Title |
Embelin Restores Carbapenem Efficacy against NDM-1-Positive Pathogens
|
---|---|
Published in |
Frontiers in Microbiology, January 2018
|
DOI | 10.3389/fmicb.2018.00071 |
Pubmed ID | |
Authors |
Nian-Zhi Ning, Xiong Liu, Fanghong Chen, Peng Zhou, Lihong Hu, Jian Huang, Zhan Li, Jie Huang, Tao Li, Hui Wang |
Abstract |
The emergence and spread of carbapenemase in Gram-negative pathogens poses an enormous threat to global public health. New Delhi metallo-β-lactamase-1 (NDM-1) inactivates nearly every class of β-lactam antibiotics, including carbapenem; however, there is no clinically useful NDM-1 inhibitor. Embelin, an important ingredient in traditional herbal medicine, has anti-tumor effects. The current study is the first to discover and examine the inhibitory activity of embelin against β-lactamase NDM-1. The IC50 of embelin was 2.1 ± 0.2 μM when tested against NDM-1 carbapenemase. Most regions of the embelin molecule were buried within NDM-1's active site, and the hydroxyl group of embelin interacted directly with the metal ion Zn2+, as shown by molecular dynamic simulation. Systematic analysis of the antibacterial activities of embelin and antibiotics demonstrated that embelin restored meropenem activity against a panel of NDM-positive pathogens, such as Escherichia coli, Klebsiella pneumoniae, and Acinetobacter baumannii. Based on these results, embelin could be a promising carbapenem adjuvant candidate against NDM-1-producing bacterial strains. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
Australia | 1 | 13% |
France | 1 | 13% |
Germany | 1 | 13% |
Spain | 1 | 13% |
India | 1 | 13% |
Unknown | 3 | 38% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 7 | 88% |
Scientists | 1 | 13% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
Unknown | 30 | 100% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 5 | 17% |
Student > Bachelor | 4 | 13% |
Student > Master | 3 | 10% |
Researcher | 3 | 10% |
Student > Doctoral Student | 1 | 3% |
Other | 4 | 13% |
Unknown | 10 | 33% |
Readers by discipline | Count | As % |
---|---|---|
Chemistry | 5 | 17% |
Biochemistry, Genetics and Molecular Biology | 3 | 10% |
Agricultural and Biological Sciences | 2 | 7% |
Immunology and Microbiology | 2 | 7% |
Veterinary Science and Veterinary Medicine | 1 | 3% |
Other | 3 | 10% |
Unknown | 14 | 47% |