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

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. has been known for its anti-inflammatory and antidiarrheal properties in Mexican t...

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Published in:Molecules (Basel, Switzerland) Switzerland), 2017-05, Vol.22 (5), p.799
Main Authors: Gutiérrez-Gutiérrez, Filiberto, Puebla-Pérez, Ana María, González-Pozos, Sirenia, Hernández-Hernández, José Manuel, Pérez-Rangel, Armando, Alvarez, Laura Patricia, Tapia-Pastrana, Gabriela, Castillo-Romero, Araceli
Format: Article
Language:English
Subjects:
Adhesion
Antiprotozoal Agents - chemistry
Antiprotozoal Agents - pharmacology
Antiviral drugs
Bursera - chemistry
Caco-2 Cells
Cell growth
Cell Survival - drug effects
Developing countries
Diarrhea
Drug dosages
Drugs
Electron microscopy
Epithelium
Flagella
Giardiasis
Humans
In vitro methods and tests
Inflammation
Inhibition
Intestine
LDCs
Lignans
Microscopy
Morphology
Parasites
Plant Extracts - chemistry
Plant Extracts - pharmacology
Podophyllotoxin
Podophyllotoxin - chemistry
Podophyllotoxin - pharmacology
Protozoa
Side effects
Toxicity
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Summary: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. 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 var. , namely, 5'-desmethoxy-β-peltatin-A-methylether (5-DES), acetylpodophyllotoxin (APOD), burseranin (BUR), and podophyllotoxin (POD). All lignans affected the 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.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules22050799