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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.
Highlights
Giardia lamblia is one of the most ancient eukaryotes known
Treatment with 2 μM APOD resulted in cell viability of 45%, suggesting that APOD is more active against Giardia trophozoites
Drugs commonly used in the treatment of giardiasis produce different results as to their effectiveness, and all of them have undesirable side effects [6,7,8,9]
Summary
It is a flagellated protozoan parasite that infects the small intestine of humans and other mammals producing the diarrheal disease giardiasis [1]. Several drugs are available for treatment; all of them present variable efficacies and undesirable side effects [6,7,8,9], and some strains of Giardia have shown resistance towards common drugs. For these reasons, the search for new therapies with fewer side effects and better effectiveness is of great significance. Podophyllotoxin, an Molecules 2017, 22, 799; doi:10.3390/molecules22050799 www.mdpi.com/journal/molecules
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