(-)-Epicatechin gallate serves as a novel new delhi metallo-β-lactamase-1(NDM-1)inhibitor
一种新型NDM-1抑制剂:(–)-表儿茶素没食子酸酯作者机构:National Key Laboratory for Screening New Microbial DrugsInstitute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing 100050China
出 版 物:《Journal of Chinese Pharmaceutical Sciences》 (中国药学(英文版))
年 卷 期:2021年第30卷第9期
页 面:716-724页
核心收录:
学科分类:1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 100706[医学-药理学] 100602[医学-中西医结合临床] 10[医学]
基 金:Natural Sciences Foundation of China(NSFC,Grant No.81872913) National High-tech R&D Program(863 Program,Grant No.2015AA020911)
主 题:NDM-1 (-)-Epicatechin gallate Inhibitor Antibiotics resistance
摘 要:Theβ-lactam antibiotic resistance caused by NDM-1 has become a major crisis of global public *** have previously screened out(-)-epicatechin gallate(ECG)as a potent NDM-1 *** further discussed its inhibitory effect and action mode in the present *** to our results,ECG reversibly inactivated NDM-1 in a non-competitive mode,with an IC50 value of 4.48μ*** effectively recovered the activity of severalβ-lactam antibiotics against resistant strain harboring ***,the effects on carbapenems were worth *** zinc supplement assay indicated a zinc-related mechanism of *** from traditional chelating agents,it showed low toxicity both in vivo and in *** a word,our findings provided a promising NDM-1 inhibitor,ECG,which was able to assist carbapenems against NDM-1-producing strain.