| Literature DB >> 27075046 |
Luo-Sheng Wan1, Yin Nian2, Chen-Jun Ye2, Li-Dong Shao1, Xing-Rong Peng1, Chang-An Geng1, Zhi-Li Zuo1, Xiao-Nian Li1, Jian Yang2,3, Ming Zhou2,4, Ming-Hua Qiu1.
Abstract
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.Entities:
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Year: 2016 PMID: 27075046 DOI: 10.1021/acs.orglett.6b00787
Source DB: PubMed Journal: Org Lett ISSN: 1523-7052 Impact factor: 6.005