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钩藤根中吲哚生物碱对去甲肾上腺素能神经递质传递的影响。

Effect of indole alkaloids from roots of Rauvolfia ligustrina in the noradrenergic neurotransmission.

机构信息

Departamento de Química Orgânica e Inorgânica, Universidade Federal do Ceará, 60971-270 Fortaleza, CE, Brazil.

Instituto Superior de Ciências Biomédicas, Universidade Estadual do Ceará, 60714-903 Fortaleza, CE, Brazil.

出版信息

Fitoterapia. 2020 Jun;143:104545. doi: 10.1016/j.fitote.2020.104545. Epub 2020 Mar 7.

Abstract

The new glucosyl sarpagan alkaloid designated as 21(R*)-(O-β-glucosyl)-hydroxy-sarpagan-17-oic acid, along with eleven known alkaloids were isolated from a soluble alkaloidal fraction from the ethanol extract of Rauvolfia ligustrina. Their structures were elucidated by interpretation of spectroscopic data (1D and 2D NMR), HRESIMS experiment, GIAO C NMR calculations, and comparison with literature data. All the isolated alkaloids were screened by their neuroinhibitory effects using the electrically stimulated mice vas deferens bioassay. Compounds 1, 2 and 9 presented a potent inhibitory effect in the neurotransmission while 3 and 11 showed an acute neuroexcitatory effect. Compound 10 exhibited a very effective post-synaptic inhibitory activity.

摘要

从白花藤(Rauvolfia ligustrina)乙醇提取物的可溶生物碱部分分离得到一种新的葡萄糖基萨帕烷生物碱,命名为 21(R*)-(O-β-葡萄糖基)-羟基萨帕烷-17-酸,以及 11 种已知生物碱。通过光谱数据(1D 和 2D NMR)、高分辨率电喷雾质谱(HRESIMS)实验、GIAO C NMR 计算以及与文献数据的比较,解析了它们的结构。采用电刺激小鼠输精管生物测定法,对所有分离得到的生物碱进行了神经抑制作用筛选。化合物 1、2 和 9 在神经传递中表现出很强的抑制作用,而化合物 3 和 11 则表现出急性神经兴奋作用。化合物 10 表现出非常有效的突触后抑制活性。

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