Next Article in Journal
Identification of a Recombinant Human Interleukin-12 (rhIL-12) Fragment in Non-Reduced SDS-PAGE
Next Article in Special Issue
In-Vitro Evaluation of 52 Commercially-Available Essential Oils Against Leishmania amazonensis
Previous Article in Journal
Characterization of a New DyP-Peroxidase from the Alkaliphilic Cellulomonad, Cellulomonas bogoriensis
Previous Article in Special Issue
Antitrypanosomal Activity of Sesquiterpene Lactones from Helianthus tuberosus L. Including a New Furanoheliangolide with an Unusual Structure
Article Menu
Issue 7 (April-1) cover image

Export Article

Open AccessArticle

Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis

1
CONICET—Universidad de Buenos Aires, Instituto de Química y Metabolismo del Fármaco (IQUIMEFA), Junín 956 2° floor, Buenos Aires 1113, Argentina
2
Cátedra de Farmacognosia, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956 2° floor, Buenos Aires 1113, Argentina
3
Instituto de Fisiología Animal, Fundación Miguel Lillo and Facultad de Ciencias Naturales e Instituto Miguel Lillo, Universidad Nacional de Tucumán, Tucumán T4000INI, Argentina
4
CONICET—Universidad Nacional de Luján, Instituto de Ecología y Desarrollo Sustentable (INEDES), Ruta 5 y Avenida Constitución, Luján 6700, Argentina
5
Cátedra de Inmunología, Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Junín 956 4° floor, Buenos Aires 1113, Argentina
6
Instituto de Estudios de la Inmunidad Humoral (IDEHU), UBA-CONICET, Junín 956 4° floor, Buenos Aires 1113, Argentina
7
CONICET—Universidad de Buenos Aires, Instituto de Microbiología y Parasitología Médica—CONICET (IMPaM), Facultad de Medicina, Paraguay 2155. 13° floor, Buenos Aires C1121ABG, Argentina
8
CONICET—Centro de Referencia para Lactobacilos (CERELA), Batalla de Chacabuco 145, San Miguel de Tucumán T4000INI, Argentina
9
CONICET—Universidad Nacional de Tucumán, Instituto de Química del Noroeste—CONICET (INQUINOA), Ayacucho 471, San Miguel de Tucumán T4000INI, Argentina
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Molecules 2019, 24(7), 1209; https://doi.org/10.3390/molecules24071209
Received: 28 February 2019 / Revised: 22 March 2019 / Accepted: 25 March 2019 / Published: 28 March 2019
(This article belongs to the Special Issue Drug Discovery for Neglected Diseases)
  |  
PDF [1055 KB, uploaded 28 March 2019]
  |     |  

Abstract

Sesquiterpene lactones are naturally occurring compounds mainly found in the Asteraceae family. These types of plant metabolites display a wide range of biological activities, including antiprotozoal activity and are considered interesting structures for drug discovery. Four derivatives were synthesized from estafietin (1), isolated from Stevia alpina (Asteraceae): 11βH,13-dihydroestafietin (2), epoxyestafietin (3a and 3b), 11βH,13-methoxyestafietin, (4) and 11βH,13-cianoestafietin. The antiprotozoal activity against Trypanosoma cruzi and Leishmania braziliensis of these compounds was evaluated. Epoxyestafietin was the most active compound against T. cruzi trypomastigotes and amastigotes (IC50 values of 18.7 and 2.0 µg/mL, respectively). Estafietin (1) and 11βH,13-dihydroestafietin (2) were the most active and selective compounds on L. braziliensis promastigotes (IC50 values of 1.0 and 1.3 μg/mL, respectively). The antiparasitic activity demonstrated by estafietin and some of its derivatives make them promising candidates for the development of effective compounds for the treatment of Chagas disease and leihsmaniasis. View Full-Text
Keywords: sesquiterpene lactones; Stevia alpina; Trypanosoma cruzi; Leishmania braziliensis sesquiterpene lactones; Stevia alpina; Trypanosoma cruzi; Leishmania braziliensis
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Sülsen, V.P.; Lizarraga, E.F.; Elso, O.G.; Cerny, N.; Sanchez Alberti, A.; Bivona, A.E.; Malchiodi, E.L.; Cazorla, S.I.; Catalán, C.A.N. Activity of Estafietin and Analogues on Trypanosoma cruzi and Leishmania braziliensis. Molecules 2019, 24, 1209.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top