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Three new antinociceptive diterpenoids from the roots of Rhododendron micranthum
Bing Chai1, Yong Li1, Shi-Shan Yu1
1State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union, Medical College, Beijing 100050, China.
Abstract:
Two new grayanane-type (1 and 2) and one new kalmane-type diterpenoids (3), together with 16 known compounds, were isolated from the roots of Rhododendron micranthum. The structures of new compounds were fully determined on the basis of spectroscopic analysis, including HRESIMS, 1 D and 2 D NMR data. An acetic acid-induced writhing test in mice was proceeded to evaluate the antinociceptive activities of compounds 1-3, 5-6, 9-14 and 16. Compared to vehicle-injected mice, compounds 1, 6, 14 and 16 showed significant antinociceptive effects with writhe inhibition rates of 45.8%-64.2% at a dose of 0.1 mg/kg, and compounds 10, 12 and 13 showed significant antinociceptive effects with writhe inhibition rates of 33.9%-64.8% at a dose of 5 mg/kg. Compound 2 showed potent antinociceptive effects with writhe inhibition rates of 86.1% and 54.7% at doses of 8 mg/kg and 0.8 mg/kg, respectively. [Formula: see text].
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