title: Three Minor Diterpenoids with Three Carbon Skeletons from Euphorbia peplus.
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.
authors.affiliation: 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.
authors.forename: Luo-Sheng
authors.initials: LS
authors.lastname: Wan
authors.affiliation: 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.
authors.forename: Yin
authors.initials: Y
authors.lastname: Nian
authors.affiliation: 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.
authors.forename: Chen-Jun
authors.initials: CJ
authors.lastname: Ye
authors.affiliation: 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.
authors.forename: Li-Dong
authors.initials: LD
authors.lastname: Shao
authors.affiliation: 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.
authors.forename: Xing-Rong
authors.initials: XR
authors.lastname: Peng
authors.affiliation: 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.
authors.forename: Chang-An
authors.initials: CA
authors.lastname: Geng
authors.affiliation: 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.
authors.forename: Zhi-Li
authors.initials: ZL
authors.lastname: Zuo
authors.affiliation: 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.
authors.forename: Xiao-Nian
authors.initials: XN
authors.lastname: Li
authors.affiliation: 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.|Department of Biological Sciences, Columbia University , New York, New York 10027, United States.
authors.forename: Jian
authors.initials: J
authors.lastname: Yang
authors.affiliation: 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.|Verna and Marrs McLean Department of Biochemistry and Molecular Biology, Baylor College of Medicine , Houston, Texas 77030, United States.
authors.forename: Ming
authors.initials: M
authors.lastname: Zhou
authors.affiliation: 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.
authors.forename: Ming-Hua
authors.initials: MH
authors.lastname: Qiu
mesh_terms: D018360:Crystallography, X-Ray; D004224:Diterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D028481:Euphorbia / Q000737:chemistry*; D006801:Humans; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors* / Q000378:metabolism; D008958:Models, Molecular; D008968:Molecular Conformation; D026902:Potassium Channel Blockers / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D004224:Diterpenes; D051664:Kv1.3 Potassium Channel; D026902:Potassium Channel Blockers