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

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  • معلومة اضافية
    • بيانات النشر:
      Elsevier
    • Collection:
      CONICET Digital (Consejo Nacional de Investigaciones Científicas y Técnicas)
    • نبذة مختصرة :
      The 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. ; Fil: Lozano, Esteban Sebastián. Consejo Nacional de Investigaciones Cienti­ficas y Tecnicas. Centro Cientifico Tecnologico Mendoza. Instituto Histologia y Embriologia de Mendoza "Dr. M. Burgos"; Argentina ; Fil: Spina Zapata, Renata María. Consejo Nacional de Investigaciones Cienti­ficas y Tecnicas. Centro Cientifico Tecnologico Mendoza. Instituto Histologia y Embriologia de Mendoza "Dr. M. Burgos"; Argentina ; Fil: Tonn, Carlos Eugenio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico San Luis. Instituto de Investigaciones en Tecnología Química; Argentina ; Fil: Sosa Escudero, Miguel Angel. Consejo Nacional de Investigaciones Cienti­ficas y Tecnicas. Centro Cientifico Tecnologico Mendoza. Instituto Histologia y Embriologia de Mendoza "Dr. M. Burgos"; Argentina ; Fil: Cifuente, Diego Alberto. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico San Luis. Instituto de ...
    • File Description:
      application/pdf
    • ISSN:
      0960-894X
    • Relation:
      info:eu-repo/semantics/altIdentifier/url/http://www.sciencedirect.com/science/article/pii/S0960894X15301906; info:eu-repo/semantics/altIdentifier/doi/; http://hdl.handle.net/11336/5820; Lozano, 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
    • Rights:
      info:eu-repo/semantics/openAccess ; https://creativecommons.org/licenses/by-nc-nd/2.5/ar/
    • الرقم المعرف:
      edsbas.89D013AE