Antinociceptive grayanane-derived diterpenoids from flowers of Rhododendron molle

• 作者: Jing Qu Li Li Shishan Yu Shuanggang Ma Yong Li Yunbao Liu Yuxun Zhu Zhaoxin Zhang
• 来源期刊: 药学学报（英文版）
• 年，卷（期）: 2020,（6）
• 所属期刊栏目: Original articles
• 页码范围: 1073-1082
• 页数: 10页
• 语种: 英文

摘要

Twelve new grayanoids (1-12) along with five known compounds were isolated from flowers of Rhododendron molle.Their structures were fully characterized using a combination of spectroscopic analyses,computational calculations,and single crystal X-ray diffraction.Rhomollone A (1)possesses an unprecedented 5/6/6/5 tetra-cyclic ring system (B-nor grayanane) incorporating a cyclopentene-l,3-dione scaffold.Rhodomollein XLⅢI (2) is a dimeric grayanoid,containing a novel 14-membered heterocyclic ring with a C2 symmetry axis.The antinociceptive activities of compounds 3,4,6,7,and 12 -17 were evaluated by an acetic acid-induced writhing test.Among them,compounds 3,7,12,15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from 41.9％ to 91.6％.Compounds 6 and 13 inhibited 46.0％ and 39.4％ of the acetic acid-induced writhes at a dose of 2 mg/kg,while compound 17 inhibited 34.3％ of the writhes at a dose of 0.4 mg/kg.