Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies
ABSTRACT: 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, phytoche...
- Autores:
-
Robledo Restrepo, Sara María
Cardona Galeano, Wilson
Ligardo Restrepo, Karen Patricia
Henao Peláez, Jéssica Natalia
Arbeláez Córdoba, Natalia
Montoya Cuervo, Edwin Andrés
Alzate Guarín, Fernando
Pérez Cardona, Juan Manuel
Arango Valencia, Víctor Hugo
Vélez Bernal, Iván Darío
Sáez Vega, Jairo Antonio
- Tipo de recurso:
- Article of investigation
- Fecha de publicación:
- 2015
- Institución:
- Universidad de Antioquia
- Repositorio:
- Repositorio UdeA
- Idioma:
- eng
- OAI Identifier:
- oai:bibliotecadigital.udea.edu.co:10495/22106
- Acceso en línea:
- http://hdl.handle.net/10495/22106
- Palabra clave:
- Enfermedades de la Piel
Skin Diseases
Leishmaniasis
Picramnia
- Rights
- openAccess
- License
- http://creativecommons.org/licenses/by/2.5/co/
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oai:bibliotecadigital.udea.edu.co:10495/22106 |
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|
dc.title.spa.fl_str_mv |
Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
title |
Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
spellingShingle |
Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies Enfermedades de la Piel Skin Diseases Leishmaniasis Picramnia |
title_short |
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_sort |
Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies |
dc.creator.fl_str_mv |
Robledo Restrepo, Sara María Cardona Galeano, Wilson Ligardo Restrepo, Karen Patricia Henao Peláez, Jéssica Natalia Arbeláez Córdoba, Natalia Montoya Cuervo, Edwin Andrés Alzate Guarín, Fernando Pérez Cardona, Juan Manuel Arango Valencia, Víctor Hugo Vélez Bernal, Iván Darío Sáez Vega, Jairo Antonio |
dc.contributor.author.none.fl_str_mv |
Robledo Restrepo, Sara María Cardona Galeano, Wilson Ligardo Restrepo, Karen Patricia Henao Peláez, Jéssica Natalia Arbeláez Córdoba, Natalia Montoya Cuervo, Edwin Andrés Alzate Guarín, Fernando Pérez Cardona, Juan Manuel Arango Valencia, Víctor Hugo Vélez Bernal, Iván Darío Sáez Vega, Jairo Antonio |
dc.subject.decs.none.fl_str_mv |
Enfermedades de la Piel Skin Diseases Leishmaniasis |
topic |
Enfermedades de la Piel Skin Diseases Leishmaniasis Picramnia |
dc.subject.proposal.spa.fl_str_mv |
Picramnia |
description |
ABSTRACT: 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. |
publishDate |
2015 |
dc.date.issued.none.fl_str_mv |
2015 |
dc.date.accessioned.none.fl_str_mv |
2021-09-03T02:17:55Z |
dc.date.available.none.fl_str_mv |
2021-09-03T02:17:55Z |
dc.type.spa.fl_str_mv |
info:eu-repo/semantics/article |
dc.type.coarversion.fl_str_mv |
http://purl.org/coar/version/c_970fb48d4fbd8a85 |
dc.type.hasversion.spa.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.coar.spa.fl_str_mv |
http://purl.org/coar/resource_type/c_2df8fbb1 |
dc.type.redcol.spa.fl_str_mv |
https://purl.org/redcol/resource_type/ART |
dc.type.local.spa.fl_str_mv |
Artículo de investigación |
format |
http://purl.org/coar/resource_type/c_2df8fbb1 |
status_str |
publishedVersion |
dc.identifier.citation.spa.fl_str_mv |
Robledo, S., Cardona, W., Ligardo, K., Henao, H., Arbeláez, N., Montoya, A., Alzate, F., Pérez, J., Arango, V., Vélez, I., Sáez, J. (2015). Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies. Advances in Pharmacological and Pharmaceutical Sciences, vol. 2015, 1-8. https://doi.org/10.1155/2015/978379 |
dc.identifier.issn.none.fl_str_mv |
1687-6334 |
dc.identifier.uri.none.fl_str_mv |
http://hdl.handle.net/10495/22106 |
dc.identifier.doi.none.fl_str_mv |
10.1155/2015/978379 |
dc.identifier.eissn.none.fl_str_mv |
1687-6342 |
identifier_str_mv |
Robledo, S., Cardona, W., Ligardo, K., Henao, H., Arbeláez, N., Montoya, A., Alzate, F., Pérez, J., Arango, V., Vélez, I., Sáez, J. (2015). Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies. Advances in Pharmacological and Pharmaceutical Sciences, vol. 2015, 1-8. https://doi.org/10.1155/2015/978379 1687-6334 10.1155/2015/978379 1687-6342 |
