Antibacterial compounds against non-growing and intracellular bacteria
(2025) In npj antimicrobials and resistance 3(1).- Abstract
Slow- and non-growing bacterial populations, along with intracellular pathogens, often evade standard antibacterial treatments and are linked to persistent and recurrent infections. This necessitates the development of therapies specifically targeting nonproliferating bacteria. To identify compounds active against non-growing uropathogenic Escherichia coli (UPEC) we performed a drug-repurposing screen of 6454 approved drugs and drug candidates. Using dilution-regrowth assays, we identified 39 compounds that either kill non-growing UPEC or delay its regrowth post-treatment. The hits include fluoroquinolones, macrolides, rifamycins, biguanide disinfectants, a pleuromutilin, and anti-cancer agents. Twenty-nine of the hits have not... (More)
Slow- and non-growing bacterial populations, along with intracellular pathogens, often evade standard antibacterial treatments and are linked to persistent and recurrent infections. This necessitates the development of therapies specifically targeting nonproliferating bacteria. To identify compounds active against non-growing uropathogenic Escherichia coli (UPEC) we performed a drug-repurposing screen of 6454 approved drugs and drug candidates. Using dilution-regrowth assays, we identified 39 compounds that either kill non-growing UPEC or delay its regrowth post-treatment. The hits include fluoroquinolones, macrolides, rifamycins, biguanide disinfectants, a pleuromutilin, and anti-cancer agents. Twenty-nine of the hits have not previously been recognized as active against non-growing bacteria. The hits were further tested against non-growing Pseudomonas aeruginosa and Staphylococcus aureus. Ten compounds - solithromycin, rifabutin, mitomycin C, and seven fluoroquinolones-have strong bactericidal activity against non-growing P. aeruginosa, killing >4 log10 of bacteria at 2.5 µM. Solithromycin, valnemulin, evofosfamide, and satraplatin are unique in their ability to selectively target non-growing bacteria, exhibiting poor efficacy against growing bacteria. Finally, 31 hit compounds inhibit the growth of intracellular Shigella flexneri in a human enterocyte infection model, indicating their ability to permeate the cytoplasm of host cells. The identified compounds hold potential for treating persistent infections, warranting further comparative studies with current standard-of-care antibiotics.
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- author
- Kaldalu, Niilo
; Bērziņš, Normunds
; Berglund Fick, Stina
; Sharma, Atin
; Andersson, Naomi Charlotta
; Aedla, Jüri
; Hinnu, Mariliis
; Puhar, Andrea
; Hauryliuk, Vasili
LU
and Tenson, Tanel
- organization
- publishing date
- 2025-04-11
- type
- Contribution to journal
- publication status
- published
- subject
- in
- npj antimicrobials and resistance
- volume
- 3
- issue
- 1
- article number
- 25
- external identifiers
-
- pmid:40216902
- ISSN
- 2731-8745
- DOI
- 10.1038/s44259-025-00097-0
- language
- English
- LU publication?
- yes
- additional info
- © 2025. The Author(s).
- id
- 9e5f47a4-5715-4678-8daf-ccc1a3bfd195
- date added to LUP
- 2025-04-12 13:11:44
- date last changed
- 2025-04-14 08:46:38
@article{9e5f47a4-5715-4678-8daf-ccc1a3bfd195, abstract = {{<p>Slow- and non-growing bacterial populations, along with intracellular pathogens, often evade standard antibacterial treatments and are linked to persistent and recurrent infections. This necessitates the development of therapies specifically targeting nonproliferating bacteria. To identify compounds active against non-growing uropathogenic Escherichia coli (UPEC) we performed a drug-repurposing screen of 6454 approved drugs and drug candidates. Using dilution-regrowth assays, we identified 39 compounds that either kill non-growing UPEC or delay its regrowth post-treatment. The hits include fluoroquinolones, macrolides, rifamycins, biguanide disinfectants, a pleuromutilin, and anti-cancer agents. Twenty-nine of the hits have not previously been recognized as active against non-growing bacteria. The hits were further tested against non-growing Pseudomonas aeruginosa and Staphylococcus aureus. Ten compounds - solithromycin, rifabutin, mitomycin C, and seven fluoroquinolones-have strong bactericidal activity against non-growing P. aeruginosa, killing >4 log10 of bacteria at 2.5 µM. Solithromycin, valnemulin, evofosfamide, and satraplatin are unique in their ability to selectively target non-growing bacteria, exhibiting poor efficacy against growing bacteria. Finally, 31 hit compounds inhibit the growth of intracellular Shigella flexneri in a human enterocyte infection model, indicating their ability to permeate the cytoplasm of host cells. The identified compounds hold potential for treating persistent infections, warranting further comparative studies with current standard-of-care antibiotics.</p>}}, author = {{Kaldalu, Niilo and Bērziņš, Normunds and Berglund Fick, Stina and Sharma, Atin and Andersson, Naomi Charlotta and Aedla, Jüri and Hinnu, Mariliis and Puhar, Andrea and Hauryliuk, Vasili and Tenson, Tanel}}, issn = {{2731-8745}}, language = {{eng}}, month = {{04}}, number = {{1}}, series = {{npj antimicrobials and resistance}}, title = {{Antibacterial compounds against non-growing and intracellular bacteria}}, url = {{http://dx.doi.org/10.1038/s44259-025-00097-0}}, doi = {{10.1038/s44259-025-00097-0}}, volume = {{3}}, year = {{2025}}, }