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Molecules 2017, 22(5), 799; doi:10.3390/molecules22050799

Antigiardial Activity of Podophyllotoxin-Type Lignans from Bursera fagaroides var. fagaroides

1
Departamento de Química y Farmacobiología, Universidad de Guadalajara, Guadalajara 44430, Jalisco, Mexico
2
Unidad de Microscopía Electrónica LaNSE, Centro de Investigación y Estudios Avanzados del Instituto Politécnico Nacional, Ciudad de México 07360, Mexico
3
Departamento de Biología Celular, Centro de Investigación y Estudios Avanzados del Instituto Politécnico Nacional, Ciudad de México 07360, Mexico
4
Centro de Investigaciones Químicas, Universidad Autónoma del Estado de Morelos, Morelos 62209, Mexico
5
Laboratorio de Investigación Biomédica, Hospital Regional de Alta Especialidad de Oaxaca, Oaxaca 71256, Mexico
6
Departamento de Microbiología y Patología, Universidad de Guadalajara, Guadalajara 44340, Jalisco, Mexico
*
Author to whom correspondence should be addressed.
Academic Editor: Thomas J. Schmidt
Received: 4 March 2017 / Revised: 8 May 2017 / Accepted: 9 May 2017 / Published: 13 May 2017
(This article belongs to the Section Natural Products)
View Full-Text   |   Download PDF [4021 KB, uploaded 13 May 2017]   |  

Abstract

Giardiasis, a diarrheal disease, is highly prevalent in developing countries. Several drugs are available for the treatment of this parasitosis; unfortunately, all of them have variable efficacies and adverse effects. Bursera fagaroides has been known for its anti-inflammatory and antidiarrheal properties in Mexican traditional medicine. We investigated the in vitro anti-giardial activities of four podophyllotoxin-type lignans from Bursera fagaroides var. fagaroides, namely, 5′-desmethoxy-β-peltatin-A-methylether (5-DES), acetylpodophyllotoxin (APOD), burseranin (BUR), and podophyllotoxin (POD). All lignans affected the Giardia adhesion and electron microscopy images revealed morphological alterations in the caudal region, ventral disk, membrane, and flagella, to different extents. Only 5-DES, APOD, and POD caused growth inhibition. Using the Caco-2 human cell line as a model of the intestinal epithelium, we demonstrated that APOD displayed direct antigiardial killing activity and low toxicity on Caco-2 cells. This finding makes it an attractive potential starting point for new antigiardial drugs. View Full-Text
Keywords: Bursera fagaroides; lignans; antiprotozoal activity; Giardia lamblia Bursera fagaroides; lignans; antiprotozoal activity; Giardia lamblia
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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).

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MDPI and ACS Style

Gutiérrez-Gutiérrez, F.; Puebla-Pérez, A.M.; González-Pozos, S.; Hernández-Hernández, J.M.; Pérez-Rangel, A.; Alvarez, L.P.; Tapia-Pastrana, G.; Castillo-Romero, A. Antigiardial Activity of Podophyllotoxin-Type Lignans from Bursera fagaroides var. fagaroides. Molecules 2017, 22, 799.

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