ProjectTl 07.003_124 – Characterisation of the antimalarial properties of Dehalogenil
Basic data
Acronym:
Tl 07.003_124
Title:
Characterisation of the antimalarial properties of Dehalogenil
Duration:
01/04/2025 to 30/09/2026
Abstract / short description:
Nonetheless, among the widely used therapy regimens (Artemisinin-based combination therapies or “ACTs”) only few are able to effectively target
Gametocytes. Furthermore, the therapy’s backbone Artemisinin has become the target of drug resistances. These first appeared in the Mekong-region but were independently detected on the African continent as well. That is why concern regarding a loss of effectiveness of seasoned therapy regimens is growing. To counteract these developments research into new antimalarials has already picked up pace. One promising candidate for a new antimalarial is the Macrolide Chlorotonil. Its precise mode of action still awaits comprehensive characterisation, but it seems to be diverging from established antimalarials such as Artemisinin and Chloroquin. Invitro assays on the compound indicated towards some desirable traits. It displayed high biological activity against laboratory strains as well as clinical isolates from Gabon, its onset of action is fast and it even showed effective against Gametocytes. Further in-vivo experiments on mice infected with Plasmodium berghei underscored the positive outlook on the substance’s effects.
The focus now lies on the properties of its derivate Dehalogenil. Through its increased water-solubility, higher in-vivo stability and reduced toxicity in animal experiments this substance might combine easier application with the favourable aspects of Chlorotonil.
Gametocytes. Furthermore, the therapy’s backbone Artemisinin has become the target of drug resistances. These first appeared in the Mekong-region but were independently detected on the African continent as well. That is why concern regarding a loss of effectiveness of seasoned therapy regimens is growing. To counteract these developments research into new antimalarials has already picked up pace. One promising candidate for a new antimalarial is the Macrolide Chlorotonil. Its precise mode of action still awaits comprehensive characterisation, but it seems to be diverging from established antimalarials such as Artemisinin and Chloroquin. Invitro assays on the compound indicated towards some desirable traits. It displayed high biological activity against laboratory strains as well as clinical isolates from Gabon, its onset of action is fast and it even showed effective against Gametocytes. Further in-vivo experiments on mice infected with Plasmodium berghei underscored the positive outlook on the substance’s effects.
The focus now lies on the properties of its derivate Dehalogenil. Through its increased water-solubility, higher in-vivo stability and reduced toxicity in animal experiments this substance might combine easier application with the favourable aspects of Chlorotonil.
Involved staff
Managers
Faculty of Medicine
University of Tübingen
University of Tübingen
Local organizational units
Department VII, Tropical Medicine
Department of Internal Medicine
Hospitals and clinical institutes, Faculty of Medicine
Hospitals and clinical institutes, Faculty of Medicine
Funders
Braunschweig, Niedersachsen, Germany