Siddiqui B S, Sultana R, Begum S, Zia A, Suria A
H.E.J. Research Institute of Chemistry, University of Karachi, Pakistan.
J Nat Prod. 1997 Jun;60(6):540-4. doi: 10.1021/np960679d.
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.
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。
