New Quinone Antibiotics against Methicillin-Resistant S. aureus

被引：8

作者：

Campanini-Salinas, Javier ^{[1
,2
]}

Andrades-Lagos, Juan ^{[1
]}

Hinojosa, Nicolas ^{[1
]}

Moreno, Fabian ^{[1
]}

Alarcon, Pedro ^{[3
]}

Gonzalez-Rocha, Gerardo ^{[4
,5
]}

Burbulis, Ian E. ^{[6
,7
]}

Vasquez-Velasquez, David ^{[1
]}

机构：

[1] Univ Chile, Fac Chem & Pharmaceut Sci, Drug Dev Lab, Sergio Livingstone 1007, Santiago 8380492, Chile

[2] Univ San Sebastian, Fac Med & Ciencia, Lago Panguipulli 1390, Puerto Montt 5501842, Chile

[3] Inst Salud Publ Chile, Agents Bacterial Meningitis Lab, Santiago 7780050, Chile

[4] Univ Concepcion, Fac Ciencias Biol, Dept Microbiol, Lab Invest Agentes Antibacterianos LIAA, Concepcion 4070386, Chile

[5] Millennium Initiat Collaborat Res Bacterial Resis, Av Las Condes 12-438, Santiago 8320000, Chile

[6] Univ San Sebastian, Fac Med & Ciencias, Ctr Invest Biomed, Sede Patagonia, Lago Panguipulli 1390, Puerto Montt 5501842, Chile

[7] Univ Virginia, Sch Med, Dept Biochem & Mol Genet, 1340 Jefferson Pk Ave, Charlottesville, VA 22908 USA

来源：

ANTIBIOTICS-BASEL | 2021年 / 10卷 / 06期

基金：

美国国家卫生研究院;

关键词：

methicillin-resistant S; aureus (MRSA); drug discovery; quinone-antibiotics; GALLERIA-MELLONELLA LARVAE; IN-VIVO MODEL; STAPHYLOCOCCUS-AUREUS; EFFICACY; VANCOMYCIN; GLYCOPEPTIDE; COMBINATION; DAPTOMYCIN; CHALLENGES; INFECTION;

D O I：

10.3390/antibiotics10060614

中图分类号：

R51 [传染病];

学科分类号：

100401 ;

摘要：

There is an urgent need for the development of new antibiotics. Here, we describe the inhibitory activity of new quinone compounds against methicillin-resistant Staphylococcus aureus (ATCC(R) 43300), methicillin-sensitive S. aureus (ATCC(R) 29213), and two clinical isolates from Chile (ISP-213 and ISP-214). We observed 99.9% reduction in viability within 2 h of exposure without the cultures exhibiting any post-antibiotic effect, which was twice the kinetics to that observed with vancomycin. These clinical isolates did not acquire resistance to these quinone derivatives during the course of our study. We found that these compounds protected larvae of the greater wax moth, sp. Galleria mellonella, from infection by these MRSA clinical strains as effectively as vancomycin. These quinone derivatives are potential drug candidates worth further development.

引用

页数：11

共 42 条

[1] Galleria mellonella larvae allow the discrimination of toxic and non-toxic chemicals [J].