Antinociceptive Grayanoids from the Roots of Rhododendron molle
Antinociceptive Grayanoids from the Roots of Rhododendron molle
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来自杜鹃花根的抗伤害性Grayanoids
DOI：
10.1021/acs.jnatprod.5b00456
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发表时间：
2015-12-01
影响因子：
5.1
通讯作者：
Yu, Shi-Shan
中科院分区：
文献类型：
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作者：
Li, Yong;Liu, Yun-Bao;Yu, Shi-Shan
从羊耳杜鹃（Rhodododendronmolle）根中分离得到9个新的灰烷酸类化合物（1-9）和11个已知化合物。新化合物（1-9）的结构通过波谱分析（包括HRESIMS、1D和2D NMR数据）确定。化合物4、6、12和14 - 20在醋酸扭体实验中表现出明显的镇痛活性。特别地，发现14和15对于急性和炎性疼痛模型都比吗啡更有效，并且在糖尿病神经性疼痛模型中比加巴喷丁更有效100倍。
Nine new grayanoids (1-9), together with 11 known compounds, were isolated from the roots of Rhododendron molle. The structures of the new compounds (1-9) were determined on the basis of spectroscopic analysis, including HRESIMS, and 1D and 2D NMR data. Compounds 4, 6, 12, and 14 20 showed significant antinociceptive activities in an acetic acid-induced writhing test. In particular, 14 and 15 were found to be more potent than morphine for both acute and inflammatory pain models and 100-fold more potent than gabapentin in a diabetic neuropathic pain model.