Tsou M F, Chen G W, Hung C F, Yeh F T, Chang H L, Lu H F, Chung J G
Department of Clinical Laboratory, China Medical College Hospital, Taichung, Taiwan, Republic of China.
Microbios. 2001;104(408):87-97.
Growth inhibition and arylamine N-acetyltransferase (NAT) activity in Neisseria gonorrhoeae were inhibited by luteolin, a drug which originated from herbs. The growth inhibition was based on changes in optical density (OD) using a spectrophotometer, and arylamine NAT activity with 2-aminofluorene (2-AF) was determined using high pressure liquid chromatography. The inhibition of growth in N. gonorrhoeae demonstrated that luteolin elicited a dose-dependent growth inhibition in the N. gonorrhoeae cultures. Suspensions of N. gonorrhoeae with or without specific concentrations of luteolin cotreatment showed different percentages of 2-AF acetylation. The data indicated that there was reduced NAT activity associated with increased levels of luteolin in N. gonorrhoeae suspensions. Time-course experiments showed that NAT activity measured from intact N. gonorrhoeae cells was inhibited by luteolin for at least 4 h. Using standard steady-state kinetic analysis, it was demonstrated that luteolin was a possible uncompetitive inhibitor to NAT activity in N. gonorrhoeae. This report is the first to show that luteolin can inhibit N. gonorrhoeae NAT activity.
木犀草素可抑制淋病奈瑟菌的生长及芳胺N - 乙酰基转移酶(NAT)活性,木犀草素是一种源自草药的药物。生长抑制通过使用分光光度计检测光密度(OD)变化来确定,而芳胺NAT活性则采用高压液相色谱法测定2 - 氨基芴(2 - AF)来确定。淋病奈瑟菌生长抑制实验表明,木犀草素在淋病奈瑟菌培养物中引起剂量依赖性生长抑制。含或不含特定浓度木犀草素共处理的淋病奈瑟菌悬液显示出不同百分比的2 - AF乙酰化。数据表明,淋病奈瑟菌悬液中木犀草素水平升高与NAT活性降低有关。时间进程实验表明,木犀草素对完整淋病奈瑟菌细胞测得的NAT活性抑制至少持续4小时。通过标准稳态动力学分析表明,木犀草素可能是淋病奈瑟菌NAT活性的非竞争性抑制剂。本报告首次表明木犀草素可抑制淋病奈瑟菌NAT活性。