夹竹桃叶甲醇提取物中的强心甾类化合物对小鼠具有中枢神经系统抑制活性。

Cardenolides from the methanolic extract of Nerium oleander leaves possessing central nervous system depressant activity in mice.

作者信息

Siddiqui B S, Sultana R, Begum S, Zia A, Suria A

机构信息

H.E.J. Research Institute of Chemistry, University of Karachi, Pakistan.

出版信息

J Nat Prod. 1997 Jun;60(6):540-4. doi: 10.1021/np960679d.

DOI:10.1021/np960679d

PMID:9214727

Abstract

Two new cardenolides, 3 beta-O-(D-2-O-methyldigitalosyl)-14 beta-hydroxy-5 beta-carda-16,20(22)-dienolide (1) and 3 beta-hydroxy-8,14-epoxy-5 beta-carda-16,20(22)-dienolide (2), and two known cardenolides, 3 beta-O-(D-digitalosyl)-14 beta-hydroxy-16 beta-acetoxy-5 beta-card-20(22)-enolide (3) and 3 beta-O-(D-digitalosyl)-14 beta-hydroxy-5 beta-card-20(22)-enolide (4), have been isolated from the leaves of Nerium oleander following a bioactivity-directed isolation of the MeOH extract, which showed central nervous system (CNS) depressant activity in mice at a dosage of 50 mg/kg i.p. Their structures were established on the basis of chemical and spectral data. Compounds 1, 3, and 4 were found to exhibit sedation in mice at a dosage of 25 mg/kg, although 2 had no effect on the CNS of mice at a dosage of up to 50 mg/kg.

摘要

在对夹竹桃甲醇提取物进行生物活性导向分离后，从夹竹桃叶子中分离出两种新的强心苷，即3β - O -（D - 2 - O - 甲基洋地黄糖基）- 14β - 羟基 - 5β - 卡丹 - 16,20(22) - 二烯醇内酯（1）和3β - 羟基 - 8,14 - 环氧 - 5β - 卡丹 - 16,20(22) - 二烯醇内酯（2），以及两种已知的强心苷，3β - O -（D - 洋地黄糖基）- 14β - 羟基 - 16β - 乙酰氧基 - 5β - 卡丹 - 20(22) - 烯醇内酯（3）和3β - O -（D - 洋地黄糖基）- 14β - 羟基 - 5β - 卡丹 - 20(22) - 烯醇内酯（4）。该甲醇提取物经腹腔注射给予小鼠50 mg/kg剂量时显示出中枢神经系统（CNS）抑制活性。它们的结构是根据化学和光谱数据确定的。发现化合物1、3和4在25 mg/kg剂量时对小鼠有镇静作用，而化合物2在高达50 mg/kg剂量时对小鼠中枢神经系统无影响。