| 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F2。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，且不同活性基因对新狼毒素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。 |
| 关键词: 抑菌活性 结构修饰 新狼毒素B 构效关系 |
| DOI： |
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| 基金项目:国家自然科学基金资助项目（30571402） |
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| Study on structure modification of neochamaejasmine B and relationship of structure-antibacterial activity |
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| Abstract: |
| Compounds F1,F1-0,B1 and B2 were obtained from neochamaejasmine B by using NaBH4 as the reductant and BrCH2COOH as the carboxymethyl etherification reagent respectively.The antibacterial activity of neochamaejasmine B and its four derivatives,were tested with dish diffusion of Neo-Sensitab in vitro againstS.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. |
| Key words: antibacterial activity structure modification neochamaejasmine B structure-activity relationship |
