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Planta Med ; 83(3-04): 239-244, 2017 Feb.
Article in English | MEDLINE | ID: mdl-27442262

ABSTRACT

The trypanocidal potential of the natural chalcone flavokawin B, which was isolated from the hexanic extract of Polygonum ferrugineum Wedd., is reported here. Although flavokawin B is widespread, this is the first report about its trypanocidal properties on both Trypanosoma cruzi (IC50 = 9.5 µM, IC50 = 34.7 µM benznidazol, Y strain) epimastigotes and Trypanosoma brucei (IC50 = 4.8 µM, IC50 = 6.4 µM pentamidine, 29-13 strain) procyclic forms, which was also corroborated on T. brucei strain 427 (IC50 = 6.2 µM). In order to learn more about its properties, unspecific cytotoxicity on Hep G2 cells was investigated as well as the trans-splicing inhibitory potential on T. brucei cells. The results shown here point to flavokawin B as a candidate in the search for new agents. It is also cheaper and less toxic than the available drugs to treat trypanosomiasis with a special focus on sleeping sickness disease.


Subject(s)
Flavonoids/pharmacology , Trypanocidal Agents/pharmacology , Trypanosoma brucei brucei/drug effects , Trypanosoma cruzi/drug effects , Trypanosomiasis/drug therapy , Cell Survival/drug effects , Chalcone/pharmacology , Dose-Response Relationship, Drug , Flavonoids/chemistry , Flavonoids/isolation & purification , Hep G2 Cells , Humans , Inhibitory Concentration 50 , Polygonum/chemistry , Trypanocidal Agents/chemistry , Trypanocidal Agents/isolation & purification , Trypanosoma brucei brucei/genetics , Trypanosomiasis, African/drug therapy
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