url |
http://hdl.handle.net/10495/22106 |
dc.language.iso.spa.fl_str_mv |
eng |
language |
eng |
dc.relation.ispartofjournalabbrev.spa.fl_str_mv |
Adv. Pharmacol. Sci. |
dc.rights.spa.fl_str_mv |
info:eu-repo/semantics/openAccess |
dc.rights.uri.*.fl_str_mv |
http://creativecommons.org/licenses/by/2.5/co/ |
dc.rights.accessrights.spa.fl_str_mv |
http://purl.org/coar/access_right/c_abf2 |
dc.rights.creativecommons.spa.fl_str_mv |
https://creativecommons.org/licenses/by/4.0/ |
eu_rights_str_mv |
openAccess |
rights_invalid_str_mv |
http://creativecommons.org/licenses/by/2.5/co/ http://purl.org/coar/access_right/c_abf2 https://creativecommons.org/licenses/by/4.0/ |
dc.format.extent.spa.fl_str_mv |
8 |
dc.format.mimetype.spa.fl_str_mv |
application/pdf |
dc.publisher.spa.fl_str_mv |
Hindawi |
dc.publisher.group.spa.fl_str_mv |
Grupo de Estudios Botánicos Programa de Estudio y Control de Enfermedades Tropicales (PECET) Química de Plantas Colombianas |
dc.publisher.place.spa.fl_str_mv |
Londres, Inglaterra |
institution |
Universidad de Antioquia |
bitstream.url.fl_str_mv |
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bitstream.checksumAlgorithm.fl_str_mv |
MD5 MD5 MD5 |
repository.name.fl_str_mv |
Repositorio Institucional Universidad de Antioquia |
repository.mail.fl_str_mv |
andres.perez@udea.edu.co |
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1812173160557051904 |
spelling |
Robledo Restrepo, Sara MaríaCardona Galeano, WilsonLigardo Restrepo, Karen PatriciaHenao Peláez, Jéssica NataliaArbeláez Córdoba, NataliaMontoya Cuervo, Edwin AndrésAlzate Guarín, FernandoPérez Cardona, Juan ManuelArango Valencia, Víctor HugoVélez Bernal, Iván DaríoSáez Vega, Jairo Antonio2021-09-03T02:17:55Z2021-09-03T02:17:55Z2015Robledo, S., Cardona, W., Ligardo, K., Henao, H., Arbeláez, N., Montoya, A., Alzate, F., Pérez, J., Arango, V., Vélez, I., Sáez, J. (2015). Antileishmanial Effect of 5,3′-Hydroxy-7,4′-dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo Studies. Advances in Pharmacological and Pharmaceutical Sciences, vol. 2015, 1-8. https://doi.org/10.1155/2015/9783791687-6334http://hdl.handle.net/10495/2210610.1155/2015/9783791687-6342ABSTRACT: 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.COL0015099COL0015329COL00082278application/pdfengHindawiGrupo de Estudios BotánicosPrograma de Estudio y Control de Enfermedades Tropicales (PECET)Química de Plantas ColombianasLondres, Inglaterrainfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://purl.org/coar/resource_type/c_2df8fbb1https://purl.org/redcol/resource_type/ARTArtículo de investigaciónhttp://purl.org/coar/version/c_970fb48d4fbd8a85info:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by/2.5/co/http://purl.org/coar/access_right/c_abf2https://creativecommons.org/licenses/by/4.0/Antileishmanial Effect of 5,3´ -Hydroxy-7,4´ -dimethoxyflavanone of Picramnia gracilis Tul. (Picramniaceae) Fruit: In Vitro and In Vivo StudiesEnfermedades de la PielSkin DiseasesLeishmaniasisPicramniaAdv. Pharmacol. Sci.Advances in Pharmacological Sciences182015CC-LICENSElicense_rdflicense_rdfapplication/rdf+xml; charset=utf-8927http://bibliotecadigital.udea.edu.co/bitstream/10495/22106/2/license_rdf1646d1f6b96dbbbc38035efc9239ac9cMD52ORIGINALRobledoSara_2015_AntileishmanialEffectPicramnia.pdfRobledoSara_2015_AntileishmanialEffectPicramnia.pdfArtículo de investigaciónapplication/pdf1370909http://bibliotecadigital.udea.edu.co/bitstream/10495/22106/1/RobledoSara_2015_AntileishmanialEffectPicramnia.pdf8abf93186501a3fadc3cda7a901c42f0MD51LICENSElicense.txtlicense.txttext/plain; charset=utf-81748http://bibliotecadigital.udea.edu.co/bitstream/10495/22106/3/license.txt8a4605be74aa9ea9d79846c1fba20a33MD5310495/22106oai:bibliotecadigital.udea.edu.co:10495/221062021-09-02 21:17:55.657Repositorio Institucional Universidad de Antioquiaandres.perez@udea.edu.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 |