; Carbon skeleton; Euphorbia

Euphorbia peplus has been used in traditional medicine to treat asthma and psoriasis. Three highly modified diterpenoids, namely, pepluacetal (1) pepluanol A-B (2-3), have isolated identified from this plant. Compounds 1-3 exhibit unprecedented 5/4/7/3, 5/6/7/3, 5/5/8/3 ring systems, respectively. Their structures with absolute configurations were determined by spectroscopic analyses, X-ray crystallography, 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, psoriasis, was studied terms its response new compounds. All three compounds inhibit Kv1.3, compound 3 being most effective an IC50 value 9.50 μM.