In vitro activity of salinomycin and monensin derivatives against Trypanosoma brucei
PBN-AR
Instytucja
Wydział Chemii (Uniwersytet im. Adama Mickiewicza w Poznaniu)
Informacje podstawowe
Główny język publikacji
en
Czasopismo
Parasites & Vectors
ISSN
1756-3305
EISSN
Wydawca
BIOMED CENTRAL LTD
DOI
URL
Rok publikacji
2016
Numer zeszytu
Strony od-do
409-409[9]
Numer tomu
9
Identyfikator DOI
Liczba arkuszy
Autorzy
(liczba autorów: 3)
Pozostali autorzy
+ 2
Słowa kluczowe
en
Trypanosoma brucei
Salinomycin derivatives
Monensin derivatives
African trypanosomaisis
Drug screening
Streszczenia
Język
en
Treść
Background: African trypanosomes are the causative agents of sleeping sickness in humans and nagana disease in livestock animals. As the few drugs available for treatment of the diseases have limited efficacy and produce adverse reactions, new and better tolerated therapies are required. Polyether ionophores have been shown to display anti-cancer, anti-microbial and anti-parasitic activity. In this study, derivatives of the polyether ionophores, salinomycin and monensin were tested for their in vitro activity against bloodstream forms of Trypanosoma brucei and human HL-60 cells. Results: Most polyether ionophore derivatives were less trypanocidal than their corresponding parent compounds. However, two salinomycin derivatives (salinomycin n-butyl amide and salinomycin 2,2,2-trifluoroethyl ester) were identified that showed increased anti-trypanosomal activity with 50 \% growth inhibition values in the mid nanomolar range and minimum inhibitory concentrations of below 1 mu M similar to suramin, a drug used in the treatment of sleeping sickness. In contrast, human HL-60 cells were considerably less sensitive towards all polyether ionophore derivatives. The cytotoxic to trypanocidal activity ratio (selectivity) of the two promising compounds was greater than 250. Conclusions: The data indicate that polyether ionophore derivatives are interesting lead compounds for rational anti-trypanosomal drug development.
Cechy publikacji
discipline:Biochemia – dziedzina nauk chemicznych
discipline:Biologia medyczna
discipline:Chemia
discipline:Biochemistry – field of chemical sciences
discipline:Medical biology
discipline:Chemistry
Original article
Original article presents the results of original research or experiment.
Oryginalny artykuł naukowy
Oryginalny artykuł naukowy przedstawia rezultaty oryginalnych badań naukowych lub eksperymentu.
Inne
System-identifier
PBN-R:768055
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