An abietane diterpene from Salvia cuspidata and some new derivatives are active against Trypanosoma cruzi

dc.creatorLozano, Esteban Sebastián
dc.creatorSpina Zapata, Renata María
dc.creatorTonn, Carlos Eugenio
dc.creatorSosa Escudero, Miguel Angel
dc.creatorCifuente, Diego Alberto
dc.date.accessioned2016-05-24T19:05:21Z
dc.date.accessioned2018-11-06T15:28:10Z
dc.date.available2016-05-24T19:05:21Z
dc.date.available2018-11-06T15:28:10Z
dc.date.created2016-05-24T19:05:21Z
dc.date.issued2015-10
dc.identifierLozano, Esteban Sebastián; Spina Zapata, Renata María; Tonn, Carlos Eugenio; Sosa Escudero, Miguel Angel; Cifuente, Diego Alberto; An abietane diterpene from Salvia cuspidata and some new derivatives are active against Trypanosoma cruzi; Elsevier; Bioorganic & Medicinal Chemistry Letters; 25; 23; 10-2015; 5481-5484
dc.identifier0960-894X
dc.identifierhttp://hdl.handle.net/11336/5820
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1897487
dc.description.abstractThe Plant Kingdom is an excellent source for obtaining natural compounds with antiprotozoal activity. In the present work, we studied the effect of the diterpene 12-hydroxy-11,14-diketo-6,8,12-abietatrien-19,20-olide (HABTO) obtained from the aerial parts of Salvia cuspidata on Trypanosoma cruzi epimastigotes.This compound was found to inhibit parasite growth even at low concentrations (IC50 5 lg/mL) and with low toxicity on mammalian cells. In addition, this diterpene induced an intense vacuolization within the parasites. In order to obtain analogs with greater lipophilicity, chemical modifications on the enol moiety were carried out to obtain the acetyl (AABTO), the sylil (SABTO) and the allyl (ALLABTO) derivatives. We observed that the SABTO was the most effective one on the parasites, and the effect could be attributed to a greater lipophilicity of this compound. Taking into account these datawe conclude that the increase of lipophilicity by chemical modifications is an adequate strategy for improving the trypanocidal activity of this kind abietane diterpenes.
dc.languageeng
dc.publisherElsevier
dc.relationinfo:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X15301906
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1016/j.bmcl.2015.10.082
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.bmcl.2015.10.082
dc.rightshttps://creativecommons.org/licenses/by-nc-nd/2.5/ar/
dc.rightsinfo:eu-repo/semantics/restrictedAccess
dc.subjectProductos naturales
dc.subjectditerpenos
dc.subjectTripanosoma cruzi
dc.subjectSalvia cuspidata
dc.titleAn abietane diterpene from Salvia cuspidata and some new derivatives are active against Trypanosoma cruzi
dc.typeArtículos de revistas
dc.typeArtículos de revistas
dc.typeArtículos de revistas


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