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从黄花夹竹桃种仁中分得的一种强心甙neriifolin,乙酰化后得diacetylneriifolin,后者对心脏的作用减弱,生物活性降低。neriifolin的鸽最小致死量为0.217士0.008毫克(标准誤)/公斤,而diacetylneriifolin为0.649±0.024毫克/公斤;并且显效速度比neriifolin更为迟慢,蓄积性也增大。此外,产生明显的鎮靜催眠作用,可拮抗咖啡因引起的小鼠兴奋活动,延长环己烯巴比妥鈉的睡眠时間和降低小鼠的体溫。对化学結构改变而引起的药理作用差异的原因作了初步探討。
Acetylated diacetylneriifolin, a kind of cardiac glycoside neriifolin obtained from the yellow oleander kernel, the latter has the effect of weakening the heart and reducing the biological activity. The minimum lethal dose of neriifolin was 0.217 ± 0.008 mg / kg and diacetylneriifolin was 0.649 ± 0.024 mg / kg; and the apparent effect was slower and more cumulative than neriifolin. In addition, significant sedative and hypnotic effects were produced, which could antagonize the caffeine-induced excitatory activity of mice, prolong the sleeping time of cyclohexene sodium and reduce the body temperature of mice. The reason for the difference of pharmacological action caused by the change of chemical structure was discussed.