Identification of compounds responsible for the anthelmintic effects of chicory (Cichorium intybus) by molecular networking and bio-guided fractionation

Abstract

Increasing resistance towards anthelmintic drugs has necessitated the search for alternative treatments for the control of gastrointestinal nematode parasites. Animals fed on chicory ( Cichorium intybus L.), a temperate (pasture) crop, have reduced parasite burdens, hence making C. intybus a potentially useful source for novel anthelmintic compounds or a diet-based preventive/therapeutic option. Here, we utilized in vitro bioassays with the parasitic nematode Ascaris suum and molecular networking techniques with five chicory cultivars to identify putative active compounds. Network analysis predicted sesquiterpene lactones (SL) as the most likely group of anthelmintic compounds. Further bioassay-guided fractionation supported these predictions, and isolation of pure compounds demonstrated that the SL 8-deoxylactucin (8-DOL) is the compound most strongly associated with anti-parasitic activity. Furthermore, we showed that 8-DOL acts in a synergistic combination with other SL to exert the anti-parasitic effects. Finally, we established that chicory-derived extracts also showed activity against two ruminant nematodes ( Teladorsagia circumcincta and Cooperia oncophora ) in in vitro assays. Collectively, our results confirm the anti-parasitic activity of chicory against a range of nematodes, and pave the way for targeted extraction of active compounds or selective breeding of specific cultivars to optimize its future use in human and veterinary medicine.

Anthelmintic Properties of Essential Oils to Control Gastrointestinal Nematodes in Sheep—In Vitro and In Vivo Studies

“…As discussed earlier, the anthelmintic activity of EOs originates from their rich chemical composition and many bioactive ingredients belonging to different chemical classes [50]. However, ingredients of EOs can significantly differ in their degree of anthelmintic activity [15], suggesting the importance of compounds present in EOs and their percentages.…”

Anti-protozoal activity and metabolomic analyses of Cichorium intybus L. against Trypanosoma cruzi

“…Leaf and root fresh material from five different C. intybus cultivars was used for preparation of purified extracts, evaluation of anti-protozoal and cytotoxicity activities and metabolomic analyses. The sources of plant material, sample collection and preparation of purified extracts are described in details in Valente et al (2021) . Briefly, fresh leaves and roots were collected from four industrial C. intybus cultivars grown by Sensus B.V. (Roosendaal, The Netherlands): cultivar (cv.)…”

“…Previous in vitro studies have reported that SL-rich C. intybus extracts can induce potent anthelmintic effects against parasitic nematodes ( Foster et al, 2011 ; Peña-Espinoza et al, 2015 , 2017 , 2020 ; Williams et al, 2016 ). Recently, the anthelmintic activity of pure SL from C. intybus against parasitic nematodes has been confirmed by molecular networking and bioactivity-guided fractionation ( Valente et al, 2021 ). Nevertheless, little is known about the potential of C. intybus and its bioactive compounds against other major pathogens of medical or veterinary importance, such as protozoan parasites.…”

Dietary non-starch polysaccharides impair immunity to enteric nematode infection

“…Notably, grazing animals fed chicory have less worms [17,18], an effect that we recently showed derives from the direct anti-parasitic properties of SL found within the plant [19]. Thus, nutraceuticals based on chicory leaves may hold great promise for reducing inflammation, promoting a healthy GM, and limiting enteric pathogens.…”