溴化1-甲基-1-苄基-4-(((三苯基锡基)硫)硫代甲酰基)哌嗪-1-铵的活性测定  

Activity determination of 1-benzyl-1-methyl-4-((( triphenylstannyl)thio) carbonothioyl) piperazin-1-ium bromide

作　　者：刘树玲[1] 王保国[1] 方思南 

机构地区：[1]济宁医学院药学院,山东日照276826 [2]济宁医学院生物科学系,山东日照276826

出　　处：《中国生化药物杂志》2015年第1期34-36,共3页Chinese Journal of Biochemical Pharmaceutics

基　　金：济宁医学院校级科研项目(JY2013KJ011)

摘　　要：目的测定硫代甲酸盐有机锡类成盐化合物溴化1-甲基-1-苄基-4-(((三苯基锡基)硫)硫代甲酰基)哌嗪-1-铵对小鼠的半数致死量(median lethal dose,LD50)、对小鼠体液免疫功能的影响及其抗菌活性。方法急性毒性试验检测LD50,溶血素测定法测定体液免疫功能,纸片扩散法、倍比稀释法检测其抗菌活性。结果以小鼠急性死亡率为指标,测得LD50为93.7 mg/kg,可信限为(100.98±8.66)mg/kg,可信限率为8.58%,小于10%,表明实验方法准确度高,数据可靠性高;溶血素测定结果表明:与对照组相比,低、中、高3个剂量组的半数溶血值(half value of hemolysin,HC50)显著较高(P<0.01),差异有统计学意义,与阴性对照组相比,空白对照组及3个剂量组均较高(P<0.01),差异有统计学意义,表明此药有提高体液免疫的效果;抗菌活性测定结果表明此药对金黄色葡萄球菌、大肠杆菌和伤寒杆菌均显示抑菌作用,其中对伤寒杆菌抑制效果最好,其最低抑菌浓度(minimal inhibitory concentration,MIC值)为0.31 mg/m L。结论溴化1-甲基-1-苄基-4-(((三苯基锡基)硫)硫代甲酰基)哌嗪-1-铵为中度毒性药物,有体液免疫调节作用,且随剂量增加作用降低,对所测菌株具有抗菌活性。Objective To test median lethal dose（ LD50） of the 1-benzyl-1-methyl-4-（（（ triphenylstannyl） thio） carbonothioyl） piperazin-1-ium bromide on mice,effect on humoral immune function on mice and the antibacterial activity. Methods By acute toxicity test for the detection of median lethal dose（ LD50）,determined the humoral immune function by hemolysin assay method,and disk diffusion method,double dilution method was used to detect antibacterial activity. Results According to the acute mortality of mice as index,the LD50 for the 1-benzyl-1-methyl-4-（（（ triphenylstannyl） thio）carbonothioyl） piperazin-1-ium bromide was 93. 7 mg / kg,confidence limit was（ 100. 98 ± 8. 66） mg / kg,the rate of confidence limit was 8. 58% less than10%,which indicated that the experimental method with high accuracy,and high reliability. humoral immunity determination of HC50 value results showed that： compared with control group,HC50 value in three dose groups was higher,there was statistical significance（ P〈0. 01）,compared with negative control group,HC50 value in blank control group and three dose group were higher,there was significant difference（ P〈0. 01）,which evidicted the drug could enhance the immunologic effect. Antibacterial activity measurement results showed that the drug for Staphylococcus aureus,Escherichia coli and Salmonella typhi showed inhibitory effect,inhibitory effect on Salmonella typhi was the best,the MIC value was 0. 31 mg / m L. Conclusion 1-benzyl-1-methyl-4-（（（ triphenylstannyl） thio） carbonothioyl） piperazin-1-ium bromide is a moderately toxic drug,the effect of regulating humoral immunity with the dose increasing,and has antibacterial activity.

关 键 词：氨基二硫代甲酸盐类化合物 半数致死量 免疫调节 抗菌活性 

分 类 号：R965.3[医药卫生—药理学] R992[医药卫生—药学]