Biochemistry & Pharmacology: Open Access
Open Access
ISSN: 2167-0501
+44-77-2385-9429
ISSN: 2167-0501
+44-77-2385-9429
Mariana G Selener, Augusto Bivona, Natacha Cerny, Andres Sanchez Alberti, Emilio Malchiodi, Flavia Redko, Valeria P. Sulsen and Cesar Catalan
University of Buenos Aires, Argentina
National University of Tucuman, Argentina
Scientific Tracks Abstracts: Biochem Pharmacol (Los Angel)
Chagas disease is a parasitic disease caused by the protozoan Trypanosoma cruzi. According to the World Health Organization
(WHO) this parasitosis affects 6-7 million people worldwide. In Argentina it is estimated that approximately 1.5 million
people are infected. The current available drugs used for its treatment, nifurtimox and benznidazole, have limitations due to host
toxicity, side effects and low efficacy. In this context, it is extremely necessary to develop new drugs. Nature has provided useful
drugs that are used nowadays to treat different pains. Asteraceae species have been a rich source of active compounds and have
been attractive for drug discovery. In previous work the trypanocidal activity of the dichloromethane extract of Gymnocoronis
spilanthoides (Asteraceae) [GSDE] has been demonstrated. The aim of this investigation was to isolate and identified the active
compounds present in GSDE. GSDE was purified by liquid-liquid partition and fractionated by column chromatography using
Silicagel-60 and a gradient of CH2Cl2 and EtoAc. From fractions eluted with CH2Cl2: EtoAc (2:1) a pure compound was isolated
(compound A). The GSDE as well as compound A were analyzed by HPLC (C18 column, linear gradient elution mode and
UV/Vis absorbance detector). The structure elucidation of the isolated compound was performed by spectroscopic methods.
The trypanocidal activity of compound A was evaluated on T. cruzi epimastigotes (RA) by the [3H]-thymidine uptake assay.
The cytotoxicity of this compound on mammalian cells was performed using mouse splenocytes. Compound A presented a
significant trypanocidal activity (IC50= 1.6 �¼g/ml). This compound showed some toxicity to mammalian cells (CC50=4.9 �¼g/
ml). The compound A presented 98% purity (by HPLC) and was identified as the ent-11�±-hydroxy-15-oxokaur-16-en-19-oic
acid. The trypanocidal activity of ent-11�±-hydroxy-15-oxokaur-16-en-19-oic acid on trypomastigote and amastigote forms
will be evaluated. We will also continue with the isolation and identification of other compounds present in the active extract.
Recent Publications
1. World Health Organization (2018) Fact sheet Chagas disease (American trypanosomiasis). http://www.who.int/mediacentre/
factsheets/fs340/en/. Accessed April 2018.
2. S�¼lsen V, et al. (2013) Natural terpenoids from Ambrosia species are active in vitro and in vivo against human pathogenic
trypanosomatids. PLoSNegl Trop Dis. 7(10):e2494.
3. Herz W and Sharma R (1976) New hydroxylatedent-kauranoic acids from Eupatorium album. J. Org. Chem., 41(6):1021-1026.
Mariana G Selener has completed her Bachelor degree in Pharmacy in the Faculty of Pharmacy and Biochemistry at University of Buenos Aires (UBA) in 2011. She is pursuing her PhD at Chair of Pharmacognosy at the same University. She has expertise in analytical development. The aim of her PhD research work is the isolation and identification of bioactive compounds from Argentine Asteraceae species. She is an Assistant at the Chair of Pharmacognosy at the Faculty of Pharmacy and Biochemistry, University of Buenos Aires (UBA) for undergraduate courses.
E-mail: mgsmarian@gmail.com