Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity

Abstract Implant-associated osteomyelitis (IAOM) is a severe complication of the usage of orthopaedic implants. IAOM is difficult to treat and infection relapse is often due to insufficient treatment of bacterial persister cells. The anthelmintic drug bithionol is promising in combating persister ce...

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Main Authors: Anders Marthinsen Seefeldt, Mikkel Illemann Johansen, Freja Winther Sillesen, Maiken Engelbrecht Petersen, Lars Østergaard, Rikke Louise Meyer, Nis Pedersen Jørgensen
Format: Article
Language:English
Published: Nature Portfolio 2025-07-01
Series:Scientific Reports
Online Access:https://doi.org/10.1038/s41598-025-08879-2
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author Anders Marthinsen Seefeldt
Mikkel Illemann Johansen
Freja Winther Sillesen
Maiken Engelbrecht Petersen
Lars Østergaard
Rikke Louise Meyer
Nis Pedersen Jørgensen
author_facet Anders Marthinsen Seefeldt
Mikkel Illemann Johansen
Freja Winther Sillesen
Maiken Engelbrecht Petersen
Lars Østergaard
Rikke Louise Meyer
Nis Pedersen Jørgensen
author_sort Anders Marthinsen Seefeldt
collection DOAJ
description Abstract Implant-associated osteomyelitis (IAOM) is a severe complication of the usage of orthopaedic implants. IAOM is difficult to treat and infection relapse is often due to insufficient treatment of bacterial persister cells. The anthelmintic drug bithionol is promising in combating persister cells - including Staphylococcus aureus persister cells. We investigated bithionol alone and in combination with antibiotics both in vitro and in vivo, using a murine IAOM model. In vitro experiments confirmed bithionol’s anti-persister activity against S. aureus, demonstrating significant CFU reductions in combination with daptomycin and moxifloxacin. In the murine IAOM model, moxifloxacin led to a small but significant reduction in bacterial load in bone of approx. log 0.5 CFU/ml. However, combining bithionol with antibiotics did not further reduce bacterial load in either bone or on implants. We subsequently demonstrated dramatically reduced activity of bithionol in the presence of albumin, suggesting low bioavailability in vivo. Despite promising in vitro results, bithionol’s efficacy against persister cells did not translate into improving treatment outcome the IAOM model. The study highlights the challenges in translating in vitro findings to in vivo outcomes, and future research into application of bithionol to treat bacterial infections must first address its bioavailability or investigate local delivery options.
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spelling doaj-art-d52ff2188eab4646a4a72efcc40fdc632025-08-20T03:45:52ZengNature PortfolioScientific Reports2045-23222025-07-011511810.1038/s41598-025-08879-2Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activityAnders Marthinsen Seefeldt0Mikkel Illemann Johansen1Freja Winther Sillesen2Maiken Engelbrecht Petersen3Lars Østergaard4Rikke Louise Meyer5Nis Pedersen Jørgensen6Department of Infectious Diseases, Aarhus University HospitalDepartment of Infectious Diseases, Aarhus University HospitalInterdisciplinary Nanoscience Center (iNANO), Aarhus UniversityInterdisciplinary Nanoscience Center (iNANO), Aarhus UniversityDepartment of Infectious Diseases, Aarhus University HospitalInterdisciplinary Nanoscience Center (iNANO), Aarhus UniversityDepartment of Infectious Diseases, Aarhus University HospitalAbstract Implant-associated osteomyelitis (IAOM) is a severe complication of the usage of orthopaedic implants. IAOM is difficult to treat and infection relapse is often due to insufficient treatment of bacterial persister cells. The anthelmintic drug bithionol is promising in combating persister cells - including Staphylococcus aureus persister cells. We investigated bithionol alone and in combination with antibiotics both in vitro and in vivo, using a murine IAOM model. In vitro experiments confirmed bithionol’s anti-persister activity against S. aureus, demonstrating significant CFU reductions in combination with daptomycin and moxifloxacin. In the murine IAOM model, moxifloxacin led to a small but significant reduction in bacterial load in bone of approx. log 0.5 CFU/ml. However, combining bithionol with antibiotics did not further reduce bacterial load in either bone or on implants. We subsequently demonstrated dramatically reduced activity of bithionol in the presence of albumin, suggesting low bioavailability in vivo. Despite promising in vitro results, bithionol’s efficacy against persister cells did not translate into improving treatment outcome the IAOM model. The study highlights the challenges in translating in vitro findings to in vivo outcomes, and future research into application of bithionol to treat bacterial infections must first address its bioavailability or investigate local delivery options.https://doi.org/10.1038/s41598-025-08879-2
spellingShingle Anders Marthinsen Seefeldt
Mikkel Illemann Johansen
Freja Winther Sillesen
Maiken Engelbrecht Petersen
Lars Østergaard
Rikke Louise Meyer
Nis Pedersen Jørgensen
Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
Scientific Reports
title Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
title_full Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
title_fullStr Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
title_full_unstemmed Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
title_short Bithionol is ineffective in a mouse model of S. aureus implant-associated osteomyelitis despite potent in vitro activity
title_sort bithionol is ineffective in a mouse model of s aureus implant associated osteomyelitis despite potent in vitro activity
url https://doi.org/10.1038/s41598-025-08879-2
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