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Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. satureiifolia.
Pharm Biol. 2016 Oct; 54(10):2188-95.PB

Abstract

Context Chagas' disease and leishmaniasis produce significant disability and mortality with great social and economic impact. The genus Stevia (Asteraceae) is a potential source of antiprotozoal compounds. Objective Aerial parts of four Stevia species were screened on Trypanosoma cruzi. Stevia satureiifolia (Lam.) Sch. Bip. var. satureiifolia (Asteraceae) dichloromethane extract was selected for a bioassay-guided fractionation in order to isolate its active compounds. Additionally, the antileishmanial activity and the cytotoxicity of these compounds on mammalian cells were assessed. Materials and methods The dichloromethane extract was fractionated by column chromatography. The isolated compounds were evaluated using concentrations of 0-100 μg/mL on T. cruzi epimastigotes and on Leishmania braziliensis promastigotes for 72 h, on trypomastigotes and amastigotes of T. cruzi for 24 h and 120 h, respectively. The compounds' cytotoxicity (12.5-500 μg/mL) was assessed on Vero cells by the MTT assay. The structure elucidation of each compound was performed by spectroscopic methods and HPLC analysis. Results The dichloromethane extracts of Stevia species showed significant activity on T. cruzi epimastigotes. The flavonoids eupatorin (1.3%), cirsimaritin (1.9%) and 5-desmethylsinensetin (1.5%) were isolated from S. satureiifolia var. satureiifolia extract. Eupatorin and 5-desmethylsinensetin showed IC50 values of 0.2 and 0.4 μg/mL on T. cruzi epimastigotes and 61.8 and 75.1 μg/mL on trypomastigotes, respectively. The flavonoid 5-desmethylsinensetin showed moderate activity against T. cruzi amastigotes (IC50 value = 78.7 μg/mL) and was the most active compound on L. braziliensis promastigotes (IC50 value = 37.0 μg/mL). Neither of the flavonoids showed cytotoxicity on Vero cells, up to a concentration of 500 μg/mL.

Authors+Show Affiliations

a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ; b Instituto de Tecnología Química (INTEQUI-CONICET) , Universidad Nacional de San Luis , San Luis , Argentina ;c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ; d Instituto de Microbiología y Parasitología Médica (IMPaM) (UBA-CONICET) , Facultad de Medicina , Buenos Aires , Argentina ;a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ; c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ;c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ; d Instituto de Microbiología y Parasitología Médica (IMPaM) (UBA-CONICET) , Facultad de Medicina , Buenos Aires , Argentina ;c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ; d Instituto de Microbiología y Parasitología Médica (IMPaM) (UBA-CONICET) , Facultad de Medicina , Buenos Aires , Argentina ;a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ;c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ; d Instituto de Microbiología y Parasitología Médica (IMPaM) (UBA-CONICET) , Facultad de Medicina , Buenos Aires , Argentina ;a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ; e Cátedra de Farmacognosia, Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina.a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ;a Instituto de Química y Metabolismo del Fármaco (IQUIMEFA) (UBA-CONICET), Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina ; e Cátedra de Farmacognosia, Facultad de Farmacia y Bioquímica , Universidad de Buenos Aires , Buenos Aires , Argentina.c Cátedra de Inmunología, Instituto de Estudios de la Inmunidad Humoral (IDEHU) (UBA-CONICET) , Facultad de Farmacia y Bioquímica , Buenos Aires , Argentina ; d Instituto de Microbiología y Parasitología Médica (IMPaM) (UBA-CONICET) , Facultad de Medicina , Buenos Aires , Argentina ;

