水溶性柠檬苦素苯甲酰腙衍生物的合成及其抗菌活性  

Synthesis and antibacterial activity of water-soluble limonin benzoylhydrazone derivatives

作　　者：杨成伟 郭雅丽 李曹龙 YANG Chengwei;GUO Yali;LI Caolong(School of Science,China Pharmaceutical University,Nanjing 211198,China)

机构地区：[1]中国药科大学理学院,南京211198

出　　处：《中国药科大学学报》2022年第3期273-277,共5页Journal of China Pharmaceutical University

基　　金：国家自然科学基金资助项目(No.81660708)。

摘　　要：柠檬苦素是一种在柑橘属植物中含量较丰富的化合物,具有较广泛的生物活性,但因其水溶性较差,限制了其实际应用。本研究以柠檬苦素为起始原料,在其7位羰基处引入苯甲酰腙,设计、合成了8个新化合物7a~7h。实验结果表明,所有化合物的水溶性较柠檬苦素均有所提升,其中化合物7a、7d、7e和7f较为明显;此外,在苯环间位和对位上有取代羟基的化合物7d和7e对大肠埃希菌(E.coli)和金黄色葡萄球菌(S.aureus)具有较强的抗菌活性,化合物7e活性最好,其最低抑菌浓度分别为0.31 mg/mL和1.25 mg/mL,且化合物7e的抗E.coli效果优于苯甲酸钠。As a compound rich in citrus plants,limonin has a wide range of biological activities,but its practical application is limited because of its poor water solubility.In this paper,eight new compounds 7a-7h were designed and synthesized by introducing benzoyl hydrazone at the carbonyl position of limonin.The results showed that the water solubilities of all compounds were higher than that of limonin,especially 7a,7d,7e and 7f.In addition,the experiment showed that compounds 7d and 7e with substituted hydroxyl groups at the interposition and para-position of the benzene ring had strong antibacterial effects against Escherichia coli and Staphylococcus aureus,and that compound 7e had the best activity,with minimum inhibitory concentrations of 0.31 mg/mL and 1.25 mg/mL,respectively.And compound 7e had better antibacterial activiy in E.coli than sodium benzoate.

关 键 词：柠檬苦素 苯甲酰腙 结构修饰 水溶性 抗菌 合成 

分 类 号：R914.5[医药卫生—药物化学] R965[医药卫生—药学]