| 摘要: |
| [目的]进一步研究新狼毒素B的抑菌活性构效关系.[方法]以新狼毒素B为原料,合成了7"-甲氧基(A2-1)、7,7"-二甲氧基(E3)和7,7",4"一三甲氧基(E1)3个新狼毒素B甲醚化产物及4-亚甲基新狼毒索B(D3),利用ESI-MS、1H NMR和13C NMR对其结构进行了表征.选择金黄色葡萄球菌(S.aureas)、无乳链球菌(S.agalactiae)、大肠杆菌(E.coli)和沙门氏菌(Samonellal)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]4种修饰物对所有供试菌的抑菌活性均小于新狼毒素B;3种甲醚化产物在质量浓度为0.625～5mg/mL时,对沙门氏菌没有抑菌活性;对于其他3种供试菌,各供试物的抑菌活性次序为新狼毒素B≈D3>A2-1>E3>E1.[结论]新狼毒素B分子中,7-OH和7"-OH是其主要抑菌活性基团,C-OH和4"-OH对抑菌活性的贡献较小,4-羰基不是主要抑菌活性基团. |
| 关键词: 新狼毒素B 结构修饰 抑菌活性 |
| DOI： |
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| 基金项目:国家自然科学基金项目（30571042） |
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| Further study on relationship between structure and antibacterial activity of neochamaejasmine B |
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| Abstract: |
| 【Objective】 It further studied the relationship between structure and antibacterial activity of neochamaejasmine B.【Method】 Four compounds,7″-methoxy neochamaejasmine B (A2-1),7,7″-dimethoxy neochamaejasmine B (E3)，7,7″,4-trimethoxy neochamaejasmine B (E1) and 4-methylene neochamaejasmine B (D3) were prepared from neochamaejasmine B.Their structures were confirmed by ESI-MS，1H NMR and 13C NMR.The antibacterial activity of neochamaejasmine B and its four derivatives were tested with dish diffusion of Neo Sensitab in vitro against S.aureas,S.agalactiae,E.coli and Samonellal.【Result】 The results showed that the antibacterial activity of four derivatives against all bacteria tested was lower than that of neochamaejasmine B.The antibacterial activity of AA2-1,E3 and E1 against Samonellal disappeared at 0.625-5 mg/mL.But the order of the antibacterial activity of all compounds against other bacteria was n-B≈D3>A2-1>E3>E1.【Conclusion】 The above mentioned structure-activity relationship studies showed that 7-OH and 7″-OH of neochamaejasmine B were the main active groups,and that 4′-OH and 4"'-OH had less contribution to its antibacterial activity,and that carbonyl group was not the main active group. |
| Key words: neochamaejasmine B structure modification antibacterial activity |
