TY - JOUR
T1 - Antigiardial Activity of Podophyllotoxin-Type Lignans from Bursera fagaroides var. Fagaroides
AU - Gutiérrez-Gutiérrez, Filiberto
AU - Puebla-Pérez, Ana María
AU - González-Pozos, Sirenia
AU - Hernández-Hernández, José Manuel
AU - Pérez-Rangel, Armando
AU - Alvarez, Laura Patricia
AU - Tapia-Pastrana, Gabriela
AU - Castillo-Romero, Araceli
PY - 2017/5
Y1 - 2017/5
N2 - 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, 50-desmethoxy-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.
AB - 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, 50-desmethoxy-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.
KW - Antiprotozoal activity
KW - Bursera fagaroides
KW - Giardia lamblia
KW - Lignans
UR - http://www.scopus.com/inward/record.url?scp=85020229790&partnerID=8YFLogxK
U2 - 10.3390/molecules22050799
DO - 10.3390/molecules22050799
M3 - Artículo
C2 - 28505094
AN - SCOPUS:85020229790
SN - 1420-3049
VL - 22
JO - Molecules
JF - Molecules
IS - 5
M1 - 799
ER -
