![](/images/graphics-bg.png)
Small Molecule Inhibitor of Type Three Secretion System Belonging to a Class 2,4-disubstituted-4H-[1,3,4]-thiadiazine-5-ones Improves Survival and Decreases Bacterial Loads in an Airway Pseudomonas aeruginosa Infection in Mice
Joint Authors
Zigangirova, Naylia A.
Kapotina, Lidia N.
Gintsburg, Alexandr L.
Kobets, Natalia V.
Zayakin, Egor S.
Luyksaar, Sergei I.
Sheremet, Anna B.
Nesterenko, Ludmila N.
Source
Issue
Vol. 2018, Issue 2018 (31 Dec. 2018), pp.1-13, 13 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2018-09-10
Country of Publication
Egypt
No. of Pages
13
Main Subjects
Abstract EN
Pseudomonas aeruginosa is a cause of high mortality in burn, immunocompromised, and surgery patients.
High incidence of antibiotic resistance in this pathogen makes the existent therapy inefficient.
Type three secretion system (T3SS) is a leading virulence system of P.
aeruginosa that actively suppresses host resistance and enhances the severity of infection.
Innovative therapeutic strategies aiming at inhibition of type three secretion system of P.
aeruginosa are highly attractive, as they may reduce the severity of clinical manifestations and improve antibacterial immune responses.
They may also represent an attractive therapy for antibiotic-resistant bacteria.
Recently our laboratory developed a new small molecule inhibitor belonging to a class 2,4-disubstituted-4H-[1,3,4]-thiadiazine-5-ones, Fluorothiazinon (FT), that effectively suppressed T3SS in chlamydia and salmonella in vitro and in vivo.
In this study, we evaluate the activity of FT towards antibiotic-resistant clinical isolates of P.
aeruginosa expressing T3SS effectors ExoU and ExoS in an airway infection model.
We found that FT reduced mortality and bacterial loads and decrease lung pathology and systemic inflammation.
In addition, we show that FT inhibits the secretion of ExoT and ExoY, reduced bacteria cytotoxicity, and increased bacteria internalization in vitro.
Overall, FT shows a strong potential as an antibacterial therapy of antibiotic-resistant P.
aeruginosa infection.
American Psychological Association (APA)
Sheremet, Anna B.& Zigangirova, Naylia A.& Zayakin, Egor S.& Luyksaar, Sergei I.& Kapotina, Lidia N.& Nesterenko, Ludmila N.…[et al.]. 2018. Small Molecule Inhibitor of Type Three Secretion System Belonging to a Class 2,4-disubstituted-4H-[1,3,4]-thiadiazine-5-ones Improves Survival and Decreases Bacterial Loads in an Airway Pseudomonas aeruginosa Infection in Mice. BioMed Research International،Vol. 2018, no. 2018, pp.1-13.
https://search.emarefa.net/detail/BIM-1127527
Modern Language Association (MLA)
Sheremet, Anna B.…[et al.]. Small Molecule Inhibitor of Type Three Secretion System Belonging to a Class 2,4-disubstituted-4H-[1,3,4]-thiadiazine-5-ones Improves Survival and Decreases Bacterial Loads in an Airway Pseudomonas aeruginosa Infection in Mice. BioMed Research International No. 2018 (2018), pp.1-13.
https://search.emarefa.net/detail/BIM-1127527
American Medical Association (AMA)
Sheremet, Anna B.& Zigangirova, Naylia A.& Zayakin, Egor S.& Luyksaar, Sergei I.& Kapotina, Lidia N.& Nesterenko, Ludmila N.…[et al.]. Small Molecule Inhibitor of Type Three Secretion System Belonging to a Class 2,4-disubstituted-4H-[1,3,4]-thiadiazine-5-ones Improves Survival and Decreases Bacterial Loads in an Airway Pseudomonas aeruginosa Infection in Mice. BioMed Research International. 2018. Vol. 2018, no. 2018, pp.1-13.
https://search.emarefa.net/detail/BIM-1127527
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1127527