Salvadoran Celastraceae Species as a Source of Antikinetoplastid Quinonemethide Triterpenoids

Author:

Núñez Marvin J.1ORCID,Martínez Morena L.1ORCID,Castillo Ulises G.1ORCID,Flores Karla Carolina1,Menjívar Jenny2,López-Arencibia Atteneri345ORCID,Bethencourt-Estrella Carlos J.3ORCID,Jiménez Ignacio A.6ORCID,Piñero José E.345ORCID,Lorenzo-Morales Jacob345,Bazzocchi Isabel L.6

Affiliation:

1. Laboratorio de Investigación en Productos Naturales (LIPN), Facultad de Química y Farmacia, Universidad de El Salvador, Final Ave. Mártires Estudiantes del 30 de Julio, San Salvador 01101, El Salvador

2. Museo de Historia Natural de El Salvador, Ministerio de Cultura, Final Calle Los Viveros, Col. Nicaragua, San Salvador 01101, El Salvador

3. Instituto Universitario de Enfermedades Tropicales y Salud Pública de Canarias, Universidad de La Laguna, 38200 La Laguna, Tenerife, Spain

4. Departamento de Obstetricia y Ginecología, Pediatría, Medicina Preventiva y Salud Pública, Toxicología, Medicina Legal y Forense y Parasitología, Universidad de La Laguna, 38200 La Laguna, Tenerife, Spain

5. Centro de Investigación Biomédica en Red de Enfermedades Infecciosas (CIBERINFEC), Instituto de Salud Carlos III, 28220 Madrid, Spain

6. Departamento de Química Orgánica, Instituto Universitario de Bio-Orgánica Antonio González, Universidad de La Laguna, Avenida Astrofísico Francisco Sánchez 2, 38206 La Laguna, Tenerife, Spain

Abstract

Chagas disease and leishmaniasis are among the most widespread neglected tropical diseases, and their current therapies have limited efficacy and several toxic side effects. The present study reports the chemical and antikinetoplastid profiles of extracts from five Salvadoran Celastraceae species against the Trypanosoma cruzi epimastigotes stage and Leishmania amazonensis and Leishmania donovani promastigote forms. The phytochemical profile evinced the presence of flavonoids, tannins, sterols, and triterpenes as the main components in all plant species, whereas quinonemethide triterpenoids (QMTs) were restricted to the root bark of the studied species. Antikinetoplastid evaluation highlights the root bark extracts from Zinowewia integerrima, Maytenus segoviarum, and Quetzalia ilicina as the most promising ones, exhibiting higher potency against T. cruzi (IC50 0.71–1.58 µg/mL) and L. amazonensis (IC50 0.38–2.05 µg/mL) than the reference drugs, benznidazole (IC50 1.81 µg/mL) and miltefosine (IC50 2.64 µg/mL), respectively. This potent activity was connected with an excellent selectivity index on the murine macrophage J774A.1 cell line. These findings reinforce the potential of QMTs as antikinetoplastid agents for the development of innovative phytopharmaceuticals and the plant species under study as a source of these promising lead compounds.

Funder

Consorcio Centro de Investigación Biomédica en Red (CIBER) de Enfermedades Infecciosas (CI-BERINFEC), Instituto de Salud Carlos III, Madrid, Spain

Publisher

MDPI AG

Subject

Plant Science,Ecology,Ecology, Evolution, Behavior and Systematics

Reference51 articles.

1. World Health Organization (2023, February 03). WHO Neglected Tropical Diseases. Available online: http://www.emro.who.int/health-topics/tropical-diseases/.

2. Leishmaniasis and Chagas disease-neglected tropical diseases: Treatment updates;Sangenito;Curr. Top. Med Chem.,2019

3. World Health Organization (2023, February 03). WHO Chagas Disease (American Trypanosomiasis). Available online: https://www.who.int/health-topics/chagas-disease.

4. Centers for Disease Control and Prevention (2023, February 03). Leishmaniasis-Epidemiology & Risk Factors, Available online: https://www.cdc.gov/parasites/leishmaniasis/epi.html.

5. World Health Organization (2023, February 03). WHO Leishmaniasis. Available online: https://www.who.int/news-room/fact-sheets/detail/leishmaniasis.

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