Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies
Species of Picramnia genus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition. P. gracilis Tul. is a native species from Central and South America and although its fruits are edible, phytochemical anal...
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| Format: | Article |
| Language: | English |
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Wiley
2015-01-01
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| Series: | Advances in Pharmacological Sciences |
| Online Access: | http://dx.doi.org/10.1155/2015/978379 |
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| author | Sara M. Robledo Wilson Cardona Karen Ligardo Jéssica Henao Natalia Arbeláez Andrés Montoya Fernando Alzate Juan M. Pérez Victor Arango Iván D. Vélez Jairo Sáez |
| author_facet | Sara M. Robledo Wilson Cardona Karen Ligardo Jéssica Henao Natalia Arbeláez Andrés Montoya Fernando Alzate Juan M. Pérez Victor Arango Iván D. Vélez Jairo Sáez |
| author_sort | Sara M. Robledo |
| collection | DOAJ |
| description | Species of Picramnia genus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition. P. gracilis Tul. is a native species from Central and South America and although its fruits are edible, phytochemical analysis or medicinal uses of this species are not known. In the search of candidates to antileishmanial drugs, this work aimed to evaluate the antileishmanial activity of P. gracilis Tul. in in vitro and in vivo studies. Only ethanolic extract of fruits showed leishmanicidal activity. The majoritarian metabolite was 5,3′-hydroxy-7,4′-dimethoxyflavanone ether that exhibited high activity against L. (V.) panamensis (EC50 17.0 + 2.8 mg/mL, 53.7 μM) and low toxicity on mammalian U-937 cells, with an index of selectivity >11.8. In vivo studies showed that the flavanone administered in solution (2 mg/kg/day) or cream (2%) induces clinical improvement and no toxicity in hamsters with CL. In conclusion, this is the first report about isolation of 5,3′-hydroxy-7,4′-dimethoxyflavanone of P. gracilis Tul. The leishmanicidal activity attributed to this flavanone is also reported for the first time. Finally, the in vitro and in vivo leishmanicidal activity reported here for 5,3′-hydroxy-7,4′-dimethoxyflavanone offers a greater prospect towards antileishmanial drug discovery and development. |
| format | Article |
| id | doaj-art-7e01b9c7e41e447b95b11c5c3d7a62bc |
| institution | Kabale University |
| issn | 1687-6334 1687-6342 |
| language | English |
| publishDate | 2015-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Advances in Pharmacological Sciences |
| spelling | doaj-art-7e01b9c7e41e447b95b11c5c3d7a62bc2025-02-03T01:02:52ZengWileyAdvances in Pharmacological Sciences1687-63341687-63422015-01-01201510.1155/2015/978379978379Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo StudiesSara M. Robledo0Wilson Cardona1Karen Ligardo2Jéssica Henao3Natalia Arbeláez4Andrés Montoya5Fernando Alzate6Juan M. Pérez7Victor Arango8Iván D. Vélez9Jairo Sáez10PECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaChemistry of Colombian Plants, Institute of Chemistry, Exact and Natural Sciences School, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaBotanical Studies, Institute of Biology, Exact and Natural Sciences School, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaChemistry of Colombian Plants, Institute of Chemistry, Exact and Natural Sciences School, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPharmacy School, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaPECET, Medical Research Institute, School of Medicine, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaChemistry of Colombian Plants, Institute of Chemistry, Exact and Natural Sciences School, University of Antioquia (UdeA), Calle 70, No. 52-21, A.A. 1226, Medellín, ColombiaSpecies of Picramnia genus are used in folk medicine to treat or prevent skin disorders, but only few species have been studied for biological activity and chemical composition. P. gracilis Tul. is a native species from Central and South America and although its fruits are edible, phytochemical analysis or medicinal uses of this species are not known. In the search of candidates to antileishmanial drugs, this work aimed to evaluate the antileishmanial activity of P. gracilis Tul. in in vitro and in vivo studies. Only ethanolic extract of fruits showed leishmanicidal activity. The majoritarian metabolite was 5,3′-hydroxy-7,4′-dimethoxyflavanone ether that exhibited high activity against L. (V.) panamensis (EC50 17.0 + 2.8 mg/mL, 53.7 μM) and low toxicity on mammalian U-937 cells, with an index of selectivity >11.8. In vivo studies showed that the flavanone administered in solution (2 mg/kg/day) or cream (2%) induces clinical improvement and no toxicity in hamsters with CL. In conclusion, this is the first report about isolation of 5,3′-hydroxy-7,4′-dimethoxyflavanone of P. gracilis Tul. The leishmanicidal activity attributed to this flavanone is also reported for the first time. Finally, the in vitro and in vivo leishmanicidal activity reported here for 5,3′-hydroxy-7,4′-dimethoxyflavanone offers a greater prospect towards antileishmanial drug discovery and development.http://dx.doi.org/10.1155/2015/978379 |
| spellingShingle | Sara M. Robledo Wilson Cardona Karen Ligardo Jéssica Henao Natalia Arbeláez Andrés Montoya Fernando Alzate Juan M. Pérez Victor Arango Iván D. Vélez Jairo Sáez Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies Advances in Pharmacological Sciences |
| title | Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
| title_full | Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
| title_fullStr | Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
| title_full_unstemmed | Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
| title_short | Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
| title_sort | antileishmanial effect of 5 3 hydroxy 7 4 dimethoxyflavanone of picramnia gracilis tul picramniaceae fruit in vitro and in vivo studies |
| url | http://dx.doi.org/10.1155/2015/978379 |
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