Journal
ORGANIC LETTERS
Volume 18, Issue 9, Pages 2166-2169Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.6b00787
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Funding
- National Natural Science Foundation of China [81403050, 31370821]
- High-Level Overseas Talents of Yunnan Province
- NSFC-Joint Foundation of Yunnan Province [U1132604]
- Top Talents Program of Yunnan Province [2011HA012]
- key medicinal project of Yunnan Province [2015ZJ002]
- state key project 973 from the MOST of the P. R. China [2014CB910300]
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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.
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