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Antinociceptive grayanane-derived diterpenoids from flowers of Rhododendron molle.
Acta Pharmaceutica Sinica B ( IF 14.7 ) Pub Date : 2019-11-06 , DOI: 10.1016/j.apsb.2019.10.013
Yong Li 1 , Yuxun Zhu 1 , Zhaoxin Zhang 1 , Li Li 1 , Yunbao Liu 1 , Jing Qu 1 , Shuanggang Ma 1 , Shishan Yu 1
Affiliation  

Twelve new grayanoids (112) 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-1,3-dione scaffold. Rhodomollein XLIII (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 1217 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.



中文翻译:

从杜鹃花的花中提取的抗伤害感受态的灰烷类二萜。

十二新grayanoids(1 - 12)具有5种已知化合物一起被从花中分离杜鹃。结合光谱分析,计算计算和单晶X射线衍射对它们的结构进行了充分表征。Rhomollone A(1)具有史无前例的5/6/6/5四环系统(B-灰烷),其中并入有环戊烯-1,3-二酮骨架。Rhodomollein XLIII(2)是一种二聚体灰度类化合物,含有一个具有C 2对称轴的新颖的14元杂环。化合物的抗伤害活性3467,和12 - 17由乙酸诱导的扭体试验进行评价。其中,化合物37121516在与抑制率从41.9%至91.6%的剂量的20mg / kg的显示显著镇痛活性。化合物613以2mg / kg的剂量抑制46.0%和39.4%的乙酸诱导的扭曲,而化合物17以0.4mg / kg的剂量抑制34.3%的扭曲。

更新日期:2019-11-06
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