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

作者：Gutierrez Gutierrez Filiberto; Maria Puebla Perez Ana; Gonzalez Pozos Sirenia; Manuel Hernandez Hernandez Jose; Perez Rangel Armando; Patricia Alvarez Laura; Tapia Pastrana Gabriela; Castillo Romero Araceli

来源：Molecules, 2017, 22(5): 799.

DOI：10.3390/molecules22050799

• Bursera fagaroides
• lignans
• antiprotozoal activity
• Giardia lamblia

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-beta-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.

• 出版日期2017-5