生物加工过程2018，Vol.16Issue(3)：53-59,70,8.DOI:10.3969/j.issn.1672-3678.2018.03.008
木犀草素氨基醌抑菌活性和酶抑制活性
Antibacterial and enzyme inhibitory activity of amino quinones based on the structure of luteolin
摘要
Abstract
Luteolin 1 has a variety of biochemical and pharmacological effects. The aminoquinone compounds based on the structure of luteolin are produced by the reaction between luteolin and amines. Due to the introduction of amino,the water solubility of the compounds have been increased. Through its inhibition of microorganisms can be compared to study changes in biological activity. It is possible to explore new therapeutic approaches to Alzheimer′s disease by means of inhibition of acetylcholinesterase and butyrylcholinesterase production.The inhibitory effect of the compounds against E.coli,Bacillus subtilis and Staphylococcus aureus were examined by the inhibition zone method.It was found that the products 2, 4, 5 and 14 of reaction of luteolin with benzylamine, N-benzylisopropylamine, N, N-diethylpropylenediamine and diglycol amine respectively had antibacterial activity against E. coli,but the antibacterial effect is not obvious.The E.coli inhibition zone radius of 2,4,5 and 14 were 0. 678,0. 650, 0. 730 and 0. 680 cm,respectively. Among Staphylococcus aureus,only the reaction products 7 of luteolin and ethylamine had antibacterial activity with an antibacterial radius of 0. 600 cm, while none of the compounds showed bacteriostatic activity against Bacillus subtilis.The 96-well plate method in the Ellman method was used to test the inhibitory effect of this series of compounds on AChE and BuChE.It is showed that only the product of luteolin and isooctylamine 17 has inhibitory activity(71. 07％)against AChE.The products of luteolin and ethanolamine 11 and 3-dimethylaminopropylamine 9 had slightly higher inhibition rate of BuChE than the others. The inhibition rates were 26. 94％ and 17. 05％. Therefore, the aminoquinones based on the structure of luteolin had lower acetycholinesterase inhibition rate. The products were not yet suitable for the treatment of Alzheimer′s disease.关键词
木犀草素/氨基醌/抑菌活性/阿尔茨海默症/胆碱酯酶抑制剂/Ellman法Key words
luteolin/aminoquinone/antibacterial activity/Alzheimer′s disease/enzyme inhibitory activity/Ellman method分类
化学化工引用本文复制引用
王建,朱强,陶传洲,孙威,苏珍妮,王丽,史天智,马晓东,刘玮炜,史大华..木犀草素氨基醌抑菌活性和酶抑制活性[J].生物加工过程,2018,16(3):53-59,70,8.基金项目
国家自然科学基金(21402062) （21402062）
江苏省优势学科建设工程(BK20130404) （BK20130404）
海洋公益性行业科研专项(201505023) （201505023）
连云港市科技攻关计划( CN1401) （ CN1401）