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

26983579

Citation

Beer, María Florencia, et al. "Trypanocidal and Leishmanicidal Activities of Flavonoids Isolated From Stevia Satureiifolia Var. Satureiifolia." Pharmaceutical Biology, vol. 54, no. 10, 2016, pp. 2188-95.
Beer MF, Frank FM, Germán Elso O, et al. Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. satureiifolia. Pharm Biol. 2016;54(10):2188-95.
Beer, M. F., Frank, F. M., Germán Elso, O., Ernesto Bivona, A., Cerny, N., Giberti, G., Luis Malchiodi, E., Susana Martino, V., Alonso, M. R., Patricia Sülsen, V., & Cazorla, S. I. (2016). Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. satureiifolia. Pharmaceutical Biology, 54(10), 2188-95. https://doi.org/10.3109/13880209.2016.1150304
Beer MF, et al. Trypanocidal and Leishmanicidal Activities of Flavonoids Isolated From Stevia Satureiifolia Var. Satureiifolia. Pharm Biol. 2016;54(10):2188-95. PubMed PMID: 26983579.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Trypanocidal and leishmanicidal activities of flavonoids isolated from Stevia satureiifolia var. satureiifolia. AU - Beer,María Florencia, AU - Frank,Fernanda Maria, AU - Germán Elso,Orlando, AU - Ernesto Bivona,Augusto, AU - Cerny,Natacha, AU - Giberti,Gustavo, AU - Luis Malchiodi,Emilio, AU - Susana Martino,Virginia, AU - Alonso,María Rosario, AU - Patricia Sülsen,Valeria, AU - Cazorla,Silvia Ines, Y1 - 2016/03/17/ PY - 2016/3/18/entrez PY - 2016/3/18/pubmed PY - 2017/2/9/medline KW - Leishmania braziliensis KW - phenolic compounds; Stevia spp.; Trypanosoma cruzi SP - 2188 EP - 95 JF - Pharmaceutical biology JO - Pharm Biol VL - 54 IS - 10 N2 - Context Chagas' disease and leishmaniasis produce significant disability and mortality with great social and economic impact. The genus Stevia (Asteraceae) is a potential source of antiprotozoal compounds. Objective Aerial parts of four Stevia species were screened on Trypanosoma cruzi. Stevia satureiifolia (Lam.) Sch. Bip. var. satureiifolia (Asteraceae) dichloromethane extract was selected for a bioassay-guided fractionation in order to isolate its active compounds. Additionally, the antileishmanial activity and the cytotoxicity of these compounds on mammalian cells were assessed. Materials and methods The dichloromethane extract was fractionated by column chromatography. The isolated compounds were evaluated using concentrations of 0-100 μg/mL on T. cruzi epimastigotes and on Leishmania braziliensis promastigotes for 72 h, on trypomastigotes and amastigotes of T. cruzi for 24 h and 120 h, respectively. The compounds' cytotoxicity (12.5-500 μg/mL) was assessed on Vero cells by the MTT assay. The structure elucidation of each compound was performed by spectroscopic methods and HPLC analysis. Results The dichloromethane extracts of Stevia species showed significant activity on T. cruzi epimastigotes. The flavonoids eupatorin (1.3%), cirsimaritin (1.9%) and 5-desmethylsinensetin (1.5%) were isolated from S. satureiifolia var. satureiifolia extract. Eupatorin and 5-desmethylsinensetin showed IC50 values of 0.2 and 0.4 μg/mL on T. cruzi epimastigotes and 61.8 and 75.1 μg/mL on trypomastigotes, respectively. The flavonoid 5-desmethylsinensetin showed moderate activity against T. cruzi amastigotes (IC50 value = 78.7 μg/mL) and was the most active compound on L. braziliensis promastigotes (IC50 value = 37.0 μg/mL). Neither of the flavonoids showed cytotoxicity on Vero cells, up to a concentration of 500 μg/mL. SN - 1744-5116 UR - https://www.unboundmedicine.com/medline/citation/26983579/Trypanocidal_and_leishmanicidal_activities_of_flavonoids_isolated_from_Stevia_satureiifolia_var__satureiifolia_ L2 - http://www.tandfonline.com/doi/full/10.3109/13880209.2016.1150304 DB - PRIME DP - Unbound Medicine ER -