title: Trypanocidal Activity of Flavokawin B, a Component of Polygonum ferrugineum Wedd.
abstract: The trypanocidal potential of the natural chalcone flavokawin B, which was isolated from the hexanic extract ofPolygonum ferrugineumWedd., is reported here. Although flavokawin B is widespread, this is the first report about its trypanocidal properties on bothTrypanosoma cruzi(IC50= 9.5 µM, IC50= 34.7 µM benznidazol, Y strain) epimastigotes andTrypanosoma brucei(IC50= 4.8 µM, IC50= 6.4 µM pentamidine, 29-13 strain) procyclic forms, which was also corroborated onT. bruceistrain 427 (IC50= 6.2 µM). In order to learn more about its properties, unspecific cytotoxicity on Hep G2 cells was investigated as well as thetrans-splicing inhibitory potential onT. bruceicells. 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.
authors.affiliation: Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil.
authors.forename: Danilo F
authors.initials: DF
authors.lastname: Rodrigues
authors.affiliation: Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina.
authors.forename: David A
authors.initials: DA
authors.lastname: Maniscalco
authors.affiliation: Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil.
authors.forename: Flavia A J
authors.initials: FA
authors.lastname: Silva
authors.affiliation: Department of Drugs and Medicaments, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil.
authors.forename: Bruna G
authors.initials: BG
authors.lastname: Chiari
authors.affiliation: Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina.
authors.forename: María V
authors.initials: MV
authors.lastname: Castelli
authors.affiliation: Department of Drugs and Medicaments, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil.
authors.forename: Vera L B
authors.initials: VL
authors.lastname: Isaac
authors.affiliation: Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil.
authors.forename: Regina M B
authors.initials: RM
authors.lastname: Cicarelli
authors.affiliation: Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina.
authors.forename: Silvia N
authors.initials: SN
authors.lastname: López
mesh_terms: D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D028502:Polygonum / Q000737:chemistry; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000235:genetics; D014349:Trypanosoma cruzi / Q000187:drug effects*; D014352:Trypanosomiasis / Q000188:drug therapy*; D014353:Trypanosomiasis, African / Q000188:drug therapy
chemical_list: D005419:Flavonoids; D014344:Trypanocidal Agents; C452039:flavokawain B; D002599:Chalcone