新狼毒素B的抑菌活性构效关系研究  

Study on structure modification of neochamaejasmine B and relationship of structure-antibacterial activity

作　　者：冉晓娅[1] 周乐[1] 张武岗[1] 杨明利[1] 吴联[1] 

机构地区：[1]西北农林科技大学生命科学学院,陕西杨凌712100

出　　处：《西北农林科技大学学报（自然科学版）》2006年第4期83-86,共4页Journal of Northwest A&F University(Natural Science Edition)

基　　金：国家自然科学基金资助项目(30571402)

摘　　要：以新狼毒素B为原料,以硼氢化钠为还原剂,以溴乙酸为羧基甲基醚化试剂,分别合成出2种羰基还原产物F1和F1-0及2种羧甲醚化产物B1和B2。选择金黄色葡萄球菌、乳房链球菌、停乳链球菌、大肠杆菌和沙门氏菌为供试菌,采用药敏纸片法对新狼毒素B及其4种衍生物进行了抑菌活性测定。结果表明,与新狼毒素B相比,F1对所有供试菌的抑菌活性有一定程度增加,F1-0的抑菌活性有微小减弱,B1和B2对5种菌的抑菌活性均明显减弱。初步说明新狼毒素B分子中的7,7,″4,′4 4个酚羟基中的2个为主要活性基团,且不同活性基团对新狼毒素B的抑菌活性的选择性影响很大;羰基不是新狼毒素B的主要活性基团。Compounds F1 ,F1-0, B1 and B2 were obtained from neochamaejasmine B by using NaBH4 as the reductant and BrCH2COOH as the carboxymethyl etherifieation reagent respectively. The antibacterial activity of neochamaejasmine B and its four derivatives ,were tested with dish diffusion of Neo-Sensitab in vitro against S. aureas,S, uberis,S, dysagalactiae,Samonellal and E. coli.. The results showed that the antibacterial activity against all bacteria tested was slightly higher than that of neochamaejasmine B,but that of F1-0 was slightly lower ,and that of B1 and B2 dropped obviously. The above mentioned explained that two of 7,7＂4＇ ,4＂ four hydroxyl groups of neochamaejasmine B were the main active group,and that different active group had great effect on the selectivity of antibacterial activity of neochamaejasmine B and carbonyl group was not the main active group.

关 键 词：抑菌活性 结构修饰 新狼毒素B 构效关系 

分 类 号：S481.9[农业科学—农药学] O656.4[农业科学—植物保护]