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Planta Med 2017; 83(03/04): 239-244
DOI: 10.1055/s-0042-112031
Biological and Pharmacological Activity
Original Papers
Georg Thieme Verlag KG Stuttgart · New York

Trypanocidal Activity of Flavokawin B, a Component of Polygonum ferrugineum Wedd

Danilo F. Rodrigues
1   Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil
2   Institute of Chemistry, São Paulo State University, Araraquara, Brazil
,
David A. Maniscalco
3   Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina
,
Flavia A. J. Silva
1   Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil
,
Bruna G. Chiari
4   Department of Drugs and Medicaments, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil
,
María V. Castelli
3   Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina
,
Vera L. B. Isaac
4   Department of Drugs and Medicaments, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil
,
Regina M. B. Cicarelli
1   Department of Biological Sciences, School of Pharmaceutical Sciences of Araraquara, São Paulo State University, Araraquara, Brazil
2   Institute of Chemistry, São Paulo State University, Araraquara, Brazil
,
Silvia N. López
3   Universidad Nacional de Rosario, CONICET, Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Rosario, Argentina
› Author Affiliations
Further Information

Publication History

received 16 March 2016
revised 26 June 2016

accepted 05 July 2016

Publication Date:
21 July 2016 (online)

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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.

Key words

Trypanosoma cruzi - Trypanosoma brucei - flavokawin B - chalcone - trans-splicing - Polygonum ferrugineum - Polygonaceae
 

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