The American Trypanosomiasis, also known as Chagas disease is caused by Trypanosoma cruzi, a protozoan of the Trypanosomatidae Family. It is a zoonotic endemic that affects approximately 6-8 million people generating health, economic and social problems in the affected countries and it is considered a neglected diseases making it not attractive for pharmaceutical industries. Currently available treatments use the drugs a nitrofurfurylidene-amino (Nifurtimox) and a nitroimidazole acetamide (Benznidazole). Both are not completely effective against the disease, for several reasons: on the one hand only serve during the acute stage of the disease, since they have low efficacy during the chronic phase, in the other hand these treatments have significant variations depending on the region, a consequence of the development of resistance to drugs by T. cruzi. To overcome these problems we are using natural products combined with nuclear magnetic resonance based metabolomic analysis. We could identify the responsible compound of the trypanosomicidal activity in Baccharis trimera, this being a diterpene of the labdane type containing an aldehyde, agreeing with results obtained by the group previously where metabolites of the same nature had been described with trypanosomicidal activity in Aristeguieta glutinosa. In the present work the Baccharis trimera fractionation oriented to verified the above compound is performed using gradient of polar disolvents extractions, and the biological activity of the fractions obtained in the process is monitored by in vitro assays in the epimastigote form of T. cruzi, Tulahuen 2 strain and the 1H NMR metabolomic characterization. The results obtained confirm that the ethyl acetate Baccharis trimera fraction has an important anti-T. cruzi, and besides that the aldehyde-diterpene is not the only metabolite present in the plant, so we can also infer that we are facing a synergistic effect.
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Search of Trypanosomicidal Active Principles by Metabolomic-guided Fractionation in Baccharis trimera
Published: 06 November 2017 by MDPI in 3rd International Electronic Conference on Medicinal Chemistry session Round Table on Parasitic Diseases