摘要
目的研究浙贝乙素及其5种衍生物的急性毒性和对小鼠的半数致死量(LD50)。方法取昆明种小鼠,完全随机平均分组后腹腔注射给药,分别给予不同浓度的浙贝乙素乙酰化物、丙酰化物、丁酰化物、苯甲酰化物和氧化物药液。以小鼠急性死亡率为指标,求浙贝乙素各衍生物的LD50和LD50的95%可信区间。结果浙贝乙素乙酰化物、丙酰化物、丁酰化物、苯甲酰化物和氧化物对小鼠的LD50分别为14.39,14.47,18.41,23.21,9.98mg·kg-1,均大于浙贝乙素对小鼠的LD50。结论浙贝乙素乙酰化物、丙酰化物、丁酰化物、苯甲酰化物和氧化物的毒性均较小,有望从中筛选出高效、低毒的镇咳药物。
Objective To determine the acute toxicity and LD_50 of peiminine and its five derivatives in mice. Methods Mice of the Kunming strain were randomly divided into 33 groups with 10 animals in each group. Mice of different groups were given each an intraperitoneal injection of peiminine and its 5 derivatives in different doses separately.Values of LD_50 and 95% confidence interval of the 6 drugs were then calculated with the Bliss method. Results The LD_50 of acetyl peiminine, propionyl peiminine, butyryl peiminine, benzoyl peiminine and peiminine oxide were shown to be 14.39, 14.47, 18.41, 23.21 and 9.98 mg·kg^-1 ,respectively , all of which being larger than that of peiminine (6.86 mg·kg^-1). Corresponding results were obtained in the calculation of the LD_50 95% confidence intervals of the 6 drugs. Conclusion All the five derivatives of peiminine were shown to have lower toxicity than that of peiminine and it is hopeful to find antitussives of high potency and low toxicity from these derivatives.
出处
《医药导报》
CAS
2005年第8期660-662,共3页
Herald of Medicine
基金
国家中医药管理局新药基金资助项目(基金编号:D2X004A)
