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

• Published in: Molecules (Basel, Switzerland) Vol. 22; no. 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: Journal Article
• Language: English
• Published: Switzerland MDPI AG 13.05.2017; MDPI
• 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; Giardia lamblia; Bursera fagaroides; antiprotozoal activity; lignans
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules22050799

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.