Psilostachyin C: a natural compound with trypanocidal activity
| Autor: | Silvia I. Cazorla, Roser Vila, Liliana Muschietti, Patricia Barrera, Fernanda M. Frank, Blanca Freixa, Valeria P. Sülsen, Miguel A. Sosa, Emilio L. Malchiodi, Virginia Martino |
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| Rok vydání: | 2011 |
| Předmět: |
Male
Microbiology (medical) Cell Survival medicine.drug_class Trypanosoma cruzi Leishmania mexicana Antiprotozoal Agents Biology Sesquiterpene lactone Cell Line Rodent Diseases Inhibitory Concentration 50 Mice Microscopy Electron Transmission In vivo parasitic diseases medicine Animals Humans Chagas Disease Pharmacology (medical) Amastigote Trypanocidal agent chemistry.chemical_classification Plant Extracts Biological activity General Medicine biology.organism_classification Molecular biology Disease Models Animal Treatment Outcome Infectious Diseases chemistry Biochemistry Antiprotozoal Evaluation of complex medical interventions Auto-immunity transplantation and immunotherapy [NCEBP 2] Female Ambrosia Sesquiterpenes |
| Zdroj: | International Journal of Antimicrobial Agents, 37, 6, pp. 536-43 International Journal of Antimicrobial Agents, 37, 536-43 |
| ISSN: | 0924-8579 |
| Popis: | Item does not contain fulltext In this study, the antiprotozoal activity of the sesquiterpene lactone psilostachyin C was investigated. This natural compound was isolated from Ambrosia scabra by bioassay-guided fractionation and was identified by spectroscopic techniques. Psilostachyin C exerted in vitro trypanocidal activity against Trypanosoma cruzi epimastigotes, trypomastigotes and amastigotes, with 50% inhibitory concentration (IC(50)) values of 0.6, 3.5 and 0.9 mug/mL, respectively, and displayed less cytotoxicity against mammalian cells, with a 50% cytotoxic concentration (CC(50)) of 87.5 mug/mL. Interestingly, this compound induced ultrastructural alterations, as seen by transmission electron microscopy, in which vacuolisation and a structural appearance resembling multivesicular bodies were observed even at a concentration as low as 0.2 mug/mL. In an in vivo assay, a significant reduction in the number of circulating parasites was found in T. cruzi-infected mice treated with psilostachyin C for 5 days compared with untreated mice (7.4 +/- 1.2 x 10(5)parasites/mL vs. 12.8 +/- 2.0 x 10(5)parasites/mL) at the peak of parasitaemia. According to these results, psilostachyin C may be considered a promising template for the design of novel trypanocidal agents. In addition, psilostachyin C inhibited the growth of Leishmania mexicana and Leishmania amazonensis promastigotes (IC(50)=1.2 mug/mL and 1.5 mug/mL, respectively). |
| Databáze: | OpenAIRE |
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